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Quercetin in Oncology: A Phytochemical with Immense Therapeutic Potential. 肿瘤学中的槲皮素:具有巨大治疗潜力的植物化学物质
IF 3 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 DOI: 10.2174/0113894501292466240627050638
Raj Kamal, Priyanka Paul, Shubham Thakur, Sachin Kumar Singh, Ankit Awasthi

Quercetin is a natural flavonoid with various pharmacological actions such as anti-inflammatory, antioxidant, antimicrobial, anticancer, antiviral, antidiabetic, cardioprotective, neuroprotective, and antiviral activities. Looking at these enormous potentials, researchers have explored how they can be used to manage numerous cancers. It's been studied for cancer management due to its anti-angiogenesis, anti-metastatic, and antiproliferative mechanisms. Despite having these proven pharmacological activities, the clinical use of quercetin is limited due to its first-- pass metabolism, poor solubility, and bioavailability. To address these shortcomings, researchers have fabricated various nanocarriers-based formulations to fight cancer. The present review overshadows the pharmacological potential, mechanisms, and application of nanoformulations against different cancers. Teaser: Explore the potential of Quercetin, a natural flavonoid with diverse pharmacological activities, and its nanoformulations in managing various cancers.

槲皮素是一种天然类黄酮,具有抗炎、抗氧化、抗菌、抗癌、抗病毒、抗糖尿病、保护心脏、保护神经和抗病毒等多种药理作用。鉴于这些巨大的潜力,研究人员探索了如何利用它们来控制多种癌症。由于其抗血管生成、抗转移和抗增殖机制,它已被研究用于癌症治疗。尽管槲皮素具有这些已被证实的药理活性,但由于它的首过代谢、溶解性和生物利用度较差,其临床应用受到了限制。为了解决这些问题,研究人员制作了各种基于纳米载体的抗癌制剂。本综述介绍了纳米制剂在抗击不同癌症方面的药理潜力、机制和应用。
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引用次数: 0
An Exploratory Review on the Hypoglycemic Action of Unani Anti-diabetic Drugs via Possible Modulation of Gut Microbiota. 关于尤那尼抗糖尿病药物通过可能的肠道微生物群调控降血糖作用的探索性综述。
IF 3.2 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 DOI: 10.2174/0113894501275731231215101426
Shaheen Akhlaq, Shabnam Anjum Ara, Malik Itrat, Mohammad Fazil, Bilal Ahmad, Usama Akram, Merajul Haque, Neelam Quddusi, Ahmad Sayeed

Background and aim: Diabetes mellitus is a chronic, multi-factorial metabolic disorder and also an important public health issue that requires multi-dimensional therapeutic strategies for effective control. Unani herbs have long been used to effectively mitigate diabetes through various mechanisms. In recent years, it has been speculated that the alteration of gut microbiome ecology is potentially one of the important mechanisms through which the Unani drugs exert hypoglycemic action. This review aims at the trans-disciplinary interpretation of the holistic concepts of the Unani system of medicine and the molecular insights of contemporary medicine for novel strategies for diabetes management.

Methodology: We searched scientific databases such as PubMed, Google Scholar, and Science-Direct, etc. Unani classical texts (Urdu, Arabic, and Persian), and medical books, for diabetic control with Unani medicine through the gut microbiome.

Results: Unani medicine defines, diabetes as a urinary system disorder disrupting the transformational faculty (Quwwat Mughayyira) in the gastrointestinal tract. The Unani system and contemporary biomedicine use different epistemology and ontology for describing diabetes through gutderived factors in whole-body glucose homeostasis. Unani Pharmaceutics have reported in clinical and preclinical (in vitro/ in vivo) trials in improving diabetes by altering gut microbiota composition, microvascular dysfunction, and inflammation. However, the preventive plan is the preservance of six essential factors (Asbāb Sitta Ḍarūriyya) as a lifestyle plan.

Conclusion: This is the first study on the integrative strategy about the hypoglycemic effects of Unani herbs that could serve as a prerogative novel approach for cost-effective, holistic, rationalistic, and multi-targeted diabetes management.

