Biological Activity
vialinin a is a potent inhibitor of ubiquitin-specific peptidases with ic50 values of 1.5, 5.9 and 22.3 μm for ubiquitin-specific peptidase 4 (usp4), usp5/isopeptidase t (isot) and uch-l1 deubiquitinating enzyme (dub), respectively [1].ubiquitin-specific peptidases (usps) are a series of proteases that deubiquitinate target proteins. the dynamic modification of a protein with ubiquitin can modify its function, localization and fate in the cell. ubiquitin hydrolase plays an important role in immunology and infection [2].in rbl-2h3 cells, vialinin a inhibited tnf-ɑ production and release and inhibited usp5 enzymatic activity. in usp5 sirna-knockdown rbl-2h3 cells, vialinin a inhibited tnf-ɑ production and release in a dose dependent way. also, the mrna expression of tnf-ɑ was decreased significantly [2]. in rbl-2h3 cells, vialinin a inhibited tnf-ɑ production with ic50 value of 0.09 nm. also, it inhibited the release of interleukin 4, β-hexosaminidase and monocyte chemotactic protein 1, which suggested vialinin a had anti-allergic activities [3].
References
[1]. okada k, ye yq, taniguchi k, et al. vialinin a is a ubiquitin-specific peptidase inhibitor. bioorg med chem lett, 2013, 23(15): 4328-4331.
[2]. yoshioka y, ye yq, okada k, et al. ubiquitin-specific peptidase 5, a target molecule of vialinin a, is a key molecule of tnf-α production in rbl-2h3 cells. plos one, 2013, 8(12): e80931.
[3]. onose j, xie c, ye yq, et al. vialinin a, a novel potent inhibitor of tnf-alpha production from rbl-2h3 cells. biol pharm bull, 2008, 31(5): 831-833.
