吲哚硫代葡萄糖苷的合成及其抗炎活性
Synthesis and anti-inflammatory activity of indole glucosinolates.
作者信息
Vo Quan V, Trenerry Craige, Rochfort Simone, Wadeson Jenny, Leyton Carolina, Hughes Andrew B
机构信息
Department of Chemistry, La Trobe University, Victoria 3086, Australia.
Department of Primary Industries, Knoxfield Centre, 621 Burwood Highway, Knoxfield 3180, Australia.
出版信息
Bioorg Med Chem. 2014 Jan 15;22(2):856-64. doi: 10.1016/j.bmc.2013.12.003. Epub 2013 Dec 12.
The nitronate and nitrovinyl methods to synthesize indole glucosinolates (GLs) have been investigated. The results were applied to generally the most prevalent natural indole glucosinolates to synthesize 4-methoxyglucobrassicin (MGB) and neo-glucobrassicin (NGB) in moderate overall yield for the first time. The anti-inflammatory activity of the synthetic indole GLs was determined by inhibition of TNF-α secretion in LPS-stimulated THP-1 cells. The data showed that glucobrassicin (GB) exhibited higher activity than other synthetic indolyl GLs.
对合成吲哚硫代葡萄糖苷（GLs）的硝酮酸酯法和硝基乙烯法进行了研究。研究结果首次应用于一般最普遍的天然吲哚硫代葡萄糖苷，以中等总收率合成了4-甲氧基硫代葡萄糖苷（MGB）和新硫代葡萄糖苷（NGB）。通过抑制脂多糖刺激的THP-1细胞中TNF-α的分泌来测定合成吲哚GLs的抗炎活性。数据表明，硫代葡萄糖苷（GB）比其他合成吲哚基GLs表现出更高的活性。
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