natural compounds

天然化合物
  • 文章类型: Journal Article
    COVID-19大流行,由SARS-CoV-2病毒感染引起的,与认知障碍和阿尔茨海默病(AD)进展有关。一旦它进入大脑,SARS-CoV-2病毒刺激大脑中淀粉样蛋白的积累,对神经细胞有很强的毒性。这些淀粉样蛋白可能引发COVID-19的神经症状。脑膜淋巴管(MLV)在清除毒素和介导病毒从大脑中排出中起重要作用。MLV被认为是预防COVID-19加剧的痴呆的有希望的靶标。然而,增强MLV功能的方法有限。这篇综述强调了与神经症状相关的COVID-19介导的淀粉样蛋白在大脑中积累领域的新发现,以及通过淋巴和其他途径刺激淀粉样蛋白从大脑中清除的有希望的策略的发展。这些策略基于治疗COVID-19感染引起的脑功能障碍的创新方法,包括光生物调节的使用,疟原虫,和草药,这为应对SARS-CoV-2病毒带来的挑战提供了希望。
    The COVID-19 pandemic, caused by infection with the SARS-CoV-2 virus, is associated with cognitive impairment and Alzheimer\'s disease (AD) progression. Once it enters the brain, the SARS-CoV-2 virus stimulates accumulation of amyloids in the brain that are highly toxic to neural cells. These amyloids may trigger neurological symptoms in COVID-19. The meningeal lymphatic vessels (MLVs) play an important role in removal of toxins and mediate viral drainage from the brain. MLVs are considered a promising target to prevent COVID-19-exacerbated dementia. However, there are limited methods for augmentation of MLV function. This review highlights new discoveries in the field of COVID-19-mediated amyloid accumulation in the brain associated with the neurological symptoms and the development of promising strategies to stimulate clearance of amyloids from the brain through lymphatic and other pathways. These strategies are based on innovative methods of treating brain dysfunction induced by COVID-19 infection, including the use of photobiomodulation, plasmalogens, and medicinal herbs, which offer hope for addressing the challenges posed by the SARS-CoV-2 virus.
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  • 文章类型: Journal Article
    这篇综述的目的是介绍樟脑-双环单萜酮在预防皮肤感染中的潜在应用。皮肤病代表一组异质性疾病,其特征在于显著降低生活质量的延长症状。它们影响真皮,表皮,甚至是皮下组织.它们通常具有细菌或真菌背景。皮肤病学皮肤病的治疗是困难和长期的。因此,找到一个化合物很重要,最好是天然来源的,(i)防止这种感染的开始和(ii)支持皮肤的修复过程。根据其记录的抗炎作用,抗菌,抗真菌药,抗痤疮,麻醉剂,加强,和变暖特性,樟脑可用作皮肤传染病的预防措施,也可用作医疗和化妆品的成分。这项工作讨论了樟脑的结构和理化性质,它的发生,以及从天然来源以及通过化学合成获得它的方法。还介绍了樟脑在工业制剂中的用途。此外,在详细查阅文献后,樟脑的新陈代谢,它与其他药用物质的相互作用,讨论了其对皮肤病中涉及的细菌和真菌的抗微生物特性。
    The aim of this review is to present the potential application of camphor-a bicyclic monoterpene ketone-in the prevention of skin infections. Skin diseases represent a heterogeneous group of disorders characterized by prolonged symptoms that significantly diminish the quality of life. They affect the dermis, the epidermis, and even subcutaneous tissue. They very often have a bacterial or fungal background. Therapy for dermatological skin disorders is difficult and long-term. Therefore, it is important to find a compound, preferably of natural origin, that (i) prevents the initiation of this infection and (ii) supports the skin\'s repair process. Based on its documented anti-inflammatory, antibacterial, antifungal, anti-acne, anesthetic, strengthening, and warming properties, camphor can be used as a preventative measure in dermatological infectious diseases and as a component in medical and cosmetic products. This work discusses the structure and physicochemical properties of camphor, its occurrence, and methods of obtaining it from natural sources as well as through chemical synthesis. The use of camphor in industrial preparations is also presented. Additionally, after a detailed review of the literature, the metabolism of camphor, its interactions with other medicinal substances, and its antimicrobial properties against bacteria and fungi involved in skin diseases are discussed with regard to their resistance.
