Overview of epigenetic degraders based on PROTAC, molecular glue, and hydrophobic tagging technologies

Epigenetic pathways play a critical role in the initiation, progression, and metastasis of cancer. Over the past few decades, significant progress has been made in the development of targeted epigenetic modulators (e.g., inhibitors). However, epigenetic inhibitors have faced multiple challenges, including limited clinical efficacy, toxicities, lack of subtype selectivity, and drug resistance. As a result, the design of new epigenetic modulators (e.g., degraders) such as PROTACs, molecular glue, and hydrophobic tagging (HyT) degraders has garnered significant attention from both academia and pharmaceutical industry, and numerous epigenetic degraders have been discovered in the past decade. In this review, we aim to provide an in-depth illustration of new degrading strategies (2017-2023) targeting epigenetic proteins for cancer therapy, focusing on the rational design, pharmacodynamics, pharmacokinetics, clinical status, and crystal structure information of these degraders. Importantly, we also provide deep insights into the potential challenges and corresponding remedies of this approach to drug design and development. Overall, we hope this review will offer a better mechanistic understanding and serve as a useful guide for the development of emerging epigenetic-targeting degraders.

Raman Spectroscopy of six explanted acrylic hydrophobic foldable intraocular lenses with glistening

Purpose: To study and interpret Raman spectra of six explanted acrylic hydrophobic foldable intraocular lenses (HFIOLs) with grade six microvacuoles and to understand the possible mechanism for microvacuole formation. Methods: Clinical data, slit-lamp photographs, and optical microphotographs of the explanted analytes were obtained. RS of the analytes were registered using a confocal Raman microscope (Lab RAM HR Evolution, Horiba Jobin Yvon) and Horiba Lab Space 6 Spectroscopy Suite software. Data were interpreted by identifying the functional group and fingerprint region of the spectra about the available literature. Results: IOLs were explanted for visual impairment after an average interval of 11.2 years following implantation. Each of the HFIOLs exhibited distinctive and identical Raman bands at the frequency range of 200–1,800, 2,600–3,000, and 3,200–3,700 cm?1 which were identified with those reported in the literature. The unique bands and peaks of the spectra were specific to the functional groups, its ring and other stretching variations, hydroxyl group, and water molecule. A spike at 1,640 cm?1 revealed the presence of monomer and indicated material bioincompatibility of the samples. Conclusion: Raman spectroscopy (RS) was found specific and an effective tool to detect the material change in the HFIOL and constituents of polymer biomaterial about microvacuole formation and also suggested modification and development of a more biocompatible and non-biodegradable polymer blend where RS could be a monitoring tool.

Research progress of superhydrophilic implants / 中国基层医药

In the past few decades, some studies reported that changing the specific surface properties of titanium implants, such as surface morphology, surface chemistry, surface charge and wettability, improved the bone bonding ability of titanium implants. Based on the existing evidence, this review paper analyzes the methods and characteristics of surface chemical modification of the superhydrophilic implants (Thommen INICELL?) that were listed in China in recent years, and clarifies the process of early osseointegration from the viewpoint of histomorphology, and evaluates its clinical application effects.

Long-chain alkanol-alkyl carboxylic acid-based low-viscosity hydrophobic deep eutectic solvents for one-pot extraction of anthraquinones from Rhei Radix et Rhizoma / 药物分析学报

Natural long-chain alkanol and alkyl carboxylic acid were used to prepare novel hydrophobic deep eutectic solvents(HDESs).These HDESs are liquid at room temperature and have low viscosity(＜12.26 mPa-s),low polarity(lower than that of methanol,ChCl-based deep eutectic solvents and other reported HDESs),and low density(＜0.928 g/mL).A simple one-pot method based on a novel HDES-water two-phase extraction system was constructed for the extraction of weak-polarity bioactive components,anthraquinones,from Rhei Radix et Rhizoma.This HDES-based new extraction method does not consume hazardous organic solvents and can obtain a total anthraquinone yield of 21.52 mg/g,which is close to that obtained by the Chinese pharmacopoeia method(21.22 mg/g)and considerably higher than those by other reported HDESs-based extraction methods(14.20-20.09 mg/g,p＜0.01).The high extraction yield can be mainly attributed to the severe destruction of the RRR cell walls by the extraction system and the excellent dissolving ability of novel HDESs for anthraquinones.

