MOLECULES
·
2021
·Vol. 26
·期 18
·5722
·
IF 4.412
Yijie Lou,Kaxi Yu,Xiajun Wu,Zhaojun Wang,Yusheng Cui,Hanxiao Bao,Jianwei Wang,Xiurong Hu,Yunxi Ji,Guping Tang
Resveratrol (RSV) and polydatin (PD) have been widely used to treat several chronic diseases, such as atherosclerosis, pulmonary fibrosis, and diabetes, among several others. However, their low solubility hinders their further applications. In this work, we show that the solubility of PD can be boosted via its co-crystallization with L-proline (L-Pro). Two different phases of co-crystals, namely the RSV-L-Pro (RSV:L-Pro = 1:2) and PD-L-Pro (PD:L-Pro = 1: 3), have been prepared and characterized. As compared to the pristine RSV and PD, the solubility and dissolution rates of PD-L-Pro in water (pH 7.0) exhibited a 15.8% increase, whereas those of RSV-L-Pro exhibited a 13.8% decrease. A 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay of pristine RSV, PD, RSV-L-Pro, and PD-L-Pro against lung cancer cell line A549 and human embryonic kidney cell line HEK-293 indicated that both compounds showed obvious cytotoxicity against A549, but significantly reduced cytotoxicity against HEK-293, with PD/PD-L-Pro further exhibiting better biological safety than that of RSV/RSV-L-Pro. This work demonstrated that the readily available and biocompatible L-Pro can be a promising adjuvant to optimize the physical and chemical properties of RSV and PD to improve their pharmacokinetics.Keywords:resveratrol;polydatin;L-proline;pharmaceutical co-crystal;crystal structure;solubility and dissolution rate
研究领域:
药学
·
生物化学
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOMEDICINE & PHARMACOTHERAPY
·
2019
·
IF 3.743
Xiao-Jun Chen,Ying-Shan Shen,Min-Cong He,Fan Yang,Peng Yang,Feng-Xiang Pang,Wei He,Yan-ming Cao,Qiu-Shi Wei
Steroid-induced osteonecrosis of the femoral head (SONFH) is a refractory disease induced by glucocorticoids. Marrow mesenchymal stem cells (MSCs) differentiate into multiple bone matrix cells and have been used as cell-based therapies to treat ONFH. However, the osteogenesis of MSCs isolated from patients with SONFH is significantly decreased. Polydatin has been widely used in traditional Chinese remedies due to its multiple pharmacological actions. As shown in our previous study, Polydatin protects from oxidative stress and promotes BMSC migration. However, little is known about its role in BMSC (Bone marrow mesenchymal stem cells) osteogenesis; therefore, we further investigated the effect and mechanism of Polydatin in hBMSC osteogenesis. The ability of Polydatin to promote the proliferation and osteogenic differentiation of hBMSCs was determined using the MTT assay, ALP staining and the ALP activity assay. Next, qPCR and western blotting were performed to measure the levels of genes and proteins related to the osteogenesis of hBMSCs. Then, the effect of Polydatin on the nuclear translocation of β-catenin was determined using immunofluorescence staining. Polydatin (30 μM) markedly enhanced the proliferation of hBMSCs and alkaline phosphatase (ALP) activity. Additionally, it also significantly upregulated the expression of osteogenic genes (Runx2, osteopontin, DLX5, osteocalcin, collagen type I and BMP2) and components of the Wnt signaling pathway (β-catenin, Lef1, TCF7, c-jun, c-myc and cyclin D). These osteogenesis-potentiating effects of Polydatin were blocked by Noggin, an inhibitor of the BMP pathway, and DKK1, an inhibitor of the Wnt/β-catenin pathway. However, DKK1 did not affect Polydatin-induced BMP2 expression. Based on our results, Polydatin promotes the proliferation and osteogenic differentiation of hBMSCs through the BMP2-Wnt/β-catenin signaling pathway.
