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Chinese patent medicine preparations containing Epimedii Folium and Psoraleae Fructus have been associated with the occurrence of idiosyncratic drug-induced liver injury(IDILI). However, the specific toxic biomarkers and mechanisms underlying these effects remain unclear. This study aimed to comprehensively assess the impact of bavachin and epimedin B, two principal consti-tuents found in Psoraleae Fructus and Epimedii Folium, on an IDILI model induced by tumor necrosis factor-α(TNF-α) treatment, both in vitro and in vivo. To evaluate the extent of liver injury, various parameters were assessed. Lactate dehydrogenase(LDH) release in the cell culture supernatant, as well as the levels of alanine aminotransferase(ALT) and aspartate transaminase(AST) in mouse plasma were measured. Additionally, histological analysis employing hematoxylin-eosin staining was performed to observe liver tissue changes indicative of the severity of liver injury. Furthermore, a pseudo-targeted metabolomics approach was employed, followed by multivariate analysis, to identify differential metabolites. These identified metabolites were subsequently subjected to Kyoto Encyclopedia of Genes and Genomes(KEGG) pathway enrichment analysis. The results showed that at the cellular level, after 2 hours of TNF-α stimulation, bavachin significantly increased the release of LDH in HepG2 cells compared to the normal group and the group treated alone; after the combination of bavachin and epimedin B, the release of LDH further significantly increased on the original basis. Similarly, although the individual or combination treatments of bavachin and epimedin B did not induce liver injury in normal mice, the combination of both drugs induced marked liver injury in TNF-α treated mice, leading to a significant elevation in plasma AST and ALT levels and substantial infiltration of inflammatory immune cells in the liver tissue. Pseudo-targeted metabolomics analysis identified seven common differential metabolites. Among these, D-glucosamine-6-phosphate, N1-methyl-2-pyridone-5-carboxamide, 17beta-nitro-5a-androstane, irisolidone-7-O-glucuronide, and N-(1-deoxy-1-fructosyl) valine emerged as potential biomarkers, with an area under the curve(AUC) exceeding 0.9. Furthermore, our results suggest that the metabolism of nicotinic acid and nicotinamide, as well as the linoleic acid metabolic pathway, may play pivotal roles in bavachin and epimedin B-induced IDILI. In conclusion, within an immune-stressed environment mediated by TNF-α, bavachin and epimedin B appear to induce IDILI through disruptions in metabolic processes.
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Doença Hepática Induzida por Substâncias e Drogas , Flavonoides , Fator de Necrose Tumoral alfa , Camundongos , Animais , Fator de Necrose Tumoral alfa/metabolismo , Fígado , Biomarcadores/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/etiologia , Doença Hepática Induzida por Substâncias e Drogas/patologiaRESUMO
Background: Retroauricular injection is a local steroid hormone administration method commonly used to treat deafness or tinnitus. The acute stage of Bell's Palsy is an acute disease that requires steroid therapy. Retroauricular injection may replace oral administration of steroid hormones in the treatment of this disease as well as reduce the occurrence of adverse reactions. Methods: This study included patients with Bell's Palsy within seven days of onset. A total of 120 patients were enrolled as the study subjects and randomly divided into two groups: the experimental group and the control group. Both groups received routine acupuncture treatment and took a traditional Chinese medicine decoction corresponding with the syndrome type. Methylprednisolone sodium succinate was injected into the bone surface of retroauricula in the experimental group, and prednisone acetate was orally administered in the control group. The main outcome indicators were the House-Brackmann (HB) grade, the facial disability index (FDI), and time of postauricular pain after one month of treatment. Results: There were no significant differences in the HB grade (2.00 ± 1.06 vs. 1.88 ± 1.06, P=), FDIP (97.25 ± 6.00 vs. 97.17 ± 7.39, P=), and FDIS (0.60 ± 3.02 vs. 1.33 ± 4.27, P=) at 30 days after treatment between the two groups (P > 0.05). Postauricular pain disappeared earlier in the experimental group (3.66 ± 1.67 days) than in the control group (6.31 ± 2.34); the difference was statistically significant (P ≤ 0.001). The adverse reaction rate was lower in the experimental group (15.00%) than in the control group (21.66%). Interpretation: Although the dose of steroid hormone injected into the bone surface of retroauricula in the treatment of Bell's Palsy is lower than the administered dose of oral hormones, it has the same curative effect; however, it has a better effect regarding to the duration of postauricular pain and adverse reactions.
