Zin Nik Nor Imam Nik Mat, Mohamad Mira Nabila, Roslan Keusar, Abdul Wafi Sazeli, Abdul Moin Nurul I'zaaz, Alias Azamuddin, Zakaria Yusmazura, Abu-Bakar Nurhidanatasha
School of Health Sciences, Universiti Sains Malaysia, Kubang Kerian, Kelantan, Malaysia.
Pengiran Anak Puteri Rashidah Sa'adatul Bolkiah Institute of Health Sciences, Universiti Brunei Darussalam, Brunei Darussalam.
Malays J Med Sci. 2020 Jul;27(4):36-50. doi: 10.21315/mjms2020.27.4.4. Epub 2020 Aug 19.
The spread of resistance in common antimalarial drugs, including artemisinin-based combination therapies, has necessitated the discovery of new drugs with novel mechanisms of action. In the present study, the in vitro antimalarial and toxicological activities of acetone, methanol, ethanol and aqueous extracts of () galls were investigated.
The extracts were assessed for the antimalarial potential using a malarial SYBR Green I fluorescence-based (MSF) assay, while the toxicity was screened by using brine shrimp lethality test (BSLT), haemolytic assay, and cytotoxicity assay against normal embryo fibroblast cell line (NIH/3T3) and normal kidney epithelial cell line (Vero).
The acetone extract showed the highest antimalarial activity (50% inhibitory concentration, IC = 5.85 ± 1.64 μg/mL), followed by the methanol extract (IC = 10.31 ± 1.90 μg/mL). Meanwhile, the ethanol and aqueous extracts displayed low antimalarial activity with IC values of 20.00 ± 1.57 and 30.95 μg/mL ± 1.27 μg/mL, respectively. The significant antimalarial activity was demonstrated in all extracts and artemisinin ( < 0.05). All extracts were non-toxic to brine shrimps (50% lethality concentration, LC > 1000 ppm). Furthermore, no occurrence of haemolysis (< 5%) was observed in normal erythrocytes when treated with all extracts compared to Triton X-100 that caused 100% haemolysis ( < 0.05). The acetone and methanol extracts were non-toxic to the normal cell lines and statistically significant to artemisinin ( < 0.05).
Taken together with satisfactory selectivity index (SI) values, the acetone and methanol extracts of galls could serve as an alternative, promising and safe antimalarial agents.
包括青蒿素联合疗法在内的常见抗疟药物耐药性的传播，使得有必要发现具有新作用机制的新药。在本研究中，对（）没食子的丙酮、甲醇、乙醇和水提取物的体外抗疟和毒理学活性进行了研究。
使用基于疟原虫SYBR Green I荧光的（MSF）测定法评估提取物的抗疟潜力，同时通过卤虫致死试验（BSLT）、溶血试验以及针对正常胚胎成纤维细胞系（NIH/3T3）和正常肾上皮细胞系（Vero）的细胞毒性试验来筛选毒性。
丙酮提取物显示出最高的抗疟活性（50%抑制浓度，IC = 5.85 ± 1.64 μg/mL），其次是甲醇提取物（IC = 10.31 ± 1.90 μg/mL）。同时，乙醇和水提取物的抗疟活性较低，IC值分别为20.00 ± 1.57和30.95 μg/mL ± 1.27 μg/mL。所有提取物和青蒿素均表现出显著的抗疟活性（< 0.05）。所有提取物对卤虫均无毒（50%致死浓度，LC > 1000 ppm）。此外，与导致100%溶血的Triton X-100相比，用所有提取物处理正常红细胞时未观察到溶血现象（< 5%）（< 0.05）。丙酮和甲醇提取物对正常细胞系无毒，且与青蒿素相比具有统计学显著性（< 0.05）。
结合令人满意的选择性指数（SI）值，没食子的丙酮和甲醇提取物可作为有前景的安全抗疟替代药物。
