2. Academic Validation
  3. Metabolic degradation of lentinan in liver mediated by CYP450 enzymes and epoxide hydrolase

Metabolic degradation of lentinan in liver mediated by CYP450 enzymes and epoxide hydrolase

  • Carbohydr Polym. 2021 Feb 1;253:117255. doi: 10.1016/j.carbpol.2020.117255.
Ziming Zheng 1,  Yu Zhang 1,  Yuxuan Liu 1,  Jinglin Wang 1,  Zheng Cui 1,  Xianglin Pan 1,  Yan Liu 2,  Wenqi Tang 2,  Kaiping Wang 3
Affiliations

Affiliations

  • 1 Department of Pharmacy, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, 430030 Wuhan, PR China; Hubei Province Clinical Research Center for Precision Medicine for Critical Illness, 430030 Wuhan, PR China.
  • 2 Hubei Key Laboratory of Nature Medicinal Chemistry and Resource Evaluation, Tongji Medical College of Pharmacy, Huazhong University of Science and Technology, 430030 Wuhan, PR China.
  • 3 Hubei Key Laboratory of Nature Medicinal Chemistry and Resource Evaluation, Tongji Medical College of Pharmacy, Huazhong University of Science and Technology, 430030 Wuhan, PR China. Electronic address: [email protected].
PMID: 33279005 DOI: 10.1016/j.carbpol.2020.117255
Abstract

Lentinan (LNT), a typical triple helix β-glucan, has been widely used as drug and biomaterial. However, its pharmacokinetics in vivo is rarely reported, which severely limits its further development and application. The aim of this study is to establish a sensitive method for detecting LNT in biosamples and to evaluate the plasma level, tissue distribution and metabolic degradation of LNT in rats. 5-([4,6-Dichlorotriazin-2-yl] amino) fluorescein (DTAF) was labelled to LNT. After purification and identification, FLNT was intravenously administered to rats at dose of 32 mg/kg. LNT was predominantly incorporated into the liver and liver microsomes were used to study the degradation mechanism of LNT in the liver. The results showed that two Cytochrome P450 (CYP450) enzymes subtypes (CYP2D6 and CYP2C9), as well as Epoxide Hydrolase, were involved in the metabolic degradation of LNT. These findings provide a pharmacokinetic reference for further study and application of LNT and other β-glucans.

Keywords

CYP450; Epoxide hydrolase; Lentinan; Metabolic degradation; Tissue distribution.

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