European Journal of Medicinal Chemistry Reports最新文献

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Fabrication, characterization and transdermal properties of double cross-linked gel beads with 4-n-butylresorcinol 含有 4-正丁基间苯二酚的双交联凝胶珠的制造、表征和透皮特性
European Journal of Medicinal Chemistry Reports Pub Date : 2024-10-18 DOI: 10.1016/j.ejmcr.2024.100232
Faxin Zhang , Mengsi Yin , Wanhui Shao , Xinyi Li , Hongmen Ren , Xianglong Wang , Mengju Xu , Qianchan Pang , Yan Cheng , Jianjun Xue , Haijie Hu , Mingyuan Li
{"title":"Fabrication, characterization and transdermal properties of double cross-linked gel beads with 4-n-butylresorcinol","authors":"Faxin Zhang ,&nbsp;Mengsi Yin ,&nbsp;Wanhui Shao ,&nbsp;Xinyi Li ,&nbsp;Hongmen Ren ,&nbsp;Xianglong Wang ,&nbsp;Mengju Xu ,&nbsp;Qianchan Pang ,&nbsp;Yan Cheng ,&nbsp;Jianjun Xue ,&nbsp;Haijie Hu ,&nbsp;Mingyuan Li","doi":"10.1016/j.ejmcr.2024.100232","DOIUrl":"10.1016/j.ejmcr.2024.100232","url":null,"abstract":"<div><div>In this paper, sodium alginate (SA) -agarose double cross-linked gel beads were prepared to improve the solubility of 4-n-butylresorcinol and to reduce skin irritation. The wrappage material suitable for 4-nBR gel beads was SA-agarose double cross-linking material, and the internal inclusions were in the form of 4-n-butylresorcinol nanoemulsions (4-nBR NEs). Under the orthogonal fluorescence microscope, it was observed that the gel beads were spherical in shape, with smooth and rounded surfaces and permeable interiors. The encapsulation rate of the gel beads was 84.37 ± 3.56 %, and the average diameter was 1.93 ± 0.21 mm. Scanning electron microscopy showed that the gel beads were spherical in shape. The cumulative leakage rate of the gel beads on the 35 th day was 4.72 ± 0.06 %, suggesting that the gel beads encapsulated 4-butylresorcinol to good effect and with high stability. This proves that the gel beads wrapped with 4-nBR are highly effective and stable. <em>In vitro</em> skin permeability assessment verified the good skin permeability of nanoemulsions (NEs).</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100232"},"PeriodicalIF":0.0,"publicationDate":"2024-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142579016","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Harnessing bio-waste for biomedical applications: A new horizon in sustainable healthcare 利用生物废物进行生物医学应用:可持续医疗保健的新视野
European Journal of Medicinal Chemistry Reports Pub Date : 2024-10-18 DOI: 10.1016/j.ejmcr.2024.100234
Mehrab Pourmadadi , Ali Aslani , Roghaieh Holghoomi , Sonia Fathi-karkan , Abbas Rahdar , Zelal Kharaba , Sadanand Pandey
{"title":"Harnessing bio-waste for biomedical applications: A new horizon in sustainable healthcare","authors":"Mehrab Pourmadadi ,&nbsp;Ali Aslani ,&nbsp;Roghaieh Holghoomi ,&nbsp;Sonia Fathi-karkan ,&nbsp;Abbas Rahdar ,&nbsp;Zelal Kharaba ,&nbsp;Sadanand Pandey","doi":"10.1016/j.ejmcr.2024.100234","DOIUrl":"10.1016/j.ejmcr.2024.100234","url":null,"abstract":"<div><div>Recent studies have focused on exploring the potential biomedical applications of compounds derived from bio-waste, responding to growing environmental concerns and the need for sustainable practices in healthcare. This review examines a wide range of bio-waste materials, including coffee extracts, banana peels, rice husks, chickpea peels, and pineapple peels, with the intention of determining their potential for use in the production of biomedical devices. The distinctive properties of these bio-waste materials are highlighted, including their antioxidative and antimicrobial characteristics, as well as their capacity to generate environmentally friendly nanoparticles. The sustainable synthesis of nanoparticles such as zinc oxide and silver facilitates the development of eco-friendly alternatives, which