Dalton's Lymphoma Research Articles

Cytotoxic and antiproliferative activities of aqueous extract from aerial parts of Ampelocissus latifolia (Roxb.) Planch. on Dalton’s lymphoma cells

Ampelocissus latifolia (Roxb.) Planch. is an Indian medicinal native herb. The present study reports the cytotoxic and antiproliferative activities of the aqueous extract from aerial parts of A. latifolia (AEAAL) on Dalton’s lymphoma (DL) cells for the first time. Here, DL cells were cultured in vitro and treated with AEAAL (0.50–6 mg.mL−1) for up to 24 h. In vitro cytotoxicity and antiproliferation were measured by MTT and trypan blue assays, fluorescence microscope, agarose gel electrophoresis, and analysis of cell cycle kinetics by flow cytometer. Results indicated significant and concentration-dependent decreased survivability of AEAAL-treated DL cells, increased percentages of apoptotic cells, DNA laddering, increased sub-G1 cell frequency, and delay in cell cycle kinetics. Here, the reduced cell viability and increased sub-G1 cell populations were significantly correlated with the apoptosis rather than necrosis. Thus, the findings of our study suggested that water-soluble phytochemicals from AEAAL possess potential cytotoxic and antiproliferative activities and can hold a good future prospect as a potential drug candidate against the progression of cancer. However, advanced studies are essential for the isolation and chemical characterization of the bioactive principles and analysis of detailed molecular mechanism for the pharmacological application.

Malvidin Abrogates Oxidative Stress and Inflammatory Mediators to Inhibit Solid and Ascitic Tumor Development in Mice.

The anticancer activity of malvidin was studied in Dalton's lymphoma ascites (DLA)-induced solid and ascitic tumor mice models. Malvidin is a natural compound belonging to the family of O-methylated anthocyanidin and plays a predominant role in regulating both short- and long-term cellular activities. Animals were injected with DLA cells (1.5 × 106 cells/animal) to induce solid and ascitic tumors. The administration of malvidin (5 mg/kg bw and 10 mg/kg bw) was carried out for 10 consecutive days from the day of tumor induction for both solid and ascitic tumors. Cyclophosphamide, CTX (25 mg/kg bw), used as the standard drug, was also administered for 10 consecutive days. Treatment with malvidin showed a significant reduction in tumor volume and elevated white blood cell (WBC) count when compared to the DLA-bearing control animals. The treatment also maintained the body weight and hemoglobin level, and decreases in aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), gamma-glutamyl transferase (GGT) were also noted. This investigation also reported the decreased levels of cellular glutathione (GSH) in ascitic tumor groups. Malvidin reduced inflammatory mediator and cytokine levels, such as tumor necrosis factor level alpha (TNF-α) and interleukin-6 (IL-6), which serve as molecular targets for cancer prevention. A decrease in the level of reactive oxygen species (ROS), like nitric oxide (NO), was observed. Histopathological examination revealed altered morphological changes in tumor tissue and the alleviation of hepatic architecture due to DLA. Immunohistochemical analysis revealed the inhibition of iNOS. This study demonstrated that malvidin exhibited significant in vivo antitumor activity and that it was reasonably imputable to its increasing endogenous mechanism. We accent the pertinence of malvidin as a potential naturally derived drug target for tumor control.

Phytochemical analysis and in vitro cytostatic potential of ethnopharmacological important medicinal plants

