Quercetin

槲皮素
  • 文章类型: Journal Article
    β-葡聚糖是在各种真菌的细胞壁中发现的多糖,细菌和谷物。β-葡聚糖已被发现显示各种抗炎,抗菌,抗糖尿病抗氧化和抗癌活性。在本研究中,我们从面包师的酵母酿酒酵母和白色纽扣蘑菇双孢蘑菇中分离出β-葡聚糖,并测试了它们对前列腺癌细胞系PC3的抗氧化潜力和抗癌活性。用ζ分析仪和进一步用FTIR表征颗粒,其证实分离的颗粒是β-葡聚糖和藻酸盐密封,使得槲皮素从β-葡聚糖颗粒中缓慢和持续地释放。用SEM分析进行中空和装载槲皮素的β-葡聚糖的形态分析,并且用TGA和DSC分析进行稳定性分析,其显示藻酸盐密封颗粒的较高稳定性。抗氧化潜力的评估显示,负载槲皮素的颗粒具有比中空β-葡聚糖颗粒更高的抗氧化活性。用MTT测定法检查PC3细胞的细胞活力,发现负载槲皮素的藻酸盐密封的双孢蘑菇来源的β-葡聚糖颗粒具有最低的IC50。发现进一步的ROS产生以剂量依赖性方式增加。用碘化丙锭和AO/EtBr染色染料进行凋亡检测,其在用较高浓度的颗粒处理的细胞中显示出显著的死亡。研究表明,源自两种来源的颗粒具有有效的抗癌活性,并且在处理后显示PC3细胞中细胞死亡的剂量依赖性增加。
    β-glucans are polysaccharides found in the cell walls of various fungi, bacteria and cereals. β-glucan have been found to show various kinds of anti-inflammatory, antimicrobial, antidiabetic antioxidant and anticancerous activities. In the present study, we have isolated β-glucan from the baker\'s yeast Saccharomyces cerevisiae and white button mushroom Agaricus bisporus and tested their antioxidant potential and anticancerous activity against prostate cancer cell line PC3. Particles were characterized with zeta sizer and further with FTIR that confirmed that the isolated particles are β-glucan and alginate sealing made slow and sustained release of the Quercetin from the β-glucan particles. Morphological analysis of the hollow and Quercetin loaded β-glucan was performed with the SEM analysis and stability was analyzed with TGA and DSC analysis that showed the higher stability of the alginate sealed particles. Assessments of the antioxidant potential showed that Quercetin loaded particles were having higher antioxidant activity than hollow β-glucan particles. Cell viability of the PC3 cells was examined with MTT assay and it was found that Quercetin loaded alginate sealed Agaricus bisporus derived β-glucan particles were having lowest IC50. Further ROS generation was found to increase in a dose dependent manner. Apoptosis detection was carried out with Propidium iodide and AO/EtBr staining dye which showed significant death in the cells treated with higher concentration of the particles. Study showed that particles derived from both of the sources were having efficient anticancer activity and showing a dose dependent increase in cell death in PC3 cells upon treatment.
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  • 文章类型: Journal Article
    由于上皮-间质转化(EMT),乳腺癌(BC)细胞具有很高的转移风险。Palbociclib(CDK4/6抑制剂)是一种批准用于BC治疗的药物。然而,耐药和转移可影响Palbociclib的治疗效果。了解BC中EMT和Palbociclib耐药的机制有助于制定新的治疗策略。这里,我们研究了circHIAT1/miR-19a-3p/CADM2轴在调节BCEMT和Palbociclib耐药中的作用.cirHIAT1和CADM2在BC组织和细胞系中下调,和miR-19a-3p显示上调。cirHIAT1可以与miR-19a-3p相互作用并抑制其活性,而miR-19a-3p负向调节CADM2。circHIAT1的过度表达可损害BC细胞的EMT状态和迁移能力,这种效应被miR-19a-3p模拟物抑制。此外,我们还产生了Palbociclib抗性BC细胞,并显示circHIAT1和CADM2在抗性BC细胞中下调,而miR-19a-3p显示上调。强制circHIAT1过表达使BC细胞对Palbociclib治疗敏感。槲皮素,一种生物活性类黄酮,可以抑制BC细胞的迁移和侵袭,并使BC细胞对Palbociclib重新敏感。槲皮素的抗癌作用可归因于其对circHIAT1/miR-19a-3p/CADM2轴的调节作用。体内肿瘤发生实验进一步表明槲皮素的给药增强了Palbociclib的抗癌作用,该效应依赖于槲皮素对circHIAT1的上调。总之,这项研究确定槲皮素是一种潜在的抗癌化合物,可通过靶向circHIAT1/miR-19a-3p/CADM2轴来逆转Palbociclib耐药并损害BC细胞EMT.
