RESUMEN

Hepatic fibrosis (HF) is a process that occurs during the progression of several chronic liver diseases, for which there is a lack of effective treatment options. Carthamus tinctorius L. (CTL) is often used in Chinese or Mongolian medicine to treat liver diseases. However, its mechanism of action remains unclear. In the present study, CTL was used to treat rats with CCl4­induced HF. The histopathological, biochemical and HF markers of the livers of the rats were analyzed, and CTL­infused serum was used to treat hepatic stellate cells (HSCs) in order to detect the relevant markers of HSC activation. Protein expression pathways were detected both in vitro and in vivo. Histopathological results showed that CTL significantly improved CCl4­induced liver injury, reduced aspartate aminotransferase and alanine aminotransferase levels, promoted E­cadherin expression, and decreased α­smooth muscle actin (SMA), SOX9, collagen I and hydroxyproline expression. Moreover, CTL­infused serum was found to decrease α­SMA and collagen I expression in HSCs. Further studies showed that CTL inhibited the activity of the PI3K/Akt/mTOR pathway in the rat livers. Following the administration of the PI3K agonist 740Y­P to HSCs, the inhibitory effect of CTL on the PI3K/Akt//mTOR pathway was blocked. These results suggested that CTL can inhibit HF and HSC activation by inhibiting the PI3K/Akt/mTOR pathway.

Asunto(s)

Carthamus tinctorius , Células Estrelladas Hepáticas , Cirrosis Hepática , Fosfatidilinositol 3-Quinasas , Proteínas Proto-Oncogénicas c-akt , Transducción de Señal , Serina-Treonina Quinasas TOR , Animales , Células Estrelladas Hepáticas/metabolismo , Células Estrelladas Hepáticas/efectos de los fármacos , Serina-Treonina Quinasas TOR/metabolismo , Carthamus tinctorius/química , Proteínas Proto-Oncogénicas c-akt/metabolismo , Fosfatidilinositol 3-Quinasas/metabolismo , Cirrosis Hepática/metabolismo , Cirrosis Hepática/patología , Cirrosis Hepática/inducido químicamente , Cirrosis Hepática/tratamiento farmacológico , Transducción de Señal/efectos de los fármacos , Ratas , Masculino , Tetracloruro de Carbono , Ratas Sprague-Dawley , Extractos Vegetales/farmacología , Hígado/metabolismo , Hígado/patología , Hígado/efectos de los fármacos

RESUMEN

A two-year field trial was set up to investigate the effects of applying 3 tons ha-1 of wheat (3WB) and cotton biochar (3CB) alone or in combination with chemical nitrogen (N) and phosphorus (P) fertilizers on biochemical properties, yield and nutrient content of safflower under normal irrigation and water stress (irrigation cut-off at flowering stage) conditions. The total water applied in the chemical treatments [150 kg ha-1 N + 50 kg ha-1 P (100% of the recommended dose) and 112.5N + 37.5P (75% of the recommended dose)] under water stress, was significantly higher than other treatments. Application of 112.5N + 37.5P + 3CB increased RWC from 57.5 to 59.4% and the total chlorophyll content from 80.7 to 128.1%, compared to the control. The carotenoid content, catalase and peroxidase in 112.5N + 37.5P + 3CB were lower than chemical fertilizers. Under water stress, the seed yield of 112.5N + 37.5P + 3CB was 10.2-12.6% higher than 112.5N + 37.5P + 3WB. The higher chlorophyll content, RWC, remobilization efficiency and nutrient content in 112.5N + 37.5P + 3CB compared to other treatments was associated with seed yield enhancement. The findings indicate that the combination of CB with 75% recommended dosage of N and P, may be the optimal approach for enhancing safflower production under water stress conditions.

Asunto(s)

Carthamus tinctorius , Carbón Orgánico , Clorofila , Fertilizantes , Nutrientes , Carthamus tinctorius/metabolismo , Carthamus tinctorius/química , Carbón Orgánico/química , Carbón Orgánico/farmacología , Clorofila/metabolismo , Fertilizantes/análisis , Nutrientes/análisis , Nutrientes/metabolismo , Nitrógeno/metabolismo , Nitrógeno/análisis , Fósforo/análisis , Fósforo/metabolismo , Agua/química , Deshidratación , Carotenoides/metabolismo

