School of Pharmaceutical Science, South-central University for Nationalities, Wuhan, 430074, China; School of Medicine, Yale University, New Haven, CT, 06511, USA.
School of Pharmaceutical Science, South-central University for Nationalities, Wuhan, 430074, China.
J Ethnopharmacol. 2021 Mar 25;268:113596. doi: 10.1016/j.jep.2020.113596. Epub 2020 Nov 19.
Scutellaria baicalensis (S. baicalensis) is the root of S. baicalensis Georgi. In traditional Chinese medicine it is divided into Tiaoqin (TQ, 1-3 years old) and Kuqin (KQ, more than 3 years old). However, the differences in TQ and KQ efficacy and their exact mechanisms are still unclear.
This study aimed to clarify the difference in the efficacy of TQ and KQ in relation to different fever types (damp heat and hyperpyrexia) by using rat models, as well as to determine the primary molecular mechanism.
This study compared the compositional content of TQ and KQ by UPLC-MS/MS. Then, rat models of hyperpyrexia (HP, LPS) and damp heat (DH, high-fat and high-sugar diet feeding + fumigation in artificial climate chamber + E. coli injection) were established and their clinical symptoms, blood biochemistry, histopathological sections, cell cytokines and protein expression were compared following treatment with TQ or KQ. Finally, the mechanisms underpinning the differences observed for TQ and KQ were determined by measuring the components of these treatments in different target organs.
This study identified 31 compounds in the water extracts of both TQ and KQ, which differed significantly in their relative content. TQ and KQ showed different functional tropism in HP and DH model rats. Baicalin, wogonoside, oroxin A, baicalein, wogonin and oroxylin A appeared to be the basic functional components responsible for the functional tropism hypothesis, while the remaining compounds appeared to be the efficacy-oriented components. In addition, the difference in pharmacodynamics between TQ and KQ may be related to their absorption in vivo, which was consistent with the hypothesis of functional tropism proposed in this work.
In this study we adopted TQ and KQ-different specifications of Scutellaria baicalensis with similar chemical components-as a case study to systematically reveal the functional tropism of Chinese herbal medicine (CHM). The results showed that TQ and KQ contain the basic functional components to enable the basic function of 'clearing heat', while the variation in compositional content may result in their different therapeutic effects. A greater understanding and utilisation of the functional tropism of CHM would enormously improve the accuracy and scientific basis for the application of CHM medication, as well as in promoting the multi-function mechanism of CHM and guiding new drug development of CHM.
黄芩（S. baicalensis）是黄芩的根。在中国传统医学中，它分为条芩（TQ，1-3 年生）和枯芩（KQ，3 年以上）。然而，TQ 和 KQ 的疗效差异及其确切机制尚不清楚。
本研究旨在通过大鼠模型阐明 TQ 和 KQ 在不同发热类型（湿热和高热）方面的疗效差异，并确定主要的分子机制。
本研究通过 UPLC-MS/MS 比较了 TQ 和 KQ 的组成含量。然后，建立了高热（LPS）和湿热（高脂肪和高糖饮食喂养+人工气候箱熏制+大肠杆菌注射）大鼠模型，并比较了 TQ 或 KQ 治疗后大鼠的临床症状、血液生化、组织病理学切片、细胞因子和蛋白表达。最后，通过测量这些治疗方法在不同靶器官中的成分，确定了 TQ 和 KQ 差异的潜在机制。
本研究在 TQ 和 KQ 的水提取物中鉴定出 31 种化合物，它们的相对含量有显著差异。TQ 和 KQ 在 HP 和 DH 模型大鼠中表现出不同的功能倾向。黄芩苷、汉黄芩苷、奥洛西林 A、黄芩素、汉黄芩素和木樨草素似乎是负责功能倾向假说的基本功能成分，而其余化合物似乎是疗效导向成分。此外，TQ 和 KQ 之间药效差异可能与其体内吸收有关，这与本工作中提出的功能倾向假说一致。
本研究采用 TQ 和 KQ-黄芩的不同规格，具有相似的化学成分-作为一个案例研究，系统地揭示了中药（CHM）的功能倾向。结果表明，TQ 和 KQ 含有基本功能成分，能够实现“清热”的基本功能，而成分含量的变化可能导致其治疗效果不同。更好地理解和利用 CHM 的功能倾向将极大地提高 CHM 药物应用的准确性和科学性基础，促进 CHM 的多功能机制和指导 CHM 的新药开发。
