JOURNAL OF ELECTROANALYTICAL CHEMISTRY
·
2018
·
IF 3.235
Jing Bao,Xintong Geng,Changjun Hou,Yanan Zhao,Danqun Huo,You Wang,Zhaonan Wang,Yan Zeng,Mei Yang,Huanbao Fa
Many studies have confirmed that DNA methylation is highly correlated with the occurrence and development of various diseases including cancers. In this work, we developed a simple, sensitive, selective, and universal electrochemical biosensor for detection of DNA methylation and assay of DNA methyltransferase (MTase) activity using M.SssI MTase as an example. The thiolated single-stranded DNA S1 was self-assembled on the surface of gold nanoparticles deposition modified glassy carbon electrode via Au S bonding, then hybridization between the DNA S1 and its complementary DNA S2 formed a double-stranded target sequence for both M.SssI MTase and restriction endonuclease Hpa II. HpaII could not cleave the target sequence after it was methylated by M.SssI MTase, while the sequence without methylation could be cleaved. Here, we used methylene blue (MB) as electrochemical indicator. The electrochemical signal of MB increased linearly with increasing M.SssI MTase concentration from 0.5 to 25 U/mL and from 25 to 400 U/mL with a detection limit of 0.04 U/mL. Moreover, screening of M.SssI MTase inhibitors 5-azacytidine (5-Aza) and 5-Aza-2′-deoxycytidine (5-Aza-dC) were successfully investigated using the fabricated electrochemical biosensor and showed that the two classic drugs could both inhibit the M.SssI MTase activity with the IC 50 of 2.8 μM and 0.37 μM, respectively, indicating potential application in discovery of new anticancer drugs.
研究领域:
生物化学
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分子生物学
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分析化学
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癌症研究
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DOI
高影响因子
ChemistryOpen
·
2024
·
IF 2.5
Yuanyong Yao,Tao Wu,Meng Zhang,Daihua Fu,Hai Yang,Shixue Chen
Graphical The test method for assaying inhibitory effects of bioflavonoids on xanhine oxidase in vitro has been improved successfully with the equipment of UV-Vis technique. In the improved test method, there is a micro-environment surrounding XOD has been created in the presence of •O 2 - , which is similar to that of in vivo . Simultaneously, the inhibition of dihydromyricetin as a chiral flavonoid was effectively assayed by the improved test method, indicating dihydromyricetin enabling to be a potent inhibitor of XOD, resulting from the selective transformation of DMY to MY occurred. The difference on inhibitory effects of bioflavonoids inhibiting XOD activity assayed by varying test methods cause of us to be further in consideration. The reported test method creating a micro-environment surrounding XOD in the absence of ⋅O 2 − , which is seemly different from the assay in vivo . So, the vitro test method for assaying XOD activity is necessary to be improved for selection of potential inhibitors in the presence of ⋅O 2 − . The inhibitory results demonstrated that bioflavonoids of MY, DMY, QUE and LUT are capable to be on effective IC 50 values, but others are not. As well, their resulting inhibitions determined by the improved test method are much less than that reported in the literature, indicating that their chemical affinities with XOD become weaker. Moreover, DMY assayed on the inhibitions of XOD in the improved test method performs to be a better inhibitor, as compared to the assay of the reported test methods. Abasing on the transformation of DMY into MY in the presence of ⋅O 2 − , the good inhibition of DMY on XOD activity can be explained by the synergistic effect of MY.
