赖氨酰谷氨酸二肽的抗肿瘤活性研究

目的研究二肽Lys-Glu(Vilon)的抗肿瘤活性。方法用液相法人工合成了抗肿瘤二肽Vilon,分子量为275.3。用细胞计数法和MTT法测定Vilon对人肠癌LOVO,人胃癌MKN45和人肝癌QGY77033种肿瘤细胞生长的抑制作用,以及对人体正常细胞生长的影响;并对其进行了体内实验。结果Vilon对体外培养的LOVO,MKN45和QGY7703细胞具有剂量依赖性抑制作用,但对人正常白细胞无明显抑制作用。体内抑瘤实验表明,Vilon对小鼠肝癌H22的生长有抑制作用,有效剂量为15mg.kg-1,当使用高剂量30mg.kg-1时,对小鼠移植性肿瘤肝癌H22的抑瘤率达0.60以上,且具有剂效关系。结论Vilon具有明显的体外、体内抗肿瘤活性。     

扇贝多肽对环磷酰胺抗肿瘤的增效作用

目的探讨扇贝多肽对环磷酰胺(CTX)抗肿瘤作用的增效作用。方法无菌抽取荷H22小鼠腹水,于小鼠右前肢腋部皮下接种瘤液0.2mL/只。小鼠随机分为对照组、环磷酰胺组(CTX 10 mg.kg-1)、扇贝多肽大、中、小剂量组(1000,500和250 mg.kg-1)和扇贝多肽大、中剂量分别与CTX联用药组共7组。扇贝多肽连续灌胃给药10d,CTX连续腹腔注射10d,对照组给于同体积的生理盐水。末次给药24h后处死动物,解剖称体重、瘤重,计算抑瘤率,比较单用扇贝多肽与联合用药的药效差别。结果实验表明,单用扇贝多肽大、中、小剂量对H22均无明显抑瘤作用。在同样剂量下分别与CTX联用后,扇贝多肽大、中剂量组抑瘤率分别为55.9%和52.9%,优于单用CTX组的抑瘤效果,说明扇贝多肽与CTX联合应用对肿瘤的抑制有较好的协同作用。结论扇贝多肽能增强CTX的抗肿瘤作用。     

脱氧氟尿苷针剂对小鼠移植性肿瘤的抑制作用

目的 观察脱氧氟尿苷DFUR针剂对动物移植性肿瘤的实验治疗作用。方法 选用肉瘤S180、肝癌HepS、白血病L615和艾氏腹水癌ECA等四株小鼠移植性肿瘤，观察注射途径下脱氧氟尿苷DFUR的抗肿瘤作用。结果 腹腔、静脉或口服给药，DFUR对S180的抑瘤率均大于80％。腹腔给药对HepS的抑瘤率为78％，对L615和ECA的生命延长率为515％和202％。腹腔给药对S180的化疗指数分别为DFUR2．8，FU1．3，FT2071．4和FUDR1．5。结论 无论是静脉、腹腔或口服给药，脱氧氟尿苷DFUR对多种小鼠肿瘤均有明显的抑制作用。与FU，FT207和FUDR相比，DFUR可在较低的毒性下显示更好的抗肿瘤作用。     

抑癌因子腹腔注射对小鼠实体瘤生长的抑制作用

目的：观察抑癌因子腹腔注射对小鼠实体瘤生长的影响。方法：小鼠右腋皮下分别接种肝癌和S180肉瘤细胞，24小时后，实验组小鼠腹腔注射抑癌因子，对照组小鼠腹腔注射生理盐水，连续七天，第八天处死小鼠，剥离出瘤块称重。结果：肝癌和S180小鼠肿瘤平均重量为0．65g和0．64g，相应的对照组小鼠肿瘤的平均重量为1．41g和．134g，P值均小于0．01，抑瘤率分别为53．9％和52．2％。结论：抑癌因子腹腔注射对肝癌和S180小鼠实体瘤的生长有明显的抑制作用，其抑癌机理可能是通过启动细胞凋亡信号传递途径，诱导和加速癌细胞的凋亡。     

