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1.
Fitoterapia ; 175: 105915, 2024 Mar 19.
Artículo en Inglés | MEDLINE | ID: mdl-38508499

RESUMEN

Four undescribed ginkgolides, including two rare sesquiterpene ginkgolides (compounds 1 and 2) and two diterpenoid ginkgolides (compounds 3 and 4), were isolated from Ginkgo biloba L. The structures of these four ginkgolides were identified based on extensive spectroscopic analysis, DP4+ probability analysis and X-ray diffraction. Compounds 1 and 2 exhibited excellent antiplatelet aggregation activities with IC50 values of 1.20 ± 0.25 and 4.11 ± 0.34 µM, respectively.

2.
Phytomedicine ; 128: 155397, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38547623

RESUMEN

BACKGROUND: Acute lung injury (ALI) often leads to serious respiratory diseases with high incidence rates and mortality. For centuries, Xiebai San (XBS) has been a classical traditional Chinese medicine (TCM) about respiratory illness such as pneumonia in children. However, the related mechanism of XBS against ALI remains indistinct. PURPOSE: To reveal specific targets of XBS in lipopolysaccharide (LPS)-induced ALI mice using integrated pharmacology. STUDY DESIGN: The integrated method was to expound mechanism and targets of XBS inhibited ALI. METHODS: The primary components in XBS were identified by ultra high performance liquid chromatography-quadrupole time of flight-mass spectrometry (UHPLC-QTOF-MS). The potential drug targets were established using network pharmacology. The anti-ALI effect of XBS was evaluated in mice. Additionally, therapeutic targets were screened by integrating metabolome and transcriptome and verified in lung tissue. RESULTS: In total, 163 chemical components were identified in XBS, and a network of "3 drugs-18 components-86 targets" for XBS against ALI was constructed. In ALI mice, XBS alleviated lung inflammation by decreasing permeation and expression of neutrophils, tumor necrosis factor α (TNF-α), interleukin-6 (IL-6), and interleukin-1ß (IL-1ß) in bronchoalveolar lavage fluid (BALF), serum, and lung tissue. Next, the transcriptome of lung tissue was analyzed and enriched, indicating the importance of mitogen-activated protein kinase (MAPK), Janus kinase-signal transducer and activator of transcription (JAK-STAT), and others, which was consistent with network pharmacology prediction. Also, western blotting and immunohistochemistry results showed that XBS was against ALI mainly by inhibiting extracellular signal regulated kinase (ERK) and signal transducer and activator of transcription 3 (Stat3) phosphorylation. In addition, the metabolome of lung tissue revealed that XBS mainly regulated pathways involved in arachidonic acid, glycerophospholipid, and tryptophan metabolisms. The expression levels of leukotriene, phosphatidylcholine, kynurenine, and others were also verified. CONCLUSION: XBS alleviated inflammation of ALI by inhibiting the phosphorylation of the ERK/Stat3 pathway and regulating arachidonic acid, glycerophospholipid, and tryptophan metabolisms. This study will guide clinical precision medicine and promote modernization of XBS.


Asunto(s)
Lesión Pulmonar Aguda , Medicamentos Herbarios Chinos , Factor de Transcripción STAT3 , Lesión Pulmonar Aguda/tratamiento farmacológico , Lesión Pulmonar Aguda/metabolismo , Animales , Factor de Transcripción STAT3/metabolismo , Medicamentos Herbarios Chinos/farmacología , Ratones , Masculino , Fosforilación/efectos de los fármacos , Lipopolisacáridos , Sistema de Señalización de MAP Quinasas/efectos de los fármacos , Pulmón/efectos de los fármacos , Pulmón/metabolismo , Ratones Endogámicos C57BL , Modelos Animales de Enfermedad , Farmacología en Red , Transducción de Señal/efectos de los fármacos
3.
Zhongguo Zhong Yao Za Zhi ; 48(20): 5460-5473, 2023 Oct.
Artículo en Chino | MEDLINE | ID: mdl-38114139

RESUMEN

This study aims to establish the ultra-performance liquid chromatography(UPLC) fingerprint and multi-indicator quantitative analysis method for Schisandrae Sphenantherae Fructus(SSF) and to screen out the potential quality markers(Q-markers) of hepatoprotection based on network pharmacology. The similarity analysis was performed using the Chinese Medicine Chromatographic Fingerprint Similarity Evaluation System, which showed that the similarity of the fingerprints of 15 samples from different regions ranged from 0.981 to 0.998. Eighteen common components were identified, from which 3 differential components were selected by cluster analysis and principal component analysis. The "component-target-pathway" network was built to predict the core components related to the hepatoprotective effects. Fourteen core components were screened by network pharmacology. They acted on the targets such as AKT1, CCND1, CYP1A1, CYP3A4, MAPK1, MAPK3, NOS2, NQO1, and PTGS2 to regulate the signaling pathways of lipid metabolism and atherosclerosis, hepatitis B, interleukin-17, and tumor necrosis factor. Considering the chemical measurability, characteristics, and validity, schisantherin A, anwulignan, and schisandrin A were identified as the Q-markers. The content of schisantherin A, anwulignan, and schisandrin A in the test samples were 0.20%-0.57%, 0.13%-0.33%, and 0.42%-0.70%, respectively. Combining the fingerprint, network pharmacology, and content determination, this study predicted that schisantherin A, anwulignan, and schisandrin A were the Q-markers for the hepatoprotective effect of SSF. The results can provide reference for improving the quality evaluation standard and exploring the hepatoprotective mechanism of SSF.


Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas , Medicamentos Herbarios Chinos , Schisandra , Schisandra/química , Farmacología en Red , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/química , Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico
4.
Mol Breed ; 43(5): 34, 2023 May.
Artículo en Inglés | MEDLINE | ID: mdl-37312744

RESUMEN

Japanese apricot (Prunus mume Sieb. et Zucc.) is a traditional woody flower and fruit tree restrictedly cultivated in northern area due to its inability to survive harsh winters and early springs. In the current study, RNA-seq and physiological assay were used to study the cold response of P. mume 'Xuemei'. A total of 4705 genes were identified as differentially expressed genes (DEGs) in the 21 pairwise comparisons among seven time points under 0 °C cold treatment, and 3678 of them showed differential levels compared with control at normal temperature. The gene expression profiles indicated that the number of upregulated genes increased with prolongation of treatment time throughout the whole 48 h. Hierarchical clustering suggested three obvious phases of the gene expression profiles. Gene ontology (GO) analysis of the 4705 DEGs resulted in 102 significantly enriched GO items in which the transcription activity was dominant. 225 DEGs were predicted to encode transcription factor (TF) genes. Some important TFs (ERF, CBF, WRKY, NAC, MYB, bHLH) were strongly induced during the whole cold treatment. Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis suggested that plant signal transduction pathways such as plant hormone and calcium (Ca2+) were notable. Metabolic pathways such as sugar metabolism, especially RFOs (raffinose family oligosaccharides) were activated, which was accompanied by the accumulation of soluble sugars. SOD and POD enzyme activities coupled with reactive oxygen species (ROS)-related gene expression profile implied a gradually induced ROS scavenging system under cold treatment. These results might shed light on the sensitivity to cold stress in Japanese apricot and provide new insights into hardiness studies in P. mume and its related species. Supplementary Information: The online version contains supplementary material available at 10.1007/s11032-023-01376-2.

5.
Zhongguo Zhong Yao Za Zhi ; 48(6): 1700-1704, 2023 Mar.
Artículo en Chino | MEDLINE | ID: mdl-37005858

RESUMEN

Chinese patent medicines(CPMs) are unique therapeutic drugs in China. Establishing and improving the evaluation criteria is an important measure to promote the high-quality development of CPMs. Based on the "evaluation criteria of high-grade CPMs with quality as the core index" established by our group in 2018, the "high-quality evaluation criteria for CPMs based on whole process control" was proposed in the present study in 2022. The scope of application and basic principles of the new criteria were clarified. A quality evaluation scoring table was established in the new criteria, including five parts: raw material selection, production process, quality control, efficacy evaluation, and brand building. The technical evaluation indexes involved have increased from 20% in the original criteria to 70% in the new criteria, and efficacy evaluation has been added in the new criteria. The subjective evaluation indicators account for a large proportion in the original criteria, which is prone to bias. The improved criteria overcome this shortcoming. It is expected that the new criteria as a basis can play a better role in the selection of high-quality products of CPMs, guide enterprises and institutions to participate actively in the evaluation and research of high-quality CPMs, and promote the high-quality development of CPMs.


Asunto(s)
Medicamentos Herbarios Chinos , Medicina Tradicional China , Medicamentos Herbarios Chinos/uso terapéutico , Medicamentos sin Prescripción , Clorobencenos , China
6.
Zhongguo Zhong Yao Za Zhi ; 47(17): 4814-4822, 2022 Sep.
Artículo en Chino | MEDLINE | ID: mdl-36164888

RESUMEN

The big brand of Chinese patent medicine, Fufang Danshen Prescription(FDP), effective in promoting blood circulation, resolving blood stasis, regulating qi, and relieving pain, is wide in clinical application and diverse in dosage forms and products, but its quality and price are uneven, which causes problems for doctors and patients. To clarify the key links and weakness of quality control leading to the quality difference of FDP products, the present study carried out a comprehensive evaluation of the whole production cycle of FDP based on the "high-quality Chinese patent medicine evaluation criteria" and analyzed the advantages and disadvantages of production and quality of different FDP products according to scores. The results showed that the scores of various products in the "raw materials selection" varied greatly. The highest score(S1) and the lowest score(S2) differed by more than 3 times, indicating that different manufacturers had inconsistent requirements for the selection of raw materials, leading to fundamental differences in the quality of raw materials. The scores in the "production process" varied slightly, with an average score of 66.8%. The manufacturer S8 obtained the highest score(84.0%), which indicated the emergence of intelligent manufacturing production. The scores(with the average score of 44.0%) in the "quality control" were lower than those of the previous two items, which was attributed to the fact that most FDP products only met the "qualified" benchmark required by the 2020 edition of Chinese Pharmacopoeia, and their consistency and high quality were both uncontrollable. The scores in the "post-marketing research" were the lowest(with an average score of 28.5%), and most manufacturers were scored 0, which reflected little attention paid. Only a few brand manufacturers were scored acceptably and they were willing to carry out relevant research on post-marketing evaluation. The evaluation results demonstrated the key links and weakness leading to the production and quality differences of FDP from different manufacturers. It is expected to improve the quality of FDP, promote the formation of the "high quality and good price" mechanism, and provide information for the centralized procurement of governments.


