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1.
J Nat Med ; 78(3): 537-546, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38517624

RESUMEN

A phytochemical investigation of Kaempferia champasakensis rhizomes led to the isolation of a new 3,4-seco-isopimarane diterpene, kaempferiol A (1), and three new isopimarane diterpenes, kaempferiols B-D (2-4), together with six known isopimarane diterpenes (5-10). The structures of 1-4 were elucidated by extensive spectroscopic analyses, including HR-ESI-MS, UV, IR, and 1D and 2D NMR. The absolute configurations of 1, 3, and 4 were determined by ECD calculations, while that of 2 was established using the modified Mosher method. All isolated compounds were tested for cytotoxicity against three human cancer cell lines, lung cancer (A549), cervical cancer (HeLa), and breast cancer (MCF-7). Among them, 6 and 7 showed moderate cytotoxic activities against the three tested cell lines, with IC50 values ranging from 38.04 to 27.77 µM, respectively.


Asunto(s)
Antineoplásicos Fitogénicos , Diterpenos , Zingiberaceae , Humanos , Diterpenos/química , Diterpenos/farmacología , Diterpenos/aislamiento & purificación , Zingiberaceae/química , Vietnam , Estructura Molecular , Antineoplásicos Fitogénicos/farmacología , Antineoplásicos Fitogénicos/química , Línea Celular Tumoral , Rizoma/química , Extractos Vegetales/química , Extractos Vegetales/farmacología
2.
Nutr Neurosci ; 27(3): 262-270, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-36877601

RESUMEN

BACKGROUND: Prevalence of mental health disorders continue to increase worldwide. Over the past decades, suboptimal vitamin D (VD) levels and gut dysbiosis have been associated with neurological dysfunction and psychiatric disorders. METHODS: In this review, we examined the available literature on VD and mental health disorders, particularly depression and anxiety, in both clinical and pre-clinical studies. RESULTS: Our extensive review failed to find a link between VD deficiency, depression, and anxiety-related behavior in preclinical animal models. However, strong evidence suggests that VD supplementation may alleviate symptoms in chronically stressed rodents, with some promising evidence from clinical studies. Further, fecal microbiota transplantations suggest a potential role of gut microbiota in neuropsychiatric disorders, although the underlying mechanisms remain to be fully elucidated. It has been postulated that serotonin, primarily produced by gut bacteria, may be a crucial factor. Hence, whether VD has the ability to impact gut microbiota and modulate serotonin synthesis warrants further investigation. CONCLUSIONS: Taken together, literature has suggested that VD may serve as a key regulator in the gut-brain axis to modulate gut microbiota and alleviate symptoms of depression and anxiety. The inconsistent results of VD supplementation in clinical studies, particularly among VD deficient participants, suggests that current intake recommendations may need to be re-evaluated for individuals at-risk (i.e. prior to diagnosis) of developing depression and/or anxiety.


Asunto(s)
Depresión , Vitamina D , Animales , Humanos , Depresión/microbiología , Vitamina D/uso terapéutico , Serotonina , Trastornos de Ansiedad/tratamiento farmacológico , Ansiedad , Vitaminas
3.
Chem Biodivers ; 20(12): e202301482, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37899310

RESUMEN

A new phenolic derivative, galeomalate A (1), together with five known structurally related compounds (2-6), was isolated from the ethyl acetate extract of Galeola nudifolia collected in Vietnam. The structures were elucidated by various spectroscopic methods, including 1D and 2D NMR, HR-ESI-TOF-MS, and CD data, and chemical conversion of the sugar moiety. All isolated compounds possessed acetylcholinesterase (AChE) inhibitory activities in a dose-dependent manner. Among them, compounds 2 and 3 exhibited the first and second highest inhibitory activity on AChE with IC50 values of 122.13 and 125.49 µM, respectively. Compounds 1 and 4-6 inhibited the AChE activity by mixed modes of action comprising competitive and non-competitive modes, whereas 2 and 3 exerted their inhibitory activities in a competitive manner. Molecular docking analyses suggested that the phenyl-ß-D-glucopyranoside unit of 2 and 3 bound to the active site of AChE for the competitive inhibitory activities, while the mixed inhibitory activity of 4 was due to the two binding patterns in the active-site and the active-site entrance of AChE. Furthermore, the docking studies indicated that 1, 5, and 6 would inhibit AChE in a mixed inhibitory manner by adopting three distinct binding patterns of the additional phenyl-ß-D-glucopyranoside unit at the active-site entrance.


