Devinder Kumar Gupta

Terminalia chebula (fruit) prevents liver toxicity caused by sub-chronic administration of rifampicin, isoniazid and pyrazinamide in combination.

Terminalia chebula Gertn. (Combetraceae) is an important herbal drug in Ayurvedic pharmacopea. In the present study, a 95% ethanolic extract of T. chebula (fruit) (TC extract), which was chemically characterized on the basis of chebuloside II as a marker, was investigated for hepatoprotective activity against anti-tuberculosis (anti-TB) drug-induced toxicity. TC extract was found to prevent the hepatotoxicity caused by the administration of rifampicin (RIF), isoniazid (INH) and pyrazinamide (PZA) (in combination) in a sub-chronic mode (12 weeks). The hepatoprotective effect of TC extract could be attributed to its prominent anti-oxidative and membrane stabilizing activities. The changes in biochemical observations were supported by histological profile.

Hepatoprotective activity of Woodfordia fruticosa Kurz flowers against carbon tetrachloride induced hepatotoxicity

ETHNOPHARMACOLOGICAL RELEVANCE Dried flowers of Woodfordia fruticosa Kurz. Family Lythraceae are used in variety of diseases in traditional Indian system of medicine including hepatic ailments. AIMS OF STUDY The aim of present study was to validate hepatoprotective activity of flowers of Woodfordia fruticosa Kurz. MATERIALS AND METHODS Petroleum ether (WF1), chloroform (WF2), ethyl alcohol (WF3) and aqueous (WF4) extracts of the flowers of Woodfordia fruticosa were evaluated for hepatoprotective activity against carbon tetrachloride induced hepatotoxicity using biochemical markers, hexobarbitone sleep time, bromosulphalein (BSP) clearance test and effect on bile flow and bile solids. RESULTS The aqueous extract (WF4) was most potent among the four extracts studied in detail. WF4 showed significant hepatoprotective activity against carbon tetrachloride induced hepatotoxicity as evident by restoration of serum transaminases, alkaline phosphatase, bilirubin and triglycerides. The restoration of microsomal aniline hydroxylase and amidopyrine-N-demethylase activities indicated the improvement in functional status of endoplasmic reticulum. Restoration of lipid peroxidation and glutathione contents suggests the antioxidant property of WF4. The recovery in bromosulphalein clearance and stimulation of bile flow suggested the improved excretory and secretary capacity of hepatocytes. Light microscopy of the liver tissue further confirmed the reversal of damage induced by hepatotoxin. CONCLUSION Present study showed that the aqueous extract of Woodfordia fruticosa significantly restores physiological integrity of hepatocytes. WF4 did not show any sign of toxicity up to oral dose of 2g/kg in mice.

Synthesis and biologic activities of some novel heterocyclic chalcone derivatives

We synthesized 36 chalcone-like (E)-3-(substitutedphenyl)-1-hetrylprop-2-en-1-ones by condensing 2-acetylfuran/2-acetylpyrrole with substituted benzaldehydes under basic conditions. Of the 36 molecules synthesized, 10 are new to the literature. Bio-evaluation studies of these molecules revealed that compounds 5, 9, 15, 25, and 29 were potent NorA efflux pump inhibitors against Staphylococcus aureus by reducing MIC of ciprofloxacin fourfold, while compounds 11, 21, 25, and 26 showed promising anticancer activity in all four tested cancer cell lines (HL-60, MOLT-4, PC-3, and HeLa). Compound 25 emerged as a very good potentiator of ciprofloxacin against multidrug resistant S. aureus and also showed promising anticancer activity. The present communication describes syntheses, bio-evaluation, and structure-related activity of the (E)-3-(substitutedphenyl)-1-hetrylprop-2-en-1-ones.

