RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Panax notoginseng flowers, which are the buds of the traditional Chinese medicinal herb Sanqi, are widely used in China for their cough-ameliorating properties, with demonstrated therapeutic effects in the treatment of both acute and chronic coughs. However, both the antitussive mechanism and active compound basis of P. notoginseng flowers remain poorly understood. AIM OF THE STUDY: We investigated the antitussive effects of P. notoginseng flowers, identified the bioactive constituents responsible for alleviating cough symptoms, and elucidated the underlying pharmacological mechanisms. MATERIALS AND METHODS: We analyzed the major chemical constituents of aqueous extracts of P. notoginseng flowers using liquid chromatography-mass spectrometry and quantitatively analyzed the key component, 20S-ginsenoside Rh2, using high-performance liquid chromatography. Using a cough reflex model in healthy mice and an ovalbumin-induced, highly sensitive guinea pig cough model, we verified the suppressive effects of P. notoginseng flowers and their saponin constituents on coughing. Furthermore, we explored the mechanisms of action of the key ion channels, NaV1.7 and TRPV1, using whole-cell patch-clamp techniques and molecular docking. Finally, the therapeutic mechanisms of P. notoginseng flowers on pathological cough were revealed using hematoxylin and eosin staining, immunohistochemistry, and western blotting. RESULTS: The active components of P. notoginseng flowers were primarily protopanaxadiol-type saponins, among which 20S-ginsenoside Rh2 had the highest content (51.46 mg/g). In the mouse model, P. notoginseng flowers exhibited antitussive effects comparable to those of pentoxyverine citrate. Although its main saponin component, 20S-ginsenoside Rh2, showed slightly weaker effects, it still demonstrated concentration-dependent inhibition of channel activity. The whole-cell patch-clamp technique and virtual molecular docking showed that Rh2 might exert its effects by directly binding to the NaV1.7 and TRPV1 channels. In the guinea pig model, P. notoginseng flowers and their saponin components not only reduced cough frequency and prolonged the latency period before cough onset, but also significantly inhibited tracheal and pulmonary inflammation and the overexpression of TRPV1. CONCLUSIONS: 20S-Ginsenoside Rh2, the major bioactive saponin in P. notoginseng flowers, exhibits potent antitussive effects. The potential mechanism of action of 20S-Ginsenoside Rh2 in the treatment of cough may involve inhibiting NaV1.7 and TRPV1 channel currents through direct binding to core protein active sites and downregulating TRPV1 expression.

Asunto(s)

Antitusígenos , Tos , Regulación hacia Abajo , Flores , Ginsenósidos , Canal de Sodio Activado por Voltaje NAV1.7 , Panax notoginseng , Canales Catiónicos TRPV , Animales , Canales Catiónicos TRPV/metabolismo , Cobayas , Flores/química , Tos/tratamiento farmacológico , Ginsenósidos/farmacología , Antitusígenos/farmacología , Masculino , Ratones , Panax notoginseng/química , Regulación hacia Abajo/efectos de los fármacos , Humanos , Canal de Sodio Activado por Voltaje NAV1.7/metabolismo , Canal de Sodio Activado por Voltaje NAV1.7/efectos de los fármacos , Células HEK293 , Simulación del Acoplamiento Molecular , Cricetulus , Modelos Animales de Enfermedad , Células CHO , Saponinas/farmacología , Ovalbúmina

RESUMEN

Australian honey samples from four botanical genera (Lophostemon, Eucalyptus, Macadamia and Corymbia) were investigated for their phenolic content. An improved phenolic extraction and high-performance liquid chromatography-diode array detection (HPLC-DAD) analysis method allowed for the rapid and reliable identification of phenolic compounds. A concentrated liquid-liquid extraction method with an acidified aqueous solution and acetonitrile was optimised to isolate phenolic compounds from the honey matrix. The concentrated extraction method improved sensitivity and permitted the identification of phenolics present at low concentrations (LOD: 0.012-0.25 mg/kg and LOQ: 0.040-2.99 mg/kg). The optimised HPLC-DAD chromatographic conditions gave stable retention times, improved peak separation and allowed for the inexpensive detection of each of the 109 phenolic compounds at their maximum absorbance wavelength. Out of the 109 phenolic compounds included in this study, 49 were identified in the Australian honeys tested. Furthermore, 25 of the 49 compounds were determined to be markers specific to honey floral origin.

