白边岛衣多糖抗肿瘤作用的研究

白边岛衣多糖腹腔注射200mg/kg(1/5LD₅₀)能显著抑制小鼠肉瘤180、艾氏腹水癌和宫颈癌-u14等肿瘤的生长,但不能延长白血病L7217小鼠的存活时间,50mg/kg和100mg/kg(1/10和1/20 LD₅₀)能增加小鼠网状内皮系统的吞噬功能。     

半边旗体内外抗癌作用及急性毒性研究

本文观察了半边旗水提液(PWE)和醇提液(PAE)体内外抗癌活性及急性毒性。结果表明,PWE和PAE对培养的人白血病细胞株HL—60和K562有明显抑制细胞增殖的作用,呈浓度依赖性;并明显降低HL—60细胞的分裂指数;PWE对小鼠S180肉瘤和小鼠HepA肝癌有明显的抑瘤作用,低10倍剂量的PWE与低剂量5—Fu联合用药可使5—Fu抑瘤率提高,在抑瘤的同时不降低荷瘤鼠末梢血白细胞数(p>0.05);以75g生药/kg/d小鼠灌胃,连续观察一周无异常;PWE和PAE溶血试验均为阴性。提示急性毒性很低。     

平消止痛丸的药理作用研究

对于消止痛丸抗肿瘤、镇痛及提高免疫功能等作用进行了研究。结果表明:平消止痛丸对小鼠肉瘤180(S_(180))、艾氏癌实体型(EAC)有明显抑瘤活性,对环磷酸胺抑制小鼠S_(180)有明显增效作用;平消止痛丸4、2g/kg均有显著的镇痛作用,4g/kg平消止痛丸可显著提高小鼠单核-巨噬细胞系统吞噬功能及血清血球凝集素效价。     

植物多糖对S180、K562细胞增殖和唾液酸、磷脂、胆固醇含量的影响

本实验用ＭＴＴ比色分析法研究了茯苓多糖（ＰＰＳ）、刺五加多糖（ＡＳＰＳ）、银耳多糖（ＴＦ）和香菇多糖４种植物多糖对体外培养的小鼠腹水型肉瘤Ｓ１８０细胞和人慢性骨髓性白血病Ｋ５６２细胞增殖的影响，结果证实ＰＰＳ、ＡＳＰＳ在体外具有直接抗肿瘤作用。ＰＰＳ对两种种瘤细胞的半数有效抑制浓度（ＩＣ５０）均为１．５ｍｇ／ｍｌ，ＡＳＰＳ对Ｓ１８０和Ｋ５６２细胞的ＩＣ５０分别为０．３８ｍｇ／ｍｌ和０．２８ｍｇ／ｍ     

Antitumor and immunomodulating effects of polysaccharides isolated from Solanum nigrum Linne

We have examined the effects of the crude polysaccharides isolated from Solanum nigrum Linne (SNL‐P) in vitro and in vivo against U14 cervical cancer. SNL‐P showed no antiproliferative effects in vitro at a dose up to 1 mg/ml. In vivo administration with SNL‐P (90, 180, 360 mg/kg b.w., p.o.) decreased the number of ascites tumor cells and prolonged the survival time of U14 cervical‐cancer‐bearing mice. FACScan flow cytometer analysis showed that most of the ascites tumor cells were arrested in G2/M phase of cell cycle and the ratio of CD4+/CD8+ peripheral blood T‐lymphocyte subpopulations were restored following treatment of SNL‐P. Furthermore, the treatment with SNL‐P also caused a significant increment in IFN‐γ (p < 0.01, 90, 180 and 360 mg/kg b.w.) and a remarkable decrease in Il‐4 (p < 0.01, 90, 180 mg/kg b.w.; p < 0.05, 360 mg/kg b.w.) by the method of ELISA. These data showed that SNL‐P possess potent antitumor activity and SNL‐P might exert antitumor activity via activation of different immune responses in the host rather than by directly attacking cancer cells on the U14 cervical cancer bearing mice. Thus, SNL‐P could be used as an immunomodulator and an anticancer agent. Copyright © 2009 John Wiley & Sons, Ltd.     

