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Gamma Secretase as an Important Drug Target for Management of Alzheimer's Disease: A Comprehensive Review. γ分泌酶作为治疗阿尔茨海默病的重要药物靶点:综述。
IF 3.4 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-01-01 DOI: 10.2174/0115680266259174231006070637
Fady Tadros Hakem, Youstina Farid Fouad, Reem K Arafa

Alzheimer's disease (AD) is a neurological disease that affects the memory. AD has been attributed to the aggregations of amyloid-β (Aβ) peptides which result in the formation of plaques that block the neuron-transferring process done by the brain memory cells. These plaques are formed upon cleavage of Amyloid Precursor Protein (APP) by Gamma-Secretase (GS). GS protein has around 141 substrates, the important two are APP and Notch. Considering one of the hot spots in AD research, we focused on GS and its relation to AD. Moreover, a lot of research was done on beta-secretase and drugs were developed to target it however, few drugs are established for GS. GS contains four subunits: Presenilin (PS), PEN-2, Nicastrin, and APH-1. The catalytic subunit is PS, which contains the active site for substrate binding, as well as the allosteric and docking sites. Both PEN-2 and APH-1 are regulators for the stability and activity of GS. Nicastrin, helps the substrates bind to the PS. Additionally, the role of the immuno-protein named "IFITM3" and how it affects the immune system and its relation to AD is presented. GS is one of the most studied proteins with many developed candidates as inhibitors (GSI) and modulators (GSM). Examples of GSI are Semagacestat and Avagacestat while GSM includes E2012; which inhibits the cleavage activity of GS. In this report, each of the four subunits of GS is described in detail, along with the interactions between GS and its inhibitors or modulators. In addition, the FDA-approved drugs are enlisted.

阿尔茨海默病(AD)是一种影响记忆的神经系统疾病。AD被归因于淀粉样蛋白-β(Aβ)肽的聚集,导致斑块的形成,从而阻断大脑记忆细胞的神经元转移过程。这些斑块是在γ分泌酶(GS)切割淀粉样前体蛋白(APP)时形成的。GS蛋白有大约141个底物,其中重要的两个是APP和Notch。考虑到AD研究的热点之一,我们重点研究了GS及其与AD的关系。此外,我们对β分泌酶进行了大量研究,并开发了针对它的药物。然而,很少有针对GS的药物。GS包含四个亚基:早老素(PS)、PEN-2、尼卡斯特林和APH-1。催化亚基是PS,它包含底物结合的活性位点,以及变构和对接位点。PEN-2和APH-1都是GS稳定性和活性的调节因子。尼卡斯特林有助于底物与PS结合。此外,还介绍了名为“IFITM3”的免疫蛋白的作用及其如何影响免疫系统及其与AD的关系。GS是研究最多的蛋白质之一,有许多候选的抑制剂(GSI)和调节剂(GSM)。GSI的例子是Semagacesta和Avagacesta,而GSM包括E2012;它抑制GS的切割活性。在本报告中,详细描述了GS的四个亚基中的每一个,以及GS与其抑制剂或调节剂之间的相互作用。此外,美国食品药品监督管理局批准的药物也被列入名单。
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引用次数: 0
Exploring the Potential of Natural Products as Antiparasitic Agents for Neglected Tropical Diseases. 探索天然产品作为被忽视的热带疾病的抗寄生虫剂的潜力。
IF 3.4 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-01-01 DOI: 10.2174/0115680266256963230921061925
Dayanna Orosco, Arturo René Mendoza, Carlos Mario Meléndez

Recent developments in the use of natural product-based molecules as antiparasitic agents for Malaria, leishmaniasis (LE), Chagas disease (CD), and Human African trypanosomiasis (HAT) are reviewed. The role of diverse plants in developing bioactive species is discussed in addition to analyzing the structural diversity of natural products as active agents and the diverse biological applications in CD, HAT, LE, and Malaria. This review focuses on medicinal chemistry, emphasizing the structural characteristics of natural molecules as bioactive agents against parasitic infections caused by Leishmania, Trypanosoma, and Plasmodium parasites.

