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1.
BMC Nephrol ; 24(1): 168, 2023 06 12.
Artículo en Inglés | MEDLINE | ID: mdl-37308813

RESUMEN

BACKGROUND: A vegetarian diet is a popular alternative to the casual diet - it is considered healthy, and was proven to positively affect cardiovascular health. The Chronic Kidney Disease (CKD) progression is a major issue in the healthcare system, and constitutes a leading cause of death for 1.5% of the global population. The objective of this systematic review was to investigate the potential impact of a vegetarian diet on kidney function in CKD patients. METHOD: Our systematic review focused on randomized controlled trials (RCTs) which compared the effects of a vegetarian diet (experimental) and a standard omnivore diet (comparator) in terms of the estimated glomerular filtration rate (eGFR) in CKD patients. Inclusion criteria were based on PICO elements, with two researchers involved in browsing the Cochrane and Pubmed search engines. The investigation was performed using the PRISMA 2020 Checklist and PRISMA 2020 flow diagram. The search terms included: 'vegetarian diet' AND 'nephropathy', 'eGFR', 'albuminuria', 'chronic kidney disease'. Bias assessment was performed using RoB 2 tool to determine the validity of the data collected from studies. RESULTS: Four RCTs with a total of 346 participants were included in the presented systematic review. Two largest RCTs reported an increase in eGFR following a change to a vegetarian diet (p = 0.01 and p = 0.001). Another two found no significant differences between the experimental and control groups, also these trials were associated with a high risk of bias in terms of missing data outcome and the randomization process. CONCLUSIONS: The findings collected in this systematic review suggest that a vegetarian diet improves renal filtration function in CKD patients. Therefore, it seems essential to conduct further research involving the impact of the diet on the progression of CKD.


Asunto(s)
Dieta Vegetariana , Insuficiencia Renal Crónica , Humanos , Albuminuria , Lista de Verificación , Vegetarianos
2.
Int J Mol Sci ; 24(2)2023 Jan 06.
Artículo en Inglés | MEDLINE | ID: mdl-36674653

RESUMEN

This study aimed to examine if methanolic extracts of Pulsatilla vulgaris Mill. can inhibit HeLa cell proliferation through the modulation of cancer-related signaling pathways. The cytotoxicity and chemical composition of P. vulgaris leaves and root extracts were also determined. Research showed that root extract of P. vulgaris inhibited 12 signaling pathways in a cervical cancer cell line and the most potent activation inhibition was observed for MYC, Notch, Wnt, E2F, Ets, Stat3, Smad, Hdghog, AP-1, and NF-κB, at a concentration of 40 µg/mL. The methanolic extracts of P. vulgaris enhanced apoptotic death and deregulated cellular proliferation, differentiation, and progression toward the neoplastic phenotype by altering key signaling molecules required for cell cycle progression. This is the first study to report the influence of P. vulgaris on cancer signaling pathways. Additionally, our detailed phytochemical analysis of the methanolic extracts of P. vulgaris gives a conclusion that compounds, which strongly suppressed the growth and proliferation of HeLa cancer cells were mainly triterpenoid saponins accompanied by phenolic acids.


Asunto(s)
Neoplasias , Pulsatilla , Humanos , Células HeLa , Genes Reporteros , Transducción de Señal , Proliferación Celular , Extractos Vegetales/farmacología , Extractos Vegetales/química , Línea Celular Tumoral , Apoptosis
3.
Molecules ; 28(5)2023 Feb 27.
Artículo en Inglés | MEDLINE | ID: mdl-36903448

RESUMEN

Natural bioresources, predominantly plants, have always been regarded as the richest source of drugs for diseases threatening humanity. Additionally, microorganism-originating metabolites have been extensively explored as weapons against bacterial, fungal, and viral infections. However, the biological potential of metabolites produced by plant endophytes still remains understudied, despite significant efforts reflected in recently published papers. Thus, our goal was to evaluate the metabolites produced by endophytes isolated from Marchantia polymorpha and to study their biological properties, namely anticancer and antiviral potential. The cytotoxicity and anticancer potential were assessed using the microculture tetrazolium technique (MTT) against non-cancerous VERO cells and cancer cells-namely the HeLa, RKO, and FaDu cell lines. The antiviral potential was tested against the human herpesvirus type-1 replicating in VERO cells by observing the influence of the extract on the virus-infected cells and measuring the viral infectious titer and viral load. The most characteristic metabolites identified in the ethyl acetate extract and fractions obtained by use of centrifugal partition chromatography (CPC) were volatile cyclic dipeptides, cyclo(l-phenylalanyl-l-prolyl), cyclo(l-leucyl-l-prolyl), and their stereoisomers. In addition to the diketopiperazine derivatives, this liverwort endophyte also produced arylethylamides and fatty acids amides. The presence of N-phenethylacetamide and oleic acid amide was confirmed. The endophyte extract and isolated fractions showed a potential selective anticancer influence on all tested cancer cell lines. Moreover, the extract and the first separated fraction noticeably diminished the formation of the HHV-1-induced cytopathic effect and reduced the virus infectious titer by 0.61-1.16 log and the viral load by 0.93-1.03 log. Endophytic organisms produced metabolites with potential anticancer and antiviral activity; thus, future studies should aim to isolate pure compounds and evaluate their biological activities.


