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1.
J Orthop Surg Res ; 19(1): 171, 2024 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-38448954

RESUMO

BACKGROUND: Surgery for intertrochanteric fractures in elderly patients is challenging due to the risk of severe pain and significant stress responses. We investigated the effects of a combined approach of ultrasound-guided lumbar plexus and sacral plexus block with general anesthesia on anesthetic efficacy and surgical outcomes in these patients. METHODS: A randomized controlled trial was conducted involving 150 elderly patients, divided into two groups: the combined anesthesia group (receiving ultrasound-guided lumbar plexus and sacral plexus block along with general anesthesia) and the general anesthesia alone group. Outcome measures included hemodynamic parameters, postoperative pain levels (VAS scores), postoperative recovery times, and incidence of adverse reactions. RESULTS: In the combined anesthesia group, the patients had more stable intraoperative hemodynamics, lower postoperative VAS scores at 1, 3, and 6 h, and faster recovery times (eye-opening upon command and return of respiratory function) compared to the general anesthesia group. Furthermore, the incidence of adverse reactions was significantly lower in the combined anesthesia group. CONCLUSIONS: Ultrasound-guided lumbar plexus and sacral plexus block combined with general anesthesia enhanced the anesthetic efficacy and improved surgical outcomes in elderly patients undergoing intertrochanteric fracture surgery.


Assuntos
Anestésicos , Fraturas do Quadril , Idoso , Humanos , Anestesia Geral , Plexo Lombossacral , Fraturas do Quadril/cirurgia , Resultado do Tratamento , Ultrassonografia de Intervenção
2.
Nat Prod Commun ; 11(5): 655-6, 2016 May.
Artigo em Inglês | MEDLINE | ID: mdl-27319142

RESUMO

Despite their diverse pharmacological effects, polyphenols are poor for use as drugs, which have been traditionally ascribed to their low bioavailability. However, Baell and co-workers recently proposed that the redox potential of polyphenols also plays an important role in this, because redox reactions bring promiscuous actions on various protein targets and thus produce non-specific pharmacological effects. To investigate whether the redox reactivity behaves as a critical factor in polyphenol promiscuity, we performed a chemical bioinformatics analysis on the structure-activity relationships of twenty polyphenols. It was found that the gene expression profiles of human cell lines induced by polyphenols were not correlated with the presence or not of redox moieties in the polyphenols, but significantly correlated with their molecular structures. Therefore, it is concluded that the promiscuous actions of polyphenols are likely to result from their inherent structural features rather than their redox potential.


Assuntos
Polifenóis/química , Linhagem Celular , Biologia Computacional , Perfilação da Expressão Gênica , Humanos , Oxirredução , Relação Estrutura-Atividade
3.
Brain Res Bull ; 110: 26-9, 2015 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-25446738

RESUMO

Alzheimer's disease (AD) is a disease that threatens the elderly. No efficient therapeutic method is currently available to combat AD. Drug repurposing has provided a new route for AD drug discovery, and medical genetics has shown potential in target-based drug repurposing. We compared AD-associated genes with approved drug targets and found that three are targeted by 23 approved drugs. Thus, these drugs may be used to treat AD according to the medical genetic information of the targets. In vitro and in vivo experiments revealed that four drugs, all of which are angiotensin-converting enzyme (ACE) inhibitors, had potential to treat AD.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Doença de Alzheimer/genética , Reposicionamento de Medicamentos/métodos , Inibidores da Enzima Conversora de Angiotensina/farmacologia , Inibidores da Enzima Conversora de Angiotensina/uso terapêutico , Animais , Humanos , Nootrópicos/farmacologia , Nootrópicos/uso terapêutico
4.
J Med Food ; 17(9): 955-62, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-25045784

RESUMO

This study aims at evaluating the anticancer effects of berberine hydrochloride (berberine) and d-limonene, alone and in combination, on human gastric carcinoma cell line MGC803 to determine whether berberine and d-limonene work synergistically and elucidate their mechanisms. MGC803 cells were treated with berberine and d-limonene, alone and in combination, for 24-48 h. The inhibitory effects of these drugs on growth were determined by MTT assay. The combination index and drug reduction index were calculated with the Chou-Talalay method based on the median-effect principle. Flow cytometry and laser scanning confocal microscopy were employed to evaluate the effects of both drugs on cell-cycle perturbation and apoptosis, generation of reactive oxygen species (ROS), mitochondrial membrane potential, and expression of Bcl-2 and caspase-3 in MGC803 cells. Berberine or d-limonene alone can inhibit the growth of MGC803 cells in a dose- and time-dependent manner. Berberine and d-limonene at a combination ratio of 1:4 exhibited a synergistic effect on anti-MGC803 cells. The two drugs distinctly induced intracellular ROS generation, reduced the mitochondrial transmembrane potential (ΔΨm), enhanced the expression of caspase-3, and decreased the expression of Bcl-2. The combination of berberine and d-limonene showed more remarkable effects compared with drugs used singly in MGC803 cells. The combination of berberine and d-limonene exerted synergistic anticancer effects on MGC803 cells by cell-cycle arrest, ROS production, and apoptosis induction through the mitochondria-mediated intrinsic pathway.


