INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2023
·
IF 8.2
Peiyi Jin,Linzhou Chen,Jinjian Zhong,Tiefeng Yuan,Lin Gan,Jilong Huang,Liping Wang,Huajun Fan,Chen Lin
Dioscoreae nipponica Makino ( D. nipponica ) as the rhizome of dioscoreaceae rich in steroidal saponins, has been reported to have the hypolipidemic effects etc. However, it is still unclear which exact active components are primary responsible for the beneficial effects. This study was conducted to fish out the lipase inhibitors from D. nipponica , and evaluate the inhibitory activity on porcine pancreatic lipase (PPL) through in vitro kinetic assay using p -nitrophenyl palmitate as substrate. Accordingly, the ethanolic extract was subjected to D101 macroporous resin purification for spectrophotometric screening, high performance liquid chromatography (HPLC) separation and structural characterization by ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry. Through orlistat validation, the PPL inhibitory activity and IC 50 value of the extract were respectively 68.34 ± 1.47 % and 107.05 μg/mL under the optimized inhibition conditions. From 6 steroidal saponins identified, the inhibitory components named the protodioscin, protogracillin, dioscin and gracillin were fished out by grouping separation and HPLC analysis. Furthermore, dioscin and gracillin with the parent structure of diogenin were confirmed as the major inhibitors by virtue of stability tests based on transformation of protodioscin and protogracillin. Finally, the inhibitory mechanism of the major inhibitors toward PPL was further clarified by kinetic analysis and molecular docking analysis. The proposed method not only revealed the PPL inhibitory components in D. nipponica , but also provided an effective approach to hierarchical screening of PPL inhibitors from natural plants.
研究领域:
药理学
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生物化学
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分析化学
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天然产物
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产品关联
DOI
PubMed
高影响因子
INDUSTRIAL CROPS AND PRODUCTS
·
2022
·
IF 6.449
Mingxuan Fan,Wenxiu Jiang,Lingqian Tang,Mengqi Zhao,Qingrong Cheng,Lu Feng,Hanjun Wu,Zhiquan Pan,Hong Zhou
From the perspective of full utilization of biomass, a clean approach for the production of diosgenin from total saponins in Dioscorea zingiberensis C.H. Wright (DZW) was realized by preliminary separation and extraction. An alcoholysis approach was adopted to obtain diosgenin using a novel magnetic solid acid Fe 3 O 4 @SiO 2 -Pr-S-Pr-SO 3 H Pr = -(CH 2 ) 3 -) as the catalyst. The prepared solid acid has been fully characterized. The single factor methodology was used to optimize the process parameters. The optimum conditions were: 0.50 g Fe 3 O 4 @SiO 2 -Pr-S-Pr-SO 3 H, 6.0 mL ethanol, the reaction temperature 120 ℃, reaction time 7.0 h and the maximum yield of diosgenin was 24.18% which are higher than conventional hydrolysis with 1.5 M sulfuric acid indicating the high catalytic activity of the solid acids. In addition, the solid acid had good reusability. The LC-MS technique was applied to analyze the main steroidal saponins in total saponins and possible mechanisms and pathways of hydrolysis and alcoholysis processes. Alcoholysis by an as-prepared magnetic solid acid is clearly excellent in high efficiency and reusability. It is a promising strategy for the green production of diosgenin through a cleaner approach.
