红色红曲霉Mr-1的次级代谢产物生物活性成分分析

【背景】红曲霉(Monascus)是一种重要的药食同源性真菌,其自身产生的次级代谢产物具有多种生理活性功能,然而红曲霉中的生物活性成分却鲜有报道。利用红曲霉发酵液进行药效物质成分追溯,对了解红曲霉药效物质基础具有十分重要的意义。【目的】对红色红曲霉(M.ruber)Mr-1次级代谢产物中的生物活性成分和生物学功能进行研究。【方法】采用硅胶柱、SephadexLH-20凝胶柱等色谱技术对活性成分进行分离纯化,通过核磁共振和高分辨质谱技术对化合物结构进行解析;对鉴定的化合物进行体外抗氧化、抑菌和酶活性测定。【结果】从红色红曲霉Mr-1次级代谢产物中分离得到4个活性化合物,鉴定为3个黄酮类化合物Luteolin(1)、Hesperetin(2)、Glycitein(3)和1个萜类化合物Ursolic acid(4)。化合物1、2、4为首次从红曲菌科中分离得到。在抗氧化试验中,化合物1对ABTS⁺、DPPH和OH^-自由基具有较强的清除能力,IC₅₀分别为13.36、8.74和32.75μg/mL;在抑菌试验中,化合物4对金黄色葡萄球菌(Staphylococcus aureus)和李斯特菌(Listeria monocytogenes)表现出中等强度的抑菌能力,抑菌圈直径分别为13.4 mm和11.9 mm;在α-葡萄糖苷酶抑制活性试验中,化合物4表现出很强的抑制能力,IC₅₀为21.34μg/mL。【结论】红色红曲霉Mr-1是宝贵的微生物种质资源,其产生的次级代谢产物生物活性成分多样,具有开发成功能性食品原料的潜能。

Bioactive components of secondary metabolites from Monascus ruber Mr-1

Background]Monascus is an important food and drug homologous fungus,whose secondary metabolites have many physiological functions.However,the bioactive components in Monascus are rarely reported.It is of great significance to trace the active substances in Monascus fermentation broth for understanding the material basis of Monascus efficacy.Objective]To study the bioactive components and biological functions of secondary metabolites of Monascus ruber Mr-1.Methods]The active components were separated and purified by silica gel column and Sephadex LH-20.The structures of the compounds were analyzed by NMR and HR-ESI-MS.The antioxidant,antibacterial and enzyme activities of the identified compounds were determined in vitro.Results]Four active compounds were isolated from the secondary metabolites of Monascus ruber Mr-1,which were identified as three flavonoids,luteolin(1),hesperetin(2),glycoitin(3),and one terpenoid,ursolic acid(4).Compounds 1,2 and 4 were isolated from Monascus for the first time.In the antioxidant test,compound 1 had strong scavenging ability to ABTS⁺,DPPH and OH^-,with IC50 of 13.36,8.74 and 32.75μg/mL,respectively;in the antibacterial test,compound 4 showed moderate antibacterial activity against Staphylococcus aureus and Listeria monocytogenes,and the diameter of inhibition zone was 13.4 and 11.9 mm,respectively;in theα-glucosidase inhibitory activity test,compound 4 showed a strong inhibitory activity,with IC50 of 21.34μg/mL.Conclusion]Monascus ruber Mr-1 is a valuable microbial germplasm resource.Its metabolites contain diverse bioactive components and it has the potential to be developed into functional food materials.