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/químicaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Rheum webbianum Royle (RW) holds significant ethnopharmacological importance owing to its 5000-year history of cultivation for medicinal and culinary purposes. Demonstrating therapeutic advantages in traditional and contemporary medical practices, RW exhibits key pharmacological effects including anticancer activity, gastrointestinal control, anti-inflammatory properties, and suppression of fibrosis. Despite its recognized vast bioactivities in ethnopharmacology, its efficacy against the colorectal cancer (CRC) remains incompletely understood. AIM OF THE STUDY: This study for the first time aims to investigate the chemo-preventive capabilities of various extracts derived from RW rhizomes against CRC development. MATERIALS AND METHODS: Four types of RW extracts were prepared by using different solvents viz: Hexane, Ethy-acetate, Ethanol and Methanol. All the four extracts were evaluated for cytotoxicity on HCT-116 human CRC cells. Promising extracts were further investigated in-vivo at varying doses using 1,2-dimethylhydrazine (DMH) induced rat CRC model to assess the anti-oxidant and anticancer properties as well as their effects on the associated hepatic deterioration and hematological alterations. RESULTS: Cell viability: In-vitro assessments demonstrated a dose and time-dependent reduction in HCT-116 cell viability following treatment with methanolic and ethanolic extracts of RW, reducing viability by up to 85% and 90%, respectively, at 200 µg/ml. HISTOPATHOLOGY: Histopathological analyses revealed significant improvements in colon tissue morphology in RW extract-treated groups compared to DMH-only treated animals. RW-treated groups showed reduced structural abnormalities, congestion, inflammatory cell infiltration, crypt abscess formation, and dysplasia. In contrast, the DMH-only group exhibited irregular glandular structure, mucosal destruction, extensive inflammatory cell infiltration, crypt abscess formation, and dysplasia. These results highlight the potential of RW methanolic and ethanolic extracts in mitigating colon cancer-related histopathological alterations. Haematological, and hepatic parameters: In the DMH-induced colorectal cancer rat model, significant hematological imbalances were evident, including a 49.13% decrease in erythrocytes, 32.18% in hemoglobin, and 26.79% in hematocrit, along with a 79.62% increase in white blood cells and 68.96% rise in platelets. Administration of RW rhizome extracts effectively restored these hematological parameters to levels comparable to those in the control group. Furthermore, RW treatment significantly reduced serum ALT and AST levels, which had increased by 36.78% and 33.12%, respectively, due to DMH exposure. RW intervention also mitigated the onset of atherosclerosis, evidenced by notable reductions in serum total cholesterol and triglyceride levels. Comparative analysis indicated that RW-treated DMH groups effectively restored lipid profiles, contrasting with the DMH-only group which exhibited markers indicative of colon cancer. Oxidative stress: The DMH-treated group showed a significant increase in MDA levels by 195.59%, indicative of heightened free radical production, coupled with decreased levels of SOD (33%), CAT (48%), GSH (58%), and GR activity (49%), signifying oxidative stress. Treatment with RW extracts in DMH-treated rats markedly reduced MDA levels and enhanced SOD, CAT, GSH, and GR activities. These results underscore the antioxidant efficacy of RW extracts. CONCLUSION: This study underscores the significant potential of RW rhizome extracts in inhibiting colorectal cancer development. Further investigations are warranted to identify the active constituents responsible for these promising outcomes, positioning RW as a natural and potential agent in combating colon cancer.
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1,2-Dimetilhidrazina , Antineoplásicos Fitogénicos , Neoplasias Colorrectales , Extractos Vegetales , Rheum , Rizoma , Animales , Extractos Vegetales/farmacología , Neoplasias Colorrectales/tratamiento farmacológico , Neoplasias Colorrectales/inducido químicamente , Neoplasias Colorrectales/patología , Humanos , Ratas , 1,2-Dimetilhidrazina/toxicidad , Masculino , Células HCT116 , Rheum/química , Antineoplásicos Fitogénicos/farmacología , Supervivencia Celular/efectos de los fármacos , Hígado/efectos de los fármacos , Hígado/patología , Hígado/metabolismo , Antioxidantes/farmacologíaRESUMEN
The growing utilization of Traditional Chinese Medicine (TCM) has resulted in an increase in wastewater. Herein, a new kind of organic-inorganic redox mediator membrane by immobilizing γ-FeO(OH) and aloe-emodin(AE) with the characteristic large π-conjugation anthraquinone structure on PVDF membrane was innovatively achieved. AE exhibiting both electron deficiency and redox activity possesses a co-catalyst role in degradation of tannic acid (TA), aiding in the separation of charge carriers through the sequential hydrogenation and dehydrogenation of AE. The removal rates of TA were 92.8 % in the tannic acid solution and 60.3 % in the simulated rhubarb wastewater by the AE-γ-FeO(OH) membrane under PMS+Vis conditions in 45 min. Also, they show a higher recovery of pure water flux and owning good fouling performance. Overall, this current work presents a novel approach for the design and preparation of organic-inorganic photocatalytic composite membrane using readily available natural products for the purification TCM wastewater.
