酵母多糖对小鼠腹腔巨噬细胞产生一氧化氮和白细胞介素-1的影响

目的探讨酵母多糖对小鼠腹腔巨噬细胞产生一氧化氮 (NO)和白细胞介素 1(IL 1)的影响。方法将不同剂量的酵母多糖加入体外培养的小鼠腹腔巨噬细胞中 ,取细胞培养上清液根据Griess反应检测NO-2 的量 ,间接反映巨噬细胞产生NO的生成量 ,并用溴化四唑蓝 (MTT)比色法检测上清液中IL 1的生成量。结果酵母多糖可明显促进小鼠腹腔巨细胞产生NO和IL 1,NO的生成量呈现剂量依赖关系。结论酵母多糖可诱导小鼠腹腔巨噬细胞产生NO和IL 1,可能是酵母多糖调节机体免疫功能、杀伤病原微生物和抗肿瘤的重要途径     

花椒根总生物碱抗肿瘤活性研究

目的 探讨花椒根总生物碱的抗肿瘤活性。方法 实验分为6组,各10只,分别灌胃1 000,800,640,512,410,328 g/kg花椒根总生物碱1次（每10 g体质量灌胃0.2 mL）,计算半数致死浓度（LD50）。将60只KM小鼠随机分为正常对照组（A组,等体积生理盐水灌胃）、模型组（B组,等体积生理盐水灌胃）、阳性药物组（C组,氟尿嘧啶20 mg/kg腹腔注射）及花椒根总生物碱高、中、低剂量组（D1组、D2组、D3组,生药100,80,40 g/kg灌胃）,各10只,右上肢腋窝皮下注射单细胞悬液0.2 mL以复制H22荷瘤小鼠模型,建模成功后分别给予相应药物或生理盐水,每天1次,连续10 d。采用酶联免疫吸附（ELISA）法检测小鼠血清中白细胞介素2(IL-2)及肿瘤坏死因子-α（TNF-α）水平;剥取瘤块,称定质量,计算抑瘤率;苏木素-伊红（HE）染色,观察瘤体组织病理形态学;Tunel染色,观察H22肿瘤细胞凋亡情况。结果 与B组比较,C组和D1组小鼠瘤体质量显著减轻（P <0.05）;D1组小鼠血清中IL-2和C组、D1组、D2组小鼠血清中TNF-α水平均显著升高...     

猴头多糖对S180荷瘤小鼠的抗肿瘤作用研究

目的明确猴头多糖对荷瘤小鼠S180肉瘤的抑制作用。方法建立荷瘤小鼠S180肉瘤模型进行研究,猴头多糖给药10d后称重处死,摘取瘤体、脾脏和胸腺,计算抑瘤率和脾脏、胸腺指数。结果①猴头多糖高、中、低三个剂量组的抑瘤率为29.35%、41.50%、19.55%,对照模型组,多糖高、中剂量组与低剂量组的差异分别为(P<0.01)和(P<0.05);②猴头多糖高、中剂量组的脾脏指数对照模型组及环磷酰胺组均有显著性差异(P<0.05),多糖高剂量组的胸腺指数与模型组和环磷酰胺组差异分别为显著(P<0.05)和极显著(P<0.01),多糖中剂量组胸腺指数显著高于环磷酰胺组(P<0.05)。结论①猴头多糖对S180生长具有抑制作用;②猴头多糖高、中剂量组能在免疫器官层次增强机体免疫能力,起到间接抗肿瘤作用。     

灵芝孢子粉多糖Lzps-1的化学研究及其总多糖的抗肿瘤活性

目的研究微波软化灵芝孢子粉中的多糖组分及其抗肿瘤活性。方法用水提取微波软化灵芝孢子粉总多糖，总多糖经分级沉淀得到多糖组分Lzps-C，再采用DEAE-cellulose和Sephadex G-50柱色谱进行分离纯化，用化学和光谱方法分析其结构。结果从微波软化灵芝孢子粉的水提物中分得一个多糖Lzps-1，其平均分子量为8 000，为葡聚糖。微波软化灵芝孢子粉的水提物得到的总多糖Lzps对小鼠Lewis肺癌、小鼠S₁₈₀肉瘤有较好的抑制作用，并能明显提高荷Lewis肺癌小鼠NK活性。结论Lzps-1是首次从灵芝孢子粉中分离得到。Lzps具有抗癌活性。     