Asunto(s)

Eucalyptus , Miel , Fenoles , Miel/análisis , Cromatografía Líquida de Alta Presión , Fenoles/análisis , Fenoles/química , Eucalyptus/química , Australia , Flores/química

RESUMEN

The flowers and stems of Rhubarb (Rheum ribes L.) are known to contain effective antioxidant compounds that have potential antidiarrheal properties in traditional medicine. This study was conducted to screen various genotypes of Rhubarb for their phytochemical and antioxidant activity and optimize the extraction parameters using the response surface methodology (RSM). The study found high diversity among the different genotypes (G1-G13) in terms of their flowers and stems. The total phenolic content (TPC) in the flowers of R. ribes varied significantly, showing values between 9.80 and 81.53 mg GAE g-1 DW. In the stems, TPC ranged from 2.87 to 16.33 mg GAE g-1 DW. Similarly, the total flavonoid content (TFC) in the flowers ranged from 0.33 to 1.32 mg Qu g-1 DW, while in the stems, it was between 0.05 and 0.38 mg Qu g-1 DW. The antioxidant activity, indicated as µmol Fe2+ g-1 DW, varied from 7.42 to 59.87 in the flowers and from 0.14 to 15.99 in the stems. Hierarchical cluster analysis (HCA) identified five distinct clusters among the collected genotypes. Subsequent analysis of variance and principal components analysis (PCA) revealed that the flowers of G8 (G8F) from Tehran to Lavasan exhibited the highest total phenolic content (TPC), total flavonoid content (TFC), and antioxidant activity (FRAP). Given these findings, G8F was chosen for further optimization in the study. The RSM was designed based on a Box-Behnken design (BBD) to determine the optimal extraction conditions, including extraction temperature (30-80 °C), extraction time (5-15 min), and ethanol concentration (25-75%, ethanol to water, v/v). The responses measured were total phenolic content (TPC), total flavonoid content (TFC), total anthocyanin content (TAC), 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging, and Ferric reducing/antioxidant power (FRAP) assays. The optimal extraction conditions for all responses or desirability indices were X1: 80 °C, X2: 15 min, and X3: 53.14%, which resulted in TPC (99.32 mg GAE.g-1 DW), TFC (3.00 mg Qu.g-1 DW), TAC (1.12 mg cyanidin-3-glucoside (Cy-g) g-1 DW), FRAP (110.22 µmol Fe+2/g DW), and DPPHsc (88.20%). The R2 values (0.91-0.99) indicated that the RSM models were acceptable.

Asunto(s)

Antioxidantes , Genotipo , Fenoles , Extractos Vegetales , Rheum , Antioxidantes/química , Antioxidantes/análisis , Rheum/química , Fenoles/química , Fenoles/análisis , Extractos Vegetales/química , Flavonoides/análisis , Flavonoides/química , Flores/química , Tallos de la Planta/química

RESUMEN

The goal of preparative chromatography is to isolate suitable amounts of compound(s) at the required purity in the most cost-effective way. This study analyses the power of High-performance thin-layer chromatography (HPTLC) guided preparative flash chromatography to separate and isolate bioactive compounds from an olive flower extract for their further characterisation via spectroscopy. The structure and purity of isolated bioactive compounds were assessed using Fourier-transform infrared (FTIR) and nuclear magnetic resonance (NMR) spectroscopy. Flash chromatography of the olive flower extract successfully isolated pure oleanolic and maslinic acids. Moreover, the flash chromatography of the extract allowed isolation and phytochemical analysis of the most lipophilic fraction of the extract, which was found to contain n-eicosane and n-(Z)-eicos-5-ene, that has not been isolated previously with preparative TLC.

Asunto(s)

Flores , Espectroscopía de Resonancia Magnética , Olea , Extractos Vegetales , Flores/química , Cromatografía en Capa Delgada/métodos , Olea/química , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Espectroscopía Infrarroja por Transformada de Fourier , Triterpenos/análisis , Triterpenos/aislamiento & purificación , Triterpenos/química , Ácido Oleanólico/aislamiento & purificación , Ácido Oleanólico/análisis , Ácido Oleanólico/química , Ácido Oleanólico/análogos & derivados , Cromatografía Líquida de Alta Presión/métodos

RESUMEN

In this study, biological synthesis of silver nanoparticles (AgNPs) using Senna auriculata flower extract for antibacterial activities was reported. The silver spectra compared to the plant extract show a rightward shift in AgNP peaks, indicating successful nanoparticle formation. The absorption band at 302 nm and the disappearance or shift of other peaks further confirm the synthesis. X-ray diffraction (XRD) analysis reveals that the AgNPs synthesized with S. auriculata extract have an average crystallite size of 25 nm. Transmission electron microscopy (TEM) results exhibited a polydispersed, spherical shape with sizes ranging from 70 nm, in clear contrast to the electron microscope image that showed their spherical shape. When examining the selected area electron diffraction (SAED) image, a specific set of lattice planes was correlated with a specific spot. A histogram of AgNP particle size distribution can be seen. AgNPs were tested against four different strains of bacteria for their antibacterial effectiveness, including gram negative bacteria (Escherichia coli, Klebsiella pneumoniae, and Staphylococcus aureus), as well as gram positive bacteria (S. aureus, d. Bacillus subtilis), at various concentrations of AgNP. The results of in vitro experiments indicate that AgNPs containing S. auriculata flowers inhibit amylase well. At two concentrations, ~16.03% and ~70.99%, AgNPs inhibit the reaction at low and high concentrations, respectively.

