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1.
J Clin Psychopharmacol ; 44(3): 297-301, 2024.
Article in English | MEDLINE | ID: mdl-38506608

ABSTRACT

PURPOSE: This systematic review aimed to investigate the clinical manifestations and characteristics of venlafaxine-associated rhabdomyolysis. METHODS: A systematic search was conducted in PubMed, Elsevier, Science Direct, Embase, Springer Link, Wiley Online Library, CNKI, and Wanfang databases from the date of database inception to January 2023. Previously reported cases of venlafaxine-associated rhabdomyolysis were identified, and relevant data from these cases were collected for descriptive statistical analysis. Cases that met the inclusion criteria were evaluated to determine the correlation between adverse reactions and venlafaxine. RESULTS: A total of 12 patients with venlafaxine-associated rhabdomyolysis were included. None of these patients had a history of muscle pain or discomfort. Of the 12 patients, 5 patients received venlafaxine at doses of ≤225 mg/d, whereas the remaining 7 patients received doses exceeding 225 mg/d. The main clinical symptoms included myalgia, muscle weakness, and renal injury. All 12 patients discontinued venlafaxine and received symptomatic care. CONCLUSIONS: Venlafaxine, used either as a monotherapy or in combination with other drugs, may be associated with rhabdomyolysis. Creatine kinase levels may normalize or significantly decrease after discontinuation of venlafaxine and symptomatic treatment.


Subject(s)
Rhabdomyolysis , Venlafaxine Hydrochloride , Rhabdomyolysis/chemically induced , Venlafaxine Hydrochloride/adverse effects , Venlafaxine Hydrochloride/administration & dosage , Humans , Male , Adult , Female , Middle Aged , Creatine Kinase/blood , Myalgia/chemically induced
2.
J Fluoresc ; 2024 Feb 29.
Article in English | MEDLINE | ID: mdl-38421599

ABSTRACT

Intracellular copper ion (Cu2+) is irreplaceable and essential in regulation of physiological and biological processes, while excessive copper from bioaccumulation may cause potential hazards to human health. Hence, effective and sensitive recognition is urgently significant to prevent over-intake of copper. In this work, a novel highly sensitive and green carbon quantum dots (Green-CQDs) were synthesized by a low-cost and facile one-step microwave auxiliary method, which utilized gallic acid, carbamide and PEG400 as carbon source, nitrogen source and surface passivation agent, respectively. The decreased fluorescence illustrated excellent linear relationship with the increasing of Cu2+ concentration in a wide range. Substantial surface amino and hydroxyl group introduced by PEG400 significantly improved selectivity and sensitivity of Green-CQDs. The surface amino chelation mechanism and fluorescence internal filtration effect were demonstrated by the restored fluorescence after addition of EDTA. Crucially, the nanosensor illustrated good cell permeability, high biocompatibility and recovery rate, significantly practical application in fluorescent imaging and biosensing of intracellular Cu2+ in HepG-2 cells, which revealed a potential and promising biological applications in early diagnosis and treatment of copper ion related disease.

3.
Cost Eff Resour Alloc ; 22(1): 6, 2024 Jan 24.
Article in English | MEDLINE | ID: mdl-38267990

ABSTRACT

BACKGROUND: Programmed cell death protein 1 (PD-1) monoclonal antibody, pembrolizumab, is a promising drug for platinum-pretreated, recurrent or metastatic nasopharyngeal cancer (NPC). We aimed to assess the cost-effectiveness of pembrolizumab compared with chemotherapy for Chinese patients in this NPC. METHODS: The cost-effectiveness of pembrolizumab versus chemotherapy was evaluated using a partitioned survival model with a 5-year boundary. Efficacy and toxicity data were derived from the KEYNOTE-122 trials. Economic indicators including life-years (LYs), quality-adjusted life-years (QALYs), incremental cost-effectiveness ratio (ICER), and lifetime cost were used. One-way analysis and probabilistic sensitivity analysis (PSA) were performed to explore the uncertainties. Additionally, various scenario analyses, including different pembrolizumab price calculations and discount rates were performed. RESULTS: Pembrolizumab or chemotherapy alone respectively yielded 2.82 QALYs (3.96 LYs) and 2.73 QALYs (3.93 LYs) with an ICER of $422,535 per QALYs ($1,232,547 per LYs). This model was primarily influenced by the price of pembrolizumab. Furthermore, PSA indicated that pembrolizumab had none probability of being cost-effective compared with chemotherapy at a willingness-to- pay (WTP) of $38223. Scenario analyses revealed that irrespective of any potential price reduction or adjustments in the discount rate, no discernible impact on the ultimate outcome was observed. CONCLUSION: Pembrolizumab was less cost-effective for patients with platinum-pretreated, recurrent or metastatic NPC compared with chemotherapy in China.