Asunto(s)
Medicamentos Herbarios Chinos , Medicina Tradicional China , China , Medicamentos Herbarios Chinos/análisis , Humanos , Medicamentos sin Prescripción , Prescripciones
7.
Int J Mol Sci ; 23(15)2022 Jul 29.
Artículo en Inglés | MEDLINE | ID: mdl-35955573

RESUMEN

The B-box proteins (BBXs) are a family of zinc-finger transcription factors with one/two B-Box domain(s) and play important roles in plant growth and development as well as stress responses. Wolfberry (Lycium barbarum L.) is an important traditional medicinal and food supplement in China, and its genome has recently been released. However, comprehensive studies of BBX genes in Lycium species are lacking. In this study, 28 LbaBBX genes were identified and classified into five clades by a phylogeny analysis with BBX proteins from Arabidopsis thaliana and the LbaBBXs have similar protein motifs and gene structures. Promoter cis-regulatory element prediction revealed that LbaBBXs might be highly responsive to light, phytohormone, and stress conditions. A synteny analysis indicated that 23, 20, 8, and 5 LbaBBX genes were orthologous to Solanum lycopersicum, Solanum melongena, Capsicum annuum, and Arabidopsis thaliana, respectively. The gene pairs encoding LbaBBX proteins evolved under strong purifying selection. In addition, the carotenoid content and expression patterns of selected LbaBBX genes were analyzed. LbaBBX2 and LbaBBX4 might play key roles in the regulation of zeaxanthin and antheraxanthin biosynthesis. Overall, this study improves our understanding of LbaBBX gene family characteristics and identifies genes involved in the regulation of carotenoid biosynthesis in wolfberry.


Asunto(s)
Arabidopsis , Lycium , Arabidopsis/genética , Arabidopsis/metabolismo , Carotenoides , Regulación de la Expresión Génica de las Plantas , Lycium/genética , Lycium/metabolismo , Filogenia , Proteínas de Plantas/metabolismo
8.
J Pharm Biomed Anal ; 219: 114951, 2022 Sep 20.
Artículo en Inglés | MEDLINE | ID: mdl-35908413

RESUMEN

The compositions of traditional Chinese medicines are extremely complex,as a result, exploring consistent quality is demanded and challenging. Quality consistency of products obtained from the same manufacturer has received little attention. The strategy of quality consistency evaluation (QCE) has been proposed as a novel method for quality control of Traditional Chinese Medicine Patent Prescription (TCMPP). This study aimed to establish a comprehensive QCE strategy for Compound Danshen Tablet (CDT). High Performance Liquid Chromatography-Diode Array Detector and Gas Chromatography-Mass Spectrometry were separately applied to determinate the content of seven and two index components, which representing the quality actuality of different raw medicines. The dissolution test was designed to obtain the dissolution ratios of CDT samples. QCE can provide the intra-batch content consistency difference (PA), inter-batch content consistency difference (PB), and dissolution ratio consistency difference (PR) values. The consistency of CDT samples from 15 different manufacturers (75 batches) was evaluated by principal component analysis (PCA), which showed that the total content (nine index components) of the 75 batches of samples obtained from 15 manufacturers ranged from 22.11 to 38.45 mg·tablet-1. The dissolution ratios ranged from 74.8% to 116.4%. The PA values of 15 manufacturers ranged from 2.4% to 12.2%, and the PB (11.1-45.1%) values were higher than the PA values. The PR values reflecting the various dissolution ratios in vitro ranged from 8.1% to 57.5%. The three consistency factors were ranked by PCA, and products of the 15 manufacturers were classified into three categories. The PA, PB, and PR values provided a comprehensive and effective approach for monitoring the quality consistency of CDT and can serve as an example of QCE for other TCMPP.