Annonareticulate (Mart.), Lablab purpureus (L.) Sweet, Murrayakoenigii (L.) Spreng, Moringaoleifera (Lam.), Hibiscussabdariffa (L.) and Euphorbiahirta (L.) are most commonly used medicinal plants by the traditional healers of Karbi Anglong district of Assam, India against different human ailments including cancer suspected cases. The proposed study includes field survey related to ethnomedicinal aspects of medicinal plants, phytochemical analysis, and evaluation of their cytostatic potential with the possible mode of action against Dalton's lymphoma (DL) cell line. The phytochemical analysis of all the plant's extract was studied using standard protocol. The cytotoxicity of the methanol extracts was determined by MTT reduction assay. The effect of the same extract was also tested for development of apoptosis features in DL cells using a fluorescence microscope and flowcytometry. The underlying mechanism closely associated with apoptotic cell death was also studied by measuring reactive oxygen species (ROS), mitochondrial membrane potential, and expression level of apoptosis inducing proteins. Murraya koenigii induced more apoptotic features in DL cells, followed by Annona reticulate. The decrease in mitochondrial membrane potential, release of cytochrome- c, increase in ROS level and higher expression of caspases (3 and 9) after plant extracts treatment may cause involvement of mitochondria in the process of apoptosis. From this study, it can be concluded that the plant species mainly Murraya koenigi and Annona reticulate significantly induced cytotoxicity in DL cells through apoptosis by utilizing mitochondrial pathway.

Evaluation of In vitro Cytotoxic Activity of Methanolic leaves Extract of Chloris barbata

The present research involves cytotoxic evaluation of Chloris barbata leaves by employing various in vitro models. Extraction of active constituents of the leaves of Chloris barbata was done by using soxhlet apparatus with polar and non-polar solvents. Further the extract was subjected to phytochemical screening and the methanolic extract of the leaf reveals the presence of flavonoids, glycosides, alkaloids, saponins and triterpinoids. Invitro cytotoxic efficacy of the Chloris barbata leaf methanolic extract was assessed with Human epidermoid larynx carcinoma (Hep 2), African green monkey kidney normal (Vero), Dalton's Ascitic Lymphoma (DAL) cell lines by using tryphan blue dye exclusion test, MTT, Sulphorodamine B (SRB) and Neutral Red Uptake (NRU)assay. In Tryphan blue dye exclusion assay it was found that there is an increase in percentage of dead vero (92±0.49), DAL (76±0.47) and Hep-2 cells (82±0.36) with chloris barbata leaf extract 200μg/mlwhen compared to control. Standard 5-Fluorouracil (5μg/ml) has shown an increase in percentage of dead vero, DAL and Hep-2 cells to an extent of 100±1.49, 94±1.35 and 99±0.21 when compared to control. In MTT assay the percentage viability of DAL, Hep-2 and vero cells has been significantly reduced by chloris barbata leaf extract at 200μg/ml (DAL 0.941±0.95, Hep-2 0.714±1.62 and vero cells 1.364±1.48) when compared to control (% viability is 100). In SRB assay, the percentage growth inhibition of cell lines by methanolic leaf extract was found to be 56.362 (vero cells), 69.128 (DAL cells) and 61.354 (Hep-2 cells) when compared to control group. NRU assay has shown the IC50 values 24.11±3.82 (vero), 47.16±0.14 (DAL) and 31.26±2.15 (Hep-2 cells) with leaf extract when compared to control. The above results signify that the methanolic extract of Chloris barbata leaves have remarkable cytotoxic potential. Further isolation of active constituents and in vivo cytotoxic studies has to be carried out to establish the exact mechanism involved in anticancer activity of Chloris barbata leaf extract.

Eugenia Uniflora Active Fraction Inhibits Dalton Lymphoma Ascites in Swiss Albino Mice - An in Vivo Study

Eugenia Uniflora Active Fraction Inhibits Dalton Lymphoma Ascites in Swiss Albino Mice - An in Vivo Study - written by S. Syama , Dr. M.S Latha published on 2019/12/23 download full article with reference data and citations

Energetically significant unconventional O[sbnd]H⋯π contacts involving discrete guest (H2O)8 clusters in a fumarato bridged polymeric supramolecular host of Ni(II) phenanthroline: Antiproliferative evaluation and theoretical studies

