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1.
Int J Biol Macromol ; 266(Pt 2): 131391, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38582456

RESUMEN

Polysaccharides from Pinelliae Rhizoma Praeparatum Cum Alumine (PPA) have various biological activities, but their properties after oral administration are not clear. In this study, the absorption, digestion and fermentation properties of PPA were studied using in vivo fluorescence tracking, in vitro simulated digestion and fecal fermentation experiments. The absorption experiment showed that fluorescence was only observed in the gastrointestinal system, indicating that PPA could not be absorbed. Simulated digestion results showed that there were no significant changes in the molecular weight, Fourier transform infrared spectroscopy (FT-IR) spectrum, monosaccharides and reducing sugar of PPA during the digestion process, showing that the overall structure of PPA was not damaged. However, the carbohydrate gel electrophoresis bands of PPA enzymatic hydrolysates after simulated digestion were significantly changed, indicating that simulated digestion might impact the configuration of PPA. In vitro fermentation showed that PPA could be degraded by microorganisms to produce short chain fatty acids, leading to a decrease in pH value. PPA can promote the proliferation of Bacteroideaceae, Megasphaera, Bacteroideaceae, and Bifidobacteriaceae, and inhibit the growth of Desulfobacteriota and Enterobacteriaceae. The results indicated that PPA could treat diseases by regulating gut microbiota, providing a scientific basis for the application and development of PPA.


Asunto(s)
Digestión , Heces , Fermentación , Microbioma Gastrointestinal , Polisacáridos , Microbioma Gastrointestinal/efectos de los fármacos , Polisacáridos/química , Polisacáridos/farmacología , Humanos , Heces/microbiología , Heces/química , Digestión/efectos de los fármacos , Pinellia/química , Animales
2.
Int J Biol Macromol ; 260(Pt 1): 129431, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38237839

RESUMEN

Despite significant progress in diagnosis and treatment, asthma remains a serious public health challenge. The conventional therapeutic drugs for asthma often have side effects and unsatisfactory clinical efficacy. Therefore, it is very urgent to develop new drugs to overcome the shortcomings of conventional drugs. Natural polysaccharides provide enormous resources for the development of drugs or health products, and they are receiving a lot of attention from scientists around the world due to their safety, effective anti-inflammatory and immune regulatory properties. Increasing evidence shows that polysaccharides have favorable biological activities in the respiratory disease, including asthma. This review provides an overview of primary literature on the recent advances of polysaccharides from natural resources in the treatment of asthma. The mechanisms and practicability of polysaccharides, including polysaccharides from plants, fungus, bacteria, alga, animals and others are reviewed. Finally, the further research of polysaccharides in the treatment of asthma are discussed. This review can provide a basis for further study of polysaccharides in the treatment of asthma and provides guidance for the development and clinical application of novel asthma treatment drugs.


Asunto(s)
Asma , Polisacáridos , Animales , Polisacáridos/farmacología , Polisacáridos/uso terapéutico , Bacterias , Recursos Naturales , Asma/tratamiento farmacológico
3.
Molecules ; 28(4)2023 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-36838801

RESUMEN

The pericarp of Zanthoxylum bungeanum maxim (PZM) is a commonly used spice and herbal medicine in China. In the present study, the structural characteristics of PPZM were investigated by saccharide mapping after enzymatic digestion by using high-performance thin layer chromatography (HPTLC) and polysaccharide analysis by using carbohydrate gel electrophoresis (PACE). The mechanisms of protective effects of PPZM on Aß25-35-induced oxidative damage were explored in PC12 cells. The results showed that PPZM contained 1,4-α-D-galactosidic, 1,4-α-D-galactosiduronic, and (1→4)-ß-D-glucosidic linkages. Pretreatment with PPZM significantly increased the cell viability of Aß25-35-injured PC12 cells. Flow cytometry and Hoechst/PI staining indicated that PPZM gradually relieved the apoptosis of the Aß25-25-treated cells. PPZM markedly decreased the ROS level of PC12 cells and suppressed Aß25-35-induced oxidative stress by increasing the SOD level, and decreasing the level of MDA and LDH. The mRNA expressions of caspase-3 and Bax were significantly downregulated, and Bcl-2 expression was upregulated by treatment with PPZM. PPZM significantly increased the mRNA expression of Nrf2 and HO-1 in Aß25-35 treated cells. The results indicated that PPZM alleviated apoptosis and oxidative stress induced by Aß25-25 through the inhibition of mitochondrial dependent apoptosis and activation of Nrf2/HO-1 pathway. PPZM can be used as a potential protective agent against Aß25-25-induced neurotoxicity.


