Tea Seed Kaempferol Triglycoside Attenuates LPS-Induced Systemic Inflammation and Ameliorates Cognitive Impairments in a Mouse Model.

(1) Background: The current research intended to obtain functional compounds from agricultural by-products. A functional tea seed flavonoid, kaempferol-3-O-[2-O-β-d-xylopyranosyl-6-O-α-L-rhanmopyranosyl]-β-d-glucopyranoside (KXRG), was isolated from tea seed dregs. We further determined its chemical structure and evaluated the protective effects of KXRG against local and systemic inflammation in vivo; (2) Methods: First, cytotoxicity and proinflammatory cytokine release were examined in a cell-culture system. The biological activities of KXRG were investigated in a mouse model of ear edema, and from inflammatory damage to organs as demonstrated by histologic examination, in addition to brain function evaluation using the Y-maze test. Serum biochemical analysis and western blotting were utilized to explore the related cellular factors; (3) Results: KXRG inhibited IL-6 in RAW264.7 cells at a non-toxic concentration. Further experiments confirmed that KXRG exerted a stronger effect than indomethacin in terms of the prevention of 12-O-tetradecanoylphorbol acetate (TPA)-induced ear inflammation in a mouse model. KXRG feeding significantly prevented LPS-induced small intestine, liver, and kidney inflammatory damage, as demonstrated by histologic examination. KXRG also significantly improved LPS-induced cognitive impairments. Serum biochemical analysis showed that KXRG elevated antioxidant capacity and reduced levels of proinflammatory cytokines. Western blotting revealed that KXRG reduced the COX-2 expression induced by LPS in mouse tissues; (4) Conclusions: KXRG can be purified from agricultural waste, and hence it is inexpensive, with large amounts of raw materials available. Thus, KXRG has strong potential for further development as a wide-use anti-systemic inflammation drug to prevent human disease.