Kava is a beverage prepared from the rhizomes and roots of the tropical evergreen plant Piper methysticum. Kava contains six major kavalactones. Legacy studies found that kavalactones did not inhibit human CYPs in vitro at relevant concentrations, and kava did not inhibit the major CYPs in humans in vivo and was devoid of clinically significant drug interactions. Nevertheless, CYP2B6 was never evaluated. Recent investigation identified that (+)-dihydromethysticin, one of the six natural kavalactones, was an inhibitor of CYP2B6 in vitro. This investigation evaluated kava extract and (+)-dihydromethysticin effects on expressed CYP2B6 activity- both wild-type CYP2B6.1 and the active allelic variant CYP2B6.4. Effects on human liver microsomal CYP2B6 were also evaluated. Two independent kava extracts inhibited expressed and human liver microsomal CYP2B6 activity, in a concentration-dependent manner, assessed using the CYP2B6 probe substrates 7-ethoxy-4-trifluoromethyIcoumarin O-deethylation and S-ketamine N-demethylation. Ki values for CYP2B6 inhibition by (+)-dihydromethysticin alone and in kava extracts were 0.01-0.05 μM. Kava and (+)-dihydromethysticin interaction with expressed CYP2B6.1 and CYP2B6.4 generated a difference spectrum consistent with formation of a metabolite-inhibitor complex. (+)-Dihydromethysticin underwent NADPH-dependent metabolism by expressed CYP2B6 and human liver microsomes. These results show that kava extracts inhibit CYP2B6, an effect attributed to (+)-dihydromethysticin, which appears to act as a mechanism-based inhibitor. Because kava consumption achieves plasma (+)-dihydromethysticin concentrations exceeding the inhibitory Ki, there is a potential risk of in vivo CYP2B6-mediated herb-drug interactions. Such potential merits clinical drug-herb interaction studies using standard CYP2B6 substrate probes.
Phytochemical investigation of the stem bark of Massularia acuminata (Rubiaceae) led to the isolation of 20 triterpenoid saponins, including ten previously undescribed, designated as massularosides E-N (1-10). The compounds were purified from the methanolic extract by successive chromatographic techniques, including column chromatography, Sephadex LH-20 gel filtration, and preparative HPLC. Structure elucidation was achieved based on comprehensive spectroscopic and mass spectrometric analyses (1D and 2D NMR and HRESIMS). Additionally, the absolute configurations of sugar moieties were determined by HPLC-QTOF-MS analysis of their respective chiral derivatives. Among previously undescribed saponins, nine were characterized as bidesmosidic and one as a monodesmosidic triterpenoid glycosides, possessing either oleanolic acid or hederagenin aglycone backbone, except for massularoside N (10), which contained a nor-oleanolic acid aglycone. Notably, massularosides E-G featured a distinctive 2-acetamido-2-deoxyglucose unit, while massularoside N possessed a rare sulfoquinovose moiety attached to the C-3 of the aglycon. Other undescribed compounds (massularosides H-M) contained either a glucopyranosyl or a glucuronopyranosyl residue linked to the aglycone at C-3. This study broadens the chemical diversity of M. acuminata and provides deeper insight into the structural variability and potential chemotaxonomic relevance of molecules within the genus. Biological screening revealed that the methanolic extract of M. acuminata bark significantly enhanced LXR (liver X receptor) transcriptional activity, producing a 4.77-fold increase. Among the isolated saponins, multiple compounds exhibited LXR activation, with massularoside G (3) being the most promising, with a 4.51-fold increase in LXR activity.
