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1.
Front Immunol ; 15: 1305886, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38343532

RESUMEN

Zanthoxylum bungeanum Maxim., commonly known as Chinese prickly ash, is a well-known spice and traditional Chinese medicine ingredient with a rich history of use in treating inflammatory conditions. This review provides a comprehensive overview of the botanical classification, traditional applications, and anti-inflammatory effects of Z. bungeanum, with a specific focus on its polyphenolic components. These polyphenols have exhibited considerable promise, as evidenced by preclinical studies in animal models, suggesting their therapeutic potential in human inflammatory diseases such as ulcerative colitis, arthritis, asthma, chronic obstructive pulmonary disease, cardiovascular disease, and neurodegenerative conditions. This positions them as a promising class of natural compounds with the potential to enhance human well-being. However, further research is necessary to fully elucidate their mechanisms of action and develop safe and effective therapeutic applications.


Asunto(s)
Asma , Colitis Ulcerosa , Zanthoxylum , Animales , Humanos , Polifenoles/farmacología , Polifenoles/uso terapéutico , Medicina Tradicional China
2.
Front Immunol ; 14: 1275859, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-38022517

RESUMEN

Antimicrobial photodynamic therapy (aPDT) has become a potent contender in the fight against microbial infections, especially in the context of the rising antibiotic resistance crisis. Recently, there has been significant interest in polyphenolic natural products as potential photosensitizers (PSs) in aPDT, given their unique chemical structures and inherent antimicrobial properties. Polyphenolic natural products, abundant and readily obtainable from natural sources, are generally regarded as safe and highly compatible with the human body. This comprehensive review focuses on the latest developments and future implications of using natural polyphenols as PSs in aPDT. Paramount polyphenolic compounds, including curcumin, hypericin, quercetin, hypocrellin, celastrol, riboflavin, resveratrol, gallic acid, and aloe emodin, are elaborated upon with respect to their structural characteristics, absorption properties, and antimicrobial effects. Furthermore, the aPDT mechanism, specifically its targeted action on microbial cells and biofilms, is also discussed. Polyphenolic natural products demonstrate immense potential as PSs in aPDT, representing a promising alternate approach to counteract antibiotic-resistant bacteria and biofilm-related infections.


Asunto(s)
Fotoquimioterapia , Fármacos Fotosensibilizantes , Humanos , Fármacos Fotosensibilizantes/farmacología , Fármacos Fotosensibilizantes/uso terapéutico , Fotoquimioterapia/métodos , Antibacterianos/farmacología , Bacterias , Farmacorresistencia Microbiana
3.
Biomed Pharmacother ; 118: 109203, 2019 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-31306970

RESUMEN

According to its different occurrence mechanism, programmed cell death (PCD) is divided into apoptosis, autophagy, necrosis, paraptosis and so on. Paraptosis is morphologically different from apoptosis and autophagy, which exhibit cytoplasmic vacuolation derived from the ER, independent of caspase, absence of apoptotic morphology. Recent researches have implied that a variety of small molecule compounds, such as celastrol, curcumin, can induce paraptosis-associated cell death as the reagent to enhance anti-cancer activity. A better understanding of paraptosis will lay the foundation to develop new therapeutic strategies to treat human cancers that make full use of small-molecule compounds.


Asunto(s)
Productos Biológicos/farmacología , Neoplasias/tratamiento farmacológico , Muerte Celular Regulada/efectos de los fármacos , Bibliotecas de Moléculas Pequeñas/farmacología , Animales , Apoptosis/efectos de los fármacos , Autofagia/efectos de los fármacos , Productos Biológicos/química , Línea Celular Tumoral , Retículo Endoplásmico/efectos de los fármacos , Retículo Endoplásmico/metabolismo , Humanos , Neoplasias/metabolismo , Neoplasias/patología , Biosíntesis de Proteínas/efectos de los fármacos , Bibliotecas de Moléculas Pequeñas/química , Vacuolas/efectos de los fármacos , Vacuolas/metabolismo
4.
Cell Death Dis ; 10(1): 19, 2019 01 08.
Artículo en Inglés | MEDLINE | ID: mdl-30622245

RESUMEN

Ultraviolet radiation is markedly increased because of pollution and the depletion of the stratospheric ozone layer. Excessive exposure to sunlight can negatively affect the skin, resulting in sunburn, photo-aging, or skin cancer. In this study, we first determined the photoprotective effect of sanshool, a major component in Zanthoxylum bungeanum, on UVB-irradiated responses in human dermal fibroblasts (HDFs) and nude mouse. We found that sanshool treatment can protect cells against the effects of UVB irradiation by (i) increasing cell viability, (ii) inhibiting MMP expression, and (iii) inducing autophagy. We also used the recombinant CSF2 or anti-CSF2 antibody co-cultured with human dermal fibroblasts (HDFs) and found that CSF2 contributes to sanshool-induced autophagy. Sanshool hindered the UVB-induced activation of JAK2-STAT3 signaling in HDFs, thereby inhibiting the expression of MMPs and activation of autophagic flux. Exposure of the dorsal skin of hairless mice to UVB radiation and subsequent topical application of sanshool delayed the progression of skin inflammation, leading to autophagy and inhibiting the activation of JAK2-STAT3 signaling. These results provide a basis for the study of the photoprotective effect of sanshool and suggest that it can be potentially used as an agent against UVB-induced skin damage in humans.