Asunto(s)
Fármacos Neuroprotectores , Zanthoxylum , Animales , Ratas , Fármacos Neuroprotectores/farmacología , Zanthoxylum/metabolismo , Factor 2 Relacionado con NF-E2/metabolismo , Estrés Oxidativo , Apoptosis , Polisacáridos/química , Células PC12 , ARN Mensajero/metabolismo , Péptidos beta-Amiloides/metabolismo , Fragmentos de Péptidos/metabolismo
4.
Eur J Pharmacol ; 914: 174691, 2022 Jan 05.
Artículo en Inglés | MEDLINE | ID: mdl-34896111

RESUMEN

Hydroxy-α-sanshool (HAS) is an unsaturated fatty acid amide from Zanthoxylum bungeanum Maxim. with hypolipidemic, hypoglycemic, anti-inflammatory, and neurotrophic effects, etc. In this study, results indicated that HAS effectively ameliorated spontaneous locomotion deficit of mice induced by D-galactose (D-gal) and AlCl3 treatment in open field test. Results of Morris water maze test (MWM) showed that HAS significantly improved the spatial learning and memory ability of aging mice. Histopathological evaluations revealed that HAS markedly alleviated morphological changes and increased number of Nissl neurons in hippocampus of D-gal/AlCl3-induced Alzheimer's disease (AD)-like mice. HAS markedly reduced malondialdehyde (MDA) production, and increased the activity of antioxidative enzymes including superoxide dismutase (SOD), glutathione peroxidase (GSH-Px) and catalase (CAT), showing an inhibitory effect on oxidative stress. Furthermore, HAS treatment obviously reversed the inhibitory expressions of mRNA and protein of HO-1 and Nrf2 in the hippocampus of AD mice, suggesting that neuroprotective effects of HAS against oxidative stress might be mediated by the Nrf2/HO-1 pathway. Meanwhile, HAS significantly inhibited neuronal apoptosis by decreasing mRNA and protein expressions of Cyt-c, Bax and Caspase 3, and increasing Bcl-2 expression in the hippocampus of AD mice. These results suggest that HAS have the potential to be developed as antioxidant drug for the prevention and early therapy of AD.


Asunto(s)
Enfermedad de Alzheimer , Ácidos Grasos Insaturados/farmacología , Hemo-Oxigenasa 1/metabolismo , Proteínas de la Membrana/metabolismo , Factor 2 Relacionado con NF-E2/metabolismo , Cuerpos de Nissl , Estrés Oxidativo/efectos de los fármacos , Alcamidas Poliinsaturadas/farmacología , Enfermedad de Alzheimer/tratamiento farmacológico , Enfermedad de Alzheimer/metabolismo , Enfermedad de Alzheimer/patología , Animales , Antioxidantes/farmacología , Modelos Animales de Enfermedad , Hipocampo/patología , Malondialdehído/metabolismo , Ratones , Fármacos Neuroprotectores/farmacología , Cuerpos de Nissl/efectos de los fármacos , Cuerpos de Nissl/metabolismo , Transducción de Señal/efectos de los fármacos , Aprendizaje Espacial/efectos de los fármacos , Zanthoxylum
5.
Front Pharmacol ; 12: 604040, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33746751

RESUMEN

Epilepsy is a chronic disease that can cause temporary brain dysfunction as a result of sudden abnormal discharge of the brain neurons. The seizure mechanism of epilepsy is closely related to the neurotransmitter imbalance, synaptic recombination, and glial cell proliferation. In addition, epileptic seizures can lead to mitochondrial damage, oxidative stress, and the disorder of sugar degradation. Although the mechanism of epilepsy research has reached up to the genetic level, the presently available treatment and recovery records of epilepsy does not seem promising. Recently, natural medicines have attracted more researches owing to their low toxicity and side-effects as well as the excellent efficacy, especially in chronic diseases. In this study, the antiepileptic mechanism of the bioactive components of natural drugs was reviewed so as to provide a reference for the development of potential antiepileptic drugs. Based on the different treatment mechanisms of natural drugs considered in this review, it is possible to select drugs clinically. Improving the accuracy of medication and the cure rate is expected to compensate for the shortage of the conventional epilepsy treatment drugs.