Asunto(s)
Acetilcolinesterasa , Inhibidores de la Colinesterasa , Acetilcolinesterasa/metabolismo , Inhibidores de la Colinesterasa/farmacología , Inhibidores de la Colinesterasa/química , Simulación del Acoplamiento Molecular , Vietnam , Extractos Vegetales/farmacología , Extractos Vegetales/química , Fenoles/farmacología
4.
Environ Monit Assess ; 195(8): 963, 2023 Jul 17.
Artículo en Inglés | MEDLINE | ID: mdl-37458829

RESUMEN

Soil factors, especially metal elements in the soil, play a significant role in forming and accumulating secondary metabolites, which determine the medicinal properties of medicinal herbs. In this study, the concentrations of some metal elements (K, Mn, Fe, Cu, Zn, and Cr) in Cam Mountain and Tinh Bien Town, An Giang Province, Vietnam, were determined using the XRF method. We simultaneously determined the total phenolic and flavonoid content of some medicinal herbs collected from the collected soil sample areas, thereby assessing the influence of these elements on the formation of secondary metabolites in medicinal plants. The results showed that K, Mn, and Cr were mainly concentrated in the topsoil and transition layers; Fe and Cu elements tended to concentrate in the transition layer and the subsoil when surveying the soil profile. K, Mn, Cu, and Cr concentrations were more focused in Tinh Bien area, while Fe and Zn had higher concentrations at Cam Mountain. Additionally, results from evaluating the relationship between the content of the elements in the soil and the content of two active compounds also showed the correlation regression model between Zn and flavonoid expression by level 4 at the 5% significance level. Thus, the nonlinear model is suitable for evaluating the relationship between the content of metal elements in the soil and the active compound in medicinal plants.


Asunto(s)
Metales Pesados , Plantas Medicinales , Contaminantes del Suelo , Suelo , Rayos X , Fluorescencia , Monitoreo del Ambiente , Contaminantes del Suelo/análisis , Metales , Metales Pesados/análisis
5.
Chem Biodivers ; 20(4): e202201096, 2023 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-36891669

RESUMEN

The objective of this study was to evaluate the antioxidant, anti-skin-aging, anti-inflammatory, and anti-acetylcholinesterase activities of the hexane (n-hex), AcOEt, BuOH, MeOH, and aqueous extracts from R. oligophlebia roots. The total phenolic and flavonoid contents (TPC and TFC) were determined using Folin-Ciocalteu and AlCl3 colorimetric assays. The antioxidant capacity was examined by reducing power (RP), ferric reducing antioxidant power (FRAP), ABTS⋅+ , and DPPH⋅+ radical cation assays. All extracts potentially exhibited antioxidant activity with IC50 values ranging from 2.93 to 5.73 µg/mL for ABTS⋅+ and from 5.69 to 7.65 µg/mL for DPPH⋅+ except the n-hex extract. The BuOH, MeOH, and aqueous extract possess promising anti-skin-aging activities, as observed by an attenuation of UV-A toxicity on human keratinocytes. We proposed that these anti-skin-aging properties are possibly due to direct scavenging activity against reactive oxygen species and upregulate cellular antioxidant machinery. Moreover, we found that the antioxidant capacity was well correlated with anti-inflammatory capacity against nitric oxide (NO) production in terms of the n-hex, AcOEt, and BuOH extracts with IC50 values from 23.21 to 47.1 µg/mL. In contrast, these activities were found to be poorly correlated with AchE activity. To the best of our knowledge, this is the first report of the antioxidant, anti-skin-aging, anti-inflammatory, and anti-acetylcholinesterase activities of the extracts of R. oligophlebia roots. These findings indicated that this species could be a potential source of natural antioxidant, anti-aging, and anti-inflammatory agents. Consequently, it may be suggested as a medicinal plant that prevents diseases related to oxidative stress and inflammatory responses.


