Tumor multidrug resistance is one of the key factors affecting the therapeutic effect of non-small cell lung cancer (NSCLC). Its mechanism involves enhanced drug efflux, abnormal activation of signaling pathways, metabolic re-programming, regulation by non-coding RNA (ncRNA), and immune regulation, among other molecular mechanisms. The active components extracted from traditional Chinese medicine have the characteristics of "multi-component, multi-target and low toxicity", showing broad prospects in reversing anti-tumor drug resistance. This review focuses on the important biological processes of drug resistance in NSCLC, and introduces the intervention of effective components in traditional Chinese medicine including curcumin, baicalin, triptolide, and dauricine on the above resistance factors and their possible mechanisms of action, from aspects such as abnormal activation of drug efflux pumps and key signaling pathways, imbalance of apoptosis and ferroptosis, and ncRNA. Literature review has shown that active ingredients of traditional Chinese medicine can reverse tumor drug resistance through multiple mechanisms and, to a certain extent, enhance therapeutic efficacy when combined with chemotherapeutic drugs, suggesting that the development of traditional Chinese medicine preparations is expected to become an effective approach for reversing the drug resistance of NSCLC.
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