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Due to the broad-spectrum biological activities, fused heterocyclic compounds are one of the most important systems in medicinal chemistry. Among them, the imidazothiazole which contains a bridgehead nitrogen atom has a vital role because of various applications such as anticancer, antimalarial, antiviral, etc. Designing various imidazothiazole scaffolds has become more important because of their several biological applications. The present review paper discusses the numerous biological applications of imidazothiazole scaffolds in the field of medicine. The review would be useful in future drug design for the development of more promising drug-like scaffolds.

Six heteroleptic oxovanadium(IV) complexes with general formula [VOL1–6(nap)], where, L1–3=2-(1-(4-substitutedphenyl)ethylidene)hydrazinecarbothioamide, L4–6=2-(1-(4-substitutedphenyl)ethylidene)-N-methylhydrazinecarbothioamide and nap=naproxen, have been synthesized and characterized. FTIR spectra exhibit a strong band between 965 and 991 cm−1, characteristic of υ(V=O) stretching vibration. UV-Vis and theoretical studies suggested distorted square-pyramidal geometry and oxidation state of vanadium(IV) with d1 configuration was confirmed by EPR spectra. Cyclic voltammograms exhibit metal based irreversible redox peaks corresponding to one electron oxidation (+0.83 to +0.70 V) and reduction (−0.69 to −0.53 V) processes. In vitro antioxidant studies revealed that complexes containing electron donating substituent (−CH3) showed higher activity. In vitro antidiabetic activity of complexes with enzymes like α-amylase, α-glucosidase and glucose-6-phosphatase made them better inhibitors of insulin, which is further supported by in silico studies, and complex 6 shows better in vitro insulin mimic activity against insulin responsive 3T3-L1 adipocyte cells compared to insulin and metformin.

Eight heteroleptic nickel(II) and copper(II) complexes of the type [M(L1–4)(nap)2] (1–8), where L1–4 = 2-(1-(4-substitutedphenyl)ethylidene)hydrazinecarbothioamide, nap = naproxen, and M = Ni(II) o...

In this paper, we report the phytosynthesis of Ag/CuO nanocomposites (NCs) using Murraya koenigii and Zingiber officinale green extracts containing unique metabolites. The silver and copper oxide nanoparticles, and Ag/CuO NCs were also synthesized by chemical methods for the purpose of comparison with phytosynthesized Ag/CuO NCs. All the synthesized nanomaterials were characterized by diverse spectro-analytical methods. The phytochemical analysis confirmed the presence of active phytoconstituents in the Murraya koenigii and Zingiber officinale extracts. The major biomolecules present in the plant extracts act as reducing and capping agents in the green synthesis process, as identified using FT IR spectroscopy. The maximum absorbance at ~ 290 and ~ 460 nm corresponding to CuO and Ag evidenced the formation of Ag/CuO NCs. Further, the XRD patterns also confirmed the formation of nanocomposites by exhibiting the fcc crystalline and monoclinic nature of Ag and CuO nanoparticles, respectively. The SEM images displayed the spherical shape of the synthesized NCs, and the EDX spectra confirmed the presence of Ag, Cu and O elements in the synthesized NCs. The TEM images revealed the relatively uniform size of the synthesized nanomaterials ranging between 18 and 22 nm. The in vitro antidiabetic activity with α-amylase, α-glucosidase and glucose-6-phosphatase enzymes, and glucose uptake assay showed that the Ag/CuO NCs synthesized using Zingiber officinale extract displayed highest activity than the rest of the synthesized nanomaterials.