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Antraquinonas , Membranas Artificiales , Oxidación-Reducción , Taninos , Contaminantes Químicos del Agua , Taninos/química , Antraquinonas/química , Catálisis , Contaminantes Químicos del Agua/química , Aguas Residuales/química , Purificación del Agua/métodos , Rheum/química , Eliminación de Residuos Líquidos/métodos , PolifenolesRESUMEN
Rheum pumilum stands as both a quintessential alpine plant and a significant traditional Chinese and Tibetan medicinal herb. Unraveling the molecular intricacies of seed germination in Rh. pumilum not only unveils the genetic foundations of plant seed germination strategies in high-altitude environments but also offers insights for cultivating Rh. pumilum medicinal materials. Employing transcriptome sequencing and the Weighted Gene Co-expression Network Analysis, this study delved into the shifts in gene expression levels across various stages of seed germination in Rh. pumilum. The process of seed germination in Rh. pumilum entails a cascade of complex physiological events. Six hormones (ABA, IAA, ETH, GA, BR, CK) emerged as pivotal players in seeds breaking in shells and the facilitation of rapid seed germination in Rh. pumilum. Fourteen transcription factor families (LOB, GRAS, B3, bHLH, bZIP, EIL, MYB, MYB related, NAC, TCP, WRKY, HSF, PLATZ, and SBP) along with four key genes (E2.4.1.13, EIN3, BZR, and BIN2) were identified that may be associated with both biotic and abiotic environmental stress. The ETR, ACACA and ATPeV0C genes were linked with energy accumulation during the initial stages of seed germination, CYP707A may play an important role in breaking seed dormancy, while the BRI1 gene may be correlated with swift seed germination. Additionally, several unidentified genes were recognized to play key roles in seed germination of Rh. pumilum, warranting further investigation. Moreover, Rh. pumilum demonstrates full activation of crucial physiological functions such as energy metabolism, signal transduction, and responses to biological and abiotic stresses during the seed breaking in shells. This study provides molecular evidence elucidating the swift seed germination strategies adopted by alpine plants to thrive in high-altitude environments. Furthermore, it serves as a foundational reference for enhancing seed germination rates and breeding practices to promote the sustainable development of Rh. pumilum medicinal materials.
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Perfilación de la Expresión Génica , Regulación de la Expresión Génica de las Plantas , Germinación , Rheum , Semillas , Germinación/genética , Rheum/genética , Semillas/genética , Semillas/crecimiento & desarrollo , Perfilación de la Expresión Génica/métodos , Transcriptoma , Reguladores del Crecimiento de las Plantas/metabolismo , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo , Factores de Transcripción/genética , Factores de Transcripción/metabolismoRESUMEN
The aim of this study was to characterize the pulp of Rheum ribes L. and to determine the effect of the pulp enriched with eugenol (1 %) or thymol (1 %) on the microbiological and physico-chemical quality of chicken breast fillets. Chicken breast fillets, inoculated with Listeria monocytogenes, Salmonella enterica subsp. enterica serovar Typhimurium, and Escherichia coli O157:H7 (~6.0 log10), were marinated for 24 h in a mixture prepared from a combination of Rheum ribes L. pulp with eugenol or thymol. The quality parameters were analyzed for 15 days at +4 °C. The Rheum ribes L. pulp was found to have high antioxidant activity, high total phenolic content and contained 22 different phenolic substances, among which rutin ranked first. The pulp contained high levels of p-xylene and o-xylene as volatile substances and citric acid as an organic acid. The combination of Pulp + Eugenol + Thymol (PET) reduced the number of pathogens in chicken breast fillets by 2.03 to 3.50 log10 on day 0 and by 2.25 to 4.21 log10 on day 15, compared to the control group (P < 0.05). The marinating treatment significantly lowered the pH values of fillet samples on the first day of the study, compared to the control group (P < 0.05). During storage, TVB-N levels showed slower increase in the treatment groups compared to the control group (P < 0.05). In addition, the marinating process led to significant changes in physicochemical parameters such as water holding capacity, color, texture, cooking loss, and drip loss compared to the control group (P < 0.05). In conclusion, the results of this study showed that the pulp of Rheum ribes L., which has a high antioxidant capacity and contains various bioactive compounds. Furthermore, S. Typhimurium, E. coli O157:H7 and L. monocytogenes were inhibited considerably by marinating Rheum ribes L. pulp with a combination of eugenol and thymol.
