Phenanthrenes from Eulophia macrobulbon as Novel Phosphodiesterase-5 Inhibitors

被引:2
作者
Temkitthawon, Prapapan [1 ]
Changwichit, Kanokwan [1 ]
Khorana, Nantaka [1 ]
Viyoch, Jarupa [2 ]
Suwanborirux, Khanit [3 ,4 ]
Ingkaninan, Kornkanok [1 ]
机构
[1] Naresuan Univ, Dept Pharmaceut Chem & Pharmacognosy, Phitsanulok 65000, Thailand
[2] Naresuan Univ, Dept Pharmaceut Technol, Fac Pharmaceut Sci, Phitsanulok 65000, Thailand
[3] Chulalongkorn Univ, Dept Pharmacognosy & Pharmaceut Bot, Bangkok 10330, Thailand
[4] Chulalongkorn Univ, Ctr Bioact Nat Prod Marine Organisms & Endophyt F, Fac Pharmaceut Sci, Bangkok 10330, Thailand
关键词
Eulophia macrobulbon; Phenanthrenes; Phosphodiesterase-5; inhibitors; Erectile dysfunction; ERECTILE DYSFUNCTION; SILDENAFIL CITRATE; NUDA; 9,10-DIHYDRO-2,5-DIMETHOXYPHENANTHRENE-1,7-DIOL;
D O I
暂无
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Phosphodiesterase 5 (PDE5) inhibitors can be used for the treatment of erectile dysfunction and pulmonary hypertension. In order to search for new leads of PDE5 inhibitors, we investigated the chemical constituents of the tubers of Eulophia macrobulbon (E.C. Parish & Rchb. f.) Hook. f. A new phenanthrene, 9,10-dihydro-4-(4'-hydroxybenzy1)-2,5-dimethoxyphenanthrene-1,7-diol (1) and three known phenanthrenes i.e., 1-(4'-hydroxybenzy1)-4,8-dimethoxyphenanthrene-2,7-diol (2), (9,10-dihydro-2,5-dimethoxyphenanthrene-1,7-diol (3) and 1,5,7-trimethoxyphenanthrene-2,6-diol) (4) were isolated. Among these, 2 was the most potent PDE5 inhibitor (IC50 =1.67 +/- 0.54 mu M) evaluated by the [H-3]cGMP radioassay method, whereas 1 showed mild activity (IC50 = 62.3 +/- 3.3 mu M). Their inhibitory selectivities against PDE5 over PDE6 were also studied. This study suggests phenanthrenes as a new class of PDE5 inhibitors.
引用
收藏
页码:79 / 82
页数:4
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