螺旋藻多糖硫酸酯抗肿瘤及免疫活性的研究

目的：对螺旋藻多糖硫酸酯（SPSP）的抗肿瘤及免疫活性进行研究。方法：采用四甲基偶氮唑盐（MTT）法观察SPSP体外对多种肿瘤细胞的细胞毒作用；利用小鼠移植性肿瘤模型观察了SPSP体内对小鼠S180肉瘤和Heps肝癌的抑制作用；通过小鼠碳粒廓清速率和血清溶血素实验研究了SPSP对正常小鼠免疫功能的影响。结果：SPSP体外对肿瘤细胞表现有一定的细胞毒作用，体内对小鼠S180肉瘤和Heps肝癌具有显著的抑制作用，SPSP还能提高正常小鼠的碳粒廓清速率和血清溶血素水平。结论：SPSP的抗肿瘤活性可能与其直接细胞毒作用和增强机体的免疫功能有关。     

双参均一多糖TGP-1的分离纯化及其抗肿瘤活性

目的 从双参中分离纯化得到均一多糖,并研究其结构和抗肿瘤活性.方法 双参粗多糖经DEAE-FF和SephadexG-100串联柱色谱分离,得到组分TGP-1.采用HPGPC、IR、UV、PMP-HPLC对TGP-1的结构进行表征,并考察TGP-1对3种不同肿瘤细胞增殖的抑制作用.结果 TGP-1为酸性均一多糖、其相对分...     

2-(1-取代哌啶-4-氨基)喹唑啉类化合物的合成及抗肿瘤活性研究(英文)

本文合成了一系列新结构的2-(1-取代哌啶-4-氨基)喹唑啉衍生物,采用MTT法评价了化合物对5种肿瘤细胞系的抑制活性。研究结果表明:在哌啶环上引入小体积的疏水性烷基取代基,得到的化合物4j～4l、5a、5b和5d具有较强的细胞毒活性,IC50值在微摩尔水平。在小鼠移植瘤模型实验中,化合物4l表现出了较强的体内抗肿瘤活性,在200 mg.kg1的剂量下,对H22肿瘤生长抑制率为72.9%,对Lewis肺癌的抑制率达到了80%。     

车前子多糖抗炎作用机制的实验研究

目的:观察不同浓度车前子多糖(PSP)对各期炎症模型的影响,探讨其可能机制。方法:将小鼠和大鼠随机各分为阴性对照组、阳性对照组和PSP低、中、高剂量组,每组10只。采用二甲苯致耳廓肿胀、醋酸诱发小鼠腹腔毛细血管通透性增高,蛋清致大鼠背部气囊滑膜炎,棉球诱发小鼠肉芽肿,探讨PSP的抗炎作用。称体质量测定各组小鼠耳的炎症肿胀程度及肉芽增生水平,用化学方法检测各组小鼠腹腔洗涤液中的伊文思蓝含量、滑膜炎渗出液容积、渗出液中的白细胞(WBC)计数和肿瘤坏死因子(TNF)-α含量,渗出液和血清中超氧化物歧化酶(SOD)、丙二醛(MDA)含量。结果:与阴性对照组相比,车前子多糖能够抑制二甲苯致小鼠耳廓肿胀、醋酸致小鼠毛细血管通透性的增加,以及小鼠棉球肉芽肿的形成差异有统计学意义(P0.01);其较阴性对照组还能明显减少渗出液容积,降低渗出液中WBC、MDA、TNF-α含量及血清中MDA水平,并能提高渗出液和血清中SOD的活性,差异有统计学意义(P0.05或P0.01)结论:PSP能够减轻各期炎症形成,机制可能与抑制炎性因子的渗出、消除自由基和抑制脂质过氧化有关。     

