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Objective: Anorectal mucosal melanoma is a rare and aggressive cancer with limited treatment options. Investigating specific molecular pathways may provide insight into the development and progression of this cancer. This study aims to investigate the role of chitinase-3-like protein-1 (YKL-40) in promoting the development of anorectal mucosal melanoma through the PI3K-AKT signaling pathway. Methods: Perianal cells from healthy volunteers and melanoma cells from patients with early, middle and advanced anorectal melanoma were obtained. Western blotting was performed to detect the protein expression of PI3K, AKT, and the downstream proteins mTOR, p-mTOR, ERK, and p-ERK, respectively. Subsequently, we constructed knockout and overexpression of YKL-40 melanoma cell lines, then used western blot assay to test for YKL-40, PI3K and AKT protein expression. Results: A significant increase in the expression of PI3K, AKT, and the downstream proteins mTOR, pmTOR, ERK, and pERK was observed in melanoma cells, and the expression of these proteins increased with the development of melanoma. After YKL-40 was knocked out, PI3K and AKT expression decreased in melanoma cells in patients with advanced melanoma. On the contrary, PI3K and AKT protein expression increased significantly after YKL-40 overexpression. Conclusion: There is a positive correlation between the expression levels of PI3K, AKT, mTOR, p-mTOR, ERK, and p-ERK and the stage of tumor development. The PI3K-AKT signaling pathway promotes the progress of anorectal mucosal melanoma. Chitinase-3-like protein-1 (YKL-40) regulates the progression of anorectal mucosal melanoma through the PI3K-AKT signaling pathway. Investigating specific molecular pathways may provide a better understanding of anorectal mucosal melanoma. The findings from this study could contribute to the development of new diagnosis and treatment strategies for this rare and aggressive cancer. Future research directions may include investigating other possible pathways involved in melanoma progression.
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Silicon-based optical chaos has many advantages, such as compatibility with complementary metal oxide semiconductor (CMOS) integration processes, ultra-small size, and high bandwidth. Generally, it is challenging to reconstruct chaos accurately because of its initial sensitivity and high complexity. Here, a stacked convolutional neural network (CNN)-long short-term memory (LSTM) neural network model is proposed to reconstruct optical chaos with high accuracy. Our network model combines the advantages of both CNN and LSTM modules. Further, a theoretical model of integrated silicon photonics micro-cavity is introduced to generate chaotic time series for use in chaotic reconstruction experiments. Accordingly, we reconstructed the one-dimensional, two-dimensional, and three-dimensional chaos. The experimental results show that our model outperforms the LSTM, gated recurrent unit (GRU), and CNN models in terms of MSE, MAE, and R-squared metrics. For example, the proposed model has the best value of this metric, with a maximum improvement of 83.29% and 49.66%. Furthermore, 1D, 2D, and 3D chaos were all significantly improved with the reconstruction tasks.
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Óptica y Fotónica , Silicio , Memoria a Largo Plazo , Redes Neurales de la ComputaciónRESUMEN
BACKGROUND: Syringa microphylla Diels is a plant in the family Syringa Linn. For hundreds of years, its flowers and leaves have been used as a folk medicine for the treatment of cough, inflammation, colds, sore throat, acute hepatitis, chronic hepatitis, early liver cirrhosis, fatty liver, and oesophageal cancer. PURPOSE: For the first time, we have comprehensively reviewed information on Syringa microphylla Diels that is not included in the Pharmacopoeia, clarified the pharmacological mechanisms of Syringa microphylla Diels and its active ingredients from a molecular biology perspective, compiled in vivo and in vitro animal experimental data and clinical data, and summarized the toxicology and pharmacokinetics of Syringa microphylla Diels. The progress in toxicology research is expected to provide a theoretical basis for the development of new drugs from Syringa microphylla Diels, a natural source of compounds that are potentially beneficial to human health. METHODS: The PubMed, Google Scholar, China National Knowledge Infrastructure, Web of Science, SciFinder Scholar and Thomson Reuters databases were utilized to conduct a comprehensive search of published literature as of July 2021 to find original literature related to Syringa microphylla Diels and its active ingredients. RESULTS: To date, 72 compounds have been isolated and identified from Syringa microphylla Diels, and oleuropein, verbascoside, isoacteoside, echinacoside, forsythoside B, and eleutheroside B are the main active components. These compounds have antioxidant, antibacterial, anti-inflammatory, and neuroprotective effects, and their safety and effectiveness have been demonstrated in long-term traditional applications. Molecular pharmacology experiments have indicated that the active ingredients of Syringa microphylla Diels exert their pharmacological effects in various ways, primarily by reducing oxidative stress damage via Nrf2/ARE pathway regulation, regulating inflammatory factors and inducing apoptosis through the MAPK and NF-κB pathways. CONCLUSION: This comprehensive review of Syringa microphylla Diels provides new insights into the correlations among molecular mechanisms, the importance of toxicology and pharmacokinetics, and potential ways to address the limitations of current research. As Syringa microphylla Diels is a natural low-toxicity botanical medicine, it is worthy of development and utilization and is an excellent choice for treating various diseases.
