RESUMEN
Metergoline, a serotonin receptor antagonist, was evaluated for its antifungal activity against the opportunistic human fungal pathogen Candida krusei by a broth microdilution assay. The minimal inhibitory concentration and minimal fungicidal concentration of metergoline against C. krusei were 4 and 8 µg ml(-1) respectively. Significant synergism was found in combination of metergoline with amphotericin B (fractional inhibitory concentration index: 0.375-0.5) by a chequerboard assay. Metergoline also inhibited extracellular phospholipase secretion in a dose-dependent manner, which may be a possible action mechanism of metergoline on C. krusei.
Asunto(s)
Antifúngicos/farmacología , Candida/efectos de los fármacos , Metergolina/farmacología , Anfotericina B/farmacología , Sinergismo Farmacológico , Proteínas Fúngicas/antagonistas & inhibidores , Pruebas de Sensibilidad Microbiana , Viabilidad Microbiana/efectos de los fármacos , Fosfolipasas/antagonistas & inhibidoresAsunto(s)
Cesárea , Inhibidores de la Ciclooxigenasa 2/administración & dosificación , Dolor Postoperatorio/prevención & control , Pirazoles/administración & dosificación , Sulfonamidas/administración & dosificación , Analgesia Obstétrica/métodos , Celecoxib , Método Doble Ciego , Esquema de Medicación , Femenino , Humanos , Resultado del TratamientoRESUMEN
BACKGROUND AND PURPOSE: Ever since the discovery of photodynamic therapy, there has been a continuous search for more potent photosensitizers. Towards that end, we have synthesized a number of novel phthalocyanine derivatives. The unsymmetrical bisamino silicon(IV) phthalocyanine BAM-SiPc is one of the most potent compounds. In in vitro cell culture, it exhibits high phototoxicity against a number of cancer cell lines. EXPERIMENTAL APPROACH: In the present investigation, the in vivo effect of BAM-SiPc was studied in the tumour-bearing nude mice model. The biodistribution of BAM-SiPc was followed to evaluate its tumour selectivity and rate of clearance. The tumour volume in the hepatocarcinoma HepG2- and the colorectal adenocarcinoma HT29-bearing nude mice was measured after photodynamic therapy. The level of intrinsic toxicity induced was also investigated. Finally, the metabolism of BAM-SiPc in the 'normal' WRL68 liver cells and the hepatocarcinoma HepG2 cells was compared. KEY RESULTS: The results not only showed significant tumour regression of HepG2 and growth inhibition of HT29 in the tumour-bearing nude mice, but also no apparent hepatic or cardiac injury with the protocol used. Histological analyses showed that apoptosis was induced in the solid tumour. BAM-SiPc could be metabolized by WRL68 liver cells but not by the hepatocarcinoma HepG2 cells. Unfortunately, BAM-SiPc did not show any specific targeting towards the tumour tissue. CONCLUSIONS AND IMPLICATIONS: The efficiency of BAM-SiPc in inhibiting tumour growth makes it a good candidate for further evaluation. Enhancement of its uptake in tumour tissue by conjugation with biomolecules is currently under investigation.
