4.5 Article

Synthesis of Novel Derivatives of Esculentoside A and Its Aglycone Phytolaccagenin, and Evaluation of Their Haemolytic Activity and Inhibition of Lipopolysaccharide-Induced Nitric Oxide Production

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CHEMISTRY & BIODIVERSITY
卷 8, 期 10, 页码 1833-1852

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WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbdv.201000339

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资金

  1. Chinese Foundation for High-Tech Project '863' [2006AA090304]
  2. National Natural Sciences Fund of China [30100243, 30672533, 30772644]
  3. Shanghai Pujiang Program [05PJ14003]
  4. '11th Five Year Plan' for scientific Program of PLA [06 H013]

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A series of 46 compounds derived from esculentoside A and its aglycone were synthesized and characterized. The effect of these compounds on lipopolysaccharide (LPS)-induced NO production, haemolytic activity, and cell viability was evaluated. Structure-activity relationship was established by comparing the derivatives of esculentoside A with its aglycone derivatives. Both the aglycone and its derivatives showed higher inhibitory effects on LPS-induced NO production, and lower haemolytic activities than esculentoside A and its derivatives.

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