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Alteration in the pattern of epigenetic marking leads to cancer, neurological disorders, inflammatory problems etc. These changes are due to aberration in histone modification enzymes that function as readers, writers and erasers. Bromodomains (BDs) and BET proteins that recognize acetylation of chromatin regulate gene expression. To block the function of any of these BrDs and/or BET protein can be a controlling agent in disorders such as cancer. BrDs and BET proteins are now emerging as targets for new therapeutic development. Traditional drugs like enzyme inhibitors and protein–protein inhibitors have many limitations. Recently Proteolysis-Targeting Chimeras (PROTACs) have become an advanced tool in therapeutic intervention as they remove disease causing proteins. This review provides an overview of the development and mechanisms of PROTACs for BRD and BET protein regulation in cancer and advanced possibilities of genetic technologies in therapeutics.

In the present work, we have designed and synthesized two carbazole and phenothiazine donor moieties based metal-free organic sensitizers and their codes are WCBZ2 and WPTZ2 respectively. These sensitizers have been used for photocatalytic hydrogen (H2) evaluation application. The sensitizers exhibit good light absorption capability and electrochemical properties as well. For increasing water splitting capacity, incorporate platinum salt on TiO2 semiconductor photoanode was performed and compared hydrogen evolution with pure TiO2 photoanode. We have also studied the influence of the sensitizer's concentration and the effect of pH of the medium was explored. Using a theoretical measurement optimized both the synthesized dimer dyes structure geometry and the calculated their HOMO-LUMO energy level. Here also reported optimized pH and concentration of sensitizers in the reaction medium and found that the high hydrogen generation efficiency from water splitting is 138.3 μmol (348 TONs) by the WPTZ2 dye.

Calcium oxalate monohydrate (COM) crystals with various morphologies, such as elliptical, hexagonal, peanut-like, spherical and flower-like structures with a size of about 10 μm, were prepared through varying the reactant concentration, stirring speed, reaction temperature, and additive. X-ray diffraction and infrared spectroscopy showed that the synthesized crystals were pure-phase COM. The specific surface area and pore structure analysis demonstrated that all these COM crystals contained pores. Moreover, the zeta potential of each COM morphology was negative, and the value positively corresponded to the negative charge density of the crystal surface. Cell viability, lactate dehydrogenase (LDH) release, and reactive oxygen species (ROS) level assays suggested that these COM crystals caused injury to African green monkey renal epithelial (Vero) cells. Such an ability of the crystals to cause injury was correlated with the Ca2+ ion-rich (01) crystal plane area, crystal edge sharpness, zeta potential and crystal-specific surface area. Hence, the cytotoxicity of the COM crystals was closely related to their morphology and surface structure.

The bovine serum albumin nanoparticles (BSA-NPs) were prepared using desolvation process, in an aqueous medium with acetone as a desolvating agent. The BSA nanoparticles were found within 50 to 75 nm range confirmed by dynamic light scattering and scanning electron microscope. The interaction of prepared BSA-NPs with Cu2+ yielded Cu2+ conjugated BSA-NPs (Cu-BSA-NPs) analyzed by the same techniques. Both have been studied for their comparative thermal and dye adsorption analysis where the later was found 40% greater for Cu-BSA-NPs than BSA-NPs. Molecular modelling showed the methylene blue and methyl orange interactions into the active pocket of BSA with H-acceptor with ΔGb = −1.8 and −3.0 kcal/mol respectively. Similarly the Cu-BSA-NPs have shown better DNA binding and antioxidant activities as compared to BSA-NPs estimated through absorption spectra and free radical mechanism. Presence of metal ion has facilitated the BSA NPs for trapping the free radicals in its hydrophobic as well as hydrophilic domains. Both have also been tested in vitro against MCF (Breast cancer) cell line for their anticancer nature where Cu-BSA-NPs have been found more effective. Antimicrobial in vitro minimal inhibitory concentration (MIC) evaluation has been assessed on the basis of zone of inhibition with gram +ve and gram -ve bacteria B. cereus (MTCC430), S. aureus (MTCC 737), and E.coli (MTCC443), K. pneumonia (MTCC3384) respectively. The association of Cu2+ has impacted more in growth inhibition of bacteria.

