RESUMO
OBJECTIVE: The aim of this study was to evaluate the therapeutic effect of Smilacis Glabrae Rhixoma (SGR) on osteoporosis at the level of network pharmacology, and to find new targets and mechanisms of SGR in the treatment of osteoporosis, to better find new drugs and their clinical applications. MATERIALS AND METHODS: In the original network pharmacology mode, we used an improved mode, such as screening the ingredients and targets of SGR through tools such as GEO database, Autodock Vina, and GROMACS. Through molecular docking, we conducted further screening for the targets acting on the effective ingredients of SGR, and finally we performed molecular dynamics simulation and consulted a large amount of related literature for the validation of the results. RESULTS: By screening and validating the data, we finally confirmed that there were mainly 10 active ingredients in SGR, which were isoeruboside b, smilagenin, diosgenin, stigmasterol, beta-sitosterol, sodium taurocholate, sitogluside, 4,7-dihydroxy-5-methoxy-6-methyl-8-formyl-flavan, simiglaside B, and simiglaside E, and mainly acted on eleven targets. These targets mainly exert therapeutic effects on osteoporosis by regulating 20 signaling pathways including Th17 cell differentiation, HIF-1 signaling pathway, apoptosis, inflammatory bowel disease, and osteoclast differentiation. CONCLUSIONS: Our study successfully explains the effective mechanism by which SGR ameliorates osteoporosis while predicting the potential targets NFKB1 and CTSK of SGR for the treatment of osteoporosis, which provides a novel basis for investigating the mechanism of action of new Traditional Chinese medicines (TCMs) at the network pharmacology level and a great support for subsequent studies on osteoporosis.
Assuntos
Medicamentos de Ervas Chinesas , Osteoporose , Humanos , Simulação de Acoplamento Molecular , Farmacologia em Rede , Osteoporose/tratamento farmacológico , Apoptose , Diferenciação Celular , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêuticoRESUMO
AIMS: We aimed to purify an antimicrobial protein from Bacillus amyloliquefaciens FS6 culture supernatant, verify its antimicrobial activity against Fusarium solani and evaluate its biocontrol potential for ginseng root rot. METHODS AND RESULTS: The antimicrobial protein was purified from FS6 culture supernatant using ammonium sulphate precipitation, anion exchange and gel chromatography. Based on mass spectrometry results, the purified protein was identified as an antimicrobial protein of the LCI family and was designated APC2 . The APC2 recombinant protein expressed in Escherichia coli (BL21) significantly inhibited F. solani and decreased the infection and spread of F. solani in ginseng root. An overexpressing APC2 strain FS6-APC2 was constructed and shown to have enhanced antimicrobial activity compared to the wild-type strain FS6. CONCLUSIONS: The APC2 protein shows strong antimicrobial activity against F. solani, reduces the incidence and severity of ginseng root rot caused by F. solani and exhibits a great biocontrol potential. SIGNIFICANCE AND IMPACT OF THE STUDY: This study reports the inhibitory activity of APC2 protein (LCI family) against F. solani and its protective efficacy on ginseng root rot. These findings provide a scientific basis for future research on the biocontrol mechanism, as well as the development and application of FS6.
Assuntos
Antifúngicos/farmacologia , Proteínas de Bactérias/farmacologia , Agentes de Controle Biológico/farmacologia , Fusarium/efeitos dos fármacos , Panax/microbiologia , Antifúngicos/metabolismo , Bacillus amyloliquefaciens/genética , Bacillus amyloliquefaciens/metabolismo , Proteínas de Bactérias/genética , Proteínas de Bactérias/metabolismo , Agentes de Controle Biológico/metabolismo , Escherichia coli/genética , Escherichia coli/metabolismo , Doenças das Plantas/microbiologia , Doenças das Plantas/prevenção & controle , Raízes de Plantas/microbiologia , Proteínas Recombinantes/genética , Proteínas Recombinantes/metabolismo , Proteínas Recombinantes/farmacologiaRESUMO
In the present study, the effect of feed Se supplementation on the Se content of raw milk and mozzarella cheese as well as the effect on cheese quality and functionality were determined. The Se milk was produced by supplying dairy cow feed with Se yeast (0.3mg of Se/kg of dry matter), resulting in a Se concentration in milk of 35.81µg/L. The fat, casein, and whey protein of Se milk were separated by ultracentrifugation, and the Se content was determined by atomic absorption spectroscopy. The Se distribution in different milk fractions of fat, casein, and whey protein were 9.82, 45.56, and 44.62%, respectively. The Se mozzarella cheese was made by Se milk, and the composition and texture of Se cheese did not significantly differ from that of the control. However, the functional properties (meltability, flowability, and stretchability) of the Se cheese were better after 8 wk of storage. Moreover, the pH and water activity were lower in Se cheese, which decreased the total plate count. The Se content in mozzarella cheese was 4 fold higher than that in milk, and Se was found in the whey, hot water, and brine collected during cheesemaking. Organic and inorganic Se was found in the Se cheese after 8 wk of storage, and most Se peptides detected after storage were Se-Met and Se-Cys. The results of this study show that feed Se supplementation can improve the Se content of milk and cheese without affecting mozzarella cheese quality.
