Potential use of antimicrobial peptides as vaginal spermicides/microbicides

Nongnuj Tanphaichitr, Nopparat Srakaew, Rhea Alonzi, Wongsakorn Kiattiburut, Kessiri Kongmanas, Ruina Zhi, Weihua Li, Mark Baker, Guangshun Wang, Duane Hickling

Research output: Contribution to journalReview article

14 Citations (Scopus)

Abstract

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.

Original languageEnglish (US)
Article number13
JournalPharmaceuticals
Volume9
Issue number1
DOIs
StatePublished - Mar 11 2016

Fingerprint

Spermatocidal Agents
Anti-Infective Agents
Sexually Transmitted Diseases
Peptides
Magainins
Nonoxynol
Unwanted Pregnancies
Vagina
Innate Immunity
Surface-Active Agents
Spermatozoa
Epithelium
Population

Keywords

  • Antimicrobial peptide
  • Cathelicidin
  • HCAP-18
  • LL-37
  • Sexually transmitted infection
  • Spermicidal antimicrobial peptide
  • Spermicide
  • Vaginal contraceptive
  • Vaginal microbicide
  • Vaginitis

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmaceutical Science

Cite this

Tanphaichitr, N., Srakaew, N., Alonzi, R., Kiattiburut, W., Kongmanas, K., Zhi, R., ... Hickling, D. (2016). Potential use of antimicrobial peptides as vaginal spermicides/microbicides. Pharmaceuticals, 9(1), [13]. https://doi.org/10.3390/ph9010013

Potential use of antimicrobial peptides as vaginal spermicides/microbicides. / Tanphaichitr, Nongnuj; Srakaew, Nopparat; Alonzi, Rhea; Kiattiburut, Wongsakorn; Kongmanas, Kessiri; Zhi, Ruina; Li, Weihua; Baker, Mark; Wang, Guangshun; Hickling, Duane.

In: Pharmaceuticals, Vol. 9, No. 1, 13, 11.03.2016.

Research output: Contribution to journalReview article

Tanphaichitr, N, Srakaew, N, Alonzi, R, Kiattiburut, W, Kongmanas, K, Zhi, R, Li, W, Baker, M, Wang, G & Hickling, D 2016, 'Potential use of antimicrobial peptides as vaginal spermicides/microbicides', Pharmaceuticals, vol. 9, no. 1, 13. https://doi.org/10.3390/ph9010013
Tanphaichitr N, Srakaew N, Alonzi R, Kiattiburut W, Kongmanas K, Zhi R et al. Potential use of antimicrobial peptides as vaginal spermicides/microbicides. Pharmaceuticals. 2016 Mar 11;9(1). 13. https://doi.org/10.3390/ph9010013
Tanphaichitr, Nongnuj ; Srakaew, Nopparat ; Alonzi, Rhea ; Kiattiburut, Wongsakorn ; Kongmanas, Kessiri ; Zhi, Ruina ; Li, Weihua ; Baker, Mark ; Wang, Guangshun ; Hickling, Duane. / Potential use of antimicrobial peptides as vaginal spermicides/microbicides. In: Pharmaceuticals. 2016 ; Vol. 9, No. 1.
@article{8d957531e0864b298ccda25c541a5dbf,
title = "Potential use of antimicrobial peptides as vaginal spermicides/microbicides",
abstract = "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.",
keywords = "Antimicrobial peptide, Cathelicidin, HCAP-18, LL-37, Sexually transmitted infection, Spermicidal antimicrobial peptide, Spermicide, Vaginal contraceptive, Vaginal microbicide, Vaginitis",
author = "Nongnuj Tanphaichitr and Nopparat Srakaew and Rhea Alonzi and Wongsakorn Kiattiburut and Kessiri Kongmanas and Ruina Zhi and Weihua Li and Mark Baker and Guangshun Wang and Duane Hickling",
year = "2016",
month = "3",
day = "11",
doi = "10.3390/ph9010013",
language = "English (US)",
volume = "9",
journal = "Pharmaceuticals",
issn = "1424-8247",
publisher = "Multidisciplinary Digital Publishing Institute (MDPI)",
number = "1",

}

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, Guangshun

AU - Hickling, Duane

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

UR - http://www.scopus.com/inward/record.url?scp=84960963176&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84960963176&partnerID=8YFLogxK

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 -