Phosphodiesterase 5 Inhibitors from Derris scandens

被引：9

作者：

Chaichamnong, Nattiya ^{[1
]}

Temkitthawon, Prapapan ^{[1
]}

Khorana, Nantaka ^{[1
]}

Pitpakdeeanan, Prompan ^{[1
]}

Taepavarapruk, Pornnarin ^{[2
,3
]}

Nuengchamnong, Nitra ^{[4
]}

Siriwattanasathien, Yuthana ^{[5
]}

Suksamrarn, Apichart ^{[5
]}

Ingkaninan, Kornkanok ^{[1
]}

机构：

[1] Naresuan Univ, Fac Pharmaceut Sci, Dept Pharmaceut Chem & Pharmacognosy, Bioscreening Unit, Nakhon Sawan Rd, Phitsanulok 65000, Thailand

[2] Naresuan Univ, Fac Med Sci, Ctr Anim Res, Phitsanulok, Thailand

[3] Naresuan Univ, Fac Med Sci, Dept Physiol, Phitsanulok, Thailand

[4] Naresuan Univ, Fac Sci, Sci Lab Ctr, Phitsanulok, Thailand

[5] Ramkhamhang Univ, Fac Sci, Dept Chem, Bangkok, Thailand

来源：

PLANTA MEDICA | 2018年 / 84卷 / 15期

关键词：

Derris scandens; Fabaceae; phosphodiesterase; 5; erectile dysfunction; isoflavoner; LC-QTOF-MS; DERIVATIVES; POTENT;

D O I：

10.1055/a-0619-5547

中图分类号：

Q94 [植物学];

学科分类号：

071001 ;

摘要：

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 mu g/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 mu M, 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 mu g/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.

引用

页码：1134 / 1140

页数：7

共 29 条

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