Leishmanicidal activity of onopordopicrin isolated from the leaves of Brachylaena discolor
Journal Title: Tropical Journal of Natural Product Research - Year 2018, Vol 2, Issue 7
Abstract
Received 09 May 2018 Revised 01 July 2018 Accepted 05 July 2018 Published online 08 July 2018 Brachylaena discolor (Asteraceae) is a medicinal plant used in Mozambique to treat stomachache, tuberculosis, and diabetes. To discover new lead compounds with leishmanicidal activity, a methanolic extract of the leaves of this plant was investigated. Through fractionation, employing several chromatographic methods, two sesquiterpene lactones onopordopicrin (1) and its germacronolide epoxide derivative (2), together with other ten know phenolic compounds derivatives (3-12) were isolated. The structures of the isolated compounds were determined by spectroscopic methods, mainly 1D and 2D NMR experiments, as well as by comparing their spectroscopic data as reported in the literature. Compounds 1 and 2 were evaluated for their leishmanicidal activity using the Colorimetric method-XXT. Compound 1 showed a significant leishmanicidal activity against Leishmania amazonensis and L. braziliensis (IC50 values 39.6 and 27.9 μM, respectively) as compared to miltefosine (12.5 and 12.0 μM, respectively), a currently used agent to treat leishmaniosis. While compound 2 was inactive against both stains tested with IC50 values >50μM compared with the same agent. Compounds 3-12 were not assayed for leishmanicidal activity. This is the first study reporting the above-mentioned activity of onopordopicrin (1). The results could suggest that compound 1 is a promising lead structure to treat leishmaniosis.
Authors and Affiliations
ulião A. Monjane, Olov Sterner, Diandra Capusiri
Keywords
Related Articles
- EP ID EP491180
- DOI 10.26538/tjnpr/v2i7.5
- Views 64
- Downloads 0
Enhanced Plasma Persistence of Enzyme with Therapeutic Potential Using Polyethylene Glycol as a Coupling Agent
Therapeutic proteins of microbial origin though possess good pharmacological activities, gets quickly broken down into amino acids by the action of proteases in the body. Hence to protect its activity and integrity the e...
Selenium Treatment Ameliorates Experimentally Induced Diarrhoea in Albino Rats
Received 15 December 2017 Revised 02 January 2018 Accepted 04 January 2018 Published online 07 January 2018 Diarrhoea is one of the leading causes of death in children worldwide, accounting for 1 out of every 9 deaths...
Effect of Heat Treatment on the Antioxidant Capacity of Aqueous and Ethanol Extracts of Aframomum angustifolium Seed
Spices are rich in phytochemicals which are responsible for their observed antioxidant property. This potential can be affected by heat treatment when spices are used as food additives. This research studied the effect o...
Blood Schizonticidal Activity of Phyllanthus amarus Enhances Testovarian Antioxidant Defense Capacity in Plasmodium berghei Infected Mice
Received 30 January 2018 Revised 05 March 2018 Accepted 07 March 2018 Published online 07 March 2018 In the present study, the crude ethanol leaf extract of Phyllanthus amarus was investigated for its in vivo activity a...
Formulation and In Vitro Evaluation of Ciprofloxacin Matrix Tablets: Effect of DrugPolymer Ratio
Received 25 April 2018 Revised 08 May 2018 Accepted 09 May 2018 Published online 10 May 2018 An ideal tablet should combine good mechanical strength with adequate drug release profile. This work aims to study the effect...