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Imported fire ants are significant agricultural pests. Repellents can be used to prevent foraging fire ants from entering sensitive areas, including electrical equipment, nursing homes, and hospitals. Bioassay-guided fractionation of the essential oil extracted from gurjun balsam (Dipterocarpus turbinatus) resulted in the identification of (-)-α-copaene (1) as the repellent constituent with a minimum repellent effective dose (MRED) of 15.6 µg/g against both red imported fire ants (Solenopsis invicta) and hybrid imported fire ants (Solenopsis invicta × Solenopsis richteri). Stereoselective oxidation of 1 via autoxidation and chemical methods produced (-)-5R-hydroperoxy-α-copaene (2), (+)-3S-hydroperoxycopa-4-ene (3), (-)-α-copaene oxide (4), (+)-ß-copaen-4α-ol (5), copaenediol (6), and copaene ketol (7). Reduction of 2 and 3 with triphenylphosphine afforded (-)-5R-hydroxy-α-copaene (2a) and (+)-3S-hydroxycopa-4-ene (3a), respectively, which led to the structural revision of copa-3-en-2α-ol and copa-2-en-4-ol as 2a and 3, respectively. The configurational assignment of compound 4 in the literature was also clarified by the detailed analysis of 2D NMR spectroscopic data. Compounds 2-7 showed repellency with MREDs ranging from 3.9 to 15.6 µg/g against hybrid and red imported fire ants, indicating that chemical modification can enhance the repellent effect of (-)-α-copaene.
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The Brassicaceae family, commonly referred to as cruciferous plants, is globally cultivated and consumed, with the Brassica genus being particularly renowned for its functional components. These vegetables are rich sources of nutrients and health-promoting phytochemicals, garnering increased attention in recent years. This study presents a comprehensive microscopic, chromatographic, and spectroscopic characterization of Brassica napus L. seeds from Kazakhstan aimed at elucidating their morphological features and chemical composition. Microscopic analysis revealed distinct localization of flavonoids, total lipids, and alkaloids. High-performance thin-layer chromatography (HPTLC) analysis of seed extracts demonstrated a complex chemical profile with significant quantities of non-polar compounds in the hexane extracts. Additionally, methanolic extracts revealed the presence of diverse chemical compounds, including alkaloids, flavonoids, and glucosinolates. The chemical composition exhibited varietal differences across different Brassica species, with B. napus L. seeds showing higher concentrations of bioactive compounds. Furthermore, liquid chromatography-quadrupole time-of-flight mass spectrometry (LC-QToF-MS) analysis provided insights into the chemical composition, with sinapine isomers, feruloyl, and sinapoyl choline derivatives as major compounds in the seeds. This study contributes to a better understanding of the chemical diversity and quality control methods' approximations of B. napus L. seeds, highlighting their importance in functional food and nutraceutical applications.
