Search

The grave environmental, social, and economic concerns over the unprecedented exploitation of non-renewable energy resources have drawn the attention of policy makers and research organizations towards the sustainable use of agro-industrial food and crop wastes. Enzymes are versatile biocatalysts with immense potential to transform the food industry and lignocellulosic biorefineries. Microbial enzymes offer cleaner and greener solutions to produce fine chemicals and compounds. The production of industrially important enzymes from abundantly present agro-industrial food waste offers economic solutions for the commercial production of value-added chemicals. The recent developments in biocatalytic systems are designed to either increase the catalytic capability of the commercial enzymes or create new enzymes with distinctive properties. The limitations of low catalytic efficiency and enzyme denaturation in ambient conditions can be mitigated by employing diverse and inexpensive immobilization carriers, such as agro-food based materials, biopolymers, and nanomaterials. Moreover, revolutionary protein engineering tools help in designing and constructing tailored enzymes with improved substrate specificity, catalytic activity, stability, and reaction product inhibition. This review discusses the recent developments in the production of essential industrial enzymes from agro-industrial food trash and the application of low-cost immobilization and enzyme engineering approaches for sustainable development. [ABSTRACT FROM AUTHOR]

We fabricated carbon nanotubes (CNTs) bridged MoS 2 /ZnO nanohybrids from the hydrothermal process for the heterostructure photocatalysts. The nanohybrids were effectively operated as visible light action for the photocatalytic of organic compounds and heavy metal reduction. The results exhibit that the great photocatalytic efficiency from nanohybrids for the 94.5% of tetracycline (TC) degradation after 60 min of irradiation. Enhanced environmental pollutants removal was due to inhibition in recombination of photogenerated electron-hole pairs. The nanohybrids also displayed better photocatalytic performance and reduction capacity (Cr (VI) ions removal), about 10–15 folds as greater than that of bulk MoS 2 , and ZnO photocatalysts. The nanohybrid showing a wonderful photocatalytic antibacterial capability of 99.9% towards E. coli after 5 min and supplying a favourable environmentally friendly for water disinfection. Based on this studies, we believe that a promising candidate nanohybrids for the photocatalytic of various water contaminants under visible light activity. [Display omitted] • A new Z-scheme CNTs bridged MoS 2 /ZnO heterostructure was synthesized via simple hydrothermal process. • Nanohybrids photocatalysts exhibits increased specific surface area and heavy metal reduction. • Nanohybrids exhibits excellent light response and the separation of charge carriers. • The nanohybrids showing a wonderful photocatalytic antibacterial capability of E. coli. • A possible mechanism was proposed based on the band structure. [ABSTRACT FROM AUTHOR]

Ethyl esters of omega-3 fatty acids are active pharmaceutical ingredients used for the reduction in triglycerides in the treatment of hyperlipidemia. Herein, an ultrasonic packed-bed bioreactor was developed for continuous production of docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA) ethyl esters from DHA+EPA concentrate and ethyl acetate (EA) using an immobilized lipase, Novozym® 435, as a biocatalyst. A three-level–two-factor central composite design combined with a response surface methodology (RSM) was employed to evaluate the packed-bed bioreactor with or without ultrasonication on the conversion of DHA + EPA ethyl ester. The highest conversion of 99% was achieved with ultrasonication at the condition of 1 mL min−1 flow rate and 100 mM DHA + EPA concentration. Our results also showed that the ultrasonic packed-bed bioreactor has a higher external mass transfer coefficient and a lower external substrate concentration on the surface of the immobilized enzyme. The effect of ultrasound was also demonstrated by a kinetic model in the batch reaction that the specificity constant (V′max/K2) in the ultrasonic bath was 8.9 times higher than that of the shaking bath, indicating the ultrasonication increased the affinity between enzymes and substrates and, therefore, increasing reaction rate. An experiment performed under the highest conversion conditions showed that the enzyme in the bioreactor remained stable at least for 5 days and maintained a 98% conversion. [ABSTRACT FROM AUTHOR]

Groundwater contamination by organic aromatic compounds such as gasoline fuel is a serious worldwide problem because of their carcinogenic and mutagenic potential. This study evaluated the use of Fe 3 O 4 − carbon black (CB) composites for persulfate (PS) oxidation of benzene, toluene, ethylene, and xylene (BTEX) and methyl tert -butyl ether (MTBE) compounds from the aqueous solution. The characterization results of environmental scanning electron microscopy coupled with energy-dispersive spectroscopy, X-ray diffraction, Fourier transform infrared spectroscopy, and a superconducting quantum interference device magnetometry evidenced the successful synthesis of Fe 3 O 4 − CB composites. In addition, the in vitro cytotoxic activity and apoptotic response of these composites were investigated before and after the Fe 3 O 4 −CB/PS processes test of the BTEX and MTBE samples was performed. The effects of various operating parameters were evaluated to optimize the oxidation process, including the PS concentration, initial pH, and Fe 3 O 4 − CB amount. The results showed that increasing PS and Fe 3 O 4 − CB dosage could accelerate BTEX and MTBE oxidation when PS and Fe 3 O 4 − CB concentrations increased to 15 g L −1 and 1.0 g L −1 , respectively, at a pH of 3.0. The degradation rate of BTEX and MTBE was strongly pH-dependent. Methyl thiazolyl tetrazolium assay was employed to perform a cytotoxicity study after Fe 3 O 4 −CB/PS processing treatment of BTEX and MTBE degradation products on the zebrafish ( Danio rerio ) embryonic cell line (ZF4), which revealed that a weak effect and apoptosis in cell viability ultimately leads to cell death. The results suggested that Fe 3 O 4 −CB assisted persulfate oxidation without elevating the temperature is a suitable and economic alternative for the ex-situ treatment of BTEX- and MTBE-contaminated aquatic environments. [ABSTRACT FROM AUTHOR]

