树舌多糖对小鼠HepA癌细胞3H-TdR和(6-3H)一Glucose掺入的影响

就树舌多糖ＧＦ抗小鼠ＨｅｐＡ癌细胞作用机制方面做７初步研究，结果发现树舌多糖６Ｆ可抑制Ｈｅｐ。Ａ细胞掺入３Ｈ－ＴｄＲ（Ｐ＜０．０１）和抑制其对［６－３Ｈ］－Ｇｌｕｓｃｏｓ掺入（Ｐ＜０．０１），从而影响ＨｅｐＡ细胞的ＤＮＡ合成和糖代谢。表明树舌多糖ＧＦ是一种新型有效的抗癌活性物质     

高山红景天茎叶的化学成分研究

首次从长白山高山红景天ＲｈｏｄｉｏｌａｓａｃｈｉｌｎｅｓｉｓＡ．Ｂｏｒ．茎叶中分得７个化合物，经波谱分析和理化方法鉴定６个：蒲公英赛醇乙酸酯（ｔａｒａｘｅｒｏｌ－３β－ａｃｅｔａｔｅ，Ｉ）异莫替醇（ｉｓｏｍｏｔｉｏｌ，Ⅱ），β－谷甾醇（β－ｓｉｔｏｓｔｅｒｏｌ，Ⅲ），胡萝卜苷（ｄａｕｃｏｓｔｅｒｏｌ，ＩＶ），红景天苷（ｒｈｏｄｉｏｌｏｓｉｄｅ，Ⅵ），β－（Ｅ）－肉桂醇基－Ｏ－（６′－Ｏ－α－Ｌ－ｋ     

瞿麦化学成分研究

从石竹科植物瞿麦Ｄｉａｎｔｈｕｓ ｓｕｐｅｒｂｕｓ,Ｌ．中分得６种成分,经波谱分析鉴定为,大黄素甲醚（ｐｊｙｓｃｉｏｎ,１）大贡素（ｅｍｏｄｉｎ,Ⅱ）,３,４－二羟基苯甲酸甲酯（Ⅲ）、３－（３＇,４＇－二羟基苯基）丙酸甲酯（Ⅳ）、β－谷甾醇苷（Ⅴ）和大黄素－８－Ｏ＝葡萄糖苷（ｅｍｏｄｉｎ－８－Ｏ－ｇｌｕｃｏｓｉｄｅ,Ⅴ）。其中化合物Ⅲ（２００μｇ／ｋｇ）对受孕大鼠具有明显抗早孕作用。     

中药升麻的化学成分(Ⅴ)

首次报道升麻Ｃｉｍｉｃｉｆｕｇａ ｆｏｅｔｉｄａ Ｌ．的根茎中分得的１０个单体化合物，经理化常数测定和光谱分析，分别鉴定为异阿魏酸（ｉｓｏｆｅｒｕｌｉｃ ａｃｉｄ，Ｉ），３－乙酰氧基咖啡酸（３－ａｃｅｔｙｌｃ－ａｆｆｅｉｃ ａｃｉｄ，Ⅱ），咖啡酸葡萄糖酯甙（ｃａｆｆｅｉｃ ｅｓｔｅｒ ｇｌｕｃｏｓｉｄｅ，Ⅲ），升麻素（ｃｉｍｉｆｕｇｉｎ，Ⅳ），升麻素葡萄糖甙（ｃｉｍｉｆｕｇｉｎ ｇｌｕｃｏｓｉｄｅ     

狭序唐松草化学成分的研究(Ⅲ)

从狭窄唐松草Ｔｈａｌｉｃｔｒｕｍ ａｔｒｉｐｌｅｘ Ｆｉｎｅｒｒ ｅｔ Ｇａｎｇｅｐ．地上部分分离并鉴定了６个化合物,其中４个为生物碱,即：Ｎ－ｍｅｔｈｙｌｌａｕｒｏｔｅｔａｎｉｎｅ,（Ⅰ）、ｉｓｏｂｏｄｉｎｅ（Ⅱ）、ｔｈａｌｉｇｓｏｐｙｎｉｅ（Ⅲ）和Ｎ－ｍｅｔｈｙｌｃｏｃｕｌａｒｉｎｅ（Ⅳ）,２个为非生物碱,即：异槲皮苷（Ⅴ）和乙醇－（３,４－二羟基）－苯乙酯（Ⅳ）。６个化合物均为首次从该植物中     