Asunto(s)
Amidas/farmacología , Autofagia/efectos de los fármacos , Fibroblastos/efectos de la radiación , Janus Quinasa 2/metabolismo , Extractos Vegetales/farmacología , Protectores contra Radiación/farmacología , Factor de Transcripción STAT3/metabolismo , Piel/efectos de la radiación , Rayos Ultravioleta/efectos adversos , Amidas/uso terapéutico , Animales , Autofagia/efectos de la radiación , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Eritema/tratamiento farmacológico , Eritema/etiología , Femenino , Fibroblastos/metabolismo , Humanos , Janus Quinasa 2/antagonistas & inhibidores , Inhibidores de la Metaloproteinasa de la Matriz/farmacología , Inhibidores de la Metaloproteinasa de la Matriz/uso terapéutico , Ratones , Ratones Desnudos , Extractos Vegetales/uso terapéutico , Protectores contra Radiación/uso terapéutico , Radiodermatitis/tratamiento farmacológico , Factor de Transcripción STAT3/antagonistas & inhibidores , Transducción de Señal/efectos de la radiación , Piel/metabolismo , Zanthoxylum/química
5.
Phytomedicine ; 21(12): 1658-65, 2014 Oct 15.
Artículo en Inglés | MEDLINE | ID: mdl-25442274

RESUMEN

Polygonatum odoratum lectin (POL), a mannose-binding GNA-related lectin, has been reported to display remarkable anti-proliferative and apoptosis-inducing activities toward a variety of cancer cells; however, the precise molecular mechanisms by which POL induces cancer cell death are still elusive. In the current study, we found that POL could induce both apoptosis and autophagy in human MCF-7 breast cancer cells. Subsequently, we found that POL induced MCF-7 cell apoptosis via the mitochondrial pathway. Additionally, we also found that POL induces MCF-7 cell apoptosis via EGFR-mediated Ras-Raf-MEK-ERK pathway, suggesting that POL may be a potential EGFR inhibitor. Finally, we used proteomics analyses for exploring more possible POL-induced pathways with EGFR, Ras, Raf, MEK and ERK, some of which were consistent with our in silico network prediction. Taken together, these results demonstrate that POL induces MCF-7 cell apoptosis and autophagy via targeting EGFR-mediated Ras-Raf-MEK-ERK signaling pathway, which would provide a new clue for exploiting POL as a potential anti-neoplastic drug for future cancer therapy.


Asunto(s)
Apoptosis/efectos de los fármacos , Autofagia/efectos de los fármacos , Lectinas/farmacología , Sistema de Señalización de MAP Quinasas , Polygonatum/química , Receptores ErbB/metabolismo , Humanos , Células MCF-7 , Mitocondrias/metabolismo
6.
Int J Mol Sci ; 15(10): 17565-76, 2014 Sep 29.
Artículo en Inglés | MEDLINE | ID: mdl-25268623

RESUMEN

In the current study, the lipid-shell and polymer-core hybrid nanoparticles (lpNPs) modified by Arg-Gly-Asp(RGD) peptide, loaded with curcumin (Cur), were developed by emulsification-solvent volatilization method. The RGD-modified hybrid nanoparticles (RGD-lpNPs) could overcome the poor water solubility of Cur to meet the requirement of intravenous administration and tumor active targeting. The obtained optimal RGD-lpNPs, composed of PLGA (poly(lactic-co-glycolic acid))-mPEG (methoxyl poly(ethylene- glycol)), RGD-polyethylene glycol (PEG)-cholesterol (Chol) copolymers and lipids, had good entrapment efficiency, submicron size and negatively neutral surface charge. The core-shell structure of RGD-lpNPs was verified by TEM. Cytotoxicity analysis demonstrated that the RGD-lpNPs encapsulated Cur retained potent anti-tumor effects. Flow cytometry analysis revealed the cellular uptake of Cur encapsulated in the RGD-lpNPs was increased for human umbilical vein endothelial cells (HUVEC). Furthermore, Cur loaded RGD-lpNPs were more effective in inhibiting tumor growth in a subcutaneous B16 melanoma tumor model. The results of immunofluorescent and immunohistochemical studies by Cur loaded RGD-lpNPs therapies indicated that more apoptotic cells, fewer microvessels, and fewer proliferation-positive cells were observed. In conclusion, RGD-lpNPs encapsulating Cur were developed with enhanced anti-tumor activity in melanoma, and Cur loaded RGD-lpNPs represent an excellent tumor targeted formulation of Cur which might be an attractive candidate for cancer therapy.


