JOURNAL OF ETHNOPHARMACOLOGY
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2022
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IF 5.195
Lin Niu,Jie Wang,Fukui Shen,Jie Gao,Min Jiang,Gang Bai
Ethnopharmacological relevance Magnolia officinalis Cortex ( M. officinalis ) is a classical traditional Chinese medicine (TCM) widely used to treat digestive system diseases . It effectively regulates gastrointestinal motility to improve abdominal pain, abdominal distension and other symptoms. Magnolol (MAG) and honokiol (HON) are the main pharmacodynamic components responsible for the gastrointestinal activity of M. officinalis . Aim of the study The transient receptor potential (TRP) family is highly expressed in the gastrointestinal tract and participates in the regulation of gastrointestinal motility, visceral hypersensitivity, visceral secretion and other physiological activities. In this study, the calcium-lowering mechanisms of MAG and HON contributing to the smooth muscle relaxation associated with TRP are discussed. Materials and methods The relaxation smooth muscle effects of MAG and HON were tested by the isolated intestine tone tests. A synthetic MAG probe (MAG-P) was used to target fishing for their possible target. The distribution of MAG on the smooth muscle was identified by a molecular tracer based on chemical biology. Ca 2+ imaging and dual-luciferase reporter assays were used to determine the effects on the target proteins. Finally, the calcium-mediating effects of MAG and HON on smooth muscle cells and TRPC4-knockdown cells were compared to verify the potential mechanism. Results After confirming the smooth muscle relaxation in the small intestine induced by MAG and HON, the relaxation effect was identified mainly due to the downregulation of intracellular calcium by controlling external calcium influx. Although MAG and HON inhibited both TRPV4 and TRPC4 channels to reduce calcium levels, the inhibitory effect on TRPC4 channels is an important mechanism of their smooth muscle relaxation effect, since TRPC4 is widely expressed in the small intestinal smooth muscle cells. Conclusions The inhibition of MAG and HON on TRPC4 channels contributes to the relaxation of intestinal smooth muscle.
研究领域:
药理学
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胃肠病学
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传统中药
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细胞生物学
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产品关联
DOI
PubMed
高影响因子
EUROPEAN FOOD RESEARCH AND TECHNOLOGY
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2014
·Vol. 240
·期 4
·815-822
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IF 1.387
Tan Li-Hong,Zhang Dan,Yu Bao,Zhao Sheng-Ping,Cao Wei-Guo
The leaf of Magnolia officinalis is abundant in natural resources as a novel potential antioxidant and has great commercial value. In this study, the contents of total phenolics, total flavonoids, magnolol and honokiol in different solvent extracts (acetone, methanol and water) were measured. Meanwhile, the antioxidant activity of extracts from M. officinalis leaves were evaluated using 1,1-diphenyl-2-picrylhydrazyl free radical scavenging assay, 2,2-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt free radical scavenging assay, FRAP assays and β-carotene/linoleic acid system. In addition, the correlation between the antioxidant activity and the contents of the active compounds was analyzed. Experimental results indicated that three extracts exhibited antioxidant effects in a concentration-dependent manner, and acetone extracts had the highest antioxidant activity, next methanol and water. There was an intimate relativity between the contents of magnolol and honokiol in different solvent extracts and the antioxidant capability of them. So the magnolol and honokiol of M. officinalis leaves as a representative of the active compounds were extracted and purified by using the macroporous resin column. The purity of depurated sample could reach 82.6 %, which indicates the M. officinalis leaves have the potential to substitute the production of magnolol and honokiol in M. officinalis . The results of this study can provide theoretical and technical references for the reasonable use of the M. officinalis leaves and alleviate the shortage of M. officinalis resources.
研究领域:
植物化学
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药用植物学
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天然产物化学
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DOI
高影响因子
Scientific Reports
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2015
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IF 5.578
Caiao Guo,Liang Ma,Yudan Zhao,Anlin Peng,Biao Cheng,Qiaoqiao Zhou,Ling Zheng,Kun Huang
Amyloid formation is associated with multiple amyloidosis diseases. Human calcitonin (hCT) is a typical amyloidogenic peptide, its aggregation is associated with medullary carcinoma of the thyroid (MTC), and also limits its clinical application. Magnolia officinalis is a traditional Chinese herbal medicine; its two major polyphenol components, magnolol (Mag) and honokiol (Hon), have displayed multiple functions. Polyphenols like flavonoids and their derivatives have been extensively studied as amyloid inhibitors. However, the anti-amyloidogenic property of a biphenyl backbone containing polyphenols such as Mag and Hon has not been reported. In this study, these two compounds were tested for their effects on hCT aggregation. We found that Mag and Hon both inhibited the amyloid formation of hCT, whereas Mag showed a stronger inhibitory effect; moreover, they both dose-dependently disassembled preformed hCT aggregates. Further immuno-dot blot and dynamic light scattering studies suggested Mag and Hon suppressed the aggregation of hCT both at the oligomerization and the fibrillation stages, while MTT-based and dye-leakage assays demonstrated that Mag and Hon effectively reduced cytotoxicity caused by hCT aggregates. Furthermore, isothermal titration calorimetry indicated Mag and Hon both interact with hCT. Together, our study suggested a potential anti-amyloidogenic property of these two compounds and their structure related derivatives.
