兴安升麻总苷抗肿瘤药效研究

目的观察升麻总苷对小鼠移植性肿瘤和人肿瘤细胞裸鼠移植瘤的体内抗肿瘤作用，以及体外对人肿瘤细胞株的抑瘤活性，并对其抑瘤机制进行初步探讨。方法MTT法检测体外升麻总苷对人肿瘤细胞的增殖抑制作用；体内实验观察其对小鼠S180和裸鼠体内移植人肺腺癌A549的抑制作用；同时采用流式细胞仪和肿瘤病理切片对接种的A549肿瘤细胞凋亡进行观察。结果升麻总苷对A549、HepG2、HL60、Eca-109、MDA-MB231肿瘤细胞的半数抑制浓度（IC50）分别为20．3、27．1、21．2、23．4和32．7gg／mL。小鼠口服升麻总苷100mg／kg和200mg／kg可明显抑制S180移植瘤（抑瘤率分别为42．8％和54．6％）和裸鼠移植人肺腺癌A549的生长（T／C值分别为58．1％和52．2％），肿瘤组织病理切片和流式细胞仪对A549肿瘤细胞凋亡的检测显示，升麻提取物可诱导体内肿瘤细胞凋亡。结论升麻体内体外均具有抗肿瘤活性，其体内抑制肿瘤生长可能与诱导细胞凋亡相关。     

人肝癌组织裸鼠移植瘤模型建立及其应用

目的 建立人肝癌组织裸鼠移植瘤模型,对其特性进行鉴定,并应用于抗肿瘤药物制剂疗效的观察。方法 将人原发肝癌手术新鲜组织移植于BALB/c裸鼠皮下,建立人肝癌组织裸鼠移植瘤动物模型;于同体移植后第15 天连续ig给予长科制剂（CKBM）,通过观察动物日常状况、接种部位出现肿块时间,测定瘤体体积和质量、抑瘤率以及进行组织病理学观察,初步评价CKBM的抗肿瘤疗效。结果 人肝癌组织裸鼠移植瘤保持了人肝癌组织特性,并能通过同体移植传代;观察发现CKBM对人肝癌荷瘤裸鼠的抑瘤率达45.71%,对癌细胞生长有一定的抑制作用。结论 在成功建立人肝癌组织裸鼠移植瘤模型基础上,观察发现CKBM具有一定的抗肿瘤疗效。     

反应停对小鼠荷瘤H_(22)的影响

目的研究不同剂量反应停及反应停协同环磷酰胺对小鼠荷瘤H22(肝癌)实体型肿瘤的影响。方法建立小鼠肝癌移植实体型肿瘤模型,比较不同剂量反应停对小鼠肝癌的影响,同时观察反应停协同环磷酰胺对小鼠肝癌的影响。通过研究反应停对小鼠迟发型变态反应的影响探究其免疫作用。结果反应停对小鼠荷瘤H22呈现明显剂量依赖性抑制作用,反应停与环磷酰胺具有协同抗小鼠肝癌作用。反应停对小鼠迟发型变态反应呈剂量依赖性促进作用。结论反应停具有抗肝癌作用,而且与环磷酰胺具有协同抗肿瘤作用,此作用与反应停抗免疫作用有关。     

玉米提取物的抗肿瘤作用研究

研究玉米乙醇提取物(YM-J)和玉米多糖(YM-S)的体外和体内抗肿瘤活性.方法　采用MTT法测定YMJ,YM-S对人肿瘤细胞株BGC-823和SMMC-7721的体外抑制作用,计算IC50;分别采用人胃癌BGC803裸鼠移植瘤模型和H22小鼠肝癌移植瘤模型,ig YM-J,YM-S,剂量400,200 mg· kg-1,1次/d(胃癌BGC803连续19d,小鼠肝癌连续10 d,检测其体内抗肿瘤作用.结果　YM-J和YM-S对人胃癌细胞BGC-823细胞有较强的抑制作用,IC50分别为24.16,12.61 μg·mL-1;YM-J和YM-S对人肝癌细胞SMMC-7721的抑制作用较弱,IC50分别为127.42,1352.72 μg·mL-1.在人胃癌BGC803裸鼠移植瘤模型和H22肝癌模型,YM-J均可明显抑制肿瘤生长,抑瘤率最高分别为40.27％和44.69％.YM-S对H22肝癌有一定抑瘤作用,抑瘤率38.89％,但对人胃癌BGC803裸鼠移植瘤的抑瘤率最高为25.96％.结论　玉米乙醇提取物YM-J和玉米多糖YM-S在体外和体内均具有一定的抗肿瘤活性,其中乙醇提取物对肝癌和胃癌的抑制作用较强.     