The genus Oncosiphon (Asteraceae), consisting of aromatic herbs, is indigenous to southern Africa. Oncosiphon species have been documented in Khoi-San ethnobotany as herbal remedies for typhoid fever, pneumonia, and as diuretics. Research on the biological properties and comprehensive phytochemical profiling of these important Oncosiphon species is currently limited. This study was therefore undertaken to address the knowledge void in chemical profiling, through the application of various analytical techniques to analyse the volatile and non-volatile constituents of three South African Oncosiphon species. The aerial parts of Oncosiphon suffruticosus (n = 28), O. grandiflorus (n = 16), and O. africanus (n = 4) were collected from various locations in the Western Cape Province of South Africa. The stems and leaves (SL) were separated from the flowers (F) and analysed as distinct samples. The methanol: chloroform (1:1, v/v) extracts were prepared and analysed using ultra–high–performance liquid chromatography quadrupole time-of-flight time–of–flight mass spectrometry (UHPLC–QToF–MS) and a semi–automated high–performance thin–layer chromatography (HPTLC) system. Multivariate data analysis was performed on the UHPLC–QToF–MS data to determine interspecies chemical variation. Two-dimensional (2D) gas chromatography (GCxGC–ToF–MS) was used to determine the headspace volatile profiles of the intact aerial parts. The results show that the non-volatile profiles of the Oncosiphon species are characterised by amino acids, phenolic acids, flavonoids, sesquiterpene lactones, and fatty acid derivatives. The HPTLC profiles of O. grandiflorus and O. africanus are chemically more closely related, and O. suffruticosus has a distinct profile, which is supported by the chemometrics results of the flowers. The major headspace volatile compounds in Oncosiphon flowers are α-pinene, α-ocimene, eucalyptol, o-cymene, and artemisia alcohol, whereas the stems and leaves mainly consist of α-ocimene, eucalyptol, and yomogi alcohol.
Eryngium heterophyllum (toad grass) is native to Mexico and has been used traditionally to manage diabetes, hypercholesterolemia, and arthritis. However, its bioactive compounds remain poorly characterized. This study profiled the phytochemical composition of the methanolic extract of E. heterophyllum and explored potential bioactive pathways associated with metabolic syndrome (MetS). Nontargeted Ultra-High-Performance Liquid Chromatography-Quadrupole Time-of-Flight Mass Spectrometry analysis identified 85 metabolites across seven chemical classes, including flavonoids, phenylpropionic acids, and coumarins. 31 compounds were further analyzed using STITCH, SwissTargetPrediction, and DAVID to construct compound-disease-predicted target networks relevant to MetS-associated inflammatory conditions. This analysis identified 822 compound-target associations and highlighted key disease regulators including AKR1B1, PTGS2, ACE, and PPARA/PPARG. Flavonoids and phenylpropionic acids showed the highest network connectivity. Our findings indicate that E. heterophyllum interacts with pathways associated with inflammation, oxidative stress, insulin signaling, and lipid metabolism. These data offer a comprehensive phytochemical profile and elucidate the plant's biological significance, laying the groundwork for functional validation.
To date, the phytochemical composition of the aerial parts of Nanophyton iliense U.P. Pratov has not been comprehensively investigated. In the present study, qualitative metabolite profiling of the methanolic extract of the aerial parts was performed using liquid chromatography coupled with diode-array detection and quadrupole time-of-flight mass spectrometry (LC-DAD-QToF-MS) operating in both positive and negative electrospray ionization modes. A total of 81 metabolites were tentatively identified based on accurate mass measurements, MS/MS fragmentation patterns obtained in all-ion MS/MS mode, and comparison with previously reported literature data. The detected compounds included hydroxycinnamic acid amides, phenolic acids, flavonoids (including glycosides), amino acids, organic acids, sulfated derivatives, and nucleosides. Among them, the flavonoid narcissin (isorhamnetin-3-O-rutinoside) was isolated from the extract, and its structure was confirmed by 1H and 13C NMR spectroscopy supported by COSY, HSQC, and HMBC experiments. Additionally, a compound with the molecular formula C17H14O5 was detected; however, its structure could not be conclusively established based on the available spectroscopic data and is therefore reported as an unidentified metabolite. The present study provides the first systematic qualitative characterization of the metabolite profile of N. iliense and establishes a foundation for future quantitative and bioactivity-oriented investigations of this species.
