Abstract:Noscapine (NOS) is efficient in inhibiting
cellular proliferation
and induces apoptosis in nonsmall cell, lung, breast, lymphatic, and
prostate cancers. The micelle-assisted drug delivery is a well-known
phenomenon; however, the proper mechanism is still unclear. Therefore,
in the present study, we have shown a mechanistic approach for the
delivery of NOS from sodium dodecyl sulfate (SDS) micelles to calf
thymus deoxyribose nucleic acid (ctDNA) base-pairs using various spectroscopic
techniques. The absorption … Show more
“…Subsequently, the steady state anisotropy (r 0 ) measurement was applied to give insight into the micellar microenvironment (i.e., rigidity) around the fluorophore RhB. 26,27 The r 0 values of RhB in LL, ML, and HL micelles are 0.04, 0.11, and 0.12, respectively (Figure 4b), among which HL micelles possess the highest micellar rigidity and the most restricted microenviron- ment owing to the high drug loading boosted drug−polymer interaction, which corroborates well with the AFM results. Moreover, Fourier transform-infrared spectroscopy (FT-IR) was applied to elucidate the drug−polymer interaction and molecular self-assembly of IMC@F127 micelles (Figure 4c).…”
The rigidity of polymeric micelles plays an important role in their biological behaviors. However, how drug loading affects the rigidity of polymeric micelles remains elusive. Herein, the indomethacin (IMC)-loaded Pluronic F127 micelle is used as a model system to illustrate the impact of drug loading on the rigidity and biological behaviors of polymeric micelles. Against expectations, micelles with moderate drug loading show higher cellular uptake and more severe cytotoxicity as compared to both high and low drug loading counterparts. Extensive oneand two-dimensional nuclear magnetic resonance (NMR) measurements are employed to reveal that the higher drug loading induces stronger interaction between IMC and hydrophilic block to boost the micellar rigidity; consequently, the moderate drug loading imparts micelles with appropriate rigidity for satisfactory cellular uptake and cytotoxicity. In summary, NMR spectroscopy is an important tool to gain insight into drug loading regulated micellar rigidity, which is helpful to understand their biological behaviors.
“…Subsequently, the steady state anisotropy (r 0 ) measurement was applied to give insight into the micellar microenvironment (i.e., rigidity) around the fluorophore RhB. 26,27 The r 0 values of RhB in LL, ML, and HL micelles are 0.04, 0.11, and 0.12, respectively (Figure 4b), among which HL micelles possess the highest micellar rigidity and the most restricted microenviron- ment owing to the high drug loading boosted drug−polymer interaction, which corroborates well with the AFM results. Moreover, Fourier transform-infrared spectroscopy (FT-IR) was applied to elucidate the drug−polymer interaction and molecular self-assembly of IMC@F127 micelles (Figure 4c).…”
The rigidity of polymeric micelles plays an important role in their biological behaviors. However, how drug loading affects the rigidity of polymeric micelles remains elusive. Herein, the indomethacin (IMC)-loaded Pluronic F127 micelle is used as a model system to illustrate the impact of drug loading on the rigidity and biological behaviors of polymeric micelles. Against expectations, micelles with moderate drug loading show higher cellular uptake and more severe cytotoxicity as compared to both high and low drug loading counterparts. Extensive oneand two-dimensional nuclear magnetic resonance (NMR) measurements are employed to reveal that the higher drug loading induces stronger interaction between IMC and hydrophilic block to boost the micellar rigidity; consequently, the moderate drug loading imparts micelles with appropriate rigidity for satisfactory cellular uptake and cytotoxicity. In summary, NMR spectroscopy is an important tool to gain insight into drug loading regulated micellar rigidity, which is helpful to understand their biological behaviors.