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Brassica napus , Semillas , Brassica napus/química , Semillas/química , Extractos Vegetales/química , Extractos Vegetales/análisis , Fitoquímicos/análisis , Fitoquímicos/química , Cromatografía en Capa Delgada/métodos , Cromatografía Líquida de Alta Presión/métodos , Flavonoides/análisis , Flavonoides/química , Alcaloides/análisis , Alcaloides/química , Cromatografía Liquida/métodos , Espectrometría de Masas/métodos , Glucosinolatos/análisis , Glucosinolatos/químicaRESUMEN
BACKGROUND AND AIM: Chamomile tea, renowned for its exquisite taste, has been appreciated for centuries not only for its flavor but also for its myriad health benefits. In this study, we investigated the preventive potential of chamomile (Matricaria chamomilla L.) towards cancer by focusing on its anti-inflammatory activity. METHODS AND RESULTS: A virtual drug screening of 212 phytochemicals from chamomile revealed ß-amyrin, ß-eudesmol, ß-sitosterol, apigenin, daucosterol, and myricetin as potent NF-κB inhibitors. The in silico results were verified through microscale thermophoresis, reporter cell line experiments, and flow cytometric determination of reactive oxygen species and mitochondrial membrane potential. An oncobiogram generated through comparison of 91 anticancer agents with known modes of action using the NCI tumor cell line panel revealed significant relationships of cytotoxic chamomile compounds, lupeol, and quercetin to microtubule inhibitors. This hypothesis was verified by confocal microscopy using α-tubulin-GFP-transfected U2OS cells and molecular docking of lupeol and quercetin to tubulins. Both compounds induced G2/M cell cycle arrest and necrosis rather than apoptosis. Interestingly, lupeol and quercetin were not involved in major mechanisms of resistance to established anticancer drugs (ABC transporters, TP53, or EGFR). Performing hierarchical cluster analyses of proteomic expression data of the NCI cell line panel identified two sets of 40 proteins determining sensitivity and resistance to lupeol and quercetin, further pointing to the multi-specific nature of chamomile compounds. Furthermore, lupeol, quercetin, and ß-amyrin inhibited the mRNA expression of the proinflammatory cytokines IL-1ß and IL6 in NF-κB reporter cells (HEK-Blue Null1). Moreover, Kaplan-Meier-based survival analyses with NF-κB as the target protein of these compounds were performed by mining the TCGA-based KM-Plotter repository with 7489 cancer patients. Renal clear cell carcinomas (grade 3, low mutational rate, low neoantigen load) were significantly associated with shorter survival of patients, indicating that these subgroups of tumors might benefit from NF-κB inhibition by chamomile compounds. CONCLUSION: This study revealed the potential of chamomile, positioning it as a promising preventive agent against inflammation and cancer. Further research and clinical studies are recommended.
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BACKGROUND: Immulina®, a dietary supplement derived from Limnospira (formerly Arthrospira), is being investigated as a potential agent to increase antiviral resilience. In our recently published manuscript, we described the effects of Immulina® on influenza when taken daily, beginning before infection (prophylaxis) or after the onset of clinical symptoms of viral illness (therapeutic). However, the benefit of Immulina® in infected individuals before the manifestation of any symptoms (prodromal) has not been investigated yet. PURPOSE: To evaluate Immulina®'s potential use to increase the host antiviral immune response using a prodromal therapy regime. STUDY DESIGN: The efficacy of Immulina® extract was evaluated in rodents using a prodromal protocol (test material administered prior to the emergence of viral illness symptoms). METHODS: Immulina® (25, 50 and 100 mg/kg body weight) was orally administered to both genders of mice, 2 h following influenza A viral infection, and continued daily for 14 days. RESULTS: Compared to the infected control mice, animals fed Immulina® exhibited statistically significant reduction in the emergence of various physical symptoms of viral-induced illness and decreased viral RNA levels. The effects are likely mediated through the host immune system since the level of various cytokines (IL-6 and IFN-γ) were significantly increased in lung tissue. CONCLUSION: This study, together with our previous paper, indicate that Immulina® was most effective at enhancing immune antiviral resilience if administered before or soon after initial infection. The data generated can be used to guide additional research using human subjects.