螺旋藻多糖抗癌作用的实验研究

本实验对螺旋藻多糖的抗癌作用进行了体内外实验研究和作用机理探讨。以０．３～１．５ｇ．Ｌ＾－１对Ｂ３７乳腺癌细胞的抑制率最高可达６８．０％,对Ｋ５６２白血病细胞抑制率为４６．０％,对两细胞的１Ｃ５０分别为１．４８和１．５６ｇ．Ｌ＾－１。当螺旋藻多糖以３００,１５０和７５ｍｇ．ｋｇ＾－１灌胃给药时,对小鼠Ｓ１８０肉瘤的抑瘤率分别为５５．２％,４４．６％和３３．８％;对Ｈ２２小鼠肝癌的抑癌的抑瘤率分别为     

生血宝合剂对环磷酰胺所致小鼠白细胞减少症的影响

目的观察生血宝合剂对环磷酰胺(CTX)所致小鼠白细胞减少症的影响。方法小鼠连续给药10d,并于第6和7d各腹腔注射CTX(100mg.kg-1)1次造成外周血白细胞减少。比较给药组和模型组小鼠外周血白细胞数量、股骨中骨髓有核细胞数及肝、脾、胸腺造血免疫器官脏器系数。结果与对照组比较,连续2d腹腔注射100mg.kg-1 CTX,小鼠外周血白细胞数、骨髓有核细胞数显著减少,肝脏、脾脏和胸腺系数明显降低。生血宝合剂给药组均使小鼠外周血白细胞数、骨髓有核细胞数显著增多,但对肝脏、脾脏和胸腺系数的升高差异无统计学意义。结论生血宝合剂对CTX所致小鼠白细胞减少症有明显的治疗作用。     

银耳孢子多糖体内抑制肿瘤作用的研究

目的：研究银耳孢子多糖对小鼠U14宫颈癌、H22肝癌、S180肉瘤的抑制作用。方法：采用肿瘤抑制率评价银耳孢子多糖在1、6和12mg／kg3个剂量时，对肿瘤的抑制作用。结果：银耳孢子多糖在3个剂量下，对小鼠U14宫颈癌、H22肝癌、S180肉瘤均有一定的抑制作用。对于U14官颈癌，在1mg／kg剂量时，间隔给药抑瘤效果最明显，抑瘤率为43．6％，与对照组相比差异显著；对于H22肝癌，在6mg／kg剂量时，间隔给药抑瘤效果最明显，抑瘤率为72．3％，与对照组相比差异显著；对于S180肉瘤，在6mg／kg剂量时，间隔给药抑瘤效果最明显，抑瘤率为84．9％，与对照组相比差异显著。结论：银耳孢子多糖对小鼠U14宫颈癌、H22肝癌和S180肉瘤，均有较好的抑制作用。     

沙培林对H22小鼠肝癌抑瘤作用的实验研究

目的观察沙培林对如2小鼠肝癌抑瘸作伟及剂量皴应关系。方法H22小鼠肝癌腹水瘤移柏接种后,随机分组,腹腔分别注射沙培林250pg·k^-1、500μg·lkg^-1、750μg·lkg^-1、0．9％氯化纳(NS)、环磷酰胺(CTX)．记录各组平均生存期、计舅生命延长率。结果CTX组生命延长率为29．2％、沙培林各剂量组生命延长率分别为84．6％,92．3％、96．2％,与CTX组比较均有显差异(P<0．05)。结论沙培林对H丝小鼠肝癌有肯定的的瘤作用．且明显优于CTX。沙培林不同剂量组问生命延长率无明显剂量效应关系。     