could be applied in various biomedical fields, including drug delivery systems, biosensors, and cancer therapy. Utilizing bio-waste not only provides an innovative avenue for advanced medical technologies but also aligns with the principles of sustainable healthcare by reducing waste and minimizing the environmental footprint of biomedical production. However, challenges remain in achieving standardization, reproducibility of outcomes, and securing necessary regulatory approvals. Future interdisciplinary collaborations should prioritize sustainability and nanotechnology to fully exploit the potential of bio-sourced materials in the biomedical sector.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100234"},"PeriodicalIF":0.0,"publicationDate":"2024-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142532745","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
MolAnchor method for explaining compound predictions based on substructures 基于子结构解释化合物预测的 MolAnchor 方法
European Journal of Medicinal Chemistry Reports Pub Date : 2024-10-15 DOI: 10.1016/j.ejmcr.2024.100230
Alec Lamens , Jürgen Bajorath
{"title":"MolAnchor method for explaining compound predictions based on substructures","authors":"Alec Lamens ,&nbsp;Jürgen Bajorath","doi":"10.1016/j.ejmcr.2024.100230","DOIUrl":"10.1016/j.ejmcr.2024.100230","url":null,"abstract":"<div><div>In medicinal chemistry, the impact of machine learning remains limited if predictions are not understood, which often precludes experimental follow-up. Therefore, chemically intuitive approaches that aid in model understanding and interpretation at the molecular level of detail are sought after. While feature attribution methods quantifying feature importance for model decisions are widely used in many areas, they must typically be combined with visualization techniques, if possible, to render the results accessible from a chemical viewpoint. On the other hand, there are approaches such as counterfactuals that yield closely related chemical structures with different prediction outcomes, providing direct access to structural features that critically influence model decisions. Herein, we introduce another approach designed to rationalize chemical predictions based on molecular structure. Therefore, we adapt principles underlying the anchor concept from explainable artificial intelligence (XAI) and alter them for molecular machine learning. The resulting method, termed MolAnchor, systematically identifies substructures in test compounds that determine property predictions, thus ensuring chemical interpretability. The MolAnchor methodology is made freely available to the medicinal chemistry community as a part of our study.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100230"},"PeriodicalIF":0.0,"publicationDate":"2024-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142442386","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovering bioactive phytoconstituents from Citrullus lanatus for antimicrobial and antioxidants therapeutic applications 从南瓜中发现具有生物活性的植物成分,用于抗菌和抗氧化治疗
European Journal of Medicinal Chemistry Reports Pub Date : 2024-10-15 DOI: 10.1016/j.ejmcr.2024.100229
Lakshmana Nakkalagadda Venkataravana, Jagadesh Uppin, Nikhitha Chinna Ramanjineyulu, Poojitha Gowribidanur Krishna, Jayaram Lakshmaiah Narayana