Molecular design, pharmacology and toxicology optimization of antimicrobial peptide from Hydrophis cyanocinctus, Hc-CATH / 生物工程学报

Based on the cathelicidin family antimicrobial peptide Hc-CATH derived from sea snake, the Hc-16 and Hc-15 of 16 and 15 amino acid residues, were designed. By using CCK8, minimal inhibitory concentration, ELISA and bio-layer interferometry assays, their cytotoxicity, antibacterial activity, anti-inflammatory activity, and LPS neutralization activity was examined. Compared with Hc-15, Hc-16 had lower cytotoxicity and better broad-spectrum antibacterial activity against pathogens including clinically resistant bacteria, with the minimum inhibitory concentration of only 4.69 μg/mL. Hc-16 inhibited the expression of inflammatory cytokines of TNF-α and IL-6 induced by LPS, so as to significantly reduce the inflammatory response induced by infection. In addition, structure-activity relationship studies have shown that the phenylalanine at the C- and N-terminals of Hc-16 played a crucial role in its antibacterial and anti-inflammatory activity. Altogether, the designed Hc-16 has an excellent prospect to be developed into a novel antibiotic.

Caracterização da matéria orgânica dissolvida em processos de tratamento de água para consumo humano usando fracionamento rápido / Characterization of dissolved organic matter in drinking water treatment processes using rapid fractionation

RESUMO Matéria orgânica natural (MON) é uma complexa matriz de compostos orgânicos originados de fontes naturais que estão presentes em corpos hídricos. A MON é comprovada precursora de subprodutos da desinfecção (SPD), além de afetar processos de tratamento de água, tais como a coagulação, a desinfecção, a oxidação, a adsorção em carvão ativado e a filtração em membranas. Por essas razões, a redução da MON no tratamento de água para consumo humano é importante. Vários métodos são usados para caracterizar e quantificar a MON, tais como adsorção em resinas e parâmetros de massa. Carbono orgânico total (COT), carbono orgânico dissolvido (COD), absorção na região do ultravioleta (UV254) e absorbância específica de luz ultravioleta (AEUV) são usualmente utilizados como parâmetros de massa. O fracionamento rápido é uma técnica que usa diferentes resinas para separar frações da MON. Nesse contexto, este trabalho teve como objetivo geral caracterizar a matéria orgânica dissolvida (MOD) em processos de tratamento de água para consumo humano usando o método do fracionamento rápido e os parâmetros COD, UV254 e AEUV. Também foram analisados as variáveis turbidez, cor, pH e alcalinidade. Foram avaliados os efeitos dos processos de coagulação, sedimentação, filtração e adsorção em carvão ativado nas frações que formam a MON. Ácidos muito hidrofóbicos (AMH) constituíram a principal fração da MOD na água estudada, havendo redução de 89% entre a água bruta e o efluente do filtro de carvão ativado granular (CAG). A segunda fração predominante foi de ácidos levemente hidrofóbicos (ALH), reduzidos em 83% ao longo do tratamento. Na água bruta, as frações de matérias hidrofílicas carregadas (MHC) e de neutras (MHN) apresentaram concentrações de 0,11 mg L-1 e 0,04 mg L-1, não sendo removidas pelo tratamento.

ABSTRACT Natural organic matter (NOM) is a complex matrix of organic compounds originated from natural sources that are present in water bodies. NOM is a known precursor of disinfection by-products (DBP) and affects drinking water treatment processes such as coagulation, disinfection, oxidation, activated carbon adsorption, and membrane filtration. For these reasons, the reduction of NOM in water treatment is important. Several methods are used to characterize and quantify NOM, such as resin adsorption and mass parameters. The latter include total organic carbon (TOC), dissolved organic carbon (DOC), ultraviolet absorption at 254 nm (UV254), and specific UV absorption (SUVA). Rapid fractionation is a technique that uses different resins to separate NOM fractions. The objective of this study was to characterize dissolved organic matter (DOM) in drinking water treatment processes using rapid fractionation and the parameters DOC, UV254, and SUVA. Turbidity, color, pH, and alkalinity were also analyzed. The effects of coagulation, sedimentation, filtration, and adsorption processes on the fractions forming the NOM were evaluated. Very hydrophobic acids (VHA) constituted the main fraction of DOM in the studied water, with a reduction of 89% between raw water and granular activated carbon filter (GAC) respect to raw water. The second predominant fraction consisted of slightly hydrophobic acids (SHA), reduced by 83% throughout the treatment processes. In raw water, the hydrophilic charged (MHC) and neutral (MHN) fractions showed concentrations of 0.11 and 0.04 mg L-1, which were not removed during treatment.

