Technol Health Care. 2024;32(4):2091-2105. doi: 10.3233/THC-230738.
Rituximab resistance is one of the great challenges in the treatment of diffuse large B-cell lymphoma (DLBCL), but relevant biomarkers and signalling pathways remain to be identified. Coptis chinensis and its active ingredients have antitumour effects; thus, the potential bioactive compounds and mechanisms through which Coptis chinensis acts against rituximab-resistant DLBCL are worth exploring.
To elucidate the core genes involved in rituximab-resistant DLBCL and the potential therapeutic targets of candidate monomers of Coptis chinensis.
Using the Traditional Chinese Medicine System Pharmacology Database and Analysis Platform (TCMSP), the Similarity Ensemble Approach and Swiss Target Prediction, the main ingredients and pharmacological targets of Coptis chinensis were identified through database searches. Through the overlap between the pharmacological targets of Coptis chinensis and the core targets of rituximab-resistant DLBCL, we identified the targets of Coptis chinensis against rituximab-resistant DLBCL and constructed an active compound-target interaction network. The targets and their corresponding active ingredients of Coptis chinensis against rituximab-resistant DLBCL were molecularly docked.
Berberine, quercetin, epiberberine and palmatine, the active components of Coptis chinensis, have great potential for improving rituximab-resistant DLBCL via PIK3CG.
This study revealed biomarkers and Coptis chinensis-associated molecular functions for rituximab-resistant DLBCL.
利妥昔单抗耐药是弥漫性大 B 细胞淋巴瘤（DLBCL）治疗的重大挑战之一，但相关的生物标志物和信号通路仍有待确定。黄连及其活性成分具有抗肿瘤作用；因此，黄连作用于利妥昔单抗耐药性 DLBCL 的潜在生物活性化合物和机制值得探索。
阐明利妥昔单抗耐药性 DLBCL 中的核心基因，以及黄连候选单体的潜在治疗靶点。
通过中药系统药理学数据库和分析平台（TCMSP）、相似性综合方法和瑞士目标预测，通过数据库搜索确定黄连的主要成分和药理学靶点。通过黄连的药理学靶点与利妥昔单抗耐药性 DLBCL 的核心靶点之间的重叠，鉴定黄连针对利妥昔单抗耐药性 DLBCL 的靶点，并构建活性化合物-靶点相互作用网络。黄连针对利妥昔单抗耐药性 DLBCL 的靶点及其相应的活性成分进行了分子对接。
黄连的活性成分小檗碱、槲皮素、表小檗碱和巴马汀通过 PIK3CG 对改善利妥昔单抗耐药性 DLBCL 具有很大的潜力。
本研究揭示了利妥昔单抗耐药性 DLBCL 的生物标志物和黄连相关分子功能。
