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Design, synthesis, and anti-inflammatory activity both in vitro and in vivo of new betulinic acid analogues having an enone functionality in ring A |
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| Authors: | 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 |
| Affiliation: | aDepartment of Chemistry, Dartmouth College, Hanover, NH 03755, USA bDepartment of Pharmacology and Toxicology, Dartmouth Medical School, Hanover, NH 03755, USA |
| 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-γ. Analogue 10 is highly and orally active in vivo for induction of the anti-inflammatory and cytoprotective enzyme, heme oxygenase-1. |
| Keywords: | Triterpene Betulinic acid Inhibitors of nitric oxide production RAW 264.7 cells Inducer of heme oxygenase-1 |
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