drugs

药物
  • 文章类型: Journal Article
    四唑是由一个碳和四个氮原子组成的五元环芳族杂环分子。几种以四唑为基础的药物对细菌显示出有希望的活性,真菌,哮喘,癌症,高血压等.这项研究的总体目标是确定四唑和四唑缀合的银纳米颗粒的抗棘阿米巴性质。合成了四唑共轭银纳米粒子,并使用紫外-可见光谱法进行了确证,动态光散射,和傅里叶变换红外光谱。使用杀变形虫,封存,和测定,研究结果表明,四唑具有抗阿米巴特性,当与银纳米粒子共轭时,这些作用得到增强。当测试寄生虫杀伤时,最小抑制浓度从单独使用四唑的20μM降低到使用四唑缀合的银纳米颗粒的10μM。重要的是,与银纳米颗粒的结合在体外增加了寄生虫介导的人细胞死亡,通过乳酸脱氢酶释放来测量,但它降低了药物对人类细胞的毒性作用。在细胞致病性测定中,最小抑制浓度从单独使用四唑的约15μM降低到使用四唑缀合的银纳米颗粒的小于50μM。总的来说,这些结果清楚地表明,四唑具有有效的抗阿米巴特性,其可以通过与银纳米颗粒结合而增强,并且在合理开发针对由致病性棘阿米巴引起的寄生虫感染如角膜炎和肉芽肿性阿米巴性脑炎的治疗干预措施中具有潜在作用。
    Tetrazoles are five-membered ring aromatic heterocyclic molecules that consist of one carbon and four nitrogen atoms. Several tetrazole-based drugs have shown promising activities against bacteria, fungi, asthma, cancer, hypertension etc. The overall aim of this study was to determine anti-Acanthamoebic properties of tetrazoles and tetrazole-conjugated silver nanoparticles. Tetrazole-conjugated silver nanoparticles were synthesized and confirmed using ultraviolet-visible spectrometry, Dynamic light scattering, and Fourier-transform infrared spectroscopy. Using amoebicidal, encystment, and excystment assays, the findings revealed that tetrazoles exhibited antiamoebic properties and these effects were enhanced when conjugated with silver nanoparticles. When tested for parasite killing, the minimum inhibitory concentration was reduced from ∼20μM with tetrazole alone to 10μM with tetrazole-conjugated silver nanoparticles. Importantly, conjugation with silver nanoparticles increased parasite-mediated human cell death in vitro, as measured by lactate dehydrogenase release, but it reduced toxic effects of drugs alone on human cells. In cytopathogenicity assays, the minimum inhibitory concentration was reduced from ∼15μM with tetrazole alone to less than 50μM with tetrazole-conjugated silver nanoparticles. Overall, these results showed clearly that tetrazoles exhibit potent antiamoebic properties which can be enhanced by conjugation with silver nanoparticles and have potential role in the rational development of therapeutic interventions against parasitic infections such as keratitis and granulomatous amoebic encephalitis due to pathogenic Acanthamoeba.
    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
    尽管有相当多的研究努力,炎症性疾病仍然是人类健康的沉重负担,每年造成重大经济损失。组蛋白脱乙酰酶(HDAC)在调节炎症(通过组蛋白和非组蛋白脱乙酰),染色质结构和基因表达调控中起重要作用。在这里,我们详细描述了不同的HDACs及其功能,并分析了HDACs在炎症性疾病中的作用,包括减少促炎细胞因子的产生,免疫细胞功能调节,和抗炎细胞活性增强。尽管HDAC抑制剂已显示出广泛的炎症性疾病治疗潜力,由于它们的非特异性作用,它们的临床适用性仍然有限,不利影响,和抗药性。随着进一步的研究和见解,这些抑制剂有望成为治疗多种炎性疾病的重要工具。本文旨在探讨HDACs及其抑制剂在多种炎症性疾病中的作用机制和应用前景。
    Despite considerable research efforts, inflammatory diseases remain a heavy burden on human health, causing significant economic losses annually. Histone deacetylases (HDACs) play a significant role in regulating inflammation (via histone and non-histone protein deacetylation) and chromatin structure and gene expression regulation. Herein, we present a detailed description of the different HDACs and their functions and analyze the role of HDACs in inflammatory diseases, including pro-inflammatory cytokine production reduction, immune cell function modulation, and anti-inflammatory cell activity enhancement. Although HDAC inhibitors have shown broad inflammatory disease treatment potentials, their clinical applicability remains limited because of their non-specific effects, adverse effects, and drug resistance. With further research and insight, these inhibitors are expected to become important tools for the treatment of a wide range of inflammatory diseases. This review aims to explore the mechanisms and application prospects of HDACs and their inhibitors in multiple inflammatory diseases.
