Ptehoosines A and B: Two new sesamin-type sesquilignans with antiangiogenic activity from Pterocephalus hookeri (C.B. Clarke) Höeck

Abstract Two undescribed sesamin-type sesquilignans ptehoosines A (1) and B (2), together with 4 known lignans (3–6), were isolated from Pterocephalus hookeri (C.B. Clarke) Hoeck which was widely used as traditional Tibetan medicine for treatment of rheumatoid arthritis. Their structures were determined by HR-ESI-MS, NMR analysis and CD experiment. The in vitro antiangiogenic effect of all isolated compounds against human umbilical vein endothelial cells (HUVECs) were evaluated by CCK-8 assay. Among them, compound 1 exhibited significant proliferative inhibition on HUVECs with IC50 value of 32.82 ± 0.99 μM. Further in vitro study indicated 1 could arrest cell cycle at G0/G1 phase and reduce the migration of HUVECs. In vivo experiment exhibited 1 could inhibit tail vessels plexus in zebrafish. The above finding suggested that 1 was a promising lead compound against RA by inhibiting of angiogenesis.