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1.
Chem Biodivers ; : e202401224, 2024 Aug 16.
Artículo en Inglés | MEDLINE | ID: mdl-39149874

RESUMEN

Piper longum L.(PL)  is considered one of the most important species traditionally used for treating various ailments and has indicated the presence of alkaloids, flavonoids, and steroids. In this study, we isolated the chemical compounds of PLleaves,andmeasuredNO, IL-6, iNOS, as well as COX-2 protein levels. In addition, molecular docking analysis were used to further understand anti-inflammation effect of the compounds. We identified one new alkaloid named piperlongumine A (1) with ten known compounds (2-11). The new compound (1) and two other alkaloids 2E)-3-(4-hydroxy-3-methoxyphenyl)-1-(pyrrol-1-yl)propanone (7) and piperchabamide A (8) significantlyreduced NO production in LPS-stimulated RAW 264.7 cells with the IC50 values of 0.97 ± 0.05 mM, 0.91 ± 0.07mM, 1.63 ± 0.14 mM, respectively. Moreover, at concentration of 2 mM, compound 1 inhibited approximately 98 ± 0.64 % of IL-6 secretion, and decreased  iNOS and COX-2 protein level by about 96 and 19 folds compared to LPS treatment alone, respectively. Furthermore, compounds 1, 7, and 8 were predicted to bind and inhibit IL-6, TNF-a, and iNOS, with compound 1 showing the highest binding energy of -7.09 kcal/mol. This study provides new insights for potential anti-inflammatory drug design and warrants further investigation.

2.
RSC Adv ; 14(23): 16445-16458, 2024 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-38774611

RESUMEN

Using DFT calculations, the structural and electronic properties of the ZZ7 p-PdSe2 nanoribbons (ZZ7) with the four kinds of vacancy defects, including ZZ7-VPd, ZZ7-VSe, ZZ7-VPd+Se, and ZZ7-V2Se are studied, in which their stability, diverse geometries, and altered electronic properties are determined through the formation energies, optimal structural parameters, electronic band structures, and DOSs. Specifically, the formation energies of all studied systems show significant negative values around -3.9 eV, evidencing their good thermal stability. The geometries of four defective structures exhibit different diversification, whereas only the ZZ7-V2Se structure possesses the highly enhanced feature, identified as the most effective substrate for the acetone and acetonitrile adsorption. On the electronic behaviors, the ZZ7 band structure displays the nonmagnetic metallic characteristics that become the ferromagnetic half-metallic band structures for the ZZ7-VPd and ZZ7-VSe and the ferromagnetic semi-metallic band structures for the ZZ7-VPd+Se and ZZ7-V2Se. For adsorption of the acetone and acetonitrile on the ZZ7-V2Se structure, the energetic stability, adsorption sites, adsorption distances, charge transfers, and electronic characteristics of the adsorbed systems are determined by the adsorption energies, optimal adsorption sites, adsorption distances, Mulliken populations, and DOSs. The adsorption energies of the acetone- and acetonitrile-adsorbed ZZ7-V2Se systems display significant values at -1.2 eV and -0.86 eV at the preferable sites of 8 and 11, respectively, indicating their great adsorption ability. The adsorption mechanism of the acetone- and acetonitrile-adsorbed systems belongs to the physisorption owing to absence of chemical bonds, in which the bond lengths of the ZZ7-V2Se substrate show a very small deviation. Under the acetone and acetonitrile adsorptions, the ferromagnetic semi-metallic DOSs of the ZZ7-V2Se become the ferromagnetic half-metallic DOSs for the ZZ7-V2Se-acetone-8 and the ferromagnetic semiconducting DOSs for the ZZ7-V2Se-acetonitrile-11. Our systematic results can provide a complete understanding of the acetone- and acetonitrile adsorptions on the potential ZZ7-V2Se structure, which is very useful for nanosensor application.

