Journal of Chemistry
·
2019
·
IF 1.727
Hongbin Guo,Mengqiao Chen,Mengran Li,Mingye Hu,Baohua Chen,Chengyan Zhou
Mangiferin (MG) is an active component in natural medicines, and various studies have been reported on pharmacological effects, but the low solubility and bioavailability of MG limit its wide application. The aim of the present study was to investigate the pharmacokinetic profiles of mangiferin (MG) and mangiferin monosodium salt (MG-Na) in rat plasma by UPLC-MS/MS, which were then compared between the two groups. An appropriate high sensitivity and selectivity ultraperformance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was applied to the comparison of plasma pharmacokinetics in MG and MG-Na using carbamazepine as internal standard (IS). These results showed that there were statistically significant differences in the pharmacokinetic parameters between MG and MG-Na after a single oral administration at 100 mg/kg. When compared with pharmacokinetic parameters of MG, the AUC(0-t), AUC(0–∞), Cmax,K10, and Ka of MG-Na were increased by 5.6-, 5.7-, 20.8-, 8-, and 83.6-fold, while the Tmax and CL/F were decreased by 4- and 5.7-fold (), respectively. t1/2 value showed an increasing trend, but was statistically significant between the two groups. Moreover, the AUC value in the MG-Na group was significantly increased and the relative bioavailability was calculated to be 570% when compared with that of the MG group. These results suggested that the salification reaction of MG can effectively enhance gastrointestinal absorption and relative bioavailability by improving solubility and membrane permeability.
研究领域:
药理学
·
分析化学
✓ 已验证
DOI
高影响因子
PHYTOMEDICINE
·
2025
·
IF 8.3
Penghong Xu,Yuping Qian,Guo Xu,Jianlin Chu,Bingfang He
Background Inflammatory bowel disease (IBD), a chronic inflammatory condition categorized into ulcerative colitis (UC) and Crohn's disease (CD), affects a growing global patient population. Despite the prevalence, clinically there is a scarcity of effective therapeutic agents. Purpose This study investigated the therapeutic effects of fructosyl mangiferin (FM) on UC and elucidated its underlying mechanisms through in vivo and in vitro experiments. Methods In vivo , a UC model of C57BL/6J mice was established via dextran sulfate sodium (DSS) induction, and the therapeutic effects were assessed through intragastric administration. In vitro , the murine macrophage cell line RAW264.7 was stimulated with lipopolysaccharide (LPS) to establish an M1 polarization model and introduced to explore the role of FM in immune cells. Molecular docking was further employed to investigate the specific molecular mechanisms of FM. Results In vivo experimental findings indicate that FM, like mangiferin (M), preserves mucin secretion and the expression of occludin protein, and both significantly impede the progression of fibrosis associated with colitis. Additionally, FM effectively suppresses M1 macrophage polarization and exerts a pronounced inhibitory effect on the adaptive immune response, outperforming M in mitigating UC. In vitro results corroborate FM's inhibitory action on M1 polarization. Molecular docking studies identified FM as a potential signal transducer and activator of transcription 3 (STAT3) inhibitor, aligning with western blot analyses from both in vivo and i n vitro experiments. Conclusion In conclusion, following fructosylation, FM exhibits remarkable anti-inflammatory and colonic protective effects. FM's ability to control the progression of UC offers a novel strategy for its potential treatment, warranting further investigation into its clinical application.
研究领域:
免疫学
·
药理学
·
消化病学
✓ 已验证
DOI
PubMed
高影响因子
FOOD SCIENCE AND TECHNOLOGY RESEARCH
·
2021
·
IF 0.668
Yunbo Li,Benguo Liu,Mengmeng Yu,Sheng Geng
Cyclodextrins (CDs) are widely applied to improve the aqueous solubility and stability of nutraceuticals with the advantages of high safety and low cost. In this study, the binding capacities of CDs (α-CD, β-CD, maltosyl-β-CD, hydroxypropyl-β-CD and γ-CD) with mangiferin were compared by the phase solubility method and isothermal titration calorimetry. γ-CD could completely encapsulate mangiferin at the molar ratio of 1:1, which coincided with the molecular docking and ONIOM calculation results that γ-CD had the lowest interaction energy with mangiferin. The independent gradient model (IGM) visualized the intermolecular non-covalent binding and electrostatic potential around mangiferin during interaction. By complexing with γ-CD, mangiferin was molecularly dispersed in the matrix of γ-CD with its aromatic ring in the hydrophobic cavity. Compared with pure mangiferin, the mangiferin/γ-CD complex exhibited the stronger chemical antioxidant activities. The obtained result can promote the application of mangiferin and γ-CD in foods.
