RESUMEN
In this study, we employed a previously developed in vivo assay system to determine whether the flowers and leaves of Syringa vulgaris (S. vulgaris; commonly known as "lilac") can prevent blood stasis syndrome, known as oketsu in Japanese. This syndrome is considered an important pathology in traditional Chinese and Japanese medicine, and is related to diseases such as peripheral vascular disorders, blood vessel inflammation, and platelet aggregation, whose severities are augmented owing to lipid peroxidation, free radicals, and oxidative stress. The assay system employed in this study monitored the blood flow decrease in the tail vein of mice subjected to sensitization with hen egg white lysozyme. Through bioassay-guided fractionation of different S. vulgaris extracts, five polyphenols were isolated and identified. Among them, quercetine 3-glucoside, quercetin 3-rutinoside, and acteoside were identified as active compounds, as they significantly mitigated blood flow reduction. These findings indicate that the polyphenols obtained from S. vulgaris could be useful for preventing oketsu and improve the quality of life of individuals with disorders and diseases such as gynecopathy, cold sensitivity, poor circulation, allergy, and lifestyle-related diseases.
RESUMEN
The fibrinolysis system is thought to play an important role in liver regeneration. We previously found that plasminogen (Plg) is localized to the cell surface of regenerating liver tissue as well as proliferating hepatocytes in vitro. Here, we investigated the significance of Plg binding to the cell surface during liver regeneration. Pre-administration of tranexamic acid (TXA), which is a competitive inhibitor of Plg binding, to hepatectomized rats mildly delayed restoration of liver weight in vivo. Although binding of Plg to the cell membrane decreased following TXA administration, TXA showed little effect on hepatocyte proliferation in rats. We also discovered that Plg treatment did not stimulate proliferation of primary rat hepatocytes in vitro. These results suggest that Plg/plasmin potentiates liver regeneration via a pathway distinct from those through which hepatocyte proliferation is stimulated.
Asunto(s)
Regeneración Hepática/efectos de los fármacos , Plasminógeno/metabolismo , Ácido Tranexámico/farmacología , Animales , Membrana Celular/efectos de los fármacos , Membrana Celular/metabolismo , Proliferación Celular/efectos de los fármacos , Hígado/citología , Hígado/efectos de los fármacos , Hígado/metabolismo , Hígado/fisiología , Masculino , Unión Proteica/efectos de los fármacos , Ratas , Ratas WistarRESUMEN
Stress exacerbates allergic disorders such as atopic dermatitis and asthma. It is also an important factor affecting blood flow (BF). Allergic reactions also affect blood flow. For example, we observed that mice sensitized with hen egg-white lysozyme (HEL) have decreased BF during the allergy induction phase. Based on this finding, we established a model for evaluating chronic restraint stress-enhanced allergies. Mice were sensitized with 12.5 µg/head of HEL on day 0, then restrained for 90 min daily on days 1-3, 5, and 6 in a modified 50 mL polystyrene conical centrifuge tube with multiple air holes for ventilation. We used the decrease in BF during that time as a guide for developing an in vivo assay for substances that can inhibit stress-enhanced allergies. Finally, we demonstrated the utility of the new method by testing crude drugs that are used solely or in combination with other crude drugs to treat stress-related illness and neuropsychiatric symptoms. Our model should be useful for identifying potential anti-stress-enhanced allergy drugs.
