Clerodane Diterpenoids Isolated from the Leaves of Casearia graveolens

  • J Nat Prod. 2020 Jan 24;83(1):36-44. doi: 10.1021/acs.jnatprod.9b00515.
Feng Liu  1 ,  Jun Ma  1 ,  Zhaoyu Shi  1 ,  Qi Zhang  1 ,  Huimei Wang  1 ,  Dihua Li  2 ,  Zhaohui Song  3 ,  Chunyan Wang  4 ,  Jin Jin  1 ,  Jing Xu  1  5 ,  Muhetaer Tuerhong  6 ,  Munira Abudukeremu  6 ,  Ling Shuai  1 ,  Dongho Lee  7 ,  Yuanqiang Guo  1
Affiliations
  • 1. 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.
  • 2. 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.
  • 3. State Key Laboratory of Core Technology in Innovative Chinese Medicine , Tasly Pharmaceutical Group Co., Ltd. , Tianjin 300410 , People's Republic of China.
  • 4. Tianjin Second People's Hospital , Tianjin 300192 , People's Republic of China.
  • 5. State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources , Guangxi Normal University , Guilin 541004 , People's Republic of China.
  • 6. College of Chemistry and Environmental Sciences , Kashgar University , Kashgar 844000 , People's Republic of China.
  • 7. College of Life Sciences and Biotechnology , Korea University , Seoul 02841 , Republic of Korea.
Abstract

A phytochemical survey aiming to acquire pharmacologically active substances has resulted in the isolation of nine new clerodane Diterpenoids, named graveospenes A-I (1-9), from the leaves of Casearia graveolens. Spectroscopic methods were employed to establish the structures with their absolute configurations being confirmed by ECD data analysis. A biological evaluation was performed, and compound 1 was found to be cytotoxic to both human Lung Cancer cells (A549) and human hepatocellular carcinoma cells (HepG2). A mechanism-of-action study on 1 revealed this compound to induce Apoptosis of A549 cells and impede them at the G0/G1 stage.