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Molecular Pharmaceutics Jul 2024Prostate-specific membrane antigen (PSMA) overexpressed in prostate cancer cells can serve as a target for imaging and radioligand therapy (RLT). Previously,...
Prostate-specific membrane antigen (PSMA) overexpressed in prostate cancer cells can serve as a target for imaging and radioligand therapy (RLT). Previously, [Ga]Ga-P16-093, containing a Ga(III) chelator, ,'-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-,'-diacetic acid (HBED-CC), displayed excellent PSMA-targeting properties and showed a high tumor uptake and retention useful for diagnosis in prostate cancer patients. Recently, [Lu]Lu-PSMA-617 has been approved by the U.S. food and drug administration (FDA) for the treatment of prostate cancer patients. Derivatives of PSMA-093 using AAZTA (6-amino-6-methylperhydro-1,4-diazepinetetraacetic acid), as the chelator, were designed as alternative agents forming complexes with both diagnostic and therapeutic radiometals, such as gallium-68 (log = 22.18) or lutetium-177 (log = 21.85). The aim of this study is to evaluate AAZTA-Gly--(methylcarboxy)-Tyr-Phe-Lys-NH-CO-NH-Glu (designated as AZ-093, ) leading to a gallium-68/lutetium-177 theranostic pair as potential PSMA targeting agents. Synthesis of the desired precursor, AZ-093, , was effectively accomplished. Labeling with either [Ga]GaCl or [Lu]LuCl in a sodium acetate buffer solution (pH 4-5) at 50 °C in 5 to 15 min produced either [Ga]Ga- or [Lu]Lu- with high yields and excellent radiochemical purities. Results of binding studies, cell uptake, and retention (using PSMA-positive prostate carcinoma cells line, 22Rv1-FOLH1-oe) were comparable to that of [Ga]Ga-P16-093 and [Lu]Lu-PSMA-617, respectively. Specific cellular uptake was determined with or without the competitive blocking agent (2 μM of "cold" PSMA-11). Cellular binding and internalization showed a time-dependent increase over 2 h at 37 °C in the PSMA-positive cells. The cell uptakes were completely blocked by the "cold" PSMA-11 suggesting that they are competing for the same PSMA binding sites. In the mouse model with implanted PSMA-positive tumor cells, both [Ga]Ga- and [Lu]Lu- displayed excellent uptake and retention in the tumor. Results indicate that [Ga]Ga/[Lu]Lu- (Ga]Ga/[Lu]Lu-AZ-093) is potentially useful as PSMA-targeting agent for both diagnosis and radiotherapy of prostate cancer.
Topics: Male; Humans; Prostatic Neoplasms; Gallium Radioisotopes; Lutetium; Antigens, Surface; Radiopharmaceuticals; Glutamate Carboxypeptidase II; Cell Line, Tumor; Radioisotopes; Animals; Chelating Agents; Prostate-Specific Antigen; Tissue Distribution; Mice; Edetic Acid; Positron Emission Tomography Computed Tomography
PubMed: 38856975
DOI: 10.1021/acs.molpharmaceut.4c00020 -
Environmental Science and Pollution... Jun 2024
Comments on "Accuracy of rapid emergency medicine score and sequential organ failure assessment score in predicting acute paraphenylenediamine poisoning adverse outcomes" by El-Sarnagawy, Ghada et al., 10.1007/s11356-022-24427-1.
Topics: Humans; Phenylenediamines; Organ Dysfunction Scores; Poisoning
PubMed: 38856852
DOI: 10.1007/s11356-024-33936-0 -
International Journal of Paediatric... Jun 2024Parental perceptions of staining due to silver diamine fluoride (SDF) could affect its utilization in paediatric dentistry. This study represents the second part of a...
BACKGROUND
Parental perceptions of staining due to silver diamine fluoride (SDF) could affect its utilization in paediatric dentistry. This study represents the second part of a wider project focused on SDF esthetic acceptability among Italian parents.
AIM
To evaluate parental acceptance of SDF staining in Italy and to assess whether the parent's level of acceptance depends on location, child's behavior, or demographic background.
DESIGN
A cross-sectional study was conducted among Italian parents of children attending two university dental clinics. We used a validated Italian version of the questionnaire "Parental Perceptions of Silver Diamine Fluoride Dental Color Changes."