Asunto(s)
Antialérgicos/farmacología , Bioensayo , Mezclas Complejas/farmacología , Hipersensibilidad/tratamiento farmacológico , Flujo Sanguíneo Regional/efectos de los fármacos , Estrés Psicológico/complicaciones , Animales , Antígenos , Corticosterona/sangre , Hipersensibilidad/complicaciones , Hipersensibilidad/fisiopatología , Magnoliopsida/química , Masculino , Ratones , Muramidasa , Poria/química , Restricción Física , Estrés Psicológico/fisiopatología , Cola (estructura animal)/irrigación sanguíneaRESUMEN
Allergy-preventive activity of flower buds of Lonicera japonica THUNB. was found in the 35% EtOH extract (LJ) using an in vivo assay, The assay system uses monitoring of a decrease in blood flow (BF) in the tail vein of mice subjected to sensitization with hen-egg white lysozyme (HEL). Bioassay-guided fractionation of the 35% EtOH extract led to isolation of chlorogenic acid (1) and three known iridoid derivatives, loganin (2), secoxyloganin (3) and sweroside (4), all of which inhibited the BF decrease. This suggested that the flower buds of L. japonica and compounds isolated from them have allergy-preventive properties. The structure-activity relationship of iridoid derivatives, morroniside (5), geniposide (6), asperuloside (7), aucubin (8) and catalpol (9), were also tested using the same bioassay method. Compounds 2-5 and 9 having the sp(3) atom at C-8 showed an allergy-preventive effect, while compounds 6, 7 and 8 having a double bond at C-7, C-8 did not.
Asunto(s)
Ácido Clorogénico/uso terapéutico , Hipersensibilidad/prevención & control , Iridoides/uso terapéutico , Lonicera/química , Fitoterapia , Extractos Vegetales/uso terapéutico , Animales , Antialérgicos/aislamiento & purificación , Antialérgicos/farmacología , Antialérgicos/uso terapéutico , Pollos , Ácido Clorogénico/aislamiento & purificación , Ácido Clorogénico/farmacología , Femenino , Flores/química , Hipersensibilidad/inmunología , Glucósidos Iridoides/aislamiento & purificación , Glucósidos Iridoides/farmacología , Glucósidos Iridoides/uso terapéutico , Iridoides/aislamiento & purificación , Iridoides/farmacología , Masculino , Ratones , Ratones Endogámicos , Muramidasa , Extractos Vegetales/química , Extractos Vegetales/farmacología , Relación Estructura-Actividad , VenasRESUMEN
The allergy-preventive activity of a 35% EtOH extract (IT) of flowers of Impatiens textori MIQ. was demonstrated in a continuing search for allergy-preventive substances from natural sources. The evaluation of its activity used an in vivo assay method for monitoring the blood flow decrease in the tail vein microcirculation of mice subjected to sensitization with hen-egg white lysozyme. Among the principal compounds in IT, apigenin (1), luteolin (3), and luteolin 7-glucoside (4) showed significant allergy-preventive effects.
Asunto(s)
Antialérgicos/uso terapéutico , Glucósidos/farmacología , Hipersensibilidad Tardía/prevención & control , Impatiens/química , Extractos Vegetales/uso terapéutico , Animales , Antialérgicos/farmacología , Apigenina/farmacología , Pollos , Clara de Huevo , Flavonas/farmacología , Flores , Hemorreología/efectos de los fármacos , Hipersensibilidad Tardía/inducido químicamente , Hipersensibilidad Tardía/fisiopatología , Luteolina/farmacología , Ratones , Muramidasa , Fitoterapia , Extractos Vegetales/farmacología , Cola (estructura animal)/irrigación sanguíneaRESUMEN
Linarinic acid, (-)-1,2,3,9-tetrahydropyrrolo[2,1-b]quinazoline-1-carboxylic acid (4a), was isolated from the ethanol extract of Linaria vulgaris Mill. In our previous study, a series of tetrahydropyrrolo[2,1-b]quinazoline derivatives 4b, 4c, 5a, 5b, 6a and 6b that were structurally related to 4a and evaluated as neuroprotective agents were synthesized. The aim of the present study was to investigate the novel features of these compounds. We examined their allergy-preventive effects using an in vivo assay system we developed previously, that monitors a decrease in blood flow in the tail vein of mice subjected to sensitization with hen egg-white lysozyme. We observed that 4a and its three derivatives, amide (6a), ester (5a), bromine (4b), and alcohol substituent (6b), showed significant allergy-preventive activities. The study confirmed the allergy-preventive activity of tetrahydropyrrolo[2,1-b]quinazoline derivatives by comprehensively monitoring the specific blood flow decrease occurring in the induction phase of allergy. This finding may aid in the development of new agents for the treatment of allergic diseases such as atopic dermatitis, allergic asthma, and hay fever.
