Competitive Manner Research Articles

ZNF480 Accelerates Chemotherapy Resistance in Breast Cancer by Competing With TRIM28 and Stabilizing LSD1 to Upregulate the AKT-GSK3β-Snail Pathway.

Zinc finger protein 480 (ZNF480) may interact with lysine-specific demethylase 1 (LSD1), which is highly expressed in many malignant tumors; however, ZNF480 expression has not previously been investigated in breast cancer. Therefore, we explored the expression and molecular mechanisms of ZNF480 in breast cancer. According to public databases and immunohistochemical staining analysis, ZNF480 is highly expressed in the tissue of patients with breast cancer, and ZNF480 expression is positively correlated with advanced TNM stage (p = 0.036), lymph node metastasis (p = 0.012), and poor prognosis (p = 0.005). ZNF480 overexpression enhances breast cancer cell proliferation, migration, and stemness by activating AKT-GSK3β-Snail signaling both in vitro and in vivo. Moreover, ZNF480 binds to LSD1 through its KRAB domain, thereby activating AKT signaling. Mass spectrometry and co-immunoprecipitation revealed that ZNF480 abrogates ubiquitination degradation and subsequently stabilizes LSD1 through competitive binding with TRIM28. Ipragliflozin was identified as a small-molecule inhibitor of ZNF480 and LSD1 interaction that may block breast cancer progression. Moreover, ZNF480 expression was significantly higher in treatment-resistant patients than in treatment-sensitive patients. Thus, ipragliflozin may neutralize neoadjuvant chemotherapy resistance induced by ZNF480 overexpression. Overall, elevated ZNF480 expression is positively associated with poor patient outcomes. Mechanistically, ZNF480 accelerates proliferation and neoadjuvant chemotherapy resistance in breast cancer cells via the AKT-GSK3β-Snail pathway by interacting with and stabilizing LSD1 in a competitive manner within TRIM28. This research has implications for developing targeted drugs against chemotherapy resistance in breast cancer.

100 μs Luminescence Lifetime Boosts the Excited State Reactivity of a Ruthenium(II)-Anthracene Complex in Photon Upconversion and Photocatalytic Polymerizations with Red Light.

The triplet excited state lifetime of a photosensitizer is an essential parameter for diffusion-controlled energy- and electron-transfer, which occurs usually in a competitive manner to the intrinsic decay of a triplet excited state. Here we show the decisive role of luminescence lifetime in the triplet excited state reactivity toward energy- and electron transfer. Anchoring two phenyl anthracene chromophores to a ruthenium(II) polypyridyl complex (RuII ref) leads to a RuII triad with a luminescence lifetime above 100 μs, which is more than 40 times longer than that of the prototypical complex. The obtained RuII triad sensitizes energy transfer to anthracene-based annihilators more efficiently than RuII ref and enables red-to-blue photon upconversion with a pseudo anti-Stokes shift of 0.94 eV and a moderate upconversion efficiency near 1 % in aerated solution. Particularly, RuII triad allows rapid photoredox catalytic polymerizations of acrylate and acrylamide monomers under aerobic condition with red light, which are kinetically hindered for RuII ref. Our work shows that excited state lifetime of a photosensitizer governs the dynamics of the excited state reactions, which seems an overlooked but important aspect for photochemistry.

Alpha-Glucosidase Inhibitory Effects of Flavonoids, Phenolic Acids and Iridoids Isolated From Vinca Soneri: In Vitro and In Silico Perspectives.

Various Vinca species have been traditionally used for their antihypertensive, sedative, and hemostatic properties, as well as for treating diabetes. In this study, some flavonoids, phenolic acids and iridoids were isolated from an endemic Vinca species, Vinca soneri for the first time. α-Glucosidase inhibitory effects of the isolates were tested and kaempferol-3-O-α-rhamnopyranosyl (1→6) β-galactopyranoside (1) was found to be the most active one with an IC50 value of 285.73 ±7.35 μM. Enzyme kinetic assay revealed that it inhibited α-glucosidase in competitive manner. Molecular geometry of 1 was predicted and Frontier molecular orbital analysis was performed using Density Functional Theory (DFT) calculations. Molecular docking and MM-GBSA calculations predicted good fit for 1 in the enzyme active site and key interactions with the catalytic residues. As a result, current study identifies 1 as a promising competitive α-glucosidase inhibitor to be developed as a potential antidiabetic drug candidate.

