γ-聚谷氨酸-D-半乳糖酯化衍生物-顺铂复合物的制备及其肝靶向性分析

来源 :中国生物工程杂志 | 被引量 : 0次 | 上传用户:YouZiTou
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
制备一种γ-聚谷氨酸-D-半乳糖酯化衍生物-顺铂复合物[Poly(γ-glutamic acid)-D-galactose esterifiable derivative-Cisplatin Complex Compound,γ-D+-DDP],并考察其体内靶向性。通过生物发酵获得大分子γ-聚谷氨酸[Poly(γ-glutamic acid),γ-PGA],利用酸降解得到可以作为药物载体的小分子γ-聚谷氨酸;利用凝胶色谱柱检验小分子γ-聚谷氨酸的分子量;利用HPLC检测释放的游离顺铂含量,得到复合物在小鼠体内靶向性分布情况;利用HE组织切片染色,观察脏器受损伤情况及靶向分布。实验结果表明:成功获得γ-聚谷氨酸-D-半乳糖酯化衍生物-顺铂复合物,该复合物载药率达9.4%~10.2%;HPLC结果表明注射复合物后,肝脏中药物显著增加而肾脏中药物分布明显减少,大大减少了肾毒性,肝靶向作用明显。因此,γ-聚谷氨酸-D-半乳糖酯化衍生物-顺铂复合物是一种有效的具有肝靶向性的抗肿瘤药物,具有潜在的临床应用价值;通过生物发酵获得的γ-聚谷氨酸可用于药物载体,赋予药物新的特点。 A γ-glutamic acid-D-galactose esterifiable derivative-Cisplatin Complex Compound, γ-D + -DDP] Investigate its in vivo targeting. Poly (γ-glutamic acid), γ-PGA] was obtained by biofermentation, and then the small molecule γ-polyglutamic acid which can be used as a drug carrier was obtained by acid degradation. By using the gel column test The molecular weight of small molecule γ-polyglutamic acid; the free cisplatin released by HPLC was measured to obtain the targeted distribution of the compound in mice; the damage of the organ and the targeted distribution were observed by HE tissue section staining . The experimental results show that the drug-loading rate of the compound is 9.4% -10.2%, and the compound of γ-polyglutamic acid-D-galactosyl ester derivative and cisplatin is successfully obtained. HPLC results show that in the liver Drug significantly increased the distribution of drugs in the kidney significantly reduced, greatly reducing the nephrotoxicity, liver-specific role. Therefore, the γ-polyglutamic acid-D-galactoside-esterified derivative-cisplatin compound is an effective liver-targeting anti-tumor drug with potential clinical application value; γ - Polyglutamic acid can be used as a drug carrier, giving the drug new features.
其他文献
张改平,男,1960年生,河南省内黄县人,博士后,研究员。享受国务院特殊津贴专家,“首届百千万人才工程”国家级人选。现任河南省农业科学院 Zhang Pingping, male, born in 19
平阳霉素治疗鼻咽血管纤维瘤万浪,刘维荣湖北省黄石市第三人民医院耳鼻咽喉科(黄石市435000)鼻咽部血管纤维瘤在鼻咽部良性肿瘤的发病中居首位,但由于部位隐蔽,肿瘤可侵犯邻近重要器官,且
风湿热引起角膜病变一例黄剑,蔡爱玲,李社会(河南省济源市人民医院,454650)风湿热是主要累及心脏和关节及结缔组织的疾病,引起角膜病变极为罕见,笔者遇治一例,介绍如下。患者王某,男,15岁,深山居
Objective: To explore the effect and mechanism of Jiaotai Pill(交泰丸, JTW) on intestinal mucosal damage in rats with chronic partial sleep deprivation(PSD). Me
边角网方差分量估计得到的测边方差分量并不具体表示测距的精度。要求得测距精度的验后估值,必须根据方差分量估计过程中的有关数据,应用间接平差原理来计算,本文还通过一个
1.主轴2.四挡小齿轮3.面板垫圈4.开口弹赞环、卡环5.三挡小齿轮(2叮)6.五挡小齿轮(28T)7.二挡小齿轮(1叮)8.轴承9.油封10.轴承11.副轴组合12.二挡车轮齿轮13.面板垫圈14.开口
本文从应急联动系统的功能定位出发,在分析其现实价值的基础上,针对安全防护与管理平台的构建提出了对策建议。 Based on the functional orientation of emergency respons
我院近10余年来采用耳显微手术治疗慢性中耳炎144例,效果较为满意。现报告如下,并就慢性中耳炎与手术有关问题谈粗浅之体会。 1 临床资料 1.1 一般情况:144例中男103例,女41
当前,在高中语文教学中,部分教师墨守成规,还是采取单向灌输的模式开展语文教学,把学生束缚在“课堂中心、课本中心、教师中心”,导致学生学习兴趣不足,学习效率不高,自主学习能力也
用溶胶-凝胶法将纳米TiO2:Sb薄膜沉积在玻璃基板上。研究了掺杂浓度对薄膜的光致超亲水性、薄膜结构和晶相转变的影响.结果表明,纯TiO2薄膜中,TiO2不仅以无定型态存在,而且还