Corydalis yanhusuo,Corydalis conspersa
13aβ-Berbine, 2,3,9,10-tetramethoxy-13α-methyl-/(13S,13aR)-2,3,9,10-tetramethoxy-13-methyl-6,8,13,13a-tetrahydro-5H-isoquinolino[2,1-b]isoquinoline/d-Corydalin/(13S,13aR)-2,3,9,10-Tetramethoxy-13-methyl-5,8,13,13a-tetrahydro-6H-isoquinolino[3,2-a]isoquinoline/(13S-trans )-5,8,13,13a-Tetrahydro-2,3,9,10-tetramethoxy-13-methyl-6H-dibenzo[a,g]quinolizine/Corydaline (+)/6H-Dibenzo[a,g]quinolizine, 5,8,13,13a-tetrahydro-2,3,9,10-tetramethoxy-13-methyl-, (13S,13aR)-/Berbine,2,3,9,10-tetramethoxy-13-methyl/2,3,9,10-Tetramethoxy-13a-methyl-13ab-berbine/(13S,13aR)-2,3,9,10-Tetramethoxy-13-methyl-5,8,13,13a-tetrahydro-6H-isoquino[3,2-a]isoquinoline/Corydalin/Corydaline
10 mM in DMSO
482.3±45.0 °C at 760 mmHg
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For Reference Standard and R&D, Not for Human Use Directly.
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1. Corydaline, an isoquinoline alkaloid, is one of the major active constituents in a new prokinetic botanical agent, DA-9701. It has been recommended that preclinical pharmacokinetic studies of natural medicines include both genders. Therefore, in this study, the pharmacokinetics of corydaline in male and female rats was evaluated following intravenous and oral administration of pure corydaline or DA-9701. 2. After intravenous administration of corydaline, the area under the plasma concentration-time curve (AUC) was significantly greater (by 46.4%) in female rats compared to male rats due to a 29.3% reduction in non-renal clearance in female rats. The gender difference in corydaline hepatic metabolic clearance was supported by a significantly slower metabolism of corydaline in hepatic microsomes of female rats mediated via male-specific (CYP2C11 and CYP3A2) or male-dominant (CYP3A1) CYP isozymes. 3. Following oral administration of pure corydaline or DA-9701, the AUC and Cmax values of corydaline in female rats were significantly greater (by 793% and 466% increase for corydaline administration or by 501% and 143% increase for DA-9701 administration) than in male rats. Greater F values of corydaline in female rats could be due to smaller hepatic first-pass extraction as a result of slower hepatic metabolism of corydaline. 4. However, we observed a comparable disappearance of corydaline in male and female human liver microsomes, consistent with little gender difference in CYP2C9 and CYP3A activities in humans compared to that in rats. Thus, gender differences in corydaline metabolism are not expected to occur in humans.
CYP2C; CYP3A; Corydaline; DA-9701; gender; pharmacokinetics; rats
Gender differences in corydaline pharmacokinetics in rats.
Jung JW1, Choi MR, Kwon YS, Jeong JS, Son M, Kang HE.
Enterovirus 71 (EV71) is a huge threat to the worldwide public health and there is no approved antiviral drug for EV71-induced disease therapy. Corydaline exists antiallergic and antinociceptive activities, but the anti-EV71 activity of corydaline is still not reported. In this study, corydaline could suppress the expression of viral structural and non-structural proteins. Furthermore, corydaline inhibits EV71 replication by suppressing the COX-2 expression and the phosphorylation of JNK MAPK and P38 MAPK but not ERK MAPK in vitro. Based on these findings, corydaline could be a potential lead or supplement for the development of new anti-EV71 agents in the future.
COX-2; Corydaline; MAPK; enterovirus 71
Corydaline inhibits enterovirus 71 replication by regulating COX-2 expression.
Wang HQ1, Hu J1, Yan HY1, Wu S1, Li YH1.
1. Corydaline, an isoquinoline alkaloid obtained from the rhizomes of Corydalis yanhusuo, exhibits anti-acetylcholinesterase, anti-angiogenic, anti-allergic and gastric-emptying activities. In this study, a rapid and reliable ultra-performance liquid chromatography coupled to quadrupole time-of-flight mass spectrometry (UPLC-Q/TOF-MS) method was developed and employed for the comprehensive study of the metabolites of corydaline in rats. 2. Altogether, 43 metabolites were identified in the plasma (11), bile (9), urine (34) and feces (21) of rats after oral administration of corydaline at a dose of 4.5mg/kg. 3. It was demonstrated that demethylation, hydroxylation, sulfation and glucuronidation were the major metabolic transformation pathways. Among these, two metabolites were identified as tetrahydropalmatine and isocorybulbine, and 33 phase I and phase II products were inferred to be new metabolites arising from the in vivo metabolism of corydaline. 4. Importantly, this research provides scientific and reliable support for full understanding of the metabolic profiles of corydaline and the results could help to elucidate its safety and efficacy
Corydaline; UPLC-Q/TOF-MS; identification; in rats; metabolites
Metabolic profiles of corydaline in rats by ultra-performance liquid chromatography coupled to quadrupole time-of-flight mass spectrometry.
Chai L1,2, Donkor PO1,2,3, Wang K1,2, Sun Y1,2, Oppong MB1,4, Wang K1, Ding L2, Qiu F1,2.
Corydaline is an acetylcholinesterase inhibitor isolated from Corydalis yanhusuo.