Efficient synthesis of panaxadiol derivatives using continuous-flow microreactor and evaluation of anti-tumor activity

An efficient method has been developed for the synthesis of a series of(20R)-panaxadiol derivatives(4a–w) using a continuous-flow microreactor.The antitumor activities of the newly synthesized compounds were evaluated in vitro in two human prostate adenocarcinoma tumor cell lines(i.e.,PC-3and LNCa P cells),and their cytotoxicities were evaluated using a standard MTT assay.Compounds 4c,4h,4p,4q and 4s exhibited higher antitumor activities toward PC-3 cell line than panaxadiol,which was used as a reference standard.     

Synthesis and in vitro biological evaluation of nitric oxide-releasing derivatives of hydroxylcinnamic acids as anti-tumor agents

Novel furoxan-based nitric oxide-releasing derivatives 6a-p of hydroxylcinnamic acids were synthesized by coupling the carboxyl group of hydroxylcinnamic acids with furoxan through various alkylol amines. Compounds 6a, e-i and m-p displayed more potent anti-tumor activities superior to control 5-fluorouracil (5-FU) in most cancer cells tested. Furthermore, 6f could selectively inhibit tumor cells, but not non-tumor cell proliferation. This inhibition was attributed to high levels of NO released in cancer cells and potentially synergistic effect of NO donor moieties and the bioactivity of hydroxylcinnamic acids.     

Effect of sonication on different quality parameters of Pinus massoniana pollen

A study was initiated with the objective of evaluating the effects of sonication treatment on important quality parameters of extract of Pinus massoniana pollen. Sonication of extract was done (frequency 20 kHz and various amplitude levels) for 10, 30, 50 min, respectively. As results, total polysaccharide, phenolics and flavonoids significantly increased (P < 0.05). And sonicated P. massoniana pollen displays strong immuno-stimulating activity by increasing proliferations of splenic lymphocytes and subsets of CD4+ T cells (CD3+CD4+), CD8 T cells (CD3+CD8+), and increased Ig secretion. Sonicated P. massoniana pollen also showed anti-tumor function by inhibition of tumor cell proliferation, inhibition of ROS production, up-regulation of GSH/GSSG ration, up-regulating the gene expression of P53, Bax and down-regulating the gene expression of Bcl-2. Findings of the present study suggested the sonication treatment of P. massoniana pollen could improve the quality and bioactivity of P. massoniana pollen, indicating that sonication is effective in processing of pollen and could be a potential process in tumor prevention and treatment.     

Enantiodivergent synthesis of (−)-methylenolactocin and (+)-methylenolactocin from d-mannitol

An enantiodivergent synthesis of both enantiomers of methylenolactocin is described through stereocontrolled addition of n-pentyl magnesium bromide to two d-mannitol-derived diastereomerically related aldehydes having an α-chiral center with a β hetero atom.     

Synthesis,characterization, crystal structures, in vitro and in vivo antitumor activity of palladium(II) and zinc(II) complexes with 2-formyl and 2-acetyl pyridine N(4)-1-(2-pyridyl)-piperazinyl thiosemicarbazone

The present paper includes synthesis and spectral characterization of the novel prepared palladium(II) and zinc(II) complexes with 2-formyl pyridine N(4)-1-(2-pyridyl)-piperazinyl thiosemicarbazone, HFo4Npypipe, 1 and the 2-acetyl pyridine N(4)-1-(2-pyridyl)-piperazinyl thiosemicarbazone, HAc4Npypipe, 2. The Pd(II) complexes [PdCl(Fo4Npypipe)], 3, [PdCl(Ac4Npypipe)], 4 and the Zn(II) complexes [ZnCl₂(Fo4Npypipe)], 5 and [ZnCl₂(Ac4Npypipe)], 6 have been characterized by elemental analyses and spectroscopic studies. The crystal structure of the complexes [PdCl(Fo4Npippy)], 3 and [PdCl(Ac4Npippy)], 4, have been solved by single-crystal X-ray diffraction. The electronic, IR, UV/Vis, and NMR spectroscopic data of the complexes are reported. The results of the cytotoxic activity of 1–6 have been evaluated in vitro against the cells of three human cancer cell lines: MCF-7, T24, A-549 and a mouse L-929 (a fibroblast-like cell line cloned from strain L). For selected compounds 2 and 6 the acute toxicity and antitumor activity were evaluated on leukemia P388-bearing mice. The Zn(II) compounds 5 and 6 are considered as agents with potential antitumor activity, and can therefore be candidates for further stages of screening in vitro and/or in vivo.     