[Display omitted] • Hydrothermal pretreatment is one of the best strategies for biomass fractionation. • In-depth study of the severity factor and its effect on biomass fraction. • Microwave-assisted hydrothermal pretreatment is a promising prospect for biorefinery. • Challenges faced by microwave assisted hydrothermal pretreatment technology during commercialization. Recently, the world is experiencing a shift from petroleum refineries to biorefineries due to fossil fuel depletion and environmental concerns. To achieve sustainable development of biorefineries and other components of the biofuel production process, eco-friendly and cost-effective approaches are necessary. Therefore, lignocellulosic biomass (LCB) must be exploited in biorefineries for the generation of a broad spectrum of products. The complex structure of LCB prevents its direct saccharification by enzymatic means, so pretreatment is necessary. There are several pretreatment technologies for disrupting the lignocellulosic structure, but hydrothermal pretreatment is the leading pretreatment technology for recovering hemicellulose fraction with a low number of inhibitors and an increased amount of cellulose. The severity of hydrothermal pretreatment plays a principal role in affecting cellulose, hemicellulose, and lignin structure. A detailed account of microwave-assisted hydrothermal pretreatment technologies and the cost-effectiveness, eco-friendliness, and upcoming challenges of this technology for commercialization with the probable solution is presented. [ABSTRACT FROM AUTHOR]

[Display omitted] • Deep eutectic solvents possess excellent potential for fractionation of biomass. • DESs effectively accelerate lignin removal and cellulose valorisation from LCB. • Process efficacy is enhanced by combinatorial DES based assistive pretreatment. • Different biofuels and value-added products can be derived from LCB using DESs. Increasing reliance on non-renewable fuels has shifted research attention to environmentally friendly and sustainable energy sources. The inherently recalcitrant nature of lignocellulosic biomass (LCB) makes downstream processing of the bioprocess challenging. Deep eutectic solvents (DESs) are popular and inexpensive green liquids found effective for LCB valorisation. DESs have negligible vapor-pressure and are non-flammable, recyclable, cost-economic, and thermochemically stable. This review provides a detailed overview on the DESs types, properties and their role in effective delignification and enzymatic digestibility of polysaccharides for cost-effective conversion of LCB into biofuels and bioproducts. The conglomeration of DESs with assistive pretreatment techniques can augment the process of biomass deconstruction. The current challenges in upscaling the DESs-based pretreatment technology up to commercial scale is summarized, with possible solutions and future directions. These insights would fill the knowledge-gaps to towards development of lignocellulosic biorefineries and to address the global energy crisis and environment issues. [ABSTRACT FROM AUTHOR]

Previous studies suggest that single-walled carbon nanotube (SWCNT) exposure causes pulmonary fibrosis. We investigated the contribution of epithelial-mesenchymal transition (EMT) during SWCNT-induced pulmonary fibrosis. C57BL6 female mice were intratracheally instilled with SWCNT at 80 μg/mouse for up to 56 days. SWCNT exposure caused pulmonary epithelial and mesenchymal injury, followed by granulomatous and fibrotic changes. Immunofluorescence staining demonstrated the increasing occurrence of epithelial-derived fibroblasts up to 42 days post-exposure. Flow cytometry analysis revealed that 42.60% of N-cadherin (N-cad)-positive fibroblasts were derived from pulmonary epithelial cells, and, in separate experiments, 30.68% of SPC positive cells were stained for N-cad at 42 days. These epithelial-derived fibroblasts were functional in collagen production. With the progression of fibrosis, there were increases in the number of hyperplastic epithelial cells stained positively for TGF-β/p-Smad2 or β-catenin. Therefore, EMT contributes significantly to fibroblast expansion. Aberrant activations of TGF-β/p-Smad2 and β-catenin are postulated to induce EMT during SWCNT-induced pathogenic fibrosis. [ABSTRACT FROM AUTHOR]

Background/Aims: Mitoxanthrone (MX) is an anthracenedione antineoplastic agent. Whether this drug and other related compounds have any effects on ion currents in osteoclasts remains largely unclear. Methods: In this study, the effects of MX and other related compounds on inwardly rectifying K+ current (IK(IR)) were investigated in RAW 264.7 osteoclast precursor cells treated with lipopolysaccharide. Results: The IK(IR) in these cells are blocked by BaCl2 (1 mM). MX (1-100 μM) decreased the amplitude of IK(IR) in a concentration-dependent manner with an IC50 value of 6.4 μM. MX also slowed the time course of IK(IR) inactivation elicited by large hyperpolarization. Doxorubicin (10 μM), 17β-estradiol (10 μM) and tertiapin (1 μM) decreased the IK(IR) amplitude in these cells. In bafilomycin A1-treated cells, MX-mediated block of IK(IR) still existed. In cell-attached configuration, when the electrode was filled with MX (10 μM), the activity of inwardly rectifying K+ (Kir) channels was decreased with no change in single-channel conductance. MX-mediated reduction of channel activity is accompanied by a shortening of mean open time. Under current-clamp conditions, addition of MX resulted in membrane depolarization. Therefore, MX can interact with the Kir channels to decrease amplitude and to depolarize the membrane in these cells. Conclusion: The block by the IK(IR)this drug of Kir2.1 channels appears to be one of the important mechanisms underlying its actions on the resorptive activity of osteoclasts, if similar results occur in vivo. Targeting at Kir channels may be clinically useful as an adjunctive regimen to anti-cancer drugs (e.g., MX or doxorubicin) in influencing the resorptive activity of osteoclasts. Copyright © 2012 S. Karger AG, Basel [ABSTRACT FROM AUTHOR]

Abstract: Liver microsomes are subcellular fractions that contain many metabolizing enzymes for drugs and endogeneous compounds. Some of these enzymes are regulated by sex hormonal control and exhibit sex-dependent expression pattern and metabolizing speed. Studying these enzymes, however, are complicated by the presence of isoforms such as cytochrome P450 (CYP450), which families share more than 50% amino acid identities. In this study, we applied quantitative shot-gun proteomics approach coupled with stable-isotope dimethyl labeling, two-dimensional reversed-phase peptide separation and tandem mass spectrometry (MS) to explore the gender-dependent expression of rat liver microsomal proteins. A total of 391 proteins were identified and quantified by this approach, and 56% of quantified proteins were enzymes. Although shot-gun approach is rarely used for identifying protein isoforms, we identified 53 isoforms by at least one unique peptide including 21 isoforms of CYP450s. Moreover, by quantitative and statistics assessment, we were able to classify them into 28 male dominant enzymes including CYP2C12 CYP2C11, CYP2C13, CYP2B3, CYP2C11, CYP2C70 and CYP3A2 which are known to be male specific, 21 female dominant enzymes including CYP2A1, CYP2C7, CYP2C12, CYP2D26, alcohol dehydrogenase 1, carboxylesterase 3, glutathione S-transferase, liver carboxylesterase 4, UDP-glucuronosyltransferase 2B1, and glyceraldehyde-3-phosphate dehydrogenase which are known to be female specific; and 125 sex-independent enzymes. However, most of the sex specificities revealed from this study, such as the male specificity of CYP2D1, were novel and not yet reported. We then conducted a mass spectrometry-multiple reaction mode (MS-MRM) based enzyme activity method to determine the catalyzing rate of CYP2D1 in male and female liver microsomes using carteolol as its specific substrate. The reaction rate catalyzed by CYP2D1 in female rats was determined to differ significantly with the rate in male rats. Moreover, the ratio (female/male) of reaction rate (0.68) was found to correlate with their relative protein abundance (0.72). This study revealed novel sex dependences of many rat liver enzymes and also demonstrated a unique MS-based analytical platform that could identify novel iso-enzymes and further quantify their abundance and enzyme activity. [Copyright &y& Elsevier]

