TY - JOUR
T1 - Potential use of antimicrobial peptides as vaginal spermicides/microbicides
AU - Tanphaichitr, Nongnuj
AU - Srakaew, Nopparat
AU - Alonzi, Rhea
AU - Kiattiburut, Wongsakorn
AU - Kongmanas, Kessiri
AU - Zhi, Ruina
AU - Li, Weihua
AU - Baker, Mark
AU - Wang, Guanshun
AU - Hickling, Duane
N1 - Publisher Copyright:
© 2016 by the authors; licensee MDPI, Basel, Switzerland.
Copyright:
Copyright 2018 Elsevier B.V., All rights reserved.
PY - 2016/3/11
Y1 - 2016/3/11
N2 - The concurrent increases in global population and sexually transmitted infection (STI) demand a search for agents with dual spermicidal and microbicidal properties for topical vaginal application. Previous attempts to develop the surfactant spermicide, nonoxynol-9 (N-9), into a vaginal microbicide were unsuccessful largely due to its inefficiency to kill microbes. Furthermore, N-9 causes damage to the vaginal epithelium, thus accelerating microbes to enter the women’s body. For this reason, antimicrobial peptides (AMPs), naturally secreted by all forms of life as part of innate immunity, deserve evaluation for their potential spermicidal effects. To date, twelve spermicidal AMPs have been described including LL-37, magainin 2 and nisin A. Human cathelicidin LL-37 is the most promising spermicidal AMP to be further developed for vaginal use for the following reasons. First, it is a human AMP naturally produced in the vagina after intercourse. Second, LL-37 exerts microbicidal effects to numerous microbes including those that cause STI. Third, its cytotoxicity is selective to sperm and not to the female reproductive tract. Furthermore, the spermicidal effects of LL-37 have been demonstrated in vivo in mice. Therefore, the availability of LL-37 as a vaginal spermicide/microbicide will empower women for self-protection against unwanted pregnancies and STI.
AB - The concurrent increases in global population and sexually transmitted infection (STI) demand a search for agents with dual spermicidal and microbicidal properties for topical vaginal application. Previous attempts to develop the surfactant spermicide, nonoxynol-9 (N-9), into a vaginal microbicide were unsuccessful largely due to its inefficiency to kill microbes. Furthermore, N-9 causes damage to the vaginal epithelium, thus accelerating microbes to enter the women’s body. For this reason, antimicrobial peptides (AMPs), naturally secreted by all forms of life as part of innate immunity, deserve evaluation for their potential spermicidal effects. To date, twelve spermicidal AMPs have been described including LL-37, magainin 2 and nisin A. Human cathelicidin LL-37 is the most promising spermicidal AMP to be further developed for vaginal use for the following reasons. First, it is a human AMP naturally produced in the vagina after intercourse. Second, LL-37 exerts microbicidal effects to numerous microbes including those that cause STI. Third, its cytotoxicity is selective to sperm and not to the female reproductive tract. Furthermore, the spermicidal effects of LL-37 have been demonstrated in vivo in mice. Therefore, the availability of LL-37 as a vaginal spermicide/microbicide will empower women for self-protection against unwanted pregnancies and STI.
KW - Antimicrobial peptide
KW - Cathelicidin
KW - HCAP-18
KW - LL-37
KW - Sexually transmitted infection
KW - Spermicidal antimicrobial peptide
KW - Spermicide
KW - Vaginal contraceptive
KW - Vaginal microbicide
KW - Vaginitis
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U2 - 10.3390/ph9010013
DO - 10.3390/ph9010013
M3 - Review article
C2 - 26978373
AN - SCOPUS:84960963176
VL - 9
JO - Pharmaceuticals
JF - Pharmaceuticals
SN - 1424-8247
IS - 1
M1 - 13
ER -