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1.
J Fluoresc ; 2024 Apr 16.
Artículo en Inglés | MEDLINE | ID: mdl-38625572

RESUMEN

This study was based on the development of surface-based photoluminescence sensor for metal detection, quantification, and sample purification employing the solid sensory chip having the capability of metal entrapment. The Co(II), Cu(II) and Hg(II) sensitive fluorescence sensor (TP) was first synthesized and characterized its sensing abilities towards tested metal ions by using fluorescence spectral investigation while the synthesis and complexation of the receptor was confirmed by the chromogenic, optical, spectroscopic and spectrometric analysis. Under optical investigation, the ligand solution exhibited substantial chromogenic changes as well as spectral variations upon reacting with copper, cobalt, and mercuric ions, while these behaviors were not seen for the rest of tested metallic ions i.e., Na+, Ag+, Ni2+, Mn2+, Pd2+, Pb2+, Cd2+, Zn2+, Sn2+, Fe2+, Fe3+, Cr3+, and Al3+. These colorimetric alterations and spectral shifting could potentially be employed to detect and quantify these specific metal ions. After the establishment of the ligand's selective complexation ability towards selected metals, it was fabricated over the substituted porous silicon surface (FPS) keeping in view of the development of surface-based photoluminescence sensor (TP-FPS) for the selected metal sensation and entrapment to purify the sample just be putting off the metal entrapped sensory solid chip. Surface characterization and ligand fabrication was inspected by plan and cross sectional electron microscopic investigations, vibrational and electronic spectral analysis. The sensitivity of the ligand (TP) in the solution phase metal discrimination was determined by employing the fluorescence titration analysis of the ligand solution after progressive induction of Co2+, Cu2+, and Hg2+, which afford the detection limit values of 2.14 × 10- 8, 3.47 × 10- 8 and 3.13 × 10- 3, respectively. Concurrently, photoluminescence titration of the surface fabricated sensor (TP-FPS) revealed detection limit values of 3.14 × 10- 9, 7.43 × 10- 9, and 8.21 × 10- 4, respectively, for the selected metal ions.

2.
Biomedicines ; 11(10)2023 Oct 23.
Artículo en Inglés | MEDLINE | ID: mdl-37893241

RESUMEN

Endometriosis, which is the presence of endometrial stroma and glands outside the uterus, is one of the most frequently diagnosed gynecologic diseases in reproductive women. Patients with endometriosis suffer from various pain symptoms such as dysmenorrhea, dyspareunia, and chronic pelvic pain. The pathophysiology for chronic pain in patients with endometriosis has not been fully understood. Altered inflammatory responses have been shown to contribute to pain symptoms. Increased secretion of cytokines, angiogenic factors, and nerve growth factors has been suggested to increase pain. Also, altered distribution of nerve fibers may also contribute to chronic pain. Aside from local contributing factors, sensitization of the nervous system is also important in understanding persistent pain in endometriosis. Peripheral sensitization as well as central sensitization have been identified in patients with endometriosis. These sensitizations of the nervous system can also explain increased incidence of comorbidities related to pain such as irritable bowel disease, bladder pain syndrome, and vulvodynia in patients with endometriosis. In conclusion, there are various possible mechanisms behind pain in patients with endometriosis, and understanding these mechanisms can help clinicians understand the nature of the pain symptoms and decide on treatments for endometriosis-related pain symptoms.

3.
J Clin Med ; 12(11)2023 May 30.
Artículo en Inglés | MEDLINE | ID: mdl-37297959

RESUMEN

We evaluated the clinical outcomes of using type 1 collagen gel after therapeutic resectoscopy; overall, 150 women aged > 20 who planned to undergo therapeutic resectoscopy were enrolled. The patients were randomly assigned to either of the anti-adhesive treatment groups: the type 1 collagen gel (Collabarrier®) (study group; N = 75) or the sodium hyaluronate and sodium carboxymethylcellulose gel group (control group; N = 75) after resectoscopy. One month after applying anti-adhesive materials, postoperative intrauterine adhesions were evaluated using second-look hysteroscopy; the incidence rate of postoperative intrauterine adhesions examined through second-look hysteroscopy showed no significant differences between the groups. There were no statistical differences between the frequency and mean scores of the type and intensity of adhesions in both groups. Finally, no significant differences in adverse events, serious adverse events, adverse device effects, and serious adverse device effects were noted between the two groups; type 1 collagen gel can be effectively and safely used in intrauterine surgery to minimize postoperative adhesions, thereby eventually decreasing the prevalence of infertility, secondary amenorrhea, and recurrent pregnancy loss in reproductive women.