Abstract: We present the cDNA sequences and tissue mRNA expression of peroxisome proliferator-activated receptor (PPAR) α, β and γ isotypes in the cobia (Rachycentron canadum), a warm water pelagic fish that is becoming a fish of choice for offshore cage farming. RT-PCR and real-time PCR showed that PPARα mRNA predominated in red muscle, heart and liver whereas PPARβ was expressed mainly in liver and pyloric caeca. In contrast, PPARγ transcripts were detected in all of the tissues examined, with the highest level occurring in visceral fat depot. Our 52-wk time-series investigation showed that while the mRNA expression of PPARγ in the cobia was positively (P <0.05) related to its body lipid deposition, a negative (P <0.05) relationship was found between PPARα expression in the liver and body lipid deposition. There was a significant increase in body lipid deposition and hepatic PPARγ expression as the fish grew. The hepatic PPARγ expression could be a sufficient parameter describing the bodily expression of PPARγ because of its positive correlation with PPARγ expressions in all other tissues. These results showed that PPARγ and α played a pivotal role in the control of lipid metabolic and storage functions in the liver, muscle and visceral fat depot of the cobia. [Copyright &y& Elsevier]

[Display omitted] • Sequential ChCl/citric acid-microwave pretreatment was used for XOS production. • Maximum lignin (51.5%) and xylan (67.36%) removal obtained from pretreated mixture. • High XOS yield (52%) was obtained at 450W microwave power with ChCl/citric acid. • A high xylobiose content (69.32%) was analyzed from total xylooligosaccharides. The bioconversion of lignocellulosic biomass into novel bioproducts is crucial for sustainable biorefineries, providing an integrated solution for circular economy objectives. The current study investigated a novel microwave-assisted acidic deep eutectic solvent (DES) pretreatment of waste cocoa pod husk (CPH) biomass to extract xylooligosaccharides (XOS). The sequential DES (choline chloride/citric acid, molar ratio 1:1) and microwave (450W) pretreatment of CPH biomass was effective in 67.3% xylan removal with a 52% XOS yield from total xylan. Among different XOS of varying degrees of polymerization, a higher xylobiose content corresponding to 69.3% of the total XOS (68.22 mg/g CPH) from liquid fraction was observed. Enzymatic hydrolysis of residual xylan from pretreated CPH biomass with low commercial xylanase (10 IU/g) concentration yielded 24.2% XOS. The MW-ChCl/citric acid synergistic pretreatment approach holds great promise for developing a cost-effective and environmentally friendly method contributing to the sustainable production of XOS from agricultural waste streams. [ABSTRACT FROM AUTHOR]

[Display omitted] • Agricultural waste is a potential and abundant bioresource for biogas production. • Anaerobic digestion of biomass is an efficient, low-cost biogas production strategy. • State-of-the-art upgrading methods for biomethane enrichment are explored. • Machine learning tools can effectively predict biogas yield at an industrial scale. • Life cycle analysis of biogas systems helps assess environmental and economic effects. Recent years have seen a transition to a sustainable circular economy model that uses agro-industrial waste biomass waste to produce energy while reducing trash and greenhouse gas emissions. Biogas production from lignocellulosic biomass (LCB) is an alternative option in the hunt for clean and renewable fuels. Different approaches are employed to transform the LCB to biogas, including pretreatment, anaerobic digestion (AD), and biogas upgradation to biomethane. To maintain process stability and improve AD performance, machine learning (ML) tools are being applied in real-time monitoring, predicting, and optimizing the biogas production process. An environmental life cycle assessment approach for biogas production systems is essential to calculate greenhouse gas emissions. The current review presents a detailed overview of the utilization of agro-waste for sustainable biogas production. Different methods of waste biomass processing and valorization are discussed that contribute towards developing an efficient agro-waste to biogas-based circular economy. [ABSTRACT FROM AUTHOR]

[Display omitted] • Development of biorefineries leads to eco-friendly production of bioenergy. • Green pretreatment approaches for lignocellulosic biomass are required. • Bioengineering and immobilization techniques develop effective biocatalyst systems. • Machine learning models present possibilities in bioenergy prediction. • LCA is used to evaluate the supply chain for a biorefinery's environmental effect. The idea of environment friendly and affordable renewable energy resources has prompted the industry to focus on the set up of biorefineries for sustainable bioeconomy. Lignocellulosic biomass (LCB) is considered as an abundantly available renewable feedstock for the production of biofuels which can potentially reduce the dependence on petrochemical refineries. By utilizing various conversion technologies, an integrated biorefinery platform of LCB can be created, embracing the idea of the 'circular bioeconomy'. The development of effective pretreatment methods and biocatalytic systems by various bioengineering and machine learning approaches could reduce the bioprocessing costs, thereby making biomass-based biorefinery more sustainable. This review summarizes the development and advances in the lignocellulosic biorefineries from the LCB to the final product stage using various different state-of-the-art approaches for the progress of circular bioeconomy. The life cycle assessment which generates knowledge on the environmental impacts related to biofuel production chains is also summarized. [ABSTRACT FROM AUTHOR]

