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Aloe-emodin: Progress in Pharmacological Activity, Safety, and Pharmaceutical Formulation Applications 芦荟大黄素:药理活性、安全性和药物制剂应用方面的进展
IF 3.8 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2024-04-19 DOI: 10.2174/0113895575298364240409064833
Haimeng Luoa, Xiaoyun Jia, Mengyu Zhanga, Yaoyao Renb, Rui Tana, Hezhong Jianga, Xiaoqing Wua
: Aloe-emodin (AE) is an anthraquinone derivative and a biologically active component sourced from various plants, including Rheum palmatum L. and Aloe vera. Known chemically as 1,8-dihydroxy-3-hydroxymethyl-anthraquinone, AE has a rich history in traditional medicine and is esteemed for its accessibility, safety, affordability, and effectiveness. AE boasts multiple biochemical and pharmacological properties, such as strong antibacterial, antioxidant, and antitumor effects. Despite its array of benefits, AE's identity as an anthraquinone derivative raises concerns about its potential for liver and kidney toxicity. Nevertheless, AE is considered a promising drug candidate due to its significant bioactivities and cost efficiency. Recent research has highlighted that nanoformulated AE may enhance drug delivery, biocompatibility, and pharmacological benefits, offering a novel approach to drug design. This review delves into AE's pharmacological impacts, mechanisms, pharmacokinetics, and safety profile, incorporating insights from studies on its nanoformulations. The goal is to outline the burgeoning research in this area and to support the ongoing development and utilization of AE-based therapies.
:芦荟大黄素(AE)是一种蒽醌衍生物,是从大黄和芦荟等多种植物中提取的生物活性成分。AE 的化学名称为 1,8-二羟基-3-羟甲基-蒽醌,在传统医学中有着悠久的历史,因其易得性、安全性、经济性和有效性而备受推崇。AE 具有多种生化和药理特性,如强大的抗菌、抗氧化和抗肿瘤作用。尽管 AE 具有一系列优点,但其蒽醌衍生物的特性使人们担心它可能会对肝脏和肾脏产生毒性。然而,AE 因其显著的生物活性和成本效益而被认为是一种很有前途的候选药物。最近的研究强调,纳米制剂 AE 可增强药物输送、生物相容性和药理作用,为药物设计提供了一种新方法。本综述深入探讨了 AE 的药理作用、机制、药代动力学和安全性,并纳入了对其纳米制剂研究的见解。其目的是概述该领域的新兴研究,并为基于 AE 的疗法的持续开发和利用提供支持。
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引用次数: 0
Polyphenols Modulate the miRNAs Expression that Involved in Glioblastoma 多酚调节参与胶质母细胞瘤的 miRNAs 表达
IF 3.8 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2024-04-19 DOI: 10.2174/0113895575304605240408105201
Maede Rezaie, Mohammad Nasehi, Mohammad Shimia, Mohamad Ebrahimnezhad, Bahman Yousefi, Maryam Majidinia
: Glioblastoma multiforme (GBM), a solid tumor that develops from astrocytes, is one of the most aggressive types of brain cancer. While there have been improvements in the efficacy of treating GBM, many problems remain, especially with traditional therapy methods. Therefore, recent studies have extensively focused on developing novel therapeutic agents for combating glioblastoma. Natural polyphenols have been studied for their potential as chemopreventive and chemotherapeutic agents due to their wide range of positive qualities, including antioxidant, antiinflammatory, cytotoxic, antineoplastic, and immunomodulatory activities. These natural compounds have been suggested to act via modulated various macromolecules within cells, including microRNAs (miRNAs), which play a crucial role in the molecular milieu. In this article, we focus on how polyphenols may inhibit tumor growth by influencing the expression of key miRNAs that regulate oncogenes and tumor suppressor genes
:多形性胶质母细胞瘤(GBM)是一种由星形胶质细胞发展而来的实体瘤,是侵袭性最强的脑癌之一。虽然治疗多形性胶质母细胞瘤的疗效有所改善,但仍存在许多问题,尤其是传统治疗方法。因此,最近的研究广泛关注于开发新型治疗药物来对抗胶质母细胞瘤。天然多酚具有抗氧化、抗炎、细胞毒性、抗肿瘤和免疫调节等多种活性,因此被研究用于化学预防和化学治疗。这些天然化合物被认为是通过调节细胞内的各种大分子(包括在分子环境中发挥关键作用的微小核糖核酸(miRNA))而发挥作用的。在本文中,我们将重点讨论多酚如何通过影响调控致癌基因和抑癌基因的关键 miRNA 的表达来抑制肿瘤的生长。
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引用次数: 0
Schiff Bases: A Captivating Scaffold with Potential Anticonvulsant Activity 希夫碱:具有潜在抗惊厥活性的迷人支架
