Fanke Zeng, Yuxiang Zhu, Xiaoyan Li, Ruyi Li, Lei Pan, Yaping Dai, Shaodan Peng, Lei Fang, Jihua Li, Wei Zhou
ABSTRACT Litchi seeds are by‐products produced from the fruit consumption, which contain rich phenolic compounds and have been traditionally used in inflammatory pain relief. This study sought to reveal phenolic profiles in the litchi seeds from different cultivars and explore their contributions to anti‐inflammatory, analgesic potentials. Purified polyphenols were derived from five cultivars of litchi seeds, including Baitangying (BTY), Baila (BL), Feizixiao (FZX), Heiye (HY), and Huaizhi (HZ). Fifteen flavonoids, two phenolic acids, one coumarin, and two tannins were characterized using UPLC‐Q/TOF‐MS, while procyanidin A 1 , procyanidin A 2 , and phlorizin were identified as major phenolic compounds in HPLC. HY contained relatively higher phenolic contents. The polyphenols from different cultivars effectively inhibited LPS‐induced generation of ROS, NO, IL‐6, TNF‐ α , and PGE 2 in RAW 264.7 macrophages, which was tightly associated with the contents of procyanidin A 1 , procyanidin A 2 , and phlorizin. Procyanidin A 1 played a relatively significant role, which could strongly bind to iNOS, COX‐2 and their mixture with procyanidin A 2 and phlorizin exhibited better effect in the NO inhibition. Furthermore, the litchi seed polyphenols were demonstrated to inhibit xylene‐induced ear edema and acetic acid‐induced abdominal writhing in mice. Thus, the litchi seed polyphenols possessed potentials to be utilized as anti‐inflammatory and analgesic agents.