研究领域:
药理学
·
干细胞研究
·
骨科
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Engineering
·
2021
·
IF 7.553
Lu Zhao,Hao Liu,Yingchao Wang,Shufang Wang,Dejin Xun,Yi Wang,Yiyu Cheng,Boli Zhang
Xuanfeibaidu Formula (XFBD) is a Chinese medicine used in the clinical treatment of coronavirus disease 2019 (COVID-19) patients. Although XFBD has exhibited significant therapeutic efficacy in clinical practice, its underlying pharmacological mechanism remains unclear. Here, we combine a comprehensive research approach that includes network pharmacology, transcriptomics, and bioassays in multiple model systems to investigate the pharmacological mechanism of XFBD and its bioactive substances. High-resolution mass spectrometry was combined with molecular networking to profile the major active substances in XFBD. A total of 104 compounds were identified or tentatively characterized, including flavonoids, terpenes, carboxylic acids, and other types of constituents. Based on the chemical composition of XFBD, a network pharmacology-based analysis identified inflammation-related pathways as primary targets. Thus, we examined the anti-inflammation activity of XFBD in a lipopolysaccharide-induced acute inflammation mice model. XFBD significantly alleviated pulmonary inflammation and decreased the level of serum proinflammatory cytokines. Transcriptomic profiling suggested that genes related to macrophage function were differently expressed after XFBD treatment. Consequently, the effects of XFBD on macrophage activation and mobilization were investigated in a macrophage cell line and a zebrafish wounding model. XFBD exerts strong inhibitory effects on both macrophage activation and migration. Moreover, through multimodal screening, we further identified the major components and compounds from the different herbs of XFBD that mediate its anti-inflammation function. Active components from XFBD, including Polygoni cuspidati Rhizoma , Phragmitis Rhizoma , and Citri grandis Exocarpium rubrum , were then found to strongly downregulate macrophage activation, and polydatin, isoliquiritin, and acteoside were identified as active compounds. Components of Artemisiae annuae Herba and Ephedrae Herba were found to substantially inhibit endogenous macrophage migration, while the presence of ephedrine, atractylenolide I, and kaempferol was attributed to these effects. In summary, our study explores the pharmacological mechanism and effective components of XFBD in inflammation regulation via multimodal approaches, and thereby provides a biological illustration of the clinical efficacy of XFBD.
研究领域:
药理学
·
免疫学
·
转录组学
·
中医药
·
生物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2025
·
IF 9.8
Yanhong Bi,Ruiping Fu,Weiliang Hua,Xinyu Xiong,Chun Zhu,Xiaobao Nie,Zhaoyu Wang
The potential extractability, effectiveness, and stability of choline chloride/lactic acid (ChCl/HL) eutectics for 18 natural polyhydroxy compounds was investigated. Ultrasound-assisted ChCl/HL extraction exhibited exceptional extraction capabilities for polydatin (26.34 ± 0.44 mg/g) and black plum peel pigment (8.14 ± 0.16 mg/g), enhancements of 68.85 % and 40.34 %, respectively, over corresponding non-ultrasound systems. Certain comparative studies have reported yield 60.86–283.41 % and 71.58–317.04 % increases in glycoside and pigment analog extraction, respectively, demonstrating the broad applicability of ChCl/HL coupled with the ultrasound system. Further study revealed that the recovered pigments in the ChCl/HL system were 1.24– to 4.47–fold more than those in traditional solvents after 25 days of storage at 25 °C. An analysis of structure-function relationship revealed that the ability of ChCl/HL to extract and stabilize compounds depends on its strong hydrogen-bonding ability and the hydrogen bonding network among the H 2 O, extract, DES, and matrix.
研究领域:
植物化学
·
天然产物研究
·
食品科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
IMMUNOPHARMACOLOGY AND IMMUNOTOXICOLOGY
·
2021
·
IF 2.73
Shengyu Sun,Yourui Zou,Shaocai Hao,Zhanfeng Niu,Liang Wu
Objective Polydatin has been used in the treatment of various inflammatory diseases. However, its role in the regulation of neuroinflammation has not been reported. In this study, we designed to investigate the anti-inflammatory effects of polydatin in LPS-stimulated BV2 microglia cells.Methods Inflammatory mediators TNF-α, IL-1β, NO, and PGE2 production were measured by ELISA. The protein of signaling pathways were detected by western blot analysis.Results The results showed that polydatin significantly ameliorated the production of TNF-α, IL-1β, NO, and PGE2 up-regulated by LPS. Polydatin also blocked LPS-induced NF-κB activation. In addition, PI3K and AKT, the up-stream molecules of NF-κB signaling pathway, were inhibited by the treatment of polydatin. Also, we found the formation of lipid rafts was inhibited by polydatin through attenuating the cholesterol content. Finally, polydatin was found to increase the expression of ABCA1 and ABCG1.Conclusion In conclusion, the results of the present study suggested that polydatin exhibited its anti-inflammatory effects in BV2 cells through disrupting lipid rafts, which subsequently inhibiting PI3K/AKT signaling pathway.
