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1.
Fitoterapia ; 168: 105521, 2023 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-37146736

RESUMEN

Macathioureas A-D (1-4), four new thiourea derivatives with a carbamothioylpyrrolidine-2-carboxamide framework, were isolated from the roots of Lepidium meyenii (Maca) collected from Qujing, Yunnan Province of China. Their structures were identified based on extensive spectroscopic data, including 1D NMR, 2D NMR, and HRESIMS techniques. Their absolute configurations were assigned as 7S by the comparison of the experimental and predicted electronic circular dichroism (ECD) spectra. All the thiourea analogues were tested for their cytotoxicities against five human cancer cell lines. However, no significant activities were detected at concentrations up to 40 µM.


Asunto(s)
Lepidium , Humanos , Lepidium/química , China , Estructura Molecular , Raíces de Plantas/química , Línea Celular Tumoral , Extractos Vegetales/química
2.
Artículo en Chino | WPRIM | ID: wpr-970624

RESUMEN

Qijiao Shengbai Capsules(QJ) can invigorate Qi and replenish the blood, which is commonly used clinically for adjuvant treatment of cancer and leukopenia due to chemoradiotherapy. However, the pharmacological mechanism of QJ is still unclear. This work aims to combine the high-performance liquid chromatography(HPLC) fingerprints and network pharmacology to clarify the effective components and mechanism of QJ. The HPLC fingerprints of 20 batches of QJ were established. The similarity evaluation among 20 batches of QJ was performed by using Similarity Evaluation System for Chromatographic Fingerprint of Traditional Chinese Medicine(version 2012), resulting in a similarity greater than 0.97. Eleven common peaks were identified by reference standard, including ferulic acid, calycosin 7-O-glucoside, ononin, calycosin, epimedin A, epimedin B, epimedin C, icariin, formononetin, baohuoside I, and Z-ligustilide. The "component-target-pathway" network was constructed by network pharmacy, and 10 key components in QJ were identified, such as ferulic acid, calycosin 7-O-glucoside, ononin, and calycosin. The components were involved in the phosphoinositide 3 kinase-protein kinase B(PI3K-Akt), mitogen-activated protein kinase(MAPK), and other signaling pathways by regulating potential targets, including EGFR, RAF1, PIK3R1, and RELA, to auxiliarily treat tumors, cancers, and leukopenia. The molecular docking conducted on the AutoDock Vina platform confirmed the high binding activity of 10 key effective components with core targets, with the binding energy less than-5 kcal·mol~(-1). In this study, the effective components and mechanism of QJ have been preliminary revealed based on HPLC fingerprint and network pharmacology, which provided a basis for quality control of QJ and a refe-rence for further study on its mechanism.


Asunto(s)
Farmacología en Red , Cápsulas , Simulación del Acoplamiento Molecular , Fosfatidilinositol 3-Quinasas , Medicamentos Herbarios Chinos/farmacología
3.
Fitoterapia ; 157: 105133, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-35114336

RESUMEN

Six diterpenoids including three ent-kauranes (1-2, 4) and three cleistanthanes (3, 5-6) were isolated from the roots and stems of Phyllanthus acidus (L.) Skeels. Of them, (16S)-ent-16,17,18-tri-hydroxy-19-nor-kaur-4-en-3-one (1), phyllanthone A (2), and 6-hydroxycleistanthol (3) are new compounds, while the ent-kaurane diterpenoids were reported from the titled plant for the first time. Their structures were elucidated on the basis of the extensive spectroscopic analyses. Compounds 2 and 4-6 displayed cytotoxic potential with IC50 values ranging from 1.96 to 29.15 µM. They also showed moderate anti-inflammatory activities (IC50 = 6.30-12.05 µM). Particularly, the new ent-kaurane 2 displayed cytotoxic potential against HL-60 (IC50 = 2.00 µM) and MCF-7 (IC50 = 3.55 µM) cells, and anti-inflammatory activity (IC50 = 6.47 µM).


