Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: CAS:50-03-3 (Hydrocortisone acetate)
 99 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Affinity for the dexamethasone binding sites of tixocortol pivalate, (the ester of the 21 thiol derivatives of cortisol), a steroid with local anti-inflammatory activity similar to cortisol acetate and with no systemic activity, was investigated in comparison with other steroids: tixocortol (the thiol derivative yielded by esterase hydrolysis), cortisol acetate and cortisol. The rank order of relative affinity for dexamethasone receptor of mouse thymocytes (37 degrees C) was: dexamethasone (1), cortisol (0.20), tixocortol pivalate (0.16), tixocortol (0.065), cortisol acetate (0.05). The corresponding 21 oxygenated ester (cortisol pivalate) was found less potent (0.080). Using rat renomedullary interstitial cells in culture, tixocortol pivalate showed also a higher receptor affinity than tixocortol. Cortisol acetate was as potent as tixocortol pivalate. The biological activity of tixocortol pivalate measured by the inhibition of PGE2 secretion on the same model, was similar to cortisol acetate and cortisol (10(-6) M, 24 h incubation, 38-55% inhibition). Tixocortol was less active (26%). These results with tixocortol pivalate are in good agreement with previously reported in vivo studies and show a good correlation between its binding ability and biological effect.
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PMID:Affinity of tixocortol pivalate (JO 1016), tixocortol, cortisol acetate and cortisol for dexamethasone receptors of mouse thymus cells and rat renomedullary interstitial cells in culture. Correlation with their biological activities. 658 91

Organotypic cornea equivalents are used as in vitro models for permeation studies. Many ophthalmic drugs are applied as ester prodrugs to achieve a higher bioavailability. The esterase activity of three corneal human cell lines (epithelial, stromal, endothelial cells) as well as of excised porcine cornea, human donor cornea and human cornea construct (HCC) was investigated and compared. Esterase activity was determined using p-nitrophenyl acetate and hydrocortisone acetate (HCA) as esterase substrates. Hydrocortisone acetate permeation across porcine cornea, human donor cornea and HCC was studied in vitro using Franz-diffusion cells. Corneal epithelial cells showed the highest esterase activity and only small differences to keratocytes and endothelial cells were detectable. The permeation barrier properties of the different corneal tissues were very similar in the case of HCA permeation whereas HCA metabolism rates were in the ranking order of porcine cornea > HCC > human donor cornea. Permeation and metabolism studies indicate that the in vitro permeation model HCC is able to adequately convert hydrocortisone acetate to hydrocortisone.
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PMID:[Esterase activity of human organotypic cornea construct (HCC) as in vitro model for permeation studies]. 1578 10