Schisandrin B is a dibenzocyclooctadiene derivative isolated from Fructus Schisandrae, has been shown to produce antioxidant effect on rodent liver and heart. SB inhibited mitogen-induced proliferation and cytokine secretion by lymphocytes. SB also significantly inhibited mitogen-induced upregulation of T cell costimulatory molecules and activation markers. Similar anti-inflammatory effects of SB on lymphocyte proliferation and cytokine secretion were also observed in vivo[3]. Sch B can protect neuronal cells against oxidative challenge, presumably by functioning as a hormetic agent to sustain cellular redox homeostasis and mitoenergetic capacity in neuronal cells[4]. Sch B may exert neuroprotective activity by attenuating the microglial-mediated neuroinflammatory response by inhibiting the TLR4-dependent MyD88/IKK/NF-κB signaling pathway[5]. Sch B significantly suppressed the spontaneous lung and bone metastasis of 4T1 cells inoculated s.c. without significant effect on primary tumor growth and significantly extended the survival time of these mice[6].
Schizandrin B/五味子乙素 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HK-2 cells
40 µM
0, 6, 12, 18, 24, 30, 36, 42 hours
To evaluate the time-dependent effect of SchB on the viability of HK-2 cells. Results showed that SchB significantly increased cell viability at 18 hours and beyond.
Int J Mol Med. 2018 Apr;41(4):2108-2116.
THP-1™NF-κB cells
10 µM
1 hour
Evaluate antioxidant activity, results showed low antioxidant activity of Schizandrin B.
Int J Mol Sci. 2024 Mar 19;25(6):3465.
A549 adenocarcinoma cells
1, 10, 30 µM
1 hour pre-incubation and 14 days post-incubation
SchB treatment significantly decreased the viability of A549 adenocarcinoma cells after UV exposure.
Nucleic Acids Res. 2009 Sep;37(17):5678-89.
Primary cardiomyocytes
10 µM
1 hour pretreatment followed by HG exposure for 24 hours
1 hour pretreatment followed by HG exposure for 24 or 36 hours
SchB dose-dependently prevented HG-induced cardiac β-MyHc, collagen 1, and TGF-β1 expression, indicating inhibition of cardiomyocyte hypertrophy and fibrotic responses.
Adv Sci (Weinh). 2022 Nov;9(31):e2202590.
Cardiac fibroblasts
10 µM
1 hour pretreatment followed by HG exposure for 36 hours
SchB pretreatment prevented HG-induced collagen 1 and TGF-β1 expression, indicating inhibition of cardiac fibrotic responses.
Adv Sci (Weinh). 2022 Nov;9(31):e2202590.
Hippocampal neurons
10 µM
1 minute
SchB enhanced GABA and glycine-induced currents with EC50 values of 4.47 μM and 0.99 μM, respectively
Acta Pharmacol Sin. 2024 Mar;45(3):465-479.
HEK-293 cells
10 µM
1 minute
SchB enhanced GABA-induced current and rescued impaired GABA A receptors associated with genetic epilepsies
Acta Pharmacol Sin. 2024 Mar;45(3):465-479.
CHO cells
10 µM
1 minute
SchB enhanced GABA or glycine-induced current with EC50 values around 5 μM, and did not activate channels alone
Acta Pharmacol Sin. 2024 Mar;45(3):465-479.
HK-2 cells
20 µM
12 hours
To evaluate the effects of Sch B on oxidative stress and apoptosis in the hypoxia/reoxygenation (HR) model. Results showed that Sch B pretreatment reduced intracellular ROS levels and mitochondrial superoxide production, decreased the number of apoptotic cells, and improved mitochondrial membrane potential.
Drug Des Devel Ther. 2024 Sep 21;18:4241-4256.
HEK293T cells
7.25 µM (IC50)
20 min
SchB dose-dependently inhibited the protein kinase activity of immunoaffinity-purified ATR
Nucleic Acids Res. 2009 Sep;37(17):5678-89.
HK-2 cells
10 µM
24 hours
To evaluate the effect of SchB on cis-DDP-induced apoptosis in HK-2 cells. Results showed that SchB significantly attenuated cis-DDP-induced apoptosis.