Asunto(s)
Diterpenos de Tipo Kaurano/toxicidad , Diterpenos/toxicidad , Phyllanthus/química , Extractos Vegetales/toxicidad , Alcaloides/química , Alcaloides/aislamiento & purificación , Alcaloides/toxicidad , Línea Celular Tumoral , Diterpenos/química , Diterpenos de Tipo Kaurano/química , Humanos , Concentración 50 Inhibidora , Espectroscopía de Resonancia Magnética , Estructura Molecular , Extractos Vegetales/síntesis química , Raíces de Plantas/química , Tallos de la Planta/química
4.
Artículo en Inglés | WPRIM | ID: wpr-939908

RESUMEN

Pseudo-allergic reactions (PARs) widely occur upon application of drugs or functional foods. Anti-pseudo-allergic ingredients from natural products have attracted much attention. This study aimed to investigate anti-pseudo-allergic compounds in licorice. The anti-pseudo-allergic effect of licorice extract was evaluated in rat basophilic leukemia 2H3 (RBL-2H3) cells. Anti-pseudo-allergic compounds were screened by using RBL-2H3 cell extraction and the effects of target components were verified further in RBL-2H3 cells, mouse peritoneal mast cells (MPMCs) and mice. Molecular docking and human MRGPRX2-expressing HEK293T cells (MRGPRX2-HEK293T cells) extraction were performed to determine the potential ligands of MAS-related G protein-coupled receptor-X2 (MRGPRX2), a pivotal target for PARs. Glycyrrhizic acid (GA) and licorice chalcone A (LA) were screened and shown to inhibit Compound48/80-induced degranulation and calcium influx in RBL-2H3 cells. GA and LA also inhibited degranulation in MPMCs and increase of histamine and TNF-α in mice. LA could bind to MRGPRX2, as determined by molecular docking and MRGPRX2-HEK293T cell extraction. Our study provides a strong rationale for using GA and LA as novel treatment options for PARs. LA is a potential ligand of MRGPRX2.


Asunto(s)
Animales , Humanos , Ratones , Ratas , Antialérgicos/uso terapéutico , Calcio/metabolismo , Degranulación de la Célula , Glycyrrhiza , Células HEK293 , Hipersensibilidad/tratamiento farmacológico , Mastocitos/metabolismo , Ratones Endogámicos C57BL , Simulación del Acoplamiento Molecular , Proteínas del Tejido Nervioso/metabolismo , Receptores Acoplados a Proteínas G/metabolismo , Receptores de Neuropéptido/uso terapéutico
5.
Anticancer Agents Med Chem ; 22(8): 1561-1570, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-34102992

RESUMEN

BACKGROUND: Fomitopsis officinalis (Vill. ex Fr. Bond. et Sing) is a medicinal mushroom, commonly called 'Agarikon'; it has traditionally been used to treat cough and asthma in the Mongolian population. OBJECTIVE: The objective of the study was to examine the significance of biological activity of F. officinalis and evaluation of the antioxidant activity and anticancer activity of six fractions of F. officinalis residues (Fo1-powder form dissolved in ethanol, Fo2-petroleum ether residue, Fo3-chloroformic, Fo4-ethylacetate, Fo5-buthanolic, and Fo6-waterethanolic) against hepatocellular carcinoma cells. METHODS: We performed in vitro studies of cell proliferation and viability assay, annexin V-FITC/Propidium Iodide assay, and NF-kB signaling pathway by immunoblot analysis. RESULTS: Our findings revealed that all six fractions/extracts have antioxidant activity, and somehow, they exert anticancerous effects against cancer cells. In cancerous cell lines (HepG2 and LO2), Fo3 chloroformic extract promoted the cancer cell apoptosis and cell viability, activated G2/M-phase cell cycle, and selectively induced NF-kB proteins, revealing as a novel antitumor extract. CONCLUSION: This study reports that Fo3-chloroformic extract is rich in antitumor activity, which was previously not investigated in cancer. To develop the impact of F. officinalis among natural products to treat/prevent oxidative stress disorders or cancers, further examinations of F. officinalis are needed to develop new natural drugs to treat cancer. However, this study assessed only one extract, Fo3-chloroformic, which has a significant impact against cancer cell lines.


Asunto(s)
Agaricales , Carcinoma Hepatocelular , Neoplasias Hepáticas , Antioxidantes/química , Antioxidantes/farmacología , Apoptosis , Carcinoma Hepatocelular/tratamiento farmacológico , Línea Celular , Proliferación Celular , Coriolaceae , Humanos , Neoplasias Hepáticas/tratamiento farmacológico , FN-kappa B , Extractos Vegetales/farmacología
6.
Biochim Biophys Acta Mol Basis Dis ; 1867(12): 166242, 2021 12 01.
Artículo en Inglés | MEDLINE | ID: mdl-34389474

