flavonoid

类黄酮
  • 文章类型: Editorial
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  • 文章类型: Journal Article
    KuwanonC是桑树家族中发现的一种独特的类黄酮,特征为两个异戊烯基。虽然以前的研究集中在kuwanonC的各种性质上,如抗氧化剂,低血糖,抗菌,食品保存,皮肤美白,和线虫寿命延长,很少有人关注它在肿瘤疾病中的潜在作用。在这项研究中,我们研究了kuwanonC在宫颈癌细胞中的抗肿瘤作用,并阐明了其具体作用机制。我们使用各种实验技术评估了kuwanonC的抗肿瘤作用,包括细胞增殖试验,伤口愈合试验,EdU488增殖试验,线粒体膜电位测定,ROS水平测定,细胞周期,细胞凋亡分析,以及KuwanonC靶位点和分子对接的研究。结果表明,kuwanonC显著影响HeLa细胞的细胞周期进程,破坏了它们的线粒体膜电位,并诱导细胞内ROS水平的大幅增加。此外,kuwanonC对HeLa细胞表现出明显的抗增殖和促凋亡作用,超越了紫杉醇、顺铂等常用抗肿瘤药物的性能。值得注意的是,与紫杉醇相比,kuwanonC表现出优异的疗效,同时也更容易获得。我们的研究表明,kuwanonC通过与线粒体和内质网膜的相互作用发挥强大的抗肿瘤作用,诱导大量产生ROS,破坏了它们的正常结构,抑制细胞周期进程,并刺激凋亡信号通路,最终导致HeLa肿瘤细胞死亡。作为源自桑属的异戊烯基化合物,kuwanonC有望成为开发有效抗肿瘤药物的潜在候选人。
    Kuwanon C is a unique flavonoid found in the mulberry family, characterized by two isopentenyl groups. While previous research has focused on various properties of kuwanon C, such as antioxidant, hypoglycemic, antimicrobial, food preservation, skin whitening, and nematode lifespan extension, little attention has been given to its potential role in oncological diseases. In this study, we investigate the antitumor effect of kuwanon C in cervical cancer cells and elucidate its specific mechanism of action. We assessed the antitumor effects of kuwanon C using various experimental techniques, including cell proliferation assay, wound healing assays, EdU 488 proliferation assay, mitochondrial membrane potential assay, ROS level assay, cell cycle, apoptosis analysis, and studies on kuwanon C target sites and molecular docking. The results revealed that kuwanon C significantly impacted the cell cycle progression of HeLa cells, disrupted their mitochondrial membrane potential, and induced a substantial increase in intracellular ROS levels. Moreover, kuwanon C exhibited notable anti-proliferative and pro-apoptotic effects on HeLa cells, surpassing the performance of commonly used antitumor drugs such as paclitaxel and cisplatin. Notably, kuwanon C demonstrated superior efficacy while also being more easily accessible compared to paclitaxel. Our study demonstrates that kuwanon C exerts potent antitumor effects by its interaction with the mitochondrial and endoplasmic reticulum membranes, induces a significant production of ROS, disrupts their normal structure, inhibits cell cycle progression, and stimulates apoptotic signaling pathways, ultimately resulting in the death of HeLa tumor cells. As an isopentenyl compound derived from Morus alba, kuwanon C holds great promise as a potential candidate for the development of effective antitumor drugs.
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  • 文章类型: Journal Article
    膀胱过度活动症(OAB)对个体的身体和心理健康的影响逐年增加,如急迫性尿失禁和夜尿症所证明。OAB患者的症状可能受炎症和氧化应激的影响。黄酮类化合物被认为是重要的抗炎和抗氧化剂,这在水果中很常见,茶,蔬菜,等。以前的研究已经证明了黄酮类化合物及其亚类在治疗炎症方面的治疗潜力,和氧化应激。尽管如此,目前仍缺乏探索类黄酮消费之间潜在相关性的研究,特别是在不同的子类中,OAB。因此,本研究旨在调查黄酮类化合物摄入与OAB之间的关系,以确定OAB管理中可能的饮食干预措施.