Asunto(s)
Indoles/uso terapéutico , Neoplasias Experimentales/terapia , Compuestos de Organosilicio/uso terapéutico , Fotoquimioterapia , Fármacos Fotosensibilizantes/uso terapéutico , Animales , Línea Celular Tumoral , Células HT29 , Humanos , Etiquetado Corte-Fin in Situ , Técnicas In Vitro , Indoles/farmacocinética , Hígado/patología , Ratones , Ratones Desnudos , Trasplante de Neoplasias , Neoplasias Experimentales/metabolismo , Neoplasias Experimentales/patología , Compuestos de Organosilicio/farmacocinética , Fármacos Fotosensibilizantes/farmacocinética , Distribución TisularRESUMEN
BACKGROUND: Intrathecal morphine provides good analgesia after cesarean delivery but the side effects include nausea and vomiting. Low-dose droperidol (0.625 mg) combined with dexamethasone 4 mg is postulated to have an additive antiemetic effect with less side effects. We therefore compared single doses of dexamethasone and droperidol alone with a low-dose combination of the two, to prevent spinal morphine-induced nausea and vomiting after cesarean section. METHODS: In a double-blind study, 120 women undergoing elective cesarean section under spinal anesthesia (using 0.5% bupivacaine 10 mg and morphine 0.2 mg) were allocated randomly to receive dexamethasone 8 mg, droperidol 1.25 mg, dexamethasone 4 mg and droperidol 0.625 mg, or placebo, before the end of surgery. The incidences of nausea and vomiting, sedative score, pain score, and side effects were recorded. RESULTS: The incidence of nausea and vomiting within 6 h postoperatively was lower and incidence of no nausea and vomiting for 24 h postoperatively was significantly higher for the combination group compared to the placebo group and the dexamethasone only group. Sedation scores within 3 h postoperatively and incidence of restlessness for the combination group were significantly lower than in the droperidol only group. CONCLUSION: An additive antiemetic effect and no significant side effects were shown for the combination of dexamethasone 4 mg and droperidol 0.625 mg. This combination was more effective than either dexamethasone 8 mg or droperidol 1.25 mg alone in preventing nausea and vomiting after spinal anesthesia using 0.5% bupivacaine and morphine 0.2 mg.
Asunto(s)
Analgesia Obstétrica/métodos , Cesárea/métodos , Dexametasona/uso terapéutico , Droperidol/uso terapéutico , Morfina/efectos adversos , Náusea y Vómito Posoperatorios/prevención & control , Adulto , Analgésicos Opioides/efectos adversos , Antieméticos/uso terapéutico , Bupivacaína , Sedación Consciente/métodos , Método Doble Ciego , Sinergismo Farmacológico , Quimioterapia Combinada , Femenino , Humanos , Inyecciones Espinales , Morfina/administración & dosificación , Dimensión del Dolor/métodos , Náusea y Vómito Posoperatorios/inducido químicamente , Embarazo , Estudios ProspectivosRESUMEN
Antiquitin is a member of the aldehyde dehydrogenase superfamily. Sequence analyses indicate that the protein is highly conserved from plants to animals. The plant antiquitins are generally believed to play a role in osmoregulation and/or detoxification. The physiological functions of animal antiquitins remain largely elusive, their involvement in a number of human diseases has been implicated.
Asunto(s)
Aldehído Deshidrogenasa/fisiología , Proteínas de Plantas/fisiología , Equilibrio Hidroelectrolítico , Animales , Humanos , L-Aminoadipato-Semialdehído Deshidrogenasa , Datos de Secuencia Molecular , Proteínas/fisiologíaRESUMEN
Five trypsin inhibitors, with N-terminal sequences demonstrating homology to each other and exhibiting a molecular weight of 5100, 4800, 4400, 4100, and 3900, respectively, were isolated from Momordica cochinchinensis seeds with a protocol involving acid extraction, ion exchange chromatography on SP-Sepharose chromatography, and RP-HPLC on a C18 column. Specific inhibitory activity against trypsin was demonstrated by the trypsin isoinhibitors with Ki values ranging from 5.3 x 10(-8) to 1.8 x 10(-6) M. None of the isoinhibitors could be cleaved by trypsin.
Asunto(s)
Momordica/química , Proteínas de Plantas/química , Plantas Medicinales/química , Semillas/química , Inhibidores de Tripsina/química , Secuencia de Aminoácidos , Cromatografía Líquida de Alta Presión , Datos de Secuencia MolecularRESUMEN
Three preparations of type 1 ribosome inactivating proteins (RIPs), namely, agrostin, saporin, and luffin, were subjected to affinity chromatography on Red Sepharose and eluted with a linear concentration gradient of NaCl in 10 mM Tris-HCl buffer (pH 7.4). The eluate was assayed for ability to inhibit translation in a cell-free rabbit reticulocyte lysate system which measures RIP activity, and for ability to hydrolyze yeast transfer RNA which measures RNase activity. It was found that, in all three RIP preparations, the peak of RIP activity, which coincided with the peak of absorbance at 280 nm, was eluted earlier than the peak of RNase activity. It appears that RNase is a possible contaminant of ribosome inactivating protein preparations and that this contamination can be minimized by using Red Sepharose.