6.
Molecules ; 25(3)2020 Jan 28.
Artículo en Inglés | MEDLINE | ID: mdl-32012896

RESUMEN

Bombyx Batryticatus (BB) is a known traditional Chinese medicine (TCM) utilized to treat convulsions, epilepsy, cough, asthma, headaches, etc. in China for thousands of years. This study is aimed at investigating optimum extraction of protein-rich extracts from BB (BBPs) using response surface methodology (RSM) and exploring the protective effects of BBPs against nerve growth factor (NGF)-induced PC12 cells injured by glutamate (Glu) and their underlying mechanisms. The results indicated optimum process of extraction was as follows: extraction time 1.00 h, ratio of liquid to the raw material 3.80 mL/g and ultrasonic power 230.0 W. The cell viability of PC12 cells stimulated by Glu was determined by CCK-8 assay. The levels of γ-aminobutyric (GABA), interleukin-1ß (IL-1ß), interleukin-4 (IL-4), tumor necrosis factor-α (TNF-α), 5-hydroxytryptamine (5-HT) and glucocorticoid receptor alpha (GR) in PC12 cells were assayed by ELISA. Furthermore, the Ca2+ levels in PC12 cells were determined by flow cytometry analysis. Protein and mRNA expressions of GABAA-Rα1, NMDAR1, GAD 65, GAD 67, GAT 1 and GAT 3 in PC12 cells were evaluated by real-time polymerase chain reaction (RT-PCR) and Western blotting assays. Results revealed that BBPs decreased toxic effects due to Glu treatment and decreased Ca2+ levels in PC12 cells. After BBPs treatments, levels of GABA and 5-HT were increased and contents of TNF-α, IL-4 and IL-1ß were decreased in NGF-induced PC12 cells injured by Glu. Moreover, BBPs up-regulated the expressions of GABAA-Rα1, GAD 65 and GAD 67, whereas down-regulated that of NMDAR1 GAT 1 and GAT 3. These findings suggested that BBPs possessed protective effects on NGF-induced PC12 cells injured by Glu via γ-Aminobutyric Acid (GABA) signaling pathways, which demonstrated that BBPs has potential anti-epileptic effect in vitro. These findings may be useful in the development of novel medicine for the treatment of epilepsy.


Asunto(s)
Bombyx/metabolismo , Ácido Glutámico/efectos adversos , Proteínas de Insectos/farmacología , Transducción de Señal/efectos de los fármacos , Ácido gamma-Aminobutírico/metabolismo , Animales , Supervivencia Celular/efectos de los fármacos , Proteínas de Insectos/aislamiento & purificación , Interleucina-1beta/metabolismo , Interleucina-4/metabolismo , Factor de Crecimiento Nervioso/farmacología , Células PC12 , Ratas , Receptores de Glucocorticoides/metabolismo , Serotonina/metabolismo , Factor de Necrosis Tumoral alfa/metabolismo
7.
Food Funct ; 10(11): 7315-7324, 2019 Nov 01.
Artículo en Inglés | MEDLINE | ID: mdl-31637395

RESUMEN

Learning and memory impairments are common symptoms of dementia in neurodegenerative disorders. Occasionally, we found that Zanthoxylum bungeanum pericarps (ZBP) significantly activated the spontaneous activity of the hippocampus (HIPP) and paraHIPP (P < 0.001, uncorrected), implying the potential ability of ZBP to improve cognitive impairments. Thus, this study aimed to investigate the improving effect of hydroxy-α-sanshool (HAS), a characteristic ingredient of ZBP, against scopolamine (1 mg kg-1, i.p.)-induced learning and memory deficits. HAS (5 mg kg-1, p.o.) markedly reversed scopolamine-induced cognitive impairments, as indicated by its performance in the passive avoidance test and Morris water maze test (P < 0.01). Furthermore, HAS (2.5 and 5.0 mg kg-1, p.o.) also dose-dependently prevented changes in hippocampal neuronal morphology and apoptosis, inhibited acetylcholinesterase (AChE) activity, increased the acetylcholine (ACh) content, and increased the protein and mRNA expression of brain-derived neurotrophic factor (BDNF) and phospho-cAMP response element-binding (p-CREB) compared with those in the model group (P < 0.05 & P < 0.01). These findings demonstrated that HAS attenuated scopolamine-induced cognitive impairments mainly by enhancing the activity of the cholinergic system and increasing the CREB/BDNF signalling pathway.