研究领域:
食品科学
·
药剂学
✓ 已验证
产品关联
DOI
高影响因子
EUROPEAN JOURNAL OF PHARMACOLOGY
·
2020
·
IF 3.263
Qiurui Li,Hua Lin,Yanfen Niu,Yan Liu,Zhenyu Wang,Liudong Song,Lihui Gao,Ling Li
Increasing evidence shows that the intestinal tract plays an important role in maintaining urate homeostasis and might be a potential therapeutic target for hyperuricaemia . However, uric acid-lowering drugs available in the clinic do not target intestinal excretion as a therapeutic strategy. We previously reported that mangiferin had potent hypouricaemic effects in hyperuricaemic animals. However, the underlying mechanisms are not completely clear. Here, we investigated the effects of mangiferin on the intestinal excretion of urate and its underlying mechanisms. The data revealed that mangiferin concentration-dependently promoted the intestinal secretion of endogenous urate in in situ intestinal closed loops in normal and hyperuricaemic mice, as well as inhibited the absorption of exogenous uric acid perfused into the intestinal loops in rats. Administration of mangiferin not only decreased the serum urate levels in the hyperuricaemic mice but also increased the protein expression of ATP-binding cassette transporter, subfamily G, member 2 (ABCG2) and inhibited the protein expression of glucose transporter 9 (GLUT 9) in the intestine. These findings suggested that intestinal ABCG2 and GLUT9 might be pivotal and possible action sites for the observed hypouricaemic effects. Moreover, no significant changes in intestinal xanthine oxidoreductase activities were observed, suggesting that mangiferin did not affect intestinal uric acid generation in the hyperuricaemic mice. Overall, promoting intestinal elimination of urate by upregulating ABCG2 expression and downregulating GLUT9 expression might be an important mechanism underlying mangiferin lowering serum uric acid levels. Mangiferin supplementation might be beneficial for the prevention and treatment of hyperuricaemia.
研究领域:
药理学
·
生物化学
·
医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF LIPID SCIENCE AND TECHNOLOGY
·
2024
·
IF 1.8
Xin Yu,Xinyi Yang,Junqing Qian,Hui Guo
Mangiferin is one of the main bioactive ingredients in leaves of Mangifera indica . But the poor liposolubility and low bioavailability restrict its application. This study aimed to esterify mangiferin with lipase to improve its lipophilicity, and evaluate its antioxidant activity and hypoglycemic properties. Four fatty acids (palmitic acid, lauric acid, stearic acid, oleic acid) were selected for enzymatic esterification with mangiferin by single-factor experiments. Under the following optimum reaction conditions of tetrahydrofuran (THF): tert -amyl alcohol (2:1) was used as solvent, water activity was 0.31, TLIM lipase was 45 mg mL –1 , The ratio of mangiferin to fatty acid was 1:50, and the substrates were pretreated by ultrasonic for 0.5 h, then reacted at 55°C for 21 h, the resulting conversion rates of mangiferin-esterified derivatives exceeded 70.0%. Lipophilicity, antioxidant, and PTP1B inhibitory activity of mangiferin-esterified derivatives were determined. The results demonstrated that compared with mangiferin, the ability to scavenge DPPH radicals decreased by about 9%, but the lipophilicity was increased by 10–30 times, and the lipid antioxidant capacity was also improved significantly. Moreover, the inhibitory activity of protein tyrosine phosphatase 1B (PTP1B) exhibited minimal alteration. This indicates that esterification can not only improve the lipophilicity of mangiferin, but also improve its lipid antioxidant capacity. Practical Applications : In the study, a series of mangiferin-esterified derivatives were synthesized and their lipophilicity, antioxidant properties, and PTP1B inhibitory activity were determined. The results indicated that, compared with the untreated mangiferin, the mangiferin-esterified derivatives exhibited superior lipid antioxidant and hypoglycemic activities. Furthermore, the enzymatic esterification method employed in this study offered greater economic and environmental advantages when compared to chemical catalysis. Therefore, the preparation of mangiferin derivatives through enzymatic esterification were deemed feasible with potential application value for enhancing lipid antioxidant capacity in high-fat foods.
