INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Ru Huan,Peigen Xu,Shuang Chen,Yao Dong,Chen Zhang,Dan Lu,Yilan Ouyang,Jiangyun Liu,Zhenyu Xuan,Chunshan Gui
Human organic anion transporting polypeptides (OATPs) 1B1 and 1B3 are two closely related transporters. However, OATP1B1- and 1B3-mediated estrone-3-sulfate (E3S) uptake can be differentially modulated by quercetin-3- O -α-L-arabinopyranosyl(1 → 2)-α-L-rhamnopyranoside (QAR), a compound found in some fruits such as jujube. In this study, we isolated QAR from jujube leaves and investigated the molecular mechanism underlying the activation of OATP1B3-mediated E3S uptake by QAR through functional characterization on a range of chimeric transporters derived from OATP1B3 and molecular modeling. Our findings revealed that the residue Ser545 in transmembrane domain 10 (TM10) is crucial for the activation of OATP1B3 by QAR. Kinetic analyses showed that QAR enhances OATP1B3-mediated E3S uptake at low substrate concentrations due to an increase in substrate binding affinity. Mutational analysis and molecular modeling suggested that amino acid residues with smaller side chains at position 545 are vital for the activation of OATP1B3, as bulkier residues could lead to steric collision with E3S. While QAR stimulates OATP1B3-mediated E3S uptake, it inhibits OATP1B3-mediated estradiol-17β-glucuronide/rosuvastatin uptake, indicating that the effect of QAR on OATP1B3's function is substrate-dependent. In summary, Ser545 within TM10 is essential for the activation of OATP1B3-mediated E3S uptake by QAR.
研究领域:
药理学
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分子生物学
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膜转运
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药物代谢
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天然产物
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高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2022
·Vol. 37
·期 3
·e5571
·
IF 1.911
Shuang Guo,Shuo Liu,Jing Meng,Dongyu Gu,Yi Wang,Dajun He,Yi Yang
Morus alba leaves are a natural product with great antidiabetic potential. However, the therapeutic efficacy of natural products is usually achieved through the interaction of active compounds with specific targets. Among them, active compounds with multi-target therapeutic functions are more effective than single-target enzymes. In this study, a bienzyme system was constructed by co-immobilizing α -amylase and α -glucosidase onto Fe 3 O 4 for affinity screening of dual-target active components in the complex extract from M. alba leaves. As a result, a potential active compound was selectively screened by ligand fishing, separated by high-speed countercurrent chromatography using a solvent system of ethyl acetate– n -butanol–water (3:2:5, v/v), and identified as rutin. In addition, the result of molecular docking showed that rutin could interact with the active center of α -amylase and α -glucosidase through multiple hydrogen bonds, van der Waals forces, etc. to play an inhibitory role. These results demonstrate the effectiveness of the polydopamine magnetically immobilized bienzyme system for dual-target affinity screening of active substances. This study not only reveals the chemical basis of the antidiabetic activity of M. alba leaves from a dual-target perspective, but also promotes the progress of multitarget affinity screening.
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高影响因子
RESEARCH ON CHEMICAL INTERMEDIATES
·
2023
·Vol. 49
·期 12
·5567-5593
·
IF 3.3
Doan Manh Dung,Wang San-Lang,Nguyen Van Bon,Phan Thi Kim Phung,Phan Tu Quy,Nguyen Tan Thanh,Nguyen Thi Huyen,Nguyen Quang Vinh,Nguyen Anh Dzung
Dillenia ovata Wall. ex Hook. f. et Thomson (DOWHT)—an indigenous medicinal plant collected in the Central Highland of Vietnam—has been utilized by medical folks for ages. However, almost related scientific evidence still has not been clarified. This study aimed to report the phytochemical profiles and novel potent biofunctions of DOWHT. The testing bioactivities of different parts used of DOWHT indicated this herbal demonstrated moderated inhibition against α-amylase and α-glucosidase, while it showed potent anti-oxidant and anti-acetylcholinesterase (AChE). Of these, the inhibition against the key enzymes targeting anti-diabetes and Alzheimer's disease was notably reported for the first time. The phytochemical profiles of all the parts used of DOWHT were investigated via GC–MS and UHPLC analysis. Totally, 46 compounds, including 30 volatiles (compounds 1–30) and 16 phenolics (compounds 31–46), were newly identified from DOWHT extracts. In this work, various volatiles and phenolics were newly found in this herbal species. In the docking study, some major phenolics including Epigallocatechin gallate (34), Epicatechin gallate (36), Vitexin (37), and Apigetrin (41) possess DS values (− 12.5 to − 13.3 kcal/mol) better than Berberine chloride (− 12.1 kcal/mol). Moreover, almost tested metabolites comply with the drug-likeness properties of Lipkin's rules prediction and nontoxicity via the ADMET test. The results suggest the herb DOWHT may be a potential source for drug discovery and these in silico results may be good reference information for further in vitro and in vivo experiments.
