human serum albumin
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2022 ◽  
Vol 146 ◽  
pp. 112513
Author(s):  
Erzsébet Pászti-Gere ◽  
Anna Szentkirályi ◽  
Zsófia Fedor ◽  
Gábor Nagy ◽  
Zoltán Szimrók ◽  
...  

2022 ◽  
Vol 1249 ◽  
pp. 131550
Author(s):  
Afreen Banu ◽  
Rizwan Hasan Khan ◽  
Mohssen T.A. Qashqoosh ◽  
Yahiya Kadaf Manea ◽  
Mohammad Furkan ◽  
...  

Toxins ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 56
Author(s):  
Justin B. Renaud ◽  
Jacob P. Walsh ◽  
Mark W. Sumarah

Aflatoxins B1 (AFB1) and G1 (AFG1) are carcinogenic mycotoxins that contaminate crops such as maize and groundnuts worldwide. The broadly accepted method to assess chronic human aflatoxin exposure is by quantifying the amount of aflatoxin adducted to human serum albumin. This has been reported using ELISA, HPLC, or LC-MS/MS to measure the amount of AFB1-lysine released after proteolysis of serum albumin. LC-MS/MS is the most accurate method but requires both isotopically labelled and unlabelled AFB1-lysine standards, which are not commercially available. In this work, we report a simplified synthetic route to produce unlabelled, deuterated and 13C6 15N2 labelled aflatoxin B1-lysine and for the first-time aflatoxin G1-lysine. Additionally, we report on the stability of these compounds during storage. This simplified synthetic approach will make the production of these important standards more feasible for laboratories performing aflatoxin exposure studies.


2022 ◽  
Vol 23 (2) ◽  
pp. 719
Author(s):  
Yeonje Cho ◽  
Armin Mirzapour-Kouhdasht ◽  
Hyosuk Yun ◽  
Jeong Hoon Park ◽  
Hye Jung Min ◽  
...  

Radioactive isotopes are used as drugs or contrast agents in the medical field after being conjugated with chelates such as DOTA, NOTA, DTPA, TETA, CyDTA, TRITA, and DPDP. The N-terminal sequence of human serum albumin (HSA) is known as a metal binding site, such as for Co2+, Cu2+, and Ni2+. For this study, we designed and synthesized wAlb12 peptide from the N-terminal region of HSA, which can bind to cobalt, to develop a peptide-based chelate. The wAlb12 with a random coil structure tightly binds to the Co(II) ion. Moreover, the binding property of wAlb12 toward Co(II) was confirmed using various spectroscopic experiments. To identify the binding site of wAlb12, the analogs were synthesized by alanine scanning mutagenesis. Among them, H3A and Ac-wAlb12 did not bind to Co(II). The analysis of the binding regions confirmed that the His3 and α-amino group of the N-terminal region are important for Co(II) binding. The wAlb12 bound to Co(II) with Kd of 75 μM determined by isothermal titration calorimetry when analyzed by a single-site binding model. For the use of wAlb12 as a chelate in humans, its cytotoxicity and stability were investigated. Trypsin stability showed that the wAlb12 − Co(II) complex was more stable than wAlb12 alone. Furthermore, the cell viability analysis showed wAlb12 and wAlb12 + Co(II) to be non-toxic to the Raw 264.7 and HEK 293T cell lines. Therefore, a hot radioactive isotope such as cobalt-57 will have the same effect as a stable isotope cobalt. Accordingly, we expect wAlb12 to be used as a peptide chelate that binds with radioactive isotopes.


Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 404
Author(s):  
Letizia Canziani ◽  
Manuela Marenco ◽  
Giorgio Cavenaghi ◽  
Giulia Manfrinato ◽  
Angelo Taglietti ◽  
...  

Background: Macroaggregated human serum albumin (MAA) properties are widely used in nuclear medicine, labelled with 99mTc. The aim of this study is to improve the knowledge about the morphology, size, dimension and physical–chemical characteristics of MAA and their bond with 99mTc and 68Ga. Methods: Commercial kits of MAA (Pulmocis®) were used. Characterisation through experiments based on SEM, DLS and Stokes’ Law were carried out. In vitro experiments for Langmuir isotherms and pH studies on radiolabelling were performed and the stability of the radiometal complex was verified through competition reactions. Results: The study settles the MAA dimension within the range 43–51 μm. The Langmuir isotherm reveals for [99mTc]MAA: Bmax (46.32), h (2.36); for [68Ga]MAA: Bmax (44.54), h (0.893). Dual labelling reveals that MAA does not discriminate different radioisotopes. Experiments on pH placed the optimal pH for labelling with 99mTc at 6. Conclusion: Radiolabelling of MAA is possible with high efficiency. The nondiscriminatory MAA bonds make this drug suitable for radiolabelling with different radioisotopes or for dual labelling. This finding illustrates the need to continue investigating MAA chemical and physical characteristics to allow for secure labelling with different isotopes.


Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 401
Author(s):  
Agnieszka Szkudlarek ◽  
Jadwiga Pożycka ◽  
Karolina Kulig ◽  
Aleksandra Owczarzy ◽  
Wojciech Rogóż ◽  
...  

Conformational changes in human serum albumin due to numerous modifications that affect its stability and biological activity should be constantly monitored, especially in elderly patients and those suffering from chronic diseases (which include diabetes, obesity, and hypertension). The main goal of this study was to evaluate the effect of a mixture of fatty acids (FA) on the affinity of losartan (LOS, an angiotensin II receptor (AT1) blocker used in hypertension, a first-line treatment with coexisting diabetes) for glycated albumin—simulating the state of diabetes in the body. Individual fatty acid mixtures corresponded to the FA content in the physiological state and in various clinical states proceeding with increased concentrations of saturated (FAS) and unsaturated (FAUS) acids. Based on fluorescence studies, we conclude that LOS interacts with glycated human serum albumin (af)gHSA in the absence and in the presence of fatty acids ((af)gHSAphys, (af)gHSA4S, (af)gHSA8S, (af)gHSA4US, and (af)gHSA8US) and quenches the albumin fluorescence intensity via a static quenching mechanism. LOS not only binds to its specific binding sites in albumins but also non-specifically interacts with the hydrophobic fragments of its surface. Incorrect contents of fatty acids in the body affect the drug pharmacokinetics. A higher concentration of both FAS and FAUS acids in glycated albumin reduces the stability of the complex formed with losartan. The systematic study of FA and albumin interactions using an experimental model mimicking pathological conditions in the body may result in new tools for personalized pharmacotherapy.


2022 ◽  
Author(s):  
Muhammad Babar Taj ◽  
Omar Makarm Ali

Sixteen fuberidazole derivatives as potential new anticancer bioreductive prodrugs are prepared and characterized. The in vitro anticancer potential is examined to explore their cytotoxic properties employing apoptosis, DNA damage, and proliferation tests on chosen hypoxic cancer cells. Overall, eight substances (Compound 5a, 5c, 5d, 5e, 5g, 5h, 5i, and 5m) showed good cytotoxic properties. The potential of compounds is also examined through in silico studies (against human serum albumin), including chem-informatics to understand the structure-activity relationship (SAR), pharmacochemical strength, and the mode of interactions responsible for their action. The DFT calculations revealed that only 5b compound showed the lowest ΔET (2.29 eV) while  5i showed relatively highest βtot (69.89 x 10-31 esu), highest αave (3.18 x 10-23 esu), and dipole moment (6.49 Debye). This study presents a novel class of fuberidazole derivatives with selectivity toward hypoxic cancer cells.


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