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ACS Chemical Neuroscience · 2021 · IF 4.418

Discovery of Resorcinol-Based Polycyclic Structures as Tyrosinase Inhibitors for Treatment of Parkinson’s Disease

Qi Li,Jun Mo,Baichen Xiong,Qinghong Liao,Ying Chen,Yuanyuan Wang,Shuaishuai Xing,Siyu He,Weiping Lyu,Ning Zhang,Haopeng Sun

Tyrosinase is involved in the synthesis of neuromelanin in the substantia nigra, which is closely correlated with the pathogenesis of Parkinson’s disease. Herein, we identified S05014 (l-Tyr, IC50 = 6.25 ± 1.43 nM; l-Dopa, IC50 = 0.64 ± 0.40 μM) as a highly effective tyrosinase inhibitor. It could inhibit the tyrosinase function from different origins and decrease the expression of tyrosinase. S05014 presented good medication safety and inhibited melanogenesis in a dose-dependent manner. Moreover, as a resorcinol derivative, S05014 could scavenge the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical and significantly reduce the overproduction of LPS-induced reactive oxidative species (ROS), indicating its antioxidative profile. S05014 exhibited an excellent neuroprotective effect against methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) impairment in vitro and could remarkably alleviate movement abnormalities and exploratory activities in vivo. Altogether, S05014 is considered as a promising inhibitor for tyrosinase, melanogenesis, and oxidative stress and has great potential to be utilized in anti-Parkinsonian syndrome. From this point of view, tyrosinase inhibition has been further confirmed to be a novel strategy to improve locomotor capacity and treat Parkinson’s disease.

研究领域: 神经科学 · 药理学 · 药物发现 · 生物化学
✓ 已验证 DOI PubMed 高影响因子
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MOLECULES · 2012 ·Vol. 17 ·期 12 ·14748-14764 · IF 2.386

Nitrogen-Containing Apigenin Analogs: Preparation and Biological Activity

Rui Liu,Bin Zhao,Dong-En Wang,Tianyu Yao,Long Pang,Qin Tu,Jian-Jun Liu,Jinyi Wang

A series of nitrogen-containing apigenin analogs4a–jwas synthesized via Mannich reactions to develop anticancer, antibacterial, and antioxidant agents from plant-derived flavonoids. The chemical structures of these compounds were confirmed using1H-NMR,13C-NMR, and ESI-MS. Thein vitrobiological activities of the analogs were evaluated via assays of their antiproliferative, antibacterial, and antioxidant activities. The prepared apigenin analogs exhibited different antiproliferative activities against four human cancer cell lines, namely human cervical (HeLa), human hepatocellular liver (HepG2), human lung (A549), and human breast (MCF-7) cancer cells. Compound4ishowed the most favorablein vitroantiproliferative activity with IC50values of 40, 40, 223, and 166 μg/mL against HeLa, HepG2, A549, and MCF-7, respectively. The 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity assay also showed that4ihad the most potent antioxidant activity, with the smallest IC50value (334.8 μg/mL). The antibacterial activities of the analogs were determined using a two-fold serial dilution technique against four pathogenic bacteria, namelyStaphylococcus aureus,Bacillus subtilis,Escherichia coli, andPseudomonas aeruginosa. All the prepared apigenin analogs exhibited more potent activities than the parent apigenin. Compounds4hand4j, in particular, exhibited the best inhibitory activities against the Gram-positive bacteriaStaphylococcus aureusandBacillus subtiliswith MIC values of 3.91 and 1.95 μg/mL, respectively.Keywords:apigenin analogs;antiproliferative activity;antibacterial activity;antioxidant activity

CAS / MDL: 50-81-7
研究领域: 药理学 · 化学 · 肿瘤学 · 微生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Food Science and Human Wellness · 2023 · IF 7

Antarctic krill antioxidant peptides show inferior IgE-binding ability and RBL-2H3 cell degranulation

