Biotechnological Engineering Center for Pharmaceutical Research and Development, Jiangxi Agricultural University, Nanchang 330045, China.
Laboratory of Natural Medicine and Microbiological Drug, College of Bioscience and Bioengineering, Jiangxi Agricultural University, Nanchang 330045, China.
Molecules. 2023 Apr 29;28(9):3813. doi: 10.3390/molecules28093813.
Four Chinese herbs from the genus, namely Aurantii Fructus Immaturus (), Aurantii Fructus (), Citri Reticulatae Pericarpium Viride () and Citri Reticulatae Pericarpium (), are widely used for treating various cardiovascular and gastrointestinal diseases. Many ingredients have already been identified from these herbs, and their various bioactivities provide some interpretations for the pharmacological functions of these herbs. However, the complex functions of these herbs imply undisclosed cholinergic activity. To discover some ingredients with cholinergic activity and further clarify possible reasons for the complex pharmacological functions presented by these herbs, depending on the extended structure-activity relationships of cholinergic and anti-cholinergic agents, a simple method was established here for quickly discovering possible choline analogs using a specific TLC method, and then stachydrine and choline were first identified from these herb decoctions based on their NMR and HRMS data. After this, two TLC scanning (TLCS) methods were first established for the quantitative analyses of stachydrine and choline, and the contents of the two ingredients and synephrine in 39 samples were determined using the valid TLCS and HPLC methods, respectively. The results showed that the contents of stachydrine (3.04‱) were 2.4 times greater than those of synephrine (1.25‱) in and about one-third to two-thirds of those of , and . Simultaneously, the contents of stachydrine, choline and synephrine in these herbs present similar decreasing trends with the delay of harvest time; e.g., those of stachydrine decrease from 5.16‱ () to 3.04‱ () and from 1.98‱ () to 1.68‱ (). Differently, the contents of synephrine decrease the fastest, while those of stachydrine decrease the slowest. Based on these results, compared with the pharmacological activities and pharmacokinetics reported for stachydrine and synephrine, it is indicated that stachydrine can be considered as a bioactive equilibrist for synephrine, especially in the cardio-cerebrovascular protection from these citrus herbs. Additionally, the results confirmed that stachydrine plays an important role in the pharmacological functions of these citrus herbs, especially in dual-directionally regulating the uterus, and in various beneficial effects on the cardio-cerebrovascular system, kidneys and liver.
四种来自芸香属的中草药，即化橘红（）、橘红（）、青皮（）和陈皮（），被广泛用于治疗各种心血管和胃肠道疾病。这些草药中已经鉴定出许多成分，它们的各种生物活性为这些草药的药理功能提供了一些解释。然而，这些草药的复杂功能暗示了未被揭示的胆碱能活性。为了发现一些具有胆碱能活性的成分，并进一步阐明这些草药呈现出复杂药理功能的可能原因，根据胆碱能和抗胆碱能药物的扩展结构-活性关系，在这里建立了一种简单的方法，使用特定的 TLC 方法快速发现可能的胆碱类似物，然后根据 NMR 和 HRMS 数据，首次从这些草药汤中鉴定出水苏碱和胆碱。在此之后，首次建立了两种 TLC 扫描（TLCS）方法，用于定量分析水苏碱和胆碱，并用有效的 TLCS 和 HPLC 方法分别测定 39 个样品中这两种成分和辛弗林的含量。结果表明，在 中，水苏碱（3.04‱）的含量比辛弗林（1.25‱）高 2.4 倍，约为 、 和 的三分之一至三分之二。同时，这些草药中水苏碱、胆碱和辛弗林的含量随着收获时间的延迟呈现出相似的降低趋势；例如，水苏碱的含量从 5.16‱（）降低到 3.04‱（），从 1.98‱（）降低到 1.68‱（）。不同的是，辛弗林的含量下降最快，而水苏碱的含量下降最慢。基于这些结果，与水苏碱和辛弗林的药理活性和药代动力学报道相比，表明水苏碱可以被认为是辛弗林的生物活性平衡剂，特别是在这些柑橘类草药对心脑血管的保护作用中。此外，结果证实水苏碱在这些柑橘类草药的药理功能中起着重要作用，特别是在双向调节子宫以及对心脑血管系统、肾脏和肝脏的各种有益作用中。
