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作者于1968年在从事墨西哥湾的海洋生物Bu-gula neritina L.的研究中,分离得抗癌成分——藓苔抑制素1(Bryostatin 1),对小鼠P 388淋巴白血病剂量为10～70μ/kg时,存活期延长52～96%;体外对P 388的EDS_(50)为0.89μg/ml。本文报道其化学结构的测定。500公斤湿重的生物用二氯甲烷萃取后,通过溶剂分配和Sephadex LH-20及硅胶柱层析纯化,收集生物活性部分。于二氯甲烷-甲醇中重结晶,得藓苔抑制素1的结晶。熔点:230～235℃,[α]_D~(25)+34.1°(甲醇),FAB质谱测定分子量为904。通过波谱及晶体X-射线衍射分析,确定其化学结构如下图所示。
In 1968, in the study of Bu-gula neritina L., a marine organism in the Gulf of Mexico, the anti-cancer component Bryostatin 1 was isolated and the dose of P 388 lymphoid leukemia was 10-70 μ / kg, the survival period extended 52-96%; in vitro P 388 EDS_ (50) 0.89μg / ml. This article reports the determination of its chemical structure. 500 kg wet weight of organism was extracted with dichloromethane and purified by solvent partitioning and Sephadex LH-20 and silica gel column chromatography to collect bioactive fractions. Recrystallization from methylene chloride-methanol gave mossostatin 1 crystals. Melting point: 230-235 ° C, [α] D 25 + 34.1 ° (methanol), FAB mass spectrum 904. By spectroscopy and crystal X-ray diffraction analysis to determine the chemical structure as shown below.