Posted by admin on Nov 30, 2019 in |
In this manuscript, we designed and synthesized 1,4-naphthoquinone derivatives. These derivatives were characterized using the different analytical techniques such as 1H NMR, 13C NMR, FTIR, Mass spectroscopy, melting point, and elemental analysis. The synthesized compounds (MB (1-10)) further subjected to assess the anticancer activity using different cancer cell lines such as MCF-7, HeLa, and HepG2. The compound MB-10 was observed to be the most active against these three cancer cell lines i.e. MCF-7 (IC50 = 16.13± 0.29 µM), HeLa (IC50 = 12.98 ± 0.37 µM) and HepG2 (IC50 = 18.73 ± 0.65 µM). Compound MB10 has also shown potent tyrosine kinase inhibitory activity with IC50 = 1.23 ± 0.12 µM. Moreover, molecular docking investigation revealed that compound MB-10 has strong binding affinity to the amino residue of the active site of enzyme protein tyrosine kinase, which contingent the cytotoxic activities. These outcomes give promising beginning stages to assist in the improvement of cancer as novel and powerful anticancer...
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Posted by admin on Nov 30, 2019 in |
A simple, efficient HPLC method has been developed and validated for simultaneous determination of Amantadine hydrochloride and Oseltamivir phosphate using pre-column derivatization with phenyl isothiocyanate (PITC). The chromatography separation was achieved on Phenomenex C18 column of 250 × 4.6 mm 5 µm particle size, mobile phase used for chromatographic run consisted of acetonitrile and water (60: 40% v/v) with a flow rate of 2 mL/min. The analysis was performed at ambient temperature, and the eluent was monitored at 250 nm using a UV detector. The retention time of Amantadine hydrochloride and Oseltamivir phosphate was found to be 7.1 min and 3.2 min. The limit of detection (LOD) for Amantadine hydrochloride and Oseltamivir phosphate was observed to be 0.1µg/mL and 0.25 µg/mL, respectively. Limit of quantification (LOQ) was found to be 0.5 µg/mL and 0.25 µg/mL. The developed method was validated as per ICH guidelines using parameters like linearity, specificity, precision, linearity, accuracy, ruggedness, robustness, LOD, and LOQ. All the validation parameters were found to be well within the acceptance...
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Posted by admin on Nov 30, 2019 in |
In recent years, there is an increasing interest in finding antioxidant phytochemicals for the prevention and treatment of complex diseases like diabetes, cancer, and atherosclerosis, which are associated with excessive biological oxidative stress. Plants are rich source of natural antioxidants that inhibit the propagation of free radical reactions and protect the human body from degenerative diseases. For the present study, entire vine (aerial part) of Cyclea peltata was selected based on their extensive use in folk medicine and ayurvedic medicine to cure various ailments. Hexane, chloroform, ethyl acetate, methanol and water extracts of Cyclea peltata were subjected to various in-vitro antioxidant activity studies. In most of the antioxidant parameters, ethyl acetate and methanol extracts showed potent activity and chloroform extract showed minimum antioxidant activity. From these studies, it can be concluded that ethyl acetate and methanol extracts of Cyclea peltata could be used as a source of potent natural antioxidant that can be used in various plant-based drugs or formulations for the treatment of complex diseases caused due to...
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Posted by admin on Nov 30, 2019 in |
In different myeloid leukemia cases resistance to diverse treatment regimen owes to multiple molecular mechanisms of cellular network. Epigenetic dysregulation, gene mutations, overexpression of multidrug resistance genes, abnormal immune function, the presence of chemotherapy-resistant leukemia-initiating cells, and aberrant signaling pathways could be the lead cause of this kind of aberration. Some marketed drug is considered as a first-generation drug that can inhibit the enzymatic action by inhibiting the ATP binding with different key pathway regulator protein. Later on, insensitivity of myeloid leukemia cells towards these drugs has been observed may be due to mutation in tyrosine kinase domain of the kinase receptor. By enchanting into account of bioavailability and resistance developed, there is an extreme need to find some natural and nature-derived inhibitors for the kinase proteins of different key metabolic pathways. For computational screening and in-vitro studies against cancer cell lines and marker proteins, Mangiferin and Euxanthic acid isolated from leaves of Mangifera indiaca had been used as mentioned in Ayurveda / Indian Traditional Medicine (ITM). Docking analysis...
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Posted by admin on Nov 30, 2019 in |
Objective: Wedelolactone is a naturally (WDL) occurring coumestan of phytoestrogen category that possess anticancer and anti-inflammatory property. In this study, the anti-inflammatory effect of WDL on human cervical cancer cells (HeLa) and initiation of apoptosis mechanism were investigated. Methods: MTT assay and Trypan blue assay were demonstrated to detect the inhibitory effects of WDL on cell proliferation. The mRNA expression of IL-1β, TNFα, IL-6, TGFβ, and NFκB were detected by RT PCR. Western blotting was performed to detect the expression of apoptosis-associated proteins; cleaved caspase-3, cleaved PARP, Bcl-2, and Bax. Results: WDL significantly inhibited the growth and proliferation of HeLa cells in a concentration dependent manner with the IC50 of 10µM. mRNA expression of inflammatory cytokines and NFκB was significantly reduced in WDL treated groups. Moreover, WDL promoted the apoptosis of HeLa cells dose-dependently by down-regulating Bcl-2 and up-regulating cleaved caspase-3, cleaved PARP, and Bax. Conclusion: Collectively, WDL exerted anti-inflammatory effect through the suppression of NF-kB activation, IL-1β, TNFα, IL-6 and promoted apoptosis in HeLa cells. Thus, use of...
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