title: Inhibition of rabbit sperm acrosomal enzymes by gossypol.
abstract: The effect of gossypol on the activities of 10 acrosomal enzymes of the rabbit sperm was evaluated. Acrosin, Azocoll proteinase, neuraminidase, and arylsulfatase were significantly inhibited or completely inactivated by 12-76 microM gossypol. Hyaluronidase, beta-glucuronidase, and acid phosphatase were inhibited only at a higher concentration of gossypol (380 microM). Phospholipase C, alkaline phosphatase, and beta-N-Acetyl glucosaminidase were not inhibited even at 380 microM gossypol. Gossypol was found to be a noncompetitive inhibitor of arylsulfatase with a Ki of 120 microM. The inhibition was reversible and dose-dependent. As the acrosomal enzymes were more sensitive to the inhibition by gossypol compared to sperm enzymes involved in glycolysis or energy production, these assays may serve as a more reliable indicator for monitoring the occurrence of gossypol-induced sterility.
authors.affiliation: Department of Biochemistry, University of Georgia, Athens 30602, USA.
authors.forename: Y Y
authors.initials: YY
authors.lastname: Yuan
authors.forename: Q X
authors.initials: QX
authors.lastname: Shi
authors.forename: P N
authors.initials: PN
authors.lastname: Srivastava
mesh_terms: D000118:Acetylglucosaminidase / Q000037:antagonists & inhibitors; D000135:Acid Phosphatase / Q000037:antagonists & inhibitors; D000176:Acrosin / Q000037:antagonists & inhibitors; D000177:Acrosome / Q000201:enzymology*; D000469:Alkaline Phosphatase / Q000037:antagonists & inhibitors; D000818:Animals; D001192:Arylsulfatases / Q000037:antagonists & inhibitors; D001391:Azo Compounds / Q000378:metabolism; D003094:Collagen / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D005966:Glucuronidase / Q000037:antagonists & inhibitors; D006072:Gossypol / Q000494:pharmacology*; D006821:Hyaluronoglucosaminidase / Q000037:antagonists & inhibitors; D006867:Hydrolases / Q000037:antagonists & inhibitors*; D007700:Kinetics; D008297:Male; D010447:Peptide Hydrolases / Q000378:metabolism; D011480:Protease Inhibitors / Q000494:pharmacology; D011817:Rabbits; D010738:Type C Phospholipases / Q000037:antagonists & inhibitors
chemical_list: D001391:Azo Compounds; D011480:Protease Inhibitors; D003094:Collagen; D006867:Hydrolases; D000469:Alkaline Phosphatase; D000135:Acid Phosphatase; D010738:Type C Phospholipases; D001192:Arylsulfatases; D005966:Glucuronidase; D006821:Hyaluronoglucosaminidase; D000118:Acetylglucosaminidase; D010447:Peptide Hydrolases; C039653:azocoll proteinase; D000176:Acrosin; D006072:Gossypol