The Fifth College of Clinic Medicine, Guangzhou University of Chinese Medicine, 60 Hengfu rd, Guangzhou 510095, China; Guangdong Provincial Key Laboratory of Research and Development in Traditional Chinese Medicine, 60 Hengfu rd, Guangzhou 510095, China.
The Fifth College of Clinic Medicine, Guangzhou University of Chinese Medicine, 60 Hengfu rd, Guangzhou 510095, China; Guangdong Provincial Key Laboratory of Research and Development in Traditional Chinese Medicine, 60 Hengfu rd, Guangzhou 510095, China.
Biomed Pharmacother. 2024 Jan;170:116089. doi: 10.1016/j.biopha.2023.116089. Epub 2023 Dec 28.
Hyperlipidaemia is described as "excessive phlegm" and "blood stasis" in the classic theory of traditional Chinese medicine. Exocarpium Citri Grandis has the effect of dispelling blood stasis and removing phlegm, which can better meet the treatment needs of this disease. However, there is still a lack of focus and depth in the study of the chemical composition of this medicine, and the correlation between the study of relevant medicinal substances and the efficacy of dispelling stasis and removing phlegm is insufficient. To address this issue, this study was carried out to validate the overall efficacy and identify and determine the chemical composition of Exocarpium Citri Grandis. The regulatory mechanism of the PXR-CYP3A4/FXR-LXRα pathway and its active ingredients were screened, and a pharmacokinetic study of active ingredients was performed. The obtained multidimensional data were statistically analysed and comprehensively evaluated. The quality marker of Exocarpium Citri Grandis in the treatment of hyperlipidaemia based on the PXR-CYP3A4/FXR-LXRα mechanism to exert the efficacy of dispelling blood stasis and removing phlegm was finally determined. Based on the above experiments, we identified 27 compounds from the ethanol extract of Exocarpium Citri Grandis. Among them, naringenin, meranzin hydrate, apigenin, caffeic acid phenethyl ester, anacardiin, hesperidin and naringin can significantly regulate all or part of the targets in the PXR-CYP3A4/FXR-LXRα pathway. It also has suitable content and pharmacokinetic characteristics in vivo. In conclusion, this study established quality markers to characterize the efficacy of Exocarpium Citri Grandis in dispelling blood stasis and removing phlegm, which provides a scientific basis for the targeted evaluation of the hypolipidaemic activity of this medicinal plant.
高脂血症在中医经典理论中被描述为“痰浊”和“血瘀”。陈皮具有化瘀祛痰的作用，能更好地满足该病的治疗需要。然而，该药的化学成分研究仍缺乏重点和深度，相关药用物质的研究与化瘀祛痰功效的相关性不足。针对这一问题，本研究旨在验证陈皮的整体疗效，并鉴定和确定其化学成分。筛选了 PXR-CYP3A4/FXR-LXRα 通路的调节机制及其活性成分，并进行了活性成分的药代动力学研究。对获得的多维数据进行了统计分析和综合评价。最终确定了基于 PXR-CYP3A4/FXR-LXRα 机制发挥化瘀祛痰功效的陈皮治疗高脂血症的质量标志物。基于上述实验，我们从陈皮的乙醇提取物中鉴定出 27 种化合物。其中，柚皮苷、橙皮素水合物、芹菜素、咖啡酸苯乙酯、阿魏酸、橙皮苷和柚皮苷能显著调节 PXR-CYP3A4/FXR-LXRα 通路中的全部或部分靶点，且体内含量适宜，具有药代动力学特征。综上所述，本研究建立了质量标志物来表征陈皮化瘀祛痰的功效，为该药用植物降脂活性的靶向评价提供了科学依据。
