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INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES · 2016 ·Vol. 17 ·期 5 ·788 · IF 3.257

Extraction Optimization, Preliminary Characterization and Bioactivities in Vitro of Ligularia hodgsonii Polysaccharides

Xueping Song,Jun Tang

The optimization extraction, preliminary characterization and bioactivities ofLigularia hodgsoniipolysaccharides were investigated. Based on single-factor experiments and orthogonal array test, the optimum extraction conditions were obtained as follows: extraction time 3 h, temperature 85 °C, water/raw material ratio 36. Further Sevag deproteinization and dialysis yielded the dialyzedLigularia hodgsoniipolysaccharides (DLHP, 19.2 ± 1.4 mg/g crude herb). Compositional analysis, size-exclusion chromatography connected with multi-angle laser light-scattering and refractive index (SEC-MALLS-RI), Fourier transform infrared (FT-IR) and1H nuclear magnetic resonance (NMR) spectroscopy were employed for characterization of the polysaccharides. DLHP was found to have a major component with a weight-average molecular weight of 1.17 × 105Da, mainly comprising of glucose, galactose, arabinose, mannose, rhamnose, glucuronic acid and galacturonic acid. Byin vitroantioxidant activity assays, DLHP presented remarkable scavenging capacities towards 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and hydroxyl radicals, and ferrous ions chelating ability. Moreover, it exhibited appreciable anti-hyperglycemic activity as demonstrated by differential inhibition of α-glucosidase and α-amylase. The results indicated that DLHP could potentially be a resource for antioxidant and hypoglycemic agents.Keywords:Ligularia hodgsoniiHook.;polysaccharides;extraction optimization;characterization;antioxidant activity;anti-hyperglycemic activity

研究领域: 植物化学 · 药理学
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INDUSTRIAL CROPS AND PRODUCTS · 2017 · IF 3.181

Antioxidant/antihyperglycemic activity of phenolics from sugarcane (Saccharum officinarum L.) bagasse and identification by UHPLC-HR-TOFMS

Rui Zheng,Shan Su,Huifang Zhou,Huaifeng Yan,Junhua Ye,Zhengang Zhao,Lijun You,Xiong Fu

Sugarcane bagasse, one of the most abundant agro-food by-products, is a very promising raw material available at low cost for recovering bioactive substances. In this study, the total phenolic content was measured by Folin-Ciocalteu method and the antioxidant activity of the extracts was determined by DPPH , ABTS + and ROO (ORAC) methods. The results indicated that 30% hydroalcoholic fraction (30%E) had the highest total phenolic content (170.68   ±   3.25   mg GAE/g DW) among the hydroalcoholic extracts and was the most active fraction in antioxidant activity. Besides, intestinal α-glucosidase inhibitory activity was conducted to assess the antihyperglycemic ability of the extracts and 30%E showed a significant effect at 10   mg/mL (82.64% inhibition of sucrase and 74.26% inhibition of maltase, respectively). Glucose uptake assay based on HepG2 cells was used to evaluate the glucose uptake effect of 30%E. Five phenolic compounds (tricin 4- O -guaiacylglyceryl ether-7- O -glucopyranoside, genistin, p -coumaric acid, quercetin and genistein) were identified in 30%E using UHPLC-HR-TOFMS. Taken together, the data indicated that sugarcane bagasse can be used as a potential source of bio-active phenolics and may play a role in functional agents exploitation and agro-industrial revenue increase.

研究领域: 食品科学 · 植物化学
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INDUSTRIAL CROPS AND PRODUCTS · 2016 · IF 3.449

Antihyperglycemic, antioxidant activities of two Acer palmatum cultivars, and identification of phenolics profile by UPLC-QTOF-MS/MS: New natural sources of functional constituents