Design, synthesis and pharmacological evaluation of 1,2,3,4-tetrahydrobenzofuro[2,3-c]pyridine derivatives as p21-activated kinase 4 inhibitors for treatment of pancreatic cancer

The p21-activated kinase 4 (PAK4), a key regulator of malignancy, is negatively correlated with immune infiltration and has become an emergent drug target of cancer therapy. Given the lack of high efficacy PAK4 inhibitors, we herein reported the identification of a novel inhibitor 13 bearing a tetrahydrobenzofuro[2,3-c]pyridine tricyclic core and possessing high potency against MIA PaCa-2 and Pan02 cell lines with IC50 values of 0.38 and 0.50 μmol/L, respectively. This compound directly binds to PAK4 in a non-ATP competitive manner. In the mouse Pan02 model, compound 13 exhibited significant tumor growth inhibition at a dose of 100 mg/kg, accompanied by reduced levels of PAK4 and its phosphorylation together with immune infiltration in mice tumor tissue. Overall, compound 13 is a novel allosteric PAK4 inhibitor with a unique tricyclic structural feature and high potency both in vitro and in vivo, thus making it worthy of further exploration.

An Improved MOEA/D with an Auction-Based Matching Mechanism

Multi-objective optimization problems (MOPs) constitute a vital component in the field of mathematical optimization and operations research. The multi-objective evolutionary algorithm based on decomposition (MOEA/D) decomposes a MOP into a set of single-objective subproblems and approximates the true Pareto front (PF) by optimizing these subproblems in a collaborative manner. However, most existing MOEA/Ds maintain population diversity by limiting the replacement region or scale, which come at the cost of decreasing convergence. To better balance convergence and diversity, we introduce auction theory into algorithm design and propose an auction-based matching (ABM) mechanism to coordinate the replacement procedure in MOEA/D. In the ABM mechanism, each subproblem can be associated with its preferred individual in a competitive manner by simulating the auction process in economic activities. The integration of ABM into MOEA/D forms the proposed MOEA/D-ABM. Furthermore, to make the appropriate distribution of weight vectors, a modified adjustment strategy is utilized to adaptively adjust the weight vectors during the evolution process, where the trigger timing is determined by the convergence activity of the population. Finally, MOEA/D-ABM is compared with six state-of-the-art multi-objective evolutionary algorithms (MOEAs) on some benchmark problems with two to ten objectives. The experimental results show the competitiveness of MOEA/D-ABM in the performance of diversity and convergence. They also demonstrate that the use of the ABM mechanism can greatly improve the convergence rate of the algorithm.

The effects of Cannabis sativa and cannabinoids on the inhibition of pancreatic lipase – An enzyme involved in obesity

IntroductionObesity is a chronic noncommunicable disease characterized by excessive body fat that can have negative health consequences. Obesity is a complex disease caused by a combination of genetic, environmental, and lifestyle factors. It is characterized by a discrepancy between caloric intake and expenditure. Obesity increases the risk of acquiring major chronic diseases, including heart disease, stroke, cancer, and Type 2 diabetes mellitus (T2DM). Currently, the inhibition of pancreatic lipases (PL) is a promising pharmacological therapy for obesity and weight management. In this study, the inhibition of pancreatic lipase by Cannabis sativa (C. sativa) plant extract and cannabinoids was investigated. MethodsThe inhibitory effect was assessed using p-nitrophenyl butyrate (pNPB), and the results were obtained by calculating the percentage relative activity and assessed using one-way analysis of variance (ANOVA). Kinetic studies and spectroscopy techniques were used to evaluate the mode of inhibition. Diet-induced; and diabetic rat models were studied to evaluate the direct effects of C. sativa extract on PL activity. ResultsKinetic analyses showed that the plant extracts inhibited pancreatic lipase, with tetrahydrocannabinol (THC) and cannabinol (CBN) being the potential cause of the inhibition noted for the C. sativa plant extract. CBN and THC inhibited the pancreatic lipase activity in a competitive manner, with the lowest residual enzyme activity of 52 % observed at a 10 μg/mL concentration of CBN and 39 % inhibition at a 25 μg/mL concentration of THC. Circular dichroism (CD) spectroscopy revealed that the inhibitors caused a change in the enzyme's secondary structure. At low concentrations, THC showed potential for synergistic inhibition with orlistat. C.sativa treatment in an in vivo rat model confirmed its inhibitory effects on pancreatic lipase activity. ConclusionThe findings in this study provided insight into the use of cannabinoids as pancreatic lipase inhibitors and the possibility of using these compounds to develop new pharmacological treatments for obesity.

