Isolation and quantification of pinitol in Argyrolobium roseum plant, by 1H-NMR

Chemical investigations on ethanolic extract of Argyrolobium roseum led to the isolation of Pinitol as the major constituent of the plant. Pinitol is chemically known as 3-O-methyl-D-Chiro-inositol and has been found to possess anti-diabetic activity. It helps in the regeneration of beta cells, present in the areas of the pancreas called as islets – of Langerhans. These cells make and release insulin, a hormone which controls the level of glucose in the blood. Pinitol was isolated from the ethanolic extract of the plant and a sensitive & reliable method, based on Proton Nuclear Magnetic Resonance (PNMR), was developed and used as an analytical tool for quantification and identification of this relatively UV insensitive compound in the alcoholic extract of the plant. The method involves the use of pyrazinamide (an anti-tuberculosis drug), as a reference. Validation of the method was carried out by preparing a known concentration of an artificial mixture of pinitol and pyrazinamide. The recovery of pinitol in the mixture was in the range of 98.5–101.3%. Pinitol in pure form was isolated from the ethanolic extract of A. roseum by repeated column chromatography over silica gel followed by crystallization in methanol. Pinitol isolated from the plant was identified on the basis of 1H-NMR, 13C-NMR, DEPT (45°, 90° and 135°) experiments and mass spectral data. The method was successfully applied for the quantitation of pinitol in various extracts of the said plant

A New Glycoside, 3-o-Demethylcolchicine-3-o-α-d-Glucopyranoside, fromGloriosa SuperbaSeeds

A new colchicine glycoside, 3-O-demethylcolchicine-3-O-a-~-glucopyranosidhea,s been isolated from Gloriosa superba seeds. The assigned structure has been corroborated by spectroscopic data and enzymatic hydrolysis

6α,7α-epoxy-5α,17α,dihydroxy-1-oxo-22R-witha-2,24-dienolide in leaves of Withania somnifera: Isolation and its crystal structure

6α,7α-epoxy-5α,17α,dihydroxy-1-oxo-22R-witha-2,24-dienolide (C28H38O6) was isolated from Withania somnifera leaves. The structure of the withanolide was established by spectral analysis and X-ray diffraction studies as withanone. The compound crystallizes in the orthorhombic space group P212121 with unit cell parameters: a=9.191(10) A° , b=12.858(6) A° , c=21.400(16) A° , Z=4. The crystal structure was solved by direct methods and refined to R=0.0603 for 1742 observed reflections. There is positional disorder of the H atom in a hydroxy group (O5), resulting in two possible hydrogen-bond linkages. All the rings of the steroid skeleton are trans connected. Ring A exists in a half-chair conformation, ring B is intermediate between a half-chair and a sofa, ring C a distorted chair, and five-membered ring D is intermediate between a half-chair and an envelope. The δ-lactone ring E adopts a sofa conformation. The twist along the length of the steroid nucleus is negligible [C19–C10. . .C13–C18=1.8◦]. Both the hydroxy groups are involved in hydrogen bonding

Ameliorative Effect of Hydroethanolic Leaf Extract of Byrsocarpus coccineus in Alcohol- and Sucrose-Induced Hypertension in Rats

Hypertension remains a major health problem worldwide considering the prevalence of morbidity and mortality. Plants remain a reliable source of efficacious and better tolerated drugs and botanicals. This study was designed to investigate the effect of the chemo-profiled hydroethanolic leaf extract of Byrsocarpus coccineus in ethanol- and sucrose-induced hypertension. Groups of rats were treated orally (p.o.) with distilled water (10 ml/kg), ethanol (35%; 3 g/kg), sucrose (5-7%), and B. coccineus (100, 200, and 400 mg/kg), and nifedipine together with ethanol and sucrose separately for 8 weeks. At the end of the treatment period, blood pressure and heart rate of rats were determined. Blood was collected for serum biochemical parameters and lipid profile assessment, and the liver, aorta, kidney, and heart were harvested for estimation of in vivo antioxidants and malondialdehyde (MDA). Results obtained in this study showed that B. coccineus at the various doses administered reduced the systolic, diastolic, and arterial blood pressure elevated by ethanol and sucrose. Also, the extract reversed the reduction in catalase (CAT), reduced glutathione (GSH), glutathione peroxidase (GPx), and superoxide dismutase (SOD) induced by ethanol and sucrose. The level of MDA was reduced compared to the ethanol- and sucrose-induced hypertensive group. With respect to lipid profile, administration of B. coccineus at the various doses reduced the levels of triglycerides, low-density lipoprotein (LDL), cholesterol, and atherogenic indices, compared to the ethanol and sucrose groups. In conclusion the hydroethanolic leaf extract of B. coccineus exerted significant antihypertensive effect and this is probably related to the antioxidant property and improvement of lipid profile observed in this study