RESUMEN

The aim of this study was to investigate the effect of varying concentrations of furcellaran (FUR) and safflower (Carthamus Tinctorius) oil on the functional properties of emulgels as potential carriers of bioactive substances. The textural, mechanical, thermal and structural properties of twenty different formulations were characterised. The pH stability and zeta-potential of the emulgels was also examined. It was found clear correlation between gelling agent and oil fraction content and investigated properties. The hardness, strength, thermal stability expressed as melting point of the investigated systems increased with increasing concentration of the furcellaran and decreasing proportion of safflower oil, which indicated a significant weakening of the structure as a result of the addition of the oil fraction. Stored under refrigeration, emulgels appeared to be relatively stable showing a slight decrease in pH values after 7 days. Swelling ratio (SW) of emulgels increased with increasing both, polysaccharide and oil content, in emulgels. Based on the microstructure analyses, it can also be concluded that only part of the added safflower oil chemically bound to the functional groups of the polysaccharide, while the vast majority of it was only physically immobilized in the furcellaran matrix. Colour of furcellaran - safflower oil emulsion gels depended largely on the amount of oil fraction. The presented research demonstrating the wide spectrum of functional properties of polysaccharide-oil systems is a first step to developing a carrier composition for lipophilic compounds at further stages of research.

Asunto(s)

Geles , Aceite de Cártamo , Aceite de Cártamo/química , Concentración de Iones de Hidrógeno , Geles/química , Temperatura , Carthamus tinctorius/química

RESUMEN

INTRODUCTION: Traditional Chinese medicinal plant, safflower, shows effective for treating pulmonary arterial hypertension (PAH), yet the underlying mechanisms remain largely unexplored. This study is aimed at exploring the potential molecular mechanisms of safflower in the treatment of PAH. METHODS: Network pharmacology approach and molecular docking were applied to identify the core active compounds, therapeutic targets, and potential signaling pathways of safflower against PAH. Meanwhile, high-performance liquid chromatography (HPLC) assay was performed to determine the core compounds from safflower. Further, the mechanism of action of safflower on PAH was verified by in vivo and in vitro experiments. RESULTS: A total of 15 active compounds and 177 targets were screened from safflower against PAH. Enrichment analysis indicated that these therapeutic targets were mainly involved in multiple key pathways, such as TNF signaling pathway and Th17 cell differentiation. Notably, molecular docking revealed that quercetin (core compound in safflower) displayed highest binding capacity with NLRP3. In vivo, safflower exerted therapeutic effects on PAH by inhibiting right ventricular hypertrophy, inflammatory factor release, and pulmonary vascular remodeling. Mechanistically, it significantly reduced the expression of proangiogenesis-related factors (MMP-2, MMP-9, Collagen 1, and Collagen 3) and NLRP3 inflammasome components (NLRP3, ASC, and Caspase-1) in PAH model. Similarly, these results were observed in vitro. Besides, we further confirmed that NLRP3 inhibitor had the same therapeutic effect as safflower in vitro. CONCLUSION: Our findings suggest that safflower mitigates PAH primarily by inhibiting NLRP3 inflammasome activation. This provides novel insights into the potential use of safflower as an alternative therapeutic approach for PAH.

Asunto(s)

Carthamus tinctorius , Simulación del Acoplamiento Molecular , Proteína con Dominio Pirina 3 de la Familia NLR , Farmacología en Red , Hipertensión Arterial Pulmonar , Proteína con Dominio Pirina 3 de la Familia NLR/metabolismo , Carthamus tinctorius/química , Animales , Simulación del Acoplamiento Molecular/métodos , Farmacología en Red/métodos , Hipertensión Arterial Pulmonar/tratamiento farmacológico , Hipertensión Arterial Pulmonar/metabolismo , Modelos Animales de Enfermedad , Ratas , Masculino , Humanos , Transducción de Señal/efectos de los fármacos , Ratones , Inflamasomas/metabolismo , Inflamasomas/efectos de los fármacos , Remodelación Vascular/efectos de los fármacos , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/uso terapéutico