A common druggable signature of oncogenic c-Myc, mutant KRAS and mutant p53 reveals functional redundancy and competition among oncogenes in cancer

The major driver oncogenes MYC, mutant KRAS, and mutant TP53 often coexist and cooperate to promote human neoplasia, which results in anticancer therapeutic opportunities within their downstream molecular programs. However, little research has been conducted on whether redundancy and competition among oncogenes affect their programs and ability to drive neoplasia. By CRISPR‒Cas9-mediated downregulation we evaluated the downstream proteomics and transcriptomics programs of MYC, mutant KRAS, and mutant TP53 in a panel of cell lines with either one or three of these oncogenes activated, in cancers of the lung, colon and pancreas. Using RNAi screening of the commonly activated molecular programs, we found a signature of three proteins - RUVBL1, HSPA9, and XPO1, which could be efficiently targeted by novel drug combinations in the studied cancer types. Interestingly, the signature was controlled by the oncoproteins in a redundant or competitive manner rather than by cooperation. Each oncoprotein individually upregulated the target genes, while upon oncogene co-expression each target was controlled preferably by a dominant oncoprotein which reduced the influence of the others. This interplay was mediated by redundant routes of target gene activation - as in the case of mutant KRAS signaling to c-Jun/GLI2 transcription factors bypassing c-Myc activation, and by competition - as in the case of mutant p53 and c-Myc competing for binding to target promoters. The global transcriptomics data from the cell lines and patient samples indicate that the redundancy and competition of oncogenic programs are broad phenomena, that may constitute even a majority of the genes dependent on oncoproteins, as shown for mutant p53 in colon and lung cancer cell lines. Nevertheless, we demonstrated that redundant oncogene programs harbor targets for efficient anticancer drug combinations, bypassing the limitations for direct oncoprotein inhibition.

Advancing Alzheimer’s biomarker Detection: A hairpin Aptamer-Based competitive electrochemical biosensor for trace Amyloid beta 40 analysis

Accurate detection of Alzheimer’s disease (AD) core biomarkers in body fluid is critical for identifying latent asymptomatic AD patients and prediction AD progress. Amyloid beta 1–40 (Aβ-40) as one of the core biomarkers, is expected to be an early diagnostic indicator for AD. Here, we establish a competitive method based on hairpin-structured aptamer for rapid and highly sensitive detection of Aβ-40 using square wave voltammetry (SWV). A hairpin aptamer with redox-active moiety methylene blue (MB) are immobilized on a gold working electrode as a recognition element. In the detection, a short complementary oligonucleotide strand is first introduced to switch on the hairpin, whereafter the targets Aβ-40 join in and selectively react with the aptamer in a competitive manner with the complementary strand, leading to the changes in the proximity of MB to the electrode and thereby in the electrochemical signal. Various parameters such as aptamer concentration, complementary chain length, incubation time, and temperature were optimized to achieve maximum sensing performance. By introducing a complementary chain, the sensor significantly reduces the detection limit to 7.14 pg/mL, with a dynamic range of 20 pg/mL to 200 ng/mL. Additionally, high selectivity of the sensor for Aβ-40 monomer (Aβ-40 m) over other forms of Aβ peptides has been validated. The hairpin-mediated detection method enables rapid, facile and highly sensitive detection of Aβ-40 using low-cost screen-printed electrode (SPE) platform, providing a wide range of possibilities for the early diagnosis of AD in point-of-care technologies (POCT).

Edaravone N-benzyl pyridinium derivatives: BACE-1 inhibition, kinetics and in silico binding pose determination

BACE-1 plays a pivotal role in the production of β-amyloid (Aβ) peptides, implicated in Alzheimer's Disease (AD) pathology. We previously described edaravone N-benzyl pyridinium derivatives (EBPDs) that exhibited multifunctional activity against multiple AD targets. In this study we explored the EBPDs BACE-1 inhibitory activity to potentially enhance the compounds therapeutic profile. The EBPDs exhibited moderate BACE-1 inhibitory activity (IC50 = 44.10 µM - 123.70 µM) and obtained IC50 values between 2.0 and 5.8-fold greater than resveratrol, a known BACE-1 inhibitor (IC50 = 253.20 µM), in this assay. Compound 3 was the most potent inhibitor with an IC50 of 44.10 µM and a Ki of 19.96 µM and a mixed-type mode of inhibition that favored binding in a competitive manner. Molecular docking identified crucial interactions with BACE-1 active site residues, supported by 100 ns MD simulations. The study highlighted the EBPDs therapeutic potential as BACE-1 inhibitors and multifunctional anti-AD therapeutic agents.