互叶醉鱼草化学成分研究

从互叶醉鱼草地上部分得到三个化合物。经化学及光谱方法测定结构为６－Ｏ－α－Ｌ－（２″－Ｏ－ｉｓｏｆｅｒｕｌｏｙｌ）ｒｈａｍｎｏｐｙｒａｎｏｓｙｌｃａｔａｌｐｏｌ，６－Ｏ－α－ｌ－（３″－Ｏ－ｉｓｏｆｅｒｕｌｏｙｌ）ｒｈａｍｎｏｐｙｒａｎｏｓｙｌｃａｔａｌｐｏｌ和ｍａｒｔｙｎｏｓｉｄｅ。这三种成分均为首次从该属植物中得到。     

水溶性金属卟啉衍生物的合成及其对癌细胞生长的抑制活性

 用聚乙二醇（ｐｏｌｖｅｔｈｙｌｅｎｅｇｌｙｃｏｌ，ＰＥＧ）修饰原卟啉（ｐｒｏｔｏｐｏｒｐｈｙｒｉｎ，ＰＰ），以及在原卟啉环中导入金属离子合成７种水溶性金属卟啉衍生物，这些卟啉衍生物对癌细胞的生长有显著的抑制作用，特别是ＰＰ－ＰＥＧ，ｈｅｍｉｎ－ＰＥＧ以及ＰＰ（Ｍｎ）－ＰＥＧ抑制率很高。在浓度为１００μｍｏｌ／Ｌ时抑制率几乎达１００％，对于ＰＰ－ＰＥＧ和ｈｅｍｉｎ－ＰＥＧ当浓度为０．８μｍｏｌ／Ｌ时抑制率即达３０％。这种抑制活性与其过氧化物歧化酶样活性和过氧化物酶样活性无平行关系。     

电针足三里对MG大鼠神经-肌肉接头传递的影响

本研究复制大鼠重症肌无力（ＭＧ）模型，采用放射性同位素测定法（ＲＩＡ）测定其血清抗乙酰胆碱受体（ＡｃｈＲＡｂ）滴度，采用玻璃微电极记录法，测定大鼠左侧膈神经－膈肌标本的小终板电位（ＭＥＰＰ）及乙酰胆碱电位（Ａｃｈｐ），同时观察针刺通电刺激足三里穴对ＭＧ大鼠ＡｃｈＲＡｂ滴度、ＭＥＰＰ及Ａｃｈｐ的影响及其作用机制。结果表明：ＭＧ大鼠的ＡｃｈＲＡｂ滴度显著高于健康大鼠（Ｐ＜０．０１）；ＭＥＰＰ与Ａｃｈｐ的振幅均明显低于健康大鼠（Ｐ＜０．０５），但ＭＥＰＰ的频率、Ａｃｈｐ的时程与健康大鼠相比较却无显著性差异（Ｐ＞０．０５）；针刺足三里能使ＭＧ大鼠的ＭＥＰＰ与Ａｃｈｐ的振幅升高，但对ＭＥＰＰ的频率与Ａｃｈｐ时程没有影响，且针刺前后血清ＡｃｈＲＡｂ滴度也没有明显变化；针刺非经穴处则对上述３项指标均没有明显影响。提示：针刺足三里穴可增强ＭＧ大鼠神经－肌肉接头传递的功能，作用机制可能是通过改变神经－肌肉接头突触后膜乙酰胆碱受体（ＡｃｈＲ）与乙酰胆碱（Ａｃｈ）或ＡｃｈＲＡｂ的亲和力来实现的     

石香薷挥发油的GC-MS分析

石香薷挥发油的ＧＣ－ＭＳ分析李伟，谈献和，邹惠仙，郭戎，文红梅（南京２１００２９南京中医药大学中药学院；南京：１０００８南京大学环境科学与工程系）石香薷（ＭｏｓｌａｃｈｉｎｅｎｓｉｓＭａｘｉｍ．）为唇形科（Ｌａｂｉ－ａｔａｅ）荠属植物，具有发汗解表、...     

