Gong Wei-Yi, Zhao Zheng-Xiao, Liu Bao-Jun, Lu Lin-Wei, Dong Jing-Cheng
The Department of Integrative Medicine, Huashan Hospital, Fudan University, 12 Middle Wulumiqi Road, Shanghai, PR China; The Institutes of Integrative Medicine of Fudan University, 12 Middle Wulumuqi Road, Shanghai, PR China.
The Department of Integrative Medicine, Huashan Hospital, Fudan University, 12 Middle Wulumiqi Road, Shanghai, PR China; The Institutes of Integrative Medicine of Fudan University, 12 Middle Wulumuqi Road, Shanghai, PR China.
Eur J Med Chem. 2017 Jan 27;126:844-852. doi: 10.1016/j.ejmech.2016.11.058. Epub 2016 Dec 1.
Solid tumors contain a huge mass of malignant tumors other than hematological malignancies. Novel therapies based on bio-safe agents against solid tumors are urgently required. Baicalin and its aglycone baicalein, the major bioactive flavones derived from Scutellaria baicalensis, have potential roles in the management of cancer. The chemopreventive properties governed by baicalin and baicalein were multi-fold, via apoptosis induction, autophagy triggering, cell cycle arrest, inhibition of 12-lipoxygenase and metastasis suppression. However, their poor solubility and low oral bioavailability severely limited the clinical application. This extensive review focused on the promising anti-cancer activities of baicalin and baicalein and new techniques to improve their bioavailability.
实体瘤包含大量除血液系统恶性肿瘤之外的恶性肿瘤。迫切需要基于生物安全制剂的实体瘤新疗法。黄芩苷及其苷元黄芩素是从黄芩中提取的主要生物活性黄酮类化合物，在癌症治疗中具有潜在作用。黄芩苷和黄芩素所具有的化学预防特性是多方面的，包括诱导细胞凋亡、触发自噬、使细胞周期停滞、抑制12-脂氧合酶以及抑制转移。然而，它们的低溶解度和低口服生物利用度严重限制了其临床应用。这篇全面的综述聚焦于黄芩苷和黄芩素颇具前景的抗癌活性以及提高其生物利用度的新技术。