Investigation of the surface charge behaviour of ettringite: Influence of pH, calcium, and sulphate ions

Ettringite is an important mineral that contributes to the overall performance of cementitious materials. Knowledge of the surface charge behaviour of a solid is necessary for a mechanistic description of surface processes such as adsorption or particle-particle interactions. The objective of this study was to develop a model capable of reproducing ettringite surface charge as a function of calcium, sulphate, and pH.Ettringite was synthesised and characterised using different analytical, microscopic, and spectroscopic techniques with the help of density functional theory. Electrophoretic mobility was measured using laser Doppler electrophoresis in alkaline waters representative of the cementitious environment.The behaviour of the ettringite surface charge was shown to be quite complex as sulphate and calcium acted in a competitive manner on the overall charge. The ζ-potential increases when the calcium content increases, whereas it decreases when sulphate increases. This is due to the possible adsorption of these ions at the surface, and the extent of the effect depends on the relative concentrations of Ca and SO42−.An electrostatic double layer model (DLM) was used to calculate the surface potential, considering the adsorption of both calcium and sulphate, as possible ions determining the potential (IDP), and formation of different complexes with ettringite surface functional groups (SOH). The variations of the ζ-potential could be satisfactorily predicted under the different chemical conditions of interest in a cementitious environment.

Design, synthesis, biological evaluation of a new tricyclicthiazolopy‐rimidinone derivatives as acetylcholinesterase inhibitors

AbstractThe novel serious of tricyclicthiazolo[5,4‐d]pyrimidinone were designed and synthesized as acetylcholinesterase (AChE) inhibitor agents. The main factors affecting the reactions of syntheses and the structure–activity relationships (SARs) were investigated as well. All compounds were confirmed by 1H NMR, 13C NMR, and HRMS. The in vitro enzyme assays proved that most of the compounds effectively inhibited AChE in the micromolar range with little cytotoxicity. Especially the compound G15 exhibited the best inhibitory activity against AChE with IC50 values of 4.41 ± 0.46 μM. Furthermore, kinetic analysis and molecular modeling studies pointed out the competitive inhibition manner of G15 on AChE. Thus, the derivative G15 can be considered a promising leading compound on AChE.

Exploring the mechanism and inhibitory effect of robinin on xanthine oxidase using multi-spectroscopy and molecular dynamics simulation methods

Xanthine oxidase (XOD) is a key enzyme in purine metabolism that is tightly associated with hyperuricemia (HUA). Natural flavonoids can inhibit XOD activity. In this study, the inhibitory activity and mechanism of the novel flavonoid robinin on XOD were analyzed using enzyme inhibition kinetics, multispectral techniques, molecular docking, and molecular dynamics (MD) simulations. Robinin reversibly inhibited the activity of XOD in a mixed competitive manner, with an IC50 value of 31.79 ± 0.15 μg/mL. Moreover, robinin spontaneously binds to a specific site on XOD and effectively quenches its intrinsic fluorescence via a single static quenching mechanism. The combination of XOD and robinin induced secondary structure rearrangement and conformational changes in XOD and prevented the entry of substrates, thus producing a strong inhibitory effect. Molecular docking and MD simulation revealed that robinin mainly binds to XOD through hydrogen bonding and hydrophobic interactions to form more stable complexes with a binding energy of −7.4 kcal/mol. Overall, this study established a theoretical reference for robinin as a promising natural XOD inhibitor for relieving HUA.

The National Bilingualism Plan (PNB) and the Challenge of Internationalization in Colombia: Background and Perspectives

This article intends to analyze the interdependence between the National Bilingualism Plan of Colombia and the challenge of internationalization of higher education in the country, as public policies that aim to improve the quality of education at different levels. The first focuses on strengthening the teaching of foreign languages in primary, basic, and secondary education; the latter, in higher education with the promotion of regional and global agreements for the recognition of studies, titles, and diplomas to promote access to greater academic and cultural ­opportunities for students, which would contribute to the economic development and the insertion of the country in the global context in a competitive manner. It aims to understand the challenge of internationalization and its deep connection with economic globalization and to establish its link with the teaching of foreign languages and the promotion of bilingualism. The National Bilingualism Plan and the development of the learning of foreign languages in Colombia are explored, and then the disconnection between both programs as a possible cause of the truncated development of bilingualism in the country is analyzed.

Zastaprazan: First Approval.

