Anti-inflammatory actions biological activity

As an example, suppose that it is known to experts in the field that an extract from the plant Clusia criuva has anti-inflammatory activity. Therefore, a specialist in the subject would be led to test other species of the genus Clusia for the same biological activity (anti-inflammatory). Nevertheless, a way to prove inventive step would be to demonstrate that the species of interest, for example Clusia rosea, presents an unexpected technical effect. In other words, while the species Clusia criuva has an undesirable side effect associated with its anti-inflammatory action, such... 

Despite its widespread and long history of use its specific mechanism of action is not established. It elicits several biological and immunological responses including anti-infective, anti-inflammatory and immunomodulatory activities. The present evidence seems to be that the multiple effects work in concert with each other. Each mechanism contributes differently depending on the disease (Ballow, 2005 Shah, 2005). 

A possible explanation for the anti-inflammatory action of cortisol based on the prevention of release of plasma kinins has been published. A number of 8-dehydro analogs of corticosteroids have been synthesized and their thymolytic and salt retaining properties measured. The compound found to have the highest thymolytic activity was 1 (11.4 x hydrocortisone). Again the fallacy of projecting biological activity from one series of steroids to another was demonstrated by the large decrease in activity exhibited by the 8-dehydro steroid 2 as compared with 16a-methylprednisolone (3). 

The urea (289) was dehydrated in the presence of triphenylphosphine, carbon tetrachloride and triethylamine to give the carbodi-imide (290) and addition of 2-aminothiazole precipitated timegadine (291). This has a powerful anti-inflammatory action, but no hypotension or other biological activity could be detected Scheme 5.66.) [358]. 

The ionization as anions of many commonly used anti-inflammatory agents is positively correlated with their biological action provided that ionization is not complete and that they are sufficiently lipophilic to reach their prostaglandin-inhibiting site of action. Examples include indomethacin 4.5) and the salicylates (Whitehouse and Dean, 1965). In the phenylindanedione 9.39) series, observation of the effect of varying the (on the anti-inflammatory action) pointed to a need for more accurate determinations of in the or Ao-substituted aryl derivatives, which are by far the most biologically active (van der B vgetaL, 1975). 

Owing to the presence of high concentrations of A -THC, biomedical attention on C. sativa has so far mainly focused on the psychotropic varieties of this plant, while the pharmacological potential of fiber hemp has been largely overlooked. However, certain biological properties of THC are shared also by non-psychotropic cannabinoids, and thus, some pharmacologically useful activities of C. sativa, such as antibacterial and anti-inflammatory actions, could be dissected from its psychotropic potential and an easier therapeutic application found [58]. 

Miscellaneous - Specific amino acids have been studied for anti-inflammatory activity. Thus, the combination of calcium D,L-aspartate/indometha-cin has been repor gd to be effective in primary chronic polyarthritis Dilauroyl-L-lyslne and trans U-aminomethyl-cyclohexane-l-carboxylic acid (tranexamic acid) have anti-inflammatory properties. The activity of tranexamic acid was not attributed to anti-plasmin action. Detailed pharmacology on SKF 17,910-A (X) has been published. This anti-inflammatory and diuretic agent shares some biological properties with glucocorticoids. 

But now, a strategy, used for the synthesis of derivative (622) (lit. synthesis (622) see in Ref. 555), which is the most efficient analog of the commercial drug rolipram with a broad spectrum of action (in particular, anti-inflammatory, antidepressant, neuroprotective, and immunodepressing effects), is presented in Scheme 3.286. (The principle action of rolipram is based on selective inhibition of adenosine monophosphate (AMP)-specific phosphodiesterase.) Derivative (622) is almost 10 times more efficient than rolipram, but the biological activity of (622) was determined only for the racemate (555). 

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