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Chemical Compound Review

AC1NWAPO     (10S,11S,13S,17R)-11,17- dihydroxy-17-(2...

Synonyms: CHEMBL416516, SureCN2737385, BSPBio_002500, KBioGR_001317, KBioGR_002263, ...
 
 
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Disease relevance of prednisolone

  • 2. Results of the 5-day rat croton oil ear edema bioassay indicated that, in contrast to the parent compound P, the novel steroidal antedrugs did not significantly alter body weight gain, thymus weights, or plasma corticosterone levels [1].
  • In a 5-day semi-chronic study at the equipotent doses, the novel steroidal antedrugs did not significantly alter body weight gain, thymus weights or plasma corticosterone levels unlike the parent compound Pred [2].
  • The binding affinities for cytosolic hepatoma tissue culture glucocorticoid receptors were 33, 201, 471, 5304, and 3765 nM for P, PClCM, FPClCM, methyl 21-desoxy-21-chloro-11beta-hydroxy-3,20-dioxo-1, 4-pregnadien-16alpha-carboxylate (DPClCM), and FDPClCM, respectively [3].
  • The 17 alpha-dehydroxy analogue of P16CM (DeoxyP16CM) retained one-half the local activity of P in the cotton pellet granuloma bioassay and topical activity equal to P in the croton oil induced ear edema bioassay [4].
  • The effectiveness of combined therapy with PE, PD and cyclophosphamide appeared to confirm a role of humoral factors in the pathogenesis of Graves' ophthalmopathy [5].
 

High impact information on prednisolone

  • Concomitant potencies for inhibition of NO generation by macrophages stimulated with lipopolysaccharide were Pred; 159, FP16CM-acetyl; 377, FP16CM-propionyl; 405, FP16CM-valeryl; 344, FP16CM-pivalyl; 311 nM, respectively [2].
  • Results of the 5-day rat croton oil ear edema bioassay indicated that, in contrast with the parent compound P, the novel steroidal antedrugs did not significantly alter body weight gain, thymus weights, or plasma corticosterone levels [3].
  • Carbenoxolone, 0.17 mmol/l, also increased mucin synthesis in the left colon by 242% [P < 0.05, n = 15 (three patients)] [6].
  • Results indicate that incorporation of a methoxycarbonyl group at the 16 position of prednisolone, as in P16CM, resulted in 5.5 times more local activity in the cotton pellet granuloma assay and 14 times more topical activity in the croton oil induced ear edema bioassay as compared with the parent compound prednisolone (P) [4].
 

Associations of prednisolone with other chemical compounds

  • Nicotine significantly increased mucin synthesis (180-220% of control values) between 62.5 nmol/l and 6.25 mumol/l (P < 0.05 at all concentrations) in both the right and left colon [6].
 

Analytical, diagnostic and therapeutic context of prednisolone

  • Thus an inhibitory effect of Aza was also observed in HCMV-infected cells treated with CsA and Pred at their concentrations used for immunosuppression [7].

References

  1. New steroidal anti-inflammatory antedrugs: methyl 3,20-dioxo-9 alpha-fluoro-11 beta,17 alpha,21-trihydroxy-1,4-pregnadiene-16 alpha-carboxylate and methyl 21-acetyloxy-3,20-dioxo-11 beta, 17 alpha-dihydroxy-9 alpha-fluoro-1,4-pregnadiene-16 alpha-carboxylate. Heiman, A.S., Ko, D.H., Chen, M., Lee, H.J. Steroids (1997) [Pubmed]
  2. New steroidal antiinflammatory antedrugs: Methyl 3,20-dioxo-9 alpha-fluoro-11 beta,17 alpha,21-trihydroxy-1,4-pregnadiene-16 alpha-carboxylate and its 21-O-acyl derivatives. Ko, D.H., Heiman, A.S., Hudson, C.E., Lee, H.J. Steroids (2002) [Pubmed]
  3. New steroidal anti-inflammatory antedrugs: methyl 21-desoxy-21-chloro-11beta,17alpha-dihydroxy-3,20-dioxo-1, 4-pregnadiene-16alpha-carboxylate, methyl 21-desoxy-21-chloro-11beta-hydroxy-3,20-dioxo-1, 4-pregnadiene-16alpha-carboxylate, and their 9alpha-fluoro derivatives*. Ko, D., Heiman, A.S., Chen, M., Lee, H.J. Steroids (2000) [Pubmed]
  4. A novel class of local antiinflammatory steroids. 2nd communication: pharmacological studies of methyl 11 beta,17 alpha,21- trihydroxy-3,20-dioxo-pregna-1,4-diene-16 alpha-carboxylate and methyl 11 beta,21-dihydroxy-3,20-dioxo-pregna-1,4-diene-16 alpha-carboxylate. Heiman, A.S., Kim, H.P., Taraporewala, I.B., Lee, H.J. Arzneimittel-Forschung. (1989) [Pubmed]
  5. Changes in thyrotropin binding inhibitor immunoglobulin (TBII) concentration before and after various treatments in a patient with infiltrative Graves' ophthalmopathy. Mori, T., Tanaka, K., Akamizu, T., Yokota, T., Ishii, H., Nakamura, H., Imura, H. Endocrinol. Jpn. (1985) [Pubmed]
  6. Stimulation of colonic mucin synthesis by corticosteroids and nicotine. Finnie, I.A., Campbell, B.J., Taylor, B.A., Milton, J.D., Sadek, S.K., Yu, L.G., Rhodes, J.M. Clin. Sci. (1996) [Pubmed]
  7. Immunosuppressive dose of azathioprine inhibits replication of human cytomegalovirus in vitro. Shiraki, K., Ishibashi, M., Okuno, T., Namazue, J., Yamanishi, K., Sonoda, T., Takahashi, M. Arch. Virol. (1991) [Pubmed]
 
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