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DRUG METABOLISM AND DISPOSITION · 2016 ·Vol. 44 ·期 1 ·40-49 · IF 3.21

Application of a New Dynamic Model to Predict the In Vitro Intrinsic Clearance of Tolbutamide Using Rat Microsomes Encapsulated in a Fab Hydrogel

Ning Zhou,Yuanting Zheng,Junfen Xing,Huiying Yang,Hanmei Chen,Xiaoqiang Xiang,Jing Liu,Shanshan Tong,Bin Zhu,Weimin Cai

Currently used in vitro models for estimating liver metabolism do not take into account the physiologic structure and blood circulation process of liver tissue. The Bio-PK metabolic system was established as an alternative approach to determine the in vitro intrinsic clearance of the model drug tolbutamide. The system contained a peristaltic pump, recirculating pipeline, reaction chamber, and rat liver microsomes (RLMs) encapsulated in pluronic F127-acrylamide-bisacrylamide (FAB) hydrogel. The metabolism of tolbutamide at initial concentrations of 100, 150, and 200 μM was measured in both the FAB hydrogel and the circular medium. The data from the FAB hydrogel and the circular medium were fitted to a mathematical model to obtain the predicted intrinsic clearance of tolbutamide after different periods of preincubation. The in vitro clearance value for tolbutamide was incorporated into Simcyp software and used to predict both the in vivo clearance value and the dynamic process of elimination. The predicted in vivo clearance of tolbutamide was 0.107, 0.087, and 0.095 L/h/kg for i.v. injection and 0.113, 0.095, and 0.107 L/h/kg for oral administration. Compared with the reported in vivo clearance of 0.09 L/h/kg (i.v.) and 0.10 L/h/kg (oral), all the predicted values differed by less than twofold. Thus, the Bio-PK metabolic system is a reliable and general in vitro model, characterized by three-dimensional structured RLM and circulation and perfusion processes for predicting the in vivo intrinsic clearance of low-extraction compounds, making the system more analogous with the rat in terms of both morphology and physiology

研究领域: 药代动力学 · 药物代谢 · 生物医学工程
✓ 已验证 DOI PubMed 高影响因子
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Journal of Future Foods · 2025 · IF 7.2

Preparation and characterization of polypeptide film/coating derived from Idesia polycarpa Maxim. Cake meal and their application in nectarine freshness preservation

Lei Dou,Zimu Zhang,Xiufang Huang,Yaobing Chen,Kai Luo,Jianquan Kan

Considering that the peptide from Idesia polycarpa Maxim.cake meal polypeptide (CIP) is a novel antioxidant agent, this study aimed to develop an efficient and safe food film by incorporating the CIP agent into a gelatin matrix. The films with different concentrations of CIP were characterised and applied in the preservation of nectarines. The results indicated that the CIPF/3% fraction exhibited significant moisture barrier properties, with a water vapor permeability (WVP) of only 8.12 % ± 0.09 %. Additionally, it demonstrated excellent mechanical and antioxidant properties, with scavenging capacities of 76.31 % ± 0.597 %, 65.98 % ± 0.444 %, and 60.98 % ± 0.231% for DPPH, ABTS, and hydroxyl radicals, respectively, surpassing those of other fractions. In nectarine freshness preservation, the Coating/3% fraction showed the best performance. It significantly reduced the weight loss rate of nectarines, improved fruit firmness, maintained the pH value, and minimized nutrient losses, including ascorbic acid and Total soluble sugars (TSS). Furthermore, it effectively preserved the bright surface color of nectarines and extended their shelf life. In summary, the specific environmental protection, safety, and preservation qualities of the CIPF/Coating in food packaging suggest a promising potential for its application.

CAS / MDL: 9000-70-8
研究领域: 食品科学 · 高分子科学 · 抗氧化技术 · 食品保鲜 · 材料表征 · 可食用涂层 · 农业副产物利用
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ChemistrySelect · 2022 ·Vol. 7 ·期 42 ·e202203493 · IF 2.307

Synthesis of a Nanoparticle of Selenious Acid Acyl Diaquercetin for Skin Care Products