Asunto(s)

Antibacterianos , Flores , Nanopartículas del Metal , Pruebas de Sensibilidad Microbiana , Extractos Vegetales , Plata , Plata/química , Plata/farmacología , Nanopartículas del Metal/química , Antibacterianos/farmacología , Antibacterianos/química , Antibacterianos/síntesis química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Flores/química , Tamaño de la Partícula , Difracción de Rayos X

RESUMEN

Melanin naturally exists in organisms and is synthetized by tyrosinase (TYR); however, its over-production may lead to aberrant pigmentation and skin conditions. Loquat (Eriobotrya japonica (Thunb.) Lindl.) flowers contain a variety of bioactive compounds, while studies on their suppressive capabilities against melanin synthesis are limited. Loquat flower isolate product (LFP) was obtained by ethanol extraction and resin purification, and its inhibitory efficiency against TYR activity was investigated by enzyme kinetics and multiple spectroscopy analyses. In addition, the impact of LFP on melanin synthesis-related proteins' expression in mouse melanoma B16 cells was analyzed using Western blotting. HPLC-MS/MS analysis indicated that LFP was composed of 137 compounds, of which 12 compounds, including flavonoids (quercetin, isorhamnoin, p-coumaric acid, etc.) and cinnamic acid and its derivatives, as well as benzene and its derivatives, might have TYR inhibitory activities. LFP inhibited TYR activity in a concentration-dependent manner with its IC50 value being 2.8 mg/mL. The inhibition was an anti-competitive one through altering the enzyme's conformation rather than chelating copper ions at the active center. LFP reduced the expression of TYR, tyrosinase-related protein (TRP) 1, and TRP2 in melanoma B16 cells, hence inhibiting the synthesis of melanin. The research suggested that LFP had the potential to reduce the risks of hyperpigmentation caused by tyrosinase and provided a foundation for the utilization of loquat flower as a natural resource in the development of beauty and aging-related functional products.

Asunto(s)

Eriobotrya , Flores , Melaninas , Melanoma Experimental , Monofenol Monooxigenasa , Extractos Vegetales , Animales , Monofenol Monooxigenasa/metabolismo , Monofenol Monooxigenasa/antagonistas & inhibidores , Ratones , Melaninas/biosíntesis , Melaninas/metabolismo , Flores/química , Melanoma Experimental/metabolismo , Melanoma Experimental/patología , Eriobotrya/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Línea Celular Tumoral , Inhibidores Enzimáticos/farmacología , Inhibidores Enzimáticos/química

RESUMEN

Matricaria chamomilla (Asteraceae), commonly known as chamomile can tolerate freezing temperatures and grows in many soil types. This plant is found on all continents and has significant medicinal value. There are more than 120 chemicals detected in chamomile flowers, with the majority found in the essential oil. In this study, M. chamomilla was given the NaCl stress of 0 mM, 1 mM, 100 mM, and 150 mM concentrations This study was the first to assess the efficacy of German chamomile upon exposure to salt stress hence plant particles that had been dried and powdered were analyzed using, phytochemical tests, Fourier Transform Infrared and UV-Vis spectroscopy, thin layer chromatography, fluorescence recovery after photobleaching assay, antibacterial and antioxidant activity. The characterization and results of these activities show amazing results which enhance their antibacterial property with an increased zone of inhibition when the samples of salt stress of the above-given concentrations were compared to the control samples. More graph analysis indicates an effective impact of salt stress on the phytoconstituents of M. chamomilla. Other than that, there was a clear flower induction upon salt stress, as a variety of compounds are regarded as essential to the biological functions of chamomile flowers according to the phytoconstituent screening which can be further used in the cosmetic industry, pharmaceutical industry, and all other fields as well for various application as a nano-drug or bio-drug. Due to this, this plant became essential for plant biotechnology research.

Asunto(s)

Antibacterianos , Antioxidantes , Matricaria , Matricaria/química , Antioxidantes/farmacología , Antioxidantes/química , Antibacterianos/farmacología , Antibacterianos/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Estrés Salino , Espectroscopía Infrarroja por Transformada de Fourier , Fitoquímicos/química , Fitoquímicos/farmacología , Flores/química , Cloruro de Sodio

RESUMEN

Phytochemical study on the flowers of Hypericum formosanum Maxim. (Hypericaceae) led to the isolation of formohyperins G-L (1-6), whose structures were assigned by detailed spectroscopic analysis. Formohyperins G-L (1-6) are new benzoylphloroglucinols substituted by a C10 unit, a prenyl group, and a methyl group. Formohyperins G-J (1-4) possess a 6/6/6-tricyclic structure, while formohyperins K (5) and L (6) have a unique 6/6/5/4-tetracyclic structure consisting of cyclohexadienone, dihydropyrane, cyclopentane, and cyclobutane rings. The absolute configurations of 1-6 were deduced by analysis of the ECD spectra. Formohyperins G-J (1-4) and L (6) were found to show potent inhibitory activities against IL-1ß release from LPS-treated murine microglial cells with EC50 values of 5.0, 10.9, 6.3, 10.8, and 13.7 µM, respectively, without cytotoxicity. 6-O-Methylformohyperins G (1a) and I (3a) also exhibited the inhibitory activities with EC50 values of 4.7 and 2.7 µM, respectively, although they were cytotoxic against microglial cells.

