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Molecular Diversity Jun 2023A detailed computational analysis of acridine derivatives viz. acridone, 9-amino acridine hydrochloride hydrate, proflavin, acridine orange and acridine yellow is done...
A detailed computational analysis of acridine derivatives viz. acridone, 9-amino acridine hydrochloride hydrate, proflavin, acridine orange and acridine yellow is done in terms of conceptual density functional theory (CDFT). CDFT-based global descriptors-ionization potential, electron affinity, HOMO-LUMO gap, hardness, softness, electronegativity and electrophilicity index of acridine derivatives for ground state as well as excited state are estimated with the help of different hybrid functionals B3LYP/6-31G (d, p), B3LYP/6-311G (d, p), B3LYP/DGDZVP and B3LYP/LANL2DZ. Acridine derivatives show higher values of ionization potential and electron affinity in excited state as compared to ground state, indicating that these compounds are willing to accept electrons in excited state rather than donating electron. Acridone shows the maximum HOMO-LUMO energy gap in ground and excited state which implies that one-way electron transfer is most feasible with this compound. Our computed results emphasize the pronounced electron acceptor behaviour of the acridine derivatives in the excited state which has already been experimentally verified. It is observed that the trend in the computed values of the descriptors is not much improved on refinement of the basis set.
Topics: Density Functional Theory; Acridines
PubMed: 35781180
DOI: 10.1007/s11030-022-10486-6 -
Bone & Joint Research Oct 2022Acridine orange (AO) demonstrates several biological activities. When exposed to low doses of X-ray radiation, AO increases the production of reactive radicals...
AIMS
Acridine orange (AO) demonstrates several biological activities. When exposed to low doses of X-ray radiation, AO increases the production of reactive radicals (radiodynamic therapy (AO-RDT)). We elucidated the efficacy of AO-RDT in breast and prostate cancer cell lines, which are likely to develop bone metastases.
METHODS
We used the mouse osteosarcoma cell line LM8, the human breast cancer cell line MDA-MB-231, and the human prostate cancer cell line PC-3. Cultured cells were exposed to AO and radiation at various concentrations followed by various doses of irradiation. The cell viability was then measured. In vivo, each cell was inoculated subcutaneously into the backs of mice. In the AO-RDT group, AO (1.0 μg) was locally administered subcutaneously around the tumour followed by 5 Gy of irradiation. In the radiation group, 5 Gy of irradiation alone was administered after macroscopic tumour formation. The mice were killed on the 14th day after treatment. The change in tumour volume by AO-RDT was primarily evaluated.
RESULTS
The viability of LM8, MDA-MB-231, and PC-3 cells strongly decreased at AO concentration of 1.0 μg/ml and a radiation dose of 5 Gy. In xenograft mouse model, the AO-RDT also showed a strong cytocidal effect on tumour at the backside in osteosarcoma, breast cancer, and prostate cancer. AO-RDT treatment was more effective for tumour control than radiotherapy in breast cancer.
CONCLUSION
AO-RDT was effective in preventing the proliferation of osteosarcoma, breast cancer, and prostate cancer cell lines in vitro. The reduction in tumour volume by AO-RDT was also confirmed in vivo.Cite this article: 2022;11(10):685-692.
PubMed: 36214462
DOI: 10.1302/2046-3758.1110.BJR-2022-0105.R2 -
Organic & Biomolecular Chemistry Mar 2019DNA aptamers represent a way to target cancer cells at a molecular level and continue to be developed with a view to improve treatment and imaging in cancer medicine....
DNA aptamers represent a way to target cancer cells at a molecular level and continue to be developed with a view to improve treatment and imaging in cancer medicine. AT11-L0, derived from the DNA sequence AT11, forms a single major parallel G-quadruplex (G4) conformation and exhibits an anti-proliferative activity similar to that of AT11 and AS1411 aptamers. On the other side, acridine orange derivatives represent a valuable class of G4 ligands. Herein, we evaluate AT11-L0 G4 as a supramolecular carrier for the delivery of acridine ligands C3, C5 and C8 to HeLa cancer cells. The CD titrations suggest no changes in the chiroptical signal upon addition of an excess of ligands maintaining the parallel G4 topology and C8 stabilizes the structure for more than 20 °C. All the ligands exhibit high affinity (micromolar range) towards AT11-L0 G4, and the respective complexes against nucleolin (nanomolar range) suggesting that the ligands do not negatively affect the recognition of the nucleolin by AT11-L0 G4. NMR studies showed that AT11-L0 forms a G4 containing four G-tetrad layers. Ligand C8 binds AT11-L0 G4 through π-π stacking of the acridine moiety onto the top-tetrad with the involvement of additional interactions with the ligand's side chain and iodobenzene ring. In vitro, the complexes lowered the ligand's cytotoxicity towards non-malignant cells but have a weak inhibitory effect in HeLa cancer cells, except for the AT11-L0-C5 complex. All complexes are efficiently internalized into nucleolin-positive HeLa cells. Overall, these results suggest that AT11-L0 can act as an aptamer by targeting nucleolin and a delivery system of cytotoxic ligands for cervical cancer.
