BIOMEDICINE & PHARMACOTHERAPY
·
2018
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IF 3.457
YingHui Zhang,Bing Wang,Feng Guo,ZhiZhen Li,GuiJun Qin
Diabetic nephropathy is one of the manifestations of systemic microangiopathy in diabetes. Hesperetin , a natural flavanone glycoside compound in citrus fruits, has been demonstrated to exert hypoglycemic effects and protect kidney in experimental diabetic animals. The current study was aimed to investigate the mechanisms underlying the hypoglycemic effects of hesperetin in high-fat/streptozocin (STZ)–induced diabetic nephropathy. The results showed that mice in whom hesperetin was administered for 4 weeks attenuated the increased fasting blood glucose and impaired glucose tolerance ability that was observed in high-fat/STZ mice. In addition, we found that hesperetin ameliorated the abnormalities of biochemical parameters in serum, liver, and kidney of mice with diabetic nephropathy. Hesperetin also rescued the irregular distortions in glomerular basement membrane and expanded mesangial regions. Moreover, hesperetin repaired the function of podocyte by increasing renal nephrin expression and decreasing renal alpha-smooth muscle actin expression. Furthermore, hesperetin inhibited the expression of transforming growth factor-β1 (TGF-β1) and its downstream effectors integrin-linked kinase (ILK) and Akt. In conclusion, our study implies that hesperetin produced protective effects in diabetic nephropathy possibly by suppressing TGF-β1-ILK-Akt signaling.
研究领域:
药理学
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内分泌学
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肾病学
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DOI
PubMed
高影响因子
Foods
·
2023
·Vol. 12
·期 22
·4142
·
IF 5.2
Kumaravel Kaliaperumal,Linyan Zhang,Liangliang Gao,Qin Xiong,Yan Liang,Yueming Jiang,Jun Zhang
The α-glucosidase inhibitor is of interest to researchers due to its association with type-II diabetes treatment by suppressing postprandial hyperglycemia. Hesperidin is a major flavonoid in orange fruit with diverse biological properties. This paper evaluates the effects of hesperidin on α-glucosidase through inhibitory kinetics, fluorescence quenching, and molecular docking methods for the first time. The inhibition kinetic analysis shows that hesperidin reversibly inhibited the α-glucosidase activity with an IC50value of 18.52 μM and the inhibition was performed in an uncompetitive type. The fluorescence quenching studies indicate that the intrinsic fluorescence of α-glucosidase was quenched via a static quenching process and only one binding site was present between the hesperidin and α-glucosidase. The interaction between them was spontaneous and mainly driven by hydrogen bonds, as well as hydrophobic forces. Furthermore, the molecular docking results suggest that hesperidin might bond to the entrance or outlet part of the active site of α-glucosidase through a network of five hydrogen bonds formed between hesperidin and the four amino acid residues (Trp709, Arg422, Asn424, and Arg467) of α-glucosidase and the hydrophobic effects. These results provide new insight into the inhibitory mechanisms of hesperidin on α-glucosidase, supporting the potential application of a hesperidin-rich orange product as a hypoglycemic functional food.Keywords:hesperidin;α-glucosidase;antidiabetic;flavonoid;orange
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PubMed
高影响因子
FOOD HYDROCOLLOIDS
·
2023
·
IF 10.7
Haihua Jiang,Xiaoyun Fei,Guowen Zhang,Xing Hu,Deming Gong,Junhui Pan
Hesperitin (Ht) and hesperidin (Hd) have a variety of biological activities, but their applications are limited due to the poor aqueous dispersion, weak stability and low bioavailability. In this study, a complex coacervate, formed by glutenin heated at pH 2, 80 °C for 8 h and orange peel pectin (P), was used as a carrier to enhance the water dispersibility of Ht/Hd, and their release behavior in vitro were investigated. The main driving forces for the complexes of Ht/Hd with glutenin (Glu) or fibrillated glutenin (Glu-F) were hydrogen bonding and hydrophobic forces. However, the enthalpy change of the interaction of the fibrillated glutenin with Ht/Hd was reduced, implying the formation of a more stable Ht/Hd-Glu-F complex. Furthermore, the optimum mass parameter ratio of Ht/Hd:P:Glu-F obtained from orthogonal experiments was 5:4:40 at pH 6. Both Ht and Hd were almost insoluble in water (pH 6), while the formation of the Ht-Glu-F-P and Hd-Glu-F-P complexes increased the solubility of the almost insoluble Ht and Hd to 102.16 ± 4.82 and 220.57 ± 10.82 μg/mL, respectively. After 30 days of storage, the particle size of the emulsions formed by Ht-Glu-F-P and Hd-Glu-F-P complexes increased from 171.90 to 174.84 nm to 231.82 and 219.81 nm, respectively, which had better storage stability than those formed from Ht/Hd-Glu-P complexes. The increased intermolecular repulsion caused by fibrillation modification improved the stability of the delivery system. These results provide a unique method for improving the aqueous dispersion and storage stability of Ht/Hd.