Xiang Yu,Mengyu Liu,Zaiheng Huang,Yanzhi Tao,Hao Yang,Hongbin Gan,Guangzai Nong

Graphical Quercetin and selenite were combined to form a quercetin selenium complex at 100°C. The mass of the product was 30.3 % of the mass of quercetin and the structure was analyzed in depth. The complex had a DPPH antioxidant activity of 97.91 %, and the prepared skin cream containing 1 % of the complex had an antioxidant activity of 82.4 %. Flavonoid complexes have more biological activities than parent flavonoids, including antioxidant, anticancer, antibacterial, and many others. Selenium is an essential trace element for human body. Therefore, a quercetin-Se complex was synthesized and analyzed in this paper, getting the results as following: (1) A light- yellow product was obtained with the max yield of 30.30 %. (2) The complex molecule contains two quercetin units and a selenoxyl group, called selenious acid acyl diquercetin. (3) It has a strong antioxidant activity with a maximum DPPH scavenging rate of 97.71 %. In addition, we prepared a skin cream containing 1 % quercetin selenium complex, and it has excellent antioxidant activity with a DPPH scavenging rate of 82.4 %. Therefore, the generated selenious acid acyl diquercetin is a potential antioxidant material for skin care products.

研究领域: 化学 · 生物学 · 药学
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Journal of Food Measurement and Characterization · 2024 · IF 2.9

Optimization of ultrasound-assisted deep eutectic solvent extraction, characterization, and biological studies of polysaccharide from seeds of Toona sinensis

Wen Yao,Chen Geping,Zhang Xiaobing

The present study aimed to evaluate the polysaccharides extracted from Toona sinensis seeds using ultrasound-assisted deep eutectic solvent (DES). The extracted polysaccharides (TSRP) were purified and studied for their hypoglycemic and antioxidant activities. The purified polysaccharides (TSRPs-1) were hydrolyzed and derivatized to study their monosaccharide composition. The optimum extraction conditions were DES (choline chloride to oxalic acid) at a molar ratio of 1.473:1, ultrasound time of 50.643 min, and a material-to-liquid ratio of 1:31.838 g/mL. The ultrasound-assisted DES extraction was more effective (56.1%) as compared to the water extraction (35.89%). The inhibition of α-glucosidase by TSRPs-1 was 42.77% at a concentration of 0.8 mg/mL. At 3.2 mg/mL, TSRPs-1 inhibited α-amylase by 34.38%. The clearance of DPPH by TSRPs-1 was 24.36% at 3.2 mg/mL. The IC 50 for ABTS· + clearance by TSRPs-1 was 0.233 mg/mL. It was shown that the monosaccharides of TSRPs-1 were composed of Man, Rha, GlcA, GalA, Glc, Gal, Xyl, and Ara in a molar ratio of 1:563.13:41.81:51.20:21.81:2244.58:3.73:1130.48. In this paper, the process of extracting TSRP with ultrasound-assisted DES was investigated and optimized. TSRPs-1 possesses certain hypoglycemic and antioxidant activities. Therefore, this paper can provide an experimental basis for the establishment of an industrialized production process of polysaccharides and the study of their biological activities.

CAS / MDL: 56180-94-0 3767-28-0
研究领域: 药学 · 食品化学 · 生物化学 · 植物科学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2024 · IF 7.7

Preparation of antibacterial composite film based on arginine-modified chitosan and its application in the preservation of ready-to-eat sea cucumber

Jinghe Sun,Yimeng Li,Tingting Yan,Jingfeng Yang

An edible composite film was developed and applied for ready-to-eat sea cucumber storage to improve the product quality. The PAC film base is first prepared by mixing 0.5 % glycerin (GL) with 4 % polyvinyl alcohol (PVA) and 1 % arginine-modified chitosan (Arg-CTS) in the same volume. After the addition of nano-ZnO (ZnO) and thymol (Thy) to the PAC film base, the mechanical properties and functions were tested. Compared to the PAC film, the PAC-ZnO-ThyH composite film showed a 1.34-fold increase in the DPPH scavenging rate and a 2.19-fold increase in the ABTS scavenging rate. Contrary to the PAC film, the inhibition zone diameter of Escherichia coli and Staphylococcus aureus significantly increased by 2.35 and 4.08 folds in the PAC-Zno-ThyH film, respectively. After applying the PAC-ZnO-ThyH film to store ready-to-eat sea cucumber for 10 days, there was a significant reduction in weight loss, total volatile basic nitrogen (TVB-N), and lipid oxidation levels to 1.47 and 1.26 folds to the Ctrl group. After preservation, the hardness and chewiness of ready-to-eat sea cucumber were maintained at 1079.62 ± 138.86 N and 913.73 ± 175.79 N, respectively. The novel PAC-ZnO-ThyH composite film can be used as an active food packaging for promising seafood applications.