Asunto(s)
Endófitos , Marchantia , Animales , Chlorocebus aethiops , Humanos , Endófitos/química , Células Vero , Bacterias , Antivirales/farmacología
4.
Molecules ; 28(7)2023 Apr 05.
Artículo en Inglés | MEDLINE | ID: mdl-37050009

RESUMEN

The mutualistic coexistence between the host and endophyte is diverse and complex, including host growth regulation, the exchange of substances like nutrients or biostimulants, and protection from microbial or herbivore attack. The latter is commonly associated with the production by endophytes of bioactive natural products, which also possess multiple activities, including antibacterial, insecticidal, antioxidant, antitumor, and antidiabetic properties, making them interesting and valuable model substances for future development into drugs. The endophytes of higher plants have been extensively studied, but there is a dearth of information on the biodiversity of endophytic microorganisms associated with bryophytes and, more importantly, their bioactive metabolites. For the first time, we name bryophyte endophytes "bryendophytes" to elaborate on this important and productive source of biota. In this review, we summarize the current knowledge on the diversity of compounds produced by endophytes, emphasizing bioactive molecules from bryendophytes. Moreover, the isolation methods and biodiversity of bryendophytes from mosses, liverworts, and hornworts are described.


Asunto(s)
Briófitas , Hepatophyta , Hongos/metabolismo , Simbiosis , Endófitos/metabolismo
5.
Molecules ; 28(12)2023 Jun 17.
Artículo en Inglés | MEDLINE | ID: mdl-37375384

RESUMEN

The large quantity of olive roots resulting from a large number of old and unfruitful trees encouraged us to look for ways of adding value to these roots. For this reason, the current research work is devoted to the valorization of olive roots by identifying active phytochemicals and assessing their biological activities, including the cytotoxicity and antiviral potential of different extracts from the Olea europaea Chemlali cultivar. The extract, obtained by ultrasonic extraction, was analyzed using the liquid chromatography-mass spectrometry technique (LC-MS). The cytotoxicity was evaluated through the use of the microculture tetrazolium assay (MTT) against VERO cells. Subsequently, the antiviral activity was determined for HHV-1 (Human Herpesvirus type 1) and CVB3 (Coxsackievirus B3) replication in the infected VERO cells. LC-MS analysis allowed the identification of 40 compounds, classified as secoiridoids (53%), organic acids (13%), iridoids (10%), lignans (8%), caffeoylphenylethanoid (5%), phenylethanoids (5%),sugars and derivatives (2%), phenolic acids (2%), and flavonoids (2%). It was found that extracts were not toxic to the VERO cells. Moreover, the extracts did not influence the appearance of HHV-1 or CVB3 cytopathic effects in the infected VERO cells and failed to decrease the viral infectious titer.


Asunto(s)
Olea , Chlorocebus aethiops , Animales , Humanos , Olea/química , Espectrometría de Masas en Tándem/métodos , Espectrometría de Masa por Ionización de Electrospray/métodos , Células Vero , Cromatografía Líquida de Alta Presión/métodos , Fenoles/química , Hojas de la Planta/química , Cromatografía Liquida , Iridoides/química , Extractos Vegetales/química , Flavonoides/química
6.
Molecules ; 28(22)2023 Nov 10.
Artículo en Inglés | MEDLINE | ID: mdl-38005252

