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Discovery and biological evaluation of a new type of dual inhibitors of indoleamine 2,3-dioxygenase 1 and tryptophan 2,3-dioxygenase from ethnomedicinal plant Dactylicapnos scandens
Bao,Mei-Fen; Yang,Xin-Ni; Wu,Jing; Liu,Jiang-Xin; Cai,Xiang-Hai
2023
发表期刊PHYTOCHEMISTRY
ISSN1873-3700
卷号214页码:113794
摘要The root of Dactylicapnos scandens (D.Don.) Hutch (Papaveraceae), one of the most famous ethno-medicinal plants from the Bai communities in P. R. China, is used to treat various inflammations and tumours. Bioassay guided phytochemical research on D. scandens followed by semi-synthesis led to a series of undescribed tetrahydroisoquinoline alkaloids with dual inhibitory activities against indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO). The previously undescribed dark-green alkaloid dactycapnine A exhibited the best dual inhibitor effects among the identified compounds. Structure-activity relationship analysis revealed the importance of the base skeleton with a hyperconjugation system. The performed semi-synthesis further yielded bioactive dimeric and trimeric compounds with hyperconjugated systems. Performed STD NMR experiments disclosed direct interactions between dactycapnine A and IDO1/TDO. Inhibition kinetics indicated dactycapnine A as a mixed-type dual inhibitor. These findings provided a possible explanation for the anticancer properties of the ethno-medicinal plant species D. scandens.
关键词Dactylicapnos scandens (D. don) hutch. Isoquinoline alkaloids Aporphine-type alkaloids Dactycapnine a IDO1/TDO dual inhibitor APORPHINE ALKALOIDS N-OXIDE INFLAMMATION PATHWAY THALIPORPHINE COMPLEXES CANCER ROOTS
DOI10.1016/j.phytochem.2023.113794
收录类别SCI
WOS记录号WOS:001054551600001
引用统计
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/75527
专题中国科学院昆明植物研究所
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Bao,Mei-Fen,Yang,Xin-Ni,Wu,Jing,et al. Discovery and biological evaluation of a new type of dual inhibitors of indoleamine 2,3-dioxygenase 1 and tryptophan 2,3-dioxygenase from ethnomedicinal plant Dactylicapnos scandens[J]. PHYTOCHEMISTRY,2023,214:113794.
APA Bao,Mei-Fen,Yang,Xin-Ni,Wu,Jing,Liu,Jiang-Xin,&Cai,Xiang-Hai.(2023).Discovery and biological evaluation of a new type of dual inhibitors of indoleamine 2,3-dioxygenase 1 and tryptophan 2,3-dioxygenase from ethnomedicinal plant Dactylicapnos scandens.PHYTOCHEMISTRY,214,113794.
MLA Bao,Mei-Fen,et al."Discovery and biological evaluation of a new type of dual inhibitors of indoleamine 2,3-dioxygenase 1 and tryptophan 2,3-dioxygenase from ethnomedicinal plant Dactylicapnos scandens".PHYTOCHEMISTRY 214(2023):113794.
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