Staurosporine Derivatives Generated by Pathway Engineering in a Heterologous Host and Their Cytotoxic Selectivity

doi:10.1021/acs.jnatprod.8b00103

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	Staurosporine Derivatives Generated by Pathway Engineering in a Heterologous Host and Their Cytotoxic Selectivity
	Xiao, Fei 1; Li, Huayue 1,2; Xu, Mingyuan 1; Li, Tong 1; Wang, Ju 3; Sun, Chaomin 2,3; Hong, Kui 4; Li, Wenli 1,2
刊名	JOURNAL OF NATURAL PRODUCTS
	2018-08-01
卷号	81 期号:8 页码:1745-1751
ISSN号	0163-3864
DOI	10.1021/acs.jnatprod.8b00103
通讯作者	Li, Wenli(liwenli@ouc.edu.cn)
英文摘要	Two new staurosporine derivatives, staurosporines M1 and M2 (4 and 5), in addition to five previously reported metabolites (1-3, 6, and 7), were generated by the heterologous expression of engineered spc gene clusters in Streptomyces coelicolor M1146. The structures of these derivatives were determined by a combination of spectroscopic methods and CD measurement. Compounds 1, 2, 4, and 5 showed effective activities against three tumor cell lines (HCT-116, K562, and Huh 7.5), and 3 was active against HCT-116 and K562 cells. In addition, compounds 3 and 5 showed undetectable toxicity up to 100 mu M toward the normal hepatic cell line LO2. Based on the IC50 values, their structure and activity relationships are discussed.
资助项目	National Natural Science Foundation of China[41506157] ; National Natural Science Foundation of China[31570032] ; NSFC-Shandong Joint Foundation[U1706206] ; NSFC-Shandong Joint Foundation[U1406403]
WOS研究方向	Plant Sciences ; Pharmacology & Pharmacy
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000443103700006
内容类型	期刊论文
源URL	[http://ir.qdio.ac.cn/handle/337002/159927]
专题	海洋研究所_实验海洋生物学重点实验室
通讯作者	Li, Wenli
作者单位	1.Ocean Univ China, Key Lab Marine Drugs, Minist Educ China, Sch Med & Pharm, Qingdao 266003, Peoples R China 2.Qingdao Natl Lab Marine Sci & Technol, Lab Marine Drugs & Bioprod, Qingdao 266000, Peoples R China 3.Chinese Acad Sci, Key Lab Expt Marine Biol, Inst Oceanol, Qingdao 266071, Peoples R China 4.Wuhan Univ, Key Lab Combinatorial Biosynth & Drug Discovery, Minist Educ China, Sch Pharmaceut Sci, Wuhan 430071, Hubei, Peoples R China
推荐引用方式 GB/T 7714	Xiao, Fei,Li, Huayue,Xu, Mingyuan,et al. Staurosporine Derivatives Generated by Pathway Engineering in a Heterologous Host and Their Cytotoxic Selectivity[J]. JOURNAL OF NATURAL PRODUCTS,2018,81(8):1745-1751.
APA	Xiao, Fei.,Li, Huayue.,Xu, Mingyuan.,Li, Tong.,Wang, Ju.,...&Li, Wenli.(2018).Staurosporine Derivatives Generated by Pathway Engineering in a Heterologous Host and Their Cytotoxic Selectivity.JOURNAL OF NATURAL PRODUCTS,81(8),1745-1751.
MLA	Xiao, Fei,et al."Staurosporine Derivatives Generated by Pathway Engineering in a Heterologous Host and Their Cytotoxic Selectivity".JOURNAL OF NATURAL PRODUCTS 81.8(2018):1745-1751.