RESUMO
Maca has been traditionally used to enhance sexual behavior and fertility. Recently, maca's neuroprotective effects have been reported. The purpose of this study was to investigate whether the ethanol extract of maca (EEM) (100 mg/kg/bw, 200 mg/kg/bw, 400 mg/kg/bw, p.o.) exerted neuroprotective effects in corticosterone (CORT)-induced (40 mg/kg/bw, s.c.) rats, to determine the neuroprotective effects of EEM (12.5, 25, 50 µg/ml) and macamides in H2O2-induced (50 µM) PC12 cells. The acute toxicity (2000 mg/kg/bw, p.o.) and subacute toxicity (200 mg/kg/bw, 500 mg/kg/bw, 1000 mg/kg/bw, p.o.) of EEM were evaluated by mouse models. EEM reversed CORT-induced abnormal behaviors, reduced the contents of TNF-α, IL-6 in hippocampi, and increased the positive cells of doublecortin (DCX), bromodeoxyuridine (BrdU) and DCX + BrdU in the hippocampus of rats. Moreover, EEM and 4 macamides remarkably increased the cell viability in H2O2-induced PC12 cells. EEM promoted the phosphorylation of IκBα and p65, suppressed the NF-κB activation, and inhibited the levels of pro-inflammatory cytokines such as TNF-α, IL-6 and their mRNA levels in H2O2-induced PC12 cells. In conclusion, EEM could exert neuroprotective effects in CORT-induced rats and in H2O2-induced PC12 cells. Moreover, EEM did not present relevant toxicity after exposure to single and repeated doses.
Assuntos
Corticosterona/antagonistas & inibidores , Corticosterona/toxicidade , Etanol/química , Peróxido de Hidrogênio/antagonistas & inibidores , Peróxido de Hidrogênio/toxicidade , Lepidium/química , Fármacos Neuroprotetores/farmacologia , Extratos Vegetais/farmacologia , Animais , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Corticosterona/administração & dosagem , Relação Dose-Resposta a Droga , Proteína Duplacortina , Feminino , Hipocampo/efeitos dos fármacos , Hipocampo/metabolismo , Peróxido de Hidrogênio/administração & dosagem , Masculino , Camundongos , Camundongos Endogâmicos , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/isolamento & purificação , Células PC12 , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Ratos , Ratos Wistar , Testes de Toxicidade AgudaRESUMO
Poor wound healing is a major and global threat to public health. Efforts have been made to better understand the underlying mechanisms and develop effective remedies, though the advancements that have been made are still limited. As there are no effective and generally applicable therapies available for skin injuries and fibrosis, it is urgent to develop new drugs and therapies that facilitate wound healing and effectively improve scars. In this study, GC-MS analysis was performed to identify the chemical composition of rosehip oil. The excisional wound healing model and the carrageenan-induced paw edema method were respectively applied to evaluate the wound healing activity and anti-inflammatory activity of rosehip oil. Hematoxylin and eosin staining was used to assess the pathological changes of sections, and Sirius-red staining was performed to analyze the ratio of collagen I/III in wound tissues. Immunohistological staining for CD68, CCR7 (CD197), CD163, TGF-ß1, and α-SMA was applied to determine the macrophage phenotypes transition (M1-to-M2) and demonstrate the scar-improving efficacy of rosehip oil on wound healing. Results showed that rosehip oil significantly promoted wound healing and effectively improved scars. This efficacy might be exerted by accelerating the macrophage phenotypes transition and inhibiting the process of epithelial-mesenchymal transition.
Assuntos
Macrófagos/efeitos dos fármacos , Óleos de Plantas/farmacologia , Rosa/química , Cicatrização/efeitos dos fármacos , Animais , Antígenos CD/análise , Diferenciação Celular/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas , Masculino , Camundongos , Fenótipo , Óleos de Plantas/química , Ratos WistarRESUMO
Persistent bacterial colonization, abnormal inflammatory responses, and impaired angiogenesis pose significant challenges to effective wound repair, particularly in diabetic wounds. Employing exogenous bioactive substances in wound dressings is a recognized approach to dynamically respond to the wound microenvironment and accelerate the repair process. However, this strategy can lead to the development of drug resistance and induce further tissue damage. To address these challenges, we are synthesizing a novel hydrogel for diabetic wound treatment using functional poly (ionic liquid) and modified dextran. The hydrogel is characterized by its excellent tissue adhesion, exceptional self-healing capacity, and substantial compressive deformation. It exhibits broad antibacterial activity, reduces the expression of pro-inflammatory cytokines and enhances the healing in diabetic wounds. Its efficacy is superior to that of the positive control group. This innovative non-releasing hydrogel presents as a promising alternative to conventional antibiotics, offering significant potential for the treatment and healing of diabetic chronic wounds.