Topics: Acridines; Antineoplastic Agents; Aptamers, Nucleotide; Cell Proliferation; Cell Survival; Dose-Response Relationship, Drug; Drug Carriers; Drug Screening Assays, Antitumor; Female; HeLa Cells; Humans; Ligands; Molecular Structure; Structure-Activity Relationship; Uterine Cervical Neoplasms
PubMed: 30810582
DOI: 10.1039/c9ob00318e -
Environmental Research Oct 2022The adsorption of acridine orange and Cr ion onto plaster of paris reinforced glutamic acid-grafted-polyacrylamide hydrogel nanocomposite modified with riboflavin,...
Statistical evaluation of liquid phase sequestration of acridine orange and Cr by novel mesoporous glutamic acid-g-polyacrylamide/plaster of paris/riboflavin hydrogel nanocomposite.
The adsorption of acridine orange and Cr ion onto plaster of paris reinforced glutamic acid-grafted-polyacrylamide hydrogel nanocomposite modified with riboflavin, Glu-g-PAM/POP/Rb HNC was studied. The Glu-g-PAM/POP/Rb HNC was physico-chemically characterized by Fourier transform infrared spectroscopy, X-ray diffraction analysis, scanning electron microscopy coupled with energy dispersive X-ray spectroscopy, transmission electron microscopy and Brunauer-Emmett-Teller analysis. The specific surface area, pore volume and pore diameter were 15.48 m/g, 0.015 cm/g and 4.23 nm, respectively. Adsorption process was strategized by response surface methodology (RSM) based on a 3-level 5-factor (initial solution pH, contact time, adsorbent dose, initial adsorbate concentration and temperature) central composite design (CCD), and validity of the estimated parameters was statistically evaluated using analysis of variance (ANOVA). The optimized operating variables were: pH (AO = 10; Cr = 4.15), contact time (AO = 60 min; Cr = 59 min), adsorbent dose (0.8 g/L), initial adsorbate concentration (60 mg/L) and temperature (298 K). Isotherm results were coincident with Langmuir isotherm model. The experimental kinetic adsorption data was congruous with pseudo-second order model, with the uptake rate controlled by both intraparticle and liquid film diffusions. The relatively high Langmuir saturation capacity of 202.63 mg AO/g and 143.68 mg Cr/g, supported by the decent recyclability up to four times affirmed the promising performance of the adsorbent. The efficacy of the adsorbent for simultaneous removal of AO and Cr from bi-component system was assessed. The possible adsorption mechanism mainly involved hydrogen bonding, van der Waals forces, electrostatic and π-π interactions. Adsorption of AO and Cr onto Glu-g-PAM/POP/Rb HNC was feasible and exothermic as revealed by the thermodynamic parameters. The findings demonstrated superior adsorbent efficacy for the seizure of pollutants, particularly AO and Cr from aqueous solution.
Topics: Acridine Orange; Acrylic Resins; Adsorption; Calcium Sulfate; Glutamic Acid; Hydrogels; Hydrogen-Ion Concentration; Kinetics; Nanocomposites; Riboflavin; Spectroscopy, Fourier Transform Infrared; Thermodynamics; Water Pollutants, Chemical
PubMed: 35718168
DOI: 10.1016/j.envres.2022.113712 -
Journal of Oral and Maxillofacial... 2023Sex determination in forensic medicine is considered one of the first and foremost steps in personal identification. The need for identifying the exact sex of the...
UNLABELLED
Sex determination in forensic medicine is considered one of the first and foremost steps in personal identification. The need for identifying the exact sex of the individual arises when deciding whether a person can exercise certain civil rights reserved for one particular sex, for competing in sex-specific athletic and sports events, legitimacy, divorce, paternity disputes and also to some criminal offenses. Nuclear sexing by Barr body examination can be done using buccal smears to establish the sex of the individual when routine methods fail to disclose the exact gender of the individual.
