Matrine is an alkaloid found in Sophora japonica plants that acts as a kappa opioid receptor and µ-receptor agonist[1]. Matrine has multiple pharmacological effects, including anticancer, anti-oxidative stress, anti-inflammatory and anti-apoptotic effects[2].
In vitro, treatment of A549, DU145 and MIA PaCa-2 cells with Matrine (50 μM) for 24 h inhibited the expression of CXC chemokine receptor type 4 (CXCR4), downregulated the levels of matrix metalloproteinases (MMP-2 and MMP-9), and weakened cell migration activity[3]. Matrine (50-500 μg/ml) treated gastric cancer cell line MNK45 inhibited cell proliferation in a dose-dependent manner with an IC50 value of 540 μg/ml, and significantly affected the expression of intracellular NF-κB, XIAP, CIAP and p-ERK proteins[4]. Matrine (0.5-2.0 mg/mL) treated D341 cells for 24-72h induced apoptosis in a dose-dependent manner and increased the expression of apoptosis-related genes such as Bax, caspase-3, and caspase-9 [5].
In vivo, Matrine (300mg/kg) was orally administered to diabetic cardiomyopathy (DbCM) rats for 10 days, which reduced left ventricular function damage, restored cardiac compliance loss, and inhibited cardiac fibrosis caused by activation of the TGF-β1/Smad signaling pathway[6]. Matrine (150, 25mg/kg) was intraperitoneally injected to treat experimental autoimmune encephalomyelitis (EAE) rats, which reduced the clinical severity of EAE, reduced central nervous system cell infiltration, protected type IV collagen and ZO-1 mRNA expression, and regulated the balance between MMP-9 and tissue inhibitor of metalloproteinases (TIMP-1) in serum[7].
References:
[1] Alamgir A N M, Alamgir A N M. Secondary metabolites: Secondary metabolic products consisting of C and H; C, H, and O; N, S, and P elements; and O/N heterocycles[J]. Therapeutic use of medicinal plants and their extracts: volume 2: phytochemistry and bioactive compounds, 2018: 165-309.
[2] Chen X, Liu P, Mao Y, et al. Research Advancements in Pharmacological Activities and Mechanisms of Matrine[J]. Pharmacognosy Magazine, 2024, 20(1): 189-205.
[3] Jung Y Y, Um J Y, Narula A S, et al. Identification of matrine as a novel regulator of the CXCR4 signaling axis in tumor cells[J]. International Journal of Molecular Sciences, 2020, 21(13): 4731.
[4] Luo C, Zhong H J, Zhu L M, et al. Inhibition of matrine against gastric cancer cell line MNK45 growth and its anti-tumor mechanism[J]. Molecular Biology Reports, 2012, 39: 5459-5464.
[5] Zhou K, Ji H, Mao T, et al. Effects of matrine on the proliferation and apoptosis of human medulloblastoma cell line D341[J]. International journal of clinical and experimental medicine, 2014, 7(4): 911.
[6] Zhang Y, Cui L, Guan G, et al. Matrine suppresses cardiac fibrosis by inhibiting the TGF‑β/Smad pathway in experimental diabetic cardiomyopathy[J]. Molecular Medicine Reports, 2018, 17(1): 1775-1781.
[7] Zhang S, Kan Q C, Xu Y, et al. Inhibitory Effect of Matrine on Blood‐Brain Barrier Disruption for the Treatment of Experimental Autoimmune Encephalomyelitis[J]. Mediators of Inflammation, 2013, 2013(1): 736085.