Phosphodiesterase 5 Inhibitors from Derris scandens.

Planta Med 2018 Oct 27;84(15):1134-1140. Epub 2018 Apr 27.

Bioscreening Unit, Department of Pharmaceutical Chemistry and Pharmacognosy, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok, Thailand.

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 stem showed phosphodiesterase 5 inhibitory activity with an IC 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 IC 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 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 stem was comprised of all eight compounds, with derrisisoflavone A (2: ) and lupalbigenin (3: ) presenting as the major constituents.

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Source
http://www.thieme-connect.de/DOI/DOI?10.1055/a-0619-5547
Publisher Site
http://dx.doi.org/10.1055/a-0619-5547DOI Listing
October 2018

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