Crystal Structure of Taxinine A

Here reported is the crystal structure of taxinine A (C_(26)H_(36)O_8, Mr=476.76) which was isolated from the needles of Taxus cuspidata. The crystal belongs to monoclinic system, space group is P2_1 with a=9. 122 (2), b=10.451 (3), c=13.661(2),β=93. 92(1)°,Z=2, V=1299.3(5), D_x=1.218 g/cm￣3, F (000)=512,μ=0.08 mm-1, and the final R-factors are 0. 061 (Rf) and 0. 056(Rw) for 1796 observed diffractions. The molecule taxinine A is one of the taxane diterpenoids which possesses 6-8-6 fused tricycle skeleton.

MDR逆转活性紫杉烷类化合物的合成

目的:合成天然产物taxinine NN-3和taxinine NN-14,研究其对肿瘤细胞的多药耐药逆转活性。方法:以紫杉宁为出发原料,通过选择性水解9,10位的乙酰氧基,制成原乙酸酯后再水解。结果:以紫杉宁为原料经过3步反应,可以同时获得taxinine NN-3,taxinine NN-4两种天然产物,其中taxinine NN-3的收率为25%,taxinine NN-4的收率为68%。结论:高收率地合成了taxinine NN-3和taxinine NN-14。

紫杉烷类多药耐药逆转剂的合成及其逆转耐药活性

目的 设计合成一系列新型紫杉烷类化合物并进行逆转多药耐药肿瘤细胞耐药活性的筛选。方法 以本所生物合成的紫杉烷 ,SinenxanA为原料 ,合成了 1 0个 (I1～ 7,II1 ,2 ,III)新的紫杉烷类化合物 ,其结构经FABMS ,2DNMR确证 ,并对多药耐药癌细胞进行了逆转耐药性的试验。结果 9个 (I2～ 7,II1 ,2 ,III)化合物对多药耐药的人口腔上皮癌细胞KB V2 0 0 ,能够显著逆转其耐药性 ,增强抗癌药的活性 ,其中化合物I2 ,I3 ,I4逆转活性明显好于已知对照药Verapamil。结论 紫杉烷类化合物作为多药耐药逆转剂有较好的逆转耐药活性 。

Taxoids from the Needles of Taxus×media Hicksii

A new taxane diterpenoid, named 7-deacetoxy taxinine J, together with ten knowncompounds were isolated from the needles of Taxus × media Hickiii. The structures of allcompounds were elucidated and identified by spectroscopic methods. T'he structure of 7-deacetoxytaxinine J was further confirmed by X-ray crystallographic analysis. The structure of the knowncompound, taxinine E, was also revised.