The Experts below are selected from a list of 72 Experts worldwide ranked by ideXlab platform

Fatih M Uckun - One of the best experts on this subject based on the ideXlab platform.

  • Contraceptive Activity of a Spermicidal Aryl Phosphate Derivative of Bromo-Methoxy Zidovudine (Compound WHI-05) in Rabbits
    Drug Research, 2011
    Co-Authors: Osmond J. D'cruz, Fatih M Uckun
    Abstract:

    WHI-05 (5-bromo-6-methoxy-5,6-dihydro-3’-azidothymidine-5’-(p-methoxyphenyl) methoxyalaninyl phosphate, CAS 213982-93-5) is a highly promising antiviral and Spermicidal Agent with clinical potential as a vaginal contraceptive which can prevent the sexual transmission of AIDS. In this study, the contraceptive activity of WHI-05 in rabbits was evaluated. Exposure of semen to WHI-05 at the time of artificial insemination inhibited pregnancy and embryo implantation by 90 %. Intravaginal application of 2 % WHI-05 containing gel also inhibited the pregnancy rate by 90 %. WHI-05 had no side effects for the offspring of rabbits who became pregnant despite WHI-05.

  • a 13 week subchronic intravaginal toxicity study of the novel broad spectrum anti hiv and Spermicidal Agent n 2 1 cyclohexenyl ethyl n 2 5 bromopyridyl thiourea phi 346 in mice
    Toxicologic Pathology, 2002
    Co-Authors: Osmond J Dcruz, Barbara Waurzyniak, Fatih M Uckun
    Abstract:

    The nonnucleosid e inhibitor (NNI) of HIV-1 reverse transcriptase, PHI-346 (N -[2-(1-cyclohexenyl)ethyl]- N -[2-(5-bromopyridyl)]-thiourea ), is a dual-function Spermicidal Agent with potent anti-HIV activity against drug-sensitive as well as drug-resistant HIV-1 strains with genotypic and phenotypic NNI resistance. PHI-346 was formulated via a lipophilic gel-microemulsion for intravaginal use as a potentia l dual-function microbicide. To evaluate the toxicity potential of short-term intravaginal exposure to PHI-346, groups of 15 female B 6C3F1 and CD-1 mice were exposed intravaginally to a gel-microemulsion containing 0, 0.5, 1.0, or 2.0% PHI-346, 5 days per week for 13 consecutive weeks . On a molar basis, these concentrations of PHI-346 are 350 to 1,400-times higher than its Spermicidal EC 50 and nearly 5 10 6 to 2 10 7 times higher than its in vitro anti-HIV IC50. After 13 weeks of intravaginal treatment, B6C3F1 mice were evaluated for survival, body weight gain, absolute and relative organ weights. Blood was analyzed for hematology and clinical chemistry proŽles. Microscopic examination was performed on hematoxylin and eosinstained tissue sections from each study animal. Placebo control and PHI-346 dosed female CD-1 mice were mated with untreated males in order to evaluate if PHI-346 has any deleterious effects on the reproductive performance. There were no treatment-related mortalities. Mea n body weight gain during the dosing period was not reduced by PHI-346 treatment. The hemogram or blood chemistry proŽles revealed lack of systemic toxicity following daily intravaginal instillation of PHI-346 for 13 weeks. No clinically signiŽcant changes in absolute and relative organ weights were noted in PHI-346 dose groups. Extensive histopathological examination of tissues revealed no treatment-related abnormalities in any of the thr ee PHI-346 dose groups. Repeated intravaginal exposure of CD-1 mice to increasing concentrations of PHI-346 for 13 weeks had no adver se effect on their subsequen t reproductive capability, perinatal outcome, growth, and developmen t of offspring. Collectively, these Žn dings demonstrate that repetitive intravaginal administration of PHI-346 at concentrations as high as 1,400-times its Spermicidal EC 50 and 2 10 7 times its in vitro anti-HIV IC50 was not associated with local or systemic toxicity and did not adversely affect the reproductive performance in mice. PHI-346 may be useful as an active ingredient of a safe vaginal microbicide for prevention of the sexual transmission of multidrug-resistant HIV-1.

