^99mTc标记Laminin—YIGSR肿瘤小显像的实验研究鼠模型

目的探讨^99mTc—YIGsR作为一种新型的肿瘤显像剂在埃氏腹水肿瘤受体显像中的应用价值。方法①制备^99mTc—MAG3-YIGSR探针．以S-乙基-琥珀酰亚胺-巯乙苷肽（S—Acetly-NHS-MAG3）为螯合剂，将^99mTc标记到层黏素多肽片断YIGSR上；②对肿瘤模型组及封闭模型组行^99mTc—YIGSR生物学分布实验；③观察肿瘤模型组、炎症模型组及封闭模型组动物模型显像。结果①反相Sep-PakC18柱层析结果表明，YIGSR可以很好地与S-Acetly—NHS-MAG3偶联，偶联物在室温及中性条件下可完成^99mTc标记，标记率为62形．纯化后放射化学纯度〉95％。室温放置1、2、4h，放射化学纯度分别是91％，86％及81％。未与S—Acetly—NHS-MAG3偶联之YIGSR进行标记时，标记率为4％；②生物学分布结果显示^99mTc—YIGSR在小鼠血液内清除迅速，主要经。肾脏排泄，其次为肝脏；③^99mTcYIGSR静脉注入肿瘤模型组小鼠体内后，15min肿瘤部位有摄取．3h摄取达高峰，肿瘤／对侧肢体比值为11．36．此后显像剂清除较为缓慢，8h时下降至7．50。封闭模型组肿瘤细胞的摄取明显低下，肿瘤／对侧肢体比值是4．61（3h）、0．89（8h）；炎症模型组中，炎症／对侧肢体比值是3．72（3h）、1．29（8h）。与炎症模型组及封闭模型组比较．肿瘤模型组3h、8h肿瘤／对侧肢体的比值明显增高（P〈0．01）。结论通过螯合剂S-Acetly—NHS-MAG。可顺利完成层黏素多肽片段YIGSR的^99mTc标记^99mTcTc—YIGSR用于肿瘤显像具有显像时间早，显像清晰．灵敏度高．特异性强，靶／非靶比值高等特点，是一种有发展前景的新型肿瘤受体显像剂。     

小分子肽99mTc-YIGSR与99mTc-MIBI进行肿瘤显像的对比研究

目的将小分子肽YIGSR经99mTc标记后用于肿瘤受体显像并与99mTc-MIBI进行对比。方法①显像剂制备。YIGSR经双功能螯合剂S-Acetyl-MAG3偶联后室温下进行99mTc标记;99mTc-MIBI采用煮沸法制备。②取昆明种小鼠,每只皮下注射1×106埃氏腹水癌细胞以复制肿瘤模型。③经尾静脉注射显像剂后,将99mTc-YIGSR与99mTc-MIBI显像结果进行比较。结果99mTc-YIGSR肿瘤显像可见肿瘤部位自30 min开始有明显摄取,3 h达高峰,肿瘤/非肿瘤比值(T/NT)为11.36。显像剂清除缓慢,8 h T/NT降至3.01;99mTc-MIBI在肿瘤部位的浓聚明显低于99mTc-YIGSR,其T/NT比值依次为1.40(3 h)及0.55(8 h)。结论99mTc-YIGSR肿瘤显像结果优于99mTc-MIBI,作为一种特异性强的新型肿瘤受体显像剂,具有一定的应用前景。     

荷乳腺癌小鼠c-myc mRNA反义寡核苷酸显像研究

目的 建立99mTc标记寡核苷酸的方法并用于荷乳腺癌小鼠反义寡核苷酸显像研究.方法 利用双功能螯合剂N-羟基琥珀酰亚胺-巯乙苷肽(S-Acetyl-NHS-MAG3)对一段15碱基c-myc mRNA反义寡核苷酸片段进行99mTc标记;对荷乳腺癌昆明种小鼠进行标记反义寡核苷酸生物学分布与显像研究.结果 生物学分布结果表明,相对于正义核酸而言,反义核酸在肿瘤组织中的摄取明显增高(P<0.05).在反义寡核苷酸显像组,肿瘤组织显像剂摄取活跃,肿瘤/肌肉比值最高可达5.5.在正义寡核苷酸显像组及阻断组,肿瘤组织均未出现明显的显像剂浓聚.结论 99mTc标记反义寡核苷酸有望成为一种新的显像剂,在分子水平上用于恶性肿瘤的早期、特异和无创性诊断.     

