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1.
BMC Health Serv Res ; 20(1): 57, 2020 Jan 23.
Artigo em Inglês | MEDLINE | ID: mdl-31973759

RESUMO

BACKGROUND: To assess the effects of a motivational interviewing (MI)-based patient empowerment program (PEP) on type 2 diabetes mellitus (DM) patient self-management compared to traditional diabetes health education. METHODS: Two hundred and twenty-five patients, recruited from community health centers (CHCs) and the family medicine clinic in the University of Hong Kong-Shenzhen Hospital in Shenzhen, were randomly assigned to the intervention or control groups. Patients in the intervention group (n = 117) received a four-session PEP in small groups over 1 month by trained nurses and doctors. The control group (n = 108) received the traditional lecture-style health education on DM. All the patients were followed up for 3 months. Outcomes included problem areas in diabetes (PAID) that measures diabetes-related emotional distress, patient enablement index (PEI), mental health, patient satisfaction respectively as well as lifestyle behaviors were assessed at baseline, post-activity and 3 months. RESULTS: At post-intervention and the 3-month follow-up, the PAID score improved significantly in the intervention group (12.7 ± 13.6, 5.8 ± 7.6) compared to the control group (22.7 ± 22.8, 11.7 ± 14.6). No difference was found between groups for changes to exercise, diet, and medication adherence. The PEI score improved significantly at the 3-month follow-up in the MI group (7.27 ± 2.45 vs 5.81 ± 2.97). CONCLUSION: The PEP has a significant effect on improving diabetes-related distress, but MI was not significantly different from the traditional health education programs when it comes to the readiness to change. TRIAL REGISTRATION: NCT04120844, ClinicalTrials.Gov. Date of registration: October 9th 2019 (Retrospectively registered).

2.
J Labelled Comp Radiopharm ; 63(3): 129-143, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31919866

RESUMO

Prostate-specific membrane antigen (PSMA) is the most promising target for radioligand therapy of prostate cancer. The aim of this study was to prepare a small molecular ligand p-SCN-Bn-TCMC-PSMA (NG001) and compare it with the commonly used DOTA-based PSMA-617. The PSMA-targeting ability of the 212 Pb-labelled ligands was evaluated using PSMA-positive C4-2 human prostate cancer cells. Lead-212 is an in vivo generator of alpha particles by its daughter nuclides 212 Bi and 212 Po. NG001 was synthesized by conjugating the isothiocyanato group of p-SCN-Bn-TCMC to the amino group of a glutamate-urea-based PSMA-binding entity. Molecular size, chelator unit and chelator linking method are different in NG001 and PSMA-617. Both ligands were efficiently labelled with 212 Pb using a 224 Ra/212 Pb-solution generator in transient equilibrium with progeny. Lead-212-labelled NG001 was purified with a yield of 85.9±4.7% and with 0.7±0.2% of 224 Ra. Compared with [212 Pb]Pb-PSMA-617, [212 Pb]Pb-NG001 displayed a similar binding and internalization in C4-2 cells, with comparable tumour uptake in mice bearing C4-2 tumours, but almost a 2.5-fold lower kidney uptake. Due to the rapid normal tissue clearance and tumour cell internalization, any significant translocalization of 212 Bi was not detected in mice. In conclusion, the obtained results warrant further preclinical studies to evaluate the therapeutic efficacy of [212 Pb]Pb-NG001.

3.
Anal Chem ; 2019 Nov 14.
Artigo em Inglês | MEDLINE | ID: mdl-31682106

RESUMO

Surface enhanced Raman spectroscopy (SERS) is an ultrasensitive label-free analytical technique that can provide unique chemical and structural fingerprint information. However, gaining reliable quantitative analysis with SERS remains a huge challenge because of poor reproducibility and the instability of nanostructured SERS active surfaces. Herein, an effective strategy of coating Au nanoparticles (NPs) with ultrathin and uniform Prussian blue (PB) shell (Au@PB NPs) was developed for quantitative detection of dopamine (DA) concentrations in blood serum and crystal violet (CV) contaminants in lake water. The only intense PB Raman signal at 2155 cm-1 served as an ideal and interference-free internal standard (IS) for correcting fluctuations in the Raman intensities of analytes. Also, the stability of Au@PB NPs was investigated, exhibiting good functionality in strong acid solutions and thermal stability at 100 °C. This work demonstrates a convenient and fast quantitative SERS technique for detecting analyte concentrations in complex systems and has a great number of potential applications for use in analytical chemistry.