蝙蝠葛活性成分体内外抗肿瘤作用研究

目的探讨蝙蝠葛活性成分在体内外抗肿瘤的作用。方法将30只BALB/c A裸小鼠按随机数字表法随机分为阴性对照组、阳性对照组、药物低剂量组、药物高剂量组。进行体外细胞培养,在细胞复苏和培养之后,进行细胞活力检测。使用MTT比色法按照实验标准方法进行。每周对所有小鼠测量移植瘤的长度、宽度,动态观察裸鼠移植瘤的生长情况,并计算体积,制作裸鼠移植瘤的生长去曲线图。结果蝙蝠葛活性成分对人肺癌A-549细胞株,人肝癌Hep G2细胞株,人肝癌Hep3B细胞株,人宫颈癌Hela细胞株、人乳腺癌MCF-7细胞株、人白血病K-562细胞株、人胃癌MGC-803细胞株、人胃癌SGC-7901细胞株和小鼠黑色素瘤B-16细胞株均有明显抑制增殖作用。药物低剂量组的T/C值为68.4%,对裸小鼠移植瘤的生长无明显地抑制作用;药物高剂量组的T/C值为58.8%(P0.05)。结论蝙蝠葛活性成分在体外具有较强的广谱抗肿瘤细胞增殖作用,且高剂量组蝙蝠葛对移植肿瘤的抑制效果非常明显。     

氧化苦参碱对人胃癌MGC-803细胞裸鼠皮下移植瘤

目的：通过观察氧化苦参碱（oxymatrine,OXY）对人胃癌MGC-803细胞系裸鼠移植瘤的抑制作用,观察氧化苦参碱对该移植瘤形态学的影响,阐述其抗肿瘤作用。方法：将60只裸鼠分为阴性对照组、阳性对照组、氧化苦参碱小剂量组、氧化苦参碱中剂量组、氧化苦参碱大剂量组,腹腔注射给药。观察荷瘤鼠肿瘤生长情况,分析氧化苦参碱对MGC-803细胞裸鼠皮下移植瘤增形态学的影响。结果：氧化苦参碱具有抑制MGC-803细胞裸鼠皮下移植瘤生长的作用,各用药组肿瘤平均体积明显小于阴性对照组,差异具有统计学意义（P〈0．05）;从第9天开始,阳性对照组与其他各用药组裸鼠体质量相比,差异均有统计学意义（P〈0．05）。结论：氧化苦参碱对人胃癌MGC-803细胞系裸鼠肿瘤有抑制作用。     

中药固金磨积片抗肝肺肿瘤移植和转移作用的实验研究

目的：探讨固金磨积片抗肿瘤转移作用。方法肝癌：应用小鼠移植肝癌22（腹水型）。按1：3比例制成瘤细胞悬液，每只小鼠0．2ml（约1～2×106）接种于NIH小鼠腹腔内，次日随机分为5组（n＝10），给药的3组分别按高（1．88g／kg），中（1．02g／kg）和低（0．592g／kg）三种剂量，每天1次灌胃给药，连续10d，停药后次日处死小鼠，抽腹水量，计算肿瘤细胞数。肺癌：取Lewis肺癌瘤组织悬液0．2ml接种于C57系小鼠右前腋皮下，24h后，随机分为5组（n＝10），用药组每天1次灌胃给药，剂量高、中、低三种（药量同肝癌组），连续20d，停药24h后处死小鼠，取肺组织在倒置显微镜下观察并计算肺转移瘤结节数。结果：①、固金磨积片对小鼠转性肝癌22瘤细胞生长有明显抑制作用，各用药组腹水形成缓慢，腹水量及每升腹水中所含的肿瘤细胞数与对照组比较均有明显差异（P＜0．05）。②、固金磨积片对Lewis肺癌转移结节有明显的抑制作用，与对照组比较（P＜0．05～0．01）。结论：本研究提示固金磨积片通过活血化瘀，清热解毒，扶正益气，保护和增强机体免疫功能，从而达到抑制肿瘤生长，抗肿瘤转移作用。     

