Effect of Triclosan and Chloroxylenol on Bacterial Membranes

Poger, David; Mark, Alan E.

doi:10.1021/acs.jpcb.9b02588

Cited by 24 publications

(7 citation statements)

References 91 publications

(157 reference statements)

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“…Levofloxacin [236][237][238], Clarithromycin [236], Isoniazid N -acylated derivatives [239], Rifampicin [234,240], Mangostin [241], Trimethoprim [242], Negamycin [243] Potential antibiotic Kanamycin A [133], nTZDpa and its derivatives [244], Cholic acid derived amphiphiles [245], γ-terpineol [246], Bithionol [247] Antimicrobial compound Chlorhexidine [248][249][250], Triclosan [251], Octenidine [250] Antiparasitic Praziquantel [252] Antiviral drugs Darunavir [253], Amantadine [254][255][256], Spiro[pyrrolidine-2,2 -adamantane] [254,255], 20,30-dideoxyadenosine (Didanosine) [242], Saffron [257] Antifungal drug Itraconazole, [184,186,187,258], Nystatin [259], Amphotericin B [260] Rheumatoid arthritis Lapatinib [213] Nonsteroidal antiinflammatory drugs, inhibitor of cyclooxygenase-1 and -2…”

Section: Application and Target Drugs And Pharmaceuticsmentioning

confidence: 99%

Mechanistic Understanding from Molecular Dynamics in Pharmaceutical Research 2: Lipid Membrane in Drug Design

2021

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We review the use of molecular dynamics (MD) simulation as a drug design tool in the context of the role that the lipid membrane can play in drug action, i.e., the interaction between candidate drug molecules and lipid membranes. In the standard “lock and key” paradigm, only the interaction between the drug and a specific active site of a specific protein is considered; the environment in which the drug acts is, from a biophysical perspective, far more complex than this. The possible mechanisms though which a drug can be designed to tinker with physiological processes are significantly broader than merely fitting to a single active site of a single protein. In this paper, we focus on the role of the lipid membrane, arguably the most important element outside the proteins themselves, as a case study. We discuss work that has been carried out, using MD simulation, concerning the transfection of drugs through membranes that act as biological barriers in the path of the drugs, the behavior of drug molecules within membranes, how their collective behavior can affect the structure and properties of the membrane and, finally, the role lipid membranes, to which the vast majority of drug target proteins are associated, can play in mediating the interaction between drug and target protein. This review paper is the second in a two-part series covering MD simulation as a tool in pharmaceutical research; both are designed as pedagogical review papers aimed at both pharmaceutical scientists interested in exploring how the tool of MD simulation can be applied to their research and computational scientists interested in exploring the possibility of a pharmaceutical context for their research.

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Section: Application and Target Drugs And Pharmaceuticsmentioning

confidence: 99%

Mechanistic Understanding from Molecular Dynamics in Pharmaceutical Research 2: Lipid Membrane in Drug Design

2021

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“…The selection of the substances CLX and TRP to be incorporated in the acrylic water-based paint, previously used in our other studies [ 28 , 45 ], is related to the fact that these are well-studied and well-characterized substances, with proven antimicrobial activity [ 35 , 46 ]. Besides, both substances are frequently used in hygiene products, disinfectants, and cosmetics since they present low toxicity when in lower concentrations [ 4 , 41 ].…”

Section: Discussionmentioning

confidence: 99%

Development and In Vitro Validation of Antibacterial Paints Containing Chloroxylenol and Terpineol

Querido

Paulo²,

Hariharakrishnan³

et al. 2022

Toxics

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The establishment of self-disinfecting surfaces is an important method to avoid surface contamination. Recently, paints with antimicrobial properties have been developed to be applied on different surfaces, avoiding contamination with pathogens. In this work, self-disinfecting paints containing Chloroxylenol (CLX), Terpineol (TRP), and a mixture of both substances were developed. The goal was to evaluate and validate these paints using international standards for eventual commercialization and application in scenarios where surface contamination represents a problem. The paints were challenged with five different bacteria, Gram-positive and Gram-negative, before and after a scrub resistance test, where the long-term efficacy of the paints was evaluated. The antibacterial activity assessment was performed following ISO 22196 and JIS Z2801. In general, the paints showed very promising results, demonstrating their antibacterial activity, before and after scrub resistance test. The paint incorporating the mixture of CLX and TRP (CLX+TRP) stood out by revealing consistent results of antibacterial activity both before and after the scrub resistance test for most of the tested bacteria. The cytotoxicity of the developed paints was assessed in vitro by performing tests by direct contact with a human skin cell line, HaCaT, and testes on extracts with HaCaT and a pulmonary cell line, A549. The methodologies for cytotoxicity assessment were developed based in ISO 10993. For genotoxicity assessment, alkaline comet assay was conducted on both cell lines. The cytotoxicity assessment revealed promising results with the paints, demonstrating values of cellular viability above 70% and values of lactate dehydrogenase (LDH) leakage below 30%. The genotoxic assessment also revealed acceptable values of primary DNA damage for the developed antibacterial paints. In general, the selected methodologies presented good potential to be applied in the validation of both efficacy and safety of the antimicrobial paints, aiming to be applied in real scenarios.