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Syringa , Animales , Antioxidantes , Etnofarmacología , Humanos , Medicina Tradicional , Fitoquímicos/toxicidad , Extractos Vegetales/toxicidadRESUMEN
Background: In December 2019, a novel coronavirus, SARS-CoV-2 caused a series of acute atypical respiratory diseases worldwide. However, there is still a lack of drugs with clear curative effects, and the clinical trial research of vaccines has not been completely finished. Purpose: LH capsules are approved TCM patent medicine that are widely used for the treatment of respiratory tract infectious diseases caused by colds and flu. On April 12, 2020, LH capsules and granules were officially repurposed by the China Food and Drug Administration (CFDA) for patients with mild COVID-19 based on their safety and efficacy demonstrated through multicentre, randomized, controlled clinical trials. We hope to conduct a comprehensive review of it through modern pharmacy methods, and try to explain its possible mechanism. Methods: Using the full names of LH capsules Lianhuaqingwen, Lianhua Qingwen andSARS-COV-2, COVID-19 as the keywords of the search terms, systemically search for existing related papers in various databases such as Web of Science and PubMed. And completed the collection of clinical data in ClinicalTrials.gov and Chinese Clinical Trial Registry. Last but not least, we have sorted out the anti-inflammatory and antiviral mechanisms of LH capsules through literature and Selleck. Results: This review systematically sorted out the active ingredients in LH capsules. Furthermore, the related pharmacological and clinical trials of LH capsule on SARS-CoV-2, IAV and IBV were discussed in detail. Moreover, the present review provides the first summary of the potential molecular mechanism of specific substances in LH capsules involved in resistance to SARS-COV-2 infection and the inhibition of cytokine storm syndrome (CSS) caused by IL-6. Conclusion: This review summarizes the available reports and evidence that support the use of LH capsules as potential drug candidates for the prevention and treatment of COVID-19. However, TCM exerts its effects through multiple targets and multiple pathways, and LH capsules are not an exception. Therefore, the relevant mechanisms need to be further improved and experimentally verified.
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We report on a cyclic peptide that inhibits matrix metalloproteinase-2 (MMP2) activation with a low-nM-level potency. This inhibitor specifically binds to the D570-A583 epitope on proMMP2 and interferes with the protein-protein interaction (PPI) between proMMP2 and tissue inhibitor of metalloproteinases-2 (TIMP2), thereby preventing the TIMP2-assisted proMMP2 activation process. We developed this cyclic peptide inhibitor through an epitope-targeted library screening process and validated its binding to proMMP2. Using a human melanoma cell line, we demonstrated the cyclic peptide's ability to modulate cellular MMP2 activities and inhibit cell migration. These results provide the first successful example of targeting the PPI between proMMP2 and TIMP2, confirming the feasibility of an MMP2 inhibition strategy that has been sought after for 2 decades.