研究领域:
食品科学
·
生物化学
✓ 已验证
产品关联
DOI
高影响因子
Chinese Journal of Natural Medicines
·
2013
·
IF 0
Xue-Jian LI,Zheng-Cai DU,Yan HUANG,Bu-Ming LIU,Wen-Ji HU,Wen-Jie LU,Jia-Gang DENG
Aim To synthesize three novel esterified-derivatives of mangiferin and evaluate their hypoglycemic activities. Methods Acetic, propionic, and butyric anhydride were reacted with mangiferin, respectively. The hypoglycemic activity of the derivatives was evaluated using a hyperglycemic mouse model induced by streptozotocin (STZ), and the islet cells were checked by biopsy inspection. Results 7, 2′, 3′, 4′, 6′-penta-acetyl-mangiferin (PAM), 3, 6, 7, 2′, 3′, 4′, 6′-hepta-propionyl-mangiferin (HPM) and 3, 6, 7, 2′, 3′, 4′-hexa-butyryl-mangiferin (HBM) were synthesized and their structures were identified by MS, 1 H, 13 C NMR, and 2D NMR. These three compounds were reported for the first time. PAM group (0.5, 0.25 mmol·kg −1 ), HPM group (0.5, 0.25 mmol·kg −1 ), and HBM group (0.5, 0.25, 0.125 mmol·kg −1 ) mice showed strong hypoglycemic activity ( P < 0.01); mangiferin group (1, 0.5 mmol·kg −1 ), PAM group (0.125 mmol·kg −1 ) and HPM group (0.125 mmol·kg −1 ) showed marginal hypoglycemic activity ( P < 0.05); mangiferin group (0.25 mmol·kg −1 ) had the potential for a hypoglycemic effect, although it did not demonstrate that statistically. In histological examination, the islet cells of the PAM, HPM, and HBM groups could recover from the STZ damage; islet cells of the mangiferin group could recover also, but less than the esterified-derivative groups. Conclusion Derivatives could repair the damaged islet cells, and had higher lipid-solubility and stronger hypoglycemic activity than mangiferin itself. There existed a structure activity effect, and a solubility effect relationship: the larger esterification moieties, or the higher lipid-solubility, the stronger the hypoglycemic activity (no ester → acetyl → propionyl → butyryl). Esterified derivatives of mangiferin are potential compounds for new anti-diabetes drugs.
研究领域:
药理学
·
有机化学
·
糖尿病研究
✓ 已验证
DOI
IBRO Neuroscience Reports
·
2025
·
IF 2.9
Wei Nong,Xiaoli Chen,Yixin Chen,Xueping Feng,Wen Kong,Rui Chi,Li Yan,Zhiquan Wei
Extracellular β-amyloid protein (Aβ) plaques are prominent pathological feature of Alzheimer's disease (AD). Aβ oligomers and plaques induce sustained microglial activation via the adenosine monophosphate-activated protein kinase (AMPK)/mammalian target of rapamycin (mTOR)/interferon regulatory factor 5 (IRF5) signaling pathway. This microglial activation-mediated neuroinflammation can accelerate neuronal cell senescence. Consequently, the regulation of the AMPK/mTOR/IRF5 pathway presents a potential therapeutic target for AD, as it may inhibit neuroinflammation and delay neuronal cell senescence. Mangiferin, a bioactive natural polyphenol extracted from the leaves of Mangifera indica Linn ., has garnered significant attention for its anti-inflammatory properties. However, it remains unclear whether mangiferin can modulate the AMPK/mTOR/IRF5 pathway to inhibit microglial activation-mediated neuroinflammation and delay neuronal cell senescence. This study employed both cellular and animal models of neuronal cell senescence to explore the effects of mangiferin on the regulation of the AMPK/mTOR/IRF5 pathway, aiming to inhibit neuroinflammation and delay neuronal cell senescence in vitro and in vivo . Specifically, SH-SY5Y neuroblastoma cells were subjected to a neuroinflammatory microenvironment induced by Aβ1–42-mediated HMC3 microglial activation to induce neuronal cell senescence in vitro . Additionally, SAMP8 accelerated aging mice were utilized as an aging animal model. The results indicate that mangiferin significantly enhances AMPK phosphorylation in microglial cells, inhibits mTOR activation, and downregulates IRF5 expression. These effects collectively suppress microglial activation and markedly reduce the production of pro-inflammatory cytokines by activated microglia. Consequently, there is a decrease in the proportion of neurons arrested in the G0/G1 phase and a reduction in the number of senescence-associated β-galactosidase (SA-β-gal) positive neurons. Furthermore, mangiferin significantly decreases the expression of neuronal cell senescence markers P16Ink4a and P21Cip1. Collectively, these findings suggest that mangiferin effectively regulates the AMPK/mTOR/IRF5 pathway, inhibits neuroinflammation mediated by microglial activation, and delays neuronal cell senescence. This study underscores the potential of mangiferin for the treatment of neuroinflammation and neurodegenerative diseases.
