Cytotoxic pterosins from Pteris multifida roots against HCT116 human colon cancer cells

  • Bioorg Med Chem Lett. 2017 Jul 15;27(14):3144-3147. doi: 10.1016/j.bmcl.2017.05.034.
Jung Wha Kim  1 Hong Pyo Kim  2 Sang Hyun Sung  3
Affiliations
  • 1. College of Pharmacy and Research Institute of Pharmaceutical Science, Seoul National University, Seoul 08826, Republic of Korea.
  • 2. College of Pharmacy, Ajou University, Suwon 16499, Republic of Korea.
  • 3. College of Pharmacy and Research Institute of Pharmaceutical Science, Seoul National University, Seoul 08826, Republic of Korea. Electronic address: [email protected].
Abstract

Two new pterosin glycosides, (2S,3S)-pterosin C 3-O-β-d-(4'-(E)-caffeoyl)-glucopyranoside (1) and (2S,3S)-pterosin C 3-O-β-d-(6'-(E)-p-coumaroyl)-glucopyranoside (2), were isolated from Pteris multifida (Pteridaceae) roots along with ten known pterosin compounds (3-12). The chemical structures of the isolated compounds were elucidated by extensive analysis of the 1D, 2D NMR, HRESIMS, and CD spectroscopic data. The cytotoxicities of 1-12 against HCT116 human colorectal Cancer cell line were evaluated. Among the isolates, compound 1 showed moderate antiproliferative activity in HCT116 cells with an IC50 value of 8.0±1.7μM. Additionally, 1 induced the upregulation of the caspase-9 and procaspase-9 levels in Western blots and increased the annexin V/propidium iodide (PI)-positive cell population in flow cytometry.

Keywords
Cytotoxicity; HCT116 cells; Pteris multifida; Pterosin.