Posterior capsule opacification after cataract surgery in children over five years of age with square-edge hydrophobic versus hydrophilic acrylic intraocular lenses: a prospective randomized study

OBJECTIVE: To compare the effects of hydrophobic and hydrophilic materials in square-edged acrylic intraocular lenses (IOLs) on the development of posterior capsule opacification (PCO) after pediatric cataract surgery. METHODS: Patients were randomly assigned to group 1 (hydrophobic acrylic square-edged IOLs; 13 eyes) or group 2 (hydrophilic acrylic square-edged IOLs; 13 eyes). The study evaluated PCO rates using Evaluation of Posterior Capsule Opacification (EPCO) 2000 software at one, three, six and 12 months postoperatively. Postoperative measurements also included corrected distance visual acuity (CDVA), neodymium:yttrium‐aluminum‐garnet (Nd:YAG) capsulotomy and postoperative complications other than PCO. RESULTS: Both groups had significant increases in PCO rates after one year. Comparison of the groups showed no significant differences in the EPCO scores at three (group 1, 0.007±0.016 vs group 2, 0.008±0.014; p=0.830), six (group 1, 0.062±0.103 vs group 2, 0.021±0.023; p=0.184), or twelve months postoperatively (group 1, 0.200±0.193 vs group 2, 0.192±0.138; p=0.902). We also found no significant group differences regarding the change (delta, Δ) in EPCO scores between three and six months (group 1, 0.055±0.09 vs group 2, 0.013±0.02; p=0.113) or between six and twelve months postoperatively (group 1, 0.139±0.14 vs group 2, 0.171±0.14; p=0.567). Twenty-three percent of patients required Nd:YAG capsulotomy at the twelve-month visit. CONCLUSIONS: No differences in PCO rates were found between hydrophobic and hydrophilic acrylic square-edged IOLs in children between five and twelve years of age at one year of follow-up.

Microtensile Bond Strength and Failure Type Analysis of Self-Etch Adhesive Systems on Superficial and Deep Dentin After Long-term Water Storage / Análise de resistência de adesão à microtração e tipo de falha de sistemas adesivos autocondicionantes em dentina superficial e profunda após armazenamento longitudinal em água

Objective: The aim of this study was to evaluate and compare the microtensile bond strengths of four current adhesive materials that contain different monomers at deep and superficial dentin. Material and Methods: Forty non-carious human third molars (n=5) were used in the study. Specimens were divided into two main groups according to dentin thickness as superficial and deep dentin. Groups were further divided into four subgroups in terms of the adhesive systems used: Nova Compo B Plus (NCBP), Nova Compo B (NCB), Futurabond M (FB) and Clearfil S3 Bond Plus (CS3). All specimens were bonded to resin composite and stored in 37 °C water for 9-months. Teeth were sectioned into 3 x 3 mm thick beams. Microtensile bond strength test was carried out by using a universal testing device (1 mm/min). After fracture, failure types were observed using an optical microscope and the fractured dentin surfaces were observed by a scanning electron microscopy (SEM). One-way ANOVA and Tukey tests were used to compare the adhesive system in each dentin group. An unpaired T-test was used to compare the dentin thickness in each adhesive material. Results: As compared to deep dentin, superficial dentin showed higher µTBS values in groups NCBP, FB and CS, as opposed to group NCB. Only NCB revealed higher bond strength at deep dentin layers when compared to superficial dentin. In the superficial dentin group, NCBP showed the highest bond strength value while NCB showed the lowest bond strength. In the deep dentin group, while NCB showed the highest bond strength value, NCBP revealed the lowest bond strength value after 9-months storage. While 4-META and 10-MDP monomer combination (NCBP) resulted in the highest bond strength value among the adhesive systems in the superficial dentin group, the GPDMA and 4-META monomer combination (NCB) resulted in the highest bond strength in deep dentin group. Conclusions: Microtensile bond strength performance are affected by both the type of monomer in the adhesive combination and the depth of the dentin. (AU)

Objetivo: o objetivo deste estudo foi avaliar e comparar a resistência de união à microtração de quatro materiais adesivos atuais que contêm monômeros diferentes na dentina profunda e superficial. Material e Métodos: Quarenta terceiros molares humanos não cariados (n = 5) foram usados no estudo. Os espécimes foram divididos em dois grupos principais de acordo com a espessura da dentina em superficial e profunda. Os grupos foram subdivididos em quatro subgrupos quanto aos sistemas adesivos usados: Nova Compo B Plus (NCBP), Nova Compo B (NCB), Futurabond M (FB) e Clearfil S3 Bond Plus (CS3). Todos os espécimes foram aderidos à resina composta e armazenados em água a 37 ° C por 9 meses. Os dentes foram seccionados em palitos de 3 x 3 mm de espessura. O teste de microtração foi realizado com o uso de um dispositivo de teste universal (1 mm / min). Após a fratura, os tipos de falha foram observados em microscópio óptico e as superfícies de dentina fraturadas por microscopia eletrônica de varredura (MEV). Os testes ANOVA e Tukey um fator foram usados para comparar o sistema adesivo em cada grupo de dentina. Um teste T não pareado foi usado para comparar a espessura da dentina em cada material adesivo. Resultados: Em comparação com a dentina profunda, a dentina superficial apresentou maiores valores de µTBS nos grupos NCBP, FB e CS, ao contrário do grupo NCB. Apenas NCB revelou maior resistência de união na dentina profunda quando comparada à dentina superficial. No grupo de dentina superficial, NCBP apresentou o maior valor de resistência de união, enquanto NCB apresentou a menor resistência de união. No grupo de dentina profunda, enquanto NCB apresentou o valor de resistência de união mais alto, NCBP revelou o valor de resistência de união mais baixo após 9 meses de armazenamento. Enquanto a combinação de monômero 4-META e 10-MDP (NCBP) resultou no maior valor de resistência de união entre os sistemas adesivos no grupo de dentina superficial, a combinação de monômero (NCB) resultou na maior força de união no grupo de dentina profunda. Conclusões: O desempenho da resistência de união à microtração é afetado tanto pelo tipo de monômero na combinação adesiva quanto pela profundidade da dentina. (AU)