Effect of Emblica officinalis (fruit) against UVB-induced photo-aging in human skin fibroblasts

Ethnopharmacological relevance: Emblica officinalis fruit (EO), commonly known as Amla is a reputed traditional medicine and functional food used in Indian subcontinent. It has long been used in Indian folk medicine to treat liver diseases, stomach ulcers, inflammatory diseases, metabolic disorders, geriatric complaints, skin disorders and beauty care.Aim of the study: Recently, it has been shown to promote pro-collagen content and inhibit matrix metalloproteinase levels in skin fibroblast. The aim of the present study was to investigate the efficacy of EO to inhibit UVB-induced photo-aging in human skin fibroblasts.Materials and methods: Mitochondrial activity of human skin fibroblasts was measured by MTT-assay. Quantifications of pro-collagen 1 and matrix metalloproteinase 1 (MMP-1) release were performed by immunoassay techniques. Hyaluronidase inhibition assay was studied in vitro using bovine testicular hyaluronidase and human umbilical cord hyaluronic acid. Cell cycle analysis was performed by flowcytometry using propidium iodide. Results: EO stimulated, the otherwise UVB inhibited cellular proliferation and protected pro-collagen 1 against UVB-induced depletion via inhibition of UVB-induced MMP-1 in skin fibroblasts (10–40�g/mL,p > 0.001). EO exhibited inhibitory activity of hyaluronidase (10–40�g/mL, p > 0.001). Treatment with EO also prevented UVB disturbed cell cycle to normal phase. Conclusion: The results of the present study suggests that EO effectively inhibits UVB-induced photoaging in human skin fibroblast via its strong ROS scavenging ability and its therapeutic and cosmetic applications remain to be explored

Development and Validation of a RP-HPLC Method for the Simultaneous Determination of Rifampicin and a Flavonoid Glycoside - A Novel Bioavailability Enhancer of Rifampicin

Purpose: To develop and validate a sensitive HPLC method for the separation and simultaneous estimation of two ingredients in a composition comprising of rifampicin and a flavonoid glycoside (an enhancer of oral bioavailability of rifampicin). Methods: Reverse phase (RP) chromatographic separation and estimation was achieved using a Shimadzu HPLC system. RP-18 column was used at the following optimised conditions: mobile phase, acetonitrile:phosphate buffer, 50 mM, pH 5.0 in a ratio of 60:40 v/v; oven temperature, 40 °C; flow rate, 0.8 ml min-1; detection wavelength, 340 nm; and total run time, 15 min. Results: The developed method was validated in terms of linearity, range, accuracy, precision, limit of detection, limit of quantification, robustness and specificity. Good linearity was observed (r2 > 0.999) over the study range of both ingredients. The precision values for rifampicin and the flavonoid glycoside were in the range 1.08-2.77 and 1.14-2.98 %, respectively, while the limit of quantification was 0.10 and 0.05μg mL-1 respectively. The method was found to be robust and specific for both ingredients. Conclusion: The developed method has a potential application in preclinical and clinical studies

Synthesis and biological evaluation of pyrrole-based chalcones as CYP1 enzyme inhibitors, for possible prevention of cancer and overcoming cisplatin resistance

© 2017 Elsevier Ltd Inhibitors of CYP1 enzymes may play vital roles in the prevention of cancer and overcoming chemo-resistance to anticancer drugs. In this letter, we report synthesis of twenty-three pyrrole based heterocyclic chalcones which were screened for inhibition of CYP1 isoforms. Compound 3n potently inhibited CYP1B1 with an IC50 of ∼0.2μM in Sacchrosomes™ and CYP1B1-expressing live human cells. However, compound 3j which inhibited both CYP1A1 and CYP1B1 with an IC50 of ∼0.9µM, using the same systems, also potently antagonized B[a]P-mediated induction of AhR signaling in yeast (IC50, 1.5µM), fully protected human cells from B[a]P toxicity and completely reversed cisplatin resistance in human cells that overexpress CYP1B1 by restoring cisplatin's cytotoxicity. Molecular modeling studies were performed to rationalize the observed potency and selectivity of enzyme inhibition by compounds 3j and 3n

In Vitro and In Vivo Anticancer Activity of Root Extracts of Sansevieria liberica Gerome and Labroy (Agavaceae)