Zastaprazan (JAQBO®) is a next-generation potassium-competitive acid blocker being developed by Onconic Therapeutics, a subsidiary of Jeil Pharmaceutical, for the treatment of acid-related diseases. Zastaprazan binds directly to proton pumps in a competitive manner to reduce gastric acid secretion, allowing for a quick onset of action. On 24 April 2024, zastaprazan received approval in South Korea for the treatment of erosive gastroesophageal reflux disease (GERD). Zastaprazan is also undergoing phaseIII development for the treatment of gastric ulcer and for the prevention of non-steroidal anti-inflammatory drug (NSAID)-induced peptic ulcer. This article summarizes the milestones in the development of zastaprazan leading to this first approval for erosive GERD.

Discovery of novel benzimidazole derivatives as selective and reversible monoamine oxidase B inhibitors for Parkinson's disease treatment

Parkinson's disease (PD) is a common neurodegenerative disorder characterized by the loss of dopaminergic neurons in the substantia nigra pars compacta. The development of novel scaffolds for human monoamine oxidase B (hMAO-B) inhibitors with reversible properties represents an important strategy to improve the efficacy and safety for PD treatment. In the current work, we have devised and assessed two innovative derivative series serving as hMAO-B inhibitors. These series have utilized benzimidazole as a scaffold and strategically incorporated a primary amide group, which is recognized as a pivotal pharmacophore in subsequent activity screening and reversible mode of action. Among these compounds, 16d has emerged as the most potent hMAO-B inhibitor with an IC50 value of 67.3 nM, comparable to safinamide (IC50 = 42.6 nM) in vitro. Besides, 16d demonstrated good selectivity towards hMAO-B isoenzyme with a selectivity index over 387. Importantly, in line with the design purpose, 16d inhibited hMAO-B in a competitive and reversible manner (Ki = 82.50 nM). Moreover, 16d exhibited a good safety profile in both cellular and acute toxicity assays in mice. It also displayed ideal pharmacokinetic properties and blood-brain barrier permeability in vivo, essential prerequisites for central nervous system medicines. In the MPTP-induced PD mouse model, 16d significantly alleviated the motor impairment, especially muscle relaxation and motor coordination. Therefore, 16d, serving as a lead compound, holds instructive significance for subsequent investigations regarding its application in the treatment of PD.

Succinimide Derivatives as Acetylcholinesterase Inhibitors-In Silico and In Vitro Studies.

We studied the effect of succinimide derivatives on acetylcholinesterase activity due to the interest in compounds that influence this enzyme's activity, which could help treat memory issues more effectively. The following parameters were established for this purpose based on kinetic investigations of the enzyme in the presence of succinimide derivatives: the half-maximal inhibitory concentration, the maximum rate, the inhibition constant, and the Michaelis-Menten constant. Furthermore, computational analyses were performed to determine the energy required for succinimide derivatives to dock with the enzyme's active site. The outcomes acquired in this manner demonstrated that all compounds inhibited acetylcholinesterase in a competitive manner. The values of the docking energy parameters corroborated the kinetic parameter values, which indicated discernible, albeit slight, variations in the inhibitory intensity among the various derivatives.

Highly selective granulation adsorbents for lithium recovery from gas field brine: Selectivity, kinetics and mechanism

Polyvinyl chloride (PVC)-based granulated adsorbents with high mechanical stability have proven effective for extracting lithium from salt lake brine on a commercial scale. However, granular materials with high adsorption selectivity for Na+/Li+ separation and long service life still remain a great challenge. Here, we prepared granulated spherical adsorbents by a phase conversion method using PVC as a binder; PEG, PMMA, PAN, and PAA as hydrophilic co-binders; and Li1.33Mn1.67O4 (LMO) as a powder adsorbent. Among these materials, P-PAA exhibited excellent hydrophilicity and excellent binder compatibility, facilitating the dispersion of LMO powders and ensuring high adsorption. Moreover, the mechanism of action of the PVC/PAA binders was first explored via experiments and simulations, which revealed that Li+ migration was promoted and occurred primarily on LMO rather than on binders, so nonselective adsorption decreased. Therefore, P-PAA demonstrated exceptional Li+ adsorption capacity (12.9 mg/g) and selectivity for Li+ (distribution factor of 1391.3 mL/g) over other coexisting cations and a separation factor of αNaLi= 718, which are greater than those of other adsorbents reported in the literature. Furthermore, the unique structure of P-PAA, which was obtained by interconnecting larger core pores (5–10 μm) and abundant smaller pores (0.5–1 μm), accelerated the water/ion transfer kinetics without causing powder leakage. Hence, the lifespan of these materials has been extended, as salt crystals or internal cracks did not form during long-term cyclic use, unlike in the case of other granules. All of the above factors made P-PAA effectively recover Li+ from Puguang gas brine, which contains a high sodium salt content and organic pollutants, with an efficiency of 98.4 %. All these properties demonstrate that P-PAA could be used in an appealing and competitive manner for industrial processes.