Jie Ding,Chunyan Zhu,Pengfei Jiang,Libo Qi,Na Sun,Songyi Lin

Enzymatic hydrolysis, isolation, and purification might make a great deal of difference in antioxidant activity and antigenicity of peptide components. This study aimed to isolate and purify antioxidant peptide components from Antarctic krill and evaluate their allergenicity of them. Electron paramagnetic resonance (EPR) spectroscopy results indicated 3 10 kDa Antarctic krill hydrolysates (AKHs) had higher DPPH and · OH radical scavenging rates. And the second component (N2-2) purified 3 10 kDa hydrolysate showed better ability to scavenge DPPH and · OH radicals ( P < 0.05), which were (47.43 ± 2.18)% and (34.33 ± 1.25)%, respectively. Additionally, indirect-ELISA results revealed that N2-1 had a weaker ability to bind specific IgE and that N2-2 had a lower binding capability to specific IgG1 ( P < 0.05). And N2-2 had a higher EC 50 value of (5.29 ± 0.95) ng/mL ( P < 0.05) in cell degranulation assay, which was about 13.80 times that of Antarctic krill. Therefore, N2-2 might be the potential source of the antioxidant peptides with lower allergenicity.

CAS / MDL: 3317-61-1
研究领域: 食品科学 · 生物化学 · 免疫学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Regulatory effects of different spacer alkyl chains on the in vitro antioxidant and antibacterial activities of chitosan quaternary ammonium/phosphonium salt derivatives

Zhongwen Su,Yonggang Peng,Ying Yu,Yujing Zhong,Junyue Zeng,Yikai Chen,Sekar Vijayakumar,Yangfan Mao,Lin Wang,Meihua Xin,Mingchun Li

In this study, three chitosan quaternary phosphonium salts and three chitosan quaternary ammonium salts with varying spacer chain lengths were synthesized. Structure characterization of the obtained products was conducted using Fourier-transform infrared spectroscopy, nuclear magnetic resonance, thermogravimetric analysis, and elemental analysis. Additionally, the in vitro scavenging efficiency of these derivatives against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide radicals, as well as their antibacterial activities against Escherichia coli ( E. coli ) and Staphylococcus aureus ( S. aureus ), were evaluated. The results indicated that the scavenging efficiency of the chitosan quaternary phosphonium salt at a concentration of 1.6 mg/mL ranged from 36.9 % to 48.7 % for DPPH free radicals and from 48.3 % to 66.3 % for superoxide free radicals, outperforming that of the chitosan quaternary ammonium salt with long alkyl chains. Furthermore, an increase in the length of the spacer alkyl chain was associated with enhanced antibacterial activities of the corresponding chitosan derivatives. At a concentration of 1.0 mg/mL, the synthesized chitosan derivatives demonstrated antibacterial rates exceeding 90 % against both E. coli and S. aureus . Notably, the CCK-8 assay confirmed that these derivatives are non-toxic to 293 T cells. Among the six derivatives, TPPBOC and DMDOC, characterized by longer spacer alkyl chains, demonstrated superior antioxidant and antibacterial activities. This research establishes a robust theoretical foundation for the development of more effective and safer antioxidants and antibacterial agents, thereby enriching the knowledge base in chitosan chemistry and functional materials, and paving new pathways for the innovation of novel antioxidant and antibacterial materials.

研究领域: 生物化学 · 材料科学 · 药学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Journal of Aquatic Food Product Technology · 2017 · IF 0.478

Kinetics of Antioxidant-Producing Maillard Reaction in the Mixture of Ribose and Sea Cucumber (Stichopus japonicus) Gut Hydrolysates

Jia-Run Han,Zhi-Mo Zhu,Hai-Tao Wu,Na Sun,Yue Tang,Cui-Ping Yu,Chen-Chen Zhao,Zheng-Yu Zhang,Ao-Ting Li,Jia-Nan Yan

Maillard reaction products (MRPs) were produced in sea cucumber gut hydrolysates (SCGHs)-ribose system at 75°C, 85°C, and 95°C with a pH value of 7.0 or 8.0 for 12 hour. The parameters of amount of intermediate products, fluorescence intensity, browning development, and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging ability showed a positive correlation with each other in SCGHs-ribose system. The amount of intermediate products, fluorescence intensity, and browning development followed the zero-order kinetic with activation energy from 62 to 91 kJ/mol in the Maillard reaction of SCGHs-ribose system. Moreover, 2-methyl-butanal has positive and significant correlation with DPPH radical scavenging ability of SCGHs-ribose MRPs. These results suggest that Maillard reaction improves the antioxidant activity of SCGHs, which contributes to the generation of intermediate, fluorescent, browning, and volatile products of SCGHs-ribose system.