Lu Zhang,Zong-cai Tu,Xing Xie,Yu Lu,Zhen-xing Wang,Hui Wang,Xiao-mei Sha

This research aimed to compare the antihyperglycemic and antioxidant abilities, and to characterize the bioactive constituents of two Acer palmatum cultivars, Acer palmatum ‘ Atropurpureum ’ (APA) and Acer palmatum Thunb (APT). Dry materials were respectively extracted with 70% and 90% methanol, followed by sequentially fractionation with ethyl acetate and n -butanol. The phytochemical profile of selected fraction was determined by using UPLC-QTOF-MS/MS. APT is a better source of natural antioxidants and α- glucosidase inhibitors than APA due to its higher total phenolic content (TPC), and stronger antioxidant and α- glucosidase inhibitory activities. The highest total phenolic and total flavonoid content were found in the ethyl acetate fraction (EAF) of 90% methanol extract of APT (468.49   mg GAE/g Extract) and 70% methanol extract of APA (142.60   mg QuE/g Extract), respectively. The EAF of 70% methanol extract of APT gave the strongest DPPH· scavenging ability, ABTS + · scavenging ability and α- glucosidase inhibitory, with the IC 50 values of 7.06, 4.18 and 1.99   μg/mL, respectively. The latter two were much higher than that of individual positive control. HPLC analysis revealed similar phytochemical profiles of all EAFs. Twenty-five compounds, including 3 organic acids, 5 phenolic acids, 8 tannins, 7 flavonoids and 2 proanthocyanidins, were identified or tentatively identified from APT, with tannins and flavonoid glucosides as the major active compounds. The results indicated a strong potential of Acer palmatum as a natural source of excellent antioxidants and antihyperglycemic compounds in the prevention and treatment of type II diabetes and its complication.

研究领域: 植物学 · 药理学 · 代谢疾病研究
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CHEMISTRY & BIODIVERSITY · 2017 ·Vol. 14 ·期 12 ·e1700305 · IF 1.44

Chemical Components, Biological Activities, and Toxicological Evaluation of the Fruit (Aril) of Two Precious Plant Species from Genus Taxus

Na Li,Zheng Pan,Dan Zhang,Hua-Xing Wang,Bao Yu,Sheng-Ping Zhao,Jia-Jia Guo,Jian-Wei Wang,Ling Yao,Wei-Guo Cao

The fruit (aril) of the endangered genus Taxus plants is an abandoned herbal resource. Traditionally, people enthusiastically focus on its bark, its renewable, tremendous arils fall into the soil with seeds after they are mature. The present research investigated the fruit of two species from the genus Taxus , Taxus chinensis var. mairei , and Taxus media , with regards to their antioxidant and antihyperglycaemic activities, safety, and bioactive constituents. Results showed that T . chinensis var. mairei and T . media both had certain biological activities with T . chinensis var. mairei better in antioxidant activity and T . media better in antihyperglycaemic activity. Correlation analysis revealed that the differences in bioactivities depended on content of their mainly chemical components. The mice acute oral toxicity test indicated that the methanol extracts of the two biotypes of Taxus were safe. And nineteen compounds were tentatively assigned from the two varieties, via tandem mass spectrometry using a LC-ESI-Q-TOF-MS instrument, which included phenols, flavonoids, and terpenes. These results indicate a possible application of Taxus fruit extracts in various fields like in food industry, however, this still needs further investigations. Graphical

研究领域: 植物学 · 药理学 · 毒理学
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JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE · 2024 · IF 3.3

Preparation and structural characteristics of polysaccharides from loquat peel waste, and their preliminary bioactivities

Dan Liu,Lingju Zhang,Hongge Huang,Changchun Fu,Yunxiao Wei,Zuolong Yu,Chao Han,Wei Tang

BACKGROUND Loquat peel, often as food waste, is a valuable source of bioactive polysaccharides. However, study of such polysaccharides is insufficient, leaving a significant gap in understanding their preparation, structure and bioactivities. RESULTS In this study, three types of loquat peel polysaccharides (LPWP, LPHP and LPNP) were sequentially extracted using hot water, HCl and NaOH solutions, respectively. Among them, LPWP was the purest, with a yield of 3.4% and molecular weight of 470.6 kDa, and it differed from LPHP and LPNP in structure, as evidenced by Fourier transform infrared spectroscopy, X-ray diffraction and scanning electron microscopy, which demonstrated that LPWP consisted of more arabinose (Ara) but less galacturonic acid, rhamnose and galactose, with molar percentages of 71.3%, 23.3%, 3.5% and 1.9%, respectively. Besides, LPWP also exhibited superior antioxidant and antihyperglycemic activities in vitro , particularly in inhibiting α-amylase and α-glucosidase. Methylation and nuclear magnetic resonance analysis confirmed that LPWP was a methyl-esterified pectic polysaccharide rich in branched arabinan, as evidenced by the notable proportion of α-Ara residues, including T-α-Ara f , 1,5-α-Ara f and 1,2,3,5-α-Ara f , with molar percentages of 27.1%, 23.1% and 10.2%, respectively. AFM imaging further revealed its branched-chain morphology and aggregation behavior. CONCLUSION This study highlights the potential of loquat peel polysaccharides as a bioactive ingredient with significant antioxidant and antihyperglycemic properties, particularly LPWP, which was found as a methyl-esterified pectic polysaccharide with abundant-branched arabinan. Our work provides valuable insights into the application of loquat peel polysaccharides in functional foods. © 2024 Society of Chemical Industry.