IF 3.8 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2024-04-17 DOI: 10.2174/0113895575302197240408121537
Rakesh Sahu, Kamal Shah
:: One of the most important organic compounds, also known as a Schiff base, imine, or azomethine, has been associated with several biological processes. The group is a component of both natural or synthetic chemicals and functions as both a precursor and an intermediary in the synthesis of therapeutically active substances. The review highlights the various non-metal Schiff bases' structure-activity relationship (SAR) studies, general model, docking, and design approach for anticonvulsant actions. Schiff bases serve as linkers in numerous synthetic compounds with a variety of activities, according to the findings of several investigations. As a result, the current review will give readers a thorough understanding of the key ideas put forth by different researchers regarding the anticonvulsant properties of Schiff bases. It will serve as a valuable information source for those planning to synthesize new anticonvulsant molecules that contain Schiff bases as pharmacophores or biologically active moieties.
::最重要的有机化合物之一,又称希夫碱、亚胺或偶氮甲胺,与多种生物过程有关。该基团是天然或合成化学品的组成部分,在合成治疗活性物质的过程中既是前体也是中间体。本综述重点介绍了各种非金属希夫碱的结构-活性关系(SAR)研究、一般模型、对接以及抗惊厥作用的设计方法。根据多项研究结果,希夫碱可作为许多合成化合物的连接物,具有多种活性。因此,本综述将使读者全面了解不同研究人员就希夫碱的抗惊厥特性提出的主要观点。对于那些计划合成含有希夫碱作为药基或生物活性分子的新抗惊厥分子的人来说,本综述将是一个宝贵的信息来源。
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引用次数: 0
The Pivotal Function of SLC16A1 and SLC16A1-AS1 in Cancer Progress: Molecular Pathogenesis and Prognosis SLC16A1 和 SLC16A1-AS1 在癌症进展中的关键功能:分子发病机制和预后
IF 3.8 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2024-04-15 DOI: 10.2174/0113895575284780240327103039
Yunxi Zhou, Fangshun Tan, Zhuowei Wang, Gang Zhou, Chengfu Yuan
: More than 300 membranes make up the SLC family of transporters, utilizing an ion gradient or electrochemical potential difference to move their substrates across biological membranes. The SLC16 gene family contains fourteen members. Proton-linked transportation of monocarboxylates can be promoted by the transporters MCT1, which the SLC16A1 gene family encodes. Glycolysis is constitutively up-regulated in cancer cells, and the amount of lactate produced as a result is correlated with prognosis. Further speaking, SLC16A1 plays an essential role in controlling the growth and spread of tumors, according to mounting evidence. Additionally, LncRNAs are the collective term for all genes that produce RNA transcripts longer than 200 nucleotides but do not convert into proteins. It has steadily developed into a hub for research, offering an innovative approach to tumor study as technology related to molecular biology advances. The growing study has uncovered SLC16A1-AS1, an RNA that acts as an antisense to SLC16A1, which is erroneously expressed in various types of cancers. Therefore, we compiled the most recent information on the physiological functions and underlying processes of SLC16A1 and the LncRNA SLC16A1-AS1 during tumor development to explore their impact on cancer treatment and prognosis. We compiled the most recent information on the physiological functions and underlying processes of SLC16A1 and the LncRNA SLC16A1-AS1 during tumor development to explore their impact on cancer treatment and prognosis. Relevant studies were retrieved and collected through the PubMed system. After determining SLC16A1 and SLC16A1-AS1 as the research object, we found a close relationship between SLC16A1 and tumorigenesis as well as the influencing factors through the analysis of the research articles. SLC16A1 regulates lactate chemotaxis while uncovering SLC16A1- as1 as an antisense RNA acting through multiple pathways; they affect the metabolism of tumor cells and have an impact on the prognosis of patients with various cancers.
