Enhanced absorption and inhibited metabolism of emodin by 2, 3, 5, 4′-tetrahydroxystilbene-2- O-β -D-glucopyranoside: Possible mechanisms for Polygoni Multiflori Radix-induced liver injury
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Abstract
Polygoni Multiflori Radix (PMR) has been commonly used as a tonic in China for centuries.
However, PMR-associated hepatotoxicity is becoming a safety issue. In our previous
in vivo study, an interaction between stilbenes and anthraquinones has been discovered
and a hypothesis is proposed that the interaction between stilbene glucoside-enriching
fraction and emodin may contribute to the side effects of PMR. To further support
our previous in vivo results in rats, the present in vitro study was designed
to evaluate the effects of 2, 3, 5, 4′-tetrahydroxystilbene-2- O - β -D-glucopyranoside
(TSG) on the cellular absorption and human liver microsome metabolism of emodin. The
obtained results indicated that the absorption of emodin in Caco-2 cells was enhanced
and the metabolism of emodin in human liver microsomes was inhibited after TSG treatment.
The effects of the transport inhibitors on the cellular emodin accumulation were also
examined. Western blot assay suggested that the depressed metabolism of emodin could
be attributed to the down-regulation of UDP-glucuronosyltransferases (UGTs) 1A8, 1A10,
and 2B7. These findings definitively demonstrated the existence of interaction between
TSG and emodin, which provide a basis for a better understanding of the underlying
mechanism for PMR-induced liver injury.
Author and article information
Journal
Title:
Chinese Journal of Natural Medicines
Abbreviated Title:
Chinese Journal of Natural Medicines