New Perspectives in Cancer Therapy: The Biotin-Antitumor Molecule Conjugates

Collina, Simona

doi:10.4172/2161-0444.s1-004

Cited by 28 publications

(10 citation statements)

References 71 publications

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“…Other than the FR (see Section 4‐A), biotin is a promising vitamin‐based agent for targeted delivery of drugs or diagnostic . Biotin is required for cell growth, and the biotin demand in tumors is higher than in normal tissues.…”

Section: Examples Of Targeting Molecules and Their Small‐molecule Conmentioning

confidence: 99%

Small Molecules for Active Targeting in Cancer

Kue

Kamkaew

Burgess

et al. 2016

Medicinal Research Reviews

115

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For the purpose of this review, active targeting in cancer research encompasses strategies wherein a ligand for a cell surface receptor expressed on tumor cells is used to deliver a cytotoxic or imaging cargo. This area of research is more than two decades old, but in those 20 and more years, how many receptors have been studied extensively? What kinds of the ligands are used for active targeting? Are they mostly naturally occurring molecules such as folic acid, or synthetic substances developed in campaigns for medicinal chemistry efforts? This review outlines the most important receptor or ligand combinations that have been used in active targeting to answer these questions, and therefore to address the most important one of all: is research in active targeting affording diminishing returns, or is this an area for which the potential far exceeds progress made so far?

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Section: Examples Of Targeting Molecules and Their Small‐molecule Conmentioning

confidence: 99%

Small Molecules for Active Targeting in Cancer

Kue

Kamkaew

Burgess

et al. 2016

Medicinal Research Reviews

115

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“…Solid tumor cells require high levels of biotin due to their high metabolic activity [34]. Biotin receptors are overexpressed on the surface of many tumor cells and thus represent a biomarker for targeting tumor cells [35][36][37][38]. Due to this properties, biotin has emerged as a prominent active targeting moiety for drug nanocarrier systems.…”

Section: Introductionmentioning

confidence: 99%

Biotin-Decorated PAMAM G4.5 Dendrimer Nanoparticles to Enhance the Delivery, Anti-Proliferative, and Apoptotic Effects of Chemotherapeutic Drug in Cancer Cells

et al. 2020

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Biotin receptors are overexpressed by various types of solid cancer cells and play a significant role in tumor metabolism, growth, and metastasis. Thus, targeting the biotin receptors on tumor cells may enhance the efficiency and reduce the side-effects of chemotherapy. The aim of this study was to develop a biotin-coupled poly(amido)amine (PAMAM) (PG4.5) dendrimer nanoparticle to enhance the tumor-specific delivery and intracellular uptake of anticancer drugs via receptor-mediated endocytosis. We modified PG4.5 with diethylenetriamine (DETA) followed by biotin via an amide bond and characterized the resulting PG4.5-DETA-biotin nanoparticles by 1H NMR, FTIR, and Raman spectroscopy. Loading and releasing of gemcitabine (GEM) from PG4.5-DETA-biotin were evaluated by UV–Visible spectrophotometry. Cell viability and cellular uptake were examined by MTT assay and flow cytometry to assess the biocompatibility, cellular internalization efficiency and antiproliferative activity of PG4.5-DETA-biotin/GEM. Gemcitabine-loaded PG4.5-DETA-biotin nanoparticles were spherical with a particle size of 81.6 ± 6.08 nm and zeta potential of 0.47 ± 1.25 mV. Maximum drug-loading content and encapsulation efficiency were 10.84 ± 0.16% and 47.01 ± 0.71%, respectively. Nearly 60.54 ± 1.99% and 73.96 ± 1.14% of gemcitabine was released from PG4.5-DETA-biotin/GEM nanoparticles after 48 h at the acidic pH values of 6.5 and 5, respectively. Flow cytometry and fluorescence microscopy of cellular uptake results revealed PG4.5-DETA-biotin/GEM nanoparticles selectively targeted cancer cells in vitro. Cytotoxicity assays demonstrated gemcitabine-loaded PG4.5-DETA-biotin significantly reduced cell viability and induced apoptosis in HeLa cells. Thus, biotin-coupled PG4.5-DETA nanocarrier could provide an effective, targeted drug delivery system and selectively convey gemcitabine into tumor cells.

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“…Several known anticancer agents in clinical use, such as paclitaxel, 8 doxorubicin, 9 and gemcitabine, 10 functionalized with biotin to improve their efficiency and efficacy while reducing their toxicity. 6 Furthermore, a prospective Pt(IV) prodrug (Figure 1a) based on cisplatin scaffold and bearing biotin and the nonsteroidal anti-inflammatory drug indomethacin (biotin-Pt(IV)-indomethacin conjugate) showed selectivity toward cancer cells vs. normal cells, while being cytotoxic and effective against cisplatin-resistant cancer cells. 11 The inclusion of biotin lead to a substantial increase in Pt uptake by the cells relative to cisplatin demonstrating a possible promotion of the compound's uptake via biotin receptor-mediated pathway.…”

Section: ■ Introductionmentioning

confidence: 99%

Ruthenium–Cyclopentadienyl Bipyridine–Biotin Based Compounds: Synthesis and Biological Effect

et al. 2019

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Prospective anticancer metallodrugs should consider target-specific components in their design in order to overcome the limitations of the current chemotherapeutics. The inclusion of vitamins, which receptors are overexpressed in many cancer cell lines, has proven to be a valid strategy. Therefore, in this paper we report the synthesis and characterization of a set of new compounds [Ru(η 5 -C 5 H 5 )(P(C 6 H 4 R) 3 )(4,4′-R′-2,2′-bpy)] + (R = F and R′ = H, 3; R = F and R′ = biotin, 4; R = OCH 3 and R′ = H, 5; R = OCH 3 and R′ = biotin, 6), inspired by the exceptional good results recently obtained for the analogue bearing a triphenylphosphane ligand. The precursors for these syntheses were also described following modified literature procedures, [Ru(η 5 -C 5 H 5 )(P(C 6 H 4 R) 3 ) 2 Cl], where R is −F (1) or −OCH 3 (2). The structure of all compounds is fully supported by spectroscopic and analytical techniques and by X-ray diffraction studies for compounds 2, 3, and 5. All cationic compounds are cytotoxic in the two breast cancer cell lines tested, MCF7 and MDA-MB-231, and much better than cisplatin under the same experimental conditions. The cytotoxicity of the biotinylated compounds seems to be related with the Ru uptake by the cells expressing biotin receptors, indicating a potential mediated uptake. Indeed, a biotin−avidin study confirmed that the attachment of biotin to the organometallic fragment still allows biotin recognition by the protein. Therefore, the biotinylated compounds might be potent anticancer drugs as they show cytotoxic effect in breast cancer cells at low dose dependent on the compounds' uptake, induce cell death by apoptosis and inhibit the colony formation of cancer cells causing also less severe side effects in zebrafish.

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New Perspectives in Cancer Therapy: The Biotin-Antitumor Molecule Conjugates

Cited by 28 publications

References 71 publications

Small Molecules for Active Targeting in Cancer

Small Molecules for Active Targeting in Cancer

Biotin-Decorated PAMAM G4.5 Dendrimer Nanoparticles to Enhance the Delivery, Anti-Proliferative, and Apoptotic Effects of Chemotherapeutic Drug in Cancer Cells

Ruthenium–Cyclopentadienyl Bipyridine–Biotin Based Compounds: Synthesis and Biological Effect

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