4.
Front Oncol ; 13: 1210487, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37456235

RESUMEN

Prostate cancer (PCa) remains the most diagnosed non-skin cancer amongst the American male population. Treatment for localized prostate cancer consists of androgen deprivation therapies (ADTs), which typically inhibit androgen production and the androgen receptor (AR). Though initially effective, a subset of patients will develop resistance to ADTs and the tumors will transition to castration-resistant prostate cancer (CRPC). Second generation hormonal therapies such as abiraterone acetate and enzalutamide are typically given to men with CRPC. However, these treatments are not curative and typically prolong survival only by a few months. Several resistance mechanisms contribute to this lack of efficacy such as the emergence of AR mutations, AR amplification, lineage plasticity, AR splice variants (AR-Vs) and increased kinase signaling. Having identified SRC kinase as a key tyrosine kinase enriched in CRPC patient tumors from our previous work, we evaluated whether inhibition of SRC kinase synergizes with enzalutamide or chemotherapy in several prostate cancer cell lines expressing variable AR isoforms. We observed robust synergy between the SRC kinase inhibitor, saracatinib, and enzalutamide, in the AR-FL+/AR-V+ CRPC cell lines, LNCaP95 and 22Rv1. We also observed that saracatinib significantly decreases AR Y534 phosphorylation, a key SRC kinase substrate residue, on AR-FL and AR-Vs, along with the AR regulome, supporting key mechanisms of synergy with enzalutamide. Lastly, we also found that the saracatinib-enzalutamide combination reduced DNA replication compared to the saracatinib-docetaxel combination, resulting in marked increased apoptosis. By elucidating this combination strategy, we provide pre-clinical data that suggests combining SRC kinase inhibitors with enzalutamide in select patients that express both AR-FL and AR-Vs.

5.
Nanomaterials (Basel) ; 13(11)2023 May 25.
Artículo en Inglés | MEDLINE | ID: mdl-37299633

RESUMEN

One-dimensional (1D) novel pentagonal materials have gained significant attention as a new class of materials with unique properties that could influence future technologies. In this report, we studied the structural, electronic, and transport properties of 1D pentagonal PdSe2 nanotubes (p-PdSe2 NTs). The stability and electronic properties of p-PdSe2 NTs with different tube sizes and under uniaxial strain were investigated using density functional theory (DFT). The studied structures showed an indirect-to-direct bandgap transition with slight variation in the bandgap as the tube diameter increased. Specifically, (5 × 5) p-PdSe2 NT, (6 × 6) p-PdSe2 NT, (7 × 7) p-PdSe2 NT, and (8 × 8) p-PdSe2 NT are indirect bandgap semiconductors, while (9 × 9) p-PdSe2 NT exhibits a direct bandgap. In addition, under low uniaxial strain, the surveyed structures were stable and maintained the pentagonal ring structure. The structures were fragmented under tensile strain of 24%, and compression of -18% for sample (5 × 5) and -20% for sample (9 × 9). The electronic band structure and bandgap were strongly affected by uniaxial strain. The evolution of the bandgap vs. the strain was linear. The bandgap of p-PdSe2 NT experienced an indirect-direct-indirect or a direct-indirect-direct transition when axial strain was applied. A deformability effect in the current modulation was observed when the bias voltage ranged from about 1.4 to 2.0 V or from -1.2 to -2.0 V. Calculation of the field effect I-V characteristic showed that the on/off ratio was large with bias potentials from 1.5 to 2.0 V. This ratio increased when the inside of the nanotube contained a dielectric. The results of this investigation provide a better understanding of p-PdSe2 NTs, and open up potential applications in next-generation electronic devices and electromechanical sensors.

6.
Radiol Case Rep ; 18(7): 2427-2433, 2023 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-37214326

RESUMEN

Top-of-the-basilar artery occlusion frequently causes infarction of the midbrain, thalamus, and portions of the temporal and occipital lobes as the vascular supply of these regions comes from the posterior communicating and posterior cerebral arterial tributaries of the basilar artery. Clinical signs include an array of visual, oculomotor, and behavioral abnormalities, usually without prominent motor dysfunction, which makes diagnosis challenging for those inexperienced with these sign. We describe a 59-year-old male presenting with acute ischemic stroke due to top-of-the-basilar artery occlusion. Despite attempting several paraclinical examinations relating the sudden coma with Glasgow Coma Scale of 6 points, the neuroimaging detected the large vessel occlusion that was difficult to recognize. After confirming top-of-the-basilar artery occlusion, the recanalization was realized immediately. The patient was discharged with good clinical recovery.

