Shang Xiaofei, Guo Xiao, Yang Feng, Li Bing, Pan Hu, Miao Xiaolou, Zhang Jiyu
Key Laboratory of New Animal Drug Project of Gansu Province, Key Laboratory of Veterinary Pharmaceutical Development of Ministry of Agriculture, Lanzhou Institute of Husbandry Pharmaceutical Sciences, Chinese Academy of Agricultural Sciences Lanzhou 730050, PR China.
Key Laboratory of New Animal Drug Project of Gansu Province, Key Laboratory of Veterinary Pharmaceutical Development of Ministry of Agriculture, Lanzhou Institute of Husbandry Pharmaceutical Sciences, Chinese Academy of Agricultural Sciences Lanzhou 730050, PR China.
Vet Parasitol. 2017 Jun 15;240:17-23. doi: 10.1016/j.vetpar.2017.04.019. Epub 2017 Apr 20.
Adonis coerulea Maxim. is a perennial herbaceous plant that grows in scrub, grassy slope areas, and as traditional medicine it has been used to treat animal acariasis for thousands of years. In this paper, we aimed to study the acute toxicity and cytotoxicity of the methanol extract of A. coerulea (MEAC) in vivo and in vitro for supporting the clinic uses. The acaricidal activity and the mechanism of action against Psoroptes cuniculi were investigated.
The results showed that isoorientin, luteolin and apigenin were the primary compounds in MEAC. The toxicity test showed that median lethal dose (LD) and the 50% inhibitory concentration (IC) of MEAC were estimated to be more than 5000mg/kg in mice in vivo and more than 50mg/ml against RAW 264.7 and GM00637 cells in the 3-(4, 5-dimethylthiazol-2- yl)-2,5-diphenyltetrazolium bromide (MTT) test. After culturing with MEAC, the activities of superoxide dismutase (SOD), catalase (CAT), malonyldialdehyde (MDA), glutathione-S-transferase (GST), acetylcholinesterase (AChE) and Na-K-ATPase of mites were evaluated. Compared with the control group, SOD activity of MEAC-treated group of mites was inhibited, and CAT activity was activated at the preliminary phase but was gradually inhibited over the period of incubation. MDA content reached a peak at 6h and then gradually decreased. However, GST activity in the mites was activated in a dose- and time-dependent manner. AChE and Na-K-ATPase activities related to neural conduction, vital functions and the transmembrane ion gradient of the mites were inhibited.
MEAC is safe in the given doses in both the in vitro and the in vivo tests, can be applied in the clinic and it had good acaricidal activity. The extension of the incubation time in the mites led to dynamic disequilibrium between the production and clearing of superoxide anions, a disruption of the energy metabolism and the transmembrane ion gradient, and the inhibition of motor function. These factors may have resulted in mite death.
冰凉花是一种多年生草本植物,生长于灌木丛、草坡地区,作为传统药物,它已被用于治疗动物螨虫病达数千年之久。在本文中,我们旨在研究冰凉花甲醇提取物(MEAC)在体内和体外的急性毒性和细胞毒性,以支持其临床应用。我们还研究了其杀螨活性及对兔痒螨的作用机制。
结果表明,异荭草素、木犀草素和芹菜素是MEAC中的主要化合物。毒性试验表明,在体内试验中,MEAC对小鼠的半数致死剂量(LD)估计超过5000mg/kg,在3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐(MTT)试验中,对RAW 264.7和GM00637细胞的半数抑制浓度(IC)超过50mg/ml。用MEAC培养后,评估了螨虫的超氧化物歧化酶(SOD)、过氧化氢酶(CAT)、丙二醛(MDA)、谷胱甘肽-S-转移酶(GST)、乙酰胆碱酯酶(AChE)和钠钾-ATP酶的活性。与对照组相比,MEAC处理组螨虫的SOD活性受到抑制,CAT活性在初期被激活,但在孵育期间逐渐受到抑制。MDA含量在6小时达到峰值,然后逐渐下降。然而,螨虫体内的GST活性以剂量和时间依赖性方式被激活。与螨虫神经传导、重要功能和跨膜离子梯度相关的AChE和钠钾-ATP酶活性受到抑制。
在体外和体内试验的给定剂量下,MEAC是安全的,可应用于临床,且具有良好的杀螨活性。螨虫孵育时间的延长导致超氧阴离子产生与清除之间的动态失衡、能量代谢和跨膜离子梯度的破坏以及运动功能的抑制。这些因素可能导致螨虫死亡。