Gut microbial β-glucuronidases (gmβ-GUS) played crucial roles in regulating a variety of endogenous substances and xenobiotics on the circulating level, thus had been recognized as key modulators of drug toxicity and human diseases. Inhibition or inactivation of gmβ-GUS enzymes has become a promising therapeutic strategy to alleviate drug-induced intestinal toxicity. Herein, the Rhodiola crenulata extract (RCE) was found with potent and broad-spectrum inhibition on multiple gmβ-GUS enzymes.
View Article and Find Full Text PDFMater Today Bio
August 2023
Eukaryotic expression systems are frequently employed for the production of recombinant proteins as therapeutics as well as research tools. Among which mammalian cell protein expression approach is the most powerful one, which can express complex proteins or genetic engineered biological drugs, such as PD-1. However, the high expense, which partially derives from its low protein yielding efficiency, limited the further application of such approach in large scale production of target proteins.
View Article and Find Full Text PDFHuman cytochrome P450 1B1 (hCYP1B1), an extrahepatic cytochrome P450 enzyme over-expressed in various tumors, has been validated as a promising target for preventing and treating cancers. Herein, two series of chalcone derivatives were synthesized to discover potent hCYP1B1 inhibitors without AhR agonist effect. Structure-activity relationship (SAR) studies demonstrated that 4'-trifluoromethyl on the B-ring strongly enhanced the anti-hCYP1B1 effects, identifying A9 as a promising lead compound.
View Article and Find Full Text PDFEnzymes constitute an extremely important class of biomacromolecules with diverse catalytic functions, which have been validated as key mediators for regulating cellular metabolism and maintaining homeostasis in living organisms [...
View Article and Find Full Text PDFThree-dimensional (3D) tumor cell culture offers a more tissue-recapitulating model in cancer treatment evaluation. However, conventional models based on cell-substrate adhesion deprivation are still of insufficient real tumor mimic. In this work, a novel method is proposed for inducing multicellular spheroids (MCSs) formation based on hydrogel with tunable microenvironmental properties.
View Article and Find Full Text PDFYing Yong Sheng Tai Xue Bao
April 2020
Under the background of climate change, the spatial-temporal distribution of precipita-tion in Heilongjiang Province is uneven, and drought and flood frequently change, which is not conducive to the safety of soybean production for the province. To clarify the influence mechanism of drought and flood in the growing season on soybean yield in Heilongjiang Province, we analyzed the time-series characteristics of drought and flood in soybean growing season and its effect on soybean yield in different growth stages, based on data of daily precipitation from 60 meteorological stations during 1961 to 2018 and soybean yield in the same period, with the standardized precipitation index (SPI) as the drought and flood evaluation index. The results showed that, from 1961 to 2018, the influence range of drought in soybean growing season in Heilongjiang Province showed a weak decreasing trend, while that of flood showed a weak increasing trend.
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