CAS / MDL: 108-94-1
研究领域: 食品化学 · 营养科学 · 生物化学
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Food Bioscience · 2023 · IF 5.2

Probiotic properties of Lactobacillus paraplantarum LS-5 and its effect on antioxidant activity of fermented sauerkraut

Hongchi Zhou,Sixuan Wang,Weichao Liu,Lixuan Chang,Xuemei Zhu,Guangqing Mu,Fang Qian

This study aimed to investigate the safety and probiotic properties of Lactobacillus paraplantarum LS-5 isolated from traditional northeastern sauerkraut , and to assess the antioxidant capacity of different solvent extracts (ethanol, water, and hot water) of L. paraplantarum LS-5-inoculated sauerkraut. L. paraplantarum LS-5 was shown to have various probiotic characteristics, such as good survival ability under artificial gastrointestinal conditions, antagonistic activity of various pathogens, non-biogenic amines, antibiotic susceptibility , and non-hemolytic. The 2,2′-azino-bis-3-ethylbenzothiazoline-6-sulfonate (ABTS) radical scavenging activity of the L. paraplantarum LS-5-inoculated sauerkraut alcohol extract (71.13%) was significantly higher than water extract (59.59%) ( p  < 0.05). The ferric reducing antioxidant power (FRAP) of sauerkraut alcohol extract (614.93 Trolox μmol L −1 ) exhibited a slightly stronger ability compared to water extract (388.53 Trolox μmol L −1 ) and the heated sauerkraut water extract (383.20 Trolox μmol L −1 ) at extract concentrations of 5.0 mg mL −1 . Its 1, 1-diphenyl1-2-picrylhydrazyl (DPPH) radical scavenging activity was also stronger. It was found by principal component analysis (PCA) and Pearson that the DPPH radical-scavenging activities of sauerkraut extracts were significantly correlated with the content of polyphenols and flavonoids ( p  < 0.05). Unlike kimchi , Northeastern sauerkraut is consumed mainly by heating, so this study could contribute to understanding the antioxidant capacity of different solvent extracts of sauerkraut, and before and after heating water extracts.

研究领域: 微生物学 · 食品科学 · 营养学 · 生物化学
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JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE · 2024 · IF 3.3

Anti-oxidant activity of 1-(1H-imidazo[4,5-c]pyridin-4-yl)ethenone, a Maillard reaction product derived from fructose and histidine

Kangyu Zhao,Xin Long,Junle Li,Ying Wang,Ping Lan,Yong Wang

BACKGROUND The Maillard reaction involves the interaction of various amino acids and reducing sugars, resulting in food browning. It often produces appealing aromas and flavors. The complexities of the reaction are such that it can be challenging to identify the often numerous and frequently volatile products formed by it. In the present study, we sought to identify and evaluate an unusual product with anti-oxidant activity arising from a fructose-histidine Maillard reaction model. The anti-oxidant profile of this product was assessed by computational means. RESULTS The fructose-histidine Maillard reaction products (FH-MRPs) were generated by heating a 2:1 mixture of the sugar and the amino acid at 140 °C for 2 h. Chromatographically separable fractions, labelled DM-1 to DM-8, were obtained using silica gel as the stationary phase and dichloromethane/methanol (DCM/MeOH) mixtures as the mobile one. Fraction DM-5 exhibited the highest 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, and further bio-assay guided fractionation led to isolation and identification of 1-(1 H -imidazo[4,5- c ]pyridin-4-yl)ethenone (IMPE) as the active principal, the structure of which was established by nuclear magnetic resonance (NMR) spectroscopic and mass spectral techniques. A mechanism for the formation of IMPE from its precursors is proposed. Density functional theory (DFT) calculations suggest this novel heterocyclic compound exerts its anti-oxidant effects by interacting with DPPH and 2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals. Essentially, IMPE was non-toxic below 300 ug mL −1 , showing a concentration-dependent free radical clearance capacity and reducing power within the 100–1000 μg mL −1 range, and moreover, exhibiting significant Fe 2+ chelating abilities wihin the 50-200 μg mL −1 range. CONCLUSION This study identified the unique FH-MRP, IMPE, and found that it acts as food antioxidant through the chelation of metal ions. © 2024 Society of Chemical Industry.