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Infecciones por Orthomyxoviridae , Animales , Infecciones por Orthomyxoviridae/tratamiento farmacológico , Infecciones por Orthomyxoviridae/prevención & control , Femenino , Masculino , Ratones , Antivirales/farmacología , Interferón gamma , Ratones Endogámicos BALB C , Suplementos Dietéticos , Pulmón/efectos de los fármacos , Pulmón/virología , Virus de la Influenza A/efectos de los fármacos , Cianobacterias/química , Síntomas ProdrómicosRESUMEN
BACKGROUND: In April 2022, French Lentil and Leek Crumble (FLLC), a new frozen food preparation manufactured by Daily Harvest™ (containing Tara flour) was offered as a natural high-protein meal product. Soon thereafter, widespread anecdotal reports of acute gastrointestinal symptoms with liver injury were reported, leading to its voluntary withdrawal in June 2022, after shipment of 28,000 preparations. AIMS: To summarise the clinical and laboratory features of 17 patients with FLLC associated liver injury from the Drug Induced Liver Injury Network (DILIN). METHODS: Patients with FLLC-associated liver injury were enrolled into a prospective protocol and followed for 6 months. Cases were adjudicated by expert opinion causality assessment with summary statistics for data analysis. RESULTS: Enrolled subjects had a mean age of 41 years, 82% were female with mean BMI of 24 kg/m2. All were Caucasian without underlying liver disease. In most cases, abdominal pain and nausea arose within hours of FLLC ingestion. Mean days from ingestion to identification of liver injury was 3.1 days (±2.8). On enrolment, 53% had jaundice, 47% nausea, 24% fever, 59% abdominal pain, 41% itching and 12% rash. The mean initial serum ALT was 475 U/L (±302), AST 315 U/L (±315), alkaline phosphatase 190 U/L (±76), with a total bilirubin of 2.6 mg/dL (±2). In this study, 63% presented with a hepatocellular pattern of liver injury, 6% cholestatic and 31% mixed as determined by the R value. In addition, 24% of patients were hospitalised, and there were no fatalities or liver transplants. Liver biopsy in one subject revealed acute hepatitis with mild ductular reaction, mild lymphocytic and eosinophilic portal inflammation, mild lobular inflammation, preserved bile ducts and absence of interface hepatitis, steatosis, granulomatous reaction or cholestasis. Phylogenetic analysis confirmed the presence of Tara spinosa, the source of Tara flour. CONCLUSIONS: Natural food products are increasingly ubiquitous and may unexpectedly cause significant illness. All clinicians should inquire whether patients are consuming natural food products or herbal supplements and consider them as a potential cause of liver injury.
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Enfermedad Hepática Inducida por Sustancias y Drogas , Suplementos Dietéticos , Brotes de Enfermedades , Humanos , Femenino , Adulto , Masculino , Enfermedad Hepática Inducida por Sustancias y Drogas/etiología , Suplementos Dietéticos/efectos adversos , Estudios Prospectivos , Persona de Mediana Edad , Adulto JovenRESUMEN
BACKGROUND: Illness resulting from influenza is a global health problem that has significant adverse socioeconomic impact. Although various strategies such as flu vaccination have beneficial effects, the risk of this illness has not been eliminated. The use of botanicals may provide a complementary approach by enhancement of the host antiviral immune response. PURPOSE: Generate preclinical data using rodent models to determine the most effective utility of a Limnospira (formerly Arthrospira)-derived oral supplement (Immulina®) for enhancing host immunity to improve antiviral resilience. STUDY DESIGN: Two non-lethal mouse models (prophylactic and therapeutic) were used to evaluate the impact of Immulina® on increasing host resilience against experimental influenza infection. METHODS: Mice were fed Immulina® only for the 2 weeks prior to viral infection (prophylactic regime) or starting 3 days post-viral infection (at the onset of symptoms, therapeutic design). Three doses of Immulina® were evaluated in each model using both female and male mice. RESULTS: Significant protective effect of Immulina® against viral illness was observed in the prophylactic model (improved clinical scores, less body weight loss, decreased lung/body weight ratio, lower lung viral load, and increased lung IFN-γ and IL-6). Substantially less (minimal) protective effect was observed in the therapeutic model. CONCLUSION: This study demonstrates that Immulina® exerts a protective effect against influenza illness when administered using a prophylactic regime and may not be effective if given after the onset of symptoms. The results will help to optimally design future clinical trials.
