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1.
J Mol Recognit ; 37(2): e3072, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38126580

RESUMEN

G-quadruplexes are important drug targets and get attention due to their existence in telomere, ribosomal DNA, promoter regions of some oncogenes, and the untranslated regions of mRNA. Due to the biological roles of G-quadruplexes, investigating of the G-quadruplex-small molecule interaction is essential. The primary motivation for these studies is the possibility of inhibiting cell functions associated with G-quadruplex sequences by binding with small molecules. Targeting the small molecules to desired tissue with the G-quadruplex vehicles is the second important goal of the G-quadruplex-small molecule interaction studies. In the present study, the new peripherally 2-mercaptopyridine octasubstituted copper(II) phthalocyanine and its quaternized derivative (CuPc) were synthesized and characterized by elemental analysis FT-IR, UV-Vis, and mass spectra. The excellent solubility of CuPc in water is essential for its transport in the organism. Because of this feature, its affinity toward G-quadruplex forming aptamers, AS1411, Tel21, and Tel45, was investigated. The UV-Vis spectrophotometric titration data confirmed the prevention of aggregation upon interaction with G-quadruplex, which is very important for biomedical applications. The CD spectroscopic analyses and binding stoichiometry confirmed the "end stacking" model for interaction of AS1411 with CuPc. The interaction of CuPc caused the equilibrium shift from hybrid conformation to antiparallel conformation for Tel21 and Tel45. The isothermal titration calorimeter (ITC) was used for the determination of thermodynamic parameters. The thermodynamic data of the interaction was fitted well with the one-site model. The negative values of Gibbs free energy change confirmed the spontaneous nature of the reactions. Besides, the negative values of enthalpy change and entropy change proved that the nature of processes was "enthalpy driven." The interaction stoichiometry was 2 for AS1411 and Tel21 and 1.5 for Tel45. The binding constants were 1.3(±0.3) × 105 , 3.2(±0.4) × 105 , and 1.1(±0.3) × 105 M-1 , which were at the level of ethidium bromide intercalation binding constant given in the literature. The DNA polymerase stop assay further supported the interaction of CuPc with G-quadruplex DNA. The experimental results confirm that the CuPc has a potential photosensitizer behaviour for photodynamic therapy.


Asunto(s)
G-Cuádruplex , Piridinas , Cobre , Sulfatos , Espectroscopía Infrarroja por Transformada de Fourier , Dicroismo Circular , Termodinámica , Telómero
2.
Calcif Tissue Int ; 114(4): 340-347, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38342790

RESUMEN

We aimed to investigate the relationship among probable sarcopenia, osteoporosis (OP) and supraspinatus tendon (SSP) tears in postmenopausal women. Postmenopausal women screened/followed for OP were recruited. Demographic data, comorbidities, exercise/smoking status, and handgrip strength values were recorded. Probable sarcopenia was diagnosed as handgrip strength values < 20 kg. Achilles and SSP thicknesses were measured using ultrasound. Among 1443 postmenopausal women, 268 (18.6%) subjects had SSP tears. Unilateral tears were on the dominant side in 146 (10.1%) and on the non-dominant side in 55 women (3.8%). In contrast to those without, women with SSP tears had older age, lower level of education, thinner SSP and lower grip strength (all p < 0.05). In addition, they had higher frequencies of hypertension, hyperlipidemia, DM, OP and probable sarcopenia, but lower exercise frequency (all p < 0.05). Binary logistic regression modeling revealed that age [odds ratio (OR): 1.046 (1.024-1.067 95% CI)], hypertension [OR: 1.560 (1.145-2.124 95% CI)], OP [OR: 1.371 (1.022-1.839 95% CI)] and probable sarcopenia [OR: 1.386 (1.031-1.861 95% CI)] were significant predictors for SSP tears (all p < 0.05). This study showed that age, presence of hypertension, probable sarcopenia and OP were related with SSP tears in postmenopausal women. To this end, although OP appeared to be related to SSP tears, SSP tear/thickness evaluation can be recommended for OP patients, especially those who have other risk factors such as older age, higher BMI, hypertension, and probable sarcopenia.


Asunto(s)
Hipertensión , Osteoporosis , Lesiones del Manguito de los Rotadores , Sarcopenia , Humanos , Femenino , Manguito de los Rotadores/patología , Sarcopenia/complicaciones , Sarcopenia/epidemiología , Sarcopenia/patología , Fuerza de la Mano , Posmenopausia , Lesiones del Manguito de los Rotadores/complicaciones , Lesiones del Manguito de los Rotadores/patología , Osteoporosis/patología , Hipertensión/patología
3.
Int J Mol Sci ; 24(5)2023 Feb 23.
Artículo en Inglés | MEDLINE | ID: mdl-36901830

