具有A环烯酮官能团的新型桦木酸类似物的设计、合成及其体外和体内抗炎活性
Design, synthesis, and anti-inflammatory activity both in vitro and in vivo of new betulinic acid analogues having an enone functionality in ring A.
作者信息
Honda Tadashi, Liby Karen T, Su Xiaobo, Sundararajan Chitra, Honda Yukiko, Suh Nanjoo, Risingsong Renee, Williams Charlotte R, Royce Darlene B, Sporn Michael B, Gribble Gordon W
机构信息
Department of Chemistry, Dartmouth College, Hanover, NH 03755, USA.
出版信息
Bioorg Med Chem Lett. 2006 Dec 15;16(24):6306-9. doi: 10.1016/j.bmcl.2006.09.012. Epub 2006 Sep 25.
Abstract
Fifteen new betulinic acid analogues were designed, synthesized, and tested for anti-inflammatory activity. Many of these analogues effectively suppress nitric oxide (NO) production in RAW cells stimulated with interferon-gamma. Analogue 10 is highly and orally active in vivo for induction of the anti-inflammatory and cytoprotective enzyme, heme oxygenase-1.
摘要
设计、合成了15种新的桦木酸类似物，并对其抗炎活性进行了测试。这些类似物中的许多能有效抑制经γ干扰素刺激的RAW细胞中一氧化氮（NO）的产生。类似物10在体内对诱导抗炎和细胞保护酶血红素加氧酶-1具有高度口服活性。
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