    我们利用了国家健康与营养调查(NHANES)和美国农业部饮食研究食品和营养数据库(FNDDS)的调查数据,以13063名合格的美国成年人为基础,研究了总黄酮和亚类黄酮的饮食摄入量与OAB风险之间的关系。从两次24小时的饮食回顾中估算了饮食中类黄酮的摄入量。加权多元逻辑回归模型,基于分位数的g计算,受限三次样条模型,并采用分层分析探讨黄酮类化合物摄入量与OAB的关系,分别。
    被诊断为OAB的参与者表现出更高的女性比例,年长的,非西班牙裔黑人,未婚,以前的饮酒者,家庭年收入较低,较低的贫困收入比,受教育程度较低,肥胖和吸烟者的可能性更高。在调整混杂因素后,加权logistic回归模型显示,花青素消费的第三个四分位数和黄酮消费的第二个四分位数与OAB的降低几率显着相关,而总黄酮消费量与OAB的风险没有显着相关性。基于分位数的g计算模型表明,黄酮,花青素和黄酮醇是观察到的负相关的主要因素。此外,限制性三次样条模型表明花青素摄入量与OAB风险之间存在J形非线性暴露-反应相关性(P非线性=0.00164).分层和交互作用分析显示,花青素摄入量与OAB风险之间的关系受年龄(P交互作用=0.01)和受教育程度(P交互作用=0.01)的显着影响。同时发现黄酮摄入量与OAB风险之间的关系因种族(P交互作用=0.02)和体育锻炼持续时间(P交互作用=0.05)而异。
    我们的研究表明,食用富含类黄酮亚类花青素和黄酮的饮食与OAB的风险降低有关,可能在预防OAB发展中提供临床意义。这强调了饮食调整在OAB症状管理中的重要性。
    UNASSIGNED: The increasing influence of overactive bladder (OAB) on physical as well as mental health of individuals is becoming more pronounced annually, as evidenced by the urge urinary incontinence and nocturia. Symptoms in OAB patients may be influenced by inflammation and oxidative stress. Flavonoids are recognized as significant anti-inflammatory and antioxidant agents, which are commonly available in fruits, tea, vegetables, etc. Previous research has demonstrated the therapeutic potential of flavonoids and their subclasses in treating inflammation, and oxidative stress. Despite this, there remains a paucity of research exploring the potential correlation between flavonoid consumption, specifically within distinct subclasses, and OAB. Thus, our study aims to investigate the relationship between flavonoid intake and OAB to identify possible dietary interventions for OAB management.
    UNASSIGNED: We utilized the survey data from the National Health and Nutrition Examination Survey (NHANES) and the USDA Food and Nutrient Database for Dietary Studies (FNDDS) to investigate the relationship between dietary intake of total and subclass flavonoids and the risk of OAB based on 13,063 qualified American adults. The dietary flavonoid intake was estimated from two 24-h dietary recalls. Weighted multivariate logistic regression model, quantile-based g-computation, restricted cubic spline model, and stratified analysis were used to explore the association between flavonoid intake and OAB, respectively.
    UNASSIGNED: The participants diagnosed with OAB exhibited a higher percentage of being female, older, Non-Hispanic Black, unmarried, former drinkers, having a lower annual household income, lower poverty to income ratio, lower educational attainment, and a higher likelihood of being obese and smokers. Upon adjusting for confounding factors, the weighted logistic regression models revealed that the third quartile of consumption of anthocyanidin and the second quartile of consumption of flavone were significantly associated with the reduced odds of OAB, while total flavonoid consumption did not show a significant correlation with the risk of OAB. The quantile-based g-computation model indicated that flavone, anthocyanidin and flavonol were the primary contributors to the observed negative correlation. Furthermore, the restricted cubic spline models demonstrated a J-shaped non-linear exposure-response association between anthocyanidin intake and the risk of OAB (P nonlinear = 0.00164). The stratified and interaction analyses revealed that the relationship between anthocyanidin intake and the risk of OAB was significantly influenced by age (P interaction = 0.01) and education level (P interaction = 0.01), while the relationship between flavone intake and the risk of OAB was found to vary by race (P interaction = 0.02) and duration of physical activity (P interaction = 0.05).