  • Structural and biological characterization of a novel Spermicidal vanadium(IV) complex: Bis(π-cyclopentadienyl)-N,N-diethyl dithiocarbamato vanadium(IV) tetrafluoro borate, [VCp2(DeDtc)](BF4)
    Journal of Inorganic Biochemistry, 1998
    Co-Authors: Phalguni Ghosh, Osmond J. D'cruz, Sutapa Ghosh, Fatih M Uckun
    Abstract:

    This paper describes the detailed biologic and physiochemical characterization of a lead Spermicidal compound by computer-assisted sperm analysis spectroscopy electrochemistry and X-ray crystallography. Vanadocene dithiocarbamato complex at physiologic pH was identified as the most potent and stable Spermicidal compound. Its structural integrity has been confirmed through UV-visible spectrum electron paramagnetic resonance spectroscopy and electrochemical studies. In addition the three-dimensional solid state structural characterization of this complex has been achieved by single crystal X-ray diffraction. Extensive studies have been performed on the stabilizing effects of the dithiocarbamate ligand for higher oxidation state metal ions like vanadium. Overall this study confirms and extends previous studies of the Spermicidal activity of vanadocenes. However the molecular targets of vanadocenes as a new class of Spermicidal Agent and the structure activity relationships affecting their Spermicidal activity remain unknown. Hence future studies aimed at determining the structure activity relationships critical for the sperm immobilizing function of vanadocenes are recommended.

Seymour J Klebanoff - One of the best experts on this subject based on the ideXlab platform.

  • effects of the Spermicidal Agent nonoxynol 9 on vaginal microbial flora
    The Journal of Infectious Diseases, 1992
    Co-Authors: Seymour J Klebanoff
    Abstract:

    The relationship of normal vaginal Lactobacillus bacteria peroxides halide salts and the vaginal spermicide nonoxynol-9 in killing the vaginal contaminant bacteria E. coli was explored. Nonoxynol is toxic to most bacteria including lactobacillus but not to E. coli. Normally lactobacilli suppress the growth of coliforms by releasing H202 hydrogen peroxide acting with halide ions. These relationships were verified in these experiments and extended to show that nonoxynol is toxic in to E. coli in hypotonic solution at high concentrations of nonoxynol and at low pH values. The halide can be chloride iodide bromide or thiocyanate ion; the peroxide generating system could be myeloperoxidase or eosinophil peroxidase; the non-ionic detergent could be Tween 20 or Tween 80 but not Triton X-100 or Nonidet P-40. Many of the non-ionic detergents contain peroxides as contaminants: purified Tween 20 was not bactericidal to E. coli. The implications of E. coli displacing lactobacilli of peroxide content to nonoxynol-9 and relative sensitivity of E. coli and lactobacilli to these toxins were discussed in connection with vaginal colonization with coliforms and bacteriuria in women.

Michael L. Chikindas - One of the best experts on this subject based on the ideXlab platform.

  • ResearchArticle Spermicidal Activity of the Safe Natural Antimicrobial Peptide Subtilosin
    2020
    Co-Authors: Katia E. Sutyak, Robert A. Anderson, Sara E. Dover, Kenneth A. Feathergill, Alla A. Aroutcheva, Sebastian Faro, Michael L. Chikindas
    Abstract:

    , but not against the tested healthy vaginal microbiota of lactobacilli. After conducting tissue sensitivity assaysusing an ectocervical tissue model, we determined that human cells remained viable after prolonged exposures to partially-purifiedsubtilosin, indicating the compound is safe for human use. Subtilosin was shown to eliminate the motility and forward progressionof human spermatozoa in a dose-dependent manner, and can therefore be considered a general Spermicidal Agent. These resultssuggest subtilosin would be a valuable component in topical personal care products aimed at contraception and BV prophylaxisand treatment.Copyright © 2008 Katia E. Sutyak et al. This is an open access article distributed under the Creative Commons Attribution License,which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

  • Spermicidal Activity of the Safe Natural Antimicrobial Peptide Subtilosin
    Infectious Diseases in Obstetrics & Gynecology, 2008
    Co-Authors: Katia E. Sutyak, Robert A. Anderson, Sara E. Dover, Kenneth A. Feathergill, Alla A. Aroutcheva, Sebastian Faro, Michael L. Chikindas
    Abstract:

    Bacterial vaginosis (BV), a condition affecting millions of women each year, is primarily caused by the gram-variable organism Gardnerella vaginalis. A number of organisms associated with BV cases have been reported to develop multidrug resistance, leading to the need for alternative therapies. Previously, we reported the antimicrobial peptide subtilosin has proven antimicrobial activity against G. vaginalis, but not against the tested healthy vaginal microbiota of lactobacilli. After conducting tissue sensitivity assays using an ectocervical tissue model, we determined that human cells remained viable after prolonged exposures to partially-purified subtilosin, indicating the compound is safe for human use. Subtilosin was shown to eliminate the motility and forward progression of human spermatozoa in a dose-dependent manner, and can therefore be considered a general Spermicidal Agent. These results suggest subtilosin would be a valuable component in topical personal care products aimed at contraception and BV prophylaxis and treatment.

