Antiproliferative Effects of the Methanolic Extracts of Sideritis libanotica Labill. subsp. linearis (original) (raw)
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Evaluation of Various Biological Activities of Endemic Sideritis libanotica Extracts
NOTULAE SCIENTIA BIOLOGICAE
In recent years, using of plants to develop combine therapies for treatment of certain diseases such as cancer, Alzheimer's disease, and diabetes mellitus is extremely plausible approach. Perhaps, the definitive treatment of some of these diseases is hidden in the complex content of a plant in nature. Thus, in the present study, we decided to determine the biological activities of methanol and water extracts of the endemic Sideritis libanotica. To the best of our knowledge, the present study is the first investigation on antioxidant, enzyme inhibitory activity, antimicrobial activity, and in vitro cytotoxicity of S. libanotica. According to results, while the methanol extract shows better anti-cholinesterase, α-glucosidase, and α-amylase inhibition activity and cytotoxicity than the water extract, the tyrosinase inhibitory activity of the water extract was found to be better than the methanol extract. This study provides valuable information on how the biological activity of end...
Journal of Pharmaceutical and Biomedical Analysis, 2019
This study was geared towards assessing the possible antioxidant, enzyme inhibitory, and cytotoxic activities of ethyl acetate, methanol, and water extracts of Sideritis ozturkii Aytaç & Aksoy. The phytochemical profiles of the studied extracts were characterised by HPLC-MS/MS. The methanol extract, rich in phenolics (78.04 mg gallic acid equivalent/g), exhibited the strongest antioxidant activities. However, the ethyl acetate extract was the most active extract in the enzyme inhibitory assays. The water extract of S. ozturkii (1 mg/ml, 48 h incubation) slightly inhibited (22%) growth of human breast cancer cell line (MDA-MB-231 cells). On the other hand, the ethyl acetate and methanol extracts showed strong inhibition (98% and 97%, respectively) of MDA-MB-231 cells and caused apoptotic cell death. Scientific data generated from this study further appraises the multiple biological activities of plants belonging to the Sideritis genus. In addition, preliminary evidence gathered from the current investigation advocates for further studies geared towards the preparation of therapeutic formulations from S. ozturkii.
Of the phytochemical research performed to date on sideritis species
Serbian Journal of Experimental and Clinical Research, 2011
From a botanical perspective, the large number of species of the genus Sideritis coupled with the tendency to hybridise between the different species has prompted an accurate study designed to clarify all the controversial points in the botanical classification of this genus. The past phytochemical studies of the Sideritis species have been performed with different extracts from the aerial parts, essential oils and isolated compounds such as diterpenoids, flavonoids or phenylpropanoid glycosides. These investigations have justified the traditional uses for these plants and provided direction for new pharmacological research. In recent years, other compounds such as iridoids, coumarins, lignans and phenylpropanoid glycosides have also been isolated and identified. The results have shown that essential oils act as good antimicrobial agents against both Gram-positive and Gram-negative bacteria and against the Candida albicans fungus. Diterpenoids have shown antimicrobial, anti-inflammatory and antifeedant activity, and flavonoids are active as anti-ulcerous, anti-inflammatory and antioxidant agents. Future research should focus on the pharmacological activity of these isolated compounds to find new active principles and identify their mechanisms of action. In addition, it would be interesting to investigate new pharmacological activities apart from those used in traditional medicine; recent studies have shown that diterpenes and some diterpene derivatives act as effective anti-HIV and antiproliferative agents.