Int J Mol Med. 2018 Apr;41(4):2108-2116.
HK-2 cells
0, 2.5, 5, 10, 20, 40, 80 µM
24 hours
To evaluate the effect of SchB on the viability of HK-2 cells. Results showed that 20 or 40 µM SchB significantly increased cell viability, while 80 µM SchB was toxic to the cells.
Int J Mol Med. 2018 Apr;41(4):2108-2116.
Hepa1-6 cells
25, 50, 100 µM
24 hours
To investigate the inhibitory effect of Sch B on the proliferation of Hepa1-6 cells and its mechanism. The results showed that Sch B significantly inhibited the proliferation of Hepa1-6 cells in a dose-dependent manner.
Front Immunol. 2022 Mar 28;13:857069.
Zebrafish larvae
0.75, 1.5, 3 µM
24 hours
Evaluate the effect of Schizandrin B on PTZ-induced convulsant behavior in zebrafish larvae. Results showed that 1.5 and 3 µM Schizandrin B significantly reduced PTZ-induced hyperlocomotion.
Int J Mol Sci. 2023 Aug 18;24(16):12949.
Airway smooth muscle cells (ASMCs)
100 µM
24 hours
Schizandrin B reversed the expression changes of miR-150 and BCYRN1 in MV-induced ASMCs and inhibited the viability, proliferation, and migration of ASMCs.
Cell Prolif. 2017 Dec;50(6):e12382.
MCF-10A
0 µM to 20 µM
24 hours, 48 hours
Sch B did not significantly affect the viability of normal human breast cells.
Biomolecules. 2024 Jan 5;14(1):74.
TCHBC5
10 µM, 20 µM
24 hours, 48 hours
Sch B significantly suppresses the growth, migration, and invasion of TNBC cells by inhibiting NLRP3 inflammasome activation and IL-1β production.
Biomolecules. 2024 Jan 5;14(1):74.
Hs-578T
5 µM, 10 µM, 20 µM
24 hours, 48 hours
Sch B significantly suppresses the growth, migration, and invasion of TNBC cells by inhibiting NLRP3 inflammasome activation and IL-1β production.
Biomolecules. 2024 Jan 5;14(1):74.
MDA-MB-231
5 µM, 10 µM, 20 µM
24 hours, 48 hours
Sch B significantly suppresses the growth, migration, and invasion of TNBC cells by inhibiting NLRP3 inflammasome activation and IL-1β production.
Biomolecules. 2024 Jan 5;14(1):74.
Human cardiac myocytes (HCMs)
1, 5, 10, 20, 50, 100 µM
48 hours
To evaluate the in vitro cytotoxicity of Sch B-loaded SLNs, results showed that all samples had cell viability above 80% with no obvious cytotoxicity.
Int J Nanomedicine. 2017 Sep 26;12:7121-7130.
MNT-1 cells
1, 5, 10 µM
72 hours
The inhibitory effect of Gomisin N on melanin production was not significant.
Int J Mol Sci. 2017 Feb 22;18(2):471.
NHEM cells
1, 5, 10 µM
72 hours
NHEM cells treated with Gomisin N exhibited decreased levels of L-DOPA.
Int J Mol Sci. 2017 Feb 22;18(2):471.
B16F10 cells
1, 5, 10 µM
72 hours
Gomisin N significantly reduced the melanin content without cellular toxicity.
Int J Mol Sci. 2017 Feb 22;18(2):471.
Melan-A cells
1, 5, 10 µM
72 hours
Gomisin N significantly reduced the melanin content without cellular toxicity.
Int J Mol Sci. 2017 Feb 22;18(2):471.
HepG2 cells
100 µM
90 minutes
Schizandrin B inhibited CYP2D6*10-mediated AMMC-O-demethylation activity with an inhibition rate of 59.26%.
Acta Pharmacol Sin. 2014 May;35(5):685-96.
Mast cells (MCs)
100 µM
Schizandrin B reversed the IgE/anti-IgE-induced decrease in miR-150 expression in MCs.
