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1.
Mar Drugs ; 22(6)2024 Jun 13.
Artigo em Inglês | MEDLINE | ID: mdl-38921586

RESUMO

Cyclic pentapeptide compounds have garnered much attention as a drug discovery resource. This study focused on the characterization and anti-benign prostatic hyperplasia (BPH) properties of avellanin A from Aspergillus fumigatus fungus in marine sediment samples collected in the Beibu Gulf of Guangxi Province in China. The antiproliferative effect and molecular mechanism of avellanin A were explored in testosterone propionate (TP)-induced RWPE-1 cells. The transcriptome results showed that avellanin A significantly blocked the ECM-receptor interaction and suppressed the downstream PI3K-Akt signalling pathway. Molecular docking revealed that avellanin A has a good affinity for the cathepsin L protein, which is involved in the terminal degradation of extracellular matrix components. Subsequently, qRT-PCR analysis revealed that the expression of the genes COL1A1, COL1A2, COL5A2, COL6A3, MMP2, MMP9, ITGA2, and ITGB3 was significantly downregulated after avellanin A intervention. The Western blot results also confirmed that it not only reduced ITGB3 and FAK/p-FAK protein expression but also inhibited PI3K/p-PI3K and Akt/p-Akt protein expression in the PI3K-Akt signalling pathway. Furthermore, avellanin A downregulated Cyclin D1 protein expression and upregulated Bax, p21WAF1/Cip1, and p53 proapoptotic protein expression in TP-induced RWPE-1 cells, leading to cell cycle arrest and inhibition of cell proliferation. The results of this study support the use of avellanin A as a potential new drug for the treatment of BPH.


Assuntos
Proliferação de Células , Fosfatidilinositol 3-Quinases , Proteínas Proto-Oncogênicas c-akt , Transdução de Sinais , Humanos , Proteínas Proto-Oncogênicas c-akt/metabolismo , Transdução de Sinais/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Fosfatidilinositol 3-Quinases/metabolismo , Simulação de Acoplamento Molecular , Linhagem Celular , Masculino , Apoptose/efeitos dos fármacos
2.
Chem Biodivers ; 21(4): e202301993, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38342755

RESUMO

A new alkaloids, aplysingoniopora A (1), and new configuration pregnane type steroid compound, 9,17-α-pregn-1,4,20-en-3-one (2), and two known pregnane type steroid compounds (3 and 4) were isolated from hydranth of Goniopora columna corals. The compounds structures and absolute configurations were determined by extensive spectroscopic analysis, MS data, single-crystal X-ray diffraction analysis and quantum chemical calculation. The anticancer effect of the compounds were explored in human non-small-cell lung cancer (NSCLC) A549 cell lines. As the results, the compound 3 and 4 induces toxicity and has proliferation inhibitory effects on A549 cells (IC50=58.99 µM and 58.77 µM, respectively) in vitro.


Assuntos
Alcaloides , Antozoários , Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , Animais , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Alcaloides/farmacologia , Alcaloides/química , Esteroides/farmacologia , Esteroides/química , Pregnanos/farmacologia , Estrutura Molecular
3.
Clin Kidney J ; 17(1): sfad027, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38186883

RESUMO

Objective: To explore the advantages of urinary matrix metalloproteinase-7 (MMP-7) in evaluating renal tubular injury in minimal change disease (MCD) and focal segmental glomerulosclerosis (FSGS) patients compared with urinary cystatin C (CysC) and retinol-binding protein (RBP). Methods: Serum and urine samples were collected from 20 healthy volunteers, and 40 MCD and 20 FSGS patients. Serum and urinary MMP-7 levels were measured by enzyme-linked immunosorbent assay. Urinary total protein, CysC and RBP levels were measured by automatic specific protein analyzer and compared with urinary creatinine level for calibration. The renal tissue serial sections were stained by MMP-7 immunohistochemistry and periodic acid-Schiff. Results: Under light microscopy, MMP-7 granular weak positive expression was showed sporadically in the cytoplasm of a few renal tubular epithelial cells without obvious morphological changes in MCD patients, and MMP-7-positive expression was observed in the cytoplasm of some renal tubular epithelial cells in FSGS patients. There was no significant difference in serum MMP-7 level among the three groups. Compared with the control group, the urinary MMP-7 level in MCD patients was higher, but urinary CysC and RBP levels were not increased significantly. Compared with the control group and MCD patients, urinary MMP-7, CysC and RBP levels in FSGS patients were upregulated significantly. Conclusions: Urinary MMP-7 could not only evaluate the mild renal tubular epithelial cells injury in MCD patients with massive proteinuria, but also evaluate the continuous renal tubular epithelial cells injury in FSGS patients.

