JOURNAL OF FOOD SCIENCE
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2025
·Vol. 90
·期 4
·e70162
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IF 3.4
Lu Zhang,Mei Deng,Qinghui Wen,Yutong Xie,Qiao Ding,Xing Xie,Quanyuan Xie,Mingshun Chen
Nowadays, obesity is a global health risk factor, and its development is closely related to the absorption and metabolism of lipids. In this study, the main chemical constituents and antiobesity effect of Artemisia selengensis Turcz extract (ASTE) were investigated by HPLC-QTOF-MS 2 and obese mice models. Twenty-three compounds were identified from ASTE, and caffeoylquinic acid and dicaffeoylquinic acid are the dominant bioactive compounds. ASTE administration reduced body weight (9.8%), improved glucose tolerance (14.2%), corrected dyslipidemia (the levels of total cholesterol, total triglyceride, and low-density lipoprotein cholesterol dropped by 19.8%, 24.4%, and 27.2%, respectively, and the high-density lipoprotein cholesterol level rose by 27.6%), and alleviated hepatic lipid accumulation. ASTE improved the gut microbiota dysbiosis caused by High-Fat Diet (HFD), mainly by increasing the relative abundance of Odoribacter , Candidatus_Saccharimonas , Bacteroides , and unclassified_f__Lachnospiraceae , and reducing the relative abundance of Faecalibaculum . Gene expression heatmaps and pathway enrichment analyses based on transcriptomics indicated that ASTE significantly reduced HFD-induced increases in fatty acid uptake, triglyceride synthesis, and cholesterol synthesis. Our findings indicated that ASTE holds significant potential as a candidate for modulating lipid metabolism and preventing or treating obesity, meriting further investigation.
研究领域:
营养学
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药理学
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微生物学
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DOI
PubMed
高影响因子
CARBOHYDRATE POLYMERS
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2020
·
IF 7.182
Xue Zhang,Pei Hu,Xiaorui Zhang,Xiaojun Li
ABSTRACT A neutral polysaccharide (LCPS) was obtained from Lobelia chinensis via hot water extraction and ethanol precipitation. After separation and purification, the homogeneous polysaccharide was obtained with a molecular weight of 2.6 × 10 3 Da. The chemical composition of the extracted polysaccharide contains fructose and glucose with protein-free identified by gas chromatography-mass spectrometer (GC-MS) method. Chemical structure of LCPS was indicated by nuclear magnetic resonance (NMR) spectroscopy. Data indicated that LCPS was an inulin-type fructan with α-D-Glc p -(1→[1)-β-D-Fru f -(2] 15 linkage. LCPS intake reduced at significant level high fat diet (HFD)-induced body weight gain, liver weight, total cholesterol and triglyceride in serum and hepatic tissue, respectively. The lipid droplet accumulation in hepatic tissue was similar between lean and LCPS groups lower than in HFD-induced mice from tissue section staining results. Together, polysaccharides from Lobelia chinensis could be a new source of natural anti-obesity agent against obesity with potential value in the manufacturing supplements and drugs.