RESUMEN

BACKGROUND: The combination of Astragalus membranaceus and Carthamus tinctorius (AC) exhibits significant therapeutic effects in cerebral ischemia/reperfusion injury (CIRI). Understanding the metabolic characteristics of brain microregions and disturbances in tissues and systemic circulation is crucial for elucidating the mechanisms of CIRI and the therapeutic benefits of AC. However, in situ metabolic regulation of the complex brain structure has not been adequately studied, and the therapeutic mechanism of AC requires immediate clarification. PURPOSE: The present study aimed to unveil the specific metabolic reprogramming of CIRI at systemic and microregional levels, identify key metabolic pathways and metabolites, and elucidate the therapeutic mechanisms of AC. METHODS: Air flow-assisted desorption electrospray ionization mass spectrometry imaging (AFADESI-MSI), a newly developed technique, was used to investigate metabolites in brain microregions. Hematoxylin-eosin, Nissl, and immunofluorescence staining were performed to visualize the microscopic changes associated with spatial metabolism. A comprehensive metabolomics study was conducted on serum, brain tissue, and microregions, along with neurological assessments, cerebral infarction measurements, and Evans blue experiments, to assess the systemic and local metabolic effects of AC treatment for CIRI. RESULTS: AC significantly reduced neurological damage, minimized infarct size, and repaired blood-brain barrier damage in CIRI rats. AFADESI-MSI demonstrated that the metabolic imbalance caused by CIRI primarily occurs in the cerebral cortex, hippocampus, caudate putamen, thalamus, cerebellar cortex, and fiber tract regions. Significant changes in 16 metabolites were observed in these regions, corresponding to neuron damage, glial cell activation, and neural repair. 20 metabolites from serum and 4 from brain tissue varied significantly with the sham group. Comprehensive metabolomics analysis indicated a close relationship among serum, tissue, and microregional metabolism. CIRI-induced systemic and localized metabolic disorders involve 14 metabolic pathways. AC conferred therapeutic benefits in CIRI by reversing various metabolic imbalances. CONCLUSION: AFADESI-MSI efficiently visualized brain microregion metabolism. Comprehensive metabolomics analysis revealed detailed insights into the specific metabolic reprogramming in CIRI and the therapeutic impacts of AC. AC demonstrated significant clinical potential as an adjunct therapy to existing CIRI treatments.

Asunto(s)

Astragalus propinquus , Encéfalo , Carthamus tinctorius , Metabolómica , Ratas Sprague-Dawley , Daño por Reperfusión , Animales , Carthamus tinctorius/química , Astragalus propinquus/química , Masculino , Daño por Reperfusión/tratamiento farmacológico , Daño por Reperfusión/metabolismo , Encéfalo/metabolismo , Encéfalo/efectos de los fármacos , Ratas , Isquemia Encefálica/tratamiento farmacológico , Espectrometría de Masa por Ionización de Electrospray

RESUMEN

Carthamus tinctorius L. (Safflower) is extensively used as a functional food and herbal medicine, with its application closely associated with hydroxysafflor yellow A (HSYA). However, the low oral bioavailability of HSYA in safflower extract (SFE) limits its health benefits and application. Our study found that co-administration of 250, 330, and 400 mg/kg peach kernel oil (PKO) increased the oral bioavailability of HSYA in SFE by 1.99-, 2.11-, and 2.49-fold, respectively. The enhanced bioavailability is attributed to improved lipid solubility and intestinal permeability of HSYA in SFE due to PKO. PKO is believed to modify membrane fluidity and tight junctions, increase paracellular penetration, and inhibit the expression and function of P-glycoprotein, enhancing the transcellular transport of substrates. These mechanisms suggest that PKO is an effective absorption enhancer. Our findings provide valuable insights for developing functional foods with improved bioavailability.

Asunto(s)

Disponibilidad Biológica , Carthamus tinctorius , Chalcona , Extractos Vegetales , Prunus persica , Quinonas , Chalcona/química , Chalcona/análogos & derivados , Chalcona/farmacología , Extractos Vegetales/química , Extractos Vegetales/administración & dosificación , Extractos Vegetales/metabolismo , Quinonas/química , Quinonas/metabolismo , Carthamus tinctorius/química , Animales , Prunus persica/química , Prunus persica/metabolismo , Humanos , Aceites de Plantas/química , Masculino , Ratas Sprague-Dawley , Ratas , Absorción Intestinal/efectos de los fármacos

RESUMEN

Food waste is responsible for the loss of 1.3 billion tons of food, some of which are related to by-products with great nutritional and energy potential that are still underexplored, such as safflower cake derived from the oil extraction industry. Therefore, the aim of this study was to evaluate the effects of incorporating safflower cake (Carthamus tinctorius) and the mixing method used to produce composite wheat-based flour in order to develop a new ingredient. The results were analyzed using ANOVA, and the Tukey test was applied at a significance level of 5 %. The composite flours obtained by the conventional mixing method showed, when compared to wheat flour, a higher concentration of proteins (+5g 100 g-1), minerals (+86 mg kg-1 of Fe, +30 mg kg-1 of Zn), phenolic compounds (15 mg GAE g-1), flavonoids (0.3 mg QE g-1), and lower oil absorption (-0.5 g oil g sample-1), making them suitable for hot flour-based sauces, salad dressings, frozen desserts, cookies and fried products. While extruded composite flours presented better homogenization, reduction of moisture (1 g 100 g-1), lipids (3 g 100 g-1), and mycotoxin concentrations, increased antioxidant activity (DPPH -0.07 IC50 mg/L and ORAC +9 µmol Trolox Eq/g), water absorption and solubility indexes, and oil absorption index, making it suitable for bakery products, meat, and dairy sausages. The developed composite flour proved to be a good nutritional ingredient; thus, its consumption can represent an important nutritional strategy with low production costs, as well as a sustainable solution, reducing food waste and, therefore, toward the concepts of the circular economy.