A new coordination polymer of nickel(II) involving bridging fumarato viz. catena[μ-fumarato(1,10-phenanthroline monohydrate(diaqua))nickel(II)trihydrate], {[Ni(μ-fum)(phen)(H2O)2].3H2O}n (1) (where, fum = fumarate, phen = 1,10-phenanthroline monohydrate) has been synthesized in purely aqueous medium at room temperature. The crystal structure of the polymer has been determined by single crystal X-ray Diffraction analysis. The polymer has been characterised by FT-IR, electronic spectroscopy, thermal and elemental analysis. The zig-zag polymeric chain of 1 self assembles into 2D supramolecular network architecture via reciprocal π-π stacking interactions. The lattice water molecules are involved in the formation of unique supramolecular octameric linear water clusters involving alternate trimeric rings that stabilizes the 2D network architecture. The crystal structure of the polymer also reveals the self-assembled enclathration of (H2O)8 cluster into polymeric Ni(II) host involving fum ligands that brings rigidity to the structure. Theoretical calculations have been performed to analyse the non-covalent interactions observed in the solid-state structure of 1. In particular, we have analysed the π–π stacking interactions between the phen ligands and also the energetically significant unconventional OH⋯π interaction involving the π-system of fum. For the latter, we have investigated the ability of the double bond of fum (coordinated to Ni) to establish OH⋯π interaction with water in comparison to fum acid and simple ethene. Finally, the polymer has been investigated for potential anticancer activities considering cell cytotoxicity, apoptosis and molecular docking as a major parameters against Dalton’s lymphoma (DL) malignant cancer cell line and the results were compared with cisplatin (reference drug) under the same experimental conditions. DNA interaction and fragmentations have been investigated for compound 1 and pharmacophore features establish structure activity relationship (SAR).

Integration of a Nonsteroidal Anti-Inflammatory Drug with Luminescent Copper for in Vivo Cancer Therapy in a Mouse Model.

A facile, process of fabrication of a luminescent bovine serum albumin-copper nanocluster (BSA-CuNC) customized ibuprofen nanodrug (BSA-CuNC-Ibf), encapsulating the ibuprofen was developed. Ibuprofen, which is commonly used to treat inflammation, was utilized here as a model drug. The formation of BSA-CuNC initiated by encapsulation of the Cu ions within the protein moiety followed by gradual reduction of the Cu ions by certain amino acid residues like tyrosine and tryptophan at alkaline pH resulted in the formation of BSA-CuNC within the protein template. Heat treatment and lowering the pH fitted the ibuprofen in the center by hydrogen bonding, hydrophobic and electrostatic interactions, and resulted in the formation of nanoparticles. The nanodrug (BSA-CuNC-Ibf) thus formed was characterized by transmission electron microscopy (TEM), dynamic and static light scattering (DLS), and zeta potential. The spherical shaped nanodrug has a hydrodynamic diameter of about 100.4 ± 28.9 nm. The encapsulation efficiency was found to be 94% which corresponds to 1880 μg/mL of ibuprofen in the BSA-CuNC-Ibf nanodrug. The as synthesized BSA-CuNC-Ibf exhibited cytotoxicity on both human cervical cancer cells (HeLa) and human lung cancer cells (A549). The present nanodrug when explored for its tumor preventive role on Daltons lymphoma ascites (DLA) bearing Swiss albino mice, exemplified sizable inhibition of tumor growth by reactive oxygen species mediated apoptosis and by modulating prostaglandin (PGE2) levels. It also inhibited metastasis of the cancer cells, thus enhancing the life expectancy of the mice.

Cu(II) and Zn(II) complexes from a thiosemicarbazone derivative: Investigating the intermolecular interactions, crystal structures and cytotoxicity

