Thiol Drugs Research Articles

Investigating the Significances of Thiol Functionalities in SARS-CoV-2 Using Carbon Dots for Viral Inhibition.

While the World Health Organization has declared the end of the SARS-CoV-2 public health emergency, studies related to corona viruses are still under course. As of 2024, the severity of COVID-19 has diminished with current treatments and vaccinations. However, individuals can still face severe complications, highlighting the importance of ongoing research into innovative treatments for current and future coronavirus-related diseases. This study approaches the mechanism of viral entrance into the host cells and the current evidence on the use of sulfhydryl groups for the COVID-19 treatment. Certain thiol drugs, a key contributor to inflammatory processes, exhibit both viral inhibition properties and the potential to regulate cellular oxidative stress by scavenging free radicals. Herein, we developed biocompatible thiol-functionalized carbon dots (CDs) and investigated the correlation between the number of thiols and pseudo-SARS-CoV-2 inhibition, reactive oxygen species (ROS) scavenging, and anti-inflammatory response. The free-radical scavenging experiment and the ROS cellular assay indicate that thiolated CDs serve as effective reducing agents and potential regulators of cellular oxidative stress. The CDs also demonstrated good cell viability alongside significant antiviral capabilities, with inhibition levels up to 60.4%. Furthermore, the flow cytometry results suggest that in an inflammatory environment, the presence of thiolated CDs promotes an anti-inflammatory response. Overall, the results demonstrate a strong correlation between the number of thiols and the increased efficacy observed across experiments, presenting thiolated CDs as promising candidates to prevent and treat COVID-19 infection.

Molecular identification of missense variants in SLC3A1 gene; an approach leading to computer-aided drug design for cystinuria

Cystinuria is a rare congenital disorder characterized by the formation of cystine stones in urinary system, mainly kidneys and urinary tract. It follows the autosomal recessive inheritance pattern, where both of the parents contain the mutant allele. Cystine is an oxidized dimeric form of amino acid cysteine, shining crystal of greenish-yellow color sized greater than 5 mm. A minor genetic defect in SLC3A1 gene, downregulate the cystine transporter, rBAT protein, to absorb cystine and other dibasic amino acids in proximal tubule of nephron, causing Cystinuria. Computational and molecular analysis of SLC3A1 gene was performed to identify the deleterious missense single nucleotide variations (mSNVs) linked with Cystinuria in Pakistani population. In silico analysis of whole SLC3A1 gene nsSNPs has revealed that the exon 1, 6 and 10 are the hotspot areas, which potentially alter the protein structure and function. Three SNVs including one synonymous SNV A186C in exon 1, and two mSNVs including G314T in exon 1 and G44972A in exons 10 were identified. Both mSNVs were confirmed by ARMS PCR in all the 68 samples. The results have shown that 10% of the patients have G314T, 16% have G44972A and 74% of the patients have both of these mSNVs. Both of these mSNVs were involved in the structural and functional deterioration of rBAT protein. Additionally, computer aided drug designing tools were used to design diaminobenzylpyrimidine drug around the mutant residues which exhibit the lowest binding affinity with the target as compared to the previously reported cystine binding thiol drugs. In future, the present study could be extended to a large scale for mass screening of reported SNVs and mSNVs which, ultimately, lead to the development of knockouts for the functional studies and treatments.

Self-Assembly of Cysteine into Nanofibrils Precedes Cystine Crystal Formation: Implications for Aggregation Inhibition.

The self-association of metabolites into well-ordered assemblies at the nanoscale has significant biological and medical implications. The thiol-containing amino acid cysteine (CYS) can assemble into amyloid-like nanofibrils, and its oxidized form, the disulfide-bonded cystine (CTE), forms hexagonal crystals as those found in cystinuria due to metabolic disorder. Yet, there have been no attempts to connect these two phenomena, especially the fibril-to-crystal transition. Here, we reveal that these are not separated events, and the CYS-forming amyloid fibrils are mechanistically linked to hexagonal CTE crystals. For the first time, we demonstrated that cysteine fibrils are a prerequisite for forming cystine crystals, as observed experimentally. To further understand this mechanism, we studied the effects of thiol-containing cystinuria drugs (tiopronin, TIO; and d-penicillamine, PEN) and the canonical epigallocatechin gallate (EGCG) amyloid inhibitor on fibril formation by CYS. The thiol-containing drugs do not solely interact with monomeric CYS via disulfide bond formation but can disrupt amyloid formation by targeting CYS oligomers. On the other hand, EGCG forms inhibitor-dominant complexes (more than one EGCG molecule per cysteine unit) to prevent CYS fibril formation. Interestingly, while CYS can be oxidized into CTE, the thiol drugs can reduce CTE back to CYS. We thus suggest that the formation of crystals in cystinuria could be halted at the initial stage by targeting CYS fibril formation as an alternative to solubilizing the water-insoluble hexagonal CTE crystals at a later stage. Taken together, we depicted a complex hierarchical organization in a simple amino acid assembly with implications for therapeutic intervention.

