Characterization of osthenol metabolism in vivo and its pharmacokinetics

  title={Characterization of osthenol metabolism in vivo and its pharmacokinetics},
  author={Pil Joung Cho and Su Min Choi and Younah Kim and Doohyun Lee and Ye Eun Noh and Sujeong Kim and Ju Hyun Kim and Taeho Lee and Sangkyu Lee},
  pages={839 - 846}
Abstract Osthenol, a prenylated coumarin, is a C8-prenylated derivative of umbelliferone isolated from the root of Angelica koreana and Angelica dahurica, an intermediate and is known as a major metabolite of desmethyl-osthole. The various pharmacological effects of osthenol have been reported. In previous studies, we investigated five hydroxylated metabolites by cytochromes P450 (CYP) and glucuronide conjugates of osthenol by uridine diphosphate-glucuronosyltransferases (UGTs). However… Expand
2 Citations
Identification of suberosin metabolites in human liver microsomes by high-performance liquid chromatography combined with high-resolution quadrupole-orbitrap mass spectrometer.
Suberosin is a natural prenylated coumarin derivative isolated from Citropsis articulata. It has various pharmacological properties, especially as an anticoagulant, for which it has been used sinceExpand
HPLC-MS/MS studies of brimonidine in rabbit aqueous humor by microdialysis.
The pharmacokinetic study showed that the AUC(0-t) of in situ gel was 3.5-times than that of eyedrops, which significantly improve the bioavailability of brimonidine. Expand


Characterization of CYPs and UGTs Involved in Human Liver Microsomal Metabolism of Osthenol
This study elucidated the structure of generated metabolites using a high-resolution quadrupole-orbitrap mass spectrometer and characterized the major human cytochrome P450 and uridine 5′-diphospho-glucuronosyltransferase (UGT) isozymes involved in osthenol metabolism in human liver microsomes (HLMs). Expand
Isolation and identification of metabolites of osthole in rats
  • X. Lv, C. Wang, +10 authors X.-C. Ma
  • Chemistry, Medicine
  • Xenobiotica; the fate of foreign compounds in biological systems
  • 2012
On the basis of the metabolites profile, a possible metabolic pathway for Ost metabolism in rats has been proposed and this is the first systematic study on the phases I and II metabolites of 8-isopentenoxy-coumarin derivative. Expand
Metabolic map of osthole and its effect on lipids
The insights about the metabolic pathways of osthole in vivo, including hydroxylation, glucuronidation, and sulfation are given, as well as the levels of the lipids regulated by osthole indicated its potential effects on adipogenesis. Expand
Osthenol, a prenylated coumarin, as a monoamine oxidase A inhibitor with high selectivity.
Osthenol, a prenylated coumarin isolated from the dried roots of Angelica pubescens, potently and selectively inhibited recombinant human monoamine oxidase-A (hMAO-A) and can be regarded a potential lead compound for the design of novel reversible MAo-A inhibitors. Expand
Metabolism and Disposition of Acetaminophen: Recent Advances in Relation to Hepatotoxicity and Diagnosis
Recent data providing novel insights into these processes, particularly in humans, are reviewed in the context of earlier work, and the effects of altered metabolism and reactive metabolite formation are discussed. Expand
Antitumor effects of Osthol from Cnidium monnieri: an in vitro and in vivo study
It is suggested that osthol could inhibit P‐388 D1 cells in vivo and induce apoptosis in HeLa cells in vitro, and that ost hol is good lead compound for developing antitumor drugs. Expand
Inhibitors of 5alpha -reductase type I in LNCaP cells from the roots of Angelica koreana.
Two compounds, a prenylated coumarin, osthenol and a sesquiterpene, have been isolated as active principles with 5alpha-reductase type I inhibitory effects in LNCaP cells from the roots of Angelica koreana Max. Expand
A coumarin-specific prenyltransferase catalyzes the crucial biosynthetic reaction for furanocoumarin formation in parsley.
The results demonstrate that a single prenyltransferase, such as PcPT, opens the pathway to linear furanocoumarins in parsley, but may also catalyze the synthesis of osthenol, the first intermediate committed to the angular furanOCoumarin pathway, in other plants. Expand
Separation and quantitative analysis of coumarin compounds from Angelica dahurica (Fisch. ex Hoffm) Benth. et Hook. f by pressurized capillary electrochromatography.
A pressurized capillary electrochromatography method with post-column detection cell has been developed for the therapeutically important coumarins from Angelica dahurica extract and showed satisfactory retention time and peak area repeatability with the first use of post- column detection cell in the pCEC instrument. Expand
Antitumor-promoting activity of coumarins from citrus plants.
Osthenol exhibited a marked inhibitory effect on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test and 9-substituted coumarins, including dihydroosthenon, were found to significantly inhibit EBV-EA activation. Expand