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Biotransformation of Glucoaurantio-Obtusin Towards Aurantio-Obtusin Increases the Toxicity of Irinotecan Through Increased Inhibition Towards SN-38 Glucuronidation

Biotransformation of Glucoaurantio-Obtusin Towards Aurantio-Obtusin Increases the Toxicity of Irinotecan Through Increased Inhibition Towards SN-38 Glucuronidation

Jian Yu, Jing-Chun Han, Ya-Jie Gao

Phytother Res. 2014 Oct;28(10):1577-80.

PMID: 24842785

Abstract:

The present study aims to investigate the influence of irinotecan's toxicity by the biotransformation of glucoaurantio-obtusin to aurantio-obtusin. Intraperitoneal administration (i.p.) of 100 mg/kg aurantio-obtusin significantly increased the toxicity of irinotecan, but the i.p. administration of 100 mg/kg glucoaurantio-obtusin showed negligible influence towards irinotecan's toxicity. Furthermore, the mechanism was explained through determining the inhibition potential of glucoaurantio-obtusin and aurantio-obtusin towards the glucuronidation metabolism of SN-38 that has been regarded to be the major active product responsible for the toxicity of irinotecan. The results showed that aurantio-obtusin exhibited strong competitive inhibition towards the glucuronidation of SN-38, but negligible inhibition potential of glucoaurantio-obtusin towards SN-38 glucuronidation was observed. These results showed that biotransformation of glucoaurantio-obtusin towards aurantio-obtusin increased the toxicity of irinotecan through increased inhibition of SN-38 glucuronidation.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP67979253	Aurantio-obtusin		67979-25-3	Price

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