Six polyacetylenes from Atractylodes macrocephala Koidz and their anti-colon cancer activity

Abstract

Six undescribed polyacetylenes Atracetylenes A-F (1-6) and three known ones (7-9) were isolated from the rhizomes of Atractylodes macrocephala Koidz.. The comprehensive interpretation of NMR, HR-ESI-MS, DP4+ calculations, and electronic circular dichroism (ECD) calculations resulted in the elucidation of their structures and absolute configurations. The anti-colon cancer activities of (1-9) were evaluated by assaying the cytotoxicity and apoptosis on CT-26 cell lines. Notably, 5 (IC₅₀ 17.51 ± 1.41 μM) and 7 (IC₅₀ 18.58 ± 1.37 μM) exhibited significant cytotoxicity, and polyacetylenes 3-6 showed excellent abilities to promote apoptosis of CT-26 cell lines by Annexin V-FITC/PI assay. The results demonstrated that the polyacetylenes in A. macrocephala may be prospective for the treatment of colorectal cancer.

Keywords: Atracetylenes A-F; Atractylodes macrocephala Koidz.; CT-26 cell lines; Cytotoxicity, apoptosis; Polyacetylenes.