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Scientists design novel anticancer agents by mimicking a herbal drug

In an attempt to fight cancer using synthetic compounds, scientists from the Indian Institute of Integrative Medicine (IIIM), Jammu, have synthesised 28 derivatives from bavachinin, a natural anticancer agent. The study, published in the European Journal of Medicinal Chemistry, explores the potential of these compounds to be used as a weapon against cancer. It was funded by the Council of Scientific and Industrial Research (CSIR), New Delhi.

Bavachinin belongs to a group of biologically active compounds called flavonoids. The medicinal herb Babchi (Psoralea corylifolia) is a major source of bavachinin. It is a common herb used in Ayurveda, Siddha and Chinese systems of medicine. Bavachinin has several beneficial effects—it is anticancer, antimicrobial, antiallergic and also acts against Alzheimer’s.

The researchers synthesised the anticancer agents by modifying the chemical structure of the parent compound bavachinin. To start the synthesis process, they extracted large amounts of bavachinin from the seeds of Psoralea corylifolia, or Bavanchiyan in Hindi. They then modified the chemical structure of the bavachinin molecule by reactions with different chemical compounds. For instance, for synthesising the compound called aliphatic ether, they made bavachinin react with chemicals alkyl halides and potassium carbonate. A group of chemicals was used for the synthesis of the rest of the derivatives.

The researchers checked if these synthetic compounds were effective against cancer cells by studying the activity of these compounds against four different human cancer cell lines. They tested the derivatives in cancerous cells from lung, prostate, colon and breast. The efficacy of the parent compound bavachinin was also studied to compare it with its synthetic derivatives.

The researchers found that many of the synthesised derivatives of bavachinin were able to kill cancerous cells and three of them were found to be up-and-coming anticancer agents. Surprisingly, one of those active compounds (a 1,2,3-triazole analog) was found to be three to four-fold more active than the parent molecule bavachinin in killing the cancer cells.

“All the experiments indicated the potential of the 1,2,3-triazole analog to develop as a potent anticancer agent”, say the researchers. When treated with this active compound, the cancer cells showed a significant change in their morphology and decrease in their capacity to form a colony.

Although reporting the anticancer activity of bavachinin derivatives is not new, the active compounds developed in the present study might provide a new dimension to the use of structural derivatives of herbal drugs for the treatment of cancer.