One unique steroidal sapogenin obtained through the microbial transformation of ruscogenin by Phytophthora cactorum ATCC 32134 and its potential inhibitory effect on tissue factor (TF) procoagulant activity

被引：30

作者：

Chen, Nai-Dong ^{[1
]}

Yue, Lei ^{[2
]}

Zhang, Jian ^{[1
]}

Kou, Jun-Ping ^{[2
]}

Yu, Bo-Yang ^{[2
]}

机构：

[1] China Pharmaceut Univ, Dept Complex Prescript Tradit Chinese Med, 639 Long Mian Rd, Nanjing 211198, Peoples R China

[2] China Pharmaceut Univ, Key Lab Modern Chinese Med, Minist Educ, Nanjing 210009, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 14期

关键词：

Ruscogenin; 1-beta-Hydroxy-spirost-4-en-3-one; Phytophthora cactorum ATCC 32134; Tissue factor; Steroidal sapogenin; FLUOROPYRIDINE-BASED INHIBITORS; RADIX-OPHIOPOGON-JAPONICUS; ASPERGILLUS-TAMARII KITA; FACTOR MUTANT; LACTONIZATION; THROMBOSIS; DISCOVERY; EXTRACT; PATHWAY;

D O I：

10.1016/j.bmcl.2010.05.103

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

With the aim to obtain more effective tissue factor (TF) inhibitors, the microbial transformation of three steroidal sapogenins, ruscogenin (1), diosgenin (2) and sarsasapogenin (3), was carried out and only ruscogenin was selectivity converted to 1-hydroxy-spirost-4-en-3-one (4) by Phytophthora cactorum ATCC 32134. The in vitro anti-TF procoagulant activity of this metabolite was enhanced almost 10 times to an IC50 value of 0.29 mu M. The chemical assignments of compound 4 were made unambiguously using ESI-MS, IR and 2D NMR spectroscopy. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：4015 / 4017

页数：3

共 22 条

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MICROBIAL TRANSFORMATION OF ANTIBIOTICS .5. CLINDAMYCIN RIBONUCLEOTIDES [J].