Although various antibacterial strategies have been developed, antibiotic chemotherapy remains the primary clinical treatment for bacterial infections. To address the limitations associated with the traditional antibiotic therapy, like burst drug release, rapid drug clearance, and the emergence of drug resistance, it is highly desirable to develop drug release systems that can realize controlled and sustained drug release to enhance the therapeutic efficacy. Herein, we present a novel drug release system, CIP@SU-102, which shows superior and long-lasting antibacterial activity.
View Article and Find Full Text PDFBackground: From 2004 onwards, the Chinese government has freely offered complimentary Chinese herbal medicine (CHM) to Chinese HIV/AIDS patients, alongside the prescribed first line therapy of highly active antiretroviral therapy (HAART). Thus, we aimed to explore the effectiveness and safety of CHM for patients with HIV/AIDS.
Methods: The data from the Guangxi pilot database and antiviral treatment sites database have been respectively developed into two datasets in this prospective cohort real-world study, the CHM combined HAART group (the integrated group) and the HAART group.
The abuse of antibiotics leads to an increasing emergence of drug-resistant bacteria, which not only causes a waste of medical resources but also seriously endangers people's health and life safety. Therefore, it is highly desirable to develop an efficient antibacterial strategy to reduce the reliance on traditional antibiotics. Antibacterial photodynamic therapy (aPDT) is regarded as an intriguing antimicrobial method that is less likely to generate drug resistance, but its efficiency still needs to be further improved.
View Article and Find Full Text PDFBackground: Pilomatricoma is a common but easily misdiagnosed tumor in children.
Aims: To differentiate pilomatricoma from other common subcutaneous nodules in children.
Patients/methods: Misdiagnosed subcutaneous nodules in four children were recorded.
A multi-parameter controllable automatic fire-acupuncture instrument was developed by integrating traditional fire needling with modern medical device technology. A gun-like appearance was designed for easy hand-held operation, the electromagnetic induction was for heating needle body, a scale knob was for controlling the needle insertion depth, the combination of electromagnetic ejection and spring return was for the precise control of the needle retention time; and the changeable single ste-rile needle or multiple needles were adopted to meet individual demand, obtain high efficiency and prevent infection. All of these designs are associated with the overall process control system to ensure the exact controllability of needle body temperature, needling density, insertion depth and needle retention time.
View Article and Find Full Text PDFHDAC inhibitors (HDACis) have been intensively studied for their roles and potential as drug targets in T-cell lymphomas and other hematologic malignancies. Bisthianostat is a novel bisthiazole-based pan-HDACi evolved from natural HDACi largazole. Here, we report the preclinical study of bisthianostat alone and in combination with bortezomib in the treatment of multiple myeloma (MM), as well as preliminary first-in-human findings from an ongoing phase 1a study.
View Article and Find Full Text PDFSimple and reliable mass production of platinum-based alloy catalysts with excellent activity and stability is an enormous challenge for the wide commercialization of proton-exchange membrane fuel cells (PEMFC), especially those with ultralow loading of Pt. Herein, an economical, highly durable, and efficient catalyst consisting of structurally ordered intermetallic PtCo alloy nanoparticles with ultralow Pt loading (1.4 wt %) supported on hierarchically porous carbon structure (three-dimensional, 3D PtCo/C) were synthesized with large-scale production by the NaCl-template-assisted approach.
View Article and Find Full Text PDFColorectal cancer (CRC) is the 5 leading cancer in China. Alcohol consumption has been reported to be one of the risk factors of CRC. However, it remains unclear whether genetic variants of alcohol metabolic genes are associated with CRC risk.
View Article and Find Full Text PDFBackground: The term vascular anomalies include various vascular tumors and vascular malformations, among them infantile hemangiomas and capillary malformations are the most well-known associated diseases in early ages. Multiple drugs have been introduced for intervention, but susceptibility test in vitro were scarcely reported.
Objective: To evaluate the inhibition effect of different drugs by adenosine triphosphate sensitivity assay in vitro before the treatment of infantile hemangiomas and capillary malformations.
