RESUMEN
OBJECTIVE: Increasing research suggested that Cimicifugae rhizoma might be protective against osteoporosis. In this study, we investigated the effects of three cycloartane-type triterpenoids isolated from Cimicifugae rhizoma, cimicidol-3-O-beta-D-xyloside (1), cimicidanol-3-O-beta-D-xyloside (2) and acetylacteol-3-O-beta-d-xyloside (3) on bone resorption in vitro and bone loss in ovariectomized (OVX) mice. METHODS: The activities of the tested compounds on bone resorption were evaluated using three assays, neonatal mouse parietal bone organ culture, osteoclast-like cells (OCLs) formation and pit formation. The effects on bone mineral density (BMD) and uterine weight were examined using OVX mice. Using LC-MS/MS method, the serum concentrations of the triterpenoids were measured in mice serum collected at 0.5, 1, 3, 6 and 12h following its oral administration. RESULTS: All of the tested compounds exerted the inhibitory effects on bone resorption in bone organ culture, suppressed both of the formation and the resorbing activity of OCLs. Furthermore, a synergistic effect was observed among those compounds. In vivo studies revealed that compounds 1-3 and the mixture of compounds 1-3 prevented the bone loss in OVX mice without affecting uterine weight, and each compound was detected in the mice serum after single oral administration. CONCLUSIONS: The triterpenoids exerted the inhibitory effects on osteoclastic bone resorption through the suppression of both OCLs formation and the resorbing activity of OCLs, and also showed a significant protective effect on BMD in OVX mice. The present results might provide a new pharmacological potential for the treatment of osteoporosis.
Asunto(s)
Resorción Ósea/tratamiento farmacológico , Cimicifuga/química , Medicamentos Herbarios Chinos/farmacología , Osteoclastos/efectos de los fármacos , Osteoporosis/tratamiento farmacológico , Ovariectomía/efectos adversos , Fitoterapia , Animales , Índice de Masa Corporal , Resorción Ósea/etiología , Cimicifuga/clasificación , Medicamentos Herbarios Chinos/química , Femenino , Ratones , Osteoporosis/etiología , Osteoporosis/prevención & control , Fitoterapia/métodos , Relación Estructura-Actividad , Resultado del Tratamiento , Triterpenos/química , Triterpenos/aislamiento & purificaciónRESUMEN
The gene encoding the alpha isoform of rat Ca2+/calmodulin-dependent protein kinase II was cloned, and its exon-intron organization was analyzed. The coding region of cDNA consists of 18 exons spanning more than 50 kilobase pairs. Each of the discrete functional units, such as the ATP-binding site, the autophosphorylation site responsible for Ca2+-independent activity, the calmodulin-binding site, and link structure is encoded by a single exon. The largest and smallest exons consist of 229 and 41 base pairs, respectively. All splice junction sequences flanking the introns conform to the consensus splice junction sequence and the GT-AG splice rule.