Assuntos
Ração Animal/análise , Queijo/análise , Qualidade dos Alimentos , Selênio/administração & dosagem , Animais , Caseínas/análise , Bovinos , Contagem de Colônia Microbiana , Dieta/veterinária , Suplementos Nutricionais , Ácidos Graxos/análise , Feminino , Concentração de Íons de Hidrogênio , Leite/química , Selênio/análise , Proteínas do Soro do LeiteRESUMO
OBJECTIVES: Protein kinases orchestrate activation of signalling cascades in response to extra- and intracellular stimuli for regulation of cell proliferation. They are directly involved in a variety of diseases, particularly cancers. Systems biology approaches have become increasingly important in understanding regulatory frameworks in cancer, and thus may facilitate future anti-cancer discoveries. Moreover, it has been suggested and confirmed that high-throughput virtual screening provides a novel, effective way to reveal small molecule protein kinase inhibitors. Accordingly, we aimed to identify kinase targets and novel kinase inhibitors. MATERIALS AND METHODS: A series of bioinformatics methods, such as network construction, molecular docking and microarray analyses were performed. RESULTS: In this study, we computationally constructed the appropriate global human protein-protein interaction network with data from online databases, and then modified it into a kinase-related apoptotic protein-protein interaction network. Subsequently, we identified several kinases as potential drug targets according to their differential expression observed by microarray analyses. Then, we predicted relevant microRNAs, which could target the above-mentioned kinases. Ultimately, we virtually screened a number of small molecule natural products from Traditional Chinese Medicine (TCM)@Taiwan database and identified a number of compounds that are able to target polo-like kinase 1, cyclin-dependent kinase 1 and cyclin-dependent kinase 2 in HeLa cervical carcinoma cells. CONCLUSIONS: Taken together, all these findings might hopefully facilitate discovery of new kinase inhibitors that could be promising candidates for anti-cancer drug development.
Assuntos
Inibidores de Proteínas Quinases/metabolismo , Proteínas Serina-Treonina Quinases/metabolismo , Antineoplásicos/química , Antineoplásicos/metabolismo , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Proteínas de Ciclo Celular/antagonistas & inibidores , Proteínas de Ciclo Celular/metabolismo , Proliferação de Células/efeitos dos fármacos , Quinase 2 Dependente de Ciclina/antagonistas & inibidores , Quinase 2 Dependente de Ciclina/metabolismo , Bases de Dados de Proteínas , Células HeLa , Humanos , MicroRNAs/metabolismo , Simulação de Acoplamento Molecular , Mapas de Interação de Proteínas , Inibidores de Proteínas Quinases/química , Inibidores de Proteínas Quinases/farmacologia , Proteínas Serina-Treonina Quinases/antagonistas & inibidores , Proteínas Serina-Treonina Quinases/química , Estrutura Terciária de Proteína , Proteínas Proto-Oncogênicas/antagonistas & inibidores , Proteínas Proto-Oncogênicas/metabolismo , Quinase 1 Polo-LikeRESUMO