4.
Spectrochim Acta A Mol Biomol Spectrosc ; 309: 123733, 2024 Mar 15.
Article in English | MEDLINE | ID: mdl-38157745

ABSTRACT

Hypochlorite (ClO-) is an important redox regulator in reactive oxygen species, which play a considerable role in oxidative stress and related diseases. Hence, accurate and sensitive monitoring of ClO- concentration was urgently needed in the fields of life sciences, food and environment. Bright green fluorescent carbon quantum dots (G-CQDs) were synthesized utilizing one-step hydrothermal method with citric acid and acriflavine precursors. Through TEM, FTIR, XPS and zeta potential characterization procedures, G-CQDs illustrated uniformly dispersed and significant number of -NH2 and -OH on the surface. Meanwhile, the fluorescence and colorimetric analysis exhibited wide linear range and low detection limit response to ClO-. The fluorescence changes of G-CQDs were identified via smartphone to realize mobile sensing of ClO-. Subsequently, G-CQDs was applied for visualization and quantitative detection of ClO- in drinking water samples with satisfactory recovery rate. More importantly, G-CQDs demonstrated good water solubility, optical stability and excellent biocompatibility, which offered a promising analysis approach in cell imaging and exogenous ClO- detection in living cells. G-CQDs illustrated bright prospect and great potential in practical application of ClO- associated disease prevention and early clinical diagnosis.


Subject(s)
Quantum Dots , Hypochlorous Acid , Carbon , Fluorescence , Solubility
5.
Future Oncol ; 19(38): 2525-2536, 2023 Dec.
Article in English | MEDLINE | ID: mdl-38059348

ABSTRACT

Background: We aimed to compare the cost-effectiveness of bruton tyrosine kinase inhibors (BTKis) versus bendamustine-rituximab (R-bendamustine) as a first-line treatment for Chinese patients with relapsed or refractory chronic lymphocytic leukemia. Methods: A partitioned survival model was constructed using TreeAge Pro 2022 software and transition probabilities were estimated from the reported survival probabilities using parametric survival modeling. One-way analysis and probabilistic sensitivity analysis were performed to explore the uncertainty of the modeling results. In addition, several scenario analyses were evaluated. Results: In comparison to R-bendamustine, zanubrutinib had an incremental cost-effectiveness ratio (ICER; life years) and ICER (quality-adjusted life years) of US$12,173.38 and $17,983.40, respectively. While ibrutinib had a higher ICER relative to R-bendamustine. Conclusion: Zanubrutinib was cost-effective for patients with relapsed or refractory chronic lymphocytic leukemia in China.


Subject(s)
Leukemia, Lymphocytic, Chronic, B-Cell , Humans , Rituximab/therapeutic use , Bendamustine Hydrochloride/therapeutic use , Leukemia, Lymphocytic, Chronic, B-Cell/drug therapy , Leukemia, Lymphocytic, Chronic, B-Cell/etiology , Cost-Benefit Analysis , China , Antineoplastic Combined Chemotherapy Protocols/adverse effects
6.
Immun Inflamm Dis ; 11(9): e1002, 2023 09.
Article in English | MEDLINE | ID: mdl-37773697

