Differential induction of C6 glioma apoptosis and autophagy by 3β-hydroxysteroid-indolamine conjugates.

In a previous work, we reported the synthesis of four novel indole steroids and their effect on rat C6 glioma proliferation in vitro. The steroid derived from dehydroepiandrosterone and tryptamine (IS-1) was the most active (52 % inhibition at 10 µM), followed by one of the epimers derived from pregnenolone and tryptamine (IS-3, 36 % inhibition at 10 µM). By contrast, the steroid derived from estrone and tryptamine (IS-2) showed negligible activity at 10 µM.

New 3β-hydroxysteroid-indolamine conjugates: Design, synthesis and inhibition of C6 glioma cell proliferation.

Four novel indole steroids based on dehydroepiandrosterone (IS-1), estrone (IS-2) and pregnenolone (IS-3) were obtained and studied for their ability to inhibit C6 glioma proliferation. A reduction in cell proliferation by 52 ± 13% was observed for IS-1 at 10 μM, whereas IS-3 and abiraterone acetate at 10 μM caused a 36 ± 8% decrease. Surprisingly, the cellular effects reported for abiraterone, namely, cytochrome P450 CYP17A1 inhibition and endoplasmic reticulum stress were not detected for IS-1.