Asunto(s)

Carthamus tinctorius , Harina , Manipulación de Alimentos , Harina/análisis , Carthamus tinctorius/química , Manipulación de Alimentos/métodos , Valor Nutritivo , Triticum/química , Ingredientes Alimentarios/análisis , Fenoles/análisis , Minerales/análisis , Minerales/química , Flavonoides/análisis

RESUMEN

Carthami Flos(flowers of Carthamus tinctorius) with the effects of activating blood, dredging meridians, dissipating stasis, and relieving pain is one of the commonly used traditional Chinese medicines for promoting blood circulation and resolving stasis in clinical practice. So far, more than 210 compounds in Carthami Flos have been isolated and reported, including quinochalcones(safflower yellow pigments and red pigments), flavonoids, spermidines, alkaloids, polyacetylenes, and organic acids. Safflower yellow pigments, as the main water-soluble active components of Carthami Flos, is commonly obtained by the water extraction method, while red pigments are commonly obtained by the alkali extraction and acid precipitation method. In recent years, natural deep eutectic solvents as green solvents have demonstrated promising application prospects in the extraction and separation of pigments from Carthami Flos. This review systematically summarizes the chemical constituents of Carthami Flos and analyzes the extraction process of pigment components from Carthami Flos, aiming to provide a reference for further utilization of Carthami Flos resources.

Asunto(s)

Carthamus tinctorius , Medicamentos Herbarios Chinos , Flores , Flores/química , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/aislamiento & purificación , Carthamus tinctorius/química , Pigmentos Biológicos/química , Pigmentos Biológicos/aislamiento & purificación

RESUMEN

BACKGROUND: The research about sustainable and alternative plant protein sources has accelerated with the increasing need for protein. Safflower meal has a potential to be used in protein production due to its high protein content. This research aimed to produce an alternative plant-based protein powder using safflower meal. Both extraction and spray-drying parameters of safflower protein powder production were optimized using response surface methodology to achieve maximum yield. Moreover, the physicochemical and functional properties of safflower protein were determined and compared with those of commercial protein powders (soy, sunflower, pea, fava bean, and rice). RESULTS: The optimum extraction conditions were found to be 33.06:1 mL-1 g solvent-to-meal ratio, pH 11.00, 23.34 °C extraction temperature, and 30.86 min extraction time, which were achieved with a protein yield response of 75.21%. The highest powder yield (51.28%) was recorded for drying conditions of inlet air temperature of 160.11 °C, aspiration rate of 54.17 m3 h-1, and feed flow rate of 16.01 mL min-1. According to the amino acid profile of safflower protein, the glutamic acid content (14 475 mg (100 g)-1) was highest, while the methionine content (96 mg (100 g)-1) was lowest. Moreover, safflower protein can be regarded as a high-quality protein due to its high essential amino acid ratio (41.55%). The experiments showed that safflower protein had high solubility and good foam and emulsifying properties. CONCLUSION: Safflower protein could be a nutritional and functional protein source for the food industry. © 2024 Society of Chemical Industry.

Asunto(s)

Carthamus tinctorius , Proteínas de Plantas , Polvos , Carthamus tinctorius/química , Polvos/química , Proteínas de Plantas/química , Manipulación de Alimentos/métodos , Secado por Pulverización , Desecación/métodos , Temperatura , Aminoácidos/química , Aminoácidos/análisis

RESUMEN

Non-alcoholic fatty liver disease (NAFLD) is a complex pathogenic metabolic syndrome characterized by increased inflammation and endoplasmic reticulum stress. In recent years, natural polysaccharides derived from traditional Chinese medicine have shown significant anti-inflammatory effects, making them an attractive therapeutic option. However, little research has been conducted on the therapeutic potential of dried tangerine peel polysaccharide (DTPP) - one of the most important medicinal resources in China. The results of the present study showed that DTPP substantially reduced macrophage infiltration in vivo and suppressed the expression of pro-inflammatory factors and endoplasmic reticulum stress-related genes. Additionally, surface plasmon resonance analysis revealed that DTPP had a specific affinity to myeloid differentiation factor 2, which consequently suppressed lipopolysaccharide-induced inflammation via interaction with the toll-like receptor 4 signaling pathway. This study provides a potential molecular mechanism underlying the anti-inflammatory effects of DTPP on NAFLD and suggests DTPP as a promising therapeutic strategy for NAFLD treatment.