Castanopsis sieboldii is a phenolic-rich evergreen species in the family Fagaceae, yet comprehensive quantitative and tissue-specific metabolite profiling remains limited. In this study, an integrated analytical workflow comprising UHPLC-PDA quantification, LC-QToF-MS identification, and chemometric analysis was developed to characterize phenolic constituents in leaves, flowers, fruits, and stems. A validated UHPLC-PDA method enabled the simultaneous quantification of six major phenolics, with limits of detection ranging from 0.01 to 0.05 μg/mL and limits of quantification from 0.025 to 0.1 μg/mL. Among all tissues, 3‑O‑galloylshikimic acid (Compound 1) was the predominant metabolite (0.1-204 mg/g), followed by caffeoylquinic acids (Compounds 2-3), ellagic acid (Compound 4), and flavonoid glycosides (Compounds 5-6). LC-QToF-MS analysis facilitated the tentative annotation of 185 metabolites, including phenolic acids, ellagitannins, galloylshikimic acids, and flavonoid glycosides, based on accurate mass measurements and characteristic MS/MS fragmentation patterns. Chemometric evaluation using principal component analysis (PCA), partial least squares discriminant analysis (PLS-DA), and hierarchical clustering analysis (HCA) revealed clear tissue-specific clustering, with leaves exhibiting the highest chemical diversity and phenolic abundance, whereas fruits showed minimal levels. PCA captured 80% of total variance in the first two components, and the PLS-DA model showed strong predictive performance (R²Y ≈ 1.00; Q² ≈ 0.98) although interpretation should consider the limited sample size. This study provides a comprehensive, tissue-resolved phenolic profile of C. sieboldii, establishing a robust chemical foundation for future pharmacological, ecological, and quality-control applications.
CONTEXT:Curcumin-containing dietary supplements are widely marketed with claims of enhanced bioavailability, despite well-recognized limitations related to poor aqueous solubility, chemical instability, and extensive first-pass metabolism. Comparisons among commercially available products using physiologically relevant performance metrics remain limited. OBJECTIVE:To systematically evaluate disintegration, dissolution, and bioaccessibility of curcuminoids and (S)-ar-turmerone from a cross section of commercially available turmeric dietary supplements under fasted- and fed-state biorelevant conditions. MATERIALS AND METHODS:Eight marketed turmeric supplements representing diverse formulation strategies were assessed for disintegration and dissolution using USP-aligned methods in fasted- and fed-state simulated gastric and intestinal media (FaSSGF, FaSSIF, FeSSGF, FeSSIF). Bioaccessible concentrations, quantities, and dose fractions of curcuminoids and (S)-ar-turmerone were quantified after 3 h. RESULTS:All products exhibited poor dissolution overall, with no formulation achieving greater than 40% total release. Dissolution was lowest under fasted-state conditions and improved modestly in fed-state gastric media, reflecting the influence of lipid content. Products with higher curcuminoid loads per capsule generated greater absolute bioaccessible concentrations despite poor release efficiency, whereas a phytosome formulation achieved superior release despite a lower dose. Several products marketed as "enhanced" formulations demonstrated poor disintegration and low bioaccessibility. DISCUSSION:These findings indicate that bioaccessible concentration is governed jointly by dosage-form performance and curcuminoid dose loading, and that plasma exposure metrics dominated by conjugated metabolites may not reliably reflect formulation performance. CONCLUSION:Commercial turmeric supplements exhibit substantial limitations in biorelevant disintegration and dissolution. Superior in vitro release is a prerequisite - but not a guarantee - for enhanced systemic exposure, underscoring the need for cautious interpretation of bioavailability claims.