研究领域:
植物化学
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天然产物化学
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绿色化学
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产品关联
DOI
高影响因子
CATALYSIS LETTERS
·
2022
·Vol. 152
·期 11
·3453-3464
·
IF 2.936
Zhao Mengqi,Pan Zhiquan,Chen Qingrong,Zhou Hong
Diosgenin is an important intermediate of drugs, the special structure similar to hormone determines its important position in drug synthesis. Diosgenin was generally obtained by sulfuric acid hydrolysis of dioscorea, which produced too much acid wastewater, and caused environmental issues. A new solid acid based on TiO 2 was designed and synthesized through the sulfonation of the prepared TiO 2 , the structure was fully characterized by FTIR, SEM, EDX, XPS and XRD. Under the optimized conditions, the yield of diosgenin reached 30.75%, the value was much higher than that of H 2 SO 4 of the same quality. To explore the factors that affect the yield, the usage amount of the solid acid, the temperature, the solvent volume and the extraction time were taken into the analysis, and the results of the recycling experiments indicated that the prepared solid acid can be used for three time and maintain its high activity. A highly efficient solid acid catalyst for diosgenin extraction from saponins was successfully synthesized, and the extraction method was environmentally friendly. Graphical Abstract
研究领域:
药物化学
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环境科学
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DOI
高影响因子
JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
·
2017
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IF 2.603
Ling-Li Wang,Dong-Sheng Zhao,Wei Shi,Zhuo-Qing Li,Zi-Tian Wu,Ping Li,Hui-Jun Li
It is vital to monitor the holistic toxicokinetics of toxic Chinese herbal medicines (CHMs) for safety. Although an integrated strategy based on the area under the curve (AUC) has been proposed to characterize the pharmacokinetic/toxicokinetic properties of CHMs, improvement is still needed. This study attempted to use 50% inhibitory concentration (IC 50 ) as weighting coefficient to investigate holistic toxicokinetics of the major diosbulbins i.e. diosbulbin A (DA), diosbulbin B (DB), and diosbulbin C (DC) after oral administration of Dioscorea bulbifera rhizome (DBR) extract. Firstly, the cytotoxicities of the three diosbulbins on human hepatic L02 cells were evaluated and the IC 50 values were calculated. Then, integrated toxicokinetics of multiple diosbulbins based on AUC and IC 50 were determined. Finally, correlations between integrated plasma concentrations and hepatic injury biomarkers including alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), and total bile acid (TBA) were analyzed. As a result, integrated plasma concentrations were correlated well with TBA and the correlation between TBA and IC 50 -weighting integrated plasma concentrations was better than that of AUC-weighting integrated plasma concentrations. In conclusion, the newly developed IC 50 -weighting method is expected to generate more reasonable integrated toxicokinetic parameters, which will help to guide the safe usage of DBR in clinical settings.
研究领域:
中药学
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毒理学
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生物医学
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产品关联
DOI
PubMed
高影响因子
Chinese Herbal Medicines
·
2023
·
IF 3.8
Miao Sha,Xiaohuan Li,Yu Liu,Hongyue Tian,Xu Liang,Xia Li,Wenyuan Gao
Objective Pseudostellaria heterophylla has been paid more attention in recent years, mainly as a medicine food homology plant. The content determination of P. heterophylla is not specified in the Chinese Pharmacopoeia (version 2020). The environmental conditions in different production areas could exert an influence on the quality of P. heterophylla . The purpose of this study is to discriminate P. heterophylla collected from different geographical origins of China. Methods In this study, the content of polysaccharide in 28 batches of P. heterophylla was determined using phenol–sulfuric acid. HPLC fingerprints were established under optimised HPLC-PDA methods. Subsequently, the similarity analysis (SA) and the quantification of heterophyllin B were analyzed. The metabolites of P. heterophylla were identified and evaluated using UHPLC-Q Exactive HF orbitrap MS system. Principal component analysis (PCA), partial least squares discriminant analysis (PLS-DA), hierarchical cluster analysis (HCA) and orthogonal PLS-DA (OPLS-DA) were performed based on all peak areas. Results The polysaccharide content in Guizhou and Jiangsu was higher than that of other production areas, which varied significant from different origins. While the content of heterophyllin B in Anhui and Jiangsu was high. The correlation coefficients of HPLC fingerprints for 28 batches samples ranged from 0.877 to 0.990, and the characteristic map can be used to identify and evaluate the quality of P. heterophylla . The samples from Fujian, Guizhou, Jiangsu provinces can be relatively separated using multivariate statistical analysis including PCA, PLS-DA, HCA, OPLS-DA, indicating that their metabolic compositions were significantly different. Ultimately, a total of 15 metabolites which were filtrated by a VIP-value > 1 and a P -value < 0.05 associated with the separation of different origins were identified. Conclusion HPLC fingerprint was established to evaluate the quality and authenticity of P. heterophylla . The present work showed that the difference of geographic distributions had an influence on the internal chemical compositions. A sensitive and rapid untargeted metabolomics approach by UHPLC-Q Exactive HF orbitrap MS was utilized to evaluate P. heterophylla from different origins in China for the first time. Overall, this study provides insights to metabolomics of P. heterophylla and supplies important reference values for the development of functional foods.