Asunto(s)
Cromatografía de Afinidad/métodos , Proteínas de Plantas/aislamiento & purificación , Ribonucleasas/aislamiento & purificación , Animales , Inmunotoxinas/aislamiento & purificación , Inmunotoxinas/metabolismo , Inmunotoxinas/farmacología , N-Glicosil Hidrolasas/aislamiento & purificación , N-Glicosil Hidrolasas/metabolismo , N-Glicosil Hidrolasas/farmacología , Proteínas de Plantas/metabolismo , Proteínas de Plantas/farmacología , Plantas/química , Biosíntesis de Proteínas/efectos de los fármacos , Inhibidores de la Síntesis de la Proteína/farmacología , ARN de Transferencia/metabolismo , Conejos , Ribonucleasas/metabolismo , Proteínas Inactivadoras de Ribosomas Tipo 1 , Saporinas , Semillas/química , Sefarosa/análogos & derivadosRESUMEN
Syrian golden hamster (Mesocricetus auratus) is extraordinary among laboratory rodents in its ability to drink alcohol. After being given a free choice between 15% ethanol and water for 5 days, both male and female hamsters derived at least 85% of the fluid intake from the ethanol solution. Analysis of the alcohol-metabolizing enzymes in alcohol-naïve hamsters showed that the male had a higher activity of 57%, 58% and 34% in stomach alcohol dehydrogenase, liver cytochrome P450 1A2 and liver aldehyde dehydrogenase, respectively, compared with the female. The activity of lung angiotensin-converting enzyme, which influence fluid intake, was twofold higher in the male. After 4 weeks of ethanol consumption, the activities of the hepatic alcohol-metabolizing enzymes remained unchanged except cytochrome P450 2E1 which increased 42% and 88% in male and female hamsters, respectively. A reduction of approximately 80% in the activity of cytochrome P450 1A2 was observed in both genders. The activities of several other cytochrome P450 enzymes were also decreased. Although ethanol consumption did not increase plasma aminotransferase levels, it caused a significant increase in liver weight in female, but not male hamsters.
Asunto(s)
Consumo de Bebidas Alcohólicas/metabolismo , Consumo de Bebidas Alcohólicas/fisiopatología , Hígado/enzimología , Mesocricetus/metabolismo , Caracteres Sexuales , Alcohol Deshidrogenasa/metabolismo , Aldehído Deshidrogenasa/metabolismo , Animales , Cricetinae , Sistema Enzimático del Citocromo P-450/metabolismo , Ingestión de Líquidos/fisiología , Activación Enzimática/fisiología , Femenino , Hígado/patología , Pulmón/enzimología , Masculino , Tamaño de los Órganos/fisiología , Peptidil-Dipeptidasa A/metabolismoRESUMEN
The aqueous and methanol extracts of twenty herbs traditionally used in Chinese medicine were screened for anti-HIV-1 integrase activity in a non-radioactive ELISA-based HIV-1 integrase assay. The screening was performed at an herb extract concentration of 50 microg/ml. It was found that most of the aqueous and methanol herb extracts could elicit strong inhibition of HIV-I integrase activity. The inhibition was most likely due to tannins or polyphenolics in the herb extracts. In most of the herb extracts, 40-80% of the anti-HIV-1 integrase activity could be removed after passing through a minicolumn of polyamide resin. After removal of polyphenolic compounds, the methanol extract of Paeonia suffruticosa still exerted potent inhibition of HIV-1 integrase (EC50 = 15 microg/ml) and the aqueous extract of Prunella vulgaris caused moderate inhibition (EC50 = 45 microg/ml). The results support the view that herbs represent a rich source of anti-HIV compounds.