Elymus repens (L.) Gould has a long history of use in traditional medicine across the British Isles, particularly among Gaelic and Anglo-Saxon communities, where it has been employed as a diuretic and anti-inflammatory agent. Despite its ethnopharmacological significance, comprehensive insights into its phytochemical composition and biological activities remain limited. The present study aimed to provide an integrated characterization of E. repens through macro- and microscopic analyses, advanced phytochemical profiling, and evaluation of the biological activities of the rhizome part. Microscopic examination revealed distinct anatomical features differentiating rhizome and stem, leaf tissues, supporting accurate identification and pharmacognostic standardization. Chemical profiling using Liquid Chromatography-Quadrupole Time-of-Flight Mass Spectrometry (LC-QToF-MS) enabled the tentative identification of 93 metabolites, including amino acids, in aerial and rhizome extracts. These compounds were primarily classified into polyamines (e.g., feruloylputrescine, hydroxycoumaroylagmatine), phenolic acids (gallic, vanillic, and ferulic acids), flavonoids (apigenin, tricin, saponarin analogues), amino acids (arginine, tyrosine, tryptophan), organic acids (malic, succinic acids), nucleosides (adenosine, thymidine), and phospholipids. Biological evaluation demonstrated that the hydroethanolic rhizome extract exhibited notable antifungal activity against Aspergillus fumigatus (IC50 = 34.9 µg/mL). Additionally, hydroethanolic extracts of both the aerial and rhizome parts showed no cytotoxicity in the Artemia salina lethality assay at concentrations up to 10 mg/mL, indicating a favorable preliminary safety profile. Of particular interest is tricin, which possesses anti-inflammatory, antioxidant, antimicrobial, and potential nephroprotective therapeutic effects; its mechanism of action is associated with the suppression of oxidative stress, the inhibition of pro-inflammatory mediators, and the disruption of metabolic processes in microbial cells. Overall, this study provides a comprehensive phytochemical and pharmacognostic characterization of E. repens, highlighting its potential as a source of bioactive compounds. The metabolite profile obtained directly from the biologically active extract, combined with its proven antifungal activity, serves as direct confirmation of the antimicrobial aspect of this plant’s traditional use, while its broader applications in ethnomedicine require targeted pharmacological testing. These findings contribute valuable data for chemotaxonomic classification and future pharmacological investigations.
Medicinal and aromatic plants are vital to the global herbal trade, with Panax species (ginseng) being highly valued for their health-promoting benefits. Ensuring the quality and safety of the plant raw material is essential; however, intentional or unintentional adulteration with morphologically similar species often comprises product authenticity, which is common in herbal products. Comparative morphoanatomy together with high-performance liquid chromatography coupled with ultraviolet detection (HPLC-UV) analyses were conducted on four Panax species (P. ginseng, P. quinquefolius, P. japonicus, and P. notoginseng) and two common adulterants (Codonopsis pilosula and Platycodon grandiflorus). Microscopic examination of intact roots, rhizomes, and their powders revealed critical diagnostic traits. The presence of secretory ducts and abundant starch grains were consistent in Panax species, but absent or scarce in adulterants. While xylem architecture effectively differentiated most species, the high anatomical similarity between P. ginseng and P. quinquefolius remained a challenge. The morphology of starch grains and xylem vessels also served as diagnostic features to differentiate the ginseng species from both adulterants. HPLC-UV profiles corroborated these findings, identifying eight major ginsenosides in Panax samples, while adulterants were entirely devoid of these compounds. These results confirm that anatomical analysis provides robust, practical criteria for the authentication of ginseng. Integrating microscopic techniques with chemical profiling offers a reliable, complementary approach to detecting adulteration, including economically motivated bulking, thereby ensuring the botanical integrity and safety of herbal products.
