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•~6 nm β-cyclodextrin-conjugated dextran-coated magnetic Ni1.04Fe1.96O4 NPs are prepared.•Enhanced camptothecin loading and sustained release are observed.•Stimuli-responsive ...(pH-dependent) release of the drug from the nanocarrier occurs.•The efficacy of the drug-loaded nanocarrier is intense on cervical, breast, and lung cancer cells.•The material works as a pH-responsive and host: guest complexation-based drug vehicle.
This paper fortifies the idea of smart drug vehicles, by exploring nickel ferrite nanoparticles. The material is made smart by covering with a novel biocompatible dextran fastened with a hydrophobic cavity containing molecule, β-cyclodextrin (β-CD). The approximately 6 nm MNPs, embodied with the β-CD-dextran conjugate, permit a sustained in vitro release of camptothecin. Cytotoxicity studies are done on HaCaT, 3T3, HeLa, MDA-MB-231, and A549 cell lines. It is fascinating the stacked camptothecin indicates upgraded viability against cancer cells, rendering the nanocarrier viable for transporting the anticancer drug.
New cyclometallated ruthenium(ii) complexes of 3-acetyl-7-methoxycoumarin-4
-substituted thiosemicarbazones were synthesized and characterized by analytical and spectral techniques. The crystal ...structures of the ligands H
L
and complexes (1, 2 and 4) were confirmed by X-ray crystallography. The analysis showed that the ligands have undergone C-H activation at the C(4) carbon of the pyrone ring and acted in a tridentate fashion by binding through C, N and S atoms. CT-DNA and protein (BSA/HSA) binding studies were carried out to analyze their interaction with biomolecules. Good binding affinity with DNA was observed with intercalative binding mode, which was further confirmed by EB displacement and viscosity measurement studies. The quenching mechanism with BSA/HSA was found to be static. Three dimensional (3D) fluorescence measurements were carried out to validate the micro environmental changes in the serum albumins. Their antioxidant propensity and antimicrobial study insisted that the compounds displayed good spectrum of activity. Evaluation of their anticancer potential against MCF-7 (human breast cancer) and A549 (human lung carcinoma) cell lines revealed that the complexes exhibited better activity than the ligands and cisplatin. Further, the results of LDH and NO release assays supported the cytotoxic nature of the compounds. The non-toxic nature of the compounds was established by testing against the non-cancerous cell line HaCaT (human normal keratinocyte).
New Schiff base ligands are prepared by the condensation of 7-hydroxy-3-formylchromone with semicarbazone and phenyl semicarbazone. The complexation of these ligands with Cu(II) ion is proposed in ...the light of spectral studies (IR, UV–Vis, 1H NMR, 13C NMR, Mass and ESR). In the complexes 1 and 2, the ligands coordinate to the Cu(II) ion in a neutral fashion via ONO donor atoms. The single crystal XRD studies reveal a slightly distorted square-pyramidal geometry for cationic complex (1) and an octahedral geometry for neutral complex (2). Preliminary biological studies such as DNA and Protein binding are carried out by using absorption and emission titration methods. Observation of intercalative mode of binding with Calf Thymus DNA (CT-DNA) is confirmed by means of viscosity measurements. The micro-environmental changes occurring in Bovine Serum Albumin (BSA) and Human Serum Albumin (HSA) are monitored via three dimensional (3D) fluorescence studies. The compounds ability in inhibiting microbial growth is tested against different pathogens. MCF-7 (human breast cancer) and A549 (human lung carcinoma) cell lines are utilized to check the anticancer potential of the synthesized compounds by using MTT, LDH and NO assays. The results show that complexes 1 and 2 exhibited potent cytotoxic activity over standard drug cisplatin.
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•New water soluble copper(II) complexes have been synthesized and characterized.•The DNA/protein interactions of ligands and complexes were studied by a variety of techniques.•The antimicrobial activity against four different bacteria and five fungi has also been examined.•The antiproliferative activity was evaluated against MCF-7 and HeLa cell lines.•Assay on HaCaT cell lines showed that the compounds were non-toxic to those cells.
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•Four octahedral Co(III) complexes were synthesized and characterized.•Partial intercalation with DNA and static quenching with BSA was established.•MTT assay on A549 and MCF-7 cells ...revealed their anticancer activity•The complexes showed significant microbial activity.•Complex 3 possessed better biological activity than the ligands and other complexes.