    Breast cancer (BC) cells have a high risk of metastasis due to epithelial-mesenchymal transition (EMT). Palbociclib (CDK4/6 inhibitor) is an approved drug for BC treatment. However, the drug resistance and metastasis can impair the treatment outcome of Palbociclib. Understanding the mechanisms of EMT and Palbociclib drug resistance in BC is conducive to the formulation of novel therapeutic strategy. Here, we investigated the role of circHIAT1/miR-19a-3p/CADM2 axis in modulating EMT and Palbociclib resistance in BC. circHIAT1 and CADM2 were down-regulated in BC tissues and cell lines, and miR-19a-3p showed an up-regulation. circHIAT1 could interact with miR-19a-3p and suppress its activity, while miR-19a-3p functioned to negatively regulate CADM2. Forced over-expression of circHIAT1 could impaired the EMT status and migratory ability of BC cells, and this effect was inhibited by miR-19a-3p mimic. In addition, we also generated Palbociclib resistant BC cells, and showed that circHIAT1 and CADM2 were down-regulated in the resistant BC cells while miR-19a-3p showed an up-regulation. Forced circHIAT1 over-expression re-sensitized BC cells to Palbociclib treatment. Quercetin, a bioactive flavonoid, could suppressed the migration and invasion of BC cells, and re-sensitized BC cells to Palbociclib. The anti-cancer effect of quercetin could be attributed to its regulatory effect on circHIAT1/miR-19a-3p/CADM2 axis. In vivo tumorigenesis experiment further revealed that quercetin administration enhanced the anti-cancer effect of Palbociclib, an effect was dependent on the up-regulation of circHIAT1 by quercetin. In summary, this study identified quercetin as a potential anti-cancer compound to reverse Palbociclib resistance and impair EMT in BC cells by targeting circHIAT1/miR-19a-3p/CADM2 axis.
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  • 文章类型: Journal Article
    Cornelian樱桃果实含有广泛的酚酸,黄酮类化合物,和其他次生代谢产物。选择的类黄酮可以抑制苦味的感知,然而,所有TAS2R苦味受体的完整机制尚不清楚。该研究的目的是通过功能性体外测定和偶联研究来确定山茱萸酚类对苦味受体TAS2R13和TAS2R3的抑制作用。通过分析用测试的矢车菊樱桃提取物处理的细胞中受体活性的抑制来验证总体效果。与两种TAS2R受体相互作用的强度在具有不同结合亲和力的研究化合物之间变化。大多数化合物通过与Trp89A和酚类和色氨酸芳环之间的π-π轨道重叠的长距离疏水相互作用与TAS2R3受体键合。对于TAS2R13,观察到与化合物相互作用的各种机制。尽管如此,柚皮苷和槲皮素与受体的模型激动剂-氯喹和地那铵具有最相似的结合亲和力。
    Cornelian cherry fruits contain a wide range of phenolic acids, flavonoids, and other secondary metabolites. Selected flavonoids may inhibit the perceiving of bitterness, however, the full mechanism with all TAS2R bitter taste receptors is not known. The aim of the study was to determine the inhibitory effect of Cornus mas phenolics against the bitterness receptors TAS2R13 and TAS2R3 through functional in vitro assays and coupling studies. The overall effect was validated by analysing the inhibition of the receptors activity in cells treated with tested cornelian cherry extracts. The strength of interaction with both TAS2R receptors varied between studied compounds with different binding affinity. Most compounds bonded with the TAS2R3 receptor through a long-distant hydrophobic interaction with Trp89A and π-π orbital overlapping-between phenolic and tryptophane aromatic rings. For TAS2R13 observed were various mechanisms of interaction with the compounds. Nonetheless, naringin and quercetin had most similar binding affinity to chloroquine and denatonium-the model agonists for the receptor.