Asunto(s)

Estrés del Retículo Endoplásmico , Inflamación , Polisacáridos , Receptor Toll-Like 4 , Receptor Toll-Like 4/metabolismo , Receptor Toll-Like 4/antagonistas & inhibidores , Polisacáridos/farmacología , Polisacáridos/química , Animales , Estrés del Retículo Endoplásmico/efectos de los fármacos , Ratones , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Antígeno 96 de los Linfocitos/antagonistas & inhibidores , Antígeno 96 de los Linfocitos/metabolismo , Carthamus tinctorius/química , Ratones Endogámicos C57BL , Estructura Molecular , Relación Dosis-Respuesta a Droga , Relación Estructura-Actividad , Enfermedad del Hígado Graso no Alcohólico/tratamiento farmacológico , Enfermedad del Hígado Graso no Alcohólico/patología , Enfermedad del Hígado Graso no Alcohólico/metabolismo , Humanos , Lipopolisacáridos/antagonistas & inhibidores , Lipopolisacáridos/farmacología , Masculino , Células RAW 264.7 , Antiinflamatorios/farmacología , Antiinflamatorios/química

RESUMEN

Safflopentsides A-C (1-3), three highly oxidized rearranged derivatives of quinochalcone C-glycosides, were isolated from the safflower yellow pigments. Their structures were determined based on a detailed spectroscopic analysis (UV, IR, HR-ESI-MS, 1D and 2D NMR), and the absolute configurations were confirmed by the comparison of experimental ECD spectra with calculated ECD spectra. Compounds 1-3 have an unprecedented cyclopentenone or cyclobutenolide ring A containing C-glucosyl group, respectively. The plausible biosynthetic pathways of compounds have been presented. At 10 µM, 2 showed strong inhibitory activity against rat cerebral cortical neurons damage induced by glutamate and oxygen sugar deprivation.

Asunto(s)

Carthamus tinctorius , Glicósidos , Oxidación-Reducción , Glicósidos/química , Glicósidos/farmacología , Glicósidos/aislamiento & purificación , Animales , Carthamus tinctorius/química , Ratas , Estructura Molecular , Neuronas/efectos de los fármacos , Relación Estructura-Actividad , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/química , Fármacos Neuroprotectores/aislamiento & purificación , Relación Dosis-Respuesta a Droga , Corteza Cerebral/efectos de los fármacos , Chalconas/farmacología , Chalconas/química , Chalconas/aislamiento & purificación

RESUMEN

Safflower (Carthamus tinctorius) oleosomes are unique organelles that house triglycerides and fatty acids and demonstrate a natural resilience to environmental stresses. There is recent growing interest in safflower oleosomes due to their potential applications in dermatology, especially as a carrier technology to improve drug penetration through the skin. This paper explores various aspects of safflower oleosomes, including their production, safety, absorption, and applications in photoprotection and epidermal remodeling. Oleosomes have shown encouraging results in targeted drug delivery in in vitro and in vivo animal models; however, human clinical research is required to determine their efficacy and safety in dermatology. Oleosomes are comprise a novel biotechnology that has the potential to transform sustainable and natural treatments in dermatology by utilizing their unique structure. Safflower oleosomes are stable lipid molecules that can deliver small and large molecules with high efficacy. This review will examine the current research findings and prospective future applications of oleosomes.

Asunto(s)

Carthamus tinctorius , Animales , Humanos , Carthamus tinctorius/química , Gotas Lipídicas/química , Piel , Epidermis

RESUMEN

Breast cancer is the most common type of cancer in women and the second  cause of cancer-related death after lung cancer. Although the common methods used in the treatment of breast cancer are chemotherapy, radiotherapy and surgery, the search for alternative treatments continues.  The leading  alternative treatments are medicinal plants which actually inspire the production of many cancer drugs. In this study, the proliferative and metastatic effects of Carthamus tinctorius L., known for its many therapeutic properties, on metastatic breast cancer were investigated. Here, intending to evaluate the the content and actions of different extracts of safflower leaves extracts were prepared by extracting in water, alcohol and oil and analysed by FTIR. Their antioxidant effect was tested and then the extracts were applied to metastatic breast cancer cells. FTIR spectrums of all three extracts have revealed the presence of organic compounds.  It is found that all extracts but mostly the oil extract has antioxidant property. MTT assay, wound healing assay and gene expression analysis were performed to assess the antiproliferative and anti metastatic effects of the extracts on breast cancer cells. It is found that, there is no significant antiproliferative effect of extracts on MDA-MB-231 cells except the alcohol extract. However, all safflower extracts, especially the oil extract, significantly reduced the metastatic potential of breast cancer cells. It is concluded that safflower contents are potent chemicals which inhibit the cellular mechanisms underlying the spreading of cancer cells and further analysis may lead to new initiatives in drug design research.

