Inhibitory Activity and Docking Analysis of Antimalarial Agents from Stemona sp. toward Ferredoxin-NADP+ Reductase from Malaria Parasites.
Inhibitory Activity and Docking Analysis of Antimalarial Agents from Stemona sp. toward Ferredoxin-NADP+ Reductase from Malaria Parasites.
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DOI：
10.1155/2018/3469132
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发表时间：
2018
影响因子：
2.2
通讯作者：
Nahar L
中科院分区：
文献类型：
--
作者：
Pudjiastuti P;Puspaningsih NNT;Siswanto I;Fanani MZ;Ariga YK;Hase T;Sarker SD;Nahar L
Ferredoxin-NADP+还原酶（FNRs, EC 1.18.1.2）存在于疟原虫的质体中，已被认为是开发新型抗疟药物的靶点。研究了从Stemona sp.根中分离得到的Croomine、epi-croomine、tuberostemonine、javastemonine A和isoprotostemonine等生物碱对恶性疟原虫（PfFNR）的抑制作用。对PfFNR向PfFd的电子转移的抑制作用以克罗米明（33.9%）最高，而对PfFNR的diaphorase活性的抑制作用以tuberstomonine（55.4%）最高。对接分析表明，croomine位于PfFNR和PfFd的中间位置。从结核分枝杆菌中提取的克罗米碱似乎具有作为抗疟剂的潜力。
Ferredoxin-NADP+ reductases (FNRs, EC 1.18.1.2) were found in the plastids of Plasmodium and have been considered as a target for the development of new antimalarial agents. Croomine, epi-croomine, tuberostemonine, javastemonine A, and isoprotostemonine are isolated alkaloids from the roots of Stemona sp. and their inhibitory effect on FNRs from Plasmodium falciparum (PfFNR) was investigated. Croomine showed the highest level of inhibition (33.9%) of electron transfer from PfFNR to PfFd, while tuberstemonine displayed the highest level of inhibition (55.4%) of diaphorase activity of PfFNR. Docking analysis represented that croomine is located at the middle position of PfFNR and PfFd. Croomine from S. tuberosa appeared to have potential as an antimalarial agent.