:300 多种膜组成了 SLC 转运体家族,它们利用离子梯度或电化学电位差将底物移过生物膜。SLC16 基因家族包含 14 个成员。SLC16A1 基因家族编码的转运体 MCT1 可促进单羧酸盐的质子连接运输。糖酵解在癌细胞中会持续上调,由此产生的乳酸量与预后相关。此外,越来越多的证据表明,SLC16A1 在控制肿瘤的生长和扩散方面起着至关重要的作用。此外,LncRNA 是产生超过 200 个核苷酸的 RNA 转录本但不转化为蛋白质的所有基因的总称。随着分子生物学相关技术的进步,它已稳步发展成为一个研究中心,为肿瘤研究提供了一种创新方法。随着研究的不断深入,我们发现了 SLC16A1-AS1,它是一种与 SLC16A1 反义的 RNA,而 SLC16A1 在各种癌症中都有错误表达。因此,我们汇编了有关 SLC16A1 和 LncRNA SLC16A1-AS1 在肿瘤发生发展过程中的生理功能和潜在过程的最新信息,以探讨它们对癌症治疗和预后的影响。我们汇编了有关 SLC16A1 和 LncRNA SLC16A1-AS1 在肿瘤发生发展过程中的生理功能和基本过程的最新信息,以探讨它们对癌症治疗和预后的影响。我们通过 PubMed 系统检索并收集了相关研究。确定SLC16A1和SLC16A1-AS1为研究对象后,通过对研究文章的分析,我们发现SLC16A1与肿瘤发生的密切关系以及影响因素。SLC16A1调控乳酸趋化,而SLC16A1- as1是一种反义RNA,通过多种途径发挥作用;它们影响肿瘤细胞的新陈代谢,并对各种癌症患者的预后产生影响。
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引用次数: 0
The Indispensable Roles of GMDS and GMDS-AS1 in the Advancement of Cancer: Fucosylation, Signal Pathway and Molecular Pathogenesis. GMDS 和 GMDS-AS1 在癌症进展中不可或缺的作用:岩藻糖基化、信号通路和分子发病机制。
IF 3.8 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2024-04-09 DOI: 10.2174/0113895575285276240324080234
Ziyan Zhang, Zhuowei Wang, Hong Fan, Jiayi Li, Jiaqi Ding, Gang Zhou, Chengfu Yuan
: Fucosylation is facilitated by converting GDP-mannose to GDP-4-keto-6-deoxymannose, which GDP-mannose 4,6-dehydratase, a crucial enzyme in the route, carries out. One of the most prevalent glycosylation alterations linked to cancer has reportedly been identified as fucosylation. There is mounting evidence that GMDS is intimately linked to the onset and spread of cancer. Furthermore, the significance of long-chain non-coding RNAs in the development and metastasis of cancer is becoming more well-recognized, and the regulatory mechanism of lncRNAs has emerged as a prominent area of study in the biological sciences. GMDS-AS1, an antisense RNA of GMDS, was discovered to have the potential to be an oncogene. We have acquired and analyzed relevant data to understand better how GMDS-AS1 and its lncRNA work physiologically and in tumorigenesis and progression. Additionally, we have looked into the possible effects of these molecules on cancer treatment approaches and patient outcomes. The physiological roles and putative processes of GMDS and lncRNA GMDS-AS1 throughout the development and progression of tumors have been assembled and examined. We also examined how these chemicals might affect patient prognosis and cancer therapy approaches. GMDS and GMDS-AS1 were determined to be research subjects by searching and gathering pertinent studies using the PubMed system. The analysis of these research articles demonstrated the close relationship between GMDS and GMDS-AS1 and tumorigenesis and the factors that influence them. GMDS plays a vital role in regulating fucosylation. The related antisense gene GMDS-AS1 affects the biological behaviors of cancer cells through multiple pathways, including the key processes of proliferation, migration, invasion, and apoptosis, providing potential biomarkers and therapeutic targets for cancer treatment and prognosis assessment.