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  • 文章类型: Journal Article
    5-羟色胺(5-羟色胺,5-HT)是一种调节众多生理功能的神经递质,它的失调是精神分裂症病理过程的重要组成部分,抑郁症,偏头痛,和肥胖。5-HT与14种不同的受体相互作用,其中5-HT1A-1FR,5-HT2A-CR,5-HT4-7Rs是G蛋白偶联受体(GPCRs),而5-HT3R是配体门控离子通道。多年来,已经确定了几乎所有5-羟色胺受体的选择性正构配体,产生几种临床相关药物。然而,5-HTRs和其他GPCRs之间的高度同源性意味着正构配体可能具有严重的副作用。因此,最近对开发更安全的GPCRs配体的兴趣增加,绑定到不太保守的,更具体的网站,不同于受体的天然配体。本综述描述了5-羟色胺受体的变构配体的鉴定,主要是天然化合物(油酰胺,大麻二酚,THC,和阿帕芬生物碱),补充合成调节剂在很大程度上为5-HT2C受体开发。后者是积极的变构调节剂,因为它们作为药物的潜力优于正构激动剂作为抗肥胖剂,因为它们可能更安全。如果可用,将提供有关配体和变构结合位点之间相互作用的详细信息。还将对该领域的未来研究进行展望。
    Serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter regulating numerous physiological functions, and its dysregulation is a crucial component of the pathological processes of schizophrenia, depression, migraines, and obesity. 5-HT interacts with 14 different receptors, of which 5-HT1A-1FRs, 5-HT2A-CRs, and 5-HT4-7Rs are G protein-coupled receptors (GPCRs), while 5-HT3R is a ligand-gated ion channel. Over the years, selective orthosteric ligands have been identified for almost all serotonin receptors, yielding several clinically relevant drugs. However, the high degree of homology between 5-HTRs and other GPCRs means that orthosteric ligands can have severe side effects. Thus, there has recently been increased interest in developing safer ligands of GPCRs, which bind to less conserved, more specific sites, distinct from that of the receptor\'s natural ligand. The present review describes the identification of allosteric ligands of serotonin receptors, which are largely natural compounds (oleamide, cannabidiol, THC, and aporphine alkaloids), complemented by synthetic modulators developed in large part for the 5-HT2C receptor. The latter are positive allosteric modulators sought after for their potential as drugs preferable over the orthosteric agonists as antiobesity agents for their potentially safer profile. When available, details on the interactions between the ligand and allosteric binding site will be provided. An outlook on future research in the field will also be provided.
