[Effects of Buyang Huanwu Decoction and its alkaloids and glycosides on aortic intimal hyperplasia and expression of proliferating cell nuclear antigen in rats with aortic intimal injuries].

OBJECTIVE: To explore the effects of alkaloids and glycosides extracted from Buyang Huanwu Decoction (BYHWD), a compound of traditional Chinese herbal medicine, on aortic intimal hyperplasia and the expression of the proliferating cell nuclear antigen (PCNA) in rats with aortic intimal injuries. METHODS: The vessel restenosis model was established by denuding aortic endothelium with domestic balloon catheter in rats. Drugs were administered intragastrically on the first day after operation. The injured segments of aorta were taken on the fifteenth day after operation to determine the degree of intimal hyperplasia and observe the expression of PCNA. RESULTS: Aortic intimal hyperplasias were very obvious on the fifteenth day after operation. The media hyperplasias in the drug-treated groups were not significant (P>0.05), but the intimal hyperplasia were remarkable as compared with that in the sham-operated group (P<0.01). The degrees of intimal hyperplasia in BYHWD, alkaloids, glycosides and atorvastatin groups were less than that in the untreated group (P<0.01). There was significant difference of PCNA expression between the untreated group and the sham-operated group (P<0.01). The expressions of PCNA in alkaloids, glycosides, and atorvastatin groups were higher than that in the sham-operated group (P<0.01, P<0.05), but still lower than that in the untreated group (P<0.01). The expression of PCNA in BYHWD group was higher than that in the sham-operated group (P<0.01), and no significant difference was found between the BYHWD group and the untreated group (P>0.05). CONCLUSION: Alkaloids and glycosides extracted from BYHWD can inhibit intimal hyperplasia induced by denuding arterial endothelium with domestic balloon catheter in rats. Alkaloids and glycoside may be among basal substances in BYHWD inhibiting intimal hyperplasia of blood vessel, the effect of which may relate to down-regulating the expression of PCNA.

Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.

N1-Arylsulfonyltryptamines have been identified as 5-HT6 receptor ligands. In particular, N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine (11q) is a high affinity, potent full agonist (5-HT6 Ki = 2 nM, EC50 = 6.5 nM, Emax = 95.5%). Compound 11q is selective in a panel of over 40 receptors and ion channels, has good pharmacokinetic profile, has been shown to increase GABA levels in the rat frontal cortex, and is active in the schedule-induced polydipsia model for obsessive compulsive disorders.