摘要
本研究旨在筛选具有抗弓形虫活性的萜类化合物,并进行体外活性评价。对26个萜类化合物进行体外抗弓形虫增殖作用的筛选,采用CCK-8法确定活性化合物对Vero细胞的毒性和安全浓度,Giemsa染色进一步确定对弓形虫的活性,通过细胞免疫荧光、Giemsa染色和生物化学发光法评价活性化合物对弓形虫的体外活性。结果表明,26个萜类化合物中,桧烯对弓形虫有显著的活性,桧烯对RH-2F的IC50为90.76μg·mL^(-1),Giemsa染色和细胞免疫荧光的结果表明,桧烯对细胞内的两种弓形虫虫株都有显著的抗增殖作用,并且对弓形虫的入侵有极显著的抑制作用(P<0.001)。综上表明,桧烯对弓形虫的入侵和细胞内增殖具有显著的抑制作用,可作为潜在的抗弓形虫先导化合物。
This study aimed at screening terpenoids with anti-Toxoplasma gondii activity and evaluating their activity in vitro.The activity of 26 terpenoids against Toxoplasma gondii(T.gondii)in vitro was screened.The toxicity and safe concentration of these active compounds to Vero cells were determined by CCK-8 kit.The activity against T.gondii was further identified by Giemsa staining.The activity of the active compounds against T.gondii in vitro was evaluated by cell immunofluorescence,Giemsa staining and biochemical luminescence method.The results showed that among the 26 terpenoids,sabinene had a significant activity against T.gondii.The IC50 of sabinene to RH-2F was 90.76μg·mL^(-1).The results of Giemsa staining and cellular immunofluorescence showed that sabinene had significant anti-proliferative effect on two intracellular strains of T.gondii and had a very significant inhibitory effect on the invasion of T.gondii(P<0.001).It has been found that sabinene had a significant inhibitory effect on the invasion and intracellular proliferation of T.gondii,and can be used as a potential lead compound against T.gondii.
作者
邱燕华
翟斌涛
尚小飞
周绪正
李冰
张继瑜
QIU Yanhua;ZHAI Bintao;SHANG Xiaofei;ZHOU Xuzheng;LI Bing;ZHANG Jiyu(Key Laboratory of New Veterinary Medicine Engineering of Gansu Province, Key Laboratory of Veterinary Pharmaceutical Development of Ministry of Agriculture /Lanzhou Institute of Husbandry and Pharmaceutical Sciences, Chinese Academy of Agricultural Sciences, Lanzhou 730050, China)
出处
《畜牧兽医学报》
CAS
CSCD
北大核心
2021年第10期2915-2923,共9页
ACTA VETERINARIA ET ZOOTECHNICA SINICA
基金
甘肃省基础研究创新群体项目(18 JR3RA397)
肉牛牦牛产业技术体系(CARS-37)。
关键词
弓形虫
萜类化合物
莪术烯
环黄芪醇
桧烯
Toxoplasma gondii
terpenoids
curzerene
astramembrangenin
sabinene
