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Article in Chinese | WPRIM | ID: wpr-921770


At present, 141 compounds have been isolated from Picrorhiza scrophulariiflora and P. kurroa of the Scrophulariaceae plants, including 46 iridoid glycosides, 29 tetracyclic triterpenoids, 25 phenylpropanoids, and 11 phenylethanoid glycosides. Pharmacological studies have demonstrated that they have liver-, heart-, brain-, kidney-, and nerve cells-protecting effects as well as anti-tumor, anti-inflammatory, anti-bacterial, anti-asthma, anti-diabetic, immunomodulatory, and blood lipid-lowering activities. This article reviews the chemical components and pharmacological activities of P. scrophulariiflora and P. kurroa, aiming to provide a basis for the in-depth research, development, and utilization of the two plants.

Iridoid Glycosides , Picrorhiza , Triterpenes/pharmacology
Frontiers of Medicine ; (4): 79-90, 2021.
Article in English | WPRIM | ID: wpr-880969


Natural killer (NK) cells, a type of cytotoxic lymphocytes, can infiltrate into ischemic brain and exacerbate neuronal cell death. Astragaloside IV (ASIV) is the major bioactive ingredient of Astragalus membranaceus, a Chinese herbal medicine, and possesses potent immunomodulatory and neuroprotective properties. This study investigated the effects of ASIV on post-ischemic brain infiltration and activation of NK cells. ASIV reduced brain infarction and alleviated functional deficits in MCAO rats, and these beneficial effects persisted for at least 7 days. Abundant NK cells infiltrated into the ischemic hemisphere on day 1 after brain ischemia, and this infiltration was suppressed by ASIV. Strikingly, ASIV reversed NK cell deficiency in the spleen and blood after brain ischemia. ASIV inhibited astrocyte-derived CCL2 upregulation and reduced CCR2

Animals , Brain , Histone Deacetylases , Killer Cells, Natural , Rats , Saponins/pharmacology , Triterpenes/pharmacology
Article in Chinese | WPRIM | ID: wpr-878984


One new and two known dammarane-type saponins were isolated from the leaves of Gynostemma pentaphyllum using various chromatographic methods. Their structures were identified by HR-ESI-MS,~( 1)H-NMR, ~(13)C-NMR, 2 D-NMR spectra as 2α,3β,12β,20,24(S)-tetrahdroxydammar-25-en-3-O-[β-D-glucopyranosyl(1→2)-β-D-glucopyranosyl]-20-O-β-D-xylopyranosyl(1→6)-β-D-glucopyranoside(1, a new compound, namely gypenoside J5) and 2α,3β,12β,20,24(R)-tetrahdroxydammar-25-en-3-O-[β-D-glucopyranosyl(1→2)-β-D-glucopyranosyl]-20-O-β-D-xylopyranosyl(1→6)-β-D-glucopyranoside(2) and 2α,3β,12β,20-tetrahydroxy-25-hydroperoxy-dammar-23-en-3-O-[β-D-glucopyranosyl(1→2)][β-D-glucopyranosyl]-20-O-[β-D-xylopyranosyl(1→6)]-β-D-glucopy-ranoside(3), respectively. Compounds 1 and 2 were a pair of C-24 epimers. All compounds showed weak cytotoxicity agxinst H1299, HepG2, PC-3, SH-SY5 Y cancer cell lines. However, they exerted protective effect against SH-SY5 Y cellular damage induced by H_2O_2 dose-dependently, of which compound 1 displayed the strongest antioxidant effect. The present study suggested that G. pentaphyllum has antioxidative potential and the saponins from G. pentaphyllum are considered as the active compounds with neuroprotecitve effect.

Gynostemma , Molecular Structure , Neuroprotective Agents/pharmacology , Saponins/pharmacology , Triterpenes/pharmacology
Article in Chinese | WPRIM | ID: wpr-879092


Chemical constituents were isolated and purified from fruiting bodies of Ganoderma calidophilum by various column chromatographic techniques, and their chemical structures were identified through combined analysis of physicochemical properties and spectral data. As a result, 11 compounds were isolated and identified as(24E)-lanosta-8,24-dien-3,11-dione-26-al(1), ganoderone A(2), 3-oxo-15α-acetoxy-lanosta-7,9(11), 24-trien-26-oleic acid(3),(23E)-27-nor-lanosta-8,23-diene-3,7,25-trione(4), ganodecanone B(5), ganoderic aldehyde A(6), 11β-hydroxy-lucidadiol(7), 3,4-dihydroxyacetophenone(8), methyl gentiate(9), ganoleucin C(10), ganotheaecolumol H(11). Among them, compound 1 is a new triterpenoid. The cytotoxic activities of all of the compounds against tumor cell lines were evaluated. The results showed that compounds 1, 3, 4 and 6 showed cytotoxic activity against BEL-7402, with IC_(50) values of 26.55, 11.35, 23.23, 18.66 μmol·L~(-1); compounds 1 and 3-6 showed cytotoxic activity against K562, with IC_(50) values of 5.79, 22.16, 12.16, 35.32, and 5.59 μmol·L~(-1), and compound 4 showed cytotoxic activity against A549, with IC_(50) value of 42.50 μmol·L~(-1).

