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贝尼尔和甲基乙二醛双(脒腙)的抗利什曼原虫活性及其与S-腺苷甲硫氨酸脱羧酶和多胺的相关性。

Antileishmanial activity of berenil and methylglyoxal bis (guanylhydrazone) and its correlation with S-adenosylmethionine decarboxylase and polyamines.

作者信息

Mukhopadhyay R, Madhubala R

机构信息

School of Life Sciences, Jawaharlal Nehru University, New Delhi, India.

出版信息

Int J Biochem Cell Biol. 1995 Jan;27(1):55-9. doi: 10.1016/1357-2725(95)93432-p.

DOI:10.1016/1357-2725(95)93432-p
PMID:7757882
Abstract

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.

摘要

发现杜氏利什曼原虫的S-腺苷-L-甲硫氨酸(AdoMet)脱羧酶呈现出与生长相关的模式。甲基乙二醛双(脒腙)(MGBG)和贝尼尔以剂量依赖的方式抑制杜氏利什曼原虫前鞭毛体(菌株UR6)的生长。抑制生长速率50%所需的MGBG和贝尼尔浓度分别为67和47微摩尔。亚精胺(100微摩尔)和精胺(100微摩尔)可部分逆转MGBG对生长的抑制作用。100微摩尔亚精胺可部分逆转贝尼尔对前鞭毛体生长的抑制作用,而100微摩尔精胺并未导致生长的任何逆转。这些抑制剂在体外使寄生虫血症降低的同时,伴随着AdoMet脱羧酶活性和亚精胺水平的抑制。

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