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  • 文章类型: Journal Article
    天花属涵盖约280种,其中大部分用于医疗目的。而P.graveolens,P.ododatissimum,和P.zonale已知表现出抗菌活性,显然没有研究评估这三个物种以了解它们的化学差异和生物学效应。通过对甘草的水醇提取物的分析,P.ododatissimum,还有P.zonale,采用HPLC-DAD-MS/MS,在这三个物种中鉴定出槲皮素和山奈酚衍生物。相反,胆单宁和花色苷是在P.zonale中唯一检测到的。P.graveolens脱颖而出,由于各种类型的杨梅素衍生物,未检测到在P.ododatissimum和P.zonale提取物。对其生物活性的评估表明,与其他两个物种相比,P.zonale显示出优异的抗菌和抗生物膜活性。观察到P.zonale对金黄色葡萄球菌ATCC25923、耐甲氧西林金黄色葡萄球菌(MRSA)333、粪肠球菌ATCC29212和耐万古霉素粪肠球菌INSPI032的临床相关菌株的抗菌功效。P.zonale的分级分析表明,归因于该植物的抗菌活性是由于槲皮素衍生物和山奈酚及其衍生物的存在,以及它们与没食子酸和花色苷的协同相互作用。最后,这三种天竺葵物种表现出显著的抗氧化活性,这可能归因于它们的总酚类化合物含量高。
    The Pelargonium genus encompasses around 280 species, most of which are used for medicinal purposes. While P. graveolens, P. odoratissimum, and P. zonale are known to exhibit antimicrobial activity, there is an evident absence of studies evaluating all three species to understand their chemical differences and biological effects. Through the analysis of the hydroalcoholic extracts of P. graveolens, P. odoratissimum, and P. zonale, using HPLC-DAD-MS/MS, quercetin and kaempferol derivatives were identified in these three species. Conversely, gallotannins and anthocyanins were uniquely detected in P. zonale. P. graveolens stood out due to the various types of myricetin derivatives that were not detected in P. odoratissimum and P. zonale extracts. Evaluation of their biological activities revealed that P. zonale displayed superior antibacterial and antibiofilm activities in comparison to the other two species. The antibacterial efficacy of P. zonale was observed towards the clinically relevant strains of Staphylococcus aureus ATCC 25923, Methicillin-resistant Staphylococcus aureus (MRSA) 333, Enterococcus faecalis ATCC 29212, and the Vancomycin-resistant E. faecalis INSPI 032. Fractionation analysis of P. zonale suggested that the antibacterial activity attributed to this plant is due to the presence of quercetin derivatives and kaempferol and its derivatives, alongside their synergistic interaction with gallotannins and anthocyanins. Lastly, the three Pelargonium species exhibited notable antioxidant activity, which may be attributed to their high content of total phenolic compounds.
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  • 文章类型: Journal Article
    最近的证据报道,一些膳食化合物,如槲皮素和芹菜素,作为具有抗炎作用的最著名的类黄酮,可能会抑制SARS-CoV-2的主要蛋白酶。本文评估了槲皮素对COVID-19的有希望的作用和可能的作用机制的假设。
    使用以下搜索策略收集了关于槲皮素对COVID-19的抑制作用的相关论文:“电晕或冠状病毒或COVID或COVID-19或病毒或病毒”和“营养素或类黄酮或槲皮素”。
    研究结果表明,槲皮素由于其SARS-CoV-2主要蛋白酶和RNA依赖性RNA聚合酶抑制作用,可被认为是对抗COVID-19的有效药物。此外,槲皮素可能会减弱血管紧张素转换酶2(ACE-2)受体,导致SARS-CoV-2进入宿主细胞的能力降低。此外,抗病毒,抗炎,槲皮素的免疫调节活性已被频繁报道。
    槲皮素可能是治疗COVID-19并发症的有效药物。进一步的纵向人体研究是必要的。
    UNASSIGNED: Recent evidence reported that some dietary compounds like quercetin and apigenin as the most well-known flavonoids with anti-inflammatory effects may inhibit SARS-CoV-2 main protease. The hypothesis of the promising effects and possible mechanisms of action of quercetin against COVID-19 were assessed in this article.
