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实用肿瘤杂志 2011年第4期26卷 403-405页

作者：王志愿孙玲井延涛郑州大学第一附属医院血液内科河南郑州450052

目的探讨VAD方案和VTD方案治疗初治多发性骨髓瘤的疗效。方法回顾性分析43例初治多发性骨髓瘤患者的治疗情况,其中VAD治疗组24例,VTD治疗组19例。结果 VAD治疗组有效率62.5%(15/24),VTD治疗组有效率68.4%(13/19),两治疗组疗效差异无统... 详细信息

目的探讨VAD方案和VTD方案治疗初治多发性骨髓瘤的疗效。方法回顾性分析43例初治多发性骨髓瘤患者的治疗情况,其中VAD治疗组24例,VTD治疗组19例。结果 VAD治疗组有效率62.5%(15/24),VTD治疗组有效率68.4%(13/19),两治疗组疗效差异无统计学意义(P>0.05)。不良反应中,心脏毒性发生率VAD治疗组高于VTD治疗组,差异有统计学意义(P<0.05)。结论对于伴有心脏功能异常的初治多发性骨髓瘤患者应首选VTD方案治疗。

关键词：多发性骨髓瘤/药物疗法多柔比星/投药与剂量多柔比星/类似物和衍生物地塞米松/投药和剂量长春新碱/投药和剂量抗肿瘤联合化疗方案/治疗应用

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Antiproliferative effect of a lectin- and anti-Thy-1.2 antibody-targeted HPMA copolymer-bound doxorubicin on primary and metastatic human colorectal carcinoma and on human colorectal carcinoma transfected with the mouse Thy-1.2 gene

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BIOCONJUGATE CHEMISTRY 2000年第5期11卷 664-673页

作者： Ríhová, B Jelínková, M Strohalm, J St'astny, M Hovorka, O Plocová, D Kovár, M Dráberová, L Ulbrich, K Acad Sci Czech Republ Inst Microbiol CR-14220 Prague 4 Czech Republic Acad Sci Czech Republ Inst Macromol Chem CR-16206 Prague Czech Republic Acad Sci Czech Republ Inst Mol Genet CR-14220 Prague 4 Czech Republic

The aim of this study was to compare the potential of two plant lectins [peanut agglutinin (PNA) and wheat germ agglutinin (WGA)], monoclonal antibody (anti-Thy-1.2), its F(ab')(2) fragments, and galactosamine as targeting moieties bound to the polymer drug carrier to deliver a xenobiotic, doxorubicin, to selected cancer cell lines. We have used primary (SW 480, HT 29) and metastatic (SW 620) human colorectal cancer cell lines and a transfectant, genetically engineered SW 620 cell line with mouse gene Thy-1.2 (SW 620/T) to test the possibility of marking human cancer with xenogeneic mouse gene and use it for effective site-specific targeting. The targeting moieties and doxorubicin were conjugated to a water-soluble copolymer based on N-(2-hydroxypropyl)methacrylamide (HPMA) acting as a carrier responsible for controlled intracellular release of the targeted drug. FAGS analysis showed a strong binding of WGA-FITC to all tested cell lines. Binding of PNA-FITC was considerably weaker. The in vitro antiproliferative effect of lectin-targeted HPMA carrier-bound doxorubicin evaluated as [H-3]TdR incorporation reflected both the intensity of the binding and the different sensitivity of the tested cancer cells lines to doxorubicin. The antiproliferative effect of conjugates targeted with WGA was comparable to that with the conjugates targeted with the anti-Thy-1.2 monoclonal antibody or their F(ab')(2) fragments. The magnitude of the cytotoxic effect of HPMA-doxorubicin targeted with PNA was lower in all tested cell lines. While the conjugates with WGA were more cytotoxic, the conjugates with PNA were more specific as their binding is limited to cancer cells and to the sites of inflammation. Noncytotoxic conjugates with a very low concentration of doxorubicin and targeted with PNA, anti-Thy-1.2, or their F(ab')(2) fragments exerted in some lines (SW 480, SW 620) low mitogenic activity. The Thy-1.2 gene-transfected SW 620 metastatic colorectal cancer cell line was sensitive

关键词：抗体单克隆/毒性抗原 Thy-1/遗传学抗原 Thy-1/免疫学细胞分裂/药物作用结直肠肿瘤多柔比星/类似物和衍生物多柔比星/毒性免疫球蛋白Fab片段/毒性指示剂和试剂淋巴细胞活化甲基丙烯酸盐花生凝集素重组蛋白质类/免疫学 T淋巴细胞/药物作用 T淋巴细胞/免疫学转染肿瘤细胞培养的麦胚凝集素类动物人类小鼠