7.
RSC Adv ; 13(15): 10082-10089, 2023 Mar 27.
Artículo en Inglés | MEDLINE | ID: mdl-37006357

RESUMEN

The use of non-invasive approaches for monitoring therapy processes in cancer patients at late stages is truly needed. In this work, we aim to develop an electrochemical interface based on polydopamine combined with gold nanoparticles and reduced graphene oxide for impedimetric detection of lung cancer cells. Gold nanoparticles (around 75 nm) were dispersed onto reduced graphene oxide material pre-electrodeposited onto disposable fluorine doped tin oxide electrodes. The coordination between gold and carbonaceous material has somehow improved the mechanical stability of this electrochemical interface. Polydopamine was later introduced onto modified electrodes via self-polymerization of dopamine in an alkaline solution. The result has demonstrated the good adhesion and biocompatibility of polydopamine towards A-549 lung cancer cells. The presence of the two conductive materials (gold nanoparticles and reduced graphene oxide) has led to a six-times decrease in charge transfer resistance of polydopamine film. Finally, the as-prepared electrochemical interface was employed for impedimetric detection of A-549 cells. The detection limit was estimated to be only 2 cells per mL. These findings have proved the possibilities to use advanced electrochemical interfaces for point-of-care applications.

8.
Nat Prod Res ; 37(12): 1969-1977, 2023 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-35994376

RESUMEN

Four new N-phenethylbenzamide derivatives, named piperbetamides A-D (1-4), and six allylbenzene derivatives (5-10) were isolated from the stems of Piper betle L. Their structures were determined by HR-ESI-MS and NMR spectroscopic methods. Compounds 1-10 were evaluated for their inhibitory effects on the growth of nine microorganisms including five Gram-negative (Escherichia coli, Salmonella enterica serovar Typhimurium, Shigella flexneri, Pseudomonas aeruginosa, and Extended-spectrum beta-lactam resistant Klebsiella pneumoniae), three Gram-positive (Listeria monocytogenes, Methicilin-resistant Staphylococcus aureus, Vancomycin-resistant Enterococcus faecalis), and one yeast (Candida albicans) strains. Compounds 1, 3, 4, 6 and 10 exhibited potential antimicrobial activity against S. flexneri, L. monocytogenes, methicillin-resistant S. aureus and vancomycin-resistant E. faecalis with minimum inhibitory concentration (MIC) values in the range of 16-32 µg/mL.


Asunto(s)
Staphylococcus aureus Resistente a Meticilina , Piper betle , Antibacterianos/química , Vancomicina/farmacología
9.
Int Immunopharmacol ; 111: 109038, 2022 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-35932612

RESUMEN

Bone homeostasis is maintained by a combination of osteoclast-mediated bone resorption and osteoblast-mediated bone formation. Excessive osteoclast activity is linked to several bone-related disorders, including osteoporosis and rheumatoid arthritis. Pharmacological therapy might have a number of adverse effects. Therefore, the development of natural anti-osteoclastogenic drugs with greater efficacy and fewer adverse effects is desirable. In this study, the anti-osteoclastogenic effects of 23-hydroxyursolic acid (HUA), a triterpene isolated from Viburnum lutescens, were investigated in vitro and in vivo. HUA significantly inhibited receptor activator of nuclear factor kappa-B ligand (RANKL)-induced mature osteoclast differentiation by reducing the number of tartrate-resistant acid phosphatase (TRAP)-positive osteoclasts and F-actin ring formation. It also inhibited the expression of osteoclast-specific marker genes such OSCAR, MMP-9, TRAP, DC-STAMP, and CtsK, as well as transcription factors, c-Fos and nuclear factor of activated T cells cytoplasmic 1 (NFATc1) in response to RANKL. Mice orally administered with HUA (25 and 50 mg/kg) exhibited significant protection against bone loss and osteoclast formation induced by lipopolysaccharide (LPS). HUA suppressed RANKL-induced nuclear factor kappa B (NF-κB) activation and phosphorylation of JNK and ERK mitogen-activated protein kinases (MAPKs). These results suggest that HUA attenuates osteoclast formation in vitro and in vivo by suppressing the RANKL-mediated AP1, NF-κB, and NFATc1 pathways. Therefore, HUA may be a lead compound for the prevention or treatment of osteolytic bone disorders.


