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1.
Molecules ; 29(13)2024 Jun 23.
Artículo en Inglés | MEDLINE | ID: mdl-38998935

RESUMEN

This article systematically reviews the extraction and purification methods, structural characteristics, structure-activity relationship, and health benefits of C. speciosa polysaccharides, and their potential application in food, medicine, functional products, and feed, in order to provide a useful reference for future research. Chaenomeles speciosa (Sweet) Nakai. has attracted the attention of health consumers and medical researchers as a traditional Chinese medicine with edible, medicinal, and nutritional benefits. According to this study, C. speciosa polysaccharides have significant health benefits, such as anti-diaetic, anti-inflammatory and analgesic, anti-tumor, and immunomodulatory effects. Researchers determined the molecular weight, structural characteristics, and monosaccharide composition and ratio of C. speciosa polysaccharides by water extraction and alcohol precipitation. This study will lay a solid foundation for further optimization of the extraction process of C. speciosa polysaccharides and the development of their products. As an active ingredient with high value, C. speciosa polysaccharides are worthy of further study and full development. C. speciosa polysaccharides should be further explored in the future, to innovate their extraction methods, enrich their types and biological activities, and lay a solid foundation for further research and development of products containing polysaccharides that are beneficial to the human body.


Asunto(s)
Polisacáridos , Polisacáridos/química , Polisacáridos/aislamiento & purificación , Polisacáridos/farmacología , Humanos , Extractos Vegetales/química , Extractos Vegetales/farmacología , Extractos Vegetales/aislamiento & purificación , Rosaceae/química , Antiinflamatorios/química , Antiinflamatorios/farmacología , Antiinflamatorios/aislamiento & purificación , Medicina Tradicional China , Monosacáridos/química , Monosacáridos/análisis , Relación Estructura-Actividad , Animales
2.
Molecules ; 29(13)2024 Jun 27.
Artículo en Inglés | MEDLINE | ID: mdl-38998999

RESUMEN

Phellinus is a precious perennial medicinal fungus. Its polysaccharides are important bioactive components, and their chemical composition is complex. The polysaccharides are mainly extracted from the fruiting body and mycelium. The yield of the polysaccharides is dependent on the extraction method. They have many pharmacological activities, such as antitumor, immunomodulatory, antioxidant, hypoglycemic, anti-inflammatory, etc. They are also reported to show minor toxic and side effects. Many studies have reported the anticancer activity of Phellinus polysaccharides. This review paper provides a comprehensive examination of the current methodologies for the extraction and purification of Phellinus polysaccharides. Additionally, it delves into the structural characteristics, pharmacological activities, and mechanisms of action of these polysaccharides. The primary aim of this review is to offer a valuable resource for researchers, facilitating further studies on Phellinus polysaccharides and their potential applications.


Asunto(s)
Polisacáridos Fúngicos , Humanos , Polisacáridos Fúngicos/química , Polisacáridos Fúngicos/farmacología , Polisacáridos Fúngicos/aislamiento & purificación , Basidiomycota/química , Polisacáridos/química , Polisacáridos/farmacología , Polisacáridos/aislamiento & purificación , Antioxidantes/farmacología , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Antineoplásicos/farmacología , Antineoplásicos/química , Antineoplásicos/aislamiento & purificación , Hipoglucemiantes/farmacología , Hipoglucemiantes/química , Hipoglucemiantes/aislamiento & purificación , Animales , Phellinus/química
3.
Pharm Biol ; 62(1): 563-576, 2024 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-39021070

RESUMEN

CONTEXT: Virtually all parts of Salvadora persica L. (Salvadoraceae) are used in traditional medicine. The twigs and leaves are used for oral health, but leaves are far less investigated. OBJECTIVE: This study assesses the oral health-promoting potential of S. persica leaves with emphasis on anti-inflammatory and antiproliferative effects and provides an in depth-characterization of their metabolite profile. MATERIALS AND METHODS: Hot-water and methanolic S. persica leaf extracts (1, 10, and 100 µg/mL) and their major constituents (5, 10, and 50 µM), were subjected to cellular assays on IL-8 and TNFα release in LPS-stimulated human neutrophils, NO-release in LPS/IFNγ stimulated mouse macrophages, and proliferation of HNO97 human tongue carcinoma cells. Metabolite profiling was performed by UHPLC-HRMS analysis. Major constituents were isolated and structurally elucidated. RESULTS AND DISCUSSION: Both extracts showed pronounced anti-inflammatory activity in LPS-stimulated neutrophils. Major identified compound classes were flavonoid glycosides, the glucosinolate glucotropaeolin, phenyl- and benzylglycoside sulfates, and megastigmane glycosylsulfates, the latter ones identified for the first time in S. persica. Glucotropaeolin strongly inhibited the release of IL-8 and TNF-α (13.3 ± 2.0 and 22.7 ± 2.6% of the release of stimulated control cells at 50 µM), while some flavonoids and 3-(3'-O-sulfo-ß-d-glucopyranosyloxy)-7,8-dihydro-ß-ionone, a newly isolated megastigmane glycosylsulfate, were moderately active. Benzylisothiocyanate, which is likely formed from glucotropaeolin during traditional application of S. persica, showed considerable antiproliferative activity (IC50 in HNO97 cells: 10.19 ± 0.72 µM) besides strongly inhibiting IL-8 and TNFα release. CONCLUSIONS: Glucotropaeolin and benzylisothiocyanate are likely implicated in the oral health-promoting effects of S. persica leaves. The chemistry and pharmacology of the newly identified megastigmane glycosylsulfates should be further evaluated.