RESUMEN

In the present study, we performed comprehensive LC-MS chemical profiling and biological tests of Vepris boiviniana leaves and stem bark extracts of different polarities. In total, 60 bioactive compounds were tentatively identified in all extracts. The 80% ethanolic stem bark extract exhibited the highest activity in the ABTS assay, equal to 551.82 mg TE/g. The infusion extract of stem bark consistently demonstrated elevated antioxidant activity in all assays, with values ranging from 137.39 mg TE/g to 218.46 mg TE/g. Regarding the enzyme inhibitory assay, aqueous extracts from both bark and leaves exhibited substantial inhibition of AChE, with EC50 values of 2.41 mg GALAE/g and 2.25 mg GALAE/g, respectively. The 80% ethanolic leaf extract exhibited the lowest cytotoxicity in VERO cells (CC50: 613.27 µg/mL) and demonstrated selective cytotoxicity against cancer cells, particularly against H1HeLa cells, indicating potential therapeutic specificity. The 80% ethanolic bark extract exhibited elevated toxicity in VERO cells but had reduced anticancer selectivity. The n-hexane extracts, notably the leaves' n-hexane extract, displayed the highest toxicity towards non-cancerous cells with selectivity towards H1HeLa and RKO cells. In viral load assessment, all extracts reduced HHV-1 load by 0.14-0.54 log and HRV-14 viral load by 0.13-0.72 log, indicating limited antiviral activity. In conclusion, our research underscores the diverse bioactive properties of Vepris boiviniana extracts, exhibiting potent antioxidant, enzyme inhibitory, and cytotoxicity potential against cancer cells.


Asunto(s)
Antioxidantes , Extractos Vegetales , Animales , Chlorocebus aethiops , Antioxidantes/farmacología , Antioxidantes/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Células Vero , Fitoquímicos/farmacología , Fitoquímicos/química , Etanol , Antivirales/farmacología
7.
Molecules ; 28(14)2023 Jul 19.
Artículo en Inglés | MEDLINE | ID: mdl-37513392

RESUMEN

Phytogenically synthesised nanoparticle (NP)-based drug delivery systems have promising potential in the field of biopharmaceuticals. From the point of view of biomedical applications, such systems offer the small size, high surface area, and possible synergistic effects of NPs with embedded biomolecules. This article describes the synthesis of silver nanoparticles (Ag-NPs) using extracts from the flowers and leaves of tansy (Tanacetum vulgare L.), which is known as a remedy for many health problems, including cancer. The reducing power of the extracts was confirmed by total phenolic and flavonoid content and antioxidant tests. The Ag-NPs were characterised by various analytical techniques including UV-vis spectroscopy, scanning electron microscopy (SEM), energy-dispersive spectrometry (EDS), Fourier transform infrared (FT-IR) spectroscopy, and a dynamic light scattering (DLS) system. The obtained Ag-NPs showed higher cytotoxic activity than the initial extracts against both human cervical cancer cell lines HeLa (ATCC CCL-2) and human melanoma cell lines A375 and SK-MEL-3 by MTT assay. However, the high toxicity to Vero cell culture (ATCC CCL-81) and human fibroblast cell line WS-1 rules out the possibility of their use as anticancer agents. The plant-mediated Ag-NPs were mostly bactericidal against tested strains with MBC/MIC index ≤4. Antifungal bioactivity (C. albicans, C. glabrata, and C. parapsilosis) was not observed for aqueous extracts (MIC > 8000 mg L-1), but Ag-NPs synthesised using both the flowers and leaves of tansy were very potent against Candida spp., with MIC 15.6 and 7.8 µg mL-1, respectively.


Asunto(s)
Antiinfecciosos , Antineoplásicos , Nanopartículas del Metal , Humanos , Plata/farmacología , Plata/química , Espectroscopía Infrarroja por Transformada de Fourier , Nanopartículas del Metal/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Antiinfecciosos/farmacología , Antibacterianos/farmacología , Antibacterianos/química , Antineoplásicos/farmacología , Pruebas de Sensibilidad Microbiana
8.
Molecules ; 27(6)2022 Mar 13.
Artículo en Inglés | MEDLINE | ID: mdl-35335228

RESUMEN

This study focused on the biological evaluation and chemical characterisation of Ficus sur Forssk. (F. sur) (Family: Moraceae). The methanolic and aqueous extracts' phytochemical profile, antioxidant, and enzyme inhibitory properties were investigated. The aqueous stem bark extract yielded the highest phenolic content (115.51 ± 1.60 mg gallic acid equivalent/g extract), while the methanolic leaves extract possessed the highest flavonoid content (27.47 ± 0.28 mg Rutin equivalent/g extract). In total, 118 compounds were identified in the tested extracts. The methanolic stem bark extract exhibited the most potent radical scavenging potential against 2,2-diphenyl-1 picrylhydrazyl and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (475.79 ± 6.83 and 804.31 ± 4.52 mg Trolox equivalent/g extract, respectively) and the highest reducing Cu2+ capacity (937.86 ± 14.44 mg Trolox equivalent/g extract). The methanolic stem bark extract substantially depressed tyrosinase (69.84 ± 0.35 mg kojic acid equivalent/g extract), α-amylase (0.77 ± 0.01 mmol acarbose equivalent/g extract), acetylcholinesterase and butyrylcholinesterase (2.91 ± 0.07 and 6.56 ± 0.34 mg galantamine equivalent/g extract, respectively) enzymes. F. sur extracts were tested for anticancer properties and antiviral activity towards human herpes virus type 1 (HHV-1). Stem bark infusion and methanolic extract showed antineoplastic activity against cervical adenocarcinoma and colon cancer cell lines, whereas leaf methanolic extract exerted moderate antiviral activity towards HHV-1. This investigation yielded important scientific data on F. sur which might be used to generate innovative phytopharmaceuticals.


