Objectives To prepare a lyophilized saffron aqueous extract (SFE) and determine its chemical profile and serum and tissue pharmacokinetics after intravenous and oral administration to C57/Bl6J mice. Methods Lyophilized SFE was prepared, characterized using semi‐preparative HPLC and NMR analysis, and stability studies at room temperature, and was quantified for crocin content with an HPLC‐PDA method. After intravenous and oral administration of SFE (60 mg/kg, reconstituted with water for injection) to C57/Bl6J mice, crocetin (derived from in vivo crocin hydrolysis) serum and tissue levels (unconjugated and total) were measured with an HPLC‐PDA method and subjected to compartmental and non‐compartmental PK analysis. Key findings Saffron aqueous extract was rich in all‐trans‐crocin (27.8 ± 0.1% w/w) and stable for more than 15 months. One‐compartment PK model described crocetin's (unconjugated) kinetics after intravenous administration of SFE, while a first‐order kinetic parameter described the rate of crocetin biotransformation to crocetin metabolite (conjugated). Α οne‐compartment PK model with first‐order absorption described crocetin and crocetin's metabolite kinetics after SFE oral administration. Relative oral bioavailability was calculated at 1.17 for total crocetin. Tissue NCA PK analysis revealed extensive crocetin distribution to liver and kidneys. Conclusions SFE is a stable lyophilized extract rich in all‐trans‐crocin. The PK study allowed the estimation of basic PK parameters and the bioavailability of SFE’s main bioactive component, crocetin, after peros administration.
The volatile compositions of three closely related Hypericum species growing wild on the island of Crete were studied, all belonging to the section Coridium. Hydro-distillation in a modified Clevenger-type apparatus was performed according to the Hellenic Pharmacopoeia in order to obtain the essential oils, which were analyzed by GC-MS. Identification of the compounds was carried out by comparison of MS spectra and retention indices with literature data, as well as by co-chromatography with authentic samples. In total, 123 different compounds were identified and the main compounds were by order of their abundance as follows: H. empetrifolium: α-pinene, germacrene D, β-pinene, E-caryophyllene; H. amblycalyx: β-elemene, β-selinene, α-pinene, E-caryophyllene, α-selinene; H. jovis: trans-calamenene, α-selinene, β-elemene. The chemical results revealed the differences and similarities (qualitative and quantitative) between the studied oils, supporting the hypothesis that essential oils from Hypericum spp. do not serve as chemotaxonomic markers. Moreover, the essential oils were subjected to antimicrobial screening. According to the given results, the essential oils possessed better antifungal and anticandidal activities than antibacterial activities.
Hypericum genus, considered to comprise over 500 species that exhibit cosmopolitan distribution, has attracted human interest since ancient times. The present review aims to provide and summarize the recent literature (2012–2022) on the essential oils of the title genus. Research articles were collected from various scientific databases such as PubMed, ScienceDirect, Reaxys, and Google Scholar. Scientific reports related to the chemical composition, as well as the in vitro and in vivo pharmacological activities, are presented, also including a brief outlook of the potential relationship between traditional uses and Hypericum essential oils bioactivity.
Knowledge within the field of phytochemistry research has accelerated at a tremendous speed. The excess of literature reports featuring plants of high ethnopharmacological importance, in combination with our interest in the Asteraceae family and traditional medicine, led us to acknowledge the value of the Achillea L. genus. In a broad context, the various Achillea species are used around the globe for the prevention and treatment of different diseases, including gastrointestinal problems, haemorrhages, pneumonia, rheumatic pains, diuresis, inflammation, infections, and wounds, as well as menstrual and gynaecologic abnormalities. The present review aims to provide and summarize the recent literature (2011–2021) on the phytochemistry of the Achillea genus. In parallel, this study attempts to bridge the reports on the traditional uses with modern pharmacological data. Research articles that focused on secondary metabolites, traditional uses and pharmacological activities were collected from various scientific databases such as Pubmed, ScienceDirect, Reaxys and Google Scholar. This study revealed the presence of 141 phytochemicals, while 24 traditionally used Achillea spp. were discussed in comparison to current data with an experimental basis.
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