Cell Line, Tumor , Fruiting Bodies, Fungal , Ganoderma , Molecular Structure , Triterpenes/pharmacology
Bol. latinoam. Caribe plantas med. aromát ; 18(4): 347-358, jul. 2019. ilus
Article in English | LILACS | ID: biblio-1008172


Manilkara zapota (Sapotaceae), commonly known as Sapodilla, is widely known for its delicious fruit. Various parts of this plant are also used in folk medicine to treat a number of conditions including fever, pain, diarrhoea, dysentery, haemorrhage and ulcers. Scientific studies have demonstrated analgesic, anti-inflammatory, antioxidant, cytotoxic, antimicrobial, antidiarrheal, anti-hypercholesteremic, antihyperglycemic and hepatoprotective activities in several parts of the plant. Phytochemical studies have revealed the presence of phenolic compounds including protocatechuic acid quercitrin, myricitrin, catechin, gallic acid, vanillic acid, caffeic acid, syringic acid, coumaric acid, ferulic acid, etc. as main constituents of the plant. Several fatty acids, carotenoids, triterpenes, sterols, hydrocarbons and phenylethanoid compounds have also been isolated from M. zapota. The present review is a comprehensive description focused on pharmacological activities and phytochemical constituents of M. zapota.

Manilkara zapota (Sapotaceae), comúnmente conocida como Sapodilla, es ampliamente conocida por su delicioso fruto. Variadas partes de esta planta se usan en medicina popular para tratar una serie de afecciones, como fiebre, dolor, diarrea, disentería, hemorragia y úlceras. Estudios científicos han demostrado actividad analgésica, antiinflamatoria, antioxidante, citotóxica, antimicrobiana, antidiarreica, antihipercolesterolémica, antihiperglucémica y hepatoprotectora en diferentes partes de la planta. Los estudios fitoquímicos han revelado la presencia de compuestos fenólicos que incluyen ácido protocatechúico, quercitrina, miricitrina, catequina, ácido galico, ácido vanílico, ácido cafeico, ácido sirínico, ácido cumárico, ácido fúnico y ácido ferúlico como componentes principales de la planta. Varios ácidos grasos, carotenoides, triterpenos, esteroles, hidrocarburos y compuestos feniletanoides también han sido aislados de M. zapota. La presente revisión es una descripción exhaustiva centrada en las actividades farmacológicas y los constituyentes fitoquímicos de M. zapota.

Plant Extracts/pharmacology , Manilkara/chemistry , Phenols/isolation & purification , Phenols/pharmacology , Saponins/isolation & purification , Saponins/pharmacology , Sterols/isolation & purification , Sterols/pharmacology , Triterpenes/isolation & purification , Triterpenes/pharmacology , Carotenoids/isolation & purification , Carotenoids/pharmacology , Sapotaceae/chemistry , Phenolic Compounds/analysis , Medicine, Traditional
Braz. oral res. (Online) ; 33: e032, 2019. tab, graf
Article in English | LILACS | ID: biblio-1001608


Abstract: This study aimed to investigate the effects of astragaloside IV (AsIV) on inflammation and immunity in rats with experimental periodontitis. Periodontitis was established in 48 Wistar rats, which were then randomly divided into model and 10, 20 and 40 mg/kg AsIV groups, with 12 rats in each group. The latter 3 groups were treated with AsIV at doses of 10, 20 and 40 mg/kg, respectively. The control group (12 rats, without periodontitis) and model group were given the same amount of 5% sodium carboxymethyl cellulose. The treatment was performed once per day for 8 weeks. Before and after treatment, the tooth mobility scores of the rats were determined. After treatment, the salivary occult blood index (SOBI), plaque index (PLI), peripheral blood T lymphocyte subsets, and serum inflammatory factor and immunoglobulin levels were determined. The results showed that, after treatment, compared with that in model group, in 40 mg/kg AsIV group, the general state of rats was improved, while the tooth mobility score, SOBI and PLI were significantly decreased (p < 0.05); the peripheral blood CD4+ T cell percentage and CD4+/CD8+ ratio were significantly increased (p < 0.05), while the CD8+ T cell percentage was significantly decreased (p < 0.05); the serum tumor necrosis factor-α, interleukin-1β and interleukin-2 levels were significantly decreased (p < 0.05); the serum immunoglobulin A and immunoglobulin G levels were significantly decreased (p < 0.05). In conclusion, AsIV can alleviate inflammation and enhance immunity in rats with experimental periodontitis.

Animals , Male , Female , Periodontitis/drug therapy , Saponins/pharmacology , Triterpenes/pharmacology , Immune System/drug effects , Periodontitis/immunology , Periodontitis/pathology , Reference Values , Tooth Mobility , Immunoglobulins/blood , Random Allocation , Reproducibility of Results , T-Lymphocyte Subsets , Interleukin-2/blood , Tumor Necrosis Factor-alpha/blood , Treatment Outcome , Rats, Wistar , Interleukin-1beta/blood
Acta cir. bras ; 34(7): e201900708, 2019. tab, graf
Article in English | LILACS | ID: biblio-1038121