Two complexes of Cu(II) and Zn(II) were prepared from a thiosemicarbazone derivative (H 2 esct) using their corresponding metal acetates and 2,2′-bipyridine as base. The complexes were characterized by elemental analyses, UV–visible, FT-IR and NMR spectroscopy. The structure of the thiosemicarbazone derivative and its five coordinated complexes were also determined by the single crystal X-ray diffraction study. Copper complex got crystallized in triclinic P 1 ¯ space group and zinc complex in monoclinic P 2 1 / c space group. The crystal structures of the complexes exhibited different types of intermolecular interactions, which have been further analyzed by Hirshfeld surface analysis and fingerprint plots. The in vitro cytotoxicity against Dalton lymphoma ascites cell lines showed that the Zn(II) and Cu(II) complexes are more cytotoxic than their corresponding proligand. • A new thiosemicarbazone and some of its transition metal(II) complexes were synthesized. • The compounds were characterized using spectroscopic techniques such as IR, UV–Vis, NMR etc . • Single crystal X-ray analysis confirmed that during complexation, the ligand acts as tridentate ONS donor forming five coordinateded geometry. • Visual analysis of short contacts was achieved through Hirshfeld surface analysis. • Cu(II) complex exhibited greater cytotoxicity as compared to a standard drug molecule.

Energetically significant antiparallel π-stacking contacts in Co(II), Ni(II) and Cu(II) coordination compounds of pyridine-2,6-dicarboxylates: Antiproliferative evaluation and theoretical studies

Three new coordination compounds of types [Co(py)(2,6-PDC)(H2O)2].H2O (1), [Ni(py)(2,6-PDC)(H2O)2].H2O (2) and [Cu(py)(2,6-PDC)(H2O)].2H2O (3) (py = pyridine, 2,6-PDC = Pyridine-2,6-dicarboxylate) have been synthesized from purely aqueous media and characterized using elemental analysis, spectroscopic (IR and electronic) and single crystal X-ray diffraction techniques. Several supramolecular contacts of types OH⋯O, CH⋯O, CH⋯π, CH⋯C and π–π stacking stabilize the crystal structures. The layers in the crystal structures stack in perpendicular direction resulting in 1D channel with enclathrated water molecules. The strength of the antiparallel π-stacking interactions involving the pyridine rings in the supramolecular dimer of the compounds have been evaluated using DFT calculations and the influence of the pyridine coordination to the strength of the stacking assembly have been confirmed. The anti-proliferative potential of the compounds has been studied in Dalton’s lymphoma (DL) cell line by using MTT cell viability assay and apoptosis assay. All the three complexes exhibit short term (24 h) cytotoxicity (∼20–30%) through apoptotic cell death with negligible cytotoxicity (∼5–10%) in normal cells. In silico docking simulation has been performed with apoptosis regulator protein BCL-2 for the identification of possible molecular mode of action of the synthesized complexes. The pharmacophore features based on structure activity relationship (SAR) of the complexes have been identified. The SAR results reveal that the molecular features such as, hydrophobic, aromatic, positive ionizable, negative ionizable, H-bond donor and acceptor and halogen bond donor associated with the structures of the compounds play important role in the biological activities. The ADMET features, viz., physicochemical properties, pharmacokinetics, drug-likeness and medicinal chemistry friendliness of the synthesized complexes have been investigated.

Novel Thiazine Substituted 9-Anilinoacridines: Synthesis, Antitumour Activity and Structure Activity Relationships.

9-anilinoacridines are acting as DNA-intercalating agents which plays an important role as antitumor drugs, due to their anti-proliferative properties. Some anticancer agents contain 9- anilinoacridines such as amsacrine (m-AMSA), and nitracrine (Ledakrine) have been already developed. In this study, novel 9-anilinoacridines substituted with thiazines 4a-r were designed, synthesized, characterized by physical and spectral data and their cytotoxic activities against DLA cell lines were evaluated. Among those compounds, 4b, c, e, g, i, j, k, m, o, p, q, r exhibited significant short term in vitro cytotoxic activity against Daltons lymphoma ascites (DLA) cells with CTC50 value of 0.18 to 0.31μM. The compounds 4b, c, e, g, i, j, k, m, o, p, q, r are also exhibited significant long term in vitro anti-tumour activity against human tumor cell lines, HEp-2 (laryngeal epithelial carcinoma) by Sulforhodamine B assay with CTC50 value of 0.20 to 0.39μM. The compounds 4b, i, j exhibited significant in vivo antitumor activity with % Increase in Life Span (ILS) 48-82%. Results obtained in this study clearly demonstrated that many of the thiazine substituted 9- anilinoacridines exert interesting anti-tumour activity. The compounds 4b, i, j have significant anti-tumour activity and useful drugs after further refinement. The above derivatives will encourage to design future antitumor agents with high therapeutic potentials.