藤黄总酸对实验性肿瘤及肿瘤细胞体外生长的抑制作用

目的 :研究藤黄总酸的体内外抗肿瘤活性。方法 :以抑瘤率和生命延长率观察药物的体内抗肿瘤活性 ,以药物对肿瘤细胞株的抑制率为指标 ,探讨其体外抗瘤作用。结果 :藤黄总酸 (8,4 ,2mg/kg)iv对Heps、EC及S1 80 的肿瘤生长具有明显的抑制作用 (P <0 0 1 ) ;ip(1 5 ,0 75 ,0 375mg/kg )能显著延长Heps、EAC、S1 80 腹水型小鼠移植瘤的存活天数 ;藤黄总酸对人肝癌细胞BEL 74 0 2及人肺腺癌细胞SPC A1有较强的抑制作用。结论 :藤黄总酸对肿瘤细胞的体内外生长有明显抑制作用。     

钩吻提取物抗肿瘤作用的实验研究

目的 :探讨钩吻及其减毒后抗肿瘤的作用。方法 :以小鼠肉瘤180、小鼠肝癌为靶瘤 ,观察钩吻醇提物及其加玉叶金花混合提取物的抗肿瘤作用。并分别测定药物的半数致死量LD50 。结果 :钩吻醇提物(以生药计)0.45g/kg·d -1,0.11g/kg·d -1和钩吻 +玉叶金花混合提取物(以钩吻生药计)0.76g/kg·d -1,0.19g/kg·d -1 ,连续灌胃给药14天 ,对小鼠移植性肉瘤180实体型生长均有明显的抑制作用(P<0.05或P<0.01) ,但对小鼠移植性肝癌实体型生长抑制不明显。钩吻醇提物和钩吻 +玉叶金花混合提取物对小鼠的LD50 分别为2.23g/kg,7.64g/kg。结论 :钩吻醇提物具有一定的抗肿瘤作用 ,和玉叶金花混合提取后 ,即可保持疗效 ,又可降低毒性。     

脂质体载药降低阿霉素毒性的实验研究

 目的：研究阿霉素(F-ADM)和脂质体阿霉素(L-ADM)对正常NIH小鼠和肝癌腹水型(HcAC)小鼠的毒性。方法：采用卵磷脂、磷脂酸和胆固醇，应用冰冻融解法制成多层脂质体。NIH小鼠分为阿霉素和脂质体阿霉素两组。每组分为7.5,15,20和30 mg/kg 4个对应剂量组，尾静脉给药，观察60 d。NIH小鼠腹内接种HcAC 96 h后分为阿霉素和脂质体阿霉素两组，每组分为9,15和20 mg/kg 3个对应剂量组，腹腔内给药。结果：脂质体组动物体重和器官失重明显减轻；血生化变化相对减小；外周血白细胞下降幅度减小，恢复加快；心、肾、胃肠道病理损害减轻；药物的LD₅₀从14.7 mg/kg提高到21.9 mg/kg。在接种肿瘤96 h的延迟治疗组，动物对药物的耐受性下降，毒性死亡率升高。而脂质体组仍有较好疗效，生存期有所延长。结论：脂质体载药后可降低阿霉素的毒性并保留药物的抗肿瘤活性。     

黄芩总黄酮对移植性肉瘤S180的干预作用

目的：研究黄芩总黄酮对肉瘤S180的治疗作用以及黄芩总黄酮与常用化疗药的联合作用。方法：采用抗移植性肿瘤实验方法,观察黄芩总黄酮对移植性肉瘤的干预作用。结果：黄芩总黄酮以5、10和20mg/kg连续8天灌胃给药,对移植性肉瘤S180的抑制率分别为20.46%,33.48%和46.98%（P〈0.05）;黄芩总黄酮以5、10和20mg/kg连续15日灌胃给药,对S180抑瘤率分别为47.95%,59.06%和62.57%（P〈0.001）;黄芩总黄酮分别与化疗药物CTX,PDD及5-Fu联合,对治疗S180有良好的协同作用;结论：黄芩总黄酮对S180有良好的抗种瘤作用。     