背景和目的:糖尿病是一种慢性、多因素代谢紊乱疾病,也是一个重要的公共卫生问题,需要多维治疗策略才能有效控制。长期以来,尤那尼草药通过各种机制有效缓解糖尿病。近年来,人们推测肠道微生物群生态的改变可能是乌纳尼药物发挥降糖作用的重要机制之一。这篇综述旨在跨学科解读乌纳尼医学体系的整体概念和当代医学的分子洞察力,为糖尿病管理提供新策略:我们检索了 PubMed、Google Scholar 和 Science-Direct 等科学数据库。方法:我们检索了 PubM、Google Scholar、Science-Direct 等科学数据库,乌纳尼经典文本(乌尔都语、阿拉伯语和波斯语)和医学书籍,通过肠道微生物组了解乌纳尼医学对糖尿病的控制:结果:尤那尼医学将糖尿病定义为泌尿系统疾病,破坏了胃肠道的转化能力(Quwwat Mughayyira)。乌纳尼系统和当代生物医学使用不同的认识论和本体论,通过全身葡萄糖稳态中的肠道因素来描述糖尿病。据报道,在临床和临床前(体外/体内)试验中,尤那尼医药学通过改变肠道微生物群组成、微血管功能障碍和炎症来改善糖尿病。然而,预防计划是保持六个基本要素(Asbāb Sitta arūriyya)的生活方式计划:这是第一项关于尤那尼草药降血糖作用的综合策略研究,可作为一种具有成本效益、整体、合理和多目标糖尿病管理的首选新方法。
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引用次数: 0
Trends on Novel Targets and Nanotechnology-Based Drug Delivery System in the Treatment of Parkinson's disease: Recent Advancement in Drug Development. 治疗帕金森病的新靶点和纳米技术给药系统的发展趋势:药物开发的最新进展。
IF 3 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 DOI: 10.2174/0113894501312703240826070530
Manisha Majumdar, Hemant Badwaik

Parkinson's disease (PD) is a progressive neurodegenerative disorder that impacts a significant portion of the population. Despite extensive research, an effective cure for PD remains elusive, and conventional pharmacological treatments often face limitations in efficacy and management of symptoms. There has been a lot of discussion about using nanotechnology to increase the bioavailability of small- molecule drugs to target cells in recent years. It is possible that PD treatment might become far more effective and have fewer side effects if medication delivery mechanisms were to be improved. Potential alternatives to pharmacological therapy for molecular imaging and treatment of PD may lie in abnormal proteins such as parkin, α-synuclein, leucine-rich repeat serine and threonine protein kinase 2. Published research has demonstrated encouraging outcomes when nanomedicine-based approaches are used to address the challenges of PD therapy. So, to address the present difficulties of antiparkinsonian treatment, this review outlines the key issues and limitations of antiparkinsonian medications, new therapeutic strategies, and the breadth of delivery based on nanomedicine. This review covers a wide range of subjects, including drug distribution in the brain, the efficacy of drug-loaded nano-carriers in crossing the blood-brain barrier, and their release profiles. In PD, the nano-carriers are also used. Novel techniques of pharmaceutical delivery are currently made possible by vesicular carriers, which eliminate the requirement to cross the blood-brain barrier (BBB).

帕金森病(PD)是一种影响许多人的神经退行性疾病(ND)。然而,帕金森病仍无法治愈,传统药物也难以奏效。近年来,关于利用纳米技术提高小分子药物在靶细胞中的生物利用度的讨论不绝于耳。如果药物输送机制得到改善,那么帕金森病的治疗可能会变得更加有效,副作用也会更少。帕金森病分子成像和治疗的药物疗法的潜在替代方法可能在于异常蛋白质,如帕金蛋白、α-突触核蛋白、富亮氨酸重复丝氨酸和苏氨酸蛋白激酶2。已发表的研究表明,使用基于纳米药物的方法来应对帕金森病治疗的挑战取得了令人鼓舞的成果。因此,为了解决目前抗帕金森病治疗的难题,本综述概述了抗帕金森病药物的关键问题和局限性、新的治疗策略以及基于纳米药物的给药广度。这篇综述涵盖了广泛的主题,包括药物在大脑中的分布、载药纳米载体穿过血脑屏障的功效及其释放特征。此外,纳米载体还被应用于 "帕金森病"。目前,囊泡载体使新的给药技术成为可能,这种载体无需穿过血脑屏障(BBB)。
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引用次数: 0
Genetic Factors and MicroRNAs in the Development of Gallbladder Cancer: The Prospective Clinical Targets. 胆囊癌发病过程中的遗传因素和微RNA:前瞻性临床目标。
IF 3 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 DOI: 10.2174/0113894501182288240319074330
Roshni Quraishi, Somali Sanyal, Medha Dwivedi, Monika Moitra, Manish Dwivedi

