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1.
Cureus ; 15(9): e44574, 2023 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-37790044

RESUMEN

Ganoderma lucidum is traditionally used to prevent and treat some diseases such as liver disorders, hypertension, insomnia, diabetes, and cancer. G. lucidum spore extracts are also reported to share similar bioactivities as extracts from its other parts. However, there is no systematic review that elucidates its pharmacological effect. Our aim is to comprehensively summarise current evidence of G. lucidum spore extracts to clarify its benefits to be applied in further studies. We searched five primary databases: PubMed, Virtual Health Library (VHL), Global Health Library (GHL), System for Information on Grey Literature in Europe (SIGLE), and Google Scholar on September 13, 2021. Articles were selected according to inclusion and exclusion criteria. A manual search was applied to find more relevant articles. Ninety studies that reported the pharmacological effects and/or safety of G. lucidum spores were included in this review. The review found that G. lucidum spore extracts showed quite similar effects as other parts of this medicinal plant including anti-tumor, anti-inflammatory, antioxidant effects, and immunomodulation. G. lucidum sporoderm-broken extract demonstrated higher efficiency than unbroken spore extract. G. lucidum extracts also showed their effects on some genes responsible for the body's metabolism, which implied the benefits in metabolic diseases. The safety of G. lucidum should be investigated in depth as high doses of the extract could increase levels of cancer antigen (CA)72-4, despite no harmful effect shown on body organs. Generally, there is a lot of potential in the studies of compounds with pharmacological effects and new treatments. Sporoderm breaking technique could contribute to the production of extracts with more effective prevention and treatment of diseases. High doses of G. lucidum spore extract should be used with caution as there was a concern about the increase in CA.

2.
Pharmaceuticals (Basel) ; 16(10)2023 Oct 16.
Artículo en Inglés | MEDLINE | ID: mdl-37895947

RESUMEN

Eclipta prostrata L. (EPL), a medicinal plant, is widely utilized in the central highlands of Vietnam. This study aims to assess the chemical profile and potential medical effects of an EPL extract rich in flavonoids. A total of 36 secondary metabolites were identified from the EPL extract through GC-MS and UHPLC-UV analysis. Among them, 15 volatile compounds and several phenolic and flavonoid chemicals, including salicylic acid, epicatechin gallate, isovitexin, and apigetrin, were reported in EPL extract for the first time. This herbal extract demonstrated moderate inhibition against α-amylase and α-glucosidase, and high anti-oxidant and anti-acetylcholinesterase activities (IC50 = 76.8 ± 0.8 µg/mL). These promising attributes can be likely attributed to the high levels of major compounds, including wedelolactone (1), chlorogenic acid (3), epicatechin gallate (6), salicylic acid (8), isovitexin (9), apigetrin (11), and myricetin (12). These findings align with the traditional use of EPL for enhancing memory and cognitive function, as well as its potential benefits in diabetes management. The results of the molecular docking study reveal that the major identified compounds (1, 6, 9, and 11) showed a more effective acetylcholinesterase inhibitory effect than berberine chloride, with good binding energy (DS values, -12.3 to -14.3 kcal/mol) and acceptable values of RMSD (1.02-1.67 Å). Additionally, almost all the identified major compounds exhibited good ADMET properties within the required limits.