Assuntos
Antineoplásicos Fitogênicos/uso terapêutico , Berberina/uso terapêutico , Cicloexenos/uso terapêutico , Fitoterapia , Extratos Vegetais/uso terapêutico , Neoplasias Gástricas/tratamento farmacológico , Terpenos/uso terapêutico , Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Berberina/farmacologia , Caspase 3/metabolismo , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Coptis/química , Cicloexenos/farmacologia , Relação Dose-Resposta a Droga , Sinergismo Farmacológico , Evodia/química , Humanos , Limoneno , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Extratos Vegetais/farmacologia , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Neoplasias Gástricas/metabolismo , Terpenos/farmacologia
5.
Molecules ; 13(5): 1189-94, 2008 May 23.
Artigo em Inglês | MEDLINE | ID: mdl-18560337

RESUMO

Epidemiological analyses in a large Chinese population have revealed that consumption of vegetables and legumes is inversely associated with the risk of type 2 diabetes (T2D). However, the health benefits of these plants have not been fully explained, which stimulated our interest to identify antidiabetic components from vegetables and legumes through searching medicinal databases, especially those containing traditional Chinese medicines. The results not only provide meaningful clues to understanding the antidiabetic potentials of these plants but also display the possibility of pinpointing food component functions by searching medicinal databases.


Assuntos
Fabaceae/química , Hipoglicemiantes/farmacologia , Verduras/química , Diabetes Mellitus Tipo 2/tratamento farmacológico , Avaliação Pré-Clínica de Medicamentos , Hipoglicemiantes/química , Hipoglicemiantes/uso terapêutico , Medicina Tradicional Chinesa , Estruturas Vegetais
7.
Molecules ; 12(4): 878-84, 2007 Apr 30.
Artigo em Inglês | MEDLINE | ID: mdl-17851440

RESUMO

By examination of the 8659 drugs recorded in the Comprehensive Medicinal Chemistry (CMC) database, 78 catecholics (including five pyrogallolics) were identified, of which 17 are currently prescribed by FDA. Through analyzing the substituent patterns, ClogPs and O-H bond dissociation enthalpies (BDEs) of the catecholic drugs, some molecular features that may benefit circumventing the toxicity of catecholics were revealed: i) strong electron-donating substituents are excluded; ii) ClogP 3; iii) an energy penalty exists for quinone formation. Besides, the present analyses also suggest that the clinical usage and dosage of currently prescribed catecholic drugs are of importance in designing or screening catecholic antioxidants.


Assuntos
Catecóis/química , Química Farmacêutica/métodos , Antioxidantes/química , Bases de Dados como Assunto , Desenho de Fármacos , Avaliação Pré-Clínica de Medicamentos , Radicais Livres , Hidrogênio/química , Ligação de Hidrogênio , Modelos Químicos , Estrutura Molecular , Oxigênio/química , Termodinâmica
8.
Drug Discov Today ; 11(15-16): 749-54, 2006 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-16846803

RESUMO

Free-radicals play an important role in the pathogenesis of many diseases, accounting for continuing interest in the identification and development of novel antioxidants that prevent radical-induced damage. To develop more-powerful weapons that address complex diseases in which free-radicals might be significant, but not exclusive drivers, antioxidants that also have other pharmacological effects are desired. To obtain multipotent antioxidants, one can screen drug collections and/or natural-product libraries, or couple an antioxidant group with other pharmacophores. It is interesting to note that most rationally designed multifunctional antioxidants are structurally different from their naturally occurring counterparts. Therefore, nature's design strategy provides important clues as to how the design concept for multipotent antioxidants can be improved.


Assuntos
Antioxidantes/farmacologia , Desenho de Fármacos , Avaliação Pré-Clínica de Medicamentos/métodos , Animais , Antioxidantes/química , Antioxidantes/uso terapêutico , Humanos , Estrutura Molecular , Tecnologia Farmacêutica/métodos , Tecnologia Farmacêutica/tendências
9.
Bioorg Med Chem ; 13(4): 1031-6, 2005 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-15670910

RESUMO

To elucidate the structure-activity relationships of metabolites of folates as antioxidants, the O-H bond dissociation enthalpies (BDEs) and ionization potentials (IPs) for these compounds were calculated by density functional theory (DFT) on B3LYP/6-31+G(,3pd) level. Accordingly, the antioxidant activity difference for metabolites of folates can be elucidated by O-H BDE and IP values and can be further explained in terms of electronic effect and intramolecular hydrogen bond effect of substituents. Furthermore, the potential of the active center of metabolites of folates, 4-hydroxypyrimidine (4-HP), as lead antioxidant, was evaluated by comparing the BDEs and IPs of 4-HP with those of 5-hydroxypyrimidine (5-HP). It was revealed that 4-HP and 5-HP held identical IPs, but the O-H BDE of the former was 22.84 kcal/mol higher than that of the latter, which meant 4-HP was inert in H-atom donation. Nevertheless, the O-H BDE of 4-HP was very sensitive to the substituents, which made NH2-derivatives of 4-HP very active as antioxidants. Therefore, 4-HP is also a potential lead antioxidant and deserves attention in rational design of antioxidants.


Assuntos
Antioxidantes/química , Antioxidantes/farmacologia , Desenho de Fármacos , Ácido Fólico/metabolismo , Modelos Químicos , Ácido Fólico/química , Ácido Fólico/farmacologia , Relação Estrutura-Atividade
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