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1.
Kidney Blood Press Res ; 48(1): 545-555, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37517398

RESUMO

INTRODUCTION: The evidence about the optimal revascularization strategy in patients with left main coronary artery (LMCA) disease and impaired renal function is limited. Thus, we aimed to compare the outcomes of LMCA disease revascularization (percutaneous coronary intervention [PCI] vs. coronary artery bypass grafting [CABG]) in patients with and without impaired renal function. METHODS: This retrospective cohort study included 2,138 patients recruited from 14 centers between 2015 and 2,019. We compared patients with impaired renal function who had PCI (n= 316) to those who had CABG (n = 121) and compared patients with normal renal function who had PCI (n = 906) to those who had CABG (n = 795). The study outcomes were in-hospital and follow-up major adverse cardiovascular and cerebrovascular events (MACCE). RESULTS: Multivariable logistic regression analysis showed that the risk of in-hospital MACCE was significantly higher in CABG compared to PCI in patients with impaired renal function (odds ratio [OR]: 8.13 [95% CI: 4.19-15.76], p < 0.001) and normal renal function (OR: 2.59 [95% CI: 1.79-3.73]; p < 0.001). There were no differences in follow-up MACCE between CABG and PCI in patients with impaired renal function (HR: 1.14 [95% CI: 0.71-1.81], p = 0.585) and normal renal function (HR: 1.12 [0.90-1.39], p = 0.312). CONCLUSIONS: PCI could have an advantage over CABG in revascularization of LMCA disease in patients with impaired renal function regarding in-hospital MACCE. The follow-up MACCE was comparable between PCI and CABG in patients with impaired and normal renal function.


Assuntos
Doença da Artéria Coronariana , Intervenção Coronária Percutânea , Humanos , Intervenção Coronária Percutânea/efeitos adversos , Estudos Retrospectivos , Resultado do Tratamento , Ponte de Artéria Coronária/efeitos adversos , Doença da Artéria Coronariana/complicações , Doença da Artéria Coronariana/cirurgia , Rim/cirurgia
2.
Molecules ; 25(11)2020 May 31.
Artigo em Inglês | MEDLINE | ID: mdl-32486455

RESUMO

Infectious diseases are the second major cause of death worldwide, and the ability to resist multiple classes of antibiotics is the key factor in enabling pathogenic organisms to survive and spread in the nosocomial environment. Unfortunately, the available ß-lactamase inhibitors are not efficient against ß-lactamase B, C, and D which necessitates discovering either broad spectrum ß-lactamase inhibitors or new ß-lactam antibiotics resistant to bacterial enzymes. In this regard, products of natural origin have prompted the disclosure of new compounds and medicinal leads. Chloroform fraction of Clutia myricoides (Soa'bor) showed a pronounced activity against extended-spectrum ß-lactamase (ESBL) strains. Bio-guided fractionation resulted in isolation of two new compounds; 2-methoxy chrysophanol (2) and Saudin-I (5) in addition to three known compounds that were identified as chrysophanol (1), stigmasterol (3) and ß-sitosterol (4). Antibacterial and anti ESBL activities of the isolated compounds were performed. No antibacterial activities were detected for any of the tested compounds. Meanwhile, compound 2 showed promising anti ESBL activity. Compound 2 has shown an obvious activity against K. pneumoniae ATCC 700603 with a marked enlargement of inhibition zones (>5mm) in combination with third generation cephalosporin antibiotics. To further understand the mechanism of action of compound 2, molecular docking was carried out against CTX-M-27 ESBL. The results showed binding site interactions strikingly different from its analogue, compound 1, allowing compound 2 to be active against ESBL. These results proposed the concomitant use of these active compounds with antibiotics that would increase their efficiency. Nevertheless, the interaction between this active compound and antibiotics should be taken into consideration. Therefore, in order to evaluate the safety of this active compound, further in vitro and in vivo toxicity assays must be carried out.


