Jilin Ginseng Academy, Changchun University of Chinese Medicine, Changchun, China.
School of Pharmacy, Jiangxi University of Traditional Chinese Medicine, Nanchang, China.
J Food Biochem. 2021 Jul;45(7):e13752. doi: 10.1111/jfbc.13752. Epub 2021 Jun 4.
Fructus Gardeniae (FG) is medicine food widely used for the treatment and prevention of various diseases. However, in recent years, research has suggested that high doses of FG can cause hepatotoxicity and nephrotoxicity. To assess this potential toxicity in more depth, this study investigated the effects of decocted FG and two of its bioactive constituents (geniposide and genipin) on liver and kidney function in rats. Rats were intragastrically administered FG (330 mg/kg body weight), geniposide (50 mg/kg body weight), or genipin (50 mg/kg body weight) for 12 weeks. Changes in body weight, liver and kidney indices, biochemical indices, and inflammatory factors were monitored. In addition, pathological sections were assessed and the expression of caspase-3, NF-κBp65, COX-2, and iNOS was detected by immunohistochemistry and Western blot. It was found that the levels of aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, creatinine, and urea nitrogen increased following administration of FG, geniposide, and genipin. Furthermore, the activities of superoxide dismutase and reduced glutathione decreased following treatment, while malondialdehyde levels increased. Pathological and immunohistochemical evaluations further confirmed that FG and its constituents may cause damage to the liver and kidneys. The mechanism study revealed that the protein level of inflammatory pathway increased and further promoted apoptosis, suggesting that it should not be taken orally for extended periods of time. PRACTICAL APPLICATIONS: Chinese medicine and food safety have always been public health concerns. Fructus Gardeniae (FG) is a plant with a dual-purpose as it is used as both a medicine and food. Medicinally, it has the effects of heat-clearing and detoxification. However, its adverse effects and related mechanisms are not clear, and this has potential safety implications. In this study, rats were treated with FG for 12 weeks and found that the long-term administration of FG or high dosing can lead to damage to liver and kidney function. Therefore, close attention must be paid to the dosage of FG in order to achieve a therapeutic effect and avoid adverse reactions. Thus, this study lays a foundation for the safety evaluation and clinical application of FG.
栀子（FG）是一种广泛用于治疗和预防各种疾病的药食同源植物。然而，近年来的研究表明，高剂量的 FG 可能会导致肝毒性和肾毒性。为了更深入地评估这种潜在的毒性，本研究探讨了栀子及其两种生物活性成分（栀子苷和京尼平）对大鼠肝功能和肾功能的影响。大鼠灌胃给予 FG（330mg/kg 体重）、栀子苷（50mg/kg 体重）或京尼平（50mg/kg 体重），连续 12 周。监测体重、肝肾功能指标、生化指标和炎症因子的变化。此外，通过免疫组织化学和 Western blot 检测 caspase-3、NF-κBp65、COX-2 和 iNOS 的表达。结果发现，FG、栀子苷和京尼平给药后，天冬氨酸转氨酶、丙氨酸转氨酶、碱性磷酸酶、肌酐和尿素氮水平升高。此外，治疗后超氧化物歧化酶和还原型谷胱甘肽活性降低，而丙二醛水平升高。病理和免疫组织化学评价进一步证实，FG 及其成分可能导致肝、肾损伤。机制研究表明，炎症通路蛋白水平升高，进一步促进细胞凋亡，提示不宜长期口服。
中药和食品安全一直是公众健康关注的焦点。栀子（FG）是一种药食两用植物，具有清热解毒的功效。然而，其不良反应及其相关机制尚不清楚，这存在一定的安全隐患。在这项研究中，大鼠用 FG 治疗 12 周，发现 FG 长期给药或高剂量给药可导致肝肾功能损害。因此，必须密切关注 FG 的剂量，以达到治疗效果，避免不良反应。因此，本研究为 FG 的安全性评价和临床应用奠定了基础。