Abstract Purpose: To investigate the effect of astragaloside IV (As-IV) on myocardial ischemia-reperfusion (I/R) injury in rats and reltaed mechanisms. Methods: Sixty rats were randomly divided into sham-operated, control I/R and 2.5, 5 and 10 mg/kg As-IV groups, 12 rats in each group. The later three groups were intragastrically administered with As-IV for 7 days, with a dose of 2.5, 5 and 10 mg/kg, respectively. The myocardial I/R injury model was constructed in later four groups. At the end of reperfusion, the cardiac function indexes, serum lactate dehydrogenase (LDH) and creatine kinase (CK) levels, heart weight (HW)/body weight (BW) ratio and infarct size, and expressions of phosphatidylinositol-3 kinase/serine-threonine protein kinase (PI3K/AKT) and glycogen synthase kinase-3β (GSK-3β) proteins and the phosphorylated forms (p-AKT, p-GSK-3β) were determined. Results: Compared with control I/R group, in 5 and 10 mg/kg As-IV groups the left ventricular systolic pressure, fractional shortening and ejection fraction were increased, the left ventricular end-diastolic pressure was decreased, the serum LDH and CK levels were decreased, the HW/BW ratio and myocardial infarct size were decreased, and the p-Akt/Akt ratio and p-GSK-3β/GSK-3β ratio were increased (all P < 0.05). Conclusion: As-IV can alleviate the myocardial I/R injury in rats through regulating PI3K/AKT/GSK-3β signaling pathways.

Animals , Male , Rats , Saponins/pharmacology , Triterpenes/pharmacology , Myocardial Reperfusion Injury/prevention & control , Signal Transduction/drug effects , Phosphatidylinositol 3-Kinases/metabolism , Proto-Oncogene Proteins c-akt/metabolism , Glycogen Synthase Kinase 3 beta/metabolism , Phosphorylation , Myocardial Reperfusion Injury/drug therapy , Rats, Sprague-Dawley
An. acad. bras. ciênc ; 89(3): 1369-1379, July-Sept. 2017. tab, graf
Article in English | LILACS | ID: biblio-886755


ABSTRACT Natural steroids and triterpenes such as b-sitosterol, stigmasterol, lupeol, ursolic and betulinic acids were transformed into its hexanoic and oleic esters, to evaluate the influence of chemical modification towards the cytotoxic activities against tumor cells. The derivatives were evaluated against five tumor cell lines [OVCAR-8 (ovarian carcinoma); SF-295 (glioblastoma); HCT-116 (colon adenocarcinoma); HL-60 (leukemia); and PC-3 (prostate carcinoma)] and the results showed only betulinic acid hexyl ester exhibits cytotoxic potential activity.

Humans , Triterpenes/pharmacology , Lamiaceae/chemistry , Pentacyclic Triterpenes/pharmacology , Fabaceae/chemistry , Antineoplastic Agents/pharmacology , Triterpenes/isolation & purification , Triterpenes/chemistry , Drug Screening Assays, Antitumor , Lamiaceae/classification , Inhibitory Concentration 50 , Cell Line, Tumor , Esters , Pentacyclic Triterpenes/isolation & purification , Pentacyclic Triterpenes/chemistry , Fabaceae/classification , Antineoplastic Agents/isolation & purification , Antineoplastic Agents/chemistry
Bol. latinoam. Caribe plantas med. aromát ; 14(5): 403-422, Sept. 2015. ilus, tab
Article in English | LILACS | ID: biblio-907502


In addition to eucalyptin the methanol extract from leaves of Eucalyptus citriodora (Myrtaceae) afforded the known compounds apigenin, chrysin, luteolin, naringenin, quercetin; together with betulinic acid, oleanolic, ursolic acid, and two remaining complex mixtures of unidentified flavonoids and triterpenes. These compounds together with triterpenes mixtures, hexane and ethyl acetate extracts showed antifeedant, insecticidal and insect growth regulatory activities against fall armyworm [Spodoptera frugiperda JE Smith (Lepidoptera: Noctuidae)] an important pest of corn, and yellow mealworm [Tenebrio molitor (Coleoptera:Tenebrionidae)] a pest of stored grains. The most active compounds were chrysin, eucalyptin, quercetin, luteolin, and betulinic and oleanolic acids and the mixtures of flavonoids and triterpenes (M1 and M2). These compounds and mixtures had IGR activity between 0.2 to 5.0 ug/mL and insecticidal effects between 5.0 and 10.0 μg/mL.The extracts were insecticidal to larvae, with lethal doses between 20-100 ug/mL. These compounds appear to have selective effects on the pre-emergence metabolism of the Lepidoptera, since in all treatments of the larvae of S. frugiperda the pupation was shortened and this process showed precociousness in relation to control. Thus, these substances may be useful as potential natural insecticidal agents.

Extracto metanolico de hojas de Eucalyptus citriodora (Myrtaceae) proporcionó además de eucalyptin, flavonoides tales como apigenina, crisina, luteolina, naringenina, quercetina; los triterpenos, ácido oleanólico, ácido ursólico betulínico, y dos mezclas complejas de flavonoides y triterpenos no identificados M1 y M2. Los flavonoides, triterpenos y mezclas de triterpenos, extractos de acetato de etilo y hexano mostraron efectos antialimentarios, insecticida y actividad reguladora de crecimiento (IGR) frente al gusano cogollero [Spodoptera frugiperda JE Smith (Lepidoptera: Noctuidae)], una plaga importante del maíz y frente al gusano de la harina [Tenebrio molitor (Coleoptera: Tenebrionidae)], una plaga de los granos almacenados. Los compuestos más activos fueron crisina, eucalyptin, quercetina, luteolina, ácido betulínico y ácido oleanólico y las mezclas de flavonoides y triterpenos (M1 y M2). Estos compuestos y mezclas mostraron actividad IGR entre 0,2 y 5,0 ug/mL y efectos insecticidas entre 5,0 y 10,0 μg/mL. Los extractos mostraron carácter insecticida para las larvas a dosis letales entre 20-100 ug/mL. Estas muestras parecen tener efectos selectivos sobre el metabolismo de pre-emergencia de los lepidópteros, ya que en todos los tratamientos de las larvas de S. frugiperda el tiempo de la pupación se acortó; este proceso muestra precocidad en relación con el control, las substancias ensayadas en este trabajo pueden ser útiles como potenciales agentes insecticidas naturales.