Asunto(s)
Ficus , Acetilcolinesterasa , Butirilcolinesterasa , Humanos , Fitoquímicos/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología
9.
Molecules ; 27(21)2022 Nov 03.
Artículo en Inglés | MEDLINE | ID: mdl-36364367

RESUMEN

Iphiona mucronata (Family Asteraceae) is widely distributed in the Eastern desert of Egypt. It is a promising plant material for phytochemical analysis and pharmacologic studies, and so far, its specific metabolites and biological activity have not yet been thoroughly investigated. Herein, we report on the detailed phytochemical study using UPLC-Q-TOF-MS approach. This analysis allowed the putative annotation of 48 metabolites belonging to various phytochemical classes, including mostly sesquiterpenes, flavonoids, and phenolic acids. Further, zebrafish embryotoxicity has been carried out, where 100 µg/mL extract incubated for 72 h resulted in a slow touch response of the 10 examined larvae, which might be taken as a sign of a disturbed peripheral nervous system. Results of in vitro testing indicate moderate cytotoxicity towards VERO, FaDu, and HeLa cells with CC50 values between 91.6 and 101.7 µg/mL. However, selective antineoplastic activity in RKO cells with CC50 of 54.5 µg/mL was observed. To the best of our knowledge, this is the first comprehensive profile of I. mucronata secondary metabolites that provides chemical-based evidence for its biological effects. A further investigation should be carried out to precisely define the underlying mechanisms of toxicity.


Asunto(s)
Asteraceae , Pez Cebra , Humanos , Animales , Células HeLa , Extractos Vegetales/farmacología , Fitoquímicos/farmacología , Fitoquímicos/análisis , Cromatografía Líquida de Alta Presión/métodos
10.
Molecules ; 27(15)2022 Jul 22.
Artículo en Inglés | MEDLINE | ID: mdl-35897865

RESUMEN

Spathodea campanulata is an important medicinal plant with traditional uses in the tropical zone. In the current work, we aimed to determine the chemical profiles and biological effects of extracts (methanolic and infusion (water)) from the leaves and stem bark of S. campanulata. The chemical components of the tested extracts were identified using LC-ESI-QTOF-MS. Biological effects were tested in terms of antioxidant (radical scavenging, reducing power, and metal chelating), enzyme inhibitory (cholinesterase, amylase, glucosidase, and tyrosinase), antineoplastic, and antiviral activities. Fifty-seven components were identified in the tested extracts, including iridoids, flavonoids, and phenolic acids as the main constituents. In general, the leaves-MeOH extract was the most active in the antioxidant assays (DPPH, ABTS, CUPRAC, FRAP, metal chelating, and phosphomolybdenum). Antineoplastic effects were tested in normal (VERO cell line) and cancer cell lines (FaDu, HeLa, and RKO). The leaf infusion, as well as the extracts obtained from stem bark, showed antineoplastic activity (CC50 119.03-222.07 µg/mL). Antiviral effects were tested against HHV-1 and CVB3, and the leaf methanolic extract (500 µg/mL) exerted antiviral activity towards HHV-1, inhibiting the viral-induced cytopathic effect and reducing the viral infectious titre by 5.11 log and viral load by 1.45 log. In addition, molecular docking was performed to understand the interactions between selected chemical components and viral targets (HSV-1 DNA polymerase, HSV-1 protease, and HSV-1 thymidine kinase). The results presented suggest that S. campanulata may be a bright spot in moving from natural sources to industrial applications, including novel drugs, cosmeceuticals, and nutraceuticals.