Asunto(s)
Ácidos Grasos Insaturados/farmacología , Aprendizaje/efectos de los fármacos , Trastornos de la Memoria/inducido químicamente , Trastornos de la Memoria/tratamiento farmacológico , Alcamidas Poliinsaturadas/farmacología , Escopolamina/farmacología , Zanthoxylum/química , Animales , Encéfalo/efectos de los fármacos , Factor Neurotrófico Derivado del Encéfalo/genética , Factor Neurotrófico Derivado del Encéfalo/metabolismo , Ácidos Grasos Insaturados/química , Femenino , Regulación de la Expresión Génica/efectos de los fármacos , Hipocampo/citología , Humanos , Imagen por Resonancia Magnética , Masculino , Ratones , Neuronas/efectos de los fármacos , Alcamidas Poliinsaturadas/química , ARN Mensajero/genética , ARN Mensajero/metabolismo , Trimetoprim/análogos & derivados
8.
Int J Mol Sci ; 20(14)2019 Jul 20.
Artículo en Inglés | MEDLINE | ID: mdl-31330806

RESUMEN

Pinelliae Rhizoma Praeparatum cum Alumine (PRPCA) is an important traditional processed herbal medicine mainly used for treating phlegm in China for more than 2000 years. In our previous studies, extraction optimization, characterization, and bioactivities of total polysaccharides from PRPCA were investigated. In this study, further purification of these polysaccharides was performed. Two polysaccharides named neutral fraction of total polysaccharides-II (TPN-II) and acidic fraction of total polysaccharides-II (TPA-II) were obtained by gradient ion-exchange chromatography followed by gel-permeation chromatography. Results of scanning electron microscopy (SEM) analysis in the present study showed that TPN-II had a tight structure with a rough and uneven surface, while TPA-II had a relative homogeneous surface and a loose structure. Further studies indicated that TPN-II was a homosaccharide mainly composed by glucose with a molecular weight of 8.0 kDa. TPA-II was mainly composed of mannose, rhamnose, glucuronic acid, galacturonic acid, glucose, galactose and arabinose in a molar ratio of 2.1, 2.3, 1.7, 10.6, 2.6, 14.2, and 2.5, with a molecular weight of 1250 kDa. The nuclear magnetic resonance (NMR) results indicated that α and ß form glycoside bonds existed in TPN-II and TPA-II, and TPN-II was composed of α-glucopyranose. In addition, both purified polysaccharides have significant anti-inflammatory effects on mucus secretion of human airway epithelial NCI-H292 cells without cytotoxicity. Compared with TPN-II, TPA-II exhibited more significant anti-inflammatory effects on lipopolysaccharide (LPS)-induced airway inflammation by regulating levels of interleukin-4 (IL-4) and interferon-γ (IFN-γ) and inhibiting mucus secretion. The results suggest that polysaccharides from PRPCA could be explored as therapeutic agents in treating inflammation and over secretion of mucus in asthma.


Asunto(s)
Antiinflamatorios/química , Antiinflamatorios/farmacología , Moco/metabolismo , Pinellia/química , Polisacáridos/química , Polisacáridos/farmacología , Línea Celular , Supervivencia Celular/efectos de los fármacos , Humanos , Moco/efectos de los fármacos
9.
Oxid Med Cell Longev ; 2019: 7897584, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31198493