Hyaluronic acid (HA) and cell-penetrating peptide (CPP) R6H4-SA modified artesunate nanostructured lipid carrier (HA-R6H4-NLC/ART) for anti-tumor therapy was prepared. The physicochemical properties and in vitro drug release of HA-R6H4-NLC/ART were evaluated, and the uptake and cytotoxicity of liver cancer HepG2 cells were studied. The results showed that HA-R6H4-NLC/ART was spherical like in appearance, and the average particle size was about 160 nm.
View Article and Find Full Text PDFA new series of the structural and functional models for the active site of [NiFe]-Hases has been prepared by a simple and convenient synthetic route. Thus, treatment of diphosphines RN(PPh) (1a, R = p-MeCHCH; 1b, R = EtOCCH) with an equimolar NiCl·6HO, NiBr·3HO, and NiI in refluxing CHCl/MeOH or EtOH gave the mononuclear Ni complexes RN(PPh)NiX (2a, R = p-MeCHCH, X = Cl; 2b, R = EtOCCH, X = Cl; 3a, R = p-MeCHCH, X = Br; 3b, R = EtOCCH, X = Br; 4a, R = p-MeCHCH, X = I; 4b, R = EtOCCH, X = I) in 67-97% yields. Further treatment of complexes 2a,b-4a,b with an equimolar mononuclear Fe complex (dppv)(CO)Fe(pdt) and NaBF resulted in formation of the targeted model complexes [RN(PPh)Ni(μ-pdt)(μ-X)Fe(CO)(dppv)](BF) (5a, R = p-MeCHCH, X = Cl; 5b, R = EtOCCH, X = Cl; 6a, R = p-MeCHCH, X = Br; 6b, R = EtOCCH, X = Br; 7a, R = p-MeCHCH, X = I; 7b, R = EtOCCH, X = I) in 60-96% yields.
View Article and Find Full Text PDFBackground/objectives: In addition to increase mortality, comorbidities can increase medical costs for systemic lupus erythematosus (SLE). Healthcare utilization can dramatically increase medical costs. It is essential to better understand the comorbidities that can lead to healthcare utilization, such as emergency department visit and/or hospitalization, for SLE patients.
View Article and Find Full Text PDFThis study aims to examine the associations between comorbid conditions and healthcare utilization, medical charges, or mortality of patients with rheumatoid arthritis (RA). Nebraska state emergency department (ED) discharge, hospital discharge, and death certificate data from 2007 to 2012 were used to study the comorbid conditions of patients with RA. RA was defined using the standard International Classification of Diseases (ICD-9-CM 714 or ICD-10-CM M05, M06, and M08).
View Article and Find Full Text PDFIntroduction: Persistent inflammation and oxidative stress are the main mechanisms that increase the risks of cardiovascular disease-related morbidity and mortality in systemic lupus erythematosus (SLE). As a natural antioxidant, lycopene can alleviate oxidative stress and suppress inflammation. We hypothesized that lycopene could have the potential to reduce mortality in SLE.
View Article and Find Full Text PDFAs active site models of [Fe]-hydrogenase, tridentate 2-acylmethyl-6-methoxymethoxy-difunctionalized pyridine-containing complexes η(3)-(2-COCH2-6-MeOCH2OC5H3N)Fe(CO)2(L1) (4, L1 = I; 5, SCN; 6, PhCS2) were prepared via the following multistep reactions: (i) etherification of 2-MeO2C-6-HOC5H3N with ClCH2OMe to give 2-MeO2C-6-MeOCH2OC5H3N (1), (ii) reduction of 1 with NaBH4 to give 2-HOCH2-6-MeOCH2OC5H3N (2), (iii) esterification of 2 with 4-toluenesulfonyl chloride to give 2-TsOCH2-6-MeOCH2OC5H3N (3), (iv) nucleophilic substitution of 3 with Na2Fe(CO)4 followed by treatment of the resulting Fe(0) intermediate Na[(2-CH2-6-MeOCH2OC5H3N)Fe(CO)4] (M1) with I2 to give complex 4, and (v) condensation of 4 with KSCN and PhCS2K to give complexes 5 and 6, respectively. In contrast to the preparation of complexes 4-6, bidentate 2-acylmethyl-6-methoxymethoxy-difunctionalized pyridine-containing model complexes η(2)-(2-COCH2-6-MeOCH2OC5H3N)Fe(CO)2(I)(L2) (7, L2 = PPh3; 8, Cy-C6H11NC) and η(2)-(2-COCH2-6-MeOCH2OC5H3N)Fe(CO)2(L3) (9, L3 = 2-SC5H4N; 10, 8-SC9H6N) were prepared by ligand exchange reactions of 4 with PPh3, Cy-C6H11NC, 2-KSC5H4N, and 8-KSC9H6N, respectively. Particularly interesting is that the tridentate 2,6-bis(acylmethyl)pyridine- and 2-acylmethyl-6-arylthiomethylpyridine-containing model complexes η(3)-[2,6-(COCH2)2C5H3N]Fe(CO)2(L4) (11, L4 = PPh3; 12, CO) and η(3)-2-(COCH2-6-ArSCH2C5H3N)Fe(CO)2(ArS) (13, ArS = PhS; 14, 2-S-5-MeC4H2O) were obtained, unexpectedly, when 2,6-(TsOCH2)2C5H3N reacted with Na2Fe(CO)4 followed by treatment of the resulting mixture with ligands PPh3 and CO or disulfides (PhS)2 and (2-S-5-MeC4H2O)2.
