| Description | Rutaecarpine (Rhetine) is an inhibitor of COX-2 with IC50 of 0.28 μM. |
| In vitro | Rutaecarpine is an indolopyridoquinazolinone alkaloid isolated from Evodia rutaecarpa and related herbs, which has shown a variety of intriguing biological properties such as anti-thrombotic, anticancer, anti-inflammatory and analgesic, anti-obesity and thermoregulatory, vasorelaxing activity, as well as effects on the cardiovascular and endocrine systems. [1] |
| Cell experiments | Rutaecarpine is dissolved in DMSO and diluted with appropriate medium before use. COX-1 and COX-2 cDNA-transfected HEK293 cells are prepared. For measuring inhibitory activity on COX-1 and COX-2 by rutaecarpine, cells in 1 mL of culture medium are seeded into each well of 24-well. After culture for 4 days, the supernatants are removed and 250 mL of fresh medium is added to the cells with or without rutaecarpine. After preincubation for 5 h at 37°C, the cells are further incubated at 37°C for 30 min with 50 mM arachidonic acid. All reactions are stopped by centrifugation at 120 g at 4°C for 5 min. Concentrations of PGE2 in the supernatant are measured[1]. |
| Target activity | COX-2:0.28 μM. |
| Synonyms | Rutacarpine, 吴茱萸次碱, Rhetine, Rutecarpine |
| molecular weight | 287.32 |
| Molecular formula | C18H13N3O |
| CAS | 84-26-4 |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 18.33 mg/mL (63.81 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Lee SH, et al. Molecules, 2008, 13(2), 272-300. 2. Yang XW, et al. J Asian Nat Prod Res, 2006, 8(8), 697-703. 3. Moon TC, et al. Inflamm Res. 1999, 48(12):621-5. |