Anita Mahapatra

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.

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.

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.

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.

Chyawanprash: A review of therapeutic benefits as in authoritative texts and documented clinical literature.

ETHNOPHARMACOLOGICAL RELEVANCE Chyawanprash (CP), a traditional immune booster recipe, has a long history of ethnic origin, development, household preparation and usage. There are even mythological stories about the origin of this recipe including its nomenclature. In the last six decades, CP, because of entrepreneurial actions of some research Vaidyas (traditional doctors) has grown to industrial production and marketing in packed forms to a large number of consumers/patients like any food or health care product. Currently, CP has acquired a large accepted user base in India and in a few countries out-side India. AIM OF THE STUDY Authoritative texts, recognized by the Drugs and Cosmetics Act of India, describe CP as an immunity enhancer and strength giver meant for improving lung functions in diseases with compromised immunity. This review focuses on published clinical efficacy and safety studies of CP for correlation with health benefits as documented in the authoritative texts, and also briefs on its recipes and processes. MATERIALS AND METHODS Authoritative texts were searched for recipes, processes, and other technical details of CP. Labels of marketing CP products (Indian) were studied for the health claims. Electronic search for studies of CP on efficacy and safety data were performed in PubMed/MEDLINE and DHARA (Digital Helpline for Ayurveda Research Articles), and Ayurvedic books were also searched for clinical studies. RESULTS The documented clinical studies from electronic databases and Ayurvedic books evidenced that individuals who consume CP regularly for a definite period of time showed improvement in overall health status and immunity. However, most of the clinical studies in this review are of smaller sample size and short duration. Further, limitation to access and review significant data on traditional products like CP in electronic databases was noted. CONCLUSIONS Randomized controlled trials of high quality with larger sample size and longer follow-up are needed to have significant evidence on the clinical use of CP as immunity booster. Additional studies involving measurement of current biomarkers of immunity pre- and post-consumption of the product as well as benefits accruing with the use of CP as an adjuvant are suggested.

Synthesis and Antitubercular Activity of Berberine Derivatives

The isoquinoline alkaloid berberine (1) was isolated from the roots of Berberis aristata and its new, 13-benzyl (3–6), 13-allyl (7, 8), 8-(2-oxopropyl) (2), and 9-hydroxy (9) derivatives have been synthesized under mild conditions with good yield. The structures of the new derivatives were confirmed by spectroscopic (UV, IR, NMR, and MS) analysis. The antitubercular activity of the derivatives against Mycobacterium tuberculosis H37Rv was studied (microdilution assay) and compared with rifampicin as standard drug. The results demonstrated that the 4-chlorobenzyl (4), 2,4-dichlorobenzyl (5), 4-fluorobenzyl (6), and 3′,3′-dimethylallyl (8) derivatives exhibited (MIC, 4–8 μg/mL) 2–4 fold more activity than berberine (MIC, 16 μg/mL), which is probably due to the 13-benzyl and allyl substitution in the molecule.

Cytotoxicity of synthesized 1,4-naphthoquinone analogues on selected human cancer cell lines

In an effort to establish new candidates with enhanced anticancer activity of 5-hydroxy-7-methyl-1,4-naphthoquinone scaffold (7-methyljuglone) previously isolated from the root extract of Euclea natalensis, a series of 7-methyljuglone derivatives have been synthesized and assessed for cytotoxicity on selected human cancer lines. These compounds were screened in vitro for anticancer activity on MCF-7, HeLa, SNO and DU145 human cancer cell lines by MTT assay. Most of them exhibited significant toxicity on cancer cell lines with lower IC50 values. The most potent derivative (19) exhibited the toxicity on HeLa and DU145 cell lines with IC50 value of 5.3 and 6.8μM followed by compound (5) with IC50 value of 10.1 and 9.3μM, respectively. Structure-activity relationship reveals that the fluoro substituents at position C-8 while hydroxyl substituents at C-2 and C-5 positions played an important role in toxicity.

Quantitative Analysis of Corosolic Acid, a Type-II Anti-Diabetic Agent, in Different Parts of Lagerstroemia speciosa Linn.

An HPTLC method has been established for rapid and simple quantitative determination of corosolic acid, a type-II (non-insulin dependant) anti-diabetic agent found in the plant Lagerstroemia speciosa. To identify the high-yielding parts of the plant, different tissues, for example leaf, stem, stem bark, root, heartwood, calyx, and fruit were extracted with 80% ethanol. The extracts were chromatographed on aluminum plates coated with silica gel 60F254, with chloroform-methanol 8.5:1.5 (v/v) as mobile phase. Densitometric quantification of corosolic acid was performed in absorbance mode at 366 nm after derivatization. Amounts of corosolic acid in the different samples were calculated by use of the regression equations (r = 0.99603) of calibration plots, which showed there was a good linear relationship between peak area and amount of corosolic acid in the range 0.5–4.5 μg. The limits of detection (LOD) and quantitation (LOQ) were 6 and 16 ng, respectively. The method was validated for precision, repeatability, and accuracy. Recovery was determined by spiking samples with corosolic acid standard before and after extraction and found to be in the range 95.80–97.13%. The maximum corosolic acid content (0.89%) was found in the leaves.

An efficient chemical method for separation of corsolic acid from its isomeric maslinic acid

Based on the difference in steric bulk around C12–C13 double bond, the two isomeric dihydroxy pentacyclic triterpenic acids viz: corsolic acid and maslinic acid have been quantitatively separated via their methyl esters by reacting with the bulky m-chloroperbenzoic acid. Corsolic acid methyl ester was obtained in pure form, whereas maslinic acid methyl ester was separated as 12-oxo derivative formed via its epoxide. Alkaline hydrolysis of corsolic acid methyl ester afforded the desired acid. This method was also found to work well with the isomeric amyrin mixture (α- and β-), but not highly selective. The high selectivity of this method with corsolic maslinic acid system can be rationalized in terms of 2α-hydroxy functionality, which provides additional crowding around the double bond and completely prevented corsolic acid from its reaction with perbenzoic acid.