Cyclin-Dependent Kinase 6 (CDK6) plays an important role in cancer progression, and thus, it is considered as an attractive drug target in anticancer therapeutics. This study presents an evaluation ...of dietary phytochemicals, capsaicin, tocopherol, rosmarinic acid, ursolic acid, ellagic acid (EA), limonene, caffeic acid, and ferulic acid for their potential to inhibit the activity of CDK6. Molecular docking and fluorescence binding studies revealed appreciable binding affinities of these compounds to the CDK6. Among them, EA shows the highest binding affinity for CDK6, and thus a molecular dynamics simulation study of 200 ns was performed to get deeper insights into the binding mechanism and stability of the CDK6-EA complex. Fluorescence binding studies revealed that EA binds to the CDK6 with a binding constant of
= 10
M
and subsequently inhibits its enzyme activity with an IC
value of 3.053 µM. Analysis of thermodynamic parameters of CDK6-EA complex formation suggested a hydrophobic interaction driven process. The treatment of EA decreases the colonization of cancer cells and induces apoptosis. Moreover, the expression of CDK6 has been downregulated in EA-treated human breast cancer cell lines. In conclusion, this study establishes EA as a potent CDK6 inhibitor that can be further evaluated in CDK6 directed anticancer therapies.
Folium artemisiae argyi (FAA) leaves have a long history of usage as a food colorant throughout China, but their usage as a biocolorant for textile substrates has not been fully exploited yet. The ...present research focused on the extraction of functional components of FAA leaves and their applications for simultaneous coloration and biofunctionalization of wool fabrics. Examination of different extracting solvents (ethanol/water combinations); identification and stability of color components using UV–vis, FT-IR, TG, and DTG; and examination of dyeing methods were successfully carried out during the course of this work. Additionally, the dyes extracted in different solvent systems were subjected to total phenolic and flavonoid content analysis and expressed as gallic acid and catechin equivalents, respectively. The different solvent extracts (50% aqueous ethanol in conjunction with small amounts of acid and alkali) gave the maximum biocolorant yield at 80 °C for 60 min. Wool fabrics dyed in different solvent systems gave different colors with good washing fastness. The inadequate fastness characteristics were evidently ameliorated by premordanting with Fe2+ and Al3+ salts. An adequate amount of FAA leaf extract on wool fabrics exhibited good UV protection, antibacterial, and antioxidant behaviors. Premordanting enhanced UV protection, antibacterial, and antioxidant behaviors of dyed wool fabrics. Wool fabrics treated with FAA leaf extracts exhibited diverse color variations (such as green color with alum mordant) and proved to be greatly promising for industrial application as a source of natural biocolorants, as well as a value-adding application for the plant in addition to its normal usage as a food colorant.
Recently, there has been an increasing interest towards the fabrication/finishing of bioactive materials using natural plant extracts, which can achieve a wide range of functional properties and ...environmental benefits. This study presents an environmentally benign bioactive finishing of wool fabric via the use of unexplored tannin-rich waste/fallen leaves extract of Chinese tallow/Sapium sebiferum L. through simple adsorption technique. Simple aqueous extraction followed by the evaluations of build-up properties on wool fabric using Chinese Tallow (CT) leaves extract were studied in due course of this study. Optimization of extraction and dyeing variables/conditions such as pH, temperature, CT concentration, and time were conducted using UV–Visible and reflectance spectral method. The nature of functional groups of the extracted dye were investigated through FT-IR spectral analysis with further in depth thermal analyses using TG and DSC measurements. Additionally, the extracted dye was subjected to quantitative analytical tests to check the relative amounts of total phenolics and flavonoid with respect to gallic acid and catechin equivalents, respectively. Build-up properties and fastness characteristics were studied in the presence and absence of mordants (two metal and one biomordant) under corresponding ISO standards. Results showed that wool fabric treated with CT leaves extract exhibit excellent antioxidant activity, good UV protection and high antibacterial activities against E. coli and S. aureus. The use of biomordant to alter the functional properties provide an eco-friendly method for wool finishing. In general, the treated wool fabric in this work has shown a promising future for the preparation of health and hygiene-related textile materials.
•An environmentally friendly benign cleaner production procedure has been presented.•Waste/fallen leaves of Sapium sebiferum L. were used for natural dye production.•Extracted dye was characterized by UV–visible and FT-IR analysis.•Potential antibacterial and antioxidant wool fabrics were produced.•Finished wool fabric possesses excellent UV protective properties.
