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标题：Gαq-Protein Carboxyl Terminus Imitation Polypeptide GCIP-27 Attenuates Proliferation of Vascular Smooth Muscle Cells and Vascular Remodeling in Spontaneously Hypertensive Rats
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作者：Hai-Gang Zhang ; Yi-Qun Cheng ; Ya Liu 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2011
卷号：34
期号：10
页码：1527-1532
DOI：10.1248/bpb.34.1527
出版社：The Pharmaceutical Society of Japan
摘要：Gq-protein is located at the convergent point in signal transduction pathways leading to vascular remodeling. The carboxyl terminus of Gα-subunit plays a vital role in G-protein-receptor interaction. The present study was designed to explore the effects of a synthetic Gαq carboxyl terminus imitation peptide, namely GCIP-27, on vascular smooth muscle cells (VSMC) in vitro and vascular remodeling in spontaneous hypertensive rats (SHR). Hyperplasia and hypertrophy of VSMC wre determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, [³H]-thymidine and [³H]-leucine incorporation, and [Ca²⁺]_i was measured with Fluo-3/AM staining. Systolic blood pressure (SBP), the ratio of media thickness to lumen diameter (MT/LD) of aorta, collagen content, and phospholipase C activity in aorta were measured in SHR. GCIP-27 (3—100 μg/l) significantly decreased proliferation activity, protein content, incorporation of [³H]-thymidine and [³H]-leucine, and [Ca²⁺]_i level in VSMC. SBP, MT/LD, collagen content, and phospholipase C activity in aorta of SHR were decreased significantly in GCIP-27 (7, 20, 60 μg/kg)-treated groups and losartan (6 mg/kg) group compared with vehicle group. In conclusion, GCIP-27 could inhibit vascular remodeling effectively in vitro and in vivo .
关键词：polypeptide drug;Gq protein;hypertension;vascular remodeling;vascular smooth muscle cell