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Natural Products for Drug Discovery(Chemistry)

Arai MasayoshiProfessor

My life's work is “Finding secondary metabolites with diverse chemical structures like works of art, and elucidating how they react chemically with molecules in the body to produce medicinal effects”. I am also conducting research with the goal of creating “novel pharmaceutical seeds” from these studies and linking them to drug discovery in academia.

Research theme

Exploring novel pharmaceutical seeds from marine medicinal resources.

Researchers around the world are conducting pathological analysis for various diseases, and the achievements are reported in scientific journal and at national and international conferences. We are constantly incorporating the latest such information, constructing a screening system to find novel pharmaceutical seeds for various intractable diseases such as cancer and infectious diseases, and search for pharmaceutical seeds from our own library of marine medicinal resources.

Target identification of bioactive natural products.

In order to develop the discovered bioactive natural products as pharmaceutical leads, it is necessary to clarify their mechanism of action and target molecules. Target identification of bioactive natural products is also important research that leads to the development of new drug targets. We utilize the methods of chemical biology and chemical genetics to analyze the mechanism of action and target molecules of the bioactive natural products.

Expansion and advancement of marine medicinal resource library.

We are collaborating with overseas universities and research institutes to construct the extract library from marine organisms and cultured marine-derived microorganisms. Furthermore, to expand the diversity of compounds contained in cultured extracts of marine-derived microorganisms, we are also studying methods to activate dormant secondary metabolite biosynthesis genes that are not expressed under normal culture conditions.

Representative achievements

Y. Sumii, K. Kamiya, T. Nakamura, K. Tanaka, T. Kaji, N. Kotoku, M. Arai, Structure activity relationship study of 3-(Phenethylamino)demethyl(oxy)aaptamine as an anti-dormant mycobacterial substance to create probe molecule for detecting target protein. Mar Drugs (2022) 20 (2), 98.

R. Tang, D. Zhou, A. Kimishima, A. Setiawan, M. Arai, Selective cytotoxicity of marine-derived fungal metabolite (3S,6S)-3,6-dibenzylpiperazine-2,5-dione against cancer cells adapted to nutrient starvation. J. Antibiot. (2020) 73 (12), 873-875.

R. Tang, A. Kimishima, R. Ishida, A. Setiawan, M. Arai, Selective cytotoxicity of epidithiodiketopiperazine DC1149B, produced by marine-derived Trichoderma lixii on the cancer cells adapted to glucose starvation. J. Nat. Med. (2020) 74 (1), 153-158.

T. Jomori, Y. Hara, M. Sasaoka, K. Harada, A. Setiawan, K. Hirata, A. Kimishima, M. Arai, Mycobacterium smegmatis alters the production of secondary metabolites by marine-derived Aspergillus niger. J. Nat. Med. (2020) 74 (1), 76-82.

T. Kawachi, S. Tanaka, A. Fukuda, Y. Sumii, A. Setiawan, N. Kotoku, M. Kobayashi, M. Arai, Target identification of the marine natural products dictyoceratin-A and -C as selective growth inhibitors in cancer cells adapted to hypoxic environments. Mar. Drugs (2019) 17(3), E163.