RESUMEN

Endoplasmic reticulum (ER) stress, with adaptive unfolded protein response (UPR), is a key link between obesity, insulin resistance and type 2 diabetes, all of which are often present in the most common endocrine-metabolic disorder in women of reproductive age, polycystic ovary syndrome (PCOS), which is characterized with hyperandrogenism. However, the link between excess androgen and endoplasmic reticulum (ER) stress/insulin resistance in patients with polycystic ovary syndrome (PCOS) is unknown. An unexpected role of kisspeptin was reported in the regulation of UPR pathways and its involvement in the androgen-induced ER stress in hypothalamic neuronal cells. To evaluate the relationship of kisspeptin and ER stress, we detected kisspeptin and other factors in blood plasm of PCOS patients, rat models and hypothalamic neuronal cells. We detected higher testosterone and lower kisspeptin levels in the plasma of PCOS than that in non-PCOS women. We established a PCOS rat model by dihydrotestosterone (DHT) chronic exposure, and observed significantly downregulated kisspeptin expression and activated UPR pathways in PCOS rat hypothalamus compared to that in controls. Inhibition or knockdown of kisspeptin completely mimicked the enhancing effect of DHT on UPR pathways in a hypothalamic neuronal cell line, GT1-7. Kp10, the most potent peptide of kisspeptin, effectively reversed or suppressed the activated UPR pathways induced by DHT or thapsigargin, an ER stress activator, in GT1-7 cells, as well as in the hypothalamus in PCOS rats. Similarly, kisspeptin attenuated thapsigargin-induced Ca2+ response and the DHT- induced insulin resistance in GT1-7 cells. Collectively, the present study has revealed an unexpected protective role of kisspeptin against ER stress and insulin resistance in the hypothalamus and has provided a new treatment strategy targeting hypothalamic ER stress and insulin resistance with kisspeptin as a potential therapeutic agent.


Asunto(s)
Estrés del Retículo Endoplásmico/genética , Kisspeptinas/sangre , Neuronas/metabolismo , Síndrome del Ovario Poliquístico/genética , Andrógenos/efectos adversos , Animales , Diabetes Mellitus Tipo 2/metabolismo , Diabetes Mellitus Tipo 2/patología , Modelos Animales de Enfermedad , Retículo Endoplásmico/metabolismo , Retículo Endoplásmico/patología , Femenino , Hipotálamo/metabolismo , Hipotálamo/patología , Resistencia a la Insulina/genética , Kisspeptinas/genética , Neuronas/patología , Obesidad/metabolismo , Obesidad/patología , Síndrome del Ovario Poliquístico/sangre , Síndrome del Ovario Poliquístico/patología , Ratas , Testosterona/sangre , Respuesta de Proteína Desplegada/genética
7.
Artículo en Chino | WPRIM | ID: wpr-888012

RESUMEN

Isomers are widely distributed in Chinese herbal medicines,and can be discriminated by energy-resolved mass spectrometry( ER-MS). However,ER-MS was performed through direct injection of reference compounds with syringe pump,which encountered a significant technical barrier for high-throughput and automated measurements. Herein,online ER-MS was conducted using LC-MS platform,and a pair of isomers,kaempferol vs luteolin,were employed as a case study to illustrate and assess the utility of online ER-MS for isomeric discrimination. High-resolution tandem mass spectrometry data of both flavonoids were acquired on LC-QE-Orbitrap-MS,and the fragmentation pathways responsible for the primary fragment ions were proposed. The primary signal in MS1 occurred at m/z 285( [M-H]-),and the primary signals of either compound generated by retro-Diels-Alder fragmentation were observed at m/z 151 and 133. The spectral information was subsequently transferred onto LC-Qtrap-MS platform to carry out online ER-MS. Two precursor-to-product ion transition candidates were constructed as m/z 285>151 and 285>133,and either afterward derived a set of pseudo-ion transitions( PITs) and so forth,exactly corresponding to a series of progressive collision energies( eg-5,-8,-11 e V,and so on). All PITs were typed into the monitoring list of multiple reaction monitoring program to generate the peak area datasets. Either dataset was normalized using the highest values in the set and imported into Graph Pad Prism software to plot the Gaus-sian-shaped curve that was termed as the break-down graph. The apex of the regressive curve was termed as optimal collision energy( OCE). The OCE values corresponding to m/z 285>151 were calculated as-29. 06 e V and-35. 71 e V for kaempferol and luteolin,respectively. In the case of m/z 285>133,the OCEs were yielded as-44. 15 e V for kaempferol and-49. 01 e V for luteolin. With re-ference to their chemical structures,the location of hydroxyl group was regarded to be responsible for the differences of either m/z 285>151 or 285>133 between the isomers,attributing to their different bond properties. Above all,online ER-MS offers an eligible tool for isomeric discrimination,and provides meaningful information for the accurate chemical composition characterization based on LC-MS,which is not limited to Chinese herbal medicines.


