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路易波士茶(线叶金雀花)及其黄酮类化合物 Chrysoeriol 的选择性支气管扩张作用。

Selective bronchodilatory effect of Rooibos tea (Aspalathus linearis) and its flavonoid, chrysoeriol.

作者信息

Khan Arif-ullah, Gilani Anwarul Hassan

机构信息

Dept. of Biological and Biomedical Sciences, The Aga Khan University Medical College, Karachi, 74800, Pakistan.

出版信息

Eur J Nutr. 2006 Dec;45(8):463-9. doi: 10.1007/s00394-006-0620-0. Epub 2006 Nov 1.

Abstract

BACKGROUND

Rooibos tea (Aspalathus linearis) is commonly used for hyperactive gastrointestinal, respiratory and cardiovascular disorders.

AIM OF STUDY

The aqueous extract of Rooibos tea (RT) was studied for the possible bronchodilator, antispasmodic and blood pressure lowering activities in an attempt to rationalize some of its medicinal uses.

METHODS

Isolated tissue preparations, such as rabbit jejunum, aorta and guinea-pig trachea and atria were set up in appropriate physiological salt solutions and aerated with carbogen. For in vivo studies rats were anesthetized with pentothal sodium and blood pressure was measured through carotid artery cannulation.

RESULTS

In jejunum, RT caused a concentration-dependent relaxation of low K(+) (25 mM)-induced contractions, with mild effect on the contractions induced by high K(+) (80 mM). In presence of glibenclamide, the relaxation of low K(+)-induced contractions was prevented. Similarly, cromakalim caused glibenclamide-sensitive inhibition of low K(+), but not of high K(+), while verapamil did not differentiate in its inhibitory effect on contractions produced by the two concentrations of K(+). Like in jejunum, RT caused glibenclamide-sensitive relaxation of low K(+)-induced contractions in trachea and aorta, but with a 20 times higher potency in trachea. In atria, RT was least potent with weak inhibitory effect on atrial force and rate of contractions. RT caused a dose-dependent fall in arterial blood pressure in rats under anesthesia. Among the tested pure compounds of Rooibos, chrysoeriol showed selective bronchodilator effect. Chrysoeriol (luteolin 3'-methyl ether) is a bioactive flavonoid known for antioxidant, antiinflammatory, antitumor, antimicrobial, antiviral, and free radical scavenging activities.

CONCLUSION

These results indicate that the bronchodilator, antispasmodic and blood pressure lowering effects of Rooibos tea are mediated predominantly through K(ATP) channel activation with the selective bronchodilatory effect. This study provides a sound mechanistic basis for the wide medicinal use of Rooibos tea, with the therapeutic potential to be developed for congestive respiratory ailments.

摘要

背景

路易波士茶(Aspalathus linearis)常用于治疗胃肠道功能亢进、呼吸系统疾病和心血管疾病。

研究目的

研究路易波士茶水提取物(RT)的支气管扩张、解痉和降压活性,以阐明其部分药用价值的合理性。

方法

将分离的组织标本,如兔空肠、主动脉、豚鼠气管和心房,置于合适的生理盐溶液中,并用混合气体通气。在体内研究中,用戊硫代巴比妥钠麻醉大鼠,通过颈动脉插管测量血压。

结果

在空肠中,RT引起低K⁺(25 mM)诱导收缩的浓度依赖性舒张,对高K⁺(80 mM)诱导的收缩影响较小。在格列本脲存在的情况下,低K⁺诱导收缩的舒张被阻止。同样,克罗卡林引起格列本脲敏感的低K⁺抑制,但对高K⁺无抑制作用,而维拉帕米对两种浓度K⁺诱导的收缩的抑制作用无差异。与空肠一样,RT引起气管和主动脉中低K⁺诱导收缩的格列本脲敏感舒张,但在气管中的效力高20倍。在心房中,RT效力最低,对心房力和收缩速率的抑制作用较弱。RT使麻醉大鼠的动脉血压呈剂量依赖性下降。在测试的路易波士纯化合物中, Chrysoeriol显示出选择性支气管扩张作用。 Chrysoeriol(木犀草素3'-甲醚)是一种具有抗氧化、抗炎、抗肿瘤、抗菌、抗病毒和自由基清除活性的生物活性黄酮类化合物。

结论

这些结果表明,路易波士茶的支气管扩张、解痉和降压作用主要通过K⁺ATP通道激活介导,并具有选择性支气管扩张作用。本研究为路易波士茶的广泛药用提供了合理的机制基础,具有开发用于充血性呼吸系统疾病治疗潜力。

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