Anti-inflammatory and anti-osteoporotic activities of base-boronated nucleosides and phosphate-boronated nucleotides in rodents

✍ Scribed by K. G. Rajendran; Bruce S. Burnham; S. Y. Chen; A. Sood; B. F. Spielvogel; Barbara R. Shaw; Iris H. Hall

• Publisher: John Wiley and Sons
• Year: 1994
• Tongue: English
• Weight: 563 KB
• Volume: 83
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600831005

✦ Synopsis

The 2'-deoxynbonucleoside cyanoboranes were effective antiinflammatory agents in rodents at 2-8 mglkg; they blocked induced edema, septic shock, and pleurisy. Overall compounds 3',5'-0(bis-(triisopropylsilyl)-2'-deoxyinosine (l), 3',5'-Obis(triisopropylsilyl)-2'-deoxy-

were the most active when all of the antiinflammatory screens are considered. The agents also blocked both local and central pain caused by inflammation. These nucleosides blocked calcium resorption but were less effective compared to other amine carboxyboranes. The inflammation process appeared blocked by these compounds because of their effectiveness in reducing both hydrolytic lysosomal enzyme and proteolytic enzyme activities. The agents were also dual inhibitors of prostaglandin cyclooxygenase and 5'-lipoxygenase activities in leukocytes and macrophages. These agents at M demonstrated no specific organ toxicity to ileum mucosa cells grown in tissue culture.