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黄姜素可诱导大鼠胸主动脉产生非内皮依赖性舒张。

Xanthorrhizol induces endothelium-independent relaxation of rat thoracic aorta.

作者信息

Campos M G, Oropeza M V, Villanueva T, Aguilar M I, Delgado G, Ponce H A

机构信息

UIM Farmacologica, Hospital de Especialdades, Centro Medico Nacional Siglo XXI; IMSS, Col. Narvarte, Mexico.

出版信息

Life Sci. 2000 Jun 8;67(3):327-33. doi: 10.1016/s0024-3205(00)00619-6.

Abstract

Xanthorrhizol, a bisabolene isolated from the medicinal plant Iostephane heterophylla, was assayed on rat thoracic aorta rings to elucidate its effect and likely mechanism of action, by measuring changes of isometric tension. Xanthorrhizol (1, 3, 10, 30 and 100 microg/mL) significantly inhibited precontractions induced by KCI-; (60mM), noradrenaline (10(-6) M) or CaCl2 (1.0 mM). Increasing concentrations of external calcium antagonized the inhibitory effect on KCl-induced contractions. The vasorelaxing effect of xanthorrhizol was not affected by indomethacin (10 microM) or L-NAME (100 microM) in intact rat thoracic aorta rings precontracted by noradrenaline, which suggested that the effect was not mediated through either endothelium-derived prostacyclin (PGI2) or nitric oxide release from endothelial cells. Endothelium removal did not affect the relaxation induced by xanthorrhizol on rat thoracic aorta rings, discarding the participation of any substance released by the endothelium. Xanthorrhizol inhibitory effect was greater on KCI- and CaCl2-induced contractions than on those induced by noradrenaline. Xanthorrhizol inhibitory effect in rat thoracic aorta is likely explained for interference with calcium availability by inhibiting calcium influx through both voltage- and receptor-operated channels.

摘要

从药用植物异叶败酱中分离得到的倍半萜烯类化合物黄根醇,通过测量等长张力的变化,在大鼠胸主动脉环上进行了测定,以阐明其作用效果及可能的作用机制。黄根醇(1、3、10、30和100微克/毫升)显著抑制由氯化钾(60毫摩尔)、去甲肾上腺素(10⁻⁶摩尔)或氯化钙(1.0毫摩尔)诱导的预收缩。增加细胞外钙的浓度可拮抗对氯化钾诱导收缩的抑制作用。在由去甲肾上腺素预收缩的完整大鼠胸主动脉环中,吲哚美辛(10微摩尔)或L-硝基精氨酸甲酯(100微摩尔)不影响黄根醇的血管舒张作用,这表明该作用不是通过内皮衍生的前列环素(PGI2)或内皮细胞释放的一氧化氮介导的。去除内皮不影响黄根醇对大鼠胸主动脉环的舒张作用,排除了内皮释放的任何物质的参与。黄根醇对氯化钾和氯化钙诱导的收缩的抑制作用比对去甲肾上腺素诱导的收缩的抑制作用更强。黄根醇在大鼠胸主动脉中的抑制作用可能是通过抑制电压门控通道和受体操纵通道的钙内流来干扰钙的可用性来解释的。

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