Pharmacokinetic Study of Anti-osteoarthritic Compounds of a Standardized Fraction from Sphaeralcea Angustifolia

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.

The Journey of a Medicinal Plant throughout Science: Sphaeralcea angustifolia (Cav.) G. Don (Malvaceae)

“…The detection and time course of the compounds were followed in the plasma, urine, and feces of mice after a single oral dose (400 mg/kg) of the standardized fraction. The authors describe the extraction of the biomass and its chemical fractionation to obtain the standardized active fraction, HPLC analysis, and the extraction and stability of the active compounds based on the guidelines established by the FDA (Food and Drug Administration) for plasma samples [ 28 ]. The pharmacokinetic profile of the mixture of coumarins and sphaeralcic acid showed that these compounds were detected in mouse plasma, and no products of their biotransformation were registered.…”

“…It was determined that coumarins and sphaeralcic acid circulate to the white site and are subsequently detected in urine and feces. It was concluded that the mixture of scopoletin and tomentin are eliminated by the renal route and sphaeralcic acid by the enterohepatic route [ 28 , 29 ].…”

Potential role of nutraceuticals via targeting a Wnt/β‐catenin and NF‐κB pathway in treatment of osteoarthritis

“…It slows OA development by preventing chondrocytes from responding in a catabolic manner. Wnt/β‐catenin and ERK1/2–Runx2 pathways are activated when estrogen is present, inhibiting monocyte recruitment and bone formation (Serrano‐Román et al, 2021). Using oroxylin A, a flavonoid molecule produced from Oroxylum indicum , researchers could inhibit inflammation, prevent apoptosis, and fight tumors simultaneously.…”

Optimization, Characterization and Pharmacokinetic Study of Meso-Tetraphenylporphyrin Metal Complex-Loaded PLGA Nanoparticles

“…The volume of distribution (Vd), mean residence time (MRT), elimination half-life (t 1/2 ), and area under the plasma concentration-time curve from 0 h to infinity (AUC inf ) were determined after intravenous administration of MeP-loaded NPs to animals. All calculations were performed using the PKSolver add-in program for Microsoft Excel [114].…”