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Glycosylation derivatization, bioactivity evaluation of benzophenone polyphenols and their interaction with protein disulfide isomerase A6
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Qiang LI1, Ning-ning CHENG1, Xiu-e FENG1, 2, *, Qing-shan LI1, 2, 3, *
Acta Pharmaceutica Sinica | 2024, 59(6) : 1706 - 1719
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Acta Pharmaceutica Sinica | 2024, 59(6): 1706-1719
• Original Articles •
Glycosylation derivatization, bioactivity evaluation of benzophenone polyphenols and their interaction with protein disulfide isomerase A6
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Qiang LI1, Ning-ning CHENG1, Xiu-e FENG1, 2, *, Qing-shan LI1, 2, 3, *
Affiliations
  • 1. School of Pharmaceutical Science, Shanxi Medical University, Taiyuan 030001, China
  • 2. Medicinal Basic Research Innovation Center of Chronic Kidney Disease, Ministry of Education, Shanxi Medical University, Taiyuan 030001, China
  • 3. 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: 2024-06-12 doi: 10.16438/j.0513-4870.2023-1384
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Protein disulfide isomerase A6 (PDIA6) is closely related to inflammation and endoplasmic reticulum stress. To obtain the glycosyl derivatives of benzophenone polyphenols targeting PDIA6 with strong anti-inflammatory effects, twenty-five target glycosyl derivatives were synthesized by Friedel-Crafts acylation and deacetylation reaction, starting from the substituted benzophenone and α-bromoacetyl saccharide, and their interactions with PDIA6 were quantitatively investigated by bio-layer interferometry (BLI) technique. Their in vitro anti-inflammatory properties were also evaluated. The results showed that target compounds 4b, 10b, 17b, 18b, and 25b not only exhibit high affinity with PDIA6, but also present strong anti-inflammatory abilities. Above results suggest that this class of compounds can affect the signaling pathways related to inflammation by directly acting on PDIA6. In particular, such compounds exhibit the strong inhibitory effects on IL-1β and IL-6 release, suggesting the potential development prospect in the treatment of inflammatory diseases.

benzophenone polyphenol  /  synthesis  /  glycosylation  /  protein disulfide-isomerase A6  /  anti-inflammation
Qiang LI, Ning-ning CHENG, Xiu-e FENG, Qing-shan LI. Glycosylation derivatization, bioactivity evaluation of benzophenone polyphenols and their interaction with protein disulfide isomerase A6[J]. Acta Pharmaceutica Sinica, 2024 , 59 (6) : 1706 -1719 . DOI: 10.16438/j.0513-4870.2023-1384
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doi: 10.16438/j.0513-4870.2023-1384
  • Receive Date：2023-12-12
  • Online Date：2025-11-26
  • Published：2024-06-12
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  • Received：2023-12-12
  • Revised：2024-04-15
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Affiliations
    1. School of Pharmaceutical Science, Shanxi Medical University, Taiyuan 030001, China
    2. Medicinal Basic Research Innovation Center of Chronic Kidney Disease, Ministry of Education, Shanxi Medical University, Taiyuan 030001, China
    3. 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
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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
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Genus		 种数
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Percentage of total
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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
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