蝙蝠葛酚性碱对BXPC-3荷瘤小鼠细胞凋亡基因p16表达的影响

目的：观察蝙蝠葛酚性碱（PAMD）的抗肿瘤作用并进一步探讨其作用机制。方法：通过实时定量PCR（Real-timePCR）技术观察PAMD对胰腺癌细胞株BXPC-3皮下异位移植瘤细胞凋亡相关基因p16mRNA表达的影响,以此探讨PAMD抗肿瘤作用机理。结果：PAMD能够显著升高胰腺癌细胞株BXPC-3裸鼠皮下异位移植瘤组织中p16mRNA表达量。结论：PAMD对胰腺癌细胞株BXPC-3裸鼠皮下异位移植瘤表现出明显抑制作用,能够有效的抑制肿瘤生长,其机理可能与PAMD能够诱导细胞凋亡及影响凋亡相关基因表达有关。     

四逆散对HepG2移植性肝癌裸鼠Sirt1和p53表达的影响

目的:探讨四逆散对裸鼠移植性肝癌的抑制作用。方法:利用HepG2细胞裸鼠移植瘤模型,观察四逆散的抗肿瘤作用,采用ELISA法测定白介素-6(IL-6)、白介素-12(IL-12)和肿瘤坏死因子-α(TNF-α)的水平,并用Western blot法探讨其作用机制。结果:与模型组比较,四逆散(1.8⁷.2g/kg)对荷瘤小鼠肿瘤的生长具有明显的抑制作用,四逆散中(3.6g/kg)剂量组和高(7.2g/kg)剂量组能够明显增加活性氧(ROS)的含量,并提高小鼠脾脏指数、IL-6、IL-12和TNF-α的水平,同时,显著下调Bcl-2、Sirt1蛋白表达,上调Bax、Caspase 3和p53的蛋白表达。结论:四逆散能够抑制人肝癌细胞HepG2裸鼠移植瘤生长,并通过ROS依赖的Sirt1-p53凋亡途径发挥作用。     

蛇葡萄素对人肺癌GLC-82裸鼠移植瘤的抑制作用

目的:为了进一步研究蛇葡萄素体内抗肿瘤作用,我们进行了人肺癌GLC-82裸小鼠移植瘤的抑瘤实验研究.方法:人肺癌GLC-82 细胞接种于裸鼠腋窝建立移植模型.荷瘤BALB/C裸鼠随机分成6组,蛇葡萄素以3个剂量腹腔给药.观察肿瘤体积、相对肿瘤体积、瘤重、相对肿瘤增殖率以及肿瘤生长曲线,以此评价蛇葡萄素的抗瘤作用.结果:250mg/kg蛇葡萄素对裸鼠移植瘤的抑制率,二次实验结果分别为35.5%(P＜0.01)和37.1%(P＜0.01),相对肿瘤增殖率则分别为55.24%(P＜0.01)和57.71%(P＜0.05).结论:蛇葡萄素对人肺癌GLC-82裸鼠移植瘤具有显著的抑制作用.     

Recent progress in pharmacological research of propolis.

