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1.
Fitoterapia ; 175: 105938, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38565379

RESUMO

Five new B-seco-limonoids, namely toonanoronoids A-E (1-5), in conjunction with three previously reported compounds, were isolated from the EtOAc extract of the twigs and leaves of Toona ciliata var. yunnanensis. Their structures were elucidated through comprehensive spectroscopic and X-ray crystallographic analysis. The cytotoxic activities of new compounds against five human tumor cell lines (HL-60, SMMC-7721, A549, MCF-7, and SW480) were screened, Compounds 4 and 5 exerted inhibition toward two tumor cell lines (HL-60, SW-480) with IC50 values between 1.7 and 5.9 µM.


Assuntos
Antineoplásicos Fitogênicos , Limoninas , Compostos Fitoquímicos , Folhas de Planta , Toona , Humanos , Estrutura Molecular , Linhagem Celular Tumoral , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Folhas de Planta/química , Limoninas/isolamento & purificação , Limoninas/farmacologia , Limoninas/química , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , China , Toona/química , Caules de Planta/química
2.
Int J Biol Macromol ; 263(Pt 2): 130320, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38412933

RESUMO

Angelica gigas (A. gigas) is traditional medicinal herb that mainly exists in Korea and northeastern China. There have been relatively few studies conducted thus far on its polysaccharides and their bioactivities. We purified and described a novel water-soluble polysaccharide derived from A. gigas and investigated its immunoenhancing properties. The basic components of crude and purified polysaccharides (F1 and F2) were total sugar (41.07% - 70.55%), protein (1.12-10.33%), sulfate (2.9-5.5%), and uronic acids (0.5-31.05%) in total content. Our results demonstrated that the crude and fractions' molecular weights (Mw) varied from 42.2 to 285.2 × 103 g/mol. As the most effective polysaccharide, F2 significantly stimulated RAW264.7 cells to release nitric oxide (NO) and express several cytokines. Furthermore, F2 increased the expression of tumor necrosis factor-α (TNF-α), interferon-gamma (IFN-É£), natural killer cytotoxicity receptors (NKp44), and granzyme-B in NK-92 cells and enhanced the cytotoxicity against HCT-116 cells. In our experiments, we found that F2 stimulated RAW264.7 cells and NK-92 cells via MAPK and NF-κB pathways. The monosaccharide and methylation analysis of the high immunostimulant F2 polysaccharide findings revealed that the polysaccharide was primarily composed of 1 â†’ 4, 1 â†’ 6, 1 â†’ 3, 6, 1 â†’ 3 and 1 â†’ 3, 4, 6 galactopyranose residues, 1 â†’ 3 arabinofuranose residues, 1 â†’ 4 glucopyranose residues. These results demonstrated that the F2 polysaccharide of A. gigas which possesses potential immunostimulatory attributes, could be used to create a novel functional food.


Assuntos
Angelica , NF-kappa B , Animais , Camundongos , Humanos , NF-kappa B/metabolismo , Células HCT116 , Ativação de Macrófagos , Células RAW 264.7 , Transdução de Sinais , Células Matadoras Naturais/metabolismo , Polissacarídeos/química
3.
Bioorg Chem ; 144: 107174, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38320369

RESUMO

Ursonic acid (UNA) is a natural pentacyclic triterpene found in some medicinal plants and foods. The reproductive protective effect of UNA was evaluated in a mouse model of oligozoospermia induced by busulfan (BUS) at 30 mg/kg b.w.. The mice were initially divided into groups with UNA concentrations of 10, 30, 50, 100 mg/kg. Subsequently, based on sperm parameters, the optimal concentration of 50 mg/kg was identified. As a control, an additional group was supplemented with ursolic acid at a concentration of 50 mg/kg. The results indicated that BUS caused the loss of spermatogenic cells in testis, the decrease of sperm in epididymis, the disorder of testicular cytoskeleton, the decrease of serum sex hormones such as testosterone which induced an increase in feedback of androgen receptor and other testosterone-related proteins, the increase of malondialdehyde and reactive oxygen species levels and the increase of ferroptosis in testis while UNA successfully reversed these injuries. High-throughput sequencing revealed that UNA administration significantly upregulated the expression of genes associated with spermatogenesis, such as Tnp1, Tnp2, Prm1, among others. These proteins are crucial in the histone to protamine transition during sperm chromatin remodeling. Network pharmacology analysis reveals a close association between UNA and proteins related to the transformation of histones to protamine. Molecular docking studies reveal that UNA can interact with the ferroptosis-inhibiting gene SLC7A11, thereby modulating ferroptosis. Taken together, UNA alleviated BUS-induced oligozoospermia by regulating hormone secretion, mitigating oxidative stress and promoting recovery of spermatogenesis by inhibiting the ferroptosis.