A series of six new bis(thiosemicarbazone)copper(I) complexes of the type [Cu(L1–6)2Cl] (1−6) were synthesized and characterized. The complexes adopted trigonal planar ′Y′ shaped geometry coordinating through two thione sulphur atoms of two ligand molecules and one chloride ion. All the complexes intercalatively bind with calf thymus DNA (CT−DNA) as evidenced by spectral and molecular docking studies. The absorption and emission spectral techniques confirmed the strong interaction of the complexes with BSA via static quenching mode. The complexes efficiently cleave pBR322 DNA via hydrolytic pathway, and significantly interact with epidermal growth factor receptor. All the complexes were assessed for their anti‐proliferative activity, in which the complexes 2, 3 and 4 containing methyl, methoxy and hydroxyl groups, respectively, showed significant activity. The complexes induce apoptosis in EAC cells as evidenced by acridine orange (AO)/ethidium bromide (EB), Hoechst 33258 and propidium iodide (PI) staining methods, and cell cycle analysis. Cellular uptake studies revealed the ability of the complexes to go into the cytoplasm and accumulation in the cell nuclei. The complexes are involved in the generation of reactive oxygen species (ROS), mitochondrial mediated and caspase‐dependent apoptosis. Further, using a female Swiss albino mice model, we found that the complexes 2 and 3 inhibited Ehrlich ascites carcinoma (EAC) tumour cell growth in vivo.

A series of six new bis(thiosemicarbazone)copper(I) complexes of the type [Cu(L1–6)2Cl] (1–6) have been synthesized and characterized. The molecular structure of the ligand L4 was determined by the single crystal XRD method. All the complexes adopted trigonal planar (Y-shaped) geometry. All the complexes strongly bind with CT-DNA via intercalative mode, which was further supported by molecular docking studies. Further, the complexes were effectively bind with BSA as observed by UV-Vis and fluorescence spectra. All the complexes effectively cleave pBR322 DNA through hydrolytic pathway as evidenced from T4 ligase experiments. All the complexes interact with the anticancer receptor focal adhesion kinase (FAK) via electrostatic, van der Waals, hydrogen bonding, σ–π and π–π interactions. In vitro cytotoxicity of the complexes were assessed by MTT assay against four cancer cell lines such as human breast adenocarcinoma (MCF-7), cervical (HeLa), epithelioma (Hep-2) and Ehrlich ascites carcinoma (EAC), and two normal cell lines namely normal human dermal fibroblasts (NHDF) and L6 myotubes with respect to the commercially used anticancer drug cisplatin. All the complexes induce apoptosis in EAC cells, which was confirmed by AO/EB, Hoechst 33258 and PI staining methods. The complexes block cell cycle progression of EAC cells in S phase (DNA synthesis). The cellular uptake studies confirmed the ability of the complexes to go into the cytoplasm and accumulation in the cell nuclei. In the in vivo anticancer studies, the complexes significantly reduce the tumour volume in female Swiss albino mice. Overall, our results ensure the role of thiosemicarbazone-based copper(I) complexes as prospective anticancer agents, induction of apoptosis and S phase arrest with the mitochondrial controlled pathway.

A series of heteroleptic silver(I) complexes of the type [Ag(L1 − 3)(nap)] (1–3), where L1–3 = 4′-(4-substituted)-2,2′:6′,2″-terpyridines and nap = naproxen have been synthesized and characterized by elemental analysis and spectroscopic methods. The geometric parameters of the complexes were determined using UV–Vis and DFT calculations together with the IR spectral data. All the complexes adopted distorted tetrahedral geometry around silver(I) ion. The small HOMO-LUMO energy gap supports the bioefficacy of the complexes. DNA binding and melting experiments suggest the intercalative binding mode of the complexes to CT–DNA, which was further supported by molecular docking studies. The molecular docking studies of the heteroleptic silver(I) complexes with EGFR/VEGFR2 kinase receptors show hydrophobic, π-π, σ-π and hydrogen bonding interactions. All the complexes have been found to promote DNA cleavage through hydrolytic pathway. In vitro cytotoxicity activity of the complexes was tested against four human breast adenocarcinoma (MCF-7), cervical (HeLa), epithelioma (Hep-2) and hepatoma (HepG2) cancerous, and one normal human dermal fibroblasts (NHDF) cell lines by MTT reduction assay. The morphological study by Hoechst 33258 staining revealed that the complex 3 induces apoptosis much more effectively than the other complexes. Further, all the complexes increases the DNA synthesis in S phase with the corresponding reduction in G0–G1 and G2/M phase, which suggest the growth inhibition mechanism on HepG2 cells was DNA damage mediated S phase arrest.

