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Curcumin is a non‐competitive and selective inhibitor of phosphorylase kinase
Abstract
Recently, we reported that curcumin (diferuloylmethane) inhibits the growth of several different kinds of tumor cells. In order to investigate the mechanism of this inhibition, we examined the effects of curcumin on different protein kinases: highly purified protein kinase A (PkA), protein kinase C (PkC), protamine kinase (cPK), phosphorylase kinase (PhK), autophosphorylation‐activated protein kinase (AK) and pp60 c‐src tyrosine kinase. While all kinases tested were inhibited by curcumin, only PhK was completely inhibited at relatively lower concentrations. At around 0.1 mM curcumin, PhK, pp60 c‐src, PkC, PkA, AK, and cPK were inhibited by 98%, 40%, 15%, 10%, 1%, and 0.5%, respectively. Lineweaver‐Burk plot analysis indicated that curcumin is a non‐competitive inhibitor of PhK with a K i of 0.075 mM. Overall, our results indicate that curcumin is a potent and selective inhibitor of phosphorylase kinase, a key regulatory enzyme involved in the metabolism of glycogen. This has important implications for the anti‐proliferative effects of curcumin.
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Cited by
Therapeutic Roles of Curcumin: Lessons Learned from Clinical Trials
Gupta, S. C., Patchva, S., & Aggarwal, B. B. (2013) · The AAPS Journal · doi:10.1208/s12248-012-9432-8 · Cited by 2,110
Self-citationMultiple biological activities of curcumin: A short review
Maheshwari, R. K., Singh, A. K., Gaddipati, J., & Srimal, R. C. (2006) · Life Sciences · doi:10.1016/j.lfs.2005.12.007 · Cited by 1,674
CURCUMIN: THE INDIAN SOLID GOLD
Aggarwal, B. B., Sundaram, C., Malani, N., & Ichikawa, H. (2007) · ADVANCES IN EXPERIMENTAL MEDICINE AND BIOLOGY · doi:10.1007/978-0-387-46401-5_1 · Cited by 1,647
Self-citationAggarwal, B. B., & Sung, B. (2009) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2008.11.002 · Cited by 1,140
Self-citationCurcumin: An Anti-Inflammatory Molecule from a Curry Spice on the Path to Cancer Treatment
Basnet, P., & Skalko-Basnet, N. (2011) · Molecules · doi:10.3390/molecules16064567 · Cited by 733
Metadata
- Authors
- Reddy, S., & Aggarwal, B. B.
- Venue
- FEBS Letters
- Publisher
- Wiley
- Published
- 1994-03-14
- Volume
- 341
- Issue
- 1
- Pages
- 19-22
- ISSN
- 0014-5793 (ISSN-L)
- 1873-3468
- OpenAlex
- W2086046451
- Cited by
- 225
- References
- 0
- FWCI
- 2.22
- Type
- journal article
- Language
- en
- Open access
- closed
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- Reddy, S., & Aggarwal, B. B. (1994). Curcumin is a non‐competitive and selective inhibitor of phosphorylase kinase. FEBS Letters. https://doi.org/10.1016/0014-5793(94)80232-7
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