Cinnamates

肉桂酸盐
  • 文章类型: Journal Article
    鉴于人们越来越关注紫外线(UV)辐射引起的皮肤损伤,对紫外线过滤剂的需求有所增加。目前,UV过滤剂被认为是新兴的污染物。UV过滤剂的广泛生产和使用已导致其广泛释放到水生环境中。因此,人们越来越担心紫外线过滤剂可能在环境中生物积累并表现出持久的特性,提出了一些安全健康问题。甲氧基肉桂酸辛酯(OMC)在化妆品工业中广泛用作UV-B过滤剂。虽然最初设计是为了减轻紫外线辐射的不利光生物效应,OMC的安全性受到质疑,一些研究报告对环境有毒性作用。这篇评论的目的是提供有关最广泛使用的有机紫外线过滤剂(OMC)的科学信息的概述,及其对生物多样性和水生环境的影响。
    Given the increasing concern surrounding ultraviolet (UV) radiation-induced skin damage, there has been a rise in demand for UV filters. Currently, UV-filters are considered emerging contaminants. The extensive production and use of UV filters have led to their widespread release into the aquatic environment. Thus, there is growing concern that UV filters may bioaccumulate and exhibit persistent properties within the environment, raising several safety health concerns. Octyl-methoxycinnamate (OMC) is extensively employed as a UV-B filter in the cosmetic industry. While initially designed to mitigate the adverse photobiological effects attributed to UV radiation, the safety of OMC has been questioned with some studies reporting toxic effects on environment. The aim of this review to provide an overview of the scientific information regarding the most widely used organic UV-filter (OMC), and its effects on biodiversity and aquatic environment.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

  • 文章类型: Journal Article
    用于治疗各种疾病的传统疗法越来越受欢迎。传统上,最有价值的治疗草药之一是PicrorhizakurroaRoyleexBenth。传统和民间使用的P.kurroa包括慢性便秘,皮肤相关问题,灼烧感,慢性复发发热,黄疸,心脏问题,呼吸,消化,过敏,结核病,与血液有关的问题,糖尿病前期和肥胖,泻药,霍乱,和肝脏刺激。植物成分,如糖苷,生物碱,葫芦素,环烯醚萜类,酚类物质,和萜烯在P.kurroa显示有希望的药理潜力。为了发现可以治愈慢性病的新化合物,比如心血管,糖尿病,癌症,呼吸,和肝脏保护疾病,对P.kurroa的筛查是必不可少的。本研究综合评价了民族药效,植物化学,药理活性,剂量,和P.kurroa的毒性。这篇综述为未来的研究和治疗应用提供了对这种传统药物的全面见解。这篇综述文章的目的是确定P.kurroa对多种疾病的药理作用。P.kurroa可能是根除新发展的疾病的标准治疗的天然替代品。这项研究旨在作为未来基础和临床研究的资源。
    Traditional remedies for the treatment of various ailments are gaining popularity. Traditionally, one of the most valuable therapeutic herbs has been Picrorhiza kurroa Royle ex Benth. Traditional and folk uses of P. kurroa include chronic constipation, skin-related problems, burning sensation, chronic reoccurring fever, jaundice, heart problems, breathing, digestion, allergy, tuberculosis, blood-related problems, prediabetes and obesity, laxative, cholagogue, and liver stimulatory. Phytoconstituents such as glycosides, alkaloids, cucurbitacins, iridoids, phenolics, and terpenes in P. kurroa have shown promising pharmacological potential. In order to uncover novel compounds that may cure chronic illnesses, such as cardiovascular, diabetes, cancer, respiratory, and hepatoprotective diseases, the screening of P. kurroa is essential. This study comprehensively evaluated the ethnopharmacological efficacy, phytochemistry, pharmacological activity, dose, and toxicity of P. kurroa. This review provides comprehensive insights into this traditional medication for future research and therapeutic application. The purpose of this review article was to determine the pharmacological effects of P. kurroa on a variety of disorders. P. kurroa may be a natural alternative to the standard treatment for eradicating newly evolving diseases. This study is intended as a resource for future fundamental and clinical investigations.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

