Page 32 - I. Chemical biology and drug discovery

[I. Chemical biology and drug discovery-17]

Antileukemic activities of ampelopsin in human leukemia

HL60 and K562 cells

Hong Lae Kim¹, Jang Mi Han¹˙#, Hye Jin Jung¹˙*

¹Pharmaceutical Engineering & Biotechnology, Sun Moon University, Asan 31460, Korea

Leukemia is a type of cancer of blood, which is caused by the rapid proliferation of abnormal white blood cells.
Although chemo/radiotherapies are used in the treatment of leukemia, the morbidity and mortality of leukemia
patients are still high. Ampelopsin is a natural flavonoid that possesses multiple pharmacological functions. However,

the anticancer effect and action mechanism of ampelopsin on leukemia have not been identified. We here evaluated

the antileukemic effects of ampelopsin against acute promyelocytic HL60 and chronic myelogenous K562 leukemia
cells. Ampelopsin significantly reduced the viability of HL‑60 and K562 cells at the concentrations that did not show
cytotoxicity against normal cells. The compound induced cell cycle arrest at S phase and apoptosis in both leukemia

cells. The antileukemic effects of ampelopsin were associated with the activation of caspase‑9, caspase-3, and PARP,
as well as the decrease in ROS production. Furthermore, we investigated the effects of ampelopsin on PI3K/AKT,

MAPK, and NFkB signaling pathways. Notably, it exhibited more potent antileukemic activity in HL60 cells compared
to K562 cells. Therefore, our findings suggest that ampelopsin may represent a promising natural compound for

the development of antileukemia therapeutics.