4.
Acta Biomater ; 170: 344-359, 2023 10 15.
Artigo em Inglês | MEDLINE | ID: mdl-37607615

RESUMO

Poly(polyol sebacate) (PPS) polymer family has been recognized as promising biomaterials for biomedical applications with their characteristics of easy production, elasticity, biodegradation, and cytocompatibility. Poly(xylitol sebacate)-co-poly(ethylene glycol) (PXS-co-PEG) has been developed to fabricate PPS-based hydrogels; however, current PXS-co-PEG hydrogels presented limited properties and functions due to the limitations of the crosslinkers and crosslinking chemistry used in the hydrogel formation. Here, we fabricate a new type of PXS-co-PEG hydrogels through the use of multifunctional crosslinkers as well as dynamic bonds. In our design, polyethyleneimine-polydopamine (PEI-PDA) macromers are utilized to crosslink aldehyde-functionalized PXS-co-PEG (APP) through imine bonds and hydrogen bonds. PEI-PDA/APP hydrogels present multiple functional properties (e.g., fluorescent, elastomeric, biodegradable, self-healing, bioadhesive, antioxidant, and antibacterial behaviors). These properties of PEI-PDA/APP hydrogels can be fine-tuned by changing the PDA grafting degrees in the PEI-PDA crosslinkers. Most importantly, PEI-PDA/APP hydrogels are considered promising wound dressings to promote tissue remodeling and prevent bacterial infection in vivo. Taken together, PEI-PDA/APP hydrogels have been demonstrated as versatile biomaterials to provide multiple tailorable properties and desirable functions to expand the utility of PPS-based hydrogels for advanced biomedical applications. STATEMENT OF SIGNIFICANCE: Various strategies have been developed to fabricate poly(polyol sebacate) (PPS)-based hydrogels. However, current PPS-based hydrogels present limited properties and functions due to the limitations of the crosslinkers and crosslinking chemistry used in the hydrogel formation. This work describes that co-engineering crosslinkers and interfacial crosslinking is a promising approach to synthesizing a new type of poly(xylitol sebacate)-co-poly(ethylene glycol) (PXS-co-PEG) hydrogels as multifunctional hydrogels to expand the utility of PPS-based hydrogels for advanced biomedical applications. The fabricated hydrogels present multiple functional properties (e.g., fluorescent, biodegradable, elastomeric, self-healing, bioadhesive, antioxidative, and antibacterial), and these properties can be fine-tuned by the defined crosslinkers. The fabricated hydrogels are also used as promising wound dressing biomaterials to exhibit promoted tissue remodeling and prevent bacterial infection in vivo.


Assuntos
Infecções Bacterianas , Xilitol , Humanos , Polietilenoglicóis/química , Materiais Biocompatíveis/farmacologia , Materiais Biocompatíveis/química , Antioxidantes/farmacologia , Cicatrização , Hidrogéis/farmacologia , Hidrogéis/química , Polietilenoimina , Antibacterianos
5.
Fitoterapia ; 165: 105418, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-36587747

RESUMO

Fourteen new sulphur-containing amides, glycocramides A-N (1-14), as well as nine known analogues (15-23) were isolated and characterized from Glycosmis craibii Tanaka. The chemical structures of new sulphur-containing amides 1-14 were ambiguously elucidated by extensive spectroscopic methods, while the known compounds 15-23 were identified by the comparison of their experimental spectral data with those described data in the literatures. The antiproliferative effects of all isolated sulphur-containing amides were evaluated in vitro. As a result, part of sulphur-containing amides showed remarkable inhibitory effects against MGC-803 cell line with IC50 values ranging from 13.12 ± 0.10 to 20.03 ± 0.13 µM. These research results suggest that the sulphur-containing amides are potentially to be developed as a new natural anti-tumor drugs.