Asunto(s)
Medicamentos Herbarios Chinos , Salvia miltiorrhiza , Cromatografía Líquida de Alta Presión/métodos , Medicamentos Herbarios Chinos/química , Medicina Tradicional China , Control de Calidad , Salvia miltiorrhiza/química , Comprimidos
9.
Eur J Med Chem ; 228: 114031, 2022 Jan 15.
Artículo en Inglés | MEDLINE | ID: mdl-34875520

RESUMEN

Alzheimer's disease (AD) possesses a complex pathogenetic mechanism. Nowadays, multitarget agents are considered to have potential in effectively treating AD via triggering molecules in functionally complementary pathways at the same time. Here, based on the screening (∼1400 compounds) against neuroinflammation, an imidazolylacetophenone oxime ether (IOE) was discovered as a novel hit. In order to obtain SARs, a series of imidazolylacetophenone oxime derivatives were constructed, and their C=N bonds were confirmed as the Z configuration by single crystals. These derivatives exhibited potential multifunctional neuroprotective effects including anti-neuroinflammatory, antioxidative damage, metal-chelating, inhibition of acetylcholinesterase (AChE) properties. Among these derivatives, compound 12i displayed the most potent inhibitory activity against nitric oxide (NO) production with EC50 value of 0.57 µM 12i can dose-dependently suppress the expression of iNOS and COX-2 but not change the expression of HO-1 protein. Moreover, 12i exhibited evidently neuroprotective effects on H2O2-induced PC12 cells damage and ferroptosis without cytotoxicity at 10 µM, as well as selectively metal chelating properties via chelating Cu2+. In addition, 12i showed a mixed-type inhibitory effect on AChE in vitro. The structure-activity relationships (SARs) analysis indicated that dioxolane groups on benzene ring and rigid oxime ester can improve the activity. Parallel artificial membrane permeation assay (PAMPA) also verified that 12i can overcome the blood-brain barrier (BBB). Overall, this is the first report on imidazolylacetophenone oxime-based multifunctional neuroprotective effects, suggesting that this type of compounds might be novel multifunctional agents against AD.


Asunto(s)
Acetofenonas/farmacología , Descubrimiento de Drogas , Inhibidores Enzimáticos/farmacología , Imidazoles/farmacología , Fármacos Neuroprotectores/farmacología , Oximas/farmacología , Acetofenonas/síntesis química , Acetofenonas/química , Acetilcolinesterasa/metabolismo , Animales , Compuestos de Bifenilo/antagonistas & inhibidores , Línea Celular , Ciclooxigenasa 2/metabolismo , Relación Dosis-Respuesta a Droga , Electrophorus , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/química , Humanos , Imidazoles/síntesis química , Imidazoles/química , Lipopolisacáridos/antagonistas & inhibidores , Lipopolisacáridos/farmacología , Ratones , Estructura Molecular , Fármacos Neuroprotectores/síntesis química , Fármacos Neuroprotectores/química , Óxido Nítrico/antagonistas & inhibidores , Óxido Nítrico/biosíntesis , Oximas/síntesis química , Oximas/química , Picratos/antagonistas & inhibidores , Ratas , Relación Estructura-Actividad
10.
Bioorg Chem ; 116: 105389, 2021 11.
Artículo en Inglés | MEDLINE | ID: mdl-34601295

RESUMEN

Dried flowers of Inula britannica commercially serve as pharmaceutical/nutraceutical herbs in the manufacture of medicinal products and functional tea that has been reported to possess extensive biological property. However, the neuroprotective constituents in I. britannica flowers are not known. In the current study, phytochemicals of sesquiterpenoid-enriched I. britannica flowers extract and their potential multifunctional neuroprotective effects were investigated. Nineteen structurally diverse sesquiterpenoids, including two new sesquiterpenoid dimers, namely, inubritanolides A and B (1, 2), and four new sesquiterpenoid monomers (3-6), namely, 1-O-acetyl-6-O-chloracetylbritannilactone (3), 6-methoxybritannilactone (4), 1-hydroxy-10ß-methoxy-4αH-1,10-secoeudesma-5(6),11(13)-dien-12,8ß-olide (5) and 1-hydroxy-4αH-1,10-secoeudesma-5(6),10(14),11(13)-trien-12,8ß-olide (6), as well as 13 known congeners (7-19) were isolated from this source. The structures of compounds 1-6 were elucidated by 1D- and 2D- NMR and HR-ESI-MS data, and their absolute configurations were discerned by electronic circular dichroism (ECD) data analysis and single crystal X-ray diffraction. Interestingly, inubritannolide A (1) is a new type [4 + 2] Diels-Alder dimer featuring a hepta-membered cycloether skeleton. Most of the compounds showed potential multifunctional neuroprotective effects, including antioxidative, anti-neuroinflammatory, and microglial polarization properties. Specifically, 1 and 6 displayed slight strong neuroprotective potency against different types of neuronal cells mediated by various inducers including H2O2, 6-hydroxydopamine (6-OHDA), and lipopolysaccharide (LPS). Overall, this is the first report on multifunctional neuroprotective effects of sesquiterpenoid-enriched I. britannica flowers extract, which supports its potential pharmaceutical/nutraceutical application in neurodegenerative diseases.


