RESUMEN
Sixteen compounds were isolated from the ethanol extract of Illigera rhodantha by silica gel, ODS, and Sephadex LH-20 column chromatographies. These compounds were identified as (2R,3R)-2,3-dihydroxy-2-methylbutane-1,4-diyldibenzoate (1), p-hydroxyphenethyl trans-ferulate (2), 4-O-benzoyl-2-C-methyl-D-erythritol (3), N-trans feruloyl-3-methyldopamine (4), tribulusamide A (5), cryptomeridiol (6), teuclatriol (7), oleanolic acid (8), icario A2 (9), vanillic acid (10), p-hydroxybenzoic acid (11), gallic acid (12), ethyl gallate (13), chrysophanol (14), D-1-O-methyl-inositol (15), and hexadecanoic acid (16) based on their spectral data and physico-chemical properties. Compound 1 is an undescribed compound, of which its absolute configurations were determined by Mosher and ROESY methods; all the compounds except 10, 11 and 14 were isolated from Illigera genus for the first time. Compared with the positive control indomethacin, compounds 4-6, 8 and 9 inhibited significantly against the NO production in LPS-induced RAW 264.7 cells.
RESUMEN
Seven terpenoids and three sterols were isolated from the methanol extracts of the aerial parts of Ricinus communis by chromatography methods and their structures were identified by spectra analysis as ficusic acid( 1), phytol(2), callyspinol(3) , lupeol(4), 30-norlupan-3beta-ol-20-one(5) , lup-20(29)-en-3beta,15alpha-diol(6) , acetylaleuritolic acid( 7), stigmast4-en-3-one(8) , stig-mast-4-en-6beta-ol-3-one(9) , and stigmast4-en-3,6-dione(10). Compounds 1-3 and 5-10 were obtained from this species for the first time and 5 and 6 showed significant inhibitive activity and good selectivity against 11beta-HSD of mouse and human in vitro. [Key words] Ricinus communis; terpenoids; sterols; 11beta-HSD
Asunto(s)
Animales , Humanos , Ratones , 11-beta-Hidroxiesteroide Deshidrogenasa de Tipo 1 , 11-beta-Hidroxiesteroide Deshidrogenasa de Tipo 2 , Diabetes Mellitus , Quimioterapia , Hipoglucemiantes , Farmacología , Usos Terapéuticos , Concentración 50 Inhibidora , Ricinus , Química , Esteroles , Farmacología , Usos Terapéuticos , Terpenos , Farmacología , Usos TerapéuticosRESUMEN
Objective: To investigate the chemical constituents from the barks of Melia azedarach and their antidiabetes activities. Methods: The constituents were isolated and purified by silica gel, reverse phase silica gel, and Sephadex LH-20 column chromatography, and their structures were identified by spectra and physiochemical characteristic analysis. The agonist activities of the isolated triterpenoids against glucokinase (GK) and SIRT1, and the inhibitory activity against dipeptidyl peptidasesIV (DPPIV), and 11β-hydroxysteroid dehydrogenase (11β-HSD) were tested in vitro. Results: Six triterpenoids and three sterols were obtained from MeOH extract in the barks of M. azedarach and were elucidated as meliastatin 3 (1), kulonic acid (2), kulactone (3), sendanolactone (4), dubione B (5), 20, 24-cyclotirucalla-7(8)-en-16β, 21α, 25-trihydroxy-3-one (6), 3β-hydroxy-5, 8-epidioxy-ergosta-6, 22-diene (7), 2β, 3β, 4β-trihydroxy-pregn-16-one (8), and 3β-hydroxy-pregn-5, 17 (20)-dien-16-one (9). Compound 2 showed the inhibitory activity against 11β-HSD1 with the IC50 value of 54.15 nmol/L. Conclusion: Compounds 6-9 are obtained from this species for the first time. The tested compounds 1-4 are inactive against GK, SIRT1, and DPPIV, but compound 2 shows high selectivity against human 11β-HSD.