研究领域: 食品科学 · 生物化学
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Food & Function · 2019 ·Vol. 10 ·期 8 ·4868-4876 · IF 3.241

Antihyperglycemic and antihyperlipidemic activities of a polysaccharide from Physalis pubescens L. in streptozotocin (STZ)-induced diabetic mice

Xiaoyong Chen,Xiong Li,Xiaobo Zhang,Lijun You,Peter Chi-Keung Cheung,Riming Huang,Jianbo Xiao

In this study, a polysaccharide was extracted from Physalis pubescens L. (named PP). Its antihyperglycemic and antihyperlipidemic activities were evaluated in STZ-induced diabetic mice. Results showed that PP was determined to be composed of rhamnose (Rha), arabinose (Ara), fucose (Fuc), xylose (Xyl), mannose (Man), glucose (Glc) and galactose (Gal) with molar percentages of 4.65%, 17.34%, 1.43%, 6.24%, 5.52%, 45.5%, and 19.31%, respectively. The average molecular weight (Mw) was found to be 20.0 kDa. It had a strong α-glucosidase inhibitory activity in vitro. PP treatment could enhance the oral glucose tolerance, and increase the levels of SOD, GSH, CAT, vitamin C, vitamin E, HDL-c, C-peptide, GCK and hepatic glycogen in diabetic mice. Besides, PP treatment could also decrease the levels of MDA, TG, TC, LDL-c, BUN and G-6-Pase. The regulating effects were stronger in high dose PP treatment than those in the low and medium dose treatments. In short, PP played an important role in protecting STZ-induced diabetic mice, and the effect was closely related to its activities in antioxidation and regulating glucose and lipid metabolism.

研究领域: 药理学 · 代谢生物学
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FOOD RESEARCH INTERNATIONAL · 2020 · IF 4.972

Curcumin-loaded liposomes prepared from bovine milk and krill phospholipids: Effects of chemical composition on storage stability, in-vitro digestibility and anti-hyperglycemic properties

Yujie Wu,Bolin Mou,Shuang Song,Chin-Ping Tan,Oi-Ming Lai,Cai Shen,Ling-Zhi Cheong

Present study prepared curcumin liposomes with high encapsulation efficiency (>70%) using bovine milk and krill phospholipids; and investigated the effects of phospholipids composition on storage stability, in-vitro bioavailability, antioxidative and anti-hyperglycemic properties of the curcumin liposomes. Curcumin liposomes prepared from bovine milk phospholipids have smaller particle sizes (163.1 ± 6.42 nm) and greater negative zeta potentials (−26.7 mv) as compared to that prepared from krill phospholipids (particle size: 212.2 ± 4.1 nm, zeta potential: −15.23 mv). In addition, curcumin liposomes from bovine milk phospholipids demonstrated better stability under harsh storage conditions (alkaline conditions, oxygen, high temperature and relative humidity). Nevertheless, curcumin-loaded liposomes prepared from bovine milk phospholipids have inferior bioavailability compared to that prepared from krill phospholipids. No significant differences can be observed in terms of anti-oxidative and anti-hyperglycemic properties of liposomes prepared from both bovine milk and krill phospholipids. Findings from present study will open up new opportunities for development of stable curcumin liposomes with good functional properties (high digestibility, bioavailability and pharmacological effects).

研究领域: 药剂学 · 食品科学 · 营养学
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DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY · 2022 · IF 3.727

Preparation, in vitro and in vivo evaluation of pinocembrin-loaded TPGS modified liposomes with enhanced bioavailability and antihyperglycemic activity

Xinyi Shen,Wanjing Rong,Michael Adu-Frimpong,Qing He,Xiaoxiao Li,Feng Shi,Hao Ji,Elmurat Toreniyazov,Xiaoli Xia,Jian Zhang,Qilong Wang,Jiangnan Yu,Ximing Xu

