Document Detail

AF-2364 is a prospective spermicide candidate.
MedLine Citation:
PMID:  20418891     Owner:  NLM     Status:  MEDLINE    
AbstractInhibition of sperm motility has recently become a promising target for male contraceptive development. AF-2364, an analogue of Lonidamine (LND), had a contraceptive effect when orally administered to adult Sprague-Dawley rats. LND can also target mitochondria to inhibit oxygen consumption and block energy metabolism in tumour cells. However, there are no reports of the effects of AF-2364 on human sperm function. Herein we describe the action of AF-2364 on human sperm in vitro, as well as the mechanisms involved. AF-2364 specifically blocked human sperm motility in vitro. Further experiments revealed that AF-2364 can target sperm mitochondrial permeability transition (MPT) pores to induce the loss of sperm mitochondrial membrane potential (DeltaPsim) and decrease ATP generation; however, no significant changes in the cytoskeletal network or the human sperm proteome were detected after exposure to AF-2364. Incubation of AF-2364 with other human or mouse cell lines indicated that the spermicidal effect at the lower concentration was specific. In summary, the spermicidal effect of AF-2364 involves direct action on sperm MPT pores, and this compound should be further investigated as a new spermicide candidate.
Hui Wang; Xiang-Xiang Chen; Li-Rong Wang; Yun-Dong Mao; Zuo-Min Zhou; Jia-Hao Sha
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-04-26
Journal Detail:
Title:  Asian journal of andrology     Volume:  12     ISSN:  1745-7262     ISO Abbreviation:  Asian J. Androl.     Publication Date:  2010 May 
Date Detail:
Created Date:  2010-05-03     Completed Date:  2010-08-05     Revised Date:  2013-09-17    
Medline Journal Info:
Nlm Unique ID:  100942132     Medline TA:  Asian J Androl     Country:  China    
Other Details:
Languages:  eng     Pagination:  322-35     Citation Subset:  IM    
Laboratory of Reproductive Medicine, Department of Histology and Embryology, Nanjing Medical University, Nanjing 210029, China.
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MeSH Terms
Adenosine Triphosphate / metabolism
Cell Line, Tumor
Cell Survival / drug effects
Cyclosporine / pharmacology
Drug Therapy, Combination
Hydrazines / pharmacology*
Indazoles / pharmacology*
Mitochondria / drug effects
Permeability / drug effects
Seminal Plasma Proteins / analysis
Sperm Motility / drug effects
Spermatocidal Agents / pharmacology*
Spermatozoa / drug effects*,  metabolism,  pathology
Tetrazolium Salts / metabolism
Thiazoles / metabolism
Reg. No./Substance:
0/1-(2,4-dichlorobenzyl)indazole-3-carbohydrazide; 0/Hydrazines; 0/Indazoles; 0/Seminal Plasma Proteins; 0/Spermatocidal Agents; 0/Tetrazolium Salts; 0/Thiazoles; 298-93-1/thiazolyl blue; 56-65-5/Adenosine Triphosphate; 59865-13-3/Cyclosporine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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