RESUMEN
Tripterygium glycosides liposome(TPGL) were prepared by thin film-dispersion method, which were optimized accor-ding to their morphological structures, average particle size and encapsulation rate. The measured particle size was(137.39±2.28) nm, and the encapsulation rate was 88.33%±1.82%. The mouse model of central nervous system inflammation was established by stereotaxic injection of lipopolysaccharide(LPS). TPGL and tripterygium glycosides(TPG) were administered intranasally for 21 days. The effects of intranasal administration of TPG and TPGL on behavioral cognitive impairment of mice due to LPS-induced central ner-vous system inflammation were estimated by animal behavioral tests, hematoxylin-eosin(HE) staining of hippocampus, real-time quantitative polymerase chain reaction(RT-qPCR) and immunofluorescence. Compared with TPG, TPGL caused less damage to the nasal mucosa, olfactory bulb, liver and kidney of mice administered intranasally. The behavioral performance of treated mice was significantly improved in water maze, Y maze and nesting experiment. Neuronal cell damage was reduced, and the expression levels of inflammation and apoptosis related genes [tumor necrosis factor-α(TNF-α), interleukin-1ß(IL-1ß), BCL2-associated X(Bax), etc.] and glial activation markers [ionized calcium binding adaptor molecule 1(IBA1) and glial fibrillary acidic protein(GFAP)] were decreased. These results indicated that liposome technique combined with nasal delivery alleviated the toxic side effects of TPG, and also significantly ameliorated the cognitive impairment of mice induced by central nervous system inflammation.
Asunto(s)
Glicósidos Cardíacos , Disfunción Cognitiva , Ratones , Animales , Tripterygium , Liposomas , Glicósidos/uso terapéutico , Administración Intranasal , Lipopolisacáridos , Sistema Nervioso Central , Disfunción Cognitiva/tratamiento farmacológico , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Factor de Necrosis Tumoral alfa/metabolismoRESUMEN
Histone lysine-specific demethylase 1(LSD1) has become a promising molecular target for lung cancer therapy. Upon the screening platform for LSD1 activity, some Chinese herbal extracts were screened for LSD1 activity inhibition, and the underlying mechanism was preliminarily investigated at both molecular and cellular levels. The results of LSD1 inhibition showed that Puerariae Lobatae Radix extract can effectively reduce LSD1 expression to elevate the expression of H3 K4 me2 and H3 K9 me2 substrates in H1975 and H1299 cells. Furthermore, Puerariae Lobatae Radix was evaluated for its anti-lung cancer activity. It had a potent inhibitory ability against the proliferation and colony formation of both H1975 and H1299 cells. Flow cytometry and DAPI staining assays indicated that Puerariae Lobatae Radix can induce the apoptosis of lung cancer cells. In addition, it can significantly suppress the migration and reverse the epithelial-mesenchymal transition(EMT) process of lung cancer cells by activating E-cadherin and suppressing the expression of N-cadherin, slug and vimentin. To sum up, Puerariae Lobatae Radix displayed a robust inhibitory activity against lung cancer, and the mechanism may be related to the down-regulation of LSD1 expression to induce the cell apoptosis and suppress the cell migration and EMT process. These findings will provide new insights into the action of Puerariae Lobatae Radix as an anti-lung cancer agent and offer new ideas for the study on the anti-cancer action of Chinese medicine based on the epigenetic modification.
Asunto(s)
Neoplasias , Pueraria , Pueraria/química , Histona Demetilasas/genética , Histona Demetilasas/análisis , Raíces de Plantas/química , Transición Epitelial-MesenquimalRESUMEN
The present study was envisaged to investigate the chemical constituents and the intervention effects of Portulaca oleracea extract (POE) on acute alcoholic liver injury of rats. The chemical composition of POE was detected by high performance liquid chromatography (HPLC). Sixty male Wistar rats were divided into 6 groups: Normal control (NC) group, acute alcoholic liver injury model group (ALI), low, medium and high dose of POE (25, 50, 100 mg/kg) groups and bifendate (BF, 3.75 mg/kg) group. Each group was given by intragastrical administration for 7 days. Alcoholic liver injury was induced in the experimental model by administering 50% ethanol at 8 mL/kg and repeated administration after 6 h, for a period of 7 days. The results showed that pretreatment with POE significantly reduced the ethanol-elevated serum level of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP) and triglyceride (TG). The activities of superoxide dismutase (SOD) and glutathione peroxidase (GSH-PX) in liver were enhanced followed by administration of POE, while the content of nitric oxide (NO) and malondialdehyde (MDA) was found to decrease. Hepatic content of tumor necrosis factor-α (TNF-α), and interleukin-6 (IL-6) was also reduced by POE treatment. These results indicated that POE could increase the antioxidant capacity and relieve the inflammatory injury of the liver cells induced by ethanol. Meanwhile, in our study, POE reduced the expression of miR-122, acetyl coenzyme A carboxylase (ACC) 1 mRNA and protein and increased the expression of lipoprotein lipase (LPL) mRNA and protein in liver, which indicated that POE could improve the lipid metabolism disorder induced by ethanol. Our findings suggested that POE had protective effects on acute alcoholic liver injury of rats.
Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas/etiología , Enfermedad Hepática Inducida por Sustancias y Drogas/patología , Extractos Vegetales/farmacología , Portulaca/química , Animales , Biomarcadores , Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Enfermedad Hepática Inducida por Sustancias y Drogas/metabolismo , Cromatografía Líquida de Alta Presión , Citocinas/metabolismo , Regulación de la Expresión Génica/efectos de los fármacos , Mediadores de Inflamación/metabolismo , Metabolismo de los Lípidos/efectos de los fármacos , Hígado/efectos de los fármacos , Hígado/metabolismo , Hígado/patología , Pruebas de Función Hepática , MicroARNs/genética , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/química , ARN Mensajero/genética , ARN Mensajero/metabolismo , RatasRESUMEN
BACKGROUND: This study presents a case of rapidly developing respiratory failure due to antisynthetase syndrome (AS) following coronavirus disease 2019 (COVID-19) in a 33-year-old man diagnosed with Klinefelter syndrome (KS). CASE SUMMARY: A 33-year-old man with a diagnosis of KS was admitted to the Department of Pulmonary and Critical Care Medicine of a tertiary hospital in China for fever and shortness of breath 2 wk after the onset of COVID-19. Computed tomography of both lungs revealed diffuse multiple patchy heightened shadows in both lungs, accompanied by signs of partial bronchial inflation. Metagenomic next-generation sequencing of the bronchoalveolar lavage fluid suggested absence of pathogen. A biopsy specimen revealed organizing pneumonia with alveolar septal thickening. Additionally, extensive auto-antibody tests showed strong positivity for anti-SSA, anti-SSB, anti-Jo-1, and anti-Ro-52. Following multidisciplinary discussions, the patient received a final diagnosis of AS, leading to rapidly progressing respiratory failure. CONCLUSION: This study underscores the clinical progression of AS-associated interstitial lung disease subsequent to viral infections such as COVID-19 in patients diagnosed with KS.
RESUMEN
Taking Taihu Lake as the research object, for the aged polystyrene microplastics (PSMPs), the influence of hydraulic disturbance intensity on the migration process of PSMPs between mud and water phases was discussed, and the morphology and elements of PSMPs were analyzed using microscopic characterization methods including FTIR and SEM-EDS, as was done for characterization. The results showed that under disturbance conditions (55 r·min-1 and 120 r·min-1), the suspended solids (SS) and PSMPs in the overlying water were higher than those in the control experiment. This was due to the fact that the PSMPs were affected by buoyancy and reunited on the water surface under undisturbed conditions. Under low-intensity (55 r·min-1) disturbances, SS and PSMPs in the overlying water were (264.67±16.01) mg·L-1 and (239.67±6.51) n·mL-1, respectively, and (120 r·min-1) under high intensity. Under disturbance, the SS and PSMPs in the overlying water were (264.67±16.01) mg·L-1 and (239.67±6.51) n·mL-1, respectively. In the bottom mud, PSMPs were (491.00±23.46) mg·L-1 and 2.00 n·mL-1, respectively. Additionally, according to the SEM-EDS analysis, the surface of PSMPs had sediment elements (Si, etc.), which showed that it was easier to promote the adsorption of PSMPs by suspended solids under high strength. The abundance of PSMPs in the sediments also confirmed that the greater the intensity of the disturbance, the easier it was to promote the migration of PSMPs to the sediments.
Asunto(s)
Microplásticos , Contaminantes Químicos del Agua , China , Monitoreo del Ambiente , Sedimentos Geológicos , Lagos , Plásticos , Poliestirenos , Agua , Contaminantes Químicos del Agua/análisisRESUMEN
Objectives: Lysine-specific demethylase1 (LSD1), an important class of histone demethylases, plays a crucial role in regulation of mammalian biology. The up-regulated LSD1 expression was frequently associated with progress and oncogenesis of multiple human cancers, including non-small cell lung cancer (NSCLC). Therefore, inhibition of LSD1 may provide an attractive strategy for cancer treatment. We investigated the effect of sanguinarine against lung cancer cells as a natural alkaloid LSD1 inhibitor. Materials and Methods: The inhibition properties of sanguinarine to the recombinant LSD1 were evaluated by a fluorescence-based method. Subsequently, assays such as viability, apoptosis, clonogenicity, wound healing, and transwell were performed on H1299 and H1975 cells after treatment with sanguinarine. Results: Upon screening our in-house natural chemical library toward LSD1, we found that sanguinarine possessed a potent inhibitory effect against LSD1 with the IC50 value of 0.4 µM in a reversible manner. Molecular docking simulation suggested that sanguinarine may inactivate LSD1 by inserting into the binding pocket of LSD1 to compete with the FAD site. In H1299 and H1975 cells, sanguinarine inhibited the demethylation of LSD1, validating its cellular activity against the enzyme. Further studies showed that sanguinarine exhibited a strong capacity to suppress colony formation, inhibit migration and invasion, as well as induce apoptosis of H1299 and H1975 cells. Conclusion: Our findings present a new chemical scaffold for LSD1 inhibitors, and also provide new insight into the anti-NSCLC action of sanguinarine.
