Detecting membrane progestin receptor (mPR)-interacting compounds from coral seawater in Mauritius
Detecting membrane progestin receptor (mPR)-interacting compounds from coral seawater in Mauritius
复制标题
检测毛里求斯珊瑚海水中的膜孕激素受体 (mPR) 相互作用化合物
DOI：
--
复制
发表时间：
2017
期刊：
影响因子：
--
通讯作者：
R. Bhagooli
中科院分区：
文献类型：
--
作者：
T. Tokumoto;S. Kodani;Takehiro Miyazaki;Yoshimi Suzuki;B. Casareto;T. Bahorun;R. Bhagooli
孕激素是生殖的关键调节因子。虽然孕酮的生理作用是通过调节核孕酮受体(NPR)相关基因的表达来实现的，但当细胞膜孕激素受体(MPR)被识别时，对孕酮活性的研究提供了新的见解。此外，MPR已被证明是内分泌干扰物(EDCs)的新靶点。与MPR相互作用的天然激素化合物或人工化学物质被寻求作为可能的新型药物或EDCs。在这项研究中，对毛里求斯阿尔比昂珊瑚礁海水中溶解的与MPR相互作用的化学物质进行了筛选。用含有mprα基因的稳定表达细胞的破碎细胞膜进行类固醇结合实验，评价这些化合物与mprα基因的相对结合性。结果，从珊瑚礁中获得的化合物中检测到结合活性。与礁滩地区相比，泻湖地区的结合活性最高。这些结果表明，在阿尔比翁珊瑚礁海域的海水中产生了与mprα有关的天然激素化合物，并在某些特定条件下积累。
Progestins are key regulators of reproduction. Although the physiological e ects of progesterone are mediated by regulating the expression of genes associated with nuclear progesterone receptors (nPRs), new insights into proges- terone activity was provided when membrane progestin receptors (mPRs) were identi ed. Also, mPRs have been shown to be a novel target for endocrine disrupting chemicals (EDCs). Natural hormonal compounds or arti cial chemicals that interact with mPRs were sought as possible novel pharmaceuticals or EDCs. Chemicals dissolved in coral reef seawater from Albion, Mauritius that interact with mPRs were screened during this study. The relative binding a nity of these compounds to the mPR α in vitro was evaluated using a steroid binding assay with crushed cell membranes from stably transfected cells containing the mPR α gene. As a result, binding activity in the compounds obtained from coral reef was detected. The highest binding activity was detected in a lagoon area when compared with that in the reef and beach areas. These results suggest that natural hormonal compounds with a nity for mPR α are produced, and under some speci c conditions, accumulated, in seawater of a coral reef area at Albion.