, popularly known as Rudraksha, is of immense holistic importance in traditional Indian culture with spiritual and medicinal benefits. The present study aims to characterize and explore the cytotoxic and tumor inhibitory..., popularly known as Rudraksha, is of immense holistic importance in traditional Indian culture with spiritual and medicinal benefits. The present study aims to characterize and explore the cytotoxic and tumor inhibitory potential of hydroalcoholic extract of Rudraksha beads in preclinical models. Hydroalcoholic extract was prepared from powdered Rudraksha beads and was characterized through qualitative and quantitative phytochemical analysis, FT-IR, and LC-MS/MS analysis. cytotoxic activity of Rudraksha bead extract was evaluated in PC3, U87MG, A549, HCT116, FaDu, MCF-7, and LLC1 cell lines by MTT assay. Apoptotic activity was assessed by Western blot analysis of Bax, Caspase-3, and Cleaved Caspase-3 proteins in the HCT116 cell line. antitumor efficacy was evaluated in the LLC1 allograft and HCT116 xenograft mouse model. Hydroalcoholic extract of Rudraksha bead showed abundance of polyphenolic compounds and their subtypes like phenols, flavonoids, and anthocyanins in different analytical techniques. Treatment with hydroalcoholic extract elicited a dose-dependent decrease in cell viability in all the tested cell lines, with the best response in HCT116 (CC50 = 47.22, 95% confidence interval (CI): 42.75 - 49.06 µg/mL), with upregulated expression of pro-apoptotic markers, Caspase-3 (1.53-fold), Cleaved Caspase-3 (1.47-fold), and Bax (6.4-fold). Treatment with 500 mg/kg of Rudraksha extract in the LLC1 tumor allograft model (QD × 9 days) and HCT116 xenograft model (QD × 21 days) demonstrated significantly reduced tumor volume in comparison to the vehicle control. Hydroalcoholic extract of Rudraksha demonstrated a promising tumor inhibition response in preclinical settings, therefore making it a potential therapeutic candidate for cancer treatment.
Infectious diseases caused by viruses, fungi, parasites, and bacteria continue to pose significant challenges to public health globally. In this context, the Ibero-American Program of Science and Technology for Developme...Infectious diseases caused by viruses, fungi, parasites, and bacteria continue to pose significant challenges to public health globally. In this context, the Ibero-American Program of Science and Technology for Development (CYTED) Network, "Potential Antimicrobial Agents Present in Plant Foods of Regional Interest" (REDALIM-MIC), aims to detect antimicrobial compounds in edible plants from Ibero-American countries and to promote collaborative research on their potential applications in health and nutrition. This report summarizes the main discussions and key outcomes of expert meetings conducted within the REDALIM-MIC Network, underscoring the importance of integrated and interdisciplinary research, with particular emphasis on the potential of edible plants as innovative and sustainable sources of bioactive compounds for the prevention and control of infectious diseases. Key outcomes included the identification of promising plant species and, the prioritization of bioactive extracts for further phytochemical characterization and pharmacological evaluation. The potential application of these findings in the development of functional foods and novel therapeutics, as well as the importance of strengthening regional collaboration, were also recognized. The REDALIM-MIC Network focuses on detecting antimicrobial compounds in edible plant species, evaluating their immunomodulatory properties, assessing their nutritional and health value, and fostering collaboration among Ibero-American institutions to support innovative, food-based approaches for preventing and managing infectious diseases. During the meetings, key topics such as regulatory frameworks, analytical techniques, quality control and methodologies and cell-based assays for the evaluation of their antimicrobial activity were discussed. In addition, good agricultural practices and biotechnological tools for sustainable production were addressed.