Asunto(s)
Antiinflamatorios , Inhibidores de la Colinesterasa , Connaraceae , Humanos , Antiinflamatorios/química , Antiinflamatorios/farmacología , Antioxidantes/química , Antioxidantes/farmacología , Connaraceae/química , Flavonoides/química , Flavonoides/farmacología , Extractos Vegetales/farmacología , Plantas Medicinales/química , Inhibidores de la Colinesterasa/química , Inhibidores de la Colinesterasa/farmacología , Fenoles/química , Fenoles/farmacología
6.
Sci Rep ; 13(1): 1545, 2023 01 27.
Artículo en Inglés | MEDLINE | ID: mdl-36707691

RESUMEN

Lung cancer is one of the leading cancers and causes of cancer-related deaths worldwide. Due to its high prevalence and mortality rate, its clinical management remains a significant challenge. Previously, the in vitro anticancer activity of Aspiletrein A, a steroid and a saponin from Aspidistra letreae, against non-small cell lung cancer (NSCLC) cells was reported. However, the anticancer molecular mechanism of other Aspiletreins from A. letreae remains unknown. Using in silico network pharmacology approaches, the targets of Aspiletreins were predicted using the Swiss Target Prediction database. In addition, key mediators in NSCLC were obtained from the Genetic databases. The compound-target interacting networks were constructed using the STRING database and Cytoscape, uncovering potential targets, including STAT3, VEGFA, HSP90AA1, FGF2, and IL2. Gene Ontology and Kyoto Encyclopedia of Genes and Genomes pathway analysis demonstrated that several pathways were highly relevant to cancer pathogenesis. Additionally, molecular docking and molecular dynamic analyses revealed the interaction between key identified targets and Aspiletreins, including hydrogen bonding and Van der Waals interaction. This study provides potential targets of Aspiletreins in NSCLC, and its approach of integrating network pharmacology, bioinformatics, and molecular docking is a powerful tool for investigating the mechanism of new drug targets on a specific disease.


Asunto(s)
Asparagaceae , Carcinoma de Pulmón de Células no Pequeñas , Medicamentos Herbarios Chinos , Neoplasias Pulmonares , Carcinoma de Pulmón de Células no Pequeñas/tratamiento farmacológico , Carcinoma de Pulmón de Células no Pequeñas/genética , Neoplasias Pulmonares/tratamiento farmacológico , Neoplasias Pulmonares/genética , Simulación del Acoplamiento Molecular , Farmacología en Red , Saponinas/farmacología
7.
Front Microbiol ; 13: 886206, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35966651

RESUMEN

Probiotic bacteria are increasingly popular as dietary supplements and have the potential as alternatives to traditional antibiotics. We have recently shown that pretreatment with Lactobacillus spp. Lb21 increases the life span of C. elegans and results in resistance toward pathogenic methicillin-resistant Staphylococcus aureus (MRSA). The Lb21-mediated MRSA resistance is dependent on the DBL-1 ligand of the TGF-ß signaling pathway. However, the underlying changes at the metabolite level are not understood which limits the application of probiotic bacteria as timely alternatives to traditional antibiotics. In this study, we have performed untargeted nuclear magnetic resonance-based metabolic profiling. We report the metabolomes of Lactobacillus spp. Lb21 and control E. coli OP50 bacteria as well as the nematode-host metabolomes after feeding with these diets. We identify 48 metabolites in the bacteria samples and 51 metabolites in the nematode samples and 63 across all samples. Compared to the control diet, the Lactobacilli pretreatment significantly alters the metabolic profile of the worms. Through sparse Partial Least Squares discriminant analyses, we identify the 20 most important metabolites distinguishing probiotics from the regular OP50 food and worms fed the two different bacterial diets, respectively. Among the changed metabolites, we find lower levels of essential amino acids as well as increased levels of the antioxidants, ascorbate, and glutathione. Since the probiotic diet offers significant protection against MRSA, these metabolites could provide novel ways of combatting MRSA infections.