Pluronics® and Tetronics® are used in industry for solubilizing various kinds of hydrophobic compounds since decades. In present study, moderately hydrophobic linear and star block copolymer viz. Pluronic® P104 and Tetronic® T1304 are employed for the solubilization of four polycyclic aromatic hydrocarbons (PAHs) viz. naphthalene (Np), anthracene (An), phenanthrene (Ph) and pyrene (Py). The aggregation behaviour of these block copolymers in an aqueous media has been investigated by cloud point (CP), viscometry, dynamic light scattering (DLS), and small angle neutron scattering (SANS) techniques. The aqueous solubilities of these PAHs are quite poor, hence their extractions from contaminated areas are difficult. Cloud point of block copolymers linearly decreases as a function of PAHs concentration and strongly depends on the structure of PAHs. The aqueous solutions of both block copolymers are Newtonian fluid. The solubilization of PAHs in these copolymeric micelles leads to increase in the viscosity of solution suggesting the growth of micelles. The effect of concentration and temperature on the size and shapes of micelles were evaluated from DLS and SANS studies. The study provides an alternative method for the remediation of PAHs using inexpensive commercially available block copolymers.

This work investigated the effect of Potassium Permanganate (KMnO4) on graphene oxide (GO) properties, especially on electrical properties. The GO thin films were deposited on a glass substrate using drop casting technique and were analysed by using various type of spectroscopy (e.g. Scanning Electron Microscopy (SEM), Ultra- Violet Visible (UV–VIS), Fourier Transform Infrared (FTIR), X-Ray Diffraction (XRD), optical band gap, Raman Spectroscopy). Furthermore, the electrical experiments were carried out by using current–voltage (I-V) characteristic. The GO thin film with 4.5 g of KMnO4 resulted in higher conductivity which is 3.11 × 10−4 S/cm while GO with 2.5 g and 3.5 g of KMnO4 achieve 2.47 × 10−9 S/cm and 1.07 × 10−7 S/cm, respectively. This further affects the morphological (SEM), optical (band gap, UV–Vis, FTIR, and Raman), and crystalline structural (XRD) properties of the GO thin films. The morphological, elemental, optical, and structural data confirmed that the properties of GO is affected by different amount of KMnO4 oxidizing agent, which revealed that GO can potentially be implemented for electrical and electronic devices.

The biomorphic carbide (Bio-C) with highly interconnected pore-joined carbon structure consisting of three dimensional alignments was prepared based on balsa wood, a non-hazardous herbal stuff, resulting an economic, environment-friendly fabrication process. The balsa wood gives hierarchical natural porous structure after the hydrothermal process, which offers ample enlargement area for MnO2 and eliminates the aggregation of MnO2 particles. Evolution of structure, morphology, and porous properties from pristine carbonized wood to porous Bio-C/MnO2 was systematically studied. The electrochemical performance of the Bio-C/MnO2 composite has been studied in a flexible symmetric supercapacitor (FSC) using PVA/H2SO4 hydrogel as an electrolyte. The as-prepared Bio-C/MnO2 composite demonstrated staggering electrochemical output, which is majorly resulted due to the large amount of pore volume along with 3D hierarchical pores. Electrochemical study showed that the Bio-C/MnO2 composites used in FSC had a specific capacitance (sp. cap.) of 148 F.g−1 at current density of 0.8 A.g−1, and exhibited stable long cycle life with a capacitance retention ratio of 78.77 % after 10000 cycles. The Bio-C/MnO2 hybrid materials having three dimensional porous structures are excellent materials in the wide area of bendable power storage system.

This review article provides an overview of the advances in the field of hydro-conversion of n-alkanes with particular stress on the promising ways to meet the requirements for improved quality of motor fuels and oils, which have been marked during the past decades. Particular attention is given to a catalyst formulation for conversion of n-alkanes to branched hydrocarbons. The particular challenge is to find an effective catalyst, which favors the isomerization of n-alkanes without too much cracking. The regulation of active sites and adsorption properties, as well as the topology of support surfaces, allows a potential predictive design of novel catalysts for conversion of n-alkanes into their branched isomers.