Cell Prolif. 2017 Dec;50(6):e12382.
Rat aortic endothelial cells (RAECs)
10 and 20 µM
1 hour pretreatment
SchB significantly ameliorated oxidative stress, mitochondrial membrane-potential depolarization and apoptosis in angiotensin II-challenged rat aortic endothelial cells.
Drug Des Devel Ther. 2018 Nov 22;12:3985-3997
Cardiac fibroblasts
1 µM
1 hour pretreatment followed by 24 or 36 hours HG exposure
Sch B prevented HG-induced collagen 1 and TGF-β1 expression, reducing fibrotic responses
Adv Sci (Weinh). 2022 Nov;9(31):e2202590.
Rat primary cardiomyocytes
1 µM
1 hour pretreatment followed by 24 or 36 hours HG exposure
Sch B prevented HG-induced β-MyHc expression, reducing cardiomyocyte hypertrophy
Adv Sci (Weinh). 2022 Nov;9(31):e2202590.
Rat cardiomyocyte-like H9C2 cells
2.5, 5, 10 µM
1 hour pretreatment followed by 24 or 36 hours HG exposure
Sch B dose-dependently prevented HG-induced cardiac β-MyHc, collagen 1, and TGF-β1 expression, reducing cardiomyocyte hypertrophy and fibrotic responses
Adv Sci (Weinh). 2022 Nov;9(31):e2202590.
Hippocampal neurons
10 µM
1 minute
SchB significantly enhanced GABA or glycine-induced current with EC50 values of 4.47 ± 0.92 μM and 0.99 ± 0.12 μM, respectively.
Acta Pharmacol Sin. 2024 Mar;45(3):465-479.
CHO/HEK-293 cells
10 µM
1 minute
SchB significantly enhanced GABA or glycine-induced current with EC50 values around 5 μM, and SchB alone did not activate the channels in the absence of GABA or glycine.
Acta Pharmacol Sin. 2024 Mar;45(3):465-479.
Bone marrow macrophages (BMMs)
5, 10, 20 µM
1, 3, 5 days
To evaluate the effect of Schizandrin B on the viability of BMMs, results showed no effect on cell viability at concentrations below 20 μM.
Front Pharmacol. 2020 Jul 31;11:1175
HK-2 cells
20 µM
12 hours
To evaluate the effect of Sch B on oxidative stress and apoptosis in the hypoxia-reoxygenation (HR) model. Results showed that Sch B pretreatment reduced intracellular ROS levels and mitochondrial superoxide production, decreased apoptosis levels, and improved mitochondrial membrane potential.
Drug Des Devel Ther. 2024 Sep 21;18:4241-4256.
SW480
75 µM
24 hours
Evaluate the inhibitory effect of Sch B on SW480 cell proliferation.
Cancer Cell Int. 2025 Mar 15;25(1):97
HT-29
75 µM
24 hours
Evaluate the inhibitory effect of Sch B on HT-29 cell proliferation.
Cancer Cell Int. 2025 Mar 15;25(1):97
HCT-116
75 µM
24 hours
Evaluate the inhibitory effect of Sch B on HCT-116 cell proliferation, with results showing an IC50 of 75 µM.
Cancer Cell Int. 2025 Mar 15;25(1):97
Airway smooth muscle cells (ASMCs)
100 µM
24 hours
Schizandrin B inhibited the viability, proliferation and migration of MV-induced ASMCs
Cell Prolif. 2017 Dec;50(6):e12382.
Hepa1-6 cells
25, 50, 100 µM
24 hours
To investigate the inhibitory effect of Sch B on Hepa1-6 cell proliferation and its mechanism. Results showed that Sch B significantly inhibited Hepa1-6 cell proliferation in a dose-dependent manner.
Front Immunol. 2022 Mar 28;13:857069.
Zebrafish larvae
0.75, 1.5, 3 µM
24 hours
Evaluate the effect of Schizandrin B on PTZ-induced seizure-like activity in zebrafish larvae. Results showed that 1.5 and 3 µM significantly reduced locomotor activity.