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ADRIAMYCIN - REVIEW

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JOURNAL OF THE NATIONAL CANCER INSTITUTE 1975年第6期55卷 1265-1274页

作者： CARTER, SK NCI DIV CANC TREATMENTBETHESDAMD 20014

Adriamycin is adding significantly to the effects achieved with cancer chemotherapy. It is the purpose of this editorial to put this drug into current perspective. The following chapters are discussed: preclinical stu... 详细信息

关键词：腺癌/药物疗法乳腺肿瘤/药物疗法癌支气管原/药物疗法多柔比星/投药和剂量多柔比星/副作用多柔比星/类似物和衍生物多柔比星/代谢多柔比星/药理学多柔比星/治疗应用药物评价药物评价临床前药物疗法联合心力衰竭/化学诱导霍奇金病/药物疗法免疫/药物作用白血病淋巴样/药物疗法淋巴瘤大B细胞弥漫性/药物疗法淋巴瘤非霍奇金/药物疗法小鼠近交系有丝分裂/药物作用肿瘤转移/药物疗法肿瘤/药物疗法肿瘤实验性/药物疗法神经母细胞瘤/药物疗法骨肉瘤/药物疗法肉瘤/药物疗法甲状腺肿瘤/药物疗法膀胱肿瘤/药物疗法动物人类小鼠

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Pilot study of the tolerability and toxicity of intravesical valrubicin immediately after transurethral resection of superficial bladder cancer

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UROLOGY 2000年第2期56卷 232-235页

作者： Patterson, AL Greenberg, RE Weems, L Bahnson, R Wajsman, Z Israel, M Sweatman, T Webber, D Gulfo, J Univ Tennessee Coll Med Dept Urol Memphis TN 38104 USA Vet Affairs Med Ctr Memphis TN USA Fox Chase Canc Ctr Philadelphia PA 19111 USA Mississippi Urol Clin Jackson MS USA Univ Pittsburgh Pittsburgh PA USA Univ Florida Med Ctr Gainesville FL USA Anthra Pharmaceut Princeton NJ USA

Objectives. To assess in a pilot study the safety, tolerability, and technical feasibility of administering intravesical valrubicin immediately after transurethral resection of bladder tumors (TURBT) in patients with superficial bladder cancer and to evaluate the optimal dose of valrubicin and its systemic absorption. Methods. Twenty-two patients with recurrent or newly diagnosed Stage Ta or T1 transitional cell tumors received a single dose of 400 mg, 600 mg, or 800 mg of intravesical valrubicin immediately after TURBT, Four patients thought to be at high risk of recurrence were followed up with five additional doses of 800 mg valrubicin, given weekly. Results. The use of valrubicin after TURBT was generally well tolerated, Little evidence was found to suggest a direct relationship among the dose of valrubicin, the time between the end of TURBT and drug instillation, and the occurrence of most bladder symptoms. The most commonly reported adverse events included dysuria (77%), hematuria (59%), and urgency/frequency (23%), Pharmacokinetic analyses revealed that the mean systemic exposure to valrubicin and its metabolites depended on the extent of the TURBT and the damage to the bladder wall. Conclusions. The results of this study indicated that administration of valrubicin immediately after TURBT is feasible. UROLOGY 56: 232-235, 2000. (C) 2000, Elsevier Science Inc.

关键词：投药膀胱内原位癌/药物疗法原位癌/预防和控制原位癌/外科学综合疗法多柔比星/投药和剂量多柔比星/副作用多柔比星/类似物和衍生物多柔比星/治疗应用用药计划表试点项目手术后并发症/诊断手术后并发症/流行病学手术后并发症/病因学挽救疗法治疗结果膀胱/外科学膀胱肿瘤/药物疗法膀胱肿瘤/预防和控制膀胱肿瘤/外科学排尿障碍/诊断排尿障碍/流行病学排尿障碍/病因学老年人人类男(雄)性

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BIOENERGETICS IN CLINICAL MEDICINE - PREVENTION BY FORMS OF COENZYME-Q OF INHIBITION BY ADRIAMYCIN OF COENZYME Q10-ENZYMES IN MITOCHONDRIA OF MYOCARDIUM

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PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA 1976年第12期73卷 4653-4656页

作者： KISHI, T WATANABE, T FOLKERS, K UNIV TEXAS INST BIOMED RES AUSTIN TX 78712 USA

The antitumor agent adriamycin inhibits the succinoxidase system and the NADH [beef heart] oxidase system. Both of the intact mitochondrial enzymes and the pentane extracted preparations are inhibited. Inhibition can be prevented by a molar ratio of coenzyme to adriamycin of 3:1 for coenzyme Q1O (ubiquinone), 5:1 for coenzyme Q7 and 5:1 for coenzyme Q4. Prevention of inhibition was observed in the decreasing order of coenzyme Q1O > coenzyme Q7 > H6 coenzyme Q4 > coenzyme Q4. Adriamycinone was 3 times more inhibitory than adriamycin, which is compatible with a less polar fragment necessary to inhibit the lipoidal coenzyme Q1O. Daunomycinone was not inhibitory at a concentration at which adriamycinone is effective, indicating that the hydroxyl group of the latter could be binding at the receptor, since it should not influence electron transfer of rings B and C.

