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The screened triterpene acids from Loquat fruit by CysLTR1-immobilized column could serve as alternative
Tian Yang1,2,3, YiFan Yan1,3, YiYing Xu3
1Northwest University Chang An Hospital, Faculty of Life Sciences and Medicine, Northwest University, Xi'an, Shaanxi, 710069, China.
Background:
Loquat (Eriobotrya japonica Lindl.) fruit has been used as a heath food and folk medicine for preventing and treating the respiratory tract inflammation diseases, however, the active compounds responsible for anti-inflammation effects remain unclear.
Methods:
Cysteinyl leukotriene receptor-1 (CysLTR1) has become an important target protein for developing therapeutics to manage the inflammation-associated diseases. Herein, a rapid approach was established by immobilizing CysLTR1 onto microspheres for the column packing, and it was applied in screening the active compounds from Loquat fruit.
Results:
The screened compounds targeting CysLTR1 were identified as corosolic acid, ursolic acid and oleanolic acid in combination with Mass Spectrum. The high-dose combination of the three ones exhibited the stronger anti-inflammatory activity than triterpene acid alone and the Loquat extract, which can significantly decrease the counts of inflammatory cells and inhibit the production of pro-inflammatory mediators as well as increase the secretion of anti-inflammatory mediator in the LPS-inflamed mice. It was proved that three triterpene acids exhibited anti-inflammatory activities by the attenuation of CysLTR1 expression.
Conclusions:
Our results indicated that CysLTR1-immobilized column was a rapid and effective tool to seek out the target-specific components from herbal extract, and the screened triterpene acids could serve as alternative anti-inflammatory agents to Loquat fruit.
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