综述了基于天然产物的分子作为抗寄生虫剂治疗疟疾、利什曼病(LE)、查加斯病(CD)和非洲锥虫病(HAT)的最新进展。除了分析作为活性剂的天然产物的结构多样性以及在CD、HAT、LE和疟疾中的不同生物学应用外,还讨论了不同植物在开发生物活性物种中的作用。这篇综述的重点是药物化学,强调天然分子作为生物活性剂对抗由利什曼原虫、锥虫和疟原虫引起的寄生虫感染的结构特征。
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引用次数: 0
Traditional uses, Phytochemistry, Pharmacology, and Toxicology of the Genus Artemisia L. (Asteraceae): A High-value Medicinal Plant. 蒿属植物(菊科)的传统用途、植物化学、药理学和毒理学:一种高价值药用植物。
IF 3.4 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-01-01 DOI: 10.2174/1568026623666230914104141
Manzoor Hussain, Rakesh Kr Thakur, Jabeena Khazir, Sajad Ahmed, Mohammad Imtiyaj Khan, Praveen Rahi, Latif Ahmad Peer, Pragadheesh Vppalayam Shanmugam, Satwinderjeet Kaur, Soom Nath Raina, Zafar Ahmad Reshi, Deepmala Sehgal, Vijay Rani Rajpal, Bilal Ahmad Mir

Biologically active secondary metabolites, essential oils, and volatile compounds derived from medicinal and aromatic plants play a crucial role in promoting human health. Within the large family Asteraceae, the genus Artemisia consists of approximately 500 species. Artemisia species have a rich history in traditional medicine worldwide, offering remedies for a wide range of ailments, such as malaria, jaundice, toothache, gastrointestinal problems, wounds, inflammatory diseases, diarrhoea, menstrual pains, skin disorders, headache, and intestinal parasites. The therapeutic potential of Artemisia species is derived from a multitude of phytoconstituents, including terpenoids, phenols, flavonoids, coumarins, sesquiterpene lactones, lignans, and alkaloids that serve as active pharmaceutical ingredients (API). The remarkable antimalarial, antimicrobial, anthelmintic, antidiabetic, anti-inflammatory, anticancer, antispasmodic, antioxidative and insecticidal properties possessed by the species are attributed to these APIs. Interestingly, several commercially utilized pharmaceutical drugs, including arglabin, artemisinin, artemether, artesunate, santonin, and tarralin have also been derived from different Artemisia species. However, despite the vast medicinal potential, only a limited number of Artemisia species have been exploited commercially. Further, the available literature on traditional and pharmacological uses of Artemisia lacks comprehensive reviews. Therefore, there is an urgent need to bridge the existing knowledge gaps and provide a scientific foundation for future Artemisia research endeavours. It is in this context, the present review aims to provide a comprehensive account of the traditional uses, phytochemistry, documented biological properties and toxicity of all the species of Artemisia and offers useful insights for practitioners and researchers into underutilized species and their potential applications. This review aims to stimulate further exploration, experimentation and collaboration to fully realize the therapeutic potential of Artemisia in augmenting human health and well-being.

从药用植物和芳香植物中提取的具有生物活性的次生代谢物、精油和挥发性化合物在促进人类健康方面发挥着至关重要的作用。在菊科植物中,蒿属植物约有 500 种。蒿属植物在全球传统医学中有着悠久的历史,可治疗多种疾病,如疟疾、黄疸、牙痛、肠胃问题、伤口、炎症、腹泻、痛经、皮肤病、头痛和肠道寄生虫。蒿属植物的治疗潜力来自于多种植物成分,包括萜类、酚类、黄酮类、香豆素类、倍半萜内酯类、木脂素类和生物碱类等活性药物成分(API)。该物种所具有的抗疟、抗菌、驱虫、抗糖尿病、抗炎、抗癌、解痉、抗氧化和杀虫等特性都归功于这些原料药。有趣的是,一些商业用药,包括阿格拉滨、青蒿素、蒿甲醚、青蒿琥酯、山托宁和塔拉林也是从不同的蒿属植物中提取的。然而,尽管青蒿具有巨大的药用潜力,但只有少数青蒿物种得到了商业开发。此外,关于青蒿的传统和药理用途的现有文献缺乏全面的综述。因此,迫切需要弥补现有的知识差距,为未来的青蒿研究工作奠定科学基础。正是在这种背景下,本综述旨在全面介绍所有青蒿物种的传统用途、植物化学、有文献记载的生物特性和毒性,为从业人员和研究人员了解未充分利用的物种及其潜在应用提供有用的见解。本综述旨在促进进一步的探索、实验和合作,以充分发挥青蒿在增进人类健康和福祉方面的治疗潜力。
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引用次数: 0
Use of Immunoglobulin Y Antibodies: Biosensor-based Diagnostic Systems and Prophylactic and Therapeutic Drug Delivery Systems for Viral Respiratory Diseases. 使用免疫球蛋白 Y 抗体:基于生物传感器的诊断系统以及病毒性呼吸道疾病的预防和治疗药物输送系统。
IF 2.9 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-01-01 DOI: 10.2174/0115680266289898240322073258
Yasemin Budama-Kilinc, Ozan Baris Kurtur, Bahar Gok, Nisanur Cakmakci, Serda Kecel-Gunduz, Necdet Mehmet Unel, Taylan Kurtulus Ozturk

