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1.
Pharmaceuticals (Basel) ; 16(5)2023 May 10.
Article in English | MEDLINE | ID: mdl-37242507

ABSTRACT

The antihyperglycemic activity of ethanolic extract from Annona cherimola Miller (EEAch) and its products were evaluated using in vivo and in silico assays. An α-glucosidase inhibition was evaluated with oral sucrose tolerance tests (OSTT) and molecular docking studies using acarbose as the control. SGLT1 inhibition was evaluated with an oral glucose tolerance test (OGTT) and molecular docking studies using canagliflozin as the control. Among all products tested, EEAc, the aqueous residual fraction (AcRFr), rutin, and myricetin reduced the hyperglycemia in DM2 mice. During the carbohydrate tolerance tests, all the treatments reduced the postprandial peak such as the control drugs. In the molecular docking studies, rutin showed more affinity in inhibiting α-glucosidase enzymes and myricetin in inhibiting the SGLT1 cotransporter, showing ∆G values of -6.03 and -3.32 kcal/mol-1, respectively, in α-glucosidase enzymes. In the case of the SGLT1 cotransporter, molecular docking showed ∆G values of 22.82 and -7.89 in rutin and myricetin, respectively. This research sorts in vivo and in silico pharmacological studies regarding the use of A. cherimola leaves as a source for the development of new potential antidiabetic agents for T2D control, such as flavonoids rutin and myricetin.

3.
Pharmaceuticals (Basel) ; 16(1)2023 Jan 12.
Article in English | MEDLINE | ID: mdl-36678609

ABSTRACT

Ethanolic extract obtained from Annona cherimola Miller (EEAc) and the flavonoid rutin (Rut) were evaluated in this study to determine their antihyperglycemic content, % HbA1c reduction, and antihyperlipidemic activities. Both treatments were evaluated separately and in combination with the oral antidiabetic drugs (OADs) acarbose (Aca), metformin (Met), glibenclamide (Gli), and canagliflozin (Cana) in acute and subchronic assays. The evaluation of the acute assay showed that EEAc and Rut administered separately significantly reduce hyperglycemia in a manner similar to OADs and help to reduce % HbA1c and hyperlipidemia in the subchronic assay. The combination of EEAc + Met showed the best activity by reducing the hyperglycemia content, % HbA1c, Chol, HDL-c, and LDL-c. Rutin in combination with OADs used in all treatments significantly reduced the hyperglycemia content that is reflected in the reduction in % HbA1c. In relation to the lipid profiles, all combinate treatments helped to avoid an increase in the measured parameters. The results show the importance of evaluating the activity of herbal remedies in combination with drugs to determine their activities and possible side effects. Moreover, the combination of rutin with antidiabetic drugs presented considerable activity, and this is the first step for the development of novel DM treatments.

5.
Molecules ; 27(20)2022 Oct 21.
Article in English | MEDLINE | ID: mdl-36296714

ABSTRACT

Annona macroprophyllata Donn (A. macroprophyllata) is used in traditional Mexican medicine for the treatment of cancer, diabetes, inflammation, and pain. In this work, we evaluated the antitumor activity of three acyclic terpenoids obtained from A. macroprophyllata to assess their potential as antilymphoma agents. We identified the terpenoids farnesyl acetate (FA), phytol (PT) and geranylgeraniol (Gg) using gas chromatography-mass spectroscopy (GC-MS) and spectroscopic (1H, and 13C NMR) methods applied to petroleum ether extract of leaves from A. macroprophyllata (PEAm). We investigated antitumor potential in Balb/c mice inoculated with U-937 cells by assessing brine shrimp lethality (BSL), and cytotoxic activity in these cells. In addition, to assess the potential toxicity of PEAm, FA, PT and Gg in humans, we tested their acute oral toxicity in mice. Our results showed that the three terpenoids exhibited considerable antilymphoma and cytotoxic activity. In terms of lethality, we determined a median lethal dose (LD50) for thirteen isolated products of PEAm. Gg, PT and AF all exhibited a higher lethality with values of 1.41 ± 0.42, 3.03 ± 0.33 and 5.82 ± 0.58 µg mL-1, respectively. To assess cytotoxic activity against U-937 cells, we calculated the mean cytotoxic concentration (CC50) and found that FA and PT were closer in respect to the control drug methotrexate (MTX, 0.243 ± 0.007 µM). In terms of antilymphoma activity, we found that FA, PT and Gg considerably inhibited lymph node growth, with median effective doses (ED50) of 5.89 ± 0.39, 6.71 ± 0.31 and 7.22 ± 0.51 mg kg-1 in females and 5.09 ± 0.66, 5.83 ± 0.50 and 6.98 ± 0.57mg kg -1 in males, respectively. Regarding acute oral toxicity, we classified all three terpenoids as category IV, indicating a high safety margin for human administration. Finally, in a molecular docking study of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, we found binding of terpenoids to some amino acids of the catalytic site, suggesting an effect upon activity with a resulting decrease in the synthesis of intermediates involved in the prenylation of proteins involved in cancer progression. Our findings suggest that the acyclic terpenoids FA, PT, and Gg may serve as scaffolds for the development of new treatments for non-Hodgkin's lymphoma.


