Luteolin (Luteolol) belongs to the flavonoid group of natural products and is a Nrf2 inhibitor, PDE inhibitor. Luteolin has a wide range of biological activities including antitumor, antioxidant, anti-inflammatory, antimicrobial, antiviral, antiallergic, and procoagulant.

PDE5:9.5 μM(Ki), PDE1:15.0 μM(Ki), PDE3:13.9 μM(Ki), PDE2:6.4 μM(Ki), PDE4:11.1 μM(Ki)

METHODS: ESCC cell lines EC1, EC9706, KYSE30 and KYSE450 were treated with Luteolin (10-80 µM) for 48-72 h. Cell viability was measured using the CCK-8 Assay.
RESULTS: Luteolin inhibited the growth of ESCC cell lines in a dose-dependent manner with IC50 in the range of 20-60 µM. [1]
METHODS: Human cervical cancer cells, HeLa, were treated with Luteolin (5-20 µM) for 48 h. Cell cycle profiles were analyzed using Flow Cytometry.
RESULTS: Luteolin treatment blocked the cell cycle progression of HeLa cells in sub-G1 phase. [2]

METHODS: To detect anti-tumor activity in vivo, Luteolin (50 mg/kg) was injected intraperitoneally once daily for eighteen days into BALB/C-nu mice bearing ESCC tumor EC1.
RESULTS: The Luteolin treatment group showed a reduction in tumor size and a reduction in total tumor weight of about 65%. [1]
METHODS: To study the effect on intestinal mucositis, Luteolin (3-30 mg/kg in water plus 1% Tween) was administered by gavage or intraperitoneally to irinotecan-induced intestinal mucositis in Swiss mice once a day for fourteen days.
RESULTS: Luteolin prevented irinotecan-induced intestinal damage by reducing weight loss and diarrhea scores as well as attenuating duodenal and colonic shortening. [3]