Respiratory viruses have caused many pandemics from past to present and are among the top global public health problems due to their rate of spread. The recently experienced COVID-19 pandemic has led to an understanding of the importance of rapid diagnostic tests to prevent epidemics and the difficulties of developing new vaccines. On the other hand, the emergence of resistance to existing antiviral drugs during the treatment process poses a major problem for society and global health systems. Therefore, there is a need for new approaches for the diagnosis, prophylaxis, and treatment of existing or new types of respiratory viruses. Immunoglobulin Y antibodies (IgYs) obtained from the yolk of poultry eggs have significant advantages, such as high production volumes, low production costs, and high selectivity, which enable the development of innovative and strategic products. Especially in diagnosing respiratory viruses, antibody-based biosensors in which these antibodies are integrated have the potential to provide superiority in making rapid and accurate diagnosis as a practical diagnostic tool. This review article aims to provide information on using IgY antibodies in diagnostic, prophylactic, and therapeutic applications for respiratory viruses and to provide a perspective for future innovative applications.

从古至今,呼吸道病毒已造成多次大流行,并因其传播速度快而成为全球公共卫生的首要问题之一。最近发生的 COVID-19 大流行使人们认识到快速诊断检测对预防流行病的重要性以及开发新疫苗的困难。另一方面,在治疗过程中出现的对现有抗病毒药物的抗药性也给社会和全球卫生系统带来了重大问题。因此,需要新的方法来诊断、预防和治疗现有或新型呼吸道病毒。从禽蛋蛋黄中提取的免疫球蛋白 Y 抗体(IgYs)具有产量高、生产成本低、选择性强等显著优势,可用于开发创新型战略产品。特别是在诊断呼吸道病毒方面,集成了这些抗体的基于抗体的生物传感器有可能作为一种实用的诊断工具,在快速准确诊断方面提供优越性。这篇综述文章旨在介绍 IgY 抗体在呼吸道病毒诊断、预防和治疗中的应用,并为未来的创新应用提供展望。
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引用次数: 0
Stimuli-sensitive Chitosan-based Nanosystems-immobilized Nucleic Acids for Gene Therapy in Breast Cancer and Hepatocellular Carcinoma. 用于乳腺癌和肝细胞癌基因治疗的对刺激敏感的壳聚糖基纳米系统固定化核酸
IF 2.9 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-01-01 DOI: 10.2174/0115680266293173240506054439
Seyed Morteza Naghib, Bahar Ahmadi, M R Mozafari

Chitosan-based nanoparticles have emerged as a promising tool in the realm of cancer therapy, particularly for gene delivery. With cancer being a prevalent and devastating disease, finding effective treatment options is of utmost importance. These nanoparticles provide a unique solution by encapsulating specific genes and delivering them directly to cancer cells, offering immense potential for targeted therapy. The biocompatibility and biodegradability of chitosan, a naturally derived polymer, make it an ideal candidate for this purpose. The nanoparticles protect the genetic material during transportation and enhance its cellular uptake, ensuring effective delivery to the site of action. Furthermore, the unique properties of chitosan-based nanoparticles allow for the controlled release of genes, maximizing their therapeutic effect while minimizing adverse effects. By advancing the field of gene therapy through the use of chitosan-based nanoparticles, scientists are making significant strides toward more humane and personalized treatments for cancer patients.

