INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2025
·Vol. 26
·期 9
·4266
·
IF 4.9
Fumin Xue,Xinyue Yuan,Xingyi Li,Shimin Fang,Yan Cheng
Improving the stability of drugs in the solid state, as well as improving their solubility and poor bioavailability, is highly physiologically relevant. In this study, we focused on enhancing the solubility of hypoxanthine (HYP) through salt formation resulting from the preparation of hypoxanthine–maleic acid salt (HYP-MAL). Single crystals were obtained through solvent evaporation methods, and DSC, TGA, PXRD, FT-IR, and1H NMR spectra were used to characterize the samples. The salt system had higher solubility properties than HYP, with an equilibrium solubility in water that was roughly 2.4 times greater than that of HYP, but the salt’s equilibrium solubility increased when the pH shifted from 7.4 to 1.2; additionally, from 0 to 10 min, the powder dissolution rate was 1.8 times that of HYP, resulting in increased bioavailability. The anti-obesity impact of HYP-MAL salt on obese mice was investigated, providing important insights for the development of future weight-loss medications.
研究领域:
药学
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生物化学
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药物开发
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DOI
PubMed
高影响因子
MICROCHEMICAL JOURNAL
·
2019
·
IF 3.206
Yanmei Shi,Kai Hu,Yongxia Cui,Jiamin Cheng,Wenjie Zhao,Xiumin Li
A magnetic triptycene-based CTF (M-CTF-TPC) has been synthesized by a covalent bonding method, and was characterized by scanning electron microscopy, transmission electron microscopy , X-ray diffraction, and nitrogen adsorption-desorption isotherms. The M-CTF-TPC exhibits the properties of high porosity, large surface area and strong magnetism. The extraction conditions were optimized, and a novel method coupled with magnetic solid phase extraction (MSPE) and ultra-performance liquid chromatographic analysis-fluorescence detection (UHPLC-FLD) was established the analysis of anthraquinones . The enrichment factors for the proposed method were 72.8–88.6, and the limits of detection for the five anthraquinones were found to be in the range of 0.010–0.077 μg g −1 . The proposed method was applied to the determination of anthraquinones in slimming tea with satisfactory recoveries (94.5–105.4%) and lower RSDs (3.0–5.8%), demonstrating its excellent accuracy. These results suggest that the promising potential of M-CTF-TPC as sorbent in sample pretreatment.
研究领域:
分析化学
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材料科学
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DOI
高影响因子
MOLECULES
·
2022
·Vol. 27
·期 21
·7390
·
IF 4.927
Shi-Hui Lu,Hao-Jiang Zuo,Jing Huang,Ran Chen,Jia-Ping Pan,Xiu-Xia Li
The phytochemical study on the leaves ofLigustrum robustum, which have been used as Ku-Ding-Cha, led to the isolation and identification of three new phenylethanoid glycosides and three new phenylmethanoid glycosides, named ligurobustosides R1(1b), R2–3(2), R4(3), S1(4b), S2(5), and S3(6), and five reported phenylethanoid glycosides (7–11). In the bioactivity test, (Z)-osmanthuside B6(11) displayed strong fatty acid synthase (FAS) inhibitory activity (IC50: 4.55 ± 0.35 μM) as the positive control orlistat (IC50: 4.46 ± 0.13 μM), while ligurobustosides R4(3) and S2(5), ligupurpuroside B (7),cis-ligupurpuroside B (8), ligurobustoside N (9), osmanthuside D (10), and (Z)-osmanthuside B6(11) showed stronger ABTS radical scavenging activity (IC50: 2.68 ± 0.05~4.86 ± 0.06 μM) than the positive control L-(+)-ascorbic acid (IC50: 10.06 ± 0.19 μM). This research provided a theoretical basis for the leaves ofL. robustumas a tea with function in treating obesity and diabetes.Keywords:Ligustrum robustum;phenylethanoid glycoside;phenylmethanoid glycosides;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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代谢生物学
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DOI
PubMed
高影响因子
Journal of Materials Chemistry B
·
2020
·Vol. 9
·期 2
·421-427
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IF 5.344
Haichuan Peng,Yan Zhou,Chuxi Zhang,Manyu Wang,Siyu Zhao,Yingying Xu,Wei Zhang,Hongbo Xin,Xiaolei Wang
Obesity is a chronic and recurrent disease with potential risks. Traditional weight-loss methods (like exercises, surgeries, oral drugs, etc.) have shown different side effects. In this experiment, the microneedle (MN) patch was selected as the drug carrier of the weight-loss drug Rosiglitazone (Rosi). Besides, melanin was added to enhance the photo-thermal effect and accelerate the release of drugs to the target fat region under near-infrared (NIR) light. Afterwards, with exterior cold stimulation, the significant and accurate effect of body slimming could be achieved. This combination of soluble MN patches and variable temperatures provides an attractive nonsurgical method for future accurate body slimming management.