8.
J Nat Med ; 76(3): 621-633, 2022 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-35218459

RESUMEN

This study aims to clarify the bioactive constituents responsible for the anti-dementia effects of Ocimum sanctum Linn. ethanolic extract (OS) using olfactory bulbectomized (OBX) mice, an animal model of dementia. The effects of OS or its extract further fractionated with n-hexane (OS-H), ethyl acetate (OS-E), and n-butanol (OS-B) on the spatial cognitive deficits of OBX mice were elucidated by the modified Y-maze tests. The effects of the major constituents of the most active OS fraction were also elucidated using the reference drug donepezil. The administration of OS and OS-E ameliorated the spatial cognitive deficits caused by OBX, whereas OS-H or OS-B had no effect. Two major constituents, ursolic acid (URO) and oleanolic acid (OLE), and three minor constituents were isolated from OS-E. URO (6 and 12 mg/kg) and OLE (24 mg/kg) attenuated the OBX-induced cognitive deficits. URO (6 mg/kg) and donepezil reversed the OBX-induced down-regulation of vascular endothelial growth factor (VEGF) and choline acetyltransferase expression levels in the hippocampus. URO inhibited the ex vivo activity of acetylcholinesterase with similar efficacy to donepezil. URO inhibited the in vitro activity of acetylcholinesterase (IC50 = 106.5 µM), while the effects of OS, OS-E, and other isolated compounds were negligible. These findings suggest that URO and OLE are responsible for the anti-dementia action of OS extract, whereas URO possesses a more potent anti-dementia effect than its isomer OLE. The effects of URO are, at least in part, mediated by normalizing the function of central cholinergic systems and VEGF protein expression.


Asunto(s)
Ocimum sanctum , Ácido Oleanólico , Acetilcolinesterasa , Animales , Donepezilo , Ratones , Ácido Oleanólico/farmacología , Ácido Oleanólico/uso terapéutico , Bulbo Olfatorio/cirugía , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Triterpenos , Factor A de Crecimiento Endotelial Vascular , Ácido Ursólico
9.
Chem Biodivers ; 19(4): e202100882, 2022 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-35146904

RESUMEN

Four compounds, luteolin (1), 6-γ,γ-dimethylallylquercetin 7-O-ß-D-glucopyranoside (2), 6-γ,γ-dimethylallylkaempferol 7-O-ß-D-glucopyranoside (3), and 6-γ,γ-dimethylallyldihydrokaempferol 7-O-ß-D-glucoside (4), were isolated for the first time from AcOEt extract of the O. integerrima flower. We then evaluated the antioxidant effects of AcOEt, butanol, and MeOH extracts and their effects on H2 O2 against oxidative stress in HaCaT keratinocyte cell lines. Furthermore, 2,2-diphenyl-1-picrylhydrazyl hydrate (DPPH⋅) radical scavenging activities of 1-4 were determined and their mechanisms of action on tyrosinase were predicted by in silico studies. The results revealed that the AcOEt extract and 1-3 exhibited good DPPH⋅ radical scavenging activity. Furthermore, this extract also had a significant protective effect against H2 O2 -induced oxidative stress in HaCaT cells. In silico studies indicated that the activity of 1-3 may be due to tyrosinase inhibition with MM-GBSA free binding energies of -78.9, -70.1, and -71.1 kcal mol-1 , respectively, compared to 4 with an energy -56.9 kcal mol-1 .


Asunto(s)
Antioxidantes , Ochnaceae , Antioxidantes/química , Antioxidantes/farmacología , Flores , Queratinocitos , Monofenol Monooxigenasa , Extractos Vegetales/química , Extractos Vegetales/farmacología
10.
Artículo en Inglés | MEDLINE | ID: mdl-35085064

RESUMEN

Fourteen strains of Streptomyces isolated from scab lesions on potato are described as members of a novel species based on genetic distance, morphological observation and biochemical analyses. Morphological and biochemical characteristics of these strains are distinct from other described phytopathogenic species. Strain NE06-02DT has white aerial mycelium and grey, cylindrical, smooth spores on rectus-flexibilis spore chains. Members of this species group can utilize most of the International Streptomyces Project sugars, utilize melibiose and trehalose, produce melanin, grow on 6-7 % NaCl and pH 5-5.5 media, and are susceptible to oleandomycin (100 µg ml-1), streptomycin (20 µg ml-1) and penicillin G (30 µg ml-1). Though the 16S rRNA gene sequences from several members of this novel species are identical to the Streptomyces bottropensis 16S rRNA gene sequence, whole-genome average nucleotide identity and multi-locus sequence analysis confirm that the strains are members of a novel species. Strains belonging to this novel species have been isolated from the United States, Egypt and China with the earliest known members being isolated in 1961 from common scab lesions of potato in both California, USA, and Maine, USA. The name Streptomyces caniscabiei sp. nov. is proposed for strain NE06-02DT (=DSM111602T=ATCC TSD-236T) and the other members of this novel species group.


