Nanomolar Antimalarial Agents against Chloroquine-Resistant Plasmodium falciparum from Medicinal Plants and Their Structure-Activity Relationships
文献类型：期刊论文
| 作者 | Zhou, Bin1,2; Wu, Yan1,2; Dalal, Seema3; Merino, Emilio F.3; Liu, Qun-Fang1,2 ; Xu, Cheng-Hui1,2; Yuan, Tao1,2; Ding, Jian1,2; Kingston, David G. I.4,5; Cassera, Maria B.3
|
| 刊名 | JOURNAL OF NATURAL PRODUCTS
 |
| 出版日期 | 2017-01 |
| 卷号 | 80期号:1页码:96-107 |
| ISSN号 | 0163-3864 |
| DOI | 10.1021/acs.jnatprod.6b00744 |
| 文献子类 | Article |
| 英文摘要 | Inspired by the discovery of the antimalarial drug artemisinin from a traditional Chinese medicine (TCM), a natural product library of 44 lindenane-type sesquiterpenoids was assessed for activities against the Dd2 chloroquine-resistant strain of the malaria parasite Plasmodium falciparum. These compounds were mainly isolated from plants of the Chloranthus genus, many species of which are named "Sikuaiwa" in TCM and have long been used to treat malaria. The compounds consisted of 41 sesquiterpenoid dimers and three monomers, including the 12 new dimers 1-12 isolated from Chloranthus fortunei. The results showed that 16 dimers exhibited potent antiplasmodial activities (<100 nM); in particular, compounds 1, 14, and 19 exhibited low nanomolar activities with IC50 values ranging from 1 to 7 nM, which is comparable to the potency of artemisinin, and selectivity index values toward mammalian cells greater than 500. A comprehensive structure-activity relationship study indicated that three functional groups are essential and two motifs can be modified. |
| WOS关键词 | CHLORANTHUS-JAPONICUS ; CHEMICAL-CONSTITUENTS ; SESQUITERPENOID DIMERS ; ARTEMISININ RESISTANCE ; SARCANDRA-GLABRA ; C-F ; SPICATUS ; MULTISTACHYS ; SERRATUS ; ROOTS |
| 资助项目 | National Natural Science Foundation[21532007] ; National Natural Science Foundation[81321092] ; Ministry of Science and Technology of People's Republic of China[2012CB721105] ; National Center for Complementary and Integrative Health[1 R01 AT008088] |
| WOS研究方向 | Plant Sciences ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000393089600014 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275742]  |
| 专题 | 天然药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Yue, Jian-Min |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; 2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China; 3.Virginia Tech, Dept Biochem, MC 0308-0212, Blacksburg, VA 24061 USA; 4.Virginia Tech, Dept Chem, MC 0308-0212, Blacksburg, VA 24061 USA; 5.Virginia Tech, Ctr Drug Discovery, MC 0308-0212, Blacksburg, VA 24061 USA |
| 推荐引用方式 GB/T 7714 | Zhou, Bin,Wu, Yan,Dalal, Seema,et al. Nanomolar Antimalarial Agents against Chloroquine-Resistant Plasmodium falciparum from Medicinal Plants and Their Structure-Activity Relationships[J]. JOURNAL OF NATURAL PRODUCTS,2017,80(1):96-107. |
| APA | Zhou, Bin.,Wu, Yan.,Dalal, Seema.,Merino, Emilio F..,Liu, Qun-Fang.,...&Yue, Jian-Min.(2017).Nanomolar Antimalarial Agents against Chloroquine-Resistant Plasmodium falciparum from Medicinal Plants and Their Structure-Activity Relationships.JOURNAL OF NATURAL PRODUCTS,80(1),96-107. |
| MLA | Zhou, Bin,et al."Nanomolar Antimalarial Agents against Chloroquine-Resistant Plasmodium falciparum from Medicinal Plants and Their Structure-Activity Relationships".JOURNAL OF NATURAL PRODUCTS 80.1(2017):96-107. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。