2-(2-Phenylethyl)chromone is the main bioactive component of agarwood which showed diverse pharmaceutical activities, such as anti-inflammatory activity, anticancer activity, neuroprotective activity, antioxidant activity, acetylcholinesterase inhibition activity[1].
In vitro, 2-(2-Phenylethyl)chromone (10, 50 and100μg/mL; 24h) inhibits oxLDL uptake of macrophages[2]. 2-(2-Phenylethyl)chromone (5 and 10μg/mL; 24h) significantly inhibits TCA-induced apoptosis in GES-1 cells by suppressing the PERK/eIF2α/CHOP pathway[3].
In vivo, 2-(2-Phenylethyl)chromone (50 and 100mg/kg; 6 weeks; p.o.) effectively reduces the formation of aortic plaques in atherosclerotic ApoE mice[2]. 2-(2-Phenylethyl)chromone (20 and 40mg/kg; 7 days; p.o.) reduced the gastric occurrence and ulcer inhibition rates by up to more than 70% in a dose-dependent manner[4].
References:
[1] Wang Y, Huang W, Tian W, Mo T, Yan Y, Cui X, Liu X. Enzymatic biosynthesis of novel 2-(2-phenylethyl)chromone glycosides catalyzed by UDP-glycosyltransferase UGT71BD1. Biochem Biophys Res Commun. 2023 Sep 3;671:80-86.
[2] Ma J, Wang L, Zhao Y, Gao Y, Yin Z, Zhao M, Zhao Y, Pang X, Wang J, Xue W, Tu P, Li J, Zheng J. 2-(2-Phenylethyl)chromone-enriched extract of Chinese agarwood (Aquilaria sinensis) inhibits atherosclerosis progression through endoplasmic reticulum stress-mediated CD36 expression in macrophages. J Ethnopharmacol. 2024 Feb 10;320:117411.
[3] Ma J, Huo H, Zhang H, Wang L, Meng Y, Jin F, Wang X, Zhao Y, Zhao Y, Tu P, Song Y, Zheng J, Li J. 2-(2-phenylethyl)chromone-enriched extract of the resinous heartwood of Chinese agarwood (Aquilaria sinensis) protects against taurocholic acid-induced gastric epithelial cells apoptosis through Perk/eIF2α/CHOP pathway. Phytomedicine. 2022 Apr;98:153935.
[4] Wang C, Wu Y, Gong B, Mou J, Cheng X, Zhang L, Wei J. Agarwood Chromone Alleviates Gastric Ulcers by Inhibiting the NF-κB and Caspase Pathways Based on Network Pharmacology and Molecular Docking. Pharmaceuticals (Basel). 2025 Mar 31;18(4):514.
2-(2-Phenylethyl)chromone是沉香的主要活性成分，具有多种药理作用，包括抗炎、抗癌、神经保护、抗氧化及乙酰胆碱酯酶抑制活性[1]。
在体外：2-(2-Phenylethyl)chromone (10, 50和100μg/mL; 24h)可抑制巨噬细胞对氧化低密度脂蛋白(oxLDL)的摄取[2]。2-(2-Phenylethyl)chromone (5和10μg/mL; 24h)通过抑制PERK/eIF2α/CHOP通路，显著减少TCA诱导的GES-1细胞凋亡[3]。
在体内：2-(2-Phenylethyl)chromone (50和100mg/kg; 6周; 口服)可有效减少动脉粥样硬化ApoE小鼠主动脉斑块的形成[2]。2-(2-Phenylethyl)chromone (20和40mg/kg; 7天; 口服)以剂量依赖方式使胃溃疡发生率降低、溃疡抑制率提高至70%以上[4]。