Cytotoxic Research Papers - Academia.edu (original) (raw)

Extract from the leaves of Antidesma ghaesembilla were screened for their antithrombotic, cytotoxic and antimicrobial exercises. The cytotoxicity was surveyed with the brine shrimp lethality bioassay and antithrombotic impact with human... more

Extract from the leaves of Antidesma ghaesembilla were screened for their antithrombotic, cytotoxic and antimicrobial exercises. The cytotoxicity was surveyed with the brine shrimp lethality bioassay and antithrombotic impact with human blood. The brine shrimp lethality bioassay was utilized to assess cytotoxicity (LC 50 = 432.13 μg/ml) contrasted with Vincristine sulfate (LC 50 = 0.74 μg/ml). It was also assessed as antithrombotic activity when contrasted with streptokinase. It has significant antithrombotic movement (63.45±2.08%) contrasted with standard streptokinase (81.32±1.46%). The extract indicated zone of inhibition against Gram positive bacteria (Staphylococcus aureus and Bacillus subtilis) and Gram negative bacteria (Salmonella typhi, Salmonella paratyphi, Escherichia coli, Pseudomonas aeruginosa) 1000 µg/disc. Gram negative bacteria Bacillus cereus demonstrated no action against at both doses. A. ghaesembilla leaves extract and relative percentage inhibition of the extract also calculated. These results indicate that A. ghaesembilla have favorable Antithrombotic, cytotoxic and antibacterial effects of A. ghaesembilla extract to be processed for pharmaceutical use.

Background: Thioredoxin reductase is an important enzyme in antioxidant defense and regulation of cell function, its inhibition has cytotoxic effects. Aim: To predict if; there is correlation between the already in vitro... more

Background: Thioredoxin reductase is an important enzyme in
antioxidant defense and regulation of cell function, its inhibition has
cytotoxic effects.
Aim: To predict if; there is correlation between the already in vitro
cytotoxic studied Au (III) complexes & their docking studies
Material & Method: The enzyme in complex with a potential
inhibitor will be downloaded from the Protein Data Bank (PDB). The
inhibitory binding site of the enzyme will be defined as the 8 A°-sphere of residues surrounding the inhibitor.
Four gold-based compounds along with cisplatin and XAN were then
docked into the defined site and their poses inside the active site were
analyzed.
Results: These compounds have already shown in vitro activity
against the Hep-2 cell line and this cytotoxicity compared with the
results generated by the computer
Conclusion: Computer aided drug design is excellent & modern tool
to correlate between the structures & inhibition properties of Au (III)
complexes.

Brine shrimp lethality assay (BSLA) is an important method in the evaluation of plantbioactivity for the subsequent isolation of bioactive compounds from the plant extracts which may lead tothe development of new drugs. In this study,... more

Brine shrimp lethality assay (BSLA) is an important method in the evaluation of plantbioactivity for the subsequent isolation of bioactive compounds from the plant extracts which may lead tothe development of new drugs. In this study, BSLA was employed to evaluate the potential cytotoxicproperties of the whole plant extracts of
Eleusine indica. E. indica has been widely used for the treatmentof several diseases like kidney problems, diabetes, gastro-intestinal diseases and is used as diuretic. Themost common methods of extraction (decoction, absolute ethanol, 50% water - 50% ethanol) weretested to determine cytotoxic effects against the brine shrimp nauplii. Results showed that the bestextraction method for the whole plant samples of
E. indica is through the use of 50:50 ethanol-watermixture extract. The acute lethal concentration (LC50) ofE. indica after 6 h exposure to mixture extractwas 153.99 ppm, while the ethanolic extract obtained an LC50 of 409.73 ppm. After 24 h exposure,increased mortalities of brine shrimps were recorded in all prepared extracts. Maximum mortalities(100%) were observed in the three concentrations of 100-1000 ppm in the mixture extract of E. indica. In this respect, E. indica possesses cytotoxic behavior suggesting the presence of potential bioactivechemical components in the plant’s extract.