:通过将 GDP-甘露糖转化为 GDP-4-酮-6-脱氧甘露糖,促进了岩藻糖基化,GDP-甘露糖 4,6-脱水酶是这一过程中的关键酶。据报道,与癌症有关的最普遍的糖基化改变之一是岩藻糖基化。越来越多的证据表明,GMDS 与癌症的发病和扩散密切相关。此外,长链非编码 RNA 在癌症发生和转移过程中的重要性也日益得到认可,lncRNA 的调控机制已成为生物科学研究的一个突出领域。GMDS的反义RNA GMDS-AS1被发现可能是一种癌基因。我们获取并分析了相关数据,以更好地了解 GMDS-AS1 及其 lncRNA 在生理上以及肿瘤发生和发展过程中的作用。此外,我们还研究了这些分子对癌症治疗方法和患者预后可能产生的影响。我们汇集并研究了 GMDS 和 lncRNA GMDS-AS1 在肿瘤发生和发展过程中的生理作用和假定过程。我们还研究了这些化学物质如何影响患者预后和癌症治疗方法。通过使用 PubMed 系统搜索和收集相关研究,确定 GMDS 和 GMDS-AS1 为研究对象。对这些研究文章的分析表明了 GMDS 和 GMDS-AS1 与肿瘤发生之间的密切关系以及影响它们的因素。GMDS 在调节岩藻糖基化方面发挥着重要作用。相关的反义基因 GMDS-AS1 通过多种途径影响癌细胞的生物学行为,包括增殖、迁移、侵袭和凋亡等关键过程,为癌症治疗和预后评估提供了潜在的生物标志物和治疗靶点。
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引用次数: 0
Structural Perspectives in the Development of Novel EGFR Inhibitors for the Treatment of NSCLC 开发治疗 NSCLC 的新型表皮生长因子受体抑制剂的结构视角
IF 3.8 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2024-04-05 DOI: 10.2174/0113895575296174240323172754
Rahul Makhija, Anushka Sharma, Rahul Dubey, Vivek Asati
: Non-small cell Lung cancer (NSCLC) is the most common type of lung cancer, which is caused by high consumption of tobacco and smoking. It is an epithelial lung cancer that affects about 2.2 million people across the globe, according to International Agency for Research on Cancer (IARC). Non-small cell lung cancer is a malignant tumor caused by EGFR mutation that occurs in the in-frame deletion of exon 19 and L858R point mutation in exon 21. Presently, clinically available inhibitors of EGFR (including erlotinib, lapatinib, gefitinib, selumetinib, etc.) are not specific and responsible for undesirable adverse effects. Moreover, to solve this problem search for newer EGFR inhibitors is the utmost need for the treatment and/or management of increasing lung cancer burden. The discovery of therapeutic agents that inhibit the specific target in tumorous cells, such as EGFR, is one of the successful strategies in treating many cancer therapies, including lung cancer. The exhaustive literature survey (2018-2023) has shown the importance of medicinally privileged pyrimidine derivatives together, fused and/or clubbed with other heterocyclic rings to design and develop novel EGFR inhibitors. Pyrimidine derivatives substituted with phenylamine, indole, pyrrole, piperazine, pyrazole, thiophene, pyridine and quinazoline derivatives substituted with phenylamine, pyrimidine, morpholine, pyrrole, dioxane, acrylamide, indole, pyridine, furan, pyrimidine, pyrazole etc. are privileged heterocyclic rings shown promising activity by inhibiting EGFR and TKIs. The present review summarizes the structure-activity relationship (SAR) and enzyme inhibitory activity, including IC50 values, percentage inhibition, and kinetic studies of potential compounds from various literature. The review also includes various aspects of molecular docking studies with compounds under clinical trials and patents filed on pyrimidine-based EGFR inhibitors in treating non-small cell lung cancer. The present review may benefit the medicinal chemist for developing novel compounds such as EGFR inhibitors.