Assuntos
Amidas , Rutaceae , Amidas/farmacologia , Amidas/química , Estrutura Molecular , Enxofre , Extratos Vegetais/química , Rutaceae/química , Linhagem Celular Tumoral
6.
RSC Adv ; 12(49): 31943-31949, 2022 Nov 03.
Artigo em Inglês | MEDLINE | ID: mdl-36380958

RESUMO

In this study alginate-based microbubbles with a raspberry-like or core-shell-like morphology and with an average particle size of 553.6 ± 69.6 µm were synthesized; this was done through a novel procedure of transforming the structure with a 40 kHz ultrasonication which also stimulated the release of the components inside. Through the use of the electrospray technique in conjunction with agitation processes, components such as shikonin (SHK) and indocyanine green (ICG) were simultaneously encapsulated in alginate microbubbles to produce SHK-ICG alginate microbubbles; these microbubbles had half-maximal inhibitory concentrations of approximately 2.08 and 4.43 µM toward CP70 and SKOV3 ovarian cancer-cell lines, respectively, in an in vitro cell model. Moreover, these SHK-ICG alginate microbubbles enhanced brightness by 2.5 fold in ultrasound imaging relative to CaCl2 medium only. In conclusion, SHK-ICG alginate microbubbles have promise for use in theranostics.

7.
J Antibiot (Tokyo) ; 75(9): 526-529, 2022 09.
Artigo em Inglês | MEDLINE | ID: mdl-35918478

RESUMO

One new xanthene derivative, named penicixanthene E (1), together with one known compound 2, was isolated from the EtOAc extract of the endophytic fungus Penicillium sp. GXIMD 03101, which was identified from the mangrove Acanthus ilicifolius L. collected in the South China Sea. The structure of 1 was elucidated by 1D and 2D NMR spectral interpretation and HREISMS data. The absolute configurations of C-9 and C-11 in 1 were proposed based on electronic circular dichroism (ECD), but the configuration at C-3 in 1 was unassigned. Compound 1 represents a xanthene derivative that was first reported, in which carbon-carbon double bond has been reduced. The cytotoxic activities of all compounds were evaluated, the result showed that compound 1 has weak activity against pancreatic cancer SW1990.


Assuntos
Penicillium , Carbono , Dicroísmo Circular , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Penicillium/química , Xantenos/farmacologia
8.
Chemosphere ; 307(Pt 1): 135675, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-35842039

RESUMO

Phosphorus-accumulating organisms (PAOs), which harbor metabolic mechanisms for phosphorus removal, are widely applied in wastewater treatment. Recently, novel PAOs and phosphorus removal metabolic pathways have been identified and studied. Specifically, Dechloromonas and Tetrasphaera can remove phosphorus via the denitrifying phosphorus removal and fermentation phosphorus removal pathways, respectively. As the main PAOs in biological phosphorus removal systems, the conventional PAO Candidatus Accumulibacter and the novel PAOs Dechloromonas and Tetrasphaera are thoroughly discussed in this paper, with a specific focus on their phosphorus removal metabolic mechanisms, process applications, community abundance and influencing factors. Dechloromonas can achieve simultaneous nitrogen and phosphorus removal in an anoxic environment through the denitrifying phosphorus removal metabolic pathway, which can further reduce carbon source requirements and aeration energy consumption. The metabolic pathways of Tetrasphaera are diverse, with phosphorus removal occurring in conjunction with macromolecular organics degradation through anaerobic fermentation. A collaborative oxic phosphorus removal pathway between Tetrasphaera and Ca. Accumulibacter, or a collaborative anoxic denitrifying phosphorus removal pathway between Tetrasphaera and Dechloromonas are future development directions for biological phosphorus removal technologies, which can further reduce carbon source and energy consumption while achieving enhanced phosphorus removal.