研究领域: 食品化学 · 分析化学 · 计算化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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LWT-FOOD SCIENCE AND TECHNOLOGY · 2022 · IF 6.056

Purification and identification of antioxidant peptides from millet gliadin treated with high hydrostatic pressure

Yidan Zhang,Xu Jing,Zhenjia Chen,Xiaowen Wang

In this paper, the preparation, purification, and identification of the antioxidant peptides of millet gliadin after high hydrostatic pressure (HHP) treatment were studied to broaden the utilization range of millet and provide certain theoretical basis for its further processing and utilization. Millet gliadin treated with 300 MPa was enzymatically hydrolyzed by pepsin, and the optimal hydrolysis time was determined to be 50 min by in-vitro antioxidant activity evaluation method [1,1-diphenyl-2-trinitrophenylhydrazine (DPPH) free radical, hydroxyl radical, and superoxide anion scavenging activity]. The enzymatic hydrolysate was separated and purified by gel filtration and RP-HPLC, and the fraction with the strongest antioxidant activity (S4) was obtained. The scavenging ability of DPPH, •OH, and O 2 − were 53.96% ± 0.86%, 31.30% ± 0.90%, and 52.73% ± 0.99%, respectively. However, it still had lower antioxidant capacity compared with VC. Seven peptide sequences, namely, SLSHLTVQ, SLAHVTVQ, LHALTLQ, SGILAPSPVL, SHLTVQ, VSAAAA, and SPAAF, were identified from S4. The presence of certain amino acids, such as Glycine, Leucine, Phenylalanine, and Proline , is considered to induce high antioxidant activity against lipid peroxidation. Therefore, the antioxidant peptide extracted from millet gliadin after HHP treatment may be used as a natural antioxidant component in functional food.

研究领域: 食品科学 · 生物化学 · 农业加工
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CARBOHYDRATE POLYMERS · 2019 · IF 6.044

Structural characterization and antioxidant activity of polysaccharide from four auriculariales

Yue Su,Liang Li

The structural characterization and antioxidant activity of four Auricularia polysaccharides (A.cornea ACP)、A.auricula(AAP)、A.polytricha (APP) and M.fungus(MFP)) were studied in this paper. The results shown: polysaccharides of four Auricularia were mainly composed of mannose and galactose, all polysaccharides contained uronic acid and pyran ring structure with spectroscopy and NMR analysis. There was a significant difference in the total antioxidant capacity and APP was significantly higher than the other polysaccharides. The ability of APP to scavenge DPPH radicals and hydroxyl radicals was significantly higher than that of other polysaccharides, respectively. The molecular weight was significantly positively correlated with DPPH radicals, superoxide anion radicals and hydroxyl radicals. Total antioxidant capacity was significantly negatively correlated with fucose and galactose. The result indicated that fucose and galactose jointly determine total antioxidant capacity. The polysaccharide from four Auricularia had good oxidation resistance and could be used as natural antioxidants.

研究领域: 生物化学 · 食品科学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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LWT-FOOD SCIENCE AND TECHNOLOGY · 2015 · IF 2.416

Hydrolysis of rapeseed meal protein under simulated duodenum digestion: Kinetic modeling and antioxidant activity

