Tetrahydroberberine

The barks of Phellodendron chinense Schneid.

Tetrahydroberberine, an isoquinoline alkaloid isolated from corydalis tuber, enhances gastrointestinal motor function.[Pubmed:21659472]

J Pharmacol Exp Ther. 2011 Sep;338(3):917-24.

Because delayed gastric emptying and impaired gastric accommodation are regarded as pathophysiological mechanisms underlying functional dyspepsia (FD), prokinetics and fundic relaxants have been suggested as a new treatment for FD. We isolated Tetrahydroberberine (THB), an isoquinoline alkaloid (5,8,13,13a-tetrahydro-9,10-dimethoxy-6H-benzo[g]-1,3-benzodioxolo[5,6-a]quinoliz ine) from Corydalis tuber, and found that it has micromolar affinity for dopamine D(2) (pK(i) = 6.08) and 5-HT(1A) (pK(i) = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors (i.e., 5-HT(1B), 5-HT(1D), 5-HT(3), and 5-HT(4); pK(i) < 5.00). Oral administration of THB not only resulted in significantly accelerated gastric emptying of normal rats in a bell-shaped relationship, with a maximal efficacy at a dose of 30 mug/kg, but also restored the delayed gastric emptying caused by apomorphine, which might be mediated by an antidopaminergic effect. Data from electromyography indicated enhanced motor function of the upper gastrointestinal tract by THB, which occurred through strengthening contractility and shortening the contraction interval. Furthermore, in rats stressed by repeated restraint, a significantly higher shift in the pressure-volume curve by THB (10 mug/kg, p < 0.05), which was inhibited by [O-methyl-3H]-N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclo hexanecarboxamide trihydrochloride (WAY-100635), a 5-HT(1A) antagonist, and N(omega)-nitro-l-arginine methyl ester, a nitric-oxide synthase inhibitor but not a vasoactive intestinal peptide antagonist, was observed. Oral administration of THB resulted in a drastic increase of gastric accommodation in Beagle dogs. Area under the volume versus time curve was increased significantly by THB (30 mug/kg, p < 0.01) and comparable with that of sumatriptan (3 mg/kg), a potent fundic relaxant. Taken together, our data suggested that THB, with D(2) receptor antagonist and 5-HT(1A) receptor agonist properties, has significant potential as a therapeutic for treatment of FD.

Tetrahydroberberine suppresses dopamine-induced potassium current in acutely dissociated CA1 pyramidal neurons from rat hippocampus.[Pubmed:8728473]

Neurosci Lett. 1996 Apr 5;207(3):155-8.

Effects of Tetrahydroberberine (THB) on dopamine (DA)-induced response have been investigated in single pyramidal neurons freshly dissociated from CA1 area of the hippocampus using the nystatin perforated patch-clamp, whole-cell recording technique under voltage-clamp configuration. At a holding potential (VH) of -20mV, DA-induced responses included a transient outward current, a slow inward current and a combination of the two. The outward current had a reversal potential of -83.5 +/- 8.0 mV which was close to K+ equilibrium potential and was sensitive to TEA, suggesting that this outward current was carried by K+. Application of THB reversibly suppressed three type responses induced by DA with different degrees of inhibitory ratio. THB inhibited the DA-induced outward current in a concentration-dependent manner with an IC50 of 13 microM. The maximal value of the concentration-response curve for DA-induced outward current was suppressed by THB, suggesting a non-competitive inhibition. The results support the hypothesis that THB acts as a novel dopaminergic system antagonist. Furthermore, THB inhibits the DA-induced K+ current non-competitively in single dissociated cells, implying that THB may exhibit other pharmacological action on the central nervous system.

Tetrahydroberberine, a pharmacologically active naturally occurring alkaloid.[Pubmed:25836282]

Acta Crystallogr C Struct Chem. 2015 Apr;71(Pt 4):262-5.

Tetrahydroberberine (systematic name: 9,10-dimethoxy-5,8,13,13a-tetrahydro-6H-benzo[g][1,3]benzodioxolo[5,6-a]quinolizi ne), C20H21NO4, a widely distributed naturally occurring alkaloid, has been crystallized as a racemic mixture about an inversion center. A bent conformation of the molecule is observed, with an angle of 24.72 (5) degrees between the arene rings at the two ends of the reduced quinolizinium core. The intermolecular hydrogen bonds that play an apparent role in crystal packing are 1,3-benzodioxole -CH2...OCH3 and -OCH3...OCH3 interactions between neighboring molecules.

Inhibitory effect of tetrahydroberberine on platelet aggregation and thrombosis.[Pubmed:8010106]

Zhongguo Yao Li Xue Bao. 1994 Mar;15(2):133-5.

Tetrahydroberberine (THB), an alkaloid extracted from Corydalis ambigua, inhibited the rabbit platelet aggregation triggered by arachidonic acid (AA), ADP, and collagen with IC50 of 0.86, 1.31, and 1.10 mmol.L-1, respectively. THB reduced the thromboxane B2 (TXB2) generation in rabbit platelet-rich plasma triggered by AA. THB 30 mg.kg-1.d-1 ip for 3 or 5 d restrained the ADP-induced platelet aggregation in rats. THB 30 mg.kg-1.d-1 ip for 1, 3, or 5 d inhibited the AA-induced platelet aggregation in rats. THB 15-30 mg.kg-1 iv showed an inhibition of venous thrombosis in rats. The results show that THB is a potent inhibitor of platelet aggregation in vitro and in vivo and is a promising antithrombotic drug.

Tetrahydroberberine is an isoquinoline alkaloid isolated from corydalis tuber; has micromolar affinity for dopamine D(2) (pK(i) = 6.08) and 5-HT(1A) (pK(i) = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors (5-HT(1B), 5-HT(1D), 5-HT(3), and 5-HT(4); pK(i) < 5.00).

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