    UNASSIGNED: Related papers on the inhibitory effects of quercetin against COVID-19 were collected using the following search strategy: \"corona or coronavirus or COVID or COVID-19 or viral or virus\" AND \"nutrient or flavonoid or Quercetin\".
    UNASSIGNED: The findings indicated that quercetin can be considered an effective agent against COVID-19 because of its SARS-CoV-2 main protease and RNA-dependent RNA polymerase inhibitory effects. In addition, quercetin may attenuate angiotensin-converting enzyme-2 (ACE-2) receptors leading to a reduction of SARS-CoV-2 ability to enter host cells. Moreover, the antiviral, anti-inflammatory, and immunomodulatory activities of quercetin have been frequently reported.
    UNASSIGNED: Quercetin may be an effective agent for managing the complications of COVID-19. Further longitudinal human studies are warranted.
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  • 文章类型: Journal Article
    背景:最近的证据表明,从槲寄生叶(DendrophthoepentandraL.Miq)的粗甲醇提取物中获得的一些类黄酮化合物,也被称为BenaluDuku(BD),具有抗菌作用。因此,该工厂有可能消除可能导致养鸡场爆发的病毒。本研究旨在证明黄酮类化合物的体外能力,即槲皮素类化合物(QLCs),为了消除现场病毒,特别是新城疫病毒(NDV)。方法:本研究分两个阶段进行。使用体外测试,并在0.05的显著性下设计对照组的后测试。BD叶(5公斤)用甲醇浸渍法提取,然后用己烷分离,氯仿,乙酸乙酯,和甲醇馏分。使用半制备型高效液相色谱(HPLC)分离最终的提取产物以获得QLC。使用HPLC鉴定QLCs并与槲皮素进行比较,质子和碳核磁共振波谱,傅里叶变换红外分光光度法,和超高效液相色谱-质谱联用。在10-5组织培养感染剂量50%(TCID50)的毒度滴度下和在鸡肾细胞培养物中,体外测试QLC对NDV的活性。结果:发现0.05%(w/v)QLCs的溶液对NDV具有抗病毒活性,在10-5稀释度下具有平均致细胞病变作用抗原性(p<0.05)。结论:来自BD叶子的黄酮类化合物的QLC具有针对NDV的抗病毒生物活性,并且可能具有被开发为用于治疗其他人类或动物病毒感染的药物化合物的潜力。
    Background: Recent evidence suggests that some flavonoid compounds obtained from crude methanol extract of mistletoe leaves ( Dendrophthoe pentandra L. Miq), also known as Benalu Duku (BD), have antimicrobial effects. Thus, the plant has the potential to eliminate viruses that may cause outbreaks in chicken farms. This study aimed to prove the in vitro ability of flavonoid compounds, namely quercetin-like compounds (QLCs), to eliminate field viruses, specifically the Newcastle disease virus (NDV). Methods: This research was performed in two stages. An in vitro test was used with a post-test of the control groups designed at a significance of 0.05. BD leaves (5 kg) were extracted using a maceration method with methanol and then separated into hexane, chloroform, ethyl acetate, and methanol fractions. The final extracted products were separated using semi-preparative high-performance liquid chromatography (HPLC) to obtain QLCs. The QLCs were identified and compared with quercetin using HPLC, proton and carbon nuclear magnetic resonance spectrometry, Fourier transform infrared spectrophotometry, and ultra-performance liquid chromatography-mass spectrometry. The activity of QLCs was tested in vitro against the NDV at a virulency titer of 10 -5 Tissue Culture Infectious Dose 50% (TCID50) and in chicken kidney cell culture. Results: Solutions of 0.05% (w/v) QLCs were discovered to have antiviral activity against NDVs, with an average cytopathogenic effect antigenicity at a 10 -5 dilution (p<0.05). Conclusions: QLCs from flavonoids from the leaves of BD have antiviral bioactivity against NDVs and may have the potential to be developed as medicinal compounds for the treatment of other human or animal viral infections.
