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Compounds from Toddalia asiatica: Immunosuppressant Activity and Absolute Configurations
Journal of Natural Products ( IF 3.3 ) Pub Date : 2020-10-01 , DOI: 10.1021/acs.jnatprod.0c00564 Jakob K Reinhardt 1 , Amy M Zimmermann-Klemd 2 , Ombeline Danton 1 , Martin Smieško 3 , Carsten Gründemann 3 , Matthias Hamburger 1
Journal of Natural Products ( IF 3.3 ) Pub Date : 2020-10-01 , DOI: 10.1021/acs.jnatprod.0c00564 Jakob K Reinhardt 1 , Amy M Zimmermann-Klemd 2 , Ombeline Danton 1 , Martin Smieško 3 , Carsten Gründemann 3 , Matthias Hamburger 1
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In a screening of an extract library from plants used in Traditional Chinese Medicine the MeOH extract of Toddalia asiatica inhibited proliferation of human primary T cells with an IC50 of 25.8 μg/mL. Activity in the extract was tracked by HPLC activity profiling, and a total of 15 compounds were characterized. Three compounds, toddalic acid (6) and both enantiomers (7a and 7b) of toddanolic acid (7), were new natural products, and two recently published compounds, (2′R)-toddalolactone 3′-O-β-d-glucopyranoside (10) and (2′S)-toddalolactone 2′-O-β-d-glucopyranoside (11), were described in detail for the first time. The absolute configurations of compounds 8, 9, 10, 12, 13, and 15 were determined by comparison of experimental and calculated ECD spectra. For glucosides 9 and 10, ECD data and chiral-phase HPLC of the aglycones after enzymatic hydrolysis confirmed the results. Nitidine chloride (4) inhibited proliferation of primary human T cells with an IC50 of 0.4 μM.
中文翻译：
来自 Toddalia asiatica 的化合物：免疫抑制剂活性和绝对构型
在对用于中药的植物提取物文库的筛选中，积雪草的甲醇提取物抑制人原代 T 细胞的增殖，IC 50为 25.8 μg/mL。通过 HPLC 活性分析跟踪提取物中的活性，并表征了总共 15 种化合物。三种化合物，toddalic酸（6）和两种对映体（图7a和图7b toddanolic酸（的）7），为新天然产物，和两个最近发表的化合物，（2' - [R）-toddalolactone 3'- ö -β- d -吡喃葡萄糖苷 ( 10 ) 和 (2' S )-toddalolactone 2'-O- β- d-吡喃葡萄糖苷( 11 )，首次被详细描述。化合物的绝对构型8，9，10，12，13，和15是由实验的比较和计算的ECD谱确定。对于糖苷9和10，酶水解后苷元的 ECD 数据和手性相 HPLC 证实了结果。Nitidine chloride ( 4 ) 抑制原代人类 T 细胞的增殖，IC 50为 0.4 μM。
更新日期：2020-10-26
中文翻译：
来自 Toddalia asiatica 的化合物：免疫抑制剂活性和绝对构型
在对用于中药的植物提取物文库的筛选中，积雪草的甲醇提取物抑制人原代 T 细胞的增殖，IC 50为 25.8 μg/mL。通过 HPLC 活性分析跟踪提取物中的活性，并表征了总共 15 种化合物。三种化合物，toddalic酸（6）和两种对映体（图7a和图7b toddanolic酸（的）7），为新天然产物，和两个最近发表的化合物，（2' - [R）-toddalolactone 3'- ö -β- d -吡喃葡萄糖苷 ( 10 ) 和 (2' S )-toddalolactone 2'-O- β- d-吡喃葡萄糖苷( 11 )，首次被详细描述。化合物的绝对构型8，9，10，12，13，和15是由实验的比较和计算的ECD谱确定。对于糖苷9和10，酶水解后苷元的 ECD 数据和手性相 HPLC 证实了结果。Nitidine chloride ( 4 ) 抑制原代人类 T 细胞的增殖，IC 50为 0.4 μM。
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