4.
Mol Divers ; 27(1): 193-208, 2023 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-35344136

RESUMEN

In this work, we have synthesized various organic compounds possessing 1,3,4-oxadiazole as a core structure and the structure of the newly synthesized target compounds has been revealed using different analytical approaches such as FT-IR, LCMS, and NMR (proton and carbon), respectively. The in vitro carbonic anhydrase potentials of these synthesized 17 different analogues were investigated. The result suggests that compound 7g, a 3-pyridine substituted analogue with an IC50 of 0.1 µM, was found to have the most potent carbonic inhibitory activity (11-fold more active) than the positive control (acetazolamide) with an IC50 of 1.1 ± 0.1 µM. Besides, among the series 7(a-q) approved in the identification of four potent carbonic anhydrase inhibitors with the IC50 standards varies from 0.1 to 1.0 ± 0.1 µM. Additionally, the non-competitive behaviour for potent compound 7g was analysed using the Lineweaver-Burk plot from the kinetic study. Furthermore, the anticancer activity of all the synthesized compounds screened against B16F10 melanoma cells using the MTT assay method. Additionally, the molecular docking studies revealed that 7g inhibitor shows good binding energy as well as good binding interaction pattern along with enzyme.


Asunto(s)
Anhidrasas Carbónicas , Anhidrasas Carbónicas/metabolismo , Simulación del Acoplamiento Molecular , Relación Estructura-Actividad , Espectroscopía Infrarroja por Transformada de Fourier , Inhibidores de Anhidrasa Carbónica/farmacología , Inhibidores de Anhidrasa Carbónica/química , Estructura Molecular
5.
Medicine (Baltimore) ; 101(31): e29726, 2022 Aug 05.
Artículo en Inglés | MEDLINE | ID: mdl-35945797

RESUMEN

To evaluate the efficacy and safety of a gonadotropin-releasing hormone (GnRH) agonist for treating large-sized submucosal leiomyoma before hysteroscopic myomectomy. The data were retrospectively collected from patients who underwent a hysteroscopic myomectomy for a submucosal leiomyoma >3.5 cm in size from January 2009 to December 2018. The patients were divided into the GnRH group and the control group according to whether they were pretreated before surgery. A total of 61 patients were included in the study, 31 in the GnRH agonist group and 30 in the control group. At diagnosis, the maximum leiomyoma diameter was similar between the 2 groups (4.67 ± 0.6 cm in the GnRH agonist group vs 3.82 ± 0.6 cm in the control group, P = .061). After pretreatment with the GnRH agonist, the maximum diameter was significantly smaller in the GnRH agonist group compared to the control group (3.82 ± 0.6 vs 4.33 ± 0.8 cm, respectively, P = .004). The leiomyoma volume in the GnRH agonist group decreased by 55.6%, from 41.68 ± 15.7 to 23.19 ± 10.4 cm3, which led to significant differences in leiomyoma volume between the 2 groups (23.19 ± 10.4 cm3 in the GnRH agonist group vs 33.22 ± 24.7 cm3 in the control group, P = .042). The GnRH agonist group showed a shorter operation time (37.7 vs 43.9 minutes, P = .040) and less uterine distention media was used (6800 vs 9373.3 mL, P = .037) compared to the control group. Postoperative complications such as estimated blood loss, remnant leiomyoma, and recurrence were similar between the 2 groups. Treatment with a GnRH agonist before hysteroscopic myomectomy for large submucosal leiomyoma might decrease the volume of the leiomyoma, reduce operation time, and the amount of uterine-distension media used without surgical complications.


