Peganine hydrochloride dihydrate an orally active antileishmanial agent

Khaliq, Tanvir ; Misra, Pragya ; Gupta, Swati ; Reddy, K. Papi ; Kant, Ruchir ; Maulik, P. R. ; Dube, Anuradha ; Narender, T. (2009) Peganine hydrochloride dihydrate an orally active antileishmanial agent Bioorganic & Medicinal Chemistry Letters, 19 (9). pp. 2585-2586. ISSN 0960-894X

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Protozoic infections caused by genus Leishmania pose an enormous public health threat in developing countries, compounded by the toxicity and resistance to current therapies. Under the aegis of our ongoing program on drug discovery and development on antileishmanial agents from plants, we carried out bioassay guided fractionation on Peganum harmala seeds which resulted in the isolation of 1 as an antileishmanial agent. 2D-NMR spectral data and single crystal X-ray crystallography data indicated 1 as peganine hydrochloride in dihydrated form. The compound 1 exhibited in-vitro activity against both extracellular promastigotes as well as intracellular amastigotes residing within murine macrophages in Leishmania donovani. Furthermore, 1 also exhibited in-vivo activity, 79.6 (±8.07)% against established VL in hamsters at a dose of 100 mg/kg b.wt.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science.
Keywords:Peganinehydrochloridedihydrate; In-Vivo and In-Vitro Antileishmanial Activity; Apoptosis; Topoisomerase Inhibition
ID Code:101801
Deposited On:11 Mar 2017 15:15
Last Modified:11 Mar 2017 15:15

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