RESUMO
The inhibitory effect against 5-α reductase of the ethyl acetate (EA) extract from Physalis angulata was evaluated in vitro using mouse prostate homogenates, and the suppression of benign prostatic hyperplasia (BPH) was assessed in a mouse model of testosterone-induced BPH. The EA extract exhibited a potentially inhibitory effect on 5-α reductase with an IC50 of 197 µg/ml. In BPH mice, the EA extract at a dose of 12 mg/kg was comparable to finasteride 5 mg/kg in suppressing BPH in terms of reducing absolute enlarged prostate weight (p < 0.05 vs. BPH group) and mitigating the hypertrophy of glandular elements and prostate connective tissue. Identification of chemical ingredients in the EA extract by UPLC-QTOF-MS revealed 37 substances belonging chiefly to flavonoids and physalins. Further quantification of the EA extract by HPLC-PDA methods revealed that chlorogenic acid, and rutin were the main components. Molecular docking studies of chlorogenic acid and rutin on 5-α reductase showed their high affinity to the enzyme with binding energies of -9.3 and - 9.2 kcal/mol, respectively compared with finasteride (- 10.3 kcal/mol). Additionally, chlorogenic acid inhibited 5-α reductase with an IC50 of 12.07 µM while rutin did not. The presence of chlorogenic acid in the EA extract may explain the inhibitory effects of the EA extract on 5-α reductase, and thus the suppression of BPH.
Assuntos
Inibidores de 5-alfa Redutase , Simulação de Acoplamento Molecular , Physalis , Extratos Vegetais , Hiperplasia Prostática , Animais , Hiperplasia Prostática/tratamento farmacológico , Masculino , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Camundongos , Physalis/química , Inibidores de 5-alfa Redutase/farmacologia , Inibidores de 5-alfa Redutase/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Estrutura Molecular , Ácido Clorogênico/farmacologia , Ácido Clorogênico/isolamento & purificação , Próstata/efeitos dos fármacos , Modelos Animais de DoençasRESUMO
A new compound, 3β-acetoxylanosta-7,9(11),24-triene-26-al (3), and seven known compounds (1 – 2 and 4 – 8) were isolated from Ganoderma tropicum (Jung.) Bres. collected in Tay Nguyen, Vietnam. The structures of these compounds were determined by one- and two-dimensional nuclear magnetic resonance spectroscopy, electrospray ionization mass spectrometry (ESI-MS), and high-resolution ESI-MS, and by comparison with literature data. All of the isolated compounds were tested for nitroblue tetrazolium (NBT) reduction activity in Saccharomyces cerevisiae-stimulated RAW 246.7 cells. Among them, compounds 2 – 4 and 6 – 8 enhanced the NBT reduction in a dose-dependent manner.
RESUMO
A new compound, 3β-acetoxylanosta-7,9(11),24-triene-26-al (3), and seven known compounds (1 – 2 and 4 – 8) were isolated from Ganoderma tropicum (Jung.) Bres. collected in Tay Nguyen, Vietnam. The structures of these compounds were determined by one- and two-dimensional nuclear magnetic resonance spectroscopy, electrospray ionization mass spectrometry (ESI-MS), and high-resolution ESI-MS, and by comparison with literature data. All of the isolated compounds were tested for nitroblue tetrazolium (NBT) reduction activity in Saccharomyces cerevisiae-stimulated RAW 246.7 cells. Among them, compounds 2 – 4 and 6 – 8 enhanced the NBT reduction in a dose-dependent manner.