Asunto(s)
Filogenia , Enfermedades de las Plantas/microbiología , Solanum tuberosum , Streptomyces , Técnicas de Tipificación Bacteriana , Composición de Base , ADN Bacteriano/genética , Ácidos Grasos/química , ARN Ribosómico 16S/genética , Análisis de Secuencia de ADN , Solanum tuberosum/microbiología , Streptomyces/clasificación , Streptomyces/aislamiento & purificación
11.
Phytochemistry ; 196: 113109, 2022 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-35091214

RESUMEN

Kaempferia marginata rhizomes are used as an herb in food and as traditional medicine for the treatment of inflammatory-related diseases in Asian countries. In contrast to the previously reported phytochemical investigation of Thai and Chinese K. marginata rhizomes, which demonstrated the presence of sandaracopimaradiene and ent-sandaracopimaradiene, our first investigation of Vietnamese K. marginata rhizomes led to the isolation of eight undescribed pimarane diterpenoids, marginols A‒H, along with 18 known pimarane diterpenoids. The structures of these compounds were elucidated by spectroscopic techniques, including 1D and 2D NMR, HRESIMS, and CD spectroscopy and/or by comparisons of their NMR data with previously reported data. Furthermore, evaluations of the NO production inhibitory activity against LPS-stimulated RAW264.7 cells revealed that the undescribed compounds, marginols B and D‒G, and the known compounds, sandaracopimaradien-6ß,9α-diol-1-one and 6-acetoxysandaracopimardien-9-ol-1-one, showed potent activities. These results provide insights into the chemodiversity of Vietnamese K. marginata rhizomes as well as their traditional usage from the viewpoint of their chemical constituents.


Asunto(s)
Diterpenos , Zingiberaceae , Abietanos/química , Abietanos/farmacología , Diterpenos/química , Estructura Molecular , Rizoma/química , Tailandia , Zingiberaceae/química
12.
Planta Med ; 88(11): 913-920, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-34474490

RESUMEN

Three new flavanols, (2R,3S)-7-methoxy-flavan-3-ol (1: ), (2R,3S)-7-hydroxy-flavan-3-ol (2: ), and (2R,3S)-2'-hydroxy-7-methoxy-flavan-3-ol (3: ), together with two known flavans (4: and 5: ), were isolated from the chloroform extract of Crinum asiaticum. Their structures were elucidated by various spectroscopic methods, including 1D and 2D NMR, HR-ESI-MS, and CD data. The isolated compounds 1: and 3: -5: showed inhibitory activity toward LPS-induced nitric oxide (NO) production. Further investigation of the NF-κB pathway mechanisms indicated that 1: and 3: -5: inhibited the LPS-induced IL-6 production and p65 subunit phosphorylation of NF-κB in RAW264.7 cells, with an effective dose of 10 µM.


Asunto(s)
Crinum , Flavonoides/química , FN-kappa B , Animales , Crinum/metabolismo , Lipopolisacáridos/farmacología , Ratones , FN-kappa B/metabolismo , Óxido Nítrico/metabolismo , Óxido Nítrico Sintasa de Tipo II/metabolismo , Polifenoles , Células RAW 264.7 , Transducción de Señal
13.
Molecules ; 26(17)2021 Sep 03.
Artículo en Inglés | MEDLINE | ID: mdl-34500805

RESUMEN

Panax vietnamensis, or Vietnamese ginseng (VG), an endemic Panax species in Vietnam, possesses a unique saponin profile and interesting biological activities. This plant is presently in danger of extinction due to over-exploitation, resulting in many preservation efforts towards the geographical acclimatization of VG. Yet, no information on the saponin content of the acclimatized VG, an important quality indicator, is available. Here, we analyzed the saponin content in the underground parts of two- to five-year-old VG plants acclimatized to Lam Dong province. Nine characteristic saponins, including notoginsenoside-R1, ginsenoside-Rg1, -Rb1, -Rd, majonoside-R1, -R2 vina-ginsenoside-R2, -R11, and pseudoginsenoside-RT4, were simultaneously determined by HPLC coupled with UV and with a charged aerosol detector (CAD). Analyzing the results illustrated that the detection of characteristic ocotillol-type saponins in VG by CAD presented a superior capacity compared with that of UV, thus implying a preferential choice of CAD for the analysis of VG. The quantitative results indicating the saponin content in the underground parts of VG showed an increasing tendency from two to five years old, with the root and the rhizome exhibiting different saponin accumulation patterns. This is the first study that reveals the preliminary success of VG acclimatization and thereby encourages the continuing efforts to develop this valuable saponin-rich plant.