壳聚糖基纳米粒子已成为癌症治疗领域的一种前景广阔的工具,尤其是用于基因递送。癌症是一种普遍存在的毁灭性疾病,因此找到有效的治疗方案至关重要。这些纳米颗粒提供了一种独特的解决方案,它们封装了特定基因并将其直接输送到癌细胞,为靶向治疗提供了巨大的潜力。壳聚糖是一种天然聚合物,其生物相容性和生物可降解性使其成为实现这一目的的理想候选材料。这种纳米颗粒在运输过程中保护遗传物质,并提高细胞对其的吸收率,从而确保将药物有效送达作用部位。此外,壳聚糖基纳米粒子的独特性能还能控制基因的释放,最大限度地提高治疗效果,同时将不良反应降至最低。通过使用壳聚糖基纳米粒子推进基因治疗领域的发展,科学家们在为癌症患者提供更加人性化和个性化的治疗方面取得了重大进展。
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引用次数: 0
Neurotrophic Factors in Cannabis-induced Psychosis: An Update. 大麻诱发精神病中的神经营养因子:最新进展。
IF 2.9 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-01-01 DOI: 10.2174/1568026623666230829152150
Valerio Ricci, Domenico de Berardis, Giovanni Martinotti, Giuseppe Maina

Background: Cannabis is the most widely used illicit substance. Numerous scientific evidence confirm the strong association between cannabis and psychosis. Exposure to cannabis can induce the development of psychosis and schizophrenia in vulnerable individuals. However, the neurobiological processes underlying this relationship are unknown. Neurotrophins are a class of proteins that serve as survival factors for central nervous system (CNS) neurons. In particular, Nerve Growth Factor (NGF) plays an important role in the survival and function of cholinergic neurons while Brain Derived Neurotrophic Factor (BDNF) is involved in synaptic plasticity and the maintenance of midbrain dopaminergic and cholinergic neurons. Glial Cell Derived Neurotrophic Factor (GDNF) promotes the survival of midbrain dopaminergic neurons and Neuregulin 1 (NrG- 1) contributes to glutamatergic signals regulating the N-methyl-D-aspartate (NMDA). They have a remarkable influence on the neurons involved in the Δ-9-THC (tethra-hydro-cannabinol) action, such as dopaminergic and glutamatergic neurons, and can play dual roles: first, in neuronal survival and death, and, second, in activity-dependent plasticity.

Methods: In this brief update, reviewing in a narrative way the relevant literature, we will focus on the effects of cannabis on this class of proteins, which may be implicated, at least in part, in the mechanism of the psychostimulant-induced neurotoxicity and psychosis.

Conclusion: Since altered levels of neurotrophins may participate in the pathogenesis of psychotic disorders which are common in drug users, one possible hypothesis is that repeated cannabis exposure can cause psychosis by interfering with neurotrophins synthesis and utilization by CNS neurons.

背景:大麻是使用最广泛的非法药物。大量科学证据证实,大麻与精神病之间存在密切联系。接触大麻会诱发易感人群患上精神病和精神分裂症。然而,这种关系的神经生物学过程尚不清楚。神经营养素是一类作为中枢神经系统(CNS)神经元生存因子的蛋白质。其中,神经生长因子(NGF)对胆碱能神经元的存活和功能起着重要作用,而脑衍生神经营养因子(BDNF)则参与突触可塑性以及中脑多巴胺能神经元和胆碱能神经元的维持。胶质细胞衍生神经营养因子(GDNF)可促进中脑多巴胺能神经元的存活,而神经胶质蛋白 1(NrG- 1)则有助于调节 N-甲基-D-天冬氨酸(NMDA)的谷氨酸能信号。它们对参与Δ-9-THC(tethra-hydro-cannabinol,四氢大麻酚)作用的神经元(如多巴胺能神经元和谷氨酸能神经元)有显著影响,并能发挥双重作用:首先是在神经元存活和死亡中,其次是在依赖活动的可塑性中:在这篇简短的最新报告中,我们将以叙述的方式回顾相关文献,重点讨论大麻对这一类蛋白质的影响,它们可能至少部分与精神刺激剂诱发神经毒性和精神病的机制有关:由于神经营养素水平的改变可能与吸毒者常见的精神病发病机制有关,一种可能的假设是,反复接触大麻会干扰中枢神经系统神经元合成和利用神经营养素,从而导致精神病。
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引用次数: 0
Evaluation of Thiazolidine Derivatives with Potential Anti-ZIKV Activity. 评估具有潜在抗 ZIKV 活性的噻唑烷衍生物
IF 2.9 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-01-01 DOI: 10.2174/0115680266315388240801053401
Sayonara Maria Calado Gonçalves, Lília Vieira Galdino, Morganna Costa Lima, José Arion da Silva Moura, Douglas Carvalho Francisco Viana, Michelle Melgarejo da Rosa, Luiz Felipe Gomes Rebello Ferreira, Marcelo Zaldini Hernandes, Michelly Cristiny Pereira, Moacyr Jesus Barreto de Melo Rêgo, Ivan da Rocha Pitta, Rafael de Oliveira França, Marina Galdino da Rocha Pitta, Maira Galdino da Rocha Pitta

Objective: In this study, we have synthesized 19 Thiazolidine (TZD) derivatives to investigate their potential anti-ZIKV effects.