Asunto(s)

Neoplasias de la Mama , Carthamus tinctorius , Humanos , Femenino , Carthamus tinctorius/química , Carthamus tinctorius/metabolismo , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/genética , Células MDA-MB-231 , Antioxidantes/farmacología , Antioxidantes/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/química

RESUMEN

Carthamus tinctorius L. leaves, a waste product after Carthami flos production, are rich in flavonoids. Total flavonoids from C. tinctorius L. leaves (TFCTLL) exhibited the protective effect on acute liver injury in mice in previous studies. The aim of the present study was to evaluate the hepatoprotective effect of TFCTLL on chronic liver injury (CLI) and investigate the underlying mechanism. The chemical components of TFCTLL were identified by UPLC-Q-TOF/MS, and their migration into blood was evaluated. The protective effect of TFCTLL on CLI was evaluated by antioxidative and anti-inflammatory experiments in vitro, network pharmacology and a carbon tetrachloride (CCl4)-induced CLI mouse model. We indentified 18 chemical components in the TFCTLL samples and 4 components in plasma. TFCTLL showed significant anti-inflammatory activity and antioxidant capacity in vitro and in vivo. TFCTLL administration prominently improved the liver function and structure, decreased the mRNA expression levels of TLR2, TLR3, TLR4, NF-κB p65, IRF3, AKT1, TRIF, PI3K, MyD88, IL-1ß and TNF-α and inhibited the protein expression and nuclear translocation of NF-κB p65 in mice with CLI. The molecular docking results showed that components in plasma had high binding affinity for the targets TLR4, PI3K and AKT1. Therefore, TFCTLL has a protective effect against CCl4-induced CLI, and the underlying mechanisms may be related to antioxidation, anti-inflammation and modulation of the TLRs/NF-κB and PI3K/AKT pathways.

Asunto(s)

Tetracloruro de Carbono , Carthamus tinctorius , Ratones , Animales , Tetracloruro de Carbono/metabolismo , Tetracloruro de Carbono/farmacología , Carthamus tinctorius/química , Carthamus tinctorius/metabolismo , Estrés Oxidativo , FN-kappa B/metabolismo , Flavonoides/farmacología , Flavonoides/metabolismo , Simulación del Acoplamiento Molecular , Receptor Toll-Like 4/metabolismo , Fosfatidilinositol 3-Quinasas/metabolismo , Estructura Molecular , Hígado , Antioxidantes/farmacología , Antiinflamatorios/farmacología , Antiinflamatorios/metabolismo

RESUMEN

The quality of traditional Chinese medicine (TCM) guarantees its clinical efficacy. Although advanced analytical techniques and methods can accurately determine the content of chemical components in TCM, it is difficult to accurately determine its clinical efficacy. In addition, the current analytical methods and technologies are complex and have difficulty meeting the requirements of a rapid, accurate and convenient determination of TCM quality. In this study, we first propose the concept of "indistinct" evaluation of the quality of TCM, that is, combining biological potency with character evaluation, quantifying the character evaluation, and preparing the safflower quality grade evaluation card based on the character analysis, which provides research ideas and methods for the rapid and accurate evaluation of the quality of TCM. We determined the biological potency of different batches of safflower based on the in vitro antiplatelet aggregation model and divided the safflower samples into two grades based on the biological potency. We further collected the color information of different grades of safflower samples, quantified the color information of different grades of safflower, drew a quality grade evaluation card for the rapid judgment of safflower quality grade and verified its accuracy by pharmacodynamic evaluation. To further analyze the differences in the material basis of different grades of safflower, the LC-MS method was used to simultaneously determine the contents of 19 chemical components, such as myricetin, in different grades of safflower samples to analyze the differences in the material basis of different grades of safflower. The result shows that the different grades of safflower exhibited significant differences in color. The pharmacodynamic results show that the quality evaluation card prepared based on color information can accurately evaluate quality, and the effect of first-class safflower is significantly better than that of second-class safflower. The chemical analysis results of different grades of safflower show that there are also significant differences between them, among which hypericin, 6-hydroxyapin-6-O-glucose-7-O-glucuronide, 6-hydroxykaempferol-3,6-O-diglucoside-7-O-glucuronic acid glycoside, 6-hydroxykaempferol-3,6,7-tri-O-glucoside and hydroxysafflower yellow A exhibit significant differences, which may be the main differentiating components of different grades of safflower. This study preliminarily confirmed that the "indistinct" evaluation of the quality of TCM based on character analysis is accurate and scientific, and the quality evaluation card prepared can accurately judge the quality of TCM, providing a reference for the rapid application of TCM character evaluation.