Gallbladder cancer (GBC) is an uncommon condition in which malignant (cancer) cells are detected in gallbladder tissue. Cancer is often triggered when normal cells turn malignant and begin to spread. Cancer can also be caused by genetic anomalies that result in uncontrolled cell proliferation and tumor development. MicroRNAs (also known as miRNAs or miRs) are a group of small, endogenous, non-coding RNAs of 19-23 nucleotides in length, which play a key role in post-transcriptional gene regulation. These miRNAs serve as negative gene regulators by supervising target genes and regulating biological processes, including cell proliferation, migration, invasion, and apoptosis. Cancer development and progression relate to aberrant miRNA expression. This review demonstrated the implication of various genetic factors and microRNAs in developing and regulating GBC. This suggests the potential of genes and RNAs as the diagnostic, prognostic, and therapeutic targets in gallbladder cancer.

胆囊癌(GBC)是一种在胆囊组织中发现恶性(癌)细胞的不常见疾病。癌症通常是由正常细胞恶变并开始扩散而引发的。癌症也可能由基因异常引起,导致细胞增殖失控和肿瘤发展。microRNA(又称 miRNA 或 miRs)是一组长度为 19-23 个核苷酸的小型内源性非编码 RNA,在转录后基因调控中发挥关键作用。这些 miRNA 作为负性基因调控因子,通过监督靶基因和调控生物过程,包括细胞增殖、迁移、侵袭和凋亡。癌症的发生和发展与 miRNA 的异常表达有关。本综述展示了各种遗传因素和 microRNA 在 GBC 的发展和调控中的作用。这表明基因和 RNA 有可能成为胆囊癌的诊断、预后和治疗靶点。
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引用次数: 0
A Review on the Recent Advancements and Artificial Intelligence in Tablet Technology. 平板电脑技术的最新进展和人工智能回顾。
IF 3 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 DOI: 10.2174/0113894501281290231221053939
Amit Sahu, Sunny Rathee, Shivani Saraf, Sanjay K Jain

Background: Tablet formulation could be revolutionized by the integration of modern technology and established pharmaceutical sciences. The pharmaceutical sector can develop tablet formulations that are not only more efficient and stable but also patient-friendly by utilizing artificial intelligence (AI), machine learning (ML), and materials science.

Objectives: The primary objective of this review is to explore the advancements in tablet technology, focusing on the integration of modern technologies like artificial intelligence (AI), machine learning (ML), and materials science to enhance the efficiency, cost-effectiveness, and quality of tablet formulation processes.

Methods: This review delves into the utilization of AI and ML techniques within pharmaceutical research and development. The review also discusses various ML methodologies employed, including artificial neural networks, an ensemble of regression trees, support vector machines, and multivariate data analysis techniques.

Results: Recent studies showcased in this review demonstrate the feasibility and effectiveness of ML approaches in pharmaceutical research. The application of AI and ML in pharmaceutical research has shown promising results, offering a potential avenue for significant improvements in the product development process.

Conclusion: The integration of nanotechnology, AI, ML, and materials science with traditional pharmaceutical sciences presents a remarkable opportunity for enhancing tablet formulation processes. This review collectively underscores the transformative role that AI and ML can play in advancing pharmaceutical research and development, ultimately leading to more efficient, reliable and patient-centric tablet formulations.

背景:片剂制剂可以通过现代技术与成熟的制药科学的结合而发生革命性的变化。制药行业可以利用人工智能(AI)、机器学习(ML)和材料科学,开发出不仅更高效、更稳定,而且对患者更友好的片剂配方:本综述的主要目的是探讨片剂技术的进步,重点关注人工智能(AI)、机器学习(ML)和材料科学等现代技术的整合,以提高片剂制备过程的效率、成本效益和质量:本综述深入探讨了人工智能和 ML 技术在制药研发中的应用。本综述还讨论了所采用的各种 ML 方法,包括人工神经网络、回归树集合、支持向量机和多元数据分析技术:结果:本综述中展示的最新研究证明了 ML 方法在制药研究中的可行性和有效性。人工智能和 ML 在制药研究中的应用已取得了可喜的成果,为产品开发过程的重大改进提供了潜在的途径:纳米技术、人工智能、ML 和材料科学与传统制药科学的结合为改进片剂制备工艺提供了难得的机会。本综述共同强调了人工智能和 ML 在推动药物研究与开发方面可发挥的变革性作用,最终实现更高效、可靠和以患者为中心的片剂配方。
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引用次数: 0
Targeting Protein Phosphatases for the Treatment of Chronic Liver Disease. 以蛋白磷酸酶为靶点治疗慢性肝病。
IF 3.2 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 DOI: 10.2174/0113894501278886231221092522
Yi-Ming Li, Hong-Wei He, Na Zhang