BACKGROUND: Ginsenoside Rd shows positive effects on T2DM, but its mechanism is still unknown. We explore its mechanism from inflammation levels in pancreas and intestine, and provide some evidences that this is related...BACKGROUND: Ginsenoside Rd shows positive effects on T2DM, but its mechanism is still unknown. We explore its mechanism from inflammation levels in pancreas and intestine, and provide some evidences that this is related to modulate GLP-1/MAPK/NF-κB signaling pathway. METHODS: We recorded and compared the changes in metabolic indicators about T2DM, and tested levels of GLP-1 and GLP-1R through immunohistochemistry, Western blotting, and PCR after the mice were euthanized. Moreover, we detected the effects of ginsenoside Rd on inflammatory related molecules such as AMPK, Sirt1, MAPK and NF-κB by ELISA, Transcriptomics, Western blot, and PCR. At the same time, we conducted in vitro experiments to investigate GLP-1 signaling pathway. RESULTS: After treatment with ginsenoside Rd, blood glucose decreased and insulin resistance weakened in db/db mice. The results showed an increase in the expression of GLP-1 and GLP-1R. Transcriptome analysis shows differences in inflammatory response related signaling pathways after treatment. Western blot results showed an increase in AMPK phosphorylation and a decrease in MAPK phosphorylation. Consistent experimental results were also obtained in vitro experiments. CONCLUSION: Our data suggest that Ginsenoside Rd may ameliorate T2DM in db/db mice, potentially through the inhibition of inflammatory responses in the intestine and pancreas, an effect that might be mediated by the promotion of GLP-1 secretion.
infection is related to several gastric pathologies, including gastritis, peptic ulcer, and gastric cancer. Substances capable of eradicating have been subject to the attention of researchers. This study evaluated a ful...infection is related to several gastric pathologies, including gastritis, peptic ulcer, and gastric cancer. Substances capable of eradicating have been subject to the attention of researchers. This study evaluated a fully characterized ethyl-acetate fraction (EAF), obtained from the rhizomes of and its microparticulate pharmaceutical form (mpEAF) against , and in addition for potential immunomodulatory and antitumor activities associated with infection. UHPLC analysis of EAF indicated the presence of samaragenins A and B beside gallic acid, (epi)gallocatechin, epigallocatechin-3--gallate. Antioxidant activity showed IC values of 5.7 (95% CI: 5.21-6.83), 31.9 (95% CI: 19.57-51.99), and 33.1 (95% CI: 24.4-44.73) µg/mL for HOCl, O2•- and NO, respectively. EAF exerts MIC values of 1024 and 128 µg/mL against the (ATCC 43504, clinical isolate P7). In vivo treatments in mice with EAF and mpEAF (100 mg/kg, in single daily doses for 20 consecutive days) improved gastric pathology in infected animals reducing urease positivity (14,3% vs. 54,5% in untreated controls), reducing inflammation (TNF-α, IL-1β, and IL-6 reduced, p < 0.05) and morphological damage compared with the untreated control group. urease was inhibited with IC of 521.6 µg/mL (95% CI: 419.2-649.0). In addition, EAF showed antiproliferative activity against gastric adenocarcinoma cells (CC of 21.7, 95% CI: 18.1-26.04). In LPS-stimulated macrophages, EAF reduced the TNF-α and IL-6 production by 16% and 35%, respectively. These results indicate the potential of as a source of compounds capable of attenuating gastric diseases related to infection.
Phytochemical study of aerial parts apolar extract led to the isolation of a new abietane diterpene (1: ), an abietane diterpene reported for the first time as a genuine natural product (2: ), 2 new megastigmane glycosi...Phytochemical study of aerial parts apolar extract led to the isolation of a new abietane diterpene (1: ), an abietane diterpene reported for the first time as a genuine natural product (2: ), 2 new megastigmane glycosides (3: -4: ), and 9 known compounds (5: -13: ), including 7 abietanes. Their structures were elucidated by 1D and 2D NMR spectroscopy and HRMS experiments. The crude extract was then evaluated through a broad screening against both Gram-positive and Gram-negative bacterial strains, with being the only affected microorganism. In a next step, a selection of pure compounds was also investigated, and the diterpene 15-hydroxydehydroabietic acid (15-HDAA) (11: ) was shown to exhibit detectable antibacterial activity against . Growth kinetics analysis revealed a clear modulation of bacterial growth at sub-minimum inhibitory concentration (MIC), indicating a measurable physiological impact on the bacterium. This effect, when combined, allows a significant reduction in the effective concentration of ampicillin.
