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Uptake and metabolism of α‐mangostin by human cell lines: HepG2 liver cells, HT‐29 colon cells, and THP‐1 macrophage‐like cells
Author(s) -
Orozco Fabiola Gutierrez,
Chitchumroonchokchai Chureeporn,
Riedl Kenneh M,
Schwartz Steven J
Publication year - 2012
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.26.1_supplement.646.17
Subject(s) - garcinia mangostana , metabolism , garcinia , cell culture , chemistry , biochemistry , intracellular , cell growth , cell , sulfation , pharmacology , biology , traditional medicine , botany , medicine , genetics
Xanthones present in the pericarp of mangosteen fruit ( Garcinia mangostana L.) possess a distinct isoprenylated tricyclic structure and have been reported to exhibit anti‐inflammatory and anti‐proliferative/ pro‐apoptotic activities. However, information on the absorption, metabolism and in vivo efficacy of xanthones remains elusive. Recent results from our lab show that ingested xanthones and their phase 2 metabolites are present in several tissues of mice. This study investigated the uptake and metabolism of α‐mangostin (α‐MG) by human liver, colon, and macrophage‐like cell lines. Free and conjugated (glucuronidated/sulfated) α–MG were analyzed by RP‐HPLC. Our results suggest that degree of uptake, metabolism and intracellular retention of α–MG is dependent on cell type. HepG2 readily accumulated free α–MG in cells. The conjugated α–MG was the majority detected in HT‐29 cells. α–MG content in THP‐1 cells was low and conjugates were predominant. Conversion of α–MG to other xanthones also was observed. LC‐MS‐MS analysis confirmed γ‐MG and 9‐ hydroxycalabaxanthone in HepG2 medium and cells. Other xanthones present in HepG2 and HT‐29 cells remain to be identified. These data suggest cell‐specific metabolism of α–MG. Mass spectrometric analysis and study of anti‐inflammatory activity of α–MG and metabolites are ongoing. Grant Funding Source : OSU Food Innovation Center, Nutrient and Phytochemical Analytic Shared Resource and Conacyt Fellowship (Mexico)