Subject(s)
Annona , Antineoplastic Agents , Male , Female , Mice , Humans , Animals , Annona/chemistry , Terpenes/pharmacology , Molecular Docking Simulation , Methotrexate , Plant Extracts/pharmacology , Plant Extracts/chemistry , Antineoplastic Agents/pharmacology , Phytol , Amino Acids
6.
Plants (Basel) ; 11(5)2022 Feb 22.
Article in English | MEDLINE | ID: mdl-35270046

ABSTRACT

The antihyperglycemic activity of ethanolic extract from Salvia polystachya (EESpS) and its products was evaluated using in vivo, ex vivo and in silico assays; additionally, an acute toxicity assay was evaluated. EESpS was classified as a nontoxic class 5 drug. EESpS, ethyl acetate fraction (EtOAcFr), secondary-6-fraction (SeFr6), ursolic acid (UA), and oleanolic acid (OA) reduced the hyperglycemia in DM2 mice. α-glucosidase inhibition was evaluated with oral sucrose and starch tolerance tests (OSuTT and OStTT), an intestinal sucrose hydrolysis (ISH) assay and molecular docking studies using acarbose as control. SGLT1 inhibition was evaluated with oral glucose and galactose tolerance tests (OGTT and OGaTT), an intestinal glucose absorption (IGA) assay and molecular docking studies using canagliflozin as the control. During the carbohydrate tolerance tests, all the treatments reduced the postprandial peak, similar to the control drugs. During the ISH, IC50 values of 739.9 and 726.3 µM for UA and OA, respectively, were calculated. During the IGA, IC50 values of 966.6 and 849.3 for UA, OA respectively, were calculated. Finally, during the molecular docking studies, UA and OA showed ∆G values of -6.41 and -5.48 kcal/mol-1, respectively, on α-glucosidase enzymes. During SGLT1, UA and OA showed ∆G values of -10.55 and -9.65, respectively.

7.
Pharmaceuticals (Basel) ; 15(2)2022 Feb 03.
Article in English | MEDLINE | ID: mdl-35215308

ABSTRACT

Incomptines A (IA) and B (IB) are two sesquiterpene lactones with antiprotozoal, antibacterial, cytotoxic, antitumor, spermicidal, and phytotoxic properties. The antibacterial activity of IA and IB against bacteria causing diarrhoea have been reported; however, no information is available regarding their antibacterial activity on Vibrio cholerae. In this work, both compounds were evaluated for their anti-diarrhoeal potential using the bacterium V. cholerae, sodium dodecyl sulphate-polyacrylamide gel electrophoresis (SDS-PAGE) analysis on cholera toxin, and a cholera toxin-induced diarrhoea model in male Balb/c mice. In addition, a molecular docking study was carried out to understand the interaction of IA and IB with cholera toxin. In terms of antibacterial activity, IB was three times more active than IA on V. cholerae. In the case of SDS-PAGE analysis and the in silico study, IA was most effective, revealing its potential binding mode at a molecular level. In terms of anti-diarrhoeal activity, IA was 10 times more active than IB and racecadotril, an antisecretory drug used as positive control; the anti-diarrheal activity of IB was also closer than racecadotril. The results obtained from in vitro, in vivo, and computational studies on V. cholerae and cholera toxin support the potential of IA and IB as new anti-diarrhoeal compounds.

