Anticancer Drugs Research Papers - Academia.edu (original) (raw)

BACKGROUND Colorectal cancer (CRC) or bowel cancer is one of the most important cancer diseases, needing serious attention. The cell surface receptor gene human epidermal growth factor receptor (EGFR) may have an important role in provoking CRC. In this pharmaceutical era, it is always attempted to identify plant-based drugs for cancer, which will have less side effects for human body, unlike the chemically synthesized marketed drugs having serious side effects. So, in this study the authors tried to assess the activity of two important plant compounds, ferulic acid (FA) and p-coumaric acid (pCA), on CRC. MATERIALS AND METHODS FA and pCA were tested for their cytotoxic effects on the human CRC cell line HCT 15 and also checked for the level of gene expression of EGFR by real time PCR analysis. Positive results were confirmed by in silico molecular docking studies using Discovery Studio (DS) 4.0. The drug parallel features of the same compounds were also assessed in silico. RESULTS C...

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- Chemistry, Medicine, Gene expression, Colorectal cancer

Two new ternary platinum(II) complexes of general formula [Pt(DTC)LCl], where DTC = 4-(2-pyridyl)piperazine-1-carbodithioate (1 and 2) and L = tri(p-tolyl)phosphine (1) and tri(o-tolyl)phosphine (2), have been synthesized and characterized. Both complexes have shown phenanthriplatin and picoplatin type axial protection, albeit from both sides, offered by CeH moiety of the organophosphine (X-ray single crystal and DFT analysis). Furthermore, 2 has shown greater degree of axial shielding of platinum center than 1. In vitro anticancer activity against three cancer cell lines has revealed greater anticancer potency of 2 than 1. The activity against NF-κB (a cancer promoting protein) signified that death of the cancer cells may be due to hindering the activity of NF-κB and subsequent initiation of the apoptosis. High activity of 2 than 1 can be attributed to its greater lipophilicity and stronger axial protection (CeH⋯Pt = 2.752 Å, HeC⋯Pt 3.496 Å, ∠H⋯Pt-P = 78.37°a nd ∠ C⋯Pt-P = 64.19°), from both sides of the axial plane, that may hinder the diversion to off target biomolecules and thus may enhance cellular uptake. Based upon DNA binding and DNA denaturing studies with CT-DNA, a cooperative binding and non-intercalative (electrostatic/covalent) mode of interaction have been suggested.

- by Zia-Ur-Rehman Qau
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- Coordination Chemistry, Anticancer Drugs

In breast cancer cells, overexpression of human epidermal growth factor receptor 2 (HER2) increases the translation of fatty acid synthase (FASN) by altering the activity of PI3K/Akt signaling pathways. Cancer chemotherapy causes major side effects and is not effective enough in slowing down the progression of the disease. Earlier studies showed a role for resveratrol in the inhibition of FASN, but the molecular mechanisms of resveratrol-induced inhibition are not known. In the present study, we examined the novel mechanism of resveratrol on Her2-overexpressed breast cancer cells.

- by Masood Khan
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- Anticancer Drugs

Anticancer activity of novel compound 4-(4-(3, 4-
dimethoxyphenyl) hexahydrofuro [3,4-c]furan-1-yl)-2-
methoxyphenyl acetate isolated from Pandanus
odoratissimus was studied against Ehrlich Ascites
Carcinoma (EAC) cells in Swiss albino mice. Anticancer
activity of compound was examined by determining the
body weight, average tumor weight, tumor cell volume, cell
count, viable, mean survival time, life span and
hematological studies. Treatment of mice with this phenolic
compound resulted in a cell growth inhibition by 75.02%,
63.36%, and 27.28% at doses of 50, 25, and 10 mg/kg (i.p.)
respectively. Standard drug Vinblastine at 0.5 mg/kg (i.p.)
exhibited maximum inhibition (86.12%). The tumor bearing
mice treated with the test compound at different doses
showed significant increase in life span of mice by 29.12%,
58.78%, and 80.51% at the doses of 10, 25 and 50 mg/kg
(i.p.), respectively. The compound increased the life span of
EAC treated mice and restored the hematological
parameters. Thus, the present study reveals anticancer
potential of the tested phenolic compound against EAC in
experimental models

- by Dr. Sharangouda J. Patil and +2
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- In Vitro and Vivo Pharmacology, Anticancer Drugs

Abstract: To determine the histological changes induced by the human therapeutic dose of 5-Fluorouracil (5-FU) and study the histological effects of a single intraperitoneal injection of one tenth, three tenths and five tenths 5-FU LD50 on liver and kidney of healthy mice and to show if these changes are irreversible or not after stopping the treatment. For testing the effects of the drug human therapeutic regime, 18 mice were allocated in six cages (3 mice each); one acted as a control and five acted as a treated group. Treated group received the following treatment through intraperitoneal injection, an initial dose (12 mg/kg 5-FU) was injected intraperitoneally for three consecutive days and a maintenance dose (15 mg/kg 5-FU) was injected intraperitoneally once a week for three weeks. For testing effects of a single intraperitoneal injection of one tenth, three tenths and five tenths 5-FU LD50, the mice were randomized into four groups (one control group and three treated groups) 10 mice each. The treated groups received 50, 150 and 250 mg/kg 5-FU through intraperitoneal injection, respectively. The human therapeutic regime induced histological change only in liver. The treated groups received 50, 150 and 250 mg/kg 5-FU, fatty degeneration and portal area inflammatory cells infiltration were noticed after one week. Liver multinucleated giant cells were detected only in histological sections of mice that received 150 mg/kg. The 250
mg/kg 5-FU induced liver apoptosis. Kidney tubular necrosis was induced by a single injection of 150 and 250 mg/kg 5-FU. The 5-FU human therapeutic regime induced no histological changes in the mice studied organs except for the liver. It induced liver focal necrosis and hydropic degeneration. While, the liver hydropic degeneration disappeared later on, the liver focal necrosis persisted. Using higher doses induced histological change to the liver and the kidney and these pathological changes persisted.

- by Heba N A G E H Gad EL-Hak
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- Pharmacology, Cancer, Histology, Cancer Cell Biology

The identification of signaling pathways that are involved in gliomagenesis is crucial for targeted therapy design. In this study we assessed the biological and therapeutic effect of ingenol-3-dodecanoate (IngC) on glioma. IngC exhibited dose-time-dependent cytotoxic effects on large panel of glioma cell lines (adult, pediatric cancer cells, and primary cultures), as well as, effectively reduced colonies formation. Nevertheless, it was not been able to attenuate cell migration, invasion, and promote apoptotic effects when administered alone. IngC exposure promoted S-phase arrest associated with p21CIP/WAF1 overexpression and regulated a broad range of signaling effectors related to survival and cell cycle regulation. Moreover, IngC led glioma cells to autophagy by LC3B-II accumulation and exhibited increased cytotoxic sensitivity when combined to a specific autophagic inhibitor, bafilomycin A1. In comparison with temozolomide, IngC showed a mean increase of 106-fold in efficacy, wit...