研究领域:
生物化学
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药理学
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分析化学
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DOI
PubMed
高影响因子
ANALYTICAL AND BIOANALYTICAL CHEMISTRY
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2021
·Vol. 413
·期 9
·2553-2563
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IF 4.157
Li Cong,Zi Yuqiu,Xu Dawei,Jiang Dafeng,Qu Fei,Zhao Xian-En
Herein, the self-assembly of 1-dodecanethiol-capped Cu nanoclusters (DT-Cu NCs) is obtained by annealing of dibenzyl ether solution of nanoclusters. These aggregates are composed of small clusters and emit a high level of aggregation-induced emission (AIE) in water. Based on the quenching effect of 4-nitrophenol (4-NP) on DT-Cu NCs, a fluorescence strategy is developed to monitor α-glucosidase (α-Glu) activity and screen its inhibitors from Chinese herbal medicines. 4-Nitrophenyl-α-D-glucopyranoside (NGP) is selected as the substrate, which is further hydrolyzed to yield 4-NP through the catalysis of α-Glu. The quenching efficiency is positively correlated to the concentration of α-Glu. Furthermore, the inhibitory effects of the extracts from four Chinese herbal medicines (i.e., the rind of Punica granatum L., Momordica grosvenorii Swingle., Crataegus pinnatifida Bge., and Lycium barbarum L.) on the α-Glu activity have been studied. The IC 50 values of extracts from the rind of Punica granatum L. and Momordica grosvenorii Swingle are 0.23 and 0.37 g/L, respectively, so they show obvious inhibitory effects on α-Glu. The extracts of Crataegus pinnatifida Bge. and Lycium barbarum L. exhibit relatively weak inhibitory effects. Hence, the proposed strategy can be applicable for screening α-Glu inhibitors from Chinese herbal medicines. Last but not the least, by immobilizing DT-Cu NCs into agarose hydrogels in polyethylene tubes, a visual device is fabricated to screen α-Glu inhibitors with high throughput and sensitivity. Graphical abstract
研究领域:
纳米技术
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生物技术
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药学
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分析化学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2018
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IF 3.909
Mengting Wang,Jinyuan Shi,Lei Wang,Yaqin Hu,Xingqian Ye,Donghong Liu,Jianchu Chen
In this study, lotus leaf flavonoids (LLF) were found to show a notable inhibition activity on α-amylase in a mixed-type manner with IC 50 value of (5.58 ± 0.10) mg/mL. The intrinsic fluorescence of α-amylase was quenched by the interaction with LLF through a static quenching mechanism, and LLF-α-amylase complex was spontaneously formed mainly driven by the hydrophobic interaction and hydrogen bonding. Multispectroscopic analyses (synchronous fluorescence, three-dimensional fluorescence, circular dichroism (CD) and fourier transform infrared spectra (FT-IR)) comprehensively demonstrated that the binding of LLF to α-amylase would change the conformation and microenvironment of α-amylase, resulting in inhibiting the enzyme activity. The present study indicated that LLF had potential to be as an ingredient in functional food for the prevention of type-2 diabetes.
研究领域:
生物化学
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药理学
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食品科学
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糖尿病研究
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产品关联
DOI
PubMed
高影响因子
LUMINESCENCE
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2021
·Vol. 36
·期 7
·1767-1774
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IF 2.464
Bing Jie Jia,Min Lin,Jian Ping Wang,Ning Peng Wu
In this study, nitrobenzene was used as dummy template to synthesize a type of specific molecularly imprinted microspheres for chloramphenicol, and 4-nitroaniline was coupled with three fluorophores to synthesize three fluorescent tracers. Then a competitive fluorescence method was developed on a conventional microplate for detection of chloramphenicol in chicken and pork samples. This method contained only one sample-loading step, so one assay was finished within 30 min. The IC 50 was 1.8 ng/ml, and the limit of detection was 0.06 ng/g. The recoveries from chloramphenicol-fortified blank meat samples were in the range 67.5–96.2%. Furthermore, this method could be recycled three times. The detection results for some real meat samples were identical to that of a LC–MS/MS method. Therefore, this method could be used as a practical tool for routine screening for the residue of chloramphenicol in large number of meat samples.
研究领域:
分析化学
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食品科学
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生物技术
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产品关联
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
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2021
·
IF 9.229
Fan Zhang,Angelina Angelova,Vasil M. Garamus,Borislav Angelov,Shuyang Tu,Liangliang Kong,Xinlei Zhang,Na Li,Aihua Zou
Targeted therapies of melanoma are of urgent need considering the resistance of this aggressive type of cancer to chemotherapeutics. The voltage-dependent anion channel 1 (VDAC1)–hexokinase-II (HK-II) complex is an emerging target for novel anticancer therapies based on induced mitochondria-mediated apoptosis. The low cell membrane permeability of the anticancer 12-mer peptide N-Ter (RDVFTKGYGFGL) derived from the N-terminal fragment of the VDAC1 protein impedes the intracellular targeting. Here, novel multiblock VDAC1-derived cationic amphiphilic peptides (referred to as Pal-N-Ter-TAT, pFL-N-Ter-TAT, and Pal-pFL-N-Ter-TAT) are designed with a self-assembly propensity and cell-penetrating properties. The created multiblock amphiphilic peptides of partial α-helical conformations form nanoparticles of ellipsoid-like shapes and are characterized by enhanced cellular uptake. The amphiphilic peptides can target mitochondria and dissociate the VDAC1–HK-II complex at the outer mitochondrial membrane, which result in mitochondria-mediated apoptosis. The latter is associated with decrease of the mitochondrial membrane potential, cytochrome c release, and changes of the expression levels of the apoptotic proteins in A375 melanoma cells. Importantly, the mitochondrial VDAC1-derived amphiphilic peptides have a comparable IC50 value for melanoma cells to a small-molecule drug, sorafenib, which has been previously used in clinical trials for melanoma. These results demonstrate the potential of the designed peptide constructs for efficient melanoma inhibition.
