Anti-inflammatory effects of 7-methoxycryptopleurine and structure-activity relations of phenanthroindolizidines and phenanthroquinolizidines |
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Authors: | Yang Cheng-Wei Chuang Ta-Hsien Wu Pei-Lin Huang Wen-Hsin Lee Shiow-Ju |
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Affiliation: | Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli county, Taiwan, ROC. |
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Abstract: | A cryptopleurine analogue, 7-methoxycryptopleurine, a phenanthroquinolizidine, was first found to exert potent anti-inflammatory activity in vitro and in vivo as well as have remarkable cytotoxic activity against cancer cells. The non-planar structure between the two major moieties, phenanthrene and indolizidine/quinolizidine, played a crucial role in the activity of phenanthroindolizidines or phenanthroquinolizidines in terms of cytotoxic effects on cancer cells and anti-inflammatory activity. We also showed that increase in planarity and rigidity of the indolizidine/quinolizidine moiety and change of the amine group into an amide by introducing a keto group to phenanthroindolizidines or phenanthroquinolizidines at the equivalent position 9 of tylophorine significantly reduced their activities. Moreover, in general, phenanthroquinolizidines are more potent than their respective phenanthroindolizines. |
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Keywords: | Anti-inflammation Anti-cancer Cryptopleurine HONE-1 IFNγ Inducible nitric oxide synthase iNOS LPS Nitric oxide NO NUGC-3 Phenanthroindolizidine Phenanthroquinolizidine RAW264.7 Tylophorine |
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