Asunto(s)
Cromatografía Liquida , Flavonoides , Quempferoles , Luteolina , Espectrometría de Masas en Tándem
8.
Med Chem ; 17(9): 963-973, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33155927

RESUMEN

BACKGROUND: Reactive oxygen species are involved in the etiology and progress of many kinds of diseases such as cancer, cardiovascular diseases, inflammatory and neurodegenerative disorders. Epidemiological studies reported that fruits, vegetables, and wines containing a high percentage of phenolics and flavonoids showed a positive impact in treating inflammatory diseases, reducing cancer risk, and increasing life expectancy. OBJECTIVE: Some Mongolian medicinal plants were studied for their antioxidant activity and anticancer effects. METHODS: Selected Mongolian medicinal plant extracts were examined for their antioxidant activity by the DPPH-radical scavenging assay, the content of phenolics and flavonoids by Folin-Ciocalteu and the Dowd method, respectively, and anti-cancer activities in human hepatoma cell line HepG2 cells by MTT assay. RESULTS: Methanol extract from Hippophae rhamnoides L. leaf and ethanol extract from Artemisia macrocephala Jacq. ex Bess. showed the highest efficiency to scavenge free radicals. Ethanol extracts from Hippophae rhamnoides L. grain and Paeonio anomala L. leaf showed the highest total phenolics content, whereas Hippophae rhamnoides L. fruit methanol extract and ethanol extract from Caragana leucophloea pojark. mentioned the highest flavonoids content. The Artemisia macrocephala Jacq. ex Bess seed wallet and Paeonia anomala L. seed wallet showed the most potent antiproliferative effects against human liver cancer HepG2 cell line. Gnetin-H compound was isolated from the Paeonio anomala L. seed wallet extract, and its molecular structure was determined by 1H and 13C NMR spectrum and IR spectroscopy methods. CONCLUSION: The screening study on anti-oxidative effects of 21 extracts from 15 Mongolian medicinal plants showed anti-oxidative activities and was rich in phenolics and flavonoids. Among these, methanol extract of the Hippophae rhamnoides L. leaf showed a better anti-oxidative effect than the ethanol extract. Artemisia macrocephala Jacq. ex Bess and Paeonia anomala L. seed wallet mentioned the best anti-cancer effects. Gnetin-H, methyl gallate, ethylgallate were the major components in the extract from the Paeonio anomala L. seed wallet. Finally, the molecular structure of gnetin-H was determined by NMR and IR spectroscopy. Further investigation, especially in vivo antioxidant activity, is needed to justify the use of a natural source of antioxidants to prevent the progression of diseases such as cancer.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Extractos Vegetales/farmacología , Plantas Medicinales/química , Resorcinoles/química , Estilbenos/química , Antineoplásicos Fitogénicos/química , Antioxidantes/química , Evaluación Preclínica de Medicamentos , Flavonoides/análisis , Frutas/química , Células Hep G2 , Humanos , Espectroscopía de Resonancia Magnética , Estructura Molecular , Mongolia , Paeonia/química , Fenoles/análisis , Extractos Vegetales/química , Resorcinoles/aislamiento & purificación , Semillas/química , Estilbenos/aislamiento & purificación
9.
Artículo en Chino | WPRIM | ID: wpr-873017

RESUMEN

Objective:The effects of Atractylodes lancea, A. coreana, A. japonica, A. chinensis and Atractylodis Macrocephalae Rhizoma on spleen-Qi deficiency rats were compared. Method:A model of spleen-Qi deficiency was induced in rats by diet and overwork.The rats are given different suspensions of A.japonica, A.chinesis, A.coreana, A.lancea and Atractylodis Macrocephalae Rhizoma To test the indicators of the digestive system, immune system and antioxidant enzyme system related to spleen deficiency.Compare the similarities and differences between Atractylodis Macrocephalae Rhizoma and Atractylodis Rhizoma from four different sources. Result:All the drug-administered groups can increase the levels of γ interferon (IFN-γ), gastric secrete element(GAS),serum amylase (AMS) and catalase(CAT) in rats with spleen-deficiency syndrome,in addition to the CAT index, the other indicators of the A. coreana, A.japonica, and A.lancea were significantly increased(P<0.05). The MTL content of the A.chinesis, A.lancea, A.coreana and A.japonica increased and was significant(P<0.05). The SDH content of A.japonica.and A.chinesis increased, and the difference was not significant.The increase of GSH-Px in the A.chinesis is significant(P<0.05). All the drug-administered groups can reduce the content of IgG, TNF-α and MDA in rats with spleen deficiency and deficiency syndrome. Among them, the IgG content of the A.chinesis. and the A.lancea was significantly decreased(P<0.05). The content of TNF-α in A.japonica group was significantly decreased(P<0.05). The content of MDA in the A.chinesis, the A.lancea, the A.coreana,the A.japonica and the Atractylodis Macrocephalae Rhizoma were significantly decreased(P<0.05).The decrease of IL-6 in the A.lancea was significant(P<0.05). Conclusion:Four different sources of Atractylodes Rhizome and A.macrocephala have certain therapeutic effects on spleen-deficiency rats with deficiency syndrome.The therapeutic effect of A.lancea and A.japonica is basically the same,regulating the absorption,secretion and elimination of inflammation in the digestive system of rats with spleen deficiency A.coreana, A.chinesis, and Atractylodis Macrocephalae Rhizoma have certain regulatory effects in the digestive system, digestive tract inflammation, and antioxidant enzymes.