3.
J Infect Dev Ctries ; 17(9): 1213-1220, 2023 09 30.
Artículo en Inglés | MEDLINE | ID: mdl-37824353

RESUMEN

INTRODUCTION: Evidence on post-COVID-19 conditions is emerging. This study aims to assess post-COVID conditions and related factors in COVID-19 patients in Central Vietnam. METHODOLOGY: A descriptive cross-sectional study was performed on people who have recovered from COVID-19 at least 2 weeks prior to the online survey. Participants were interviewed face-to-face after 6 and 9 months from the first survey. RESULTS: 53 patients (21.2%) were confirmed to have persistent symptoms, of which, 100% and 94.3% reported prolonged fatigue and full-body weakness respectively. Loss of appetite was reported by 90.6%, while persistent cough, insomnia, and trouble sleeping were reported by 86.3% of patients. Headaches and dyspnea were reported by 69.5% and 56.8% respectively, while other symptoms had lower rates. The prevalence of post-COVID condition showed a statistically significant relationship with the time of infection, duration of illness, treatment place, use of herbal medicine, adherence to the 5K message from Vietnam's Ministry of Health, and daily saltwater mouthwash (p < 0.05). However, the use of medicine and supplements was not related to the post-COVID condition (p > 0.05). After 6 months, 125 participants were interviewed face-to-face, and only 15 people (12.0%) reported having post-COVID symptoms, mainly prolonged fatigue (33.3%) and persistent cough (26.7%). After 9 months, these 15 patients no longer had symptoms related to the post- COVID-19 condition. CONCLUSIONS: The post-COVID condition can persist for several weeks or months, but will mostly be in remission after 6 months, and completely resolve after 9 months from the onset of the infection.


Asunto(s)
COVID-19 , Humanos , COVID-19/epidemiología , Tos/epidemiología , Estudios Transversales , Vietnam/epidemiología , Síndrome Post Agudo de COVID-19 , Fatiga/epidemiología
4.
J Tradit Chin Med ; 43(4): 795-800, 2023 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-37454265

RESUMEN

OBJECTIVE: To evaluate the efficacy of bee venom acupuncture in humeroscapularis (PHS) patients. METHODS: One hundred and twenty patients diagnosed with PHS were assigned into four groups: BV1 (0.01 mg/kg), BV2 (0.005 mg/kg), BV3 (0.0025 mg/kg), and control group (vitamin B1 plus novocain 3% injection) with 15 d of treatment. The outcomes of the study including visual analogue scale (VAS) score and ß-endorphin, inflammatory cytokines including interleukin-10 (IL-10), IL-1ß and tumor necrosis factor α (TNF-α) and shoulder function score were assessed at baseline, after 10 and 15 d of treatment. RESULTS: All four groups reported statistically significant improvement in VAS score, motion range, and shoulder function score ( < 0.01), only the BV3 group showed significant increase of anti-inflammatory (IL-10) and decrease of pro-inflammatory (IL-1ß, TNF-α) cytokines after treatment ( < 0.05). The BV3 group presented a significant difference between all outcomes compared to the control and other groups. CONCLUSION: BV3 groups showed better recovery including reduced pain, improved motor function and normalized inflammatory cytokines than current therapy used in Vietnam and other groups.


Asunto(s)
Terapia por Acupuntura , Venenos de Abeja , Periartritis , Humanos , Periartritis/terapia , Interleucina-10 , Factor de Necrosis Tumoral alfa , Venenos de Abeja/uso terapéutico , Citocinas
5.
J Tradit Complement Med ; 13(4): 408-416, 2023 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-37396160

RESUMEN

Background and aims: Brown algae (Dictyopteris polypodioides) extract (DP) presented high inhibitory potential against α-amylase. The present study aims to isolate, purify and evaluate the antihyperglycemic and anti-type 2 diabetic activities of marine hydroquinone from DP. Methods: Marine hydroquinones were isolated using silica gel, HPLC, and NMR spectroscopy was used to identify compound 1 and compound 2 as zonarol and isozonarol, respectively. The anti-hyperglycemic and anti-type 2 diabetic activities of zonarol were investigated by in vitro assay (α-amylase, α-glucosidase), Lineweaver-Burk plot and Type 2 diabetes mellitus model (T2DM) mice induced by streptozotocin (STZ). Result: Zonarol had the highest content and the strongest inhibitory activity against α-glucosidase (IC50 value of 6.03 mg L-1) and α-amylase (IC50 value of 19.29 mg L-1) in a competitive inhibition and mix-type manner, respectively. The maltose and starch loading tests revealed that zonarol significantly reduced postprandial glycemia after 30 min loading (9.12 and 8.12 mg/dL, respectively), compared to normal (11.37 and 12.37 mg/dL, respectively). Zonarol exhibited pancreatic islet cell rejuvenation, as evidenced by increased pancreatic islet mass, and hence helps in the restoration of insulin levels and therefore improves the glucose metabolism in STZ-induced diabetic mice. Zonarol treatment in T2DM elevated abundant levels of main SCFAs (propionate, butyrate, and valeric acid), which are closely related to glucose metabolism homeostasis. Conclusion: Our finding indicates that zonarol could be used as a food supplement to treat hyperglycemia and diabetes.