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ETHNOPHARMACOLOGICAL RELEVANCE: Thesium chinense Turcz. has been used to treat mastitis, pulmonitis, tonsillitis, iaryngopharyngitis and upper respiratory tract infections in the indigenous medicine of China for a long history. Presently, several pharmaceutics prepared by this medical herb have been clinically used for the therapy of infectious diseases. AIM OF THE REVIEW: This review aims to comprehensively summarize the current researches on the ethnomedical, phytochemical and pharmacological aspects of T. chinense, and discuss their possible opportunities for the future research. MATERIALS AND METHODS: Extensive database searches, including Web of Science, SciFinder, Google Scholar and China Knowledge Resource Integrated, were performed using keywords such as 'Thesium chinense', 'Bai Rui Cao', and their chemical constituents. In addition, local classic herbal literature on ethnopharmacology and relevant textbooks were consulted to provide a comprehensive survey of this ethnomedicine. RESULTS: Thirty four chemical constituents, including flavonoids, alkaloids, and terpenoids, have been identified from T. chinense. Of which, flavonoids are the predominant and characteristic constituents. The crude extracts, the purified constituents, and commercial available pharmaceutics have displayed diverse in vitro and in vivo pharmacological functions (e.g. anti-inflammation, antimicrobial activity, analgesic effect, hepaprotection), and are particularly useful as a potential therapeutic agent against inflammation-related diseases. CONCLUSIONS: T. chinense is an important ethnomedical medicine and possesses a satisfying effect for treating inflammation, microbial infection, and upper respiratory diseases. It has received plenty of researches on its phytochemical and pharmacological aspects since 1970s. These findings definitely establish the link between chemical composition and pharmacological application, and support the ethnomedical use of T. chinense in the indigenous medicine of China. However, chemical composition of this plant and the molecular mechanisms of purified constituents have not been comprehensively investigated, and thus the trace constituents and the therapeutic targets of bioactive constituents deserve a further exploration. Collectively, the researchers should pay more attention to a better understanding and application of this ethnomedical plant.
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Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Santalaceae/química , Animais , Estudos Clínicos como Assunto , Medicamentos de Ervas Chinesas/uso terapêutico , Medicamentos de Ervas Chinesas/toxicidade , Humanos , Medicina Tradicional Chinesa , Compostos Fitoquímicos/uso terapêutico , Compostos Fitoquímicos/toxicidadeRESUMO
Medicinal plants with complex matrices are endowed with a wide scope of biological activities. The separation, quantification, characterization and purification of bioactive components from herbal medicine extracts have always challenged analysts. Fortunately, the advancement of various emerging techniques has provided potent support for improving the method selectivity, sensitivity and run speeds in medicinal plant analyses. In recent years, the advent of new-generation supercritical fluid chromatography (SFC) instruments and a wide diversity of column chemistries, coupled with the intrinsic technical features of SFC, have made it an alternative and prominent analytical platform in the medicinal plant research area. This work aims to give a comprehensive overview of the fundamentals, technical advancement and investigating parameters of SFC in combination with three prevalent detectors. Moreover, the latest research progress of SFC applications in medicinal plant analyses is illuminated, with focus on herbal medicine-related SFC papers on the analytical and preparative scale that were published during the period of 2012 to December 2018. The most relevant applications were classified based on the constituents to be analysed. As for the respective research cases, analytical protocols and data processing strategies were provided, along with the indicated restrictions or superiority of the method; thus, the current status of SFC in medicinal plant analysis was presented.
Assuntos
Cromatografia com Fluido Supercrítico/métodos , Compostos Fitoquímicos/análise , Plantas Medicinais/química , Cromatografia com Fluido Supercrítico/instrumentaçãoRESUMO
BACKGROUND: Oxidative stress contributes to the pathogenesis of many human diseases. Cinnamon is a worldwide used spice, dietary supplement and traditional medicine, and is used for the therapy of oxidative stress related diseases. A well-established concept is that the functions of cinnamon preventing oxidative stress-induced diseases are attributed to the occurrence of cinnamaldehyde and its analogues. HYPOTHESIS: In our continuous searching of natural molecules with antioxidant capacity, we have found that cinnamaldehyde and its analogues in cinnamon are weak inhibitors of oxidative stress, and thus we speculate that there are novel and/or potent molecules inhibiting oxidative stress in cinnamon. STUDY DESIGN AND METHODS: A systemic phytochemical investigation of cinnamon using column chromatography was performed to identify the chemical constituents of cinnamon, and then their capacity of inhibiting oxidative stress and action of mechanism targeting Nrf2 pathway were investigated using diverse bioassay, including NAD(P)H: quinone reductase (QR) assay, immunoblot analysis, luciferase reporter gene assay, immunofluorescence and flow cytometry. RESULTS: Cinnamon improved the intracellular antioxidant capacity. A systemic phytochemical investigation of cinnamon gave the isolation of twenty-two chemical ingredients. The purified constituents were tested for their potential inhibitory effects against oxidative stress. Besides cinnamaldehyde analogues, a lignan pinoresinol (PRO) and a flavonol (-)-(2R,3R)-5,7-dimethoxy-3', 4'-methylenedioxy-flavan-3-ol (MFO) were firstly identified to be inhibitors of oxidative stress. Further study indicated that PRO and MFO activated Nrf2-mediated antioxidant response, and protected human lung epithelial cells against sodium arsenite [As(III)]-induced oxidative insults. CONCLUSION: The lignan PRO and the flavonoid MFO are two novel Nrf2 activators protecting tissues against oxidative insults, and these two constituents support the application of cinnamon as an agent against oxidative stress related diseases.