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  • 文章类型: Journal Article
    毒死蜱(CPF)是一种广泛使用的有机磷酸盐杀虫剂,尽管它的过度使用会导致环境污染,引起人们对其对人类健康的不利影响的担忧。在这方面,由于其治疗特性,荨麻是抵消化学“污染物”毒性的有希望的候选者。因此,我们的研究旨在研究荨麻乙醇提取物(UDE)减轻毒死蜱诱导的毒性的潜力。已经鉴定了荨麻乙醇提取物中的八种化合物,其中大多数都具有作为抗氧化剂的巨大潜力,抗炎,和神经保护剂.毒死蜱暴露改变了孵化率,增加了致畸作用的发生率,并上调斑马鱼幼虫端脑脑源性神经营养因子(Bdnf)的表达。另一方面,UDE证明了对CPF诱导的致畸性的预防作用,表现为较低的形态畸形率。此外,UDE表现出相当的保护作用,维持端脑的生理状态。此外,CPF改变了幼虫的运动行为,其特征是不规则游泳和活动增加。UDE略微减弱了这种有缺陷的行为模式。我们的发现表明,UDE对CPF诱导的毒性具有显著的保护特性,可能是由其天然抗氧化剂和抗炎含量赋予的。尽管如此,需要进一步的研究来阐明UDE保护作用的招募机制和相关途径。
    Chlorpyrifos (CPF) is a widely used organophosphate insecticide, though its excessive use causes environmental contamination, raising concerns about its adverse effects on human health. In this regard, Urtica dioica stands out as a promising candidate for counteracting chemical \'contaminant\' toxicity thanks to its therapeutic properties. Therefore, our study aimed to investigate the potential of an Urtica dioica ethanolic extract (UDE) to mitigate chlorpyrifos-induced toxicity. Eight compounds in the Urtica dioica ethanolic extract have been identified, most of which present significant potential as antioxidant, anti-inflammatory, and neuroprotective agents. Chlorpyrifos exposure altered hatching rates, increased the incidence of teratogenic effects, and upregulated the expression of brain-derived neurotrophic factor (Bdnf) in zebrafish larvae telencephalon. On the other hand, UDE demonstrated a preventive effect against CPF-induced teratogenicity, which is expressed by a lower morphological deformity rate. Moreover, the UDE showed a rather protective effect, maintaining the physiological condition of the telencephalon. Additionally, CPF altered the locomotor behavior of larvae, which was characterized by irregular swimming and increased activity. This defective behavioral pattern was slightly attenuated by the UDE. Our findings suggest that the UDE possesses significant protective properties against CPF-induced toxicity, probably conferred by its natural antioxidant and anti-inflammatory contents. Still, further research is needed to elucidate the recruited mechanisms and implicated pathways on UDE\'s protective effects.
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  • 文章类型: Journal Article
    这篇综述评估了具有药用和食用特性的蘑菇多糖的治疗效果。最近研究了真菌多糖,关注它们对肠道微生物群的调节及其对各种疾病的影响。该研究涵盖了临床和临床前研究,详述结果,并强调这些多糖对肠道微生物群调节的显著影响。它讨论了将这些多糖纳入饮食以管理糖尿病等慢性疾病的潜在健康益处,神经退行性疾病,和癌症。此外,这篇综述强调了真菌多糖与肠道微生物群之间的相互作用,强调它们在调节肠道微生物群落中的作用。它对研究结果进行了系统分析,证明真菌多糖对肠道菌群组成和功能的实质性影响,这可能有助于它们在各种慢性疾病中的治疗效果。我们得出的结论是,这些多糖对肠道微生物群的调节可能在介导其治疗效果中起着至关重要的作用。为疾病预防和治疗的进一步研究和潜在应用提供了有希望的途径。
    This review evaluates the therapeutic effects of polysaccharides derived from mushroom species that have medicinal and edible properties. The fungal polysaccharides were recently studied, focusing on their modulation of the gut microbiota and their impact on various diseases. The study covers both clinical and preclinical studies, detailing the results and highlighting the significant influence of these polysaccharides on gut microbiota modulation. It discusses the potential health benefits derived from incorporating these polysaccharides into the diet for managing chronic diseases such as diabetes, neurodegenerative disorders, and cancer. Furthermore, the review emphasizes the interaction between fungal polysaccharides and the gut microbiota, underscoring their role in modulating the gut microbial community. It presents a systematic analysis of the findings, demonstrating the substantial impact of fungal polysaccharides on gut microbiota composition and function, which may contribute to their therapeutic effects in various chronic conditions. We conclude that the modulation of the gut microbiota by these polysaccharides may play a crucial role in mediating their therapeutic effects, offering a promising avenue for further research and potential applications in disease prevention and treatment.
