Johann Karl

Determination of platinum and biologically important trace elements in structure-activity relationship studies on platinum-containing anti-cancer drugs. Special procedures for removing32P as well as for the estimation of99 Mo and199Au

As part of an examination of the cytostatic effects of 1,2-diarylethylenediamine-platinum(II)-complexes the contents of platinum and biologically essential trace elements of tumour tissue and different organs were determined. The activation analysis procedure — separation of32P, isolation of199Au and99Mo — is described. In the course of a pharmakokinetical experiment with tumourbearing rats (DMBA induced hormone-dependent tumours) the desired enrichment of the administered drug in the tumour tissue was found. Changes of the trace element level of tumour tissue were found for hormone-dependent MXT-mammary tumours on mice.

Effect of estrophilic platinum complex on the mouse uterus

SummaryResistance of hormone-dependent mammary carcinoma to cisplatin as a potent antitumor agent led to the synthesis of other estrophilic platinum complexes. In this investigation, the effects of a newly synthesized estrogen-receptor affine platinum complex on the mouse uterus were studied using light and electron-microscopy. The results have been compared with Tamoxifen®, cisplatin and the estrophilic ligand. Both estrophilic ligand and estrophilic platinum complex produced strong estrogenic effects as well as features characteristic of the uterine epithelial cell in the luteal phase of the cycle, corresponding to a massive stimulation of the surface and glandular epithelial cells. The uteri showed large glandular lumina. An increase in the number of multivesicular and residual bodies, accompanied by a proliferation of eosinophilic granulocytes, was also seen. The appearance of inter- and intracellular lumina and the activation of smooth muscle cells represent further characteristic effects of the estrophilic ligand and estrophilic platinum complex. Anticipated increases in the incidence of cell death and/or deviant cyto-nuclear architecture in the uteri treated with cisplatin or platinum complex, were not observed.