Methods: Nineteen thiazolidine derivatives were synthesized and evaluated for their cytotoxicity and antiviral activity against the ZIKA virus.

Results: Among them, six demonstrated remarkable selectivity against the ZIKV virus, exhibiting IC50 values of <5μM, and the other compounds did not demonstrate selectivity for the virus. Interestingly, several derivatives effectively suppressed the replication of ZIKV RNA copies, with derivatives significantly reducing ZIKV mRNA levels at 24 hours post-infection (hpi). Notably, two derivatives (ZKC-4 and -9) stood out by demonstrating a protective effect against ZIKV cell entry. Informed by computational analysis of binding affinity and intermolecular interactions within the NS5 domain's N-7 and O'2 positions, ZKC-4 and FT-39 displayed the highest predicted affinities. Intriguingly, ZKC-4 and ZKC-9 derivatives exhibited the most favorable predicted binding affinities for the ZIKV-E binding site.

Conclusion: The significance of TZDs as potent antiviral agents is underscored by these findings, suggesting that exploring TZD derivatives holds promise for advancing antiviral therapeutic strategies.

研究目的在这项研究中,我们合成了 19 种噻唑烷(TZD)衍生物,以研究它们潜在的抗 ZIKV 作用:方法:合成了 19 种噻唑烷衍生物,并评估了它们对 ZIKA 病毒的细胞毒性和抗病毒活性:结果:其中六种噻唑烷衍生物对 ZIKV 病毒具有显著的选择性,其 IC50 值为 结论:噻唑烷衍生物对 ZIKV 病毒的细胞毒性和抗病毒活性具有重要意义:这些发现凸显了 TZDs 作为强效抗病毒药物的重要性,表明探索 TZD 衍生物有望推进抗病毒治疗策略。
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引用次数: 0
Current Status of Hedgehog Signaling Inhibitors. 刺猬信号抑制剂的现状。
IF 3.4 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-01-01 DOI: 10.2174/0115680266280850231221074340
Xiaotang Wang, Tian Wang, Xiaona Song, Jiping Gao, Guoqiang Xu, Yunhui Ma, Guohua Song

The Hedgehog (Hh) signaling pathway plays a crucial role in diverse biological processes such as cell differentiation, proliferation, senescence, tumorigenesis, malignant transformation, and drug resistance. Aberrant Hh signaling, resulting from mutations and excessive activation, can contribute to the development of various diseases during different stages of biogenesis and development. Moreover, it has been linked to unfavorable outcomes in several human cancers, including basal cell carcinoma (BCC), multiple myeloma (MM), melanoma, and breast cancer. Hence, the presence of mutations and excessive activation of the Hh pathway presents obstacles and constraints in the realm of cancer treatment. Extant research has demonstrated that small molecule inhibitors are regarded as the most effective therapeutic approaches for targeting the Hh pathway in contrast to traditional chemotherapy and radiotherapy. Consequently, this review focuses on the present repertoire of small molecule inhibitors that target various components of the Hh pathway, including Hh ligands, Ptch receptors, Smo transmembrane proteins, and Gli nuclear transcription factors. This study provides a comprehensive analysis of small molecules' structural and functional aspects in the preclinical and clinical management of cancer. Additionally, it elucidates the obstacles encountered in targeting the Hh pathway for human cancer therapy and proposes potential therapeutic approaches.