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  • 文章类型: Journal Article
    结直肠癌是众所周知的癌症形式之一,并且是全世界癌症死亡的主要原因。动物研究加强了体外实验,以及人类大肠癌的流行病学研究表明,这种疾病的生长可以通过饮食方面来调节。饮食摄入包括绿色蔬菜和水果可能会减少结肠癌的机会。该发现表明,膳食营养素的组合可以提供附加或协同作用,并且可能是避免或根除结肠癌开始和/或发展的有效方法。黄酮醇是多酚类黄酮中最广泛的膳食营养素之一,也是葱和十字花科蔬菜的主要成分。葱科和十字花科蔬菜中存在的黄酮醇是山奈酚,杨梅素,槲皮素,和isorhametin.据称这些黄酮醇在体内和体外对结肠直肠癌具有抗增殖活性。这篇综述的目的是总结从饮食来源获得的黄酮醇在预防和治疗结直肠癌中的作用。
    Colorectal cancer is among the well-known forms of cancer and a prominent cause of cancer demises worldwide. In vitro experiments reinforced by animal studies, as well as epidemiological studies of human colorectal cancer propose that the growth of this disease can be moderated by eating aspects. Dietary intake including green vegetables and fruits may result in the reduction of colon cancer chances. The finding suggests that the combinations of dietary nutrients may deliver additive or synergistic effects and might be a powerful method to avoid or eradicate colon cancer beginning and/or development. Flavonols are one of the most widespread dietary nutrients of the polyphenols-flavonoids and major constituent of Allium and Brassicaceae vegetables. Flavonols present in vegetables of Allium and Brassicaceae family are kaempferol, myricetin, quercetin, and isorhamnetin. These flavonols are claimed to have antiproliferative activity in vivo and in vitro against colorectal cancer. The objective of this review is to summarize the role of flavonols obtained from dietary sources in the prevention and treatment of colorectal cancer.
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  • 文章类型: English Abstract
    本研究旨在系统地评估槲皮素(QCT)的保护作用,一种天然存在的类黄酮,抗过氧化氢(H2O2)诱导的人子宫内膜基质细胞(HESCs)氧化损伤。氧化应激,例如由H2O2诱导的,已知对细胞损伤有显著贡献,并且已经牵涉到各种生殖健康问题。该研究的重点是研究QCT如何与特定的分子途径相互作用以减轻这种损害。特别注意p38MAPK/NOX4信号通路,这对于调节细胞系统中的氧化应激反应至关重要。通过阐明这些机制,本研究试图证实QCT不仅是一种抗氧化应激的保护剂,而且是一种治疗药物,可用于治疗以子宫内膜细胞氧化应激增强为特征的疾病.
    用不同浓度(0、10、20和40μmol/L)的QCT处理HESCs体外培养24h,以验证QCT对正常子宫内膜细胞的无毒性作用。随后,用250μmol/LH2O2孵育细胞12h,建立H2O2诱导的HESCs损伤模型。HESCs用QCT预处理24h,然后用H2O2刺激。然后,进行CCK-8测定以检查细胞活力并筛选有效的干预浓度。HESCs分为3组,对照组,H2O2模型组,和H2O2+QCT组。使用DCFH-DA荧光测定法精确定量细胞内活性氧(ROS)的水平,一种以检测和定量细胞内氧化变化的准确性而闻名的方法。通过JC-1染色测定线粒体膜电位。采用膜联蛋白Ⅴ/PI双染色和流式细胞术检测QCT对H2O2诱导的HESCs凋亡的影响。此外,为了更深入地研究观察到的效应背后的细胞机制,进行蛋白质印迹分析以测量参与氧化应激反应的关键蛋白的表达水平。包括NADPH氧化酶4(NOX4),p38丝裂原活化蛋白激酶(p38MAPK),和磷酸化p38MAPK(p-p38MAPK)。这种分析有助于增加对QCT治疗所影响的特定细胞内信号通路的理解。特别注意其调节p38MAPK/NOX4通路的潜力,在抗氧化应激的细胞防御机制中起着重要作用。
    在这项研究中,我们从评估QCT对正常子宫内膜细胞的毒性开始.我们的发现表明,QCT在各种浓度(0,10,20和40μmol/L)没有表现出任何细胞毒性作用,为进一步研究其保护作用奠定了基础。在H2O2诱导的HESCs损伤模型中,观察到细胞活力显着降低,这与ROS的产生和由此产生的氧化损伤有关。然而,QCT(10μmol/L和20μmol/L)预处理后24h细胞活力显著提高(P<0.05),20μmol/L浓度显示出最显著的效果。这表明QCT可以有效逆转H2O2引起的细胞损伤。此外,细胞凋亡实验表明,与对照组相比,H2O2模型组的细胞凋亡率显着增加(P<0.01)。然而,联合QCT治疗显著逆转了这一趋势(P<0.05),表明QCT在减轻细胞凋亡方面具有潜在的保护作用。ROS检测表明,与对照组相比,H2O2模型组ROS平均荧光强度明显升高(P<0.01)。QCT治疗后H2O2+QCT组的ROS荧光强度明显低于H2O2模型组,提示氧化损伤的有效缓解(P<0.05)。线粒体膜电位变化的JC-1染色显示,与对照组相比,H2O2模型组线粒体膜电位下降的细胞比例明显增加(P<0.01)。然而,与H2O2模型组相比,QCT治疗组的这一比例显着降低(P<0.05)。最后,Westernblot分析显示,模型组大鼠的NOX4和p-p38MAPK蛋白表达水平较对照组升高(P<0.05)。QCT治疗后,与H2O2模型组相比,这些蛋白水平显着降低(P<0.05)。这些结果表明,QCT可能通过调节p38MAPK/NOX4信号通路发挥其对氧化应激的保护作用。
