In vitro screening of known drugs identified by scaffold hopping techniques shows promising leishmanicidal activity for suramin and netilmicin

Khanra, S. , Kumar, Y. P., Dash, J. and Banerjee, R. (2018) In vitro screening of known drugs identified by scaffold hopping techniques shows promising leishmanicidal activity for suramin and netilmicin. BMC Research Notes, 11(1), 319. (doi: 10.1186/s13104-018-3446-y) (PMID:29784022) (PMCID:PMC5963029)

Abstract

Objective: The rapid emergence of drug resistant Leishmanial strains makes it imperative to continue the development of cheap and effective drugs against the parasite. Due to the absence of effective vaccines against leishmaniasis, current therapeutic measures exclusively rely on chemotherapy. Here we attempt, to identify novel antileishmanial from a list of known drugs determined from a previous bioinformatics study. Synergism between various drug combinations (involving netilmicin, suramin, paromomycin and curcumin) have been estimated to identify potent multidrug therapies to combat the disease. Results: The drugs were screened against Leishmania promastigotes by utilizing the MTT assay and against intracellular amastigotes using murine Macrophage like tumor cell, RAW 264.7 as a host. In vitro drug interactions were tested for several drug combinations with a modified fixed ratio isobologram method against both Leishmania major and Leishmania donovani. This work reports the in vitro antileishmanial activity for the aminoglycoside netilmicin (for some Leishmania parasites) and the anti-trypanosomatid suramin. Synergism was also observed between paromomycin–suramin and netilmicin–curcumin.

• Item Type: Articles
• Status: Published
• Refereed: Yes
• Glasgow Author(s) Enlighten ID: Khanra, Dr Supriya
• Authors: Khanra, S., Kumar, Y. P., Dash, J., and Banerjee, R.
• College/School: College of Medical Veterinary and Life Sciences > School of Infection & Immunity
• Journal Name: BMC Research Notes
• Publisher: BioMed Central
• ISSN: 1756-0500
• ISSN (Online): 1756-0500
• Copyright Holders: Copyright © 2018 The Author(s)
• First Published: First published in BMC Research Notes 11(1):319
• Publisher Policy: Reproduced under a Creative Commons licence