Asunto(s)
Portadores de Fármacos/química , Lípidos/química , Nanopartículas/química , Oligopéptidos/química , Polímeros/química , Animales , Antineoplásicos/administración & dosificación , Antineoplásicos/química , Antineoplásicos/farmacología , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Colesterol/análogos & derivados , Colesterol/química , Curcumina/administración & dosificación , Curcumina/química , Curcumina/farmacología , Evaluación Preclínica de Medicamentos , Femenino , Células Endoteliales de la Vena Umbilical Humana , Humanos , Ácido Láctico/química , Melanoma/tratamiento farmacológico , Melanoma/metabolismo , Melanoma/patología , Ratones , Ratones Endogámicos BALB C , Poliésteres , Polietilenglicoles/química , Trasplante Homólogo
7.
Drug Des Devel Ther ; 8: 1195-210, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-25214764

RESUMEN

Compared with normal differentiated cells, cancer cells upregulate the expression of pyruvate kinase isozyme M2 (PKM2) to support glycolytic intermediates for anabolic processes, including the synthesis of nucleic acids, amino acids, and lipids. In this study, a combination of the structure-based pharmacophore modeling and a hybrid protocol of virtual screening methods comprised of pharmacophore model-based virtual screening, docking-based virtual screening, and in silico ADMET (absorption, distribution, metabolism, excretion and toxicity) analysis were used to retrieve novel PKM2 activators from commercially available chemical databases. Tetrahydroquinoline derivatives were identified as potential scaffolds of PKM2 activators. Thus, the hybrid virtual screening approach was applied to screen the focused tetrahydroquinoline derivatives embedded in the ZINC database. Six hit compounds were selected from the final hits and experimental studies were then performed. Compound 8 displayed a potent inhibitory effect on human lung cancer cells. Following treatment with Compound 8, cell viability, apoptosis, and reactive oxygen species (ROS) production were examined in A549 cells. Finally, we evaluated the effects of Compound 8 on mice xenograft tumor models in vivo. These results may provide important information for further research on novel PKM2 activators as antitumor agents.


Asunto(s)
Antineoplásicos/farmacología , Proteínas Portadoras/metabolismo , Descubrimiento de Drogas , Proteínas de la Membrana/metabolismo , Quinolinas/farmacología , Hormonas Tiroideas/metabolismo , Animales , Antineoplásicos/química , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos , Ensayos de Selección de Medicamentos Antitumorales , Citometría de Flujo , Humanos , Ratones , Modelos Moleculares , Estructura Molecular , Neoplasias Experimentales/tratamiento farmacológico , Neoplasias Experimentales/patología , Quinolinas/química , Especies Reactivas de Oxígeno/metabolismo , Relación Estructura-Actividad , Proteínas de Unión a Hormona Tiroide
8.
Antimicrob Agents Chemother ; 58(9): 5342-9, 2014 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-24982064

RESUMEN

To design and discover new antimicrobial peptides (AMPs) with high levels of antimicrobial activity, a number of machine-learning methods and prediction methods have been developed. Here, we present a new prediction method that can identify novel AMPs that are highly similar in sequence to known peptides but offer improved antimicrobial activity along with lower host cytotoxicity. Using previously generated AMP amino acid substitution data, we developed an amino acid activity contribution matrix that contained an activity contribution value for each amino acid in each position of the model peptide. A series of AMPs were designed with this method. After evaluating the antimicrobial activities of these novel AMPs against both Gram-positive and Gram-negative bacterial strains, DP7 was chosen for further analysis. Compared to the parent peptide HH2, this novel AMP showed broad-spectrum, improved antimicrobial activity, and in a cytotoxicity assay it showed lower toxicity against human cells. The in vivo antimicrobial activity of DP7 was tested in a Staphylococcus aureus infection murine model. When inoculated and treated via intraperitoneal injection, DP7 reduced the bacterial load in the peritoneal lavage solution. Electron microscope imaging and the results indicated disruption of the S. aureus outer membrane by DP7. Our new prediction method can therefore be employed to identify AMPs possessing minor amino acid differences with improved antimicrobial activities, potentially increasing the therapeutic agents available to combat multidrug-resistant infections.