ABSTRACT

OBJECTIVE: Allergic rhinitis (AR) is a common allergic disorder, afflicting thousands of human beings. Aberrant mitochondrial dynamics are important pathological elements for various immune cell dysfunctions and allergic diseases. However, the connection between mitochondrial dynamics and AR remains poorly understood. This study aimed to determine whether mitochondrial dynamics influence the inflammatory response in AR. METHODS: In the present study, we established a murine model of AR by sensitization with ovalbumin (OVA). Then, we investigated the mitochondrial morphology in mice with AR by transmission electron microscopy and confocal fluorescence microscopy, and evaluated the role of Mdivi-1 (an inhibitor of mitochondrial fission) on allergic symptoms, inflammatory responses, allergic-related signals, and reactive oxygen species formation. RESULTS: There was a notable enhancement in mitochondrial fragmentation in the nasal mucosa of mice following OVA stimulation, whereas Mdivi-1 prevented aberrant mitochondrial morphology. Indeed, Mdivi-1 alleviated the rubbing and sneezing responses in OVA-sensitized mice. Compared with vehicle-treated ones, mice treated with Mdivi-1 exhibited a reduction in interleukin (IL)-4, IL-5, and specific IgE levels in both serum and nasal lavage fluid, and shown an amelioration in inflammatory response of nasal mucosa. Meanwhile, Mdivi-1 treatment was associated with a suppression in JAK2 and STAT6 activation and reactive oxygen species generation, which act as important signaling for allergic response. CONCLUSION: Our findings reveal mitochondrial dynamics modulate the allergic responses in AR. Mitochondrial dynamics may represent a promising target for the treatment of AR.


Subject(s)
Mitochondrial Dynamics , Rhinitis, Allergic , Humans , Animals , Mice , Disease Models, Animal , Reactive Oxygen Species , Immunoglobulin E , Inflammation
7.
Cancer Chemother Pharmacol ; 92(3): 211-221, 2023 09.
Article in English | MEDLINE | ID: mdl-37432399

ABSTRACT

PURPOSE: Head and neck squamous cell carcinoma (HNSCC) ranks as the sixth most prevalent cancer. In recent years, the modification of platinum(II) into platinum(IV) derivative compounds, by introducing biologically active molecules, has been extensively employed to develop novel platinum-based prodrugs. We investigated the anti-proliferative activity against HNSCC of a new veratric acid (COX-2 inhibitor)-platinum(IV) complex. METHODS: In this study, a new veratric acid (COX-2 inhibitor)-platinum(IV) complex, termed veratricplatin, was synthesized. We evaluated the anti-tumor effect of in vitro and in vivo by western blotting, flow cytometry and DNA damage analysis. RESULTS: Veratricplatin displayed remarkable anti-proliferative activity against various cancer cell lines, including A549, FaDu, HeLa, and MCF-7. Furthermore, veratricplatin demonstrated significantly stronger cytotoxicity than either platinum(II) or veratric acid monotherapy or their combination. Importantly, the synthesized prodrug exhibited less toxicity toward normal cells (MRC-5), while dramatically enhanced DNA damage in FaDu cells inducing apoptosis. Moreover, veratricplatin markedly reduced the migration ability of FaDu cells compared to the control or monotherapy. In vivo, veratricplatin displayed potent anti-tumor activity with no apparent toxicity in BALB/c nude mice bearing FaDu tumors. In addition, tissue immunofluorescence analysis revealed that veratricplatin could substantially inhibit the formation of tumor blood vessels. CONCLUSION: Veratricplatin demonstrated remarkable drug efficacy, in terms of increased cytotoxicity in vitro and high efficiency with low toxicity in vivo.