Asunto(s)
Medicamentos Herbarios Chinos/farmacología , Inhibidores de Integrasa VIH/farmacología , Integrasa de VIH/metabolismo , Ensayo de Inmunoadsorción Enzimática , Humanos , Metanol , Fenoles/farmacología , Extractos Vegetales/farmacología , Solventes , AguaRESUMEN
The aqueous and methanol extracts of thirty-one herbs traditionally used as anti-fever remedies in China were screened for their in vitro inhibition on human immunodeficiency virus type-1 protease (HIV-1 PR). The activity of recombinant HIV-1 protease was determined by sequence-specific cleavage at the Tyr-Pro bond of the fluorogenic substrate (Arg-Glu(EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)- Arg) or by HPLC anaylsis of the cleavage products after incubation of the enzyme with a synthetic peptide substrate (Acetyl-Ser-Gln-Asn-Tyr-Pro-Val-Val-amide). Among the herbal extracts examined, the aqueous extracts of Prunella vulgaris and Scutellaria baicalensis and the methanol extracts of Woodwardia unigemmata, Paeonica suffruticosa and Spatholobus suberectus elicited significant inhibition (>90%) at a concentration of 200 microg/ml.
Asunto(s)
Inhibidores de la Proteasa del VIH/farmacología , Proteasa del VIH/metabolismo , Medicina Tradicional China , Fitoterapia , Extractos Vegetales/farmacología , VIH-1/enzimología , Humanos , Cinética , Magnoliopsida , Metanol , Proteínas Recombinantes/antagonistas & inhibidores , AguaRESUMEN
Epidemiological studies have suggested that repeated weight cycling over time may increase the risk of coronary heart disease. The mechanism involved remains poorly understood, but the change in lipid metabolism during weight cycling has been offered as a possible explanation. The present study investigated the effect of weight cycling on the size and fatty acid composition of rat fat pads as well as serum cholesterol, triglyceride, glucose, insulin, and glucagon in rats. Two consecutive weight cycles were induced by 40% energy restriction followed by ad libitum refeeding of either a moderate-fat (MF; 22% energy) or a high-fat (HF; 45% energy) diet. The lipogenic enzymes, including fatty acid synthase, acetyl-CoA carboxylase, malic enzyme, pyruvate kinase, and lipoprotein lipase in the weight-cycled (WC) rats fed only the HF diet, yielded an overshoot of activities at the end of two weight cycles. These changes were accompanied by an 80% increase in the size of the adipocyte and a 40-50% increase in the size of perirenal and epididymal fat tissues in HF-WC rats. Regardless of whether the rats were fed the HF or MF diet, all WC rats showed a gradual reduction in linoleic and alpha-linolenic acid and an increase in palmitic, palmitoleic, and stearic acid in total body lipid. It is concluded that weight cycling in rats may promote body fatness if an HF diet is consumed and can significantly alter whole body fatty acid balance irrespective of whether they consumed an MF or HF diet. Most importantly, the weight cycling led to an overshoot or fluctuation of serum cholesterol, triglyceride, glucose, insulin, and glucagon. If weight cycling is associated with an increased risk of cardiovascular disease, then, part of the mechanism may involve the changes in these risk factors.