Assuntos
Magnoliopsida/química , Inibidores de beta-Lactamases/química , beta-Lactamases/química , Antibacterianos/farmacologia , Sítios de Ligação , Bioensaio , Cefalosporinas/química , Clorofórmio/química , Escherichia coli/efeitos dos fármacos , Escherichia coli/enzimologia , Furanos/química , Klebsiella pneumoniae/efeitos dos fármacos , Klebsiella pneumoniae/enzimologia , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Modelos Moleculares , Simulação de Acoplamento Molecular , Ligação Proteica , Inibidores de beta-Lactamases/farmacologia
3.
Z Naturforsch C J Biosci ; 72(1-2): 35-41, 2017 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-27458662

RESUMO

A comparative investigation of hydro-distilled essential oils from aerial parts of Mentha longifolia L. (ML), Mentha microphylla K.Koch (MM), Mentha australis R.Br. (MA), and Teucrium polium L. (TP) growing in Al Madinah Al Munawwarah, Saudi Arabia, was carried out. The total numbers of identified constituents were 22, 23, 14, and 20 in ML, MM, MA, and TP oils, representing 93.0, 99.3, 78.1, and 81.1% of the total oil composition, respectively. Pulegone (40.7%) and cineole (33.4%) were the major components in ML, whereas carvone (64.6%) was the major one in MM. Furthermore, ß-linalool (22.9%) and α-terpineol (12%) were the major components in MA, whereas, (E)-3-caren-2-ol accounted for 12.1% in TP. The essential oils of TP and MA exhibited promising activities against Leishmania donovani promastigotes with IC50 values of 2.3 and 3.7 µg/mL, respectively. In contrast, MA essential oils exhibited antifungal activities towards Candida krusei and C. glabrata with IC50 values of 1 and 1.2 µg/mL, respectively.


Assuntos
Mentha/química , Óleos Voláteis/isolamento & purificação , Óleos de Plantas/isolamento & purificação , Teucrium/química , Antifúngicos/isolamento & purificação , Antifúngicos/farmacologia , Antimaláricos/isolamento & purificação , Antimaláricos/farmacologia , Antiprotozoários/isolamento & purificação , Antiprotozoários/farmacologia , Avaliação Pré-Clínica de Medicamentos , Fungos/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas , Leishmania donovani/efeitos dos fármacos , Óleos Voláteis/farmacologia , Óleos de Plantas/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Arábia Saudita , Especificidade da Espécie
4.
BMC Complement Altern Med ; 16: 359, 2016 Sep 13.
Artigo em Inglês | MEDLINE | ID: mdl-27618982

RESUMO

BACKGROUND: Exaggerated vasoconstriction plays a very important role in the hypertension, a major component of metabolic syndrome (MetS). In the current work, the potential protective effect of methanol extract of fruit hulls of Garcinia mangostana L. on the exaggerated vasoconstriction in MetS has been investigated. In addition, the bioactive fraction and compounds as well as the possible mechanism of action have been illustrated. METHODS: The effect of methanol extract of G. mangostana (GMT) fruit hulls on the vascular reactivity of aorta isolated from animals with MetS was investigated through bioassay-guided fractionation procedures. GMT was partitioned with chloroform (I) and the remaining mother liquor was fractionated on a Diaion HP-20 with H2O, 50 and 100 % methanol to give fractions II, III, and IV, respectively. The effect of total extract (GMT), bioactive fraction and the bioactive compounds on the vasoconstriction were examined in aortae isolated from animals with MetS by incubation for 30 min before exposing aortae to cumulative concentrations of phenylephrine (PE). The direct relaxant effect was also examined by adding cumulative concentrations of the bioactive fraction and its bioactive compounds to PE precontracted vessels. In addition, aortic nitric oxide (NO) and reactive oxygen species (ROS) production was investigated. RESULTS: Bioassay-guided fractionation of GMT revealed isolation of garcimangosone D (1), aromadendrin-8-C-ß-D-glucopyranoside (2), 2,4,3'-trihydroxy benzophenone-6-O-ß-D-glucopyranoside (3), maclurin-6-O-ß-D-glucopyranoside (rhodanthenone) (4), epicatechin (5), and 2,3',4,5',6-pentahydroxy benzophenone (6). Only compounds 2, 4, and 5 significantly alleviated the exaggerated vasoconstriction of MetS aortae and in the same time showed significant vasodilation of PE pre-contracted aortae. To further illustrate the mechanism of action, the observed vasodilation was completely blocked by the nitric oxide (NO) synthase inhibitor, Nω-nitro-L-arginine methyl ester hydrochloride and inhibited by guanylate cyclase inhibitor, methylene blue. However, vasodilation was not affected by the potassium channel blocker, tetraethylammonium or the cyclooxygenase inhibitor, indomethacin. In addition, compounds 2, 4, and 5 stimulated NO generation from isolated aortae to levels comparable with acetylcholine. Furthermore, 4 and 5 inhibited reactive oxygen species generation in MetS aortae. CONCLUSION: The phenolic compounds 2, 4, and 5 ameliorated the exaggerated vasoconstriction in MetS aortae through vasodilatation-NO generation mechanism.