- by Marcela Rosa
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- Organic Chemistry, Medicinal Plants, Glioma, Anticancer Drugs

Combining the chemotherapeutic agent, sorafenib (SRF), with the essential oil, carrot seed oil, can help in reducing the adverse side effects of the SRF. However, the different solubilities of both components impede the mixing, which can be overcome by formulating the carrot oil in a nanoemulsion (NANO). The aim of the present study was to evaluate the anticancer activity, hematoxicity and hepatoxicity of SRF when mixed with the nanoemulsion formulated of the carrot oil (NANO-SRF). As measured by the zetasizer, it has been found that the dispersed nanodroplets of the formulated NANO and NANO-SRF have z-average diameters of 10.27 ± 2.39 nm and 68.92 ± 10.6nm, respectively. Forty female Swiss Albino mice bearing Ehrlich ascites carcinoma (EAC) were split into four groups (n =10). Group I served as the untreated EAC mice while groups II-IV were administered via oral gavage with the 30 mg/kg mouse of SRF solubilized in 0.2 mL of Chremophore/ethanol solution, 30 mg/kg mouse of SRF solubilized in 0.2 mL of NANO and 0.2mL of drug-free NANO, respectively. The results of the antitumor assessment revealed that the GPX and LDH activities in the ascetic fluid of III-NANO-SRF group were enhanced when compared to II-SRF group. The white blood cell counts reduced while the number of the platelets increased for III-NANO-SRF group when compared to II-SRF group. The amounts of alanine aminotransferase (ALT), alkaline phosphatase (ALP), total bilirubin (T.BIL) and direct bilirubin (D. BIL) of the mice treated with the NANO-SRF were ameliorated when compared to the mice treated with the SRF formula. Mixing the SRF with the NANO has improved the efficacy of SRF while reducing its hematoxicity and hepatotoxicity.

- by Mayson H . Alkhatib
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- Physiology, Toxicity, Anticancer Drugs, Tyrosine Kinase Inhibitor

The organotin(IV) compounds used in chemotherapy due to its lipophilicity, affected by the number of carbon atoms and the cytotoxicity. These are affected by the obtainability of Sn coordination bond and bond stabilization between ligand and tin. Two novel organotin(IV) complexes were synthesized, characterized, and tested against human lung cancer cells (A549). The cytotoxic effect of the prepared organotin(IV) complexes against human lung cancer cells (A549) was investigated using the MTT colorimetric assay. Apoptosis was investigated by flow cytometry. The cytotoxicity assay reveals that the Bu 2 SnL 2 complex is more active to inhibit the growth of A549 cells compared to the Ph 2 SnL 2 , and doxorubicin, nevertheless at high concentration (50 and 100) µg/mL the doxorubicin was more affective to inhibit the viability of A549 cells.

- by Alaa Mohammed
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- Apoptosis, Organotin, Anticancer Drugs, Flowcytometry

Cisplatin [cis-diamminedichloroplatinum-(II)] has been used since 1978 to treat a number of different cancer cell lines. However, its effectiveness has been limited due to both harmful side effects as well as the development of cisplatin resistant cancers. Thus, alternatives to cisplatin have become an important focus in anti-cancer research. Gold-(III), an isoelectronic species to platinum-(II), has been of focus to us because of its ability to form metal complexes with similar geometries to platinum-(II) complexes. Previously, 2-sec-butyl-1,10-phenanthroline (sec-butylphen) and its corresponding [(sec-butylphen)AuCl3] complex were synthesized and their anticancer properties subsequently characterized by means of in-vitro tumor cytotoxicity studies. These studies showed a significantly higher cytotoxicity for the sec-butylphen ligand and gold-(III) complex than cisplatin. In addition, when the IC50 values of the free ligand and gold-(III) complex were compared, it was revealed that the free ligand was more cytotoxic, suggesting that it is more active in tumor cell death. In order to determine if gold-(III) complexes have a distinct mechanism for killing cancer cells, structural analogues were synthesized: 2-methyl-9-sec-butyl-1,10-phenanthroline, 2,9-di-sec-butyl-1,10-phenanthroline, and 2,9-di-methyl-1,10-phenanthroline, as well as their corresponding gold-(III) complexes. Their structures were verified using 1H NMR, X-ray crystallography, and elemental analysis. SRB cytotoxicity studies revealed that both ligand and gold-(III) complexes displayed greater cytotoxicity than cisplatin. The data also indicated that the gold-(III) complex antitumor activity does not change as a function of ligand IC50, suggesting that the gold-(III) complexes have a distinct mechanism of tumor cell death. Current research in our laboratory is focused on mono-substituted analogues of 1,10-phenanthroline. 2-n-butyl-1,10-phenanthroline and its gold-(III) complex have been synthesized and their structures have been verified by means of 1H NMR and X-ray crystallography. Elemental analysis, as well as GSH and SRB studies are currently underway.

- by Daniel Lussier
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- Chemistry, Inorganic Chemistry, Organic Chemistry, Coordination Chemistry

Mark and I had a good relationship, however, we also had many bumps in the road and sometimes those bumps become mountains that you can no longer climb up or even try to. MDMA (or Ecstasy) melted the mountains so you could see the one you Love on the other side. It didn’t resolve the problems; it simply removed them completely. I saw Mark for the first time again. I saw him like the moment I first laid eyes on him seven years prior, actually I probably saw him even more clearly and more beautifully than I had ever seen him before. I absolutely had no doubt that he loved me completely and I him. It wasn’t based on what we did or didn’t do for one another; it was simply deep and abiding Love.

- by Joy Sters
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- Psychology, Cognitive Psychology, Social Psychology, Psychiatry

This study was performed to asses and establishes the prevalence of Polypharmacy in geriatric population in the Medicine ward of Rajah Muthaiya Medical College and Hospital, Annamalai University, during one year from January 2013 to January 2014. Demographic analyses of this prospective study revealed that out of 520 patients, 342 (65.76%) were males and 178 (34.23%) were females. All the collected prescriptions were scrutinized for Polypharmacy and were categorized as minor Polypharmacy -concurrent use of ≤ 5 drugs; and major Polypharmacy -concurrent use of > 5 drugs. Out of 502 Prescriptions 61(11.73%) prescriptions were minor Polypharmacy and 457(88.26%) prescriptions were major Polypharmacy. The maximum patients were in the age group of 60-64 (38.84%) range lead to a significant increase in the number of medications. The most common diseases associated systems were Cardiovascular system 147 (28.26 %) patients, and followed by Respiratory system 103(19.80%). Our results show that there is a higher prevalence of Polypharmacy among the males than females. The length of hospital stay of geriatric patients is increase in major Polypharmacy compare with minor Polypharmacy. The prevalence of cardiovascular drugs and respiratory drugs were often involved in Polypharmacy among geriatric patients. Polypharmacy is very common among geriatric patient and health care professional’s interventions to improve the optimal use of medication in geriatric could lead to reduction in the drug related problems associated with Polypharmacy.

Anti-inflammatory, anti-oxidant, anti-cancerous, radioprotective and
anti-microbial properties of ginger (Zingiber officinale) rhizome are
well recognized worldwide. Ginger consumption also helps in the
management of inflammatory damage in Alzheimer’s and
Parkinson’s disease. Biological properties of ginger rhizome are
attributed to its active compounds including, gingerols, shogaols,
paradols and zingerone. Zingerone is active component of dried
ginger rhizome and used in food industry as flavouring agent.
Various observations on the protective role of zingerone against
radiation induced oxidative stress; tissue inflammatory damage and
drug induced toxicity have been made using a wide range of
experimental models. Mechanism of antioxidant and antiinflammatory action of zingerone has been linked to potent radical
scavenging effect, causing alteration in gene/protein expression and
interference with intracellular cell signalling pathways of
inflammation. Our laboratory for the first time revealed antibiofilm
activity of zingerone against opportunistic pathogen Pseudomonas
aeruginosa. This study suggested that zingerone can be explored as a
safe anti-infective agent against P. aeruginosa biofilm associated
infections. Hence, comprehensive information showing health
benefits of zingerone are urgently needed that may provide an update
on its therapeutic potential. We conducted a detailed search of
literature to summarize the proven health benefits and biological
properties of zingerone. This review article summarizes in detail the
in vitroand in vivopharmacological benefits of zingerone.