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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中医药
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2024
·
IF 4.8
Lin Niu,Shilong Wang,Yanyan Xu,Xingwang Zu,Xinyu You,Qiuyang Zhang,Pengwei Zhuang,Min Jiang,Jie Gao,Xiaotao Hou,Yanjun Zhang,Gang Bai,Jiagang Deng
Ethnopharmacological relevance As a classic traditional Chinese medicine , Magnolia officinalis ( M . officinalis ) is widely used in digestive diseases . It has rich gastrointestinal activity including inflammatory bowel disease (IBD) treatment, but the mechanism is not clear. Aim of the study In recent years, there has been a growing interest in investigating the regulatory effects of herbal compounds on transient receptor potential (TRP) channel proteins. Transient receptor potential vanilloid 4 (TRPV4), a subtype involved in endothelial permeability regulation, was discussed as the target of M . officinalis in the treatment of IBD in the study. Based on the targeting effect of TRPV4, this study investigated the active ingredients and mechanism of M . officinalis extract in treating IBD. Materials and methods To reveal the connection between the active ingredients in M . officinalis and TRPV4, a bioactivity-guided high performance liquid chromatography system coupled with mass spectrometry identification was utilized to screen for TRPV4 antagonists. TRPV4 siRNA knockdown experiment was employed to validate the significance of TRPV4 as a crucial target in regulating endothelial permeability by honokiol (HON). The interaction of the active ingredient representing HON with TRPV4 was confirmed by molecular docking, fluorescence-based thermal shift and live cell calcium imaging experiments. The potential binding sites and inhibitory mechanisms of HON in TRPV4 were analyzed by molecular dynamics simulation and microscale thermophoresis. The therapeutic effect of HON based on TRPV4 was discussed in DSS-IBD mice. Results Our finding elucidated that the inhibitory activity of M . officinalis against TRPV4 is primarily attributed to HON analogues. The knockdown of TRPV4 expression significantly impaired the calcium regulation and permeability protection in endothelial cells. The mechanism study revealed that HON specifically targets the Q239 residue located in the ankyrin repeat domain of TRPV4, and competitively inhibits channel opening with adenosine triphosphate (ATP) binding. The immunofluorescence assay demonstrated that the administration of HON enhances the expression and location of VE-Cadherin to protect the endothelial barrier and attenuates immune cell infiltration. Conclusions The finding suggested that HON alleviates IBD by improving endothelial permeability through TRPV4. The discovery provides valuable insights into the potential therapeutic strategy of active natural products for alleviating IBD.
研究领域:
药理学
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民族药理学
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胃肠病学
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分子生物学
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细胞生物学
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产品关联
DOI
PubMed
高影响因子
HIGH PERFORMANCE POLYMERS
·
2024
·
IF 1.8
Ming Yuan Wang,Shou Wu Yu,Chen Jing Zhao,Tian Yu Zhang,Gui Xiang Hou
Reducing the dependence of epoxy resin preparation on petroleum resources and developing thermosetting epoxy resins with excellent comprehensive performance are important directions for the current development of epoxy resins. This article uses biomass resource magnolol as the main raw material to prepare magnolol epoxy monomer (DGEM). Then, using 4,4-diaminodiphenylmethane (DDM) as the curing agent, the DGEM and bisphenol A epoxy resin (E44) were blended and cured. The results showed a dual modification effect of DGEM on the toughening and strengthening of E44 epoxy resin. When the mass ratio of DGEM to E44 is 30:70, the bending strength of the cured blended resin is 18.7% higher than that of the E44 system, and the tensile strength is 57.7% higher. When the mass ratio of DGEM to E44 is 5:95, the cured blended resin exhibits the optimal impact strength (5.10 kJ/mol), which is 22.9% higher than the pure E44 system. However, the addition of DGEM reduced the glass transition temperature and crosslinking degree of the blended resin system. The addition of DGEM improves the heat resistance and flame retardancy of the blended resin. When the mass ratio of DGEM: E44 was 50:50, the vertical combustion reached UL-94 V-0 level.
