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.
苦参碱（Matrine）是一种存在于槐属植物中的生物碱，可作为 kappa 阿片受体和µ-受体激动剂[1]。Matrine具有多种药理作用，包括抗癌、抗氧化应激、抗炎和抗凋亡作用[2]。
在体外，Matrine（50μM）处理A549、DU145和MIA PaCa-2细胞24h，抑制了细胞中CXC趋化因子受体4型（CXCR4）的表达，下调了基质金属蛋白酶（MMP-2和MMP-9）水平，减弱了细胞迁移活性[3]。Matrine（50-500μg/ml）处理胃癌细胞系MNK45，以剂量依赖性方式抑制细胞增殖，IC50值为540μg/ml，显著影响了细胞内NF-κB、XIAP、CIAP和 p-ERK蛋白的表达[4]。Matrine（0.5-2.0 mg/mL）处理D341细胞24-72h，以剂量依赖性方式诱导细胞凋亡，增加Bax、caspase-3、caspase-9等凋亡相关基因的表达[5]。
在体内，Matrine（300mg/kg）通过口服治疗糖尿病心肌病（DbCM）大鼠10天，减轻了左心室功能损伤，恢复心脏顺应性损失，抑制TGF-β1/Smad信号通路激活引起的心脏纤维化[6]。Matrine（150、250mg/kg）通过腹腔注射治疗实验性自身免疫性脑脊髓炎（EAE）大鼠，减轻了EAE的临床严重程度，减少了中枢神经系统细胞浸润，保护了IV型胶原蛋白和ZO-1 mRNA表达，调节血清中MMP-9和金属蛋白酶组织抑制剂（TIMP-1）之间的平衡[7]。