marine drugs

海洋药物
  • 文章类型: Journal Article
    通过监测淀粉样蛋白β肽(1-40)和复合脂质体的混合分散体多分散性的变化,间接研究了淀粉样蛋白聚集的动力学。脂质体由1,2-二油酰基-sn-glicero-3-磷胆碱(DOPC)磷脂制备,并通过κ-角叉菜胶的静电吸附稳定。所产生的装载和卸载的高牛磺酸的脂质体在磷酸盐缓冲液(pH4和7.4)中具有高度负的电动电势和显着的稳定性。第一次,Aβ聚集的出现和演变通过从粒度分布分析获得的标准百分位数读数(D10,D50和D90)的变化来呈现。动力学实验表明在混合脂质体和肽溶液后几乎30分钟出现第一聚集体。观察到通过添加未加载的脂质体,分散体中90%的颗粒的尺寸(D90)增加。相比之下,在动力学实验过程中,添加负载高牛磺酸的脂质体对较大颗粒级分的大小影响几乎最小.尽管高牛磺酸在天然细胞膜的存在下具有特定的生物活性,这项研究报道,由于电荷效应和“分子拥挤”,该化合物对淀粉样肽聚集有额外的抑制作用。
    The kinetics of amyloid aggregation was studied indirectly by monitoring the changes in the polydispersity of mixed dispersion of amyloid β peptide (1-40) and composite liposomes. The liposomes were prepared from the 1,2-dioleoyl-sn-glicero-3-phoshocholine (DOPC) phospholipid and stabilised by the electrostatic adsorption of κ-carrageenan. The produced homotaurine-loaded and unloaded liposomes had a highly negative electrokinetic potential and remarkable stability in phosphate buffer (pH 4 and 7.4). For the first time, the appearance and evolution of the aggregation of Aβ were presented through the variation in the standard percentile readings (D10, D50, and D90) obtained from the particle size distribution analysis. The kinetic experiments indicated the appearance of the first aggregates almost 30 min after mixing the liposomes and peptide solution. It was observed that by adding unloaded liposomes, the size of 90% of the particles in the dispersion (D90) increased. In contrast, the addition of homotaurine-loaded liposomes had almost minimal impact on the size of the fractions of larger particles during the kinetic experiments. Despite the specific bioactivity of homotaurine in the presence of natural cell membranes, this study reported an additional inhibitory effect of the compound on the amyloid peptide aggregation due to the charge effects and \'molecular crowding\'.
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  • 文章类型: Journal Article
    过渡金属催化有助于新方法的发现和天然产物的制备,以及增加药物发现计划中化学空间的新机会。在海洋药物的情况下,这一策略被用来实现选择性,可持续和有效的转型,否则无法获得。从这个角度来看,我们的目标是展示在过去几年中,各种过渡金属如何在各种类似海洋药物的支架中提供了富有成效的连接,通过加速这些有价值的分子的生产。
    Transition metal catalysis has contributed to the discovery of novel methodologies and the preparation of natural products, as well as new chances to increase the chemical space in drug discovery programs. In the case of marine drugs, this strategy has been used to achieve selective, sustainable and efficient transformations, which cannot be obtained otherwise. In this perspective, we aim to showcase how a variety of transition metals have provided fruitful couplings in a wide variety of marine drug-like scaffolds over the past few years, by accelerating the production of these valuable molecules.