翻白叶的化学成分

首次从翻白叶Ｐｏｔｅｎｔｉｌｌａ ｇｒｉｆｆｉｔｈｉｉ Ｈｏｏｋ．ｆ．ｖｅｌｕｔｉｎａ Ｃａｒｄ．全草的甲醇提取物中分得６个化合物,分别为黄酮苷和三萜类化合物,经光谱及化学方法分别鉴定为翻白叶苷Ａ（ｐｏｔｅｎｇｒｉｆｆｉｏｓｉｄｅ Ａ．Ⅰ）,委陵菜酸（ｔｏｒｍｅｎｔｉｃ ａｃｉｄ,Ⅱ）,野蔷薇苷（ｒｏｓａｍｕｌｔｉｎ,Ⅲ）,ｅｕｓｃａｐｈｉｃ ａｃｉｄ（Ⅳ）,ｋａｊｉ－ｉｃｈｉｇｏｓｉｄｅ Ｆ１（     

Shikonin derivatives protect immune organs from damage and promote immune responses in vivo in tumour-bearing mice

Shikonin, a major component of Lithospermum erythrorhizon and Arnebia euchroma, exhibits antiinflammatory, immunomodulatory and antitumour activities. Although many recent studies have focused on the antitumour effects of shikonin, the exact mechanisms underlying its antitumour and immunomodulatory effects in tumour‐bearing mice remain unclear. The aim of the present study was to investigate the antitumour and immunomodulatory effects of shikonin derivatives (ShD) in tumour‐bearing mice. Swiss mice inoculated with hepatoma HepA₂₂ or sarcoma 180 (S₁₈₀) cells were treated with ShD or 5‐fluorouracil (5Fu). Survival time, immune organs, natural killer cell activity, lymphocytes, lymphocyte transformation and interleukin (IL)‐2 production were analysed. ShD significantly prolonged the survival (median survival time prolonged by >7 days) of tumour‐bearing mice in a dose‐dependent manner, inhibited the growth of transplantable neoplasms (inhibitory rate, > 33%), and recovered (at [ShD] = 2.5 mg/kg/day) or increased (at [ShD] > 5 mg/kg/day) the number of CD3‐ and CD19‐positive cells. ShD also played a role in protecting the immune organs from damage and reversed or enhanced immune responses, as noted by the nearly normal thymic structure; enlarged splenic corpuscles; and improved natural killer cell activity, lymphocyte transformation and IL‐2 production in ShD‐treated mice. ShD reduced the tumour load of tumour‐bearing mice and protected the immune organs against tumour‐induced damage and immune function impairment. Copyright © 2011 John Wiley & Sons, Ltd.     

The antitumour growth and antiangiogenesis effects of xanthatin in murine glioma dynamically evaluated by dynamic contrast‐enhanced magnetic resonance imaging

To investigate the suppressive effects of xanthatin on glioma growth in a nude mouse xenograft model and rat orthotopic implantation model using magnetic resonance imaging (MRI) to dynamically monitor the antitumour growth and antiangiogenesis effects of xanthatin. The nude mouse xenograft tumour model and rat orthotopic implantation model were established to observe the antitumour effects of xanthatin in vivo. In the rat orthotopic implanted tumour model, MRI scanning was used to dynamically monitor the antitumour growth effect and evaluate the antiangiogenesis effect of xanthatin. We found that xanthatin at a dose of 0.4 mg/10 g dramatically decreased the growth of xenograft tumours in nude mice. The antiangiogenesis effect of xanthatin C6 glioma was evaluated by dynamic contrast‐enhanced (DCE) MRI via comparison of the volume transfer constant (K^trans) value, a parameter that reflects vessel permeability. We found that xanthatin at the doses of 8 and 16 mg/kg significantly decreased the K^trans value, which suggests that xanthatin has antiangiogenesis effects. These data demonstrate the suppressive effects of xanthatin on C6 glioma occur via antiangiogenesis. Meanwhile, this study also provides evidence for the application of quantitative parameters of DCE‐MRI for dynamically evaluating the growth and angiogenesis of intracranial tumours and for experimental and clinical research.     