RESUMEN

Photodynamic therapy (PDT) is a curative method, firstly developed for cancer therapy with fast response after treatment and minimum side effects. Two zinc(II) phthalocyanines (3ZnPc and 4ZnPc) and a hydroxycobalamin (Cbl) were investigated on two breast cancer cell lines (MDA-MB-231 and MCF-7) in comparison to normal cell lines (MCF-10 and BALB 3T3). The novelty of this study is a complex of non-peripherally methylpyridiloxy substituted Zn(II) phthalocyanine (3ZnPc) and the evaluation of the effects on different cell lines due to the addition of second porphyrinoid such as Cbl. The results showed the complete photocytotoxicity of both ZnPc-complexes at lower concentrations (<0.1 µM) for 3ZnPc. The addition of Cbl caused a higher phototoxicity of 3ZnPc at one order lower concentrations (<0.01 µM) with a diminishment of the dark toxicity. Moreover, it was determined that an increase of the selectivity index of 3ZnPc, from 0.66 (MCF-7) and 0.89 (MDA-MB-231) to 1.56 and 2.31, occurred by the addition of Cbl upon exposure with a LED 660 nm (50 J/cm2). The study suggested that the addition of Cbl can minimize the dark toxicity and improve the efficiency of the phthalocyanines for anticancer PDT applications.


Asunto(s)
Compuestos Organometálicos , Fotoquimioterapia , Humanos , Fármacos Fotosensibilizantes/farmacología , Fotoquimioterapia/métodos , Vitamina B 12 , Compuestos Organometálicos/farmacología , Isoindoles , Células MCF-7 , Zinc , Línea Celular Tumoral
4.
Molecules ; 28(10)2023 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-37241842

RESUMEN

In this work, we have described the synthesis and characterization of novel zinc (II) phthalocyanine bearing four 2-(2,4-dichloro-benzyl)-4-(1,1,3,3-tetramethyl-butyl)-phenoxy substituents on the peripheral positions. The compound was characterized by elemental analysis and different spectroscopic techniques, such as FT-IR, 1H NMR, MALDI-TOF, and UV-Vis. The Zn (II) phthalocyanine shows excellent solubility in organic solvents such as dichloromethane (DCM), n-hexane, chloroform, tetrahydrofuran (THF), and toluene. Photochemical and electrochemical characterizations of the complex were performed by UV-Vis, fluorescence spectroscopy, and cyclic voltammetry. Its good solubility allows a direct deposition of this compound as film, which has been tested as a solid-state sensing material in gravimetric chemical sensors for gas detection, and the obtained results indicate its potential for qualitative discrimination and quantitative assessment of various volatile organic compounds, among them methanol, n-hexane, triethylamine (TEA), toluene and DCM, in a wide concentration range.

5.
Curr Issues Mol Biol ; 44(5): 1950-1959, 2022 Apr 29.
Artículo en Inglés | MEDLINE | ID: mdl-35678662

RESUMEN

Antimicrobial photodynamic therapy (aPDT) has been considered as a promising methodology to fight the multidrug resistance of pathogenic bacteria. The procedure involves a photoactive compound (photosensitizer), the red or near infrared spectrum for its activation, and an oxygen environment. In general, reactive oxygen species are toxic to biomolecules which feature a mechanism of photodynamic action. The present study evaluates two clinical isolates of Gram-negative Flavobacteriumhydatis (F. hydatis): a multidrug resistant (R) and a sensitive (S) strain. Both occur in farmed fish, leading to the big production losses because of the inefficacy of antibiotics. Palladium phthalocyanines (PdPcs) with methylpyridiloxy groups linked peripherally (pPdPc) or non-peripherally (nPdPc) were studied with full photodynamic inactivation for 5.0 µM nPdPc toward both F. hydatis, R and S strains (6 log), but with a half of this value (3 log) for 5.0 µM pPdPc and only for F. hydatis, S. In addition to the newly synthesized PdPcs as a "positive control" was applied a well-known highly effective zinc phthalocyanine (ZnPcMe). ZnPcMe showed optimal photocytotoxicity for inactivation of both F. hydatis R and S. The present study is encouraging for a further development of aPDT with phthalocyanines as an alternative method to antibiotic medication to keep under control the harmful pathogens in aquacultures' farms.

6.
Anal Biochem ; 654: 114777, 2022 10 01.
Artículo en Inglés | MEDLINE | ID: mdl-35750250

RESUMEN

In the present study, the phthalocyanine (Pc) integrated mercaptopropionic acid capped quantum dot (mpa@QD) biosensor has been developed for the quantitative determination of G-quadruplex and double-stranded DNA. The working principle of the developed biosensor platform is based on the quenching of the emission signal of the mpa@QD in the presence of Pc (closed position) and the recovery of the fluorescence signal in the presence of DNA (open position). The parameters affecting biosensor performance, such as Pc type and concentration, were optimized. Since the developed biosensor aimed to determine G-quadruplex and double-stranded DNA in biological samples, the effect of common ions (such as Na+, Mg2+) and serum albumin found in many biological matrices on the biosensor performance were examined. The effect of common ions on biosensor signal was negligible, except Zn2+. The analytical properties of the biosensor, such as linear range, calibration sensitivity, relative standard deviation %, the limit of detection, and quantification, were determined. The limit of detection and quantification values were found 0.055 µM and 0.18 µM for AS1411, 0.061 µM and 0.20 µM for Tel21, 0.038 µM and 0.13 µM for Tel45 and 0.091 µM and 0.30 µM for ctDNA. Several different synthetic samples were prepared. The spiked synthetic samples such as mammalian cell medium were used to evaluate the analytical performance of Pc-mpa@QD. All synthetic samples were prepared with polyethylene glycol, which resembles biological samples' crowded environment.