AIM
To determine and compare the Barr bodies present in exfoliated buccal epithelial cells in males, females and transgender populations using light and fluorescence microscopy.
MATERIALS AND METHODS
A total of 90 patients were recruited for the study. Group I consisted of 30 female patients. Group II consisted of 30 male patients and group III consisted of 30 transgender patients. The buccal mucosa was then scraped using a wooden spatula and the cells obtained were fixed in 95% ethanol. Two smears per individual were made and stained. One smear was stained with papanicolaou (PAP) stain and the other with Acridine orange and viewed under light microscopy and fluorescent microscopy, respectively.
RESULTS
When PAP stained slides were examined, the percentage of Barr-bodies in females ranged from 3% to 5% and in males it was 0% and in transgenders, it ranged from 0% to 5%. In Acridine orange stained smears, the percentage of Barr bodies in females ranged from 1% to 3% and in males it was 0% and in transgenders, it was 0%. Kruskal-Wallis test to study the relation of Barr body percentage in females, males and transgender subjects demonstrated significant differences between the groups ( < 0.001). Wilcoxon signed rank test was done for pairwise comparison, which showed that the distribution of percentage of positive cells in females are statistically significant from males and transgenders ( < 0. 001).
CONCLUSION
Nuclear sexing using Barr bodies offers a simple yet effective method for determining the sex of transgender patients which could help them in understanding their gender identity better and diagnose any underlying chromosomal aberration.
PubMed: 38304528
DOI: 10.4103/jomfp.jomfp_342_23 -
Anatomical Record (Hoboken, N.J. : 2007) Jul 2020The current study investigated the macroscopic and microscopic differences between pennaceous and plumulaceous feathers. The morphology of the barbules distinguished...
The current study investigated the macroscopic and microscopic differences between pennaceous and plumulaceous feathers. The morphology of the barbules distinguished pennaceous and plumulaceous feathers, particularly the shape of barbules during their development. In pennaceous feathers, the initial barbules were large and elongated or pyriform in shape, while plumulaceous feathers had small, thin, elongated initial barbules. The spinous barbules were characteristic of pennaceous feathers. The histochemical reactivity of both feather types for Mallory trichrome, orange G, and acridine orange, safranin O, PAS, and methylene blue was determined. Keratin was detected by Mallory trichrome, orange G, and acridine orange. In conclusion, the histochemical properties of pennaceous and plumulaceous feathers of quail, particularly the distribution and nature of keratin during development, should be considered in future studies. The unique morphological features of pennaceous and plumulaceous feathers could be used as a guide for phylogenetic identification. Anat Rec, 2019. © 2019 American Association for Anatomy Anat Rec, 303:1865-1883, 2020. © 2019 American Association for Anatomy.
Topics: Animals; Feathers; Phylogeny; Quail
PubMed: 31581344
DOI: 10.1002/ar.24276 -
Antibiotics (Basel, Switzerland) Jul 2023The development and implementation of diagnostic methods that allow rapid assessment of antibiotic activity against pathogenic microorganisms is an important step...
The development and implementation of diagnostic methods that allow rapid assessment of antibiotic activity against pathogenic microorganisms is an important step towards antibiotic therapy optimization and increase in the likelihood of successful treatment outcome. To determine whether fluorescence microscopy with acridine orange can be used for rapid assessment (≤8 h) of the meropenem activity against , six isolates including three OXA-48-carbapenemase-producers were exposed to meropenem at different levels of its concentration (0.5 × MIC, 1 × MIC, 8 or 16 µg/mL) and the changes in the viable counts within 24 h were evaluated using fluorescence microscopy and a control culture method. The approach was to capture the regrowth of bacteria as early as possible. Within the first 8 h fluorescence microscopy allowed to categorize 5 out of 6 strains by their meropenem susceptibility (based on the MIC breakpoint of 8 mg/L), but meropenem activity against three isolates, two of which were OXA-48-producers, could not be accurately determined at 8 h. The method proposed in our study requires improvement in terms of accelerating the bacterial growth and regrowth for early meropenem MIC determination. Volume-dependent elevation in meropenem MICs against OXA-48-producers was found and this phenomenon should be studied further.
PubMed: 37508266
DOI: 10.3390/antibiotics12071170 -
Pharmaceuticals (Basel, Switzerland) Jan 2022Two-dimensional nanosilicate particles (NS) have shown promise for the prolonged release of small-molecule therapeutics while minimizing burst release. When incorporated...