Asunto(s)
Pollos , Eugenol , Rheum , Timol , Animales , Timol/farmacología , Eugenol/farmacología , Rheum/química , Conservación de Alimentos/métodos , Microbiología de Alimentos , Listeria monocytogenes/efectos de los fármacos , Listeria monocytogenes/crecimiento & desarrollo , Carne/microbiología , Escherichia coli O157/efectos de los fármacos , Escherichia coli O157/crecimiento & desarrollo , Salmonella typhimurium/efectos de los fármacos , Salmonella typhimurium/crecimiento & desarrollo , Extractos Vegetales/farmacología , Antioxidantes/farmacología , Recuento de Colonia MicrobianaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Rheum palmatum (RP) is a widely used traditional herb, which possesses antioxidant properties, inhibits ROS production and reduces fever. AIM OF THE STUDY: The aim of this study was to examine the antioxidative properties of the water extract of RP on oxidative-stressed mice. MATERIALS & METHODS: Forty mice were administered with DL-homocysteine (DL-Hcy) to induce oxidative stress and were divided into four groups: 1) CK: NaCl and water; 2) DL-Hcy: DL-Hcy and water; 3) DL-Hcy+50RP: DL-Hcy with 50 mg kg-1 body weight (BW) d-1 RP; and 4) DL-Hcy+150RP: DL-Hcy with 150 mg kg-1 BW d-1 RP. Rhein (0.3 mg g-1 dry matter) was the main active ingredient in RP. RESULTS: When compared with Dl-Hcy mice, the mice with supplementary RP mitigated oxidative stress by reducing the liver concentrations of superoxide dismutase (SOD) by 27% and glutathione peroxidase (GSH-Px) by 32%, and the reactive oxygen species (ROS) in the kidney and spleen. These responses were more pronounced in DL-Hcy+150RP than DL-Hcy+50RP mice. RP also exhibited therapeutic effects on liver steatosis, chronic kidney nephritis and intestinal villus width shortening caused by oxidative stress, and concomitantly decreased the serum glucose concentration (RP vs. DL-HCY, 2.3 vs. 4.1 mmol L-1). CONCLUSION: It was concluded that RP possesses antioxidant and therapeutic properties that can mitigate lesions on organs and prevent diabetes in oxidative-stressed mice. This study highlights the potential of RP as a medicinal supplement for animals in the future.
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Antioxidantes , Estrés Oxidativo , Extractos Vegetales , Especies Reactivas de Oxígeno , Rheum , Animales , Rheum/química , Antioxidantes/farmacología , Antioxidantes/aislamiento & purificación , Extractos Vegetales/farmacología , Especies Reactivas de Oxígeno/metabolismo , Estrés Oxidativo/efectos de los fármacos , Ratones , Masculino , Agua/química , Hígado/efectos de los fármacos , Hígado/metabolismo , Hígado/patología , Superóxido Dismutasa/metabolismo , Riñón/efectos de los fármacos , Riñón/metabolismo , Riñón/patología , Glutatión Peroxidasa/metabolismo , Bazo/efectos de los fármacos , Bazo/metabolismoRESUMEN
Rhei Radix et Rhizoma and Magnoliae Officinalis Cortex have been used together to treat constipation in the clinical practices for more than 2000 years. Nonetheless, their compatibility mechanism is still unclear. In this study, the amelioration of Rhei Radix et Rhizoma combined with Magnoliae Officinalis Cortex on constipation was systematically and comprehensively evaluated. The results showed that their compatibility could markedly shorten gastrointestinal transport time, increase fecal water content and frequency of defecation, improve gastrointestinal hormone disorders and protect colon tissue of constipation rats compared with the single drug. Furthermore, according to 16S rRNA sequencing in conjunction with UPLC-Q-TOF/MS, the combination of two herbal medications could greatly raise the number of salutary bacteria (Lachnospiraceae, Romboutsia and Subdoligranulum) while decreasing the abundance of pathogenic bacteria (Erysipelatoclostridiaceae). And two herb drugs could markedly improve the disorder of fecal metabolic profiles. A total of 7 different metabolites associated with constipation were remarkably shifted by the compatibility of two herbs, which were mainly related to arachidonic acid metabolism, alpha-linolenic acid metabolism, unsaturated fatty acid biosynthesis and other metabolic ways. Thus, the regulation of intestinal microbiome and its metabolism could be a potential target for Rhei Radix et Rhizoma and Magnoliae Officinalis Cortex herb pair to treat constipation. Furthermore, the multi-omics approach utilized in this study, which integrated the microbiome and metabolome, had potential for investigating the mechanism of traditional Chinese medicines.
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Estreñimiento , Medicamentos Herbarios Chinos , Heces , Microbioma Gastrointestinal , Magnolia , Ratas Sprague-Dawley , Rheum , Ratas , Animales , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/farmacología , Magnolia/química , Microbioma Gastrointestinal/efectos de los fármacos , Estreñimiento/tratamiento farmacológico , Estreñimiento/metabolismo , Masculino , Rheum/química , Heces/microbiología , Heces/química , Cromatografía Líquida de Alta Presión , Metabolómica , Rizoma/química , Metaboloma/efectos de los fármacos , MultiómicaRESUMEN
This study employed segmented variable-frequency ultrasound synergistic hot-air drying (SVFU-HAD) for Rhubarb slices, selected two sets of time nodes for frequency conversion (60 min, 120 min, and 90 min, 150 min), and two sequences of frequency conversion (high-frequency to low-frequency, and low-frequency to high-frequency). It aimed to investigate the effects of SVFU-HAD on the drying characteristics, quality, and heat transfer of Rhubarb slices. The findings indicated that segmented variable-frequency ultrasound has advantages in increasing drying rate and improving uniformity of cavitation effects compared to constant-frequency ultrasound. Analysis of physical properties revealed that the rehydration performance of dried products subjected to ultrasonic variable-frequency treatment (90 min, 150 min) according to the drying rate was better (RR > 3.3). The transition mode from high-frequency to low-frequency in variable-frequency ultrasonic treatment contributes to maintaining the overall color of Rhubarb. Analysis of chemical properties unveiled that Rhubarb treated with 40 kHz (0 min)-28 kHz (60 min)-25 kHz (120 min) segmented variable-frequency ultrasound contained overall higher levels of tannins, dianthrones and free anthraquinones content, which exceeded the average values by 3.24%, 26.65%, and 14.42%, respectively. In addition, thermal analysis results based on ANSYS Workbench software demonstrated that the drying uniformity of SVFU-HAD is superior to that of hot-air drying and constant-frequency ultrasound synergistic hot-air drying (CFU-HAD). Overall, the SVFU-HAD method employed in this study presents an innovative approach to ultrasound synergistic hot-air drying research with promising potential for enhancing the efficiency and quality characteristics of Rhubarb slices.