Asunto(s)
Bignoniaceae , Farmacia , Antioxidantes/química , Antioxidantes/farmacología , Antivirales/farmacología , Bignoniaceae/química , Simulación del Acoplamiento Molecular , Extractos Vegetales/química , Extractos Vegetales/farmacología
11.
Molecules ; 27(11)2022 May 27.
Artículo en Inglés | MEDLINE | ID: mdl-35684407

RESUMEN

The composition of the ethanolic extract from the aerial parts of Crocus alatavicus Regel & Semen from southern Kazakhstan spontaneous flora was analyzed together with the determination of its antibacterial, antifungal, antiviral and anticancer activity. The phytochemical profile analysis by high-performance liquid chromatography-electrospray ionization-quadrupole-time of flight-mass spectrometry (HPLC/ESI-QTOF-MS) revealed the presence of multiple kaempferol derivatives. High-performance reverse-phase liquid chromatography combined with a photodiode-array detection (RP-HPLC/PDA) found that kaempferol 3-O-dihexoside and kaempferol 3-O-acyltetrahexoside accounted for 70.5% of the kaempferol derivatives. The minimum inhibitory concentration (MIC) values of the extract for all the tested reference microorganisms were high, reaching 10 mg/mL for yeasts and 20 mg/mL for bacteria. In contrast, antiviral activity was observed at 2 mg/mL, resulting in the inhibition of the HSV-1-induced cytopathic effect and the reduction in virus infectious titer by 1.96 log, as well as the viral load by 0.85 log. Among the tested prostate cancer cell lines, significant cytotoxic activity of the extract was noted only on the LNCaP cell line, with an IC50 value of 1.95 mg/mL. The LNCaP cell line treated with 2 mg/mL of the extract showed a noticeably reduced number of spindle-shaped cells with longer cellular projections, a significant increase in the peak corresponding to the population of apoptotic cells in the sub-G1 phase and a decreased intracellular glutathione (GSH) level, suggesting the prooxidative properties of the extract. The obtained data provide novel information about the flavonoids present in the aerial part of C. alatavicus and suggest its potential application as a source of the compounds active against HSV-1 and metastatic, androgen-sensitive prostate cancer.


Asunto(s)
Crocus , Etanol , Extractos Vegetales , Semillas , Antivirales/farmacología , Cromatografía Líquida de Alta Presión/métodos , Etanol/química , Etanol/farmacología , Humanos , Quempferoles/análisis , Kazajstán , Masculino , Fitoquímicos/análisis , Fitoquímicos/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Neoplasias de la Próstata/tratamiento farmacológico , Semillas/química , Espectrometría de Masa por Ionización de Electrospray/métodos
12.
Int J Mol Sci ; 22(14)2021 Jul 16.
Artículo en Inglés | MEDLINE | ID: mdl-34299238

RESUMEN

This study focused on the biological evaluation and chemical characterization of Geranium pyrenaicum Burm. f. Different solvent extracts (hexane, ethyl acetate, methanol, and water extracts) were prepared. The phytochemical profile, antioxidant, and enzyme inhibitory activity were investigated. Cytotoxicity was assessed using VERO, FaDu, HeLa and RKO cells. The antiviral activity was carried out against HSV-1 (Herpes simplex virus 1) propagated in VERO cell line. The aqueous extract, possessing high phenolic content (170.50 mg gallic acid equivalent/g extract), showed the highest reducing capacity (613.27 and 364.10 mg Trolox equivalent/g extract, for cupric reducing antioxidant capacity and ferric reducing antioxidant power, respectively), radical scavenging potential (469.82 mg Trolox equivalent/g extract, against 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)), metal chelating ability (52.39 mg ethylenediaminetetraacetic acid equivalent/g extract) and total antioxidant capacity (3.15 mmol Trolox equivalent/g extract). Liquid chromatography-electrospray ionization-quadrupole time-of-flight-mass spectrometry (LC-ESI-QTOF-MS/MS) alloved to tentatively identify a total of 56 compounds in the extracts, including ellagitannins, gallic acid and galloyl derivatives amongst others. The ethyl acetate extracts substantially depressed cholinesterase enzymes (4.49 and 12.26 mg galantamine equivalent/g extract against AChE and BChE, respectively) and α-amylase enzyme (1.04 mmol acarbose equivalent/g extract). On the other hand, the methanolic extract inhibited tyrosinase (121.42 mg kojic acid equivalent/g extract) and α-glucosidase (2.39 mmol acarbose equivalent/g extract) activities. The highest selectivity towards all cancer cell lines (SI 4.5-10.8) was observed with aqueous extract with the FaDu cells being the most sensitive (CC50 40.22 µg/mL). It can be concluded that the presence of certain bioactive antiviral molecules may be related to the high anti HSV-1 activity of the methanolic extract. This work has generated vital scientific data on this medicinal plant, which is a prospective candidate for the creation of innovative phyto-pharmaceuticals.