Asunto(s)
Resorción Ósea , Triterpenos , Viburnum , Animales , Resorción Ósea/prevención & control , Diferenciación Celular , Lipopolisacáridos/farmacología , Ratones , FN-kappa B/metabolismo , Factores de Transcripción NFATC/metabolismo , Osteoclastos , Osteogénesis , Ligando RANK/metabolismo , Triterpenos/farmacología , Triterpenos/uso terapéutico , Viburnum/metabolismo
10.
Phytomedicine ; 105: 154378, 2022 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-35961265

RESUMEN

BACKGROUND: Elevated activity of osteoclasts (OCs) is linked to osteolytic bone diseases, such as osteoporosis and rheumatoid arthritis. Developing natural anti-osteoclastogenic compounds with greater efficacy and fewer adverse effects is crucial for preventing or treating osteolytic bone diseases. N-triterpene cycloartane saponins (NTCSs) are rarely found in nature, and their inhibitory effects on OC differentiation in vitro and in vivo have not yet been explored. PURPOSE: This study was aimed to investigate the effect of mussaendoside O, an NTCS isolated from Mussaenda pubescens, on RANKL-induced OC differentiation and its underlying mechanism in vitro, and lipopolysaccharide (LPS)-induced bone resorption in a mouse model. METHODS: The content of mussaendoside O in methanol extract of M. pubescens was determined by HPLC. The inhibitory effects of mussaendoside O on RANKL-induced OC formation were assessed using TRAP staining, western blotting, immunofluorescence staining, and real-time qPCR. Meanwhile, the effects of mussaendoside O on LPS-induced inflammatory responses were assessed using a Griess reagent and qPCR. The effects of mussaendoside O on LPS-induced bone resorption in a mouse model were evaluated using micro-CT and immunohistochemical staining. RESULTS: Mussaendoside O inhibited RANKL-induced TRAP-positive multinucleated OC formation in a concentration-dependent manner without affecting cell viability. However, mussaendoside O did not inhibit LPS-induced mRNA expression of COX-2, iNOS, and TNF-α. Mice orally administrated with mussaendoside O exhibited significant protection from LPS-induced bone resorption and OC formation. At the molecular level, mussaendoside O suppressed RANKL-activated phosphorylation of p38 MAPK and JNK, as well as c-Fos expression. In addition, mussaendoside O suppressed RANKL-induced NFATc1 activation and the expression of its target genes, including OSCAR, DC-STAMP, CtsK, and TRAP. CONCLUSION: Mussaendoside O attenuates OC differentiation in vitro and LPS-induced bone resorption in a mouse model by inhibiting the RANKL-activated c-Fos/NFATc1 signaling pathways. Therefore, mussaendoside O may be a valuable lead compound for preventing or treating of osteolytic bone diseases.