Asunto(s)

Carthamus tinctorius , Medicamentos Herbarios Chinos , Medicina Tradicional China , Carthamus tinctorius/química , Medicina de Precisión , Medicamentos Herbarios Chinos/química , Cromatografía Liquida

RESUMEN

Carthami Flos, as a traditional blood-activating and stasis-resolving drug, possesses anti-tumor, anti-inflammatory, and immunomodulatory pharmacological activities. Flavonoid glycosides are the main bioactive components in Carthamus tinctorius. Glycosyltransferase deserves to be studied in depth as a downstream modification enzyme in the biosynthesis of active glycoside compounds. This study reported a flavonoid glycosyltransferase CtUGT49 from C. tinctorius based on the transcriptome data, followed by bioinformatic analysis and the investigation of enzymatic properties. The open reading frame(ORF) of the gene was 1 416 bp, encoding 471 amino acid residues with the molecular weight of about 52 kDa. Phylogenetic analysis showed that CtUGT49 belonged to the UGT73 family. According to in vitro enzymatic results, CtUGT49 could catalyze naringenin chalcone to the prunin and choerospondin, and catalyze phloretin to phlorizin and trilobatin, exhibiting good substrate versatility. After the recombinant protein CtUGT49 was obtained by hetero-logous expression and purification, the enzymatic properties of CtUGT49 catalyzing the formation of prunin from naringenin chalcone were investigated. The results showed that the optimal pH value for CtUGT49 catalysis was 7.0, the optimal temperature was 37 ℃, and the highest substrate conversion rate was achieved after 8 h of reaction. The results of enzymatic kinetic parameters showed that the K_m value was 209.90 μmol·L~(-1) and k_(cat) was 48.36 s~(-1) calculated with the method of Michaelis-Menten plot. The discovery of the novel glycosyltransferase CtUGT49 is important for enriching the library of glycosylation tool enzymes and provides a basis for analyzing the glycosylation process of flavonoid glycosides in C. tinctorius.

Asunto(s)

Carthamus tinctorius/química , Filogenia , Flavonoides/análisis , Glicósidos/análisis , Glicosiltransferasas/genética , Antiinflamatorios , Chalconas

RESUMEN

Carthami Flos, as a traditional blood-activating and stasis-resolving drug, possesses anti-tumor, anti-inflammatory, and immunomodulatory pharmacological activities. Flavonoid glycosides are the main bioactive components in Carthamus tinctorius. Glycosyltransferase deserves to be studied in depth as a downstream modification enzyme in the biosynthesis of active glycoside compounds. This study reported a flavonoid glycosyltransferase CtUGT49 from C. tinctorius based on the transcriptome data, followed by bioinformatic analysis and the investigation of enzymatic properties. The open reading frame(ORF) of the gene was 1 416 bp, encoding 471 amino acid residues with the molecular weight of about 52 kDa. Phylogenetic analysis showed that CtUGT49 belonged to the UGT73 family. According to in vitro enzymatic results, CtUGT49 could catalyze naringenin chalcone to the prunin and choerospondin, and catalyze phloretin to phlorizin and trilobatin, exhibiting good substrate versatility. After the recombinant protein CtUGT49 was obtained by hetero-logous expression and purification, the enzymatic properties of CtUGT49 catalyzing the formation of prunin from naringenin chalcone were investigated. The results showed that the optimal pH value for CtUGT49 catalysis was 7.0, the optimal temperature was 37 ℃, and the highest substrate conversion rate was achieved after 8 h of reaction. The results of enzymatic kinetic parameters showed that the K_m value was 209.90 µmol·L~(-1) and k_(cat) was 48.36 s~(-1) calculated with the method of Michaelis-Menten plot. The discovery of the novel glycosyltransferase CtUGT49 is important for enriching the library of glycosylation tool enzymes and provides a basis for analyzing the glycosylation process of flavonoid glycosides in C. tinctorius.

Asunto(s)

Carthamus tinctorius , Chalconas , Carthamus tinctorius/genética , Carthamus tinctorius/química , Filogenia , Flavonoides/análisis , Glicósidos/análisis , Glicosiltransferasas/genética , Antiinflamatorios