Coleoptera , Eucalyptus/chemistry , Insecticides/pharmacology , Plant Extracts/pharmacology , Spodoptera , Coleoptera/growth & development , Flavonoids/pharmacology , Methanol , Myrtaceae/chemistry , Spodoptera/growth & development , Triterpenes/pharmacology
Braz. j. microbiol ; 46(2): 613-617, Apr-Jun/2015. tab, graf
Article in English | LILACS | ID: lil-749716


In this study, we revealed that OA and UA significantly inhibited the expression of most genes related to peptidoglycan biosynthesis in S. mutans UA159. To the best of our knowledge, this is the first report to introduce the antimicrobial mechanism of OA and UA against S. mutans.

Anti-Bacterial Agents/pharmacology , Biosynthetic Pathways/drug effects , Biosynthetic Pathways/genetics , Oleanolic Acid/pharmacology , Peptidoglycan/biosynthesis , Streptococcus mutans/drug effects , Triterpenes/pharmacology , Gene Expression Regulation, Bacterial/drug effects
Bol. latinoam. Caribe plantas med. aromát ; 14(3): 179-189, mayo 2015. tab, ilus
Article in English | LILACS | ID: biblio-907483


Seven compounds were isolated from the methanol extract of leaves of Ziziphus mauritiana. The structures of the isolated compounds were elucidated as y-fagarine (1), beta-sitosterol (2), stigmasterol (3), alfa-amyrin (4), lupeol (5), beta-amyrin (6) and betulin (7) by extensive spectroscopic studies and by co-TLC with authentic samples. This is the first report of isolation of compounds 1-7 from this plant species. The extractives from leaves were investigated for thrombolytic, membrane stabilizing, antimicrobial, antidiarrheal and analgesic potentials along with sleep inducing property on animal model. The thrombolytic and membrane stabilizing activities were assessed by using human erythrocyte comparing with standard streptokinase and acetylsalicylic acid, respectively. The methanolic extract reduced frequency of diarrheal faeces when compared to the standard loperamide. In castor oil induced diarrhea in mice a dose dependent decrease of gastrointestinal transits were observed. In radiant heat tail-flick method the methanol extract showed moderate antinociceptive activity, compared to standard morphine.

Siete compuestos fueron aislados del extracto metanólico de hojas de Ziziphus mauritiana. Las estructuras de los compuestos aislados fueron identificadas como y-fagarina (1), beta-sitosterol (2), estigmasterol (3), alfa-amirina (4), lupeol (5), beta-amirina (6) y betulina (7 ) por medio de extensivos estudios espectroscópicos y por co-TLC con muestras auténticas. Este es el primer informe de aislamiento de los compuestos 1-7 a partir de esta especie vegetal. Los extractos de las hojas fueron investigados por efectos trombolíticos, estabilizadores de membrana, antimicrobianos, antidiarreicos y potenciales analgésicos junto a la propiedad de inducir sueño en el modelo animal. Las actividades trombolíticos y la estabilización de la membrana se evaluaron mediante el uso de eritrocitos humanos comparando con estreptoquinasa estándar y el ácido acetilsalicílico, respectivamente. El extracto metanólico redujo la frecuencia de las heces diarreicas en comparación con el estándar de loperamida. En la inducción por aceite de ricino de diarrea en ratones, se observó una disminución dosis dependiente de los tránsitos gastrointestinales. En el método del coletazo producido por calor radiante, el extracto metabólico mostró una actividad antinociceptiva moderada, en comparación con la morfina estándar.

Animals , Mice , Rats , Anti-Infective Agents/pharmacology , Antidiarrheals/pharmacology , Plant Leaves/chemistry , Triterpenes/pharmacology , Ziziphus/chemistry , Fibrinolytic Agents/pharmacology , Methanol , Triterpenes/isolation & purification
Electron. j. biotechnol ; 18(2): 88-95, Mar. 2015. graf, tab
Article in English | LILACS | ID: lil-745575


Background Triterpenoids are multifunctional secondary metabolites in plants. But little information is available concerning the actual yield, optimal extraction method and pharmacologic activity with regard to triterpenoids from Jatropha curcas leaves (TJL). Hence, response surface methodology (RSM) was used to optimize the extraction parameters. The effects of three independent variables, namely liquid-to-solid ratio, ethanol concentration and extraction time on TJL yield were investigated. TJL obtained by silica column chromatography was tested against bacterial and fungal species relevant to oral disease and wounds through broth microdilution. Antioxidant activity was assessed using the 2,2-diphenyl-2-picrylhydrazyl and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) assays. Results A second order polynomial model produced a satisfactory fitting of the experimental data with regard to TJL yield (R2 = 0.983, P < 0.01). The optimum extraction conditions were 16 mL/g (liquid-to-solid ratio), 70% (ethanol concentration) and 50 min (extraction time). Predicted values agreed well with the experimental values. TJL had extraordinarily strong antibacterial and antifungal activities (24.42 µg/mL < MIC < 195.31 µg/mL) against all the tested human pathogens except Bacteroides vulgatus (390.62 µg/mL) and Bacteroides stercoris (781.25 µg/mL). The DPPH and ABTS assays revealed a moderate antioxidant activity of TJL compared with ascorbic acid. Conclusion These results provided reliable scientific basis for further investigation of triterpenoids from J. curcas.

