关附甲素
| 中文名称 | 关附甲素 |
|---|---|
| 中文同义词 | 关附甲素;关附甲素,关白附子甲素;关白附子甲素;盐酸关附甲素,关白附子甲素;盐酸关附甲素标准品;关附素A;关附甲素标准品;关附甲素对照品 |
| 英文名称 | Guan-fu base A |
| 英文同义词 | Guan-fu base A;(2α,11α,13R)-Hetisan-2,11,13,14-tetrol 2,11-diacetate;(2alpha,11alpha,13R)-Hetisan-2,11,13,14-tetrol 2,13-diacetate;Acehytisine;Kwan-fu base A;Hetisan-2,11,13,14-tetrol, 2,13-diacetate, (2α,11α,13R)-;Hetisan-2,11,13,14-tetrol,2,13-diacetate, (2a,11a,13R)-;Guan-fu base A USP/EP/BP |
| CAS号 | 1394-48-5 |
| 分子式 | C24H31NO6 |
| 分子量 | 429.51 |
| EINECS号 | |
| 相关类别 | 植物提取物;中药对照品;标准品;中草药成分;标准品 -中药标准品;生物碱 |
| Mol文件 | 1394-48-5.mol |
| 结构式 |  |
关附甲素 性质
| 沸点 | 541.5±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.43±0.1 g/cm3(Predicted) |
| 储存条件 | 4°C, away from moisture and light |
| 酸度系数(pKa) | 12.97±0.70(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
| InChIKey | OGNUSOJAYIHLNS-UFZRWAKRNA-N |
| SMILES | O[C@]12[C@@H]([C@]3([H])C(=C)CC41C[C@@]1([H])[C@]5([H])[C@]6(C[C@H](OC(=O)C)C[C@]5([C@]4([H])[C@@H]3O)C2N1C6)C)OC(=O)C |&1:1,2,3,10,12,14,16,22,23,25,r| |
CYP2D6; HERG channel
Guanfu base A has no inhibitory activity on mouse or rat CYP2Ds. Guanfu base A does not exhibit any inhibition activity on human recombinant CYP1A2, 2A6, 2C8, 2C19, 3A4, or 3A5, but shows slight inhibition of 2B6 and 2E1.
Guanfu base A is a potent inhibitor of CYP2D6, with an
IC
50
recorded at ~0.46 μM in HLM (Dextromethorphan 5 μM) and 0.12 μM in rCYP2D6 (Bufuralol 5 μM).
The effects of Guanfu base A is investigated in human embryonic kidney 293 (HEK293) cells transiently transfected with HERG complementary DNA using a whole-cell patch clamp technique. Guanfu base A inhibits HERG channel current in concentration-, voltage-, and time-dependent manners with an
IC
50
of 1.64 mM. Guanfu base A shifts the activation curve in a negative direction and accelerated channel inactivation but shows no effect on the inactivation curve.
Beagle dogs treated intravenously with Dextromethorphan (2 mg/mL) after pretreatment with Guanfu base A injection shows reduced CYP2D metabolic activity, with the C max of dextrorphan being one-third that of the saline-treated group and area under the plasma concentration-time curve half that of the saline-treated group.