6.
J Tradit Chin Med ; 43(2): 352-358, 2023 04.
Artículo en Inglés | MEDLINE | ID: mdl-36994524

RESUMEN

OBJECTIVE: To evaluate the effectiveness of cycling in combination with electroacupuncture in treatment of post-stroke hemiplegia patients at National Hospital of Acupuncture, Vietnam. METHODS: The study was designed as a single-centre, outcome-assessor-blinded parallel randomised controlled trial with 120 post-stroke hemiplegia patients randomly assigned into two groups: electroacupuncture plus cycling (CT group) and electroacupuncture (AT group). Patients were assessed before and after the treatment (using muscle grading, modified Rankin, Barthel, Orgorozo scores and electromyography). Statistical Man-Whitney U test, and Fisher's exact tests were used to compare between CT and AT groups. RESULTS: The results reported statistically significant improvement in motor function in patients suffering from hemiplegia following ischemic stroke in both CT and AT groups. Patients in CT group experienced a greater improvement compared to those in AT group including better muscle contraction (increased frequency and amplitude of electromyography and increased muscle grading scale); increased recovery (Orgogozo scale), increased independency (Barthel scale) and decreased disability (Modified Rankin scale) (< 0.01). CONCLUSIONS: Combination with cycling training significantly improves the recovery of post-stroke patients treated with electroacupuncture.


Asunto(s)
Terapia por Acupuntura , Electroacupuntura , Accidente Cerebrovascular , Humanos , Electroacupuntura/métodos , Hemiplejía/etiología , Hemiplejía/terapia , Accidente Cerebrovascular/complicaciones , Accidente Cerebrovascular/terapia , Terapia por Acupuntura/métodos , Terapia Combinada , Resultado del Tratamiento
7.
J Nat Med ; 77(2): 403-411, 2023 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-36746835

RESUMEN

In the continuing discovery and structure elucidation of natural xanthone dimers, which are still rarely reported in absolute configuration, three new xanthone dimers, eumitrins I-K (1-3) were isolated from the lichen Usnea baileyi, a rich source of natural xanthone dimers. Their structures were elucidated unambiguously by spectroscopic analyses, including high-resolution electrospray ionization mass spectrometry (HRESIMS), 1D and 2D nuclear magnetic resonance spectroscopy (1D and 2D NMR). The absolute configuration of all three compounds was established through DP4 probability and ECD calculation. All compounds revealed weak activity for their enzymatic inhibition against α-glucosidase and tyrosinase, as well as antibacterial activity.


Asunto(s)
Líquenes , Xantonas , Estructura Molecular , Xantonas/química
8.
Nat Prod Res ; 37(9): 1480-1490, 2023 May.
Artículo en Inglés | MEDLINE | ID: mdl-34984944

RESUMEN

The lichen Usnea baileyi is a fruticose lichen belonging to the Usnea genus. It is well known as a rich source of natural xanthone dimers and possesses various bioactivities. Nevertheless, the chemical investigation on this type of lichen is still rare as most of researches reported its components without structural elucidation. Herein, in the continuous study on this type of lichen, we further isolate xanthone dimers from the dichloromethane extract and explore three new xanthone dimers, eumitrins F - H (1 - 3). Their structures were elucidated unambiguously by spectroscopic analyses, including high resolution electrospray ionisation mass spectrometry (HRESIMS), 1 D and 2 D nuclear magnetic resonance spectroscopy (1 D and 2 D NMR), and DP4 probability. All compounds were evaluated for their enzyme inhibition against α-glucosidase, tyrosinase, and antibacterial activity. They revealed moderate antimicrobial and weak tyrosinase inhibition. For α-glucosidase inhibition, compound 3 displayed the most significant inhibitory against α-glucosidase possessing an IC50 value of 64.2 µM.


