scholarly journals A “Double-Locked” and Enzyme/pH-Activated Theranostic Agent for Accurate Tumor Imaging and Therapy

Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 425
Author(s):  
Jia Luo ◽  
Zongyu Guan ◽  
Weijie Gao ◽  
Chen Wang ◽  
Zhongyuan Xu ◽  
...  
Keyword(s):  
Tumor Imaging ◽  
Tumor Therapy ◽  
Tumor Resection ◽  
Acid Group ◽  
Inhibitory Effect ◽  
Theranostic Agent ◽  
Precise Diagnosis ◽  
Group A ◽  
Theranostic Agents ◽  
Therapy And Diagnosis

Theranostic agents for concurrent cancer therapy and diagnosis have begun attracting attention as a promising modality. However, accurate imaging and identification remains a great challenge for theranostic agents. Here, we designed and synthesized a novel theranostic agent H6M based on the “double-locked” strategy by introducing an electron-withdrawing nitro group into 1-position of a pH-responsive 3-amino-β-carboline and further covalently linking the hydroxamic acid group, a zinc-binding group (ZBG), to the 3-position of β-carboline to obtain histone deacetylase (HDAC) inhibitory effect for combined HDAC-targeted therapy. We found that H6M can be specifically reduced under overexpressed nitroreductase (NTR) to produce H6AQ, which emits bright fluorescence at low pH. Notably, H6M demonstrated a selective fluorescence imaging via successive reactions with NTR (first “key”) and pH (second “key”), and precisely identified tumor margins with a high S/N ratio to guide tumor resection. Finally, H6M exerted robust HDAC1/cancer cell inhibitory activities compared with a known HDAC inhibitor SAHA. Therefore, the NTR/pH-activated theranostic agent provided a novel tool for precise diagnosis and efficient tumor therapy.

scholarly journals Assessment of the Theranostic Potential of Gold Nanostars—A Multimodal Imaging and Photothermal Treatment Study

Nanomaterials ◽  
2020 ◽  
Vol 10 (11) ◽  
pp. 2112 ◽  
Author(s):  
Antoine D’Hollander ◽  
Greetje Vande Velde ◽  
Hilde Jans ◽  
Bram Vanspauwen ◽  
Elien Vermeersch ◽  
...  
Keyword(s):  
Near Infrared ◽  
Tumor Imaging ◽  
Photoacoustic Imaging ◽  
Tumor Therapy ◽  
Infrared Region ◽  
Tumor Cell Death ◽  
Gold Nanostars ◽  
Theranostic Agents

Gold nanoparticles offer the possibility to combine both imaging and therapy of otherwise difficult to treat tumors. To validate and further improve their potential, we describe the use of gold nanostars that were functionalized with a polyethyleneglycol-maleimide coating for in vitro and in vivo photoacoustic imaging (PAI), computed tomography (CT), as well as photothermal therapy (PTT) of cancer cells and tumor masses, respectively. Nanostar shaped particles show a high absorption coefficient in the near infrared region and have a hydrodynamic size in biological medium around 100 nm, which allows optimal intra-tumoral retention. Using these nanostars for in vitro labeling of tumor cells, high intracellular nanostar concentrations could be achieved, resulting in high PAI and CT contrast and effective PTT. By injecting the nanostars intratumorally, high contrast could be generated in vivo using PAI and CT, which allowed successful multi-modal tumor imaging. PTT was successfully induced, resulting in tumor cell death and subsequent inhibition of tumor growth. Therefore, gold nanostars are versatile theranostic agents for tumor therapy.

scholarly journals Radiopharmaceutical and Eu3+ doped gadolinium oxide nanoparticles mediated triple-excited fluorescence imaging and image-guided surgery

2021 ◽  
Vol 19 (1) ◽  
Author(s):  
Xiaojing Shi ◽  
Caiguang Cao ◽  
Zeyu Zhang ◽  
Jie Tian ◽  
Zhenhua Hu
Keyword(s):  
Fluorescent Probes ◽  
Signal Intensity ◽  
Tumor Imaging ◽  
Tumor Resection ◽  
Optical Signal ◽  
Gadolinium Oxide ◽  
Image Guided Surgery ◽  
Guided Surgery ◽  
Image Guided ◽  
The Impact

