Heterophyllin B

Heterophyllin B inhibits the adhesion and invasion of ECA-109 human esophageal carcinoma cells by targeting PI3K/AKT/β-catenin signaling.[Pubmed: 26647768 ]

Mol Med Rep. 2016 Feb;13(2):1097-104.

The present study aimed to measure the effect of Heterophyllin B (HB) on the adhesion and invasion of ECA-109 human esophageal carcinoma cells, and examine the possible mechanism involved.
METHODS AND RESULTS:
A Cell Counting kit 8 assay was performed to determine the cell viability. Cell adhesion and invasion were determined following treatment of the ECA-109 cells with HB (0, 10, 25 and 50 μM) for 24 h. The levels of phosphorylated (p-)ATK and p-phosphoinositide 3-kinase (PI3K), and the protein levels of β-catenin were measured using western blot analysis. The mRNA and protein expression levels of E-cadherin, vimentin, snail, matrix metalloproteinase (MMP)2 and MMP9 were detected using reverse transcription-quantitative polymerase chain reaction and western blot analyses, respectively. HB (10, 25 and 50 μM) significantly suppressed the adhesion and invasion of the ECA-109 human esophageal carcinoma cells in a dose-dependant manner. The expression levels of p-ATK, p-PI3K and β-catenin were markedly decreased. The expression of E-cadherin was promoted, whereas the expression levels of snail, vimentin, MMP 2 and MMP 9 were decreased significantly in the ECA-109 cells treated with HB. In addition, HB inhibited the adhesion and invasion induced by PI3K activating peptide in the ECA-109 cells, and the protein expression levels were also adjusted.
CONCLUSIONS:
These results suggested that HB effectively suppressed the adhesion and invasion of the human esophageal carcinoma cells by mediating the PI3K/AKT/β-catenin pathways and regulating the expression levels of adhesion- and invasion-associated genes.

Biomed Chromatogr. 2015 Nov;29(11):1693-9.

LC-ESI-MS/MS analysis and pharmacokinetics of heterophyllin B, a cyclic octapeptide from Pseudostellaria heterophylla in rat plasma.[Pubmed: 25967583]

Heterophyllin B (HB) is a cyclic octapeptide isolated from Pseudostellaria heterophylla. Heterophyllin B is used as the quality control index for evaluating P. heterophylla in the Chinese Pharmacopoeia.
METHODS AND RESULTS:
A rapid and sensitive LC-ESI-MS/MS method was developed and validated for the analysis of Heterophyllin B in rat plasma. Sample preparation consisted of a solid-phase extraction step for the removal of interference and preconcentration of the target analyte Heterophyllin B and the internal standard N-acetylcysteine before chromatographic analysis by MS/MS detection. The separation of Heterophyllin B and N-acetylcysteine was performed using a Hypersil GOLDTM C18 column and a mixture of methanol-water (60:40, v/v) containing 10 mmol/L ammonium formate and 0.1% formic acid as the mobile phase. The determination step was optimized in the selected reaction monitoring mode for the highly selective and sensitive quantitation of Heterophyllin B in rat plasma. Intra- and inter-assay precision (as relative standard deviation) was ≤9.1%, and accuracy was between 92.6 and 102.7%. The validated method was successfully applied to quantify Heterophyllin B concentrations up to 7 h after tail intravenous injections of 2.08, 4.16 and 8.32 mg/kg Heterophyllin B in rats.
CONCLUSIONS:
The LC-MS/MS method identified the relevant pharmacokinetic parameters of Heterophyllin B and its studied analog.