Graphical abstract Highlights • Highly microporous Fe 3 O 4 –BB was prepared from Moso bamboo. • Persulfate oxidation processes are proposed for the degradation of 4-NP in real river sediments. • 4-NP degradation rate depends on pH value and Fe 3 O 4 –BB dose. • The K obs of 4-NP degradation followed the order: Fe 3 O 4 –BB/PS ˃ PS ˃ Fe 3 O 4 –BB. • The Langmuir-Hinshelwood model was found to fit the kinetic equation. Abstract In this study, an environmentally friendly and economically viable bamboo biochar (BB) was modified by Fe 3 O 4 and was applied for the treatment of real river sediments containing the endocrine disruptor chemical (EDC) 4-nonylphenol (4-NP). The microporosity of Fe 3 O 4 –BB was clearly observed from the N 2 adsorption isotherms. The catalytic performance of Fe 3 O 4 –BB is highly dependent on pH and the catalyst dosage. The degradation efficiency of 4-NP (85%) was achieved at pH 3.0 using an initial dosage of 3.33 g L−1 Fe 3 O 4 –BB and 2.3 × 10−5 M persulfate (PS) in a biochar–sediment system. The kinetic behavior of 4-NP degradation with catalysis can be accounted by using the Langmuir-Hinshelwood type kinetic model. The MTT assay results indicated that Fe 3 O 4 –BB has a low potent cytotoxic effect and is therefore suitable for application in remediation of contaminated sediment. [ABSTRACT FROM AUTHOR]

The semiconducting metal oxides coupled with carbon materials show a broad interest in developing low-cost and accurate electrochemical sensors. Herein, we designed a sensitive and selective electrode material of hexagonal zinc oxide nanodiscs decorated (ZnO NDs) boron-doped graphitic carbon nitride (B-CN) sheets fabricated over glassy carbon electrode (GCE) for efficient detection of rutin (RT). The prepared electrocatalyst and fabricated sensors were analyzed using different physicochemical and electrochemical characteristics. The prepared electrocatalyst and fabricated sensor confirmed physicochemical and electrochemical characteristics. Notably, the developed sensor shows good sensitive recognition of RT detection (1.0225 μA·μM-1·cm-2), a low limit of detection (LOD= 0.0027 µM), and a wide linear range (0.005–589.685 µM) in phosphate buffer (PB, pH 3.0). The newly developed sensor was also applied to detect potential interfering species and real-sample analysis. The proposed sensor show excellence in selectivity, reproducibility, stability (89.55%), and practicability during electrochemical RT detection. The present report demonstrates to development of a cheap and sensitive platform for RT determination in fruit samples. [Display omitted] • The B-CN Sheets decorated ZnO NDs via a simple sonochemical method. • The developed ZnO NDs/B-CN/GCE sensor displayed a wide linear range (0.005 to 589.685 µM) and a low LOD (0.0027 µM). • The ZnO NDs/B-CN/GCE sensor shows good selectivity with potential interfering compounds. • The developed sensor was successful in the detection of RT in fresh fruit samples. [ABSTRACT FROM AUTHOR]

The urgent demand for alternative energy sources has been sparked by the tremendous burden on fossil fuels and the resulting acute energy crisis and climate change issues. Lignocellulosic biomass is a copious renewable and alternative bioresource for the generation of energy fuels and biochemicals in biorefineries. Different pretreatment strategies have been established to overcome biomass recalcitrance and face technological challenges, such as high energy consumption and operational costs and environmental hazards, among many. Biological pretreatment using microbial enzymes is an environmentally benign and low-cost method that holds promising features in the effective pretreatment of lignocellulosic biomass. Due to their versatility and eco-friendliness, cellulases, hemicellulases, and ligninolytic enzymes have been recognized as "green biocatalysts" with a myriad of industrial applications. The current review provides a detailed description of different types of lignocellulolytic enzymes, their mode of action, and their prospective applications in the valorization of lignocellulosic biomass. Solid state fermentation holds great promise in the microbial production of lignocellulolytic enzymes owing to its energy efficient, environment friendly, and higher product yielding features utilizing the lignocellulosic feedstocks. The recent trends in the application of enzyme immobilization strategies for improved enzymatic catalysis have been discussed. The major bottlenecks in the bioprocessing of lignocellulosic biomass using microbial enzymes and future prospects have also been summarized. [ABSTRACT FROM AUTHOR]

Growth in population and thereby increased industrialization to meet its requirement, has elevated significantly the demand for energy resources. Depletion of fossil fuel and environmental sustainability issues encouraged the exploration of alternative renewable eco-friendly fuel resources. Among major alternative fuels, bio-ethanol produced from lignocellulosic biomass is the most popular one. Lignocellulosic biomass is the most abundant renewable resource which is ubiquitous on our planet. All the plant biomass is lignocellulosic which is composed of cellulose, hemicellulose and lignin, intricately linked to each other. Filamentous fungi are known to secrete a plethora of biomass hydrolyzing enzymes. Mostly these enzymes are inducible, hence the fungi secrete them economically which causes challenges in their hyperproduction. Biomass's complicated structure also throws challenges for which pre-treatments of biomass are necessary to make the biomass amorphous to be accessible for the enzymes to act on it. The enzymatic hydrolysis of biomass is the most sustainable way for fermentable sugar generation to convert into ethanol. To have sufficient ethanol concentration in the broth for efficient distillation, high solid loading ~<20% of biomass is desirable and is the crux of the whole technology. High solid loading offers several benefits including a high concentration of sugars in broth, low equipment sizing, saving cost on infrastructure, etc. Along with the benefits, several challenges also emerged simultaneously, like issues of mass transfer, low reaction rate due to water constrains in, high inhibitor concentration, non-productive binding of enzyme lignin, etc. This article will give an insight into the challenges for cellulase action on cellulosic biomass at a high solid loading of biomass and its probable solutions. [ABSTRACT FROM AUTHOR]

Icilin is recognized as a chemical agonist of nociceptors and can activate TRPM8 channels. However, whether this agent has any effects on immune cells remains unknown. In this study, the effects of icilin on ion currents were investigated in RAW 264.7 murine macrophage-like cells. Icilin (1-100 μM) increased the amplitude of nonselective (NS) cation current (INS) in a concentration-dependent manner with an EC50 value of 8.6 μM. LaCl3 (100 μM) or capsazepine (30 μM) reversed icilin-induced INS; however, neither apamin (200 nM) nor iberiotoxin (200 nM) had any effects on it. In cell-attached configuration, when the electrode was filled with icilin (30 μM), a unique population of NS cation channels were activated with single-channel conductance of 158 pS. With the use of a long-lasting ramp pulse protocol, increasing icilin concentration produced a left shift in the activation curve of NS channels, with no change in the slope factor of the curve. The probability of channel opening enhanced by icilin was increased by either elevated extracellular Ca2+ or application of ionomycin (10 μM), while it was reduced by BAPTA-AM (10 μM). Icilin-stimulated activity is associated with an increase in mean open time and a reduction in mean closed time. Under current-clamp conditions, icilin caused membrane depolarization. Therefore, icilin interacts with the TRPM8-like channel to increase INS and depolarizes the membrane in these cells. [ABSTRACT FROM AUTHOR]

