Synthesis and pharmacological activity evaluation of 2-(2-Phenylethyl)chromone analogues: The principal components in agarwood

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia Pub Date : 2024-11-13 DOI:10.1016/j.fitote.2024.106296

Mingliang Zhang , Mengrong Niu , Jiangping Fan , Zihan Lu , Zhixiang Zhu , Bowen Gao , She-Po Shi

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Abstract

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.

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2-(2-苯基乙基)铬酮类似物的合成和药理活性评价：沉香中的主要成分。

2-(2-苯基乙基)色酮（PECs）是沉香木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，由于沉香的可获得性有限，阻碍了对其生物特性进行全面系统的评估。在这项研究中，我们用化学方法合成了 38 种 PEC 衍生物，其中包括 23 种以前从未从沉香木中分离出来的新化合物。然后对这些化合物对一氧化氮释放、中性粒细胞超氧化物生成的抑制作用，以及对酪氨酸酶、乙酰胆碱酯酶和α-葡萄糖苷酶的活性进行了评估。通过初步筛选，确定了具有潜在治疗活性的有希望的先导化合物，并简要讨论了合成的 PECs 的结构-活性关系。这些结果为 PECs 的合成和药理探索奠定了基础，从而揭示了沉香次生代谢物的药理潜力。

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来源期刊

Fitoterapia 医学-药学

CiteScore

5.80

自引率

2.90%

发文量

198

审稿时长

1.5 months

期刊介绍： Fitoterapia is a Journal dedicated to medicinal plants and to bioactive natural products of plant origin. It publishes original contributions in seven major areas: 1. Characterization of active ingredients of medicinal plants 2. Development of standardization method for bioactive plant extracts and natural products 3. Identification of bioactivity in plant extracts 4. Identification of targets and mechanism of activity of plant extracts 5. Production and genomic characterization of medicinal plants biomass 6. Chemistry and biochemistry of bioactive natural products of plant origin 7. Critical reviews of the historical, clinical and legal status of medicinal plants, and accounts on topical issues.