Chulabhorn International College of Medicine, Thammasat University (Rangsit Campus), Pathumtani 12121, Thailand.
Molecular and Biochemical Parasitology, Liverpool School of Tropical Medicine, University of Liverpool, Liverpool L3 5QA, United Kingdom; Clinical Laboratory Sciences Department, College of Applied Medical Sciences, King Saud University, P.O. Box 10219, Riyadh 11433, Saudi Arabia.
Exp Parasitol. 2014 Oct;145:80-6. doi: 10.1016/j.exppara.2014.07.013. Epub 2014 Aug 4.
Multidrug resistant Plasmodium falciparum is the major health problem in the tropics. Discovery and development of new antimalarial drugs with novel modes of action is urgently required. The aim of the present study was to investigate antimalarial activities of Garcinia mangostana Linn. crude ethanolic extract including its bioactive compounds as well as the metabolic footprinting of P. falciparum following exposure to G. mangostana Linn. extract. The median (range) IC50 (concentration that inhibits parasite growth by 50%) values of ethanolic extract of G. mangostana Linn., α-mangostin, β-mangostin, gartanin, 9-hydroxycarbaxathone, artesunate, and mefloquine for 3D7 vs K1 P. falciparum clones were 12.6 (10.5-13.2) vs 4.5 (3.5-6.3) μg/ml, 7.3 (7.1-8.5) vs 5.0 (3.7-5.9) μg/ml, 47.3 (46.8-54.0) vs 35.0 (30.0-43.7) μg/ml, 9.2 (8.1-11.9) vs 6.8 (6.2-9.1) μg/ml, 0.6 (0.4-0.8) vs 0.5 (0.4-0.7) μg/ml, 0.4 (0.2-1.2) vs 0.7 (0.4-1.0)ng/ml, and 5.0 (4.2-5.0) vs 2.7 (2.5-4.6) ng/ml, respectively. The action of G. mangostana Linn. started at 12 h of exposure, suggesting that the stage of its action is trophozoite. The 12-h exposure time was used as a suitable exposure time for further analysis of P. falciparum footprinting. G. mangostana Linn. extract was found to target several metabolic pathways particularly glucose and TCA metabolisms. The malate was not detected in culture medium of the exposed parasite, which may indirectly imply that the action of G. mangostana Linn. is through interruption of TCA metabolism.
耐多药恶性疟原虫是热带地区的主要健康问题。迫切需要发现和开发具有新型作用模式的新抗疟药物。本研究旨在研究藤黄属植物粗乙醇提取物的抗疟活性，包括其生物活性化合物，以及藤黄属植物提取物暴露后恶性疟原虫的代谢足迹。G. mangostana Linn. 乙醇提取物、α-倒捻子素、β-倒捻子素、倒捻子素、9-羟基碳杂噻酮、青蒿琥酯和甲氟喹对 3D7 与 K1 恶性疟原虫克隆的 IC50 值（抑制寄生虫生长 50%的浓度）中位数（范围）分别为 12.6（10.5-13.2）μg/ml 和 4.5（3.5-6.3）μg/ml、7.3（7.1-8.5）μg/ml 和 5.0（3.7-5.9）μg/ml、47.3（46.8-54.0）μg/ml 和 35.0（30.0-43.7）μg/ml、9.2（8.1-11.9）μg/ml 和 6.8（6.2-9.1）μg/ml、0.6（0.4-0.8）μg/ml 和 0.5（0.4-0.7）μg/ml、0.4（0.2-1.2）μg/ml 和 0.7（0.4-1.0）ng/ml，以及 5.0（4.2-5.0）ng/ml 和 2.7（2.5-4.6）ng/ml。G. mangostana Linn. 的作用始于暴露 12 小时，表明其作用阶段是滋养体。12 小时暴露时间被用作进一步分析恶性疟原虫足迹的合适暴露时间。发现藤黄属植物提取物靶向几种代谢途径，特别是葡萄糖和 TCA 代谢。在暴露寄生虫的培养基中未检测到苹果酸，这可能间接暗示藤黄属植物的作用是通过中断 TCA 代谢。
