Konyanee Atthaphon, Chaniad Prapaporn, Phuwajaroanpong Arisara, Plirat Walaiporn, Viriyavejakul Parnpen, Septama Abdi Wira, Punsawad Chuchard
College of Graduate Studies, Walailak University, Nakhon Si Thammarat, Thailand.
School of Allied Health Sciences, Walailak University, Nakhon Si Thammarat, Thailand.
PLoS One. 2024 Dec 2;19(12):e0312047. doi: 10.1371/journal.pone.0312047. eCollection 2024.
The increased resistance of Plasmodium falciparum to artemisinin and its partner drugs poses a serious challenge to global malaria control and elimination programs. This study aimed to investigate the therapeutic potential of Mesua ferrea Linn., a medicinal plant, as a source for novel antimalarial compounds. In this study, we conducted in vitro assays to evaluate the antimalarial activity and cytotoxicity of crude extracts derived from M. ferrea L. leaves and branches. Subsequently, the most promising extracts were subjected to assessments of their antimalarial efficacy and acute oral toxicity tests in mouse models. Furthermore, selected crude extracts underwent gas chromatography-mass spectrometry (GC-MS) analysis to identify their phytochemical compositions. Our findings revealed that the ethanolic extract of M. ferrea L. branches (EMFB) exhibited high antimalarial activity, with an IC50 value of 4.54 μg/mL, closely followed by the ethanolic extract of M. ferrea L. leaves (EMFL), with an IC50 value of 6.76 μg/mL. Conversely, the aqueous extracts of M. ferrea L. branches (AMFB) and leaves (AMFL) exhibited weak and inactive activity, respectively. The selected extracts, EMFB and EMFL, demonstrated significant dose-dependent parasitemia suppression, reaching a maximum of 62.61% and 54.48% at 600 mg/kg body weight, respectively. Furthermore, the acute oral toxicity test indicated no observable toxicity at a dosage of 2,000 mg/kg body weight for both extracts. GC-MS analysis revealed abundant compounds in the EMFB, such as oleamide, cis-β-farnesene, alloaromadendrene, physcion, palmitic acid, 5-hydroxymethylfurfural, and 4H-pyran-4-one, 2,3-dihydro-3,5-dihydroxy-6-methyl-, while the EMFL contained friedelin, friedelinol, betulin, β-caryophyllene, oleamide, and 5-hydroxymethylfurfural. Notably, both extracts shared several phytochemical compounds, including 4H-pyran-4-one, 2,3-dihydro-3,5-dihydroxy-6-methyl-, 5-hydroxymethylfurfural, α-copaene, cyperene, β-caryophyllene, alloaromadendrene, palmitic acid, ethyl palmitate, and oleamide. Additionally, further study is needed to isolate and characterize these bioactive compounds from M. ferrea L. leaves and branches for their potential utilization as scaffolds in the development of novel antimalarial drugs.
恶性疟原虫对青蒿素及其联合药物的耐药性增加，给全球疟疾控制和消除计划带来了严峻挑战。本研究旨在调查药用植物铁力木作为新型抗疟化合物来源的治疗潜力。在本研究中，我们进行了体外试验，以评估铁力木叶片和树枝粗提物的抗疟活性和细胞毒性。随后，对最有前景的提取物在小鼠模型中进行抗疟疗效评估和急性口服毒性试验。此外，对选定的粗提物进行气相色谱-质谱（GC-MS）分析，以确定其植物化学成分。我们的研究结果表明，铁力木树枝乙醇提取物（EMFB）表现出较高的抗疟活性，IC50值为4.54μg/mL，其次是铁力木叶片乙醇提取物（EMFL），IC50值为6.76μg/mL。相反，铁力木树枝水提取物（AMFB）和叶片水提取物（AMFL）分别表现出较弱和无活性。选定的提取物EMFB和EMFL表现出显著的剂量依赖性疟原虫血症抑制作用，在体重600mg/kg时分别达到最大值62.61%和54.48%。此外，急性口服毒性试验表明，两种提取物在体重2000mg/kg的剂量下均未观察到毒性。GC-MS分析显示EMFB中含有丰富的化合物，如油酰胺、顺式-β-法尼烯、别香橙烯、大黄素甲醚、棕榈酸、5-羟甲基糠醛和4H-吡喃-4-酮，2,3-二氢-3,5-二羟基-6-甲基-，而EMFL中含有木栓酮、木栓醇、桦木醇、β-石竹烯、油酰胺和5-羟甲基糠醛。值得注意的是，两种提取物共有几种植物化学成分，包括4H-吡喃-4-酮，2,3-二氢-3,5-二羟基-6-甲基-，5-羟甲基糠醛、α-可巴烯、环香叶烯、β-石竹烯、别香橙烯、棕榈酸、棕榈酸乙酯和油酰胺。此外，需要进一步研究从铁力木叶片和树枝中分离和鉴定这些生物活性化合物，以潜在地将其用作开发新型抗疟药物的支架。
