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1.
Rev. fitoter ; 17(2): 145-163, dic. 2017. ilus
Artigo em Espanhol | IBECS | ID: ibc-174303

RESUMO

Ganoderma lucidum é um fungo que pertenece ao filo Basidiomycota e à classe Basidiomycetes , que é utilizado há milénios, principalmente na Medicina Tradicional Chinesa. Este cogumelo tem demonstrado inúmeras potencialidades medicinais atribuídas à elevada diversidade de substâncias ativas presentes no basidiocarpo, micélio e esporos, dentro dos quais se destacam polissacáridos de elevado peso molecular, nomeadamente, b-glucanos, e triterpenos, em particular os ácidos ganodéricos. Neste contexto, o presente artigo tem como objetivo fazer uma revisão sobre as potencialidades medicinais deste cogumelo, especialmente o seu papel na imunoestimulação bem como no auxílio à terapêutica de algumas das doenças mais relevantes do presente século (cancro, diabetes mellitus, dislipidémia e inflamação). Pretendeu-se enfatizar aspetos de eficácia dos extratos e constituintes bioativos do cogumelo, incluindo os seus possíveis mecanismos de ação, bem como diversos aspetos de segurança inerentes à sua utilização


Ganoderma lucidum es un hongo que pertenece al filo Basidiomycota y a la clase Basidiomycetes, que se utiliza hace milenios, principalmente en la Medicina Tradicional China. Este hongo ha demostrado innumerables potencialidades medicinales atribuidas a la elevada diversidad de sustancias activas presentes en el basidiocarpo, micelio y esporas, dentro de los cuales se destacan polisacáridos de elevado peso molecular, en particular los b-glucanos, y triterpenos, como los ácidos ganodéricos. En este contexto, el presente artículo tiene como objetivo hacer una revisión sobre las potencialidades medicinales de este hongo, especialmente su papel en la inmunoestimulación así como complemento al tratamiento de algunas de las enfermedades más relevantes del presente siglo (cáncer, diabetes mellitus, dislipemia e inflamación). Se destacan los aspectos de eficacia de los extractos y constituyentes bioactivos del hongo, incluyendo sus posibles mecanismos de acción, así como diversos aspectos de seguridad inherentes a su utilización


Ganoderma lucidum es un hongo que pertenece al filo Basidiomycota y a la clase Basidiomycetes, que se utiliza hace milenios, principalmente en la Medicina Tradicional China. Este hongo ha demostrado innumerables potencialidades medicinales atribuidas a la elevada diversidad de sustancias activas presentes en el basidiocarpo, micelio y esporas, dentro de los cuales se destacan polisacáridos de elevado peso molecular, en particular los b-glucanos, y triterpenos, como los ácidos ganodéricos. En este contexto, el presente artículo tiene como objetivo hacer una revisión sobre las potencialidades medicinales de este hongo, especialmente su papel en la inmunoestimulación así como complemento al tratamiento de algunas de las enfermedades más relevantes del presente siglo (cáncer, diabetes mellitus, dislipemia e inflamación). Se destacan los aspectos de eficacia de los extractos y constituyentes bioactivos del hongo, incluyendo sus posibles mecanismos de acción, así como diversos aspectos de seguridad inherentes a su utilización


Assuntos
Humanos , Reishi , Medicamentos de Ervas Chinesas/uso terapêutico , Dislipidemias/terapia , Inflamação/terapia , Mecanismo de Ação do Medicamento Homeopático , Triterpenos , Polissacarídeo-Liase , Imunização , Diabetes Mellitus/terapia
2.
J. physiol. biochem ; 72(2): 345-352, jun. 2016. tab, graf, ilus
Artigo em Inglês | IBECS | ID: ibc-168278

