PMID- 34041764 OWN - NLM STAT- MEDLINE DCOM- 20210722 LR - 20210722 IS - 1745-4514 (Electronic) IS - 0145-8884 (Linking) VI - 45 IP - 7 DP - 2021 Jul TI - Rat plasma protein binding of kaempferol-3-O-rutinoside from Lu'an GuaPian tea and its anti-inflammatory mechanism for cardiovascular protection. PG - e13749 LID - 10.1111/jfbc.13749 [doi] AB - Previous study found a high content of kaempferol-3-O-rutinoside (KR) in Lu'an GuaPian tea, however, the rat plasma protein binding and mechanism of KR for cardiovascular protection are unclear. Thus, we studied plasma protein binding using ultrafiltration followed by UPLC, and screened its inhibition against LPS-induced inflammation injury in vitro as well as the underlying mechanism by molecular docking and western blot. KR showed over 74% plasma protein binding ratio. Furthermore, KR may act on the toll-like receptor 4 (TLR4) and myeloid differentiation factor 88 (MyD88). In vitro experiments showed that KR decreases the overexpression of TLR4, MyD88, and nuclear factor-kappaB (NF-kappaB), which further validates the molecular docking results, suggesting that KR could block TLR4/MyD88/NF-kappaB signaling. These results indicate that KR could be a potential active agent in the protection of myocardial injury. PRACTICAL APPLICATIONS: Health benefits of tea are largely dependent on the intake of flavonoids. Flavonoids are a group of compounds beneficial to cardiovascular disease and an important part of "functional foods." Lu'an GuaPian tea is mainly produced in Lu'an City, Anhui Province and is one of the top 10 famous teas in China. Kaempferol-3-O-rutinoside in Lu'an GuaPian has good hypoglycemic effect, mainly manifested in a strong inhibition of alpha-glucosidase and alpha-amylase activities. Present study showed that kaempferol-3-O-rutinoside could block TLR4/MyD88/NF-kappaB signaling, suggesting that it could be a potential active agent in the protection of myocardial injury. CI - (c) 2021 Wiley Periodicals LLC. FAU - Hua, Fang AU - Hua F AD - Natural Products Laboratory, State Key Laboratory of Tea Plant Biology and Utilization, Anhui Agricultural University, Hefei, China. AD - School of Pharmacy, Anhui Xinhua University, Hefei, China. FAU - Zhou, Peng AU - Zhou P AD - Department of Integrated Traditional Chinese and Western Medicine, Anhui University of Chinese Medicine, Hefei, China. FAU - Liu, Pei-Pei AU - Liu PP AD - Department of Integrated Traditional Chinese and Western Medicine, Anhui University of Chinese Medicine, Hefei, China. FAU - Bao, Guan-Hu AU - Bao GH AUID- ORCID: 0000-0003-4336-5678 AD - Natural Products Laboratory, State Key Laboratory of Tea Plant Biology and Utilization, Anhui Agricultural University, Hefei, China. LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20210526 PL - United States TA - J Food Biochem JT - Journal of food biochemistry JID - 7706045 RN - 0 (Anti-Inflammatory Agents) RN - 0 (Kaempferols) RN - 0 (Tea) RN - 4056D20K3H (kaempferol-3-O-rutinoside) SB - IM MH - Animals MH - *Anti-Inflammatory Agents/pharmacology MH - China MH - Kaempferols MH - Molecular Docking Simulation MH - Protein Binding MH - Rats MH - *Tea OTO - NOTNLM OT - Lu'an GuaPian tea OT - TLR4/MyD88/NF-kappaB signaling OT - anti-inflammatory effects OT - kaempferol-3-O-rutinoside OT - plasma protein binding EDAT- 2021/05/28 06:00 MHDA- 2021/07/23 06:00 CRDT- 2021/05/27 07:06 PHST- 2021/04/13 00:00 [revised] PHST- 2021/02/05 00:00 [received] PHST- 2021/04/15 00:00 [accepted] PHST- 2021/05/28 06:00 [pubmed] PHST- 2021/07/23 06:00 [medline] PHST- 2021/05/27 07:06 [entrez] AID - 10.1111/jfbc.13749 [doi] PST - ppublish SO - J Food Biochem. 2021 Jul;45(7):e13749. doi: 10.1111/jfbc.13749. Epub 2021 May 26.