Assuntos
Ferroptose , Oligospermia , Triterpenos , Humanos , Masculino , Camundongos , Animais , Oligospermia/induzido quimicamente , Oligospermia/tratamento farmacológico , Simulação de Acoplamento Molecular , Sêmen/metabolismo , Espermatogênese/fisiologia , Testosterona/farmacologia , Histonas/farmacologia , Protaminas/genética , Protaminas/metabolismo , Protaminas/farmacologia
4.
Medicine (Baltimore) ; 102(43): e35744, 2023 Oct 27.
Artigo em Inglês | MEDLINE | ID: mdl-37904349

RESUMO

BACKGROUND: The objectives of the researchers are as follows: First, to investigate whether intraoperative or postoperative administration of Intravenous (IV) iron supplements in patients undergoing primary total knee arthroplasty (TKA) can contribute to the hemoglobin recovery during the postoperative period (between 4 and 8 weeks after surgery). Second, to examine whether the administration of IV iron supplements during or immediately after TKA in patients undergoing primary TKA can reduce the need for allogenic blood transfusion during hospitalization. METHODS: Articles published between January 1, 1990, and June 30, 2023 were searched in PubMed, Cochrane, and Embase. The population, intervention, comparison, and outcome of this study are as follows; Population: Patients undergoing primary total knee arthroplasty; Intervention: Administration of IV iron supplements during or immediately after surgery; Comparison: Non-administration of IV iron supplements; Outcome: Degree of hemoglobin recovery (between 4 and 8 weeks after surgery) and the need for blood transfusion during hospitalization. RESULTS: There was a statistically significant difference in the amount of change in hemoglobin between iron supplementation group and non-iron supplementation group. The effect size were -0.44 (95% confidence interval: -0.69 to -0.19, P value < .001) in all patients. This means that the amount of change in hemoglobin were significantly reduced in the iron supplementation group than in the non-iron supplementation group. There was a statistically significant difference for post-operative transfusion rate between 2 groups. The effect size were 0.28 (95% confidence interval: 0.10-0.81, P value = .02) in all patients. This means that the post-operative transfusion rate was significantly less in the iron supplementation group than in the non-iron supplementation group. CONCLUSION: The administration of IV iron supplements during or after TKA surgery increases hemoglobin recovery between 4 and 8 weeks after surgery and reduces the need for allogeneic blood transfusion during hospitalization.


Assuntos
Antifibrinolíticos , Artroplastia do Joelho , Ácido Tranexâmico , Humanos , Ferro/uso terapêutico , Artroplastia do Joelho/efeitos adversos , Hemoglobinas/análise , Administração Intravenosa , Período Pós-Operatório , Suplementos Nutricionais , Perda Sanguínea Cirúrgica
5.
Br J Radiol ; 96(1152): 20230503, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37750830

RESUMO

OBJECTIVE: To test the performance of the National Comprehensive Cancer Network (NCCN) CT resectability criteria for predicting the surgical margin status of pancreatic neuroendocrine tumor (PNET) and to identify factors associated with margin-positive resection. METHODS: Eighty patients with pre-operative CT and upfront surgery were retrospectively enrolled. Two radiologists assessed the CT resectability (resectable [R], borderline resectable [BR], unresectable [UR]) of the PNET according to NCCN criteria. Logistic regression was used to identify factors associated with resection margin status. κ statistics were used to evaluate interreader agreements. Kaplan-Meier method with log-rank test was used to estimate and compare recurrence-free survival (RFS). RESULTS: Forty-five patients (56.2%) received R0 resection and 35 (43.8%) received R1 or R2 resection. R0 resection rates were 63.6-64.2%, 20.0-33.3%, and 0% for R, BR, and UR diseases, respectively (all p ≤ 0.002), with a good interreader agreement (κ, 0.74). Tumor size (<2 cm, 2-4 cm, and >4 cm; odds ratio (OR), 9.042-18.110; all p ≤ 0.007) and NCCN BR/UR diseases (OR, 5.918; p = 0.032) were predictors for R1 or R2 resection. The R0 resection rate was 91.7% for R disease <2 cm and decreased for larger R disease. R0 resection and smaller tumor size in R disease improved RFS. CONCLUSION: NCCN resectability criteria can stratify patients with PNET into distinct groups of R0 resectability. Adding tumor size to R disease substantially improves the prediction of R0 resection, especially for PNETs <2 cm. ADVANCES IN KNOWLEDGE: Tumor size and radiologic resectability independently predicted margin status of PNETs.


