Galenic preparations of German chamomile are used to treat mild skin diseases, inflammation, and spasms, and they have also been reported to have anxiolytic and sedative effects. The medicinal use of chamomile is well known in ethnomedicine. After obtaining its galenic preparations, there is lots of waste left, so it is expedient to develop waste-free technologies. The aims of this study were to gain knowledge of the ethnomedical status of chamomile in the past and present, develop methods for preparing essential oils and dry extracts from German chamomile flowers using complex processing, reveal the phytochemical composition of such extracts, and verify the analgesic and soporific activity of the extracts. Two methods for the complex processing of German chamomile flowers were developed, which allowed us to obtain the essential oil and dry extracts of the tincture and aqueous extracts as byproducts. A total of 22 phenolic compounds (7 hydroxycinnamic acids, 13 flavonoids, and 2 phenolic acids) were found in the dry extracts by using UPLC-MS/MS. In total, nine main terpenoids were identified in the chamomile oil, which is of the bisabolol chemotype. During the production of chamomile tincture, a raw material–extractant ratio of 1:14–1:16 and triple extraction are recommended for its highest yield. In in vivo studies with mice and rats, the extracts showed analgesic activity and improvements in sleep. The highest sedative and analgesic effects in rodents were found with the dry extract prepared by using a 70% aqueous ethanol solution for extraction at a dose of 50 mg/kg. The developed methods for the complex processing of German chamomile flowers are advisable for implementation into the pharmaceutical industry to reduce the volume of waste during the production of its essential oil and tincture, and to obtain new products.
German chamomile (Matricaria chamomilla L.) is an essential oil- containing medicinal plant used worldwide. The aim of this study was to gain knowledge of the phytochemical composition and the analgesic and soporific activity of Matricaria chamomilla L. (German chamomile) flower extract and its amino acid preparations, to predict the mechanisms of their effects by molecular docking and to develop aqueous printing gels and novel 3D-printed oral dosage forms for the flower extracts. In total, 22 polyphenolic compounds and 14 amino acids were identified and quantified in the M. chamomilla extracts. In vivo animal studies with rodents showed that the oral administration of such extracts revealed the potential for treating of sleep disorders and diseases accompanied by pain. Amino acids were found to potentiate these effects. Glycine enhanced the analgesic activity the most, while lysine and β-alanine improved the soporific activity. The molecular docking analysis revealed a high probability of γ-aminobutyric acid type A (GABAA) and N-methyl-D-aspartate (NMDA) receptor antagonism and 5-lipoxygenase (LOX-5) inhibition by the extracts. A polyethylene oxide (PEO)-based gel composition with the M. chamomilla extracts was proposed for preparing a novel 3D-printed dosage form for oral administration. These 3D-printed extract preparations can be used, for example, in dietary supplement applications.
The leaves and fruits of various Sorbus L. genotypes have long ethnopharmacological and food-usage histories, but inflorescences are still underutilized and neglected materials with scarce phytochemical scientific evidence. The aim of this study was to determine the phenolic profiles of inflorescence extracts of 26 Sorbus species, genotypes, and cultivars. HPLC and UPLS with MS detection were applied, and coupled data revealed unique phytochemical phenolic profiles. Neochlorogenic and chlorogenic acids were the key compounds, reaching up to 5.8 mg/g of dw. Rutin, isoquercitrin, quercetin 3-O-malonylglucoside, isorhamnetin 3-O-rutinoside, sexangularetin derivative, and kaempferol acetyl hexoside were detected in all Sorbus inflorescence samples. Overall, high quantitative heterogeneity across the various Sorbus genotypes was found by profiling. Phenolic fingerprint profiles and sexangularetin derivatives could serve as markers in authenticity studies and quality control schemes. The species S. amurensis, S. arranensis, S. commixta, and S. discolor and the cultivars ‘Chamsis Louing’, ‘Coral Beauty’, and ‘Edulis’ could be used as target genotypes for production of smart and innovative inflorescence matrix-based ingredients.