研究领域:
神经生物学
·
药理学
·
老年医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Letters in Drug Design & Discovery
·
2024
·Vol. 21
·期 7
·1263-1273
·
IF 1.2
Zhang Guangjie,Xue Peiyu,Zhao Hongmei,Guan Tianzhu,Ma Zheng
Background: As one of the main by-products of mango production, the mango peel is rich in multiple polyphenols, such as mangiferin. Therefore, there is an urgent need to explore the potential mechanism of mangiferin for nutrition intervention of oxidative stress-related diseases.
Methods: Mangiferin was extracted and purified from the mango peel and was identified by the reverse phase high-performance liquid chromatography. The antioxidant potential of mangiferin was determined in vitro (potassium ferricyanide reducing capacity, DPPH, hydroxyl radicals scavenging
ability, and superoxide anion radicals reducing capacity). In order to explore the potential mechanism for the antioxidant activity of mangiferin, a combination of network pharmacology and molecular docking approaches was performed. Results: The purity of mangiferin from the mango peel
was ≥ 95.0%, and its antioxidant activity was confirmed by different in vitro assays. ALB, ESR1, CASP8, CASP3, BCL2L1, CXCL8, AKT1, CTNNB, and EGFR were identified as the potential oxidative stress-related targets of mangiferin. These results suggested that mangiferin might play
a key role in the antioxidant process through multi-targets. Conclusion: Integrated with network pharmacology and molecular docking methods, this work demonstrated the potential mechanism of mangiferin for nutrition intervention of oxidative stress-related diseases.
研究领域:
营养学
·
药理学
·
生物信息学
✓ 已验证
DOI
高影响因子
JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
·
2025
·
IF 3.5
Shuang Wang,Yuan Qin,Yashi Liu,Rui Jiao,Rui Lin,Zongxiang Yuan,Zouyan He
Background The inhibition of pancreatic lipase activity to reduce dietary lipid absorption is an effective strategy to combat obesity. Mangiferin, a bioactive flavonoid derived from Mangifera indica , exhibits potent lipid-lowering potential. However, although its in vitro inhibitory effect on pancreatic lipase has been identified, the underlying mechanism remains poorly understood. Direct in vivo evidence of its impact on dietary lipid absorption is also lacking. This study aimed to elucidate the mechanism of mangiferin's inhibition of pancreatic lipase through in vitro inhibitory kinetics assays and in silico molecular docking analysis. Its effects on dietary lipid absorption were also evaluated in a mouse model of high-fat diet (HFD)-induced obesity. Results Inhibitory kinetics assays demonstrated that mangiferin inhibited pancreatic lipase in a reversible, non-competitive manner, with a half- maximal inhibitory concentration (IC 50 ) of 82.31 μmol L −1 . Molecular docking showed that mangiferin bound to the enzyme's allosteric site through hydrogen bonds with Glu-188, Arg-191, Gln-22, and Val-21 residues, consistent with non-competitive inhibition. In vivo studies revealed that administration of 200 mg kg −1 body weight of mangiferin alleviated HFD-induced obesity, hepatic steatosis, and hyperlipidemia significantly. Notably, mangiferin increased fecal lipid excretion by 52.5%, which was significant, indicating reduced dietary lipid absorption. Conclusion These findings suggest that mangiferin is a promising pancreatic lipase inhibitor, which may reduce dietary lipid absorption, contributing, at least partially, to its lipid-lowering effects. © 2025 Society of Chemical Industry.
研究领域:
药理学
·
营养学
·
生物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
LWT-FOOD SCIENCE AND TECHNOLOGY
·
2024
·
IF 6
Yun Sun,Bohai Guo,Xianrui Liang,Zheng Luo,Jianzhong Han,Daofeng Qu
The biological activity of mangosteen peel proanthocyanidin extracts is related to digestive properties and colonic metabolism. Therefore, the study's aim was to investigate the dynamics of proanthocyanidin extracts during in vitro digestion and colonic fermentation, their protective effects against oxidative damage in PEC-J2 cells, and their interactions with the intestinal flora. The results showed that epicatechin and proanthocyanidin B2 were the most abundant in proanthocyanidin. In addition, the catechin was increased by 27.7 ± 0.2 μg/mL. The total phenol content, total flavonoid content, and proanthocyanidin content of mangosteen peel were reduced by 32.36%, 90.63%, and 78.06%, respectively. However, the antioxidant capacity was increased by two-fold, protecting against oxidative damage in cells. Proanthocyanidin polymers that are not digested by the gastrointestinal tract go to the colon, where they are metabolized by microorganisms to produce short-chain fatty acids (SCFAs). Proanthocyanidin extracts modulated the microbial flora structure: the relative abundance of Phascolarctobacterium , Roseburia , Faecalibacterium , Coprococcu , and Clostridium sensu stricto all increased significantly. The ratio of Bacteroides to Firmicutes increased, and Bifidobacterium grew and multiplied. This study improves the utilization of mangosteen peel and provides a theoretical basis for the scientific evaluation of the antioxidant activity and gut microbiota modulation of mangosteen peel.