苦豆子生物碱衍生物9002#急性毒性及体内抑癌活性的实验研究

目的使用昆明种小白鼠对苦豆子生物碱衍生物9002#进行急性毒性实验.使用IRM-2纯系小鼠进行淋巴瘤和乳腺癌的体内抑癌活性的实验研究.方法急性毒性实验以腹腔给药(ip)方式给药,测定小鼠LD50.抑癌试验建立荷瘤小鼠模型,IP方式给予2个不同剂量的药物水溶液,观察瘤重和体重,测定抑瘤率.结果经实验测定9002#的LD50为4362±810mg*kg-1,毒性较低,经重复试验9002#确有明显的抑癌作用.对淋巴瘤,剂量50mg*kg-1×10,抑瘤率50.3%～53.5%(P＜0.01),150mg*kg-1为31.3%～35.7%(P＜0.05);对乳腺癌,剂量50mg*kg-1×10,抑瘤率为57.1%(P＜0.01),150mg*kg-1为48.6%(P＜0.01).结论苦豆子生物碱衍生物9002#属低毒而有抑癌活性的化合物,对IRM-2纯系小鼠移植肿瘤有明显的抑制作用,以50mg*kg-1×10剂量组对淋巴瘤和乳腺癌抑制效果最显著,值得深入研究.     

2种给药方式的胂酸基乙酸对H_(22)肝癌荷瘤小鼠的抑瘤作用比较

目的 :比较不同给药方式的胂酸基乙酸 (ASAC)对H22 肝癌移植瘤在小鼠体内生长的抑制作用。方法 :采用腹腔注射和静脉注射2种给药方式 ,分别在小鼠右腋皮下接种肝癌H22 细胞后 ,随机将其分为5组 ,分别注射生理盐水、环磷酰胺及不同剂量的ASAC ,观察癌细胞株的成瘤率、受试物对H22 肝癌荷瘤小鼠的抑瘤作用及其对小鼠脏器的影响。结果 :与腹腔注射给药方式比较 ,静脉注射给予ASAC高、中、低剂量后均产生显著抑制肿瘤生长作用 ,其抑瘤率分别为46. 59 %、46 .31 %和32 .48 % ;2种给药方式的ASAC低剂量组小鼠脾重指数均有升高 ,但静脉注射给予ASAC高剂量组出现了小鼠中毒死亡。结论 :与腹腔注射给药方式比较 ,ASAC静脉注射给药方式的抑瘤作用更好。     

抗人绒毛膜促性腺激素β—亚基单克隆抗体杂交瘤的建立

用绒毛膜促性腺激素（HCG）及其β亚基（HCG-β）脾内免疫BALB/C小鼠后，取脾细胞与sp2/o小鼠骨髓瘤细胞融合，其融合剂PEG终浓度为37%，融合率100%，经反复筛选，克隆化后，获得三株持续分泌抗HCG-β单克隆抗体杂交瘤-E2、E12和F6，经亚型鉴定E2和E12为IgG1,F6为IgG2b。该杂交瘤所分泌的抗体公能与HCG和HCG-β特异性结合，而不与促共同体素（hLH)、促卵泡素（hFSH)和促甲状腺素（hTSH)发生交叉反应，并经ELISA抑制试验证实，单克隆抗HCG-β具有高度的特异性，可以为早孕和妇科肿瘤的特异性诊断提供原料，本文还对免疫程序各融合方法进行了讨论。     