Asunto(s)
Antioxidantes/farmacología , Flores/química , Inula/química , Fármacos Neuroprotectores/farmacología , Extractos Vegetales/farmacología , Sesquiterpenos/farmacología , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Relación Dosis-Respuesta a Droga , Humanos , Inflamación/tratamiento farmacológico , Estructura Molecular , Neuronas/efectos de los fármacos , Fármacos Neuroprotectores/química , Fármacos Neuroprotectores/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Sesquiterpenos/química , Sesquiterpenos/aislamiento & purificación , Relación Estructura-Actividad
11.
Phytother Res ; 35(1): 346-360, 2021 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-32749748

RESUMEN

Aurantio-obtusin (AUR) is the main bioactive compound among the anthraquinones, from Cassia seed extract. This study was conducted to identify whether AUR could improve obesity and insulin resistance, induced by a high-fat diet in obese mice. Mice were fed a high-fat diet for 6 weeks and were then assigned to the high-fat diet (HFD) control group, the AUR 5 mg/kg group, or the AUR 10 mg/kg group. AUR improves glucose by activating the expression of PI3K, Akt and GLUT4, GLUT2. AUR altered the expression levels of several lipid metabolism-related and adipokine genes. AUR decreased the mRNA expression of PPAR-γ, FAS and increased the mRNA expression of PPAR-α in liver. AUR lowered SREBP-1c, FAS, SCD-1, inflammatory cytokines, and increased the expression of PPAR-γ, PPAR-α, CPT-1, and adiponectin in white adipose tissue (WAT). AUR docking with the insulin receptor showed that the residues of the insulin receptor, ectodomain, were the same as those around the emodin. The effect of AUR may be elicited by regulating the activity of the insulin signaling pathway, expression of lipid metabolism-related genes, and expression of inflammatory cytokine markers to improve adiposity, insulin resistance, and dyslipidemia.


Asunto(s)
Antraquinonas/uso terapéutico , Resistencia a la Insulina , Obesidad/tratamiento farmacológico , Adiponectina/metabolismo , Tejido Adiposo Blanco/metabolismo , Animales , Cassia/química , Dieta Alta en Grasa , Metabolismo de los Lípidos/efectos de los fármacos , Hígado/efectos de los fármacos , Masculino , Ratones , Ratones Endogámicos C57BL , Ratones Obesos , Obesidad/metabolismo , PPAR gamma/metabolismo , Receptor de Insulina/metabolismo , Semillas/química , Transducción de Señal/efectos de los fármacos , Proteína 1 de Unión a los Elementos Reguladores de Esteroles/metabolismo
12.
Zhongguo Zhong Yao Za Zhi ; 44(17): 3732-3737, 2019 Sep.
Artículo en Chino | MEDLINE | ID: mdl-31602946

RESUMEN

Grade evaluation method of quality constant is a kind of grading method for Chinese medicinal materials and decoction pieces,combining the external morphological index and internal content index. This method was used in this paper for grade evaluation of Gardeniae Fructus. By measuring the morphological and content indexes of 14 batches of Gardeniae Fructus,a method for calculating the quality constant of fruits was established,and the grade evaluation criteria were formed. At the same time,the NO inhibition effect of different grades of Gardeniae Fructus samples on RAW264. 7 cells induced by LPS was determined to investigate the relationship between the quality grade and pharmacodynamics of decoction pieces. The results showed that the quality constants of Gardeniae Fructus decoction piece samples ranged from 1. 46 to 4. 42. If the percentage quality constant ≥80% was classified into first-class,50%-80%as second-class and the rest as third-class,the quality constant was ≥3. 54 for first-class,2. 21-3. 54 for second-class and <2. 21 for third-class Gardeniae Fructus decoction pieces. The pharmacodynamic results showed that the pharmacodynamic intensity was positively correlated with the grade,which also proved the rationality of the grade evaluation method of quality constant.


Asunto(s)
Medicamentos Herbarios Chinos/normas , Frutas/química , Gardenia/química , Animales , Medicamentos Herbarios Chinos/análisis , Ratones , Control de Calidad , Células RAW 264.7
13.
Food Chem ; 279: 339-346, 2019 May 01.
Artículo en Inglés | MEDLINE | ID: mdl-30611499

RESUMEN

A rapid method for the determination of fatty acid (FA) composition in camellia oils was developed based on the 1H NMR technique combined with partial least squares (PLS) method. Outliers detection, LVs optimization and data pre-processing selection were explored during the model building process. The results showed the optimal models for predicting the content of C18:1, C18:2, C18:3, saturated, unsaturated, monounsaturated and polyunsaturated FA were achieved by Pareto scaling (Par) pretreatment, with correlation coefficient (R2) above 0.99, the root mean square error of estimation and prediction (RMSEE, RMSEP) lower than 0.954 and 0.947, respectively. Mean-centering (Ctr) was more suitable for the model of C16:0 and C18:0 with the best performance indicators (R2 ≥ 0.945, RMSEE ≤ 0.377, RMSEP ≤ 0.212). This study indicated that 1H NMR has the potential to be applied as a rapid and routine method for the analysis of FA composition in camellia oils.


