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Synthesis and activity evaluation of aloperine derivatives based on PD-L1 tumor immunity
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Xin-tong ZHANG1, Kun WANG1, 2, Qing-xuan ZENG1, Zhi-hao GUO1, Dan-qing SONG1, Ying-hong LI1, *
Acta Pharmaceutica Sinica | 2022, 57(4) : 1085 - 1094
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Acta Pharmaceutica Sinica | 2022, 57(4): 1085-1094
• Original Articles •
Synthesis and activity evaluation of aloperine derivatives based on PD-L1 tumor immunity
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Xin-tong ZHANG1, Kun WANG1, 2, Qing-xuan ZENG1, Zhi-hao GUO1, Dan-qing SONG1, Ying-hong LI1, *
Affiliations
  • 1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
  • 2. School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China
Published: 2022-04-12 doi: 10.16438/j.0513-4870.2021-1597
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Totally 28 new 12N-substituted aloperine derivatives were designed, synthesized and evaluated for their down-regulating PD-L1 activities in breast cancer MDA-MB-231 cells. Among them, compound 7f could significantly down-regulate PD-L1 level in concentration- and time-dependent manners, and exhibit a low cytotoxicity. It activated the killing activity of co-cultured T cells against tumor cells in a concentration-dependent manner, showing the potential of tumor immunotherapy. Further study indicated that 7f mediated the degradation of PD-L1 through a lysosomal pathway. This study provides useful guidance for the development of aloperine compounds into new small molecule tumor immune suppressants.

aloperine derivative  /  PD-L1  /  antitumor  /  tumor immuno-suppression  /  lysosome
Xin-tong ZHANG, Kun WANG, Qing-xuan ZENG, Zhi-hao GUO, Dan-qing SONG, Ying-hong LI. Synthesis and activity evaluation of aloperine derivatives based on PD-L1 tumor immunity[J]. Acta Pharmaceutica Sinica, 2022 , 57 (4) : 1085 -1094 . DOI: 10.16438/j.0513-4870.2021-1597
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Article Info
doi: 10.16438/j.0513-4870.2021-1597
  • Receive Date：2021-11-09
  • Online Date：2025-12-22
  • Published：2022-04-12
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History
  • Received：2021-11-09
  • Revised：2021-12-15
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    1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
    2. School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, 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
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
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