Louisianin A 為一多取代呲啶類的天然物,具有抑testosterone-responsive
Shionogi carcinoma SC 115 細胞生長的生理活性,而且可藉由簡單的化學反應步驟將louisianin A 轉化為louisianin C,而louisianin C 不但具有抑制血管內皮樣細胞生成的作用,更可利用異構化的反應而形成louisianin D 或製備天然物ulupyrinone。
目前我們將合成Louisianin A 的步驟分成兩條不同的途徑,嚐試以不同的合成方法來達到Louisianin A 的最佳合成條件,並將進一步與生科系其他研究團隊合作,探討Louisianin A 其他的生理活性與應用。
Louisianin A was produced from the fermentation broth of Streptomyces sp.WK-4028 which was isolated from a soil sample collected in the state of Louisiana(USA). The louisianin A remarkably inhibited the growth of testosterone-resposive Shionogi carcinoma SC 115 cells in the presence of 10-7 M testosterone with an IC50value of 0.6 μg/ml.
Recently, louisianin C and D were reported which potently supressed the tubeformation of cultured vascular endothelical cell in vitro, although louisianin C and Dshowed only slight inhibitory activity on the growth of testosterone-resposive Shionogi carcinoma SC 115 cells.
Up to date, we have designed two strategies for the synthesis of louisianin A, andwe are not only interested in the synthesis of louisianin A, but also can develop thederivatives of louisianins.