Propolis is a resinous hive product collected by honeybees from various plant sources. It is a popular folk medicine possessing a broad spectrum of biological activities. It has also been used as a health drink in various Asian, European and American countries. Several groups of researchers have focused their attention on the biological activity of propolis and its active principles. Many scientific articles are published every year in different international journals related to the pharmacological properties of propolis. This review article compiles recent findings (since 1995) on the pharmacological properties of propolis focusing on its antihepatotoxic, antitumour, antioxidative, antimicrobial and antiinflammatory properties. The possible mechanism of action of propolis as well as the active compounds are discussed.     

天然桃叶珊瑚苷及其衍生物的化学结构和药理作用研究进展

桃叶珊瑚苷在植物界中分布广泛,是玄参、杜仲、车前草等常用中药的有效成分之一,其药理作用也受到越来越多地关注,然而,桃叶珊瑚苷衍生物则鲜有报道。对桃叶珊瑚苷衍生物的结构类型(主要包括6-O取代型、10-O取代型、6,10-O双取代型、6′-O取代类型和其他类型)及近10年桃叶珊瑚苷及其衍生物的抗氧化、抗炎、抗菌、神经保护、抗肿瘤等药理活性进行综述。     

Biological effects of Myristica fragrans (nutmeg) extract

The chloroform extract of nutmeg has been evaluated for antiinflammatory, analgesic and antithrombotic activities in rodents. The extract inhibited the carrageenan‐induced rat paw oedema, produced a reduction in writhings induced by acetic acid in mice and offered protection against thrombosis induced by ADP/adrenaline mixture in mice. Copyright © 1999 John Wiley & Sons, Ltd.     

Antifertility activity of Artemisia vulgaris leaves on female Wistar rats

AIM： To evaluate the antifertility activity of Artemisia vulgar＆ leaves on female Wistar rats. METHOD： The plant extract was tested for its effect on implant formation at two dose levels, 300 and 600 mg.kg 1, respectively. The effective methanolic plant extract was further studied for estrogenic potency on ovariectomised immature female Wistar rats. RESULTS： The data presented in this study demonstrate the antifertility potential of Artemisia vulgar＆ methanolic leaf extract, which shows a strong and significant decrease in implant formation （100%）, and a strong estrogenic effect resulting in a significant increase in uterine weight in immature ovariectomised rats. These observations suggest that the methanolic extract of Artemisia vulgaris leaves has strong anti-implantation activity and estrogenic activity. CONCLUSION： The methanolic plant extract ofA. vulgaris has antifertility activity.     

The antiinflammatory, gastroprotective and antioxidant activities of Hieracium gymnocephalum extract

The present study investigated the antiinflammatory, gastroprotective and antioxidant activities of a CH(2)Cl(2) extract of western Balkan endemic Hieracium gymnocephalum Griseb. ex Pant. (Compositae). The carrageenan-induced rat paw oedema test was used as an experimental model for screening the antiinflammatory activity. The extract was administrated p.o. in doses of 25, 50, 100 and 200 mg/kg to rats and its effects compared with indomethacin, used p.o. as a reference drug. The results showed that the investigated extract reduced the oedema in a concentration-dependent manner. The obtained antiinflammatory effect was 5.9%, 11.7%, 31.2% and 44.1% at doses of 25, 50, 100 and 200 mg/kg, respectively, being statistically significant at a dose of 100 mg/kg. Indomethacin had a strong antiinflammatory effect of 73.4% at a dose of 8 mg/kg, but caused large gastric lesions. When the plant extract in the highest tested dose (200 mg/kg) was concomitantly given with indomethacin, the antiinflammatory effect was slightly enhanced, but the gastric lesions were significantly reduced. The antioxidant activity of the H. gymnocephalum extract, investigated using DPPH radical assay, OH-radical assay and TBA-test, was not substantial.     

