柠檬苦素：药理学、毒性和药代动力学综述,Molecules

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柠檬苦素：药理学、毒性和药代动力学综述
Molecules ( IF 4.2 ) Pub Date : 2019-10-12 , DOI: 10.3390/molecules24203679
Shunming Fan ₁ , Chunling Zhang ₁ , Ting Luo ₁ , Jiaqi Wang ₁ , Yu Tang ₁ , Zhimin Chen ₁ , Lingying Yu ₁

Affiliation

柠檬苦素是一种天然的四环三萜类化合物，广泛存在于Euodia rutaecarpa (Juss.) Benth.、Phellodendron chinense Schneid.和Coptis chinensis Franch。近年来，其广泛的药理作用引起了人们的广泛关注。然而，没有系统评价侧重于柠檬苦素的药理学、毒性和药代动力学。因此，本综述旨在提供柠檬苦素的药理学、毒性和药代动力学的最新信息，探索该化合物的治疗潜力，并寻找提高疗效和生物利用度的方法。柠檬苦素具有广泛的药理作用，包括抗癌、抗炎和镇痛、抗菌和抗病毒、抗氧化、保肝等特性。然而，柠檬苦素还被证明会导致肝毒性、肾毒性和遗传损伤。此外，柠檬苦素对肝脏代谢酶也有复杂的影响。药代动力学研究表明柠檬苦素的生物利用度较差，其主要代谢途径是还原、水解和甲基化。我们还发现柠檬苦素取代基的位置和基团是影响药理活性和生物利用度的关键。然而，柠檬苦素的抗氧化作用机制尚不明确等问题仍然存在。此外，关于柠檬苦素的毒性机制的研究较少，柠檬苦素浓度对药理作用和毒性的影响尚不清楚，也没有研究人员报道任何降低柠檬苦素毒性的方法。所以，

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Limonin: A Review of Its Pharmacology, Toxicity, and Pharmacokinetics

Limonin is a natural tetracyclic triterpenoid compound, which widely exists in Euodia rutaecarpa (Juss.) Benth., Phellodendron chinense Schneid., and Coptis chinensis Franch. Its extensive pharmacological effects have attracted considerable attention in recent years. However, there is no systematic review focusing on the pharmacology, toxicity, and pharmacokinetics of limonin. Therefore, this review aimed to provide the latest information on the pharmacology, toxicity, and pharmacokinetics of limonin, exploring the therapeutic potential of this compound and looking for ways to improve efficacy and bioavailability. Limonin has a wide spectrum of pharmacological effects, including anti-cancer, anti-inflammatory and analgesic, anti-bacterial and anti-virus, anti-oxidation, liver protection properties. However, limonin has also been shown to lead to hepatotoxicity, renal toxicity, and genetic damage. Moreover, limonin also has complex impacts on hepatic metabolic enzyme. Pharmacokinetic studies have demonstrated that limonin has poor bioavailability, and the reduction, hydrolysis, and methylation are the main metabolic pathways of limonin. We also found that the position and group of the substituents of limonin are key in affecting pharmacological activity and bioavailability. However, some issues still exist, such as the mechanism of antioxidant activity of limonin not being clear. In addition, there are few studies on the toxicity mechanism of limonin, and the effects of limonin concentration on pharmacological effects and toxicity are not clear, and no researchers have reported any ways in which to reduce the toxicity of limonin. Therefore, future research directions include the mechanism of antioxidant activity of limonin, how the concentration of limonin affects pharmacological effects and toxicity, finding ways to reduce the toxicity of limonin, and structural modification of limonin—one of the key methods necessary to enhance pharmacological activity and bioavailability.

更新日期：2019-10-12

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