Inhibition of 5 alpha-reductase and aromatase by PHL-00801 (Prostatonin(R)), a combination of PY 102 (Pygeum africanum) and UR102 (Urtica dioica) extracts

被引:25
作者
Hartmann, RW
Mark, M
Soldati, F
机构
[1] PHARMATON SA,RES & DEV,CH-6903 LUGANO,SWITZERLAND
[2] UNIV SAARLAND,FACHRICHTUNG PHARMAZEUT CHEM,D-66041 SAARBRUCKEN,GERMANY
[3] DR KARL THOMAE GMBH,DEPT BIOCHEM RES,D-88937 BIBERACH,GERMANY
关键词
5; alpha-reductase; aromatase; benign prostatic hyperplasia; Urtica dioica UR 102 extract; Pygeum africanum PY 102 extract; PHL-00801 (Prostatonin(R));
D O I
10.1016/S0944-7113(96)80025-0
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
This study was undertaken to evaluate a possible effect of the extracts PY 102 of Pygeum africanum (Hook), and UR 102 of Urtica dioica L. as well as their combination PHL-00801 (Prostatonin(R)) on the enzymes 5 alpha-reductase (5 alpha-RE) and aromatase (AR): Inhibition of 5 alpha-RE: Pygeum africanum extract PY 102, and Urtica dioica extract UR 102, inhibited the 5 alpha-RE activity in a concentration dependent manner. Whereas UR 102 extract was only able to influence the enzyme activity at high concentrations (greater than or equal to 12 mg/ml) and its ED(50) being calculated as 14.7 mg/ml, the PY 102 extract showed a much higher activity starting with low concentrations (0.1 mg/ml) its ED(50) being calculated as 0.78 mg/ml. When compared with the effects of UR 102, the combination of both extracts, PHL-00801 (Prostatonin(R)), led to a similar inhibition of the enzyme (ED(50) 14.15 mg/ml). Inhibition of AR: The PY 102 extract showed a concentration dependent and strong activity (ED(50) = 0.98 mg/ml). The activity of the UR 102 extract was also concentration dependent (ED(50) = 3.58 mg/ml). The combination of both extracts, PHL-00801 (Prostatonin(R)) showed a synergistic action and significantly (p = 0.05) increased the AR-inhibitory activity in concentrations as low as 0.1 mg/ml (ED(50) 0.24 mg/ml). These observations are an explanation for the beneficial effects of PHL-00801 (Prostatonin(R)) observed in the clinical studies on BPH.
引用
收藏
页码:121 / 128
页数:8
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