  • 文章类型: Journal Article
    天然产物一般可以表现出多种生物活性,但大多数在初步活动评估中表现平平。天然产物通常需要结构修饰才能获得有前途的先导化合物。肉桂酸(CA)易于获得,具有多种生物活性和低细胞毒性。将CA引入天然产品可能会提高其性能,增强生物活性,减少毒副作用。在这里,本文旨在探讨CA在天然产物结构修饰中的相关应用,为未来天然产物的衍生化和药物开发提供理论依据。已发表的文章,Web数据库(PubMed,科学直接,SCIFinder,和CNKI),和临床试验网站(https://clinicaltrials.gov/)相关的天然产品和CA衍生物被包括在讨论中。根据纳入标准,本文选择并讨论了128项研究。筛选CA衍生物的天然产物,可根据其生物活性进行分类。全文是根据衍生物的生物活性,具有以下类别:抗肿瘤,神经保护,抗糖尿病,抗微生物,抗寄生虫,抗氧化,抗炎,和其他活动。详细讨论了每种CA衍生物的生物活性。值得注意的是,与先导化合物相比,大多数衍生物表现出增强的生物活性和降低的细胞毒性。CA具有各种优点,可广泛用于天然产物衍生物的合成,以增强候选药物或先导化合物的性质。
    Natural products can generally exhibit a variety of biological activities, but most show mediocre performance in preliminary activity evaluation. Natural products often require structural modification to obtain promising lead compounds. Cinnamic acid (CA) is readily available and has diverse biological activities and low cytotoxicity. Introducing CA into natural products may improve their performance, enhance biological activity, and reduce toxic side effect. Herein, we aimed to discuss related applications of CA in the structural modification of natural products and provide a theoretical basis for future derivatization and drug development of natural products. Published articles, web databases (PubMed, Science Direct, SCI Finder, and CNKI), and clinical trial websites (https://clinicaltrials.gov/) related to natural products and CA derivatives were included in the discussion. Based on the inclusion criteria, 128 studies were selected and discussed herein. Screening natural products of CA derivatives allowed for classification by their biological activities. The full text is organized according to the biological activities of the derivatives, with the following categories: anti-tumor, neuroprotective, anti-diabetic, anti-microbial, anti-parasitic, anti-oxidative, anti-inflammatory, and other activities. The biological activity of each CA derivative is discussed in detail. Notably, most derivatives exhibited enhanced biological activity and reduced cytotoxicity compared with the lead compound. CA has various advantages and can be widely used in the synthesis of natural product derivatives to enhance the properties of drug candidates or lead compounds.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

  • 文章类型: Journal Article
    抑郁症和焦虑症是最普遍的神经精神疾病,已成为全球健康问题。抗焦虑和抗抑郁药,例如苯二氮卓类药物,选择性5-羟色胺再摄取抑制剂,单胺氧化酶抑制剂,和三环,是治疗焦虑和抑郁的第一线。虽然这些药物缺乏疗效,有延迟的反应时间和许多副作用,他们的广泛滥用和市场持续增长。随着时间的推移,使用天然和植物化学物质作为化学药物替代疗法的传统习俗已经出现,以治疗许多病理状况,包括焦虑和抑郁.最近的临床前研究表明,酚类化合物,迷迭香酸,对几种神经精神疾病有效,包括焦虑和抑郁.此外,迷迭香酸表现出多种药理作用,比如心脏保护,保肝,肺保护,抗氧化剂,抗炎,和神经保护作用。然而,迷迭香酸治疗神经系统相关疾病的潜力,比如焦虑和抑郁,较少或尚未审查。因此,这篇综述的目的是介绍一些临床前和临床研究,当可用时,从不同的数据库调查迷迭香酸对焦虑和抑郁的影响。这些研究表明迷迭香酸通过其强大的抗氧化和抗炎特性对焦虑和抑郁产生有利的作用。本文将研究和讨论迷迭香酸的抗焦虑和抗抑郁作用可能与其有效的抗氧化和抗炎活性有关的可能性。
    Depression and anxiety are the most prevalent neuropsychiatric disorders that have emerged as global health concerns. Anxiolytic and antidepressant drugs, such as benzodiazepines, selective serotonin reuptake inhibitors, monoamine oxidase inhibitors, and tricyclics, are the first line used in treating anxiety and depression. Although these drugs lack efficacy and have a delayed response time and numerous side effects, their widespread abuse and market continue to grow. Over time, traditional practices using natural and phytochemicals as alternative therapies to chemical drugs have emerged to treat many pathological conditions, including anxiety and depression. Recent preclinical studies have demonstrated that the phenolic compound, rosmarinic acid, is effective against several neuropsychiatric disorders, including anxiety and depression. In addition, rosmarinic acid showed various pharmacological effects, such as cardioprotective, hepatoprotective, lung protective, antioxidant, anti-inflammatory, and neuroprotective effects. However, the potentialities of the use of rosmarinic acid in the treatment of nervous system-related disorders, such as anxiety and depression, are less or not yet reviewed. Therefore, the purpose of this review was to present several preclinical and clinical studies, when available, from different databases investigating the effects of rosmarinic acid on anxiety and depression. These studies showed that rosmarinic acid produces advantageous effects on anxiety and depression through its powerful antioxidant and anti-inflammatory properties. This review will examine and discuss the possibility that the anxiolytic and anti-depressive effects of rosmarinic acid could be associated with its potent antioxidant and anti-inflammatory activities.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

