Natural compounds

天然化合物
  • 文章类型: Journal Article
    监测非传染性疾病被认为是一个至关重要的问题,必须加以管理,以避免各种并发症,例如称为血脂异常的血脂水平升高。他汀类药物,大多数情况下,研究了瑞舒伐他汀(RSV)治疗血脂异常的有效性。然而,达到最有效的治疗是至关重要的,提高RSV的效果是至关重要的。因此,联合治疗是获得显著获益的良好方法.虽然RSV是疏水性的,这将影响其口服后的吸收和生物利用度,克服这个障碍很重要。
    为此,本研究的目的是将RSV掺入某些基于脂质的纳米载体中,即,用初榨椰子油(CCO)制备的纳米结构脂质载体(NLC)。
    选择了优化的RSV-NLC配方,表征和检查其体外,动力学,和稳定性配置文件。最终,研究了该配方的体内降血脂作用。
    优化的NLC制剂显示出合适的粒度(279.3±5.03nm),PDI为0.237,并显示出良好的包封效率(75.6±1.9%)。关于体外释放,有效延长24小时,提供93.7±1.47%。优化的配方在4°C和25°C两种不同条件下储存3个月后稳定。重要的是,在RSV-NLC的开发中包括CCO可以令人印象深刻地增强肥胖大鼠模型中总胆固醇水平的降低,这证明了RSV和CCO之间的潜在协同作用。
    该研究可以阐明使用CCO开发NLC对改善RSV抗高脂血症活性的影响。
    UNASSIGNED: Monitoring noncommunicable diseases is regarded as a critical concern that has to be managed in order to avoid a wide variety of complications such as increasing blood lipid levels known as dyslipidemia. Statin drugs, mostly, Rosuvastatin (RSV) was investigated for its effectiveness in treating dyslipidemia. However, reaching the most efficient treatment is essential and improving the effect of RSV is crucial. Therefore, a combination therapy was a good approach for achieving significant benefit. Although RSV is hydrophobic, which would affect its absorption and bioavailability following oral administration, overcoming this obstacle was important.
    UNASSIGNED: To that end, the purpose of the present investigation was to incorporate RSV into certain lipid-based nanocarriers, namely, nanostructured lipid carrier (NLC) prepared with virgin coconut oil (CCO).
    UNASSIGNED: The optimized RSV-NLC formula was selected, characterized and examined for its in vitro, kinetic, and stability profiles. Eventually, the formula was investigated for its in vivo hypolipidemic action.
    UNASSIGNED: The optimized NLC formulation showed a suitable particle size (279.3±5.03 nm) with PDI 0.237 and displayed good entrapment efficiency (75.6±1.9%). Regarding in vitro release, it was efficiently prolonged for 24 h providing 93.7±1.47%. The optimized formula was established to be stable after 3 months storage at two different conditions; 4°C and 25°C. Importantly, including CCO in the development of RSV-NLC could impressively enhance lowering total cholesterol level in obese rat models, which endorse the potential synergistic action between RSV and CCO.
    UNASSIGNED: The study could elucidate the impact of developing NLC using CCO for improving RSV anti-hyperlipidemic activity.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    全球结直肠癌(CRC)和胃癌(GC)的发病率不断上升,再加上目前化疗药物的疗效有限,优先考虑寻找新的治疗方案。天然物质,通常表现出细胞抑制特性,在这方面有很大的希望。本文综述了三种天然生物碱小檗碱的抗癌特性。血根碱,和白屈菜红碱-抗CRC和GC。体内和体外研究表明,这些物质可以减小肿瘤体积并抑制肿瘤的上皮-间质转化(EMT)。在分子水平上,这些生物碱破坏癌细胞的关键信号通路,包括mTOR,MAPK,EGFR,PI3K/AKT,和NF-κB。此外,它们表现出免疫调节作用,通过凋亡和自噬导致程序性细胞死亡的诱导。值得注意的是,这些物质与经典的细胞抑制剂如环磷酰胺组合时显示出协同作用,5-氟尿嘧啶,西妥昔单抗,还有厄洛替尼.此外,小檗碱已证明能够恢复最初对顺铂GC耐药的个体的敏感性。鉴于这些发现,天然化合物在恶性胃肠道肿瘤的化疗中成为一种有希望的选择,特别是在治疗选择有限的情况下。然而,更多的研究是必要的,以充分了解他们的治疗潜力。
    The rising incidence of colorectal cancer (CRC) and gastric cancer (GC) worldwide, coupled with the limited effectiveness of current chemotherapeutic agents, has prioritized the search for new therapeutic options. Natural substances, which often exhibit cytostatic properties, hold significant promise in this area. This review evaluates the anticancer properties of three natural alkaloids-berberine, sanguinarine, and chelerythrine-against CRC and GC. In vivo and in vitro studies have demonstrated that these substances can reduce tumor volume and inhibit the epithelial-mesenchymal transition (EMT) of tumors. At the molecular level, these alkaloids disrupt key signaling pathways in cancer cells, including mTOR, MAPK, EGFR, PI3K/AKT, and NF-κB. Additionally, they