Katia E. Sutyak - One of the best experts on this subject based on the ideXlab platform.

  • ResearchArticle Spermicidal Activity of the Safe Natural Antimicrobial Peptide Subtilosin
    2020
    Co-Authors: Katia E. Sutyak, Robert A. Anderson, Sara E. Dover, Kenneth A. Feathergill, Alla A. Aroutcheva, Sebastian Faro, Michael L. Chikindas
    Abstract:

    , but not against the tested healthy vaginal microbiota of lactobacilli. After conducting tissue sensitivity assaysusing an ectocervical tissue model, we determined that human cells remained viable after prolonged exposures to partially-purifiedsubtilosin, indicating the compound is safe for human use. Subtilosin was shown to eliminate the motility and forward progressionof human spermatozoa in a dose-dependent manner, and can therefore be considered a general Spermicidal Agent. These resultssuggest subtilosin would be a valuable component in topical personal care products aimed at contraception and BV prophylaxisand treatment.Copyright © 2008 Katia E. Sutyak et al. This is an open access article distributed under the Creative Commons Attribution License,which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

  • Spermicidal Activity of the Safe Natural Antimicrobial Peptide Subtilosin
    Infectious Diseases in Obstetrics & Gynecology, 2008
    Co-Authors: Katia E. Sutyak, Robert A. Anderson, Sara E. Dover, Kenneth A. Feathergill, Alla A. Aroutcheva, Sebastian Faro, Michael L. Chikindas
    Abstract:

    Bacterial vaginosis (BV), a condition affecting millions of women each year, is primarily caused by the gram-variable organism Gardnerella vaginalis. A number of organisms associated with BV cases have been reported to develop multidrug resistance, leading to the need for alternative therapies. Previously, we reported the antimicrobial peptide subtilosin has proven antimicrobial activity against G. vaginalis, but not against the tested healthy vaginal microbiota of lactobacilli. After conducting tissue sensitivity assays using an ectocervical tissue model, we determined that human cells remained viable after prolonged exposures to partially-purified subtilosin, indicating the compound is safe for human use. Subtilosin was shown to eliminate the motility and forward progression of human spermatozoa in a dose-dependent manner, and can therefore be considered a general Spermicidal Agent. These results suggest subtilosin would be a valuable component in topical personal care products aimed at contraception and BV prophylaxis and treatment.

Sebastian Faro - One of the best experts on this subject based on the ideXlab platform.

  • ResearchArticle Spermicidal Activity of the Safe Natural Antimicrobial Peptide Subtilosin
    2020
    Co-Authors: Katia E. Sutyak, Robert A. Anderson, Sara E. Dover, Kenneth A. Feathergill, Alla A. Aroutcheva, Sebastian Faro, Michael L. Chikindas
    Abstract:

    , but not against the tested healthy vaginal microbiota of lactobacilli. After conducting tissue sensitivity assaysusing an ectocervical tissue model, we determined that human cells remained viable after prolonged exposures to partially-purifiedsubtilosin, indicating the compound is safe for human use. Subtilosin was shown to eliminate the motility and forward progressionof human spermatozoa in a dose-dependent manner, and can therefore be considered a general Spermicidal Agent. These resultssuggest subtilosin would be a valuable component in topical personal care products aimed at contraception and BV prophylaxisand treatment.Copyright © 2008 Katia E. Sutyak et al. This is an open access article distributed under the Creative Commons Attribution License,which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

  • Spermicidal Activity of the Safe Natural Antimicrobial Peptide Subtilosin
    Infectious Diseases in Obstetrics & Gynecology, 2008
    Co-Authors: Katia E. Sutyak, Robert A. Anderson, Sara E. Dover, Kenneth A. Feathergill, Alla A. Aroutcheva, Sebastian Faro, Michael L. Chikindas
    Abstract:

    Bacterial vaginosis (BV), a condition affecting millions of women each year, is primarily caused by the gram-variable organism Gardnerella vaginalis. A number of organisms associated with BV cases have been reported to develop multidrug resistance, leading to the need for alternative therapies. Previously, we reported the antimicrobial peptide subtilosin has proven antimicrobial activity against G. vaginalis, but not against the tested healthy vaginal microbiota of lactobacilli. After conducting tissue sensitivity assays using an ectocervical tissue model, we determined that human cells remained viable after prolonged exposures to partially-purified subtilosin, indicating the compound is safe for human use. Subtilosin was shown to eliminate the motility and forward progression of human spermatozoa in a dose-dependent manner, and can therefore be considered a general Spermicidal Agent. These results suggest subtilosin would be a valuable component in topical personal care products aimed at contraception and BV prophylaxis and treatment.