Inhibition of squalene synthase of rat liver by abietane diterpenes derivatives

Inhibition of squalene synthase of rat liver by abietane diterpenes derivatives
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DOI:
10.1080/14786419.2019.1678614
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发表时间:
2019-10-19
影响因子:
2.2
通讯作者:
Marrero, Joaquin G.
Marrero, Joaquin G.
中科院分区:
化学3区
文献类型:
--
作者:
Macias-Alonso, Mariana;Andres, Lucia S.;Marrero, Joaquin G.

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本研究对人工栽培的加拿利鼠尾草的化学成分进行了测定。鼠尾草酚是分离的主要产物。我们从鼠尾草酚中制备了更多的亲脂性衍生物,并对分离和半合成的松香烷二萜进行了评价。在体外作为角鲨烯合酶的抑制剂。在测试的化合物中,鼠尾草酚是最有效的抑制剂(IC 50 = 17.6?M)。这些结果突出了该物种在生产用于治疗高脂血症的营养补充剂中的新成分方面的巨大潜力。
In the current study, chemical composition of cultivated Salvia canariensis L was determined. Carnosol was the main product isolated. We prepared more lipophilic derivatives from carnosol, and both isolated and semisynthetic abietane diterpenes were evaluated in?vitro as inhibitors of squalene synthase. Among the compounds tested, carnosol was the most potent inhibitor (IC50 = 17.6 ?M). These results highlight the great potential of this species for the production of new ingredients in nutritional supplements for the treatment of hyperlipidemia.