Investigation of Bucillamine as anti-COVID-19 drug: DFT study, molecular docking, molecular dynamic simulation and ADMET analysis

The novel coronavirus disease-2019 (COVID-19), caused by SARS-CoV-2, is a global health pandemic beginning in early December 2019 in Wuhan, Hubei province, China. The effective drug target among coronaviruses is the SARS-CoV-2 main protease (Mpro), because of its crucial role in processing viral polyproteins translated from the viral RNA. In this study, the bioactivity of the selected thiol drug named Bucillamine (BUC) was evaluated as a potential drug for COVID-19 treatment by using computational modeling strategies. First, the molecular electrostatic potential density (ESP) calculation was performed to estimate the chemically active atoms of BUC. Additionally, BUC was docked to the Mpro (PDB: 6LU7) to evaluate the protein–ligand binding affinities. Besides, the estimated ESP results by density functional theory (DFT) were used to illustrate the molecular docking findings. Moreover, the frontier orbitals analysis was calculated to determine the charge transfer between the Mpro and BUC. Then, the stability of protein–ligand complex was subjected to the molecular dynamic simulations. Finally, an in silico study was performed to predict drug-likeness and absorption, distribution, metabolism, excretion and toxicity profiles (ADMET) of BUC. These results propose that BUC can be a potential drug candidate against the COVID-19 disease progression. Communicated by Ramaswamy H. Sarma

Accurate 24-h urine cystine quantification for patients on cystine-binding thiol drugs

Cystinuria is a rare disorder resulting in development of recurrent kidney stones, adversely affecting patient quality of life. The goal of cystinuria management is to reduce stone formation by increasing cystine solubility in urine, which includes lowering the urinary cystine level below its solubility limit. Treatment usually involves alkalinization of the urine and often requires initiating pharmacotherapy with a cystine-binding thiol drug (CBTD) such as tiopronin; however, proper dose adjustment requires accurate measurement of urinary cystine. The goal of this study was to validate a novel high-performance liquid chromatography tandem mass spectrometry (HPLC–MS/MS) method for quantification of cystine in the urine of patients with cystinuria receiving a CBTD. Urine samples were collected over 24 h from 24 patients and separated into 2 aliquots. Chromatographic separation of samples was conducted and separation of cystine from the cysteine-tiopronin drug complex was complete in < 3 min. The method was validated for accuracy, precision, linearity, limit of detection (LOD), and limit of quantification (LOQ). Mean accuracy range was 97.7–102.3%; intermediate precision was high with relative percent difference values calculated at 1.2–9.3%; the calibration curve resulted in a linear response throughout the concentration range (R2 = 0.998); and the LOD and LOQ were 0.002 and 0.005 mg/mL, respectively. Mean (range) cystine concentrations measured were 111.10 (51.31–179.46) and 242.21 (61.14–741.80) g/L in Aliquots A and B, respectively. The HPLC–MS/MS method presented here indicates that urine cystine can be reliably quantified in patients receiving a CBTD.

Exploring antiviral and anti-inflammatory effects of thiol drugs in COVID-19.