Platinum containing compounds have shown antineoplastic potential, but their clinical applications have been limited by high toxicity. Ruthenium containing complexes have long been known to be well suited for biological applications, and... more

Platinum containing compounds have shown antineoplastic potential, but their clinical applications have been limited by high toxicity. Ruthenium containing complexes have long been known to be well suited for biological applications, and have long been utilized as replacements to popular platinum based-drugs. Here, we report a novel series of ruthenium(II) arene compounds bearing thiosemicarbazone and isonicotinylhydrazone ligands with potent anticancer activity their structure activity relationships and apoptosis was studied. The cytotoxic activity of the new ruthenium(II) arene compounds has been evaluated in several cell lines (Molt 4/C8, L1210, CEM, HL60 and BEL7402). Among them, ten complexes were found to be excellent in vitro growth inhibitory activity against various cell lines with IC50 in the sub-micromolar range.

Background: Among marine organisms, seaweeds are a highly diverse group of organisms from which many new substances have been isolated and many of these compounds have been demonstrated to possess a large spectrum of... more

Background: Among marine organisms, seaweeds are a highly
diverse group of organisms from which many new substances have
been isolated and many of these compounds have been demonstrated
to possess a large spectrum of bioactivities.
Objective: In this study, we aim to evaluate the antibacterial,
cytotoxic and antioxidant activity of green algae, Cladophora
prolifera (Roth) Kutzing, collected from the northern Mediterranean
coast of Morocco.
Material and Method: The antibacterial activity was determined by
disk diffusion method. After fractionation by column
chromatography, the fractions from C. prolifera were tested against
Staphylococcus aureus ATCC 25923 using the broth microdilution
assay. The antitumor effect on human colon cancer cells was
investigated via sulforhodamine-B (SRB) assay. Then the Crude
extract has been tested in radical-scavenging assays to assess their
antioxidant activity.
Results: In vitro screening of methanolic extract of C. prolifera
showed specific activity to inhibit the growth of five virulent strains
of pathogenic bacteria, Escherichia coli (ATCC 25922),
Staphylococcus aureus (ATCC 25923), Staphylococcus aureus
(ATCC 29213), Enterococcus faecalis (ATCC 29212) and Klebsiella
pneumoniae (ATCC 700603). The obtained results indicated that the
extracts of C. prolifera were cytotoxic against HT29 human colon
cancer cells. In addition, based on the capacity of the algae to
scavenge the ABTS radical cation, we revealed that C. prolifera
extract presented a satisfactory antioxidant activity.
Conclusion: These results suggest that C. prolifera has a great
biological potential, which could be considered for future uses in
food, pharmaceutical and cosmetic industries.

Cancer is the second leading cause of death worldwide and oxidative stress is one of the factors responsible for causing cancer. Antioxidants play a very important role in prevention of cancer. Therefore, efforts... more

Cancer is the second leading cause of death worldwide and oxidative
stress is one of the factors responsible for causing cancer.
Antioxidants play a very important role in prevention of cancer.
Therefore, efforts have been made to identify natural antioxidants
having anti-cancer potential. Various herbs, fruits and vegetables
have diverse phytochemicals that display antioxidant properties and
help in reducing the risk of cancer. Wheatgrass has a potent
antioxidant efficacy and has been used as a health drink to cure many
diseases in folk medicine. In the present study, anumber of solvent
extracts of wheatgrass was tested for their antioxidant ability. The
most effective solvent extract was further evaluated for cytotoxic
effect in Hep2 cell lines and apoptotic induction was demonstrated by
propidium iodide (PI) fluorescent staining. The bioactive constituents
were analysed by GC-MS. Methanol extract (ME) showed the
highest quantity of phenols and flavonoids. PI staining showed
apoptotic features like nuclear fragmentation and chromatin
condensation and GC-MS analysis showed the presence of nine
bioactive phytoconstituents in methanol extract. Hence we conclude
that wheatgrass has good antioxidant and cytotoxic property and
being a natural product, could be a good candidate for cancer
prevention and treatment.