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Desecación , Calor , Rheum , Rheum/química , Desecación/métodos , Aire , Ondas UltrasónicasRESUMEN
BACKGROUND: Rheum tanguticum root, cataloged as "Daehwang" in the Korean Pharmacopeia, is rich in various anthraquinones known for their anti-inflammatory and antioxidant properties. Formulations containing Daehwang are traditionally employed for treating neurological conditions. This study aimed to substantiate the antiepileptic and neuroprotective efficacy of R. tanguticum root extract (RTE) against trimethyltin (TMT)-induced epileptic seizures and hippocampal neurodegeneration. METHODS: The constituents of RTE were identified by ultra-performance liquid chromatography (UPLC). Experimental animals were grouped into the following five categories: control, TMT, and three TMT+RTE groups with dosages of 10, 30, and 100 mg/kg. Seizure severity was assessed daily for comparison between the groups. Brain tissue samples were examined to determine the extent of neurodegeneration and neuroinflammation using histological and molecular biology techniques. Network pharmacology analysis involved extracting herbal targets for Daehwang and disease targets for epilepsy from multiple databases. A protein-protein interaction network was built using the Search Tool for the Retrieval of Interacting Genes/Proteins (STRING) database, and pivotal targets were determined by topological analysis. Enrichment analysis was performed using the Database for Annotation, Visualization, and Integrated Discovery (DAVID) tool to elucidate the underlying mechanisms. RESULTS: The RTE formulation was found to contain sennoside A, sennoside B, chrysophanol, emodin, physcion, (+)-catechin, and quercetin-3-O-glucuronoid. RTE effectively inhibited TMT-induced seizures at 10, 30, and 100 mg/kg dosages and attenuated hippocampal neuronal decay and neuroinflammation at 30 and 100 mg/kg dosages. Furthermore, RTE significantly reduced mRNA levels of tumor necrosis factor (TNF-α), glial fibrillary acidic protein (GFAP), and c-fos in hippocampal tissues. Network analysis revealed TNF, Interleukin-1 beta (IL-1ß), Interleukin-6 (IL-6), Protein c-fos (FOS), RAC-alpha serine/threonine-protein kinase (AKT1), and Mammalian target of rapamycin (mTOR) as the core targets. Enrichment analysis demonstrated significant involvement of R. tanguticum components in neurodegeneration (p = 4.35 × 10-5) and TNF signaling pathway (p = 9.94 × 10-5). CONCLUSIONS: The in vivo and in silico analyses performed in this study suggests that RTE can potentially modulate TMT-induced epileptic seizures and neurodegeneration. Therefore, R. tanguticum root is a promising herbal treatment option for antiepileptic and neuroprotective applications.
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Anticonvulsivantes , Modelos Animales de Enfermedad , Epilepsia , Hipocampo , Fármacos Neuroprotectores , Extractos Vegetales , Raíces de Plantas , Rheum , Compuestos de Trimetilestaño , Animales , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/administración & dosificación , Extractos Vegetales/farmacología , Extractos Vegetales/administración & dosificación , Rheum/química , Raíces de Plantas/química , Masculino , Anticonvulsivantes/farmacología , Epilepsia/tratamiento farmacológico , Epilepsia/inducido químicamente , Hipocampo/efectos de los fármacos , Hipocampo/metabolismo , Enfermedades Neurodegenerativas/tratamiento farmacológico , Simulación por Computador , Farmacología en Red , Mapas de Interacción de Proteínas , RatasRESUMEN
BACKGROUND: Rheum palmatum, R. tanguticum, and R. officinale, integral species of the genus Rheum, are widely used across global temperate and subtropical regions. These species are incorporated in functional foods, medicines, and cosmetics, recognized for their substantial bioactive components. PURPOSE: This review aims to synthesize developments from 2014 to 2023 concerning the botanical characteristics, ethnopharmacology, nutritional values, chemical compositions, pharmacological activities, mechanisms of action, and toxicity of these species. METHODS: Data on the three Rheum species were gathered from a comprehensive review of peer-reviewed articles, patents, and clinical trials accessed through PubMed, Google Scholar, Web of Science, and CNKI. RESULTS: The aerial parts are nutritionally rich, providing essential amino acids, fatty acids, and minerals, suitable for use as health foods or supplements. Studies have identified 143 chemical compounds, including anthraquinones, anthrones, flavonoids, and chromones, which contribute to their broad pharmacological properties such as laxative, anti-diarrheal, neuroprotective, hepatoprotective, cardiovascular, antidiabetic, antitumor, anti-inflammatory, antiviral, and antibacterial effects. Notably, the materials science approach has enhanced understanding of their medicinal capabilities through the evaluation of bioactive compounds in different therapeutic contexts. CONCLUSION: As medicinal and economically significant herb species, Rheum species provide both edible aerial parts and medicinal underground components that offer substantial health benefits. These characteristics present new opportunities for developing nutritional ingredients and therapeutic products, bolstering the food and pharmaceutical industries.
