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1.
Angew Chem Int Ed Engl ; 60(23): 12829-12834, 2021 06 01.
Artigo em Inglês | MEDLINE | ID: mdl-33817919

RESUMO

Heme-like metal-chelating macrocycles, including expanded and contracted porphyrins, are of everlasting interest as drug candidates for numerous diseases. Still, all reported corrole derivatives (and most other heme analogues) do not fulfill the most basic standards expected for oral drug administration: a combination of low molecular weight and reasonable water solubility. We now disclose a very straightforward synthetic method that relies on surprisingly facile trifluoromethyl hydrolysis for gaining access to a new class of corroles that do satisfy all druglikeness criteria. The relevance is briefly exemplified for the iron corroles by demonstrating the ability to affect their association with plasma proteins and their performance for catalase-like decomposition of hydrogen peroxide.


Assuntos
Complexos de Coordenação/química , Hidrocarbonetos Fluorados/química , Hidrólise , Estrutura Molecular
2.
Surg Technol Int ; 35: 17-26, 2019 11 10.
Artigo em Inglês | MEDLINE | ID: mdl-31476791

RESUMO

Due to its decreased recovery time and increased patient satisfaction, laparoscopic surgery has witnessed an exponential rise in the last decade. In fact, the indications for laparoscopic surgery are currently numerous and involve multiple disciplines, including gastro-intestinal and gynecological surgery. With this boom, there is much focus on decreasing the rate of complications due to laparoscopy. This includes, but is not limited to, an increased interest in decreasing the risk of port-site herniation by ensuring proper closure of the abdominal wall at the site of port-insertion.


Assuntos
Parede Abdominal , Técnicas de Fechamento de Ferimentos Abdominais , Laparoscopia , Fáscia , Feminino , Procedimentos Cirúrgicos em Ginecologia , Humanos , Laparoscopia/métodos
3.
Surg Technol Int ; 31: 140-143, 2017 Dec 22.
Artigo em Inglês | MEDLINE | ID: mdl-29313317

RESUMO

Nabothian cysts are mucinous retention cysts formed through the accumulation of cervical mucus inside blocked cervical crypts leading to non-neoplastic mucinous cystic lesion in relation to the uterine cervix. The formation of Nabothian cysts is a common gynecological benign condition in women of reproductive age. While the presence of small-sized Nabothian cysts is usually clinically asymptomatic and requires no treatment or intervention, the diagnosis of larger Nabothian cysts can be mistaken with malignant tumors, including mucin producing carcinomas such as Adenoma malignum. In this study, we report the case of a large Nabothian cyst that was correctly diagnosed preoperatively using ultrasonography and magnetic resonance imaging (MRI), and successfully treated through laparoscopic excision, avoiding the performance of unnecessary hysterectomy. A 44-year old Lebanese patient presented with chronic dyspareunia and pelvic pain. An ultrasound was performed and revealed an 8cm multiloculated anechoic pelvic cystic lesion with no solid components. An MRI was performed and showed an 8cm mass lateral to the right vaginal wall, suggestive of a Nabothian cyst. The patient was scheduled for laparoscopic removal of the Nabothian cyst. The patient tolerated the procedure well and was discharged under stable condition a few hours after the operation. Careful preoperative examination, including the use of imaging methods such as ultrasonogoraphy and MRI, is crucial for diagnosis and differentiation of atypical presentation of benign, but large and complex, Nabothian cysts from other differential conditions of malignancies, consequently avoiding unnecessary hysterectomy. Use of laparoscopy as a minimally-invasive technique to excise such cysts is considered a valid option, allowing for a fast recovery for the patients.


Assuntos
Colo do Útero , Cistos , Neoplasias do Colo do Útero , Adulto , Colo do Útero/diagnóstico por imagem , Colo do Útero/cirurgia , Cistos/diagnóstico por imagem , Cistos/cirurgia , Feminino , Humanos , Laparoscopia , Imageamento por Ressonância Magnética , Ultrassonografia , Neoplasias do Colo do Útero/diagnóstico por imagem , Neoplasias do Colo do Útero/cirurgia
5.
J Med Chem ; 66(1): 766-776, 2023 01 12.
Artigo em Inglês | MEDLINE | ID: mdl-36516110

RESUMO

A nanoparticle-based system, composed of the gallium(III) complex of a minimally substituted corrole that is coated by transferrin as a targeting vehicle (3-Ga NPs), has been used for pre-clinical evaluation of its efficacy against human metastatic castration-resistant prostate cancer (mCRPC) tumor xenografts. All mice (N = 9) responded to a dose of 10 mg/kg, with a remarkable tumor growth inhibition of 400% following 2 weeks of treatment; Ames and hERG tests excluded potential concerns regarding mutagenicity and cardiotoxicity, respectively. Also demonstrated is the potential application of these 3-Ga NPs as sonodynamic agents for the preclinical treatment of pancreatic cancer. 10 mg/kg 3-Ga NPs combined with exposure to ultrasound waves (2 min of 1 MHz 0.1 w/cm2 twice a week) induced up to 77% tumor shrinkage. Consistently, tumor/tissue distribution and serum levels of 3-Ga NPs in mice revealed high tumor specificity, favorable pharmacokinetics, fast absorption, slower redistribution, and very slow drug clearance.


Assuntos
Nanopartículas , Neoplasias Pancreáticas , Porfirinas , Neoplasias de Próstata Resistentes à Castração , Masculino , Humanos , Animais , Camundongos , Neoplasias de Próstata Resistentes à Castração/tratamento farmacológico , Porfirinas/uso terapêutico , Neoplasias Pancreáticas/tratamento farmacológico , Neoplasias Pancreáticas
6.
Org Lett ; 22(8): 3119-3122, 2020 04 17.
Artigo em Inglês | MEDLINE | ID: mdl-32227962

RESUMO

Separate focus on the oligomerization and oxidative cyclization steps required for the synthesis of 5,10,15-tris(trifluoromethyl)corrole revealed [bis(trifluoroacetoxy)iodo]benzene (PIFA) as a superior alternative oxidant. Under optimized conditions, the pure free-base corrole was obtained with a 6-fold increase in chemical yield and an 11-fold rise in isolated material per synthesis. The corresponding gallium(III) and manganese(III) complexes were isolated by adding the appropriate metal salt prior to corrole purification.


Assuntos
Porfirinas/síntese química , Gálio/química , Manganês/química , Estrutura Molecular , Compostos Organometálicos/química , Porfirinas/química , Porfirinas/isolamento & purificação
7.
Radiol Res Pract ; 2019: 1406291, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31354994

RESUMO

Ovarian/adnexal torsion is a rather frequent occurrence in women of reproductive age group worldwide. Etiologies are quite diverse with ovarian lesions and corpus luteal cysts being the most two common. Pelvic or intravaginal ultrasound remains the first-line imaging modality used for diagnosis and evaluation of suspected ovarian/adnexal torsion. In this study, we have adopted a case-based statistical analysis to identify important sonographic markers and further evaluated their contribution in identifying ovarian torsion. Our study successfully determined the important sonographic markers. Our observation and analysis suggest that ovarian enlargement is the most sensitive marker. Ovarian edema was found to be the most specific marker to identify the ovarian torsion with higher level of accuracy and confidence. This pioneer study will provide valuable information and direction to the medical practitioners and radiologists for better diagnosis. Further studies with large sample size will help in establishing our findings universally.

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