Triterpenes/analysis , Triterpenes/pharmacology , Jatropha/chemistry , Anti-Infective Agents/pharmacology , Anti-Inflammatory Agents/pharmacology , Time Factors , Bacteria/drug effects , Ultrasonics , Free Radical Scavengers , Ethanol/analysis , Fungi/drug effects
Rev. bras. cir. cardiovasc ; 30(1): 33-39, Jan-Mar/2015. tab
Article in English | LILACS | ID: lil-742888


Introduction: The knowledge of the prevalence of risk factors and comorbidities, as well as the evolution and complications in patients undergoing coronary artery bypass graft allows comparison between institutions and evidence of changes in the profile of patients and postoperative evolution over time. Objective: To profile (risk factors and comorbidities) and clinical outcome (complications) in patients undergoing coronary artery bypass graft in a national institution of great surgical volume. Methods: A retrospective cohort study of patients undergoing coronary artery bypass graft in the hospital Beneficência Portuguesa de São Paulo, from July 2009 to July 2010. Results: We included 3,010 patients, mean age of 62.2 years and 69.9% male. 83.8% of patients were hypertensive, 36.6% diabetic, 44.5% had dyslipidemia, 15.3% were smokers, 65.7% were overweight/obese, 29.3% had a family history of coronary heart disease. The expected mortality calculated by logistic EuroSCORE was 2.7%. The isolated CABG occurred in 89.3% and 11.9% surgery was performed without cardiopulmonary bypass. The most common complication was cardiac arrhythmia (18.7%), especially acute atrial fibrillation (14.3%). Pneumonia occurred in 6.2% of patients, acute renal failure in 4.4%, mediastinites in 2.1%, stroke in 1.8% and AMI in 1.2%. The in-hospital mortality was 5.4% and in isolated coronary artery bypass graft was 3.5%. The average hospital stay was 11 days with a median of eight days (3-244 days). Conclusion: The profile of patients undergoing coronary artery bypass graft surgery in this study is similar to other published studies. .

Introdução: O conhecimento da prevalência dos fatores de risco e comorbidades, bem como a evolução com complicações nos pacientes submetidos à cirurgia de revascularização miocárdica, permite a comparação entre instituições e a comprovação de modificações no perfil de pacientes e na evolução pós-operatória ao longo do tempo. Objetivo: Conhecer o perfil (fatores de risco e comorbidades) e a evolução clínica (complicações) nos pacientes submetidos à cirurgia de revascularização miocárdica em uma instituição nacional de grande volume cirúrgico. Métodos: Estudo de coorte retrospectivo de pacientes submetidos ao procedimento de cirurgia de revascularização miocárdica no Hospital Beneficência Portuguesa de São Paulo, no período de julho de 2009 a julho de 2010. Resultados: Foram incluídos 3010 pacientes, com idade média de 62,2 anos e 69,9% do sexo masculino. 82,8% dos pacientes eram hipertensos, 36,6% diabéticos, 44,5% dislipidêmicos, 15,3% tabagistas, 65,7% com sobrepeso/obesidade e 29,3% tinham antecedentes familiares de doença coronária. A mortalidade média esperada calculada pelo EuroSCORE logístico foi de 2,7%. A cirurgia de revascularização miocárdica isolada ocorreu em 89,3% e em 11,9% foi realizada cirurgia sem circulação extracorpórea. A complicação mais comum foi arritmia cardíaca (18,7%), especialmente a fibrilação atrial aguda (14,3%). Pneumonia ocorreu em 6,2% dos pacientes, lesão renal aguda em 4,4%, mediastinite em 2,1%, acidente vascular encefálico em 1,8% e infarto agudo do miocárdio em 1,2%. A mortalidade intra-hospitalar foi de 5,4% e na cirurgia de revascularização miocárdica isolada foi de 3,5%. O tempo de permanência hospitalar médio foi de 11 dias, com mediana de oito dias (3 - 244 dias). Conclusão: O perfil dos pacientes submetidos à cirurgia de revascularização miocárdica neste estudo assemelha-se ao de outros estudos publicados. .

Animals , Humans , Mice , Gene Expression Profiling , Muscle, Skeletal/pathology , Muscular Atrophy/genetics , Triterpenes/pharmacology , Cell Line , Fasting , Gene Expression Regulation , Gene Expression/drug effects , Hindlimb/innervation , Insulin-Like Growth Factor I/metabolism , Insulin/metabolism , Muscle Denervation , Muscle Fibers, Skeletal/drug effects , Muscle Fibers, Skeletal/metabolism , Muscle Strength/drug effects , Muscle, Skeletal/drug effects , Muscle, Skeletal/metabolism , Muscular Atrophy/drug therapy , Muscular Atrophy/metabolism , Oligonucleotide Array Sequence Analysis , Signal Transduction/drug effects
Indian J Exp Biol ; 2014 Oct; 52(10): 972-982
Article in English | IMSEAR | ID: sea-153791


