Fan Guan-Wei, Gao Xiu-Mei, Wang Hong, Zhu Yan, Zhang Ju, Hu Li-Min, Su Yan-Fang, Kang Li-Yuan, Zhang Bo-Li
Institute of Traditional Chinese Medicine Research, Tianjin University of Traditional Chinese Medicine, 312 Anshanxi Road, Tianjin, China.
J Steroid Biochem Mol Biol. 2009 Feb;113(3-5):275-80. doi: 10.1016/j.jsbmb.2009.01.011. Epub 2009 Feb 7.
Tanshinone IIA (Tan IIA) is a major compound extracted from a traditional herbal medicine Salvia miltiorrhiza BUNGE, which is used to treat cardiovascular diseases, cerebrovascular diseases and postmenopausal syndrome. It has also been shown to possess anti-inflammatory activity. Since Tan IIA has a similar structure to that of 17beta-estradiol (E(2)), the present study was undertaken to characterize the estrogenic activity of Tan IIA and to demonstrate a functional role of this activity in RAW 264.7 cells. In transient transfection assay, Tan IIA (10 microM) increases ERE-luciferase activity in an estrogen receptor (ER) subtype-dependent manner when either ERalpha or ERbeta were co-expressed in Hela cells. In LPS-induced RAW 264.7 cells, Tan IIA exerts anti-inflammatory effects by inhibition of iNOS gene expression and NO production, as well as inhibition of inflammatory cytokine (IL-1beta, IL-6, and TNF-alpha) expression via ER-dependent pathway. Therefore, it could serve as a potential selective estrogen receptor modulator (SERM) to treat inflammation-associated neurodegenerative and cardiovascular diseases without increasing the risk of breast cancer.
丹参酮IIA（Tan IIA）是从传统草药丹参中提取的一种主要化合物，丹参用于治疗心血管疾病、脑血管疾病和绝经后综合征。它还具有抗炎活性。由于Tan IIA的结构与17β-雌二醇（E₂）相似，因此本研究旨在表征Tan IIA的雌激素活性，并证明这种活性在RAW 264.7细胞中的功能作用。在瞬时转染试验中，当雌激素受体（ER）α或ERβ在Hela细胞中共同表达时，Tan IIA（10微摩尔）以雌激素受体亚型依赖性方式增加ERE-荧光素酶活性。在脂多糖诱导的RAW 264.7细胞中，Tan IIA通过抑制诱导型一氧化氮合酶（iNOS）基因表达和一氧化氮（NO）产生发挥抗炎作用，以及通过雌激素受体依赖性途径抑制炎性细胞因子（IL-1β、IL-6和肿瘤坏死因子-α）表达。因此，它可作为一种潜在的选择性雌激素受体调节剂（SERM），用于治疗与炎症相关的神经退行性疾病和心血管疾病，而不会增加患乳腺癌的风险。