Asunto(s)
Camellia/química , Ácidos Grasos/análisis , Aceites de Plantas/química , Espectroscopía de Protones por Resonancia Magnética/métodos , Análisis de Varianza , Ácidos Grasos Insaturados/análisis , Análisis de los Mínimos Cuadrados , Aceites de Plantas/análisis , Espectroscopía de Protones por Resonancia Magnética/estadística & datos numéricos , Procesamiento de Señales Asistido por Computador
14.
Biomed Pharmacother ; 111: 188-197, 2019 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-30583226

RESUMEN

BACKGROUND: Both Chuanxiong (Ligusticum chuanxiong Hort) and Tianma (Gastrodia elata Blume) have the effects of vasorelaxation and antihypertension. However, the effects of Tianshu Capsule (TSC, composed of Chuanxiong and Tianma in the mass ratio of 4:1) on antihypertensive activity have not been explored. This study aimed to investigate the eff ;ects of TSC on vascular tension and blood pressure in rats and to explore the underlying mechanisms. METHODS: The vasorelaxant effect of TSC was explored on thoracic aortic rings (both intact endothelium and denuded) preincubated with phenylephrine (Phe) or potassium chloride (KCL). The mechanism was investigated in the presence of antagonists or blockers on aorta isolated from normotensive rats. The in vivo antihypertensive effect was assessed using a tail-cuff method on spontaneously hypertensive rats (SHRs). RESULTS: TSC (0.125-4 mg/mL) produced a concentration-dependent vasorelaxation on aortic rings preincubated with Phe (1 µM) or KCL (60 mM). Removal of aorta endothelium markedly attenuated the TSC activity. Pretreatment of aortic rings with ß-adrenoceptor blocker propranolol (1 µM), muscarinic receptor antagonist atropine (1 µM), cyclooxygenase inhibitor indomethacin (IDO, 1 µM), adenylyl cyclase inhibitor 9-(tetrahydro-2-furanyl)-9H-purine-6-amine (SQ22536, 100 µM), K+ channel blockers 4-aminopyridine(4-AP, 1 mM) or barium chloride(BaCl2, 1 mM) followed by addition of Phe (1 µM) prior to TSC did not influence the TSC-induced relaxation. In contrast, the vasorelaxant effects of TSC were markedly inhibited by the NO synthase inhibitor L-NG-nitroarginine methyl ester (L-NAME, 10 µM), guanylyl cyclase inhibitor 1H- [1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one (ODQ, 10 µM), K+ channel blockers, glibenclamide (100 µM) and clotrimazole (5 mM). Moreover, TSC (2 mg/mL, 4 mg/mL) inhibited CaCl2-induced contractions and caused a concentration-dependent rightward shift of the response curves. Additionally, TSC (2 mg/mL, 4 mg/mL) depressed the constriction caused by Phe (1 µM) in the absence of extracellular Ca2+. Furthermore, TSC (2.15 g/kg) lowered the systolic blood pressure (SBP), with no alteration in heart rate (HR) in SHRs. CONCLUSIONS: These findings demonstrated that TSC induced vasorelaxant effects via both endothelium-dependent and endothelium-independent pathways. The NO/sGC/cGMP pathway, ATP-sensitive K+ channels, Ca2+-activated K+ channels, inhibition of extracellular Ca2+ influx and intracellular Ca2+ release were probably involved in this relaxation. The vasorelaxant effects of TSC may make the greatest contribution to the reduction in high blood pressure.


Asunto(s)
Antihipertensivos/farmacología , Aorta Torácica/efectos de los fármacos , Medicamentos Herbarios Chinos/farmacología , Vasodilatación/efectos de los fármacos , Vasodilatadores/farmacología , Animales , Antihipertensivos/síntesis química , Aorta Torácica/fisiología , Relación Dosis-Respuesta a Droga , Medicamentos Herbarios Chinos/síntesis química , Endotelio Vascular/efectos de los fármacos , Endotelio Vascular/fisiología , Masculino , Técnicas de Cultivo de Órganos , Ratas , Ratas Endogámicas WKY , Ratas Sprague-Dawley , Resultado del Tratamiento , Vasodilatación/fisiología , Vasodilatadores/síntesis química
15.
Biomed Pharmacother ; 105: 187-194, 2018 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-29857298

RESUMEN

INTRODUCTION: Dangguishaoyao-San (DSS) is composed of six traditional Chinese medicines, including Angelica sinensis, Paeoniae radix, Rhizoma Ligusticum, Poria cocos, Rhizoma Atractylodis Macrocephalae, and Rhizoma Alismatis. DSS has been reported to be effective in alleviating the symptoms of Alzheimer's disease (AD). The aim of this study was to investigate the mechanism of action of DSS in vitro using lipopolysaccharide (LPS)-stimulated BV-2 microglia cells. MATERIALS AND METHODS: BV-2 cells were pretreated with 0.58-1.16 mg/mL of DSS for 2 h and then treated with 1 µg/mL LPS for 24 h. Cell viability was determined by an 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The protein expression levels were measured by Western blots. Inflammatory factors were detected by enzyme-linked immunosorbent assays (ELISAs). The mRNA levels of inflammatory factors were analyzed by quantitative real-time PCR (qRT-PCR). RESULTS: DSS treatment at concentrations of 0.58-1.16 mg/mL resulted in no significant cytotoxicity. DSS attenuated the release of pro-inflammatory factors, such as interleukin-1ß (IL-1ß), iNOS and tumor necrosis factor-α (TNF-α) in LPS-induced BV-2 cells. DSS attenuated the mRNA expression of pro-inflammatory cytokines, TLR2, and TLR4 and decreased TLR4 and TLR protein levels as well as the phosphorylation of IκB in LPS-induced BV-2 cells. DSS also down-regulated the nuclear translocation of p65. CONCLUSION: This study demonstrated that DSS has a protective effect on neuroinflammation in LPS-induced BV-2 microglia cells through the TLRs/NF-κB signaling pathway.


