Department of Pharmacy, Chengdu Seventh People's Hospital, Chengdu, 610213, Sichuan, China.
Department of Pharmacy, Clinical Medical College & Affiliated Hospital of Chengdu University, Chengdu, 610081, Sichuan, China.
Arch Pharm Res. 2022 Aug;45(8):535-557. doi: 10.1007/s12272-022-01397-z. Epub 2022 Jul 31.
Cancer, which is a leading cause of deaths around the world, is characterized by genetic mutations and epigenetic changes. Baicalin and its aglycone baicalein, the major bioactive flavones derived from the dried root of Scutellaria baicalensis Georigi, belong to flavonoid compounds. Many studies demonstrated that both of them exhibited remarkable promising anticancer activities. This study summarized potential anticancer mechanisms of baicalin and baicalein including induction of apoptosis, initiation of cell cycle arrest, suppression of metastasis, induction of autophagy, and regulation of immunity. Combination strategies involving baicalin or baicalein as chemotherapeutic adjuvants, clinical trial and safety were also discussed. In addition, we compared the difference in their anticancer effects. Interestingly, baicalein showed quicker and stronger inhibitory effects on multiple cancers than those of baicalin, probably due to its smaller size and high lipophilicity which contribute to fast absorption and improve ability to penetrate cells. Taken together, both baicalin and baicalein are effective in treating cancer with good tolerance. However, deglycosylation of baicalin to baicalein was found to have stronger anticancer potential.
癌症是全球主要死因之一，其特征为基因突变和表观遗传改变。黄芩苷及其苷元黄芩素是从黄芩的干燥根中提取的主要生物活性黄酮类化合物，属于黄酮类化合物。许多研究表明，它们都具有显著的抗肿瘤活性。本研究总结了黄芩苷和黄芩素的潜在抗肿瘤机制，包括诱导细胞凋亡、启动细胞周期停滞、抑制转移、诱导自噬和调节免疫。还讨论了涉及黄芩苷或黄芩素作为化疗辅助剂的联合策略、临床试验和安全性。此外，我们比较了它们在抗肿瘤作用方面的差异。有趣的是，黄芩素对多种癌症的抑制作用比黄芩苷更快、更强，这可能是由于其体积更小、亲脂性更高，有助于快速吸收和提高细胞穿透能力。总之，黄芩苷和黄芩素在治疗癌症方面都有效，且具有良好的耐受性。然而，已发现黄芩苷的去糖基化生成黄芩素具有更强的抗肿瘤潜力。