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Metaloproteinasa 2 de la Matriz/metabolismo , Péptidos Cíclicos/farmacología , Secuencia de Aminoácidos , Línea Celular , Movimiento Celular/efectos de los fármacos , Evaluación Preclínica de Medicamentos , Activación Enzimática/efectos de los fármacos , Humanos , Biblioteca de Péptidos , Péptidos Cíclicos/química , Unión Proteica/efectos de los fármacos , Relación Estructura-Actividad , Inhibidor Tisular de Metaloproteinasa-2/metabolismoRESUMEN
Cardiovascular diseases (CVDs) are the leading cause of mortality worldwide. Rehmanniae Radix Praeparata (RRP) is a popular medicinal herb widely used in traditional Chinese medicine (TCM) to treat CVDs. However, the development of this novel therapeutic product has been stagnant, and its molecular mechanism of action remains unclear. This study aims to explore the effective ingredients of RRP against CVDs, especially atherosclerosis (AS). Using the AutoDock Vina software, the RRP's ingredients were docked with the targets which can be collected by RCSB and UniProt. Then the screened ingredients and targets could be used to dispose the pathways by the Kyoto Encyclopedia of Genes and Genomes (KEGG). We used GEO, GCBI and DAVID databases to analyze the microarray data of AS which could be used to verify the results of molecular docking, all of which could show the molecular mechanism of RRP on CVDs. We also constructed a compound-target interaction network of CVD with 85 nodes and 272 edges on the basis of molecular docking analysis through Cytoscape. The network showed that forsythiaside, acteoside and stigmasterol are the most important compounds and 2HRR (ACAT (Acyl-CoA cholesterol acyl transferase) protein), 4ATB (MMP13) and 1JBQ (cystathionine beta-synthase) are the most valuable targets in the action of RRP against CVD. We also examined the biological functions involved in the biological process, molecular function and cellular components. In accordance with the analysis of GSE6054 microarray data of AS disease, the 20 most specifically expressed genes (differentially expressed genes [DEGs]) and the top 10 pathways of DEGs were discovered. Five key pathways, including non-alcoholic fatty liver disease (NAFLD), pathways in cancer and PI3K-Akt signalling pathway were also explored. Amongst these pathways, the top three were the pathways in cancer, MAPK signalling pathway and human T-cell lymphotropic virus infection. The pathways in cancer and PI3K-Akt signalling pathway were found simultaneously in the pathway analysis for CVD on RRP and for AS on microarray data. This study provided a new potential herbal medicine against CVD and has increased the understanding on the molecular mechanisms of RRPmediated protection against CVD, especially AS.
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Enfermedades Cardiovasculares/terapia , Medicina Tradicional China , Simulación del Acoplamiento Molecular , Extractos Vegetales/química , Raíces de Plantas/química , Biología Computacional , Evaluación Preclínica de Medicamentos , Humanos , Fosfatidilinositol 3-Quinasas/metabolismo , Extractos Vegetales/uso terapéutico , Programas InformáticosRESUMEN
Selective inhibition of cyclin-dependent kinaseâ 8 and cyclinâ C (CDK8/CycC) has been suggested as a promising strategy for decreasing mitogenic signals in cancer cells with reduced toxicity toward normal cells. We developed a novel virtual screening protocol for drug development and applied it to the discovery of new CDK8/CycC typeâ II ligands, which is likely to achieve long residence time and specificity. We first analyzed the binding thermodynamics of 11 published pyrazolourea ligands using molecular dynamics simulations and a free-energy calculation method, VM2, and extracted the key binding information to assist virtual screening. The urea moiety was found to be the critical structural contributor of the reference ligands. Starting with the urea moiety, we conducted substructure-based searches with our newly developed superposition and single-point energy evaluation method, followed by free-energy calculations, and singled out three purchasable compounds for bioassay testing. The ranking from the experimental results is completely consistent with the predicted rankings. A potent drug-like compound was found to have a Kd value of 42.5â nm, which is similar to those of the most potent reference ligands; this provided a good starting point for further improvement. This study shows that our novel virtual screening protocol is an accurate and efficient tool for drug development.
