Anti-tumoral activity of native compound morelloflavone in glioma

Abstract

The aim of the study was to investigate the anti-tumoral activity of morelloflavone substances with different structures. We also studied the possible link between morelloflavone structure and its function. Various types of chromatographic techniques were used to isolate and screen morelloflavone substances from the extracts of gambogic tree trunk and the morelloflavone structures were identified by analytical techniques such as high resolution mass spectrometry and nuclear magnetism. Anti-tumoral activities of different compounds were investigated and the link between the antitumor activity and the structure of compound was exaimed. Our results showed that the isolated morelloflavone substances demonstrated a certain level of antitumor activity. The compound no. 1 had the strongest effect to inhibit glioma U87 and C6 cells followed by compound no. 2 while compound no. 5 was the weakest among them. We conducted a preliminary analysis on the structure-function relationship through the structure comparison and we concluded that the antitumor effects of morelloflavone substances with different structures were significantly different from each other. Thus, the glucose chain in C4 position of biflavone structure can enhance the antitumor activity of the compound in glioma cells. Additionally, the formation of intramolecular hydrogen bonds in biflavone compounds may also play a role in enhancing the antitumor activity and inhibition rate.

Potential Anticancer Agents Characterized from Selected Tropical Plants

“…(+)-Morelloflavone ( 61 ) was found to be inactive (IC 50 > 10 μM) when tested in a cell viability assay toward the HT-29 human colon cancer cell line . In addition, it was noncytotoxic toward both MCF-7 human breast cancer and U87 human glioma cells at a concentration up to 80 μM , and toward PC-3 human prostate cancer cells at a concentration up to 100 μM . However, (+)-morelloflavone ( 61 ) was found to effectively inhibit tumor angiogenesis.…”

Salts Influence Cathechins and Flavonoids Encapsulation in Liposomes: A Molecular Dynamics Investigation

“…Its antimicrobic properties recently emerged as inhibitor of bacterial efflux pumps . Moreover, it showed a promising antitumoral activity against glioma and it results also an inhibitor of Leshmania mexicana cysteine protease, thus showing Antileishmanial Activity . However, like all catechins and flavonoids, EGCG and MF have a high solubility in water due to the polyphenolic groups; they are easily oxidized and unstable, and hence, it is difficult to use them as drugs or as natural food additives.…”

Camboginol and Morelloflavone from Garcinia dulcis (Roxb.) Kurz Flower Extract Promote Autophagic Cell Death against Human Glioblastoma Cells through Endoplasmic Reticulum Stress

“…Morelloflavone from G. dulcis has antiangiogenesis in human umbilical vascular endothelial cell by targeting the activation of Rho-GTPases and extracellular signal-regulated kinase signaling pathways ( Pang et al, 2009 ). The isolated morelloflavone from the Gambogic tree trunk inhibited the growth of U87 and xenografted C6 glioma cells, which were associated with the formation of intramolecular hydrogen bonds in biflavone compounds ( Li et al, 2016 ).…”