Assuntos
Tumores Neuroectodérmicos Primitivos , Tumores Neuroendócrinos , Neoplasias Pancreáticas , Humanos , Margens de Excisão , Estudos Retrospectivos , Tumores Neuroendócrinos/diagnóstico por imagem , Tumores Neuroendócrinos/cirurgia , Neoplasias Pancreáticas/diagnóstico por imagem , Neoplasias Pancreáticas/cirurgia , Neoplasias Pancreáticas/patologia , Tomografia Computadorizada por Raios X/métodos , Terapia Neoadjuvante
6.
Int J Mol Sci ; 24(14)2023 Jul 22.
Artigo em Inglês | MEDLINE | ID: mdl-37511556

RESUMO

The removal of nitrogen from coal tar pitch (CTP) through the hydrodenitrogenation (HDN) of CTP and its molecular behavior were evaluated in the presence of NiMo/γ-alumina and CoMo/γ-alumina catalysts. Fourier transform ion cyclotron resonance mass spectrometry with atmospheric pressure photoionization was used to analyze the complicated chemical classes and species of CTP and the treated products at the molecular level. Nitrogen species were qualitatively analyzed before and after hydrotreatment. A single-stage hydrotreatment with an HDN catalyst resulted in a high sulfur removal performance (85.6-94.7%) but a low nitrogen removal performance (26.8-29.2%). Based on relative abundance analyses of nitrogen and binary nitrogen species, CcHh-NnSs was the most challenging species to remove during HDN treatment. Furthermore, prior hydrodesulfurization was combined with HDN treatment, and the dual hydrotreatments yielded a significantly improved nitrogen removal performance (46.4-48.7%).


Assuntos
Alcatrão , Nitrogênio/química , Óxido de Alumínio , Desnitrificação , Espectrometria de Massas/métodos
7.
J Inflamm Res ; 16: 1671-1691, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37092134

RESUMO

Autophagy is a highly conserved process that maintains cell stability in eukaryotes, participates in the turnover of intracellular substances to maintain cell function, helps to resist pathogen invasion, and improves cell tolerance to environmental changes. Autophagy has been observed in many diseases, and the symptoms of these diseases are significantly improved by regulating autophagy. Autophagy is also involved in the development of lung diseases. Studies have shown that autophagy may play a beneficial or harmful role in acute lung injury (ALI), and ALI has been treated with traditional Chinese medicine designed to promote or inhibit autophagy. In this paper, the molecular mechanism and common pathways regulating autophagy and the relationship between autophagy and ALI are introduced, and the active ingredients of traditional Chinese medicine that improve ALI symptoms by regulating autophagy are summarized.

8.
J Ethnopharmacol ; 309: 116341, 2023 Jun 12.
Artigo em Inglês | MEDLINE | ID: mdl-36889418

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The fruit of Kadsura coccinea (Lem.) A. C. Smith is an ethnomedicine used to treat abnormal menstruation, menopausal syndrome, and female infertility among the Dong Nationality in China. AIM OF THE STUDY: Our study aimed to identify the volatile oil profiles of the K. coccinea fruit and elucidate their estrogenic activity. MATERIALS AND METHODS: The peel volatile oil (PeO), pulp volatile oil (PuO), and seed volatile oil (SeO) of K. coccinea were extracted using hydrodistillation and qualitatively analyzed using gas chromatography-mass spectrometry (GC-MS). Estrogenic activity was evaluated in vitro using cell assay and in vivo using immature female rats. Serum 17ß-Estradiol (E2) and follicle-stimulating hormone (FSH) levels were detected using ELISA. RESULTS: In total, 46 PeO, 27 PuO, and 42 SeO components representing 89.96%, 90.19%, and 97% of the total composition, respectively, were identified. The compounds with the highest content in PeO, PuO, and SeO were ß-caryophyllene, γ-amorphene, and n-hexadecanoic acid, respectively. PeO induced proliferation of MCF-7 cells with an EC50 of 7.40 µg/mL. Subcutaneous administration of 10 mg/kg PeO significantly increased the weight of the uteri in immature female rats, with no effect on serum E2 and FSH levels. PeO acted as an agonist of ERα and ERß. PuO and SeO showed no estrogenic activity. CONCLUSION: The chemical compositions of PeO, PuO, and SeO of K. coccinea are different. PeO is the main effective fraction for estrogenic activities, providing a new source of phytoestrogen for the treatment of menopausal symptoms.


