Antileishmanial activity of berenil and methylglyoxal bis (guanylhydrazone) and its correlation with S-adenosylmethionine decarboxylase and polyamines.
Leishmania donovani S-adenosyl-L-methionine (AdoMet) decarboxylase was found to show a growth related pattern. Methylglyoxal bis (guanylhydrazone) (MGBG) and Berenil inhibited the growth of Leishmania donovani promastigotes (strain UR6) in a dose dependent manner. The concentrations of MGBG and Berenil required for 50% inhibition of rate of growth were 67 and 47 microM, respectively. The growth inhibition of MGBG was partially reversed by spermidine (100 microM) and spermine (100 microM). Berenil inhibition of promastigote growth was partially reversed by 100 microM spermidine whereas 100 microM spermine did not result in any reversal of growth. The reduction in parasitemia in vitro by these inhibitors was accompanied by inhibition of AdoMet decarboxylase activity and spermidine levels.
Mukhopadhyay
R
R
School of Life Sciences, Jawaharlal Nehru University, New Delhi, India.
Madhubala
R
R
D012437:Adenosylmethionine Decarboxylase / Q000378:metabolism*; D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D004133:Diminazene / Q000031:analogs & derivatives* / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D007700:Kinetics; D007893:Leishmania donovani / Q000187:drug effects* / Q000254:growth & development / Q000378:metabolism; D008935:Mitoguazone / Q000494:pharmacology*; D011073:Polyamines / Q000378:metabolism*; D011336:Probability; D013997:Time Factors
D000981:Antiprotozoal Agents; D011073:Polyamines; D012437:Adenosylmethionine Decarboxylase; C003915:diminazene aceturate; D008935:Mitoguazone; D004133:Diminazene