RESUMO

The aim of this present study was to investigate the effect of ursolic acid (UA) and rosiglitazone (RSG) on insulin sensitivity and proximal insulin signaling pathways in high-fat diet (HFD)-fed C57/BL/6J mice. Male C57BL/6J mice were fed either normal diet or HFD for 10 weeks, after which animals in each dietary group were divided into the following six groups (normal diet, normal diet plus UA and RSG, HFD alone, HFD plus UA, HFD plus RSG, and HFD plus UA and RSG) for the next 5 weeks. UA (5 mg/kg BW) and RSG (4 mg/kg BW) were administered as suspensions directly into the stomach using a gastric tube. The HFD diet elevated fasting plasma glucose, insulin, and homeostasis model assessment index. The expression of insulin receptor substrate (IRS)-1, phosphoinositide 3-kinase (PI3-kinase), Akt, and glucose transporter (GLUT) 4 were determined by Western blot analyses. The results demonstrated that combination treatment (UA/RSG) ameliorated HFD-induced glucose intolerance and insulin resistance by improving the homeostatic model assessment (HOMA) index. Further, combination treatment (UA/RSG) stimulated the IRS-1, PI3-kinase, Akt, and GLUT 4 translocation. These results strongly suggest that combination treatment (UA/RSG) activates IRS-PI3-kinase-Akt-dependent signaling pathways to induce GLUT 4 translocation and increases the expression of insulin receptor to improve glucose intolerance (AU)


No disponible


Assuntos
Animais , Masculino , Diabetes Mellitus Tipo 2/tratamento farmacológico , Resistência à Insulina , Músculo Esquelético , Hipoglicemiantes/uso terapêutico , Triterpenos/uso terapêutico , Tiazolidinedionas/uso terapêutico , Proteínas Substratos do Receptor de Insulina/agonistas , Fármacos Antiobesidade , Antioxidantes/uso terapêutico , Dieta Hiperlipídica/efeitos adversos , Quimioterapia Combinada/efeitos adversos , Ganho de Peso , Obesidade/metabolismo , Camundongos Endogâmicos C57BL , Fosfatidilinositol 3-Quinases/metabolismo
3.
Ars pharm ; 57(2): 55-62, abr.-jun. 2016. ilus, graf
Artigo em Espanhol | IBECS | ID: ibc-156808

RESUMO

Objetivos: Sintetizar conjugados del acetónido de la uridina con triterpenos (colesterol y 3β-5α,8α- endoperoxido-colest-6-en-3-ol) y ácido succínico como puente. Métodos: Se preparó el acetónido de la uridina en acetona mediante catálisis ácida. Se prepararon los succinatos de los esteroles con anhídrido succínico y catalizador nucleofílico 4-N,N-dimetilamino-piridina (DMAP). Los conjugados 1 y 2 se sintetizaron mediante la esterificación de Steglich, con agente de acoplamiento N,N’-diciclohexilcarbodiimida (DCC)y DMAP. Los compuestos se caracterizaron por espectroscopia de RMN (1H RMN y 13C RMN) y espectrometría de masas. Los derivados se evaluaron sobre líneas celulares de ovario de hámster chino (CHO-K1) y de cáncer de mamá (MCF-7). Resultados: Se obtuvieron derivados conjugados del acetónido de la uridina con dos triterpenos con rendimientos superiores al 80%. Los conjugados de uridina con triterpenos no presentaron inhibición significativa de la viabilidad celular sobre las líneas celulares MCF-7 y CHO-K1, tampoco se evidenció una relación dosis-respuesta para los compuestos evaluados. Conclusiones: El método de esterificación con agentes de acoplamiento permitió obtener conjugados de la uridina con triterpenos empleando el ácido succínico como puente. Sin embargo los derivados de uridina obtenidos no presentaron actividad citotóxica significativa (p < 0,05) sobre las líneas celulares evaluadas


