| HOME | HELP | FEEDBACK | SUBSCRIPTIONS | ARCHIVE | SEARCH | TABLE OF CONTENTS |
|
|
|
|||||||
|
|||||||||
Biology of Reproduction, Vol 58, 1515-1526, Copyright © 1998 by Society for the Study of Reproduction
ARTICLES |
OJ D'Cruz, P Ghosh and FM Uckun
Department of Reproductive Biology, Wayne Hughes Institute, Roseville, Minnesota 55113, USA. odcruz@ih.org
We have used computer-assisted sperm analysis (CASA) to evaluate the spermicidal activity of 8 metallocene dihalides (vanadocene dichloride [VDC], titanocene dichloride [TDC], zirconocene dichloride [ZDC], molybdocene dichloride [MDC], hafnocene dichloride [HDC], vanadocene dibromide [VDB], bis[methylcyclopentadienyl] vanadium dichloride [VMDC], and vanadocene diiodide [VDI]); 5 vanadocene di-pseudohalides (vanadocene diazide [VDA], vanadocene dicyanide [VDCN], vanadocene dioxycyanate [VDOCN], vanadocene dithiocyanate [VDSCN], and vanadocene diselenocyanate [VDSeCN]); and 3 disubstituted derivatives (vanadocene ditriflate [VDT], vanadocene monochloro oxycyanate [VDCO], and vanadocene monochloro acetonitrilo tetrachloro ferrate [VDFe]). Whereas the metallocene complexes containing titanium, zirconium, molybdenum, and hafnodium were inactive, all 12 vanadocene complexes elicited potent spermicidal activity at nano-micromolar concentrations with an order of efficacy VDSeCN > VDSCN > VDB > VMDC > VDCN > VDA > VDC > VDOCN > VDI > VDT > VDFe > VDCO without disrupting the acrosomal membrane, as determined by high-resolution low-voltage scanning electron microscopy. The sperm-immobilizing activity of the vanadocene complexes was rapid and irreversible, since the treated sperm underwent apoptosis as determined by the flow cytometric annexin V binding assay, DNA nick end-labeling, and confocal laser scanning microscopy. These results provide unprecedented evidence that metallocene complexes containing vanadium(IV), especially VDSeCN, may be useful as contraceptive agents.
This article has been cited by other articles:
|
|
 |
|
  O. J. D'Cruz and F. M. Uckun Preclinical Evaluation of a Dual-Acting Microbicidal Prodrug WHI-07 in Combination with Vanadocene Dithiocarbamate in the Female Reproductive Tract of Rabbit, Pig, and Cat Toxicol Pathol, December 1, 2007; 35(7): 910 - 927. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 R.K. Jain, J.P. Maikhuri, S.T.V.S. Kiran Kumar, V.L. Sharma, A.K. Dwivedi, K. Mitra, V.K. Bajpai, and G. Gupta Novel disulphide esters of carbothioic acid as potent, non-detergent spermicides with low toxicity to Lactobacillus and HeLa cells in vitro Hum. Reprod., March 1, 2007; 22(3): 708 - 716. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 O. J. D'Cruz and F. M. Uckun Discovery of 2,5-dimethoxy-substituted 5-bromopyridyl thiourea (PHI-236) as a potent broad-spectrum anti-human immunodeficiency virus microbicide Mol. Hum. Reprod., October 1, 2005; 11(10): 767 - 777. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 J. K. Jain, A. Li, D. L. Nucatola, P. Minoo, and J. C. Felix Nonoxynol-9 Induces Apoptosis of Endometrial Explants by Both Caspase-Dependent and -Independent Apoptotic Pathways Biol Reprod, August 1, 2005; 73(2): 382 - 388. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