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Ciclina C/antagonistas & inhibidores , Quinasa 8 Dependiente de Ciclina/antagonistas & inhibidores , Descubrimiento de Drogas/métodos , Evaluación Preclínica de Medicamentos/métodos , Ligandos , Inhibidores de Proteínas Quinasas/farmacología , Ciclina C/metabolismo , Quinasa 8 Dependiente de Ciclina/metabolismo , Relación Dosis-Respuesta a Droga , Humanos , Estructura Molecular , Inhibidores de Proteínas Quinasas/química , Relación Estructura-Actividad , TermodinámicaRESUMEN
BACKGROUND AND PURPOSE: Polygonum orientale L. (family: Polygonaceae), named Hongcao in China, has effects of dispelling wind and dampness, promoting blood circulation, and relieving pain. Our group has already studied and confirmed that POEa and POEe (ethyl acetate and ethyl ether extract of P. orientale, respectively) had anti-inflammatory and analgesic effects in early research, which was mainly relevant to the existence of flavonoids. According to the clinical application of P. orientale in traditional Chinese medicine, it has long been used for rheumatic arthralgia and rheumatoid arthritis. Therefore, our group further explored whether flavonoids of P. orientale have anti-rheumatoid arthritis effect and how does they play this role. METHODS: Dried small pieces of the stems and leaves of P. orientale were decocted with water and partitioned successively to obtain POEa and POEe, respectively. The anti-rheumatoid arthritis effect of P. orientale was studied by using a Freund's complete adjuvant (FCA)-induced arthritis (AIA) in a rat model. The levels of PGE2, TNF-α, and IL-1ß in serum of AIA rats were detected by enzyme linked immunosorbent assay (ELISA) to explore its mechanisms. In addition, we computationally studied the relationships between the 15 chemical components of POEa and POEe, and the currently focused 9 target proteins of rheumatoid arthritis by molecular docking. RESULTS: Pharmacological experiments showed that POEa and POEe significantly ameliorate symptoms of rheumatoid arthritis via reducing paw swelling volume, arthritis score, and thymus and spleen indices, as well as increasing body weight in AIA rats. Simultaneously, the concentrations of PGE2, TNF-α, and IL-1ß were significantly decreased by POEa and POEe. Histopathology revealed noticeable reduction in bone and cartilage, synovial hyperplasia, inflammatory cell infiltration, cartilage surface erosion, and joint degeneration by POEa and POEe treatment. In addition, the molecular docking studies showed that docking scores of 14 chemical compositions (including 12 flavonoids and 2 phenolic acids) of POEa and POEe with anti-rheumatoid arthritis protein targets were better than the complexed ligands of the anti-rheumatoid arthritis protein targets. Among them, six flavonoids in POEa and POEe had more docking protein targets (n ≥ 3). Five anti-rheumatoid arthritis targets including high-temperature requirement A1 protease (HtrA1), janus kinase 1 (JAK1), cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (i-NOS), and prostaglandin E2 (PGE2) had better docking score compared with the complexed ligands. Moreover, most of the chemical components in POEa and POEe showed strong interaction with HtrA1. CONCLUSIONS: The flavonoids of P. orientale have anti-rheumatoid arthritis effect. In addition, the molecular docking results indicate that quercetin, catechol, orientin, and other six flavonoids may be closely related to HtrA1, JAK1, COX-2, i-NOS, and PGE2 protein target receptors. It suggests that these chemical compositions form strong protein-ligand complexes with these protein targets, especially HtrA1 to exert anti-rheumatoid arthritis. Further experimental studies show that mechanisms of anti-rheumatoid arthritis effects may also be relevant to inhibit the levels of PGE2, TNF-α, and IL-1ß in serum. Therefore, our group can further explore the possible active ingredients and mechanisms of the anti-rheumatoid arthritis effects of flavonoids, and focus on the inhibition of the expression of inflammatory factors and the TGF-ß1/Smad signaling pathway associated with HtrA1 protein target receptors, which can provide a direction and powerful reference for the action mechanism and drug research of anti-rheumatoid arthritis of flavonoids in P. orientale.
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Antiinflamatorios/uso terapéutico , Artritis Experimental/terapia , Artritis Reumatoide/terapia , Fitoterapia/métodos , Extractos Vegetales/uso terapéutico , Polygonum/inmunología , Animales , Modelos Animales de Enfermedad , Humanos , Mediadores de Inflamación/metabolismo , Masculino , Medicina Tradicional China , Simulación del Acoplamiento Molecular , Ratas , Ratas Sprague-DawleyRESUMEN
This paper aimed to investigate the anti-influenza virus activity of the genus Paeonia, screen potential anti-influenza virus compounds and predict targets of anti-influenza virus to explore the mechanism of anti-influenza virus activity. First of all, a total of 301 compounds of the genus Paeonia were summarized from the literatures in recent ten years. The candidate active ingredients from the genus Paeonia were identified by database such as PubChem and Chemical Book. The ligands were constructed by ChemDraw, Avogadro and Discovery Studio Visualizer. Secondly, 23 potential anti-influenza virus targets were developed by combining the target database and the literatures. Uniprot database was used to find the anti-influenza virus targets, and RCSB was used to identify targets associated with anti-influenza virus activity as docked receptor proteins. QuickVina 2.0 software was used for molecular docking. Finally, the Cytoscape 3.5.1 software was used to map the potential activity compounds of the genus Paeonia against influenza virus and the anti-influenza virus target network. Uniprot online database was used to analyze the target GO enrichment and KEGG metabolic pathways. The results showed that 74 compounds of the genus Paeonia had anti-influenza virus effect and 18 potential anti-influenza virus targets were screened. GO analysis concluded that the mechanism of the genus Paeonia anti-influenza virus is consistent with the mechanism of NA anti-influenza virus in order to stop the sprouting, dispersion and diffusion of virus and reduce the ability of virus to infect, so that the infection can be restricted so as to achieve the anti-influenza virus effect.