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Antioxidantes/farmacologia , Cinnamomum zeylanicum/química , Flavonoides/farmacologia , Lignanas/farmacologia , Acroleína/análogos & derivados , Animais , Arsenitos/toxicidade , Linhagem Celular , Avaliação Pré-Clínica de Medicamentos/métodos , Células Epiteliais/efeitos dos fármacos , Células Epiteliais/metabolismo , Flavonoides/química , Furanos/farmacologia , Humanos , Lignanas/química , Camundongos , NAD(P)H Desidrogenase (Quinona)/metabolismo , Fator 2 Relacionado a NF-E2/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Substâncias Protetoras/farmacologia , Compostos de Sódio/toxicidadeRESUMO
Oxidative stress plays a central role in the pathogenesis of many human diseases. The nuclear factor erythroid 2-related factor 2 (Nrf2) is a key transcription factor regulating the intracellular antioxidant response and is an emerging target for the prevention and therapy of oxidative stress-related diseases. Salviae Miltiorrhizae Radix et Rhizoma (SMRR) is a traditional Chinese medicine (TCM) and is commonly used for the therapy of cardiac cerebral diseases. Cumulative evidences indicated that the extract of SMRR and its constituents, represented by lipophilic diterpenoid quinones and hydrophilic phenolic acids, were capable of activating Nrf2 and inhibiting oxidative stress. These bioactive constituents demonstrated a therapeutic potential against human diseases, exemplified by cardiovascular diseases, neurodegenerative diseases, diabetes, nephropathy, and inflammation, based on the induction of Nrf2-mediated antioxidant response and the inhibition of oxidative stress. In the present review, we introduced the SMRR and Nrf2 signaling pathway, summarized the constituents with an Nrf2-inducing effect isolated from SMRR, and discussed the molecular mechanism and pharmacological functions of the SMRR extract and its constituents.
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Antioxidantes/metabolismo , Medicina Tradicional Chinesa/métodos , Fator 2 Relacionado a NF-E2/metabolismo , Humanos , Estresse Oxidativo/efeitos dos fármacos , Salvia miltiorrhiza , Transdução de Sinais/efeitos dos fármacosRESUMO
Oxidative stress and inflammation undoubtedly contribute to the pathogenesis of many human diseases. The nuclear transcription factor erythroid 2-related factor (Nrf2) and the nuclear factor κB (NF-κB) play central roles in regulation of oxidative stress and inflammation and thus are targets for developing agents against oxidative stress- and inflammation-related diseases. Our previous study indicated that the EtOH extract of Litsea garrettii protected human bronchial epithelial cells against oxidative insult via the activation of Nrf2. In the present study, a systemic phytochemical investigation of L. garrettii led to the isolation of twenty-one chemical ingredients, which were further evaluated for their inhibitions on oxidative stress and inflammation using NAD(P)H:quinone reductase (QR) assay and nitric oxide (NO) production assay. Of these ingredients, 3-methoxy-5-pentyl-phenol (MPP, 5) was identified as an Nrf2 activator and an NF-κB inhibitor. Further studies demonstrated the following: (i) MPP upregulated the protein levels of Nrf2, NAD(P)H:quinone oxidoreductase 1 (NQO1), and glutamate-cysteine ligase regulatory subunit (GCLM); enhanced the nuclear translocation and stabilization of Nrf2; and inhibited arsenic [As(III)]-induced oxidative insult in normal human lung epithelial Beas-2B cells. And (ii) MPP suppressed the nuclear translocation of NF-κB p65 subunit; inhibited the lipopolysaccharide- (LPS-) stimulated increases of NF-κB p65 subunit, COX-2, iNOS, TNF-α, and IL-1ß; and blocked the LPS-induced biodegrade of IκB-α in RAW 264.7 murine macrophages. Taken together, MPP displayed potential preventive effects against inflammation- and oxidative stress-related diseases.
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Anti-Inflamatórios/uso terapêutico , Brônquios/patologia , Células Epiteliais/efeitos dos fármacos , Inflamação/tratamento farmacológico , Estresse Oxidativo/efeitos dos fármacos , Fenóis/uso terapêutico , Extratos Vegetais/uso terapêutico , Animais , Anti-Inflamatórios/química , Células Epiteliais/fisiologia , Etanol/química , Regulação da Expressão Gênica , Humanos , Interleucina-1beta/metabolismo , Litsea/imunologia , Camundongos , Fator 2 Relacionado a NF-E2/metabolismo , NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Fenóis/química , Extratos Vegetais/química , Quinona Redutases/metabolismo , Células RAW 264.7 , Fator de Necrose Tumoral alfa/metabolismoRESUMO
With the growth of number of Chinese patent medicines and clinical use, the rational use of Chinese medicine is becoming more and more serious. Due to the complexity of Chinese medicine theory and the uncertainty of clinical application, the prescription review of Chinese patent medicine always relied on experience in their respective, leading to the uncontrolled of clinical rational use. According to the traditional Chinese medicine (TCM) theory and characteristics of the unique clinical therapeutics, based on the practice experience and expertise comments, our paper formed the expert consensus on the prescription review of Chinese traditional patent medicine for promoting the rational use of drugs in Beijing. The objective, methods and key points of prescription review of Chinese patent medicine, were included in this expert consensus, in order to regulate the behavior of prescription and promote rational drug use.