exhibit immunomodulatory effects, leading to the induction of programmed cell death through both apoptosis and autophagy. Notably, these substances have shown synergistic effects when combined with classical cytostatic agents such as cyclophosphamide, 5-fluorouracil, cetuximab, and erlotinib. Furthermore, berberine has demonstrated the ability to restore sensitivity in individuals originally resistant to cisplatin GC. Given these findings, natural compounds emerge as a promising option in the chemotherapy of malignant gastrointestinal tumors, particularly in cases with limited treatment options. However, more research is necessary to fully understand their therapeutic potential.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    胶质母细胞瘤(GBM)是一种严重的脑肿瘤,致死率高。它生长迅速,大多数时候导致对传统治疗如化疗和放疗和手术的抵抗。生物多样性,除了代表人类福祉的重要资源之外,提供了几种天然化合物,显示出作为抗癌药物的巨大潜力。其中许多正在被广泛研究,并通过降低增殖率显着减慢GBM的进展,迁移,和炎症,也通过调节氧化应激。这里,一些天然化合物的使用,比如葱葱,succisapratensis,还有Dianthus超级巴士,被探索以解决GBM;他们展示了他们对细胞数量减少的影响,部分由细胞周期静止给出。此外,据报道,细胞迁移能力降低,通过形态细胞骨架的变化来完成,这甚至突出了间质-上皮转化。此外,代谢研究显示诱导的细胞氧化应激调节和大量的代谢重排。因此,研究人员提出了一种新的治疗选择,以克服常规治疗的局限性,从而改善患者的预后.
    Glioblastoma (GBM) is a severe form of brain tumor that has a high fatality rate. It grows aggressively and most of the time results in resistance to traditional treatments like chemo- and radiotherapy and surgery. Biodiversity, beyond representing a big resource for human well-being, provides several natural compounds that have shown great potential as anticancer drugs. Many of them are being extensively researched and significantly slow GBM progression by reducing the proliferation rate, migration, and inflammation and also by modulating oxidative stress. Here, the use of some natural compounds, such as Allium lusitanicum, Succisa pratensis, and Dianthus superbus, was explored to tackle GBM; they showed their impact on cell number reduction, which was partially given by cell cycle quiescence. Furthermore, a reduced cell migration ability was reported, accomplished by morphological cytoskeleton changes, which even highlighted a mesenchymal-epithelial transition. Furthermore, metabolic studies showed an induced cell oxidative stress modulation and a massive metabolic rearrangement. Therefore, a new therapeutic option was suggested to overcome the limitations of conventional treatments and thereby improve patient outcomes.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    植物来源的天然化合物是发现潜在抗癌药物的重要资源。虽然近年来植物抗癌领域的研究激增,涵盖较长时期并包含最新出版物的系统文献计量分析仍然很少。这里,我们对过去三十年来植物天然化合物的抗癌特性进行了文献计量分析,利用文献计量框架和开放获取平台,KNIME.我们的发现表明,从1992年到2023年,与植物抗癌相关的出版物数量加速增长。国家和机构分析显示,拥有传统医疗系统的国家在植物抗癌领域贡献了很大一部分出版物,比如印度,中国,和韩国。这项研究还突出了十大杰出研究人员和出版物,协助研究人员识别关键文献。主要出版物是化学和生物学相关领域,如药理学和药学,植物科学,生物化学和分子生物学。此外,我们注意到类黄酮是抗癌中的主要植物化合物,具有很强的抗癌潜力。我们的研究为植物抗癌领域的进展和趋势提供了新的见解,并将有助于研究人员掌握未来的研究方向。
    Plant-derived natural compounds are significant resources for the discovery of potential anticancer drugs. While research in the plant-based anticancer field has surged in recent years, systematic bibliometric analyses covering a longer period and containing up-to-date publications remain scarce. Here, we conducted a bibliometric analysis of literature on the anticancer properties of plant natural compounds over the past three decades, leveraging the bibliometric framework and open-access platform, KNIME. Our findings showed that the number of plant anticancer-related publications underwent an accelerating growth from 1992 to 2023. The country and institution analyses revealed that countries with traditional medical systems contributed a large portion of publications in the plant anticancer field, such as India, China, and South Korea. This study also