IR@PKUHSC  > 北京大学基础医学院  > 药理学系
Endothelium-dependent vasorelaxant and antiproliferative effects of apigenin
Zhang, YH; Park, YS; Kim, TJ; Fang, LH; Ahn, HY; Hong, JT; Kim, Y; Lee, CK; Yun, YP
Source PublicationGENERAL PHARMACOLOGY-THE VASCULAR SYSTEM
2000-12-01
Volume35Issue:6Pages:341-347
Indexed BySCI
Abstract

This study was designed to determine whether the relaxant effect of apigenin was endothelium dependent and to examine the possible antiproliferative effect of apigenin. Apigenin relaxed the phenylephrine-precontracted endothelium-intact aortic rings with IC50 value of 3.7+/-0.5 muM and removal of a functional endothelium significantly attenuated this relaxation (IC50 = 8.2+/-0.9 muM). However, apigenin did not affect the 0.1 muM phorbol 12,13-dibutyrate-induced contraction (IC50 = 34.6 +/- 1.2 muM) within the concentration range that relaxed the phenylephrine-contracted arteries, suggesting that apigenin did not influence protein kinase C-mediated contractile mechanisms in rat aorta. Pretreatment of apigenin significantly potentiated the relaxant effect of acetylcholine on phenylephrine-induced contraction. Pretreatment with N-G-nitro-L-arginine methyl ester (L-NAME) or methylene blue reduced the relaxant effect of apigenin. Apigenin (10 muM) increased the guanosine 3′,5′-cyclic monophosphate (cGMP) content of endothelium-intact tissues. Pretreatment with L-NAME (100 muM) or removal of endothelium significantly suppressed the effect of apigenin on cGMP production. In addition, apigenin significantly inhibited [H-3]thymidine incorporation into DNA of primary cultured rat aortic smooth muscle cell in a dose-dependent manner. These findings suggest that besides influx and release of Ca2+, nitric oxide (NO) and cGMP may account for the apigenin-induced endothelium-dependent relaxation and hypotensive activity. Both vasorelaxant and antiproliferative activities may contribute to a benefit of apigenin in the vascular system. (C) 2002 Elsevier Science Inc. All rights reserved.

KeywordApigenin Nitric Oxide Cgmp Vasorelaxation Proliferation Rat Aorta
Subject Area基础医学
SubtypeArticle
WOS HeadingsScience & Technology
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS KeywordSMOOTH-MUSCLE CELL ; PROTEIN-KINASE-C ; NITRIC-OXIDE ; METHYLENE-BLUE ; GUINEA-PIG ; FLAVONOIDS ; ATHEROSCLEROSIS ; PROLIFERATION ; INHIBITION ; RELAXATION
WOS IDWOS:000177023800008
Citation statistics
Cited Times:35[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.bjmu.edu.cn/handle/400002259/62562
Collection北京大学基础医学院_药理学系
北京大学基础医学院
Affiliation1.Chungbuk Natl Univ, Coll Pharm, Heungduk Gu, Cheongju 361763, Chungbuk, South Korea
2.Peking Univ, Sch Basic Med Sci, Dept Pharmacol, Beijing 100083, Peoples R China
3.Chungbuk Natl Univ, Res Ctr Bioresource & Hlth, Cheongju 361763, South Korea
4.Chungbuk Natl Univ, Coll Med, Cheongju 361763, South Korea
Recommended Citation
GB/T 7714
Zhang, YH,Park, YS,Kim, TJ,et al. Endothelium-dependent vasorelaxant and antiproliferative effects of apigenin[J]. GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM,2000,35(6):341-347.
APA Zhang, YH.,Park, YS.,Kim, TJ.,Fang, LH.,Ahn, HY.,...&Yun, YP.(2000).Endothelium-dependent vasorelaxant and antiproliferative effects of apigenin.GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM,35(6),341-347.
MLA Zhang, YH,et al."Endothelium-dependent vasorelaxant and antiproliferative effects of apigenin".GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM 35.6(2000):341-347.
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