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Chebulic acid derivatives from Balakata baccata and their antineuroinflammatory and antioxidant activities
Bioorganic Chemistry ( IF 5.1 ) Pub Date : 2021-09-04 , DOI: 10.1016/j.bioorg.2021.105332
Hai-Yan Zhao 1 , Qian Lan 1 , Shuang He 1 , Bao-Jun Su 1 , Ya-Qi Wang 1 , Hai-Bing Liao 1 , Heng-Shan Wang 1 , Dong Liang 1
Affiliation  

Sixteen chebulic acid derivatives, including nine new (19) and seven known (1016) ones, were isolated from an ethanol extract of the branches and leaves of Balakata baccata. The structures of the new compounds were elucidated by their UV, IR, HRESIMS, NMR, electronic circular dichroism (ECD) and single-crystal X-ray diffraction data. The effects of all the isolates on antineuroinflammatory and antioxidant activities were evaluated. Compared with the positive control minocycline (IC50 = 1.21 ± 0.71 μM), compounds 116 with IC50 values being greater than 50 μM, displayed almost no effects on the inhibition of NO production in LPS-induced BV-2 microglial cells, however, the results of antioxidant activity for compounds 116 showed significant DPPH-radical scavenging abilities with EC50 value ranging from 3.98 to 14.24 μM, while the EC50 value of positive control vitamin C was 14.31 μM. At last, the results of PCR (qRT-PCR) analysis showed that compound 1 could enhance the expression of antioxidases (HO-1, GCLC, and NQO1) at the mRNA levels.



中文翻译:

来自 Balakata baccata 的 Chebulic 酸衍生物及其抗炎症和抗氧化活性

十六chebulic酸衍生物,包括九个新(1 - 9)和七个已知的(10 - 16)的,从的枝叶的乙醇提取物中分离Balakata荆子。通过紫外、红外、HRESIMS、核磁共振、电子圆二色性(ECD)和单晶X射线衍射数据阐明了新化合物的结构。评估了所有分离株对抗神经炎症和抗氧化活性的影响。与阳性对照米诺环素 (IC 50  = 1.21 ± 0.71 μM) 相比,化合物116的 IC 50值大于50μm时,显示在NO生产中LPS诱导的BV-2小胶质细胞,然而,抗氧化活性的对化合物的结果的抑制几乎没有影响1 - 16显示显著DPPH自由基清除能力与EC 50值范围从 3.98 到 14.24 μM,而阳性对照维生素 C的 EC 50值为 14.31 μM。最后,PCR(qRT-PCR)分析结果表明,化合物1可以在mRNA水平上增强抗氧化酶(HO-1、GCLC和NQO1)的表达。

更新日期:2021-09-09
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