{"title":"Discovering bioactive phytoconstituents from Citrullus lanatus for antimicrobial and antioxidants therapeutic applications","authors":"Lakshmana Nakkalagadda Venkataravana,&nbsp;Jagadesh Uppin,&nbsp;Nikhitha Chinna Ramanjineyulu,&nbsp;Poojitha Gowribidanur Krishna,&nbsp;Jayaram Lakshmaiah Narayana","doi":"10.1016/j.ejmcr.2024.100229","DOIUrl":"10.1016/j.ejmcr.2024.100229","url":null,"abstract":"<div><div>In recent decades, significant interest in natural bioactive compounds has led many researchers to study plants as primary natural sources of bioactive compounds, mainly when considering a few biological properties, including antioxidant, antimicrobial, and anti-inflammatory activities, and as nutritional supplements with health benefits. We designed this study to explore the phytochemicals profiling of <em>Citrallus lanatus</em> and evaluate their <em>in vitro</em> bioactive properties<em>.</em> The methanol extraction of the watermelon's stem, rind, and leaf parts through Soxhlet extraction was analyzed using Gas Chromatography-Mass Spectrometry. The GC-MS profiling of <em>Citrullus lanatus</em> examines the presence of numerous bioactive phytoconstituents with potential biological activities such as antioxidant, anti-inflammatory, antimicrobial, anticancer, and other properties. We have evidenced that the stem, rind, and leaf extracts with significant antioxidant and antimicrobial activities against clinically relevant pathogens like <em>Salmonella typhi</em>, <em>Pseudomonas aeruginosa</em>, <em>Bacillus subtilis</em>, and <em>Staphylococcus aureus</em>. Overall, our study sheds light on exploring novel bioactive phytoconstituents from C<em>itrullus lanatus</em> and explore, harness these compounds' therapeutic potential for human health.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100229"},"PeriodicalIF":0.0,"publicationDate":"2024-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142532746","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Combination of heme oxygenase-1 inhibitors and temozolomide to improve the anticancer effect in glioblastoma 血红素加氧酶-1抑制剂与替莫唑胺联合使用提高胶质母细胞瘤的抗癌效果
European Journal of Medicinal Chemistry Reports Pub Date : 2024-10-09 DOI: 10.1016/j.ejmcr.2024.100227
Sebastiano Intagliata , Valeria Ciaffaglione , Valeria Consoli , Agata Grazia D'Amico , Luca Vanella , Valeria Pittalà , Federica Sodano , Marica Erminia Schiano , Valeria Sorrenti , Loredana Salerno
{"title":"Combination of heme oxygenase-1 inhibitors and temozolomide to improve the anticancer effect in glioblastoma","authors":"Sebastiano Intagliata ,&nbsp;Valeria Ciaffaglione ,&nbsp;Valeria Consoli ,&nbsp;Agata Grazia D'Amico ,&nbsp;Luca Vanella ,&nbsp;Valeria Pittalà ,&nbsp;Federica Sodano ,&nbsp;Marica Erminia Schiano ,&nbsp;Valeria Sorrenti ,&nbsp;Loredana Salerno","doi":"10.1016/j.ejmcr.2024.100227","DOIUrl":"10.1016/j.ejmcr.2024.100227","url":null,"abstract":"<div><div>Heme oxygenase-1 (HO-1) is involved in the oncogenesis of glioblastoma (GBM). In this work, we investigated for the first time how the co-administration (combo) of the HO-1 inhibitors <strong>SI1/09</strong> or <strong>LS6/42</strong> with temozolomide (<strong>TMZ</strong>) or temozolomide acid (<strong>TMZ Ac</strong>) may influence the proliferation of U87MG GBM cell lines. Moreover, two novel TMZ/HO-1 inhibitors codrugs <strong>LS8/21</strong> and <strong>LS8/24</strong> were synthesised, characterised and tested. Results indicate that the combos <strong>TMZ</strong> or <strong>TMZ Ac</strong> with <strong>LS6/42</strong>, as well as the corresponding <strong>LS8/24</strong>, are more efficacious in reducing U87MG cell proliferation with respect to reference drugs, allowing a possible reduction of the <strong>TMZ</strong> dosage and related side effects in clinical practice. The chemical and enzymatic stability of the most potent codrug <strong>LS8/24</strong> was evaluated. The observed high potency performed by both combos and <strong>LS8/24</strong> in cells suggests that HO-1 inhibition may give additional contribution to the antiproliferative effect of <strong>TMZ</strong>.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100227"},"PeriodicalIF":0.0,"publicationDate":"2024-10-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142418306","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Combinational delivery of berbamine and 5-fluorouracil in cerium oxide nanoparticles for colon cancer therapy: Insights from in vitro and in silico studies 氧化铈纳米颗粒中的伯胺和 5-氟尿嘧啶联合给药用于结肠癌治疗:体外和硅学研究的启示