研究领域:
药理学
·
神经科学
·
免疫学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Microbial Biotechnology
·
2020
·Vol. 13
·期 4
·1118-1131
·
IF 5.328
Tao Ma,W. Wu,Y. Tu,N. Zhang,Q. Diao
Summary This study aimed to investigate the effect of resveratrol on methane production, rumen fermentation and microbial composition under high-concentrate (HC) and high-forage (HF) diets using the in vitro fermentation system. A total of 25 mg of resveratrol was supplemented into 300 mg of either HC or HF diet. Methane production, total volatile fatty acid (VFA) concentration, molar proportion of VFA, metabolites of resveratrol and prokaryotic community composition were measured after 12 and 24 h of in vitro fermentation. Resveratrol reduced methane production (ml per mg of dry matter degraded) by 41% and 60% under both HC and HF diets ( P < 0.001), respectively, and this result could be associated with the lower abundance of Methanobrevibacter ( P < 0.001) in response to resveratrol. The molar proportion of propionate was significantly higher in the resveratrol group only under the HC diet ( P = 0.045). The relative abundance of 10 bacterial genera was affected by the three-way interaction of treatment, diet and time ( P < 0.05). Resveratrol was partly converted to dihydroresveratrol after 24 h of fermentation, and its degradation could be associated with microbes belonging to the order Coriobacteriales . Our results suggest that multiple factors (e.g. diet and time) should be considered in animal experiments to test the effect of polyphenol or other plant extracts on rumen fermentation, methane emission and microbial composition.
研究领域:
动物科学
·
微生物学
·
营养学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
·
2021
·
IF 3.205
Zilong Chen,Hongdong Liu,Jie Chen,Weifeng Zhu,Yong Liu,Jianxin Min,Xiaotian Chen,Bin Li,Xin Yang
In this work, a novel strategy was developed for separation and enrichment of sibiskoside by dummy molecular imprinting technology and magnetic separation technology. The structural analogue geniposide was selected as the dummy template, using 4-vinylpyridine as the functional monomer, ethylene glycol dimethacrylate as the cross-linking agent, and acetonitrile as the porogen. The molecularly imprinted layer was formed on the surface of the magnetic carrier to prepare dummy template molecularly imprinted polymers (DMIPs) with a core–shell structure. The DMIPs were characterized by scanning electron microscope (SEM), Fourier transform infrared spectroscopy (FT-IR), thermogravimetric analysis (TGA) and Vibration sample magnetometer (VSM). The results of adsorption kinetics experiments and isothermal adsorption experiments showed that DMIPs can reach adsorption equilibrium in a short period of time and the maximum adsorption capacity can reach 14.67 mg/g. The imprinting factor was 2.08. Compared with the andrographolide, polydatin, arbutin, caffeic acid, neohesperidin dihydrochalcone and quercetin, DMIPs have good adsorption capacity for the sibiskoside. And the reusability was better. After the adsorption of DMIPs, the purity of sibiskoside in the crude extracts from Sibiraea angustata increased to 78%. It provided a basis for the further development and utilization of Sibiraea angustata as well as the separation and enrichment of monoterpenes.