N-乙酰半胱氨酸对猪急性肝衰竭血清肿瘤坏死因子-α、白介素-1β的影响

目的探讨N-乙酰半胱氨酸（NAC）对猪急性肝衰竭血清肿瘤坏死因子1α、白介素-1β的影响。方法随机将16只雌性中国实验小型猪分为正常对照组（2只），急性肝衰竭组（6只）和药物治疗组（8只）；急性肝衰竭组和药物治疗组分别应用D-氨基半乳糖（1．2g/kg）静脉滴注制备药物性急性肝衰竭动物模型，正常对照组未给予任何处理：药物治疗组给予NAC治疗．急性肝衰竭组同期给予相同剂量的生理盐水：分别测定3组动物血清生化指标以及肿瘤坏死因子、白介素-1β水平。结果急性肝衰竭组和正常对照组相比，血清丙氨酸氨基转移酶（ALT）、天冬氨酸氨基转移酶（AST）和总胆红素（TBil），水平显著升高，PTA显著降低，凝血酶原时间（PT）明显延长，细胞因子肿瘤坏死因子-α，白介素-1β水平显著升高，差异有统计学意义（P〈0．01）。药物治疗组和急性肝衰竭组ALT水平12h（89．5±23．5）U／L和（77．2±18．5）U／L，P〈0.05；24h分别为（242．6±30．5）U／L和（211．1±34．0）U／L，P〈0．05。TBil水平12h分别为（13．1±2．5）μmol／L和（7．8±1．5）μmol／L，P〈0．05；48h分别为（86．2±10．5）μmol／L和（79．7±10．7）μmol／L，P〈0．05。药物治疗组和急性肝衰竭组相比，TNF-α水平24h分别为（19．3±4．2）pg／ml和（24．0±5．3）pg／ml；48h分别为（26．1±3．8）pg/ml和（29．2±8．7）pg/ml、IL-1β24h分别为（15．2±3．4）pg／ml和（18．5±3．6）pg／ml；48h分别为（20．1±5．2）pg／ml和（24．3±6．3）pg／ml，水平均有下降，差异具有统计学意义（P〈0．05）。结论NAC可改善猪急性肝衰竭肝脏功能，可减少体内肿瘤坏死因子-α、白介素-1β炎症细胞因子的生成，抑制炎症反应的快速发展．稳定机体的内环境。     

小鼠树突状细胞体外培养的实验研究

目的研究体外大量扩增小鼠树突状细胞(DCs)的实验方法。方法用细胞因子[肿瘤坏死因子-α(TNF-α)、白介素-4(IL-4)、粒细胞-巨噬细胞集落刺激因子(GM-CSF)]组合体外诱导培养DCs,混合淋巴细胞实验检测DCs的免疫刺激活性。结果培养6-8 d,细胞表面有大量毛刺状突起生长,即DCs;该DCs具有很强的刺激T淋巴细胞增殖的能力,且在T细胞与DCs比值为10∶1时最强。结论 TNF-α、IL-4、GM-CSF组合是诱导体外扩增DCs的较佳方法。     

丹皮多糖-2b降血糖作用的实验研究

目的：研究丹皮多糖－2b（CMP－2b)降血糖作用及作用机制。方法：用小鼠和大鼠建立葡萄糖性高血糖及四氧嘧啶性糖尿病模型，氢化可的松琥珀酸纳（HCSS)诱导胰岛素抵抗，观察丹皮多糖－2b对正常和高血糖模型动物的影响，并测定糖尿病动物SOD、Insulin、GHb、ApoA1等水平。结果：CMP－2b可降低葡萄糖和四氧嘧啶诱发的鼠高血糖，并能升高糖尿病小鼠SOD和大鼠ApoA1水平，降低GHb水平，改善小鼠胰岛素抵抗。结论：CMP－2b可有效地控制实验性高血糖，其降糖机理可能与改善机体对胰岛素的敏感性，促进外周组织对葡萄糖的利用有关。     

