Atyaf Talal Mahmood, Islam Khalid Kamal, Yasser Fakri Mustafa
{"title":"香豆素骨架是研究氯氧苯酚作为口服抗菌剂的开门钥匙:一项体外-硅内研究","authors":"Atyaf Talal Mahmood, Islam Khalid Kamal, Yasser Fakri Mustafa","doi":"10.1134/S1068162024060013","DOIUrl":null,"url":null,"abstract":"<p><b>Objective:</b> Formulations containing chloroxylenol (COL), particularly Dettol, are commonly used in homes and hospitals for its antiseptic activity. Many studies documented the toxicity of this COL when human accidentally intake it in concentration less than 5%. <b>Methods:</b> The aim of this work is to use COL as a building block to create seven coumarin-based chemicals. Their structural frameworks were confirmed by various spectrophotometric methods. Also, these chemicals were submitted into two kinds of studies: <i>in vitro</i> and <i>in silico</i>. For the former one, the antimicrobial activity of these chemicals was specified against ten strains of infectious aerobes, anaerobes, and fungi. To explore the biocompatibility, the exploratory chemicals were studied using two normal bacteria and three healthy cellular lines. The <i>in silico</i> study include checking the theoretical capacity of the exploratory chemicals to oral-administrated and their toxicity-anticipated profiles. <b>Results and Discussion:</b> The gathered findings indicated that these chemicals has outstanding potential to inhibit the growth of infectious aerobes and fungi, and (<b>AA4</b>) being the best of their growth-inhibitor. Also, the same potential was observed against the infectious anaerobes, but here (<b>AA1</b>) was the superior growth-inhibitor. These wide-spectrum antimicrobial activities were coupled with great biocompatibilities with normal species under study. On the other hand, the results gathered from <i>in silico</i> study demonstrated that the exploratory chemicals have a powerful potential to oral-administrated with minimal anticipated toxicity. <b>Conclusions:</b> From these findings, the authors concluded that it is possible to use COL as a building unit to create biocompatible, wide-spectrum, low toxicity, oral-administrated antimicrobial prospects.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2252 - 2268"},"PeriodicalIF":1.1000,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Coumarin Backbone as a Door-Opening Key for Investigating Chloroxylenol as Oral Antimicrobial Agents: an In Vitro–In Silico Study\",\"authors\":\"Atyaf Talal Mahmood, Islam Khalid Kamal, Yasser Fakri Mustafa\",\"doi\":\"10.1134/S1068162024060013\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><b>Objective:</b> Formulations containing chloroxylenol (COL), particularly Dettol, are commonly used in homes and hospitals for its antiseptic activity. 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The <i>in silico</i> study include checking the theoretical capacity of the exploratory chemicals to oral-administrated and their toxicity-anticipated profiles. <b>Results and Discussion:</b> The gathered findings indicated that these chemicals has outstanding potential to inhibit the growth of infectious aerobes and fungi, and (<b>AA4</b>) being the best of their growth-inhibitor. Also, the same potential was observed against the infectious anaerobes, but here (<b>AA1</b>) was the superior growth-inhibitor. These wide-spectrum antimicrobial activities were coupled with great biocompatibilities with normal species under study. 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引用次数: 0
摘要
目的:含氯甲酚(COL)的制剂,尤其是 Dettol,因其具有杀菌作用而常用于家庭和医院。许多研究表明,当人体意外摄入浓度低于 5%的氯甲酚时,会产生毒性。方法:这项工作的目的是以 COL 为构件,创造出七种基于香豆素的化学物质。通过各种分光光度法确认了它们的结构框架。此外,还对这些化学物质进行了两种研究:体外研究和硅学研究。前者针对十株感染性需氧菌、厌氧菌和真菌的抗菌活性进行了研究。为了探索生物相容性,我们使用两种正常细菌和三种健康细胞系对这些探索性化学物质进行了研究。硅学研究包括检查探索性化学物质口服的理论能力及其毒性预期特征。结果与讨论:研究结果表明,这些化学物质在抑制感染性需氧菌和真菌的生长方面具有突出的潜力,其中 AA4 是最好的生长抑制剂。此外,对感染性厌氧菌也有同样的抑制潜力,但(AA1)的生长抑制效果更好。这些广谱抗菌活性与所研究的正常菌种具有很好的生物相容性。另一方面,硅学研究的结果表明,这些探索性化学物质具有强大的口服潜力,而且预期毒性极低。结论从这些发现中,作者得出结论,有可能利用 COL 作为构建单元,创造出生物相容性好、广谱、低毒、可口服的抗菌前景。
Coumarin Backbone as a Door-Opening Key for Investigating Chloroxylenol as Oral Antimicrobial Agents: an In Vitro–In Silico Study
Objective: Formulations containing chloroxylenol (COL), particularly Dettol, are commonly used in homes and hospitals for its antiseptic activity. Many studies documented the toxicity of this COL when human accidentally intake it in concentration less than 5%. Methods: The aim of this work is to use COL as a building block to create seven coumarin-based chemicals. Their structural frameworks were confirmed by various spectrophotometric methods. Also, these chemicals were submitted into two kinds of studies: in vitro and in silico. For the former one, the antimicrobial activity of these chemicals was specified against ten strains of infectious aerobes, anaerobes, and fungi. To explore the biocompatibility, the exploratory chemicals were studied using two normal bacteria and three healthy cellular lines. The in silico study include checking the theoretical capacity of the exploratory chemicals to oral-administrated and their toxicity-anticipated profiles. Results and Discussion: The gathered findings indicated that these chemicals has outstanding potential to inhibit the growth of infectious aerobes and fungi, and (AA4) being the best of their growth-inhibitor. Also, the same potential was observed against the infectious anaerobes, but here (AA1) was the superior growth-inhibitor. These wide-spectrum antimicrobial activities were coupled with great biocompatibilities with normal species under study. On the other hand, the results gathered from in silico study demonstrated that the exploratory chemicals have a powerful potential to oral-administrated with minimal anticipated toxicity. Conclusions: From these findings, the authors concluded that it is possible to use COL as a building unit to create biocompatible, wide-spectrum, low toxicity, oral-administrated antimicrobial prospects.
期刊介绍:
Russian Journal of Bioorganic Chemistry publishes reviews and original experimental and theoretical studies on the structure, function, structure–activity relationships, and synthesis of biopolymers, such as proteins, nucleic acids, polysaccharides, mixed biopolymers, and their complexes, and low-molecular-weight biologically active compounds (peptides, sugars, lipids, antibiotics, etc.). The journal also covers selected aspects of neuro- and immunochemistry, biotechnology, and ecology.