highlighted the top ten eminent researchers and publications, assisting researchers in identifying pivotal literature. The primary publications were domains of chemistry and biology-related fields, such as Pharmacology & Pharmacy, Plant Sciences, and Biochemistry & Molecular Biology. Additionally, we noted that flavonoids have been focal plant compounds in anticancer, with strong anticancer potential. Our study provides new insights into the progress and trends in the plant anticancer field and will assist researchers in grasping the future research direction.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    鼻病毒(RV)引起儿童和成人的上呼吸道感染和肺炎。这些无包膜病毒含有四种衣壳蛋白的病毒外壳:VP1、VP2、VP3和VP4。VP1上的峡谷使用细胞表面受体ICAM-1作为附着位点并用于病毒的内化。迄今为止,目前还没有针对房车的药物或疫苗。在这项研究中,迷迭香(丹参迷迭香L.)的生物活性天然化合物,以其药理潜力而闻名,被认为是靶向VP1蛋白。共有30种迷迭香的生物活性天然化合物被用作靶向病毒蛋白的配体。PkCSM工具用于检测它们对Lipinski规则5的坚持以及所选配体的ADMET性质。Further,CB-Dock工具用于VP1蛋白和配体之间的分子对接研究。根据分子对接和ADMET分析结果,选择苯乙胺(4一甲氧基苄基)作为先导化合物。在先导化合物和两种抗病毒药物之间进行了比较研究,胎盘和硝唑尼特,研究天然化合物相对于合成药物的更高潜力。胎盘也靶向VP1,但在临床试验中失败,而硝唑尼特在针对鼻病毒的临床试验中进行了检查。从这项研究中发现,与其他测试药物相比,(4-甲氧基苄基)苯乙胺对RV表现出更低的毒性。需要更多的研究来确定其潜力,并使其成为对抗房车的良好药物。
    Rhinoviruses (RVs) cause upper respiratory tract infections and pneumonia in children and adults. These non-enveloped viruses contain viral coats of four capsid proteins: VP1, VP2, VP3, and VP4. The canyon on VP1 used cell surface receptor ICAM-1 as the site of attachment and for the internalization of viruses. To date, there has been no drug or vaccine available against RVs. In this study, bioactive natural compounds of rosemary (Salvia rosmarinus L.), which are known for their pharmacological potential, were considered to target the VP1 protein. A total of 30 bioactive natural compounds of rosemary were taken as ligands to target viral proteins. The PkCSM tool was used to detect their adherence to Lipinski\'s rule of five and the ADMET properties of the selected ligands. Further, the CB-Dock tool was used for molecular docking studies between the VP1 protein and ligands. Based on the molecular docking and ADMET profiling results, phenethyl amine (4 methoxy benzyl) was selected as the lead compound. A comparative study was performed between the lead compound and two antiviral drugs, Placonaril and Nitazoxanide, to investigate the higher potential of natural compounds over synthetic drugs. Placonaril also targets VP1 but failed in clinical trials while Nitazoxanide was examined in clinical trials against rhinoviruses. It was discovered from this study that the (4 methoxy benzyl) phenethyl amine exhibited less toxicity in comparison to other tested drugs against RVs. More research is needed to determine its potential and make it a good medication against RVs.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    被认为是糖尿病(DM)常见的微血管并发症,糖尿病肾病(DN)是慢性终末期肾病(ESRD)的主要原因。患有糖尿病的患者具有发展进行性肾脏疾病的大约25%的风险。DN控制的基本原则目标是通过钠葡萄糖协同转运蛋白2(SGLT2)阻断进行血糖调节和通过肾素-血管紧张素-醛固酮抑制进行高血压管理的双重结果。然而,这些治疗在阻止疾病进展为肾衰竭和心血管合并症方面无效.最近,亚细胞信号传导通路的失调越来越多地参与DN的发病机制。天然化合物正在成为靶向细胞内途径的有效且无副作用的治疗剂。这篇叙述性综述综合了最近对DN维持途径失调的见解,来自动物和人类研究。为了编写这篇评论,从PubMed收集了报道DN信号通路及其用天然类黄酮治疗的文章,Cochrane图书馆WebofScience,自2000年以来,GoogleScholar和EMBASE数据库。由于治疗干预措施通常基于临床试验的结果,对当前DNII期和III期临床试验的数据进行了简要分析。