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Medicamentos de Ervas Chinesas , Medicina Tradicional Chinesa , Medicamentos sem Prescrição , Pequim , Consenso , PrescriçõesRESUMO
Human lung tissue, directly exposed to the environmental oxidants and toxicants, is apt to be harmed to bring about acute or chronic oxidative insults. The nuclear factor erythroid 2-related factor 2 (Nrf2) represents a central cellular defense mechanism, and is a target for developing agents against oxidative insult-induced human lung diseases. Our previous study found that the EtOH extract of Cinnamomum chartophyllum protected human bronchial epithelial cells against oxidative insults via Nrf2 activation. In this study, a systemic phytochemical investigation of the aerial parts of C. chartophyllum led to the isolation of thirty chemical constituents, which were further evaluated for their Nrf2 inducing potential using NAD(P)H: quinone reductase (QR) assay. Among these purified constituents, a sesquiterpenoid bearing α, ß-unsaturated ketone group, 3S-(+)-9-oxonerolidol (NLD), and a diphenyl sharing phenolic groups, 3, 3', 4, 4'-tetrahydroxydiphenyl (THD) significantly activated Nrf2 and its downstream genes, NAD(P)H quinone oxidoreductase 1 (NQO-1), and γ-glutamyl cysteine synthetase (γ-GCS), and enhanced the nuclear translocation and stabilization of Nrf2 in human lung epithelial cells. Importantly, NLD and THD had no toxicities under the Nrf2 inducing doses. THD also demonstrated a potential of interrupting Nrf2-Keap1 protein-protein interaction (PPI). Furthermore, NLD and THD protected human lung epithelial cells against sodium arsenite [As(III)]-induced cytotoxicity. Taken together, we conclude that NLD and THD are two novel Nrf2 activators with potential application of preventing acute and chronic oxidative insults in human lung tissue.
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Cinnamomum/química , Fator 2 Relacionado a NF-E2/agonistas , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/química , Substâncias Protetoras/farmacologia , Animais , Arsenitos/toxicidade , Sítios de Ligação , Compostos de Bifenilo/química , Compostos de Bifenilo/metabolismo , Compostos de Bifenilo/farmacologia , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Cinnamomum/metabolismo , Células Epiteliais/citologia , Células Epiteliais/efeitos dos fármacos , Células Epiteliais/metabolismo , Glutamato-Cisteína Ligase/química , Glutamato-Cisteína Ligase/metabolismo , Humanos , Camundongos , Simulação de Acoplamento Molecular , NAD(P)H Desidrogenase (Quinona)/química , NAD(P)H Desidrogenase (Quinona)/metabolismo , Fator 2 Relacionado a NF-E2/metabolismo , Componentes Aéreos da Planta/química , Componentes Aéreos da Planta/metabolismo , Extratos Vegetais/farmacologia , Substâncias Protetoras/química , Estrutura Terciária de Proteína , Sesquiterpenos/química , Sesquiterpenos/metabolismo , Sesquiterpenos/farmacologia , Compostos de Sódio/toxicidadeRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: The calyxes and fruits of Physalis alkekengi L. var. franchetii (Mast.) Makino (Physalis Calyx seu Fructus), have been widely used in traditional and indigenous Chinese medicines for the therapy of cough, excessive phlegm, pharyngitis, sore throat, dysuria, pemphigus, eczema, and jaundice with a long history. AIM OF THE REVIEW: The present review aims to achieve a comprehensive and up-to-date investigation in ethnomedical uses, phytochemistry, pharmacology, and toxicity of P. alkekengi var. franchetii, particularly its calyxes and fruits. Through analysis of these findings, evidences supporting their applications in ethnomedicines are illustrated. Possible perspectives and opportunities for the future research are analyzed to highlight the gaps in our knowledge that deserves further investigation. MATERIAL AND METHODS: Information on P. alkekengi var. franchetii was collected via electronic search of major scientific databases (e.g. Web of Science, SciFinder, Google Scholar, Pubmed, Elsevier, SpringerLink, Wiley online and China Knowledge Resource Integrated) for publications on this medicinal plant. Information was also obtained from local classic herbal literature on ethnopharmacology. RESULTS: About 124 chemical ingredients have been characterized from different parts of this plant. Steroids (particularly physalins) and flavonoids are the major characteristic and bioactive constituents. The crude extracts and the isolated compounds have demonstrated various in vitro and in vivo pharmacological functions, such as anti-inflammation, inhibition of tumor cell proliferation, antimicrobial activity, diuretic effect, anti-diabetes, anti-asthma, immunomodulation, and anti-oxidation. CONCLUSIONS: P. alkekengi var. franchetii is an important medicinal plant for the ethnomedical therapy of microbial infection, inflammation, and respiratory diseases (e.g. cough, excessive phlegm, pharyngitis). Phytochemical and pharmacological investigations of this plant definitely increased in the past half century. The chemical profiles, including ingredients and structures, have been adequately verified. Modern pharmacological studies supported its uses in the traditional and folk medicines, however, the molecular mechanisms of purified compounds remained unclear and were worth of further exploration. Therefore, the researchers should be paid more attention to a better utilization of this plant.