Antiproliferative evaluation and supramolecular association involving electrostatically enhanced π-π interaction in isostructural coordination solids of Mn(II), Co(II) and Zn(II) chlorobenzoates: Experimental and theoretical studies

Three new isostructural coordination solids viz. [Co(3-CNpy)2(2-ClBz)2(H2O)2] (1), [Mn(3-CNpy)2(2-ClBz)2(H2O)2] (2) and [Zn(3-CNpy)2(2-ClBz)2(H2O)2] (3) (3-CNpy = 3-cyanopyridine, 2-ClBz = 2-chlorobenzoate) have been synthesized from purely aqueous media and characterized by X-ray crystal structure analysis, FT-IR, electronic spectra and TGA. Several non-covalent hydrogen bonding interactions of the types OH⋯O, CH⋯O, CH⋯N, CH⋯Cl and π-π stacking contacts build up the supramolecular networks in the crystal structures. Electrostatically enhanced π-π interactions are observed in 1–3 between the phenyl rings of 2-ClBz and pyridine ring of 3-CNpy of the monomeric units of the complexes. We have used the molecular DFT calculations to evaluate energetically the strength of these contacts and also to analyze the effect of the metal on the interaction energies. The energetic features of the H-bonding and π-stacking interactions for 1–3 reveal that the H-bonded assembly is more favorable than the π-stacked contacts. The electrostatically enhanced energy of the π-stacking interactions is stronger than that usually observed for π-stacking interactions involving arenes. The cytostatic potential of all complexes have been studied in Dalton’s lymphoma (DL) cell line by MTT assay, apoptosis assay and further corroborated with molecular docking simulation. The complexes exhibit cytotoxicity (∼25–30%) through apoptotic cell death with negligible cytotoxicity (∼5–10%) in normal PBMC cells. In silico-docking techniques have been performed with apoptosis regulator protein BCL-2 for the identification of critical amino acids and their possible binding affinity with the synthesized complexes. The pharmacophore features based on structure activity relationship (SAR) of the complexes have been identified and the study reveal that the features viz., hydrophobic, aromatic, positive ionizable, negative ionizable, H-bond donor and acceptor and halogen bond donor properties play important role for the biological activities of the complexes.

Supramolecular association involving antiparallel CO⋯CO and anion–π contacts in Co(II) and Mn(II) complexes involving 2,5-pyridinedicarboxylate: Anticancer evaluation and theoretical studies

Two new coordination solids viz. [Co(2,5-PDC)(H2O)4] 2H2O (1) and [Mn(2,5-PDC)(H2O)4] 2H2O [2,5-PDC = 2,5-pyridinedicarboxylat] (2) have been synthesized and characterized by Single crystal X-ray analysis, FT-IR, electronic spectra and TGA. Single-crystal X-ray diffraction studies reveal that compounds 1 and 2 are isostructural and extensive OH⋯O hydrogen bonds along with CH⋯O and anion⋯π interactions stabilize the crystal structures. The lattice water molecules are responsible for the 3D framework of the complexes. The remarkable combination of OH⋯O, anion–π and antiparallel CO⋯CO interactions observed in the solid state structures have been analyzed by means of DFT calculations, molecular electrostatic potential (MEP) surface and non-covalent interaction (NCI plot) index computational tools. The anticancer activity of synthesized complexes has been studied in Dalton’s lymphoma (DL) cell line using MTT based cytotoxicity study, fluorescence based apoptosis study, molecular docking and pharmacophore modeling. Both complexes significantly (P ≤ 0.05) induced cytotoxicity through apoptotic cell death in DL cells with negligible cytotoxicity (∼5–10%) in normal blood cells. It is worth mentioning that compounds 1 and 2 interact with highly expressed anti-apoptotic cancer target proteins under study with higher binding affinity and the results are comparable with respective reference inhibitors. Moreover, both complexes also bear significant pharmacophore features such as H-bond donor and acceptor, aromatic and hydrophobic sites which are responsible for anticancer activities.

