pharmacological actions

药理作用
  • 文章类型: Journal Article
    在过去的几个世纪里,草药成分一直是科学兴趣的主题,对其治疗潜力的最新研究正在进行中。金雀异黄素是一种大豆异黄酮,在大豆中大量存在,以及豆科植物。科学研究已经证明了金雀异黄素对各种健康状况的有益作用。金雀异黄素具有广泛的药理活性,包括抗癌,神经保护,心脏保护,抗溃疡,抗糖尿病,伤口愈合,抗菌,抗病毒,皮肤,和辐射防护作用。然而,金雀异黄素的疏水性导致吸收受限并限制了其治疗潜力。在这次审查中,已经探索了用于金雀异黄素递送的纳米载体的数量,如聚合物纳米颗粒,纳米结构脂质载体,固体脂质纳米粒,脂质体,胶束,转移体,纳米乳液和纳米纤维。这些金雀异黄素的纳米制剂已被用作各种疾病的潜在策略,采用各种离体,在体外,体内模型和各种给药途径。这篇综述得出结论,金雀异黄素是治疗各种疾病的潜在治疗剂,包括癌症,神经退行性疾病,心血管疾病,肥胖,糖尿病,溃疡,等。,当在合适的纳米载体中配制时。
    Throughout the past several centuries, herbal constituents have been the subject of scientific interest and the latest research into their therapeutic potential is underway. Genistein is a soy-derived isoflavone found in huge amounts in soy, along with the plants of the Fabaceae family. Scientific studies have demonstrated the beneficial effects of genistein on various health conditions. Genistein presents a broad range of pharmacological activities, including anticancer, neuroprotective, cardioprotective, antiulcer, anti-diabetic, wound healing, anti-bacterial, antiviral, skin, and radioprotective effects. However, the hydrophobic nature of genistein results in constrained absorption and restricts its therapeutic potential. In this review, the number of nanocarriers for genistein delivery has been explored, such as polymeric nanoparticles, nanostructured lipid carriers, solid lipid nanoparticles, liposomes, micelles, transferosomes, and nanoemulsions and nanofibers. These nano-formulations of genistein have been utilized as a potential strategy for various disorders, employing a variety of ex vivo, in vitro, and in vivo models and various administration routes. This review concluded that genistein is a potential therapeutic agent for treating various diseases, including cancer, neurodegenerative disorders, cardiovascular disorders, obesity, diabetes, ulcers, etc., when formulated in suitable nanocarriers.
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  • 文章类型: Journal Article
    SCH23390是一种广泛使用的D1多巴胺受体(D1R)拮抗剂,也引起一些不依赖D1R的作用。我们之前发现苯并氮杂卓,SKF83959,SCH23390的类似物,产生Sigma-1受体(Sig1R)的正变构调节。SCH23390不结合Sig1R的邻位氧位点,但增强3H(+)-喷他佐辛与Sig1R的结合。在这项研究中,我们研究了SCH23390是否充当Sig1R的变构调节剂。我们在转染的HEK293T和SH-SY5Y细胞中检测到响应SCH23390的结合免疫球蛋白蛋白(BiP)和Sig1R易位到质膜的Sig1R解离增加,分别。通过以时间和剂量依赖性方式抑制GSK3β活性进一步证实了SCH23390对Sig1R的激活;这种作用被Sig1R拮抗剂预处理阻断,BD1047,并通过敲低Sig1R。SCH23390还在野生型小鼠中抑制GSK3β,但在Sig1R敲除小鼠中不抑制。最后,我们显示SCH23390变构调节Sig1R激动剂SKF10047对GSK3β的抑制作用。SCH23390的这种正变构效应通过促进SKF10047在用MPP+攻击的原代皮质神经元中提供的神经元保护而得到进一步证实。这些结果提供了SCH23390引发Sig1R的功能性变构调节的第一个证据。我们的发现不仅揭示了SCH23390的新药理作用,而且还表明了SCH23390介导的D1R非依赖性作用的潜在机制。因此,在解释对SCH23390的药理反应时,应注意这些Sig1R介导的作用。
    SCH23390 is a widely used D1 dopamine receptor (D1R) antagonist that also elicits some D1R-independent effects. We previously found that the benzazepine, SKF83959, an analog of SCH23390, produces positive allosteric modulation of the Sigma-1 receptor (Sig1R). SCH23390 does not bind to the orthodoxic site of Sig1R but enhances the binding of 3H (+)-pentazocine to Sig1R. In this study, we investigated whether SCH23390 functions as an allosteric modulator of Sig1R. We detected increased Sig1R dissociation from binding immunoglobulin protein (BiP) and translocation of Sig1R to the plasma membrane in response to SCH23390 in transfected HEK293T and SH-SY5Y cells, respectively. Activation of Sig1R by SCH23390 was further confirmed by inhibition of GSK3β activity in a time- and dose-dependent manner; this effect was blocked by pretreatment with the Sig1R antagonist, BD1047, and by knockdown of Sig1R. SCH23390 also inhibited GSK3β in wild-type mice but not in Sig1R knockout mice. Finally, we showed that SCH23390 allosterically modulated the effect of the Sig1R agonist SKF10047 on inhibition of GSK3β. This positive allosteric effect of SCH23390 was further confirmed via promotion of neuronal protection afforded by SKF10047 in primary cortical neurons challenged with MPP+. These results provide the first evidence that SCH23390 elicits functional allosteric modulation of Sig1R. Our findings not only reveal novel pharmacological effects of SCH23390 but also indicate a potential mechanism for SCH23390-mediated D1R-independent effects. Therefore, attention should be paid to these Sig1R-mediated effects when explaining pharmacological responses to SCH23390.
