Zhang He, Tang Jun, Cao Huiliang, Wang Chenguang, Shen Chong, Liu Jun
State Key Laboratory of Dynamic Measurement Technology, School of Instrument and Electronics, North University of China, Taiyuan, 030051, China.
State Key Laboratory of Dynamic Measurement Technology, School of Instrument and Electronics, North University of China, Taiyuan, 030051, China.
J Ethnopharmacol. 2025 Feb 10;338(Pt 1):119007. doi: 10.1016/j.jep.2024.119007. Epub 2024 Oct 28.
Colorectal cancer (CRC) is a prevalent malignant tumor of the digestive tract. Traditional Chinese medicine (TCM) has a long history of treating CRC, with advantages such as effectiveness, multi-target, multi-pathway, and minimal side effects. TCM Magnolia officinalis (M. officinalis) refers to the dried bark, root bark, and branch bark of either Magnolia officinalis Rehd.et Wils. or Magnolia officinalis Rehd.et Wils. var. biloba Rehd.et Wils. It is commonly utilized to alleviate the side effects of chemotherapy for CRC, owing to its anti-inflammatory and anti-tumor properties. However, current research primarily focuses on the individual components and does not take into consideration the characteristics of multi-component-multi-target action.
Our aim is to study the new action characteristics of M. officinalis in the treatment of CRC.
Utilizing network pharmacology to identify potential active ingredients, key targets, and main signaling pathways of M. officinalis for the treatment of CRC. The binding effect was further validated through molecular docking analysis. Furthermore, the aforementioned components were identified using liquid chromatography-mass spectrometry (LC-MS), and the cleavage pathways of the main components were analyzed. Subsequently, both in vitro and in vivo experiments were carried out to investigate the anti-CRC effect of the active ingredients of M. officinalis and its potential mechanism.
Network pharmacology and Molecular docking identified 5 main active ingredients and 6 core targets of M. officinalis for the treatment of CRC. Then, LC-MS identified the active components of M. officinalis. At the same time, both in vitro and in vivo experiments have confirmed the ability of Eucalyptol (Euc) and Obovatol (Obo)to inhibit inflammation and tumor cell proliferation. The possible mechanism involved is that Euc and Obo counteract CRC by inhibiting the over-activation of NF-κBp65/JAK and Bcl-2/Caspase signaling pathways, respectively. They also play a role in the anti-CRC effect of M. officinalis.
Magnolol (MAG), Honokiol (HK), Euc, Obo, and Neohesperidin (NHP) in M. officinalis may be the pharmacological substance basis for its anti-cancer effect on CRC. The treatment of CRC with M. officinalis is characterized by its multi-component, multi-target, and multi-pathway approach. These findings provide a theoretical basis for further inspiring the clinical application of M. officinalis and the development of efficacy targets.
结直肠癌（CRC）是一种常见的消化道恶性肿瘤。中医在治疗CRC方面有着悠久的历史，具有疗效显著、多靶点、多途径以及副作用小等优势。中药厚朴指的是厚朴（Magnolia officinalis Rehd.et Wils.）或凹叶厚朴（Magnolia officinalis Rehd.et Wils. var. biloba Rehd.et Wils.）的干燥树皮、根皮和枝皮。因其具有抗炎和抗肿瘤特性，常用于减轻CRC化疗的副作用。然而，目前的研究主要集中在单个成分上，未考虑多成分多靶点作用的特点。
我们的目的是研究厚朴在治疗CRC中的新作用特性。
利用网络药理学确定厚朴治疗CRC的潜在活性成分、关键靶点和主要信号通路。通过分子对接分析进一步验证结合效果。此外，使用液相色谱 - 质谱联用（LC - MS）鉴定上述成分，并分析主要成分的裂解途径。随后，进行体外和体内实验，研究厚朴活性成分的抗CRC作用及其潜在机制。
网络药理学和分子对接确定了厚朴治疗CRC的5种主要活性成分和6个核心靶点。然后，LC - MS鉴定了厚朴的活性成分。同时，体外和体内实验均证实桉叶油素（Euc）和和厚朴酚（Obo）具有抑制炎症和肿瘤细胞增殖的能力。可能的机制是Euc和Obo分别通过抑制NF - κBp65/JAK和Bcl - 2/Caspase信号通路的过度激活来对抗CRC。它们在厚朴的抗CRC作用中也发挥作用。
厚朴中的厚朴酚（MAG）、和厚朴酚（HK）、桉叶油素（Euc）、和厚朴酚（Obo）以及新橙皮苷（NHP）可能是其对CRC抗癌作用的药理物质基础。厚朴治疗CRC具有多成分、多靶点和多途径的特点。这些发现为进一步启发厚朴的临床应用和疗效靶点的开发提供了理论依据。
