金雀花碱的生物活性研究进展

金雀花碱(Cytisine,Cyt)是一种主要存在于豆科毒豆属植物种子中的喹诺里西啶生物碱。近年来金雀花碱的多种生物活性被逐渐发掘,其具有戒烟、促呼吸、镇痛、抗肿瘤等功效。在抗癌活性方面能够诱导癌细胞凋亡,已被广泛应用于抑制多种肿瘤细胞的增殖;在戒烟方面能够作为选择性局部激动剂,降低吸烟者对尼古丁的依赖,有望广泛应用于戒烟;在镇痛方面能够反射性的兴奋呼吸,已被广泛应用于临床手术对患者的麻醉作用。本文通过对大量文献的查阅及验证,将对金雀花碱的生物活性及其相关作用机制进行总结,以期为金雀花碱的开发和利用提供理论基础。     

Molecular simulations of Taxawallin I inside classical taxol binding site of β-tubulin

A new taxoid Taxawallin I (1) along with two known taxoids (2-3) were isolated from methanolic bark extract of Taxus wallichiana Zucc. Structural characterization was confirmed by mass and NMR spectral techniques. Taxawallin I exhibited significant in-vitro anticancer activity against HepG2, A498, NCI-H226 and MDR 2780AD cancer lines. Tubulin binding assay was performed to assess its tubulin binding activity. Molecular docking analysis was performed to study the potential binding mode inside the taxol binding site of β-tubulin.     

Single agent gemcitabine chemotherapy in dogs with spontaneously occurring lymphoma

BACKGROUND: Gemcitabine has been shown to be effective as a single agent in a variety of tumors including nonHodgkin's lymphoma. Its use in veterinary medicine has been limited and to date this drug has not been used as a first-line therapy in dogs with lymphoma. HYPOTHESIS: Gemcitabine as a single agent may be efficacious in dogs presented for the first time with lymphoma. ANIMALS: Twenty-four dogs with spontaneously occurring lymphoma. METHODS: All dogs were clinically staged and given gemcitabine at 400 mg/m(2) over a 30-minute intravenous infusion weekly for 3 weeks and then given 1 week off treatment before starting a second cycle. RESULTS: A single dose of gemcitabine lowered both neutrophil count (decrease in mean neutrophil count from 10,640 cells/ microL to 3,140 cells/microL) and platelet count (decrease in mean platelet count from 201,290 cells/microL to 139,190 cells/microL) 7 days after administration. Consequently gemcitabine dosage was reduced at the second treatment in 8 of 21 dogs or a dose delay of 1-7 days and a reduction of dosage was used in 7 of 21 dogs. Seven dogs completed the assigned 4-week cycle. Two of these dogs had progressive disease and 5 had stable disease. No objective responses were seen in dogs treated with a second cycle of gemcitabine. CONCLUSIONS AND CLINICAL IMPORTANCE: Gemcitabine administration as a single agent resulted in hematologic toxicity and did not reduce lymphoma burden. If gemcitabine is to be used in veterinary medicine, additional prospective pharmacologic studies should be done to determine the appropriate dosage, regimen, and schedule of use before it can be recommended for use in the treatment of dogs with lymphoma as a single agent.     

螺旋藻的营养价值及药用特性

 螺旋藻是一类可供人和动物食用药用的微生物,重点阐述了螺旋藻及其多糖的抗疲劳、抗福射、抗癌、抗病毒作用,营养特性及其免疫力提高作用。     

Clinical evaluation of methoximorpholino-doxorubicin (FCE 23762) in dogs with spontaneous malignancies

We conducted a clinical evaluation of FCE 23762, a methoxymorpholino analog of doxorubicin, in 48 dogs with metastatic, nonresectable, or chemotherapy-resistant spontaneous malignancies at an initial dosage of 50-60 microg/kg IV every 3 weeks. Clinical evidence of toxicity was minimal; 6 dogs developed grades I, II, and III hematologic toxicities after the 1st treatment, and 1 dog developed grade II gastrointestinal toxicity. One dog became pancytopenic 4 months after discontinuation of FCE 23762. No other adverse effects were noted. Partial or complete remissions were observed in 32% of the dogs. Responses were observed both in previously untreated dogs and in those that had received prior chemotherapy, including doxorubicin. FCE 23762 is a promising new antineoplastic agent that can be used safely in dogs with cancer; doses higher than those used in this study may be used eventually in practice.     