In vivo assessment of safety and mechanisms underlying in vitro relaxation induced by Mikania laevigata Schultz Bip. ex Baker in the rat trachea

Mikania laevigata, popularly known in Brazil as "guaco", is largely used in folk medicine against respiratory diseases. However, neither the assessment of the toxicity of "guaco" syrup (GS, used by humans) nor its efficacy or mechanisms of action has been properly investigated. Using in vitro procedures, we showed that the hydroalcoholic extract (HE) from Mikania laevigata induces a concentration-dependent relaxation of rat trachea which does not depend on epithelium-derived substances but involves changes in the cellular mobilization of calcium, perhaps due to a direct effect on membrane potassium channels. In addition, we assessed both oral and intraperitoneal acute toxicity, as well as the oral subchronic and chronic toxicity of GS containing controlled amounts of coumarin, the main biological marker of Mikania laevigata preparations used in humans. The calculated LD(50) of GS after intraperitoneal administration was 0.904 g/kg in mice (both sexes) and 0.967 and 0.548 g/kg in male and female rats, respectively. However, the LD(50) values of GS by the oral route were calculated to be up to 10 g/kg, in both male and female mice and rats. Repeated dose 28- or 90-day oral treatment with GS (75, 150 and 300 mg/kg) did not produce any disturbances in the hematological or biochemical parameters of either male or female rats, nor did it provide evidence of toxicity in the hepatic, renal or pancreatic systems. Besides the mechanistic findings, our results provide evidence of the safety of Mikania laevigata in rodents, even after subchronic and chronic administration, at least in relation to the evaluated parameters.     

海洋真菌多糖YCP抑瘤作用(Ⅰ)

目的：研究海洋真菌多糖YCP对动物抑瘤作用和免疫功能的调节作用，探讨其抗肿瘤作用的机理。方法：采用抗移植性肿瘤实验方法，检测受试药物对荷瘤小鼠的瘤重及体重的影响。以荷瘤小鼠的血清半数溶血值（HC50）及吞噬指数K及吞噬系数α值等为指标，观察药物对免疫功能的影响。结果：与空白对照组相比，YCP（9．3mg／kg，iv、ip）对小鼠移植瘤肝癌实体型（Heps）、肉瘤180（S180）、Lewis肺癌的肿瘤生长具有明显的抑制作用（P〈0．01），且对小鼠的体重无明显的抑制作用。YCP（9,3mg／kg）可显著提高S180荷瘤小鼠的吞噬指数k和血清半数溶血值（P〈0．01，P〈0．05）。结论：YCP具有明显的抗肿瘤活性和显著提高S180荷瘤小鼠免疫功能的作用。     

复合多糖的免疫协同作用

目的探索复合多糖的组成及剂量,研究复合多糖对 S180肿瘤生长的抑制作用.方法采用 MTT法测定小鼠脾淋巴细胞增殖活性来探索复合多糖的配伍及剂量的组成;利用体内动物移植性肿瘤模型,观察药物的体内抗肿瘤活性.结果香菇多糖 100 mg/kg、姬松茸多糖 200 mg/kg、茯苓多糖 50 mg/kg组成的复合多糖可协同增强小鼠的脾淋巴细胞活性.复合多糖对 S180肿瘤的生长有一定的抑制作用.结论合适的多糖配伍具有免疫协同作用,可抑制肿瘤的生长.     

