Bioenhancing effects of naringin on atorvastatin.

Naringin (CAS no: 10236-47-2) is a flavonone glycoside obtained from Citrus paradisi (grapefruit), a natural bioenhancer and reported to enhance the bioavailability of drugs by inhibiting cytochrome P450 and P-glycoprotein (P-gp). The aim of the present study was to investigate the effect of naringin on antihyperlipidemic properties of atorvastatin (AST) in tyloxapol induced hyperlipidemic rats and the effects were supported with measurement of plasma concentrations of AST by HPLC method. Animals received AST along with naringin (15 and 30 mg/kg) shown higher percent reduction in both cholesterol and triglycerides levels, when compared to animals received AST alone at dose of 25 and 50 mg/kg and it was found that the higher percent reduction in cholesterol and triglycerides was proportional to increase in plasma concentration of AST. From the results it is evident that the co-administration of naringin along with AST increased the plasma concentration of AST. The findings of the present study confirmed that naringin could be used as bioenhancer. The co-administration of AST and the diet with naringin (grapefruit) to the patients may potentiate the therapeutic efficacy of AST.

Scientific evidence for traditional claim of anti-obesity activity of Tecomella undulata bark.

ETHNOPHARMACOLOGICAL RELEVANCE: The bark of Tecomella undulata is traditionally claimed in the treatment of various disease ailments including obesity and cancer. Till now there are no studies about anti-obesity activity of Tecomella undulata bark. AIM OF THE STUDY: The present study was aimed to establish a scientific evidence for anti-obesity efficiency of ethyl acetate extract of Tecomella undulata bark (EATUB). Further to standardize the active fractions of EATUB using different biomarkers. MATERIALS AND METHODS: We investigated activity of EATUB fractions (F1-F7) using 3T3-L1 fibroblasts. Further, F1-mediated effects were characterized by determining mRNA and protein levels of SIRT1, one of the key targets for the treatment of obesity, using semi-quantitative RT-PCR (sqRT-PCR) and western blot analysis. The consequences of modulation of SIRT1 on mRNA and protein levels of various adipogenesis mediators like PPARγ, C/EBPα, E2F1, leptin, adiponectin and LPL were also studied. In vivo studies were performed using High Fat Diet (HFD) obese mice. RESULTS: Our data showed that compared to controls, preadipocytes and adipocytes incubated with F1 exhibited a significant decrease in adipogenesis and lipogenesis. In addition, sqRT-PCR and western blot analysis showed significant increase in SIRT1 and adiponectin levels and decrease in PPARγ, C/EBPα, E2F1, leptin and LPL levels in preadipocytes and adipocytes. In vivo studies of F1 in HFD induced obese mice showed significant improvement in lipid profile and glucose levels. The bioactive fraction (F1) was determined to possess 4.95% of ferulic acid. CONCLUSION: Thus, our findings signified the beneficial effects of Tecomella undulata bark in pharmacologic interventions related to obesity and metabolic disorders. Ferulic acid and rutin are being reported and quantified for the first time from the bark of Tecomella undulata.

Anticancer activity of Pupalia lappacea on chronic myeloid leukemia K562 cells.

BACKGROUND: Cancer is one of the most prominent human diseases which has enthused scientific and commercial interest in the discovery of newer anticancer agents from natural sources. Here we demonstrated the anticancer activity of ethanolic extract of aerial parts of Pupalia lappacea (L) Juss (Amaranthaceae) (EAPL) on Chronic Myeloid Leukemia K562 cells. METHODS: Antiproliferative activity of EAPL was determined by MTT assay using carvacrol as a positive control. Induction of apoptosis was studied by annexin V, mitochondrial membrane potential, caspase activation and cell cycle analysis using flow cytometer and modulation in protein levels of p53, PCNA, Bax and Bcl2 ratio, cytochrome c and cleavage of PARP were studied by Western blot analysis. The standardization of the extract was performed through reverse phase-HPLC using Rutin as biomarker. RESULTS: The results showed dose dependent decrease in growth of K562 cells with an IC50 of 40 ± 0.01 µg/ml by EAPL. Induction of apoptosis by EAPL was dose dependent with the activation of p53, inhibition of PCNA, decrease in Bcl2/Bax ratio, decrease in the mitochondrial membrane potential resulting in release of cytochrome c, activation of multicaspase and cleavage of PARP. Further HPLC standardization of EAPL showed presence 0.024% of Rutin. CONCLUSION: Present study significantly demonstrates anticancer activity of EAPL on Chronic Myeloid Leukemia (K562) cells which can lead to potential therapeutic agent in treating cancer. Rutin, a known anti cancer compound is being reported and quantified for the first time from EAPL.

Antiproliferative activity and standardization of Tecomella undulata bark extract on K562 cells.

ETHNOPHARMACOLOGICAL RELEVANCE: The bark of Tecomella undulata is primarily used in the treatment of syphilis, painful swellings and cancer by traditional healers. Also, it is claimed to be useful in treating urinary discharges, enlargement of spleen, leucorrhoea, leukoderma, tumors, liver disorders, gonorrhea, gout and promotes wound healing in Indian traditional system of medicine. AIM: To establish a scientific validation for the antitumor effects of Tecomella undulata bark and explore the mechanistic pathway in chronic myeloid leukemia cell line, K562. The study was further extended to standardize the extract using quercetin as biomarker. METHODS: Induction of apoptosis by chloroform extract of Tecomella undulata bark (CTUB) was determined by MTT, Annexin V and caspase activation assays. The cell cycle analysis was done by flow cytometer and nuclear staining by DAPI. The standardization of the extract was performed through reverse phase-HPLC method under PDA detection. RESULT: Results clearly showed the induction of apoptosis by CTUB in K562 cells. The effect was found to be dose dependent, having IC(50) of 30 µg/ml with activation of FAS, FADD, caspase 8, caspase 3/7 and fragmentation of DNA. The bioactive CTUB was determined to possess 0.03% (w/w) of quercetin. CONCLUSION: The investigation clearly demonstrated the potential antitumor effect of CTUB, thereby validating the traditional claim. Quercetin, known to have anticancer activity is being reported and quantified for the first time from the bark of Tecomella undulata.