    UNASSIGNED: Our research suggests that consuming a diet rich in flavonoid subclass anthocyanidin and flavone is associated with a reduced risk of OAB, potentially offering clinical significance in the prevention of OAB development. This underscores the importance of dietary adjustments in the management of OAB symptoms.
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  • 文章类型: Editorial
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  • 文章类型: Journal Article
    微生物基因组仍然是发现各种天然产物的巨大宝库。红霉素的工业生产商赤孢菌NRRL23338,有十几个生物合成基因簇,其编码产物尚未鉴定。白链霉菌B4底盘中聚酮化合物簇pks7之一的异源表达导致其功能的表征,该功能负责合成6-甲基水杨酸和6-乙基水杨酸。同时,分离出两种新的6-乙基水杨酸酯衍生物作为分流代谢物。通过MS和NMR实验的综合分析鉴定了它们的结构。还讨论了pks7BGC内基因的推定功能。
    The microbial genome remains a huge treasure trove for the discovery of diverse natural products. Saccharopolyspora erythraea NRRL23338, the industry producer of erythromycin, has a dozen of biosynthetic gene clusters whose encoding products are unidentified. Heterologous expression of one of the polyketide clusters pks7 in Streptomyces albus B4 chassis resulted in the characterization of its function responsible for synthesizing both 6-methylsalicyclic acid and 6-ethylsalicyclic acid. Meanwhile, two new 6-ethylsalicyclic acid ester derivatives were isolated as shunt metabolites. Their structures were identified by comprehensive analysis of MS and NMR experiments. Putative functions of genes within the pks7 BGC were also discussed.
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  • 文章类型: Journal Article
    胃癌(GC)是一种常见的胃肠道肿瘤,其特征是高死亡率和复发率。目前的治疗方法往往有局限性,促使研究人员探索新的抗肿瘤物质和开发新的药物。黄酮类化合物,具有多种生物活性的天然化合物,在这方面越来越受到关注。我们从PubMed搜索,WebofScience,SpringerLink和其他数据库查找近二十年来的相关文献。使用“胃癌”,“胃癌”,\"类黄酮\",\"生物类黄酮\",“2-苯基-铬烯”作为关键词,被搜查,并对黄酮类化合物处理GC的机理进行了分析和总结。揭示了黄酮类化合物的抗肿瘤机制涉及抑制肿瘤生长,扩散,入侵,和转移,以及通过各种过程如细胞凋亡诱导细胞死亡,自噬,铁性凋亡,和焦亡。此外,黄酮类化合物与其他化疗药物如5-FU和铂化合物的结合可以潜在地降低化学耐药性。当与其他天然产物组合使用时,类黄酮还表现出增强的生物活性。因此,这篇综述提出了开发黄酮类化合物作为新型抗GC药物的创新观点。
    Gastric cancer (GC) is a prevalent gastrointestinal tumor characterized by high mortality and recurrence rates. Current treatments often have limitations, prompting researchers to explore novel anti-tumor substances and develop new drugs. Flavonoids, natural compounds with diverse biological activities, are gaining increasing attention in this regard. We searched from PubMed, Web of Science, SpringerLink and other databases to find the relevant literature in the last two decades. Using \"gastric cancer\", \"stomach cancers\", \"flavonoid\", \"bioflavonoid\", \"2-Phenyl-Chromene\" as keywords, were searched, then analyzed and summarized the mechanism of flavonoids in the treatment of GC. It was revealed that the anti-tumor mechanism of flavonoids involves inhibiting tumor growth, proliferation, invasion, and metastasis, as well as inducing cell death through various processes such as apoptosis, autophagy, ferroptosis, and pyroptosis. Additionally, combining flavonoids with other chemotherapeutic agents like 5-FU and platinum compounds can potentially reduce chemoresistance. Flavonoids have also demonstrated enhanced biological activity when used in combination with other natural products. Consequently, this review proposes innovative perspectives for the development of flavonoids as new anti-GC agents.
