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

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.

Emodin and Its Combination with Cytarabine Induce Apoptosis in Resistant Acute Myeloid Leukemia Cells in Vitro and in Vivo

“…Plant-derived natural products have garnered considerable attention in recent years due to the remarkable pharmacological properties in hematological malignancies [5,9,23]. Here, we presented the anti-leukemic effects of emodin and its combination with Ara-C on multidrug-resistant HL-60/ADR cells.…”

“…HL-60/ADR cells were maintained in RPMI-1640 medium with 0.2-0.8 µg/ml ADR and were grown in ADR-free culture medium at least two weeks for each experiment. 5 /ml cells in RPMI 1640 medium with 10% fetal bovine serum were plated in 6-well plates. After 24 h of incubation with emodin, Ara-C, or emodin plus Ara-C, cells were harvested and washed with PBS, and then stained with Annexin V-PE/7-AAD (Becton Dickinson, NJ, USA) according to the manufacturer's instruction.…”

“…A lot of traditional Chinese medicine and their active extracts have shown anti-leukemia activities. Many of them have been widely used for the treatment of leukemia patients, such as Taxol, Vincristine, Homoharringtonine and Arsenic Trioxide [5][6][7][8].…”

Evolution in medicinal chemistry of ursolic acid derivatives as anticancer agents

“…One of the potential approaches to access better UA derivatives with improved aqueous solubility may take advantage of our published strategies by generating O -alkylamino-tethered derivatives, capable of having more favorable physicochemical properties [55-57]. Beneficial effects of making glucosides widely used in pharmaceutical industry may be another viable approach for the enhancement of solubility [58,59]. (4) Drug delivery systems are well known to improve aqueous solubility and bioavailability of many clinically used anticancer drugs [60,61].…”

Anticancer properties of baicalein: a review

“…Previous researches have shown that baicalein exerts numerous biological activities, such as anti-cancer, anti-inflammation, anti-cardiovascular diseases, anti-bacterial or viral infection, and anti-neurodegenerative diseases. Studies have demonstrated that baicalein suppresses cancer cell proliferation, induces apoptosis and cell cycle arrest in human breast, prostate, hepatocellular, myeloma and T24 bladder cancer cells (Chen et al 2014b; Li et al 2013a). Baicalein inhibits migration and invasion of human breast cancer cells, hepatoma cells and skin cancer cells (Chiu et al 2011; Wang et al 2010b; Wu et al 2011).…”