Cytotoxic activity and antioxidative properties of Sideritis scardica extracts
Planta Medica, 2008
The promising new source of therapeutic agents refers to plant secondary metabolites, irregularly occurring compounds that characterize certain plants or plant groups. There is continuously increasing interest in assessing the role of the phenolic compounds which show antioxidative properties and may act with beneficial health effects, reducing the risk of chronic diseases (inflammation, cancer, osteporosis, and cardiovascular diseases). Among them, flavonoids, as a large group of plant secondary metabolites, have been pro-duced in the plant for the purpose of protection from photosynthetic stress, reactive oxygen species (ROS), wounds, and herbivores. Studies of flavonoids have revealed the most compelling data for cytotoxic activities in various types of cancers, and several flavonoids have been shown to inhibit cancer development while exhibiting antioxidant activities in different animal models. Furthermore, some studies suggest that the most promising use of these compounds may be as an adjuvant to currently used therapies in antitumor treatment [1]. Abstract ! Sideritis scardica Griseb. (ironwort, mountain tea), an endemic plant of the Balkan Peninsula, has been used in traditional medicine in the treatment of gastrointestinal complaints, inflammation, and rheumatic disorders. This study aimed to evaluate its gastroprotective and anti-inflammatory activities. Besides, continuously increasing interest in assessing the role of the plant active constituents preventing the risk of cancer was a reason to make a detailed examination of the investigated ethanol, diethyl ether, ethyl acetate, and n-butanol extracts regarding cytotoxicity. Oral administration of the investigated extracts caused a dose-dependent anti-inflammatory effect in a model of carrageenan-induced rat paw edema. Gastroprotective activity of the extracts was investigated using an ethanol-induced acute stress ulcer in rats. The cytotoxic activity of plant extracts was assessed on PBMC, B16, and HL-60 cells and compared to the cytotoxicity of phenolic compounds identified in extracts. Apoptotic and necrotic cell death were analyzed by double staining with fluoresceinisothiocyanate (FITC)-conjugated annexin V and PI. The developed HPLC method enabled qualitative finger-print analysis of phenolic compounds in the investigated extracts. Compared to the effect of the positive control, the anti-inflammatory drug indomethacine (4 mg/kg), which produced a 50 % decrease in inflammation, diethyl ether and n-butanol extracts exhibited about the same effect in doses of 200 and 100 mg/kg (53.6 and 48.7 %; 48.4 and 49.9 %, respectively). All investigated extracts produced dose-dependent gastroprotective activity with the efficacy comparable to that of the reference drug ranitidine. The diethyl ether extract showed significant dose-dependent cytotoxicity on B16 cells and HL-60 cells, decreasing cell growth to 51.3 % and 77.5% of control, respectively, when used at 100 µg/mL. It seems that phenolic compounds (apigenin, luteolin, and their corresponding glycosides) are responsible for the diethyl ether extract cytotoxic effect. It also appears that induction of oxidative stress might be involved in its cytotoxicity, since B16 and HL-60 cells increased their ROS production in response to treatment with diethyl ether extract. Neither of the tested extracts nor any phenolic compounds showed significant cytotoxic effect to human PBMC. These results demonstrated the potent anti-inflammatory and gastroprotective activities, as well as the promising cytotoxicity.
Journal of Applied Pharmaceutical Science, 2015
The breast cancer is one of the most common types of cancer. Many scientists have focused on the treatment of this disease for a long time by studying anti-cancer activities of plant extracts as well as synthetics. Lamiaceae and Asteraceae have been used in anticancer studies due to their phytochemical content. The genus Sideritis, Achillea and Tanacetumare the members of these families. Sideritis, Achillea and Tanacetum are used as herbal medication for the treatment ofvariety of diseases. In present study, we demonstrated the biological activity of Sideritis syriaca (SS), Achillea aleppica (AAZ) and Tanacetum argenteum (TAA) methanol extracts on cell viability of the breast cancer line MCF7. MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay was used to determine the cell viability and proliferation of MCF7 cells. In a dose dependent manner, methanol extracts (0, 1, 5, 25, 100 and 250 µg/ml) of SS, AZZ and TAA were examined on MCF7, and viability of cells were determined with MTT staining. Especially, concentrations in 100 and 250 µg/ml of extracts decreased the cell viability (p<0.001). The results of the current study showed that methanol extracts of SS, AZZ and TAA effectively inhibited the cell proliferation by decreasing the cell viability of MCF7 cells. Suggesting that SS, AZZ and TAA can be considered as natural herbal-based anti-cancerous agents.
