Artemisinin is highly soluble in polyethylene Glycol 4000 and such solution has multiple biological effects

Yu Bao; Zhi Li; Si-Hao Chen; Li-Zhi Gao; Zu-Lan Liu; Lan Cheng; Yan Peng; Xiao-Ling Tong; Fang-Yin Dai

doi:10.18388/abp.2020_5190

Yu Bao 1State Key Laboratory of Silkworm Genome Biology, Southwest University, Chongqing, China; 2Chongqing Engineering Research Center of Biomaterial Fiber and Modern Textile, College of Textile and Garment, Southwest University, Chongqing, China
Zhi Li 1State Key Laboratory of Silkworm Genome Biology, Southwest University, Chongqing, China; 2Chongqing Engineering Research Center of Biomaterial Fiber and Modern Textile, College of Textile and Garment, Southwest University, Chongqing, China https://orcid.org/0000-0002-1852-6866
Si-Hao Chen 1State Key Laboratory of Silkworm Genome Biology, Southwest University, Chongqing, China; 2Chongqing Engineering Research Center of Biomaterial Fiber and Modern Textile, College of Textile and Garment, Southwest University, Chongqing, China
Li-Zhi Gao 1State Key Laboratory of Silkworm Genome Biology, Southwest University, Chongqing, China; 2Chongqing Engineering Research Center of Biomaterial Fiber and Modern Textile, College of Textile and Garment, Southwest University, Chongqing, China
Zu-Lan Liu 1State Key Laboratory of Silkworm Genome Biology, Southwest University, Chongqing, China; 2Chongqing Engineering Research Center of Biomaterial Fiber and Modern Textile, College of Textile and Garment, Southwest University, Chongqing, China
Lan Cheng 1State Key Laboratory of Silkworm Genome Biology, Southwest University, Chongqing, China; 2Chongqing Engineering Research Center of Biomaterial Fiber and Modern Textile, College of Textile and Garment, Southwest University, Chongqing, China; 3Key Laboratory of Sericultural Biology and Genetic Breeding, Ministry of Agriculture, College of Biotechnology, Southwest University, Chongqing, China
Yan Peng 1State Key Laboratory of Silkworm Genome Biology, Southwest University, Chongqing, China; 2Chongqing Engineering Research Center of Biomaterial Fiber and Modern Textile, College of Textile and Garment, Southwest University, Chongqing, China
Xiao-Ling Tong 1State Key Laboratory of Silkworm Genome Biology, Southwest University, Chongqing, China; 2Key Laboratory of Sericultural Biology and Genetic Breeding, Ministry of Agriculture, College of Biotechnology, Southwest University, Chongqing, Chin
Fang-Yin Dai 1State Key Laboratory of Silkworm Genome Biology, Southwest University, Chongqing, China; 2Chongqing Engineering Research Center of Biomaterial Fiber and Modern Textile, College of Textile and Garment, Southwest University, Chongqing, China; 3Key Laboratory of Sericultural Biology and Genetic Breeding, Ministry of Agriculture, College of Biotechnology, Southwest University, Chongqing, China https://orcid.org/0000-0002-0215-2177

DOI: https://doi.org/10.18388/abp.2020_5190

Abstract

Artemisinin has a significant role in treatment of malaria, as well as effective anti-inflammatory and anti-cancer activities. However, such problems as poor water solubility and easy recrystallization limit its application. In this study, polyethylene glycol, a solvent which is widely used in pharmaceutics, was introduced to prepare an artemisinin dissolution. Under the action of hydrogen bonding in 12% polyethylene glycol 4000 solvent, the maximum solubility of artemisinin could reach up to 1 mg/mL. Meanwhile, biological functions of such artemisinin solution were evaluated. The obtained artemisinin solution had a significant inhibitory effect on Gram-positive bacteria, Gram-negative bacteria and fungi. As for the anti-inflammatory property, 0.031 mg/mL artemisinin solution had an obvious inhibitory effect on nitric oxide release in inflammatory cells, and the survival rate of cells was greater than 50%. Low concentration of the obtained artemisinin solution (0.031 mg/mL) had no significant cytotoxicity, while it displayed selective inhibition in cancer cells. IC50 for human hepatoma cells BEL-7404, SMMC7721 and Hep G2 is 0.0016 mg/mL, 0.0084 mg/mL and 0.0541 mg/mL, respectively. In conclusion, the 12% PEG4000-assisted artemisinin solution has a good biological effect and it can be further applied in pharmaceutics, biomaterials and medicine.