New natural sesquiterpenes as modulators of daunomycin resistance in a multidrug-resistant Leishmania tropica line.

Perez Victoria-JM; Tincusi BM; Jimenez IA; Bazzocchi IL; Gupta MP; Castanys S; Gamarro F; Ravelo AG

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New natural sesquiterpenes as modulators of daunomycin resistance in a multidrug-resistant Leishmania tropica line.

机译：新的天然倍半萜作为多药耐药热带利什曼原虫系中对道诺霉素抗性的调节剂。

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摘要

The effects produced by nine dihydro-beta-agarofuran sesquiterpenes isolated from Crossopetalum tonduzii (1-8) and Maytenus macrocarpa (9) (Celastraceae) on the reversion of the resistant phenotype on a multidrug-resistant Leishmania line and their binding to recombinant C-terminal nucleotide-binding domain of Leishmania P-glycoprotein-like transporter were studied. The structures of the new compounds (1-5) were elucidated by spectroscopic methods, including (1)H-(13)C heteronuclear correlation (HMQC), long-range correlation spectra with inversal detection (HMBC), ROESY experiments, and chemical correlations. The absolute configuration of one of them (1) was determined by CD studies. The structure-activity relationship is discussed.

机译：分离自通心粉菌（1-8）和大叶美叶锦葵（9）（Celastraceae）的九种二氢-β-agarofuran倍半萜对多药抗性利什曼原虫系的耐药表型回复及其与重组C-结合的影响研究了利什曼原虫P-糖蛋白样转运蛋白的末端核苷酸结合结构域。通过光谱方法阐明了新化合物（1-5）的结构，包括（1）H-（13）C异核相关（HMQC），具有反向检测的远程相关光谱（HMBC），ROESY实验和化学方法相关性。其中一项（1）的绝对构型由CD研究确定。讨论了构效关系。

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来源
《Journal of Medicinal Chemistry》 |1999年第21期|共6页
作者
Perez Victoria-JM; Tincusi BM; Jimenez IA; Bazzocchi IL; Gupta MP; Castanys S; Gamarro F; Ravelo AG;
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正文语种 eng
中图分类药学;
关键词
Antibiotics; Anthracycline; Daunorubicin; Leishmania tropica; Rosales; Sesquiterpenes; 抗生素类; 蒽环; 柔红霉素; 利什曼原虫; 热带; 蔷薇目; 倍半萜类; 抗锥虫药;

机译：Antibiotics;Anthracycline;Daunorubicin;Leishmania tropica;Rosales;Sesquiterpenes;抗生素类;蒽环;柔红霉素;利什曼原虫;热带;蔷薇目;倍半萜类;抗锥虫药;

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1. 已被证实用于多药耐药性研究的一种新的多发性骨髓瘤细胞系 [J] . Hui Xiao, Qi Xiao, Ke jianZhang, 中德临床肿瘤学杂志（英文版） . 2009,第005期
2. New natural sesquiterpenes as modulators of daunomycin resistance in a multidrug-resistant Leishmania tropica line. [J] . Perez Victoria-JM, Tincusi BM, Jimenez IA, Journal of Medicinal Chemistry . 1999,第21期

机译：新的天然倍半萜作为多药耐药热带利什曼原虫系中对道诺霉素抗性的调节剂。
3. High-affinity binding of silybin derivatives to the nucleotide-binding domain of a Leishmania tropica P-glycoprotein-like transporter and chemosensitization of a multidrug-resistant parasite to daunomycin. [J] . Perez-Victoria JM, Perez-Victoria FJ, Conseil G, Antimicrobial agents and chemotherapy. . 2001,第2期

机译：水飞蓟宾衍生物与热带利什曼原虫P-糖蛋白样转运蛋白的核苷酸结合结构域的高亲和力结合以及多药耐药性寄生虫对道诺霉素的化学增感作用。
4. Alkyl-lysophospholipid resistance in multidrug-resistant Leishmania tropica and chemosensitization by a novel P-glycoprotein-like transporter modulator. [J] . Perez-Victoria JM, Perez-Victoria FJ, Parodi-Talice A, Antimicrobial agents and chemotherapy. . 2001,第9期

机译：耐多药热带利什曼原虫的烷基溶血磷脂抗性和新型P-糖蛋白样转运蛋白调节剂的化学增敏作用。
5. Importance of the C9 absolute configuration for the antifungal activity of natural and semisynthetic sesquiterpenes [C] . M. Derita, M. Di Liberto, S. Zacchino International Conference on Antimicrobial Research . 2011

机译：C9绝对配置对自然和半合成阶段的抗真菌活动的绝对配置
6. Proteasome inhibitor biosynthesis and self-resistance in the marine actinobacterium Salinispora tropica. [D] . Kale, Andrew John. 2012

机译：蛋白酶体抑制剂的生物合成和自抗性在海洋放线杆菌热带萨利氏菌中。
7. High-Affinity Binding of Silybin Derivatives to the Nucleotide-Binding Domain of a Leishmania tropica P-Glycoprotein-Like Transporter and Chemosensitization of a Multidrug-Resistant Parasite to Daunomycin [O] . José M. Pérez-Victoria, F. Javier Pérez-Victoria, Gwenaëlle Conseil, 2001

机译：水飞蓟宾衍生物高亲和力结合到热带利什曼原虫P-糖蛋白样转运蛋白的核苷酸结合域和多药耐药性对道诺霉素的化学敏感性。
8. New natural sesquiterpenes as modulators of daunomycin resistance in a multidrug-resistant Leishmania tropica line [O] . Pérez-Victoria J. M., Tincusi B. M., Jiménez I. A., 2013

机译：新的天然倍半萜作为多药耐药热带利什曼原虫系中对道诺霉素抗性的调节剂
9. Macrophage Activation to Kill Leishmania Tropica: Characterization of P/J Mouse Macrophage Defects for Lymphokine-Induced Antimicrobial Activities Against Leishmania Tropica Amastigotes. [R] . Nacy, C. A., Meltzer, M. S., Fortier, A. H. 1984

机译：巨噬细胞激活杀死利什曼原虫Tropica：表征p / J小鼠巨噬细胞缺陷的淋巴因子诱导抗真菌活性对利什曼原虫Tmasica amastigotes。

New natural sesquiterpenes as modulators of daunomycin resistance in a multidrug-resistant Leishmania tropica line.

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