Williams C F, Vacca A R, Dunham L, Lloyd D, Coogan M P, Evans G, Graz M, Cable J
Cardiff University, School of Biosciences, Museum Avenue, Cardiff CF10 3AT, Wales, UK.
Cardiff University, School of Biosciences, Museum Avenue, Cardiff CF10 3AT, Wales, UK.
Mol Biochem Parasitol. 2016 Mar-Apr;206(1-2):20-8. doi: 10.1016/j.molbiopara.2016.03.001. Epub 2016 Mar 9.
Spironucleus vortens is a protozoan parasite associated with significant mortalities in the freshwater angelfish, Pterophyllum scalare. Control of this parasite is especially problematic due to restrictions on the use of the drug of choice, metronidazole (MTZ), on fish farms. Use of garlic (Allium sativum) is undergoing a renaissance following experimental validations of its antimicrobial efficiency. Ajoene ((E,Z)-4,5,9-trithiadodeca-1,6,11-triene 9-oxide), is a stable transformation product of allicin, the primary biologically active component of garlic. In the current study, an ajoene oil crude extract had a minimum inhibitory concentration (MIC) of 40μg/ml against S. vortens. GC-MS and NMR spectroscopy revealed this ajoene extract contained a mixture of the (E) and (Z)-ajoene isomers along with diallyl disulphide (DADS) and diallyl trisulphide (DATS). The only component of the ajoene crude oil found to substantially inhibit S. vortens growth by optical density monitoring (Bioscreen C Reader) was (Z)-ajoene (MIC 16μg/ml). Ajoene oil acted in synergy with MTZ in vitro, reducing the individual MIC of this drug (4μg/ml) by 16-fold, and that of ajoene oil by 200-fold with a fractional inhibitory concentration (FIC) index of 0.263. This synergistic interaction was confirmed in vivo. S. vortens-infected Pterophyllum scalare angelfish dosed orally with 0.5% (v/w) MTZ combined with 0.05% (v/w) ajoene displayed a significant reduction in faecal trophozoite count, whilst those fed on 0.5% MTZ flakes (half the recommended oral dose) alone did not. This study demonstrates for the first time the synergistic interaction between the synthetic drug MTZ and natural ajoene oil both in vitro and in vivo. Future work should evaluate the potential synergy of ajoene and MTZ against MTZ-resistant bacteria and protists.
旋核涡鞭毛虫是一种原生动物寄生虫,与淡水神仙鱼(Pterophyllum scalare)的大量死亡有关。由于养鱼场对首选药物甲硝唑(MTZ)的使用限制,控制这种寄生虫尤其成问题。在大蒜抗菌效率的实验验证之后,大蒜(Allium sativum)的使用正在复兴。阿霍烯((E,Z)-4,5,9-三硫杂十二碳-1,6,11-三烯9-氧化物)是大蒜素的稳定转化产物,大蒜素是大蒜的主要生物活性成分。在当前研究中,一种阿霍烯油粗提物对旋核涡鞭毛虫的最低抑菌浓度(MIC)为40μg/ml。气相色谱-质谱联用(GC-MS)和核磁共振光谱(NMR)显示,这种阿霍烯提取物含有(E)-阿霍烯和(Z)-阿霍烯异构体的混合物,以及二烯丙基二硫化物(DADS)和二烯丙基三硫化物(DATS)。通过光密度监测(Bioscreen C Reader)发现,阿霍烯原油中唯一能显著抑制旋核涡鞭毛虫生长的成分是(Z)-阿霍烯(MIC为16μg/ml)。阿霍烯油在体外与MTZ协同作用,将该药物的个体MIC(4μg/ml)降低了16倍,将阿霍烯油的MIC降低了200倍,部分抑菌浓度(FIC)指数为0.263。这种协同相互作用在体内得到了证实。用0.5%(v/w)MTZ与0.05%(v/w)阿霍烯口服给药的感染旋核涡鞭毛虫的淡水神仙鱼粪便滋养体数量显著减少,而仅喂食0.5%MTZ薄片(推荐口服剂量的一半)的鱼则没有。这项研究首次证明了合成药物MTZ与天然阿霍烯油在体外和体内的协同相互作用。未来的工作应该评估阿霍烯和MTZ对耐MTZ细菌和原生生物的潜在协同作用。