Aims: Synthesize of uridine acetonide conjugates with triterpenoids (cholesterol and 3β-5α,8α-endoperoxide- cholest-6-en-3-ol) and succinic acid as linking. Methods: The acetonide derivative of uridine was prepared with acid catalysis in acetone. Sterols succinates were prepared with succinic anhydride and nucleophilic catalyst 4-N,N-dimethylamino-pyridine (DMAP). The conjugates were synthesized by Steglich method with N,N’-dicyclohexylcarbodiimide (DCC) Coupling agent and DMAP. The compounds were characterized by NMR spectroscopy (1H NMR, 13C NMR), and mass spectrometry. The derivatives were assessed in Chinese Hamster Ovary (CHO) and breast cancer (MCF-7) cell lines. Results: The conjugates of uridine acetonide with two triterpenes were obtained with yields higher than 80%. The conjugates prepared don’t showed significant inhibition of cell viability on MCF-7 and CHO cell lines, furthermore these substances did not show a relationship dose-response. Conclusions: The esterification method with coupling agents allowed obtained uridine conjugates with triterpenoids. However the uridine derivatives don’t showed significant cytotoxic activity (p < 0,05) against cell lines evaluated


Assuntos
Humanos , Feminino , Uridina/farmacologia , Uridina/toxicidade , Triterpenos/farmacologia , Triterpenos/toxicidade , Neoplasias da Mama/tratamento farmacológico , Ácido Succínico/toxicidade , Ácido Succínico/uso terapêutico , Microanálise por Sonda Eletrônica/instrumentação , Nucleosídeos/toxicidade , Nucleosídeos/uso terapêutico , Análise de Variância
4.
Nutr. hosp ; 32(1): 242-249, jul. 2015. tab
Artigo em Espanhol | IBECS | ID: ibc-141366

RESUMO

Objetivo: evaluar el posible efecto hipotensor en sujetos pre-hipertensos e hipertensos, de un extracto de hoja de olivo (EHO) estandarizado al 15% (m/m) en oleoeuropeína y con un contenido medio del 10% (m/m) en ácidos triterpénicos y del 1% (m/m) en hidroxitirosol. Asimismo, se ha valorado su acción sobre el estatus antioxidante y el perfil lipídico sanguíneos. Material y métodos: se ha llevado a cabo un ensayo de intervención en humanos con administración de 1.600 mg de extracto/día. Los parámetros evaluados han sido presión sistólica y diastólica, retardo de la oxidación del colesterol LDL (lag time) y niveles sanguíneos de óxido nítrico (NO), malondialdehído (MDA), capacidad antioxidante (CAO), perfil lipídico, glucosa, transaminasas y creatinina. Resultados: se observó en todos los sujetos una disminución estadísticamente significativa de la presión sistólica y diastólica, y un aumento de los niveles de NO (P<0,050). En los sujetos con presión sistólica más elevada también se redujo significativamente su valor tras la intervención (P=0,002). El «lag time» de las LDL aumentó significativamente (P=0,047), y en todos los sujetos los niveles de colesterol (CHO) se redujeron significativamente. Los niveles de colesterol LDL, triglicéridos (TG) y del índice CHO/colesterol HDL disminuyeron con tendencia a la significancia (P=0,076; P=0,059; P=0,056; respectivamente). Conclusión: este estudio, aunque preliminar, pone de relieve por primera vez la influencia positiva del EHO ensayado en la regulación de la hipertensión así como en la velocidad de oxidación de las LDL y en el perfil lipídico sanguíneo (AU)