:非小细胞肺癌(NSCLC)是最常见的肺癌类型,由大量吸烟引起。根据国际癌症研究机构(IARC)的数据,这是一种上皮性肺癌,全球约有 220 万人罹患此病。非小细胞肺癌是由表皮生长因子受体(EGFR)突变引起的恶性肿瘤,该突变发生在第 19 号外显子的框内缺失和第 21 号外显子的 L858R 点突变。目前,临床上可用的表皮生长因子受体(EGFR)抑制剂(包括厄洛替尼、拉帕替尼、吉非替尼、塞鲁米替尼等)并不具有特异性,会产生不良反应。此外,为解决这一问题,寻找更新的表皮生长因子受体抑制剂是治疗和/或控制日益加重的肺癌负担的迫切需要。发现抑制肿瘤细胞(如表皮生长因子受体)特异性靶点的治疗药物是治疗包括肺癌在内的多种癌症疗法的成功策略之一。详尽的文献调查(2018-2023 年)显示,具有药用价值的嘧啶衍生物与其他杂环一起、融合和/或联合,对于设计和开发新型表皮生长因子受体抑制剂具有重要意义。与苯胺、吲哚、吡咯、哌嗪、吡唑、噻吩、吡啶取代的嘧啶衍生物,以及与苯胺、嘧啶、吗啉、吡咯、二噁烷、丙烯酰胺、吲哚、吡啶、呋喃、嘧啶、吡唑等取代的喹唑啉衍生物都是具有抑制 EGFR 和 TKIs 活性的杂环。本综述总结了各种文献中潜在化合物的结构-活性关系(SAR)和酶抑制活性,包括 IC50 值、抑制百分比和动力学研究。综述还包括与正在进行临床试验的化合物进行的分子对接研究的各个方面,以及嘧啶类表皮生长因子受体抑制剂治疗非小细胞肺癌的专利申请情况。本综述将有助于药物化学家开发表皮生长因子受体抑制剂等新型化合物。
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引用次数: 0
Mini-Review on Vitamin D in Pediatric Population and its Role in Respiratory and Atopic Disorders 儿科人群中的维生素 D 及其在呼吸系统和特应性疾病中的作用》微型综述
IF 3.8 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2024-02-22 DOI: 10.2174/0113895575284873240212045431
Cristiana Indolfi, Angela Klain, Giulio Dinardo, Fabio Decimo, Maria Maddalena Marrapodi, Amelia Licari, Michele Miraglia del Giudice
: In recent years, our comprehension of the function of vitamin D has significantly evolved. The ubiquitous presence of the vitamin D receptor (Vitamin D Receptor- VDR) in the body has led to its redefinition from a steroidal hormone primarily involved in skeletal functions to a hormone with pleiotropic effects, exerting its influence on the circulatory, nervous, and immune systems. This has prompted investigations into its potential use in preventing and treating chronic metabolic disorders, cardiovascular diseases, infections, and allergic and autoimmune diseases. This comprehensive review explores the various aspects of vitamin D, including its sources, synthesis, functions, and its impact on different physiological systems. It delves into the epidemiology of vitamin D deficiency, highlighting its occurrence among various age demographics and geographic regions. The impact of vitamin D on the immune system is also explored, elucidating its immunomodulatory and anti-inflammatory properties, particularly in the context of respiratory infections. The review discusses emerging evidence concerning the potential advantages of vitamin D in respiratory diseases, pediatric asthma and atopic dermatitis. It also addresses vitamin D supplementation recommendations for various pediatric populations, including term and preterm infants. The growing concern regarding the global health impacts of insufficient vitamin D levels necessitates further research to bridge gaps in knowledge, particularly in enhancing screening, prevention, and approaches to address vitamin D deficiency from birth onwards. In summary, this comprehensive overview underscores the vital role of vitamin D, highlighting the significance of understanding its multifaceted functions and the need for tailored supplementation strategies, especially in vulnerable populations.
