摘要
目的:对采自我国南海的蓖麻海绵Biemna fortis Topsent的化学成分进行研究,从中寻找有生物活性的次生代谢产物。方法:用硅胶柱层析和凝胶柱层析对蓖麻海绵的甲醇提取物进行分离纯化,根据其化学性质,结合现代波谱技术(MS,NMR等),对得到的化合物进行结构鉴定。结果:分离得到9个甾体、2个邻苯二甲酸酯、1个长链脂肪醛类化合物,其结构分别鉴定为melithasterol B(1),(24R)-ergosta-7,22-diene-3,5,6-triol(2),(24R)-er-gosta-4,6,8(14),22-tetraene-3-one(3),(24R)-ergosta-4,7,22-triene-3-one(4),(24R)-ergosta-6,22-diene-5,8-epidioxy-3-ol(5),6-hydroxy-cholest-4-en-3-one(6),cholest-4-ene-3,6-dione(7),cholest-4-en-3-one(8),cholest-5,22-diene-3-one(9),bis-(2-ethylhexyl)phthalate(10),bis-diisobutyl phthalate(11)和hexaldehyde(12)。结论:化合物1-4,6-10,12系首次从蓖麻海绵中分离得到;化合物7不但对T和B淋巴细胞的增殖具有显著抑制活性,而且对II型糖尿病靶标分子蛋白质酪氨酸磷酸酯酶PTP1B具有显著的抑制活性,其IC50为1.6mol·L1。
AIM： To study the chemical constituents of the South China Sea sponge Biemnafortis to search for new bioactive substances. METHODS： The methanol extract of Biemnafortis Topsent was subjected to repeated silica gel column chromatographies to afford thirteen pure compounds （1-12）, the structures of which were elucidated on the basis of detailed spectroscopic analysis and comparison with the data reported in the literature. RESULTS： Twelve known compounds were isolated and identified as melithasterol B （1）, （24R）-ergosta-7,22-diene-3,5,6-triol （2）, （24R）-ergosta-4,6,8（14）, 22-tetraene-3-one （3）, （24R）-crgosta-4,7,22-triene-3-one （4）, （24R）-ergosta-6,22-diene-5,8-epidioxy-3-ol （5）, 6-hydroxy-cho-lest-4-en-3-one （6）, cholest-4-ene-3,6-dione （7）, cholest-4-en-3-one （8）, cholest-5,22-diene-3-one （9）, bis-（2-ethylhexyl） phthalate （10）, bis-diisobutyl phthalate （11） and hexaldehyde （12）, respectively. CONCLUSION： Compounds 1-4, 5-10 and 12 were isolated from the examined sample for the first time. 7 exhibited significant T and B lymphocytes proliferation in- hibitory activity and significant hPTP1B inhibitory activity with IC50 1.6 mol·L^-1.
出处
《中国天然药物》
SCIE
CAS
CSCD
2008年第5期348-353,共6页
基金
国家海洋863计划(Nos.2006AA09Z447
2006AA09Z412 & 2007AA09Z447)
国家自然基金委 (Nos.20572116
30730108 & 20721003)
上海市科委基础研究 (Nos.07XD14036 & 06DZ22028)
中国科学院重点项目(KSCX2-YW-R-18)资助项目~~