研究领域:
肿瘤学
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药学
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生物技术
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分子生物学
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纳米技术
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产品关联
DOI
PubMed
高影响因子
BIOORGANIC & MEDICINAL CHEMISTRY
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2009
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IF 3.075
Wen-Jun Mao,Peng-Cheng Lv,Lei Shi,Huan-Qiu Li,Hai-Liang Zhu
Fourteen metronidazole derivatives (compounds 3a – f and 4b – h ) have been synthesized by coupling of metronidazole and salicylic acid derivatives. All of them are reported for the first time. Their chemical structures are characterized by 1 H NMR, MS, and elemental analysis. The inhibitory activities against Helicobacter pylori urease have been investigated in vitro and many compounds have showed promising potential inhibitory activities of H. pylori urease. The effect of compounds 4b (IC 50 = 26 μM) and 4g (IC 50 = 12 μM) was comparable with that of acetohydroxamic acid, a well known H. pylori urease inhibitor used as a positive control. The experimental values of IC 50 showed that inhibitor was potent urease inhibitor. A docking analysis using the autodock 4.0 program could explain the inhibitory activities of compound 4g against H. pylori urease.
研究领域:
药物化学
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药理学
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微生物学
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生物化学
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产品关联
DOI
PubMed
高影响因子
LUMINESCENCE
·
2015
·Vol. 31
·期 1
·96-101
·
IF 1.518
Si-Yao Liu,Huan Wang,Tian He,Liang Qi,Zhi-Qi Zhang
A fluorescence method was established for a α-glucosidase activity assay and inhibitor screening based on β-cyclodextrin-coated quantum dots. p -Nitrophenol, the hydrolysis product of the α-glucosidase reaction, could quench the fluorescence of β-cyclodextrin-coated quantum dots via an electron transfer process, leading to fluorescence turn-off, whereas the fluorescence of the system turned on in the presence of α-glucosidase inhibitors. Taking advantage of the excellent properties of quantum dots, this method provided a very simple, rapid and sensitive screening method for α-glucosidase inhibitors. Two α-glucosidase inhibitors, 2,4,6-tribromophenol and acarbose, were used to evaluate the feasibility of this screening model, and IC 50 values of 24 μM and 0.55 mM were obtained respectively, which were lower than those previously reported. The method may have potential application in screening α-glucosidase inhibitors. Copyright © 2015 John Wiley & Sons, Ltd.
研究领域:
生物化学
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分子生物学
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分析化学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2013
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IF 2.906
Ping Lu,Song Yang,Deyu Hu,Xiaoyan Ding,Mengmeng Shi
An indirect competitive enzyme-linked immunosorbent assay (ic-ELISA) was developed for the quantitative detection of the antiviral agent against tobacco mosaic virus (TMV). Hapten 6-[2-((methyllbenzothiazol-2-yl)-1-(2-ethoxy)-O, O-diethyl-α-aminophosphonate)acetamido)] hexanoic acid (DHS) was prepared from commercial chemicals and incorporated into the spacer arm through a carbon–carbon single bond. The prepared hapten was then coupled to carrier proteins keyhole limpet hemocyanin (KLH) to be used as an immunogen for monoclonal antibody (mAb) production together with ELISA development. This assay was further optimized by the assessment of the dependence of assay parameters on organic solvents, pH, and ionic strength. The IC50 values of the optimized assay for Dufulin and the calculated limit of detection in phosphate-buffered saline (PBS) were 9.6 ± 0.59 and 0.3 ± 0.05 ng/mL, respectively. Using the optimized assays Dufulin residues in soil and tobacco samples were determined with recovery values ranging from 81.5 to 95.3%, intra-assay variation ranging from 2.88 to 6.10%, and interassay variation ranging from 6.11 to 9.42%.