Objective: to evaluate the possible hypotensive effect in pre-hypertensive and hypertensive subjects of an olive leaf extract (OLE) standardized to 15% (w/w) in oleoeuropein, and with a 10% (w/w) mean content of triterpenic acids and 1% (w/w) in hydroxytirosol. Moreover, the possible effects on the blood antioxidant status and lipid profile have been also evaluated. Materials and methods: this interventional study has been performed in human volunteers, to whom 1600 mg OLE/days, was administered. The analyzed parameters at the beginning and end of the study were diastolic and systolic pressure, delay in the LDL-cholesterol oxidation «lag time» and blood levels of nitric oxide (NO), malonic dialdehyde (MDA), antioxidant capacity (AOC) lipid profile, glucose, transaminases and creatinine. Results: a decrease in the diastolic and systolic pressure, and an increase in the NO values all statistically significant (CHO) for all volunteers, was found. In volunteers with higher systolic pressure their levels were also significantly diminished after the intervention trial (P=0,002). The LDL lag time increased significantly (P=0,047). Additionally, in all volunteers CHO levels were significantly decreased, and those of LDL cholesterol, triglycerides (TG) and the CHO/HDL cholesterol ratio were diminished with a tendency to the significance (P=0,076; P=0,059; P=0,056; respectively). Conclusions: this preliminary study reports by the first time the positive influence of the OLE assayed in the regulation of the hypertension, LDL lag time and blood lipid profile. Therefore, further studies are of great interest (AU)


Assuntos
Humanos , Compostos Fitoquímicos/farmacocinética , Hipertensão/tratamento farmacológico , Anti-Hipertensivos/farmacocinética , Extratos Vegetais/farmacocinética , Folhas de Planta , Olea , Triterpenos/farmacocinética
5.
J. physiol. biochem ; 69(4): 687-695, dic. 2013.
Artigo em Inglês | IBECS | ID: ibc-121628

RESUMO

Hepatocellular carcinoma is one of the leading causes of death in cancer and yet no drug has proven to be a successful candidate for its treatment in advanced stages. Ursolic acid stearoyl glucoside (UASG) is a newly discovered triterpene in Lantana camara and there lies a possibility that it possess anti-hepatocellular carcinoma property. In the present study, we induced hepatocellular carcinoma in Wistar rats by diethylnitrosamine (DENA) and treated it with ursolic acid stearoyl glucoside. The ability to treat hepatocellular carcinoma was measured by comparing biochemical serum markers such as serum alanine aminotransferase, serum aspartate aminotransferase, serum alkaline phosphatase, and the specific marker for hepatocellular carcinoma, alpha fetoprotein. The histological studies of the livers were also performed. The results have shown significant elevated levels of these parameters as compared to normal control and the drug receiving groups have shown significant reduction in these marker levels. Histopathological studies also indicated the reduced liver damage in drug-treated groups. It was noted that a significant and dose-dependent reversal of DENA-diminished activity of antioxidant enzymes like superoxide dismutase, catalase, glutathione peroxidase, glutathione transferase, and the reduced DENA-elevated level of lipid peroxidation (LPO) with a marked change. UASG significantly suppressed free radical formation by scavenging the hydroxyl radicals. It also modulates the levels of LPO and markedly increases the endogenous antioxidant enzymes level in DENA-induced hepatocellular carcinogenesis (AU)


Assuntos
Animais , Ratos , Anticarcinógenos/farmacocinética , Carcinoma Hepatocelular/prevenção & controle , Triterpenos/farmacocinética , Substâncias Protetoras/farmacocinética , Modelos Animais de Doenças , Alanina Transaminase , Peróxidos Lipídicos/metabolismo
6.
Rev. fitoter ; 8(2): 135-146, jul.-dic. 2008. tab, ilus
Artigo em Espanhol | IBECS | ID: ibc-132780

RESUMO

Ganoderma lucidum (Leyss. ex Fr.) Karst. (Poliporáceas) es conocido con el nombre de Lingzhi en China y Reishi en Japón. Tradicionalmente se ingiere la infusión del carpóforo para mejorar la salud, aumentar la longevidad y para la prevención y/o tratamiento de hepatitis, bronquitis crónica, gastritis, crecimientos tumorales y trastornos inmunológicos. Existen dos grupos principales de compuestos: los triterpenos y los polisacáridos, junto a derivados esteroídicos, lectinas y análogos de la adenosina. Entre las propiedades demostradas en los estudios experimentales destacan las anticancerosas, inmunomoduladoras, antiinflamatorias, hipoglucemiantes, hipolipemiantes y hepatoprotectoras. En general se relaciona la actividad anticancerosa con el contenido en triterpenos, y las propiedades inmunomoduladoras con los polisacáridos. Algunos ensayos clínicos postulan el uso de G. lucidum para potenciar las defensas inmunológicas de pacientes con cáncer, especialmente en combinación con los tratamientos quimioterápicos y/o radioterápicos, aunque el número de estudios es limitado (AU)