Asunto(s)
Peso Corporal/fisiología , Metabolismo Energético/fisiología , Ácidos Grasos/metabolismo , Acetil-CoA Carboxilasa/metabolismo , Adipocitos/citología , Adipocitos/enzimología , Tejido Adiposo/citología , Tejido Adiposo/enzimología , Animales , Glucemia , Recuento de Células , Colesterol/sangre , Grasas de la Dieta/farmacocinética , Ingestión de Alimentos/fisiología , Ayuno/fisiología , Ácido Graso Sintasas/metabolismo , Ácidos Grasos/análisis , Conducta Alimentaria/fisiología , Glucagón/sangre , Insulina/sangre , Lipoproteína Lipasa/metabolismo , Malato Deshidrogenasa/metabolismo , Masculino , Piruvato Quinasa/metabolismo , Ratas , Ratas Sprague-Dawley , Triglicéridos/sangre , Ácido alfa-Linolénico/farmacocinéticaRESUMEN
The ribosome inactivating proteins (RIPs) are a group of proteins that are able to inactivate eukaryotic protein synthesis by attacking the 28S ribosomal RNA. Recent studies have shown that some RIPs possess strong anti-human immunodeficiency virus (HIV) activity. In this study, several common plant RIPs including agrostin, gelonin, luffin, alpha-momorcharin, beta-momorcharin, saporin and trichosanthin were examined for the ability to interfere with HIV-1 replication in a variety of mechanistic assays in vitro. These assays included the CD4/gp120 interaction assay, HIV-1 reverse transcriptase (RT) assay, HIV-1 protease assay and HIV-1 integrase assay. At the concentration of 100 nM, all RIPs appeared to enhance the CD4/gp120 interaction by about 50%. These RIPs exhibited a very weak suppressive effect on HIV-1 RT and on HIV-1 protease. In contrast, with the exception of agrostin, all the RIPs tested could strongly inhibit HIV-1 integrase, the extent of inhibition ranging from 26.1 to 96.3% in an ELISA-based assay. Two RIPs, saporin and luffin, which licited over 90% inhibition in the ELISA-based assay, were further characterized in a radiometric assay. Both of these two RIPs evoked a strong dose-dependent inhibition in the 3'-end processing and strand-transfer activities of integrase. The results from this study suggest that the anti-HIV property of RIPs may be due to inhibition of HIV-1 integrase.
Asunto(s)
Inhibidores de Integrasa VIH/farmacología , Integrasa de VIH/metabolismo , VIH-1/efectos de los fármacos , Inmunotoxinas , N-Glicosil Hidrolasas , Proteínas de Plantas/farmacología , Proteínas Ribosómicas , Fármacos Anti-VIH/farmacología , Antígenos CD4/metabolismo , Proteína gp120 de Envoltorio del VIH/metabolismo , Proteasa del VIH/metabolismo , Inhibidores de la Proteasa del VIH/farmacología , Transcriptasa Inversa del VIH/antagonistas & inhibidores , Transcriptasa Inversa del VIH/metabolismo , VIH-1/enzimología , VIH-1/fisiología , Concentración 50 Inhibidora , Plantas/química , Unión Proteica/efectos de los fármacos , Proteínas Inactivadoras de Ribosomas , Proteínas Inactivadoras de Ribosomas Tipo 1 , Ribosomas/efectos de los fármacos , Ribosomas/metabolismo , Saporinas , Tricosantina/farmacología , Replicación Viral/efectos de los fármacosRESUMEN
Alpha- and beta-momorcharins are ribosome-inactivating proteins present in the seeds of the bitter gourd (Momordica charantia). Both of them possess ribonuclease activity which may account for some of their biological properties. However, the activity is weak and hence it is important to confirm that the ribonuclease activity observed is not due to any contamination. To this end, the ribonuclease from the seeds of M. charantia (RNase-MC) was purified and compared with the ribonuclease activity of the momorcharins. Purification was achieved by ion-exchange chromatographies on DEAE-cellulose, SP-Sepharose and Mono-S. RNase-MC had a molecular mass of 22 kDa. It acted on tRNA to release acid-soluble UV-absorbing species with a pH optimum around 6.0-6.5. When polyhomoribonucleotides were used as substrates, it was found that RNase-MC acted preferentially on polyU but exerted much weaker activity on polyC, polyG and polyA. Chromatographic analysis of the reaction product indicated that mono- and oligo-ribonucleotides, but not free base, were generated from polyU, suggesting that the enzymatic action involved ribonucleolytic cleavage. RNase-MC exhibited a much more potent (at least 1000-fold higher) ribonuclease activity than alpha- and beta-momorcharins. RNase-MC, alpha-momorcharin and beta-momorcharin were separable on Mono-S, indicating that the ribonuclease activities present in the three proteins were distinct entities.