Introduction. Sansevieria liberica Gerome and Labroy (Agavaceae) is a perennial plant widely distributed in tropical Africa. Preparations of the plant are commonly used across Nigeria for the treatment of inflammatory conditions. Based on the fact that herbal medicine is a strong component of integrative medicine, this study was conducted to evaluate the anticancer activity of root extracts of Sansevieria liberica. Methods. Sulforhodamine B (SRB) in vitro cytotoxicity assay, Sarcoma-180 (S-180) ascites and solid tumor, and L1210 lymphoid leukemia in vivo models were used in this study. Results. SL-A002 (IC50 23 µg/mL with HeLa), SL-A003 (IC50 22 µg/mL with HCT-116), and SL-A004 (IC50 23 and 18 µg/mL with A549 and THP-1, resp.) demonstrated significant activity in the SRB cytotoxicity assay. Potency was highest with the following pairs of extract : cancer cell line: SL-A002 : HeLa (IC50 23 µg/mL), SL-A003 : HCT-116 (IC50 22 µg/mL), and SL-A004 : THP-1 (IC50 18 µg/mL). SL-A002 demonstrated significant dose-dependent antitumor activity in the Sarcoma-180 (S-180) ascites model with peak effect produced at the dose of 120 mg/kg (i.p.) with inhibition of 89.36% compared to 97.96% for 5-FU (20 mg/kg i.p.). The inhibition of tumor growth by SL-A002 in the S-180 solid tumor model was 47.40% compared to a value of 50.18% for 5-FU. SL-A002 was also significantly active in the L1210 lymphoid leukemia model with 158.33% increase in mean survival time, the same value for 5-FU. Conclusions. The hydroethanolic extract of Sansevieria liberica, SL-A002, possesses significant anticancer activity to warrant further extensive study to identify, isolate, and characterize the specific bioactive molecules responsible for the observed antitumor activity and the precise mechanism(s) of action

Potential herb-drug interaction of a flavone glycoside from <em>Cuminum cyminum</em>: Possible pathway for bioenhancement of rifampicin

776-782Traditional knowledge on classical herbal based Ayurvedic formulation namely ‘Trikatu’ in the Indian system of medicine has led to the discovery of ‘Risorine’, a world’s first boosted rifampicin in combination with piperine (one of ingredient in Trikatu) as bioenhancer for the treatment of tuberculosis. This encourages us to combine rifampicin with a flavone glycoside (CC-I), one of ingredient of Cuminum cyminum which found its application in culinary purposes and immensely widespread in diverse ethnomedical systems worldwide as an integral part of folklore therapy. Therefore, aim of the study is to explore the reason for bioenhancement of rifampicin by CC-I using a panel of in vitro and in vivo experimentations for the first time. Plasma concentration of rifampicin was markedly enhanced by CC-I orally in Wistar rats. Mechanistic studies showed that CC-I have action on efflux transporters based on rhodamine transport and P-glycoprotein dependent ATPase assay but no alteration of in vitro transcellular diffusion and plasma protein binding of rifampicin. Intestinal transit of rat was not affected upon treatment with CC-I whereas inhibition of CYP3A4 in rat and human liver microsomes was occurred to a little extent. Bioenhancer effect of CC-I was mainly through improving absorption by down regulation of efflux transporters

Development and Validation of a RP-HPLC Method for the Simultaneous Determination of Rifampicin and a Flavonoid Glycoside - A Novel Bioavailability Enhancer of Rifampicin

Purpose: To develop and validate a sensitive HPLC method for the separation and simultaneous estimation of two ingredients in a composition comprising of rifampicin and a flavonoid glycoside (an enhancer of oral bioavailability of rifampicin). Methods: Reverse phase (RP) chromatographic separation and estimation was achieved using a Shimadzu HPLC system. RP-18 column was used at the following optimised conditions: mobile phase, acetonitrile:phosphate buffer, 50 mM, pH 5.0 in a ratio of 60:40 v/v; oven temperature, 40 °C; flow rate, 0.8 ml min-1; detection wavelength, 340 nm; and total run time, 15 min. Results: The developed method was validated in terms of linearity, range, accuracy, precision, limit of detection, limit of quantification, robustness and specificity. Good linearity was observed (r2 > 0.999) over the study range of both ingredients. The precision values for rifampicin and the flavonoid glycoside were in the range 1.08-2.77 and 1.14-2.98 %, respectively, while the limit of quantification was 0.10 and 0.05μg mL-1 respectively. The method was found to be robust and specific for both ingredients. Conclusion: The developed method has a potential application in preclinical and clinical studies