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The present work was carried out to the chracterization and the evaluation of antimicrobial and anti-oxidant activity of Vn-ZnO NPs. The present research work focussed on the biosynthesized ZnO NPs by sodium hydroxide, zinc acetate and bio components of leaves of Vitex negundo in the reaction mixture was monitored in the precipitate from, which proved the formation of ZnO NPs. The biosynthesized nanoparticles were characterized by advanced tool viz. UV-Vis spectrophtometer, FT-IR, Particle size and zeta potential, X-ray diffraction and TEM along with EDAX. The UV-Vis peak was aquiered at 375nm. The zeta average 28 nm and the zeta potential value was -16.3mV.The average size of the nanoparticles was 34.46 nm and the minimum sized NPs read 16.2 nm by HR-TEM. Antibacterial activity of Vn-ZnO NPs was evaluated by examine against selected two gram negative (Escherichia coli, Salmonella typhi) and gram positive bacteria (Bacillus subtilis, Staphylococcus aureus). Antimicrobial activity of Vn-ZnO NPs was found to be more suceptable to the against gram negative bacteria. Strong DPPH activity was found by the Vn-ZnO NPs.

In the present investigation, we report simple, robust and eco-friendly synthesis of silver nanoparticles (AgNPs) using leaf extract of Flemingia wightiana. The leaf extract of F. wightiana acts as reducing agent which reduces the silver ions into FW-AgNPs, as well as stabilizing agent by capping around them. Biosynthesized FW-AgNPs were characterized by different spectroscopic techniques. UV–Vis spectrum showed the characteristic SPR peak between 380 and 460 nm. EDX analysis revealed the presence of metallic silver at 3 keV. XRD analysis clearly revealed that FW-AgNPs are crystalline in nature with FCC structure. TEM analysis depicted the spherical morphology with 20–40 nm in size. DLS analysis showed that average hydrodynamic size and PDI value of FW-AgNPs were found to be 47.6 nm and 4.5 respectively. Biosynthesized FW-AgNPs showed high negative zeta potential value of − 25.3 mV. FTIR analysis revealed the participation of polyphenols and proteins in the bioreduction and stabilization of FW-AgNPs. FW-AgNPs showed strong DPPH and H2O2 scavenging activity with IC50 values of 71.96 and 80.59 µg/mL respectively. Further FW-AgNPs also showed effective cytotoxicity against cancer cells including SKOV3 and COLO205 with maximum inhibition of 83.2% and 75.9% respectively.

The endophytic fungi Fusarium equseti was isolated from the healthy tissues of Terminalia pallida and the EtOAc extracts of the culture was subjected to primary antimicrobial screening against two fungal cultures, along with anticancer activity in breast cancer cell lines. As a result, potential extracts exhibiting anticancer and antimicrobial activity among them, were selected for further investigation and identification of active metabolites. Bioassay-guided fraction of the EtOAc extract of liquid culture were identified as (E)-3- (2,3- dihydroxy phenyl) acrylic acid by mass and spectral means (MS, IR NMR). In vitro anticancer and antimicrobial assay showed that compound was substantially active against Candida tropicalis and Candida albicans and breast cancer cell lines evident from MTT (3-(4, 5-Dimethylthiazol-2-yl)-2,5-DiphenyltetrazoliumBromide) assay.

