• Proceedings of the Korean Society of Applied Pharmacology
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• 2001.11a
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• pp.82-82
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• 2001

Previously, several prenylated flavonoids having a C-8 lavandulyl moiety were found to inhibit cyclooxygenase-1 (COX-1) as well as 5-lipoxygenase (5-LOX), and sophoraflavanone G was the most potent inhibitor against these eicosanoid generating enzymes among the prenylated flavonoids tested. In this investigation, effects of sophoraflavanone G on COX-2 induction from RAW 264.7 cells and in vivo inflammatory response were studied. Sophoraflavanone G inhibited prostaglandin E$_2$(PGE$_2$) production from lipopolysaccharide (LPS)-treated RAW cells by COX-2 down-regulation without significantly affecting COX-2 activity at 1 50 $\mu$M. Other prenylated flavonoids including kuraridin and sanggenon D also down-regulated COX-2 induction at 10-25 $\mu$M, lirhile kurarinone and echinoisoflavanone did not. In addition, sophoraflavanone G shelved in vivo anti-inflammatory activity against mouse croton oil-induced ear edema and rat carrageenan paw edema via oral (2-250mg/kg) or topical administration (10 - 250 $\mu\textrm{g}$/ear). Although the potencies of inhibition were far less than that of a reference drug, prednisolone, this compound showed higher anti-inflammato교 activity when applied topically, suggesting a potential use for several eicosanoid-related skin inflammation such as atopic dermatitis.

• Natural Product Sciences
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• v.27 no.3
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• pp.193-200
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• 2021

Sophora flavescens Ait. (Fabaceae) is a medicinal plant widely founded in Northeast Asia, and its dried root (Kushen) has been used as a traditional Chinese herbal medicine. The therapeutic effects of Kushen in micturition disorder was not investigated comprehensively yet. In the present study, we examined and compared the efficacy of three batches of Kushen extract using different ethanol content through an in vitro cell-based assay. Among them, we chose the batch with the highest efficacy and augmented the volume of extract for industrial purpose. The bulk extract was examined in its efficacy in the in vitro cell-based assay, and the therapeutic effects through an in vivo behavioral assay of OAB rats. The main components of the extracts were analyzed by liquid chromatography. Cytotoxicity of the extracts was investigated by MTT assay. The overall efficacy of the extract was as much as, or more than, kurarinone, a potent BK_Ca channel activator. Thus, the extract was a potent relaxant of urinary smooth muscle by upregulating the activity of BK_Ca channel. The Kushen extract could be explored as an alternative medicine against overactive bladder patients indicating severe dysfunction of BK_Ca channel.