RESUMO
A non-destructive method of collecting samples for DNA analysis of the Chinese giant salamander is described and validated. DNA was extracted from the skin secretion and shedding using a Chelex-based method, and partial 12S rRNA gene sequences were amplified and sequenced. Sequences from skin secretion and shedding were cross-checked against the reported sequences from liver and were found to be identical. This method provides a non-destructive way of carrying out larger studies of the genetics of rare amphibians and may be of general use for genetic-based field studies of amphibians.
Assuntos
Pele/metabolismo , Urodelos/fisiologia , Animais , Sequência de Bases , Primers do DNA , Eletroforese em Gel de Poliacrilamida , Feminino , Dados de Sequência Molecular , Reação em Cadeia da Polimerase , Homologia de Sequência de Aminoácidos , Urodelos/genéticaRESUMO
Uncontrolled bleeding is one of the leading causes of human mortality. Existing hemostatic materials or techniques cannot meet the clinical requirements for safe and effective hemostasis. The development of novel hemostatic materials has always been of great interest. Chitosan hydrochloride (CSH), a derivative of chitin, is extensively used on wounds as an antibacterial and hemostatic agent. However, the formation of intra- or intermolecular hydrogen bonds between hydroxyl and amino groups limits its water solubility and dissolution rate and affects its effectiveness in promoting coagulation. Herein, we covalently grafted aminocaproic acid (AA) to the hydroxyl and amino groups of CSH via ester and amide bonds, respectively. The solubility of CSH in water (25 °C) was 11.39 ± 0.98 % (w/v), whereas the AA-grafted CSH (CSH-AA) reached 32.34 ± 1.23 % (w/v). Moreover, the dissolution rate of CSH-AA in water was 6.46 times higher than that of CSH. Subsequent studies proved that CSH-AA is non-toxic, biodegradable, and has superior antibacterial and hemostatic properties to CSH. Additionally, anti-plasmin activity can be exerted by the dissociated AA from the CSH-AA backbone, which can help to lessen secondary bleeding.
Assuntos
Quitosana , Hemostáticos , Humanos , Hemostáticos/química , Quitosana/química , Ácido Aminocaproico/farmacologia , Hemorragia/tratamento farmacológico , Hemorragia/prevenção & controle , Hemostasia , Antibacterianos/químicaRESUMO
Amphibian skin can produce abundant secretion which contains many bioactive compounds. In this work, skin secretion of the Chinese giant salamander (Andrias davidianus) was obtained by mild electrical stimulation of the dorsal skin surface, and the main physiopathological properties of the secretion were described. Intraperitoneal administration of the skin secretion caused lethal effects in mice. Low doses of the skin secretion induced significant systemic and local effects like edema and nociception in mice. The activities of phospholipase A2 and proteolytic enzyme were likely related to the physiopathological activities observed. The work proved the complex toxic effects of the Chinese giant salamander skin secretion and provided clues to study its physiological function further.