Ginseng (Panax ginseng) is an economically valuable medicinal herb mainly planted in Jilin Province, China. In September 2013, during harvest, suspected bacterial rots were observed on ginseng roots with about 10% incidence in Fusong County, Jilin Province, China (127°29.48' N, 42°11.12' E). Rotted roots completely lost their economic value. Symptoms on roots began as water-soaked lesions, and developed rapidly into a soft, watery, decayed mass within 3 to 5 days. Three diseased root tissues were surface-sterilized in 70% ethanol for 30 s, rinsed 3 times in sterilized water and cut into small pieces (2 to 3 mm). Tissues were then macerated for 5 min in sterilized water, streaked onto nutrient agar (NA) medium, and incubated at 28°C for 2 days. Representative colonies were selected from each plate and further purified by sub-culturing onto NA medium. Five strains of the bacteria were gram-negative, short straight rods, 0.5 to 1.0 × 1.5 to 3.0 µm with a single, polar flagellum. Colonies were round, smooth, translucent, and yellowish green on NA medium. The bacteria were identified based on physiological and biochemical tests as follows (3): They were levan and potato rot negative, oxidase, aerobic, and arginine dihydrolase positive, converted nitrate to N2, hydrolyzed gelatin, produced nitrites from nitrates, produced pyocyanin, and grew at 41°C. Bacterial identity was further confirmed by amplifying the 16S rRNA (1,461 bp), gyrB (1,134 bp), and 16S-23S ITS genes (523 bp) with 27F/1492R, UP1/UP2, and L1/L2 primer sets, respectively. The 16S rRNA gene sequence (NCBI Accession No. KJ156527), gyrB gene sequence (KJ748373), and 16S-23S ITS gene sequence (KJ748374) had 99% identity to that of Pseudomons aeruginosa strain BS01 (JQ229778), ATCC25011 (FJ652721), and ATCC15522 (AB547908), respectively. The strains were also identified by using BD Phoenix-100 Automated Microbiology System (BD Ltd., New Jersey) as P. aeruginosa with 99% confidence. A pathogenicity test was conducted by spraying a suspension of five strains individually (108 CFU/ml) onto 4-year-old ginseng roots (cv. Damaya) wounded with a sterilized needle. Five ginseng roots were inoculated with each strain and five ginseng roots were inoculated with sterilized water as controls. All inoculated plants were maintained at 28°C with 80 to 85% relative humidity. Soft, watery tissue rot symptoms developed 3 to 5 days after inoculation, and were similar to those observed on the diseased plants under natural conditions. In contrast, no symptoms developed on control plants. The bacteria were readily re-isolated from inoculated plants and identified as P. aeruginosa using bacterial colony morphology, physiological and biochemical tests, as well as sequence analysis of the 16S rRNA gene, fulfiling Koch's postulates. The bacterium was not isolated from control plants. P. aeruginosa has been reported to cause diseases in a variety of plants including onion (1,2), arabidopsis, and sweet basil (4). To our knowledge, this is the first report of P. aeruginosa causing ginseng root rot in China. References: (1) E. J. Cother et al. Phytopathology 66:828, 1976. (2) X. J. Hao, and G. L. Xie. J. Plant Pathol. 88:340, 2006. (3) N. W. Schaad et al. Laboratory Guide for the Identification of Plant Pathogenic Bacteria, 3rd edition. APS Press, St. Paul, MN, 2001. (4) T. S. Walker et al. Plant Physiol. 134:320, 2004.