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  • 文章类型: Journal Article
    阿尔茨海默病是导致认知功能缺陷的神经退行性疾病之一。目前治疗阿尔茨海默病的药物很少,尽管研究人员花了大量时间研究这种情况并提供了许多好处。因此,只有少数药物可用于治疗阿尔茨海默病。黄酮是在许多植物和草药中发现的饮食成分,具有多种健康优势。在临床前试验中,黄酮对一系列脑部疾病表现出强大的保护作用,最常见的是阿尔茨海默病。黄酮,一种双类黄酮,分离后可以在各种草药中鉴定。考虑到这种化合物的有益性质,这篇综述强调了胺黄酮的药理作用和植物来源,以及该化合物的益处和在治疗阿尔茨海默氏症中的可能应用。
    Alzheimer\'s disease is one of the neurodegenerative diseases which causes cognition deficit. There are currently few medications available to treat Alzheimer\'s disease, even though researchers have devoted a great deal of time studying the condition and offering many benefits. Thus, only a few drugs are available for the treatment of Alzheimer\'s disease. Amentoflavone is a dietary component found in many plants and herbs that has several health advantages. Amentoflavone has demonstrated strong protective benefits against a range of brain illnesses in preclinical trials, most frequently in Alzheimer\'s disease. Amentoflavone, a biflavonoid, can be identified in a variety of herbs upon isolation. Considering the beneficial properties of this compound, this review emphasizes the pharmacological effects and botanical sources of amentoflavone, as well as the compound\'s benefits and possible applications in the treatment of Alzheimer\'s disorders.
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  • 文章类型: Journal Article
    Talinumtriangulare(Jacq.)威尔德。是部落社区使用的传统绿叶蔬菜,用于种族和民族烹饪。本文回顾了其多种用途的当前知识,包括药理活性和营养成分。文献调查表明,传统上它在治疗几种疾病方面是有用的,比如贫血,糖尿病,麻疹,溃疡和各种传统食物的制备。对其植物化学物质的文献分析显示其生物活性化合物的丰富度。Further,研究还表明,这种植物具有抗糖尿病作用,抗肥胖,抗肿瘤,抗溃疡,保肝,和神经保护活性,除了抗炎和抗氧化特性。植物的营养分析揭示了Ca的存在,Zn,Fe,维生素C和E,大量的膳食纤维和蛋白质。抗糖尿病的药理研究结果,抗溃疡和抗贫血活动为其种族医学用途提供了支持。生物活性化合物的存在和药理活性表明了该植物作为功能性食品的有用性。
    Talinum triangulare (Jacq.) Willd. is a traditional leafy vegetable used by tribal communities for ethnomedicinal and ethnoculinary preparations. This article reviews the current knowledge of its multiple uses, including pharmacological activities and nutritional composition. The literature survey shows that it has been traditionally useful in the treatment of several diseases, such as anaemia, diabetes, measles, and ulcers and the preparation of various traditional foods. Analysis of the literature on its phytochemicals shows its richness in bioactive compounds. Further, research also shows that this plant has antidiabetic, antiobesity, antitumor, antiulcer, hepatoprotective, and neuroprotective activities besides anti-inflammatory and antioxidant properties. Nutrient analysis of the plant reveals the presence of Ca, Zn, Fe, vitamins C and E, dietary fibre and protein in considerable quantities. The results of the pharmacological studies on the antidiabetic, antiulcer and anti-anaemic activities provide support in favour of its ethnomedicinal uses. The presence of bioactive compounds and pharmacological activities show the usefulness of this plant as a functional food.