三七培养细胞与三七生药醇提物药理作用的比较

三七培养细胞(SC)与三七生药(SM)醇提物均能明显降低小鼠自发活动的次数,对抗由冰醋酸引起的扭体反应及提高对热刺激的痛阈值,减轻由二甲苯所致的鼠耳肿胀及蛋清所致的大鼠关节肿。小鼠口服SC或SM15g(生药)/kg均未见中毒,静脉注射LD_(50)SC为2.91g(生药)/kg,SM为3.03g(生药)/kg,中毒表现相似。     

银杏叶聚戊烯醇对移植性肉瘤的治疗作用

采用抗移植性肿瘤实验方法研究银杏叶(Folium Ginkgo)的活性物质—聚戊烯醇(Polyprenols GP-1)对肉瘤S180的治疗作用。结果表明,GP-1以20.0 mg/kg连续给药8天对S180的抑制率为47.35%,连续给药15天对S180抑制率可达62.57%;GP-1分别与化疗药物CTX,PDD及5-Fu联合,对治疗S180有良好的协同作用;低剂量GP-1可增强S180荷瘤小鼠对60Co放射治疗的敏感性。GP-1对S180有良好的抗种瘤作用。     

半边旗提取物5F-Na盐注射液制备及其对小鼠S180型肉瘤抑制作用研究

目的制备5F-Na盐注射液,并考察其对荷S180型肉瘤小鼠肿瘤的抑制作用。方法用0.5 mol.L-1 NaOH使半边旗提取物5F完全溶解,稀HCl调节pH值为7.4,加入磷酸盐缓冲液(PBS)稳定pH值并定容,灭菌,分装。高效液相色谱法测定5F-Na盐注射液中5F的含量,其标示量为10 mg.ml-1。将所制备的5F-Na盐注射液分为高、中、低3个剂量组(25,50,100 mg.kg-1),以小鼠S180型肉瘤实体瘤和腹水瘤为模型检测其体内抗癌活性。结果所制备5F-Na盐注射液为微黄色澄清透明液体。5F-Na盐注射液25,50,100 mg.kg-1 3个剂量组对S180型肉瘤实体瘤的抑制率分别为(16.53±4.90)%,(48.13%±11.09)%,(63.04±6.76)%,对腹水瘤的生命延长率分别为(42.24±25.66)%,(74.55±23.31)%,(141.86±13.91)%。结论该研究用的5F-Na盐注射液制备方法简单可靠,对小鼠S180型肉瘤的生长有明显抑制作用。     

Antineoplasic activity of Copaifera multijuga oil and fractions against ascitic and solid Ehrlich tumor

The aim of this study was to investigate the effect of chronic treatment with C. multijuga oil on Ehrlich tumor evolution. C. multijuga was fractionated in a KOH impregnated silica gel column chromatography to give three distinct fractions, i.e., hexanic, chloroformic, and methanolic, mainly composed by hydrocarbon sesquiterpenes, oxygenated sesquiterpenes and acidic diterpenes, respectively. Results demonstrated that the C. multijuga oil, the hexanic, and chloroformic fractions did not develop toxic effects. The oil, hexanic and chloroformic fractions (doses varying between 100 and 200mg/kg) showed antineoplasic properties against Ehrlich ascitic tumor (EAT) and solid tumor during 10 consecutive days of treatment inhibiting ascitic tumor cell number, reverting medulla and blood cell counts to values similar to control group, and inhibiting the increase on several inflammatory mediators (total protein, PGE(2), nitric oxide, and TNF) on ascitic fluid. The treatment also inhibited the increase in paw volume on tumor-inoculated mice. In conclusion, C. multijuga as well as its fractions demonstrated antineoplasic effect even after oral administration confirming its use by traditional medicine.     

