Diverse Biological Activities of Lignins : Structure-Activity Relationship

(1)木质素的抗HIV活性一类合成木质素(p-香豆酸、阿魏酸和咖啡酸的脱氢聚合物)可抑制HIV-1和HIV-2感染的细胞致病作用。这些聚合物抑制了感染细胞中艾滋病毒特异性抗原的表达，也抑制了艾滋病毒与细胞的结合，但并不是完全抑制，即使在几乎完全抑制艾滋病毒诱导的细胞病变效应的剂量下也是如此。这些结果表明，木质素的结构，无论是人工合成的还是天然的，都可能通过一种未知的过程抑制HIV的复制，从而被证明是一类新的抗HIV药物，可能在治疗艾滋病方面有效。(2)木质素在细菌测试菌株中没有致突变作用。为了进行遗传毒性的安全性评估，对鼠伤寒沙门氏菌测试菌株进行了木质素和相关化合物的诱变测试，结果表明，所考察的化合物均未被证明是诱变的。本文还介绍了它们的抗霉变性能的初步结果并进行了论证。人工合成的木质素和一些天然木质素对2-硝基荧烯和1-硝基吡喃的致突变性有显著的抑制作用。(3)木质素的抗肿瘤活性7，12-二甲基苯并蒽涂在小鼠皮肤上后，TPA能有效地促进肿瘤的产生。然而，当在TPA治疗前给予合成木素时，肿瘤产生减少到50%以下。(4)针叶湿地松水提物对小鼠脾细胞有丝分裂有明显的诱导作用。有丝分裂主要在B细胞亚群的脾细胞中诱导。该提取物有可能被纳入一种新型的免疫调节剂，以促进宿主防御机制。

(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.