| Description: |
Allocryptopine has certain effects on anti-injury for hepatocyte, ameliorating liver function, and prohibiting hepatic fibrosis; it increases mRNA levels of cytochromes P450 1A in human hepatocytes and HepG2 cells independently of AhR. Allocryptopine induces a relaxing effect on the ileum by inhibiting phosphodiesterase enzyme, and thus elevating cellular cAMP and its contractile effect on the urinary bladder by affecting alpha-adrenergic receptors in this tissue, it can block human ether-a-go-go related gene (hERG) potassium channels expressed in HEK293 cells. |
| Targets: |
cAMP | P450 (e.g. CYP17) | Potassium channel |
| In vitro: |
| Acta Pharmacol Sin. 2013 Jun;34(6):847-58. | | Allocryptopine and benzyltetrahydropalmatine block hERG potassium channels expressed in HEK293 cells.[Pubmed: 23524574] | Allocryptopine (ALL) is an alkaloid extracted from Corydalis decumbens (Thunb) Pers. Papaveraceae, whereas benzyltetrahydropalmatine (BTHP) is a derivative of tetrahydropalmatine extracted from Corydalis ambigua (Pall) Cham et Schlecht. The aim of this study was to investigate the effects of ALL and BTHP on the human ether-a-go-go related gene (hERG) current expressed in HEK293 cells.
METHODS AND RESULTS:
Cultured HEK293 cells were transiently transfected with hERG channel cDNA plasmid pcDNA3.1 using Lipofectamine. The whole-cell current IHERG was evoked and recorded using Axon MultiClamp 700B amplifier. The drugs were applied via supserfusion.
Both ALL and BTHP reversibly suppressed the amplitude and density of IHERG in concentration- and voltage-dependent manners (the respective IC50 value was 49.65 and 22.38 μmol/L). BTHP (30 μmol/L) caused a significant negative shift of the steady-state inactivation curve of IHERG, while ALL (30 μmol/L) did not affect the steady-state inactivation of IHERG. Furthermore, BTHP, but not ALL, shortened the time constants of fast inactivation and slow time constants of deactivation of IHERG. But both the drugs markedly lengthened the time constants for recovery of IHERG from inactivation. Using action potential waveform pulses, it was found that both the drugs at 30 μmol/L significantly suppressed the current densities in the late phase of action potential, but did not significantly affect the current densities in the early phase of action potential.
CONCLUSIONS:
Both ALL and BTHP derived from Chinese herbs potently block hERG current. |
|
| In vivo: |
| Gen Pharmacol. 1997 Oct;29(4):621-3. | | Effects of allocryptopine, an alkaloid isolated from Glaucium arabicum on rat isolated ileum and urinary bladder.[Pubmed: 9352312] | 1. The alkaloid, Allocryptopine, was isolated from the chloroform extract of Glaucium arabicum.
METHODS AND RESULTS:
2. The effect of Allocryptopine on urinary bladder and ileal smooth muscles was investigated in this study. 3. Allocryptopine, in concentrations from 1 x 10(-5) to 3 x 10(-3) M caused a concentration-dependent contraction of rat isolated urinary bladder and a concentration-dependent relaxation of rat ileal smooth muscles. 4. Theophylline (10(-5) M) shifted to the left the Allocryptopine concentration-effect curve on ileum and increased the maximum inhibitory effect of Allocryptopine. 5. Methylene blue (10(-3) M) had no significant effect on the concentration-effect curve of Allocryptopine of the ileum. 6. Phentolamine (10(-6) M) shifted to the right the Allocryptopine concentration-effect curve of urinary bladder.
CONCLUSIONS:
7. These observations suggest that Allocryptopine induces a relaxing effect on the ileum by inhibiting phosphodiesterase enzyme, and thus elevating cellular cAMP and its contractile effect on the urinary bladder by affecting alpha-adrenergic receptors in this tissue. |
|
Cell. 2018 Jan 11;172(1-2):249-261.e12. doi: 10.1016/j.cell.2017.12.019.IF=36.216(2019)
Cell Metab. 2020 Mar 3;31(3):534-548.e5. doi: 10.1016/j.cmet.2020.01.002.IF=22.415(2019)
Mol Cell. 2017 Nov 16;68(4):673-685.e6. doi: 10.1016/j.molcel.2017.10.022.IF=14.548(2019)
ACS Nano. 2018 Apr 24;12(4): 3385-3396. doi: 10.1021/acsnano.7b08969.IF=13.903(2019)
Nature Plants. 2016 Dec 22;3: 16206. doi: 10.1038/nplants.2016.205.IF=13.297(2019)
Sci Adv. 2018 Oct 24;4(10): eaat6994. doi: 10.1126/sciadv.aat6994.IF=12.804(2019)