10.
Artículo en Inglés | WPRIM | ID: wpr-827079

RESUMEN

OBJECTIVES@#To develop a new Chinese medicine (CM)-based drug and to evaluate its safety and effect for suppressing acute respiratory distress syndrome (ARDS) in COVID-19 patients.@*METHODS@#A putative ARDS-suppressing drug Keguan-1 was first developed and then evaluated by a randomized, controlled two-arm trial. The two arms of the trial consist of a control therapy (alpha interferon inhalation, 50 µg twice daily; and lopinavir/ritonavir, 400 and 100 mg twice daily, respectively) and a testing therapy (control therapy plus Keguan-1 19.4 g twice daily) by random number table at 1:1 ratio with 24 cases each group. After 2-week treatment, adverse events, time to fever resolution, ARDS development, and lung injury on newly diagnosed COVID-19 patients were assessed.@*RESULTS@#An analysis of the data from the first 30 participants showed that the control arm and the testing arm did not exhibit any significant differences in terms of adverse events. Based on this result, the study was expanded to include a total of 48 participants (24 cases each arm). The results show that compared with the control arm, the testing arm exhibited a significant improvement in time to fever resolution (P=0.035), and a significant reduction in the development of ARDS (P=0.048).@*CONCLUSIONS@#Keguan-1-based integrative therapy was safe and superior to the standard therapy in suppressing the development of ARDS in COVID-19 patients. (Trial registration No. NCT04251871 at www.clinicaltrials.gov ).


Asunto(s)
Adulto , Femenino , Humanos , Masculino , Persona de Mediana Edad , Administración por Inhalación , China , Infecciones por Coronavirus , Diagnóstico , Quimioterapia , Mortalidad , Relación Dosis-Respuesta a Droga , Esquema de Medicación , Medicamentos Herbarios Chinos , Estudios de Seguimiento , Medicina Integrativa , Interferón-alfa , Lopinavir , Pandemias , Neumonía Viral , Diagnóstico , Quimioterapia , Mortalidad , Medición de Riesgo , Síndrome Respiratorio Agudo Grave , Diagnóstico , Quimioterapia , Mortalidad , Índice de Severidad de la Enfermedad , Tasa de Supervivencia
11.
Artículo en Inglés | WPRIM | ID: wpr-827441

RESUMEN

OBJECTIVES@#To develop a new Chinese medicine (CM)-based drug and to evaluate its safety and effect for suppressing acute respiratory distress syndrome (ARDS) in COVID-19 patients.@*METHODS@#A putative ARDS-suppressing drug Keguan-1 was first developed and then evaluated by a randomized, controlled two-arm trial. The two arms of the trial consist of a control therapy (alpha interferon inhalation, 50 µg twice daily; and lopinavir/ritonavir, 400 and 100 mg twice daily, respectively) and a testing therapy (control therapy plus Keguan-1 19.4 g twice daily) by random number table at 1:1 ratio with 24 cases each group. After 2-week treatment, adverse events, time to fever resolution, ARDS development, and lung injury on newly diagnosed COVID-19 patients were assessed.@*RESULTS@#An analysis of the data from the first 30 participants showed that the control arm and the testing arm did not exhibit any significant differences in terms of adverse events. Based on this result, the study was expanded to include a total of 48 participants (24 cases each arm). The results show that compared with the control arm, the testing arm exhibited a significant improvement in time to fever resolution (P=0.035), and a significant reduction in the development of ARDS (P=0.048).@*CONCLUSIONS@#Keguan-1-based integrative therapy was safe and superior to the standard therapy in suppressing the development of ARDS in COVID-19 patients. (Trial registration No. NCT04251871 at www.clinicaltrials.gov ).


