COX-2 and JAK3 inhibitory meroterpenoids from the mushroom Ganoderma theaecolum

Ganoderma mushrooms possess antioxidant, anticancer, and immunomodulatory properties. In this study, eleven new meroterpenoids, ganotheaecolumols A-K (1–6, 10,11, 13, 14, and 17), together with nine known ones (7–9, 12, 15, 16, and 18–20) were isolated from the fruiting bodies of G. theaecolum. Thei...

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Bibliographic Details
Published in:Tetrahedron 2018-08, Vol.74 (31), p.4259-4265
Main Authors: Luo, Qi, Li, Min-Ke, Luo, Jing-Feng, Tu, Zheng-Chao, Cheng, Yong-Xian
Format: Article
Language:English
Subjects:
COX-2
Ganoderma theaecolum
Ganotheaecolumols A−K
JAK3
Meroterpenoids
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Summary:Ganoderma mushrooms possess antioxidant, anticancer, and immunomodulatory properties. In this study, eleven new meroterpenoids, ganotheaecolumols A-K (1–6, 10,11, 13, 14, and 17), together with nine known ones (7–9, 12, 15, 16, and 18–20) were isolated from the fruiting bodies of G. theaecolum. Their structures were elucidated by spectroscopic and computational methods. All the new compounds and iso-ganotheaecolumol I (12) were tested for their inhibitory activities against COX-2 and JAK3 kinases, and cytotoxic effects. It was found that most meroterpenoids could inhibit COX-2 and JAK3 with compounds 3, 4, 12, 13, and 17 having IC50 values of 1.05 ± 0.10, 1.38 ± 0.11, 2.61 ± 0.79, 3.47 ± 0.58, and 4.84 ± 0.60 μM towards COX-2. Whereas, none of the test compounds exhibited cytotoxic effects against human cancer cells (K562, A549, and Huh-7). [Display omitted]
ISSN:0040-4020
1464-5416
DOI:10.1016/j.tet.2018.06.053