Asunto(s)
Líquenes , Usnea , Xantonas , alfa-Glucosidasas , Monofenol Monooxigenasa , Usnea/química , Xantonas/química , Hidrógeno/química , Flúor/química
9.
Environ Monit Assess ; 194(Suppl 2): 770, 2022 Oct 18.
Artículo en Inglés | MEDLINE | ID: mdl-36255542

RESUMEN

The impact of high siltation and accumulation of organic and waste material in the intertidal of the dammed Ba Lai River in Vietnam as part of the Mekong estuarine system was investigated by means of marine free-living nematodes. Nutrients content (nitrate, ammonium, total phosphorus, total nitrogen), total suspended solids, total organic carbon, coliform, bacteria E. coli, pH, dissolved oxygen, total dissolved solids, methane and hydrogen sulfide concentration, and the nematode communities were characterized in sediment at selected stations along the river above and below the dam. Our results found elevated methane concentrations at the upstream side of the dam while hydrogen sulfide concentrations found to be highest in the downstream side of the dam. Furthermore, methane and hydrogen sulfide concentrations were correlated to nematode community characteristics such as trophic composition densities and genera composition. There was a clear difference between the communities above and below the dam. The discontinuous nematode community distribution indicated that the Ba Lai River is impacted by dam construction. Potentially the high deposition and eutrophication could turn the area into a methane-rich area related to predicted impact on nematodes.


Asunto(s)
Compuestos de Amonio , Sulfuro de Hidrógeno , Nematodos , Contaminantes Químicos del Agua , Animales , Estuarios , Monitoreo del Ambiente , Contaminantes Químicos del Agua/análisis , Nitratos , Vietnam , Escherichia coli , Fósforo/análisis , Nitrógeno/análisis , Carbono , Metano , Oxígeno , Sedimentos Geológicos/química
10.
World J Microbiol Biotechnol ; 38(7): 112, 2022 May 16.
Artículo en Inglés | MEDLINE | ID: mdl-35570219

RESUMEN

Eriodictyol (ED) is a flavonoid in the flavanones subclass. It is abundantly present in a wide range of medicinal plants, citrus fruits, and vegetables. In addition, ED owns numerous importantly medicinal bioactivities such as inhibition of proliferation, metastasis and induction of apoptosis in glioma cells or inhibition of glioblastoma migration, and invasion. This study described the heterologous production of ED by E. coli based co-culture engineering system from the simple carbon substrate D-glucose. Two E. coli strains were engineered and functioned as constitutive components of biological system. Specifically, the first strain (upstream module) contained genes for synthesis of p-coumaric acid (pCA) from D-glucose. And, the second strain (downstream module) consisted of genes for the synthesis of ED from pCA. The highest yield in ED production was achieved 51.5 ± 0.4 mg/L using stepwise optimal culture conditions, while monoculture was achieved 21.3 ± 0.2 mg/L only. In conclusion, co-culture was the most efficient alternative approach for the synthesis of ED and other natural products.


Asunto(s)
Escherichia coli , Flavanonas , Técnicas de Cocultivo , Escherichia coli/genética , Flavanonas/farmacología , Glucosa , Ingeniería Metabólica
11.
Chemosphere ; 288(Pt 2): 132577, 2022 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-34662641

