School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, China; Institute of Innovative Medicine Ingredients of Southwest Specialty Medicinal Materials, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, China; State Key Laboratory of Characteristic Chinese Medicine Resources in Southwest China, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, China.
School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, China.
J Ethnopharmacol. 2021 Apr 6;269:113713. doi: 10.1016/j.jep.2020.113713. Epub 2020 Dec 25.
ETHNOPHARMACOLOGICAL RELEVANCE: Dysmenorrhea is one of the most common gynecological problems among menstruating females. Blood-activating and stasis-resolving herbs (BASRHs) have been employed to be the first choice for treating dysmenorrhea in China. Especially, the essential oils of some BASRHs have been confirmed to play important roles in the treatment of dysmenorrhea, but the constituents and uterine smooth muscle relaxant activity of some commonly used BASRH essential oils have not been fully assessed, and whether there are differences in the constituents and anti-dysmenorrhea effect among BASRH essential oils has not been evaluated. AIM OF THE STUDY: This study aims to systematically investigate the chemical constituents of 10 BASRH essential oils and assess their uterine smooth muscle relaxant activity and the preliminary mechanism of the most effective essential oil. MATERIALS AND METHODS: The chemical constituents of 10 BASRH essential oils were analyzed by Gas Chromatography-Mass Spectrometer. A rat model of dysmenorrhea in vitro was established to investigate the uterine smooth muscle relaxant activity of 10 kinds of essential oils. Rat isolated uterus strips were given different dose of 10 kinds of essential oils (0.04, 0.08, 0.16 mg/mL). The contractile responses were recorded with Power Lab recording system, and contractile tension, contractile frequency, and contractile activity were evaluated. The preliminary mechanism of the essential oil of the rhizomes of Curcuma phaeocaulis Valeton (CPEO) was assessed using a rat model of dysmenorrhea in vivo and in vitro, and rats were given the CPEO (15, 30, and 60 mg/kg) by gavage. The level of Ca in uterine tissue of rats was determined by methyl thyme phenol blue colorimetric and Bradford methods. The effects of CPEO on extracellular Ca influx and intracellular Ca release were evaluated using the isolated uterus. RESULTS: The results of Gas Chromatography-Mass Spectrometer analysis showed that more than 81 components (content: 1% max appearance) were identified. The main components of the 10 BASRH essential oils were found to be monoterpenoids, sesquiterpenoids, diterpenoids, aromatics, aliphatics, and phthalides. The study of in vitro smooth muscle relaxant activity demonstrated that all the essential oils except the essential oil of the roots of Cyathula officinalis K.C.Kuan markedly decrease the contractile activity, tension, and frequency (P < 0.05 or P < 0.01). Among these oils, CPEO has the most pronounced effect. Further in vivo studies indicated that CPEO can significantly decrease the level of Ca in uterine tissue when compared with the model group (P < 0.05 or P < 0.01). In vitro studies indicated that CPEO can inhibit the extracellular Ca influx and intracellular Ca release in favor of uterine relaxation. CONCLUSIONS: BASRH essential oils play an important role in inhibiting uterine smooth muscle contractions, and sesquiterpenoids and phthalides in BASRH essential oils are important active compounds for relaxing uterine smooth muscle. CPEO is a favorable candidate for developing anti-dysmenorrhea drugs.
民族药理学相关性：痛经是经期女性最常见的妇科问题之一。在中国，活血化瘀草药（BASRHs）一直被用作治疗痛经的首选药物。特别是，一些 BASRH 的精油已被证实对治疗痛经具有重要作用，但一些常用 BASRH 精油的成分和子宫平滑肌松弛活性尚未得到充分评估，而且不同 BASRH 精油之间的成分和抗痛经效果是否存在差异也尚未得到评估。
研究目的：本研究旨在系统研究 10 种 BASRH 精油的化学成分，并评估其子宫平滑肌松弛活性和最有效的精油的初步机制。
材料和方法：采用气相色谱-质谱联用仪分析 10 种 BASRH 精油的化学成分。建立大鼠痛经体外模型，研究 10 种精油的子宫平滑肌松弛活性。给予不同剂量的 10 种精油（0.04、0.08、0.16mg/mL）至大鼠离体子宫条。用 Power Lab 记录系统记录收缩反应，并评估收缩张力、收缩频率和收缩活性。采用大鼠痛经体内和体外模型评估姜黄根茎精油（CPEO）的初步机制，并通过灌胃给予 CPEO（15、30 和 60mg/kg）。采用甲基百里酚蓝比色法和 Bradford 法测定大鼠子宫组织中 Ca 的水平。通过分离子宫评估 CPEO 对细胞外 Ca 内流和细胞内 Ca 释放的影响。
结果：气相色谱-质谱联用仪分析结果表明，鉴定出超过 81 种成分（含量：1%max 出现）。10 种 BASRH 精油的主要成分被发现为单萜、倍半萜、二萜、芳烃、脂肪族和苯酞。体外平滑肌松弛活性研究表明，除了川牛膝根精油外，所有精油均显著降低收缩活性、张力和频率（P<0.05 或 P<0.01）。在这些油中，CPEO 的效果最为显著。进一步的体内研究表明，与模型组相比，CPEO 可显著降低子宫组织中的 Ca 水平（P<0.05 或 P<0.01）。体外研究表明，CPEO 可抑制细胞外 Ca 内流和细胞内 Ca 释放，有利于子宫松弛。
结论：BASRH 精油在抑制子宫平滑肌收缩方面发挥着重要作用，BASRH 精油中的倍半萜和苯酞是松弛子宫平滑肌的重要活性化合物。CPEO 是开发抗痛经药物的理想候选药物。
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