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Medicina Tradicional Chinesa/métodos , Physalis/química , Extratos Vegetais/farmacologia , Animais , Etnofarmacologia , Flores , Humanos , Medicina Tradicional , Fitoterapia/métodosRESUMO
BACKGROUND: The aim of this study was to assess the efficacy and safety of vinorelbine and cisplatin (NP chemotherapy) alone or in combination with Aidi injection for the treatment of advanced nonsmall cell lung cancer (NSCLC). METHODS: Pertinent publications were identified in PubMed, EMBASE, Cochrane Library, CNKI, CQVIP, and Wanfang databases, up to December 8, 2015. After quality assessment of all included randomized controlled trials evaluating Aidi injection combined with NP chemotherapy for the treatment of advanced NSCLC, a meta-analysis was performed by Review Manager 5.2 and STATA 12.0 for statistical analyses. RESULTS: Twelve studies including 509 and 503 cases in the experimental and control groups, respectively, were finally analyzed. The meta-analysis revealed that when cisplatin dose ranging from 20 to 40 mg/m 2 , combination of Aidi injection and NP chemotherapy was statistically different compared with NP chemotherapy alone in enhancing efficiency (relative risk [RR] = 1.24, 95% confidence interval [CI] [1.05-1.47], P = 0.010) and reducing the incidence of Grade II or above nausea and vomiting (RR = 0.49, 95% CI [0.30-0.80], P = 0.005). Meanwhile, with cisplatin ranging from 80 to 120 mg/m 2 , no significant differences in efficiency (RR = 1.11, 95% CI [0.87-1.42], P = 0.390) and Grade II or above nausea and vomiting (RR = 0.88, 95% CI [0.71-1.10], P = 0.260) were obtained. In addition, Aidi injection combined with NP chemotherapy was superior to NP chemotherapy alone in improving the quality of life, alleviating Grade II or above leukopenia and thrombocytopenia. CONCLUSIONS: Aidi injection combined with NP chemotherapy can enhance efficiency, improve the quality of life, and decrease adverse effects in patients with advanced NSCLC.
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Protocolos de Quimioterapia Combinada Antineoplásica/uso terapêutico , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Medicamentos de Ervas Chinesas/administração & dosagem , Neoplasias Pulmonares/tratamento farmacológico , Protocolos de Quimioterapia Combinada Antineoplásica/efeitos adversos , Carcinoma Pulmonar de Células não Pequenas/psicologia , Cisplatino/administração & dosagem , Humanos , Injeções , Neoplasias Pulmonares/psicologia , Viés de Publicação , Qualidade de Vida , Vimblastina/administração & dosagem , Vimblastina/análogos & derivados , VinorelbinaRESUMO
To observe the effect of geniposide on non-alcoholic fatty liver disease (NAFLD), and discuss the mechanism of geniposide for NAFLD from the aspect of free fatty acid, forty healthy Wistar male rats were randomly divided into normal group, model group, geniposide and Xuezhikang group. The rats in normal group were fed with normal diets, and the rats in other 3 groups were given with high-fat diet for 8 weeks to induce the NAFLD models. From the week 5 to end of week 8, the rats in geniposide and Xuezhikang group were intervened with corresponding medicines. The body weight, liver wet weight, and fat weight of the rats were recorded. Visual and pathological changes in hepatic tissues were observed with HE staining. The contents of TG, FFA, FAS, AMPK, ACCase and Malonyl-CoA in hepatic tissue, contents of CHO and LDL-C in serum and activities of AST and ALT in serum were detected by using corresponding methods. The results showed that the body weight, liver wet weight, and fat weight of the rats, CHO, LDL-C, ALT and AST levels in serum, TG, FFA, FAS, ACCase and Malonyl-CoA levels in hepatic tissues of the rats in model group were significantly higher than those in normal group (P<0.01), while AMPK activity was significantly lower than that of the normal group (P<0.01), with obvious visual and pathological steatosis in hepatic tissues, and inflammatory injury occurred in model group. Compared with the model group, body weight of the rat, fat weight, levels of FFA in hepatic tissues, ALT and AST activities in serum, liver wet weight, TG, FAS, ACCase and Malonyl-CoA levels were significantly decreased in geniposide group (P<0.01), while the AMPK activity in hepatic tissues was significantly increased (P<0.05),with improvement in visual and pathological performance. Compared with the model group, liver wet weight, fat weight, TG and FFA levels in hepatic tissues, and LDL-C level in serum were significantly decreased in Xuezhikang group (P<0.05). Compared with Xuezhikang group, the body weight of rat, fat weight and FFA level in hepatic tissues were significantly lower in geniposide group (P<0.01), but with no significant difference in other aspects. These findings indicated that geniposide was highly effective in improving the pharmacological effect of NAFLD induced by high-fat diet, and the mechanism was achieved through AMPK-ACCase-Malonyl-CoA-FFA axis.
