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Staurosporine Derivatives Generated by Pathway Engineering in a Heterologous Host and Their Cytotoxic Selectivity
Xiao, Fei1; Li, Huayue1,2; Xu, Mingyuan1; Li, Tong1; Wang, Ju3; Sun, Chaomin2,3; Hong, Kui4; Li, Wenli1,2
2018-08-01
Source PublicationJOURNAL OF NATURAL PRODUCTS
ISSN0163-3864
Volume81Issue:8Pages:1745-1751
Corresponding AuthorLi, Wenli(liwenli@ouc.edu.cn)
AbstractTwo 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.
DOI10.1021/acs.jnatprod.8b00103
Indexed BySCI
Language英语
Funding ProjectNational Natural Science Foundation of China[41506157] ; National Natural Science Foundation of China[31570032] ; NSFC-Shandong Joint Foundation[U1706206] ; NSFC-Shandong Joint Foundation[U1406403]
WOS Research AreaPlant Sciences ; Pharmacology & Pharmacy
WOS SubjectPlant Sciences ; Chemistry, Medicinal ; Pharmacology & Pharmacy
WOS IDWOS:000443103700006
PublisherAMER CHEMICAL SOC
Citation statistics
Document Type期刊论文
Identifierhttp://ir.qdio.ac.cn/handle/337002/159928
Collection实验海洋生物学重点实验室
Corresponding AuthorLi, Wenli
Affiliation1.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
Recommended Citation
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.
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