European Journal of Medicinal Chemistry Reports Pub Date : 2024-10-08 DOI: 10.1016/j.ejmcr.2024.100224
Sneha Shriparna Satpathy , Sweta Mishra , Saswati Pattnaik, Chandana Mohanty
{"title":"Combinational delivery of berbamine and 5-fluorouracil in cerium oxide nanoparticles for colon cancer therapy: Insights from in vitro and in silico studies","authors":"Sneha Shriparna Satpathy ,&nbsp;Sweta Mishra ,&nbsp;Saswati Pattnaik,&nbsp;Chandana Mohanty","doi":"10.1016/j.ejmcr.2024.100224","DOIUrl":"10.1016/j.ejmcr.2024.100224","url":null,"abstract":"<div><div>Colon cancer is traditionally treated by an antimetabolite drug 5-fluorouracil (5FU) but has been linked to several drawbacks and systemic toxicity. To overcome drug associated toxicity, combination therapy is a promising strategy that synergistically enhances the therapeutic effects of co-delivered drugs while minimizing administration doses. Therefore, the current study aims to investigate the anti-colon cancer potency of 5FU co-delivered with a phytochemical i.e., berbamine (BERB) in a Cerium oxide nanoparticles (CONPs) delivery system. CONPs loaded 5FU (5FU-CONPs) and BERB (BERB-CONPs) were prepared and characterized using different analytical techniques. Successful entrapment of both drugs into CONPs formulations was detected under X-ray diffraction (XRD) observations. Drug-loaded CONPs in combination showed effective anti-oxidant activity by preventing reactive oxygen species (ROS) generations and had superior cytotoxic effects on HT-29 cell lines compared to treatment with native drugs singly or in combination. They also triggered apoptosis through p21, p53, Bax upregulation, and Bcl-2 downregulation, as confirmed by western blot studies. Additionally, <em>in silico</em> analysis was performed using molecular docking and molecular dynamics simulation (MDS) to validate the <em>in vitro</em> results. Results of the study suggest that 5FU and BERB CONPs in combination could be taken as a possible therapeutic approach for colon cancer treatment.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100224"},"PeriodicalIF":0.0,"publicationDate":"2024-10-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142418305","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Anticancer α-, γ-, and δ-carboline derivatives: structures, mechanisms of action, and SARs 抗癌 α-、γ- 和 δ-咔啉衍生物:结构、作用机制和 SARs
European Journal of Medicinal Chemistry Reports Pub Date : 2024-10-04 DOI: 10.1016/j.ejmcr.2024.100221
Jingliang Cui, Wanru Gao, Ziwei Liu, Shuang Cao, Sihui Long
{"title":"Anticancer α-, γ-, and δ-carboline derivatives: structures, mechanisms of action, and SARs","authors":"Jingliang Cui,&nbsp;Wanru Gao,&nbsp;Ziwei Liu,&nbsp;Shuang Cao,&nbsp;Sihui Long","doi":"10.1016/j.ejmcr.2024.100221","DOIUrl":"10.1016/j.ejmcr.2024.100221","url":null,"abstract":"<div><div>Carboline consists of a pyridine ring fused with an indole skeleton, and it serves as a potential drug scaffold. Depending on the relative position of the pyridine N to the indole N, carbolines can be categorized into <em>α-, β-, γ-,</em> and <em>δ</em>-subfamilies. They have diverse pharmacological activities, such as anticancer, antimalaria, antibacterial, antifungal, anti-Alzheimer's disease, etc. Among them, <em>β</em>-carbolines are the most widely studied and are also well reviewed. Herein, we review the anticancer activity of <em>α-, γ-,</em> and <em>δ</em>-carboline natural products and their synthetic derivatives, as they provide new inroads for cancer therapy. Particularly, we highlight the new derivatives of <em>α-, γ-,</em> and <em>δ</em>-carboline with anticancer activity, and their anticancer mechanisms, as well as structure-activity relationship. Meanwhile, we propose strategies for the development of new <em>α-</em>, <em>γ-</em>, and <em>δ</em>-carboline derivatives for cancer therapy.