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Small molecule PZL318: forming fluorescent nanoparticles capable of tracing their interactions with cancer cells and activated platelets, slowing tumor growth and inhibiting thrombosis.

Li S, Wang Y, Wang F, Wang Y, Zhang X, Zhao M, Feng Q, Wu J, Zhao S, Wu W, Peng S - Int J Nanomedicine (2015)

Bottom Line: In vivo, 10 nmol/kg of PZL318 slowed the tumor growth of S180 mice and alleviated the thrombosis of ferric chloride-treated ICR mice, while 100 μmol/kg of PZL318 did not injure healthy mice and they exhibited no liver toxicity.By using mesoscale simulation, a nanoparticle of 3.01 nm in diameter was predicted containing 13 trimers.Scavenging free radicals, downregulating sP-selectin expression and intercalating toward DNA were correlated with the antitumor mechanism of PZL318.

View Article: PubMed Central - PubMed

Affiliation: Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Beijing Laboratory of Biomedical Materials, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, College of Pharmaceutical Sciences of Capital Medical University, Beijing, People's Republic of China.

ABSTRACT
Low selectivity of chemotherapy correlates with poor outcomes of cancer patients. To improve this issue, a novel agent, N-(1-[3-methoxycarbonyl-4-hydroxyphenyl]-β-carboline-3-carbonyl)-Trp-Lys-OBzl (PZL318), was reported here. The transmission electron microscopy, scanning electron microscopy, and atomic force microscopy images demonstrated that PZL318 can form nanoparticles. Fluorescent and confocal images visualized that PZL318 formed fluorescent nanoparticles capable of targeting cancer cells and tracing their interactions with cancer cells. In vitro, 40 μM of PZL318 inhibited the proliferation of tumorigenic cells, but not nontumorigenic cells. In vivo, 10 nmol/kg of PZL318 slowed the tumor growth of S180 mice and alleviated the thrombosis of ferric chloride-treated ICR mice, while 100 μmol/kg of PZL318 did not injure healthy mice and they exhibited no liver toxicity. By analyzing Fourier transform-mass spectrometry and rotating-frame Overhauser spectroscopy (ROESY) two-dimensional nuclear magnetic resonance spectra, the chemical mechanism of PZL318-forming trimers and nanoparticles was explored. By using mesoscale simulation, a nanoparticle of 3.01 nm in diameter was predicted containing 13 trimers. Scavenging free radicals, downregulating sP-selectin expression and intercalating toward DNA were correlated with the antitumor mechanism of PZL318.

No MeSH data available.


Related in: MedlinePlus

TEM, SEM, and AFM images.Notes: (A) TEM image of PZL318 in ultrapure water (pH 7.0; 10−6 M) and the diameter of the smallest nanoparticle is 3 nm. (B) SEM image of the powders from the aqueous solution of PZL318 (pH 7.0; 10−6 M). (C) These arrowheads were used to note the calculated area of minimum and maximum nano-sizes on the black line. AFM image of PZL318 in rat plasma and the diameter of the nanoparticles is ~47 nm.Abbreviations: TEM, transmission electron microscopy; SEM, scanning electron microscopy; AFM, atomic force microscopy.
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f5-ijn-10-5273: TEM, SEM, and AFM images.Notes: (A) TEM image of PZL318 in ultrapure water (pH 7.0; 10−6 M) and the diameter of the smallest nanoparticle is 3 nm. (B) SEM image of the powders from the aqueous solution of PZL318 (pH 7.0; 10−6 M). (C) These arrowheads were used to note the calculated area of minimum and maximum nano-sizes on the black line. AFM image of PZL318 in rat plasma and the diameter of the nanoparticles is ~47 nm.Abbreviations: TEM, transmission electron microscopy; SEM, scanning electron microscopy; AFM, atomic force microscopy.

Mentions: The nanofeature of PZL318 was visualized with TEM, SEM, and AFM images. The TEM image (Figure 5A) is characterized by the nanoparticles of 3–150 nm in diameter (90% were <100 nm). The SEM image (Figure 5B) is characterized by the nanoparticles of 3.01–36.7 nm in diameter. The AFM image (Figure 5C) is characterized by the nanoparticles of ~47 nm in diameter. The TEM, SEM, and AFM images consistently visualize the nanoscale self-assembly and the formation of nanoparticles of PZL318.


