plant compounds

植物化合物
  • 文章类型: Journal Article
    酵母是果汁和其他饮料中常见的污染物,负责降低此类产品的质量和保质期。防腐剂主要添加到这些饮料中以提高它们的保质期。随着消费者对化学食品添加剂的日益关注,植物来源的抗微生物剂作为高效、安全的抗酵母剂已经引起了研究者的注意。然而,目前用于确定其抗酵母活性的方法是耗时和耗时的。在这项研究中,使用微量滴定板评估了苹果汁和橙汁食品模型中植物酚类化合物的抗酵母作用,以验证用于筛选果汁防腐剂抗菌活性的改良肉汤微量稀释方法。在测试的12种化合物中,四个对所有测试的酵母(酿酒酵母,贝里酵母菌,橙汁和苹果汁中的rouxii酵母)。在两种最低抑制浓度(MIC)为32至128μg/mL的果汁中,蝶芪均获得最佳结果。其他化合物,即氧白藜芦醇,piceatannol,和阿魏酸,表现出中等抑制作用,MIC为256-512μg/mL。此外,结果表明,测试化合物的化学结构差异显着影响酵母抑制水平,而具有甲氧基和羟基的二苯乙烯产生的作用最强。此外,本研究中开发的创新测定法可用于筛选果汁防腐剂的抗酵母活性,因为它节省了准备和分析时间,实验室用品,和人力比较常用的方法。
    Yeasts are the usual contaminants in fruit juices and other beverages, responsible for the decrease in the quality and shelf-life of such products. Preservatives are principally added to these beverages to enhance their shelf-life. With the increasing consumer concern towards chemical food additives, plant-derived antimicrobials have attracted the attention of researchers as efficient and safer anti-yeast agents. However, the methods currently used for determining their anti-yeast activity are time- and material-consuming. In this study, the anti-yeast effect of plant phenolic compounds in apple and orange juice food models using microtiter plates has been evaluated in order to validate the modified broth microdilution method for screening the antimicrobial activity of juice preservative agents. Among the twelve compounds tested, four showed a significant in vitro growth-inhibitory effect against all tested yeasts (Saccharomyces cerevisiae, Zygosaccharomyces bailii, and Zygosaccharomyces rouxii) in both orange and apple juices. The best results were obtained for pterostilbene in both juices with minimum inhibitory concentrations (MICs) ranging from 32 to 128 μg/mL. Other compounds, namely oxyresveratrol, piceatannol, and ferulic acid, exhibited moderate inhibitory effects with MICs of 256-512 μg/mL. Furthermore, the results indicated that differences in the chemical structures of the compounds tested significantly affected the level of yeast inhibition, whereas stilbenes with methoxy and hydroxy groups produced the strongest effect. Furthermore, the innovative assay developed in this study can be used for screening the anti-yeast activity of juice preservative agents because it saves preparatory and analysis time, laboratory supplies, and manpower in comparison to the methods commonly used.