研究领域:
材料科学
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生物质资源利用
✓ 已验证
DOI
高影响因子
Viruses-Basel
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2022
·Vol. 14
·期 7
·1421
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IF 5.818
Yingjie Jin,Fei Yang,Gengrong Zhang,Qing Yu,Gaoxue Wang,Fei Ling,Tianqiang Liu
Micropterus salmoidesrhabdovirus (MSRV) is a primary viral pathogen in largemouth bass aquaculture, which leads to tremendous economic losses yearly. Currently, there are no approved drugs for the treatment and control of this virus. Our previous studies screened the herbMagnolia officinalisfrom many traditional Chinese medicines, and we isolated and identified magnolol as its main active compound against multiple rhabdoviruses, including MSRV. On the basis of the structure–activity relationship and pharmacophore model of magnolol, two new magnolol derivatives, namely, hydrogenated magnolol and 2,2′-dimethoxy-magnolol, were designed and synthesized. Their anti-MSRV activities were systematically investigated both in vitro and in vivo. By comparing the half-maximal inhibitory concentration (IC50), it was found that hydrogenated magnolol possessed a higher anti-MSRV activity than magnolol and 2,2′-dimethoxy-magnolol, with an IC50of 13.37 μM. Furthermore, hydrogenated magnolol exhibited a protective effect on the grass carp ovary (GCO) cell line by reducing the cytopathic effect induced by MSRV. Further studies revealed that hydrogenated magnolol did not directly impact virions or interfere with MSRV adsorption. It worked within the 6–8 h of the phase of virus replication. In vivo treatment of MSRV infection with magnolol and hydrogenated magnolol showed that they significantly improved the survival rate by 44.6% and 62.7%, respectively, compared to MSRV-infected groups. The viral load measured by the expression of viral glycoprotein in the organs including the liver, spleen, and kidney also significantly decreased when fish were intraperitoneally injected at a dose of 20 mg/kg. Altogether, the structural optimization of magnolol via hydrogenation of the propylene groups increased its anti-MSRV activity both in vitro and in vivo. These results may provide a valuable reference for anti-MSRV drug discovery and development in aquaculture.Keywords:Micropterus salmoidesrhabdovirus (MSRV);magnolol;largemouth bass;antiviral activity
研究领域:
水产养殖学
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病毒学
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药物化学
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DOI
PubMed
高影响因子
Journal of Oleo Science
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2022
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IF 1.628
Yi-Xi Feng,Xin-Xin Lu,Yue-Shen Du,Yu Zheng,Ding Zeng,Shu-Shan Du
Stored products have been damaged by insects. Multiple approaches for pest management are employed. Among these approaches, botanical insecticide is an emerging one. This work investigated the pest management potential of Magnolia coriacea and Magnolia macclurei essential oils (EOs) to three major stored-product insects, namely the red flour beetle, cigarette beetle and booklouse. Magnolia coriacea and M. macclurei EOs showed promising contact toxicity to the cigarette beetle, with LD50 values of 11.7 and 12.3 μg/adult. The contact toxicity of M. coriacea EOs to the booklouse (LC50 = 95.5 μg/cm2) was much stronger than that of M. macclurei EOs (LC50 = 245.4 μg/cm2). To explore the contribution of individual compounds to insecticidal activity of EOs, chemical analysis was performed by GC-MS. Results showed that nerolidol (27.84%), agarospirol (18.34%), elixene (15.84%) and helminthogermacrene (12.69%) were major compounds of M. coriacea EOs, β-guaiene (60.31%) and elixene (20.42%) dominated in M. macclurei EOs. Nerolidol and β-guaiene showed contact activity to three insect species. Nerolidol showed stronger contact toxicity to the red flour beetle and cigarette beetle than M. coriacea EOs did, both samples were similar to the booklouse. β-Guaiene was much stronger to the red flour beetle and booklouse, but weaker to the cigarette beetle than M. macclurei EOs did. The repellent effects of EOs and compounds were at various levels. Generally, results suggested that the contact toxic potential of samples could serve as management for the cigarette beetle and booklouse, while repellent effect would be used to control the red flour beetle.
