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1.
Rev. chil. endocrinol. diabetes ; 14(1): 7-13, 2021. tab, ilus
Article in Spanish | LILACS | ID: biblio-1146465

ABSTRACT

INTRODUCCIÓN: La enfermedad del hígado graso no alcohólico (EHGNA) es la forma más común de enfermedad hepática. A nivel celular se caracteriza por la acumulación de triglicéridos (TG) en forma de gotas lipídicas (GL) dando lugar a esteatosis e inflamación. Entre los factores relevantes para la síntesis de TG se encuentran las enzimas DGAT1/2 que catalizan la etapa final de la síntesis de TG, y la proteína FABP4 que transporta lípidos intracelulares y se expresa en modelos de enfermedad hepática dependiente de obesidad. Por otra parte, TNF-α es una reconocida citoquina involucrada en el proceso inflamatorio en la EHGNA. La medicina popular del norte de Chile ha utilizado la planta Lampaya medicinalis Phil. (Verbenaceae) para el tratamiento de algunas enfermedades inflamatorias. OBJETIVO: Evaluar el efecto de un extracto hidroalcóholico de lampaya (EHL) sobre la esteatosis y expresión de marcadores de inflamación en hepatocitos tratados con ácidos grasos. Diseño experimental: Estudio in vitro en cultivos de la línea celular humana HepG2 tratadas con ácido oleico (AO) y ácido palmítico (AP). MÉTODOS: Se incubó hepatocitos HepG2 con AO/AP por 24 horas en presencia o no de EHL. Se evaluó la presencia de GL y el contenido de TG intracelulares por Oil Red O y Nile Red, respectivamente. La expresión de DGAT1/2, FABP4 y TNF-α fue evaluada por qPCR. RESULTADOS: Los hepatocitos tratados con AO/AP mostraron un aumento en las GL y TG, así como una mayor expresión de DGAT2 en comparación al control. El cotratamiento con EHL revirtió los efectos inducidos por AO/AP. CONCLUSIONES: EHL revierte el incremento en las GL, TG y en la expresión de DGAT2 inducido por AO/AP en células HepG2. Estos hallazgos sugieren un efecto hepatoprotector de la Lampaya contra la esteatosis, y apoyarían su uso complementario en el tratamiento de patologías con componente inflamatorio como la EHGNA.


Non-alcoholic fatty liver disease (NAFLD) is the most common liver disease. At the cellular level, it is characterized by the accumulation of triglycerides (TG) in the form of lipid droplets (LD), which leads to steatosis and inflammation. Among relevant factors for TG synthesis are the enzymes DGAT1/2 catalyzing the final stage of TG synthesis, and the protein FABP4 which transports intracellular lipids and is expressed in cell models of obesity-dependent liver disease. Additionally, TNF-α is a cytokine involved in the inflammatory process associated to NAFDL. Lampaya medicinalis Phil. (Verbenaceae) is a plant used in folk medicine in northern Chile to treat some inflammatory diseases. OBJECTIVE: To evaluate the effect of the hydroalcoholic extract of lampaya (HEL) on steatosis and the expression of inflammatory markers in hepatocytes treated with fatty acids. Study design: In vitro study in cultures of the human HepG2 cell line treated with oleic acid (OA) and palmitic acid (PA). METHODS: HepG2 hepatocytes were incubated with OA/PA for 24 hours in the presence and absence of HEL. The formation of LD and the accumulation of intracellular TG were assessed by Oil Red O and Nile Red, respectively. The expression of DGAT1/2, FABP4 and TNF-α was assessed by qPCR. RESULTS: The treatment with OA/PA increased the levels of LD and TG as well as the expression of DGAT2 in HepG2 hepatocytes compared to control cells. HEL cotreatment counteracted OA/PA-induced effects. CONCLUSIONS: HEL prevents the increase in LD and TG levels and DGAT2 expression induced by OA/PA in HepG2 cells. These findings suggest that lampaya may have a protective effect against hepatic steatosis, which would support its complementary use in the treatment of pathologies associated with inflammation, such as NAFLD.


