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Minhsiung Pan - One of the best experts on this subject based on the ideXlab platform.

  • a mixture of citrus Polymethoxyflavones green tea polyphenols and lychee extracts attenuates adipogenesis in 3t3 l1 adipocytes and obesity induced adipose inflammation in mice
    Food & Function, 2019
    Co-Authors: Minhsiung Pan, Meiling Tsai, Chih Yu Pan, Vladimir Badmaev, Ching Shu Lai
    Abstract:

    Adipocyte–macrophage interaction in obesity can cause adipose tissue inflammation and contribute to insulin resistance. Here, we investigated the effect of SlimTrym®—a formulated product containing citrus Polymethoxyflavones (PMFs), green tea extract, and lychee polyphenols—on 3T3-L1 adipocyte differentiation and obesity-induced inflammation. SlimTrym® inhibited mitotic clonal expansion (MCE) of 3T3-L1 adipocytes by inducing G1 cell cycle arrest via upregulation of p21 and p53. SlimTrym® attenuated adipogenic differentiation by downregulating adipogenic factors, such as CCAAT-enhancer-binding proteins (C/EBPs) and peroxisome proliferator-activated receptor γ (PPARγ), and upregulating AMP-activated protein kinase (AMPK). Pretreatment with compound C significantly reduced SlimTrym®-mediated suppression of lipid accumulation. SlimTrym® reduced the expression of pro-inflammatory cytokines, including monocyte chemoattractant protein 1 (MCP-1), interleukin (IL)-1β and IL-6, in co-cultured 3T3-L1 adipocytes and RAW264.7 macrophages. C57BL/6 mice administered with SlimTrym® for 16 weeks showed markedly reduced high-fat diet (HFD)-induced infiltration of monocytes/macrophages in adipose tissue; however, the level of M2 macrophage markers (CD163 and IL-10) was increased. Taken together, these findings indicate that SlimTrym® exerts both anti-adipogenic and anti-inflammatory effects, and can potentially treat obesity and adipose tissue inflammation.

  • combination of citrus Polymethoxyflavones green tea polyphenols and lychee extracts suppresses obesity and hepatic steatosis in high fat diet induced obese mice
    Molecular Nutrition & Food Research, 2017
    Co-Authors: Minhsiung Pan, Meiling Tsai, Vladimir Badmaev, Guliang Yang, Ching Shu Lai
    Abstract:

    cope SlimTrym® is a formulated product composed of citrus Polymethoxyflavones (PMFs), green tea extract and lychee extract. We investigated the effect of dietary SlimTrym® on diet-induced obesity and associated non-alcoholic fatty liver disease (NAFLD) in mice. Methods and results Male C57BL/6 mice were fed a normal diet (ND), high fat diet (HFD) or HFD containing 0.1% or 0.5% SlimTrym® for sixteen weeks. Dietary SlimTrym® significantly reduced weight gain and relative perigonadal, retroperitoneal, mesenteric fat weight as well as the size of adipocyte in HFD-fed mice. SlimTrym® supplementation also effectively diminished hepatic steatosis and the serum levels of glutamate oxaloacetate transaminase (GOT), glutamate pyruvate transaminase (GPT), triacylglycerol (TG) and total cholesterol (TCHO). Down-regulation of peroxisome proliferator-activated receptor (PPAR)γ, sterol regulatory element-binding protein (SREBP)-1, and the activation of AMP-activated protein kinase (AMPK) signaling by SlimTrym® in both adipose tissue and liver may be responsible for the observed anti-obesity effects. Conclusion SlimTrym® supplementation potentially diminished diet-induced obesity and hepatic steatosis via regulating AMPK signaling and molecules involved in lipid metabolism. This article is protected by copyright. All rights reserved

  • 5‑Demethylnobiletin and 5‑Acetoxy-6,7,8,3′,4′-pentamethoxyflavone Suppress Lipid Accumulation by Activating the LKB1-AMPK Pathway in 3T3-L1 Preadipocytes and High Fat Diet-Fed C57BL/6 Mice
    2016
    Co-Authors: Yen-chen Tung, Qingrong Huang, Wei-lun Hung, Guor-jien Wei, Minhsiung Pan
    Abstract:

    Polymethoxyflavones (PMFs) and hydroxylated Polymethoxyflavones (HPMFs), such as nobiletin (Nob) and 5-demethylnobiletin (5-OH-Nob), are unique flavonoids that are found exclusively in citrus peels. Nobiletin has been shown to suppress adipogenesis in vitro, but the antiadipogenic activity of 5-OH-Nob has not been investigated. Both nobiletin and 5-OH-Nob have poor aqueous solubility and low oral bioavailability. We employed chemical modification to produce the acetyl derivative of 5-OH-Nob, that is, 5-acetyloxy-6,7,8,3′,4′-pentamethoxyflavone (5-Ac-Nob), to improve its bioavailability and bioactive efficiency. We found that 5-Ac-Nob reduced triacylglycerol (TG) content to a greater extent than 5-OH-Nob in 3T3-L1 preadipocytes. Orally administered 5-Ac-Nob resulted in a significant reduction in body weight, intra-abdominal fat, plasma and liver TG levels, and plasma cholesterol level in high fat diet-induced obese male C57BL/6J mice. The 5-Ac-Nob treatment decreased lipid accumulation by triggering the adenosine 5′-monophosphate-activated protein kinase (AMPK) pathway to alter transcriptional factors or lipogenesis-related enzymes in vivo and in vitro

  • safety evaluation of tangeretin and the effect of using emulsion based delivery system oral acute and 28 day sub acute toxicity study using mice
    Food Research International, 2015
    Co-Authors: Yuwen Ting, Minhsiung Pan, Yishiou Chiou, Yike Jiang, Zhengyu Lin, Qingrong Huang
    Abstract:

    Polymethoxyflavones, found widely in the peel of citrus fruits, is an emerging group of bioactive compounds with wide arrays of disease prevention functionalities. To understand the potential oral toxicity, tangeretin, being one of the most abundant Polymethoxyflavones from natural sources, was used as model compound for the safety evaluation. Acute oral toxicity study was conducted using both male and female mice giving 1000, 2000, or 3000mg/kgbody weight (bw) of tangeretin in oil suspension from single gavage administration. No evidence of death was observed during 14-day post-administration period. Alterations of the hepatic cell and clinical chemistry profile increased dose dependently and exhibited distinct injury recovery pattern among different sexes. To determine the potential safety concern related to emulsification, the sub-acute toxicity of tangeretin in emulsion was evaluated and compared with un-processed oil suspension when conducting the sub-acute toxicity study over 28days. In the sub-acute study, emulsion system did not induce a significant increase of toxicity response. However, the daily low-dose application of tangeretin showed U-shaped dose-response pattern in regard to hepatic alteration. The result from this study can serve as a good safety reference for future application of polymethoxyflavone as a functional ingredient in food.

  • in vitro and in vivo anti cancer activity of tangeretin against colorectal cancer was enhanced by emulsion based delivery system
    Journal of Functional Foods, 2015
    Co-Authors: Yuwen Ting, Minhsiung Pan, Yishiou Chiou, Qingrong Huang
    Abstract:

    Abstract The oral bioavailability and efficacy of citrus polymethoxyflavone, tangeretin, was attenuated by its poor aqueous solubility. An emulsion-based delivery system was utilized to enhance the anti-tumourigenesis activity of tangeretin. The in vitro anti-proliferative activity of tangeretin was first evaluated using methyl thiazol tetrazolium bromide (MTT) test on colonic carcinoma cell lines, HCT116 and HT29. The utilization of emulsion system significantly improved the efficacy of tangeretin at dosing concentrations at 12.5 and 25 µM. The effectiveness of the emulsion system in enhancing the in vivo oral efficacy of tangeretin against colorectal cancer development was also evaluated by azoxymethane/dextran sodium sulphate (AOM/DSS)-induced colitis related colon tumourigenesis model. The tumour incidence, multiplicity, and pathological signs of colorectal adenoma were significantly reduced when tangeretin emulsion was applied. The regulation on tumourigenesis related protein expression was more effective in mice treated with tangeretin emulsion than unformulated suspension. Our finding indicated that emulsion-based delivery system was an effective means to increase the oral efficacy of tangeretin. This study is the first successful demonstration of the effect of delivery system on the oral efficacy of nutraceutical using long-term animal model.