  • 文章类型: Journal Article
    暂无摘要。
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

  • 文章类型: Clinical Trial, Phase I
    血小板减少症和慢性肝病患者由于血小板计数低,在侵入性手术期间出血的风险增加。Lusutrombopag,一种口服活性血小板生成素受体激动剂,在接受有计划的侵入性手术的血小板减少的慢性肝病患者中,血小板计数增加,血小板输注需要减少。lusutrombopag在Child-PughC级慢性肝病患者中的安全性尚不清楚。进行本分析以确定药代动力学,功效,和lusutrombopag在Child-PughC级慢性肝病患者中的安全性。
    Child-PughC级慢性肝病患者的数据来自三个数据集:1/2Child-PughC级研究(n=5)(JapicCTI-163289[日本制药信息中心]),第3阶段关键研究(L-PLUS2,n=3)(NCT02389621[Clinicaltrials.gov]),和正在进行的上市后监测(n=27)(JapicCTI-163432[日本医药信息中心])。患者接受3mg的卢舒曲波帕格治疗长达7天。从两项临床研究和上市后监测收集安全性和有效性评估;从1/2期研究收集药代动力学数据。
    Child-PughC级患者的平均Cmax和AUC0-τ低于Child-PughA级和B级;个别患者的Cmax和AUC0-τ值在Child-Pugh类别中重叠。在未接受血小板输注的lusutrombopag患者中(1/2期n=4,3期n=1,上市后监测n=24),最大血小板计数中位数(范围)为88.5×109/L(54-105×109/L),80×109/L,91×109/L(41-186×109/L;n=23),分别。没有治疗相关的不良事件或治疗相关的严重不良事件。1/2期研究的一名患者患有非严重门静脉血栓形成,这不被认为是治疗相关的。
    这项研究中提出的分析表明,lusutrombopag增加Child-PughC级患者的血小板计数,并且在该患者人群中是安全且耐受性良好的。
    L-PLUS2:NCT02389621(Clinicaltrials.gov)。阶段1/2:JapicCTI-163289(日本医药信息中心[JAPIC])。上市后监测:JapicCTI-163432(JAPIC)。
    Patients with thrombocytopenia and chronic liver disease are at increased risk of bleeding during invasive procedures due to low platelet counts. Lusutrombopag, an orally active thrombopoietin receptor agonist, increases platelet count and reduces the need for platelet transfusion in chronic liver disease patients with thrombocytopenia undergoing a planned invasive procedure. The safety of lusutrombopag in patients with Child-Pugh class C chronic liver disease is not known. The present analysis was performed to determine the pharmacokinetics, efficacy, and safety of lusutrombopag in patients with Child-Pugh class C chronic liver disease.
    Data for patients with Child-Pugh class C chronic liver disease were collected from three data sets: a phase 1/2 Child-Pugh class C study (n = 5) (JapicCTI-163289 [Japan Pharmaceutical Information Center]), a phase 3 pivotal study (L-PLUS 2, n = 3) (NCT02389621 [Clinicaltrials.gov]), and ongoing post-marketing surveillance (n = 27) (JapicCTI-163432 [Japan Pharmaceutical Information Center]). Patients received lusutrombopag at 3 mg for up to 7 days. Safety and efficacy assessments were collected from two clinical studies and the post-marketing surveillance; pharmacokinetic data were collected from the phase 1/2 study.
    Mean Cmax and AUC0-τ were lower in Child-Pugh class C patients than Child-Pugh class A and B; individual patients\' Cmax and AUC0-τ values overlapped among Child-Pugh classes. In lusutrombopag patients who did not receive platelet transfusion (n = 4 in phase 1/2, n = 1 in phase 3, n = 24 in post-marketing surveillance), the median (range) maximum platelet count was 88.5 × 109/L (54-105 × 109/L), 80 × 109/L, and 91 × 109/L (41-186 × 109/L; n = 23), respectively. There were no treatment-related adverse events or treatment-related serious adverse events. One patient from the phase 1/2 study had a non-serious portal vein thrombosis, which was not considered treatment-related.
    The analysis presented in this study suggests that lusutrombopag increases platelet counts in Child-Pugh class C patients and is safe and well tolerated in this patient population.
    L-PLUS 2: NCT02389621 (Clinicaltrials.gov). Phase 1/2: JapicCTI-163289 (Japan Pharmaceutical Information Center [JAPIC]). Post-marketing surveillance: JapicCTI-163432 (JAPIC).
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

