2. Academic Validation
  3. Chemical modifications of ergostane-type triterpenoids from Antrodia camphorata and their cytotoxic activities

Chemical modifications of ergostane-type triterpenoids from Antrodia camphorata and their cytotoxic activities

  • Bioorg Med Chem Lett. 2021 Jul 1:43:128066. doi: 10.1016/j.bmcl.2021.128066.
Bin Li 1,  Yi Kuang 2,  Yang Yi 2,  Xue Qiao 2,  Lei Liang 3,  Min Ye 4
Affiliations

Affiliations

  • 1 State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing 100191, China; Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100193, China.
  • 2 State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing 100191, China.
  • 3 State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing 100191, China. Electronic address: leiliang@bjmu.edu.cn.
  • 4 State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing 100191, China. Electronic address: yemin@bjmu.edu.cn.
PMID: 33915258 DOI: 10.1016/j.bmcl.2021.128066
Abstract

In order to discover potential antitumor agents from Natural Products, chemical modifications of ergostane-type triterpenoids from Antrodia camphorata yielded ten new compounds. They include nine C-26 amide derivatives of antcin G (1) and a methyl antcin B (4) derivative with hydroxyamino groups at C-3 and C-7. Chemical structures of the new compounds were elucidated by NMR and MS analyses. Furthermore, cytotoxicities of the triterpenoid derivatives were evaluated using four human Cancer cell lines (HL60, U251, SW480, and MCF-7). As a result, 1a, 1g, and 4a exhibited potent cytotoxic activities against HL60, U251, and SW480 with IC50 values of 0.7 ± 0.9, 2.9 ± 1.3, and 2.2 ± 0.6 μM, respectively. Molecular docking indicates that 1a, 1g, and 4a have strong binding affinity with DNA Topoisomerase IIα (-9.3, -7.9, and -7.4 kcal/mol, respectively), and that they could be potent Topoisomerase IIα inhibitors.

Keywords

Antrodia camphorata; Chemical modification; Cytotoxicity; DNA topoisomerase IIα; Ergostane-type triterpenoid.

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