乳糖化多聚赖氨酸拉咪呋啶在慢性乙型病毒肝炎小鼠体内的肝靶向性研究

目的观察用乳糖化多聚赖氨酸化学修饰后的拉咪呋啶—乳糖化多聚赖氨酸拉咪呋啶在慢性乙型病毒性肝炎小鼠体内的分布情况,探讨Lac-PLL-LA的肝靶向性。方法将LA进行偶联合成后以放射性核素99mTc对偶联物Lac-PLL-LA及LA进行标记,分别通过单光子正电子发射断层显像(SPECT)和γ-放射免疫记数观察其在慢性乙型病毒性肝炎小鼠体内的分布情况。结果(1)慢性乙型病毒性肝炎小鼠注射99mTc标记的LA0.5h、2h及5h后肝脏部位显像模糊不清,各时间点99mTc标记的Lac-PLL-LA组小鼠肝脏部位显像剂的聚集程度均明显高于99mTc标记的LA组,两组显像剂的聚集程度差异有显著性(P<0.01)。(2)小鼠注射99mTc标记的Lac-PLL-LA后1到6h,肝脏/血液和肝脏/骨骼肌放射性比值分别从1.24、2.28上升到4.1、12.1,注射99mTc-LA后1到6h,肝脏/血液和肝脏/骨骼肌放射性比值分别从0.28、0.55上升到0.49、1.36。各时间点99mTc标记的Lac-PLL-LA肝脏/血液和肝脏/骨骼肌放射性比值均高于99mTc-LA,差别有非常显著性(P<0.01)。结论Lac-PLL-LA可在慢性乙型肝炎小鼠肝组织中特异性聚集,偶联后的拉咪呋啶能提高对肝脏组织的亲和力,乳糖化多聚赖氨酸能使LA获得较满意的肝靶向性,提高其抗乙肝病毒的作用。     

锝-99m标记survivin反义寡核苷酸肝细胞癌显像的实验研究

目的研究放射性核素锝99m(99mTc)标记survivin反义寡核苷酸(ASON)显像诊断肝细胞癌的价值。方法用DNA合成仪合成18碱基单链survivinASON,在5′末端经氨基修饰后,以S乙酰基N羟基琥珀酰亚胺巯基乙酰基三甘氨酸(SacetylNHSMAG3)作为螯合剂对survivinASON进行99mTc标记,并对99mTcsurvivinASON在荷瘤(SMMC7721)裸鼠模型体内的生物学分布、肿瘤反义基因显像、肿瘤反义基因抑制显像进行了分析。结果肿瘤组织显像时间早,0.5h即已开始显影。99mTcsurvivinASON在肿瘤组织内的聚集程度随时间延长而逐渐增加,于4h时达到最大,肿瘤/对侧肢体肌肉比值分别为2.48±0.44(体外显像)和3.35±0.57(生物学分布)。正义寡核苷酸(SON)在肿瘤组织内的聚集各时间点均明显低于ASON,差异有统计学意义(P<0.01)。用未标记的survivinASON进行抑制后,99mTcsurvivinASON在肿瘤组织中的聚集明显减少,4h时的肿瘤/对侧肢体肌肉比值降为0.93±0.23,与抑制前的2.48±0.44相比有明显减低(P<0.01)。结论99mTcsurvivinASON可在荷瘤裸鼠模型的肿瘤组织中特异性聚集,为肝细胞癌的特异性诊断提供了一种可能的新方法。     

^99mTc-YIGSR as a Receptor Tracer in Imaging the Ehrlich Ascites Tumor-bearing Mice as Compared with ^99mTc-MIBI

