Melognine, a novel monoterpenoid indole alkaloid from Melodinus fusiformis that induce apoptosis in BT549 cells

Abstract

A novel monoterpenoid indole alkaloid, melognine (1) possessing an unprecedented skeleton with a 6/6/5/5/6/6 hexatomic rearranged ring system was isolated from the stems of Melodinus fusiformis. The structure with absolute configuration of 1 was established by extensive spectroscopic analyses and quantum ECD calculations. Melognine showed significant cytotoxicity on human breast cancer BT549 cells with an IC₅₀ value of 1.49 μM by MTT assay. Further mechanism of action study indicated that melognine demonstrated the ability to induce apoptosis by activation of caspase-3 and p53, and downregulation of Bcl-2 in BT549 cells.

Graphical Abstract

Keywords:

• Melodinus fusiformis
• monoterpenoid indole alkaloid
• cytotoxicity
• apoptosis

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This research was funded by Natural Science Foundation of China (21772065), Shandong Provincial Natural Science Foundation (ZR2017MH019), and Shandong Provincial Key Research Project (2018GSF118158, 2017GSF19111).