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        Latest research progress on anticancer effect of baicalin and its aglycone baicalein

        Lin Wang,Ting Feng,Zhilian Su,Chao Pi,Yumeng Wei,Ling Zhao 대한약학회 2022 Archives of Pharmacal Research Vol.45 No.8

        Cancer, which is a leading cause of deathsaround the world, is characterized by genetic mutationsand epigenetic changes. Baicalin and its aglycone baicalein,the major bioactive fl avones derived from the driedroot of Scutellaria baicalensis Georigi, belong to fl avonoidcompounds. Many studies demonstrated that both of themexhibited remarkable promising anticancer activities. Thisstudy summarized potential anticancer mechanisms of baicalinand baicalein including induction of apoptosis, initiationof cell cycle arrest, suppression of metastasis, induction ofautophagy, and regulation of immunity. Combination strategiesinvolving baicalin or baicalein as chemotherapeuticadjuvants, clinical trial and safety were also discussed. In addition, we compared the diff erence in their anticancereff ects. Interestingly, baicalein showed quicker and strongerinhibitory eff ects on multiple cancers than those of baicalin,probably due to its smaller size and high lipophilicity whichcontribute to fast absorption and improve ability to penetratecells. Taken together, both baicalin and baicalein are eff ectivein treating cancer with good tolerance. However, deglycosylationof baicalin to baicalein was found to have strongeranticancer potential.

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