毛萼香茶菜中黄酮和二萜化合物的分离制备及其抗病毒活性

Antiviral activities of flavonoids and diterpenoids isolated from Isodon eriocalyx (Dunn.) Hara

从毛萼香茶菜中分离制备2种黄酮和2种二萜化合物,并研究其体外抗病毒活性。首先采用硅胶、ODS、制备型HPLC等多种色谱技术和波谱方法,从毛萼香茶菜乙醇提取物中分离制备了4个化合物,分别鉴定为8-羟基蓟黄素(1)、蓟黄素(2)、假细锥甲素(3)、毛萼晶D(4)。然后对毛萼香茶菜乙醇提取物和4个化合物开展了体外抗流感病毒(H1N1,H3N2)和呼吸道合胞病毒(RSV)活性研究。结果显示,毛萼香茶菜乙醇提取物和4个化合物对流感病毒H1N1均有一定的抑制作用,其中化合物1和2的抑制效果较优,半数有效浓度(EC50)分别为(14. 45±4. 90)和(24. 54±3. 82)μmol/L。但化合物1和2对H3N2和RSV的抑制作用则相对较弱。以上结果表明,毛萼香茶菜乙醇提取物及化合物1~4有一定的抗病毒作用,尤其是对甲型流感病毒H1N1具有较好的抑制作用,黄酮类化合物可能是其抗病毒作用的有效物质之一,本研究为毛萼香茶菜的临床应用提供了科学依据。

This study aims to isolate two flavonoids and two diterpenoids from Isodon eriocalyx(Dunn.)Hara and investigate their antiviral activities in vitro.Firstly,four compounds were isolated from the ethanol extract of I.eriocalyx by silica gel,ODS and RP-HPLC chromatography,and then identified by spectral data as isothymusin(1),cirsimaritin(2),coetsoidin A(3),and maoecrystal D(4).Next,in vitro antiviral activities against influenza(H1N1/H3N2)and respiratory syncytial virus(RSV)was investigated for the ethanol extract of I.eriocalyx and four compounds.Results showed that the ethanol extract of I.eriocalyx and four compounds exhibited inhibitory effects against influenza H1N1.Especially,compounds 1 and 2 showed better activities with EC 50 of(14.45±4.90)and(24.54±3.82)μmol/L.However,they showed weak inhibitory effects against influenza H3N2 and RSV.These results demonstrate that the ethanol extract of I.eriocalyx and compounds 1 4 have antiviral activity,especially against influenza H1N1.The flavonoids may be one kind of the effective antiviral substances.This study provides a scientific basis for the clinical application of I.eriocalyx.