Arsenijević J, Renouard C, Bacova K
… +21 more, Bilgi C, Cousin C, Di Loria A, Drobac M, Dungen FVD, Efthimiou G, Foitova I, Hunyadi A, Jacques AM, Kosakowsk O, Kristofova R, Laborieux L, Marčetić M, Pogány Simonova M, Semen Z, Styczyńska S, Schlittenlacher T, Vargas-Murga L, Walkenhorst M, Yurdakok-Dikmen B, Mendel M
ABSTRACT: The growing urgency to reduce antimicrobial and antiparasitic use in livestock has renewed scientific interest in medicinal plants as sustainable components of veterinary healthcare. However, the absence of a d...ABSTRACT: The growing urgency to reduce antimicrobial and antiparasitic use in livestock has renewed scientific interest in medicinal plants as sustainable components of veterinary healthcare. However, the absence of a dedicated regulatory framework for herbal veterinary medicinal products (HVMPs) in the European Union continues to hinder their wider application. ABSTRACT: The need for a science-based, multi-criteria framework to identify medicinal plant species as sources of active substances of herbal origin, with the highest potential for future inclusion in a dedicated EU registration pathway for HVMPs, resulted in the establishment of a multidisciplinary expert panel. The panel evaluated over 100 medicinal plant species with documented veterinary application, using a structured scoring system integrating regulatory, pharmacopoeial, toxicological, and sustainability sources. These included regulations and documents related to veterinary, pharmaceutical, food, and feed data, as well as considerations for conservation. Weighted scores reflecting all these aspects were applied to rank the species. ABSTRACT: The assessment resulted in the creation of List A, which contains the most promising candidates for future HVMPs, and List B, which compiles plant species whose simplified registration is currently not considered a priority or is not advisable based on the available data. Eighty-three species received positive overall scores. These medicinal plants demonstrate strong regulatory recognition, pharmacopoeial inclusion, and well-documented safety profiles, highlighting their suitability for evidence-based veterinary use. ABSTRACT: The proposed framework offers a clear, reproducible method for prioritizing botanical species for regulatory consideration as HVMPs. It supports EU initiatives to enhance sustainable animal health, antimicrobial stewardship, and innovation in veterinary phytotherapy.
(ground ivy) is an aromatic perennial plant extensively utilized in traditional medicine. Its therapeutic properties have been recorded in Europe since antiquity. Traditionally, it is still used to treat gastrointestinal...(ground ivy) is an aromatic perennial plant extensively utilized in traditional medicine. Its therapeutic properties have been recorded in Europe since antiquity. Traditionally, it is still used to treat gastrointestinal disorders, liver/bile diseases, respiratory ailments, and skin disorders. This review presents, for the first time, an in-depth examination of ethnopharmacology, phytochemistry, botany, safety of use, biological activity, and non-medical aspects associated with ground ivy. The data were extracted through detailed probing of key databases, including PubMed, Web of Science, Scopus, and SciFinder. In addition, books, papers from conference proceedings, and websites were used. This study reveals that compounds belonging to various classes, including phenolic acids, flavonoids, lignans, alkaloids, and terpenoids, have been identified. Crude extracts, fractions, and some individual compounds have shown various pharmacological activities, including hepatoprotective, anti-inflammatory, antioxidant, anticancer, and melanogenesis-modulating effects. Apart from its value in phytotherapy, also shows potential as a natural pesticide and stabilizing agent in the food industry. The traditional medicinal uses of the ground ivy, combined with modern scientific research, underscore its pharmacological potential. However, future studies should incorporate relevant animal experiments and clinical studies to provide a more comprehensive assessment of the efficacy and bioavailability. Although there is a rich literature on secondary metabolites detected in , it seems right to fill in which compounds are determinants of a given activity. Finally, research on using as a natural pesticide, which could lead to its implementation, warrants further investigation.
(kratom) is a psychoactive plant native to Southeastern Asia, belonging to the Rubiaceae family. Traditionally, its fresh leaves have been consumed in the region for centuries due to their therapeutic properties, includi...(kratom) is a psychoactive plant native to Southeastern Asia, belonging to the Rubiaceae family. Traditionally, its fresh leaves have been consumed in the region for centuries due to their therapeutic properties, including pain relief. The leaves contain a variety of phytochemicals with the alkaloids being the most biologically significant constituents. In the present study-the first investigation exploring sustainable extraction methods for kratom-47 natural deep eutectic solvent (NaDES) systems were screened. The most effective system demonstrated significantly higher extraction efficiency compared to commonly used organic solvents. The food-grade system, lactic acid : glucose was subsequently selected for optimization using a one-factor-at-a-time approach, and the optimal conditions were a molar ratio of 4 : 1 and a water content of 20%. Further optimization using a Box-Behnken design and response surface methodology identified the optimal extraction conditions as a solid-to-liquid ratio of 30 mg/mL, a temperature of 70 °C and an ultrasound treatment time of 12 min. Finally, three recovery methods were evaluated: solid phase extraction (including strong cation exchange and reversed-phase types), macroporous resins (six types), and acid-base extraction. The highest recovery yields were obtained with strong cation exchange solid phase extraction (95%) followed by the macroporous resins XAD 18 and XAD 1600 N (85%).
