Background:

IC50: 9 μM

Conduritol B epoxide is a β-glucosidase inhibitor.

β-glucosidase catalyzes the hydrolysis of the glycosidic bond to terminal non-reducing residues in β-D-glucosides and oligosaccharides, with release of glucose.

In vitro: Conduritol B epoxide was identifies as an active-site-directed inhibitor of some glucosidases. The inactivation of α-glucosidase from Monascus ruber by conduritol B epoxide was found to be irreversible and first-order with respect to time and inhibitor concentration. The inactivation could be prevented in the presence of maltose [1].

In vivo: The time course of the distribution of [3H]conduritol B epoxide was determined in various organs of mice, which had received a single i.p. dose. Results showd that the epoxide was rapidly distributed over all tissues except brain, indicating that the epoxide could pass the blood/brain barrier only with difficulty. A 4-fold enrichment was observed in the kidney. [3H]conduritol B epoxide was excreted with a half-life of about 7 h. A parallel determination of beta-glucosidase activity in the tissues showed greater than 90% inhibition within 1 and 2 h and a beginning recovery between 4 and 12 h. The only exception was brain, where no effects could be found after 1 h and a subsequent decrease to 37% of normal was seen after 12 h [2].

Clinical trial: So far, no clinical study has been conducted.

参考文献:
[1] Yang SJ, Ge SG, Zeng YC, Zhang SZ.  Inactivation of alpha-glucosidase by the active-site-directed inhibitor, conduritol B epoxide. Biochim Biophys Acta. 1985 Apr 29;828(3):236-40.
[2] Stephens MC, Bernatsky A, Singh H, Kanfer JN, Legler G.  Distribution of conduritol B epoxide in the animal model for Gaucher's disease (Gaucher mouse). Biochim Biophys Acta. 1981 Jan 7;672(1):29-32.