Asunto(s)
Aminoácidos/química , Antiinfecciosos/uso terapéutico , Péptidos Catiónicos Antimicrobianos/uso terapéutico , Animales , Antiinfecciosos/efectos adversos , Antiinfecciosos/síntesis química , Antiinfecciosos/farmacología , Péptidos Catiónicos Antimicrobianos/efectos adversos , Péptidos Catiónicos Antimicrobianos/síntesis química , Péptidos Catiónicos Antimicrobianos/farmacología , Diseño de Fármacos , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Humanos , Masculino , Ratones , Ratones Endogámicos BALB C , Pruebas de Sensibilidad Microbiana , Microscopía Electrónica , Modelos Biológicos , Infecciones Estafilocócicas/tratamiento farmacológico , Staphylococcus aureus/efectos de los fármacos , Staphylococcus aureus/ultraestructura , Relación Estructura-Actividad
9.
ScientificWorldJournal ; 2014: 546176, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-24578646

RESUMEN

An amphiphilic polymer RGD-PEG-Chol which can be produced in large scale at a very low cost has been synthesized successfully. The synthesized intermediates and final products were characterized and confirmed by ¹H nuclear magnetic resonance spectrum (¹H NMR) and Fourier transform infrared spectrum (FT-IR). The paclitaxel- (PTX-) loaded liposomes based on RGD-PEG-Chol were then prepared by film formation method. The liposomes had a size within 100 nm and significantly enhanced the cytotoxicity of paclitaxel to B16F10 cell as demonstrated by MTT test (IC50 = 0.079 µg/mL of RGD-modified PTX-loaded liposomes compared to 9.57 µg/mL of free PTX). Flow cytometry analysis revealed that the cellular uptake of coumarin encapsulated in the RGD-PEG-Chol modified liposome was increased for HUVEC cells. This work provides a reasonable, facile, and economic approach to prepare peptide-modified liposome materials with controllable performances and the obtained linear RGD-modified PTX-loaded liposomes might be attractive as a drug delivery system.


Asunto(s)
Antineoplásicos Fitogénicos , Colesterol , Sistemas de Liberación de Medicamentos , Oligopéptidos , Paclitaxel , Polietilenglicoles , Animales , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Línea Celular , Colesterol/química , Colesterol/farmacología , Cumarinas/química , Cumarinas/farmacología , Evaluación Preclínica de Medicamentos , Células Endoteliales de la Vena Umbilical Humana , Humanos , Liposomas , Ratones , Oligopéptidos/química , Oligopéptidos/farmacología , Paclitaxel/química , Paclitaxel/farmacología , Polietilenglicoles/química , Polietilenglicoles/farmacología
10.
Chin J Integr Med ; 19(8): 610-5, 2013 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-22610956

RESUMEN

OBJECTIVE: To determine the changes in the levels of endogenous metabolites in rats with chronic immobilization stress (CIS) taking Xiaoyao Powder (XYP) and its modified prescription version, which lacks the volatile oils extracted from Herba Menthae. METHODS: Twenty-four experimental male SD rats were randomly divided into 4 groups of 6 rats each: control, model, XYP-1 (containing volatile oils from Herba Menthae), and XYP-2 (lacking volatile oils). All rats except control group rats were subjected to CIS 3 h per day for 21 consecutive days. Groups XYP-1 and XYP-2 were given the extracted XYS with or without volatile oils (3.854 g/kg; suspended in distilled water) via gavage 1 h before CIS each day for 21 days. Rats were anesthetized using intraperitoneal injection of pentobarbital sodium (40 mg/kg) on the 22nd day. Observations were made using a Varian INOVA 600 MHz NMR spectrometer at 27 °C. Carr-Purcell-Meiboom-Gill (CPMG) and longitudinal eddy-delay (LED) were applied, resulting in spectra showing only the signals from micro- and macro-metabolites. RESULTS: Compared to controls, rats subjected to CIS showed increased levels of plasma metabolites, such as acetic acid, choline, N-glycoprotein (NAC), saturated fatty acid, and blood sugars. Levels of low-density lipoprotein (LDL), very low-density lipoprotein (VLDL), and unsaturated fatty acids were decreased. The biochemical effects of XYS were characterized by elevated levels of VLDL, LDL, threonine, methionine, and glutamic acid in plasma. CONCLUSION: Some common and characteristic metabolites on the anti-CIS of XYP and its modified prescription were obtained. The metabolomics technology is a valuable tool and may be used to identify the specific metabolites and potential biomarkers of therapeutic effect of Chinese medicinal prescriptions.


Asunto(s)
Proteínas Sanguíneas/metabolismo , Medicamentos Herbarios Chinos/farmacología , Metaboloma/efectos de los fármacos , Estrés Psicológico/metabolismo , Animales , Proteínas Sanguíneas/efectos de los fármacos , Enfermedad Crónica , Evaluación Preclínica de Medicamentos , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/uso terapéutico , Masculino , Polvos , Ratas , Ratas Sprague-Dawley , Restricción Física , Estrés Psicológico/sangre , Estrés Psicológico/tratamiento farmacológico
11.
Artículo en Inglés | WPRIM | ID: wpr-347177