Asunto(s)
Leiomioma , Miomectomía Uterina , Neoplasias Uterinas , Femenino , Hormona Liberadora de Gonadotropina , Humanos , Leiomioma/tratamiento farmacológico , Leiomioma/cirugía , Estudios Retrospectivos , Neoplasias Uterinas/tratamiento farmacológico , Neoplasias Uterinas/cirugía
6.
Gynecol Obstet Invest ; 87(1): 79-88, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35500567

RESUMEN

OBJECTIVE: In the present study, we attempted to identify the effects of fenofibrate on human cervical cancer cells. METHODS: The cytotoxicity of fenofibrate in cervical cancer cells was determined by Cell Counting Kit-8. Immunoblotting assay was used to determine the protein expression of caspase-3, poly ADP-ribose polymerase cleavage, B-cell lymphoma 2 family protein expression, microtubule-associated protein 1A/1B-light chain 3 (LC3), as well as cyclins and cyclin-dependent kinases. Immunofluorescence imaging was used to determine the expression of cleaved caspase-3 and LC3. Flow cytometry was used to determine cell cycle and apoptosis. RESULTS: We first showed that fenofibrate treatment reduced cell viability in HeLa cervical cancer cells in a dose-dependent manner at 24 h and 48 h. Importantly, fenofibrate-induced cell death was mediated through cell cycle arrest in the G0-G1 phase and caspase-dependent apoptosis. Moreover, fenofibrate also induced autophagy activation in a dose-dependent manner and pharmacological inhibition of autophagy led to increase of sub-G1 phase and caspase-dependent cell death in HeLa cells. CONCLUSION: In conclusion, these data demonstrated that fenofibrate initially induced cell cycle arrest, followed by caspase-3-dependent cell death in cervical cancer HeLa cells. However, fenofibrate also induced autophagy activation, which is closely related to the survival of diverse cancer cells, thus reducing the anticancer effects of fenofibrate. Therefore, the combination of an autophagy inhibitor and fenofibrate might have the potential to become a new therapeutic strategy for cervical cancer.


Asunto(s)
Apoptosis , Puntos de Control del Ciclo Celular , Fenofibrato , Neoplasias del Cuello Uterino , Caspasa 3/metabolismo , Femenino , Fenofibrato/farmacología , Células HeLa , Humanos , Neoplasias del Cuello Uterino/patología
7.
Medicine (Baltimore) ; 101(10): e29023, 2022 Mar 11.
Artículo en Inglés | MEDLINE | ID: mdl-35451403

RESUMEN

ABSTRACT: This study evaluated the efficacy and feasibility of long-term use of levonorgestrel releasing intrauterine system (LNG-IUS) in endometriosis patients after using LNG-IUS for >5 years as their postoperative maintenance therapy.Data were obtained retrospectively from patients who maintained medical therapy for >5 years after surgical treatment of endometriosis from January 2008 to April 2015. Patients were divided into study group and control group according to the type of medication; the study group consisted of patients who received LNG-IUS as maintenance therapy, and patients in the control group received combined oral contraceptives (ethinyl estradiol 20 µg and drospirenone 3 mg) or dienogest 2 mg.A total of 263 patients (94 patients in the study group, 169 in the control group) were included in the study. 91.5% (86/94) of the patients in the study group maintained the treatment for >5 years, whereas only 21.9% (37/169) of patients in the control group maintained the treatment for >5 years.LNG-IUS significantly decreased the pain score for non-cyclic pelvic/back pain (from 4.0 ±â€Š1.6 to 0.6 ±â€Š1.3, P < .001), dysmenorrhea (from 6.5 ±â€Š1.7 to 6.5 ±â€Š1.7, P < .001), and dyspareunia/dyschezia (from 6.5 ±â€Š1.7 to 1.3 ±â€Š1.4, P = .006) after 1 year, and the effect was persistent for 10 years (P < .01). When compared with control group, the effect on pain reduction was comparable to the oral contraceptives or dienogest, with less systemic side effects such as mood change or nausea.LNG-IUS for >5 years as a postoperative maintenance therapy for endometriosis patients is an effective and feasible treatment that shows significant effect on pain reduction with less systemic side effect compared with other types of treatment. Therefore, LNG-IUS can be recommended as a long-term postoperative therapy for endometriosis patients who do not plan to become pregnant for several years.


