INFLUENCE OF STEROIDS ON FIBROBLASTS .2. FIBROBLAST AS AN ASSAY SYSTEM FOR TOPICAL ANTI-INFLAMMATORY POTENCY OF CORTICOSTEROIDS

[摘要] A number of naturally occurring and synthetic steroids were tested for fibroblast inhibiting potency in a tissue culture system. The [DELTA]4, 3-ketone, 21-hydroxyl, and 11 [beta]-hydroxyl groups are necessary to the steroid nucleus for insuring fibroblast inhibition. The 17[alpha]-OH group is also important in this regard. Increasing steroidal fibroblast depression is attained by addition of complex substituents such as 6 [alpha]- and 9 [alpha]-fluorines, and presence of a 16, 17-acetonide structure on the steroid molecule. Fibroblast inhibiting potency and toplcal anti-inflammatory activity are possessed by 9[alpha], 11[beta]-dichloro compounds, desplte their lack of potency in anti-granuloma and thymus involution tests. Comparison of steroid potency measured by this test and by other laboratory procedures to toplcal anti-inflammatory activity manifest by clinical trial, indicated that the tissue culture assay is an excellent addition to the bioassay systems available.