Present communication reports the community structure and distribution pattern of intertidal invertebrate macrofauna at four shores of the Kathiawar peninsular coastline off the Arabian Sea (India). The selected shores have different levels of human activities. Present report tests three hypotheses; that is, (i) distribution of invertebrate macrofauna in these shores is influenced by space and time, (ii) abiotic factors have a profound influence on the distribution pattern of intertidal macrofaunal assemblages, and (iii) human activities influence the community structure of the intertidal invertebrate macrofauna at these shores. To test these hypotheses, spatiotemporal variations in different ecological indices were studied. A total of 60 species from six phyla were considered for the study. High species diversity was recorded during winter and monsoon seasons in almost all the shores studied. It was also evident that a few environmental factors had a cumulative influence on the distribution pattern of intertidal macrofauna. Significant spatial variations in the species diversity and evenness were also observed. Though the shores studied have similar coast characteristics and climatic conditions, they face different levels of human activities. Therefore, the observed variations in the intertidal faunal assemblage were possibly caused by anthropogenic stress.

Herein, we report the cytotoxicity of cyclopentapeptide analogues of marine natural product galaxamide towards breast carcinoma cells and the underlying mechanisms. We examined the effect of the novel galaxamide analogues on cancer cell proliferation by MTT assay and also further examined the most active compound for morphological changes using Hoechst33342 staining technique, induction of apoptosis, cell cycle phases, mitochondrial membrane potential (MMP), and reactive oxygen species (ROS) generation using flow cytometry in human breast cancer MCF-7 cells in vitro. Galaxamide and its analogues effectively induced toxicity in human hepatocellular carcinoma HepG2, human breast carcinoma MCF-7, human epitheloid cervix carcinoma HeLa, and human breast carcinoma MB-MDA-231 cell lines. Amongst them, compound 3 exhibited excellent toxicity towards MCF-7 cells. This galaxamide analogue significantly induced apoptosis in a dose-dependent manner in MCF-7 cells involves cell cycle arrest in the G1 phase, a reduction of MMP, and a marked increase in generation of ROS. Particularly, compound 3 of galaxamide analogues might be a potential candidate for the treatment of breast cancer.

Marine bis-indole alkaloids comprise a large and increasingly growing class of secondary metabolites, and continue to deliver a great variety of structural templates for diverse biological targets. The alkaloids derived from marine resources play a crucial role in medicinal chemistry and as chemical agents. In particular, bis-indole alkaloid caulerpin which has been isolated from marine green algae Caulerpa and a red algae Chondria armata at various places around the world, was tested for several therapeutic potentials such as anti-diabetic, antinociceptive, anti-inflammatory, anti-tumor, anti- larvicidal, anti-herpes, anti-tubercular, anti-microbial and immunostimulating activities as well as a means of other chemical agents. Herein, we summarized the discovery and isolation of caulerpin, and its potential medicinal and chemical applications in chronological order with various aspects. Additionally, synthesis of caulerpin and its functional analogues have also been reviewed.

This study aimed to investigate the protective effects of degraded soybean polysaccharides (DSP) on oxidatively damaged African green monkey kidney epithelial (Vero) cells. Low DSP concentration (10 μg/mL) elicited an evident protective effect on H2O2-induced cell injury (0.3 mmol/L). The cell viabilities of the H2O2-treated group and the DSP-protected group were 57.3 and 93.1%, respectively. The cell viability decreased to 88.3% when the dosage was increased to 100 μg/mL. DSP protected Vero cells from H2O2-mediated oxidative damage by enhancing cellular superoxide dismutase activity and total antioxidant capacity and by decreasing malonaldehyde content and lactate dehydrogenase release. The H2O2-treated cells stimulated the aggregation of calcium oxalate monohydrate crystals. DSP could also reduce the crystal size, decrease the attached crystal content, and prevent the cell aggregation by alleviating oxidative injury and lipid peroxidation, enhancing antioxidant capacity, and decreasing hyaluronan expres...