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Modelos Animales de Enfermedad , Infecciones por Orthomyxoviridae , Animales , Femenino , Masculino , Infecciones por Orthomyxoviridae/tratamiento farmacológico , Infecciones por Orthomyxoviridae/inmunología , Ratones , Pulmón/efectos de los fármacos , Interferón gamma/metabolismo , Ratones Endogámicos BALB C , Interleucina-6/metabolismo , Antivirales/farmacología , Suplementos DietéticosRESUMEN
The Cichorium plants are particularly notable due to their remarkable therapeutic and medicinal properties, besides being used as food and conventional medication. Although Cichorium plants have been studied for their phytoconstituents and biological activities, there is limited knowledge about the constituents of the roots of C. bottae. A phytochemical study of the 90% MeOH extract of C. bottae roots resulted in the isolation of twelve compounds belonging to guaianolide sesquiterpene lactones, sesquiterpene lactone glucosides, and phenolic derivatives, of which two compounds designated as 9α-hydroxycrepediaside B (1) and cichobotinal (2) were previously undescribed. The isolated compounds were assessed for their anti-inflammatory potential through the inhibition of inducible nitric oxide synthase (iNOS) and resultant decrease in nitric oxide generation in LPS-induced macrophages. Among the isolates, compounds 2 and 11 (8-deoxylactucin) inhibited iNOS activity with IC50 values of 21.0 ± 4 and 6.8 ± 0.1 µM, respectively. The methanolic extract of C. bottae inhibited iNOS with an IC50 of 10.5 ± 0.5 µg/mL.
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Antiinflamatorios , Macrófagos , Óxido Nítrico Sintasa de Tipo II , Óxido Nítrico , Fitoquímicos , Extractos Vegetales , Raíces de Plantas , Antiinflamatorios/farmacología , Antiinflamatorios/aislamiento & purificación , Fitoquímicos/farmacología , Fitoquímicos/aislamiento & purificación , Raíces de Plantas/química , Células RAW 264.7 , Ratones , Animales , Estructura Molecular , Óxido Nítrico Sintasa de Tipo II/antagonistas & inhibidores , Óxido Nítrico Sintasa de Tipo II/metabolismo , Óxido Nítrico/metabolismo , Macrófagos/efectos de los fármacos , Extractos Vegetales/farmacología , Extractos Vegetales/química , Lactonas/farmacología , Lactonas/aislamiento & purificación , Sesquiterpenos/farmacología , Sesquiterpenos/aislamiento & purificación , Fenoles/farmacología , Fenoles/aislamiento & purificación , Glucósidos/farmacología , Glucósidos/aislamiento & purificación , Sesquiterpenos de Guayano/farmacología , Sesquiterpenos de Guayano/aislamiento & purificaciónRESUMEN
Many polyprenylated acylphloroglucinols with fascinating chemical structures and intriguing biological activities have been identified as key to phytochemicals isolated from Garcinia, Hypericum, and related genera. In the present work, two chiral, tautomeric, highly-oxygenated polyprenylated acylphloroglucinols tethered with acyl and prenyl moieties on a bicyclo[3.3.1]nonanetrione core were isolated from the 95% ethanolic extract of Garcinia gummi-gutta fruit. The structures of both compounds were elucidated based on the NMR and MS data with ambiguity in the exact position of the enol and keto functions at C-1 and C-3 of the core structure. The structures of both polyprenylated acylphloroglucinols were established as a structurally revised guttiferone J and the new iso-guttiferone J with the aid of gauge-independent atomic orbital NMR calculations, CP3 probability analyses, specific rotation calculations, and electronic circular dichroism calculations in combination with the experimental data. The structures of both compounds resemble hyperforin, a potent activator of the human pregnane X receptor. As expected, both compounds showed strong pregnane X receptor activation at 10 µM [7.1-fold (guttiferone J) and 5.0-fold (iso-guttiferone J)], explained by a molecular docking study, necessitating further in-depth investigation to substantiate the herb-drug interaction potential of G. gummi-gutta upon co-administration with pharmaceutical drugs.