Africa is home to two major floral kingdoms: the Paleotropical kingdom of central Africa and the Capensis
kingdom of the Western Cape province of South Africa, the latter of which consists of approximately
10,000 species, representing about 20% of Africa’s floral ‘gold mine’, better known as the Cape herbal
medicine. Needless to say, such rich flora comes with numerous plants with a potential to cause poisoning
to humans. This review document reports important toxic medicinal plants and their toxic ingredients
for plant species resident in the southern African region. These include important medicinal uses
and pharmacological properties ranging from antimicrobial, antiviral, anticancer, anti-inflammatory as
well as those that are used as aphrodisiacs and for maternal health care.

- by Ambrose Okem and +1
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- Traditional Medicine, Toxicology, Medicinal Plants, Phytotherapy

Chemistry of heterocyclic organic compounds is as logical as that of aliphatic/aromatic
compounds and of great interests both from the theoretical as well as practical synthetic view to
design novel compounds that becomes one of the most important areas of research today.
Electron-flux of six member/annulated N heterocycles plays vital roles to exhibit diverse potent
biological activities from pharmaceuticals to industrial materials. The Pyrimidine and fused
pyrimidine annulated rings in the chemistry of biological systems has attracted much attention
due to availability in the substructures of therapeutic imperative natural products. As a result of
their prominent and remarkable pharmacological activity, pyrimidine derivative’s intensive
research has been made especially focused on its anticancer activity. The present review gives
brief information about anticancer activity of assorted six member/annulated pyrimidine
derivatives.

- by Ajmal Bhat and +1
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- Pharmacology, Medicinal Chemistry, Heterocyclic chemistry, Anticancer Drugs

Triazole compounds containing three nitrogen atoms in the five-membered aromatic azole ring are readily able to bind with a variety of enzymes and receptors in biological system via diverse non-covalent interactions, and thus display versatile biological activities. The related researches in triazole-based derivatives as medicinal drugs have been an extremely active topic, and numerous excellent achievements have been acquired. Noticeably, a large number of triazole compounds as clinical drugs or candidates have been frequently employed for the treatment of various types of diseases, which have shown their large development value and wide potential as medicinal agents. This work systematically reviewed the recent researches and developments of the whole range of triazole
compounds as medicinal drugs, including antifungal, anticancer, antibacterial, antitubercular, antiviral, anti-inflammatory and analgesic, anticonvulsant, antiparasitic, antidiabetic, anti-obesitic, antihistaminic, anti-neuropathic, antihypertensive as well as other biological activities. The perspectives of the foreseeable future in the research and development of triazole-based compounds as medicinal drugs are also presented. It is hoped that this review will serve as a stimulant for new thoughts in the quest for rational designs of more active and less toxic triazole medicinal drugs.

- by Current Medicinal Chemistry
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- Antifungal Drugs, Anticancer Drugs, Antiviral, Antibacterial

Emblica officinalis (Amla, EO, and E. officinalis) is one of the most important herbs in the Indian traditional medicine system, especially Ayurveda and also known as the king of all medicinal plants. EO is famous ayurvedic herb (the name means sour in Sanskrit) is likely one of the most useful drug treatments within the Indian pharmacopoeia, and is considered to be one of the most strongest uvenatives (Rasayana), particularly for the blood, bones, liver, and heart. It is an exceptionally rich source of vitamin C containing 30 times the amount found in oranges. It is one of the oldest oriental medicines mentioned in Ayurveda as potential remedy for various ailments. EO (Amla) is widely used in the ayurvedic medicines and believed to increase defense or immune power against diseases. Several parts of the plant are used to treat a variety of diseases, but the most important is the " fruit. " The fruit is rich in quercetin, phyllemblic compounds, gallic acid, tannins, flavonoids, pectin, and vitamin C and also contains various polyphenolic compounds. A wide range of phytochemical components including terpenoids, alkaloids, flavonoids, carbohydrates, and tannins have been shown to possess useful biological activities. Many pharmacological studies have demonstrated the ability of EO as antioxidant, anticarcinogenic, antitumor, antigenotoxic, anti-inflammatory activities, anticancer, anti HIV-reverse transcriptase, antidiabetic, inhibitory effects, antidepressant, antiulcerogenic, hair growth tonic, wound healing activities, cardiovascular diseases, neurodegenerative diseases, cancer, and many other traditional uses of the plant. The present study also includes macroscopy, microscopy, preliminary phytoconstituent, and physico-chemical evaluation.

- by Dr. Pushpendra Kumar Jain
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- Pharmacy, Electron Microscopy, Microscopy, Traditional Medicine

Psychedelic drugs are some of the most powerful tools in the world for personal healing and psychological growth. Research at major medical centers over the past few years have shown remarkable results in the treatment of conditions such as depression, post-traumatic stress disorder (PTSD), and anxiety. Psychedelic drugs provide a path of treatment that is often more effective and rapid than other methods, and with many fewer side effects than pharmaceutical options. This paper will be focusing on hallucinogens such as lysergic acid diethylamide (LSD), and psilocybin and entheogens such as ayahuasca and ibogaine.

- by Justin Briglio
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- Religion, Cultural History, Pharmacology, Neuroscience

Cancer is a multifactorial disease, and therefore, a multitarget approach is needed to face the complex cancer biology, based on the combined use of different natural and synthetic anticancer agents able to target synergistically multiple signaling pathways involved in carcinogenesis, including angiogenesis and metastasis. In this view, the plant kingdom represents an unlimited source of phytotherapeutics with promising perspectives in the field of anticancer drug discovery. This narrative review aims to provide an updated overview on the bioactive phytochemicals exhibiting a promising potential as adjuvants in conventional anticancer therapies, with emphasis on antiangiogenic and antimetastatic activities.

- by Dr. Bahare Salehi and +2
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- Chemotherapy, Signal Transduction, Biological Sciences, Phytotherapy

Nepalese medicinal plants were selected to study phytochemical presence, antioxidant, anti-inflammatory
and analgesic activity of plants. Extraction was carried out by double maceration by ethanol and water.
Phytochemical screening was performed by standard methods. Total phenol content was determined by
Folin Ciocalteu method, flavonoid content was determined by aluminium chloride colorimetric method.
The antioxidant activity was tested by DPPH free radical scavenging assay. In Vivo anti-inflammatory
and analgesic activity was performed by carrageenan induced rat hind paw edema and hot plate methods
respectively. The phytochemical analysis revealed the presence of flavonoids, alkaloids, tannins,
saponins, phenols, terpenoids, glycosides and carbohydrates. The ethanolic and aqueous extract of
Viscum album showed total phenols content, total flavonoids content and has significant antioxidant
activity. Similarly, the aqueous extract of Viscum album has dose dependent analgesic activity. Thus,
medicinal plants possess different compounds with valuable antioxidant properties which can contribute
to the development of modern medicines.

