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1.
Biophys Chem ; 285: 106808, 2022 06.
Artigo em Inglês | MEDLINE | ID: mdl-35358908

RESUMO

The mechanisms of interaction of DNA with pharmacological molecules are critical to understanding their therapeutic actions on physiological systems. Piperlongumine is widely studied for its anticancer potential. Multi-spectrometry, calorimetry and in silico studies were employed to study the interaction of piperlongumine and calf thymus DNA. UV-Vis spectroscopy illustrated a hyperchromic pattern in spectra of the calf thymus DNA-piperlongumine complex, while fluorescent quenching was observed in emission spectral studies. Competitive displacement assay demonstrated higher displacement and binding constant for DNA-rhodamine B complex by piperlongumine than DNA-methylene blue complex. Differential scanning calorimetry presented non-significant changes in melting temperature and molecular docking presented the precise interaction site of piperlongumine with calf thymus DNA at minor groove. Further, piperlongumine treatment did not result in pBluescript KS plasmid DNA cleavage as revealed from the DNA topology assay. All these experiments confirmed the binding of piperlongumine with DNA through minor groove binding mode.


Assuntos
DNA de Forma B , Dicroísmo Circular , DNA/química , Dioxolanos , Simulação de Acoplamento Molecular , Conformação de Ácido Nucleico , Espectrometria de Fluorescência , Espectrofotometria Ultravioleta , Termodinâmica
2.
Turk J Biol ; 44(1): 48-60, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32123495

RESUMO

Renal ischemia-reperfusion (I/R) injury, one of the drastic outcomes of renal failure and organ transplantation, tends to deteriorate over time; therefore, noninvasive therapeutic strategies will avail the progression-free survival of the patients. Magnetic field has been proposed as a noninvasive treatment strategy; however, with recent scientific advances, many controversies have arisen regarding its efficacy. Pterostilbene, a natural analog of resveratrol, was documented to be effective in treatment of I/R injuries. This study aims to assess the acute therapeutic effects of combined extremely low-frequency magnetic field (ELF-MF) and pterostilbene treatment on renal I/R injury. After induction of renal I/R in Wistar rats, treatments of 50 Hz, 1 mT ELF-MF applied alone or in combination with pterostilbene were applied for 5 consecutive days. Kidney homogenates were analyzed by Fourier transform infrared spectroscopy. I/R injury resulted in an altered protein and lipid structure with the dominance of longer acyl chains; a slight decrease in lipid, protein, unsaturated lipid, and unsaturated/saturated lipid content; and an increase in membrane fluidity and lipid peroxidation in rat kidneys. Although ELF-MF treatment alone was not sufficient to restore all ischemia-induced alterations, the combined treatment strategy of pterostilbene administration in the presence of ELF-MF was successful and warrants further investigation.

3.
Ayu ; 41(2): 130-135, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-34908798

RESUMO

BACKGROUND: Cardiovascular diseases are the leading causes of deaths despite several advancements in the current medical interventions. Among them, myocardial infarction (MI) is the most alarming disease as about 17.1 million peoples die every year due to MI. AIM: The present study was designed to investigate the potential cardioprotective effect of combination of standardized extracts of Tinospora cordifolia (SETC) (250 mg/kg and 500 mg/kg) and Ocimum sanctum (SEOS) (50 mg/kg) in isoproterenol (ISO)-induced MI. MATERIALS AND METHODS: MI was induced in rats by subcutaneous injection of ISO for 2 consecutive days at an interval of 24 h. Rats were pretreated with test drugs for the period of 21 days, and ISO was administered on the 20th and 21st days. At the end of experiment, i.e., on 22nd-day electrocardiograph, a hemodynamic, biochemical, and histopathological study of heart tissues was evaluated from control and experimental groups and statistically analyzed by one-way analysis of variance followed by Tukey's test. RESULTS: ISO-administered rats showed significant changes in electrocardiograph, mean arterial blood pressure, heart rate, biochemical markers, antioxidant parameters, and histopathology of heart. The activities of cardiac biomarkers were reduced in serum, and there was an increase in antioxidants in heart tissue of test drug-treated animals. Similarly, electrocardiograph, mean arterial blood pressure, and heart rate were restored to normalcy in all test and standard drug-treated animals. CONCLUSION: The SETC 500 mg/kg in combination with SEOS 50 mg/kg was found to be effective in prevention of myocardial injury induced by ISO.

4.
Nat Prod Res ; 32(17): 2116-2120, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28820275

RESUMO

This study is aimed to isolate the phytoactives from the stem bark of Artocarpus hirsutus and evaluate their in vitro anti-acne activity. The ethanolic stem bark extract of A. hirsutus provided two major phytoactive constituents: (i) pyranocycloartobiloxanthone A, (1) and (ii) Artonine E, (2) whose structures were determined by NMR and MS spectroscopic analysis. The present study is the first to report compound 1 as a mixture of two anomers (α and ß), approximately 70:30 ratio. Both compounds 1 and 2 were isolated for the first time from this plant. In vitro anti-acne activity of compounds 1 and 2 were evaluated by agar well diffusion method and the minimum inhibition was determined by broth micro dilution method. The result of anti-microbial activity (MIC = 2.0 µg/mL each) is comparable to antibiotic, Clindamycin (MIC = 0.03 µg/mL) and clearly demonstrate their potential as anti-acne agents.


Assuntos
Acne Vulgar/tratamento farmacológico , Artocarpus/química , Xantonas/química , Antibacterianos/farmacologia , Testes de Sensibilidade Microbiana , Estrutura Molecular , Casca de Planta/química , Extratos Vegetais/química , Propionibacterium acnes/efeitos dos fármacos , Análise Espectral
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