前体药物

抗体导向酶-前体药物疗法（antibody-directedenzymeprodrugtherapy，ADEPT）是近年来肿瘤抗体导向治疗研究中一项引人注目的新进展。

Antibody-directed enzyme prodrug therapy ( ADEPT ) is one of the noticeable new progresses in the research of antibody-directed treatment for tumor in recent years .

缬更昔洛韦（valganciclovir）是抗病毒药更昔洛韦的前体药物，用于治疗AIDS病人发生的巨细胞病毒（CMV）视网膜炎。

Valganciclovir is a prodrug of ganciclovir which has been developed for the treatment of cytomegalovirus ( CMV ) retinitis in patients with AIDS .

N1-羧酰-5-氟脲嘧啶系列前体药物的合成

Synthesis of prodrugs of n_1 alkyl 5 fluorouracil derivatives

目的：探讨双自杀基因CD和TK对K562细胞的体内外抑制作用及前体药物对肿瘤的杀伤作用。

OBJECTIVE : To study the killing effect of double suicide genes system on K562 cells in vivo and in vitro .

结果表明，地塞米松前体药物ig后，地塞米松主要集中在盲肠和结肠内释放，吸收显著减少。

We found that dexamethasone and dexamethasone hemisuccinate were mainly released in cecum and colon contents after oral administration of dexamethasone prodrug .

在6种已转染的肺癌细胞株中，有2种肺癌细胞株（SPCA－1，A549）对前体药物5－FC和GCV有较高的敏感性；

Two out of six human lung cancer cell lines ( SPCA-1 , A549 ) have a high sensitivity to 5-FC and GCV ;

结论氧化苦参碱与甘珀酸钠不同比例复合物的毒性均比其前体药物低；对小鼠急性CCl4肝损伤有保护作用。

Conclusion The toxicity of the complex in different proportions on acute hepatic injuried mice by CCl_4 decreases obviously , compared with their precursor drugs .

方法将前体药物分别与不同pH值缓冲液、含葡聚糖酶的缓冲液及含大肠杆菌的培养基于37℃水浴中一起孵育，采用HPLC法测定前体药物释放泼尼松龙的情况。

METHODS After the prodrug was incubated at 37 ℃ with buffers of different pH , buffers with dextranase and with culture medium containing bacterium coli respectively , the release of prednisolone ( PL ) from prodrug were determined by HPLC .

FCU／5-氟胞嘧啶自杀基因前体药物系统联合放射治疗鼻咽癌的实验研究

Combining FCU / 5-FU suicide gene / prodrug system and radiation in treating nasopharyngeal carcinoma : an experimental study

应用重组病毒联合前体药物lin进行多种肿瘤细胞系的体内、体外治疗，探讨腺病毒载体介导的lis/lin系统的抑瘤效果及作用机理；3.克隆AFP启动子，检测其靶向转录活性。

The antitumor effect and the mechanism of the adenovirus mediated lis / lin system is explored in vitro and in vivo . 3 . To clone AFP promoter and detect its target transcription activity .

与同浓度姜黄素比较，两种前体药物对HKC细胞生长的抑制作用均显著降低（P0.01）。

When compared with the curcumin of same concentrations , the growth inhibitory effects of these two prodrugs on HKC cells were significantly decreased ( P0.01 ) .

南极假丝酵母脂肪酶B（CandidaAntarcticalipaseB，CALB）具有广谱底物接受性和对映体选择性，广泛应用于食品、化工、前体药物的合成和生物能源等领域。

For its broad spectrum of substrate acceptance and enantioselectivity , Candida antarctica lipase B ( CALB ) has been widely used in the fields of food , chemicals , drug precursors synthesis and bio-energy .

福辛普利（蒙诺）是其活性二价酸福辛普利拉的酯类前体药物，也是新的磷酸类血管紧张素转换酶（ACE）抑制剂家族中的第一个成员。

Fosinopril ( MoNopril ) is an ester pro-drug of the active Daicel fosinoprilat and is the first member of a new class of angiotensin-converting enzyme ( ACE ) inhibitors , the phosphoric acids .

药物敏感基因能将无毒的前体药物（prodrug）转化为有毒的药物而杀伤细胞，故又称自杀基因。

Drug sensitive gene can convert nontoxic prodrugs into toxic drugs thus kills the cells , therefore it is also called " suicide " gene .