Cunshan Zhou,Xiaojie Yu,Xiaopei Qin,Haile Ma,Abu ElGasim A. Yagoub,Jiali Hu

Kinetics modelling, DPPH radical scavenging activity and reducing power of rapeseed meal protein were investigated under simulated duodenum digestion. Kinetics of the reaction was considered in relation to initial substrate concentration, initial enzyme concentration, and hydrolysis time. Optimum hydrolysis conditions were trypsin concentration of 10 g/L, substrate concentration of 4 g/L, time of 40 min and temperature of 37 °C. From the results a general kinetic enzymolysis equation was suggested, providing a rational theoretical basis for determining the parameters of the reaction. The highest antioxidant activity was in accordance with the optimum reaction conditions. Antioxidant free amino acids increased after hydrolysis. Antioxidant oligopeptides of molecular weights of 2608, 1695 and 211 Da were identified. At a concentration of 2 mg/mL, the peptide fraction of CS-F 2 -CC 2 ; with molecular weight of 1000–1500 Da; showed the highest DPPH radical scavenging activity and reducing power, accounting for 70.32% and 0.538, respectively. The trypsin-hydrolysate displayed a potential capacity to scavenge free radicals and binding irons after duodenal digestion, appearing as promising ingredient to formulate functional foods with antioxidant activity.

CAS / MDL: 1898-66-4
研究领域: 食品科学 · 生物化学 · 营养学
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FITOTERAPIA · 2023 · IF 3.4

Basic characterization, antioxidant and immunomodulatory activities of polysaccharides from sea buckthorn leaves

Yang Liu,Limei Ran,Yahong Wang,Peng Wan,Hongli Zhou

The polysaccharides from Sea buckthorn leaves (SBLPs) were extracted by hot water and purified by DEAE cellulose , then separated into six polysaccharides (SBLP-S) by DEAE-52 column. Six separated polysaccharides were characterized by Ultraviolet Spectroscopy, Infrared Spectrum, High Performance Liquid Chromatographic and Congo red analysis. The antioxidant activity and immunological activity were investigated in vitro . The results revealed that the monosaccharide composition of SBLP-S-1, SBLP-S-2, SBLP-S-3, SBLP-S-5 and SBLP-S-6 contained Man , GlcN , Rib , Rha , GluA , GalA , Glu, Gal, Xyl , Ara and Fuc , among them, rare glucosamine was found. And SBLP-S-4 contained all above components except GlcN and GluA. FT-IR showed that SBLP-S were sulfated polysaccharide containing uronic acid . Molecular weights of SBLP-S were 338.659, 401.305, 599.849, 393.904, 626.895 and 176.862 kDa. The Congo-red test indicated that SBLP-S-2, SBLP-S-4, SBLP-S-5, and SBLP-S-6 had triple helix conformation. Crude polysaccharides had the strong scavenging activities on DPPH radicals, ABTS radicals and hydroxyl radicals . The six polysaccharides had the activity of immune stimulation on RAW264.7 cell. SBLP-S-2 promoted the phagocytosis best and SBLP-S-6 promoted the NO production best. The results suggested that SBLPs could be used as potential antioxidants and immunomodulatory agents in pharmaceutical and functional food fields.

研究领域: 药理学 · 食品科学 · 生物化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2011 · IF 2.502

Chemical compositions and bioactivities of crude polysaccharides from tea leaves beyond their useful date

Jianbo Xiao,Jianglei Huo,Huixian Jiang,Fan Yang

The chemical compositions and bioactivities of crude tea polysaccharides (TPS) from the out-of-date tea leaves (beyond their useful date), namely Xihu Longjing (XTPS), Anxi Tieguanyin (TTPS), Chawentianxia (CTPS) and Huizhoulvcha (HTPS), in market were investigated. These TPS showed similar neutral sugar content and different distribution of molecular weight (1–800   kD). These crude TPS were mainly composed of rhamnose, arabinose, galactose, glucose, xylose, mannose, and galacturonic acid. IR spectra confirmed that these crude TPS were composed of polysaccharide, protein and uronic acids. These TPS showed similar DPPH scavenging activity and exhibited lower DPPH scavenging activities than Vc within 25–200   μg/mL. However, these TPS with higher concentrations (200–400   μg/mL) showed similar DPPH scavenging activity with Vc. HTPS exhibited significant higher superoxide anion scavenging activity than others TPS and gallic acid. XTPS showed significant higher inhibitory effects on α-glucosidase and α-amylase with inhibitory percentages of 64.35% and 82.24% than others TPS. TTPS, XTPS, and HTPS exhibited similar inhibition ability on α- d -glucosidase and α-amylase. The overdue tea leaves can be a resource of tea polysaccharides as function food.

研究领域: 食品科学 · 营养学 · 药理学 · 农业化学
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