JOURNAL OF BIOMEDICAL SCIENCE
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2023
·Vol. 30
·期 1
·1-14
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IF 11
Shen Weiyi,Shao Wentao,Wang Qihan,Wang Bo,Zhao Gang,Gu Aihua,Jiang Zhaoyan,Hu Hai
Background Cholesterol gallstone disease is a common disease. Reducing cholesterol burden is important to prevent/treat gallstone. In this study, we investigated the application of diosgenin (DG) to prevent the formation of gallstone in mice.Methods Adult male C57BL/6J mice were fed with the lithogenic diet (LD) only or LD supplemented with DG or ezetimibe for 8 weeks. Incidences of gallstone formation were documented. Intestine and liver tissues were collected to measure the lipid contents and expression of genes in cholesterol metabolism. Caco2 cells were treated with DG to monitor the regulation on cholesterol absorption and the transcriptional regulation of Npc1l1 gene. Changes of gut microbiota by DG was analyzed. Intraperitoneal injection of LPS on mice was performed to verify its effects on STAT3 activation and Npc1l1 expression in the small intestine.Results LD led to 100% formation of gallstones in mice. In comparison, dietary DG or ezetimibe supplementary completely prevents gallstones formation. DG inhibited intestinal cholesterol absorption in mice as well as in Caco2 cells by down-regulation of Npc1l1 expression. DG could directly inhibit phosphorylation of STAT3 and its transcriptional regulation of Npc1l1 expression. Furthermore, DG could modulate gut microbiota profiles and LPS mediated STAT3 activation and Npc1l1 expression.Conclusion Our results demonstrated that dietary DG could inhibit intestinal cholesterol absorption through decreasing NPC1L1 expression to prevent cholesterol gallstone formation.
研究领域:
药理学
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胃肠病学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
MATERIALS CHEMISTRY AND PHYSICS
·
2024
·
IF 4.3
YanXiao Zhang,XiaoNing Gao,Nan Ma,Hong Zhou,Lu Feng
Diosgenin is an indispensable intermediate in the production of various steroid drugs. Conventional hydrolysis of sulfuric acid produces large amounts of acidic wastewater and has always faced stringent restrictions from environmental requirements. Here, UiO-66-NH 2 and its derivative of UiO-66-NH 2 -AT (AT = 3-amino-1,2,4-triazole) were synthesized, and these two compounds were further grafted with high-concentration CF 3 SO 3 H molecules to obtain the MOF-based solid superacids, namely UiO-66-NH 2 -[SO 3 CF 3 ] and UiO-66-NH 2 -AT-[SO 3 CF 3 ], respectively. They have been applied to the alcoholysis of total saponins to extract diosgenin, and the alcoholysis conditions, including the solid acid dosage, extraction temperature and extraction time, have been optimized by single-factor experiments. Subsequently, the alcoholysis conditions of UiO-66-NH 2 -AT-[SO 3 CF 3 ] with more prominent catalytic performance and cycle stability were further optimized by the response surface method, and under the optimum conditions, the diosgenin yield reached 20.8 %, which was close to the predicted value of 21.3 % and was superior to the conventional hydrolysis of sulfuric acid and our previously reported solid acids. Additionally, the alcoholysis pathways and alcoholysis mechanism of the total saponins catalyzed by UiO-66-NH 2 -AT-[SO 3 CF 3 ] have been proposed by the analysis of high-resolution electrospray mass spectrometry.