Asunto(s)
Proteínas Quinasas Dependientes de Calcio-Calmodulina/genética , Clonación Molecular , Exones , Intrones , Adenosina Trifosfato/metabolismo , Animales , Composición de Base , Secuencia de Bases , Sitios de Unión , Proteína Quinasa Tipo 2 Dependiente de Calcio Calmodulina , Secuencia de Consenso , ADN Complementario/genética , Biblioteca Genómica , Isoenzimas/genética , Fosforilación , Reacción en Cadena de la Polimerasa , Ratas , Análisis de Secuencia de ADNRESUMEN
We investigated the effect of tetrahydroswertianolin (THS), a hepatoprotective agent from Swertia japonica, on tumor necrosis factor-alpha (TNF-alpha)-dependent hepatic apoptosis induced by D-galactosamine (D-GalN) (700 mg/kg, i.p.) and lipopolysaccharide (LPS) (10 microg/kg, i.p.) in mice. Apoptotic symptoms were observed at the initial stage of liver damage. By 5 hr after intoxication, hepatic DNA fragmentation had risen to 2123%, with the value in untreated mice set at 100%, without a significant elevation of serum alanine transaminase (ALT) activity. There was a parallel increase in hepatocytes undergoing chromatin condensation and apoptotic body formation. By 8 hr after intoxication, serum ALT activity had risen to 3707 U/L. Pretreatment with THS (50 mg/kg, p.o.) at 18 and 2 hr before intoxication significantly reduced DNA fragmentation to 821% of that in untreated mice and prevented the emergence of chromatin condensation and apoptotic body formation. A significant and dose-dependent reduction in serum ALT activity at 8 hr also was observed with THS pretreatment. These effects of THS were different from those observed from pretreatment with glycyrrhizin (GCR), which is a clinically used hepatoprotective agent with membrane-stabilizing activity. GCR pretreatment (100 mg/kg, p.o.) did not inhibit hepatic DNA fragmentation (1588% of untreated mice), although this compound significantly protected against serum ALT elevation (1463 U/L). These data suggest that an inhibitory effect on the progression of hepatic apoptosis prior to liver injury may be involved in the hepatoprotective mechanisms of THS, whereas it appears that GCR affects the processes after apoptosis. In a separate experiment, we found that the concentration of serum TNF-alpha rose to 2016 pg/mL at 1 hr after intoxication of mice with D-GalN and LPS, but this increase was suppressed by THS pretreatment (10, 50, or 200 mg/kg, p.o.) to 716, 454, or 406 pg/mL, respectively. Further study with a reverse transcriptase-polymerase chain reaction method showed that THS blocked TNF-alpha production at the transcriptional level. Because TNF-alpha is a critical mediator to elicit apoptosis in this model, the property of suppressing TNF-alpha production may be of prime importance for THS inhibition of hepatic apoptosis.
Asunto(s)
Apoptosis/efectos de los fármacos , Glucósidos/farmacología , Iridoides , Hepatopatías/patología , Sustancias Protectoras/farmacología , Factor de Necrosis Tumoral alfa/fisiología , Análisis de Varianza , Animales , Enfermedad Hepática Inducida por Sustancias y Drogas , Fragmentación del ADN/efectos de los fármacos , Ensayo de Inmunoadsorción Enzimática , Galactosamina/farmacología , Glucósidos/uso terapéutico , Glucósidos Iridoides , Lipopolisacáridos/farmacología , Hepatopatías/prevención & control , Masculino , Ratones , Sustancias Protectoras/uso terapéutico , Factor de Necrosis Tumoral alfa/antagonistas & inhibidoresRESUMEN
Woodfruticosin (woodfordin C) (WFC), a new inhibitor of DNA topoisomerase II (topo-II), was isolated from methanol extract of Woodfordia fruticosa Kurz (Lythraceae) and studied for in vitro and in vivo antitumor activities in comparison with Adriamycin (ADR) and etoposide (ETP), well known inhibitors of topo-II. The inhibitory activity against DNA topo-II shown by WFC was much stronger than that shown by ETP or ADR. WFC inhibited strongly intracellular DNA synthesis but not RNA and protein synthesis. On the other hand, WFC had a weaker growth inhibitory activity against various human tumor cells than ETP or ADR, but it showed remarkable activity against PC-1 cells and moderate activity against MKN45 and KB cells. Furthermore, WFC had in vivo growth inhibitory activity against s.c. inoculated colon38. These results indicate that the mechanism by which WFC exhibits antitumor activity may be through inhibition of topo-II.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Taninos Hidrolizables , Taninos/farmacología , Inhibidores de Topoisomerasa II , Animales , Muerte Celular , Doxorrubicina/farmacología , Etopósido/farmacología , Células HeLa/efectos de los fármacos , Humanos , Leucemia P388/tratamiento farmacológico , Ratones , Trasplante de NeoplasiasRESUMEN