8.
Molecules ; 26(24)2021 Dec 18.
Article in English | MEDLINE | ID: mdl-34946755

ABSTRACT

Annona muricata (Am) is a plant used in traditional Mexican medicine to treat cancer. In this study, ethanol extracts of Am collected in Acapulco and Tecpan from Guerrero state were evaluated orally on Balb/c mice inoculated with 4T1 cells, for cytotoxic activity (CA) on 4T1 cells, in brine shrimp lethality assay (BSLA), and for acute oral toxicity in mice. In addition, ethanol extracts were subjected to high-performance liquid chromatography (HPLC) with diode array detection. Results showed that the extracts collected in December in Acapulco (AcDe) and Tecpan (TeDe) exhibited the most significant antitumor and cytotoxic activity. In the BSLA, the most important effect was observed in the extracts from Acapulco and Tecpan collected in June (AcJu) and August (TeAg), respectively. The samples from Acapulco (AcJu, and AcAg) and Tecpan (TeJu and TeAg) showed the highest toxicity. The analysis of the extracts, AcDe and TeDe, by HPLC revealed that flavonoids, rutin, narcissin, and nicotinflorin were the major components. These findings suggest that extracts from Am collected in Acapulco and Tecpan in the month of December may be an important source to obtain flavonoid glycosides with anticancer potential specifically against breast cancer. This also supports the use of Am to treat cancer in Mexican traditional medicine.


Subject(s)
Annona/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Plant Extracts/pharmacology , Plants, Medicinal/chemistry , Animals , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/isolation & purification , Artemia/drug effects , Cell Proliferation/drug effects , Cell Survival/drug effects , Drug Screening Assays, Antitumor , Female , Mammary Neoplasms, Experimental/drug therapy , Mammary Neoplasms, Experimental/pathology , Medicine, Traditional , Mexico , Mice , Mice, Inbred BALB C , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Tumor Cells, Cultured
10.
Rev. Finlay ; 11(2): 189-199, 2021. tab, graf
Article in Spanish | LILACS-Express | LILACS | ID: biblio-1340760

ABSTRACT

RESUMEN El cáncer gástrico es una de las principales causas de muerte por neoplasias en el mundo. Las guías de prácticas clínicas actuales ofrecen modelos de tratamiento que involucran a la cirugía, radioterapia, quimioterapia, inmunoterapia y terapia dirigida a receptores de crecimiento específicos, sin embargo, los aspectos genéticos y de la biología molecular no siempre son tenidos en cuenta en la práctica médica. El objetivo de la presente revisión es articular los aspectos actuales más relevantes de la genética y la biología molecular en relación con el cáncer gástrico, para integrarlos en las guías clínicas de pacientes y familiares con el diagnóstico o con riesgo de padecer este tipo de neoplasia. Para ello se revisaron los avances genéticos y los síndromes relacionados con el cáncer gástrico, clasificaciones moleculares e implicaciones en su manejo. Se utilizaron las bases de datos Google Scholar, Elsevier y PubMed en los últimos 10 años, seleccionándose los de mayor importancia a texto completo desde el punto de vista cualitativo. La integración de antecedentes personales y familiares con elementos genéticos precisan ser tenidos en cuenta en el manejo, diagnóstico y prevención de esta enfermedad. Se sugiere la inclusión de elementos genéticos y moleculares en toda guía de práctica clínica.


ABSTRACT Gastric cancer is one of the leading causes of death from neoplasms in the world. Current clinical practice guidelines offer treatment models that involve surgery, radiotherapy, chemotherapy, immunotherapy and therapy directed at specific growth receptors, however, genetic and molecular biology aspects are not always taken into account in medical practice. The objective of this review is to articulate the most relevant current aspects of genetics and molecular biology in relation to gastric cancer, to integrate them into the clinical guidelines of patients and relatives with the diagnosis or at risk of suffering from this type of neoplasia. For them, genetic advances and syndromes related to gastric cancer, molecular classifications and implications in their management were reviewed. The databases Google Scholar, Elsevier, and PubMed were used in the last 10 years, selecting the most important full-text from a qualitative point of view. The integration of personal and family history with genetic elements needs to be taken into account in the diagnostic management and prevention of this disease. The inclusion of genetic and molecular elements in all clinical practice guidelines is suggested.

