Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
Regular Articles
Papain-Like Protease (PLpro) Inhibitory Effects of Cinnamic Amides from Tribulus terrestris Fruits
Yeong Hun SongDae Wook KimMarcus John Curtis-LongHeung Joo YukYan WangNingning ZhuangKon Ho LeeKwon Seok JeonKi Hun Park
著者情報
ジャーナル フリー HTML
電子付録

2014 年 37 巻 6 号 p. 1021-1028

詳細
抄録

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 (16) and ferulic acid (7). Compound 6 emerged as new compound possessing the very rare carbinolamide motif. These compounds (17) were evaluated for severe acute respiratory syndrome coronavirus (SARS-CoV) PLpro inhibitory activity to identify their potencies and kinetic behavior. Compounds (16) displayed significant inhibitory activity with IC50 values in the range 15.8–70.1 µM. The new cinnamic amide 6 was found to be most potent inhibitor with an IC50 of 15.8 µM. In kinetic studies, all inhibitors exhibited mixed type inhibition. Furthermore, the most active PLpro inhibitors (16) 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).

著者関連情報
© 2014 The Pharmaceutical Society of Japan
前の記事 次の記事
feedback
Top