RESULTS
Two hundred and thirty-four parents took part in the survey. Of parents, 65.4% considered the staining on posterior teeth esthetically "acceptable" or "somewhat acceptable," and 19.3% on anterior teeth (p = .001). In a scenario of positive cooperation, 48.5% of parents were "somewhat likely" or "very likely" to choose SDF to treat posterior teeth, and 17.6% on anterior teeth (p = .001). Level of acceptance increased as the difficulty the child would experience to receive conventional treatment increased.
CONCLUSION
Staining on posterior teeth is more acceptable to parents than staining on anterior teeth. Level of acceptance on anterior teeth increases when sedation or general anesthesia is the alternative for the child.
PubMed: 38853387
DOI: 10.1111/ipd.13226 -
Journal of the American Chemical Society Jun 2024Aminoboronic acids represent a class of significant compounds that have attracted significant attention in the fields of drug discovery and organic synthesis. Despite...
Aminoboronic acids represent a class of significant compounds that have attracted significant attention in the fields of drug discovery and organic synthesis. Despite notable progress in their synthesis, the efficient construction of chiral β-aminoboronic acids with alkyl side chains remains a challenging endeavor. Here, we introduce an unprecedented nickel-catalyzed asymmetric borylalkylation of enamides, employing a simple chiral diamine ligand, readily available Bpin, and alkyl halides as coupling partners. This reaction serves as an efficient platform for assembling a diverse range of β-aminoboronic acid derivatives with flexible alkyl side chains, displaying exceptional regio-, stereo-, and enantioselectivities. Moreover, this transformation exhibits a broad substrate scope and remarkable tolerance toward various functional groups. Theoretical calculations demonstrate that the benzyl group on the ligand is the key to the high enantiocontrol in this transformation. Additionally, we exemplify the practical application of this strategy through the concise synthesis of complex bioactive molecules.
PubMed: 38853359
DOI: 10.1021/jacs.4c03700 -
Si-doped carbonized polymer dot as robust hydrophilic coating using for high efficiency antifogging.Journal of Colloid and Interface Science Jun 2024Hydrophilic coating can prevent surface from fogging but its application is limited by low mechanical performance. In this study, a hydrophilic coating was prepared by...
Hydrophilic coating can prevent surface from fogging but its application is limited by low mechanical performance. In this study, a hydrophilic coating was prepared by crosslinking the Si-doped carbonized polymer dot (Si-CPD) with 3-glycidyloxypropyltrimethoxysilane (GPTMS) and ethylene oxide (EO). The hydrophilic coating can be used as robust hydrophilic anti-fogging coating. The Si-CPD derived from ethylene diamine tetraacetic acid (EDTA) and aminopropyl oligosiloxanes (APOS) was successfully prepared via one-step hydrothermal method. Then, a resin solution was prepared by mixing Si-CPD, GPTMS and EO. Epoxy group of GPTMS and EO can react with amino group of Si-CPD. Finally, a composite coating with antifogging function can be obtained by simple heating curing. Due to the introduction of hydroxyl which derived from EO, the coating shows excellent antifogging performance. Meanwhile, the presence of inorganic component endows the coating with outstanding mechanical performance. The coating has great potential in related applications, such as optical lenses, mirrors and other transparency substrates.
PubMed: 38852350
DOI: 10.1016/j.jcis.2024.06.012 -
Amino Acids Jun 2024Periodontitis is an inflammatory condition of supporting structures of teeth leading to attachment and bone loss. Cigarette smoking is the single most important and...
Periodontitis is an inflammatory condition of supporting structures of teeth leading to attachment and bone loss. Cigarette smoking is the single most important and modifiable risk factor with 5 to 20-fold susceptibility for periodontal diseases. Reverse smoking is a peculiar habit of smoking where the lit end is kept inside the mouth, which is predominant in the northern coastal districts of Andhra Pradesh. Polyamines are biologically active amines involved in tissue regeneration and modulation of inflammation. The study aimed to evaluate polyamines and check their utility as a marker in detection of periodontitis among different groups. Total polyamine levels showed significant increase in reverse smokers with periodontitis when compared to the other groups. Qualitative analysis by thin layer chromatography showed three polyamine bands with varying intensity among the different groups. Mass spectrometric and NMR analyses of the three bands identified them as N1, N8-diacetyl spermidine, N-acetyl cadaverine and lysine. Most significantly elevated levels of lysine was observed in the smoker and reverse smoker periodontitis groups when compared to healthy and non-smoker periodontitis groups. The significantly elevated levels of N-acetyl cadaverine could be responsible for the more destruction of periodontium in the reverse smoker group. Antioxidant potential decreased significantly in different smoker periodontitis groups. The present study suggests that the quantitative analysis of salivary polyamines, lysine and N-acetyl cadaverine can aid as an easy noninvasive diagnostic method for assessing the periodontal status, especially in smokers.