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Fitoquímicos , Rheum , Etnofarmacología , Fitoquímicos/farmacología , Fitoquímicos/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Rheum/químicaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: The pathophysiological mechanism of thromboinflammation involves the intricate interplay between the inflammatory responses and coagulation cascades. Rhubarb is frequently used in traditional Chinese medicine to treat thromboinflammatory diseases. The scorched rhubarb (prepared by stir-baking the dried raw rhubarb till it partly turns to charcoal) is believed to possess enhanced blood-cooling and stasis-removing functions compared to the raw rhubarb, thereby augmenting the therapeutic effects on thromboinflammation. AIM OF THE STUDY: This study aimed to explore the chemical and pharmacological foundations of the scorch processing of rhubarb in order to ensure and enhance the efficacy and safety of the scorched rhubarb for treating thromboinflammatory diseases. MATERIALS AND METHODS: The dried raw rhubarb pieces were subjected to stir-baking at 180 °C for 10â¼80 min to obtain the rhubarbs with varying degrees of scorching. Typical ingredients present in rhubarb pieces and extracts were determined by high-performance liquid chromatography. The therapeutic effects of the raw and scorched rhubarb on thromboinflammation were evaluated using a rat model. Proteomics analysis was employed to screen potential biological pathways associated with thromboinflammation treatment by the raw and scorched rhubarb, which were further verified using a cell model. RESULTS: Morphological properties indicated that the rhubarb baked at 180 °C for 50 min in this research showed the optimal degree of scorching. Compared to the raw rhubarb, the properly scorched rhubarb exhibited lower levels of anthraquinone glucosides, higher levels of anthraquinone aglycones, superior anti-thromboinflammatory effects, and no purgative side effects. Proteomics analysis revealed that the complement and coagulation cascades pathway played a significant role in mediating the therapeutic effects of the raw and scorched rhubarb on thromboinflammation. Furthermore, it was found that anthraquinone aglycones were more effective than their glucoside counterparts in restoring the impaired vascular endothelial cells as well as regulating the complement and coagulation cascades pathway. CONCLUSIONS: Proper scorch processing may augment the therapeutic effects of rhubarb on thromboinflammation via relieving inflammation and oxidative stress, repairing vascular endothelial cells, restoring coagulation cascades and blood rheology, and regulating some other biological processes. This may be partly caused by the scorch-induced thermolysis of anthraquinone glucosides into their aglycone counterparts that seemed to perform better in regulating the complement and coagulation cascades pathway.
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Antraquinonas , Coagulación Sanguínea , Glucósidos , Ratas Sprague-Dawley , Rheum , Animales , Rheum/química , Antraquinonas/farmacología , Coagulación Sanguínea/efectos de los fármacos , Masculino , Glucósidos/farmacología , Glucósidos/química , Ratas , Inflamación/tratamiento farmacológico , Trombosis/tratamiento farmacológico , Antiinflamatorios/farmacología , Proteínas del Sistema Complemento/metabolismo , Modelos Animales de Enfermedad , Extractos Vegetales/farmacología , Extractos Vegetales/químicaRESUMEN
In this study, the collision induced dissociation tandem mass spectrometry (CID-MS/MS) fragmentation pathway of chemical components in rhubarb was wholly explored using 34 standards by UHPLC-QTOF-MS/MS in negative ion mode. In consequently, the diagnostic product ions for speedy screening and categorization of chemical components in rhubarb were ascertained based on their MS/MS splitting decomposition patterns and intensity analysis. According to these findings, a fresh two-step data mining strategy had set up. The initial key step involves the use of characteristic product ions and neutral loss to screen for different types of substituents and basic skeletons of compounds. The subsequent key step is to screen and classify different types of compounds based on their characteristic product ions. This method can be utilized for rapid research, classification, and identification of compounds in rhubarb. A total of 356 compounds were rapidly identified or tentatively characterized in three rhubarb species extracts, including 150 acylglucoside, 125 anthraquinone, 65 flavanols and 15 other compounds. This study manifests that the analytical strategy is feasible for the analysis of complex natural products in rhubarb.
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Antraquinonas , Rheum , Espectrometría de Masas en Tándem , Cromatografía Líquida de Alta Presión/métodos , Rheum/química , Espectrometría de Masas en Tándem/métodos , Antraquinonas/química , Antraquinonas/análisis , Extractos Vegetales/química , Extractos Vegetales/análisis , Glucósidos/análisis , Glucósidos/químicaRESUMEN
A method involving chitosan-assisted magnetic-stirring-enhanced mechanical amorphous dispersion extraction was developed and utilized to extract hydrophobic anthraquinones from Rhei Radix et Rhizoma prior to ultrahigh performance liquid chromatography analysis. Incorporating natural chitosan as a dispersant facilitated the extraction of hydrophobic anthraquinones using purified water, considerably enhancing the eco-friendliness of the extraction methodology. To optimize extraction efficiency, an extensive evaluation of the crucial parameters influencing rhubarb yield was conducted. Furthermore, a response surface methodology was applied to optimize the extraction conditions. Under these optimized conditions, the method exhibited linearity ranges of 0.1-100⯵g/mL, with correlation coefficients between 0.9990 and 0.9998. The method's intraday (n = 6) and interday (n = 6) precision levels were maintained at ≤3.58%, which was considered to be within acceptable limits. The computed detection and quantification limits were 16.54-24.60 and 54.91-82.04â¯ng/mL, respectively. Consequently, this optimized method was effectively employed to extract five specific compounds (aloe-emodin, emodin, rhein, chrysophanol, and physcion) from Rhei Radix et Rhizoma, achieving recoveries ranging from 86.43% to 102.75%.