There exists a huge number of patients suffering from chronic liver disease worldwide. As a disease with high incidence and mortality worldwide, strengthening the research on the pathogenesis of chronic liver disease and the development of novel drugs is an important issue related to the health of all human beings. Phosphorylation modification of proteins plays a crucial role in cellular signal transduction, and phosphatases are involved in the development of liver diseases. Therefore, this article summarized the important role of protein phosphatases in chronic liver disease with the aim of facilitating the development of drugs targeting protein phosphatases for the treatment of chronic liver disease.

全世界有大量的慢性肝病患者。作为世界范围内发病率和死亡率较高的疾病,加强对慢性肝病发病机理的研究和新型药物的开发是关系到全人类健康的重要课题。蛋白质的磷酸化修饰在细胞信号传导中起着至关重要的作用,而磷酸酶与肝病的发生发展有关。因此,本文总结了蛋白磷酸酶在慢性肝病中的重要作用,旨在促进针对蛋白磷酸酶治疗慢性肝病药物的开发。
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引用次数: 0
Revolutionizing the World of Pharmaceuticals: Unleashing the Game-Changing Power of 3D Printing. 彻底改变制药世界:释放 3D 打印改变游戏规则的力量。
IF 3 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 DOI: 10.2174/0113894501304163240429081741
Abhishek Chahuan, Abhishek Verma, Devank Shekho, Ritika Mishra, Ankit Awasthi
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引用次数: 0
Targeted Treatment Strategies for Mitochondria Dysfunction: Correlation with Neurological Disorders. 线粒体功能障碍的靶向治疗策略:与神经系统疾病的相关性。
IF 3 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 DOI: 10.2174/0113894501303824240604103732
Rishav Sharma, Rishabha Malviya, Saurabh Srivastava, Irfan Ahmad, Safia Obaidur Rab, Prerna Uniyal

Mitochondria are an essential intracellular organelle for medication targeting and delivery since they seem to create energy and conduct many other cellular tasks, and mitochondrial dysfunctions and malfunctions lead to many illnesses. Many initiatives have been taken to detect, diagnose, and image mitochondrial abnormalities, and to transport and accumulate medicines precisely to mitochondria, all because of special mitochondrial aspects of the pathophysiology of cancer. In addition to the negative membrane potential and paradoxical mitochondrial dynamics, they include high temperatures, high levels of reactive oxygen species, high levels of glutathione, and high temperatures. Neurodegenerative diseases represent a broad spectrum of debilitating illnesses. They are linked to the loss of certain groups of neurons based on an individual's physiology or anatomy. The mitochondria in a cell are generally accepted as the authority with respect to ATP production. Disruption of this system is linked to several cellular physiological issues. The development of neurodegenerative disorders has been linked to mitochondrial malfunction, according to pathophysiological studies. There seems to be substantial evidence connecting mitochondrial dysfunction and oxidative stress to the development of neurodegenerative disorders. It has been extensively observed that mitochondrial malfunction triggers autophagy, which plays a role in neurodegenerative disorders. In addition, excitotoxicity and mitochondrial dysfunction have been linked to the development of neurodegenerative disorders. The pathophysiology of neurodegenerative illnesses has been linked to increased apoptosis and necrosis, as well as mitochondrial malfunction. A variety of synthetic and natural treatments have shown efficacy in treating neurodegenerative illnesses caused by mitochondrial failure. Neurodegenerative illnesses can be effectively treated with existing drugs that target mitochondria, although their precise formulations are poorly understood. Therefore, there is an immediate need to focus on creating drug delivery methods specifically targeted at mitochondria in the treatment and diagnosis of neurodegenerative disorders.

