【作者】 李延平； 刘义； 吴科锋； 邓亦峰； 艾春梅； 龚先玲； 吕应年； 崔燎；

【Author】 LI Yan-ping,LIU Yi,WU Ke-feng,Deng yifeng,AI Chun-mei,GONG xian-ling,LV ying-nian,Cui liao.(Guangdong key Laboratory for Research and Development of Natural Drugs,zhanjiang 524023,China)

【机构】 广东天然药物研究与开发重点试验室；

【摘要】 目的综合评价抗骨质疏松产品-骨元肽结肠靶向胶囊。方法抗骨质疏松试验采用新生SD大鼠成骨细胞体外培养法,测定MTT、ALK和矿化骨结节。体内试验:对SD大鼠实施手术去除双侧卵巢,造成骨质疏松模型,口服三种(5.0、20.0、80.0mg.kg-1.d-1)剂量骨元肽结肠靶向胶囊,检测血清中雌二醇(E2)、骨钙素(BGP)、转化生长因子(TGF-β1)、碱性磷酸酶(ALK);骨密度、24小时尿液中Ca、P含量;测定骨元肽分子量分布及大鼠在体结肠吸收率。结果骨元肽对新生SD大鼠成骨细胞有明显增殖作用,ALK活性增强、矿化骨结节数量增多;骨元肽结肠靶向胶囊组可明显提高去卵巢大鼠血清中E2、TGF-β,增加BMD,降低血清中ALK、BGP和24小时尿Ca、P含量;骨元肽Mw为189～1000D,其中189-512D组分占68.5%以上;口服4h结肠平均吸收率为49.61%。结论骨元肽结肠靶向胶囊一种安全、有效,质量可控,增加骨密度、防治中老年人骨质疏松症的健康产品。更多还原

【Abstract】 Objective To perform comprehensive evaluation on colon targeting capsule of Guyuan peptide(GYP)for anti-osteoporosis action.Methods In vitro anti-osteoporosis product was investigated by MTT method,detecting alkaline phosphatase(ALK)and mineralized nodes in osteoblasts from SD rats.In vivo the rat models of osteoporosis were induced by ovariectomy and treated with three doses of colon targeting capsule of GYP(5.0,20.0,80.0mg.kg-1.d-1).The serum levels of estradiol(E2),osteocalcin(BGP),transforming growth factors(TGF-β1)and ALK,bone mineral density(BMD),and the contents of calcium(Ca)and phosphorus(P)in 24h urine were detected.The distribution and absorption of GYP’s MW in the colon of rats were also investigated.Results GYP enhanced cell proliferation,ALK activity and the number of mineralized nodes in rats’ osteoblasts.The colon targeting capsule of GYP were significantly increased the serum level of E2,TGF-β1,and BMD,decreased the serum level of ALK,BGP and the contents of Ca,P in 24h urine,and the capsules had no side effects and the shelf life of them reached 24 months.The Mw of GYP is between 189-1000 D,in which the component of 189-512D takes 68.5% or above.The average absorption rate is 49.61% in the colon of rats.Conclusion The colon targeting capsule of Guyuan peptide is an effective and safe product with controllable quality for BMD enhancement,prevention and control of osteoporosis in middle-aged and senile groups.更多还原