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CHEMICAL & PHARMACEUTICAL BULLETIN · 2011 ·Vol. 59 ·期 8 ·1045-1047 · IF 1.507

Synthesis and Biological Evaluation of Two Salidroside Analogues in the PC12 Cell Model Exposed to Hypoglycemia and Serum Limitation

Yibing Guo,Xiaohong Li,Yahong Zhao,Yongxing Si,Hui Zhu,Yumin Yang

Salidroside is a phenylpropanoid glycoside isolated from Rhodiola rosea L., a traditional Chinese medicinal plant, and has displayed a broad spectrum of pharmacological properties. In this paper, two analogues were prepared with the glucosamine and N-acetylglucosamine as glycosyl donor, 2-(4-hydroxyphenyl)ethanol as glycosyl acceptor. The effects of them over PC12 cell model exposed to hypoglycemia and serum limitation were assessed with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, Flow Cytometry and Western blot analysis.

研究领域: 药理学 · 神经生物学
✓ 已验证 DOI PubMed 高影响因子
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Marine Drugs · 2020 ·Vol. 18 ·期 9 ·444 · IF 4.073

Sargassum fusiforme Polysaccharides Prevent High-Fat Diet-Induced Early Fasting Hypoglycemia and Regulate the Gut Microbiota Composition

Bin Wei,Qi-Wu Zhong,Song-Ze Ke,Tao-Shun Zhou,Qiao-Li Xu,Si-Jia Wang,Jian-Wei Chen,Hua-Wei Zhang,Wei-Hua Jin,Hong Wang

A low fasting blood glucose level is a common symptom in diabetes patients and can be induced by high-fat diet (HFD) feeding at an early stage, which may play important roles in the development of diabetes, but has received little attention. In this study, five polysaccharides were prepared fromSargassumfusiformeand their effects on HFD-induced fasting hypoglycemia and gut microbiota dysbiosis were investigated. The results indicated that C57BL/6J male mice fed an HFD for 4 weeks developed severe hypoglycemia and fourSargassumfusiformepolysaccharides (SFPs), consisting of Sf-2, Sf-3, Sf-3-1, and Sf-A, significantly prevented early fasting hypoglycemia without inducing hyperglycemia. Sf-1 and Sf-A could also significantly prevent HFD-induced weight gain. Sf-2, Sf-3, Sf-3-1, and Sf-A mainly attenuated the HFD-induced decrease in Bacteroidetes, and all five SFPs had a considerable influence on the relative abundance ofOscillospira,Mucispirillum, andClostridiales. Correlation analysis revealed that the fasting blood glucose level was associated with the relative abundance ofMucispinllumandOscillospira. Receiver operating characteristic analysis indicated thatMucispinllumandOscillospiraexhibited good discriminatory power (AUC = 0.745–0.833) in the prediction of fasting hypoglycemia. Our findings highlight the novel application of SFPs (especially Sf-A) in glucose homeostasis and the potential roles ofMucispinllumandOscillospirain the biological activity of SFPs.Keywords:Sargassum fusiformepolysaccharides;high-fat diet;gut microbiota;early fasting hypoglycemia

研究领域: 营养学 · 微生物学 · 代谢病研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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MOLECULES · 2023 ·Vol. 28 ·期 20 ·7136 · IF 4.6

Phellinus igniarius Polysaccharides Ameliorate Hyperglycemia by Modulating the Composition of the Gut Microbiota and Their Metabolites in Diabetic Mice

Zaizhong Ni,Jinting Li,Xinyi Qian,Yidan Yong,Mengmeng Wu,Yanan Wang,Wendi Lv,Simeng Zhang,Yifei Zhang,Ying Shao,Anhui Chen