Asunto(s)
Geranium/metabolismo , Extractos Vegetales/química , Animales , Antioxidantes , Antivirales , Línea Celular , Cromatografía Líquida de Alta Presión/métodos , Flavonoides/análisis , Humanos , Fenoles/análisis , Fitoquímicos/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Plantas Medicinales/química , Estudios Prospectivos , Espectrometría de Masa por Ionización de Electrospray/métodos , Espectrometría de Masas en Tándem/métodos
13.
Molecules ; 27(1)2021 Dec 28.
Artículo en Inglés | MEDLINE | ID: mdl-35011384

RESUMEN

Liverwort endophytes could be a source of new biologically active substances, especially when these spore-forming plants are known to produce compounds that are not found in other living organisms. Despite the significant development of plant endophytes research, there are only a few studies describing liverwort endophytic microorganisms and their metabolites. In the presented study, the analysis of the volatile compounds obtained from thallose liverwort species, Marchantia polymorpha L., and its endophytes was carried out. For this purpose, non-polar extracts of plant material and symbiotic microorganisms were obtained. The extracts were analyzed using gas chromatography coupled to mass spectrometry. Compounds with the structure of diketopiperazine in the endophyte extract were identified. Liverwort volatile extract was a rich source of cuparane-, chamigrane-, acorane-, and thujopsane-type sesquiterpenoids. The cytotoxicity of ethyl acetate extracts from endophytic microorganisms was evaluated on a panel of cancer (FaDu, HeLa, and SCC-25) cell lines and normal (VERO), and revealed significant anticancer potential towards hypopharyngeal squamous cell carcinoma and cervical adenocarcinoma.


Asunto(s)
Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Endófitos/química , Marchantia/química , Fitoquímicos/química , Fitoquímicos/farmacología , Animales , Línea Celular , Cromatografía de Gases y Espectrometría de Masas , Humanos , Metabolómica/métodos , Estructura Molecular , Extractos Vegetales/química , Extractos Vegetales/farmacología , Compuestos Orgánicos Volátiles
14.
J Enzyme Inhib Med Chem ; 31(5): 787-95, 2016 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-26212601

RESUMEN

Novel 1-(1-aryl-4,5dihydro-1H-imidazoline)-3-chlorosulfonylourea derivatives 3a-3f were synthesized in the reaction of 1-aryl-4,5-dihydro-1H-imidazol-2-amines with chlorosulfonyl isocyanate. The second series of compounds 4a-4f was prepared from the respective 1-(1-aryl-4,5-dihydro-1H-imidazoline)-3-chlorsulfonylureas 3a-3f and 1,1'-carbonyldiimidazole (CDI). The selected compounds were tested for their activity against Herpes simplex virus and coxsackievirus B3 (CVB3). It was determined that three derivatives, i.e 3d, 4a and 4d are active against Herpes simplex virus (HSV-1). Compounds 3d and 4c are active against CVB3. Their favorable activity can be primarily attributed to their low lipophilicity values. Moreover, the lack of substituent in the phenyl moiety or 4-methoxy substitution can be considered as the most beneficial for the antiviral activity.


Asunto(s)
Antivirales/química , Antivirales/farmacología , Enterovirus Humano B/efectos de los fármacos , Simplexvirus/efectos de los fármacos , Urea/química , Urea/farmacología , Animales , Antivirales/síntesis química , Chlorocebus aethiops , Infecciones por Coxsackievirus/tratamiento farmacológico , Ciclización , Herpes Simple/tratamiento farmacológico , Imidazolinas/síntesis química , Imidazolinas/química , Imidazolinas/farmacología , Modelos Moleculares , Estructura Molecular , Relación Estructura-Actividad , Ácidos Sulfónicos/síntesis química , Ácidos Sulfónicos/química , Ácidos Sulfónicos/farmacología , Urea/síntesis química , Células Vero
15.
J Enzyme Inhib Med Chem ; 31(3): 361-8, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-25798689

RESUMEN

Novel 1-(1,3-disubstituted-imidazolidyn-2-ylidene)-3-ethoxycarbonylmethylurea derivatives (3a-3j) were obtained from appropriate 1-aryl-3-arylsulfonyl-1H-imidazolidine-2-imines (1a-1j) and ethyl isocyanatoacetate (2), which were subjected to condensation. Seven compounds were tested for their antiviral activity against HSV-1 and CVB3 viruses. Among the tested compounds, 3c was found to be active against HSV-1, proving that 4-methoxy substituent as R and 4-methyl substituent as R1 are most beneficial for activity against this virus. Furthermore, 3e and 3g were active against CVB3, which demonstrated that both 4-methyl and 4-chloro substitution is tolerated as R1, whereas 4-chloro and 2-methoxy substituents are best as R. It was also shown that the active compounds are characterized by relatively big surface area, small ovality, and greatest HOMO and LUMO energies in comparison to the rest of the compounds.