Abstract: Rosemary (Rosmarinus officinalis), a culinary spice and medicinal herb, has been widely used in European folk medicine to treat numerous ailments. Many studies have shown that rosemary extracts play important roles in anti-inflammation, anti-tumor, and anti-proliferation in various in vitro and in vivo settings. The roles of tumor suppression of rosemary have been attributed to the major components, including carnosic acid, carnosol, and rosmarinic acid, rosmanol, and ursolic acid. This study was to explore the effect of rosmanol on the growth of COLO 205 human colorectal adenocarcinoma cells and to delineate the underlying mechanisms. When treated with 50μM of rosmanol for 24h, COLO 205 cells displayed a strong apoptosis-inducing response with a 51% apoptotic ratio (IC50 ∼42μM). Rosmanol increased the expression of Fas and FasL, led to the cleavage and activation of pro-caspase-8 and Bid, and mobilized Bax from cytosol into mitochondria. The mutual activation between tBid and Bad decreased the mitochondrial membrane potential and released cytochrome c and apoptosis-inducing factor (AIF) to cytosol. In turn, cytochrome c induced the processing of pro-caspase-9 and pro-caspase-3, followed by the cleavage of poly-(ADP-ribose) polymerase (PARP) and DNA fragmentation factor (DFF-45). These results demonstrate that the rosmanol-induced apoptosis in COLO 205 cells is involvement of caspase activation and involving complicated regulation of both the mitochondrial apoptotic pathway and death receptor pathway. [ABSTRACT FROM AUTHOR]

Macro- and microalgae-based foods are becoming popular due to their high nutritious value. The algal biomass is enriched with polysaccharides, protein, polyunsaturated fatty acids, carotenoids, vitamins and minerals. However, the most promising fraction is polysaccharides (PS) or their derivatives (as dietary fibers) which are not entirely fermented by colonic bacteria hence act as potential prebiotic. Primarily, algae become famous as prominent protein sources. Recently, these are widely adopted as functional food (e.g., desserts, dairy products, oil-derivatives, pastas etc.) or animal feed (for poultry, cattle, fish etc.). Besides prebiotic and balanced amino acids source, algae derived compounds implied as therapeutics due to comprising bioactive properties to elicit immunomodulatory, antioxidative, anticancerous, anticoagulant, hepato-protective, and antihypertensive responses. Despite the above potentials, broader research determinations are inevitable to explore these algal compounds until microalgae become a business reality for broader and specific applications in all health domains. However, scale up of algal bioprocess remains a major challenge until commercial affordability is accomplished which can be possible by discovering their hidden potentials and increasing their value and application prospects. This review provides an overview of the significance of algae consumption for several health benefits in humans and animals mainly as prebiotics, however their functional food and animal feed potential are briefly covered. Moreover, their potential to develop an algal-based food industry to meet the people's requirements not only as a sustainable food solution with several health benefits but also as therapeutics is inevitable. [ABSTRACT FROM AUTHOR]

This study evaluated the level of the contaminant of the heavy metals in sludge from different sources and the ecological risk criteria associated with it was also analyzed to establish its reuse in agriculture. The sludge samples were collected from the water plant (WTP), wastewater treatment plant (WWTP), and industrial water treatment plant (IPT) in Taiwan. The inductively coupled plasma mass spectrometry was used to measure the trace metals in sludge. The pollution level and ecological risk criteria for heavy metals in sludge were also used to evaluate its reuse in agriculture. The result shows the average concentrations of trace metals in sludge for three groups (WTP, WWTP, and ITP). Significant correlations were found between concentrations of Zn-Ag (p < 0.001). The higher values of Igeo showed in ITP, indicated Hg to be a major pollutant. In Taiwan, the regulations did not establish the reuse of sludge in agriculture. However, the concentration level of trace metals in sludge was particularly lower than the regular levels in most groups, like WTP and WWTP groups. The industrial sludge was not recommended for the use in agriculture. The results of this study can be used for regular monitoring to establish a reference for sludge management and application to agriculture. [ABSTRACT FROM AUTHOR]

Background: Mechanical ventilation is a life-saving procedure for patients with acute respiratory failure, although it may cause pulmonary vascular inflammation and leakage, leading to ventilator-induced lung injury (VILI). Ly6C+high monocytes are involved in the pathogenesis of VILI. In this study, we investigated whether pulmonary infiltrated Ly6C+high monocytes produce vascular endothelial growth factor (VEGF) and contribute to VILI. Methods: A clinically relevant two-hit mouse model of VILI, with intravenous lipopolysaccharide (LPS, 20 ng/mouse) immediately before high tidal volume (HTV, 20 mL/kg) ventilation (LPS+HTV), was established. Blood gas and respiratory mechanics were measured to ensure the development of VILI. Flow cytometry and histopathological analyses revealed pulmonary infiltration of leukocytes subsets. Clodronate liposomes were intravenously injected to deplete pulmonary monocytes. In vitro endothelial cell permeability assay with sorted Ly6C+high monocytes condition media assessed the role of Ly6C+high monocytes in vascular permeability. Results: LPS+HTV significantly increased total proteins, TNF-α, IL-6, vascular endothelial growth factor (VEGF) and mononuclear cells in the bronchoalveolar lavage fluid (BALF). Pulmonary Ly6C+high monocytes (SSClowCD11b+F4/80+Ly6C+high), but not Ly6C+low monocytes (SSClowCD11b+F4/80+Ly6C+low), were significantly elevated starting at 4 hr. Clodronate liposomes were able to significantly reduce pulmonary Ly6C+high monocytes, and VEGF and total protein in BALF, and restore PaO2/FiO2. There was a strong correlation between pulmonary Ly6C+high monocytes and BALF VEGF (R2 = 0.8791, p<0.001). Moreover, sorted Ly6C+high monocytes were able to produce VEGF, resulting in an increased permeability of endothelial cell monolayer in an in vitro endothelial cell permeability assay. Conclusion: VEGF produced by pulmonary infiltrated Ly6C+high monocytes regulates vasculature permeability in a two-hit model of HTV-induced lung injury. Ly6C+high monocytes play an important role in the pathogenesis of VILI. [ABSTRACT FROM AUTHOR]