Assuntos
Proteínas/farmacologia , Pele/metabolismo , Urodelos , Animais , Eletroforese em Gel de Poliacrilamida , Dose Letal Mediana , Camundongos , Pele/enzimologiaRESUMO
Lycoris species have been known since long ago as a multi-utility ethnomedicinal herbal in China. It has been reported to exhibit a number of properties such as anticancer, neuroprotective, and antibacterial activities. In the present study, the anticancer efficacy of dichloromethane extracts of Lycoris aurea (DELA), was evaluated both in vivo and in vitro using murine sarcoma 180 cells. To evaluate the effects of DELA on apoptotic cell death, flow cytometry and Western blotting were performed. DELA demonstrated promising inhibition effects on sarcoma 180 cells in vitro and a 53.49% inhibitory rate on cancer cells in vivo. DELA treatment increased thymus indices and spleen indices in vivo, indicating that it reduced tumours, but did not damage the main immune organs. The DELA-evoked increase in apoptotic cell death was accompanied by occurrence of cleaved caspase-3 and decreases in the ratio of Bcl-2/Bax. Further purification and LCMS analysis showed DELA contained homolycorine, 2α-hydroxyoduline, oduline, hippeastrine, 2α-hydroxy-6-O- methyloduline, and 2α-methoxy-6-O-methyloduline. These results indicate that DELA exerted its anticancer effects, at least in part, by inducing cancer cell apoptosis and thus can be considered as a potential candidate agent for treatment of cancer.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Lycoris/química , Extratos Vegetais/farmacologia , Alcaloides/química , Animais , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/química , Caspase 3/metabolismo , Proliferação de Células/efeitos dos fármacos , Masculino , Camundongos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Sarcoma 180/tratamento farmacológico , Sarcoma 180/metabolismoRESUMO
9-Methoxycamptothecin (MCPT) was found to have antitumour activities through topoisomerase inhibition. However, the type of cell death induced in the tumour cells treated with MCPT was not elucidated. In this study, MCPT and camptothecin were isolated from Nothapodytes foetida distributed in Hubei Province, China and identified by NMR spectroscopy. MCPT was tested by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide (MTT) assay using camptothecin as reference. Annexin V-FITC/propidium iodide double staining and real-time PCR were also performed. The IC50 value was (0.385 +/- 0.08) microM. The apoptosis rates increased from 9.5% to 17.27%, 30.14%, and 66.46% with an increase in MCPT concentrations from 0, 0.19, 0.38, to 0.95 microM, respectively. The ratio of Bax/Bcl-2 also increased from 1 to 1.61, 2.43, and 4.57, respectively. Bax and Bcl-2 are crucial to the mitochondria pathway. The results indicate that the mitochondria pathway may be involed in MCPT-induced murine sarcoma S180 apoptosis.
Assuntos
Apoptose/efeitos dos fármacos , Camptotecina/análogos & derivados , Magnoliopsida/química , Sarcoma Experimental/patologia , Animais , Sequência de Bases , Camptotecina/farmacologia , Linhagem Celular Tumoral , Primers do DNA , Citometria de Fluxo , Espectroscopia de Ressonância Magnética , Camundongos , Reação em Cadeia da Polimerase em Tempo Real , Espectrometria de Massas por Ionização por ElectrosprayRESUMO
The present study aims to investigate the protective effects of N-(3-methoxybenzyl)-(9Z,12Z,15Z)-octadecatrienamide (M 18:3) on corticosterone-induced neurotoxicity. A neurotoxic model was established by subcutaneous injection of corticosterone (40 mg per kg bw) for 21 days. Depressive behaviors (the percentage of sucrose consumption, the immobility time in the forced swimming test, and the total distance in the open field test) were observed. The levels of the brain-derived neurotrophic factor, the contents of tumor necrosis factor-α and interleukin-6, and the numbers of positive cells of doublecortin and bromodeoxyuridine in the hippocampus were measured. The density of hippocampal neurons was calculated. The morphological changes of hippocampal neurons (the density of dendritic spines, the dendritic length, and the area and volume of dendritic cell bodies) were observed. The expression levels of synaptophysin, synapsin I, and postsynaptic density protein 95 were measured. Behavioral experiments showed that M 18:3 (5 and 25 mg per kg bw) could remarkably improve the depressive behaviors. The enzyme-linked immunosorbent assay showed that M 18:3 could considerably reduce hippocampal neuroinflammation and increase hippocampal neurotrophy. Nissl staining showed that M 18:3 could remarkably improve the corticosterone-induced decrease in the hippocampal neuron density. Immunofluorescence analysis showed that M 18:3 could considerably promote hippocampal neurogenesis. Golgi staining showed that M 18:3 could remarkably improve the corticosterone-induced changes in the hippocampal dendritic structure. Western blotting showed that M 18:3 could considerably increase the expression levels of synaptic-structure-related proteins in the hippocampus. In conclusion, the protective effects of M 18:3 may be attributed to the anti-inflammatory, neurotrophic, and synaptic protection properties.