Asunto(s)
Endometriosis , Dispositivos Intrauterinos Medicados , Anticonceptivos Orales Combinados , Dismenorrea/tratamiento farmacológico , Endometriosis/cirugía , Femenino , Humanos , Dispositivos Intrauterinos Medicados/efectos adversos , Levonorgestrel , Dolor Pélvico/tratamiento farmacológico , Dolor Pélvico/etiología , Estudios Retrospectivos
8.
Molecules ; 27(5)2022 Mar 07.
Artículo en Inglés | MEDLINE | ID: mdl-35268831

RESUMEN

A series of nine novel 1,2,4-triazole based compounds were synthesized through a multistep reaction pathway and their structures were scrutinized by using spectral methods such as FTIR, LC-MS, 1H NMR, and 13C NMR. The synthesized derivatives were screened for inhibitory activity against the mushroom tyrosinase and we found that all the synthesized compounds demonstrated decent inhibitory activity against tyrosinase. However, among the series of compounds, N-(4-fluorophenyl)-2-(5-(2-fluorophenyl)-4-(4-fluorophenyl)-4H-1,2,4-triazol-3-ylthio) acetamide exhibited more prominent activity when accompanied with the standard drug kojic acid. Furthermore, the molecular docking studies identified the interaction profile of all synthesized derivatives at the active site of tyrosinase. Based on these results, N-(4-fluorophenyl)-2-(5-(2-fluorophenyl)-4-(4-fluorophenyl)-4H-1,2,4-triazol-3-ylthio) acetamide could be used as a novel scaffold to design some new drugs against melanogenesis.


Asunto(s)
Monofenol Monooxigenasa
9.
Sci Rep ; 11(1): 17996, 2021 09 09.
Artículo en Inglés | MEDLINE | ID: mdl-34504276

RESUMEN

Herein, for the first time the carbon dots (CDs) were synthesized by reflux method from sawmill waste material. We also represent a novel strategy based on fluorescent CDs for determination of ponceau 4R and allura red dyes in soft drinks. Interestingly, both the dyes were sensitive and showed effective fluorescence quenching of the CDs owing to the interaction between them. The analytical applicability of CDs were evaluated for detection of both the dyes with a good linear relationship between the concentration range of 0.0 to 3.0 µg mL-1 and having detection limit 0.45 and 0.47 µg mL-1 for allura red and ponceau 4R dyes respectively. Meanwhile, the potential application of this novel fluorescent probe for dyes determination in real samples was validated in different soft drink samples with good accuracy and precision. Thus, these findings provides new insights for the potential risk assessment of both the dyes. Moreover, CDs acted as an excellent fluorescent material in cellular imaging owing to their cellular uptake and localization.

10.
J Fluoresc ; 31(6): 1739-1749, 2021 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-34468922

RESUMEN

We have prepared Schiff base functionalized 1,2,4-triazole and pyrene derivative for selective, sensitive, and naked eye colorimetric detection of Cu2+ in the mixed organic- aqueous media. Amongst the 18 different metal ions studied for absorption and fluorescence titration, only Cu2+ ion encourages the modification in spectral properties of Schiff base functionalized 1,2,4-Triazole and Pyrene Probe. The stoichiometric ratio of the TP-Cu2+ complex was determined to be 2:1 according to Job's plot. The lower detection limit estimated for Cu2+ is 0.234 nM which shows excellent sensitivity and selectivity of the present analytical method towards detection of Cu2+ ion in the mixed organic-aqueous media. The present approach has been successfully utilized for the quantitative determination of Cu2+ ion from environmental aqueous solution.


