Anticancer Advances of Matrine and Its Derivatives

Abstract

As the second leading cause of death in the world, the total number caused by cancer in 2008 is 1.4 million. The great cancer incidence worldwide increases the search for new, safer and efficient anticancer agents (especially to find the new structures and more active anticancer drugs from the natural products) aiming the prevention or the cure of such illness. For a century, matrine (an alkaloid isolated from sophorae flavescens Ait.) has been widely studied in the field of cancer. This review briefly describes the progress of matrine, its derivatives and their anticancer activity.

Linear Quantitative Profiling Method Fast Monitors Alkaloids of Sophora Flavescens That Was Verified by Tri-Marker Analyses

“…Modern research has also shown various pharmacological effects of Alkaloids of Sophora flavescens (ASF), such as antimicrobial, antiinflammatory, anti-allergic, anti-tumor, anti-arrhythmia, anti-hepatitis, and regulation of the immune system [2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17]. Among many chemical components from the ASF, quinolizidine alkaloids such as matrine (MT), sophoridine (SPR) and oxymatrine (OMT) have been demonstrated to be important active compounds [18][19][20][21][22][23][24][25][26][27][28][29]. The quality of ASF as herbal medicine is typically evaluated and controlled by the total alkaloid content.…”

Therapeutic effects of matrine derivate MASM in mice with collagen-induced arthritis and on fibroblast-like synoviocytes

“…Therapies aimed at inducing apoptosis of RA-FLS could be valuable for RA treatment 5, 43 . The anti-cancer and apoptosis-inducing properties of matrine are well documented 10, 12, 44, 45 . A previous study investigated the effects of MASM on rat hepatocytes and hepatic stellate cells (HSCs).…”

“…Matrine is an active alkaloid compound that is isolated from the traditional Chinese herb Sophora flavescens and has a wide spectrum of biological properties, such as anti-inflammatory 6–8 , antiviral 9 , anti-cancer 10–12 , anti-fibrotic 13 and anti-dementia 14 properties. However, until now matrine has not been developed into a drug because of its low therapeutic efficacy.…”

Synthesis, biological evaluation and mechanism studies of matrine derivatives as anticancer agents

“…However, the low water solubility, bioavailability and bioactivity of matrine, coupled with its considerable side effects, which include general toxicity to the central nervous system, have limited its utility as a therapeutic drug (17,18). Therefore, studies have been focusing on developing derivatives and analogues of matrine by total synthesis or structural modifications in order to improve its activity and bioavailability (19)(20)(21).…”

“…However, the low water solubility, bioavailability and bioactivity of matrine, coupled with its considerable side effects, which include general toxicity to the central nervous system, have limited its utility as a therapeutic drug (17,18). Therefore, studies have been focusing on developing derivatives and analogues of matrine by total synthesis or structural modifications in order to improve its activity and bioavailability (19)(20)(21).A previous study demonstrated that the amide bond may be required for the antitumor activities of matrine as following opening of the D-ring and breaking of the amide bond, the anti-proliferative activities of matrine are lost (22). Based on the potential positions for modifying matrine, the present study designed, synthesized and characterized five matrine derivatives for their anti-proliferation potential.…”