线粒体是细胞内靶向给药的重要细胞器,因为线粒体似乎创造能量并执行许多其他细胞任务,而线粒体功能障碍和失调会导致许多疾病。由于线粒体在癌症病理生理学中的特殊地位,人们已经采取了许多措施来检测、诊断和成像线粒体异常,并精确地向线粒体输送和积聚药物。除了负膜电位和矛盾的线粒体动力学外,还包括高温、高水平的活性氧、高水平的谷胱甘肽和高温。神经退行性疾病是一种范围广泛的使人衰弱的疾病。根据个人的生理或解剖结构,它们与某些神经元群的丧失有关。细胞中的线粒体被公认为是产生 ATP 的权威。这一系统的破坏与多个细胞生理问题有关。病理生理学研究表明,神经退行性疾病的发生与线粒体功能失调有关。似乎有大量证据表明,线粒体功能障碍和氧化应激与神经退行性疾病的发生有关。据广泛观察,线粒体功能失调会引发自噬,而自噬在神经退行性疾病中发挥着作用。此外,兴奋性毒性和线粒体功能障碍也与神经退行性疾病的发生有关。神经退行性疾病的病理生理学与细胞凋亡和坏死增加以及线粒体功能失调有关。各种人工合成和天然疗法对治疗线粒体功能失调引起的神经退行性疾病都有疗效。现有的针对线粒体的药物可以有效治疗神经退行性疾病,但对其精确配方的了解还很不够。因此,在治疗和诊断神经退行性疾病时,迫切需要重点研究专门针对线粒体的给药方法。
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引用次数: 0
Quantum Dot-based Bio-conjugates as an Emerging Bioimaging Tool for Cancer Theranostic- A Review. 基于量子点的生物共轭物作为一种新兴的癌症治疗生物成像工具--综述。
IF 3.2 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 DOI: 10.2174/0113894501283669240123105250
Lipika Priya, Smit Mehta, Darshan Gevariya, Raghav Sharma, Drishti Panjwani, Shruti Patel, Priyanka Ahlawat, Abhay Dharamsi, Asha Patel
<p><p>Cancer is the most widely studied disorder in humans, but proper treatment has not yet been developed for it. Conventional therapies, like chemotherapy, radiation therapy, and surgery, have been employed. Such therapies target not only cancerous cells but also harm normal cells. Conventional therapy does not result in specific targeting and hence leads to severe side effects. The main objective of this study is to explore the QDs. QDs are used as nanocarriers for diagnosis and treatment at the same time. They are based on the principle of theranostic approach. QDs can be conjugated with antibodies <i>via</i> various methods that result in targeted therapy. This results in their dual function as a diagnostic and therapeutic tool. Nanotechnology involving such nanocarriers can increase the specificity and reduce the side effects, leaving the normal cells unaffected. This review pays attention to different methods for synthesising QDs. QDs can be obtained using either organic method and synthetic methods. It was found that QDs synthesised naturally are more feasible than the synthetic process. Top or bottom-up approaches have also emerged for the synthesis of QDs. QDs can be conjugated with an antibody <i>via</i> non-covalent and covalent binding. Covalent binding is much more feasible than any other method. Zero-length coupling plays an important role as EDC (1-Ethyl-3-Ethyl dimethylaminopropyl)carbodiimide is a strong crosslinker and is widely used for conjugating molecules. Antibodies work as surface ligands that lead to antigen- antibody interaction, resulting in site-specific targeting and leaving behind the normal cells unaffected. Cellular uptake of the molecule is done by either passive targeting or active targeting. QDs are tiny nanocrystals that are inorganic in nature and vary in size and range. Based on different sizes, they emit light of specific wavelengths. They have their own luminescent and optical properties that lead to the monitoring, imaging, and transport of the therapeutic moiety to a variety of targets in the body. The surface of the QDs is modified to boost their functioning. They act as a tool for diagnosis, imaging, and delivery of therapeutic moieties. For improved therapeutic effects, nanotechnology leads the cellular uptake of nanoparticles <i>via</i> passive targeting or active targeting. It is a crucial platform that not only leads to imaging and diagnosis but also helps to deliver therapeutic moieties to specific sites. Therefore, this review concludes that there are numerous drawbacks to the current cancer treatment options, which ultimately result in treatment failure. Therefore, nanotechnology that involves such a nanocarrier will serve as a tool for overcoming all limitations of the traditional therapeutic approach. This approach helps in reducing the dose of anticancer agents for effective treatment and hence improving the therapeutic index. QDs can not only diagnose a disease but also deliver drugs to the
癌症是人类研究最为广泛的疾病,但目前尚未开发出适当的治疗方法。传统疗法,如化疗、放疗和手术,已被采用。这些疗法不仅针对癌细胞,也伤害正常细胞。传统疗法并不具有特定的靶向性,因此会导致严重的副作用。本研究的主要目的是探索 QDs。QDs 可作为纳米载体同时用于诊断和治疗。它们基于治疗方法的原理。QDs 可以通过各种方法与抗体结合,从而实现靶向治疗。因此,它们具有诊断和治疗工具的双重功能。涉及此类纳米载体的纳米技术可以提高特异性,减少副作用,使正常细胞不受影响。本综述关注合成 QDs 的不同方法。QDs 可通过有机方法和合成方法获得。研究发现,自然合成的 QDs 比合成工艺更可行。合成 QDs 还出现了自上而下或自下而上的方法。QDs 可以通过非共价和共价结合的方式与抗体结合。共价结合比其他方法更可行。零长偶联起着重要作用,因为 EDC(1-乙基-3-乙基二甲基氨基丙基)碳二亚胺是一种强交联剂,被广泛用于偶联分子。抗体作为表面配体发挥作用,导致抗原与抗体相互作用,从而产生特异性靶向作用,而正常细胞则不受影响。细胞通过被动靶向或主动靶向吸收分子。QDs 是一种微小的无机纳米晶体,其大小和范围各不相同。根据不同的尺寸,它们会发出特定波长的光。它们具有自身的发光和光学特性,可对治疗药物进行监测、成像,并将其输送到体内的各种靶点。对 QDs 的表面进行修饰可增强其功能。它们是诊断、成像和输送治疗分子的工具。为了提高治疗效果,纳米技术通过被动靶向或主动靶向引导细胞吸收纳米粒子。它是一个重要的平台,不仅能进行成像和诊断,还有助于将治疗药物输送到特定部位。因此,本综述认为,目前的癌症治疗方案存在诸多弊端,最终导致治疗失败。因此,涉及这种纳米载体的纳米技术将成为克服传统治疗方法所有局限性的工具。这种方法有助于减少有效治疗所需的抗癌剂剂量,从而提高治疗指数。QDs 不仅能诊断疾病,还能将药物输送到癌症部位。
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引用次数: 0
Endogenous Ligands of TLR4 in Microglia: Potential Targets for Related Neurological Diseases. 小胶质细胞中 TLR4 的内源性配体:相关神经系统疾病的潜在靶点
IF 3 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 DOI: 10.2174/0113894501316051240821060249
Bo Chen, Bin Di

