1. Baicalin and baicalein in modulating tumor microenvironment for cancer treatment: A comprehensive review with future perspectives.
- Author
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Wang, Ruolei, Wang, Chunyan, Lu, Lianheng, Yuan, Fuwen, and He, Feng
- Subjects
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TUMOR microenvironment , *DRUG discovery , *CANCER treatment , *EXTRACELLULAR matrix , *CHINESE skullcap ,CAUSE of death statistics - Abstract
Cancer is a leading cause of death worldwide. The burden of cancer incidence and mortality is increasing rapidly. New approaches to cancer prevention and treatment are urgently needed. Natural products are reliable and powerful sources for anticancer drug discovery. Baicalin and baicalein, two major flavones isolated from Scutellaria baicalensis Georgi, a multi-purpose traditional medicinal plant in China, exhibit anticancer activities against multiple cancers. Of note, these phytochemicals exhibit extremely low toxicity to normal cells. Besides their cytotoxic and cytostatic activities toward diverse tumor cells, recent studies demonstrated that baicalin and baicalein modulate a variety of tumor stromal cells and extracellular matrix (ECM) in the tumor microenvironment (TME), which is essential for tumorigenesis, cancer progression and metastasis. In this review, we summarize the therapeutic potential and the mechanism of action of baicalin and baicalein in the regulation of tumor microenvironmental immune cells, endothelial cells, fibroblasts, and ECM that reshape the TME and cancer signaling, leading to inhibition of tumor angiogenesis, progression, and metastasis. In addition, we discuss the biotransformation pathways of baicalin and baicalein, related therapeutic challenges and the future research directions to improve their bioavailability and clinical anticancer applications. Recent advances of baicalin and baicalein warrant their continued study as important natural ways for cancer interception and therapy. [Display omitted] • Natural products are reliable and powerful sources for cancer drug discovery. • Baicalin and baicalein are two major flavones isolated from Scutellaria baicalensis Georgi. • Baicalin and baicalein exhibit anticancer activities against multiple cancers with extremely low toxicity to normal cells. • Baicalin and baicalein modulate tumor stromal cells and extracellular matrix in the tumor microenvironment. • Future research needs to reveal TID and improve the bioavailability for clinical applications of baicalin and baicalein. [ABSTRACT FROM AUTHOR]
- Published
- 2024
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