从蓝刺头中提取的炔属噻吩的抗疟活性
Antimalarial Activity of Acetylenic Thiophenes from Echinops hoehnelii Schweinf.
机构信息
Department of Pharmaceutical Chemistry and Pharmacognosy, School of pharmacy, College of Health Sciences, Addis Ababa University, Addis Ababa P.O. Box 9086, Ethiopia.
DDepartment of Pharmacognosy, School of Pharmacy, College of Health Sciences, Mekelle University, P.O.Box 1871, Ethiopia.
出版信息
Molecules. 2017 Nov 21;22(11):1965. doi: 10.3390/molecules22111965.
Malaria is one of the world's most severe endemic diseases and due to the emergence of resistance to the currently available medicines, the need for new targets and relevant antimalarial drugs remains acute. The crude extract, four solvent fractions and two isolated compounds from the roots of were tested for their antimalarial activity using the standard four-day suppressive method in infected mice. The 80% methanol extract exhibited suppression of 4.6%, 27.8%, 68.5% and 78.7% at dose of 50, 100, 200 and 400 mg/kg respectively. The dichloromethane fraction displayed chemosuppression of 24.9, 33.5 and 43.0% dose of 100, 200 and 400 mg/kg of body weight. Five acetylenicthiophenes were isolated from the dichloromethane fraction of which 5-(penta-1,3-diynyl)-2-(3,4-dihydroxybut-1-ynyl)-thiophene decreased the level of parasitaemia by 43.2% and 50.2% while 5-(penta-1,3-diynyl)-2-(3-chloro-4-acetoxy-but-1-yn)-thiophene suppressed by 18.8% and 32.7% at 50 and 100 mg/kg, respectively. The study confirmed the traditional claim of the plant to treat malaria and could be used as a new lead for the development of antimalarial drugs.
疟疾是世界上最严重的地方性疾病之一，由于目前可用药物的耐药性出现，仍然迫切需要新的靶点和相关的抗疟药物。使用感染小鼠的标准四天抑制法，测试了 的根的粗提取物、四种溶剂级分和两种分离化合物的抗疟活性。80%甲醇提取物在 50、100、200 和 400mg/kg 剂量下分别显示出 4.6%、27.8%、68.5%和 78.7%的抑制作用。二氯甲烷级分在 100、200 和 400mg/kg 体重剂量下显示出 24.9%、33.5%和 43.0%的化学抑制作用。从二氯甲烷级分中分离出五种炔基噻吩，其中 5-(戊-1,3-二炔基)-2-(3,4-二羟基丁-1-炔基)-噻吩使寄生虫血症水平降低了 43.2%和 50.2%，而 5-(戊-1,3-二炔基)-2-(3-氯-4-乙酰氧基-丁-1-炔基)-噻吩分别在 50 和 100mg/kg 时抑制率为 18.8%和 32.7%。该研究证实了该植物治疗疟疾的传统说法，并可作为开发抗疟药物的新先导。
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