In the present investigation, here we first report the phytosynthesis of silver nanoparticles (AgNPs) using shade dried aqueous leaf extract of Rhynchosia heynei Wight & Arn is a crop wild relatives (CWR) of pigeon peas (Cajanus), beans (Phaseolus) and grams (Vigna). R. heynei is a rare, an endemic and vulnerable category as an according to the IUCN Red list of threatened species (ver.2012.2), a global database of Plant species to track at risk species, it is herbaceous under shrub, an important, indigenous, threatened forestry species of traditional shrub of tribal medicinal plant species belonging to family Fabacaea and it is classified in Tribe phaceoleae and sub-tribe Cajaninae and subfamily papilionoideae and it is found in the forests of seshachalam biosphere reserve in Tirumala hills, Chittoor district, Rayalaseema region, Andhra Pradesh state, Eastern Ghats of India. The shade dried aqueous leaf extract of R. heynei acts as reducing and capping agent that mediates the synthesis and stabilization of RH-AgNPs (R. heynei leaf synthesized AgNPs). Phytosynthesized RH-AgNPs were 5–20 nm in size, face centered cubic crystalline in nature, spherical in shape, and possesses zeta potential value of −31.4 mV. UV-Vis spectroscopy analysis confirmed the formation of silver nanoparticles. FTIR analysis demonstrated that polyhydroxy compounds and proteins respectively involved the bioreduction and capping processes of the particles that prevents agglomeration which in turn gives stability. The stability of RH-AgNPs will be further confirmed through zeta potential measurement by dynamic light scattering (DLS) analysis technique. Both X-ray Diffraction (XRD) and SAED results emphasized that the phytosynthesized RH-AgNPs were crystal particles in nature. Particle size distribution showed that RH-AgNPs were 5–20 nm in size with hydrodynamic radius of 11.2 nm. In addition to silvernano particles energy -dispersive X-ray analysis (EDX) analysis of the RH-AgNPs showed the elemental composition of colloidal solution of RH-AgNPs. The EDX spectrum of RH-AgNPs exhibit strong signal of silver (Ag) element. The elemental composition of the colloidal solution of RH-AgNPs. Transmission electron microscope (TEM) micrographs showed that the RH-AgNPs formed were polydispersed in nature without agglomeration. Phytosynthesized RH-AgNPs exhibited excellent bactericidal activity against different human pathogens including Klebsiella pneumoniae, Escherichia coli (Gram-ve), Bacillus subtilis and Staphylococcus aureus (Gram +ve). RH-AgNPs exhibited effective antioxidant property by scavenging DPPH and H2O2 radicals with the IC50 values of 77.7 and 88.6 µg/mL respectively. Further RH-AgNPs exhibited dose-dependent anticancer activity with maximum inhibition of 85% and 72% respectively against different cancer cell lines of human colon carcinoma (COLO205) and lung adenocarcinoma (A549). Application of silver nanoparticles (AgNPs) have revolutionized the medicinal industry. Due to their distinctive properties small size (1–100 nm), shape and electrical properties these nanoparticles are able to cross cell and nuclear membrane and induce cyto/genotoxicity. Phytosynthesized (plant based) AgNPs have targeting biological pathways has become tremendously prominent due to the higher efficiency and fewer side effects as compared to other commercial cancer drugs and have emerged as alternative antimicrobial agent to chemically synthesiszed nanoparticles assume their methods of synthesis is a simple, rapid and single-step bioreduction method which is environment friendly and non toxic and cost effective.

Treatment of obesity and its associated immune mediated diseases is challenging due to impaired function of leptin system. Thus leptin is providing an interesting target for therapeutic intervention. Leptin, an adipose tissue-derived adipokine, displays a variety of immune functions, and regulate both innate and adaptive immune responses. The increased secretion of leptin (hyperleptinemia) and production of proinflammatory cytokines has been implicated in the pathogenesis of obesity-related immune diseases such as diabetes mellitus, hypertension, atherosclerosis, cancer, systemic lupus erythematosus, rheumatoid arthritis, crohn's disease and multiple sclerosis. These disorders are managed through antibiotics and by cytokines replacement. However, the effectiveness of cytokines coupled to the complexity of the cytokine network leads to severe side-effects, which can still occur after careful preclinical evaluation. In addition, synthetic immunotherapeutics carries a degree of risk, is time-consuming and expensive. Hence, the complexity of existing therapy and adverse effects emphasizes the need of an alternative approach for the management of immune dysfunction associated with obesity and its related diseases. For the aforementioned diseases that are related to leptin overabundance, new drugs blocking leptin signaling need to be generated. The research on the discovery of clinically important novel compounds from natural source is expanding due to their safety and no side effect. The fungal endophytes are the microbes that colonize internal tissue of plants without causing negative effects to the host. They produce plethora of substances of potential use to modern medicinal and pharmaceutical industry. The increasing body of evidence associated with application of bioactive metabolites derived from fungal endophytes in diverse disease states merits its use as therapeutic drugs. In particular, the saponins have been extensively proved to modulate the immune system, which has raised a significant interest in their potential as immunomodulators. Thus, our hypothesis is that the saponins derived from fungal endophytes can be explored as clinical applicable leptin inhibitors for treating immune mediated diseases.

