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Biological activities of cyclophellitol.

S Atsumi1, H Iinuma, C Nosaka

  • 1Institute of Microbial Chemistry, Tokyo, Japan.

The Journal of Antibiotics
|December 1, 1990
PubMed
Summary

Cyclophellitol specifically inhibits almond beta-glucosidase, acting as a potent, irreversible inhibitor. This compound also shows strong inhibitory effects on beta-glucocerebrosidase in Molt-4 cells, with significant neurological effects observed in mice.

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Area of Science:

  • Biochemistry
  • Enzyme Inhibition
  • Pharmacology

Background:

  • Glycosidases are crucial enzymes involved in various biological processes.
  • Specific inhibitors are needed to study enzyme function and develop therapeutics.
  • Cyclophellitol is a compound with potential enzyme inhibitory properties.

Purpose of the Study:

  • To investigate the inhibitory activity of cyclophellitol against various glycosidases.
  • To determine the mechanism and specificity of cyclophellitol's inhibition.
  • To evaluate the in vivo effects of cyclophellitol administration.

Main Methods:

  • Enzyme inhibition assays were performed against nine different glycosidases.
  • Lineweaver-Burk plot analysis was used to determine the inhibition kinetics.
  • Fluorimetric assays and studies with synthetic substrates were employed.
  • In vivo studies in mice were conducted to assess neurological effects.

Main Results:

  • Cyclophellitol is a specific and potent inhibitor of almond beta-glucosidase (IC50 = 0.8 µg/ml), acting via a competitive and likely irreversible mechanism.
  • It showed weak activity against fungal beta-xylosidase but was inactive against other tested glycosidases.
  • Cyclophellitol strongly inhibited Molt-4 beta-glucocerebrosidase, exceeding the potency of known inhibitors like nojirimycin.
  • Mice treated with cyclophellitol exhibited severe neurological abnormalities resembling Gaucher's disease.

Conclusions:

  • Cyclophellitol is a highly specific irreversible inhibitor of almond beta-glucosidase and a potent inhibitor of beta-glucocerebrosidase.
  • Its significant neurological effects in mice suggest potential implications for studying lysosomal storage disorders.
  • Further research into cyclophellitol's mechanism and therapeutic potential is warranted.

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