Synalar
Effects of 12-O-tetradecanoylphorbol-13-acetate and retinoids on intercellular junctional communication measured with a citrulline incorporation assay.

Davidson JS, Baumgarten IM, Harley EH.

Inhibition of intercellular junctional communication by 12-O-tetradecanoylphorbol-13-acetate (TPA) and retinoids was investigated using a citrulline incorporation assay. This new assay uses metabolic co-operation between argininosuccinate lyase-deficient human fibroblasts and arginosuccinate synthetase-deficient cells as a measure of junctional communication. Short-term exposure to TPA resulted in virtually complete inhibition of metabolic co-operation when V79 cells were used as the synthetase-deficient type. When synthetase-deficient human fibroblasts were used, inhibition by TPA was only partial. Exposure to high concentrations of TPA for prolonged periods resulted in partial reversal of communication inhibition and a refractory state in which cells were unresponsive to TPA. Retinoic acid and other retinoids also inhibited metabolic co-operation, but did not cause desensitisation of the type seen with TPA after prolonged exposure. Cultures which had been made refractory to TPA remained sensitive to inhibition by retinoic acid and 1,1,1-trichloro-2,2-bis(p-chlorophenyl)ethane, indicating that these latter compounds inhibit junctional communication by a mechanism different from TPA. Simultaneous exposure of cultures to TPA and retinoic acid showed that the inhibitory effects on metabolic co-operation of these compounds were additive. Fluocinolone acetonide did not antagonise the effect of TPA. These results suggest that retinoic acid and fluocinolone acetonide exert their anti-tumor-promoting action by mechanisms which are not mediated by intercellular junctional communication.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3986968&dopt=Abstract fluocinolone Synalar



Synalar
Synthesis and anti-inflammatory properties of budesonide, a new non-halogenated glucocorticoid with high local activity.

Thalen A, Brattsand R.

As part of a study of the local anti-inflammatory activity of corticosteroid 16 alpha, 17 alpha-acetals it was found that on acetalization of 16 alpha-hydroxyprednisolone with n-butyraldehyde the two possible epimers were formed in the ratio of 1: 1. The reaction product was resolved by column chromatography on Sephadex LH-20. The isolated epimers were studied by NMR and mass spectrometry. The epimeric mixture of this new non-halogenated corticoid, 16 alpha, 17 alpha-(22R,S)-propylmethylenedioxypregna-1,4-diene-11 beta,21-diol-3,20-dione (budesonide), was shown to have a local antiinflammatory potency comparable to that of fluocinolone acetonide in cotton pellet tests in rats. In contrast, its systemic glucocorticoid activity was found to be 4--7 times lower than that of fluocinolone acetonide, however.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=543875&dopt=Abstract fluocinolone Synalar



Synalar
The effect of topical drugs on mouse ear epidermal transglutaminase activity.

De Young L, Ballaron S.

The response of mouse ear epidermal transglutaminase to single applications of anthralin, retinoic acid (both 59 micrograms/ear) or fluocinolone acetonide (2 micrograms/ear) was determined. Anthralin and retinoic acid caused inflammation and accumulation of epidermal protein and DNA, whereas fluocinolone acetonide resulted in ear thinning and decreased epidermal protein and DNA. Treatment with either anthralin or retinoic acid caused increases in absolute amounts of epidermal transglutaminase activity/ear. Anthralin increased this parameter 70-100% above acetone-treated controls from 48 hr through 7 days. Retinoic acid-treated ears showed a slower initial increase but peaked at 4 times control level by 96 hr before returning to normal at 7 days. Fluocinolone acetonide treatment had no effect on this parameter. The specific activity of epidermal transglutaminase (total epidermal transglutaminase/total soluble epidermal protein) was decreased by retinoic acid treatment; was maintained at normal levels by anthralin (except for the 7-day point where it decreased 50%); and was dramatically stimulated by fluocinolone acetonide. In the latter case, specific activity was more than 5 x control by 96 hr and still near this level at 7 days. Epidermal transglutaminase activity is a marker of differentiation, and protein and DNA accumulation an indication of growth. Thus, at the doses studied, retinoic acid favors growth over differentiation, anthralin maintains a normal to near normal ratio of growth to differentiation, and fluocinolone acetonide strongly favors differentiation over growth.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6125546&dopt=Abstract fluocinolone Synalar



Synalar
Preservative activity in diluted corticosteroid creams.

Hugo WB, Denyer SP, York HL, Tucker JD.

The preservative efficacy of both 'Betnovate' and 'Synalar' creams diluted 1:1 with 'Unguentum Merck' was investigated. Each formulation was challenged with Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa at an initial inoculum level of approximately 1 X 10(6) viable organisms per gram of cream. All formulations tested were found to be effectively preserved against the organisms used and no viable bacteria were detected 7 days after inoculation.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6208253&dopt=Abstract fluocinolone Synalar



Synalar
[Fluocinolone Acetonide Reference Standard (Control 981) of National Institute of Health Sciences]

[Article in Japanese]

Iwata M, Maekawa K, Saito H, Tanimoto T, Okada S.

The raw material of fluocinolone acetonide was examined for preparation of the "Fluocinolone Acetonide Reference Standard (Control 981)". The analytical data obtained were: melting point, 271.5 degree C; UV spectrum, Lambda max of 237.0 nm and specific absorbance in ethanol at 237 nm of 359.3; IR spectrum, same as that of the Fluocinolone Acetonide Reference Standard (Control 904); optical rotation, [alpha]20(D) = + 102.8; thin-layer chromatography, no impurities detected; high-performance liquid chromatography, one impurity detected and total amount estimated to be about 0.17%; loss on drying, 0.29%; assay by HPLC, 100.9%. Based on the above results, the raw material was authorized as the Fluocinolone Acetonide Reference Standard (Control 981) of the National Institute of Health Sciences.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10939860&dopt=Abstract fluocinolone Synalar