Synthesis and in vitro activity of new biguanide-containing dendrimers on pathogenic isolates of Acanthamoeba polyphaga and Acanthamoeba griffini

Martín-Pérez, Tania; Lozano-Cruz, Tania; Criado–Fornelio, A.; Ortega, Paula; Gómez, Rafael; Mata, F. Javier de la; Pérez-Serrano, Jorge

doi:10.1007/s00436-019-06341-7

Cited by 7 publications

(6 citation statements)

References 33 publications

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“…Dendrimers are highly branched synthetic polymers with a wide range of applications due to their unique characteristics. They have been tested as antibacterial [ 14 , 19 , 27 , 28 , 29 , 30 ] or antiamoebic agents [ 16 , 17 ], as nanocarriers against bacteria, viruses, and parasites [ 31 , 32 , 33 , 34 ], and as nanocarriers for the delivery of nucleic acids [ 35 ], among others applications. The dendrimers used in these studies present two different cores: one core containing a silicon atom (Si) from which four branches extend, and the other containing a polyphenoxo core (P) attached to three branches.…”

Section: Discussionmentioning

confidence: 99%

“…Recently, different studies have provided evidence that various classes of dendrimers present antibacterial, antiviral, antifungal, and antiparasitic activity [ 14 ]. Previous work from our laboratory identified some specific classes of dendrimers, such as carbosilane, ammonium, and biguanide dendrimers, that have antiamoebic activity against trophozoites and cysts of Acanthamoeba producing growth inhibition and cell death [ 15 , 16 , 17 ] and antibacterial activity [ 18 , 19 ]. The activity of these compounds depends largely on the multivalency (number of terminal groups) of the molecule; however, the mechanism by which these dendrimers act on Acanthamoeba remained unclear.…”

Section: Introductionmentioning

confidence: 99%

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Ultrastructural Study of Acanthamoeba polyphaga Trophozoites and Cysts Treated In Vitro with Cationic Carbosilane Dendrimers

et al. 2020

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Cationic carbosilane dendrimers are branched molecules with antimicrobial properties. Their activity has been tested against Acanthamoeba polyphaga, a causative agent of Acanthamoeba keratitis, a severe ocular disease in humans. A. polyphaga trophozoites and cysts were exposed to different noncytotoxic cationic carbosilane dendrimers with proven antiamoebic activity. The effects of treatment on cell surface and cell ultrastructure were examined by scanning and transmission electron microscopy, respectively. Two of the dendrimers tested induced dramatic alterations of cellular ultrastructure in both trophozoites and cysts, including vacuolization, depletion of cytoplasmic contents, and reduced cell size. Additionally, we observed severe alterations of the plasma membrane with membrane blebbing in trophozoites and disruption in cysts. These alterations were also observed with chlorhexidine, a drug used for treatment of Acanthamoeba keratitis. Our results support that these compounds may target membranes, and their action is critical for parasite integrity.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Ultrastructural Study of Acanthamoeba polyphaga Trophozoites and Cysts Treated In Vitro with Cationic Carbosilane Dendrimers

et al. 2020

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“…This multivalency and the diversity of functional groups that can be introduced in it are very attractive for biomedical applications. Previous studies have reported the antibacterial [ 16 , 18 , 19 , 20 , 21 , 22 ] and antiamoebic [ 21 , 23 ] activity of these cationic dendrimers and have found that their main target is the plasma membrane of microorganisms. One type of cationic dendrimer with attractive microbicide properties is carbosilane dendrimers (CBS), which contains a framework made of weakly polar C-C and C-Si bonds [ 24 ].…”

Section: Introductionmentioning

confidence: 99%

In Vitro Activity of Carbosilane Cationic Dendritic Molecules on Prevention and Treatment of Candida Albicans Biofilms

et al. 2020

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Candida spp. are one of the most common fungal pathogens. Biofilms formed by Candidaalbicans offer resistance mechanisms against most antifungal agents. Therefore, development of new molecules effective against these microorganisms, alone or in combination with antifungal drugs, is extremely necessary. In the present work, we carried out a screening process of different cationic carbosilane dendritic molecules against C. albicans. In vitro activity against biofilm formation and biofilms was tested in both Colección Española de Cultivos Tipo (CECT) 1002 and clinical C. albicans strains. Cytotoxicity was studied in human cell lines, and biofilm alterations were observed by scanning electron microscopy (SEM). Antifungal activity of the carbosilane dendritic molecules was assessed by monitoring cell viability using both established and novel cell viability assays. One out of 14 dendritic molecules tested, named BDSQ024, showed the highest activity with a minimum biofilm inhibitory concentration (MBIC) for biofilm formation and a minimum biofilm damaging concentration (MBDC) for existing biofilm of 16–32 and 16 mg/L, respectively. Synergy with amphotericin (AmB) and caspofungin (CSF) at non-cytotoxic concentrations was found. Therefore, dendritic compounds are exciting new antifungals effective at preventing Candida biofilm formation and represent a potential novel therapeutic agent for treatment of C. albicans infection in combination with existing clinical antifungals.

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“…and protozoa. Treatments against amoebae both in the trophozoite and cyst phases have been registered [34][35][36][37][38]. But in addition, its effectiveness against viruses has also been reported.…”

Section: Dendritic Cationic Compoundsmentioning

confidence: 99%

Novel Treatment Approach against Candida spp.: Evaluation of Antifungal and Antibiofilm In Vitro Activity of Dendritic Molecules

Gómez-Casanova¹,

Copa-Patiño²,

Heredero‐Bermejo³

2023

Candida and Candidiasis

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Infections caused by the genus Candida are a serious threat, especially in the sanitary field. These pathogens are able to generate biofilms, which is one of the main problems because they are difficult to eradicate and are associated with a high mortality rate. These biofilms provide Candida species with increased resistance to health care drugs and disinfectants. Currently, the resistance to antifungals is increasing gradually and there are few drugs accepted for clinical use capable of combating them, and, unfortunately, these substances are sometimes toxic at the effective doses required. Therefore, finding new molecules capable of preventing the formation of biofilms or eradicating them once generated is of vital importance. In addition, it is essential to know the appropriate techniques to evaluate a new compound, guaranteeing reliable and precise data. Studies with dendritic systems of cationic nature are recently being carried out, presenting interesting and encouraging results as antimicrobials, against cells cancer cells, surface activating agents, and encapsulation of antibiotic, among others. In this chapter, we will focus on its antifungal capacity, especially its antibiofilm activity against Candida spp.

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Synthesis and in vitro activity of new biguanide-containing dendrimers on pathogenic isolates of Acanthamoeba polyphaga and Acanthamoeba griffini

Cited by 7 publications

References 33 publications

Ultrastructural Study of Acanthamoeba polyphaga Trophozoites and Cysts Treated In Vitro with Cationic Carbosilane Dendrimers

Ultrastructural Study of Acanthamoeba polyphaga Trophozoites and Cysts Treated In Vitro with Cationic Carbosilane Dendrimers

In Vitro Activity of Carbosilane Cationic Dendritic Molecules on Prevention and Treatment of Candida Albicans Biofilms

Novel Treatment Approach against Candida spp.: Evaluation of Antifungal and Antibiofilm In Vitro Activity of Dendritic Molecules

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