Knowledge Management System of Kunming Institute of Botany,CAS
| 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
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| 2022 | |
| Source Publication | FOOD CHEMISTRY
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| ISSN | 0308-8146 |
| Volume | 376Pages:131923 |
| Abstract | 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. |
| Keyword | 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 ID | WOS:000741200300008 |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | http://ir.kib.ac.cn/handle/151853/73390 |
| Collection | 中国科学院昆明植物研究所 |
| Affiliation | 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 |
| Recommended Citation 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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