Apoptosis induction capability of silver nanoparticles capped with Acorus calamus L. and Dalbergia sissoo Roxb. Ex DC. against lung carcinoma cells.

Silver nanoparticles (AgNPs) were prepared using a one-step reduction of silver nitrate (AgNO3) with sodium borohydride (NaBH4) in the presence of polyvinylpyrrolidone (PVP) as a capping agent. Plant extracts from D. sissoo (DS) and A. calamus L. (AC) leaves were incorporated during the synthesis process. The crystalline nature of the AgNPs was confirmed through X-ray diffraction (XRD), confirming the face-centered cubic structure, with a lattice constant of 4.08 Å and a crystallite size of 18 nm. Field Emission Gun Transmission Electron Microscopy (FEG-TEM) revealed spherical AgNPs (10-20 nm) with evident PVP adsorption, leading to size changes and agglomeration. UV-Vis spectra showed a surface plasmon resonance (SPR) band at 417 nm for AgNPs and a redshift to 420 nm for PVP-coated AgNPs, indicating successful synthesis. Fourier Transform Infrared Spectroscopy (FTIR) identified functional groups and drug-loaded samples exhibited characteristic peaks, confirming effective drug loading. The anti-cancer potential of synthesized NPs was assessed by MTT assay in human adenocarcinoma lung cancer (A549) and lung normal cells (WI-38) cells. IC50 values for all three NPs (AgPVP NPs, DS@AgPVP NPs, and AC@AgPVP NPs) were 41.60 ± 2.35, 14.25 ± 1.85, and 21.75 ± 0.498 µg/ml on A549 cells, and 420.69 ± 2.87, 408.20 ± 3.41, and 391.80 ± 1.55 µg/ml respectively. Furthermore, the NPs generated Reactive Oxygen Species (ROS) and altered the mitochondrial membrane potential (MMP). Differential staining techniques were used to investigate the apoptosis-inducing properties of the three synthesized NPs. The colony formation assay indicated that nanoparticle therapy prevented cancer cell invasion. Finally, Real-Time PCR (RT-PCR) analysis predicted the expression pattern of many apoptosis-related genes (Caspase 3, 9, and 8).

Biochanin A - A G6PD inhibitor: In silico and in vitro studies in non-small cell lung cancer cells (A549).

Secondary metabolites from medicinal plants have a well-established therapeutic potential, with many of these chemicals having specialized medical uses. Isoflavonoids, a type of secondary metabolite, have little cytotoxicity against healthy human cells, making them interesting candidates for cancer treatment. Extensive research has been conducted to investigate the chemo-preventive benefits of flavonoids in treating various cancers. Biochanin A (BA), an isoflavonoid abundant in plants such as red clover, soy, peanuts, and chickpeas, was the subject of our present study. This study aimed to determine how BA affected glucose-6-phosphate dehydrogenase (G6PD) in human lung cancer cells. The study provides meaningful insight and a significant impact of BA on the association between metastasis, inflammation, and G6PD inhibition in A549 cells. Comprehensive in vitro tests revealed that BA has anti-inflammatory effects. Molecular docking experiments shed light on BA's high binding affinity for the G6PD receptor. BA substantially decreased the expression of G6PD and other inflammatory and metastasis-related markers. In conclusion, our findings highlight the potential of BA as a therapeutic agent in cancer treatment, specifically by targeting G6PD and related pathways. BA's varied effects, which range from anti-inflammatory capabilities to metastasis reduction, make it an appealing option for future investigation in the development of new cancer therapeutics.

Isolation, identification, and characterization of α- asarone, from hydromethanolic leaf extract of Acorus calamus L. and its apoptosis-inducing mechanism in A549 cells.