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  • 文章类型: Journal Article
    牙医必须以符合科学文献和专业组织制定的指南的当前建议的方式使用本地递送的抗微生物剂(LDA)。考虑到对该主题的研究不足,目前尚不清楚在牙周实践中使用LDAs时采用何种策略。所以,这项研究的目的是调查牙科专业人员在不同的牙周实践中如何利用LDAs。
    这项横断面研究使用了封闭式问卷。牙科专业人员收到了八项问卷的电子副本。问卷评估了LDA的相关性,它们的使用频率,哪些是最常用的,接受它们的患者数量,他们对药理活性的理解,以及他们对当前治疗指南的了解。在提交给参与者之前,对问卷的有效性和可靠性进行了评估。使用社会科学统计软件包(SPSS),对输入进行了分析。
    总共120名牙科专业人员,平均年龄为34.7岁,回答了问卷。这些人中有一半没有使用LDA的历史。以不同形式使用的最常见的LDA是葡萄糖酸氯己定(CHX),其次是四环素。大多数参与者在少于10名患者中放置了LDAs(80%)。不到一半的人承认不同的LDA及其药理活性。甚至没有70%的临床医生是最新的欧洲牙周病联合会(EFP)指南。没有参与者低估LDAs在牙周护理中的重要性。
    牙科专业人员认为LDAs对牙周治疗至关重要。然而,他们缺乏一般知识,药理学,和临床方面。患者使用LDA的经验受到不适当的部署模式的限制。
    UNASSIGNED: Dentists must employ locally delivered antimicrobial agents (LDAs) in a way that is in line with current recommendations from the scientific literature and the guidelines set by professional organizations. Considering the dearth of research on this topic, it is not known what strategies are adapted when using LDAs in their periodontal practice. So, the purpose of this research was to investigate how LDAs are utilized by dental professionals in their distinct periodontal practices.
    UNASSIGNED: This cross-sectional study used a closed-ended questionnaire. Dental professionals received electronic copies of the eight-item questionnaire. The questionnaire assessed the relevance of LDAs, how frequently they are used, which ones are used most, the number of patients who receive them, their understanding of pharmacological activities, and their knowledge of current treatment guidelines. The questionnaire\'s validity and reliability were evaluated before being presented to participants. Using the Statistical Package for the Social Sciences (SPSS), the input was analyzed.
    UNASSIGNED: A total of 120 dental professionals, with an average age of 34.7 years, answered the questionnaire. Half of these individuals have no history of ever using LDAs. The most frequent LDA used in its different forms was chlorhexidine gluconate (CHX), followed by tetracycline. The majority of participants placed LDAs (80%) in less than 10 patients. Less than half acknowledged the different LDAs and their pharmacological activities. Not even 70% of clinicians were up-to-date on the current European Federation of Periodontology (EFP) guidelines. None of the participants discounted the significance of LDAs in periodontal care.
    UNASSIGNED: Dental professionals regard LDAs as essential to periodontal therapy. Yet, they lacked knowledge about general, pharmacological, and clinical aspects. The patient experience with LDAs was limited by an inappropriate deployment pattern.
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  • 文章类型: Journal Article
    纳豆是由纳豆细菌发酵的大豆制品。它富含多种氨基酸,维生素,蛋白质和活性酶。它具有多种生物活性,如溶栓,预防骨质疏松症,抗菌,抗癌,抗氧化剂等。它广泛用于医学,保健食品,生物催化等领域。纳豆富含多种药理活性物质,具有重要的药用研究价值。本文综述了纳豆在国内外的药理活性和应用,从而为纳豆的进一步研究和开发提供参考。
    Natto is a soybean product fermented by natto bacteria. It is rich in a variety of amino acids, vitamins, proteins and active enzymes. It has a number of biological activities, such as thrombolysis, prevention of osteoporosis, antibacterial, anticancer, antioxidant and so on. It is widely used in medicine, health-care food, biocatalysis and other fields. Natto is rich in many pharmacological active substances and has significant medicinal research value. This paper summarizes the pharmacological activities and applications of natto in and outside China, so as to provide references for further research and development of natto.
