STUDIES OF HETEROCYCLIC-COMPOUNDS .8. SYNTHESIS, ANTIINFLAMMATORY AND ANTIALLERGIC ACTIVITIES OF N-ALKYL-2,3,4,9-TETRAHYDROFURO[2,3-B]QUINOLINE-3,4-DIONES AND RELATED-COMPOUNDS

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Title:	STUDIES OF HETEROCYCLIC-COMPOUNDS .8. SYNTHESIS, ANTIINFLAMMATORY AND ANTIALLERGIC ACTIVITIES OF N-ALKYL-2,3,4,9-TETRAHYDROFURO[2,3-B]QUINOLINE-3,4-DIONES AND RELATED-COMPOUNDS
Authors:	KUO, SC;HUANG, SC;HUANG, LJ;CHENG, HE;LIN, TP;WU, CH;ISHII, K;NAKAMURA, H
Contributors:	藥學院藥學系;CHINA MED COLL,SCH PHARM,TAICHUNG 40421,TAIWAN;DAINIPPON PHARMACEUT CO LTD,RES LABS,SUITA,OSAKA 564,JAPAN
Date:	1991
Issue Date:	2010-09-24 18:54:43 (UTC+8)
Publisher:	HETERO CORPORATION
Abstract:	The possible mechanism underlying the vasorelaxant effect of emodin isolated from a Chinese herb, was investigated in this study. Emodin dose dependently relaxed isolated vascular rings of human internal mammary artery and saphenous vein, rabbit thoracic aorta, abdominal aorta and mesenteric artery, and rat thoracic aorta. There were no differences in the sensitivity (IC50) and maximal relaxation between intact and endothelium-denuded preparations of rat aorta. In the presence of emodin (10-mu-M), the contractile responses of rat aorta to phenylephrine, serotonin and potassium chloride were depressed. The relaxation response to acetylcholine was attenuated by emodin, whereas that to isoproterenol was unaffected. The relaxation response to emodin was inhibited by free radical scavengers, superoxide dismutase, catalase and mannitol, and guanylate cyclase inhibitors, methylene blue and hemoglobin. Catalase was the most effective scavenger. Quinacrine (phospholipase A2 inhibitor), indomethacin (cyclooxygenase inhibitor) and nordihydroguaiaretic acid (NDGA, lipoxygenase inhibitor) potentiated the relaxation induced by emodin. NDGA was the most effective potentiator. Exposure of aortic rings to emodin (10-mu-M) increased the basal level of guanosine 3',5'-cyclic monophosphate (cGMP). It is suggested that the vasorelaxant effect of emodin may be mainly due to cGMP accumulation as a result of guanylate cyclase activation by free radicals and/or hydrogen peroxide generated from semiquinone.
Relation:	JOURNAL OF HETEROCYCLIC CHEMISTRY 28(4):955-963
Appears in Collections:	[School of Pharmacy/Master Degree Program, Ph. D program] Journal articles

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