Anti-inflammation activity

Whatever the mechanism of action for the inhibition of 5-lipoxygenase by flavonoids, it appears to be distinct from the antioxidant properties of these compounds. The results comparing antioxidant activity with leukotriene inhibitory activity clearly demonstrate this distinction. The profound effects of metabolic transformation on the anti-inflammation activity of dietary flavonoids such as quercetin must also be considered in relation to in vitro studies, and further highlights the need to use actual metabolic forms of flavonoids rather than the free aglycone or glycosides occurring in the diet. 

According to Ramadan and cowoikers (36), aqueous extract of the baobab fruit pulp produces a marked anti-inflammation activity. The effect was comparable to that induced by standard phenylbutazone (15 mg/kg). This antiinflammatory effect may be due to the presence of sterols, saponins and triterpenes in the aqueous extract. The extract also shows a marked antipyretic activity (36). The antipyretic activity of the extract resembles that normally induced by standard dose of administered acetylsalicyhc acid (ASA) in hyperthermic rats. Leaves are applied locally for a variety of inflammatoiy conditions, insect bites and guinea worm sores (8). Anti-pyretic activity has been reported (36). 

The ghicocorticoids are used as replacement therapy for adrenocortical insufficiency, to treat allergic reactions, collagen diseases (eg, systemic lupus erythematosus), dermatologic conditions, rheumatic disorders, shock, and other conditions (see Display 50-1). The anti-inflammatory activity of these hormones make them valuable as anti-inflammatories and as immunosuppressants to suppress inflammation and modify the immune response... 

These drugp possess anti-inflammatory activity and are used for inflammatory conditions, such as allergic conjunctivitis, keratitis, herpes zoster keratitis, and inflammation of the iris. Corticosteroids also may be used after injury to the cornea or after corneal transplants to prevent rejection. 

Index for anti-inflammatory activity. Model acute inflammation, method Carragennan induced edema, test animal albino rats, number of animals per group 6, route of administration oral, standard phenylbutazone (100 mgkg ), test compounds lOOmgkg ... 

Huang S-T, Liao J-S, Fang H-W, Lin C-M (2008) Synthesis and anti-inflammation evaluation of new C60 fulleropyrrolidines bearing biologically active xanthine. Bioorg. Med. Chem. Lett. 

Go 6850 (GF-109203X) (485), a dimethylaminoethyl analog of 2,3-bis(indol-3-yl) maleimide was shown to be a selective inhibitor of PKC with anti-inflammatory activity in several in vivo and in vitro murine models of acute inflammation (432) (Scheme 4.7). 

Adenosine 2a receptor ADORA2A Agonism Inhibition of platelet aggregation, anti-inflammation and neuroprotective effects, coronary vasodilation, decreased blood pressure, increased plasma renin activity and sleep induction. Antagonism Increased platelet aggregation, hypertension, nervousness (tremor, agitation), arousal, insomnia, cerebral and coronary vasodilation (in microvessels only). 

Murphey, D. K., and Buescher, E. S. (1993). Human colostrum has anti-inflammatory activity in a rat subcutaneous air pouch model of inflammation. Pediatr. Res. 34, 208-212. 

Apart from their anti-inflammatory activity the NSAIDs also show, dependent on the condition and the type of pain, considerable analgesic efficacy. In some forms of postoperative pain the NSAID s can be as efficacious as opioids, especially when prostaglandins, bradykinin and histamine, which are released by inflammation, have caused sensitization of pain receptors to normally painless stimuli. In Table 4 some advantages and disadvantages of NSAID s and opioids are compared. Although analgesic effects at peripheral or central neurons cannot be excluded completely, most studies indicate that... 

Anti-inflammatory activity. Extract of the green seed, administered externally to adult with skin inflammations by free radical inhibition at a concentration of 1%, was active . 

Anti-edema activity. Methanol extract of the rhizome, applied topically to mice at a dose of 2 mg/ear, was active vs 12-0-tetradecanoyl-13-acetate-induced ear inflammation. The inhibition ratio was nine " . 

The most important clinical application of glucocorticoids and their semisynthetic analogs is their anti-inflammatory activity, discovered in 1949 by Hench and co-workers. The profound anti-inflammatory effects of glucocorticoids arise from the combined effects of these steroids on both the cellular and molecular mediators of inflammation these effects are separate from the metabolic effects described above and further indication of the widespread diversity of macromolecules to which steroids can bind. Glucocorticoids suppress inflammation at the cellular level by downregulating the concentration, distribution, and function of leukocytes (white blood cells) that profoundly influence inflammation and response to infection within the body (In this way, steroids help to mediate the overlap between the endocrine systems [chapter 5] and the immune systems [chapter 6]). Glucocorticoids also suppress inflammation at the molecule level by suppressing inflammatory cytokines, chemokines, and other molecular mediators of inflammation. 

Drug interactions Vitravene is not recommended for use in patients who have recently (2-4 weeks) been treated with either intravenous or intravitreal cidofovir because of the risk of exaggerated ocular inflammation. Results from in vitro tests demonstrated no inhibition of anti-CMV activity of fomivirsen by zidovudine or zalcitabine. 

Classically, inflammation is a protective reaction of the body in response to some physical, chemical, or microbial injury and insult of the cells. Acute inflammation, rapid onset and shorter duration, is considered as a healthy response. However, when inflammation continues for prolonged period of time, it becomes detrimental and may raise the first step of a chronic disease (Medzhitov, 2008). Arachidonic acid/COX and nuclear factor- (NF- ) are well known inflammatory pathways which induce production of inflammatory mediators such as prostaglandins, thromboxanes, leukotrienes, and cytokines. Most commonly accepted mechanism of anti-inflammation is inhibition of cyclooxygenase (COX) activity. There are two kinds of cyclooxygenases COX-1 is natural protective enzyme of intestinal mucosa while COX-2 is induced by tissue damage as an inflammatory mediator (Maroon et al., 2006). NF- is a recently identified... 

The concept that inflammation and carcinogenesis are related phenomena has been the subject of many studies that have attempted to link these two processes in a mechanistic fashion [94-99]. In connection with this, as is evident in some triterpenoids such as oleanolic acid (142), glycyrrhetic acid (147), and ursolic acid (210) in Table 2, those possessing anti-inflammatory activity in various experimental models exhibited antitumor-promoting activity as well. This suggests that most of the other anti-inflammatory triterpenoids and sterols listed in Table 2 might have antitumor-promoting properties which have not been evaluated, yet. 

Both avarol and avarone inhibit replication of the ethiological agent of acquired immuno-deficiency syndrome (AIDS) [77], Additionally, avarol and avarone effectively control acute inflammation in experimental models after either oral or topical administration. Their anti-inflammatory activity may result from inhibition of eicosanoid release and depression of superoxide generation in leukocytes [78], Several studies reviewed the structures and bioactivity of compounds related to avarone as an antihuman immuno-deficiency virus (HIV), antitopoisomerase II activity and as proteinkinase C (PKC) inhibitors [3, 79],... 

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