Studies On The Biotransformation Of Taxoids And Biosynthesis Of Chiral Pharmaceutical L-3-n-butylphthalide

In this thesis, we report the studies on the biotransformation of taxoids and biosynthesis of chiral pharmaceutical 1-3-n-butylphthalide.The studies on the biotransformation of taxoids mainly included the following:1. Studies on the biotransformation of sinenxan ASinenxan A was converted to 108-hydroxy-2a, 5a, 14β-triacetoxy-4(20), 11-taxadiene [10-deacetyl sinenxan A] about in 17% yield by Fusarium equiseti (Corda) Sacc.2. Biotransformation of 14-deacetoxyl sinenxan A by Ginkgo cell suspensioncultures14-Deacetoxyl sinenxan A [2a, 5a, 10β-triacetoxy-4(20), 11-taxadiene] wasconverted to two new products, 106-hydroxy-2a,5a-diacetoxy- 4(20), 11-taxadiene (I) and 10β-butyloxy-2a,5a-diacetoxy-4(20),ll-taxadiene( II) both about in 19% yields by Ginkgo cell suspension cultures. Their structures were identified on the basis of their chemical and spectroscopic data. The three compounds were evaluated for their in vitro cytotoxic activities against two solid tumor cell lines and their drug-resistant counterparts (KB and KB/V, MCF-7 and MCF-7/ADR), and the decreased activities were observed in the case of the two products.The studies on the biosynthesis of chiral pharmaceutical 1-3-n-butylphthalide mainly included the following:1. Analysis of the components in callus and cell suspension cultures of Ligusticum chuanxiong Hort. by gas chromatography-mass spectrometryMedia for initiation of callus cultures consisted of MS medium supplemented with 30 g/L sucrose, 8 g/L agar, 1.0 mg/L 2,4-D, and 0.5mg/L CTK.The callus cultures were grown on MS media supplemented as above except without CTK. Callus was grown in the dark at 25 °C and subcultured every 35 days by transferring 5 g (fresh weight) of callus to 100 mL of fresh medium in 250 mL Erlenmeyer flasks. Media for initiation of suspension cultures consisted of MS media supplemented as above except without CTK...