    QCT已证明对H2O2诱导的HESCs氧化损伤具有显著的保护作用。这种保护主要通过有效减少ROS积累和抑制参与氧化应激反应的关键信号通路来实现。尤其是p38MAPK/NOX4通路。这项研究的结果表明,QCT调节这些途径的能力在减轻与氧化应激条件相关的细胞损伤中起着关键作用。这不仅表明其作为抗细胞氧化应激的保护剂的潜力,但也强调了其在治疗以子宫内膜氧化应激增加为特征的疾病中的治疗应用潜力,从而提供了增强生殖健康的前景。未来的研究应探讨QCT的长期影响及其在体内的临床疗效,从而为其整合到治疗方案中提供了明确的途径。
    UNASSIGNED: This study aims to systematically evaluate the protective role of quercetin (QCT), a naturally occurring flavonoid, against oxidative damage in human endometrial stromal cells (HESCs) induced by hydrogen peroxide (H2O2). Oxidative stress, such as that induced by H2O2, is known to contribute significantly to cellular damage and has been implicated in various reproductive health issues. The study is focused on investigating how QCT interacts with specific molecular pathways to mitigate this damage. Special attention was given to the p38 MAPK/NOX4 signaling pathway, which is crucial to the regulation of oxidative stress responses in cellular systems. By elucidating these mechanisms, the study seeks to confirm the potential of QCT not only as a protective agent against oxidative stress but also as a therapeutic agent that could be integrated in treatments of conditions characterized by heightened oxidative stress in endometrial cells.
    UNASSIGNED: I n vitro cultures of HESCs were treated with QCT at different concentrations (0, 10, 20, and 40 μmol/L) for 24 h to verify the non-toxic effects of QCT on normal endometrial cells. Subsequently, 250 μmol/L H2O2 was used to incubate the cells for 12 h to establish an H2O2-induced HESCs injury model. HESCs were pretreated with QCT for 24 h, which was followed by stimulation with H2O2. Then, CCK-8 assay was performed to examine the cell viability and to screen for the effective intervention concentration. HESCs were divided into 3 groups, the control group, the H2O2 model group, and the H2O2+QCT group. Intracellular levels of reactive oxygen species (ROS) were precisely quantified using the DCFH-DA fluorescence assay, a method known for its accuracy in detecting and quantifying oxidative changes within the cell. The mitochondrial membrane potential was determined by JC-1 staining. Annexin Ⅴ/PI double staining and flow cytometry were performed to determine the effect of QCT on H2O2-induced apoptosis of HESCs. Furthermore, to delve deeper into the cellular mechanisms underlying the observed effects, Western blot analysis was conducted to measure the expression levels of the critical proteins involved in oxidative stress response, including NADPH oxidase 4 (NOX4), p38 mitogen-activated protein kinase (p38 MAPK), and phosphorylated p38 MAPK (p-p38 MAPK). This analysis helps increase understanding of the specific intracellular signaling pathways affected by QCT treatment, giving special attention to its potential for modulation of the p38 MAPK/NOX4 pathway, which plays a significant role in cellular defense mechanisms against oxidative stress.
