The Open Conference Proceedings Journal

2013, 4 : 210 -210
Published online 2013 March 01. DOI: 10.2174/2210289201304010210
Publisher ID: TOPROCJ-4-4-210

Curcumin Analogues as Lead for PDE5 Inhibitors

Kanokwan Changwichit , Prapapan Temkitthawon , Nantaka Khorana , Apichart Suksamrarn and Kornkanok Ingkaninan
Bioscreening Unit, Department of Pharmaceutical Chemistry and Pharmacognosy, Faculty of Pharmaceutical Sciences and Center of Excellence for Innovation in Chemistry, Naresuan University, 65000 Phitsanulok, Thailand.

ABSTRACT

Erectile Dysfunction (ED) is a common public health problem affecting millions of men worldwide. Phosphodiesterase 5 (PDE5) inhibitors can be used for the treatment of ED. However, most of PDE5 inhibitors show some undesirable side effects. The aim of the study is to search for new PDE5 inhibitors from synthesis and natural sources. In our preliminary screening, we found that curcumin, a major component in Curcuma longa L., together with its analogues showed inhibition effect on PDE5. Interestingly, some analogs showed no effect on PDE6 which is the isozyme that can be found in rod and cone cells within the eye. The IC50 value of curcumin analogue, ASKI087 against PDE5 was in a micromolar range. The curcuminoid structure could be a promising lead for PDE5 inhibitors.

Keywords:

Erectile dysfunction , Phosphodiesterase 5 inhibitors , Curcumin analogues .