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  • 文章类型: Journal Article
    姜黄植物在古代医学中用于治疗各种疾病,包括咳嗽,糖尿病,和肝脏疾病。数据显示,姜黄的主要化学成分,姜黄素,对身体有多种有益作用。因此,有兴趣记录姜黄治疗活动的数据,包括它的提取物和可能的医疗用途,以及其口腔和牙科用途以及对这些用途的安全性评估。姜黄素,最纯净的姜黄,在牙科领域表现出了希望。
    The turmeric plant was used in ancient medicine to cure a wide range of diseases, including cough, diabetes, and liver disease. Data shows that the principal chemical component of turmeric, curcumin, has a variety of beneficial effects on the body. Therefore, it is of interest to document data on the therapeutic activities of turmeric, including its extracts and possible medical uses, as well as its oral and dental uses and a safety assessment of those uses. Curcumin, the most pure form of turmeric, has shown promise in dentistry.
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  • 文章类型: Journal Article
    含三唑并嘧啶核的分子表现出不同的生物活性,包括抗老年痴呆症,抗糖尿病药,抗癌,抗菌,抗结核药,抗病毒,抗疟药,抗炎,反帕金森主义活动,和青光眼的治疗。三唑并嘧啶具有约8种异构结构,包括最稳定的1,2,4-三唑并[1,5-a]嘧啶。三唑并嘧啶是通过使用各种化学反应获得的,其中a)1,2,4-三唑核与嘧啶环合,b)嘧啶环化为1,2,4-三唑结构,c)1,2,4-三唑[l,5-a]嘧啶重排,和d)嘧啶-四嗪重排。这篇综述讨论了合成方法,三唑并嘧啶的药理作用和给药前景。
    Molecules containing triazolopyrimidine core showed diverse biological activities, including anti-Alzheimer\'s, anti-diabetes, anti-cancer, anti-microbial, anti-tuberculosis, anti-viral, anti-malarial, anti-inflammatory, anti-parkinsonism, and anti-glaucoma activities. Triazolopyrimidines have 8 isomeric structures, including the most stable 1,2,4-triazolo[1,5- a] pyrimidine ones. Triazolopyrimidines were obtained by using various chemical reactions, including a) 1,2,4-triazole nucleus annulation to pyrimidine, b) pyrimidines annulation to 1,2,4-triazole structure, c) 1,2,4-triazolo[l,5-a] pyrimidines rearrangement, and d) pyrimidotetrazine rearrangement. This review discusses synthetic methods, recent pharmacological actions and drug delivery perspectives of triazolopyrimidines.
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  • 文章类型: Journal Article
    背景:全球每年有数千人因神经系统疾病而去世,心血管疾病,癌症,代谢紊乱,和微生物感染。此外,相当大的人群也受到肝毒性的影响,溃疡,胃食管反流病,和乳房裂。随着预期寿命的增加,这些疾病也在稳步增加。寻找创新的疗法来治愈,从而减轻这些疾病的影响,因此,全球关注。
    方法:使用各种电子数据库,例如PubMed,谷歌学者,WebofScience,Elsevier,Springer,ACS,CNKI,和书籍通过关键词Guaiazulene,洋甘菊,GA相关化合物,和Guaiazulene类似。
    结果:FDA已批准双环倍半萜烯GA,通常称为azulon或1,4-二甲基-7-异丙基氮烯,作为化妆品着色剂中的一种成分。GA和相关物质的多效性健康优势,尤其是它们的抗氧化和抗炎作用,吸引了大量的研究。大量研究发现,GA可以帮助管理各种条件,包括细菌感染,肿瘤,免疫调节,祛痰药,利尿剂,排汗,溃疡,皮炎,扩散,和胃炎。这些病症都涉及脂质过氧化和炎症反应。在这次审查中,我们已经涵盖了GA的生物医学应用。此外,我们还强调了愈创木烯衍生物在临床前和临床环境中的治疗潜力,以及它们的潜在机制。
    结论:GA及其相关化合物在几种疾病中显示出治疗潜力。尽管如此,有必要研究它们在各种其他疾病的动物模型中的潜力,并建立它们的安全性。他们可能是一个很好的候选人推进临床试验。
    BACKGROUND: Thousands of people worldwide pass away yearly due to neurological disorders, cardiovascular illnesses, cancer, metabolic disorders, and microbial infections. Additionally, a sizable population has also been impacted by hepatotoxicity, ulcers, gastroesophageal reflux disease, and breast fissure. These ailments are likewise steadily increasing along with the increase in life expectancy. Finding innovative therapies to cure and consequently lessen the impact of these ailments is, therefore, a global concern.