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Antivirales/farmacología , Orthomyxoviridae/efectos de los fármacos , Paeonia/química , Fitoquímicos/farmacología , Simulación del Acoplamiento MolecularRESUMEN
This paper aimed to investigate the antibacterial activity of flowers and leaves from Paeonia rockii, screen antibacterial compounds and predict targets of antibacterial to explore its multi-component, multi-target antibacterial mechanism. In this study, minimal inhibitory concentration(MIC) of seven strains of Staphylococcus aureus, S. epidermidisï¼ Bacillus subtilis, B. cereus, Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa were determined by microdilution method. Uniprot databases was used to find the antibacterial targets, and RCSB was used to identify targets associated with antimicrobial activity as docked receptor proteins. The candidate active ingredients from flowers and leaves of P. rockii were identified by database such as PubChem. The ligands were constructed by ChemDraw, Avogadro and Discovery Studio Visualizer. QuickVina 2.0 software was used to molecular docking. Besides, the Cytoscape 3.5.1 software was used to construct activity compounds of flowers and leaves from P. rockii ingredients-targets network, and Uniprot software was used to analyze gene ontology and KEGG pathway. In vitro antibacterial experiments found antibacterial effect of the flowers and leaves from P. rockii, especially methanol extraction of flowers has the strongest antibacterial effect. The network pharmacology indicated that total 29 activity ingredients and their 18 targets were screened in flowers and leaves from P. rockii. Comparison of the active ingredients and the number of antimicrobial target networks, it is predicted that the antibacterial components are mainly flavonoids and phenolic acids and main mechanism of antibacterial is to inhibit the synthesis of bacterial proteins. In this study, potential antibacterial activity of flowers and leaves from P. rockii has be found by antibacterial experiments in vitro and network pharmacology screening. And this study provides new clues for further basic study on the antibacterial agents of flowers and leaves from P. rockii.
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Antibacterianos/farmacología , Simulación del Acoplamiento Molecular , Paeonia/química , Flores/química , Pruebas de Sensibilidad Microbiana , Fitoquímicos/farmacología , Extractos Vegetales , Hojas de la Planta/químicaRESUMEN
The genus Paeonia, also known as the "King of Flowers" in China, is an important source of traditional Chinese medicine (TCM). Plants of this genus have been used to treat a range of cardiovascular and gynecological diseases. However, the potential pharmacological activity of one particular species, Paeonia rockii, has not been fully investigated. In the first part of the present study, 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonic) acid (ABTS), reducing power assays, and metal ion chelating assays were used to investigate the in vitro antioxidant activities of Paeonia rockii. In the second portion of the study, a mouse model of d-galactose-induced aging was used to validate the antioxidant effects of the flowers from Paeonia rockii in vivo. Lastly, potential antioxidant constituents were screened and identified by ultra-high pressure liquid chromatography and electrospray ionization coupled with high-resolution mass spectrometry (UHPLC-ESI-HRMSn) combined with the DPPH assay. Results indicated that the flowers and leaves exhibited stronger antioxidant activity than ascorbic acid in vitro. The therapeutic effect of Paeoniarockii was determined in relation to the levels of biochemical indicators, such as 8-iso-prostaglandin F2α (8-iso PGF2α) in the serum, superoxide dismutase (SOD), protein carbonyl, malondialdehyde (MDA), and glutathione (GSH) in the liver and brain, after daily intra-gastric administration of different concentrations of extracts (100, 200 and 400 mg/kg) for three weeks. The levels of 8-iso PGF2α (p < 0.01) and protein carbonyl groups (p < 0.01) were significantly reduced, whereas those of SOD (p < 0.05) had significantly increased, indicating that components of the flowers of Paeonia rockii had favorable antioxidant activities in vivo. Furthermore, UHPLC-ESI-HRMSn, combined with pre-column DPPH reaction, detected 25 potential antioxidant compounds. Of these, 18 compounds were tentatively identified, including 11 flavonoids, four phenolic acids, two tannins, and one monoterpene glycoside. This study concluded that the leaves and flowers from Paeonia rockii possess excellent antioxidant properties, highlighting their candidacy as "new" antioxidants, which can be utilized therapeutically to protect the body from diseases caused by oxidative stress.