研究领域:
药理学
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植物化学
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药物开发
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高影响因子
Journal of Future Foods
·
2022
·
IF 0
Yuetong Chen,Wenhao Yu,Shanshan Zhang,Yabin Niu,Yanrong Zhang,Tingting Liu
ABSTRACT In this paper, using to the comprehensive scoring method, pressure shear assisted extraction was used to prepare polysaccharide from Auricularia auricula (PS-AAP)by orthogonal test to optimize the extraction. The highest comprehensive score (90.70) was obtained under 1: 70 g/mL solid-liquid ratio, 110 °C reaction temperature, 60 min reaction time and 1.0 MPa reaction pressure. Compared to AAP by water bath(WB-AAP), PS-AAP led to a higher extraction efficiency and decreased the relative molecular weight. In addition, infrared spectrum(FT-IR) analysis showed that pressure shear assisted did not change the polysaccharide structure. Scanning electron microscope(SEM) showed that PS-AAP was smaller and more broken by pressure shear assisted. Furthermore, the ratio of glucose to mannose in PS-AAP was relatively higher than WB-AAP, which also proved that PS-AAP had certain antioxidant and hypoglycemic activities. Compared with WB-AAP, the inhibition α -glucosidase and α -amylase activity of PS-AAP increased by 11.37% and 24.43% respectively. These results revealed that PS-AAP has the poten- tial value of being a antioxidant and hypoglycemic agent.
研究领域:
食品科学
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生物化学
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JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2024
·Vol. 333
·期 3
·1357-1365
·
IF 1.5
Mei Lingzi,Shao Hui,Cui Lingzhi,Yang Jinmin,Zhang Lei
A novel method for rapid radioanalytical measurement of uranium and plutonium in 100ml emergency urine samples was developed, through optimized selection of the separation and purification process and a combined measurement with ICP-TOF-MS and alpha spectrometry. The typical analytical time is within 6 h, the recovery rates are more than 80%, and the minimum detection activity concentrations are 3.4 × 10 −4 Bq/L for 238 U and 2.5 × 10 −3 Bq/L for 239 Pu respectively. The spiked test shows that this method can be used for quantitative evaluation of the activity concentration of 238 U and 239 Pu in urine samples accurately.
研究领域:
放射化学
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环境科学
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医学检测
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高影响因子
CHEMISTRY & BIODIVERSITY
·
2026
·Vol. 23
·期 1
·e03315
·
IF 2.5
Shi-Hui Lu,Xiu-Xia Li,Xiao-Yan Xia,Wei-Neng Li,Kai-Jie Luo,Jing Huang
In the phytochemical study of the leaves of Ligustrum robustum , two new monoterpenoid glycosides named ligurobustosides V ( 1a ), V 1 ( 1b ), and a new secoiridoid glycoside named ligurobustoside W ( 2 ), together with three known glycosides ( 3 – 5 ), were isolated and identified by spectroscopic and chemical methods. The biological research discovered, compounds 3 and 4 showed powerful fatty acid synthase inhibitory activity (half inhibitory concentration [IC 50 ]: 4.21 ± 0.16–4.51 ± 0.12 µM); compounds 1 , 4 , and 5 displayed some α -glucosidase inhibitory activity; compounds 1 - 5 revealed some α -amylase inhibitory activity; compounds 1 , 3 , and 4 showed stronger 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt radical scavenging effect (IC 50 : 3.98 ± 0.01–6.80 ± 0.07 µM) than L-(+)-ascorbic acid (IC 50 : 10.06 ± 0.19 µM). Compounds 1 , 3 , and 4 were considered as some functional constituents of L. robustum to prevent diabetes mellitus and its complications. Graphical This article reports two new monoterpenoid glycosides and a new secoiridoid glycoside from the leaves of Ligustrum robustum; meanwhile describes their inhibitory capacities on alpha-glucosidase, alpha-amylase, fatty acid synthase, and their antioxidant effects.