RESUMEN

In this study, biochar derived from spent coffee grounds (SCGB) was used to adsorb norfloxacin (NOR) in water. The biochar properties were interpreted by analysis of the specific surface area, morphology, structure, thermal stability, and functional groups. The impacts of pH, NOR, and ion's present on SCGB performance were examined. The NOR adsorption mode of SCGB is best suited to the Langmuir model (R2 = 0.974) with maximum absorption capacity (69.8 mg g-1). By using a Response Surface Method (RSM), optimal adsorption was also found at pH of 6.26, NOR of 24.69 mg L-1, and SCGB of 1.32 g L-1. Compared with biochars derived from agriculture such as corn stalks, willow branches, potato stem, reed stalks, cauliflower roots, wheat straw, the NOR adsorption capacity of SCGB was 2-30 times higher, but less than 3-4 times for biochars made from Salix mongolica, luffa sponge and polydopamine microspheres. These findings reveal that spent coffee grounds biochar could effectively remove NOR from aqueous solutions. Approaching biochar derived from coffee grounds would be a promising eco-friendly solution because it utilizes solid waste, saves costs, and creates adsorbents to deal with emerging pollutants like antibiotics.


Asunto(s)
Café , Norfloxacino , Adsorción , Carbón Orgánico , Agua
12.
BMB Rep ; 54(10): 528-533, 2021 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-34488936

RESUMEN

Osteoarthritis (OA) is a degenerative disorder that can result in the loss of articular cartilage. No effective treatment against OA is currently available. Thus, interest in natural health products to relieve OA symptoms is increasing. However, their qualities such as efficacy, toxicity, and mechanism are poorly understood. In this study, we determined the efficacy of avenanthramide (Avn)-C extracted from oats as a promising candidate to prevent OA progression and its mechanism of action to prevent the expression of matrix-metalloproteinases (MMPs) in OA pathogenesis. Interleukin-1 beta (IL-1ß), a proinflammatory cytokine as a main causing factor of cartilage destruction, was used to induce OAlike condition of chondrocytes in vitro. Avn-C restrained IL-1ß- mediated expression and activity of MMPs, such as MMP-3, -12, and -13 in mouse articular chondrocytes. Moreover, Avn-C alleviated cartilage destruction in experimental OA mouse model induced by destabilization of the medial meniscus (DMM) surgery. However, Avn-C did not affect the expression of inflammatory mediators (Ptgs2 and Nos) or anabolic factors (Col2a1, Aggrecan, and Sox9), although expression levels of these genes were upregulated or downregulated by IL-1ß, respectively. The inhibition of MMP expression by Avn-C in articular chondrocytes was mediated by p38 kinase and c-Jun N-terminal kinase (JNK) signaling, but not by ERK or NF-κB. Interestingly, Avn-C added with SB203580 and SP600125 as specific inhibitors of p38 kinase and JNK, respectively, enhanced its inhibitory effect on the expression of MMPs in IL-1ß treated chondrocytes. Taken together, these results suggest that Avn-C is an effective candidate to prevent OA progression and a natural health product to relieve OA pathogenesis. [BMB Reports 2021; 54(10): 528-533].


Asunto(s)
Condrocitos/metabolismo , Osteoartritis/tratamiento farmacológico , ortoaminobenzoatos/farmacología , Animales , Avena/metabolismo , Condrocitos/efectos de los fármacos , Modelos Animales de Enfermedad , Expresión Génica/efectos de los fármacos , Expresión Génica/genética , Regulación de la Expresión Génica/efectos de los fármacos , Regulación de la Expresión Génica/genética , Interleucina-1beta/efectos de los fármacos , Interleucina-1beta/metabolismo , Proteínas Quinasas JNK Activadas por Mitógenos/metabolismo , Sistema de Señalización de MAP Quinasas/efectos de los fármacos , Metaloproteinasas de la Matriz/efectos de los fármacos , Metaloproteinasas de la Matriz/genética , Ratones , FN-kappa B/metabolismo , Osteoartritis/patología , Extractos Vegetales/farmacología , Cultivo Primario de Células , Transducción de Señal/efectos de los fármacos , ortoaminobenzoatos/metabolismo
14.
Med Acupunct ; 33(6): 420-427, 2021 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-34976275