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  • 文章类型: Journal Article
    尽管是几十年研究的焦点,女性乳腺癌(BC)仍然是世界上最致命的癌症之一。鉴于所有确诊的BC病例中有80%是雌激素受体阳性(ER),其致癌作用由雌激素-ERα信号驱动,目前的标准护理(SOC)激素疗法旨在调节雌激素及其受体的功能和表达水平,ERα和ERβ。目前,芳香化酶抑制剂(AI),选择性ER调节剂(SERM)和选择性ER降解剂(SERD)在临床上被规定用于ER+BC的管理和治疗,随着AIs的抗芳香化酶活性消除雌激素的生物合成,而抗雌激素SERM和SERD拮抗和降解ER,分别。使用SOC激素疗法是,然而,严重副作用的发作和耐药性的发展显着阻碍。鉴于许多研究已经报道了植物化合物和/或提取物的有益作用以及它们靶向ER+乳腺癌发生的多种途径,最近的研究集中在使用饮食化学预防剂进行BC管理。当与SOC治疗相结合时,这些植物组分和/或提取物中的几种已经显示出改善的功效和/或协同影响。此外,尽管缺乏体内研究,据报道,植物产品的副作用通常低于SOC疗法,因此被认为是更安全的治疗选择.因此,本综述总结了过去五年关于植物产品抗芳香化酶和抗雌激素活性的发现,以及它们与SOC疗法组合的协同抗ER+BC效应。
    Despite being the focal point of decades of research, female breast cancer (BC) continues to be one of the most lethal cancers in the world. Given that 80 % of all diagnosed BC cases are estrogen receptor-positive (ER+) with carcinogenesis driven by estrogen-ERα signalling, current standard of care (SOC) hormone therapies are geared towards modulating the function and expression levels of estrogen and its receptors, ERα and ERβ. Currently, aromatase inhibitors (AIs), selective ER modulators (SERMs) and selective ER degraders (SERDs) are clinically prescribed for the management and treatment of ER+ BC, with the anti-aromatase activity of AIs abrogating estrogen biosynthesis, while the anti-estrogenic SERMs and SERDs antagonise and degrade the ER, respectively. The use of SOC hormone therapies is, however, significantly hampered by the onset of severe side-effects and the development of resistance. Given that numerous studies have reported on the beneficial effects of plant compounds and/or extracts and the multiple pathways through which they target ER+ breast carcinogenesis, recent research has focused on the use of dietary chemopreventive agents for BC management. When combined with SOC treatments, several of these plant components and/or extracts have demonstrated improved efficacy and/or synergistic impact. Moreover, despite a lack of in vivo investigations, plant products are generally reported to have a lower side-effect profile than SOC therapies and are therefore thought to be a safer therapeutic choice. Thus, the current review summarizes the findings from the last five years regarding the anti-aromatase and anti-estrogenic activity of plant products, as well as their synergistic anti-ER+ BC effects in combination with SOC therapies.
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  • 文章类型: Journal Article
    阿霉素(DOX)是一种蒽环类抗癌剂,在治疗实体肿瘤中非常有效。鉴于多柔比星诱导的心脏毒性涉及多种机制,很难确定毒性的精确分子靶标。文献综述的结果表明,天然产物可能对阿霉素诱导的心脏毒性提供心脏保护作用。在体外和体内。然而,需要进一步的验证性研究来证实这一说法。最重要的是将更多的注意力转向复杂的信号网络,这些信号网络对于心肌细胞的存活和功能障碍至关重要。尽管在预防DOX引起的心脏毒性的天然产物的临床前研究中取得了令人鼓舞的进展,这些尚未翻译为临床使用。阻碍开发基于天然产物的心脏保护性佐剂的最重要障碍之一是在人体中缺乏足够的生物利用度。这篇综述概述了关于多柔比星DOX诱导的心脏毒性的最新知识,重点关注天然化合物和草药制剂在预防这种不良反应方面的潜在益处。作为文献搜索引擎,Scopus中的浏览器,PubMed,使用了WebofScience数据库和ClinicalTrials.gov寄存器。
    Doxorubicin (DOX) is an anthracycline anticancer agent that is highly effective in the treatment of solid tumors. Given the multiplicity of mechanisms involved in doxorubicin-induced cardiotoxicity, it is difficult to identify a precise molecular target for toxicity. The findings of a literature review suggest that natural products may offer cardioprotective benefits against doxorubicin-induced cardiotoxicity, both in vitro and in vivo. However, further confirmatory studies are required to substantiate this claim. It is of the utmost importance to direct greater attention towards the intricate signaling networks that are of paramount importance for the survival and dysfunction of cardiomyocytes. Notwithstanding encouraging progress made in preclinical studies of natural products for the prevention of DOX-induced cardiotoxicity, these have not yet been translated for clinical use. One of the most significant obstacles hindering the development of cardioprotective adjuvants based on natural products is the lack of adequate bioavailability in humans. This review presents an overview of current knowledge on doxorubicin DOX-induced cardiotoxicity, with a focus on the potential benefits of natural compounds and herbal preparations in preventing this adverse effect. As literature search engines, the browsers in the Scopus, PubMed, Web of Science databases and the ClinicalTrials.gov register were used.
