Ekasari Wiwied, Fatmawati Dwi, Khoiriah Siti M, Baqiuddin Wenda A, Nisa Hawi Q, Maharupini Adinda A S, Wahyuni Tutik S, Oktarina Rice D, Suhartono Eko, Sahu Ram K
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Airlangga University, Surabaya 60115, East Java, Indonesia.
Department of Medical Chemistry/Biochemistry, Faculty of Medicine, Lambung Mangkurat University, Banjarmasin 70122, South Kalimantan, Indonesia.
Scientifica (Cairo). 2022 Sep 8;2022:3552491. doi: 10.1155/2022/3552491. eCollection 2022.
(L.) Merr., in the Indonesian local name known as "Katuk," is a tropical shrub plant of the family Euphorbiaceae. Based on genus and chemotaxonomic approaches, as well as in vitro testing of , leaves of are presumed to have an active compound content as an antimalarial. The current study aims to investigate the antimalarial activity of 96% ethanol extract and fractions of leaves. The ethanolic extract was fractionated using the vacuum liquid chromatography (VLC) method with three solvents of different polarities (n-hexane, chloroform, and 96% ethanol). The fraction obtained was then evaluated for antimalarial activity against 3D7 strain. The ethanolic extract was evaluated for antimalarial suppressive and prophylactic activity against -infected mice, as well as inhibitory activity against the heme detoxification process in vitro. Fractionation of ethanolic extract resulted in seven combined fractions, with the most active fraction being FV (50% inhibitory concentration (IC) = 2.042 g/mL). The ethanolic extract showed good parasitic suppressive (therapeutic) activity with a median effective dose (ED) value of 15.35 mg/kg body weight. In a prophylactic test, ethanolic extract showed parasite growth inhibitory activity of 67.74 ± 9.21% after the administration of 400 mg/kg body weight for 4 days before infection, and 65.30 ± 10.44% after the administration of 200 mg/kg body weight for 8 consecutive days (4 days before and after infection). The ethanolic extract also showed an effect in inhibiting the formation of -hematin of about 26.87-79.36% at a concentration of 0.1-4 mg/mL and an IC value of 0.479 mg/mL. The leaves were shown to have antimalarial activity in vitro and in vivo, where ethanolic extract were more active compared with the fraction obtained. The antimalarial properties of the extract showed a higher suppressive activity than prophylactic activity.
（L.）Merr.，在印尼当地被称为“Katuk”，是大戟科的一种热带灌木植物。基于属和化学分类学方法，以及对其进行的体外测试，推测其叶子含有作为抗疟药的活性化合物。本研究旨在调查其叶子96%乙醇提取物及其馏分的抗疟活性。乙醇提取物采用真空液相色谱（VLC）法，用三种不同极性的溶剂（正己烷、氯仿和96%乙醇）进行分馏。然后对得到的馏分针对恶性疟原虫3D7株进行抗疟活性评估。对乙醇提取物针对感染疟原虫的小鼠进行抗疟抑制和预防活性评估，以及在体外对血红素解毒过程的抑制活性评估。乙醇提取物分馏得到七个合并馏分，活性最高的馏分为FV（50%抑制浓度（IC）=2.042 g/mL）。乙醇提取物显示出良好的寄生虫抑制（治疗）活性，中位有效剂量（ED）值为15.35 mg/kg体重。在预防试验中，乙醇提取物在感染前4天给予400 mg/kg体重后，显示出67.74±9.21%的寄生虫生长抑制活性，在连续8天（感染前4天和感染后4天）给予200 mg/kg体重后，显示出65.30±10.44%的寄生虫生长抑制活性。乙醇提取物在0.1 - 4 mg/mL浓度下还显示出对疟原虫血红素形成的抑制作用，抑制率约为26.87 - 79.36%，IC值为0.479 mg/mL。其叶子在体外和体内均显示出抗疟活性，其中乙醇提取物比得到的馏分更具活性。提取物的抗疟特性显示出比预防活性更高的抑制活性。