研究领域:
化学工程
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药物化学
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环境科学
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产品关联
DOI
高影响因子
CRYSTAL GROWTH & DESIGN
·
2016
·
IF 4.425
Yajing Wang,Yingnan Chi,Wenwen Zhang,Qiuhong Yang,Song Yang,Chong Su,Zhengguo Lin,Jingkai Gu,Changwen Hu
Four hemihydrates (HH-I, HH-II, HH-III, and HH-IV) and two monohydrates (MH-I, MH-II) of diosgenin, a steroid sapogenin, have been prepared. Hydrates HH-I, HH-III, HH-IV, MH-I, and MH-II have been thoroughly characterized by single-crystal X-ray diffraction, powder X-ray diffraction, Fourier transform infrared spectroscopy, thermogravimetry, and differential scanning calorimetry. Although in these cases diosgenin has a similar conformation, hydrogen bonding interactions connect diosgenin and the lattice water molecule into different supermolecular structures. More importantly, three controlling factors, including initial concentration, water volume fraction, and solvent, have been investigated in the crystallization of diosgenin hydrates. The control experiments in ethanol display that as the initial concentration increases, HH-III, HH-I, and HH-II appear in order, and with the increase of water content, HH-I, HH-III, MH-I, and MH-II are obtained correspondingly. When acetone is used as solvent, HH-IV was synthesized. Moreover, we observed that stick-like crystals of HH-III gradually transform to plate-like ones of MH-I in solution at ambient conditions. This transformation is prevented by lowering temperature and is accelerated by adding water.
研究领域:
晶体工程
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药物化学
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固态化学
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结构化学
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DOI
高影响因子
Heliyon
·
2024
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IF 3.4
Min Cai,Yangchen Mao,Wenjing Gao,Zhenzhen Wang,Jianwei Mao,Ruyi Sha
Inflammatory bowel disease (IBD) is a growing global health problem. IBD is commonly prevalent in Europe and America and the incidence rate in Asia is on the rise due to altered dietary structure. Diosgenin is a natural steroidal saponin derived from Dioscorea plants. Diosgenin is the main active ingredient of some Chinese medicines which are mainly used to treat coronary heart disease, angina and hyperlipidemia. Recently, growing evidence has exhibited a crucial role of diosgenin and dioscin in alleviating IBD in multiple ways. However, the precise mechanism of diosgenin against IBD needs further exploration. In this study, network pharmacological and systematic bioinformatic analyses were performed to investigate the diosgenin's targets against IBD. 71 targets such as SRC, TNF and STAT3 were identified as overlapped genes between diosgenin and IBD. Gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analysis exhibited their involvement in the tyrosine kinase signaling pathway and its membrane receptors. Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor resistance and its downstream Ras-MAPK pathway and PI3K-Akt pathway might become the mechanism of diosgenin against IBD. In addition, molecular docking analysis showed that diosgenin has the massive potential of direct binding to tyrosine kinase and its receptors such as SRC, EGFR, FGFR1 and VEGFR. The results above collectively provided evidence that diosgenin is a promising nutraceutical food against IBD.
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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功能性食品
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产品关联
DOI
PubMed
高影响因子
Journal of Cleaner Production
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2020
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IF 7.246
Bowei Shen,XueJun Yu,Farong Zhang,Wenxiu Jiang,Hui Yuan,Zhiquan Pan,Hong Zhou
A new method of the catalytic alcoholysis of Dioscorea zingiberensis C. H. Wright into diosgenin by magnetic solid acid in a Teflon-lined stainless-steel autoclave for the first time. The magnetic solid acid, Fe 3 O 4 @SiO 2 –SO 3 H, was prepared by the connecting the –SO 3 H groups on the surface of SiO 2 encapsulated Fe 3 O 4 microspheres . The synthesized catalysts were systematically analyzed by Fourier transform infrared (FT-IR) spectroscopy, thermogravimetric analyzer (TGA), X-ray diffraction (XRD), vibrating sample magnetometry (VSM), temperature programmed desorption of ammonia (NH 3 -TPD), scanning electron microscope (SEM), transmission electron microscope (TEM) and transmission electron microscope-mapping(TEM-mapping). To obtain the best conditions for the alcoholysis of Dioscorea zingiberensis C. H. Wright, single factor test was first utilized to determine the range of optimal conditions and optimized by response surface method . A three-level-three-factor Box-Behnken design was adopted to illustrate the effect of solid acid mass, solvent volume, reaction time and temperature on the yield of diosgenin. The optimum conditions obtained by response surface methodology were: 0.42 g Fe 3 O 4 @SiO 2 –SO 3 H, 4.38 mL solvent of ethanol, the reaction temperature at 100 °C and 6.09 h reaction time. At the optimal conditions, this method can reach the highest yield 2.64% from Dioscorea zingiberensis C. H. Wright. The yield of the new method was 21.66% higher than conventional sulfuric acid hydrolysis based on the analysis results of UV and HPLC. Importantly, the catalysts and solvents used in the alcoholysis process by the solid acid can be recovered, which is green and environmentally friendly, indicating that the catalytic alcoholysis with magnetic solid acid under hydrothermal conditions had a broad application prospect in diosgenin production.