The validity of ^99mTc-YIGSR, a novel receptor radio-tracer, in imaging the Ehrlich ascites tumor was evaluated. YIGSR, a pentapeptide of laminin, was labeled with ^99mTc by using a bifunctional chelator S-Acetly-NH3-MAG3. The MIBI was labeled with ^99mTc by following the kit instruction. The mice of tumor group were intravenously injected 1-2 mCi of ^99mTc-YIGSR or ^99mTc-MIBI via caudal vein, immobilized and imaged under a Gamma camera. The same procedure was performed in mice of blockade group, in which the unlabeled YIGSR was previously injected to block the receptor-recognition sites, and inflammation group serving as control. The reverse-phase Sep-Pak C18 chromatogram was found to have an essentially complete conjugation between YIGSR and S-Acetly-NH3-MAG3. The conjugated YIGSR could be radio-labeled successfully with ^99mTC at room temperature and neutral pH, with a radio-labeling yield of 62%. Without the chelator S-Acetly-NH3-MAG3, the YIGSR was labeled with ^99mTc at an efficiency of 4%. The imagological study revealed obvious tumor accumulation of ^99mTc-YIGSR 15 min after the injection, and the uptake peaked after 3 h with a tumor-to-muscle ratio （T/M） of 11.36. The radio-tracer was slowly cleared up and resulted in a T/M of 3.01 at the 8th h after the injection. As for blocked group, the tumor uptake of radiotracer was significantly lower, with the highest T/M being 4.61 after 3 h and 0.89 after 8 h. The T/M was 3.72 at the 3rd h and 1.29 at the 8th h after the ^99mTc-YIGSR injection in the inflammatory group. The T/M was significantly higher in tumor group than in inflammatory group or control group （P〈0.001）. In the ^99mTc-MIBI group, the T/M was 1.40 at the 3rd h and 0.55 at the 8th h after the injection, which showed a significant difference as compared with ^99mTc-YIGSR （P〈0.001）. It is concluded that YIGSR can be successfully radiolabelled by using S-Acetly-NH3-MAG3. ^99mTc-YIGSR has many advantages in tumor imaging, such as quick and clear visualization, high sensitivity and sp     

99mTC-5-FU免疫纳米粒在荷人胃癌SCID鼠模型体内的分布

目的 探索制备99mTc标记载5-FU抗VEGF单克隆抗体纳米粒(99mTc-5-FU-Ab-NPs)的方法,并观察99mTc-5-FU-Ab-NPs胃癌移植瘤模型体内的分布情况.方法 用改进的Schwarz方法对载5-FU抗VEGF单克隆抗体纳米粒进行99mTc标记,经SephadexG250柱分离纯化,用纸层析法测定标记率与放化纯度;ELISA法和免疫组化法测定标记物的免疫活性;经荷人胃癌鼠静脉注射99mTc-Ab-5-FU-NPs(实验组)及99mTc标记鼠源性多克隆IgG纳米粒(对照组),并于2、6 h行放射免疫ECT显像,用感兴趣区(ROI)技术获得实验组和对照组荷人胃癌鼠全身和肿瘤放射性计数及肿瘤与对侧正常组织(T/NT)的放射性比值;24 h显像后处死鼠,测定体内放射性分布,计算每克组织百分注射剂量率(%ID/g)及T/NT比值.高效液相色谱法检测两组鼠肿瘤组织和血液中5-FU的浓度.结果 制备所得99mTc-5-FU-Ab-NPs标记率为90%～95%,抗体的活性在标记前后无明显下降;荷人胃癌鼠放射免疫显像结果提示静脉注射99mTc-5-FU-Ab-NPs 2 h后肿瘤已显影,随时间延长到6 h更清晰,2和6 h肿瘤组织ID%/g均显著高于对照组;6 h时实验组肿瘤组织ID%/g和肿瘤与血液的放射性比值较2 h时升高;同时,实验组肿瘤组织中5-FU浓度随着时间延长呈持续升高且与对照组5-FU浓度相比有显著性差别.结论 本研究制备所得99mTc-5-FU-Ab-NPs能较好地满足放射免疫显像的要求;抗VEGF单克隆抗体的免疫导向作用可靠,注射后6 h,99mTc-5-FU-Ab-NPs在肿瘤组织中有相对较高的特异性浓聚.     

^99mTc标记抗人喉癌单克隆抗体在荷人喉癌裸鼠模型体内的分布研究

目的 :探索99mTc标记抗人喉癌单克隆抗体 (McAb -Lc)的方法 ,观察99mTc-McAb -Lc在喉癌移植瘤模型体内的分布情况。方法 :应用改良Schwarz法进行99mTc标记McAb -Lc,用γ计数仪测定放射强度 ,计算肿瘤和非肿瘤组织的单位质量摄取放射性活度的百分比 (ID % g)和肿瘤与非肿瘤组织的放射性比值 (T NT)。结果 :改良Schwarz法制备的99mTc -McAb -Lc无毒、无菌、无热原 ,性质稳定 ,标记率在 90 %～ 95% ,抗体的活性在标记前后无明显改变。注射99mTc -McAb -Lc后 ,各时相肿瘤组织ID % g均显著高于注射99mTc-鼠IgG对照组 (P≤ 0 .0 0 3) ,注射99mTc -McAb -Lc后 2h和 6h ,肿瘤组织ID % g和肿瘤与血液的放射性比值 (T B)分别从 4.56± 0 .51、1 .0 3± 0 .1 7增加到 7.84± 1 .46和 1 .84± 0 .30 ,差异有高度显著性 (P≤ 0 .0 0 5)。结论 :改良Schwarz法制备的99mTc -McAb -Lc ,能较好地满足放射免疫显像 (RII)的要求 ,McAb -Lc的免疫导向作用可靠 ,注射后 6h ,99mTc -McAb -Lc在肿瘤组织中有相对较高的特异性浓聚。     