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Antraquinonas , Interacciones Hidrofóbicas e Hidrofílicas , Plantas Medicinales , Rheum , Antraquinonas/química , Antraquinonas/análisis , Cromatografía Líquida de Alta Presión/métodos , Rheum/química , Plantas Medicinales/química , Quitosano/química , Fitoquímicos/química , Fitoquímicos/análisis , Fitoquímicos/aislamiento & purificación , Agua/química , Emodina/análogos & derivados , Emodina/química , Emodina/análisis , Límite de Detección , Extractos Vegetales/químicaRESUMEN
Rhei Radix et Rhizoma is common traditional Chinese medicine with multiple original plants. The content and proportion of the active components in Rhei Radix et Rhizoma from different plant species were compared to accurately evaluate the medicine qua-lity and provide a theoretical basis for precise use of this medicine in clinical practice. In this study, fresh Rhei Radix et Rhizoma samples were collected from the four-year-old plants of Rheum palmatum, R. tanguticum, and R. officinale. The relative content of 220 anthraquinones, anthrones, and tannins in the samples were determined by pseudo-targeted metabolomics, and the differential components were screened by multivariate statistical methods. The principal component analysis classified the samples into three clusters according to the original plants. The orthogonal partial least squares-discriminant analysis(OPLS-DA) screened out 117 differential components, including 8 free anthraquinones, 18 anthraquinone glycosides, 80 anthrones, and 11 tannins. Twenty-eight components had the highest content in R. tanguticum, mainly including sennosides, anthraquinone glycosides, and procyanidins. Thirty-five components showed the highest content in R. officinale, mainly including free anthraquinones and catechines. Fifty-four components showed the highest content in R. palmatum, mainly including dianthrones, while the structures of most of them cannot be determined temporarily. The content distribution of differential components in the three original plants indicates that R. tanguticum has the strongest effect of purging, while R. officinale has the strongest effect of clearing heat and purging fire, and both have stronger effects of resolvong stasis and dredging meridians than R. palmatum.
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Medicamentos Herbarios Chinos , Metabolómica , Rheum , Rizoma , Rheum/química , Rizoma/química , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/análisis , Antraquinonas/química , Antraquinonas/análisis , Cromatografía Líquida de Alta PresiónRESUMEN
This study compared the therapeutic difference effects of the raw and scorched rhubarb for the treatment of ulcerative colitis(UC) and explored their difference in chemical components and mechanisms by using ultra-high performance liquid chromatography-quadrupole-electrostatic field orbitrap high-resolution mass spectrometry(UPLC-QE-Orbitrap-MS) and network pharmacology. The UC therapeutic effects of Shaoyao Decoction with the raw rhubarb or the scorched rhubarb were evaluated by dextran sulfate sodium(DSS)-induced mouse model. The results showed that Shaoyao Decoction with either the raw rhubarb or the scorched rhubarb could relieve the UC symptoms of mice to different extents, while the scorched rhubarb-based formula showed advantages in reducing hemorrhagic diarrhea and inflammation levels. UPLC-QE-Orbitrap-MS was used to identify a total of 78 small molecules in the water decoction of the raw and scorched rhubarb. Multivariate statistical methods were used to screen components increasing significantly after the scorching process. The seven compounds included five free anthraquinones, gallic acid, and 5-hydroxymethylfurfural(HMF). Meanwhile, the nine compounds decreasing scorching were mainly combined anthraquinones and catechins-related compounds. Network pharmacology and molecular docking suggested that free anthraquinones, gallic acid, and 5-HMF may act on core targets such as B-cell lymphoma-2(BCL2), epidermal growth factor receptor(EGFR), tumor necrosis factor(TNF), and caspase-3(CASP3) and influence the signaling pathways such as phosphoinositide-3-kinase/protein kinase B(PI3K/Akt), hypoxia inducible factor-1(HIF-1), TNF, and mitogen-activated protein kinase(MAPK), so as to regulate the inflammation response, oxidative stress, and cell apoptosis to relieve UC symptoms. This study compared the therapeutic effects and chemical components of the raw and scorched rhubarb, providing the clinical reference for using rhubarb to treat UC.