研究领域:
植物化学
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药物化学
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绿色化学
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产品关联
DOI
高影响因子
Evidence-based Complementary and Alternative Medicine
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2016
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IF 1.931
Ke Fang,Hui Dong,Shujun Jiang,Fen Li,Dingkun Wang,Desen Yang,Jing Gong,Wenya Huang,Fuer Lu
To determine the effects and the underlying mechanism of diosgenin (DSG) and 5-methoxypsoralen (5-MOP), two main active components in the classical Chinese prescription Hu-Lu-Ba-Wan (HLBW), on insulin resistance, HepG2 cells were incubated in medium containing insulin. Treatments with DSG, 5-MOP, and their combination were performed, respectively. The result showed that the incubation of HepG2 cells with high concentration insulin markedly decreased glucose consumption and glycogen synthesis. However, treatment with DSG, 5-MOP, or their combination significantly reversed the condition and increased the phosphorylated expression of estrogen receptor-α (ERα), sarcoma (Src), Akt/protein kinase B, glycogen synthase kinase-3β (GSK-3β), and the p85 regulatory subunit of phosphatidylinositol 3-kinase p85 (PI3Kp85). At the transcriptional level, expression of the genes mentioned above also increased except for the negative regulation of GSK-3β mRNA. The increased expression of glucose transport-4 (GLUT-4) was meanwhile observed through immunofluorescence. Nevertheless, the synergistic effect of DSG and 5-MOP on improving glycometabolism was not obvious in the present study. These results suggested that DSG and 5-MOP may improve insulin resistance through an ER-mediated PI3K/Akt activation pathway which may be a new strategy for type 2 diabetes mellitus, especially for women in an estrogen-deficient condition.
研究领域:
药理学
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内分泌学
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细胞生物学
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中医
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF NANOPARTICLE RESEARCH
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2023
·Vol. 25
·期 7
·1-15
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IF 2.5
Fan Mingxuan,Tang Lingqian,Wang Yihan,Feng Lu,Zhou Hong
In this work, thiol-functionalized silica SiO 2 -Pr-SH (Pr = −(CH 2 ) 3 ) was synthesized by self-hydrolysis of 3-mercaptopropyltrimethoxysilane (MPTMS) with the average particle sizes up to 1.9 μm. Then sulfonic acid-functionalized SiO 2 -PrSPr-SO 3 H was prepared by the 1,3-Propanesultone grafted onto SiO 2 -Pr-SH and used as solid acid catalysts for alcoholysis of total saponins in Dioscorea zingiberensis C. H. Wright (DZW) to the production of diosgenin. The as-prepared solid acid was fully characterized with FT-IR, Raman, TGA, BET, FESEM, EDS, elemental mapping, XPS, and XRD, respectively. The solid acid quantity, solvent dosage, extraction temperature, and time were studied by single-factor experiments. The maximum yield of diosgenin was calculated to be 16.73% relative to 0.1 g total saponins, which was higher than the sulfuric acid hydrolysis method. Importantly, it is an efficient alcoholysis approach for the production of diosgenin from total saponins and the prepared solid acid can be recycled in the reaction medium. The possible alcoholysis products and reaction mechanism were proposed on the basis of LC-MS results. This work not only provides a new solid acid for the production of diosgenin from DZW but also gives a beneficial synthetic reference for the preparation of high-activity SO 3 H-functionalized catalysts based on the organosilane. Graphical abstract SO 3 H-functionalized silica as an efficient solid acid catalyst for the production of diosgenin from Dioscorea zingiberensis C. H. Wright
研究领域:
化学工程
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植物化学
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药物合成
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产品关联
DOI
高影响因子
ACS Omega
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2021
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IF 3.512
Bowei Shen,XueJun Yu,Wenxiu Jiang,Hui Yuan,Mengqi Zhao,Hong Zhou,Zhiquan Pan
