Artematrovirenins A-P, guaiane-type sesquiterpenoids with cytotoxicities against two hepatoma cell lines from Artemisia atrovirens
| Autor: | Shuang Tang, Zhen Gao, Li-Hua Su, Yun-Bao Ma, Chang-An Geng, Ji-Jun Chen, Tian-Ze Li, Cheng Shen, Xue-Mei Zhang, Xiao-Yan Huang, Xin Zhang, Jing Hu |
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| Rok vydání: | 2021 |
| Předmět: |
Stereochemistry
Cell Survival 01 natural sciences Biochemistry Sesquiterpenes Guaiane Structure-Activity Relationship Cell Line Tumor Drug Discovery Ic50 values Humans Cytotoxicity Molecular Biology Density Functional Theory Cell Proliferation Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Chemistry Organic Chemistry Huh7 cell Artemisia atrovirens Antineoplastic Agents Phytogenic 0104 chemical sciences 010404 medicinal & biomolecular chemistry Artemisia Hepg2 cells Drug Screening Assays Antitumor Hepatoma cell Sesquiterpenes |
| Zdroj: | Bioorganic chemistry. 114 |
| ISSN: | 1090-2120 |
| Popis: | Random screening revealed that the EtOH extract of Artemisia atrovirens showed significant cytotoxicity against two human hepatoma cell lines (HepG2 and Huh7) with the inhibitory ratio of 98.9% and 99.7% at the concentration of 100 μg/mL. Further bioactivity-guided isolation of active fraction led to 16 new guaiane-type sesquiterpenoids, artematrovirenins A–P (1–16). Their structures were elucidated by extensive spectroscopic data. The absolute stereochemistry of compounds 1 and 14 was determined by single-crystal X-ray diffraction analyses. Pharmacological evaluation suggested that five compounds (3, 5, 8, 10, and 15) exhibited cytotoxicity, compounds 3 and 5 displayed cytotoxicity against HepG2 cell line with an IC50 values of 8.0 and 16.0 μM, as well as against Huh7 cell line with values of 18.2 and 32.2 μM. |
| Databáze: | OpenAIRE |
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