Anti-Inflammatory ent-Kaurane Diterpenoids from Isodon serra,Journal of Natural Products

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Anti-Inflammatory ent-Kaurane Diterpenoids from Isodon serra
Journal of Natural Products ( IF 3.3 ) Pub Date : 2020-09-29 , DOI: 10.1021/acs.jnatprod.9b01281
Honghong Xing ₁ , Lijun An ₁ , Ziteng Song ₁ , Shanshan Li ₁ , Huimei Wang ₁ , Chunyan Wang ₂ , Jie Zhang ₃ , Muhetaer Tuerhong ₄ , Munira Abudukeremu ₄ , Dihua Li ₅ , Dongho Lee ₆ , Jing Xu _{1,

7} , Namrita Lall ₈ , Yuanqiang Guo ₁

Affiliation

State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, People's Republic of China.
Tianjin Second People's Hospital, Tianjin 300192, People's Republic of China.
Key Laboratory for Green Processing of Chemical Engineering of Xinjiang Bingtuan, School of Chemistry and Chemical Engineering, Shihezi University, Shihezi 832003, People's Republic of China.
College of Chemistry and Environmental Sciences, Kashgar University, Kashgar 844000, People's Republic of China.
Tianjin Institute of Acute Abdominal Diseases of Integrated Traditional Chinese and Western Medicine, Nankai Hospital Affiliated to Nankai University, Tianjin 300100, People's Republic of China.
College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea.
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, People's Republic of China.
Department of Plant and Soil Sciences, University of Pretoria, Pretoria 0002, South Africa.

Ten new ent-kaurane diterpenoids, including two pairs of epimers 1/2 and 4/5 and a 6,7-seco-ent-kauranoid 10, were obtained from the aerial parts of Isodon serra. The structures of the new compounds were confirmed by extensive spectroscopic methods and electronic circular dichroism (ECD) data analysis. An anti-inflammatory assay was applied to evaluate their nitric oxide (NO) inhibitory activities by using LPS-stimulated BV-2 cells. Compounds 1 and 9 exhibited notable NO production inhibition with IC₅₀ values of 15.6 and 7.3 μM, respectively. Moreover, the interactions of some bioactive diterpenoids with inducible nitric oxide synthase (iNOS) were explored by employing molecular docking studies.

中文翻译：

来自 Isodon serra 的抗炎 ent-Kaurane Diterpenoids

十个新ENT -kaurane二萜类化合物，其中包括2双差向异构体的1 / 2和4 / 5和6,7-开环- ENT -kauranoid 10，从地上部分获得香茶塞拉。新化合物的结构通过广泛的光谱方法和电子圆二色性 (ECD) 数据分析得到证实。通过使用 LPS 刺激的 BV-2 细胞，应用抗炎测定来评估它们的一氧化氮 (NO) 抑制活性。化合物1和9表现出显着的NO产生抑制作用，IC ₅₀值分别为 15.6 和 7.3 μM。此外，通过分子对接研究探索了一些生物活性二萜与诱导型一氧化氮合酶 (iNOS) 的相互作用。

更新日期：2020-10-26

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