Biological Activity of Coumarin Derivatives as Anti-Leishmanial Agents

Abstract

Cutaneous leishmaniasis affects nearly 0.7 to 1.3 million people annually. Treatment of this disease is difficult due to lack of appropriate medication and the growing problem of drug resistance. Natural compounds such as coumarins serve as complementary therapeutic agents in addition to the current treatment modalities. In this study, we have performed an in-silico screening of the coumarin derivatives and their anti-leishmanial properties has been explored both in-vitro and in-vivo. One of the compounds (compound 2) exhibited leishmanicidal activity and to further study its properties, nanoliposomal formulation of the compound was developed. Treatment of cutaneous lesions in BALB/c mice with compound 2 showed significantly reduced lesion size as compared to the untreated mice (p<0.05) suggesting that compound 2 may possess anti-leishmanial properties.

Coumarin: a novel player in microbial quorum sensing and biofilm formation inhibition

“…The role of coumarins as antimicrobial molecules has been extensively studied to date (Al-Majedy et al 2016 ) with compounds having long chain hydrocarbon substitutions being particularly active (Venugopala et al 2013 ). Among many other relevant therapeutic activities, coumarins are notable for their role as anticancer, anti-inflammatory, antimicrobial, anti-oxidant and anticoagulant bioactive compounds (Joubert et al 2017 ; Kapp et al 2017 ; Mandlik et al 2016 ; Venugopala et al 2013 ). Structurally, these naturally produced coumarins comprise a diverse spectrum of modifications from the parent molecule (Murray 2002 ), with pyrano- and furano-coumarins being particularly pharmacologically active.…”

Identifying inhibitors of the Leishmania inositol phosphorylceramide synthase with antiprotozoal activity using a yeast-based assay and ultra-high throughput screening platform

“…The Leishmania IPC synthase has been previously identified as a putative drug target 18 , 21 , and more recent work has employed a modelling approach to identify coumarin derivatives as enzyme inhibitors with in vivo antileishmanial activity 33 , 34 . To search for new classes of Leishmania IPC synthase inhibitors, in a multidisciplinary public-private partnership, we developed a novel yeast-based assay to screen the 1.8 million entity GSK compound library against the protozoan enzyme.…”

Synthesis and cytotoxic activity of some novel benzocoumarin derivatives under solvent free conditions

“…Moreover, the solvent-free reactions have numerous advantages: reduced pollution, low costs, high yields and purities of products (5,6). Otherwise, many compounds which contain coumarin nucleus exhibit antimicrobial (7), analgesic (8), ulcerogenic (9), anticoagulant (10), antiviral (11) and antimalarial (12), anti-inflammatory (13,14) anti-leishmanial (15) as well as antioxidant (16,17) activities. The antitumor activity of coumarins received a considerable interest owing to their cytotoxic activity against various types of cancer cells, including gastric cancer, liver cancer, colon cancer, breast cancer, prostate cancer, Periodontal Ligament, fibroblast, nasopharyngeal carcinoma, and normal fibroblast cell lines (18)(19)(20)(21)(22).…”