Asunto(s)
Técnicas Biosensibles , Puntos Cuánticos , Animales , ADN , Iones , Isoindoles , Mamíferos
7.
J Fluoresc ; 32(5): 1801-1813, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-35704139

RESUMEN

In this current study, the novel bis[4,5-(pyrene-2-yl)-3,6-(hexyloxy)] phthalonitrile (SPN) fluorophore has been successfully synthesized. Structural characterization of this novel compound was performed by different spectroscopic methods such as FT-IR, MALDI-TOF, 1H-NMR, 13C-NMR and elemental analyses as well. In addition, the photophysical properties were determined using UV-vis absorption, steady-state fluorescence, time-resolved fluorescence spectroscopic methods and quantum chemical calculations. The metal sensing behavior of the SPN was determined in the presence of various metals (Li+, Na+, K+, Mg2+, Ca2+, Ba2+, Mn2+, Fe3+, Cr3+, Co2+, Ni2+, Ag+, Cd2+, Al3+, Hg+ and Zn2+) using fluorescence spectroscopy. The novel pyrene based phthalonitrile (SPN) showed high sensitivity and selectivity towards Fe3+ ion over other examined metal ions. In order to perform the determination of Fe3+ ion in environmental samples, experimental conditions such as selectivity, stability, precision, sensitivity, accuracy and recovery were optimized. Also, the complex stoichiometry of the novel pyrene based phthalonitrile (SPN) and Fe3+ ions was determined by a Job's plot. The compound was also studied via density functional theory calculations revealing the interaction mechanism of the molecule with Fe3+ ions.

8.
Int J Clin Pract ; 2022: 6840960, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36263238

RESUMEN

Methods: This is a prospective, observational study. Patients between the ages of 18 and 65 with BMI of 18.5-34.9, who are expected to be under general anesthesia for less than 6 hours, were divided into 3 groups according to their BMI (Group 1 BMI = 18.5-24.9, Group 2 BMI = 25-29.9, Group 3 BMI = 30-34.9). These groups were randomly divided into 2 subgroups: Groups LBW; 1 LBW, 2 LBW, and 3 LBW were given rocuronium intubation dosages based on their LBW while control groups; 1K, 2K, and 3K were given 0.6 mg/kg rocuronium according to their total body weight. The data on the duration of action of rocuronium and its effects on the endotracheal intubation conditions were evaluated. Results: In Group 1, T1 time was found to be significantly longer (p=0.001). Intubation score and the use of additional rocuronium dose were found to be significantly higher in Group 1 LBW than in Group 1K (p=0.001). In Group 1, an additional rocuronium dose was needed to achieve optimal intubation conditions for subgroup 1 LBW. Rocuronium duration of action was found to be significantly longer in control groups 2 and 3, that received TBW-based dosage. Conclusion: In adult patients with a BMI of 18.5 and 24.9 BMI, we report optimal intubation conditions with the LBW-adjusted rocuronium dosage. This trial is registered with NCT05476952.


Asunto(s)
Androstanoles , Fármacos Neuromusculares no Despolarizantes , Adulto , Humanos , Adolescente , Adulto Joven , Persona de Mediana Edad , Anciano , Rocuronio , Androstanoles/farmacología , Fármacos Neuromusculares no Despolarizantes/farmacología , Intubación Intratraqueal , Peso Corporal
9.
Aging Clin Exp Res ; 34(9): 2149-2154, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-35583720

RESUMEN

BACKGROUND: Cognitive impairment may cause significant decline in muscle function and physical performance via affecting the neuromotor control. AIM: To investigate the relationship between cognition and sarcopenia-related parameters in middle-aged and older adults. METHODS: Demographic data and comorbidities of adults ≥ 45-year-old were noted. The Mini-Mental State Examination (MMSE) was used to evaluate global cognitive function. Sonographic anterior midthigh muscle thickness, handgrip strength, chair stand test (CST) and gait speed were measured. The diagnosis of sarcopenia was established if low muscle mass was combined with low muscle function. Dynapenia was defined as low grip strength or increased CST duration. RESULTS: Among 1542 subjects (477 M, 1065 F), sarcopenia and dynapenia were detected in 22.6 and 17.2% of males, and 17.2 and 25.3% of females, respectively. Sarcopenic patients were older and had higher body mass index, higher frequencies of hypertension, diabetes mellitus and obesity. They had lower muscle thickness, grip strength in males only, CST performance in females only and gait speed than the other groups (all p < 0.05). Sarcopenic and dynapenic patients had similar MMSE scores which were lower than those of normal subjects (both p < 0.001). After adjusting for confounding factors, MMSE values were positively related with grip strength in females only, CST performance and gait speed (all p < 0.001); but not with muscle thickness in either gender. CONCLUSION: Cognitive impairment may unfavorably affect muscle function and physical performance, but not muscle mass. Accordingly, its prompt management can help to decrease patient morbidity and mortality.


