油茶蒲提取物抑制前列腺增生活性化合物的分离与鉴定

Isolation and Identification of Active Compounds on Benign Prostate Hyperplasia from Oiltea camellia Extract

为了探究油茶蒲提取物中对前列腺增生具有抑制作用的天然活性化合物,本研究采用高效制备液相(preparative HPLC)从油茶蒲聚酰胺组分中分离得到抑制前列腺增生(benign prostatic hyperplasia,BPH)的活性化合物。运用质谱(Mass Spectrometer,MS)和核磁共振技术(Nuclear magnetic resonance,NMR)对其化学结构进行鉴定,并采用MTT法检测各化合物对人前列腺增生细胞BPH-1增殖的抑制作用。结果表明:纯化组分F1、F2和F3对BPH-1细胞增殖均具有较强抑制作用,低剂量(50μg/m L)时抑制率分别为30.31%、43.26%和29.00%,抑制效果均优于阳性对照非那雄胺(26.50%)。经化学结构鉴定确定F1、F2和F3分别为橡椀酸双内酯、3-O-没食子酰基-4,6-[(S)-六羟基联苯二酰基]-(α/β)-D-吡喃葡萄糖和3,4,6-三-O-没食子酰基-(α/β)-D-葡萄糖。本研究可为开发改善前列腺疾病的天然产物提供理论参考与物质基础。

In order to investigate bioactive constituents with inhibiting effect on benign prostatic hyperplasia from Oiltea camellia ,preparative high-performance liquid chromatography （preparative HPLC） was adopted to isolate key bioactive compounds from polyamide fraction of O. camellia extracts （OCE）. The chemical structures of those compounds were i- dentified using mass spectrometer（MS） and nuclear magnetic resonance（NMR） analyses. In addition, its growth inhibi- tory activity against BPH-1 cells was detected by MTr assay. The results indicated that F1, F2 and F3, as main active substances in FrS, showed stronger inhibitory effect on BPH-1 ceils at low doses （50 μg/mL） than that of positive control finasteride（26.50% ）, with the inhibition rates of 30.31% ,43.26% and 29.00% , respectively. F1, F2 and F3 were i- dentified as valoneic acid dilactone, 3-O-galloyl-4,6 - [ （S） -hexahydroxydiphenoyl ] - （α/β） -D-glucopyranose and 3,4,6 - tri-O-galloyl-（α/β） -D-glucose,respectively. This study provided theoretical reference and material foundation for the de- velopment of natural products on the improvement of prostate disease.