RESUMO
Ginseng (Panax ginseng C.A. Meyer) is a treasure of traditional Chinese medicine resources and has been used in food, health care products, and medicines in China for over 4,000 years. Jilin Province is the largest producing region in the world. Ginseng root rot disease caused by Fusarium spp. is the chief disease of ginseng with more than 25% incidence. Infected ginseng roots could not be used, which brought economic losses, and the species of the pathogens were not clear. The above-ground leaves of infected ginseng plants became red in the early stages and later wilted or died. All parts of root including rhizome, taproot, and fibrous root can be infected. Brown lesions were mainly formed on the surface and expanded gradually. Finally, multiple lesions converged and caused root rot. Diseased roots collected in June 2012 from 4-year-old ginseng (cv. Damaya) from Jingyu County and Jiaohe City, Jilin Province. Six isolates were obtained by cutting the roots into 5 mm3 pieces, disinfecting in 3% NaOCl for 3 min, and isolating on half-strength acidified potato dextrose agar (PDA). All isolates were purified from single spore. They produced white and cottony aerial mycelium cultured on PDA, microconidia were in the majority, oval or reniform, and length ranged from 5.97 to 12.01 µm. Macroconidia were in the minority, fusiform to conical, usually 3 to 5 septa, length ranged from 13.99 to 26.50 µm, thin-walled, with a hooked apical cell and a foot-shaped basal cell. A variety of structures of chlamydospores were produced, in chains or in pairs, basidixed or in the middle of the hyphae. Preliminary conclusions were made according to the morphological characteristics, which were consistent with the descriptions of Fusarium redolens (2). All the isolates of Fusarium spp. were accurately identified based on molecular biological methods of rDNA internal transcribed spacer (ITS) and the elongation factor (EF1-α) gene sequences analysis. ITS sequences analysis (GenBank Accession No. KF499035) resulted in a 100% match for one accession of F. redolens (X94169) by BLAST in the NCBI nucleotide database, and EF1-α gene (KF499036) had 100% similarity with 12 accessions of F. redolens (e.g., AF324319) by BLAST in the FUSARIUM-ID database (1). All isolates of F. redolens were tested for pathogenicity on ginseng root in vitro and healthy plants in a greenhouse, respectively. The surface of healthy ginseng roots were washed and disinfested in 70% alcohol for 3 min and plant in flower pots with sterile sand and sorghum grain infested with 14-day-old isolates and no inoculation as the control. Each experiment was repeated three times. Root rots were assessed 21 days after planting and all the isolates consistently caused root rot on inoculated plants, taproot and fibrous root exhibited brown to black root rot and plant wilting, whereas no root rot was observed in the controls and the pathogen was successfully re-isolated. The results were confirmed by the in vitro and healthy plant inoculation of ginseng root. F. redolens was identified previously as F. oxysporum, but recent molecular studies have shown that they are distant species in phylogenetic analysis (3). To our knowledge, this is the first report of F. redolens causing root rot of ginseng in China. References: (1) M. D. Geiser et al. Eur. J. Plant Pathol. 110:473, 2004. (2) J. F. Leslie and B. A. Summerell. The Fusarium Laboratory Manual. Blackwell Publishing, Ames, IA, 2006. (3) K. O'Donnell et al. Mycologia 90:465,1998.
RESUMO
Previous studies have indicated that the renin-angiotensin-aldosterone system (RAAS) is implicated in the induction of sodium appetite in rats and that different dietary sodium intakes influence the mRNA expression of central and peripheral RAAS components. To determine whether dietary sodium deprivation activates regional brain neurons related to sodium appetite, and changes their gene expression of RAAS components of rats, the present study examined the c-Fos expression after chronic exposure to low sodium diet, and determined the relationship between plasma and brain angiotensin I (ANG I), angiotensin II (ANG II) and aldosterone (ALD) levels and the sodium ingestive behavior variations, as well as the effects of prolonged dietary sodium deprivation on ANG II type 1 (AT1) and ANG II type 2 (AT2) receptors and angiotensin-convertion enzyme (ACE) mRNA levels in the involved brain regions using the method of real-time polymerase chain reaction (PCR). Results showed that the Fos immunoreactivity (Fos-ir) expression in forebrain areas such as subfornical organ (SFO), paraventricular hypothalamic nuclei (PVN), supraoptic nucleus (SON) and organum vasculosum laminae terminalis (OVLT) all increased significantly and that the levels of ANG I, ANG II and ALD also increased in plasma and forebrain in rats fed with low sodium diet. In contrast, AT1, ACE mRNA in PVN, SON and OVLT decreased significantly in dietary sodium depleted rats, while AT2 mRNA expression did not change in the examined areas. These results suggest that many brain areas are activated by increased levels of plasma and/or brain ANG II and ALD, which underlies the elevated preference for hypertonic salt solution after prolonged exposure to low sodium diet, and that the regional AT1 and ACE mRNA are down-regulated after dietary sodium deprivation, which may be mediated by increased ANG II in plasma and/or brain tissue.
