PubMed · 5498747
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J Richter, L Kny, K Gerecke. 1970. [Vasoactive agents. 48].. https://pubmed.ncbi.nlm.nih.gov/5498747/
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Apomine (SR-45023A) is a new antineoplastic compound which is currently in clinical trials and representative of the family of cholesterol synthesis inhibitors 1,1-bisphosphonate esters. Apomine inhibits growth of a wide variety of tumor cell lines with IC(50) values ranging from 5 to 14 microM. The antiproliferative activity of apomine was studied in comparison with that of other inhibitors of the mevalonate/isoprenoid pathway of cholesterol synthesis, simvastatin, farnesol, and 25-hydroxycholesterol. All these compounds inhibit 3-hydroxy-3-methylglutaryl-coenzyme A reductase activity. Apomine (IC(50) = 14 microM), simvastatin (IC(50) = 3 microM), farnesol (IC(50) = 60 microM), and 25-hydroxycholesterol (IC(50) = 2 microM) inhibited HL60 cell growth. Growth inhibition due to simvastatin was reverted by mevalonate, whereas the antiproliferative activity of apomine, farnesol, and 25-hydroxycholesterol was not. Apomine triggered apoptosis in HL60 cells in less than 2 h. Apomine and farnesol induced caspase-3 activity at concentrations similar to their IC(50) values for cell proliferation, whereas a 10-fold excess of simvastatin was necessary to trigger apoptosis compared to its potency on proliferation. Caspase-3 activity was not induced by 25-hydroxycholesterol. The overall similar profile on mevalonate synthesis inhibition, cell growth inhibition, and apoptosis suggests that apomine acts as a synthetic mimetic of farnesol.
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The revised guidelines of the Dutch College of General Practitioners on cholesterol are more in accordance with the consensus guidelines of the Dutch Institute for Health Care Improvement. The number of people with a history of cardiovascular disease who will receive medication is probably underestimated. The guidelines attach little value to diet measurements; however, in individual cases a diet can be a realistic possibility for treatment. Screening for hypercholesterolaemia is now focused more on other risk factors. This and stopping medication in people who have been told in the past they have a treatable disease can turn out to be a problem, for which a national campaign of the public might be helpful.