11.
Molecules ; 26(9)2021 Apr 21.
Article in English | MEDLINE | ID: mdl-33919145

ABSTRACT

The antihyperglycemic and antilipidemic effects of the tea infusion extracts of leaves from Annona cherimola Miller (IELAc-0.5, IELAc-1.5, and IELAc-3.0) were evaluated on normoglycemic (NG) and streptozocin-induced diabetic (STID) mice. In the acute test, IELAc-1.5 at 300 mg/kg bodyweight (bw) exhibited antihyperglycemic activity on STID mice since the first hour of treatment. Then, its antidiabetic potential was analyzed in a subchronic evaluation. IELAc-1.5 was able to reduce the blood glucose level, glycated hemoglobin (HbA1c), cholesterol (CHO), and triglycerides (TG); high-density lipoprotein (HDL) showed an increase at the end of treatment. IELAc-1.5 did not modify the urine profile at the end of the evaluation, and neither toxicity nor macroscopic organ damage were observed in acute and subchronic assays. In addition, a major flavonol glycoside present in the tea infusion extracts was identified using high-performance liquid chromatography with diode array detection (HPLC-DAD). The analysis of the tea infusion extracts by HPLC revealed that rutin was the major component. This study supports the use of tea infusions from Annona cherimola for the treatment of diabetes and suggests that rutin could be responsible, at least in part, for their antidiabetic properties.


Subject(s)
Hypoglycemic Agents/pharmacology , Hypolipidemic Agents/pharmacology , Plant Extracts/pharmacology , Animals , Annona/chemistry , Blood Glucose/drug effects , Body Weight/drug effects , Chromatography, High Pressure Liquid , Diabetes Mellitus, Experimental , Diabetes Mellitus, Type 2/drug therapy , Diabetes Mellitus, Type 2/metabolism , Hypoglycemic Agents/chemistry , Hypolipidemic Agents/chemistry , Mice , Organ Size/drug effects , Plant Extracts/chemistry , Plant Leaves/chemistry , Tea
12.
Rev. habanera cienc. méd ; 20(2): e3675, mar.-abr. 2021. graf
Article in Spanish | LILACS, CUMED | ID: biblio-1251797

ABSTRACT

Introducción: La Endocarditis infecciosa sigue desafiando a la Medicina moderna a pesar de no ser una entidad frecuente. Objetivo: Se presenta un caso con una lesión valvular previa no diagnosticada antes, y sin síntomas, y que se consideró el diagnóstico tempranamente de endocarditis en el nivel hospitalario. Presentación del caso: Paciente de 20 años, mujer, con antecedentes de salud referidos, fumadora. Ingresa en sala del Servicio de Medicina el 21 de enero de 2020 por fiebres que se mantienen todo el día de 38-38,50 C, con picos que alcanzan los 400 C con escalofríos en determinados momentos. Desde hace un mes presenta esta sintomatología. Ruidos cardiacos rítmicos, taquicárdicos, de buena intensidad. Clic sistólico con arrastre sistólico fuerte de regurgitación IV/VI audible en foco mitral con frémito que se irradia a la axila, anemia, VSG acelerada, leucocitosis con desviación izquierda, hemocultivos negativos y en ecocardiograma prolapso de válvula mitral, valva anterior y posterior, con regurgitación que ocupa toda la aurícula izquierda hasta el techo de la misma. Múltiples vegetaciones en cara auricular de valva posterior de válvula mitral, la mayor de 7 x 3 mm. Conclusiones: El método clínico es fundamental en el proceso diagnóstico en la práctica clínica secundado por los medios diagnósticos como en la enfermedad que nos ocupa(AU)


Introduction: Infective endocarditis continues to be a great challenge for modern medicine although it is not a frequent entity. Objective: We present a case of an undiagnosed previous valve lesion without symptoms. The early diagnosis of endocarditis was made at the hospital level. Case Presentation: A 20-year-old woman, smoker, with previous history of good health was admitted to the medical ward on January 21, 2020. The patient reported continuous fever (38-38,50 C) throughout the day, with spikes up to 400 C and intermittent chills. She has been having these symptoms for a month. Rhythmic heart sounds and high intensity tachycardia and systolic click with strong systolic displacement of regurgitation grade IV/VI audible in mitral area with fremitus radiating to the armpit were heard. Anemia, accelerated ESR, leukocytosis with left deviation, and negative blood cultures were confirmed. The echocardiogram showed a mitral valve prolapse with regurgitation of anterior and posterior valves that occupies all the left atrium until its top. There was multiple vegetation in the atrial side of the posterior leaflet of the mitral valve; the greatest is 7 x 3 mm. Conclusions: The clinical method is essential in the diagnostic process performed in clinical practice supported by diagnostic means, as in the current case(AU)


Subject(s)
Humans , Female , Young Adult , Mitral Valve Prolapse/diagnosis , Mitral Valve Prolapse/prevention & control , Early Diagnosis , Endocarditis/diagnosis , Blood Culture/methods
13.
PPAR Res ; 2021: 5100531, 2021.
Article in English | MEDLINE | ID: mdl-35003235