Assuntos
Actinomycetales , Betaproteobacteria , Actinomycetales/metabolismo , Betaproteobacteria/metabolismo , Reatores Biológicos , Carbono , Nitrogênio , Fósforo/metabolismo , Polifosfatos/metabolismo , Esgotos
9.
J Mol Histol ; 53(3): 589-598, 2022 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-35661289

RESUMO

Interstitial cells of Cajal (ICCs) function as pacemaker cells in the gastrointestinal tract. Acute thoracic trauma is a common and lethal cause of death due to physical trauma caused by traffic accidents. This study aimed to explore the distribution of esophageal ICCs and distribution changes observed after acute thoracic trauma. Thirty rabbits were randomly divided into a control group and two study groups. The control group animals underwent an esophagectomy. All animals in the study groups underwent right chest puncture using the Hopkinson bar technique. The study groups were subjected to esophagectomy 24 and 72 h after chest puncture. Distribution, morphology, and density of esophageal ICCs were detected using transmission electron microscopy, toluidine blue staining, and immunohistochemistry. Apoptosis of esophageal ICCs was evaluated using the terminal deoxynucleotidyl transferase (TdT) dUTP Nick-End Labeling assay. Western blotting and reverse transcription polymerase chain reaction were used to detect changes in the SCF/c-kit signaling pathway. Esophageal ICCs distribution and SCF/c-kit signal pathway decreased from the upper part to the lower part in both physiological state and after thoracic trauma. In contrast, death of ICCs increased from the upper part to the lower part, both in physiological and injured state (P < 0.05). After thoracic trauma, increased ICCs and decreased death of ICCs in all parts of the esophagus (P < 0.05) were observed. The observed distribution and changes in esophageal ICCs would have an impact on motility and motility disorders of the esophagus.


Assuntos
Células Intersticiais de Cajal , Animais , Western Blotting , Esôfago/metabolismo , Imuno-Histoquímica , Células Intersticiais de Cajal/metabolismo , Proteínas Proto-Oncogênicas c-kit/metabolismo , Coelhos
10.
BMC Surg ; 22(1): 96, 2022 Mar 14.
Artigo em Inglês | MEDLINE | ID: mdl-35287657

RESUMO

BACKGROUND: From a biomechanical point of view, pedicle screws (PS) are better than other kinds of screws for implantation in the seventh cervical vertebra (C7). However, the application of PS is limited because of the high risk of severe complications. It is essential to define the optimal entry point and trajectory. The aim of this study was to comprehensively analyze the starting point and trajectory for C7 PS insertion using three dimensional (3D) models. METHODS: Overall, 60 subjects aged 18 to 67 years old were included. All CT images were used to construct 3D computer models of the C7 vertebrae. A new coordinate system was established for the next evaluation. The pedicle axis was calculated with respect to the entire pedicle; then, the ideal entry point, screw diameter and length, sagittal angle and lateral angle were assessed. RESULTS: All the ideal entry points were located at the medial superior to lateral notch (LN), and the mean distance between the entry point and LN was 5.86 ± 1.67 mm in the horizontal direction and 3.47 ± 1.57 mm in the vertical direction. The mean distance between the entry point and the middle point of the inferior edge of the C6 articular process (MP) was 0.74 ± 1.83 mm in the horizontal direction. The mean sagittal angle of the pedicle axis was 90.42°, and the mean pedicle transverse angle was 30.70°. The average diameter and length of the PS were 6.51 ± 0.76 mm and 31.58 ± 4.40 mm, respectively. CONCLUSIONS: This study provided a novel method to calculate the ideal starting point and trajectory for C7 PS insertion. These measurements may be helpful for preoperative planning. It is recommended that 3D CT imaging is used preoperatively to carefully evaluate the anatomy of each individual.


