<p>A Gastric Cancer Peptide GX1-Modified Nano-Lipid Carriers Encapsulating Paclitaxel: Design and Evaluation of Anti-Tumor Activity</p>

Abstract

The aim of this study was to develop a GX1-modified nanostructured lipid carrier (NLCs) and to evaluate its ability to improve the anti-gastric cancer tumor effects of paclitaxel (PTX). Main Methods: The GX1-modified NLCs were synthesized and loaded with PTX (GX1-PTX-NLCs) by emulsion solvent evaporation technique. The anti-tumor activity and pharmacodynamics were then evaluated by in vitro cell studies and animal experiments. Key Findings: The GX1-modified NLCs were successfully synthesized and confirmed by 1 H NMR and MALDI-TOF-MS. PTX-loaded NLCs produced particles with average size distribution less than or equal to 222 nm and good drug loading and entrapment efficiency. In vitro studies demonstrated that GX1-PTX-NLCs had a more obvious inhibitory effect on Co-HUVEC cells than PTX and unmodified PTX-NLCs. The cellular uptake results also showed that GX1-PTX-NLCs were largely concentrated in Co-HUVEC cells, and the uptake rates of GX1-PTX-NLCs in Co-HUVEC were higher than those of the free drug and the PTX-NLC. In vivo studies demonstrated that GX1-PTX-NLCs possess strong anti-tumor effect and showed higher tumor growth inhibition and lower toxicity in nude mice. Significance: These results suggest that GX1-modified NLCs enhanced the anti-tumor activity of PTX and reduced its toxicity effectively. GX1-PTX-NLCs may be considered as a potent drug delivery system for therapy of gastric cancer.

Peptide-assembled nanoparticles targeting tumor cells and tumor microenvironment for cancer therapy

“…GX1, the cyclic 7-mer peptide motif CGNSNPKSC, was identified as a human gastric tumor vasculature homing peptide at first and bound to transglutaminase-2 (TMG2) to inhibit angiogenesis ( Lei et al, 2018 ). The GX1-modified liposomes have been used to treat gastric cancer, such as GX1-modified liposomes encapsulating PTX (GX1-PTX-NLCs) and GX1-mediated anionic liposomes carrying adenoviral vectors integrating with the tumor suppressor gene of PTEN (GX1-Ad5-AL), which all promoted the cellular uptake by HUVEC cells, enhanced the inhibition of HUVEC cells and significantly suppressed the migration of gastric cancer cell in vitro ( Xiong et al, 2015 ; Jian et al, 2020 ). In vivo studies demonstrated that GX1-PTX-NLCs significantly inhibited tumor growth with lower toxicity in MKN45 tumor-bearing nude mice model ( Jian et al, 2020 ).…”

“…The GX1-modified liposomes have been used to treat gastric cancer, such as GX1-modified liposomes encapsulating PTX (GX1-PTX-NLCs) and GX1-mediated anionic liposomes carrying adenoviral vectors integrating with the tumor suppressor gene of PTEN (GX1-Ad5-AL), which all promoted the cellular uptake by HUVEC cells, enhanced the inhibition of HUVEC cells and significantly suppressed the migration of gastric cancer cell in vitro ( Xiong et al, 2015 ; Jian et al, 2020 ). In vivo studies demonstrated that GX1-PTX-NLCs significantly inhibited tumor growth with lower toxicity in MKN45 tumor-bearing nude mice model ( Jian et al, 2020 ). GX1-conjugated poly (lactic acid) nanoparticles encapsulating Endostar, a novel recombinant human endostatin, and labeled with the near-infrared dye were developed for colorectal cancer targeting and therapy in vivo , which accumulated in tumor site and improved antitumor efficacy in the colorectal mouse model ( Du et al, 2015 ).…”

The Anticancer Potential of Maslinic Acid and Its Derivatives: A Review

“…53 Furthermore, another study also showed that MA inhibited Epstein-Barr virus (EBV) early-antigen expression in Raji cells with an IC 50 value of 0.1 ± 0.04 μg/mL. Phorbol 12-myristate 13-acetate (PMA) can also induce early-antigen EBV expression; the antitumor activity of MA may be attributed to its hydrophilic moieties interacting with protein kinase C, which prevents PMA from binding and activating protein kinase C. 54…”

Anti-Gastric Cancer Activity of the Cell-free Culture Supernatant of Serofluid Dish and Lactiplantibacillus plantarum YT013

“…The predominant gastric cancer diagnosed cases are a type referred to as adenocarcinoma of the stomach and develop from the cells of superficial stomach mucous membrane ( Wang et al, 2019 ). In recent years, the age of onset of gastric cancer has decreased, and the morbidity has increased ( Jian et al, 2020 ). As most gastric cancer patients are diagnosed at the late stage, the response to chemotherapy is often very poor, resulting in long-term and serious side effects and a very low 5-years survival rate.…”