  • 文章类型: Journal Article
    Lusutrombopag是一种口服血小板生成素受体激动剂(TPO-RA)。临床试验表明,卢舒曲泊帕可减少慢性肝病(CLD)和严重血小板减少症患者术前血小板输注的需要。该分析评估了lusutrombopag在接受计划侵入性手术的严重血小板减少症和CLD患者中的疗效和安全性。
    电子数据库搜索(到2020年12月1日)确定了三个随机的,安慰剂对照,在CLD和血小板计数低于50×109/L的患者中比较lusutrombopag和安慰剂的双盲临床试验计划接受围手术期出血风险的手术。随机效应荟萃分析检查了治疗效果,使用CochraneCollaboration的工具评估偏差风险。
    荟萃分析包括343(lusutrombopag3mg,n=173;安慰剂,n=170)患者。更多的患者符合治疗反应标准(血小板计数至少50×109/L,在研究期间任何时间从基线增加至少20×109/L)与安慰剂(风险比[RR]6.39;95%置信区间[CI]3.69,11.07;p<0.0001)。主要疗效结果,术后至少7天不需要血小板输注和出血抢救治疗的患者比例,lusutrombopag治疗的患者多于安慰剂治疗的患者(RR3.42;95%CI1.86,6.26;p=0.0001)。与安慰剂组相比,lusutrombopag组发生任何出血事件的风险显著降低(RR0.55;95%CI0.32,0.95;p=0.03);相反,lusutrombopag和安慰剂组的血栓形成事件发生率相似(RR0.79;95%CI0.19,3.24;p=0.74).
    这项荟萃分析显示,在计划的侵入性手术之前,用lusutrombopag治疗CLD患者的严重血小板减少症在增加血小板计数方面是有效且安全的。避免血小板输注的需要,降低出血风险,从而提高了支持lusutrombopag疗效和安全性的证据的确定性。
    Lusutrombopag is an oral thrombopoietin receptor agonist (TPO-RA). Clinical trials have shown lusutrombopag\'s efficacy in reducing need for preoperative platelet transfusion in patients with chronic liver disease (CLD) and severe thrombocytopenia. This analysis assessed efficacy and safety of lusutrombopag in patients with severe thrombocytopenia and CLD undergoing planned invasive procedures.
    An electronic database search (through 1 December 2020) identified three randomised, placebo-controlled, double-blind clinical trials comparing lusutrombopag with placebo in patients with CLD and platelet count below 50 × 109/L scheduled to undergo a procedure with a perioperative bleeding risk. A random-effects meta-analysis examined treatment effect, with Cochrane Collaboration\'s tool assessing risk of bias.
    The meta-analysis included 343 (lusutrombopag 3 mg, n = 173; placebo, n = 170) patients. More patients met the criteria for treatment response (platelet count at least 50 × 109/L and increase of at least 20 × 109/L from baseline anytime during the study) with lusutrombopag versus placebo (risk ratio [RR] 6.39; 95% confidence interval [CI] 3.69, 11.07; p < 0.0001). The primary efficacy outcome, proportion of patients requiring no platelet transfusion and no rescue therapy for bleeding for at least 7 days post procedure, was achieved by more patients treated with lusutrombopag versus placebo (RR 3.42; 95% CI 1.86, 6.26; p = 0.0001). The risk of any bleeding event was significantly lower with lusutrombopag compared to placebo (RR 0.55; 95% CI 0.32, 0.95; p = 0.03); conversely, thrombosis event rates were similar between lusutrombopag and placebo (RR 0.79; 95% CI 0.19, 3.24; p = 0.74).
    This meta-analysis showed that treatment of severe thrombocytopenia with lusutrombopag in patients with CLD prior to a planned invasive procedure was efficacious and safe in increasing platelet counts, avoiding the need for platelet transfusions, and reducing risk of bleeding, thereby enhancing the certainty of evidence supporting the efficacy and safety of lusutrombopag.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