Herein, we report design and synthesis of novel 26 galaxamide analogues with N-methylated cyclo-pentapeptide, and their in vitro anti-tumor activity towards the panel of human tumor cell line, such as, A549, A549/DPP, HepG2 and SMMC-7721 using MTT assay. We have also investigated the effect of galaxamide and its representative analogues on growth, cell-cycle phases, and induction of apoptosis in SMMC-7721 cells in vitro. Reckon with the significance of conformational space and N-Me aminoacid (aa) comprising this compound template, we designed the analogues with modification in N-Me-aa position, change in aa configuration from l to d aa and substitute one Leu-aa to d/l Phe-aa residue with respective to the parent structure. The efficient solid phase parallel synthesis approach is employed for the linear pentapeptide residue containing N-Me aa, followed by solution phase macrocyclisation to afford target cyclo pentapeptide compounds. In the present study, all galaxamide analogues exhibited growth inhibition in A549, A549/DPP, SMMC-7721 and HepG2 cell lines. Compounds 6, 18, and 22 exhibited interesting activities towards all cell line tested, while Compounds 1, 4, 15, and 22 showed strong activity towards SMMC-7221 cell line in the range of 1–2 μg/mL IC50. Flow cytometry experiment revealed that galaxamide analogues namely Compounds 6, 18, and 22 induced concentration dependent SMMC-7721 cell apoptosis after 48 h. These compounds induced G0/G1 phase cell-cycle arrest and morphological changes indicating induction of apoptosis. Thus, findings of our study suggest that the galaxamide and its analogues 6, 18 and 22 exerted growth inhibitory effect on SMMC-7721 cells by arresting the cell cycle in the G0/G1 phase and inducing apoptosis. Compound 1 showed promising anti-tumor activity towards SMMC-7721 cancer cell line, which is 9 and 10 fold higher than galaxamide and reference DPP (cisplatin), respectively.

Qiong-Zhi Gan,1,2 Xin-Yuan Sun,1,2 Poonam Bhadja,1,2 Xiu-Qiong Yao,1,2 Jian-Ming Ouyang1,2 1Department of Chemistry, Jinan University, Guangzhou, People’s Republic of China; 2Institute of Biomineralization and Lithiasis Research, Jinan University, Guangzhou, People’s Republic of China Background: Renal epithelial cell injury facilitates crystal adhesion to cell surface and serves as a key step in renal stone formation. However, the effects of cell injury on the adhesion of nano-calcium oxalate crystals and the nano-crystal-induced reinjury risk of injured cells remain unclear.Methods: African green monkey renal epithelial (Vero) cells were injured with H2O2 to establish a cell injury model. Cell viability, superoxide dismutase (SOD) activity, malonaldehyde (MDA) content, propidium iodide staining, hematoxylin–eosin staining, reactive oxygen species production, and mitochondrial membrane potential (ΔΨm) were determined to examine cell injury during adhesion. Changes in the surface structure of H2O2-injured cells were assessed through atomic force microscopy. The altered expression of hyaluronan during adhesion was examined through laser scanning confocal microscopy. The adhesion of nano-calcium oxalate monohydrate (COM) and calcium oxalate dihydrate (COD) crystals to Vero cells was observed through scanning electron microscopy. Nano-COM and COD binding was quantitatively determined through inductively coupled plasma emission spectrometry.Results: The expression of hyaluronan on the cell surface was increased during wound healing because of Vero cell injury. The structure and function of the cell membrane were also altered by cell injury; thus, nano-crystal adhesion occurred. The ability of nano-COM to adhere to the injured Vero cells was higher than that of nano-COD crystals. The cell viability, SOD activity, and ΔΨm decreased when nano-crystals attached to the cell surface. Bycontrast, the MDA content, reactive oxygen species production, and cell death rate increased.Conclusion: Cell injury contributes to crystal adhesion to Vero cell surface. The attached nano-COM and COD crystals can aggravate Vero cell injury. As a consequence, crystal adhesion and aggregation are enhanced. These findings provide further insights into kidney stone formation. Keywords: nano-calcium oxalate crystals, cell injury, crystal adhesion, kidney stones

