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首页> 外文期刊>RSC Advances >Microbial glycosylation of tanshinone IIA by Cunninghamella elegans AS 3.2028
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Microbial glycosylation of tanshinone IIA by Cunninghamella elegans AS 3.2028

机译：Cunninghamella elegans的丹参酮Iia的微生物糖基化为3.2028

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摘要

Tanshinone IIA (TIIA) is a natural product with significant anti-atherogenic activities. However, poor water-solubility and low bioavailability hinder its further exploitation as a drug candidate. In this study, microbial transformation of TIIA by Cunninghamella elegans AS 3.2028 was conducted to obtain two new glycosylated derivatives. Their structures were identified as hydroquinone TIIA 11-O-beta-D-glucopyranoside (1) and hydroquinone TIIA 12-O-beta-D-glucopyranoside (2) based on extensive NMR and MS spectral analyses. The solubility of 1 in 50% MeOH-H2O solution was approximately 50-fold that of TIIA, and 1 showed remarkably improved oral absorption in mice. Furthermore, 1 and 2 exhibited similar Nrf2 activation activity to TIIA.
机译：丹参酮IIA（TIIA）是一种具有重要抗动脉粥类产活动的天然产物。 然而，水溶性差和低生物利用度阻碍了其进一步的剥削作为毒品候选者。 在这项研究中，进行了Cunninghamella elegans的Tiia的微生物转化为3.2028，以获得两种新的糖基化衍生物。 它们的结构被鉴定为氢醌TIIA 11-O-β-D-吡喃葡萄糖苷（1），基于广泛的NMR和MS光谱分析，基于广泛的NMR和MS光谱分析。依赖于氢醌TIIA12-β-D-吡喃葡萄糖苷（2）。 在50％MeOH-H 2 O溶液中的溶解度为Tiia的约50倍，1显示在小鼠中显着提高口服吸收。 此外，1和2表现出与TIIA类似的NRF2活化活性。

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  • 来源
    《RSC Advances》 |2015年第78期|共4页
  • 作者

    Liang Wen-fei; Li Zi-wei; Ji Shuai; Wang Qi; Qiao Xue; Guo De-an; Ye Min;

  • 作者单位

    Peking Univ Sch Pharmaceut Sci State Key Lab Nat &

    Biomimet Drugs Beijing 100191 Peoples R China;

    Peking Univ Sch Pharmaceut Sci State Key Lab Nat &

    Biomimet Drugs Beijing 100191 Peoples R China;

    Peking Univ Sch Pharmaceut Sci State Key Lab Nat &

    Biomimet Drugs Beijing 100191 Peoples R China;

    Peking Univ Sch Pharmaceut Sci State Key Lab Nat &

    Biomimet Drugs Beijing 100191 Peoples R China;

    Peking Univ Sch Pharmaceut Sci State Key Lab Nat &

    Biomimet Drugs Beijing 100191 Peoples R China;

    Peking Univ Sch Pharmaceut Sci State Key Lab Nat &

    Biomimet Drugs Beijing 100191 Peoples R China;

    Peking Univ Sch Pharmaceut Sci State Key Lab Nat &

    Biomimet Drugs Beijing 100191 Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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