Chemical and Biological Characterization of the Pineal Anti-Tumor Activity

01.01.2021 bis 31.12.2021

During the 1930s aqueous pineal extracts were used in Vienna for the treatment of cancer patients in conjunction with surgery and radiotherapy. After the discovery of melatonin in 1958 as the principal pineal hormone it was analysed in which way the tumor-inhibitory effect of raw pineal extracts could be attributed to melatonin. Over the years it became clear that melatonin primarily inhibits the growth of relatively highly differentiated and slow-growing tumors whereas pineal extracts are more potent. Since this effect could not be explained by other known pineal substances it became necessary to attempt a chemical isolation of the possible substances involved. For this purpose low-molecular weight pineal fractions purified via initial ultramembrane filtration and subsequent separatiuon on different types of HPLC-columns are tested in their cell-inhibitory effect on the erythroleukemic cell-line K-562 in a micro-bioassay in the current project. These effects are strictly blank controlled to avoid artefactual effects due to solvents and column material. Fractions with cell-inhibitory activity are analysed by common as well as HRMS-mass spectrometry. A central question will be whether the anti-tumor activity of aqueous pineal extracts can be attributed to a single substance or is rather due to the complex mixture of low-molecular weight substances present.