Hang Xiao - One of the best experts on this subject based on the ideXlab platform.

  • Encapsulation of Polymethoxyflavones in Citrus Oil Emulsion-Based Delivery Systems.
    Journal of agricultural and food chemistry, 2017
    Co-Authors: Ying Yang, Zhao Chengying, Jingjing Chen, Tian Guifang, Hang Xiao, Jinkai Zheng
    Abstract:

    The purpose of this work was to elucidate the effects of citrus oil type on polymethoxyflavone (PMF) solubility and on the physicochemical properties of PMF-loaded emulsion-based delivery systems. Citrus oils were extracted from mandarin, orange, sweet orange, and bergamot. The major constituents were determined by GC/MS: sweet orange oil (97.4% d-limonene); mandarin oil (72.4% d-limonene); orange oil (67.2% d-limonene); and bergamot oil (34.6% linalyl acetate and 25.3% d-limonene). PMF-loaded emulsions were fabricated using 10% oil phase (containing 0.1% w/v nobiletin or tangeretin) and 90% aqueous phase (containing 1% w/v Tween 80) using high-pressure homogenization. Delivery systems prepared using mandarin oil had the largest mean droplet diameters (386 or 400 nm), followed by orange oil (338 or 390 nm), bergamot oil (129 or 133 nm), and sweet orange oil (122 or 126 nm) for nobiletin- or tangeretin-loaded emulsions, respectively. The optical clarity of the emulsions increased with decreasing droplet si...

  • enhanced lymphatic transport of bioactive lipids cell culture study of polymethoxyflavone incorporation into chylomicrons
    Food & Function, 2013
    Co-Authors: Mingfei Yao, Jingjing Chen, Jinkai Zheng, Mingyue Song, David Julian Mcclements, Hang Xiao
    Abstract:

    Polymethoxyflavones (PMFs) are bioactive flavonoids found in citrus fruits that have been shown to have potential health promoting properties. However, their application as nutraceuticals in functional foods and beverages is currently limited due to their low water solubility and high melting point. The oral bioavailability of lipophilic compounds can be enhanced by promoting their intestinal lymphatic transport through co-administration with digestible lipids. We investigated the effects of chylomicron-mediated intestinal lymphatic transport on the bioavailability of 5-hydroxy-6,7,8,3',4'-pentamethoxylflavone (5-HPMF), one of representative PMFs in Caco-2 cells. Our results demonstrated that oleic acid and bile acid promoted secretion of chylomicrons in Caco-2 cells, with mean diameter ranged from 70 to 150 nm. The intracellular level of 5-HPMF increased 3-fold by co-incubation with the mixed micelle solution. Moreover, the basolateral level of 5-HPMF increased 3-fold due to enhanced chylomicron-mediated transport. Overall, our results demonstrated for the first time that the bioavailability of Polymethoxyflavones can be enhanced by promoting their incorporation into chylomicrons.

  • nanoemulsion based delivery systems for poorly water soluble bioactive compounds influence of formulation parameters on polymethoxyflavone crystallization
    Food Hydrocolloids, 2012
    Co-Authors: Jinkai Zheng, Hang Xiao, David Julia Mcclements
    Abstract:

    Polymethoxyflavones (PMFs) extracted from citrus peel exhibit potent anti-cancer activity, but are highly hydrophobic molecules with poor solubility in both water and oil at ambient and body temperature, which limits their bioavailability. The possibility of encapsulating PMFs within nanoemulsion-based delivery systems to facilitate their application in nutraceutical and pharmaceutical products was investigated. The influence of oil type (corn oil, MCT, orange oil), emulsifier type (β-lactoglobulin, lyso-lecithin, Tween, and DTAB), and neutral cosolvents (glycerol and ethanol) on the formation and stability of PMF-loaded nanoemulsions was examined. Nanoemulsions (r < 100 nm) could be formed using high pressure homogenization for all emulsifier types, except DTAB. Lipid droplet charge could be altered from highly cationic (DTAB), to near neutral (Tween), to highly anionic (β-lactoglobulin, lyso-lecithin) by varying emulsifier type. PMF crystals formed in all nanoemulsions after preparation, which had a tendency to sediment during storage. The size, morphology, and aggregation of PMF crystals depended on preparation method, emulsifier type, oil type, and cosolvent addition. These results have important implications for the development of delivery systems for bioactive components that have poor oil and water solubility at application temperatures.

