Sulphated oligosaccharides as inhibitors of hyaluronidases from bovine testis, bee venom and Streptococcus agalactiae.
Potent and specific inhibitors of hyaluronidases, a group of enzymes preferentially catalysing the hydrolysis of hyaluronic acid, are not known so far. Such compounds could be useful as pharmacological tools for studying the physiological and pathophysiological role of both hyaluronan and hyaluronidases. The effects of sulphated and non-sulphated structurally different oligosaccharides on bovine testicular hyaluronidase, hyaluronidase from bee venom and hyaluronate lyase from Streptococcus agalactiae (hylB (4755)) were studied with the Morgan-Elson reaction. Several active compounds were identified within a series of sulphated beta-(1,4)-galacto-oligosaccharides. The determined IC (50) values of these sulphated oligosaccharides ranged from 4 microM to 630 microM for all hyaluronan-degrading enzymes. Sulphated oligosaccharides like verbascose, planteose and neomycin showed comparable inhibition on all hyaluronidases, thereby possessing 100 - 500 times the activity of the widely accepted hyaluronidase inhibitor apigenin.
Salmen
Sunnhild
S
Institute of Pharmacy, University of Regensburg, Regensburg, Germany.
Hoechstetter
Julia
J
Käsbauer
Christian
C
Paper
Dieter H
DH
Bernhardt
Günther
G
Buschauer
Armin
A
D000818:Animals; D001514:Bee Venoms / Q000201:enzymology; D001516:Bees; D002417:Cattle; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D006821:Hyaluronoglucosaminidase / Q000037:antagonists & inhibitors*; D020128:Inhibitory Concentration 50; D008297:Male; D009844:Oligosaccharides / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D010946:Plants, Medicinal; D013292:Streptococcus agalactiae / Q000201:enzymology*; D013431:Sulfates; D013737:Testis / Q000201:enzymology
D001514:Bee Venoms; D004791:Enzyme Inhibitors; D009844:Oligosaccharides; D010936:Plant Extracts; D013431:Sulfates; D006821:Hyaluronoglucosaminidase