Asunto(s)
Encéfalo/patología , Medicamentos Herbarios Chinos/uso terapéutico , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , FN-kappa B/metabolismo , Transducción de Señal , Receptores Toll-Like/metabolismo , Animales , Muerte Celular/efectos de los fármacos , Línea Celular , Núcleo Celular/efectos de los fármacos , Núcleo Celular/metabolismo , Medicamentos Herbarios Chinos/farmacología , Inflamación/patología , Mediadores de Inflamación/metabolismo , Interleucina-1beta/metabolismo , Lipopolisacáridos , Ratones , Óxido Nítrico Sintasa de Tipo II/metabolismo , Transporte de Proteínas/efectos de los fármacos , ARN Mensajero/genética , ARN Mensajero/metabolismo , Factor de Transcripción ReIA/metabolismo , Factor de Necrosis Tumoral alfa/genética , Factor de Necrosis Tumoral alfa/metabolismo
16.
Gen Comp Endocrinol ; 259: 45-53, 2018 04 01.
Artículo en Inglés | MEDLINE | ID: mdl-29154946

RESUMEN

The Dio2/3 gene is related to the photoperiodic response in mammals and plays an important role in the development of gonadal organs and seasonal breeding. Our previous studies have reported synchronous variations in the gonadal mass and photoperiodical transition around the summer solstice in a wild Brandt's vole population, a species with striking seasonal breeding. To investigate the role of the Dio2/3 gene in the control of seasonal breeding in this species, we cloned and characterized its expression levels by high-throughput Real-Time PCR during the period around the summer solstice. We selected a domesticated strain to ensure similar development of samples. The synchronous variation pattern between the Dio2/3 expression levels and gonadal mass around the summer solstice supports the prediction that the Dio2/3 gene plays an important role in the seasonal transition in this species. We suggest that the observed photoperiod response may be triggered by differences in the day length rather than the absolute daylength in this species. However, the similar Dio2/3 gene expression patterns but inconsistent gonadal mass patterns between the domesticated strain and the wild strain in the samples collected on Sep 8th, an absolute nonbreeding stage in the wild, lead us to speculate that the core function of the Dio2/3 gene should be restricted in response to the photoperiod rather than factors directly regulating gonadal development, and this laboratory strain could be used as an animal model to test the mechanism of environmental adaptation.


Asunto(s)
Arvicolinae/genética , Arvicolinae/fisiología , Domesticación , Regulación de la Expresión Génica , Hipotálamo/metabolismo , Yoduro Peroxidasa/genética , Fotoperiodo , Secuencia de Aminoácidos , Animales , Ritmo Circadiano , Clonación Molecular , Perfilación de la Expresión Génica , Gónadas/anatomía & histología , Gónadas/metabolismo , Yoduro Peroxidasa/química , Yoduro Peroxidasa/metabolismo , Masculino , Tamaño de los Órganos
17.
Food Funct ; 8(1): 341-351, 2017 Jan 25.
Artículo en Inglés | MEDLINE | ID: mdl-28045183

RESUMEN

The present work aimed at the recovery and characterization of dietary fiber and polyphenolic compounds extracted from red grape pomace, a by-product generated after grape fruit processing. High contents of total DF were found in the dietary fiber extracts (57.24%), whereas insoluble fiber was the major fraction (51.70%). And it showed good functional properties, including swelling capacity (4.01-8.32 mL g-1), water holding capacity (1.91-4.23 g g-1) and oil holding capacity (0.59-0.65 g g-1). After separation from the dietary fiber, phenolic extracts with high concentrations of total phenolic compounds and total flavonoids, showed high antioxidant activities, while the separated dietary fiber showed little antioxidant activities. This indicated that the phenolic composition is essential for the antioxidant activity of "antioxidant dietary fiber (ADF)". The identification of individual polyphenols was performed applying the HPLC-ESI-MS/MS technique and 31 compounds have been identified belonging to 4 groups, including anthocyanins, flavonols, flavan-3-ols and phenolic acids. Based on this study, we believe grape juice pomace could potentially be exploited as an inexpensive source of natural dietary fiber and phenolics and possibly used as a functional food ingredient.