Asunto(s)
Antivirales/síntesis química , Antivirales/farmacología , Enterovirus Humano B/efectos de los fármacos , Herpesvirus Humano 1/efectos de los fármacos , Compuestos de Metilurea/farmacología , Antivirales/química , Relación Dosis-Respuesta a Droga , Compuestos de Metilurea/síntesis química , Compuestos de Metilurea/química , Pruebas de Sensibilidad Microbiana , Relación Estructura-Actividad
16.
Molecules ; 20(4): 6254-72, 2015 Apr 09.
Artículo en Inglés | MEDLINE | ID: mdl-25859782

RESUMEN

We have synthesized and examined the antibacterial activity, toxicity and affinity towards bacterial type II topoisomerases of a series of 1,2,4-triazole-ciprofloxacin hybrids. A number of these compounds displayed enhanced activity against Gram-positive and Gram-negative bacteria when compared to ciprofloxacin. The toxic concentrations of the obtained derivatives, evaluated on HEK-293 cells using MTT assay, were much higher than concentrations required to produce antibacterial effect. Finally, the results of enzymatic studies showed that the analyzed compounds demonstrated other preferences as regards primary and secondary molecular targets than ciprofloxacin.


Asunto(s)
Antibacterianos/farmacología , Ciprofloxacina/farmacología , Inhibidores de Topoisomerasa II/farmacología , Triazoles/farmacología , Antibacterianos/síntesis química , Antibacterianos/química , Ciprofloxacina/síntesis química , Ciprofloxacina/química , ADN-Topoisomerasas de Tipo II/efectos de los fármacos , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Células HEK293 , Humanos , Relación Estructura-Actividad , Inhibidores de Topoisomerasa II/síntesis química , Inhibidores de Topoisomerasa II/química , Triazoles/síntesis química , Triazoles/química
17.
J Clin Med ; 13(10)2024 May 18.
Artículo en Inglés | MEDLINE | ID: mdl-38792518

RESUMEN

Background: Three-dimensional (3D) printing is becoming increasingly popular around the world not only in engineering but also in the medical industry. This trend is visible, especially in aortic modeling for both training and treatment purposes. As a result of advancements in 3D technology, patients can be offered personalized treatment of aortic lesions via physician-modified stent grafts (PMSG), which can be tailored to the specific vascular conditions of the patient. The objective of this systematic review was to investigate the utility of 3D printing in PMSG in aortic lesion repair by examining procedure time and complications. Methods: The systematic review has been performed using the PRISMA 2020 Checklist and PRISMA 2020 flow diagram and following the Cochrane Handbook. The systematic review has been registered in the International Prospective Register of Systematic Reviews: CRD42024526950. Results: Five studies with a total number of 172 patients were included in the final review. The mean operation time was 249.95± 70.03 min, and the mean modification time was 65.38 ± 10.59 min. The analysis of the results indicated I2 of 99% and 100% indicating high heterogeneity among studies. The bias assessment indicated the moderate quality of the included research. Conclusions: The noticeable variance in the reviewed studies' results marks the need for larger randomized trials as clinical results of 3D printing in PMSG have great potential for patients with aortic lesions in both elective and urgent procedures.