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Medicamentos de Ervas Chinesas/administração & dosagem , Ácidos Graxos não Esterificados/metabolismo , Iridoides/administração & dosagem , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Alanina Transaminase/metabolismo , Animais , Aspartato Aminotransferases/metabolismo , Humanos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Hepatopatia Gordurosa não Alcoólica/enzimologia , Hepatopatia Gordurosa não Alcoólica/metabolismo , Ratos , Ratos Wistar , Triglicerídeos/metabolismoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: The genus Litsea, mainly distributed in the tropical and subtropical regions, has been used in traditional and indigenous Chinese medicines for the treatment of diarrhea, stomachache, dyspepsia, gastroenteritis, diabetes, edema, cold, arthritis, asthma, pain, traumatic injury, etc. for a long history. The present review aims to provide a comprehensive summary on the ethnomedical uses, phytochemistry, and pharmacology of the Litsea species used in traditional Chinese medicine (TCM). Based on these data, evidences supporting their ethnopharmacological effectiveness are illustrated, and opportunities for the future research and development as well as the therapeutic potential of this genus are analyzed to highlight the gaps in our knowledge that deserves further investigation. MATERIAL AND METHODS: Information on the Litsea species was collected via electronic search (using Pubmed, SciFinder, Google Scholar, Web of Science and CNKI) and a library search for articles published in peer-reviewed journals. Furthermore, information was also obtained from some local books on ethnopharmacology. RESULTS: Twenty plants of the genus Litsea are found to be important traditional medicines in China, and have a long medicinal application for diarrhea, stomachache, dyspepsia, gastroenteritis, diabetes, edema, cold, arthritis, asthma, pain, traumatic injury, etc. Over 200 ingredients have been identified from these 20 Litsea species used in TCM, and flavonoids, terpenoids and alkaloids are considered as the characteristic and bioactive constituents. The crude extracts and the isolated metabolites of these medicinal plants have exhibited some in vitro and in vivo pharmacological effects, including antimicrobial, hepatoprotection, anti-inflammatory, antiasthmatic, immunomodulation, anti-diabetic, anticholelithogenic, as well as function on central nervous system, etc. CONCLUSIONS: The extensive literature survey reveals Litsea species to be a group of important medicinal plants used for the ethnomedical treatment of gastrointestinal diseases, diabetes, inflammatory disorders, and microbial infection in TCM. Pharmacological investigations have supported the use of some Litsea species in the traditional medicines. In addition, further researches targeting individual ingredients responsible for the pharmacological effects, as well as their mechanisms of action are necessary. The outcome of these studies will further support the therapeutic potential of the genus Litsea, and provide convincing evidences to its future clinical applications in modern medicine.
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Litsea , Animais , Etnofarmacologia , Humanos , Litsea/química , Medicina Tradicional Chinesa , Compostos Fitoquímicos/análise , Fitoterapia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêuticoRESUMO
AIMS: Although compelling evidence suggests that human hypothalamic hamartoma (HH) is intrinsically epileptogenic for gelastic seizures, the molecular mechanisms responsible for epileptogenesis within HH remain to be elucidated. The aim of this study was to test the hypothesis that hyperactivation of BDNF-TrkB signaling pathways in surgically resected HH tissue is a possible mechanism for downregulation of KCC2 expression, which in turn underlies GABA-mediated excitation within HH. METHODS: Activation of three major BDNF-TrkB signaling pathways including MAPKs, Akt, and PLCγ1 were evaluated in surgically resected HH tissue (n = 14) versus human hypothalamic control tissue (n = 8) using combined methodologies of biochemistry, molecular biology, cell biology, and electrophysiology. RESULTS: Our data show that compared with hypothalamic control tissue, in HH tissue, (i) activation of TrkB and expression of mature BDNF are elevated; (ii) MAPKs (including ERK1/2, p38, and JNK), Akt, and PLCγ1 are highly activated; (iii) KCC2 expression is downregulated; and (iv) pharmacological manipulation of TrkB signaling alters HH neuronal firing rate. CONCLUSION: Our findings suggest that multiple BDNF-TrkB signaling pathways are activated in HH. They act independently or collaboratively to downregulate KCC2 expression, which is the key component for GABA-mediated excitation associated with gelastic seizures.