Asunto(s)

Flores , Hypericum , Floroglucinol , Hypericum/química , Animales , Floroglucinol/química , Floroglucinol/farmacología , Flores/química , Ratones , Estructura Molecular , Interleucina-1beta/metabolismo , Microglía/efectos de los fármacos , Microglía/metabolismo , Prenilación , Extractos Vegetales/química , Extractos Vegetales/farmacología , Lipopolisacáridos/farmacología , Línea Celular

RESUMEN

German chamomile (Matricaria chamomilla L.) is an essential oil- containing medicinal plant used worldwide. The aim of this study was to gain knowledge of the phytochemical composition and the analgesic and soporific activity of Matricaria chamomilla L. (German chamomile) flower extract and its amino acid preparations, to predict the mechanisms of their effects by molecular docking and to develop aqueous printing gels and novel 3D-printed oral dosage forms for the flower extracts. In total, 22 polyphenolic compounds and 14 amino acids were identified and quantified in the M. chamomilla extracts. In vivo animal studies with rodents showed that the oral administration of such extracts revealed the potential for treating of sleep disorders and diseases accompanied by pain. Amino acids were found to potentiate these effects. Glycine enhanced the analgesic activity the most, while lysine and ß-alanine improved the soporific activity. The molecular docking analysis revealed a high probability of γ-aminobutyric acid type A (GABAA) and N-methyl-D-aspartate (NMDA) receptor antagonism and 5-lipoxygenase (LOX-5) inhibition by the extracts. A polyethylene oxide (PEO)-based gel composition with the M. chamomilla extracts was proposed for preparing a novel 3D-printed dosage form for oral administration. These 3D-printed extract preparations can be used, for example, in dietary supplement applications.

Asunto(s)

Aminoácidos , Flores , Matricaria , Simulación del Acoplamiento Molecular , Fitoquímicos , Extractos Vegetales , Impresión Tridimensional , Extractos Vegetales/química , Extractos Vegetales/farmacología , Animales , Matricaria/química , Aminoácidos/química , Flores/química , Fitoquímicos/química , Fitoquímicos/farmacología , Ratas , Analgésicos/química , Analgésicos/farmacología , Masculino , Ratones

RESUMEN

The prevention and treatment of gastrointestinal mucosal injury caused by a plateau hypoxic environment is a clinical conundrum due to the unclear mechanism of this syndrome; however, oxidative stress and microbiota dysbiosis may be involved. The Robinia pseudoacacia L. flower, homologous to a functional food, exhibits various pharmacological effects, such as antioxidant, antibacterial, and hemostatic activities. An increasing number of studies have revealed that plant exosome-like nanoparticles (PELNs) can improve the intestinal microbiota and exert antioxidant effects. In this study, the oral administration of Robinia pseudoacacia L. flower exosome-like nanoparticles (RFELNs) significantly ameliorated hypoxia-induced gastric and small intestinal mucosal injury in mice by downregulating hypoxia-inducible factor-1α (HIF-1α) and HIF-2α expression and inhibiting hypoxia-mediated ferroptosis. In addition, oral RFELNs partially improved hypoxia-induced microbial and metabolic disorders of the stomach and small intestine. Notably, RFELNs displayed specific targeting to the gastrointestinal tract. In vitro experiments using gastric and small intestinal epithelial cell lines showed that cell death caused by elevated HIF-1α and HIF-2α under 1% O2 mainly occurred via ferroptosis. RFELNs obviously inhibited HIF-1α and HIF-2α expression and downregulated the expression of NOX4 and ALOX5, which drive reactive oxygen species production and lipid peroxidation, respectively, suppressing ferroptosis under hypoxia. In conclusion, our findings underscore the potential of oral RFELNs as novel, naturally derived agents targeting the gastrointestinal tract, providing a promising therapeutic approach for hypoxia-induced gastric and small intestinal mucosal ferroptosis.

Asunto(s)

Factores de Transcripción con Motivo Hélice-Asa-Hélice Básico , Exosomas , Ferroptosis , Flores , Mucosa Gástrica , Subunidad alfa del Factor 1 Inducible por Hipoxia , Mucosa Intestinal , Intestino Delgado , Peroxidación de Lípido , Nanopartículas , Animales , Ferroptosis/efectos de los fármacos , Subunidad alfa del Factor 1 Inducible por Hipoxia/metabolismo , Ratones , Exosomas/metabolismo , Exosomas/efectos de los fármacos , Peroxidación de Lípido/efectos de los fármacos , Intestino Delgado/efectos de los fármacos , Intestino Delgado/metabolismo , Intestino Delgado/patología , Administración Oral , Mucosa Intestinal/efectos de los fármacos , Mucosa Intestinal/metabolismo , Masculino , Factores de Transcripción con Motivo Hélice-Asa-Hélice Básico/metabolismo , Mucosa Gástrica/efectos de los fármacos , Mucosa Gástrica/metabolismo , Flores/química , Nanopartículas/química , Hipoxia/tratamiento farmacológico , Hipoxia/metabolismo , Humanos , Ratones Endogámicos C57BL

