Assessment of 177 Lu‐labeled carboxyl‐terminated polyamidoamine (PAMAM) dendrimer‐RGD peptide conjugate

2021 ◽  
Author(s):  
Kusum Vats ◽  
Rohit Sharma ◽  
Amit Kumar Sharma ◽  
Haladhar D. Sarma ◽  
Drishty Satpati
Keyword(s):  
Pamam Dendrimer ◽  
Rgd Peptide

Targeting Breast Cancer Cells with G4 PAMAM Dendrimers and Valproic Acid Derivative Complexes

2020 ◽  
Vol 20 (15) ◽  
pp. 1857-1872
Author(s):  
Alberto M. Muñoz ◽  
Manuel J. Fragoso-Vázquez ◽  
Berenice P. Martel ◽  
Alma Chávez-Blanco ◽  
Alfonso Dueñas-González ◽  
...  
Keyword(s):  
Valproic Acid ◽  
Cell Lines ◽  
Water Solubility ◽  
Md Simulations ◽  
Pamam Dendrimer ◽  
Pamam Dendrimers ◽  
Force Microscopy ◽  
Micromolar Concentration ◽  
Atomic Force

Background: Our research group has developed some Valproic Acid (VPA) derivatives employed as anti-proliferative compounds targeting the HDAC8 enzyme. However, some of these compounds are poorly soluble in water. Objective: Employed the four generations of Polyamidoamine (G4 PAMAM) dendrimers as drug carriers of these compounds to increase their water solubility for further in vitro evaluation. Methods: VPA derivatives were subjected to Docking and Molecular Dynamics (MD) simulations to evaluate their affinity on G4 PAMAM. Then, HPLC-UV/VIS, 1H NMR, MALDI-TOF and atomic force microscopy were employed to establish the formation of the drug-G4 PAMAM complexes. Results: The docking results showed that the amide groups of VPA derivatives make polar interactions with G4 PAMAM, whereas MD simulations corroborated the stability of the complexes. HPLC UV/VIS experiments showed an increase in the drug water solubility which was found to be directly proportional to the amount of G4 PAMAM. 1H NMR showed a disappearance of the proton amine group signals, correlating with docking results. MALDI-TOF and atomic force microscopy suggested the drug-G4 PAMAM dendrimer complexes formation. Discussion: In vitro studies showed that G4 PAMAM has toxicity in the micromolar concentration in MDAMB- 231, MCF7, and 3T3-L1 cell lines. VPA CF-G4 PAMAM dendrimer complex showed anti-proliferative properties in the micromolar concentration in MCF-7 and 3T3-L1, and in the milimolar concentration in MDAMB- 231, whereas VPA MF-G4 PAMAM dendrimer complex didn’t show effects on the three cell lines employed. Conclusion: These results demonstrate that G4 PAMAM dendrimers are capableof transporting poorly watersoluble aryl-VPA derivate compounds to increase its cytotoxic activity against neoplastic cell lines.

Evaluation of biodistribution and anti-tumor effect of a dimeric RGD peptide–paclitaxel conjugate in mice with breast cancer

2008 ◽  
Vol 35 (8) ◽  
pp. 1489-1498 ◽  
Author(s):  
Qizhen Cao ◽  
Zi-Bo Li ◽  
Kai Chen ◽  
Zhanhong Wu ◽  
Lina He ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Rgd Peptide ◽  
Dimeric Rgd Peptide

Osteoblastic potency of bone marrow cells cultivated on functionalized biometals with cyclic RGD-peptide

2013 ◽  
Vol 101 (10) ◽  
pp. 2905-2914 ◽  
Author(s):  
M. Jäger ◽  
C. Böge ◽  
R. Janissen ◽  
D. Rohrbeck ◽  
T. Hülsen ◽  
...  
Keyword(s):  
Bone Marrow ◽  
Bone Marrow Cells ◽  
Rgd Peptide ◽  
Marrow Cells

scholarly journals Biotin-Containing Third Generation Glucoheptoamidated Polyamidoamine Dendrimer for 5-Aminolevulinic Acid Delivery System

2021 ◽  
Vol 22 (4) ◽  
pp. 1982 ◽  
Author(s):  
Aleksandra Kaczorowska ◽  
Małgorzata Malinga-Drozd ◽  
Wojciech Kałas ◽  
Marta Kopaczyńska ◽  
Stanisław Wołowiec ◽  
...  
Keyword(s):  
Reactive Oxygen Species ◽  
Aminolevulinic Acid ◽  
Reactive Oxygen ◽  
Pamam Dendrimer ◽  
Variable Number ◽  
Amide Bond ◽  
Oxygen Species ◽  
Nmr Spectrum ◽  
Guest Molecules ◽  
Amine Groups