Subject(s)
Cyclooxygenase 2 Inhibitors , Head and Neck Neoplasms , Mice , Animals , Squamous Cell Carcinoma of Head and Neck/drug therapy , Cyclooxygenase 2 Inhibitors/pharmacology , Mice, Nude , Apoptosis , Cell Line, Tumor , Head and Neck Neoplasms/drug therapy
8.
Mini Rev Med Chem ; 2023 Jul 17.
Article in English | MEDLINE | ID: mdl-37461341

ABSTRACT

Histone deacetylases (HDACs) are a class of enzymes that are responsible for the removal of acetyl groups from the ε-N-acetyl lysine of histones, allowing histones to wrap DNA more tightly. HDACs play an essential role in many biological processes, such as gene regulation, transcription, cell proliferation, angiogenesis, migration, differentiation and metastasis, which make it an excellent target for anticancer drug discovery. The search for histone deacetylase inhibitors (HDACis) has been intensified, with numerous HDACis being discovered, and five of them have reached the market. However, currently available HDAC always suffers from several shortcomings, such as limited efficacy, drug resistance, and toxicity. Accordingly, dual-targeting HDACis have attracted much attention from academia to industry, and great advances have been achieved in this area. In this review, we summarize the progress on inhibitors with the capacity to concurrently inhibit tubulin polymerization and HDAC activity and their application in cancer treatment.

9.
Ther Adv Drug Saf ; 14: 20420986231181335, 2023.
Article in English | MEDLINE | ID: mdl-37377748

ABSTRACT

Aims: To investigate the safety of oral iron therapy in pregnant women with iron-deficiency anemia (IDA) in the real world. Methods: A retrospective analysis was performed on 1792 pregnant patients with IDA who received oral iron supplements from 12 hospitals in Shandong Province from 1 April to 31 June 2021; follow-up and adverse reactions were recorded. They were divided into six groups according to the treatment drugs. Results: The overall adverse reaction rate was 15.4%, and the main adverse reaction site was the digestive system. The incidence of all kinds of oral iron adverse reactions from high to low in order: compound ferrous sulfate and folic acid tablets (21.88%); iron proteinsuccinylate oral solution (20.90%); ferrous succinate tablets (19.76%); ferrous succinate sustained-release tablets (18.00%); iron polysaccharide complex capsule (12.06%); and iron dextran oral solution (6.94%). It was found that there was a significant difference in the incidence of adverse reactions among the six drugs (p < 0.05). Pairwise comparison showed that the incidence of adverse reactions was higher in the iron proteinsuccinylate oral solution than that in the iron polysaccharide complex capsule (p < 0.05). There was no significant difference in the incidence of adverse reactions in different ages (p > 0.05), but there was a significant difference in the incidence of adverse reactions in different gestational ages (p < 0.05). In Adverse Drug Reaction (ADR) patients, the adverse reaction result of most patients is recovery or improvement, and there was no serious adverse reaction outcome such as sequela and death. Conclusion: All the adverse reactions of oral iron were mainly gastrointestinal adverse reactions, and no heavy adverse reactions were found. Iron proteinsuccinylate oral solution has a higher incidence of adverse reactions than iron polysaccharide complex capsule. The results showed that oral iron was safer for anemia patients during pregnancy.


Safety of oral iron in the treatment of iron-deficiency anemia during pregnancy Introduction: The safety of different oral iron agents varies. At present, the safety evaluation of iron supplements in the treatment of anemia during pregnancy is mainly focused on intravenous iron supplements, and there is no comprehensive study on the safety of commonly used oral iron supplements. This study compared the safety of six commonly used oral iron supplements in the treatment of iron-deficiency anemia during pregnancy, aiming to provide a reference for clinical medication. Methods: We conducted a study involving 1792 patients in 12 hospitals in Shandong Province from 1 April to 31 June 2021. Results: Among the six groups, 276 ADR patients reported 302 adverse reactions. There were significant differences in the rates of adverse reactions among the six oral iron agents, and the incidence of adverse reactions in the iron proteinsuccinylate oral solution was significantly higher than that of iron polysaccharide complex capsules. The main incidence of adverse reactions was constipation (6.96%), and most of the outcomes were cured or improved. Conclusion: In this study, there were no heavy adverse reactions. The incidence of adverse reactions of iron proteinsuccinylate oral was higher than that of iron polysaccharide compound capsule. The results showed that oral iron had a good safety in patients with anemia during pregnancy.

