Ya-Qiao Wang's research while affiliated with Shanghai University of Traditional Chinese Medicine and other places

Publications (5)

Article
Human carboxylesterase 2 (CES2A), one of the most abundant hydrolases distributed in human small intestine and colon, play key roles in the hydrolysis of a wide range of prodrugs and other esters. Recent studies have demonstrated that CES2A inhibitors may ameliorate irinotecan-induced severe diarrhea, but the specific and efficacious inhibitors tar...
Article
Magnolol, the most abundant bioactive constituent of the Chinese herb Magnolia officinalis, has been found with multiple biological activities, including anti-oxidative, anti-inflammatory and enzyme-regulatory activities. In this study, the inhibitory effects and inhibition mechanism of magnolol on human carboxylesterases (hCEs), the key enzymes re...
Article
This study investigated the inhibitory effect of eight natural flavonoids in Chinese herb Scutellariae Radix on huamn cytochrome P450 1A (CYP1A), a key cancer chemo-preventive target. In this study, phenacetin was used as a probe substrate for CYP1A, while human liver microsomes and recombinant human CYP1A enzymes were used as enzyme sources. Liqui...
Article
Human carboxylesterase 1 (hCE1) is a key enzyme responsible for the hydrolysis of a wide range of endogenous and xenobiotic esters, but the highly selective inhibitors against hCE1 are rarely reported. This study aimed to assess the inhibitory effects of natural flavonoids against hCE1 and to find potential specific hCE1 inhibitors. To this end, fi...

Citations

... According to the MS/MS spectra, these metabolites were primarily formed by hydrolysis. Since the catalytic efficiency and affinity of substrate(s) are fundamental for evaluating species-specific differences towards given biotransformation Wang et al. 2020), the enzyme kinetics for toddalolactone metabolism in liver microsomes from various species were established. Enzymatic kinetic analyses showed that oxidative metabolism profiles of toddalolactone for humans, rats, rabbits, mice and pigs followed the classic Michaelis-Menten kinetics, as evidenced by an Eadie-Hofstee plot, suggesting that toddalolactone was metabolized by the species through only one isozyme or two isozymes with the same K m value (Jiang et al. 2020), while such biotransformation in monkeys and dogs obeyed biphasic kinetics and substrate inhibition, respectively. ...
... Yet studies of Atgl −/− -and Hsl −/− mice revealed pronounced residual TG hydrolase activity in non-adipose tissues and members of the carboxylesterase (hCES/mCes) family are suggested to act as additional neutral lipid hydrolases [6][7][8][9][10][11][12]. Enzymes, that play key roles in lipid metabolism and/or metabolic activation of many drugs, like members of the human CES family, are very interesting pharmaceutical targets [10][11][12][13]. The human CES superfamily is divided into five families (CES1, CES2, CES3, CES4A, and CES5A) and all proteins have approx. ...
... Magnolol is widely used as medicine, because it has been identified as having anticancer, anti-inflammatory, and antimicrobial effects; liver protection; and anti-mutagenesis properties [49][50][51][52]. As an extract of traditional Chinese medicine, magnolol is often used as an oral drug and has shown obvious positive effects on human health [53,54]. Therefore, the safety of magnolol is certain. ...
... Our results show that the binding energy of three toxicants under study was similar to that documented for carbaryl, a carbamate pesticide potent inhibitor of cholinesterases in the presence of interfering enzymes such as chymotrypsin, lipase, proteinase K, and others (Dai et al., 2021). In contrast, these values were lower than reported for nevadensin, a natural flavonoid highly selective inhibitor for human CES1 and CES2 (Wang et al., 2018). In agreement with current results, it has been documented that NP is a potent inhibitor of CES present in the hepatic microsomal fraction or the hepatic post-mitochondrial fraction of different fish species and decapods (Solé and Sanchez-Hernandez, 2015). ...