Study on biological activities of a naturally occurring flavone, Factor-X

麦黄酮（4′，5，7-trihydroxy-3′，5′-dimethoxyflavone，4 ′，5 ′-trihydroxy-3 ′，5′-dimethoxyflavone，4 ′，5 ′-trihydroxy-3 ′，5′-dimethoxyflavone）是一种天然黄酮类化合物，具有抗炎作用，并具有多种生物学活性，包括对多种人癌细胞系的抑制作用和对小鼠胃肠道肿瘤的化学预防作用。本研究旨在研究麦黄酮对肝星状细胞（hepatic stellate cells，HSC）的生物学作用，探讨其作为肝纤维化治疗药物的潜力，因为HSC增殖与慢性肝病导致不可逆肝硬化和肝细胞癌的肝纤维化进展密切相关。麦黄酮抑制血小板衍生生长因子（PDGF）-BB诱导的细胞增殖，通过阻断细胞周期的进展和细胞迁移的人HSC株LI 90和培养活化的HSC。它还降低了PDGF受体及其下游信号分子ERK 1/2和Akt的磷酸化，这可能是由于其酪氨酸激酶抑制剂性质，而不是抑制PDGF-BB与其受体之间的直接结合。我们的研究结果表明，麦黄酮可能是有益的HSC靶向治疗或化学预防应用肝纤维化。

Tricin(4′, 5, 7-trihydroxy-3′, 5′-dimethoxyflavone), a naturally occurring flavone, has anti-inflammatory potential and exhibits diverse biological activities including antigrowth activity in several human cancer cell lines and cancer chemopreventive effects in the gastrointestinal tract of mice. The present study aimed to investigate the biological actions of tricin on hepatic stellate cells(HSCs) in vitro, exploring its potential as a treatment of liver fibrosis, since HSC proliferation is closely related to the progression of hepatic fibrogenesis in chronic liver diseases leading to irreversible liver cirrhosis and hepatocellular carcinoma. Tricin inhibited platelet-derived growth factor(PDGF)-BB-induced cell-proliferation by blocking cell cycle progression and cell migration in the human HSC line LI90 and culture-activated HSCs. It also reduced the phosphorylation of PDGF receptor and the downstream signaling molecules ERK1/2 and Akt, which might be due to its tyrosine kinase inhibitor properties rather than inhibition of the direct binding between PDGF-BB and its receptor. Our findings suggest that tricin might be beneficial in HSC-targeting therapeutic or chemopreventive applications for hepatic fibrosis.