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咖啡酸 阿魏酸和CA |
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王峰 王京媛 李菲 刘敏 杨连春 程言亮 吕敏 季小慎
摘 要 目的：探讨咖啡酸、阿魏酸和CA-1201对ET-1生物效应的拮抗作用。方法：用不同剂量的咖啡酸、阿魏酸和CA-1201拮抗ET-1引起小鼠急性死亡、缩血管效应、升压效应及致平滑肌细胞增殖效应。 结果：(1)咖啡酸、阿魏酸和CA-1201在0.1～100 mg/kg剂量范围内，对ET-1致小鼠死亡有明显的对抗作用，该作用存在剂量依赖性；(2)三种药物对ET-1缩血管效应有明显的拮抗作用，咖啡酸和CA-1201拮抗效能相近，而阿魏酸的拮抗效能强于咖啡酸和CA-1201；(3)三种药物均能拮抗ET-1的升血压作用，与对照组相比，该作用有显著差异；(4)三种药物对ET-1致家兔血管平滑肌细胞增殖有明显的抑制作用，该作用具剂量依赖性。结论：咖啡酸、阿魏酸和CA-1201能有效地拮抗ET-1的生物效应，是一类新的ET拮抗剂。
主题词 桂皮；内皮缩血管肽类；咖啡酸类
Antagonism effects of caffeic acid, ferulic acids and CA-1201 on
ET-1 biological responses
WANG Feng, WANG Jing-Yuan, LI Fei, LIU Min, YANG Lian-Chun,
CHENG Yan-Liang, LU Min, JI Xiao-Shen
General Hospital of Air Force, PLA, Beijing (100036)
Abstract AIM:To evaluate the antagonistic effects of caffeic acid, ferulic acid and CA-1201 on endothelin-1 biological responses.METHODS：The acute death of mouse, vasoconstriction of isolated aortic ring, systolic blood pressure evaluation and vascular smooth muscle cells (VSMC) proliferation induced by ET-1 were antagonitized by caffeic acid, ferulic acid and CA-1201.RESULTS：(1)Caffeic acid, ferulic acid and CA-1201 of 0.1～10 mg/kg could protect mouse from acute death induced by ET-1 in a dose dependent manner;(2)These drugs against vasoconstriction induced by ET-1, in which the antagonism efficacy of caffeic acid and CA-1201 was similar and the efficacy of ferulic acid was better than both caffeic acid and CA-1201;(3)These drugs could blunted significantly blood pressure elevation by ET-1 comparing with control groups respectively;(4)These drugs could inhibit the VSMC proliferation induced by ET-1 in concentration-dependent manner.CONCLUSION：Caffeic acid, ferulic acid and CA-1201 can antagonize ET-1 biological effects, which may be a new kind of ET-1 antagonists.
MeSH Cinnamon; Endothelins; Caffeic acids
内皮素(endothelin, ET)是由21个氨基酸组成的多肽，其具有强大的缩血管作用和致平滑肌细胞有丝分裂效应，现已明确ET参与多种心脑血管疾病的病理生理过程。近年来，国内外对其拮抗剂的研究较为深入和[1] [2] 下一页
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