99m Tc-MAG3-ASON的制备及其在荷乳腺癌裸鼠中的分布

目的:探讨99mTc标记的反义寡核苷酸(ASON)的制备及其在荷乳腺癌裸鼠中的分布.方法:一步法合成巯基乙酰三甘氨酰-N-羟基琥珀酰亚胺酯(NHS-MAG3),并与c-erbB2 mRNA互补的5'末端氨基修饰的15个碱基的ASON偶联;随后进行99mTc的标记,并用SephadexG25分离纯化99mTc-MAG3-ASON,并评价其稳定性;最后检测其在荷乳腺癌BALB/c裸鼠体内的分布.结果:99mTc-MAC3-ASON平均标记率为70.6%;纯化后,在室温下放置4h,其放化纯度为94.3%;与人血清孵育后,其放化纯度为93.8%;与血浆蛋白结合率为11.8%.乳腺癌组织的摄取率2h达峰值(6.09% ID/g).结论:以NHS-MAG3为螯合剂制备的99mTc-MAG3-ASON具有良好的稳定性,在乳腺癌部位高浓聚,可望用于肿瘤的显像诊断和治疗.     

~(99m)Tc-MIBI显像预测非小细胞肺癌化疗疗效的应用研究

目的　探讨99mTc -MIBI肺显像在预测非小细胞癌化疗疗效的价值。方法　 36例肺癌患者静脉注射99mTc -MIBI 74 0～ 1110MBq后 2 0min及 2～ 3h分别行早期及延迟显像 ,计算摄取比值T/Ne、T/Nd和清除指数E值。分析化疗有效组与化疗无效组T/Ne、T/Nd和E值之间的区别。结果　两组间的早期摄取比值T/Ne及清除指数E值差异有统计学意义 (P <0 0 5 ) ,T/Nd两组间差异无统计学意义 (P >0 0 5 )。T/N比值及E值与组织学类型之间无明显关系 (P >0 0 5 )。结论　99mTc -MIBI肺肿瘤显像在预测肺癌化疗疗效、为临床制定合适的化疗方案方面具有重要的临床价值。     

An imaging study using laminin peptide 99mTc-YIGSR in mice bearing Ehrlich ascites tumour

Background The YIGSR is a pentapeptide, from the laminin-1 of the β1 chain, which can mediate cell adhesion and bind the 67 kD laminin receptor. The purpose is to evaluate the usefulness of 99mTc-YIGSR, a novel tumour radiotracer, in the receptor imaging of Ehrlich ascites tumour. Methods Using S-Acetly-NH3-MAG3 as chelate, YIGSR, a pentapeptide from laminin, was tagged with 99mTc. 99mTc-YIGSR was detected in the tumour group bearing Ehrlich ascites tumour and blocked group. Tumour, normal, inflammatory and blocked groups were imaged. Results Through reverse phase Sep-Pak C18 chromatogram, it was revealed that YIGSR could conjugate with S-Acetly-NH3-MAG3, and be radiolabelled at room temperature and neutral pH with a radiolabelling yield of 62%, and of 4% without chelate. 99mTc-YIGSR was rapidly cleared from kidney, then liver. The imaging findings showed tumour tissue accumulated initial radioactivity at fifteen minutes after injection in the tumour group, and the uptake increased to peak at three hours with a tumour/muscle ratio (T/M) of 11.36, then cleared slowly to a T/M of 7.50 at eight hours. The tumour uptake of radiotracer in blocked group was significantly lower with T/M of 4.61 at three hours and 0.89 at eight hours. The T/M was only 3.72 at three hours and 1.29 at eight hours after injection in inflammatory group. Compared with inflammatory group and control obstructive group, the ratio of T/M in tumour group was significantly different (P&lt;0.001). Conclusions Using S-Acetly-NH3-MAG3, we radiolabelled YIGSR with 99mTc. 99mTc-YIGSR possesses many merits of tumour imaging: rapid visualization, high sensitivity and specificity, and satisfactory target/nontarget ratio. Our data suggest 99mTc-YIGSR is a promising tumour radiotracer.     