The redox status of the cysteine-rich SARS-CoV-2 spike glycoprotein (SARS-2-S) is important for the binding of SARS-2-S to angiotensin-converting enzyme 2 (ACE2), suggesting that drugs with a functional thiol group ("thiol drugs") may cleave cystines to disrupt SARS-CoV-2 cell entry. In addition, neutrophil-induced oxidative stress is a mechanism of COVID-19 lung injury, and the antioxidant and anti-inflammatory properties of thiol drugs, especially cysteamine, may limit this injury. To first explore the antiviral effects of thiol drugs in COVID-19, we used an ACE-2 binding assay and cell entry assays utilizing reporter pseudoviruses and authentic SARS-CoV-2 viruses. We found that multiple thiol drugs inhibit SARS-2-S binding to ACE2 and virus infection. The most potent drugs were effective in the low millimolar range, and IC50 values followed the order of their cystine cleavage rates and lower thiol pKa values. To determine if thiol drugs have antiviral effects in vivo and to explore any anti-inflammatory effects of thiol drugs in COVID-19, we tested the effects of cysteamine delivered intraperitoneally to hamsters infected with SARS-CoV-2. Cysteamine did not decrease lung viral infection, but it significantly decreased lung neutrophilic inflammation and alveolar hemorrhage. We speculate that the concentration of cysteamine achieved in the lungs with intraperitoneal delivery was insufficient for antiviral effects but sufficient for anti-inflammatory effects. We conclude that thiol drugs decrease SARS-CoV-2 lung inflammation and injury, and we provide rationale for future studies to test if direct (aerosol) delivery of thiol drugs to the airways might also result in antiviral effects.

Exploring antiviral and anti-inflammatory effects of thiol drugs in COVID-19 (Supplementary file)

Exploring antiviral and anti-inflammatory effects of thiol drugs in COVID-19 (Supplementary file)

Bucillamine in the treatment of patients with mild to moderate COVID-19: an interview with Michael Frank.

Bucillamine in the treatment of patients with mild to moderate COVID-19: an interview with Michael Frank.

Development and Validation CFIA / MZ System as a Green Method for Determination of Thiol Drug (D-PEN)

A simple, automated and sensitive continues flow-injection analysis/merging zones technique (CFIA/MZ) method was developed for the determination of D-Penicillamine (thiol drug) in pure, pharmaceutical formulations and biological sample. This method involved the reaction of 1,2-Naphthoquinone-4-Sulphonic acid Sodium Salt (NQS) with D-Penicillamine to produce a brawn-colored complex which has maximum absorbance at 463nm. The method was cheap, economic, precise and accurate where the limit of detection was 6.3 µg.mL-1 and the RSD% was 0.34 and Recovery was 99.31%. Various chemical and physical conditions that affected the reaction have been studied. A wide calibration curve was rectilinear within the concentration range (15-1000) μg.mL-1 with a sample through put of 103 sample.hour-1. The proposed procedure was applied successfully for the estimation of PEN in pharmaceutics and biological sample and the results obtained were favorably compared with those given by a reference method of United States Pharmacopoeia (USP), and there was no significant difference between the obtained results, regarding accuracy and precision at the 95% confidence level.

Update on cystine stones: current and future concepts in treatment.

Cystine stones are relatively uncommon compared with other stone compositions, constituting just 1% to 2% of adult urinary tract stone diseases, and accounting for up to 10% of pediatric stone diseases. Two responsible genes of cystinuria have been identified, the SLC3A1 and the SLC7A9. Cystinuria is diagnosed by family history, stone analysis, or by measurement of urine cystine excretion. Current treatments for cystinuria include increased fluid intake to increase cystine solubility by maintaining daily urine volume of greater than 3 Liter (L). Limiting sodium and protein intake can decrease cystine excretion. When conservative therapy fails, then pharmacologic therapy may be effective. Alkaline urine pH in the 7.0-7.5 range will reduce cystine solubility and can be achieved by the addition of alkali therapy. If these measures fail, cystine-binding thiol drugs such as tiopronin and D-penicillamine are considered. These compounds bind cysteine and prevent the formation of less soluble cystine. These drugs, however, have poor patient compliance due to adverse effects. Captopril can be useful in the treatment of cystine stones but the drug has not been tested in rigorous clinical trials. Novel potential therapies such as alpha-lipoic acid and crystal growth inhibitors (L-cystine dimethyl ester (L-CDME) and L-cystine methyl ester (L-CME)) were developed and tested in animals. Those therapies showed promising results. Compliance with treatment was associated with a lower rate of cystine stone formation.

Medicinal Thiols: Current Status and New Perspectives.