研究领域:
植物化学
·
分离科学
·
药物开发
✓ 已验证
产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2018
·Vol. 8
·期 46
·25941-25948
·
IF 2.936
Shujing Li,Li Yuan,Bing Zhang,Wei Zhou,Xinrui Wang,Dongsheng Bai
The inclusion complexes of trans-polydatin and three cyclodextrins (CDs), namely β-cyclodextrin (β-CD), methyl-β-cyclodextrin (Me-β-CD) and (2-hydroxy) propyl-β-cyclodextrin (HP-β-CD) were prepared. The effects of the inclusion behavior of trans-polydatin with three kinds of CDs were investigated in both solution and the solid state with the following methods: phase-solubility, X-ray diffraction (XRD), thermogravimetric analysis (TG), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM), proton nuclear magnetic resonance (1H-NMR) and two-dimensional rotational frame nuclear overhauser effect spectroscopy (2D ROESY). The results indicated that trans-polydatin formed a 1 : 1 stoichiometric inclusion complex with CDs. Meanwhile, the solubility and thermal stability of the inclusion complexes were improved after encapsulating by CDs. Furthermore, the photostability of trans-polydatin was enhanced after forming the inclusion complexes. The antioxidant activities results showed that the antioxidant performance of the inclusion complexes was enhanced in comparison to the native trans-polydatin. Therefore, it can be a potentially promising way to promote its drug bioavailability or phytochemical preparations.
研究领域:
药剂学
·
植物化学
·
分析化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CELLULAR AND MOLECULAR BIOLOGY
·
2019
·Vol. 65
·期 7
·
IF 1.463
Lijuan Wang,Liji Huang,Nan Li,Junjun Miao,Wei Liu,Jiangyi Yu
To investigate the effect of polydatin on glucose transporter, blood glucose homeostasis and renal injury in streptozotocin (STZ)-induced diabetic rats. The in vitro inhibitory effect of polydatin on sodium-glucose cotransporter-1 (SGLT1) and 2 (SGLT2) was determined using HEK293 cells. The inhibitory effect of polydatin on GLUT1 and GLUT4 was evaluated using 3T3-L1 adipocytes. Streptozotocin-induced diabetic rats were used for this study. Fasting blood glucose (FBG), glycosylated hemoglobin (HbA1c), urea nitrogen, serum creatinine and urinary protein were determined using biochemical analyzer. Histopathological examination was performed on renal tissue. Serum levels of interleukin 1β (IL-1β), tumor necrosis factor α (TNF-α), monocyte chemoattractant protein 1 (MCP-1) and C-reactive protein (CRP) were also determined. Polydatin significantly inhibited SGLT1/2 and exhibited high selectivity for both GLUT1 and GLUT4. It significantly and dose-dependently decreased hyperglycemia, enhanced urine glucose excretion in the diabetic rats. The polydatin treatment significantly ameliorated symptoms of DN such as polyuria, polydipsia and hyperphagia. The hypoglycemic effect of polydatin was maintained throughout the treatment period. In addition,the levels of IL-1β, TNF-α, MCP-1 and CRP were significantly reduced in treated group. Treatment with polydatin significantly ameliorated most of the structural and morphological changes induced by STZ. Moreover, the levels of urinary protein, serum creatinine and urea nitrogen were significantly reduced after treatment with polydatin. As a potential dual inhibitor of SGLT1/2, polydatin has high selectivity for GLUT1 and GLUT4. Its long-term administration delays the development of DN, protects renal function and ameliorates renal tissue injury.
研究领域:
药理学
·
内分泌学
·
分子生物学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF CELLULAR AND MOLECULAR MEDICINE
·
2018
·Vol. 22
·期 11
·5720-5731
·
IF 4.302
Jianle Wang,Chongan Huang,Zongze Lin,Xiangxiang Pan,Jiaoxiang Chen,Gang Zheng,Naifeng Tian,Yingzhao Yan,Zengjie Zhang,Jianing Hu,Pu Cheng,Xiangyang Wang,Xiaolei Zhang
Intervertebral disc degeneration (IVDD) is one of the major causes of low back pain. Polydatin (PD) has been shown to exert multiple pharmacological effects on different diseases; here, we test the therapeutic potential of PD for IVDD. In in-vitro experiments, we confirmed PD is nontoxic to nucleus pulposus cells (NPCs) under the concentration of 400 μmol/L. Furthermore, PD was able to decrease the level of senescence in TNF-α-treated NPCs, as indicated by β-gal staining as well as senescence markers p53 and p16 expression. In the aspect of extracellular matrix (ECM), PD not only reduced metalloproteinase 3 (MMP-3), metalloproteinase 13 (MMP-13) and a disintegrin-like and metalloproteinase thrombospondin type 1 motif 4 (ADAMTS-4) expression, but also increased aggrecan and collagen II levels. Mitochondrion is closely related to cellular senescence and ECM homeostasis; mechanistically, we found PD may rescue TNF-α-induced mitochondrial dysfunction, and it may also promote Nrf2 expression and activity. Silencing Nrf2 partly abolished the protective effects of PD on mitochondrial homeostasis, senescence and ECM homeostasis in TNF-α-treated NPCs. Correspondingly, PD ameliorated IVDD in rat model by promoting Nrf2 activity, preserving ECM and inhibiting senescence in nucleus pulposus cells. To sum up, our study suggests that PD exerts protective effects in NPCs against IVDD and reveals the underlying mechanism of PD on Nrf2 activation in NPCs.