- by Biswash Sapkota
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- Antioxidants, Anticancer Drugs, Antiulcer, Antiinflammatory Activity

Background: The emergence of multi drug-resistant (MDR) bacterial infections and cancer has necessitated the development and discovery of alternative eco-safe antibacterial and anticancer agents. Biogenic fabrication of metallic nanoparticles is an emerging discipline for production of nanoproducts that exert potent anticancer and antibacterial activity, and do not suffer from the limitations inherent in physiochemical synthesis methods. Methodology: In this study, we isolated, purified, and characterized a novel cyanobacteria extract (Desertifilum IPPAS B-1220) to utilize in biofabrication of silver nanoparticles (D-SNPs). D-SNPs were produced by adding Desertifilum extract to silver nitrate solution under controlled conditions. Biofabrication of D-SNPs was confirmed using a UV-Vis spectrophotometer. The resultant D-SNPs were characterized using XRD, FTIR, SEM, and TEM. The toxicity of D-SNPs against five pathogenic bacteria and three cancer cell lines (MCF-7, HepG2, and Caco-2) was evaluated. Results: Formation of D-SNPs was indicated by a color change from pale yellow to dark brown. The peak of the surface plasmon resonance of the D-SNPs was at 421 nm. The XRD detected the crystallinity of D-SNPs. FTIR showed that polysaccharides and proteins may have contributed to the biofabrication of D-SNPs. Under SEM and TEM, the D-SNPs were spherical with diameter ranges from 4.5 to 26 nm. The D-SNPs significantly suppressed the growth of five pathogenic bacteria, and exerted cytotoxic effects against MCF-7, HepG2, and Caco-2 cancer cells with IC 50 values of 58, 32, and 90 µg/mL, respectively. Conclusion: These findings showed for the first time the potentiality of novel cyanobacteria strain Desertifilum IPPAS B-1220 to fabricate small SNPs that acted as potent anticancer and antibacterial material against different cancer cell lines and pathogenic bacterial strains. These findings encourage the researchers to focus on cyanobacteria in general and especially Desertifilum sp. IPPAS B-1220 for synthesizing different NPs that opening the window for new applications.

- by Reham S A M I R Hamida and +1
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- Antibacterial agents, Anticancer Drugs, Biological Synthesis of Nanoparticles

Scurrula ferruginea is a type of mistletoe from the Loranthaceae family found in Southeast Asia and distributed in tropical regions, is known to have healing effects for many disorders. Preservation of the bioactive metabolites is dependent on the sample preparation and drying methods as well as extraction solvents used. Thus, the present study was carried out to investigate the effect of different drying methods and extraction solvents on the total phenolic and the antioxidant activities of S. ferruginea leaves. The leaves of S. ferruginea were air and oven (60°C) dried and extracted with aqueous, organic and aqueous-organic solvents. The total phenolic content (TPC) and total flavonoid content (TFC) were used to gauge the phenolic antioxidants extracted, while the antioxidant activity was evaluated by measuring the scavenging effect on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical and via the ferric reducing antioxidant power (FRAP) assay. The optimum conditions obtained were oven drying, 80% acetone with values of 3.47 mg/10 g DW (extract yield), 171.29 mg GAE/1 g DW (TPC), 31.91 mg QE/1 g DW (TFC), 93.2% (DPPH), 26.41 mg TE/1 g DW (FRAP) and 7.41 µg/mL (IC 50). The present findings suggested that sample preparation variability using different drying methods and solvents for extraction play a crucial role in enhancing the efficiency of extraction and efficacy of the antioxidant compounds in S. ferruginea leaf extracts.

Adenium obesum (Forssk.) Roem. and Schult. is a succulent shrub commonly known as desert rose belongs to the family Apocynaceae. Adenium obesum is a native of Africa but nowadays is cultivated in several parts of the world including India as a popular ornamental plant. This plant represents one of the richest sources of phytochemicals such as glycosides and posses great potential for pharmaceutical and piscicultural applications. This review is therefore, an effort to give a detailed study of the literature on biological activities of Adenium obesum. It shows remarkable anticancer, antiviral, antibacterial, trypanocidal, acaricidal, molluscicidal, antioxidant and piscicidal activities. This review concludes that Adenium obesum has a great potential to treat various diseases, and could be used as a source for novel healthcare products in the near future, which requires further experimentation.

Incidence of cancer is growing swiftly worldwide and sparse supply of anticancer drugs; unaffordable cost and its lethal effect have shown the way to adopt complementary and alternative medicine for the treatment and/or prevention of cancer. The isolation of anti-cancer alkaloids vinblastine, vincristine and podophyllotoxins during 1950s prompts research on anticancer agents from plant origins. Lawsonia inermis (L.) popularly known as Mehndi or Henna, is a cosmetically renowned plant of the oriental region possesses diverse pharmacological activity including anti-carcinogenic, antimicrobial, anti-inflammatory, analgesic, antipyretic, hepatoprotective, anti-tuberculostatic. In search of new anticancer drugs from natural sources many researchers have reported anticancer and chemopreventive properties of Henna extracts/compounds in their pre-clinical studies. Lawsone, one of the major constituent of henna, is used as a starting material in the synthesis of a variety of clinically valuable anticancer drugs such as atovaquone, lapachol and dichloroallyl lawsone. This plant contain other chemicals such as isoplumbagin, apigenin, apigenin glycosides, luteolin, luteolin-7 glucosides, p-coumarin and lupeol among which many are reported for their cytotoxicity and chemopreventive activity against different type of cancer cell. Here in this review, we are reporting a palingenesis of information regarding anticancer potential of Mehndi/Henna. We have included maximum available information from its in vitro and in vivo studies by referring different websites, text-books, notes, and articles, abstract, summary and consulting worldwide accepted scientific databases. The present review recapitulates some important findings on the anticancer potential of Mehndi/Henna and to a great extent more work has to be undertaken to explore its novel target(s). Future investigation on novel molecules from Mehndi/Henna may offer great hope for discovering new cancer chemotherapeutic and/or chemopreventive agents from this miraculous plant.

- by Biomed Resther
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- Cancer Biology, Anticancer Drugs

A series of new benzimidazole derivatives, namely 2-acylbenzimidazoles 2-9 , a dihydroquinoxaline 10 , a benzoxazine 11 , quinolines 13-15 and fused 1,2,4-tri-azines 17-24 were synthesized. Structure elucidation of the compounds was conducted using IR, 1 H NMR, 13 C NMR, mass spectral data and elemental analysis. These products were evaluated for in vitro antitumor activity against MCF7 cell line (human breast cancer). Compounds 13-15 and 24 manifested significant antitumor activity.

- by Rania Gomaa
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- Breast Cancer, Anticancer Drugs, Benzimidazoles

In this short review, the current knowledge on the chemical constituents and anticancer properties of Cerbera odollam and Cerbera manghas is updated with some description of their botany and uses. Although these two closely-related coastal tree species have overlapping geographical distribution, they can be distinguished by the eye colour of flowers and the shape of fruits. Chemical constituents of C. odollam and C. manghas include lignans, iridoids, terpenoids, cardiac glycosides (cardenolides), flavonoids, phenolic acids and steroids. Cardiac glycosides of cerberin, dehydrocerberin, neriifolin, tanghinin, deacetyltanghinin and tanghinigenin possess promising anticancer properties with apoptotic activities. However, these cardiac glycosides are also cardiotoxic. Fatal cases of suicides by ingesting Cerbera fruits or seeds have been reported in India and Sri Lanka. In two suicide cases, one in Taiwan and another in the United States, the patients recovered completely. In New Caledonia, four death-threatening cases of poisoning (two were fatal) occurred through consuming toxic coconut crabs. Taken together, both C. odollam and C. manghas are endowed with cardiac glycosides, which have useful pharmacological properties but lethal toxicity.