Asunto(s)
Cucurbitaceae/química , Proteínas de Plantas/metabolismo , Ribonucleasas/metabolismo , Proteínas Ribosómicas , Ribosomas/metabolismo , Cromatografía en Agarosa , Proteínas de Plantas/química , Proteínas de Plantas/aislamiento & purificación , ARN de Transferencia/metabolismo , Ribonucleasas/química , Ribonucleasas/aislamiento & purificación , Ribonucleótidos/metabolismo , Proteínas Inactivadoras de Ribosomas , Semillas/químicaRESUMEN
A trypsin inhibitor, MCCTI-1, with a molecular weight of 3479 Da as determined by mass spectrometry, was isolated from Momordica cochinchinensis seeds with a procedure involving extraction with 5% acetic acid, ammonium sulfate precipitation, ion exchange chromatography on CM-Sepharose and reverse-phase high performance liquid chromatography. The sequence of its first 13 N-terminal amino acid residues was ILKKCRRDSDCPG which was about 85% identical with the sequence of trypsin inhibitor MCTI-1 from Momordica charantia Linn. When compared with the sequences of most other squash family trypsin inhibitors, the sequence of MCCTI-1 was characterized by the deletion of a pentapeptide from the N-terminus. Trypsin inhibitors also existed in seeds of some hitherto uninvestigated Cucurbitaceae species.
Asunto(s)
Medicamentos Herbarios Chinos/química , Inhibidores de Tripsina/química , Secuencia de Aminoácidos , Cromatografía Líquida de Alta Presión , Cromatografía por Intercambio Iónico , Cucurbitaceae/química , Espectrometría de Masas , Datos de Secuencia Molecular , Momordica , Fragmentos de Péptidos/química , Proteínas de Plantas , Semillas/química , Homología de Secuencia de Aminoácido , Inhibidores de Tripsina/farmacologíaRESUMEN
These studies were designed to test the hypolipidemic activity of green tea epicatechins (GTE) isolated from jasmine green tea. In Experiment 1, three groups of hamsters were given a semisynthetic diet containing 200 g lard/kg and 1 g cholesterol/kg for 4 wk. The control group received distilled water, and the other two groups received either 15 g/L green tea water extract (GTWE) or 5.0 g/L GTE solution. Both the GTWE and GTE groups had lower concentrations of serum total cholesterol (TC) and triacylglycerols (TG) than the controls (P < 0.05). In Experiment 2, four groups of hamsters received tap water as the drinking fluid, but they were given the same high fat and cholesterol diet supplemented with 0 (control), 1.1, 3.4 or 5.7 g GTE/kg diet. The hypolipidemic effect of jasmine GTE was dose dependent. In Experiment 3, the time-course of changes in serum TC and TG was monitored in hamsters given the high fat diet supplemented with 5.7 g GTE/kg in comparison with that of controls. The hypolipidemic effects of dietary GTE were evident after feeding for 2 wk. Dietary supplementation of GTE did not affect liver fatty acid synthase. However, GTE-supplemented hamsters had higher fecal excretions of total fatty acids, neutral sterols and acidic sterols compared with the control group. In Experiment 4, hamsters were fed nonpurified diet; the control group drank distilled water, and the GTE group drank distilled water containing 5.0 g GTE/L. No differences in activities of 3-hydroxy-3-methyl glutaryl coenzyme A reductase and intestinal acyl CoA:cholesterol acyltransferase were observed. This study suggests that the hypolipidemic activity of GTE is not due to inhibition of synthesis of cholesterol or fatty acid but is most likely mediated by its influence on absorption of dietary fat and cholesterol.
