Inhibitory activity of isolated compounds from Crepis sancta on A23187- and antigen-induced degranulation.
| Compound | % Viability, RBL-2H3a | % Inhibition of A23187-induced degranulationb | % Inhibition of antigen-induced degranulationc | ||||||
|---|---|---|---|---|---|---|---|---|---|
| 100 μM | 1 μM | 10 μM | 100 μM | IC50d (μM) | 1 μM | 10 μM | 100 μM | IC50d (μM) | |
| (6S,7S,10R)-3-Oxo-di-nor-eudesm-4-en-6α-hydroxy-11-oic acid (1) | >90% | 2.1 ± 1.8 | 7.6 ± 6.6 | 7.7 ± 3.8 | 11.3 ± 3.6 | ||||
| (6S,7S,10R)-3-Oxo-6α-hydroxy-γ-costic acid (2) | >90% | 0.2 ± 0.2 | 0.3 ± 0.3 | 11.7 ± 4.2 | 19.8 ± 2.5 | ||||
| 3-Oxo-γ-costic acid (3) | >90% | 2.7 ± 2.3 | 1.8 ± 1.6 | 2.8 ± 1.0 | 0.3 ± 0.2 | ||||
| 3-Oxo-γ-costic acid methyl ester (4) | >90% | 7.2 ± 5.9 | 61.8 ± 7.4*** | 80.6 | 18.2 ± 4.4 | 36.2 ± 6.5*** | |||
| (6S,9R)-Roseoside (5) | >90% | 5.3 ± 4.3 | 16.8 ± 7.9 | 19.9 ± 4.3 | 21.6 ± 1.8 | ||||
| Jaceidin (6) | >90% | 5.3 ± 4.3 | 25.5 ± 5.0* | 3.9 ± 2.9 | 46.5 ± 10.2*** | ||||
| Kumatakenin (7) | >90% | 12.6 ± 9.1 | 36.8 ± 5.4 | 11.1 ± 7.6 | 60.9 ± 8.8*** | 80.4 | |||
| Penduletin (8) | >90% | 4.8 ± 3.9 | 25.1 ± 7.3 | e | 33.9 ± 8.6** | 85.8 ± 5.1*** | e | 3.8 | |
| Pachypodol (9) | >90% | 3.4 ± 2.8 | 22.6 ± 3.4 | e | 12.9 ± 6.5 | 47.2 ± 5.0*** | e | ||
| Chrysosplenetin (10) | >90% | 7.3 ± 5.9 | 41.6 ± 9.5*** | e | 12.4 ± 5.1 | 83.3 ± 7.5*** | e | 5.8 | |
| Azelastineb,c | >90% (20 μM) | 10.9 | 15.4 | ||||||
The cytotoxicity of samples to RBL-2H3 was evaluated using MTT viability assay. Results are presented as mean (n = 3) compared to untreated control (DMSO). All samples were nontoxic towards RBL-2H3 cells.
Azelastine (20 μM) was used as a positive control and inhibited 78.4 ± 1.4% *** of A23187-induced degranulation. The inhibition of degranulation was assessed by A23187-induced β-hexosaminidase release in RBL-2H3 cells. Results are presented as mean ± S.E.M. (n = 3); *P < 0.05, **P < 0.01, ***P < 0.001 (Prism, ANOVA, Dunnet's test) compared with the control value (A23187 only).
Azelastine (20 μM) was used as a positive control and inhibited 66.8 ± 9.8% *** of antigen-induced degranulation. The inhibition of degranulation was assessed by antigen-induced β-hexosaminidase release in RBL-2H3 cells. Results are presented as mean ± SEM (n = 3); *P < 0.05, **P < 0.01, ***P < 0.001 (Prism, ANOVA, Dunnet's test) compared with the control value (antigen only).
Concentration necessary for 50% inhibition (IC50).
Compounds 8, 9 and 10 at concentration of 100 μM formed crystal-like precipitates upon the addition into medium, thus the effects could not be justified.