Due to the presence of several active secondary metabolites, the traditional Indian and Chinese medicinal herb Acorus calamus L. has been utilized for both medical and culinary purposes since ancient times. A recent report has underscored the promising cytotoxic effect of A. calamus leaves extract against non-small cell lung cancer A549 cells. Thus, we want to separate the bioactive substance from the hydromethanolic extract of A. calamus leaves in the current investigation. Thin-layer chromatography was used to separate the compounds and different spectroscopic methods (UV, FTIR, NMR, and LCMS/MS) were used for the structure prediction. α-asarone was found to be the main bioactive compound present and it was isolated from A. calamus leaves extract. It exerted a good cytotoxic effect with an IC50 value of 21.43 ± 1.27 µM against A549 cells and IC50 value of 324.12 ± 1.32 µM against WI-38 cells. The induction of apoptosis in A549 cells by α-asarone was reaffirmed by the diverse differential staining methods including DAPI, Acridine Orange/Ethidium Bromide, and Giemsa staining. Additionally, α-asarone induced mitochondrial membrane potential (ΔΨm) dissipation with a concomitant increase in the production of ROS. Furthermore, it also increased expressions of caspase-3, caspase-9, caspase-8, DR4, and DR5 genes in A549 cells. In conclusion, α-asarone-induced apoptotic cell death in non-small lung cancer cells (A549) as a result of loss of mitochondrial function, increased ROS production, subsequent activation of an internal and extrinsic caspase pathway, and altered expression of genes controlling apoptosis. As a whole, α-asarone is a plausible therapeutic agent for managing lung cancer. HIGHLIGHTSIsolation of bioactive compound from hydromethanolic leaves extract of Acorus calamus L. by thin layer chromatography.Structural elucidation of the bioactive compound was carried out using different methods like UV analysis, FTIR, NMR, and LC-MS/MS analysis.A plausible mode of action revealed that α-asarone can induce apoptosis in lung cancer cells (A549).Communicated by Ramaswamy H. Sarma.

Lactiplantibacillus plantarum PGB02 Improved Serum Cholesterol Profile by Tweaking Genes Involved in Cholesterol Homeostasis in Male Swiss Albino Mice.

The effect of Lactiplantibacillus plantarum PGB02 isolated from buttermilk on serum cholesterol profile of normal and hypercholesterolemic mice was evaluated. Further changes in the expression of mice genes were determined. The hypercholesterolemia was induced in experimental mice by feeding high cholesterol and fat diet. Serum cholesterol parameters, physical parameters, cholic acid excretion, and cholesterol metabolism related gene expression analysis was carried out. L. plantarum PGB02 efficiently reduced total cholesterol, triglycerides, and LDL-cholesterol and improved HDL-cholesterol in hypercholesterolaemic mice. Body weight was reduced and fecal cholic acid increased in probiotic treatment groups. Gene expression analysis revealed that L. plantarum PGB02 up-regulated the expression of LDL receptors, CYP7A1, ABCA1, ABCG5, ABCG8, and down-regulated the expression of FXR and NPC1L1 genes. Summarizing the mechanism, L. plantarum PGB02 improved hypercholesterolemia by increasing bile acid synthesis and excretion, reducing exogeneous cholesterol absorption from the intestine, and increased LDL clearance through upregulation of LDL-receptors. The present study has given insight into the mechanism of serum cholesterol reduction by bile salt hydrolase positive L. plantarum PGB02 in mice. L. plantarum PGB02 reduced the serum cholesterol level through increased bile acid synthesis and deconjugation and reduced absorption of cholesterol in the intestine. Isolate PGB02 shown cholesterol removal potential as good as statin.

Synthesis, characterization, and biological applications of pyrazole moiety bearing osmium(IV) complexes.

Osmium (IV) complexes with pyrazole nucleus containing ligands were synthesized. Os(IV) compounds were characterized using ESI-MS, ICP-OES, IR spectroscopy, electronic spectroscopy, conductance, and magnetic measurements. Whereas, ligands were characterized by heteronuclear spectroscopy, (1H and 13C), IR spectroscopy, and elemental analysis. All the compounds were tested for their potential to interact with HS-DNA by absorption titration, fluorescence spectroscopy, viscosity measurement, and docking study. The quenching constant and Stern Volmer constant values were calculated using fluorescence study. The synthesized compounds were studied for in-vitro bacteriostatic and cytotoxic activities. The cancer cell line studies of all the synthesized complexes were carried out on human lung cancer cells (A549).Supplemental data for this article is available online at https://doi.org/10.1080/15257770.2021.1921795 .

Induction of pre-chorismate, jasmonate and salicylate pathways by Burkholderia sp. RR18 in peanut seedlings.