Asunto(s)
Antiinflamatorios , Mediadores de Inflamación , Neutrófilos , Enfermedades Periodontales , Extractos Vegetales , Hojas de la Planta , Salvadoraceae , Humanos , Extractos Vegetales/farmacología , Extractos Vegetales/aislamiento & purificación , Animales , Ratones , Antiinflamatorios/farmacología , Antiinflamatorios/aislamiento & purificación , Salvadoraceae/química , Mediadores de Inflamación/metabolismo , Mediadores de Inflamación/antagonistas & inhibidores , Enfermedades Periodontales/tratamiento farmacológico , Neutrófilos/efectos de los fármacos , Neutrófilos/metabolismo , Proliferación Celular/efectos de los fármacos , Línea Celular Tumoral , Factor de Necrosis Tumoral alfa/metabolismo , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Relación Dosis-Respuesta a Droga , Células RAW 264.7 , Interleucina-8/metabolismo , Fitoquímicos/farmacología , Fitoquímicos/aislamiento & purificación
4.
Chin J Nat Med ; 22(7): 643-653, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-39059833

RESUMEN

The resin of Ferula sinkiangensis has been traditionally utilized for treating gastrointestinal disorders, inflammation, tumors, various cancers, and alopecia areata. The primary bioactive constituents, sesquiterpene coumarins, have demonstrated notable therapeutic potential against neuroinflammation. In this study, a structure-guided fractionation method was used to isolate nine novel sesquiterpene coumarins from the resin of F. sinkiangensis. These compounds were characterized and structurally elucidated using comprehensive physicochemical and spectroscopic techniques, including calculated electronic circular dichroism (ECD). Anti-neuroinflammatory assays revealed that compounds 2, 3, and 6 significantly inhibited nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated BV2 microglial cells, with IC50 values ranging from 1.63 to 12.25 µmol·L-1.


Asunto(s)
Antiinflamatorios , Cumarinas , Ferula , Microglía , Óxido Nítrico , Sesquiterpenos , Ferula/química , Cumarinas/farmacología , Cumarinas/aislamiento & purificación , Cumarinas/química , Sesquiterpenos/farmacología , Sesquiterpenos/química , Sesquiterpenos/aislamiento & purificación , Microglía/efectos de los fármacos , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Estructura Molecular , Animales , Ratones , Línea Celular , Lipopolisacáridos/farmacología , Resinas de Plantas/química , Extractos Vegetales/farmacología , Extractos Vegetales/química
5.
Biomed Pharmacother ; 177: 117072, 2024 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-38991301

RESUMEN

The development of natural substances derived from nature poses a significant challenge as technologies for the extraction and characterization of active principles advance. Hispolon has received a lot of attention in recent years, ascribable to its wide range of biological activities. It is a phenolic molecule that was extracted from several mushroom species such as Phellinus igniarius, Phellinus linteus, Phellinus lonicerinus, Phellinus merrillii, and Inonotus hispidus. To provide a comprehensive overview of the pharmacological activities of hispolon, this review highlights its anticancer, anti-inflammatory, antioxidant, antibacterial, and anti-diabetic activities. Several scientific research databases, including Google Scholar, Web of Science, PubMed, SciFinder, SpringerLink, Science Direct, Scopus, and, Wiley Online were used to gather the data on hispolon until May 2024. The in vitro and in vivo studies have revealed that hispolon exhibited significant anticancer properties through modifying several signaling pathways including cell apoptosis, cycle arrest, autophagy, and inhibition of angiogenesis and metastasis. Hispolon's antimicrobial activity was proven against many bacterial, fungal, and viral pathogens, highlighting its potential use as a novel antimicrobial agent. Additionally, hispolon displayed potent anti-inflammatory activity through the suppression of key inflammatory mediators, such as inducible NO synthase (iNOS), tumor necrosis factor-α (TNF-α), and cyclooxygenases-2 (COX-2), and the modulation of mitogen-activated protein kinases (MAPK) and nuclear factor kappa B (NF-κB) signaling pathways. The antioxidant potential of hispolon was attributed to its capacity to neutralize reactive oxygen species (ROS) and to increase the activity of antioxidant enzymes, indicating a possible involvement in the prevention of oxidative stress-related illnesses. Hispolon's antidiabetic activity was associated with the inhibition of aldose reductase and α-glucosidase. Studies on hispolon emphasized its potential use as a promising scaffold for the development of novel therapeutic agents targeting various diseases, including cancer, infectious diseases, inflammatory disorders, and diabetes.


Asunto(s)
Antiinflamatorios , Antineoplásicos , Antioxidantes , Animales , Humanos , Antiinflamatorios/farmacología , Antiinflamatorios/aislamiento & purificación , Antioxidantes/farmacología , Antioxidantes/aislamiento & purificación , Antineoplásicos/farmacología , Antineoplásicos/aislamiento & purificación , Hipoglucemiantes/farmacología , Hipoglucemiantes/aislamiento & purificación , Iminoazúcares/farmacología , Iminoazúcares/química , Transducción de Señal/efectos de los fármacos , Catecoles
6.
J Nat Prod ; 87(7): 1817-1825, 2024 Jul 26.
Artículo en Inglés | MEDLINE | ID: mdl-38964296