Asunto(s)
Resorción Ósea , Saponinas , Triterpenos , Animales , Diferenciación Celular , Lipopolisacáridos , Ratones , Factores de Transcripción NFATC , Osteoclastos , Osteogénesis , Ligando RANK
11.
Nat Prod Res ; 36(24): 6232-6239, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-34989301

RESUMEN

Using combined chromatographic separation techniques, three new triterpenoids named lycomclavatols A-C (1-3), a new natural product, methyl lycernuate-A (4), as well as seven known compounds (5-11), were isolated from the methanol extract of the whole plants of Lycopodium clavatum. Their chemical structures were established based on 1 D/2D NMR and HR-ESI-MS spectroscopic analyses. Among the isolates, compound 1 exhibited inhibitory activity on NO production in LPS-stimulated BV2 cells (IC50 = 36.0 µM). In addition, 1 was cytotoxic against both HepG2 and A549 cancer cell lines, with IC50 values of 40.7 and 87.0 µM, respectively. Compounds 10 and 11 showed cytotoxicity on only HepG2 and A549 cells, with IC50 values of 91.2 and 57.6 µM, respectively. Our results contribute to understanding more the secondary metabolites produced by L. clavatum and provide a scientific rationale for further investigations of anti-inflammatory and anticancer effects for this valuable medicinal plant.


Asunto(s)
Lycopodium , Plantas Medicinales , Triterpenos , Lycopodium/química , Triterpenos/farmacología , Triterpenos/química , Óxido Nítrico/metabolismo , Plantas Medicinales/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Concentración 50 Inhibidora
12.
Nat Prod Res ; 36(18): 4597-4604, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-34898346

RESUMEN

The methanolic extract of Mussaenda pubescens Dryand leaves exhibited significant anti-osteoclastogenic activity. Chemical investigation of M. pubescens led to the isolation of one new cycloartane saponin, mussaendoside X (1) along with eight known compounds: heinsiagenin A 3-O-[α-L-rhamnopyranosyl-(1→2)-O-ß-D-glucopyranosyl-(1→2)]-O-ß-D-glucopyranoside (2), mussaendoside O (3), heinsiagenin A 3-O-[α-L-rhamnopyranosyl-(1→2)-O-ß-D-glucopyranosyl-(1→2)]-O-ß-D-glucopyranosyl-(1→4)-O-ß-D-glucopyranoside (4), mussaendoside G (5), mussaendoside U (6), shanzhiside methyl ester (7), barlerin (8) and musaenoside (9). Their structures were elucidated by extensive spectroscopic methods including 1D- and 2D-NMR as well as MS analysis and comparison with the literature. Cycloartane saponins 1-6 positively suppressed osteoclast formation in an anti-osteoclastogenic screening assay. Consequently, treatment of RANKL-stimulated RAW 264.7 cells with compounds 1-4 significantly decreased the number of osteoclasts in a concentration-dependent manner. Six compounds from M. pubescens, with the new cycloartane, mussaendoside X, were shown for the first time as potential effective inhibitors of osteoclastogenesis.


Asunto(s)
Rubiaceae , Saponinas , Triterpenos , Espectroscopía de Resonancia Magnética , Osteogénesis , Rubiaceae/química , Saponinas/química , Saponinas/farmacología , Triterpenos/química , Triterpenos/farmacología
13.
Nat Prod Res ; 36(16): 4045-4051, 2022 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-34498971

RESUMEN

Phytochemical investigation of the whole plants of Lycopodiella cernua resulted in the isolation and identification of three new compounds (1-3), namely lycocernuaside E (1), lycernuic ketone F (2), and lycernuic B (3) and 12 known ones (4-15). Their chemical structures were established based on 1 D/2D NMR spectroscopic and HR-ESI-MS data analyses. Compounds 5, 12, and 13 displayed NO inhibitory effects in LPS-stimulated BV2 cells, with IC50 values of 21.2 ± 1.1, 28.5 ± 1.4, and 21.9 ± 1.1 µM, respectively. In addition, cytotoxic activity of the isolated compounds against MCF7 (breast carcinoma), HepG2 (hepatocarcinoma), and SK-Mel2 (melanoma) cancer cell lines were also reported.


