I.Estrogenic/antiestrogenic Bioassay Using Transgenic Plants, pER8:GUS and pER8:GFPII.Studies on the Chemical Constituents and Bioactivities of Caesalpinia sappan L.

• Main Authors: Wan-Chun Lai, 賴宛君
• Other Authors: Fung-Rung Cheng
• Format: Others
• Language: zh-TW
• Published: 2008
• Online Access: http://ndltd.ncl.edu.tw/handle/36493483430705198027

碩士 === 高雄醫學大學 === 天然藥物研究所 === 96 === In recent years, phytoestrogens have substituted synthetic estrogens, as the supplement source of estrogen, used to modify symptoms of postmenopausal women. Most of Phytoestrogens belong to isoflavonoids widely existent in our daily diet. The bioactivity of phytoestrogen is lower than estrogen around 1/102 ~ 1/105. According to some researches, phytoestrogens induced cell proliferation of hormone-dependent carcinoma. In the other articles, phytoestrogens also showed antiestrogenic activity. Therefore, investigations on the physiological functions of phytoestrogens still have no identical conclusion about the advantage and harm. For the reason, the research of phytoestrogens is imperative and very important. In this study, we applied pER8:GFP, a transgenic plant as a tool of estrogenic activity assay model to screen anti-estrogenic activity combined with the clinical drug Tamoxifen. Further, we used the other transgenic plant pER8:GUS as a detector for estrogenic activity. The new estrogenic assay model showed higher sensitivity and needed shorter time to culture. In addition, we determined twenty Chinese traditional herbs according to traditional Chinese medical theory by pER8:GUS estrogenic activity assay. Then, we got an active extract from Su Mu, Caesalpinia sappan. Su Mu is a natural, sweet and salty traditional Chinese medicine, which can invigorate circulation, break up blood stasis condition, and promote menstruation including injuries from impact, swollen boils, irregular menses, and pain from blood stasis after birth. It is an important Chinese medicine in gynecology. Bioactivity-guided fractionation of the active extract of Su Mu led to the isolation of eleven compounds including ten known compounds and one new compound. Ten known compounds are as follows: brazilein (1)、brazilin (2)、protosappain A (3)、3,7-dihydroxy-4H-chromen-4-one (4)、3’-deoxyepisappanol (6)、3’-deoxysappanol (7)、3-deoxysappanone B (8)、4-(7-hydroxy-2,2-dimethyl-9bH-1,3,5-trioxa-cyclopenta[a]naphthalene- 3a-ylmethyl-)-benzene-1,2-diol (9)、3-deoxysappanchalcone (10)、3’-deoxysappanone B (11). Moreover, (S)-2,3-dihydro-3,7-dihydroxychromen-4-one (5) is a new compound. Most pure compounds belong to homoisoflavonoids. Compounds 3、4、8、10 and 11 showed estrogenic activity. Among those five compounds , compounds 3、8 and 11 also proposed antiestrogenic activity. Compounds 1、2、5 and 10 exhibited cytotoxicity to different cancer cell. Furthermore, compounds 1、3、4、7 and 10 inhibited platelet aggregation.