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  • 文章类型: Journal Article
    慢性粒细胞白血病(CML)是一种以造血干细胞的肿瘤转化为特征的血液系统恶性肿瘤,由费城(Ph)染色体驱动,该染色体由9号和22号染色体之间的易位引起。该Ph染色体包含具有组成型酪氨酸激酶活性的断点簇区(BCR)和Abelson(ABL)癌基因(BCR-ABL1)。然而,BCR-ABL1的酪氨酸激酶活性已被确定为通过c-Abl激酶启动和维持CML的关键参与者。尽管酪氨酸激酶抑制剂取得了进展,挑战,如功效,安全问题,反复出现的耐药性持续存在。本研究旨在从具有抗白血病特性的植物化合物中发现潜在的c-Abl激酶抑制剂。采用药物相似性评估,分子对接,计算机药代动力学(ADMET)筛选,密度泛函理论(DFT),和分子动力学模拟(MDS)。在58种筛选的药物相似性化合物中,44与c-Abl激酶对接。对最受欢迎的化合物(异硫酸酯)和尼洛替尼(对照药物)进行了严格的分析,包括ADMET分析,DFT评估,和100ns的MDS。Isovitexin表现出明显的结合亲和力(-15.492kcal/mol),与尼洛替尼(-16.826千卡/摩尔)非常相似,展示了相似的结合姿态和优越的结构稳定性和反应性。虽然这些发现表明异硫酸酯素是一种潜在的c-Abl激酶抑制剂,必须通过紧急的体外和体内实验进行进一步验证。这项研究有望为解决现有的CML治疗和管理挑战提供替代途径。由RamaswamyH.Sarma沟通。
    Chronic myeloid leukemia (CML) is a hematological malignancy characterized by the neoplastic transformation of hematopoietic stem cells, driven by the Philadelphia (Ph) chromosome resulting from a translocation between chromosomes 9 and 22. This Ph chromosome harbors the breakpoint cluster region (BCR) and the Abelson (ABL) oncogene (BCR-ABL1) which have a constitutive tyrosine kinase activity. However, the tyrosine kinase activity of BCR-ABL1 have been identified as a key player in CML initiation and maintenance through c-Abl kinase. Despite advancements in tyrosine kinase inhibitors, challenges such as efficacy, safety concerns, and recurring drug resistance persist. This study aims to discover potential c-Abl kinase inhibitors from plant compounds with anti-leukemic properties, employing drug-likeness assessment, molecular docking, in silico pharmacokinetics (ADMET) screening, density function theory (DFT), and molecular dynamics simulations (MDS). Out of 58 screened compounds for drug-likeness, 44 were docked against c-Abl kinase. The top hit compound (isovitexin) and nilotinib (control drug) were subjected to rigorous analyses, including ADMET profiling, DFT evaluation, and MDS for 100 ns. Isovitexin demonstrated a notable binding affinity (-15.492 kcal/mol), closely comparable to nilotinib (-16.826 kcal/mol), showcasing a similar binding pose and superior structural stability and reactivity. While these findings suggest isovitexin as a potential c-Abl kinase inhibitor, further validation through urgent in vitro and in vivo experiments is imperative. This research holds promise for providing an alternative avenue to address existing CML treatment and management challenges.Communicated by Ramaswamy H. Sarma.