Small molecule PZL318: forming fluorescent nanoparticles capable of tracing their interactions with cancer cells and activated platelets, slowing tumor growth and inhibiting thrombosis.

Li S, Wang Y, Wang F, Wang Y, Zhang X, Zhao M, Feng Q, Wu J, Zhao S, Wu W, Peng S - Int J Nanomedicine (2015)

TEM, SEM, and AFM images.Notes: (A) TEM image of PZL318 in ultrapure water (pH 7.0; 10−6 M) and the diameter of the smallest nanoparticle is 3 nm. (B) SEM image of the powders from the aqueous solution of PZL318 (pH 7.0; 10−6 M). (C) These arrowheads were used to note the calculated area of minimum and maximum nano-sizes on the black line. AFM image of PZL318 in rat plasma and the diameter of the nanoparticles is ~47 nm.Abbreviations: TEM, transmission electron microscopy; SEM, scanning electron microscopy; AFM, atomic force microscopy.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4554418&req=5

f5-ijn-10-5273: TEM, SEM, and AFM images.Notes: (A) TEM image of PZL318 in ultrapure water (pH 7.0; 10−6 M) and the diameter of the smallest nanoparticle is 3 nm. (B) SEM image of the powders from the aqueous solution of PZL318 (pH 7.0; 10−6 M). (C) These arrowheads were used to note the calculated area of minimum and maximum nano-sizes on the black line. AFM image of PZL318 in rat plasma and the diameter of the nanoparticles is ~47 nm.Abbreviations: TEM, transmission electron microscopy; SEM, scanning electron microscopy; AFM, atomic force microscopy.
Mentions: The nanofeature of PZL318 was visualized with TEM, SEM, and AFM images. The TEM image (Figure 5A) is characterized by the nanoparticles of 3–150 nm in diameter (90% were <100 nm). The SEM image (Figure 5B) is characterized by the nanoparticles of 3.01–36.7 nm in diameter. The AFM image (Figure 5C) is characterized by the nanoparticles of ~47 nm in diameter. The TEM, SEM, and AFM images consistently visualize the nanoscale self-assembly and the formation of nanoparticles of PZL318.

Bottom Line: In vivo, 10 nmol/kg of PZL318 slowed the tumor growth of S180 mice and alleviated the thrombosis of ferric chloride-treated ICR mice, while 100 μmol/kg of PZL318 did not injure healthy mice and they exhibited no liver toxicity.By using mesoscale simulation, a nanoparticle of 3.01 nm in diameter was predicted containing 13 trimers.Scavenging free radicals, downregulating sP-selectin expression and intercalating toward DNA were correlated with the antitumor mechanism of PZL318.

View Article: PubMed Central - PubMed

Affiliation: Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Beijing Laboratory of Biomedical Materials, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, College of Pharmaceutical Sciences of Capital Medical University, Beijing, People's Republic of China.

ABSTRACT
Low selectivity of chemotherapy correlates with poor outcomes of cancer patients. To improve this issue, a novel agent, N-(1-[3-methoxycarbonyl-4-hydroxyphenyl]-β-carboline-3-carbonyl)-Trp-Lys-OBzl (PZL318), was reported here. The transmission electron microscopy, scanning electron microscopy, and atomic force microscopy images demonstrated that PZL318 can form nanoparticles. Fluorescent and confocal images visualized that PZL318 formed fluorescent nanoparticles capable of targeting cancer cells and tracing their interactions with cancer cells. In vitro, 40 μM of PZL318 inhibited the proliferation of tumorigenic cells, but not nontumorigenic cells. In vivo, 10 nmol/kg of PZL318 slowed the tumor growth of S180 mice and alleviated the thrombosis of ferric chloride-treated ICR mice, while 100 μmol/kg of PZL318 did not injure healthy mice and they exhibited no liver toxicity. By analyzing Fourier transform-mass spectrometry and rotating-frame Overhauser spectroscopy (ROESY) two-dimensional nuclear magnetic resonance spectra, the chemical mechanism of PZL318-forming trimers and nanoparticles was explored. By using mesoscale simulation, a nanoparticle of 3.01 nm in diameter was predicted containing 13 trimers. Scavenging free radicals, downregulating sP-selectin expression and intercalating toward DNA were correlated with the antitumor mechanism of PZL318.

No MeSH data available.


Related in: MedlinePlus