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Garcinia , Espectroscopía de Resonancia Magnética , Garcinia/química , Estructura Molecular , Frutas/química , Benzofenonas/química , Benzofenonas/aislamiento & purificación , Benzofenonas/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Fitoquímicos/aislamiento & purificación , Fitoquímicos/química , Fitoquímicos/farmacología , Floroglucinol/química , Floroglucinol/aislamiento & purificación , HumanosRESUMEN
Importance: Dietary supplements for weight loss, among the most popular supplement products on the market, are promoted not only for losing weight and shedding fat, but also for added benefits of energy and performance, all packed into 1 capsule with multiple combinations of ingredients. Fraudulent marketing of weight loss supplements, some with exaggerated claims, some that are potentially dangerous, and some that contain illegal ingredients, is ever present, especially through online sources, where multiple manufacturers target service members by offering military discounts. Objectives: To examine whether select dietary supplements marketed online for weight loss from companies advertising military discounts are accurately labeled according to the Supplement Facts listed ingredients, whether they contain any ingredients prohibited for use in the military, and to qualitatively describe the products' label claims. Design, Setting, and Participants: In this case series, 30 dietary supplement products marketed for weight loss were selected and purchased in June 2023 from 12 online companies advertising military discounts. Data were analyzed from July to August 2023. Main Outcomes and Measures: Liquid chromatography-mass spectrometry was used to verify whether products were accurately labeled according to the Supplement Facts listed ingredients and whether they contained any substances on the DoD Prohibited Dietary Supplement Ingredients List. A separate analysis was conducted to describe product label claims by using the Operation Supplement Safety (OPSS) Risk Assessment Scorecard. Results: Of the 30 products tested, analysis showed that 25 had inaccurate labels. Of these, 24 had ingredients listed on the label that were not detected (misbranded); 7 had hidden components not present on the label, some of which would be considered adulterated; and 10 had substances on the DoD Prohibited Dietary Supplement Ingredients List either on or hidden from the label. All products were rated as risky when applying the OPSS Scorecard. Conclusions and Relevance: In this case series study, the majority of products had inaccurate labels. Some were misbranded, others would be considered adulterated with ingredients not allowed in dietary supplements, and some contained ingredients prohibited for use in the military.
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Suplementos Dietéticos , Pérdida de Peso , Suplementos Dietéticos/normas , Suplementos Dietéticos/análisis , Humanos , Personal Militar , Estados Unidos , Etiquetado de Productos/normas , Publicidad , Mercadotecnía , Fármacos Antiobesidad/análisisRESUMEN
The inflorescences of the Mexican gordolobo are used as a folk medicine to treat various respiratory diseases. Currently, the botanical species that bear the name Mexican gordolobo belong to the genera Gnaphalium and Pseudognaphalium. Despite a long history of traditional use, most Mexican gordolobo species have never been fully chemically characterized, and the range of constituents in the species has not been comprehensively reported. To establish a quality control and chemical characterization method, a total of 49 samples belonging to 18 species of Pseudognaphalium and four species of Gnaphalium were studied. Nine flavones were quantified using a UPLC-PDA method. The method was validated in terms of linearity (R2 > 0.99), precision (intra- and inter-day: 0.1-3.9%), accuracy (96-103%), detection limit (10â¯ng/mL), limit of quantification (25â¯ng/mL) and robustness. 3-Methylquercetin, luteolin, quercetin, 3,5-dihydroxy-6,7,8-trimethoxyflavone, apigenin and gnaphaliin A were present at relatively high levels in most of the samples analyzed. The samples of P. oxyphyllum and P. liebmannii showed the highest content of the 9 compounds analyzed. Whereas the samples of the 5 species of Gnaphalium showed the lowest levels, including non-detectable, of the 9 compounds quantified. This marks an important difference with Pseudognaphalium species. Furthermore, using UHPLC-ESI-QToF data with targeted and non-targeted approaches, 57 compounds, were identified in Mexican gordolobo samples. Flavonoids were the main group of compounds found in Mexican gordolobo.