Asunto(s)
Catequina/análogos & derivados , Dieta con Restricción de Grasas , Hipolipemiantes/farmacología , Lípidos/sangre , Té/química , Animales , Colesterol/sangre , Cricetinae , Relación Dosis-Respuesta a Droga , Ácidos Grasos/análisis , Heces/química , Masculino , Mesocricetus , Valores de Referencia , Esteroles/análisis , Factores de Tiempo , Triglicéridos/sangreRESUMEN
Estrogen can be hydroxylated at both 2- and 16alpha-positions. These two reactions are mutually exclusive. The 2-hydroxylated estrogen is relatively inactive compared with the 16alpha-derivative; hence, one approach in anti-estrogenic therapy is to look for drugs that can induce the 2-hydroxylation pathway. In the present study, using Balb/c and C57B/6 mice as the animal models, the induction effect of several isoprenyl compounds on estradiol-2-hydroxylase and ethoxyresorufin-O-deethylase activities was studied. The compounds examined included 2'- and 3'-methylbutadienyl-indoles and their respective acid condensation products, isopropyl indolocarbazole and yuehchukene; positional isomers of indole carbinols and carboxyaldehydes, as well as 3-methylcholanthrene, the prototype inducer of cytochrome P450 1A1. Our results demonstrated that while all of them were capable of inducing cytochrome P450 1A1-mediated ethoxyresorufin-O-deethylase activity, only the 3' isomers could induce estradiol-2-hydroxylase activity. The induction of these two activities did not show any direct correlation, suggesting that cytochrome P450 1A1 was not the same enzyme catalyzing both ethoxyresorufin-O-deethylation and estradiol-2-hydroxylation. Nevertheless, both inductions were mediated by the aryl hydrocarbon receptor. Among the compounds tested, yuehchukene showed competitive binding to estrogen receptor. This, together with the induction of estradiol-2-hydroxylase activity, may account for the anti-estrogenic effect of yuehchukene.
Asunto(s)
Alcaloides/farmacología , Anticonceptivos Poscoito/farmacología , Citocromo P-450 CYP1A1/metabolismo , Sistema Enzimático del Citocromo P-450/metabolismo , Indoles/farmacología , Esteroide Hidroxilasas/metabolismo , Animales , Inducción Enzimática , Antagonistas de Estrógenos/farmacología , Femenino , Ratones , Ratones Endogámicos BALB C , Receptores de Hidrocarburo de Aril/efectos de los fármacosRESUMEN
An improved method for the removal of polyphenolic compounds from aqueous extracts of plants is presented. The method removes > 99% polyphenolic compounds from 5 mg of extract. The method is simple, robust and reproducible. We examined the removal of polyphenolics from 5 different aqueous extracts of Chinese medicinal herbs.
Asunto(s)
Cromatografía , Medicamentos Herbarios Chinos/química , Flavonoides , Nylons , Fenoles/aislamiento & purificación , Polímeros/aislamiento & purificación , Taninos/aislamiento & purificación , Centrifugación , Taninos Hidrolizables/aislamiento & purificación , PolifenolesRESUMEN
Two chymotrypsins were purified from the hepatopancreas of grass carp (Ctenopharyngodon idellus) by chromatographies on phenyl-Sepharose and Q-Sepharose. The molecular weights of chymotrypsins I and II were 28 and 27 kDa, respectively. The two chymotrypsins showed similar susceptibility to inhibitions by phenylmethylsulfonyl fluoride and soybean trypsin inhibitor, but differed in their response to tosyl-L-phenylalanine chloromethyl ketone and aprotinin in which chymotrypsin I was more resistant. Chymotrypsin I was a less typical chymotrypsin and exhibited lower catalytic efficiency with the chymotrypsin-specific ester and amide substrates, when compared with chymotrypsin II. For both chymotrypsins, optimal activity was detected in the pH range 7.0-8.5.