  • chemoprevention of colonic tumorigenesis by dietary hydroxylated Polymethoxyflavones in azoxymethane treated mice
    Molecular Nutrition & Food Research, 2011
    Co-Authors: Ching Shu Lai, Hang Xiao, Meiling Tsai, Anchin Cheng, Yu Wang, Ying Jan Wang, Minhsiung Pan
    Abstract:

    Scope: Hydroxylated Polymethoxyflavones (PMFs), existing exclusively in citrus genus, have been reported to exhibit a broad spectrum of biological activity. Here we investigated the chemopreventive effects and underlying molecular mechanisms of dietary administration of hydroxylated PMFs in an azoxymethane (AOM)-induced colonic tumorigenesis model. Methods and results: Male, Institute of Cancer Research (ICR), mice at age of 6 wk were injected with AOM twice weekly at a dose of 5 mg/kg for 2 wk and continuously fed control diet or diets containing 0.01 and 0.05% hydroxylated PMFs, respectively. Mice were then sacrificed at 6 and 20 wk, and colonic tissues were collected and examined. Hydroxylated PMFs feeding dose-dependently decreased the number of aberrant crypt foci in colonic tissues of mice. More importantly, we found that hydroxylated PMFs caused a strong reduction in numbers of large aberrant crypt foci and tumors in colonic tissue. Molecular analysis exhibited the anti-proliferative, anti-inflammatory, anti-angiogenic and pro-apoptotic activities of hydroxylated PMFs by significantly decreasing the levels of inducible nitric oxide synthase, cyclooxygenase, cyclin D1 and vascular endothelial growth factor through interfering with Wnt/β-catenin and epidermal growth factor receptor/Ras/mitogen-activated protein kinase signaling pathways as well as the activation of transcription factors NF-κB and STAT3 in colonic tissue, thus resulting in suppression of colonic tumorigenesis. Conclusion: Taken together, these results demonstrated for the first time the in vivo chemopreventive efficacy and molecular mechanisms of dietary hydroxylated PMFs against AOM-induced colonic tumorigenesis.

  • monodemethylated Polymethoxyflavones from sweet orange citrus sinensis peel inhibit growth of human lung cancer cells by apoptosis
    Molecular Nutrition & Food Research, 2009
    Co-Authors: Hang Xiao, Chung S Yang, Huanyu Jin, Trusha Patel
    Abstract:

    Polymethoxyflavones (PMFs) are almost exclusively found in the Citrus genus, particularly in the peels of sweet orange (Citrus sinensis L. Osbeck) and mandarin (C. reticulate Blanco). We studied the effects of two major PMFs, namely, nobiletin and 3,5,6,7,8,3',4'-heptamethoxyflavone (HMF), and two major monodemethylated PMFs, namely 5-hydroxy-3,7,8,3',4'-pentamethoxyflavone (5HPMF), and 5-hydroxy-3,6,7,8,3',4'-hexamethoxyflavone (5HHMF), on the growth of human lung cancer H1299, H441, and H460 cells. Monodemethylated PMFs were much more potent in growth inhibition of lung cancer cells than their permethoxylated counterpart PMFs. In H1299 cells, cell cycle analyses further revealed that monodemethylated PMFs caused significant increase in sub-G0/G1 phase, suggesting possible role of apoptosis in the growth inhibition observed, whereas the permethoxylated counterpart PMFs did not affect cell cycle distribution at same concentrations tested. These results strongly suggested that the phenolic group is essential for the growth inhibitory activity of monodemethylated PMFs. Further studies in H1299 cells demonstrated that monodemethylated PMFs downregulated oncogenic proteins, such as iNOS, COX-2, Mcl-1, and K-ras, as well as induced apoptosis evidenced by activation of caspase-3 and cleavage of PARP. Our results provide rationale to develop orange peel extract enriched with monodemethylated PMFs into value-added nutraceutical products for cancer prevention.