Assuntos
Garcinia mangostana/química , Síndrome Metabólica/metabolismo , Óxido Nítrico/metabolismo , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Substâncias Protetoras/farmacologia , Vasoconstrição/efeitos dos fármacos , Animais , Aorta/efeitos dos fármacos , Masculino , Fenóis/química , Extratos Vegetais/química , Substâncias Protetoras/química , Ratos , Ratos Wistar , Vasodilatação/efeitos dos fármacos
5.
Molecules ; 21(2): 251, 2016 Feb 22.
Artigo em Inglês | MEDLINE | ID: mdl-26907243

RESUMO

Accumulation of Advanced Glycation Endproducts (AGEs) in body tissues plays a major role in the development of diabetic complications. Here, the inhibitory effect of bioactive metabolites isolated from fruit hulls of Garcinia mangostana on AGE formation was investigated through bio-guided approach using aminoguanidine (AG) as a positive control. Including G. mangostana total methanol extract (GMT) in the reaction mixture of bovine serum albumin (BSA) and glucose or ribose inhibited the fluorescent and non-fluorescent AGEs formation in a dose dependent manner. The bioassay guided fractionation of GMT revealed isolation of four bioactive constituents from the bioactive fraction; which were identified as: garcimangosone D (1), aromadendrin-8-C-glucopyranoside (2), epicatechin (3), and 2,3',4,5',6-pentahydroxybenzophenone (4). All the tested compounds significantly inhibited fluorescent and non-fluorescent AGEs formation in a dose dependent manner whereas compound 3 (epicatechin) was found to be the most potent. In search for the level of action, addition of GMT, and compounds 2-4 inhibited fructosamine (Amadori product) and protein aggregation formation in both glucose and ribose. To explore the mechanism of action, it was found that addition of GMT and only compound (3) to reaction mixture increased protein thiol in both glucose and ribose while compounds 1, 2 and 4 only increased thiol in case of ribose. In conclusion, phenolic compounds 1-4 inhibited AGEs formation at the levels of Amadori product and protein aggregation formation through saving protein thiol.


Assuntos
Garcinia mangostana/química , Produtos Finais de Glicação Avançada/antagonistas & inibidores , Agregação Patológica de Proteínas/tratamento farmacológico , Compostos de Sulfidrila/química , Animais , Benzofenonas/química , Benzofenonas/isolamento & purificação , Benzofenonas/uso terapêutico , Catequina/química , Catequina/isolamento & purificação , Catequina/uso terapêutico , Bovinos , Flavonoides/química , Flavonoides/isolamento & purificação , Flavonoides/uso terapêutico , Glucose/química , Glucosídeos/química , Glucosídeos/isolamento & purificação , Glucosídeos/uso terapêutico , Produtos Finais de Glicação Avançada/química , Extratos Vegetais/química , Soroalbumina Bovina/química
6.
Mar Drugs ; 13(11): 6609-19, 2015 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-26516870

