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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 investigate the antibacterial and antiviral activity of stromelactam (STR), and provide some experimental evidences for the treatment of upper respiratory tract infections. Methods: In vitro and in vivo inhibition of 10 Staphylococcus aureus isolates were determined by in vitro and in vitro methods. The protective effect of Staphylococcus aureus and Streptococcus pneumoniae on mice was observed. The mice were divided into normal group , Model group and Renduining control group (crude drug dose 8.7 g · kg-1) and allosgenin lactamase low and high dose (20, 40 mg · kg-1) 7 d, 1 h after the last administration, intraperitoneal injection of Staphylococcus aureus (or Streptococcus pneumoniae) bacteria to observe the mice within 7 d of death; vaccination of influenza A virus [A / PR8 / 34 (H1N1)] and Influenza B virus (B / KYO 98-76) in MDCK (dog kidney cells) was used to observe its anti-virus effect in vitro. The anti-virus effect of influenza virus A The rats in the normal group, model group and Renduining group were treated with low dose (8.7 g · kg -1) of raw herbs and low and high dose (20,40 mg · kg -1) For 5 consecutive days. The mice were infected intranasally with virus allantoic fluid on the first day after administration, and the lungs were observed after 4 days of administration. Pathological examination and pulmonary index and inhibition rate were calculated. Results: Allisin had inhibitory activity against seven strains of Escherichia coli, with MIC of 5 g · L-1. When the concentration of 10 g · L-1 was 5 g · L-1, The diameter of the zone of inhibition was 13-25 mm. Survival rates of Staphylococcus aureus and S. pneumoniae infected mice were 70% and 55% at the dose of 40 mg · kg-1, respectively. Influenza A and B The IC50 of the virus was 0.649 and 0.233 g · L-1, respectively. The increase of pulmonary index and pulmonary lesion in mice induced by influenza A virus were also significantly reduced and ameliorated. At 40 mg · kg-1, the lung index The inhibition rate was 39.8%. Conclusion: Allisin has antibacterial and antiviral activities.