LSD1 inhibitors from the roots of Pueraria lobata

Abstract

One new 6a,11a-dehydropterocarpan derivative, 6-O-methyl-anhydrotuberosin (1), one new 6a-hydroxypterocarpan, (6aR,11aR,11bR)-hydroxytuberosone (7), and seven known compounds including two 6a,11a-dehydropterocarpans (2 and 4), two coumestans (3 and 5), one isoflavonoid (6) and two other phenolic compounds (8 and 9) were isolated from the roots of Pueraria lobata. The structures of the isolated compounds were elucidated with spectroscopic and spectrometric methods (1 D and 2DNMR, HRESIMS). Compounds 1, 2, 4–5 showed potent LSD1 inhibitory activities with IC₅₀ values ranging from 1.73 to 4.99 μM. Furthermore, compound 2 showed potent cytotoxicity against gastric cancer cell lines MGC-803 and BGC-823, and lung cancer cell lines H1299 and H460.

Graphical Abstract

Keywords:

• Pueraria lobata
• pterocarpan
• LSD1 inhibitors
• isoflavonoid

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

We acknowledge the financial support from the Key Projects for Science and Technology Development of Henan Province, China (NO. 182102310288, NO. 212102310314), and the Doctoral Research Fund of Henan University of Chinese Medicine (NO. BSJJ2018-19, NO. 00104311-2019-7).