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Cancer Lett. 2014 Nov 1;354(1):5-11. doi: 10.1016/j.canlet.2014.08.003. Epub 2014 Aug 13.

Exploring therapeutic potentials of baicalin and its aglycone baicalein for hematological malignancies.

Author information

1
College of Chemistry, Fuzhou University, Fuzhou, Fujian 350108, China; Chemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, Texas 77555, USA.
2
College of Chemistry, Fuzhou University, Fuzhou, Fujian 350108, China.
3
Fujian Institute of Hematology, Fujian Provincial Key Laboratory of Hematology, Fujian Medical University Union Hospital, Fuzhou, Fujian 350001, China.
4
Fujian Institute of Hematology, Fujian Provincial Key Laboratory of Hematology, Fujian Medical University Union Hospital, Fuzhou, Fujian 350001, China. Electronic address: jdhu@medmail.com.cn.
5
Chemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, Texas 77555, USA. Electronic address: jizhou@utmb.edu.

Abstract

Despite tremendous advances in the targeted therapy for various types of hematological malignancies with successful improvements in the survival rates, emerging resistance issues are startlingly high and novel therapeutic strategies are urgently needed. In addition, chemoprevention is currently becoming an elusive goal. Plant-derived natural products have garnered considerable attention in recent years due to the potential dual functions as chemotherapeutics and dietary chemoprevention. One of the particularly ubiquitous families is the polyphenolic flavonoids. Among them, baicalin and its aglycone baicalein have been widely investigated in hematological malignancies because both of them exhibit remarkable pharmacological properties. This review focuses on the recent achievements in drug discovery research associated with baicalin and baicalein for hematological malignancy therapies. The promising anticancer activities of these two flavonoids targeting diverse signaling pathways and their potential biological mechanisms in different types of hematological malignancies, as well as the combination strategy with baicalin or baicalein as chemotherapeutic adjuvants for recent therapies in these intractable diseases are discussed. Meanwhile, the biotransformation of baicalin and baicalein and the relevant approaches to improve their bioavailability are also summarized.

KEYWORDS:

Baicalein; Baicalin; Cancer targets; Flavonoids; Hematological malignancies

PMID:
25128647
PMCID:
PMC4179973
DOI:
10.1016/j.canlet.2014.08.003
[Indexed for MEDLINE]
Free PMC Article

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