RESUMEN

Our ongoing exploration of Australian rainforest plants for the biodiscovery of anti-inflammatory agents led to the isolation and structural elucidation of eight new arylalkenyl α,ß-unsaturated-δ-lactones, triplinones A-H (1-8), from the leaves of the Australian rainforest plant Cryptocarya triplinervis B. Hyland (Lauraceae). The chemical structures of these compounds were established by NMR spectroscopic data analysis, while their relative and absolute configurations were established using a combination of Mosher ester analysis utilizing both Riguera's and Kishi's methods, ECD experiments, and X-ray crystallography analysis. Compounds 1-8 exhibited good inhibitory activities toward nitric oxide (NO) production in lipopolysaccharide (LPS) and interferon (IFN)-γ induced RAW 264.7 macrophages, in particular compounds 1-3 and 5, with IC50 values of 7.3 ± 0.5, 6.0 ± 0.3, 5.6 ± 0.3, and 5.4 ± 2.5 µM, respectively.


Asunto(s)
Antiinflamatorios , Cryptocarya , Lactonas , Óxido Nítrico , Hojas de la Planta , Bosque Lluvioso , Hojas de la Planta/química , Ratones , Animales , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Australia , Células RAW 264.7 , Estructura Molecular , Lactonas/farmacología , Lactonas/química , Lactonas/aislamiento & purificación , Óxido Nítrico/biosíntesis , Óxido Nítrico/antagonistas & inhibidores , Cryptocarya/química , Lipopolisacáridos/farmacología , Macrófagos/efectos de los fármacos , Cristalografía por Rayos X
7.
Biomed Pharmacother ; 177: 117163, 2024 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-39018876

RESUMEN

Graveoline exhibits various biological activities. However, only limited studies have focused on its hepatoprotective properties. This study evaluated the anti-inflammatory and hepatoprotective activities of graveoline, a minor 2-phenylquinolin-4-one alkaloid isolated from Ruta graveolens L., in a liver injury model in vitro and in vivo. A network pharmacology approach was used to investigate the potential signaling pathway associated with the hepatoprotective activity of graveoline. Subsequently, biological experiments were conducted to validate the findings. Topological analysis of the KEGG pathway enrichment revealed that graveoline mediates its hepatoprotective activity through genes associated with the hepatitis B viral infection pathway. Biological experiments demonstrated that graveoline effectively reduced the levels of alanine transaminase and aspartate transaminase in lipopolysaccharide (LPS)-induced HepG2 cells. Graveoline exerted antihepatitic activity by inhibiting the pro-inflammatory cytokine tumor necrosis factor-α (TNF-α) and elevated the anti-inflammatory cytokines interleukin-4 (IL-4) and interleukin-10 (IL-10) in vitro and in vivo. Additionally, graveoline exerted its hepatoprotective activity by inhibiting JAK1 and STAT3 phosphorylation both in vitro and in vivo. In summary, graveoline can attenuate acute liver injury by inhibiting the TNF-α inflammasome, activating IL-4 and IL-10, and suppressing the JAK1/STAT3 signaling pathway. This study sheds light on the potential of graveoline as a promising therapeutic agent for treating liver injury.


Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas , Galactosamina , Janus Quinasa 1 , Lipopolisacáridos , Factor de Transcripción STAT3 , Transducción de Señal , Factor de Transcripción STAT3/metabolismo , Janus Quinasa 1/metabolismo , Janus Quinasa 1/antagonistas & inhibidores , Animales , Humanos , Lipopolisacáridos/toxicidad , Transducción de Señal/efectos de los fármacos , Enfermedad Hepática Inducida por Sustancias y Drogas/metabolismo , Enfermedad Hepática Inducida por Sustancias y Drogas/prevención & control , Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Masculino , Células Hep G2 , Galactosamina/toxicidad , Ratones , Antiinflamatorios/farmacología , Antiinflamatorios/aislamiento & purificación , Citocinas/metabolismo , Quinolinas/farmacología
8.
Molecules ; 29(11)2024 Jun 05.
Artículo en Inglés | MEDLINE | ID: mdl-38893558

RESUMEN

Polysaccharides have been assessed as a potential natural active component in Chinese herbal medicine with anti-inflammatory properties. However, the complex and indefinite structures of polysaccharides limit their applications. This study explains the structures and anti-inflammatory potentials of three neutral polysaccharides, RIP-A1 (Mw 1.8 × 104 Da), RIP-B1 (Mw 7.4 × 104 Da) and RIP-B2 (Mw 9.3 × 104 Da), which were isolated from the roots of Isatis indigotica Fort. with sequenced ultrafiltration membrane columns, DEAE-52 and Sephadex G-100. The planar structures and microstructures of RIP-A1, RIP-B1 and RIP-B2 were further determined by HPGPC, GC-MS, methylation analysis, FT-IR, SEM and AFM, in which the structure of RIP-A1 was elucidated in detail using 1D/2D NMR. The Raw 264.7 cells were used for the anti-inflammatory activity in vitro. The results showed that RIP-A1, RIP-B1 and RIP-B2 are all neutral polysaccharides, with RIP-A1 having the smallest Mw and the simplest monosaccharide composition of the three. RIP-A1 is mainly composed of Ara and Gal, except for a small quantity of Rha. Its main structure is covered with glycosidic linkages of T-α-Araf, 1,2-α-Rhap, 1,5-α-Araf, T-ß-Galp, 1,2,4-α-Rhap, 1,3,5-α-Araf and 1,6-ß-Galp with 0.33:0.12:1.02:0.09:0.45:11.41:10.23. RIP-A1 significantly inhibited pro-inflammatory cytokines (NO, TNF-α, IL-6 and IL-1ß) and increased anti-inflammatory cytokines (IL-4) in LPS-stimulated RAW 264.7 cells. Moreover, RIP-A1 could significantly inhibit the mRNA expression of TNF-α, IL-6 and L-1ß. It could also activate IKK, p65 and IκBα (the components of the NF-κB signaling pathway). In conclusion, the above results show the structural characterization and anti-inflammatory potentials of RIP-A1 as an effective natural anti-inflammatory drug.


