Resveratrol derivatives: an updated patent review (2012-2015)

ABSTRACT

Introduction: Resveratrol is a well-studied natural small molecule that possesses diverse bioactivities. Chemical derivation based on the resveratrol scaffold is of great importance to overcome the drawbacks of resveratrol and to improve its therapeutic potential. Continuous efforts have been established to develop resveratrol derivatives that target different therapeutic applications.

Areas covered: This review covers patents published from 2012 to 2015. All resveratrol derivatives discussed are classified based on its derivation strategy as simple derivatives, conjugated derivatives and miscellaneous derivatives. Their therapeutic related activities are reviewed and discussed.

Expert opinion: Chemical derivation is an effective strategy to enhance the benefits of resveratrol and ameliorate its disadvantages. Recent studies on resveratrol derivatives have made great progress in the treatment of cancer and neurodegenerative diseases to name a few, demonstrating improved activity compared with resveratrol. Notably, its bioavailability was also improved in some cases. However, the ‘next generation’ of resveratrol derivatives still requires the development of new strategies and techniques.

KEYWORDS:

• Resveratrol
• resveratrol derivatives
• anticancer
• antioxidant
• chemoprevention
• bioavailability
• polymer-drug conjugate

Article highlights

• Patents on resveratrol derivatives using diverse strategies to ameliorate the limitations of resveratrol in therapeutic applications are reported for the years 2012–2015.

• Different strategies were employed to prepare effective resveratrol derivatives, including modification of the hydroxyl groups and conjugation, among others.

• Conjugated resveratrol derivatives have been introduced in recent years and some patents covered several task-specific conjugates, with better solubility in water and thus potentially higher bioavailability.

• Most resveratrol derivatives described in the patents targeted cancer, cardio diseases, metabolism disorders (e.g., diabetes and obesity) and neurological diseases (e.g., Alzheimer’s).

• There is increasing interest in the potential of resveratrol derivatives in chemoprevention and cosmetic products.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.

Additional information

Funding

This paper has been funded by National Science Foundation of China (21502168) and Fundamental Research Funds for the Central Universities (2016QNA7027).