Assuntos
Parafusos Pediculares , Fusão Vertebral , Adolescente , Adulto , Idoso , Vértebras Cervicais/diagnóstico por imagem , Vértebras Cervicais/cirurgia , Simulação por Computador , Humanos , Pessoa de Meia-Idade , Fusão Vertebral/métodos , Tomografia Computadorizada por Raios X , Adulto Jovem
11.
Anim Biotechnol ; 33(5): 981-991, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-33325776

RESUMO

Circular RNA (circRNA) is a new non-coding RNA with a highly conserved and stable covalently closed loop structure, and it plays an important role in a variety of biological processes and the occurrence of diseases. Based on the sequencing results, circRNA_3079 had the most significant difference between the infected group and normal group, up to about 8 times. It has attracted our attention and was selected for further verification and analysis. Though the characteristics analysis of circRNA_3079 in chicken, we found circRNA_3079 is a stable, circular transcript, which mainly exists in the cytoplasm. And it is widely expressed in various tissues of chickens, and highly expressed in lung, spleen, lymph and bursa of fabricius. Bioinformatics analysis results showed that circRNA_3079 and the predicted target genes are enriched in many pathways related to immunity or tumors, such as p53 signaling pathway, Jak-STAT signaling pathway and NOD-like receptor signaling pathway, which revealed that circRNA_3079 may indirectly regulate the ALV-J infection process through the regulation of target genes.HIGHLIGHTSCircRNA_3079 is an abundant and stable circular RNA expressed in different tissues and cells in chicken.The circularization of circRNA_3079 does not depend on the reverse complementary repetitive sequence of the flanking sequence.CircRNA_3079 may indirectly regulate the ALV-J infection process.


Assuntos
Vírus da Leucose Aviária , Leucose Aviária , Animais , Leucose Aviária/genética , Vírus da Leucose Aviária/genética , Galinhas/genética , Proteínas NLR , RNA Circular/genética , RNA não Traduzido , Proteína Supressora de Tumor p53
12.
Polymers (Basel) ; 13(23)2021 Dec 03.
Artigo em Inglês | MEDLINE | ID: mdl-34883750

RESUMO

Cigarette smoking is a popular habit that has negative health consequences for populations. In this study, we developed a gallic acid-containing, gelatin-based nonwoven mat with photodegradation and photoindication functions. This could react with sidestream cigarette smoke and simultaneously inhibit the activity of the microbe growth in the air. The results of a fluorescence emission spectrum evidenced this photoindication function. Neither the nicotine nor gallic acid showed a redshift emission spectrum. However, the emission spectrum of the nonwoven mat exhibited the redshift and increased in intensity after absorbing the sidestream cigarette smoke. In this spectral evidence, the natural polymer played a key role in the photoindication function's display because it could dissolve the nicotine of the sidestream cigarette smoke and cause it to react with the gelatin structure. The high performance liquid chromatography-mass spectroscopy results indicated that the gallic acid and ultraviolet (UV) light enhanced the absorption of nicotine and nicotine-like derivatives, which were dissolved by the Tween 80 of nonwoven mat. The liquid paraffin and Tween 80 could oxidize, dehydrogenate, and demethylate the nicotine that was absorbed by the gelatin nonwoven mat. In conclusion, the nonwoven mat developed in this study provided the functions to filter the nicotine of sidestream smoke and activate the photoindication property by absorbing 365-nm UV light.

13.
AAPS PharmSciTech ; 23(1): 41, 2021 Dec 28.
Artigo em Inglês | MEDLINE | ID: mdl-34964079

RESUMO

Drugs are referred to as drug nanocrystals when they exist as nanoscale crystal structures. This kind of nanocarrier has been widely utilized to increase the solubility and absorption for poorly aqueous soluble drugs after oral administration, or prolong the drug circulation when intravenous administration. The systemic cytotoxicity caused by antitumor drugs usually come from the nonspecific drug distribution. To solve the disadvantage of poor targetability, drug nanocrystals for tumor targeted delivery have been developed in recent years. In this review, the targeting mechanisms of various surface modified drug nanocrystals are introduced with the focus on passive targeting, active targeting and stimuli-responsive targeting in details. Function and application of common surface modified materials are also discussed.


