Stereoselective glucuronidation of carvedilol by Chinese liver microsomes

You, Linya; Yu, Chunna; Xie, Sheng; Chen, Shuqing; Zeng, Su

doi:10.1631/jzus.2007.b0756

Cited by 5 publications

(5 citation statements)

References 26 publications

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“…Following incubation at 37°C for 1 hour, the reactions were terminated by adding cold acetonitrile containing IS. After centrifugation, aliquots of the supernatant were analyzed by LC-MS/MS as described previously (You et al, 2007;Hauser et al, 2008;Sten et al, 2009b;Joo et al, 2014). The selected reaction monitoring transitions and collision energies determined for each metabolite are listed in Table 1.…”

Section: Methodsmentioning

confidence: 99%

Ginsenoside Rc Is a New Selective UGT1A9 Inhibitor in Human Liver Microsomes and Recombinant Human UGT Isoforms

et al. 2019

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Ginseng is known to have inhibitory effects on UGT1A9 activity. However, little is known about the inhibitory effects of ginsenosides, the major active compounds in ginseng, on UGT1A9 activity. In vitro investigation of UGT1A9 inhibition by ginsenosides was carried out using human liver microsomes (HLMs). Among 10 ginsenosides, ginsenoside Rc was the strongest inhibitor of UGT1A9-mediated mycophenolic acid glucuronidase activity. Further inhibition kinetic studies using HLMs suggested that ginsenoside Rc competitively and noncompetitively inhibited UGT1A9-mediated propofol and mycophenolic acid glucuronidation activities, with K i values of 2.83 and 3.31 mM, respectively. Next, to investigate whether the inhibitory effect of ginsenoside Rc is specific to the UGT1A9 isoform, we studied the inhibitory potency of ginsenoside Rc on nine human uridine diphospho-glucuronosyltransferase (UGT) activities using recombinant human UGT isoforms. Ginsenoside Rc exhibited a 12.9-fold selectivity (which was similar to niflumic acid at 12.5-fold) for UGT1A9 inhibition. Ginsenoside Rc at 50 mM also inhibited none of the other UGT isoform-specific activities above 12.0%, except for UGT1A9 (>91.5%) in HLMs, indicating that ginsenoside Rc might be used as a selective UGT1A9 inhibitor in reaction phenotyping studies of new chemical entities. Considering lower plasma concentrations (0.01 mM) of ginsenoside Rc in healthy subjects and no induction potential on UGT isoforms, ginsenoside Rc does not cause pharmacokinetic drug interactions with other coadministered drugs metabolized by UGT1A9. SIGNIFICANCE STATEMENT Ginsenoside Rc selectively inhibited UGT1A9-mediated propofol and mycophenolic acid glucuronidation activities in human liver microsomes and recombinant uridine diphospho-glucuronosyltransferase (UGT) isoforms. It exhibited a 12.9-fold selectivity for UGT1A9 inhibition. Therefore, ginsenoside Rc might be used as a selective UGT1A9 inhibitor in reaction phenotyping studies of new chemical entities, such as niflumic acid.

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Section: Methodsmentioning

confidence: 99%

Ginsenoside Rc Is a New Selective UGT1A9 Inhibitor in Human Liver Microsomes and Recombinant Human UGT Isoforms

et al. 2019

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“…GNNR was established as a National Forest Reserve in 1975, and became a National Nature Reserve in 2001. The site is characterized by subtropical monsoon climate, with a mean annual temperature of 15.3uC and receives an average of 1964 mm of rain annually [30]. The topography is relatively undulating.…”

Section: Study Site and Data Collectionmentioning

confidence: 99%

“…The parent rock of the mountain range is granite, with soil pH ranging from 5.5 to 6.5 [31]. The predominant vegetation type of GNNR is subtropical evergreen broad-leaved forest [30]. A large portion of broad-leaved forests in the GNNR is in advanced successional stages [29] and a total of 1426 seed-plant species of 648 genera and 149 families have been recorded as occurring naturally in the GNNR, which covers 8107 ha in total [31].…”

