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地枫皮中新木脂素 difengpienol C 的结构鉴定及抗炎机制研究。

Structure elucidation and anti-inflammatory mechanism of difengpienol C, a new neolignan isolated from Illicium difengpi.

机构信息

Guangxi Key Laboratory of Functional Phytochemicals Research and Utilization, Guangxi Institute of Botany, Chinese Academy of Sciences, Guilin 541006, China.

Guangxi Key Laboratory of Functional Phytochemicals Research and Utilization, Guangxi Institute of Botany, Chinese Academy of Sciences, Guilin 541006, China.

出版信息

Fitoterapia. 2021 Sep;153:104949. doi: 10.1016/j.fitote.2021.104949. Epub 2021 Jun 2.

DOI:10.1016/j.fitote.2021.104949
PMID:34087408
Abstract

Illicium difengpi is well-known as its stem barks that have been widely used in the Traditional Chinese Medicine (TCM) for therapy rheumatoid arthritis and traumatic injury. To comprehensive utilization of resources, the phytochemical investigation on the branches and leaves of this plant was carried out, which led to the isolation of an undescribed neolignan along with three known lignans. Their structures were elucidated on the basis of extensive spectroscopic data and the new compound was elucidated as a neolignan possessing a dihydropyran ring formed by a unique conjugation way and named difengpienol C. Difengpienol C showed the strongest anti-inflammatory activity in lipopolysaccharide (LPS)-stimulated RAW264.7 cells, which powerfully inhibited nitric oxide (NO), interleukin 6 (IL-6), tumor necrosis factor α (TNF-α) production and suppressed the mRNA transcription of inducible nitric oxide synthase (iNOS), IL-6 and TNF-α. Besides, difengpienol C blocked the activation of TLR4/MyD88/NF-κB signaling pathway. Therefore, difengpienol C might be a potent agent for anti-inflammatory drug development, and the non-traditional medicinal parts of Illicium difengpi can be identified as the source of natural anti-inflammatory molecules.

摘要

八角枫皮在中医临床上被广泛用于治疗类风湿关节炎和创伤,其茎皮是众所周知的。为了综合利用资源,对该植物的枝叶进行了植物化学研究,从中分离得到一个新的木脂素和三个已知的木脂素。根据广泛的光谱数据阐明了它们的结构,新化合物被阐明为具有独特共轭方式形成的二氢吡喃环的木脂素,命名为八角枫酚 C。八角枫酚 C 在脂多糖 (LPS) 刺激的 RAW264.7 细胞中表现出最强的抗炎活性,能强力抑制一氧化氮 (NO)、白细胞介素 6 (IL-6)、肿瘤坏死因子 α (TNF-α) 的产生,并抑制诱导型一氧化氮合酶 (iNOS)、IL-6 和 TNF-α 的 mRNA 转录。此外,八角枫酚 C 阻断了 TLR4/MyD88/NF-κB 信号通路的激活。因此,八角枫酚 C 可能是一种有潜力的抗炎药物开发的候选药物,八角枫的非传统药用部位可以被确定为天然抗炎分子的来源。

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