Recent progress on curcumin-based therapeutics: a patent review (2012-2016). Part II: curcumin derivatives in cancer and neurodegeneration

ABSTRACT

Introduction: Curcumin, the main bioactive compound found in the rhizome of Curcuma longa L., is considered a ‘privileged structure’, due to its ability to modulate different signaling pathways involved in the pathogenesis of several diseases. Unfortunately, its poor pharmacodynamic and pharmacokinetic properties, mainly related to chemical instability, low solubility and rapid metabolism, greatly reduce its therapeutic potential. In the last years a number of derivatives were developed and patented, aimed both at improving its multifaceted biological profile and overcoming its undesired effects.

Areas covered: This review summarizes the patent literature of the last five years dealing with synthetic curcumin-related compounds in cancer and neurodegeneration, properly designed in order to avoid the so-called ‘dark side of curcumin’, and to take advantage of the beneficial properties of this molecule, worth to be further exploited to obtain effective therapeutics.

Expert opinion: Due to the synergistic binding to several networked targets, curcumin turned out to be suitable for polypharmacological approaches, and its ‘privileged structure’ could also provide the key scaffold to develop novel multipotent drugs useful for treating multifactiorial pathologic conditions such as cancer and neurodegeneration.

KEYWORDS:

• Azheimer’s disease
• cancer
• curcumin
• natural products
• neurodegeneration
• privileged structures

Article highlights

• Natural products have continued to enter clinical trials and to provide leads to be developed in order to both take advantage of the multiple biological activities and improve the pharmacokinetic profile, often unsatisfactory.

• Curcumin, the main bioactive compound found in the rhizome of Curcuma longa L., emerged as promising scaffold to be properly optimized in order to exploit its recognized biological actions.

• A large variety of curcumin-based analogues have been designed and synthesized with the aim to improve and expand its pharmacological profile.

• Hybrid compounds obtained by covalently linking curcumin to properly selected molecular fragments are of great potential in obtaining effective therapeutic agents.

• Effective anticancer and neurotherapeutic drug-candidates have been developed, providing supports on recognizing curcumin as worth to be considered a valuable lead compound in medicinal chemistry.

This box summarizes key points contained in the article.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

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Funding

This paper has not been funded.