CAS / MDL: 9012-76-4
研究领域: 食品科学 · 材料科学 · 生物技术
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JOURNAL OF FOOD PROCESSING AND PRESERVATION · 2021 ·Vol. 45 ·期 12 ·e16074 · IF 2.19

Degradation by Vc-H2O2, characterization and antioxidant activity of polysaccharides from Passiflora edulis peel

Xia Li,Guozhu Zhang,Jing Li,Tiemin Jiang,Huiying Chen,Peijun Li,Yuan Guan

In this paper, water extracted polysaccharides from Passiflora edulis peel (WPEP) was degraded by ascorbic acid-hydrogen peroxide (Vc-H 2 O 2 ). The degradation conditions were optimized by response surface methodology (RSM). The 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging rate of degraded WPEP (DWPEP) was 45.38% under optimal conditions (Vc-H 2 O 2 concentration 9.3 mM, temperature 52°C, time 1.4 hr). And the molecular weight (Mw) of DWPEP (38 kDa) was 32.20% (WPEP was 118 kDa). WPEP and DWPEP were mainly composed of galacturonic acid. Their backbone structures, functional groups and β-glycoside linkage patterns are similar, however, still with some differences. Antioxidant tests showed that WPEP and DWPEP had strong DPPH radical scavenging ability (93.03% and 81.70%), moderate hydroxyl radical scavenging ability (53.99% and 26.59%), and low reducing power (0.698 and 0.52). In conclusion, these differences in structures and properties may be an important factor affecting the antioxidant activity of polysaccharides. Novelty impact statement In this paper, the Vc-H 2 O 2 system was used to degrade the polysaccharides extracted from Passiflora edulis peel. The molecular weight, intrinsic viscosity, and rigid conformation changed obviously. The degraded polysaccharides are valuable to expand their application and to improve the practical efficacy.

CAS / MDL: 50-81-7 7722-84-1
研究领域: 食品科学 · 生物化学
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RSC Advances · 2025 ·Vol. 15 ·期 19 ·14594-14603 · IF 4.6

Electron structure variations in hindered phenolic antioxidant induced enhancement of thermo-oxidative aging performance in polyamide 6

Bingxue Guo,Jinfen Lou,Tingting Kuang,Yanping Wang,Kai Zhang,Jun Qin,Min He,Yufei Liu,Yong-Ji Gong

PA6 is widely used but vulnerable to thermo-oxidative aging, impacting its durability. Hindered phenols are key antioxidants that extend the service life of PA6 by slowing this aging process. However, the effect of molecular structural differences on their antioxidant activity is still elusive, impeding their development and application. Here, two antioxidants, 2-((3-(3,5-di-tert-butyl-4-hydroxyphenyl)propionyl)oxy)ethyl acrylate (PEA) and 2-((3-(3,5-di-tert-butyl-4-hydroxyphenyl)propionyl)oxy)propyl acrylate (PPA), were utilized to enhance the thermo-oxidative aging resistance of PA6. Their primary difference is that PPA possesses an electron-donating group in its molecular structure. The methyl functional group in the PPA molecule can increase the electron cloud density around the benzene ring, resulting in PPA having a higher free radical scavenging rate compared to PEA. In addition, in contrast to PEA, the low volatility and mobility of PPA ensure that its antioxidant activity can be fully utilized during aging. These factors collectively support the excellent antioxidant activity of PPA (PPA > PEA). As a result, the PA6/PPA composite maintains 88% of its original tensile strength after 12 days of continuous aging, whereas PA6/PEA and PA6/1010 (commercial antioxidant) composites retained 70% and methyl 30%, respectively. These encouraging findings provide a theoretical basis for the synthesis of antioxidants.

研究领域: 材料科学 · 化学工程
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PHARMACOLOGY · 2016 · IF 1.533

Effects of 22 CYP2D6 Genetic Variations Newly Identified in Chinese Population on Olanzapine Metabolism in vitro

Zhou Hong-Yu,Gu Er-Min,Chen Qiu-lei,Zhan Yun-Yun,Wang Shuang-Hu,Liang Bing-Qing,Dai Da-Peng,Cai Jian-Ping,Hu Guo-Xin