研究领域:
植物化学
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营养学
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代谢研究
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产品关联
DOI
PubMed
高影响因子
Journal of Advanced Research
·
2024
·
IF 11.4
Sijia Lu,Quanxin Jiang,Peihui Zhou,Limin Yin,Ning Wang,Junting Xu,Qiqi Qian,Mijia Tao,Hanrui Yin,Liu Han,Yunqing Gu,Fei Gao,Junli Liu,Suzhen Chen
Introduction Promoting adipose thermogenesis is considered as a promising therapeutic intervention in obesity. However, endeavors to develop anti-obesity medications by targeting the canonical thermogenesis regulatory pathway, particularly β3-adrenergic receptor (β3-AR)-dependent mechanism, have failed due to the off-target effects of β3-AR agonists, exacerbating the risk of cardiovascular disease. Hyperforin (HPF), a natural compound extracted from the traditional herbal St. John’s Wort, binds to Dihydrolipoamide s-acetyltransferase (Dlat) and exerts effective anti-obesity properties through promoting adipose thermogenesis. Objectives The objective of this study was to investigate the oral efficacy and pharmacokinetics profile of HPF, and explore the detailed mechanism by which Dlat modulates HPF-mediated adipose thermogenesis. Methods To assess the anti-obesity efficacy of orally administered HPF in vivo , Dlat heterozygous knockout (Dlat +/- ) mice and wild-type (WT) mice, both fed a high-fat diet (HFD), underwent a validation process that involved the use of metabolic cages, NMR analysis, and infrared imaging. Sprague Dawley rats were employed to determine the pharmacokinetic parameters of HPF. Seahorse assays, JC-1 staining, qPCR, and immunoblotting were performed to evaluate cellular thermogenic efficacy of HPF and Dlat in vitro . Results Our study uncovered a non-canonical thermogenesis pathway involving Dlat, transient receptor potential vanilloid 3 (Trpv3, a calcium channel) and AMPK. Dlat interacted with Trpv3 to activate it, resulting in an increase in intracellular calcium (Ca 2+ ) and the activation of Camkkβ. Camkkβ then stimulated AMPK, leading to elevated Ucp1 expression and initiating adipose thermogenesis. HPF promoted thermogenesis in adipose tissues through enhancing the Dlat-Trpv3 interaction independently of β3-AR, causing minimal cardiac side effects. Notably, HPF’s thermogenic effects were reduced in Dlat +/- mice. Moreover, HPF exerted favorable oral bioavailability, a relatively long half-life, and extensive distribution within adipose tissues. Conclusion In summary, our study demonstrates that HPF targets a novel mechanism for promoting adipose thermogenesis and exhibits potent and safe anti-obesity efficacy.
研究领域:
药理学
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分子生物学
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代谢
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DOI
PubMed
高影响因子
MOLECULES
·
2022
·Vol. 27
·期 12
·3709
·
IF 4.927
Shi-Hui Lu,Jing Huang,Hao-Jiang Zuo,Zhong-Bo Zhou,Cai-Yan Yang,Zu-Liang Huang
The leaves ofLigustrum robustumhave been applied as Ku-Ding-Cha, a functional tea to clear heat, remove toxins, and treat obesity and diabetes, in Southwest China. The phytochemical research on the leaves ofL. robustumled to the isolation and identification of eight new monoterpenoid glycosides (1–8) and three known monoterpenoid glycosides (9–11). Compounds1–11were tested for the inhibitory activities on fatty acid synthase (FAS),α-glucosidase,α-amylase, and the antioxidant effects. Compound2showed stronger FAS inhibitory activity (IC50: 2.36 ± 0.10 μM) than the positive control orlistat (IC50: 4.46 ± 0.13 μM), while compounds1,2,5and11displayed more potent ABTS radical scavenging activity (IC50: 6.91 ± 0.10~9.41 ± 0.22 μM) than the positive control L-(+)-ascorbic acid (IC50: 10.06 ± 0.19 μM). This study provided a theoretical basis for the leaves ofL. robustumas a functional tea to treat obesity.Keywords:Ligustrum robustum;monoterpenoid glycoside;FAS;α-glucosidase;antioxidant;anti-obesity;hypoglycemic
研究领域:
植物化学
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药理学
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生物活性研究
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PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2020
·
IF 4.192
Suwen Liu,Xuedong Chang,Jincheng Yu,Weifeng Xu
This study aimed to determine the anti-obesity effects and mechanisms of Cerasus humilis polyphenol (CHP) in C57BL/6 obese mice and 3T3-L1 cells. High-performance liquid chromatography–electrospray ionization-tandem mass spectrometry was used for the qualitative and quantitative identification of CHP components. The obese mice, induced by feeding high-fat diet (HFD), were treated with CHP (250 mg/kg/day) by gavage for 12 weeks. Orlistat was gavaged at 15.6 mg/kg bw/day, as a positive control group. The analysis revealed that the main components of CHP were procyanidin B2, cyanidin-3-glucoside, and pelargonidin-3-glucoside. CHP dietary supplementation significantly reduced body weight and improved blood lipid measurements in HFD-fed mice (p < 0.01). Moreover, it inhibited mRNA expression of miR-122, Srebp-1c, and Cpt1a (p < 0.01) and reduced hepatic lipid deposition, as seen by hematoxylin and eosin staining. CHP downregulated the protein expression of PPARγ and C/EBPα in HFD-induced obese mice and inhibited adipocyte differentiation (p < 0.01). Compared with the HFD group, CHP supplementation had an obvious anti-inflammatory effect (decreased protein expression, such as TNF-α, IL-6, and MCP1), reducing leptin levels and TNF-α secretion in serum and cells (p < 0.01). CHP significantly inhibited the expression of miR-27a/b (53.3 and 29.9%, p < 0.01) in mice retroperitoneal white adipocytes, enhancing the expression of the target gene Prdm16 and significantly upregulating Sirt1 (105.5%, p < 0.01) compared with the HFD group. Moreover, CHP supplementation effectively improved oxidative stress (ROS, T-AOC, SOD, CAT, and GSH-Px) induced by HFD in obese mice (p < 0.01). Thus, CHP mitigates adipocyte differentiation, browning of white adipocytes, and reduction of inflammation and antioxidant activity to reduce obesity. Consequently, these results provide novel insights into the anti-obesity roles of CHP in HFD-induced obesity.