    UNASSIGNED: In this study, we started off by assessing the toxicity of QCT on normal endometrial cells. Our findings revealed that QCT at various concentrations (0, 10, 20, and 40 μmol/L) did not exhibit any cytotoxic effects, which laid the foundation for further investigation into its protective roles. In the H2O2-induced HESCs injury model, a significant reduction in cell viability was observed, which was linked to the generation of ROS and the resultant oxidative damage. However, pretreatment with QCT (10 μmol/L and 20 μmol/L) significantly enhanced cell viability after 24 h (P<0.05), with the 20 μmol/L concentration showing the most substantial effect. This suggests that QCT can effectively reverse the cellular damage caused by H2O2. Furthermore, the apoptosis assays demonstrated a significant increase in the apoptosis rates in the H2O2 model group compared to those in the control group (P<0.01). However, co-treatment with QCT significantly reversed this trend (P<0.05), indicating QCT\'s potential protective role in mitigating cell apoptosis. ROS assays showed that, compared to that in the control group, the average fluorescence intensity of ROS in the H2O2 model group significantly increased (P<0.01). QCT treatment significantly reduced the ROS fluorescence intensity in the H2O2+QCT group compared to the that in the H2O2 model group, suggesting an effective alleviation of oxidative damage (P<0.05). JC-1 staining for mitochondrial membrane potential changes revealed that compared to that in the control, the proportion of cells with decreased mitochondrial membrane potential significantly increased in the H2O2 model group (P<0.01). However, this proportion was significantly reduced in the QCT-treated group compared to that of the H2O2 model group (P<0.05). Finally, Western blot analysis indicated that the expression levels of NOX4 and p-p38 MAPK proteins were elevated in the H2O2 model group compared to those of the control group (P<0.05). Following QCT treatment, these protein levels significantly decreased compared to those of the H2O2 model group (P<0.05). These results suggest that QCT may exert its protective effects against oxidative stress by modulating the p38 MAPK/NOX4 signaling pathway.
    UNASSIGNED: QCT has demonstrated significant protective effects against H2O2-induced oxidative damage in HESCs. This protection is primarily achieved through the effective reduction of ROS accumulation and the inhibition of critical signaling pathways involved in the oxidative stress response, notably the p38 MAPK/NOX4 pathway. The results of this study reveal that QCT\'s ability to modulate these pathways plays a key role in alleviating cellular damage associated with oxidative stress conditions. This indicates not only its potential as a protective agent against cellular oxidative stress, but also highlights its potential for therapeutic applications in treating conditions characterized by increased oxidative stress in the endometrium, thereby offering the prospect of enhancing reproductive health. Future studies should explore the long-term effects of QCT and its clinical efficacy in vivo, thereby providing a clear path toward its integration into therapeutic protocols.
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  • 文章类型: Journal Article
    背景:槲寄生是一种生长在杜库植物(Lanciumdemosticum)上的草本植物,在印度尼西亚被称为benaluduku(BD)。预计它具有抗癌或抗病毒特性等益处,它也被认为具有抗糖尿病的药理活性。槲皮素类化合物(QLC)是具有抗糖尿病活性的次级代谢产物,其预期在口服给药后降低动物的血糖水平。
    目的:本研究旨在使用实验动物作为临床模型分析QLC降低随机血糖水平的能力。
    材料和方法:使用的研究方法是探索性的,使用了前后测试模型,并观察治疗后的随机血糖水平。从BD叶中提取次生代谢产物,然后进行筛选。通过每天以0.045mg/g体重施用链脲佐菌素2天,在30只大鼠(褐家鼠)中诱发了糖尿病。在糖尿病大鼠中测试了剂量为0.5mg/kg体重(每天两次)的次生代谢物的抗糖尿病作用。使用OneTouchUltraPlus医疗设备测量随机糖水平(mg/dL),以观察随机血糖水平。结果和新颖性:结果表明,次级代谢产物,作为BD叶提取物的分析物,能显著降低随机血糖水平。
    结论:从BD中提取的次生代谢产物,可用于治疗大鼠糖尿病。
    Background: Mistletoe is an herb that grows on duku plants (Lancium demosticum) and is known as benalu duku (BD) in Indonesia. It is predicted to have benefits such as anticancer or antiviral properties, and it is also thought to have anti-diabetic pharmacological activity. Quercetin-like compounds (QLCs) are secondary metabolites with antidiabetic activity that are expected to lower blood sugar levels in animals after oral administration.