Topics: Humans; Periodontitis; Cadaverine; Biomarkers; Lysine; Adult; Male; Smokers; Female; Middle Aged; Smoking; Saliva
PubMed: 38851640
DOI: 10.1007/s00726-024-03396-4 -
Journal of Environmental Management Jul 2024Conventional methods of metal recovery involving solvents have raised environmental concerns. To address these concerns and promote sustainable resource recovery, we...
Conventional methods of metal recovery involving solvents have raised environmental concerns. To address these concerns and promote sustainable resource recovery, we explored the use of deep eutectic solvents (DES) and chelating agents (CA) as more environmentally friendly alternatives. Goethite and blast oxide slag dust (BOS-D) from heap piles at their respective sites and characterised via ICP-MS. The greatest extraction of critical metals was from goethite, removing 38% of all metals compared to 21% from the blast oxide slag. Among the tested CA, nitrilotriacetic acid (NTA) was the most effective, while for DES, choline chloride ethylene glycol (ChCl-EG) demonstrated superior performance in extracting metals from both blast oxide slag dust and goethite. The study further highlighted the selectivity for transition metals and metalloids was influenced by the carboxyl groups of DES. Alkaline metals and rare earth lanthanides extractions were favoured with DES due to improved mass transfer and increased denticity, respectively. In comparison to ethylenediaminetetraacetic acid (EDTA), typically used for metal extraction, CA and DES showed comparable extraction efficiency for Fe, Cu, Pb, Li, Al, Mn, and Ni. Using these greener chelators and solvents for metal extraction show significant promise in enhancing the sustainability of solvometallurgy. Additional conditions e.g., temperature and agitation combined with a cascading leaching process could further enhance metal extraction potential.
Topics: Chelating Agents; Edetic Acid; Metals; Deep Eutectic Solvents; Solvents
PubMed: 38850901
DOI: 10.1016/j.jenvman.2024.121350 -
Environmental Science & Technology Jun 2024Wet-chemically recovering phosphorus (P) from sewage sludge incineration ash (SSIA) has already become a global initiative to address P deficit, but effectively...
Wet-chemically recovering phosphorus (P) from sewage sludge incineration ash (SSIA) has already become a global initiative to address P deficit, but effectively isolating P from these accompanying metals (AMs) through adsorption in a SSIA-derived extract remains elusive. Here, we devised a hydrothermal stimulus-motivated thermodynamic and kinetic enhancement to gain anionic ethylenediaminetetraacetic acid (EDTA) molecular interfaces for AM enclosure to resolve this conundrum. A new dosage rule based on the EDTA coordination ratio with AMs was established for the first time. Upon hydrothermal extraction at 140 °C for 1 h, the P extraction efficiency reached 96.7% or higher for these obtained SSIA samples, and then exceptional P sequestration from these EDTA-chelated AMs was realized by the peculiar lanthanum (La)-based nanoadsorbent (having 188.86 mg P/g adsorbent at pH ∼ 3.0). Relevant theoretical calculations unraveled that these delocalized electrons of tetravalent EDTA molecules boosted the enclosure of liberated AMs, thereby entailing a substantially increased negative adsorption energy (-408.7 kcal/mol) of P in the form of HPO through intruding lattice-edged carbonates to coordinate La with monodentate mononuclear over LaCO(1 0 1). This work highlights the prospect of molecular adaptation of these common extractants in wet-chemical P recovery from various P-included wastes, further sustaining global P circularity.
Topics: Phosphorus; Incineration; Sewage; Adsorption; Electrons; Edetic Acid
PubMed: 38850558
DOI: 10.1021/acs.est.4c03290 -
Clinical Oral Investigations Jun 2024Currently, premixed putty-type bioceramic cements (PPBCs) have become popular materials for root-end fillings. This study investigated three root-end filling techniques...
OBJECTIVES
Currently, premixed putty-type bioceramic cements (PPBCs) have become popular materials for root-end fillings. This study investigated three root-end filling techniques using PPBCs and calcium silicate-based sealers including EDTA pretreatment.
