Herba Hedyotis Diffusae (HD)), the whole herb of Hedyotis diffusa Willd, is a Chinese herbal medicine used for treating cancer.It is reported to have antineoplastic, antitoxic and immunoenhancing properties, and is also used in treating malignancies.A key hallmark of many cancers, particularly the most aggressive cancers, is the capacity to metabolize glucose at an elevated rate.After rapid entry of glucose into cancer cells on the glucose transporter, the highly glycolytic phenotype is supported by hexokinase (primarily RKⅡ) that is overexpressed and bound to the outer mitochondrial membrane.Via its mitochondrial location, HKⅡ, also suppresses the death of cancer cells by inhibiting cytochrome C release, thus increasing cancer cells possibility for metastasis and the ultimate death of the human host.We found that HD can target the keyenzyme, HKⅡ.After treatment with HD in Hela cells, the decrease of protein and mRNA levels of HKⅡ and induction of apoptosis were observed.The expression level reduction of HKⅡ attenuates HKⅡs ability of preventing apoptotic events and energy supply for cancer ceils.Thus, it is speculated that HD induces apoptosis through targeting HKⅡ in Hela cells.(Supported by a grant, FRG/06-07/Ⅱ-67, from Hong Kong Baptist University).