Division of Pharmacology, Department of Diagnostic and Therapeutic Sciences, Meikai University School of Dentistry, Japan.
Pharmacol Ther. 2010 Oct;128(1):91-105. doi: 10.1016/j.pharmthera.2010.05.004. Epub 2010 Jun 12.
Lignin-carbohydrate complexes (LCCs) are major cell wall components formed by the dehydrogenation of three monolignols, p-coumaryl, coniferyl and sinapyl alcohols. Diverse pharmacological activities of LCCs distributed into various plants were summarized. LCCs showed one order higher anti-HIV activity than tannins and flavonoids. Mechanism of anti-HIV activity induction includes the inhibition of HIV adsorption to and penetration into the cells, and inhibition of reverse transcriptase and protease. Limited digestion experiments demonstrated that a phenylpropenoid polymer, but not a sugar moiety, is important for anti-HIV activity. Dehydrogenation polymers of phenylpropenoids without carbohydrate showed higher anti-HIV activity, whereas phenylpropenoid monomers were inactive, suggesting the importance of highly polymerized structure. LCCs inhibited the plaque formation and RNA polymerase activity of influenza virus, and reduced the lethality of virus infection in mice. LCCs inhibited the plaque formation of HSV-1, and oral intake of LCC-vitamin C tablet reduced the symptoms in HSV-1-infected patients. LCCs stimulated the iodination of myeloperoxidase-positive human monocytes, neutrophiles and promyelocytic leukemia that may be involved in the bacterial killing mechanism. LCCs stimulated splenocyte proliferation, and showed both pro- and anti-inflammatory activity in activated macrophage. Preliminary DNA array analysis demonstrated the activation of the signal pathway of chemokine expression via TLR2. The molecular weight, solubility, sterilization method and association with other components during extraction step may produce diverse biological activity of LCCs. Broad and potent anti-viral activity and synergism with vitamin C suggest functionality of LCC as alternative medicine.
木质素-碳水化合物复合物（LCC）是由三种单体木质素，对香豆醇、松柏醇和芥子醇脱氢形成的主要细胞壁成分。综述了分布在不同植物中的 LCC 的多种药理活性。LCC 的抗 HIV 活性比单宁和类黄酮高一个数量级。抗 HIV 活性诱导机制包括抑制 HIV 吸附和穿透细胞，以及抑制逆转录酶和蛋白酶。有限消化实验表明，具有苯丙烯聚合物，但不是糖部分，对抗 HIV 活性很重要。没有碳水化合物的苯丙烯单体的脱氢聚合物显示出更高的抗 HIV 活性，而苯丙烯单体则没有活性，这表明高度聚合的结构很重要。LCC 抑制流感病毒的斑块形成和 RNA 聚合酶活性，并降低病毒感染小鼠的致死率。LCC 抑制 HSV-1 的斑块形成，口服 LCC-维生素 C 片剂可减轻 HSV-1 感染患者的症状。LCC 刺激髓过氧化物酶阳性的人单核细胞、中性粒细胞和早幼粒细胞的碘化，这可能与细菌杀伤机制有关。LCC 刺激脾细胞增殖，并在活化的巨噬细胞中表现出促炎和抗炎活性。初步的 DNA 芯片分析表明，TLR2 信号通路的表达被激活。分子量、溶解度、灭菌方法以及在提取步骤中与其他成分的结合可能产生 LCC 的多种生物活性。广泛而有效的抗病毒活性以及与维生素 C 的协同作用表明 LCC 作为替代药物的功能。
