Guan-fu base A
Guan-fu base A
CAS: 1394-48-5
Molecular Formula: C24H31NO6
Guan-fu base A - Names and Identifiers
| Name | Guan-fu base A |
| Synonyms | BRN 5165899 Acehytisine Kwan-fu base A Guan-fu base A Kwan-Fu Base A (2α,11α,13R)-Hetisan-2,11,13,14-tetrol 2,11-diacetate Hetisan-2,11,13,14-tetrol,2,13-diacetate, (2a,11a,13R)- Hetisan-2,11,13,14-tetrol, 2,13-diacetate, (2α,11α,13R)- (2alpha,11alpha,13R)-Hetisan-2,11,13,14-tetrol 2,13-diacetate Hetisan-2,11,13,14-tetrol, 2,11-diacetate, (2-alpha,11-alpha,13R)- (2alpha,9xi,11alpha,20xi)-11,14-dihydroxyhetisan-2,13-diyl diacetate |
| CAS | 1394-48-5 |
| InChI | InChI=1/C24H31NO6/c1-10-5-22-8-14-17-21(4)6-13(30-11(2)26)7-23(17)18(22)16(28)15(10)19(31-12(3)27)24(22,29)20(23)25(14)9-21/h13-20,28-29H,1,5-9H2,2-4H3/t13-,14?,15+,16+,17+,18?,19?,20?,21-,22?,23?,24-/m0/s1 |
Guan-fu base A - Physico-chemical Properties
| Molecular Formula | C24H31NO6 |
| Molar Mass | 429.51 |
| Density | 1.43±0.1 g/cm3(Predicted) |
| Boling Point | 541.5±50.0 °C(Predicted) |
| Specific Rotation(α) | (CHCl3)+49 |
| Flash Point | 281.3°C |
| Solubility | Soluble in methanol, ethanol, DMSO and other organic solvents |
| Vapor Presure | 5.55E-14mmHg at 25°C |
| Appearance | White crystal |
| pKa | 12.97±0.70(Predicted) |
| Storage Condition | 2-8℃ |
| Refractive Index | 1.648 |
| Physical and Chemical Properties | White Crystal, soluble in methanol, ethanol, DMSO and other organic solvents, derived from the root of the plant of the family of Ranunculaceae. |
| In vitro study | 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. |
| In vivo study | 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. |
Guan-fu base A - Reference Information
| overview | Guanfu A is one of the main active substances in Aconitum chrysalis of Ranunculaceae. Preclinical pharmacological studies have shown that Guanfu A hydrochloride can resist high calcium, coronary artery ligation and aconitine-induced ventricular tachycardia and ventricular fibrillation, and can resist acetylcholine-induced atrial flutter and atrial fibrillation; It can reduce the Vmax of the fast response action potential to the myocardium in a concentration-dependent manner. |
| Biological activity | Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum. It is an effective non-competitive CYP2D6 inhibitor. The Ki of human liver microsomes (HLM) is 1.20 μM, and the Ki of human recombinant (rCYP2D6) is 0.37 μM. Guanfu base A is also a potent competitive inhibitor of CYP2D, with Ki of 0.38 μM and 2.4 μM for microsomes of monkeys and dogs, respectively. Guanfu base A can also suppress HERG channel current. |
| target | CYP2D6; HERG channel |
| use | guanfu a has antiarrhythmic effect. |
Last Update：2024-04-10 22:29:15
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