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Dinesh Shetty
복잡계 자기조립 연구단
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Eliminating the heart from the curcumin molecule: Monocarbonyl curcumin mimics (MACs)

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Title
Eliminating the heart from the curcumin molecule: Monocarbonyl curcumin mimics (MACs)
Author(s)
Dinesh Shetty; Kim Y.J.; Shim H.; Snyder J.P.
Publication Date
2015-01
Journal
MOLECULES, v.20, no.1, pp.249 - 292
Publisher
MDPI AG
Abstract
Curcumin is a natural product with several thousand years of heritage. Its traditional Asian application to human ailments has been subjected in recent decades to worldwide pharmacological, biochemical and clinical investigations. Curcumin’s Achilles heel lies in its poor aqueous solubility and rapid degradation at pH ~ 7.4. Researchers have sought to unlock curcumin’s assets by chemical manipulation. One class of molecules under scrutiny are the monocarbonyl analogs of curcumin (MACs). A thousand plus such agents have been created and tested primarily against cancer and inflammation. The outcome is clear. In vitro, MACs furnish a 10–20 fold potency gain vs. curcumin for numerous cancer cell lines and cellular proteins. Similarly, MACs have successfully demonstrated better pharmacokinetic (PK) profiles in mice and greater tumor regression in cancer xenografts in vivo than curcumin. The compounds reveal limited toxicity as measured by murine weight gain and histopathological assessment. To our knowledge, MAC members have not yet been monitored in larger animals or humans. However, Phase 1 clinical trials are certainly on the horizon. The present review focuses on the large and evolving body of work in cancer and inflammation, but also covers MAC structural diversity and early discovery for treatment of bacteria, tuberculosis, Alzheimer’s disease and malaria.
URI
http://pr.ibs.re.kr/handle/8788114/1638
DOI
10.3390/molecules20010249
ISSN
1420-3049
Appears in Collections:
Center for Self-assembly and Complexity(복잡계 자기조립 연구단) > Journal Papers (저널논문)
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