    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
    与精神分裂症相关的认知障碍(CIAS)代表精神分裂症谱系障碍(SSD)的核心维度之一,对使用SSD的人们的实际功能结果产生重要的负面影响。CIAS的治疗代表了一个相当重要的治疗目标,虽然以认知为导向的基于证据的心理社会干预是可用的,有效的药物治疗可能代表SSD患者生活中的游戏规则改变者。本关键审查报告并讨论了临床实践中可用或正在研究中的几种药物的作用的证据,评论CIAS治疗的当前和未来观点。特别是,抗精神病药物对CIAS的影响,抗胆碱能药物,苯二氮卓类药物,目前常用于SSD的治疗,和伊利珀林,d-丝氨酸,Luvadaxistat,黄omeline-trospium,ulotaront,抗炎分子,和催产素,正在接受监管试验或可以被视为实验药物,将被报告和讨论。目前,现有的药理学药物似乎对CIAS没有实质性的益处,但准确管理抗精神病药物和避免可能进一步加重ASCI的治疗是重要的策略.目前正在2期和3期试验中研究的一些分子提供了非常有希望的初步结果,但目前需要更多信息来评估其在现实环境中的有效性,并就其在临床实践中的使用提供明确的建议.正在进行和未来研究的结果将揭示这些分子中的任何一个是否代表了在CIAS治疗中等待的药理学游戏规则改变者。
    Cognitive Impairment Associated with Schizophrenia (CIAS) represents one of the core dimensions of Schizophrenia Spectrum Disorders (SSD), with an important negative impact on real-world functional outcomes of people living with SSD. Treatment of CIAS represents a therapeutic goal of considerable importance, and while cognition-oriented evidence-based psychosocial interventions are available, effective pharmacological treatment could represent a game-changer in the lives of people with SSD. The present critical review reports and discusses the evidence regarding the effects of several pharmacological agents that are available in clinical practice or are under study, commenting on both current and future perspectives of CIAS treatment. In particular, the effects on CIAS of antipsychotic medications, anticholinergic medications, benzodiazepines, which are currently commonly used in the treatment of SSD, and of iclepertin, d-serine, luvadaxistat, xanomeline-trospium, ulotaront, anti-inflammatory molecules, and oxytocin, which are undergoing regulatory trials or can be considered as experimental agents, will be reported and discussed. Currently, available pharmacological agents do not appear to provide substantial benefits on CIAS, but accurate management of antipsychotic medications and avoiding treatments that can further exacerbate CIAS represent important strategies. Some molecules that are currently being investigated in Phase 2 and Phase 3 trials have provided very promising preliminary results, but more information is currently required to assess their effectiveness in real-world contexts and to provide clear recommendations regarding their use in clinical practice. The results of ongoing and future studies will reveal whether any of these molecules represents the awaited pharmacological game-changer in the treatment of CIAS.
    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
    这项研究探讨了非法药物使用对墨西哥男性劳动力市场结果的影响。我们利用来自可比国家调查的三波统计信息,并利用Lewbel基于异方差的工具变量策略来处理药物消耗的内生性。我们的结果表明,毒品消费在墨西哥背景下具有相当的负面影响:它减少了就业,职业成就和形式,并增加当地男性的失业率。这些影响似乎比高收入经济体的估计更大。
    This research addresses the impact of illicit drug use on labour market outcomes of men in Mexico. We leverage statistical information from three waves of a comparable national survey and make use of the Lewbel\'s heteroskedasticity-based instrumental variable strategy to deal with the endogeneity of the drug consumption. Our results suggests that drug consumption has fairly negative effects in the Mexican context: it reduces employment, occupational attainment and formality and raises unemployment of local males. These effects seem larger than those estimated for high-income economies.