Asunto(s)
Adulto , Femenino , Humanos , Masculino , Persona de Mediana Edad , Administración por Inhalación , China , Infecciones por Coronavirus , Diagnóstico , Quimioterapia , Mortalidad , Relación Dosis-Respuesta a Droga , Esquema de Medicación , Medicamentos Herbarios Chinos , Estudios de Seguimiento , Medicina Integrativa , Interferón-alfa , Lopinavir , Pandemias , Neumonía Viral , Diagnóstico , Quimioterapia , Mortalidad , Medición de Riesgo , Síndrome Respiratorio Agudo Grave , Diagnóstico , Quimioterapia , Mortalidad , Índice de Severidad de la Enfermedad , Tasa de Supervivencia
12.
J Ethnopharmacol ; 239: 111894, 2019 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-31026555

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Breynia fruticosa is a folk medicine in China, traditionally used to treat gastroenteritis, sore throat, eczema and arthritis. However, the bioactive ingredients are unknown. AIM OF THE STUDY: To identify and isolate the anti-inflammatory ingredients of B. fruticosa. MATERIALS AND METHODS: B. fruticosa extracts were fractioned by Amberchrom CG161M and Toyopearl HW40C resins. Acetic acid-induced capillary permeability mice model was used to evaluate the anti-inflammation activities of fractions. The anti-inflammatory ingredients were identified by high performance liquid chromatography/mass spectroscopy (HPLC-MS). On-line two dimensional liquid chromatography system was constructed to remove the tannins and enrich the breynins. The breynins were purified by preparative HPLC and evaluated for their anti-arthritis activities using complete Freund's adjuvant (CFA) induced arthritis rats model. RESULTS: The anti-inflammatory ingredients of B. fruticosa are sulfur containing sesquiterpenoids (breynins). The on-line two dimensional preparative liquid chromatography system can effectively remove the tannins and enrich the bioactive ingredients in large scale within 1 h. Four major breynins were purified, and their structures were elucidated by analysis of MS and NMR data. Breynins can significantly prevent the rats' arthritis deterioration, with inhibition ratio 50% at dose 0.2 mg kg-1, comparable with that of indomethacin at dose 2 mg kg-1. CONCLUSION: The breynins have strong anti-arthritis activities, which is responsible to the anti-inflammatory effects of B. fruticosa. However, breynins are also toxic components of B. fruticosa.


Asunto(s)
Antiinflamatorios/uso terapéutico , Artritis Experimental/tratamiento farmacológico , Artritis Reumatoide/tratamiento farmacológico , Magnoliopsida , Extractos Vegetales/uso terapéutico , Sesquiterpenos/uso terapéutico , Ácido Acético , Animales , Antiinflamatorios/aislamiento & purificación , Antiinflamatorios/farmacología , Permeabilidad Capilar/efectos de los fármacos , Femenino , Dosificación Letal Mediana , Masculino , Medicina Tradicional China , Ratones , Extractos Vegetales/farmacología , Ratas Sprague-Dawley , Sesquiterpenos/aislamiento & purificación , Sesquiterpenos/farmacología
13.
Artículo en Inglés | WPRIM | ID: wpr-776865

RESUMEN

In the present study, we investigated anti-inflammatory effect of Cardamine komarovii flower (CKF) on lipopolysaccharide (LPS)-induced acute lung injury (ALI). We determined the effect of CKF methanolic extracts on LPS-induced pro-inflammatory mediators NO and prostaglandin E2 (PGE2), production of pro-inflammatory cytokines (IL-1β, TNF-α, and IL-6), and related protein expression levels of MyD88/TRIF signaling pathways in peritoneal macrophages (PMs). Nuclear translocation of NF-κB-p65 was analyzed by immunofluorescence. For the in vivo experiments, an ALI model was established to detect the number of inflammatory cells and inflammatory factors (IL-1β, TNF-α, and IL-6) in bronchoalveolar lavage fluid (BALF) of mice. The pathological damage in lung tissues was evaluated through H&E staining. Our results showed that CKF can decrease the production of inflammatory mediators, such as NO and PGE2, by inhibiting their synthesis-related enzymes iNOS and COX-2 in LPS-induced PMs. In addition, CKF can downregulate the mRNA levels of IL-1β, TNF-α, and IL-6 to inhibit the production of inflammatory factors. Mechanism studies indicated that CKF possesses a fine anti-inflammatory effect by regulating MyD88/TRIF dependent signaling pathways. Immunocytochemistry staining showed that the CKF extract attenuates the LPS-induced translocation of NF-kB p65 subunit in the nucleus from the cytoplasm. In vivo experiments revealed that the number of inflammatory cells and IL-1β in BALF of mice decrease after CKF treatment. Histopathological observation of lung tissues showed that CKF can remarkably improve alveolar clearance and infiltration of interstitial and alveolar cells after LPS stimulation. In conclusion, our results suggest that CKF inhibits LPS-induced inflammatory response by inhibiting the MyD88/TRIF signaling pathways, thereby protecting mice from LPS-induced ALI.