Asunto(s)
Antiinflamatorios , Isatis , Raíces de Plantas , Polisacáridos , Ratones , Animales , Raíces de Plantas/química , Polisacáridos/química , Polisacáridos/farmacología , Polisacáridos/aislamiento & purificación , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Isatis/química , Células RAW 264.7 , FN-kappa B/metabolismo , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Citocinas/metabolismo
9.
Int J Biol Macromol ; 272(Pt 1): 132861, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38838884

RESUMEN

Semen Coicis (S. Coicis) has been regarded as a valuable source of traditional herbal medicine in China for thousands of years. S. Coicis polysaccharides (SCPs) are one of the most important bioactive ingredients of S. Coicis, which have attracted worldwide attention, because of their great marketing potential and development prospects. Hot water extraction is currently the most commonly used method to isolate SCPs. The structural characteristics of SCPs have been extensively investigated through various advanced modern analytical techniques to dissect the structure-activity relationships. SCPs are mainly composed of diverse monosaccharides, from which Rha and Ara are the most prevalent glycosyl groups. In addition, the structures of SCPs are found to be closely related to their multiple biological activities, including antioxidant activity, immunomodulatory function, antitumor activity, hypoglycemic effect, intestinal microbiota regulatory activity, anti-inflammatory activity, among others. In view of this, this review aimed to provide systematic and current information on the isolation, structural characteristics, and bioactivities of SCPs to support their future applications as therapeutic agents and functional foods.


Asunto(s)
Polisacáridos , Polisacáridos/química , Polisacáridos/farmacología , Polisacáridos/aislamiento & purificación , Antioxidantes/farmacología , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Humanos , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Animales , Relación Estructura-Actividad , Monosacáridos/análisis , Monosacáridos/química , Factores Inmunológicos/farmacología , Factores Inmunológicos/química , Factores Inmunológicos/aislamiento & purificación
10.
Mar Drugs ; 22(6)2024 May 22.
Artículo en Inglés | MEDLINE | ID: mdl-38921546

RESUMEN

Neurodegenerative diseases involve neuroinflammation and a loss of neurons, leading to disability and death. Hence, the research into new therapies has been focused on the modulation of the inflammatory response mainly by microglia/macrophages. The extracts and metabolites of marine sponges have been presented as anti-inflammatory. This study evaluated the toxicity of an extract and purified compound from the Brazilian marine sponge Aplysina fulva as well as its neuroprotection against inflammatory damage associated with the modulation of microglia response. PC12 neuronal cells and neonatal rat microglia were treated with the methanolic extract of A. fulva (AF-MeOH, 0.1-200 µg/mL) or with its purified dimethyl ketal of 3,5-dibromoverongiaquinol (AF-H1, 0.1-100 µM). Cytotoxicity was determined by MTT tetrazolium, Trypan blue, and propidium iodide; microglia were also treated with the conditioned medium (CM) from PC12 cells in different conditions. The microglia phenotype was determined by the expression of Iba-1 and CD68. AF-MeOH and AF-H1 were not toxic to PC12 or the microglia. Inflammatory damage with Escherichia coli lipopolysaccharide (LPS, 5 µg/mL) was not observed in the PC12 cells treated with AF-MeOH (1-10 µg/mL) or AF-H1 (1-10 µM). Microglia subjected to the CM from PC12 cells treated with LPS and AF-MeOH or AF-H1 showed the control phenotype-like (multipolar, low-CD68), highlighting the anti-neuroinflammatory and neuroprotective effect of components of this marine sponge.


Asunto(s)
Microglía , Fármacos Neuroprotectores , Poríferos , Animales , Microglía/efectos de los fármacos , Ratas , Poríferos/química , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/química , Células PC12 , Brasil , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Hidrocarburos Bromados/farmacología , Inflamación/tratamiento farmacológico
11.
Phytochemistry ; 225: 114191, 2024 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-38901625

RESUMEN

Herein, 17 previously undescribed polyacetylenes and 9 known ones were isolated from Tridax procumbens L. Their structures were identified using spectroscopic techniques (NMR, UV, IR, MS and optical rotation), the modified Mosher method, electronic circular dichroism (ECD) data and ECD calculation. The cytotoxicity of polyacetylenes on six human tumour cell lines (K562, K562/ADR, AGS, MGC-803, SPC-A-1 and MDA-MB-231) was evaluated. (3S,10R)-tridaxin B (2a), (3S,10S)-tridaxin B (2b) and tridaxin F (8) demonstrated substantial cytotoxic effects against the K562 cell line, with half-maximal inhibitory concentration (IC50) values of 2.62, 14.43 and 17.91 µM, respectively. Cell and nucleus morphology assessments and Western blot analysis confirmed that the cytotoxicity of the three polyacetylenes on K562 cells was mediated through a dose-dependent apoptosis pathway. Furthermore, (3S,10R)-tridaxin A (1a) and tridaxin G (9) exhibited considerable inhibitory effects on lipopolysaccharide-stimulated nitric oxide production in RAW 264.7 macrophages, with IC50 values of 15.92 and 20.35 µM, respectively. Further investigations revealed that 9 exerted anti-inflammatory activities by impeding the nuclear translocation of NF-κB and down-regulating the expression of pro-inflammatory factors, including those of iNOS, COX-2, IL-1ß and IL-6, in a concentration-dependent manner. The study provides evidence that polyacetylenes from T. procumbens may serve as a potential source of anti-tumour or anti-inflammatory agents for treating related diseases.