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  • 文章类型: Journal Article
    在龋齿预防中,存在从使用常规药物口腔护理产品到使用草药提取物和传统疗法的日益转变。这归因于当代口腔产品的潜在环境和健康影响。这篇全面的综述旨在分析植物衍生化合物作为龋齿研究中的预防方式。它侧重于从2019年到最近收集的数据,试图强调这个话题的当前趋势。研究结果表明,几种植物来源的化合物,水性或乙醇,对变形链球菌和其他与龋齿相关的细菌表现出显著的抗菌作用,一些提取物证明了与氯己定相当的功效。此外,使用掺入食品衍生物中的植物衍生化合物进行体内研究,比如棒棒糖,通过显着减少高风险龋齿儿童的变形链球菌,已显示出有希望的结果。对植物衍生化合物的体外研究揭示了对变异链球菌的杀菌和抑菌活性,提示它们作为龋齿预防药物的潜在用途。药用植物,植物来源的植物化学物质,精油,和其他食品化合物对口腔病原体表现出了有希望的抗菌活性,要么通过它们的抗粘连活性,细胞外微生物酶的抑制,或它们对微生物物种和酸生产的直接作用。然而,需要进一步的研究来评估它们的抗菌活性,并评估这些植物衍生化合物的细胞毒性和安全性,然后才能推荐其广泛的临床应用.
    There is a growing shift from the use of conventional pharmaceutical oral care products to the use of herbal extracts and traditional remedies in dental caries prevention. This is attributed to the potential environmental and health implications of contemporary oral products. This comprehensive review aims at the analysis of plant-derived compounds as preventive modalities in dental caries research. It focuses on data collected from 2019 until recently, trying to emphasize current trends in this topic. The research findings suggest that several plant-derived compounds, either aqueous or ethanolic, exhibit notable antibacterial effects against Streptococcus mutans and other bacteria related to dental caries, with some extracts demonstrating an efficacy comparable to that of chlorhexidine. Furthermore, in vivo studies using plant-derived compounds incorporated in food derivatives, such as lollipops, have shown promising results by significantly reducing Streptococcus mutans in high-risk caries children. In vitro studies on plant-derived compounds have revealed bactericidal and bacteriostatic activity against S. mutans, suggesting their potential use as dental caries preventive agents. Medicinal plants, plant-derived phytochemicals, essential oils, and other food compounds have exhibited promising antimicrobial activity against oral pathogens, either by their anti-adhesion activity, the inhibition of extracellular microbial enzymes, or their direct action on microbial species and acid production. However, further research is needed to assess their antimicrobial activity and to evaluate the cytotoxicity and safety profiles of these plant-derived compounds before their widespread clinical use can be recommended.
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  • 文章类型: Journal Article
    复杂生理液的成功替代,比如人类的唾液,仍然是药物开发的主要挑战。虽然市场上有大量的唾液替代品,由于在口中的停留时间短,它们的功效通常不足,不愉快的口感,或牙齿保护不足。因此,需要识别模拟唾液功能的系统,特别是唾液粘蛋白MUC5B和唾液的独特生理特性。为此,研究了已知含有水胶体多糖并具有粘液形成特性的植物提取物,以评估其作为唾液替代品的适用性。金盏花的水性植物提取物,Fucussp.Thalli,使用一系列技术检查了地衣和地衣的成分,包括GC-MS,NMR,SEC,pH值评估,渗透压,缓冲能力,粘弹性,与人类唾液的粘弹性相互作用,水胶体网络形成,和体外细胞粘附。为此,使用人颊上皮细胞开发了一种生理适应的粘附试验。结果表明,地衣多糖是模拟MUC5B特性的最有希望的候选物。通过调节pH值,渗透压,与K2HPO4的缓冲能力,表明地衣多糖表现出很高的细胞粘附力,具有与未刺激的整个口腔唾液相当的最大分离力。
    The successful substitution of complex physiological fluids, such as human saliva, remains a major challenge in drug development. Although there are a large number of saliva substitutes on the market, their efficacy is often inadequate due to short residence time in the mouth, unpleasant mouthfeel, or insufficient protection of the teeth. Therefore, systems need to be identified that mimic the functions of saliva, in particular the salivary mucin MUC5B and the unique physiological properties of saliva. To this end, plant extracts known to contain hydrocolloid polysaccharides and to have mucus-forming properties were studied to evaluate their suitability as saliva substitutes. The aqueous plant extracts of Calendula officinalis, Fucus sp. thalli, and lichenan from Lichen islandicus were examined for composition using a range of techniques, including GC-MS, NMR, SEC, assessment of pH, osmolality, buffering capacity, viscoelasticity, viscoelastic interactions with human saliva, hydrocolloid network formation, and in vitro cell adhesion. For this purpose, a physiologically adapted adhesive test was developed using human buccal epithelial cells. The results show that lichenan is the most promising candidate to mimic the properties of MUC5B. By adjusting the pH, osmolality, and buffering capacity with K2HPO4, it was shown that lichenan exhibited high cell adhesion, with a maximum detachment force that was comparable to that of unstimulated whole mouth saliva.