刺猬(Hh)信号通路在细胞分化、增殖、衰老、肿瘤发生、恶性转化和耐药性等多种生物学过程中发挥着至关重要的作用。突变和过度作用导致的 Hh 信号转导异常可在生物生成和发育的不同阶段导致各种疾病的发生。此外,它还与基底细胞癌(BCC)、多发性骨髓瘤(MM)、黑色素瘤和乳腺癌等多种人类癌症的不良后果有关。因此,Hh 通路的突变和过度激活给癌症治疗带来了障碍和限制。现有研究表明,与传统的化疗和放疗相比,小分子抑制剂被认为是靶向 Hh 通路的最有效治疗方法。因此,本综述重点介绍了目前针对 Hh 通路各种成分的小分子抑制剂,包括 Hh 配体、Ptch 受体、Smo 跨膜蛋白和 Gli 核转录因子。本研究全面分析了小分子在癌症临床前和临床治疗中的结构和功能方面。此外,它还阐明了针对 Hh 通路进行人类癌症治疗所遇到的障碍,并提出了潜在的治疗方法。
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引用次数: 0
Effect of Withaferin-A, Withanone, and Caffeic Acid Phenethyl Ester on DNA Methyltransferases: Potential in Epigenetic Cancer Therapy. Withaferin-A、Withanone 和咖啡酸苯乙酯对 DNA 甲基转移酶的影响:表观遗传学癌症疗法的潜力。
IF 3.4 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-01-01 DOI: 10.2174/1568026623666230726105017
Vipul Kumar, Jaspreet Kaur Dhanjal, Anissa Nofita Sari, Mallika Khurana, Sunil C Kaul, Renu Wadhwa, Durai Sundar

Background: DNA methyltransferases (DNMTs) have been reported to be potential drug targets in various cancers. The major hurdle in inhibiting DNMTs is the lack of knowledge about different DNMTs and their role in the hypermethylation of gene promoters in cancer cells. Lack of information on specificity, stability, and higher toxicity of previously reported DNMT inhibitors is the major reason for inadequate epigenetic cancer therapy. DNMT1 and DNMT3A are the two DNMTs that are majorly overexpressed in cancers.

Objective: In this study, we have presented computational and experimental analyses of the potential of some natural compounds, withaferin A (Wi-A), withanone (Wi-N), and caffeic acid phenethyl ester (CAPE), as DNMT inhibitors, in comparison to sinefungin (SFG), a known dual inhibitor of DNMT1 and DNMT3A.

Methods: We used classical simulation methods, such as molecular docking and molecular dynamics simulations, to investigate the binding potential and properties of the test compounds with DNMT1 and DNMT3A. Cell culture-based assays were used to investigate the inactivation of DNMTs and the resulting hypomethylation of the p16INK4A promoter, a key tumour suppressor that is inactivated by hypermethylation in cancer cells, resulting in upregulation of its expression.

Results: Among the three test compounds (Wi-A, Wi-N, and CAPE), Wi-A showed the highest binding affinity to both DNMT1 and DNMT3A; CAPE showed the highest affinity to DNMT3A, and Wi-N showed a moderate affinity interaction with both. The binding energies of Wi-A and CAPE were further compared with SFG. Expression analysis of DNMTs showed no difference between control and treated cells. Cell viability and p16INK4A expression analysis showed a dose-dependent decrease in viability, an increase in p16INK4A, and a stronger effect of Wi-A compared to Wi-N and CAPE.

Conclusion: The study demonstrated the differential binding ability of Wi-A, Wi-N, and CAPE to DNMT1 and DNMT3A, which was associated with their inactivation, leading to hypomethylation and desilencing of the p16INK4A tumour suppressor in cancer cells. The test compounds, particularly Wi-A, have the potential for cancer therapy.