RESUMO

In the course of our continuing efforts to identify bioactive secondary metabolites from Red Sea marine invertebrates, we have investigated the sponge Hemimycale arabica. The antimicrobial fraction of an organic extract of the sponge afforded two new hydantoin alkaloids, hemimycalins A and B (2 and 3), together with the previously reported compound (Z)-5-(4-hydroxybenzylidene)imidazolidine-2,4-dione (1). The structures of the compounds were determined by extensive 1D and 2D NMR (COSY, HSQC and HMBC) studies and high-resolution mass spectral determinations. Hemimycalins A (2) and B (3) represent the first examples of the natural N-alkylated hydantoins from the sponge Hemimycale arabica. Compounds 1-3 displayed variable antimicrobial activities against E. coli, S. aureus, and C. albicans. In addition, compound 1 displayed moderate antiproliferative activity against the human cervical carcinoma (HeLa) cell line. These findings provide further insight into the chemical diversity as well as the biological activity of this class of compounds.


Assuntos
Alcaloides/farmacologia , Anti-Infecciosos/farmacologia , Hidantoínas/farmacologia , Poríferos/metabolismo , Alcaloides/química , Alcaloides/isolamento & purificação , Animais , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Candida albicans/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Feminino , Células HeLa , Humanos , Hidantoínas/química , Hidantoínas/isolamento & purificação , Oceano Índico , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Metabolismo Secundário , Staphylococcus aureus/efeitos dos fármacos , Neoplasias do Colo do Útero/tratamento farmacológico
7.
Crit Pathw Cardiol ; 23(1): 12-16, 2024 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-37948094

RESUMO

BACKGROUND: The use of dual antiplatelet therapy (DAPT) after coronary revascularization for left-main disease is still debated. The study aimed to characterize patients who received dual versus single antiplatelet therapy (SAPT) after coronary artery bypass grafting (CABG) for unprotected left-main disease and compare the outcomes of those patients. RESULTS: This multicenter retrospective cohort study included 551 patients who were grouped into 2 groups: patients who received SAPT (n = 150) and those who received DAPT (n = 401). There were no differences in age ( P = 0.451), gender ( P = 0.063), smoking ( P = 0.941), diabetes mellitus ( P = 0.773), history of myocardial infarction ( P = 0.709), chronic kidney disease ( P = 0.615), atrial fibrillation ( P = 0.306), or cerebrovascular accident ( P = 0.550) between patients who received SAPT versus DAPT. DAPTs were more commonly used in patients with acute coronary syndrome [87 (58%) vs. 273 (68.08%); P = 0.027], after off-pump CABG [12 (8%) vs. 73 (18.2%); P = 0.003] and in patients with radial artery grafts [1 (0.67%) vs. 32 (7.98%); P < 0.001]. While SAPTs were more commonly used in patients with low ejection fraction [55 (36.67%) vs. 61 (15.21%); P < 0.001] and in patients with postoperative acute kidney injury [27 (18%) vs. 37 (9.23%); P = 0.004]. The attributed treatment effect of DAPT for follow-up major adverse cerebrovascular and cardiac events was not significantly different from that of SAPT [ß, -2.08 (95% confidence interval (CI), -20.8-16.7); P = 0.828]. The attributed treatment effect of DAPT on follow-up all-cause mortality was not significantly different from that of SAPT [ß, 4.12 (CI, -11.1-19.32); P = 0.595]. There was no difference in bleeding between groups ( P = 0.666). CONCLUSIONS: DAPTs were more commonly used in patients with acute coronary syndrome, after off-pump CABG, and with radial artery grafts. SAPTs were more commonly used in patients with low ejection fraction and acute kidney injury. Patients on DAPT after CABG for left-main disease had comparable major adverse cerebrovascular and cardiac events and survival to patients on SAPT, with no difference in bleeding events.