RESUMEN

<p><b>OBJECTIVE</b>To determine the changes in the levels of endogenous metabolites in rats with chronic immobilization stress (CIS) taking Xiaoyao Powder (XYP) and its modified prescription version, which lacks the volatile oils extracted from Herba Menthae.</p><p><b>METHODS</b>Twenty-four experimental male SD rats were randomly divided into 4 groups of 6 rats each: control, model, XYP-1 (containing volatile oils from Herba Menthae), and XYP-2 (lacking volatile oils). All rats except control group rats were subjected to CIS 3 h per day for 21 consecutive days. Groups XYP-1 and XYP-2 were given the extracted XYS with or without volatile oils (3.854 g/kg; suspended in distilled water) via gavage 1 h before CIS each day for 21 days. Rats were anesthetized using intraperitoneal injection of pentobarbital sodium (40 mg/kg) on the 22nd day. Observations were made using a Varian INOVA 600 MHz NMR spectrometer at 27 °C. Carr-Purcell-Meiboom-Gill (CPMG) and longitudinal eddy-delay (LED) were applied, resulting in spectra showing only the signals from micro- and macro-metabolites.</p><p><b>RESULTS</b>Compared to controls, rats subjected to CIS showed increased levels of plasma metabolites, such as acetic acid, choline, N-glycoprotein (NAC), saturated fatty acid, and blood sugars. Levels of low-density lipoprotein (LDL), very low-density lipoprotein (VLDL), and unsaturated fatty acids were decreased. The biochemical effects of XYS were characterized by elevated levels of VLDL, LDL, threonine, methionine, and glutamic acid in plasma.</p><p><b>CONCLUSION</b>Some common and characteristic metabolites on the anti-CIS of XYP and its modified prescription were obtained. The metabolomics technology is a valuable tool and may be used to identify the specific metabolites and potential biomarkers of therapeutic effect of Chinese medicinal prescriptions.</p>


Asunto(s)
Animales , Masculino , Ratas , Proteínas Sanguíneas , Metabolismo , Enfermedad Crónica , Evaluación Preclínica de Medicamentos , Medicamentos Herbarios Chinos , Química , Farmacología , Usos Terapéuticos , Metaboloma , Polvos , Ratas Sprague-Dawley , Restricción Física , Estrés Psicológico , Sangre , Quimioterapia , Metabolismo
12.
Int J Mol Sci ; 13(12): 15668-78, 2012 Nov 23.
Artículo en Inglés | MEDLINE | ID: mdl-23443087

RESUMEN

Focal adhesion kinase (FAK) is a tyrosine kinase that functions as a key orchestrator of signals leading to invasion and metastasis. In the current study, the multicomplex-based pharmacophore (MCBP)-guided method has been suggested to generate a comprehensive pharmacophore of FAK kinase based on seven crystal structures of FAK-inhibitor complexes. In this investigation, a hybrid protocol of virtual screening methods, comprising of pharmacophore model-based virtual screening (PB-VS) and docking-based virtual screening (DB-VS), is used for retrieving new FAK inhibitors from commercially available chemical databases. This hybrid virtual screening approach was then applied to screen several chemical databases, including the Specs (202,408 compounds) database. Thirty-five compounds were selected from the final hits and should be shifted to experimental studies. These results may provide important information for further research of novel FAK inhibitors.


Asunto(s)
Descubrimiento de Drogas , Quinasa 1 de Adhesión Focal/antagonistas & inhibidores , Quinasa 1 de Adhesión Focal/química , Simulación del Acoplamiento Molecular , Inhibidores de Proteínas Quinasas/química , Evaluación Preclínica de Medicamentos , Humanos
13.
J Med Chem ; 53(1): 273-81, 2010 Jan 14.
Artículo en Inglés | MEDLINE | ID: mdl-19904929

RESUMEN

A large amount of evidence suggests that monocytes/macrophages infiltration is implicated in a variety of inflammatory diseases including acute liver injury. Monocyte chemoattractant protein 1 (MCP-1) plays a crucial role in the process of macrophages recruitment. We herein presented a small-molecule library and a feasible quick screening method of evaluating potency of inhibition of chemotaxis of RAW264.7 cells stimulated by MCP-1. Fifty-three small molecules were synthesized and screened, and four compounds (2g, 2h, 4f, and 6h) showed inhibitory effects with IC(50) values range from 0.72 to 20.47 microM, with compound 4f being the most efficient. Further in vivo studies demonstrated that oral administration of 2g, 2h, 4f, or 6h decreases, most significantly for 4f, the serum levels of alanine aminotransaminase (ALT) and asparate aminotransaminase (AST) in ConA-induced acute livery injury BALB/c mice. Histopathological evaluation liver sections confirmed 4f as a potent, orally active compound for hepatoprotective effects against ConA-induced acute liver injury in BALB/c mice.


Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas , Descubrimiento de Drogas , Fallo Hepático Agudo/prevención & control , Tiazolidinedionas/administración & dosificación , Animales , Movimiento Celular/efectos de los fármacos , Células Cultivadas , Concanavalina A , Modelos Animales de Enfermedad , Evaluación Preclínica de Medicamentos , Femenino , Fallo Hepático Agudo/inducido químicamente , Fallo Hepático Agudo/patología , Pruebas de Función Hepática , Ratones , Ratones Endogámicos BALB C , Bibliotecas de Moléculas Pequeñas , Estereoisomerismo , Relación Estructura-Actividad , Tiazolidinedionas/síntesis química , Tiazolidinedionas/química , Tiazolidinedionas/farmacología
14.
Chinese Acupuncture & Moxibustion ; (12): 1003-1006, 2010.
Artículo en Chino | WPRIM | ID: wpr-322693

RESUMEN

<p><b>OBJECTIVE</b>To provide appropriate needling angle and depth for the acupuncture and acupoint injection at Neiguan (PC 6), and to avoid damaging nerves and vessels so as to produce its maximum effect.</p><p><b>METHODS</b>Thirty adults' upper-limb samples were used to dissect and observe the referred hierarchical structure and adjoining crucially nerves and vessels in needling Neiguan (PC 6) according to the national standard Acupoint Location (GB 12346-90).</p><p><b>RESULTS</b>In this punctuation region, there are three parts rich in connective tissues containing the nerves and blood vessels. The surface part is between the skin and the musculus flexor digitorum superficialis and it is the tissue which contains medial and lateral antebrachial cutaneous nerve and its nutrient artery. The middle part is between the musculus flexor digitorum superficialis and the flexor digitorum profundus muscle and contains the median nerve, its palmar branch of and artery. The deep part is between the pronator quadratus muscle and the interosseous membrane and contains the anterior interosseous nerve. When perpendicular needling, the depth of needling the body from skin to the superficial surface of the musculus flexor digitorum superficialis and to the superficial surface of the flexor digitorum profundus muscle is (6.68 +/- 0.64) mm and (12.37 +/- 0.87) mm respectively. The depth of needling the body from skin to the superficial surface of the pronator quadratus muscle and to the superficial surface of the anterior interosseous terminal branch of the nerves is (17.83 +/- 1.00) mm and (30.87 +/- 1.85) mm respectively, and the proportional cun is (2.20 +/- 0.14) cm. The ulnaris cord of median nerves are located at the radial of the needle. The deep layers could touch the anterior interosseous nerve ending.</p><p><b>CONCLUSION</b>Perpendicularly needling Neiguan (PC 6) for 3 fen (6.68 mm), 5 fen (12.37 mm) and 1.4 cun (30.87 mm) will stimulate the nervus vascularis of the rich part of surface, middle and deep connective tissues respectively and produce the acupuncture effect. During the acupoint injection, perforating the needle perpendicularly at the middle point of the two tendons or deviating slightly to the direction of tendon of palmaris longus can avoid the damage of the median nerve cord.</p>


Asunto(s)
Adulto , Humanos , Masculino , Puntos de Acupuntura , Terapia por Acupuntura , Vasos Sanguíneos , Músculo Esquelético , Tejido Nervioso
15.
Zhongguo Zhong Xi Yi Jie He Za Zhi ; 28(12): 1112-7, 2008 Dec.
Artículo en Chino | MEDLINE | ID: mdl-19317170

RESUMEN

OBJECTIVE: To provide a scientific basis for systematic research on the mechanism of chronic immobilization stress (CIS) induced metabolic network change in rats, through detecting the changes of endogenous metabolites in rats with CIS, treated or un-treated with Xiaoyao Powder (XYP), for determining the small molecule marker compound that closely associated with the metabonomical specificity of CIS and acting mechanism of XYP. METHODS: Thirty-six experimental male SD rats were divided into 3 groups, the normal control group, the model group and the XYP group. And all the three groups were subdivided into two subgroups respectively on day 7 and day 21 of the experiment. The stress rat model of CIS was made by chronic restraining method for 3 h every day. Starting from the first day of modeling, XYP 3.854 g/kg in volume of 1 mL/100 g body weight was administered 1 h before restraining via gastrogavage to rats in the XYP group, while equal volume of distilled water was given to rats in the other two groups instead. Blood samples were collected on the 8 th day and 22 th day for detection in the following procedure: at 27 degrees C, 300 microL supernate of blood plasma was taken, calling the Carr-Purcell-Meiboom-Gill (CPMG) and longitudinal eddy-delay (LED) sequence respectively on a Fourier variable nuclear magnetic resonance (NMR) spectrometer, pre-saturated inhibition of the water peak was performed; free induction decay (FID) signals were transferred via 32 k Fourier transformation to gain one-dimensional NMR spectrogram; by taking TSP as the chemical migration reference peak, the segmental integral calculus (0.04 ppm per segment) was performed from 4.5 - 0.5 ppm (CPMG) and 6.0 - 0 ppm (LED) within the peak ranges in 1H spectra using the VNMR software; after normalization, centering and scaling were conducted on data, then used for pattern recognition of principal component analysis (PCA) using the SIMCA-P 10.0 software, or if necessary, the partial least squares discriminate analysis (PLS-DA) was performed. RESULTS: (1) The metabolites in the model group were significantly different from those in the control group, suggesting that the animal model was successfully established with the metabolic network different to that of control. The model group and the XYP group could be differentiated from the control group by the differences of metabolites and metabolic networks between groups; XYP could intervene the metabolites or the metabolic path to cause changes in final metabolites. (2) The serum contents of lactic acid (1.4, 4.16), choline (3.24), N-acetylgalactosamine (NAC) and saturated fatty acids (1-3) increased, but unsaturated fatty acids (1.99,4-5), blood sugar (34), HDL (0.83), etc. reduced in the CIS rats. XYP showed obvious regulatory effects on final metabolites, causing decrease of lactic acid, choline, NAC, saturated fatty acids and blood sugar, and increase of unsaturated fatty acids, blood sugar, HDL, 3.44 ppm compound, etc. CONCLUSIONS: The metabolic phenotype in CIS rats includes the increase of lactic acid, choline, NAC, saturated fatty acid, and the decrease of blood sugar contents, unsaturated fatty acid, HDL, 3.44 ppm compound, etc., these may be the markers of the metabolites. The final metabolites changes induced by CIS are primarily the lipid substances. XYP markedly regulates the contents of final metabolites, showing the regulatory effects on final metabolites, but what is the metabolite or metabolic pathways it interferes to alter the final metabolites should be confirmed by further studies.