Asunto(s)
Sarcopenia , Anciano , Cognición , Estudios Transversales , Femenino , Fuerza de la Mano/fisiología , Humanos , Masculino , Persona de Mediana Edad , Fuerza Muscular/fisiología , Velocidad al Caminar/fisiología
10.
J Biol Inorg Chem ; 26(4): 455-465, 2021 06.
Artículo en Inglés | MEDLINE | ID: mdl-33944997

RESUMEN

In the current research, two novel zinc(II) phthalocyanines (ZnPcs) (1 and 2) directly connecting with 4-(4-methylpiperazin-1-yl)phenyl groups have been synthesized through the Suzuki-Miyaura coupling reaction. These ZnPcs 1 and 2 were converted to their water-soluble derivatives (1Q and 2Q) by quaternization. The photochemical and photophysical properties were determined in DMSO for the non-ionic zinc(II) phthalocyanines (1 and 2) and in both DMSO and aqueous solutions for the quaternized cationic derivatives (1Q and 2Q) to establish their photosensitizer capabilities in photodynamic therapy (PDT). The spectrofluorometric and spectrophotometric techniques were employed for the determination of interaction between water-soluble ZnPcs (1Q and 2Q) and BSA or ct-DNA. The binding constants of these compounds to BSA were found in the order of 108 M-1. The binding constant of the ct-DNA interaction with 2Q (1.09 × 105 M-1) was found higher than 1Q (6.87 × 104 M-1). The thermodynamic constants were determined for both 1Q and 2Q. The endothermic and spontaneous nature of interaction was observed with ct-DNA. Besides, the thermal denaturation and viscosity studies proved the non-intercalative mode of binding for both compounds to ct-DNA.


Asunto(s)
ADN/química , Isoindoles/química , Isoindoles/síntesis química , Piperazina/química , Albúmina Sérica Bovina/química , Compuestos de Zinc/química , Estructura Molecular , Procesos Fotoquímicos , Unión Proteica , Termodinámica
11.
J Biol Inorg Chem ; 26(2-3): 235-247, 2021 05.
Artículo en Inglés | MEDLINE | ID: mdl-33558997

RESUMEN

Photodynamic therapy (PDT) has drawn a great scientific attention to cancer treatment over the last decades. However, the bottleneck for the PDT is to find good photosensitizers (PSs) with greater water solubility, no aggregation, and fast discharge from the body. Therefore, there are still a big scientific desire for the synthesizing new rational PSs for treatment of cancer by PDT technique. In favor of improving the competence of PDT, an axially bis[4-(diphenylamino-1,1'-biphenyl-4-ol)] substituted silicon(IV) phthalocyanine (3) was converted to its water-soluble quaternized derivative (3Q). Their structures were fully characterized by single-crystal X-ray diffraction, elemental analysis, and different spectroscopic methods such as FT-IR, UV-Vis, MALDI-TOF, and 1H-NMR. The photophysical properties such as fluorescence quantum yields and lifetimes, and the photochemical properties such as singlet oxygen generation of both phthalocyanines were investigated. Ground and excited-state calculations were performed to explain the observed electronic absorption spectra. The addition of the 4-diphenylamino-1,1'-biphenyl-4-ol groups on the axially positions of the silicon(IV) phthalocyanine increased the singlet oxygen quantum yield from 0.15 to around 0.20. Especially quaternized compound 3Q showed high singlet oxygen quantum yield of 0.26 in water solution. In addition, a spectroscopic investigation of the binding behavior of the quaternized silicon (IV) phthalocyanine complex to bovine serum albumin (BSA) is also studied in this work, confirming the possible interaction. Further theoretical calculations were carried out to find out the plausible-binding regions of the BSA protein. Axially bis[4-(diphenylamino-1,1'-biphenyl-4-ol)] substituted silicon(IV) phthalocyanine (3) was converted to its quaternized water soluble derivative (3Q). The photophysical properties such as fluorescence quantum yields and lifetimes, and the photochemical properties such as singlet oxygen generation of both phthalocyanines were investigated. In addition, a spectroscopic investigation of the binding behavior of the quaternized silicon (IV) phthalocyanine complex to bovine serum albumin (BSA) is also studied in this work, confirming the possible interaction. Further theoretical calculations were carried out to find out the plausible binding regions of the BSA protein.