Recent study was conducted to develop a simple UV spectrophotometric method to determine an HCV inhibitor, Velpatasvir in bulk form according to official requirement and validate as per ICH guidelines. λmax of Velpatasvir was found 303... more

Recent study was conducted to develop a simple UV spectrophotometric method to determine an HCV inhibitor, Velpatasvir in bulk form according to official requirement and validate as per ICH guidelines. λmax of Velpatasvir was found 303 nm. Linearity existedperceived in the concentration assortment 5-40 μg/ml (r 2 =0.999) for the method. The method was validated pertaining to linearity, precision and accuracy studies, LOD and LOQ consistent with ICH guidelines. Recovery studies for absorption maxima method was found to be 100.35%, 100.0% and 100.08% respectively. The existent method was establish to be simple, linear, precise, accurate as well as sensitive and can be applied for routine quality control enquiry for the analysis of Velpatasvir in bulk form.

1,4-Disubstituted bis-chromenyl triazole hybrids 5a–m have been synthesized in a three-step reaction sequence from 4-(bromomethyl)-2H-chromen-2-ones 3a–m. The intermediate azides 4a–m underwent a regioselective 1,3-dipolar cycloaddition... more

1,4-Disubstituted bis-chromenyl triazole hybrids 5a–m have been synthesized in a three-step reaction sequence from 4-(bromomethyl)-2H-chromen-2-ones 3a–m. The intermediate azides 4a–m underwent a regioselective 1,3-dipolar cycloaddition with a 2H-chromen-2-one linked acetylenic dipolarophile in the presence of Cu (II)/ascorbate/water/n-butanol reaction medium. Three compounds 5h–j exhibited 6.25 μg/mL MIC against M. tuberculosis. Among the compounds screened for antifungal activity, lowest MIC of 6.25 μg/mL was observed for 5c against A. niger that also exhibited DNA cleavage observed by agarose gel electrophoresis. All the compounds were moderately active against both Gram-positive and Gram-negative bacterial strains. The cytotoxic effect of potent compounds on normal cells (V79 and HBL100) was assessed by MTT assay.

Solvent leaf extracts of Terminalia catappa were evaluated for their cytotoxic and their radical scavenging potential. Brine shrimp assay was used for exploring cytotoxic activity, all the extracts namely hexane, DCM, chloroform,... more

Solvent leaf extracts of Terminalia catappa were evaluated for
their cytotoxic and their radical scavenging potential. Brine shrimp
assay was used for exploring cytotoxic activity, all the extracts
namely hexane, DCM, chloroform, acetone and methanol were
tested at the dose level of 25, 50, 100 and 200microgram /ml. A
dose dependent response was obtained in all the extracts.
Chloroform extract showed 100percent activity at the highest dose
of 200μg/ml. Antioxidant activity was evaluated by one
qualitative(TLC based) and two quantitative radical scavenging
assays namely DPPH (2, 2- Diphenyl-1- picryl hydrazyl) assay
and ferric reducing antioxidant power (FRAP) assay. In both
assays acetone extract exhibited significant reduction of free
radicals. The IC50 value of acetone extract was 36.9μg/ml.
Ascorbic acid was used in these assays as reference compound.
FRAP value of acetone extract was found to be 6.73 much higher
than all the other extracts.

The inhibition ability of phthalhydrazide (PTD) for mild steel in 1 M HCl at 30 °C was investigated by electrochemical measurements [impedance spectroscopy (EIS) and potentiodynamic polarization techniques] and quantum chemical... more

The inhibition ability of phthalhydrazide (PTD) for mild steel in 1 M HCl at 30 °C was investigated by electrochemical measurements [impedance spectroscopy (EIS) and potentiodynamic polarization techniques] and quantum chemical calculations. The frontier molecular orbital energy E HOMO (highest occupied molecular orbital), E LUMO (lowest unoccupied molecular orbital), and the Mulliken charge distribution were calculated and are discussed. Results showed that the inhibition efficiency of PTD increased with inhibitor concentration. The maximum corrosion inhibition efficiency was 77.6% at 2 mM PTD. Adsorption of the inhibitor followed the Langmuir adsorption isotherm. Adsorption of inhibitor molecules on mild steel surface occurred spontaneously and chemically. Quantum chemical calculations showed that the low performance of PTD as a corrosion inhibitor is due to the large energy gap (E HOMO − E LUMO).