RESUMEN

Wound healing is a complex process orchestrated by interactions between a variety of cell types, including keratinocytes, fibroblasts, endothelial cells, inflammatory cells, and bioactive factors such as extracellular matrix (ECM) components, growth factors, and cytokines. Chronic wounds exhibit delayed proliferative phase initiation, reduced angiogenesis, impaired ECM synthesis, and persistent inflammatory response. Chronic wounds are one of the main challenges to the healthcare system worldwide, with a high cost for medical services. Hence, investigation of new approaches to accelerate wound healing is essential. Phytomedicines are considered as potential agents for improving the wound healing by accelerating epithelization, collagen synthesis, and angiogenesis. These natural compounds have various advantages including availability, ease of application, and high effectiveness in wound managment. This study aimed to investigate the biological effects of saffron or Crocus sativus L. (C. sativus) petal extract on cell survival, migration, and angiogenesis using MTT, scratch and in vitro tube formation assays. Moreover, the expression of collagen type I alpha 1 (COL1A1) and vascular endothelial growth factor (VEGF) were evaluated in human dermal fibroblasts (HDF)s and human umbilical vein endothelial cells (HUVEC)s, respectively. The effect of the C. sativus extract on the skin of diabetic mice was also monitored. The results showed that C. sativus petal extract promoted the viability and migration of HDFs and HUVECs. Moreover, C. sativus petal extract enhanced the formation of tube-like structures by HUVECs cultured on the Matrigel basement membrane matrix, indicating its potential to stimulate angiogenesis. Gene expression studies have shown the the C. sativus extract increases wound healing by upregulation of COL1A1 and VEGF, which are crucial factors involved in collagen deposition, epithelialization, and angiogenesis. Histological analysis revealed that C. sativus petal extract enhanced vascularity and increased the number of fibroblasts and collagen synthesis, ultimately accelerating wound closure compared to wounds treated with eucerin and commercial ointment in diabetic mice. Therefore, C. sativus petal extract has potential as a herbal treatment to improve the healing of diabetic wounds.

Asunto(s)

Crocus , Fibroblastos , Células Endoteliales de la Vena Umbilical Humana , Extractos Vegetales , Factor A de Crecimiento Endotelial Vascular , Cicatrización de Heridas , Cicatrización de Heridas/efectos de los fármacos , Crocus/química , Animales , Humanos , Extractos Vegetales/farmacología , Células Endoteliales de la Vena Umbilical Humana/efectos de los fármacos , Ratones , Fibroblastos/efectos de los fármacos , Fibroblastos/metabolismo , Factor A de Crecimiento Endotelial Vascular/metabolismo , Factor A de Crecimiento Endotelial Vascular/genética , Diabetes Mellitus Experimental/tratamiento farmacológico , Colágeno Tipo I/metabolismo , Colágeno Tipo I/genética , Movimiento Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Cadena alfa 1 del Colágeno Tipo I , Flores/química , Neovascularización Fisiológica/efectos de los fármacos , Masculino

RESUMEN

The hibiscus calyx contains 0.3-2.4% total anthocyanins, and is a promising source for naturally red food colorants. In this study, commercially available hibiscus calyces were subjected to ethanolic-aqueous extraction and chromatographic enrichment with the XAD-7HP resin, to create scalable, high-anthocyanin and low-acidity natural food colorants. Anthocyanins, organic and phenolic acids were monitored after each step using UHPLC-DAD and UHPLC-QQQ/MS. 75.67% total anthocyanins were recovered from calyces after double extractions, and the content increased by 8.50-14.90 times after the column enrichment, reaching 14.51-31.90% (by dry weight) in the final product. Chromatographic fractionation was also shown to effectively increase the total phenolic acids by 11.01-16.22 times, and remove an average of 98.58% of the total organic acids. High intensity redness at pH 2.5-3.5 indicated that the final product may be a promising, versatile natural food and beverage colorant in low pH products.