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  • 文章类型: Journal Article
    抗癌肽是短且结构异质的氨基酸链,主要针对肿瘤细胞显示选择性细胞毒性,但不是健康的细胞,基于它们不同的细胞表面特性。它们的抗肿瘤活性是通过干扰细胞内稳态来进行的,如浆膜的完整性,细胞周期控制,酶活性和线粒体功能,最终充当血管生成-,耐药和转移抑制剂,免疫刺激剂,分化诱导剂和坏死或外在/内在凋亡启动子。海洋环境的生物多样性水平不断提高,就生物医学感兴趣的天然产物而言,海洋和海洋是开采不足的地雷。适应极端和竞争性环境条件的过程导致海洋物种产生独特的代谢物,作为一种化学策略,允许个体间的信号传递并确保抵抗捕食者的生存,传染剂或紫外线辐射。这些天然代谢物已广泛用于医疗保健管理的各种应用中,由于它们的抗癌作用,抗血管生成,抗炎和再生能力。这篇综述的目的是选择一些研究,这些研究报告了海洋动物衍生肽的分离及其在癌细胞体外培养物中的抗癌活性的鉴定,并根据源生物的分类等级列出它们。
    Anticancer peptides are short and structurally heterogeneous aminoacidic chains, which display selective cytotoxicity mostly against tumor cells, but not healthy cells, based on their different cell surface properties. Their anti-tumoral activity is carried out through interference with intracellular homeostasis, such as plasmalemma integrity, cell cycle control, enzymatic activities and mitochondrial functions, ultimately acting as angiogenesis-, drug resistance- and metastasis-inhibiting agents, immune stimulators, differentiation inducers and necrosis or extrinsic/intrinsic apoptosis promoters. The marine environment features an ever-growing level of biodiversity, and seas and oceans are poorly exploited mines in terms of natural products of biomedical interest. Adaptation processes to extreme and competitive environmental conditions led marine species to produce unique metabolites as a chemical strategy to allow inter-individual signalization and ensure survival against predators, infectious agents or UV radiation. These natural metabolites have found broad use in various applications in healthcare management, due to their anticancer, anti-angiogenic, anti-inflammatory and regeneration abilities. The aim of this review is to pick selected studies that report on the isolation of marine animal-derived peptides and the identification of their anticancer activity in in vitro cultures of cancer cells, and list them with respect to the taxonomical hierarchy of the source organism.
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  • 文章类型: Journal Article
    炎症是机体对病原体等有害刺激的防御机制,受损细胞,有毒化合物或辐射。然而,慢性炎症在多种疾病的发病机制中起着重要作用。目前有多种抗炎药可用于治疗炎症,但都表现出较少的功效。这推动了对专注于自然资源的新型抗炎化合物的寻找。海洋生物产生具有抗炎活性的广谱生物活性化合物。几种被认为是开发成药物的先导化合物。已经从藻类中提取了抗炎化合物,珊瑚,海藻和其他海洋生物。我们以前回顾了抗炎化合物,以及从海参等棘皮动物中分离出的粗提物,海胆和海星.在本次审查中,我们评估了其他海洋生物化合物的抗炎作用,包括大型藻类(海藻),海洋被子植物(海草),水母(水母),苔藓动物(苔藓动物),软体动物(贝类)和花生虫。我们还对这些化合物的抗炎活性的分子机制进行了综述。我们在这篇综述中的目的是概述海洋来源的抗炎化合物的研究现状以及将其转化为新型抗炎药物的前景。
    Inflammation is a defense mechanism of the body in response to harmful stimuli such as pathogens, damaged cells, toxic compounds or radiation. However, chronic inflammation plays an important role in the pathogenesis of a variety of diseases. Multiple anti-inflammatory drugs are currently available for the treatment of inflammation, but all exhibit less efficacy. This drives the search for new anti-inflammatory compounds focusing on natural resources. Marine organisms produce a broad spectrum of bioactive compounds with anti-inflammatory activities. Several are considered as lead compounds for development into drugs. Anti-inflammatory compounds have been extracted from algae, corals, seaweeds and other marine organisms. We previously reviewed anti-inflammatory compounds, as well as crude extracts isolated from echinoderms such as sea cucumbers, sea urchins and starfish. In the present review, we evaluate the anti-inflammatory effects of compounds from other marine organisms, including macroalgae (seaweeds), marine angiosperms (seagrasses), medusozoa (jellyfish), bryozoans (moss animals), mollusks (shellfish) and peanut worms. We also present a review of the molecular mechanisms of the anti-inflammatory activity of these compounds. Our objective in this review is to provide an overview of the current state of research on anti-inflammatory compounds from marine sources and the prospects for their translation into novel anti-inflammatory drugs.