Polyamidoamine PAMAM dendrimer generation 3 (G3) was modified by attachment of biotin via amide bond and glucoheptoamidated by addition of α-D-glucoheptono-1,4-lacton to obtain a series of conjugates with a variable number of biotin residues. The composition of conjugates was determined by detailed 1-D and 2-D NMR spectroscopy to reveal the number of biotin residues, which were 1, 2, 4, 6, or 8, while the number of glucoheptoamide residues substituted most of the remaining primary amine groups of PAMAM G3. The conjugates were then used as host molecules to encapsulate the 5-aminolevulinic acid. The solubility of 5-aminolevulinic acid increased twice in the presence of the 5-mM guest in water. The interaction between host and guest was accompanied by deprotonation of the carboxylic group of 5-aminolevulinic acid and proton transfer into internal ternary nitrogen atoms of the guest as evidenced by a characteristic chemical shift of resonances in the 1H NMR spectrum of associates. The guest molecules were most likely encapsulated inside inner shell voids of the host. The number of guest molecules depended on the number of biotin residues of the host, which was 15 for non-biotin-containing glucoheptoamidated G3 down to 6 for glucoheptoamidated G3 with 8 biotin residues on the host surface. The encapsulates were not cytotoxic against Caco-2 cells up to 200-µM concentration in the dark. All encapsulates were able to deliver 5-aminolevulinic acid to cells but aqueous encapsulates were more active in this regard. Simultaneously, the reactive oxygen species were detected by staining with H2DCFDA in Caco-2 cells incubated with encapsulates. The amount of PpIX was sufficient for induction of reactive oxygen species upon 30-s illumination with a 655-nm laser beam.

Synthesis and characterization of fluorescent PAMAM dendrimer modified with 1,8-naphthalimide units and its Cu(II) complex designed for specific biomedical application

2021 ◽  
pp. 113312
Author(s):  
Michela Cangiotti ◽  
Desislava Staneva ◽  
M. Francesca Ottaviani ◽  
Evgenia Vasileva-Tonkova ◽  
Ivo Grabchev
Keyword(s):  
Biomedical Application ◽  
Pamam Dendrimer ◽  
Synthesis And Characterization

scholarly journals Investigating surface topology and cyclic-RGD peptide functionalization on vascular endothelialization

2013 ◽  
Vol 102 (2) ◽  
pp. 532-539 ◽  
Author(s):  
Colton McNichols ◽  
Justin Wilkins ◽  
Atsutoshi Kubota ◽  
Yan T. Shiu ◽  
Samir M. Aouadi ◽  
...  
Keyword(s):  
Rgd Peptide ◽  
Surface Topology ◽  
Peptide Functionalization

Tumor acidic microenvironment-induced drug release of RGD peptide nanoparticles for cellular uptake and cancer therapy

2021 ◽  
pp. 111673
Author(s):  
Zhongying Gong ◽  
Xiaoying Liu ◽  
Baolong Zhou ◽  
Guohui Wang ◽  
Xiuwen Guan ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Drug Release ◽  
Cellular Uptake ◽  
Rgd Peptide ◽  
Acidic Microenvironment ◽  
Peptide Nanoparticles

Engineered Fluorescent Carbon Dots and G4-G6 PAMAM Dendrimer Nanohybrids for Bioimaging and Gene Delivery

2021 ◽  
Author(s):  
Ivo Martins ◽  
Helena Tomás ◽  
Fernando Lahoz ◽  
João Rodrigues
Keyword(s):  
Gene Delivery ◽  
Carbon Dots ◽  
Pamam Dendrimer ◽  
Fluorescent Carbon Dots ◽  
Fluorescent Carbon

Metal adsorption properties of multi‐functional PAMAM dendrimer based gels

2021 ◽  
Author(s):  
Dilgeş Baskın ◽  
Özge Yılmaz ◽  
Muhammad Nazrul Islam ◽  
Metin Tülü ◽  
İkbal Koyuncu ◽  
...  
Keyword(s):  
Pamam Dendrimer ◽  
Adsorption Properties ◽  
Metal Adsorption
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