Assuntos
Encéfalo/metabolismo , Neurônios/metabolismo , Peptidil Dipeptidase A/genética , Receptor Tipo 1 de Angiotensina/genética , Sódio na Dieta/metabolismo , Sódio/deficiência , Aldosterona , Angiotensina I/metabolismo , Angiotensina II/metabolismo , Animais , Encéfalo/citologia , Regulação para Baixo/fisiologia , Regulação da Expressão Gênica/fisiologia , Hipotálamo/citologia , Hipotálamo/metabolismo , Hipotálamo Anterior/citologia , Hipotálamo Anterior/metabolismo , Masculino , Núcleo Hipotalâmico Paraventricular/citologia , Núcleo Hipotalâmico Paraventricular/metabolismo , Proteínas Proto-Oncogênicas c-fos/metabolismo , RNA Mensageiro/metabolismo , Ratos , Ratos Sprague-Dawley , Órgão Subfornical/citologia , Órgão Subfornical/metabolismoRESUMO
One kinds of glycolipid (SBI) have been isolated from the marine brown alga Sargassum hemiphyllum (Turn.) Ag. The structures of SBI have been determined as the sodium salt of 1-0-acyl-3-0-(6'-sulfo-alpha-D-quinovopyrannosyl) glycerol (acyl: tetradecanoyl, pentadecanoyl, 11-hexadecenoyl, hexadecanoyl, 10,13-octadecadienoyl, 9-octade cenoyl, 15-metylheptadecanoyl and 11-eicosenoyl 17: 1.5: 19: 153: 1: 19: 1: 2) on the basis of chemical and spectral evidence and GC-MS analysis, respectively. Four constituents of the SBI were new compounds [the sodium salt of 1-0-(11"-hexadecenoyl)-3-0-(6'-sulfo-alpha-D-quinovopyrannosyl) glycerol, the sodium salt of 1-0-(10",13"-octadecadienoyl)-3-0-(6'-sulfo-alpha-D-quinovopyrannosyl) glycerol, and the sodium salt of 1-0-(15"-metylhexadecenoyl)-3-0-(6'-sulfo-alpha-D-quinovopyrannosyl) glycerol, and the sodium salt of 1-0-(11"-eicosenoyl)-3-0-(6'-sulfo-alpha-D-quinovopyrannosyl) glycerol]. All compounds were isolated from marine brown alga for the first time.
Assuntos
Glicolipídeos/química , Phaeophyceae/química , Sulfoglicoesfingolipídeos/química , China , Medicamentos de Ervas Chinesas/química , Glicolipídeos/isolamento & purificação , Espectroscopia de Ressonância Magnética , Conformação Molecular , Sulfoglicoesfingolipídeos/isolamento & purificaçãoRESUMO
Sensory nerve-derived neuropeptides such as substance P demonstrate a number of proinflammatory bioactivities, but less is known about their role in inflammatory skin disease. The cell surface metalloprotease neutral endopeptidase (NEP) is the principal proteolytic substance P-degrading enzyme. This study tests the hypothesis that the absence of NEP results in dysregulated inflammatory skin responses. The effector phase of allergic contact dermatitis (ACD) responses was examined in NEP(-/-) knockout and NEP(+/+) wild-type mice and compared with the irritant contact dermatitis response in these animals. NEP was found to be normally immunolocalized in epidermal keratinocytes and dermal blood vessels. The ACD ear swelling response was 2.5-fold higher in animals lacking NEP and was accompanied by a significant increase in plasma extravasation and infiltration of inflammatory leukocytes. The augmented ACD response in NEP(-/-) animals was abrogated by either administration of a neurokinin receptor 1 antagonist or by repeated pretreatment with topical capsaicin. Similar to NEP(-/-) mice, the acute inhibition of NEP in NEP(+/+) animals resulted in an augmented ACD response. In contrast to the ACD responses, little differences were observed in the irritant contact dermatitis response of NEP(-/-) compared with NEP(+/+) animals after epicutaneous application of the skin irritants croton oil or SDS. Thus, these results indicate that NEP and cutaneous neuropeptides have a significant role in the pathogenesis of ACD.
Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Dermatite Alérgica de Contato/patologia , Dermatite Alérgica de Contato/prevenção & controle , Neprilisina/fisiologia , Substância P/toxicidade , Administração Cutânea , Animais , Anti-Inflamatórios não Esteroides/antagonistas & inibidores , Anti-Inflamatórios não Esteroides/metabolismo , Permeabilidade Capilar/genética , Permeabilidade Capilar/imunologia , Capsaicina/administração & dosagem , Óleo de Cróton/toxicidade , Dermatite Alérgica de Contato/enzimologia , Dermatite Alérgica de Contato/genética , Dermatite Irritante/enzimologia , Dermatite Irritante/genética , Dermatite Irritante/patologia , Dermatite Irritante/prevenção & controle , Inibidores Enzimáticos/administração & dosagem , Feminino , Glicopeptídeos/administração & dosagem , Injeções Intravenosas , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Knockout , Neprilisina/antagonistas & inibidores , Neprilisina/deficiência , Neprilisina/metabolismo , Antagonistas dos Receptores de Neurocinina-1 , Piperidinas/administração & dosagem , Quinuclidinas/administração & dosagem , Pele/irrigação sanguínea , Pele/enzimologia , Pele/patologiaRESUMO
AIM: To prepare lung targeted tetrandrine (TET) loaded sustained-release drug delivery system by microencapsulation, decrease the toxicity and enhance the therapeutic function of anti-pulmonary hypertension of TET. METHODS: Albumin microcapsules were produced by spray drying-thermal denaturation, a new technique. Some characterization of the prepared microcapsules was evaluated. Distribution of the microcapsules and their anti-pulmonary hypertension effect in vivo were investigated. RESULTS: The spherical microcapsules showed a drug loading of 37.88%. Compared to the original drug, the rate of TET released from the positively charged microcapsules in vitro was significantly decreased and fitted well by Higuchi equation. The TET concentrations in mouse lungs of TET microcapsules were significantly higher than those of TET injection, and the mean retained time of TET in lungs was prolonged from 157.1 h to 223.6 h after microencapsulation. The in vitro--in vivo correlation was established and confirmed (P < 0.001). CONCLUSION: The new spray drying-thermal denaturation method allows the preparation of drug loaded albumin microcapsules with desired results. The prepared microcapsules were found to have the potential function of delivering TET to pulmonary artery via i.v., with low toxicity and high efficacy.
Assuntos
Alcaloides/administração & dosagem , Anti-Hipertensivos/administração & dosagem , Benzilisoquinolinas , Sistemas de Liberação de Medicamentos , Medicamentos de Ervas Chinesas/administração & dosagem , Pulmão/metabolismo , Alcaloides/farmacocinética , Alcaloides/farmacologia , Animais , Anti-Hipertensivos/farmacocinética , Anti-Hipertensivos/farmacologia , Pressão Sanguínea/efeitos dos fármacos , Cápsulas , Preparações de Ação Retardada , Medicamentos de Ervas Chinesas/farmacocinética , Medicamentos de Ervas Chinesas/farmacologia , Hipertensão Pulmonar/metabolismo , Camundongos , Distribuição Aleatória , Ratos , Ratos Wistar , Distribuição TecidualRESUMO
OBJECTIVE: To explore the effect of Nephropathy mixture on genetic expression of liver albunin in rats with adriamycin-induced nephrotic syndrome. METHODS: The rat model of adriamycin-induced nephrotic syndrome was established and the liver albumin mRNA expression level was observed with Northern hybridization and Dot-blot quantitative analysis. RESULTS: The liver albumin mRNA expression level in the Nephropathy Mixture treated group was significantly higher than that in the model group and the normal control group (P < 0.05). CONCLUSION: Nephropathy Mixture could up-regulate the liver albumin mRNA expression level and promote the synthesis of albumin in rats with adriamycin-induced nephrotic syndrome.