研究领域:
食品科学
·
微生物学
✓ 已验证
产品关联
DOI
高影响因子
Scientific Reports
·
2023
·Vol. 13
·期 1
·1-9
·
IF 4.6
Zhang Lijun,Liu Chuhe,Yin Liufang,Huang Cheng,Fan Shengjie
Hepatic fibrosis is a late stage process of many chronic liver diseases. Blocking the fibrosis process will be beneficial to the treatment and recovery of the diseases. Mangiferin has many pharmacological activities. Recently, it has been reported that mangiferin may relieve tissue fibrosis, including renal, myocardial, pulmonary fibrosis via anti-inflammatory and anti-oxidative effects in animal models. Here, we investigate the effects of mangiferin on CCl4-induced liver fibrosis and the underlying mechanism in mice. Thirty-two male C57BL/6 mice were randomly divided into 4 groups (n = 8 in each group), injected with carbon tetrachloride (10% CCl4) for 8 weeks, and oral administrated with mangiferin (50 mg/kg or 100 mg/kg) from the fifth week. The serum levels of ALT, AST were analyzed to evaluate liver function. H&E, Masson’s trichrome and Sirius red staining were used to assess liver morphology and the degree of liver fibrosis. Quantitative RT-PCR and Western blot were used to assay the gene expression and protein levels. The results showed that mangiferin alleviated the serum levels of AST, ALT, ALP, TBA and TBIL, reduced liver lesions, prevented hepatic parenchymal necrosis, and ameliorated collagen accumulation in the liver of CCl4-treated mice. Meanwhile, mangiferin inhibited the expression of inflammatory genes IL-6 and IL-1β, fibrogenic genes α-SMA, TGF-β and MMP-2 and bile acid metabolism genes ABCB4, ABCB11, SULT2A1 in the liver of CCl4-treated mice. Furthermore, mangiferin reduced collagen accumulation and HSCs activation, inhibited the p-IκB and p-p65 protein levels. Our results suggest that mangiferin could alleviate liver fibrosis in CCl4-treated mice through inhibiting NF-κB signaling, and mango consuming may have beneficial effects to hepatic fibrosis.
研究领域:
药理学
·
肝病学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Chemical Neuroscience
·
2023
·
IF 5
Hang Zhou,Zhang Mao,Xiaonan Zhang,Ruomiao Li,Jian Yin,Yinghui Xu
Parkinson’s disease (PD), known as a neurodegenerative disease, is characterized by movement disorders, with increasing age being the predominant risk factor for its development. Mangiferin, a bioactive compound isolated from mango, shows potent neuroprotection. In our work, we investigated the neuroprotection and mechanisms of mangiferin against PD. We established PD models by treating SH-SY5Y cells with rotenone and mice with 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and investigated the therapeutic effects of mangiferin. Our results showed that mangiferin exhibited a cell-protective effect. Mangiferin also improved the motor behavior and attenuated the activation of microglia and astrocytes in MPTP mice. In addition, mangiferin decreased reactive oxygen species (ROS) levels and increased glutathione (GSH) and superoxide dismutase (SOD). Mangiferin also markedly activated GIT1, p-ERK, Nrf2, HO-1, and SOD expression and inhibited Keap1 expression in vitro and in vivo. To further investigate the role of GIT1, GIT1 siRNA was used. In the presence of GIT1 siRNA, the neuroprotection of mangiferin in PD was weakened. Our results indicate that mangiferin exhibited its therapeutic effect against PD by regulating GIT1 and its downstream Keap1/Nrf2 pathways. Our studies exhibited that mangiferin showed neuroprotection in PD, and its main target was GIT1. What is more, mangiferin could reduce the oxidative stress of PD by targeting GIT1 and its downstream Keap1/Nrf2 pathways. These indicated that mangiferin is a good candidate for PD therapy. However, the role of p-ERK in mangiferin-treated PD requires further investigation.
研究领域:
神经科学
·
药理学
·
分子生物学
·
神经退行性疾病
✓ 已验证
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）