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高影响因子
Polymer Chemistry
·
2020
·Vol. 11
·期 14
·2492-2501
·
IF 5.342
Wenpeng Zhao,Bo Dong,Heng Liu,Yanming Hu,Xuequan Zhang
A new alternative for accessing metal–ligand containing polymers via coordination insertion copolymerization of 1-hexene and ligated α-olefin is disclosed herein. To overcome the deactivation of active species by heteroatoms, the present study employed a less electrophilic late transition metal complex, and efficient copolymerizations were successfully achieved, giving rise to poly(1-hexene) elastomers containing a benzimidazolyl quinoline ligand up to 5.77%. Moreover, the copolymerization displayed a living nature, demonstrating a capability of control over the molecular weights and molecular weight distribution. Coordination of the obtained ligated poly(1-hexene) elastomers with metal ions produced polymer networks with the ligand–metal complexes as crosslinkers and thus led to a significant enhancement of the mechanical properties of the resultant materials.
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JOURNAL OF ALLOYS AND COMPOUNDS
·
2025
·
IF 6.3
Jiabao Zang,Haifeng Li,Qingzhi Zhu,Ziheng Wang,Hubuli Bazaerbieke,Li Sun,Meijie Zhang
There are few reports about the electromagnetic wave (EMW) absorption properties of α−SiC based composites, and almost all of them focus on β−SiC polymorphs. In this study, α−SiC p /α−SiC nw /SiO 2 /C hybrid composites (sample SiC−C1500) with heterostructure α−SiC nanowires (α−SiC nw ) of multiple interfaces 4H−SiC/6H−SiC/SiO 2 /C were successfully prepared using mixed powder (α−SiC+m−SiO 2 +C) as raw material based on the heterogeneous nucleation−growth mechanism, and their microwave absorption properties were investigated. Meanwhile, the samples SiC−V2150 and Si−C1500 were obtained by vacuum calcination (α−SiC+m−SiO 2 +C) at 2150 0 C and carbothermal reduction (Si+m−SiO 2 +C) at 1500 0 C, respectively, and their phase compositions were α−SiC p /C and β−SiC p /β−SiC nw /SiO 2 /C, respectively. The sample SiC−C1500 exhibited excellent EMW absorption properties, with a minimum reflection loss (RL min ) value of −18.37 dB at a thickness of 1.3 mm, and a maximum effective absorption bandwidth (EAB max ) value of 4.9 GHz at a thickness of 1.5 mm. In contrast, the EMW absorption performance of the samples SiC−V2150 and Si−C1500 was obviously poor, which was consistent with the RCS (Radar Cross−Section) simulation results. The formation of α−SiC p /α−SiC nw /SiO 2 /C composites (sample SiC−C1500) containing 4H−SiC/6H−SiC/SiO 2 /C multi-interfaces heterostructure α−SiC nanowires (α−SiC nw ) was analyzed. The excellent EMW absorption performance of SiC−C1500 sample could be attributed to the effective regulation of α polymorphs, nanowire heterostructure, multi−component hybridization. This study supplies a helpful experience and reference for improving the high temperature EMW absorption performance of SiC matrix composites.