- by Eric W C Chan
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- Phytochemistry, Malaria, Cytotoxicity, Antimalarial

A series of two biologically active Schiff base ligands L1
, L2 have been synthesized in equimolar reaction of
4-amino-5-(pyridin-4-yl)-4H-1,2,4-triazole-3-thiol with thiophene-2-carbaldehyde and furan-2-carbaldehyde.
The synthesized Schiff bases were used for complexation with different metal ions like
Co(II), Ni(II) and Cu(II) by using a molar ratio of ligand: metal as 1:1 and 2:1. The characterization of
Schiff bases and metal complexes was done by 1
H NMR, UV–Vis, TGA, IR, mass spectrometry and molar
conductivity studies. The in DFT studies the geometries of Schiff bases and metal complexes were fully
optimized with respect to the energy using the 6-31+g(d,p) basis set. On the basis of the spectral studies
an octahedral geometry has been assigned for Co(II), Ni(II) and Cu(II) complexes. The effect of these complexes
on proliferation of human breast cancer cell line (MCF-7) and human hepatocellular liver carcinoma
cell line (Hep-G2) were studied and compared with those of free ligand. The anticancer cell line
results reveal that all metal complexes show moderate to significant % cytotoxicity on cell line HepG2
and MCF-7.

- by prateek tyagi
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- Anticancer Drugs

Biosynthesis of silver nanoparticles has been carried out by using the cell free filtrate of marine sediment
fungal species of Southern peninsular coastal region of India and identified based on the sequence
analysis of Internal Transcribed Spacer region of rRNA genes. Species were identified as Aspergillus flavus
SP-3, Trichoderma gamsii SP-4, Talaromyces flavus SP-5, and Aspergillus oryzae SP-6. The phylogenetic
relationship between the fungal isolates and other fungal strains was compared. Treatment of silver
nitrate with the fungal extract produced stable, predominant, monodispersed and spherical silver
nanoparticles. Preliminary characterization revealed that the nano-particles were in the range of
20–60 nm in all the fungal isolates. Among all the fungi the silver nano-particles of T. gamsii SP-4
showed an enhanced antimicrobial activity against Gram positive bacteria, Gram negative bacteria and
fungi pathogens; an anti-oxidant activity at an effective concentration of 99 mg/ml; and a dose
dependent cytotoxic activity against HEp2 cell lines at LC50 value of 23 mg/ml. Thus, the strains, SP3,
SP4, SP5, and SP6 could be used for simple, non-hazardous and efficient synthesis of antimicrobial and
HEp2 cytotoxic silver nano-particles.

- by Bibin.G. Anand
- •
- Marine Biology, Nanobiotechnology, Nanoparticles, Fungi

Background: Cytotoxic effects of Frankincense resin have been shown on some cancer cell lines. Due to its low side effects, this study was designed to evaluate the anticancer properties of water soluble elements of Frankincense oleo-gum-resin on human oral squamous cell carcinoma cell line. Methods: Oleo-gum-resin was macerated in ethanol. After filtration, the water soluble fraction of dried residue was extracted. KB cells were treated with 0, 62.5, 125, 250 and 500 µg/mL concentrations of obtained Frankincense aqueous fractions and with Doxorubicin as positive control. Frankincense induced cell cytotoxicity; apoptosis and proliferation were investigated using WST assay, Annexin V-FITC/PI, and Ki-67 staining, respectively. Data were analyzed using Kruskal-Wallis test by SPSS 17 software. Results: IC50 of 137.21 µg/mL was obtained from Frankincense aqueous fraction after 48 hours. The percentage of apoptotic cells was elevated in a time-and dose-dependent manner. There was no statistical difference in the Ki-67 expression of KB cells, using different concentration of Frankincense aqueous fraction after 24 and 48 hours (P = 0.083). Doxorubicin inhibited cells growth essentially through apoptosis. Conclusions: Frankincense aqueous fractions seem to suppress KB cell growth through the induction of apoptosis and necrosis rather than the inhibition of proliferation and hence might be a potential anticancer agent. Structural analysis and purification of potent components are suggested for determining more definitive results.

- by azadeh h and +1
- •
- Dentistry, Natural Products Chemistry, Traditional Medicine, Cytotoxicity

Mammalian target of rapamycin (mTOR) is a PI3K (phosphatidylinositol-3-kinase)-related kinase, via two distinct forms – mTOR complex 1 (mTORC1) and mTORC2 coordinates various extracellular and intracellular signals like growth factors, nutrients, amino acids, energy levels in order to achieve optimum cell growth. mTORC1 regulates protein synthesis, lipid biogenesis, oxygen homeostasis, proliferation, autophagy; mTORC2 plays role in cell survival. Since this pathway controls major cellular processes, its dysregulation is associated with pathological conditions like cancer, obesity, type 2 diabetes mellitus. Rapamycin, a naturally occurring mTOR inhibitor, along with synthetically derived compounds of rapamycin – rapamycin analogs (rapalogs), produced by chemical modification of parent drug have achieved clinical success in certain tumor subtypes. Rapalogs have shown their own limitations due to development of resistance and activation of feedback pathways, focusing on the need for efficient mTOR inhibition. In this regard, mTORC1/mTORC2 (mTOR Kinase) inhibitors and dual mTOR/PI3K inhibitors have shown promising results in various in-vitro tumor models, and are currently in phase I/II of clinical trials. With the better understanding of dynamics of mTOR signaling pathway and its function in tumor microenvironment, mTOR inhibitors may provide a good alternative against advanced and refractory cancers.

- by Rupam Gill
- •
- Pharmacology, Pharmacy, Molecular Biology, Cancer

Since time immemorial, medicinal plants have been used by various communities to cure a large number of ailments. Research in medicinal plants has received a renewed focus in recent years. The plant-based system of medicine being natural does not pose any serious complications. Phytochemical compounds in plants are known to be biologically active aiding. Malva sylvestris L. (Malvaceae) is a medicinal plant usually known as common mallow. The purpose of this article is to review information available in the scientific literature on the biological activities of the plant. M. sylvestris having a strong antioxidant, anti-inflammatory, anticancer, wound healing, hepatoprotective, antinociceptive, and antimicrobial activities are reviewed in this article. It is evident from the current literature that M. sylvestris is one of the most promising medicinal plant species. However, extensive research in the area of isolation and characterization of the active compounds of M. sylvestris is essential so that better, safer, and cost-effective drugs for curing various diseases and infections can be developed.

Structure activity relationship (SAR) and mechanism of paclitaxel and its analogues in recent years are discussed in the following areas: SAR of paclitaxel analogues toward “normal” and multi-drug resistance tumors; paclitaxel prodrugs with improved water solubitily and specificity; mechanism of paclitaxel related to tubulin binding and quest for its pharmacophore.