Assuntos
Nanopartículas , Neoplasias , Preparações Farmacêuticas , Sistemas de Liberação de Medicamentos , Humanos , Neoplasias/tratamento farmacológico , Solubilidade
14.
Pharmaceutics ; 13(9)2021 Aug 27.
Artigo em Inglês | MEDLINE | ID: mdl-34575423

RESUMO

Disulfiram is a drug used to support the treatment of chronic alcoholism. Recently, it has been found to have an off-label ability to inhibit the growth of ovarian cancer cells. However, the original formulation was designed for use via oral administration, which is not suitable to be given by a direct spray on the affected area. Therefore, in this study, we designed and prepared alginate (ALG) microparticles loaded with disulfiram and superparamagnetic iron oxide (cross-linking disulfiram/SPIO/ALG MPs), which have great potential application for inhibiting the growth of ovarian cancer simultaneously via two treatments, i.e., chemotherapy and hyperthermia. The drug-encapsulating alginate microparticles were prepared using an electrospray system and then cross-linked with calcium chloride ions. The particles were observed by optical microscopy and scanning electron microscopy, and found to be approximately 200 µm in diameter. The disc-shape morphology of the microparticles could be controlled by up to 95%. The drug-encapsulation efficiency of the microparticles reached 98%, and the suppression of tumor growth for the free-form disulfiram-treated group and disulfiram/SPIO/ALG MPs-treated group were 48.2% and 55.9% of tumor volume reduction, respectively, compared with a cisplatin-treated group. A hyperthermic effect can be achieved by applying a magnetic field to oscillate SPIO. The results of this study showed that these cross-linking disulfiram/SPIO/ALG MPs are potential drug carriers for the treatment of ovarian cancer.

15.
Chin J Nat Med ; 19(3): 225-230, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33781456

RESUMO

The phytochemical investigation of the stems of Homalium stenophyllum afforded seven new phenolic glycosides (1-5 and 8-9) and two known compounds (6 and 7). Their structures were elucidated by comprehensive analyses of NMR spectroscopic, mass spectrometric data and chemical hydrolysis. Additionally, their anti-inflammatory activities against the NO production in LPS-induced macrophages were evaluated.


Assuntos
Glicosídeos , Fenóis , Salicaceae/química , Anti-Inflamatórios/farmacologia , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Macrófagos/efeitos dos fármacos , Estrutura Molecular , Fenóis/isolamento & purificação , Fenóis/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Caules de Planta/química
16.
Stem Cell Reports ; 15(1): 110-124, 2020 07 14.
Artigo em Inglês | MEDLINE | ID: mdl-32668219

RESUMO

Mesenchymal stem/stromal cells (MSCs) reside in the perivascular niche and modulate tissue/organ homeostasis; however, little is known about whether and how their localization and function are linked. Particularly, whether specific MSC subsets couple with and regulate specialized vessel subtypes is unclear. Here, we show that Gli1+ cells, which are a subpopulation of MSCs couple with and regulate a specialized form of vasculature. The specific capillaries, i.e., CD31hiEMCNhi type H vessels, are the preferable vascular subtype which Gli1+ cells are adjacent to in bone. Gli1+ cells are further identified to be phenotypically coupled with type H endothelium during bone growth and defect healing. Importantly, Gli1+ cell ablation inhibits type H vessel formation associated with suppressed bone generation and regeneration. Mechanistically, Gli1+ cells initiate angiogenesis through Gli and HIF-1α signaling. These findings suggest a morphological and functional framework of Gli1+ cells modulating coupled type H vasculature for tissue homeostasis and regenerative repair.