研究领域:
营养学
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药理学
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分子生物学
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PubMed
高影响因子
FOOD CHEMISTRY
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2020
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IF 6.306
Jinhong Wu,Qiaoyu Wu,Danlu Yang,Mi Zhou,Jingshen Xu,Qing Wen,Yan Cui,Yalong Bai,Shannan Xu,Zhengwu Wang,Shaoyun Wang
Patatin, the major protein found in potatoes, was purified and shows several isoforms. The essential amino acid content of patatin was as high as 76%, indicating that it is a valuable protein source. Patatin was an O-linked glycoprotein that contained fucose monosaccharides, as well as mannose, rhamnose, glucose, galactose, xylose, and arabinose. Patatin had a fucosylated glycan structural feature, which strongly bound AAL ( Aleuria aurantia Leukoagglutinin), a known fucose binding lectin. Moreover, the lipid metabolism regulatory effects of patatin on the fat catabolism, fat absorption, and inhibition of lipase activity were measured after high-fat feeding of zebrafish larvae. Results revealed that 37.0 μg/mL patatin promoted 23% lipid decomposition metabolism. Meanwhile patatin could inhibite lipase activity and fat absorption, whose effects accounted for half that of a positive control drug. Our findings suggest that patatin, a fucosylated glycoprotein, could potentially be used as a natural active constituent with anti-obesity effects.
研究领域:
营养学
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生物化学
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分子生物学
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PubMed
高影响因子
Food Science & Nutrition
·
2025
·Vol. 13
·期 9
·e70881
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IF 3.8
Zhuohui Luo,Zaibin Xu,Kongyan Wang,Huiyu Hu,Jiawen Huang
Citri Sarcodactylis Fructus (CSF), an ornamental and edible fruit belonging to the genus Citrus in the Rutaceae family, has been shown to exhibit anti‐inflammatory, antioxidant, and anti‐obesity effects. However, its impact on the progression of acute lung injury (ALI) remains unclear. In this study, CSF significantly alleviated LPS‐induced pulmonary edema in ALI mice and improved oxidative stress markers, as evidenced by reduced serum malondialdehyde (MDA) levels and increased serum superoxide dismutase (SOD) levels. It also decreased macrophage and neutrophil counts as well as protein levels in bronchoalveolar lavage fluid (BALF), and inhibited inflammatory responses‐specifically, it reduced the protein and gene expression of IL1β, IL6, and TNF‐α in lung tissues, downregulated the mRNA levels of chemokines, and suppressed LPS‐induced activation of NF‐κB signaling. Moreover, CSF significantly reduced NLRP3 inflammasome activation. The components of CSF exhibit high binding activity and stability to NF‐κB p65 or NLRP3, along with low binding free energy, within their respective binding pockets. This study reveals that CSF alleviates LPS‐induced ALI by inhibiting NF‐κB signaling and NLRP3 inflammasome activation‐mediated inflammatory response, thereby providing a scientific basis for the utilization of CSF resources. Citri Sarcodactylis Fructus (CSF) has been shown to exhibit anti‐inflammatory, antioxidant, and anti‐obesity effects. However, its impact on the progression of acute lung injury (ALI) remains unclear. This study reveals that CSF alleviates LPS‐induced ALI by inhibiting NF‐κB signaling and NLRP3 inflammasome activation‐mediated inflammatory response, thereby providing a scientific basis for the utilization of CSF resources.