10.
Curr Med Chem ; 30(20): 2267-2311, 2023.
Article in English | MEDLINE | ID: mdl-36043742

ABSTRACT

Inhibition of histone deacetylases (HDACs) has proven to be an effective strategy for cancer therapy. To date, five histone deacetylase inhibitors (HDACis) have been approved for cancer treatment, and numerous others are undergoing clinical trials. An agent that can simultaneously and effectively inhibit two or more targets may offer greater therapeutic benefits over single-acting agents in preventing resistance to treatment and potentiating synergistic effects. A prime example of a bifunctional agent is the hybrid HDACi. Representative classes of reported hybrid HDACis are reviewed here to shed light on the design of novel hybrid HDACis for cancer therapy.


Subject(s)
Antineoplastic Agents , Neoplasms , Humans , Histone Deacetylase Inhibitors/pharmacology , Histone Deacetylase Inhibitors/therapeutic use , Histone Deacetylases , Antineoplastic Agents/pharmacology , Antineoplastic Agents/therapeutic use , Neoplasms/drug therapy
11.
Front Pharmacol ; 13: 943674, 2022.
Article in English | MEDLINE | ID: mdl-36304151

ABSTRACT

Background: Tigecycline was recently found to cause coagulation disorders, especially hypofibrinogenemia, which may interfere with the administration of antimicrobial therapy. This study aimed to investigate the incidence and clinical characteristics of and risk factors for tigecycline-associated hypofibrinogenemia. Methods: In this multicenter retrospective study, patients receiving tigecycline or imipenem-cilastatin to treat Gram-negative bacterial infections in nine Chinese tertiary hospitals between January 2020 and December 2020 were enrolled. Baseline data and coagulation variables were compared using cohort and case-control studies. Results: Totals of 485 patients treated with tigecycline and 490 patients treated with imipenem-cilastatin were included in this study. Compared with imipenem-cilastatin, tigecycline was associated with reduced fibrinogen and prolonged activated partial thromboplastin time and prothrombin time (all p < 0.001), with the most remarkable change in fibrinogen (down by 48.0%). The incidence of hypofibrinogenemia in patients treated with tigecycline was >50%, with propensity score-matched analysis or not. The relative risk of hypofibrinogenemia with tigecycline versus imipenem-cilastatin was 2.947 (95% CI: 2.151-4.039) at baseline balance. Tigecycline-associated hypofibrinogenemia led to a higher incidence (12.1%) of bleeding events. However, none of supplemental therapies after withdrawal had an effect on the normalization of fibrinogen levels. The risk factors for tigecycline-associated hypofibrinogenemia were treatment duration ≥6 days (odds ratio [OR] 5.214, 95% confidence interval [CI] 2.957-9.191, p < 0.001), baseline fibrinogen <4 g/L (OR 4.625, 95% CI 2.911-7.346, p < 0.001), cumulative dose ≥1,000 mg (OR 2.637, 95% CI 1.439-4.832, p = 0.002), receiving CRRT (OR 2.436, 95% CI 1.179-5.031, p = 0.016), baseline PT > 14 s (OR 2.110, 95% CI 1.317-3.380, p = 0.002) and baseline total bilirubin >21 µmol/L (OR 1.867, 95% CI 1.107-3.147, p = 0.019), while the protective factor was skin and soft tissue infection (OR 0.110, 95% CI 0.026-0.473, p = 0.003). Conclusion: The clinical characteristics of and risk factors for tigecycline-associated hypofibrinogenemia identified in this study can offer practical reference for the clinical management of patients.

12.
Chem Commun (Camb) ; 58(23): 3803-3806, 2022 Mar 18.
Article in English | MEDLINE | ID: mdl-35229844

ABSTRACT

Tumor growth and metastasis are caused by many factors. The complexity means that a multi-target combination therapy strategy should be selected against tumor growth and metastasis. Here, cisplatin (CDDP) and bendazac (Ben) were designed as a novel NSAID-Pt(IV) nanoplatform, which is an effective weapon for combating tumor growth and metastasis.