The thiol (-SH) functional group is found in a number of drug compounds and confers a unique combination of useful properties. Thiol-containing drugs can reduce radicals and other toxic electrophiles, restore cellular thiol pools, and form stable complexes with heavy metals such as lead, arsenic, and copper. Thus, thiols can treat a variety of conditions by serving as radical scavengers, GSH prodrugs, or metal chelators. Many of the compounds discussed here have been in use for decades, yet continued exploration of their properties has yielded new understanding in recent years, which can be used to optimize their clinical application and provide insights into the development of new treatments. The purpose of this narrative review is to highlight the biochemistry of currently used thiol drugs within the context of developments reported in the last five years. More specifically, this review focuses on thiol drugs that represent the standard of care for their associated conditions, including N-acetylcysteine, 2,3-meso-dimercaptosuccinic acid, British anti-Lewisite, D-penicillamine, amifostine, and others. Reports of novel dosing regimens, delivery strategies, and clinical applications for these compounds were examined with an eye toward emerging approaches to address a wide range of medical conditions in the future.

Evaluation and Medical Management of Patients with Cystine Nephrolithiasis: A Consensus Statement.

Purpose: Cystinuria is a genetic disorder with both autosomal recessive and incompletely dominant inheritance. The disorder disrupts cystine and other dibasic amino acid transport in proximal tubules of the kidney, resulting in recurrent kidney stone formation. Currently, there are no consensus guidelines on evaluation and management of this disease. This article represents the consensus of the author panel and will provide clinicians with a stepwise framework for evaluation and clinical management of patients with cystinuria based on evidence in the existing literature. Materials and Methods: A search of MEDLINE®/PubMed® and Cochrane databases was performed using the following key words: "cystine nephrolithiasis," "cystinuria," "penicillamine, cystine," and "tiopronin, cystine." In total, as of May 2018, these searches yielded 2335 articles, which were then evaluated for their relevance to the topic of evaluation and management of cystinuria. Evidence was evaluated by the Grading of Recommendations Assessment, Development, and Evaluation (GRADE) system. Results: Twenty-five articles on the topic of cystinuria or cystine nephrolithiasis were deemed suitable for inclusion in this study. The literature supports a logical evaluation process and step-wise treatment approach beginning with conservative measures: fluid intake and dietary modification. If stone formation recurs, proceed to pharmacotherapeutic options by first alkalinizing the urine and then using cystine-binding thiol drugs. Conclusions: The proposed clinical pathways provide a framework for efficient evaluation and treatment of patients with cystinuria, which should improve overall outcomes of this rare, but highly recurrent, form of nephrolithiasis.

Pemphigus foliaceus in a patient with gastrointestinal stromal tumor treated with adjuvant imatinib mesylate

Pemphigus is an autoimmune bullous disease with a number of described associations, including medications, which have been grouped into three structural categories - thiol drugs, phenol drugs, and drugs with neither functional group [1]. Discontinuation of the offending medication is considered a mainstay of therapy. We report a patient in whom the onset of pemphigus foliaceus was associated with initiation of imatinib mesylate adjuvant therapy in a patient with resected gastrointestinal stromal tumor (GIST). Imatinib was continued because of the survival benefit to the patient with a resected, high risk GIST. Treatment with rituximab resulted in near resolution of his blistering rash and follow up enzyme-linked immunosorbent assay (ELISA) demonstrated reference range immunoreactivity for both desmoglein 1 and desmoglein 3. After dose increase of imatinib therapy owing to tumor growth, the patient subsequently again developed a similar eruption. Re-biopsy and ELISA were consistent with recurrence of pemphigus. In conclusion, although the patient's pemphigus was cleared with a single cycle of rituximab infusions while continuing imatinib therapy, the disease returned after imatinib dose was increased a year later, suggesting a dose-response relationship.

Effect of nanodiamond surface chemistry on adsorption and release of tiopronin

Tiopronin is an FDA-approved thiol drug currently used to treat cystinuria and rheumatoid arthritis. However, due to its antioxidant properties, it may be beneficial in a variety of other conditions. One primary obstacle to its wider application is its limited bioavailability, which necessitates administration of high systemic doses to achieve localized therapeutic effects. Incorporation of a drug delivery vehicle can solve this dilemma by providing a means of controlled, targeted release. Functionalized nanodiamond is a promising theranostic platform that has demonstrated great potential for biomedical applications, including drug delivery. Design of nanodiamond theranostic platforms requires comprehensive understanding of drug-platform interactions, and the necessary physical chemical investigations have only been realized for a limited number of compounds. Towards the long-term goal of developing a nanodiamond-tiopronin treatment paradigm, this study aims to shed light on the effects of nanodiamond surface chemistry on adsorption and release of tiopronin. Specifically, adsorption isotherms were measured and fit to Langmuir and Freundlich models for carboxylated, hydroxylated, and aminated nanodiamonds, and release was monitored in solutions at pH 4.0, 5.8, 7.3, and 8.1. Our results indicate that aminated nanodiamonds exhibit the highest loading capacity while hydroxylated nanodiamonds are the most effective for sustained release. Therefore, a high degree of flexibility may be afforded by the use of nanodiamonds with different surface chemistries optimized for specific applications.

