Usnic Acid Potassium Salt: Evaluation of the Acute Toxicity and Antinociceptive Effect in Murine Model

• Main Authors: Hallysson Douglas A. Araújo, José G. Silva Júnior, João R. Saturnino Oliveira, Maria Helena M. L. Ribeiro, Mônica C. Barroso Martins, Marcos A. Cavalcanti Bezerra, André Lima Aires, Mônica C. P. Azevedo Albuquerque, Mário R. Melo-Júnior, Nicodemos T. Pontes Filho, Eugênia C. Pereira, Diego J. Raposo Silva, Janaína V. dos Anjos, Emerson Peter S. Falcão, Nicácio H. Silva, Vera L. Menezes Lima
• Format: Article
• Language: English
• Published: MDPI AG 2019-05-01
• Series: Molecules
• Subjects: lichen; <i>Cladonia substellata</i>; usnic acid derivatives; antinociceptive activity (phase I and II); toxicological survey; soluble drug; histopathology
• Online Access: https://www.mdpi.com/1420-3049/24/11/2042

To obtain usnic acid potassium salt (PS-UA), the usnic acid (UA) was extracted and purified from the lichen <i>Cladonia substellata</i>, and modified to produce PS-UA. The structure was determined by ¹H-NMR, IR and elemental analysis, ratified through computational models, as well as identification the site of K⁺ insertion in the molecule. Antinociceptive activity was detected through contortions in mice induced by acetic acid and formalin (phases I and II) after treatments with 10 and 20 mg/kg of PS-UA, indicating interference in both non-inflammatory and inflammatory pain. After oral administration at doses of 500, 1000 and 2000 mg/kg, no deaths of mice with treatments below 2000 mg/kg were observed. Except for body weight gain, food and water consumption decreased with treatments of 1000 and 2000 mg/kg, and the number of segmented leukocytes was higher for both treatments. Regarding serum levels, cholesterol and triglycerides decreased, however, there was an increase in hepatic transaminases with both treatments. Liver and kidney histological changes were detected in treatments of 2000 mg/kg, while the spleen was preserved. The PS-UA demonstrated antinociceptive activity while the acute toxicity at the concentration of 2000 mg/kg was the only dose that presented morphological changes in the liver and kidney.