Abstract
Sphaeralcea angustifolia has been widely used in inflammatory conditions such as blows, bruises, fractures, and wounds. The compounds identified as active in plants and suspension cell culture of S. angustifolia were tomentin, scopoletin, and sphaeralcic acid. To consolidate the integral use of knowledge about the S. angunstifolia and strengthen its pharmacological use in patients with knee osteoarthritis, the pharmacokinetic behavior of the active compounds was characterized. The SaTSS (S. angustifoloia standardized in Tomentin, Scopoletin, and Sphaeralcic acid) anti-ostearthritic fraction was obtained from cell suspension. The analytical method of High-Performance Liquid Chromatography (HPLC) for tomentin, scopoletin, and sphaeralcic acid were validated determining the accuracy, precision linearity, sensibility, specificity, detection limits, and quantification time-range parameters, as well as extraction efficiency and stability of compounds. The pharmacokinetic assay was performed with ICR mice strain, in which the mice were administrated with a single oral or intravenous dose (400 mg/kg with 7.1 mg/kg of scopoletin and tomentin in mixture and 34.6 mg/kg of sphaeralcic acid) of the SaTSS standardized active fraction. The results of the validated analytical methods allowed establishing, in a validated manner, that a coumarin mixture and sphaeralcic acid present in the SaTES fraction were detected in plasma. According to the values of Akaike Information Criteria (AIC), Sum of Squares (SS), Schwarz Criteria (SC), and by the determination coefficient (R2), the compounds follow a two-compartment model.
Highlights
The results suggest that the tomentin, scopoletin, and sphaeralcic acid present in the SaTSS standardized fraction could be adequately analyzed due to sample stability in the storage processes to which the real samples from experimental animals would be subjected
The analytical method was implemented for scopoletin, tomentin, and sphaeralcic acid; to our knowledge, this is the first report of a validated method for tomentin and sphaeralcic acid detection
A reliable analytical method was developed for anti-osteoarthritic compounds tomentin, scopoletin, and sphaeralcic acid, which was useful in their pharmacokinetic evaluation
Summary
The articular inflammation, regardless of its etiology, is associated with high direct and indirect costs, and represents the main cause of permanent disability in the right-holder population of the Instituto Mexicano del Seguro Social (IMSS, the institution with the largest coverage of health care in Mexico), which represents 11%. OA is a chronic degenerative disease with disabling consequences [2,4]. The treatment of OA is based on non-steroidal anti-inflammatories and glucocorticoids, as well as on biological and nonbiological drugs that modify the disease; prolonged use of these treatments has adverse side effects [5]. There is not a relevant treatment available, there is a need to find new drugs that have fewer side effects than those currently used; medicinal plants are a potential source to find new active compounds
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