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Colitis Ulcerosa , Medicamentos Herbarios Chinos , Espectrometría de Masas , Farmacología en Red , Rheum , Rheum/química , Animales , Colitis Ulcerosa/tratamiento farmacológico , Ratones , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/farmacología , Cromatografía Líquida de Alta Presión/métodos , Masculino , HumanosRESUMEN
In this study, J774A.1 macrophages stimulated by lipopolysaccharide(LPS) and adenosine triphosphate(ATP) were used to establish an in vitro model of pyroptosis, and the intervention mechanism of free total rhubarb anthraquinones(FTRAs) on pyroptosis was investigated. J774A.1 macrophages were cultured in vitro, and the experiment was assigned to the control group and groups with different concentrations of LPS(0.25, 0.5, and 1 µg·mL~(-1)) and ATP(1.25, 2.5, and 5 mmol·L~(-1)). An in vitro model of macrophage pyroptosis was established by detecting cell viability through CCK-8, propidium iodide(PI) apoptotic cell staining, lactate dehydrogenase(LDH), interleukin(IL)-18, and tumor necrosis factor(TNF)-α release. Then, J774A.1 macrophages were randomly divided into six groups: blank control group, LPS+ATP group, high-dose FTRA group, and low, medium, and high-dose FTRA pre-protection group. The phenotypic characteristics and key indicators of pyroptosis were detected as the basis for evaluating the effect of FTRAs on pyroptosis induced by LPS and ATP. Western blot and RT-PCR were used to detect the expression levels of protein and mRNA related to the pyroptosis pathway in caspase-1/11 and elucidate the molecular mechanism of the anti-pyroptosis effect. The results showed that the stimulation condition of 0.50 µg·mL~(-1) LPS+5.00 mmol·L~(-1) ATP was the most effective in the in vitro model of macrophage pyroptosis. FTRAs pre-protected cells for 24 h and then can increase cell viability under pyroptosis conditions, alleviate cell damage, lower the positive rate of PI staining, and reduce the release of LDH, IL-18, and TNF-α. FTRAs were able to significantly inhibit the activation of GSDMD proteins and significantly down-regulate the protein expression of the pyroptosis pathway signature molecules, TLR4, NLRP3, cleaved-caspase-1, and cleaved-caspase-11, but they had no significant effect on ASC proteins. FTRAs were also able to significantly inhibit the mRNA expression of caspase-1, caspase-11, and GSDMD. These results indicate that FTRAs have an inhibitory effect on the pyroptosis model induced by LPS and ATP and play an anti-pyroptosis effect by regulating classical and non-classical pyroptosis signaling pathways and reducing the production of inflammatory cytokines.
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Antraquinonas , Macrófagos , Piroptosis , Rheum , Piroptosis/efectos de los fármacos , Rheum/química , Animales , Ratones , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Macrófagos/citología , Antraquinonas/farmacología , Antraquinonas/química , Línea Celular , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/química , Adenosina Trifosfato/metabolismo , Factor de Necrosis Tumoral alfa/genética , Factor de Necrosis Tumoral alfa/metabolismo , Lipopolisacáridos/farmacología , Supervivencia Celular/efectos de los fármacos , Interleucina-18/genética , Interleucina-18/metabolismoRESUMEN
The mechanism by which DNMT3B facilitates esophageal cancer (ESCA) progression is currently unknown, despite its association with adverse prognoses in several cancer types. To investigate the potential therapeutic effects of the Chinese herbal medicine rhubarb on esophageal cancer (ESCA), we adopted an integrated bioinformatics approach. Gene Set Enrichment Analysis (GSEA) was first utilized to screen active anti-ESCA components in rhubarb. We then employed Weighted Gene Co-expression Network Analysis (WGCNA) to identify key molecular modules and targets related to the active components and ESCA pathogenesis. This system-level strategy integrating multi-omics data provides a powerful means to unravel the molecular mechanisms underlying the anticancer activities of natural products, like rhubarb. To investigate module gene functional enrichment, Gene Ontology (GO), and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyses were conducted. In addition, we evaluated the predictive impact of DNMT3B expression on ESCA patients utilizing the Kaplan-Meier method. Finally, we conducted experiments on cell proliferation and the cell cycle to explore the biological roles of DNMT3B. In this study, we identified Rhein as the main active ingredient of rhubarb that exhibited significant anti-ESCA activity. Rhein markedly suppressed ESCA cell proliferation. Utilizing Weighted Gene Co-expression Network Analysis (WGCNA) and Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis, we determined that the blue module was associated with Rhein target genes and the cell cycle. Additionally, DNMT3B was identified as a Rhein target gene. Analysis of The Cancer Genome Atlas (TCGA) database revealed that higher DNMT3B levels were associated with poor prognosis in ESCA patients. Furthermore, Rhein partially reversed the overexpression of DNMT3B to inhibit ESCA cell proliferation. In vitro studies demonstrated that Rhein and DNMT3B inhibition disrupted the S phase of the cell cycle and affected the production of cell cycle-related proteins. In this study, we found that Rhein exerts its anti-proliferative effects in ESCA cells by targeting DNMT3B and regulating the cell cycle.