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  • 文章类型: Journal Article
    细胞外基质的产生增加是对组织损伤和应激的必要反应。在正常的愈合过程中,细胞外基质的增加是短暂的。然而,在某些情况下,细胞外基质的增加可以作为纤维化持续存在,导致器官结构的有害改变,生物力学特性,和功能。的确,纤维化现在被认为是死亡率和发病率的重要原因。广泛的研究表明,纤维化可以减缓,被逮捕甚至被撤销;然而,很少有药物被批准专门用于抗纤维化治疗。这部分是由于负责纤维发生的复杂途径和靶向这些途径的药物的不良副作用。天然产物作为传统药物的主要成分已经使用了数千年,目前占全球临床使用药物的近三分之一。已经证明多种植物衍生的化合物对纤维化具有预防或甚至逆转作用。这篇综述将讨论已经确定影响纤维化的一些主要植物衍生化合物的作用和潜在机制。
    Increased production of extracellular matrix is a necessary response to tissue damage and stress. In a normal healing process, the increase in extracellular matrix is transient. In some instances; however, the increase in extracellular matrix can persist as fibrosis, leading to deleterious alterations in organ structure, biomechanical properties, and function. Indeed, fibrosis is now appreciated to be an important cause of mortality and morbidity. Extensive research has illustrated that fibrosis can be slowed, arrested or even reversed; however, few drugs have been approved specifically for anti-fibrotic treatment. This is in part due to the complex pathways responsible for fibrogenesis and the undesirable side effects of drugs targeting these pathways. Natural products have been utilized for thousands of years as a major component of traditional medicine and currently account for almost one-third of drugs used clinically worldwide. A variety of plant-derived compounds have been demonstrated to have preventative or even reversal effects on fibrosis. This review will discuss the effects and the underlying mechanisms of some of the major plant-derived compounds that have been identified to impact fibrosis.
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  • 文章类型: Journal Article
    迫切需要找到有效预防和治疗皮肤感染的替代抗菌化合物,这使我们研究了八种植物来源的生物活性化合物(桦木醇,姜黄素,甘草酸,guaiazulene,胡椒碱,槲皮素,奎宁,单宁酸)针对根据抗生素耐药性和毒力特征选择的14种犬科皮肤分离株(11种革兰氏阳性细菌和3种革兰氏阴性细菌)。用肉汤微量稀释法测定最小抑菌浓度(MIC)和最小杀菌浓度(MBC)。详细来说,8种不同植物化合物的结果在0.04至16mg/ml(MIC)和0.25至16mg/ml(MBC)的浓度范围内显示出它们的抑制活性。最有效的化合物似乎是单宁酸,其次是奎宁和姜黄素(MIC0.04-16.0mg/ml)。总体上对测试试剂最敏感的菌株是蜡状芽孢杆菌AE13,而屎肠球菌AA14是测试细菌中最具抗性的菌株(最高MIC)。以不同比例(1:1、1:2、2:1)的混合物测试了两种最有效的植物衍生化合物(单宁酸和奎宁)。对于1:2的比例,观察到最低的MIC和MBC值,用于制备具有不同奶油基质的奶油。根据测试菌株,其中一种乳膏制剂(乳膏F)在高达63.0mg/ml(MIC)下有效,微生物灭活时间为1-6小时。这项研究提供了证据,表明一些植物来源的化合物可能对犬科动物的皮肤细菌具有抗菌作用,其强度取决于细菌菌株。
    An urgent need to find alternative antimicrobial compounds effective in the prevention and treatment of skin infections led us to study the inhibitory activity of eight plant-derived bioactive compounds (betulin, curcumin, glycyrrhizic acid, guaiazulene, piperine, quercetin, quinine, tannic acid) against 14 canine skin isolates (11 Gram-positive and three Gram-negative bacteria) selected based on antibiotic resistance and virulence features. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined using the broth microdilution method. In detail, the results for the eight different plant compounds showed their inhibitory activity in the concentration range from 0.04 to more than 16 mg/ml (MIC) and from 0.25 to more than 16 mg/ml (MBC). The most potent compounds appear to be tannic acid, followed by quinine and curcumin (MIC 0.04-16.0 mg/ml). The most susceptible strain to the tested agents in general was Bacillus cereus AE13, while Enterococcus faecium AA14 was the most resistant strain (the highest MICs) among the tested bacteria. The two most potent plant-derived compounds (tannic acid and quinine) were tested in mixture in different ratios (1:1, 1:2, 2:1). The lowest MIC and MBC values were observed for the 1:2 ratio, which was used for preparation of creams with different cream bases. One of the cream formulations (cream F) was effective up to 63.0 mg/ml (MIC) with a microbial inactivation time of 1-6 h according to the tested strain. This study provides evidence that some plant-derived compounds could have an antimicrobial effect against canine skin bacteria, the strength of which is bacterial strain dependent.