Arjunolic acid (AA) obtained from plants of the Combretaceae family has shown anti-diabetic effects. Here, we analyzed whether the diabetogenic effects of dexamethasone (DEX) treatment on glucose homeostasis may be prevented or attenuated by the concomitant administration of AA. Adult Wistar rats were assigned to the following groups: vehicle-treated (Ctl), DEX-treated (1 mg/kg body weight intraperitoneally for 5 days) (Dex), AA-treated (30 mg/kg body weight by oral gavage twice per day) (Aa), AA treatment previous to and concomitant to DEX treatment (AaDex), and AA treatment after initiation of DEX treatment (DexAa). AA administration significantly ameliorated (AaDex) (P>0.05), but did not attenuate (DexAa), the glucose intolerance induced by DEX treatment. AA did not prevent or attenuate the elevation in hepatic glycogen and triacylglycerol content caused by DEX treatment. All DEX-treated rats exhibited hepatic steatosis that seemed to be more pronounced when associated with AA treatment given for a prolonged period (AaDex). Markers of liver function and oxidative stress were not significantly altered among the groups. Therefore, AA administered for a prolonged period partially prevents the glucose intolerance induced by DEX treatment, but it fails to produce this beneficial effect when given after initiation of GC treatment. Since AA may promote further hepatic steatosis when co-administered with GCs, care is required when considering this phytochemical as a hypoglycemiant and/or insulin-sensitizing agent.

Animals , Blood Glucose/drug effects , Blood Glucose/metabolism , Body Weight/drug effects , Glucocorticoids/blood , Glucocorticoids/metabolism , Insulin/metabolism , Lipids/blood , Liver/chemistry , Liver/drug effects , Liver/pathology , Male , Organ Size/drug effects , Rats , Rats, Wistar , Triterpenes/pharmacology
Indian J Exp Biol ; 2014 Jul; 52(7): 683-691
Article in English | IMSEAR | ID: sea-153748


Ursolic acid (UA) is a pentacyclic triterpenoid compound that naturally occurs in fruits, leaves and flowers of medicinal herbs. This study investigated the dose-response efficacy of UA (0.01 and 0.05%) on glucose metabolism, the polyol pathway and dyslipidemia in streptozotocin/nicotinamide-induced diabetic mice. Supplement with both UA doses reduced fasting blood glucose and plasma triglyceride levels in non-obese type 2 diabetic mice. High-dose UA significantly lowered plasma free fatty acid, total cholesterol and VLDL-cholesterol levels compared with the diabetic control mice, while LDL-cholesterol levels were reduced with both doses. UA supplement effectively decreased hepatic glucose-6-phosphatase activity and increased glucokinase activity, the glucokinase/glucose-6-phosphatase ratio, GLUT2 mRNA levels and glycogen content compared with the diabetic control mice. UA supplement attenuated hyperglycemia-induced renal hypertrophy and histological changes. Renal aldose reductase activity was higher, whereas sorbitol dehydrogenase activity was lower in the diabetic control group than in the non-diabetic group. However, UA supplement reversed the biochemical changes in polyol pathway to normal values. These results demonstrated that low-dose UA had preventive potency for diabetic renal complications, which could be mediated by changes in hepatic glucose metabolism and the renal polyol pathway. High-dose UA was more effective anti-dyslipidemia therapy in non-obese type 2 diabetic mice.

Animals , Antineoplastic Agents, Phytogenic/pharmacology , Blotting, Western , Diabetes Complications/etiology , Diabetes Complications/pathology , Diabetes Complications/prevention & control , Diabetes Mellitus, Experimental/complications , Diabetes Mellitus, Experimental/drug therapy , Diabetes Mellitus, Experimental/metabolism , Diabetes Mellitus, Type 2/complications , Diabetes Mellitus, Type 2/drug therapy , Diabetes Mellitus, Type 2/metabolism , Dyslipidemias/drug therapy , Dyslipidemias/etiology , Dyslipidemias/pathology , Glucokinase/metabolism , Glucose/metabolism , Glucose Transporter Type 2/genetics , Glucose-6-Phosphatase/metabolism , Glycogen/metabolism , Hyperglycemia/complications , Kidney Diseases/etiology , Kidney Diseases/pathology , Kidney Diseases/prevention & control , Male , Mice , Mice, Inbred ICR , Mice, Inbred NOD , Polymers/metabolism , RNA, Messenger/genetics , Real-Time Polymerase Chain Reaction , Reverse Transcriptase Polymerase Chain Reaction , Signal Transduction/drug effects , Triterpenes/pharmacology
Biomédica (Bogotá) ; 34(2): 237-249, abr.-jun. 2014. ilus, tab
Article in English | LILACS | ID: lil-712406


Introduction: Despite efforts to control malaria, around 10% of the world population is at risk of acquiring this disease. Plasmodium falciparum accounts for the majority of severe cases and deaths. Malaria control programs have failed due to the therapeutic failure of first-line antimalarials and to parasite resistance. Thus, new and better therapeutic alternatives are required. Proteomic analysis allows determination of protein expression levels under drug pressure, leading to the identification of new therapeutic drug targets and their mechanisms of action. Objective: The aim of this study was to analyze qualitatively the expression of P.falciparum trophozoite proteins (strain ITG2), after exposure to antimalarial drugs, through a proteomic approach. Materials and methods: In vitro cultured synchronized parasites were treated with quinine, mefloquine and the natural antiplasmodial diosgenone. Protein extracts were prepared and analyzed by two-dimensional electrophoresis. The differentially expressed proteins were selected and identified by MALDI-TOF mass spectrometry. Results: The following proteins were identified among those differentially expressed in the parasite in the presence of the drugs tested: enolase (PF10_0155), calcium-binding protein (PF11_0098), chaperonin (PFL0740c), the host cell invasion protein (PF10_0268) and proteins related to redox processes (MAL8P1.17). These findings are consistent with results of previous studies where the parasite was submitted to pressure with other antimalarial drugs. Conclusion: The observed changes in the P. falciparum trophozoite protein profile induced by antimalarial drugs involved proteins mainly related to the general stress response.

