In the laboratory of pharmacognosy and phytochemistry, we are studying natural products chemistry. We are investigating the possibility of producing drugs from natural products on the basis of organic chemistry, using two main methods.

【To find biologically active substances from natural resources】

①We are searching for natural inhibitors of angiogenesis, which plays an important role in the growth and progression of cancer, from the metabolites of marine micro-organisms, mushrooms and plants.

・KDR Kinase Inhibitor Isolated from the Mushroom Boletopsis leucomelas
A. Kaneko, J. Nat. Prod, 73, 1002-1004 (2010)
・Phenolic compounds from Cryptocarya konishii: their cytotoxic and tyrosine kinase inhibitory properties
F. Kurniadewi, J. Nat. Med., 64, 121-125 (2010)
・Phomactin I, 13-epi-Phomactin I and Phomactin J, three novel diterpenes from a marine-derived fungus
M. Ishino, et al., Tetrahedron Lett., 66, 2594-2597 (2010)
・Anti-angiogenic metabolites from a marine-derived fungus Hypocrea vinosa
Y. Ohkawa, et al., J. Nat. Prod.,73, 579-582 (2010)
・Phomactin H, a novel diterpene from an unidentified marine-derived fungus
K. Koyama, et al., Tetrahedron Lett., 45, 6947-6948 (2004)

②We are studying cactus saponins to find the possibility of new biological activities.

・New triterpene saponins from Stenocereus eruca (Cactaceae)
S. Okazaki, et al., J. Nat. Med., 61, 24-29 (2007)
・Triterpenoid saponins from cultural plants of Stenocereus stellatus (Cactaceae)
T. Imai., et al., J. Nat. Med., 60, 49-53 (2006)

③We are developing culture methods for lichen mycobionts to produce biological active substances and new effective compounds

・Antioxidant activity of red pigments from the lichens Lethariella sernanderi, L. cashmeriana, and L. sinensis
K. Kinoshita, et al., J. Nat. Med., 64, 85-88 (2010)
・Red Pigments from the Cultured Mycobiont of a lichen, Sphaerophorus fragilis
K. Kinoshita, et al., Lichenology, 8, 1-4 (2009)
・Fluorescent Compounds from the Cultured Mycobiont of Amygdalaria panaeola
K. Kinoshita., et al., J. Nat. Prod., 68, 1723-1727 (2005)
・A novel secondary metabolite from Lethariella sernanderi
K. Kinoshita, et al., Heterocycles, 63, 1023-1026 (2004)

④We are searching for inhibitors of b-secretase (BACE) which plays a critical role in the progression of Alzheimer’s disease (AD) from natural products.

・β-Secretase (BACE-1) inhibitory effect of biflavonoids
H. Sasaki, Bioorganic & Medicinal Chemistry Letters, 20, 4558-4560 (2010)

⑤We are researching for azole resistance anti-fungal component from natural sources.

【To develop new derivatives of the biological active natural products?the development of anti-influenza virus drugs】

①We are trying to synthesize new glycosides of biflavonoids and triterpenoids by coupling sialic acid from animal resources as a sugar moiety.

・Synthesis and evaluation of influenza virus sialidase inhibitory activity of hinokiflavone-sialic acid conjugates
K. Miki, et al., Heterocycles, 75, 879-885 (2008)
・New biflavonoids from Cephalotaxus harringtonia var. fastigiata (Cephalotaxaceae)
H. Sasaki, et al., Heterocycles, 75, 939-946 (2008)
・Anti-influenza virus activity of biflavonoids
K. Miki, et al., Bioorg. Med. Chem. Lett., 17, 772-775 (2007)

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