Extraction of biologically active compounds from Sideritis ssp. L
Food and Bioproducts Processing, 2011
In this study extraction of polyphenols and flavonoids from cultivated hybrid Sideritis scardica × Sideritis syriaca, known for its rich content of phenolics and flavonoids with antioxidant activity, was investigated. Extractions have been done by ethanol and water-ethanol, respectively. High equilibrium values of the extracted species were obtained-17.55 mg/(g solid) total phenolics and 5.7 mg/(g solid) total flavonoids with ethanol as solvent. The influence of the solvent on the total yield and the content of biologically active compounds were studied. Maximum polyphenolics and flavonoids extraction was observed for water-ethanol solvent ratio 20/80. Increase of the content of ethanol in the solvents led to lower total yield of extracts but higher percentage of polyphenolics. The extraction kinetics showed that 90% of the phenolic compounds were extracted during the first 2.5 h. The experimental kinetics was described by a constant effective diffusion coefficient D e = 1.5 × 10 −12 m 2 /s in the solid, accounting for the actual particle size distribution.
Phytochemical Study of a Species with Ethnopharmacological Interest: Sideritis romana L
European Journal of Medicinal Plants, 2016
The phytochemical analysis of Sideritis romana L., a species largely used as a traditional remedy, led to the isolation and the identification of several acetylated flavonoid glycosides with apigenin, luteolin, hypolaetin and isoscutellarein backbone. Among these, an apigenin derivative (2) was recognized for the first time in Sideritis as well as in the Lamiaceae family. The iridoidic pattern of this species showed the presence of harpagide, currently considered the main taxonomical maker in this genus, together with 6-deoxyharpagide which is a rare compound since it was previously recognized in a limited number of species of Lamiaceae. Other identified iridoids were ajugoside and bartsioside, the latter recognized for the first time in the species as well as in the family. Acetylated flavonoid glycosides and iridoid glucosides are considered of chemotaxonomic relevance in several genera comprised in the Lamioideae subfamily and the occurrence of both of these classes of compounds in S. romana was discussed. The co-presence of the acetylated Original Research Article
Biological activities of the extracts of two endemic Sideritis species in Turkey
Innovative Food Science & Emerging Technologies, 2008
It has long been known that herbs and their extracts have an antimicrobial activity. Sideritis ozturkii Aytac & Aksoy and Sideritis caesarea Duman, Aytaç et Baser endemic plant species for Turkey have been traditionally used as medicinal tea and spice in different regions of Turkey especially the Mediterranean and the middle part of Anatolia. In this study, total phenolic, flavanol and flavonol compounds of the methanolic extracts of S. ozturkii and S. caesarea, and their antimicrobial and antioxidant effects were determined. Total phenolics and total flavonol contents of S. caesarea extract were higher than those of S. ozturkii extract. Antioxidant activities of the extracts tested by the DPPH radical scavenging system were 41.68 ± 1.96% and 72.47 ± 0.73% at 100 ppm concentration of S. ozturkii and S. caesarea extracts, respectively. Antimicrobial activity was assessed by the agar diffusion method against fifteen microorganisms. In conclusion, it can be said that the extracts of S. ozturkii and S. caesarea could be used as natural antimicrobial and antioxidant agents in the food preservation and human health.
Antioxidant Properties and Phenolic Composition of Sideritis Species
Chemistry of Natural Compounds, 2004
The antioxidant properties and phenolic composition of 27 Sideritis species were studied. Plant samples were extracted with petroleum ether using a Soxhlet apparatus. The defatted plant materials were extracted with 70% methanol. Antioxidant activities of the extracts were measured using Fe+2 induced linoleic acid peroxidation, as indicated by thiobarbituric acid reactive substance (TBARS) production. Free radical scavenging activities were determined based on 1,1-diphenyl-2-picrylhydrazyl radical (DPPH). Results were compared with standard BHT. Total phenol concentration of the extracts was estimated with Folin-Ciocalteu reagent using gallic acid as standard, and phenolic components were quantified by HPLC-DAD.