Re: Urine Proteomic Profiling in Patients with Nephrolithiasis and Cystinuria.

No AccessJournal of UrologyUrological Survey1 Jul 2019Re: Urine Proteomic Profiling in Patients with Nephrolithiasis and Cystinuria Dean G. AssimosMD Dean G. AssimosDean G. Assimos More articles by this author View All Author Informationhttps://doi.org/10.1097/JU.0000000000000265AboutFull TextPDF ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareFacebookLinked InTwitterEmail "Re: Urine Proteomic Profiling in Patients with Nephrolithiasis and Cystinuria." The Journal of Urology, 202(1), p. 25 Suggested Reading : Do urinary cystine parameters predict clinical stone activity?J Urol 2018; 199: 495. Link, Google Scholar : The interaction of thiol drugs and urine pH in the treatment of cystinuria. J Urol 2013; 189: 2147. Link, Google Scholar : Penicillamine therapy for pediatric cystinuria: experience from a cohort of American children. J Urol 2008; 180: 2620. Link, Google Scholar © 2019 by American Urological Association Education and Research, Inc.FiguresReferencesRelatedDetails Volume 202Issue 1July 2019Page: 25-25 Advertisement Copyright & Permissions© 2019 by American Urological Association Education and Research, Inc.MetricsAuthor Information Dean G. Assimos More articles by this author Expand All Advertisement Loading ...

Effect of increasing doses of cystine-binding thiol drugs on cystine capacity in patients with cystinuria.

Appropriate dosing of cystine-binding thiol drugs in the management of cystinuria has been based on clinical stone activity. When new stones form, the dose is increased. Currently, there is no method of measuring urinary drug levels to guide the titration of therapy. Increasing cystine capacity, a measure of cystine solubility, has been promoted as a method of judging the effects of therapy. In this study, we gave increasing doses of tiopronin or D-penicillamine, depending on the patients' own prescriptions, to ten patients with cystinuria and measured cystine excretion and cystine capacity. The doses were 0, 1, 2, 3g per day, given in two divided doses, and administered in a random order. Going from 0 to 1g/day led to an increase in cystine capacity from - 39.1 to 130.4mg/L (P < 0.009) and decreased 24h cystine excretion from 1003.9 to 834.8mg/day (P = 0.039). Increasing the doses from 1 to 2 to 3g/day had no consistent or significant effect to further increase cystine capacity or decrease cystine excretion. Whether doses higher than 1g/day have additional clinical benefit is not clear from this study. Limiting doses might be associated with fewer adverse effects without sacrificing the benefit of higher doses if higher doses do not offer clinical importance. However, trials with stone activity as an outcome would be desirable.

Cystinuria: genetic aspects, mouse models, and a new approach to therapy.

Cystinuria, a genetic disorder of cystine transport, is characterized by excessive excretion of cystine in the urine and recurrent cystine stones in the kidneys and, to a lesser extent, in the bladder. Males generally are more severely affected than females. The disorder may lead to chronic kidney disease in many patients. The cystine transporter (b0,+) is a heterodimer consisting of the rBAT (encoded by SLC3A1) and b0,+AT (encoded by SLC7A9) subunits joined by a disulfide bridge. The molecular basis of cystinuria is known in great detail, and this information is now being used to define genotype-phenotype correlations. Current treatments for cystinuria include increased fluid intake to increase cystine solubility and the administration of thiol drugs for more severe cases. These drugs, however, have poor patient compliance due to adverse effects. Thus, there is a need to reduce or eliminate the risks associated with therapy for cystinuria. Four mouse models for cystinuria have been described and these models provide a resource for evaluating the safety and efficacy of new therapies for cystinuria. We are evaluating a new approach for the treatment of cystine stones based on the inhibition of cystine crystal growth by cystine analogs. Our ongoing studies indicate that cystine diamides are effective in preventing cystine stone formation in the Slc3a1 knockout mouse model for cystinuria. In addition to crystal growth, crystal aggregation is required for stone formation. Male and female mice with cystinuria have comparable levels of crystalluria, but very few female mice form stones. The identification of factors that inhibit cystine crystal aggregation in female mice may provide insight into the gender difference in disease severity in patients with cystinuria.