Asunto(s)

Antocianinas , Colorantes de Alimentos , Hibiscus , Extractos Vegetales , Hibiscus/química , Antocianinas/química , Antocianinas/análisis , Colorantes de Alimentos/química , Colorantes de Alimentos/análisis , Colorantes de Alimentos/aislamiento & purificación , Cromatografía Líquida de Alta Presión , Extractos Vegetales/química , Flores/química

RESUMEN

Saussurea laniceps is a traditional medicinal herb. In our previous study, a pectin polysaccharide, SLP-4, was isolated from the petals of S. laniceps. In this study, the immunomodulatory activity of SLP-4 was studied by analyzing its effects on macrophage (RAW 264.7 cells) polarization. The immunomodulatory activity assays indicated that SLP-4 could significantly enhance the pinocytic and phagocytic capacity and promote the expression and secretion of cytotoxic molecules (nitric oxide, increased by 6.4 times when the SLP-4 concentration was 800 µg/mL) and cytokines (tumor necrosis factor-α and interleukin-6 increased by 7.7 and 11.9 times, respectively) in original macrophage. The possible mechanism could be attributed to the activation of the mitogen-activated protein kinase and nuclear factor-κB signaling pathways through Toll-like receptors 2 and 4. Moreover, SLP-4 significantly induced M1 polarization of original macrophages and transferred macrophages from M2 to M1, but had little effect on the conversion of M1 macrophages into M2 phenotype. Overall, these results demonstrate the potential of SLP-4 as an attractive immunomodulating functional supplement.

Asunto(s)

Macrófagos , Óxido Nítrico , Pectinas , Fagocitosis , Saussurea , Animales , Ratones , Pectinas/farmacología , Pectinas/química , Pectinas/aislamiento & purificación , Células RAW 264.7 , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Macrófagos/inmunología , Saussurea/química , Fagocitosis/efectos de los fármacos , Óxido Nítrico/metabolismo , FN-kappa B/metabolismo , Citocinas/metabolismo , Transducción de Señal/efectos de los fármacos , Receptor Toll-Like 2/metabolismo , Flores/química , Receptor Toll-Like 4/metabolismo , Activación de Macrófagos/efectos de los fármacos , Pinocitosis/efectos de los fármacos , Polisacáridos/farmacología , Polisacáridos/química , Polisacáridos/aislamiento & purificación , Interleucina-6/metabolismo , Agentes Inmunomoduladores/farmacología , Agentes Inmunomoduladores/química , Agentes Inmunomoduladores/aislamiento & purificación , Factor de Necrosis Tumoral alfa/metabolismo

RESUMEN

A high performance liquid chromatography-ultraviolet-visible detector-electrospray ionization-ion trap-time-of-flight-mass spectrometry-total antioxidant capacity determination (HPLC-UVD-ESI-IT-TOF-MS-TACD) new online technique was developed for efficient screening of potential antioxidant active components in Prunus persica flowers (PPF) from 4 origins. Through this online system, 46 compounds were initially identified, while 20 compounds with DPPH binding activity and 21 compounds with FRAP binding activity were detected. The antioxidant activities of 9 compounds obtained from the screening were then validated in DNA oxidative damage protection study. The results showed that this online system can cope well with the complexity of the samples. This also provides technical basis for rapid screening of antioxidant resources of PPF. In short, this study made the chemical composition of PPF more abundant and its potential antioxidant active compounds more explicit, which provided new ideas for the detection and development of natural antioxidants and provided scientific basis for PPF as functional food.

Asunto(s)

Antioxidantes , Daño del ADN , Flores , Prunus persica , Antioxidantes/farmacología , Antioxidantes/química , Antioxidantes/análisis , Flores/química , Daño del ADN/efectos de los fármacos , Prunus persica/química , Cromatografía Líquida de Alta Presión , Espectrometría de Masa por Ionización de Electrospray , Compuestos de Bifenilo/antagonistas & inhibidores , Compuestos de Bifenilo/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Estrés Oxidativo/efectos de los fármacos , Picratos/antagonistas & inhibidores , Picratos/química

RESUMEN

BACKGROUND: Chrysanthemi Flos as a medicine food homology species is widely used in the prevention and treatment of diseases, whereas comprehensive research of its active compounds related to multi-pharmacological effects remains limited. This study aimed to systematically explore the active compounds through artificial intelligence-based target prediction and activity evaluation. METHODS: The information on compounds in Chrysanthemi Flos was obtained from six cultivars containing Gongju, Chuju, Huaiju, Boju, Hangbaiju, and Fubaiju, using UPLC-Q-TOF/MS. The main differential metabolites in six cultivars were also screened through the PLS-DA model. Then the potential targets of differential compounds were predicted via the DrugBAN model. Enrichment and topological analysis of compound-target networks were performed to identify key pharmaceutical compounds. Subsequently, the pharmacological effects of predictively active compounds were confirmed in vitro. Based on the active compounds, the pharmacological activities of Chrysanthemi Flos from the six origins were also investigated and compared for the further evaluation of medicinal quality. RESULTS: A total of 155 secondary metabolites were obtained from Chrysanthemi Flos. Among them, 26 differential components were screened, and 9 key pharmacological compounds with 1141 targets were identified. Enrichment analysis indicated the main pharmacological effects of Chrysanthemi Flos related to inflammation, oxidative stress, and lipid metabolism. In addition, 9 key pharmaceutical compounds were evaluated in vitro experiments, indicating the significant therapeutic effect in regulating inflammation, oxidative stress, and lipid metabolism. CONCLUSION: This study successfully identified 9 key pharmaceutical compounds in Chrysanthemi Flos and predicted the pharmacodynamic advantages of six origins. The findings would provide improved guidance for the discovery of active constituents and the assessment of pharmacodynamic advantages of different geographical origins.