Assuntos
Alcenos/farmacologia , Compostos de Benzil/farmacologia , Hipocampo/efeitos dos fármacos , Lepidium , Fármacos Neuroprotetores/farmacologia , Alcenos/farmacocinética , Animais , Anti-Inflamatórios não Esteroides/farmacologia , Antidepressivos/farmacologia , Comportamento Animal/efeitos dos fármacos , Compostos de Benzil/farmacocinética , Barreira Hematoencefálica/metabolismo , Contagem de Células , Forma Celular , Corticosterona , Depressão/tratamento farmacológico , Hipocampo/citologia , Hipocampo/metabolismo , Hipocampo/fisiologia , Masculino , Proteínas do Tecido Nervoso/genética , Proteínas do Tecido Nervoso/metabolismo , Neurogênese , Neurônios/citologia , Fármacos Neuroprotetores/farmacocinética , Extratos Vegetais/química , Extratos Vegetais/farmacocinética , Extratos Vegetais/farmacologia , Ratos , Ratos Wistar , Sinapses/efeitos dos fármacos , Sinapses/fisiologiaRESUMO
This study investigated the protective effects of maca ethanol extract (EEM) and N-(3-methozybenzyl)-(9Z,12Z,15Z)-octadecatrienamide (M 18:3) on corticosterone (CORT)-induced testicular toxicity. Male Wistar rats were divided into 5 groups. Except for the control group, CORT (40 mg per kg·bw) was injected subcutaneously for 21 consecutive days to induce testicular toxicity. 1 h before CORT injection, the rats were treated with EEM (400 mg per kg·bw) and M 18:3 (5 mg per kg·bw, 25 mg per kg·bw) by gavage, except for the control group and model group. Epididymal sperm and biochemical, and histological parameters were evaluated for the protective effects of the drugs. EEM (400 mg per kg·bw) and M 18:3 (5 mg per kg·bw, 25 mg per kg·bw) increased the sperm concentration and sperm motility, decreased the production of abnormal sperms, and increased the number of spermatogonia and primary spermatocytes in the seminiferous tubules of CORT-induced rats. Moreover, EEM and M 18:3 decreased the MDA levels and the positive expression rates of TUNEL, whereas they increased the activities of SOD, CAT, GSH-Px, and GST, and the contents of GSH in the testicles of CORT-induced rats. Furthermore, EEM and M 18:3 alleviated CORT-induced reduction in the positive expression rates of PCNA and Ki67 in the testicles of rats. Besides, EEM and M 18:3 reduced the expression levels of Keap-1 and increased the expression levels of Nrf2, HO-1, γ-GCS, and NQO1 in the testicles of CORT-induced rats. In summary, the protective effects of EEM and M 18:3 may be attributed to their anti-oxidative and anti-apoptotic properties.
Assuntos
Corticosterona/toxicidade , Lepidium/química , Extratos Vegetais/farmacologia , Testículo/efeitos dos fármacos , Animais , Antioxidantes/metabolismo , Apoptose/efeitos dos fármacos , Antígeno Ki-67/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Extratos Vegetais/química , Antígeno Nuclear de Célula em Proliferação/metabolismo , Ratos , Ratos Wistar , Receptores Androgênicos/genética , Receptores Androgênicos/metabolismo , Túbulos Seminíferos/efeitos dos fármacos , Túbulos Seminíferos/patologia , Contagem de Espermatozoides , Motilidade dos Espermatozoides/efeitos dos fármacos , Espermatogênese/efeitos dos fármacos , Espermatozoides/anormalidades , Espermatozoides/efeitos dos fármacos , Espermatozoides/fisiologia , Testículo/metabolismoRESUMO
We have reported previously that 9-methoxycamptothecin (MCPT) showed significant antitumor activity in vitro. Here, agarose gel electrophoresis experiments were performed to evaluate MCPT's unwinding ability toward plasmid DNA and inhibitory activities against topoisomerases (Topo) I and II. Binding properties of MCPT to calf thymus DNA (CT-DNA) were evaluated by UV-vis, melting temperature, fluorescence, circular dichroism methodologies and molecular docking technique. Results showed that MCPT at 100 µM inhibited Topo I activity, but had no effect on Topo II. Studies on the binding properties indicated that minor groove binding was the most probable binding mode of MCPT to DNA. The abilities of MCPT to act as Topo I inhibitor and minor groove binding agent may be related to its strong antitumor activity.