RESUMEN
The naphthalene fused ring of the title compound, C(12)H(4)Br(2)F(6)O(6)S(2), is slightly buckled (r.m.s. deviation = 0.036â Å) along the common C-C bond and the benzene rings are twisted by 3.2â (3)°. The two trifluoro-methyl-sulfonyl groups lie on opposite sides of the fused-ring system. The crystal structure features short inter-molecular Fâ¯F contacts [2.715â (4) and 2.832â (4)â Å].
RESUMEN
In the title compound, C(38)H(38)N(2)O(4), the 16 atoms comprising the four six-membered rings that are fused together are approximately coplanar (maximum r.m.s. deviation = 0.033â Å). The benzene rings at either ends are nearly perpendicular to the mean plane of the fused-ring system; one is aligned at 80.4â (1) ° and the other at 82.2â (1)°.
RESUMEN
In the title mol-ecule, [Fe(C(5)H(5))(C(7)H(6)BrO)], the C atoms of the substituted ring have disparate Fe-C bond lengths compared with the unsubstituted ring. In the bromo-acetyl residue, the Br and O atoms are co-planar [the O-C-C-Br torsion angle is 5.7â (4)°] and are syn to each other. Helical supra-molecular chains along the b axis are formed in the crystal structure mediated by C-Hâ¯O contacts; the carbonyl-O atom is bifurcated. The chains are linked into layers by C-Hâ¯π(unsubstituted ring) inter-actions that stack along the a-axis direction.
RESUMEN
The title mol-ecule, C(10)H(8)ClN(3)O(7), is twisted with the dihedral angle between the amide and benzene ring being 38.75â (11)°. The C-N-C-C torsion angle between the amide and acetyl groups is -150.1â (2)°. Finally, each nitro group is twisted out of the plane of the benzene ring to which it is connected [O-N-C-C torsion angles = 34.0â (3) and -64.5â (3)°]. Linear supra-molecular chains along [010] and mediated by N-Hâ¯O hydrogen bonds between successive amide groups dominate the crystal packing. The chains are consolidated into the three-dimensional structure by C-Hâ¯O contacts.
RESUMEN
In the title compound, C(11)H(14)N(4)O(4)·C(2)HCl(3)O(2), the dioxolane ring adopts an envelope conformation. Doxophylline [7-(1,3-dioxolan-2-yl-meth-yl)-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione] and trichloro-acetic acid mol-ecules are linked by O-Hâ¯N and C-Hâ¯O hydrogen bonds.
RESUMEN
The complete mitochondrial genome (mitogenome) of the Gymnocephalus cernua has been studied. The genome sequence was 16,614 bp in length, including the typical structure of 22 transfer RNA genes, 13 protein-coding genes, two ribosomal RNA genes, and the non-coding control region. The overall base composition of G. cernua mitogenome is 27.84% A, 27.60% T, 16.61% G, and 27.94% C, with a high A + T content of 55.45%. The complete mitochondrial genome of G. cernua provides basic genome data for relative studies on Perciformes.
Asunto(s)
ADN Mitocondrial/genética , Genoma Mitocondrial/genética , Perciformes/genética , Animales , ARN Ribosómico/genética , ARN de Transferencia/genéticaRESUMEN
Based on the super fluorescence quenching efficiency of graphene oxide and exonuclease III aided signal amplification, we develop a facile, sensitive, rapid and cost-effective method for DNA detection. In the presence of target DNA, the target-probe hybridization forms a double-stranded structure and exonuclease III catalyzes the stepwise removal of mononucleotides from the blunt 3' termini of probe, resulting in the recycling of the target DNA and signal amplification. Therefore, our proposed sensor exhibits a high sensitivity towards target DNA with a detection limit of 20 pM, which was even lower than previously reported GO-based DNA sensors without enzymatic amplification, and provides a universal sensing platform for sensitive detection of DNA.