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首页> 外文期刊>Acta Pharmacologica Sinica >Phytoestrogen genistein decreases contractile response of aortic artery in vitro and arterial blood pressure in vivo
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Phytoestrogen genistein decreases contractile response of aortic artery in vitro and arterial blood pressure in vivo

机译：植物雌激素染料木黄酮可降低体外主动脉收缩反应和体内动脉血压

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AIM: To determine the mechanisms of effects of phytoestrogen genistein on the contracted rabbit aortic arteries in vitro, and observe the effect of genistein and 17-β estradiol on mean arterial pressure (MAP) in ovariectomized (OVX) rats. METHODS: (1) Strips of rabbit aortic smooth muscle were suspended in organ baths containing Kreb's solution, and then isometric tension was measured. (2) Female mature Wistar rats underwent a bilateral ovariectomy (OVX). Sham-operated rats (SHAM) were used as controls. After administration of genistein (0.4 mg·kg~(-1)·d~(-1), sc), 17-β estradiol (1 mg·kg~(-1)·d~(-1), sc) or their vehicle sesame oil for 21 d, MAP was measured. RESULTS: (1) Similar to 17-β estradiol, genistein could dose-dependently relax 40 mmol/L KCl-precontracted arterial strips. Incubation with N~ω-L-nitro-arginine (L-NNA), methylene blue (MB), indomethacin, propranolol or endothelium removal did not affect relaxation induced by genistein. In calcium-free solution containing 0.01mmol/L egtazic acid (EGTA), genistein inhibited not only the first phase contraction induced by noradrenaline (NA), but also the second contraction induced by CaCl_2. In addition, genistein could reduce the contractile responses of NA, KCl and CaCl_2, and shift their cumulative concentration-response curves rightward. (2) MAP in OVX rats was significantly higher compared with that of SHAM rats. However, after chronically treatment with genistein or 17-β estradiol for 21 d the baseline MAP in OVX rats was reduced significantly. CONCLUSIONS: (1) The vasodilator effect of genistein in vitro is endothelium independent and not related to the nitric oxide, its mechanisms being probably due to inhibition of Ca~(2+) influx through calcium channels in a noncompetitive manner and Ca~(2+) release from intracellular store induced by NA. (2) Administration of genistein or 17-β estradiol can chronically decrease MAP in OVX rats.
机译：目的：确定植物雌激素染料木黄酮对体外兔主动脉收缩的作用机制，并观察染料木黄酮和17-β雌二醇对去卵巢（OVX）大鼠平均动脉压（MAP）的影响。方法：（1）将家兔主动脉平滑肌条悬于含有克雷布氏溶液的器官浴中，然后测定等轴测张力。 （2）雌性成年Wistar大鼠进行了双侧卵巢切除术（OVX）。假手术大鼠（SHAM）用作对照。给予染料木黄酮（0.4 mg·kg〜（-1）·d〜（-1），sc），17-β雌二醇（1 mg·kg〜（-1）·d〜（-1），sc）或他们的车用香油21 d，测得MAP。结果：（1）类似于17-β雌二醇，金雀异黄素可以剂量依赖性地松弛40 mmol / L KCl预收缩的动脉条。与N〜ω-L-硝基精氨酸（L-NNA），亚甲基蓝（MB），消炎痛，普萘洛尔或内皮细胞一起孵育不会影响染料木黄酮引起的松弛。在含有0.01mmol / L的依他唑酸（EGTA）的无钙溶液中，染料木黄酮不仅抑制去甲肾上腺素（NA）诱导的第一相收缩，而且抑制CaCl_2诱导的第二相收缩。此外，金雀异黄素可以减少NA，KCl和CaCl_2的收缩反应，并向右移动它们的累积浓度-反应曲线。 （2）OVX大鼠的MAP明显高于SHAM大鼠。但是，在用染料木黄酮或17-β雌二醇进行长期治疗21天后，OVX大鼠的基线MAP明显降低。结论：（1）金雀异黄素在体外的血管舒张作用与内皮无关，与一氧化氮无关，其作用机制可能是由于通过非竞争性方式抑制钙〜（2+）通过钙通道的流入和钙〜（2）。 +）从NA诱导的细胞内储存中释放。 （2）给予染料木黄酮或17-β雌二醇可长期降低OVX大鼠的MAP。

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