ABSTRACT

Thiazolidinediones (TZDs), used to treat type 2 diabetes mellitus, act as full agonists of the peroxisome proliferator-activated receptor gamma. Unfortunately, they produce adverse effects, including weight gain, hepatic toxicity, and heart failure. Our group previously reported the design, synthesis, in silico evaluation, and acute oral toxicity test of two TZD derivatives, compounds 40 (C40) and 81 (C81), characterized as category 5 and 4, respectively, under the Globally Harmonized System. The aim of this study was to determine whether C40, C81, and a new compound, C4, act as euglycemic and antioxidant agents in male Wistar rats with streptozotocin-induced diabetes. The animals were randomly divided into six groups (n = 7): the control, those with diabetes and untreated, and those with diabetes and treated with pioglitazone, C40, C81, or C4 (daily for 21 days). At the end of the experiment, tissue samples were collected to quantify the level of glucose, insulin, triglycerides, total cholesterol, and liver enzymes, as well as enzymatic and nonenzymatic antioxidant activity. C4, without a hypoglycemic effect, displayed the best antioxidant activity. Whereas C81 could only attenuate the elevated level of blood glucose, C40 generated euglycemia by the end of the treatment. All compounds produced a significant decrease in triglycerides.

14.
Rev. Finlay ; 10(4): 347-354, oct.-dic. 2020. tab
Article in Spanish | LILACS-Express | LILACS | ID: biblio-1155439

ABSTRACT

RESUMEN Fundamento: la aterosclerosis es una enfermedad de origen multifactorial. El estudio y abordaje de sus factores de riesgo modificables y la actuación sobre estos factores puede cambiar positivamente la situación de salud. Objetivo identificar algunas señales aterogénicas tempranas en estudiantes de medicina del segundo año de la Facultad de Ciencias Médicas Dr. Enrique Cabrera de la Habana. Método: se realizó un estudio descriptivo para identificar algunos factores de riesgo aterogénicos entre el 2018 y el 2019, que incluyó 170 estudiantes de nacionalidad cubana que cursaban el segundo año de la carrera de medicina de la Facultad de Ciencias Médicas Dr. Enrique Cabrera con edades comprendidas entre 19 y 24 años, de ambos sexos y que no referían algún síntoma o enfermedad. Se aplicó encuesta confeccionada al efecto validada por el Centro de Investigación y Referencias de Aterosclerosis de La Habana modificada. Las variables consideradas fueron: sexo, índice de masa corporal, hábito de fumar, hipertensión arterial, hipercolesterolemia, hipertrigliceridemia, hábitos nutricionales, consumo de alcohol y los antecedentes patológicos familiares. Resultados: los factores de riesgo aterogénicos más frecuentes detectados fueron: obesidad (17,65 %), dislipidemia (16,7 %), hábito de fumar (33,5 %), hipertensión arterial (9,4 %), consumo frecuente de bebidas alcohólicas (28,2 %), antecedentes patológicos familiares relacionados (22,9 %) y dietas inadecuadas (62,2 %), cuyos valores en el análisis estadístico fueron significativos. Más del 40 % de los pacientes presentaron dos o más factores de riesgo. Conclusiones: los resultados mostraron cifras elevadas de factores de riesgo, solos o combinados. Los factores de riesgo que predominaron fueron el tabaquismo, malos hábitos nutricionales, dislipidemias y la ingestión de bebidas alcohólicas.


ABSTRACT Background: atherosclerosis is a multifactorial origin disease. The study and approach of its modifiable risk factors and action on these factors can positively change the health situation. Objective: to identify some early atherogenic signs in second-year medical students at the Dr. Enrique Cabrera Medical Sciences Faculty in Havana. Method: a descriptive study was carried out to identify some atherogenic risk factors between 2018 and 2019, which included 170 students of cuban nationality who were studying the second year of medicine at the Dr. Enrique Cabrera Faculty of Medical Sciences, with ages between 19 and 24 years old, of both sexes and did not report any symptoms or disease. Survey was applied, made for this purpose and validated by the Atherosclerosis Center for Research and References of Havana modified. The variables considered were: sex, body mass index (BMI), smoking habit, arterial hypertension, hypercholesterolemia, hypertriglyceridemia, nutritional habits, alcohol consumption and family pathological history. Results: the most frequent atherogenic risk factors detected were: obesity (17.65 %), dyslipidemia (16.7 %), smoking (33.5 %), arterial hypertension (9.4 %), frequent consumption of alcoholic beverages (28.2 %), related family pathological history (22.9 %) and inadequate diets (62.2 %), whose values ​​in the statistical analysis were significant. More than the 40 % of the patients had two or more risk factors. Conclusions the results showed high numbers of risk factors, alone or in combination. The risk factors that predominated were smoking, poor nutritional habits, dyslipidemia and the ingestion of alcoholic beverages.