关键词：柔红霉素/类似物和衍生物柔红霉素/药理学多柔比星/类似物和衍生物多柔比星/拮抗剂和抑制剂多柔比星/药理学 NADH NADPH氧化还原酶类/拮抗剂和抑制剂醌还原酶类/拮抗剂和抑制剂构效关系琥珀酸脱氢酶/拮抗剂和抑制剂泛醌/药理学动物牛

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IMMUNODEPRESSIVE ACTIVITY OF FCE-23762 ON HUMORAL AND CELL-MEDIATED IMMUNE-RESPONSES IN NORMAL MICE - COMPARISON WITH DOXORUBICIN

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AGENTS AND ACTIONS 1992年第3-4期37卷 311-318页

作者： FORNASIERO, MC FERRARI, M GNOCCHI, P TRIZIO, D ISETTA, AM FARMITALIA CARLO ERBA SPA R&DDEPT ONCOL IMMUNOL INFECTVIA GIOVANNI 23I-20014 NERVIANOITALY

FCE 23762 (3'desamino-3'[2(s)methoxyl-4-morpholinyl]doxorubicin) is a new doxorubicin (Dx) derivative that has been selected for clinical testing for its favourable antitumor characteristics, which include efficacy on Dx-resistant tumors. Immunosuppression is an undesirable side-effect of anti-cancer chemotherapy and the therapeutic efficacy of Dx is probably also related to its low immunotoxicity. It was, thus, of interest to compare the effects of FCE 23762 and its parental drug on the immune responses. Both compounds were injected i.v. into healthy mice at equitoxic doses and according to different treatment schedules. Single doses of FCE 23762 and Dx, given concomitant or after the antigen, suppressed at the same degree and dose-dependently the primary anti-SRBC antibody response. Following a multiple treatment schedule after the antigen, FCE 23762 was less suppressive than Dx on both primary and secondary antibody production. Differently from Dx, that was completely inactive, FCE 23762 moderately inhibited DTH reaction to SRBC, only at the highest single dose tested or for repeated administrations given simultaneously or after priming. Both drugs were totally ineffective in delaying skin allograft rejection. Since spleen cellularity and ex vivo lymphocyte proliferation to Con A and LPS were similarly impaired by the two drugs, the differentiated immunodepressive activity of FCE 23762 and Dx cannot be merely associated to their cytotoxic and antiproliferative action. The hypothesis of a selective effect on different regulatory cell subsets and/or immune mechanisms is discussed.

关键词：抗体生成/药物作用 B淋巴细胞/药物作用多柔比星/类似物和衍生物多柔比星/药理学移植物排斥/药物疗法超敏反应迟发型/免疫学免疫细胞/药物作用免疫抑制剂/药理学小鼠近交C3H 小鼠近交C57BL 有丝分裂原/药理学绵羊/免疫学皮肤移植/生理学脾/细胞学脾/药物作用 T淋巴细胞/药物作用动物小鼠

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4′-iodo-4′-deoxydoxorubicin disrupts the fibrillar structure of transthyretin amyloid

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AMERICAN JOURNAL OF PATHOLOGY 2000年第6期156卷 1919-1925页

作者： Palha, JA Ballinari, D Amboldi, N Cardoso, I Fernandes, R Bellotti, V Merlini, G Saraiva, MJ Inst Mol & Cellular Biol Amyloid Unit P-4150 Porto Portugal Inst Super Ciencias Saude Paredes Portugal Pharmacia & Upjohn Nerviano Italy Discovery Res Oncol Nerviano Italy Univ Porto Inst Ciencia Biomed Abel Salazar P-4100 Porto Portugal Univ Hosp Pavia IRCCS Policlin San Matteo Biotechnol Res Labs Pavia Italy Univ Pavia Dept Biochem I-27100 Pavia Italy