研究领域:
药理学
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免疫学
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植物学
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分子生物学
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呼吸系统疾病
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DOI
PubMed
高影响因子
Food Bioscience
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2021
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IF 4.24
Fuqiang Liang,Yumeng Shi,Weiwei Cao,Jiayi Shi
This study aimed to elucidate the inhibition mechanism of apigenin against porcine pancreatic lipase (PPL), and, moreover, to comprehensively reveal the molecular basis of its anti-obesity via network pharmacology approach. The results showed that apigenin inhibited PPL with an IC 50 value of 0.377 ± 0.041 mM. Spectroscopic techniques combined molecular docking suggested that apigenin could bind into the PPL active pocket, affecting its normal spatial conformation. Moreover, molecular dynamic (MD) simulations revealed that the open conformation of PPL tended to transit to the closed in the presence of apigenin, which might one important reason for the inhibition of PPL catalytic ability. Network pharmacology analysis revealed that a total of 49 proteins could be identified as potential targets for the anti-obesity effects of apigenin. According to the protein-protein interaction (PPI) network analysis, six hub targets were extracted including IGF1 , ESR1, MMP9 , PPARA , MAPK14 and NR3C1. Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment indicated that the 49 potential targets could be mapped to 30 pathways (p<0.05). Among them, PI3K-Akt signaling pathway and insulin resistance can be considered as two major pathways regulated by apigenin. Further docking studies indicated that apigenin can bind into the binding pocket of the six hub target proteins identified according to the PPI network. The results indicated that in addition to inhibiting PPL, apigenin could exhibit anti-obesity benefit through the molecular mechanisms uncovered by network pharmacology. This study proposes a new strategy to reveal the mechanisms of dietary polyphenols at the level of network pharmacology.
研究领域:
药理学
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分子生物学
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生物信息学
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高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2022
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IF 8.025
Weihong Jing,Mingyue Jiang,Xiaoxue Fu,Jiaxin Yang,Lu Chen,Feng Leng,Ping Xu,Wenyan Huang,Chao Yu,Zhangyou Yang
Nonalcoholic fatty liver disease (NAFLD) is a chronic metabolic liver disease closely related to obesity, which has become a global health problem. However, current pharmacological therapies for NAFLD are limited by potential side effects, low effectiveness and poor aqueous solubility. Herein, we designed functionalized drug-albumin nanocomposites ( [email protected] NPs), which were prepared by self-assembly of the anti-obesity small-molecule drug (BAM15) and bovine serum albumin (BSA), for treatment of NAFLD. The proposed [email protected] NPs not only improve aqueous solubility and half-life of BAM15 but also exhibit hepatic-targeted capacity and an increased therapeutic efficacy. In vitro experiments revealed that [email protected] NPs possessed excellent biocompatibility, and improved resistance to adipogenesis and reduced lipid accumulation in human hepatocellular carcinoma cells. In vivo , [email protected] NPs showed liver targeting ability and powerful anti-obesity effects without altering body temperature or affecting food intake, and could effectively alleviate hepatic steatosis and improve therapeutic efficacy for NAFLD treatment. The above findings demonstrated that [email protected] NPs potentially served as a safe and effective drug for NAFLD treatment.
研究领域:
药理学
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纳米技术
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肝病学
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代谢疾病
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产品关联
DOI
PubMed
高影响因子
BIOORGANIC CHEMISTRY
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2024
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IF 4.5
Jiao Li,Chao-Feng Qin,Nai-Dong Chen
Phenylpropanoids (PPs), a group of natural compounds characterized by one or more C6-C3 units, have exhibited considerable potential in addressing metabolic disease. However, the comprehensive investigation on the relationship of compound structures and involved activity, along with the action mechanisms on the drug target is absent. This study aimed to evaluate the antioxidant and inhibitory activities of 16 PPs against two digestive enzymes, including α-glucosidase and pancreatic lipase, explore the structure–activity relationships and elucidate the mechanisms underlying enzyme inhibition. The findings revealed the similarities in the rules governing antioxidant and enzyme inhibitory activities of PPs. Specifically, the introduction of hydroxyl groups generally exerted positive effects on the activities, while the further methoxylation and glycosylation were observed to be unfavorable. Among the studied PPs, esculetin exhibited the most potent antioxidant activity and dual enzymes inhibition potential, displaying IC 50 values of 0.017 and 0.0428 mM for DPPH and ABTS radicals scavenging, as well as 1.36 and 6.67 mM for α-glucosidase and lipase inhibition, respectively. Quantification analysis indicated esculetin bound on both α-glucosidase and lipase successfully by a mixed-type mode. Further analyses by UV–Vis, FT-IR, fluorescence spectra, surface hydrophobicity, SEM, and molecular docking elucidated that esculetin could bind on the catalytic or non-catalytic sites of enzymes to form complex, impacting the normal spatial conformation for hydrolyzing the substrate, thus exhibiting the weakened activity. These results may shed light on the utilization value of natural PPs for the management of hyperglycemia and hyperlipemia, and afford the theoretical basis for designing drugs with stronger inhibition against the dual digestive enzymes based on esculetin.