研究领域:
药学
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生物医学工程
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治疗学
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DOI
高影响因子
JOURNAL OF FOOD BIOCHEMISTRY
·
2021
·Vol. 45
·期 5
·e13737
·
IF 2.72
Ming-Xi Zhou,Xing Tian,Zhong-Qin Wu,Ke Li,Zong-Jun Li
Areca nut and Fuzhuan brick tea, a type of natural plant products, have obvious effects of fat reduction and weight loss; however, there is no report on their synergistic effect. This study investigated the effects of Fuzhuan brick tea supplemented with different concentrations of areca nut (5% (LAF), 10% (MAF), and 20% (HAF)) on serum and gut microbiota in Kunming (KM) mice. The results showed that Fuzhuan brick tea supplemented with areca nuts (AFTs) could reduce weight, prevent the accumulation of fat, inhibit the increase in the levels of serum triglyceride, total cholesterol, low-density lipoprotein cholesterol, blood glucose, free fatty acid, insulin, and total bile acid, alleviate the decrease in high-density lipoprotein cholesterol level, and regulate the composition of gut microbiota by high-fat diet intervention. The HAF group with 20% areca nut content showed the best effect. These results could provide a novel approach to prevent obesity and hyperlipidemia. Practical applications Consumption of areca nut and tea is widespread in Asia and other regions. As a controversial raw material, the damage due to areca nut to oral mucosa health has often aroused public concern and heated discussion; however, its medicinal value has been confirmed in terms of its pharmacological effects in various aspects. Fuzhuan brick tea, a type of traditional postfermented dark tea, has been confirmed to exert effects of antiobesity. Therefore, the areca nut and Fuzhuan brick tea, as a type of natural plant products, have obvious effects of fat reduction and weight loss; however, their synergistic effect has not been reported. To our knowledge, this study is the first to explore the effects of the Fuzhuan brick tea supplemented with areca nuts (AFTs) on serum and gut microbiota in mice. On the premise of exerting their beneficial effects (especially in terms of easing food stagnation and eliminating indigestion) and reducing their toxic and side effects, the effects of AFTs on health were further clarified, which could provide a novel direction for the development and utilization of areca nut. Moreover, our research would increase public understanding of areca nut and provide guidance to the Fuzhuan brick tea processing 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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动物科学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2025
·
IF 3.1
Lin Chen,Han Huang,Xiali Liu,Peijing Zhao,Biao Zhou
A novel oxyphenisatin analogue was identified in a type of jelly candy during routine inspections of food products marketed for weight-loss purposes. Through analysis utilizing ultra-high-performance quadrupole-Orbitrap high-resolution mass spectrometry (UHPLC-Q-Orbitrap-HRMS), the fragment ions at m/z 258 and 195 observed in the MS/MS experiments were found to be consistent with those of 4-Chloro-oxyphenisatin diacetate. It was inferred that the unknown compound is likely a derivative of 4-Chloro-oxyphenisatin diacetate. The candy was separated and purified by column chromatography, and the purified compound was determined to be 96.4 % by high-performance liquid chromatography (HPLC). Subsequently, the structure was confirmed through nuclear magnetic resonance (NMR) spectroscopy. Based on the data, it was concluded that the structure of the unknown compound involved the substitution of two symmetrical acetyl groups in the 4-chloro-oxyphenisatin diacetate molecule with two isobutyl groups. Ultimately, the novel oxyphenisatin analogue was identified as (5-chloro-2-oxoindolin-3,3-ylidene) bis (4,1-phenylbutan-2-yl) diisobutyrate and designated as 4-Chloro-oxyphenisatin diisobutyrate. Finally, a quantitative analysis of the novel unknown compound in the jelly candy revealed a concentration of 6 mg per pellet. Based on the recommended daily consumption of one pellet, as indicated on the product packaging, the level of illegal additives may lead to diarrhoea and consequently poses a risk to human health. To the best of our knowledge, this represents the first report on the identification of 4-Chloro-oxyphenisatin diisobutyrate.
