ChemInform Abstract: Synthesis of New N-Acylphenothiazinic Derivatives with Potential Activity in Chemotherapy.

Background: Monoclonal antibodies (mAbs) against cancer biomarkers are key reagents in diagnosis and therapy. One such relevant biomarker is a preferentially expressed antigen in melanoma (PRAME) that is selectively expressed in many tumors. Knowing mAb’s epitope is of utmost importance for understanding the potential activity and therapeutic prospective of the reagents. Methods: We generated a mAb against PRAME immunizing mice with PRAME fragment 161–415; the affinity of the antibody for the protein was evaluated by ELISA and SPR, and its ability to detect the protein in cells was probed by cytofluorimetry and Western blotting experiments. The antibody epitope was identified immobilizing the mAb on bio-layer interferometry (BLI) sensor chip, capturing protein fragments obtained following trypsin digestion and performing mass spectrometry analyses. Results: A mAb against PRAME with an affinity of 35 pM was obtained and characterized. Its epitope on PRAME was localized on residues 202–212, taking advantage of the low volumes and lack of fluidics underlying the BLI settings. Conclusions: The new anti-PRAME mAb recognizes the folded protein on the surface of cell membranes suggesting that the antibody’s epitope is well exposed. BLI sensor chips can be used to identify antibody epitopes.

Download Full-text

Microbiome of Seven Full-Scale Anaerobic Digestion Plants in South Korea: Effect of Feedstock and Operational Parameters

Energies ◽

10.3390/en14030665 ◽

2021 ◽

Vol 14 (3) ◽

pp. 665

Author(s):

Michal Sposob ◽

Hee-Sung Moon ◽

Dongjin Lee ◽

Yeo-Myeong Yun

Keyword(s):

Microbial Population ◽

Ammonium Nitrogen ◽

H2 Production ◽

Full Scale ◽

Organic Loading Rate ◽

Operational Parameters ◽

Sludge Digestion ◽

Secondary Sludge ◽

Potential Activity ◽

Total Ammonium

In this study, the microbiomes linked with the operational parameters in seven mesophilic full-scale AD plants mainly treating food waste (four plants) and sewage sludge (three plants) were analyzed. The results obtained indicated lower diversity and evenness of the microbial population in sludge digestion (SD) plants compared to food digestion (FD) plants. Candidatus Accumulibacter dominated (up to 42.1%) in SD plants due to microbial immigration from fed secondary sludge (up to 89%). Its potential activity in SD plants was correlated to H2 production, which was related to the dominance of hydrogenotrophic methanogens (Methanococcus). In FD plants, a balance between the hydrogenotrophic and methylotrophic pathways was found, while Flavobacterium and Levilinea played an important role during acidogenesis. Levilinea also expressed sensitivity to ammonia in FD plants. The substantial differences in hydraulic retention time (HRT), organic loading rate (OLR), and total ammonium nitrogen (TAN) among the studied FD plants did not influence the archaeal methane production pathway. In addition, the bacterial genera responsible for acetate production through syntrophy and homoacetogenesis (Smithella, Treponema) were present in all the plants studied.

Download Full-text

Antiulcerogenic Potential Activity of Free and NanoencapsulatedPassiflora serratodigitataL. Extracts

BioMed Research International ◽

10.1155/2014/434067 ◽

2014 ◽

Vol 2014 ◽

pp. 1-7 ◽

Cited By ~ 5

Author(s):

Marc Strasser ◽

Peky Noriega ◽

Raimar Löbenberg ◽

Nádia Bou-Chacra ◽

Elfriede M. Bacchi

Keyword(s):

Entrapment Efficiency ◽

Aqueous Solubility ◽

Residual Water ◽

Flavonoid Content ◽

Organic Extract ◽

Water Fraction ◽

Physical Chemical ◽

Potential Activity ◽

Antiulcerogenic Activity ◽

Herbal Formulations

This paper provides evidence that the leaves and stem ofPassiflora serratodigitataL. dry crude extract (DCE), ethylacetate fraction (EAF), and residual water fraction show potential antiulcerogenic activity. Interestingly, the polymeric nanocapsule loaded with EAF had 10-fold more activity than the free EAF. Furthermore, the polymer nanoparticles provided homogeneous colloidal drug delivery systems and allowed overcoming challenges such as poor aqueous solubility as well as the physical-chemical instability of the organic extract, which presented 90% (w/w) of the flavonoid content. The entrapment efficiency of the total flavonoid was 90.6 ± 2.5% (w/v) for the DCE and 79.9 ± 2.7% (w/v) for the EAF. This study shows that nanoencapsulation improves both the physicochemical properties and the efficacy of the herbal formulations. Therefore, free and encapsulated extracts have the potential to be suitable drug design candidates for the therapeutic management of ulcer.