Bulbine Wolf (Asphodelaceae) comprises over 80 species, with five holding significant medicinal value in South Africa for treating skin and gastrointestinal ailments. While roots are traditionally prioritised, the chemical profiles of leaves and rhizomes remain underexplored although they are also medicinally important. This study used chromatographic and mass spectrometry-based analytical techniques (HPTLC, LC-QToF-MS, and UPLC-MS) combined with chemometric analysis to chemically profile the metabolites of five Bulbine species from the Eastern Cape. Chemical profiling tentatively identified 73 compounds, including flavonoids, phenolic acids, and anthraquinones. Phenylanthraquinones, specifically knipholone and knipholone 6 '-methyl ether, were ubiquitous across all taxa. Species-specific markers were identified, such as bulbine-knipholone in B. abyssinica, gaboroquinones in B. frutescens, and bulbnatalonosides in B. latifolia. Chemometric modelling revealed that while rhizome chemistry is relatively conserved, root profiles provide the most robust inter-species differentiation. Bulbine frutescens and B. latifolia displayed the highest chemical diversity, whereas B. asphodeloides was notably rich in anthocyanins. The significant overlap in bioactive constituents between leaves, roots and rhizomes suggests that aerial parts could serve as viable substitutes in traditional remedies. These findings establish a chemical basis for species authentication and support sustainable harvesting practices by reducing the destructive exploitation of rhizomes and roots.
The thermodynamic activity of an active pharmaceutical ingredient (API) is a key driver of permeation performance in topical formulations. This study investigated how solvent composition and evaporation impact the degree of saturation (DS) and skin permeation of three representative APIs: diclofenac sodium, metronidazole, and lidocaine. Model hydroxyethyl cellulose gels containing 1%, 10%, or 20% w/w Polyethylene Glycol (PEG-200) were prepared and characterized for solubility, pH, viscosity, and drying behavior. The solubility of all APIs increased with increasing PEG-200 concentration, whereas the DS varied correspondingly at a given drug load. Polystyrene substrate drying studies demonstrated that higher PEG-200 levels slowed solvent loss. The in situ drying studies on human cadaver skin using Franz cells enabled dynamic tracking of PEG-200 content and API saturation. Diclofenac sodium and lidocaine gels formulated with 1% PEG-200 showed progressively increasing DS over time and correspondingly higher permeation fluxes in in vitro permeation studies. In contrast, metronidazole gels showed little discrimination in DS and flux across PEG-200 concentrations, consistent with their hydrophilic nature and distinct solubility dynamics. The cumulative absorption confirmed a strong concordance between DS and permeation for diclofenac sodium and lidocaine, but not for metronidazole. Overall, the findings highlight that thermodynamic activity, modulated by solvent evaporation and shifts in solubility, governs the performance of topical formulations. These results underscore the value of monitoring DS profiles as predictive markers of drug delivery efficiency in topical product design.
The pharmacological potential of (+)‐dihydromethysticin [(+)‐DHM, 1 ] from kava kava, as a strong inhibitor of methadone metabolism, is currently constrained by the absence of a direct, scalable, and stereoselective synthesis. Isolation from natural sources is limited by low yields and difficult purification. The requirement for the nonnatural enantiomer, (−)‐DHM, to investigate biological activity necessitates a robust synthetic approach. To overcome this, we report an efficient, enantioselective total synthesis of both DHM enantiomers. Our strategy uses an Evans syn ‐aldol reaction as the pivotal chirality‐inducing step, enabling the stereospecific installation of the C‐6 absolute configuration within the α‐pyrone core via readily available chiral oxazolidinone antipodes. Subsequent transformations of aldol adducts provided access to the target DHM enantiomers in 9 steps, with >25% overall yield and >95% ee, starting from thiomethylacetyloxazolidinone. Induced‐fit docking studies using the hCYP2B6 crystal structure suggest that both enantiomers of DHM adopt similar binding orientations within the CYP2B6 active site, independent of stereochemistry. In this orientation, the methylenedioxy group is directed toward the heme center and interacts with Thr302, potentially producing a reactive carbene that inhibits CYP2B6 catalytic activity. These computational data are consistent with previously reported in vitro findings and provide insights into DHM–CYP2B6 interactions at the molecular level.
