Albumin roles in developing anticancer compounds

Ribeiro, Amélia Galdino; Alves, Josival Emanuel Ferreira; Soares, José Cleberson Santos; Santos, Keriolaine Lima dos; Jacob, Iris Trindade Tenório; Ferreira, Cindy Juliane da Silva; Santos, Jéssica Celerino dos; Azevedo, Rafael David Souto de; Almeida, Sinara Mônica Vitalino de; Lima, Maria do Carmo Alves de

doi:10.1007/s00044-021-02748-z

Cited by 11 publications

(7 citation statements)

References 145 publications

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“…Albumin is a highly circulating protein and one of its main functions is the transport of endogenous and exogenous compounds, being responsible for the distribution of drugs in the body (Hoogenboezem& Duvall 2018). Therefore, it is necessary to search for drugs that bind reversibly to albumin and that do not promote changes in its conformation (Ribeiro et al 2021). The human serum albumin used in this interaction experiment was kindly provided by the Molecular Biology Laboratory of the University of Pernambuco, located in Garanhuns, Pernambuco, Brazil.…”

Section: Interaction Assays Of Compounds With Human Albumin (Hsa)mentioning

confidence: 99%

“…Human serum albumin (HSA) is the most abundant plasma protein in human blood, present at a concentration around 40 to 50 mg/mL (Ribeiro et al 2021). As it is a widely circulated protein, one of its main functions is the transport of endogenous and exogenous ligands, including being responsible for the distribution of drugs in the body (Hoogenboezem & Duvall 2018).…”

Section: Interaction Assays Of Compounds With Human Albumin (Hsa)mentioning

confidence: 99%

“…As it is a widely circulated protein, one of its main functions is the transport of endogenous and exogenous ligands, including being responsible for the distribution of drugs in the body (Hoogenboezem & Duvall 2018). Thus, the pharmacological properties of a drug can be highly influenced by its ability to bind albumin protein (Hoogenboezem & Duvall, 2018;Ribeiro et al 2021). An important feature of the drug-albumin interaction is that the binding is reversible in nature, leading to an equilibrium between the bound molecule and its free portion in the circulation (Ribeiro et al 2021).…”

Section: Interaction Assays Of Compounds With Human Albumin (Hsa)mentioning

confidence: 99%

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Preliminary evaluation of the interaction with Albumin/DNA and in vitro evaluation of the antioxidant properties promoted by thiosemicarbazones and thiazole compounds

Nascimento,

Santos,

Pereira

et al. 2024

Sci. Electronic Arch

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Thiosemicarbazones and thiazoles are known for their diverse biological activities. This study introduced two series of molecules, 4-(3-(4-nitrophenyl)-4-phenylthiazol-2(3H)-ylidene)-hydrazine)-methyl)-phenol and 4-(3-(4-chlorophenyl)-4-phenylthiazol-2(3H)-ylidene)-hydrazine)-methyl)-phenol, which exhibit biological potential as antioxidant agents. The study also assessed the interaction of these compounds with various HSA/DNA macromolecules. The results of the antioxidant activity showed that thiazoles in the DPPH assay exhibited IC50 values ranging from 439.4 to 691.67 µM. In the ABTS assay, thiosemicarbazones exhibited significant activity, ranging from 39.19 to 50.03 µM. Interaction assays were carried out with human serum albumin (HSA) and DNA. All compounds were able to interact with both DNA (low to moderate interaction) and HSA (moderate to high interaction).

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Section: Interaction Assays Of Compounds With Human Albumin (Hsa)mentioning

confidence: 99%

Section: Interaction Assays Of Compounds With Human Albumin (Hsa)mentioning

confidence: 99%

Section: Interaction Assays Of Compounds With Human Albumin (Hsa)mentioning

confidence: 99%

See 1 more Smart Citation

Preliminary evaluation of the interaction with Albumin/DNA and in vitro evaluation of the antioxidant properties promoted by thiosemicarbazones and thiazole compounds

Nascimento,

Santos,

Pereira

et al. 2024

Sci. Electronic Arch

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“…A study concerning doxorubicin, 18 an initial antitumor drug for the treatment of breast cancer, 19 publicized the relevance of albumin for drug binding 20 to restrain the trials concerning bioavailability, pharmacokinetics, 21 and cellular uptake of drug molecules, 22 specifically in the background of multidrug treatment. 23 Albumin protein can gather in the tumor microenvironment 24 and also at the inflammation spots because of the leakage of blood capillaries and helps in the retention of the moiety in the tumor opening.…”

Section: ■ Introductionmentioning

confidence: 99%

Inhibition of Human Colorectal Cancer by a Natural Product 7-Acetylhorminone and Interactions with BSA/HSA: Multispectral Analysis and In Silico and In Vitro Studies

Pakrashy,

Chakraborty,

Manna

et al. 2024

ACS Appl. Bio Mater.