Assuntos
Síndrome Coronariana Aguda , Injúria Renal Aguda , Doença da Artéria Coronariana , Intervenção Coronária Percutânea , Humanos , Inibidores da Agregação Plaquetária/uso terapêutico , Síndrome Coronariana Aguda/cirurgia , Síndrome Coronariana Aguda/induzido quimicamente , Estudos Retrospectivos , Resultado do Tratamento , Ponte de Artéria Coronária/efeitos adversos , Hemorragia/induzido quimicamente , Injúria Renal Aguda/induzido quimicamente
8.
Eur J Med Res ; 28(1): 210, 2023 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-37393361

RESUMO

BACKGROUND: The optimal revascularization strategy in patients with left main coronary artery (LMCA) disease in the emergency setting is still controversial. Thus, we aimed to compare the outcomes of percutaneous coronary interventions (PCI) vs. coronary artery bypass grafting (CABG) in patients with and without emergent LMCA disease. METHODS: This retrospective cohort study included 2138 patients recruited from 14 centers between 2015 and 2019. We compared patients with emergent LMCA revascularization who underwent PCI (n = 264) to patients who underwent CABG (n = 196) and patients with non-emergent LMCA revascularization with PCI (n = 958) to those who underwent CABG (n = 720). The study outcomes were in-hospital and follow-up all-cause mortality and major adverse cardiovascular and cerebrovascular events (MACCE). RESULTS: Emergency PCI patients were older and had a significantly higher prevalence of chronic kidney disease, lower ejection fraction, and higher EuroSCORE than CABG patients. CABG patients had significantly higher SYNTAX scores, multivessel disease, and ostial lesions. In patients presenting with arrest, PCI had significantly lower MACCE (P = 0.017) and in-hospital mortality (P = 0.016) than CABG. In non-emergent revascularization, PCI was associated with lower MACCE in patients with low (P = 0.015) and intermediate (P < 0.001) EuroSCORE. PCI was associated with lower MACCE in patients with low (P = 0.002) and intermediate (P = 0.008) SYNTAX scores. In non-emergent revascularization, PCI was associated with reduced hospital mortality in patients with intermediate (P = 0.001) and high (P = 0.002) EuroSCORE compared to CABG. PCI was associated with lower hospital mortality in patients with low (P = 0.031) and intermediate (P = 0.001) SYNTAX scores. At a median follow-up time of 20 months (IQR: 10-37), emergency PCI had lower MACCE compared to CABG [HR: 0.30 (95% CI 0.14-0.66), P < 0.003], with no significant difference in all-cause mortality between emergency PCI and CABG [HR: 1.18 (95% CI 0.23-6.08), P = 0.845]. CONCLUSIONS: PCI could be advantageous over CABG in revascularizing LMCA disease in emergencies. PCI could be preferred for revascularization of non-emergent LMCA in patients with intermediate EuroSCORE and low and intermediate SYNTAX scores.


Assuntos
Doença da Artéria Coronariana , Intervenção Coronária Percutânea , Humanos , Estudos Retrospectivos , Ponte de Artéria Coronária/efeitos adversos , Doença da Artéria Coronariana/cirurgia
9.
Cardiovasc Revasc Med ; 46: 52-61, 2023 01.
Artigo em Inglês | MEDLINE | ID: mdl-35961856

