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首页> 外文期刊>Bioorganic and medicinal chemistry >Design, development and synthesis of mixed bioconjugates of piperic acid-glycine, curcumin-glycine/alanine and curcumin-glycine-piperic acid and their antibacterial and antifungal properties.
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Design, development and synthesis of mixed bioconjugates of piperic acid-glycine, curcumin-glycine/alanine and curcumin-glycine-piperic acid and their antibacterial and antifungal properties.

机译：胡椒酸-甘氨酸，姜黄素-甘氨酸/丙氨酸和姜黄素-甘氨酸-哌酸混合生物共轭物的设计，开发和合成及其抗菌和抗真菌特性。

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摘要

In the present communication different curcumin bioconjugates viz. 4,4'-di-O-glycinoyl-curcumin, 4,4'-di-O-d-alaninoyl-curcumin, 4,4'-di-O-(glycinoyl-di-N-piperoyl)-curcumin, 4,4'-di-O-piperoyl curcumin, curcumin-4,4'-di-O-beta-d-glucopyranoside, 4,4'-di-O-acetyl-curcumin along with piperoyl glycine, have been synthesised and characterised by spectra UV, (1)H NMR and elemental analysis. All the covalent bonds used are biodegradable. This makes these derivatives as potent prodrugs, which can get hydrolysed at the target sites. These bioconjugates were tested in vitro against different bacteria and fungi. The 4,4'-di-O-(glycinoyl-di-N-piperoyl)-curcumin and 4,4'-di-O-acetyl-curcumin are more effective than Cefepime, an antibacterial drug available in market, at the same concentration. The 4,4'-di-O-(glycinoyl-di-N-piperoyl)-curcumin and 4,4'-di-O-piperoyl curcumin had antifungal activity in vitro almost comparable with fluconazole, the most popular antifungal drug. The enhanced activity of these bioconjugates vis-a-vis the parent molecule that is curcumin may be due to improved cellular uptake or reduced metabolism of these bioconjugates resulting in building up of enough concentration inside the infected cells. It opens a new era for exploring suitably designed curcumin bioconjugates as potential antibacterial/antifungal drugs.
机译：在本发明中，不同的姜黄素生物缀合物即。 4,4'-二-O-甘氨酰姜黄素，4,4'-二-Od-丙氨酰-姜黄素，4,4'-二-O-（甘氨酰-二-N-哌啶基）-姜黄素，4,4合成了'-二-O-哌酰基姜黄素，姜黄素-4,4'-二-O-β-d-吡喃葡萄糖苷，4,4'-二-O-乙酰基姜黄素以及哌啶基甘氨酸，并通过光谱进行了表征UV，（1）H NMR和元素分析。所有使用的共价键都是可生物降解的。这使得这些衍生物成为有效的前药，可以在目标部位水解。这些生物结合物在体外针对不同的细菌和真菌进行了测试。 4,4'-二-O-（甘氨酰基-二-N-哌啶基）姜黄素和4,4'-二-O-乙酰基姜黄素比头孢吡肟（Cefepime）更有效，后者是市场上出售的抗菌药物。浓度。 4,4'-二-O-（甘氨酰基-二-N-哌啶基）姜黄素和4,4'-二-O-哌啶基姜黄素在体外具有抗真菌活性，几乎与最受欢迎的抗真菌药氟康唑相当。这些生物结合物相对于姜黄素的亲本分子的活性增强可能是由于这些生物结合物的细胞摄取提高或代谢降低，从而导致在感染细胞内积累了足够的浓度。它为探索适当设计的姜黄素生物共轭物作为潜在的抗菌/抗真菌药物开辟了一个新时代。

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