Amphiphilic Aminated Derivatives of [60]Fullerene as Potent Inhibitors of Tumor Growth and Metastasis

Abstract

Malignant proliferation and metastasis are the hallmarks of cancer cells. Aminated [70]fullerene exhibits notable antineoplastic effects, promoting it a candidate for multi‐targeted cancer drugs. It is an urgent need to reveal the structure–activity relationship for antineoplastic aminated fullerenes. Herein, three amphiphilic derivatives of [60]fullerene with clarified molecular structures are synthesized: TAPC‐4, TAPC‐3, and TCPC‐4. TAPC‐4 inhibits the proliferation of diverse tumor cells via G0/G1 cell cycle arrest, reverses the epithelial–mesenchymal transition, and abrogates the high mobility of tumor cells. TAPC‐4 can be excreted from the organism and achieves an in vivo inhibition index of 75.5% in tumor proliferation and 87.5% in metastatic melanoma with a wide safety margin. Molecular dynamics simulations reveal that the amphiphilic molecular structure and the ending amino groups promote the targeting of TAPC‐4 to heat shock protein Hsp90‐beta, vimentin, and myosin heavy chain 9 (MYH9), probably resulting in the alteration of cyclin D1 translation, vimentin expression, and MYH9 location, respectively. This work initially emphasizes the dominant role of the amphiphilic structure and the terminal amino moieties in the antineoplastic effects of aminated fullerenes, providing fundamental support for their anti‐tumor drug development.

Curdlan-Decorated Fullerenes Mitigate Immune-Mediated Hepatic Injury for Autoimmune Hepatitis Therapeutics via Reducing Macrophage Infiltration

“…BALB/c mice were treated with Cy5-labeled Cur-F (Cur-F-Cy5) or Cy5-labeled F-Gly (F-Gly-Cy5) via tail intravenous injection, and their primary organs (heart, liver, spleen, lung, and kidneys) were harvested for imaging ex vivo at different time intervals. It was demonstrated that Cur-F-Cy5 and F-Gly-Cy5 were mainly distributed in liver and kidney tissues (Figure A,B), which is consistent with other fullerene-based materials. , And the distribution of Cur-F in the liver is significantly higher than that of F-Gly (Figure C), suggesting the liver-targeting effect of Cur-F. These most abundant Cur-F concentrations in the liver inspired the application of it on hepatic diseases.…”

“…Furthermore, we investigated the intracellular antioxidative effects of Cur-F. First, the cytotoxicity of Cur-F was evaluated by coincubation with RAW 264.7 cells and L02 hepatocytes at different concentrations for 24 h. It was and F-Gly-Cy5 were mainly distributed in liver and kidney tissues (Figure 3A,B), which is consistent with other fullerenebased materials. 42,43 And the distribution of Cur-F in the liver is significantly higher than that of F-Gly (Figure 3C), suggesting the liver-targeting effect of Cur-F. These most abundant Cur-F concentrations in the liver inspired the application of it on hepatic diseases.…”

Nanocomposite fibers based on cellulose acetate loaded with fullerene for cancer therapy: preparation, characterization and in-vitro evaluation

“…An assessment of their safety profile was carried out using cytotoxicity screening on normal fibroblasts (Wi-38), followed by a comparison of their anticancer potential with 5-fluorouracil (5-FU) against three selected cancer cell lines (Caco-2, MDA-MB 231 and HepG-2). Fullerene@CA nanocomposite fibers, loaded with fullerene concentrations (0.1, 0.3, and 0.5 mg.g −1 ), are initially used as prescription carriers for anticancer treatments because fullerene has anticancer properties—according to previous studies 50 – 52 . The effect of Fullerene@CA nanocomposite fiber as an anti-cancer material was revealed, and it began to be evaluated as a standalone drug for anti-tumor growth where Bacakova et.al.…”

Asymmetric Cyclodextrin-Dimer-Involved Nanoassemblies by Selective Host–Guest Interactions: Concentration-Dependent Morphology Evolution and Light-Regulated Biomedical Applications

“…Polymeric assemblies including spherical, star-like, or worm-like nanoparticles, vesicles, or other complex structures could perform numerous applications in drug carriers or nanoreactors because of their unique characteristics and stability in a water environment. − The self-assembly of amphiphilic copolymers with both hydrophilic and hydrophobic building blocks have been studied extensively, and several ripe experiences have been summarized. However, besides amphiphilic copolymers, covalently linked organic–inorganic hybrid materials bearing organic polymer chains and inorganic units, such as carbon or metal nanoparticles, have attracted a lot of research interest. − Among inorganic nanobuilding blocks, polymer chain-modified fullerene C 60 has been widely investigated. − As one of the typical examples, a series of supramolecular nanoassemblies, including the core–shell structure, spherical nanoparticles (SNPs), and nanonetwork architectures could be constructed from isotactic (it-) and syndiotactic (st-) C 60 -end-capped poly­(methyl methacrylate)­s through adjusting the types of solvents and block ratios …”