Asunto(s)
Panax/química , Saponinas/análisis , Cromatografía Líquida de Alta Presión , Rayos Ultravioleta , Vietnam
14.
Artículo en Inglés | MEDLINE | ID: mdl-34306149

RESUMEN

This study aimed to clarify the antidementia effects of ethanolic extract of Ocimum sanctum Linn. (OS) and its underlying mechanisms using olfactory bulbectomized (OBX) mice. OBX mice were treated daily with OS or a reference drug, donepezil (DNP). Spatial and nonspatial working memory performance was measured using a modified Y maze test and a novel object recognition test, respectively. Brain tissues of the animals were subjected to histochemical and neurochemical analysis. OS treatment attenuated OBX-induced impairment of spatial and nonspatial working memories. OBX induced degeneration of septal cholinergic neurons, enlargement of the lateral ventricles, and suppression of hippocampal neurogenesis. OS and DNP treatment also depressed these histological damages. OS administration reduced ex vivo activity of acetylcholinesterase in the brain. OBX diminished the expression levels of genes coding vascular endothelial growth factor (VEGF) and VEGF receptor type 2 (VEGFR2). Treatment with OS and DNP reversed OBX-induced decrease in VEGF gene and protein expression levels without affecting the expression of the VEGFR2 gene. These results demonstrate that the administration of OS can lessen the cognitive deficits and neurohistological damages of OBX and that these actions are, at least in part, mediated by the enhancement of central cholinergic systems and VEGF expression.

15.
Int J Antimicrob Agents ; 56(4): 106085, 2020 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-32659466

RESUMEN

First-generation oral cephalosporins (cephalexin and cefadroxil) have traditionally been considered second-line treatment options for uncomplicated lower urinary tract infections (uLUTIs).  However, in the current age of "bad bugs, few drugs", where there are increasingly limited oral options against resistant Enterobacteriaceae, there is an urgent need to rethink how best to utilize the available antibiotic armamentarium.  This review examines the historical clinical trials and experimental studies of cephalexin and cefadroxil, particularly through the modern lens of pharmacokinetics/pharmacodynamics (PK/PD), to better appreciate the efficacy of these drugs in uLUTIs.  Furthermore, newer cefazolin-cephalexin surrogate testing, as recommended by the Clinical and Laboratory Standards Institute (CLSI) and the United States Committee on Antimicrobial Susceptibility Testing (USCAST), has recategorized cephalexin in many instances from resistant to susceptible.  We conclude that cephalexin and cefadroxil have very good early bacteriological and clinical cures in uLUTIs due to non-extended-spectrum beta-lactamase-producing (ESBL) Enterobacteriaceae comparable to many traditionally first-line agents.  Cephalexin can be conveniently administered as 500 mg twice or thrice daily, similar to cefadroxil (500 mg twice daily); therefore, either agent may be used as a fluoroquinolone-sparing alternative. Cephalexin may be the more practical choice for many clinicians because reliable antimicrobial susceptibility test interpretative criteria (STIC) are provided by CLSI, USCAST, and the European Committee on Antimicrobial Susceptibility Testing (EUCAST), whereas direct cefadroxil STIC is offered only by EUCAST.


Asunto(s)
Antibacterianos/farmacocinética , Antibacterianos/uso terapéutico , Cefadroxilo/uso terapéutico , Cefalexina/uso terapéutico , Infecciones Urinarias/tratamiento farmacológico , Adolescente , Adulto , Anciano , Anciano de 80 o más Años , Cefadroxilo/farmacocinética , Cefalexina/farmacocinética , Niño , Farmacorresistencia Bacteriana Múltiple/fisiología , Enterobacteriaceae/efectos de los fármacos , Enterobacteriaceae/metabolismo , Femenino , Humanos , Masculino , Pruebas de Sensibilidad Microbiana , Persona de Mediana Edad , Adulto Joven , beta-Lactamasas/metabolismo
16.
Molecules ; 25(14)2020 Jul 21.
Artículo en Inglés | MEDLINE | ID: mdl-32708204