RESUMO

BACKGROUND: Real-world data for managing patients with diabetes and left main coronary artery (LMCA) disease are scarce. We compared percutaneous coronary intervention (PCI) outcomes versus coronary artery bypass grafting (CABG) in diabetes and LMCA disease patients. METHODS: We retrospectively studied patients with LMCA presented to 14 centers from 2015 to 2019. The study included 2138 patients with unprotected LMCA disease; 1468 (68.7 %) had diabetes. Patients were grouped into; diabetes with PCI (n = 804) or CABG (n = 664) and non-diabetes with PCI (n = 418) or CABG (n = 252). RESULTS: In diabetes, cardiac (34 (5.1 %) vs. 22 (2.7 %); P = 0.016), non-cardiac (13 (2 %) vs. 6 (0.7 %); P = 0.027) and total hospital mortality (47 (7.1 %) vs. 28 (3.5 %); P = 0.0019), myocardial infarction (45 (6.8 %) vs. 11 (1.4 %); P = 0.001), cerebrovascular events (25 (3.8 %) vs. 12 (1.5 %); P = 0.005) and minor bleeding (65 (9.8 %) vs. 50 (6.2 %); P = 0.006) were significantly higher in CABG patients compared to PCI; respectively. The median follow-up time was 20 (10-37) months. In diabetes, total mortality was higher in CABG (P = 0.001) while congestive heart failure was higher in PCI (P = 0.001). There were no differences in major adverse cerebrovascular events and target lesion revascularization between PCI and CABG. Predictors of mortality in diabetes were high anatomical SYNTAX, peripheral arterial disease, chronic kidney disease, and cardiogenic shock. CONCLUSIONS: In this multicenter retrospective study, we found no significant difference in clinical outcomes during the short-term follow-up between PCI with second-generation DES and CABG except for lower total mortality and a higher rate of congestive heart failure in PCI group of patients. Randomized trials to characterize patients who could benefit from each treatment option are needed.


Assuntos
Doença da Artéria Coronariana , Diabetes Mellitus , Insuficiência Cardíaca , Intervenção Coronária Percutânea , Humanos , Doença da Artéria Coronariana/diagnóstico por imagem , Doença da Artéria Coronariana/cirurgia , Estudos Retrospectivos , Intervenção Coronária Percutânea/efeitos adversos , Revascularização Miocárdica , Diabetes Mellitus/diagnóstico , Diabetes Mellitus/epidemiologia , Insuficiência Cardíaca/etiologia , Resultado do Tratamento
10.
Int J Gen Med ; 11: 457-461, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30584348

RESUMO

OBJECTIVES: Type 2 diabetes mellitus (DM-II) is highly prevalent in Saudi Arabia and only few studies have assessed it as a risk factor for hypothyroidism. This study aimed to examine the association between DM-II and hypothyroidism. SUBJECTS AND METHODS: We conducted a hospital-based case-control study. As cases, we included all adults admitted to King Abdulaziz University Hospital (KAUH) with laboratory-confirmed hypothyroidism. As controls, we drew a random sample of patients admitted to the orthopedic clinic at KAUH with laboratory-confirmed absence of hypothyroidism. We extracted data from the medical records regarding age, sex, presence of DM-II, HbA1c, comorbidities, treatment, and complications. We used multivariate logistic regression to identify factors associated with hypothyroidism. RESULTS: We included 121 cases and 121 controls. In comparison to controls, cases were older (P=0.005), had higher prevalence of DM-II (P<0.001), had higher levels of HbA1c (P=0.03), used insulin (P<0.001) and oral hypoglycemic drugs (P<0.001) more often, and suffered more often from hypertension (P<0.001), coronary artery disease (CAD) (P<0.001), stroke (P=0.04), diabetic foot (P<0.001), and nephropathy (P<0.001). According to multivariate regression, the risk of hypothyroidism was significantly increased among patients with DM-II (OR=4.14; 95% CI=20.20-7.80; P<0.001) and CAD (OR=14.15; 95% CI=1.80-111.43; P=0.01). CONCLUSION: Patients with DM-II were at increased risk of developing hypothyroidism. Adequate management and control of DM-II might reduce the risk of developing hypothyroidism. Further research using a prospective cohort study design is needed to confirm these findings. KEY MESSAGES: Patients with DM-II had an increased risk of developing hypothyroidism.