MATERIALS AND METHODS
Ninety root segments were prepared and standardized with an artificial fin and lateral canal, and assigned to three groups (n = 30). Root-end fillings were placed using BC-RRM Putty alone (Group PA), injection of BC sealer followed by BC-RRM Putty (Lid Technique: Group LT) or BC-RRM Putty with BC sealer coating (Deep putty packing technique: Group DP). Half of each group was pretreated with 17% EDTA. The radiographic images of the specimens were assessed by five graders and push-out bond strength tests were conducted. The data were analyzed with a general linear model including two-way ANOVA and chi-square test at a significance level of 5%.
RESULTS
DP approach demonstrated significantly higher bond strength than LT (P < 0.05). However, there was no statistically significant difference in bond strength between PA and either DP or LT. EDTA pretreatment had no significant effect on push-out bond strength. Radiographically, for the main canal, PA and DP scored significantly higher than LT. In the fin, PA scored significantly higher than others (P < 0.05).
CONCLUSION
Our study highlights variations in root-end filling techniques. Injecting a bulk of bioceramic sealer before the placement of PPBCs may reduce bond strength and radiopacity. The application of PPBCs alone or in the deep putty technique demonstrates potential for favorable outcomes. EDTA pretreatment did not enhance bond-strength.
CLINICAL RELEVANCE
Careful selection and application of bioceramic materials and techniques in root-end fillings may influence the outcome of endodontic root-end surgery. When PPBCs and calcium silicate-based sealers are used together for root-end fillings, sealer followed by deep putty application may offer improved bond strength and radiographic fill compared to the lid technique.
Topics: Root Canal Filling Materials; Silicates; Materials Testing; Calcium Compounds; In Vitro Techniques; Humans; Dental Bonding; Ceramics; Dental Cements; Retrograde Obturation; Edetic Acid; Dental Stress Analysis
PubMed: 38849637
DOI: 10.1007/s00784-024-05759-3 -
Heliyon Jun 2024Shenfu (SF) injection, a traditional Chinese medication, would improve microcirculation in cardiogenic shock and infectious shock. This study was aimed to explore the...
BACKGROUND
Shenfu (SF) injection, a traditional Chinese medication, would improve microcirculation in cardiogenic shock and infectious shock. This study was aimed to explore the therapeutic potential of the SF injection in gut ischemia-reperfusion (I/R) injury after severe hemorrhagic shock (SHS) and resuscitation. Furthermore, we also investigated the optimal adm? inistration timing.
METHODS
Twenty-four male SD rats were randomly divided into four groups: Sham group (sham, n = 6), Control group (n = 6), SF injection group (SF, n = 6), and Delayed Shenfu injection administration group (SF-delay, n = 6). In SHS and resuscitation model, rats were induced by blood draw to a mean arterial pressure (MAP) of 40 ± 5 mmHg within 1 h and then maintained for 40 min; HR, MAP 'were recorded, microcirculation index [De Backer score, perfused small vessel density (PSVD), total vessel density (TVD), microcirculation flow index score (MFI), flow heterogeneity index (HI)] were analyzed. The blood gas index was detected, interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), diamine oxidase (DAO), malondialdehyde (MDA) were measured by ELISA; ZO-1, and claudin-1 were measured by Western blotting. In addition, hematoxylin-eosin (HE) and periodic acid schiff (PAS) staining pathological sections of the intestinal mucosal tissues were also performed.
RESULTS
SF injection increased the MAP, relieved the metabolic acidosis degree associated with the hypoperfusion, and improved the intestinal microcirculatory density and perfusion quality after I/R injury. The expression of DAO, MDA in intestinal tissue, and plasma IL-6, TNF-α significantly decreased in the SF injection group compared to the control group. The concentration of ZO-1 and claudin-1 is also higher in the SF injection group. In addition, the HE and PAS staining results also showed that SF injection could decrease mucosal damage and maintain the structure. In the SF-delay group, the degree of intestinal tissue damage was intermediate between that of the control group and SF injection group.
CONCLUSIONS
SF injection protect the intestine from I/R injury induced by SHS and resuscitation, the mechanism of which might be through improving intestinal microcirculation, reducing the excessive release of inflammatory factors and increasing intestinal mucosal permeability. Furthermore, the protection effect is more pronounced if administration during the initial resuscitation phase.
PubMed: 38845930
DOI: 10.1016/j.heliyon.2024.e31377