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  • 文章类型: Journal Article
    海洋生物多样性已成为来自不同海洋生物的生物活性化合物和次生代谢物的非常有希望的资源。海绵的次生代谢产物表现出多种生物活性和潜在的药理特性。这篇系统的文献综述侧重于海洋海绵体外抗氧化潜力方面取得的进展。审查是根据PRISMA指南进行的。分析的主要纳入标准是鉴定出具有体外抗氧化活性的萜类化合物的文章。在三个不同的数据库中搜索,两百篇文章被选中。筛选摘要后,标题和手稿资格评估包括14篇文章。检测抗氧化活性的最多的分析是清除活性2,2-二苯基-1-吡啶酰肼(DPPH)和细胞内活性氧(ROS)的测量。有可能在体外鉴定出17种具有明显抗氧化活性的萜类化合物。GRADE分析获得了本综述中包含的研究的科学证据。萜烯在生态方面发挥着重要作用,此外,这些分子具有药物和工业应用。
    Marine biodiversity has emerged as a very promising resource of bioactive compounds and secondary metabolites from different sea organisms. The sponge\'s secondary metabolites demonstrated various bioactivities and potential pharmacological properties. This systematic review of the literature focuses on the advances achieved in the antioxidant potential of marine sponges in vitro. The review was performed in accordance with PRISMA guidelines. The main inclusion criterion for analysis was articles with identification of compounds from terpene classes that demonstrate antioxidant activity in vitro. Searching in three different databases, two hundred articles were selected. After screening abstracts, titles and evaluating for eligibility of manuscripts 14 articles were included. The most performed analyzes to detect antioxidant activity were scavenging activity 2,2-diphenyl-1-picrylhydrazyl (DPPH) and measurement of intracellular reactive oxygen species (ROS). It was possible to identify 17 compounds of the terpene class with pronounced antioxidant activity in vitro. Scientific evidence of the studies included in this review was accessed by the GRADE analysis. Terpenes play an important ecological role, moreover these molecules have a pharmaceutical and industrial application.
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  • 文章类型: Journal Article
    从这个角度来看,我们展示了连续流化学和光化学的好处,以及这些有价值的工具如何从海洋环境中合成有机支架。这些技术不仅促进了先前描述的合成途径,而且在制备具有显着的药理特性的新型有机分子方面也开辟了新的机会,可用于药物发现计划。
    In this perspective, we showcase the benefits of continuous flow chemistry and photochemistry and how these valuable tools have contributed to the synthesis of organic scaffolds from the marine environment. These technologies have not only facilitated previously described synthetic pathways, but also opened new opportunities in the preparation of novel organic molecules with remarkable pharmacological properties which can be used in drug discovery programs.
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  • 文章类型: Journal Article
    来自海洋微生物的天然产物作为用于药物发现的新化合物实体的潜在资源受到了极大的关注。独特的海洋环境为我们带来了一大批具有抗肿瘤等丰富生物功能的含硫天然产物,抗生素,抗炎和抗病毒活性。我们回顾了从海洋微生物中分离出的所有484种含硫天然产物(非硫酸化),其中59.9%是硫醚,29.8%是含噻唑/噻唑啉的化合物,10.3%是亚砜,砜,硫酯和许多其他。进一步讨论了133个化合物的构效关系,行动机制,生物合成,和可吸毒性。这是自1987年1月以来对海洋微生物含硫天然产物进行的第一次系统综述,至2020年12月。
    在线版本包含补充材料,可在10.1007/s42995-021-00101-2获得。
    Natural products derived from marine microorganisms have received great attention as a potential resource of new compound entities for drug discovery. The unique marine environment brings us a large group of sulfur-containing natural products with abundant biological functionality including antitumor, antibiotic, anti-inflammatory and antiviral activities. We reviewed all the 484 sulfur-containing natural products (non-sulfated) isolated from marine microorganisms, of which 59.9% are thioethers, 29.8% are thiazole/thiazoline-containing compounds and 10.3% are sulfoxides, sulfones, thioesters and many others. A selection of 133 compounds was further discussed on their structure-activity relationships, mechanisms of action, biosynthesis, and druggability. This is the first systematic review on sulfur-containing natural products from marine microorganisms conducted from January 1987, when the first one was reported, to December 2020.
