中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Discovery of novel coffee diterpenoids with inhibitions on Ca(v)3.1 low voltage-gated Ca2+ channel

文献类型:期刊论文

作者Hu,Guilin; Dong,Ding; Du,Shuzong; Peng,Xingrong; Wu,Mingkun; Shi,Qiangqiang; Hu,Kun; Hong,Defu; Wang,Xiaoyuan; Zhou,Lin
刊名FOOD CHEMISTRY
出版日期2022
卷号376页码:131923
关键词Coffea arabica L Roasted coffee Coffee diterpenoid Cafestol Kahweol T-type Ca2+ channels Ca(v)3.1 low voltage-gated Ca2+ channel Ca(v)3.1 inhibitors CALCIUM-CHANNELS CAFESTOL KAHWEOL PHYSIOLOGY ESTERS NOMENCLATURE PHARMACOLOGY APOPTOSIS FURANS
ISSN号0308-8146
DOI10.1016/j.foodchem.2021.131923
英文摘要Seven new (1-4, 6-8) diterpenoids with rare skeletons and seven known ones (9, 12, 17, 18 and 23-25) were isolated from roasted beans of Coffea arabica L. Together with previously obtained diterpenoids, a total of 26 molecules (1-25, 4a) were evaluated their activities on Ca(v)3.1 low voltage-gated Ca2+ channel. Compounds 1, 3, 6, 7, 12, 13, 17, 19 and 24 exhibited noticeable Ca(v)3.1 inhibitions (41.2%-96.1%) at 10 mu M. The IC50 values of 1, 6, 7, 12, 13, 17 and 24 are 2.9, 2.3, 0.68, 14.8, 11.6, 6.1 and 6.8 mu M, respectively. The ring moiety at C-18 and C-19, and esterification of OH-17 with long-chain fatty acids seem important for their activities. Further studies indicated that 1 and cafestol may act on different binding sits with the Ca(v)3.1 blocker Z944, which is in clinical trial. Significantly, the present study initially shows that coffee diterpenoids are potential natural resources for Ca(v)3.1 inhibitors.
WOS记录号WOS:000741200300008
源URL[http://ir.kib.ac.cn/handle/151853/73390]  
专题中国科学院昆明植物研究所
作者单位1.Chinese Acad Sci, Kunming Inst Zool, Ion Channel Res & Drug Dev Ctr, Kunming 650223, Yunnan, Peoples R China
2.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China
3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
4.Chinese Acad Sci, Kunming Inst Zool, Key Lab Anim Models & Human Dis Mech, Kunming 650223, Yunnan, Peoples R China
推荐引用方式
GB/T 7714
Hu,Guilin,Dong,Ding,Du,Shuzong,et al. Discovery of novel coffee diterpenoids with inhibitions on Ca(v)3.1 low voltage-gated Ca2+ channel[J]. FOOD CHEMISTRY,2022,376:131923.
APA Hu,Guilin.,Dong,Ding.,Du,Shuzong.,Peng,Xingrong.,Wu,Mingkun.,...&Qiu,Minghua.(2022).Discovery of novel coffee diterpenoids with inhibitions on Ca(v)3.1 low voltage-gated Ca2+ channel.FOOD CHEMISTRY,376,131923.
MLA Hu,Guilin,et al."Discovery of novel coffee diterpenoids with inhibitions on Ca(v)3.1 low voltage-gated Ca2+ channel".FOOD CHEMISTRY 376(2022):131923.

入库方式: OAI收割

来源:昆明植物研究所

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