A new class of antimicrobial and antioxidant agents, based on thiourea and urea derivatives of 6-fluoro-3-(piperidin-4-yl)benzo[d] isoxazole were synthesized by adopting a simple and efficient method. Synthesized compounds were characterized by spectral data of IR, 1H, 13C NMR and mass spectra. The compounds were evaluated for their efficacy as antimicrobial and antioxidant agents. A few compounds showed good antibacterial, antifungal and antioxidant activity when compared to standard drugs and thus represent a new class of promising lead compounds.

A new class of methylthio linked pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles were prepared under conventional and ultrasound irradiation methods. All the compounds were obtained in higher yields and in shorter reaction times in ultrasound irradiation method when compared with the conventional method. The title compounds were tested for antimicrobial activity. The compounds 12c and 12f exhibited promising antibacterial activity against P. aeruginosa whereas the compounds 13c and 13f showed pronounced antifungal activity against A. niger.

A variety of bis heterocycles-heteroaryl pyrazoles (5) and pyrroles (6) were prepared from heteroaryl chalcones adopting 1,3-dipolar cycloaddition reaction and studied their antimicrobial activity. The compounds 5d and 5f having bromo and nitro substituents on the aromatic ring are the potent antimicrobial agents against Bacillus subtilis and Aspergillus niger.

A variety of bis heterocycles, oxazolyl/thiazolyl/imidazolyl oxadiazoles having a styryl sulfonylmethyl group at the 5-position of oxadiazole and tris heterocycles having a pyrrolyl/pyrazolyl sulfonylmethyl group at the 5-position of oxadiazole were prepared adopting simple and versatile synthetic methodologies. All the compounds were screened for their antioxidant activities. Compound 5b displayed radical scavenging activity in all the three methods greater than the standard ascorbic acid, whereas compounds 8b and 14b showed activities equal to the standard ascorbic acid.

Synthesis of a series of novel phosphorylated ganciclovir derivatives with bioactive amines/aminoacid esters as substituents was accomplished. These compounds were structurally characterized by IR, NMR (1H, 13C, 31P), mass spectra and CHN analysis. The compounds (5a–m) have been evaluated for its in vitro and in vivo immunomodulatory activities. The amino acid ester-substituted ganciclovir derivatives, especially the 5g and 5i, increased the intracellular killing activity of the stimulated neutrophils. The in vivo experiment results show that the administration of compounds 5g and 5i (8 mg/kg body weight) to diet-induced immune impaired obese rats ameliorated the significant increase in immune cell counts (lymphocytes, neutrophils and monocytes). In addition, TNF-α, IL-6 and IL-1 secretions were considerably restored to normal by the compounds 5g and 5i with regulation in the release of C-reactive protein suggesting their potentiating effect on immune system dysfunction. These in vitro and in vivo results suggest that the phosphorylated ganciclovir derivatives 5g and 5i are strong immunomodulators.