Asunto(s)

Inteligencia Artificial , Chrysanthemum , Medicamentos Herbarios Chinos , Flores , Chrysanthemum/química , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/farmacología , Flores/química , Humanos

RESUMEN

OBJECTIVE: This study investigates the biological activities of Rhododendron arboreum Sm from the eastern Himalayas, addressing a literature gap on its properties. It explores the plant's phytochemical, antioxidant, and medicinal characteristics. SIGNIFICANCE: Evaluating methanolic extracts of R. arboreum offers valuable insights into its bioactive potential. Comprehensive GC-MS analysis identified a diverse array of compounds, highlighting the plant's chemical composition. METHODS: Methanolic leaf and flower extracts underwent sequential extraction and phytochemical profiling using column chromatography, TLC, and GC-MS analysis. Spectral studies aided compound identification, and antioxidant activity was assessed via spectrophotometric assays. RESULTS: Column chromatography separated methanol leaf and flower extracts into 17 and 24 distinct fractions, respectively. TLC analysis showed specific Rf values for leaf (0.58, 0.65, 0.75, 0.8, 0.86, 0.9) and flower samples (0.91, 0.38, 0.48, 0.51, 0.56, 0.6, 0.65, 0.75, 0.85, 0.96). GC-MS analysis revealed a variety of organic functional groups, including aliphatic hydrocarbons, aromatic compounds, heterocyclic molecules, phenolic compounds, steroids, terpenoids, alcohols, esters, and other bioactive compounds. FTIR spectra identified functional groups such as hydroxyls, primary amines, alkanes, and alkynes. NMR data indicated a complex molecular composition with diverse proton environments. Leaf extracts demonstrated superior antioxidant activity compared to flower extracts in DPPH, ABTS, hydrogen peroxide scavenging, lipid peroxidation inhibition, and FRAP assays. CONCLUSION: The study identifies diverse phytochemicals in R.arboreum extracts and highlights their potential applications in pharmaceuticals, nutraceuticals, and functional foods, owing to the superior antioxidant activity of leaf extracts compared to flowers.

Asunto(s)

Antioxidantes , Flores , Cromatografía de Gases y Espectrometría de Masas , Fitoquímicos , Extractos Vegetales , Hojas de la Planta , Rhododendron , Rhododendron/química , Hojas de la Planta/química , Antioxidantes/farmacología , Antioxidantes/química , Antioxidantes/análisis , Flores/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Fitoquímicos/farmacología , Fitoquímicos/análisis , Fitoquímicos/química , Cromatografía de Gases y Espectrometría de Masas/métodos

RESUMEN

The occurrence of inflammation is closely related to the activation of the NLRP3 inflammasome. IL-1ß produced during the activation of the NLRP3 inflammasome has strong pro-inflammatory activity and can also promote the release of inflammatory factors by other immune cells, exacerbating inflammatory damage to tissues. Utilizing IL-1ß as the detection index to find small-molecule inhibitors targeting NLRP3 from natural products will benefit the search for drugs for inflammation-related diseases. During the exploration of anti-inflammatory active components derived from the flowers of Dolichos lablab L., an ingredient in traditional Chinese medicine with dual applications in both medicinal treatment and dietary consumption, fourteen compounds (1-14), including seven previously unreported ones, named flosdolilabnitrogenousols A-D (1-4) and flosdolilabsaponins A-C (5-7), were found. Their structures were established through extensive NMR spectra determination, HR-ESI-MS analysis, ECD calculations, and chemical reactions. Flosdolilabsaponin A (5) stands out as an exceptionally rare tetracyclic lactone oleane-type saponin. Additionally, the inhibitory activity on IL-1ß release of all compounds, without cytotoxicity, was evaluated using BMDMs stimulated with LPS/Nigericin. An Elisa assay revealed that compounds 1, 8, 9, and 11-14 exhibited significant inhibition of IL-1ß release at a concentration of 30 µM. Structure-activity relationships were also discussed. This study indicates that D. lablab flowers possess anti-inflammatory activity, which might exert its effect by suppressing the activation of the NLRP3 inflammasome.

