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Study of antiviral and anticancer effects of polyphenols

多酚的抗病毒和抗癌作用研究

基本信息

批准号：
15590238
负责人：
NAKASHIMA Hideki
金额：
$ 2.05万
依托单位：
St.Marianna University School of Medicine
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
2003
资助国家：
日本
起止时间：
2003 至 2004
项目状态：
已结题

项目摘要

1)Antiviral study(1)Anti-HTV assay : MT-4 cells were infected with HIV-I and incubated in the presence of various concentrations of test compounds. After incubation for 5 days, cell viability was quantified by MTT assay to estimate a inhibition activity of test compounds against HIV induced CPE. Test compounds were alkyl-ologosaccharides, synthetic peptides, and an extract from, an Indian medical plant, Indigofera cordifora.(2)Anti-HSV assay : HSV-1 infected Vero cells were incubated in the presence of test compounds and antiviral activity was evaluated as the inhibition activity against virus induced CPE.2)Study for anticancer activities(1)Assay for cytotoxic activity : Three human oral tumor cell lines, (HSG, HSC-2, HSC-3), and 3 human normal cells, (HGF, HPC, HPLF) were incubated in the presence of test compounds. After 24 h incubation, the relative viable cell number was detenraned by MTT assay.(2)Assay for DNA fragmentation : DNA fragmentation from cultured cells with test compoun … More ds treatment was determined to estimate the inhibitory activity against apoptosis.(3)L5179 mouse T cell lymphoma cell line was transfected with MDR1/A containing retrovirus and MDR1 expressing cells were selected. The reversed activity of test compounds were studied.(4)Caspase activation and anti-radical activity using by ESR spectroscopy were also carried out.(5)Anti-melanoma metastatic activity was assessed using an experimental pulmonary metastasis assay of B16-BL6 melanoma cells.According to the results of these experiments, extracts from several plants, such as Anastasia Red, demonstrate anticancer activity and inhibition of MDR expression. Tropolone derivatives have anticancer activity due to radical mediated redox reaction. 4F-benzoyl-TE14011,an analog of synthetic peptide T22 and CXCR4 antagonist, was encapsulating with a biodegradable polymer, poly D, L-lactic acid (PLA). Subcutaneous single administration of 4F-benzoyl-TE14011-PLA significantly reduced the number of colonies formed by pulmonary metastasis of B16-BL6 melanoma cells. Less

1)抗病毒研究（1）抗HIV测定：用HIV-I感染MT-4细胞，并在不同浓度的供试化合物存在下孵育。孵育5天后，通过MTT测定法定量细胞活力，以估计测试化合物对HIV诱导的CPE的抑制活性。测试化合物是烷基-寡糖、合成肽和来自印度药用植物木蓝的提取物。（2）抗HSV测定：将HSV-1感染的Vero细胞在测试化合物存在下温育，并将抗病毒活性评价为对病毒诱导的CPE的抑制活性。2）抗癌活性的研究（1）细胞毒性活性的测定：将三种人口腔肿瘤细胞系（HSG、HSC-2、HSC-3）和三种人正常细胞（HGF、HPC、HPLF）在测试化合物存在下温育。培养24 h后，MTT法测定相对活细胞数。（2）DNA片段化的测定：用测试化合物从培养的细胞中进行DNA片段化。 ...更多信息测定DS处理以评估对细胞凋亡的抑制活性。（3）用含MDR 1/A的逆转录病毒转染L5179小鼠T细胞淋巴瘤细胞系，筛选表达MDR 1的细胞。研究了供试化合物的逆转活性。（4）采用ESR波谱法研究了Caspase活性和抗自由基活性。（5）采用B16-BL 6黑色素瘤细胞肺转移实验评价抗黑色素瘤转移活性，结果表明，Anastasia Red等几种植物提取物具有抗肿瘤活性和抑制MDR表达的作用。环酚酮衍生物由于自由基介导的氧化还原反应而具有抗癌活性。将合成肽T22和CXCR 4拮抗剂的类似物4F-benzoyl-TE 14011用可生物降解的聚合物聚D，L-乳酸（PLA）包封。4F-苯甲酰基-TE 14011-PLA的皮下单次给药显著减少了B16-BL 6黑色素瘤细胞肺转移形成的集落数量。少

项目成果

期刊论文数量（99）

专著数量（0）

科研奖励数量（0）

会议论文数量（0）

专利数量（0）

Identification of novel low molecular weight CXCR4 antagonists by structural tuning of cyclic tetrapeptide-scahffolds.

通过环状四肽支架的结构调整鉴定新型低分子量 CXCR4 拮抗剂。

DOI：
发表时间：
2005
期刊：
J.Med.Chem. 48
影响因子：
0
作者：
Tamamura;H.;Araki;T.;Ueda;S.;Wang;Z.;Oishi;S.;Esaka;A.;Trent;J.O.;Nakashima;H.;Yamamoto;N.;Peiper;S.C.;Otaka;A.;Fujii;N.
通讯作者：
N.

Cytotoxic activity of Azulenequiiiones against human oral tumor cell lines.

Azulenequiiones 对人口腔肿瘤细胞系的细胞毒活性。

DOI：
发表时间：
2005
期刊：
Anticancer Res. 25
影响因子：
0
作者：
Wakabayashi;H.;Nishishiro;M.;Arikawa;S.;Hashimoto;K.;Kikuchi;H.;Nishikawa;H.;Kurihara;T.;Terakubo;S.;Shoji;Y.;Nakashima;H.;Motohashi;N.;Sakagami;H.
通讯作者：
H.

Tamamura, H., Hiramatsu, K., Nakashima, H., et al.: "Synthesis of potent CXCR4 inhibitors possessing low cytotoxicity and improved biostability based on T140 derivatives."Org.Biomol.Chem.. 1. 3656-3662 (2003)

Tamamura, H.、Hiramatsu, K.、Nakashima, H. 等人：“基于 T140 衍生物合成具有低细胞毒性和改善的生物稳定性的有效 CXCR4 抑制剂。”Org.Biomol.Chem.. 1. 3656-3662 (