This study investigates the endophytic fungal diversity of three endemic plants of Tirumala hills also their capabilities for the production of hydrolysing enzymes and secondary metabolites. Our study provides the first evidence on the diversity, enzyme and metabolite charecterisation of fungal endophytes from the untapped endemic plants of Tirumala Hills of Seshachalam Biosphere Reserve, Easternghats, Andhra Pradesh, India. A total of 13 endophytic fungi isolates were obtained and grouped into seven genera based on the morphological traits, indicating endophytic fungi in Shorea thumbuggaia, Boswellia ovalifoliolata, Pterocarpus santalinus were diverse and abundant. Fusarium, Penicillium, Aspergillus and Colletotrichum were the dominant genera, whereas the remaining genera were less frequent. The 13 representative species of the distinct genera were capable of producing hydrolysing enzymes. Phytochemical analysis showed the production of various secondary metabolites that included saponins, carbohydrates, phenolics, glycosides and flavonoids. This investigation also reveals that the metabolites produced by a variety of endophytic fungi can be a potential source of novel natural therapeutic agents.Keywords: Endemic plants, fungal endophytes, hydrolyzing enzymes, secondary metabolites, Tirumala Hills.African Journal of Biotechnology Vol. 12(27), pp. 4317-4323

Vasudeva Reddy Netala,1 Murali Satyanarayana Bethu,2,3 Bobbu Pushpalatha,1 Vijaya Bhaskar Baki,4 Sani Aishwarya,1 J Venkateswara Rao,2 Vijaya Tartte5 1Department of Biotechnology, Sri Venkateswara University, Tirupati, 2Biology Division, Indian Institute of Chemical Technology, Hyderabad, 3Academy of Scientific and Innovative Research, New Delhi, 4Department of Bioinformatics, 5Department of Botany, Sri Venkateswara University, Tirupati, India Abstract: An endophytic fungal strain isolated from the leaves of Gymnema sylvestre was identified as Pestalotiopsis microspora VJ1/VS1 based on nucleotide sequencing of internal transcribed spacer region (ITS 1-5.8S-ITS 2) of 18S rRNA gene (NCBI accession number KX213894). In this study, an efficient and ecofriendly approach has been reported for the synthesis of silver nanoparticles (AgNPs) using aqueous culture filtrate of P. microspora. Ultraviolet-visible analysis confirmed the synthesis of AgNPs by showing characteristic absorption peak at 435 nm. Fourier transform infrared spectroscopy analysis revealed the presence of phenolic compounds and proteins in the fungal filtrate, which are plausibly involved in the biosynthesis and capping of AgNPs. Transmission electron microscopy (TEM) showed that the AgNPs were spherical in shape of 2–10 nm in size. Selected area electron diffraction and X-ray diffraction studies determined the crystalline nature of AgNPs with face-centered cubic (FCC) lattice phase. Dynamic light scattering analysis showed that the biosynthesized AgNPs possess high negative zeta potential value of -35.7 mV. Biosynthesized AgNPs were proved to be potential antioxidants by showing effective radical scavenging activity against 2,2'-diphenyl-1-picrylhydrazyl and H2O2 radicals with IC50 values of 76.95±2.96 and 94.95±2.18 µg/mL, respectively. The biosynthesized AgNPs exhibited significant cytotoxic effects against B16F10 (mouse melanoma, IC50 =26.43±3.41 µg/mL), SKOV3 (human ovarian carcinoma, IC50 =16.24±2.48 µg/mL), A549 (human lung adenocarcinoma, IC50 =39.83±3.74 µg/mL), and PC3 (human prostate carcinoma, IC50 =27.71±2.89 µg/mL) cells. The biosynthesized AgNPs were found to be biocompatible toward normal cells (Chinese hamster ovary cell line, IC50 =438.53±4.2 µg/mL). Cytological observations on most susceptible SKOV3 cells revealed concentration-dependent apoptotic changes that include cell membrane blebbing, cell shrinkage, pyknotic nuclei, karyorrhexis followed by destructive fragmentation of nuclei. The results together in this study strongly provided a base for the development of potential and versatile biomedical applications of biosynthesized AgNPs in the near future. Keywords: AgNPs, Pestalotiopsis microspora, 18S rRNA, SKOV3, B16F10, AO-EB staining

A novel class of the title thiourea and urea derivatives are synthesized and evaluated for their antimicrobial and antioxidant activities.

A series of diethyl/ethylphenyl {2-(benzo[d]thiazol-2-yl)phenylamino}phosphonates and phosphinates were synthesized under microwave irradiation and neat conditions via Kabachnik-Fields reaction in high yields (80%–93%). The compounds were screened for antimicrobial and antioxidant properties. A few compounds showed effective antibacterial and antifungal activities at MIC value 12.5 μg/mL as compared with the standard at MIC value 6.25 μg/mL.