研究领域:
食品科学
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生物化学
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DOI
高影响因子
Regenerative Biomaterials
·
2022
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IF 5.763
Ren Xiuli,Hu Yanan,Chang Linna,Xu Shibo,Mei Xifan,Chen Zhenhua
Bacterial infection and excessive inflammation are still the main obstacles to wound repair. Thus, antibacterial and anti-inflammation nanomaterials are always attracting for infected wound healing. In this work, ultra-uniform (∼20 nm) and colloidally stable Ag nanoparticles (Ag-Hes NPs) with core-shell structure were prepared by using hesperidin as reducing and capping agent. The obtained Ag-Hes NPs present effective antibacterial properties on both Staphylococcus aureus and Escherichia coli. Ag-Hes NPs also got high 1,1-diphenyl-1-picrylhydrazyl scavenging capability of 69%. Under the package of polyvinyl alcohol and sodium alginate, Ag-Hes NPs were encapsulated into electro spun nanofibers to form hydrogel (Ag-Hes@H). This strategy provides a moisture environment which could enrich and release Ag-Hes NPs gradually. Cell experiments and animal wound healing investigation proved that Ag-Hes@H could promote the proliferation and migration of human umbilical vein endothelial cells and accelerate infected wound healing. Meanwhile, Ag-Hes@H significantly reduced the expression of inflammatory cytokines, including IL-6, MMP9 and TNF-α. Immunohistochemistry data further suggested that Ag-Hes@H accelerated wound closure by promoting collagen deposition and skin cell proliferation. The designed antibacterial and anti-inflammatory Ag-Hes@H has great potential for promoting infected wound healing.
研究领域:
材料科学
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纳米技术
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生物医学工程
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药剂学
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DOI
PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
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2023
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IF 5.8
Kehong Dong,Yuxuan Sun,Xintao Gao,Jing Wang,Xiaochen Wu,Chuanlong Guo
Excessive acetaminophen (APAP) is the main cause of drug-induced acute liver failure, and the pathogenesis has not been elucidated and there is a lack of effective drugs. Hesperidin (Hes), a rich flavanone in citrus peel with excellent biological activities, is a potential agent for treatment liver injury. Due to poor water solubility of Hes, this study prepared mixed micelles using polyvinyl pyrrolidone (PVP K17) and poloxamer 188, and encapsulated Hes (Hes-MMs). The results showed that Hes-MMs exhibited a uniform spherical shape with a particle size of 66.80 ± 0.83 nm, and Hes-MMs significantly improved the dispersibility, antioxidant activity , and cellular uptake of Hes. In vitro results showed that Hes-MMs protected the proliferation inhibition of HepG2 cells induced by APAP, inhibited the production of reactive oxygen species (ROS) and the damage of mitochondrial membrane potential (MMP) induced by APAP. Furthermore, Hes-MMs exerted liver protective effects by inhibiting APAP induced mtDNA release and activating the cGAS-STING pathway. In vivo results demonstrated that Hes-MMs showed protective and therapeutic effects on APAP induced liver injury, and their mechanisms were related to the mtDNA-cGAS-STING signaling pathway . In summary, our study demonstrated that the mtDNA-cGAS-STING pathway was involved in APAP induced acute liver injury, and Hes-MMs might be a potential therapeutic agent for treating APAP induced acute liver injury.