Subject(s)
Humans , Plant Extracts/pharmacology , Hepatocytes/drug effects , Verbenaceae/chemistry , Non-alcoholic Fatty Liver Disease/drug therapy , Triglycerides/analysis , In Vitro Techniques , Plant Extracts/therapeutic use , Cell Survival , Polymerase Chain Reaction , Cell Culture Techniques , Oleic Acid , Ethanol/chemistry , Hep G2 Cells/drug effects , Inflammation
2.
Biol. Res ; 47: 1-7, 2014. ilus, tab
Article in English | LILACS | ID: lil-710929

ABSTRACT

BACKGROUND: Algesia and inflammation are related with several pathological conditions. It is known that many drugs available for the treatment of these problems cause unwanted side effects. This study was aimed at evaluating acute toxicity and anti-inflammatory activity of Lampaya medicinalis Phil. (Verbenaceae) widely used in the folk medicine of Northern Chile against rheumatism, arthritis and body joints pain. RESULTS: Oral administration of hydroalcoholic extract (HAE) at the highest dose of 3000 mg/ Kg body weight resulted in no mortalities or evidence of significant behavioral changes. Histological examination revealed normal architecture and no significant adverse effects were observed on the liver, kidney, heart, lung or ovaries and testicles. The results suggest that the oral administration of hydroalcoholic extract (HAE) from Lampaya medicinalis did not produce any toxic effect in rats. Hydroalcoholic extract (HAE) significantly inhibited the carrageenan-induced rat paw edema in dose - response relationship, at test doses of 37.5, 75, 150 and 300 mg/Kg body weight. Maximum inhibition (61.98 ± 2.69%) was noted at 300 mg/Kg after 2 h of drug treatment carrageenan induced paw edema, whereas indomethacin produced 47.90 ± 1.16% of inhibition. The inhibitory values of edema at 3 h postcarrageenan were 31.04±0.75%, 40.51 ± 2.36%, 48.97 ± 1.14% and 56.87 ± 0.41% for 37.5, 75, 150, and 300 mg/kg of extract respectively. Indomethacin (10 mg/Kg) gave a percentage inhibition of 49.44 ± 1.44. HAE (300 and 150 mg/kg) induced an anti-inflammatory effect greater than (or comparable) with the effect of indomethacin from 2nd to 4th hours of the experiment. CONCLUSIONS: Our results reveal for first time that compounds contained in the hydroalcoholic extract ofLampaya medicinalis Phil exert anti-inflammatory effect and the oral administration is safe and non toxic up to dose level 3000 mg/kg body weight. The anti-inflammatory activity may be associated with the presence of flavonoids. These findings also justify the traditional use of the plant for treating pain.


Subject(s)
Animals , Female , Male , Anti-Inflammatory Agents/toxicity , Edema/drug therapy , Inflammation/drug therapy , Plant Extracts/toxicity , Verbenaceae , Administration, Oral , Alanine Transaminase/blood , Anti-Inflammatory Agents/isolation & purification , Aspartate Aminotransferases/blood , Chile , Carrageenan/administration & dosage , Heart/drug effects , Hindlimb/injuries , Indomethacin/therapeutic use , Kidney/drug effects , Liquid-Liquid Extraction , Liver/drug effects , Lung/drug effects , Medicine, Traditional , Myocardium , Ovary/drug effects , Plant Extracts/chemistry , Plant Leaves/chemistry , Rats, Sprague-Dawley , Testis/drug effects , Toxicity Tests, Acute/methods
3.
Biol. Res ; 41(2): 151-155, 2008. ilus
Article in English | LILACS | ID: lil-495749