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  • 文章类型: Journal Article
    细菌和真菌生物膜增加了抗生素耐药性,在许多持续性疾病中起着至关重要的作用。生物膜相关的慢性感染难以治疗并降低医疗设备的功效。这个全球性问题促使人们进行广泛的研究,以寻找对抗微生物慢性感染的替代策略。已知具有抗生物膜活性的植物生物活性代谢物是缓解该问题的潜在资源。一些药用植物的植物化学筛选显示不同的活性基团,比如二苯乙烯,单宁,生物碱,萜烯,多酚,黄酮类化合物,木脂素,醌,还有香豆素.在植物化合物和常规药物之间的相互作用中可以观察到协同作用。这篇综述分析并总结了植物代谢物与常规抗菌剂对金黄色葡萄球菌生物膜的协同作用的最新知识,铜绿假单胞菌,和白色念珠菌.常规抗菌剂与植物化合物的协同作用可以改变和抑制获得性抗性的机制,减少不良影响,并在较低剂量下获得适当的治疗效果。需要对这些组合及其可能的抗生物膜靶标有更深入的了解,以开发下一代新型抗微生物剂和/或改善当前的抗微生物剂以对抗归因于生物膜的耐药性感染。
    Bacterial and fungal biofilm has increased antibiotic resistance and plays an essential role in many persistent diseases. Biofilm-associated chronic infections are difficult to treat and reduce the efficacy of medical devices. This global problem has prompted extensive research to find alternative strategies to fight microbial chronic infections. Plant bioactive metabolites with antibiofilm activity are known to be potential resources to alleviate this problem. The phytochemical screening of some medicinal plants showed different active groups, such as stilbenes, tannins, alkaloids, terpenes, polyphenolics, flavonoids, lignans, quinones, and coumarins. Synergistic effects can be observed in the interaction between plant compounds and conventional drugs. This review analyses and summarises the current knowledge on the synergistic effects of plant metabolites in combination with conventional antimicrobials against biofilms of Staphylococcus aureus, Pseudomonas aeruginosa, and Candida albicans. The synergism of conventional antimicrobials with plant compounds can modify and inhibit the mechanisms of acquired resistance, reduce undesirable effects, and obtain an appropriate therapeutic effect at lower doses. A deeper knowledge of these combinations and of their possible antibiofilm targets is needed to develop next-generation novel antimicrobials and/or improve current antimicrobials to fight drug-resistant infections attributed to biofilm.
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  • 文章类型: Journal Article
    2型糖尿病(T2D)的特征是胰腺β细胞功能障碍,尽管长期治疗,细胞死亡和β细胞质量损失增加。因此,人们对开发以β细胞为中心的疗法越来越感兴趣。β细胞再生是由增加的β细胞增殖介导的,其他胰岛细胞类型转分化为功能性β样细胞或β细胞祖细胞重编程为完全分化的β细胞。这种介导是由β细胞分化转录因子和细胞周期机制的调节所协调的。这篇综述研究了抗糖尿病植物提取物和植物化学物质的β细胞再生潜力。各种临床前研究,包括体外,体内和离体研究,被突出显示。Further,讨论了潜在的再生机制以及重要的细胞内和细胞外介质。此外,强调了植物化学物质转化为T2D患者再生疗法的潜力,并就未来前景提出了一些建议。
    Type 2 diabetes (T2D) is characterized by pancreatic beta-cell dysfunction, increased cell death and loss of beta-cell mass despite chronic treatment. Consequently, there has been growing interest in developing beta cell-centered therapies. Beta-cell regeneration is mediated by augmented beta-cell proliferation, transdifferentiation of other islet cell types to functional beta-like cells or the reprograming of beta-cell progenitors into fully differentiated beta cells. This mediation is orchestrated by beta-cell differentiation transcription factors and the regulation of the cell cycle machinery. This review investigates the beta-cell regenerative potential of antidiabetic plant extracts and phytochemicals. Various preclinical studies, including in vitro, in vivo and ex vivo studies, are highlighted. Further, the potential regenerative mechanisms and the intra and extracellular mediators that are of significance are discussed. Also, the potential of phytochemicals to translate into regenerative therapies for T2D patients is highlighted, and some suggestions regarding future perspectives are made.