Four new heteroleptic silver(I) complexes with the general formula [Ag(L1–4)(nap)] (1–4), where L1–4 = 2-(1-(4-substitutedphenyl)ethylidene)hydrazinecarbothioamide and nap = naproxen, have been synthesized and characterized. The geometric parameters determined from density functional theory and UV-Vis studies indicate distorted tetrahedral geometry around silver(I) ion. Fourier transform infrared (FT IR) spectra evidenced asymmetric bidentate coordination mode of carboxyl oxygen atoms of naproxen with silver(I) ion. The complexes are stable for 72 h and biocompatibility was analysed towards normal human dermal fibroblast cells, which showed non-toxic nature up to 100 ng/ml. In vitro anti-proliferative activity of the complexes by MTT assay was tested against three human cancerous cell lines and one non-tumorigenic human breast epithelial cell line (MCF-10a) in which the complex 4 exhibited enhanced activity. The morphological changes observed by acridine orange/ethidium bromide and Hoechst 33258 staining method reveal apoptosis-inducing ability of the complexes. The molecular docking studies suggest hydrogen bonding, hydrophobic and π-pair interactions with the active site of epidermal growth factor receptor, vascular endothelial growth factor receptor 2 and lipoxygenase receptors.

Eight heteroleptic nickel(II) and copper(II) complexes of the type [M(L

Indigofera cordifolia Roth. (Fabales: Fabaceae) has been widely used in Indian system of medicine to treat various disorders. Earlier studies showed that I. cordifolia (EIC) possess antioxidant, free radical scavenging and antitumour activities. The present investigation was designed to evaluate the anticarcinogenic potential of EIC against diethylnitrosamine (DEN) induced hepatocellular carcinoma in male Wistar rats. Hepatocarcinogenesis was induced by a single intraperitoneal administration of DEN (200 mg/kg) and the carcinogenic effect was promoted by phenobarbital given through drinking water for 16 successive weeks. EIC at the dose of 200 and 400 mg/kg/day were administered orally for the entire study period. After the end of experimental period, changes in body weight, the weight of liver, relative liver weight, lipid peroxidation, antioxidant, serum hepatic parameters, tumour markers, DNA, RNA and protein content were analysed. Treatment with EIC significantly increased the body weight (P < 0.01-0.001), reduced the liver weight and relative liver weight (P < 0.01-0.001), restored the altered serum hepatic parameters (P < 0.001), down-regulated the serum tumour markers such as alpha-fetoprotein and carcinoembryonic antigen (P < 0.001) when compared to DEN group. EIC treatment restored the antioxidant enzymes and significantly reduced the lipid peroxidation in DEN-treated animals (P < 0.001). EIC treatment also significantly reduced the elevated levels of nucleic acid levels and restored the protein content in liver tissues (P < 0.001). We investigated the anticarcinogenic potential of EIC against DEN-induced HCC in rats. Chemoprotective effect of the extract might be related with antioxidant, free radical scavenging and reduction of lipid peroxidation. The results suggested that EIC would be a potent anticarcinogenic agent inhibiting DEN-induced hepatic carcinoma.

Indigofera linnaei Ali., has been widely used in folk medicine to treat inflammation, liver disorders and swelling of stomach. Earlier studies showed that methanolic extract of Indigofera linnaei (MEIL) possess antioxidant, free radical scavenging, antitumour, anti-inflammatory and analgesic activities but its effect on chemoprevention on chemical induced carcinogenesis have not been studied. Hence the present study is aimed to investigate chemopreventive efficacy of MEIL against diethylnitrosamine (DEN) induced phenobarbital promoted rat liver carcinoma model. Liver tumour was induced in rats by intraperitoneal administration of DEN (200 mg/kg). After two weeks, the carcinogenic effect was promoted by phenobarbital given through drinking water for 16 successive weeks. MEIL (200 and 400 mg/kg/day) and silymarin (200 mg/kg/day) were administered orally for entire study period. After the experimental period, changes in body weight, liver weight, relative liver weight, tumour incidence, antioxidant, serum hepatic parameters, serum specific tumour markers, nucleic acid and protein content were analysed. MEIL treatment significantly increased the body weight, reduced the liver weight and tumour incidence, restored the altered serum hepatic parameters, down-regulated the serum tumour markers such as alpha fetoprotein, carcinoembryonic antigen, vasculoendothelial growth factor and tumor necrosis factor-α. In addition, treatment with MEIL restored the antioxidant enzyme pool and significantly reduced the lipid peroxidation in carcinogen treated animals. MEIL treatment also reduced the elevated levels of nucleic acid levels and restored the protein content in liver tissues. The results suggested that MEIL would be a potent chemopreventive agent inhibiting chemically induced hepatic cancer.

