Calycosin, a phytoestrogen, is a partial agonist of ER and a calcium channel blocker. It also shows prevention of reperfusion injury. Calycosin can be isolated and purified from the herb of Astragalus membranaceus Bge. var. mongholicus with anti-oxidative activity. Calycosin had obvious anti-proliferation effects on SKOV3 cells in a dose- and time-dependent manner. calycosin up-regulated the Bax/Bcl-2 ratio and cleaved caspase-3, cleaved caspase-9 expression in a dose-dependent manner[3]. In mice bearing MCF-7 or SKBR3 xenografts, tumor growth was inhibited by calycosin, and changes in expression the levels of WDR7-7 and GPR30 (G-protein coupled estrogen receptor 30) in tumor tissues were similar to those in cultured MCF-7 and SKBR3 cells[4]. Calycosin is more effective in inhibiting breast cancer growth in comparison with genistein, through its regulation of Akt signaling pathways and HOTAIR expression[5]. Calycosin inhibited oxidative stress and autophagy in CKD (chronic kidney disease) induced skeletal muscle atrophy and in TNF-α-induced C2C12 myotube atrophy, partially by regulating the AMPK/SKP2/CARM1 signalling pathway[6]. Calycosin dose-dependently inhibited cell viability and increased LDH release in CC (cervical cancer) cells, suggesting the cytotoxic effect of calycosin on CC cells. Calycosin enhanced the apoptotic rate and caspase-3 activity and decreased the number of invaded cells in CC cells. Calycosin inhibited viability, induced apoptosis, and suppressed invasion of CC cells by upregulating tumor suppressor miR-375[7].
Calycosin/毛蕊异黄酮 细胞实验
Cell Line
Concentration
Treated Time
Description
References
B-CPAP cells
100 µM
12 days
Inhibited the colony formation of B-CPAP cells
Front Pharmacol. 2022 Dec 16;13:1056687.
B-CPAP cells
100 µM
24 hours
Promoted the autophagy of B-CPAP cells
Front Pharmacol. 2022 Dec 16;13:1056687.
U251 cells
100 and 200 µM
18 hours
To evaluate the inhibitory effect of Calycosin on cell migration, results showed that 100 and 200 μM significantly reduced the number of migrating cells.
J Exp Clin Cancer Res. 2017 Nov 2;36(1):153.
B-CPAP cells
0, 25, 50, 100 µM
24 hours
Inhibited the proliferation of B-CPAP cells
Front Pharmacol. 2022 Dec 16;13:1056687.
U87 cells
100 and 200 µM
18 hours
To evaluate the inhibitory effect of Calycosin on cell migration, results showed that 100 and 200 μM significantly reduced the number of migrating cells.
J Exp Clin Cancer Res. 2017 Nov 2;36(1):153.
U251 cells
0-800 µM
24 hours
To evaluate the effect of Calycosin on cell proliferation, results showed that high concentrations (>400 μM) significantly inhibited cell proliferation.
J Exp Clin Cancer Res. 2017 Nov 2;36(1):153.
U87 cells
0-800 µM
24 hours
To evaluate the effect of Calycosin on cell proliferation, results showed that high concentrations (>400 μM) significantly inhibited cell proliferation.
J Exp Clin Cancer Res. 2017 Nov 2;36(1):153.
Rat thoracic aortic smooth muscle cell line A7r5
0-20 µM
24 hours
Calycosin inhibited vascular calcification by enhancing autophagic flux, reducing calcium nodule formation, decreasing calcium content and ALP activity, and suppressing the upregulation of RUNX2, BMP2, and OPN as well as the downregulation of SM22α.
Nutrients. 2023 Dec 27;16(1):99.
H9c2 cardiomyocytes
10 µM, 20 µM, 30 µM, 50 µM
24 hours
To evaluate the protective effect of Calycosin on doxorubicin-induced myocardial cell damage. Results showed that Calycosin significantly protected cells from damage at lower concentrations (10-30μM) while exhibiting cytotoxicity at higher concentrations (50 μM).
Front Pharmacol. 2024 Nov 12;15:1497733.
HK-2 cells
8 µM, 16 µM, 32 µM
24 hours
To investigate the inhibitory effect of CAL on H/R-induced inflammatory response in HK-2 cells. Results showed that CAL dose-dependently reduced HIF-1α expression, inhibited the production of inflammatory cytokines (IL-1β, IL-6, TNF-α), and suppressed NF-κB activation.
Front Pharmacol. 2022 Oct 7;13:970616.
Bone marrow-derived macrophages (BMMs)
2.5, 5, 10 µM
3 days
To investigate the effect of Calycosin on RANKL-induced osteoclast differentiation. Results showed that Calycosin significantly inhibited RANKL-induced osteoclast formation in a dose-dependent manner.
Int J Mol Sci. 2015 Dec 10;16(12):29496-507.
HCT116 cells
100 µM
48 hours
Calycosin suppressed TGF-β-induced EMT and migration by upregulating BATF2 expression.
J Exp Clin Cancer Res. 2019 Jun 7;38(1):240.
B16F10 melanoma cells
20, 40, 80 µM
48 hours
Evaluate the inhibitory effect of Calycosin on α-MSH-induced melanin synthesis and tyrosinase activity. Results showed that Calycosin significantly inhibited melanin synthesis and tyrosinase activity in a dose-dependent manner.