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100221"},"PeriodicalIF":0.0,"publicationDate":"2024-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142418786","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A review on progress of thiazole derivatives as potential anti-inflammatory agents 噻唑衍生物作为潜在抗炎剂的研究进展综述
European Journal of Medicinal Chemistry Reports Pub Date : 2024-10-04 DOI: 10.1016/j.ejmcr.2024.100225
Kereyagalahally H. Narasimhamurthy , Toreshettahally R. Swaroop , Kanchugarakoppal S. Rangappa
{"title":"A review on progress of thiazole derivatives as potential anti-inflammatory agents","authors":"Kereyagalahally H. Narasimhamurthy ,&nbsp;Toreshettahally R. Swaroop ,&nbsp;Kanchugarakoppal S. Rangappa","doi":"10.1016/j.ejmcr.2024.100225","DOIUrl":"10.1016/j.ejmcr.2024.100225","url":null,"abstract":"<div><div>Inflammation is a body response against infection that activates other biological components that include various cytokines, chemokines and other biological compounds that trigger body response against pathological activities. The Arachidonic acid pathway is involved in the inflammation that is connected with lipoxygenase (LOX) and cyclooxygenase (COX) enzymes. The importance of the isoforms of LOX and COX in inflammation is well studied. At the cellular level, some of the thiazole derivatives showed potent anti-inflammatory activities especially to block LOX5 and COX2 in the inflammation. These factors include both acute and chronic inflammation in various tissues like the heart, kidney, pancreas, brain, intestine, lungs and other organs as well that lead to the damage of the organs or cells. Whether it's the infectious or non-infectious response it will further activate some of the downstream signaling pathways like lipoxygenase, cyclooxygenase, cytochrome 450, JAK-STAT, MAPK, JNK, TNF-α, Nfr2, and many more pathways that lead to activation of another chronic disease in the body. In this review, we will concentrate on thiazole molecules that serve as anti-inflammatory responses to both acute and chronic inflammation. Further, we discussed the evidence that correlates the possible connection with LOX and COX enzymes in the inflammatory pathways and their blocking ability especially through thiazole derivatives has been discussed in this present review. The current assessment is the best part of the present consequence of thiazole derivatives on anti-inflammatory studies, covering articles published from 1973 to 2023.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100225"},"PeriodicalIF":0.0,"publicationDate":"2024-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142418785","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovery of novel favipiravir derivatives with improved pharmacokinetic properties as anti-SFTSV agents 发现具有更好药代动力学特性的新型法非拉韦衍生物作为抗 SFTSV 药物
European Journal of Medicinal Chemistry Reports Pub Date : 2024-10-04 DOI: 10.1016/j.ejmcr.2024.100226
Xiaomeng He , Fan Wu , Wei Li , Runze Zhang , Ruiyang Sun , Zhihong Hu , Wu Zhong , Manli Wang
