Morusin is a prenylated flavonoid isolated from M. australis with various biological activities, such as antitumor, antioxidant, and anti-bacteria property. Morusin shows suppression of NF-κB and STAT3 in many cancer cell lines including HT-29, A549, MCF-7, and MDA-MB-231. Morusin exhibits a dose- and time-dependent inhibitory effect on murine and human breast cancer cells. IC50 is 9.48 μg/mL for normal mammary epithelial cells (MCF-10A); 2.03 and 1.87 μg/mL for murine breast cancer cells (4 T1 and EMT6); and 2.71 and 3.86 μg/mL for human breast cancer cells (MCF-7 and MDA-MB-231), respectively, the maximal inhibition of cell growth (>80 %) is obtained at 8 μg/mL[3]. Morusin significantly inhibited the growth and clonogenicity of human colorectal cancer HT-29 cells. Morusin also inhibited the phosphorylation of IKK-alpha, IKK-beta and IkappaB-alpha, increased expression of IkappaB-alpha, and suppressed nuclear translocation of NF-kappaB and its DNA binding activity[4]. Morusin reduces the OA (Osteoarthritis) inflammatory response in vitro and protects against articular cartilage degradation in vivo potentially via regulation of the NF-κB pathway[5]. Morusin could inhibit the growth of RCC (Renal cell carcinoma) cells in vitro and in vivo through MAPK signal pathways[6].
Morusin/桑辛素 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human breast cancer cells (MDA-MB-231)
1, 2, 4, 6, 8 μg/ml
1, 2, 3, 4, 5 days
Test the cytotoxicity of Morusin on MDA-MB-231 cells, IC50 was 3.86 μg/ml
J Exp Clin Cancer Res. 2015 Nov 4;34:137.
Human breast cancer cells (MCF-7)
1, 2, 4, 6, 8 μg/ml
1, 2, 3, 4, 5 days
Test the cytotoxicity of Morusin on MCF-7 cells, IC50 was 2.71 μg/ml
J Exp Clin Cancer Res. 2015 Nov 4;34:137.
Murine breast cancer cells (EMT6)
1, 2, 4, 6, 8 μg/ml
1, 2, 3, 4, 5 days
Test the cytotoxicity of Morusin on EMT6 cells, IC50 was 1.87 μg/ml
J Exp Clin Cancer Res. 2015 Nov 4;34:137.
Murine breast cancer cells (4T1)
1, 2, 4, 6, 8 μg/ml
1, 2, 3, 4, 5 days
Test the cytotoxicity of Morusin on 4T1 cells, IC50 was 2.03 μg/ml
J Exp Clin Cancer Res. 2015 Nov 4;34:137.
Human normal mammary epithelial cells (MCF-10A)
1, 2, 4, 6, 8 μg/ml
1, 2, 3, 4, 5 days
Test the cytotoxicity of Morusin on normal mammary epithelial cells, IC50 was 9.48 μg/ml
J Exp Clin Cancer Res. 2015 Nov 4;34:137.
Aortic valve interstitial cells (VICs)
1 μM
21 days
To evaluate the long-term effect of Morusin on osteogenic differentiation of VICs. Results showed Morusin significantly reduced calcific nodule formation.
Adv Sci (Weinh). 2024 May;11(20):e2307319.
Aortic valve interstitial cells (VICs)
1 μM
7 days
To evaluate the inhibitory effect of Morusin on osteogenic differentiation of VICs. Results showed Morusin significantly suppressed OM-induced ALP activity and calcific nodule formation.
Adv Sci (Weinh). 2024 May;11(20):e2307319.
Bone marrow mesenchymal stem cells (BMSCs)
2.5-10 μM
3, 5, 7, 14 days
Promoted proliferation and osteogenic differentiation of BMSCs, with 10 μM Morusin showing the strongest effect
Stem Cell Res Ther. 2021 Mar 12;12(1):173.
