Structure modification and anti-tumor activity evaluation on sesquiterpene lactones TBA and TBB from Sphagneticola trilobata

Abstract

Thirteen sesquiterpene lactone derivatives were designed and synthesised using the sesquiterpene lactone epimers TBA and TBB as the parent molecules, isolated from Sphagneticola trilobata. Their structures were elucidated by extensive spectroscopic studies and chemical evidence. Furthermore, the structures of 1a, 4b and 5a were confirmed by X-ray single-crystal diffraction analyses. All of the compounds were further examined for their in vitro antiproliferative activity against human cancer cell lines HeLa and MCF-7. Unfortunately, the activity of all derivatives were weaker than that of the parental compounds.

Graphical Abstract

Keywords:

• Sesquiterpene lactones
• chemical synthesis
• anticancer activity

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was supported by the National Natural Science Foundation of China (22167013), the Key Project of Research and Development of Hainan Province (ZDYF2021SHFZ221), the Specific Research Fund of the Innovation Platform for Academicians of Hainan Province (YSPTZX202030), the Program for Hainan Provincial Graduate Innovation Research Project (Qhyb2021-44), and the Innovation Training Program for College Students (Nos. S20211165800; 202111658004).