Diterpenoids from the leaves of Casearia kurzii showing cytotoxic activities.,Bioorganic Chemistry

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Diterpenoids from the leaves of Casearia kurzii showing cytotoxic activities.
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2020-03-09 , DOI: 10.1016/j.bioorg.2020.103741
Yue Liang ₁ , Qi Zhang ₁ , Xueyuan Yang ₁ , Ying Li ₁ , Xuke Zhang ₁ , Yuhao Li ₂ , Qing Du ₃ , Da-Qing Jin ₂ , Jianlin Cui ₂ , Namrita Lall ₄ , Muhetaer Tuerhong ₅ , Dongho Lee ₆ , Munira Abudukeremu ₅ , Jing Xu ₇ , Ling Shuai ₁ , 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.
School of Medicine, Nankai University, Tianjin 300071, People's Republic of China.
Key Laboratory for Tibet Plateau Phytochemistry of Qinghai Province, College of Pharmacy, Qinghai Nationalities University, Xining 810007, People's Republic of China.
Department of Plant and Soil Sciences, University of Pretoria, Pretoria 0002, South Africa.
College of Chemistry and Environmental Sciences, Laboratory of Xinjiang Native Medicinal and Edible Plant Resources Chemistry, Kashgar University, Kashgar 844000, People's Republic of China.
Department of Biosystems and Biotechnology, College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea.
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; State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Guangxi Normal University, Guilin 541004, People's Republic of China.

A phytochemical investigation to obtain bioactive substances as lead compounds or agents for cancer led to the obtainment of six new and two known clerodane diterpenoids from the leaves of Casearia kurzii. Their structures were elucidated using NMR techniques and electronic circular dichroism (ECD) calculations. The subsequent biological cytotoxicity evaluation of these isolates toward human lung cancer A549, human cervical cancer HeLa, human chronic myeloid leukemia K562, and human hepatocellular carcinoma HepG2 was carried out. The most active compound 4 with an IC50 value of 9.7 μM against HepG2 cells was selected to examine the cytotoxic mechanism, which induced the apoptosis and arrested the HepG2 cell cycle at S stage. The in vivo zebrafish experiments revealed that compound 4 had the property of inhibiting tumor proliferation and migration.

中文翻译：

卡氏菌叶中的二萜类化合物显示出细胞毒活性。

为了获得生物活性物质作为癌症的先导化合物或治疗剂而进行的植物化学研究导致从卡氏酵母属的叶子中获得了六种新的和两种已知的双氯丁烷二萜。使用NMR技术和电子圆二色性（ECD）计算阐明了它们的结构。随后对这些分离株进行了针对人肺癌A549，人宫颈癌HeLa，人慢性髓细胞性白血病K562和人肝细胞癌HepG2的生物学细胞毒性评估。选择最具活性的化合物4对HepG2细胞的IC50值为9.7μM，以检查其细胞毒性机制，该机制诱导细胞凋亡并在S期停止HepG2细胞周期。体内斑马鱼实验表明，化合物4具有抑制肿瘤增殖和迁移的特性。

更新日期：2020-03-09

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