Cytostatic activity of synthetic O-alkylglycerolipids.
A series of halogen-containing alkylglycerolipid analogs has been checked for their cytostatic activity both in vitro and in vivo. The compounds included alkyldeoxyhaloglycerols (I), alkyldeoxyhaloglycerophosphocholines (II), and alkyldeoxyhaloglycerophosphoric acids and alkyl esters (III). While compounds I and III were moderately active, compounds II were found to have a strong inhibitory effect on the proliferation of Ehrlich ascites tumor cells in vitro. Cell growth inhibition of 50% or more was found mainly in the late S- or G2-phase of the cell cycle as revealed by flow cytometry. Alkyl lysophospholipid analogs II and cholesterol form liposomes with high encapsulation efficiency and low permeability for entrapped substances. Compounds II were active against Lewis lung carcinoma in mice when applied in free form or as liposomes.
Brachwitz
H
H
Academy of Sciences, German Democratic Republic, Central Institute of Molecular Biology.
Langen
P
P
Arndt
D
D
Fichtner
I
I
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002277:Carcinoma / Q000188:drug therapy; D002286:Carcinoma, Ehrlich Tumor; D002453:Cell Cycle / Q000187:drug effects; D003603:Cytotoxins / Q000494:pharmacology; D004910:Erythrocyte Membrane / Q000187:drug effects / Q000378:metabolism; D005434:Flow Cytometry; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy; D008246:Lysophospholipids / Q000138:chemical synthesis / Q000494:pharmacology*; D051379:Mice; D010743:Phospholipids / Q000378:metabolism; D011493:Protein Kinase C / Q000378:metabolism; D014407:Tumor Cells, Cultured / Q000187:drug effects* / Q000378:metabolism
D000970:Antineoplastic Agents; D003603:Cytotoxins; D008246:Lysophospholipids; D010743:Phospholipids; D011493:Protein Kinase C