Assuntos
Kadsura , Óleos Voláteis , Feminino , Ratos , Animais , Frutas , Kadsura/química , Fitoestrógenos/farmacologia , Estrona , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Hormônio Foliculoestimulante
9.
Biomass Convers Biorefin ; : 1-15, 2023 Feb 08.
Artigo em Inglês | MEDLINE | ID: mdl-36785542

RESUMO

A deep eutectic solvent (choline chloride (ChCl)-urea) was chosen to extract flavonoids from Moringa oleifera leaves (FMOL), the condition of extraction was tailor-made, under the optimal extraction conditions (material-to-liquid ratio of 1:60 g/mL, extraction time of 80 min, extraction temperature of 80 °C), the highest extraction efficiency reached 63.2 ± 0.3 mg R/g DW, and nine flavonoids were identified. Then, the biological activities including antioxidant activities, antibacterial activities, and anti-tumor activities were systematically studied. FMOL was superior to positive drugs in terms of antioxidant activity. As to DPPH investigation, the IC50 of FMOL and Vc were 64.1 ± 0.7 and 176.1 ± 2.0 µg/mL; for the ABTS, the IC50 of FMOL and Vc were 9.5 ± 0.3 and 38.2 ± 1.2 µg/mL, the FRAP value of FMOL and Vc were 15.5 ± 0.6 and 10.2 ± 0.4 mg TE/g, and ORAC value of FMOL and Vc were 4687.2 ± 102.8 and 3881.6 ± 98.6 µmol TE/g. The bacteriostatic (MICs were ≤ 1.25 mg/mL) activities of FMOL were much better than propyl p-hydroxybenzoate. Meanwhile, FMOL had comparable inhibitory activity with genistein on tumor cells, IC50 was 307.8 µg/mL, and could effectively induce apoptosis in HCT116. Microcapsules were prepared with xylose-modified soybean protein isolate and gelatin as wall materials; after that, the intestinal release of modified FMOL microcapsules was 86 times of free FMOL. Therefore, this study confirmed that FMOL extracted with ChCl/urea has rich bioactive components, and microencapsulated FMOL has potential application in food industry. Supplementary Information: The online version contains supplementary material available at 10.1007/s13399-023-03877-8.

10.
Int Orthop ; 47(1): 175-186, 2023 01.
Artigo em Inglês | MEDLINE | ID: mdl-36401020

RESUMO

PURPOSE: This study aimed to evaluate the infection control rate of palliative arthroscopic debridement, antibiotics, and implant retention (DAIR) for the high mortality risk or terminal cancer stage patients. METHODS: From March 2018 to August 2021, 21 patients met the following inclusion criteria: old age of more than 80, diagnosed as a terminal stage of cancer, high risk of mortality and morbidity representing as Charlson comorbidity index (CCI) ≥ 5, low daily activity with disabled extremity, and re-infection after two-stage revision. Each patient underwent arthroscopic DAIR and additional continuous irrigation for 48 hours. The need for subsequent re-arthroscopic DAIR or two-stage revision was determined by the post-operative trends of C-reactive protein (CRP) levels. Infection control was defined as continuing controlled status of infection based on clinical and laboratory results by one or two times of arthroscopic DAIR within initial two months. Treatment failure was defined as more than three times arthroscopic debridement, two-stage revision surgery, or expired due to uncontrolled infection. RESULTS: Arthroscopic DAIR controlled the infection in 19 (90.5%) of the 21 cases. The other knee underwent a total of three times of re-arthroscopic DAIR and the other one underwent two-stage revision. Although five patients expired during the follow-up period due to worsening medical problems or terminal cancer, there were no deaths from uncontrolled infection, sepsis, or surgery-related complications. CONCLUSIONS: Arthroscopic debridement with continuous irrigation for the infection TKA with high mortality risk or terminal cancer patients showed a 90.5% infection control rate. For high-risk patients, arthroscopic debridement with continuous irrigation can be an alternative treatment to improve the quality of life during survival.