A series of six new bis(thiosemicarbazone)copper(i) complexes of the type [Cu(L

A series of heteroleptic copper(II) complexes of the type [Cu(L1–6)(nap)Cl] (1–6) (L1–6 = 4′-(4-substituted)-2,2′:6′,2′′-terpyridines, nap = naproxen) has been synthesized and characterized. The single crystal analyses of complexes 1 and 6 show distorted octahedral geometry around the copper(II) ion. Structural parameters from the crystallographic and DFT studies are in good agreement with each other. HOMO–LUMO energy levels are constructed and the corresponding theoretical frontier energy gaps are calculated to understand the charge transfer occurring in the molecule, and the lowering of the HOMO–LUMO band gap supports the bioactive properties of the molecule. Electrochemical studies show a one-electron irreversible reduction process in the cathodic potential (Epc) region from −0.75 to −0.82 V. The obtained room-temperature magnetic moment values (1.82–1.93 BM), XRD and EPR spectral data support a distorted octahedral geometry for the copper(II) complexes. The binding studies of complexes 1, 5 and 6 with CT-DNA imply a groove mode of binding, and complex 5 exhibits a higher binding affinity than the other complexes. The binding results are further supported by molecular docking studies. The higher binding propensity of complex 5, containing R5, was proved by computationally derived factors such as chemical potential (μ), chemical hardness (η), electrophilicity (ω) and nuclease-independent chemical shift (NICS). All the complexes display pronounced nuclease activity against supercoiled pBR322 DNA. The in vitro antiproliferative activity of complexes 1, 5 and 6 against human breast cancer cells (MCF-7) was assessed by MTT assay, which shows the potency of 1 and 5, with lower IC50 values than cisplatin and values comparable to doxorubicin. The complexes induce mitochondrial-mediated and caspase-dependent apoptosis with an increase in G0–G1 and subsequent arrest in the S phase in cell cycle evaluation.

The bis(4′-(4-tolyl)-2,2′:6′,2″-terpyridine)copper(II) complex [Cu(ttpy)2]Cl2 was synthesized and authenticated by single crystal analysis, which shows distorted octahedral geometry around copper(II) ion. The crystal packing is stabilized by C–H···π inter and intramolecular interactions. The complex was found to be lipophilic as determined by shake-flask method. In vitro cytotoxicity of the complex was tested against Ehrlich ascites carcinoma (EAC) and L6 myotube cell lines. The complex exhibit potent cytotoxicity with respect to the commercially available anticancer drug cisplatin. Hoechst 33258, AO/EB and PI (flow cytometry) staining methods suggest that the complex can induce apoptosis in EAC cells. Cell cycle analyses also support the induced apoptosis. Cellular uptake studies revealed that the complex can go into the cytoplasm and accumulate in the cell nuclei. The complex induces EAC cell apoptosis through a ROS-mediated mitochondrial pathway by activating caspase 3 and caspase 7 and regulates the Bcl-2 family proteins. In vivo study of the complex was validated against the animal tumor growth (EAC) cell in Swiss albino mice. The bis(4′-(4-tolyl)-2,2′:6′,2″-terpyridine)copper(II) complex induces EAC cell apoptosis through a ROS-mediated mitochondrial pathway and significantly reduced the body weight and solid tumor volume in Swiss albino mice.

