Pharmacokinetic and Metabolic Profiling of Key Active Components of Dietary Supplement Magnolia officinalis Extract for Prevention against Oral Carcinoma.
Pharmacokinetic and Metabolic Profiling of Key Active Components of Dietary Supplement Magnolia officinalis Extract for Prevention against Oral Carcinoma.
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DOI:
10.1021/acs.jafc.0c01475
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发表时间:
2020-06-17
影响因子:
6.1
通讯作者:
Hu M
中科院分区:
文献类型:
--
作者:
Bui D;Li L;Yin T;Wang X;Gao S;You M;Singh R;Hu M
Among the three key active components (KACs) of Magnolia officinalis bark extract (ME), 4-O-methylhonokiol (MHNK) and honokiol (HNK) showed higher antiproliferation activities than magnolol (MGN) in the oral squamous cancer cell lines (Cal-27, SCC-9 and SCC-4). Oral bioavailabilities of ME-KACs were poor (<0.2%) in C57BL/6 mice primarily due to their extensive first-pass phase II metabolism and poor solubilities. High plasma concentration of glucuronides upon oral administration and faster rate of glucuronidation by intestinal microsomes indicated intestine as one of the major metabolic organs for ME-KACs. Despite the increase in bioavailabilities of ME-KACs (~8–10-folds) and decrease in AUC0–24 of glucuronides (~10-folds) upon ME solubility enhancement, systemic exposure of ME-KACs failed to improve meaningfully. In conclusion, we propose a quality-controlled and chemically-defined ME mixture, containing an optimized ratio of three KACs, delivered locally in the oral cavity as the most promising strategy for ME use as an oral cancer chemopreventive dietary supplement.
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影响因子:
5
作者:
Biersack B
通讯作者:
Biersack B
影响因子:
3
作者:
Hsieh, Shu-Feng;Chou, Chiang-Ting;Jan, Chung-Ren
通讯作者:
Jan, Chung-Ren
影响因子:
3.3
作者:
Lee YK;Yuk DY;Kim TI;Kim YH;Kim KT;Kim KH;Lee BJ;Nam SY;Hong JT
通讯作者:
Hong JT
影响因子:
6.1
作者:
Greenberg, Michael;Urnezis, Philip;Tian, Minmin
通讯作者:
Tian, Minmin
DOI:
10.1124/jpet.103.053496
发表时间:
2003-10-01
影响因子:
3.5
作者:
Hu, M;Chen, J;Lin, HM
通讯作者:
Lin, HM