Assuntos
Artroplastia do Joelho , Infecções Relacionadas à Prótese , Humanos , Artroplastia do Joelho/efeitos adversos , Desbridamento/efeitos adversos , Desbridamento/métodos , Qualidade de Vida , Estudos Retrospectivos , Resultado do Tratamento , Antibacterianos/uso terapêutico , Infecções Relacionadas à Prótese/epidemiologia , Infecções Relacionadas à Prótese/cirurgia , Infecções Relacionadas à Prótese/diagnóstico
11.
Environ Res ; 212(Pt C): 113448, 2022 09.
Artigo em Inglês | MEDLINE | ID: mdl-35580664

RESUMO

Alum sludge from water treatment was calcined and extracted to synthesize high quality boehmite and γ-alumina for phosphate removal. Synthesized boehmite and γ-alumina were able to remove phosphate quickly and effectively. Boehmite (hydrothermal treatment at 60 °C) showed maximum phosphate removal (adsorption) of 61 mg P/g followed by γ-alumina (50 mg P/g) and the boehmite hydrothermally treated at 120 °C (41 mg P/g). The degree of crystallinity gave more effect on phosphate adsorption of boehmite than that of γ-alumina. The lower the pH, the more phosphate adsorbed on the boehmite and γ-alumina (adsorb phosphate more than 4 times at pH 3 than at pH 11). Spectroscopic analysis (SEM-EDS and FTIR) indicates that phosphate are removed by ligand exchange, electrostatic attraction, and surface precipitation on the synthesized boehmite and γ-alumina.


Assuntos
Fósforo , Esgotos , Adsorção , Hidróxido de Alumínio , Óxido de Alumínio/química , Fosfatos , Fósforo/química
12.
Radiology ; 301(1): 81-90, 2021 10.
Artigo em Inglês | MEDLINE | ID: mdl-34282972

RESUMO

Background The Coronary Artery Disease Reporting and Data System (CAD-RADS) was established in 2016 to standardize the reporting of coronary artery disease at coronary CT angiography (CCTA). Purpose To assess the prognostic value of CAD-RADS at CCTA for major adverse cardiovascular events (MACEs) in patients presenting to the emergency department with chest pain. Materials and Methods This multicenter retrospective observational cohort study was conducted at four qualifying university teaching hospitals. Patients presenting to the emergency department with acute chest pain underwent CCTA between January 2010 and December 2017. Multivariable Cox regression analysis was used to evaluate risk factors for MACEs, including clinical factors, coronary artery calcium score (CACS), and CAD-RADS categories. The prognostic value compared with clinical risk factors and CACS was also assessed. Results A total of 1492 patients were evaluated (mean age, 58 years ± 14 years [standard deviation]; 759 men). During a median follow-up period of 31.5 months, 103 of the 1492 patients (7%) experienced MACEs. Multivariable Cox regression analysis showed that a moderate to severe CACS was associated with MACEs after adjusting for clinical risk factors (hazard ratio [HR] range, 2.3-4.4; P value range, <.001 to <.01). CAD-RADS categories from 3 to 4 or 5 (HR range, 3.2-8.5; P < .001) and high-risk plaques (HR = 3.6, P < .001) were also associated with MACEs. The C statistics revealed that the CAD-RADS score improved risk stratification more than that using clinical risk factors alone or combined with CACS (C-index, 0.85 vs 0.63 [P < .001] and 0.76 [P < .01], respectively). Conclusion The Coronary Artery Disease Reporting and Data System classification had an incremental prognostic value compared with the coronary artery calcium score in the prediction of major adverse cardiovascular events in patients presenting to the emergency department with acute chest pain. © RSNA, 2021 Online supplemental material is available for this article. See also the editorial by Vliegenthart in this issue.


Assuntos
Dor no Peito/complicações , Angiografia por Tomografia Computadorizada/métodos , Sistemas de Informação em Radiologia , Calcificação Vascular/complicações , Calcificação Vascular/diagnóstico por imagem , Doença Aguda , Estudos de Coortes , Vasos Coronários/diagnóstico por imagem , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Estudos Retrospectivos , Medição de Risco
13.
Environ Sci Pollut Res Int ; 28(36): 49602-49612, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-33939095

