[E-(+)-Matrine (Matrine) is an alkaloid found in plants from the Sophora genus. It has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor and u-receptor agonist. Matrine treatment dose-dependently reduced cell viability and increased the apoptotic rate of HepG2 cells. Matrine treatment induced mitochondrial dysfunction and activated mitochondrial apoptosis by inhibiting protective mitophagy[3]. Matrine activates p38 pathway leading to a caspase-dependent apoptosis by inducing generation of ROS (reactive oxygen species) in NSCLC (Non-small cell lung carcinoma) cells[4]. Matrine can alleviate muscle atrophy and improve myoblast differentiation possibly by inhibiting E3 ubiquitin ligases and activating the Akt/mTOR/FoxO3α signaling pathway[5]. MAT (Matrine) significantly improved the D-gal-induced recognition and spatial memory impairment in novel object recognition and Y maze tests, and exercise endurance decreased in the weight-loaded swimming test at 2 and 10 mg/kg[6]. Matrine inhibited proliferation of cancer cells in a dose- and time-dependent manner. Matrine induced cell-cycle arrest at G1/G0 phase, induced apoptosis and reduced expression of Bcl-2 and caspase-3 while up-regulating Bax and cleaved caspase-3 in the four CRC (colorectal cancer) cells[7].
Matrine/苦参碱 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human monocytes
100 µM
18 hours
To investigate the effect of Matrine on the production of IFN-β, IL-27, and IL-10 in human monocytes and its inhibitory effect on TNF-α. The results showed that Matrine significantly increased the production of IFN-β and induced the production of IL-27 and IL-10 while suppressing TNF-α.
Front Immunol. 2020 Sep 25;11:569530.
Human peritoneal mesothelial cells
0.2, 0.4, 0.6 g/L
24 and 72 hours
Matrine inhibited LPS-induced EMT in HPMCs in a dose-dependent manner, increased the expression of E-cadherin, and decreased the expression of alpha-smooth muscle actin.
Chin Med J (Engl). 2019 Mar 20;132(6):664-670.
H9C2 cells
200 µM
24 hours
To verify the protective effect of matrine on DOX-induced oxidative stress and cardiomyocyte apoptosis, the results showed that matrine alleviated DOX-induced oxidative stress and apoptosis by activating the AMPK α/UCP2 pathway.
Acta Pharm Sin B. 2019 Jul;9(4):690-701.
A2780/DDP cells
2.0 mg/mL
24 hours
To detect the inhibitory effect of matrine on the proliferation of cisplatin-resistant ovarian cancer cells, the results showed that matrine significantly inhibited the proliferation of A2780/DDP cells.
Cell Death Dis. 2019 Oct 10;10(10):770.
Neonatal rat cardiac fibroblasts
200 µM
24 hours
Matrine significantly inhibited the proliferation, migration, collagen production, and phenotypic transdifferentiation of cardiac fibroblasts.
Acta Pharmacol Sin. 2021 Apr;42(4):573-584.
Human cardiac fibroblasts
200 µM
24 hours
Matrine significantly suppressed α-SMA protein levels and the mRNA levels of Col1 and Col3 in human cardiac fibroblasts.
Acta Pharmacol Sin. 2021 Apr;42(4):573-584.
A2780 cells
0-2.0 mg/mL
24, 48, 72 hours
To detect the inhibitory effect of matrine on the proliferation of ovarian cancer cells, the results showed that matrine significantly inhibited the proliferation of A2780 and SKOV3 cells in a dose- and time-dependent manner.
Cell Death Dis. 2019 Oct 10;10(10):770.
SKOV3 cells
0-2.0 mg/mL
24, 48, 72 hours
To detect the inhibitory effect of matrine on the proliferation of ovarian cancer cells, the results showed that matrine significantly inhibited the proliferation of A2780 and SKOV3 cells in a dose- and time-dependent manner.
Cell Death Dis. 2019 Oct 10;10(10):770.
Mz-ChA-1 cells
0.25, 0.5, 1.0, 1.5, 2.0 mg/ml
48 hours
To investigate the toxic effect of matrine on Mz-ChA-1 cells, results showed that matrine induced cell death in a dose-dependent manner.
Cell Death Discov. 2017 Jan 23;3:16096.
QBC939 cells
0.25, 0.5, 1.0, 1.5, 2.0 mg/ml
48 hours
To investigate the toxic effect of matrine on QBC939 cells, results showed that matrine induced cell death in a dose-dependent manner.
Cell Death Discov. 2017 Jan 23;3:16096.