The present work deals with the synthesis and characterization of four Co(III) complexes derived from 7-hydroxy-4-oxo-4H-chromene-3-carbaldehyde-4(N)-substituted thiosemicarbazones. Structural confirmation of the complexes 2 and 3 were aided by X-ray crystallographic analysis, which revealed the coordination of azomethine nitrogen, ring carbonyl oxygen and thiol sulfur atoms of the ligands. DNA and Bovine serum albumin (BSA) binding studies brought about the binding ability of the complexes to biomolecules. The binding constant values calculated for the complexes were in the range (0.30–1.19) × 106 M−1 and the mode of interaction was found to be partially intercalative. The mechanism of quenching with BSA was static with quenching constants in the order 1012 M−1s−1. Their antimicrobial profile has been established by testing against four pathogenic bacterial and fungal species. The cytotoxic potential of the complexes were examined against MCF-7 and A549 cells by MTT assay. The IC50 values of the complexes were less than cisplatin, which indicated their greater activity over the standard drug. In addition, testing on human normal keratinocyte cells HaCaT indicated their non toxic nature. Lactate dehydrogenase (LDH) and Nitric oxide (NO) release assays supported the cytotoxic ability and suggested apoptotic mode of cell death induced by the complexes.
Four different mononuclear palladium(II) complexes of 3‐acetyl‐8‐methoxycoumarin Schiff bases were synthesized and characterized by spectrochemical techniques. Further analysis through X‐ray ...crystallography confirmed the structures of the complexes. Their interactive ability with Calf Thymus DNA and protein (Bovine Serum Albumin and Human Serum Albumin) were investigated by means of absorption and emission methods. The intercalative mode of binding with DNA was supported by EB displacement studies and viscosity measurements. Configurational changes that occurred in the proteins have been analysed with the help of 3D fluorescence studies. The complexes were shown to have good antimicrobial activity against the tested bacterial and fungal pathogens. In addition, antiproliferative activity of the complexes was evaluated on A549 and MCF‐7 cell lines and the complexes were comparatively more active than the standard drug cisplatin. Among the compounds, complex 3 was the most effective against MCF‐7 (IC50 value of 5.20 ± 0.15 μM) and A549 (5.09 ± 0.13 μM) compared with the other complexes 1 (6.48 ± 0.17 μM; 5.98 ± 0.09 μM), 2 (5.53 ± 0.12 μM; 5.85 ± 0.11 μM), 4 (6.73 ± 0.19 μM; 6.63 ± 0.16 μM) and cisplatin (16.79 ± 0.08 μM; 15.10 ± 0.05 μM) respectively. LDH and NO release assays confirmed the cytotoxic potential of the synthesized complexes.
The present work describes the synthesis and characterization of Pd(II) complexes derived from 3‐acetyl‐8‐methoxy‐2H‐chromen‐2‐one Schiff bases. Their biological activities were evaluated in terms of DNA/Protein binding, antimicrobial and anticancer abilities.
Four binuclear Ni(II) complexes Ni2(H-DEAsal-tsc)2(μ-dppm)·2Cl (1), Ni2(DEAsal-mtsc)2(μ-dppm) (2), Ni2(DEAsal-etsc)2(μ-dppm) (3) and Ni2(DEAsal-ptsc)2(μ-dppm) (4) were synthesized from the ligands ...namely 4(N,N)-diethylaminosalicylaldehyde-4(N)-thiosemicarbazone H2-DEAsal-tsc H2L1/4(N,N)-diethylaminosalicylaldehyde-4(N)-methyl thiosemicarbazone H2-DEAsal-mtsc H2L2/4(N,N)-diethylaminosalicylaldehyde-4(N)-ethyl thiosemicarbazone H2-DEAsal-etsc H2L3/4(N,N)diethylaminosalicylaldehyde-4(N)-phenyl thiosemicarbazone H2-DEAsal-ptsc H2L4 and 1,1′-bis(diphenylphosphino)methane (dppm) and characterized by a number of spectro analytical techniques. The molecular structure of complexes Ni2(H-DEAsal-tsc)2(μ-dppm)·2Cl (1) and Ni2(DEAsal-ptsc)2(μ-dppm) (4) have been confirmed by single crystal X-ray diffraction studies. The analysis indicated that in complex 1, the ligand H2-DEAsal-tsc coordinated as monobasic tridentate donor through phenolic oxygen, azomethine nitrogen and thione sulfur atoms. However, in complex 4, the ligand H2-DEAsal-ptsc behaved as dibasic tridentate donor with thiolate sulfur coordination. Their ability to bind with Calf Thymus Deoxyribonucleic acid (CT-DNA) and Bovine Serum Albumin (BSA) were analysed spectrometrically. Intercalative interaction of the complexes with DNA was confirmed by ethidium bromide (EB) displacement studies and DNA viscosity measurements. The interaction mechanism of the complexes with BSA was found as static. In vitro antiproliferative studies of the ligands and complexes in A549 (human lung carcinoma cancer), MCF-7 (human breast cancer) and HeLa (human cervical cancer) cell lines witnessed significant cytotoxic nature of the complexes with low IC50 values (in μM) than the standard metallo-drug cisplatin. Further, the results of Lactate Dehydrogenase (LDH) and Nitric oxide (NO) release assays supported the effectiveness of the complexes on the above said cancer cells.
