期刊
BIOLOGICAL & PHARMACEUTICAL BULLETIN
卷 37, 期 6, 页码 1021-1028出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/bpb.b14-00026
关键词
papain-like protease; Tribulus terrestris; cinnamic amide; carbinolamide
资金
- National Research Foundation [2013M3A9A6003180]
- Next-Generation BioGreen 21 Program (SSAC), Rural Development Administration, Republic of Korea [PJ009571]
- BK21 plus program
- National Research Foundation of Korea [2013M3A9A6003180] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
Tribulus terrestris fruits are well known for their usage in pharmaceutical preparations and food supplements. The methanol extract of T. terrestris fruits showed potent inhibition against the papain-like protease (PLpro), an essential proteolylic enzyme for protection to pathogenic virus and bacteria. Subsequent bioactivity-guided fractionation of this extract led to six cinnamic amides (1-6) and ferulic acid (7). Compound 6 emerged as new compound possessing the very rare carbinolamide motif. These compounds (1-7) were evaluated for severe acute respiratory syndrome coronavirus (SARS-CoV) PLpro inhibitory activity to identify their potencies and kinetic behavior. Compounds (1-6) displayed significant inhibitory activity with IC50 values in the range 15.8-70.1 mu M. The new cinnamic amide 6 was found to be most potent inhibitor with an IC50 of 15.8 mu M. In kinetic studies, all inhibitors exhibited mixed type inhibition. Furthermore, the most active PLpro inhibitors (1-6) were proven to be present in the native fruits in high quantities by HPLC chromatogram and liquid chromatography with diode array detection and electrospray ionization mass spectrometry (LC-DAD-ESI/MS).
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