背景:据报道,DNA 甲基转移酶(DNMTs)是各种癌症的潜在药物靶点。抑制 DNMTs 的主要障碍是缺乏对不同 DNMTs 及其在癌细胞基因启动子超甲基化中作用的了解。缺乏有关特异性、稳定性和先前报道的 DNMT 抑制剂毒性较高的信息,是表观遗传癌症疗法不充分的主要原因。DNMT1和DNMT3A是癌症中主要过度表达的两种DNMT:在这项研究中,我们通过计算和实验分析了一些天然化合物(withaferin A (Wi-A)、withanone (Wi-N)和咖啡酸苯乙酯 (CAPE))作为 DNMT 抑制剂的潜力,并与已知的 DNMT1 和 DNMT3A 双重抑制剂正弦霉素 (SFG) 进行了比较:方法:我们采用分子对接和分子动力学模拟等经典模拟方法研究了测试化合物与 DNMT1 和 DNMT3A 的结合潜力和特性。利用基于细胞培养的实验研究了DNMTs的失活及其导致的p16INK4A启动子的低甲基化,p16INK4A是一种关键的肿瘤抑制因子,在癌细胞中因高甲基化而失活,导致其表达上调:在三种测试化合物(Wi-A、Wi-N和CAPE)中,Wi-A与DNMT1和DNMT3A的结合亲和力最高;CAPE与DNMT3A的结合亲和力最高;Wi-N与DNMT1和DNMT3A的结合亲和力中等。Wi-A 和 CAPE 的结合能与 SFG 进行了进一步比较。DNMTs的表达分析表明,对照细胞和处理过的细胞之间没有差异。细胞存活率和 p16INK4A 表达分析表明,与 Wi-N 和 CAPE 相比,Wi-A 会导致细胞存活率呈剂量依赖性下降,p16INK4A 会增加,而且 Wi-A 的作用更强:研究表明,Wi-A、Wi-N和CAPE与DNMT1和DNMT3A的结合能力不同,这与它们的失活有关,从而导致癌细胞中p16INK4A肿瘤抑制因子的低甲基化和去丝氨酸化。测试化合物,尤其是 Wi-A 具有治疗癌症的潜力。
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引用次数: 0
Combating COVID-19 Crisis using Artificial Intelligence (AI) Based Approach: Systematic Review. 利用基于人工智能(AI)的方法应对 COVID-19 危机:系统回顾。
IF 3.4 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-01-01 DOI: 10.2174/0115680266282179240124072121
Kavya Singh, Navjeet Kaur, Ashish Prabhu

Background: SARS-CoV-2, the unique coronavirus that causes COVID-19, has wreaked damage around the globe, with victims displaying a wide range of difficulties that have encouraged medical professionals to look for innovative technical solutions and therapeutic approaches. Artificial intelligence-based methods have contributed a significant part in tackling complicated issues, and some institutions have been quick to embrace and tailor these solutions in response to the COVID-19 pandemic's obstacles. Here, in this review article, we have covered a few DL techniques for COVID-19 detection and diagnosis, as well as ML techniques for COVID-19 identification, severity classification, vaccine and drug development, mortality rate prediction, contact tracing, risk assessment, and public distancing. This review illustrates the overall impact of AI/ML tools on tackling and managing the outbreak.

Purpose: The focus of this research was to undertake a thorough evaluation of the literature on the part of Artificial Intelligence (AI) as a complete and efficient solution in the battle against the COVID-19 epidemic in the domains of detection and diagnostics of disease, mortality prediction and vaccine as well as drug development.

Methods: A comprehensive exploration of PubMed, Web of Science, and Science Direct was conducted using PRISMA (Preferred Reporting Items for Systematic Reviews and Meta-Analysis) regulations to find all possibly suitable papers conducted and made publicly available between December 1, 2019, and August 2023. COVID-19, along with AI-specific words, was used to create the query syntax.

Results: During the period covered by the search strategy, 961 articles were published and released online. Out of these, a total of 135 papers were chosen for additional investigation. Mortality rate prediction, early detection and diagnosis, vaccine as well as drug development, and lastly, incorporation of AI for supervising and controlling the COVID-19 pandemic were the four main topics focused entirely on AI applications used to tackle the COVID-19 crisis. Out of 135, 60 research papers focused on the detection and diagnosis of the COVID-19 pandemic. Next, 19 of the 135 studies applied a machine-learning approach for mortality rate prediction. Another 22 research publications emphasized the vaccine as well as drug development. Finally, the remaining studies were concentrated on controlling the COVID-19 pandemic by applying AI AI-based approach to it.

Conclusion: We compiled papers from the available COVID-19 literature that used AI-based methodologies to impart insights into various COVID-19 topics in this comprehensive study. Our results suggest crucial characteristics, data types, and COVID-19 tools that can aid in medical and translational research facilitation.