Asunto(s)
Hipersensibilidad/prevención & control , Linaria/química , Quinazolinas/química , Animales , Hipersensibilidad/tratamiento farmacológico , RatonesRESUMEN
In the course of our survey of natural compounds inhibiting prostaglandin E2 release and/or lipopolysaccharide (LPS)-induced transcriptional stimulation via NF-kappaB, a central regulator of inflammatory genes, from natural resources, we found garcinone B, a xanthone from callus tissue culture of Hypericum patulum, as a compound with such pharmacological activities, that is a derivative of gamma-mangostin which potently inhibits COX-1 and COX-2 activities to reduce PGE2 release from C6 rat glioma cells, and inhibits IKK activity to prevent NF-kappaB-dependent COX-2 gene transcription. Garcinone B, to a lesser extent, reduced A23187-induced increase in prostaglandin E2 release than gamma-mangostin and its structurally related compound, patulone, in C6 cells. This compound also prevented LPS-induced stimulation of NF-kappaB-dependent transcription. These results suggest that garcinone B becomes a unique pharmacological tool to investigate intracellular signaling pathways involved in inflammation.
Asunto(s)
Neoplasias Encefálicas/metabolismo , Dinoprostona/metabolismo , Glioma/metabolismo , FN-kappa B/genética , Antagonistas de Prostaglandina/farmacología , Transcripción Genética/efectos de los fármacos , Xantonas/farmacología , Animales , Calcimicina/farmacología , Línea Celular Tumoral , Ciclooxigenasa 1/metabolismo , Hypericum/química , Mediadores de Inflamación/metabolismo , Lipopolisacáridos/farmacología , Ratas , Xantinas/farmacologíaRESUMEN
Kinka-cha (dried leaf of Camellia nitidissima) is used as a folk tea for detoxication, diuresis and antihypertension. In the present study, we evaluated the extract of kinka-cha on metabolic, vascular and oxidative stress parameters in a model of metabolic syndrome, SHR/NDmcr-cp/cp (SHR/cp) rats that manifest hypertension, obesity, glucose intolerance and hyperlipidemia. Treatment with the extract of kinka-cha alleviated the increase in blood pressure, decrease in tail blood flow and elevated serum oxidative stress marker levels including lipid peroxides, 8-hydroxy-2'-deoxyguanosine, 3-nitrotyrosine and 3-chlorotyrosine. However, kinka-cha did not affect weight gain, hyperglycemia and hyperlipidemia, nor the relaxation responses of the aorta mesenteric artery, thoracic aortas and tail vein, and blood clotting and platelet aggregation. These results suggest that kinka-cha can help reduce the risk of developing metabolic syndrome, possibly due to the presence of antioxidants.
Asunto(s)
Síndrome Metabólico/sangre , Síndrome Metabólico/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Té/química , Animales , Presión Sanguínea/efectos de los fármacos , Cromatografía Líquida de Alta Presión , Modelos Animales de Enfermedad , Femenino , Extractos Vegetales/química , Ratas , Ratas Endogámicas WKY , Flujo Sanguíneo Regional/efectos de los fármacosRESUMEN
Allergy-preventive activity was demonstrated for the MeOH extract (HM) of the petals of Hibiscus mutabilis L. 'versicolor' MAKINO in a continuing search for allergy-preventive substances from natural sources, using the in vivo assay method. This assay system uses monitoring of a decrease in the blood flow at the tail vein of mice subjected to hen egg-white lysozyme (HEL) sensitization. By bioassay-directed fractionation, a new flavonol triglycoside, quercetin 3-O-[beta-D-xylopyranosyl(1-->2)-alpha-L-rhamnopyranosyl(1-->6)]-beta-D-galactopyranoside (1: mutabiloside), was isolated, together with four known flavonols identified as quercetin 3-O-[beta-D-xylopyranosyl(1-->2)]-beta-D-galactopyranoside (2) and kaempferol 3-O-[beta-D-xylopyranosyl(1-->2)]-beta-D-galactopyranoside (3), quercetin (4) and hyperoside (5). The structure of the new flavonol 1 was elucidated by spectroscopic methods. Among these flavonol derivatives, compounds 1 and 2 showed significant allergy-preventive effects.