One hundred forty-two kinds of traditional medicines, which have been historically used in China, Indonesia, and Japan, were examined for the antiviral activity of their hot water (HW) extracts against herpes simplex virus type 1 (HSV-1), poliovirus type 1, and measles virus by plaque reduction assay. Thirty-two, 55, and 30 HW-extracts of them showed anti-HSV-1, antipoliovirus, and anti-measles virus activities, respectively. Among the 32 HW-extracts with anti-HSV-1 activity, 3 HW-extracts had anti-HSV-1 activity alone and the others showed anti-HSV-1 activity with anti-poliovirus and/or anti-measles virus activities. The 32 HW-extracts were further examined for their therapeutic efficacies of HSV-1 infection in mice. The mice were infected cutaneously with HSV-1 and HW-extracts were orally administered three times daily. Twelve HW-extracts, currently used for the treatment of various diseases other than viral infection, were found to be significantly effective in limiting the development of skin lesions and/or in prolonging the mean survival times of HSV-1-infected mice. These results suggested that 12 of 142 HW-extracts that exhibited therapeutic efficacy in an animal infection model were possible candidates for anti-HSV-1 traditional medicine.
Asunto(s)
Antivirales/uso terapéutico , Herpes Simple/tratamiento farmacológico , Medicina Tradicional de Asia Oriental , Extractos Vegetales/uso terapéutico , Animales , Antivirales/farmacología , Evaluación Preclínica de Medicamentos , Femenino , Herpesvirus Humano 1/efectos de los fármacos , Virus del Sarampión/efectos de los fármacos , Ratones , Ratones Endogámicos BALB C , Extractos Vegetales/farmacología , Poliovirus/efectos de los fármacos , Células Vero , Ensayo de Placa ViralRESUMEN
Traditional herbal medicines have been safely used for the treatment of various human diseases since ancient China. We selected 10 herbal extracts with therapeutic antiherpes simplex virus type 1 (HSV-1) activity. Among these, Geum japonicum Thunb., Rhus javanica L., Syzygium aromaticum (L.) Merr. et Perry, or Terminalia chebula Retzus showed a stronger anti-HSV-1 activity in combination with acyclovir than the other herbal extracts in vitro. When acyclovir and/or a herbal extract were orally administered at doses corresponding to human use, each of the 4 combinations significantly limited the development of skin lesions and/or prolonged the mean survival times of infected mice compared with both acyclovir and the herbal extract alone (P < 0.01 or 0.05). These combinations were not toxic to mice. They reduced virus yields in the brain and skin more strongly than acyclovir alone and exhibited stronger anti-HSV-1 activity in the brain than in the skin, in contrast to acyclovir treatment by itself. Combinations of acyclovir with historically used herbal medicines showed strong combined therapeutic anti-HSV-1 activity in mice, especially reduction of virus yield in the brain.
Asunto(s)
Aciclovir/uso terapéutico , Medicamentos Herbarios Chinos/uso terapéutico , Herpes Simple/tratamiento farmacológico , Herpesvirus Humano 1/efectos de los fármacos , Aciclovir/toxicidad , Animales , Chlorocebus aethiops , Quimioterapia Combinada , Medicamentos Herbarios Chinos/toxicidad , Femenino , Herpesvirus Humano 1/crecimiento & desarrollo , Humanos , Ratones , Ratones Endogámicos BALB C , Células Vero , Ensayo de Placa ViralRESUMEN
[formula: see text] Staminolactones A (1) and B (2) and norstaminol A (3), three highly oxygenated staminane-type diterpenes having mild cytotoxic activities against highly liver-metastatic colon 26-L5 carcinoma cells, were isolated from the aerial part of the Vietnamese medicinal plant Orthosiphon stamineus (Lamiaceae). Their structures were elucidated on the basis of the extensive spectral analyses.