AIMS: To characterize the mechanisms by which bacteria in the peanut rhizosphere promote plant growth and suppress Aspergillus niger, the fungus that causes collar rot of peanut. METHODS AND RESULTS: In all, 131 isolates cultured from the peanut rhizosphere were assayed for growth promotion in a seedling germination assay. The most effective isolate, RR18, was identified as Burkholderia sp. by 16S sequencing analysis. RR18 reduced collar rot disease incidence and increased the germination rate and biomass of peanut seeds, and had broad-spectrum antifungal activity. Quantitative analyses showed that RR18 induced long-lasting accumulation of jasmonic acid, salicylic acid and phenols, and triggered the activity of six defence enzymes related to these changes. Comparative proteomic analysis of treated and untreated seedlings revealed a clear induction of four abundant proteins, including a member of the pre-chorismate pathway, a regulator of clathrin-coated vesicles, a transcription factor and a hypothetical protein. CONCLUSION: Burkholderia sp. RR18 promotes peanut growth and disease resistance, and stably induces two distinct defence pathways associated with systemic resistance. SIGNIFICANCE AND IMPACT OF THE STUDY: This study demonstrates that a strain of the Burkholderia cepacia complex can elicit both salicylic- and jasmonic-acid-mediated defences, in addition to having numerous other beneficial properties.

Biological Significance of Hetero-Scaffolds Based Gold(III) Complexes.

Synthesized ligands and complexes, [Au(Ln)Cl2]Cl, have been characterized by various techniques such as elemental analysis, LC-MS, FT-IR, UV-Vis, 1H and 13C NMR spectroscopy, conductance measurement and magnetic moments measurement. The experimental results show that complexes exhibit higher antibacterial activity against Gram(+ve) and Gram(-ve) microorganisms than free ligands. The in vitro cytotoxicity and cellular level cytotoxicity suggest that Au(III) complexes show better activity than corresponding ligands. The DNA interaction study has been evaluated using absorption titration. The experimental evidence indicates (Kb = 1.08-3.44 • 105 M-1) that all the complexes have been bind to HS-DNA by intercalation mode. To further verify the nature of interaction viscosity measurement and molecular modeling have been carried out which suggest the intercalation binding between complex and DNA. The Schizosaccharomyces pombe cell DNA cleavage has been performed using agarose gel and their photographic images of complexes show smearing of DNA due to DNA cleavage from the nucleus.

Benzothiazole analogues: Synthesis, characterization, MO calculations with PM6 and DFT, in silico studies and in vitro antimalarial as DHFR inhibitors and antimicrobial activities.

Benzothiazole analogues are of interest due to their potential activity against malarial and microbial infections. In search of suitable antimicrobial and antimalarial agents, we report here the synthesis, characterization and biological activities of benzothiazole analogues (J 1-J 10). The molecules were characterized by IR, Mass, 1H NMR, 13C NMR and elemental analysis. The in vitro antimicrobial activity was investigated against pathogenic strains; the results were explained with the help of DFT and PM6 molecular orbital calculations. In vitro cytotoxicity and genotoxicity of the molecules were studied against S. pombe cells. In vitro antimalarial activity was studied. The active compounds J 1, J 2, J 3, J 5 and J 6 were further evaluated for enzyme inhibition efficacy against the receptor Pf-DHFR, computational and in vitro studies were carried out to examine their candidatures as lead dihydrofolate reductase inhibitors.

Phytol induces ROS mediated apoptosis by induction of caspase 9 and 3 through activation of TRAIL, FAS and TNF receptors and inhibits tumor progression factor Glucose 6 phosphate dehydrogenase in lung carcinoma cell line (A549).

A number of drugs as well as lead molecules are isolated from natural sources. Phytol is one of such lead molecule belongs to terpenes group distributed widely in medicinal plants. In the present work, we investigated the cytotoxic behavior of phytol on human lung carcinoma cells (A549). Phytol was found to cause characteristic apoptotic morphological changes and generation of ROS in A549 cells. The mechanism of phytol involved the activation of TRAIL, FAS and TNF-α receptors along with caspase 9 and 3. In silico molecular docking studies revealed that phytol has a good binding affinity with glucose-6-phosphate dehydrogenase (G6PD), which is known to promote tumor proliferation. The ability of phytol to become potential drug candidate has been revealed from the pharmacokinetic study performed in the present study.

Maslinic Acid Inhibits Proliferation of Renal Cell Carcinoma Cell Lines and Suppresses Angiogenesis of Endothelial Cells.