Assuntos
Fator Neurotrófico Derivado do Encéfalo/metabolismo , Regulação para Baixo/fisiologia , Hamartoma/patologia , Doenças Hipotalâmicas/patologia , Hipotálamo/metabolismo , Glicoproteínas de Membrana/metabolismo , Proteínas Tirosina Quinases/metabolismo , Transdução de Sinais/fisiologia , Adolescente , Adulto , Fator Neurotrófico Derivado do Encéfalo/genética , Fator Neurotrófico Derivado do Encéfalo/farmacologia , Carbazóis/farmacologia , Criança , Pré-Escolar , Inibidores Enzimáticos/farmacologia , Feminino , Humanos , Hipotálamo/patologia , Técnicas In Vitro , Alcaloides Indólicos/farmacologia , Lactente , Masculino , Glicoproteínas de Membrana/genética , Potenciais da Membrana/efeitos dos fármacos , Potenciais da Membrana/fisiologia , Neurônios/efeitos dos fármacos , Neurônios/fisiologia , Técnicas de Patch-Clamp , Fosforilação/efeitos dos fármacos , Proteínas Tirosina Quinases/genética , Receptor trkB , Transdução de Sinais/efeitos dos fármacos , Simportadores/metabolismo , Tirosina/metabolismo , Adulto Jovem , Cotransportadores de K e Cl-RESUMO
The objective of this study was to evaluate the efficacy and safety of a traditional Chinese medicine, Fufang Xuelian Burn Ointment (FXBO), to treat superficial and deep second-degree burn wounds. A four-center, randomized, controlled, and prospective study was conducted. Overall, 240 patients with either superficial or deep second-degree burn wounds were enrolled consecutively in this study. Patients who were randomly assigned to the control group (superficial: 72, deep: 48) underwent common burn wound therapy, whereas those randomized to the treatment group (superficial: 72, deep: 48) received common burn wound therapy plus topical FXBO. The healing rate, healing time, effective rate, and safety data were compared between the two groups. The baseline characteristics were comparable for the two groups. The healing rate was 94.79(±7.50) in the control group and 98.60(±5.69) in the FXBO group after 14 days for patients with superficial second-degree burn wounds (P = 0.000), and 95.17(±9.68) versus 97.44(±9.81) at 28 for deep second-degree burn wounds (P = 0.025). The median healing time in the FXBO group were 9 and 21 days for superficial and deep second-degree burns, respectively, compared to 10.5 and 22.5 days, respectively, in control group (P(superficial) = 0.000 and P(deep) = 0.009). The results of the effective rate showed that comprehensive efficacy of the FXBO group was improved compared to the control group for either superficial or deep second-degree burns (P(superficial) = 0.035 and P deep = 0.003). There were no reported drug-related adverse events in both groups. Therefore, FXBO was well tolerated and more effective than control group for treating superficial and deep second-degree burn wounds.
Assuntos
Queimaduras/tratamento farmacológico , Medicamentos de Ervas Chinesas/uso terapêutico , Adolescente , Adulto , Idoso , Queimaduras/fisiopatologia , Medicamentos de Ervas Chinesas/efeitos adversos , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Pomadas , Estudos Prospectivos , Segurança , Resultado do Tratamento , Cicatrização/efeitos dos fármacos , Adulto JovemRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: The resinous exudates of the Commiphora species, known as 'myrrh', are used in traditional Chinese medicine for the treatment of trauma, arthritis, fractures and diseases caused by blood stagnation. Myrrh has also been used in the Ayurvedic medical system because of its therapeutic effects against inflammatory diseases, coronary artery diseases, gynecological disease, obesity, etc. AIM OF THE REVIEW: Based on a comprehensive review of traditional uses, phytochemistry, pharmacological and toxicological data on the genus Commiphora, opportunities for the future research and development as well as the genus' therapeutic potential are analyzed. METHODS: Information on the Commiphora species was collected via electronic search (using Pubmed, SciFinder, Scirus, Google Scholar and Web of Science) and a library search for articles published in peer-reviewed journals. Furthermore, information also was obtained from some local books on ethnopharmacology. This paper covers the literature, primarily pharmacological, from 2000 to the end of December 2011. RESULTS: The resinous exudates from the bark of plants of the genus Commiphora are important indigenous medicines, and have a long medicinal application for arthritis, hyperlipidemia, pain, wounds, fractures, blood stagnation, in Ayurvedic medicine, traditional Chinese medicine and other indigenous medical systems. Phytochemical investigation of this genus has resulted in identification of more than 300 secondary metabolites. The isolated metabolites and crude extract have exhibited a wide of in vitro and in vivo pharmacological effects, including antiproliferative, antioxidant, anti-inflammatory and antimicrobial. The bioactive steroids guggulsterones have attracted most attention for their potent hypolipidemic effect targeting farnesoid X receptor, as well as their potent inhibitory effects on tumor cells and anti-inflammatory efficiency. CONCLUSIONS: The resins of Commiphora species have emerged as a good source of the traditional medicines for the treatment of inflammation, arthritis, obesity, microbial infection, wound, pain, fractures, tumor and gastrointestinal diseases. The resin of C. mukul in India and that of C. molmol in Egypt have been developed as anti-hyperlipidemia and antischistosomal agents. Pharmacological results have validated the use of this genus in the traditional medicines. Some bioassays are difficult to reproduce because the plant materials used have not been well identified, therefore analytical protocol and standardization of extracts should be established prior to biological evaluation. Stem, bark and leaf of this genus should receive more attention. Expansion of research materials would provide more opportunities for the discovery of new bioactive principles from the genus Commiphora.