RESUMO

Phytoextraction is widely used to remove environmental pollutants such as heavy metals or radionuclides from soil. It is important to understand how to enhance the accumulation of contaminants by plants. Previously, we found that Napier grass (Pennisetum purpureum Schum.) has the potential to effectively remove Cs (133Cs and 137Cs). In order to enhance the remediation efficiency of Napier grass, we evaluated the effects of low-level K (K), ethylenediaminetetraacetic acid (EDTA), or the combination of low-level K and EDTA (K+EDTA). We also examined the differences in 137Cs decontamination between two cropping years (2018 and 2019). Overall, there were no prominent effects from the K, EDTA, or K+EDTA treatments on plant growth (plant height, tiller number), aboveground biomass, 137Cs concentration, and 137Cs removal ratio (CR) in 2 years. However, the aboveground biomass (P < 0.001), 137Cs concentration (P < 0.001 in 2019 only), and CR (P < 0.001) in plants grown in the first growing period were significantly higher than in plants grown in the second growing period in both years. The mean 137Cs concentration (P < 0.001) and total CR (P < 0.001) per year was significantly greater in 2019 than in 2018. The precipitation amount during the cultivation period in 2019 (1197 mm) was 1.8-fold higher than in 2018 (655 mm). In this study, the K, EDTA, and K+EDTA treatments had less effect plant growth than the natural environmental conditions. To enhance remediation efficiency, soil moisture is one important factor to produce more aboveground biomass to achieve high CR in Napier grass.


Assuntos
Pennisetum , Poluentes do Solo , Biodegradação Ambiental , Descontaminação , Ácido Edético , Potássio , Solo , Poluentes do Solo/análise
14.
Int J Mol Sci ; 22(4)2021 Feb 20.
Artigo em Inglês | MEDLINE | ID: mdl-33672769

RESUMO

Traditional endocrine therapy for prostate cancer (PCa) has been directed at suppression of the androgen receptor (AR) signaling axis since Huggins et al. discovered that diethylstilbestrol (DES; an estrogen) produced chemical castration and PCa tumor regression. Androgen deprivation therapy (ADT) still remains the first-line PCa therapy. Insufficiency of ADT over time leads to castration-resistant PCa (CRPC) in which the AR axis is still active, despite castrate levels of circulating androgens. Despite the approval and use of multiple generations of competitive AR antagonists (antiandrogens), antiandrogen resistance emerges rapidly in CRPC due to several mechanisms, mostly converging in the AR axis. Recent evidence from multiple groups have defined noncompetitive or noncanonical direct binding sites on AR that can be targeted to inhibit the AR axis. This review discusses new developments in the PCa treatment paradigm that includes the next-generation molecules to noncanonical sites, proteolysis targeting chimera (PROTAC), or noncanonical N-terminal domain (NTD)-binding of selective AR degraders (SARDs). A few lead compounds targeting each of these novel noncanonical sites or with SARD activity are discussed. Many of these ligands are still in preclinical development, and a few early clinical leads have emerged, but successful late-stage clinical data are still lacking. The breadth and diversity of targets provide hope that optimized noncanonical inhibitors and/or SARDs will be able to overcome antiandrogen-resistant CRPC.


Assuntos
Antagonistas de Receptores de Andrógenos/uso terapêutico , Terapia de Alvo Molecular , Neoplasias da Próstata/tratamento farmacológico , Receptores Androgênicos/metabolismo , Antagonistas de Receptores de Andrógenos/química , Antagonistas de Receptores de Andrógenos/farmacologia , Animais , Avaliação Pré-Clínica de Medicamentos , Humanos , Masculino , Proteólise/efeitos dos fármacos
15.
Biomed Res Int ; 2021: 6890679, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33604384

RESUMO

MATERIALS AND METHODS: Mice were divided into four groups: normal, untreated, low- (2 mg), and high-dose (8 mg) beluga lentil treatment groups. Beluga lentil was orally administered for 2 weeks, followed by bilateral renal ischemia for 20 min and reperfusion for 30 min. Blood samples and kidney tissues were collected and analyzed to investigate renal function, histopathology, epithelial and endothelial cell damage, apoptosis, oxidative stress, and inflammatory responses. RESULTS: The pretreated groups maintained renal function, with significantly lower blood urea nitrogen (BUN) and creatinine levels, compared with the other groups. The histopathological analysis showed reduced proximal tubule injury and decreased injury-related molecule (kidney injury molecule 1 (KIM-1) and neutrophil gelatinase-associated lipocalin (NGAL)) secretion in the pretreated groups compared with the other groups. Terminal deoxynucleotidyl transferase dUTP nick-end labeling- (TUNEL-) positive cells and the secretion of apoptosis-related molecules (Fas and caspase 3) were significantly reduced in the pretreated groups compared with the other groups. The pretreated groups showed positive microvessel-associated gene (cluster of differentiation (CD31)) expression and negative adhesion molecule (intracellular adhesion molecule 1 (ICAM-1)) expression. An antioxidant effect was observed in the pretreatment groups, with reduced malonaldehyde (MDA) expression and increased antioxidant enzyme (superoxide dismutase (SOD), catalase (CAT), glutathione (GSH), and glutathione peroxidase (GPx)) secretion. In the pretreated groups, F4/80+ macrophages and CD4+ T cell infiltration were inhibited and proinflammatory cytokine (interleukin- (IL-) 1ß, IL-6, and tumor necrosis factor- (TNF-) α) levels decreased; however, the levels of anti-inflammatory cytokines (transforming growth factor- (TGF-) ß, IL-10, and IL-22) increased. CONCLUSIONS: Beluga lentil pretreatment demonstrated protective effects against I/R-induced renal damage, via antiapoptotic, anti-inflammatory, and antioxidant activities.