Asunto(s)
Antiinflamatorios , Antineoplásicos Fitogénicos , Poliinos , Humanos , Poliinos/farmacología , Poliinos/química , Poliinos/aislamiento & purificación , Ratones , Antineoplásicos Fitogénicos/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Animales , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Apoptosis/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Células RAW 264.7 , Estructura Molecular , Relación Dosis-Respuesta a Droga , Lipopolisacáridos/farmacología , Lipopolisacáridos/antagonistas & inhibidores , Asteraceae/química , Células K562 , Relación Estructura-Actividad , Proliferación Celular/efectos de los fármacos , Óxido Nítrico/antagonistas & inhibidores , Óxido Nítrico/biosíntesis , FN-kappa B/metabolismo , FN-kappa B/antagonistas & inhibidores , Línea Celular Tumoral
12.
Phytochemistry ; 225: 114170, 2024 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-38830388

RESUMEN

Eleven alkaloids including four previously undescribed oxoisoaporphine alkaloids, menisoxoisoaporphines A-D (1-4), four known analogues (5-8), and three aporphine alkaloids (9-11), were isolated and identified from the rhizomes of Menispermum dauricum. Their structures were elucidated by extensive spectroscopic data and single-crystal X-ray diffraction analyses. Among them, compounds 1 and 4 were the first samples of oxoisoaporphine with C-6 isopentylamino moiety, and 2 was a rare C-4 methylation product of oxoisoaporphine alkaloid. The in vitro anti-inflammatory activity of compounds 1-11 was performed by evaluating the inhibition of NO level in LPS-induced RAW264.7 macrophages. Among them, compound 4 exhibited the most potent NO inhibition activity with an IC50 value of 1.95 ± 0.33 µM. The key structure-activity relationships of those oxoisoaporphine alkaloids for anti-inflammatory effects have been summarized.


Asunto(s)
Alcaloides , Aporfinas , Menispermum , Óxido Nítrico , Ratones , Células RAW 264.7 , Animales , Relación Estructura-Actividad , Alcaloides/farmacología , Alcaloides/química , Alcaloides/aislamiento & purificación , Estructura Molecular , Óxido Nítrico/antagonistas & inhibidores , Óxido Nítrico/biosíntesis , Menispermum/química , Aporfinas/farmacología , Aporfinas/química , Aporfinas/aislamiento & purificación , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Lipopolisacáridos/farmacología , Lipopolisacáridos/antagonistas & inhibidores , Relación Dosis-Respuesta a Droga , Antiinflamatorios no Esteroideos/farmacología , Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/aislamiento & purificación , Macrófagos/efectos de los fármacos
13.
Phytochemistry ; 225: 114188, 2024 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-38878943

RESUMEN

Phytochemical investigation on the fruits of Cydonia oblonga Mill., a traditional Uighur medicine, led to the isolation of seven undescribed and nine known megastigmane glycosides. Their structures including absolute configurations were characterized by an extensive analysis of spectroscopic data including HRESIMS and NMR, combined with ECD calculations. Additionally, compounds 1, 2, 4, and 6-16 exhibited anti-inflammatory activity by inhibiting the secretion of cytokines TNF-α and IL-6 in RAW264.7 cells induced by lipopolysaccharides (LPS) with inhibitory rates of 10.79%-44.58% at 20 µM.


Asunto(s)
Ciclohexanonas , Glicósidos , Lipopolisacáridos , Norisoprenoides , Norisoprenoides/química , Norisoprenoides/farmacología , Norisoprenoides/aislamiento & purificación , Ratones , Glicósidos/química , Glicósidos/aislamiento & purificación , Glicósidos/farmacología , Células RAW 264.7 , Animales , Ciclohexanonas/química , Ciclohexanonas/farmacología , Ciclohexanonas/aislamiento & purificación , Lipopolisacáridos/farmacología , Lipopolisacáridos/antagonistas & inhibidores , Estructura Molecular , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Interleucina-6/antagonistas & inhibidores , Interleucina-6/metabolismo , Factor de Necrosis Tumoral alfa/antagonistas & inhibidores , Relación Estructura-Actividad , Relación Dosis-Respuesta a Droga , Glucósidos
14.
J Ethnopharmacol ; 333: 118427, 2024 Oct 28.
Artículo en Inglés | MEDLINE | ID: mdl-38844251