Section: Study Site and Data Collectionmentioning

confidence: 99%

Correction: Topographic Variation in Aboveground Biomass in a Subtropical Evergreen Broad-Leaved Forest in China

Lin¹,

Lai²,

Muller‐Landau³

et al. 2013

PLoS ONE

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The subtropical forest biome occupies about 25% of China, with species diversity only next to tropical forests. Despite the recognized importance of subtropical forest in regional carbon storage and cycling, uncertainties remain regarding the carbon storage of subtropical forests, and few studies have quantified within-site variation of biomass, making it difficult to evaluate the role of these forests in the global and regional carbon cycles. Using data for a 24-ha census plot in east China, we quantify aboveground biomass, characterize its spatial variation among different habitats, and analyse species relative contribution to the total aboveground biomass of different habitats. The average aboveground biomass was 223.0 Mg ha 21 (bootstrapped 95% confidence intervals [217.6, 228.5]) and varied substantially among four topographically defined habitats, from 180.6 Mg ha 21 (bootstrapped 95% CI [167.1, 195.0]) in the upper ridge to 245.9 Mg ha 21 (bootstrapped 95% CI [238.3, 253.8]) in the lower ridge, with upper and lower valley intermediate. In consistent with our expectation, individual species contributed differently to the total aboveground biomass of different habitats, reflecting significant species habitat associations. Different species show differently in habitat preference in terms of biomass contribution. These patterns may be the consequences of ecological strategies difference among different species. Results from this study enhance our ability to evaluate the role of subtropical forests in the regional carbon cycle and provide valuable information to guide the protection and management of subtropical broad-leaved forest for carbon sequestration and carbon storage.

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“…The substituents (X) on benzene-ring are H, F and Cl. The starting compounds 1m and 2n were synthesized according to literature 6,11,14,27,28 . In the DE-mXn series, the DE-mX6 series of products are excepted because of the corresponding ω-bromoheptanoic acid is hard to obtain from reagent marketplace.…”

Section: Synthesismentioning

confidence: 99%

Synthesis and Properties of Dimesogenic Compounds Containing Cholesterol and 4‐(trans‐4‐n‐Alkylcyclohexyl)‐benzoic Acid Moieties

Yu¹,

Hou²,

Chen³

et al. 2009

Chin. J. Chem.

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A series of novel dimesogenic compounds containing cholesterol and 4-(trans-4-n-alkylcyclohexyl)benzoic acid moieties were synthesized. The two mesogenic units of these compounds are linked with ω-oxyalkanoyl spacers of varying lengths. The chemical structure and mesomorphic properties of this series of compounds were characterized by FT-IR, MS, 1 H NMR, polarizing optical microscopy (POM) and DSC techniques. The average viscosity and helical twisting power (HTP) in host liquid crystals of selected dimesogenic compounds were also measured. It was found that most of the present novel series of compounds exhibited only cholesteric mesophase with lower phase transition temperatures, and the average viscosity and HTP of selected compounds were similar to or superior to cholesteryl nonylate.

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Stereoselective glucuronidation of carvedilol by Chinese liver microsomes

Cited by 5 publications

References 26 publications

Ginsenoside Rc Is a New Selective UGT1A9 Inhibitor in Human Liver Microsomes and Recombinant Human UGT Isoforms

Ginsenoside Rc Is a New Selective UGT1A9 Inhibitor in Human Liver Microsomes and Recombinant Human UGT Isoforms

Correction: Topographic Variation in Aboveground Biomass in a Subtropical Evergreen Broad-Leaved Forest in China

Synthesis and Properties of Dimesogenic Compounds Containing Cholesterol and 4‐(trans‐4‐n‐Alkylcyclohexyl)‐benzoic Acid Moieties

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