4.
Cancer Biol Med ; 14(1): 42-49, 2017 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-28443202

RESUMO

Colorectal carcinoma (CRC) is a common cause of morbidity and mortality worldwide. Two pathogenic pathways are involved in the development of adenoma to CRC. The first pathway involvesAPC/ß-catenin characterized by chromosomal instability resulting in the accumulation of mutations. The second pathway is characterized by lesions inDNA mismatch repair genes. Aberrant DNA methylation in selected gene promoters has emerged as a new epigenetic pathway in CRC development. CRC screening is the most efficient strategy to reduce death. Specific DNA methylation events occur in multistep carcinogenesis. Epigenetic gene silencing is a causative factor of CRC development. DNA methylations have been extensively examined in stool from CRC and precursor lesions. Many methylated genes have been described in CRC and adenoma, although no definite DNA methylation biomarkers panel has been established. Multiple DNA methylation biomarkers, including secreted frizzled-related protein 2, secreted frizzled-related protein 1, tissue factor pathway inhibitor 2, vimentin, and methylguanine DNA methyltransferase, have been further investigated, and observations have revealed that DNA methylation biomarkers exhibit with high sensitivity and specificity. These markers may also be used to diagnose CRC and adenoma in early stages. Real time polymerase chain reaction (qPCR) is sensitive, scalable, specific, reliable, time saving, and cost effective. Stool exfoliated markers provide advantages, including sensitivity and specificity. A stool qPCR methylation test may also be an enhanced tool for CRC and adenoma screening.

5.
J Cell Physiol ; 232(9): 2308-2311, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-27791271

RESUMO

The mammalian Sirtuins are a family of highly conserved nicotinamide adenine dinucleotide (NAD+)-dependent histone deacetylase. The mammalian Sirtuins family has identified seven different types of sirtuin. Sirtuins 3(SirT3) is localized to mitochondria, and is a multiple functional protein deacylase through deacetylating a variety of substrates. Cellular senescence represents a permanent withdraw from cell cycle in response to diverse stress; it is controlled by the p53 and retinoblastoma protein (RB) tumor suppressors, and constitutes a potent anticancer mechanisms. p53 can be deacetylated by a protein complex containing histone deacetylases (HDAC1). There is possibility that SirT3 may also deacetylate p53. We introduce the recent research on the SirT3-p53 interplay directly and indirectly, and discuss the significance of p53 deacetylation by SirT3 in the aging and cancer. J. Cell. Physiol. 232: 2308-2311, 2017. © 2016 Wiley Periodicals, Inc.


Assuntos
Envelhecimento/metabolismo , Neoplasias/enzimologia , Transdução de Sinais , Sirtuína 3/metabolismo , Proteína Supressora de Tumor p53/metabolismo , Acetilação , Envelhecimento/patologia , Animais , Humanos , Modelos Moleculares , Neoplasias/patologia , Conformação Proteica , Sirtuína 3/química , Proteína Supressora de Tumor p53/química
6.
Eur J Med Chem ; 62: 605-13, 2013 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-23434529

RESUMO

Nordihydroguaiaretic acid (NDGA) and its synthetic analogues are potentially useful in treating diseases related to cancers, diabetes, viral and bacterial infections, and inflammation. In this paper, we report the optimal synthetic methods and the bioactivity study of terameprocol 2, NDGA derivative 3, and its cyclized analogue 4. The IC50 of these three compounds 2, 3 and 4 on the growth metabolism of Schizosacchromyces pombe and K562 cell lines were determined by microcalorimetry. The preliminary results showed that the compounds 2, 3 and 4 possessed good inhibition activities on S. pombe and K562 cell lines, and exhibited bidirectional biological effect and Hormesis effect. In particular, terameprocol 2 was found to possess the most potent inhibitory effect on K562 cell lines.