Subject(s)
Antineoplastic Agents , Neoplasms , Prodrugs , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Antineoplastic Agents/pharmacology , Antineoplastic Agents/therapeutic use , Cell Line, Tumor , Cisplatin , Humans , Neoplasms/drug therapy , Prodrugs/pharmacology
13.
Biochim Biophys Acta Gen Subj ; 1866(2): 130050, 2022 02.
Article in English | MEDLINE | ID: mdl-34800580

ABSTRACT

BACKGROUND: Candida albicans (C. albicans) is an opportunistic pathogen that can cause superficial and life-threatening systemic infections in immunocompromised patients. However, the available clinically antifungals are limited. Therefore, the development of effective antifungal agents and therapies is urgently needed. Quinoline type of compounds were reported to possess potent anti-fungal effect. A series of quinoline derivatives were synthesized. Moreover their inhibitory activities and mechanisms on C. albicans were evaluated in this study. METHODS: The structure of D319 was identified by extensive spectroscopic analysis. The antifungal activity of D319 on C. albicans was evaluated using conventional methods, including the inhibition zone diameters with filter paper, Clinical Laboratory Standard Institute (CLSI) broth microdilution method in vitro, and in a murine model in vivo. Flow cytometry, fluorescence microscopy, western blot, knockout mutant and revertant strain techniques, and molecular modeling were applied to explore the mechanism of action of D319 in anti-Candida. RESULTS: D319 exhibited potent anti-Candida activity with Minimum Inhibitory Concentration value of 2.5 µg/mL in vitro. D319 significantly improved survival rate and reduced fungal burden compared to vehicle control in a murine model in vivo. The treatment of C. albicans with D319 resulted in fungal apoptosis through reactive oxygen species (ROS) accumulation in C. albicans. Furthermore, D319 inhibited the glyoxylate enzyme isocitrate lyase (ICL) of C. albicans, which was also confirmed by docking analysis. CONCLUSIONS: Quinoline compound D319 exhibited strong anti-Candida activities in vitro and in vivo models through inhibiting ICL activity and ROS accumulation in C. albicans. GENERAL SIGNIFICANCE: This study showed that compound D319 as a novel isocitrate lyase inhibitor, would be a promising anti-Candida lead compound, which provided a potential application of this type of compounds in fighting clinical fungal infections. Furthermore, this study also supported ICL as a potential target for anti-Candida drug discovery.


Subject(s)
Antifungal Agents
14.
Front Pharmacol ; 13: 987337, 2022.
Article in English | MEDLINE | ID: mdl-36686677

ABSTRACT

Background: Maintenance therapy with the poly (ADP-ribose) polymerase inhibitors (PARPis) for platinum-sensitive recurrent ovarian carcinoma (OC) have proven to be effective compared with placebo. We aimed to evaluate the cost-effectiveness (CE) of maintenance fuzuloparib compared to routine surveillance (RS), niraparib and olaparib for platinum-sensitive recurrent OC from the Chinese healthcare systems. Method: A partitioned survival model with three-state (progression-free, progressed, death) was constructed utilizing TreeAge Pro 2011 software to evaluate the economic value of fuzuloparib, niraparib and olaparib maintenance treatment for platinum-sensitive recurrent OC based on the clinical data derived from FZOCUS-2, ENGOT-OV16/NOVA and ENGOT-Ov21/SOLO2. Transition probabilities were estimated from the reported survival probabilities in those trials. Cost and health preference data were derived from the literature. The quality-adjusted life-years (QALYs) and lifetime costs were measured for this analysis. A 5 years horizon and 5%/year discount rates were used. One-way analysis, and probabilistic sensitivity analysis (PSA) were performed to explore the model uncertainties. Results: Total cost of fuzuloparib, niraparib and olaparib were $31628.10, $48183.48 and $54605.54, whereas they had an incremental cost-utility ratio of $31992.69, $32216.08 and $23359.26 per additional progression-free survival (PFS) QALYs gained compared with RS, relatively. Model showed that maintenance fuzuloparib achieved at least an 85.5% probability of CE at the threshold of $37654.50/QALY. One-way sensitivity analysis revealed that the results were sensitive to the PFS and the price of medicines. Conclusion: Fuzuloparib was less cost-effective for patients with germline BRCA1/2 mutation and platinum-sensitive recurrent OC compared to olaparib, but was superior to niraparib from the Chinese healthcare systems perspective.

