Department of Pharmacy Health and Nutritional Sciences, University of Calabria, Rende, Italy.
Department of Pharmacy School of Medicine and Surgery, University of Naples Federico II, Naples, Italy.
Nat Prod Res. 2021 Mar;35(5):863-866. doi: 10.1080/14786419.2019.1607337. Epub 2019 May 20.
Bunge extract was investigated for the first time for its inhibitory activity against pancreatic lipase (PL), an important enzyme involved in the digestion of dietary fats. It showed a concentration-dependent activity with an IC value of 3.54 ± 0.22 mg/mL. Two compounds, cryptotanshinone and tanshinone IIA (the major lipophilic constituents of ), have been selected as potential ligands of PL. Cryptotanshinone showed a higher lipase inhibitory activity (IC = 6.86 ± 0.43 µM) compared to the parent tanshinone IIA. Molecular docking studies were undertaken to establish whether a direct interaction of the principal constituents of the extract with the human pancreatic lipase could be evoked. All these findings provided new insights into the understanding of the interactions between natural constituents of extract and PL, also suggesting that cryptotanshinone could be used as lead compound for the development of efficacious PL inhibitors.
姜黄油首次被研究其对胰脂肪酶（PL）的抑制活性，PL 是一种参与消化膳食脂肪的重要酶。它表现出浓度依赖性活性，IC 值为 3.54 ± 0.22 mg/mL。两种化合物，隐丹参酮和丹参酮 IIA（的主要亲脂性成分），已被选为 PL 的潜在配体。隐丹参酮显示出比母体丹参酮 IIA 更高的脂肪酶抑制活性（IC = 6.86 ± 0.43 µM）。进行了分子对接研究，以确定姜黄油的主要成分是否可以与人类胰脂肪酶直接相互作用。所有这些发现为理解姜黄油提取物的天然成分与 PL 之间的相互作用提供了新的见解，也表明隐丹参酮可用作开发有效 PL 抑制剂的先导化合物。
