Assignment 2: Writing an introduction

Water Solubility, Stability and Anticancer Activity of Curcumin and

Curcumin Diglutaric Acid

Stage 1:

To date, a number of phytochemicals have been explored for pharmaceutical applications as therapeutic agents by virtue of their high biological activities. They have been shown to play crucial roles in the pathogenesis of chronic diseases, such as inflammation, atherosclerosis and cancer (Aggarwal & Shishodia, 2006).  One of the extensively investigated plants is Curcuma longa L., called turmeric in English and Kamin-Chan in Thai.

Stage 2:

Tumeric contains turmerin, essential oils and curcuminiods. Commercial curcuminiods contain approximately 77% diferuloylmethane (curcumin), 17% demethoxycurcumin, and 6% bis-demethoxycurcumin. Therefore, curcumin has been identified as the major active component of turmeric extract (Jayaprakasha et al., 2002). Curcumin has been identified as the major active component of turmeric extract and shown to exhibit many pharmaceutical actions such as antioxidant (Ruby et al., 1995; Sabari et al., 2005), anti-inflammatory (Aggarwal et al., 2003; Lantz et al., 2005), and anticancer activities (Sugiyama et al., 1996; Sharma et al., 2005). Various animal models or human studies proved that curcumin is extraordinarily safe even at very high doses uptake (Ringman et al., 2005).

Stage 3:

Despite the fact that its efficacy and safety has been known, curcumin has not yet been approved as a therapeutic agent because of a major problem of its low bioavailability caused by low water solubility and instability in aqueous and basic solutions.  

Stage 4&5:

The objective of this study is an attempt to enhance solubility and stability for increase oral bioavailability of curcumin by using a prodrug methodology. A curcumin prodrug, curcumin diglutaric acid, was synthesized by conjugation of curcumin with diglutaric acid via ester bonds. Curcumin diglutaric acid was designed to have improved aqueous solubility and enhanced chemical stability by comparing with curcumin. Moreover, the anticancer activity of curcumin and curcumin diglutaric acid were also tested against human cancer cell lines such as colon and liver cancer cells.