期刊
NATURAL PRODUCT RESEARCH
卷 32, 期 4, 页码 406-411出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2017.1314279
关键词
Arctigenin; amino acid derivatives; antitumour activity; nitrite-clearing activity; water solubility
资金
- Science and Technology Research Projects in 12th Five-Year Plan of the Jilin Provincial Education Department [201459]
Arctigenin (ARG) is famous in its abundant pharmacological activity. However, many researches in it entered the bottleneck period because of its poor water solubility. The derivatives of ARG have been synthesised with five amino acids which have t-Butyloxy carbonyl (BOC) as a protective group. We examined the effects of removing BOC. The results showed that the amino acid derivatives without protective group have better water solubility and nitrite-clearing ability than ARG. Based on these results, ARG6 and ARG9 were selected at a dosage of 40mg/kg to evaluate their antitumour activity. The percentage inhibition rate of ARG6 and ARG9 were 55.87 and 51.40, respectively, which was twice as much as ARG. Furthermore, they could increase liver and kidney indexes and produce less damage in these organs. In brief, this study provides a basis for new drug development. [GRAPHICS] .
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