桃儿七的抗肿瘤作用

桃儿七根及根茎的乙醇提取物对体外培养的人红白血病K_(562)细胞、小鼠白血病L_(1210)细胞及L_(7712)细胞,用小孔板法,10.0、5.0、2.5及1.0μg/ml终浓度剂量,24h后残留率分别为44.17％、47.63％、64.43％、79.57％,42.84％、50.73％、63.21％、75.10％及39.76％、46.36％、61.42％、75.24％;该药品小鼠单次腹腔注射LD_(50)为76.3～60.6mg/kg;对小鼠移植性肿瘤EAC、U_(14)及H_C,该药品用14.0mg/kg及7.0mg/kg剂量,瘤重抑制率分别为42.2％、37.8％,38.8％、33.3％及41.5％、35.6％。     

General behavior, toxicity, and cytotoxic activity of elenoside, a lignan from Justicia hyssopifolia

Cytotoxicity, acute toxicity, and general pharmacological effects in mice of an arylnaphthalene lignan isolated from Jisticia hyssopifolia were studied. Elenoside was cytotoxic to human cancer cell lines in a range of concentrations from 10(-5) to 10(-4)M. It has an LD(50), ip in mice, of 305 mg/kg and central depressive properties at doses of 25, 50, and 100 mg/kg. Thus, elenoside appears to be a sedative with broad spectrum cytotoxicity.     

阿诺宁乳化剂的抗瘤作用和急性毒性试验

 目的研究阿诺宁乳化剂的抗瘤作用和急性毒性反应。方法用小鼠和裸鼠移植性肿瘤模型测定体内抗瘤活性，用Blliss方法计算小鼠给药的急性毒性的LD₅₀。结果阿诺宁乳化剂在4，8和16 mg·kg^-1，灌胃(ig)qd×10 d，对小鼠肝癌HepS 3批实验的平均抑瘤率分别为39.2%，46.9%和55.7%；对小鼠肉瘤S-180的平均抑瘤率分别为34.6%，47.3%和54.4%；对小鼠L₂的平均抑瘤率分别为37.5%，45.9%和56.5%。阿诺宁乳化剂在7.5，15，30和60 μg·kg^-1腹腔注射(ip)×10d 剂量下，对小鼠肝癌(HepS)实验的平均抑瘤率分别为31.0%，42.9%，50.2%和62.4%；对小鼠肉瘤S-180的平均抑瘤率依次为23.6%，39.4%，50.9%和61.2%；在15，30和60μg·kg^-1，ip，每日1次，每周6次，共4周的剂量下，对人肝癌(Bel-7402)裸鼠移植瘤的抑瘤率分别为32.0%，50.5%和60.2%；在上述3个剂量下，对人肺腺癌(GLC-82)裸鼠移植瘤的抑瘤率分别为30.3%，41.9%和56.1%。结果表明，阿诺宁乳化剂ig，ip对上述5种肿瘤均有明显的抑制作用，且其抑瘤率与阿诺宁乳剂的剂量相关。用Bliss方法统计出阿诺宁乳化剂对小鼠ig一次的半数致死量(LD₅₀)及其95%可信限为74.75 (58.67～5.26) mg·kg^-1；ip的LD₅₀)为1.12 (1.01～1.24)mg·kg^-1)，静脉注射(iv)的LD₅₀为1.81(1.61～2.03) mg·kg^-1。结论阿诺宁乳化剂对多种小鼠和裸鼠移植瘤均有明显抗瘤作用。     

红花桑寄生多糖抑制小鼠S180肉瘤生长的研究

目的:研究红花桑寄生多糖的体内外抑瘤作用.方法:采用水提醇沉法提取分离红花桑寄生多糖(Scurrula para-sitica polysaccharides,SP),MTT法检测了SP对S180,K562和HL-60细胞增殖的抑制作用,腹腔给药检测SP对S180的体内抑瘤效果,并采用免疫组化方法分析了SP对瘤组织中Ki-67,CyclinD1,Bax和Bcl-2等细胞增殖与凋亡抗原表达的影响.结果:SP体外无抑瘤作用,体内抑制S180实体瘤生长的最适剂量为100 mg·kg~(-1)·d~(-1),抑瘤率为54%,SP对小鼠体重增长无影响.SP可下调瘤组织中Ki-67,CyclinD1和Bcl-2抗原的表达,上调Bax的表达.结论:SP可通过体内途径抑制瘤细胞增殖和促进瘤细胞凋亡而起到抗肿瘤作用.