Ferreira Ana M, Sales Isabela, Santos Sónia A O, Santos Tiago, Nogueira Fátima, Mattedi Silvana, Pinho Simão P, Coutinho João A P, Freire Mara G
CICECO - Aveiro Institute of Materials, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal.
Escola Politécnica, Universidade Federal da Bahia, Bahia 40210-630, Brazil.
Chem Bio Eng. 2024 Jan 4;1(1):44-52. doi: 10.1021/cbe.3c00005. eCollection 2024 Feb 22.
Artemisinin, a drug used to treat malaria, can be chemically synthesized or extracted from L. However, the extraction method for artemisinin from biomass needs to be more sustainable while maintaining or enhancing its bioactivity. This work investigates the use of aqueous solutions of salts and ionic liquids with hydrotropic properties as alternative solvents for artemisinin extraction from L. Among the investigated solvents, aqueous solutions of cholinium salicylate and sodium salicylate were found to be the most promising. To optimize the extraction process, a response surface method was further applied, in which the extraction time, hydrotrope concentration, and temperature were optimized. The optimized conditions resulted in extraction yields of up to 6.50 and 6.44 mg·g, obtained with aqueous solutions of sodium salicylate and cholinium salicylate, respectively. The extracts obtained were tested for their antimalarial activity, showing a higher efficacy against the strain compared with pure (synthetic) artemisinin or extracts obtained with conventional organic solvents. Characterization of the extracts revealed the presence of artemisinin together with other compounds, such as artemitin, chrysosplenol D, arteannuin B, and arteannuin J. These compounds act synergistically with artemisinin and enhance the antimalarial activity of the obtained extracts. Given the growing concern about artemisinin resistance, the results here obtained pave the way for the development of sustainable and biobased antimalarial drugs.
青蒿素是一种用于治疗疟疾的药物，可以通过化学合成或从黄花蒿中提取。然而，从生物质中提取青蒿素的方法需要更具可持续性，同时保持或提高其生物活性。这项工作研究了具有助溶性质的盐和离子液体水溶液作为从黄花蒿中提取青蒿素的替代溶剂的用途。在所研究的溶剂中，发现水杨酸胆碱和水杨酸钠的水溶液最有前景。为了优化提取过程，进一步应用了响应面法，其中对提取时间、助溶剂浓度和温度进行了优化。优化后的条件分别用水杨酸钠和水杨酸胆碱水溶液得到了高达6.50和6.44 mg·g的提取产率。对所获得的提取物进行了抗疟活性测试，结果表明，与纯（合成）青蒿素或用传统有机溶剂获得的提取物相比，其对疟原虫菌株具有更高的疗效。提取物的表征显示，除了青蒿素外，还存在其他化合物，如青蒿酮、金腰醇D、青蒿素B和青蒿素J。这些化合物与青蒿素协同作用，增强了所获得提取物的抗疟活性。鉴于对青蒿素耐药性的日益关注，这里获得的结果为开发可持续的生物基抗疟药物铺平了道路。