Curcumin is a versatile natural compound that has been extensively studied for its potential activity in cancer models. However, its clinical development faces challenges, including poor water solubility, chemical instab...Curcumin is a versatile natural compound that has been extensively studied for its potential activity in cancer models. However, its clinical development faces challenges, including poor water solubility, chemical instability under physiological conditions, rapid metabolism, and limited systemic bioavailability. These issues have driven efforts to modify the curcumin structure to enhance stability, pharmacokinetics, and target interaction, while preserving or improving its antiproliferative effects. This review highlights key medicinal chemistry strategies for creating analogs beyond curcumin, including (i) monocarbonyl variants that replace the -diketone group to improve stability, (ii) aromatic ring modifications that adjust electronic properties, lipophilicity, and cellular entry, (iii) prodrug designs that conceal phenolic groups to increase solubility or permeability, and (iv) hybrid molecules and conjugates for dual targeting or better delivery. Additionally, we discuss metal-curcumin(oid) complexes as promising options to modify stability, redox activity, and biological effects in cancer models. We also propose a basic evaluation toolkit to support more consistent comparisons among analogs, emphasizing the need to report chemical stability, microsomal metabolism, selectivity, and exposure, alongside viability/proliferation readouts and, where available, orthogonal cytotoxicity endpoints. Rather than treating beyond-curcumin chemistry as a catalog of potency-improving modifications, this review frames the major scaffold classes in terms of developability, evidentiary burden, and translational pragmatism. Overall, successful translation will depend less on isolated IC gains and more on standardized profiling and alignment of mechanism claims with achievable exposure.
Cultivated lichen mycobionts represent a valuable resource for obtaining unique natural compounds. Mycobionts of and , collected in Vietnam, were isolated, cultivated, and subjected to chemical investigation. Consequent...Cultivated lichen mycobionts represent a valuable resource for obtaining unique natural compounds. Mycobionts of and , collected in Vietnam, were isolated, cultivated, and subjected to chemical investigation. Consequently, three new compounds, straminones A - B (A1: and A2: ) and chlorosemivioxanthin (N1: ), along with five known compounds, 3,4-(+)-4-hydroxymellein (A3: ), 6-methoxymellein (A4: ), vioxanthin (N2: ), pigmentosin A (N3: ), and semivioxanthin (N4: ), were isolated and structurally elucidated. Straminones A and B represent the first examples of 3-methylhexahydrocyclopenta[]pyran-1(3)-one skeletons found in nature. The relative configuration of A1: was confirmed by DFT calculation. Compounds A3: and N4: demonstrated weak alpha-glucosidase inhibitory activity, with IC values of 314 and 366 µM, respectively. The other compounds showed no inhibition in the tested assay. Notably, compounds N1: -N3: showed significant inhibitory effects on NO production, with IC values ranging from 14 to 25 µM, compared with the positive control L-NMMA (IC = 49 µM). Further molecular docking clarified the inhibitory mechanism of the active compounds.
Hydroxychloroquine (HCQ), a commonly used drug for Sjögren's syndrome (SS), is ineffective, highlighting the need for better treatments for salivary gland damage in SS. The study evaluated the effects of (HJ) on SS usin...Hydroxychloroquine (HCQ), a commonly used drug for Sjögren's syndrome (SS), is ineffective, highlighting the need for better treatments for salivary gland damage in SS. The study evaluated the effects of (HJ) on SS using non-obese diabetic (NOD) mice treated with HJ, HCQ, or both for six weeks. Body weight, saliva levels, and submandibular gland histology were assessed. Various techniques were used to analyze apoptosis and oxidative stress. Network pharmacology identified therapeutic targets, and lentivirus technology was used to suppress CHRM3 gene expression to understand HJ's mechanisms against SS. HJ treatment significantly mitigates salivary gland damage, resulting in increased body weight, reduced water intake, and improved saliva flow rates. Histological evaluations revealed HJ reduced lymphocytic infiltration, restored glandular architecture, and alleviated oxidative stress. In addition, the study has the following key mechanistic finding: HJ upregulated the expression of the target proteins CHRM3 and AQP5 in submandibular glands. Additionally, HJ can significantly enhance the expression of CHRM3 and AQP5 in human salivary gland (HSG) cells after silencing CHRM3. This study revealed that HJ may act as a novel SS treatment by activating the CHRM3/AQP5 axis, promoting water channel transport, alleviating salivary gland damage, and enhancing saliva secretion. Moreover, the combination of HJ and HCQ could significantly improve the therapeutic benefit. These findings provide a new therapeutic strategy for SS.