Purpose To prepare polyethylene glycol succinate-vitamin E modified pinocembrin (PCB)-loaded liposomes (PCBT-liposomes) and evaluate PCBT-liposomal pharmacokinetics and antihyperglycemic activity.Significance The novel PCBT-liposomes demonstrated a promising application prospect as a nano drug carrier for future research.Methods Thin film dispersion was used to prepare PCBT-liposomes. We measured a series of characterization, followed by in vitro cumulative release, in vivo pharmacokinetic study, and antihyperglycemic activity evaluation.Results PCBT-liposomes displayed spherical and bilayered nanoparticles with mean particle size (roughly 92 nm), negative zeta potential (about −26.650 mV), high drug encapsulation efficiency (87.32 ± 1.34%) and good storage (at 4 or 25 °C) stability during 48 h after hydration. The cumulative release rate of PCBT-liposomes was markedly higher than free PCB in four different pH media. In vivo investigation showed that PCBT-liposomes could obviously improve oral bioavailability of PCB by 1.96 times, whereas the Cmax, MRT0–t, and T1/2 of PCBT-liposomes were roughly 1.700 ± 0.139 µg·mL−1, 12.695 ± 1.647 h, and 14.244 h, respectively. In terms of biochemical analysis, aspartate amino-transferase (AST), alanine amino-transferase (ALT), interleukin-1 (IL-1), and tumor necrosis factor-α (TNF-α) concentrations in serum of diabetic mice were respectively decreased 28.28%, 17.23%, 17.77%, and 8.08% after PCBT-liposomal treatment.Conclusion These results show PCBT-liposomal preparation as an excellent nano-carrier which has the potential to improve water solubility, bioavailability, and antihyperglycemic activity of PCB, amid broadening the application of PCB in the clinical settings.

研究领域: 药剂学 · 药理学 · 纳米技术 · 糖尿病研究
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BIOORGANIC CHEMISTRY · 2021 · IF 5.275

Design, synthesis and bioactivity evaluation of thiazolidinedione derivatives as partial agonists targeting PPARγ

Juan Sun,Han-Yu Liu,Yi-Heng Zhang,Ze-Yu Fang,Peng-Cheng Lv

Thiazolidinedione (TZD) is a novel peroxides proliferator activated receptor γ (PPAR γ ) agonist with many side effects. Herein, we developed a series of novel TZD analogues as partial agonists targeting PPAR γ . The study of anti-hyperglycemic activity and anti-inflammatory activity enabled us to identify a novel compound, 4 g , which quickly recover the blood glucose of mice at the concentration of 100 mg/kg, and show similar anti-inflammatory activity to ibuprofen at the concentration of 20 mg/kg. The competitive binding assay confirmed direct binding of 4 g to the LBD of PPAR γ with IC 50 being 1790 nM, and dose-dependently increased the transcriptional activity of PPAR γ . Besides, through computer-aided drug design software simulation docking, it was found that compound 4 g showed the best binding ability to target protein PPAR γ . Furthermore, because of the introduction of benzene containing group at N3 position, the stability of H12 in the active pocket is reduced and the stability of H3 and β -fold is increased, showing the characteristics of some PPAR γ agonists, based on the docking model analysis. Together, these results suggest that 4 g is a promising PPAR γ agonist that deserves further investigation.

研究领域: 药理学 · 药物化学
✓ 已验证 DOI PubMed 高影响因子
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Journal of Advanced Research · 2022 · IF 12.822

Amelioration of type 2 diabetes by the novel 6, 8-guanidyl luteolin quinone-chromium coordination via biochemical mechanisms and gut microbiota interaction

Xiaodong Ge,Xiaoyu He,Junwei Liu,Feng Zeng,Ligen Chen,Wei Xu,Rong Shao,Ying Huang,Mohamed A. Farag,Esra Capanoglu,Hesham R. El-Seedi,Chao Zhao,Bin Liu

Introduction Luteolin is a plant-derived flavonoid that exhibits a broad range of pharmacological activities. Studies on luteolin have mainly focused on its use for hyperlipidaemia prevention, whereas the capacity of the flavonoid to hinder hyperglycaemia development remains underexplored. Objectives To probe the anti-hyperglycemic mechanism of 6,8-guanidyl luteolin quinone-chromium coordination (GLQ.Cr), and to assess its regulatory effect on intestinal microbiota in type 2 diabetes mellitus (T2DM) mice. Methods High-sucrose/high-fat diet-induced and intraperitoneal injection of streptozotocin was used to develop a T2DM model. Glycometabolism related indicators, histopathology, and gut microbiota composition in caecum samples were evaluated, and RNA sequencing (RNA-seq) of liver samples was conducted. Faecal microbiota transplantation (FMT) was further used to verify the anti-hyperglycemic activity of intestinal microbiota. Results The administration of GLQ.Cr alleviated hyperglycaemia symptoms by improving liver and pancreatic functions and modulating gut microbe communities ( Lactobacillus, Alistipes , Parabacteroides , Lachnoclostridium , and Desulfovibrio ). RNA-seq analysis showed that GLQ.Cr mainly affected the peroxisome proliferative activated receptor (PPAR) signalling pathway in order to regulate abnormal glucose metabolism. FMT significantly modulated the abundance of Lactobacillus , Alloprevotella , Alistipes , Bacteroides, Ruminiclostridium, Brevundimonas and Pseudomonas in the caecum to balance blood glucose levels and counteract T2DM mice inflammation. Conclusion GLQ.Cr improved the abnormal glucose metabolism in T2DM mice by regulating the PPAR signalling pathway and modulating intestinal microbial composition. FMT can improve the intestinal microecology of the recipient and in turn ameliorate the symptoms of T2DM-induced hyperglycaemia.

