Inhibition Of5alpha Reductase

In different cell systems, the Iipid-sterolic extract acts as a non-competitive inhibitor of both type 1 and type 2 5-alpha reductase activity, thereby preventing the conversion of testosterone to dihydrotestosterone (Bayne et al 2000, Raynaud et al 2002, Sultan et al 1984). However, it is currently unclear whether the effect is apparent in humans, as contradictory evidence exists. Raynaud et al (2002) explained that the discrepancies found by different authors were due to different experimental conditions and selectivity for fatty acids, as only specific aliphatic unsaturated fatty acids have been shown to inhibit 5-alpha reductase activity.

One study that analysed and compared BPH samples taken from both untreated and treated subjects (320 mg saw palmetto extract taken for 3 months) found that local levels of testosterone were raised, whereas dihydrotestosterone levels were reduced, suggestive of local 5-alpha reductase inhibition (Di Silverio et al 1998). An earlier, short-term study found that a dose of 160 mg of a liposterolic extract (Permixon) produced no changes to serum dihydrotestosterone levels, whereas finasteride 5 mg induced a significant reduction (Strauch et al 1994). Since prostate levels were untested in this study, it is not known whether a local effect occurred, even though serum levels remained unchanged.

Unlike other 5-alpha reductase inhibitors, there is no interference with the cell's capacity to secrete prostate-specific antigens because it does not affect the transcription of the gene for prostate-specific antigen (PSA), as demonstrated both in vitro and in vivo (Maccagnano et al 2006). Although having an obvious clinical advantage in regard to PSA screening for prostate cancer, this also suggests that 5-alpha reductase inhibition is not a major activity.

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