This work proposed to prepare solid acid from phosphorus tailings and successfully convert Dioscorea zingiberensis C.H. Wright (DZW) into diosgenin from the perspective of solid waste resource reuse and clean production. The results showed that SiO2–SO3H solid acid could catalyze the production of diosgenin from total saponins under solvothermal reaction conditions. In addition, the parameters of a single factor, such as the amount of SiO2–SO3H, solvent volume, reaction temperature, and reaction time, were optimized to confirm the optimal range of reaction conditions, and the optimal process conditions were determined by the response surface method. The yield of diosgenin was 2.45 ± 0.17% under the optimum conditions, and the yield of diosgenin was increased by 12.90% compared with the traditional acid hydrolysis process. Except the relatively higher catalytic activity, the alcoholysis approach for the production of diosgenin has no waste liquid to discharge. The products were analyzed by high-performance liquid chromatography-mass spectrometry, and the pathway to convert total saponins into diosgenin under SiO2–SO3H has been proposed. Moreover, the adopted catalyst can be prepared with very low cost from phosphorus tailings. Considering the obvious superiorities, the alcoholysis approach in this work could be a promising strategy for green production of diosgenin as well as a possible utilization pathway of phosphorus tailings.
研究领域:
中药化学
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环境科学
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催化化学
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产品关联
DOI
PubMed
高影响因子
Journal of Pharmaceutical Innovation
·
2026
·Vol. 21
·期 2
·116
·
IF 2.7
Mohamed Rasha,Hussein Mohammed,El Tamany El Sayed,Mostafa Nasser,Abbas Ahmed
Background Obesity, characterized by lipid accumulation, oxidative stress, and inflammation, remains a major public health challenge. This study aimed to investigate the therapeutic efficacy of diosgenin-loaded silver nanoparticles (Dio-AgNPs) in modulating obesity-induced metabolic and molecular dysfunction through integrated biochemical, gene expression, and molecular docking approaches. Methods Male albino rats were randomly assigned to control and experimental groups, with Dio-AgNPs administered at two distinct doses. Dio-AgNPs were synthesized and characterized using UV-Vis spectroscopy, TEM, DLS, and zeta potential measurements to confirm particle size and stability. Biochemical analyses included serum lipid profile (triglycerides, total cholesterol, LDL-c, HDL-c), fasting glucose, insulin levels, and HOMA-IR for insulin sensitivity. Oxidative stress markers (MDA) and antioxidant enzymes (SOD, CAT, GPx) were measured spectrophotometrically. Inflammatory cytokines (TNF-α and IL-6) were quantified by ELISA. Gene expression of lipogenic enzymes ( ACC and FAS ) and antioxidant-related genes was assessed using quantitative real-time PCR (qRT-PCR). Molecular docking simulations were performed to evaluate diosgenin’s binding affinities and interactions with ACC and FAS enzyme active sites. Results Dio-AgNP-treated rats showed significant reductions in serum triglycerides, total cholesterol, LDL-c, and fasting glucose compared to controls, while HDL-c and insulin sensitivity were markedly improved. Antioxidant enzyme activities (SOD, CAT, GPx) increased significantly, and MDA levels decreased, indicating oxidative stress attenuation. ELISA confirmed reduced levels of TNF-α and IL-6, revealing anti-inflammatory effects. Gene expression analysis demonstrated dose-dependent downregulation of ACC and FAS , along with upregulation of antioxidant and insulin-responsive genes. Molecular docking results revealed strong binding interactions of diosgenin with both ACC and FAS enzymes, supporting enzymatic inhibition and the transcriptional trends observed. Silver nanoparticle delivery enhanced bioavailability and target specificity. Conclusion This is the first report, to our knowledge, that combines biochemical, gene expression, and molecular docking data to investigate Dio-AgNPs’ anti-obesity effects. The findings highlight a promising nanomedicine-based approach for metabolic regulation and pave the way for further research in therapeutic nanoparticle design and application.