研究领域:
药物化学
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食品安全
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分析化学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
·
2017
·
IF 2.603
Qiaoyuan Cheng,Linjun Shou,Cen Chen,Shi Shi,Minghao Zhou
In this paper, an ultra-high-performance liquid chromatography coupled with linear ion trap quadrupole Orbitrap high resolution mass spectrometry (UHPLC-LTQ-Orbitrap HRMS) method was developed and validated for identification, confirmation and quantitation of illegal adulterated weight-loss drugs in plant dietary supplements. 13 wt-loss drugs were well separated by the gradient elution of 10 mmol/L ammonium acetate − 0.05% formic acid H 2 O and acetonitrile at a flow rate of 0.2 mL/min within 12 min. The MS analysis was operated under the positive ion and in full MS/dd-MS 2 (data-dependent MS 2 ) mode. The full MS scan with resolution at 60 000 FWHM and narrow mass windows at 5 ppm acquired data for identification and quantitation, and dd-MS 2 scan with resolution at 15 000 FWHM obtained product ions for confirmation. The method validation showed good linearity with coefficients of determination (r 2 ) higher than 0.9951 for all analytes. Meantime, all the LOD and LLOQ values were in the respective range of 0.3–2 and 1–9 ng/g. The accuracy, intra- and inter-day precision were in the ranges of −1.7 to 3.4%, 1.7–5.0% and 1.9–4.4%, respectively. The mean recoveries ranged from 85.4 to 107.1%, while the absolute and relative matrix effect were in the corresponding range of 98.2–108.6% and 2.6–8.7%. Among 120 batches of weight loss plant dietary supplements, sibutramine and fluoxertine or both were positive in 29 samples. In general, LTQ-Orbitrap HRMS technology was a powerful tool for the analysis of illegal ingredients in dietary supplements.
研究领域:
分析化学
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药学
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产品关联
DOI
PubMed
高影响因子
COMPOSITES PART B-ENGINEERING
·
2022
·
IF 11.322
Xin Jin,Chengxiong Wei,Chengwei Wu,Wei Zhang
Hydrogels have been widely investigated as gastric retention systems for drug delivery and bariatric intervention due to their good biocompatibility , degradability, and similarity with human tissues or organs. To realize long-term retention, hydrogels need to swell considerably on contact with gastric fluid to prevent passing through the pylorus and simultaneously maintain their mechanical stability after swelling to resist the damage of gastric pressure. However, high swelling ratio often results in the reduction of mechanical strength . Here, a swelling hydrogel with long-term mechanical stability for gastric retention is proposed. The hydrogel is designed as double networks, namely, the polyacrylamide as the first network and chitosan/sodium alginate as the second network. The hydrogel can reside in the stomach by the swelling of first network and maintain mechanical stability through the gradual formation of second network under the action of gastric fluid. The animal model test proves that the hydrogel can reside in the stomach with intact shape for 16 days, and then is biologically degraded in the gastric environment.
研究领域:
材料科学
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生物医学工程
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药学
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产品关联
DOI
高影响因子
Biomaterials Science
·
2024
·
IF 5.8
Zichun Gao,Yixuan Liu,Wenjiao Lin,He Lian,Zhaoxu Meng
As a globally prevalent disease, obesity leads to many chronic diseases, so it is important to develop safe and effective treatments with fewer side effects and lasting weight loss. In this study, we developed a biodegradable hyaluronic acid microneedle patch loaded with polydopamine nanoparticles and mirabegron, which directly acted on subcutaneous white adipose tissue, and then induced browning of white adipose tissue through mild photothermal therapy. The approach showed excellent browning-promoting ability and biocompatibility. It is noteworthy that the weight of untreated mice increased by 9%, while the weight of obese mice decreased by nearly 19% after photothermal treatment. In addition, when mirabegron was used in combination with photothermal therapy, the weight loss of obese mice was more significant, with a weight loss of about 22%. This microneedle patch exhibited attractive potential for body slimming.