Asunto(s)
Lycopodiaceae , Triterpenos , Antiinflamatorios/química , Antiinflamatorios/farmacología , Línea Celular Tumoral , Lycopodiaceae/química , Estructura Molecular , Triterpenos/química
14.
Nat Prod Res ; 35(20): 3390-3395, 2021 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-31821052

RESUMEN

In our search for anti-inflammatory constituents from Vietnamese plants, the methanolic extract of Helicteres viscida was found to exhibit inhibitory effect on LPS-induced NO production in RAW264.7 cells. Phytochemical investigation of this plant led to isolation of four sulphated flavones (1-4), including one new compound 5,3',4'-trihydroxy-7-methoxy-8-O-sulphate flavone (1), and two pregnane-type steroids (5 and 6), including one new compound 7-epi-heligenin B (5). Their structures were elucidated by 1D and 2D NMR as well as HR-QTOF-MS experiments. Among isolated compounds, heligenin B (6) exhibited potent inhibitory effect on LPS-induced NO production in RAW264.7 cells with IC50 of 1.23 ± 0.05 µM. The activity of 6 was comparable to that of the positive control cardamonin.


Asunto(s)
Flavonas , Malvaceae , Flavonas/farmacología , Estructura Molecular , Fitoquímicos , Pregnanos , Sulfatos
15.
Nat Prod Res ; 35(9): 1399-1405, 2021 May.
Artículo en Inglés | MEDLINE | ID: mdl-31402701

RESUMEN

Sixteen sesquiterpenoids (1 - 16), including two new compounds namely saussucostusosides A and B (1 and 2), were isolated from the roots of Saussurea costus by various chromatographic separations. Their structures were elucidated by 1 D and 2 D NMR and HR-QTOF-MS experiments. Among isolated compounds, costunlide (6), 3ß-[4-hydroxymethacryloyloxy]-8α-hydroxycostunolide (10) and 11ß,13-dihydrozaluzanin C (16) exhibited potent inhibitory effects on LPS-induced NO production in RAW264.7 cells with IC50 values of 7.08 ± 0.34, 2.40 ± 0.06 and 5.55 ± 0.24 µM, respectively.


Asunto(s)
Saussurea/química , Sesquiterpenos/aislamiento & purificación , Animales , Espectroscopía de Resonancia Magnética con Carbono-13 , Concentración 50 Inhibidora , Lipopolisacáridos/farmacología , Ratones , Óxido Nítrico/biosíntesis , Extractos Vegetales/química , Raíces de Plantas/química , Espectroscopía de Protones por Resonancia Magnética , Células RAW 264.7 , Sesquiterpenos/química
16.
Int J Anal Chem ; 2020: 8873614, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-33204273

RESUMEN

A precise HPLC-DAD-based quantification together with the metabolomics statistical method was developed to distinguish and control the quality of Fallopia multiflora, a popular medicinal material in Vietnam. Multivariate statistical methods such as hierarchical clustering analysis and principal component analysis were utilized to compare and discriminate six natural and twelve commercial samples. 2,3,4',5-Tetrahydroxystilbene 2-O-ß-D-glucopyranoside (THSG) (1), emodin (4), and the new compound 6-hydroxymusizin 8-O-α-D-apiofuranosyl-(1⟶6)-ß-D-glucopyranoside (5) could be considered as important markers for classification of F. multiflora. Furthermore, seven phenolics were quantified that the variation in the contents of selected metabolites revealed the differences in the quality of natural and commercial samples. Recovery of the compounds from the analytes was more than 98%, while the limits of detection (LOD) and the limits of quantitation (LOQ) ranged from 0.5 to 6.6 µg/ml and 1.5 to 19.8 µg/ml, respectively. The linearity, LOD, LOQ, precision, and accuracy satisfied the criteria FDA guidance on bioanalytical methods. Overall, this method is a promising tool for discrimination and quality assurance of F. multiflora products.