:近年来,我们对维生素 D 功能的认识有了重大发展。维生素 D 受体(维生素 D 受体-VDR)在人体内无处不在,这使它从一种主要参与骨骼功能的类固醇激素被重新定义为一种具有多种效应的激素,对循环系统、神经系统和免疫系统产生影响。这促使人们研究它在预防和治疗慢性代谢紊乱、心血管疾病、感染以及过敏性和自身免疫性疾病方面的潜在用途。本综述探讨了维生素 D 的各个方面,包括其来源、合成、功能及其对不同生理系统的影响。它深入探讨了维生素 D 缺乏症的流行病学,强调了它在不同年龄人口和地理区域的发生率。此外,还探讨了维生素 D 对免疫系统的影响,阐明了其免疫调节和抗炎特性,尤其是在呼吸道感染方面。综述讨论了有关维生素 D 在呼吸系统疾病、小儿哮喘和特应性皮炎中潜在优势的新证据。它还讨论了针对不同儿科人群(包括足月儿和早产儿)的维生素 D 补充建议。人们日益关注维生素 D 水平不足对全球健康的影响,因此有必要开展进一步的研究,以弥补知识上的差距,尤其是在加强筛查、预防以及从出生开始就解决维生素 D 缺乏问题的方法方面。总之,本综述强调了维生素 D 的重要作用,强调了了解其多方面功能的重要性以及制定有针对性的补充策略的必要性,尤其是对弱势群体而言。
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引用次数: 0
The Search for Antidotes Against Ricin 寻找蓖麻毒素的解毒剂
IF 3.8 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2024-01-24 DOI: 10.2174/0113895575270509231121060105
Fernanda Diniz Botelho, Tanos Celmar Costa Franca, Steven R. LaPlante
The castor plant (Ricinus communis) is primarily known for its seeds, which contain a unique fatty acid called ricinoleic acid with several industrial and commercial applications. Castor seeds also contain ricin, a toxin considered a chemical and biological warfare agent. Despite years of investigation, there is still no effective antidote or vaccine available. However, some progress has been made, and the development of an effective treatment may be on the horizon. To provide an updated overview of this issue, we have conducted a comprehensive review of the literature on the current state of research in the fight against ricin. This mini-review is based on the reported research and aims to address the challenges faced by researchers, as well as highlight the most successful cases achieved thus far. Our goal is to encourage the scientific community to continue their efforts in this critical search.
