肠道菌群对中药有效成分的生物转化研究进展

肠道是口服药物在体内代谢的重要场所,肠道内寄居的大量细菌对药物的生物转化起到了不可避免的作用,因而近年来肠道菌群对中药有效成分的生物转化研究已经成为国内外学者关注的热点,作者综述了近年来肠道菌群对中药单一有效成分以及复方成分的代谢转化研究,探索总结肠道菌群对中药有效成分代谢转化的一般规律。检索中国期刊全文数据库、中文生物学期刊数据库、中文科技期刊全文数据库、中国生物医学数据库、万方数据库、中国中医药在线、Pub Med、数据库中肠道菌群对中药有效成分代谢转化的相关研究文献,提取文献中有效信息。在肠道菌群的作用下,苷类化合物水解后生成苷元而发挥药理作用;生物碱类化合物易发生水解和脱水,双酯型生物碱可转化为相对应的单酯型和脂类生物碱,从而降低毒性;内酯类化合物可能引起内酯结构断裂或脱甲基等反应。肠道菌群在中药复方的代谢中也起到证实配伍合理性以及增效减毒的重要作用。多类中药有效成分均在肠道菌群的作用下,在体内发生了生物转化,引起结构的改变而形成新的活性成分。肠道菌群对中药有效成分及中药复方的代谢起重要作用。

Research Progress of Biotransformation on Effective Ingredients of Chinese Medicine Via Intestinal Bacteria

The intestine is an important place for oral drug metabolism in the body, a large number of bacteria in the gut has played an inevitable role in drug biological conversion. Thus, the intestinal flora biotransformation of the active ingredients of traditional Chinese medicine (TCM) has become the focus of attention in recent years. In order to further explore the regularization of biotransformation, the relevant literatures of biotransformation on TCM including a single active ingredient and compound ingredients were collected. Related literature searches were performed in CNKI, CMCC, VIP, CBM WanFang and PubMed Data in the past 20 years. The results implied that the glycosides could be hydrolyzed to aglycone;alkaloids could be hydrolysised and dehydrated easily;diester could be converted to the corresponding mono-type alkaloids and lipids, which reduced the toxicity;lactones structure may cause breakage or demethylation reactions. In vivo biotransformations were occurred in many types of active ingredients of TCM via intestinal flora, which caused changes in the structure or the formation of new active ingredients. Intestinal flora also played an important role in the metabolism of TCM, such as for the confirmation of the rationality and efficiency of herbal compatibility.