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Berberine (BBR), a bioactive compound from various plants, shows significant therapeutic promise against lung cancer. Research indicates that berberine effectively inhibits cell proliferation in lung cancer cell lines and promotes apoptosis. Its mechanisms of action include inducing apoptosis and inhibiting metastasis-related pathways, showcasing its multifaceted approach to tumor suppression. Berberine also influences important signaling pathways like mitogen-activated protein kinase, phosphoinositide 3-kinase/protein kinase B, and nuclear factor kappa-light-chain-enhancer of activated B cells, thereby boosting its anti-cancer properties. Preclinical animal studies have further demonstrated berberine's effectiveness, especially when combined with conventional chemotherapy, suggesting a synergistic relationship that could enhance treatment efficacy. These promising results have led to ongoing clinical trials exploring berberine's potential as part of lung cancer treatment regimens. However, challenges persist regarding dosage standardization, bioavailability, and the translation of preclinical results into clinical applications. This review highlights the therapeutic mechanisms of berberine, its potential efficacy as a standalone or adjunctive treatment, and the obstacles that must be addressed to leverage its benefits in lung cancer therapy fully. Overcoming these challenges may provide valuable opportunities for improving treatment outcomes, positioning berberine as a key component in future lung cancer therapies. Continued research is essential to better understand its precise mechanisms and enhance its clinical application.