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  • 文章类型: Journal Article
    抗肿瘤药物的开发显著提高了恶性肿瘤患者的生存率和生活质量。然而,这些药物的副作用,尤其是心脏毒性,严重限制了其临床应用。与抗肿瘤药物相关的心脏毒性一直是人们广泛关注和研究的课题。传统的减轻这些副作用包括减少药物剂量,缩短治疗时间,修改管理方法,选择毒性较低的药物。然而,任何一种方法都可能损害药物的抗肿瘤功效。因此,探索其他有效的抗心脏毒性方法将是未来研究的重点。中医药在管理心血管疾病和癌症治疗方面的潜力已获得广泛认可。中药因其副作用最小而受到重视,负担能力,和可访问性,为预防和治疗由抗肿瘤药物引起的心脏毒性提供了有希望的途径。在它的组成部分中,黄酮类化合物,存在于许多TCM中,尤其值得注意。这些具有不同结构组分的单体化合物已被证明具有心血管保护特性和抗肿瘤能力。在这次讨论中,我们将深入研究抗肿瘤药物的分类,并探讨其相关心脏毒性的潜在机制。此外,我们将研究中药中发现的黄酮类化合物,并研究其心血管保护机制。这将包括分析这些天然化合物如何减轻抗肿瘤疗法的心脏副作用,同时潜在地增强患者的整体健康和治疗结果。
    The development of anti-tumor drugs has notably enhanced the survival rates and quality of life for patients with malignant tumors. However, the side effects of these drugs, especially cardiotoxicity, significantly limit their clinical application. The cardiotoxicity associated with anti-tumor drugs has been a subject of extensive attention and research. Traditional to mitigate these side effects have included reducing drug dosages, shortening treatment duration, modifying administration methods, and opting for drugs with lower toxicity. However, either approach may potentially compromise the anti-tumor efficacy of the medications. Therefore, exploring other effective methods for anti-cardiotoxicity will be the focus of future research. The potential of traditional Chinese medicine (TCM) in managing cardiovascular diseases and cancer treatment has gained widespread recognition. TCM is valued for its minimal side effects, affordability, and accessibility, offering promising avenues in the prevention and treatment of cardiotoxicity caused by anti-tumor drugs. Among its constituents, flavonoids, which are present in many TCMs, are particularly notable. These monomeric compounds with distinct structural components have been shown to possess both cardiovascular protective properties and anti-tumor capabilities. In this discussion, we will delve into the classification of anti-tumor drugs and explore the underlying mechanisms of their associated cardiotoxicity. Additionally, we will examine flavonoids found in TCM and investigate their mechanisms of cardiovascular protection. This will include an analysis of how these natural compounds can mitigate the cardiac side effects of anti-tumor therapies while potentially enhancing overall patient health and treatment outcomes.