The objective of this study was to assess the catalytic activity of 22 novel CYP2D6 allelic variants (2D6*87-*98, R25Q, F164L, E215K, F219S, V327M, D336N, V342M, R344Q, R440C and R497C) to olanzapine in vitro. Their protein products expressed in Spodoptera frugiperda 21 (Sf21) insect cells were incubated with olanzapine 100-2,000 μmol/l for 30 min. The kinetic parameters of Km, Vmax and intrinsic clearance were determined by 2-hydroxymethylolanzapine, the metabolite of olanzapine mediated by CYP2D6, using ultra-performance liquid chromatography tandem mass spectrometry. Results showed that the kinetic parameters of 2 alleles, CYP2D6*92 and 2D6*96, could not be detected; 17 allelic variants, CYP2D6*87-*88, 2D6*90-*91, 2D6*93-*95, 2D6*97, R25Q, F164L, E215K, F219S, V327M, V342M, R344Q, R440C and R497C, significantly reduced the intrinsic clearance of olanzapine; 2 variants, CYP2D6*89 and 2D6*98, increased the intrinsic clearance of olanzapine; no difference was found in intrinsic clearance of D336N. Furthermore, 6 alleles, CYP2D6*87, 2D6*88, 2D6*91, 2D6*93, 2D6*97 and R497C, exhibited higher Km values in a range of 120.80-217.56% relative to wild-type CYP2D6*1. The research demonstrated the metabolic phenotype of the 22 novel CYP2D6 variants for olanzapine that were different from probe drugs we used previously and might provide beneficial information to the personalized medicine of olanzapine

CAS / MDL: 631-61-8
研究领域: 药理学 · 临床医学 · 分子生物学
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LWT-FOOD SCIENCE AND TECHNOLOGY · 2024 · IF 6

Covalent modification of soy protein isolates by hydroxytyrosol: Effects on structural and functional properties of adducts

Meiyu Gu,Jiahui Shi,Boya Zhang,Xibo Wang,Xu Wang

The effect of covalent binding of different concentrations of hydroxytyrosol (HT) to soy protein isolate (SPI) by enzymatic method on the structure and function of the complex was investigated. Polyphenol binding rate increased and then decreased with increasing hydroxytyrosol concentration, with a maximum binding rate of 38.10 ± 1.08%. Covalent binding to HT resulted in a significant increase in the turbidity of the adduct and a significant decrease in the free sulfhydryl content and surface hydrophobicity. The structure of the adduct was altered and the α-helix structure was converted to a β-sheet one. The maximum foaming property of the adducts was observed at a HT concentration of 40 μmol/g, which was 28.84% higher than the control SPI. The adduct had maximum solubility (52.84 ± 0.18%) at HT concentration of 50 μmol/g. The emulsifying properties of the adducts were maximized at a hydroxytyrosol concentration of 60 μmol/g. When the HT concentration was 70 μmol/g, the DPPH and ABTS radical scavenging rates of the adducts were increased by 245.03% and 26.35%, respectively, compared with the control SPI.

CAS / MDL: 10597-60-1
研究领域: 食品科学 · 蛋白质化学 · 生物技术
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JOURNAL OF MEMBRANE SCIENCE · 2022 · IF 10.53

Constructing hierarchical surface structure of hemodialysis membranes to intervene in oxidative stress through Michael addition reaction between tannic acid and PEtOx brushes

Qi Chen,Miaoshen Kou,Yang He,Yiping Zhao,Li Chen

Chronic kidney disease (CKD) patients undergoing hemodialysis is often accompanied by high levels of oxidative stress, profoundly affecting the survival rate and long-term outcome of patients. Functionalized hemodialysis membranes with relieving oxidative stress and outstanding biocompatibility have aroused more attention among researchers. In this work, we incorporated a tannic acid (TA) coating onto the poly (ether sulfone) (PES) hemodialysis membrane in order to alleviate the increased oxidative stress status during hemodialysis. Further modification of poly(2-ethyl-2-oxazoline) (PEtOx) brushes devoted to improving the biocompatibility of hemodialysis membrane. The TA/PEtOx brushes functionalized membranes effectively eliminated reactive oxygen species (ROS), increased serum antioxidant level, and inhibited lipid peroxides and glycation products generation. The functionalized membranes attenuated the H 2 O 2 -induced oxidative damage to cardiomyocytes (H9C2) and vascular endothelial cells (HUVEC) by modulating the antioxidant enzymes expression (SOD, CAT and GSH). The immobilization of PEtOx brushes significantly improved the biocompatibility, and the TA/PEtOx brushes functionalized membranes have been constructed through the Michael addition reaction between TA and PEtOx brushes. Simultaneously, the cyclic PEtOx (C-PEtOx) brushes simulating the structure of endothelial glycocalyx formed a stronger steric hindrance and a denser hydration layer that significantly suppressed the platelets and erythrocytes adhesion on membrane surface. The optimal functionalized membrane exhibited a 76.5% of urea clearance, 53.4% of lysozyme clearance and 95.9% of bovine serum albumin (BSA) retention. This present work fabricated a biomimetic surface structure for the development and preparation of novel hemodialysis membrane, which would greatly improve the therapeutic effect in patients.