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产品关联
DOI
高影响因子
Nanomedicine-Nanotechnology Biology and Medicine
·
2018
·
IF 6.5
Zeliang Wei,Guang Xin,Haibo Wang,Huajie Zheng,Chengjie Ji,Jun Gu,Limei Ma,Chaoyi Qin,Zhihua Xing,Hai Niu,Wen Huang
Thrombosis is the leading cause of death in patients with cardiovascular disease in the world. Current antithrombotic agent aspirin has serious side effects such as higher bleeding risk and serious gastrointestinal ulcers . Diosgenin reported in clinical research could prevent thrombosis without side effects. However, poor bioavailability and low knowledge on its molecular targets limit its clinical application. A novel prodrug with antithrombotic effect was prepared based on conjugating diosgenin derivatives to PEG with Schiff-base bond. The prodrug with long blood circulation time and satisfying safety could self-assemble into micelles in water. The prodrug micelles with pH-responsibility could targetedly release diosgenin in position of thrombus in vivo . The results indicate that the prodrug micelles without bleeding risk and histological damages prevent thrombosis by inhibiting platelet activation and apoptosis . Our studies demonstrate that the prodrug micelles could obviously enhance the efficacy in the prevention of arterial thrombus and venous thrombus than aspirin.
研究领域:
药剂学
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心血管疾病
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药物递送系统
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分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Molecular Catalysis
·
2021
·
IF 5.062
Bowei Shen,Farong Zhang,Mengqi Zhao,Zhiquan Pan,Qingrong Cheng,Hong Zhou
The magnetic solid acid, Fe 3 O 4 @PEI@SO 3 H, was synthesized and used as a catalyst to transfer steroid saponins into diosgenin in an alcoholysis approach. The results showed that the magnetic solid acid greatly improved the alcoholysis efficiency for extraction diosgenin from steriod saponins. To optimize the parameters for alcoholysis, such as the mass of the solid acid, solvent volume, the reaction temperature and time, single factor experiments as well as response surface experiment have been performed. Under the optimal conditions, the diosgenin yield obtained by alcoholysis is higher than that of the traditional inorganic acid hydrolysis. And it worth to mention that no waste liquid is discharged. The catalyst is very stable and can be used for three times without obvious mass loss and activity decrease, indicating that the technology of extracting diosgenin from Dioscorea zingiberensis C.H. Wright tuber has a broad prospect in industrial application.
研究领域:
生物化学
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有机合成
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制药工程
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DOI
高影响因子
JOURNAL OF MEDICINAL FOOD
·
2022
·Vol. 25
·期 3
·261-271
·
IF 2.542
Yushu He,Ruilin Luo,Manying Xia,Jiayu Liu,Yanpeng Yao,Fenyi Min,Ruyi Jin,Ruolin Wang,Xiaoli Peng
Diosgenin (DIO) is a kind of steroid sapogenin derived from natural plants. It exerts strong anti-infection, antiallergy, antiviral, and antishock pharmacological properties. In this article, the protective effects of DIO against dextran sulfate sodium (DSS)-induced colitis in mice were researched. Compared with the 2.5% DSS treatment group, 15 mg/kg body weight of diosgenin alleviated colitis disease, evidenced by the increased body weight, the decrease in the disease activity index, and the histological scores. Furthermore, 16S rRNA high-throughput sequencing results demonstrated that DIO improved the colon homeostasis through modulating the gut microbiota, including increases in the relative abundance of several probiotic bacteria, such as Prevotellaceae (from 1.4% to 5.8%), Lactobacillus (from 12.3% to 29.7%), Mucispirillum (from 0.07% to 0.49%), and decreases in the pathogenic bacteria, such as Streptococcus (from 1.6% to 0.6%) and Pseudomonadaceae (from 0.004% to 0%).In addition, the concentration of gut microbial metabolites, total short-chain fatty acids (SCFAs), acetic acid, and propionic acid were significantly increased after DIO supplementation. In conclusion, our findings suggested that DIO attenuates DSS-induced colitis in mice by means of modulating imbalanced gut microbiota and increases in SCFA generation.
研究领域:
药理学
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微生物学
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胃肠病学
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DOI
PubMed
高影响因子
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