The scientific literature is increasingly challenged by miscitation, publication bias, and the uncritical perpetuation of false information. One such case concerns the purported presence of caffeine in damiana, a botanic...The scientific literature is increasingly challenged by miscitation, publication bias, and the uncritical perpetuation of false information. One such case concerns the purported presence of caffeine in damiana, a botanical ingredient marketed for "sexual well-being". While consumer perception and regulatory implications make caffeine content highly relevant, a systematic review of the literature indicates that claims of caffeine in damiana () largely stem from erroneous or circular referencing, including citations of studies where caffeine was never reported. To address this discrepancy experimentally, we conducted NMR analyses on authenticated aerial and seed material of and seeds of . No caffeine was detected, with a detection limit of < 4 nM, corresponding to < 4 µg caffeine per daily serving of damiana. These findings confirm that damiana is effectively caffeine-free. Beyond correcting a specific phytochemical misconception, this study highlights how flawed referencing practices can perpetuate modern "scientific myths", emphasizing the need for more rigorous citation ethics and the value of experimental data. Addressing such errors is critical not only for scientific accuracy but also for consumer trust and evidence-based regulatory decision-making.
, a widely used West African palm, is a staple food source and a traditional medicinal plant with emerging relevance to immunometabolic pharmacology. This narrative review integrates ethnobotanical, phytochemical and pha..., a widely used West African palm, is a staple food source and a traditional medicinal plant with emerging relevance to immunometabolic pharmacology. This narrative review integrates ethnobotanical, phytochemical and pharmacological evidence, with particular emphasis on oxidative stress, cytokine signalling and low-grade inflammation. Available non-clinical and limited human data indicate that preparations derived from inflorescences, fruit pulp and kernels may exert antioxidant, anti-inflammatory and cardiometabolic effects, although the evidence base remains heterogeneous. Major constituents, including polyphenols, terpenoids, sterols, saponins and lipid fractions, are discussed in relation to redox-sensitive and inflammation-related pathways, particularly nuclear factor-kappa B (NF-B) and nuclear factor erythroid 2-related factor 2 (Nrf2), as well as cytokine networks implicated in metabolic and cardiovascular disorders. In rodent models, preparations have been associated with reductions in oedema, nociception, pyrexia, hyperglycaemia and dyslipidaemia, often alongside lower C-Reactive protein and oxidative stress markers. Preliminary human studies using -enriched bread in individuals at cardiometabolic risk have reported improvements in blood pressure (BP) and lipid profile, suggesting a possible effect on low-grade inflammatory status. Overall, the available evidence supports a multi-target framework in which may influence cytokine-related and redox-regulated processes, while highlighting substantial limitations, including variable extraction methods, incomplete phytochemical characterisation, sparse cytokine measurements and small clinical samples. Future work should prioritise standardised chemo-fingerprinting, multiplex cytokine profiling, metabolomic integration and pragmatic dietary or extract-based interventions in at-risk populations. may therefore serve as a useful model for a structured pharmacological evaluation of plant-derived foods within an immunometabolic context.
Herbal medicinal products (HMPs) are widely used in European paediatric practice, but formal authorisations for their use in children remain limited. Following the 2024 workshop in Krakow, the Foundation Plants for Healt...Herbal medicinal products (HMPs) are widely used in European paediatric practice, but formal authorisations for their use in children remain limited. Following the 2024 workshop in Krakow, the Foundation Plants for Health (FPfH) organised a further workshop in Naples on 31 August 2025 as part of the 73rd International Congress and Annual Meeting of the Society for Medicinal Plant and Natural Product Research (GA) to present updates of recent activities in the field of real-world data (RWD) and real-world evidence (RWE) for rationalising the usage of herbal medicines in children. Speakers presented concrete new data sources - private health insurance claims, patient reported outcome cohorts, and a social-media-based user survey - as well as modern methods in epidemiology. The workshop concluded that decision-relevant paediatric data on the use of HMPs can be generated efficiently by establishing new RWD data sources. For the subsequent next steps, it is necessary to engage with regulators to open usage of these data pools in regulatory practice.