A Comparative Study of ^99mTc-YIGSR and ^99mTc-MIBI Uptake in Tumor Cells

Summary To investigate a new kind of tumor tracer^99mTc-YIGSR developed from a five amino structure (YIGSR) of the Laminin-chain, which can bind to the laminin receptors of tumor specifically, and radiolabeled with MAG₃. (1) Preparation of the^99mTc-YIGSR probe: with S-Acetly-NH₃-MAG₃ as the chelator and with proper reductants YIGSR was labeled with^99mTc; (2) Cell culture and viability measurement: EAC was maintained in RPMI 1640 supplemented with calf serum; the trypan blue exclusion was applied to calculate the cell viability; (3) Study of the cell dynamic: The EAC's uptake of^99mTc-YIGSR and^99mTc-MIBI was observed at 37 °C and 22 °C, respectively. (1) The labeling efficiencies of^99mTc-YIGSR and^99mTc-MIBI were (62±3)% and (96±2)%, respectively; (2) The cell viability was declined with time of incubation; (3) At 37 °C, the EAC'S uptake of^99mTc-YIGSR and^99mTc-MIBI reached the peak of (43.16±2.4)% and (24.4±1.8)% at 60 min, respectively; and at 22 °C, the highest uptake was (26.5±2.1)% and (9.47±1.9)% at 60 min, respectively. Thein vitro study suggests that^99mTc-YIGSR is superior to^99mTc-MIBI in cell uptake and has potential value in tumor imaging. HU Jia, female, born in 1963, Technician     

Synthesis of Metronidazole Derivative and Its Distribution in Sarcoma 180 Bearing Mice

A metronidazole derivative(CM)was synthesized through reaction ofmetronidazole on a carrier,and identified by a series of analyses(e.g.mpdetermination,TLC,paper electrophoresis & UV,IR).The product obtained bylabelling CM with ~(99m)Tc(~(99m)Tc-CM)could concentrate and reach a highconcentration in tumor of mice bearing sarcoma 180(S_(180))within 24 h after ivinjection.The radioactive ratio of ~(99m)Tc-CM retained in tumor was about 5 and10 respectively as compared with that in muscle and brain,suggesting that~(99m)Tc-CM has a strong tumor-localizing effect.Becasue of its lowerconcentration in the brain,its neurotoxicity was low,When CM was complexedwith C~,the product CMCa showed a strong ability to sensitize sarcoma 180to radiation(paper in preparation).These results suggest that CM might be anew type of tumor-localizing and radiosensitizing compound.Further pharma-cological experiments are in progress.     

~(99m)Tc-转铁蛋白在乳腺癌裸鼠的放射性核素显像研究

目的:探讨99mTc-转铁蛋白(Tf)诊断乳腺癌的价值。方法:以99mTc标记转铁蛋白,测定人乳腺癌MCF7细胞膜转铁蛋白受体数及99mTc-Tf与转铁蛋白受体结合的解离常数(Kd)。对人乳腺癌细胞系MCF7裸鼠进行显像研究,获取肿瘤与肌肉、肿瘤与血的单位像素放射性比值。观察99mTc-Tf在BALB/c小鼠体内生物分布。结果:人乳腺癌MCF7细胞膜转铁蛋白受体数为1.95×105/cell,Kd为4.13 nmol/L。人乳腺癌MCF7裸鼠注入99mTc-Tf后12 h,肿瘤/肌肉及肿瘤/血比值分别为4.42±0.46和3.06±0.579。9mTc-Tf主要分布于肝、血及肾脏。结论:99mTc-Tf制备简便,在高表达转铁蛋白受体的肿瘤病变部位聚积。99mTc-Tf为乳腺癌的诊断提供了一种可能的新方法。     