O. J. D'Cruz, P. Samuel, and F. M. Uckun PHI-443: A Novel Noncontraceptive Broad-Spectrum Anti-Human Immunodeficiency Virus Microbicide Biol Reprod, December 1, 2004; 71(6): 2037 - 2047. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 M. Muratori, I. Porazzi, M. Luconi, S. Marchiani, G. Forti, and E. Baldi Annexin V Binding and Merocyanine Staining Fail to Detect Human Sperm Capacitation J Androl, September 1, 2004; 25(5): 797 - 810. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 O. J. D'Cruz, B. Waurzyniak, and F. M. Uckun Antiretroviral Spermicide WHI-07 Prevents Vaginal and Rectal Transmission of Feline Immunodeficiency Virus in Domestic Cats Antimicrob. Agents Chemother., April 1, 2004; 48(4): 1082 - 1088. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. Muratori, M. Maggi, S. Spinelli, E. Filimberti, G. Forti, and E. Baldi Spontaneous DNA Fragmentation in Swim-Up Selected Human Spermatozoa During Long Term Incubation J Androl, March 1, 2003; 24(2): 253 - 262. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
O. J. D'Cruz, T. K. Venkatachalam, C. Mao, S. Qazi, and F. M. Uckun Structural Requirements for Potent Anti-Human Immunodeficiency Virus (HIV) and Sperm-Immobilizing Activities of Cyclohexenyl Thiourea and Urea Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase Biol Reprod, December 1, 2002; 67(6): 1959 - 1974. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
E. T. Donnelly, M. O'Connell, N. McClure, and S. E.M. Lewis Differences in nuclear DNA fragmentation and mitochondrial integrity of semen and prepared human spermatozoa Hum. Reprod., July 1, 2000; 15(7): 1552 - 1561. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
O. J. D'Cruz, T. K. Venkatachalam, and F. M. Uckun Novel Thiourea Compounds as Dual-Function Microbicides Biol Reprod, July 1, 2000; 63(1): 196 - 205. [Abstract] [Full Text]
|
|
|
|
|
|
O. J. D'Cruz, A. Vassilev, and F. M. Uckun Studies in Humans on the Mechanism of Potent Spermicidal and Apoptosis-Inducing Activities of Vanadocene Complexes Biol Reprod, April 1, 2000; 62(4): 939 - 949. [Abstract] [Full Text]
|
|
|
|
|
|
O. J. D'Cruz, T. K. Venkatachalam, and F. M. Uckun Structural Requirements for Potent Human Spermicidal Activity of Dual-Function Aryl Phosphate Derivative of Bromo-Methoxy Zidovudine (Compound WHI-07) Biol Reprod, January 1, 2000; 62(1): 37 - 44. [Abstract] [Full Text]
|
|
|
|
 |
|
 E. A. Sudbeck, X.-P. Liu, R. K. Narla, S. Mahajan, S. Ghosh, C. Mao, and F. M. Uckun Structure-based Design of Specific Inhibitors of Janus Kinase 3 as Apoptosis-inducing Antileukemic Agents Clin. Cancer Res., June 1, 1999; 5(6): 1569 - 1582. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
O. J. D'Cruz and F. M. Uckun Novel Derivatives of Phenethyl-5-Bromopyridylthiourea and Dihydroalkoxybenzyloxopyrimidine Are Dual-Function Spermicides with Potent Anti-Human Immunodeficiency Virus Activity Biol Reprod, June 1, 1999; 60(6): 1419 - 1428. [Abstract] [Full Text]
|
|
|
|
|
|
O. J. D'Cruz, M.-J. Shih, S. H. Yiv, C.-L. Chen, and F. M. Uckun Synthesis, characterization and preclinical formulation of a dual-action phenyl phosphate derivative of bromo-methoxy zidovudine (compound WHI-07) with potent anti-HIV and spermicidal activities Mol. Hum. Reprod., May 1, 1999; 5(5): 421 - 432. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
O. J. D'Cruz, Y. Dong, and F. M. Uckun Spermicidal Activity of Oxovanadium(IV) Complexes of 1,10-Phenanthroline, 2,2'-Bipyridyl, 5'-Bromo-2'-Hydroxyacetophenone and Derivatives in Humans Biol Reprod, February 1, 1999; 60(2): 435 - 444. [Abstract] [Full Text] [PDF]
|
|
| HOME | HELP | FEEDBACK | SUBSCRIPTIONS | ARCHIVE | SEARCH | TABLE OF CONTENTS |