Asunto(s)
Fibras de la Dieta/análisis , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Polifenoles/química , Polifenoles/aislamiento & purificación , Vitis/química , Residuos/análisis , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Flavonoides/química , Flavonoides/aislamiento & purificación , Fenoles/química , Fenoles/aislamiento & purificación
18.
Fitoterapia ; 116: 17-23, 2017 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-27847306

RESUMEN

Uncariols A (1) and B (2), two new phenylpropanoid-substituted flavan-3-ols, and (±)-uncariols C (3a/3b) and D (4a/4b), two pairs of new phenylpropanoid-substituted flavonol enantiomers, together with nine known compounds (5-13), were isolated from the leaves of Uncaria rhynchophylla. The structures of 1-4 were established primarily by NMR and HRESIMS experiments. The absolute configurations of the new ones were deduced via the circular dichroism (CD) and quantum chemical calculations of the electronic circular dichroic (ECD) spectra. In addition, all of the isolated compounds showed potent antioxidant activity in the DPPH radical scavenging test.


Asunto(s)
Flavonoides/química , Flavonoles/química , Depuradores de Radicales Libres/química , Uncaria/química , Flavonoides/aislamiento & purificación , Flavonoles/aislamiento & purificación , Depuradores de Radicales Libres/aislamiento & purificación , Estructura Molecular , Hojas de la Planta/química
19.
Zhong Yao Cai ; 38(8): 1622-5, 2015 Aug.
Artículo en Chino | MEDLINE | ID: mdl-26983231

RESUMEN

OBJECTIVE: To develop an HPLC method for simultaneous determination of notoginsenoside R1 and ginsenosides Rg1 Re, Rh1, Rb1, Rd, Rk3, Rh4, 20(S)-Rg3 and 20(R)-Rg3 in raw and steamed Panax notoginseng root and rhizome. METHODS: Vision HT C18 column (250 mm x 4.6 mm, 5 µm) was used with the mobile phase consisted of acetonitrile-H2O in a gradient elution mode at the flow rate of 1.2 ml/min. The column temperature was maintained at 20 °C and the detection wavelength was set at 203 nm. RESULTS: The methodological study showed a good linear relationship ( r > 0. 9995 ) . The average recoveries of the ten saponins were 95.93%-102.54%. CONCLUSION: The method is accurate and reproducible, which can be used for simultaneous determination of saponins in raw and steamed Panax notoginseng root and rhizome, and can provide reference for the relationship between material basis and pharmacological effects.


Asunto(s)
Panax notoginseng/química , Raíces de Plantas/química , Rizoma/química , Saponinas/análisis , Cromatografía Líquida de Alta Presión , Ginsenósidos/análisis , Plantas Medicinales/química , Reproducibilidad de los Resultados , Vapor
20.
Asian Pac J Cancer Prev ; 15(10): 4129-33, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-24935358

RESUMEN

BACKGROUND: The objective was to study the effect of Scutellaria baicalensis Georgi ethanol extracts (SBGE) on immune and anti-oxidant function in U14 tumor-bearing mice. MATERIALS AND METHODS: U14 tumor-bearing mice were randomly divided into eight groups: a control group, a cyclophosphamide (CTX) group, three dose groups of SBGEI (high, medium, low), and three dose groups of SBGEII (high, medium, low). After two weeks, the thymus and spleen weight indices of mice bearing U14 cervical cancer were calculated. Enzyme linked immunosorbent assays (ELISA) was used to determine the levels of serum IL-2, TNF-α, IL-8, and PCNA. MDA activity and SOD activity in plasma were measured with detection kits. RESULTS: In the SBGE groups, thymus weight and spleen weight indices of U14 tumor-bearing mice were significantly higher than in the control group or CTX group (p<0.05). Compared to control group, the levels of serum IL-2 and TNF-α in U14 tumor-bearing mice increased significantly, whereas the contents of serum IL-8 and PCNA decreased (p<0.05). The activity of SOD increased with the growing dose of SBGE, while the activity of MDA decreased significantly in the higher- dose groups of SBGE. CONCLUSIONS: These findings suggested that SBGE, especially at high dose, 1000 mg/kg, showed significant immune and anti-oxidant effects in U14 tumor-bearing mice, which might be the mechanisms of SBGE inhibition of tumor growth.


Asunto(s)
Antioxidantes/farmacología , Extractos Vegetales/farmacología , Scutellaria baicalensis/metabolismo , Neoplasias del Cuello Uterino/tratamiento farmacológico , Animales , Línea Celular Tumoral , Ciclofosfamida/farmacología , Medicamentos Herbarios Chinos/farmacología , Femenino , Interleucina-2/sangre , Interleucina-8/sangre , Medicina Tradicional China , Ratones , Fitoterapia , Antígeno Nuclear de Célula en Proliferación/sangre , Bazo/fisiología , Superóxido Dismutasa/sangre , Timo/fisiología , Factor de Necrosis Tumoral alfa/sangre , Neoplasias del Cuello Uterino/inmunología , Neoplasias del Cuello Uterino/patología
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