17.
Int J Mol Sci ; 21(15)2020 Jul 23.
Artículo en Inglés | MEDLINE | ID: mdl-32718089

RESUMEN

Olean-12-en-27-oic acids possess a variety of pharmacological effects. However, their effects and underlying mechanisms on osteoclastogenesis remain unclear. This study aimed to investigate the anti-osteoclastogenic effects of five olean-12-en-27-oic acid derivatives including 3α,23-isopropylidenedioxyolean-12-en-27-oic acid (AR-1), 3-oxoolean-12-en-27-oic acid (AR-2), 3α-hydroxyolean-12-en-27-oic acid (AR-3), 23-hydroxy-3-oxoolean-12-en-27-oic acid (AR-4), and aceriphyllic acid A (AR-5). Among the five olean-12-en-27-oic acid derivatives, 3-hydroxyolean-12-en-27-oic acid derivatives, AR-3 and AR-5, significantly inhibited receptor activator of nuclear factor-κB ligand (RANKL)-induced mature osteoclast formation by reducing the number of tartrate-resistant acid phosphatase (TRAP)-positive osteoclasts, F-actin ring formation, and mineral resorption activity. AR-3 and AR-5 decreased RANKL-induced expression levels of osteoclast-specific marker genes such as c-Src, TRAP, and cathepsin K (CtsK) as well as c-Fos and nuclear factor of activated T cells cytoplasmic 1 (NFATc1). Mice treated with either AR-3 or AR-5 showed significant protection of the mice from lipopolysaccharide (LPS)-induced bone destruction and osteoclast formation. In particular, AR-5 suppressed RANKL-induced phosphorylation of JNK and ERK mitogen-activated protein kinases (MAPKs). The results suggest that AR-3 and AR-5 attenuate osteoclast formation in vitro and in vivo by suppressing RANKL-mediated MAPKs and NFATc1 signaling pathways and could potentially be lead compounds for the prevention or treatment of osteolytic bone diseases.


Asunto(s)
Resorción Ósea , Lipopolisacáridos/toxicidad , Sistema de Señalización de MAP Quinasas/efectos de los fármacos , Ácido Oleanólico/análogos & derivados , Osteoclastos , Ligando RANK/metabolismo , Animales , Resorción Ósea/inducido químicamente , Resorción Ósea/tratamiento farmacológico , Resorción Ósea/metabolismo , Resorción Ósea/patología , Ratones , Ratones Endogámicos ICR , Ácido Oleanólico/farmacología , Osteoclastos/metabolismo , Osteoclastos/patología , Células RAW 264.7
18.
PLoS Negl Trop Dis ; 14(6): e0008430, 2020 06.
Artículo en Inglés | MEDLINE | ID: mdl-32555599

RESUMEN

BACKGROUND: Data on incidence of snakebites and the responsible snake species are largely missing in Vietnam and comprehensive national guidelines for management of snakebite envenoming are not yet available. They are needed to estimate the scope of this health problem, to assess the demand for snake antivenom and to ensure the best possible treatment for snakebite victims. METHODOLOGY/PRINCIPLE FINDINGS: A cross-sectional community-based survey was conducted from January to April 2018. Multistage cluster sampling was applied and snakebite incidence in Can Tho municipality, excluding two central districts of Can Tho city, was calculated at 48 (95%-confidence interval (CI): 20.5-99.8) snakebites per 100,000 person-years. Seven snakebite victims found during the survey reported 3 bites from green pit vipers and 4 bites from non-venomous snakes. In 2017 two treatment centres for snakebite envenoming in Can Tho city, the Military Hospital 121 and the Paediatric Hospital, received 520 admissions of snakebite victims. Two hundred sixty-seven came from Can Tho Municipality and 253 from neighbouring provinces. According to these data, the incidence of snakebites for Can Tho municipality was calculated at 21 (95%-CI: 18.5-23.7) snakebites per 100,000 person-years. Incidence was 14 (95%-CI: 12-17) snakebites per 100,000 person years in those 7 districts of the municipality which were part of the community survey. Green pit vipers were responsible for 92% of snakebite envenoming. Antivenom, antibiotics and corticosteroids were administered to 405 (90%), 379 (84%), and 310 (69%) out of 450 patients, respectively. CONCLUSIONS: Incidence of snakebites in Can Tho Municipality is relatively low and green pit vipers are responsible for the vast majority of bites. Approximately one third of snakebite patients sought medical care in hospitals and although hospital data still underestimate the real incidence of snakebites, these statistics are valuable and can be obtained fast and inexpensively. Evaluation of patients' records indicates the need for development of guidelines for management of snakebite envenoming in Vietnam to ensure a rational use of antivenom and ancillary treatments.