Asunto(s)
Antineoplásicos/química , Diterpenos/química , Lamiaceae/química , Antineoplásicos/farmacología , Neoplasias del Colon/patología , Diterpenos/farmacología , Neoplasias Hepáticas/patología , Neoplasias Hepáticas/secundario , Estructura Molecular , Oxígeno/química , Análisis Espectral , Células Tumorales CultivadasRESUMEN
[formula: see text] Epicalyxin F (1) and calyxin I (2), two novel diarylheptanoids, were isolated from a residual fraction of an EtOH extract of Alpinia blepharocalyx. Calyxin I (2) represented a new carbon skeleton, and epicalyxin F (1) possessed potent antiproliferative activity toward HT-1080 fibrosarcoma and colon 26-L5 carcinoma with ED50 values of 1.71 and 0.89 microM, respectively.
Asunto(s)
Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Diarilheptanoides , Plantas Medicinales/química , Piranos/aislamiento & purificación , China , Ensayos de Selección de Medicamentos Antitumorales , Medicamentos Herbarios Chinos/química , Humanos , Espectroscopía de Resonancia Magnética , Semillas/química , Estereoisomerismo , Células Tumorales CultivadasRESUMEN
Nitric oxide (NO) is one of the pro-inflammatory molecules. Some phenylethanoids have been previously shown to possess anti-inflammatory effects. Seven phenylethanoids from the stems of Cistanche deserticola, viz. isoacteoside, tubuloside B, acteoside, 2'-O-acetylacteoside, echinacoside, cistanoside A and tubuloside A, were tested for their effect on NO radical generation by activated murine macrophages. At the concentration of 100-200 microM, all the phenylethanoids reduced (6.3-62.3%) nitrite accumulation in lipopolysaccharide (0.1 microgram/ml)-stimulated J774.1 cells. At 200 microM, they inhibited by 32.2-72.4% nitrite accumulation induced by lipopolysaccharide (0.1 microgram/ml)/interferon-gamma (100 U/ml) in mouse peritoneal exudate macrophages. However, these compounds did not affect the expression of inducible nitric oxide (iNOS) mRNA, the iNOS protein level, or the iNOS activity in lipopolysaccharide-stimulated J774.1 cells. Instead, they showed a clear scavenging effect (6.9-43.9%) at the low concentrations of 2-10 microM of about 12 microM nitrite generated from an NO donor, 1-propanamine-3-hydroxy-2-nitroso-1-propylhydrazino (PAPA NONOate). These results indicate that the phenylethanoids have NO radical-scavenging activity, which possibly contributes to their anti-inflammatory effects.
Asunto(s)
Antiinflamatorios no Esteroideos/farmacología , Flavonoides , Depuradores de Radicales Libres/farmacología , Macrófagos/metabolismo , Óxido Nítrico/antagonistas & inhibidores , Fenoles/farmacología , Plantas Medicinales , Polímeros/farmacología , Animales , Línea Celular , Concentración de Iones de Hidrógeno , Lipopolisacáridos/farmacología , Activación de Macrófagos , Masculino , Ratones , Ratones Endogámicos ICR , Óxido Nítrico Sintasa/antagonistas & inhibidores , Óxido Nítrico Sintasa/genética , Óxido Nítrico Sintasa de Tipo II , Polifenoles , ARN Mensajero/análisisRESUMEN
Three new phenylethanoid glycoside, named scrosides A-C and a new iridoid glycosides, named picroside IV, have been isolated from the underground parts of Picrorhiza scrophulariiflora, together with 11 known compounds. Their structures were elucidated by the means of 2D NMR spectroscopy and chemical methods.