Exploring the hydrophobic channel of NNIBP leads to the discovery of novel piperidine-substituted thiophene3,2-pyrimidine derivatives as potent HIV-1 NNRTIs

In this report, a series of novel piperidine-substituted thiophene[3,2-]pyrimidine derivatives were designed to explore the hydrophobic channel of the non-nucleoside reverse transcriptase inhibitors binding pocket (NNIBP) by incorporating an aromatic moiety to the left wing of the lead . The newly synthesized compounds were evaluated for anti-HIV potency in MT-4 cells and inhibitory activity to HIV-1 reverse transcriptase (RT). Most of the synthesized compounds exhibited broad-spectrum activity toward wild-type and a wide range of HIV-1 strains carrying single non-nucleoside reverse transcriptase inhibitors (NNRTI)-resistant mutations. Especially, compound exhibited the most potent activity against wild-type and a panel of single mutations (L100I, K103N, Y181C, Y188L and E138K) with an EC ranging from 6.02 to 23.9 nmol/L, which were comparable to those of etravirine (ETR). Moreover, the RT inhibition activity, preliminary structure-activity relationship and molecular docking were also investigated. Furthermore, exhibited favorable pharmacokinetics (PK) profiles and with a bioavailability of 33.8%. Taken together, the results could provide valuable insights for further optimization and compound holds great promise as a potential drug candidate for the treatment of HIV-1 infection.

Conversion of renewable substrates for biosurfactant production by Rhizopus arrhizus UCP 1607 and enhancing the removal of diesel oil from marine soil

BACKGROUND: The use of agro-industrial wastes to produce high value-added biomolecules such as biosurfactants is a promising approach for lowering the total costs of production. This study aimed to produce biosurfactants using Rhizopus arrhizus UCP 1607, with crude glycerol (CG) and corn steep liquor (CSL) as substrates. In addition, the biomolecule was characterized, and its efficiency in removing petroderivatives from marine soil was investigated. RESULTS: A 22 factorial design was applied, and the best condition for producing the biosurfactant was determined in assay 4 (3% CG and 5% CSL). The biosurfactant reduced the surface tension of water from 72 to 28.8 mN/m and produced a yield of 1.74 g/L. The preliminary biochemical characterization showed that the biosurfactant consisted of proteins (38.0%), carbohydrates (35.4%), and lipids (5.5%). The compounds presented an anionic character, nontoxicity, and great stability for all conditions tested. The biomolecule displayed great ability in dispersing hydrophobic substrates in water, thereby resulting in 53.4 cm2 ODA. The best efficiency of the biosurfactant in removing the pollutant diesel oil from marine soil was 79.4%. CONCLUSIONS: This study demonstrated the ability of R. arrhizus UCP1607 to produce a low-cost biosurfactant characterized as a glycoprotein and its potential use in the bioremediation of the hydrophobic diesel oil pollutant in marine soil

Caracterização interna de materiais restauradores indiretos com diferentes condicionamentos de superfície / Internal characterization of indirect restorative materials with different surface etching protocols