研究领域:
植物学
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昆虫学
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害虫管理
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化学生态学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF FISH DISEASES
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2022
·Vol. 45
·期 11
·1599-1607
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IF 2.58
Xin-Yuan Jiang,Zong-Yi Ren,Nian-Kun Zhang,Ke-Chen Yang,Gao-Xue Wang,Hai-Feng Jiang
Nocardiosis caused by Nocardia seriolae is a major threat to the aquaculture industry. Given that prolonged therapy administration can lead to a growth of antibiotic resistant strains, new antibacterial agents and alternative strategies are urgently needed. In this study, 80 medicinal plants were selected for antibacterial screening to obtain potent bioactive compounds against N. seriolae infection. The methanolic extracts of Magnolia officinalis exhibited the strongest antibacterial activity against N. seriolae with the minimal inhibitory concentration (MIC) of 12.5 μg/ml. Honokiol and magnolol as the main bioactive components of M. officinalis showed higher activity with the MIC value of 3.12 and 6.25 μg/ml, respectively. Sequentially, the evaluation of antibacterial activity of honokiol in vivo showed that honokiol had good biosafety, and could significantly reduce the bacterial load of nocardia-infected largemouth bass ( p < .001). Furthermore, the survival rate of nocardia-infected fish fed with 100 mg/kg honokiol was obviously improved ( p < .05). Collectively, these results suggest that medicinal plants represent a promising reservoir for discovering active components against Nocardia , and honokiol has great potential to be developed as therapeutic agents to control nocardiosis in aquaculture.
研究领域:
水产养殖学
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药用植物学
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微生物学
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产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACOLOGY
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2024
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IF 4.2
Yi Chu,Sisi Gui,Yazhen Zheng,Jingwu Zhao,Yaxiang Zhao,Yingying Li,Xiaodong Chen
Non-alcoholic fatty liver disease (NAFLD) is closely associated with the body's energy metabolism. A potential strategy to regulate energy metabolism, combat obesity, and reduce NAFLD is by enhancing adipocyte thermogenesis and increasing energy expenditure. In this study, our objective was to examine the effects of phenolic extracts derived from Magnolia officinalis on the regulation of NAFLD. Specifically, we investigated the impact of Magnolol or Honokiol treatment on high-fat diet (HFD)-induced obese C57BL6/J male mice. Firstly, we monitored energy metabolism, dissected tissues, and analyzed tissue sections. Additionally, we conducted experiments on HepG2 and primary adipocytes to gain insights into the roles of Magnolol or Honokiol. To further understand the effects of these compounds on related signaling pathways and marker genes, we performed molecular docking, dual-luciferase assays, and interfered with target genes. Our findings revealed that Magnolol or Honokiol activate the peroxisome proliferator activated receptor alpha (PPARα) signaling pathway, leading to the alleviation of NAFLD. This activation promotes fatty acid oxidation, reduces lipogenesis, and enhances the expression and secretion of FGF21. Notably, Fibroblast growth factor 21 (FGF21), secreted by the liver, plays a crucial role in improving communication between the liver and adipocytes while also promoting the browning of adipose tissue. Additionally, Magnolol or Honokiol activate the peroxisome proliferator activated receptor gamma (PPARγ) signaling pathway, resulting in increased uncoupling protein 1 (UCP1) expression, heightened heat production in adipose tissue, and anti-obesity. Therefore, Magnolol or Honokiol alleviate NAFLD, promote adipose tissue browning and resist obesity through dual activation of PPARα/γ.
研究领域:
药理学
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代谢
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分子生物学
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营养学
✓ 已验证
DOI
PubMed
高影响因子
REACTIVE & FUNCTIONAL POLYMERS
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2024
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IF 4.5
Xinru Bai,Zhiyong Li,Yuting Dong,Xinyi Gao,Jingjing Meng
The magnolol- (MEP) and honokiol-epoxy resin (HEP) were prepared from the extract of the natural plant Magnolia officinalis. Those monomers were cured with hardeners, such as 4,4-diamino diphenyl sulfone (DDS) and 4,4′-bis (3-aminophenoxy) diphenyl sulfone (BDS), respectively via solvent-free process to fabricate networks with excellent mechanical properties. The curing procedures occurred in a wide temperature interval (65 °C), which made the concerning vacuum-assisted resin infusion feasible. Notedly, all combinations exhibited increased thermal stability ( T d5 , 359.7–381.9 °C) with T max fluctuating around 450 °C. The phase transition temperature ( T α ) screen suggested that except MEP/BDS ( T α , 147.2 °C), other combinations varied from 264.2 °C to 281.2 °C. In addition, DDS allowed the networks with slightly lower thermal expansion coefficients ( CTE, 68.1 ppm/ o C, <180 °C for HEP/DDS), while the BDS yielded relatively high CTE values (87.1 ppm/ o C, <106 °C, for MEP/BDS). The LOI value (33 %) and vertical burning test (UL-94) indicated their outstanding flame retardancy (UL 94 V -0). Furthermore, for MEP/BDS, the unique solvolysis (in DMF or THF) and thermally induced shape memory properties along with the superior flame retardancy demonstrated its overall high performances. As a whole, these performance improvements further facilitate the high-end applications of sustainable resins in cutting-edge areas.