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We have semi-synthesized a natural product 7-acetylhorminone from crude extract of Premna obtusifolia (Indian headache tree), which is active against colorectal cancer after probation through computational screening methods as it passed through the set parameters of pharmacokinetics (most important nonblood−brain barrier permeant) and drug likeliness (e.g., Lipinski's, Ghose's, Veber's rule) which most other phytoconstituents failed to pass combined with docking with EGFR protein which is highly upregulated in the colorectal carcinoma cell. The structure of 7-acetylhorminone was confirmed by single crystal Xray diffraction studies and 1 H NMR, 13 C NMR, and COSY studies. To validate the theoretical studies, first, in vitro experiments were carried out against human colorectal carcinoma cell lines (HCT116) which revealed the potent cytotoxic efficacy of 7acetylhorminone and verified preliminary investigation. Second, the drugability of 7-acetylhorminone interaction with serum albumin proteins (HSA and BSA) is evaluated both theoretically and experimentally via steady-state fluorescence spectroscopic studies, circular dichroism, isothermal titration calorimetry, and molecular docking. In summary, this study reveals the applicability of 7-acetylhorminone as a potent drug candidate or as a combinatorial drug against colorectal cancer.

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“…Drugs are transported in the circulation either in a free form, dissolved in the aqueous phase of plasma, or complexed with plasma proteins in varying degrees [1,2]. This drug-protein binding is reversible in nature, and an equilibrium between the bound and free drug molecules exists [3,4]. Serum albumin is the most abundant circulatory protein in blood plasma and plays an important role in the transport and deportation of different types of endogenous and exogenous compounds to target cells [5,6].…”

Section: Introductionmentioning

confidence: 99%

PI3K/mTOR Dual Inhibitor Pictilisib Stably Binds to Site I of Human Serum Albumin as Observed by Computer Simulation, Multispectroscopic, and Microscopic Studies

Yang

Zhang

et al. 2022

Molecules

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Pictilisib (GDC-0941) is a well-known dual inhibitor of class I PI3K and mTOR and is presently undergoing phase 2 clinical trials for cancer treatment. The present work investigated the dynamic behaviors and interaction mechanism between GDC-0941 and human serum albumin (HSA). Molecular docking and MD trajectory analyses revealed that GDC-0941 bound to HSA and that the binding site was positioned in subdomain IIA at Sudlow’s site I of HSA. The fluorescence intensity of HSA was strongly quenched by GDC-0941, and results showed that the HSA–GDC-0941 interaction was a static process caused by ground-state complex formation. The association constant of the HSA–GDC-0941 complex was approximately 105 M−1, reflecting moderate affinity. Thermodynamic analysis conclusions were identical with MD simulation results, which revealed that van der Waals interactions were the vital forces involved in the binding process. CD, synchronous, and 3D fluorescence spectroscopic results revealed that GDC-0941 induced the structural change in HSA. Moreover, the conformational change of HSA affected its molecular sizes, as evidenced by AFM. This work provides a useful research strategy for exploring the interaction of GDC-0941 with HSA, thus helping in the understanding of the transport and delivery of dual inhibitors in the blood circulation system.

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Albumin roles in developing anticancer compounds

Cited by 11 publications

References 145 publications

Preliminary evaluation of the interaction with Albumin/DNA and in vitro evaluation of the antioxidant properties promoted by thiosemicarbazones and thiazole compounds

Preliminary evaluation of the interaction with Albumin/DNA and in vitro evaluation of the antioxidant properties promoted by thiosemicarbazones and thiazole compounds

Inhibition of Human Colorectal Cancer by a Natural Product 7-Acetylhorminone and Interactions with BSA/HSA: Multispectral Analysis and In Silico and In Vitro Studies

PI3K/mTOR Dual Inhibitor Pictilisib Stably Binds to Site I of Human Serum Albumin as Observed by Computer Simulation, Multispectroscopic, and Microscopic Studies

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