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Screening of natural small molecule IDO-1 inhibitors with anti-tumor role
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Wei-qiang PANG1, Lei GAO2, Yue-ying DOU1, Lu LIU1, Na ZHANG1, Xiao-jia LIU1, Yang LIU1, Zhao-yong YANG1, Dan-qing SONG1, Hong-bin DENG1, *
Acta Pharmaceutica Sinica | 2017, 52(9) : 1416 - 1423
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Acta Pharmaceutica Sinica | 2017, 52(9): 1416-1423
• ORIGINAL ARTICLES •
Screening of natural small molecule IDO-1 inhibitors with anti-tumor role
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Wei-qiang PANG1, Lei GAO2, Yue-ying DOU1, Lu LIU1, Na ZHANG1, Xiao-jia LIU1, Yang LIU1, Zhao-yong YANG1, Dan-qing SONG1, Hong-bin DENG1, *
Affiliations
  • 1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
  • 2. Jilin Institute for Drug Control, Changchun 130000, China
Published: 2017-09-15 doi: 10.16438/j.0513-4870.2017-0506
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Fragments of the human indoleamine 2, 3-dioxygenase 1 (IDO1) gene 5'-UTR (untranslated 1 245 bp region) promoters were amplified by PCR and cloned into pGL4.20 vector in the construction of reporter vector pGL4-IDO1-luc. A549 cells were transfected with the constructed plasmid and IDO1 inhibitor screening model was established with dual-luciferase reporter assay. Based on the model, we screened natural small molecules which could down-regulate the expression of IDO1 on tumor cells. The anti-tumor activities were examined by MTT, Western blotting and lactic dehydrogenase (LDH) release assays. Toosendanin (NS-180) down regulated the IDO1 expression and inhibited IFN-γ-induced STAT1 and STAT3 phosphorylation in A549 cells. Moreover, NS-180 significantly increased the cytotoxicity of co-cultured NK cells on A549 cells in LDH release assays. In summary, NS-180 is a novel and potent IDO1 inhibitor, which has an antitumor activity for cancer immunotherapies.

indoleamine 2, 3-dioxygenase 1  /  promoter  /  luciferase  /  toosendanin
Wei-qiang PANG, Lei GAO, Yue-ying DOU, Lu LIU, Na ZHANG, Xiao-jia LIU, Yang LIU, Zhao-yong YANG, Dan-qing SONG, Hong-bin DENG. Screening of natural small molecule IDO-1 inhibitors with anti-tumor role[J]. Acta Pharmaceutica Sinica, 2017 , 52 (9) : 1416 -1423 . DOI: 10.16438/j.0513-4870.2017-0506
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Article Info
doi: 10.16438/j.0513-4870.2017-0506
  • Receive Date：2017-05-22
  • Online Date：2026-01-14
  • Published：2017-09-15
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History
  • Received：2017-05-22
  • Revised：2017-06-12
Funding
Affiliations
    1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
    2. Jilin Institute for Drug Control, Changchun 130000, 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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