11.
J Nat Med ; 71(1): 216-226, 2017 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-27738860

RESUMO

Advanced glycation end-products (AGEs) are associated with a non-enzymatic reaction between the amino group of a protein and the carbonyl group of a sugar during hyperglycemia. The precipitation of AGEs in different tissues leads to many complications, such as endothelial dysfunction, cardiovascular complications, atherosclerosis, retinopathy, neuropathy, and Alzheimer's disease. Garcinia mangostana L. (Clusiaceae) (GM) was selected owing to the ability of its polar and non-polar fractions to inhibit AGE formation. For the first time, the bioguided fractionation of its pericarp MeOH extract (GMT) gave rise to two new xanthones, namely, mangostanaxanthones III (1) and IV (3), in addition to six known compounds, ß-mangostin (2), garcinone E (4), rubraxanthone (5), α-mangostin (6), garcinone C (7), and 9-hydroxycalabaxanthone (8), from the non-polar faction. Their structures were verified by various spectroscopic methods, including 1D and 2D NMR studies and high-resolution MS data. All of the isolated xanthones significantly inhibited both sugar (ribose) and dicarbonyl compound (methylglyoxal)-induced protein glycation in a dose-dependent manner. This is explained by the ability of the isolated xanthones to inhibit protein oxidation, as indicated by the decreases in dityrosine and N'-formylkynurenine formation.


Assuntos
Frutas/química , Garcinia mangostana/química , Produtos Finais de Glicação Avançada/antagonistas & inibidores , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Estrutura Molecular
12.
Saudi Med J ; 37(8): 834-42, 2016 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-27464858

RESUMO

Incretin-based therapies such as glucagon-like peptide-1 (GLP-1) receptor agonists (RA) and dipeptidyl peptidase-4 (DPP-4) inhibitors have gained prominence in recent years for the treatment of type 2 diabetes (T2D). Such therapies offer the potential to stimulate endogenous insulin activity in proportion to circulating glucose levels; thereby, lowering the risk of hypoglycemic episodes. The synthetic GLP-1 RA exenatide, the human GLP-1 RA liraglutide, and the DPP-4 inhibitor sitagliptin are the first agents in their respective classes to be approved for the treatment of T2D and their efficacy and safety has been studied extensively in clinical trials. This article reviewed the efficacy of liraglutide once daily in achieving clinical guidelines-recommended glycated hemoglobin A1c levels in patients with T2D compared with exenatide twice daily, or sitagliptin once daily, based on published literature, with an aim to elucidate the preferred choice of incretin-related therapy in treating uncontrolled T2D.


Assuntos
Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Liraglutida/uso terapêutico , Peptídeos/uso terapêutico , Fosfato de Sitagliptina/uso terapêutico , Peçonhas/uso terapêutico , Esquema de Medicação , Exenatida , Hemoglobinas Glicadas/análise , Humanos , Hipoglicemiantes/administração & dosagem , Liraglutida/administração & dosagem , Peptídeos/administração & dosagem , Fosfato de Sitagliptina/administração & dosagem , Peçonhas/administração & dosagem
13.
Nat Prod Res ; 28(19): 1583-90, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24938488

RESUMO

One new compound, (2S)-1-O-(Z)-tetracos-6-enoate glycerol (1) named urgineaglyceride A, along with six known compounds, 3,5,7,3',5'-pentahydroxydihydroflavonol (2), stigmasterol (3), (25S)-5ß-furostane-3ß-22α-26-triol (4), scillaridin A (5), (2S)-(+)-2-hydroxynaringenin-4'-O-ß-D-glucopyranoside (6) and quercetin-3'-O-ß-D-glucopyranoside (7), were isolated from the EtOAc fraction of Drimia maritima (L.) Stearn bulbs. Their structures were secured based on their IR, UV, 1D and 2D NMR data, in addition to HR-MS data and comparison with the literature data. The isolated compounds were evaluated for their in vitro growth inhibitory activity against A549 non-small cell lung cancer (NSCLC), U373 glioblastoma (GBM) and PC-3 prostate cancer cell lines. Compounds 2 and 3 displayed variable activities against the tested cancer cell lines. Compound 2 was a selective inhibitor of the NSCLC cell line with an IC50 of 2.3 µM, whereas 3 was selective against GBM with IC50 of 0.5 µM and against PC-3 with 2.0 µM.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Liliaceae/química , Monoglicerídeos/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Egito , Humanos , Concentração Inibidora 50 , Masculino , Estrutura Molecular , Monoglicerídeos/química , Monoglicerídeos/farmacologia , Monossacarídeos , Ressonância Magnética Nuclear Biomolecular , Raízes de Plantas/química , Quercetina/análogos & derivados
14.
Rev. bras. farmacogn ; 29(2): 206-212, Mar.-Apr. 2019. tab, graf
Artigo em Inglês | LILACS-Express | LILACS | ID: biblio-1003495