Introducción. A pesar de los esfuerzos para controlar la malaria, esta sigue siendo un problema de salud pública. Plasmodium falciparum es responsable de la mayoría de los casos graves y de las muertes. Los programas de control de la malaria han sido cuestionados debido al fracaso del tratamiento y a la resistencia del parásito a los antipalúdicos de primera línea, por lo que se requieren nuevas y mejores alternativas. El análisis proteómico permite identificar y determinar los niveles de expresión de las proteínas bajo la presión de los medicamentos, lo que posibilita la identificación de nuevos blancos terapéuticos y mecanismos de acción. Objetivo. Analizar cualitativamente la expresión diferencial de proteínas del citosol del trofozoíto de P. falciparum bajo tratamiento con quinina, mefloquina y el compuesto natural diosgenona mediante una aproximación proteómica. Materiales y métodos. Se trataron trofozoítos sincronizados y cultivados in vitro de P. falciparum (cepa ITG2) con quinina, mefloquina y el compuesto natural diosgenona. Los extractos proteicos se prepararon y analizaron por electroforesis bidimensional. Las proteínas con aparente expresión diferencial se seleccionaron e identificaron mediante espectrometría de masas MALDI-TOF. Resultados. Se encontraron las siguientes proteínas diferencialmente expresadas en el trofozoíto: la enolasa (PF10_0155), la proteína de unión a calcio (PF11_0098), la chaperonina (PFL0740c), la proteína de invasión a la célula del huésped (PF10_0268) y la proteína relacionada con procesos de reducción y oxidación (redox) (MAL8P1.17). Estos hallazgos son congruentes con resultados previos de estudios en los que el parásito fue presionado con otros medicamentos antipalúdicos. Conclusión. Los cambios observados en el perfil de proteínas del trofozoíto de P. falciparum tratado con antipalúdicos involucraron preferencialmente proteínas relacionadas con la respuesta al estrés general.

Humans , Antiprotozoal Agents/pharmacology , Mefloquine/pharmacology , Plasmodium falciparum/drug effects , Protozoan Proteins/biosynthesis , Quinine/pharmacology , Spiro Compounds/pharmacology , Triterpenes/pharmacology , Amino Acid Sequence , Electrophoresis, Gel, Two-Dimensional , Erythrocytes/parasitology , Gene Expression Regulation/drug effects , Heat-Shock Proteins/biosynthesis , Heat-Shock Proteins/genetics , Heat-Shock Proteins/isolation & purification , In Vitro Techniques , Molecular Sequence Data , Proteome , Plasmodium falciparum/growth & development , Plasmodium falciparum/metabolism , Protozoan Proteins/genetics , Protozoan Proteins/isolation & purification , Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
Pakistan Journal of Pharmaceutical Sciences. 2014; 27 (1): 187-191
in English | IMEMR | ID: emr-143000


The roots of Ichnocarpus frutescens along with roots of Cissampelos pareira, Bauhinia vahlii and Ardisia solanacea are processed together and given orally to cure stomach cancer by the tribes of Chotanagpur and Santhal parganas of Bihar, India. In vitro anticancer activity of the residue from methanolic extract of roots of I. frutescens [MIF] and isolated triterpenes were evaluated by 3-[4, 5-dimethyl thiazol-2-yl]-2, 5-diphenyltetrazolium bromide [MTT] assay using MCF-7, BEL-7402, SPC-A-1 and SGC-7901 cancer cell lines. MIF showed significant anticancer activity on four cancer cell lines with IC[50] values 163.5 +/- 3.58, 156.3 +/- 2.95, 142.6 +/- 2.60 and 112.4 +/- 1.85 respectively as compared to vehicle treated control. Ursolic acid showed anticancer activity on four cancer cell lines with IC[50] values 8.5 +/- 0.29, 9.9 +/- 0.12, 8.1 +/- 0.40 and 6.2 +/- 0.23 respectively, while IC[50] values for alpha-amyrin on four cancer cell lines was found to be 7.2 +/- 0.12, 8.2 +/- 0.29, 7.6 +/- 0.06 and 5.0 +/- 0.12 respectively.