研究领域: 药理学 · 糖尿病 · 微生物学 · 分子生物学 · 生物化学
✓ 已验证 DOI PubMed 高影响因子
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Foods · 2024 ·Vol. 13 ·期 17 ·2729 · IF 4.7

Antihyperglycemic, Antiaging, and L. brevis Growth-Promoting Activities of an Exopolysaccharide from Agrobacterium sp. FN01 (Galacan) Evaluated in a Zebrafish (Danio rerio) Model

Xiaoqing Xu,Lingling Du,Meng Wang,Ran Zhang,Junjie Shan,Yu Qiao,Qing Peng,Bo Shi

Agrobacteriumsp. are notable for their ability to produce substantial amounts of exopolysaccharides. Our study identified an exopolysaccharide (Galacan, 4982.327 kDa) fromAgrobacteriumsp. FN01. Galacan is a heteropolysaccharide primarily composed of glucose and galactose at a molar ratio of 25:1. The FT-IR results suggested that Galacan had typical absorption peaks of polysaccharide. The results of periodate oxidation, Smith degradation, and NMR confirmed the presence of structural units, such as β-D-Galp(→, →3)β-D-Galp(1→, →2,3)β-D-Glcp(1→, β-D-Glcp(1→, and →2)β-D-Glcp(1→. Galacan demonstrated significant biological activities. In experiments conducted with zebrafish, it facilitated the proliferation ofLactobacillus brevisin the intestinal tract, suggesting potential prebiotic properties. Moreover, in vivo studies revealed its antihyperglycemic effects, as evidenced by significant reductions in blood glucose levels and enhanced fluorescence intensity of pancreatic β cells in a streptozotocin (STZ)-induced hyperglycemic zebrafish model. Additionally, antiaging assays demonstrated Galacan’s ability to inhibit β-galactosidase activity and enhance telomerase activity in a hydrogen peroxide (HP)-induced aging zebrafish model. These findings emphasized the potential of Galacan as a natural prebiotic with promising applications in diabetes prevention and antiaging interventions.

研究领域: 微生物学 · 生物化学 · 药理学 · 分子生物学 · 水生生物学
✓ 已验证 DOI PubMed 高影响因子
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STARCH-STARKE · 2024 · IF 2.6

Optimization of Ultrasound-Assisted Deep Eutectic Solvent Extraction and Bioactivities of Polysaccharide from Porphyra haitanensis

Wendie Hu,Bing Liu,Yao Wen

In this paper, ultrasound-assisted method and deep eutectic solvent (DES) are used to extract polysaccharides from Porphyra haitanensis . The single-factor experiment is carried out first, and then the response surface experiment is designed to obtain the optimal process conditions. The optimal extraction conditions are the molar ratio of choline chloride to oxalate of 1:1, the water content of DES of 60%, the solid–liquid ratio of 1:60 g mL −1 , the time of 120 min, the power of 200 W, and the temperature of 80 °C, with the extraction yield of 4.42%. And the yield of P. haitanensis polysaccharides (PHPs) is 3.14% and 3.31% by water immersion and ultrasonic water extraction, respectively, indicating that the DES extraction method is superior to these two methods, and the optimization effect is good. The extracted polysaccharides are tested for biological activity after separation and purification on DEAE and Sephadex G-75 columns. The results of α-glucosidase inhibitory activity and α-amylase inhibitory activity show that PHPs have certain antioxidant activity. 1,1-Diphenyl-3-nitrophenylhydrazine (DPPH) and 2,2-diazo-di-3-ethylbenzothiazolin-6-sulfonic acid (ABTS) free radical scavenging assays show that PHPs have certain antiglycemic activity.

CAS / MDL: 56180-94-0 3767-28-0
研究领域: 食品科学 · 生物技术 · 药物化学
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