New gold(III) complex, [AuL2]Cl3 was synthesized from (2-(4-morpholinobenzylidene)-1-(4-(trifluoromethyl)pyrimidin-2-yl)hydrazine) and characterized by analytical and miscellaneous spectral methods. These results show that Au(III) complex has square planar geometry. Density functional theory (DFT) calculations have been done to understand the electronic structure of the Au(III) complexand free ligand while time dependent density functional theory (TDDFT) calculations have been employed to compute absorption spectra of ligand and Au(III) complex. Antimicrobial results suggest that ligand and complex have been inhibited the E. coli bacteria (13 mm) and C. albicans fungi (16 mm) than other microbes. Antioxidant results exhibit the ligand and complex has enhanced scavenging activities against several free radicals. In vitro anticancer activities of cisplatin, ligand and complex have been explored by MTT assay against various human cancer cell lines (breast-MCF-7, liver-HepG2, cervical-HeLa, lung-A549) and one normal cell line (NHDF- normal human dermal fibroblasts). The results show that complex has low IC50 values against cancer cell lines (20.6 ± 0.98 μg/mL, MCF-7; 22.68 ± 1.13 μg/mL, HepG2; 32.00 ± 1.60 μg/mL, HeLa; 33.19 ± 1.66 μg/mL, A549) than ligand. Moreover, complex has ten times least toxic activity (109.65 ± 5.48 μg/mL) on NHDF cell line as compared to cisplatin (10.28 ± 0.51 μg/mL). Based on the least toxic activity of complex has been further discovered by in vivo anticancer study using Ehrlich Ascites Carcinoma (EAC) tumor bearing Swiss albino mice. DNA interactions of ligand and complex have been studied by electronic absorption, fluorescence, viscometric and cyclic voltammetic methods. The results suggest that ligand and complex binds with CT-DNA through an intercalative interaction. Further confirm the nature of interaction between ligand and Au(III) complex towards DNA and BSA protein, molecular docking analysis has been carried out. These results reveal that Au(III) complex shows greater binding ability towards DNA and BSA than the ligand.

Indigofera linnaei Ali. (Tamil Name: Cheppu Nerinjil) belongs to the family Fabaceae, used for the treatment of various ailments in the traditional system of medicine. In the present study, the beneficial effects of methanol extract of whole plant of I. linnaei (MEIL) were evaluated on inflammation and nociception responses in rodent models. In vitro nitric oxide (NO), lipoxygenase (LOX) and cyclooxygense (COX) inhibitory activities were also performed to understand the mode of action. MEIL at the dose of 200 & 400 mg/kg, p.o. significantly inhibited carrageenan induced rat paw volume and reduced the weight of granuloma in cotton pellet granuloma model. The results obtained were comparable with the standard drug aceclofenac. The anti-nociceptive effect of MEIL in mice was evaluated in hot plate and acetic acid induced writhing model. The plant extract significantly reduced the number of writhes and the analgesic effect was higher than that of the standard drug aspirin. However, the extract fails to increase the latency period in hot plate method suggesting that the extract produce nociception by peripheral activity. The extract produced inhibitory effect on NO, LOX and COX in concentration dependent manner. The extract exhibited pronounced and selective COX-2 inhibition. Altogether, these results suggested that the methanol extract of Indigofera linnaei could be considered as a potential anti-inflammatory and analgesic agent. RESUMO Indigofera linnaei Ali pertence à família Leguminosae e é utilizada para o tratamento de várias doenças na medicina tradicional. No presente estudo, os efeitos benéficos do extrato metanólico da planta inteira de I. linnaei (MEIL) foram avaliados em respostas inflamatórias e nocicepção em modelos de roedores. Testes in vitro de atividade inibitória do óxido nítrico (NO), lipoxigenase (LOX) e ciclooxigenase (COX) também foram realizados para compreender o modo de ação. MEIL nas doses de 200 e 400 mg/kg, p.o. inibiu significativamente o volume da pata de rato induzido por carragenana e reduziu o peso do granuloma no modelo de pélete de algodão. Os resultados obtidos foram comparáveis ao do fármaco padrão, aceclofenaco. O efeito anti-nociceptivo de MEIL foi avaliado em camundongos no modelo de placa quente e de contorção induzida por ácido acético. O extrato da planta reduziu significativamente o número de contorções e o efeito analgésico foi maior do que o do fármaco padrão, ácido acetilsalicílico. Porém, o extrato não conseguiu aumentar o período de latência no método da placa quente, sugerindo que este produz nocicepção por atividade periférica. O extrato produziu efeito inibitório sobre o NO, LOX e COX dependente da concentração. O extrato exibiu inibição acentuada e seletiva da COX-2. No seu conjunto, estes resultados sugerem que o extrato metanólico de Indigofera linnaei poderia ser considerado como agente anti-inflamatório e analgésico potencial.