Oxovanadium(V) and Dioxomolybdenum(VI) Complexes of Amide-Imine Conjugates: Structures, Catalytic and Antitumor Activities.

Three new amide-imine conjugates, namely [(E)-2-hydroxy-N'-((2-hydroxynaphthalen-1-yl)methylene)benzohydrazide] (SALNP), [(E)-N'-(4-(diethylamino)-2-hydroxybenzylidene)-2-hydroxybenzohydrazide] (SALSD), and [(E)-N'-(3-ethoxy-4-hydroxybenzylidene)-2-hydroxybenzohydrazide] (SALVN), derived by reacting 2-hydroxybenzohydrazide (SAL) with three different aldehyde, 2-hydroxynapthaldehyde, 4-(diethylamino)-2-hydroxybenzaldehyde, and 3-ethoxy-4-hydroxybenzaldehyde, respectively. Three mononuclear oxovanadium(V) and two μoxo-bridged dinuclear molybdenum(VI) complexes have been synthesized using SALNP and SALSD. Besides, SALVN is used to prepare oxovanadium(V) and dioxomolybdenum(VI) complexes. All five metal complexes along with three amide-imine conjugates are characterized by single crystal XRD analysis. Some of them have been explored as catalyst for oxidation of alkyl benzene and styrene. Antitumor activities of the metal complexes along with ligands have been studied on Dalton lymphoma (DL) and 2PK3 murine lymphoma cells.

Antimetabolic Agent 3-Bromopyruvate Exerts Myelopotentiating Action in a Murine Host Bearing a Progressively Growing Ascitic Thymoma

ABSTRACTTumor growth and its chemotherapeutic regimens manifest myelosuppression, which is one of the possible causes underlying the limited success of immunotherapeutic anticancer strategies. Hence, approaches are being designed to develop safer therapeutic regimens that may have minimal damaging action on the process of myelopoiesis. 3-Bromopyruvate (3-BP) is a highly potent antimetabolic agent displaying a broad spectrum antineoplastic activity. However, 3-BP has not been investigated for its effect on the process of myelopoiesis in a tumor-bearing host. Hence, in this investigation, we studied the myelopoietic effect of in vivo administration of 3-BP to a murine host bearing a progressively growing ascitic thymoma designated as Dalton’s lymphoma (DL). 3-BP administration to the DL-bearing mice resulted in a myelopotentiating action, reflected by an elevated count of bone marrow cells (BMC) accompanied by augmented proliferative ability and a declined induction of apoptosis. The BMC of 3-BP-administered mice displayed enhanced responsiveness to macrophage colony-stimulating factor for colony-forming ability of myeloid lineage along with an enhanced differentiation of F4/80+ bone marrow-derived macrophages (BMDM). BMDM differentiated from the BMC of 3-BP-administered DL-bearing mice showed an augmented response to lipopolysaccharide and interferon-γ for activation, displaying an augmented tumor cytotoxicity, expression of cytokines, reactive oxygen species, nitric oxide, CD11c, TLR-4, and HSP70. These features are indicative of the differentiation of M1 subtype of macrophages. Thus, this study demonstrates the myelopotentiating action of 3-BP, indicating its hematopoietic safety and potential for reinforcing the differentiation of macrophages in a tumor-bearing host.

