A triterpenoid saponin possessing antileishmanial activity from the leaves of Careya arborea.

Bioguided-fractionation of the methanol extract of the leaves of Careya arborea led to isolation of a triterpenoid saponin, designated arborenin, and characterized as 3-O-beta-D-glucopyranosyl(1-->2)-beta-D-glucopyranosyl-2 alpha,3beta-dihydroxy-taraxast-20-en-28-oic acid (1), together with desacylescin III (2). The structures were determined on the basis of extensive 2D NMR spectroscopic analysis. The saponin showed in vitro antileishmanial activity against Leishmania donovani (strain AG 83).

Polyoxypregnane glycosides from the flowers of Dregea volubilis.

Three novel polyoxypregnane glycosides, volubiloside A, B and C (1-3), were isolated from the flowers of Dregea volubilis Linn., and their structures were elucidated as drevogenin D-3-O-beta-D-glucopyranosyl (1-->4)-6-deoxy-3-O-methyl-beta-D-allopyranosyl (1-->4)-beta-D-cymaropyranosyl (1-->4)-beta-D-cymaropyranoside, drevogenin D-3-O-beta-D-glucopyranosyl (1-->4)-6-deoxy-3-O-methyl-beta-D-allopyranosyl (1-->4)-beta-D-cymaropyranosyl (1-->4)-beta-D-digitoxopyranoside and drevogenin P-3-O-beta-D-glucopyranosyl (1-->4)-6-deoxy-3-O-methyl-beta-D-allopyranosyl (1-->4)-beta-D-cymaropyranosyl (1-->4)-beta-D-cymaropyranoside, respectively, on the basis of extensive NMR experiments, MALDI-TOF MS, and some chemical strategies.

Evaluation of the wound healing activity of methanol extract of Pedilanthus tithymaloides (L.) Poit leaf and its isolated active constituents in topical formulation.

ETHNOPHARMACOLOGICAL RELEVANCE: Pedilanthus tithymaloides leaves are widely used in Indian medicine to heal wounds, burn, mouth ulcers. However, systematic evaluation of these activities is lacking. Thus, the present study aimed to assesses the wound healing activity of Pedilanthus leaves and its isolated constituents in topical ointment formulation. MATERIALS AND METHODS: Bioassay-guided chromatographic fractionation of the methanol extract of leaves resulted in the isolation of 2-(3,4-dihydroxy-phenyl)-5,7-dihydroxy-chromen-4-one and 1, 2-tetradecanediol, 1-(hydrogen sulfate), sodium salt. The ointment formulation of methanol extract (2.5%, 5% w/w) and isolated compounds (0.25% w/w) was prepared and evaluated on excision, incision and dead space wound models in rats. The effects of formulations on wound healing were assessed by the rate of wound closure, period of epithelialization, tensile strength, granulation tissue weight, hydroxyproline content and histopathology. RESULTS: Significant wound healing activity was observed with methanol extract and isolated constituents. Topical application of isolated compound ointments caused faster epithelialization, significant wound contraction (95.41%), and better tensile strength (565.33 g) on 16 post-wounding day, while 5% extract showed wound epithelialization with 95.55% contraction on 18th post-wounding day, better than the control group (76.39% on 22 day). The tensile strength of incision wound was significantly increased in extract and compound treated animals. Moreover, in dead space model the extract significantly increased granuloma tissue weight, tensile strength and hydroxyproline content. The tissue histology of ointment treated groups showed complete epithelialization with increased collagenation, compared to the povidone-iodine group. CONCLUSIONS: The results validated the traditional use of Pedilanthus tithymaloides for cutaneous wound management.

Combination therapy with indolylquinoline derivative and sodium antimony gluconate cures established visceral leishmaniasis in hamsters.

2-(2"-Dichloroacetamidobenzyl)-3-(3'-indolylquinoline), designated indolylquinoline derivative A, reduced the splenic and the liver parasite burdens by >93.0% in Leishmania donovani-infected hamsters, whereas sodium antimony gluconate (SAG) reduced the burdens approximately 80.0%. Complete clearance of parasitemia from the livers and spleens was noticed when infected animals received indolylquinoline derivative A plus SAG, suggesting that indolylquinoline derivative A has potential as a new agent for sole or conjunctive therapy for leishmaniasis.

Synthesis of a novel quinoline derivative, 2-(2-methylquinolin-4-ylamino)-N-phenylacetamide--a potential antileishmanial agent.

Some novel quinoline derivatives were prepared and tested for antileishmanial activity. 2-(2-Methylquinolin-4-ylamino)-N-phenylacetamide (2) was found to be significantly more active than the standard antileishmanial drug sodium antimony gluconate (SAG) in reducing the parasite load both in the spleen and liver at a much lower concentration in hamster models. The results suggest that the compound could be exploited as an antileishmanial drug.