- by Mini-Reviews in Medicinal Chemistry MRMC
- •
- Prodrugs, Anticancer Drugs, Paclitaxel, Microtubules

SnxCu1-xO (wherex¼0, 0.04,0.06&0.10)nanostructureshavebeenpreparedviaco-precipitationtechniqueandcharacterizedfordifferent physiochemical... more

SnxCu1-xO (wherex¼0, 0.04,0.06&0.10)nanostructureshavebeenpreparedviaco-precipitationtechniqueandcharacterizedfordifferent
physiochemical propertiesandanticanceractivity.ThesynthesizednanostructuresexhibitsinglephasemonoclinicstructureofCuOasconfirmed
by x-raydiffraction(XRD),RamanandFouriertransforminfrared(FTIR)spectroscopyresults.TheSnionsdopingintoCuOhasbeenfoundto
tailor thestructuralandmorphologicalproperties.TheUV–visible absorptionspectrashowthatCuOnanostructureshavewideabsorptionpeak
extended fromUVtovisibleregionwhichisstronglyinfluenced bytheintroductionofSnionsinthehostmatrix.Finally,anticanceractivityof
the synthesizednanostructureshasbeendeterminedagainstHeLacancercellline.UndopedCuOexhibitsastrongeranticanceractivityas
compared toSndopedCuOnanostructureswhichhasbeenlinkedwiththeopticalpropertiesofthesenanostructures.

- by Malik Maaza
- •
- Anticancer Drugs

Nature has always been an excellent source for many therapeutic compounds providing us with many medicinal plants and microorganisms producing beneficial chemicals. Therefore, the demand for medicinal plants, cosmetics, and health products is always on the rise. One such plant from the Leguminosae family is licorice and the scientific name is Glycyrrhiza glabra Linn. It is an herb-type plant with medicinal value. In the following article, we shall elaborately look at the plants' phytochemical constituents and the pharmacological impact of those substances. Several compounds such as glycyrrhizin, glycyrrhizinic acid, isoliquiritin, and glycyrrhizic acid have been found in this plant, which can provide pharmacological benefit to us with its anti-cancer, anti-atherogenic, antidiabetic, anti-asthmatic, anti-inflammatory, anti-microbial, and antispasmodic activity. Alongside, these products have a different role in hepatoprotective, immunologic, memory-enhancing activity. They can stimulate hair growth, control obesity, and have anti-depressants, sedatives, and anticoagulant activity. This review examines recent studies on the phytochemical and pharmacological data and describes some side effects and toxicity of licorice and its bioactive components.

- by Md. K A M R U L Hasan and +1
- •
- Medicinal Plants, Anticancer Drugs, Anti-Diabetic herbs, Phytochemicals

The aim of this present article is to underscore the recent evidence linking anticancer activity and free radical scavenging activity of mycotoxins and its significance in the development of newer anticancer drugs. For this purpose extensive bibliographic search of articles were conducted from different referred journals and indexing services. The literature reviewed suggests that mycotoxins not all mycotoxins are toxic and some mycotoxins or mycotoxin derivatives have found use as anticancer drugs. The development of cancer in humans is a complex process including cellular and molecular changes mediated by diverse endogenous and exogenous stimuli and oxidative DNA damage. Reactive oxygen species (ROS), the key mediators of cellular oxidative stress and redox dysregulation involved in cancer initiation and progression, have recently emerged as promising targets for anticancer drug discovery. T-2 toxin and related tricocethecenes, patulin, calicheamicin , chaetocin, gliotoxin, pseurotin, synerazol, rubratoxin, clavines, andrastin, 5methoxysterigmatocystin, penicillic acid, beauvericin, tenuazonic acid, MT 81 etc. showed antitumour activities in different types of cancer cell line. Mycotoxins obtained from marine source such as leptosin, verrucarin, gymnastatins, libertellone, roridin, roseotoxin, secalonic acid, tetrahydrobisvertinolone, zygosporamide also have anticancer activity. The present review enlightens the development of potential anticancer agent from mycotoxins.

- by RAJA CHAKRAVERTY
- •
- Mycotoxins, Anticancer Drugs

"Black Peel Pomegranate" is a rare pomegranate cultivar that its specific features are still uncovered particularly in the bio-nano researches. The present study was organized to evaluate this pomegranate's potential in the biosynthesis of silver nanoparticles as well as bio-medical activities. According to the results, the pomegranate peel extract incredibly inhibited 100 % of DPPH free radicals (EC 50 = 5 mg/mL). This extract also induced more than 70 % cell death in the treated breast tumor cell lines, BT-20 and MCF-7. Interestingly, the extract was capable of biosynthesis very stable and small (15.6 nm) silver nanoparticles at ambient temperature in an ultra-fast pace. Likewise, these nanoparticles inhibited 77 % of DPPH free radicals (EC 50 = 9 mg/mL). Although this antioxidant capacity was lower than that of the extract, instead, the anticancer activity of the synthesized nanoparticles was significantly enhanced, so that they led to more than 81 % and 89 % cell death in the breast tumor cell lines BT-20 and MCF-7, respectively. Considerably, neither the extract nor the biosynthesized silver nanoparticles, showed significant toxicity against non-tumor cell lines (L-929) at the same concentrations. These features of the biosynthesized nanoparticles were quite outstanding in comparison with chemical/commercial ones. Overall, the present study introduces black peel pomegranate as a worthy bio-agent in the biosynthesis of silver nanoparticles with unique activities as well as a cancer treatment.

- by Sadegh Khorrami and +2
- •
- Green Synthesis of nanoparticles, Antioxidants, Silver Nanoparticles, Anticancer Drugs

Treatment of Sodium-3-(2,5-dichlorothiophene-3-yl) prop-3-oxo-1-en-1-olate 2 with aminopyrazoles 3 , aminotriazole 4 and aminotetrazole 5 was produced pyrazolopyrimidines 6, triazolopyrimidines 7 and tetrazolopyrimidines 8 derivatives respectively. These derivatives showed potent anti-tumor cytotoxic activity in vitro using Human hepatocarcinoma cell lines (HepG2) and anti-oxidant activity. also compound 2 was reacted with cyanoethanethioamide 9 , cyanoethaneamide 10 and 2-cyanoacetohydrazide 11 afforded 6-(2,5-dichlorothiophene-3-yl)-2mercaptopyridine-3-carbonitrile 12, 6-(2,5-dichlorothio phene-3-yl)-1,2-dihydro-2-oxopyridine-3-carbonitrile 13 and 2-amino-6-(2,5dichlorothiophene-3-yl)-1,2-dihydro-2-oxopyridine-3-carbonitrile 14 respectively. 6-(2,5-dichlorothiophene -3-yl ) -1,2 -dihydro -2-oxopyridine -3 -carbonitrile 13 was reacted with different reagents to yield pyridinethiol derivatives 15,16 and thienopyridine 17,18,19.

- by Osama M Ahmed
- •
- Synthetic Organic Chemistry, Anticancer Drugs, Antioxidant Activity

The present study reports the phytochemical profiling, antimicrobial, antioxidant, and anticancer activities of Bauhinia variegata leaf extracts. The reducing sugar, anthraquinone, and saponins were observed in polar extracts, while terpenoids and alkaloids were present in nonpolar and ethanol extracts. Total flavonoid contents in various extracts were found in the range of 11-222.67 mg QE/g. In disc diffusion assays, petroleum ether and chloroform fractions exhibited considerable inhibition against Klebsiella pneumoniae. Several other extracts also showed antibacterial activity against pathogenic strains of E. coli, Proteus spp. and Pseudomonas spp. Minimum bactericidal concentration (MBC) values of potential extracts were found between 3.5 and 28.40 mg/mL. The lowest MBC (3.5 mg/mL) was recorded for ethanol extract against Pseudomonas spp. The antioxidant activity of the extracts was compared with standard antioxidants. Dose dependent response was observed in reducing power of extracts. Polar extracts demonstrated appreciable metal ion chelating activity at lower concentrations (10-40 g/mL). Many extracts showed significant antioxidant response in beta carotene bleaching assay. AQ fraction of B. variegata showed pronounced cytotoxic effect against DU-145, HOP-62, IGR-OV-1, MCF-7, and THP-1 human cancer cell lines with 90-99% cell growth inhibitory activity. Ethyl acetate fraction also produced considerable cytotoxicity against MCF-7 and THP-1 cell lines. The study demonstrates notable antibacterial, antioxidant, and anticancer activities in B. variegata leaf extracts.

