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Identification of PD-1 small molecule inhibitors and validation in Panax ginseng
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Dai-dong WANG, Peng-fei TU, Ya-zhuo HUANG, Wan-wan WANG, Jing WANG, Ya HAN, Hong WANG, Shi-zhong CHEN*
Acta Pharmaceutica Sinica | 2020, 55(10) : 2428 - 2434
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Acta Pharmaceutica Sinica | 2020, 55(10): 2428-2434
• Original Articles •
Identification of PD-1 small molecule inhibitors and validation in Panax ginseng
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Dai-dong WANG, Peng-fei TU, Ya-zhuo HUANG, Wan-wan WANG, Jing WANG, Ya HAN, Hong WANG, Shi-zhong CHEN*
Affiliations
  • School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
Published: 2020-10-12 doi: 10.16438/j.0513-4870.2020-0901
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Tumor immune therapy has been remarkably successful in recent years and several kinds of PD-1/PD-L1 (programmed death-1/programmed death-ligand 1) antibody drugs have been approved by the FDA for treatment of advanced malignant neoplasms. However, as biomacromolecules these antibody drugs have certain drawbacks such as high cost, injection-only administration and immunogenicity; thus, we turned to small molecules that have lower immune risks and better modifiability. Considering the structural diversity of natural products, we chose to investigate the active components in Panax ginseng, a famous and highly valued traditional Chinese medicine. Nine compounds were separated and identified in this research using a HPLC-coupled MS system, and 3 PD-1 binding compounds were identified using the SPR method. The PD-1/PD-L1 inhibitory ability of ginsenoside Rg1, as a representative ginsenoside, was verified by cytopharmacological methods. This research provides a new method for the identification of immune blockade inhibitors in natural products.

PD-1  /  HPLC-MS  /  Panax ginseng  /  SPR  /  immunofluorescence  /  flow cytometry
Dai-dong WANG, Peng-fei TU, Ya-zhuo HUANG, Wan-wan WANG, Jing WANG, Ya HAN, Hong WANG, Shi-zhong CHEN. Identification of PD-1 small molecule inhibitors and validation in Panax ginseng[J]. Acta Pharmaceutica Sinica, 2020 , 55 (10) : 2428 -2434 . DOI: 10.16438/j.0513-4870.2020-0901
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doi: 10.16438/j.0513-4870.2020-0901
  • Receive Date：2020-06-05
  • Online Date：2026-01-23
  • Published：2020-10-12
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  • Received：2020-06-05
  • Revised：2020-06-23
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    School of Pharmaceutical Sciences, Peking University, Beijing 100191, 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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