研究领域: 生物医学工程 · 材料科学 · 生物材料 · 细胞生物学 · 肾病学
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JOURNAL OF MEMBRANE SCIENCE · 2022 · IF 10.53

Flexible Zr-MOF anchored polymer nanofiber membrane for efficient removal of creatinine in uremic toxins

Wenyan Li,Yumei Li,Xinggui Wen,Yakun Teng,Jing Wang,Tianyi Yang,Xiang Li,Lijuan Li,Ce Wang

High-performance and low-cost hemodialysis membranes are urgently needed by patients suffering from end-stage renal disease. Here, we designed a flexible multifunctional Zr-MOF anchored polyacrylonitrile (PAN) nanofiber membrane (UAPNFM), which has good adsorption, dialysis, and regeneration ability. A novel adhesive layer modification method was used to make UIO-66-(COOH) 2 nanocrystals grow in-situ on the composite nanofibers . The UIO-66-(COOH) 2 nanocrystals were uniformly and stably anchored on the nanofibers with the content of 54.99 wt%. The obtained UAPNFM has the capability to effectively remove uremic toxins with excellent retain protein rate. The Langmuir isotherm and pseudo-second-order kinetic model can be applied to better describe the adsorption process . The maximum adsorption capacity of UAPNFM for creatinine reached 168.63 mg/g. After 4 h of simulate dialysis, the clearance rate of creatinine was 82.48% and the protein retention rate of bovine serum albumin (BSA) by the UAPNFM was 93.09%. In addition, after four cycles, the removal efficiency for creatinine still remained at 82.31%. The results show that the UAPNFM has good regenerability. Moreover, the composite nanofiber membrane exhibited satisfactory blood compatibility. Therefore, this unique flexible Zr-MOF anchored polymer composite nanofiber membrane with an outstanding creatinine removal performance provides a new opportunity for cost reduction for clinical hemodialysis.

研究领域: 生物医学工程 · 材料科学 · 肾脏病学
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS · 2025 · IF 5.4

Layers of Electrostatically Self-assembled Composite Hydrogel Beads Based on Porous Starch and ZnO Filling for Intestinal Sustained Release of Quercetin

Shuqi Guo,Xueze Zhang,Shangxuan Li,Huifang Wang,Xianghua Gao,Baolong Niu,Wenfeng Li

Quercetin (Que) is a naturally occurring bioactive compound with various potential health benefits, but its low stability and low bioaccessibility limit its application in functional foods. Therefore, there is an urgent need to prepare a novel composite hydrogel bead with efficient and controlled release. Specifically, porous starch (PS) was first prepared by enzymatic hydrolysis to increase the specific surface area and thus enhance the adsorption rate of Que. Scanning electron microscopy confirmed the formation of the PS and the adsorption of Que. The maximum swelling properties of carboxymethylcellulose-porous starch composite hydrogel beads (CQPZ) were reduced by adding different amounts of zinc oxide to achieve slow release. The results showed that the higher the amount of zinc oxide, the stronger the slow-release performance, while the lower the drug loading capacity. To obtain composite hydrogel beads with both low swelling and high drug-carrying properties, bilayer gel beads (CQPZ/CS) were prepared by electrostatic self-assembly of carboxymethyl cellulose and chitosan. The experimental results showed that the drug loading was significantly increased by nearly 2-fold while enhancing the slow-release performance. In addition, the CQPZ/CS composite hydrogel beads enhanced the stability of Que under light and heat conditions, and the DPPH radical scavenging rate after UV irradiation was still greater than 75%, which was much higher than that of free quercetin (31.08%). In conclusion, the prepared hydrogel beads are a promising delivery system for bioactive compounds.

CAS / MDL: 7705-08-0 9004-32-4
研究领域: 食品科学 · 药剂学 · 材料科学 · 生物技术 · 纳米技术
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