Chemical and Bioactivity Diversity of 2‐(2‐Phenylethyl)chromones in Agarwood: A Review

Abstract 2‐(2‐Phenylethyl)chromone derivatives are regarded as key components in agarwood. An oxygen‐containing heterocycle with a benzoannelated γ‐pyrone moiety form the bioactive core of 2‐(2‐phenylethyl)chromones. With different substituents and positions, 2‐(2‐phenylethyl)chromone derivatives exhibit diverse biological properties, such as antioxidant, antimicrobial, neuroprotective, anti‐inflammatory, and acetylcholinesterase inhibitory activities. In this review, we summarized the studies (from January 1976 to September 2021) on phytochemistry, bioactivity and quality control of 2‐(2‐phenylethyl)chromones. These studies aimed to clarify the chemical specificity, diversity and structure‐activity relationship of 2‐(2‐phenylethyl)chromones. In addition, we assumed that diverse factors such as tree species, induction methods and formation time contribute to the chemical diversity of 2‐(2‐phenylethyl)chromones. Furthermore, this review contends that different types of 2‐(2‐phenylethyl)chromones should be utilized in the quality control methods of agarwood.