    UNASSIGNED: The online version contains supplementary material available at 10.1007/s42995-021-00101-2.
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  • 文章类型: Editorial
    暂无摘要。
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  • 文章类型: Journal Article
    由新型严重急性呼吸道综合征冠状病毒2(SARS-CoV-2)引起的COVID-19,迅速传播到世界各地,构成全球健康问题。持续的流行使得有必要为感染SARS-CoV-2的患者开发新的药物和潜在的疗法。疫苗接种和药物开发的进展,没有预防性疫苗接种,迄今为止,已经开发了针对SARS-CoV-2感染的可行疗法。因此,需要进行更多的研究,以找到解决这一毁灭性状况的长期解决方案。正在进行临床研究以确定从海洋物种起始材料回收或合成的生物活性化合物的功效。本研究的重点是海洋来源的植物化学物质的抗SARS-CoV-2潜力,已经在计算机上进行了研究,在体外,和体内模型来确定它们的有效性。海洋生物活性物质,如类黄酮,单宁,生物碱,萜类化合物,肽,凝集素,多糖,和脂质,可以影响SARS-CoV-2在病毒颗粒的渗透和进入细胞,病毒核酸的复制,和病毒体从细胞中释放;它们还可以作用于宿主的细胞靶标。COVID-19已被证明对海洋资源产生的几种污染物具有抗性。本文对作为海洋药物的各种海洋资源及其治疗SARS-CoV-2的潜力进行了概述和总结。我们讨论了许多天然化合物作为从天然来源产生的海洋药物,用于治疗COVID-19和控制当前的大流行情景。
    COVID-19, which is caused by the novel severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has quickly spread over the world, posing a global health concern. The ongoing epidemic has necessitated the development of novel drugs and potential therapies for patients infected with SARS-CoV-2. Advances in vaccination and medication development, no preventative vaccinations, or viable therapeutics against SARS-CoV-2 infection have been developed to date. As a result, additional research is needed in order to find a long-term solution to this devastating condition. Clinical studies are being conducted to determine the efficacy of bioactive compounds retrieved or synthesized from marine species starting material. The present study focuses on the anti-SARS-CoV-2 potential of marine-derived phytochemicals, which has been investigated utilizing in in silico, in vitro, and in vivo models to determine their effectiveness. Marine-derived biologically active substances, such as flavonoids, tannins, alkaloids, terpenoids, peptides, lectins, polysaccharides, and lipids, can affect SARS-CoV-2 during the viral particle\'s penetration and entry into the cell, replication of the viral nucleic acid, and virion release from the cell; they can also act on the host\'s cellular targets. COVID-19 has been proven to be resistant to several contaminants produced from marine resources. This paper gives an overview and summary of the various marine resources as marine drugs and their potential for treating SARS-CoV-2. We discussed at numerous natural compounds as marine drugs generated from natural sources for treating COVID-19 and controlling the current pandemic scenario.
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  • 文章类型: Journal Article
    In the last decades Blue Growth policy in european and non-european countries produced a great impulse in applied marine sciences, comprehending the research of new bioactive molecules in marine organisms. These organisms are a great source of natural compounds with unique features resulting from the huge variability of marine habitats and species living in them. Most of the marine compounds in use and in clinical trials are drugs for cancer therapy and many of them are conjugated to antibody to form antibody-drug conjugates (ADCs). Severe pain, viral infections, hypertriglyceridemia, obesity, Alzheimer\'s and other CNS diseases are further target conditions for these pharmaceuticals. This review summarizes the state-of-the-art marine drugs focusing on the most successful results in the fast expanding field of marine pharmacology.
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