Multifloroside Suppressing Proliferation and Colony Formation, Inducing S Cell Cycle Arrest, ROS Production, and Increasing MMP in Human Epidermoid Carcinoma Cell Lines A431

Abstract

Multifloroside (4), together with 10-hydroxyoleoside 11-methyl ester (1), 10-hydroxyoleoside dimethyl ester (2), and 10-hydroxyligustroside (3), are all secoiridoids, which are naturally occurring compounds that possess a wide range of biological and pharmacological activities. However, the anti-cancer activity of 1-4 has not been evaluated yet. The objective of this work was to study the anti-cancer activities of 1-4 in the human epidermoid carcinoma cell lines A431 and the human non-small cell lung cancer (NSCLC) cell lines A549. The results indicate that 1-4 differ in potency in their ability to inhibit the proliferation of human A431 and A549 cells, and multifloroside (4) display the highest inhibitory activity against A431 cells. The structure-activity relationships suggest that the o-hydroxy-p-hydroxy-phenylethyl group may contribute to the anti-cancer activity against A431 cells. Multifloroside treatment can also inhibit cell colony formation, arrest the cell cycle in the S-phase, increase the levels of reactive-oxygen-species (ROS), and mitochondrial membrane potential (MMP), but it did not significantly induce cell apoptosis at low concentrations. The findings indicated that multifloroside (4) has the tendency to show selective anti-cancer effects in A431 cells, along with suppressing the colony formation, inducing S cell cycle arrest, ROS production, and increasing MMP.

Metabolomics analysis of Ligustri Lucidi Fructus at different harvest times during the whole growing period based on ultra‐high‐performance liquid chromatography with mass spectrometry

“…These components have been reported to have many pharmacological activities. Forty (10‐Hydroxyligustroside) had inhibitory effects against human cancer cell lines A431 and A549 [47], 25 (oleoside 11‐methyl ester) could promote the activity of ROS‐detoxifying enzymes [48], 106 (salidroside) had anti‐tumor [49], anti‐osteoporosis and immunomodulatory effects [50], 12 (specnuezhenide) had the function of anti‐liver damage [51], 72 (nuezhenoside G13) [52] and 33 (neonuezhenide) [50] had antioxidant activity, which was related to the hepatoprotective effect of LLF.…”

Editorial to the Special Issue “Biological and Pharmacological Activity of Plant Natural Compounds”

“…Four different secoiridoids were studied for their potential anticancer effects on human epidermoid carcinoma (A431) and non-small cell lung cancer (A549) cell lines [ 7 ]. One of these compounds, multifloroside showed the highest inhibitory activity against A431 cells, with the ability to suppress colony formation, induce S cell cycle arrest, and increase reactive oxygen species (ROS) production and mitochondrial membrane potential.…”