Asunto(s)
Medicamentos Herbarios Chinos/administración & dosificación , Metabolómica , Estrés Fisiológico/efectos de los fármacos , Animales , Análisis Químico de la Sangre , Modelos Animales de Enfermedad , Femenino , Humanos , Espectroscopía de Resonancia Magnética , Masculino , Polvos , Distribución Aleatoria , Ratas , Ratas Sprague-Dawley
16.
Artículo en Chino | WPRIM | ID: wpr-337571

RESUMEN

<p><b>OBJECTIVE</b>To provide a scientific basis for systematic research on the mechanism of chronic immobilization stress (CIS) induced metabolic network change in rats, through detecting the changes of endogenous metabolites in rats with CIS, treated or un-treated with Xiaoyao Powder (XYP), for determining the small molecule marker compound that closely associated with the metabonomical specificity of CIS and acting mechanism of XYP.</p><p><b>METHODS</b>Thirty-six experimental male SD rats were divided into 3 groups, the normal control group, the model group and the XYP group. And all the three groups were subdivided into two subgroups respectively on day 7 and day 21 of the experiment. The stress rat model of CIS was made by chronic restraining method for 3 h every day. Starting from the first day of modeling, XYP 3.854 g/kg in volume of 1 mL/100 g body weight was administered 1 h before restraining via gastrogavage to rats in the XYP group, while equal volume of distilled water was given to rats in the other two groups instead. Blood samples were collected on the 8 th day and 22 th day for detection in the following procedure: at 27 degrees C, 300 microL supernate of blood plasma was taken, calling the Carr-Purcell-Meiboom-Gill (CPMG) and longitudinal eddy-delay (LED) sequence respectively on a Fourier variable nuclear magnetic resonance (NMR) spectrometer, pre-saturated inhibition of the water peak was performed; free induction decay (FID) signals were transferred via 32 k Fourier transformation to gain one-dimensional NMR spectrogram; by taking TSP as the chemical migration reference peak, the segmental integral calculus (0.04 ppm per segment) was performed from 4.5 - 0.5 ppm (CPMG) and 6.0 - 0 ppm (LED) within the peak ranges in 1H spectra using the VNMR software; after normalization, centering and scaling were conducted on data, then used for pattern recognition of principal component analysis (PCA) using the SIMCA-P 10.0 software, or if necessary, the partial least squares discriminate analysis (PLS-DA) was performed.</p><p><b>RESULTS</b>(1) The metabolites in the model group were significantly different from those in the control group, suggesting that the animal model was successfully established with the metabolic network different to that of control. The model group and the XYP group could be differentiated from the control group by the differences of metabolites and metabolic networks between groups; XYP could intervene the metabolites or the metabolic path to cause changes in final metabolites. (2) The serum contents of lactic acid (1.4, 4.16), choline (3.24), N-acetylgalactosamine (NAC) and saturated fatty acids (1-3) increased, but unsaturated fatty acids (1.99,4-5), blood sugar (34), HDL (0.83), etc. reduced in the CIS rats. XYP showed obvious regulatory effects on final metabolites, causing decrease of lactic acid, choline, NAC, saturated fatty acids and blood sugar, and increase of unsaturated fatty acids, blood sugar, HDL, 3.44 ppm compound, etc.</p><p><b>CONCLUSIONS</b>The metabolic phenotype in CIS rats includes the increase of lactic acid, choline, NAC, saturated fatty acid, and the decrease of blood sugar contents, unsaturated fatty acid, HDL, 3.44 ppm compound, etc., these may be the markers of the metabolites. The final metabolites changes induced by CIS are primarily the lipid substances. XYP markedly regulates the contents of final metabolites, showing the regulatory effects on final metabolites, but what is the metabolite or metabolic pathways it interferes to alter the final metabolites should be confirmed by further studies.</p>