Ganoderma lucidum (Leyss. ex Fr.) Karst. (Polyporaceae), known as Lingzhi in China and Reishi in Japan, is usually used in infusions of carpophores for improving health and longevity and for preventing and/or treating hepatitis, chronic, gastritis, tumour growth and immunological troubles. Contains two relevant groups of compounds, triterpenes and polysaccharides, together with steroids, lectins and adenosine analogues. Among its demonstrated pharmacological properties, ganoderma’s anticancer, immunomodulatory, anti-inflammatory, hypoglycaemic, hypolipidemic and hepatoprotective properties stand out. Various pharmacological studies have demonstrated the relationship between the plant’s anticancer properties and its triterpene content, while its immunological properties have generally been associated with its polysaccharide components. Several clinical trials have also shown the potential usefulness of G. lucidum as immunostimulant in patients undergoing chemotherapy or anticancer drug treatment, but the number of trials is limited (AU)


Assuntos
Humanos , Masculino , Feminino , Reishi/metabolismo , Antineoplásicos/uso terapêutico , Fatores Imunológicos/uso terapêutico , Triterpenos , Adjuvantes Imunológicos/uso terapêutico , Reishi/química , Medicamentos de Ervas Chinesas/uso terapêutico , Polissacarídeos/uso terapêutico , Medicamentos de Ervas Chinesas/classificação , Medicamentos de Ervas Chinesas/história
7.
Int. microbiol ; 4(2): 93-102, jun. 2001. tab, ilus
Artigo em Inglês | IBECS | ID: ibc-163499

RESUMO

Echinocandins, the lipopeptide class of glucan synthase inhibitors, are an alternative to ergosterol-synthesis inhibitors to treat candidiasis and aspergillosis. Their oral absorption, however, is low and they can only be used parenterally. During a natural product screening program for novel types of glucan synthesis inhibitors with improved bioavailability, a fungal extract was found that inhibited the growth of both a wild-type Saccharomyces cerevisiae strain and the null mutant of the FKS1 gene (fks1::HIS). The mutant strain was more sensitive to growth inhibition, suggesting that the fungal extract could contain an inhibitor of glucan synthesis. A novel acidic steroid, named arundifungin, was purified from a fungal extract obtained from a liquid culture of Arthrinium arundinis collected in Costa Rica. Arundifungin caused the same pattern of hallmark morphological alterations in Aspergillus fumigatus hyphae as echinocandins, further supporting the idea that arundifungin belongs to a new class of glucan synthesis inhibitors. Moreover, its antifungal spectrum was comparable to those of echinocandins and papulacandins, preferentially inhibiting the growth of Candida and Aspergillus strains, with very poor activity against Cryptococcus. Arundifungin was also detected in nine other fungal isolates which were ecologically and taxonomically unrelated, as assessed by sequencing of the ITS1 region. Further, it was also found in two more Arthrinium spp from tropical and temperate regions, in five psychrotolerant conspecific isolates collected on Macquarie Island (South Pacific) and belonging to the Leotiales, and in two endophytes collected in central Spain (a sterile fungus belonging to the Leotiales and an undetermined coelomycete) (AU)


No disponible


Assuntos
Fungos/classificação , Fungos , Antifúngicos/farmacologia , Proteínas de Membrana , Triterpenos , Proteínas de Schizosaccharomyces pombe , Fungos/metabolismo , Antifúngicos/química , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Terpenos/química , Terpenos/farmacologia
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