This study was to determine the effects of high pressure processing (HPP; 200–600 MPa for 3 min) on the microbial, chemical, and organoleptic properties and the bacterial flora of freshwater clam (Corbicula fluminea) during cold storage. The results indicated that with an increase in pressure, the expanding rate, moisture content, shucking ratio, pH, lightness (L*), and whiteness (W) increased, whereas redness (a*), yellowness (b*), aerobic plate count (APC), psychrotrophic bacteria count (PBC), coliform, and Salmonella spp. decreased. In addition, HPP treatment of >300 MPa on samples significantly retarded the increases in APC, PBC, coliform, Salmonella spp., and total volatile basic nitrogen and a drop in pH during cold storage. Results of organoleptic analysis showed that HPP at 300 and 500 MPa prolonged the shelf life from 6 days (control group) to 9 days and 12 days, respectively. High-throughput sequencing (HTS) revealed that HPP considerably changed the spoilage microflora in samples after 15 days storage and delayed the spoilage process. These results demonstrate that pressurisation at least 300 MPa for 3 min on clam samples were able to reach 100% shucking, inactivate microbial growth, and retard quality loss, while they effectively extended shelf life of freshwater clam during cold storage. • HPP on clam was effective to shuck and increase the expanding rate, moisture and pH. • With increasing pressure, clam meat showed a brighter and translucent appearance. • HPP> 300 MPa delayed the growth of microbial loads, and drop of pH during 4 °C storage. • Self life of samples by 300 and 500 MPa extended from 6 to 9–12 days in cold storage. • HTS showed that HPP changed the microbiota of clam and delayed the spoilage process. [ABSTRACT FROM AUTHOR]

[Display omitted] • Lignocellulosic biomass can be directly converted into valuable products via CBP. • Single vessel decreases the infrastructure input, hence enabling economic feasibility. • A potential microbe or consortium could be instrumental for efficient CBP. • Bioengineering is a potential tool to obtain a robust microbial cell factory. Consolidated bioprocessing (CBP) is characterized by a single-step production of value-added compounds directly from biomass in a single vessel. This strategy has the capacity to revolutionize the whole biorefinery concept as it can significantly reduce the infrastructure input and use of chemicals for various processing steps which can make it economically and environmentally benign. Although the proof of concept has been firmly established in the past, commercialization has been limited due to the low conversion efficiency of the technology. Either a native single microbe, genetically modified microbe or a consortium can be employed. The major challenge in developing a cost-effective and feasible CBP process is the recognition of bifunctional catalysts combining the capability to use the substrates and transform them into value-added products with high efficiency. This article presents an in-depth analysis of the current developments in CBP around the globe and the possibilities of advancements in the future. [ABSTRACT FROM AUTHOR]

Potential toxic chemicals, specifically, polycyclic aromatic hydrocarbons (PAHs), are major sediment contaminants. Herein, green seaweed (Ulva lactuca) was used as a feedstock and pyrolyzed at temperature in the range between 300 and 900 °C. The metal-free carbocatalyst (GSBC) for peroxymonosulfate (PMS) activation to degrade PAHs contaminated sediments was studied. The effects of GSBC‒PMS treatment on microbial community abundance was studied as well. The pyrolysis temperature of GSBC preparation affected the PMS activation performance. Results show that GSBC700 exhibited remarkable catalytic characteristics in PAHs degradation by effective activation of PMS. The results also demonstrated that the sulfate radical-carbon-driven advanced oxidation processes (SR-CAOP) reaction achieved 87% and apparent rate constant (k obs) of 6.3 × 10−2 h−1 of total PAHs degradation in 24 h at 3.3 g/L of GSBC, PMS dose of 1 × 10−4 M, and pH 3.0. The degradation of 2-, 3-, 4-, 5-, and 6-ring PAHs was 84, 83, 83, 80, and 89%, respectively. The synergetic effect established between GSBC and PMS enhanced the formation of ROSs, namely, SO 4 -, HO , and 1O 2 , which were major species contributing to PAHs degradation. The synergistic effect of π‒π stacking structure and graphitization of GSBC formed electron shuttle, which contributed to PAHs degradation performance. Microbial community structure analyses in the GSBC‒PMS treated sediments showed that the relative abundance of Lactobacillus_rhamnosus species, most of which belonged to the Lactobacillus genus and Firmicutes phylum, which aided in continuing PAHs biodegradation post GSBC‒PMS treatment. Therefore, GSBC can be a promising carbocatalyst produced via biomass-to-biochar conversion as biowaste-to-energy source used in the SR-CAOP-mediated process for sediment remediation. • Green seaweed (Ulva lactuca) was pyrolyzed to obtain metal-free carbocatalyst for PMS activation. • Pyrolysis temperature mainly influenced the promotion of SR-CAOP reactions. • Synergetic effect between GSBC and PMS enhanced the formation of ROSs. • Combining GSBC/PMS treatment shifted the sediment bacterial community structure. • Green seaweed biochar is a safe and promising carbocatalyst for PAHs remediation. [ABSTRACT FROM AUTHOR]

Phthalate esters (PAEs) are a group of ubiquitous organic environmental contaminants. Engineered ferromanganese-bearing sludge-derived biochar (SDB), synthesized using one-step pyrolysis in the temperature range between 300 and 900 °C, was used to enable Fenton-like processes that decontaminated PAE-laden sediments. SDB was thoroughly characterized using scanning electron microscopy energy-dispersive spectroscopy, transmission electron microscopy, Brunauer–Emmett–Teller surface area, thermogravimetric analysis, Raman spectroscopy, Fourier-transform infrared spectroscopy, electron paramagnetic resonance, X-ray photoelectron spectroscopy, and fluorescence excitation–emission matrix spectroscopy coupled with parallel factor analysis. The maximum PAE degradation was remarkable at 90% in 12 h at pH 6.0 in the presence of 1.7 g L−1 of SDB 900. The highly-effective PAE degradation was mainly attributed to the synergism between FeO x and MnO x , which strengthened the activation of percarbonate (PC) via electron transfer, hydroxy addition, and hydrogen abstraction through radical (HO•) and nonradical (1O 2) oxidation mechanisms, thereby facilitating PAE catalytic degradation over SDB in real sediments, which clearly proved the efficacy of ferromanganese-bearing SDB and PC for the remediation of contaminated sediments. The cytotoxicity exhibited by human skin keratinocyte cells exposure to high SDB concentration (100–400 µg mL−1) for 24–48 h was low indicating insignificant cellular toxicity and oxidative damages. This study provides a new strategy for freshwater sludge treatment and reutilization, which enables a water-cycle-based circular economy and waste-to-resource recycling. [Display omitted] • Sludge-derived biochar (SDB) was synthesized by pyrolysis of freshwater sludge. • SDB activation of percarbonate effectively degraded phthalate ester (PAE) in sediments. • Fe and Mn minerals in SDB played a synergistic role on PAE degradation. • Radical (HO•) and nonradical (1O 2) were involved in PAE degradation. • Cytotoxicity in HaCaT cells exposure to SDB was low. [ABSTRACT FROM AUTHOR]