7-Hydroxymitragynine (7-OH), a minor alkaloid in kratom (Mitragyna speciosa (Korth.) Havil.) (Rubiaceae) and an active metabolite of mitragynine, is a critical transient precursor to mitragynine pseudoindoxyl, which exhibits >2-fold μ-opioid receptor-biased agonism and improved isoform selectivity relative to its precursors. Although present only in trace amounts in kratom leaves, a recent survey identified hundreds of consumer products with semisynthetic 7-OH and mitragynine pseudoindoxyl. Their high potency, ease of access, and risk of addiction have prompted the US FDA to recommend scheduling 7-OH as a Schedule I controlled substance. To address this public health crisis and the associated analytical challenges, a comprehensive analysis of commercially available kratom products was performed. The results revealed substantial inconsistencies between the quantities claimed on the products' labels and the actual 7-OH amount detected in several of these products. Along with 7-OH and mitragynine pseudoindoxyl, several (over)oxidized byproducts were detected, providing crucial insights into their synthetic origins. Analysis of >98% of 7-OH-labeled products indicated a semisynthetic origin, with labeled doses ranging from 0.001 to 33.6 mg per serving. Furthermore, consistent with the prior report, 7-OH degrades into the potentially toxic byproduct 3-dehydromitragynine under simulated gastric conditions. These findings underscore significant safety concerns over oral 7-OH products and necessitate validated analytical monitoring to guide regulatory oversight and consumer protection.
Entada elephantina (Burch.) S.A. O'Donnell & G.P. Lewis (formerly Elephantorrhiza elephantina (Burch.) Skeels), a member of the Fabaceae, is an ethnomedicinal plant widely used in South Africa. Despite studies supporting its traditional applications, comprehensive phytochemical characterisation remains limited. In this study, chemical profiling and marker quantification were performed on methanolic root extracts of E. elephantina (n = 50) collected from the Northern Cape Province, South Africa. High-performance thin-layer chromatography coupled to mass spectrometry (HPTLC-MS) and LC-MS analyses confirmed the presence of catechin, epicatechin gallate (ECG), epigallocatechin gallate (EGCG), quercetin 3'-glucoside, and gallic acid across all samples. Ultra-high performance liquid chromatography-diode array detector-quadrupole time-of-flight mass spectrometry (UHPLC-DAD-QToF-MS) enabled the tentative identification of 93 metabolites, predominantly flavonoids and their acylated derivatives, alongside minor phenolic and organic acids. Detected flavonoids included (epi)catechin aglycone derivatives, galloylated flavonoids such as taxifolin galloylated hexoside, and dimeric and trimeric ECG derivatives. Quantification using a validated UPLC-PDA method demonstrated notable variation in quercetin 3'-glucoside (1.23-2.54 mg/kg), catechin (0.42-0.88 mg/kg), ECG (0.39-0.74 mg/kg), kaempferol (0.008-0.018 mg/kg), and EGCG (0.004-0.014 mg/kg). Molecular networking revealed two principal structural subclusters, reflecting spectral similarity and shared fragmentation patterns within flavonoid families. This comprehensive chromatography-based approach establishes a phytochemical reference framework to support quality control, standardisation, and potential commercial development of this medicinal species.
Elderberry (Sambucus nigra) has received considerable attention for its health-promoting properties, particularly during the COVID-19 pandemic, when its products became one of the top-selling herbal supplements in the United States. While the anthocyanin profile of elderberry is well characterised, comprehensive studies of its non-anthocyanin constituents are underexplored. An in-depth phytochemical investigation of dried elderberry fruits, focusing on non-anthocyanin constituents, led to the discovery of a novel iridoid glycoside named elderberoside (1). Additionally, ten known metabolites were isolated, including an iridoid (2), an alkaloid (3), and eight flavonoids (4-11). Structural elucidation of these compounds was achieved through detailed one-dimensional (1D) and two-dimensional (2D) nuclear magnetic resonance (NMR) spectroscopy and confirmed by mass spectrometry.