Kitchen waste water emerging from Tirumala hills, a world famous piligrim centre was used as a source of nutrients for cultivation of Nostoc muscorum. A complete randomized design (CRD) was created for the experiment which was performed on BG-11 medium, 100% kitchen waste water (100% KW) and 75% kitchen waste water (75% KW). The physicochemical properties of kitchen waste water and the yield of biomass were determined from the cultures harvested every three days for a period of 15 days. After cultivation the kitchen waste water met the standards of safe discharge in India. The organisms could able to remove maximum of 98% of contaminants during its growth in waste water. The highest production of biomass was achieved in BG-11 medium followed by 100% KW and 75% KW.

New 2-amino-N-hydroxybenzamide derivatives (3a–j) have been synthesized in good to excellent yields from the reaction of isatoic anhydride with different hydroxamic acids. All the compounds of the series were screened against both Gram-positive and Gram-negative bacteria and fungi, and some of them have antibacterial and antifungal activities compared to the standard drugs.

Aim: The aim of this study was to evaluate the heavy metal resistance potentiality of endophytic fungi isolated from the leaves of Boswellia ovalifoliolata,an endemic medicinal plant of Tirumala Hills.Methods: Initially, isolation of fungal endophytes was carried out. Isolated fungi were screened for the heavy metal resistance against Co, Cd, Cuand Zn using growth and evaluated their maximum tolerant capacity. Molecular identification of endophytic fungi was carried out by 18S rRNA geneamplification and Sanger’s nucleotide sequencing. Phylogenetic tree was constructed using NCBI Clustal W.Results: Ten different endophytic fungi were isolated from the leaves of B. ovalifoliolata. Among the isolated endophytic fungi, five showed resistanceto Co, Cd, Cu, and Zn. The most resistant fungus was identified as Lasiodiplodia theobromae based on 18S rRNA gene sequencing.Conclusions: L. theobromae was isolated from B. ovalifoliolata and identified as one of the useful fungi involved in mycoremediation against heavymetal toxicity.Keywords: Heavy metals, Endophytic fungi, Endemic plant, Bioremediation.

New compound (IIIa) displays radical scavenging activity in all the three tested methods greater than the standard ascorbic acid, and compounds (Va) and (VIIIa) show activities equal to the standard ascorbic acid.

We examined the antiobesity effect of a saponin-rich fraction of a Gymnema sylvestre R. Br. aqueous leaf extract (SGE) using cafeteria and high-fat diet-induced obese rats for a period of eight weeks. SGE was orally administered at a dose of 100 mg/kg body weight once a day to the treatment group. It significantly decreased the body weight, food consumption, visceral organs weight, and the levels of triglycerides, total cholesterol, low-density lipoproteins, very low-density lipoproteins, atherogenic index, glucose, and increased the levels of high-density lipoproteins. There was no significant difference with respect to all parameters of the study in case of normal (N) diet and N diet + SGE rats. In vitro, SGE inhibited the pancreatic lipase activity. The present study gave clear evidence that the SGE has a significant antiobese action, supporting its use in traditional medicine, and can be used as a substitute for synthetic drugs.

A new benzophenone, 2-hydroxy-3,4-dimethoxybenzophenone (1), together with a known C-glycosylxanthone, mangiferin (2) and two known C-glycosylflavones, isovitexin (3) and isoorientin (4), were isolated from the flowers of Rhynchosia suaveolens DC. (Fabaceae). The structure of the new compound (1) and the known compounds (2-4) were elucidated by extensive 1D and 2D NMR spectral studies. The plant extracts, as well as the isolated compounds, were evaluated for their total phenolic content (TPC), total flavonoid content (TFC) and DPPH radical scavenging activity. Among the isolated compounds, mangiferin (2) and isoorientin (4) showed significant radical scavenging activity comparable with that of ascorbic acid.