Primaryin vitroandin vivoevaluation of norcantharidin-chitosan/poly (vinyl alcohol) for cancer treatment

Abstract

Two novel polymer-drug conjugates norcantharidin-poly(vinyl alcohol) and norcantharidinchitosan (NCTD-PVA and NCTD-CS) were synthesized via alcoholysis reaction and characterized by 1 H-NMR and FTIR. NCTD was released from the conjugates via hydrolysis, faster in PBS (pH 5.0) than that in PBS (pH 7.4). NCTD-PVA and NCTD-CS inhibited human esophageal carcinoma ECA-109 cell and murine breast cancer EMT6 cell growth in a dose-dependent manner. The IC 50 values of NCTD, NCTD-PVA and NCTD-CS on ECA-109 cell at 48 h were 9.4 AE 0.9, 55.3 AE 3.0 and 168.8 AE 8.9 mg/ml, respectively, and the IC 50 values of the three compounds on EMT6 cell were 3.1 AE 0.3, 30.5 AE 5.4 and 90.7 AE 8.1 mg/ml, respectively. The two conjugates both induced esophageal carcinoma ECA-109 cell apoptosis and arrested cell cycle at the S phase. Caspase-8 and caspase-3 were activated in the ECA-109 cell after incubating with NCTD-PVA or NCTD-CS. The primary in vivo antitumor activity was assessed in the EMT6 tumor-bearing mouse model. NCTD-PVA and NCTD-CS displayed higher tumor inhibition rates than that of free NCTD.

In-situ crosslinked nanofiber mats of chitosan/poly(vinyl alcohol) blend: Fabrication, characterization and MTT assay with cancerous bone cells

“…The acquired results propose that the cancerous bone cells did not grow in the presence of the incorporated constituents. Li et al showed the inhibition effect of CS or PVA on cancerous cells as NCTD-PVA and NCTD-CS inhibited human esophageal carcinoma ECA-109 cell and murine breast cancer EMT6 cell growth in a dose-dependent manner [30].…”

Planar Chiral Ferrocene Cyclopalladated Derivatives Induce Caspase-Dependent Apoptosis and Antimetastasis in Cancer Cells

“…The activities of caspase-3, -8, and -9 in SK-Hep-1 cells were assessed based on the specific protease-peptide substrate chromogenic reaction. , In brief, SK-Hep-1 cells cultured in 6-well plates at 4 × 10 5 cells/well were treated for 12 h with PBS (as control) and different concentrations of compound 7 . After that, the cells were harvested, lysed, and centrifugated.…”

Promising positive liver targeting delivery system based on arabinogalactan-anchored polymeric micelles of norcantharidin

“…While NCTD reduces the effects of cantharidin on the urinary system, it remains effective against liver cancer. NCTD has been shown to inhibit the growth of numerous cancer cell lines including liver cancer, esophageal cancer, gastric cancer and other cancers via apoptosis, autophagy and cell cycle arrest [1][2][3][4]. It increases white blood cell count, protects liver cells, regulates immunity, and does not cause bone marrow suppression.…”