Objetivo: O objetivo do estudo foi avaliar o efeito da aplicação de ácido fluorídrico com diferentes tempos e concentrações na superfície de materiais restauradores indiretos obtidos a partir de blocos utilizados na tecnologia CAD-CAM. Materiais e Métodos: Amostras dos materiais restauradores indiretos medindo 4x4x0,8mm foram obtidos a partir de blocos CAD para cada material estudado: resina nanocerâmica Lava Ultimate (3M Espe), monossilicato de lítio reforçado por zircônia Celtra Duo (Dentsply) e cerâmica híbrida Vita Enamic (Vita). Os materiais foram submetidos à aplicação de ácido fluorídrico com concentração de 5% ou 10%, sendo o mesmo aplicado pelos tempos de 20, 40, 60 ou 90 segundos. Um grupo controle para cada material foi avaliado, sem nenhum tratamento de superfície, contabilizando nove grupos de cada material (n=10). As amostras foram avaliadas em relação à rugosidade de superfície (Ra e Rz), avaliadas em microscopia óptica confocal; ângulo de contato (θ), energia de superfície (s) e energia livre total de interação (∆G) avaliados em goniômetro, e resistência de união ao cimento resinoso avaliada através do teste de microcisalhamento. Imagens das amostras foram obtidas em microscopia eletrônica de varredura (MEV), microscopia óptica confocal e microscopia de força atômica. Os dados de rugosidade de superfície, ângulo de contato, energia de superfície, energia livre total de interação e resistência de união foram submetidos à ANOVA dois fatores e teste de Tukey (p<0,05). Resultados: Os resultados mostraram que, de maneira geral, o monosilicato de lítio reforçado por zircônia Celtra Duo apresentou melhores resultados quando submetido ao condicionamento com ácido fluorídrico 10% por 40 ou 60 segundos de aplicação. A resina nanocerâmica Lava Ultimate apresentou melhor performance quando condicionada com ácido fluorídrico 10% por 20 ou 40 segundos, enquanto que a cerâmica híbrida Vita Enamic apresentou melhores resultados quando condicionada com ácido fluorídrico 5% por 90 segundos. Conclusão: Cada material interagiu de maneira diferente ao condicionamento com ácido fluorídrico, sendo que o conhecimento do adequado protocolo para cada material é essencial para garantir melhorias nos processos de adesão e durabilidade das restaurações indiretas. Celtra Duo apresentou de maneira geral propriedades mecânicas superiores aos demais. Relevância clínica: Recomenda-se protocolos específicos de tratamento de superfície com ácido fluorídrico de acordo com a composição de cada material restaurador indireto(AU)

Purpose: The aim of this study was to evaluate the effect of different times and concentration of hydrofluoric acid etching on the surface of indirect restorative materials obtained from blocks used in CAD-CAM technology. Methods and Materials: Samples of indirect restorative materials measuring 4x4x0.8mm were obtained for each restorative material studied: Lava Ultimate nanoceramic resin (3M Espe), Celtra Duo zirconia-reinforced lithium silicate ceramic (Dentsply) and Vita Enamic polymer-infiltrated ceramic-network material (Vita). The materials were submitted to etching with 5% or 10% hydrofluoric acid for 20, 40, 60 or 90 seconds. A control group for each material was evaluated without any surface treatment, totaling nine experimental groups for each material (n = 10). The samples were evaluated in relation to surface roughness (Ra and Rz), evaluated by confocal optical microscopy; contact angle (θ), surface energy (s) and total free interaction energy (∆G) evaluated by goniometer; and microshear bond strength to resin cement. Sample images were obtained by scanning electron microscopy (SEM), confocal optical microscopy and atomic force microscopy. Data of surface roughness, contact angle, surface energy, total free interaction energy and bond strength were submitted to two-way ANOVA and Tukey test (p<0.05). Results: The results showed that, in general, the Celtra Duo zirconia-reinforced lithium silicate ceramic showed better results when subjected to etching with 10% hydrofluoric acid for 40 or 60 seconds. Lava Ultimate nanoceramic resin showed better performance when etched with 10% hydrofluoric acid for 20 or 40 seconds, while Vita Enamic polymer-infiltrated ceramic-network showed better results when etched with 5% hydrofluoric acid for 90 seconds. Conclusion: Each material showed different characteristics after etching with hydrofluoric acid, and the knowledge of the proper protocol for each material is essential to ensure improvements in the adhesion process and durability of indirect restorations. Celtra Duo presents general ways of mechanical properties superior to the others. Clinical relevance: Specific surface treatment protocols with hydrofluoric acid are recommended based on the different compositions of indirect restorative materials(AU)

Preparation of hydrophobic chitosan from Catharsius molossus and its hemostatic effect / 中草药

Objective To prepare hydrophobic chitosan from Catharsius molossus and study its hemostatic effect. Methods The chitosan from C. molossus was used as material to carry out hydrophobic modification and characterization by acylation with lauric anhydride. At the same time, the hemostatic effect was studied by in vitro agglutination test and mouse liver wound experiment. Results The prepared hydrophobic chitosan had a hydrophobic group substitution degree of (11.69 ± 0.14)%, which was higher than that of commercially available hydrophobic chitosan. The in vitro agglutination experiment showed that it could coagulate in (3.42 ± 0.39) s when mixed with blood at a concentration of 6.0 mg/g, which was better than chitosan and hydrophobically modified commercial chitosan. The mouse liver wound experiment showed that chitosan from C. molossus could shorten hemostatic time significantly compared with chitosan and hydrophobically modified commercial chitosan. Conclusion Hydrophobically modified chitosan can significantly improve the coagulation performance of chitosan, and the hydrophobic chitosan from C. molossus is excellent, and it is expected to be a new hemostatic material with great potential.

