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由 Scutia buxifolia Reiss(瑞香科)树皮的正丁醇部分引起的内皮依赖性和非内皮依赖性血管舒张。

Endothelium-dependent and independent vasorelaxation induced by an n-butanolic fraction of bark of Scutia buxifolia Reiss (Rhamanaceae).

机构信息

Department of Pharmacology, UFPR, Brazil.

出版信息

J Ethnopharmacol. 2012 Jun 14;141(3):997-1004. doi: 10.1016/j.jep.2012.03.045.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Scutia buxifolia has been widely used in Brazilian folk medicine as an anti-hypertensive agent. We evaluated the vascular effects and mechanism involved in the relaxation of aorta induced by an n-butanolic fraction (BuOH) from Scutia buxifolia.

MATERIALS AND METHODS

Rat aortic rings precontracted by phenylephrine (1 μM) were exposed to cumulative concentrations (3–3000 μg/ml) of crude extracts or fractions obtained from bark or leaves of Scutia buxifolia. Classical receptor antagonists, channel and enzymatic inhibitors were used to check the mechanisms involved.

RESULTS

The crude extracts of both leaves and bark of Scutia buxifolia, as well as several fractions, were able to induce partial or total relaxation of rat aortic rings. The BuOH fraction of bark of Scutia buxifolia was the most potent in endothelium-intact (E+) preparations, and also induced a partial, but very significant relaxation in endothelium-denuded (E−) vessels. The non-selective nitric oxide synthase inhibitor L-NAME, as well as the soluble guanylate cyclase inhibitor ODQ, vanished the relaxation in E+. In E− preparations, K+ channel blockers, such as tetraethylammonium, glibenclamide, 4-aminopyridine, and the large-conductance calcium-activated K+ channel blocker iberiotoxin, were able to significantly reduce the maximum relaxation elicited by BuOH fraction.

CONCLUSION

Our results demonstrated that BuOH fraction obtained from barks of Scutia buxifolia induced both endothelium-dependent and -independent relaxation in rat aortic rings. The endothelium-dependent relaxation is fully dependent on NO/cGMP system, while direct activation of K+ channels may explain, at least in part, the endothelium-independent relaxation induced by BuOH fraction of Scutia buxifolia.

摘要

植物药理学相关性

Scutia buxifolia 在巴西民间医学中被广泛用作抗高血压药物。我们评估了 Scutia buxifolia 的正丁醇部分(BuOH)引起的血管舒张作用及其涉及的机制。

材料和方法

用苯肾上腺素(1 μM)预收缩的大鼠主动脉环暴露于粗提取物或树皮或叶子获得的馏分的累积浓度(3-3000 μg/ml)。使用经典受体拮抗剂、通道和酶抑制剂来检查所涉及的机制。

结果

Scutia buxifolia 的树皮和叶子的粗提取物以及几种馏分均能引起大鼠主动脉环的部分或完全舒张。Scutia buxifolia 树皮的 BuOH 馏分在完整内皮(E+)制剂中最有效,并且在去内皮(E−)血管中也引起部分但非常显著的舒张。非选择性一氧化氮合酶抑制剂 L-NAME 以及可溶性鸟苷酸环化酶抑制剂 ODQ 消除了 E+中的松弛作用。在 E−制剂中,K+通道阻滞剂,如四乙铵、格列本脲、4-氨基吡啶和大电导钙激活的 K+通道阻滞剂 Iberiotoxin,能够显著降低 BuOH 馏分引起的最大舒张。

结论

我们的结果表明,从 Scutia buxifolia 树皮中获得的 BuOH 馏分在大鼠主动脉环中诱导了内皮依赖性和非依赖性舒张。内皮依赖性舒张完全依赖于 NO/cGMP 系统,而 BuOH 馏分诱导的非内皮依赖性舒张至少部分可以通过直接激活 K+通道来解释。

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