Premium
A broadly neuroprotective derivative of curcumin
Author(s) -
Liu Yuanbin,
Dargusch Richard,
Maher Pamela,
Schubert David
Publication year - 2008
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.2008.05236.x
Subject(s) - neuroprotection , curcumin , excitotoxicity , pharmacology , oxidative stress , chemistry , extracellular , programmed cell death , biochemistry , apoptosis , biology
The plant polyphenolic curcumin alters the response of nerve cells to some forms of toxic stress. The steroid‐like compound, cyclohexyl bisphenol A, has broad neuroprotective properties that are very distinct from those of curcumin. To incorporate both families of biological activities into a single molecule, a pyrazole derivative of curcumin, called CNB‐001, was synthesized. CNB‐001 acquires a new activity and is far superior in neuroprotection assays to either parental molecule, but retains some of the properties of both. It is neuroprotective in cell culture assays for trophic factor withdrawal, oxidative stress, excitotoxicity, and glucose starvation, as well as toxicity from both intracellular and extracellular amyloid. While the creation of CNB‐001 was based upon an uncommon approach to drug design, it has the potential of a lead drug candidate for treating multiple conditions involving nerve cell death.