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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| Authors: | Gong Wei Jiang Zhihui Sun Peng Li Ling Jin Yongsheng Shao Lucheng Zhang Wen Liu Baoshu Zhang Hongwei Tang Hua Chen Yufeng Yi Yanghua Zhang Dazhi |
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| Institution: | 1. School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, P.?R. China (phone/fax: +86‐21‐81871226);2. Department of Pharmacy, the Eighth Hospital of PLA, 5 Western Zhufeng Road, Xigaze 857000, P.?R. China;3. Department of Pharmacy, the Shenyang North Hospital, 83 Wenhua Road, Shenyang 110016, P.?R. China |
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| Abstract: | 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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| Keywords: | Esculentoside A Phytolaccagenin Haemolytic activity Inhibitors Structure?activity relationship (SAR) |
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