Two new vanadyl(IV) complexes with the non-steroidal antiinflammatory drugs Indomethacin and Diclofenac were synthesized and characterized by elemental analysis, electronic, diffuse reflectance and FTIR spectroscopies and thermal... more

Two new vanadyl(IV) complexes with the non-steroidal antiinflammatory drugs Indomethacin and Diclofenac were synthesized and characterized by elemental analysis, electronic, diffuse reflectance and FTIR spectroscopies and thermal behavior. The structures of the oxo-vanadium(IV) complexes were obtained by carrying out ab initio calculations (B3LY/3–21G**) owing to the difficulties of obtaining single crystals of good quality for X-ray studies. Indomethacin and Diclofenac did not cause any effect when tested on cellular proliferation in two osteoblast-cell lines in culture (MC3T3E1 and UMR106). The biological effect of the complexes depends on the cellular type and on the nature of the coordinated ligands. Copyright © 2005 John Wiley & Sons, Ltd.

Cancer is a leading cause of death worldwide and novel chemotherapeutic agents with better efficacy and safety profiles are much needed. Coumarins are natural polyphenolic compounds with important pharmacological activities, which are... more

Cancer is a leading cause of death worldwide and novel chemotherapeutic agents with better efficacy and safety profiles are much needed. Coumarins are natural polyphenolic compounds with important pharmacological activities, which are present in many dietary plants and herbal remedies. The objective of this study is to investigate natural and synthetic coumarin derivatives with considerable anticancer capacity against three human cancer cell lines. We synthesized 27 coumarin derivatives (mostly having 4-methyl moiety) and examined their cytotoxic effect on three human cancer cell lines, K562 (chronic myelogenous leukemia), LS180 (colon adenocarcinoma), and MCF-7 (breast adenocarcinoma) by MTT reduction assay. Screened compounds included 7-hydroxy-4-methylcoumarins (7-HMCs), 7-acetoxy-4-methylcoumarins (7-AMCs), and different dihydroxy-4-methylcoumarin (DHMC) and diacetoxy-4-methylcoumarin (DAMC) derivatives. Some compounds with methoxy, amine, and bromine substitutions were also exa...

Pyrrolizidine alkaloid (PA) producing plants belonging to the Boraginaceae (Echium wildpretti) and Asteraceae (Canariothamnus palmensis, Kleinia neriifolia, Pericallis appendiculata, Pericallis echinata, Pericallis hansenii, Pericallis... more

Pyrrolizidine alkaloid (PA) producing plants belonging to the Boraginaceae (Echium wildpretti) and Asteraceae (Canariothamnus palmensis, Kleinia neriifolia, Pericallis appendiculata, Pericallis echinata, Pericallis hansenii, Pericallis multiflora, Pericallis steetzii and Senecio bollei) were selected to study their alkaloidal composition and the defensive properties (antifeedant and phytotoxic effects) of their ethanolic and alkaloidal extracts plus their isolated PAs against insects (Spodoptera littoralis, Leptinotarsa decemlineata, the aphids Myzus persicae and Rhopalosiphum padi) and Lactuca sativa seeds. We also tested the selective cytotoxic effects of these PAs on insect-derived Sf9 and mammalian CHO cells. Most of the insect antifeedant effects were found in the ethanolic extracts. The isolated PAs had species- and structure-dependent antifeedant effects and all of them decreased L. sativa radicle growth, suggesting a specific mode of action against insects and a generalized one against plants. Given the relatively low alkaloid content of these species, we assume that their herbivore defenses are not only alkaloid-based.

The purpose of the research is to find out the comparative cytotoxic potentials of Ipomoea Pes-Caprae and Murraya koenigii fractions (crude methanol, Pet ether, Chloroform) by using brine shrimp mortality assay. These two plant... more

The purpose of the research is to find out the comparative
cytotoxic potentials of Ipomoea Pes-Caprae and Murraya koenigii
fractions (crude methanol, Pet ether, Chloroform) by using brine
shrimp mortality assay. These two plant extracts were tested at
concentration 400, 200, 100, 50, 25, 12.5, 7.25, 3.125 μg/ml. The
extracts of both plants showed remarkable cytotoxic activity.
Following, the ascertainment of LC50 values of the extracts
(crude, Chloroform, pet ether) the extracts of Ipomoea Pes-
Caprae (1.649,5.691, 1.583 μg/ml) and Murraya koenigii( 4.365,
10, 5.370 μg/ml) were respectively compared to a reference drug
vincristin sulphate with LC50 0.839 μg/ml. Ipomoea Pes-Caprae
was determined as more cytotoxic than Murraya koenigii. Where
chloroform extract of Murraya koenigii showed low cytotoxicity
than all the extract of Ipomoea Pes-Caprae.