Assuntos
Camptotecina/análogos & derivados , Magnoliopsida/química , Inibidores da Topoisomerase I/farmacologia , Camptotecina/isolamento & purificação , Camptotecina/farmacologia , Dicroísmo Circular , DNA , Simulação de Acoplamento Molecular , Inibidores da Topoisomerase I/isolamento & purificaçãoRESUMO
Ginkgo biloba has long been used in ancient China for the treatment of cough, asthma, and other lung diseases. However, the active constituents in G. biloba for pulmonary disease treatment remain unclear. The objective of this study was to evaluate the anti-inflammatory active constituents in G. biloba and clarify their associated molecular mechanisms. The biological effects of different G. biloba extracts were evaluated in an ovalbumin-induced allergic mouse model. Anti-inflammatory compounds were present in the ethyl acetate phase of the extract, which were analysed by HPLC-MS. Biflavones were identified as the main compounds, which were further evaluated by docking calculations. Leukocyte elastase showed a high fit score with ginkgetin, one of the identified biflavones. The lowest binding free energy was -6.69 kcal mol-1. The effects of biflavones were investigated in vivo and in vitro. Ginkgetin markedly suppressed the abnormal expression of the Akt and p38 pathways in human neutrophil elastase (HNE)-stimulated A549 cells. Biflavones also decreased MUC5AC mRNA expression in HNE-stimulated A549 cells and the allergic mouse model. Inflammatory cells (neutrophils) and cytokines (IL-8) also decreased in mice treated with biflavones. The results suggest that G. biloba biflavones could inhibit the activity of leukocyte elastase. This in turn implicates G. biloba as a functional food for the treatment of airway inflammation.
Assuntos
Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/química , Ginkgo biloba/química , Pneumopatias/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Animais , Anti-Inflamatórios/isolamento & purificação , Biflavonoides/administração & dosagem , Biflavonoides/química , Biflavonoides/isolamento & purificação , Feminino , Humanos , Interleucina-8/genética , Interleucina-8/imunologia , Pneumopatias/genética , Pneumopatias/imunologia , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Mucina-5AC/genética , Mucina-5AC/imunologia , Extratos Vegetais/isolamento & purificação , Folhas de Planta/químicaRESUMO
Maca has attracted considerable attention owing to its neuroprotective effects in vitro and vivo. Macamides, a series of nonpolar and long-chain fatty acid N-benzylamides, are considered unique constituents in maca. This study investigated the protective effects of ethanol extracts of maca (EEM) and macamides on corticosterone-induced (CORT) neurotoxicity in rat pheochromocytoma (PC12) cells. CORT reduced cell viability and increased LDH release, intracellular ROS levels, and MMP decline rate, and induced mitochondrial apoptosis. However, pretreatment with EEM and macamides ameliorated CORT-induced neurotoxicity. EEM increased the cell viability and reduced the LDH release. M 18:1, M 18:2, and M 18:3 increased cell viability and reduced LDH release and intracellular ROS generation. M 18:2 and M 18:3 inhibited MMP reduction and reduced the Bax/Bcl-2 ratios. M 18:1 reduced the intracellular ROS without affecting other factors. Moreover, M 18:3 prevented CORT-induced mitochondrial apoptosis, restrained the expression levels of pro-apoptotic proteins, namely, Bax, cytochrome C, cleaved-caspase-3, and cleaved-PARP, and increased the expression levels of Bcl-2. In addition, M 18:3 increased Akt phosphorylation and the ability of M 18:3 to protect against CORT-induced cytotoxicity was remarkably reduced by LY294002, a PI3K phosphorylation inhibitor. M 18:3 also elevated the phosphorylation of CREB and activated the BDNF protein levels in CORT-induced PC12 cells. In conclusion, macamides, especially M 18:3, exert protective effects on CORT-induced PC12 cells. The cellular mechanism of M 18:3 against CORT-induced cytotoxicity may involve inhibition of mitochondrial apoptosis, and activation of Akt and CREB phosphorylation. Overall, macamides may potentially treat neuronal damage induced by CORT.