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Flavonas , Gnaphalium , Extractos Vegetales , Cromatografía Líquida de Alta Presión/métodos , Flavonas/análisis , Flavonas/química , Gnaphalium/química , Extractos Vegetales/química , Extractos Vegetales/análisis , Límite de Detección , Reproducibilidad de los Resultados , México , Control de Calidad , Medicina Tradicional/métodos , Espectrometría de Masas en Tándem/métodos , Espectrometría de Masas/métodosRESUMEN
A novel nor-megastigmane, normegastigmane-5α,9-epoxy-3ß,8-diol (1), together with 10 known compounds of diverse classes including megastigmanes, sesquiterpenoids, and triterpenoids were isolated from the leaves of Rhaphiostylis beninensis. The structure of 1 was established by 1D and 2D NMR and HRESIMS data analysis. The known compounds were identified as 5,11-epoxy-3,9-megastigmanediol (2), 7-megastigmene-3,6,9-triol (3), 1,3-dihydroxypropan-2-yl stearate (4), (1E,5E)-1,5-dimethyl-8-(propan-2-ylidene)cyclodeca-1,5-diene germacrene (5) 3,5-dihyroxy-6,7-megastigmadien-9-one (6), squalene (7), ß-amyrin (8), ß-amyrone (9), ß-amyrin eicosanoate (10), and ß-sitosterol (11). Compounds 2, 3, and 6 displayed inhibitory effects on acetylcholinesterase enzyme. This is the first report of these compounds from the plant and their anticholinesterase activity.
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In this study, bioactive compounds were isolated and characterized from the leaves and root-barks extracts of S.latifolius, with subsequent in vitro experimental investigations for antihyperglycemic potentials on α-amylase and α-glucosidase enzymes. Thirteen bioactive compounds were identified, including 10-Hydroxystrictosamide (2) and Quinovic acid-3-O-α-L-rhamnosyl-28-O-ß-d-glucopyranosyl ester (8), using chromatographic, nuclear magnetic resonance spectroscopy (NMR), and mass spectrometry (MS) techniques. Experimental assays revealed that compounds 1-4 exhibited potent inhibition of α-amylase and α-glucosidase, with compound 2 demonstrating the most potent α-amylase inhibition (IC50 value of 0.52 ± 0.003 µg/mL). Compound 8 showed a lower IC50 value (0.098 ± 0.016 µg/mL) against α-glucosidase compared to compound 2 and acarbose. Synergistic effects among the compounds could enhance their inhibitory actions on the enzymes, positioning them as potential anti-hyperglycemia agents. Compound 2 displayed the highest binding affinity (-7.970 kcal/mol) when docked against α-amylase (PDB ID: 2QV4), comparable to acarbose (-8.515 kcal/mol). It also ranked among the top ligands against α-glucosidase (PDB ID 3TOP), although compound 13 and acarbose had higher docking scores. All compounds exhibited ideal ADMET properties, suggesting good bioavailability and low toxicity. In conclusion, the isolated compounds exhibit promising antihyperglycemic potential and favourable safety profiles for further exploration.
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Inhibidores de Glicósido Hidrolasas , Hipoglucemiantes , Simulación del Acoplamiento Molecular , Fitoquímicos , Hojas de la Planta , Raíces de Plantas , alfa-Amilasas , Fitoquímicos/farmacología , Fitoquímicos/aislamiento & purificación , Hojas de la Planta/química , alfa-Amilasas/antagonistas & inhibidores , Inhibidores de Glicósido Hidrolasas/farmacología , Inhibidores de Glicósido Hidrolasas/aislamiento & purificación , Raíces de Plantas/química , Estructura Molecular , Hipoglucemiantes/farmacología , Hipoglucemiantes/química , Hipoglucemiantes/aislamiento & purificación , alfa-Glucosidasas/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/química , Simulación por ComputadorRESUMEN
Aleurites moluccanus (candlenut) and Bertholletia excelsa (Brazil nut) are marketed as dietary supplements for weight loss. These dietary supplements have been found to sometimes be adulterated with toxic nuts/seeds from Cascabela thevetia, commonly known as yellow oleander or lucky nut. This study emphasizes the key identification parameters to differentiate the genuine and adulterated nuts. Samples were obtained from authenticated sources of the nuts and from commercial sources of dietary supplements. This study examined 38 samples, including voucher and commercial samples. All eight commercial candlenut dietary supplement samples were adulterated. Additionally, two samples sold as Brazil nuts were also found to be adulterated. Other nuts were screened for the presence of Cardiac Glycosides, but none were found to be positive. The presence of yellow oleander was confirmed in all commercial dietary supplement samples marketed as candlenut as well as in commercial samples of Brazil nut. This study provides simple key identification characters using micro-morphology and histochemical localization of cardiac glycosides in the commercial nuts, HPTLC fingerprints, and LC-DAD-Q-ToF analytical parameters to detect and identify adulteration in commercial products.
