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目的设计并合成马铃薯三糖吉托皂苷(Ⅱ),研究先导化合物chlorogenin 3-O-β-chacotrioside(Ⅰ)苷元结构中不同C6-OH位点对目标化合物抑制H5N1假病毒活性的影响。方法采用逐步线性合成的策略,以3α-吉托皂苷类似物为起始原料,依次经酯化、氧化、还原、糖苷化、脱保护基等反应操作制备得到化合物Ⅱ;利用建立在细胞水平的H5N1假病毒活性检测方法测试了其抑制活性。结果目标化合物Ⅱ的总收率为20.9%,其化学结构经NMR、MS确证。结论将化合物Ⅰ结构中的6-羟基薯蓣皂苷元替换成吉托皂苷元可致抗病毒活性下降。
OBJECTIVE To design and synthesize potato triglyceride-based GITAS (Ⅱ) to study the effect of different C6-OH sites on the activity of target compounds against H5N1 pseudovirions in chlorogenin 3-O-β-chacotrioside (Ⅰ) aglycones. Methods The compound Ⅱ was prepared by stepwise linear synthetic method using 3α-Gatoside analogues as the starting material, followed by esterification, oxidation, reduction, glycosylation, deprotection and other reactions. H5N1 pseudovirus activity assay was tested for its inhibitory activity. Results The total yield of target compound Ⅱ was 20.9%. Its chemical structure was confirmed by NMR and MS. Conclusion Substitution of 6-hydroxy-diosgenin in compound I with ketosin can result in a decrease in antiviral activity.