School of Pharmaceutical Sciences and Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Chun Rong West Street No. 1168, Chenggong, Kunming 650500, PR China.
School of Pharmaceutical Sciences and Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Chun Rong West Street No. 1168, Chenggong, Kunming 650500, PR China.
Phytomedicine. 2018 Mar 15;42:66-74. doi: 10.1016/j.phymed.2018.03.021. Epub 2018 Mar 14.
Scutellarin is the major constituent responsible for the clinical benefits of Erigeron breviscapus (Vant.) Hand.-Mazz which finds a long history of ethnopharmacological use in Traditional Chinese Medicine. Scutellarin as a pure compound is now under investigation for its protections against various tissue injuries.
This study aims to examine the effects of scutellarin on oxidative stress-induced vascular endothelial dysfunction and endothelial cell damage, and then to evaluate the therapeutic efficacy of scutellarin in preventing atherosclerosis in rats.
Radical scavenging ability of scutellarin was determined in vitro. Impact of scutellarin on endothelium-dependent relaxation (EDR) of rabbit thoracic aortic rings upon 1, 1-diphenyl-2-picrylhydrazyl (DPPH) challenge was measured. Influences of scutellarin pre-treatment on the levels of reactive oxygen species (ROS), activities of antioxidant enzymes superoxide dismutase (SOD), glutathione peroxidase and catalase, and the expression of SOD1 and NADPH oxidase 4 (Nox4) in human umbilical vein endothelial cells (HUVECs) injured by HO were examined. Anti-atherosclerotic effect of scutellarin was evaluated in rats fed with high fat diet (HFD).
Scutellarin showed potent antioxidant activity in vitro. Pretreatment of scutellarin retained the EDR of rabbit thoracic aortic rings damaged by DPPH. In HO injured-HUVECs the deleterious alterations in ROS levels and antioxidant enzymes activity were reversed by scutellarin and the mRNA and protein expression of SOD1 and Nox4 were restored also. Oral administration of scutellarin dose-dependently ameliorated hyperlipidemia in HFD-fed rats and alleviated oxidative stress in rat serum, mimicking the effects of reference drug atorvastatin.
Scutellarin protects against oxidative stress-induced vascular endothelial dysfunction and endothelial cell damage in vitro and prevents atherosclerosis in vivo through antioxidation. The results rationalize further investigation into the clinical use of scutellarin in cardiovascular diseases.
灯盏乙素是灯盏细辛（Erigeron breviscapus（Vant.）Hand.-Mazz）发挥临床功效的主要成分，在中药中有悠久的药用历史。灯盏乙素作为一种纯化合物，目前正在研究其对各种组织损伤的保护作用。
本研究旨在探讨灯盏乙素对氧化应激诱导的血管内皮功能障碍和内皮细胞损伤的作用，然后评估灯盏乙素预防大鼠动脉粥样硬化的治疗效果。
体外测定灯盏乙素的自由基清除能力。测量灯盏乙素对 1,1-二苯基-2-苦基肼（DPPH）诱导的兔胸主动脉环内皮依赖性舒张（EDR）的影响。检测灯盏乙素预处理对 H2O2 损伤的人脐静脉内皮细胞（HUVECs）中活性氧（ROS）水平、抗氧化酶超氧化物歧化酶（SOD）、谷胱甘肽过氧化物酶和过氧化氢酶的活性以及 SOD1 和 NADPH 氧化酶 4（Nox4）表达的影响。
灯盏乙素在体外具有很强的抗氧化活性。灯盏乙素预处理保留了 DPPH 损伤的兔胸主动脉环的 EDR。在 H2O2 损伤的 HUVECs 中，ROS 水平和抗氧化酶活性的有害变化被灯盏乙素逆转，SOD1 和 Nox4 的 mRNA 和蛋白表达也得到恢复。灯盏乙素口服给药剂量依赖性地改善了高脂饮食喂养大鼠的高脂血症，并减轻了大鼠血清中的氧化应激，模拟了参考药物阿托伐他汀的作用。
灯盏乙素通过抗氧化作用，在体外保护血管内皮功能障碍和内皮细胞损伤，并在体内预防动脉粥样硬化。这些结果为进一步研究灯盏乙素在心血管疾病中的临床应用提供了依据。