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Bertholletia , Suplementos Dietéticos , Suplementos Dietéticos/análisis , Bertholletia/química , Contaminación de Alimentos/análisis , Cromatografía en Capa Delgada , Nueces/química , Cromatografía Líquida de Alta Presión , Pérdida de Peso , MicroscopíaRESUMEN
Anemoside B4 (AB4), a triterpenoidal saponin from Pulsatilla chinensis, shows significant anti-inflammatory activity, and may be used for treating inflammatory bowel disease (IBD). Nevertheless, its application is limited due to its high molecular weight and pronounced water solubility. To discover new effective agents for treating IBD, we synthesized 28 AB4 derivatives and evaluated their cytotoxic and anti-inflammatory activities in vitro. Among them, A3-6 exhibited significantly superior anti-inflammatory activity compared to AB4. It showed a significant improvement in the symptoms of DSS-induced colitis in mice, with a notably lower oral effective dose compared to AB4. Furthermore, we discovered that A3-6 bound with pyruvate carboxylase (PC), then inhibited PC activity, reprogramming macrophage function, and alleviated colitis. These findings indicate that A3-6 is a promising therapeutic candidate for colitis, and PC may be a potential new target for treating colitis.
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Antiinflamatorios , Colitis , Piruvato Carboxilasa , Saponinas , Animales , Humanos , Ratones , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Antiinflamatorios/química , Antiinflamatorios/síntesis química , Colitis/tratamiento farmacológico , Colitis/inducido químicamente , Sulfato de Dextran , Descubrimiento de Drogas , Ratones Endogámicos C57BL , Piruvato Carboxilasa/antagonistas & inhibidores , Piruvato Carboxilasa/metabolismo , Células RAW 264.7 , Saponinas/farmacología , Saponinas/química , Saponinas/uso terapéutico , Saponinas/síntesis química , Relación Estructura-ActividadRESUMEN
One undescribed compound, striasinol (1), and twelve previously described compounds were isolated from the aerial parts of Striga asiatica. Structure elucidation of isolated compounds was achieved by the interpretation of 1D and 2D NMR and HRESIMS data. The absolute configuration (1S,5S) of 1 was ascertained based on GIAO NMR calculations, DP4+ probability analysis, and a comparison of the experimental and calculated specific rotation values. The isolated compounds were evaluated for their antimalarial action, and none was found to be effective against the chloroquine-sensitive (D6) or chloroquine-resistant (W2) strains of Plasmodium falciparum. The isolates were found non-toxic to the Vero cell line as well. Subsequent testing of these metabolites for antimicrobial activities against various bacterial and fungal strains (up to 20 µg/mL), revealed that compounds 6 (chryseriol) and 7 (apigenin) showed a reasonable activity towards methicillin-resistant Staphylococcus aureus ATCC 1708 (MRSA), with IC50 values of 5.81 and 3.60 µg/mL, respectively.