77 - Nanodiamonds as antioxidant carriers: applications for drug delivery

Tiopronin is a small-molecular weight thiol drug used clinically to treat cystinuria and rheumatoid arthritis. Its thiol moiety confers antioxidant properties, enabling it to scavenge free radicals as well as reduce and chelate transition metal ions, and undergo thiol-disulfide exchange, which can serve to spare or restore levels of endogenous thiols, including GSH. Its primary metabolite, thiolactic acid (TLA) retains these properties. In addition, experiments conducted in our lab suggest that both the DPPH radical scavenging and CUPRAC reducing power of tiopronin and TLA exceed that of the well-known and widely used N-acetylcysteine (NAC). Thus, tiopronin possesses several characteristics that make it an attractive candidate for development as a treatment for oxidative stress-related conditions, such as cataracts. However, its labile thiol group represents a double-edged sword for implementation in living systems and ultimately the clinic because thiol drugs are often oxidized before they reach the proposed site of action, rendering them ineffective or even detrimental. Therefore, drug delivery strategies can be employed to safeguard and mediate sustained release of tiopronin. For this purpose, nanodiamonds represent a nearly ideal platform, as they are inert and biocompatible, with highly tailorable surface chemistry and extremely favorable surface area-to-mass ratio. Moreover, preliminary results in our laboratory suggest that detonation nanodiamonds synergistically increase the radical scavenging ability of tiopronin. Comparisons between nanodiamonds with different surface functionalization and specific current and potential applications will be discussed.

P-398 - Thiols as antioxidant drugs

Drugs containing the thiol moiety (or those metabolized to thiol-containing species) play important and diverse roles in biological systems. Thiols are highly sensitive to the redox environment and form stable disulfide bonds upon oxidation. Thiol drugs exhibit mucolytic and antiurolithic activity, as well as the ability to chelate heavy metals such as lead and mercury. In addition, thiol drugs have untapped potential as primary and adjuvant therapies in a wide variety of oxidative stress-related conditions. Thiol drugs bolster GSH levels following acetaminophen overdose, protect tissues against free radical attack after ionizing radiation exposure, and may mitigate lens protein disruption in cataract. Moving forward, chemical alterations or drug delivery strategies may further improve the effectiveness of thiol drugs by increasing bioavailability while reducing systemic side-effects. This presentation will highlight research on the effects of thiol drugs in conditions with therapeutically exploitable redox dysregulation, including heavy metal toxicity, radiation poisoning, acetaminophen toxicity, cataracts and others.

Optical Detection of Thiol Drugs by Core–Shell Luminous Carbon Dots—Gold Nanoparticles System

Nowadays, carbon quantum dots (CQDs) with size less than 10 nm have emerged as one of the most exciting areas of chemical research in the class of inorganic nanomaterials. This article presents interesting characteristics of CQDs and their fluorescence turn-on/turn-off quenching for the detection of 6-Thioguanine (6-TG). The CQDs were fabricated by a simple one-step microwave technique and used for the simultaneous reduction of Au3+ to form Au0-CQD core–shell (Au@CQD) nanocomposites. The CQDs formed were spherical in shape having an average size of ~ 7 nm confirmed by high-resolution transmission electron microscopy (HRTEM) and DLS study. The interaction of CQDs with Au leads to its fluorescence turn-off up to 96% analyzed by UV-visible, fluorescence spectroscopy, and fluorescence lifetime measurements. The turn-on fluorescence of CQDs has been witnessed by the formation of complex with 6-TG [Au-(6-TG)n]3− in the presence of thiols. Meanwhile, linear relationship between turn-on fluorescence against the concentration of 6-TG is obtained in the range of 0–100 μM with the correlation coefficient of 0.9944 and limit of detection for 6-TG has been found to be 0.01 μM. The Au@CQDs could also act as biosensor for the detection of various amino acids, enzymes, and pentids drug.