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Envejecimiento/metabolismo , Antioxidantes/química , Compuestos de Bifenilo/antagonistas & inhibidores , Galactosa/antagonistas & inhibidores , Paeonia/química , Picratos/antagonistas & inhibidores , Envejecimiento/efectos de los fármacos , Animales , Antioxidantes/aislamiento & purificación , Antioxidantes/farmacología , Ácido Ascórbico/farmacología , Benzotiazoles/antagonistas & inhibidores , Encéfalo/efectos de los fármacos , Encéfalo/metabolismo , Dinoprost/análogos & derivados , Dinoprost/sangre , Flavonoides/química , Flavonoides/aislamiento & purificación , Flavonoides/farmacología , Flores/química , Galactosa/farmacología , Vida Libre de Gérmenes , Glutatión/agonistas , Glutatión/metabolismo , Glicósidos/química , Glicósidos/aislamiento & purificación , Glicósidos/farmacología , Hidroxibenzoatos/química , Hidroxibenzoatos/aislamiento & purificación , Hidroxibenzoatos/farmacología , Hígado/efectos de los fármacos , Hígado/metabolismo , Masculino , Malondialdehído/antagonistas & inhibidores , Malondialdehído/metabolismo , Ratones , Estrés Oxidativo , Extractos Vegetales/química , Hojas de la Planta/química , Carbonilación Proteica , Espectrometría de Masa por Ionización de Electrospray , Ácidos Sulfónicos/antagonistas & inhibidores , Superóxido Dismutasa/metabolismo , Taninos/química , Taninos/aislamiento & purificación , Taninos/farmacologíaRESUMEN
Bletilla striata has attracted extensive research interest due to the potential uses for its extracts to treat skin burns and inflammatory disorders in a clinical setting. My current research focuses on Bletilla striata polysaccharides (BSP), and often ignores the residues that remain after polysaccharide extraction. It also remains unclear whether the residues have medical value related its traditional clinic function. During this work, we firstly identified the contents of the post-extraction residue by UPLC-Q-Exactive Orbitrap-MS and evaluated its in vivo wound healing and in vitro antioxidant activity. The wound healing activity of the ointment containing residue was assessed for 15days the scald model was used in mice, followed by histopathology and histomorphological analysis. The in vitro antioxidant effect of Bletilla residue was researched using DPPH, ABTS, Hydroxyl radical scavenging, superoxideanion radical scavenging, and reducing power assays. AUPLC-Q-Exactive Orbitrap-MS analysis identified 6 phenolic compounds: protocatechuic acid, p-hydroxybenzoic acid, caffeic acid, p-hydroxybenzaldehyde, 3-Hydroxycinnamic acid, and ferulic acid. Animals treated with "mixed ointment" experienced inflammatory infiltration, which was lower than that of other groups. Both "BSPG ointment" and "Bletilla phenolic ointment" demonstrated superior tissue repair compared to the control. This study was the first to confirm that the residual liquid after polysaccharide extraction has excellent antioxidant and wound healing activities. In addition to Bletilla striata polysaccharides, the residual liquid can improve skin regeneration after burns and reduce inflammatory marker levels. These results have implications that the residual liquid has potential wound healing medicinal value.