Asunto(s)
Indoles/química , Indoles/metabolismo , Fármacos Fotosensibilizantes/química , Fármacos Fotosensibilizantes/metabolismo , Albúmina Sérica Bovina/metabolismo , Silicio/química , Agua/química , Indoles/farmacología , Isoindoles , Modelos Moleculares , Conformación Molecular , Fármacos Fotosensibilizantes/farmacología , Unión Proteica , Teoría Cuántica , Solubilidad
12.
Molecules ; 25(9)2020 Apr 29.
Artículo en Inglés | MEDLINE | ID: mdl-32365538

RESUMEN

In this work, the novel hybrid nanomaterial SWCNT/SiPc made of single walled carbon nanotubes (SWCNT) cross-linked via axially substituted silicon (IV) phthalocyanine (SiPc) was studied as the active layer of chemiresistive layers for the detection of ammonia and hydrogen. SWCNT/SiPc is the first example of a carbon-based nanomaterial in which an axially substituted phthalocyanine derivative is used as a linker. The prepared hybrid material was characterized by spectroscopic methods, thermogravimetry, scanning and transmission electron microscopies. The layers of the prepared hybrid were tested as sensors toward ammonia and hydrogen by a chemiresistive method at different temperatures and relative humidity as well as in the presence of interfering gases like carbon dioxide, hydrogen sulfide and volatile organic vapors. The hybrid layers exhibited the completely reversible sensor response to both gases at room temperature; the recovery time was 100-200 s for NH3 and 50-120 s in the case of H2 depending on the gas concentrations. At the relative humidity (RH) of 20%, the sensor response was almost the same as that measured at RH 5%, whereas the further increase of RH led to its 2-3 fold decrease. It was demonstrated that the SWCNT/SiPc layers can be successfully used for the detection of both NH3 and H2 in the presence of CO2. On the contrary, H2S was found to be an interfering gas for the NH3 detection.


Asunto(s)
Técnicas Biosensibles , Técnicas Electroquímicas , Indoles/química , Nanoestructuras/química , Nanotubos de Carbono/química , Silicio/química , Gases/análisis , Gases/química , Isoindoles , Espectroscopía Infrarroja por Transformada de Fourier , Termogravimetría
13.
Turk J Med Sci ; 50(8): 1955-1962, 2020 12 17.
Artículo en Inglés | MEDLINE | ID: mdl-32682357

RESUMEN

Background/aim: The aim of this study was to compare the effects of different epidural initiation volumes on postoperative pain scores, analgesic requirements, and side effects in pregnant women administered patient-controlled epidural analgesia (PCEA) for postoperative pain after cesarean sections. Materials and methods: Eighty-one pregnant women, aged 18­45 years, were included in this randomized, double-blind study. Combined spinal epidural anesthesia was administered for each cesarean section. The patients were divided into 3 groups and different volumes (20 mL, 10 mL, and 5 mL) of the study drug (0.0625% bupivacaine plus 2 µg/mL of fentanyl) were administered 90 min after the spinal block via epidural catheter. The visual analogue scale (VAS) scores at rest and during movement, first PCEA dose time, number of PCEA doses required per hour, total analgesic consumed, and side effects were recorded postoperatively. Results: There were no statistically significant differences among the groups in terms of the VAS rest and VAS movement scores. The times to the first analgesic dose requirement were longer in Group 10 and Group 20 than in Group 5. The analgesic requirement during the first 2 h was lower in Group 20 than in the other groups. Conclusions: The PCEA initiations with different volumes provided similar pain scores. However, the 20 mL volume resulted in a lower analgesic dose requirement during the early postoperative period, and it also delayed the requirement for analgesia.


Asunto(s)
Analgesia Epidural/métodos , Analgesia Controlada por el Paciente/métodos , Analgésicos Opioides/uso terapéutico , Anestésicos Locales/uso terapéutico , Cesárea , Dolor Postoperatorio/tratamiento farmacológico , Adolescente , Adulto , Analgésicos Opioides/administración & dosificación , Anestésicos Locales/administración & dosificación , Bupivacaína/administración & dosificación , Bupivacaína/uso terapéutico , Relación Dosis-Respuesta a Droga , Método Doble Ciego , Femenino , Fentanilo/administración & dosificación , Fentanilo/uso terapéutico , Humanos , Persona de Mediana Edad , Embarazo , Resultado del Tratamiento , Adulto Joven
14.
J Biol Inorg Chem ; 24(2): 191-210, 2019 03.
Artículo en Inglés | MEDLINE | ID: mdl-30673878