Asunto(s)
Antialérgicos/farmacología , Flavonoides/farmacología , Glicósidos/farmacología , Hibiscus/química , Animales , Antialérgicos/aislamiento & purificación , Flavonoides/aislamiento & purificación , Glicósidos/aislamiento & purificación , Masculino , Ratones , Muramidasa/inmunología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Agregación Plaquetaria/efectos de los fármacos , Flujo Sanguíneo Regional/efectos de los fármacos , Cola (estructura animal)/irrigación sanguíneaRESUMEN
Allergy-preventive activity was demonstrated for an extract of resins from Xanthorrhoea hastilis R. BR. in a search for allergy-preventive substances from natural sources. By bioassay-directed fractionation of this plant extract, a new flavanone, 3',5'-dihydroxy-7,4'-dimethoxyflavanone (1), and two new chalcones, 3,5,2'-trihydroxy-4,4'-dimethoxychalcone (2) and 5,2'-dihydroxy-3,4,4'-trimethoxychalcone (3), were isolated together with five known compounds, 5'-hydroxy-7,3',4'-trimethoxyflavanone (4), 3'-hydroxy-7,4'-dimethoxyflavanone (5), liquiritigenin 7-methyl ether (6), 4,2'-dihydroxy-4'-methoxychalcone (7) and sakuranetin (8). The structures of 1, 2 and 3 were elucidated by spectroscopic methods. All of these compounds showed allergy-preventive effects.
Asunto(s)
Flavonoides/farmacología , Hipersensibilidad/prevención & control , Magnoliopsida/química , Flavonoides/química , Flavonoides/aislamiento & purificación , Espectroscopía de Resonancia Magnética , Espectrometría de Masa por Ionización de Electrospray , Espectrofotometría UltravioletaRESUMEN
Our in vivo assay system developed to search for allergy-preventive substances, assesses the blood flow decrease in tail vein microcirculation of mice subjected to sensitization with hen-egg white lysozyme (HEL). The blood flow decrease appears to be regulated by various factors such as nitric oxide (NO), thromboxane (TX) A(2), prostacyclin (PGI(2)) and endothelin (ET)-1 together with cyclooxygenase (COX)-1, COX-2, inducible nitric oxide synthase (iNOS), and constitutive nitric oxide synthase (cNOS). In this study, we examined in detail the roles of iNOS in this assay system using an iNOS knockout (KO) mouse. We found that the blood flow decrease in the HEL-sensitized iNOS KO mice was slightly weaker than that in their wild type (WT) mice. This blood flow decrease was not affected by a selective COX-1 inhibitor, a selective COX-2 inhibitor and a PGI(2) agonist unlike the case of the WT mice. However, it was inhibited by a nonselective NOS inhibitor, a specific TXA(2) synthase inhibitor and a specific ET-1 receptor blocker as in the case of the WT mice. The present results indicate that the blood flow decrease occurs via two pathways; one is an iNOS-independent response involving TXA(2) and ET-1, and the other is an iNOS-dependent response involving COX-1, COX-2 and PGI(2). cNOS appears to play some roles in the blood flow decrease and iNOS acts as an exacerbation factor. Our method using HEL-sensitized should be useful for searching for agents that can prevent allergy via new mechanisms.