Differential inhibition of sildenafil and macitentan on saxagliptin metabolism

The development of diabetes mellitus (DM) is generally accompanied by erectile dysfunction (ED) and pulmonary arterial hypertension (PAH), which increases the use of combination drug therapy and the risk of drug-drug interactions. Saxagliptin for the treatment of DM, sildenafil for the treatment of ED and PAH, and macitentan for the treatment of PAH are all substrates of CYP3A4, which indicates their potential involvement in drug-drug interactions. Therefore, we investigated potential pharmacokinetic interactions between saxagliptin and sildenafil/macitentan. We investigated this speculation both in vitro and in vivo, and explored the underlying mechanism using in vitro hepatic metabolic models and molecular docking assays. The results showed that sildenafil substantially inhibited the metabolism of saxagliptin by occupying the catalytic site of CYP3A4 in a competitive manner, leading to the alterations in the pharmacokinetic properties of saxagliptin in terms of increased maximum plasma concentration (Cmax), area under the plasma concentration–time curve from time 0 to 24 h (AUC(0-t)), area under the plasma concentration–time curve from time 0 extrapolated to infinite time (AUC(0-∞)), decreased clearance rate (CLz/F), and prolonged terminal half-life (t1/2). In contrast, a slight inhibition was observed in saxagliptin metabolism when concomitantly used with macitentan, as no pharmacokinetic parameters were altered, except for CLz/F. Thus, dosage adjustment of saxagliptin may be required in combination with sildenafil to achieve safe therapeutic plasma concentrations and reduce the risk of potential toxicity, but it is not necessary for co-administration with macitentan.

In vitro and in silico investigation of FDA-approved drugs to be repurposed against Alzheimer's disease.

Alzheimer's disease (AD), one of the main causes of dementia, is a neurodegenerative disorder. Cholinesterase inhibitors are used in the treatment of AD, but prolonged use of these drugs can lead to serious side effects. Drug repurposing is an approach that aims to reveal the effectiveness of drugs in different diseases beyond their clinical uses. In this work, we investigated in vitro and in silico inhibitory effects of 11 different drugs on cholinesterases. The results showed that trimebutine, theophylline, and levamisole had the highest acetylcholinesterase inhibitory actions among the tested drugs, and these drugs inhibited by 68.70 ± 0.46, 53.25 ± 3.40, and 44.03 ± 1.20%, respectively at 1000 µM. In addition, these drugs are bound to acetylcholinesterase via competitive manner. Molecular modeling predicted good fitness in acetylcholinesterase active site for these drugs and possible central nervous systemaction for trimebutine. All of these results demonstrated that trimebutine was determined to be the drug with the highest potential for use in AD.

A comparative study of Fe (II) doped chiral L/D-methionine carbon dots (MCDs) as a “Turn-on” fluorescent probe for the sensitive detection of L – cysteine

Chiral carbon dots have prominently influenced in the field of chemical, biological, and medicinal research. Comparing to achiral carbon dots, chiral carbon dots exhibit unique characteristics in biosensing application. In this perspective, we have developed bright blue, fluorescent L and d-Methionine Chiral carbon dots (MCDs) using a simple microwave assisted process for effective sensing of l-Cysteine. l-Cysteine plays a vital role in balancing the physiological redox in the body. These MCDs can be complexed with Fe2+ ions to create an energy transfer quenching system due to distinctive N and S functional group distribution on their surface. However, l-Cysteine attaches to Fe2+ ions in a competitive manner, leads to recovery of MCDs fluorescence. As a result, a "turn-on" fluorescent sensing platform based on L and d-Methionine-CDs has been developed for the rapid identification and detection of l-Cysteine. The probe shows good selectivity and sensitivity with coexisting biomolecules and ions. From comparative PL studies, d- MCDs are more responsive than l-Meth CDs towards the detection of l-cysteine with LOD of 0.71 µM and 0.94 µM respectively. The chiroptical properties were evaluated and the probe extends its practical application in paper strip and in biological matrix such as human blood serum with satisfactory recoveries in the range 85–104%.