15.
Mater Sci Eng C Mater Biol Appl ; 116: 111196, 2020 Nov.
Article in English | MEDLINE | ID: mdl-32806317

ABSTRACT

Ovarian cancer (OC) is the deadliest gynecological cancer. Standard treatment of OC is based on cytoreductive surgery followed by chemotherapy with platinum drugs and taxanes; however, innate and acquired drug-resistance is frequently observed followed by a relapse after treatment, thus, more efficient therapeutic approaches are required. Combination therapies involving phototherapies and chemotherapy (the so-called chemophototherapy) may have enhanced efficacy against cancer, by attacking cancer cells through different mechanisms, including DNA-damage and thermally driven cell membrane and cytoskeleton damage. We have designed and synthesized poly(lactic-co-glycolic) nanoparticles (PLGA NPs) containing the chemo-drug carboplatin (CP), and the near infrared (NIR) photosensitizer indocyanine green (ICG). We have evaluated the drug release profile, the photodynamic ROS generation and photothermal capacities of the NPs. Also, the antitumoral efficiency of the NPs was evaluated using the SKOV-3 cell line as an in vitro OC model, observing an enhanced cytotoxic effect when irradiating cells with an 800 nm laser. Evidence here shown supports the potential application of the biodegradable photoresponsive NPs in the clinical stage due to the biocompatibility of the materials used, the spatiotemporal control of the therapy and, also, the less likely development of resistance against the combinatorial therapy.


Subject(s)
Hyperthermia, Induced , Nanoparticles , Ovarian Neoplasms , Photochemotherapy , Animals , Cell Line, Tumor , Female , Humans , Indocyanine Green , Mice , Mice, Nude , Ovarian Neoplasms/drug therapy , Phototherapy
16.
Molecules ; 25(15)2020 Jul 24.
Article in English | MEDLINE | ID: mdl-32722136

ABSTRACT

Annona diversifolia Safford and two acyclic terpenoids were evaluated to determine their antihyperglycemic activity as potential α-glucosidase and selective SGLT-1 inhibitiors. Ethanolic extract (EEAd), chloroformic (CHCl3Fr), ethyl acetate (EtOAcFr), aqueous residual (AcRFr), secondary 5 (Fr5) fractions, farnesal (1), and farnesol (2) were evaluated on normoglycemic and streptozocin-induced diabetic mice. EEAd, CHCl3Fr, Fr5, (1) and (2) showed antihyperglycemic activity. The potential as α-glucosidase inhibitors of products was evaluated with oral sucrose and lactose tolerance (OSTT and OLTT, respectively) and intestinal sucrose hydrolysis (ISH) tests; the potential as SGLT-1 inhibitors was evaluated using oral glucose tolerance (OGTT), intestinal glucose absorption (IGA), and urinary glucose excretion (UGE) tests. In OSTT and OLTT, all treatments showed significant activity at two and four hours. In ISH, half maximal effective concentrations (CE50) of 565, 662 and 590 µg/mL, 682 and 802 µM were calculated, respectively. In OGTT, all treatments showed significant activity at two hours. In IGA, CE50 values of 1059, 783 and 539 µg/mL, 1211 and 327 µM were calculated, respectively. In UGE Fr5, (1) and (2) showed significant reduction of the glucose excreted compared with canagliflozin. These results suggest that the antihyperglycemic activity is mediated by α-glucosidase and selective SGLT-1 inhibition.