Int J Mol Sci. 2023 Aug 18;24(16):12949.
H9C2 cardiomyocytes
25 µM, 50 µM, 100 µM, 200 µM
24 hours
SchB significantly improved the decreased cell activity induced by THP, with 50 μM concentration showing the best effect.
Front Pharmacol. 2021 Oct 15;12:733805.
Rat chondrocytes
25, 50 µM
24, 48 hours
To evaluate the effect of Schizandrin B on chondrocyte viability and phenotype. Results showed that Schizandrin B had no obvious cytotoxicity at concentrations ≤100 μM (24 hours) and ≤75 μM (48 hours), and did not affect chondrocyte phenotype at concentrations ≤50 μM.
Drug Des Devel Ther. 2018 May 9;12:1195-1204
Human umbilical cord mesenchymal stem cells (hUCMSCs)
2.5 µM and 20 µM
3 to 5 days
To evaluate the protective effects of SchB on hypothermic preservation of hUCMSCs. Results showed that SchB significantly improved cell viability and maintained unique properties.
Tissue Eng Regen Med. 2023 Jun;20(3):447-459
SW620
0-200 µM
48 hours
SchB inhibited the proliferation of SW620 cells in a concentration-dependent manner with an IC50 value of 50 μM. SchB treatment significantly reduced the colony-forming ability of SW620 cells.
ACS Pharmacol Transl Sci. 2024 Feb 22;7(3):863-877
HT29
0-200 µM
48 hours
SchB inhibited the proliferation of HT29 cells in a concentration-dependent manner with an IC50 value of 50 μM. SchB treatment significantly reduced the colony-forming ability of HT29 cells.
ACS Pharmacol Transl Sci. 2024 Feb 22;7(3):863-877
HCT116
0-200 µM
48 hours
SchB inhibited the proliferation of HCT116 cells in a concentration-dependent manner with an IC50 value of 50 μM. SchB treatment induced cell cycle arrest at G0/G1 phase and apoptosis.
ACS Pharmacol Transl Sci. 2024 Feb 22;7(3):863-877
Rat chondrocytes
25, 50 µM
48 hours
To evaluate the effect of Schizandrin B on IL-1β-induced inflammation and cartilage gene expression changes. Results showed that Schizandrin B significantly reduced IL-1β-induced upregulation of inflammatory genes (IL-6, iNOS) and matrix-degrading genes (MMP3, MMP13), and reversed IL-1β-induced downregulation of collagen II, aggrecan, and sox9.
Drug Des Devel Ther. 2018 May 9;12:1195-1204
Bone marrow macrophages (BMMs)
5, 10, 20 µM
5 days
To evaluate the effect of Schizandrin B on osteoclast differentiation, results showed Schizandrin B significantly inhibited osteoclast formation.
Front Pharmacol. 2020 Jul 31;11:1175
Human umbilical cord mesenchymal stem cells (UC-MSCs)
10 µM
from the second stage of thourse differentiation process
Promotes hepatic differentiation and maturation of UC-MSCs into hepatocyte-like cells (HLCs), increasing hepatic marker levels and hepatic function
iScience. 2024 Jan 15;27(2):108912
Schizandrin B/五味子乙素 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Zebrafish embryos
Zebrafish embryo model
1, 10, 20, 30 µM
72 hours
Gomisin N treatment significantly reduced melanin formation in zebrafish embryos.
Int J Mol Sci. 2017 Feb 22;18(2):471.
Sprague-Dawley rats
Myocardial infarction model
Tail vein injection
10 mg/kg
Single dose, observed for 72 hours
To evaluate the pharmacokinetics and biodistribution of Sch B-loaded SLNs, results showed that MMP-Sch B SLNs had significantly higher drug concentration in the heart and significantly reduced myocardial infarction size.
Int J Nanomedicine. 2017 Sep 26;12:7121-7130.
CD-1 mice
PTZ-induced seizure model
Intraperitoneal injection
10, 30, 60 mg/kg
Single dose, 30 minutes prior
SchB dose-dependently delayed the onset of GTCS and reduced the incidence of GTCS and mortality
Acta Pharmacol Sin. 2024 Mar;45(3):465-479.