The present study describes the use of Cinnamomum camphora waste/fallen leaves as an eco-friendly natural colorant for developing colorful and antibacterial wool fibers in view of growing ...environmental pollution and increasing needs for biomedical textiles in healthcare sector. Extraction of the natural colorant from C. camphora reddish colored/middle-aged waste/fallen leaves was carried out via simple water bath and ultrasound water bath extraction methods. While optimizing the colorant extraction in an aqueous solvent, ultrasound water bath provided enhanced extraction efficiency at pH 3, temperature of 70 °C, an initial dose level of 1.0 gm/50 ml of H2O, time of 80 min, and ultrasonic frequency of 80 kHz. Phytochemical analysis of extracted dye was successfully carried out using simple qualitative experimental analysis. The extracted colorants from C. camphora waste leaves were used to dye merino wool fibers through exhaustion dyeing technique. The optimal dyeing conditions, dye performances, and the ultrasonic effects were reported effectively. Build-up properties and fastness characteristics were studied in the presence and absence of mordants under corresponding ISO standards. Increasing ethanol concentration, increased discoloration properties of dyed wool fiber. Dyeing kinetics and dyeing rates under both simple water bath and ultrasound water bath conditions were compared. The structural and thermal changes in the dyed fibers under both conditions were analyzed using FT-IR, TG, and SEM analysis. An adequate amount of C. camphora leaves extract on wool fiber exhibited good antibacterial behaviors with high durability to increasing number of washing cycles. Premordanting with Cu2+, Fe2+, and Al3+ salts had a slightly negative effect on the antibacterial activity of dyed wool fibers but showed enhanced durability. Camphor waste leaves will prove great potential for industrial application as a source of natural colorant, as well as a value-adding application (biomedical textile) in addition to its normal usage.
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•This research presents an alternative use of C. camphora waste/fallen leaves.•Bioactive wool fiber was developed from the extracted anthocyanin dye components.•Pre-mordanting with different metal salts improved color parameters and wash fastness.•Resulting dyes exhibit good antibacterial properties with an inhibition of 79–95%.•Increasing ethanol concentration increased discoloration properties.
Methionine aminopeptidases (MetAPs) are attractive drug targets due to their essential role in eukaryotes as well as prokaryotic cells. In this study, biochemical assays were performed on newly ...synthesized Isatin-pyrazole hydrazones (PS1–14) to identify potent and selective bacterial MetAPs inhibitors. Compound PS9 inhibited prokaryotic MetAPs, i.e., MtMetAP1c, EfMetAP1a and SpMetAP1a with Ki values of 0.31, 6.93 and 0.37 µM, respectively. Interestingly, PS9 inhibited the human analogue HsMetAP1b with Ki (631.7 µM) about ten thousand-fold higher than the bacterial MetAPs. The in vitro screening against Gram-positive (Enterococcus faecalis, Bacillus subtilis and Staphylococcus aureus) and Gram-negative (Pseudomonas aeruginosa, Klebsiella pneumonia and Escherichia coli) bacterial strains also exhibited their antibacterial potential supported by minimum bactericidal concentration (MBC), disk diffusion assay, growth curve and time-kill curve experiments. Additionally, PS6 and PS9 had synergistic effects when combined with ampicillin (AMP) and ciprofloxacin (CIP) against selective bacterial strains. PS9 showed no significant cytotoxic effect on human RBCs, HEK293 cells and Galleria mellonella larvae in vivo. PS9 inhibited the growth of multidrug-resistant environmental isolates as it showed the MIC lower than the standard drugs used against selective bacterial strains. Overall, the study suggested PS9 could be a useful candidate for the development of antibacterial alternatives.
The recognition of the alarming increased cost and looming exhaustion of petroleum resources for the production of polymeric resins for versatile applications has prompted us to switch towards green ...and sustainable resources. There is an immediate urge to develop bio-based polymeric resins via sustainable routes with enhanced properties for their utilization in polymer and coating applications. The present investigation reports the synthesis and characterization of aliphatic amine, Hexamethylene tetramine (HMTA) modified Cardanol(Col)-Formaldehyde(F) (Col-FA) free standing films and coatings for versatile applications through the use of cost-effective and renewable starting material, Col (agro byproduct of cashew nut processing) and HMTA (optimum amount, 15%) obviating the toxic solvent usage. The result indicated transparent (red-yellow colored), homogenous Col-FA films with amorphous morphology, and can serve as an eco-friendly, thermally stable (up to 430–440 °C), chemically resistant (against various solvents), mechanically robust and biologically active (moderate activity) material. The overall synthesis strategy is environmentally benign, employs safer chemistry and is consistent with the principles of “Green Chemistry” (principles 1, 2, 3, 4, 5, 6, 7, 8, and 12). This is a highly desirable and excellent approach to develop free standing, transparent, flexible, thermally stable, chemically resistant and antibacterial thin films/coatings to increase the application of Col.
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•Aliphatic amine modified Cardanol (phenolic lipid)-Formaldehyde thin films were prepared by a cleaner and sustainable route via green chemistry principles.•Films/coatings obtained were transparent, reddish-yellow in color, flexible, chemically resistant, mechanically robust, and thermally stable.•Showed moderate antibacterial activity of Col-FA material against E. coli, S. aureus and B. substilis.•Can be safely employed up to 430–440 °C.