Asunto(s)
Animales , Femenino , Humanos , Masculino , Ratones , Lesión Pulmonar Aguda , Quimioterapia , Genética , Metabolismo , Proteínas Adaptadoras del Transporte Vesicular , Genética , Metabolismo , Antiinflamatorios , Química , Cardamine , Química , Ciclooxigenasa 2 , Genética , Metabolismo , Flores , Química , Lipopolisacáridos , Factor 88 de Diferenciación Mieloide , Genética , Metabolismo , FN-kappa B , Genética , Metabolismo , Óxido Nítrico Sintasa de Tipo II , Genética , Metabolismo , Extractos Vegetales , Química , Transducción de Señal , Factor de Necrosis Tumoral alfa , Genética , Metabolismo
14.
Journal of Medical Postgraduates ; (12): 954-957, 2019.
Artículo en Chino | WPRIM | ID: wpr-818354

RESUMEN

Objective At present, there are few reports on the stability of carotid plaque and left ventricular function at home and abroad. The article investigated the factors influencing the stability of left ventricular function on carotid atherosclerotic plaque. Methods 90 patients with carotid atherosclerosis (carotid intima-media thickness >0.2 cm) admitted in the Department of Neurology, Jiangsu Provincial Hospital of Traditional Chinese Medicine from June 10, 2017 to January 8, 2019 were selected and their stability of plaques was graded by contrast-enhanced ultrasound (CEUS). The patients were divided into two groups according to the stability of plaque. The differences of general clinical data, related biochemical indexes and left ventricular function indexes between the two groups were compared. The effects of left ventricular structural function on plaque stability were examined by logistic multivariate regression analysis. Results Univariate analysis showed that E peak (χ2=2.170, P=0.034), ventricular septal thickness (χ2=-1.972, P=0.049), diabetes history (χ2=10.102, P=0.001) were the risk factors of plaque stability and the differences were statistically significant (P < 0.05). Multivariate analysis showed that E peak (OR=0.022, P=0.014) and diabetes history (OR=0.185, P=0.002) were independent influencing factors of plaque stability. Conclusion There is an independent correlation between left ventricular function and plaque stability, and plaque stability can predict changes in ventricular structural function.

15.
Fitoterapia ; 125: 89-93, 2018 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-29288714

RESUMEN

Four new cleistanthane diterpenoids, phyllaciduloids A-D (1-4), were isolated from the roots and stems of Phyllanthus acidus (L.) Skeels (Phyllanthaceae). Their structures were elucidated on the basis of extensive spectroscopic analysis. Phyllaciduloids B-D (2-4) present in their structures with ether bond between C-7 and C-16, which were rarely reported. All the isolates were evaluated for their cytotoxic activities against five human cancer cell lines.


Asunto(s)
Diterpenos/aislamiento & purificación , Phyllanthus/química , Antineoplásicos Fitogénicos , Línea Celular Tumoral , Humanos , Estructura Molecular , Raíces de Plantas/química , Tallos de la Planta/química
16.
Artículo en Chino | WPRIM | ID: wpr-852759

RESUMEN

Bletillae striata is an important Chinese materia medica of traditional whitening recipe. This paper systematically expounded the traditional theory and modern pharmacological research of whitening from multiple perspectives for B. striata, such as Chinese medicine theory in whitening and its historical evolution, modern biological and pharmacological mechanism studies of whitening, and the related chemical composition in B. striata for "white treat black". And then, the industrial development idea of B. striata was initially proposed. This research provided an important idea and reference for the development and industrialization of B. striata whitening effect.

17.
Artículo en Chino | WPRIM | ID: wpr-338237

RESUMEN

Guizhi Decoction was one of the most commonly used traditional Chinese Medicine which possesses the effects of "jie-ji-fa-biao, regulating Ying and Wei". It was mainly used to treat mind-cold due to exogenous evils such as fever, headache, sweating, hate the wind, et al. Modern studies indicated that the chemical constituents of Guizhi decoction mainly include phenylpropanoid, monoterpenes, organic acids, flavonoids, triterpenoid saponins and so on. Pharmacological experimental studies had shown that Guizhi decoction could play a big role in dual-directional regulation on sweat gland, body temperature, immune function, gastrointestinal peristalsis, and blood pressure, and could also play the role of anti-inflammatory, antibacterial, antiviral, anti-allergic, analgesic, hypoglycemic, and cardiovascular protection. Many diseases such as internal, external, gynecological and pediatric diseases were treated in the clinical by using Guizhi decoction and its analogous formulae involving circulatory, immune, urinary, reproductive, endocrine, digestive, nervous and other systems. This article reviews the latest research progress of Guizhi decoction from three aspects: chemical constituents, pharmacological mechanism and clinical application. It will provide reference for further research and development of Guizhi decoction.

