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Eight phenolic glycosides, tachioside (1), isotachioside (2), koaburaside (3), 2,6-dimethoxy-4-hydroxyphenyl-1-O-beta-D-glucopyranoside (4), 4,6-dihydroxy-2-methoxyphenyl-1-O-beta-D-glucopyranoside (5), a mixture of erigeside C (6a) and salidroside (6b), and 6-hydroxyphenyl)-1-O-beta-D-glucopyranoside (7) were isolated from the stems of Lindera obtusiloba Blume. The structures of the isolates were determined by 1H-, 13C-NMR, COSY, HMQC, and HMBC spectroscopy. To evaluate their anti-allergic inflammatory activities, the inhibitory effects of isolates (1-7) on histamine release and on the gene expressions of tumor necrosis factor (TNF)-a and interleukin (IL)-6 were examined using human mast cells; previous studies have reported that TNF-alpha and IL-6 release from mast cells is positively related to the severity of allergic symptoms. Of the tested compounds, koaburaside (3), 2,6-dimethoxy-4-hydroxyphenyl-1-O-beta-D-glucopyranoside (4), and (6-hydroxyphenyl)-1-O-beta-D-glucopyranoside (7) suppressed histamine release from mast cells as compared with gallic acid (positive control). In particular, 6-hydroxyphenyl)-1-O-beta-D-glucopyranoside (7) attenuated the gene expressions of the proinflammatory cytokines TNF-alpha and IL-6 in human mast cells. Our results support the notion that phenolic glycosides isolated from L. obtusiloba inhibit mast-cell-derived allergic inflammation, histamine, and proinflammatory cytokines.


Hyun Gyu Choi, Hwa Dong Lee, Sang Hyun Kim, Min Kyun Na, Jeong Ah Kim, Seung Ho Lee. Phenolic glycosides from Lindera obtusiloba and their anti-allergic inflammatory activities. Natural product communications. 2013 Feb;8(2):181-2

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PMID: 23513723

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