Nanomolar Antimalarial Agents against Chloroquine-Resistant Plasmodium falciparum from Medicinal Plants and Their Structure-Activity Relationships

doi:10.1021/acs.jnatprod.6b00744

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	Nanomolar Antimalarial Agents against Chloroquine-Resistant Plasmodium falciparum from Medicinal Plants and Their Structure-Activity Relationships
	Zhou, Bin 1,2; Wu, Yan 1,2; Dalal, Seema 3; Merino, Emilio F.3; Liu, Qun-Fang1,2 ; Xu, Cheng-Hui 1,2; Yuan, Tao 1,2; Ding, Jian1,2 ; Kingston, David G. I.4,5; Cassera, Maria B.3
刊名	JOURNAL OF NATURAL PRODUCTS
	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.
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关键词	CHLORANTHUS-JAPONICUS ; CHEMICAL-CONSTITUENTS ; SESQUITERPENOID DIMERS ; ARTEMISININ RESISTANCE ; SARCANDRA-GLABRA ; C-F ; SPICATUS ; MULTISTACHYS ; SERRATUS ; ROOTS
WOS研究方向	Plant Sciences ; Pharmacology & Pharmacy
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000393089600014
内容类型	期刊论文
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.