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ETHNOPHARMACOLOGICAL RELEVANCE: In traditional Chinese medicine, the aerial parts of Aeschynomene indica L. (AIL) have been used for wound healing, and to treat urinary tract infection, hepatitis, enteritis, dysentery, nyctalopia, conjunctivitis, urticaria, and furuncle. However, no scientific investigation has been conducted on its wound healing potential. AIM OF THE STUDY: To investigate the effects of AIL extract on wound healing, isolate the active constituent and reveal the possible mechanism of enhancing wound healing. MATERIALS AND METHODS: The circular excision wound healing model was used to evaluate in vivo wound-healing activity. Hematoxylin and eosin staining was applied to assess inflammatory cells infiltration, angiogenesis, fibroblast proliferation, collagen synthesis, collagen remodeling, and skin appendages generation. Sirius red-picric acid staining was employed for quantitative analysis of the ratio of collagen I/III. Immunohistochemical staining for CD68, CCR7 (CD197), CD163, TGF-ß1 and α-SMA was performed to determine macrophages phenotypes transition (M1-to-M2) and prove the scar-improving effect of AIL on wound healing. RESULTS: We successfully isolated the active constituent (Sub-Fr0.2) for wound healing from AIL extract, circular excision wound healing experiment and hematoxylin & eosin staining showed Sub-Fr0.2 has a significant promoting effect on wound healing. Results of sirius red-picric acid staining demonstrated a reduced ratio of collagen I/III in the Sub-Fr0.2 group as compared with the vehicle group. Immunohistochemical staining for CD68, CCR7 (CD197), and CD163 in the Sub-Fr0.2 group exhibited an elevated speed of macrophages transiting from M1 phenotype to M2 phenotype, when compared with the vehicle group. Besides, the expression of TGF-ß1 and α-SMA were inhibited on wounds treated with the ointment containing Sub-Fr0.2. CONCLUSION: Leaves of AIL and its active constituent (Sub-Fr0.2) effectively promoted wound healing and reduced scar formation, this efficacy might be exerted by accelerating macrophages phenotypes transition and inhibiting TGF-ß1 and α-SMA expression.
Assuntos
Dalbergia , Extratos Vegetais/farmacologia , Cicatrização/efeitos dos fármacos , Animais , Macrófagos/efeitos dos fármacos , Masculino , Fitoterapia , Folhas de Planta , Ratos Wistar , Pele/efeitos dos fármacos , Pele/patologiaRESUMO
Pyracantha fortuneana fruits are consumed as a dietary supplement in China and attenuate obesity and metabolic disorders. Obesity is known to be associated with intestinal barrier dysfunction driven by hyperglycemia and gut dysbiosis. However, whether the health benefits of P. fortuneana fruits are linked with the intestinal barrier function (IBF) remains unknown. This study aimed to evaluate the restorative effects of P. fortuneana fruit extract (PFE) on the IBF. Sprague Dawley rats were fed with a chow, a high-fat diet (HFD), or a PFE-supplemented diet for 8 weeks. Results showed that PFE intervention ameliorated HFD-induced intestinal barrier dysfunction by attenuating impaired structural integrity, reducing the elevated lactulose/mannitol ratio, and improving the mRNA and protein expression levels of tight junction proteins in HFD-fed rats. The ameliorations were associated with a beneficial effect on glycolipid homeostasis, as evidenced from the PFE decreasing intestinal absorptive capacity based on the d-xylose excretory rate, lowering the expression of GLUT2 and inhibiting digestive enzyme activities. The proanthocyanidins in the PFE showed greater in vitro inhibition on α-amylase, α-glucosidase, and lipase compared with triterpenoid saponins. Furthermore, the ameliorations on the IBF were also associated with effects on the microbial composition based on 16S rRNA gene sequence analysis. Several bacterial groups, which were linked with gut barrier integrity, were modulated after PFE administration, that is, Actinobacteria, Bacteroidaceae, Corynebacteriaceae, Lactobacillaceae, and S24-7 were elevated and the HFD-induced increase in Clostridia, Ruminococcaceae, Oscillospira, and Flexispira was restored. These data provide evidence for the ameliorative effect of the PFE on diet-induced intestinal barrier functional alternations in association with its capacity to modulate glycolipid digestion and gut microbiota in HFD-fed obese rats.