    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
    这项研究的目的是监测处方模式,临床结果,各种间质性肺疾病(ILD)患者的药物不良反应(ADR)。
    这项前瞻性研究是在药理学和治疗学系与呼吸内科合作进行的,乔治国王医科大学,勒克瑙,为期12个月(2020年10月至2021年9月)。在满足纳入和排除标准后,共纳入77例患者。收集了处方,病例报告表上注明了必要的细节。研究完成后,分析数据的处方模式,临床结果,在经过验证的问卷-King的简短ILD(KBILD)问卷的帮助下,提高生活质量。同时,美国存托凭证,如果有的话,采用Hartwig严重程度评估量表和Naranjo因果关系评估量表进行评估。
    最常见的ILD是急性/慢性过敏性肺炎(HP)。每次遇到的平均药物数量为4.45。起跳是最常见的临床体征。据报道,特发性肺纤维化中的clubbing和rhonchi最大。人们发现心理上,呼吸困难和活动,胸部症状,与基线相比,3个月后总KBILD显着降低,统计学差异为P<0.01。在23.38%(18)的受试者中发现了ADR。报告的最大不良反应为胃炎(9.09%),其次是肝炎(3.90%)。
    在我们的研究中,临床诊断为HP的患者比例很高,这凸显了详细的环境暴露史在ILD患者的诊断评估中的重要性,以避免不准确的诊断。与ADR相关的住院是医疗保健系统中的一个重大问题。
    UNASSIGNED: The aim of this study was to monitor prescription patterns, clinical outcomes, and adverse drug reactions (ADR) among patients of various interstitial lung diseases (ILDs).
    UNASSIGNED: This prospective study was conducted in the Department of Pharmacology and Therapeutics in collaboration with the Department of Respiratory Medicine, King George\'s Medical University, Lucknow, for a period of 12 months (October 2020-September 2021). A total of 77 patients were enrolled after satisfying the inclusion and exclusion criteria. The prescriptions were collected, and necessary details were noted on the case report form. After completion of the study, the data were analyzed for prescription patterns, clinical outcomes, and quality of life with the help of a validated questionnaire-King\'s Brief ILD (KBILD) questionnaire. At the same time, ADRs, if any, were assessed using Hartwig\'s Severity Assessment Scale and Naranjo Causality Assessment Scale.
    UNASSIGNED: The most common ILD was acute/chronic hypersensitivity pneumonitis (HP). Average number of drugs per encounter was 4.45. Crepitations were the most common clinical signs. Clubbing and rhonchi were reported maximum in idiopathic pulmonary fibrosis. It was found that psychological, breathlessness and activities, chest symptoms, and total KBILD reduced significantly after 3 months as compared to baseline with a statistically significant difference as P < 0.01. ADRs were found in 23.38% (18) of the subjects. Maximum ADR reported was gastritis (9.09%), followed by hepatitis (3.90%).
    UNASSIGNED: The high proportion of patients clinically diagnosed with HP in our study highlights the importance of a detailed environmental exposure history in the diagnostic evaluation of patients with ILD to avoid inaccurate diagnoses. ADR-related hospital admissions are a significant problem in the health-care system.
    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
    肺动脉高压(PH)是一种慢性进行性疾病,死亡率高。关于AMPK在PH中的作用的研究越来越多。AMPK由三个亚基-α组成,β,和γ。这些子单元之间的串扰最终导致影响PH的微妙平衡,这导致关于AMPK在PH中的作用的相互矛盾的结论。尚不清楚这些亚基如何相互干扰并达到平衡以改善或恶化PH。AMPK在PH治疗中的几个信号通路与,包括AMPK/eNOS/NO通路,Nox4/mTORC2/AMPK通路,AMPK/BMP/Smad通路,和SIRT3-AMPK途径。在这些途径中,AMPK/eNOS/NO和Nox4/mTORC2/AMPK通路的作用和机制比其他通路更清楚,而SIRT3-AMPK通路在PH的治疗中仍不清楚。有针对AMPK的药物可以改善PH,如二甲双胍(MET),MET组合,和红景天提取物.此外,几个新的因素靶向AMPK来改善PH,如ADAMTS8,TUFM,和盐诱导型激酶。然而,未来还需要更多的研究来探索与这些新因子相关的AMPK信号通路。总之,AMPK在PH中起重要作用。
    Pulmonary hypertension (PH) is a chronic progressive disease with high mortality. There has been more and more research focusing on the role of AMPK in PH. AMPK consists of three subunits-α, β, and γ. The crosstalk among these subunits ultimately leads to a delicate balance to affect PH, which results in conflicting conclusions about the role of AMPK in PH. It is still unclear how these subunits interfere with each other and achieve balance to improve or deteriorate PH. Several signaling pathways are related to AMPK in the treatment of PH, including AMPK/eNOS/NO pathway, Nox4/mTORC2/AMPK pathway, AMPK/BMP/Smad pathway, and SIRT3-AMPK pathway. Among these pathways, the role and mechanism of AMPK/eNOS/NO and Nox4/mTORC2/AMPK pathways are clearer than others, while the SIRT3-AMPK pathway remains still unclear in the treatment of PH. There are drugs targeting AMPK to improve PH, such as metformin (MET), MET combination, and rhodiola extract. In addition, several novel factors target AMPK for improving PH, such as ADAMTS8, TUFM, and Salt-inducible kinases. However, more researches are needed to explore the specific AMPK signaling pathways involved in these novel factors in the future. In conclusion, AMPK plays an important role in PH.