RESUMEN

(1) Background: The florets of Carthamus tinctorius L. are traditionally used as a blood-activating drug and can be used for the treatment of atherosclerosis, but no compounds with anti-atherosclerotic activity have been reported. (2) Methods: This study investigated the chemical compounds from the florets of C. tinctorius. Comprehensive spectroscopic techniques revealed their structures, and ECD calculations established their absolute configurations. Nile Red staining, Oil Red O staining, and cholesterol assessment were performed on these compounds and their aglycones for the inhibitory activity against the formation of foam cells induced by oxidized low-density lipoprotein (ox-LDL) in RAW264.7 macrophages. In addition, RAW264.7 macrophages were tested for their anti-inflammatory activity by measuring the inhibition of NO production caused by LPS. (3) Results: Five new sesquiterpenoids (1-5) isolated from the florets of C. tinctorius were identified as (-)-(1R,4S,9S,11R)-caryophyll-8(13)-en-14-ol-5-one (1), (+)-(1R,4R,9S,11R)-caryophyll-8(13)-en-14-ol-5-one (2), (-)-(3Z,1R,5S,8S,9S,11R)-5,8-epoxycaryophyll-3-en-14-O-ß-D-glucopyranoside (3), (+)-(1S,7R,10S)-guai-4-en-3-one-11-O-ß-D-fucopyranoside (4), and (-)-(2R,5R,10R)-vetispir-6-en-8-one-11-O-ß-D-fucopyranoside (5). All compounds except for compound 3 reduced the lipid content in ox-LDL-treated RAW264.7 cells. Compounds 3 and 4 and their aglycones were found to reduce the level of total cholesterol (TC) and free cholesterol (FC) in ox-LDL-treated RAW264.7 cells. However, no compounds showed anti-inflammatory activity. (4) Conclusion: Sesquiterpenoids from C. tinctorius help to decrease the content of lipids, TC and FC in RAW264.7 cells, but they cannot inhibit NO production, which implies that their anti-atherogenic effects do not involve the inhibition of inflammation.

Asunto(s)

Aterosclerosis , Carthamus tinctorius , Sesquiterpenos , Carthamus tinctorius/química , Sesquiterpenos/farmacología , Sesquiterpenos/química , Macrófagos , Antiinflamatorios/farmacología , Aterosclerosis/tratamiento farmacológico

RESUMEN

This study investigated the chemical components from the florets of Carthamus tinctorius. Five compounds were isolated from C. tinctorius by column chromatography with silica gel and toyopearl HW-40 F, preparative thin-layer chromatography(TLC), and semi-preparative reverse phased high performance liquid chromatography(RP-HPLC). Their structures were identified by mass spectrometry(MS), one-dimension nuclear magnetic resonance(1 D-NMR), two-dimension nuclear magnetic resonance(2 D-NMR), and single-crystal X-ray diffraction as(-)-(2S,3S,5S,7S,10R)-eudesma-4(15)-en-2,3,11-triol(1 a),(+)-(2R,3R,5R,7R,10S)-eudesma-4(15)-en-2,3,11-triol(1 b), rosin(2),(+)-syringaresinol(3), and(E)-1-(4'-hydroxyphenyl)-but-1-en-3-one(4). Compounds 1 a and 1 b are a pair of enantiomeric sesquiterpenoids. Compound 1 a is a new eudesmene and is named(-)-plucheol A. Compound 1 a at 100 µmol·L~(-1) showed significant antioxidant activity against ABTS~(+·) and DPPH·, with the scavenging rates of 30.98%±4.17% and 27.52%±1.24%, respectively, while compound 1 b was inactive. In addition, compounds 1 a and 1 b showed no obvious anti-inflammatory activity.

Asunto(s)

Carthamus tinctorius , Sesquiterpenos , Carthamus tinctorius/química , Cromatografía Líquida de Alta Presión/métodos , Sesquiterpenos/química , Estereoisomerismo , Espectrometría de Masas , Estructura Molecular

RESUMEN

Safflower (Carthamus tinctorius L.) is cultivated in various countries for the flavonoid compounds it contains. These flavonoids have been used in many industries as drugs and/or dyes. Over 60 flavonoids have been isolated from safflower. These flavonoids can be divided into two groups: special and common, both of which are active pharmaceutical ingredients efficacious in the treatment of cardiovascular and cerebrovascular diseases. Gene functions have been studied to figure out the biosynthesis of flavonoids in safflower. However, there is no comprehensive summary of the flavonoids in safflower. Research was recognised through systematic searches of ScienceDirect, PubMed, Web of Science, and CNKI databases by searching terms of "Carthamus tinctorius L.", "safflower", "flavonoid", "pharmacology", and "gene". More than 200 research reports were included after eligibility checks. This study summarizes the application of flavonoids in medicine and other industries. Comprehensively collects the chemical structure information of the two groups of flavonoids, and organic acids, alkaloids, spermidine, polyacetylene, and polysaccharides. The mechanism of two groups of flavonoids in treatment of cardiovascular and cerebrovascular diseases was describe in detail, and pharmacological mechanisms of protecting liver, lung and bone, and anti-cancer and anti-inflammatory were also summarised. Besides, the study updated the latest information on the molecular biology of safflower flavonoids. It is found that two groups of flavonoids in safflower have obvious differences in application, chemical structure, pharmacological mechanism, and biosynthetic pathway. It is hoped that this summative research will provide a new insight to flavonoids research in safflower.

Asunto(s)

Alcaloides , Carthamus tinctorius , Alcaloides/metabolismo , Vías Biosintéticas/genética , Carthamus tinctorius/química , Flavonoides/metabolismo