Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing, 100850, China; College of Pharmacy, Gansu University of Chinese Medicine, Lanzhou, 730000, China; National Key Laboratory of Kidney Diseases, Beijing, 100850, China.
Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing, 100850, China; College of Pharmacy, Gansu University of Chinese Medicine, Lanzhou, 730000, China.
J Ethnopharmacol. 2024 May 23;326:117934. doi: 10.1016/j.jep.2024.117934. Epub 2024 Feb 20.
The desiccative ripe fruits of Gardenia (Gardenia jasminoides Ellis) (called Zhizi in China) are known with cold character and the effects of reducing fire except vexed, clearing away heat evil, and cooling blood and eliminating stasis. Zhizi is often clinical formulated to treat various types of fever. Fever is a sign of inflammation and, geniposide from Zhizi has been proved with anti-inflammatory in various inflammatory models.
The aim of this study was to investigate the antipyretic role of geniposide with three classical inflammatory fever models and explore the underlying mechanisms.
Water extract (WE), high polar part (HP), iridoid glycoside part (IG), and gardenia yellow pigment part (GYP) from Gardeniae Fructus (GF) were obtained from Zhizi. The antipyretic activities of these composes were tested with dry yeast induced fever rats. Geniposide was further purified from IG and the antipyretic activity was evaluated by gavage, intraperitoneal injection, and caudal intravenous injection to rats of fever induced by dry yeast, lipopolysaccharide (LPS), and 2, 4-dinitrophenol (DNP) in rats. Then, the mechanism of geniposide by intragastric administration was studied. The contents of thermoregulatory mediators and inflammatory factors relating to TLR4/NF-κB pathway in serum were determined by ELISA and Western blot, and the pathological changes of the hypothalamus were observed by HE staining.
The temperature was decreased by geniposide in the three fever model rats. Geniposide can not only inhibit the increase of inflammatory factors in serum but also protect the hypothalamus from fever pathological damage in the three fever models. Western blot showed that geniposide could inhibit the TLR4/NF-κB pathway.
Geniposide exerts antipyretic effect in febrile rats through modulating the TLR4/NF-κB signaling pathway.
栀子（Gardenia jasminoides Ellis）的干燥成熟果实（在中国称为栀子）具有寒性，除烦泻火、清热利湿、凉血化瘀的功效。栀子常被临床用于治疗各种发热。发热是炎症的标志，栀子中的京尼平苷已被证明在各种炎症模型中具有抗炎作用。
本研究旨在通过三种经典的炎症发热模型研究京尼平苷的解热作用，并探讨其潜在机制。
从栀子中提取栀子水提取物（WE）、高极性部分（HP）、环烯醚萜苷部分（IG）和栀子黄色素部分（GYP）。用干酵母诱导发热大鼠检测这些成分的解热活性。进一步从 IG 中纯化京尼平苷，通过灌胃、腹腔注射和尾静脉注射评估其对干酵母、脂多糖（LPS）和 2,4-二硝基苯酚（DNP）诱导发热大鼠的解热活性。然后，通过灌胃研究京尼平苷的作用机制。通过 ELISA 和 Western blot 测定血清中与 TLR4/NF-κB 通路相关的体温调节介质和炎症因子的含量，并通过 HE 染色观察下丘脑的病理变化。
京尼平苷可降低三种发热模型大鼠的体温。京尼平苷不仅能抑制血清中炎症因子的增加，还能保护下丘脑免受三种发热模型的发热病理损伤。Western blot 显示，京尼平苷能抑制 TLR4/NF-κB 通路。
京尼平苷通过调节 TLR4/NF-κB 信号通路对发热大鼠发挥解热作用。
Zotero 插件