Spermicidal activity of dermaseptins

Zaïri, Amira; Belaid, Afifa; Gahbiche, Amina; Hani, Khaled

doi:10.1016/j.contraception.2005.06.055

Cited by 24 publications

(14 citation statements)

References 50 publications

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“…The presence of 0.1% chelating agent ethylenediaminetetraacetic acid (EDTA) reduced the EC100 of S4 to 10 μ g/mL whereas less than a two-time enhancement in S1 activity was observed upon combination with EDTA. The striking phenomenon of synergistic enhancement with EDTA, suggests that S probably affects the motility of sperm membrane by depleting cytosolic potassium and sodium whereas EDTA chelates extracellular calcium [27]. The action of DSs on sperm motility was observed to be dose dependent.…”

Section: Dermaseptins Smentioning

confidence: 99%

“…Nisin showed a time and dose dependent effect on sperm motility with limited activity against STI causing pathogens [22]. Interestingly, peptides found in the skin secretions of frogs, such as dermaseptins and magainins, posses a potent spermicidal activity against human sperm along with their large spectrum of action against sexually transmitted pathogens [23–27]. This review aims to show that these two peptides are new sources for a promising spermicides microbicides basing on their biological properties.…”

Section: Introductionmentioning

confidence: 99%

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Dermaseptins and Magainins: Antimicrobial Peptides from Frogs′ Skin—New Sources for a Promising Spermicides Microbicides—A Mini Review

Zaïri

Tangy

Bouassida

et al. 2009

BioMed Research International

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Sexually transmitted infections (STIs) and human immunodeficiency virus (HIV), the causative agents of acquired immunodeficiency syndrome (AIDS), are two great concerns in the reproductive health of women. Thus, the challenge is to find products with a double activity, on the one hand having antimicrobial/antiviral properties with a role in the reduction of STI, and on the other hand having spermicidal action to be used as a contraceptive. In the absence of an effective microbicide along with the disadvantages of the most commonly used spermicidal contraceptive worldwide, nonoxynol-9, new emphasis has been focused on the development of more potential intravaginal microbicidal agents. Topical microbicides spermicides would ideally provide a female-controlled method of self-protection against HIV as well as preventing pregnancies. Nonoxynol-9, the only recommended microbicide spermicide, damages cervicovaginal epithelium because of its membrane-disruptive properties. Clearly, there is an urgent need to identify new compounds with dual potential microbicidal properties; antimicrobial peptides should be candidates for such investigations. Dermaseptins and magainins are two classes of cationic, amphipathic α-helical peptides that have been identified in the skin extracts of frogs Phyllomedusa sauvagei and Xenopus laevis. Regarding their contraceptive activities and their effect against various STI-causing pathogens, we believe that these two peptides are appropriate candidates in the evaluation of newer and safer microbicides spermicides in the future.

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Section: Dermaseptins Smentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Dermaseptins and Magainins: Antimicrobial Peptides from Frogs′ Skin—New Sources for a Promising Spermicides Microbicides—A Mini Review

Zaïri

Tangy

Bouassida

et al. 2009

BioMed Research International

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“…8,10,11 Recently, it has been demonstrated that dermaseptins possess a potent spermicidal activity against human sperm. 12 In addition, some synthetic peptides derived from dermaseptin S4 showed activity against Neisseria gonorrhoeae 13 indicating a potential role as microbicidal compounds. There has been renewed interest in the antimicrobial activity of dermaseptins in response to the isolation and characterization of DS 01, from the skin secretions of the Brazilian species Phyllomedusa oreades, a novel dermaseptin characterized by antibacterial and anti-protozoal activity.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and antimicrobial activity of dermaseptin S1 analogues

Savoia

Guerrini

Marzola

et al. 2008

Bioorganic & Medicinal Chemistry

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a b s t r a c tDermaseptins are peptides found in the skin secretions of Phyllomedusinae frogs. These peptides exert lytic action on some microorganisms without substantial haemolysis. In an attempt to understand the antimicrobial activity of these peptides we designed several dermaseptin S1 (ALWKTMLKKLGTMALHAG-KAALGAAADTISQGTQ) (DS1) analogues. All peptides were tested on the growth of prokaryotic (Grampositive and Gram-negative bacteria) and eukaryotic (the yeast Candida albicans and the protozoon Leishmania major) organisms. Our data showed a dose-dependent killing effect by most DS1 derivatives. Maximal antibacterial activity was displayed by a 16-mer peptide that was more active than native DS1.

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“…These peptides consist of 28-34 amino acids that are structured in amphipathic α-helices in apolar solvents. DSs are cytotoxic to a range of bacteria and protozoa and inhibit HSV-1 replication [36]. The mechanism of antimicrobial action of DSs involves interaction of the α-helix with membrane phospholipids causing cell permeation.…”

Section: Ionophoresmentioning

confidence: 99%

“…Dermaseptins (DSs) are antimicrobial peptides synthesised by amphibians [36]. These peptides consist of 28-34 amino acids that are structured in amphipathic α-helices in apolar solvents.…”

Section: Ionophoresmentioning

confidence: 99%

The Search for a Topical Dual Action Spermicide/Microbicide

Hughes¹,

Griffith²,

Aitken

2007

CMC

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There is an urgent clinical need to research novel methods of fertility control that are also protective against sexually transmitted diseases (STDs) such as the human immunodeficiency virus (HIV) or Chlamydia. The most obvious way to generate such a dual-purpose contraceptive method would be to develop safe, effective spermicides that were also active against a wide range of pathogenic organisms. The currently available formulations such as nonoxynol-9, gramicidin and benzalkonium chloride are effective spermicides but are toxic to the vaginal epithelium and do not provide protection against STDs. Over 60 agents are in clinical trials as potentially safer topical spermicides and/or microbicides. Compounds that have reached this stage of development include acid buffers, detergents, dendrimers, non-nucleoside reverse transcriptase inhibitors and anionic polymers. In addition, a number of potential spermicides/microbicides are the subject of preclinical investigation, including beta-cyclodextrin, cyanovirin, porphyrins, cyclotriazadisulfonamides, dermaseptins, short-interfering RNA (siRNA) and HIV antibodies. The chemical principles underlying these disparate approaches and potential avenues for future investigation are discussed.

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Spermicidal activity of dermaseptins

Cited by 24 publications

References 50 publications

Dermaseptins and Magainins: Antimicrobial Peptides from Frogs′ Skin—New Sources for a Promising Spermicides Microbicides—A Mini Review

Dermaseptins and Magainins: Antimicrobial Peptides from Frogs′ Skin—New Sources for a Promising Spermicides Microbicides—A Mini Review

Synthesis and antimicrobial activity of dermaseptin S1 analogues

The Search for a Topical Dual Action Spermicide/Microbicide

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