Subject(s)
Annona/chemistry , Diabetes Mellitus, Experimental/drug therapy , Diabetes Mellitus, Type 2/drug therapy , Hypoglycemic Agents/administration & dosage , Sodium-Glucose Transporter 1/metabolism , Terpenes/administration & dosage , alpha-Glucosidases/metabolism , Administration, Oral , Animals , Blood Glucose/drug effects , Diabetes Mellitus, Experimental/metabolism , Diabetes Mellitus, Type 2/chemically induced , Diabetes Mellitus, Type 2/metabolism , Gene Expression Regulation/drug effects , Glycoside Hydrolase Inhibitors/administration & dosage , Glycoside Hydrolase Inhibitors/chemistry , Glycoside Hydrolase Inhibitors/pharmacology , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/pharmacology , Male , Mice , Molecular Structure , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Rats , Streptozocin , Terpenes/chemistry , Terpenes/pharmacology
17.
Rev. cuba. med. gen. integr ; 36(2): e1123, abr.-jun. 2020. graf
Article in Spanish | LILACS, CUMED | ID: biblio-1138969

ABSTRACT

Introducción: Los tumores cerebrales a veces tienen una presentación clínica compleja y atípica en sus inicios, en dependencia de su localización, lo que puede confundirse con trastornos de la esfera psiquiátrica. Objetivo: Describir un caso clínico interpretado como una psicosis por su sintomatología cuyo diagnóstico resultó un glioblastoma multiforme de alta malignidad. Caso clínico: Mujer de 35 años que comienza desde hace varios meses con trastornos de la conducta, síntomas depresivos, irritabilidad y conflictos en el hogar. Se instala un cuadro de depresión profunda que no mejora con tratamiento farmacológico impuesto por psiquiatría y se decide tratamiento electroconvulsivo, después del cual cae en estado de coma con elementos de hipertensión intracraneal y focalización neurológica. La tomografía de urgencia evidencia un tumor intracraneal, con áreas de necrosis, infiltración y desplazamiento de estructuras adyacentes y signos de hipertensión intracraneal. Al realizar intervención microquirúrgica fallece. La necropsia reveló glioblastoma multiforme de alta malignidad con focos de necrosis y de hemorragias. Conclusiones: La depresión y manifestaciones de trastornos mentales pueden tener causa orgánica, un hecho que debe considerarse en el contexto clínico. La historia clínica bien obtenida, la evaluación psicopatológica y las técnicas de imágenes en la actualidad son herramientas fundamentales en la precisión diagnóstica(AU)


Introduction: Brain tumors sometimes have a complex and atypical clinical presentation at the beginning, depending on their location, which can be mistaken for psychiatric disorders. Objective: To describe a clinical case interpreted as a psychosis for its symptoms and whose diagnosis was a highly malignant glioblastoma multiforme. Clinical case: This is the case of a 35-year-old woman who, several months ago, started to present behavioral disorders, depressive symptoms, irritability, and conflicts at home. Clinical signs of deep depression onset, which does not improve with pharmacological treatment prescribed by the psychiatry specialist; electroconvulsive treatment is decided, after which she falls into a coma with elements of intracranial hypertension and a neurological focus. The emergency tomography shows an intracranial tumor, with necrotic areas, infiltration, and displacement of adjacent structures, as well as signs of intracranial hypertension. When microsurgical intervention is performed, she died. The necropsy revealed highly malignant glioblastoma multiforme with necrosis focuses and hemorrhage. Conclusions: Depression and manifestations of mental disorders may have an organic cause, a fact that must be considered in the clinical setting. A well-obtained clinical history, psychopathological evaluation, and imaging techniques are currently essential tools for an accurate diagnosis(AU)


Subject(s)
Humans , Female , Bipolar Disorder/diagnosis , Tomography, X-Ray Computed/methods , Glioblastoma/diagnostic imaging , Intracranial Hypertension/diagnosis
18.
Rev. habanera cienc. méd ; 19(3): e3379, mayo.-jun. 2020. graf
Article in Spanish | LILACS, CUMED | ID: biblio-1126890

ABSTRACT

Introducción: La COVID-19 y el Síndrome Respiratorio Agudo Severo o SARS-CoV-2 por el nuevo coronavirus está causando una pandemia con alta mortalidad. Aunque aún quedan incógnitas por definir como enfermedad infecciosa viral nueva se ha avanzado en los conocimientos en relación con el comportamiento clínico y la patogenia. Objetivo: Revisar las evidencias científicas más actuales sobre la patogenia de la enfermedad y su vínculo con la elevada mortalidad en adultos mayores afectados con comorbilidades. Material y Métodos: Se realizó una revisión de la literatura existente hasta la fecha en publicaciones de revistas indexadas en MEDLINE, LILACS, SciELO, LATINDEX, MEDIGRAPHY, MEDSCAPE, Science Direct Elsevier y PubMed y noticias divulgadas en boletines de la OMS/OPS, el Portal de INFOMED y otras agencias de noticias con buenas evidencias científicas. Desarrollo: Se realiza el análisis de los conocimientos actuales en la patogenia y el proceso inflamatorio pulmonar de no ser una simple neumonía viral sino un proceso inflamatorio local y sistémico que involucra diferentes órganos, trastornos de la coagulación y alteraciones en la inmunidad y hace más vulnerables sobre todo al adulto mayor con comorbilidades, al ocasionar gravedad y elevar la mortalidad. Conclusiones: La patogenia de esta enfermedad, mejor conocida en la actualidad, explica las implicaciones en los casos críticos y graves con elevada mortalidad, sobre todo en los más vulnerables. El SARS y sus complicaciones evolutivas no son explicables solo por la inflamación pulmonar. Intervienen otros factores involucrados en la conocida patogenia de mucha mayor gravedad que conducen a un desenlace fatal(AU)