Assuntos
Anti-Infecciosos/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Antineoplásicos Fitogênicos/uso terapêutico , Antioxidantes/uso terapêutico , Commiphora/química , Fitoterapia , Extratos Vegetais/uso terapêutico , Animais , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Humanos , Ayurveda , Medicina Tradicional Chinesa , Casca de Planta , Extratos Vegetais/farmacologia , Resinas VegetaisRESUMO
OBJECTIVE: To investigate the effects of Zhi Zi (Fructus Gardeniae) on non-alcoholic fatty liver disease (NAFLD) induced by a high-fat diet in the rat. METHODS: A rat model of NAFLD was established using a high-fat diet. Twenty one rats were randomly divided into a normal group, a model group and a Zhi Zi treatment group, 7 rats per group. Drinking water and the drug were intragastrically administrated for 5 weeks. Samples were then taken to observe pathological changes of the liver tissue (HE staining); changes in the fat metabolism pathway e. g. triglyceride (TG) and free fatty acid (FFA) content; alterations in liver function, i.e. serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activity; and differences in tumor necrosis factor alpha (TNF-alpha) and P-IkB protein expression in the liver tissue. RESULTS: Fatty degeneration and vacuole-like changes of different degrees occurred in hepatic cells of the model group. Markers for fat metabolism, serum ALT and AST activities, and expression of TNF-alpha and P-IkB proteins in liver tissue significantly increased. Fat metabolism in the Zhi Zi group significantly reduced, as shown by a drop in marker levels. Serum ALT and AST activities, and expression of TNF-alpha, P-IkB proteins in liver tissue were also significantly decreased in this group. CONCLUSION: Zhi Zi has a very strong inhibitory action on lipidosis and inflammatory injury in the rat model of NAFLD. This mechanism may possibly be related to the inhibition of the free fatty acid metabolism pathway.
Assuntos
Medicamentos de Ervas Chinesas/administração & dosagem , Fígado Gorduroso/tratamento farmacológico , Alanina Transaminase/sangue , Animais , Aspartato Aminotransferases/sangue , Modelos Animais de Doenças , Fígado Gorduroso/sangue , Fígado Gorduroso/genética , Fígado Gorduroso/metabolismo , Expressão Gênica/efeitos dos fármacos , Humanos , Proteínas I-kappa B/genética , Proteínas I-kappa B/metabolismo , Masculino , Hepatopatia Gordurosa não Alcoólica , Ratos , Ratos Sprague-Dawley , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/metabolismoRESUMO
In an attempt to understand the neuroprotective effect of Fructus Alpinia oxyphylla (AOE) and to elucidate its underlying mechanism of action, the ethanolic extract of AOE was investigated using zebrafish and PC12 cell models. AOE prevented and restored 6-hydroxydopamine (6-OHDA)-induced dopaminergic (DA) neuron degeneration and attenuated a deficit of locomotor activity in a zebrafish (Danio rerio) model of Parkinson's disease (PD). Treatment with AOE increased the viability of 6-OHDA-treated PC12 cells in vitro in a dose-dependent manner by attenuating cellular apoptosis. However, protocatechuic acid (PCA) and chrysin, two known polyphenol components of AOE, could not reproduce the neuroprotective activity of AOE in the PD zebrafish or PC12 cell models. A mechanistic study found that the protective effect of AOE against 6-OHDA-induced neuronal injury involved anti-inflammatory action (down-regulation of gene expression of IL-1ß and TNF-α) and anti-oxidative action (inhibition of NO production and iNOS expression in PC12 cells). Moreover, the PI3K-AKT pathway might be part of the mechanism of neuroprotection of AOE. The results of this research are expected to provide a scientific rationale for the use of AOE in the treatment of PD. However, it is important that the active components that contribute to the neuroprotective action of AOE are identified and characterized.
Assuntos
Citoproteção/efeitos dos fármacos , Neurônios Dopaminérgicos/efeitos dos fármacos , Oxidopamina/toxicidade , Extratos Vegetais/farmacologia , Alpinia , Animais , Comportamento Animal/efeitos dos fármacos , Morte Celular/efeitos dos fármacos , Neurônios Dopaminérgicos/fisiologia , Embrião não Mamífero , Etanol/farmacologia , Larva/efeitos dos fármacos , Larva/crescimento & desenvolvimento , Larva/fisiologia , Locomoção/efeitos dos fármacos , Células PC12 , Extratos Vegetais/química , Ratos , Peixe-Zebra/embriologia , Peixe-Zebra/crescimento & desenvolvimentoRESUMO
Forty three cultivated and wild Chinese medical herbs erigeron breviscapus were scanned on two Fourier transform near-infrared spectroscopy instruments. Twenty samples were used to set up the BP-NN models and the others were used to validate the models. Fifteen principal components, whose variance contribution rate is above 99%, were collected as input nodes for BP-NN models. The correct identification rates of calibration samples were 100% for the models on both the two instruments, and the correct identification rates of validation samples were 100% and 95.7%, irrespectively. The results showed that using NIR to fast detect cultivated and wild Chinese medical herbs erigeron breviscapus was feasible.