RESUMEN

Bombyx batryticatus is a known traditional Chinese medicine (TCM) utilized to treat convulsions, epilepsy, cough, asthma, headaches, and purpura in China for thousands of years. This study is aimed at investigating the antiepileptic effects of protein-rich extracts from Bombyx batryticatus (BBPs) on seizure in mice and exploring the protective effects of BBPs against H2O2-induced oxidative stress in PC12 cells and their underlying mechanisms. Maximal electroshock-induced seizure (MES) and pentylenetetrazole- (PTZ-) induced seizure in mice and the histological analysis were carried out to evaluate the antiepileptic effects of BBPs. The cell viability of PC12 cells stimulated by H2O2 was determined by MTT assay. The apoptosis and ROS levels of H2O2-stimulated PC12 cells were determined by flow cytometry analysis. Furthermore, the levels of malondialdehyde (MDA), superoxide dismutase (SOD), lactate dehydrogenase (LDH), and glutathione (GSH) in PC12 cells were assayed by ELISA and expressions of caspase-3, caspase-9, Bax, Bcl-2, PI3K, Akt, and p-Akt were evaluated by Western blotting and quantitative real-time polymerase chain reaction (RT-qPCR) assays. The results revealed that BBPs exerted significant antiepileptic effects on mice. In addition, BBPs increased the cell viability of H2O2-stimulated PC12 cells and reduced apoptotic cells and ROS levels in H2O2-stimulated PC12 cells. By BBPs treatments, the levels of MDA and LDH were reduced and the levels of SOD and GSH-Px were increased in H2O2-stimulated PC12 cells. Moreover, BBPs upregulated the expressions of PI3K, Akt, p-Akt, and Bcl-2, whereas they downregulated the expressions of caspase-9, caspase-3, and Bax in H2O2-stimulated PC12 cells. These findings suggested that BBPs possessed potential antiepileptic effects on MES and PTZ-induced seizure in mice and protective effects on H2O2-induced oxidative stress in PC12 cells by exerting antioxidative and antiapoptotic effects via PI3K/Akt signaling pathways.


Asunto(s)
Anticonvulsivantes/farmacología , Bombyx/química , Regulación de la Expresión Génica/efectos de los fármacos , Proteínas de Insectos/administración & dosificación , Fármacos Neuroprotectores/farmacología , Fosfatidilinositol 3-Quinasas/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo , Convulsiones/tratamiento farmacológico , Animales , Anticonvulsivantes/administración & dosificación , Antioxidantes/farmacología , Apoptosis , Supervivencia Celular , Convulsivantes/toxicidad , Electrochoque/efectos adversos , Peróxido de Hidrógeno/toxicidad , Proteínas de Insectos/farmacología , Masculino , Malondialdehído/metabolismo , Ratones , Fármacos Neuroprotectores/administración & dosificación , Oxidantes/toxicidad , Estrés Oxidativo/efectos de los fármacos , Células PC12 , Pentilenotetrazol/toxicidad , Fosfatidilinositol 3-Quinasas/genética , Proteínas Proto-Oncogénicas c-akt/genética , Ratas , Convulsiones/etiología , Convulsiones/metabolismo , Convulsiones/patología , Transducción de Señal
10.
Rev. bras. farmacogn ; 29(1): 111-124, Jan.-Feb. 2019. tab, graf
Artículo en Inglés | LILACS | ID: biblio-990759

RESUMEN

Abstract Toona sinensis (Juss.) M.Roem, Meliaceae, a deciduous plant native to eastern and southeastern Asia, is widely used in Traditional Chinese Medicine. This paper was aimed to summarize the current advances in traditional usage, phytochemistry, pharmacology and toxicology of T. sinensis. In this review, various types of data of T. sinensis are discussed in the corresponding parts of this paper, and perspectives for possible future studies of this plant are discussed. The main constituents of T. sinensis are terpenoids, phenylpropanoids and flavonoids, etc., and its pharmacological activities include anti-tumor effects, antioxidant activities, anti-diabetic effects and anti-inflammatory effects. Although a series of phytochemical and pharmacological researches of this plant have been conducted, the active constituents and action mechanism of these activities should be also further explored. Furthermore, the present review also indicates that T. sinensis has potentials to develop into drugs for treating various diseases with high efficacy and low toxicity, particularly in cancer, diabetes and inflammatory disorders. In conclusion, the paper provides a full-scale profile of the traditional usage, phytochemistry, pharmacology and toxicology of T. sinensis, and also provides potential therapeutic uses and drug development prospects of this plant.