AbstractCerenkov luminescence imaging (CLI) is a novel optical imaging technique that has been applied in clinic using various radionuclides and radiopharmaceuticals. However, clinical application of CLI has been limited by weak optical signal and restricted tissue penetration depth. Various fluorescent probes have been combined with radiopharmaceuticals for improved imaging performances. However, as most of these probes only interact with Cerenkov luminescence (CL), the low photon fluence of CL greatly restricted it’s interaction with fluorescent probes for in vivo imaging. Therefore, it is important to develop probes that can effectively convert energy beyond CL such as β and γ to the low energy optical signals. In this study, a Eu3+ doped gadolinium oxide (Gd2O3:Eu) was synthesized and combined with radiopharmaceuticals to achieve a red-shifted optical spectrum with less tissue scattering and enhanced optical signal intensity in this study. The interaction between Gd2O3:Eu and radiopharmaceutical were investigated using 18F-fluorodeoxyglucose (18F-FDG). The ex vivo optical signal intensity of the mixture of Gd2O3:Eu and 18F-FDG reached 369 times as high as that of CLI using 18F-FDG alone. To achieve improved biocompatibility, the Gd2O3:Eu nanoparticles were then modified with polyvinyl alcohol (PVA), and the resulted nanoprobe PVA modified Gd2O3:Eu (Gd2O3:Eu@PVA) was applied in intraoperative tumor imaging. Compared with 18F-FDG alone, intraoperative administration of Gd2O3:Eu@PVA and 18F-FDG combination achieved a much higher tumor-to-normal tissue ratio (TNR, 10.24 ± 2.24 vs. 1.87 ± 0.73, P = 0.0030). The use of Gd2O3:Eu@PVA and 18F-FDG also assisted intraoperative detection of tumors that were omitted by preoperative positron emission tomography (PET) imaging. Further experiment of image-guided surgery demonstrated feasibility of image-guided tumor resection using Gd2O3:Eu@PVA and 18F-FDG. In summary, Gd2O3:Eu can achieve significantly optimized imaging property when combined with 18F-FDG in intraoperative tumor imaging and image-guided tumor resection surgery. It is expected that the development of the Gd2O3:Eu nanoparticle will promote investigation and application of novel nanoparticles that can interact with radiopharmaceuticals for improved imaging properties. This work highlighted the impact of the nanoprobe that can be excited by radiopharmaceuticals emitting CL, β, and γ radiation for precisely imaging of tumor and intraoperatively guide tumor resection.

A Triple-responsive Targeted Hybrid Liposomes with High MRI Performance for Tumor Diagnosis and Therapy

2021 ◽  
Author(s):  
Weihe Yao ◽  
Chenyu Liu ◽  
Ning Wang ◽  
Hengjun Zhou ◽  
Hailiang Chen ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Tumor Therapy ◽  
Delivery Systems ◽  
Tumor Diagnosis ◽  
Diagnosis And Therapy ◽  
Promising Strategy ◽  
Therapy And Diagnosis

The targeted multi-responsive drug delivery systems with MRI capacity were anticipated as a promising strategy for tumor therapy and diagnosis. Herein, we successfully synthesized anisamide-modified and non-modified UV/GSH-responsive molecules (10,10-NB-S-S-P-AA...

Recent advances in microneedles for tumor therapy and diagnosis

2021 ◽  
Vol 23 ◽  
pp. 101036
Author(s):  
Shiyang Lin ◽  
Yi Cao ◽  
Jiajie Chen ◽  
Zhengfang Tian ◽  
Yufang Zhu
Keyword(s):  
Tumor Therapy ◽  
Recent Advances ◽  
Therapy And Diagnosis

Polymeric Matrix-Based Nanoplatforms toward Tumor Therapy and Diagnosis

2021 ◽  
pp. 21-48
Author(s):  
Houjuan Zhu ◽  
Xian Jun Loh ◽  
Enyi Ye ◽  
Zibiao Li
Keyword(s):  
Tumor Therapy ◽  
Polymeric Matrix ◽  
Therapy And Diagnosis

scholarly journals Phase I Trial of Polifeprosan 20 With Carmustine Implant Plus Continuous Infusion of Intravenous O6-Benzylguanine in Adults With Recurrent Malignant Glioma: New Approaches to Brain Tumor Therapy CNS Consortium Trial

2007 ◽  
Vol 25 (4) ◽  
pp. 399-404 ◽  
Author(s):  
Jon Weingart ◽  
Stuart A. Grossman ◽  
Kathryn A. Carson ◽  
Joy D. Fisher ◽  
Shannon M. Delaney ◽  
...  
Keyword(s):  
Phase I ◽  
Continuous Infusion ◽  
Phase I Trial ◽  
Tumor Therapy ◽  
Optimal Dose ◽  
Patient Cohort ◽  
Carmustine Wafers ◽  
Cohort Group ◽  
Group A ◽  
Group B

Purpose This phase I trial was designed to (1) establish the dose of O6-benzylguanine (O6-BG) administered intravenously as a continuous infusion that suppresses O6-alkylguanine-DNA alkyltransferase (AGT) levels in brain tumors, (2) evaluate the safety of extending continuous-infusion O6-BG at the optimal dose with intracranially implanted carmustine wafers, and (3) measure the pharmacokinetics of O6-BG and its metabolite. Patients and Methods The first patient cohort (group A) received 120 mg/m2 of O6-BG over 1 hour followed by a continuous infusion for 2 days at escalating doses presurgery. Tumor samples were evaluated for AGT levels. The continuous-infusion dose that resulted in undetectable AGT levels in 11 or more of 14 patients was used in the second patient cohort. Group B received the optimal dose of O6-BG for 2, 4, 7, or 14 days after surgical implantation of the carmustine wafers. The study end point was dose-limiting toxicity (DLT). Results Thirty-eight patients were accrued. In group A, 12 of 13 patients had AGT activity levels of less than 10 fmol/mg protein with a continuous-infusion O6-BG dose of 30 mg/m2/d. Group B patients were enrolled onto 2-, 4-, 7-, and 14-day continuous-infusion cohorts. One DLT of grade 3 elevation in ALT was seen. Other non-DLTs included ataxia and headache. For up to 14 days, steady-state levels of O6-BG were 0.1 to 0.4 μmol/L, and levels for O6-benzyl-8-oxoguanine were 0.7 to 1.3 μmol/L. Conclusion Systemically administered O6-BG can be coadministered with intracranially implanted carmustine wafers, without added toxicity. Future trials are required to determine if the inhibition of tumor AGT levels results in increased efficacy.