RESUMEN

Objective: Major depressive disorder (MDD) is a major public health problem due to MDD's increasing incidence among adults worldwide. While selective serotonin reuptake inhibitors (SSRIs), such as paroxetine, are considered to be the most effective treatment for MDD, the adverse effects of SSRIs should not be neglected. The aim of this research was to evaluate the effectiveness of acupuncture as a complement to paroxetine systematically for improving quality of life (QoL) for patients with MDD. Methods and Materials: Chinese and English electronic databases were searched, randomized controlled clinical studies were collected, data entry was managed, and a meta-analysis was performed to evaluate the QoL of the patients pre and post treatment. Results: There were 5 studies included in the review, in which the researchers compared the QoL of patients with MDD treated with: paroxetine + acupuncture (both electroacupuncture and traditional acupuncture) or paroxetine alone. In all aspects-including physical health, psychologic health, social relationships, and environment-patients treated with the combination therapy experienced a significant improvements in QoL compared the patients treated with the single therapy. Conclusions: Using acupuncture as a complementary treatment improved QoL in patients with MDD.

15.
Nat Prod Res ; 35(20): 3384-3389, 2021 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-31815547

RESUMEN

A new norlupane triterpenoid, 29-norlupane-1ß-hydroxy-3,20-dione (1), along with ten known compounds, 29-norlup-1-ene-3,20-dione (2), phyllanthol (3), phyllanthone (4), glochidone (5), lupeol (6), lupeone (7), 4-hydroxybenzoic acid (8), 4-hydroxybenzaldehyde (9), phyllane A (10) and methyl ß-orsellinate (11) were isolated the twigs and leaves of Phyllanthus acidus. The structure of 1 was identified by interpretation of their spectroscopic data and comparison with those reported in the literature. In addition, all isolated compounds 1-11 were evaluated for their antioxidant activity.


Asunto(s)
Phyllanthus , Triterpenos , Antioxidantes , Extractos Vegetales , Hojas de la Planta
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.
Planta Med ; 86(11): 776-781, 2020 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-32483775

RESUMEN

Chemical investigation of the lichen Parmotrema tsavoense led to the isolation of 5 new depsidones, parmosidones F - J (1:  - 5: ). These compounds were structurally elucidated using spectroscopic methods including HRESIMS and 2D NMR data. Compounds 1, 3: , and 4: were evaluated for their inhibition of α-glucosidase. All exhibited potent α-glucosidase inhibitory activity with IC50 values ranging from 10.7 to 17.6 µM, which was much lower than that of the positive control acarbose (IC50 449 µM).


Asunto(s)
Líquenes , alfa-Glucosidasas , Depsidos , Inhibidores de Glicósido Hidrolasas , Lactonas , Extractos Vegetales
18.
Eur J Med Chem ; 196: 112295, 2020 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-32325366

RESUMEN

Prion diseases or transmissible spongiform encephalopathies (TSEs) are a group of rare neurodegenerative disorders. TSEs are characterized by the accumulation of prions (PrPSc) that represent pathological isoforms of the physiological cellular prion protein PrPC. Although the conversion of PrPC to PrPSc is still not completely understood, blocking this process may lead to develop new therapies. Here, we have generated a pharmacophore model, based on anti-prion molecules reported in literature to be effective in phenotypic assay. The model was used to conduct a virtual screen of commercial compound databases that selected a small library of ten compounds. These molecules were then screened in mouse neuroblastoma cell line chronically infected with prions (ScN2a) after excluding neurotoxicity. 1 has been identified as the therapeutic hit on the basis of the following evidence: chronic treatments of ScN2a cells using 1 eliminate PrPSc loaded in both Western blotting analysis and Real-Time Quaking-Induced Conversion (RT-QuIC) assay. We also proposed the mechanism of action of 1 by which it has the ability to bind PrPC and consequentially blocks prion conversion. Herein we describe the results of these efforts.


