Study on Dual Inhibitors of HIV-1 IN/CCR5 Caffeoyl Derivatives as Neuroprotective Agents

被引：2

作者：

Hao, Yameng ^{[1
]}

Wu, Bolin ^{[1
]}

Chen, Ying ^{[1
]}

Sun, Xuefeng ^{[1
]}

Sun, Yixing ^{[1
]}

Liu, Junyi ^{[1
,2
]}

Wang, Xiaowei ^{[1
]}

机构：

[1] Peking Univ, Sch Pharmaceut Sci, Dept Chem Biol, Beijing 100191, Peoples R China

[2] Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China

来源：

CHEMISTRYSELECT | 2018年 / 3卷 / 22期

基金：

中国国家自然科学基金;

关键词：

Anti-inflammatory property; Antioxidant property; Antiviral agents; HIV-associated neurocognitive disorders; Neurological agents; ACID PHENETHYL ESTER; FACTOR-KAPPA-B; OXIDATIVE STRESS; HYDROGEN-PEROXIDE; NEURODEGENERATIVE DISEASES; CELLS; INFLAMMATION; CYTOTOXICITY; INTEGRASE; MICROGLIA;

D O I：

10.1002/slct.201801313

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

(E)-3,4-diacetoxystyryl aralkyl ketone and sulfone derivatives, with the skeleton of CAPE, were reported as dual inhibitors of HIV-1 IN/CCR5 in our previous study. CAPE could show multifunctional neuroprotective properties through its antioxidant and anti-inflammatory effects. In this study, neuroprotective effects of these dual inhibitors were evaluated, and the biological results revealed that the reduction of conjugated double bonds in ketones did not significantly influence their antioxidant and anti-inflammatory effects. In addition, unsaturated ketones displayed better anti-inflammatory activities than corresponding sulfones. Sulfone compounds 11b and 11d had the best antioxidant effects among all these compounds. Overall, most of these HIV-1 dual inhibitors exhibited both antioxidant and anti-inflammatory activities, and thus had the potential to reduce the morbidity of HIV-associated neurocognitive disorders.

引用

页码：6170 / 6173

页数：4

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