Momordicatin purified from fruits of Momordica charantia is effective to act as a potent antileishmania agent.
Aqueous extract of the green fruits of the Indian plant Momordica charantia and purified Momordicatin structurally established as 4-(o-carboethoxyphenyl) butanol were evaluated in vitro and in vivo against kala-azar caused by Leishmania donovani. 50% inhibitory concentration (IC(50)) against Leishmania promastigotes in vitro for the crude extract and momordicatin were 0.6mg/L and 0.02mg/L, respectively. When administered in the hamster model of visceral leishmaniasis, 100% parasite clearance was achieved at a dose of 300mg/kg body weight of crude extract and 10mg/kg body weight of Momordicatin. Fe containing parasite superoxide dismutase (SOD) was totally inhibited when treated with 0.72mg/L crude extract and 0.20mg/L Momordicatin, respectively, whereas Cu-Zn containing SOD present in host remained unaffected. Results reveal that the mode of action of these newly found antileishmanial agents is mediated through inhibiting parasite SOD which is one of the key enzymes of the oxidative burst. It may be proposed from the present study that both crude extract of Momordica charantia and Momordicatin obtained from the fruits of the said plant may be considered as potential candidates towards developing new chemotherapeutics against leishmaniasis.
Gupta
Shreedhara
S
Department of Biological Chemistry, 4 Raja S. C. Mullick Road, Kolkata, India.
Raychaudhuri
Bikramjit
B
Banerjee
Shouvik
S
Das
Banasri
B
Mukhopadhaya
Sibabrata
S
Datta
Salil C
SC
D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology*; D000440:Butanols / Q000737:chemistry / Q000494:pharmacology*; D006224:Cricetinae; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D005638:Fruit / Q000737:chemistry*; D006801:Humans; D007893:Leishmania donovani / Q000187:drug effects* / Q000201:enzymology; D007898:Leishmaniasis, Visceral / Q000188:drug therapy* / Q000469:parasitology; D029777:Momordica charantia / Q000737:chemistry* / Q000254:growth & development; D021261:Parasitic Sensitivity Tests; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D013482:Superoxide Dismutase / Q000037:antagonists & inhibitors
D000981:Antiprotozoal Agents; D000440:Butanols; D004791:Enzyme Inhibitors; D010936:Plant Extracts; D013482:Superoxide Dismutase