The Japanese pearl tree (), an ornamental species native to East Asia, has long been valued in traditional Chinese medicine and is now gaining renewed attention for its multifaceted pharmacological potential. This review...The Japanese pearl tree (), an ornamental species native to East Asia, has long been valued in traditional Chinese medicine and is now gaining renewed attention for its multifaceted pharmacological potential. This review synthesizes the current knowledge of its bioactive compounds, particularly flavonoids such as genistein, rutoside, quercetin, and sophoricoside, and their broad-spectrum biological activities, including antioxidant, anti-inflammatory, antimicrobial, neuroprotective, and wound-healing effects. These phytochemicals contribute to protective mechanisms against oxidative stress, skin photoaging, osteoporosis, cardiovascular dysfunction, and metabolic disorders such as diabetes and obesity. Emerging evidence also supports their role in managing neurodegenerative and inflammatory diseases, alopecia, and postmenopausal symptoms. Despite its promise, the clinical translation of remains limited by gaps in safety, pharmacokinetic characterization, and standardized extraction protocols. Looking ahead, integrative approaches combining phytochemistry, pharmacogenomics, and advanced biotechnology are expected to unlock its full therapeutic potential. By bridging traditional use with precision medicine and sustainable bioprocessing, stands as a prospective source of next-generation plant-based therapeutics for modern healthcare.
Flavonoids are a large group of polyphenolic secondary metabolites of plants with high biologically active properties. Their determination in plant extracts (medicinal, edible, and other plants, as well as products made...Flavonoids are a large group of polyphenolic secondary metabolites of plants with high biologically active properties. Their determination in plant extracts (medicinal, edible, and other plants, as well as products made from them) with a complex chemical composition is a difficult task and requires effective separation of the components. In this study, a new approach to the determination of 18 flavonoids in plant extracts using reversed-phase comprehensive two-dimensional liquid chromatography with UV detection (LC×LC-UV) is proposed. The approach has been successfully tested on various plant raw materials: above-ground parts of bog rosemary, bog bilberry, bilberry, lingonberry, and cranberry, as well as aspen and apricot knots. It was found that aspen knots are a rich source of aromadendrin and naringenin and their derivatives, while apricot knots are a rich source of catechin and epicatechin, and bog rosemary is a rich source of quercetin glycosides-hyperoside, reinoutrin, and avicularin. The approach for isolation of pure hyperoside, reinoutrin, and avicularin from bog rosemary extract by preparative HPLC was proposed. Other phenolic compounds of the studied plant extracts were classified (by LC×LC-MS/MS) as hydroxycinnamic acid derivatives, iridoids, and flavonoids. The developed approaches are promising for bioprospecting of flavonoids and phenolic compounds in various plant materials. It can also be used for quality control of medicinal, edible, and other plants, as well as products made from them.
