补骨脂酚的体外抗肿瘤活性及其关键中间体的合成研究

In vitro antitumor activity and synthesis of the key intermediate of bakuchiol

摘要:
以他莫西芬为阳性对照物, 考察了补骨脂酚的体外抗人乳腺癌细胞株生物活性。生物活性测试结果表明补骨脂酚在低剂量下即有抑制人乳腺癌细胞增殖作用, 它对人乳腺癌细胞T-47D及MDA-MB-231的IC₅₀分别为2.89×10⁻⁵ mol·L⁻¹及8.29×10⁻³ mol·L⁻¹。另一方面, 本文以Ireland-Claisen重排为关键步骤, 在合成补骨脂酚所需的关键中间体时, 改进了常规Claisen重排反应的条件及试剂, 避免了有毒试剂的使用。

Abstract:
The in vitro antitumor activity of bakuchiol was exploited, compared with tamoxifen. The result of biological activities showed that bakuchiol could inhibit human breast cancer and the IC₅₀ values were 2.89×10⁻⁵ mol·L⁻¹ and 8.29×10⁻³ mol·L⁻¹ against the cells line T-47D and MDA-MB-231 respectively. On the other hand, the key intermediate to synthesize bakuchiol was obtained by the method of Ireland-Claisen rearrangement. Comparing with traditional Claisen rearrangement, the reaction conditions are milder and the reaction reagents are safer.