The current study deals with the use of Terminalia arjuna natural dye as an ecofriendly finishing agent for producing highly functional antimicrobial and fluorescent woolen yarn along with the ...evaluation of kinetic and thermodynamic adsorption characteristics. The effect of pH on the adsorption was investigated, showing an increase in adsorption capacity with decreasing pH over the range of 2–9, with maximum adsorption at pH 3.5. Two kinetic equations pseudo-first order and pseudo-second order were employed for determining adsorption rates. The pseudo-second order equation provided the best fit to experimental data with an activation energy of 105.58 kJ mol −1 , indicating chemisorption. The equilibrium adsorption data was fitted to Langmuir, Freundlich and Redlich–Peterson adsorption isotherms. The adsorption behavior accorded with the Redlich–Peterson isotherm with exceptionally high regression coefficients for dyeing temperatures of 50, 70 and 90 °C with dye concentration varying from 0.5–10% (o.w.f). Comparative results of the colorimetric properties (CIEL* a * b * and K / S ) using a spectrophotometer under D65 illuminant (10° standard observer) and color fastness (light, wash, and rub) of dyed woolen yarns were studied to quantify the effect of metal mordants. The antimicrobial potential of Terminalia arjuna solution and dyed woolen yarn were assessed in terms of percentage inhibition of bacterial growth against a wide variety of bacterial strains, showing more than 85% inhibition. Reduction in antimicrobial activity of dyed woolen yarn was observed with mordanted samples, however they were found to retain more antimicrobial activity as compared to unmordanted samples as a function of successive washing cycles. The chemical nature of different mordants and wool–mordant–dye complex forming ability were found to have significant impact on the colorimetric and fluorescence characteristics of dyed woolen yarn.
Prolactin inducible protein (PIP) is a small secretary glycoprotein present in most biological fluids and contributes to various cellular functions, including cell growth, fertility, antitumor, and ...antifungal activities.
The present study evaluated the antibacterial activities of recombinant PIP against multiple broad-spectrum MDR bacterial strains.
The PIP gene was cloned, expressed and purified using affinity chromatography. Disk diffusion, broth microdilution, and growth kinetic assays were used to determine the antibacterial activities of PIP.
: Disk diffusion assay showed that PIP has a minimum and maximum zone of inhibition against
and
, respectively, compared to the reference drug ampicillin. Furthermore, growth kinetics studies also suggested that PIP significantly inhibited the growth of
and
. The minimum inhibitory concentration of PIP was 32 µg/mL for
(443), a standard bacterial strain, and 64 µg/mL for
sp. (LG1), an environmental multidrug-resistant (MDR) strain. The synergistic studies of PIP with ampicillin showed better efficacies towards selected bacterial strains having MDR properties.
Our findings suggest that PIP has a broad range of antibacterial activities with important implications in alleviating MDR problems.
High susceptibility of wool toward bacterial growth owing to proteinous nature and moisture retention ability leads to need for antibacterial functionalization of wool to cure the resulting ...deterioration. Antibacterial colored wool was designed via application of Terminalia chebula, Alkanna tinctoria, and Tagetes erecta natural dyes. Characteristics in terms of color and antibacterial activity were compared to correlate coloring compound's effect on characteristics of dyes and, both T. chebula and A. tinctoria dyes inferred themselves actively resisting bacterial growth while T. erecta was not efficient against bacterial strains. Colorful shades of good color and fastness properties were obtained from selected natural dyes on woolen yarn. Results show Bacillus subtilis and Staphylococcus aureus (gram positive) were highly resisted by the effect of T. chebula and A. tinctoria dyes, and T. chebula among them proved best in terms of both color characteristics and antibacterial potential.
Cyclin-dependent kinase 6 (CDK6) is an important protein kinase that regulates cell growth, development, cell metabolism, inflammation, and apoptosis. Its overexpression is associated with ...reprogramming glucose metabolism through alternative pathways and apoptosis, which ultimately plays a significant role in cancer development. In the present study, we have investigated the structural and conformational changes in CDK6 at varying pH employing a multi-spectroscopic approach. Circular dichroism (CD) spectroscopy revealed at extremely acidic conditions (pH 2.0-4.0), the secondary structure of CDK6 got significantly disrupted, leading to aggregates formation. These aggregates were further characterized by employing Thioflavin T (ThT) fluorescence. No significant secondary structural changes were observed over the alkaline pH range (pH 7.0-11.0). Further, fluorescence and UV spectroscopy revealed that the tertiary structure of CDK6 was disrupted under extremely acidic conditions, with slight alteration occurring in mild acidic conditions. The tertiary structure remains intact over the entire alkaline range. Additionally, enzyme assay provided an insight into the functional aspect of CDK at varying pH; CDK6 activity was optimal in the pH range of 7.0-8.0. This study will provide a platform that provides newer insights into the pH-dependent dynamics and functional behavior of CDK6 in different CDK6 directed diseased conditions, viz. different types of cancers where changes in pH contribute to cancer development.
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