Diterpenoids from the leaves of Casearia kurzii showing cytotoxic activities

  • Liang, Yue
  • Zhang, Qi
  • Yang, Xueyuan
  • Li, Ying
  • Zhang, Xuke
  • ... Lee, Dongho
  • 외 10명
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초록

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 mu M 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.

키워드

Zebrafish xenograft modelCytotoxic activitiesApoptosisCell cycleClerodane diterpenoidsCasearia kurziiBIOACTIVE CLERODANE DITERPENOIDSAPOPTOSIS INDUCERSDERIVATIVESROOTSSYLVESTRISPRODUCTSGROWTHCELLSTWIGS
제목
Diterpenoids from the leaves of Casearia kurzii showing cytotoxic activities
저자
Liang, YueZhang, QiYang, XueyuanLi, YingZhang, XukeLi, YuhaoDu, QingJin, Da-QingCui, JianlinLall, NamritaTuerhong, MuhetaerLee, DonghoAbudukeremu, MuniraXu, JingShuai, LingGuo, Yuanqiang
DOI
10.1016/j.bioorg.2020.103741
발행일
2020-05
유형
Article
저널명
Bioorganic Chemistry
98