蓖麻(Ricinus communis)主要因其种子而闻名,种子中含有一种名为蓖麻油酸的独特脂肪酸,具有多种工业和商业用途。蓖麻籽还含有一种被视为化学和生物战剂的毒素--蓖麻毒素。尽管经过多年的研究,目前仍然没有有效的解毒剂或疫苗。不过,目前已经取得了一些进展,有效的治疗方法可能即将问世。为了提供有关这一问题的最新概述,我们对有关抗击蓖麻毒素研究现状的文献进行了全面回顾。这篇微型综述以报告的研究为基础,旨在探讨研究人员面临的挑战,并重点介绍迄今为止最成功的案例。我们的目标是鼓励科学界在这一关键的探索中继续努力。
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引用次数: 0
Levothyroxine and Non-alcoholic Fatty Liver Disease: A Mini Review. 左甲状腺素与非酒精性脂肪肝:小型回顾
IF 3.8 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2024-01-01 DOI: 10.2174/1389557523666230314113543
Partha Sarathi Singha, Suvendu Ghosh, Debosree Ghosh

Levothyroxine or l-thyroxine is artificially manufactured thyroxine, which is used as a drug to treat underactive thyroid conditions in humans. The drug, levothyroxine, is consumed daily in a prescribed dose to replace the missing thyroid hormone thyroxine in an individual with an underactive thyroid, and it helps to maintain normal physiological conditions. Though it is a life-maintaining drug, it replaces the missing thyroid hormone and performs the necessary daily metabolic functions in our body. Like all other allopathic drugs, it comes with certain side effects, which include joint pain, cramps in muscle, weight gain/loss, hair loss, etc. The thyroid hormone, thyroxine, is known to mobilize fat in our body, including the ones from the hepatic system. An underactive thyroid may cause an accumulation of fat in the liver, leading to a fatty liver, which is clinically termed Non-Alcoholic Fatty Liver Disease (NAFLD). The correlation between hypothyroidism and NAFLD is now well-studied and recognized. As levothyroxine performs the functions of the missing thyroxine, it is anticipated, based on certain preliminary studies, that the drug helps to mobilize hepatic fat and thus may have a crucial role in mitigating the condition of NAFDL.

左甲状腺素或l-甲状腺素是人工制造的甲状腺素,是治疗人类甲状腺功能不全的药物。甲状腺功能不全患者每天按规定剂量服用左甲状腺素这种药物,以补充缺失的甲状腺激素甲状腺素,帮助维持正常的生理状态。虽然它是一种维持生命的药物,但它可以补充缺失的甲状腺激素,并在我们体内执行必要的日常代谢功能。与所有其他对抗疗法药物一样,它也有一定的副作用,包括关节疼痛、肌肉痉挛、体重增加/减轻、脱发等。众所周知,甲状腺激素--甲状腺素--能调动人体内的脂肪,包括来自肝脏系统的脂肪。甲状腺功能减退可能会导致脂肪在肝脏中堆积,从而形成脂肪肝,这在临床上被称为非酒精性脂肪肝(NAFLD)。甲状腺功能减退症与非酒精性脂肪肝之间的相关性现已得到充分研究和认可。由于左甲状腺素具有缺失的甲状腺素的功能,根据某些初步研究,预计该药物有助于动员肝脏脂肪,因此可能在缓解非酒精性脂肪肝方面发挥重要作用。
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引用次数: 0
Quinoline Derivatives as Promising Scaffolds for Antitubercular Activity: A Comprehensive Review. 喹啉衍生物作为抗结核活性的前景看好的支架:全面回顾。
IF 3.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2024-01-01 DOI: 10.2174/0113895575281039231218112953
Mohammad Owais, Arun Kumar, Syed Misbahul Hasan, Kuldeep Singh, Iqbal Azad, Arshad Hussain, Suvaiv, Mohd Akil
<p><strong>Background: </strong>Heterocyclic compounds and their derivatives play a significant role in the design and development of novel quinoline drugs. Among the various pharmacologically active heterocyclic compounds, quinolines stand out as the most significant rings due to their broad pharmacological roles, specifically antitubercular activity, and their presence in plant-based compounds. Quinoline is also known as benzpyridine, benzopyridine, and 1-azanaphthalene. It has a benzene ring fused with a pyridine ring, and both rings share two carbon atoms. The importance of quinoline lies in its incorporation as a key component in various natural compounds found in medicinal plant families like <i>Fumariaceae, Berberidaceae, Rutaceae, Papavaraceae</i>, and others.