Assuntos
Microbioma Gastrointestinal/efeitos dos fármacos , Glicolipídeos/metabolismo , Mucosa Intestinal/efeitos dos fármacos , Obesidade/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Pyracantha/química , Animais , Bactérias/classificação , Bactérias/efeitos dos fármacos , Bactérias/genética , Bactérias/isolamento & purificação , Dieta Hiperlipídica/efeitos adversos , Frutas/química , Transportador de Glucose Tipo 2/genética , Transportador de Glucose Tipo 2/metabolismo , Humanos , Mucosa Intestinal/metabolismo , Mucosa Intestinal/microbiologia , Masculino , Obesidade/genética , Obesidade/metabolismo , Obesidade/microbiologia , Ratos , Ratos Sprague-DawleyRESUMO
Licochalcone A was isolated from the roots of Glycyrrhiza inflata and evaluated for its anti-inflammatory activity in xylene-induced mice ear edema and carrageenan-induced paw edema tests. At the same time, the inhibition of prostaglandin biosynthesis by licochalcone A was also studied in lipopolysaccharide (LPS)-induced mouse macrophage cells. At 5 mg/ ear, licochalcone A showed remarkable effects against acute inflammation induced by xylene, and at the doses of 2.5, 5, 10 mg/kg (p.o.), licochalcone A reduced significantly paw edema induced by carrageenan compared to the control at the fourth hour. Both COX-2 activity and expression were significantly inhibited by licochalcone A at all the test doses. Therefore, licochalcone A could be a useful compound for the development of new anti-inflammatory agents.
Assuntos
Anti-Inflamatórios/isolamento & purificação , Chalconas/isolamento & purificação , Glycyrrhiza/química , Animais , Anti-Inflamatórios/farmacologia , Chalconas/farmacologia , Ciclo-Oxigenase 2/efeitos dos fármacos , Ciclo-Oxigenase 2/metabolismo , Dinoprostona/metabolismo , Lipopolissacarídeos/farmacologia , Macrófagos Peritoneais/efeitos dos fármacos , Macrófagos Peritoneais/enzimologia , Camundongos , Camundongos Endogâmicos , Raízes de Plantas/química , Ratos , Ratos WistarRESUMO
Maca (Lepidium meyenii Walp.) is a cruciferous plant from the Andes of Peru. The root of Maca is traditionally employed for its supposed properties in aphrodisiacs and improving fertility, it also has been widely used to help alleviate the symptoms of menopause. The purpose of this study was to evaluate the effect of ethanol extract of Maca on postmenopausal osteoporosis in ovariectomized rats. Female Sprague-Dawley rats were divided into four groups: Sham-operated and ovariectomized groups were fed with equivolume of distilled water, and the remaining ovariectomized groups were orally administrated with ethanol extract of Maca at 0.096 and 0.24 g/kg for 28 weeks. The findings derived from the basis of bone mineral density, biomechanical, biochemical and histopathological parameters indicated that higher dose of ethanol extract of Maca was effective in the prevention of estrogen deficient bone loss.
Assuntos
Etanol/química , Lepidium/química , Osteoporose/prevenção & controle , Extratos Vegetais/farmacologia , Animais , Fenômenos Biomecânicos , Peso Corporal/efeitos dos fármacos , Feminino , Fêmur/efeitos dos fármacos , Tamanho do Órgão/efeitos dos fármacos , Ovariectomia , Ratos , Ratos Sprague-DawleyRESUMO
OBJECTIVE: To study the extraction technique for the flavonoids from Glycyrrhiza inflata and their bacteriostatic bioactivities. METHODS: It was investigated about comparison of extraction methods such as ultrasonic-assisted extraction (UAE), enzymatic extraction (EE), whisk extraction (WE) and repeat freeze-dissolve extraction (FDE). The UAE conditions were optimized by orthogonal array. The bacteriostatic effect was studied using doubling dilution. RESULTS: The UAE was the most effective method and the optimal UAE conditions were adding 20-fold ethanol (30% v/v), extracting for two times, 20 min each time. Futhermore, the minimal inhibitory concentrations (MIC) of the flavonoids against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Bacillus subtilis were 0.03125, 0.03125, 0.125, 0.03125 mg/ml respectively. CONCLUSION: UAE is suitable for fast and effective extraction of flavonoids. The flavonoids have obvious bacteriostatic bioactivities against microorganisms mentioned above.
