Synthesis and Evaluation of Ga-68-Labeled Rhein for Early Assessment of Treatment-Induced Tumor Necrosis

Zhang, Aimi; Wu, Tianze; Bian, Li; Li, Panli; Liu, Qiufang; Zhang, Dongjian; Jin, Qiaomei; Zhang, Jian; Huang, Gang; Song, Shaoli

doi:10.1007/s11307-019-01365-y

Cited by 11 publications

(20 citation statements)

References 37 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Autoradiography and TTC staining studies further confirmed the results of biodistribution, revealing the specific avidity of 68 Ga-DOTA-rhein for necrotic tissues [49]. Micro-PET/CT imaging showed that an obvious hotspot was observed in the necrotic region of the left hind limb but not in the right normal hind limb at 1 h post injection of 68 Ga-DOTA-rhein, suggesting that 68 Ga-DOTA-rhein could be used for visualization of necrotic tissues in vivo [49]. In a S180 tumor-bearing mouse model, PET/CT imaging showed significantly higher radioactive uptake in the CA4P-treated tumors compared to the untreated tumors at 1 h post injection of 68 Ga-DOTA-rhein [49].…”

Section: Early Monitoring Of Tumor Response To Therapysupporting

confidence: 58%

“…Micro-PET/CT imaging showed that an obvious hotspot was observed in the necrotic region of the left hind limb but not in the right normal hind limb at 1 h post injection of 68 Ga-DOTA-rhein, suggesting that 68 Ga-DOTA-rhein could be used for visualization of necrotic tissues in vivo [49]. In a S180 tumor-bearing mouse model, PET/CT imaging showed significantly higher radioactive uptake in the CA4P-treated tumors compared to the untreated tumors at 1 h post injection of 68 Ga-DOTA-rhein [49]. The result of ex vivo biodistribution was consistent with the finding of PET/CT imaging [49].…”

Section: Early Monitoring Of Tumor Response To Therapymentioning

confidence: 92%

“…Considering the significantly higher sensitivity and acceptable spatial resolution of positron emission tomography (PET) imaging compared to MRI, a rhein-based PET probe ( 68 Ga-DOTA-rhein, Figure 1) has been developed by substituting the Gd 3+ in GdL 2 with positron radionuclide 68 Ga 3+ for early monitoring of therapy-induced tumor necrosis [49]. The initial biodistribution study in a mouse model of induced muscular necrosis demonstrated that 68 Ga-DOTA-rhein exhibited a significantly higher uptake in necrotic muscle than in normal muscle at both 30 and 60 min post injection [49].…”

Section: Early Monitoring Of Tumor Response To Therapymentioning

confidence: 99%

“…[18][19][20]. More recently, based on our previous studies on necrosis avidity of bisanthracene nuclear anthraquinone compounds and in pursuit for NAAs with improved physicochemical properties, pharmacokinetics and biodistribution, monomeric anthraquinone compound rhein was demonstrated to have a newly discovered necrosis-avid trait and to show promising applications in noninvasive visualization of myocardial necrosis and early monitoring of tumor response to therapy [44][45][46][47][48][49].…”

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Discovery of necrosis avidity of rhein and its applications in necrosis imaging

Zhang

Jin

et al. 2020

Journal of Drug Targeting

Self Cite

View full text Add to dashboard Cite

Necrosis-avid agents possess exploitable theragnostic utilities including evaluation of tissue viability, monitoring of therapeutic efficacy as well as diagnosis and treatment of necrosis-related disorders. Rhein (4,5-dihydroxyl-2-carboxylic-9,10-dihydrodiketoanthracene), a naturally occurring monomeric anthraquinone compound extensively found in medicinal herbs, was recently demonstrated to have a newly discovered necrosis-avid trait and to show promising application in necrosis imaging. In this overview, we present the discovering process of rhein as a new necrosis-avid agent as well as its potential imaging applications in visualization of myocardial necrosis and early evaluation of tumor response to therapy. Moreover, the molecular mechanism exploration of necrosis avidity behind rhein are also presented. The discovery of necrosis avidity with rhein and the development of rhein-based molecular probes may further expand the scope of necrosis-avid compounds and highlight the potential utility of necrosis-avid molecular probes in necrosis imaging.

show abstract

Section: Early Monitoring Of Tumor Response To Therapysupporting

confidence: 58%

Section: Early Monitoring Of Tumor Response To Therapymentioning

confidence: 92%

Section: Early Monitoring Of Tumor Response To Therapymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Discovery of necrosis avidity of rhein and its applications in necrosis imaging

Zhang

Jin

et al. 2020

Journal of Drug Targeting

Self Cite

View full text Add to dashboard Cite

show abstract

“…As this compound has a highly stable structure, various hydrophilic and lipophilic nano-formulations have been developed to improve its oral absorption, bioavailability, and sustained targeted release [59]. A conjugate of rhein, rhein-DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) has been used to treat sarcoma and owing to its remarkable necrosis avidity; studies suggest that it could be used as a significant probe for PET/CT-imaging-mediated early detection of response to antitumor therapy [87].…”

Section: Chemistry Of Rheinmentioning

confidence: 99%

Therapeutic Emergence of Rhein as a Potential Anticancer Drug: A Review of Its Molecular Targets and Anticancer Properties

et al. 2020

View full text Add to dashboard Cite

According to the World Health Organization (WHO), cancer is the second-highest cause of mortality in the world, and it kills nearly 9.6 million people annually. Besides the fatality of the disease, poor prognosis, cost of conventional therapies, and associated side-effects add more burden to patients, post-diagnosis. Therefore, the search for alternatives for the treatment of cancer that are safe, multi-targeted, effective, and cost-effective has compelled us to go back to ancient systems of medicine. Natural herbs and plant formulations are laden with a variety of phytochemicals. One such compound is rhein, which is an anthraquinone derived from the roots of Rheum spp. and Polygonum multiflorum. In ethnomedicine, these plants are used for the treatment of inflammation, osteoarthritis, diabetes, and bacterial and helminthic infections. Increasing evidence suggests that this compound can suppress breast cancer, cervical cancer, colon cancer, lung cancer, ovarian cancer, etc. in both in vitro and in vivo settings. Recent studies have reported that this compound modulates different signaling cascades in cancer cells and can prevent angiogenesis and progression of different types of cancers. The present review highlights the cancer-preventing and therapeutic properties of rhein based on the available literature, which will help to extend further research to establish the chemoprotective and therapeutic roles of rhein compared to other conventional drugs. Future pharmacokinetic and toxicological studies could support this compound as an effective anticancer agent.

show abstract

Palindrome-mediated DNA nanotubes with cell-specific aptamers to improve targeted antitumor effects and reduce toxicity on non-small cell lung cancer

Zheng,

Song,

et al. 2024

Sci. China Life Sci.

View full text Add to dashboard Cite

Synthesis and Evaluation of Ga-68-Labeled Rhein for Early Assessment of Treatment-Induced Tumor Necrosis

Cited by 11 publications

References 37 publications

Discovery of necrosis avidity of rhein and its applications in necrosis imaging

Discovery of necrosis avidity of rhein and its applications in necrosis imaging

Therapeutic Emergence of Rhein as a Potential Anticancer Drug: A Review of Its Molecular Targets and Anticancer Properties

Palindrome-mediated DNA nanotubes with cell-specific aptamers to improve targeted antitumor effects and reduce toxicity on non-small cell lung cancer

Contact Info

Product

Resources

About