Amorphophallus titanum (Becc.) Becc., commonly known as titan arum, corpse flower or carrion flower, is famous for having the largest inflorescence in the world. In addition to mimicking rotting meat with its flesh-colored floral parts and thermogenesis features, the bloom produces a variety of odorous chemical compounds that give the inflorescence its characteristic rotting animal smell when blooming, in order to attract a specific group of pollinators. This study analyses the volatile chemical profiles of the odors emitted during various stages of blooming. The floral odor samples were collected at different times of the bloom using HS-SPME fibers, and the samples were analyzed by GC/Q-ToF. A total of 66 volatile compounds were identified in the bloom, representing 31.62-96.92% of the volatile composition. Several malodorous compounds were detected, including trimethylamine, dimethyl disulfide, dimethyl trisulfide, dimethyl tetrasulfide, and indole. We also analyzed the nonvolatile phytochemical constituents of various floral and vegetative organs of the plant for the first time using LC/Q-ToF and identified 40 compounds, including flavonoids, anthocyanins, amino acids, xanthones, C-glycosylflavones, and organic acids in different organs of the plant. The main constituents of anthocyanins were cyanidin-3-O-glucoside and cyanidin-3-O-rutinoside. Leucine, isoleucine, phenylalanine, tryptophan, and methionine were the major amino acids found in the plant's organs. We observed that A. titanum emits distinct odor compounds from different parts of the inflorescence at various stages of blooming.
The psychedelic mushroom market has expanded rapidly due to changing regulations and increasing consumer demand. Product diversity now extends beyond traditional capsules and tablets to include gummies, powders, and confectionery items, complicating quality control efforts. To assess the quality and potential adulteration of Amanita musca-ria and Psilocybe cubensis-based products, a validated LC-QToF-MS method was developed. This method focused on five characteristic compounds: ibotenic acid (IBA), muscimol (MUS), muscarine, psilocin, and psilocybin that are constituents of A. muscaria and P. cubensis mushrooms. Method validation demonstrated satisfactory linearity, precision, and recovery of all five analytes. Psilocin and psilocybin levels ranged from 0.001-1.6% and 9.9-19.3%, respectively, in five Psilocybe species samples, while IBA, MUS, and muscarine levels in two samples of Amanita muscaria were 0.03-0.04%, 0.01- 0.02%, and 0.01-0.02%, respectively. By comparing commercial products to authentic samples, we evaluated the overall quality of 27 across various formulations. Our analysis included 14 gummies, three chocolates, six capsules, one tablet, and three powders. Although 11 of 14 gummies claimed to contain Amanita mushroom extracts, only MUS and muscarine were detected, without IBA. Interestingly, one gummy product indicated the presence of psilocin and psilocybin despite the labeling that claimed, "no psilocybin." Eleven products contained psilocin and psilocybin as anticipated, but five products lacked all target compounds. These findings underscore the need for standardized product specifications. Nevertheless, the established LC-QToF-MS approach could serve as a valuable tool for evaluating the quality of magic mushroom-based consumer products.
