Antiangiogenic Effect of Curcumin in Pure Versus in Extract Forms

Abstract

Curcumin isolated from turmeric (Curcuma longa L., Zingaberaceae) root was found to be anti-angiogenic in a human tissue-based angiogenesis assay. As a liposoluble compound, curcumin can be extracted from turmeric root with organic solvents such as ethanol or acetone. Curcumin in its pure form has poor solubility in water, potentially limiting its medicinal use for humans when it is taken orally or injected. This study attempted to investigate the possibility of improving curcumin's low solubility using an extract as a carrier. This would maintain anti-angiogenic properties with improved water-solubility. Experiments were undertaken to determine the extraction efficiency of different solvents for curcumin. Anti-angiogenic activities of curcumin in its pure form and in extracts were compared as a general trend ethanol or acetone was more efficient in extracting curcumin than their aqueous counterparts. Using 50 and 70% aqueous ethanol as well as 70% aqueous acetone yielded significantly more turmeric extracts by weight than absolute acetone, which was the lowest. Conversely, turmeric extracts extracted with 95% ethanol and absolute acetone contained significantly higher curcumin concentrations than water extract, which was the lowest. Combining the higher extract yield and highest curcumin concentrations in the extract, 95% ethanol gave the highest yield of single entity curcumin. In the angiogenesis assay, pure curcumin at the concentration of 85 µM (in 1% ethanol v/v) in the culture medium totally suppressed angiogenic responses. In contrast, a curcumin concentration of 18.5 µM (in the form of 100 µg/ml turmeric extract) achieved the same total inhibition of angiogenesis in culture. This nearly 5 fold gap reflected the unaccounted involvement of other antiangiogenic compounds including curcumin derivatives, and/or enhancement of curcumin by Accepted: 11 February 2008 Address correspondence to: Zhijun Liu, School of Renewable Natural Resources, LSU Agricultural Center, Baton Rouge, LA 70803. E-mail: zhiliu@lsu.edu non-antiangiogenic compounds in the extract. This finding suggests that curcumin in the form of extracts be potentially more pharmacologically active than pure curcumin. Further investigations of this hypothesis and possible interactions are warranted.

A Novel Solubility-Enhanced Curcumin Formulation Showing Stability and Maintenance of Anticancer Activity

“…1) is a natural compound found in the root of Curcuma longa L. (Zingiberaceae), which has been widely used as a yellow pigment, a spice in the food industry, and a traditional medicine in Asia. Mounting scientific evidence indicates that CUR is a versatile bioactive compound possessing antioxidant, 1 anti-inflammatory, 2 antihyperlipidemic, 3 liver antifibrotic, 4 antiangiogenic, 5 antineoplastic, and chemoprotective properties. 6 The diverse bioactivities displayed by this single natural compound have made CUR a subject of intense and broad investigations for potential functional and medicinal foods as well as drug development for the prevention and treatment of various diseases such as colon cancer, 7 cystic fibrosis, 8 inflammatory bowel disease, 9 and HIV infection.…”

Turmeric (Curcuma longa) Decoctum Had no Effect on Vascular Endothelial Growth Factor (VEGF) and Vascular Endothelial Cadherin (VE-cadherin) Expression in the Chick Embryo

“…Curcuminoids are poorly soluble in water, but soluble in ethanol, methanol, acetone and DMSO (Li et al, 2011). The limit of curcumin solubility in water is 0.29% (w/w) (Liu et al, 2008).…”

Recycling preparative high performance liquid chromatography for the separation of curcumin from curcuminoids incurcuma longaL.

“…The optimum condition for good resolution was obtained with C18 column, methanolwater (50:50 v/v), at pH = 7, flow rate 1 mL/min and without any salts at room temperature. 1 Gradient technique by using methanol and water as mobile phase solvents 2 Isocratic method by using methanol and water as mobile phases with ratio of 50:50, respectively 3 Separation factor between BDMC and DMC 4 Resolution between BDMC and DMC 5 Resolution between C and DMC 6 Separation factor between C and DMC…”

“…1). These compounds have many physiological properties, but lately, it was reported that curcumin is the main bioactive constituent of turmeric rhizome and has a wide range of pharmacological activities, including antiinflammatory [1,2], anticancer [1,3,4], anti-oxidant [1,5], anti-angiogenic [6], and immune modulatory [7]. Another study has also shown that cur-cumin is a potential chemotherapeutic agent for cancer as well as a promising agent in the treatment and prevention of Alzheimer's disease [8].…”