15.
Drug Des Devel Ther ; 15: 4701-4711, 2021.
Article in English | MEDLINE | ID: mdl-34815665

ABSTRACT

PURPOSE: The resistance of C. albicans to traditional antifungal drugs brings a great challenge to clinical treatment. To overcome the resistance, developing antifungal agent sensitizers has attracted considerable attention. This study aimed to determine the anti-Candida activity of BEH alone or BEH-FLC combination and to explore the underlying mechanisms. MATERIALS AND METHODS: In vitro antifungal effects were performed by broth microdilution assay and XTT reduction assay. Infected Galleria mellonella larvae model was used to determine the antifungal effects in vivo. Probes Fluo-3/AM, FITC-VAD-FMK and rhodamine 6G were used to study the influence of BEH and FLC on intracellular calcium concentration, metacaspase activity and drug efflux of C. albicans. RESULTS: BEH alone exhibited obvious antifungal activities against C. albicans. BEH plus FLC not only showed synergistic effects against planktonic cells and preformed biofilms within 8 h but also enhanced the antifungal activity in infected G. mellonella larvae. Mechanistic studies indicated that antifungal effects of drugs might be associated with the increasement of calcium concentration, activation of metacaspase activity to reduce virulence and anti-biofilms, but were not related to drug efflux. CONCLUSION: BEH alone or combined with FLC displayed potent antifungal activity both in vitro and in vivo, and the underlying mechanisms were related to reduced virulence factors.


Subject(s)
Antifungal Agents/pharmacology , Benserazide/pharmacology , Candida albicans/drug effects , Fluconazole/pharmacology , Animals , Antifungal Agents/chemistry , Benserazide/chemistry , Biofilms/drug effects , Dose-Response Relationship, Drug , Drug Resistance, Fungal/drug effects , Drug Therapy, Combination , Fluconazole/chemistry , Microbial Sensitivity Tests , Moths
16.
Nucl Med Commun ; 40(10): 995-1000, 2019 Oct.
Article in English | MEDLINE | ID: mdl-31365496

ABSTRACT

OBJECTIVE: Our purpose was to establish a simple and feasible method for monitoring and controlling the Tc-Technegas inhaled to improve the success ratio of imaging and ensure the imaging quality. MATERIALS AND METHODS: The relationship between the success ratio and the pulmonary ventilation counting rate (VCR) of 113 cases, the activity of perfusion imaging agents injected and the pulmonary perfusion counting rate (PCR) of another 114 cases were analysed retrospectively. And combined with the relationship between the surface radioactivity monitoring value and the SPECT probe counting rate of a pulmonary model, the effective range of the VCR and the surface radioactivity monitoring value were determined. Two hundred fifty cases with Tc-Technegas inhaled monitored and controlled were used to verify the reliability and practicability of this method. RESULTS: The VCR of the ventilation/perfusion imaging with deep venous thrombosis imaging and the ventilation/perfusion imaging without deep venous thrombosis imaging was in 1.0-3.0 kct/s and 1.0-2.0 kct/s when the monitoring values of handheld radiation monitor was within the range of 60-170 µSv/h and 60-110 µSv/h, respectively. The success ratio of the V/Q-Only increased from 48.9% (43/88) of the control group to 80.8% (122/151) of the experimental group. The VCR in the two groups was examined by the non-parametric Mann-Whitney U test (P < 0.001), which indicated that there was a significant difference between the experimental group and the control group. CONCLUSION: The external monitoring method established in this study was of great significance in improving the success ratio of 1-day pulmonary ventilation/perfusion imaging and ensuring the image quality.


