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PHYTOTHERAPY RESEARCH · 2011 ·Vol. 26 ·期 1 ·86-90 · IF 1.878

Investigation of UDP-glucuronosyltransferases (UGTs) Inhibitory Properties of Carvacrol

Rui-Hua Dong,Zhong-Ze Fang,Liang-Liang Zhu,Si-Cheng Liang,Guang-Bo Ge,Ling Yang,Ze-Yuan Liu

UDP-glucuronosyltransferases (UGTs), the most important phase II drug metabolizing enzymes (DMEs), could metabolize many drugs and various endogenous substances including bilirubin, steroid hormones, thyroid hormones, bile acids and fat-soluble vitamins. Evaluation of the inhibitory effects of compounds on UGTs is clinically important because inhibition of UGT isoforms could not only result in serious drug–drug interactions (DDIs), but also induce metabolic disorders of endogenous substances. The aim of the present study was to investigate the inhibitory effects of carvacrol on major UGT isoforms. The results showed that carvacrol could inhibit the activity of UGT1A9 with negligible effects on other UGT isoforms. When 4-methylumbelliferone (4-MU) was used as a nonspecific probe substrate and recombinant UGT enzymes were utilized as an enzyme resource, the inhibition of UGT1A9 was best fit to the competitive type and the inhibition kinetic parameter ( K i ) was calculated to be 5.7 µ m . Furthermore, another specific probe substrate, propofol, was employed to determine the inhibitory kinetics of UGT1A9, and the results demonstrated that the inhibitory type was noncompetitive. The inhibition kinetic parameter ( K i ) was determined to be 25.0 µ m . Because this substrate-dependent inhibition of UGT1A9 might confuse the in vitro–in vivo extrapolation, these in vitro inhibition kinetic parameters should be interpreted with special caution. Copyright © 2011 John Wiley & Sons, Ltd.

CAS / MDL: 499-75-2
研究领域: 药理学 · 生物化学
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FOOD CHEMISTRY · 2024 · IF 8.5

Microfluidic-blow-spinning of carvacrol-loaded porphyrin metal − organic framework nanofiber films with synergistic antibacterial capabilities for food packaging

Zi-An Deng,Menglu Wu,Chaoyi Shen,Xiangzheng Yang,Da Wang,Jiangkuo Li,Di Wu,Kunsong Chen

The adherence of foodborne microorganisms threatens human health, necessitating the development of antibacterial food packaging films. In this study, the antibacterial agent carvacrol (CV), hindered by its high volatility and intense aromatic odor, was encapsulated within the photosensitive metal-organic frameworks (MOFs) material PCN-224 (loading rate 50%). Subsequently, the microfluidic-blow-spinning (MBS) technique was employed for the rapid fabrication of CV@PCN-224/polycaprolactone (PCL)/chitosan (CS) nanofiber films. The incorporation of CV@PCN-224 NPs enhances the nanofiber films' thermal stability and mechanical properties and improves the water vapor permeability while maintaining the sustained release of CV over an extended period and good biocompatibility. Due to the simultaneous loading of antibacterial agent (CV) and photosensitive agent (PCN-224), the CV@PCN-224/PCL/CS films exhibited good synergistic antibacterial functionality, as demonstrated by effective inhibition against both E. coli and S. aureus . All results show the vast potential of the prepared nanofiber films in antibacterial food packaging.

研究领域: 材料科学 · 食品科学 · 微生物学
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