Asunto(s)
Animales , Femenino , Humanos , Masculino , Ratas , Análisis Químico de la Sangre , Modelos Animales de Enfermedad , Medicamentos Herbarios Chinos , Espectroscopía de Resonancia Magnética , Metabolómica , Polvos , Distribución Aleatoria , Ratas Sprague-Dawley , Estrés Fisiológico
17.
Zhong Xi Yi Jie He Xue Bao ; 5(3): 307-13, 2007 May.
Artículo en Chino | MEDLINE | ID: mdl-17498492

RESUMEN

OBJECTIVE: To determine the changes of the plasma metabolic phenotype in rats with chronic restraint stress (rats with syndrome of liver qi stagnation and spleen deficiency), so as to reveal the biological features of the syndrome of liver qi stagnation and spleen deficiency, and to examine potential application of metabonomic analysis in studies of syndromes in traditional Chinese medicine. METHODS: Twenty-four male Sprague-Dawley rats were randomly divided into four groups: group A, 7 d normal control group; group B, 21 d normal control group; group C, 7 d stress group; and group D, 21 d stress group, with 6 rats in each group. Chronic restraint was used to induce stress in rats. Blood was collected from the cardio-ventricle under anesthesia on the 8th (groups A and C) or 22nd day (groups B and D) and detected by using the Fourier variable superconducting nuclear magnetic resonance (NMR) spectrometer (Varian UnityInova 600 M). Free induction decay signals were transferred into one-dimensional NMR spectrogram via 32 k Fourier transformation. Segmental integral calculus (0.04 ppm per segment) was performed from 4.5-0.5 ppm (Carr-Purcell-Meiboom-Gill, CPMG) or 6.0-0 ppm (longitudinal eddy-delay, LED) as defaulted 1H spectra values by using the VNMR software. Data were saved as text or excel files after normalization and then used for pattern recognition analyses. All the data were analyzed by principal component analysis (PCA) using the SIMCA-P 10.0 software (Umetrics AB, Umea, Sweden). RESULTS: The PCA analysis of rat plasma (1)H NMR spectra revealed different metabolic spectra between stress and control groups, which were consistent with alterations of in vivo metabolisms in rats under stress stimuli. Compared with the normal control group, rats with repeated stress displayed significant changes in spectral peak shapes of acetate, lactate, tyrosine, low-density lipoprotein, and unknown compounds (3.44 ppm). These altered metabolites can be used as biomarkers of syndrome of liver qi stagnation and spleen deficiency for further studies. CONCLUSION: The (1)H NMR spectra of metabolites in the rat blood are differentially changed after chronic stress. Specific, characteristic metabolic products can be identified by analyses of metabonomics, which lead to interpretation of biological feature of Chinese medicine syndromes. Therefore, metabonomic analysis is an approach with good development prospects to studies of TCM syndromes.


Asunto(s)
Medicina Tradicional China , Estrés Psicológico/sangre , Estrés Psicológico/patología , Ácido Acético/sangre , Animales , Diagnóstico Diferencial , Ácido Láctico/sangre , Lipoproteínas LDL/sangre , Masculino , Resonancia Magnética Nuclear Biomolecular , Análisis de Componente Principal , Distribución Aleatoria , Ratas , Ratas Sprague-Dawley , Restricción Física , Estrés Psicológico/etiología , Síndrome
18.
Artículo en Chino | WPRIM | ID: wpr-307576

RESUMEN

<p><b>OBJECTIVE</b>To analyse the dynamical changes of the Ginkgo biloba's resources from 2001 to 2006, in Pizhou city, Jiangshu province by useing spatial analytical function of GIS and RS technology.</p><p><b>METHOD</b>Use the GIS and RS technology, extracted the information of G. biloba by scientific investigation, researched the spatial distribution and dynamical changes of G. biloba based on landsat 5 TM: the Apr. 3rd, 2001; Jan. 16th, 2005; July 30th, 2006.</p><p><b>RESULT</b>Ginkgo biloba's resource was 1.61 x 10(5) hm2 in 2001, 1.84 x 10(5) hm2 in 2005, 1.88 x 10(5) hm2 in 2006.</p><p><b>CONCLUSION</b>Ginkgo biloba's resource rised from 1.61 x 10(5) hm2 to 1.88 x 10(5) hm2 from 2001 to 2006, showed the gradually rise.</p>


Asunto(s)
China , Conservación de los Recursos Naturales , Ecosistema , Sistemas de Información Geográfica , Geografía , Ginkgo biloba , Plantas Medicinales , Dinámica Poblacional , Comunicaciones por Satélite
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