Crispene E, a new clerodane-type diterpene, inhibited STAT3 dimerization in a cell-free fluorescent polarisation assay and was found to have significant toxicity against STAT3-dependent MDA-MB 231 breast cancer cell line and selectively inhibited the expression of STAT3 and STAT3 target genes cyclin D1, Fascin and bcl-2. Molecular docking studies suggest the molecule inhibits STAT3 by interacting with its SH2 domain. The compound has been isolated from Tinospora crispa and characterized using standard spectroscopic techniques.
This study was designed to identify some bioactive phytochemicals from ethanolic extract of roots of Litsea polyantha and to evaluate some of its pharmacological activities. Phytochemical tests indicated the presence of reducing sugar, combined reducing sugar, tannins, flavonoids, alkaloids, terpenoids, and phenol. In the antioxidant assay using 2-diphenyl-1-picryl-hydrazyl (DPPH) free radical scavenging method, the IC50 value was found to be 82.31 μg/mL. Total content of phenolic compounds, flavonoid, and tannin was found to be 152.69 mg GAE/gm, 85.60 mg QE/gm, and 77.22 mg GAE/gm of dry extract, respectively. In disc diffusion antibacterial assay, the extract exhibited highest zone of inhibition up to 12.25 mm against Escherichia coli at the concentration of 500 μg/disc. For brine shrimp lethality bioassay, the extract exhibited LC50 56.082 μg/mL. In in vivo antihyperglycemic activity test by oral glucose tolerance test using Swiss Albino mice at the oral dose of 250 and 500 mg/kg, the extract showed statistically significant antihyperglycemic effect. Finally, in vivo, the extract exhibited the dose dependent CNS depressant effects by reducing the locomotors of Swiss Albino mice which was confirmed through three different neuropharmacological activity tests such as open field, hole cross, and hole board test.
Background: In folk medicine leaves and stem of Bruguiera gymnorrhiza (L.) are commonly used to treat diarrhea, fever, diabetes, pain and a number of ailments. The present study was carried out to explore antioxidant, analgesic and antidiarrhoeal activities of ethanol extract of leaves and stem of B. gymnorrhiza and also to analyze its major bioactive natural polyphenols by HPLC-DAD. Methods: Total polyphenol content was spectrophotometrically determined using Folin Chiocalteu's reagent while the flavonoids by aluminum chloride colorimetric assay. Antioxidant activity was determined by DPPH free radical scavenging, reducing power, nitric oxide and hydrogen peroxide scavenging assays. Identification and quantification of bioactive polyphenols were done by HPLC-DAD method. Antidiarrhoeal activity of the extracts was evaluated using experimentally castor oil induced diarrhea in mice. Acetic acid induced writhing method was used to evaluate the analgesic activity. Acute oral toxicity and brine shrimp lethality assay were performed to check the cytotoxic potential. Results: Both the leave and stem extracts contain significant amount of phenolic and flvonoid content. Extracts showed DPPH radical scavenging, nitric oxide, hydrogen peroxide scavenging and also concentration dependent reducing power activity. HPLC analysis of both extract indicated the presence of significant amount of vanillic acid along with other phenolic constituents. Both extracts showed significant (P < 0.01) analgesic and antidiarrhoeal activity. Furthermore, extracts showed negligible toxic effect. Conclusion: Along with other phenolic compounds, vanillic acid present in the extract may be responsible for antioxidant, analgesic and antidiarrhoeal activities. Altogether these results rationalize the use of this plant in traditional medicine.
A simple, specific, accurate and stability-indicating high performance liquid chromatographic method was developed and validated for the determination of Epinastine Hydrochloride in pharmaceutical dosage form. The chromatographic conditions comprised of a reverse-phase, C18 column (150×4.6 mm), 5μm with a mobile phase consisting of a mixture of aqueous phase (3.8g of sodium pantanesulphonate monohydrate and 4.0g of potassium dihydrogen orthophosphate was dissolved in 1L of water and pH of solution was adjusted to 4.5 with o-phosphoric acid) and organic phase (acetonitrile and methanol was mixed in the ratio of 4:1 v/v) in the ratio of 60:40 v/v at a flow rate of 1.0ml/min. Detection was carried out at 220nm. The retention time of Epinastine Hydrochloride was found to be 3.5 min. The calibration curve was found linear between 2-200μg/ml. The percentage recoveries of Epinastine Hydrochloride were found to be in the range of 99.05-100.50%. The method was validated for accuracy, linearity, precision, detection limit, quantitation limit and robustness. The drug was subjected to acidic hydrolysis, basic hydrolysis, neutral hydrolysis, oxidation, photochemical and thermal degradation. All the peaks of degraded product were resolved from the active pharmaceutical ingredient with significantly different retention time. As the method could effectively separate the drug from its degradation product, it can be employed as a stability indicating one. Key Words: Epinastine hydrochloride; validation; stability indicating method; HPLC; dosage form. DOI: http://dx.doi.org/10.3329/icpj.v1i3.9662 International Current Pharmaceutical Journal 2012, 1(3): 50-55
Plants are the major source of therapeutic compounds and have huge applications in Pharma Industry. To identify new sources of therapeutic compounds, we studied acute toxicity, antihyperglycemic, anti-inflammatory, and anticoagulant activities of the polar and nonpolar fractions of Justicia aurea (J. aurea). Our initial phytochemical screening of J. aurea exhibited the presence of numerous secondary metabolites such as reducing sugars, glycosides, tannins, gums, alkaloids, phenolic compounds, and carbohydrates which might be primarily responsible for its medicinal properties. In the acute toxicity test, the result showed no toxicity up to 2000 mg/kg. In the antihyperglycemic activity test, administration of petroleum ether fraction and water fraction of J. aurea extract to glucoseloaded mice at 250 and 500 mg/kg body weight (BW) reduced the blood glucose levels compared to control mice. Between two fractions, the water fraction was found to exhibit better potentiality at 500 mg/kg BW. In the anti-inflammatory assay, at 250 and 500 mg/kg water fraction exhibited anti-inflammation by 20.00% and 31.67%, respectively and petroleum ether fraction by 13.33% and 18.00%, respectively. In anticoagulant activity, the test indicated that water fraction has minor anticoagulant potentiality compared to control. In conclusion, the polar water fraction shows better medicinal properties than the nonpolar petroleum ether fraction of J. aurea.
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