Planta Med 2018; 84(15): 1134-1140
DOI: 10.1055/a-0619-5547
Natural Product Chemistry and Analytical Studies
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Phosphodiesterase 5 Inhibitors from Derris scandens

Nattiya Chaichamnong
1  Bioscreening Unit, Department of Pharmaceutical Chemistry and Pharmacognosy, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok, Thailand
,
Prapapan Temkitthawon
1  Bioscreening Unit, Department of Pharmaceutical Chemistry and Pharmacognosy, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok, Thailand
,
Nantaka Khorana
1  Bioscreening Unit, Department of Pharmaceutical Chemistry and Pharmacognosy, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok, Thailand
,
Prompan Pitpakdeeanan
1  Bioscreening Unit, Department of Pharmaceutical Chemistry and Pharmacognosy, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok, Thailand
,
Pornnarin Taepavarapruk
2  Center for Animal Research and Department of Physiology, Faculty of Medical Science, Naresuan University, Phitsanulok, Thailand
,
Nitra Nuengchamnong
3  Science Laboratory Center, Faculty of Science, Naresuan University, Phitsanulok, Thailand
,
Yuthana Siriwattanasathien
4  Department of Chemistry, Faculty of Science, Ramkhamhaeng University, Bangkok, Thailand
,
Apichart Suksamrarn
4  Department of Chemistry, Faculty of Science, Ramkhamhaeng University, Bangkok, Thailand
,
Kornkanok Ingkaninan
1  Bioscreening Unit, Department of Pharmaceutical Chemistry and Pharmacognosy, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok, Thailand
› Author Affiliations
Further Information

Publication History

received 03 January 2018
revised 10 April 2018

accepted 19 April 2018

Publication Date:
27 April 2018 (eFirst)

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.

Supporting Information