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Antioxidantes/farmacología , Orchidaceae/química , Fenoles/química , Extractos Vegetales/farmacología , Cicatrización de Heridas/efectos de los fármacos , Animales , Cromatografía Líquida de Alta Presión , Ensayo de Inmunoadsorción Enzimática , Depuradores de Radicales Libres/farmacología , Riñón/efectos de los fármacos , Riñón/patología , Hígado/efectos de los fármacos , Hígado/patología , Masculino , Espectrometría de Masas , Ratones , Pomadas , Estándares de Referencia , Coloración y EtiquetadoRESUMEN
The study was undertaken to investigate the blood stasis of chronic pelvic inflammatory disease (PID) with scientific method, hemorheology. The whole blood viscosities of chronic PID increased significantly compared with normal level, which was consistent with the blood stasis of Traditional Chinese Medicine (TCM) theory. Moreover, sixty women suffering from chronic PID were treated with Enema Retention of Li Chong Tang Combined with Moxibustion (ERM) for 6 weeks. The chronic PID score and the whole blood viscosity were evaluated before and after the ERM. The parameters of whole blood viscosities at low, median and high shear rate of chronic PID group decreased from 12.32±0.31, 6.66±0.13 and 5.15±0.52, to the normal levels, 9.19±0.13, 5.42±0.56 and 4.34±0.43 (p<0.05) after therapy of ERM and the symptoms score decreased from 13.73±3.7 to 3.8±1.4 (p<0.05), which shows that the ERM is an effective therapy method to treat chronic PID.
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Enema , Medicina Tradicional China , Moxibustión , Enfermedad Inflamatoria Pélvica/terapia , Adulto , Viscosidad Sanguínea , Enfermedad Crónica , Femenino , Humanos , Persona de Mediana Edad , Enfermedad Inflamatoria Pélvica/sangreRESUMEN
Three new trace bisindole alkaloids geleganimines A and B (1, 2) and geleganamide (3) were isolated from the aerial parts of Gelsemium elegans. Their structures were elucidated by spectroscopy, particularly from their carbon-proton coupling constants, and electronic circular dichroism. Compounds 1-3 are the first bisindole alkaloids discovered from the genus Gelsemium. Geleganimine B exhibited anti-inflammatory activity indirectly by suppressing lipopolysaccharide-induced pro-inflammatory factors in BV2 microglial cells with an IC50 value of 10.2 µM. These findings confirm the importance of bioactive trace components in medicinal plant research.
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Antiinflamatorios/aislamiento & purificación , Antiinflamatorios/farmacología , Medicamentos Herbarios Chinos/aislamiento & purificación , Medicamentos Herbarios Chinos/farmacología , Gelsemium/química , Alcaloides Indólicos/aislamiento & purificación , Alcaloides Indólicos/farmacología , Plantas Medicinales/química , Animales , Antiinflamatorios/química , Medicamentos Herbarios Chinos/química , Humanos , Alcaloides Indólicos/química , Concentración 50 Inhibidora , Lipopolisacáridos/farmacología , Ratones , Microglía/citología , Microglía/efectos de los fármacos , Estructura MolecularRESUMEN
OBJECTIVES: The emergence of antibiotic-resistant Helicobacter pylori strains has necessitated a search for alternative therapies for the treatment of this infection. The aim of this study was to evaluate whether or not polysaccharide fractions from Aloe vera are effective in inhibiting the adherence of H. pylori in vitro. METHODS: Polysaccharide fractions were extracted from A. vera and subjected to carbohydrate analysis. The adhesive effect was determined by co-incubation of H. pylori and cells with polysaccharides followed by fluorescein isothiocyanate labelling and Gram staining in vitro. Inhibition of H. pylori growth and cellular viability was tested by agar diffusion and MTT assay. KEY FINDINGS: APS-F2 contained significant amounts of galacturonic acid, galactose and arabinose. APS-F1 was galacturonic acid-free and consisted of mannose, glucose and galactose. APS-F2 (0.1, 0.5 and 1.0 mg/ml) reduced the count of H. pylori attached to MKN45 cells to 88, 76 and 64%, respectively. APS-F1 did not show the same effect. Neither polysaccharide revealed an inhibitory effect on the growth of H. pylori or cell viability. In addition, APS-F2 was shown to have a potent anti-adhesive effect against Escherichia coli. CONCLUSIONS: The results show that the acidic polysaccharide from A. vera has a potent anti-adhesive effect against H. pylori in vitro. However, there have yet to be any in-vivo studies to demonstrate the clinical relevance of this finding.