Asunto(s)
Cobre/análisis , Colorantes Fluorescentes/química , Pirenos/química , Triazoles/química , Colorimetría , Iones/análisis , Bases de Schiff/química , Espectrometría de Fluorescencia , Agua/química
11.
Am J Reprod Immunol ; 86(6): e13492, 2021 12.
Artículo en Inglés | MEDLINE | ID: mdl-34363283

RESUMEN

PROBLEM: Intravenous immunoglobulin G (IVIG) is an emerging regimen for women with reproductive failures (RF) during- or pre-pregnancy who have aberrant cellular immune reactions. Studies investigating teratogenicity of IVIG have been limited. Herein, we evaluated the fetal teratogenicity of IVIG and IVIG-related obstetric complications. METHOD OF STUDY: Women who used IVIG during pregnancy due to RF with cellular immune aberrances were enrolled from four medical centers in Korea. The pregnancy outcomes were collected. RESULTS: A total of 370 RF women who used IVIG during their pregnancy were enrolled. Most of the patients started the IVIG therapy before 12 weeks of gestation and 229 women continued IVIG treatment beyond 12 weeks of gestation. The mean age of the subjects was 34.8 years and the mean total dosage of IVIG was 125.3 g. A total of 307 women had livebirths and six of them were twins. Of 301 singleton livebirths, obstetric complications were developed as follows: preterm births (12.0%), gestational diabetes (7.0%), preeclampsia (4.0%), placental abruption (1.3%), placenta previa (4.3%), and placenta accrete (1.7%). Total six cases (1.99%) had major fetal anomalies in livebirths. The incidence of birth defects is similar to those of the general population in Korea and the previous report in infertile women. No IVIG -related viral contamination was noted. CONCLUSION: IVIG use during pregnancy did not increase obstetric complications and fetal teratogenicity. This study can be an evidence of maternal and fetal safety of IVIG administration during pregnancy.


Asunto(s)
Inmunoglobulinas Intravenosas/efectos adversos , Infertilidad Femenina/tratamiento farmacológico , Complicaciones del Embarazo/epidemiología , Nacimiento Prematuro/epidemiología , Adulto , Femenino , Humanos , Incidencia , Placenta/metabolismo , Embarazo , Complicaciones del Embarazo/inducido químicamente , Resultado del Embarazo , Nacimiento Prematuro/inducido químicamente
12.
Endocrinol Metab (Seoul) ; 36(3): 661-671, 2021 06.
Artículo en Inglés | MEDLINE | ID: mdl-34154043

RESUMEN

BACKGROUND: The nature and role of the mitochondrial stress response in adipose tissue in relation to obesity are not yet known. To determine whether the mitochondrial unfolded protein response (UPRmt) in adipose tissue is associated with obesity in humans and rodents. METHODS: Visceral adipose tissue (VAT) was obtained from 48 normoglycemic women who underwent surgery. Expression levels of mRNA and proteins were measured for mitochondrial chaperones, intrinsic proteases, and components of electron-transport chains. Furthermore, we systematically analyzed metabolic phenotypes with a large panel of isogenic BXD inbred mouse strains and Genotype-Tissue Expression (GTEx) data. RESULTS: In VAT, expression of mitochondrial chaperones and intrinsic proteases localized in inner and outer mitochondrial membranes was not associated with body mass index (BMI), except for the Lon protease homolog, mitochondrial, and the corresponding gene LONP1, which showed high-level expression in the VAT of overweight or obese individuals. Expression of LONP1 in VAT positively correlated with BMI. Analysis of the GTEx database revealed that elevation of LONP1 expression is associated with enhancement of genes involved in glucose and lipid metabolism in VAT. Mice with higher Lonp1 expression in adipose tissue had better systemic glucose metabolism than mice with lower Lonp1 expression. CONCLUSION: Expression of mitochondrial LONP1, which is involved in the mitochondrial quality control stress response, was elevated in the VAT of obese individuals. In a bioinformatics analysis, high LONP1 expression in VAT was associated with enhanced glucose and lipid metabolism.