PHARMACOLOGICAL COMPARISON OF HUMAN ISOLATED DIGITAL ARTERIES AND METACARPAL VEINS

1 The responses of human digital arteries and metacarpal veins obtained postmortem to various pharmacological agents have been tested. 2 pD₂ values for potassium chloride and barium chloride were found to be greater in arteries than in veins. 3 There was no difference between the arteries and veins in the pA₂ values for phentolamine as an antagonist of either noradrenaline or phenylephrine. pD₂ values for noradrenaline however, were significantly higher in the veins than in the arteries, whereas pD₂ values for phenylephrine in the two tissues were not significantly different. This raises the possibility of there being differences in the populations of a-adrenoceptors in the two tissues. 4 Differences were found between arteries and veins in the contractile and relaxant responses to histamine and in the antagonism of the responses to histamine by cimetidine and mepyramine, thereby suggesting differences in the populations of Hi-and H₂-receptors in these tissues. 5 No differences were found in the responses of arteries and veins to serotonin or in the antagonism of the response to this agonist by phentolamine. 6 Isoprenaline produced relaxant responses in veins (in which tone was induced with 30 mmol/1 potassium chloride) but not in arteries. 7 Dopamine produced very weak relaxant responses in preparations in which tone was induced using 30 mmol/1 potassium chloride. The mean £max value for this response was significantly greater in veins than in arteries. 8 Slight relaxant responses to acetylcholine were seen in veins and arteries precontracted with 30 mmol/1 potassium chloride. The mean £max value was significantly greater in veins than in arteries. 9. It is concluded that human digital arteries and metacarpal veins have differing pharmacological receptor populations and probably also differ in their non-receptor mediated contractile mechanisms.     

国产冻干人凝血酶原复合物质量标准的研究

目的通过对国产人凝血酶原复合物 (PCC)质量的研究 ,建立与国际接规的质量标准。方法用人凝血因子Ⅱ、Ⅶ、Ⅸ、Ⅹ (FⅡ、FⅦ、FⅨ、FⅩ )浓制剂国家标准品 ,采用一期法测定国内用不同原料制备的PCC中FⅡ、FⅦ、FⅨ、FⅩ的效价 ;用正常人血浆作标准 ,用凝固法检测PCC的总效价及PCC中的肝素。结果用血浆作原料提纯制备的PCC ,FⅣ的效价能达到 1 0IU/ml以上 ,FⅦ效价最低 ;用组分Ⅲ作原料 ,FⅣ活性损失很大 ,只有 2 / 7批次能达到 1 0IU/ml;而FⅦ效价最高。无论用何种原料 ,FⅡ和FⅩ活性均能保持在一定水平。结论从血浆中直接提纯制备PCC ,能有效地保持FⅣ活性 ,各项指标易达到国外同品种的质量标准     

论人体生命的三重品格

本文讨论的是人体生命观的问题,从人的本质来看,人体生命与其它生命体有着原则的区别。人体生命是神圣品格、质量品格和价值品格的辩证统一。人体生命三重品格以价值品格为核心,密不可分地联系在一起。片面强调人体生命的质量品格或神圣品格,必然使人们在理论和实践上陷入二难境地。     

Human embryonic stem cells and lung regeneration

Human embryonic stem cells are pluripotent cells derived from the inner cell mass of preimplantation stage embryos. Their unique potential to give rise to all differentiated cell types has generated great interest in stem cell research and the potential that it may have in developmental biology, medicine and pharmacology. The main focus of stem cell research has been on cell therapy for pathological conditions with no current methods of treatment, such as neurodegenerative diseases, cardiac pathology, retinal dysfunction and lung and liver disease. The overall aim is to develop methods of application either of pure cell populations or of whole tissue parts to the diseased organ under investigation. In the field of pulmonary research, studies using human embryonic stem cells have succeeded in generating enriched cultures of type II pneumocytes in vitro. On account of their potential of indefinite proliferation in vitro, embryonic stem cells could be a source of an unlimited supply of cells available for transplantation and for use in gene therapy. Uncovering the ability to generate such cell types will expand our understanding of biological processes to such a degree that disease understanding and management could change dramatically.     

