Pharmacokinetic Properties of Moracin C in Mice

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초록

Moracin C from Morus alba fruits, also known as the mulberry, has been proven to exhibit inhibitory activities against lipoxygenase enzymes, TNF- alpha and interleukin-1 beta secretion, and proprotein convertase subtilisin/kexin type 9 expression. Despite the various pharmacological activities of moracin C, its pharmacokinetic characteristics have yet to be reported. Here, the pharmacokinetic parameters and tissue distribution of moracin C have been investigated in mice, and the plasma concentration of moracin C with multiple dosage regimens was simulated via pharmacokinetic modeling. Our results showed that moracin C was rapidly and well absorbed in the intestinal tract, and was highly distributed in the gastrointestinal tract, liver, kidneys, and lungs. Moracin C was distributed in the ileum, cecum, colon, and liver at a relatively high concentration compared with its plasma concentration. It was extensively metabolized in the liver and intestine, and its glucuronidated metabolites were proposed. In addition, the simulated plasma concentrations of moracin C upon multiple treatments (i.e., every 12 and 24h) were suggested. We suggest that the pharmacokinetic characteristics of moracin C would be helpful to select a disease model for in vivo evaluation. The simulated moracin C concentrations under various dosage regimens also provide helpful knowledge to support its pharmacological effect.

키워드

moracin C; mulberry; Morus alba; Moraceae; pharmacokinetics; tissue distribution; LC-MS; MS; simulation; ALBA L. FRUIT; MORUS-ALBA; TISSUE DISTRIBUTION; NATURAL-PRODUCTS; ALPHA-MANGOSTIN; ISOLIQUIRITIGENIN; METABOLISM; EXPOSURE; EFFICACY
제목
Pharmacokinetic Properties of Moracin C in Mice
저자
You, Byoung Hoon; BasavanaGowda, Melanayakanakatte Kuberappa; Lee, Jae Un; Chin, Young-Won; Choi, Won Jun; Choi, Young Hee
DOI
10.1055/a-1321-1519
발행일
2021-07
유형
Article
저널명
Planta Medica
권
87
호
08
페이지
642 ~ 651