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Dioscoreae Rhizoma, a kind of Chinese yam, is a medicinal and edible plant used in China for strengthening the spleen and stomach. However, there is a lack of modern pharmacology studies regarding its anti-gastric injury activity. AIM OF THE STUDY: This study aimed to investigate the phytochemical composition of Chinese yam aqueous extract (CYW) and evaluate its gastroprotective effects against ethanol-induced gastric injury in vitro and in vivo. MATERIALS AND METHODS: The active components of CYW were identified using HPLC-QTOF-MS/MS in combination with the GNPS molecular networking and network pharmacology. In vitro studies were performed in the RAW264.7/GES-1 cell coculture system. In vivo study, mice were treated with CYW (0.31, 0.63, and 3.14 g/kg BW, orally) for 14 days, followed by a single oral dose of ethanol (10 mL/kg BW) to induce gastric injury. The biochemical, inflammation and oxidative stress markers were analyzed using commercial kits. Histopathology was used to assess the degree of gastric injury. Gene and protein expressions were studied using RT-qPCR and western blotting, respectively. RESULTS: CYW significantly restored the levels of SOD, GPx and CAT, and reduced the MDA content. Further analyses showed that CYW significantly alleviated the gastric oxidative stress by inhibiting the inflammation via decreasing p-NF-κB and p-IκB-α expression levels and inhibiting the generation of IL-6, TNF-α, and IL-1ß. At the same time, the fraction remarkably upregulated Bcl-2, downregulated Bax and increased growth factor secretion, thereby prevented gastric mucous cell. Besides, The combination of HPLC-QTOF-MS/MS, GNPS molecular networking analysis, and network pharmacology demonstrated that linoleic acid, 3-acetyl-11-keto-beta-boswellic acid, adenosine, aminocaproic acid, tyramine, DL-tryptophan, cycloleucine, lactulose, melibiose, alpha-beta-trehalose, and sucrose would be the main active compounds of CYW against ethanol-induced gastric injury. CONCLUSION: This study showed that CYW is potentially rich source of anti-oxidant and anti-inflammatory bioactive compounds. It showed efficacy against ethanol-induced gastric injury by inhibiting inflammation, oxidative stress, and apoptosis in the stomach. The results of the current work indicate that Dioscoreae Rhizoma could be utilized as a type of natural resource for production of new medicine and functional foods to prevent and/or ameliorate ethanol-induced gastric injury.


Asunto(s)
Dioscorea , Etanol , Extractos Vegetales , Rizoma , Animales , Etanol/química , Dioscorea/química , Ratones , Masculino , Rizoma/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Células RAW 264.7 , Estrés Oxidativo/efectos de los fármacos , Fitoquímicos/farmacología , Fitoquímicos/análisis , Mucosa Gástrica/efectos de los fármacos , Mucosa Gástrica/patología , Mucosa Gástrica/metabolismo , Humanos , Antiinflamatorios/farmacología , Antiinflamatorios/aislamiento & purificación
15.
J Ethnopharmacol ; 333: 118459, 2024 Oct 28.
Artículo en Inglés | MEDLINE | ID: mdl-38897034

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: In Brazilian popular medicine, Lippia alba leaves are used in teas to treat pain and inflammatory diseases. AIM OF THE STUDY: to evaluate the chemical composition, antinociceptive, and anti-inflammatory activities of Lippia alba essential oil and its major compound geraniol. MATERIAL AND METHODS: Lippia alba leaves were collected in Pará state, Brazil. The leaf essential oil was obtained using a modified Clevenger-type extractor. Then, the oil was analyzed by GC and GC-MS analyses. To evaluate the toxicity of LaEO and geraniol, the doses of 50, 300, and 2000 mg/kg were used in a mouse model. For antinociception tests, abdominal contortion, hot plate, and formalin tests were used; all groups were treated with LaEO and geraniol at doses of 25, 50, and 100 mg/kg; and to evaluate inflammation using the ear edema model. RESULTS: The constituents identified in the highest content were oxygenated monoterpenes: geraniol (37.5%), geranial (6.7%) and neral (3.8%). The animals treated with LaEO and geraniol demonstrated atypical behaviors with aspects of lethargy and drowsiness, characteristics of animals in a state of sedation; the relative weights showed no significant difference compared to the controls. In the abdominal contortion test, LaEO at 25 mg/kg, 50 mg/kg doses, and 100 mg/kg reduced the number of contortions, representing a percentage reduction of 84.64%, 81.23%, and 66.21% respectively. In the hot plate test, LaEO and geraniol increased the latency time at doses of 25, 50, and 100 mg/kg in all test periods; there was no statistical difference between LaEO and geraniol. In the first phase of the formalin test, only doses of 25 mg/kg and 100 mg/kg of LaEO showed significant activity, reducing the latency time by 53.40% and 58.90%. LaEO at doses of 25 mg/kg and 100 mg/kg reduced the size of the edema, demonstrating an anti-inflammatory activity of 59.38% (25 mg/kg) and 50% (100 mg/kg). CONCLUSION: Lippia alba essential oil and geraniol showed central/peripheral analgesic and anti-inflammatory potential and can be used as an alternative or complementary treatment to conventional drugs. More studies are needed to evaluate its action mechanisms and its analgesic effects.


Asunto(s)
Monoterpenos Acíclicos , Analgésicos , Antiinflamatorios , Edema , Lippia , Aceites Volátiles , Hojas de la Planta , Animales , Lippia/química , Aceites Volátiles/farmacología , Aceites Volátiles/química , Brasil , Analgésicos/farmacología , Analgésicos/aislamiento & purificación , Ratones , Antiinflamatorios/farmacología , Antiinflamatorios/aislamiento & purificación , Masculino , Hojas de la Planta/química , Edema/tratamiento farmacológico , Edema/inducido químicamente , Monoterpenos Acíclicos/farmacología , Plantas Medicinales/química , Dolor/tratamiento farmacológico , Conducta Animal/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Dimensión del Dolor/efectos de los fármacos
16.
J Ethnopharmacol ; 333: 118472, 2024 Oct 28.
Artículo en Inglés | MEDLINE | ID: mdl-38901681