Assuntos
Albuminas/biossíntese , Medicamentos de Ervas Chinesas/farmacologia , Fígado/metabolismo , Síndrome Nefrótica/metabolismo , Albuminas/genética , Animais , Doxorrubicina , Masculino , Síndrome Nefrótica/induzido quimicamente , RNA Mensageiro/biossíntese , RNA Mensageiro/genética , Ratos , Ratos Sprague-DawleyRESUMO
AIM: To establish innovational triangular phase diagrams for preparation of pharmaceutical microemulsion (ME) with low toxicity as a result of reducing the amount of the emulsifiers. METHODS: Lecithin and polyoxyethylene octyl phenyl ether (OP) were used as emulsifiers (E), absolute alcohol and n-octyl alcohol as assistant emulsifiers (A), ethyl oleate and olive oil as the oil phase (O). For the innovational triangular phase diagrams, lecithin-ethyl oleate-water and absolute alcohol (optimized ratio W/A = 0.6) system, and OP(olive oil and n-octyl alcohol (O/A = 0.34)-water system were used for preparation of the ME. While for the traditional triangular phase diagrams, OP and n-octyl alcohol (E/A = Km = 1.5)-olive oil-water system, lecithin and absolute alcohol (E/A = Km = 1.12)-ethyl oleate-water system were used. Then, the corresponding amounts of the emulsifiers used in both methods were compared. RESULTS: In the ME of lecithin systems by the innovational and the traditional methods, the amounts of emulsifier are 6%-28% and 28%-29.6%, respectively. In the ME of OP systems by the innovational and the traditional methods, the amounts of emulsifier are 23%-40% and 27.6%-49.8%, respectively. CONCLUSION: The method of innovational triangular phase diagram for preparation of ME is superior to the traditional method in finding out the lower amounts of emulsifiers for ME, and is a feasible method with guiding significance for preparing ME.
Assuntos
Emulsões/química , Preparações Farmacêuticas , Álcoois , Excipientes/química , Ácidos Oleicos , Azeite de Oliva , Fosfatidilcolinas , Óleos de Plantas , Tecnologia Farmacêutica/métodosRESUMO
Peripheral blood lymphocyte sister chromatid exchange(SCE) frequencies, serum folic acid(FA) levels were examined in 15 epileptic patients treated with carbamazepine(CBZ), and another 15 epileptic patients treated with CBZ and folic acid(FA). The untreated epileptic patients and the healthy subjects served as control. The results showed that SCE frequencies were significantly higher in CBZ Group, compared with CBZ plus FA Group and control(P < 0.01). Serum FA levels were lower in CBZ Group compared with healthy control(P < 0.01). It suggests that CBZ can induce the increase of SCE frequencies. Supplementation with FA may effectively prevent chromosome DNA damage induced by CBZ.
Assuntos
Anticonvulsivantes/uso terapêutico , Carbamazepina/uso terapêutico , Epilepsia Parcial Complexa/genética , Ácido Fólico/uso terapêutico , Troca de Cromátide Irmã , Adolescente , Criança , Epilepsia Parcial Complexa/sangue , Epilepsia Parcial Complexa/tratamento farmacológico , Feminino , Ácido Fólico/sangue , Humanos , MasculinoRESUMO
The effect of PIC-BE on the expression of mdr-1, bcl-2 and bax genes and their protein products (P-gp, Bcl-2 and Bax) was observed respectively in a multidrug resistance (MDR) cell variant K562/ADM. The results showed that PIC-BE could significantly inhibit the expression of mdr-1 and bcl-2 genes at both mRNA and protein levels in K562/ADM cell line, and the effect was dose- and time-dependent within limited range. Under same condition, although PIC-BE could increase the expression of Bax slightly, there was no statistically significant difference. These results suggest that the reversal of the MDR of K562/ADM cell line by PIC-BE may result from its effect on the expression of mdr-1, bcl-2 genes and their protein products.
Assuntos
Antineoplásicos/farmacologia , Resistência a Múltiplos Medicamentos/genética , Resistencia a Medicamentos Antineoplásicos/genética , Genes MDR , Genes bcl-2 , Extratos Vegetais/farmacologia , Sesquiterpenos , Membro 1 da Subfamília B de Cassetes de Ligação de ATP/biossíntese , Relação Dose-Resposta a Droga , Doxorrubicina/farmacologia , Expressão Gênica/efeitos dos fármacos , Humanos , Células K562/efeitos dos fármacos , Proteínas Proto-Oncogênicas/biossíntese , Proteínas Proto-Oncogênicas c-bcl-2/biossíntese , Proteína X Associada a bcl-2RESUMO
The enzymatic mechanism of a small ribosome-inactivating protein, gamma-momorcharin, purified from the seeds of Momordica charantia, has been characterized. By SDS-polyacrylamide and electrospray ionization mass spectrometry, its molecular weight was measured to be 11,500 daltons which is much lower than other RIPs known to date. It can inhibit the protein synthesis in the rabbit reticulocyte cell-free system with ID50 of 55 nM. When rat liver ribosome was incubated with gamma-momorcharin, a diagnostic RNA fragment appeared on the gel after rRNAs were treated with acid aniline. Sequencing of the RNA fragment indicates that the action site of gamma-momorcharin in 28S ribosomal RNA of rat liver is at a specific adenosine (position 4324), which is in a highly conserved loop of 28S rRNA.