Assuntos
Rim/efeitos dos fármacos , Lens (Planta) , Preparações de Plantas , Substâncias Protetoras , Traumatismo por Reperfusão/metabolismo , Administração Oral , Animais , Apoptose/efeitos dos fármacos , Nitrogênio da Ureia Sanguínea , Rim/metabolismo , Rim/patologia , Masculino , Camundongos , Camundongos Endogâmicos ICR , Estresse Oxidativo/efeitos dos fármacos , Preparações de Plantas/administração & dosagem , Preparações de Plantas/farmacologia , Substâncias Protetoras/administração & dosagem , Substâncias Protetoras/farmacologia , Traumatismo por Reperfusão/patologia
16.
Environ Pollut ; 272: 116180, 2021 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-33445152

RESUMO

Although liquid products derived from the pyrolysis of biomass are promising for the production of petroleum-like hydrocarbon fuels, the catalytic burden of hydrodeoxygenation must be reduced to achieve feasible upgrading processes. Herein, mild hydrotreating of an acid-rich biomass pyrolysis oil (bio-oil) with an unusually high total acid number (588 mg KOH/g bio-oil) was performed to stabilize the low-quality bio-oil. Ru-added TiO2-supported transition metal catalysts stabilized the bio-oil by reducing its acidity more compared to what could be achieved by Ru-free catalysts; this process also leads to lower loss of organic compounds compared to when using a Ru/TiO2 catalyst. Based on the performance of transition metal catalysts, including Ni, Co, and Cu, supported on TiO2, tungstate-zirconia, or SiO2, supported bimetallic catalysts were prepared by adding Ru to the TiO2-supported metal catalysts. The bimetallic catalysts Ru/Ni/TiO2 and Ru/Co/TiO2 exhibited good decarboxylation activity for the removal of carboxylic acids and a higher yield of organic compounds compared to that provided by Ru, which can be deemed appropriate for feedstocks when hydrodeoxygenation needs to suppress the loss of organic reactants. Using these catalysts, the carboxylic acid concentration was reduced to 319-323 mg KOH/g bio-oil with organic yields of 62-63 wt% at reaction temperatures 150-170 °C lower than the temperature required for direct conversion of carboxylic acids to alcohols or deoxygenates. The improved catalytic hydrotreating activity of Ru-added transition metals can be attributed to the high acid site densities of these catalysts along with their improved hydrogenation activities.


Assuntos
Biocombustíveis , Dióxido de Silício , Catálise , Temperatura Alta , Óleos de Plantas , Polifenóis
17.
J Ginseng Res ; 45(1): 66-74, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-33437158

RESUMO

BACKGROUND: Abnormal chloride (Cl-) transport has a detrimental impact on mucociliary clearance in both cystic fibrosis (CF) and non-CF chronic rhinosinusitis. Ginseng is a medicinal plant noted to have anti-inflammatory and antimicrobial properties. The present study aims to assess the capability of red ginseng aqueous extract (RGAE) to promote transepithelial Cl- secretion in nasal epithelium. METHODS: Primary murine nasal septal epithelial (MNSE) [wild-type (WT) and transgenic CFTR-/-], fisher-rat-thyroid (FRT) cells expressing human WT CFTR, and TMEM16A-expressing human embryonic kidney cultures were utilized for the present experiments. Ciliary beat frequency (CBF) and airway surface liquid (ASL) depth measurements were performed using micro-optical coherence tomography (µOCT). Mechanisms underlying transepithelial Cl- transport were determined using pharmacologic manipulation in Ussing chambers and whole-cell patch clamp analysis. RESULTS: RGAE (at 30µg/mL of ginsenosides) significantly increased Cl- transport [measured as change in short-circuit current (ΔISC = µA/cm2)] when compared with control in WT and CFTR-/- MNSE (WT vs control = 49.8±2.6 vs 0.1+/-0.2, CFTR-/- = 33.5±1.5 vs 0.2±0.3, p < 0.0001). In FRT cells, the CFTR-mediated ΔISC attributed to RGAE was small (6.8 ± 2.5 vs control, 0.03 ± 0.01, p < 0.05). In patch clamp, TMEM16A-mediated currents were markedly improved with co-administration of RGAE and uridine 5-triphosphate (8406.3 +/- 807.7 pA) over uridine 5-triphosphate (3524.1 +/- 292.4 pA) or RGAE alone (465.2 +/- 90.7 pA) (p < 0.0001). ASL and CBF were significantly greater with RGAE (6.2+/-0.3 µm vs control, 3.9+/-0.09 µm; 10.4+/-0.3 Hz vs control, 7.3 ± 0.2 Hz; p < 0.0001) in MNSE. CONCLUSION: RGAE augments ASL depth and CBF by stimulating Cl- secretion through CaCC, which suggests therapeutic potential in both CF and non-CF chronic rhinosinusitis.

