当归芍药散活性部位DSS-A-N-30对大鼠离体子宫平滑肌收缩的影响

目的观察当归芍药散提取部位DSS-A-N-30对离体子宫平滑肌收缩的影响,并探讨其可能的作用机制。方法制备离体大鼠子宫肌条,观察DSS-A-N-30对子宫平滑肌自发性收缩,子宫收缩激动剂诱发的子宫平滑肌条剧烈收缩,KCl致子宫平滑肌条强直收缩及缩宫素(催产素)在无钙平衡盐溶液中致子宫平滑肌条持续收缩的影响。结果DSS-A-N-30(141.5,283和566mg.L-1)可以显著抑制子宫平滑肌的自发性收缩;对缩宫素(10IU.L-1)、前列腺素F2α(1mg.L-1)和乙酰胆碱(10μmol.L-1)引起的子宫平滑肌剧烈收缩有抑制作用;对KCl(60mmol.L-1)引起的子宫平滑肌强直收缩无明显作用;对缩宫素(10IU.L-1)在无钙平衡盐溶液中引起的子宫平滑肌条持续收缩有显著抑制作用。结论DSS-A-N-30可能主要通过抑制细胞内钙库释放而松弛子宫平滑肌,对子宫平滑肌收缩产生直接的抑制作用。提示DSS-A-N-30是当归芍药散的活性部位之一,有可能开发为新型痛经治疗药物。

Effect of DSS-A-N-30, an active ingredient of Danggui Shaoyao San, on contractility of rat uterine smooth muscle in vitro

AIM To observe the effect of DSS-A-N-30, the extracted ingredient of Danggui Shaoyao San, on rat uterine smooth muscle contractility in vitro, and to analyze its possible physiological mechanism. METHODS The isolated rat uterine strips were made and the effect of DSS-A-N-30 on spontaneous uterine contraction, and uterine contraction induced by agonists, K⁺-depolarization and oxytocin in Ca²⁺-free solution was observed. RESULTS DSS-A-N-30(141.5, 283, 566 mg·L^-1) inhibited the spontaneous uterine contraction, and the intense contraction induced by three agonists (10 IU·L^-1 oxytocin, 1 mg·L^-1prostaglandin F_2α, and 10 μmol·L^-1acetylcholine). The contraction induced by K⁺-depolarization was not inhibited by DSS-A-N-30, but sustained contractile induced by oxytocin in Ca²⁺-free solution could be inhibited by DSS-A-N-30. CONCLUSION DSS-A-N-30 directly inhibits the uterine contraction, mainly by inhibiting the release of Ca²⁺ from intracellular stores to relax uterine smooth muscle. These findings clearly show that DSS-A-N-30 is one of the active ingredients of Danggui Shaoyao San and has the potential to be developed into an effective drug for the treatment of primary dysmenorrhea.