The antitumor activity of ethanol extract of Prosopis glandulosa Torr. (EPG) was evaluated against Ehrlich ascites carcinoma (EAC) tumor model in Swiss albino mice on dose dependent manner. The activity was assessed using survival time, average increase in body weight, hematological parameters and solid tumor volume. Oral administration of EPG at the dose of 100, 200 and 400 mg/Kg, significantly (p < 0.001) increased the survival time and decreased the average body weight of the tumor bearing mice. After 14 days of inoculation, EPG was able to reverse the changes in the hematological parameters, protein and PCV consequent to tumor inoculation. Oral administration of EPG was effective in reducing solid tumor mass development induced by EAC cells. The results indicate that EPG possess significant antitumor activity on dose dependent manner.

An in vitro antimicrobial activity and phytochemical analysis of various extracts of Indigofera trita L. viz. petroleum ether, chloroform, acetone, ethanol and aqueous extracts were carried out. A total of 21 microorganisms (19 bacteria and 2 fungal strains) were used for antimicrobial activity by disc diffusion method and a standard procedure was used to identify the phytochemical constituents. Petroleum ether extract showed moderate inhibitory activity against Staphylococcus aureus (14.40 mm), S. epidermidis (14.20 mm), Salmonella paratyphi A (12.80 mm), Streptococcus mutans (12.20 mm), Escherichia coli, Proteus vulgaris, S. typhi and Burkholderia cepacia (12.00 mm). The chloroform extract also showed antimicrobial activity against S. epidermidis (14.20 mm), S. typhimurium (12.60 mm), S. paratyphi A, S. brunei and Yersinia enterocolitica (12.00 mm). The acetone extract of I. trita showed considerable inhibitory activity against S. epidermidis (18.20 mm), S. typhimurium (14.60 mm), S. infantis (13.80 mm), S. aureus (13.40 mm), Y. enterocolitica (13.00 mm) and Enterobacter aerogenes (12.00 mm) were documented. Ethanol extract showed significant antimicrobial activity against S. epidermidis (18.60 mm), S. paratyphi A (14.60 mm), Y. enterocolitica (13.40 mm), S. typhi (12.40 mm), S. aureus, E. aerogenes, S. typhimurium and S. infantis (12.00 mm). Aqueous extract of I. trita considerably inhibited S. epidermidis (13.80 mm), S. paratyphi A and Y. enterocolitica (12.20 mm), E. aerogenes and Haemophilus parahaemolyticus (12.00 mm). All the five extracts showed a minimal antifungal activity when compared to antibacterial activity. The result revealed that the antimicrobial properties of I. trita might be associated with the presence of phenolic compounds, flavonoids, tannins, glycosides, saponins, phytosterols and alkaloids.

