Institute of Specific Prophylaxis and Tropical Medicine, Medical University of Vienna, Austria.
Acta Trop. 2012 Aug;123(2):96-100. doi: 10.1016/j.actatropica.2012.04.002. Epub 2012 Apr 17.
According to the WHO, in 2008, there were 247 million reported cases of malaria and nearly one million deaths from the disease. Parasite resistance against first-line drugs, including artemisinin and mefloquine, is increasing. In this study the plant-derived compounds aglafolin, rocaglamid, kokusaginine, arborine, arborinine and tuberostemonine were investigated for their anti-plasmodial activity in vitro. Fresh Plasmodium falciparum isolates were taken from patients in the area of Mae Sot, north-western Thailand in 2008 and the inhibition of schizont maturation was determined for the respective compounds. With inhibitory concentrations effecting 50%, 90% and 99% inhibition (IC(50), IC(90) and IC(99)) of 60.95 nM, 854.41 nM and 7351.49 nM, respectively, rocaglamid was the most active of the substances, closely followed by aglafoline with 53.49 nM, 864.55 nM and 8354.20 nM. The activity was significantly below that of artemisinin, but moderately higher than that of quinine. Arborine, arborinine, tuberostemonine and kokusaginine showed only marginal activity against P. falciparum characterized by IC(50) and IC(99) values higher than 350 nM and 180 μM, respectively, and regressions with relatively shallow slopes S>14.38. Analogues of rocaglamid and aglafoline merit further exploration of their anti-plasmodial activity.
根据世界卫生组织（WHO）的数据，2008 年全球报告疟疾病例达 2.47 亿例，并有近 100 万人死于疟疾。寄生虫对包括青蒿素和甲氟喹在内的一线药物的耐药性正在增加。在这项研究中，研究人员检测了植物衍生化合物 aglafolin、rocaglamid、kokusaginine、arborine、arborinine 和 tuberostemonine 的抗疟原虫活性。2008 年从泰国西北部湄索地区的疟疾病例中提取新鲜的恶性疟原虫分离株，并测定了这些化合物对裂殖体成熟的抑制作用。rocaglamid 的抑制浓度分别为 50%、90%和 99%的效应浓度（IC50、IC90 和 IC99）为 60.95 nM、854.41 nM 和 7351.49 nM，是最有效的化合物，紧随其后的是 aglafolin，其 50%、90%和 99%的效应浓度（IC50、IC90 和 IC99）分别为 53.49 nM、864.55 nM 和 8354.20 nM。rocaglamid 的活性明显低于青蒿素，但略高于奎宁。arborine、arborinine、tuberostemonine 和 kokusaginine 对恶性疟原虫的活性较低，IC50 和 IC99 值均高于 350 nM 和 180 μM，且回归线斜率 S>14.38。rocaglamid 和 aglafolin 的类似物值得进一步研究其抗疟原虫活性。