Two-dimensional nanosilicate particles (NS) have shown promise for the prolonged release of small-molecule therapeutics while minimizing burst release. When incorporated in a hydrogel, the high surface area and charge of NS enable electrostatic adsorption and/or intercalation of therapeutics, providing a lever to localize and control release. However, little is known about the physio-chemical interplay between the hydrogel, NS, and encapsulated small molecules. Here, we fabricated polyethylene glycol (PEG)-NS hydrogels for the release of model small molecules such as acridine orange (AO). We then elucidated the effect of NS concentration, NS/AO incubation time, and the ability of NS to freely associate with AO on hydrogel properties and AO release profiles. Overall, NS incorporation increased the hydrogel stiffness and decreased swelling and mesh size. When individual NS particles were embedded within the hydrogel, a 70-fold decrease in AO release was observed compared to PEG-only hydrogels, due to adsorption of AO onto NS surfaces. When NS was pre-incubated and complexed with AO prior to hydrogel encapsulation, a >9000-fold decrease in AO release was observed due to intercalation of AO between NS layers. Similar results were observed for other small molecules. Our results show the potential for use of these nanocomposite hydrogels for the tunable, long-term release of small molecules.
PubMed: 35056113
DOI: 10.3390/ph15010056 -
Journal of Oral and Maxillofacial... 2020is a yeast-like fungus, and it causes candidiasis. Since it is commonly encountered in many cases, the need of the hour is for rapid and reliable method for...
Comparative evaluation of staining efficacy of calcofluor white and acridine orange for detection of species using fluorescence microscopy - A prospective microbiological study.
CONTEXT
is a yeast-like fungus, and it causes candidiasis. Since it is commonly encountered in many cases, the need of the hour is for rapid and reliable method for identification of these fungi in tissue sections.
AIM
The aim of this study was to evaluate and compare the staining efficacy of calcofluor white (CFW) and acridine orange (AO) for the detection of species in formalin-fixed paraffin-embedded tissue samples of oral squamous cell carcinoma (OSCC) using fluorescence microscopy.
SETTINGS AND DESIGN
Sample size comprised forty cases of OSCC.
MATERIALS AND METHODS
Before tissue sampling, a swab of the area was taken, it was immediately inoculated on Sabouraud's dextrose agar media and germ tube test was performed for positive cultures for species identification. Tissue sections were obtained from cases of OSCC from the formalin-fixed paraffin-embedded tissue blocks of the same cases in which microbiological assessment was done at the time of tissue sampling, were stained with CFW and AO stain, respectively, and were examined using a fluorescent microscope.
STATISTICAL ANALYSIS
Descriptive statistics were expressed in numbers and percentage. Independent -test (unpaired -test) and Chi-square test were used. ≤0.05 was taken to be statistically significant.
RESULTS
The mean number of microorganisms per high-power field stained by CFW and AO was 6.35 and 2.57, respectively, and a statistically significant difference ( ≤ 0.001) was observed. CFW compared to swab culture gave = 0.018, which showed a statistically significant association.
CONCLUSIONS
CFW is a better fluorescent stain when compared to AO to detect species in tissue sections of OSCC cases.
PubMed: 32508453
DOI: 10.4103/jomfp.JOMFP_315_18 -
Journal of Enzyme Inhibition and... Dec 2017Photodynamic molecules represent an alternative approach for cancer therapy for their property (i) to be photo-reactive; (ii) to be not-toxic for target cells in absence... (Review)
Review
Photodynamic molecules represent an alternative approach for cancer therapy for their property (i) to be photo-reactive; (ii) to be not-toxic for target cells in absence of light; (iii) to accumulate specifically into tumour tissues; (iv) to be activable by a light beam only at the tumour site and (v) to exert cytotoxic activity against tumour cells. However, to date their clinical use is limited by the side effects elicited by systemic administration. Extracellular vesicles are endogenous nanosized-carriers that have been recently introduced as a natural delivery system for therapeutic molecules. We have recently shown the ability of human exosomes to deliver photodynamic molecules. Therefore, this review focussed on extracellular vesicles as a novel strategy for the delivery of photodynamic molecules at cancer sites. This completely new approach may enhance the delivery and decrease the toxicity of photodynamic molecules, therefore, represent the future for photodynamic therapy for cancer treatment.
Topics: Biological Products; Drug Delivery Systems; Humans; Nanoparticles; Photochemotherapy; Photosensitizing Agents
PubMed: 28708430
DOI: 10.1080/14756366.2017.1335310