Download Full-text

Accessibility and Intraurban Travel

Environment and Planning A Economy and Space ◽

10.1068/a190735 ◽

1987 ◽

Vol 19 (6) ◽

pp. 735-748 ◽

Cited By ~ 118

Author(s):

S Hanson ◽

M Schwab

Keyword(s):

Travel Behavior ◽

Activity Spaces ◽

Household Travel Survey ◽

Trip Frequency ◽

Potential Activity ◽

Using Data ◽

Household Travel ◽

Automobile Use ◽

The Relationship ◽

Travel Distances

This paper contains an examination of the fundamental assumption underlying the use of accessibility indicators: that an individual's travel behavior is related to his or her location vis-à-vis the distribution of potential activity sites. First, the conceptual and measurement issues surrounding accessibility and its relationship to travel are reviewed; then, an access measure for individuals is formulated. Using data from the Uppsala (Sweden) Household Travel Survey and controlling for sex, automobile availability, and employment status, the authors explore the relationship between both home- and work-based accessibility and five aspects of an individual's travel: mode use, trip frequencies and travel distances for discretionary purposes, trip complexity, travel in conjunction with the journey to work, and size of the activity space. From the results it can be seen that although all of these travel characteristics are related to accessibility to some degree, the travel–accessibility relationship is not as strong as deductive formulations have implied. High accessibility levels are associated with higher proportions of travel by nonmotorized means, lower levels of automobile use, reduced travel distances for certain discretionary trip purposes, and smaller individual activity spaces. Furthermore, the density of activity sites around the workplace affects the distances travelled by employed people for discretionary purposes. Overall, accessibility level has a greater impact on mode use and travel distance than it does on discretionary trip frequency. This result was unexpected in light of the strong trip frequency–accessibility relationship posited frequently in the literature.

Download Full-text

New Isolated Metschnikowia pulcherrima Strains from Apples for Postharvest Biocontrol of Penicillium expansum and Patulin Accumulation

Toxins ◽

10.3390/toxins13060397 ◽

2021 ◽

Vol 13 (6) ◽

pp. 397

Author(s):

Laura Settier-Ramírez ◽

Gracia López-Carballo ◽

Pilar Hernández-Muñoz ◽

Angélique Fontana ◽

Caroline Strub ◽

...

Keyword(s):

Liquid Medium ◽

Fungal Growth ◽

Its Region ◽

Antagonistic Activity ◽

Penicillium Expansum ◽

Metschnikowia Pulcherrima ◽

Potential Activity ◽

Different Strains ◽

Main Producer

Wild yeasts isolated from the surface of apples were screened for antagonistic activity against Penicillium expansum, the main producer of the mycotoxin patulin. Three antagonistic yeasts (Y33, Y29 and Y24) from a total of 90 were found to inhibit P. expansum growth. Identification by ITS region sequence and characterization showed that three selected isolates of yeast should be different strains of Metschnikowia pulcherrima. Several concentrations of the selected yeasts were used to study their in vitro antifungal effectivity against P. expansum on Petri dishes (plates with 63.6 cm2 surface) whereas their potential activity on patulin reduction was studied in liquid medium. Finally, the BCA that had the best in vitro antifungal capacity against P. and the best patulin degradation capacity was selected to be assessed directly on apples. All the selected strains demonstrated antifungal activity in vitro but the most efficient was the strain Y29. Isolated strains were able to reduce patulin content in liquid medium, Y29 being the only strain that completely reduced patulin levels within 120 h. The application of Y29 as biocontrol agent on the surface of apples inoculated with P. expansum, inhibited fungal growth and patulin production during storage. Therefore, the results shown that this yeast strain could be used for the reduction of P. expansum and its mycotoxin in apples or apple-based products by adapting the procedure application.

