AIM To investigate the effects of taxol on SMMC-7721 human hepatoma and its mechanisms. MLETHODS In vitro cell growth was assessed by trypan blue exclusion method. Experimental hepatoma model was established by seeding SMMC-7721 cells subcutaneously into Balb/c (nu/nu) nude mice. In vivo tumor growth was determined by measurement of tumor diameter with Vernier calipers. The syntheses of DNA,RNA and protein were analyzed by incorporation of 3H-thymidine, 3H-uridine and 3H-leucine respectively. Using light and electron microscopes to observe the morphological changes of cells including mitosis and apoptosis.RESULTS Taxol was effective against SMMC 7721 human hepetoma cell growth in the ranges of 2.5 nmol/L - 10 nmol/L with mitotic arrest and apoptosis in vitro. DNA, RNA and protein syntheses in cells were also obviously suppressed by in vitro treatment of taxol for 72 h. Taxol at 2.5 nmol/L reduced 3H-thymidine uptake to about 34% of the control value (P＜0.05). Increasing the dose of taxol to 20 nmol/L resulted in a greater decrease in 3Hthymidine incorporation to 60% of the control value (P＜0.01). At a concentration of 20 nmol/L, the 3H-uridine and 3H-leucine uptakes were reduced to 52% (P＜0.05) and 63%(P＜0.01), respectively. In vivo, taxol significantly inhibited SMMC-7721 tumor growth at 10 mg/kg, i.p., once daily for 10 d. A more than 90% decrease in tumor volume was observed by day 11 (P＜0.01) similarly with mitotic arrest and cell apoptosis.CONCLUSION Taxol has a marked anticancer activity in SMMC-7721 human hepatoma both in vitro and in nude mice. Its mechanisms might be associated with mitotic arrest, subsequently,apoptosis of the hepatoma cells. No obvious toxicity was observed with in vivo administration of taxol.

抗癌药紫杉醇的神经毒性和耳毒性

紫杉醇(Paclitaxel,商品名Taxol)是从红豆杉科红豆杉属植物中提取得到的二萜类化合物,分子式为C47H51NO14.1963年,美国化学家瓦尼和沃尔从一种生长在美国西部大森林中的太平洋杉的树皮和木材中分离到紫杉醇粗提物,在筛选实验中发现其具有很强的抗肿瘤活性.

紫杉醇注射液致过敏性休克1例

病例:患者,女,72岁,因"乳腺癌根治术后化疗",于2008年2月18日入我院治疗.患者既往无药物过敏史,患高血压、冠心病10余年.2008年2月21日给予紫杉醇注射液(商品名:特素,批号:070806,规格:30mg/支)240mg加入氯化钠注射液250mL静脉滴注.用药1分钟后,患者出现憋气,口唇青紫,面部潮红,脉搏加快等症状.

抗癌植物药紫杉醇研究进展与动态

紫杉醇(paclitaxel,商品名Taxol)是一种在红豆杉科(Taxaceae L.)红豆杉属(Taxus L.)生长缓慢的长绿乔木中分离提取到的天然化合物.紫杉醇是目前全世界公认治疗肿瘤的有效药物,也是全球抗癌药物研究的热点.近年来,紫杉醇无论在药理活性、分离测定方法、提取纯化技术、化学结构修饰、类似物的化学结构及其生物活性和主要活性物质

紫杉醇前药的开发与临床研究进展

紫杉醇(Paclitaxel,Taxol),紫杉-11-烯-9-酮,5β环氧化-1,2α,4,7β,10β,13α-六羟基-4,10-二乙酸酯-2-苯甲酸酯-β[(2'R,3'S)-N-苯甲酰-3'-苯基异丝氨酸酯],分子式C47H51,NO14,相对分子质量为853.9,是从太平洋杉树Taxuabrevifalia的树皮中分离得到的一种微管稳定剂[1],对多种癌症具有明显的治疗作用.

