Cryptotanshinone and tanshinone IIA from Salvia milthorrhiza Bunge (Danshen) as a new class of potential pancreatic lipase inhibitors
Cryptotanshinone and tanshinone IIA from Salvia milthorrhiza Bunge (Danshen) as a new class of potential pancreatic lipase inhibitors
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DOI：
10.1080/14786419.2019.1607337
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发表时间：
2019-05-15
影响因子：
2.2
通讯作者：
Conforti, Filomena
中科院分区：
文献类型：
--
作者：
Marrelli, Mariangela;Grande, Fedora;Conforti, Filomena
首次研究了丹参提取物对胰腺脂肪酶(PL)的抑制活性，该酶是参与消化膳食脂肪的重要酶。该酶具有浓度依赖性，其IC50值为3.54+/-0.22 mg/mL。两个化合物隐丹参酮和丹参酮IIA(丹参酮IIA是丹参的主要亲脂成分)已被选为潜在的PL配体。隐丹参酮具有比亲本丹参酮IIA更高的脂肪酶抑制活性(IC50=6.86+/-0.43µM)。进行了分子对接研究，以确定丹参提取物的主要成分是否可以与人胰腺脂肪酶直接相互作用。所有这些发现为理解丹参提取物的天然成分与PL之间的相互作用提供了新的见解，也表明隐丹参酮可以作为先导化合物用于开发有效的PL抑制剂。
Salvia miltiorrhiza 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 IC50 value of 3.54 +/- 0.22 mg/mL. Two compounds, cryptotanshinone and tanshinone IIA (the major lipophilic constituents of S. miltiorrhiza), have been selected as potential ligands of PL. Cryptotanshinone showed a higher lipase inhibitory activity (IC50 = 6.86 +/- 0.43 mu M) compared to the parent tanshinone IIA. Molecular docking studies were undertaken to establish whether a direct interaction of the principal constituents of the S. miltiorrhiza 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 S. miltiorrhiza extract and PL, also suggesting that cryptotanshinone could be used as lead compound for the development of efficacious PL inhibitors.[GRAPHICS].