The structure–activity relationships and repair mechanism of six low-molecular-weight seaweed polysaccharides (SPSs) on oxalate-induced damaged human kidney proximal tubular epithelial cells (HK-2) were investigated. These SPSs included Laminaria japonica polysaccharide, degraded Porphyra yezoensis polysaccharide, degraded Gracilaria lemaneiformis polysaccharide, degraded Sargassum fusiforme polysaccharide, Eucheuma gelatinae polysaccharide, and degraded Undaria pinnatifida polysaccharide. These SPSs have a narrow difference of molecular weight (from 1968 to 4020 Da) after degradation by controlling H2O2 concentration. The sulfate group (–SO3H) content of the six SPSs was 21.7%, 17.9%, 13.3%, 8.2%, 7.0%, and 5.5%, respectively, and the –COOH contents varied between 1.0% to 1.7%. After degradation, no significant difference was observed in the contents of characteristic –SO3H and –COOH groups of polysaccharides. The repair effect of polysaccharides was determined using cell-viability test by CCK-8 assay and cell-morphology test by hematoxylin-eosin staining. The results revealed that these SPSs within 0.1–100 μg/mL did not express cytotoxicity in HK-2 cells, and each polysaccharide had a repair effect on oxalate-induced damaged HK-2 cells. Simultaneously, the content of polysaccharide –SO3H was positively correlated with repair ability. Furthermore, the low-molecular-weight degraded polysaccharides showed better repair activity on damaged HK-2 cells than their undegraded counterpart. Our results can provide reference for inhibiting the formation of kidney stones and for developing original anti-stone polysaccharide drugs.

Objective: This study aims to compare the cytotoxicity and adhesion of subm icron calcium oxalate monohydrate (COM) and dehydrate (COD) crystals toward African green monkey renal epithelial cells (Vero) to reveal the mechanism of kidney stone formation at cellular level. Methods: The injury effect of COM and COD crystals in Vero was investigated by detecting the change of cell viability, lactate dehydrogenase (LDH) content and hyaluronan (HA) expression amount. The adhesion of crystals on cell surface was observed using scanning electron microscope; and the crystal adhesion amount was measured using inductively coupled plasma emission spectrometer. Results: The cellular injury induced by crystals was in a dose-dependent manner in the concentration range of 100~400μg/mL; COM caused more serious injury than COD, the adhesion amount of COM on Vero was significantly greater than COD. Conclusions: The damage of submicron COM is larger than submicron COD, the adhered COM crystals are more easily aggregated. The results in this paper indicated that the presence of high concentration of COM crystals in urine is more likely to increase the risk of stone formation than COD crystals.

Butterflies (Lepidoptera) being potent pollinators and ecological indicators are examined in the present study. The diversity of butterfly communities of the Kathiawar Peninsula ( tropical and subtropical region ) was studied at Mangrol region of Kathiawar Peninsula. The pollard walk method was followed for observing butterflies. A total 348 specimens belonging to 27 species, 21 genera and 4 families were recorded in the study sites. Among the butterfly species maximum populations were recorded of Family Nymphalidae (55.56%) followed by Pieridae (22.22%), Papilionidae (14.81%) and Lycaenidae (7.41%). Evaluation of quantitative and qualitative community structure in relation to four study sites of the Butterfly species density (29.00) and relative density (26.96) were highest in sampling Site Mangrol whereas species diversity index (H’) were also highest (04.14).  Keywords - butterfly diversity, community, habitat type, Kathiawar Peninsula, tropical and sub-tropical region

Present communication reports the physico-chemical and biological quality of seawater and status of benthos of a highly industrialized shore of the north-western coastline of India. The coastal area considered for the present study, encircled by a variety of industries, was divided into two sampling sites and monitored for two consecutive years. Results of the water quality suggest that the obtained values of the physical and chemical parameters of seawater were comparable with data reported earlier. However, data obtained in the biological parameters of the seawater showed a declining trend. Results of the intertidal macrofaunal diversity studies revealed that the muddy upper littoral zones were represented by few species of coelenterata, porifera, arthropoda and mollusca. In the rocky—muddy middle littoral zones, gastropods, stars fishes, corallites, crabs, polychetes and tubeworms were present, whereas, predominantly rocky lower littoral zones were comparatively rich in macrofaunal diversity with small patches of coral colonies. However, when the results obtained in the present study was compared with that of earlier reported data, it was clear that the macrofaunal diversity indeed declined considerably over the years. This may be due to habitat destruction and habitat alteration in the coastline caused by increased anthropogenic activities in the area. Seasonal variations in the population density and abundance were observed in most of the faunal groups except in sessile corals and sponges. This may be due to local migration of the faunal groups towards deeper regions of the Gulf, as supported by the analysis of similarity, to avoid influx of freshwater during monsoon, and high temperature during summer and post monsoon seasons. The overall assessment of different parameters of this study revealed that though the physico- chemical characteristics of the seawater did not varied much from the earlier reported status, the biological characteristics of the seawater and intertidal zone was affected possibly by a high degree of anthropogenic pressure.