Biological activities of synthetic saponins and cardiac glycosides

Comparisons of the biological activities of diosgenyl (DIO) beta-D-xylopyranosyl- (1 --> 2)-alpha-D-glucopyranoside (2DXalpha) and beta-D-glucopyranosyl- (1 --> 3)-beta-D-glucopyranoside (3GLbeta) or methyl glycyrrhetinate (GAM) 2DXalpha and 3GLbeta with those of the other DIO- or GAM- glycosides confirmed our assumption that both haemolytic and antifungal activities of DIO-glycosides (steroid saponins) generally parallel each other, while almost all haemolytic GAM-glycosides (triterpenoid saponins) have no antifungal activity. By comparisons of digitoxigenyl (DIG) 2DXalpha, beta-D-xylopyranosyl- (1 --> 2)-beta-D-glucopyranoside (2DXbeta) and 3GLbeta with the other DIG-glycosides, the previous supposition on DIG-diglycosides (cardiac diglycosides) has been developed into the assumption that those having a (1 --> 4), (1 --> 3) or (1 --> 2)beta sugar linkage show stronger anti-ATPase and antiviral activities than those with a (1 --> 6) or (1 --> 2)alpha linkage.     

Anti-nociceptive and anti-inflammatory activity of sophocarpine

Aim of the study

This study aimed to assess the anti-nociceptive and anti-inflammatory activity of sophocarpine in rodents.

Materials and methods

The anti-nociceptive effect was evaluated in two experimental animal models and anti-inflammatory effect in three animal models, and sophocarpine was given by tail vein injection for the above study.

Results

Pretreatment with a single dose of sophocarpine (20 and 40 mg/kg) produced dose-dependent anti-nociceptive effects in thermally and chemically induced mouse pain models. Pretreatment with a single dose of sophocarpine also produced significant dose-dependent anti-inflammatory effects on carrageenan-induced rat hind paw edema (15 and 30 mg/kg), xylene-induced mouse ear edema (20 and 40 mg/kg) and acetic acid-induced mouse vascular permeation (20 and 40 mg/kg).

Conclusions

Sophocarpine possesses peripheral and central analgesic properties as well as anti-inflammatory activity on acute inflammatory processes.     

兰科植物生物碱类化学成分及药理活性研究进展

生物碱类化学成分结构复杂、种类繁多,广泛存在于兰科各属植物中,且大多具有抗炎、抗肿瘤、降血糖、细胞毒性等生物活性。系统综述了兰科生物碱类化学成分的植物分布、种类结构及药理作用,为兰科植物中生物碱类成分的结构类型、结构解析及生物活性的深入研究提供理论参考。     

Antiprotozoal and cytotoxic activities in vitro of Colombian Annonaceae

Ethnobotanical and chemotaxonomical studies for antiparasitic activity of Colombian Annonaceae were carried out. In vitro antiprotozoal activity of 36 extracts obtained from six different species was determined against promastigotes of three Leishmania species, epimastigotes of Trypanosoma cruzi and both chloroquine sensitive (F32) and resistant (W2) Plasmodium falciparum. Cytotoxic activity was evaluated in U-937 cells. Active extracts were selected according their selectivity index (SI). Extracts from Annona muricata, Rollinia exsucca, Rollinia pittieri and Xylopia aromatica were active against Leishmania spp. and Trypanosoma cruzi showing IC50 values lower than 25 microg/ml. Hexane extract from Rollinia pittieri leaves was the most selective against Trypanosoma cruzi and Leishmania spp. (IS=10 and 16, respectively). The extracts from Desmopsis panamensis, Pseudomalmea boyacana, Rollinia exsucca and Rollinia pittieri showed good antiplasmodial activity (IC50 < 10 microg/ml). No correlation between antiplasmodial activity and inhibition of beta-hematin production was found. The present study gives specific and useful information about antiprotozoal and cytotoxic activities of some Annonaceae extracts. Results presented here also demonstrate which plants and/or plant parts could be useful in the treatment of leishmaniasis, Chagas' disease and malaria.     

石莼提取物抗氧化及抗菌活性研究

本文研究了石莼提取物的抗氧化及抗菌活性,研究比较了乙醇、氯仿、乙酸乙酯的石莼粗提物抗氧化、抗菌活性。结果显示三种提取物的DPPH清除率,羟自由基清除率及还原力均随浓度的增加呈递增趋势;且石莼多酚对金黄色葡萄球菌、副溶血性弧菌、创伤弧菌和麦氏弧菌有较好的抗菌作用。