An in vitro antimicrobial activity and phytochemical analysis of various extracts of Indigofera trita L. viz. petroleum ether, chloroform, acetone, ethanol and aqueous extracts were carried out. A total of 21 microorganisms (19 bacteria and 2 fungal strains) were used for antimicrobial activity by disc diffusion method and a standard procedure was used to identify the phytochemical constituents. Petroleum ether extract showed moderate inhibitory activity against Staphylococcus aureus (14.40 mm), S. epidermidis (14.20 mm), Salmonella paratyphi A (12.80 mm), Streptococcus mutans (12.20 mm), Escherichia coli, Proteus vulgaris, S. typhi and Burkholderia cepacia (12.00 mm). The chloroform extract also showed antimicrobial activity against S. epidermidis (14.20 mm), S. typhimurium (12.60 mm), S. paratyphi A, S. brunei and Yersinia enterocolitica (12.00 mm). The acetone extract of I. trita showed considerable inhibitory activity against S. epidermidis (18.20 mm), S. typhimurium (14.60 mm), S. infantis (13.80 mm), S. aureus (13.40 mm), Y. enterocolitica (13.00 mm) and Enterobacter aerogenes (12.00 mm) were documented. Ethanol extract showed significant antimicrobial activity against S. epidermidis (18.60 mm), S. paratyphi A (14.60 mm), Y. enterocolitica (13.40 mm), S. typhi (12.40 mm), S. aureus, E. aerogenes, S. typhimurium and S. infantis (12.00 mm). Aqueous extract of I. trita considerably inhibited S. epidermidis (13.80 mm), S. paratyphi A and Y. enterocolitica (12.20 mm), E.aerogenes and Haemophilus parahaemolyticus (12.00 mm). All the five extracts showed a minimal antifungal activity when compared to antibacterial activity. The result revealed that the antimicrobial properties of I. trita might be associated with the presence of phenolic compounds, flavonoids, tannins, glycosides, saponins, phytosterols and alkaloids. Key words : Inidigofera trita, Phytoconstituents, Antimicrobial activity, Antifungal activity, Disc diffusion method.

Hepatoprotective activity of ethanolic extract of flowers of Vitex trifolia (Verbenaceae) was studied against CCl4 induced hepatic injury in albino rats. The plant extract (EVT) at the dose of 200 mg/kg, p.o. showed a remarkable hepatoprotective activity. CCl4 induced a significant rise in serum glutamate pyruvate transaminase (SGPT), serum glutamate oxaloacetate transaminase (SGOT), alkaline phosphatase (ALP), total bilirubin and gamma glutamate transpeptidase (GGTP). Treatment of rats with EVT significantly (P0.001) altered serum biomarker enzyme levels to near normal against CCl4 treated rats. The activity of the extract was comparable to the standard drug, silymarin (100 mg/kg, p.o.). Histopathological observations also revealed that treatment with EVT protected the animals from CCl4 induced liver damage. The results indicate that the flowers of V. trifolia possess hepatoprotective activity on CCl4 induced hepatic injury in rats.

Ethanol extract of Pisonia aculeata (EPA) was evaluated for hepatoprotective and antioxidant activities in rats. The plant extract (250 and 500 mg/kg, p.o.) showed a remarkable hepatoprotective and antioxidant activity against carbon tetrachloride (CCl4)-induced hepatotoxicity as judged from the serum marker enzymes and antioxidant levels in liver tissues. CCl4-induced a significant rise in aspartate amino transferase (AST), alanine amino transferase (ALT), alkaline phosphatase (ALP), total bilirubin, gamma glutamate transpeptidase (GGTP), lipid peroxidase (LPO) with a reduction of total protein, superoxide dismutase (SOD), catalase, glutathione peroxidase (GPx) and glutathione S-transferase (GST). Treatment of rats with different doses of plant extract (250 and 500 mg/kg) significantly (P&lt, 0.001) altered serum marker enzymes and antioxidant levels to near normal against CCl4-treated rats. The activity of the extract at dose of 500 mg/kg was comparable to the standard drug, silymarin (50 mg/kg, p.o.). Histopathological changes of liver sample were compared with respective control. Results indicate the hepatoprotective and antioxidant properties of P. aculeata against CCl4-induced hepatotoxicity in rats.

