Department of Microbiology and Parasitology, Faculty of Medicine, The Persian Gulf Tropical and Infectious Diseases Research Center, Bushehr University of Medical Sciences, Bushehr, Iran.
Eur Rev Med Pharmacol Sci. 2013 Dec;17(24):3306-8.
Leishmania parasites are intracellular haemoflagellates that infect macrophages of the skin and viscera to produce diseases in their vertebrates hosts. Antileishmania therapy is based on pentavalent antimony compounds which toxicity of these agents and the persistence of side effects are severe. Curcumin was identified to be responsible for most of the biological effects of turmeric. Turmeric plant extracts (curcumin and other derivatives) have anti-inflammatory, anti-arthritic, antioxidant, anti-microbial, antileishmanial, hepato protective, anti-cancer, anti-ulcer and anti diabetic activity.
Stock solutions of curcumin, indium curcumin, diacetylcurcumin and Gallium curcumin were made up in DMSO. From the each stock solution serial dilutions were made with phosphate buffered saline and 100 µl of each prepared concentration was added to each well of 96-well micro plate. All tests were performed in triplicate. Negative control only received RPMI-1640 medium with a parasite density of 106 parasites /ml and the positive control contained varying concentrations of standard antileishmania compound, Amphotericine B. MTT solution was prepared as 5 mg/ml in RPMI-1640 and 20 µl of this concentration was added to each well. Antileishmania effects of test agents and control were evaluated by using the MTT assay.
Mean growth inhibition of triplicate for each concentration of test agents and control were measured. The IC50 values for curcumin, gallium curcumin [ga (CUR) 3], indium curcumin [in (CUR)3], Diacethyle Curcumin (DAC ) and Amphotericine B were 38 µg/ml, 32 µg/ml, 26 µg/ml, 52 µg/ml and 20 µg/ml respectively. Indium curcumin [in (CUR) 3] with IC50 values of 26 µg/ml was more effective than other three test agents against Leishmania. Mean growth inhibition of triplicate for Amphotericine B as control drug, was 20 µg/ml.
Indium curcumin and Gallium curcumin complex showed more antileishmanial activity than curcumin and diacetylcurcumin and could be suitable candidates for further investigations.
利什曼原虫是感染皮肤和内脏巨噬细胞的内共生血红鞭毛原生动物，导致脊椎动物宿主患病。抗利什曼原虫治疗基于五价锑化合物，这些药物的毒性和副作用的持续存在是严重的。姜黄素被认为是姜黄的大多数生物学效应的原因。姜黄植物提取物（姜黄素和其他衍生物）具有抗炎、抗关节炎、抗氧化、抗微生物、抗利什曼原虫、肝保护、抗癌、抗溃疡和抗糖尿病活性。
姜黄素、铟姜黄素、二乙酰姜黄素和镓姜黄素的储备溶液在 DMSO 中配制。从每种储备溶液中用磷酸盐缓冲盐水进行连续稀释，并将每种制备浓度的 100µl 加入到 96 孔微量滴定板的每个孔中。所有测试均重复进行三次。阴性对照仅接收 RPMI-1640 培养基，其中寄生虫密度为 106 个寄生虫/ml，阳性对照包含不同浓度的标准抗利什曼原虫化合物两性霉素 B。MTT 溶液在 RPMI-1640 中制备为 5mg/ml，并向每个孔中加入 20µl 该浓度的溶液。通过 MTT 测定法评估测试剂和对照药物的抗利什曼原虫作用。
测量每个浓度的测试剂和对照药物的重复试验的平均生长抑制率。姜黄素、镓姜黄素[ga（CUR）3]、铟姜黄素[in（CUR）3]、二乙酰姜黄素（DAC）和两性霉素 B 的 IC50 值分别为 38µg/ml、32µg/ml、26µg/ml、52µg/ml 和 20µg/ml。IC50 值为 26µg/ml 的铟姜黄素[in（CUR）3]比其他三种测试剂对利什曼原虫更有效。作为对照药物的两性霉素 B 的平均生长抑制率为 20µg/ml。
与姜黄素和二乙酰姜黄素相比，铟姜黄素和镓姜黄素复合物显示出更强的抗利什曼原虫活性，可能是进一步研究的合适候选药物。
