| Discovery of novel coffee diterpenoids with inhibitions on Ca(v)3.1 low voltage-gated Ca2+ channel |
| Hu, GL; Dong, D; Du, SZ; Peng, XR; Wu, MK; Shi, QQ; Hu, K; Hong, DF; Wang, XY; Zhou, L; Nian, Y; Qiu, MH
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| 2022
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| 发表期刊 | FOOD CHEMISTRY
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| ISSN | 0308-8146
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| 卷号 | 376 |
| 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. |
| 收录类别 | sci
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| 语种 | 英语
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| 文献类型 | 期刊论文
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| 条目标识符 | http://ir.kiz.ac.cn/handle/152453/13788
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| 专题 | 科研部门_天然药物功能蛋白质学科组（赖仞）
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推荐引用方式
GB/T 7714 |
Hu, GL,Dong, D,Du, SZ,et al. Discovery of novel coffee diterpenoids with inhibitions on Ca(v)3.1 low voltage-gated Ca2+ channel[J]. FOOD CHEMISTRY,2022,376.
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| APA |
Hu, GL.,Dong, D.,Du, SZ.,Peng, XR.,Wu, MK.,...&Qiu, MH.(2022).Discovery of novel coffee diterpenoids with inhibitions on Ca(v)3.1 low voltage-gated Ca2+ channel.FOOD CHEMISTRY,376.
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| MLA |
Hu, GL,et al."Discovery of novel coffee diterpenoids with inhibitions on Ca(v)3.1 low voltage-gated Ca2+ channel".FOOD CHEMISTRY 376(2022).
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