Humans , Antineoplastic Agents, Phytogenic/pharmacology , Triterpenes/pharmacology , Plant Extracts/pharmacology , Plant Roots , Oleanolic Acid , Cell Line, Tumor
Article in English | WPRIM | ID: wpr-56423


Betulinic acid (BA), a pentacyclic lupane-type triterpene, has a wide range of bioactivities. The main objective of this work was to evaluate the hepatoprotective activity of BA and the potential mechanism underlying the ability of this compound to prevent liver damage induced by alcohol in vivo. Mice were given oral doses of BA (0.25, 0.5, and 1.0 mg/kg) daily for 14 days, and induced liver injury by feeding 50% alcohol orally at the dosage of 10 ml/kg after 1 h last administration of BA. BA pretreatment significantly reduced the serum levels of alanine transaminase, aspartate transaminase, total cholesterol, and triacylglycerides in a dose-dependent manner in the mice administered alcohol. Hepatic levels of glutathione, superoxide dismutase, glutathione peroxidase, and catalase were remarkably increased, while malondialdehyde contents and microvesicular steatosis in the liver were decreased by BA in a dose-dependent manner after alcohol-induced liver injury. These findings suggest that the mechanism underlying the hepatoprotective effects of BA might be due to increased antioxidant capacity, mainly through improvement of the tissue redox system, maintenance of the antioxidant system, and decreased lipid peroxidation in the liver.

Animals , Antioxidants/pharmacology , Blood Chemical Analysis , Enzymes/blood , Ethanol/toxicity , Lipid Peroxidation/drug effects , Liver/drug effects , Male , Mice , Random Allocation , Triterpenes/pharmacology
Indian J Exp Biol ; 2013 Jul; 51(7): 485-491
Article in English | IMSEAR | ID: sea-147618


Breast cancer is a major public health problem and the low effectiveness of conventional therapies to achieve long term survival results in increased mortality associated with advanced breast cancers. Betulinic acid (BA) is a pentacyclic triterpene which can be isolated from number of plants grown in the tropics. It exhibits cytotoxic activity against variety of cancer cell lines. In the present study, the in vitro cytotoxic activity and in vivo antitumor activity of BA was evaluated in athymic nude mice bearing MCF-7 breast adenocarcinoma xenografts. In vitro cytotoxic activity of BA on MCF-7 cells was studied using the MTT assay and BA was cytotoxic towards MCF-7 cells with IC50 value of 13.5µg/mL. The antitumor activity of BA was studied at concentrations of 50 and 100 mg/kg body weight in mice injected with MCF-7 cells. BA treatment delayed tumor formation and statistically significant reduction (P<0.0001) of 52 and 77% in the tumor size at concentrations of 50 and 100 mg, respectively was observed. Histopathological analysis of tumors revealed decreased angiogenesis, proliferation and invasion in BA treated animals. This is one of the first studies demonstrating the in vivo antitumor activity of BA on MCF-7 breast cancer tumors in nude mice. The antitumor effect of BA can further be enhanced by use of combination therapy and novel drug delivery systems, thus making it a promising candidate for management of breast cancer patients.

Animals , Antineoplastic Agents, Phytogenic/pharmacology , Apoptosis/drug effects , Breast Neoplasms/blood supply , Breast Neoplasms/drug therapy , Breast Neoplasms/pathology , Cell Proliferation/drug effects , Female , Humans , Immunoenzyme Techniques , Mice , Mice, Inbred BALB C , Mice, Nude , Neovascularization, Pathologic , Triterpenes/pharmacology , Tumor Cells, Cultured
Bol. latinoam. Caribe plantas med. aromát ; 12(1): 108-116, ene. 2013. ilus, tab
Article in English | LILACS | ID: lil-722513


The aim of this study was to establish an analytical method to detect the presence of the responsible triterpenoids of the anti-inflammatory activity of the leaves of Ugni molinae (murtilla). Successive leaves extracts of EtOAc (EAE) and ethanol (TEE) were prepared, obtaining for the first time from TEE a triterpenoid-rich sub-fraction (TF). The topical anti-inflammatory activity of TF was assessed (43.3 percent at 1 mg/ear) by means of the TPA-induced mouse ear oedema model, which was compared to EAE (83.1 +/- 3.2 percent) and TEE (78.3 +/- 11.8 percent) activities, both previously evaluated by us. These extracts were characterized in their triterpenoids by HPLC-UV and HPLC-ESI-MS. We demonstrated that TF has triterpenoids responsible in part of the anti-inflammatory activity, among them, madecassic and maslinic acids. These two compounds have been reported for the first time for this species. ED50 for madecassic and alphitolic acids are also here reported.

El objetivo de este trabajo fue establecer un método analítico para determinar la presencia de los triterpenoides responsables de la actividad anti-inflamatoria de las hojas de Ugni molinae (murtilla). Fueron preparados los extractos seriados de EtOAc (EAE) y etanólico (TEE) desde sus hojas, obteniendo desde el TEE por primera vez una sub-fracción rica en triterpenoides (TF). Se demostró la actividad anti-inflamatoria tópica del TF por el modelo de edema de oreja de ratón inducida por TPA (43,3 por ciento a 1 mg/oreja), la cual fue comparada con las de los EAE (83,1 +/- 3,2 por ciento) y TEE (78,3 +/- 11,8 por ciento) determinadas en nuestros estudios previos. Dichos extractos fueron caracterizados en sus triterpenoides por CLAE-UV y CLAE-IES-MS. Demostramos que el TF contiene triterpenoides responsables en parte de la actividad anti-inflamatoria, entre ellos, los ácidos madecásico y maslínico, reportados por primera vez para esta especie. Se informan además las DE50 para los ácidos madecásico y alfitólico.

Animals , Rats , Anti-Inflammatory Agents , Plant Extracts/pharmacology , Plant Leaves/chemistry , Myrtaceae/chemistry , Triterpenes/isolation & purification , Triterpenes/analysis , Chile , Chromatography, High Pressure Liquid , Spectrometry, Mass, Electrospray Ionization , Triterpenes/pharmacology