Anti-tumor activity of new artemisinin-chalcone hybrids

In an attempt to develop potent and selective anti‐tumor agents, three new series of artemisinin–chalcone hybrids 10a – 10g , 11a – 11g and 12a–12h were designed, synthesized and screened for their anti‐tumor activity against five cell lines (HT‐29, A549, MDA‐MB‐231, HeLa and H460) in vitro. Among compounds 10a–g and 11a–11g , most of them displayed enhanced activity and good selectivity toward HT‐29 and HeLa cell lines with IC₅₀ values ranging from 0.12 to 0.85 µM as compared with DHA (dihydroartemisinin). Compounds 10a and 11a are most active toward HeLa cells with IC₅₀ values of 0.12 and 0.19 µM. The results revealed that the presence of chalcone moiety is beneficial to their activity and selectivity. In addition, compounds 12a ‐ 12h containing a ‘reversed chalcone’ moiety showed only slight improvement in activity than those of DHA.     

猕猴桃根抗肿瘤作用研究

目的评价猕猴桃根提取物的体外、内抗肿瘤活性。方法猕猴桃根活性成分的分离、纯化采用传统的天然产物化学方法,猕猴桃根先用甲醇回流提取,然后用乙酸乙酯、氯仿、正丁醇萃取。不同组分对体外培养的肿瘤细胞增殖的作用采用磺酰罗丹明B方法;猕猴桃根的体内抗肿瘤作用采用小鼠肿瘤和人肿瘤裸小鼠移植瘤模型评价。结果氯仿提取物对肿瘤细胞增殖抑制作用最强,甲醇提取物次之。体内实验证实氯仿提取物有效地抑制小鼠肝癌模型和人肝癌裸小鼠移植瘤模型的生长,抑制率大概在38.0%。结论猕猴桃根提取物有一定的抗肿瘤作用;其活性成分主要存在于极性较小的组分。     

Anti-tumor activity of immunomodulatory peptide alloferon-1 in mouse tumor transplantation model

Alloferons are a group of antiviral and anti-tumor peptides primarily isolated from insects and stimulating cytotoxic activity of natural killer cells in mammals including mice and humans. Alloferon-1 is currently used in the treatment of persistent viral infections; however its anti-tumor potential needs further preclinical assessment. Here we evaluate alloferon-1 anti-tumor activity in DBA/2 mice grafted with syngenic P388 murine leukemia cells. Alloferon-1 was applied alone or in combination with conventional cytotoxic chemotherapy (a mixture of cyclophosphamide, doxorubicin and vincristine). Alloferon-1 monotherapy demonstrated moderate tumoristatic and tumoricidal activities comparable with low dose chemotherapy. When alloferon-1 and the cytotoxic drugs were combined in a regime of pulse immunochemotherapy the combination anti-tumor activity evidently exceeded that of the treatments applied individually.     

Anti-tumor activity of Titanocene Y in xenografted Caki-1 tumors in mice

The benzyl-substituted unbridged titanocene bis-[(p-methoxybenzyl)cyclopentadienyl] titanium(IV) dichloride (Titanocene Y) was tested in vitro against human renal cancer cells (Caki-1), in which it showed an IC50 value of 36 x 10 mol/l. Titanocene Y was then given in vivo in doses of 10, 20, 30, 40 and 50 mg/kg on 5 consecutive days to Caki-1-bearing mice, and it showed concentration-dependent and statistically significant tumor growth reduction with respect to a solvent-treated control cohort. The maximum tolerable dose of Titanocene Y was determined to be 40 mg/kg and it showed significantly better tumor volume growth reduction than cisplatin given at a dose of 2 mg/kg. This superior activity of Titanocene Y with respect to cisplatin will hopefully lead to clinical tests against metastatic renal cell cancer in the near future.     