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PubMed
高影响因子
Drug Delivery and Translational Research
·
2023
·
IF 5.4
Yu Linrong,Zhang Qiliang,Zhou Liping,Wei Yanjun,Li Mengshuang,Wu Xianggen,Xin Meng
Alpha-glucosyl hesperidin (GH) is an aqueous soluble, amphipathic hesperidin derivative with several pharmacological effects, and it is postulated in this manuscript that GH could potentially be utilized as an active pharmaceutical excipient in eyedrops. The ocular safety of GH was evaluated according to in vitro cytotoxicity and in vivo ocular tolerance. The in vivo corneal permeation of coumarin-6 (Cou-6) with or without GH was characterized, and the in vivo inducing corneal wound healing using bisdemethoxycurcumin (BDMC) with or without GH was also evaluated to determine whether GH is an active pharmaceutical excipient in eyedrops. The results demonstrated that as high as 30 mg/ml of GH exhibits high-level in vitro and in vivo safety profiles according to four in vitro and in vivo evaluations. GH improved the corneal permeation of Cou-6 in mice, as well as demonstrated in vitro antioxidant activity. Concerning in vivo activity, a BDMC–GH suspension was shown to be synergistic in promoting corneal wound healing in mice, as well as restoring corneal sensitivity, promoting corneal epithelial wound healing, and restoring the corneal tissue structure without inflammatory cell infiltration. Overall, GH could be a novel and promising active excipient in eyedrops. Graphical Abstract
研究领域:
药学
·
眼科
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DOI
PubMed
高影响因子
Journal of Essential Oil Bearing Plants
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2022
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IF 1.971
Weilong Zheng,Fang Wu,Xi Luo,Caimiao Bian,Yingying Zhang,Fengwei Yin,Haiyu Liu,Yongqian Fu
Large amounts of citrus peel are discarded as solid waste owing to the lack of recycling methods. In this study, mixed solvent extraction combined with multi-phase salting-out extraction was performed to explore the extraction process of essential oil and hesperidin. Optimal conditions were used for mixed solvent extraction (citrus peel 6%; ratio of ethanol to n-hexane 1:5; duration, stirring speed, and temperature were 150 min, 120 r/min, and 45°C, respectively) and multi-phase salting-out extraction (citrus peel residue 10%; ratio of salt to ethanol 19:24; mass fraction of n-hexane 25%; extraction duration 120 min). Under two-step extraction conditions, 63.74±2.40% essential oil and 27.13±1.36% hesperidin were recovered, with total extraction efficiencies of 5.19±0.09 and 1.91±0.25%, respectively. The amplification effect was not significant, and the organic solvents could be reused three times while maintaining 80% recovery in both steps to balance the commercial cost and extraction efficiency.
研究领域:
食品科学
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植物化学
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DOI
高影响因子
Diabetes Metabolic Syndrome and Obesity-Targets and Therapy
·
2024
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IF 2.8
Ting Liu,Chao Lei,Qinhong Huang,Weiqi Song,Chen Li,Ning Sun,Zhihua Liu
Introduction Obesity, which is associated with gut microbiota dysbiosis, low-grade chronic inflammation and intestinal barrier dysfunction, can cause a variety of chronic metabolic diseases. Phytochemical flavonoids have a variety of biological activities, among which there may be safe and effective anti-obesity solutions.Methods We tested a plant-derived flavonoid hesperidin and fecal microbiota transplantation (FMT) to alleviate diet-induced obesity. High-fat diet (HFD)-fed mice were treated with hesperidin (100 and 200 mg/kg BW) and FMT.Results Results indicated that hesperidin had the effects of reducing obesity as indicated by reduction of body weight, fat accumulation and blood lipids, reducing inflammation as indicated by reduction of pro-inflammation factors including TNFα, IL-6, IL-1βand iNOS, and improving gut integrity as indicated by increasing colon length, reducing plasma gut permeability indicators iFABP and LBP, increased mRNA expression of mucus protein Muc2, tight junction p Claudin 2, Occludin and ZO-1 in the HFD-fed mice. The anti-obesity effects of hesperidin treatment have a dose-dependent manner. In addition, 16S rRNA-based gut microbiota analysis revealed that hesperidin selectively promoted the growth of Lactobacillus salivarius, Staphylococcus sciuri and Desulfovibrio C21_c20 while inhibiting Bifidobacterium pseudolongum, Mucispirillum schaedleri, Helicobacter ganmani and Helicobacter hepaticus in the HFD-fed mice. Horizontal feces transfer from the normal diet (ND)-fed mice to the HFD-fed mice conferred anti-obesity effects and transmitted some of the HFD-modulated microbes.Conclusion We concluded that hesperidin and FMT both affect the reduction of body weight and improve HFD-related disorders in the HFD-fed mice possibly through modulating the composition of the gut microbiota.
研究领域:
营养学
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微生物学
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药理学
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DOI
PubMed
高影响因子
INDUSTRIAL CROPS AND PRODUCTS
·
2022
·
IF 6.449
Peng Zhou,Min Zheng,Xiangzhou Li,Jun Zhou,Yaxuan Shang,ZhaoShuang Li,Limin Qu
With the proposal of the Paris Climate Agreement and double carbon policy, production enterprise is now facing green and low-carbon transformation. To promote green and low-carbon development, optimizing the production process and improving utilization rate of raw materials for the reduction of production cost is an significant technological path for the plant extract industry. Thus, the aim of this work was to develop a consecutive extraction process of pectin and hesperidin with lower cost and higher purity, as well as better properties of extract. The process parameters will be put forward through single-factor experiments, Plackett-Burman design and Box-Behnken design. The experimental results showed that the consecutive extraction process was effective and feasible. Pectin with excellent properties was obtained, and the solid-liquid ratio of extraction process parameters of hesperidin was reduced to 1:8 (g: mL). The problems of environmental pollution and high energy consumption in traditional extraction could be solved. The consecutive extraction process, an innovative, economic and environmental-friendly process, may be realized easily in industrial application. At the same time, the consecutive extraction process mechanism was revealed with the help of microscopy analysis of the plant tissue structure. The results demonstrated that preferential extraction of pectin process was helpful for the exposure and dissolution of hesperidin crystallization in cells and thus can improve extraction efficiency of hesperidin. The purity of the obtained hesperidin was up to 91.7%, which can be further purified depending on application requirements. A large amount of pectin was obtained (23.3% ± 0.5% yield), and the pectin has superior gel-property, strong antioxidant activity and certain antibacterial activity. The pectin and hesperidin obtained will have better application prospects in medicine and food because of their unique characteristics.
