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1.
Biol Pharm Bull ; 39(6): 935-45, 2016 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-26983907

RESUMO

Among mitotic kinases, Aurora kinases are the most widely studied, since their expression is restricted to mitosis. They play a key role in chromosome segregation and cell polyploidy. Aurora kinases are important therapeutic targets, and several research groups have directed their efforts toward the identification of kinase inhibitors. The aim of this study is to screen and characterize Aurora kinase inhibitors from natural substances extracted from plants that are used in the Vietnamese pharmacopoeia. We have characterized in vitro Derrone, extracted from Erythrina orientalis L. MURR, as a novel Aurora kinase inhibitor. This compound exhibited an ability to inhibit the phosphorylation of histone H3 at ser10 both in kinase assay and at the cellular level. The compound was more effective against Aurora kinase B, with a lower IC50 value as compared to Aurora A. Moreover, it impaired the mitotic spindle checkpoint and led to endoreduplication in cancer cells, a phenomenon caused by an Aurora B inhibitor. Interestingly, using the xCelligence system and real-time cell analysis (RTCA) software, we set up a comparison of cell proliferation profiles between cancer cells treated with Derrone and VX680-a well-known Aurora kinase inhibitor-and we found that these profiles exhibited considerable similarity in cell morphology, growth, and death. Additionally, Derrone significantly inhibited the formation and growth of MCF7 tumor spheroids.


Assuntos
Antineoplásicos/farmacologia , Aurora Quinase A/antagonistas & inibidores , Aurora Quinase B/antagonistas & inibidores , Flavonoides/farmacologia , Inibidores de Proteínas Quinases/farmacologia , Aurora Quinase A/metabolismo , Aurora Quinase B/metabolismo , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Histonas/metabolismo , Humanos , Mitose/efeitos dos fármacos , Piperazinas/farmacologia , Proteínas Recombinantes/metabolismo
2.
Trop Med Infect Dis ; 7(6)2022 Jun 13.
Artigo em Inglês | MEDLINE | ID: mdl-35736980

RESUMO

The purpose of this study was to determine the medication adherence of outpatients with chronic diseases and the association between both patient attitudes and preventive practices regarding COVID-19 and their medication adherence. We performed a cross-sectional study in Vietnam. Medication adherence was determined using the translated and validated Vietnamese version of the General Medication Adherence Scale (GMAS). Patient attitudes and preventive practices regarding COVID-19 were measured using the 5K message of the Vietnam Ministry of Health (facemasks, disinfection, distance, no gatherings, health declarations). The associations between patient characteristics and medication adherence were determined by multivariable regression. The study included 1852 outpatients, and 57.6% of the patients adhered to their medications. Patients who recognized the pandemic's obstruction of medical follow-ups (OR = 1.771; 95%CI = 1.461−2.147; p < 0.001), who applied ≥2 preventive methods (OR = 1.422; 95%CI = 1.173−1.725; p = 0.001), who were employed (OR = 1.677; 95%CI = 1.251−2.248; p = 0.001), who were living in urban areas (OR = 1.336; 95%CI = 1.090−1.637; p = 0.005,) who possessed higher education levels (OR = 1.313; 95%CI = 1.059−1.629; p = 0.013), or who had ≤2 comorbidities (OR = 1.293; 95%CI = 1.044−1.600; p = 0.019) were more likely to adhere to their medications. The adherence percentage for outpatients with chronic diseases was quite low during the pandemic. Patients who did not recognize the COVID-19 pandemic's obstruction of medical follow-ups or who had poor preventive practices were less likely to adhere to medications. Healthcare providers should pay more attention to these groups to achieve desired treatment outcomes.

3.
Healthcare (Basel) ; 10(9)2022 Sep 09.
Artigo em Inglês | MEDLINE | ID: mdl-36141346

RESUMO

(1) Background: COVID-19 has significantly affected the quality of life and the medication adherence of patients with chronic diseases. Attitudes towards the disease and preventive measures are the things that need to be considered for patient adherence to medication during the COVID-19 pandemic. We aimed to evaluate the rate and compare the medication adherence and the impact of the COVID-19 pandemic on medication adherence in Vietnamese patients with cardiovascular and endocrine−metabolic diseases. (2) Methods: A cross-sectional study was conducted on outpatients having chronic diseases such as cardiovascular or/and endocrine−metabolic diseases in some southern provinces in Vietnam. In each group of patients, medication adherence was measured and assessed with the General Medication Adherence Scale (GMAS), adjusted and validated in Vietnam. In addition, the study also investigated attitudes and practices to prevent COVID-19. (3) Results: Out of 1444 patients in our study, the level of adherence was recorded in 867 cases, accounting for 61.1%. The group of patients with only cardiovascular disease and patients with only endocrine−metabolic disease had relatively similar compliance rates of 62 and 61.1%, respectively. The leading cause of non-adherence to treatment in all three groups of patients in the study, as assessed by the GMAS, was non-adherence due to financial constraints. Our study showed that 71.6% of patients felt anxious when going to the hospital for a medical examination. However, only 53.7% identified the COVID-19 pandemic as obstructing treatment follow-up visits. The research results showed that the COVID-19 epidemic influences the patient's psychology with regard to re-examination and treatment adherence, with p coefficients of 0.003 and <0.001, respectively. (4) Conclusion: Medication adherence rates in two disease groups are close, and financial constraint is the fundamental reason for medication non-adherence. Regulatory agencies must take care of people's welfare to improve adherence in the epidemic context.

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