Abstract: Pterostilbene, found in grapes and berries, exhibits pleiotropic effects, including anti-inflammatory, antioxidant, and anti-proliferative activities. This study was conducted to investigate the effect of pterostilbene on liver fibrosis and the potential underlying mechanism for such effect. Sprague–Dawley rats were intraperitoneally given dimethyl n-nitrosamine (DMN) (10mg/kg) 3days per week for 4weeks. Pterostilbene (10 or 20mg/kg) was administered by oral gavage daily. Liver function, morphology, histochemistry, and fibrotic parameters were examined. Pterostilbene supplementation alleviated the DMN-induced changes in the serum levels of alanine transaminase and aspartate transaminase (p <0.05). Fibrotic status and the activation of hepatic stellate cells were improved upon pterostilbene supplementation as evidenced by histopathological examination as well as the expression of α-smooth muscle actin (α-SMA), transforming growth factor-β1 (TGF-β1), and matrix metalloproteinase 2 (MMP2). These data demonstrated that pterostilbene exhibited hepatoprotective effects on experimental fibrosis, potentially by inhibiting the TGF-β1/Smad signaling. [Copyright &y& Elsevier]

Abstract: Purification and characterization of keratinase from Meiothermus sp. I40, a newly identified strain isolated from hot springs, was carried out and reported. Crude enzyme was obtained from culture medium after incubation of I40 for 2 days and was purified by 20–80% precipitation with (NH4)2SO4, and separated by hydroxyapatite and Superdex pg 200 gel filtration chromatography. The overall recovery of enzyme activity was 45% with a 30.2-fold after purification. The molecular mass of the purified enzyme was 76 kDa with K m and V max of 0.29 mM and 1428.6 U/mg-min, respectively. The optimum pH and temperature of the keratinase I40 was 8.0; and 70 °C, respectively. When incubated at 65 °C and 70 °C for 12 h, the enzyme retained 96.7% and 71.3% of the activity, respectively. The purified enzyme was completely inhibited by phenylmethanesulfonyl fluoride (PMSF), indicating that keratinase I40 is a serine protease. Keratinase I40 exhibited good stability in the presence of dimethyl sulfoxide, ethanol, isopropanol and acetonitrile. The enzyme showed the highest activity toward chicken feather, followed by dove feather, duck feather, human hair, wool, and hog bristle. Chicken feathers treated with keratinase I40 were fully degraded in one days, but no change was detected with seven common proteases. The molecular weight (MW) of the peptides released from chicken feathers after treatment with keratinase I40 ranged from 0.48 to 10 kDa with an average of 1.84 kDa. Keratinase I40 seems to be an efficient and environmentally friendly enzyme in the biodegradation of feather keratin. [Copyright &y& Elsevier]

Summary A unicellular diazotrophic cyanobacterium strain of Group C, designated TW3, was isolated from the oligotrophic Kuroshio Current of the western Pacific Ocean. To our knowledge, this represents the first successful laboratory culture of a Group C unicellular diazotroph from oceanic water. TW3 cells are green rods, 2.5-3.0 µm in width and 4.0-6.0 µm in length. Phylogenetic analyses of both 16S rRNA and nifH gene fragments indicated that the TW3 sequences were over 98% identical to those of the previously isolated Cyanothece sp. ATCC51142 and Gloeocapsa sp., suggesting that TW3 is a member of the Group C unicellular diazotrophs. In addition, both TW3 and Cyanothece sp. ATCC51142 share morphological characteristics; both strains are sheathless and rod-shaped, display binary fission in a single plane, and possess dispersed thylakoids. TW3 grows aerobically in nitrogen-deficient artificial seawater, and exhibited the highest observed growth rate of 0.035 h−1 when cultured at 30°C and 140 µmol m−2 s−1 of light intensity. The nitrogen fixation rate, when grown optimally using a 12 h/12 h light-dark cycle, was 7.31 × 10−15 mol N cell−1 day−1. Immunocytochemical staining using Trichodesmium sp. NIBB1067 nitrogenase antiserum revealed the existence of diazotrophic cells sharing morphological characteristics of TW3 in the Kuroshio water from which TW3 was isolated. [ABSTRACT FROM AUTHOR]

The conductance catheter technique was developed in the 1980s to measure instantaneous ventricular conductance. After converting measured conductance to volume signals by use of the classic Baan conductance-to-volume equation, real-time pressure–volume (PV) relations can be obtained. A nonlinear conductance-to-volume conversion equation was proposed by Wei in 2005 to improve the accuracy of the conductance catheter system. This study tested the in vivo applicability of the nonlinear conversion equation, particularly focusing on the effect of deviation in catheter position. By altering catheter position, PV loops obtained by using the classic Baan's equation and the nonlinear equation were compared. The comparison results show that the nonlinear equation indeed compensates for the errors introduced by catheter position deviation, and gives more consistent and reliable PV relations. Moreover, the effect of variations in blood resistivity was analyzed. To obtain consistent and reliable PV relations, the nonlinear equation is suggested for use, and changes in blood resistivity should be carefully monitored. [ABSTRACT FROM AUTHOR]

Abstract: Hexahydro-β-acids (HBA) and β-acids (BA) displayed strong growth inhibitory effects against human leukemia HL-60 cells and were able to induce apoptosis in a concentration- and time-dependent manner and the morphological changes associated with apoptotic cell death; however, BA was less effective. Treatment with HBA caused a rapid loss of mitochondrial trans-membrane potential, release of mitochondrial cytochrome c into cytosol. The levels of Bad and Bax were dramatically increased in cells treated with HBA. In addition, the results showed that HBA promoted the up-regulation of Fas prior to the processing and activation of pro-caspase-8 and cleavage of Bid, suggesting the involvement of a Fas-mediated pathway in HBA-induced cells. Moreover, the changes occurred after single breaks in DNA were detected, suggesting that HBA induced irreparable DNA damage, which in turn triggered the process of apoptosis. HBA markedly enhanced the growth arrest DNA damage-inducible gene 153 (GADD153) protein in a concentration- and time-dependent manner. These findings suggest that HBA creates an oxidative cellular environment that induces DNA damage and GADD153 gene activation, which in turn triggers apoptosis in HL-60 cells. Our study identified the novel mechanisms of HBA-induced apoptosis and indicated that HBA may be used as a potential chemopreventive and chemotherapeutic agent. [Copyright &y& Elsevier]