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  • 文章类型: Journal Article
    在目前的工作中,根据目前的临床前研究结果,对天然化合物与常规化疗药物之间的协同作用进行了全面综述。肺癌患者预后较差,5年生存率为18.1%。天然化合物与常规化疗药物的组合使用作为治疗肺癌的潜在新方法已经获得了极大的关注。目前的工作强调了寻找更有效的治疗方法以提高生存率的重要性。化疗是肺癌的主要治疗选择,但它有局限性,如降低有效性,因为癌细胞变得耐药。从药用植物中分离的天然化合物已显示出有希望的抗癌或化学预防特性,并且当与常规疗法组合时,已观察到它们的协同作用。抗癌药物和天然化合物的联合使用表现出协同作用,增强对癌细胞的整体治疗作用。总之,这项工作概述了药用植物和植物衍生化合物作为肺癌化疗的替代或补充治疗方案的最新临床前研究,并讨论了天然化合物在治疗肺癌方面的潜力,副作用最小。
    In the current work, the synergy between natural compounds and conventional chemotherapeutic drugs is comprehensively reviewed in light of current preclinical research findings. The prognosis for lung cancer patients is poor, with a 5-year survival rate of 18.1%. The use of natural compounds in combination with conventional chemotherapeutic drugs has gained significant attention as a potential novel approach in the treatment of lung cancer. The present work highlights the importance of finding more effective therapies to increase survival rates. Chemotherapy is a primary treatment option for lung cancer but it has limitations such as reduced effectiveness because cancer cells become resistant. Natural compounds isolated from medicinal plants have shown promising anticancer or chemopreventive properties and their synergistic effect has been observed when combined with conventional therapies. The combined use of an anti-cancer drug and a natural compound exhibits synergistic effects, enhancing overall therapeutic actions against cancer cells. In conclusion, this work provides an overview of the latest preclinical research on medicinal plants and plant-derived compounds as alternative or complementary treatment options for lung cancer chemotherapy and discusses the potential of natural compounds in treating lung cancer with minimal side effects.
