| AF-2364 is a prospective spermicide candidate. | |
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MedLine Citation:
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PMID: 20418891 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Hui Wang; Xiang-Xiang Chen; Li-Rong Wang; Yun-Dong Mao; Zuo-Min Zhou; Jia-Hao Sha |
Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2010-04-26 |
Journal Detail:
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Title: Asian journal of andrology Volume: 12 ISSN: 1745-7262 ISO Abbreviation: Asian J. Androl. Publication Date: 2010 May |
Date Detail:
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Created Date: 2010-05-03 Completed Date: 2010-08-05 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 100942132 Medline TA: Asian J Androl Country: China |
Other Details:
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Languages: eng Pagination: 322-35 Citation Subset: IM |
Affiliation:
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Laboratory of Reproductive Medicine, Department of Histology and Embryology, Nanjing Medical University, Nanjing 210029, China. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Adenosine Triphosphate
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metabolism Animals Cell Line, Tumor Cell Survival / drug effects Cyclosporine / pharmacology Drug Therapy, Combination Humans Hydrazines / pharmacology* Indazoles / pharmacology* Male Mice 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 |
| Chemical | |
Reg. No./Substance:
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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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