研究领域:
中药学
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代谢组学
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药用植物研究
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产品关联
DOI
PubMed
高影响因子
INDUSTRIAL CROPS AND PRODUCTS
·
2020
·
IF 4.244
Wenxiu Jiang,Xuejun Yu,Yuan Hui,Bowei Shen,Zhang Farong,Zhiquan Pan,Hong Zhou
Diosgenin is an important intermediate of steroid hormone drugs, green production of diosgenin with high yield is a key research issue. In this study, a convenient, efficient, and eco-friendly approach was developed to produce diosgenin from saponins in D. zingiberensis C. H. Wright (Curcuma longa L) using a magnetic solid acid. Fe 3 O 4 @SiO 2 -Pr-S-SO 3 H is a heterogeneous catalyst and was obtained by loading 3-(mercaptopropyl) trimethoxysilane on the surface of Fe 3 O 4 @SiO 2 , followed by sulfonation with chlorosulfonic acid. The magnetic solid acid catalyst was fully characterized by Fourier Transform-Infrared (FT-IR) spectra, thermo gravimetric analysis (TGA), X-ray diffraction (XRD), vibrating sample magnetometer (VSM), and X-ray photoelectron spectroscopy (XPS), scanning electron microscope(SEM), transmission electron microscope (TEM), NH 3 -TPD, elemental mapping analysis. The effects of single factors, such as the solid acid mass, alcoholysis temperature, extraction time, and solvent volume on the diosgenin yield were analyzed. The extraction parameters for diosgenin were optimized by response surface methodology (RSM). The optimized values for the solid acid mass, solvent volume, extraction time, and temperature were 0.22 g, 7.8 mL, 7.4 h, and 100 °C, respectively. Under the optimized conditions, the maximum yield of diosgenin was 19.15 %. The solid acid reported in this work exhibited higher catalytic activity at a smaller dosage than traditional sulfuric acid and other solid acids. The alcoholysis products were identified by high-performance liquid chromatography-mass spectrometry (HPLC-MS). Alcoholysis catalysed by an as-prepared magnetic solid acid is clearly superior in terms of catalytic activity, dosage, and reusability. It is a promising strategy for the green production of diosgenin.
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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2014
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IF 2.175
He-Dong Bian,Xia-Lian Peng,Fu-Ping Huang,Di Yao,Qing Yu,Hong Liang
Diosgenin (DIO) is the active ingredient of Dioscorea species. The interaction of DIO with bovine serum albumin (BSA) was investigated through spectroscopic methods under simulated physiological conditions. The fluorescence quenching data revealed that the binding of DIO to BSA without or with Co2+ or Zn2+ was a static quenching process. The presence of Co2+ or Zn2+ both increased the static quenching constants KSV and the binding affinity for the BSA-DIO system. In the sight of the competitive experiment and the negative values of ΔH0 and ΔS0, DIO bound to site I of BSA mainly through the hydrogen bond and Van der Waals’ force. In addition, the conformational changes of BSA were studied by Raman spectra, which revealed that the secondary structure of BSA and microenvironment of the aromatic residues were changed by DIO. The Raman spectra analysis indicated that the changes of conformations, disulfide bridges, and the microenvironment of Tyr, Trp residues of BSA induced by DIO with Co2+ or Zn2+ were different from that without Co2+ or Zn2+.
研究领域:
生物化学
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药理学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF NANOPARTICLE RESEARCH
·
2023
·Vol. 25
·期 7
·1-15
·
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
MOLECULES
·
2021
·Vol. 26
·期 7
·2079
·
IF 4.412
Gui-Ya Yang,Jun-Na Song,Ya-Qing Chang,Lei Wang,Yu-Guang Zheng,Dan Zhang,Long Guo
In the present study, a simple and environmentally friendly extraction method based on natural deep eutectic solvents (NADESs) was established to extract four bioactive steroidal saponins from Dioscoreae Nipponicae Rhizoma (DNR). A total of twenty-one types of choline chloride, betaine, and L-proline based NADESs were tailored, and the NADES composed of 1:1 molar ratio of choline chloride and malonic acid showed the best extraction efficiency for the four steroidal saponins compared with other NADESs. Then, the extraction parameters for extraction of steroidal saponins by selected tailor-made NADES were optimized using response surface methodology and the optimal extraction conditions are extraction time, 23.5 min; liquid–solid ratio, 57.5 mL/g; and water content, 54%. The microstructure of the DNR powder before and after ultrasonic extraction by conventional solvents (water and methanol) and the selected NADES were observed using field emission scanning electron microscope. In addition, the four steroidal saponins were recovered from NADESs by D101 macroporous resin with a satisfactory recovery yield between 67.27% and 79.90%. The present research demonstrates that NADESs are a suitable green media for the extraction of the bioactive steroidal saponins from DNR, and have a great potential as possible alternatives to organic solvents for efficiently extracting bioactive compounds from natural products.Keywords:natural deep eutectic solvents;Dioscoreae Nipponicae Rhizoma;steroidal saponins;response surface methodology;extraction
研究领域:
植物化学
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药物化学
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DOI
高影响因子
JOURNAL OF NANOPARTICLE RESEARCH
·
2019
·Vol. 21
·期 12
·1-11
·
IF 2.009
Zhang Farong,Shen Bowei,Jiang Wenxiu,Yuan Hui,Zhou Hong
Extraction of diosgenin from the rhizome of Dioscorea by catalytic hydrolysis over recyclable solid acids is one of the most enviromentally friendly ways for the conversion of biomass into chemicals. In this paper, a magnetic solid acid, Fe 3 O 4 @SiO 2 @NH-(CH 2 ) 2 -NH 2 @SO 3 H with the particle size of about 80 nm, was synthesized by using Fe 3 O 4 (~ 20 nm) as a magnetic core and then coated orderly with tetraethyl orthosilicate (TEOS) and N-{3-(Trimethoxysilyl) propyl} ethylenediamine (TMPED) by sol-gel reactions in water/ethanol solution, followed by the sulfonation of chlorosulfonic acid. The solid acid was characterized by Fourier transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), scanning electron microscope (SEM), X-ray diffraction (XRD), vibrating sample magnetometer (VSM), and X-ray photoelectron spectroscopy (XPS). The content of acidic sites on the surface of the solid acid was 1.01 mmol/g, measured by back titration method. The prepared solid acid was used to hydrolyze and extract diosgenin from Dioscorea nipponica Makino (DNM). The results show that the magnetic solid acid has higher hydrolysis activity than 2.5 M hydrochloric acid under same hydrolysis conditions, at 110 °C for 5 h. In addition, the magnetic solid acid can be easily separated from the reaction mixture by the application of a magnet and reused several times without significant activity loss. This work has a potential application value for the extraction of diosgenin from plants.