Intestinal uptake of barley protein-based nanoparticles for -carotene delivery

Our previous study introduced a barley protein microparticle for encapsulation of hydrophobic drug/nutraceutical, which could release nanoparticles upon gastric digestion and deliver encapsulated compound to a simulated intestinal environment intact. This work focused on evaluating the potential of liberated nanoparticles to improve the absorption of encapsulated compounds (., -carotene) using Caco-2 cell and small intestine models. Nanoparticles obtained from gastric digestion of barley protein microparticles had a spherical shape and an average size of 351 nm. Nanoparticles showed low cytotoxicity in Caco-2 cells and their cellular uptake was dependent on time, concentration and temperature. In a Caco-2 cell monolayer model, significantly greater uptake and transport of -carotene were observed when it was delivered by nanoparticles (15%), compared to free -carotene suspension (2.6%). In an rat jejunum model, nanoparticles showed the capacity to retain in small intestinal tissue. Approximately 2.24 and 6.04 μg nanoparticle were able to permeate through each cm intestinal tissue and translocate to the serosal side after 60 and 90 min, respectively. Results from this study demonstrated the absorption improving effect of the barley protein nanoparticles and suggested their potential as vehicles for hydrophobic compounds.

Adsorción de acetaminofén sobre carbones activados a diferente pH. Entalpía y entropía del proceso / Acetaminophen adsorption on activated carbons at different pH. Change of enthalpy and entropy of the process / Adsorção de acetaminofeno em carvões ativados a diferentes pH. Entalpia e entropia do processo

Resumen Se analizaron los cambios entálpicos y entrópicos derivados del proceso de adsorción de acetaminofén sobre carbones activados con química superficial modificada. Se realizó, además, una variación del pH para determinar los cambios en las propiedades termodinámicas cuando existen cargas en el adsorbato y en el adsorbente. Se encontró que la máxima capacidad de adsorción (1,172 mmoles g-1) corresponde al proceso llevado a cabo en el carbón activado denominado CAR en este estudio a pH 7; los valores de las funciones termodinámicas de entalpía de inmersión y entropía de adsorción fueron -36,02 J g-1 y 0,123 J g-1 K-1, respectivamente. Así, el cambio de entropía de adsorción para el acetaminofén en los carbones activados estudiados dependió del pH. Se encontró que esta función termodinámica varía en el siguiente orden pH 2 > pH 11 > pH 7. Este comportamiento se relaciona con el número de especies presentes en la solución capaces de interactuar con la superficie del carbón activado.

Abstract The enthalpic and entropic changes resulting from the process of acetaminophen adsorption on activated carbons with modified surface chemistry were studied. A pH variation was performed to determine the changes in the thermodynamic properties when there are charges in the adsorbate and adsorbent. It was found that the maximum adsorption capacity (1.172 mmoles g-1) corresponds to the process carried out in the activated charcoal labeled as CAR in this study at pH 7; the values of the thermodynamic functions immersion enthalpy and entropy of adsorption were -36.02 J g-1 and 0.123 J g-1 K-1, respectively. Thus, the adsorption entropy change for the acetaminophen on the activated carbons depended on the pH. It was found that this thermodynamic function varies in the following order pH 2 > pH 11 > pH 7. This behavior is related to the number of species present in the solution capable of interact with the activated carbon surface.

Resumo Foram analisadas as mudanças entrópicas e entalpicas resultantes do processo de adsorção de acetaminofeno sobre carvões activados com superfície química modificada. Além disso, foi realizada uma variação do pH para determinar as alterações nas propriedades termodinâmicas quando existem cargas no adsorbato e no adsorvente. Foi encontrado que a máxima capacidade de adsorção (1.172 mmol g-1) corresponde ao processo realizado no carvão ativado chamado CAR neste estudo em pH 7; os valores das funções termodinâmicas de entalpia de imersão e entropia de adsorção foram -36,02 J g-1 e 0,123 J g-1 K-1 respectivamente. As mudança da entropia de adsorção para o acetaminofeno nos carvões activados dependeu do pH. Foi encontrado que esta função termodinâmica varia na seguinte ordem pH 2 > pH 11 > pH 7. Este comportamento está relacionado ao número de espécies presentes na solução capaz de interagir com a superfície de carvão activado.