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Atraphaxis pyrifolia is a native species of Central Asia, known for curing several disorders. The species has little knowledges about its chemical composition and any information about its morphological characteristics despite its importance in traditional Asian medicine. This is one of the first approaches to the phytochemical and morphological characterization of this species. Micro-morphology was performed on the stem, and leaf parts of this plant to profile the morpho-anatomical characters using brightfield, fluorescence, polarized and scanning electron microscopy. Leaves were extracted with hexane and methanol. The hexane extract was analyzed using GC-MS analysis revealing the major presence of γ-sitosterol and nonacosane. The methanolic extract was submitted to Vacuum Liquid Chromatography and Sephadex LH-20. HPTLC, HR-ESI-MS and NMR techniques were used to identify the main compounds. Four glycosylated flavonoids were isolated: 8-O-acetyl-7-O-methyl-3-O-α-l-rhamnopyranosylgossypetin (Compound 1), and 7-O-methyl-3-O-α-l-rhamnopyranosylgossypetin (Compound 3), and two other compounds reported for the first time in the literature (Compounds 2 and 4). The findings presented herein furnish pertinent information essential for the identification and authentication of this medicinal plant. Such insights are invaluable for facilitating robust quality control measures and serve as a foundational framework for subsequent endeavours in metabolic, pharmacological, and taxonomical analyses.
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Hexanos , Extractos Vegetales , Extractos Vegetales/química , Kazajstán , Fitoquímicos/farmacología , MetanolRESUMEN
The purity, content, and structure of the polysaccharides prepared from a specific medicinal plant are the fundamental basis to interpret the observed biological activities. An ultrafiltration-based method has been developed for rapid preparation of total and fractional polysaccharides from Radix Astragali in high yield and purity. This method involves extraction of plant material by hot water, treatment with Sevag reagent, and ultrafiltration using molecular weight cutoff concentrators. The prepared polysaccharides were assessed by 1H NMR spectroscopy, providing general purity, fingerprinting, and structural information. This method may be used to efficiently screen polysaccharides in plants.
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Astragalus propinquus , Medicamentos Herbarios Chinos , Protones , Espectroscopía de Resonancia Magnética , PolisacáridosRESUMEN
The inflorescences of Pseudognaphalium liebmannii are used as folk medicine to treat various respiratory diseases. In this work, we report the isolation of seven known flavones: 5-hydroxy-3,7-dimethoxyflavone 1, 5,8-dihydroxy-3,7-dimethoxyflavone 2, 5,7-dihydroxy-3,8-dimethoxyflavone 3 (gnaphaliin A), 3,5-dihydroxy-7,8-dimethoxyflavone 4 (gnaphaliin B), 3,5-dihydroxy-6,7,8-trimethoxyflavone 5, 3,5,7-trimethoxyflavone 6 and 3-O-methylquercetin 7. All these flavones except 1 and 6 showed a relaxant effect on guinea pig tracheal preparation with EC50 between 69.91 ± 15.32 and 118.72 ± 7.06 µM. Aminophylline (EC50 = 122.03 ± 7.05 µM) was used as a relaxant reference drug. The active flavones shifted the concentration-response curves of forskolin and nitroprusside leftward, and significantly reduced the EC50 values of these drugs. Furthermore, these flavones dose-dependently inhibited phosphodiesterase (PDE) in an in vitro assay. This reveals that the inflorescences of P. liebmannii contain several flavones with relaxant effect on airway smooth muscle and with PDEs inhibition that contribute to supporting the anti-asthmatic traditional use.
RESUMEN
The flowers of Quararibea funebris are used to make a traditional drink called tejate, to which they add aroma, flavor and consistency. The study aims to profile the morphoanatomy of the floral parts of Q.â funebris and analyze the changes in its volatile chemical composition during the drying process from 0 to 180â days by HS-SPME-GC-MS. The calyx, corolla, androecium, and gynoecium have distinct characteristics, such as non-glandular fused stellate trichomes, calcium oxalate crystals, and large secretory ducts. Histochemical localization reveals the presence of mucilage and total lipids in all parts of the flower. The chemical analysis of the essential oil, extracted from the flowers, showed that transfarnesol and geraniol were the most abundant compounds, with a yield of 0.04 %. HS-SPME analysis indicated that fresh flowers had a more complex composition than dried ones. In total, 31â components were identified. Nonanal and geranyl acetone were found to be distinctive components of dried flowers. Microscopic examination helps in identifying and authenticating raw materials and also reveals the presence of secretory ducts in all floral parts, which is a distinctive feature. The chemical profile of volatiles provides an important parameter for the evaluation of the quality of Rosita de Cacao raw materials.