Energetically significant unconventional π-π contacts involving fumarate in a novel coordination polymer of Zn(II): In-vitro anticancer evaluation and theoretical studies

A new fumarato bridged Zn(II) coordination polymer viz. catena[μ-fumaratobis(3,5-dimethylpyrazole)zinc(II)trihydrate],{[Zn2(μ-fum)2(Hdmpz)4]·3H2O}n (1) (where, fum = fumarate, Hdmpz = 3,5-dimethylpyrazole) has been synthesized in purely aqueous medium at room temperature. The compound is structurally characterized by single crystal X-ray diffraction, FT-IR, electronic spectroscopy, PXRD and TGA. The zig-zag polymeric chain of 1 self assembles into a 2D supramolecular network via CH⋯π, CH⋯C, NH⋯O and CH⋯O interactions. Particularly relevant in 1, since in addition to the aforementioned non-covalent interactions, the electron rich π-system of fumarate is involved in energetically significant unconventional π–π contacts with the electron poor π-cloud of Hdmpz, which have been analyzed by DFT calculations and characterized using the non-covalent interaction (NCI) plot index. The strong H-bond agrees well with the MEP analysis since it is established between the H-bond donor involving NH group of Hdmpz and the H-bond acceptor involving O-atom of carboxylate moiety. The compound has been investigated for anticancer activities considering cell cytotoxicity, apoptosis and molecular docking as parameters in Dalton’s lymphoma (DL) malignant cancer cell line and results were compared with cisplatin (reference drug) under the same experimental conditions. Interestingly, negligible cytotoxic effect was observed against normal cells (PBMC) in comparison to the cancer cells (DL). The treatment of the compound caused appearance of apoptotic cells as evident by fluorescence based nuclear morphology study. The in silico study reveals that the compound interacts with the antiapoptotic proteins such as bcl-2, bcl-XL and Mcl-1 which may lead to apoptotic cell death.

Design, Synthesis and Anticancer Activity of Site Specific Short Chain Cationic Peptide

In spite of current progress in treatment methods, cancer is a major source of morbidity and death rate all over the world. Traditional chemotherapeutic agents aim to divide cancerous cells, are often associated with deleterious side effects to healthy cells and tissues. Host defense peptides Cecropin A and B obtained from insects are capable to lyses various types of human cancer cells at peptide concentrations which are not fatal to normal eukaryotic cells. In the present work we have designed short chain α-helical linear and cyclic peptide from cecropin A having same cationic charge, hydrophobicity and helicity. Synthesis of designed novel short chain linear (10) and cyclic compound (12) was accomplished by using solution phase method. All the coupling reactions were carried out by using dicyclohexylcarbodiimide (DCC) as the coupling reagent at room temperature in the presence of N-methylmorpholine (NMM) as the base. The Structure of newly synthesized peptidse were elucidated by 1H-NMR, 13C-NMR, FT-IR, FABMS and elemental analysis data.Cytotoxicity of synthesized compound was tested against Dalton's Lymphoma Ascites (DLA), Ehrlich's Ascites Carcinoma (EAC) and MCF-7 cell lines by using MTT assay and 5-FU as reference compound. From biological assessment,it was found that short chain cyclicpeptide12 showed high level of cytotoxic activity against DLA and EAC cell lines. By utilizing a structure-based rational approach to anticancer peptide design from cecropin A, we were able to develop short chain linear and cyclic peptides having same charge, hydrophobicity and with improved activity. Systematically removing amino acids, we were able to retaining peptide charge and hydrophobicity/hydrophilicity in linear and cyclic peptide which results to optimize the anticancer activity against DLA and EAC cell lines.

Synthesis of spheroid shaped silver nanoparticles using Indian traditional medicinal plant Flacourtia indica and their in vitro anti-proliferative activity

