Uppuluri Venkata Mallavadhani

Screening of Plumbago Species for the Bio-active Marker Plumbagin

Three locally available Plumbago species (Plumbago auriculata, Plumbago rosea and Plumbago zeylanica) have been quantitatively screened for the bioactive marker plumbagin by high performance thin layer chromatography. In general, the root parts were found to be the rich sources for plumbagin. Most significantly, P. rosea was found to accumulate maximum plumbagin in the roots. In contrast, P. auriculata and P. zeylanica are high yielding species for the leaf and stem parts, respectively. Studies have also been extended to evaluate some P. rosea samples collected from southern India and a traditional medicine, Chitrakadi vati, which contains P. zeylanica as the major constituents.

Synthesis of novel ring-A fused hybrids of oleanolic acid with capabilities to arrest cell cycle and induce apoptosis in breast cancer cells.

Six novel oleanolic acid ring-A fused hybrids (5-10) have been synthesized by employing a four step protocol with the introduction of benzylidene functionality at C-2 as the key step. Their structures were established by high resolution NMR and Mass spectral data. The synthesized compounds have been screened against seven human cancer cell lines including ME-180 & HeLa (cervix), MCF-7, MDA-MB-453 & MDA-MB-231 (breast), PC-3 (prostate) and HT-29 (colon) using MTT assay. Most significantly, compound 10 showed potent activity against the three breast cancer cell lines. The IC₅₀ value (10.60 μM) of compound 10 against MCF-7 found to be much lower than that of the standards and parent compound. Flow cytometric analysis reveals that compound 10 arrests cell cycle in S phase and induces apoptosis in MCF cells.

On the potential of Tephrosia purpurea as anti-Helicobacter pylori agent

AIM OF THE STUDY Since Tephrosia purpurea (Linn.) Pers. (Fabaceae) has traditional use in curing different types of wounds including gastroduodenal ulcers, it was of interest to evaluate the in vitro anti-Helicobacter pylori activity profile of the plant extract and its fractions with a view to examining its therapeutic potential, if any. MATERIALS AND METHODS Employing clinical isolates and standard strains of Helicobacter pylori, the extract and fractions were bioevaluated in terms of MIC and MBC values, acid stability, time-kill kinetics, drug resistance, and synergistic potential. RESULTS The methanolic extract showed promising activity against clinical isolates and standard strains of Helicobacter pylori, including metronidazole-resistant strains. Fractionation of the extract revealed the n-hexane and chloroform fractions to possess marked activity. The extract and the less polar fractions remained functionally active in acidic condition similar to stomach environment, exhibited consistent bacteriostatic activity during repeated exposure, and demonstrated synergism, complete or partial, even with antibiotic-resistant strains. CONCLUSION Apolar fractions of Tephrosia purpurea may have therapeutic potential in combating Helicobacter pylori mediated gastroduodenal disorders.

Two novel butanol rhamnosides from an Indian traditional herb, Euphorbia hirta

Two novel butanol rhamnopyranosides (1 and 2), along with nine known compounds (3–11), have been isolated from various non-polar and polar extracts of an Indian traditional herb, Euphorbia hirta. The structures of the new compounds were elucidated as n-butyl-1-O-β-L-rhamnopyranoside (1) and n-butyl-1-O-α-L-rhamnopyranoside (2) by spectroscopic methods including IR, HR-FABMS, 1D and 2D NMR techniques.

A new tetracyclic triterpene from the latex of Euphorbia Nerifolia

A new tetracyclic triterpene 9,19-cyclolanost-22(22′), 24-diene-3β-ol, named as nerifoliene (2) along with euphol (1) were isolated from the fresh latex of Euphorbia nerifolia. Their structures were elucidated on the basis of spectral (IR, 1H and 13C NMR, FAB and EI Mass) data.