研究领域:
农业化学
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分析化学
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植物病理学
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免疫学
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产品关联
DOI
PubMed
高影响因子
BIOORGANIC & MEDICINAL CHEMISTRY
·
2024
·
IF 3.3
Yanhong Niu,Zhili Wu,Qianfang Hu,Yuchen Wu,Qihua Jiang,Xiaolan Yang
Acetohydroxy acid synthase (AHAS) is a key enzyme that catalyzes the synthesis of branched-chain amino acids, which is indispensable for the survival and growth of Mycobacterium tuberculosis ( Mtb ). Aim to discover new AHAS inhibitors from natural products, here we performed computer assistant target-based screening for Mtb- AHAS inhibitors using Discovery Studio on TCMSP and SELLECK libraries. Mtb -AHAS structure was first simulated and verified for docking, and 80 compounds with top LIBDOCK and CDDOCK scores were obtained. By experimental verification, four compounds namely Salvianolic acid A, Embelin, Celastrol and Wushanicaritin showed inhibition potency against Mtb- AHAS with IC50 ranging from 805.5 nM–32.36 μM. The most potential inhibitor Celastrol exhibited bacteriostatic activity for both Mycobacterium smegmatis and Mycobacterium tuberculosis with MIC of 62.5 μM and 80 μM, respectively. This study revealed that Celastrol is the potential Mtb- AHAS inhibitor as an anti-tuberculosis lead compound.
研究领域:
药理学
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微生物学
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药物发现
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计算生物学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY B-BIOLOGY
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2024
·
IF 3.9
Linrong Shi,Mingzhi Zhu,Ruimin Long,Shibin Wang,Pei Wang,Yuangang Liu
In recent years, there has been growing interest in size-transformable nanoplatforms that exhibit active responses to acidic microenvironments, presenting promising prospects in the field of nanomedicine for tumor therapy. However, the design and fabrication of such size-adjustable nanotherapeutics pose significant challenges compared to size-fixed nanocomposites, primarily due to their distinct pH-responsive requirements. In this study, we developed pH-activated-aggregating nanosystems to integrate chemotherapy and photothermal therapy by creating size-transformable nanoparticles based on Prussian blue nanoparticles (PB NPs) anchored with acid-responsive polyoxometalates (POMs) quantum dots via electrostatic interactions (PPP NPs). Subsequently, we utilized doxorubicin (DOX) as a representative drug to formulate PPPD NPs. Notably, PPPD NPs exhibited a significant response to acidic conditions, resulting in changes in surface charge and rapid aggregation of PPP NPs. Furthermore, the aggregated PPP NPs demonstrated excellent photothermal properties under near-infrared laser irradiation. Importantly, PPPD NPs prolonged their retention time in tumor cells via a size-transformation approach. In vitro cellular assays revealed that the anticancer efficacy of PPPD NPs was significantly enhanced. The IC50 values for the PPPD NPs groupand the PPPD NPs + NIR group were 50.11 μg/mL and 30.9 μg/mL. Overall, this study introduces a novel strategy for cancer therapy, by developing size-aggregating nano-drugs with stimuli-responsive properties, holding promise for improved therapeutic outcomes in future combination approaches involving photothermal therapy and chemotherapy.
研究领域:
纳米医学
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癌症治疗
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材料科学
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
Algal Research-Biomass Biofuels and Bioproducts
·
2019
·
IF 3.723
Jiao Yang,Chang Liu,Hengjiang Cai,Dongyu Gu,Zhenni Ji,Xinfeng Guo,Jing Tian,Jing Meng,Yi Yang
Sargassum fusiforme is an edible alga that possesses a number of bioactivities , such as antidiabetic effects. In the present study, the n -hexane extract of S. fusiforme showed inhibitory activity against α-amylase. To interpret the α-amylase inhibitory activity of this extract, a method based on GC–MS and molecular docking was established. A total of 25 compounds were identified using GC–MS and then individually docked with α-amylase to simulate interactions between the latter and the ligands. Among the compounds determined, phenol, 2,2′-methylenebis[6-(1,1-dimethylethyl)-4-methyl- (PMDM) was completely enfolded in the active site of α-amylase via hydrophilic and electrostatic interactions, van der Waals forces, hydrogen bonds and π-π stacking interactions and showed the lowest binding energy (−6.25 kcal/mol). The activity of PMDM against α-amylase was further tested and verified in vitro, and its IC 50 was found to be 79.96 ± 0.34 μM. Thus, this compound is responsible for the α-amylase inhibitory activity of the n-hexane extract of S. fusiforme .
研究领域:
药理学
·
生物化学
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海洋生物学
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分析化学
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产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）