Previous studies have highlighted the effects of lemongrass essential oil () on the cardiovascular system, particularly its hypotensive and vasodilatory properties. Given the heart's crucial role in blood pressure regula...Previous studies have highlighted the effects of lemongrass essential oil () on the cardiovascular system, particularly its hypotensive and vasodilatory properties. Given the heart's crucial role in blood pressure regulation, this study aimed to investigate the impact of lemongrass essential oil (EOCC) on cardiac excitation-contraction coupling and voltage-gated ion channel currents. Chemical analysis of EOCC, conducted through gas chromatography-mass spectrometry, identified geranial (39.9%) and neral (27.4%) as the primary components. The effect of EOCC on cardiac contractility was assessed using isolated guinea pig atria. The results showed that EOCC decreased both the contraction amplitude and the frequency of spontaneous atrial contraction in a concentration-dependent manner (IC values of 106.8 µg/mL, 95% CI=78.9 to 133 µg/mL and 258.4 µg/mL, 95% CI=202.7 to 443.2 µg/mL n = 5 - 8, respectively). Notably, EOCC exhibited arrhythmogenic activity, since it induced spontaneous contractions in isolated atrial preparations. Additionally, in an arrhythmia model induced by ouabain, EOCC significantly reduced the time to arrhythmia onset by 67.8% (n = 4). To further explore the mechanisms of the essential oil in atrial excitability, we employed the patch-clamp technique on isolated ventricular cardiomyocytes to examine EOCC's effects on the L-type calcium current (I). The human embryonic kidney cell line (HEK293) transiently expressing human Na 1.5 was used to study the effects on cardiac sodium currents (I). EOCC reduced the peak amplitude of both I and I in a concentration- and voltage-dependent manner, with IC values of 299.7 µg/mL (95% CI=241.5 to 358 µg/mL, n = 6 - 7) for I and 132.8 µg/mL (95% CI=71 to 173.8, n = 9) for I. In conclusion, the negative inotropic of EOCC may significantly contribute to its hypotensive effects. However, the association of relatively low concentrations of EOCC with cardiac arrhythmias raises concerns about its medicinal use.
Kynurenine (KYN) is a non-protein amino acid and major metabolite of tryptophan associated with human health. The acidic form, kynurenic acid (KYNA), has been previously identified in St. John's wort (SJW) tablets and te...Kynurenine (KYN) is a non-protein amino acid and major metabolite of tryptophan associated with human health. The acidic form, kynurenic acid (KYNA), has been previously identified in St. John's wort (SJW) tablets and tea, but other metabolites in the pathway are not known in the species. We developed and validated two liquid chromatography-mass spectrometry-based (UHPLC-Orbitrap MS) methods for the quantification of KYNA, KYN, 3-hydroxykynurenine (3-HK), and 3-hydroxyanthranilic acid (3-HAA). We compared two approaches: (1) derivatisation via 6-aminoquinolyl-N-hydroxysuccinimidyl carbamate (AQC) and (2) analysis of underivatised extracts. KYN was detected in both methods (78% and 101% recovery in underivatised and derivatised, respectively), and 3-HAA was detected only by the underivatised method (95%), while 3-HK was detected only by the derivatised method (90%). Methods were validated for key parameters, including linearity, accuracy, precision, limit of detection (LOD), and limit of quantification (LOQ). Three of the KYN metabolites were detected in -grown SJW shoots: KYN (101 ng/g), KYNA (104 ng/g), and 3-HAA (670 ng/g). Significantly more KYN and KYNA was detected in greenhouse-grown plants than in tissue-cultured SJW. KYN, KYNA, and 3-HAA were also quantified in commercial preparations of SJW at 0.07 - 0.42 µg/g (KYN), 2.31 - 6.45 µg/g (KYNA), and 0.86 - 3.54 µg/g (3-HAA); 3-HK was not detected in any of our SJW samples. These data support future studies to understand the role of kynurenine metabolites in plant metabolism and plant-based products.
Glycyrrhizae Radix (GR), the dried root and stolon of or , is most frequently used as a crude drug, compounding Kampo medicines to treat a variety of diseases in Japan. This key crude drug, however, would be coinstantan...Glycyrrhizae Radix (GR), the dried root and stolon of or , is most frequently used as a crude drug, compounding Kampo medicines to treat a variety of diseases in Japan. This key crude drug, however, would be coinstantaneously a risk factor for pseudoaldosteronism. This adverse effect is thought to be due to glycyrrhetinic acid (GA), a major metabolite of glycyrrhizin, which is one of the ingredients of GR. Therefore, we thought that if the blood GA concentration could be measured quickly and easily when side effects occur, the causal relationship could be clarified, and side effects could be avoided. To realize this plan, we developed the competitive ELISA using anti-GA monoclonal antibody (mAb6D6), which was labeled 'biotin' to avoid endogenous effects, such as antibodies in serum, and to detect GA sensitively. This ELISA could quantify GA from about 10 pg/mL to 25 ng/mL. The quantitative value of GA in serum based on this ELISA was significantly corelated with that of GA based on high-performance liquid chromatography. Hence, the developed competitive ELISA could be an useful tool for users who would like to quantify the blood GA concentration to clarify the relationship between GA and pseudoaldosteronism derived from the intake of medicines containing GR and to lead to avoiding side effects derived from GA.