苯并二氢吡喃衍生物抗骨质疏松活性的构效关系研究

目的 研究系列苯并二氢吡喃化合物的构效关系 ,为设计优良的绝经后骨质疏松症防治药物提供理论依据。方法 在综合考察雷洛昔芬和异丙氧基异黄酮的基础上 ,设计合成一系列苯并二氢吡喃化合物 ,从整体水平考察化合物A对去卵巢大鼠骨质疏松的影响 ,从细胞水平研究C单独给药以及与雌二醇联合给药对人成骨细胞株HOSTE85增殖的影响 ,并均在 0 1μmol·L-1水平考察比较化合物BE对HOSTE85增殖的影响。结果 化合物A可一定程度对抗去卵巢大鼠骨质疏松症。C( 1 0nmol·L-1,0 1μmol·L-1)对HOSTE85具有显著增殖作用 ,C与雌二醇联合给药显著拮抗雌二醇对HOSTE85的增殖作用 ,故C可能为雌激素受体的部分激动剂。C、D( 0 1μmol·L-1)对HOSTE85具有显著增殖作用。结论 以A作为母体化合物 ,侧链引入碱性基团 ,对其结构修饰设计抗绝经后骨质疏松症药物是可行的。

苯并二氢吡喃衍生物的合成及其对骨和血管的初步生物活性

AIM To screen optimal drugs against postmenopausal osteoporosis with cardiovascular protective activities. METHODS A series of benzodihydropyran derivatives were designed and synthesized in view of comprehensive observations of raloxifene and ipriflavone. The antiosteoporosis activities of compounds a-e (10 -7 mol·L -1 ) on the proliferation of human osteoblast cell HOS TE85 were studied. The cardiovascular protective activities were evaluated by observing their effects on proliferation of human vascular endothelium cell ECV 304 and their protective effects on ECV 304 damaged by H 2O 2. RESULTS Their structures were determined by spectrums. Compounds a, b and c (10 -7 mol·L -1 ) were shown to significantly help proliferation of HOS TE85. In addition, b, d and e (10 -8 mol·L -1 ) helped proliferation of ECV 304 significantly. Compounds b and c (10 -6 mol·L -1 ) showed strong protective activity on ECV 304 damaged by H 2O 2. Compounds b and c shifted the KCl dose response curves to the right and decreased the maximal response. CONCLUSION Compounds b and c showed some bone and vascular protective activities which benefit postmenopausal osteoporosis and cardiovascular diseases.

HPLC法测定三叉苦中异吴茱萸酮酚含量

目的:建立HPLC法测定三叉苦中异吴茱萸酮酚含量的方法,为三叉苦药材的质量控制和评价提供科学依据。方法:以十八烷基硅烷键合硅胶为填充剂,以乙腈-醋酸水体系洗脱,体积流量为1.0mL·min-1,柱温30℃,检测波长为230nm。结果:在线性范围29.5～442.8μg,异吴茱萸酮酚对照品的标准曲线呈良好的线性关系,r=0.9988,该方法的平均回收率为103.9%,RSD=0.90%。结论:本方法快速、简便、重复性好,可用于三叉苦中异吴茱萸酮酚的含量测定。