背景:SARS-CoV-2 是一种导致 COVID-19 的独特冠状病毒,它在全球范围内造成了破坏,受害者表现出各种各样的困难,这促使医疗专业人员寻找创新的技术解决方案和治疗方法。以人工智能为基础的方法在解决复杂问题方面做出了重要贡献,一些机构已迅速接受并定制了这些解决方案,以应对 COVID-19 大流行带来的障碍。在这篇综述文章中,我们介绍了一些用于 COVID-19 检测和诊断的 DL 技术,以及用于 COVID-19 识别、严重程度分类、疫苗和药物开发、死亡率预测、接触者追踪、风险评估和公众疏远的 ML 技术。本综述说明了人工智能/ML 工具对应对和管理疫情的整体影响。目的:本研究的重点是对人工智能(AI)作为应对 COVID-19 疫情的完整、高效解决方案的文献进行全面评估,涉及疾病检测和诊断、死亡率预测、疫苗和药物开发等领域:方法:采用PRISMA(系统综述和Meta分析首选报告项目)规定,对PubMed、Web of Science和Science Direct进行了全面探索,以找到2019年12月1日至2023年8月期间公开发表的所有可能合适的论文。COVID-19以及人工智能专用词被用来创建查询语法:在搜索策略覆盖的时间段内,共有 961 篇文章在网上发表和发布。其中,共有 135 篇论文被选中进行进一步调查。死亡率预测、早期检测和诊断、疫苗和药物开发,以及最后,将人工智能用于监督和控制 COVID-19 大流行,这四个主题完全集中在用于应对 COVID-19 危机的人工智能应用上。在 135 篇研究论文中,有 60 篇侧重于 COVID-19 大流行病的检测和诊断。其次,135 项研究中有 19 项采用了机器学习方法来预测死亡率。另有 22 篇研究论文强调了疫苗和药物的开发。最后,其余的研究集中于通过应用基于人工智能的 AI 方法来控制 COVID-19 大流行:在这项综合研究中,我们汇编了现有 COVID-19 文献中使用基于人工智能的方法对各种 COVID-19 主题进行深入研究的论文。我们的研究结果表明,COVID-19 的关键特征、数据类型和工具有助于医学研究和转化研究。
{"title":"Combating COVID-19 Crisis using Artificial Intelligence (AI) Based Approach: Systematic Review.","authors":"Kavya Singh, Navjeet Kaur, Ashish Prabhu","doi":"10.2174/0115680266282179240124072121","DOIUrl":"10.2174/0115680266282179240124072121","url":null,"abstract":"<p><strong>Background: </strong>SARS-CoV-2, the unique coronavirus that causes COVID-19, has wreaked damage around the globe, with victims displaying a wide range of difficulties that have encouraged medical professionals to look for innovative technical solutions and therapeutic approaches. Artificial intelligence-based methods have contributed a significant part in tackling complicated issues, and some institutions have been quick to embrace and tailor these solutions in response to the COVID-19 pandemic's obstacles. Here, in this review article, we have covered a few DL techniques for COVID-19 detection and diagnosis, as well as ML techniques for COVID-19 identification, severity classification, vaccine and drug development, mortality rate prediction, contact tracing, risk assessment, and public distancing. This review illustrates the overall impact of AI/ML tools on tackling and managing the outbreak.</p><p><strong>Purpose: </strong>The focus of this research was to undertake a thorough evaluation of the literature on the part of Artificial Intelligence (AI) as a complete and efficient solution in the battle against the COVID-19 epidemic in the domains of detection and diagnostics of disease, mortality prediction and vaccine as well as drug development.</p><p><strong>Methods: </strong>A comprehensive exploration of PubMed, Web of Science, and Science Direct was conducted using PRISMA (Preferred Reporting Items for Systematic Reviews and Meta-Analysis) regulations to find all possibly suitable papers conducted and made publicly available between December 1, 2019, and August 2023. COVID-19, along with AI-specific words, was used to create the query syntax.</p><p><strong>Results: </strong>During the period covered by the search strategy, 961 articles were published and released online. Out of these, a total of 135 papers were chosen for additional investigation. Mortality rate prediction, early detection and diagnosis, vaccine as well as drug development, and lastly, incorporation of AI for supervising and controlling the COVID-19 pandemic were the four main topics focused entirely on AI applications used to tackle the COVID-19 crisis. Out of 135, 60 research papers focused on the detection and diagnosis of the COVID-19 pandemic. Next, 19 of the 135 studies applied a machine-learning approach for mortality rate prediction. Another 22 research publications emphasized the vaccine as well as drug development. Finally, the remaining studies were concentrated on controlling the COVID-19 pandemic by applying AI AI-based approach to it.</p><p><strong>Conclusion: </strong>We compiled papers from the available COVID-19 literature that used AI-based methodologies to impart insights into various COVID-19 topics in this comprehensive study. Our results suggest crucial characteristics, data types, and COVID-19 tools that can aid in medical and translational research facilitation.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":3.4,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139691468","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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Current topics in medicinal chemistry
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