Despite the introduction of many novel therapeutics in clinical practice, metastatic renal cell carcinoma (RCC) remains a treatment-resistant cancer. As red and processed meat are considered risk factors for RCC, and a vegetable-rich diet is thought to reduce this risk, research into plant-based therapeutics may provide valuable complementary or alternative therapeutics for the management of RCC. Herein, we present the antiproliferative and antiangiogenic effects of maslinic acid, which occurs naturally in edible plants, particularly in olive fruits, and also in a variety of medicinal plants. Human RCC cell lines (ACHN, Caki-1, and SN12K1), endothelial cells (human umbilical vein endothelial cell line [HUVEC]), and primary cultures of kidney proximal tubular epithelial cells (PTEC) were treated with maslinic acid. Maslinic acid was relatively less toxic to PTEC when compared with RCC under similar experimental conditions. In RCC cell lines, maslinic acid induced a significant reduction in proliferation, proliferating cell nuclear antigen, and colony formation. In HUVEC, maslinic acid induced a significant reduction in capillary tube formation in vitro and vascular endothelial growth factor. This study provides a rationale for incorporating a maslinic acid-rich diet either to reduce the risk of developing kidney cancer or as an adjunct to existing antiangiogenic therapy to improve efficacy.

Synthesis and biological screening of novel 2-morpholinoquinoline nucleus clubbed with 1,2,4-oxadiazole motifs.

Novel series of 2-morpholinoquinoline scaffolds (6a-n), containing the 1,2,4-oxadiazole and moiety, was designed and synthesized in good yield (76-86%). The synthesized compounds were screened for their preliminary in vitro antimicrobial activity against a panel of pathogenic strains of bacteria and fungi. Molecular docking and pharmacokinetic study were carried out for the prepared compounds. The cytotoxicity of the synthesized compounds was tested at different concentrations using bioassay of S. pombe cells at the cellular level. The effect of synthesized compounds on the DNA integrity of S. pombe was observed on agarose gel. Compounds 6d, 6e, 6g, 6h, 6j and 6n exhibited excellent antimicrobial potency as compared to the standard drugs (i.e Ampicillin, Norfloxacin, Chloramphenicol, Ciprofloxacin). Compounds 6d, 6e, 6g, 6k and 6n were found to have significant antifungal activity as compared to griseofulvin. Compounds 6f, 6i, 6k, 6l were found very less cytotoxic, while compounds 6d, 6e, 6g, 6h were found to exhibit maximum toxicity. The rest of the synthesized compounds were found to be moderately toxic.

Bacillus species (BT42) isolated from Coffea arabica L. rhizosphere antagonizes Colletotrichum gloeosporioides and Fusarium oxysporum and also exhibits multiple plant growth promoting activity.

BACKGROUND: Colletotrichum and Fusarium species are among pathogenic fungi widely affecting Coffea arabica L., resulting in major yield loss. In the present study, we aimed to isolate bacteria from root rhizosphere of the same plant that is capable of antagonizing Colletotrichum gloeosporioides and Fusarium oxysporum as well as promotes plant growth. RESULTS: A total of 42 Bacillus species were isolated, one of the isolates named BT42 showed maximum radial mycelial growth inhibition against Colletotrichum gloeosporioides (78%) and Fusarium oxysporum (86%). BT42 increased germination of Coffee arabica L. seeds by 38.89%, decreased disease incidence due to infection of Colletotrichum gloeosporioides to 2.77% and due to infection of Fusarium oxysporum to 0 (p < 0.001). The isolate BT42 showed multiple growth-promoting traits. The isolate showed maximum similarity with Bacillus amyloliquefaciens. CONCLUSION: Bacillus species (BT42), isolated in the present work was found to be capable of antagonizing the pathogenic effects of Colletotrichum gloeosporioides and Fusarium oxysporum. The mechanism of action of inhibition of the pathogenic fungi found to be synergistic effects of secondary metabolites, lytic enzymes, and siderophores. The major inhibitory secondary metabolite identified as harmine (ß-carboline alkaloids).

Simultaneous Detection and Quantification of Phytohormones by a Sensitive Method of Separation in Culture of Pseudomonas sp.

A high-performance thin-layer chromatography (HPTLC)-based sensitive, rapid and stringent protocol is designed for detection and quantification of five phytohormones simultaneously. Culture filtrate of Pseudomonas bacteria was acidified with 7 M HCl and extracted with an equal volume of ethyl acetate to separate abscisic acid (ABA), jasmonic acid (JA), gibberellic acid (GA3), and indole-3-acetic acid (IAA). Kinetin was extracted from the remaining water fraction of the same extract. Various extracts were loaded on silica gel 60 F254 foil using Linomat 5 spray on applicator. Standard phytohormones were also loaded adjacent to the sample, and the foils were developed with isopropanol-ammonia-water [10:1:1 (v/v)] as the mobile phase. A quantitative estimation of the separated ABA, kinetin, JA, GA3, and IAA was performed by measuring the absorbance at 260, 275, 295, 265, and 280 nm, respectively. HPTLC method was found to be cost effective, robust technique that can be routinely used for simultaneous phytohormone detection in plant or bacterial samples. The present work is not only useful for detection and quantification of phytohormones but also for screening of phytohormone producing microorganisms.

