Discovery of novel coffee diterpenoids with inhibitions on Ca(v)3.1 low voltage-gated Ca2+ channel

doi:10.1016/j.foodchem.2021.131923

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	Discovery of novel coffee diterpenoids with inhibitions on Ca(v)3.1 low voltage-gated Ca2+ channel
	Hu,Guilin ; Dong,Ding ; Du,Shuzong ; Peng,Xingrong ; Wu,Mingkun ; Shi,Qiangqiang ; Hu,Kun; Hong,Defu ; Wang,Xiaoyuan ; Zhou,Lin ; Nian,Yin; Qiu,Minghua
	2022
发表期刊	FOOD CHEMISTRY
ISSN	0308-8146
卷号	376 页码:131923
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.
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
DOI	10.1016/j.foodchem.2021.131923
WOS记录号	WOS:000741200300008
引用统计
文献类型	期刊论文
条目标识符	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 Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Chinese Acad Sci, Kunming Inst Zool, Key Lab Anim Models & Human Dis Mech, Kunming 650223, Yunnan, Peoples R China 4.Chinese Acad Sci, Kunming Inst Zool, Ion Channel Res & Drug Dev Ctr, 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.

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