</p><p><strong>Objective: </strong>This article is expected to have a significant impact on the advancement of effective antitubercular drugs. Through harnessing the potent activity of quinoline derivatives, the research aims to make valuable contributions to combating tuberculosis more efficiently and ultimately reducing the global burden of this infectious disease.</p><p><strong>Methods: </strong>Numerous nitrogen-containing heterocyclic compounds exhibit significant potential as antitubercular agents. These chemicals have fused aromatic nitrogen-heterocyclic nuclei that can change the number of electrons they have, which can change their chemical, physical, and biological properties. This versatility comes from their ability to bind with the receptors in multiple modes, a critical aspect of drug pharmacological screening. Among these compounds, quinoline stands out as it incorporates a stable fusion of a benzene ring with a pyridine nucleus. Quinolines have demonstrated a diverse range of pharmacological activities, including but not limited to anti-tubercular, anti-tumor, anticoagulant, anti-inflammatory, antioxidant, antiviral, antimalarial, anti-HIV, and antimicrobial effects.</p><p><strong>Results: </strong>Some molecules, such as lone-paired nitrogen species, include pyrrole, pyrazole, and quinoline. These molecules contain nitrogen and take part in metabolic reactions with other molecules inside the cell. However, an excessive accumulation of reactive nitrogen species can lead to cytotoxicity, resulting in damage to essential biological macromolecules. Among these compounds, quinoline stands out as the oldest and most effective one, exhibiting a wide range of significant properties such as antitubercular, antimicrobial, anti-inflammatory, antioxidant, analgesic, and anticonvulsant activities. Notably, naturally occurring quinoline compounds, such as quinine, have proven to be potent antimalarial drugs.</p><p><strong>Conclusion: </strong>This review highlights quinoline derivatives' antitubercular potential, emphasizing recent research advancements. Utilizing IC<sub>50</sub> values, the study emphasizes the efficacy of various quinoline substitutions, hybrids, and electron-wi
背景:杂环化合物及其衍生物在新型喹啉类药物的设计和开发中发挥着重要作用。在各种具有药理活性的杂环化合物中,喹啉类化合物是最重要的环,因为它们具有广泛的药理作用,特别是抗结核活性,而且存在于植物性化合物中。喹啉的特征是一个苯环与一个吡啶环融合,两个环共享两个相邻的碳原子。喹啉还有其他名称,如苯吡啶、苯并吡啶和 1-氮杂萘。喹啉的重要性在于它是多种天然化合物的关键成分,这些化合物存在于 Fumariaceae、Berberidaceae、Rutaceae、Papavaraceae 等药用植物科中:本文有望对有效抗结核药物的发展产生重大影响。通过利用喹啉衍生物的强效活性,该研究旨在为更有效地抗击结核病做出宝贵贡献,并最终减轻这一传染性疾病给全球带来的负担:方法:许多含氮杂环化合物显示出作为抗结核药物的巨大潜力。这些化学物质的芳香氮杂环核可以改变电子数,从而改变其化学、物理和生物特性。这种多功能性源于它们能够以多种模式与受体结合,这是药物药理筛选的一个关键方面。在这些化合物中,喹啉因其苯环与吡啶核的稳定融合而脱颖而出。喹啉类化合物具有多种药理活性,包括但不限于抗结核、抗肿瘤、抗凝血、抗炎、抗氧化、抗病毒、抗疟、抗 HIV 和抗菌作用:一些分子,如孤对氮物种,包括吡咯、吡唑和喹啉。这些分子含有氧,并参与细胞内与其他分子的新陈代谢反应。然而,活性氮物种的过度积累会导致细胞毒性,从而对重要的生物大分子造成损害。在这些化合物中,喹啉是最古老、最有效的一种,具有抗结核、抗菌、消炎、抗氧化、镇痛和抗惊厥等多种有益特性。值得注意的是,天然喹啉化合物(如奎宁)已被证明是有效的抗疟药物:本综述强调了喹啉衍生物的抗结核潜力,并着重介绍了近期的研究进展。利用 IC50 值,该研究强调了各种喹啉取代基、杂交基和抽电子基对 MTB H37Rv 的疗效。继续研究对于开发强效、低毒的喹啉衍生物来抗击结核病至关重要。
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Mini reviews in medicinal chemistry
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