BALB/c mice
Ethanol-induced liver and brain injury models
Oral
20 mg/kg
Preventive model: 15 days; Corrective model: 14 days
Sch B can effectively prevent and ameliorate ethanol-induced liver injuries, lipid deposition, inflammasome activation, and fibrosis, while reversing brain damage and improving neurological function.
Nutrients. 2023 Apr 15;15(8):1909
Mice
Oligoasthenospermia mice model
Oral
20 mg/kg/day
Once daily for 2 weeks
SB could repair spermatogenic blockage in oligoasthenospermia mice, increase sperm count, motility, and motion velocities, and improve fertility.
Clin Transl Med. 2021 Feb;11(2):e333
BALB/c mice
Angiostrongylus cantonensis infection model
Oral
20 mg/kg/day
7 consecutive days
To investigate the effects of Schizandrin B in combination with albendazole on Angiostrongylus cantonensis-induced meningoencephalitis. Results showed that co-treatment significantly suppressed neuroinflammation, increased survival rate, and improved sensorimotor functions.
Biomolecules. 2020 Jul 5;10(7):1001
BALB/c mice
Renal ischemia-reperfusion injury (RIRI) model
Oral gavage
20 mg/kg/day and 40 mg/kg/day
7 consecutive days
To evaluate the protective effects of Sch B on RIRI. Results showed that Sch B pretreatment significantly reduced renal pathological damage and inflammatory response, decreased plasma creatinine and urea nitrogen levels, reduced the number of apoptotic cells, and partially restored renal function.
Drug Des Devel Ther. 2024 Sep 21;18:4241-4256.
Db/db mice (type 2 diabetes model)
Type 2 diabetic cardiomyopathy model
Oral gavage
20 or 40 mg/kg
Every other day for 8 weeks
SchB treatment protected heart function, reduced myocardial injuries, and decreased inflammatory cytokine secretion, ameliorating cardiac hypertrophy and fibrosis.
Adv Sci (Weinh). 2022 Nov;9(31):e2202590.
Drosophila melanogaster
High-fat diet-induced obesity model
Oral
25 μg/mL or 50 μg/mL
Continuous for 2 weeks
To investigate the effects of GN on HFD-induced obesity phenotypes, results showed that GN reduced body weight, improved climbing activity, and extended lifespan.
Int J Mol Sci. 2020 Sep 29;21(19):7209
Mice
Intravenous PTZ seizure model
Intraperitoneal injection
50 mg/kg
Single administration, tested at 30, 60, 120, and 240 minutes post-administration
Evaluate the effect of Schizandrin B on seizure thresholds in mice. Results showed that Schizandrin B did not significantly alter seizure thresholds in mice.
Int J Mol Sci. 2023 Aug 18;24(16):12949.
SD rats
Asthma model
Intragastric administration
80 mg/kg/day
Once daily for 6 weeks
Schizandrin B up-regulated miR-150 expression and down-regulated BCYRN1 expression in asthma model rats, inhibiting the proliferation and migration of ASMCs.
Cell Prolif. 2017 Dec;50(6):e12382.
CD-1 mice
PTZ-induced seizure model
Intraperitoneal injection
10, 30, 60 mg/kg
Single dose, 30 minutes before PTZ injection
SchB dose-dependently delayed the onset of GTCS and reduced the incidence of GTCS and mortality.
Acta Pharmacol Sin. 2024 Mar;45(3):465-479.
BALB/c mice
Ethanol-intoxicated mice model
Oral
20 mg/kg
Once daily for 14 days
Sch B can effectively prevent and ameliorate alcoholic liver diseases, such as resolving liver injuries, lipid deposition, inflammasome activation, and fibrosis. Moreover, Sch B reverses brain damage and improves the neurological function of ethanol-treated mice.
Nutrients. 2023 Apr 15;15(8):1909
Mice
Oligoasthenospermia mice model
Oral
20 mg/kg/day
Once daily for 2 weeks
SB could repair damaged seminiferous tubules and spermatogenic cells, increase sperm count, motility, and motion velocities, and improve fertility.