Abstract: Pracparatum mungo is a traditional and functional food in Traditional Chinese Medicine, especially for treating a variety of liver disorders. In this study, we first report the in vivo hepatoprotective effect of P. mungo extract (PME) on carbon tetrachloride (CCl4)-induced acute hepatotoxicity in rats. Pre-treatment with PME for 56days significantly reduced the impact of CCl4 toxicity on the serum markers of liver damage, aspartate aminotransferase (AST) and alanine aminotransferase (ALT). The results were confirmed histopathologically. In addition, an increased lipid hydroperoxide (LPO), a decreased glutathione (GSH) concentration and a decreased superoxide dismutase (SOD) were observed in the hepatic tissues. On the contrary, treatment of PME prior to the administration of CCl4 resulted in markedly decreased lipid peroxidation, increased the levels of GSH and SOD in rats. The results indicated that PME has a protective effect against acute hepatotoxicity induced by the administration of CCl4 in rats, and that the hepatoprotective effects of PME may be due to both the inhibition of lipid peroxidation and the increase of antioxidant activity. [Copyright &y& Elsevier]

Cobia, Rachycentron canadum, is a medium-size marine fish with emerging global potential for offshore aquaculture. The processing waste, cobia liver, is a raw material rich in polyunsaturated fatty acid oils. In this study, an environmentally friendly green process, aqueous extraction (AE), was used to extract the cobia liver oil. The effect of cooking time and substrate water ratio on the oil extractability was investigated herein. The cooking time of 15 min, and substrate water ratio of 1:2 obtained the highest extraction efficiency. However, the oil extractability was only 18.8%. Thus, enzyme-assisted aqueous extraction (EAAE) was used to increase oil extractability and recovery of protein hydrolysates. The commercial proteases—including alcalase, papain, trypsin, and pepsin—were employed in pretreated cobia liver in order to increase oil release during AE. The EAAE results showed that maximum oil extractability was 38% by papain pretreatment. EAAE greatly improved the extraction efficiency; the oil extractability was double than that of AE (18.8%). The fatty acid profiles revealed that ω-3 polyunsaturated fatty acid contents of extracted oil obtained from AE and EAAE were 21.3% and 19.5%, respectively. Besides, the cobia liver hydrolysates obtained from EAAE by alcalase, papain, pepsin, and trypsin pretreatment showed scavenge DPPH radical activity with EC50 values of 0.92, 1.03, 0.83, and 0.53 mg, respectively. After in vitro simulated gastrointestinal digestion, the protein hydrolysates exhibited scavenge DPPH radical activity with EC50 values of 1.15, 1.55, 0.98, and 0.76 mg for alcalase, papain, pepsin, and trypsin, respectively. The study showed that the EAAE process can be used for extracting fish oil from fish waste while simultaneously obtaining the protein hydrolysates with antioxidant activity. [ABSTRACT FROM AUTHOR]

4-Nonylphenol (4-NP), a phenolic endocrine disruptor chemical (EDC), is known to have high toxicity to aquatic organisms and humans. The remediation of 4-NP-contaminated marine sediments was studied using red algae-based biochar (RAB) thermochemically synthesized from Agardhiella subulata with simple pyrolysis process under different temperatures of 300–900 °C in CO 2 atmosphere. The RAB was characterized by XRD, Raman, FTIR spectroscopy, and zeta potential measurements. The calcium in RAB efficiently activated sodium percarbonate (SPC) to generate reactive radicals for the catalytic degradation of 4-NP at pH 9.0. The oxygen-containing functional groups reacted with H 2 O 2 , which increased the generation of reactive radicals under alkaline pH condition. Ca2+ ion was the active species responsible for 4-NP degradation. CaO/CaCO 3 on RAB surface enhanced direct electron transfer, increased HO production, and 4-NP degradation in marine sediments. Langmuir‒Hinshelwood type kinetics well described the 4-NP degradation process. Remediation of contaminated sediments using RAB could be a sustainable approach toward closed-loop biomass cycling in the degradation of 4-NP contaminants. Image 1 • RAB was successfully prepared from red algae biomass. • Real marine sediments were treated with SPC oxidation for 4-NP removal. • Calcium-enriched RAB efficiently activated SPC to generate reactive radicals. • pH and RAB dose controlled 4-NP degradation. • Langmuir-Hinshelwood model described well the kinetics of 4-NP degradation. [ABSTRACT FROM AUTHOR]

Developing new therapeutic strategies to overcome drug resistance of cancer cells is an ongoing endeavor. From among 2 million chemicals, we identified ethyl 4-oxo-2-phenyl-1,4-dihydroquinoline-6-carboxylate (AS1712) as a low-toxicity inhibitor of lung cancer cell proliferation and xenograft tumor growth. We show that AS1712 is active against broad cancer cell lines and is able to bind in the colchicine-binding pocket of β-tubulin, thereby inhibiting microtubule assembly and, consequently, inducing mitotic arrest and apoptosis. Our cell-based structure-activity relationship study identified a new lead compound, RJ-LC-15-8, which had a greater anti-proliferative potency for H1975 cells than did AS1712, while maintaining a similar mechanism of action. Notably, AS1712 and RJ-LC-15-8 overcame P-glycoprotein efflux pump and β-tubulin alterations that lead to acquired resistance against microtubule-targeting drugs of cancer cells. AS1712 and RJ-LC-15–8 may be lead compounds that overcome acquired resistance to microtubule-targeting agents of cancer cells. Image 1 • AS1712 is active against broad cancer cell lines, even in drug resistant cells. • AS1712 is a low toxic colchicine-binding site inhibitor. • RJ-LC-15-8 had a greater anti-proliferative potency with a similar mechanism. • AS1712 and RJ-LC-15-8 can induce apoptosis in p-gp mediated MDR cells. • AS1712 and RJ-LC-15-8 have great potential for cancer therapy. [ABSTRACT FROM AUTHOR]