Asunto(s)
Cinamatos/aislamiento & purificación , Disacáridos/aislamiento & purificación , Glucósidos/aislamiento & purificación , Glicósidos , Plantas Medicinales/química , Trisacáridos/aislamiento & purificación , Conformación de Carbohidratos , Secuencia de Carbohidratos , Cinamatos/química , Disacáridos/química , Glucósidos/química , Glucósidos Iridoides , Datos de Secuencia Molecular , Análisis Espectral , Trisacáridos/químicaRESUMEN
The lupane-triterpene glycosides, bourneioside A and bourneioside B, and two known saponins were isolated from Lonicera bournei Hemsl. The structures of bourneioside A and B were elucidated as 3-O-beta-D-glucopyranosyl-23-hydroxy-lup-20(29)-en-28-oic acid-28-O-beta-D-glucopyranosyl ester and 3-O-beta-D-glucopyranosyl-23-hydroxy-lup-20(29)-en-28-oic acid-28-O-[beta-D-glucopyranosyl-(1 --> 6)-beta-D-glucopyranosyl] ester, respectively, on the basis of spectral data and chemical evidence.
Asunto(s)
Glucósidos/aislamiento & purificación , Magnoliopsida/química , Triterpenos/aislamiento & purificación , Glucósidos/química , Espectroscopía de Resonancia Magnética , Estructura Molecular , Espectrometría de Masa Bombardeada por Átomos Veloces , Triterpenos/químicaRESUMEN
We assessed the effect of acteoside, a naturally occurring antioxidative phenylethanoid, on hepatic apoptosis and the subsequent liver failure induced by D-Galactosamine (D-GalN) and lipopolysaccharide (LPS). A co-administration of D-GalN (700 mg/kg) and LPS (35 microg/kg) to mice evoked typical hepatic apoptosis characterized by DNA fragmentation and apoptotic body formation, resulting in fulminant hepatitis and lethality of mice. Pre-administration of acteoside at 10 or 50 mg/kg subcutaneously at 12 and 1 h prior to D-GalN/LPS intoxication significantly inhibited hepatic apoptosis, hepatitis and lethality. Tumor necrosis factor-alpha (TNF-alpha) secreted from LPS-stimulated macrophages is an important mediator of apoptosis in this model. Acteoside showed no apparent effect on the marked elevation of serum TNF-alpha, but it partially prevented in vitro TNF-alpha (100 ng/ml)-induced cell death in D-GalN (0.5 mM)-sensitized hepatocytes at the concentrations of 50, 100 and 200 microM. These results indicated that D-GalN/LPS-induced hepatic apoptosis can be blocked by an exogenous antioxidant, suggesting the involvement of reactive oxygen intermediates (ROIs) in TNF-alpha-dependent hepatic apoptosis.
Asunto(s)
Antioxidantes/farmacología , Apoptosis/efectos de los fármacos , Enfermedad Hepática Inducida por Sustancias y Drogas/prevención & control , Glucósidos/farmacología , Fallo Hepático/prevención & control , Hígado/efectos de los fármacos , Fenoles , Alanina Transaminasa/sangre , Animales , Aspartato Aminotransferasas/sangre , Supervivencia Celular , Enfermedad Hepática Inducida por Sustancias y Drogas/sangre , Enfermedad Hepática Inducida por Sustancias y Drogas/patología , ADN/efectos de los fármacos , Sinergismo Farmacológico , Galactosamina/toxicidad , Lipopolisacáridos/toxicidad , Hígado/patología , Fallo Hepático/sangre , Fallo Hepático/inducido químicamente , Fallo Hepático/patología , Masculino , Ratones , Extractos Vegetales/farmacología , Factor de Necrosis Tumoral alfa/metabolismo , Factor de Necrosis Tumoral alfa/farmacologíaRESUMEN