Clin Transl Med. 2021 Feb;11(2):e333
BALB/c mice
Angiostrongylus cantonensis infection model
Oral
20 mg/kg/day
Once daily for 7 consecutive days
To investigate the effects of Schizandrin B in combination with albendazole to treat Angiostrongylus-induced meningoencephalitis. Results showed that co-treatment significantly inhibited inflammasome activation, pyroptosis, and apoptosis, and repaired the sensorimotor functions of the mice.
Biomolecules. 2020 Jul 5;10(7):1001
BALB/c mice
Renal ischemia-reperfusion injury (RIRI) model
Oral gavage
20 mg/kg/day and 40 mg/kg/day
7 consecutive days
To evaluate the protective effect of Sch B on the RIRI mouse model. Results showed that Sch B pretreatment significantly reduced renal pathological damage, inflammatory response, and apoptosis, lowered plasma creatinine and urea nitrogen levels, and partially restored renal function.
Drug Des Devel Ther. 2024 Sep 21;18:4241-4256.
Db/db mice (type 2 diabetes model)
Type 2 diabetic cardiomyopathy model
Oral gavage
20 or 40 mg/kg
Every other day for 8 weeks
Sch B protected heart function, reduced myocardial injuries and inflammatory cytokine secretion, and inhibited cardiac hypertrophy and fibrosis
Adv Sci (Weinh). 2022 Nov;9(31):e2202590.
C57 mice
LPS-induced endometritis model
Intraperitoneal injection
20, 40 and 80 mg/kg
Administered 1 h before LPS treatment, lasting for 24 hours
Sch B significantly inhibited the pathological injury of uterine tissue, MPO activity, the activation of NF-κB pathway and the production of TNF-α and IL-1β. Furthermore, Sch B effectively inhibited ferroptosis by inhibiting MDA and iron production and promoting the expression of ferroptosis suppressor genes GPX4 and ferritin.
J Cell Mol Med. 2024 Dec;28(23):e70281
C57BL/6 mice
Ovariectomy-induced bone loss model
Intragastric gavage
30 mg/kg
Every other day for 6 weeks
To evaluate the protective effect of Schizandrin B on ovariectomy-induced bone loss, results showed Schizandrin B significantly attenuated bone loss.
Front Pharmacol. 2020 Jul 31;11:1175
BALB/c nude mice
HCT116 xenograft model
Oral gavage
50 mg/kg
Every other day for 14 days
SchB significantly inhibited the growth of HCT116 xenograft tumors, reducing tumor volume and weight without causing significant side effects.
ACS Pharmacol Transl Sci. 2024 Feb 22;7(3):863-877
Mice
Intravenous pentylenetetrazole (PTZ) seizure model
Intraperitoneal (ip) administration
50 mg/kg
Single administration
Evaluate the anticonvulsant activity of Schizandrin B in the mouse PTZ seizure model. Results showed that Schizandrin B did not significantly alter seizure thresholds.
Int J Mol Sci. 2023 Aug 18;24(16):12949.
SD rats
THP-induced cardiotoxicity model
Dietary feeding
50 mg/kg
Once a week for 8 weeks
SchB significantly improved THP-induced cardiotoxicity, including abnormal body weight and food intake, changes in ECG and echocardiography, myocardial tissue damage, and oxidative stress state.
Front Pharmacol. 2021 Oct 15;12:733805.
Sprague Dawley rats
OA model induced by surgical resection of medial meniscus
Intra-articular injection
50 μM
Every 7 days for 4 weeks
To evaluate the effect of Schizandrin B on cartilage degeneration in rat OA model. Results showed that Schizandrin B significantly reduced Mankin’s score, cartilage degeneration, and expression of inflammatory markers (cox-2, MMP13).
Drug Des Devel Ther. 2018 May 9;12:1195-1204
SD rats
Asthma model
Intragastric administration
80 mg/kg/day
Once daily for 6 weeks
Schizandrin B up-regulated miR-150 expression and down-regulated BCYRN1 expression, and inhibited the proliferation and migration of ASMCs
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