Gut microbiota dysbiosis has been reported as a risk factor in the development of type 2 diabetes mellitus (T2DM). Polysaccharides fromPhellinus igniarius(P. igniarius) possess various properties that help manage metabolic diseases; however, their underlying mechanism of action remains unclear. Therefore, in this study, we aimed to evaluate the effect ofP. igniariuspolysaccharides (SH-P) on improving hyperglycemia in mice with T2DM and clarified its association with the modulation of gut microbiota and their metabolites using 16S rDNA sequencing and liquid chromatography–mass spectrometry. Fecal microbiota transplantation (FMT) was used to verify the therapeutic effects of microbial remodeling. SH-P supplementation alleviated hyperglycemia symptoms in T2DM mice, ameliorated gut dysbiosis, and significantly increased the abundance ofLactobacillusin the gut. Pathway enrichment analysis indicated that SH-P treatment altered metabolic pathways associated with the occurrence and development of diabetes. Spearman’s correlation analysis revealed that changes in the dominant bacterial genera were significantly correlated with metabolite levels closely associated with hyperglycemia. Additionally, FMT significantly improved insulin sensitivity and antioxidative capacity and reduced inflammation and tissue injuries, indicating improved glucose homeostasis. These results indicate that the ameliorative effects of SH-P on hyperglycemia are associated with the modulation of gut microbiota composition and its metabolites.Keywords:Phellinus igniarius;polysaccharide;hypoglycemia;gut microbiota;metabolites;fetal microbiota transplantation

CAS / MDL: 7732-18-5
研究领域: 医学 · 微生物学 · 代谢组学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2023 · IF 5.8

Practicality of non-invasive glucagon-loaded dissolving microneedle for life-saving treatment of severe hypoglycemia in a diabetic rat model

Xuejiao Wang,Yinling Ma,Xiaodan Qi,Xi Ruan,Deying Cao,Feng Zhao

The development of dissolving microneedles (DMNs) has brought light to the transdermal delivery of biomolecules that are released into the skin through the rapid dissolution of the matrix material to enter the systemic circulation and exert therapeutic effects. Herein, we aimed to prepare, characterize, and analyze the effectiveness of a glucagon-loaded DMN system that rapidly increases blood sugar levels in rats with diabetic hypoglycemia. The stability and content of biological drugs following DMNs preparation was assessed using circular dichroism and bicinchoninic acid kit for protein determination kits(BCA kits). The maximum drug loading capacity of DMNs was approximately 140 μg in each patch, and the microneedles could be stored for up to 14 days under dry storage conditions. In vitro skin permeation studies were conducted using a Franz diffusion cell apparatus for glucagon-loaded DMNs. To investigate the efficacy of transdermal drug delivery, drug-laden DMNs were administered to rats with hypoglycemic diabetes. Compared to subcutaneous injections , microneedle drug release demonstrated comparable efficacy in raising blood glucose levels in vivo. Therefore, this study demonstrated that glucagon-loaded DMNs may be a promising approach for efficient transdermal drug delivery as an alternative to subcutaneous injection for the treatment of severe hypoglycemia in patients with diabetes.

CAS / MDL: 9002-89-5
研究领域: 药剂学 · 生物医学工程 · 内分泌学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Food Bioscience · 2025 · IF 5.9

Dihydromyricetin as a Dietary Supplement Enhances Hypoglycemic Efficacy: Synergistic Modulation of the Gut-Liver with Sangzhi Alkaloids

Yuwen Guan,Qiuyue Lv,Xinyu Wang,Baoping Jiang,Peigen Xiao

Chronic hyperglycemia, a hallmark of Type 2 diabetes mellitus, presents significant challenges in long-term management due to drug resistance and adverse effects. Dihydromyricetin (DHM), a natural flavanol from vine tea ( Ampelopsis grossedentata ), widely recognized as a nutraceutical, shows potential in enhancing the efficacy of pharmacological therapies. This study investigates the role of DHM in improving the hypoglycemic effects of Sangzhi Alkaloids (SZ-A), a commercially used glucosidase inhibitor. Our results demonstrate that DHM supplementation allows for a reduction in SZ-A dosage while maintaining or surpassing its glucose-lowering efficacy, thereby mitigating gastrointestinal side effects. Mechanistic studies reveal that this combination modulates the gut-liver axis, reducing ER stress, and enhancing gut microbiota diversity, including increased beneficial bacteria and non-12OH bile acids. These findings highlight DHM’s potential as an effective adjunctive nutraceutical, offering a safer and more efficient therapeutic strategy for managing hyperglycemia and related metabolic disorders.