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高影响因子
FOOD CHEMISTRY
·
2026
·
IF 10.4
Xiaofeng Min,Qingqing Yu,Yaxin Wen,Yaoming He,Jinglin Zhao,Xuetao Xu
α-Glucosidase inhibitory effects of three curcuminoids (Cur, DMC, and BDMC) were investigated. • The inhibition mechanism of three curcuminoids on α-glucosidase was evaluated. • The binding of three curcuminoids with α-glucosidase caused changes in enzyme conformation and microenvironment, leading to a decrease in enzyme activity. • Pre-treatment of three curcuminoids would reduce mice postprandial blood glucose. Turmeric curcuminoids displayed their potential in diabetes treatment, however, their inhibition mechanisms are still unclear. Thence, the inhibition effects and mechanisms of three curcuminoids, ie , curcumin (Cur), demethoxycurcumin (DMC), and bis-demethoxycurcumin (BDMC), against α-glucosidase were investigated. Results showed that BDMC (7.1 μM) and DMC (8.8 μM) presented stronger inhibitory activity than Cur (13.3 μM). Kinetic studies revealed BDMC and DMC both as reversible mixed-type inhibitors, differing from the competitive property of Cur. Multispectral results (SPR, fluorescence spectra, and CD spectra) clarified the binding of three curcuminoids with α-glucosidase caused the changes in enzyme conformation microenvironment to inhibit the activity. Molecular docking clarified the detailed binding interactions of three curcuminoids with α-glucosidase. Mice OTGG assay indicated their ability on reducing postprandial hyperglycemia. Therefore, above findings give the efficacy data support for the development and utilization of turmeric and curcuminoids as hypoglycemic function foods and health supplements. Download: Download high-res image (185KB) Download: Download full-size image
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Small
·
2021
·Vol. 18
·期 8
·2105599
·
IF 13.281
Wuhong Xue,Qitao Jiang,Fakun Wang,Ri He,Ruixue Pang,Huali Yang,Peng Wang,Ruilong Yang,Zhicheng Zhong,Tianyou Zhai,Xiaohong Xu
2D ferroelectrics with robust polar order in the atomic-scale thickness at room temperature are needed to miniaturize ferroelectric devices and tackle challenges imposed by traditional ferroelectrics. These materials usually have polar point group structure regarding as a prerequisite of ferroelectricity. Yet, to introduce polar structure into otherwise nonpolar 2D materials for producing ferroelectricity remains a challenge. Here, by combining first-principles calculations and experimental studies, it is reported that the native Ga vacancy-defects located in the asymmetrical sites in cubic defective semiconductor α‑Ga 2 Se 3 can induce polar structure. Meanwhile, the induced polarization can be switched in a moderate energy barrier. The switched polarization is observed in 2D α‑Ga 2 Se 3 nanoflakes of ≈4 nm with a high switching temperature up to 450 K. Such polarization switching could arise from the displacement of Ga vacancy between neighboring asymmetrical sites by applying an electric field. This work removes the point group limit for ferroelectricity, expanding the range of 2D ferroelectrics into the native defective semiconductors.
研究领域:
材料科学
·
凝聚态物理
·
纳米电子学
·
功能材料
·
半导体物理
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高影响因子
ACS Nano
·
2015
·
IF 12.881
Weiguang Xie,Mingze Su,Zebo Zheng,Yu Wang,Li Gong,Fangyan Xie,Weihong Zhang,Zhi Luo,Jianyi Luo,Pengyi Liu,Ningsheng Xu,Shaozhi Deng,Huanjun Chen,Jian Chen
The hydrogenation process of the layered α-MoO3 crystal was investigated on a nanoscale. At low hydrogen concentration, the hydrogenation can lead to formation of HxMoO3 without breaking the MoO3 atomic flat surface. For hydrogenation with high hydrogen concentration, hydrogen atoms accumulated along the <101> direction on the MoO3, which induced the formation of oxygen vacancy line defects. The injected hydrogen atoms acted as electron donors to increase electrical conductivity of the MoO3. Near-field optical measurements indicated that both of the HxMoO3 and oxygen vacancies were responsible for the coloration of the hydrogenated MoO3, with the latter contributing dominantly. On the other hand, diffusion of hydrogen atoms from the surface into the body of the MoO3 will encounter a surface diffusion energy barrier, which was for the first time measured to be around 80 meV. The energy barrier also sets an upper limit for the amount of hydrogen atoms that can be bound locally inside the MoO3via hydrogenation. We believe that our findings has provided a clear picture of the hydrogenation mechanisms in layered transition-metal oxides, which will be helpful for control of their optoelectronic properties via hydrogenation.
研究领域:
材料科学
·
纳米技术
·
凝聚态物理
·
光电子学
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高影响因子
PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS
·
2016
·
IF 0.723
Xing Wang,Yuan Cai,Jian Chen,Francis Verpoort
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