Assuntos
Antifúngicos/farmacologia , Masoprocol/farmacologia , Schizosaccharomyces/efeitos dos fármacos , Antifúngicos/síntese química , Antifúngicos/química , Relação Dose-Resposta a Droga , Humanos , Células K562 , Masoprocol/síntese química , Masoprocol/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade , Células Tumorais Cultivadas
7.
Curr Top Med Chem ; 9(17): 1636-59, 2009.
Artigo em Inglês | MEDLINE | ID: mdl-19903157

RESUMO

Nordihydroguaiaretic acid is a natural occurring lignan mainly isolated and commercially produced from desert plant, creosote bush (Larrea divaricata Cav. Or Corillea tridentate), which can be widely found in the border zone of southern of USA and northern of Mexico. During past 100 years, extensive research has demonstrated that nordihydroguaiaretic acid and its synthetic analogues are potentially useful in treating diseases related to cancers, diabetes, viral, bacterial infections, and inflammation. Remarkably, terameprocol, a tetra-O-methyl derivative of nordihydroguaiaretic acid, is currently in Phase I/II clinical trials as an anticancer agent. This review deals with the chemical synthesis and bioactivities of nordihydroguaiaretic acid and its structurally-related derivatives, which possess anticancer, antioxidant, antimicrobial, anti-inflammatory and immunosuppressive activities. The review consists of the data reported in over 100 publications.


Assuntos
Anti-Infecciosos/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Anticarcinógenos/farmacologia , Antioxidantes/farmacologia , Imunossupressores/farmacologia , Masoprocol/análogos & derivados , Masoprocol/farmacologia , Animais , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Anti-Inflamatórios não Esteroides/síntese química , Anti-Inflamatórios não Esteroides/química , Anticarcinógenos/síntese química , Anticarcinógenos/química , Antioxidantes/síntese química , Antioxidantes/química , Produtos Biológicos/síntese química , Produtos Biológicos/química , Produtos Biológicos/farmacologia , Humanos , Imunossupressores/síntese química , Imunossupressores/química , Masoprocol/síntese química , Masoprocol/química
8.
PLoS One ; 3(6): e2469, 2008 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-18575595

RESUMO

BACKGROUND: Therapeutic intervention in many neurological diseases is thwarted by the physical obstacle formed by the blood-brain barrier (BBB) that excludes most drugs from entering the brain from the blood. Thus, identifying efficacious modes of drug delivery to the brain remains a "holy grail" in molecular medicine and nanobiotechnology. Brain capillaries, that comprise the BBB, possess an endogenous receptor that ferries an iron-transport protein, termed p97 (melanotransferrin), across the BBB. Here, we explored the hypothesis that therapeutic drugs "piggybacked" as conjugates of p97 can be shuttled across the BBB for treatment of otherwise inoperable brain tumors. APPROACH: Human p97 was covalently linked with the chemotherapeutic agents paclitaxel (PTAX) or adriamycin (ADR) and following intravenous injection, measured their penetration into brain tissue and other organs using radiolabeled and fluorescent derivatives of the drugs. In order to establish efficacy of the conjugates, we used nude mouse models to assess p97-drug conjugate activity towards glioma and mammary tumors growing subcutaneously compared to those growing intracranially. PRINCIPAL FINDINGS: Bolus-injected p97-drug conjugates and unconjugated p97 traversed brain capillary endothelium within a few minutes and accumulated to 1-2% of the injected by 24 hours. Brain delivery with p97-drug conjugates was quantitatively 10 fold higher than with free drug controls. Furthermore, both free-ADR and p97-ADR conjugates equally inhibited the subcutaneous growth of gliomas growing outside the brain. Evocatively, only p97-ADR conjugates significantly prolonged the survival of animals bearing intracranial gliomas or mammary tumors when compared to similar cumulated doses of free-ADR. SIGNIFICANCE: This study provides the initial proof of concept for p97 as a carrier capable of shuttling therapeutic levels of drugs from the blood to the brain for the treatment of neurological disorders, including classes of resident and metastatic brain tumors. It may be prudent, therefore, to consider implementation of this novel delivery platform in various clinical settings for therapeutic intervention in acute and chronic neurological diseases.