RESUMEN

Zinc(II) (5), indium(III) (6), and lutetium(III) (7) phthalocyanines (Pcs) peripherally substituted with poly (ethylene glycol) (PEG) monomethyl ether 2000 (PEGME-2000) blocks were synthesized via Sonogashira coupling reaction with high yields and their photophysical, photochemical and photobiological properties were investigated. We elucidated the interactions of these compounds with calf thymus DNA and bovine serum albumin (BSA), and determined K(DNA) and K(BSA) binding constants at degrees of 105 and 106, respectively. Singlet oxygen quantum yields were found (Ф∆ = 0.44, 0.54, and 0.68 for 5, 6, and 7, respectively). Thermodynamic parameters, as well as thermal denaturation profile of double-stranded CT-DNA were examined to determine the type of binding mode. According to our experimental data, we report that PEGME-2000 favors the formation of binary complex between DNA, and phthalocyanine complexes. Therein, thermodynamic data suggest that this binding mode is indeed spontaneous under reported conditions, and rather non-specific. Additionally, Pcs 5, 6, and 7 substituted with PEGME-2000 blocks showed antimicrobial activity against Gram-positive and Gram-negative bacteria, as well as fungi (yeast), and Pc 5 had the highest antimicrobial activity among them, as revealed by disc diffusion assay results. In short, our results suggest that these compounds could be used for photodynamic therapy, they have both antibacterial and antifungal activity, and the binding ability of new phthalocyanines 5, 6, and 7 with BSA paves the way for their utilization as drug vehicle in blood plasma.


Asunto(s)
Antibacterianos/farmacología , Antifúngicos/farmacología , Fármacos Fotosensibilizantes/farmacología , Animales , Antibacterianos/síntesis química , Antibacterianos/química , Antifúngicos/síntesis química , Antifúngicos/química , Bovinos , ADN/química , Éteres/química , Éteres/farmacología , Hongos/efectos de los fármacos , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Indio/química , Indio/farmacología , Indoles/química , Indoles/farmacología , Isoindoles , Lutecio/química , Lutecio/farmacología , Pruebas de Sensibilidad Microbiana , Compuestos Organometálicos/química , Compuestos Organometálicos/farmacología , Procesos Fotoquímicos , Fármacos Fotosensibilizantes/síntesis química , Fármacos Fotosensibilizantes/química , Polietilenglicoles/química , Polietilenglicoles/farmacología , Albúmina Sérica Bovina/química , Compuestos de Zinc
15.
BMC Anesthesiol ; 19(1): 244, 2019 12 30.
Artículo en Inglés | MEDLINE | ID: mdl-31888511

RESUMEN

BACKGROUND: This study were designed to investigate the usefulness of the videolaryngoscope-guided insertion technique compared with the standard digital technique for the insertion success rate and insertion conditions of the Proseal™ laryngeal mask airway (PLMA). METHODS: Prospective, one hundred and nineteen patients (ASA I-II, aged 18-65 yr) were randomly divided for PLMA insertion using the videolaryngoscope-guided technique or the standard digital technique. The PLMA was inserted according to the manufacturer's instructions in the standard digital technique group. The videolaryngoscope-guided technique was performed a C-MAC® videolaryngoscope with D-Blade, under gentle videolaryngoscope guidance, the epiglottis was lifted, and the PLMA was advanced until the tip of the distal cuff reached the oesophagus inlet. The number of insertion attempts, insertion time, oropharyngeal leak pressure, leak volume, fiberoptic bronchoscopic view, peak inspiratory pressure, ease of gastric tube placement, hemodynamic changes, visible blood on PLMA and postoperative airway morbidity were recorded. RESULTS: The first-attempt success rate (the primary outcome) was higher in the videolaryngoscope-guided technique than in the standard digital technique (p = 0.029). The effect size values with 95% confidence interval were 0.19 (0.01-0.36) for the first and second attempts, 0.09 (- 0.08-0.27) for the first and third attempts, and not computed for the second and third attempts by the groups, respectively. CONCLUSION: Videolaryngoscope-guided insertion technique can be a help in case of difficult positioning of a PLMA and can improve the PLMA performance in some conditions. We suggest that the videolaryngoscope-guided technique may be a useful technique if the digital technique fails. TRIAL REGISTRATION: ClinicalTrials.gov NCT03852589 date of registration: February 22th 2019.


Asunto(s)
Máscaras Laríngeas , Laringoscopios , Laringoscopía/métodos , Grabación en Video , Adolescente , Adulto , Anciano , Broncoscopía , Diseño de Equipo , Femenino , Humanos , Masculino , Persona de Mediana Edad , Estudios Prospectivos , Adulto Joven
16.
Curr Ther Res Clin Exp ; 90: 21-26, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-30787962