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  • 文章类型: Journal Article
    肠道菌群与认知健康之间的关系是复杂和双向的,受到我们饮食的显著影响。有证据表明,多酚和菊粉可以通过各种机制影响认知功能,其中之一是肠道微生物群。在这项研究中,在体外和体内研究了野生蓝莓处理(WBB)和富含菊苣菊粉的效果。肠道菌群组成和代谢产物,包括神经递质,在肠道模型系统中对WBB和菊粉的粪便微生物发酵进行了评估。其次,在一项小型试点(n=13)试验中,对儿童的微生物群变化和认知功能进行了评估,比较了WBB,菊粉,和麦芽糊精安慰剂,通过一系列测量执行功能和记忆功能的测试,在基线时进行粪便采样,干预后4周和4周洗脱期后。WBB和菊粉均导致微生物变化和体外短链脂肪酸水平增加。与安慰剂相比,服用菊粉和WBB后观察到体内执行功能和记忆的显着改善。在菊粉组中,认知益处伴随着普氏粪杆菌的显着增加,而在WBB组,拟杆菌显著增加,厚壁菌则显著减少(p<0.05)。因此,WBB和菊粉都影响微生物群,并可能通过不同的肠道相关或其他机制影响认知功能。这项研究强调了饮食对认知功能的重要影响,在某种程度上,由肠道微生物群介导。
    The relationship between the gut microbiota and cognitive health is complex and bidirectional, being significantly impacted by our diet. Evidence indicates that polyphenols and inulin can impact cognitive function via various mechanisms, one of which is the gut microbiota. In this study, effects of a wild blueberry treatment (WBB) and enriched chicory inulin powder were investigated both in vitro and in vivo. Gut microbiota composition and metabolites, including neurotransmitters, were assessed upon faecal microbial fermentation of WBB and inulin in a gut model system. Secondly, microbiota changes and cognitive function were assessed in children within a small pilot (n = 13) trial comparing WBB, inulin, and a maltodextrin placebo, via a series of tests measuring executive function and memory function, with faecal sampling at baseline, 4 weeks post-intervention and after a 4 week washout period. Both WBB and inulin led to microbial changes and increases in levels of short chain fatty acids in vitro. In vivo significant improvements in executive function and memory were observed following inulin and WBB consumption as compared to placebo. Cognitive benefits were accompanied by significant increases in Faecalibacterium prausnitzii in the inulin group, while in the WBB group, Bacteroidetes significantly increased and Firmicutes significantly decreased (p < 0.05). As such, WBB and inulin both impact the microbiota and may impact cognitive function via different gut-related or other mechanisms. This study highlights the important influence of diet on cognitive function that could, in part, be mediated by the gut microbiota.
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  • 文章类型: Journal Article
    Ajowan(TrachyspermumammiL.)被认为是一种有价值的香料和药草。在这项研究中,在不同的干燥处理下,研究了阿高地上部分的精油含量和组成(太阳,shade,烤箱在45°C,烤箱在65°C,微波炉,和冷冻干燥)。此外,酚类物质含量,类黄酮含量,并对样品的抗氧化能力进行了评估。新鲜样品产生的精油含量最高(1.05%),其次是那些在阳光下(0.7%)和遮阳干燥(0.95%)。基于气相色谱-质谱(GC-MS),确定了30种化合物,其中百里酚(34.84-83.1%),香芹酚(0.15-32.36%),对异丙基苯(0.09-13.66%),γ-萜品烯(3.12-22.58%)含量最高。在干燥方法中,冷冻干燥显示百里酚含量最高,然后在45°C烘箱中干燥。在新鲜样品(38.23mgTAEg-1干重(DW))和在45°C烘箱干燥的样品(7.3mgQEg-1DW)中获得了最高的TPC(总酚含量)和TFC(总黄酮含量),分别。根据HPLC结果,咖啡酸(18.04-21.32毫克/100克DW)和阿魏酸(13.102-19.436毫克/100克DW)是最丰富的酚酸,而在类黄酮中,芦丁含量最高(10.26-19.88mg/100gDW)。总的来说,冷冻干燥是保存酚类(TPC)和类黄酮(TFC)化合物和油成分的最有前途的干燥方法。
    Ajowan (Trachyspermum ammi L.) is considered a valuable spice and medicinal herb. In this study, the essential oil content and composition of the aerial parts of ajowan were investigated under different drying treatments (sun, shade, oven at 45 °C, oven at 65 °C, microwave, and freeze drying). Moreover, the phenolic content, flavonoid content, and antioxidant capacity of samples were also assessed. Fresh samples produced the highest essential oil content (1.05%), followed by those treated under sun (0.7%) and shade drying (0.95%). Based on gas chromatography-mass spectrometry (GC-MS), thirty compounds were determined in which thymol (34.84-83.1%), carvacrol (0.15-32.36%), p-cymene (0.09-13.66%), and γ-terpinene (3.12-22.58%) were the most abundant. Among the drying methods, freeze drying revealed the highest thymol content, followed by drying in a 45 °C oven. The highest TPC (total phenolic content) and TFC (total flavonoid content) were obtained in the fresh sample (38.23 mg TAE g-1 dry weight (DW)) and in the sample oven-dried at 45 °C (7.3 mg QE g-1 DW), respectively. Based on the HPLC results, caffeic acid (18.04-21.32 mg/100 gDW) and ferulic acid (13.102-19.436 mg/100 g DW) were the most abundant phenolic acids, while among flavonoids, rutin constituted the highest amount (10.26-19.88 mg/100 gDW). Overall, freeze drying was the most promising method of drying for preserving the phenolic (TPC) and flavonoid (TFC) compounds and oil components.
