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Bioassay-guided isolation of cyclooxygenase-2 inhibitory and antioxidant phenylpropanoid derivatives from the roots of Dendropanax dentiger.
Bioorganic Chemistry ( IF 5.1 ) Pub Date : 2020-09-04 , DOI: 10.1016/j.bioorg.2020.104211
Li Yang 1 , Shengzhang Liu 2 , Ronghua Liu 1 , Junwei He 3
Affiliation  

The root of Dendropanax dentiger (Harms) Merr. is a traditional Chinese medicine that has been used to treat inflammation-related diseases with little scientific validation. In this study, a bioassay-guided phytochemical investigation of D. dentiger led to the isolation of 19 phenylpropanoid derivatives including one new compound (1) and 18 known ones (219). Their structures were elucidated by NMR and HRMS as well as comparison with literature data. The ability of cyclooxygenase-2 (COX-2) inhibition and antioxidant of all isolated compounds were measured in vitro. Chlorogenic acid derivatives (1419) exhibited outstanding COX-2 inhibitory (IC50 = 5.1–93.4 μM) and antioxidant (IC50 = 13.2–31.9 μM) activities. Moreover, the tight structure-activities relationships were proposed. This is the first report on the COX-2 inhibitory activity of phenylpropanoids and D. dentiger.



中文翻译:

从Dendropanax dentiger的根部进行生物测定指导的环氧合酶2抑制性化合物和抗氧化剂苯丙烷衍生物的分离。

Dendropanax dentiger(危害)Merr的根。是一种传统中药,几乎没有经过科学验证就用于治疗炎症相关疾病。在这项研究中,生物测定引导的植物化学物质调查D. dentiger导致19个苯丙衍生物,包括一个新的化合物(的分离1)和18次公知的(2 - 19)。通过NMR和HRMS以及与文献数据的比较阐明了它们的结构。体外测定了所有分离出的化合物对环氧合酶2(COX-2)的抑制能力和抗氧化能力。绿原酸衍生物(1419)表现出出色的COX-2抑制性(IC 50  = 5.1–93.4μM)和抗氧化剂(IC 50  = 13.2–31.9μM)活性。此外,提出了紧密的结构-活性关系。这是关于苯丙烷类和D. dentiger的COX-2抑制活性的首次报道。

更新日期:2020-09-10
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