RESUMEN

OBJECTIVE: In this study, a north polar tube (Portex® North Polar tube [Ivory PVC Portex tube; Smiths Medical International, Hythe, United Kingdom]) (NPT) and spiral tube (ST) were compared for their ability to provide a nasal airway in patients during maxillofacial surgery. METHODS: Patients who were aged 18 to 65 years with American Society of Anaesthesiologists score 1 to 2 and Mallampati score 1 to 2 were included in the study. The anesthesia technique was standardized in all patients. Patients were divided into 2 groups randomly: the NPT (n = 35) and ST groups (n = 35). Anesthesia was administered with 1% to 2% sevoflurane and a mixture of 50% oxygen + 50% air in both groups. The mean arterial pressure and heart rate values of preinduction; preintubation; and the first, second, third, and fifth minutes of intubation were recorded. Epistaxis, intraoral bleeding, cuff burst, use of Magill pens, duration of intubation, intubation difficulty, laryngeal compression, head position change, and glottic grade were evaluated. RESULTS: There were no significant differences between groups in terms of demographic data (gender, age, height, weight, body mass index, American Society of Anaesthesiologists score, and Mallampati score). Macintosh laryngoscopes were used during intubation in all patients. There was no significant difference between groups in terms of intubation difficulty, duration of intubation, use of Magill pens, and determination of the glottic grade (P > 0.05). Epistaxis was significantly lower in the NPT group than in the ST group (P = 0.012). Intraoral bleeding was significantly higher in the ST group than in the NPT group (P = 0.001). During intubation, laryngeal compression (Sellick maneuver) and head position changes were significantly lower in the NPT group than in the ST group (P = 0.003 and P < 0.001, respectively). There were no significant differences in mean arterial pressure and heart rate between the 2 groups. CONCLUSIONS: We conclude that the NPT was associated with less epistaxis and manipulations such as laryngeal compression and head position changes when compared with the ST during nasotracheal intubation. The velvet-soft polyvinyl chloride material of the NPT appears to be responsible for this advantage.

17.
Z Naturforsch C J Biosci ; 73(5-6): 221-228, 2018 Apr 25.
Artículo en Inglés | MEDLINE | ID: mdl-29306935

RESUMEN

Photodynamic inactivation (PDI) has been featured as an effective strategy in the treatment of acute drug-resistant infections. The efficiency of PDI was evaluated against three periodontal pathogenic bacteria that were tested as drug-resistant strains. In vitro studies were performed with four water-soluble cationic Zn(II) phthalocyanines (ZnPc1-4) and irradiation of a specific light source (light-emitting diode, 665 nm) with three doses (15, 36 and 60 J/cm2). The well detectable fluorescence of ZnPcs allowed the cellular imaging, which suggested relatively high uptakes of ZnPcs into bacterial species. Complete photoinactivation was achieved with all studied ZnPc1-4 for Enterococcus faecalis (E. faecalis) at a light dose of 15 J/cm2. The photodynamic response was high for Prevotella intermedia (P. intermedia) after the application of 6 µM of ZnPc1 and a light dose of 36 J/cm2 and for 6 µM of ZnPc2 at 60 J/cm2. P. intermedia was inactivated with ZnPc3 (4 log) and ZnPc4 (2 log) with irradiation at an optimal dose of 60 J/cm2. Similar photoinactivation results (2 log) were achieved for Aggregatibacter actinomycetemcomitans (A. actinomycetemcomitans) treated with 6 µM ZnPc1 and ZnPc2 at a light dose of 60 J/cm2. The study suggested that PDI with quaternized Zn(II) phthalocyanines and specific light irradiation appears to be a very useful antimicrobial strategy for effective inactivation of drug-resistant periodontal pathogens.


Asunto(s)
Antibacterianos/farmacología , Indoles/farmacología , Compuestos Organometálicos/farmacología , Enfermedades Periodontales/microbiología , Fármacos Fotosensibilizantes/farmacología , Aggregatibacter actinomycetemcomitans/efectos de los fármacos , Biopelículas/efectos de los fármacos , Farmacorresistencia Bacteriana/efectos de los fármacos , Enterococcus faecalis/efectos de los fármacos , Humanos , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Enfermedades Periodontales/tratamiento farmacológico , Prevotella intermedia/efectos de los fármacos
18.
Molecules ; 24(1)2018 Dec 26.
Artículo en Inglés | MEDLINE | ID: mdl-30587817

RESUMEN

The syntheses of a novel 1,4,8,11,15,18,22,25-octahexyloxy-2,3,9,10,16,17,23,24-octa-(4-trifluoromethoxyphenyl) phthalocyanine (3a) and its zinc(II) phthalocyanine derivative (3b) have been described and characterized by elemental analysis,¹H NMR, 13C NMR, 19F NMR, mass, UV-Vis and FT-IR. The newly prepared metal-free phthalocyanine and its zinc(II) counterpart are soluble in most organic solvents. The photophysical and photochemical properties such as aggregation, fluorescence, singlet oxygen generation and photodegradation under light irradiation of these phthalocyanines have been investigated in DMF. The hexadeca-substituted phthalocyanines (3a and 3b) showed longer absorption and emission wavelength values when compared to that of reported phthalocyanine derivatives due to substitution of the all possible positions in the phthalocyanine framework. The zinc(II) phthalocyanine derivative does not only have a good singlet oxygen generation but also has other photophysicochemical properties that enables this phthalocyanine to be useful as a photosensitizer for cancer treatment using photodynamic therapy.