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  • 文章类型: Journal Article
    有机阴离子转运蛋白OAT1(SLC22A6)和OAT3(SLC22A8)是在肾脏中表达的药物转运蛋白,在药物和内源性代谢物的体内运输中具有公认的作用。这些药物转运蛋白的相对未开发的潜在功能是它们对天然产物(NP)的体内调节及其对内源性代谢的影响的贡献。这对于评估在转运蛋白位点处与其他化合物的潜在NP相互作用是重要的。这里,我们分析了亚洲几个完善的数据库中存在的NP(中国,印度阿育吠陀)和其他传统。小鼠敲除中OAT1和OAT3的丢失导致许多NP的血清改变,包括类黄酮,维生素,还有吲哚.基于化学性质的多变量分析,OAT1-和OAT3依赖性NP在很大程度上是可分离的。使用体外转运测定和蛋白质结合测定确认与转运蛋白的直接结合。我们的体内和体外结果,在以前的数据的背景下考虑,证明OAT1和OAT3在处理非合成小分子天然产物中起着关键作用,NP衍生的抗氧化剂,植物化学物质,和营养素(例如,泛酸,硫胺素)。正如遥感和信号理论所描述的,药物转运蛋白通过调节内源性抗氧化剂和营养物质在器官和生物体之间的运动来帮助调节氧化还原状态。我们的结果表明,膳食抗氧化剂和其他NPs可能会进入这些器官间和生物体间途径。
    The organic anion transporters OAT1 (SLC22A6) and OAT3 (SLC22A8) are drug transporters that are expressed in the kidney, with well-established roles in the in vivo transport of drugs and endogenous metabolites. A comparatively unexplored potential function of these drug transporters is their contribution to the in vivo regulation of natural products (NPs) and their effects on endogenous metabolism. This is important for the evaluation of potential NP interactions with other compounds at the transporter site. Here, we have analyzed the NPs present in several well-established databases from Asian (Chinese, Indian Ayurvedic) and other traditions. Loss of OAT1 and OAT3 in murine knockouts caused serum alterations of many NPs, including flavonoids, vitamins, and indoles. OAT1- and OAT3-dependent NPs were largely separable based on a multivariate analysis of chemical properties. Direct binding to the transporter was confirmed using in vitro transport assays and protein binding assays. Our in vivo and in vitro results, considered in the context of previous data, demonstrate that OAT1 and OAT3 play a pivotal role in the handling of non-synthetic small molecule natural products, NP-derived antioxidants, phytochemicals, and nutrients (e.g., pantothenic acid, thiamine). As described by remote sensing and signaling theory, drug transporters help regulate redox states by meditating the movement of endogenous antioxidants and nutrients between organs and organisms. Our results demonstrate how dietary antioxidants and other NPs might feed into these inter-organ and inter-organismal pathways.
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