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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Lanopylins A(1), A(2) and B-2, novel lanosterol synthase inhibitors from Streptomyces sp K99-5041
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Lanopylins A(1), A(2) and B-2, novel lanosterol synthase inhibitors from Streptomyces sp K99-5041

机译：Laneptylins A（1），A（2）和B-2，来自链霉菌K99-5041的新型羊毛甾醇合酶抑制剂

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From an actinomycete strain, Streptomyces sp. K99-5041, lanopylins A(1), B-1, A(2) and B-2 were isolated as new natural products that inhibited the reaction of recombinant human lanosterol synthase. The crude extract from the whole broth of this strain was fractionated by silica gel column chromatography to afford an active fraction that showed a single spot on TLC. Detailed analyses of this fraction with liquid chromatography-atmospheric pressure chemical ionization mass spectrometry revealed that it contained 20 homologous compounds with differing side chain lengths. The fraction was separated by preparative HPLC to afford four of these homologues, lanopylins A(1), B-1, A(2) and B-2. Detailed spectroscopic analyses of these isolated compounds,led to the identification of their structures. Lanopylins A(1) and B-1 were (3E)-isohexadecylmethylidene-2-methyl-1-pyrroline and (3E)-hexadecylmethylidene-2-methyl-1-pyrroline, respectively, and lanopylins A(2) and B-2 were homologues with the insertion of one cis-ethylenylidene in the side chain of lanopylins A, and B,, respectively. These compounds inhibited recombinant human lanosterol synthase with IC50 values of 15, 18, 33, and 41 mum, respectively. [References: 23]
机译：从放线菌菌株Streptomyces sp。分离出K99-5041，羊毛脂蛋白A（1），B-1，A（2）和B-2作为抑制重组人羊毛甾醇合酶反应的新天然产物。通过硅胶柱色谱分离该菌株全培养液的粗提物，得到在TLC上显示单点的活性部分。用液相色谱-大气压化学电离质谱法对该馏分进行的详细分析显示，该馏分包含20种具有不同侧链长度的同源化合物。通过制备型HPLC分离级分，得到这些同源物中的四个，羊毛脂蛋白A（1），B-1，A（2）和B-2。对这些分离的化合物进行了详细的光谱分析，从而鉴定了其结构。 Lanopylins A（1）和B-1分别是（3E）-异十六烷基亚甲基-2-甲基-1-吡咯啉和（3E）-十六烷基亚甲基-2-甲基-1-吡咯啉和Lanopylins A（2）和B-2分别是在羊毛脂蛋白A和B的侧链中插入一个顺式亚乙烯基的同源物。这些化合物抑制重组人羊毛甾醇合酶，IC50值分别为15、18、33和41毫米。 [参考：23]

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