EXTRACTION STUDIES OF PODOPHYLLUM HEXANDRUM USING CONVENTIONAL AND NONCONVENTIONAL METHODS BY HPLC–UV–DAD

The composition of lignans extracted from Podophyllum hexandrum rhizomes was studied by sequential extraction with supercritical CO2, ethyl acetate modified CO2 and methanol modified CO2. The results were compared with the extracts obtained by Accelerated Solvent Extraction (ASE) and soxhlets methods. The lignan contents comprised of Podophyllotoxin, deoxypodophyllotoxin, 4′-demethylpodophyllotoxin, Picropodophyllotoxin, Isopicropodophyllotoxin, Podophllotoxin-β-D-glucopyranoside, and 4′-demethylpodophyllotoxin β-D-glucopyranoside in the extracts of Podophyllum hexandrum rhizomes obtained by different methods was studied. There was a variation in the concentration of lignan in the extracts obtained by different methods of extraction. Podophyllotoxin formed the major component (36.55%) of the extract obtained by SFE and picropodophyllotoxin, isopicropodophyllotoxin, deoxypodophyllotoxin, and 4′-demethylpodophyllotoxin were present in 6.82, 1.51, 1.46, and 0.85%, respectively, whereas 4′-demethylpodophyllotoxin β-D-glucopyranoside was 1.89% in the extract obtained by ASE, which is higher than SFE extracts. Soxhlets derived extract contains better concentration of isopicropodophyllotoxin (24.49%) than SFE. A simple, isocratic, and reliable analytical HPLC-UV (DAD) method was developed for simultaneous identification and quantification of different seven lignans in the extracts of different extraction techniques.

Development of a validated UPLC–qTOF-MS/MS method for determination of bioactive constituent from Glycyrrhiza glabra

Abstract An ultra-performance liquid chromatography quadrupole time of flight mass spectrometry (UPLC–qTOF-MS/MS) method was developed and validated for the simultaneous determination of glycyrrhizin and glycyrrhetic acid. These analytes were separated on a reverse phase C18 column using a mobile phase of acetonitrile:2% acetic acid in water (75:25, v/v) with a flow rate of 200μL/min. The qTOF-MS was operated under multiple reaction monitoring (MRM) mode using the electrospray ionization (ESI) technique with positive ion polarity. A comparison of three different extraction techniques i.e. accelerated solvent extraction (ASE), extraction under ultrasonic waves (USW) and the classical extraction by percolation (CE) method was done and quantification of these extracts was also carried out by the proposed method.

Production of β-β,Dimethylacrylshikonin in Callus Cultures of Onosma echioides Var hispidum Clarke

AbstractCallus tissues derived from leaf segments of Onosma echioides var hispidum on three basal media viz. Murashige & Skoog (MS), Gamborg et al (B5) and White’s containing 3% sucrose produce napthaquinone pigments in presence of and NAA. However, β-β,dimethylacrylshikonin synthesis was triggered in dark in undifferentiated parenchyma cells on B5 agar medium containing 1 x10−5 M Kn and 2×10−6 M IBA when proliferated calli after 16 weeks (4th generation) were transferred to it and incubated at 23 ± 1 °C. The pigment biosynthesis increased linearly from 4th to 6th week after a lag of first 3 weeks. Callus grew exponentially after a lag of 2 weeks and diminished from 6th week onward. During 8 weeks of growth, callus grew from 0.8 to 8.2 g and the β-β, dimethylacrylshikonin showed the highest level of 25.41 μg g−1 of fresh tissue. Light microscopic examination of semi-thin sections of pigmented tissue revealed pigment accumlation between the plasma membrane and cell wall and also in the intercellular spaces. Exposure of cultures to white fluorescent light for more than 2 h resulted in complete repression of pigment bosynthesis. The investigations suggest that the regulatory mechanism for the biosynthesis and accumulation of napthaquinone pigment(s) may be similar to that of Lithospermum erythrorhizon. Pigment producing capability of callus cultures of O. echioides var hispidum can be exploited as an alternative raw source for the production of shikonin derivatives.

Erratum to: Synthesis and biologic activities of some novel heterocyclic chalcone derivatives

The online version of the original article can be found underdoi:10.1007/s00044-012-0401-7.P. Sharma P. L. Sangwan K. A. Suri B. D. Gupta D. K. Gupta P. Dutt R. A. Vishwakarma N. K. Satti (&)Natural Product Chemistry Division, CSIR-Indian Instituteof Integrative Medicine, Canal Road, Jammu 180001, Indiae-mail: nksatti@rediffmail.comS. KumarCancer Pharmacology Division, CSIR-Indian Instituteof Integrative Medicine, Canal Road, Jammu 18000, IndiaF. Ali I. A. KhanClinical Microbiology Division, CSIR-Indian Instituteof Integrative Medicine, Canal Road, Jammu 180001, IndiaS. Anthal V. K. GuptaDepartment of Physics, University of Jammu,Jammu 180006, IndiaS. SinghPharmacology Division, CSIR-Indian Institute of IntegrativeMedicine, Canal Road, Jammu 18000, India