11.
Comput Biol Chem ; 78: 297-305, 2019 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-30605855

RESUMEN

Inhibitor of nuclear factor kappa B kinase subunit beta (IKK-ß), a specific regulator of nuclear factor-κB (NF-κB), is considered a valid target to design novel candidate drugs to treat rheumatoid arthritis and various cancers. In the present study, quantitative structure-activity relationships (QSAR) and molecular docking techniques were used to screen for new IKK-ß inhibitors from a series of 2-acylamino-3-aminothienopyridine analogs. During the two-dimensional QSAR phase, the statistical model partial least square was selected from among two alternatives (r2 = 0.868, q2 (cross-validation) = 0.630). Descriptors with positive or negative contributions were derived from the created model. To build of three-dimensional QSAR models, we used three different fingerprints as analysis precepts for molecular clustering and the subsequent division of training sets and test sets. The best model, which used fingerprint model definition language public keys, was selected for further prediction of the compounds' activities. Favorable physicochemical, structural, electrostatic, and steric properties were derived from the created QSAR models and then used for drug design with an in-house library. Amongst the designed compounds, compounds B01 and B02 showed good predicted activities. Furthermore, after a selecting the protein structure and docking method, docking studies were carried out to reveal the detailed interactions between the ligands and the target protein. Binding affinity was measured and sorted using the value of "-CDOCKER_ENERGY". The high -CDOCKER_ENERGY values of compounds B01 (41.6134 kcal/mol) and B02 (40.1366 kcal/mol) indicated their prominent docking affinities.


Asunto(s)
Diseño de Fármacos , Quinasa I-kappa B/antagonistas & inhibidores , Simulación del Acoplamiento Molecular , Inhibidores de Proteínas Quinasas/farmacología , Relación Estructura-Actividad Cuantitativa , Relación Dosis-Respuesta a Droga , Humanos , Quinasa I-kappa B/metabolismo , Estructura Molecular , Inhibidores de Proteínas Quinasas/síntesis química , Inhibidores de Proteínas Quinasas/química
12.
Rev Bras Farmacogn ; 29(1): 111-124, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-32287507

RESUMEN

Toona sinensis (Juss.) M.Roem, Meliaceae, a deciduous plant native to eastern and southeastern Asia, is widely used in Traditional Chinese Medicine. This paper was aimed to summarize the current advances in traditional usage, phytochemistry, pharmacology and toxicology of T. sinensis. In this review, various types of data of T. sinensis are discussed in the corresponding parts of this paper, and perspectives for possible future studies of this plant are discussed. The main constituents of T. sinensis are terpenoids, phenylpropanoids and flavonoids, etc., and its pharmacological activities include anti-tumor effects, antioxidant activities, anti-diabetic effects and anti-inflammatory effects. Although a series of phytochemical and pharmacological researches of this plant have been conducted, the active constituents and action mechanism of these activities should be also further explored. Furthermore, the present review also indicates that T. sinensis has potentials to develop into drugs for treating various diseases with high efficacy and low toxicity, particularly in cancer, diabetes and inflammatory disorders. In conclusion, the paper provides a full-scale profile of the traditional usage, phytochemistry, pharmacology and toxicology of T. sinensis, and also provides potential therapeutic uses and drug development prospects of this plant.

13.
Molecules ; 22(10)2017 Oct 20.
Artículo en Inglés | MEDLINE | ID: mdl-29053625

RESUMEN

Bombyx batryticatus (B. batryticatus), a well-known traditional animal Chinese medicine, has been commonly used in China for thousands of years. The present paper reviewed advances in traditional uses, origin, chemical constituents, pharmacology and toxicity studies of B. batryticatus. The aim of the paper is to provide more comprehensive references for modern B. batryticatus study and application. In Traditional Chinese Medicine (TCM) culture, drugs containing B. batryticatus have been used to treat convulsions, headaches, skin prurigo, scrofula, tonsillitis and fever. Many studies indicate B. batryticatus contains various compounds, including protein and peptides, fatty acids, flavonoids, nucleosides, steroids, coumarin, polysaccharide and others. Numerous investigations also have shown that extracts and compounds from B. batryticatus exert a wide spectrum of pharmacological effects both in vivo and in vitro, including effects on the nervous system, anticoagulant effects, antitumor effects, antibacterial and antifungal effects, antioxidant effects, hypoglycemic effects, as well as other effects. However, further studies should be undertaken to investigate bioactive compounds (especially proteins and peptides), toxic constituents, using forms and the quality evaluation and control of B. batryticatus. Furthermore, it will be interesting to study the mechanism of biological activities and structure-function relationships of bioactive constituents in B. batryticatus.


