AsianScientist (Dec. 3, 2020) – By combining natural compounds, scientists in Japan have created novel anticancer drugs with potentially minimal side effects. Their findings were published in American Chemical Society Omega.
Before COVID-19 came about, perhaps the most prominent disease in our collective consciousness was cancer—and with good reason. Globally, about one in every six deaths is attributed to the disease. Despite this, a cancer diagnosis is far from a death sentence nowadays, largely due to the efforts of scientists working around the clock to stop the disease in its tracks.
In hopes of adding another weapon to the arsenal against cancer, researchers led by Professor Kouji Kuramochi from the Tokyo University of Science turned to organic compounds called phenazines. Within this group, N-alkylphenazin-1-ones represent a promising group of phenazine compounds in the fight against cancer. Found naturally in bacteria, phenazines have antibacterial, antifungal and even cytotoxic activities—meaning that the compounds are also toxic to cells, including their malignant counterparts.
However, N-alkylphenazin-1-ones have proven difficult to derive from bacteria. This inspired Kuramochi and his team to synthesize the compounds instead. By adding halogen elements like chlorine and bromine as well as oxidants and water to various phenazines, the researchers were able to selectively synthesize novel compounds with potential anticancer activity.
One halogenated phenazine in particular, namely 2-chloropyocyanin, was observed to have high cytotoxicity towards lung cancer cells. Overall, the resulting phenazines were more than four times more toxic to cancer cells compared to normal cells. Accordingly, using these compounds in cancer treatment should come with fewer side effects due to their targeted approach.
Notably, the team’s new technique overcomes one of the main drawbacks of existing phenazine synthesis methods. Traditionally, when chlorine is used to produce N-alkylphenazin-1-ones, undesirable products are formed. Moreover, through the technique, the researchers were able to synthetically produce lavanducyanin—typically isolated from Streptomyces sp. bacteria—for the first time. Even better, the whole process is environmentally-friendly, according to Kuramochi.
As promising as these results may be, it’s early days yet. Now, the team is hoping to verify the effects of the novel compounds through animal studies and later on, clinical trials.
“We have established a highly versatile synthetic method that is simple and can be applied to the synthesis of many natural products,” concluded Kuramochi.
The article can be found at: Kohatsu et al. (2020) Synthesis and Cytotoxic Evaluation of N-Alkyl-2-halophenazin-1-ones.
Source: Tokyo University of Science; Photo: National Institutes of Health/Flickr.
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