A rapid and highly sensitive UPLC–QTOF MS method for quantitative evaluation of Nardostachys jatamansi using Nardin as the marker

Nardostachys jatamansi DC. is a highly reputed Medhya and Nootropic (Learning and Memory) Ayurvedic medicinal plant. Its use as herbal medicine singly and as an ingredient of multi-herbal formulations is fast increasing. In order to authenticate and evaluate it quantitatively, its standardization is highly warranted with respect to a reliable marker. In this connection a rapid and highly sensitive UPLC-QTOF MS method has been developed. The analysis was carried out on an Acquity BEH C(18) column with gradient elution of methanol-water and 3 mm ammonium acetate using QTOF mass detector in negative ionization mode. The method was validated over a concentration range of 9.76-156.25 ng/mL nardin. The calibration curve is linear with the correlation coefficient (r) and coefficient of determination (R(2)) were 0.9997 and 0.9995 respectively. The LOD and LOQ were 3.050 and 9.277 ng/mL respectively. The recovery of nardin in the range 96.36-111.13% achieved from spiked samples was consistent and reproducible. The inter-day and intra-day assay precision of the analytes over the entire concentration range was less than 5%. The developed method required only 4 min for chromatography to authenticate and quantify the marker, viz. nardin in N. jatamansi samples, in addition to the sample preparation time.

HPTLC Method for Quantitative Evaluation of Preparations Containing Indian 'Elixir' Plant, Tinospora cordifolia, Using Jatrorrhizine as Marker

Because of its extensive use in traditional medicine, the Indian plant T. cordifolia, known as ‘Heavenly Elixir’, has been chemically and analytically screened. Because the stem is therapeutically highly valued, its methanol extract was subjected to detailed chromatograph-ic separation to isolate the marker compound jatrorrhizine, a proto-berberine alkaloid, which was identified by IR, 1H and 13C NMR, and mass spectroscopic analysis. A simple and rapid HPTLC method has been established for quantification of jatrorrhizine. The method was linear in the range 40-140 ng. Statistical data and recovery >96% reveals the accuracy of the method. The method was found to give consistent results and was suitable for evaluation of commercial preparations of T. cordifolia.

Quantitative Evaluation of Anticancer Marker Levels of an Ayurvedic Preparation, "Virala"

Virala (Diospyros tomentosa Roxb.), an important Ayurvedic preparation, was chemically screened and found to accumulate significant levels of the anticancer markers betulin and betulinic acid. In order to identify the high yielding sample of these two markers, a number of virala samples collected from different parts of India have been screened by high performance thin layer chromatography (HPTLC). The sample collected from local areas (20°15′N, 85°50′E) was found to contain the highest levels of betulinic acid (0.43%), whereas the sample collected from Vijayawada (16°30′N, 80°36′E) was found to contain maximum betulin (1.13%). Interesting correlations have been drawn between accumulations of these two markers versus the height of place above sea level where samples were collected.

Synthesis and antimicrobial screening of some novel chalcones and flavanones substituted with higher alkyl chains

Abstract As a part of our program to generate some novel flavonoid frameworks substituted with higher alkyl groups as possible antimicrobial agents, we have in total synthesized twelve novel chalcones (11–16) and their corresponding flavanones (17–22) substituted with either nonyl or dodecyl chains in ring B in very good to excellent yields. The synthesized compounds have been screened for their antimicrobial potential against six bacterial and four fungal strains. The tested compounds, in general, showed significant antibacterial and comparable antifungal activities. While the chalcone (16) with a dodecyl chain showed highly promising antibacterial activity against almost all the organisms tested, the chalcone (13) with nonyl chain showed promising antifungal activity against Candida rugosa and Aspergillus niger strains.

A new aurone and two rare metabolites from the leaves of Diospyros melanoxylon

A new aurone, 4,6-dihydroxy-2-[α,α-(4-hydroxyphenyl)hydroxy]methylene-3(2H)-benzofuranone (2) and two rare metabolites viz. selin-4(15)-en-1β,11-diol (5) and 5,7-dihydroxy-3-O-β-D-glucopyranosyl-1′′′ → 6′′glucopyranoside-2-{4-hydroxyphenyl}-4H-benzopyran-4-one (6) in addition to the known protocatechuic acid methyl ester (1), quercitin (3) and gallic acid (4) were isolated from the methanol extract of Diospyros melanoxylon leaves. The structures were elucidated by a combination of chemical and spectroscopic analysis. Interestingly, compound 2 was found to exist in both E- and Z-isomeric forms in a 15 : 85 ratio. The present isolation of compounds 2 and 5 assumes taxonomic significance as aurones and sesquiterpenes have not yet been reported from the Diospyros genus, consisting of more than 350 identified species.