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体内载白藜芦醇脂质体的抗惊厥活性。

Anticonvulsant activity of resveratrol-loaded liposomes in vivo.

机构信息

Yeditepe University, Medical School, Department of Physiology, Ataşehir, İstanbul, Turkey.

Yeditepe University, Experimental Research Center, Ataşehir, İstanbul, Turkey.

出版信息

Neuroscience. 2017 Aug 15;357:12-19. doi: 10.1016/j.neuroscience.2017.05.026. Epub 2017 Jun 1.

Abstract

Resveratrol (3,5,4'-stilbenetriol), a natural polyphenol produced by various plants, has attracted attention over the past decade because of its multiple beneficial properties, including anti-inflammatory, anti-oxidant and chemopreventive, yet, there is limited information about its antiepileptic effects. Moreover, its poor solubility in water and low bioavailability are the challenging issues. In the present study, we aimed to investigate effects of free resveratrol and resveratrol delivered in amphipathic liposomal delivery system, which has a high blood-brain barrier crossing potential, on penicillin-induced epileptic seizure model. For this purpose, adult male Sprague-Dawley rats were divided into four groups as saline (Control), liposome (LIP), free resveratrol (RES) and resveratrol+liposome (RES+LIP). Penicillin-induced epileptic activity was recorded for 120 min by electrocorticography. Glutathione S-transferase (GST), Glutathione (GSH), Superoxide dismutase (SOD) and Malondialdehyde (MDA) assays were performed in brain tissues collected. Our results showed that RES+LIP was the most effective anticonvulsant treatment on penicillin-induced epileptic seizures when compared to control, as RES+LIP immediately decreased the number of spikes per minute. GST and SOD activity, as well as the GSH levels, were significantly increased in the RES+LIP group as compared with the control group. Also, the MDA levels were significantly higher in the RES+LIP compared to RES and control groups. In conclusion, RES+LIP treatment was more effective on the decrease in spike frequency and spike amplitudes than other treatments. Our results suggest that the RES+LIP is more effective than RES on penicillin-induced epileptiform activity.

摘要

白藜芦醇(3,5,4'-三羟基二苯乙烯)是一种天然多酚类化合物,存在于多种植物中,由于其具有多种有益特性,包括抗炎、抗氧化和化学预防作用,因此在过去十年中引起了人们的关注。然而,关于其抗癫痫作用的信息有限。此外,其在水中的溶解度低和生物利用度低是具有挑战性的问题。在本研究中,我们旨在研究游离白藜芦醇和具有高血脑屏障穿透能力的两亲脂质体传递系统传递的白藜芦醇对青霉素诱导的癫痫发作模型的影响。为此,成年雄性 Sprague-Dawley 大鼠分为盐水(对照)、脂质体(LIP)、游离白藜芦醇(RES)和白藜芦醇+脂质体(RES+LIP)四组。通过皮层脑电图记录青霉素诱导的癫痫活动 120 分钟。在采集的脑组织中进行谷胱甘肽 S-转移酶(GST)、谷胱甘肽(GSH)、超氧化物歧化酶(SOD)和丙二醛(MDA)测定。结果表明,与对照组相比,RES+LIP 是青霉素诱导的癫痫发作的最有效抗惊厥治疗方法,因为 RES+LIP 立即减少了每分钟的尖峰数。与对照组相比,RES+LIP 组 GST 和 SOD 活性以及 GSH 水平显着增加。此外,与 RES 和对照组相比,RES+LIP 组 MDA 水平显着升高。总之,与其他治疗方法相比,RES+LIP 治疗在降低尖峰频率和尖峰幅度方面更有效。我们的结果表明,与 RES 相比,RES+LIP 对青霉素诱导的癫痫样活动更有效。

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