- by Amit Kumar Sharma
- •
- Antibacterial agents, Antioxidants, Anticancer Drugs, Herbal Anticancer

Aurone is a heterocyclic benzofuranone molecule which is isolated from a natural source, aurone and its derivatives add a new dimension to drug discovery and development due to its anticancer, antidiabetic, antiviral, anti-malarial, anti-hepatitis, antihormonal, anti-diabetic, anti-obesity, anti-cholinesterase inhibitor and anti-inflammatory activity, which inspired chemist due to its incomparable properties. In this review we have compiled various pharmacological activity of aurone molecule in an effort to pave a way for development in this area of research.

- by Mahesh AR
- •
- Anticancer Drugs

A series of 3-indolyl-3-hydroxy oxindole derivatives (n ¼ 41) were synthesized by the green aminocatalytic method with excellent yields under mild reaction conditions. All the newly synthesized derivatives were subjected to evaluate their cytotoxic properties against different human cancer cell lines. Results indicated that about 73% of the derivatives exhibited significant anti-proliferative activities against leukemia (U937, THP-1), lung (A549) and breast cancer (MCF7) cell lines. Among them a few of the derivatives exhibited the most potent and effective cytotoxic activities on U937 (34, 36, 38 and 41) and MCF7 (12, 35, 40 and 41) cell lines, and their anti-proliferation activities are better than the positive control, Etoposide.

- by Principal Scientist Ipc Mohan Rao M. and +1
- •
- Anticancer Research, Anticancer Drugs

Herbal medicine is established on the plants contains natural chemical substances that can promote health and have curative properties for illness and diseases. Medicinal herbs play an important role in the treatment of cancer. In this... more

- by World Journal of Pharmaceutical Sciences
- •
- Anticancer Drugs

The FT-IR and FT-Raman spectra of 5-Fluorouracil were recorded in the solid phase in the regions 400-4000 cm −1 and 50-4000 cm −1 , respectively. The vibrational spectra were analysed and the observed fundamentals were assigned to different normal modes of vibration. The experimental wavenumbers were compared with the scaled vibrational values using DFT methods: the Ar matrix data were related to gas phase calculations, while the values of the solid state spectra were compared to those with dimer simulations. The study indicates that some features that are characteristic of vibrational spectra of uracil and its derivatives are retained in the spectrum of 5-fluorouracil and it exists in ketonic form in the solid phase. The tautomerism was also studied and the spectra of the two most stable forms were simulated. The calculated wavenumbers have been employed to yield thermodynamic properties.

- by MAURICIO ALCOLEA PALAFOX
- •
- Anticancer Drugs

Cancer is one of the most extreme medical conditions in both developing and developed countries around the world, causing millions of deaths each year. Chemotherapy and/or radiotherapy are key for treatment approaches, but both have numerous adverse health effects. Furthermore, the resistance of cancerous cells to anticancer medication leads to treatment failure. The rising burden of cancer overall requires novel efficacious treatment modalities. Natural medications offer feasible alternative options against malignancy in contrast to western medication. Furanocoumarins’ defensive and restorative impacts have been observed in leukemia, glioma, breast, lung, renal, liver, colon, cervical, ovarian, and prostate malignancies. Experimental findings have shown that furanocoumarins activate multiple signaling pathways, leading to apoptosis, autophagy, antioxidant, antimetastatic, and cell cycle arrest in malignant cells. Additionally, furanocoumarins have been shown to have chemo preventiv...

- by Haroon Khan
- •
- Genetics, Pharmacy, Pharmacognosy, Anticancer Drug Delivery

The genus Hypericum is one of the most popular genera in both traditional medicine and scientific platform. This study is designed to provide conceptual insights on the biological potential and chemical characterization of H. salsugineum, which is endemic to Turkey. The qualitative and quantitative phenolic content of the extracts was characterized by HPLC-ESI-MS n. Biological efficiency was investigated by enzyme inhibitory assays (cholinester-ases, tyrosinase, amylase, and glucosidase) and anti-cancer efficacy tests (anti-proliferative activities with the iCELLigence technology, colony formation and wound healing scratch assays). Phenolic acids (3-O-caffeoylquinic, 5-O-caffeoylquinic, and 4-O-caffeoylquinic acids) were the predominant group in the studied extracts, although several flavonoids were also detected and quantified. The extracts exhibited good inhibitory effects on tyrosinase and glucosidase, while they had weak ability against cholinesterases and amylase. Computational studies were also performed to explain the interactions between the major phenolics and these enzymes. The extracts displayed significant anti-cancer effects on breast carci-noma cell lines. Our findings suggest that Hypericum salsugineum could be valued as a potential source of biologically-active compounds for designing novel products.

- by Onur Bender
- •
- Natural Products, Phytochemistry, Cell Biology, Antioxidants

Objective: The synthesis of metal nanoparticle is a growing area of research in modern material science and technology. Utilization of the silver nanoparticles in the field of biomedical nanotechnology and nanomedicines is rapidly growing because of their antimicrobial, anticancer, antioxidant property and less toxicity. Nanoparticles are synthesized by chemical methods, but are not eco-friendly. The objective of the study is to develop a fast, eco-friendly and convenient method for silver nanoparticle synthesis. Methods: In this method utilization of the reducingproperty of Aegle marmelos leaf extract was done for synthesis of stable silver nanoparticles. Characterization of the metal nanoparticles was carried out by UV- Vis spectroscopy, Fourier Transform Infrared Spectroscopy (FTIR), Scanning Electron Microscopy (SEM), X-ray Diffraction microscopy (XRD), Energy Dispersive X-ray spectroscopy (EDX) and zeta potential analysis. Results: This result showed the average particle size of 15 -30 nm and spherical structure of stable silver nanoparticles. Green synthesized nanoparticles tested for its antibacterial activity by the well diffusion method. Silver nanoparticles had shown a more inhibitory effect against Streptococcus pyogenes, Escherichia coli, and Pseudomonas aeruginosa than Staphylococcus aureus and Aeromonas hydrophila at 25, 50 and 100 µg/ml concentrations. Conclusion: This study is recommends the use of Aegle marmelos leaves for the synthesis of silver nanoparticles and can be applied as an antimicrobial agent. Keywords: Nanoparticles, Aegle marmelos, Characterization, Antibacterial activity.

- by sunita patil
- •
- Nanotechnology, Silver Nanoparticles, Anticancer Drugs

Vinblastine (VLB), a cytotoxic alkaloid is used extensively against various cancer types and the crystal structure of its tubulin complex is already known. Multitarget affinity of vinblastine has been investigated and the nature of binding with biological receptors namely, duplex DNA and Human serum albumin (HSA) has been compared to the binding characteristics of its known complex with natural high affinity receptor tubulin using molecular docking and QM–MM calculations. VLB is found to interact with DNA as well as HSA protein, though, with weaker affinity as compared to tubulin. Analysis of various docked complexes revealed that the H-bonds and cation–pi bonds do not have significant contribution to the binding interactions and despite its large size, VLB remains in relaxed conformation and fits in the hydrophobic regions on the receptors.