Juniperus spp. are used as medicinal plants in many countries like Bosnia, Lebanon, and Turkey. In folk medicines, these plants have been used for treating skin and respiratory tract diseases, urinary problems, rheumatism and gall bladder... more

Juniperus spp. are used as medicinal plants in many countries like Bosnia, Lebanon, and Turkey. In folk medicines, these plants have been used for treating skin and respiratory tract diseases, urinary problems, rheumatism and gall bladder stones. The objectives of this work were to synthesize silver nanoparticles (AgNPs) using a coniferous tree, Juniperus procera leaf extract and testing the synthesized AgNPs for its antimicrobial potentials, hemolytic activity, toxicity and the proliferative effects against normal and activated rat splenic cells. Leaf extract was prepared using acetone and ethanol as solvents. AgNPs were prepared using the acetone extract. AgNPs were validated using UV-Vis spectroscopy and scanning electron microscopy (SEM). Functional groups in the extract were identified using Fourier Transform Infrared (FT-IR) spectroscopy. SEM images of AgNPs showed spherical and cubic shapes with a uniform size distribution with an average size of 30-90 nm. FT-IR spectroscopy showed the presence of many functional groups in the plant extract. AgNPs showed promising antimicrobial activity against tested bacteria and fungus. AgNPs also expressed a stimulating activity towards the rat splenic cells in a dose dependent manner. Acetone as solvent was safer on cells than ethanol. Green synthesized AgNPs using J. procera might be used as a broad-spectrum therapeutic agent against microorganisms and as an immunostimu-lant agent. Ó 2018 Production and hosting by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

The present study was carried out to compare the potential of green and ripen fruits aqueous extract against antileishmanial, larvicidal, antioxidant and brine shrimp cytotoxicity assay. A general antileishmanial, larvicidal, antioxidant... more

The present study was carried out to compare the potential of green and ripen fruits aqueous extract against antileishmanial, larvicidal, antioxidant and brine shrimp cytotoxicity assay. A general antileishmanial, larvicidal, antioxidant and cytotoxic assays were performed at different concentrations. The green fruits expressed significant activity against L. tropica (LC 50 =0.41µg/mL), while the ripe fruits showed less activity (LC 50 =8227.51µg/mL). Upon larvicidal activity against Culex quinquefasciatus larvae, the green fruits extract expressed excellent results with LC 50 value 67.65µg/mL while ripe fruits showed less activity with LC 50 value 7171.18µg/mL. Similarly, for cytotoxicity assay for green and ripe fruits the LC 50 value obtained were 18.07µg/mL and 530.2µg/mL, respectively. The result for antioxidant potential showed that only the green fruits has some antioxidant potential (IC 50 232.23µg/mL) compared to ripe fruits (>1000µg/mL) against the reference drug (ascor...

The cytotoxic and genotoxic effects of the aqueous leaf extract of Icacina trichantha Oliv. were evaluated using Allium cepa bioassay. Onion bulbs were exposed to various concentrations, 25–100% v/v, of the extract for 48–96 h for... more

The cytotoxic and genotoxic effects of the aqueous leaf extract of Icacina trichantha Oliv. were evaluated using Allium cepa bioassay. Onion bulbs were exposed to various concentrations, 25–100% v/v, of the extract for 48–96 h for macroscopic and microscopic analyses of the onion roots. The extracts significantly inhibited the root growth of Allium cepa compared with the control in a concentration-dependent manner (P b 0.05) Also, photomicrographs revealed chromosomal aberrations ranging from chromosome laggard, vagrant, polar deviation, stickiness and bridges in the root tip cells of A. cepa. Similar studies in animal model are recommended for further evaluation of the use of I. trichantha leaf extract in human welfare.