桑黄多糖的研究进展

桑黄(Phellinus)是国际公认抗癌效果较好的大型药用真菌之一,桑黄代谢产生的多糖具有明显的抑制肿瘤和提高机体免疫力的功效,为当前新型抗癌药物研究领域的热点。就桑黄多糖的化学结构、提取纯化方式及其药理作用进行了综述,并总结了桑黄多糖的产品开发情况,旨在为开发桑黄功能保健品和药品提供理论依据。     

Investigating the cytotoxic and apoptosis inducing effects of monoterpenoid stylosin in vitro

The aim of this study was to investigate the cytotoxic and anticancer activities of stylosin, a monoterpene extracted from an edible plant, Ferula ovina, on 5637 and HFF3 cells using MTT and comet assays and DAPI staining.To assess stylosin effects, cells were cultured in the presence of various concentrations of stylosin during three days; the IC₅₀ of stylosin on cancerous 5637 cells was less than its value on HFF3 normal cells, indicating that it might have anticancer properties. Investigating the mechanism of stylosin action revealed that it quickly induced DNA lesions and increased the number of apoptotic cells.     

北沙参水提法不同提取物体外抗肿瘤的研究

［目的］研究北沙参水提法不同提取物的体外抗肿瘤活性。［方法］采用MTT法观察北沙参水提法乙醇处理后3种不同提取物对肺癌细胞株（A549）、胃癌细胞株（SGC）、肝癌细胞株（HEP）的体外药理作用。［结果］北沙参水提后醇溶物、水提后醇沉物和水提后滤渣醇溶物的不同浓度在体外对肝癌细胞株（HEP）均具有一定的抑制作用,北沙参水提后醇溶物和水提后醇沉物各浓度间无显著差异,水提后滤渣醇溶物在300.000 μg/ml时抑制率显著高于其他浓度;对肺癌细胞株（A549）,绝大部分浓度具有一定的抑制作用,水提后醇溶物浓度为37.500μg/ml时,抑制率显著高于其他浓度,水提后醇沉物各浓度间无显著差异,水提后滤渣醇溶物浓度为75.000μg/ml和18.750μg/ml时,抑制率显著高于其他浓度 而对胃癌细胞株（SGC）,只有水提后滤渣醇溶物在300.000μg/ml时具有抑制作用,且抑制率仅为6.340%,其他均没有抑制作用。［结论］北沙参水提乙醇处理后的3种提取物对肺癌细胞株（A549）和肝癌细胞株（HEP）在体外均有一定的抑制作用,但对胃癌细胞株（SGC）几乎没有抑制作用。     

青冈栎树根提取液的抗癌活性研究

[目的]探讨青冈栎树根提取液的抗癌活性。[方法]采用MTT法,以浓度分别为0．40、0．81、1．61、3．13、6．25、12．51、25．00mg/ml青冈栎树根提取液处理3种人肿瘤细胞（胃癌细胞株MGC-803、子宫颈癌细胞株Hela和肝癌细胞株BEL-7404）48h,观察不同浓度青冈栎树根提取液对上述细胞的毒性和生长抑制率。[结果]青冈栎树根提取液对3种人肿瘤细胞的生长均有抑制作用且呈剂量依赖关系,作用48h的IC50值分别为4．966、4．889和7．043mg/ml。[结论]青冈栎树根提取液在一定浓度下对3种人肿瘤细胞均有细胞毒性,显示青冈栎树根中含有抗癌的有效成分。该研究成果可为青冈栎的进一步开发和利用及研制抗癌保健药品提供理论依据。     

真瓣鳃目5种海洋贝类生物活性的研究

[目的]研究真瓣鳃目5种海洋贝类提取物的体外抗肿瘤和免疫调节活性。[方法]利用植物化学分析方法对这5种海洋贝类成分进行初步分离,将其乙醇提取液分为石油醚、乙酸乙酯、正丁醇和水4个不同极性部分,并对这些成分的抗肿瘤及免疫调节活性进行研究。[结果]5种贝类的乙醇提取物均有一定的抑制肿瘤细胞生长的作用。大多数组分对人早幼粒细胞白血病细胞HL-60有较强的抑制作用,但只有文蛤的正丁醇部分对人胃癌细胞BGC-823、四角蛤蜊的石油醚部分和文蛤的正丁醇部分对人肺癌细胞A549以及缢蛏的石油醚部分、杂色蛤仔的乙酸乙酯部分、杂色蛤仔和文蛤的正丁醇部分和青蛤的水提部分等组分对人肝癌细胞SMMC-7721有明显的抑制作用。5种贝类的大多数提取组分对小鼠脾淋巴细胞的增殖有调节作用,其中文蛤和缢蛏的增殖作用较强,文蛤的水提部分和石油醚部分对脾淋巴细胞的增殖率分别为670%和370%,缢蛏正丁醇部分对脾淋巴细胞的增殖率为500%,少数提取成分对免疫细胞的增殖具有抑制作用。[结论]真瓣鳃目5种海洋贝类提取物大多对肿瘤细胞的生长有一定的抑制作用,且对小鼠脾淋巴细胞的增殖也有较强的调节作用。