Baicalin suppresses lung cancer growth by targeting PDZ-binding kinase/T-LAK cell-originated protein kinase (2025)

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“…It is necessary to find TOPK inhibitors with low toxicity to overcome the side-effect of current TOPK inhibitors (Matsuo et al, 2014; Ishikawa et al, 2018). There were several small molecule compounds from Chinese herbal medicine reported to be an inhibitor of TOPK to reduce the proliferation of tumor cells (Diao et al, 2019; Wang et al, 2019). However, the study of inhibiting TOPK in esophageal cancer has not been reported, although TOPK was highly expressed in esophageal cancer.…”

confidence: 99%

et al. 2019

Eupafolin is the main bioactive component extracted from the traditional Chinese medicine Ay Tsao (Artemisia vulgaris L.), and its anti-tumor activity has had been studied in previous researches. T-LAK cell-originated protein kinase (TOPK) belongs to serine/threonine protein kinase and is highly expressed in several cancer cells and tissues, such as colon cancer, lung cancer, esophagus cancer, and so on. Therefore, it was recognized as an important target for treating tumors. Nowadays, we found that eupafolin suppressed TOPK activities at the first time in vitro and in vivo. The cells study indicated that eupafolin suppressed TOPK activities in JB6 Cl41 and KYSE450 cells. Furthermore, knockdown of TOPK in KYSE450 cells decreased their sensitivities to eupafolin. The animal study showed that the injection of eupafolin in patient-derived xenograft (PDX) mouse effectively suppressed tumor growth. Histone H3 and Ki67 were reduced, and cleaved caspase 3 was increased in tumor tissues after eupafolin treatment. To sum up, eupafolin as an TOPK inhibitor can suppress growth of esophagus cancer in vitro and in vivo. The TOPK downstream signaling molecule histone H3 in tumor tissues was also reduced after eupafolin treatment. In short, eupafolin can suppress growth of esophagus cancer cells as an TOPK inhibitor both in vitro and in vivo.

Baicalin, as a natural active ingredient extracted and isolated from the traditional Chinese medicine Scutellaria baicalensis Georgi., has been potentially used in various areas for its antioxidative, antitumor, anti-inflammatory, and anti-proliferative activities. Although several studies have reported the antitumor effects of baicalin against various cancer types, its beneficial effects on lung cancer have not yet been elucidated. Therefore, the therapeutic effects and molecular mechanisms of baicalin on lung cancer cell lines H1299 and H1650 were investigated. Here, the results of its antitumor activity were shown. We found that Akt/mTOR pathway inhibition was the essential determinant in baicalin-induced cell cycle arrest. Furthermore, when the Akt Agonist SC79 or Akt plasmid transfection was performed, the antitumor effect of baicalin was significantly abrogated in both H1299 and H1650 cells. In conclusion, we found that baicalin exerted its antitumor activity mainly by inducing Akt-dependent cell cycle arrest and promoting apoptosis, which show great potential for developing a new drug for lung cancer treatment.

Flavonoids as the largest group of natural phytochemical compounds have received significant attention, as demonstrated by clinical trials, due to their chemotherapeutic and/or pharmacological effects against non-small-cell lung cancer (NSCLC) and asthma. Scutellaria baicalensis (S. baicalensis), known as one of the most popular medicinal plants and used in several countries, contains natural active flavone constituents, with the major compounds of the roots being baicalein, baicalin, wogonin, wogonoside and oroxylin A. S. baicalensis and their compounds are proven to have inhibitory effects on NSCLC cells when used at different concentrations. However, the exact mechanisms by which these compounds exert their therapeutic effects against asthma remain unexplored. Indeed, the mechanisms by which S.baicalensis and its flavone compounds exert a protective effect against nicotine-induced NSCLC and asthma are not yet fully understood. Therefore, this review explores the mechanisms involved in the therapeutic potential of flavone-rich extracts from S. baicalensis in nicotine-induced NSCLC and asthma.