Asunto(s)
Bombyx/química , Bombyx/metabolismo , Proteínas de Insectos/farmacología , Animales , Antiinfecciosos/farmacología , Antineoplásicos/farmacología , Humanos , Proteínas de Insectos/química , Proteínas de Insectos/uso terapéutico , Medicina Tradicional China , Sistema Nervioso/efectos de los fármacos , Relación Estructura-Actividad
14.
Molecules ; 22(6)2017 Jun 09.
Artículo en Inglés | MEDLINE | ID: mdl-28598407

RESUMEN

In this study, the ultrasound-assisted extraction of polysaccharides (PSA) from Pinelliae Rhizoma Praeparatum Cum Alumine (PRPCA) was optimized by response surface methodology (RSM). The structural characteristics of PSA were analyzed by UV-vis spectroscopy, infrared spectroscopy, scanning electron microscopy, high performance gel permeation chromatography and high performance liquid chromatography, respectively. In addition, antioxidant and antimicrobial activities of PSA were studied by different in vitro assays. Results indicated that the optimal extraction conditions were as follows: the ratio of water to raw of 30 mL/g, extraction time of 46.50 min, ultrasonic temperature of 72.00 °C, and ultrasonic power of 230 W. Under these conditions, the obtained PSA yield (13.21 ± 0.37%) was closely agreed with the predicted yield by the model. The average molecular weights of the PSA were estimated to be 5.34 × 10³ and 6.27 × 105 Da. Monosaccharide composition analysis indicated that PSA consisted of mannose, galactose uronic acid, glucose, galactose, arabinose with a molar ratio of 1.83:0.55:75.75:1.94:0.45. Furthermore, PSA exhibited moderate antioxidant and antibacterial activities in vitro. Collectively, this study provides a promising strategy to obtain bioactive polysaccharides from processed products of herbal medicines.


Asunto(s)
Antibacterianos/aislamiento & purificación , Antioxidantes/aislamiento & purificación , Extracción Líquido-Líquido/métodos , Pinellia/química , Polisacáridos/aislamiento & purificación , Sonicación/métodos , Antibacterianos/química , Antibacterianos/farmacología , Antioxidantes/química , Antioxidantes/farmacología , Benzotiazoles/antagonistas & inhibidores , Benzotiazoles/química , Compuestos de Bifenilo/antagonistas & inhibidores , Compuestos de Bifenilo/química , Candida albicans/efectos de los fármacos , Candida albicans/crecimiento & desarrollo , Escherichia coli/efectos de los fármacos , Escherichia coli/crecimiento & desarrollo , Análisis Factorial , Extracción Líquido-Líquido/instrumentación , Pruebas de Sensibilidad Microbiana , Monosacáridos/química , Picratos/antagonistas & inhibidores , Picratos/química , Polisacáridos/química , Polisacáridos/farmacología , Staphylococcus aureus/efectos de los fármacos , Staphylococcus aureus/crecimiento & desarrollo , Ácidos Sulfónicos/antagonistas & inhibidores , Ácidos Sulfónicos/química , Superóxidos/antagonistas & inhibidores , Superóxidos/química , Temperatura , Ácidos Urónicos/química
15.
Sci Rep ; 7: 40278, 2017 01 05.
Artículo en Inglés | MEDLINE | ID: mdl-28054652

RESUMEN

Charred areca nut (CAN) is used to treat dyspepsia and abdominal distension in children. However, reports revealed that arecoline, the most important active constituent of CAN, possesses potential toxicities. This study was designed to investigate the optimum arecoline content in CAN, using the "target constituent removal combined with bioactivity assay" strategy. Based on PTLC method, we prepared CAN lacking all arecoline (WAC-100R) and a series of different ratios of arecoline-removed CAN samples (WAC-Rx). MTT and acute toxicity assays indicated that decreasing content by 50% decreased CAN toxicity significantly. Animal results revealed arecoline contents over 50% could guarantee the beneficial effects of CAN on gastrointestinal tract. Additionally, decreasing arecoline content in CAN by 50% decreased its pro-apoptotic effects significantly. Furthermore, decreasing 50% arecoline content in CAN down-regulated the expressions of Cleaved-Caspase-3, c-jun, c-fos, COX-2, PGE2, and IL-1α. Thus, our results revealed that CAN with 50% arecoline content (WAC-50R) has similar beneficial effects on the gastrointestinal tract to CAN, whereas its toxicity was decreased significantly. Collectively, our study suggested that the strategy of "target constituent removal combined with bioactivity assay" is a promising method to identify the optimum arecoline content in CAN, which is approximately 0.12%.


