RESUMO
The increasing incidence of atopic dermatitis during recent decades has prompted the development of safe and effective agents for prevention of atopic diseases. Esculeoside A, a glycoside of spirosolane type, is identified as a major component in ripe tomato fruits. The present study investigated the effects of esculeoside A and its aglycon esculeogenin A on hyaluronidase activity in vitro and antiallergy in experimental dermatitis mice. Esculeogenin A/esculeoside A (esculeogenin A equivalent) with an IC50 of about 2 µM/9 µM dose-dependently inhibited hyaluronidase activity measured by a modified Morgan-Elson method. Oral treatment with esculeoside A 10 mg/kg of experimental dermatitis mice for 4 weeks significantly decreased the skin clinical score to 2.5 without any detectable side effects compared with 6.75 of the control. The scratching frequency of esculeoside A 100 mg/kg application was decreased significantly as 107.5 times compared with 296.67 times of the control. Thus, the present study showed that esculeoside A/esculeogenin A significantly blocks hyaluronidase activity in vitro and that esculeoside A ameliorates mouse experimental dermatitis.
Assuntos
Dermatite/tratamento farmacológico , Hialuronoglucosaminidase/antagonistas & inibidores , Extratos Vegetais/administração & dosagem , Sapogeninas/administração & dosagem , Solanum lycopersicum/química , Animais , Dermatite/enzimologia , Modelos Animais de Doenças , Feminino , Frutas/química , Humanos , Hialuronoglucosaminidase/metabolismo , Camundongos , Camundongos Endogâmicos BALB CRESUMO
Six novel acyclic sulfides, named garlicnins L-1-L-4 (1-4), E (5), and F (6), were isolated from the acetone extracts, with the ability to suppress M2 macrophage activation, of the bulbs of garlic (Allium sativum L.), and their chemical structures were characterized.
Assuntos
Alho/química , Macrófagos/efeitos dos fármacos , Sulfetos/farmacologia , Tiofenos/farmacologia , Humanos , Estrutura Molecular , Relação Estrutura-Atividade , Sulfetos/química , Sulfetos/isolamento & purificação , Tiofenos/química , Tiofenos/isolamento & purificaçãoRESUMO
Several novel sulfides from acetone extracts of bulbs of garlic (Allium sativum L.), were identified and investigated. These were named garlicnins B(1) (1), C(1) (2), and D (3), and they were found to have the ability to control macrophage activation. Garlicnins B(1) (1) and C(1) (2) possess a new skeleton of cyclic sulfoxide and their structures of garlicnins B(1) (1) and C(1) (2) were characterized as 3,4-dimethyltetrahydrothiophene-S-oxide derivatives carrying the substitutions of a propenyl and a sulfenic acid, and an allyldithiine and a 1-propene-sulfenic acid (a), respectively. The mechanism of the proposed production of these compounds is discussed. Garlicnin D (3), dithiine-type, was estimated to be derived by addition of (a)+allyl thiosulfenic acid (b) derived from allicin. The identification of these novel sufoxides from onion and garlic accumulates a great deal of new chemistry to the Allium sulfide field, and future pharmacological investigations aid the development of natural, healthy foods and anti-cancer agents that could potentially prevent or combat disease.
Assuntos
Alho , Tiofenos/química , Antígenos CD/metabolismo , Antígenos de Diferenciação Mielomonocítica/metabolismo , Alho/química , Humanos , Ativação de Macrófagos/efeitos dos fármacos , Receptores de Superfície Celular/antagonistas & inibidores , Receptores de Superfície Celular/metabolismo , Tiofenos/farmacologiaRESUMO
A tomato saponin, esculeoside A, may be metabolized into various steroidal hormones such as pregnane derivatives that are expected to exhibit various bioactivities in the body, such as anti-osteoporosis, anti-menopausal disorder and anti-tumor actions. Therefore, we attempted to examine the esculeoside A contents of fresh tomatoes, tomatoes boiled in water, tomatoes heated using a microwave oven, freeze-dried tomatoes, and commercially available processed tomato products contained in plastic bottles and cans, in order to develop a health food.
Assuntos
Sapogeninas/química , Solanum lycopersicum/química , Manipulação de Alimentos , Liofilização , Temperatura Alta , Micro-OndasRESUMO
The water extract of Pruni Cortex, which is obtained from the bark of Prunus jamasakura, is a major component in Brocin. We investigated the constituents of the water and methanolic extracts of Pruni Cortex. From the water extractive, two flavonoids (sakuranin and neosakuranin; major constituents of this extractive), four known lignans, and six aromatic compounds including one new compound were obtained. In addition, we also investigated the constituents of the flowers and the leaves of Prunus yedoensis.