补骨脂提取物通过内皮依赖性和非依赖性机制引起大鼠动脉舒张，涉及抑制 TRPC3 通道活性和前列腺素的产生。
Psoralea corylifolia extract induces vasodilation in rat arteries through both endothelium-dependent and -independent mechanisms involving inhibition of TRPC3 channel activity and elaboration of prostaglandin.
机构信息
a Laboratory of Physiology, College of Veterinary Medicine , Chungnam National University , Daejeon , Republic of Korea.
b Basic Herbal Research Group , Korea Institute of Oriental Medicine , Daejeon , South Korea.
出版信息
Pharm Biol. 2017 Dec;55(1):2136-2144. doi: 10.1080/13880209.2017.1383484.
CONTEXT
Fructus Psoralea, Psoralea corylifolia L. (Leguminosae), has been widely used in traditional medicines for the treatment of dermatitis, leukoderma, asthma and osteoporosis.
OBJECTIVES
In this study, we sought to study mechanisms underlying the vasoactive properties of Psoralea corylifolia extract (PCE) and its active ingredients.
MATERIALS AND METHODS
To study mechanisms underlying the vasoactive properties of PCE prepared by extracting dried seeds of Psoralea corylifolia with 70% ethanol, isometric tension recordings of rat aortic rings and the ionic currents through TRPC3 (transient receptor potential canonical 3) channels were measured with the cumulative concentration (10-600 μg/mL) of PCE or its constituents.
RESULTS
Cumulative treatment with PCE caused the relaxation of pre-contracted aortic rings in the presence and absence of endothelium with EC values of 61.27 ± 3.11 and 211.13 ± 18.74 μg/mL, respectively. Pretreatment with inhibitors of nitric oxide (NO) synthase, guanylate cyclase, or cyclooxygenase and pyrazole 3, a selective TRPC3 channel blocker, significantly decreased PCE-induced vasorelaxation (p < 0.01). The PCE constituents, bakuchiol, isobavachalcone, isopsoralen and psoralen, inhibited hTRPC3 currents (inhibited by 40.6 ± 2.7, 27.1 ± 7.9, 35.1 ± 4.8 and 47.4 ± 3.9%, respectively). Furthermore, these constituents significantly relaxed pre-contracted aortic rings (EC 128.9, 4.5, 32.1 and 114.9 μg/mL, respectively).
DISCUSSION AND CONCLUSIONS
Taken together, our data indicate that the vasodilatory actions of PCE are dependent on endothelial NO/cGMP and also involved in prostaglandin production. PCE and its active constituents, bakuchiol, isobavachalcone, isopsoralen and psoralen, caused dose-dependent inhibition of TRPC3 channels, indicating that those ingredients attenuate Phe-induced vasoconstriction.
背景
补骨脂（Psoralea corylifolia L.，豆科）作为一种传统药材，被广泛用于治疗皮炎、白癜风、哮喘和骨质疏松症。
目的
本研究旨在探讨补骨脂提取物（PCE）及其活性成分发挥血管活性作用的潜在机制。
材料和方法
采用含 70%乙醇的溶剂从补骨脂干种子中提取 PCE，通过累积浓度（10-600μg/ml）的 PCE 或其成分处理预先收缩的大鼠主动脉环，测量等长张力记录和瞬时受体电位经典型 3（TRPC3）通道的离子电流。
结果
累积处理 PCE 可引起存在和不存在内皮的预收缩主动脉环松弛，EC 值分别为 61.27±3.11μg/ml 和 211.13±18.74μg/ml。一氧化氮（NO）合酶、鸟苷酸环化酶和环氧化酶抑制剂以及选择性 TRPC3 通道阻滞剂吡唑 3 预处理可显著降低 PCE 诱导的血管舒张作用（p<0.01）。PCE 的成分，补骨脂素、异补骨脂查尔酮、异补骨脂素和补骨脂素，抑制 hTRPC3 电流（分别抑制 40.6±2.7%、27.1±7.9%、35.1±4.8%和 47.4±3.9%）。此外，这些成分还可显著松弛预先收缩的主动脉环（EC 128.9、4.5、32.1 和 114.9μg/ml）。
讨论与结论
综上所述，我们的数据表明，PCE 的血管舒张作用依赖于内皮 NO/cGMP，也涉及前列腺素的产生。PCE 及其活性成分补骨脂素、异补骨脂查尔酮、异补骨脂素和补骨脂素可引起 TRPC3 通道的剂量依赖性抑制，表明这些成分可减轻 Phe 诱导的血管收缩。
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