A new type of biological response modifier from Chlorella vulgaris which needs protein moiety to show an antitumour activity

An immunopotentiator obtained from Chlorella vulgaris strain CK22, showed antitumour effects against various lines of syngeneic tumours, especially by intratumour administration. The immunopotentiator exhibited far greater antitumour activity against a rechallenged tumour than against the primary-inoculated tumour in Meth A and BALB/c or CDF1 mouse systems. The antitumour effect was at least comparable to that of a streptococcal preparation, OK-432, which has been widely used for clinical immunotherapy. The active compound was fractionated by anion-exchange and affinity chromatography monitoring by the Meth A rechallenge system. The most active fraction, Q2C2, consisted of galactose-rich carbohydrate (56.1%) and protein (36.3%). Antitumour activity disappeared after protease digestion, but was stable for extreme treatments of acid, alkali, heat and carbohydrate degradation. These facts indicate that the protein moiety of the glycoprotein is mainly related to express the antitumour activity. © 1998 John Wiley & Sons, Ltd.     

Cytotoxic and antitumour activity from Bursera fagaroides ethanol extract in mice with L5178Y lymphoma

Chloroform extracts of Bursera fagaroides (Burseracea) have previously shown antitumour activity against the Walker carcinoma 256 tumour system (WA16). In the present work we have determined the cytotoxic and antitumour activity of the ethanol extract (70%) of the bark of B. fagaroides using the L5178Y lymphoma. The cytotoxic activity is expressed as the ED₅₀ of the L5178Y lymphoma cells in culture, (20 µg/mL) whilst the antitumour activity was shown via a tumour growing inhibition test, measuring survival of BALB/c mice (2 × 10⁴ cells L5178Y i.p.). 24 h after inoculation mice were treated with 50 or 100 mg/kg of extract daily, over 15 days in independent groups of 10, using two administration routes. We observed the tumour evolution with and without treatment. Oral administration resulted in 8% of mice being tumour free after 60 day whilst intraperitoneal administration showed 26% survived at a dose of 100 mg/kg/day for 15 days. A significant increase in the survival of the treated animals (at 50 mg/kg/day over 15 days) was found compared with those treated with placebo or without treatment. Copyright © 1998 John Wiley & Sons, Ltd.     

Comparative study on the immunological activity of a series of isoquinoline alkaloids

A series of eight isoquinoline alkaloids were isolated from Glaucium flavum or synthesized and subsequently their immunological activity was evaluated. The structure-effect relationships were evaluated in the following in vitro tests: complement activation, phagocytosis and antibody synthesis. Oxoglaucine caused significant inhibition of classical complement activity. Representatives with two phenolic hydroxyl groups decreased the phagocytic activity of peritoneal macrophages. All substances tested possessed suppressive effects on antibody synthesis against sheep red blood cells. Oxoglaucine was the most potent of the series.     

Bioactivity-guided isolation of antiproliferative compounds from Centaurea arenaria