Assuntos
Antineoplásicos/administração & dosagem , Barreira Hematoencefálica , Portadores de Fármacos , Animais , Antineoplásicos/farmacocinética , Antineoplásicos/uso terapêutico , Neoplasias Encefálicas/tratamento farmacológico , Doxorrubicina/administração & dosagem , Doxorrubicina/farmacocinética , Doxorrubicina/uso terapêutico , Corantes Fluorescentes , Humanos , Camundongos , Camundongos Nus , Paclitaxel/administração & dosagem , Paclitaxel/farmacocinética , Paclitaxel/uso terapêutico
9.
Chemistry ; 13(13): 3630-5, 2007.
Artigo em Inglês | MEDLINE | ID: mdl-17238212

RESUMO

A series of flexible bis(9-anthryldiamine) ligands (L1-L3) linked with alkyl spacers of different chain length was synthesized and characterized, in order to investigate the coordination behavior of these diamine ligands with metal ions (Zn2+, etc.) based on fluorescence measurements. The results showed that, in the case of anthryldiamine ligands bearing two- or four-carbon links, the zinc ion induced a chelation-enhanced fluorescence (CHEF) effect in aqueous media, while a trace amount of water could selectively quench the blue emission of the Zn(II) complex with a three-carbon-linked ligand (1). Meanwhile, the introduction of more water (concentration >11 %) resulted in the formation of a new green luminescent species; the luminescence intensity was enhanced stepwise to a maximum with addition of approximately 30 % water in THF solution. The peak position (centered at approximately 500 nm) and the lifetime measurement (tau=19.59 ns) indicated that the green luminescence was attributable to a novel edge-to-face dimeric conformation ("T-shaped" conformation) of anthracene, and not to the more common face-to-face dimeric conformation. Accordingly, 1H NMR spectroscopic studies in nonaqueous or aqueous solution confirmed this T-shaped conformation, which is consistent with the results of single-crystal X-ray structure analysis and solid-state photoluminescence studies.


Assuntos
Antracenos/química , Corantes Fluorescentes/química , Raios Ultravioleta , Zinco/química , Antracenos/efeitos da radiação , Cristalografia por Raios X , Corantes Fluorescentes/efeitos da radiação , Ligantes , Espectroscopia de Ressonância Magnética , Modelos Moleculares , Estrutura Molecular , Água/química , Zinco/efeitos da radiação
11.
J Org Chem ; 67(14): 4997-5000, 2002 Jul 12.
Artigo em Inglês | MEDLINE | ID: mdl-12098323

RESUMO

Novel tetra-N-confused cyclohexapyrrole is synthesized for the first time via condensation of tripyrrinone-aldehyde with bis(2,4-dimethylpyrrole-3-yl)methane in the presence of p-toluenesulfonic acid monohydrate. X-ray crystal analysis indicates that it adopts a nonplanar conformation with a conelike shape.

12.
J Org Chem ; 63(8): 2665-2675, 1998 Apr 17.
Artigo em Inglês | MEDLINE | ID: mdl-11672135

RESUMO

A model for one-half bilirubin, the neurotoxic yellow-orange pigment of jaundice, 9-[2-(2-carboxyethyl)benzyl]-2,3,7,8-tetramethyl-1,10-dihydrodipyrrin (1, hemirubin) was synthesized following SnCl(4)-catalyzed Friedel-Crafts acylation at C(9) of 2,3,7,8-1-oxo-1,10-dihydrodipyrrin (7) with methyl o-(chlorocarbonyl)hydrocinnamate. Unlike earlier bilirubin model compounds, hemirubin is predicted and found to engage in intramolecular hydrogen bonding. Like bilirubin, the propionic acid carboxyl group of hemirubin is linked to the opposing dipyrrinone by intramolecular hydrogen bonds, and thus, 1 shares in some of the solution properties of its parent bilirubin, e.g., an acid that is less polar than its methyl ester.

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