de Souza Giovana A G, da Silva Nazaré C, de Souza Juarez, de Oliveira Karen R M, da Fonseca Amanda L, Baratto Leopoldo C, de Oliveira Elaine C P, Varotti Fernando de Pilla, Moraes Waldiney P
Laboratório de Farmacologia Experimental, Universidade Federal do Oeste do Pará - UFOPA, Brazil.
Laboratório de Farmacologia, Instituto Esperança de Ensino Superior - IESPES, Brazil.
Phytomedicine. 2017 Jan 15;24:111-118. doi: 10.1016/j.phymed.2016.11.021. Epub 2016 Dec 1.
In view of the wide variety of the flora of the Amazon region, many plants have been studied in the search for new antimalarial agents. Copaifera reticulata is a tree distributed throughout the Amazon region which contains an oleoresin rich in sesquiterpenes and diterpenes with β-caryophyllene as the major compound. The oleoresin has demonstrated antiparasitic activity against Leishmania amazonensis. Because of this previously reported activity, this oleoresin would be expected to also have antimalarial activity.
In this study we evaluated the in vitro and in vivo antimalarial potential of C. reticulata oleoresin.
In vitro assays were done using P. falciparum W2 and 3D7 strains and the human fibroblast cell line 26VA Wi-4. For in vivo analysis, BALB/c mice were infected with approximately 10 erythrocytes parasitized by P. berghei and their parasitemia levels were observed over 7 days of treatment with C. reticulata; hematological and biochemical parameters were analyzed at the end of experiment.
The oleoresin of C. reticulata containing the sesquiterpenes β-caryophyllene (41.7%) and β-bisabolene (18.6%) was active against the P. falciparum W2 and 3D7 strains (IC = 1.66 and 2.54 µg/ml, respectively) and showed low cytotoxicity against the 26VA Wi-4 cell line (IC > 100 µg/ml). The C. reticulata oleoresin reduced the parasitemia levels of infected animals and doses of 200 and 100 mg/kg/day reached a rate of parasitemia elimination resembling that obtained with artemisinin 100 mg/kg/day. In addition, treatment with oleoresin improved the hypoglycemic, hematologic, hepatic and renal parameters of the infected animals.
The oleoresin of C. reticulata has antimalarial properties and future investigations are necessary to elucidate its mechanism of action.
鉴于亚马逊地区植物种类繁多，人们对许多植物进行了研究以寻找新的抗疟药物。网脉苦配巴是一种分布于整个亚马逊地区的树木，其含有一种富含倍半萜和二萜的油树脂，其中β-石竹烯为主要成分。该油树脂已显示出对亚马逊利什曼原虫的抗寄生虫活性。基于此前报道的这种活性，预计该油树脂也具有抗疟活性。
在本研究中，我们评估了网脉苦配巴油树脂的体外和体内抗疟潜力。
使用恶性疟原虫W2和3D7菌株以及人成纤维细胞系26VA Wi-4进行体外试验。对于体内分析，用约10个被伯氏疟原虫寄生的红细胞感染BALB/c小鼠，并在使用网脉苦配巴治疗的7天内观察其疟原虫血症水平；在实验结束时分析血液学和生化参数。
含有倍半萜β-石竹烯（41.7%）和β-红没药烯（18.6%）的网脉苦配巴油树脂对恶性疟原虫W2和3D7菌株具有活性（IC50分别为1.66和2.54μg/ml），并且对26VA Wi-4细胞系显示出低细胞毒性（IC50>100μg/ml）。网脉苦配巴油树脂降低了感染动物的疟原虫血症水平，200和100mg/kg/天的剂量达到的疟原虫血症消除率类似于100mg/kg/天青蒿素所达到的水平。此外，用油树脂治疗改善了感染动物的低血糖、血液学、肝脏和肾脏参数。
网脉苦配巴油树脂具有抗疟特性，未来有必要进行研究以阐明其作用机制。