Yanjiang Qiao - One of the best experts on this subject based on the ideXlab platform.

  • rapid identification of polymethoxylated flavonoids in traditional chinese medicines with a practical strategy of stepwise mass defect filtering coupled to diagnostic product ions analysis based on a hybrid ltq orbitrap mass spectrometer
    Phytochemical Analysis, 2014
    Co-Authors: Jiayu Zhang, Fang Wang, Hong Zhang, Yanjiang Qiao
    Abstract:

    Introduction The methodology of stepwise mass defect filtering (MDF) approach coupled to diagnostic product ions (DPIs) analysis on a hybrid linear trap quadrupole (LTQ)/orbitrap mass spectrometer was the first to be established to screen and identify structural analogues from complex herbal extracts. Objective To develop an analytical methodology that could be adopted to screen and identify structural analogues in traditional Chinese medicines (TCMs) rapidly and accurately. Methods Taking polymethoxylated flavonoids (PMFs) in the leaves of Citrus reticulata Blanco as an example, high-resolution mass data were acquired by high-performance liquid chromatography (HPLC) coupled with a LTQ/orbitrap mass spectrometer. The stepwise MDF with multiple mass defect windows or mass windows enabled the original data to be analysed much faster and more accurately by reducing the potential interferences of matrix ions. Additionally, analysis of DPIs could provide a criterion to classify the target constituents detected into certain chemical families. Results In total, 81 PMFs, including 50 Polymethoxyflavones and 31 polymethoxyflavanones or polymethoxychalcones, were screened and identified from the original data and preliminarily identified. Conclusion The analytical methodology developed could be used as a rapid, effective technique to screen and identify compounds from TCM extracts and other organic matter mixtures with compounds that can also be classified into families based on the common carbon skeletons. Copyright © 2014 John Wiley & Sons, Ltd.

  • rapid screening and identification of target constituents using full scan parent ions list dynamic exclusion acquisition coupled to diagnostic product ions analysis on a hybrid ltq orbitrap mass spectrometer
    Talanta, 2014
    Co-Authors: Jiayu Zhang, Fang Wang, Zijian Wang, Qian Zhang, Zhaozhou Lin, Yanjiang Qiao
    Abstract:

    A highly sensitive and effective strategy for rapid screening and identification of target constituents has been developed using full scan-parent ions list-dynamic exclusion (FS-PIL-DE) acquisition coupled to diagnostic product ions (DPIs) analysis on a hybrid LTQ-Orbitrap mass spectrometer. The FS-PIL-DE was adopted as a survey scan to trigger the MS/MS acquisition of all the predictable constituents contained in traditional Chinese medicines. Additionally, DPIs analysis can provide a criterion to judge the target constituents detected into certain chemical families. Results from analyzing polymethoxylated flavonoids (PMFs) in the leaves of Citrus reticulata Blanco demonstrated that FS-PIL-DE was capable of targeting a greater number of constituents than FS, FS-PIL and FS-DE, thereby increasing the coverage of constituent screening. As a result, 135 PMFs including 81 Polymethoxyflavones, 54 polymethoxyflavanones or polymethoxychalcones were identified preliminarily. And this was the first time to systematically report the presence of PMFs in the leaves of Citrus reticulata Blanco, especially for polymethoxylated flavanones and chalcones, most of which were new compounds. The results indicated that the developed FS-PIL-DE coupled to DPIs analysis methodology could be employed as a rapid, effective technique to screen and identify target constituents from TCMs extracts and other organic matter mixtures whose compounds contained can also be classified into families based on the common carbon skeletons.

Jaehong Han - One of the best experts on this subject based on the ideXlab platform.