CAS / MDL: 27200-12-0
研究领域: 药理学 · 代谢组学 · 营养学
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EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS · 2012 · IF 4.269

Hypoglycemic activity and oral bioavailability of insulin-loaded liposomes containing bile salts in rats: The effect of cholate type, particle size and administered dose

Mengmeng Niu,Yi Lu,Lars Hovgaard,Peipei Guan,Yanan Tan,Ruyue Lian,Jianping Qi,Wei Wu

Oral delivery of protein or polypeptide drugs remains a challenge due to gastric and enzymatic degradation as well as poor permeation across the intestinal epithelia. In this study, liposomes containing bile salts were developed as a new oral insulin delivery system. The primary goal was to investigate the effect of cholate type, particle size and dosage of the liposomes on the hypoglycemic activity and oral bioavailability. Liposomes containing sodium glycocholate (SGC), sodium taurocholate (STC) or sodium deoxycholate (SDC) were prepared by a reversed-phase evaporation method. After oral administration, all liposomes elicited a certain degree of hypoglycemic effect in parallel with an increase in blood insulin level. The highest oral bioavailability of approximately 8.5% and 11.0% could be observed with subcutaneous insulin as reference for SGC-liposomes in non-diabetic and diabetic rats, respectively. Insulin-loaded liposomes showed slower and sustained action over a period of over 20   h with peak time around 8–12   h. SGC-liposomes showed higher oral bioavailability than liposomes containing STC or SDC and conventional liposomes. The hypoglycemic effect was size-dependent with the highest at 150   nm or 400   nm and was proportionally correlated to the administered dose. The results supported the hypothesis of insulin absorption as intact liposomes.

研究领域: 药剂学 · 生物医学
✓ 已验证 DOI 高影响因子
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JOURNAL OF FOOD PROCESS ENGINEERING · 2019 ·Vol. 42 ·期 4 ·e13023 · IF 1.448

In vitro inhibitory effect of tea extracts on starch digestibility

Ishmael Ayim,Haile Ma,Evans Adingba Alenyorege,Yuqing Duan

The effect of brown, oolong, and green teas’ extract on the in vitro inhibition of starch digestibility of cassava, corn, plantain, and yam was explored. The starches exhibited moderately low hydrolysis rate and had moderate resistant starch ratios. Tea metabolites after extraction at different temperatures were quantified and correlated to starch inhibition at 1% introduction using principal component analysis (PCA). Total polyphenols (TP), (−)-epigallocatechin (EGC), (−)-gallocatechin gallate (GCG), (−)-catechin gallate (CG), and (−)-epigallocatechin gallate (EGCG) were positively correlated with starch digestion inhibition especially in the first and second hours of digestion. The (+)-catechin (C) and Total flavonoids (TF) in the teas, however, had a negative correlation with starch inhibition. Green tea extracts were more effective in starch digestion inhibition followed by brown tea and then oolong. TP, EGC, GCG, CG, and EGCG from green tea had the strongest inhibitory effect on starch digestion and that purified extracts of these compounds could be used at a statistically optimized combination to formulate diets with improved hypoglycemic potential. Practical applications In order to identify key components in tea responsible for hypoglycemic effect, tea extracts from three different source and their starch inhibitory properties were analyzed using starches from four plant sources. To this end, key components in the tea varieties were identified with potential hypoglycemic effect. Therefore, diets with potential hypoglycemic effect could be formulated using purified extracts from tea such as TP, (−)-epigallocatechin, (−)-gallocatechin gallate, (−)-catechin gallate, and (−)-epigallocatechin gallate under optimized conditions.

