Baicalin and baicalein in modulating tumor microenvironment for cancer treatment: A comprehensive review with future perspectives

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...

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Main Authors: Ruolei Wang, Chunyan Wang, Lianheng Lu, Fuwen Yuan, Feng He
Format: Article
Language:English
Published: Elsevier 2024-01-01
Series:Pharmacological Research
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S1043661823003882
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author Ruolei Wang
Chunyan Wang
Lianheng Lu
Fuwen Yuan
Feng He
author_facet Ruolei Wang
Chunyan Wang
Lianheng Lu
Fuwen Yuan
Feng He
author_sort Ruolei Wang
collection DOAJ
description 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.
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spelling doaj.art-2da6bfc18dd049e6b3a2f2e4775f90bd2023-12-08T04:45:06ZengElsevierPharmacological Research1096-11862024-01-01199107032Baicalin and baicalein in modulating tumor microenvironment for cancer treatment: A comprehensive review with future perspectivesRuolei Wang0Chunyan Wang1Lianheng Lu2Fuwen Yuan3Feng He4The Center for Cancer Research, School of Integrative Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, ChinaThe Center for Cancer Research, School of Integrative Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, ChinaThe Center for Cancer Research, School of Integrative Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, ChinaCorresponding authors.; The Center for Cancer Research, School of Integrative Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, ChinaCorresponding authors.; The Center for Cancer Research, School of Integrative Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, ChinaCancer 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.http://www.sciencedirect.com/science/article/pii/S1043661823003882BaicalinBaicaleinNatural productsAnticancerBioavailabilityTumor microenvironment
spellingShingle Ruolei Wang
Chunyan Wang
Lianheng Lu
Fuwen Yuan
Feng He
Baicalin and baicalein in modulating tumor microenvironment for cancer treatment: A comprehensive review with future perspectives
Pharmacological Research
Baicalin
Baicalein
Natural products
Anticancer
Bioavailability
Tumor microenvironment
title Baicalin and baicalein in modulating tumor microenvironment for cancer treatment: A comprehensive review with future perspectives
title_full Baicalin and baicalein in modulating tumor microenvironment for cancer treatment: A comprehensive review with future perspectives
title_fullStr Baicalin and baicalein in modulating tumor microenvironment for cancer treatment: A comprehensive review with future perspectives
title_full_unstemmed Baicalin and baicalein in modulating tumor microenvironment for cancer treatment: A comprehensive review with future perspectives
title_short Baicalin and baicalein in modulating tumor microenvironment for cancer treatment: A comprehensive review with future perspectives
title_sort baicalin and baicalein in modulating tumor microenvironment for cancer treatment a comprehensive review with future perspectives
topic Baicalin
Baicalein
Natural products
Anticancer
Bioavailability
Tumor microenvironment
url http://www.sciencedirect.com/science/article/pii/S1043661823003882
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