Influence of Implant Surface Coated with pH Buffering Agent on Early Osseointegration

PURPOSE: Surface treatment with pH buffering agent has been developed to achieve higher and faster osseointegration. The aim of this study was to evaluate its influence by measuring removal torque and analyzing histological characteristics. MATERIALS AND METHODS: Titanium implants with following surfaces were used in this study: sand-blasted acid-etched (SA) surface (SA group as control I group), SA surface in calcium chloride aqueous solution (CA group as control II group) and SA surface coated with pH buffering agent (pH group as test group). Removal torque test after 2 weeks and bone-to-implant contact and bone area analyses at 2 and 4 weeks were performed. RESULT: The rotational torque values at 2 weeks were significantly higher in pH group (107.5±6.2 Ncm, P < 0.05). The mean values of bone-to-implant contact at 2 and 4 weeks were both higher in pH group (93.0%±6.4% at 2 weeks, 88.6%±5.5% at 4 weeks) than in SA group (49.7%±9.7% at 2 weeks, 47.3%±20.1% at 4 weeks) and CA group (73.7%±12.4% at 2 weeks, 72.5%±10.9% at 4 weeks) with significances (P < 0.05). The means of bone area showed significantly higher numbers in pH group (39.5%±11.3% at 2 weeks, 71.9%±10.9% at 4 weeks, P < 0.05). CONCLUSION: Our findings demonstrated that surface modification with pH buffering agent improved early osseointegration with superior biomechanical property.

Comparison of polymethylmethacrylate versus hydrophobic acrylic lenses for primary intraocular lens implantation in pediatric cataract surgery / 国际眼科杂志(Guoji Yanke Zazhi)

@#AIM: To compare the visual results and postoperative complications of polymethylmethacrylate(PMMA)and hydrophobic acrylic intraocular lenses(IOLs)in children who underwent cataract extraction with primary IOL implantation.<p>METHODS:This retrospective study included 117 eyes of 63 children with bilateral pediatric cataract undergoing cataract surgery and primary IOL implantation. The patients were divided into two groups, Group I included 58 eyes of 30 patients with PMMA IOLs; Group II included 59 eyes of 33 patients with hydrophobic acrylic IOLs. The clinical features, refraction errors, best corrected visual acuity(BCVA)and surgical complications were compared between two groups.<p>RESULTS:The mean age at the time of surgery was 5.8(2-12)y and mean follow up period was 40.5(6-196)mo. Postoperatively, BCVA was ≥0.5 in 80 eyes(68.4%)and this was comparable in two groups. Visual axis opacification was seen in 28 eyes(48.3%)in Group I and 16 eyes(27.1%)in Group II and this difference was statistically significant(<i>P</i>=0.018). Postoperative IOL dislocation and posterior synechia formation were also noted. When all postoperative complications were considered, there were significantly less complications in the acrylic IOL group than PMMA IOL group(<i>P</i>=0.020).<p>CONCLUSION: Pediatric cataract surgery with primary IOL implantation is a safe procedure. Hydrophobic acrylic IOLs may lead to less postoperative complications compared to PMMA IOLs.

Preparation and evaluation of long-acting injectable formulations of memantine / 中国药科大学学报

@#:In order to improve the compliance of patients with Alzheimer′s disease and maintain the continuity of treatment by reducing administration frequency of memantine hydrochloride, a series of memantine long-acting nanosuspension-based injectable formulations were prepared using a hydrophobic salt formation method. Four hydrophobic salt forms of memantine were prepared, including memantine oleate(Mem-Ole), memantine stearate(Mem-Ste), memantine palmitate(Mem-Pal)and memantine pamoate(Mem-Pam). The salt forms of memantine were characterized using fourier transform infrared(FTIR)spectroscopy, proton nuclear magnetic resonance(1H NMR)spectroscopy and powder X-ray diffraction(PXRD)analysis. The equilibrium solubilities of different salt forms of memantine and the in vitro drug release of long-acting injectable formulations were investigated. In comparison with memantine alone, the equilibrium solubilities of Mem-Ole, Mem-Ste, Mem-Pal and Mem-Pam in simulated body fluid were decreased by 95. 1%、96. 2%、96. 7% and 99. 6%, respectively. Meanwhile, the equilibrium solubilities of Mem-Pam in simulated body fluid with pH ranging from 5 to 8 were all lower than 0. 07 mg/mL. The order of the in vitro drug release rate of the four long-acting injectable formulations with nanosuspensions of memantine was Mem-Ste> Mem-Pal≈Mem-Ole> Mem-Pam> Memantine. The Mem-Pam nanosuspensions could sustain drug release for seven days and exhibited a zero-order drug release profile(y=0. 549 9x+7. 594 2, r=0. 988 3). In conclusion, injectable Mem-Pam nanosuspensions showed desired drug release behavior and might potentially be applied in vivo for a week with a steady plasma drug concentration-time profile.