ETHNOPHARMACOLOGICAL RELEVANCE:Barbeya oleoides Schweinf. (Barbeyaceae) is traditionally employed to manage diverse ailments, including infections, fever, edema, and related inflammatory conditions. AIM OF THE STUDY:This study aimed to investigate the wound-healing potential of the total methanolic extract (BO-TM) from the aerial parts of B. oleoides, as well as its defatted and mother liquor fractions (BO-ML). In addition, chemical profiling of identified bioactive constituents underpinning the observed therapeutic activity. METHODS:LC-DAD-QToF analysis was performed for BO-TM phytochemical profiling. BO-TM was prepared and subsequently defatted to yield methylene chloride (BO-MC) and mother liquor (BO-ML) fractions. In vitro wound healing effects on human skin fibroblast (HSF) migration were assessed using a scratch assay, with effective doses selected based on prior MTT cytotoxicity assay results. For in vivo evaluation, male Wistar albino rats were divided into 7 groups: Normal, positive control without treatment, reference (Mebo®), and treatment groups receiving BO-TM and BO-ML (2.5 &5 % in Vaseline base, topically) once daily for 10 days. Histopathological examination and biochemical markers analyses (MIP-2, collagen, MDA, GSH, and FOXO1) were performed to elucidate underlying mechanisms related to inflammation, oxidative stress, and tissue remodeling. RESULTS:Chemical profiling annotated 69 metabolites, comprising 20 flavonoids, 42 gallotannins and phenolic acid derivatives, and 5 triterpenoids. BO-TM (5 %) enhanced wound closure to 96 % versus 84 % in the untreated group. In vivo, treatment with BO-TM and BO-ML has achieved a significant increase in GSH, FOXO1, collagen, and MIP-2 levels while showing a significant decrease in MDA level compared to the positive control and Mebo® groups. CONCLUSION:The methanolic extract and its fraction of B. oleoides exhibited significant-wound-healing potential in in vitro and in vivo models, likely through antioxidant, anti-inflammatory, and pro-regenerative mechanisms mediated by its rich polyphenolic and triterpenoid content. These findings provide scientific support for its traditional use and highlight its therapeutic potential as a natural wound-healing agent by Yemeni and Eritrean healers. However, further preclinical and clinical investigations are warranted to comprehensively evaluate its safety, efficacy, and translational potential in human applications.
Echinacea products are among the most widely used herbal supplements in the United States, primarily valued for their purported alleviation of common cold symptoms. Herein, we report the isolation and characterization of eight alkamides including two new ones (1 and 2) from the roots of two Echinacea species: E. purpurea (1, 3, and 4) and E. angustifolia (2, and 5‒8). This study provides the first comprehensive 13C nuclear magnetic resonance assignments of all isolated alkamides. The absolute configuration of 1 was established using Diastereomeric Parameter 4 plus probability analysis and specific rotation. The anti-inflammatory activity of the purified compounds and extracts was evaluated by measuring the inhibition of inducible nitric oxide synthase in lipopolysaccharide-stimulated mouse macrophages (RAW264.7), alongside cytotoxicity assessments. The purified alkamides and the crude extracts exhibited modest anti-inflammatory effects. The current study provides an understanding of the chemical composition of Echinacea and identifies potential markers for distinguishing E. purpurea from E. angustifolia.
Turnera diffusa Willd. ex Schult. leaf has been used in traditional medicine as an aphrodisiac, tonic, and in the management of diabetes. Based on the traditional use and recent evidence of antidiabetic activity, we investigated the effects of a 95% ethanolic extract of T. diffusa leaf (TDE) on a series of ligand-activated transcription factors, namely PPARα, PPARγ, LXR and NRF2, which are involved in the regulation of metabolic pathways associated with obesity, diabetes and inflammation. Further, the effects of TDE on α-glucosidase enzyme, lipid accumulation in adipocytes (adipogenesis) and glucose uptake in myocytes were also evaluated. Phytochemical analysis of TDE was performed by mass spectrometry. TDE (50 μg/mL) demonstrated a strong agonistic effect on LXR (2.7-fold) and NRF2 (21.6-fold), while the activation of PPARα, and PPARγ was in the range of 1.4-1.8-folds under similar experimental conditions. At a concentration of 100 μg/mL TDE decreased lipid accumulation in adipocytes by 55.3% and increased glucose uptake in muscle cells by 91.3%. The adipogenic effect induced by a full PPARγ agonist (rosiglitazone) was antagonized by TDE showing a decrease of 57.6% in lipid accumulation. This is the first report to reveal the agonistic action of TDE on multiple nuclear receptors along with its glucose uptake enhancing and antiadipogenic effects. The results indicate the potential utility of TDE in alleviating the symptoms of metabolic syndrome and in preventing the undesired adipogenic effects of antidiabetic drugs of the glitazone class. Phytochemical analysis of TDE indicated the presence of flavonoids as major constituents. Further studies in animal models of type II diabetes and obesity are warranted to explore its utility as an anti-diabetic and anti-obesity supplement.