Asunto(s)
Areca/toxicidad , Arecolina/aislamiento & purificación , Arecolina/toxicidad , Animales , Apoptosis , Areca/química , Línea Celular , Vaciamiento Gástrico/efectos de los fármacos , Tracto Gastrointestinal/efectos de los fármacos , Humanos , Ratones , Motilina/metabolismo , Contracción Muscular/efectos de los fármacos , Músculo Liso/efectos de los fármacos , Extractos Vegetales/toxicidad , Ratas Sprague-Dawley , Pruebas de Toxicidad/métodos , Péptido Intestinal Vasoactivo/metabolismo
16.
Pharm Biol ; 54(11): 2753-2760, 2016 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-27046150

RESUMEN

CONTEXT: Arecoline is an effective constituent of Areca catechu L. (Arecaceae) with various pharmacological effects. However, investigations also revealed that long use of arecoline could arouse some oral diseases. OBJECTIVE: The present review gathers the fragmented information available in the literature (before 1 October 2015) regarding pharmacology and toxicology of arecoline. We also discussed the potential developments and applications of arecoline in the future. METHODS: All the available information regarding the arecoline is compiled from scientific databases, including Science Direct, PubMed, Web of Science, Scopus, etc. RESULTS: Previous research demonstrated that arecoline is one of the major effective constituents in A. catechu. Additionally, arecoline has a wide spectrum of pharmacological activities including effects on nervous, cardiovascular, digestive and endocrine systems and anti-parasitic effects. What's more, arecoline is reported to be the primary toxic constituent of A. catechu, and the main toxic effects include oral submucous fibrosis (OSF), oral squamous cell carcinoma (OSCC) and genotoxicity. CONCLUSION: Arecoline has great potential to be a therapeutic drug for various ailments. However, further investigations are needed in the future to reduce or eliminate its toxicities before developing into new drug.


Asunto(s)
Arecolina/farmacología , Animales , Arecolina/uso terapéutico , Arecolina/toxicidad , Sistema Cardiovascular/efectos de los fármacos , Glándulas Endocrinas/efectos de los fármacos , Humanos , Sistema Nervioso/efectos de los fármacos
17.
J Ethnopharmacol ; 174: 317-21, 2015 Nov 04.
Artículo en Inglés | MEDLINE | ID: mdl-26320683

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Currently, human liver is susceptible to injury caused by alcohol and virus infiltration, resulting in hepatitis, cirrhosis, and even hepatocellular carcinoma. Paederia scandens (Lour.) Merr. var. tomentosa (Rubiaceae) has been used as traditional medicine in Asian countries to treat jaundice, dysentery, and abdominal mass. Furthermore, the abundance of iridoid glycosides in Paederia species indicates their notable hepatoprotective potential. MATERIALS AND METHODS: Total iridoid glycosides (TG) was prepared, and constituents of TG were analyzed by HPLC. TG and silymarin (positive) were orally administered for 15 days. Then, acute liver injury rats was induced by intraperitoneally injection (i.p.) of 10% CCl4 (0.12%, v/v, dissolved in olive oil, 10 mL/kg, body weight). Rats were sacrificed at 16 h after CCl4 injection. Liver tissues and blood were collected. Serum samples were prepared to determine the activities of alanine transaminase (ALT) and aspartate transaminase (AST), whereas liver tissue sections were prepared for the purpose of examining possible liver histopathological changes. In addition, antioxidant enzyme activities in liver tissues were also evaluated. RESULTS: Our results demonstrated that TG significantly decreased the levels of AST and ALT, compared with those in control rats. In addition, pre-treatment of the rats with TG clearly alleviated their liver tissue injuries. What's more, the activities of GSH, GAT and SOD in the groups of TG-treated rats were significantly increased compared with those of rats in the control group, whereas the levels of MDA were decreased. CONCLUSIONS: Our present research indicated that TG possessed notable hepatoprotective activity via decreasing oxidative stress level in liver tissues.


Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas/prevención & control , Glicósidos Iridoides/uso terapéutico , Extractos Vegetales/uso terapéutico , Rubiaceae , Animales , Enfermedad Hepática Inducida por Sustancias y Drogas/sangre , Enfermedad Hepática Inducida por Sustancias y Drogas/patología , Relación Dosis-Respuesta a Droga , Glicósidos Iridoides/aislamiento & purificación , Masculino , Extractos Vegetales/aislamiento & purificación , Ratas , Ratas Sprague-Dawley
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