Asunto(s)
Diseño de Fármacos , Indoles/química , Compuestos Organometálicos/química , Procesos Fotoquímicos , Técnicas de Química Sintética , Indoles/síntesis química , Isoindoles , Metales/química , Compuestos Organometálicos/síntesis química , Fotoquimioterapia , Fotólisis , Oxígeno Singlete/química , Espectrometría de Fluorescencia , Espectroscopía Infrarroja por Transformada de Fourier , Compuestos de Zinc
19.
J Biol Inorg Chem ; 22(6): 953-967, 2017 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-28616663

RESUMEN

Two novel silicon(IV) phthalocyanines bearing 1,3-bis[3(dimethylamino)phenoxy]propan-2-ol or 1,3-bis[3(diethylamino)phenoxy]propan-2-ol groups at their axial positions were synthesized. These phthalocyanines were converted into their water soluble derivatives by the quaternization reaction with methyl iodide. The quaternized phthalocyanines show excellent solubility aqueous solutions without any aggregation which makes them potential photosensitizers for use in photodynamic therapy (PDT). For this reason, the photophysical and photochemical properties such as fluorescence quantum yields, lifetimes, singlet oxygen generation and photodegradation of both non-ionic (3 and 5) and quaternized cationic silicon(IV) phthalocyanines were investigated. Furthermore, the cytotoxicity of PDT was determined by colorimetric proliferation assay against to hepatocellular carcinoma (HuH-7) cancer cells. In this study, the cells were incubated with a novel water soluble silicon(IV) phthalocyanine derivatives and thereafter the cells were illuminated using broad-band incoherent light source.


Asunto(s)
Indoles/química , Compuestos de Organosilicio/química , Fármacos Fotosensibilizantes/química , Agua/química , Animales , Bovinos , Línea Celular Tumoral , Humanos , Indoles/metabolismo , Indoles/farmacología , Modelos Moleculares , Conformación Molecular , Compuestos de Organosilicio/metabolismo , Compuestos de Organosilicio/farmacología , Fotólisis , Fármacos Fotosensibilizantes/metabolismo , Fármacos Fotosensibilizantes/farmacología , Albúmina Sérica Bovina/metabolismo , Oxígeno Singlete/química , Solubilidad
20.
J Biol Inorg Chem ; 22(8): 1251-1266, 2017 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-29052049

RESUMEN

In this study, morpholinoethoxy-substituted metal-free (3), zinc(II) (4) and indium(III) (5) phthalocyanines were synthesized. These phthalocyanines were converted to their water-soluble quaternized derivatives (3Q-5Q) using excess methyl iodide as a quaternization agent. All these phthalocyanines (Pcs) were characterized by elemental analysis and different spectroscopic methods such as FT-IR, 1H NMR, UV-Vis and mass spectrometry. The photophysical and photochemical properties such as fluorescence and generation of singlet oxygen were investigated for determination of these phthalocyanines as photosensitizers in photodynamic therapy (PDT) applications. The binding properties of quaternized phthalocyanines (3Q-5Q) to calf thymus DNA (CT-DNA) were investigated by UV-Vis and fluorescence spectrophotometric methods. The quenching effect of all quaternized phthalocyanines on the fluorescence intensity of SYBR Green-DNA complex was determined. The mixtures of 3Q, 4Q or 5Q and DNA solutions were used to determine the change in T m of double helix DNA with thermal denaturation profile. In addition, thermodynamic parameters considering their aggregation in buffer solution, which shows the spontaneity of the reactions between DNA and quaternized Pcs were investigated. On the other hand, in vitro phototoxicity and cytotoxicity behavior of the quaternized water-soluble phthalocyanine photosensitizers (3Q-5Q) were tested against the cervical cancer cell line named HeLa for evaluation of their suitability for treatment of cancer by PDT method. Peripherally tetra-substituted neutral and quaternized metal-free and metallophthalocyanines (MPcs) (Zn, In) bearing morpholinoethoxy groups were prepared. The binding of quaternized compounds (3Q-5Q) to CT-DNA were examined using UV-Vis, fluorescence spectra, thermal denaturation profiles and K SV values. Besides, thermodynamic studies indicated that binding of 3Q-5Q to DNA was spontaneous. On the other hand, in vitro phototoxicity and cytotoxicity behavior of the quaternized water-soluble phthalocyanine photosensitizers (3Q-5Q) were tested against the cervical cancer cell line named HeLa for evaluation of their suitability for treatment of cancer by PDT method.


Asunto(s)
Fenómenos Químicos , ADN/química , Indoles/química , Indoles/farmacología , Morfolinas/química , Agua/química , Animales , Bovinos , Células HeLa , Humanos , Isoindoles , Modelos Moleculares , Conformación de Ácido Nucleico , Desnaturalización de Ácido Nucleico , Fármacos Fotosensibilizantes/química , Fármacos Fotosensibilizantes/farmacología , Oxígeno Singlete/química , Solubilidad , Temperatura
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