Sha Sha, Xu Dandan, Wang Yanwei, Zhao Weifang, Li Xiaoni
College of Pharmacy, Shanxi Medical University, Taiyuan 030001, People's Republic of China.
Can J Physiol Pharmacol. 2016 Aug;94(8):900-6. doi: 10.1139/cjpp-2015-0615. Epub 2016 Apr 19.
Fargesin, a bioactive neolignan isolated from magnolia plants, is widely used in the treatment of managing rhinitis, inflammation, histamine, sinusitis, and headache. To provide more biological information about fargesin, we investigated the effects of fargesin on rat aortic rings and 2-kidney, 1-clip (2K1C) hypertensive rats. In vitro, fargesin caused concentration-dependent vasorelaxation in rat isolated aortic rings induced by KCl and norepinephrine. The effect was weakened by endothelium denudation and nitric oxide (NO) synthesis inhibition. In vivo, the evolution of systolic blood pressure (SBP) was followed by weekly measurements. Angiotensin II (Ang II) and endothelin (ET) levels, NO and nitric oxide synthase (NOS), and plasma and liver oxidative stress markers were determined at the end of the experimental period. After 5 weeks of fargesin treatment, we found that fargesin treatment reduced SBP, cardiac hypertrophy, and Ang II and ET levels of hypertensive rats. Increased NOS activity and NO level were observed in fargesin-treated rats. Normalisation of plasma MDA concentrations and improvement of the antioxidant defence system in plasma and liver accompanied the antihypertensive effect of fargesin. Taken together, these results provided substantial evidences that fargesin has antihypertensive effect in 2K1C hypertensive rats via inhibiting oxidative stress and promoting NO release.
法尔吉辛是从木兰属植物中分离出的一种具有生物活性的新木脂素,广泛用于治疗鼻炎、炎症、组胺、鼻窦炎和头痛。为了提供更多关于法尔吉辛的生物学信息,我们研究了法尔吉辛对大鼠主动脉环和二肾一夹(2K1C)高血压大鼠的影响。在体外,法尔吉辛可使氯化钾和去甲肾上腺素诱导的大鼠离体主动脉环产生浓度依赖性血管舒张。内皮剥脱和一氧化氮(NO)合成抑制会削弱这种作用。在体内,每周测量收缩压(SBP)的变化。在实验期结束时测定血管紧张素II(Ang II)和内皮素(ET)水平、NO和一氧化氮合酶(NOS)以及血浆和肝脏氧化应激标志物。法尔吉辛治疗5周后,我们发现法尔吉辛治疗可降低高血压大鼠的SBP、心脏肥大以及Ang II和ET水平。在法尔吉辛治疗的大鼠中观察到NOS活性和NO水平升高。法尔吉辛的降压作用伴随着血浆丙二醛浓度的正常化以及血浆和肝脏抗氧化防御系统的改善。综上所述,这些结果提供了充分的证据,表明法尔吉辛通过抑制氧化应激和促进NO释放,对2K1C高血压大鼠具有降压作用。