Assuntos
Capilares/citologia , Neovascularização Fisiológica , Proteína GLI1 em Dedos de Zinco/metabolismo , Animais , Desenvolvimento Ósseo , Osso e Ossos/irrigação sanguínea , Osso e Ossos/patologia , Endotélio/irrigação sanguínea , Deleção de Genes , Subunidade alfa do Fator 1 Induzível por Hipóxia/metabolismo , Camundongos Endogâmicos C57BL , Fenótipo , Transdução de Sinais , Cicatrização
17.
BMC Musculoskelet Disord ; 21(1): 392, 2020 Jun 22.
Artigo em Inglês | MEDLINE | ID: mdl-32571287

RESUMO

BACKGROUND: Butterfly vertebrae are a rare congenital vertebral anomaly. An overlap of this spinal anomaly with other diseases has been reported. However, to the authors' knowledge, the coexistence of butterfly vertebrae and spinal cord injury has not been reported in the literature. CASE PRESENTATION: A 42-year-old male was admitted to our emergency department after a motor vehicle accident. His complaint was back pain, and he was unable to move both lower limbs. Upon physical examination, the patient was not ambulatory. Sensory examination revealed the absence of sensation below the T12 level. The strength of the bilateral lower limbs was grade 0. The patient received a radiographic evaluation. The initial diagnosis was T11 fracture with complete paraplegia of the lower limbs. Magnetic resonance imaging (MRI) was then performed. Sagittal MRI demonstrated an isointense lesion on T1-weighted imaging and a high-signal spindle-like lesion on T2-weighted imaging of the spinal cord adjacent to the T11 vertebra. The fat-suppressed sequence also revealed hyperintensities of the cord. There was no evidence of acute injury of the T11 vertebral body except for cuneiform anterior wedging. The patient was ultimately diagnosed with complete paraplegia with a T11 butterfly vertebra. He underwent urgent posterior decompressive and fixation surgery from T10 to T12. His postoperative recovery was uneventful. CONCLUSIONS: The coexistence of a butterfly vertebra with spinal cord injury was reported for the first time. Although butterfly vertebrae may be incidentally detected, it is important to be familiar with their radiographic features to distinguish them from fractures.


Assuntos
Acidentes de Trânsito , Anormalidades Musculoesqueléticas/patologia , Paraplegia/etiologia , Traumatismos da Medula Espinal/diagnóstico , Vértebras Torácicas/anormalidades , Adulto , Dor nas Costas/etiologia , Dor nas Costas/patologia , Descompressão Cirúrgica , Fixação Interna de Fraturas , Humanos , Imageamento por Ressonância Magnética , Masculino , Anormalidades Musculoesqueléticas/diagnóstico por imagem , Traumatismos da Medula Espinal/patologia , Traumatismos da Medula Espinal/cirurgia , Vértebras Torácicas/diagnóstico por imagem , Tomografia Computadorizada por Raios X , Resultado do Tratamento
18.
Bioorg Med Chem Lett ; 30(13): 127210, 2020 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-32359853

RESUMO

A series of novel bisbenzofuran-imidazolium salts were designed and prepared. The in vitro antitumor activity of these derivatives was evaluated against a panel of human tumor cell lines (A549, HL-60, MCF-7, SMMC-7721 and SW480). Results demonstrated that 2-methyl-benzimidazole ring and substitution of the imidazolyl-3-position with a 4-methoxyphenacyl or 2-naphthylacyl substituent were important for promoting cytotoxic activity. Notably, compound 23 was found to be the most potent compound with IC50 values of 0.64-1.47 µM against five human tumor cell lines, and exhibited higher selectivity to MCF-7 and SW-480 cell lines with IC50 values 15.3-fold and 9.1-fold lower than DDP.