CAS / MDL: 609-99-4
研究领域: 食品科学 · 营养学 · 植物化学
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FOOD HYDROCOLLOIDS · 2025 · IF 12.4

Co-gelatinization with rutin nanoparticles for regulating rice starch digestibility

Shupin Ye,Yuteng Fu,Fangjian Ning,Jianyong Wu,Shunjing Luo,Jiangping Ye,Chengmei Liu

Polyphenolic compounds demonstrate significant potential in inhibiting starch digestion. However, the poor solubility, poor reactivity and easy degradation of polyphenols limit their effectiveness on starch digestion. The present study aims to avoid polyphenolic limitation in an effective strategy with the utility of rutin nanoparticles, and to co-gelatinize them with rice starch for regulating starch digestibility. SEM and XRD analysis had shown that rutin existed in an amorphous and non-inclusion state within NPS sample. It was accompanied by the absorption peak intensity related to hydrogen bonding weakened and shifted to lower wavenumbers in FTIR analysis. The double-helical domain formation increased from 4.57 % to 6.13 % in 13 CP/MAS NMR analysis. In-vitro digestion study showed that rutin nanoparticles exhibited maximum inhibition of starch digestion. Rutin was gradually released from NPS sample during digestion, with the highest concentration of rutin in its digestive fluid, showing the highest inhibition for digestive enzyme activity with values decreasing from 0.178 U/mL to 0.081 U/mL. Therefore, rutin nanoparticles can significantly regulate starch digestion by altering rice starch structural domains and inhibiting digestive enzyme activity. Overall, this study established a novel strategy to inhibit starch digestion by polyphenol nanoparticles, offering potential applications in low-glycemic starchy foods.

CAS / MDL: 7647-01-0
研究领域: 食品科学 · 生物化学
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2019 · IF 3.571

Origin of Hypoglycemic Benefits of Probiotic-Fermented Carrot Pulp

Yu-Jun Wan,Hui-Fang Shi,Rou Xu,Jun-Yi Yin,Shao-Ping Nie,Tao Xiong,Ming-Yong Xie

It has been found that probiotic-fermented carrot pulp has a beneficial effect in reducing blood glucose, more so than unfermented pulp. This paper explores the reason for this by looking at fermentation-induced changes in nutritional components and hypoglycemic effects of its polysaccharides. Micronutrient content showed minor changes, except for titratable acidity. Fat and protein decreased, while total carbohydrates increased. These polysaccharides are pectinic, and the number of total polysaccharides rose after fermentation. Scanning electron microscopy showed that the morphology changed from filamentous solid to spiral. The molecular weight of water-soluble polysaccharide (WSP) diminished after fermentation, while those of acid- and alkali-soluble polysaccharides increased. WSP had stronger hydroxyl radical scavenging activity in vitro, and WSP from probiotic-fermented carrot pulps showed better hypoglycemic effects than WSP from non-fermented carrot pulps in animal experiments. Thus, the fermentation-induced improvement in diabetes control from fermented carrot pulp probably arises from its WSP.

研究领域: 食品科学 · 营养学 · 生物化学
✓ 已验证 DOI PubMed 高影响因子
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2019 · IF 3.973

Nanoemulsion improves hypoglycemic efficacy of berberine by overcoming its gastrointestinal challenge

Hong-Yu Xu,Chang-Shun Liu,Chuan-Li Huang,Li Chen,Yu-Rong Zheng,Si-Hang Huang,Xiao-Ying Long