Canine primary mammary epithelial cells
250 µg/mL
72 hours
Determine the maximum safe concentration of Matrine in canine mammary epithelial cells, results showed cell survival rate greater than 90% at 250 µg/mL
Int J Mol Sci. 2023 Dec 30;25(1):540.
Canine mammary tumor cell lines CHMm
250 µg/mL
72 hours
Matrine had a time-dependent proliferation inhibitory effect on CHMm cells within a safe concentration range and induced autophagy
Int J Mol Sci. 2023 Dec 30;25(1):540.
Canine mammary tumor cell lines CHMp
250 µg/mL
72 hours
Matrine had a time-dependent proliferation inhibitory effect on CHMp cells within a safe concentration range and induced autophagy
Int J Mol Sci. 2023 Dec 30;25(1):540.
Matrine/苦参碱 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c Nude mice
A2780 xenograft model
Intraperitoneal injection
100 mg/kg
Three times a week for 3 weeks
To investigate the role of matrine in vivo on the growth of A2780 xenograft tumors, the results showed that matrine significantly suppressed tumor growth and reduced tumor volume and weight.
Cell Death Dis. 2019 Oct 10;10(10):770.
Mice
Chronic unpredictable mild stress (CUMS)-induced depression model
Intragastric administration
15 mg/kg, 30 mg/kg, 60 mg/kg
Once daily for 2 weeks
Matrine alleviates depressive-like behaviors in CUMS-induced mice by modulating gut microbiota and metabolites, restoring intestinal permeability, reducing peripheral blood circulation and neuroinflammation, and increasing BDNF protein expression.
J Transl Med. 2023 Feb 24;21(1):145
C57BL/6 mice
Experimental autoimmune encephalomyelitis (EAE)
Intraperitoneal injection
150 mg/kg
Once daily for 13 days
To investigate the therapeutic effect of Matrine on EAE mice and its mechanism. The results showed that Matrine significantly alleviated the clinical symptoms of EAE, reduced CNS inflammation and demyelination, and exerted its therapeutic effect by inducing the production of IFN-β, IL-27, and IL-10.
Front Immunol. 2020 Sep 25;11:569530.
C57/B6 mice
Aortic banding (AB) operation or continuous injection of isoprenaline (ISO) induced cardiac fibrosis model
Intragastric administration
200 mg/kg/d
Once daily for 4 weeks
Matrine significantly attenuated AB or ISO-induced fibrotic remodeling and cardiac dysfunction and ameliorated preexisting cardiac fibrosis in mice.
Acta Pharmacol Sin. 2021 Apr;42(4):573-584.
C57/B6 mice
DOX-induced cardiotoxicity model
Intragastric administration
200 mg/kg/day
Once daily for 4 weeks
To investigate the protective effect of matrine on DOX-induced cardiotoxicity, the results showed that matrine alleviated DOX-induced oxidative stress and cardiomyocyte apoptosis by maintaining the AMPK α/UCP2 pathway.
Acta Pharm Sin B. 2019 Jul;9(4):690-701.
Nude mice
HepG2 xenograft model
Intraperitoneal injection
50, 75, 100 mg/kg
Every other day for 3 weeks
To investigate the inhibitory effect of matrine on the proliferation of HepG2 cells in nude mice, results showed that matrine significantly attenuated tumor growth with AIF release from mitochondria into nucleus.
Mol Cancer. 2014 Mar 16;13:59.
Mice
Electric pacing-induced atrial fibrillation model
Intravenous injection
15 mg/kg, 30 mg/kg, 45 mg/kg
Once daily for 15 days
Evaluated the protective effects of Matrine on atrial fibrillation, results showed Matrine reduced AF incidence and duration in a dose-dependent manner
Int J Biol Sci. 2012;8(1):150-8
BALB/c nude mice
A2780 xenograft model
Intraperitoneal injection
100 mg/kg
Three times a week for 3 weeks
Matrine significantly inhibited the growth and metastasis of A2780 xenograft tumors
Cell Death Dis. 2019 Oct 10;10(10):770.
C57/B6 mice
Aortic banding (AB) operation or continuous injection of isoprenaline (ISO) to generate pathological cardiac fibrosis
Intragastric administration
200 mg/kg/d
Once daily for 4 weeks
Matrine lavage significantly attenuated AB or ISO-induced fibrotic remodeling and cardiac dysfunction
Acta Pharmacol Sin. 2021 Apr;42(4):573-584.
BALB/c mice
Psoriasis-like mouse model
Intraperitoneal injection
50 mg/kg
Once daily for 7 consecutive days
Matrine significantly improved the skin inflammation score in psoriasis-like mouse models and showed synergistic effects with acitretin.
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