Assuntos
Antineoplásicos/farmacologia , Benzofuranos/farmacologia , Imidazóis/farmacologia , Antineoplásicos/síntese química , Benzofuranos/síntese química , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Imidazóis/síntese química , Estrutura Molecular , Relação Estrutura-Atividade
19.
Cell Prolif ; 53(5): e12810, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-32472648

RESUMO

OBJECTIVES: Gli1+ cells have received extensive attention in tissue homeostasis and injury mobilization. The aim of this study was to investigate whether Gli1+ cells respond to force and contribute to bone remodelling. MATERIALS AND METHODS: We established orthodontic tooth movement (OTM) model to assess the bone response for mechanical force. The transgenic mice were utilized to label and inhibit Gli1+ cells, respectively. Additionally, mice that conditional ablate Yes-associated protein (Yap) in Gli1+ cells were applied in the present study. The tooth movement and bone remodelling were analysed. RESULTS: We first found Gli1+ cells expressed in periodontal ligament (PDL). They were proliferated and differentiated into osteoblastic cells under tensile force. Next, both pharmacological and genetic Gli1 inhibition models were utilized to confirm that inhibition of Gli1+ cells led to arrest of bone remodelling. Furthermore, immunofluorescence staining identified classical mechanotransduction factor Yap expressed in Gli1+ cells and decreased after suppression of Gli1+ cells. Additionally, conditional ablation of Yap gene in Gli1+ cells inhibited the bone remodelling as well, suggesting Gli1+ cells are force-responsive cells. CONCLUSIONS: Our findings highlighted that Gli1+ cells in PDL directly respond to orthodontic force and further mediate bone remodelling, thus providing novel functional evidence in the mechanism of bone remodelling and first uncovering the mechanical responsive property of Gli1+ cells.


Assuntos
Remodelação Óssea/fisiologia , Osso e Ossos/metabolismo , Osso e Ossos/fisiologia , Proteína GLI1 em Dedos de Zinco/metabolismo , Animais , Diferenciação Celular/fisiologia , Mecanotransdução Celular/fisiologia , Camundongos , Camundongos Transgênicos , Osteoclastos/metabolismo , Osteoclastos/fisiologia , Ligamento Periodontal/metabolismo , Ligamento Periodontal/fisiologia , Estresse Mecânico , Técnicas de Movimentação Dentária/métodos
20.
Polymers (Basel) ; 12(2)2020 Feb 20.
Artigo em Inglês | MEDLINE | ID: mdl-32093199

RESUMO

Levamisole (LEVA) is used to treat worm infections, but it can also inhibit cancer cell growth by inhibiting the aldehyde dehydrogenase pathway. Therefore, here, we developed a drug carrier targeting CD133, a biomarker overexpressed in ovarian cancer cells. The particle structure and cytotoxicity of the prepared LEVA-containing particles-called LEVA/PVP/PMMA microparticles (MPs) (because it used matrix material polyvinylpyrrolidone (PVP) and poly(methylmethacrylate) (PMMA))-were investigated in the ovarian cancer cell lines SKOV-3 and CP70. The particle size of the MPs was determined to be 1.0-1.5 µm and to be monodispersed. The hydrophilic property of PVP created a porous MP surface after the MPs were soaked in water for 20 min, which aided the leaching of the hydrophilic LEVA out of the MPs. The encapsulation efficiency of LEVA/PVP/PMMA MPs could reach up to 20%. Free-form LEVA released 50% of drugs in <1 h and 90% of drugs in 1 day, whereas the drug release rate of LEVA/PVP/PMMA MPs was much slower; 50% released in 4 h and only 70% of drugs released in 1 day. In the in vitro cell model test, 5 mM free-form LEVA and 0.1 g/mL CD133 targeted LEVA/PVP/PMMA MPs reduced SKOV-3 cell viability by 60%; 0.1 g/mL LEVA/PVP/PMMA MPs was equivalent to a similar dosage of the free drug. In addition, the cytotoxicity of CD133-conjugated LEVA/PVP/PMMA MPs shows a different cytotoxicity response toward cell lines. For SKOV-3 cells, treatment with free-form LEVA or CD133-conjugated LEVA/PVP/PMMA MPs exerted dose-dependent cytotoxic effects on SKOV-3 cell viability. However, CD133-conjugated LEVA/PVP/PMMA MPs demonstrated no significant dose-dependent cytotoxic efficacy toward CP70 cells.

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