Kalauni Surya Kant, Awale Suresh, Tezuka Yasuhiro, Banskota Arjun Hari, Linn Thein Zaw, Asih Puji Budi Setia, Syafruddin Din, Kadota Shigetoshi
Institute of Natural Medicine, University of Toyama, Sugitani, Japan.
Biol Pharm Bull. 2006 May;29(5):1050-2. doi: 10.1248/bpb.29.1050.
Malaria is one of the most life-threatening infectious diseases worldwide and claims millions of people's lives each year. The appearance of drug-resistance Plasmodium falciparum has made the treatment of malaria increasingly problematic, and thus, it is a dire need to search the new alternatives of current drugs. In the present study, 44 cassane- and norcassane-type diterpenes isolated from Caesalpinia crista of Myanmar and Indonesia were evaluated for their antimalarial activity against the malaria parasite Plasmodium falciparum FCR-3/A2 clone in vitro. Most of the tested diterpenes displayed antimalarial activity, and norcaesalpinin E (28) showed the most potent activity with an IC50 value of 0.090 microM, more potent than the clinically used drug chloroquine (IC50, 0.29 microM). Based on the observed results, a structure-activity relationship has been established.
疟疾是全球最具生命威胁的传染病之一，每年导致数百万人死亡。耐多药恶性疟原虫的出现使疟疾治疗问题日益突出，因此，迫切需要寻找现有药物的新替代品。在本研究中，对从缅甸和印度尼西亚的苏木科云实属植物中分离得到的44种乌檀烷型和降乌檀烷型二萜类化合物进行了体外抗疟活性评价，以检测其对疟原虫恶性疟原虫FCR-3/A2克隆的抑制作用。大多数受试二萜类化合物显示出抗疟活性，其中降云实宁E（28）活性最强，IC50值为0.090微摩尔，比临床使用的药物氯喹（IC50，0.29微摩尔）更有效。基于观察结果，建立了构效关系。