Int J Mol Sci. 2022 Jan 25;23(3):1358.
HaCaT keratinocytes
10-100 µM
48 or 72 hours
Evaluate the effect of Calycosin on cell viability and determine the maximum concentration for future experiments. Results showed that cell viability remained above 80% after 48 or 72 hours.
Int J Mol Sci. 2022 Jan 25;23(3):1358.
B16F10 melanoma cells
10-80 µM
48 or 72 hours
Evaluate the effect of Calycosin on cell viability and determine the maximum concentration for future experiments. Results showed that cell viability remained above 80% after 48 or 72 hours.
Int J Mol Sci. 2022 Jan 25;23(3):1358.
LoVo cells
50, 100, 150 µM
6, 12, 24, 48 hours
Calycosin inhibited the proliferation of LoVo cells in a dose- and time-dependent manner. Significant inhibition was observed at 50 and 100 μM concentrations at 48 h, and at 150 μM concentration at 12 or 48 h (P<0.05).
J Exp Clin Cancer Res. 2019 Jun 7;38(1):240.
Calycosin/毛蕊异黄酮 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Wistar rats
Doxorubicin-induced heart failure model
Intraperitoneal injection
10 mg/kg
Once daily for four consecutive weeks
To evaluate the effect of Calycosin on cardiac function and myocardial injury in rats with heart failure. Results showed that Calycosin significantly improved cardiac function, reduced serum NT-Pro BNP levels, and alleviated myocardial cell damage and fibrosis.
Front Pharmacol. 2024 Nov 12;15:1497733.
Mice
APP/PS1 transgenic Mice model
Intraperitoneal injection
10, 20, and 40 mg/kg
Daily for 70 days
Calycosin significantly improved cognitive function in APP/PS1 mice by activating the protein kinase C (PKC) pathway, reducing hippocampal levels of beta amyloid, Tau protein, interleukin-1beta, tumor necrosis factor-alpha, acetylcholinesterase, and malondialdehyde, while increasing acetylcholine and glutathione activities. These neuroprotective effects were abolished by the PKC inhibitor calphostin C.
Neural Regen Res. 2017 Nov;12(11):1870-1876
Drosophila melanogaster
Parkinson's disease model
Oral
100 µM
48 hours
Calycosin significantly improved the survival rate, locomotor function, reduced oxidative stress, protected dopaminergic neurons, and improved mitochondrial function and autophagy regulation in PQ-exposed Drosophila.
Antioxidants (Basel). 2022 Jan 24;11(2):222
Rats
Drug metabolism model
Intragastric
25 mg/kg
Once daily for 8 days
To investigate the effect of Calycosin on the CYP450 system, results showed that Calycosin inhibits the catalytic activities of CYP1A2, CYP2D6 and CYP2C9
Drug Des Devel Ther. 2020 Jan 29;14:429-434
Sprague-Dawley rats
Diabetic nephropathy model
Oral
30 mg/kg
4 weeks
To assess the regulatory effects of calycosin-loaded nanoliposomes on mitochondrial function in diabetic nephropathy rats
J Nanobiotechnology. 2021 Jun 13;19(1):178
Sprague-Dawley rats
Hind limb unloading (HLU) model
Intragastric administration
30 mg/kg
Once daily for 4 weeks
To investigate the potential protective effects of calycosin against bone loss induced by microgravity. Results showed that calycosin significantly increased bone mineral density (BMD), improved the microstructure of femoral trabecular bone, cortical bone thickness, and biomechanical properties of the bone. Analysis of bone turnover markers in serum indicated that both bone formation and resorption markers decreased after calycosin treatment. Additionally, bone remodeling-related cytokines (IFN-γ, IL-6, IL-8, IL-12, IL-4, IL-10, and TNF-α) in serum were partially restored after calycosin treatment.
NPJ Microgravity. 2022 Jul 6;8(1):23
Sprague-Dawley rats
MNNG-induced precancerous lesions of gastric carcinoma model
Oral
40 mg/kg, 80 mg/kg
Daily administration for 10 weeks
To evaluate the protective effect and mechanism of Calycosin on MNNG-induced precancerous lesions of gastric carcinoma. Results showed that Calycosin significantly ameliorated pathological changes in gastric mucosa, reduced intestinal metaplasia and dysplasia, and exerted protective effects by regulating the integrin β1/NF-κB/DARPP-32 pathway and suppressing STAT3 expression.
Drug Des Devel Ther. 2020 Jun 9;14:2207-2219
C57BL/6 mice
Renal ischemia/reperfusion injury (IRI) model
Intragastric administration
5 mg/kg, 10 mg/kg, 20 mg/kg
Once daily for 7 days
To investigate the protective effect of CAL on renal IRI and its mechanism. Results showed that CAL dose-dependently alleviated renal injury, reduced serum creatinine and blood urea nitrogen levels, decreased renal tubular damage score, inhibited NF-κB-mediated inflammatory response, and acted through the PPARγ/EGR1 pathway.
Front Pharmacol. 2022 Oct 7;13:970616.
Nude mice (BALB/c nu/nu)
U87 xenograft model
Intravenous injection
7.5 mg/kg
Every other day for 22 days
To evaluate the antitumor effect of Calycosin in vivo, results showed that Calycosin significantly reduced tumor volume and suppressed TGF-β and its downstream molecules.
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