Theasaponin E₁ (TSE₁) has been suggested to have higher biological activity than other saponins present in tea seed. Saponins have recently been considered as a potential chemotherapeutic agent for treating cancer. We examined the anti-angiogenic and anti-obesity properties of TSE₁ contributing to anti-cancer efficacy. Treating with a 10 μg/mL concentration of TSE₁ completely inhibited tube formation in human umbilical vein endothelial cells (HUVECs). TSE₁ showed toxicity toward cancer cells and inhibited in vivo growth of the tumor. The vascular endothelial growth factor (VEGF) receptor complex was suppressed, leading to the inhibition of protein kinase B (Akt) expression and down-regulation of nuclear factor-kappa B (NF-kB) activation. The differentiating 3T3-L₁ cells treated with TSE₁ had decreased lipid droplet formation measured by Oil Red O staining. Reduced weight was measured in mice fed with a TSE₁ plus high-fat diet. The results taken together, and particularly the NF-kB inhibition, suggest that TSE₁ may have multi-target action for treating cancer as a novel chemotherapeutic agent.
Keywords: NF-kB; VEGF; anti-angiogenesis; anti-obesity; theasaponin E1.