    Objective: This study aimed to analyze the ability of QLCs to reduce random blood sugar levels using experimental animals as clinical models.
    Material and methods: The research method used was exploratory, which used a before-after test model, and observations were made on the random blood sugar levels after treatment. Secondary metabolites were extracted from BD leaves, which were then screened. Diabetes was induced in 30 rats (Rattus norvegicus) by the administration of streptozotocin at 0.045 mg/g body weight daily for 2 days. The antidiabetic effects of the secondary metabolite at doses of 0.5 mg/kg body weight (twice a day) when administered orally for up to 5 days were tested in diabetic rats. The random sugar levels (mg/dL) were measured using a One Touch Ultra Plus medical device for observation of randomized blood sugar levels. Results and novelty: The results revealed that the secondary metabolite, as an analyte from the BD leaf extract, can significantly reduce random blood sugar levels.
    Conclusion: The secondary metabolite extracted from BD, could be used to treat diabetes in rats.
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  • 文章类型: Journal Article
    槲皮素是一种黄酮类化合物,具有显着的药理作用和有前途的治疗潜力。槲皮素在神经炎症中起重要作用,这有助于降低阿尔茨海默病(AD)的严重程度。槲皮素(Q)和槲皮素3-O-葡糖苷酸(Q3OG)是一些从天然来源获得的最有效的抗氧化剂。然而,当与肠道微生物反应时,槲皮素的天然形式转化为Q3OG。该研究旨在确保Q和Q3OG的治疗潜力。在这项研究中,首先使用SwissTargetPrediction平台鉴定Q和Q3OG的潜在分子靶标,并使用DisGeNET数据库鉴定AD的致病靶标。其次是化合物和疾病靶点重叠,77个靶点被置于AKT1、EGFR、MMP9,TNF,PTGS2,MMP2,IGF1R,MCL1、MET和PARP1是排名第一的目标,这是CytoHubba插件估计的。针对Q和Q3OG朝向PDB:1UNQ靶标进行分子对接。Q和Q3OG的结合评分分别为-6.2kcal/mol和-6.58kcal/mol。在200ns下对Q和Q3OG朝向PDB:1UNQ目标进行分子动力学模拟。这项研究的结果有助于确定生物活性化合物的多个靶位点。因此,通过结构修饰合成基于化学实体的槲皮素可能有助于根除AD并发症.
    Quercetin is a flavonoid with notable pharmacological effects and promising therapeutic potential. Quercetin plays a significant role in neuroinflammation, which helps reduce Alzheimer\'s disease (AD) severity. Quercetin (Q) and quercetin 3-O-glucuronide (Q3OG) are some of the most potent antioxidants available from natural sources. However, the natural form of quercetin converted into Q3OG when reacted with intestinal microbes. The study aims to ensure the therapeutic potential of Q and Q3OG. In this study, potential molecular targets of Q and Q3OG were first identified using the Swiss Target Prediction platform and pathogenic targets of AD were identified using the DisGeNET database. Followed by compound and disease target overlapping, 77 targets were placed in that AKT1, EGFR, MMP9, TNF, PTGS2, MMP2, IGF1R, MCL1, MET and PARP1 was the top-ranked target, which was estimated by CytoHubba plug-in. The Molecular docking was performed for Q and Q3OG towards the PDB:1UNQ target. The binding score of Q and Q3OG was - 6.2 kcal/mol and - 6.58 kcal/mol respectively. Molecular dynamics simulation was conducted for Q and Q3OG towards the PDB:1UNQ target at 200 ns. This study\'s results help identify the multiple target sites for the bioactive compounds. Thus, synthesizing new chemical entity-based quercetin on structural modification may aid in eradicating AD complications.
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