研究领域:
药理学
·
骨科
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF FOOD SCIENCE
·
2015
·Vol. 80
·期 6
·C1156
·
IF 1.696
Benguo Liu,Yun Li,Huizhi Xiao,Yonglan Liu,Haizhen Mo,Hanjun Ma,Guizhao Liang
en This link goes to a English section pt This link goes to a English section Polydatin is the main bioactive ingredient in many medicinal plants, such as Hu-zhang ( Polygonum cuspidatum ), with many bioactivities. However, its poor aqueous solubility restricts its application in functional food. In this work, 6-O-α-Maltosyl-β-cyclodextrin (Malt-β-CD), a new kind of β-CD derivative was used to enhance the aqueous solubility and stability of polydatin by forming the inclusion complex. The phase solubility study showed that polydatin and Malt-β-CD could form the complex with the stoichiometric ratio of 1:1. The supermolecular structure of the polydatin/Malt-β-CD complex was characterized by ultraviolet–visible spectroscopy (UV), Fourier transform infrared spectroscopy (FT-IR), X-ray diffractometry (XRD), thermogravimetric/differential scanning calorimetry (TG/DSC), and proton nuclear magnetic resonance ( 1 H-NMR) spectroscopy. The changes of the characteristic spectral and thermal properties of polydatin suggested that polydatin could entrap inside the cavity of Malt-β-CD. Furthermore, to reasonably understand the complexation mode, the supermolecular structure of polydatin/Malt-β-CD inclusion complex was postulated by a molecular docking method based on Autodock 4.2.3. It was clearly observed that the ring B of polydatin oriented toward the narrow rim of Malt-β-CD with ring A and glucosyl group practically exposed to the wide rim by hydrogen bonding, which was in a good agreement with the spectral data. Practical Application en This link goes to a English section pt This link goes to a English section Polydatin was a nutraceutical with potential prospect in functional food. In this study, 6-O-α-Maltosyl-β-cyclodextrin, a new kind of β-CD derivative was used to improve its poor aqueous solubility by forming the inclusion complex, which can be used to develop new functional food. The introduced spectral technologies and molecular docking method could be used to characterize other complexes of bioactive compounds with CDs.
研究领域:
药剂学
·
食品科学
·
生物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PLoS One
·
2015
·Vol. 10
·期 2
·e0116879
·
IF 3.234
Li Zhang,Yuanyuan Li,Zhiwen Gu,Yuyue Wang,Mei Shi,Yun Ji,Jing Sun,Xiaopeng Xu,Lirong Zhang,Jingtin Jiang,Weifeng Shi
Polydatin and resveratrol, as major active components in Polygonum cuspidatum , have anti-inflammatory, antioxidant and antitumor functions. However, the effect and mechanism of polydatin and resveratrol on enterovirus 71 (EV71) have not been reported. In this study, resveratrol revealed strong antiviral activity on EV71, while polydatin had weak effect. Neither polydatin nor resveratrol exhibited influence on viral attachment. Resveratrol could effectively inhibit the synthesis of EV71/VP1 and the phosphorylation of IKKα, IKKβ, IKKγ, IKBα, NF-κB p50 and NF-κB p65, respectively. Meanwhile, the remarkably increased secretion of IL-6 and TNF-α in EV71-infected rhabdosarcoma (RD) cells could be blocked by resveratrol. These results demonstrated that resveratrol inhibited EV71 replication and cytokine secretion in EV71-infected RD cells through blocking IKKs/NF-κB signaling pathway. Thus, resveratrol may have potent antiviral effect on EV71 infection.
研究领域:
病毒学
·
药理学
·
分子生物学
✓ 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）