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DOI: 10.1055/a-0619-5547
Phosphodiesterase 5 Inhibitors from Derris scandens
Publikationsverlauf
received 03. Januar 2018
revised 10. April 2018
accepted 19. April 2018
Publikationsdatum:
27. April 2018 (online)
Abstract
Phosphodiesterase 5 inhibitors have been used as a first-line medicine for the treatment of erectile dysfunction. In the search for new phosphodiesterase 5 inhibitors from natural sources, we found that the 95% ethanol extract of Derris scandens stem showed phosphodiesterase 5 inhibitory activity with an IC50 value of about 7 µg/mL. Seven isoflavones and a coumarin constituent isolated from this plant were investigated for phosphodiesterase 5 inhibitory activity. The results showed that osajin (8), 4′,5,7-trihydroxybiprenylisoflavone (4), and derrisisoflavone A (2) had the ability to inhibit phosphodiesterase 5 with IC50 values of 4, 8, and 9 µM, respectively. These compounds exhibited selectivity on phosphodiesterase 5 over phosphodiesterase 1, however, the selectivity on phosphodiesterase 5 over phosphodiesterase 6 was low. In order to quantitatively determine these bioactive constituents in D. scandens extract, LC-QTOF-MS method has been developed and validated. The limit of quantitation values in the range of 0.1 – 5 µg/mL were obtained. The assay showed satisfactory precision and accuracy. The results from our method showed that the 95% ethanol extract of D. scandens stem was comprised of all eight compounds, with derrisisoflavone A (2) and lupalbigenin (3) presenting as the major constituents.
Key words
Derris scandens - Fabaceae - phosphodiesterase 5 - erectile dysfunction - isoflavoner - LC-QTOF-MSSupporting Information
- Supporting Information
The dose-response curves of the active compounds and information from the LC-QTOF-MS method validation are available as Supporting Information.
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