Zhang Mingliang, Niu Mengrong, Fan Jiangping, Lu Zihan, Zhu Zhixiang, Gao Bowen, Shi She-Po
Modern Research Center for Traditional Chinese Medicine, Beijing Institute of Traditional Chinese Medicine, Beijing University of Chinese Medicine, Beijing 102488, China; School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, China.
Modern Research Center for Traditional Chinese Medicine, Beijing Institute of Traditional Chinese Medicine, Beijing University of Chinese Medicine, Beijing 102488, China.
Fitoterapia. 2025 Jan;180:106296. doi: 10.1016/j.fitote.2024.106296. Epub 2024 Nov 13.
2-(2-Phenylethyl)chromones (PECs), the pivotal constituents responsible for the distinctive aroma and pharmacological potential of agarwood, are primarily obtained through extraction from natural materials. The restricted availability of agarwood has, however, hindered a comprehensive and systematic evaluation of their biological properties. In this study, we have chemically synthesized a total of 38 PEC derivatives, including 23 new compounds that had not been previously isolated from agarwood. These compounds were then evaluated for their inhibitory effects on nitric oxide release, neutrophil superoxide production, as well as their activities against tyrosinase, acetylcholinesterase, and α-glucosidase. The preliminary screening resulted in the identification of promising leads with potential therapeutic activities, and the structure-activity relationship of the synthesized PECs have also been briefly discussed. The results provide a foundation for the synthesis and pharmacological exploration of PECs, which sheds light on the pharmacological potential of agarwood's secondary metabolites.
2-(2-苯乙基)色酮（PECs）是沉香独特香气和药理潜力的关键成分，主要通过从天然材料中提取获得。然而，沉香的有限供应阻碍了对其生物学特性进行全面系统的评估。在本研究中，我们总共化学合成了38种PEC衍生物，其中包括23种以前未从沉香中分离出来的新化合物。然后评估了这些化合物对一氧化氮释放、中性粒细胞超氧化物产生的抑制作用，以及它们对酪氨酸酶、乙酰胆碱酯酶和α-葡萄糖苷酶的活性。初步筛选确定了具有潜在治疗活性的有前景的先导化合物，并且还简要讨论了合成的PECs的构效关系。这些结果为PECs的合成和药理探索提供了基础，揭示了沉香次生代谢产物的药理潜力。
