Catecholic Isoquinolines from Portulaca oleracea and Their Anti-inflammatory and ß2-Adrenergic Receptor Agonist Activity.
J Nat Prod
; 81(4): 768-777, 2018 04 27.
Article
en En
| MEDLINE
| ID: mdl-29517238
ABSTRACT
Isoquinoline alkaloids possess a wide range of structural features and pharmaceutical activities and are promising drug candidates. Ten water-soluble catecholic isoquinolines were isolated from the medicinal plant Portulaca oleracea, including three new (1-3) and seven known compounds (4-10), along with the known catecholamines 11 and 12 and four other known compounds (13-16). A method of polyamide column chromatography using EtOAc-MeOH as the mobile phase was developed for the isolation of catecholic isoquinolines. Alkaloids 1-12 exhibited anti-inflammatory activities (EC50 = 18.0-497.7 µM) through inhibition of NO production in lipopolysaccharide-induced murine macrophage RAW 264.7 cells. Among these compounds, 11, 2, 5, 4, and 8 were more potent than was the positive control, 3,4-dihydroxybenzohydroxamic acid (EC50 = 82.4 µM), with EC50 values of 18.0, 18.1, 35.4, 36.3, and 58.7 µM, respectively. Additionally, at 100 µM, compounds 1-12 showed different degrees of ß2-adrenergic receptor (ß2-AR) agonist activity in the CHO-K1/GA15 cell line which stably expressed ß2-AR as detected by a calcium assay. The EC50 values of 2 and 10 were 5.1 µM and 87.9 nM, respectively.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Agonistas Adrenérgicos
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Portulaca
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Agonistas de Receptores Adrenérgicos beta 2
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Isoquinolinas
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Antiinflamatorios
Límite:
Animals
Idioma:
En
Año:
2018
Tipo del documento:
Article