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Biomedical subjects

W Wohlrab

Publications and source records attributed to W Wohlrab.

At least 55 records · Page 3Linked to original sources

[Synthesis and melanoma inhibiting properties of 4-alkylpyrocatechol-2-O-beta-D-glucopyranosiduronic acids and their esters].

Using two sources of selection, the higher beta-glucuronidase and tyrosinase content of malignant melanomas, new transport forms are synthetized, which are toxified to quinoids, cytotoxic products by the above mentioned enzymes. These transport forms selectively inhibit the growth of melanomas. For instance, 4-methylcatechol-2-O-beta-D-glucopyranosiduronic acid (3) is synthetized by the reaction of 4-methylcatechol with tetra-O-acetyl-beta-D-glucopyranosiduronic acid methyl ester in the presence of p-toluenesulfonic acid following treatment with alkali. 3 inhibits the growth of B16 melanoma of the mouse significantly.

Animals↗

[Synthesis of 5-bromosalicyl-4'-chloroanilide-O-beta-D-xylopyranoside and other transport forms enzymatically activated by microbes].

The synthesis of 5-bromosalicyl-4'-chloroanilide-O-beta-D-xylopyranoside and other glycosides of 5-bromosalicyl-4'-chloroanilide, salicylanilide, 3,5-dichlorophenol and tetrachlorohydrochinone is described. Glycosidations follow the procedures described by Latham et al. Sabalitschka and Helferich et al. These glycosides represent relatively untoxic transport-forms of drugs, which are activated to the free drug by specific enzymes of the organisms to be destroyed. This new mechanisms can help to destroy fungi and parasites in dermatology, agriculture, horticulture and cultivation of decorative plants without side effects on the host.

Anti-Infective Agents↗

Penetration kinetics of liposomal hydrocortisone in human skin.

The applicability of liposomal hydrocortisone (HC) as a selective drug delivery system for cutaneous administration of glucocorticoids has been studied. With the liposomal form, a considerably better concentration-time profile was obtained in the individual layers of human skin than with the corresponding HC ointment. The pronounced carrier ability of liposomes for HC holds promise for an increase in its therapeutic efficacy, thus reducing unwanted side effects of the topical glucocorticoid therapy.

Administration, Topical↗

[Effect of a new benzodiazepine derivative on experimental malignant melanomas].

It was found, that (+)cis-3,4-dimethoxy-10,11-dimethyl-6,6aR,7,8,13, 13aS-hexahydro-[I]-benzopyrano-[4,3-b]-1,5-benzodiazepine (ZIMET 54/79) increased the life span (ILS) of C57BL/6/Jena mice suffering from transplanted B16 melanoma (ip.) by 57% (9 times ip. 250 mg/kg) and 90% (9 times ip. 500 mg/kg) respectively. In B6D2F1/Bln mice with transplanted B16 melanoma there was no ILS registered when a dose of 100-500 mg/kg was applied (ip. and p.o.). Using the Harding Passey melanoma (B6D2F1/Bln mice) only 59% tumour volume inhibition (500 mg/kg) without ILS was obtained. Finally ZIMET 54/79 tested on AMel 3 hamster melanoma (strain Z3) decreased the mean tumour volume by 72% (125 mg/kg).

Animals↗

[Experimental results of the optimization of external prednisolone therapy].

The initial steps of any topical therapy are characterized by the degree of liberation of the agent from the ointment base and their penetration into different skin layers. A high percentage of the topically applied prednisolone does not penetrate into the skin and may be removed from the skin surface even after some time. By altering the functional structure of the horny layer and considerably increase of prednisolone liberation from ointment bases urea is a effective penetration promotor also for prednisolone. The increased prednisolone penetration into human skin from urea containing ointment correspond with the degree of blanching results by vasoconstriction test under in vivo conditions. The resulting penetration optimation of prednisolone has two possible applications in topical therapy: an increased therapeutic effect for a given prednisolone concentration and a given therapeutic effect could be obtained with a reduced prednisolone concentration.

Administration, Topical↗

[Urea and the skin].

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Administration, Topical↗