FH c cells (normal fetal colonic mucosa cells)
9.1, 18.2, 36.4 µM
24, 48, 72 hours
Morusin did not significantly affect the proliferation of normal colonic mucosa cells FH c.
Int J Mol Med. 2021 Apr;47(4):1.
HCT116 human colorectal cancer cells
9.1, 18.2, 36.4 µM
24, 48, 72 hours
Morusin significantly inhibited the proliferation of HCT116 sphere cells in a concentration- and time-dependent manner.
Int J Mol Med. 2021 Apr;47(4):1.
SW480 cells
0, 2.5, 5 μM
24 hours
Evaluate the effect of Morusin on SW480 cell colony formation, results showed Morusin reduced the number of colonies
Cells. 2021 Aug 12;10(8):2065.
HCT116 cells
0, 2.5, 5 μM
24 hours
Evaluate the effect of Morusin on HCT116 cell colony formation, results showed Morusin reduced the number of colonies
Cells. 2021 Aug 12;10(8):2065.
SW480 cells
0, 2.5, 5, 10 μM
24 hours
Evaluate the effect of Morusin on SW480 cell viability, results showed Morusin inhibited cell viability
Cells. 2021 Aug 12;10(8):2065.
HCT116 cells
0, 2.5, 5, 10 μM
24 hours
Evaluate the effect of Morusin on HCT116 cell viability, results showed Morusin inhibited cell viability
Cells. 2021 Aug 12;10(8):2065.
HeLa cells
1-10 μM
12 hours
Inhibited phosphorylation of p70S6K1, promoted autophagy, and slowed cell senescence
elegans via suppressing nutrient-sensing pathways. Geroscience.
RAW264.7 macrophages
9.87 ± 0.59 μM
24 hours
Evaluate the inhibitory effect of Morusin on NO production in RAW264.7 macrophages, showing that Morusin exhibited stronger anti-NO activity than the positive control quercetin.
Antioxidants (Basel). 2022 Nov 11;11(11):2222.
Ruminal epithelial cells (RECs)
25 µg/mL and 50 µg/mL
12 hours
Morusin exerted anti-inflammatory effects in a concentration-dependent manner, with 50 µg/mL Morusin significantly downregulating the gene expression of TNF-α, CD40, IL-6, and CCL20 in RECs
Int J Mol Sci. 2022 Nov 20;23(22):14428.
Morusin/桑辛素 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Caenorhabditis elegans
Wild-type N2 and akt-1(ok525) and akt-2(ok393) mutants
NGM media or E. coli OP50-1 feeding
120 μM
Starting from the L4 stage and continued throughout lifespan
Extended mean lifespan, increased reproduction, without affecting health metrics (e.g., pharyngeal pumping rate)
elegans via suppressing nutrient-sensing pathways. Geroscience.
Nude mice
Subcutaneous xenograft model of human breast cancer MCF-7 cells
Intraperitoneal injection
5, 10 mg/kg
Three times weekly for 4 weeks
Test the tumor inhibitory effect of Morusin on MCF-7 xenografts, tumor inhibitory rates were 46.5% and 64.1% at doses of 5 mg/kg and 10 mg/kg, respectively
J Exp Clin Cancer Res. 2015 Nov 4;34:137.
ApoE−/− mice
High-fat Western diet-induced aortic valve calcification model
Gavage
40 mg/kg
Twice a week for 24 weeks
To evaluate the therapeutic effect of Morusin on aortic valve calcification. Results showed Morusin significantly alleviated high-fat diet-induced aortic valve calcification and reduced ROS levels.
Adv Sci (Weinh). 2024 May;11(20):e2307319.
Wistar rats
Ovariectomy-induced osteoporosis model
Intragastric administration
40 mg/kg
Every 5 days for 4 weeks
Morusin attenuated bone loss in OVX rats, increased trabecular number and bone mass indexes
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