    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
    在广泛的乳腺癌研究中,有价值的数据和发现通常分散在已发表的文献中,数据库和网络资源,在策划特定数据集时给研究人员和从业人员带来挑战,基因和相关信息。因此,我们开发了BRCAFEM(雌性乳房切除术),用于乳腺癌研究的综合数据库。BRCAFem包括1220个乳腺癌基因,82个FDA批准的乳腺癌预防和治疗药物以及33个测序和成像数据集。此外,BRCAFem提供有关乳腺癌的一般信息,全球统计,危险因素,与乳腺癌研究的最新进展相关的治疗选择和博客。
    Amid extensive breast cancer research, valuable data and findings often remain scattered across published literature, databases and web resources, posing challenges for researchers and practitioners in curating specific datasets, genes and relevant information. Hence, we developed BRCAFem (BReast CAncer of Females), an integrated database for breast cancer research. BRCAFem includes 1220 breast cancer genes, 82 FDA-approved breast cancer prevention and treatment drugs and 33 sequencing and imaging datasets. Additionally, BRCAFem provides general information about breast cancer, global statistics, risk factors, treatment options and blogs related to recent updates in breast cancer research.
    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
    本文提出了一种制备多功能复合生物材料的新方法,并将其应用于先进的生物医学领域。生物材料由磷酸二钙(DCPD)和生物活性硅酸盐玻璃(SiO2/Na2O和SiO2/K2O)组成,含有抗生素硫酸链霉素。通过X射线衍射和衰减全反射傅里叶变换红外光谱对材料进行了深入表征,和zeta电位分析,紫外可见分光光度法,在模拟体液(SBF)溶液中进行离子交换测量。主要结果包括在硅酸盐溶液的影响下将磷酸二钙原位化学转化为磷灰石相和抗生素的掺入。ζ电位显示表面电荷从ζ=-24.6mV降低至ζ=-16.5mV。此外,在37天的时间内观察到抗生素的受控和延长释放,释放浓度高达755ppm。小鼠毒性试验证明了对生物材料的良好耐受性,无明显不良反应。此外,这些生物材料对各种细菌菌株显示出有效的抗菌活性,包括单核细胞增生李斯特菌,金黄色葡萄球菌,大肠杆菌,铜绿假单胞菌,表明它们在组织工程中的潜在用途,药物输送,以及骨科和牙科植入物。通过将抗生素整合到生物材料复合材料中,我们实现了控制释放和延长抗菌疗效。这项研究通过探索创新的合成路线并展示其在再生医学和受控药物递送方面的前景,为推进生物材料的发展做出了贡献。
    This article presents a new method for preparing multifunctional composite biomaterials with applications in advanced biomedical fields. The biomaterials consist of dicalcium phosphate (DCPD) and bioactive silicate glasses (SiO2/Na2O and SiO2/K2O), containing the antibiotic streptomycin sulfate. Materials were deeply characterized by X-ray diffraction and attenuated total reflectance Fourier transform infrared spectroscopy, and zeta potential analysis, UV-visible spectrophotometry, and ion-exchange measurement were applied in a simulating body fluid (SBF) solution. The main results include an in situ chemical transformation of dicalcium phosphate into an apatitic phase under the influence of silicate solutions and the incorporation of the antibiotic. The zeta potential showed a decrease in surface charge from ζ = -24.6 mV to ζ = -16.5 mV. In addition, a controlled and prolonged release of antibiotics was observed over a period of 37 days, with a released concentration of up to 755 ppm. Toxicity tests in mice demonstrated good tolerance of the biomaterials, with no significant adverse effects. Moreover, these biomaterials have shown potent antibacterial activity against various bacterial strains, including Listeria monocytogenes, Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa, suggesting their potential use in tissue engineering, drug delivery, and orthopedic and dental implants. By integrating the antibiotic into the biomaterial composites, we achieved controlled release and prolonged antibacterial efficacy. This research contributes to advancing biomaterials by exploring innovative synthetic routes and showcasing their promise in regenerative medicine and controlled drug delivery.