RESUMEN

Cassaine diterpenoids amides from the stem bark of Vietnamese Erythrophleum fordii Oliver were screened for their cytotoxic activity against human cancer cells. The cell proliferation assay results showed that, among the active compounds, 3ß-acetyl-nor-erythrophlamide (3AEP) exhibited the most potential cytotoxicity against human leukemia HL-60 and KG cells with IC50 values of 12.0 ± 1.2 and 18.1 ± 2.7 µM, respectively. Treatment of 3AEP resulted in the apoptosis of HL-60 cells via the activation of caspase 3, and poly (ADP-ribose) polymerase (PARP). Molecular docking in silico results showed that the 3AEP can bind to both the procaspase-3 allosteric site and the PARP-1 active site, with binding energies of -7.51 and -9.63 kcal/mol respectively. These results indicated that the stem bark of Vietnamese E. fordii and its cassaine diterpenoid amides may be useful in the apoptosis induction of human leukemia cancer cells.


Asunto(s)
Abietanos/química , Alcaloides/química , Amidas/química , Antineoplásicos Fitogénicos/química , Diterpenos/química , Fabaceae/química , Leucemia/tratamiento farmacológico , Corteza de la Planta/química , Extractos Vegetales/química , Sitio Alostérico , Amidas/farmacología , Antineoplásicos Fitogénicos/farmacología , Apoptosis/efectos de los fármacos , Caspasa 3/química , Caspasa 3/metabolismo , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Simulación del Acoplamiento Molecular , Extractos Vegetales/farmacología , Poli(ADP-Ribosa) Polimerasa-1/química , Poli(ADP-Ribosa) Polimerasa-1/metabolismo , Unión Proteica
17.
Diagn Microbiol Infect Dis ; 97(3): 115053, 2020 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-32349909

RESUMEN

Based on antimicrobial susceptibility test interpretive breakpoint criteria from Clinical and Laboratory Standards Institute and United States Committee on Antimicrobial Susceptibility Testing, cefazolin uncomplicated urinary tract infection (uUTI) surrogate breakpoints do not accurately predict cefadroxil or cephradine susceptibility when testing indicated Enterobacteriaceae species isolates. Hence, these two orally-administered cephalosporins (OC) are not equivalent spectrum substitutes for cephalexin or six other related OC agents for contemporary uUTI therapy.


Asunto(s)
Cefadroxilo/uso terapéutico , Cefazolina/uso terapéutico , Pruebas de Sensibilidad Microbiana/normas , Infecciones Urinarias/tratamiento farmacológico , Antibacterianos/farmacología , Antibacterianos/uso terapéutico , Cefadroxilo/farmacología , Cefazolina/farmacología , Cefalosporinas/farmacología , Cefalosporinas/uso terapéutico , Enterobacteriaceae/efectos de los fármacos , Enterobacteriaceae/aislamiento & purificación , Humanos , Guías de Práctica Clínica como Asunto , Infecciones Urinarias/microbiología
18.
J Nat Med ; 74(3): 591-598, 2020 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-32200514

RESUMEN

Three new steroidal saponins, aspiletreins A-C (1-3), together with 2H-chromen-2-one (4), and α-tocopherol (5), were isolated from whole Aspidistra letreae plants collected in Vietnam. Their structures were elucidated by a combination of spectroscopic analyses, including 1D- and 2D-NMR, IR, and HRESIMS, and by comparison with the reported data in the literature. Compounds 1-3 exhibited moderate cytotoxicities against the LU-1, HeLa, MDA-MB-231, HepG2, and MKN-7 human cancer cell lines, with IC50 values ranging from 7.69 ± 0.40 to 20.46 ± 3.11 µM.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Asparagaceae/química , Proliferación Celular/efectos de los fármacos , Extractos Vegetales/farmacología , Saponinas/farmacología , Antineoplásicos Fitogénicos/química , Línea Celular Tumoral , Células HeLa , Células Hep G2 , Humanos , Estructura Molecular , Neoplasias/tratamiento farmacológico , Extractos Vegetales/química , Saponinas/química , Vietnam
19.
Chem Biodivers ; 17(5): e2000037, 2020 May.
Artículo en Inglés | MEDLINE | ID: mdl-32163220