Antitumour activity of Angelica archangelica leaf extract

BACKGROUND: The purpose of this study was to examine the effect of a leaf extract from A. archangelica on the growth of Crl mouse breast cancer cells in vitro and in vivo. Materials and METHODS: The antiproliferative activity of the extract was measured by 3H-thymidine uptake in the Crl cells in vitro. Twenty mice were injected with the Crl cells, and 11 of them were fed A. archangelica leaf extract, and the progress of the tumours was followed. RESULTS: The leaf extract was mildly antiproliferative on the Crl cells with an EC50 of 87.6 microg/ml The antitumour activity of the extract was expressed in the mice by marked reduction in tumour growth. In the experimental animals, 9 out of 11 mice developed no or very small tumours, whereas control animals, not receiving the extract, developed significantly larger tumours (p<0.01), as estimated by Mann-Whitney U-test. The antitumour activity of the leaf extract could not be explained by the antiproliferative activity of furanocoumarins present in the extract. CONCLUSION: The results demonstrate the antiproliferative activity in vitro and antitumour activity in vivo of a leaf extract from A. archangelica     

全蝎蛋白抗肿瘤活性研究

目的比较全蝎蛋白超滤分段后各分子量段对肺腺癌细胞A549的抑制作用,筛选有效部分。方法采用蛋白酶酶解法提取全蝎总蛋白,利用80%乙醇沉淀并利用改良Lowry法测定蛋白质含量,再经超滤进行分段、冷冻干燥后通过MTT法研究其对肺腺癌细胞(A549)的抑制作用。结果 80%乙醇沉淀全蝎蛋白具有较高的选择性,其<3 kDa分子量段对A549细胞无抑制作用,3~10 kDa分子量段对A549细胞的抑制作用不明显,>10 kDa分子量段对A549细胞具有显著的抑制作用,IC_(50)=204.7μg·mL~(-1)。结论 80%乙醇沉淀物中蛋白质含量为89.4%;>10 kDa分子量段全蝎蛋白对A549细胞具有显著的抑制作用。     

Anti-tumor activity of paclitaxel through dual-targeting lipoprotein-mimicking nanocarrier

In the present study, we devised a strategy that paclitaxel (PTX) with lipid and octadecylamine were prepared to lipid nanoparticle (PTX-LNP) with positive charge, folic acid-modified bovine serum albumin (FB)-coated surface of PTX-LNP through electrostatic attraction and generated the lipoprotein-mimicking nanocomplex (FB-PTX-LNP) for dual-targeting therapy. Bovine serum albumin (BSA) was used as the protein model due to its specific targeting to tumor by increased transendothelial gp60-mediated transport and increased intratumoral accumulation as a result of the secreted protein, acidic and rich in cysteine (SPARC)–albumin interaction. The further conjugating folic acid to BSA achieved the dual active targeting. In vitro cytotoxicity tests suggested FB-PTX-LNP and BSA-PTX-LNP exhibited significantly higher cytotoxic activity against MCF-7 and HepG2 cells compared to PTX-LNP. The cellular uptake experiments indicated that FB-coumarin-6-LNP modified with dual-targeting had a faster and greater cellular uptake when compared to BSA-coumarin-6-LNP and coumarin-6-LNP by MCF-7 cells. Thus, both BSA and FA did play roles in in vitro cytotoxicity and cellular uptake. Furthermore, the targeting ability and therapeutic efficacy of FB-PTX-LNP were assessed in vivo. FB-PTX-LNP produced very marked targeting ability and anti-tumor activity in MDA-MB-231 tumor-bearing mice. These results indicate the protein–lipid nanocomplex FB-PTX-LNP is a potential nanocarrier for Paclitaxel dual-targeting to tumor.     

中药材挥发油类抗肿瘤活性研究进展

中药材挥发油是一类与水不混溶,具挥发性和特殊气味的中药,在肿瘤的预防和治疗中具有重要作用。挥发油类的抗肿瘤药理作用,主要通过抗肿瘤作用机制,如抑制增殖、诱导凋亡、增强机体免疫和调控、抗氧化、酶诱导、抑制突变、调节多药耐药性和各种成分的协同作用,保证了其抗肿瘤作用的充分发挥。近年来,关于含挥发油类的中药材的抗肿瘤研究日益增多,在医药方面已显示出广阔的应用前景,因此本文对中药材挥发油类抗肿瘤的研究进展进行了综述。