  • demethylation of Polymethoxyflavones by human gut bacterium blautia sp mrg pmf1
    Journal of Agricultural and Food Chemistry, 2017
    Co-Authors: Supawadee Burapan, Mihyang Kim, Jaehong Han
    Abstract:

    Polymethoxyflavones (PMFs) were biotransformed to various demethylated metabolites in the human intestine by the PMF-metabolizing bacterium, Blautia sp. MRG-PMF1. Because the newly formed metabolites can have different biological activities, the pathways and regioselectivity of PMF bioconversion were investigated. Using an anaerobic in vitro study, 12 PMFs, 5,7-dimethoxyflavone (5,7-DMF), 5-hydroxy-7-methoxyflavone (5-OH-7-MF), 3,5,7-trimethoxyflavone (3,5,7-TMF), 5-hydroxy-3,7-dimethoxyflavone (5-OH-3,7-DMF), 5,7,4′-trimethoxyflavone (5,7,4′-TMF), 5-hydroxy-7,4′-dimethoxyflavone (5-OH-7,4′-DMF), 3,5,7,4′-tetramethoxyflavone (3,5,7,4′-TMF), 5-hydroxy-3,7,4′-trimethoxyflavone (5-OH-3,7,4′-TMF), 5,7,3′,4′-tetramethoxyflavone (5,7,3′,4′-TMF), 3,5,7,3′,4′-pentamethoxyflavone (3,5,7,3′,4′-PMF), 5-hydroxy-3,7,3′,4′-tetramethoxyflavone (5-OH-3,7,3′,4′-TMF), and 5,3′-dihydroxy-3,7,4′-trimethoxyflavone (5,3′-diOH-3,7,4′-TMF), were converted to chrysin, apigenin, galangin, kaempferol, luteolin, and quercetin after ...

  • Demethylation of Polymethoxyflavones by Human Gut Bacterium, Blautia sp. MRG-PMF1
    2017
    Co-Authors: Supawadee Burapan, Mihyang Kim, Jaehong Han
    Abstract:

    Polymethoxyflavones (PMFs) were biotransformed to various demethylated metabolites in the human intestine by the PMF-metabolizing bacterium, Blautia sp. MRG-PMF1. Because the newly formed metabolites can have different biological activities, the pathways and regioselectivity of PMF bioconversion were investigated. Using an anaerobic in vitro study, 12 PMFs, 5,7-dimethoxyflavone (5,7-DMF), 5-hydroxy-7-methoxyflavone (5-OH-7-MF), 3,5,7-trimethoxyflavone (3,5,7-TMF), 5-hydroxy-3,7-dimethoxyflavone (5-OH-3,7-DMF), 5,7,4′-trimethoxyflavone (5,7,4′-TMF), 5-hydroxy-7,4′-dimethoxyflavone (5-OH-7,4′-DMF), 3,5,7,4′-tetramethoxyflavone (3,5,7,4′-TMF), 5-hydroxy-3,7,4′-trimethoxyflavone (5-OH-3,7,4′-TMF), 5,7,3′,4′-tetramethoxyflavone (5,7,3′,4′-TMF), 3,5,7,3′,4′-pentamethoxyflavone (3,5,7,3′,4′-PMF), 5-hydroxy-3,7,3′,4′-tetramethoxyflavone (5-OH-3,7,3′,4′-TMF), and 5,3′-dihydroxy-3,7,4′-trimethoxyflavone (5,3′-diOH-3,7,4′-TMF), were converted to chrysin, apigenin, galangin, kaempferol, luteolin, and quercetin after complete demethylation. The time-course monitoring of PMF biotransformations elucidated bioconversion pathways, including the identification of metabolic intermediates. As a robust flavonoid demethylase, regioselectivity of PMF demethylation generally followed the order C-7 > C-4′ ≈ C-3′ > C-5 > C-3. PMF demethylase in the MRG-PMF1 strain was suggested as a Co-corrinoid methyltransferase system, and this was supported by the experiments utilizing other methyl aryl ether substrates and inhibitors

E-hu Liu - One of the best experts on this subject based on the ideXlab platform.