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  • 文章类型: Journal Article
    尽管过去努力进行治疗创新,癌症仍然是一种高度偶发和致命的疾病,目前的治疗缺乏效率,并导致严重的副作用。因此,必须开发新的,更有效率,更安全的疗法。蜂毒已被证明具有多重和协同的生物活性,包括抗肿瘤作用.然而,一些毒性作用与其给药有关。为了解决这些问题,在这项工作中,开发了载有蜂毒的niosomes,癌症治疗。囊泡具有小(150nm)和均匀(多分散指数为0.162)的粒度,并在体外胃中显示出良好的治疗效果,结直肠,乳房,肺,和宫颈癌模型(抑制浓度在12.37ng/mL和14.72ng/mL之间)。此外,它们还显示出实质性的抗炎活性(抑制浓度为28.98ng/mL),与直接抗肿瘤活性互补的作用。还评估了Niosome安全性,两者都在体外(皮肤,肝脏,和肾细胞)和离体(鸡卵绒毛尿囊膜),结果表明,复合包封提高了其安全性。因此,小,并成功开发了同质的蜂毒niosome,具有显著的抗癌和抗炎作用,使它们成为潜在的有前途的主要或辅助癌症疗法。未来的研究应该集中在评估开发的平台在体内模型中的潜力。
    Despite past efforts towards therapeutical innovation, cancer remains a highly incident and lethal disease, with current treatments lacking efficiency and leading to severe side effects. Hence, it is imperative to develop new, more efficient, and safer therapies. Bee venom has proven to have multiple and synergistic bioactivities, including antitumor effects. Nevertheless, some toxic effects have been associated with its administration. To tackle these issues, in this work, bee venom-loaded niosomes were developed, for cancer treatment. The vesicles had a small (150 nm) and homogeneous (polydispersity index of 0.162) particle size, and revealed good therapeutic efficacy in in vitro gastric, colorectal, breast, lung, and cervical cancer models (inhibitory concentrations between 12.37 ng/mL and 14.72 ng/mL). Additionally, they also revealed substantial anti-inflammatory activity (inhibitory concentration of 28.98 ng/mL), effects complementary to direct antitumor activity. Niosome safety was also assessed, both in vitro (skin, liver, and kidney cells) and ex vivo (hen\'s egg chorioallantoic membrane), and results showed that compound encapsulation increased its safety. Hence, small, and homogeneous bee venom-loaded niosomes were successfully developed, with substantial anticancer and anti-inflammatory effects, making them potentially promising primary or adjuvant cancer therapies. Future research should focus on evaluating the potential of the developed platform in in vivo models.
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  • 文章类型: Journal Article
    这项研究旨在获得和表征水包油纳米乳液(NE),其中装载了50%牛至的体外优化的杀菌精油混合物,40%百里香,和10%柠檬草,并评估其在三种不同浓度(0.5%,1%,和2%)在大肠杆菌的灭活中,金黄色葡萄球菌,在4°C下储存9天的虹鳟鱼鱼片中接种肠炎沙门氏菌血清型肠炎。关于NE,通过2.09W/cm2的超声成功获得了纳米尺寸(<100nm)和低多分散性(0.17±0.02)。考虑到使用的三种浓度,肠炎是最易感的。另一方面,比较使用的浓度,2%的NE表现出更好的活性,减少肠炎沙门氏菌,大肠杆菌,和金黄色葡萄球菌分别为0.33、0.20和0.73logCFU/g,分别,在鳟鱼鱼片里。因此,这些数据表明,这是一种有前途的生态友好型替代品,可以生产安全的鱼类供消费,并降低公共卫生风险。
    This study aimed to obtain and characterize an oil-in-water nanoemulsion (NE) loaded with an in vitro optimized bactericidal essential oil blend of 50% oregano, 40% thyme, and 10% lemongrass and to evaluate its potential at three different concentrations (0.5%, 1%, and 2%) in the inactivation of Escherichia coli, Staphylococcus aureus, and Salmonella enterica serotype Enteritidis inoculated in rainbow trout fillets stored at 4 °C for 9 days. Regarding the NE, the nanometric size (<100 nm) with low polydispersion (0.17 ± 0.02) was successfully obtained through ultrasound at 2.09 W/cm2. Considering the three concentrations used, S. Enteritidis was the most susceptible. On the other hand, comparing the concentrations used, the NE at 2% showed better activity, reducing S. Enteritidis, E. coli, and S. aureus by 0.33, 0.20, and 0.73 log CFU/g, respectively, in the trout fillets. Thus, this data indicates that this is a promising eco-friendly alternative to produce safe fish for consumption and reduce public health risks.
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