方法：用前体药物甲氨喋呤α苯丙氨酸（MTXαPhe）和甲氨喋呤α精氨酸（MTXαArg）对前列腺癌荷瘤裸鼠模型行肿瘤生长抑制及药物动力学的观察。

Methods : The growth inhibition and the pharmacokinetics were observed using the prodrugs of MTX α Phe and MTX α Arg on the mice model bearing with the prostate cancer .

目的研究胞嘧啶脱氨酶基因（CD）联合前体药物5氟胞嘧啶（5Fc）对结肠癌细胞的生长抑制作用。

Objective To investigate the effect of cytosine deaminase ( CD ) gene plus 5 fluorocytosine ( 5 Fc ) on the growth of human colon cancer xenograft in nude mice .

利用Hoechst-PI双染色法检测经前体药物作用后转染细胞，各组均可见凋亡细胞，但联合用药组凋亡细胞较单一用药组多。

Double prodrugs group showed more apoptosis cells than the single prodrug group according to Hoechst-PI colorant analysis .

给予前体药物5-氟胞嘧啶（5-FC）和/或无环鸟苷（GCV）后，MTT法测定细胞的存活率，流式细胞仪检测细胞的凋亡率。

After prodrug GCV or / and5-FC were administered , MTT method was used to detect the growth rate of T lymphocytes and flow cytometry ( FCM ) was used to evaluate the apoptosis rate of T lymphocytes .

MTT比色分析法比较两种姜黄素前体药物作用6~24h后，人膀胱癌EJ细胞及肾小管上皮HKC细胞生长抑制的差异。

After treatment with these two prodrugs for 6 ~ 24 h , the growth inhibition rates on human bladder cancer EJ cells and renal tubular epithelial ( HKC ) cells were detected using MTT colorimetry .

目的：研究辣根过氧化物酶（HRP）/吲哚乙酸（IAA）系统作为基因导向性酶前体药物疗法（GDEPT）体外作用于人喉鳞癌Hep-2细胞株所产生的细胞毒性作用。

Objective : To study the cytotoxicity on human laryngeal squamous carcinoma cell line Hep-2 using horseradish peroxidase ( HRP ) / indole-3-acetic acid ( IAA ) system as gene-directed enzyme prodrug therapy ( GDEPT ) .

方法将前体药物按30μmol·kg-1的剂量给大鼠灌胃，用HPLC检测大鼠胃肠道不同部位内容物中，药物浓度的变化以及血药浓度的变化，并与游离泼尼松龙作比较。

Method The prodrug was given by ig at the dosage of 30 μ mol · kg - 1 . The contents of released prednisolone in different parts of rat gastrointestinal tract and in plasma were determined by HPLC , and compared with free dexamethasone .

方法通过丁二酸酐搭桥，合成地塞米松葡聚糖酯前体药物；

METHODS Dexamethasone succinate dextran was synthesized in an anhydrous environment .

布洛芬高分子前体药物及纳米微球的合成和表征

Synthesis and Characterization of Polymeric Drug Containing Brufen and its Nano-sphere

目的研究甲硝唑前体药物甲硝唑琥珀酸酯在兔体内的药动学特性。

OBJECTIVE To study the pharmacokinetic profile of metronidazole-succinate in rabbits .

结论该法有助于他克林前体药物的研究。

CONCLUSION The prodrug of4-Aminotetrahydroacridine can be synthesized by this method .

酮洛芬前体药物皮肤渗透代谢的立体选择性研究

Studies on the Stereoselectivity in Transdermal Permeation and Metabolism of Ketoprofen Prodrugs

泼尼松龙前体药物的结肠定位研究

The Investigation of a Prednisolone Prodrug for Colon-Specific Drug Delivery

N1-羧酰-5-氟尿嘧啶系列前体药物的体外降解动力学研究

Studies on Degradation Kinetics of Various N_1-Acyl Derivatives of 5-Fluorouracil in vitro

目的：研究酮洛芬异丙酯在皮肤细胞中的代谢作用，为进一步研究利用酯类前体药物方法改善药物的经皮吸收特性提供实验依据。

OBJECTIVE To study the metabolism of ketoprofen isopropyl ester in skin cells .

前体药物甲氨喋呤-α-肽对前列腺癌细胞的细胞毒作用

Observation of cytotoxin effect of prodrugs MTX α peptides on prostatic cancer cells