    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
    过渡金属配合物的药用性质受到配合物结构中存在的配体的性质和物理化学特征的极大影响。由于有机硒化合物的独特生物学特性体现在多种药理活性(如抗氧化、抗病毒,抗菌和抗癌),近年来,人们对它们在设计和合成一系列过渡金属基配位化合物中用作配体化合物产生了越来越多的兴趣,这些配位化合物已被开发为抗肿瘤和抗微生物剂。我们在这篇综述中的目的是提供结构中带有有机硒配体的过渡金属配合物的最新发展的概述,这些配合物可能是治疗各种疾病的有希望的选择。特别是癌症和感染性疾病。为此,Co的复合物,Ni,Cu,Zn,Ru,Pd,Pt,将包括和讨论作为最多探索的示例的Au和Sn。
    The medicinal properties of transition metal complexes are greatly influenced by the nature and physico-chemical features of the ligand present in the complex structure. Due to the unique biological properties of the organoselenium compounds reflected in the variety of pharmacological activities (such as antioxidative, antiviral, antimicrobial and anticancer), the last years have brought increased interest for their use as a ligands compounds in the design and syntheses of range of transition metal-based coordination compounds that have been explored as antitumor and antimicrobial agents. Our aim in this review is to provide the overview of an recent development of the transition metal complexes bearing organoselenium ligands in the structure that could be promising choice for the treatment of various diseases, particularly cancer and infective diseases. For this purpose, the complexes of Co, Ni, Cu, Zn, Ru, Pd, Pt, Au and Sn as the most explored examples will be included and discussed.
    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
    目的:评估每周服用1%阿托品对儿童近视进展的影响,以及这种影响是否可持续。
    方法:对每周服用1%阿托品超过1年的3-15岁近视儿童的病历进行回顾性分析。收集每次就诊时的轴向长度(AL)和球面等效屈光度(SER)。使用广义估计方程分析了AL或SER随时间的变化。采用多元线性回归分析近视进展的相关因素。使用接受者工作特征分析评估短期AL变化预测阿托品不良反应者(AL变化>0.2mm/年)的性能。
    结果:共纳入694名参与者,平均年龄为8.83岁。随访时间达到1年、2年、3年和4年的参与者为256例(36.9%),250(36.0%),143(20.6%)和45(6.5%)。AL的累积变化为0.05mm,0.24mm,0.47mm,1年分别为0.56毫米,2年,3年和4年治疗。自治疗的第二年起,观察到每年大约0.20mm的伸长。年龄较大和较低的初始近视屈光度与较少的近视进展独立相关。在最初的2个月中,AL的减少超过0.04毫米可以作为在2年内识别快速进展者(AL变化>0.2毫米/年)的指标,敏感性和特异性分别为0.78和0.73。
    结论:每周1%阿托品可能是一种潜在的有效治疗方法,对近视控制儿童尤其是年龄较大和近视较低的儿童具有更持久的效果。
    OBJECTIVE: To assess the effect of weekly 1% atropine use on children\'s myopia progression and whether the effect is sustainable.
    METHODS: Medical records of myopic children aged 3-15 years receiving weekly 1% atropine for more than 1 year were retrospectively reviewed. Axial length (AL) and spherical equivalent refraction (SER) at every visit were collected. The changes in AL or SER over time were analysed using generalised estimating equation. The related factors of myopic progression were performed by multiple linear regression. The performance of short-term AL change to predict atropine-poor responders (AL change >0.2 mm/year) was assessed using receiver operating characteristic analysis.
    RESULTS: A total of 694 participants with a mean age of 8.83 years were included. The participants with follow-up time reached 1, 2, 3 and 4 years were 256 (36.9%), 250 (36.0%), 143 (20.6%) and 45 (6.5%) separately. The cumulative change in AL was 0.05 mm, 0.24 mm, 0.47 mm, 0.56 mm separately for 1-year, 2-year, 3-year and 4- year treatment. Approximate 0.20 mm elongation per year was observed since the second-year of the treatment. Older age and lower initial myopic refraction were independently associated with less myopic progression. A decrease in AL of more than 0.04 mm during the initial 2 months could serve as an indicator for identifying fast progressors (AL change >0.2 mm/year) over a 2-year period, with sensitivity and specificity rates of 0.78 and 0.73, respectively.
    CONCLUSIONS: Weekly 1% atropine may be a potentially effective treatment with longer lasting effects for children with myopia control especially in those with older age and lower myopia.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

公众号