Transthyretin (TTR) is a tetrameric protein synthesized mainly by the liver and the choroid plexus, from where it is secreted into the plasma and the cerebrospinal fluid, respectively, Some forms of polyneuropathy, vitreopathy, and cardiomyopathy are caused by the deposition of normal and/or mutant TTR molecules in the form of amyloid fibrils. Familial amyloidotic polyneuropathy is the most common form of TTR amyloidosis related to the V30M variant. It is still unclear the process by which soluble proteins deposit as amyloid. The treatment of amyloid-related disorders might attempt the stabilization of the soluble protein precursor to retard or inhibit its deposition as amyloid;or aim at the resorption of the deposited amyloid. The anthracycline 4'-iodo-4'-deoxydoxorubicin (I-DOX) has been shown to reduce the amyloid load in immunoglobulin light-chain amyloidosis, We investigated 1) whether I-DOX has affinity for TTR amyloid in tissues, 2) determined the I-DOX binding constants to TTR synthetic fibrils, and 3) determined the nature of the effect of I-DOX on TTR fibrils. We report that 1) I-DOX co-localizes with amyloid deposits in tissue sections of patients with familial amyloidotic polyneuropathy;2) I-DOX strongly interacts with TTR amyloid fibrils and presents two binding sites with k(d) of 1.5 x 10(-11) mol/L and 5.6 x 10(-10) mol/L, respectively;and 3) I-DOX disrupts the fibrillar structure of TTR amyloid into amorphous material, as assessed by electron microscopy but does not solubilize the fibrils as confirmed by filter assays. These data support the hypothesis that I-DOX and less toxic derivatives can prove efficient in, the treatment of TTR-related amyloidosis.

关键词：淀粉样蛋白/药物作用淀粉样蛋白/代谢淀粉样蛋白/超微结构淀粉样变性/代谢淀粉样变性/病理学结合部位多柔比星/类似物和衍生物多柔比星/代谢多柔比星/药理学多发性神经病/代谢多发性神经病/病理学前白蛋白/药物作用前白蛋白/代谢前白蛋白/超微结构组织分布人类

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改良CHOP方案治疗老年非何杰金淋巴瘤疗效观察

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中国误诊学杂志 2008年第33期8卷 8134-8135页

作者：梁立新闫秋红令狐锐河南省三门峡市中心医院血液内科 472000

目的:探讨改良CHOP方案治疗老年非何杰金淋巴瘤与标准的CHOP方案疗效观察。方法:对32例老年非何杰金淋巴瘤患者随机分成两组,对照组16例采用标准CHOP方案治疗,治疗组采用改良CHOP方案,3周为1周期,完成3个周期以上作疗效评价。结果:治疗... 详细信息

目的:探讨改良CHOP方案治疗老年非何杰金淋巴瘤与标准的CHOP方案疗效观察。方法:对32例老年非何杰金淋巴瘤患者随机分成两组,对照组16例采用标准CHOP方案治疗,治疗组采用改良CHOP方案,3周为1周期,完成3个周期以上作疗效评价。结果:治疗组完全缓解率高、毒副作用少。结论:改良CHOP方案治疗老年非何杰金淋巴瘤安全性高。

关键词：淋巴瘤,非霍奇金/药物疗法多柔比星/类似物和衍生物环磷酰胺/投药和剂量跃春新碱/投药和剂量泼尼松/治疗应用抗肿瘤联合化疗方案/治疗应用

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以吡柔比星为主的CTOP方案治疗非何杰金氏淋巴瘤11例分析

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中国误诊学杂志 2007年第7期7卷 1637-1638页

作者：赵艳茹周钰刘文河北省秦皇岛市第一医院 066000

我们2005?06－2006—07使用深圳万乐药业公司生产的吡柔比星(THP)进行了非何杰金氏淋巴瘤(NHL)疗效观察,现将结果分析如下。[第一段]

关键词：淋巴瘤,非霍奇金/药物疗法多柔比星/类似物和衍生物环磷酰胺/投药和剂量长春新碱/投药和剂量抗肿瘤联合化疗方案/治疗应用

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吡柔比星膀胱内灌注对膀胱肿瘤术后复发的预防

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中国误诊学杂志 2005年第17期5卷 3307-3308页

作者：廖煜中国长城铝业公司总医院外科河南郑州450041

膀胱腔内灌注化疗是预防膀胱肿瘤复发的一个重要手段.我科自2001～2005年对30例浅表性膀胱肿瘤(Ta期)行经尿道膀胱肿瘤电切术(TURBT)的患者采用吡柔比星进行膀胱内灌注以预防复发,疗效满意,现总结如下.

关键词：胱胱肿瘤/预防和控制膀胱内灌注肿瘤复发,局部/预防和控制多柔比星/类似物和衍生物多柔比星/治疗应用

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