Background/Objectives: The Canadian goldenrod (Solidago canadensis L.) is one of the most widespread species of the genus Solidago from the Asteraceae family. It has a rich composition of biologically active compounds and is traditionally used to address kidney, urinary tract, and liver diseases. Previously, it was proven that the S. canadensis extract obtained with a 40% ethanol solution had the most promising anti-inflammatory and hepatoprotective activity. Therefore, this extract was selected for the further formulation of amino acid preparations and 3D-printed dosage forms. The aims of the present study were to investigate the chemical composition, toxicity, and antimicrobial, anti-inflammatory, and hepatoprotective activity of S. canadensis dry extract, its amino acid preparations, and 3D-printed dosage forms. Results: A total of 18 phenolic compounds and 14 amino acids were determined in the extracts. The S. canadensis herb extracts were verified to be practically non-toxic preparations (toxicity class V, LD₅₀ > 5000 mg/kg). They also showed moderate antimicrobial activity against Staphylococcus aureus, Enterococcus faecalis, and β-hemolytic Streptococcus pyogenes. The most pronounced hepatoprotective activity was observed with S. canadensis herb extract and its amino acid preparations with phenylalanine, alanine, and lysine at a dose of 25 mg/kg body weight. The most pronounced anti-inflammatory activity was found with S. canadensis herb extract and its preparation with arginine. According to the calculated docking score array and the analysis of binding modes in the active sites of COX-1 and COX-2, the flavonoid fraction and caffeic acid in the S. canadensis extracts presented moderate inhibitory activity. Conclusions: The development of innovative 3D-printed oral dosage forms represents a promising strategy to formulate dietary supplements or pharmaceutical preparations for these herbal extracts.
A pipeline for metabolomics, based on UPLC-ESI-MS, was tested on two malignant breast cancer cell lines of the sub-types ER(+), PR(+), and HER2(3+) (MCF-7 and BCC), and one non-malignant epithelial cancer cell line (MCF-10A). This allowed us to quantify 33 internal metabolites, 10 of which showed a concentration profile associated with malignancy. Whole-transcriptome RNA-seq was also carried out for the three mentioned cell lines. An integrated analysis of metabolomics and transcriptomics was carried out using a genome-scale metabolic model. Metabolomics revealed the depletion of several metabolites that have homocysteine as a precursor, which was consistent with the lower activity of the methionine cycle caused by lower expression of the AHCY gene in cancer cell lines. Increased intracellular serine pools in cancer cell lines appeared to result from the over-expression of PHGDH and PSPH, which are involved in intracellular serine biosynthesis. An increased concentration of pyroglutamic acid in malignant cells was linked to the overexpression of the gene CHAC1.
Pineapple weed (Matricaria discoidea DC.) is a widespread plant in Europe and North America. In ethnomedicine, it is well-known for its anti-inflammatory and spasmolytic activities. The aim of this research was to develop novel methods of M. discoidea processing to obtain essential oil and dry extracts and to investigate their phytochemical compositions. Moreover, the molecular docking of the main substances and the in vivo studies on their soporific and analgesic activities were conducted. The essential oil and two dry extracts from M. discoidea were prepared. A total of 16 phenolic compounds (seven flavonoids, seven hydroxycinnamic acids, and two phenolic acids) in the dry extracts were identified by means of UPLC-MS/MS. In the essential oil, nine main terpenoids were identified by gas chromatography (GC). It was shown that phenolic extraction from the herb was successful when using 70% ethanol in a triple extraction method and at a ratio of 1:14–1:16. The in vivo studies with rodents demonstrated the analgesic activity of the M. discoidea extracts and improvements in the sleep of animals. The dry extracts of M. discoidea did not show any toxicity. The molecular docking analysis showed a high probability of COX-1,2 inhibition and NMDA receptor antagonism by the extracts.