Download Full-text

Immobilization of Notch ligand, Delta-1, is required for induction of notch signaling

Journal of Cell Science ◽

10.1242/jcs.113.23.4313 ◽

2000 ◽

Vol 113 (23) ◽

pp. 4313-4318 ◽

Cited By ~ 11

Author(s):

B. Varnum-Finney ◽

L. Wu ◽

M. Yu ◽

C. Brashem-Stein ◽

S. Staats ◽

...

Keyword(s):

Cell Fate ◽

Extracellular Domain ◽

Notch Ligand ◽

Cell Fate Decisions ◽

Plastic Surface ◽

Ligand Stabilization ◽

Potential Activity ◽

Inhibition Of Differentiation ◽

Notch Ligands ◽

Notch Activation

Cell-cell interactions mediated by Notch and its ligands are known to effect many cell fate decisions in both invertebrates and vertebrates. However, the mechanisms involved in ligand induced Notch activation are unknown. Recently it was shown that, in at least some cases, endocytosis of the extracellular domain of Notch and ligand by the signaling cell is required for signal induction in the receptive cell. These results imply that soluble ligands (ligand extracellular domains) although capable of binding Notch would be unlikely to activate it. To test the potential activity of soluble Notch ligands, we generated monomeric and dimeric forms of the Notch ligand Delta-1 by fusing the extracellular domain to either a series of myc epitopes (Delta-1(ext-myc)) or to the Fc portion of human IgG-1 (Delta-1(ext-IgG)), respectively. Notch activation, assayed by inhibition of differentiation in C2 myoblasts and by HES1 transactivation in U20S cells, occurred when either Delta-1(ext-myc) or Delta-1(ext-IgG) were first immobilized on the plastic surface. However, Notch was not activated by either monomeric or dimeric ligand in solution (non-immobilized). Furthermore, both non-immobilized Delta-1(ext-myc) and Delta-1(ext-IgG) blocked the effect of immobilized Delta. These results indicate that Delta-1 extracellular domain must be immobilized to induce Notch activation in C2 or U20S cells and that non-immobilized Delta-1 extracellular domain is inhibitory to Notch function. These results imply that ligand stabilization may be essential for Notch activation.

Download Full-text

Bioactive Compounds, High Performance Liquid Chromatography Screening of Phenolic Compounds, and Antioxidant Potential Activity of Saffron (Crocus sativus L.)

Journal of Biobased Materials and Bioenergy ◽

10.1166/jbmb.2021.2106 ◽

2021 ◽

Vol 15 (5) ◽

pp. 700-704

Author(s):

Mohammed Saeed Alkaltham ◽

Khizar Hayat ◽

Mohammed Asif Ahmed ◽

Ahmad Mohammad Salamatullah ◽

Rokayya Sami ◽

...

Keyword(s):

Saudi Arabia ◽

Bioactive Compounds ◽

High Performance ◽

Antioxidant Activities ◽

Reducing Power ◽

Saudi Arabian ◽

Crocus Sativus ◽

Potential Activity ◽

Different Origins ◽

Crocus Sativus L

Saffron (Crocus sativus L) has been widely used for many therapeutic purposes such as a pain reliever, inflammation cure due to the highly bioactive compounds, and antioxidant activities. The effect of boiling time (5, 10, and 15 min) was investigated on the bioactive compounds of saffron samples from different origins (Spain, Saudi Arabia, and Afghanistan). Depending on the origin of the saffron sample, the extraction time showed a different effect on their total polyphenol content (TPC). The highest TPC was noted in saffron from Spain boiled for 10 min (45.01 mg GAE/g DW), followed by the sample from Saudi Arabia (44.03 mg GAE/g DW) and Afghanistan (43.54 mg GAE/g DW) boiled for 15 min, respectively. The Spanish saffron extracted for 10 min significantly (p < 0.05) exhibited the highest total flavonoid content (TFC) (12.26 mg CE/g DW), while the Saudi saffron extracted for 5 min (6.06 mg CE/g DW) showed the lowest range among all the samples. There were no significant differences among the reducing power of Saudi Arabian saffron extracted for 10 min, and Spanish saffron extracted for 5 and 15 min, respectively. The reducing power of saffron samples echoed the results of the TPC and TFC. 1,2-DHB (dihydroxy benzene), chlorogenic acid, caffeic acid are increased upon the increase of boiling time in Saudi Arabian saffron samples. In a word, 10 min and 15 min boiling times achieved the best extraction for Spanish saffron followed by Saudi and Afghani saffron samples, respectively.

Download Full-text