    Recognized as a common microvascular complication of diabetes mellitus (DM), diabetic nephropathy (DN) is the principal cause of chronic end-stage renal disease (ESRD). Patients with diabetes have an approximately 25% risk of developing progressive renal disease. The underlying principles of DN control targets the dual outcomes of blood glucose regulation through sodium glucose cotransporter 2 (SGLT 2) blockade and hypertension management through renin-angiotensin-aldosterone inhibition. However, these treatments are ineffective in halting disease progression to kidney failure and cardiovascular comorbidities. Recently, the dysregulation of subcellular signaling pathways has been increasingly implicated in DN pathogenesis. Natural compounds are emerging as effective and side-effect-free therapeutic agents that target intracellular pathways. This narrative review synthesizes recent insights into the dysregulation of maintenance pathways in DN, drawing from animal and human studies. To compile this review, articles reporting DN signaling pathways and their treatment with natural flavonoids were collected from PubMed, Cochrane Library Web of Science, Google Scholar and EMBASE databases since 2000. As therapeutic interventions are frequently based on the results of clinical trials, a brief analysis of data from current phase II and III clinical trials on DN is discussed.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    衰老是一个受遗传因素影响的多方面过程,生活方式,和环境因素。随着时间的推移,人体经历主要功能的退行性变化。衰老的外部和内部迹象以各种方式表现出来,包括皮肤干燥,皱纹,肌肉骨骼疾病,心血管疾病,糖尿病,神经退行性疾病,和癌症。此外,癌症,比如衰老,是一种复杂的疾病,源于各种遗传和表观遗传改变的积累。昼夜节律时钟失调最近被认为是衰老和癌症发展的重要危险因素。天然化合物和草药因其在预防与年龄有关的疾病和抑制癌症进展方面的潜力而受到广泛关注。这些化合物显示出抗氧化剂,抗炎,抗增殖,促凋亡,抗转移性,和抗血管生成作用以及生物钟调节。这篇综述探讨了与年龄有关的疾病,癌症,以及特定天然化合物靶向这些疾病关键特征的潜力。
    Aging is a multifaceted process influenced by hereditary factors, lifestyle, and environmental elements. As time progresses, the human body experiences degenerative changes in major functions. The external and internal signs of aging manifest in various ways, including skin dryness, wrinkles, musculoskeletal disorders, cardiovascular diseases, diabetes, neurodegenerative disorders, and cancer. Additionally, cancer, like aging, is a complex disease that arises from the accumulation of various genetic and epigenetic alterations. Circadian clock dysregulation has recently been identified as an important risk factor for aging and cancer development. Natural compounds and herbal medicines have gained significant attention for their potential in preventing age-related diseases and inhibiting cancer progression. These compounds demonstrate antioxidant, anti-inflammatory, anti-proliferative, pro-apoptotic, anti-metastatic, and anti-angiogenic effects as well as circadian clock regulation. This review explores age-related diseases, cancers, and the potential of specific natural compounds in targeting the key features of these conditions.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    阿尔茨海默病(AD)大脑的组织学特征是存在细胞内和细胞外淀粉样蛋白沉积,这是该疾病发病机理的特征。越来越多的证据表明,某些营养素对淀粉样蛋白β(Aβ)-肽的产生和积累产生直接或间接的影响,因此,关于AD发病机制。我们利用果蝇果蝇AD模型来评估体内LisosanG的有益特性,从有机全谷物中获得的发酵粉末,对AD细胞内Aβ-42肽积累及相关病理表型的影响。我们的数据表明,富含LisosanG的饮食可减弱果蝇大脑中神经毒性Aβ肽的产生并减少神经元凋亡。值得注意的是,LisosanG发挥抗氧化作用,降低大脑活性氧的水平,增强线粒体活性。这些方面与自噬周转的增加和核仁应激的抑制平行。我们的结果支持使用果蝇模型不仅可以研究神经退行性疾病的分子遗传基础,而且可以快速可靠地测试潜在治疗剂和饮食方案的效率。
    Alzheimer\'s disease (AD) brains are histologically marked by the presence of intracellular and extracellular amyloid deposits, which characterize the onset of the disease pathogenesis. Increasing evidence suggests that certain nutrients exert a direct or indirect effect on amyloid β (Aβ)-peptide production and accumulation and, consequently, on AD pathogenesis. We exploited the fruit fly Drosophila melanogaster model of AD to evaluate in vivo the beneficial properties of Lisosan G, a fermented powder obtained from organic whole grains, on the intracellular Aβ-42 peptide accumulation and related pathological phenotypes of AD. Our data showed that the Lisosan G-enriched diet attenuates the production of neurotoxic Aβ peptides in fly brains and reduces neuronal apoptosis. Notably, Lisosan G exerted anti-oxidant effects, lowering brain levels of reactive oxygen species and enhancing mitochondrial activity. These aspects paralleled the increase in autophagy turnover and the inhibition of nucleolar stress. Our results give support to the use of the Drosophila model not only to investigate the molecular genetic bases of neurodegenerative disease but also to rapidly and reliably test the efficiency of potential therapeutic agents and diet regimens.