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Ficus erecta, a traditional Chinese She Ethnomedicine, has been historically utilized to treat various inflammatory conditions such as arthritis, nephritis, and osteoporosis. However, the underlying mechanisms accounting for its anti-inflammatory activity, as well as its active components, largely remain elusive. AIM OF THE STUDY: The purpose of this research was to investigate the chemical constituents of F. erecta that contribute to its anti-inflammatory effects. MATERIALS AND METHODS: Coumarins and flavones were obtained from the 95% EtOH extract of F. erecta using virous column chromatography and reversed-phase semipreparative HPLC. The structures of the new compounds were elucidated by extensive analysis of spectroscopic methods, including HRESIMS, 1D and 2D NMR spectra, and CD experiments. Cultured macrophage RAW264.7 cells were utilized for the anti-inflammatory experiments. MTT cell viability assay, Griess reagent method, ELISA, and Western blot experiments were employed to evaluate the anti-inflammatory activity and investigate the related mechanism. RESULTS: Four new (1-4) and eleven previously identified (5-16) coumarins, together with one new (17) and six known flavones (18-23) were isolated from the whole plant of F. erecta. Compounds 7 and 17 significantly reduced nitric oxide (NO) and prostaglandin E2 (PGE2) production without cytotoxic effects. Furthermore, compounds 7 and 17 reduced the production of proinflammatory cytokines including tumor necrosis factor (TNF)-α, interleukin (IL)-1ß, and IL-6 in a concentration-dependent manner. Western blot analysis indicated that compounds 7 and 17 suppressed the expression of iNOS, COX-2, and p-IκBα in LPS-stimulated RAW264.7 macrophage cells. CONCLUSION: The current phytochemical investigations revealed that coumarins and flavones represent the primary chemical constituents of F. erecta. Compounds 7 and 17 exhibit potent anti-inflammatory properties, linked with the inhibition of NF-κB activation by preventing the degradation of IκBα phosphorylation. These compounds may serve as promising candidates for treating or preventing certain inflammatory diseases.


Asunto(s)
Antiinflamatorios , Cumarinas , Ficus , Flavonas , Extractos Vegetales , Animales , Ficus/química , Flavonas/farmacología , Flavonas/aislamiento & purificación , Flavonas/química , Cumarinas/farmacología , Cumarinas/aislamiento & purificación , Cumarinas/química , Células RAW 264.7 , Ratones , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Extractos Vegetales/farmacología , Extractos Vegetales/química , Óxido Nítrico/metabolismo , FN-kappa B/metabolismo , Supervivencia Celular/efectos de los fármacos , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo
17.
Carbohydr Polym ; 339: 122266, 2024 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-38823930

RESUMEN

Konjac glucomannan (KG) is a dietary fiber hydrocolloid derived from Amorphophallus konjac tubers and is widely utilized as a food additive and dietary supplement. As a health-conscious choice, purified KG, along with konjac flour and KG-infused diets, have gained widespread acceptance in Asian and European markets. An overview of the chemical composition and structure of KG is given in this review, along with thorough explanations of the processes used in its extraction, production, and purification. KG has been shown to promote health by reducing glucose, cholesterol, triglyceride levels, and blood pressure, thereby offering significant weight loss advantages. Furthermore, this review delves into the extensive health benefits and pharmaceutical applications of KG and its derivatives, emphasizing its prebiotic, anti-inflammatory, and antitumor activities. This study highlights how these natural polysaccharides can positively influence health, underscoring their potential in various biomedical applications.


Asunto(s)
Amorphophallus , Mananos , Mananos/química , Mananos/aislamiento & purificación , Humanos , Amorphophallus/química , Animales , Fibras de la Dieta/análisis , Antiinflamatorios/química , Antiinflamatorios/farmacología , Antiinflamatorios/aislamiento & purificación , Suplementos Dietéticos , Prebióticos , Antineoplásicos/química , Antineoplásicos/aislamiento & purificación , Antineoplásicos/farmacología
18.
J Ethnopharmacol ; 333: 118470, 2024 Oct 28.
Artículo en Inglés | MEDLINE | ID: mdl-38909829

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Initial investigative research indicated that the essential oil from Chimonanthus nitens Oliv. Leaves (CLO) significantly reduces lung tissues inflammation and effectively repairs Acute lung injury (ALI) mice model. However, the mechanism underlying is not clear, and the impacts of CLO on oxidative stress require further investigation. AIM OF THE STUDY: The purpose of the experiment was to validate the influence of CLO in ALI model mice, as well as its potential mechanisms. MATERIALS AND METHODS: Lipopolysaccharide-induced establishment of the A549 cell inflammation model, and ALI mice model was established by intrathecal administration of LPS. RESULTS: CLO significantly reduced the release of inflammatory cytokines in A549 cells, lowered MDA and ROS levels, and enhanced SOD activity. Animal experiment results showed that CLO dramatically decreased white blood cell count, the expression of inflammatory cytokines, and the destruction of alveolar structures. CLO enhances the activity of antioxidant enzymes. Western Blot and q-PCR analyses have revealed that the mechanism of CLO is correlation with the NF-κB and Nrf2 signaling pathways in cellular and animal models. Pathway inhibitor experiments indicated that there might be functional crosstalk between these two pathways. CONCLUSIONS: CLO may regulate inflammation and oxidative stress in LPS-induced ALI through NF-κB and Nrf2 signaling pathways. This finding could be novel in the pharmacological treatment of ALI.


