White crystalline powder
herbs of Uncaria rhynchophylla.
(+/-)-corynoxeine/Corynoxeine/()-corynoxeine/Spiro[3H-indole-3,1'(5'H)-indolizine]-7'-acetic acid, 6'-ethenyl-1,2,2',3',6',7',8',8'a-octahydro-α-(methoxymethylene)-2-oxo-, methyl ester, (αE,3R,6'R,7'S,8'aS)-/ISOCORYNOXEINE/Methyl (7β,16E,20α)-17-methoxy-2-oxocorynoxa-16,18-dien-16-carboxylate
562.7±50.0 °C at 760 mmHg
HS Code Reference
Personal Projective Equipment
For Reference Standard and R&D, Not for Human Use Directly.
provides coniferyl ferulate(CAS#:630-94-4) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate
This study was designed to investigate the vasorelaxant effects and underlying mechanism of isocorynoxeine (ICN), one of the indole alkaloids from Uncaria hooks, on isolated mesenteric arteries in vitro. The myograph system was applied for isometric tension recording in the vascular rings. ICN relaxed both endothelium-intact and endothelium-denuded rat vascular rings precontracted with phenylephrine or KCl in a dose-dependent manner. Propranolol, tetraethylammonium, BaCl2, and glibenclamide had no influence on the vasodilator effect of ICN on phenylephrine-primed vascular rings, while 4-aminopyridine decreased the maximum relaxation. Furthermore, ICN produced a significant drop in maximum response in the PE log concentration-response curve without shifting to the right. In the Ca2+-free Kreb’s-Henseleit buffer, ICN inhibited the contraction in vascular rings evoked by PE, but not by KCl. The phasic contractions of segments in the Ca2+-free Kreb’s-Henseleit buffer induced by CaCl2 were restrained by ICN, while contractions elicited by caffeine displayed no differences. Furthermore, the phasic vasodilation of ICN was significantly lower than controls when pretreated with nifedipine and heparin. Both BAYK8644- and PE-evoked responses were significantly inhibited in the presence of 100 μM of ICN in human vascular smooth muscle cells loaded with the fluorescent Ca2+ indicator Fluo-4-AM. All these results suggest that ICN act in an endothelium-independent manner on the mesenteric artery. Its mechanisms of vasorelaxant action were produced by the inhibition of L-type calcium channel-mediated external Ca2+ influx and α1A-adrenoceptor-mediated intracellular Ca2+ release in vascular smooth muscle cells, and the participation of the Kv channel.
Calcium channel; Isocorynoxeine (ICN); Rat mesenteric artery; Vasorelaxation; α1A-Adrenoceptor antagonist
Endothelium-independent vasodilator effect of isocorynoxeine in vitro isolated from the hook of Uncaria rhynchophylla (Miquel).
Li T1,2, Xu K1,2, Che D1,3, Huang Z4, Jahan N1,2, Wang S5,6.
We recently focused on alkaloids in Uncaria hook (a constituent of the Kampo medicine, yokukansan) and identified the pharmacological action of geissoschizine methyl ether on several G protein-coupled receptors. However, the functions of other identified alkaloids in Uncaria hook, including hirsutine, hirsuteine, rhynchophylline, isorhynchophylline, corynoxeine, isocorynoxeine, are not clear.
To evaluate the effect of seven alkaloids in Uncaria hook (hirsutine, hirsuteine, rhynchophylline, isorhynchophylline, corynoxeine, isocorynoxeine and geissoschizine methyl ether) on the hydroxytryptamine type-3 (5-HT3) receptor ion channel.
We examined the effect of these alkaloids on the current of human 5-HT3 receptors expressed in Xenopus laevis oocytes.
The human 5-HT3A subunit alone for the 5-HT3A receptor, or 5-HT3A and 5-HT3B subunits for the 5-HT3AB receptor, were expressed in Xenopus laevis oocytes. The 5-HT current was measured with or without alkaloid application using a two-electrode voltage clamp.
Each alkaloid, except for geissoschizine methyl ether, weakly inhibited the 5-HT-mediated 5-HT3A and/or 5-HT3AB receptor current, but co-application of these seven alkaloids inhibited the current strongly.
Each alkaloid contributes to antagonism of the 5-HT3 receptor.
Copyright © 2018 Elsevier GmbH. All rights reserved.
5-HT(3); Antagonist; Ion channel; Serotonin receptor; Yi-Gan San; Yokukansan
Yokukansan contains compounds that antagonize the 5-HT3 receptor.
Nakamura Y1, Ishida Y2, Kondo M2, Shimada S2.
2018 Apr 1
An effective separation and simultaneous determination of corynoxeine and its metabolites using high-performance liquid chromatography with tandem mass spectrometry was developed and validated. The method was applied to pharmacokinetics and in vivo distribution investigations in rats after oral (0.105 mmol kg(-1)) and intravenous (0.0105 mmol kg(-1)) doses of corynoxeine. Its brain uptake index was of 3.08 × 10(-11) mol g(-1) at 3 h and 3.75 × 10(-11) mol g(-1) at 74 min after oral and intravenous doses, respectively.
Effective Separation and Simultaneous Determination of Corynoxeine and Its Metabolites in Rats by High-Performance Liquid Chromatography with Tandem Mass Spectrometry and Application to Pharmacokinetics and In Vivo Distribution in Main Organs.
Wang W1, Luo S, Chen Y, Li B, Hattori M.
Corynoxeine, isolated from the hook of Uncaria rhynchophylla, is a potent ERK1/ERK2 inhibitor of key PDGF-BB-induced vascular smooth muscle cells (VSMCs) proliferation.