Novel morpholinoquinoline nucleus clubbed with pyrazoline scaffolds: Synthesis, antibacterial, antitubercular and antimalarial activities.

A series of novel morpholinoquinoline based conjugates with pyrazoline moiety were synthesized under microwave irradiation. The newly synthesized compounds were screened for their preliminary in vitro antibacterial activity against a panel of pathogenic strains of bacteria and fungi, antituberculosis activity against Mycobacterium tuberculosis H37Rv and antimalarial activity against Plasmodium falciparum. Most of them exhibited significant antibacterial activity as compared to the first line drugs. Compounds 6a and 9d were found to possess excellent antibacterial activity potency as compared to ampicillin (286 µM), chloramphenicol (154 µM) and ciprofloxacin (150 µM). In antifungal screening, against Candida albicans, compounds 6c, 7c, 8a, 8b, 8c and 9b showed significant activity as compared to griseofulvin (1147 µM). Compounds 8b, 6b, 9d, 6a, 9b, 7b and 8a displayed brilliant activity against P. falciparum strain as compared to chloroquine (IC50 0.062 µM) as well as quinine (IC50 0.826 µM). Compounds 6d, 7b, 8b, 9c and 9d exhibited superior antitubercular activity. Among them 8b was found to be equipotent to rifampicin with 95% inhibition. The cytotoxicity of the synthesized compounds was tested using bioassay of Schizosaccharomyces pombe cells at cellular level.

Cellular Effect of Curcumin and Citral Combination on Breast Cancer Cells: Induction of Apoptosis and Cell Cycle Arrest.

PURPOSE: The unmanageable side effects caused by current chemotherapy regimens to treat cancer are an unresolved problem. Although many phytonutrients are useful as chemoprevention without side effects, their effects are slower and smaller than conventional chemotherapy. In the present work, we examined the cumulative effect of two phytonutrients, curcumin and citral, on breast cancer cell lines and compared their effect with the known chemotherapy regimen of cyclophosphamide, methotrexate, and 5-fluorouracil. METHODS: Using cultured breast cancer and normal epithelial cells, the cytotoxic and apoptotic effect of curcumin and citral was evaluated in vitro. The synergistic effect of curcumin and citral was calculated by a combination index study using the method by Chou and Talalay. Cell death pathways and mechanisms were analyzed by measuring intracellular reactive oxygen species (ROS) and apoptotic protein levels. RESULTS: Curcumin and citral caused dose and time dependent cell death and showed a synergistic effect at effective concentration EC50 and above concentrations in breast cancer cells without disturbing normal breast epithelial cells. With combination curcumin and citral treatment, apoptosis induction and cell cycle arrest at G0/G1 phase in breast cancer cells were observed. Curcumin and citral generated ROS and activated p53 and poly (ADP-ribose) polymerase-1 mediated apoptotic pathways. CONCLUSION: The results of this study suggest that curcumin and citral in combination may be a useful therapeutic intervention for breast cancer.

Addition of citral controls ROS and reduces toxicity in 5-fluorouracil treated Schizosaccharomyces pombe cells.

In systemic therapy, chemotherapeutic drugs, often, cause considerable side effects; and combination of natural compounds lessen the extent of such effects. In the present study, combined effect of citral and 5-fluorouracil was studied in Schizosaccharomyces pombe cells. The antagonistic combination index found was at 0.01 and 0.025 mM of citral with 40 µg or higher concentration of 5-fluorouracil. The combined treatment was so effective that higher number of cells underwent apoptosis compared to individual treatment of 5-fluorouracil. Citral controlled ROS levels and increased survival of normal cells. Several differentially expressed proteins observed in the citral treatment could further help understanding its mechanism of action.

Purification, characterization and application of lipoxygenase isoenzymes from Lasiodiplodia theobromae.