The antiproliferative effects of n-hexane, chloroform and aqueous methanol extracts prepared from the whole plant of Centaurea arenaria M.B. ex Willd. were investigated against cervix adenocarcinoma (HeLa), breast adenocarcinoma (MCF7) and skin epidermoid carcinoma (A431) cells, using the MTT assay. The chloroform extract displayed high tumour cell proliferation inhibitory activity (higher than 85% at 10 μg/mL concentration), and was therefore subjected to a bioassay-guided multistep separation procedure. Flavonoids (eupatilin, eupatorin, 3'-methyleupatorin, apigenin and isokaempferid), lignans (arctigenin, arctiin and matairesinol), the sesquiterpene cnicin, serotonin conjugates (moschamine and cis-moschamine), β-amyrin and β-sitosterin-β-D-glycopyranoside, identified by means of UV, MS and NMR spectroscopy, were obtained for the first time from this species. The isolated compounds were also evaluated for their tumour cell growth inhibitory activities on HeLa, MCF7 and A431 cells, and different types of secondary metabolites were found to be responsible for the antitumour effects of the extracts; in addition to moderately active compounds (isokaempferid and moschamine), especially apigenin, eupatorin, arctigenin, arctiin, matairesinol and cnicin exert marked antitumour effects against these cell lines.     

连翘酯苷抗氧化活性及构效关系研究

 目的研究中草药有效成分氯原酸、连翘酯苷对活性氧(HO·，H₂O₂，O₂)的清除作用及结构与活性的关系。方法邻菲罗啉、鲁米诺化学发光、NBT法以及量子化学计算［PM3，HF/6-31G(d)］。结果氯原酸、连翘酯苷对活性氧具有较强的清除能力；连翘酯苷结构中的A环酚羟基和B环酚羟基对活性氧的清除能力相当。结论连翘酯苷是一种有效的天然抗氧化剂。     

Antitumour activity of Ganoderma lucidum,an edible mushroom,on intraperitoneally implanted lewis lung carcinoma in synergenic mice

The antitumour activity of Ganoderma lucidum, called ‘Ling-Zhi or holy mushroom’in Chinese traditional medicine, was investigated on intraperitoneally implanted Lewis lung carcinoma in syngeneic C57BL/6 mice. An aqueous extract of Ling-Zhi significantly increased the life span of tumour-implanted mice, when administered intraperitoneally alone or in combination with cytotoxic antitumour drugs (Adriamycin, fluorouracil, thioguanine, methotrexate, Cisplatin) or a synthetic immunomodulator (Imexon). The aqueous extract was not cytotoxic in cell cultures and the antitumour activity was abolished by pretreatment of mice with cyclosporine. The active principle(s) was found to be present predominantly in the ethanol precipitable fraction of the aqueous extract.     

Effect of tea root extract (TRE) on solid tumours induced by 3-methylcholanthrene in mice

The antitumour effect of tea plant root extract (TRE) has been evaluated against a 3-methylcholanthrene (3-MC) induced solid tumour model in ICR mice. TRE inhibited the tumur weight and the tumours were found to be non-necrotic. Superoxide dismutase (SOD), a free radical scavenger, in the sera of TRE treated tumour bearing mice was found to be significantly increased while the SOD level in untreated tumour bearing animals was low. Moreover, the enhanced level of thiobarbituric acid reactive substance (TBARS) in sera of tumour bearing mice were normalized upon TRE treatment. © 1998 John Wiley & Sons, Ltd.     

Antitumour potential of pollen extract on lewis lung carcinoma implanted intraperitoneally in syngeneic mice

A defined pollen extract of selected plants has been reported to possess some pharmacological activities on chronic prostatis or benign prostatic hyperplasia. This paper describes the antitumour potential of the water soluble fraction (Cernitin T60) of pollen extract against Lewis lung carcinoma implanted intraperitoneally in syngeneic mice. Cernitin T60 was not cytotoxic in cell cultures at concentrations up to 2.5 mg/mL, while it is significantly prolonged the life-span of mice carrying the tumour without any apparent side effects at 0.5 g/kg. In addition, Cernitin T60 demonstrated beneficial therapeutic effects in an additive fashion on the life-span of mice when it was combined with standard cytotoxic antitumour drugs such as adriamycin, cisplatin, vincristine, methotrexate, fluorouracil, or thioguanine. The antitumour potential of Cernitin T60 was completely abolished by treatment with inhibitors of macrophage functions (2-chloroadenosine or carrageenan), but not with a T-cell inhibitor (cyclosporin A). Cernitin T60 appears to be a potent immunostimulator of macrophages.