Current pharmacological therapies for the management of chronic articular diseases are far from being satisfactory, so new strategies need to be investigated. We tested the intra-articular pain relieving properties of a system of molecules from a characterized Centella asiatica extract (14G1862) in a rat model of osteoarthritis induced by monoiodoacetate (MIA). 14G1862 (0.2–2 mg mL−1) was intra-articularly (i.a.) injected 7 days after MIA, behavioural and histological evaluations were performed 14, 30 and 60 days after treatments. Moreover, the effect of 14G1862 on nitrate production and iNOS expression in RAW 264.7 macrophages stimulated with LPS was assessed. In vitro, 14G1862 treatment attenuated LPS-induced NO production and iNOS expression in a comparable manner to celecoxib. In vivo, 14G1862 significantly reduced mechanical allodynia and hyperalgesia, spontaneous pain and motor alterations starting on day 14 up to day 60. The efficacy was higher or comparable to that evoked by triamcinolone acetonide (100 μg i.a.) used as reference drug. Histological evaluation highlighted the improvement of several morphological parameters in MIA + 14G1862-treated animals with particularly benefic effects on joint space and fibrin deposition. In conclusion, i.a. treatment with Centella asiatica is a candidate to be a novel effective approach for osteoarthritis therapy.
Botanical extracts are standardized to 1 marker compounds (MCs). This standardization provides a certain level of quality control, but not complete quality assurance. Thus, industries are looking for other satisfactory systems to improve standardization. This study focuses on the standardization of herbal medicines by combining 2 parameters: the concentration of the MC and antioxidant capacity. Antioxidant capacity was determined with the oxygen radical absorbance capacity (ORAC) method and the concentrations of the MCs, by high-performance liquid chromatography. Total phenols were also determined by the Folin-Ciocolteau method. The ORAC values, expressed as mol Trolox equivalents/100 g (ORAC ), of 12 commercial herbal extracts were related to the ORAC values of the respective pure MCs at the concentrations at which the MCs occur in products (ORAC-MC ). The ORAC values of 11 extracts were higher than those of the respective MCs and the ratios ORAC-MC /ORAC ranged from 0.007 to 0.7, whereas in the case of Olea europaea leaves, the same ratio was 1.36. The ORAC parameters and their ratios, as well as the linear relationship between ORAC-MC and ORAC , are described and discussed as tools for improving the standardization of herbal products and detecting modifications due to herb processing and storage.
Suspect screening and untargeted analysis using UHPLC-qToF are two advanced analytical approaches now used to achieve an extensive chemical profile of samples, which are then typically confirmed through targeted analysis. These techniques can detect a large number of chemical features simultaneously and are currently being introduced into the study of contaminants of emerging concern (CECs) and into the study of the extent of human chemical exposure (the exposome). Here is described the use of these techniques to characterize chemical mixtures derived from the OECD 301F ready biodegradability test (RBT) of a chemical and natural formulation currently used to treat reflux disease and functional dyspepsia. Untargeted analysis clearly evidenced a different behavior between formulations containing only natural products with respect to that containing synthetic and non-naturally occurring substances. Suspect screening analysis improved the untargeted analysis of the omeprazole-based medicine, leading to the tentative identification of a number of omeprazole-derived transformation products, thereby enabling their preliminary quali-quantitative evaluation. Targeted analysis was then performed to confirm the preliminary data gained from the suspect screening approach. The validation of the analytical method for the quantitative determination of omeprazole and its major metabolite, omeprazole sulphide, has provided robust data to evaluate the behavior of omeprazole during the OECD 301F test. Using advanced analytical approaches, the RBT performed on the two products under investigation confirmed that omeprazole is not readily biodegradable, while the medical device made of natural substances has proven to be readily biodegradable.
22 November 2024 in Journal of Pharmaceutical and Biomedical Analysis
Artificial sweeteners (ASs) and dyes are widely used in foods, beverages and pharmaceutical and are recognized as emerging environmental contaminants due to their persistence and widespread occurrence. These substances often pass through the human body unchanged and resist wastewater treatment processes, leading to continuous introduction into aquatic environments and potential long-lasting term environmental effects. This study investigated, for the first time, the biodegradability of nine commercial dietary supplements, both natural and those containing ASs and synthetic dyes, using the Organisation for Economic Cooperation and Development (OECD) 301 F ready biodegradation test (RBT), which is a respirometry-manometric method. While the products showed good biodegradability, those containing ASs and dyes were further studied to determine their fate at the end of the RBT. The study involved developing and validating a chromatographic method to quantitatively determine the presence of Acesulfame K (1), Sucralose (2), Tartrazine (3) and Carmoisine (4) in the RBT mineral medium, using ultra-high performance liquid chromatography (UHPLC) coupled with two detectors: a high-resolution mass-spectrometer with quadrupole time-of-flight (qToF) and a UV-Vis diode array detector (DAD). Results indicated that these additives were not readily biodegraded, highlighting a potential significant environmental concern. This issue extends beyond dietary supplements to all Pharmaceutical and Personal Care Products (PPCP) including drugs and medical devices. The findings underscore the importance of raising cultural awareness about the environmental impact of persistent substances, encouraging the healthcare chain and patients to make informed choices. From a One Health perspective, reducing environmental contamination can lead to positive outcomes for human health.