Accelerated communication: Effects of flavonoids on Naja Naja and human recombinant synovial phospholipases A2 and inflammatory responses in mice
| Autor: | G. Bustos, María Luisa Ferrándiz, Maria-Jesus Sanz, R. Gunasegaran, M. J. Alcaraz, Miguel Payá, María Carmen Terencio, Blanca Gil |
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| Rok vydání: | 1994 |
| Předmět: |
chemistry.chemical_classification
biology Scutellarein Quercetagetin Biological activity General Medicine Phospholipase Pharmacology Group II Phospholipases A2 Flavones General Biochemistry Genetics and Molecular Biology chemistry.chemical_compound Phospholipase A2 chemistry Biochemistry biology.protein Hispidulin General Pharmacology Toxicology and Pharmaceutics |
| Zdroj: | Life Sciences. 54:PL333-PL338 |
| ISSN: | 0024-3205 |
| DOI: | 10.1016/0024-3205(94)90021-3 |
| Popis: | Six flavonoid derivatives were tested for their influence on Naja naja and human recombinant synovial phospholipase A2. They showed a selectivity for the last enzyme with IC50 = 14.3, 17.6, 12.2 and 28.2 microM for quercetagetin, kaempferol-3-O-galactoside, scutellarein and scutellarein-7-O-glucuronide, respectively, while reduced effects were observed for hispidulin and hibifolin. After topical application all the flavonoids inhibited 12-O-tetradecanoylphorbol-13-acetate-induced ear oedema in mice with a potency comparable to that of indomethacin and they were also able to inhibit carrageenan-induced mouse paw oedema at a dose of 150 mg/kg p.o. The blockade of the free hydroxyl at C-7 or C-6 reduced the anti-inflammatory activity and also the inhibitory effect on human recombinant synovial phospholipase A2. These results are in accordance with the notion that group II phospholipases A2 may play a role in experimental inflammation, although several mechanisms seems to be involved in the anti-inflammatory effect of this group of flavonoids. |
| Databáze: | OpenAIRE |
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