We previously showed that the extract of Japanese angelica root (JAR-E) reversed the decrease in pentobarbital (PB) sleep induced by isolation stress and yohimbine and methoxamine, stimulants of central noradrenergic systems, in mice. Here, we tested the effects of several fractions from JAR-E and ligustilide and butylidenephthalide, phthalide components of JAR-E, on PB sleep in isolated mice to elucidate the mechanism of the action of JAR-E. Methanol-soluble (Met-S) and -insoluble (Met-IS) fractions were obtained from JAR-E. Methylenechloride-soluble (MC-S) and -insoluble fractions (MC-IS) were prepared from Met-S. MC-S (11.4-76 mg/kg, p.o.) reversed the isolation stress-induced decrease in PB sleep, but neither Met-IS (0.8-2.4 g/kg, p.o.) nor MC-IS (0.7-2 g/kg, p.o.) had the same effect. The i.p. administration of MC-S exhibited a similar activity to that observed after the p.o. administration of the same fraction. Ligustilide (5-20 mg/kg, i.p.) and butylidenephthalide (10-30 mg/kg, i.p.) reversed PB sleep decrease in isolated mice. Both components (20 mg/kg, i.p.) attenuated the suppressive effects of yohimbine (30 nmol, i.c.v.), methoxamine (200 nmol, i.c.v.) and a benzodiazepine inverse agonist FG7142 (10 mg/kg, i.p.) on PB sleep in group-housed mice. These results suggest the contribution of ligustilide and butylidenephthalide to the effect of JAR-E on PB sleep in isolated mice, and implicate central noradrenergic and/or GABA(A) systems in the effects of these components.
Asunto(s)
4-Butirolactona/análogos & derivados , Encéfalo/efectos de los fármacos , Parasimpatolíticos/farmacología , Pentobarbital/administración & dosificación , Anhídridos Ftálicos/farmacología , Extractos Vegetales/farmacología , Sueño/efectos de los fármacos , 4-Butirolactona/farmacología , Animales , Carbolinas/farmacología , Diazepam/farmacología , Relación Dosis-Respuesta a Droga , Inyecciones Intraventriculares , Masculino , Metoxamina/farmacología , Cloruro de Metileno , Ratones , Extractos Vegetales/química , Raíces de Plantas/química , Plantas Medicinales/química , Sueño/fisiología , Aislamiento Social , Yohimbina/farmacologíaRESUMEN
Four unprecedented diarylheptanoids-calyxin H (1) and epicalyxin H (2), possessing a diarylheptanoid unit and a chalcone moiety, and blepharocalyxins A (3) and B (4), possessing two diarylheptanoid units and a chalcone moiety-were isolated from the seeds of Alpiniablepharocalyx. The structures of 1-4, including absolute stereochemistry, were elucidated by spectroscopic means and after a consideration of their biogenesis.
RESUMEN
A new thiolactone containing antibiotic 834-B1 was isolated from the culture broth of Streptomyces sp. Y-0834H which has also produced thiolactomycin and thiotetromycin at the same time. The structure of 834-B1 was determined as I by the decoupling experiment in NMR.
Asunto(s)
Antibacterianos/aislamiento & purificación , Streptomyces/metabolismo , Antibacterianos/análisis , Antibacterianos/biosíntesis , Cromatografía en Gel , Medios de Cultivo , Fermentación , Lactonas/análisis , Estructura Molecular , Streptomyces/clasificación , Streptomyces/crecimiento & desarrollo , Tiofenos/análisisRESUMEN
New antibiotics designated as thiazocins A and B were isolated from the culture broth of Actinosynnema sp. C-304. Thiazocins A and B exhibited inhibitory activities against an aldose reductase from human placenta.
Asunto(s)
Aldehído Reductasa/antagonistas & inhibidores , Antibacterianos/biosíntesis , Actinomycetales/metabolismo , Antibacterianos/química , Antibacterianos/farmacología , Fenómenos Químicos , Química Física , Cromatografía , Femenino , Fermentación , Humanos , Espectroscopía de Resonancia Magnética , Placenta/enzimología , Espectrofotometría Infrarroja , Espectrofotometría UltravioletaRESUMEN
Phospholine was isolated as an antitumor antibiotic from the fermentation broth of Streptomyces hygroscopicus. Phospholine is an amphoteric compound which has an amino group and a phosphoric acid ester as functional groups. Phospholine shows strong activities against L1210, P388 and EL-4.
