Evaluation of Lethal Effect of Curcumin and its Derivatives Against Leishmania Major In Vitro

M. Fouladvand, Solyman Khorami, Behroz Naeimi, Sohila Fotouhi, Khosro Mohammadi
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Abstract

Background: Leishmania major is transmitted by sandflies of the genus Phobotomus and causes cutaneous lesions in humans. Curcumin is made from turmeric and various derivatives is derived from it. In the present study the effect of curcumin and it’s derivatives on Leishmania major in vitro was investigated. Materials and Methods: Curcumin 70% and 90% purity and it’ derivatives such as s , BDMC base methoxy curcumin, diacetyl curcumin DAC, vanadyl curcumin VO (CUR) 2, vanadyl diacetyl curcumin VO (DAC) 2, indium curcumin In(CUR)3 and Ga (CUR) 3 preparation. Curcumin derivatives were synthesized and different concentrations of 500 to 800 μg/ ml were prepared in glycerin. 106 Leishmania major promastigotes added to each well of 96 well plate and 100 µL of each curcumin derivative added and stored at 25 ° C for 24 hours. Assay of the lethality of the compounds against Leishmania major and evaluation of their toxic effects on (vero) cells were evaluated using MTT assay. Results: Lethal effect of curcumin and it’s derivatives against Leishmania, increased with increasing concentration. Anti-leishmanial index (IC 50 ) of 70% and 90% curcumin compounds, (BDMC) bis methoxy curcumin, Diacetyl curcumin (DAC), vanadyl curcumin VO (CUR)2, vanadyl diacetyl curcumin VO (DAC)2, indium curcumin In (CUR)3, Gallium Curcumin Ga (CUR)3 compounds were 110, 93, 101, 103, 98, 103, 51 and 58 µg / ml and the lethal effect of these compounds against (vero) cells were 33.1%, 19%, 21%, 20.3%, 17%, 21%, 25.3%, 16%, respectively. Conclusion: Gallium curcumin and indium curcumin, compared to curcumin and other derivatives, exhibited the highest anti-leishmanial effect and were the safest derivatives of curcumin for mammalian cells.
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姜黄素及其衍生物对利什曼原虫体外杀伤作用的评价
背景:主要利什曼原虫由Phobotomus属的沙蝇传播,并引起人类皮肤损伤。姜黄素是由姜黄及其衍生物制备而成的。本研究研究了姜黄素及其衍生物在体外对主要利什曼原虫的影响。材料和方法:姜黄素70%和90%纯度及其衍生物,如s、BDMC碱甲氧基姜黄素、二乙酰基姜黄素DAC、钒基姜黄素VO(CUR)2、钒基二乙酰基姜黄VO(DAC)2、铟姜黄素In(CUR。合成了姜黄素衍生物,并在甘油中制备了500至800μg/ml的不同浓度的姜黄素衍生物。向96孔板的每个孔中加入106个主要利什曼原虫前体,并加入100µL的每种姜黄素衍生物,在25°C下储存24小时。使用MTT法评估化合物对主要利什曼原虫的致死性的测定及其对(vero)细胞的毒性作用的评价。结果:姜黄素及其衍生物对利什曼原虫的致死作用随浓度的增加而增加。70%和90%的姜黄素化合物、(BDMC)双甲氧基姜黄素、二乙酰基姜黄素(DAC)、钒基姜黄素VO(CUR)2、钒基二乙酰基姜黄VO(DAC)2、铟-姜黄素In(CUR)3、镓-姜黄素Ga(CUR)3化合物的抗利什曼原虫指数(IC 50)分别为110、93、101、103、98、103、51和58µg/ml,这些化合物对(vero)细胞的致死作用分别为33.1%、19%、21%、20.3%、17%,分别为21%、25.3%、16%。结论:与姜黄素等衍生物相比,镓-姜黄素和铟-姜黄素对哺乳动物细胞具有最高的抗利什曼原虫作用,是最安全的姜黄素衍生物。
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