The unique properties such as high single cell working potential, energy density, long cycle life, etc., have identified secondary Li–ion batteries as the ultimate power source for portable electronic devices such as laptop computers, cellular phones, digital cameras, etc. However, their possible widespread penetration into the large-scale hybrid electric vehicle (HEV) and plug-in HEV markets can be realized only when substantial improvements such as low cost, sustainability, safety, high rate capability and long calendar life are achieved. The advancement in lithium battery technology relies mainly upon replacement of the conventional liquid electrolyte by an advanced solid polymer electrolyte. In order to achieve this goal, many lithium-conducting polymeric networks have been prepared and characterized. Among the polymer hosts explored so far, poly(ethylene oxide) - PEO has been indeed the most extensively studied system [1]. Unfortunately, solid polymer electrolytes comprising a polymer host and a lithium salt (e.g., PEO + LiClO4) exhibit low ionic conductivity at ambient and sub-ambient temperatures. Numerous attempts have been made to enhance the ionic conductivity of PEO-based electrolytes; one of the most common ways is the addition of low molecular weight liquid plasticizers like ethylene carbonate, propylene carbonate, etc. The addition of plasticizers, despite ameliorating the ionic conductivity, it adversely deteriorates the mechanical integrity and safety; moreover, side reactions with lithium metal eventually occur. Recently, new interesting structures have been described in the literature as metal organic frameworks (MOFs) [2]. Generally speaking, they are microporous solids consisting of an infinite network of metal centres (or inorganic clusters) bridged by simple organic linkers through metal–ligand coordination bonds. MOFs are widely used in catalysis, sensors, ion exchange, gas storage, purification, separation and sequestration; they are also used in optoelectronics to improve both electronic and proton conductivity. Nevertheless, to the best of our knowledge, so far no attempt has been made on the development of PEO-based composite polymer electrolytes (CPEs) encompassing an ad hoc synthesized Al-BTC (aluminium benzenetricarboxylate, see Fig. 1) MOF and a proper lithium salt showing an enhanced ionic conductivity of more than two order of magnitude at low temperature and excellent stability towards lithium metal even after a prolonged storage time. The obtained metal organic frameworks and macromolecular composite networks are thoroughly characterized from the structural, morphological and physico-chemical viewpoint of and, for the first time, an excellent long-term electrochemical behaviour in a lab-scale LiFePO4/CPE/Li cell is demonstrated (noteworthy stable even at low 50 °C), thus accounting for the development of high performing, safe all-solid-state lithium batteries. Even though lots of literature data are available on ceramic based fillers, the studies based on MOF encompassed polymer electrolytes are truly interesting due to its tailor-making capability and the broad spectrum of opportunities and possibilities it can bring. If very well-tuned, the MOF based fillers will be a true promising candidate and a vital ingredient which can enforce the intrusion of polymer electrolytes into the huge market of lithium-based batteries. [1] E. Quartarone, P. Mustarelli, Chem. Soc. Rev., 2011, 40, 2525. [2] M. Eddaoudi, H. Li, O.M. Yaghi, J. Am. Chem. Soc., 2000, 122, 1391

ObjectiveTo evaluate the antitumor, cytotoxic and antioxidant activities of methanolic leaf extract of Indigofera cassioides (MEIC) against transplantable tumors and human cancer cell lines.MethodsMEIC was investigated for its short term cytotoxicity on EAC and DLA cells by trypan blue dye exclusion method and in vitro cytotoxicity on HeLa, HEp-2, HEpG-2, MCF-7, HT-29, Vero and NIH 3T3 cells by MTT assay. In vivo antitumor activity was studied on EAC and DLA tumor bearing mice. Activity was assessed by monitoring the mean survival time, effect on hematological parameters, antioxidant enzyme levels and solid tumor volume.ResultsMEIC exhibit potent in vitro cytotoxicity against all the tested cancer cell lines, but it was found to be safe on normal cells. The extract significantly (P < 0.001) increase the mean survival time and also have a protective effect on the hemopoietic system at the tested dose levels (200 and 400 mg/kg). The extract prevented lipid peroxidation and restored the antioxidant enzymes catalase, superoxide dismutase, glutathione peroxidase and glutathione-s-transferase in the liver of tumor control animals. It also significantly (P < 0.01) reduce the solid tumor volume.ConclusionsThe results strongly support that MEIC shows potent antitumor and cytotoxic effects against EAC, DLA and human cancer cell lines. The extract prevents lipid peroxidation and promotes the enzymatic antioxidant defense system in tumor bearing animals which might be due to activities like scavenging of free radicals by the phytochemicals in MEIC.