RESUMO

ABSTRACT A new xanthone: mangostanaxanthone VIIII [1,3,5,6,7-pentahydroxy-2-(3-methylbut-2-enyl)-8-(3-hydroxy-3-methylbut-1-enyl) xanthone] (5) and four known xanthones: mangostanaxanthones I (1) and II (2), γ-mangostin (3), and mangostanaxanthone VII (4) were separated and characterized from the acetone fraction of Garcinia mangostana L., Clusiaceae (mangosteen) pericarps. Their structures were established based on various spectroscopic analyses in addition to HRMS and comparison with the literature. The α-amylase inhibitory potential of the isolated metabolites was evaluated. Compounds 1, 2, and 5 had the highest activity with % inhibition 72.5, 86.5, and 81.8, respectively compared to acarbose (97.1%, reference α-amylase inhibitor). The molecular docking study of the tested metabolites was estimated to shade up the rational explanation of the α-amylase inhibitory activity results. Moreover, the pharmacokinetic parameters were assessed using Swiss ADME. It is noteworthy that 1, 2, and 5 had similar binding poses as the X-ray crystal structure of acarbose, whereas the other metabolites possessed different binding mode that decreased their inhibitory capacity. Thus, these data reinforced the health benefit of mangosteen as an alternative medicine to help lowering the postprandial glucose absorption. Therefore, it could have a good potential for the treatment of diabetes.

15.
Stand Genomic Sci ; 9(3): 1003-19, 2014 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-25197479

RESUMO

Clostridium jeddahense strain JCD(T) (= CSUR P693 = DSM 27834) is the type strain of C. jeddahense sp. nov. This strain, whose genome is described here, was isolated from the fecal flora of an obese 24 year-old Saudian male (BMI=52 kg/m(2)). Clostridium jeddahense strain JCD(T) is an obligate Gram-positive bacillus. Here we describe the features of this organism, together with the complete genome sequence and annotation. The 3,613,503 bp long genome (1 chromosome, no plasmid) exhibits a G+C content of 51.95% and contains 3,462 protein-coding and 53 RNA genes, including 4 rRNA genes.

16.
Rev. bras. farmacogn ; 28(3): 320-324, May-June 2018. tab, graf
Artigo em Inglês | LILACS | ID: biblio-958873

RESUMO

ABSTRACT Cyperus rotundus L. (Suada, Sueda, family: Cyperaceae) is vastly spread in several world's subtropical and tropical regions. It had variable traditional uses and bioactivities. A new flavonol derivative: cyperaflavoside (myricetin 3,3',5'-trimethyl ether 7-O-β-D-glucopyranoside) and five flavonoids: vitexin, orientin, cinaroside, quercetin 3-O-β-D-glucopyranoside, and myrcetin 3-O-β-D-glucopyranoside were separated from the methanolic extract of C. rotundus aerial parts. Their structures were verified based on UV, IR, NMR (1D and 2D), HRESIMS, and comparison with literature. All metabolites were assessed for their 5-lipoxygenase inhibitory potential. All compounds possessed 5-lipoxygenase inhibitory potentials with IC50s 5.1, 4.5, 5.9, 4.0, 3.7, and 2.3 µM, respectively, in comparison to indomethacin (IC50 0.98 µM). These results supported the traditional uses of C. rotundus in treating inflammation and its related symptoms.

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