    METHODS: All provided literature on Guaiazulene (GA) and its related compounds were searched using various electronic databases such as PubMed, Google Scholar, Web of Science, Elsevier, Springer, ACS, CNKI, and books via the keywords Guaiazulene, Matricaria chamomilla, GA-related compounds, and Guaiazulene analogous.
    RESULTS: The FDA has approved the bicyclic sesquiterpene GA, commonly referred to as azulon or 1,4-dimethyl-7-isopropylazulene, as a component in cosmetic colorants. The pleiotropic health advantages of GA and related substances, especially their antioxidant and anti-inflammatory effects, attracted a lot of research. Numerous studies have found that GA can help to manage various conditions, including bacterial infections, tumors, immunomodulation, expectorants, diuretics, diaphoresis, ulcers, dermatitis, proliferation, and gastritis. These conditions all involve lipid peroxidation and inflammatory response. In this review, we have covered the biomedical applications of GA. Moreover, we also emphasize the therapeutic potential of guaiazulene derivatives in pre-clinical and clinical settings, along with their underlying mechanism(s).
    CONCLUSIONS: GA and its related compounds exhibit therapeutic potential in several diseases. Still, it is necessary to investigate their potential in animal models for various other ailments and establish their safety profile. They might be a good candidate to advance to clinical trials.
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  • 文章类型: Journal Article
    芦荟(L.)Burm.f.被昵称为“奇迹植物”,有时也被称为“奇迹植物”。它是一种自古以来就被用于与之相关的无数健康益处的植物。它是在常规药物治疗中使用的重要植物之一。它是多年生的多汁植物,Aspodelaceae家族的耐旱性成员。有许多与植物相关的特性有助于治愈各种形式的人类疾病。从植物中获得的提取物和凝胶已被证明是不同条件下的极好的治疗者,主要是各种皮肤问题。此外,这种植物在化妆品行业很受欢迎。植物的基本特性现在主要与植物中存在的天然植物化学物质有关。在植物中发现了各种各样的植物成分,包括各种酚类物质,氨基酸,糖,糖维生素,和其他不同的有机化合物,也是。在植物中发现的主要成分之一是芦荟素分子。它是蒽醌衍生物,并以AloinA和AloinB的异构体形式存在。Barbaloin属于第一组,是芦荟大黄素蒽酮分子的糖苷。植物表现出的各种类型的药理学性质可以归因于这种化学物质。很少有重要的抗氧化剂,抗炎,抗糖尿病,抗癌,抗微生物,和抗病毒,以及他们不同的提高免疫力的行动。最近,分子偶联研究还发现了这些分子作为正在进行的COVID-19疾病的潜在治疗方法的作用。这项研究全面关注从芦荟植物中获得的主要化合物barbaloin的多种药理作用,以及这些天然分子在各种条件下的作用机理和有效应用。
    Aloe vera (L.) Burm.f. is nicknamed the \'Miracle plant\' or sometimes as the \'Wonder plant\'. It is a plant that has been used since ancient times for the innumerable health benefits associated with it. It is one of the important plants that has its use in conventional medicinal treatments. It is a perennial succulent, drought-tolerant member of the family Asphodelaceae. There are scores of properties associated with the plant that help in curing various forms of human ailments. Extracts and gels obtained from plants have been shown to be wonderful healers of different conditions, mainly various skin problems. Also, this plant is popular in the cosmetics industry. The underlying properties of the plant are now mainly associated with the natural phytochemicals present in the plant. Diverse groups of phytoingredients are found in the plant, including various phenolics, amino acids, sugars, vitamins, and different other organic compounds, too. One of the primary ingredients found in the plant is the aloin molecule. It is an anthraquinone derivative and exists as an isomer of Aloin A and Aloin B. Barbaloin belonging to the first group is a glucoside of the aloe-emodin anthrone molecule. Various types of pharmacological properties exhibited by the plant can be attributed to this chemical. Few significant ones are antioxidant, anti-inflammatory, anti-diabetic, anti-cancer, anti-microbial, and anti-viral, along with their different immunity-boosting actions. Recently, molecular coupling studies have also found the role of these molecules as a potential cure against the ongoing COVID-19 disease. This study comprehensively focuses on the numerous pharmacological actions of the primary compound barbaloin obtained from the Aloe vera plant along with the mechanism of action and the potent application of these natural molecules under various conditions.
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