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[Nandeshi: a powerful inhibitor of human acrosin activity]. 2009

Gui-Hong Song, and Jue Zhang, and Xiao-Meng Zhang, and Wei-Wei Ning, and Ya-Zhong Ji, and Ning Hui, and Ya-Nan Zhao, and You-Jun Zhou, and Ju Zhu, and Jia-Guo Lü
Research Center of Reproductive Medicine, Changhai Hospital, 2. School of Pharmacology, The Second Military, Shanghai 200433, China.

OBJECTIVE To evaluate the inhibitory effect of Nandeshi, an acrosin inhibitor, on human acrosin activity. METHODS We collected sperm samples from 10 healthy fertile men and cultured them with Nandeshi at 30 degrees C for 5 minutes at the concentrations of 0. 100, 0.120, 0.144, 0.173, 0.207, 0.249, 0.299, 0.358 and 0.430 mmol/L, with the controls treated with a well-known acrosin inhibitor N-alpha-p-tosyl-L-lysine chloromethylketone (TLCK) at 150.0, 189.8, 213.6, 240.3, 270.3, 304.1 and 342.1 mmol/L. Then we determined the residual activity of human acrosin by improved Kennedy assay. RESULTS The residual activity of acrosin was negatively correlated with the Nandeshi concentration, and Nandeshi exhibited an inhibition rate about 800 times that of TLCK. CONCLUSIONS Nandeshi has a powerful inhibitory effect on human acrosin, and improved Kennedy assay is a simple, practical and highly sensitive technique for the detection of human acrosin activity.

UI MeSH Term Description Entries
D008297 Male Males
D003271 Contraceptive Agents, Female Chemical substances or agents with contraceptive activity in females. Use for female contraceptive agents in general or for which there is no specific heading. Contraceptives, Female,Agents, Female Contraceptive,Female Contraceptive Agents,Female Contraceptives
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000176 Acrosin A trypsin-like enzyme of spermatozoa which is not inhibited by alpha 1 antitrypsin. Acrosomal proteinase,Akrosin,M beta-Acrosin,M beta Acrosin,beta-Acrosin, M,proteinase, Acrosomal
D013094 Spermatozoa Mature male germ cells derived from SPERMATIDS. As spermatids move toward the lumen of the SEMINIFEROUS TUBULES, they undergo extensive structural changes including the loss of cytoplasm, condensation of CHROMATIN into the SPERM HEAD, formation of the ACROSOME cap, the SPERM MIDPIECE and the SPERM TAIL that provides motility. Sperm,Spermatozoon,X-Bearing Sperm,X-Chromosome-Bearing Sperm,Y-Bearing Sperm,Y-Chromosome-Bearing Sperm,Sperm, X-Bearing,Sperm, X-Chromosome-Bearing,Sperm, Y-Bearing,Sperm, Y-Chromosome-Bearing,Sperms, X-Bearing,Sperms, X-Chromosome-Bearing,Sperms, Y-Bearing,Sperms, Y-Chromosome-Bearing,X Bearing Sperm,X Chromosome Bearing Sperm,X-Bearing Sperms,X-Chromosome-Bearing Sperms,Y Bearing Sperm,Y Chromosome Bearing Sperm,Y-Bearing Sperms,Y-Chromosome-Bearing Sperms
D014107 Tosyllysine Chloromethyl Ketone An inhibitor of SERINE ENDOPEPTIDASES. Acts as an alkylating agent and is known to interfere with the translation process. Chlorotosylamidoaminoheptanone,TLCK,Tosyllysyl Chloromethane,Chloromethane, Tosyllysyl,Chloromethyl Ketone, Tosyllysine,Ketone, Tosyllysine Chloromethyl

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