Asunto(s)
Antibióticos Antineoplásicos/aislamiento & purificación , Antibióticos Antineoplásicos/análisis , Fenómenos Químicos , Química , Fermentación , Lactonas/aislamiento & purificación , Lactonas/uso terapéutico , Leucemia Experimental/tratamiento farmacológico , Espectroscopía de Resonancia Magnética , Compuestos Organofosforados/aislamiento & purificación , Compuestos Organofosforados/uso terapéutico , StreptomycesRESUMEN
Hatomamicin, a new alkaloid antibiotic, was isolated from the culture filtrate of a strain of Saccharopolyspora. The antibiotic was extracted with EtOAc and purified by silica gel column chromatography. The free alkaloid was obtained as pale yellowish prisms from CH3CN solution. It exhibits antimicrobial activity against Gram-positive organisms. The apparent molecular formula of hatomamicin was determined to be C22H31NO5. The structure has been established by a combination of spectroscopic and X-ray crystallographic studies.
Asunto(s)
Antibacterianos/análisis , Bacterias/metabolismo , Alcaloides/análisis , Alcaloides/biosíntesis , Alcaloides/aislamiento & purificación , Alcaloides/farmacología , Antibacterianos/biosíntesis , Antibacterianos/aislamiento & purificación , Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Cromatografía en Capa Delgada , Fermentación , Espectroscopía de Resonancia Magnética , Estructura Molecular , Microbiología del Suelo , Espectrofotometría Infrarroja , Células Tumorales Cultivadas , Difracción de Rayos XRESUMEN
Okilactomycin, a novel antibiotic, was isolated from the culture filtrate of a strain of actinomycetes. The producing organism, strain YP-02908L, was identified as Streptomyces griseoflavus subsp. zamamiensis subsp. nov. The antibiotic was extracted with ethyl acetate and purified by silica gel column chromatography. It was obtained as colorless prisms from a dichloromethane solution. It exhibited weak antimicrobial activity against Ehrlich ascites carcinoma in vivo. The apparent molecular formula of okilactomycin was determined as C24H32O6. It is a new member of the lactone group antibiotics.
Asunto(s)
Antibacterianos/aislamiento & purificación , Animales , Antibacterianos/análisis , Carcinoma de Ehrlich/tratamiento farmacológico , Fenómenos Químicos , Química , Femenino , Inyecciones Intraperitoneales , Lactonas/análisis , Lactonas/aislamiento & purificación , Lactonas/uso terapéutico , Ratones , Neoplasias Experimentales/tratamiento farmacológicoRESUMEN
Effects of aqueous extracts of Apocynum venetum leaves (Luobuma extracts) on the blood pressure were evaluated in hypertensive animal models, such as spontaneously hypertensive rats (SHR), renal hypertensive rats and NaCl-induced hypertensive rats. In SHR, administration of Luobuma (heat-processed and unprocessed leaves) extracts at a dose of 70 mg/rat per day significantly decreased the systolic blood pressure value, but their decreasing effects were weaker than that of captopril. The urine volume, and the urinary Na(+), K(+) and protein excretions were not significantly different between Luobuma-treated and untreated groups. In 3/4 nephrectomized rats, the Luobuma extracts significantly decreased the systolic blood pressure value, accompanied by significant increases of the urine volume and the urinary Na(+) and K(+) excretions. Furthermore, they decreased the blood urea nitrogen (BUN) level. In NaCl-induced hypertensive rats, the Luobuma extract decreased the systolic blood pressure value. However, it did not change the urinary excretions of Na(+), K(+) and protein. The BUN level was lower than that of control rats, but the serum total cholesterol (TC) level did not changed. From these findings, the Luobuma extracts have an anti-hypertensive effect, possibly due to amelioration of the kidney functions in the three experimental animal models.