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“…Dettol® is composed of chloroxylenol 4.8%, one of the groups of halophenol, which works by denaturing proteins, altering cell wall permeability and causing cell leakage [6]. It is known as good disinfectant for both Gram-positive and Gram-negative bacteria with greater effect on Gram-positive ones [14]; hence, it is not surprising that Staphylococcus and Streptococcus isolates were 100% susceptible to Dettol® at recommended user concentration and only 26.7% of E. coli were resistant. Savlon® has shown high activity against the isolates compared to other disinfectants, which manifested its strong activity against both the Gram-negative and Grampositive bacteria.…”

Section: Discussionmentioning

confidence: 99%

Preliminary Study on Disinfectant Susceptibility/Resistance Profiles of Bacteria Isolated from Slaughtered Village Free-Range Chickens in Nairobi, Kenya

Acsa

Caroline

Njeru

et al. 2021

International Journal of Microbiology

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Disinfectants are regularly used for cleansing poultry slaughterhouses to control microorganisms. However, the microorganisms such as bacteria are developing resistance to disinfectant(s) and complicate control of bacterial infections. The aim of this study was, therefore, to determine disinfectant susceptibility/resistance patterns manifested by bacteria (to commonly used disinfectants), which were isolated from intestines of slaughtered indigenous chickens in Nairobi, Kenya. The method used was agar well diffusion, and the six disinfectants (their active ingredients are in brackets) tested were as follows: Kupacide® (glutaraldehyde; benzalkonium chloride); TH4+® (didecyl dimethyl ammonium HCl; dioctyl dimethyl ammonium HCl; octyl decyldimethyl ammonium HCl; alkyl dimethyl ammonium HCl; and glutaraldehyde); Noro cleanse® (glutaraldehyde; coco-benzyl-dimethyl-ammonium chloride); Dettol® (chloroxylenol); Savlon® (chlorhexidine gluconate; cetrimide; and N-propylalcohol); and Jik® (sodium hypochlorite). At recommended user concentration by the manufacturer, isolates showed various resistance to the respective disinfectants. E. coli isolates were resistant to five of the tested disinfectants (Jik®, TH4+®, Noro cleanse®, Dettol®, and Kupacide®); however, they were susceptible to Savlon®; Staphylococcus isolates were resistant to disinfectants to Jik® and TH4+® and susceptible to the rest disinfectants; Streptococcus isolates were only resistant to Jik® and susceptible to the remaining disinfectants. Some E. coli and Staphylococcus isolates showed resistance to more than one disinfectant. This study has demonstrated resistance of the bacterial isolates to various disinfectants at recommended user concentrations, although some of them were susceptible at higher concentration(s) and lower concentrations. This will interfere with the cleansing of the respective premises, resulting in contaminated products, which may end-up causing disease in the humans consuming them. Hence, it is recommended that one ascertains the efficacy of respective disinfectant by carrying out disinfectant susceptibility testing to know the effective ones and the appropriate concentration to use.

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Effect of Triclosan and Chloroxylenol on Bacterial Membranes

Cited by 24 publications

References 91 publications

Mechanistic Understanding from Molecular Dynamics in Pharmaceutical Research 2: Lipid Membrane in Drug Design

Mechanistic Understanding from Molecular Dynamics in Pharmaceutical Research 2: Lipid Membrane in Drug Design

Development and In Vitro Validation of Antibacterial Paints Containing Chloroxylenol and Terpineol

Preliminary Study on Disinfectant Susceptibility/Resistance Profiles of Bacteria Isolated from Slaughtered Village Free-Range Chickens in Nairobi, Kenya

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