新型青蒿砜-哌嗪-磺酰胺类衍生物的合成及抗癌活性

以双氢青蒿素为起始原料,经胺化、氧化、烷基化、胺化和酰化反应,快速、高效地合成了青蒿砜及其衍生物,并对所有化合物进行了结构确定.采用四甲基偶氮唑盐比色法(MTT法)研究了该类化合物对人肝癌细胞株SMMC-7721的细胞毒活性,初步研究结果表明,该类化合物具有明显的抑制人肝癌细胞增殖、诱导其凋亡的细胞活性,给药72h,半抑制浓度IC50最优值为0.09μmol/mL.     

VP-16与DNA分子间电子转移的光谱学研究

运用脉冲辐解和圆二色谱技术,对用于治疗肿瘤的依托泊甙(VP-16)与鸟苷酸(GMP)和小牛胸腺DNA分子间电子转移的光谱进行了探讨。用脉冲辐解技术发现了VP-16与GMP之间的电子转移,测得两者之间的反应速率常数为3.16×107 L·mol-1·s-1,并对它们的吸收光谱进行了归属,同时用圆二色谱技术发现了VP-16与小牛胸腺DNA之间相互作用。从而为医学工作者进一步了解和探讨VP-16的抗肿瘤机理提供了直接的理论依据。     

离子型有机锡化合物的合成及其生物活性

利用有机锡卤化物与有机酸在有机胺存在下反应合成了一系列离子型有机锡化合物,分子通式为[HNR3][(PhCH2)3Sn(μ2-SCH2COO)Cl]、[HNR3][Ph3Sn)3(O2CCH2CO2)2]·CH3CH2OH和[HNR3] [MeCy2ClSnO2CCH2CO2SnClCy2Me]。化合物的体外抗肿瘤、杀菌和杀螨活性测试结果表明,部分化合物具有很好的生物活性。[HNR3][(Ph3Sn)3(O2CCH2CO2)2]·CH3CH2OH和[HNR3] [MeCy2ClSnO2CCH2CO2SnClCy2Me]配合物对人肺癌细胞株A-549、结肠癌细胞株HCT-8和肝癌细胞株Bel-7402的抑制率约为90%,[HNR3][MeCy2ClSnO2CCH2CO2SnClCy2Me]配合物对小麦赤霉、番茄早疫、芦笋茎枯、苹果轮纹、花生褐斑的杀死率都为100%,配合物[HNR3] [MeCy2ClSnO2CCH2CO2SnClCy2Me]的杀螨活性致死率大于90%。     

Anticancer Effects of Fusion Protein CAtin on DMBA-induced Carcinogenesis in Buccal Pouch of Chinese Hamster

Aberrant expression ofcarcinoembryonic antigen(CEA)is a common feature for multiple types of cancer,which makes it an attractive target for anticancer therapy.CAtin is a novel dual cancer-specific fusi...     

基于喹喔啉结构的异吲哚啉-1-酮类化合物合成及抗肿瘤活性

本文通过3-溴甲基喹喔啉-2-羧酸乙酯与芳胺或脂肪胺在回流的乙醇中经一步反应简便而有效合成了一系列结构新颖的基于喹喔啉结构的异吲哚啉酮类化合物.采用MTT法初步评价了目标化合物对肺癌细胞株A549和直肠癌细胞株HT29的体外增殖抑制活性.结果 表明,含有卤素(F,Cl,Br,I)取代的化合物7h～7k对这两个细胞株表现...