Assuntos
N-Glicosil Hidrolases/metabolismo , Proteínas de Plantas/metabolismo , Plantas Medicinais/enzimologia , Inibidores da Síntese de Proteínas/metabolismo , RNA Ribossômico 28S/metabolismo , Proteínas Ribossômicas , Relação Dose-Resposta a Droga , N-Glicosil Hidrolases/farmacologia , Proteínas de Plantas/farmacologia , Biossíntese de Proteínas/efeitos dos fármacos , Inibidores da Síntese de Proteínas/farmacologia , Proteínas Inativadoras de Ribossomos , Ribossomos/efeitos dos fármacos , Sementes/química , Especificidade por SubstratoRESUMO
Two classes of nad9 transcripts are present at different abundances in the steady-state RNA pool of potato mitochondria. The 5'- and 3' termini of the transcripts were determined by primer extension and S1 nuclease protection analyses respectively. Using two primer pairs that will either specifically amplify the larger transcript or amplify both the larger and the smaller transcripts in RT-PCR analyses it was found that the larger nad9 transcripts are partially edited, while the smaller transcripts are fully edited. Both the larger and the smaller transcripts were found to be associated with mitochondrial polysomes. The polysome association was found to be sensitive to EDTA and puromycin treatment. Therefore, both fully and partially edited nad9 transcripts appear to be engaged in translation.
Assuntos
Proteínas Mitocondriais , NADH Desidrogenase/genética , Proteínas de Plantas/genética , Edição de RNA , RNA/genética , Sequência de Bases , Primers do DNA/química , Regulação da Expressão Gênica de Plantas , Dados de Sequência Molecular , Polirribossomos/metabolismo , RNA Mensageiro/genética , RNA Mitocondrial , Solanum tuberosumRESUMO
The effect of Shengmaisan (SMS) on 62 acute viral myocarditis patients and its peroxidation damage was studied. The results revealed that the activities of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) in blood were decreased and the content of malondialdehyde (MDA) in plasma was increased in acute viral myocarditis patients in comparison with the healthy controls (P < 0.001). 62 acute viral myocarditis patients were divided into two groups: SMS group and placebo group. After treatment, both SOD and GSH-Px activities were increased and the level of MDA decreased (P < 0.001) in SMS group, while those in placebo group were not changed (P < 0.05). The results suggested that the myocardial damage of viral myocarditis is closely related with lipid peroxidation SMS acts as an effective free radical scavenger and anti-lipid peroxidation drug. SMS could prevent the damage of myocardia and might be taken as one of the effective therapeutic methods in treatment of acute viral myocarditis.
Assuntos
Medicamentos de Ervas Chinesas/uso terapêutico , Sequestradores de Radicais Livres/uso terapêutico , Peroxidação de Lipídeos/efeitos dos fármacos , Miocardite/sangue , Viroses/sangue , Adolescente , Adulto , Idoso , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Miocardite/tratamento farmacológico , Miocardite/virologia , Método Simples-Cego , Viroses/tratamento farmacológicoRESUMO
The effect of Sheng Mai San (SMS) on the coronary heart disease (CHD) patients (30 angina pectoris and 68 acute myocardial infarction, AMI) and its peroxidation damage was studied. It was shown that the activities of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) in blood were decreased and the content of malondialdehyde (MDA) in plasma was increased in CHD patients in comparison with the healthy controls (P < 0.001). When SMS was orally administered in 38 AMI patients, both SOD and GSH-Px activities were increased and the level of MDA decreased (P < 0.05), and these changes were even more significant when SMS was further ingested for another two weeks (P < 0.001). At the same time, it was found that the changes of SOD, GSH-Px and MDA in the control group (30 AMI patients not taking SMS) were not significantly different (P > 0.05). It could be assumed that the pathogenesis of CHD is associated with free radical (FR) triggering a chain reaction of the lipid peroxidation, and that SMS is acting as an effective free radical scavenger, which would ameliorate the lipid peroxidation damage. Thus, SMS could be administered in the prevention and the treatment of CHD.