研究领域:
药理学
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生物化学
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分子生物学
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营养学
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产品关联
DOI
PubMed
高影响因子
MOLECULES
·
2023
·Vol. 28
·期 1
·362
·
IF 4.6
Shi-Hui Lu,Hao-Jiang Zuo,Jing Huang,Wei-Neng Li,Jie-Lian Huang,Xiu-Xia Li
The leaves ofLigustrum robustumhave been consumed as Ku-Ding-Cha for clearing heat and removing toxins, and they have been used as a folk medicine for curing hypertension, diabetes, and obesity in China. The phytochemical research on the leaves ofL. robustumled to the isolation and identification of two new hexenol glycosides, two new butenol glycosides, and five new sugar esters, named ligurobustosides X (1a), X1(1b), Y (2a), and Y1(2b) and ligurobustates A (3a), B (3b), C (4b), D (5a), and E (5b), along with seven known compounds (4aand6–10). Compounds1–10were tested for their inhibitory effects on fatty acid synthase (FAS), α-glucosidase, and α-amylase, as well as their antioxidant activities. Compound2showed strong FAS inhibitory activity (IC504.10 ± 0.12 μM) close to that of the positive control orlistat (IC504.46 ± 0.13 μM); compounds7and9revealed moderate α-glucosidase inhibitory activities; compounds1–10showed moderate α-amylase inhibitory activities; and compounds1and10displayed stronger 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) ammonium salt (ABTS) radical scavenging effects (IC503.41 ± 0.08~5.65 ± 0.19 μM) than the positive controll-(+)-ascorbic acid (IC5010.06 ± 0.19 μM). This study provides a theoretical foundation for the leaves ofL. robustumas a functional tea to prevent diabetes and its complications.Keywords:Ligustrum robustum;hexenol glycoside;butenol glycoside;sugar ester;FAS;α-glucosidase;antioxidant;antiobesity;hypoglycemic
研究领域:
植物化学
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药理学
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代谢疾病研究
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
·
2022
·Vol. 103
·期 8
·3840-3849
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IF 4.125
Ying You,Haoran Song,Linlin Wang,Zhengqi Liu,Xiaoming Guo,Chunqing Ai,Shuang Song,Beiwei Zhu
BACKGROUND Caulerpa lentillifera has received extensive attention regarding expansion of its farming and increasing consumption. In our previous study, the structure of C. lentillifera polysaccharide (CLP) was elucidated. However, little information is available about its health effects. In this study, the anti-obesity effect of CLP was investigated by using a high-fat diet-induced obese mice model with two different supplementation methods. RESULTS In vitro simulated digestion results showed that CLP significantly decreased the lipid digestibility and induced the lipid droplets aggregation in the intestinal stage to inhibit the absorption of lipids. As revealed by 16S ribosomal RNA sequencing and non-targeted metabolomics, supplement of CLP by both pre-prandial gavage and free feeding patterns effectively prevented mice obesity via ameliorating intestinal flora disturbance and regulating bile acids circulation metabolism. Of note was that CLP administration had no effect on short-chain fatty acids production, suggesting the anti-obesity effect was uncorrelated with their production. Moreover, pre-prandial administration of CLP had a better anti-obesity effect in lowering body weight and serum lipid levels, but the free feeding resulted in a higher α -diversity of gut microbiota. CONCLUSION The findings of this study indicate that CLP could be a potential anti-obesity nutraceutical and that pre-prandial supplement of CLP may be a better intake method to exhibit its hypolipidemic effect. © 2022 Society of Chemical Industry.
研究领域:
营养学
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药理学
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微生物学
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代谢组学
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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）