Home Journals Articles Updates About
CN
image
收藏切换
Synthesis, bioactivity evaluation of dibenzoyl methane halophenols and their interactions with CAV-1
收藏切换
PDF
Heng-jiang LIU1, Ning-ning CHENG1, Meng-ru ZHANG1, Hong-xia YUAN2, Yuan-lin ZHANG2, Xiu-e FENG1, *, Qing-shan LI1, 2, *
Acta Pharmaceutica Sinica | 2021, 56(12) : 3493 - 3502
Less
收藏切换
Acta Pharmaceutica Sinica | 2021, 56(12): 3493-3502
• Original Articles •
Synthesis, bioactivity evaluation of dibenzoyl methane halophenols and their interactions with CAV-1
Full
Heng-jiang LIU1, Ning-ning CHENG1, Meng-ru ZHANG1, Hong-xia YUAN2, Yuan-lin ZHANG2, Xiu-e FENG1, *, Qing-shan LI1, 2, *
Affiliations
  • 1. School of Pharmaceutical Science, Shanxi Medical University, Taiyuan 030001, China
  • 2. Shanxi Key Laboratory of Innovative Drug for the Treatment of Serious Diseases Basing on the Chronic Inflammation, Shanxi University of Chinese Medicine, Jinzhong 030619, China
Published: 2021-12-12 doi: 10.16438/j.0513-4870.2021-1051
Outline
收藏切换

Caveolin-1 (CAV-1) is related to inflammation, oxidative damage, and immunity. In order to obtain a series of dibenzoylmethane halophenols with strong anti-inflammatory and antioxidant effects targeting CAV-1, twenty-nine target compounds were therefore synthesized by Baker-Ventaraman rearrangement and demethylation reaction, starting from the substituted benzoyl chloride and o-hydroxyacetophenone, and their interactions with CAV-1 were investigated by BLI technique. Their in vitro anti-inflammatory and antioxidant properties were also evaluated. The results showed that compounds A6, A17, A18, and A29 not only specifically bind to CAV-1, but also present strong anti-inflammatory and antioxidant effects. These results suggest that this class of compounds can affect the signaling pathways related to inflammation and oxidative stress by directly acting on CAV-1. In particular, these compounds exhibit the most significantly inhibitory effects on IL-1β and COX-2 release. IL-1β plays a key regulatory role in the development of arthritis. Therefore, it is worth expecting for the application of such compounds in the prevention and treatment of arthritis.

dibenzoyl methane  /  synthesis  /  caveolin-1  /  anti-inflammation  /  anti-oxidation
Heng-jiang LIU, Ning-ning CHENG, Meng-ru ZHANG, Hong-xia YUAN, Yuan-lin ZHANG, Xiu-e FENG, Qing-shan LI. Synthesis, bioactivity evaluation of dibenzoyl methane halophenols and their interactions with CAV-1[J]. Acta Pharmaceutica Sinica, 2021 , 56 (12) : 3493 -3502 . DOI: 10.16438/j.0513-4870.2021-1051
Appendix
Less
Year 2021 volume 56 Issue 12
PDF
114
48
Cite this Article
BibTeX
Article Info
doi: 10.16438/j.0513-4870.2021-1051
  • Receive Date：2021-07-16
  • Online Date：2025-12-18
  • Published：2021-12-12
Article Data
Affiliations
History
  • Received：2021-07-16
  • Revised：2021-08-24
Funding
Affiliations
    1. School of Pharmaceutical Science, Shanxi Medical University, Taiyuan 030001, China
    2. Shanxi Key Laboratory of Innovative Drug for the Treatment of Serious Diseases Basing on the Chronic Inflammation, Shanxi University of Chinese Medicine, Jinzhong 030619, China
References
Share
https://castjournals.cast.org.cn/joweb/yxxb/EN/10.16438/j.0513-4870.2021-1051
Share to
QR

Scan QR to access full text

Cite this article
BibTeX
Citations
表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
关闭全屏
  • BibTeX
  • EndNote
  • RefWorks
  • TxT
Links
Articles
Latest Articles
Most Read
Collections
Updates
Events
News
Multimedia
About
About Us
Contact
No. 86 Xueyuan South Road, Haidian District, Beijing
100081
010-62199257
qkjq@cast.org.cn

Copyright © 2025 China Association for Science and Technology. All rights reserved. For all open access content, the relevant licensing terms apply.
Sponsored by the Office of the Leading Group for Cybersecurity and Informatization of CAST, and supported by Science and Technology Review Publishing House