ABSTRACT
AIM:To obtain new typical compounds with dual mechanism,antagonizing Ca2+and inhibiting acetylcholinesterase,on Alzheimer's disease.METHODS:Resorcinol was chosen as primitive substrate,and AD-mix-β as asymmetrically dihydroxylated reagent;all products were screened against acetylcholinesterase in vitro.RESULTS:cis-3′R,4′R-disubstituted angular dihydropyranocoumarins were synthesized enantioselectively,however,its inhibitory activity on acetylcholinesterase is distinctively lower than that of cis-3′R,4′R-disubstituted linear dihydropyranocoumarins.
ABSTRACT
AIM:Bioactive constituents were expected to be obtained from the roots of Angelica morri Hayata. METHOD:They were extracted with 95% alcohol and isolated by using column chromatography and recrystallization methods. The structures were elucidated by means of physico-chemical data and UV,IR,1HNMR, 13CNMR,and EIMS. The inhibitory effect on the constriction of rat aortic rings was induced by K+ or Ca2+. RESULT:3′S-(-)-hamaudol,3′S-(-)-Ο-acetylhamaudol,3′R-(+)-hamaudol,and (±)-hamaudol were isolated from the pieces of Radix Angelica Morri. The inhibitory rate of 3′S-(-)-Ο-acetylhamaudol and (±)-hamaudol on the above pharmacologic model appears the relation of quantity response. CONCLUSION:All the above compounds were found in this species for the first time,and(±)-hamaudol is a new. One of effect mechanisms of 3′S-(-)-Ο-acetylhamaudol and (±)-hamaudol diluted aorta could contribute to be inhibiting Ca2+ influx of vascular smooth muscle.