  • 文章类型: Journal Article
    多酚酸是几乎每种草药植物中广泛存在的天然产物,其中迷迭香酸(RA,C18H16O8)是众所周知的,并存在于许多科的160多个物种中,尤其是唇形科.除了这种草药成分,其数十种天然衍生物也已从许多天然植物中分离和表征。近年来,随着人们越来越关注天然产品作为替代疗法,已经进行了大量的药理学研究来证明RA的各种生物活性,例如抗炎,抗氧化,抗糖尿病,抗病毒,抗肿瘤,神经保护,肝脏保护,等。此外,关于其生物合成的调查,提取,分析,临床应用,和药代动力学也已经进行。尽管在各个研究方面取得了许多成果,仍然存在一些需要回答的问题或问题,尤其是它的毒性和生物利用度。因此,我们希望在天然产品的情况下,本综述不仅可以提供对RA的全面了解,涵盖其各种研究领域,但也强调了一些值得以后研究的当前问题和未来前景,为了帮助我们更有效地利用这种多酚酸,广泛地,和安全。
    Polyphenolic acids are the widely occurring natural products in almost each herbal plant, among which rosmarinic acid (RA, C18H16O8) is well-known, and is present in over 160 species belonging to many families, especially the Lamiaceae. Aside from this herbal ingredient, dozens of its natural derivatives have also been isolated and characterized from many natural plants. In recent years, with the increasing focus on the natural products as alternative treatments, a large number of pharmacological studies have been carried out to demonstrate the various biological activities of RA such as anti-inflammation, anti-oxidation, anti-diabetes, anti-virus, anti-tumor, neuroprotection, hepatoprotection, etc. In addition, investigations concerning its biosynthesis, extraction, analysis, clinical applications, and pharmacokinetics have also been performed. Although many achievements have been made in various research aspects, there still exist some problems or issues to be answered, especially its toxicity and bioavailability. Thus, we hope that in the case of natural products, the present review can not only provide a comprehensive understanding on RA covering its miscellaneous research fields, but also highlight some of the present issues and future perspectives worth investigating later, in order to help us utilize this polyphenolic acid more efficiently, widely, and safely.
    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
    癌症,作为一种持久而戏剧性的疾病,影响全球近三分之一的人类。化疗药物在肿瘤治疗中发挥着重要作用,但是多药耐药和严重的不良反应已经成为肿瘤化疗失败的主要原因。因此,迫切需要开发新的化学疗法。肉桂酸含有一种普遍存在的α,β-不饱和酸部分在癌症治疗中表现出潜在的治疗效果,因为这些衍生物可以通过多种作用机制作用于癌细胞。因此,肉桂酸衍生物是发现新型抗癌剂的关键支架。这篇综述提供了肉桂酸杂种作为抗癌剂的全面概述。结构-活动关系,以及行动机制,还讨论了,涵盖2012年至2021年发表的文章。
    Cancer, as a long-lasting and dramatic disease, affects almost one-third of human beings globally. Chemotherapeutics play an important role in cancer treatment, but multidrug resistance and severe adverse effects have already become the main causes of failure in tumor chemotherapy. Therefore, it is an urgent need to develop novel chemotherapeutics. Cinnamic acid contains a ubiquitous α,β-unsaturated acid moiety presenting potential therapeutic effects in the treatment of cancer as these derivatives could act on cancer cells by diverse mechanisms of action. Accordingly, cinnamic acid derivatives are critical scaffolds in discovering novel anticancer agents. This review provides a comprehensive overview of cinnamic acid hybrids as anticancer agents. The structure-activity relationship, as well as the mechanisms of action, are also discussed, covering articles published from 2012 to 2021.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

  • 文章类型: Journal Article
    Phenolic acids comprise a class of phytochemical compounds that can be extracted from various plant sources and are well known for their antioxidant and anti-inflammatory properties. A few of the most common naturally occurring phenolic acids (i.e., caffeic, carnosic, ferulic, gallic, p-coumaric, rosmarinic, vanillic) have been identified as ingredients of edible botanicals (thyme, oregano, rosemary, sage, mint, etc.). Over the last decade, clinical research has focused on a number of in vitro (in human cells) and in vivo (animal) studies aimed at exploring the health protective effects of phenolic acids against the most severe human diseases. In this review paper, the authors first report on the main structural features of phenolic acids, their most important natural sources and their extraction techniques. Subsequently, the main target of this analysis is to provide an overview of the most recent clinical studies on phenolic acids that investigate their health effects against a range of severe pathologic conditions (e.g., cancer, cardiovascular diseases, hepatotoxicity, neurotoxicity, and viral infections-including coronaviruses-based ones).
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

公众号