The in vitro evaluation of anti-chlamydial and cytotoxic properties of dermaseptin S 4 and derivatives: peptides from am

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Med Chem Res DOI 10.1007/s00044-013-0601-9

ORIGINAL RESEARCH

The in vitro evaluation of anti-chlamydial and cytotoxic properties of dermaseptin S4 and derivatives: peptides from amphibian skin Ines Bergaoui • Amira Zaı¨ri • Houda Gharsallah Mahjoub Aouni • Adnene Hammami • Khaled Hani • Boulbaba Selmi



Received: 9 January 2013 / Accepted: 24 April 2013 Ó Springer Science+Business Media New York 2013

Abstract Chlamydia trachomatis is an obligate intracellular bacterium responsible for a number of health problems, including sexually transmitted infection in humans. Efforts were made for the search of alternative therapies. Accordingly, the present study was undertaken to perform a systemic in vitro investigation on the anti-chlamydial potential of cationic peptides from frog’s skin, namely dermaseptin S4 (S4) and its derivatives. Several strains of Chlamydia trachomatis serovar E were used to detect the antimicrobial activity of the new compounds. The infections tests and the toxic effects of the new compounds were determined using McCoy cells monolayers. Our data show that S4 exhibited a potent anti-chlamydial activity and found that these peptides blocked infection of McCoy cells and reduced the numbers of inclusion-forming units (81 %) after 48 h at low concentration (5 lg/ml). Besides, the finding revealed that increasing the number of positive charges of the peptide resulted in a reduced cytotoxicity without affecting the antimicrobial effect. Among all peptides, the derivative K4K20S4 was the more potent to inhibit C. trachomatis growth with 96 % reduction in the number of chlamydial inclusions compared with an untreated control infection and, therefore, can be I. Bergaoui  A. Zaı¨ri  K. Hani (&) Laboratory of Biochemistry (UR-12ES03-2012), Faculty of Medicine, 4002 Sousse, Tunisia e-mail: [email protected] I. Bergaoui  M. Aouni  B. Selmi Laboratory of Transmissible Diseases LR99-ES27, Faculty of Pharmacy, Avicenne Avenue, 5000 Monastir, Tunisia H. Gharsallah  A. Hammami Department of Microbiology and Research Laboratory ‘‘Microorganisms and Human Pathology’’, Hospital of Habib Bourguiba, Sfax, Tunisia

considered as potential agents for therapy of Chlamydia infectious diseases. Keywords Antimicrobial effect  Antimicrobial peptides  Chlamydia trachomatis  Dermaseptin S4

Introduction Chlamydia trachomatis is a well-recognized sexually transmitted pathogen (Be´be´ar and De Barbeyrac, 2009). Besides its potential to produce genital tract infection, C. trachomatis is increasingly being associated with long-term complications such as pelvic inflammatory disease, ectopic pregnancy, and infertility in women (Le Roy et al., 2012; Manavi, 2006); Yasin et al., 1996a, b). Although the fact is that C. trachomatis infections are prevalent worldwide with similar rates in males and females, infertility studies have mainly been focused on females. In fact, the burden of disease and infertility sequela is considered to be predominantly a female problem (Schautteet et al., 2012). Structurally, C. trachomati