Asunto(s)
Hipersensibilidad/prevención & control , Muramidasa/inmunología , Óxido Nítrico Sintasa de Tipo II/fisiología , Flujo Sanguíneo Regional , Animales , Epoprostenol/análogos & derivados , Epoprostenol/farmacología , Femenino , Metacrilatos/farmacología , Ratones , Ratones Endogámicos C57BL , NG-Nitroarginina Metil Éster/farmacología , Nitrobencenos/farmacología , Péptidos Cíclicos/farmacología , Sulfonamidas/farmacología , Tromboxano A2/biosíntesis , Venas/fisiologíaRESUMEN
Allergy-preventive activity was demonstrated for an extract of the bark of Populus sieboldii in a continuing search for allergy-preventive substances from natural sources. By bioassay-directed fractionation of this plant bark, two new phenolic glycosides, siebolside A {2-hydroxy-5-[(benzoyloxy)methyl]phenyl (6'-O-acetyl) beta-D-glucopyranoside} (1) and siebolside B {2-hydroxy-5-[(benzoyloxy)methyl]phenyl beta-D-glucopyranoside} (2), were isolated, together with three known compounds, salicin (3), sakuranin (4), and neosakuranin (5). The structures of 1 and 2 were elucidated by spectroscopic methods. Compounds 1-5 all showed allergy-preventive effects.
Asunto(s)
Glicósidos , Hipersensibilidad/prevención & control , Populus/química , Animales , Plaquetas/efectos de los fármacos , Glucósidos , Glicósidos/sangre , Glicósidos/química , Glicósidos/aislamiento & purificación , Glicósidos/farmacología , Japón , Ratones , Estructura Molecular , Fenoles/sangre , Fenoles/química , Fenoles/aislamiento & purificación , Fenoles/farmacología , Corteza de la Planta/químicaRESUMEN
The inhibitory effects of 22 xanthones from three Guttiferae plants (Hypericum patulum, Calophyllum inophyllum and C. austroindium) on exogenous platelet activating factor (PAF)-induced hypotension were examined using a blood pressure monitoring in vivo assay method. Guanandin (2), caloxanthone E (3), 1,3,5,6-tetrahydroxy-2-isoprenylxanthone (8), 6-deoxyjacareubin (11) and patulone (18) showed strong inhibition of PAF-induced hypotension, with inhibitory effects of more than 60 %. Their ID50 values were greater than that of ginkgolide B (BN-52 021), a natural PAF-antagonist from the Ginkgo biloba.
Asunto(s)
Antihipertensivos/farmacología , Calophyllum , Hypericum , Fitoterapia , Extractos Vegetales/farmacología , Animales , Antihipertensivos/administración & dosificación , Antihipertensivos/uso terapéutico , Presión Sanguínea/efectos de los fármacos , Hipertensión/inducido químicamente , Hipertensión/tratamiento farmacológico , Masculino , Ratones , Ratones Endogámicos , Extractos Vegetales/administración & dosificación , Extractos Vegetales/uso terapéutico , Factor de Activación PlaquetariaRESUMEN
The anti-anaphylactic and anti-pruritic activities of a 35% EtOH extract (IT) of the flowers of Impatiens textori MIQ. were investigated by in vivo assay. IT and apigenin (1), apigenin 7-glucoside (2) and luteolin (3), principal compounds from IT, inhibited compound 48/80 (COM)-induced by blood pressure (BP) decrease, which was an immunoglobulin (Ig)E-independent anaphylaxis-like response. Compounds 1-3 all inhibited BP decrease induced by IgE-dependent anaphylaxis. Furthermore, IT also inhibited the blood flow (BF) decrease induced by antigen-induced anaphylaxis in actively sensitized mice. IT showed a significant inhibitory effect on scratching behavior induced by COM without a central depressant. IT also significantly inhibited platelet activating factor (PAF)- and serotonin (5-HT)-induced scratching behavior and mitigated protease (PA)-induced scratching behavior. These findings showed that the flowers of I. textori can be utilized as an anti-anaphylactic and anti-pruritic agent in addition to the traditional applications of this plant.