Berberine (BBR) is an important natural product with poor gastrointestinal behavior includes low permeability, P-glycoprotein efflux, and mass elimination in the intestine. The aim of this study was to develop a novel nanoemulsion (NE) to improve the hypoglycemic efficacy of BBR. NE was prepared and characterized by morphology and droplet size detection, stored stability, in vitro intestinal lipolysis and metabolism, Caco-2 cells transport, in situ single-pass intestinal perfusion, oral bioavailability in rats, and hypoglycemic efficacy in high-fat diet and streptozocin-induced mice. BBR-loaded NE exhibits small droplet size (30.56 ± 0.35 nm) and good stability. NE could remain intact after lipolysis and protect BBR against the intestinal metabolism mediated by CYP2D6 and CYP3A4. Cells transport and intestinal perfusion studies revealed that NE decreases the P-glycoprotein efflux of BBR by 2-fold and enhances its permeability by 5.5-fold. Consequently, NE increased the oral bioavailability of BBR in rats by 212.02%. Compared to BBR control, blood glucose level of diabetic mice by NE was decreased by 3-fold. This novel NE provides a promising carrier to improve the hypoglycemic efficacy of BBR by overcoming its gastrointestinal deficiency, which may offer a product for the therapy of diabetes.

CAS / MDL: 110-27-0
研究领域: 药剂学 · 糖尿病治疗 · 药物递送系统
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2024 · IF 7.7

The construction of retrograded short-chain amylose beads coated with calcium alginate for increased resistant starch

Mingju Li,Zhongxiu Wang,Yang Qin,Liu Xiong,Qingjie Sun

A novel strategy was developed to embed retrograded short-chain amylose (RSCA) into calcium alginate (CA) at varying concentrations (0.25 %, 0.5 %, 0.75 %, 1 %, 1.5 %, and 2 %) through ion crosslinking, aimed at enhancing the content of heat-resistant RS. The concentration of sodium alginate (SA) significantly influenced the thickness of the CA shell, thereby affecting the structural characteristics, physicochemical properties, and digestibility of the resulting beads. As the SA concentration increased from 0.5 % to 2 %, the CA shell thickness expanded from 0.612 μm to 1.837 μm, becoming denser and limiting the infiltration of enzymatic liquids during digestion. The initial gelatinization temperature of the beads exceeded 100 °C, and the enthalpy value of the 2 % SA beads was 25.40 ± 0.17 J·g −1 , indicating excellent thermal stability. After heat treatment, the crystallinity reached 90.50 %. The RS content of the 2 % SA beads was as high as 72.66 ± 0.15 %, with an estimated glycemic index of 54.72, classifying them as low-glycemic index foods. The heat-resistant RSCA@CA developed in this study shows significant potential for application in functional foods, particularly for individuals with obesity and diabetes.

CAS / MDL: 3326-32-7
研究领域: 食品科学 · 营养学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Food Bioscience · 2024 · IF 4.8

A multi-omics analysis reveals the response mechanism of Weissella confusa ZJU.2 to gastric acid and bile salts

Xiayu Liu,Liang Zhang,Ying Shi,Donghong Liu,Peichao Zhang,Qihe Chen

Stress response pathways are critical for probiotic survival, promoting survival through adaptive changes in genes and proteins. However, the underlying stress response mechanisms of probiotics, especially Weissella confusa , are poorly understood. We have employed whole genome sequencing to assemble and annotate the W. confusa ZJU.2 genome, probing in parallel the proteome and transcriptome changes under the treatment of gastric acid and bile salts through a multi-omics approach. Stringent filtering reveals that significant upregulation of alanine, aspartate and glutamate metabolism and glycolysis/gluconeogenesis pathway are critical for gastric acid and bile salt tolerance in W. confusa ZJU.2. Concomitantly, the conjoint transcriptome and proteome analysis showed that the polysaccharide biosynthesis protein WP_039968605.1 plays an important role in gastric acid and bile salt tolerance. Parallel reaction monitoring (PRM) and Real-time quantitative polymerase chain reaction (RT-qPCR) analysis were used to demonstrate the reliability of the results. Moreover, we found that W. confusa ZJU.2 may have hypoglycemic effects through an in vivo zebrafish chip model and in vitro α-glucosidase activity assay. Collectively, this study provides a valuable multi-omics resource for the study of stress response mechanisms of Weissella and lays a solid foundation for its broader functional activity applications.

研究领域: 微生物学 · 功能基因组学 · 分子生物学
✓ 已验证 DOI 高影响因子
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