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Tytuł:
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Inhibition of soluble epoxide hydrolase activity by compounds isolated from the aerial parts of Glycosmis stenocarpa.
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Autorzy:
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Kim JH; a College of Pharmacy, Chungnam National University , Daejeon , Republic of Korea .; b Virology Unit, Department of Horticultural Environment , National Institute of Horticultural and Herbal Science, RDA , Jeollabuk-Do , Republic of Korea .
Morgan AM; a College of Pharmacy, Chungnam National University , Daejeon , Republic of Korea .
Tai BH; a College of Pharmacy, Chungnam National University , Daejeon , Republic of Korea .; c Institute of Marine Biochemistry , and.
Van DT; d Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology , Hanoi , Vietnam.
Cuong NM; d Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology , Hanoi , Vietnam.
Kim YH; a College of Pharmacy, Chungnam National University , Daejeon , Republic of Korea .
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Źródło:
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Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2016 Aug; Vol. 31 (4), pp. 640-4. Date of Electronic Publication: 2015 Oct 07.
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Typ publikacji:
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Journal Article
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Język:
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English
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Imprint Name(s):
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Original Publication: Basingstoke, UK : Taylor & Francis, c2002-
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MeSH Terms:
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Enzyme Inhibitors/*pharmacology
Epoxide Hydrolases/*antagonists & inhibitors
Plant Components, Aerial/*chemistry
Rutaceae/*chemistry
Dose-Response Relationship, Drug ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/isolation & purification ; Epoxide Hydrolases/metabolism ; Humans ; Molecular Structure ; Solubility ; Structure-Activity Relationship
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Contributed Indexing:
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Keywords: Bisisomahanine mixed-type; Glycosmis stenocarpa; Rutaceae; soluble epoxide hydrolase
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Substance Nomenclature:
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0 (Enzyme Inhibitors)
EC 3.3.2.- (Epoxide Hydrolases)
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Entry Date(s):
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Date Created: 20151008 Date Completed: 20170222 Latest Revision: 20170222
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Update Code:
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20240104
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DOI:
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10.3109/14756366.2015.1057719
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PMID:
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26444316
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The aim of this study is to search for soluble epoxide hydrolase (sEH) inhibitors from natural plants, bioassay-guided fractionation of lipophilic n-hexane and chloroform layers of an extract of the aerial parts of Glycosmis stenocarpa led to the isolation of 12 compounds (1-12) including murrayafoline-A (1), isomahanine (2), bisisomahanine (3), saropeptate (4), (24 S)-ergost-4-en-3,6-dione (5), stigmasta-4-en-3,6-dion (6), stigmast-4-en-3-one (7), β-sitosterol (8), 24-methylpollinastanol (9), trans-phytol (10), neosarmentol III (11) and (+)-epiloliolide (12). Their structures were elucidated on the basis of spectroscopic data. Among them, neosarmentol III (11) was isolated from nature for the first time. All the isolated compounds were evaluated for their inhibitory activity against sEH. Among isolated carbazole-type compounds, isomahanine (2) and bisisomahanine (3) were identified as a potent inhibitor of sEH, with IC50 values of 22.5 ± 1.7 and 7.7 ± 1.2 µM, respectively. Moreover, the inhibitory action of 2 and 3 represented mixed-type enzyme inhibition.
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