Asunto(s)

Antiinflamatorios , Flores , Interleucina-1beta , Proteína con Dominio Pirina 3 de la Familia NLR , Interleucina-1beta/metabolismo , Interleucina-1beta/antagonistas & inhibidores , Flores/química , Antiinflamatorios/farmacología , Antiinflamatorios/química , Animales , Proteína con Dominio Pirina 3 de la Familia NLR/metabolismo , Proteína con Dominio Pirina 3 de la Familia NLR/antagonistas & inhibidores , Ratones , Extractos Vegetales/farmacología , Extractos Vegetales/química , Humanos , Estructura Molecular , Inflamasomas/metabolismo , Inflamasomas/antagonistas & inhibidores , Inflamasomas/efectos de los fármacos

RESUMEN

Daylily (Hemerocallis citrina) is a perennial herb of the genus Hemerocallis of Liliaceae. It is also an economically important crop and is widely cultivated. Daylily has nutritional, medicinal and ornamental values. The research literature shows that daylily is a high-quality food raw material rich in soluble sugars, ascorbic acid, flavonoids, dietary fiber, carotenoids, mineral elements, polyphenols and other nutrients, which are effective in clearing heat and diuresis, resolving bruises and stopping bleeding, strengthening the stomach and brain, and reducing serum cholesterol levels. This article reviews the main nutrients of daylily and summarizes the drying process of daylily. In addition, due to the existence of active ingredients, daylily also has a variety of biological activities that are beneficial to human health. This article also highlights the nutritional quality of daylily, the research progress of dried vegetable rehydration technology and dried daylily. In the end, the undeveloped molecular mechanism and functional research status of daylily worldwide are introduced in order to provide reference for the nutritional quality research and dried processing industry of daylily.

Asunto(s)

Valor Nutritivo , Humanos , Verduras/química , Flores/química

RESUMEN

Abelmoschus manihot (L.) Medic flower (AMf) exhibits both nutritional value and bioactivities such as antioxidative, anti-inflammatory, neuroprotective, cardioprotective, and hepatoprotective effects. The aim of this investigation was to examine the potential impact of three different solvent extracts of AMf: supercritical CO2 extraction extract, water extract, and ethanol extract (AME), on management of diabetes. All three extracts demonstrated significant inhibitory effects on α-glucosidase (IC50 = 157-261 µg/mL) and lipase (IC50 = 401-577 µg/mL) activities while enhancing the α-amylase activity (32.4-41.8 folds at 200 µg/mL). Moreover, all three extracts exhibited notable inhibition of the formation of advanced glycation end-products, including the Amadori products (inhibition rates = 15.7-36.6%) and the dicarbonyl compounds (inhibition rates = 18.6-28.3%). Among the three extracts, AME exhibited the most pronounced inhibitory effect. AME displayed substantial in vitro and intracellular antioxidative activity, and effectively reduced ROS production (135% at 500 µg/mL) in ß-cells under hyperglycemic (HG) conditions. AME also enhanced the activity and gene expression of antioxidant enzymes, which were markedly decreased in the HG-induced ß-cells. Furthermore, AME protected ß-cell viability and maintained normal insulin secretion under HG conditions, likely due to its ability to reduce oxidative stress within ß-cells. This study demonstrated the potential of AME in preventing and managing diabetes and its associated complications. Further in vivo research is necessary to thoroughly elucidate the preventive effects and their underlying mechanisms.

Asunto(s)

Abelmoschus , Flores , Hipoglucemiantes , Extractos Vegetales , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Flores/química , Abelmoschus/química , Hipoglucemiantes/farmacología , Hipoglucemiantes/uso terapéutico , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Animales , Ratas

RESUMEN

To explore the mutagenic effect of the space environment on Pueraria montana and select the elite germplasm with good growth conditions and high isoflavone content, this study observed the agronomic traits, determined the flower isoflavone content, and labeled amplified fragment length polymorphism(AFLP) fluorescent molecular markers of 79 P. montana plants exposed to space mutagenesis(SP1 group) and 10 control plants of P. montana(CK group). Excel 2019, SPSS 25.0, NTSYSpc-2.11F, and Popgen 32 were employed to analyze the genetic diversity and perform the cluster analysis. The results showed that the SP1 group presented changed leaf hairy attitude and flower structure and higher CV and H' of quantitative traits than the CK group. The cluster analysis screened out five plants in the SP1 group. Ten P. montana plants in the SP1 group had higher content of 6″-O-xylosyl-tectoridin and tectoridin in the flowers than the control group, with the total content of both exceeding 11%. After clustering, 9 plants in the SP1 group were separated. Nine pairs of polymorphic primers were screened out frrom 64 pairs of primers. A total of 1 620 polymorphic loci were detected, with the average percentage of polymorphic loci(PPL) of 83.33%. The average Nei's gene diversity index(H) and Shannon's information index(I) were 0.192 2 and 0.305 2, respectively. After clustering, 4 plants in the SP1 group were screened out. According to the above results, plants No. 30, No. 66, and No. 89 in the SP1 group were subjected to greater mutagenic effect by the space environment and presented better growth and higher flower isoflavone content. Moreover, plant No. 30 showed the flower structure variation and flower weight two times of that in the CK group. These plants can be used as key materials for the subsequent experiments.

Asunto(s)

Flores , Variación Genética , Pueraria , Pueraria/genética , Pueraria/química , Pueraria/crecimiento & desarrollo , Flores/genética , Flores/crecimiento & desarrollo , Flores/química , Isoflavonas , Mutagénesis , Análisis del Polimorfismo de Longitud de Fragmentos Amplificados