scholarly journals Synthesis and Evaluation of Amino Acid-Based Radiotracer99mTc-N4-AMT for Breast Cancer Imaging

2011 ◽  
Vol 2011 ◽  
pp. 1-7 ◽  
Author(s):  
Fan-Lin Kong ◽  
Mohammad S. Ali ◽  
Yinhan Zhang ◽  
Chang-Sok Oh ◽  
Dong-Fang Yu ◽  
...  

Purpose. This study was to develop an efficient synthesis of99mTc-O-[3-(1,4,8,11-tetraazabicyclohexadecane)-propyl]-α-methyl tyrosine (99mTc-N4-AMT) and evaluate its potential in cancer imaging.Methods. N4-AMT was synthesized by reacting N4-oxalate and 3-bromopropyl AMT (N-BOC, ethyl ester).In vitrocellular uptake kinetics of99mTc-N4-AMT was assessed in rat mammary tumor cells. Tissue distribution of the radiotracer was determined in normal rats at 0.5–4 h, while planar imaging was performed in mammary tumor-bearing rats at 30–120 min.Results. The total synthesis yield of N4-AMT was 14%. Cellular uptake of99mTc-N4-AMT was significantly higher than that of99mTc-N4. Planar imaging revealed that99mTc-N4-AMT rendered greater tumor/muscle ratios than99mTc-N4.Conclusions. N4-AMT could be synthesized with a considerably high yield. Ourin vitroandin vivodata suggest that99mTc-N4-AMT, a novel amino acid-based radiotracer, efficiently enters breast cancer cells, effectively distinguishes mammary tumors from normal tissues, and thus holds the promise for breast cancer imaging.

2018 ◽  
Vol 11 (3) ◽  
pp. 65
Author(s):  
Alicia Vall-Sagarra ◽  
Shanna Litau ◽  
Clemens Decristoforo ◽  
Björn Wängler ◽  
Ralf Schirrmacher ◽  
...  

2017 ◽  
Vol 79 (6) ◽  
pp. 1195-1203 ◽  
Author(s):  
Elham Mousavi ◽  
Shahrzad Tavakolfar ◽  
Ali Almasirad ◽  
Zahra Kooshafar ◽  
Soudeh Dehghani ◽  
...  

RSC Advances ◽  
2016 ◽  
Vol 6 (54) ◽  
pp. 48415-48419 ◽  
Author(s):  
Tae-Hyun Kim ◽  
Jun Young Lee ◽  
Min-Kyu Kim ◽  
Jeong Hoon Park ◽  
Jae-Min Oh

Radioisotope Co-57 substituted LDH were successfully prepared by isomorphous substitution and showed high in vitro cellular uptake and tumor targeting in vivo biodistribution.


2020 ◽  
Author(s):  
Ye Yuan ◽  
Jia-Xing Song ◽  
Mei-Na Zhang ◽  
Baoshan Yuan

Abstract Present study was planned for the development of pH sensitive lipid polymer hybrid nanoparticles (pHS-LPHNPs) loaded with docetaxel (DTX) for guided and target specific cytosolic-delivery delivery of docetaxel (DTX). pHS-LPHNPs were formulated to entrap DTX by self-assembled nano-precipitation technique and characterised with respect to zeta potential, particle-size, entrapment efficiency, PDI as well as invitro drug release. The cell viability, apoptosis, cellular-uptake, pharmacokinetics, bio-distribution in vital organs, % changes in tumour volume and survival of breast cancer bearing animals were used for the evaluation of efficacy of the formulation. In-vitro studies showed increased cytotoxicity at lower IC50 and better cellular-uptake of pHS-LPHNPs mediated drug by breast cancer cell lines. We saw the better rate of apoptosis of breast cancer cells via Annexin V/Propidium iodide staining. Moreover, in-vivo studies demonstrated improved pharmacokinetics and targetability with minimum drug circulation in deep-seated organs upon delivery of DTX via pHS-LPHNPs in comparison with LPHNPs-DTX and free DTX. We observed sizeable % reduction in tumour-burden with pHS-LPHNPs-DTXthan that withLPHNPs-DTX &free DTX. In brief, pHS-LPHNPs mediated delivery of DTX exhibited promising approach for developing therapeutic-interventions against breast-cancer.


2012 ◽  
Vol 35 (5-6) ◽  
pp. 317-337 ◽  
Author(s):  
Yasaman Ardeshirpour ◽  
Amir H. Gandjbakhche ◽  
Laleh Najafizadeh

In vivooptical imaging is being conducted in a variety of medical applications, including optical breast cancer imaging, functional brain imaging, endoscopy, exercise medicine, and monitoring the photodynamic therapy and progress of neoadjuvant chemotherapy. In the past three decades,in vivodiffuse optical breast cancer imaging has shown promising results in cancer detection, and monitoring the progress of neoadjuvant chemotherapy. The use of near infrared spectroscopy for functional brain imaging has been growing rapidly. In fluorescence imaging, the difference between autofluorescence of cancer lesions compared to normal tissues were used in endoscopy to distinguish malignant lesions from normal tissue or inflammation and in determining the boarders of cancer lesions in surgery. Recent advances in drugs targeting specific tumor receptors, such as AntiBodies (MAB), has created a new demand for developing non-invasivein vivoimaging techniques for detection of cancer biomarkers, and for monitoring their down regulations during therapy. Targeted treatments, combined with new imaging techniques, are expected to potentially result in new imaging and treatment paradigms in cancer therapy. Similar approaches can potentially be applied for the characterization of other disease-related biomarkers. In this chapter, we provide a review of diffuse optical and fluorescence imaging techniques with their application in functional brain imaging and cancer diagnosis.


