Interaction of a polymeric biguanide biocide with phospholipid membranes

Ikeda, Tomiki; Ledwith, A.; Bamford, C. H.; Hann, R. A.

doi:10.1016/0005-2736(84)90009-9

Cited by 204 publications

(123 citation statements)

References 26 publications

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“…Conversely, measured LDH activity did not prove significant compared with the control. However, protein precipitation has previously been described for cationic antiseptics such as chlorhexidine and polyhexanide [28,29], which could possibly affect the LDH enzyme. This could therefore lead to an overall reduction in LDH enzyme activity in the supernatant of osteoblasts, resulting in an underestimation of LDH release in cells treated with antiseptics.…”

Section: Discussionmentioning

confidence: 99%

Human osteoblast damage after antiseptic treatment

Vörös

Dobrindt

Perka

et al. 2013

International Orthopaedics (SICOT)

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Purpose Antiseptics are powerful medical agents used for wound treatment and decontamination and have a high potential for defeating joint infections in septic surgery. Both chlorhexidine and polyhexanide are frequently used in clinical practice and have a broad antimicrobial range, but their effect on human osteoblasts has not been sufficiently studied. Our objective was to investigate the toxic effects of polyhexanide and chlorhexidine on human osteoblasts in vitro to evaluate their clinical applicability in septic surgery. Methods We isolated and cultivated human osteoblasts in vitro and assayed the toxic effects of chlorhexidine 0.1 % and polyhexanide 0.04 %, concentrations commonly applied in clinical practice. Toxicity analysis was performed by visualisation of cell structure, lactate dehydrogenase (LDH) activity and evaluation of vital cells. Toxicity was evaluated by microscopic inspection of cell morphology, trypan blue staining and determination of LDH release. Results Damaged cell structure could be shown by microscopy. Both antiseptics promoted LDH activity after incubation with osteoblasts. The evaluation of vital osteoblasts showed a significant decrease of vital cells. Conclusions Both antiseptics induced significant cell death of osteoblasts at optimum exposure. We therefore recommend cautious use of polyhexanide and chlorhexidine in septic surgery to avoid severe osteoblast toxicity.

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Section: Discussionmentioning

confidence: 99%

Human osteoblast damage after antiseptic treatment

Vörös

Dobrindt

Perka

et al. 2013

International Orthopaedics (SICOT)

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“…The insoluble part was removed by filtration, and the filtrate was made acidic (pH 2) with hydrochloric acid. The pale cream precipitate was collected, washed with water, dried under vacuum (64 g; yield, 68%) and then recrystallized from 2-propanol: mp, 172 to 174°C; NMR (DMSO-d6,b), 2.70 (2H, t, -CH2-), 3.67 (2H, t, -CH2OH), 6.92 (2H, s, dicyandiamide), 7.25 (4H, s, aromatic), 9 containing -10' cells per ml was added to 18.0 ml of the biocide solution which was preequilibrated at 37°C. At the same time, 2.0 ml of the same culture was added to 18.0 ml of saline, decimal dilutions were prepared, and the starting cell concentration was enumerated by the spread plate method.…”

Section: Methodsmentioning

confidence: 99%

New polymeric biocides: synthesis and antibacterial activities of polycations with pendant biguanide groups

Ikeda¹,

Yamaguchi²,

Tazuke³

1984

Antimicrob Agents Chemother

191

142

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Acrylate monomers with pendant biguanide groups were successfully synthesized, and their homopolymers and copolymers were prepared with acrylamide. These cationic disinfectants of polymeric forms exhibited high antibacterial activity against gram-positive bacteria, whereas they were less active against gram-negative bacteria. It was found that the activity of the polymeric disinfectants was much higher than that of the monomeric species, and the difference in activity between the polymers and the monomers was discussed on the basis of their contributions to each elementary process of the lethal action.

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“…The structure of guanidine-based antimicrobials such as PHMG-P and PHMB is characterized by guanidino groups. These groups exert antimicrobial activity by disrupting the bacterial cell wall through electrostatic interactions with the acidic phospholipid phosphatidylglycerol, a major component of the bacterial cell wall (Broxton et al, 1984;Ikeda et al, 1983Ikeda et al, , 1984). In contrast, guanidino groups do not bind well to the primary components of mammalian cell membranes, neutral phospholipids such as phosphatidyl choline or phosphatidyl ethanolamine.…”

Section: Biocidal Properties Of Phmg-pmentioning

confidence: 99%

“…In contrast, guanidino groups do not bind well to the primary components of mammalian cell membranes, neutral phospholipids such as phosphatidyl choline or phosphatidyl ethanolamine. Guanidine-based antimicrobials were thus believed to have low toxicity to humans (Ikeda et al, 1983(Ikeda et al, , 1984. However, recent accounts have reported PHMB penetrating mammalian cells and interacting with chromosomes, raising concerns about health hazards from guanidine-based antimicrobials (Allen et al, 2004(Allen et al, , 2006Chindera et al, 2016;Firdessa et al, 2015).…”

Section: Biocidal Properties Of Phmg-pmentioning

confidence: 99%

Adverse health effects of humidifier disinfectants in Korea: lung toxicity of polyhexamethylene guanidine phosphate

et al. 2016

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-Exposure to humidifier disinfectants was identified in 2011 as the potential cause of an outbreak of lung disease in Korea. It is estimated that over 8 million people have been exposed to humidifier disinfectants-chemicals added to the water used in humidifiers to prevent the growth of microorganisms-since their commercial introduction. The primary component of humidifier disinfectant products involved was polyhexamethylene guanidine phosphate (PHMG-P), a guanidine-based antimicrobial agent. Lesions observed in the lungs of patients were similar to those observed in laboratory animals exposed to PHMG-P. In this review, we outline the physicochemical and toxicological properties of PHMG-P, and introduce a putative mechanism for its lung toxicity based in large part on research findings to date.

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Interaction of a polymeric biguanide biocide with phospholipid membranes

Cited by 204 publications

References 26 publications

Human osteoblast damage after antiseptic treatment

Human osteoblast damage after antiseptic treatment

New polymeric biocides: synthesis and antibacterial activities of polycations with pendant biguanide groups

Adverse health effects of humidifier disinfectants in Korea: lung toxicity of polyhexamethylene guanidine phosphate

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