Introduction: Coronavirus disease-2019 (COVID-19) and the Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2) are causing a pandemic associated with high mortality. Although many uncertainties still remain because it is a new viral infectious disease, knowledge of clinical behavior and pathogenesis has advanced. Objective: To review the most current scientific evidence on the pathogenesis of the disease and its association with high mortality in elderly patients with comorbidities. Material and Methods: A literature review of the information published to date on this respect was carried out. Databases such as MEDLINE, LILACS, SCIELO, LATINDEX, MEDIGRAPHIC, MEDSCAPE, Science Direct, Elsevier and PubMed were searched; important data were also obtained from WHO / PAHO bulletins, the Cuban National Health Care Telecommunications Network and Portal (infomed) and other news agencies that present good scientific evidence. Development: An analysis of the current knowledge about the pathogenesis and the pulmonary inflammatory process is carried out while observing that this process does not respond to a simple viral pneumonia but to a local and systemic inflammatory process that involves different organs, coagulation disorders and alterations of immunity that make elderly patients with comorbidities more vulnerable, causing severity and increasing mortality. Conclusions: The pathogenesis of this disease, which is better known at present, explains the implications in critical and severe cases with high mortality, especially the most vulnerable ones. SARS and its evolutive complications are not explained by lung inflammation only. Other factors are involved in the well-known pathogenesis of a much greater severity that leads to the fatal outcome(AU)


Subject(s)
Humans , Blood Coagulation , Delivery of Health Care , COVID-19
19.
Rev. Finlay ; 10(2): 78-88, abr.-jun. 2020. graf
Article in Spanish | LILACS-Express | LILACS | ID: biblio-1125657

ABSTRACT

RESUMEN En los últimos 40 años, la humanidad se ha visto afectada por tres pandemias de envergadura que han cobrado muchas muertes: el aumento de la incidencia y las tasas de prevalencia de las enfermedades crónicas no transmisibles, la pandemia de la enfermedad por el virus de inmunodeficiencia humana/sida y en la actualidad la pandemia por la COVID-19. El objetivo del presente artículo es dar a conocer la relación entre las enfermedades crónicas no transmisibles y la COVID-19, a pesar de que aún quedan incógnitas en el conocimiento de esta enfermedad nueva y el porqué de la elevada mortalidad que provoca. Se analiza la repercusión que tiene para las enfermedades crónicas la patogenia de la enfermedad. La mortalidad es elevada y se concentra fundamentalmente en mayores de 60 años y con enfermedades crónicas no transmisibles asociadas, donde tiene manifestaciones atípicas y efectos devastadores. La aparición de otro brote de enfermedad infecciosa humana causada por un patógeno nuevo subraya el desafío de las enfermedades infecciosas emergentes y la importancia de una preparación sostenida para enfrentarlo. Este ambiente trae aparejado el miedo, la desinformación y muchas incógnitas que aún quedan por dilucidar en futuras investigaciones.


ABSTRACT In the last 40 years, humanity has been affected by three major pandemics that have provoked many deaths: the increase in the incidence and prevalence rates of chronic non-communicable diseases, the pandemic of human immunodeficiency virus / AIDS and currently the pandemic by COVID-19. The objective of this article is to publicize the relationship between chronic non-communicable diseases and COVID-19, despite the fact that there are still unknowns about this new disease and the reasons for the high mortality it causes. The repercussion of the pathogenesis of this disease in chronic diseases is analyzed. Mortality is high mainly in patients aged over 60 and with associated chronic non-communicable diseases where it has atypical manifestations and devastating effects. The emergence of this new human infectious disease caused by an unknown pathogen highlights the challenge of emerging infectious diseases and the importance of permanent preparation to deal with them. This environment brings fear, misinformation and many unknowns that remain to be clarified with future research.

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