研究领域:
植物化学
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环境科学
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材料科学
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产品关联
DOI
高影响因子
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2015
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IF 2.979
Min Liao,Cong Dai,Mengping Liu,Jiefeng Chen,Zuanguang Chen,Zhiyong Xie,Meicun Yao
A novel, sensitive and rapid ultra-performance liquid chromatography–tandem mass spectrometric (UPLC–MS/MS) method for simultaneous quantification of four furostanol glycosides in rat plasma was established and validated. Ginsenoside Rb1 was used as an internal standard. Plasma samples were pretreated by liquid–liquid extraction with n -butanol and chromatographed on a C18 column (2.1 × 50 mm i.d., 2.6 μm) using a gradient elution program consisting of acetonitrile and water (containing 0.03% formic acid and 0.1 mM lithium acetate) at a flow rate of 0.4 mL/min. Lithium adduct ions were employed to enhance the response of the analytes in electrospray positive ionization mode and multiple reaction monitoring transitions were performed for detection. All calibration curves exhibited good linearity ( r > 0.999) over the range of 10–20,000 ng/mL for protodioscin and 2–4000 ng/mL for protogracillin, pseudoprotodioscin and pseudoprotogracillin. The recoveries of the whole analytes were more than 80.3% and exhibited no severe matrix effect. Meanwhile, the intra- and inter-day precisions were all less than 10.7% and accuracies were within the range of −8.1–12.9%. The four saponins showed rapid excretion and relative high plasma concentrations when the validated method was applied to the PK study of Dioscorea nipponica extracts by intragastric administration at low, medium and high dose to rats. Moreover, the T 1/2 and AUC 0– t of each compound turned out to behave in a dose-dependent pattern by comparing them at different dose levels.
研究领域:
分析化学
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药理学
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DOI
PubMed
高影响因子
JOURNAL OF CELLULAR PHYSIOLOGY
·
2019
·Vol. 235
·期 3
·2911-2924
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IF 4.522
Qiuyue Ding,Wenda Zhang,Cheng Cheng,Fengbo Mo,Lei Chen,Guangfu Peng,Xianyi Cai,Jinglong Wang,Shuhua Yang,Xianzhe Liu
Pyroptosis is a form of programmed cell death (PCD) that plays a vital role in immunity and diseases. Although it was recently reported that chemotherapy drugs can induce pyroptosis through caspase-3-dependent cleavage of gasdermin E (GSDME), the role of pyroptosis in osteosarcoma (OS) with dioscin is less understood. In this study, we explored the effects of dioscin on OS in vitro and in vivo and further elucidated the underlying molecular mechanisms and found that dioscin-triggered pyroptosis in GSDME-dependent cell death and that GSDME-N was generated by caspase-3. Furthermore, dioscin inhibited cancer cell growth by inducing G2/M arrest and apoptosis through the JNK/p38 pathway. In vivo, dioscin significantly inhibited OS proliferation. Taken together, our results demonstrate that dioscin can induce apoptosis through the JNK/p38 pathway and GSDME-dependent pyroptosis in OS, identifying it as a potential therapeutic drug for treatment of this disease. HIGHLIGHTS Dioscin triggers pyroptosis in osteosarcoma. Gasdermin E is a mediator of dioscin-induced osteosarcoma (OS) cell death. Dioscin induces apoptosis and G2/M arrest. Dioscin inhibits OS proliferation in vitro and in vivo.
研究领域:
肿瘤学
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细胞生物学
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药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）