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Antraquinonas , Ciclo Celular , Proliferación Celular , ADN (Citosina-5-)-Metiltransferasas , ADN Metiltransferasa 3B , Neoplasias Esofágicas , Humanos , Antraquinonas/farmacología , Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Biología Computacional , ADN (Citosina-5-)-Metiltransferasas/genética , ADN (Citosina-5-)-Metiltransferasas/metabolismo , Neoplasias Esofágicas/genética , Neoplasias Esofágicas/tratamiento farmacológico , Neoplasias Esofágicas/patología , Neoplasias Esofágicas/metabolismo , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos , Rheum/químicaRESUMEN
Rhubarb is widely used in health care, but causing a great amount of rhein-containing herbal residue. Rhein with several toxicities might pollute environment, damage ecology and even hazard human health if left untreated. In this study, the degradation effects of bisulfite- (BS) and peroxymonosulfate- (PMS) based oxidation systems on rhein in rhubarb residue were compared and investigated. The effects of BS and PMS with two valence states of ferric ion (Fe) on the degradation of rhein in rhubarb residue were optimized for the selection of optimal oxidation system. The influences of reaction temperature, reaction time and initial pH on the removal of rhein under the optimal oxidation system were evaluated. The chemical profiles of rhubarb residue with and without oxidation process were compared by UPLC-QTOF-MS/MS, and the degradation effects were investigated by PLS-DA and S plot/OPLS-DA analysis. The results manifested that PMS showed relative higher efficiency than BS on the degradation of rhein. Moreover, Fe(III) promoted the degradation effect of PMS, demonstrated that Fe(III)/PMS is the optimal oxidation system to degrade rhein in rhubarb residue. Further studies indicated that the degradation of rhein by the Fe(III)/PMS oxidation system was accelerated with the prolong of reaction time and the elevation of reaction temperature, and also affected by the initial pH. More importantly, Fe(III)/PMS oxidation system could degrade rhein in rhubarb residue completely under the optimal conditions. In conclusion, Fe(III)/PMS oxidation system is a feasible method to treat rhein in rhubarb residue.
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Antraquinonas , Oxidación-Reducción , Peróxidos , Rheum , Antraquinonas/química , Rheum/química , Peróxidos/química , Espectrometría de Masas en Tándem , Sulfitos/química , Concentración de Iones de Hidrógeno , Compuestos Férricos/química , TemperaturaRESUMEN
BACKGROUND: Pancreatitis is a common exocrine inflammatory disease of the pancreas and lacks specific medication currently. Rhei Radix et Rhizoma (RR) and its anthraquinone derivatives (AQs) have been successively reported for their pharmacological effects and molecular mechanisms in experimental and clinical pancreatitis. However, an overview of the anti-pancreatitis potential of RR and its AQs is limited. PURPOSE: To summarize and analyze the pharmacological effects of RR and its AQs on pancreatitis and the underlying mechanisms, and discuss their drug-like properties and future perspectives. METHODS: The articles related to RR and its AQs were collected from the Chinese National Knowledge Infrastructure, Wanfang data, PubMed, and the Web of Science using relevant keywords from the study's inception until April first, 2024. Studies involving RR or its AQs in cell or animal pancreatitis models as well as structure-activity relationship, pharmacokinetics, toxicology, and clinical trials were included. RESULTS: Most experimental studies are based on severe acute pancreatitis rat models and a few on chronic pancreatitis. Several bioactive anthraquinone derivatives of Rhei Radix et Rhizoma (RRAQs) exert local protective effects on the pancreas by maintaining pancreatic acinar cell homeostasis, inhibiting inflammatory signaling, and anti-fibrosis, and they improve systemic organ function by alleviating intestinal and lung injury. Pharmacokinetic and toxicity studies have revealed the low bioavailability and wide distribution of RRAQs, as well as hepatotoxicity and nephrotoxicity. However, there is insufficient research on the clinical application of RRAQs in pancreatitis. Furthermore, we propose effective strategies for subsequent improvement in terms of balancing effectiveness and safety. CONCLUSION: RRAQs can be developed as either candidate drugs or novel lead structures for pancreatitis treatment. The comprehensive review of RR and its AQs provides references for optimizing drugs, developing therapies, and conducting future studies on pancreatitis.
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Antraquinonas , Pancreatitis , Rheum , Antraquinonas/farmacología , Antraquinonas/química , Antraquinonas/uso terapéutico , Animales , Rheum/química , Humanos , Pancreatitis/tratamiento farmacológico , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/uso terapéutico , Rizoma/química , Páncreas/efectos de los fármacos , Relación Estructura-Actividad , Ratas , Modelos Animales de EnfermedadRESUMEN
Ischemic stroke (IS) has attracted worldwide attention due to the high mortality and disability rate. Raw rhubarb (RR) is a traditional medicinal plant and whole-food that has been used in China for its various pharmacological activities, such as antioxidant and anti-inflammatory properties. Recent pharmacological research has shown the role of RR against IS, but its mechanism of action remains unclear, particularly in the context of the brain-gut axis. To address this gap in knowledge, the present study was conducted in the middle cerebral artery occlusion/reperfusion (MCAO/R) model with the aim of investigating the effects of RR on regulating the intestinal microbiota barrier and metabolism and thereby reducing inflammatory response so as to improve the IS. The results showed that pre-treatment of RR attenuated cerebral infarct area and inflammation response in MCAO rats. Furthermore, RR also improved intestinal barrier function, including the integrity and permeability of the intestinal barrier. Additionally, RR intervention significantly attenuated gut microbiota dysbiosis caused by ischemic stroke, especially the increased Firmicutes. Notably, the pseudo-germ-free (PGF) rats further demonstrated that the anti-stroke effect of RR might rely on intestinal microbiota. In addition, the UPLC/Q-Orbitrap-MS-Based metabolomics revealed the disrupted metabolic profiles caused by MCAO/R, and a total of 11 differential metabolites were modulated by RR administration, especially bile acids. Further correlation analysis and network pharmacology analysis also demonstrated a strong association between specific bacteria, such as Firmicutes and bile acids. In conclusion, our work demonstrated that RR could effectively ameliorate ischemic stroke by modulating the microbiota and metabolic disorders.