Asunto(s)
Glucosa , Grasa Intraabdominal , Tejido Adiposo/metabolismo , Animales , Femenino , Metabolismo de los Lípidos , Ratones , Obesidad/metabolismo
13.
Bioorg Med Chem ; 41: 116222, 2021 07 01.
Artículo en Inglés | MEDLINE | ID: mdl-34058664

RESUMEN

In this research work, we have designed and synthesized some biologically useful of 1,3,4-Oxadiazoles. The structural interpretation of the synthesized compounds has been validated by using FT-IR, LC-MS, HRMS, 1H NMR and 13C NMR techniques. Moreover, the in-vitro mushroom tyrosinase inhibitory potential of the target compounds was assessed. The in-vitro study reveals that, all compounds demonstrate an excellent tyrosinase inhibitory activity. Especially, 2-(5-(2-methoxyphenyl)-1,3,4-oxadiazol-2-ylthio)-N-phenylacetamide (IC50 = 0.003 ± 0.00 µM) confirms much more significant potent inhibition activity compared with standard drug kojic acid (IC50 = 16.83 ± 1.16 µM). Subsequently, the most potent five oxadiazole compounds were screened for cytotoxicity study against B16F10 melanoma cells using an MTT assay method. The survival rate for the most potent compound was more pleasant than other compounds. Furthermore, the western blot results proved that the most potent compound considerably decreased the expression level of tyrosinase at 50 µM (P < 0.05). The molecular docking investigation exposed that the utmost potent compound displayed the significant interactions pattern within the active region of the tyrosinase enzyme and which might be responsible for the decent inhibitory activity towards the enzyme. A molecular dynamic simulation experiment was presented to recognize the residual backbone stability of protein structure.


Asunto(s)
Antineoplásicos/farmacología , Melaninas/antagonistas & inhibidores , Monofenol Monooxigenasa/antagonistas & inhibidores , Oxadiazoles/farmacología , Preparaciones para Aclaramiento de la Piel/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Humanos , Melanoma/tratamiento farmacológico , Modelos Moleculares , Simulación del Acoplamiento Molecular , Oxadiazoles/síntesis química , Oxadiazoles/química , Conformación Proteica
14.
Mol Divers ; 25(4): 2089-2106, 2021 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-32399854

RESUMEN

We have created a novel series of mushroom tyrosinase inhibitors with 1,2,4-triazole as fundamental skeleton. The target compound 1,2,4-triazol-3-ylthio)-N-phenyl acetamide derivatives 9(a-l) were synthesized by the reaction of 4- and 5-substituted 1,2,4-triazole-3-thiol derivatives 6(a-c) with 2-chloro-N-sub/un-substituted phenyl acetamide derivatives 8(a-d) under basic condition. By using the analytical techniques for instance, FTIR, LC-MS, 1H NMR and 13C NMR, the structural verification was evaluated. The novel series of the target compounds 9(a-l) has been scanned for biological activity (mushroom tyrosinase inhibition potential) which demonstrates adequate results. Interestingly, compound 9k (IC50 = 0.0048 ± 0.0016 µM) exhibits 3500 times more activity compared with standard drug kojic acid (IC50 = 16.8320 ± 1.1600 µM) against mushroom tyrosinase inhibitor. Furthermore, the cytotoxicity experiment was carried out for the highly effective target compounds (9d, 9i, 9j and 9k) by using MTT assay method for A375 human melanoma cells to define the nontoxic performance of the most effective compounds ranging from 1 to 25 µM. Furthermore, the molecular docking study delivers the thought concerning the interface of the ligand with an enzyme. Also, the dynamic simulation was accomplished for compound 9k to govern the plausible binding model.