- by Prateek Pandya
- •
- Molecular Recognition, Anticancer Drugs, Docking, ONIOM

Magnetic spinel ferrite nanoparticles possess high scientific attention for the researchers attributed to its broad area for biomedicine purposes, comprising cancer magnetic hyperthermia and targeted drug delivery. Herein, we report the ultrasound irritation assisted the sol-gel method for the spinel Zn 0.5 Co 0.5-x Ag 2x Fe 2 O 4 (x = 0.00, 0.10, 0.20, and 0.30) nanoparticles (NPs) synthesis. The Rietveld refinement patterns revealed the successful synthesis of the cubic structure Zn 0.5 Co 0.5-x Ag 2x Fe 2 O 4 and the crystallite size ranged from 14.1 nm to 18.4 nm. Also, the optical band gap decreased from 2.39 eV for Co-Zn ferrite to 2.20 eV for Zn 0.5 Co 0.2 Ag 0.6 Fe 2 O 4 sample. Electron paramagnetic resonance spectroscopy was used to study ferromagnetic resonance characteristics of the Zn 0.5 Co 0.5-x Ag 2x Fe 2 O 4 samples. The resonance field was increased from 2512.2 Gauss for Co-Zn ferrite sample to 2834.8 Gauss for Zn 0.5 Co 0.2 Ag 0.6 Fe 2 O 4 sample, while the line width decreased from 2401.3 to 1990.1 Gauss. Also, the saturation was reduced from 45.68 emu.g-1 for the pristine Zn 0.5 Co 0.5 Fe 2 O 4 sample to 22.20 emu.g-1 for Zn 0.5 Co 0.2 Ag 0.6 Fe 2 O 4 sample. Furthermore, cytotoxicity of Zn 0.5-Co 0.2 Ag 0.6 Fe 2 O 4 NPs against human breast cancer MCF-7, HepG2 liver cancer, and LoVo colorectal cancer cells was examined. The cytotoxicity of Zn 0.5 Co 0.2-Ag 0.6 Fe 2 O 4 on the previous cancer cell lines resulted in inhibition of cell growth estimated by MTT assay. The exposure of MCF-7, HepG2, and LoVo cancer cells

The DNA double helix represents an important target for a huge number of anti cancer drugs, and for many years substances with toxic side effects have been used in anticancer therapy. The structure and biological function of G quadruplex structures have been explored and there is an interest in them as targets for anti cancer drugs. This report focuses on the structure and function of the G-quadruplex as well as the analysis of targeting them in oncogene cmyc, ribosomal and human telomeric DNA. The G-quadruplex-ligand complex is discussed and there is also a review on a number of small molecules that have shown to be effective in binding specifically to G-quadruplex complexes.. Information gathered from X ray crystallography and NMR, among others, is discussed. The review and the information collated will be important for the development of drugs targeting quadruplexes from particular genes.

- by kassam siddiq
- •
- Telomeres, Telomerase, Anticancer Drugs, Oncogenes

The aims of this study was to isolate compounds from the methanol extract of stem bark of Garcinia cowa and to evaluated their cytotoxic activity against breast (MCF-7) and lung (H-460) cancer cell lines. The ethyl acetate fraction was separated by successive silica gel column chromatography to give three compounds. Based on spectroscopic comparison with those of the literature, these compounds were elucidated as 6-hydroxyone(3), rubraxanthone (4), α-mangostin (5), a new compound 1,3,6-trihydoxy-7-methoxy-4-(4-acetoxy-3-methyl-2-butenyl)-8-(3,7-dimethyl-2,6-octadienyl)xanthone (6) and cowanin (7). Complete NMR assignment of 6-hydroxy-calabaxanthone (2) and cowanin (7) were published for the first time. All isolated compounds were subjected to MTT assay against MCF-7, H-460 and DU-145 cancer cell lines. α-mangostin (5) and cowanin (7) were found to be potent against MCF-7 while 6-hydroxy-calabaxanthone (2) potent against DU-145 cell lines. Conclusion: The results indicate that G. cow...

- by Johnson Stanslas
- •
- Natural Products Chemistry, Spectroscopy, Drug Discovery, NMR Spectroscopy

Abrus precatorius is highly regarded as a
universal panacea in the herbal medicine with diverse
pharmacological activity spectra. This experimental
study on the mechanism of the anticancer activity of
A. precatorius leaf extracts, may offer new evidence
for A. precatorius in the treatment of breast cancer in
clinical practice. Cell death was determined by using
MTT assay. Further analyses were carried out by doing
DNA laddering, PARP cleavage, FACS, semi-quantitative
RT-PCR and detection of cellular reactive
oxygen species (ROS) by DCFDA assay. A. precatorius
showed very striking inhibition on MDA-MB-231
cells. MTT assay showed more than 75 %inhibition of
the cells and treated cells indicated visible laddering
pattern with thick compact band. PARP cleavage
produced 89 kDa cleavage product which was associated
with apoptosis. Flow cytometer exhibited a sub-
G0/G1 peak as an indicative of apoptosis. mRNA
expression level of apoptosis-related genes p21 and
p53 was markedly increased in cells treated with the
extract as compared to control. The up-regulation of
p21 and p53 may be the molecular mechanisms by
which A. precatorius extract which induces apoptosis.
An increase in the concentration of A. precatorius
extract does not generate ROS, instead it reduces ROS
formation in MDA-MB-231 cells, as evident from the
shift in fluorescence below untreated control. This is
the first report showing that A. precatorius leaf extract
exhibits a growth inhibitory effect by induction of
apoptosis in MDA-MB-231 cells. Our results contribute
towards validation of the A. precatorius extract as a
potentially effective chemopreventive or therapeutic
agent against breast cancer.

- by Mysore Krishnaiah Sateesh
- •
- Natural Products, Phytochemistry, Cancer, Breast Cancer

A novel and simple wet chemical hydrothermal synthesis method was employed in the preparation of zinc oxide (ZnO) nanoparticles using neem (N), pepper (P) and turmeric (T) extracts as solvent media. The structural and optical properties as well as the antibacterial and anticancer properties of all the samples (ZnO, N/ZnO, P/ZnO, T/ZnO and NPT/ZnO) were characterized and analyzed. Solvent media was found to have an effect on both the size and the morphology of the nanoparticles, which in turn effected their optical and cytotoxic properties. The colony forming unit (CFU) assays were done for E. coli, S. aureus and S. typhi in which T/ZnO (~2) and P/ZnO (~3) showed a remarkable effect on S. aureus for 100 µg/ml and nearly zero for 150 µg/ml. The zone of inhibition (ZoI) was measured for S. agalactiae, S. dysgalactiae and S. pyogenes.The results showed that S. dysgalactiae is more sensitive to N/ZnO.Finally, the anticancer properties of these compounds towardsprostate cancer cells was investigated. Among the active compounds T ZnO showed the highest activity with low IC50 value (37.751 µg/ml) followed by P ZnO (45.68 µg/ml).

- by Joshua Pearce and +1
- •
- Synthesis of nanoparticles, Nanomaterials Characterization, Cancer, Nanobiotechnology