Asunto(s)
Anafilaxia/tratamiento farmacológico , Impatiens/química , Prurito/tratamiento farmacológico , Animales , Conducta Animal/efectos de los fármacos , Presión Sanguínea/efectos de los fármacos , Flores/química , Hipnóticos y Sedantes/farmacología , Inmunoglobulina E/inmunología , Masculino , Ratones , Actividad Motora/efectos de los fármacos , Muramidasa/inmunología , Factor de Activación Plaquetaria/farmacología , Prurito/psicología , Flujo Sanguíneo Regional/efectos de los fármacos , Serotonina/farmacología , p-Metoxi-N-metilfenetilamina/farmacologíaRESUMEN
We discovered a phenomenon in which the blood flow in vein microcirculation markedly decreases in response to hen-egg white lysozyme (HEL)-sensitization without any change in blood pressure. Using this blood flow decrease as a guide, we developed an in vivo assay method to search for substances, which can prevent allergies. Antagonists of histamine, serotonin and platelet activating factor (PAF) did not affect the blood flow decrease in response to HEL-sensitization. On the other hand, cyclooxygenase (COX)-1, COX-2, thromboxane (TX) A(2), endothelin-1 (ET-1), prostacyclin (PGI(2)) and granulocytic elastase (GE) as well as nitric oxide (NO) from inducible NO synthase (iNOS) were involved in the blood flow decrease. Thus, these substances might injure vascular endothelial cells, and cause a decrease in blood flow in vein microcirculation. Our method can be used to search for preventive agents against allergies involving NO, COX-1, 2 and PGI(2). This is the first report to applying to an assay method the specific blood flow decrease to occur in the promotion stage of allergy.
Asunto(s)
Antialérgicos/farmacología , Bioensayo , Muramidasa/farmacología , Flujo Sanguíneo Regional/efectos de los fármacos , Animales , Clara de Huevo , Ratones , Óxido Nítrico/biosíntesisRESUMEN
Significant selective cyclooxygenase-2 (COX-2) inhibitory activities were observed for two new 1,4-naphthoquinone sodium salts, sodium 3-hydroxide-2[[sodium 3-hydroxide-1,4-dioxo(2-naphthyl)]ethyl]naphthalene-1,4-dione (impatienolate) (1) and sodium 2-hydroxide-3-(2-hydroxyethyl)naphthalene-1,4-dione (balsaminolate) (2), which were isolated from the corolla of Impatiens balsamina L. (Balsaminaceae). Their structures were elucidated by spectral techniques. Our results offer evidence supporting the use of I. balsamina L. to treat articular rheumatism, pain, and swelling.
Asunto(s)
Inhibidores de la Ciclooxigenasa/farmacología , Impatiens/química , Isoenzimas/metabolismo , Naftoquinonas/farmacología , Prostaglandina-Endoperóxido Sintasas/metabolismo , Ciclooxigenasa 1 , Ciclooxigenasa 2 , Inhibidores de la Ciclooxigenasa 2 , Inhibidores de la Ciclooxigenasa/aislamiento & purificación , Espectroscopía de Resonancia Magnética , Naftoquinonas/aislamiento & purificación , Espectrofotometría Infrarroja , Espectrofotometría UltravioletaRESUMEN
Monitoring the blood flow of unanesthesized mice was found to be a reliable and effective method for studying their anaphylactic responses, in addition to the known method of monitoring blood pressure. Hen egg-white lysozyme (HEL)-specific anaphylaxis in mice was estimated by monitoring the decrease in blood flow with a Doppler blood flow meter. This method is convenient for searching for both anaphylaxis and anti-anaphylactic substances from natural products. Using this system, we estimated the anti-anaphylactic effects of the 35% ethanol extract (IB) of petals of Impatiens balsamina L., as well as those of anti-allergic agents currently used. Kaempferol 3-rutinoside and lawsone from IB significantly inhibited the decrease of blood flow. We also found that platelet-activating factor (PAF) and serotonin participate in decreasing the blood flow, but histamine does not.
