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.     

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.     

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。     

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。     

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。     

柠檬抗癌活性成分研究进展

柠檬含丰富的营养和生物活性物质,具有重要的营养、医药和保健价值,柠檬的类黄酮、柠檬苦素类似物、单萜类、香豆素类等多种活性成分,具有抗氧化、抗癌的功效。系统地综述了近年来柠檬中具有抗癌作用的生物活性成分的抗癌活性研究进展,旨在为进一步开发利用柠檬资源提供新信息。     

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。