ABSTRACT
<p><b>OBJECTIVE</b>To isolate and characterize the cytotoxic compounds from Diospyros quercina (Baill.) G.E. Schatz & Lowry (Ebenaceae).</p><p><b>METHODS</b>An ethno-botanical survey was conducted in the south of Madagascar from July to August 2010. Bio-guided fractionation assay was carried out on the root bark of Diospyros quercina, using cytotoxicity bioassay on murine P388 leukemia cell lines as model. The structures of the cytotoxic compounds were elucidated by 1D and 2D NMR spectroscopy and mass spectrometry.</p><p><b>RESULTS</b>Biological experiments resulted in the isolation of three bioactive pure compounds (named TR-21, TR-22, and TR-23) which exhibited very good in vitro cytotoxic activities with the IC50 values of (0.017 5±0.0060) µg/mL, (0.089±0.005) µg/mL and (1.027±0.070) µg/mL respectively. Thus, they support the claims of traditional healers and suggest the possible correlation between the chemical composition of this plant and its wide use in Malagasy folk medicine to treat cancer.</p><p><b>CONCLUSIONS</b>The ability of isolated compounds in this study to inhibit cell growth may represent a rational explanation for the use of Diospyros quercina root bark in treating cancer by Malagasy traditional healers. Further studies are, therefore, necessary to evaluate the in vivo anti-neoplastic activity of these cytotoxic compounds as effective anticancer drugs.</p>
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Objective: To perform phytochemical analyses on the leaves of Ocimum basilicum L. (O. basilicum), to elucidate the structure of isolate and then perform the antisickling activity on the crude extract and on the isolate. Methods:The Emmel test performed on the acidified methanolic extract of this plant was used to evaluate the antisickling activity. The structure characterization of the active compound was performed using chromatographic techniques for the separation and the spectroscopic ones for structure elucidation (1H-NMR, 13C-NMR, COSY, HMBC). Results: The chemical screening on the crude extract revealed the presence of polyphenols (flavonoids, anthocyanins, leucoanthocyanins, tannins, quinones) alkaloids, saponins, triterpenoids and steroids. The obtained extract after evaporation yielded 34.50 g (11.5%) out of 300 g of powdered leaves of O. basilicum. The acidified methanolic extract and butyl stearate showed an interesting antisickling activity. Conclusions:The acidified methanolic extract and butyl stearate from O. basilicum displayed a good antisickling activity. To the best of our knowledge, this is the first time to report the antisickling activity of this compound in this plant. The synthesized compound presented the same spectroscopic characteristics than the natural one and the antisickling activities of its derivatives are understudying.
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Objective: To verify the antidiabetic activity of leaf extracts from Physalis peruviana L. popularly used in the Eastern part of the Democratic Republic of the Congo and to point out the possible toxicity.Method:pigs at the dose range of 100 mg/kg to 3.2 g/kg of body weight. The hypoglycemic activity was evaluated by glucose tolerance test, loading animals with glucose 4 g/kg and measuring blood glucose concentrations at various times. The effect was compared to the control and glibenclamide as antidiabetic reference drug. Acute toxicity was evaluated by recording mortality rate, changes on blood biomarkers and damage caused to vital organs.Results:At a dose of 100 mg/kg, the aqueous extract induced a significant reduction of peak Aqueous decoctions prepared from dried leaves powder were administrated to guinea concentration at 30 min after glucose loading as compared with control or reference (P<0.05). At doses greater than 400 mg, some alterations on blood, kidney and liver markers were observed. Upper 800 mg/kg, mortality was observed with LD50 estimated at about 1280 mg/kg. At the autopsy, vital organs were in haemorrhage and swelling state.Conclusion:The crude aqueous extracts from the leaves of Physalis peruviana L. present hypoglycemic activity in animal model, but at high doses the plant may cause severe intoxication.