异长春花苷内酰胺抗菌、抗病毒作用研究  

Antibacterial and Antiviral Effects of Strictosamide

作　　者：李娜[1,2] 曹亮[1,2] 丁岗[1,3] 萧伟[1,3] 

机构地区：[1]江苏中康药物科技有限公司,南京210017 [2]江苏康缘药业股份有限公司,江苏连云港222000 [3]中药制药过程新技术国家重点实验室,江苏连云港222000

出　　处：《中国实验方剂学杂志》2012年第15期170-174,共5页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家重大新药创制项目(2009ZX09103-379);江苏省科技支撑-社会发展项目(BE2009618)

摘　　要：目的:考察异长春花苷内酰胺(strictosamide,STR)的抗菌、抗病毒活性,为其用于治疗上呼吸道感染提供一定的实验依据。方法:采用试管法与平皿法测定其对标准金黄色葡萄球菌等10株菌株的体外抑制作用,并观察对金黄色葡萄球菌和肺炎双球菌感染小鼠的保护作用,即将小鼠分为正常组,模型组,热毒宁对照组(生药剂量8.7 g·kg-1)及异长春花苷内酰胺低、高剂量(20,40 mg·kg-1)组,每天ip给药1次,连续7 d,末次给药后1 h,腹腔注射金黄色葡萄球菌(或肺炎双球菌)菌液,观察小鼠7 d内死亡情况;接种甲型流感病毒[A/PR8/34(H1N1)]和乙型流感病毒(B/京防98-76)于MDCK(狗肾细胞),观察其体外抗病毒作用,并采用甲型流感病毒感染小鼠模型考察其体内抗病毒作用,即将小鼠分为正常组,模型组,热毒宁对照组(生药剂量8.7 g·kg-1)及异长春花苷内酰胺低、高剂量(20,40 mg·kg-1)组,每天ip给药1次,连续5 d,于给药第1天以病毒尿囊液滴鼻感染小鼠,继续给药4 d后观察肺部病变,作病理组织学检查,计算肺指数与抑制率。结果:异长春花苷内酰胺对标准大肠杆菌等7株菌株具有抑制作用,MIC均为5 g·L-1;质量浓度为10 g·L-1时,对肺炎双球菌等5株菌株的抑菌圈直径为13～25 mm;40 mg·kg-1时可分别使金黄色葡萄球菌和肺炎双球菌感染小鼠的存活率达70%和55%;其体外对甲型与乙型流感病毒的IC50分别为0.649,0.323 g·L-1;对甲型流感病毒所致的小鼠肺指数升高与肺组织病变亦有明显降低和改善作用,40 mg·kg-1时的肺指数抑制率为39.8%。结论:异长春花苷内酰胺具有抗菌、抗病毒活性。Objective：To observe the antibacterial and antiviral activities,and provide certain experimental data for strictosamide that is intended for upper respiratory tract infection.Method： The in vitro antibacterial activities on standard staphylococcus aureus and other 9 strains were observed by both test-tube and plating methods,and the protective effects on mice infected by staphylococcus aureus and streptococcus pneumonia were also observed.Mice were divided into 5 groups,such as normal group,model group,reduning group（crude drugs 8.7 g·kg-1）,low and high dosage（20,40 mg·kg-1） of strictosamide groups.They were injected intraperitoneally once a day for 7 days.At 1 h after the last injection,staphylococcus aureus or streptococcus pneumonia was injected intraperitoneally to mice,and then the death of mice was observed within 7 days.The in vitro antiviral activities were observed on the model of MDCK cells infected by influenza A（A/PR8/34（H1N1）） and B（B/Jingfang 98-76） virus,and the in vivo antiviral activities were observed by the model of mice infected by influenza A virus.Mice were divided into 5 groups,such as normal group,model group,reduning group（crude drugs 8.7 g·kg-1）,low and high dosage（20,40 mg·kg-1） of strictosamide groups.They were injected intraperitoneally once a day for 5 days,and virus was given to mice by nose on the first day.After the last injection,the lung lesions and pathological changes were observed,and the pulmonary index was also calculated.Result： Strictosamide had inhibiting effects on standard escherichia coli and other 6 strains in vitro with MIC of 5 g·L-1.At 10 g·L-1,the diameters of inhibiting bacteria circle of diplococcus pneumonia and other 4 strains were 13-25 mm.At 40 mg·kg-1,the survival rate of mice infected by staphylococcus aureus and streptococcus pneumonia was 70% and 55%,separately.Strictosamide showed inhibitory effects on both influenza A and B viruses in vitro with IC50 values of 0.649,0.323 g·L-1,respectively.It also significant

关 键 词：异长春花苷内酰胺 抗菌作用 抗病毒作用 胆木 

分 类 号：R285.5[医药卫生—中药学]