卡培他滨合成路线图解

卡培他滨(capecitabine,1),化学名为5'-脱氧-5-氟-N-[(戊氧基)羰基]胞嘧啶核苷,是罗氏公司研制的5-氟尿嘧啶(5-FU)前体药物.1998年9月获美国FDA批准,临床用于治疗对紫杉醇(paclitaxel)和多柔比星(adriamycin)等药物无效的晚期原发性或转移性乳腺癌,2003年4月以相同适应症在日本上市.2001年FDA批准本品用于治疗转移性结肠直肠癌[1].

Objective: To study the effects of paclitaxel on macrophage activation. Methods:Mouse macrophages were isolated by peritoneal lavage and cultured in RPMI 1640 medium according to the following groups: paclitaxel (5μmol/L) group, IFN-γ (5U/L) group, paclitaxel (5μmol/L) and IFN-γ (5U/L) combination group, and control group(without paclitaxel and IFNγ) .24 hours later, supematants were collected for nitric oxide(NO) assessment using the Griess reagent, and ttanor necrosis factor-α(TNF-α) assessment using the enzyme linked immunosorbent assay. Antibody-dependent cell-mediated cytotoxicity(ADCC) of the macrophages was assessed using the method of hemoglobin-enzyme release assay (Hb-ERA). Results: Paclitaxel induced the production of higher levels of NO(8.86 ± 1.16μmol/L) and TNF-α(120.2 ± 10.2pg/ml) ,and enhanced the ADCC of macrophages[ (20.61 + 1.13)% ]. The differences were significant compared with the control group[no NO and TNF-α detected,ADCC (15.37 + 1.93)% ](P ＜ 0.01). Paclitaxel and IFN-γ in combination induced the production of higher levels of NO(22.85 ± 0.91μmol/L) and TNF-α(358.6 ± 27 .5pg/ml), and enhanced the ADCC of macrophages[ (42.49 + 3.09) % ]. The differences were significant compared with paclitaxel or IFN-γ[NO 8.09 ± 1.13μmol/L, TNF-α1 24.8 + 9.6pg/ml, ADCC(23.32 ± 2.63) % ] alone (P＜0.01). Conclusion: These findings indicate that paclitaxel can promote NO and TNF-α production,enhance ADCC of macrophages, and induce macrophage activation. The active effects are more significant with paclitaxel and IFN-γcombination.

紫杉醇引起过敏性休克的防治经验

病例介绍患者,男,59岁,因"胃低分化腺癌ⅢA期根治术后半月"于2009年2月6日入院.患者于2008年11月下旬无明显诱因出现上腹部不适,伴剑突下隐痛,未予重视.后因症状渐加重,于2008年1月7日行胃镜检查,病理示胃窦低分化腺癌.

紫杉醇纳米粒制剂的含量测定方法研究

紫杉醇(Paclitaxel,Taxol)是从红豆杉属植物紫杉的树干和树皮中提取的一种天然抗癌药物,临床研究已经证实了紫杉醇在抗多种实体肿瘤,包括乳癌、晚期卵巢癌、肺癌、脑部和颈部肿瘤以及急性白血病等方面都有重要而显著的作用[1].

紫杉醇放疗增敏在头颈部肿瘤治疗中的临床运用

紫杉醇(paclitaxel,商品名taxol泰素)是一种由红豆杉属植物的树皮和针叶中提取的化合物,是近年来研究开发出的化学结构新颖、作用机理独特的新型抗肿瘤药.

化疗药物紫杉醇在神经病理性痛发生中的作用

1. 化疗药物紫杉醇的概述紫杉醇(Paclitaxel,商品名为Taxol~R)是一种可从紫杉属植物Taxus brevifolia的树皮中提取的多萜醇类单体药物成分(图1).对紫杉醇生物活性的研究始于上个世纪七十年代早期,随着研究的深入,人们发现紫杉醇可以中断细胞分裂周期.