{"title":"Discovery of novel favipiravir derivatives with improved pharmacokinetic properties as anti-SFTSV agents","authors":"Xiaomeng He ,&nbsp;Fan Wu ,&nbsp;Wei Li ,&nbsp;Runze Zhang ,&nbsp;Ruiyang Sun ,&nbsp;Zhihong Hu ,&nbsp;Wu Zhong ,&nbsp;Manli Wang","doi":"10.1016/j.ejmcr.2024.100226","DOIUrl":"10.1016/j.ejmcr.2024.100226","url":null,"abstract":"<div><div>Favipiravir is a nucleobase analogue that exhibits antiviral activities against a variety of RNA viruses. Due to the lack of antivirals to combat SFTS, an emerging tickborne epidemic caused by a RNA virus belonging to the Phenuividae family within Bunyavirales, Favipiravir has been put brand new attention as optimal SFTS clinical candidate. We here disclose chemical synthesis of novel derivatives of Favipiravir. All derivatives showed favorable inhibitory effect on SFTSV replication <em>in vitro</em>. The 50 % effective concentration (EC<sub>50</sub>) of the most active compound <strong>H3</strong> was 12.06 μM, better than that of Favipiravir (15.51 μM). Most importantly, compared with the clinical candidate Favipiravir, pharmacokinetic studies conducted on rats demonstrated enhanced pharmacokinetic properties for <strong>H2</strong> and <strong>H3</strong> including parameters of T<sub>1/2</sub>, C<sub>max</sub> and AUC. These combined attributes identified novel promising drug candidates for the treatment of SFTSV infection.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100226"},"PeriodicalIF":0.0,"publicationDate":"2024-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142418788","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Progression in nano-botanical oral hygiene solutions: The Dawn of biomimetic nanomaterials 纳米植物口腔卫生解决方案的进展:仿生纳米材料的曙光
European Journal of Medicinal Chemistry Reports Pub Date : 2024-09-25 DOI: 10.1016/j.ejmcr.2024.100219
Aqsa Arif , Muhammad Sharif Khar , Nariman Shahid , Waqar Aman , Joham Javed , Amina Rubab , Mashal Nayab , khadija mastoor , Rabia Arshad , Abbas Rahdar , Sonia Fathi-karkan , Zelal Kharaba , Sadanand Pandey
{"title":"Progression in nano-botanical oral hygiene solutions: The Dawn of biomimetic nanomaterials","authors":"Aqsa Arif ,&nbsp;Muhammad Sharif Khar ,&nbsp;Nariman Shahid ,&nbsp;Waqar Aman ,&nbsp;Joham Javed ,&nbsp;Amina Rubab ,&nbsp;Mashal Nayab ,&nbsp;khadija mastoor ,&nbsp;Rabia Arshad ,&nbsp;Abbas Rahdar ,&nbsp;Sonia Fathi-karkan ,&nbsp;Zelal Kharaba ,&nbsp;Sadanand Pandey","doi":"10.1016/j.ejmcr.2024.100219","DOIUrl":"10.1016/j.ejmcr.2024.100219","url":null,"abstract":"<div><div>Pathogenic bacteria consistently pose significant challenges within the oral mucosal environment by altering bioflora, biofilm development, and enamel demineralization, thus leading to extensive clinical resources for treatment. This review aims to gather suitable and novel information in terms of providing advanced bio-inspired therapeutic facilities to alleviate the burden of treatment on both the patient and medical infrastructure. Botanical nanoparticle-based mouthwashes have been synthesized using mostly green synthesis technology. Botanical nanoformulations-based mouthwashes are efficient for maintaining microbial flora and mimicking natural extracellular matrix (ECM) components. Furthermore, dental caries can also be treated by these nanoparticles through the promotion of enamel remineralization and bacterial growth suppression. These nature-inspired oral rinses/mouthwashes confer significant advantages relative to their synthetic counterparts, particularly in terms of safety, efficacy, and formulation simplicity. The potential applications of these bioinspired nanomaterials extend beyond wound healing and dental infection management, heralding a promising frontier in oral health restoration. The diversified range of these nanomaterials, from Propolis, Miswak, and Chitosan nanoparticles (NPs) to pomegranate extract and <em>Matricaria chamomilla L.</em> extract-based mouthwashes, introduces an exciting new dimension to oral care.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100219"},"PeriodicalIF":0.0,"publicationDate":"2024-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142418210","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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