18.
Antioxidants (Basel) ; 13(6)2024 May 25.
Artículo en Inglés | MEDLINE | ID: mdl-38929082

RESUMEN

The present study was performed to determine the chemical constituents, cytotoxicity, antioxidant and enzyme inhibition activities of the aerial parts of Glaucium acutidentatum Hausskn. and Bornm. (family Papaveraceae). Methanolic and aqueous extracts were prepared by maceration, homogenizer-assisted extraction (HAE) and infusion. Results showed that the highest total phenolic and flavonoids contents were obtained from the methanol extracts obtained by HAE (53.22 ± 0.10 mg GAE/g) and maceration (30.28 ± 0.51 mg RE/g), respectively. The aporphine, beznyltetrahydroisoquinoline, and protopine types of Glaucium alkaloids have been tentatively identified. Among them, glaucine was identified in all extracts. Flavonoids, phenolic acids, coumarins, organic acids and fatty acids were also detected. Methanolic extract obtained using the HAE method displayed the highest anti-DPPH (41.42 ± 0.62 mg TE/g), total antioxidant (1.20 ± 0.17 mmol TE/g), Cu2+ (113.55 ± 6.44 mg TE/g), and Fe3+ (74.52 ± 4.74 mg TE/g) reducing properties. The aqueous extracts obtained by infusion and HAE methods exerted the best anti-ABTS (103.59 ± 1.49 mg TE/g) and chelating (19.81 ± 0.05 mg EDTAE/g) activities, respectively. Methanolic extract from HAE recorded the highest acetylcholinesterase (2.55 ± 0.10 mg GALAE/g) and α-amylase (0.51 ± 0.02 mmol ACAE/g) inhibition activities, while that obtained by maceration showed the best butyrylcholinesterase (3.76 ± 0.31 mg GALAE/g) inhibition activity. Both extracts revealed the best tyrosinase inhibitory activity (25.15 ± 1.00 and 26.79 ± 2.36 mg KAE/g, p ≥ 0.05). G. acutidentatum maceration-derived aqueous extract showed selective anticancer activity against cells originating from human hypopharyngeal carcinoma. In conclusion, these findings indicated that G. acutidentatum is a promising source of alkaloids and phenolic compounds for variable pharmaceutical formulations.

19.
Front Pharmacol ; 15: 1386509, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38769997

RESUMEN

The Stachys L. genus has been widely used in traditional medicine in many countries throughout the world. The study aimed to investigate the chemical composition and bioactivity of the hydroethanolic extract (50% v/v) obtained by ultrasonication from the aerial flowering parts of Stachys sylvatica L. (SSE) collected in Almaty region (Southern Kazakhstan). According to RP-HPLC/PDA analysis the leading metabolites of the SSE belonged to polyphenols: chlorogenic acid and its isomers (2.34 mg/g dry extract) and luteolin derivatives (1.49 mg/g dry extract), while HPLC-ESI-QTOF-MS/MS-based qualitative fingerprinting revealed the presence of 17 metabolites, mainly chlorogenic acid and its isomers, flavonoid glycosides, and verbascoside with its derivatives. GC-MS analysis of the volatile metabolites showed mainly the presence of diterpenoids and fatty acid esters. A reduction in the viability of nematodes Rhabditis sp. was obtained for the SSE concentration of 3.3 mg/mL, while 11.1 mg/mL showed activity comparable to albendazole. The SSE exhibited higher activity against Gram-positive (MIC = 0.5-2 mg/mL) than Gram-negative bacteria and yeast (MIC = 8 mg/mL), exerting bactericidal and fungicidal effects but with no sporicidal activity. The SSE showed some antiviral activity against HCoV-229E replicating in MRC-5 and good protection against the cytopathic effect induced by HHV-1 in VERO. The SSE was moderately cytotoxic towards human cervical adenocarcinoma (H1HeLa) cells (CC50 of 0.127 mg/mL after 72 h). This study provides novel information on the SSE extract composition and its biological activity, especially in the context of the SSE as a promising candidate for further antiparasitic studies.

20.
Pol Przegl Chir ; 96(0): 109-113, 2023 Nov 27.
Artículo en Inglés | MEDLINE | ID: mdl-38348974

RESUMEN

<b><br>Introduction:</b> Chronic venous disease (CVD) is a rising problem in western countries. There are several stages of CVD that can be treated with different ways. One of the methods of treating varicosity, C2 stage of CVD, is still developing endovenous laser ablation (EVLA). This method is popular due to its short operation time, less bleeding, quick recovery and no surgical scars. The compression therapy in form of compression stockings has been widely used as a conservative treatment of early stage CVD and it's also used after EVLA. However there are no strong recommendations towards using compression therapy after this kind of surgery.</br> <b><br>Aim and Method:</b> This paper is aimed to review existing knowledge about compression therapy benefits and its recommended time period after EVLA. Search engines used in review: Pubmed and Cochrane.</br> <b><br>Results:</b> Studies focusing on the compression therapy after EVLA of varicose veins have questioned the prolonged use of compression therapy as it brings no additional benefits and might be difficult for patients to adhere. The existing studies recommended the time period no greater than 1-2 weeks. There are no significant changes in reoccurrence rate and return to normal activities between compression and non-compression group. It is proven that compression therapy significantly reduces the postoperative pain and consumption of analgesics.</br> <b><br>Discussion:</b> Compression therapy seems as a safe option for low pain management. There is a need for further research involving the impact of the compression therapy after EVLA, especially in group of low energy delivered settings as the results of treatment are promising.</br>.


Asunto(s)
Terapia por Láser , Várices , Humanos , Enfermedad Crónica , Terapia por Láser/métodos , Dolor Postoperatorio , Vena Safena/cirugía , Resultado del Tratamiento , Várices/cirugía
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