Asunto(s)
Fenotiazinas/farmacología , Proteínas Priónicas/antagonistas & inhibidores , Animales , Línea Celular , Evaluación Preclínica de Medicamentos , Ratones , Modelos Moleculares , Estructura Molecular , Fenotiazinas/química , Proteínas Priónicas/aislamiento & purificación , Proteínas Priónicas/metabolismo , Relación Estructura-Actividad Cuantitativa
19.
Fitoterapia ; 142: 104512, 2020 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-32061910

RESUMEN

Chemical investigation of the cultured polyspore-derived mycobionts of a Pseudopyrenula subnudata lichen led to the isolation of two new compounds, subnudatones A and B (1 and 2), together with four known compounds, 1-(2-hydroxy-1,2,6-trimethyl-1,2,4a,5,6,7,8,8a-octahydronaphthalen-1-yl)ethanone (3), libertalide C (4), aspermytin A (5), and 6,7-dimethoxy-4-hydroxymellin (6). Their chemical structures were elucidated by extensive 1D and 2D NMR analysis and high resolution mass spectroscopy, and comparisons were made with the literature. The absolute configuration of 1 was defined unambiguously using single crystal X-ray crystallography. Compound 1 represents the first dimeric decalin polyketide to be found in nature. The in vitro cytotoxicity of 1 against two cancer cell lines (K562 and MCF-7) was evaluated. Compound 1 showed moderate cytotoxic activity with IC50 values of 23.5 ± 1.0 and 51.9 ± 1.4 µM, respectively.


Asunto(s)
Antineoplásicos/aislamiento & purificación , Ascomicetos , Policétidos/aislamiento & purificación , Antineoplásicos/química , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Células K562 , Células MCF-7 , Policétidos/química
20.
Nutr J ; 18(1): 82, 2019 12 02.
Artículo en Inglés | MEDLINE | ID: mdl-31791333

RESUMEN

BACKGROUND: Deficient and insufficient vitamin D status (defined as serum 25(OH)D < 30 nmol/L and > 50 nmol/L) is prevalent worldwide and associated with decreased muscle strength and poor bone health. We aimed to investigate the effect of vitamin D fortification on bone markers and muscle strength among younger adult women at risk of vitamin D deficiency. METHODS: A 12-week randomised double-blinded placebo-controlled winter intervention trial, providing 30 µg vitamin D3/day through fortified yoghurt, cheese, eggs and crisp-bread or similar placebo products. Participants were 143 women of Danish and Pakistani origin 18-50 years of age, living in Denmark, randomised into four groups stratified by ethnicity. Serum 25-hydroxyvitamin D (25(OH)D) by LC-MS/MS and the secondary endpoints: four specific bone markers (osteocalcin (OC), Bone specific Alkaline Phosphatase (BALP), Procollagen type 1 amino-terminal propeptide (P1NP), C-terminal crosslinked telopeptide of type 1 collagen (CTX)) and three muscle strength measures (handgrip, knee extension strength, chair-standing), were assessed using one-way ANOVA, Tukey HSD and subsequent linear ANCOVA models, adjusted for relevant covariates. RESULTS: Significantly increased serum 25(OH)D concentration from 53.3 (17) to 77.8 (14) nmol/L and from 44.5 (21) to 54.7 (18) nmol/L among Danish and Pakistani women in the fortified groups, respectively (P <  0.05). The bone turnover markers OC, BALP, P1NP and CTX did not change significantly. Muscle strength by handgrip, knee extension and chair-standing test did not change significantly following the intervention. CONCLUSIONS: Consumption of vitamin D fortified foods for 12 weeks did not result in significant changes of the bone turnover markers OC, BALP, P1NP and CTX. Muscle strength measured as hand grip strength, knee extension strength and chair-standing did not change significantly following the intervention.


Asunto(s)
Fosfatasa Alcalina/sangre , Colágeno Tipo I/sangre , Alimentos Fortificados , Fuerza Muscular , Osteocalcina/sangre , Vitamina D/administración & dosificación , Vitamina D/sangre , Adolescente , Adulto , Biomarcadores/sangre , Remodelación Ósea , Dinamarca , Método Doble Ciego , Femenino , Humanos , Persona de Mediana Edad , Pakistán , Fragmentos de Péptidos/sangre , Procolágeno/sangre , Vitaminas/administración & dosificación , Vitaminas/sangre , Adulto Joven
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