The silver nanoparticles (AgNPs) synthesized by physical and chemical methods are not much desirable due to the use of high energy consumption, environmentally toxic and biological hazards chemicals. Therefore green synthesis of AgNPs using natural plant extract is more appropriate method. Hence, in the present work we have employed an anti-cancer plant, which is used in Indian system of medicine Flacourtia indica to develop the AgNPs and also revealed their anticancer potential in Dalton Lymphoma Ascites (DLA) cell line model. Among the solvent extracts of F. indica, methanol extract was found to contain higher level of yield (5.14 g/100 g) and total phenolic compounds (9104 mg gallic acid equivalents/L) with good antioxidant power. Hence the preparation of methanolic extract from F. indica was optimized using Response Surface Methodology (RSM), which indicated that 88% of methanol concentration, 50 °C of temperature and 88 min of extraction time results in higher phenolic yield. The optimized F. indica extract strongly reduced the silver into AgNPs. The synthesized AgNPs were characterized using Ultraviolet-visible spectroscopy scanning (major peak at 455 nm), transmission electron microscopy (particle size of 14–24 nm) and zeta potential (−15 mV). The higher level of anti-proliferative activity (76.97%) was noted for AgNPs when compared to crude extract in DLA cell line model through cytotoxicity assay.

Photocatalytic degradation of environmental perilous gentian violet dye using leucaena-mediated zinc oxide nanoparticle and its anticancer activity

Phytomediated synthesis of metal oxide nanoparticles has become a key research area in nanotechnology due to its wide applicability in various biomedical fields. The present work explores the biosynthesis of zinc oxide nanoparticles (ZnO-NPs) using Leucaena leucocephala leaf extract. The synthesised ZnO-NPs were characterised by ultraviolet–visible (UV–Vis) spectroscopy, scanning electron microscopy (SEM), energy-dispersive X-ray spectroscopy (EDX), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), transmission electron microscopy (TEM) and selected area electron diffraction (SAED) studies. Biosynthesised ZnO-NPs are found to have wurtzite hexagonal structure with particles distributed in the range of 50–200 nm as confirmed by TEM studies. The anticancer activity of ZnO-NPs against MCF-7 (breast cancer) and PC-3 (human prostate cancer) cell lines was evaluated using 3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. From the assay, biosynthesised ZnO-NPs have better cytotoxic activity on PC-3 cell lines than MCF-7 cell lines. The in vitro cytotoxicity studies of biosynthesised ZnO-NPs against Dalton lymphoma ascites (DLA) cells reveal better antitumor activity of 92% inhibition with concentration of 200 µg·ml−1 of ZnO-NPs, and as the concentration increases, the anticancer efficiency as well increases, and also, it has excellent photocatalytic activity to degrade crystal violet dye in aqueous solution after irradiation of 90 min. The result suggests that the green synthesis of ZnO-NPs could be easily recovered and reused several times without any significant loss of the catalytic activity. The advantage of this technique lies in its low cost, easily climbable and non-use of toxic agents.

Some Phytochemical, Antimicrobial and Anticancer Tests for an Aqueous extract of Acmella oleracea

Acmella oleracea (family Asteraceae) is known for its diverse applications such as food supplement, vegetable, antioxidant, antineoplastic, antimicrobial, ornamental plant and pig fodder. We prepared an aqueous extract from which the presence of alkaloids, tannins and saponins were detected. These chemical groups have been known for their wide-ranging therapeutic properties. The antibacterial activity was tested on Gram-negative bacteria such as Klebsiella pneumoniae, Pseudomonas aeruginosa and Escherichia coli, and a Gram-positive species Bacillus subtilis. The plant extract showed no activity compared to that of the standard antibiotic tetracycline. Cytotoxic activity was also studied on cancer cell lines. We found an inverse relationship between treatment concentration and percent inhibition for HeLa (ATCC® CCL-2™) and V79 (ATCC® CCL-93™), however, the plant extract showed negligible effect on Dalton's lymphoma ascites even at the highest concentration tested. The lower degree of inhibitions observed at higher concentrations for HeLa and V79 suggests that the plant extract might confer proliferative effect rather than antimitogenic effects on the cancer cells. The results indicate that A. oleracea has unique medicinal properties, which in turn provide the rationale for further investigations.

Modulation of various enzyme activities and lipid peroxidation by Schima wallichii (DC.) Korth in mice bearing Dalton's ascitic lymphoma

Modulation of various enzyme activities and lipid peroxidation by<i> Schima wallichii (DC.)</i> Korth in mice bearing Dalton's ascitic lymphoma