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    类风湿性关节炎(RA)是一种以关节炎症为特征的持续性自身免疫性疾病,不适,和减值。尽管存在几种治疗方法,它们的有效性通常受到限制,并且可能与不利的副作用有关。因此,人们对研究天然衍生的化合物作为RA疾病的合理治疗剂的兴趣与日俱增.这篇综述的目的是总结现有的临床前和临床证据,关于天然提取的化合物和植物提取物在治疗RA中的功效,专注于他们的抗炎,抗氧化,和免疫调节特性。使用天然化学品的一些问题是市售制剂的质量不均匀和这些化合物的生物利用度较差。未来的调查应侧重于改进配方,进行彻底的临床试验,并探索不同的技术,以充分利用天然来源的化学物质在治疗RA的内在潜力。
    Rheumatoid arthritis (RA) is a persistent autoimmune disorder that is characterized by joint inflammation, discomfort, and impairment. Despite the existence of several therapeutic approaches, their effectiveness is often restricted and may be linked to unfavorable side effects. Consequently, there has been growing interest in investigating naturally derived compounds as plausible therapeutic agents for RA disease. The objective of this review is to summarize the existing preclinical and clinical evidence regarding the efficacy of naturally extracted compounds and plant extracts in the treatment of RA, focusing on their anti-inflammatory, anti-oxidative, and immunomodulatory properties. Some of the problems with using natural chemicals are the uneven quality of commercially available preparations and the poor bioavailability of these compounds. Future investigations should focus on improving the formulations, conducting thorough clinical trials, and exploring different techniques to fully utilize the intrinsic potential of naturally derived chemicals in treating RA.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    寄生虫病,比如疟疾,是许多低收入和中等收入国家的巨大负担。2022年,仅世界卫生组织就报告了2.49亿病例和608,000例死亡。气候变化,冲突,人道主义危机,资源限制和各种生物挑战威胁着消除疟疾的进展。不可否认,缺乏商业化疫苗和耐药寄生虫的传播,需要新的方法来治疗这种传染病。迄今为止,大多数发展抗疟药的方法都来自热带或亚热带环境;然而,有必要扩大我们的搜索范围。在这次审查中,我们强调了抗疟疾治疗的起源,并在寻找新型抗寄生虫治疗方法方面提出了新的见解。生活在恶劣和寒冷环境中的植物和微生物,例如在加拿大北部未开发的北方森林中发现的那些,经常表现出在其他环境中找不到的有趣属性。最突出的是,杜鹃花的精油。来自Nunavik的亚克菌和从Nunavut中发现的被孢霉物种中分离出的mortiamides对恶性疟原虫显示出了有希望的活性。
    Parasitic diseases, such as malaria, are an immense burden to many low- and middle-income countries. In 2022, 249 million cases and 608,000 deaths were reported by the World Health Organization for malaria alone. Climate change, conflict, humanitarian crises, resource constraints and diverse biological challenges threaten progress in the elimination of malaria. Undeniably, the lack of a commercialized vaccine and the spread of drug-resistant parasites beg the need for novel approaches to treat this infectious disease. Most approaches for the development of antimalarials to date take inspiration from tropical or sub-tropical environments; however, it is necessary to expand our search. In this review, we highlight the origin of antimalarial treatments and propose new insights in the search for developing novel antiparasitic treatments. Plants and microorganisms living in harsh and cold environments, such as those found in the largely unexploited Northern Canadian boreal forest, often demonstrate interesting properties that are not found in other environments. Most prominently, the essential oil of Rhododendron tomentosum spp. Subarcticum from Nunavik and mortiamides isolated from Mortierella species found in Nunavut have shown promising activity against Plasmodium falciparum.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

公众号