<br>4-羟基-3'-三氟甲氧基取代的白藜芦醇衍生物作为抗衰老剂的发现,Molecules

当前位置： X-MOL 学术 › Molecules › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

4-羟基-3'-三氟甲氧基取代的白藜芦醇衍生物作为抗衰老剂的发现
Molecules ( IF 4.2 ) Pub Date : 2023-12-22 , DOI: 10.3390/molecules29010086
Yinhu Liang ₁ , Xi Chen ₁ , Zhifeng Teng ₁ , Xuekun Wang ₁ , Jie Yang _{1,

2} , Guoyun Liu _{1,

2}

Affiliation

随着人口老龄化的加剧，与衰老相关的疾病越来越受到人们的关注，衰老机制和抗衰老药物的研究变得日益紧迫。白藜芦醇是一种潜在的抗衰老剂候选物，但其低生物利用度限制了其在体内的应用。在这项工作中，4-羟基-3'-三氟甲氧基取代的白藜芦醇衍生物（4-6）由于其优异的细胞积累作用，可以抑制炎症细胞模型中NO的产生，抑制氧化细胞毒性，并减少ROS积累和氧化应激细胞模型中的凋亡细胞群。在D-半乳糖（D-gal）刺激的衰老小鼠中，4-6可以逆转肝脏和肾脏损伤；保护血清、大脑和肝脏免受氧化应激；并增强人体脾脏的免疫力。进一步的D-gal诱导脑衰老研究表明，4-6可以改善海马的病理变化和胆碱能系统的功能障碍。此外，通过蛋白质印迹法测量的脑组织匀浆中与衰老、氧化应激和细胞凋亡相关的蛋白质表达也表明，4-6可以通过防止氧化应激和减少细胞凋亡来改善脑衰老。这项工作表明，间三氟甲氧基取代的4-6位值得进一步研究作为有效的抗衰老候选药物。

"点击查看英文标题和摘要"

Discovery of a 4-Hydroxy-3′-Trifluoromethoxy-Substituted Resveratrol Derivative as an Anti-Aging Agent

With the intensification of population aging, aging-related diseases are attracting more and more attention, thus, the study of aging mechanisms and anti-aging drugs is becoming increasingly urgent. Resveratrol is a potential candidate as an anti-aging agent, but its low bioavailability limits its application in vivo. In this work, a 4-hydroxy-3′-trifluoromethoxy-substituted resveratrol derivative (4–6), owing to its superior cell accumulation, could inhibit NO production in an inflammatory cell model, inhibit oxidative cytotoxicity, and reduce ROS accumulation and the population of apoptotic cells in an oxidative stress cell model. In D-galactose (D-gal)-stimulated aging mice, 4–6 could reverse liver and kidney damage; protect the serum, brain, and liver against oxidative stress; and increase the body’s immunity in the spleen. Further D-gal-induced brain aging studies showed that 4–6 could improve the pathological changes in the hippocampus and the dysfunction of the cholinergic system. Moreover, protein expression related to aging, oxidative stress, and apoptosis in the brain tissue homogenate measured via Western blotting also showed that 4–6 could ameliorate brain aging by protecting against oxidative stress and reducing apoptosis. This work revealed that meta-trifluoromethoxy substituted 4–6 deserved to be further investigated as an effective anti-aging candidate drug.

更新日期：2023-12-22

点击分享查看原文

点击收藏

公开下载

阅读更多本刊新发论文本刊介绍/投稿指南