Asunto(s)
Monofenol Monooxigenasa
15.
Obstet Gynecol Sci ; 63(6): 700-708, 2020 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-32814372

RESUMEN

OBJECTIVE: This study identified the distribution of lymphocele, as well as the factors associated with lymphocele formation, in patients undergoing pelvic and/or para-aortic lymph node dissection (PLND and/or PALND) for gynecologic malignancies. METHODS: This study was retrospective, and data were collected from patients who underwent surgical procedures including lymphadenectomy due to gynecologic malignancies from March 2013 to May 2016. Lymphocele was defined by postoperative computer tomography within 2 weeks after surgery. RESULTS: A total of 116 patients underwent lymphadenectomy, of whom, 47 (42.0%) developed lymphocele and 14 (12.1%) had symptomatic lymphocele formation. The affecting factors of lymphocele formation were PLND concomitant with PALND and a large amount of blood loss ≥600 mL (P=0.030 and P=0.006, respectively). All clinical factors were not significantly different between patients with symptomatic and asymptomatic lymphocele. Lymphocele developed more frequently in the left side (67.1%) of the body compared to the right side (48.7%), and in the pelvic area (75.9%) compared to the para-aortic area (24.1%, P<0.001, both). CONCLUSION: Lymphocele formation is more prevalent in the left and pelvic area of the body compared to the right and paraaortic side. PLND concurrent with PALND and large amounts of blood loss were significant risk factors for lymphocele formation.

16.
Spectrochim Acta A Mol Biomol Spectrosc ; 241: 118667, 2020 Nov 05.
Artículo en Inglés | MEDLINE | ID: mdl-32693367

RESUMEN

In this work, a series of the rhodamine 6G based derivatives 5a-5g, were synthesized. The structural framework of the synthesized compounds was established by using 1H NMR, 13C NMR, FT-IR, and LC-MS analytical methods. The spectroscopic properties of the target compounds were determined by using absorption and fluorescence study in four different solvents. Furthermore, the synthesized derivatives were assessed for in-vitro screening against jack bean urease inhibition and in-silico molecular docking study. The result reveals that all the compounds exhibit good urease inhibitory activity against this enzyme but among the series, the compound 5a &5c with an IC50 values of 0.1108 ±â€¯0.0038 µM and 0.1136 ±â€¯0.0295 µM shows to be most auspicious inhibitory activity compared to a standard drug (Thiourea) having IC50 value 4.7201 ±â€¯0.0546 µM. Subsequently, the molecular docking experiment was analysed to distinguish the enzyme-inhibitor binding interaction.


Asunto(s)
Ureasa , Xantenos , Inhibidores Enzimáticos/farmacología , Simulación del Acoplamiento Molecular , Espectroscopía Infrarroja por Transformada de Fourier , Relación Estructura-Actividad
17.
Medicine (Baltimore) ; 99(22): e20421, 2020 May 29.
Artículo en Inglés | MEDLINE | ID: mdl-32481439

RESUMEN

To evaluate the efficacy and feasibility of levonorgestrel-releasing intrauterine device (LNG-IUD) use longer than 5 years in women with adenomyosis.Data were retrospectively collected from patients who were treated with LNG-IUD longer than 5 years at the Chungnam National University hospital for adenomyosis diagnosed with ultrasonography from January 2006 to November 2013.A total of 131 patients who were diagnosed with adenomyosis had treated with LNG-IUD longer than 5 years. The mean duration of keeping 1 device without replacement was 58.35 ±â€Š15.98 months, and total duration of LNG-IUD treatment was 83.86 ±â€Š23.88 months. A total of 51 patients stopped using LNG-IUD after 5 years and the mean age at the time of LNG-IUD removal was 52.46 ±â€Š6.9. LNG-IUD treatment had a significant effect on both menorrhagia and dysmenorrhea starting from the first month of insertion (P < .01), which persisted until 6 years when the effect started to plateau. The decrease in uterine volume was not consistent during the treatment period. The uterine volume decreased significantly only in the first and second year of LNG-IUD treatment and then from eighth to tenth year of LNG-IUD treatment (P < .05). Adverse events after insertion of LNG-IUD decreased significantly after 5 years.LNG-IUD treatment longer than 5 years is an effective and feasible method for patients diagnosed with adenomyosis.


