双色鸡蛋花中分离得到的 plumericin 和异 plumericin 对杜氏利什曼原虫的抗寄生虫活性。
Antiparasitic activity of plumericin & isoplumericin isolated from Plumeria bicolor against Leishmania donovani.
机构信息
Department of Laboratory Medicine, All India Institute of Medical Sciences, New Delhi, India.
出版信息
Indian J Med Res. 2011 Nov;134(5):709-16. doi: 10.4103/0971-5916.91005.
BACKGROUND & OBJECTIVES: The severe toxicity, exorbitant cost and emerging resistance of Leishmania species against most of the currently used drugs underscores the urgent need for the alternative drugs. The present study evaluates in vitro anti-leishmanial activity of Plumeria bicolor and its isolated compounds.
METHODS
The in vitro anti-parasitic activity of chloroform extract of Plumeria bicolor, plumericin and isoplumericin were tested alongwith appropriate controls against promastigote and amastigote forms of Leishmania donovani using 96 well microtiter plate. The concentration used for assessing the anti-leishmanial activity of extract of Plumeria bicolor and both isolated compounds were 100 μg/ml and 15 μM, respectively. The viability of the cells was assessed by MTT assay. The cytotoxicity of these compounds was performed against J774G8 murine macrophage cells lines at the concentration of 30 μM.
RESULTS
The Plumeria bicolor extract showed activity with the IC 50 of 21±2.2 and 14±1.6 μg/ml against promastigote and amastigote forms of L. donovani, respectively. Plumericin consistently showed high activity with the IC 50 of 3.17±0.12 and 1.41±0.03 μM whereas isoplumericin showed the IC50 of 7.2±0.08 μM and 4.1±0.02 μM against promastigote and amastigote forms, respectively. Cytotoxic effect of the chloroform extract of P. bicolor, plumericin and isoplumericin was evaluated in murine macrophage (J774G8) model with CC50 value of 75±5.3 μg/ml, 20.6±0.5 and 24±0.7 μM, respectively.
INTERPRETATION & CONCLUSIONS: Our results indicated that plumericin showed more potent activity than isoplumericin and might be a promising anti-leishmanial agent against L. donovani.
背景与目的
利什曼原虫物种的严重毒性、高昂成本和日益增加的耐药性凸显了对替代药物的迫切需求。本研究评估了双色鸡蛋花及其分离化合物的体外抗利什曼原虫活性。
方法
采用 96 孔微量滴定板，用合适的对照物检测氯仿提取物、普洛马林和异普洛马林对利什曼原虫前鞭毛体和无鞭毛体的体外抗寄生虫活性。评估双色鸡蛋花提取物和两种分离化合物抗利什曼原虫活性的浓度分别为 100μg/ml 和 15μM。通过 MTT 测定法评估细胞活力。在 30μM 的浓度下，对这些化合物对 J774G8 鼠巨噬细胞系的细胞毒性进行了测定。
结果
双色鸡蛋花提取物对前鞭毛体和无鞭毛体的 IC50 分别为 21±2.2μg/ml 和 14±1.6μg/ml。普洛马林始终表现出较高的活性，IC50 分别为 3.17±0.12μM 和 1.41±0.03μM，而异普洛马林对前鞭毛体和无鞭毛体的 IC50 分别为 7.2±0.08μM 和 4.1±0.02μM。采用 CC50 值分别为 75±5.3μg/ml、20.6±0.5μM 和 24±0.7μM，评估了双色鸡蛋花氯仿提取物、普洛马林和异普洛马林对鼠巨噬细胞（J774G8）模型的细胞毒性。
结论
我们的结果表明，普洛马林比异普洛马林表现出更强的活性，可能是一种有前途的抗利什曼原虫药物。
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