18.
J Hazard Mater ; 403: 123704, 2021 02 05.
Artigo em Inglês | MEDLINE | ID: mdl-33264890

RESUMO

The drawback of biochar as a soil ameliorant is its low-nutrient content while the bottleneck of struvite production is its high chemical cost. This drew the idea of using designed biochar for nutrient recovery from nutrient-rich wastewater as struvite. Mg-biochar was used for simultaneous P and N recovery from sewage sludge ash (SSA) and food wastewater (FW) by using ground coffee bean (GCB) and palm tree trunk (PTT) waste. PTT Mg-biochar could recover 92.2% of PO43--P and 54.8% of NH4+-N while GCB Mg-biochar could recover 79.5% of PO43--P and 38.6% of NH4+-N. Adsorption, precipitation and cation-exchange mechanisms are involved in the Mg-biochar for the simultaneous recovery of PO43--P and NH4+-N as struvite. Mg-biochars also showed higher struvite selectivity than the control samples. This method not only supports waste recycling and pollution mitigation but also highlights economical struvite production and the benefits of CO2 sequestration.


Assuntos
Fósforo , Esgotos , Carvão Vegetal , Nitrogênio , Fosfatos , Estruvita , Eliminação de Resíduos Líquidos , Águas Residuárias
19.
Planta Med ; 87(3): 225-235, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33348408

RESUMO

Four new ß-resorcylic acid lactones, including penochrochlactone A (2: ), 4-O-desmethyl-aigialomycin B (4: ), and penochrochlactones C and D (5: and 6: ), two compounds isolated from a natural source for the first time, 5α, 6ß-acetonide-aigialomycin B (1: ) and penochrochlactone B (3: ), together with six known compounds, aigialomycin F (7: ), aigialomycins A, B, and D (8: -10: ), zeaenol (11: ), and oxozeaenol (12: ), were isolated from a mycelial solid culture of the endophytic fungus Penicillium ochrochloron SWUKD4.1850 from the medicinal plant Kadsura angustifolia by sequential purification over silica gel, Sephadex LH-20 column chromatography, and preparative HPLC. Their structures were elucidated by extensive spectroscopic analysis and chemical conversions. In addition, all the new compounds were evaluated for their cytotoxic and antibacterial activities in vitro. Penochrochlactone C (5: ) displayed moderate cytotoxicity against the HeLa tumor cell line with an IC50 value of 9.70 µM. In the antibacterial assays, compounds 4:  - 6: exhibited moderate activities against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa with MIC values between 9.7 and 32.0 µg/mL.


Assuntos
Kadsura , Penicillium , Antibacterianos/farmacologia , Lactonas/farmacologia , Testes de Sensibilidade Microbiana , Estrutura Molecular
20.
Fitoterapia ; 147: 104734, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33007399

RESUMO

Two new C31 triterpenes, polysimiaric acid A (1) and B (2) as well as one new clerodane diterpenoid, 16,16-dimethoxy-cleroda-3,13Z-dien-15-oic acid (3), together with six known compounds were isolated from Polyalthia simiarum. Their structures were determined by analysis of 1D and 2D NMR data. Three new compounds were tested for their cytotoxicity against five human tumour cell lines. Compound 3 showed cytotoxic activities against SMMC-7721 with the IC50 value of 22.43 µM.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Diterpenos Clerodânicos/farmacologia , Polyalthia/química , Terpenos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , China , Diterpenos Clerodânicos/isolamento & purificação , Humanos , Estrutura Molecular , Folhas de Planta/química , Terpenos/isolamento & purificação
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