Baccatin III is an important precursor for the synthesis of clinically important anticancer drug Taxol. Previously, we have characterized a key enzyme of 10-deacetylbaccatin III-10-β-O-acetyltransferase (DBAT) which catalyses the 10-deacetylbaccatin III into baccatin III in taxol biosynthesis. Here, in the present study, we have evaluated and compared the cytotoxic properties of the enzymatically synthesized baccatin III (ESB III) with standard baccatin III in different human cancer cell lines, namely human cervical cancer (HeLa), human lung cancer (A549), human skin cancer (A431) and human liver cancer cells (HepG2). Among the various cancer lines tested, HeLa was more susceptible to ESB III with IC₅₀ of 4.30 µM while IC₅₀ values for A549, A431 and HepG2 ranged from 4 to 7.81 µM. Further, it showed G2/M phase cell cycle arrest, production of reactive oxygen species and depolarised mitochondrial membrane potential. In addition, annexin V-FITC staining was performed which showed the apoptotic cell death of HeLa cells, when treated with ESB III. Hence, ESB III was capable to show anticancer activities by inducing apoptotic cell death which could further be used for the semisynthesis of taxol in future.

浆果赤霉素 III 是合成具有临床意义的抗癌药物紫杉醇的重要前体。之前，我们已经表征了 10-脱乙酰浆果赤霉素 III-10-β- O-乙酰转移酶 (DBAT)的关键酶，该酶在紫杉醇生物合成中将 10-脱乙酰浆果赤霉素 III 催化为浆果赤霉素 III。在这里，在本研究中，我们评估并比较了酶合成的浆果赤霉素 III (ESB III) 与标准浆果赤霉素 III 在不同人类癌细胞系中的细胞毒性特性，即人类宫颈癌 (HeLa)、人类肺癌 (A549) 、人类皮肤癌 (A431) 和人类肝癌细胞 (HepG2)。在测试的各种癌症系中，HeLa 对 ESB III 更敏感，IC ₅₀为 4.30 µM，而 IC ₅₀A549、A431 和 HepG2 的值范围为 4 到 7.81 µM。此外，它显示了 G2/M 期细胞周期停滞、活性氧的产生和去极化的线粒体膜电位。此外，进行了膜联蛋白 V-FITC 染色，显示了当用 ESB III 处理时 HeLa 细胞的凋亡细胞死亡。因此，ESB III 能够通过诱导凋亡细胞死亡来显示抗癌活性，这可以进一步用于未来紫杉醇的半合成。