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Artemisinin is highly soluble in polyethylene Glycol 4000 and such solution has multiple biological effects
Author(s) -
Fangyin Dai,
Yu Bao,
Zhi Li,
Sihao Chen,
LiZhi Gao,
Zu-Lan Liu,
Lan Cheng,
Peng Yan,
Xiaoling Tong
Publication year - 2020
Publication title -
acta biochimica polonica
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.452
H-Index - 78
eISSN - 1734-154X
pISSN - 0001-527X
DOI - 10.18388/abp.2020_5190
Subject(s) - artemisinin , polyethylene glycol , chemistry , pharmaceutics , nuclear chemistry , dissolution , solubility , aqueous solution , solvent , cytotoxicity , pharmacology , in vitro , biochemistry , organic chemistry , malaria , plasmodium falciparum , medicine , immunology
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.

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