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Hypertension is a common type of cardiovascular disease that remains a major cause of death in the world. Vascular remodelling is an important complication of hypertension, and vascular smooth muscle cells (VSMCs) play a major role in vascular remodelling. Sauchinone is one of the active lignins which has been found to possess vascular protective effects. However, the functional role of sauchinone in hypertension has not been investigated. The aim of this study was to evaluate the role of sauchinone in the angiotensin II (Ang II)-induced vascular remodelling model in VSMCs. The results showed that treatment of sauchinone inhibited Ang II-induced VSMCs proliferation and migration in VSMCs. Sauchinone treatment suppressed the reactive oxygen species (ROS) production and NADPH oxidase (NOX) activity in Ang II-induced VSMCs. The inhibitory effects of Ang II on expressions of VSMCs phenotype markers including α-smooth muscle actin (α-SMA), calponin, osteopontin were mitigated by sauchinone treatment. Furthermore, sauchinone inhibited Ang II-induced over-activation of TGF-β1/Smad3 signalling pathway in VSMCs. Taken together, this study identified sauchinone as a potential agent for preventing vascular remodelling in hypertension.  相似文献   
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目的对三白草中具有保肝活性的成分三白草酮进行结构修饰,意图得到保肝活性更强的衍生物。方法以三白草酮为原料,在四氢呋喃-甲醇碱性体系中,用NaBH4将C-2’羰基还原为羟基得衍生物A;再以乙酸酐为乙酰化试剂,DMAP为催化剂,吡啶为溶剂将该羟基酰化得衍生物B。以四氯化碳小鼠急性肝损伤模型考察衍生物的保肝降酶活性。结果得到2个尚未见文献报导的三白草酮衍生物A和B,其结构经1 H NMR,13 C NMR和Q-TOF-MS确定。药理实验表明A的降酶效果比三白草酮要好,B与三白草酮相当。结论将三白草酮中羰基还原为羟基能增强降酶活性,该羟基酰化后降酶活性与三白草酮相当。  相似文献   
3.

BACKGROUND AND PURPOSE

Sauchinone, an antioxidant lignan, protects hepatocytes from iron-induced toxicity. This study investigated the protective effects of sauchinone against acetaminophen (APAP)-induced toxicity in the liver and the role of nuclear factor erythroid-2-related factor-2 (Nrf2) in this effect.

EXPERIMENTAL APPROACH

Blood biochemistry and histopathology were assessed in mice treated with APAP or APAP + sauchinone. The levels of mRNA and protein were measured using real-time PCR assays and immunoblottings.

KEY RESULTS

Sauchinone ameliorated liver injury caused by a high dose of APAP. This effect was prevented by a deficiency of Nrf2. Sauchinone treatment induced modifier subunit of glutamate-cysteine ligase, NAD(P)H:quinone oxidoreductase-1 (NQO1) and heat shock protein 32 in the liver, which was abolished by Nrf2 deficiency. In a hepatocyte model, sauchinone activated Nrf2, as evidenced by the increased nuclear accumulation of Nrf2, the induction of NQO1-antioxidant response element reporter gene, and glutamate-cysteine ligase and NQO1 protein induction, which contributed to the restoration of hepatic glutathione content. Consistently, treatment of sauchinone enhanced Nrf2 phosphorylation with a reciprocal decrease in its interaction with Kelch-like ECH-associated protein-1. Intriguingly, sauchinone activated protein kinase C-δ (PKCδ), which led to Nrf2 phosphorylation. In addition, it increased the inhibitory phosphorylation of glycogen synthase kinase-3β (GSK3β), derepressing Nrf2 activity, which was supported by the reversal of sauchinone''s activation of Nrf2 by an activated mutant of GSK3β. Moreover, phosphorylation of GSK3β by sauchinone depended on PKCδ activation.

CONCLUSION AND IMPLICATIONS

Our results demonstrate that sauchinone protects the liver from APAP-induced toxicity by activating Nrf2, and this effect is mediated by PKCδ activation, which induces inhibitory phosphorylation of GSK3β.  相似文献   
4.
Sauchinone is a lignan isolated from Saururus chinensis known to suppress nitric oxide (NO) activity. Previous studies demonstrate that NO plays a key role in methamphetamine-induced neurotoxicity. Thus, we hypothesized that sauchinone could have a suppressive effect on the neurotoxicity induced by methamphetamine. Repeated injections of methamphetamine cause degeneration of dopaminergic nerve terminals, whereas sauchinone treatment significantly prevented this degeneration. Sauchinone treatment also inhibited the methamphetamine-induced activation of glia cells and the production of NO via a blockade of inducible NO synthase protein expression. Our results suggest that sauchinone can prevent methamphetamine-induced neurotoxicity through the suppression of NO production.  相似文献   
5.
三白草中三白草酮提取工艺优选   总被引:2,自引:2,他引:0  
目的:优选三白草中三白草酮的提取工艺参数.方法:采用HPLC测定三白草酮提出量,并以此为指标,正交试验法对粉碎度、乙醇体积分数、料液比、提取时间、浸泡时间5个因素进行考察,优选最佳提取工艺.结果:最佳提取条件为药材过10目筛,95%乙醇提取2次,第1次加14倍量乙醇浸泡2h,提取2h;第2次加10倍量乙醇提取1h.在此条件下,三白草酮平均提取得率0.21%,提取转移率为96%.结论:优选的提取工艺稳定、合理,可用于三白草中三白草酮的提取.  相似文献   
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