Identification of PD-1 small molecule inhibitors and validation in Panax ginseng
- VernacularTitle:人参中PD-1小分子抑制剂的筛选及活性验证
- Author:
Dai-dong WANG
1
;
Peng-fei TU
1
;
Ya-zhuo HUANG
1
;
Wan-wan WANG
1
;
Jing WANG
1
;
Ya HAN
1
;
Hong WANG
1
;
Shi-zhong CHEN
1
Author Information
- Publication Type:Research Article
- Keywords: PD-1; HPLC-MS; italic>Panax ginseng; SPR; immunofluorescence; flow cytometry
- From: Acta Pharmaceutica Sinica 2020;55(10):2428-2434
- CountryChina
- Language:Chinese
-
Abstract:
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.
