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1.
J Cancer Res Ther ; 17(6): 1583-1586, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34916403

RESUMO

BACKGROUND: The role of ascorbic acid in cancer therapy is mainly due to its structural similarity with glucose. When supplemented intravenously in high dose, ascorbic acid can get into the cancer cells and induce apoptosis by causing mitochondrial damage. AIM: The aim was to study the efficacy of high-dose intravenous (IV) ascorbic acid as monotherapy in cancer patients following ketogenic diet and its role in improving the quality of life. RESULTS: C-reactive protein (CRP) and erythrocyte sedimentation rates (ESRs) were considered as parameters to determine the efficacy of the treatment, and substantial decrease in both the levels was observed within 1-week treatment. CRP levels declined from 3.1946 ± 3.2508 mg/L to 1.0606 ± 0.6706 mg/L (P = 2.27E-10), whereas ESR levels declined from 64.1333 ± 38.8253 mm/h to 31.6 ± 16.5520 mm/h (P = 0.0041). A decline in these parameters shows the association of ascorbic acid in reducing the inflammatory response in cancer. The renal effect of ascorbic acid was also studied by analyzing the creatinine level pre- and postascorbic acid treatment sessions, and it raised from 0.8526 ± 0.22904 to 1.1666 ± 0.2894 mg/dL (P = 1.18E-14). This showed the renal impact of ascorbic acid. CONCLUSION: The study highlighted the clinical benefit of IV ascorbic acid in the reduction of inflammatory response in cancer patients. The renal adverse events associated with ascorbic acid alarm the use with caution and therapeutic drug monitoring for ascorbic acid.


Assuntos
Ácido Ascórbico/administração & dosagem , Dieta Cetogênica , Rim/efeitos dos fármacos , Neoplasias/terapia , Adulto , Ácido Ascórbico/efeitos adversos , Creatinina/sangue , Creatinina/metabolismo , Creatinina/urina , Relação Dose-Resposta a Droga , Esquema de Medicação , Feminino , Humanos , Infusões Intravenosas , Rim/metabolismo , Masculino , Pessoa de Meia-Idade , Neoplasias/sangue , Neoplasias/urina , Qualidade de Vida , Eliminação Renal/efeitos dos fármacos , Resultado do Tratamento
2.
Bioorg Chem ; 62: 22-9, 2015 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-26189013

RESUMO

A series of methoxylated chalcones with fluoro and trifluoromethyl derivatives were synthesized and investigated for their ability to inhibit human monoamine oxidase A and B. The chemical structures of the compounds have been characterized by means of their (1)H NMR, (13)C NMR, Mass spectroscopic datas and elemental analysis. The results demonstrate that these compounds are reversible and selective MAO-B inhibitors with a competitive mode of inhibition. The most potent compound (2E)-1-(4-methoxyphenyl)-3-[4-(trifluoromethyl)phenyl] prop-2-en-1-one showed the best activity and higher selectivity towards hMAO-B with Ki and SI values of 0.22±0.01µM and 0.05 comparable to that standard drug, Selegiline Ki and SI values were found as 0.33±0.03µM and 0.04, respectively. Molecular docking studies were carried out to further explain the in vitro results of the new compounds, and to identify the hypothetical binding mode for the compounds inside the inhibitor binding cavity of hMAO-B.


Assuntos
Chalconas/síntese química , Chalconas/farmacologia , Hidrocarbonetos Fluorados/síntese química , Hidrocarbonetos Fluorados/farmacologia , Simulação de Acoplamento Molecular , Inibidores da Monoaminoxidase/síntese química , Inibidores da Monoaminoxidase/farmacologia , Monoaminoxidase/efeitos dos fármacos , Propano/análogos & derivados , Humanos , Propano/síntese química , Propano/farmacologia
3.
J Res Pharm Pract ; 3(1): 34-6, 2014 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-24991634

RESUMO

OBJECTIVE: Hyponatremia is one of the most common electrolyte abnormalities in hospitalized patients. The treatment of hyponatremia is controversial as rapid correction of serum sodium can give rise to neurologic disorder and at the same time if not corrected timely, it can lead to brain damage. The aim of this study was to compare the efficacy of Tolvaptan with 3% hypertonic saline solution for the management of hyponatremia in hospitalized patients. METHODS: In this prospective observational study, data of 60 hospitalized patients having hyponatremia from February 2013 to July 2013 were collected and analyzed. Patients either received oral Tolvaptan or intravenous infusion of 3% hypertonic saline solution. The serum sodium concentration before administration of treatment and 24 h and 48 h after the administration of the drugs were recorded and analyzed. Data were analyzed using GraphPad Software, by Student's paired t-test and one-way analysis of Variance (ANOVA). FINDINGS: Tolvaptan and 3% hypertonic saline solution had significant effects in raising serum sodium level in hyponatremic patients at both 24 h and 48 h (P < 0.0001). This increase was about 8.030 ± 0.6507 mEq/L and 12.33 ± 0.6489 mEq/L for 3% hypertonic saline and about 5.111 ± 0.6616 mEq/L and 10.11 ± 0.6230 mEq/L for Tolvaptan, after 24 h and 48 h, respectively. CONCLUSION: Both drugs had significant effects in raising serum sodium level in hyponatremic patients; however administration of 3% hypertonic saline solution had a slightly superior efficacy in raising the serum sodium concentration at both 24 h and 48 h periods in Hyponatremic patients compared with oral Tolvaptan.

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