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  • 文章类型: Journal Article
    背景:实验研究强调了用于光动力疗法的植物来源的光敏剂的治疗潜力。此外,一些体外和体内研究表明,鲜为人知的蒽醌可以选择性靶向癌细胞并在光照射后消除它们,具有很好的作用。这篇文献综述总结了PDT中选择的基于植物的光敏剂的当前知识,以显示大黄素的结果,芦荟大黄素,Parietin,rubiadin,金丝桃素,和山梨二醇在光动力疗法癌症治疗中的作用,并描述了它们作为天然光敏剂的作用的综合观点。
    方法:在PubMed.gov上对所选蒽醌进行文献检索,关键字为:\"大黄素\",“芦荟大黄素”,\"金丝桃素\",\"parietin\",\"rubiadin\",“soranjidiol”与“癌症”和“光动力疗法”。
    结果:根据文献数据,这篇综述集中在所有现有的大黄素体外和体内研究,芦荟大黄素,Parietin,rubiadin,山梨二醇用作天然光敏剂,强调其在抗癌治疗中的有效性和详细作用机制。此外,对金丝桃素的全面临床前和临床研究表明,上述物质可能包括在不同癌症的光毒性治疗中。
    结论:总体而言,这篇综述介绍了鲜为人知的蒽醌及其有前途的分子作用机制。预计将来它们可以用作癌症治疗中的天然PS以及金丝桃素。
    BACKGROUND: Experimental studies emphasize the therapeutic potential of plant-derived photosensitizers used in photodynamic therapy. Moreover, several in vitro and in vivo research present the promising roles of less-known anthraquinones that can selectively target cancer cells and eliminate them after light irradiation. This literature review summarizes the current knowledge of chosen plant-based-photosensitizers in PDT to show the results of emodin, aloe-emodin, parietin, rubiadin, hypericin, and soranjidiol in photodynamic therapy of cancer treatment and describe the comprehensive perspective of their role as natural photosensitizers.
    METHODS: Literature searches of chosen anthraquinones were conducted on PubMed.gov with keywords: \"emodin\", \"aloe-emodin\", \"hypericin\", \"parietin\", \"rubiadin\", \"soranjidiol\" with \"cancer\" and \"photodynamic therapy\".
    RESULTS: According to literature data, this review concentrated on all existing in vitro and in vivo studies of emodin, aloe-emodin, parietin, rubiadin, soranjidiol used as natural photosensitizers emphasizing their effectiveness and detailed mechanism of action in anticancer therapy. Moreover, comprehensive preclinical and clinical studies on hypericin reveal that the above-described substances may be included in the phototoxic treatment of different cancers.
    CONCLUSIONS: Overall, this review presented less-known anthraquinones with their promising molecular mechanisms of action. It is expected that in the future they may be used as natural PSs in cancer treatment as well as hypericin.
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  • 文章类型: Journal Article
    存储在图书馆中的档案文件和艺术品经常经历由居住在这些地方的所谓的“生物腐败原”推动的降解过程。那些专注于文化遗产保护和寻找新的安全消毒技术的研究小组对植物衍生产品重新产生了兴趣。在这个观点中,精油(EO)及其挥发性有机成分由于其多功能性作用而非常吸引人。这里介绍了涉及EO和/或其与保护文化遗产感兴趣的纸质物品有关的主要成分的科学出版物的文献调查。旨在揭示这种特殊的植物衍生化合物的益处和局限性。
    Archival documents and artworks stored in libraries frequently undergo degradative processes promoted by the so-called \"biodeteriogens\" that inhabit these places. A renewed interest in plant-derived products has arisen in those research groups focusing on cultural heritage preservation and looking for new and safe disinfection techniques. In this view, essential oils (EOs) and their volatile organic constituents are very appealing thanks to their versatility of action. A literature survey of the scientific publications involving EOs and/or their major constituents related to the conservation of paper items of cultural heritage interest is presented here, aiming to reveal benefits and limitations of such peculiar plant-derived compounds.
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