Abstract：
:The anti-inflammatory activity of avarol and avarone, sesquiterpenoid derivatives from the Mediterranean sponge Dysidea avara, was investigated. Both compounds potently inhibited paw oedema induced by carrageenan (approximated ED50 = 9.2 and 4.6 mg/kg, p.o., respectively) as well as ear oedema induced by 12-O-tetradecanoylphorbol acetate (TPA; ED50 = 97 and 397 micrograms/ear, respectively) in mice, with effects comparable to those of indomethacin. In A23187-stimulated rat peritoneal leukocytes, avarol showed an IC50 = 0.6 and 1.4 microM for inhibition of leukotriene B4 and thromboxane B2 release, respectively, with avarone showing a slightly lower potency. Both marine metabolites failed to show xanthine oxidase inhibitory activity or superoxide scavenging effects but were potent inhibitors of superoxide generation in rat peritoneal leukocytes activated by different stimuli, with an IC50 below the microM range. Only avarol was able to inhibit human recombinant synovial phospholipase A2 activity with an IC50 = 158 microM, and thus this compound showed a potency higher than that of mepacrine. Avarol and avarone effectively control acute inflammation in experimental models after either oral or topical administration and their anti-inflammatory activity may result from inhibition of eicosanoid release and depression of superoxide generation in leukocytes.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Ferrándiz ML,Sanz MJ,Bustos G,Payá M,Alcaraz MJ,De Rosa Sdoi
10.1016/0014-2999(94)90759-5subject
Has Abstractpub_date
1994-02-21 00:00:00pages
75-82issue
1-2eissn
0014-2999issn
1879-0712pii
0014-2999(94)90759-5journal_volume
253pub_type
杂志文章abstract：:A previous report showed that transforming growth factor-beta1 (TGF-beta1) can induce heme oxygenase-1 (HO-1) expression, attenuate cellular injury, and maintain tissue homeostasis. In this study, we investigated the involvement of phosphoinositide-3-OH-kinase (PI3K)/Akt and the nuclear factor-kappaB (NF-kappaB) signa...
journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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doi：10.1016/0014-2999(82)90167-4
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abstract：:The biological activity of two galanin (GAL) fragments, GAL-(1-16) and GAL-(17-29), was tested in vivo by using a spinal nociceptive flexor reflex model in the rat. Intrathecal (i.t.) GAL-(1-16) had a similar biphasic effect on the flexor reflex, with facilitation at lower doses and facilitation followed by depression...
journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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