研究领域:
材料科学
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化学工程
✓ 已验证
产品关联
DOI
高影响因子
Pharmaceuticals
·
2024
·Vol. 17
·期 11
·1416
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IF 4.3
Ziang Zhou,Yumeng Wang,Yu Xing,Shuman Pan,Wanru Wang,Jie Yang,Wenyuan Wu,Jie Zhou,Luyi Huang,Qiongdan Liang,Dongmei Zhang,Lingdong Kong
Background/Objectives: High fructose has been implicated as an important trigger of kidney inflammation in patients and experimental models. Magnolol, isolated fromMagnolia officinalis, has an anti-inflammatory effect, but its protective role in podocytes remains underexplored. This study explored the protective effects and underlying mechanism of magnolol against high fructose-induced podocyte inflammation. Methods: The effects of magnolol on high fructose-induced podocyte inflammation were assessed in male Sprague Dawley rats administered 10% (w/v) fructose water for 12 weeks and heat-sensitive human podocyte cell lines (HPCs) exposed to 5 mM fructose. Podocyte foot processes were examined using transmission electron microscopy. The expression levels of nephrin, podocin, tumor necrosis factor-α (TNF-α), Notch1 intracellular domain (NICD1), triokinase/FMN cyclase (TKFC), specificity protein 1 (Sp1) and histone deacetylase 4 (HDAC4) were determined by Western blot, immunofluorescence and real-time quantitative polymerase chain reaction (qRT-PCR). The chromatin immunoprecipitation (ChIP) assay was performed to evaluate the interaction between Sp1 and the promoter region of HDAC4. Results: Magnolol mitigated the impairment of glomerular filtration function in high fructose-fed rats. Besides, it significantly alleviated the inflammatory responses in glomeruli and HPCs, evidenced by decreased protein levels of TNF-α and NICD1. Increased protein levels of TKFC, Sp1 and HDAC4 were observed in high fructose-stimulated HPCs and rat glomeruli. TMP195, an HDAC4 inhibitor, reduced TNF-α and NICD1 protein levels in high fructose-exposed HPCs. The increased Sp1 was shown to associate with the promoter region of HDAC4, promoting HDAC4 protein expression in high fructose-exposed HPCs. The knockdown of TKFC in HPCs byTKFCsiRNA decreased Sp1, HDAC4 and NICD1 protein levels, alleviating podocyte inflammatory response. Furthermore, magnolol inhibited TKFC/Sp1/HDAC4/Notch1 activation in vivo and in vitro. Conclusions: Magnolol attenuated high fructose-induced podocyte inflammation possibly through the suppression of TKFC/Sp1/HDAC4/Notch1 activation, providing new evidence for its potential role in podocyte protection.
研究领域:
药理学
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肾病学
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分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2021
·Vol. 22
·期 15
·7769
·
IF 5.924
Xueying Song,Liu Liu,Xiaoxia Wu,Yongfeng Liu,Jialu Yuan
The aims of this study were to develop the magnolol–chitosan films and study the positive effect of the combination of magnolol and chitosan. The addition of magnolol made the magnolol–chitosan films exhibit higher density (1.06–1.87 g/cm3), but the relatively lower water vapor permeability (12.06–7.36 × 10−11·g·m−1·s−1·Pa−1) and water content (16.10–10.64%). The dense and smooth surface and cross-section of magnolol–chitosan films were observed by environmental scanning electron microscopy (ESEM) images. The interaction of magnolol and chitosan was observed by X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy and thermogravimetric analysis (TGA). After the addition of magnolol, the antioxidant capacity of magnolol–chitosan films was increased from 18.99 to 82.00%, the growth ofP. aeruginosawas inhibited and the inhibition percentage of biofilm formation was increased from 30.89 to 86.04%. We further verified that the application of magnolol–chitosan films on chilled pork significantly reduced the increases in pH value, inhibited the growth of microorganisms and extended the shelf life. Results suggest that magnolol had a positive effect on magnolol–chitosan films and could be effectively applied to pork preservation.Keywords:magnolol;chitosan;film;antimicrobial;pork
研究领域:
食品科学
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生物材料学
✓ 已验证
产品关联
DOI
PubMed
高影响因子