Review : Herbal Medicines Are Activated by Intestinal Microflora
Review : Herbal Medicines Are Activated by Intestinal Microflora
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评论：草药被肠道微生物群激活
DOI：
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发表时间：
2002
期刊：
影响因子：
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通讯作者：
D.
中科院分区：
文献类型：
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作者：
D.
本研究以无菌动物、无菌动物和普通动物为研究对象，对中草药中的苷类化合物，如甘草苷、黄芪苷、刺楸皂苷、芦丁和Ponicirin等进行了研究，并对它们在肠道菌群中的代谢和药理作用进行了评价。口服甘草次酸（GL）后，在益生菌组和普通组大鼠的血浆和肠内容物中均检测到18β-甘草次酸（GA），而GL未检测到。但在无菌大鼠中未检测到GA。当GL与人肠道细菌孵育时，它直接代谢为GA（>95%）或通过18 β-甘草次酸-3- β-D-葡萄糖醛酸苷（<5%）代谢。口服给药GL对无菌和常规大鼠四氯化碳诱导的肝损伤有效，但对无菌大鼠无效。当人参皂苷口服给药于人类时，化合物K对肿瘤转移和变态反应具有活性。当刺楸皂苷与人体肠道菌群孵育时，它们被代谢为刺楸皂苷A、刺楸皂苷I和常春藤皂苷元。这些代谢产物对类风湿性关节炎和糖尿病有活性，而其他的刺楸皂苷没有活性。当类黄酮苷口服给药的动物，苷元和/或酚酸检测到尿液中。代谢途径由肠道细菌进行，而不是由肝脏或血液酶进行。这些代谢产物对类风湿性关节炎和糖尿病有活性，而其他的刺楸皂苷没有活性。当类黄酮苷口服给药的动物，苷元和/或酚酸检测到尿液中。代谢途径由肠道细菌进行，而不是由肝脏或血液酶进行。这些代谢产物，糖苷配基和酚酸，显示出抗肿瘤，抗血小板聚集和血小板聚集活性。这些结果表明，苷类中药是前药。
Glycosides of herbal medicines, such as glycyrrhizin, ginsenosides, kalopanaxsaponins, rutin and ponicirin, were studied regrading their metabolic fates and pharmacological actions in relation to intestinal bacterial using germ-free, gnotobiotic and conventional animals. When glycyrrhizin (GL) was orally administered, 18β-glycyrrhetinic acid (GA), not GL, was detected in plasma and intestinal contents of gnotobiotic and conventional rats. However, GA could not be detected in germ-free rats. When GL incubated with human intestinal bacteria, it was directly metabolized to GA (＞95%) or via 18 β-glycrrhetinic acid-3- β-D-glucuronide (＜5%). Orally administered GL was effective in gnotobiotic and conventional rats for liver injury induced by carbon tetrachloride, but was not effective in germ-free rats. When ginseng saponins were orally administered to human beings, compound K was active for tumor metastasis and allergy. When kalopanaxsaponins were incubated with human intestinal microflora, they were metabolized to kalopanaxsaponin, A, kalopanaxsaponin I and hederagenin. These metabolites were active for rheumatoid arthritis and diabetic mellitus while the other kalopanxsaponins were not. When flavonoid glycosides were orally administered to animals, aglycones and/or phenolic acids were detected in the urine. The metabolic pathways proceeded by intestinal bacteria rather than by liver or blood enzymes. These metabolites were active for rheumatoid arthritis and diabetic mellitus while the other kalopanxsaponins were not. When flavonoid glycosides were orally administered to animals, aglycones and/or phenolic acids were detected in the urine. The metabolic pathways proceeded by intestinal bacteria rather than by liver or blood enzymes. These metabolites, aglycones and phenolic acids, showed antitumor, antiinflammatory and antiplatelet aggregation activities. These findings suggest that glycosides of herbal medicines are prodrugs.