Inhibitory effect of carboxylic acid group on hERG binding

2006 ◽  
Vol 16 (21) ◽  
pp. 5507-5512 ◽  
Author(s):  
Bing-Yan Zhu ◽  
Zhaozhong J. Jia ◽  
Penglie Zhang ◽  
Ting Su ◽  
Wenrong Huang ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Acid Group ◽  
Inhibitory Effect ◽  
Carboxylic Acid Group

Synthesis of Novel Benzimidazole and Benzothiazole Derivatives Bearing a 1,2,3-triazole Ring System and their Acetylcholinesterase Inhibitory Activity

2017 ◽  
Vol 41 (1) ◽  
pp. 30-35 ◽  
Author(s):  
Laleh Faraji ◽  
Shiva Shahkarami ◽  
Hamid Nadri ◽  
Alireza Moradi ◽  
Mina Saeedi ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Docking Simulation ◽  
Triazole Ring ◽  
Copper Catalysts ◽  
Inhibitory Effect ◽  
Ring System ◽  
Benzothiazole Derivatives ◽  
Ache Inhibitory Activity ◽  
Group A

A series of 20 novel benzimidazole and benzothiazole derivatives linked to a 1,2,3-triazole ring system was synthesised, characterised and evaluated for in vitro acetylcholinesterase (AChE) inhibitory activity. Several copper catalysts and solvents were screened to establish the optimal conditions for the preparation of the target compounds. Three different linkers were used to optimise the enzyme inhibitory effect. Out of the 20 compounds, 13 showed some AChE inhibition. The most potent compound, which showed 84% inhibition at 100 μM, contained a 1-(2-fluorobenzyl)-1,2,3-triazole linked to a benzimidazole group. A docking simulation study showed that the most active compound bound preferentially to the catalytic anionic subsite of the AChE enzyme.

The Effect of Sho-saiko-to on Concentration of Vitamin E in Serum and on Granuloma Formation in Carrageenin Cotton Pellet-Induced Granuloma Rats

1994 ◽  
Vol 22 (02) ◽  
pp. 183-189 ◽  
Author(s):  
Kazuo Yoshida ◽  
Hiromi Mizukawa ◽  
Akie Honmura ◽  
Yasuhiko Uchiyama ◽  
Shigekatsu Nakajima ◽  
...  
Keyword(s):  
Vitamin E ◽  
Lipid Peroxide ◽  
Significant Negative Correlation ◽  
Inhibitory Effect ◽  
Granuloma Formation ◽  
Control Group ◽  
Serum Lipid Peroxide ◽  
Cotton Pellet ◽  
Group A ◽  
Inflammatory Effect

The effect of Sho-saiko-to on the concentration of vitamin E in serum and on the granuloma formation in Carrageenin cotton pellet-induced rats was investigated. As a result, in the granuloma rats of Sho-saiko-to group, a significantly improved inhibitory effect on granuloma formation and a higher concentration of vitamin E in serum, cholesterol and phospholipid were observed compared to the control group. Despite this lipid-increasing action by Sho-saiko-to, the concentration of serum lipid peroxide was significantly lower than in the control group. Furthermore, a significant negative correlation between the concentration of vitamin E and granuloma weight was observed. These results suggest that vitamin E plays an important role in promoting the anti-inflammatory effect of Sho-saiko-to.

scholarly journals Upconversion nanoparticle as a theranostic agent for tumor imaging and therapy

2016 ◽  
Vol 09 (04) ◽  
pp. 1630006 ◽  
Author(s):  
Wenkai Fang ◽  
Yanchun Wei
Keyword(s):  
Optical Properties ◽  
Tumor Imaging ◽  
Promising Material ◽  
Upconversion Nanoparticles ◽  
Multiphoton Absorption ◽  
Long Wavelength ◽  
Visible Wavelength ◽  
Theranostic Agent ◽  
Challenges And Opportunities ◽  
Wavelength Light

Upconversion nanoparticles (UCNPs) as a promising material are widely studied due to their unique optical properties. The material can be excited by long wavelength light and emit visible wavelength light through multiphoton absorption. This property makes the particles highly attractive candidates for bioimaging and therapy application. This review aims at summarizing the synthesis and modification of UCNPs, especially the applications of UCNPs as a theranostic agent for tumor imaging and therapy. The biocompatibility and toxicity of UCNPs are also further discussed. Finally, we discuss the challenges and opportunities in the development of UCNP-based nanoplatforms for tumor imaging and therapy.

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