Asunto(s)
Anafilaxia/tratamiento farmacológico , Anafilaxia/fisiopatología , Impatiens/química , Muramidasa , Cola (estructura animal)/irrigación sanguínea , Cola (estructura animal)/efectos de los fármacos , Anafilaxia/inducido químicamente , Animales , Velocidad del Flujo Sanguíneo/efectos de los fármacos , Velocidad del Flujo Sanguíneo/fisiología , Masculino , Ratones , Muramidasa/efectos adversos , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Estructuras de las Plantas , Flujo Sanguíneo Regional/efectos de los fármacos , Flujo Sanguíneo Regional/fisiologíaRESUMEN
A 35% EtOH extract of the fruits of Chaenomeles sinensis, long utilized as a folk medicine for cough, significantly inhibited the pruritogenic agent compound 48/80 (COM)-induced scratching behavior in mice. Antipruritic activity-guided fractionation and purification yielded active quercetin, apigenin, and catechin derivatives, which exhibited significant inhibitory effects on COM-induced scratching behavior. To the best of our knowledge, apigenin (5), apigenin 7-glucronide (6), and apigenin 4'-methoxy-7-glucronide (acacetin 7-glucronide) (7) were isolated from the fruits of C. sinensis for the first time. The active fraction and these compounds also inhibited serotonin-, platelet activating factor-, and prostaglandin E(2)-induced scratching behavior, but did not inhibit histamine-induced scratching behavior or locomotive behavior. This study also showed that the fruits of C. sinensis could be used to treat allergic itching sensation.
Asunto(s)
Antipruriginosos/uso terapéutico , Frutas , Prurito/tratamiento farmacológico , Rosaceae , Animales , Antipruriginosos/química , Antipruriginosos/farmacología , Locomoción/efectos de los fármacos , Locomoción/fisiología , Masculino , Ratones , Ratones Endogámicos ICR , Fitoterapia/métodos , Extractos Vegetales/química , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Prurito/inducido químicamenteRESUMEN
The antipruritic effects of orally administered 1,4-naphthoquinone derivatives and related compounds on compound 48/80-induced scratching behavior in mice were studied. 2-Hydroxy-3-(2-hydroxyethyl)-1,4-naphthoquinone, ferulic acid, 2,2'-methylenebis(3-hydroxy-1,4-naphthoquinone), and 2,2'-ethylidenebis(3-hydroxy-1,4-naphthoquinone) (impatienol) all exhibited significant antipruritic activity. However, 2-methoxy-3-(2-hydroxyethyl)-1,4-naphthoquinone (balsaquinone), which was isolated from a natural source for the first time, did not show any activity. The present results indicate that these compounds are promising for treating allergic diseases with chronic and severe pruritus.
Asunto(s)
Antipruriginosos , Naftoquinonas/farmacología , Prurito/prevención & control , Animales , Espectroscopía de Resonancia Magnética , Masculino , Ratones , Naftoquinonas/síntesis química , Naftoquinonas/aislamiento & purificación , Plantas Medicinales/química , Prurito/inducido químicamente , Espectrofotometría Infrarroja , Espectrofotometría Ultravioleta , p-Metoxi-N-metilfenetilaminaRESUMEN
A 35% EtOH extract of flowers of Impatiens textori MIQ. showed an inhibitory effect on blood pressure decrease in response to platelet activating factor (PAF) measured with a blood pressure monitoring system. Bioassay-guided fractionation of the 35% EtOH extract (IT) led to isolation of the flavones apigenin (1) and luteolin (3), which significantly inhibited blood pressure decrease in response to PAF. Their compounds and apigenin 7-glucoside (2), chrysoeriol (4), quercetin (5), quercetin 3-glucoside (6), kaempferol (7), kaempferol 3-glucoside (8) and kaempferol 3-rhamnosyldiglucoside (9) were also isolated from the flowers of I. textori for the first time. This study revealed that the flowers of I. textori might be a possible anti-allergy agent.