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Diverse Biological Activities of Lignins : Structure-Activity Relationship

木质素的多种生物活性：构效关系

基本信息

批准号：
05671875
负责人：
KAWAZOE Yutaka
金额：
$ 1.34万
依托单位：
Nagoya City University
依托单位国家：
日本
项目类别：
Grant-in-Aid for General Scientific Research (C)
财政年份：
1993
资助国家：
日本
起止时间：
1993 至 1994
项目状态：
已结题

项目摘要

(1) Anti-HIV activity of ligninsA class of synthetic lignins (dehydrogenation polymers of p-coumaric acid, ferulic acid, and caffeic acid) inhibited cytopathogenicity of HIV-1 and HIV-2 infection. The polymers inhibited expression of HIV-specific antigen in the infected cells and also inhibited HIV-binding to the cells, but not completely, even at doses that almost completely inhibited the HIV-induced cytopathogenic effect. These results suggest that lignin structure, regardless of whether synthetic or natural, may inhibit HIV replication by an unidentified process, and thus prove to be a new class of anti-HIV agents possibly effective in the treatment of AIDS.(2) Lignins are not mutagenic in bacterial tester strainsFor safety assessment on genotoxicity, lignins and related compounds were tested for mutagenicity in Salmonella typhimurium tester strains and none of the compounds examined were proved to be mutagenic. This paper also describes a preliminary result on their antimugtagenic property was also demonstrated. Synthetic and some natural lignins suppressed to a remarkable extent mutagenicities of 2-nitrofluorene and 1-nitropyrene.(3) Anti-tumor promoting activity of ligninsAfter 7,12-dimethylbenzanthracene was painted on the mouse skin, TPA is effective to promote tumor production. However, when synthetic lignine were administered prior to TPA treatment, tumor production was reduced up to less than 50%.(4) A water extract of coniferous slash pine induced appreciable splenocyte-mitogenesis in he mice. Mitogenesis was induced mainly in B-cell subset of splenocytes. It possible that this extract could be included in a new type of immunomodulator for promotion of the host defense mechanism.

(1)木质素的抗HIV活性一类合成木质素（对香豆酸、阿魏酸和咖啡酸的脱氢聚合物）抑制HIV-1和HIV-2感染的致细胞病变性。这些聚合物抑制了感染细胞中HIV特异性抗原的表达，也抑制了HIV与细胞的结合，但即使在几乎完全抑制HIV诱导的细胞病变效应的剂量下也不能完全抑制。这些结果表明，木质素结构，无论是合成的还是天然的，都可能通过一种未知的过程抑制HIV复制，从而证明是一类新的抗HIV药物，可能有效地治疗艾滋病。(2)木质素在细菌试验菌株中无致突变性对于遗传毒性的安全性评估，在鼠伤寒沙门氏菌试验菌株中检测了木质素和相关化合物的致突变性，结果证明所检测的化合物均无致突变性。本文还对它们的抗诱变性进行了初步研究。合成的和一些天然的木质素抑制到显着程度的2-硝基芴和1-硝基芘的致突变性。(3)将7，12-二甲基苯并蒽涂抹在小鼠皮肤上后，TPA有效地促进肿瘤的产生。然而，当在TPA治疗之前施用合成木质素时，肿瘤产生减少至小于50%。(4)针叶湿地松水提物诱导小鼠脾细胞有丝分裂。有丝分裂主要在脾细胞的B细胞亚群中诱导。该提取物有可能作为一种新型免疫调节剂，用于促进宿主的防御机制。