View Article and Find Full Text PDFNovel angiotensin II receptor type 1 (AT1) blockers bearing 6-substituted carbamoyl benzimidazoles with a chiral center were designed and synthesized as the first step to develop new antihypertensive agents and understand their pharmacodynamic and pharmacokinetic properties. The newly synthesized compounds were tested for their potential ability to displace [(125)I] Sar(1) Ile(8)-Ang II, which was specifically bound to human AT1 receptor. Radioligand binding assays revealed nanomolar affinity in several compounds under study.
View Article and Find Full Text PDFBoth 6-substituted aminocarbonyl and acylamino benzimidazole derivatives were designed and synthesized as nonpeptidic angiotensin II AT₁ receptor antagonists. Compounds 6f, 6g, 11e, 11f, 11g, and 12 showed nanomolar AT₁ receptor binding affinity and high AT₁ receptor selectivity over AT₂ receptor in a preliminary pharmacological evaluation. Among them, the two most active compounds 6f (AT₁ IC₅₀ = 3 nM, AT₂ IC₅₀ > 10,000 nM, PA₂ = 8.
View Article and Find Full Text PDFObjective: To investigate the prevalence of benign prostatic hyperplasia (BPH) in Pingliang City of Gansu Province.
Methods: We performed a cross-sectional randomized study of 836 men aged > or = 40 years from 26 communities of Pingliang, obtained their IPSS, measured the prostate volume by transabdominal ultrasonography, recorded the maximum flow (Qmax) by uroflowmetry, and processed the data by one-way analysis of variance.
Results: Totally 820 subjects meeting the study criteria were included in the investigation.
Usually, secreted or transmembrane proteins complete their three-dimension folding within endoplasmic reticulum (ER). Under the conditions of nutrient depletion, cell differentiation, or other stress statuses, misfolded or unfolded proteins aggregate within ER, and consequently cause ER stress and Unfolded Protein Response (UPR). In response to ER stress, BiP (Binding immunoglobulin protein) dissociates with IRE1a (Inositol-requiring kinase 1) and binds to unfolded proteins as a molecular chaperone in helping maintain their correct structure.
View Article and Find Full Text PDFGuang Pu Xue Yu Guang Pu Fen Xi
August 2012
After microwave digestion, 16 elements in pine pollen were simultaneously determined by TXRF. The results show that all the 16 elements were found in all pine pollens. There was a significant difference in the average content of the element such as Ca, Ti, Mn, Zn and Rb between different groups of pine pollen (P < or = 0.
View Article and Find Full Text PDFA series of 6-substituted carbamoyl benzimidazoles were designed and synthesised as new nonpeptidic angiotensin II AT(1) receptor antagonists. The preliminary pharmacological evaluation revealed a nanomolar AT(1) receptor binding affinity for all compounds in the series, and a potent antagonistic activity in an isolated rabbit aortic strip functional assay for compounds 6f, 6g, 6h and 6k was also demonstrated. Furthermore, evaluation in spontaneous hypertensive rats and a preliminary toxicity evaluation showed that compound 6g is an orally active AT(1) receptor antagonist with low toxicity.
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