Ketoconazole inhibited cholesterol synthesis (greater than 90% suppression in 1 hr) rapidly by blocking the conversion of methyl sterols to cholesterol.
this is really a lot.....i wonder if this is more potent than statins
http://jpet.aspetjournals.org/content/238/3/905.short
here is a full article, i will read it fully later
chol kinetics ketoconazole
http://www.jlr.org/content/34/1/59.full.pdf+html
the reason of activity on hbsag
Abstract
Studies have demonstrated that ketoconazole and related imidazoles block gonadal and adrenal steroidogenesis in humans by inhibiting several cytochrome P-450-dependent enzymes. Moreover, recent evidence suggests that cholesterol production in humans is also affected by ketoconazole. In the present experiments cultured normal human fibroblasts have been used to explore the effects of ketoconazole on cholesterol synthesis. Ketoconazole inhibited cholesterol synthesis (greater than 90% suppression in 1 hr) rapidly by blocking the conversion of methyl sterols to cholesterol. Dihydrolanosterol was the major methyl sterol which accumulated with ketoconazole. At high concentrations of ketoconazole, the conversion of squalene to methyl sterols was also inhibited. The inhibition of cholesterol synthesis was dose-dependent with an IC50 approximately 2.8 X 10(-8) M. In parallel to the inhibition of cholesterol synthesis, there was a reciprocal increase in methyl sterol production. The related imidazole antimycotic, clotrimazole, had similar effects, whereas the imidazole anesthetic, etomidate, had little effect on cholesterol synthesis. Confluent cells exposed to ketoconazole had a 90% fall in the activity of 3-hydroxy-3-methylglutaryl coenzyme A reductase that declined with a T1/2 approximately 3.7 hr. In conclusion, ketoconazole has multiple effects on cholesterol synthesis, directly inhibiting late steps by blocking the conversion of methyl sterols to cholesterol and indirectly suppressing total sterol synthesis via feedback inhibition by sterol intermediates of 3-hydroxy-3-methylglutaryl coenzyme A reductase activity.
Stef, I thought this is talking about fungi and not viral infection. Does it work the same way? Meanwhile, just wish to know. Are you a medical doctor?
this is another clear example of how drug makers avoid ANY study about hbsag reduction.......it is better to check research ourselves since most of these drugs are already approved from a long time and very cheap generics.
the evidence is that anything that destroys or lowers lipids damages hbsag virus coat