Asunto(s)
Lesión Pulmonar Aguda , Lipopolisacáridos , Aceites Volátiles , Estrés Oxidativo , Hojas de la Planta , Transducción de Señal , Animales , Humanos , Masculino , Ratones , Células A549 , Lesión Pulmonar Aguda/tratamiento farmacológico , Lesión Pulmonar Aguda/inducido químicamente , Lesión Pulmonar Aguda/metabolismo , Antiinflamatorios/farmacología , Antiinflamatorios/aislamiento & purificación , Calycanthaceae/química , Citocinas/metabolismo , Modelos Animales de Enfermedad , Inflamación/tratamiento farmacológico , Inflamación/inducido químicamente , Factor 2 Relacionado con NF-E2/metabolismo , FN-kappa B/metabolismo , Aceites Volátiles/farmacología , Estrés Oxidativo/efectos de los fármacos , Hojas de la Planta/química , Transducción de Señal/efectos de los fármacos
19.
J Pharm Biomed Anal ; 246: 116252, 2024 Aug 15.
Artículo en Inglés | MEDLINE | ID: mdl-38788622

RESUMEN

Balanophora harlandii Hook (B. harlandii), a folk medicine, has been traditionally employed to treat traumatic bleeding, gastroenteritis, icteric hepatitis, hemorrhoids, and other conditions. In this work, polysaccharides with anti-inflammatory effects were extracted from B. harlandii and purified. The extraction conditions were optimized, and the properties of one purified neutral fraction, denoted as BHPs-W-S3, were analyzed. BHPs-W-S3 has a molecular weight of 14.1 kDa, and its three main monosaccharides are glucose, galactose, and xylose, with a molar ratio of 6.4:1.7:1.1. Its main chain consists of →6)-α-D-Glcp-(1→, →4,6)-α-D-Glcp-(1→, →6)-ß-D-Galp-(1→, →3,6)-ß-D-Galp-(1→, and it has branch chains at the O-4 and/or O-3 positions. In addition, in vitro experiments showed that the polysaccharides from B. harlandi can decrease the phosphorylation level of p65 and IκBα in LPS-induced RAW264.7 cells to reduce the expression of the pro-inflammatory genes such as TNF-α, IL-6, and IL-1ß.


Asunto(s)
Antiinflamatorios , Polisacáridos , Ratones , Animales , Polisacáridos/farmacología , Polisacáridos/química , Polisacáridos/aislamiento & purificación , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Células RAW 264.7 , Peso Molecular , Balanophoraceae/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Lipopolisacáridos/farmacología , FN-kappa B/metabolismo , Factor de Necrosis Tumoral alfa/metabolismo , Inflamación/tratamiento farmacológico
20.
J Ethnopharmacol ; 332: 118374, 2024 Oct 05.
Artículo en Inglés | MEDLINE | ID: mdl-38789093

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Picrasma quassioides (D. Don) Benn is a vascular plant belonging to the genus Picrasma of Simaroubaceae family and grows in Korea, China, India, Taiwan, and Japan. Picrasma quassioides extract has been reported to have anti-inflammatory, anti-bacterial, and anti-cancer properties. Moreover, this plant has been also traditionally used to alleviate symptoms of eczema, atopic dermatitis, psoriasis, scabies, and boils in skin. AIM OF THE STUDY: The Pq-EE has been reported in Chinese pharmacopoeia for its pharmacological effects on skin. However, the detailed mechanism on alleviating skin conditions is not understood. Hence, we investigated the skin improvement potential of Pq-EE against skin damage. MATERIALS AND METHODS: We used the human keratinocyte cell line (HaCaT) and mouse melanoma cell line (B16F10) to study the effects of Pq-EE on the epidermis. Additionally, in vitro antioxidant assays were performed using a solution that included either metal ions or free radicals. RESULTS: In colorimetric antioxidant assays, Pq-EE inhibited free radicals in a dose-dependent manner. The Pq-EE did not affect cell viability and promoted cell survival under UVB exposure conditions in the MTT assay. The Pq-EE downregulated the mRNA levels of apoptotic factors. Moreover, MMP1 and inflammatory cytokine iNOS mRNA levels decreased with Pq-EE treatment. With regard to protein levels, caspases and cleaved caspases were more powerfully inhibited by Pq-EE than UVB-irritated conditions. p53 and Bax also decreased with Pq-EE treatment. The melanin contents and secretion were decreased at nontoxic concentrations of Pq-EE. The pigmentation pathway genes also were inhibited by treatment with Pq-EE. CONCLUSIONS: In summary, we suggest the cell protective potential of Pq-EE against UVB and ROS, indicating its use in UV-protective cosmeceutical materials.


Asunto(s)
Antiinflamatorios , Antioxidantes , Apoptosis , Melaninas , Picrasma , Extractos Vegetales , Animales , Antiinflamatorios/farmacología , Antiinflamatorios/aislamiento & purificación , Extractos Vegetales/farmacología , Extractos Vegetales/química , Apoptosis/efectos de los fármacos , Humanos , Ratones , Picrasma/química , Antioxidantes/farmacología , Melaninas/metabolismo , Etanol/química , Células HaCaT , Queratinocitos/efectos de los fármacos , Queratinocitos/efectos de la radiación , Línea Celular Tumoral , Melanoma Experimental/tratamiento farmacológico , Supervivencia Celular/efectos de los fármacos , Óxido Nítrico Sintasa de Tipo II/metabolismo , Óxido Nítrico Sintasa de Tipo II/genética
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