99Tcm-HL91肺癌显像评估非小细胞肺癌放射治疗敏感性的临床价值

目的探讨99Tcm-HL91肺癌显像评估非小细胞肺癌放射治疗敏感性的临床价值.方法对33例拟进行放射治疗的非小细胞肺癌患者静脉注射99Tcm-HL91后4h(早期相)、24h(延迟相)进行断层显像,在断层图像上勾画肿瘤区及对侧正常肺组织的感兴趣区,计算半定量指标早期相摄取比值(ER)及延迟相摄取比值(DR).根据放疗前后的CT影像将患者分为敏感组和不敏感组,将半定量指标与放疗前后的CT检查结果对照.结果肺鳞癌患者敏感组与不敏感组ER及DR值均有显著性差异(P<0.01),不敏感组ER及DR值明显高于敏感组,肺腺癌患者敏感组与不敏感组ER及DR值均无显著性差异(P>0.05),鳞癌患者ER及DR值明显高于腺癌(P<0.01).结论 99Tcm-HL91肺癌显像评估肺鳞癌患者放射治疗敏感性有较大价值,高ER及DR患者对放射治疗不敏感,而对腺癌患者价值有限.     

99Tcm标记葡萄糖99Tcm-EC-DG在S180肉瘤荷瘤小鼠体内的分布研究

目的 研究^99Tc^m-EC-DG在S180肉瘤荷瘤小鼠体内的分布规律，为其用于临床肿瘤显像作基础研究。方法 将S180肉瘤荷瘤小鼠48只分成8组，实验前小鼠禁食8h以上。尾静脉注射^99Tc^m-EC-DG 3．7MBq(100pCi)后5min、15min、30min、1h、2h、4h、8h和24h放血处死，取心、肝、脾、肺、脑、肾、肌肉、骨、小肠、胃、血液和肿瘤等组织或器官，称重并测量其放射性，计算每克组织百分注射剂量率(％ID／g)及肿瘤与血液、肌肉、肺、肝的放射性比值。同时，荷瘤小鼠5只，禁食，尾静脉注射^99Tc^m-EC-DG18．5MBq(500μCi)后相同时间进行显像。结果 肿瘤组织与血液、肌肉、肺、肝的放射性比值随时间的延长逐渐上升，在4h时都超过1．0。显像结果与生物分布实验结果一致，随时间的延长瘤体周围组织放射性逐渐下降，而瘤体在4h时显影清晰。结论 ^99Tc^m-EC-DG在S180肉瘤荷瘤小鼠体内的生物学分布结果表明，其可用于肿瘤的葡萄糖代谢显像。     

Detection of Ischemic Myocardium with a New Hypoxic Tissue Targeting Tracer ^99Tc^m-HL91

Theischemicandviablemyocardiumhasim pairedfunction,however,preservedmetabolicac tivity.Theviablemyocardiummayrecoveritscon tractionfunctionafterrevascularization.Neverthe lessfunctionimprovementmaynotbeachievedinmyocardialscarevenafterasuccessfulreperfusion.Itisimportanttodetectviablemyocardiumbeforerevascularizationtherapyinthepatientswithcoro naryheartdiseasesuchascoronaryarterygraftingbypassorpercutaneouscoronaryintervention.Un fortunatelyasimpleandeffectiveassessmenttech niqueforthispurpos…     

99Tcm直接法标记Angiostatin及其在荷瘤小鼠体内研究

目的:99Tcm直接法标记血管抑素(angiostatin,AS),观察其在荷瘤小鼠体内的生物分布并进行显像,以探讨其在监测肿瘤对抗血管生成治疗的应答中的价值. 方法:氯化亚锡还原法进行AS的99Tcm标记,纸层析法测标记率;用人脐静脉内皮细胞系(ECV304)观察其生物活性;为了明确99Tcm-AS与肿瘤的结合,是否存在受体特异性,我们进行了封闭实验. 在给药前2 h用未标记AS预处理荷乳腺癌EMT6瘤株的BALB/c小鼠,尾静脉注射99Tcm-AS,观察其体内分布并进行显像. 结果:氯化亚锡还原法标记AS可获得较高的标记率(>95%),其抑制内皮细胞生长的生物活性与AS相似. 在荷瘤小鼠体内分布结果显示:肿瘤的摄取率随着时间延长而增加,在注射99Tcm-AS后2～12 h,肿瘤可清晰显像,同时,用未标记AS预先封闭肿瘤可使肿瘤对99Tcm-AS摄取率下降. 结论:99Tcm-AS在荷瘤小鼠体内可浓聚于肿瘤,肿瘤对显像剂的摄取存在一定的特异性;99Tcm-AS有可能在肿瘤抗血管生成治疗疗效评价中发挥作用.