18.
Nat Prod Res ; 30(4): 419-25, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-25791206

RESUMEN

During the process of exploring bioactive lead compounds from Phyllanthus species, two new glycosides including an arylnaphthalene lignan, diphyllin 4-O-α-L-arabinopyranosyl-(1 → 3)-α-L-arabinopyranoside (1), and a phenolic compound, 3,4,5-trimethoxybenzyl alcohol 7-O-α-L-arabinofuranosyl-(1 → 6)-ß-D-glucopyranoside (2), were isolated from the methanol extract of the whole plants of Phyllanthus glaucus Wall. ex Müll. Arg. In addition, 31 known compounds, including 19 lignan derivatives (3-21), four phenylpropanoids (22-25), seven simple phenolics (26-32) and one monoterpenoid (33) were obtained. Their structures were determined on the basis of the HR-ESI-MS, 1D and 2D NMR spectroscopic analysis, and pre-column derivative/chiral HPLC analysis in case of 1 for the absolute configurations. All these compounds were obtained from P. glaucus for the first time. Moreover, the known lignan glycoside, phyllanthusmin C (5) showed in vitro cytotoxicities against HL-60, MCF-7 and SW480 cells with IC50 values of 9.2 ± 0.2, 19.2 ± 1.7 and 20.5 ± 0.9, respectively.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Disacáridos/farmacología , Glicósidos/farmacología , Lignanos/farmacología , Phyllanthus/química , Antineoplásicos Fitogénicos/química , Benzodioxoles , Línea Celular Tumoral , Cromatografía Líquida de Alta Presión , Disacáridos/química , Disacáridos/aislamiento & purificación , Humanos , Espectroscopía de Resonancia Magnética , Monoterpenos/química , Fenoles/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Espectrometría de Masa por Ionización de Electrospray
19.
Chinese Herbal Medicines ; (4): 12-23, 2016.
Artículo en Chino | WPRIM | ID: wpr-842239

RESUMEN

Herba Epimedii is widely used as a traditional Chinese medicine for "strengthening the kidney" and "reinforcing bone" for a long time in China and other Asian countries. In this study, based on the large number of domestic and international references and research results, the authors reviewed pharmacological effects and the clinical application of species in genus Epimedium L. Meanwhile, chemical conversion and biotransformation of the major active compounds during the processing of the plants in Epimedium L. and their metabolism in vivo were summarized. This provides a guidance for the application and development in clinical therapy in the future.

20.
Artículo en Chino | WPRIM | ID: wpr-503378

RESUMEN

BACKGROUND:The three-dimensional structure of acupoint anatomy was integrated into the teaching of acupuncture manipulation. Combined with the implementation and application of the acupuncture and moxibustion in digital virtual human, it can greatly improve the teaching effect and learning interest. OBJECTIVE:To investigate the acupuncture virtual human with integration of virtual reality force feedback technology and tissue deformation. METHODS:Using virtual reality technology, with computer as the core, we generated a specific range of virtual environment with realistic visual, auditory and tactile integration, col ected clinical expert acupuncture technique, matched the sensing equipment that can reflect the intensity, displacement and speed sensing of acupuncture. Based on image segmentation of virtual human, we constructed human tissue mechanics model, built virtual acupuncture-force-feedback system, and faithful y transmitted to the operator by a force feedback device. On one hand, based on VOXEL-MAN virtual human development platform, we finished the three-dimensional browser redevelopment of the science of acupuncture and moxibustion of Shu acupoint, which provided visual perception for people. On the other hand, based on modern biomechanics theory, we established models by graphics and image processing technology and force feedback technology. The stress process of the structure of each layer in the acupuncture point area was given to people in a sense of touch by the manner of virtual reality and force feedback. RESULTS AND CONCLUSION:With the man-machine interactive operation platform of virtual acupuncture force feedback system, operator could see the dynamic process of acupuncture needle into human body, and could feel the real counterforce in the control terminal of force feedback instrument. By operating acupuncture needle in virtual environment of force feedback instrument, acupuncture was performed in virtual human. The system meets the two requirements:the feedback changes produced by tissue interaction were similar to real acupuncture feedback force data measured by instrument. The acupuncture needle entered into different tissues, a sense of power changed significantly;there was progressive feeling with different layers, reaching a realistic experience. During the whole training, the image was smooth;virtual needle was responsive, which better meets the requirements of virtual reality.

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