Human Herpesvirus 6 (HHV-6) Induces Dysregulation of Glutamate Uptake and Transporter Expression in Astrocytes

Human herpesvirus 6 (HHV-6) infects and establishes latency in the central nervous system (CNS). Reactivation of latent HHV-6 has been associated with neurologic diseases including epilepsy and multiple sclerosis (MS). In vivo, HHV-6 has been localized to astrocytes and can infect human astrocytes in vitro, suggesting that this virus may have a tropism for glial cells and may affect glial cell function. An essential role of astrocytes in the CNS is active maintenance of the excitatory neurotransmitter glutamate. Dysregulation of glutamate has been implicated as a potential mechanism of disease in both epilepsy and MS. Both disorders have demonstrated elevated glutamate in CSF and may be associated with dysregulation of glutamate signaling, uptake, and metabolism. This study demonstrates dysregulation of glutamate uptake in human astrocytes infected with both variants of HHV-6, A and B, with differential effects of HHV-6 in acute and persistently infected cells. Whereas astrocytes acutely infected with HHV-6 demonstrated increased glutamate uptake, cells persistently infected with HHV-6A and HHV-6B demonstrated impaired glutamate uptake. Functional dysregulation of glutamate uptake was associated with early increases in mRNA and protein expression of the glial glutamate transporter EAAT-2 followed by a sustained decrease in mRNA expression in astrocytes infected with both HHV-6A and HHV-6B. Dysregulated glutamate uptake and transporter expression suggests a mechanism for dysregulation of glutamate levels in vivo and a potential mechanism for virus-associated neurologic disease. This work was supported by the National Institutes of Health/National Institute of Neurological Disorders and Stroke. JF was supported by the MS Society of Canada.     

Resolution of human mercapt- and nonmercaptalbumin by high-performance liquid chromatography

Gel-exclusion high-performance liquid chromatographic (HPLC) analysis of human serum albumin (HSA) on PGP 2000 column (0.10 M sodium phosphate buffer, 0.30 M NaCl, pH 6.86) showed at least two peaks, the principal component corresponding to human mercaptalbumin (HMA) and the second one to human nonmercaptalbumin (HNA). Mechanism for the separation of HMA and HNA might be due to weak resin-HSA interaction. HPLC analysis of bovine plasma albumin (BPA) showed a single peak on PGP 2000 column. The elution volume of HSA was larger than that of BPA, resulting in a clear resolution of HSA and BPA.     

Further studies on the resolution of human mercapt- and nonmercaptalbumin and on human serum albumin in the elderly by high-performance liquid chromatography

High-performance liquid chromatographic (HPLC) analysis of human serum albumin (HSA) on Asahipak GS-520 showed at least two peaks, the principal component corresponding to human mercaptalbumin (HMA) and the secondary one to nonmercaptalbumin (HNA). HPLC analysis of HSA on Asahipak ES-520 N showed three peaks, the principal component corresponding to HMA, the secondary one to HNA having mixed disulfide with cysteine or glutathione and the tertiary one to HNA oxidized higher than mixed disulfide. Two kinds of rapid HPLC for the resolution of HSA into HMA and HNA were developed by the present authors. Using these HPLC, the present authors found a significant decrease in the fraction of HMA in the elderly.     

首批人凝血因子Ⅱ和Ⅹ浓制剂国家标准品协作标定

目的协作标定首批人凝血因子Ⅱ和Ⅹ浓制剂国家标准品。方法用世界卫生组织 98 590批人凝血因子Ⅱ和Ⅹ浓制剂国际标准品 ,采用一期法标定我国首批人凝血因子Ⅱ和Ⅹ浓制剂国家标准品 ,将标准品分别于4℃、2 2℃、37℃保存 5个月 ,进行稳定性考查。结果人凝血因子Ⅱ和Ⅹ国家标准品的效价分别为 1 6 .1IU 支和 1 2 .1IU 支 ,稳定性良好。结论确定了首批人凝血因子Ⅱ和Ⅹ浓制剂的国家标准品     

Carbonic Anhydrase Inhibition with Benzenesulfonamides and Tetrafluorobenzenesulfonamides Obtained via Click Chemistry

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