Lipoxygenase oxidizes linoleic acid into hydroperoxy octadecadienoic acid (HPOD), which is important in food and flavour industries for production of bread and flavouring compounds. As Lasiodiplodia theobromae is an unexplored, good source of lipoxygenase, it was purified from it by size-exclusion (Sephadex G100) and ion-exchange (DEAE-cellulose) chromatography and characterized. Upon purification, L. theobromae was found to contain two different lipoxygenases, one of 93 kDa (LOX1) and another of 45 kDa (LOX2). Both the isoenzymes were having optimum pH 6.0 and optimum temperatures 50 and 40 °C, respectively. The catalytic efficiency of LOX1 and LOX2 was found to be 1300 and 1.67 × 10(9), respectively. The catalytic efficiency of LOX2 is higher than the catalytic efficiency of soya bean LOX1 that is 10.9 × 10(6). Both the isoenzymes of LOX oxidized linoleic acid to produce 9-HPOD and 13-HPOD both; however, LOX1 produced more of 9-HPOD and LOX2 produced more of 13-HPOD. Both the LOXes were not inhibited by jasmonic acid. Addition of LOX1 and LOX2 altered the elasticity as well as viscosity of dough prepared from bleached wheat flour.

L-carvone induces p53, caspase 3 mediated apoptosis and inhibits the migration of breast cancer cell lines.

A wide variety of natural compounds exists that possesses significant cytotoxic as well as chemopreventive activity through induction of apoptosis in cancer cells. The antiproliferative and apoptotic effect of L-carvone, an active component of spearmint (Mentha spicata) was studied on breast cancer (MCF 7 and MDA MB 231) and normal (MCF 10A) cell lines, and insight into its mechanism of action was attained. L-carvone inhibited proliferation of MCF 7 (IC50 1.2 mM) and MDA MB 231 cells (IC50 1.0 mM) and inhibited the migration of breast cancer cell lines. L-carvone induced apoptosis as observed by nuclei fragmentation and the presence of apoptotic bodies in DAPI, AnnexinV/propidium iodide, and TUNEL assays. L-carvone exposure arrested MCF 7 cells in S phase of the cell cycle. DNA damage caused by L-carvone was apparent from the increased tail moment in COMET assay, which could be induced by an increase in ROS that was measured using a fluorescence probe. Glutathione levels were also increased. The increased level of p53, Bad, cleaved caspase 3, and cleaved PARP explained p53 and caspase-mediated apoptosis.

Induction of systemic resistance in different varieties of Solanum tuberosum by pure and crude elicitor treatment.

A 10 kD elicitor protein (infestin) produced by Phytopthora infestans was purified and its efficacy for induction of systemic resistance in resistant and susceptible varieties of Solanum tuberosum was studied. Culture filtrates from P. infestans with and without purified elicitor (infestin) were used as elicitors to understand the effect of purified elicitor (infestin) on development of systemic resistance. Culture filtrate and purified elicitor (infestin) were found to induce hypersensitive reaction on the leaves of resistant varieties, but not on susceptible varieties after 48 h. Culture filtrate devoid of purified elicitor (infestin) did not induce any necrotic spots even on resistant variety. Purified elicitor (infestin) was found to induce glucose oxidase, NADPH oxidase, superoxide dismutase, glutathione reductase, catalase and peroxidase enzymes in resistant S. tuberosum plants, however the induction of these enzymes was low in susceptible varieties. The oxidative enzymes were found to induce earlier than antioxidative enzymes and there was negative correlation between these two groups of enzymes. Levels of salicylic acid, phenylalanine ammonia lyase (PAL), beta-1, 3 glucanase and chitinase activities were also found higher in resistant than in susceptible varieties. It was observed that purified elicitor (infestin) was superior to crude culture filtrate, but was not capable of inducing systemic resistance in susceptible varieties.

Ternary copper(II) complexes of levofloxacin and phenanthroline derivatives: in-vitro antibacterial, DNA interactions, and SOD-like activity.

A series of ternary copper(II) complexes have been derived using levofloxacin and five phenanthroline derivatives. Complexes were characterized using infrared spectroscopy, Thermogravimetric (TG)-analysis, fast atom bombardment mass spectroscopy and reflectance spectra. Synthesized complexes exhibit the only d-d band at ∼ 666 nm points toward a distorted square pyramidal geometry at metal centre with one unpaired electron responsible for paramagnetic behaviour of whole moiety. Binding behaviour of the complexes toward Herring Sperm DNA were determined using ultraviolet-Vis (UV-Vis) absorption titration and viscometric titration experiment, where as the cleavage efficacy of the complexes toward pUC19 DNA was determined by electrophoresis in presence of ethidium bromide. Complexes exhibit superoxide dismutase-like activity with their IC(50) values ranging from 0.7917 to 1.7432 µM.