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•Four binuclear Ni(II) Schiff base complexes were synthesized and characterized.•Molecular structures of complexes 1 and 4 were confirmed by crystallographic studies.•Binding with Calf Thymus Deoxyribonucleic acid and Bovine Serum Albumin were analysed.•IC50 values of complexes were less than cisplatin against A549, MCF-7 and HeLa cells.•Lactate dehydrogenase (LDH) and nitric oxide (NO) release assays were carried out.
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•The DNA and protein interactions of these complexes were studied by a variety of techniques.•The antimicrobial activity against four different bacteria and five fungus have also been ...examined.•The antiproliferative activity was evaluated against a human breast cancer cell line (MCF-7) and human lung cancer cell line (HeLa). The ligands and complexes 1–4 exhibited potent anticancer activity over the standard drug, Cisplatin.•Assay on human normal keratinocyte cell line HaCaT showed that the compounds were non-toxic to those cells.
Four new water soluble chromone appended copper(II) complexes of the type Cu(L)Cl were synthesized from CuCl2·2H2O and 3-formylchromone-4N-substituted thiosemicarbazones (HL1–HL4). Characterization of the compounds was done by using analytical and spectral techniques such as elemental analyses, IR, UV–Visible, EPR and Mass spectrometry, which confirmed their formation. Single crystals suitable for X-ray diffraction were obtained for complex Cu(L4)Cl, in which the ligand coordinated in a tridentate monobasic ONS donor fashion. The compounds strongly bound to CT-DNA (Calf Thymus DNA) through intercalation. BSA (Bovine Serum Albumin) and HSA (Human Serum Albumin) binding studies were carried out to check the binding ability of the compounds with protein and the mechanism of quenching was found to be static. The occurrence of microenvironmental change in protein was further confirmed by three dimensional (3D) fluorescence experiments. DNA cleavage experiments of the complexes showed that the complexes cleaved supercoiled DNA pBR322 without any external agent. The complexes have shown significant growth inhibitory activity against selected types of bacteria namely S. aureus, S. pneumonia, P. auroginosa, S. paratyphi and fungi namely C. albicans, T. rubrum, A. niger, A. fumigatus and C. tropicalis. Tests on cell proliferation of human lung cancer cell line (A549) and human breast cancer cell line (MCF-7) were performed for all the compounds. The new water soluble complexes overcome cisplatin resistance in the MCF-7 and A549 cell lines. All the compounds were found to be non-toxic against human normal keratinocyte cells (HaCaT). The biological studies indicated that the complex Cu(L3)Cl (3) exhibited better activity among the compounds and the complexes exhibited biological activity in the following order Cu(L3)Cl (3) > Cu(L2)Cl (2) > Cu(L1)Cl (1) > Cu(L4)Cl (4).
The manuscript encompasses the synthesis of four water soluble copper(II) complexes, their structural characterization and a study of biological activities such as binding with CT-DNA, BSA/HSA, ...antimicrobial and anticancer. Results implied that the complexes showed better activity than the ligands. The antiproliferative activities of both the ligands and complexes on MCF-7 (human breast cancer) and A549 (human lung carcinoma) cell lines were seen to be greater than the standard drug cisplatin. The outcomes suggested complex 3 to be a potential antitumor agent.
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7-Hydroxy-4-oxo-4H-chromene Schiff bases and their corresponding water soluble copper(II) complexes were synthesized and characterized by various spectral techniques. The structural confirmation of the complexes 2 and 3 has been provided by X-ray crystallographic analysis. The binding affinities of the ligands and complexes with Calf Thymus DNA (CT-DNA) and proteins (Bovine Serum Albumin (BSA) and Human Serum Albumin (HSA)) were studied by using absorption and emission titration methods. An intercalative mode of binding with CT-DNA and a static quenching mechanism with albumin (BSA and HSA) was confirmed from the obtained results. The efficiency of the compounds in inhibiting the microbial growth was tested against various pathogenic bacteria Pseudomonas aeruginosa, Staphylococcus aureus, Streptococcus pneumoniae and Acinetobacter baumannii by using Gentamicin as standard and fungi Candida albicans, Aspergillus niger, Trichophyton rubrum, Candida tropicalis and Aspergillus fumigatus by using ketoconazole as standard and a significant activity has been found for the complexes. The anticancer potential of the ligands and complexes were tested against A549 and MCF-7 cells by MTT assay using cisplatin as a standard. The complexes 1–4 showed better cytotoxic profile than cisplatin, when incubated for a period of 48 h and 72 h. The results of all the biological analyses indicated the higher activity of the complexes over the ligands. Out of the complexes, complex 3 with the more electron donating ethyl group exhibited the higher activity.