ABSTRACT

The antioxidant properties oí Acantholippia deserticola, a herb used in traditional northern Chilean medicine was studied using free radical - generating systems. The 50 percent aqueous - ethanol extract oí Acantholippia deserticola protected against non-enzymatic lipid peroxidation in microsomal membranes of rat, induced by an Fe++ - ascorbate system and measured spectrophotometrically by the TBARS test, and had strong free radical scavenging capacities on stable ABTS and DPPH radicáis. The results shows that the IC50 valué of the 50 percent aqueous - ethanolic extract oí A.deserticola is 18 ± 0.5 μg/mL in DPPH radical - scavenging, 15 ± 0.8 μg/mL in lipid peroxidation , Total Antioxidant Activity (TAA) is 0.95 mM of Trolox per mg/mL of extract. The total phenolics content of extract is 725 ± 12 mg of gallic acid equivalent per g of dried extract. The results indicate that the 50 percent aqueous - ethanol extract oí Acantholippia deserticola clearly has antioxidant properties.


Subject(s)
Animals , Male , Rats , Antioxidants/isolation & purification , Lipid Peroxidation/drug effects , Plant Extracts/isolation & purification , Verbenaceae/chemistry , Antioxidants/pharmacology , Phenols/isolation & purification , Phenols/pharmacology , Plant Extracts/pharmacology , Rats, Wistar
4.
Mem. Inst. Oswaldo Cruz ; 98(3): 413-418, Apr. 2003. ilus, tab
Article in English | LILACS | ID: lil-340125

ABSTRACT

The anti-Trypanosoma cruzi activity of natural products isolated from Azorella compacta was evaluated, with particular emphasis on their effect against intracellular amastigotes. Five diterpenoids from A. compacta derived from mulinane and azorellane were isolated and identified. Only two products, named azorellanol (Y-2) and mulin-11,3-dien-20-oic acid (Y-5), showed trypanocidal activity against all stages of T. cruzi including intracellular amastigotes. At 10 æM, these compounds displayed a strong lytic activity. It ranged from 88.4 ± 0.6 to 99.0 ± 1 percent for all strains and stages evaluate, with an IC50 /18 h values of 20-84 æM and 41-87 æM, respectively. The development of intracellular amastigotes was also inhibited by nearly 60 percent at 25 æM. The trypanocidal molecules Y-2 and Y-5 did show different degrees of cytotoxicity depending on the cell line tested, with an IC50 /24 h ranging from 33.2 to 161.2 æM. We evaluated the effect of diterpenoids against intracellular T. cruzi forms by immunofluorescent identification of a specific membrane molecular marker (Ssp-4 antigen) of the T. cruzi amastigote forms. The accuracy and reproducibility of the measurements were found to be outstanding when examined by confocal microscopy


Subject(s)
Animals , Bryopsida , Diterpenes , Plant Extracts , Trypanocidal Agents , Trypanosoma cruzi , Cells, Cultured , Diterpenes , Evaluation Study , Lethal Dose 50 , Microscopy, Confocal , Reproducibility of Results , Trypanocidal Agents
5.
Bol. chil. parasitol ; 53(1-2): 9-13, ene.-jun. 1998. ilus, tab
Article in Spanish | LILACS | ID: lil-233091

ABSTRACT

The trypanocidad activity against amastigote forms of SPA-14, Tulahuen and G strains and CL Brener clone of Trypanosoma cruzi of diterpenoids isolated from Azorella compacta. Phil. (Llareta), a plant with ethnomedicinal prestige from prespanish age, was investigated. Amastigocidal activity was shown in azorellanol (2), diterpene isolated by first time, with an inhitory concentration 50 (IC) that varied between 60 M (CL Brener clone) and 84 M (SPA-14 strain), and in mulin -11,13 -dien-20-oico acid (5) with IC between 41 µM (G strain) and 87 mM (CL Brener clone). The cytotoxicity levels of both compounds against Hela and Vero cells and macrophages J144 are lower than nifurtimox and similar to gentian violet


Subject(s)
Humans , Plants, Medicinal/therapeutic use , Trypanosoma cruzi/drug effects , Chagas Disease/drug therapy , Cytotoxicity, Immunologic , Nifurtimox/therapeutic use , Trypanosoma cruzi/pathogenicity
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