Assuntos
Escherichia/efeitos dos fármacos , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Glycyrrhiza/química , Celulase , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Etanol , Raízes de Plantas/química , Plantas Medicinais/química , Pós , Rizoma/química , Staphylococcus aureus/efeitos dos fármacos , Tecnologia Farmacêutica/métodos , Fatores de Tempo , UltrassomRESUMO
BACKGROUND: Rapamycin (RAPA) has been successfully used for myoblast allotransplantation in X chromosome-linked muscular dystrophy mice. However, the mechanism of skeletal myogenesis, particularly in starved condition by RAPA, remains elusive. For this reason, we investigated the effect of RAPA on C2C12 myogenesis in serum-starved condition. METHODS: Serum-free treated C2C12 cells were mimicked as skeletal myogenesis in nutrition shortage microenvironment. A methylthiazoletetrazolium (MTT) assay was used to investigate different RAPA concentrations on serum-free treated C2C12 cells and the following assays were used to detect the characteristic of C2C12 myogenesis by RAPA in vitro. RESULTS: We found that 150 ng/mL of RAPA did not significantly suppress the viability of C2C12 differentiated cells by MTT assay. The RAPA concentration could protect myoblast serum-starved cells effectively from apoptosis through flow cytometry and retain myogenic regulatory factors through quantitative polymerase chain reaction analysis. However, RAPA significantly suppressed cell migration in wound healing assay (P<0.05). Morphological analyses indicated that RAPA also significantly suppressed myotube hypertrophy in serum-starved C2C12 cells. Western blot analysis revealed that the ratio of phosphate extracellular signal-regulated kinase/extracellular signal-regulated kinase and the protein level of p-Akt decreased in the proliferation medium and in the differentiation medium, respectively. CONCLUSION: These findings suggest that myoblast cells are sensitive to RAPA under a serum-starved microenvironment. As an immunosuppressive agent, RAPA shall be used as a considering dosage and as a safe strategy for future myoblast allotransplantation.
Assuntos
Imunossupressores/farmacologia , Desenvolvimento Muscular/efeitos dos fármacos , Mioblastos/efeitos dos fármacos , Sirolimo/farmacologia , Animais , Fusão Celular , Linhagem Celular , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Meios de Cultura Livres de Soro , Relação Dose-Resposta a Droga , MAP Quinases Reguladas por Sinal Extracelular/metabolismo , Regulação da Expressão Gênica , Hipertrofia , Camundongos , Mioblastos/metabolismo , Mioblastos/patologia , Fosforilação , Proteínas Proto-Oncogênicas c-akt/metabolismo , Fatores de Tempo , Cicatrização/efeitos dos fármacosRESUMO
OBJECTIVE: To evaluate the effect of long-term ethanol extract of Lepidium meyenii (Maca) on serum hormone levels in ovariectomized (OVX) rats and compare them with the effect of diethylstilbestrol. MATERIALS AND METHODS: Fifty female Sprague-Dawley rats were ovariectomized or sham operated. Both sham and OVX control groups (n = 10, respectively) received the vehicle. The remaining OVX rats were oral administrated with ethanol extract of Maca (0.096, or 0.24g/kg; n = 10, respectively) and diethylstilbestrol (0.05 mg/kg; n = 10). The treatment continued for 28 weeks. At week 12 and week 28, the blood of rats was collected and serum hormone levels, including estradiol (E2), testosterone (T) and follicle-stimulating hormone (FSH) were measured by radioimmunoassay. RESULTS: At week 12, the levels of serum E2 were slightly higher in Maca groups than that in OVX group; T levels were significantly decreased; and FSH levels were advanced slightly in Maca groups than that in sham group. After 28 weeks administration, serum E2 levels in Maca-treated animals did not differ significantly from sham control, the low dose of Maca increased serum E2 levels, and Maca prevented increase in serum FSH levels compared with OVX group. CONCLUSIONS: Long-term Maca supply modulates endocrine hormone balance in OVX rats, especially it decreases enhanced FSH levels. It is proposed that Maca may become a potential choice for postmenopausal women.