Chronic inflammation mediated by microglia is a cause of some neuroinflammatory diseases. TLR4, a natural immune receptor on microglia, plays an important role in the occurrence of inflammation and the process of diseases. TLR4 can be activated by a variety of ligands to trigger inflammatory responses, including endogenous ligands HMGB1, S100A8/9, Heme, and Fetuin-A. As ligands derived from the body itself, they have the ability to bind directly to TLR4 and can be used as inducers of aseptic inflammation. In the past 20 years, targeting ligands rather than receptors has become an emerging therapeutic strategy for the treatment of diseases, so understanding the relationship between microglia, TLR4, TLR4 ligands, and corresponding diseases may have new implications for the treatment of diseases. In the article, we will discuss the TLR4 and the endogenous substances that can activate the TLR4 signaling pathway and present literature support for their role in neuroinflammatory diseases.

由小胶质细胞介导的慢性炎症是某些神经炎症性疾病的病因之一。TLR4是小胶质细胞上的一种天然免疫受体,在炎症的发生和疾病的过程中发挥着重要作用。TLR4 可被多种配体激活,引发炎症反应,包括内源性配体 HMGB1、S100A8/9、血红素和 Fetuin-A。作为源自人体本身的配体,它们能够直接与 TLR4 结合,可用作无菌性炎症的诱导剂。在过去的 20 年中,靶向配体而非受体已成为治疗疾病的一种新兴治疗策略,因此了解小胶质细胞、TLR4、TLR4 配体和相应疾病之间的关系可能会对疾病的治疗产生新的影响。本文将讨论 TLR4 和可激活 TLR4 信号通路的内源性物质,并介绍其在神经炎症性疾病中作用的文献支持。
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引用次数: 0
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Current drug targets
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