研究领域:
生物医学工程
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药学
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治疗学
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产品关联
DOI
PubMed
高影响因子
Food & Function
·
2022
·Vol. 13
·期 24
·12799-12813
·
IF 6.317
Liyuan Ran,Jinhui Yu,Rui Ma,Qing Yao,Mingjie Wang,Yuping Bi,Zichao Yu,Yingjie Wu
Omega-3 PUFAs rich in fish oil are believed to prevent obesity by improving lipid metabolism and regulating gut microbiota. Microalgae oil is considered as an alternative source of omega-3 PUFAs owing to diminishing fish resources. Schizochytrium microalgae oil (SMO), with a high DHA proportion, is a promising source for commercial DHA production. However, its weight-loss and gut microbiota-regulating properties are not well studied. Here we compared the obesity reducing effects of SMO, commercial fish oil (FO) and a weight-loss drug, Orlistat (OL), in a high-fat diet (HFD) induced obesity mouse model. We found that SMO is comparable to commercial FO and OL with regard to weight loss, and it even exhibits the weight-loss effects earlier than FO and OL. It can efficiently inhibit the expression of lipogenesis-related genes and induce the expression of lipolysis-related genes. Moreover, SMO has different gut microbiota modulating effects from those of FO and OL. It does not influence the diversity of bacterial community, but does increase the abundance of several beneficial SCFAs-producing bacteria and inhibits obesity-promoting Desulfovibrio and several pathogens. We also found that SMO recovers the HFD-disturbed metabolic capability of gut microbiota. It can increase the abundance of several metabolism-related pathways, such as those of amino acids, SCFAs and bile acid, and decrease the level of the LPS biosynthesis pathway, which probably contributes to an improvement of lipid metabolism and restoration of the colonic mucosal barrier impaired by HFD. Our data suggest that SMO can be used as a superior dietary supplement for alleviating obesity.
研究领域:
营养学
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微生物学
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代谢学
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药理学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF SEPARATION SCIENCE
·
2022
·Vol. 45
·期 23
·4198-4208
·
IF 3.614
Fu-Qin He,Guang-Zhen Wan,Juan Chen
As a traditional Chinese medicine, Schisandra chinensis has a potential weight-loss effect by delaying carbohydrate absorption and improving lipid metabolic disorders. However, its active components are still unclear and require in-depth research. In this study, the active components of Schisandra chinensis responsible for pancreatic lipase and alpha-glucosidase inhibitory activity were screened and identified based on a spectrum-effect relationship study in combination with ultra-performance liquid chromatography-tandem mass spectrometry analysis. The ultra-high-performance liquid chromatography fingerprints of 17 batches of Schisandra chinensis were established, and 14 common peaks were specified by similarity analysis. The half-maximal inhibition concentration values for pancreatic lipase and alpha-glucosidase inhibition were separately measured by enzymatic reactions. Using multivariate statistical methods including principal component analysis, partial least square analysis, and grey relational analysis, the correlation models between the peak areas of 14 common peaks and half-maximal inhibition concentration values were constructed, and the chromatographic peaks making a great contribution to efficacy were screened out. Peak1, Peak2, Peak4, Peak6, Peak9, Peak10, Peak11, and Peak13 were responsible for alpha-glucosidase inhibitory activity, while Peak1, Peak4, Peak6, Peak9, Peak10, and Peak11 for pancreatic lipase inhibitory activity. Finally, the 70% ethanol extracts of Schisandra chinensis were characterized by ultra-high-performance liquid chromatography-tandem mass spectrometry analysis, and 14 lignans were identified to further elucidate the active constituents of Schisandra chinensis . The positive results suggested the proposed strategy is simple and effective to screen active components from complex medicinal plants.
研究领域:
药理学
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分析化学
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中医药
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代谢紊乱
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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）