“…6 It also causes cell cycle arrest in either the S or G 2 /M phase depending on both p53 status and drug concentration. 38 Thus, conjugates 1−4 and 21.9% (1), 14.6% (2), 13.9% (3), 29.8% (4), 35.6% (SLS@1), 13.1% (SLS@2), 23.1% (SLS@3), and 43.9% (SLS@4). The cell populations in the S phase are 3.1% (control group), 9.6% (1), 12.4% (2), 20.2% (3), 12.0% (4), 11.6% (SLS@1), 16.0% (SLS@2), 15.0% (SLS@3), and 15.1% (SLS@4).…”
Section: In Vitro Genotoxicity Studymentioning
confidence: 99%
“…The relative number of cells within each cell cycle was determined by flow cytometry. The cell populations in the sub-G 1 phase are 5.7% (control group),21.9% (1), 14.6% (2), 13.9% (3), 29.8% (4), 35.6% (SLS@1), 13.1% (SLS@2), 23.1% (SLS@3), and 43.9% (SLS@4). The cell populations in the S phase are 3.1% (control group), 9.6% (1), 12.4% (2), 20.2% (3), 12.0% (4), 11.6% (SLS@1), 16.0% (SLS@2), 15.0% (SLS@3), and 15.1% (SLS@4).…”
{[Ag8(Mef)8(μ2-S,O-DMSO)2(μ2-O-DMSO)2(O-DMSO)8]·2(H2O)} (1), [Ag(Mef)(tpP)2] (2),
[Ag(Mef)(tpAs)3] (3), and {2 [Ag(Mef)(tpSb)3] (DMSO)} (4) were obtained by the conjugation
of mefenamic acid (MefH), a nonsteroidal anti-inflammatory drug (NSAID),
with a mitochondriotropic derivative of pnictogen tpE (tp = triphenyl
group; E = P, As, and Sb) through silver(I). Their hydrophilicity
was adjusted by their dispersion into sodium lauryl sulfate (SLS),
forming SLS@1–4. 1–4 and SLS@1–4 were characterized
by their spectral data and X-ray crystallography. They inhibit the
proliferation of human breast adenocarcinoma cells MCF-7 (hormone-dependent
(HD)) and MDA-MB-231 (hormone-independent (HI)). X-ray fluorescence
reveals the Ag cellular uptake. The in vitro and in vivo nongenotoxicity was confirmed with micronucleus
(MN), Artemia salina, and Allium cepa assays. Their mechanism of action was studied by cell morphology,
DNA fragmentation, acridine orange/ethidium bromide (AO/EB) staining,
cell cycle arrest, mitochondrial membrane permeabilization tests,
DNA binding affinity, and LOX inhibitory activity and was rationalized
by regression analysis.
“…Heterocyclic compounds are versatile biological applications like anti-microbial, anti-diabetic, anti-malarial etc. Noscapine is a isoquinoline based molecules and reported as cough suppressant, anti-malarial and anti-cancerous (Kumar et al, 2020dMaurya, Alzahrani, et al, 2019;. Previously, the group has reported the noscapines as potential inhibitors of main protease of SARS-CoV-2 using molecular docking and molecular dynamics simulations.…”
First case of the present epidemic, coronavirus disease (COVID-19) is reported in the Wuhan, a city of the China and all the countries throughout the world are being affected. COVID-19 is named by World Health Organization and it stands for coronavirus disease-19. As on 27 th October, 2020, 73,776,588 people around the world are infected. It is also known as SARS-CoV-2 infection. Till date, there is no promising drug or vaccine available in market to cure from this lethal infection. As the literature reported that noscapine a promising candidate to cure from malaria as well reported to be cough suppressant and anti-cancerous. In our previous work, a derivative of noscapine has shown potential behavior against the main protease of novel coronavirus or SARS-CoV-2. Based on the previous study, hybrid molecules based on noscapine and repurposing (antiviral) drugs were designed to target the main protease of novel coronavirus and falcipan-2 using molecular docking. It is proposed that the designed hydrids or conjugates may have promising antiviral property i.e. against the main protease of novel coronavirus and falcipan-2. The designed molecules were thoroughly studied by DFT and different thermodynamic parameters were determined. Further, infrared and Raman spectra of the designed hybrid molecules were determined and studied.
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