2002 ◽  
Vol 29 (8) ◽  
pp. 809-815 ◽  
Author(s):  
Holger Palmedo ◽  
Jenne Hensel ◽  
Michael Reinhardt ◽  
Dirk Von Mallek ◽  
Alexander Matthies ◽  
...  

Author(s):  
Jang Hyuk Bang ◽  
Kyung Ah Kim ◽  
Yeong Chae Ryu ◽  
Byoung Choul Kim ◽  
BYEONG HEE HWANG

Breast cancer is one of the serious diseases and has the second-highest mortality in women worldwide. RNA interference has been developed as a promising way of specific cancer treatment by silencing oncogenes efficiently. However, small RNAs exhibits difficulties in specific cellular uptake and instability. Therefore, we designed novel fusion peptides (RS and RT) for an efficient, stable, and specific delivery of small RNAs. Both RS and RT peptides could form self-assembled nanocomplexes via electrostatic attraction. RS nanocomplexes exhibited prolonged stability, enhanced cellular uptake, and target gene silencing by siRNAs to MDA-MB-231 breast cancer cells. Moreover, RS nanocomplexes successfully inhibited breast cancer cell growth via specific and efficient siRNA delivery. Furthermore, in vitro and in vivo safety tests showed negligible cytotoxicity and neither tissue damage nor significant inflammatory cytokine release. Therefore, the RS nanocomplexes could be expected to become a promising siRNA delivery platform for the treatment of breast cancer or other cancers.


Endocrinology ◽  
2016 ◽  
Vol 157 (6) ◽  
pp. 2204-2216 ◽  
Author(s):  
Jiarong Li ◽  
Aimée-Lee Luco ◽  
Benoît Ochietti ◽  
Ibtihal Fadhil ◽  
Anne Camirand ◽  
...  

Biologically active vitamin D (1,25-dihydroxycholecalciferol or 1,25(OH)2D) is synthetized from inactive prohormone 25-hydroxycholecalciferol (25(OH)D) by the enzyme CYP27B1 1-α-hydroxylase in kidney and several extrarenal tissues including breast. Although the development of breast cancer has been linked to inadequate vitamin D status, the importance of bioactive vitamin D production within tumors themselves is not fully understood. To investigate the role of tumoral vitamin D production in mammary epithelial cell progression to breast cancer, we conducted a Cre-loxP-mediated Cyp27b1 gene ablation in the mammary epithelium of the polyoma middle T antigen-mouse mammary tumor virus (PyMT-MMTV) mouse breast cancer model. Targeted ablation of Cyp27b1 was accompanied by significant acceleration in initiation of spontaneous mammary tumorigenesis. In vivo, cell proliferation, angiogenesis, cell cycle progression, and survival markers were up-regulated in tumors by Cyp27b1 ablation, and apoptosis was decreased. AK thymoma (AKT) phosphorylation and expression of several components of nuclear factor κB (NF-κB), integrin, and signal transducer and activator of transcription 3 (STAT3) signaling pathways were increased in Cyp27b1-ablated tumors compared with nonablated controls. In vitro, 1,25(OH)2D treatment induced a strong antiproliferative action on tumor cells from both ablated and nonablated mice, accompanied by rapid disappearance of NF-κB p65 from the nucleus and segregation in the cytoplasm. In contrast, treatment with the metabolic precursor 25(OH)D was only effective against cells from nonablated mice. 25(OH)D did not inhibit growth of Cyp27b1-ablated cells, and their nuclear NF-κB p65 remained abundant. Our findings demonstrate that in-tumor CYP27B1 1-α-hydroxylase activity plays a crucial role in controlling early oncogene-mediated mammary carcinogenesis events, at least in part by modulating tumoral cell NF-κB p65 nuclear translocation.


2021 ◽  
Vol 12 ◽  
Author(s):  
Jiyan Su ◽  
Xiaohong Chen ◽  
Yuanjie Xiao ◽  
Dan Li ◽  
Muxia Li ◽  
...  

Triple-negative breast cancer (TNBC) has been acknowledged as an aggressive disease with worst prognosis, which requires endeavor to develop novel therapeutic agents. Bruceae fructus oil (BO), a vegetable oil derived from the fruit of Brucea javanica (L.) Merr., is an approved marketable drug for the treatment of cancer in China for several decades. Despite that the anti–breast cancer activity of several quassinoids derived from B. javanica has been found, it was the first time that the potential of BO against TNBC was revealed. Although BO had no cytotoxicity on TNBC cell lines in vitro, the oral administration of BO exhibited a gut microbiota–dependent tumor suppression without toxicity on the non-targeted organs in vivo. By metagenomics and untargeted metabolomics, it was found that BO not only altered the composition and amino acid metabolism function of gut microbiota but also regulated the host’s amino acid profile, which was in accordance with the metabolism alternation in gut microbiota. Moreover, the activity of mTOR in tumor was promoted by BO treatment as indicated by the phosphorylation of 4E-binding protein 1 (4E-BP1) and ribosomal protein S6, and hyper-autophagy was consequently restrained. By contrast, the failure of tumor suppression by BO under pseudo germ-free (PGF) condition came with indistinctive changes in autophagy and mTOR activity, implying the critical role of the gut microbiota in BO’s anticancer activity. The present study highlighted a promising application of BO against breast cancer with novel efficacy and safety.


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