RESUMEN

The ocotillol (OCT)-type saponins have been known as a tetracyclic triterpenoid, possessing five- or six-membered epoxy ring in the side chain. Interestingly, this type saponin was mostly found in Panax vietnamensis Ha et Grushv., Araliaceae (VG), hence making VG unique from the other Panax spp. Five OCT-type saponins, majonoside R2, vina-ginsenoside R2, majonoside R1, pseudoginsenoside RT4, vina-ginsenoside R11, together with three protopanaxadiol (PPD)-type saponins and four protopanaxatriol (PPT)-type saponins from VG were evaluated for their antimelanogenic activity. All of isolates were found to be active. More importantly, the five OCT-type saponins inhibited melanin production in B16-F10 mouse melanoma cells, without showing any cytotoxicity. Besides ginsenoside Rd and ginsenoside Rg3 in PPD and notoginsenoside R1 in PPT-type saponins, majonoside R2 was the most potent melanogenesis inhibitory activity in OCT-type saponins. In this article, we highlighted antimelanogenic activity of OCT-type saponins and potential structure-activity relationship (SAR) of ginsenosides. Our results suggested that OCT-type saponins could be used as a depigmentation agent.


Asunto(s)
Antineoplásicos Inmunológicos/farmacología , Ginsenósidos/farmacología , Melanoma/tratamiento farmacológico , Panax/química , Saponinas/farmacología , Animales , Antineoplásicos Inmunológicos/química , Antineoplásicos Inmunológicos/aislamiento & purificación , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Ginsenósidos/química , Ginsenósidos/aislamiento & purificación , Melaninas/antagonistas & inhibidores , Melaninas/metabolismo , Melanoma/metabolismo , Melanoma/patología , Ratones , Conformación Molecular , Plantas Medicinales , Saponinas/química , Saponinas/aislamiento & purificación , Relación Estructura-Actividad , Células Tumorales Cultivadas
20.
J Nat Med ; 72(1): 298-303, 2018 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-28939966

RESUMEN

Sesquiterpenoid quinones with remarkable properties, such as anti-inflammatory, antibacterial, antiviral, antitumor, antiangiogenic, and differentiation-inducing activities, have reportedly been isolated from the marine sponge genera Dysidea, Spongia, and Dactylospongia. In our continuing search for bioactive compounds from marine sponges, three new sesquiterpenoid quinones, langcoquinones D-F (1-3), were isolated from the ethyl acetate extract of Spongia sp. collected from Vietnam. Their chemical structures were elucidated on the basis of extensive spectroscopic analyses. The newly isolated compounds 1-3 were assessed for their antibacterial activities against Gram-positive bacteria, Bacillus subtilis and Staphylococcus aureus, and Gram-negative bacteria, Klebsiella pneumoniae and Escherichia coli, as well as their cytotoxic activities against three human cancer cell lines (A549, lung cancer; MCF7, breast cancer; HeLa, cervical cancer) and a human normal cell line (WI-38 fibroblast). All compounds were inactive against the Gram-negative bacteria. Furthermore, langcoquinones E (2) and F (3) lacked antibacterial activities against the Gram-positive bacteria and cytotoxic activities against the tested cell lines. However, langcoquinone D (1) exhibited good antibacterial activities against Bacillus subtilis and Staphylococcus aureus, with MIC values of 12.5 and 25.0 µM, respectively. Furthermore, 1 exhibited significant cytotoxic activities against three human cancer cell lines (A549, lung cancer; MCF7, breast cancer; HeLa, cervical cancer) and a human normal cell line (WI-38 fibroblast).


Asunto(s)
Antibacterianos/química , Antineoplásicos/química , Dysidea/química , Sesquiterpenos/química , Células A549 , Animales , Antibacterianos/aislamiento & purificación , Antibacterianos/farmacología , Antineoplásicos/aislamiento & purificación , Antineoplásicos/farmacología , Bacillus subtilis/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Escherichia coli/efectos de los fármacos , Fluorouracilo/farmacología , Células HeLa , Humanos , Klebsiella pneumoniae/efectos de los fármacos , Células MCF-7 , Pruebas de Sensibilidad Microbiana , Quinonas/química , Quinonas/aislamiento & purificación , Quinonas/farmacología , Sesquiterpenos/aislamiento & purificación , Sesquiterpenos/farmacología , Staphylococcus aureus/efectos de los fármacos , Vietnam
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