Anti-inflammatory composition containing macrolactin a and a...

A - Human Necessities – 61 – K

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A61K 31/365 (2006.01) A61P 29/00 (2006.01)

Patent

CA 2761254

The present invention relates to an anti-inflammatory use of macrolactin compounds such as macrolactin A, 7-O-malonyl macrolactin A, and 7-O-succinyl macrolactin A, which are produced from a novel Bacillus strain of Bacillus polyfermenticus KJS-2 (KCCM10769P). The macrolactin compounds provided by the present invention were confirmed to greatly suppress the expression and growth of inducible nitric oxide synthetase (iNOS) and cyclooxygenase-2 (COX-2) which are proteins related to the formation of inflammatory mediators, and to accordingly inhibit the formation of nitric oxide (NO) and of prostaglandin E2 (PGE2) which are the metabolites of the proteins. In addition, the macrolactin compounds provided by the present invention were confirmed to have excellent effects in inhibiting the formation of tumor necrosis factor-alpha (TNF-a), which is a pro-inflammatory cytokine, interleukin-1ß (IL-1ß), interleukin-6 (IL-6) and granulocyte macrophage colony-stimulating factor (GM-CSF). Therefore, the macrolactin compounds produced by the Bacillus polyfermenticus KJS-2 strain according to the present invention can provide excellent anti-inflammatory agents.

La présente invention concerne une utilisation anti-inflammatoire de composés macrolactine, notamment la macrolactine A, la 7-O-malonyl macrolactine A, et la 7-O-succinyl macrolactine A, qui sont produits à partir d'une nouvelle souche de bacille, le Bacillus polyfermenticus KJS-2 (KCCM10769P). Il a été confirmé que les composés macrolactine de l'invention suppriment considérablement l'expression et la croissance de la monoxyde d'azote synthase inductible (iNOS) et de la cyclo-oxygénase-2 (COX-2) en tant que protéines liées à la formation de médiateurs inflammatoires, et qu'ils inhibent en conséquence la formation de monoxyde d'azote (NO) et de prostaglandine E2 (PGE2), qui sont des métabolites des protéines. Il a été confirmé en outre que les composés macrolactine de l'invention ont un excellent effet inhibiteur de la formation du facteur de nécrose tumorale alpha (TNF-a) qui est une cytokine pro-inflammatoire, de l'interleucine-1ß (IL-1ß), de l'interleucine-6 (IL-6), et du facteur de stimulation de colonies de granulocytes-macrophages (GM-CSF). Ainsi, les composés macrolactine de l'invention, issus de la souche de Bacillus polyfermenticus KJS-2, peuvent constituer d'excellents agents anti-inflammatoires.

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