Centro de Biociências-Departamento de Bioquímica, Universidade Federal de Pernambuco, Avenida Prof. Moraes Rego, 1235, Cidade Universitária, Recife-PE 50.670-501, Brazil.
Laboratório de Imunopatologia Keizo Asami (LIKA), Universidade Federal de Pernambuco. Avenida Prof. Moraes Rego, 1235 Cidade Universitária, Recife-PE 50.670-501, Brazil.
Molecules. 2019 May 28;24(11):2042. doi: 10.3390/molecules24112042.
To obtain usnic acid potassium salt (PS-UA), the usnic acid (UA) was extracted and purified from the lichen , and modified to produce PS-UA. The structure was determined by H-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.
为了获得钾盐（PS-UA），从地衣中提取和纯化了地衣酸（UA），并对其进行了修饰以生成 PS-UA。通过 H-NMR、IR 和元素分析确定了结构，通过计算模型进行了验证，并确定了分子中 K 插入的位置。通过用 10 和 20 mg/kg 的 PS-UA 处理后，在乙酸和甲醛（I 期和 II 期）诱导的小鼠扭体中检测到抗伤害活性，表明对非炎症性和炎症性疼痛均有干扰。在 500、1000 和 2000 mg/kg 的口服剂量下，用低于 2000 mg/kg 的剂量治疗的小鼠没有死亡。除了体重增加外，用 1000 和 2000 mg/kg 处理时，食物和水的消耗减少，两种处理的分段白细胞数量增加。关于血清水平，胆固醇和甘油三酯降低，但两种处理均使肝转氨酶升高。在 2000 mg/kg 的治疗中检测到肝和肾的组织学变化，而脾保持不变。PS-UA 表现出抗伤害活性，而在 2000 mg/kg 的浓度下的急性毒性是唯一表现出肝和肾形态变化的剂量。