Molecular cloning and characterisation of scavenger receptor class B in pearl oyster Pinctada fuctada martensii

Background: Molluscs can accumulate carotenoids in their body tissues by predominantly feeding on aquatic plant sources. Carotenoid transport and absorption are determined by the regulation of various proteins such as Scavenger receptor class B(SR-BI). We report the identification and characterisation of pearl oyster Pinctada fuctada martensii SR-BI (PmSR-BI). The correlation between total carotenoid content (TCC) and gene expression was also estimated. Results: The full-length cDNA of PmSR-BI was 1828 bp, including an open-reading frame encoding of 1518 bp with a pI value of 5.83. PmSR-BI protein contains a hydrophobic CD36 domain and four centrally clustered cysteine residues for the arrangement of disulphide bridges. The deduced amino acid sequence had an identity of 30% to 60% with the SR-B of other organisms. Reverse transcription polymerase chain reaction analysis showed that mRNA transcripts were expressed in multiple tissues of adult pearl oyster. A higher expression of PmSR-BI gene was observed in the hepatopancreas than in the adductor muscle, gill and mantle. The TCC and gene expression of PmSR-BI were significantly correlated (P b 0.05), with a correlation coefficient of 0.978. Conclusions: The results suggested that PmSR-BI is involved in the absorption of carotenoids in the pearl oyster P. fuctada martensii.

Retrospective study of ocular complication following phacoemulsification with intraocular acrylic lens implantation in dogs / Estudo retrospectivo das complicações oculares em cães submetidos à facoemulsificação com implantação de lente acrílica

The aim of this study was to analyze for 120 days, post-operative complications following bimanual phacoemulsification with implantation of hydrophilic or hydrophobic intraocular acrylic lens. The hospital records of 15 dogs were analyzed, and distributed in two groups, being Gfi and Gfo the hydrophilic intraocular lens and hydrophobic intraocular lens group, respectively. On the first day, both groups presented blepharospasm, conjunctival hyperemia and flare. On day 1, fibrin was slightly apparent in two and three eyes of Gfi and Gfo, and on day 7, present in one and two patients from Gfi and Gfo. Synechia was observed on day 1 in one eye from Gfi and Gfo. Two eyes from Gfi developed from 7 to 120 days, and in Gfo, one eye developed from 7 to 90 days, on day 120, two eyes formed them. The presence of posterior capsule opacity of the lens in all periods, there was no statistical significant between the groups. Only one eye, in Gfo, that had no opacity formation. The intraocular pressure of both groups remained within normal range. There was no statistical significance between hydrophilic and hydrophobic intraocular lens, the use of intraocular lens has led to satisfactory results in visual ability.(AU)

Objetivou-se com o presente estudo avaliar por 120 dias as complicações após a facoemulsificação bimanual com implantação de lentes acrílicas hidrofílicas ou hidrofóbicas. Os prontuários de 15 cães foram avaliados, sendo distribuídos em dois grupos, Gfi e Gfo, grupos com lentes intraoculares hidrofílicas e com lentes hidrofóbicas, respectivamente. No primeiro dia, ambos os grupos apresentaram blefarospasmo, hiperemia conjuntiva e flare. No dia 1, fibrina foi discretamente observada em dois e três olhos do Gfi e Gfo; no dia 7, observou-se em um e três olhos nos pacientes do Gfi e Gfo. Foi observada sinéquia no dia 1 em um olho do Gfi e do Gfo; em dois olhos do Gfi ocorreu do dia 7 ao dia 120. No Gfo apenas um olho teve sinéquia do dia 7 ao dia 90, contudo aos 120 dias, dois olhos formaram-na. A opacidade de cápsula posterior da lente esteve presente em todos os períodos, não havendo diferença estatística entre os grupos. Somente um olho, do Gfo, não teve formação de opacidade. A pressão intraocular foi normal em ambos os grupos. Não houve diferença estatística entre as lentes hidrofílicas e hidrofóbicas. O uso de lentes intraoculares apresentaram resultados satisfatórios na acuidade visual.(AU)

Characterization of Lactobacillus fermentum UCO-979C, a probiotic strain with a potent anti-Helicobacter pylori activity

Background: Helicobacter pylori is considered as the main risk factor in the development of gastric cancer. In the present study, we performed a detailed characterization of the probiotic properties and the anti-H. pylori activity of a previously isolated lactobacillus strain ­ Lactobacillus fermentum UCO-979C ­ obtained from human gut. Results: The strain tolerated pH 3.0; grew in the presence of 2% bile salts; produced lactic acid and hydrogen peroxide; aggregated in saline solution; showed high hydrophobicity; showed high adherence to glass; Caco-2 and gastric adenocarcinoma human cells (AGS) cells; showed an efficient colonization in Mongolian Gerbils; and potently inhibited the growth and urease activity of H. pylori strains. L. fermentum UCO-979C significantly inhibited H. pylori-induced IL-8 production in AGS cells and reduced the viability of H. pylori. With regard to innocuousness, the strain UCO-979C was susceptible to several antibiotics and did not produce histamine or beta-haemolysis in blood agar containing red blood cells from various origins. Conclusion: The results demonstrated that L. fermentum UCO-979C is a very good candidate as a probiotic for the protection of humans against H. pylori infections.