Nanosized manganese ferrite (MnFe
2
O
4
) particles were prepared by sol–gel method using natural polymers like wheat flour (WF) and potato flour (PF) as surfactants and its structural, ...morphological, optical and magnetic characteristics were studied by X-ray diffraction (XRD), Fourier Transform Infrared Spectroscopy (FT-IR), scanning electron microscope (SEM), photoluminescence spectroscopy (PL) and vibration sample magnetometer (VSM). Brunauer–Emmett–Teller (BET) surface area test also performed and the results obtained were discussed. The average crystallite size was found to be 23 and 16 nm for WF/MnFe
2
O
4
and PF/MnFe
2
O
4
samples, respectively. Magnetic hysteresis loops confirmed the super-paramagnetic behavior for both the samples. For oxidation of benzyl alcohol to benzaldehyde, the catalytic activity of MnFe
2
O
4
nanoparticles (NPs) was carried out. Antimicrobial and antifungal activity of WF/MnFe
2
O
4
and PF/MnFe
2
O
4
samples were investigated against two Gram-positive bacteria (
Staphylococcus aureus
,
Streptococcus pneumoniae
), two Gram-negative bacteria (
Pseudomonas aeruginosa
,
Salmonella paratyphi
) and fungus (
Candida albicans
) using inhibition zone method. Minimum Inhibitory Concentration (MIC) values also calculated to determine susceptibilities of bacteria to drugs and also to evaluate the activity of new antimicrobial agents. The in vitro cytotoxicity of newly synthesized samples were analyzed by MTT assay against MCF-7, A549 and HaCaT cell lines in a dose-dependent fashion. Among these two samples, sample B (using potato flour) shows better response than sample A (using wheat flour) and both the samples were non-toxic to normal cell line. The concentration required to kill 50% of the cell (IC
50
) was also calculated.
Graphical Abstract
MnFe
2
O
4
nanoparticles were synthesized by sol–gel method using natural polymers, wheat flour and potato flour, as surfactant. The as-prepared MnFe
2
O
4
was characterized by XRD, FT-IR, SEM, EDX, PL and VSM analysis. The average crystallite size was found to be 23 and 16 nm for WF/MnFe
2
O
4
and PF/MnFe
2
O
4
samples, respectively. Magnetic hysteresis loops confirmed the super-paramagnetic behavior for both the samples. The catalytic activity of MnFe
2
O
4
nanoparticles (NPs) were carried out for oxidation of benzyl alcohol to benzaldehyde. Biological activities like antimicrobial, antifungal and anticancer activities of the samples were investigated. Among these two samples, PF/MnFe
2
O
4
shows better response than WF/MnFe
2
O
4
and both the samples were non-toxic to normal cell line.
IC
50
values of WF/MnFe
2
O
4
(
a
) and PF/MnFe
2
O
4
(
b
) against A549 and MCF-7 cell lines
A series of four new, cyclometallated ruthenium (II) complexes was synthesized from 3-acetyl-8-methoxy-2H-chromen-2-one functionalized 4(N)- substituted thiosemicarbazones and characterized through ...various spectral and analytical methods. The molecular structures of the complexes 1, 2 and 4 were determined by single-crystal X-ray diffraction analysis, which confirmed that the complexes possess a distorted octahedral geometry with the ligands coordinating in a dibasic tridentate fashion via C, N and S atoms. DNA Calf Thymus DNA (CT-DNA) and protein Bovine Serum Albumin (BSA) and Human Serum Albumin (HSA) binding studies indicated an intercalative mode of binding with DNA and static quenching mechanism with proteins. The compounds cleaved plasmid DNA (pBR322) without application of any external agent and acted well as free radical scavengers. A good spectrum of antimicrobial activity was observed against four bacterial and five fungal pathogens. Two cancerous cell lines, MCF-7 (human breast cancer) and A549 (human lung carcinoma) were employed to test their in vitro cytotoxic activity using MTT assay. The complexes (1–4) showed better activity with lower IC50 values over cisplatin. Further non toxic nature of the complexes have been examined with human normal keratinocyte cell line HaCaT. Further, the results of Lactate dehydrogenase release (LDH) and Nitric Oxide (NO) release supported the cytotoxic nature of the compounds. The results of all the biological studies carried out implied that the complex 3 bearing an ethyl substituent was observed to be the best.
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•Four new organoruthenium (II) complexes have been synthesized and characterized.•The DNA/protein interactions of ligands and complexes were studied by a variety of techniques.•The antimicrobial activity against four different bacteria and five fungi have also been examined.•The antiproliferative activity was evaluated against MCF-7 and HeLa cell lines.•The complexes 1–4 showed potent anticancer activity over the standard drug, Cisplatin.
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