研究领域:
植物提取行业
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生物技术
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环境科学
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食品科学
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药学
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产品关联
DOI
高影响因子
RSC Advances
·
2022
·Vol. 12
·期 11
·6409-6415
·
IF 4.036
Hong-qi Xia,Tingting Gu,Ruiyi Fan,Jiwu Zeng
Electrocatalysis of bioflavonoids in carbon nanomaterials plays an important role in electrochemical sensors for the detection of their content in fruits. In this study, three types of carbon nanomaterials with 1D, 2D, and 3D structures, namely carbon nanotubes (CNTs), graphene oxide (GO), and Ketjen black (KB), were modified onto glassy carbon electrodes for the electrocatalysis of hesperidin and naringin, which are two important bioflavonoids in fruits. As a result, the CNT-modified electrodes showed the highest electrocatalytic activity for both hesperidin and naringin compared to GO and KB. The morphology and surface chemistry of the carbon nanomaterials were characterized. The structural defects and carbon status of carbon nanomaterials are proposed to be the most important factors affecting the electrocatalysis of hesperidin and naringin. Finally, a CNT-based electrochemical sensor was fabricated to simultaneously detect hesperidin and naringin. Real sample tests on the fruit extract of Citrus grandis “Tomentosa” show that the proposed electrochemical sensors with high recovery thus could be employed in practical applications.
研究领域:
电化学
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纳米技术
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分析化学
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食品科学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF FOOD SCIENCES AND NUTRITION
·
2022
·
IF 4.444
Xiao Guo,Xuedan Cao,Xiugui Fang,Ailing Guo,Erhu Li
This study examined the effects of phase II metabolism and efflux transportation on the bioavailability of naringin, hesperidin, and their aglycones (naringenin and hesperetin) in rats. Results indicated naringin and hesperidin have a lower oral bioavailability than their aglycones. Of all the phase II enzymes tested, UDP-glucuronosyltransferase (UGT) 1A1, UGT1A2, UGT1A3, UGT1A7 and SULT sulfotransferase (SULT) 1B1 were of minor importance regarding the phase II metabolism of naringenin and hesperetin in the small intestine. Naringin, hesperidin, and their aglycones were all extensively metabolised in the liver. Naringin and hesperidin were more extensively transported by efflux transporters compared to their aglycones. Significant correlations between phase II enzymes and efflux transporters were detected. In conclusion, more extensive metabolism of naringin and hesperidin than their aglycones in the small intestine, and the interplay of phase II enzymes and efflux transporters in the small intestine explain the lower relative oral bioavailability of naringin and hesperidin than their aglycones.
研究领域:
药理学
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生物化学
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药物动力学
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DOI
PubMed
高影响因子
Food & Function
·
2023
·Vol. 14
·期 11
·5417-5428
·
IF 6.1
Mengwei Jia,Huihui Gu,Yongling Lu,Lishuang Lv
Acrolein (ACR) is a highly reactive α,β-unsaturated aldehyde that plays a key role in the pathogenesis of human diseases, such as atherosclerosis and pulmonary, cardiovascular, and neurodegenerative disorders. We investigated the capture capacity of hesperidin (HES) and synephrine (SYN) on ACR by individual and combined means in vitro, in vivo (utilizing a mouse model), and via a human study. After proving that HES and SYN could efficiently capture ACR by generating ACR adducts in vitro, we further detected the adducts of SYN-2ACR, HES-ACR-1, and hesperetin (HESP)-ACR in mouse urine by ultraperformance liquid chromatography-tandem mass spectrometry. Quantitative assays revealed that adduct formation occurred in a dose-dependent manner, and that there was a synergistic effect of HES and SYN on capturing ACR in vivo. Moreover, quantitative analysis suggested that SYN-2ACR, HES-ACR-1, and HESP-ACR were formed and excreted through the urine of healthy volunteers consuming citrus. The maximum excretions of SYN-2ACR, HES-ACR-1, and HESP-ACR were at 2–4, 8–10, and 10–12 h, respectively, after dosing. Our findings propose a novel strategy for eliminating ACR from the human body via the simultaneous consumption of a flavonoid and an alkaloid.
研究领域:
药理学
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毒理学
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生物化学
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营养学
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）