Asunto(s)
Adenomiosis/tratamiento farmacológico , Agentes Anticonceptivos Hormonales/administración & dosificación , Dispositivos Intrauterinos Medicados , Levonorgestrel/administración & dosificación , Adenomiosis/patología , Adulto , Agentes Anticonceptivos Hormonales/efectos adversos , Estudios de Factibilidad , Femenino , Humanos , Dispositivos Intrauterinos Medicados/efectos adversos , Levonorgestrel/efectos adversos , Menorragia/tratamiento farmacológico , Persona de Mediana Edad , Tamaño de los Órganos , Manejo del Dolor , Estudios Retrospectivos , Factores de Tiempo , Útero/efectos de los fármacos , Útero/patología
18.
Bioorg Chem ; 100: 103906, 2020 07.
Artículo en Inglés | MEDLINE | ID: mdl-32422387

RESUMEN

A new series of 4H-chromene-3-carboxylate derivatives were synthesized using multicomponent reaction of salicylaldehyde, ethyl acetoacetate and dimedone in ethanol with K3PO4 as a catalyst at 80 °C. The structures of all newly synthesized compounds were confirmed by spectral techniques viz. IR, 1H NMR, 13C NMR, and LCMS analysis. The newly synthesized compounds 4a to 4j were screened against elastase enzyme. Interestingly, all these compounds found to be potent elastase inhibitors with much lower IC50 value. The compound 4b was found to be most potent elastase inhibitor (IC50 = 0.41 ± 0.01 µM) amongst the synthesized series against standard Oleanolic Acid (IC50 value = 13.45 ± 0.0 µM). The Kinetics mechanism for compound 4b was analyzed by Lineweaver-Burk plots which revealed that compound inhibited elastase competitively by forming an enzyme-inhibitor complex. Along with this, all the synthesized compounds (4a - 4j) exhibits excellent DPPH free radical scavenging ability. The inhibition constant Ki for compound 4b was found to be 0.6 µM. The computational study was comprehensible with the experimental results with good docking energy values (Kcal/mol). Therefore, these molecules can be considered as promising medicinal scaffolds for the treatment of skin-related maladies.


Asunto(s)
Benzopiranos/química , Benzopiranos/farmacología , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacología , Elastasa Pancreática/antagonistas & inhibidores , Animales , Benzopiranos/síntesis química , Ácidos Carboxílicos/síntesis química , Ácidos Carboxílicos/química , Ácidos Carboxílicos/farmacología , Quimioinformática , Inhibidores Enzimáticos/síntesis química , Simulación del Acoplamiento Molecular , Páncreas/enzimología , Elastasa Pancreática/química , Elastasa Pancreática/metabolismo , Porcinos
19.
J Fluoresc ; 30(2): 397-406, 2020 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-32088851

RESUMEN

New porphyrin analogues have been designed and synthesized using pyrrole, various aldehydes and propionic acid. The formation of desired compounds was analyzed by utilizing the spectral analysis such as IR, NMR and Mass spectroscopy. The studies on absorption and fluorescence emission of synthesized porphyrins were used to evaluate photophysical characteristics such as molar excitation coefficient and Stokes shift. The estimated values of fluorescence lifetime and fluorescence quantum yield of synthesized porphyrins were found to be variable due to the presence of change in the electron donating and withdrawing characters. The efficiency of generation of singlet oxygen by each synthesized porphyrin as photosensitizer was measured in terms of singlet oxygen quantum yield through photooxidation of 9,10-dimethylantharacene. The obtained singlet oxygen quantum yield values were found to be higher in case of porphyrins those have more electron withdrawing characters rather than donating characters as compared to reference 5,10,15,20-tetraphenylporphyrin (H2TPP). The singlet oxygen quantum yield values of synthesized porphyrins varied from 0.52 to 0.66. Pleasingly, some of synthesized porphyrins are found to be photostable and competent to discover as PDT agents as compared to reference H2TPP.


Asunto(s)
Diseño de Fármacos , Fotoquimioterapia , Fármacos Fotosensibilizantes/síntesis química , Porfirinas/síntesis química , Estructura Molecular , Fármacos Fotosensibilizantes/química , Porfirinas/química , Espectrometría de Fluorescencia
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