  • Citrus Polymethoxyflavones attenuate metabolic syndrome by regulating gut microbiome and amino acid metabolism.
    Science advances, 2020
    Co-Authors: Su-ling Zeng, Ping-ting Xiao, Yuan-yuan Cai, Chu Chu, Bai-zhong Chen, E-hu Liu
    Abstract:

    Metabolic syndrome (MetS) is intricately linked to dysregulation of gut microbiota and host metabolomes. Here, we first find that a purified citrus polymethoxyflavone-rich extract (PMFE) potently ameliorates high-fat diet (HFD)-induced MetS, alleviates gut dysbiosis, and regulates branched-chain amino acid (BCAA) metabolism using 16S rDNA amplicon sequencing and metabolomic profiling. The metabolic protective effects of PMFE are gut microbiota dependent, as demonstrated by antibiotic treatment and fecal microbiome transplantation (FMT). The modulation of gut microbiota altered BCAA levels in the host serum and feces, which were significantly associated with metabolic features and actively responsive to therapeutic interventions with PMFE. Notably, PMFE greatly enriched the commensal bacterium Bacteroides ovatus, and gavage with B. ovatus reduced BCAA concentrations and alleviated MetS in HFD mice. PMFE may be used as a prebiotic agent to attenuate MetS, and target-specific microbial species may have unique therapeutic promise for metabolic diseases.

  • enrichment of Polymethoxyflavones from citrus reticulata chachi peels and their hypolipidemic effect
    Journal of Chromatography A, 2019
    Co-Authors: Zhao Gao, Guodong Zheng, Chu Chu, Ziyuan Wang, Yong Guo, E-hu Liu
    Abstract:

    In the present study, a simple and efficient method based on orthogonal experimental design and macroporous resin chromatography was established for the first time for enrichment of Polymethoxyflavones (PMFs) from the peels of Citrus reticulata ‘Chachi’ (CRC). The optimum conditions of extraction and enrichment process were as follows: use of a liquid to solid ratio of 1 to 14, two-hour extraction time repeated twice with 70% ethanol; use of HPD-450 macroporous resin, wash solvent of purified water and 25% aqueous ethanol, and 70% aqueous ethanol as desorption solvent. The purity of PMFs in the resulting extract reached 62.26%. Our data indicate that the PMFs purified could potently alleviate high-fat diet-induced hyperlipidaemia. The PMFs were nontoxic as determined by acute toxicity test. The method established was suitable for large-scale separation of PMFs from CRC peels and the PMFs might be developed as an anti-hyperlipidaemia agent or dietary supplement.

  • Polymethoxyflavones in peel of citrus reticulata chachi and their biological activities
    Food Chemistry, 2017
    Co-Authors: Li Duan, Lili Dou, Long Guo, Chen Baizhong, E-hu Liu
    Abstract:

    Citrus Polymethoxyflavones (PMFs) have been of increasing interest due to their extensive biological activities. In the present study, a total of eight PMFs were isolated from the peel of Citrus reticulata ‘Chachi’ (CRC). They were individually identified as 5-hydroxy-6,7,8,4′-tetramethoxyflavone (1), 5,6,7,3′,4′-pentamethoxyflavanone (2), 5-hydroxy-6,7,8,3′,4′-pentamethoxyflavone (3), 3,5,6,7,8,3′,4′- heptamethoxyflavone (4), 5,6,7,8,3′,4′-hexamethoxyflavone (5), 5,6,7,8,4′-pentamethoxyflavone (6), 6,7,8,3′,4′-pentamethoxyflavanone (7) and 5,6,7,3′,4′-pentamethoxyflavone (8) by nuclear magnetic resonance and mass spectroscopic analysis. 6,7,8,3′,4′-Pentamethoxyflavanone was isolated from the peel of CRC for the first time. The content of PMFs was firstly quantified in both the peel of CRC and PMF-rich extract by HPLC analysis. Furthermore, the biological activities of PMF compounds were investigated. 3,5,6,7,8,3′,4′-Heptamethoxyflavone demonstrated potent sterol regulatory element-binding proteins inhibition activity and 5-hydroxy-6,7,8,3′,4′-pentamethoxyflavone exhibited strong antiproliferative activity against tumor cell lines. The isolated PMF compounds could also significantly inhibit NO production and the effect varied mainly depending on the number of methoxy groups.