- 标题
- 摘要
- 关键词
- 实验方案
- 产品
-
Glutathione Triggered Near Infrared Fluorescence Imaging-guided Chemotherapy by Cyanine Conjugated Polypeptide
摘要： Precise detection of tumor environment for cancer diagnosis was strongly demanded for further therapies. Here, a redox-responsive fluorescence switch off/on system PCQ was designed and synthesized conjugated with near infrared (NIR) cyanine dyes (Cy5.5) and relevant quencher (FQ) in mixed polymeric micelles (PCy and PFQ). The mixed PCQ micelles was prepared with two kinds of polymer with poly (oligo (ethylene glycol) methacrylate) (POEGMA) as the hydrophilic shell, in which fluorescence emission was quenched by fluorescence resonance energy transfer (FRET) effect. The FQ was conjugated with POEGMA by disulfide linkage, which could be broke with redox environment such as high glutathione (GSH) concentration in tumor cells. After the PCQ micelles got into tumor cells, PFQ block in PCQ would be disassembled to recompose PCy micelles. During that process, drugs like doxorubicin (DOX) could be loaded inside and formed PCQ@DOX nanoparticles and then released for accurate NIR bioimaging and drug delivery instantly.
关键词： redox responsive,polypeptide,imaging-guided,chemotherapy,Near infrared fluorescence (NIRF)
更新于2025-09-23 15:21:21
-
The near-infrared fluorescent dye IR-780 was coupled with cabazitaxel for castration-resistant prostate cancer imaging and therapy
摘要： A new drug, Caba-780, was synthesized by chemical coupling of the heptamethyl phthalocyanine near-infrared fluorescent (NIRF) dye IR-780 and the paclitaxel-based chemotherapeutic drug cabazitaxel. Then, the potential value of Caba-780 in the diagnosis and treatment of castration-resistant prostate cancer (CRPC) was evaluated. The CRPC cell lines DU145 and PC-3, as well as the normal human prostate stromal cell line WPMY-1, were used to evaluate the uptake of Caba-780 and its antitumor effect in vitro. The distribution, antitumor effect, and safety of Caba-780 were also evaluated in tumor-bearing mouse xenograft models. Our results showed that Caba-780 was efficiently absorbed by DU145 and PC-3 cells and that the cytotoxicity of Caba-780 was significantly stronger than that of IR-780 and cabazitaxel. In addition, Caba-780 inhibited the migration and invasion of DU145 and PC-3 cells and promoted apoptosis by prolonging the G2 phase of the cell cycle. Further analysis indicated that Caba-780 could be used to effectively image tumor xenografts. At the same time, this drug inhibited the growth of tumors in vivo. Therefore, the new synthetic drug Caba-780 has potential applications in the diagnosis and treatment of CRPC.
关键词： Organic anion-transporting polypeptide,Chemotherapy,Castration-resistant prostate cancer,Near-infrared fluorescent dye
更新于2025-09-23 15:21:01
-
PACAP through EGFR transactivation preserves human corneal endothelial integrity
摘要： The corneal endothelium is composed of a single hexagonal‐shaped cells layer adherent to the Descemet's membrane. The primary function of these cells is maintaining of tissue clarity by regulating its hydration. Trauma, aging or other pathologies cause their loss, counterbalanced by enlargement of survived cells fluid pumping to and from the stroma. unable to guarantee an efficient Regenerative medicine using human corneal endothelial cells (HCECs) isolated from peripheral corneal‐scleral tissue of a donor could be an attractive solution, overcoming transplantation problems. In a previous study, we have demonstrated that HCECs treatment with pituitary adenylate cyclase–activating polypeptide following growth factors deprivation prevents their degeneration. (PACAP) However, the molecular mechanism mediating this effect has not been clarified, yet. Here, we have shown for the first time the expression of PACAP and its receptor (PAC1R) in human corneal endothelium and demonstrated that this peptide, selectively binding to PAC1R, induces epidermal growth factor receptor (EGFR) phosphorylation and the MAPK/ERK1/2 signaling pathway activation. In conclusion, our data have suggested that PACAP could represent an important trophic factor in maintaining human corneal endothelial integrity through EGFR transactivation. Therefore, PACAP, as well as epidermal growth factor and fibroblast growth factor, could co‐operate to guarantee tissue physiological functioning by supporting corneal endothelial barrier integrity.
关键词： epidermal growth factor receptor,human corneal endothelial cells,mitogen‐activated protein kinase,pituitary adenylate cyclase–activating polypeptide
更新于2025-09-23 15:19:57
-
Sharp pH-responsive mannose prodrug polypeptide nanoparticles encapsulating a photosensitizer for enhanced near infrared imaging-guided photodynamic therapy
摘要： Mannose has been reported as a novel drug to kill cancer cells. The prodrug of mannose will promote its targeted delivery and enrichment at the tumor site and cancer cells. Here, a pH-sensitive polypeptide copolymer with a tertiary amine group has been prepared and a mannose molecule was conjugated to the polymer through the formation of a Schiff base. At the same time, an iodinated boron dipyrromethene (BDPI) photosensitizer with high singlet oxygen generation efficacy and near infrared (NIR) fluorescence was encapsulated by the nanoparticles, which makes it a potential pH-sensitive NIR imaging-guided chemotherapy/PDT agent. In vitro and in vivo studies reveal that in a tumor acidic environment, the protonation of the tertiary amine group destroyed the nanostructure of the nanoparticles, resulting in increased BDPI release. Meanwhile, the bond cleavage of the Schiff base led to the release of conjugated mannose and synergistic inhibition of tumor cell growth with the PDT effect was realized. The combination of these two kinds of tumor suppression effects and photodynamic therapy made this pH-sensitive polypeptide delivery system show great potential for further cancer therapy.
关键词： polypeptide nanoparticles,mannose prodrug,pH-responsive,photodynamic therapy,photosensitizer,near infrared imaging
更新于2025-09-16 10:30:52
-
Unusual Light-Tunable Thermoresponsive Behavior of OEGylated Homopolypeptide with Azobenzene and Thioether Spacers
摘要： OEGylated homopolypeptide (i.e., P(Azo-S-OEG7)) bearing azobenzene, thioether spacers, and oligo(ethylene glycol) OEG tails were prepared via a copper-mediated 1,3-dipolar cycloaddition. P(Azo-S-OEG7) showed an upper critical solution temperature (UCST)-type thermo-, light-, and oxidation-responsive in ethanol/water solvent mixtures. The UCST-type cloud point temperature (Tcp) decreased after UV irradiation and it increased after visible light irradiation due to the trans-cis isomerization of azobenzene moieties. P(Azo-S-OEG7) can be readily oxidized in the presence of H2O2, yielding P(Azo-SOX-OEG7) with sulfone or sulfoxide spacers. P(Azo-SOX-OEG7) showed an increase of UCST-type Tcp after UV irradiation and the Tcp decreased after visible light irradiation, which is an opposite trend to the UCST-type phase behavior of P(Azo-S-OEG7) as well as previous report. P(Azo-S-OEG7) showed poor water-solubility, yet it underwent H2O2 induced solution phase transition yielding P(Azo-SOX-OEG7) with lower critical solution temperature (LCST)-type phase behavior in water. The P(Azo-SOX-OEG7) aqueous solutions showed a decrease of LCST-type Tcp after UV irradiation and consequently Tcp decreased after visible light irradiation.
关键词： upper critical solution temperature,oxidation-responsive polymer,light-responsive polymer,polypeptide,lower critical solution temperature
更新于2025-09-04 15:30:14