Huma Aslam Bhatti

Evaluation of the antimycobacterium activity of the constituents from Ocimum basilicum against Mycobacterium tuberculosis

ETHNOPHARMACOLOGICAL RELEVANCE Ocimum basilicum belongs to the genus Ocimum (Lamiaceae). Many species of this genus including O. basilicum have been traditionally used for the treatment of a variety of diseases including respiratory diseases and symptoms of tuberculosis. AIM OF STUDY The aim of the study was to evaluate the activity of pure constituents of O. basilicum, a plant used in traditional medicine to treat respiratory diseases including symptoms of tuberculosis, against Mycobacterium tuberculosis H37Rv. MATERIALS AND METHODS The crude methanolic extract from the aerial parts (leaves, fruits and flowers) of the plant was separated into EtOAc and water subextracts and the EtOAc subextract was further divided into acidic and neutral fractions. Each of these was subjected to fractionation through column chromatography followed by prep. TLC. Several pure compounds were thus isolated and their activity was determined against M. tuberculosis H37Rv using MABA assay. RESULTS Nine compounds were assayed for antituberculosis activity which exhibited upto 49% inhibition of M. tuberculosis H37Rv at 6.25 μg/mL. These include one new compound bacilicin, the structure of which was elucidated based on 2D-NMR (HSQC, HMBC, COSY and NOESY) and Ms spectral analysis. The known compounds were identified on the basis of comparison of their spectral data with those reported earlier. CONCLUSIONS Inhibition of M. tuberculosis by pure compounds from O. basilicum supports the use of this plant in ethnomedicine as a remedy for symptoms of tuberculosis. The results also suggest that the activity of the plant may be due to a synergistic effect of active compounds including those investigated in the present studies, and hence this plant is a potential candidate for obtaining further new antituberculosis natural products.

Synthesis of dihydrodehydrodiconiferyl alcohol: the revised structure of lawsonicin

Structural revision of lawsonicin, a natural product of Lawsonia alba, is reported based upon comparison of its spectral data with that of the naturally occurring dihydrobenzo[b]furan neolignan (rac)-trans-dihydrodehydrodiconiferyl alcohol, which is found to be identical. A concise synthesis of dihydrodehydrodiconiferyl alcohol, via Rh(2)[S-DOSP](4)-catalysed intramolecular C-H insertion, is described.

Flavonoid and cardenolide glycosides and a pentacyclic triterpene from the leaves of Nerium oleander and evaluation of cytotoxicity

A pentacyclic triterpene, oleanderocioic acid, two flavonoidal glycosides, quercetin-5-O-[α-L-rhamnopyranosyl-(1→6)]-β-D-glucopyranoside and kaempferol-5-O-[α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranoside, and a cardenolide, oleandigoside, together with 11 known compounds, were isolated from the leaves of Nerium oleander. Their structures were elucidated on the basis of spectroscopic analysis. The growth inhibitory and cytotoxic activities of eight compounds were evaluated against the MCF-7 human breast cancer cell line using a sulforhodamine B assay. Three compounds, oleandrin, odoroside A and B were further assayed using a panel of 57 human cancer cell lines.

Cinnamomum cassia: an implication of serotonin reuptake inhibition in animal models of depression

The aim of the study was to explore the traditional use of Cinnamomum cassia against depression. The standardised methanolic extract of the bark of C. cassia was evaluated for antidepressant activity using various behavioural tests, i.e. tail suspension test (TST), forced swim test (FST) and locomotor activity test. The serotonergic and noradrenergic modulation was assessed using 5-hydroxytryptophan (5-HTP)-induced head twitches and yohimbine potentiation tests, respectively. The fluoxetine and phenelzine were used as positive controls in the study. The C. cassia extract significantly decreased the immobility time in TST (maximum effective dose tested was 50 mg/kg) while no effect was observed in FST and locomotor activity test. The extract significantly increased the 5-HTP-induced head twitches while yohimbine-induced lethality remained unaltered. The aforementioned results are similar to that caused by fluoxetine. The standardised methanolic extract of C. cassia demonstrated antidepressant activity that can be attributed to rise in serotonin levels.

Synthesis, molecular modelling and biological evaluation of tetrasubstituted thiazoles towards cholinesterase enzymes and cytotoxicity studies

Alzheimer is a neurodegenerative disease and requires the development of new scaffold to treat it. In this regard, thiazoles derivative are playing their significant role. In the current research paper we have focused our attention for the development of tetrasubstituted thiazole (3a-h) derivatives using domino synthesis by mixing the thiourea as a precursor, with acetophenone in the presence of iodine and tosic acid in DMSO and refluxed for 12-22 h. The structures of the newly synthesized compounds were confirmed by FTIR, 1H NMR, 13C NMR and EIMS analysis. Thiazole derivatives were analyzed for their biological significances against acetyl and butylcholinesterase enzymes and compound 3b and 3d were found more active against these enzyme, respectively. The mode of inhibition was determined for the potent compounds against both the enzymes. Moreover, the molecular docking studies were carried out to explore the interactive behavior of the compounds within the active pocket of enzymes. Furthermore, the derivatives (3a-h) were evaluated for their anticancer potential against HeLa cancer cell lines. Most potent inhibition was observed by compound 3b.

Facile dimethyl amino group triggered cyclic sulfonamides synthesis and evaluation as alkaline phosphatase inhibitors

Owing to the biological importance of cyclic sulfonamides (sultams), herein we report a new, facile and cost-effective method for the synthesis of sultams that makes use of a reaction between dansyl amide and easily accessible benzaldehydes under mildly acidic conditions. All compounds were obtained in good yields (69-96%). Consequently a series of cyclic sulfonamides (7a-7n) was synthesized and characterized using FTIR, MS and NMR spectroscopy, crystal structure of compound 7b has also been determined. All compounds were evaluated for their potential to inhibit alkaline phosphatase (bTNAP and bIAP). All compounds were found to be excellent inhibitors of bTNAP with IC50 values in lower micro-molar range (0.11-6.63μM). Most of the compounds were selective inhibitors of bTNAP over bIAP. Only six compounds were found to be active against bIAP (IC50 values in the range 0.38-3.48μM). Molecular docking studies were carried out to identify and rationalize the structural elements necessary for efficient AP inhibition.

Protocatecheuic Acid Underlies the Antioxidant Activity Exhibited by Illicium Verum Fruit

Submit Manuscript | http://medcraveonline.com and its dried fruit is consumed as spice in the food and drink industry as it provides flavor and enhances the taste of food. It is used as a condiment for flavoring curries, confectionery and for pickling [1]. In traditional medicine I .verum has been used as aromatic, anti-spasmodic, carminative, diuretic, expectorant, stomachic as well as stimulant. It is also useful in colic, constipation, dysentery, flatulence and insomnia [2,3]. Nadkarni (1976) Anti-HIV constituents are also reported from the roots of the plant [4].