Subject(s)
Inhalation , Perfusion Imaging/adverse effects , Pulmonary Ventilation , Sodium Pertechnetate Tc 99m/administration & dosage , Sodium Pertechnetate Tc 99m/adverse effects , Adolescent , Adult , Aged , Aged, 80 and over , Female , Humans , Male , Middle Aged , Retrospective Studies , Time Factors , Tomography, Emission-Computed, Single-Photon/adverse effects , Young Adult
17.
Clin Nucl Med ; 44(6): 469-471, 2019 Jun.
Article in English | MEDLINE | ID: mdl-30829869

ABSTRACT

Chest CT images were acquired in a 67-year-old man to evaluate a left lung mass revealed by chest radiography. The image findings suggested possible pulmonary malignancy. FDG PET/CT was performed for staging, which showed the abnormally increased activity in the lung mass with hypermetabolic lymph node. Pathology from the biopsy confirmed malignant perivascular epithelioid cell tumor.


Subject(s)
Lung Neoplasms/diagnostic imaging , Perivascular Epithelioid Cell Neoplasms/diagnostic imaging , Positron Emission Tomography Computed Tomography , Aged , Fluorodeoxyglucose F18 , Humans , Male , Radiopharmaceuticals
18.
Mini Rev Med Chem ; 17(8): 675-682, 2017.
Article in English | MEDLINE | ID: mdl-27670582

ABSTRACT

BACKGROUND: Tip60, the founding member of MYST histone acetyltransferase family, was originally identified as a cellular acetyltransferase protein that interacts with HIV-1 Tat. Tip60 plays roles in many processes such as cellular signaling transmission, DNA damage repair, cell cycle and checkpoint control and apoptosis by acetylating its histone or non-histone substrates. RESULTS: Dysfunction of Tip60 could promote or suppress diseases including different kinds of cancers. CONCLUSION: Here, main functions and its known inhibitors were summarized.


Subject(s)
Enzyme Inhibitors/pharmacology , Histone Acetyltransferases/antagonists & inhibitors , Histone Acetyltransferases/metabolism , Enzyme Inhibitors/chemistry , Humans , Lysine Acetyltransferase 5 , Models, Molecular , Molecular Structure
19.
Article in Chinese | MEDLINE | ID: mdl-25248267

ABSTRACT

OBJECTIVE: To investigate the mechanism. METHOD: We isolate the mouse bone marrow cells and cultured with rGM-CSF and rIL-4 to stimulate bone marrow cells to transfer to immature dendritic cells. And then the immature dendritic cells were costimulated with ILPS and different concentrations of Bimingan Granule. RESULT: MHC II, CD80, CD86 were detected by flow cytometer and TNF-alpha, IL-1beta, IL-6 and IL-10 were quantified by ELISA. CONCLUSION: Our results showed that Bimingan Granule may significantly inhibit the differentiation of immature dendritic cells to mature dendritic cells.


Subject(s)
Dendritic Cells/immunology , Drugs, Chinese Herbal/pharmacology , Rhinitis, Allergic/immunology , Animals , Cell Differentiation/drug effects , Cells, Cultured , Dendritic Cells/drug effects , Mice , Mice, Inbred C57BL , Rhinitis, Allergic/drug therapy
20.
Curr Med Chem ; 19(21): 3622-34, 2012.
Article in English | MEDLINE | ID: mdl-22612709

ABSTRACT

Hydrogen peroxide (H(2)O(2)) has entrapped the abundant concern of numerous researchers in the cutting edge of chemistry, biology and medicine since it is thought to be associated with various biological and pathological conditions. Fluorescent probes are the promising tools for the detection and understanding of the physiological roles of H(2)O(2), considering that they are able to provide spatial and temporal information about target biomolecules in living cells. Nevertheless, the existent fluorescent probes have low selectivity and sensitivity on discerning H(2)O(2). This review would like to demonstrate a comprehensive examination on the design, recognition, and performance of state-of-the-art boronate-based fluorogenic switch for the detection of H(2)O(2), a field in which remarkable improvements have been accomplished over the last decade.


Subject(s)
Boronic Acids/chemistry , Fluorescent Dyes/chemistry , Hydrogen Peroxide/analysis , Molecular Structure
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