A new study describes the laboratory synthesis of the most active component of grape seed extract, B2G2, and shows this synthesised compound induces the cell death known as apoptosis in prostate cancer cells while leaving healthy cells unharmed.
"We've shown similar anti-cancer activity in the past with grape seed extract (GSE), but now we know B2G2 is its most biologically active ingredient which can be synthesised in quantities that will allow us to study the detailed death mechanism in cancer cells," said Alpna Tyagi, of the University of Colorado Skaggs School of Pharmacy and Pharmaceutical Sciences.
The group has spent more than a decade demonstrating the anti-cancer activity of GSE in controlled, laboratory conditions.
For example, previous studies have shown the GSE effectiveness against cancer cells and have also shown its mechanism of action.
"But until recently, we didn't know which constituent of GSE created this effect. This naturally occurring compound, GSE, is a complex mixture of polyphenols and also so far it has been unclear about the biologically active constituents of GSE against cancer cells," said Tyagi, who works in the lab of CU Cancer Center investigator, Chapla Agarwal.
Eventually the group pinpointed B2G2 as the most active compound, but, "it's expensive and it takes a long time to isolate B2G2 from grape seed extract," Tyagi said.
So instead of purifying B2G2 from GSE, the group decided to synthesise it in the lab. The study reported the success of this effort, including the ability to synthesise gram-quantity of B2G2 reasonably
quickly and inexpensively.
The group showed anti-cancer activity of synthesised B2G2 similar in mechanism and degree to overall GSE effectiveness.
"Our goal all along has been a clinical trial of the biologically active compounds from GSE against human cancer. But it's difficult to earn FDA approval for a trial in which we don't know the mechanisms and possible effects of all active components.
"Therefore, isolating and synthesising B2G2 is an important step because now we have the ability to conduct more experiments with the pure compound. Ongoing work in the lab further increases our understanding of B2G2's mechanism of action that will help for the preclinical and clinical studies in the future," said Tyagi.
The study was published in the journal Nutrition and Cancer.