Asunto(s)
Mordeduras de Serpientes/epidemiología , Serpientes/clasificación , Adolescente , Adulto , Anciano , Anciano de 80 o más Años , Animales , Antibacterianos/sangre , Antivenenos/uso terapéutico , Niño , Preescolar , Estudios Transversales , Composición Familiar , Femenino , Humanos , Incidencia , Lactante , Masculino , Persona de Mediana Edad , Mordeduras de Serpientes/terapia , Encuestas y Cuestionarios , Vietnam/epidemiología , Adulto Joven
19.
Biomed Res Int ; 2020: 5924856, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32420353

RESUMEN

Essential oils were extracted from the culm and leaf of Cymbopogon citratus collected from different regions of Vietnam and analyzed using GC/MS. The results showed that citral is the major component accounting for 61.20%-76.46% of the essential oils. The citral content was higher in the essential oil obtained from the leaf than in that from the culm of lemongrass in all regions. In particular, camphene, valerianol, and epi-α-muurolol can be used to differentiate essential oils originating from leaves versus culms. The cytotoxic effects of the essential oils on various lung cancer cell lines were evaluated in the present study. All essential oils exhibited cytotoxicity in the tested cells. The Ha Loc leaf essential oil (HLL) exhibited the most potent effects on A549 and H1975 cells, with IC50 values of 1.73 ± 0.37 and 4.01 ± 0.30 µg/mL, respectively. The Hy Cuong leaf essential oil (HCL) showed the strongest effect on H1299 cells, with an IC50 value of 2.45 ± 0.21 µg/mL. The Kim Duc culm (KDC) essential oil exerted the strongest cytotoxic effects against H1650 cells, with an IC50 value of 4.86 ± 0.29 µg/mL. The HLL induced apoptosis and cycle arrest in A549 cells according to flow cytometric analysis and fluorescent nuclear staining assays. The western blot analysis indicated that HLL induced the apoptotic effect by altering the regulating proteins of the apoptosis process such as caspase-3, Bcl-2, and Bax. The data strongly suggested that the intrinsic pathway may play an important role in the apoptotic effects of HLL.


Asunto(s)
Apoptosis/efectos de los fármacos , Puntos de Control del Ciclo Celular/efectos de los fármacos , Cymbopogon/química , Aceites de Plantas , Terpenos , Células A549 , Antineoplásicos/química , Antineoplásicos/farmacología , Humanos , Aceites Volátiles/química , Aceites Volátiles/farmacología , Aceites de Plantas/química , Aceites de Plantas/farmacología , Terpenos/química , Terpenos/farmacología
20.
Nat Prod Res ; 34(9): 1276-1281, 2020 May.
Artículo en Inglés | MEDLINE | ID: mdl-30676065

RESUMEN

Using various chromatographic separations, three new acylated flavonoid glycosides, namely barringosides G-I (1-3), were isolated from the water-soluble extract of Barringtonia racemosa branches and leaves. The structure elucidation was performed by extensive analysis of the 1D and 2D NMR and HR-QTOF-MS data. Of the isolated compounds, barringoside I (3) showed moderate inhibitory effects on LPS-induced NO production in RAW264.7 cells with an IC50 of 52.48 ± 1.04 µM.


Asunto(s)
Barringtonia/química , Flavonoides/química , Flavonoides/farmacología , Acilación , Animales , Glicósidos/química , Glicósidos/farmacología , Lipopolisacáridos/química , Lipopolisacáridos/farmacología , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Ratones , Estructura Molecular , Óxido Nítrico/metabolismo , Extractos Vegetales/química , Hojas de la Planta/química , Células RAW 264.7
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