Dioscin is a natural steroid saponin derived from several plants, showing potent anti-cancer effect against a variety of tumor cell lines. Dioscin (1, 2 and 4 μmol/L) could significantly inhibit the viability of LNCaP cells in a time- and concentration-dependent manner[3]. Dioscin suppressed RANKL-mediated osteoclast differentiation and bone resorption in vitro in a dose-dependent manner. Dioscin abrogated AKT phosphorylation, which subsequently impaired RANKL-induced nuclear factor-kappaB (NF-κB) signaling pathway and inhibited NFATc1 transcriptional activity[4]. Oral treatment dioscin delays crystalline silica-induced pulmonary fibrosis and exerts pulmonary protective effects in mice[5]. Dioscin could promote autophagy in macrophages. Dioscin-triggered AMs autophagy limited mitochondrial reactive oxygen species (mtROS) mass stimulated by CS(crystalline silica), reduced mitochondria-dependent apoptosis pathway activation and facilitated cell survival. Dioscin treatment alleviated macrophage-derived inflammation and subsequent abnormal collagen repair[6].
Dioscin/薯蓣皂苷 细胞实验
Cell Line
Concentration
Treated Time
Description
References
U2OS and 143B cells
2.5 µM
24 hours
Dioscin induced G2/M phase arrest
Cell Death Dis. 2018 Mar 1;9(3):343.
Human periodontal ligament stem cells (hPDLSCs)
1 μg/mL and 3 μg/mL
1 day and 3 days
Dioscin promoted osteogenic differentiation of hPDLSCs under LPS-induced inflammatory conditions, increasing the expression of osteogenic markers and the formation of mineralized nodules.
Int J Biol Sci. 2024 Jan 27;20(4):1375-1388.
HT29 cells
2 µM
12 hours
Screening of a natural product library revealed that Dioscin significantly inhibited glycolysis in HT29 cells.
EBioMedicine. 2020 Jan;51:102570.
H9C2 cells
50, 100, 200 ng/mL
24 hours
To investigate the protective effect of Dioscin against DOX-induced H9C2 cell injury, the results showed that Dioscin significantly increased cell viability and improved cell morphology
Redox Biol. 2018 Jun;16:189-198.
RAW264.7 cells
37.5, 75, 150, 300, 600, 1200, 2400 ng/mL
24 hours
To evaluate the effect of Dioscin on the viability of RAW264.7 cells, results showed that Dioscin had no significant effect on cell viability within the concentration range.
Theranostics. 2017 Sep 26;7(17):4255-4275.
NIH-3T3 cells
125, 250, 500, 1000, 2000, 4000, 8000 ng/mL
24 hours
To evaluate the effect of Dioscin on the viability of NIH-3T3 cells, results showed that Dioscin had no significant effect on cell viability within the concentration range.
Theranostics. 2017 Sep 26;7(17):4255-4275.
SMMC7721 cells
1.4, 2.9, 5.8 µM
24 hours
Dioscin significantly inhibited the proliferation, migration, and invasion of SMMC7721 cells, and induced apoptosis, autophagy, and DNA damage.
Br J Pharmacol. 2019 Apr;176(7):919-937.
HepG2 cells
1.4, 2.9, 5.8 µM
24 hours
Dioscin significantly inhibited the proliferation, migration, and invasion of HepG2 cells, and induced apoptosis, autophagy, and DNA damage.
Br J Pharmacol. 2019 Apr;176(7):919-937.
SK-MES-1
0, 1.25, 2.5, 5, 10 µM
24 hours and 48 hours
Dioscin significantly inhibited the proliferation of lung SCC cells, with an IC50 value of 2.05 μM at 48 h.
Int J Biol Sci. 2020 Sep 2;16(15):2883-2894.
NCI-H520
0, 1.25, 2.5, 5, 10 µM
24 hours and 48 hours
Dioscin significantly inhibited the proliferation of lung SCC cells, with an IC50 value of 4.59 μM at 48 h.
Int J Biol Sci. 2020 Sep 2;16(15):2883-2894.
HBE
0, 1.25, 2.5, 5, 10 µM
24 hours and 48 hours
Dioscin had a weaker inhibitory effect on HBE cells, with an IC50 value of 8.47 μM at 48 h.
Int J Biol Sci. 2020 Sep 2;16(15):2883-2894.
MC3T3-E1 cells
0.25 μg/ml, 0.5 μg/ml, 1.0 μg/ml
24 hours, 48 hours, 72 hours
Dioscin significantly promoted the proliferation of MC3T3-E1 cells in a dose-dependent manner at 48 h and 72 h.
J Biomed Sci. 2014 Apr 17;21(1):30.
MG-63 cells
0.25 μg/ml, 0.5 μg/ml, 1.0 μg/ml
24 hours, 48 hours, 72 hours
Dioscin significantly promoted the proliferation of MG-63 cells in a dose-dependent manner at 48 h and 72 h.
J Biomed Sci. 2014 Apr 17;21(1):30.
NOZ cells
0, 1, 2, 4, 6, 8 µM
24hours, 48 hours, 72 hours
To evaluate the inhibitory effect of Dioscin on NOZ cell proliferation
Int J Biol Sci. 2017 Jun 1;13(6):782-793.
SGC996 cells
0, 1, 2, 4, 6, 8 µM
24hours, 48 hours, 72 hours
To evaluate the inhibitory effect of Dioscin on SGC996 cell proliferation
Int J Biol Sci. 2017 Jun 1;13(6):782-793.
293T cells
0, 1, 2, 4, 6, 8 µM
24hours, 48 hours, 72 hours
To evaluate the effect of Dioscin on 293T cells
Int J Biol Sci. 2017 Jun 1;13(6):782-793.
NIH-3T3 cells
1000, 500, 250 ng/mL
30 minutes
To evaluate the effect of Dioscin on the TGF-β/Smad3 signaling pathway in NIH-3T3 cells, results showed that Dioscin significantly inhibited the phosphorylation of Smad3.
Theranostics. 2017 Sep 26;7(17):4255-4275.
Bone marrow-derived macrophages (BMDMs)
1 μg/mL and 3 μg/mL
4 hours
Dioscin inhibited the LPS-induced elevation of Il1β, Il6, Tnfα, and Nlrp3 mRNA expression and reduced the secretion of IL-6 and TNF-α.
Int J Biol Sci. 2024 Jan 27;20(4):1375-1388.
PC9GR cells
2.1 µM
48 hours
Dioscin inhibits cell viability and induces apoptosis in PC9GR cells
Int J Biol Sci. 2018 Jan 11;14(1):47-56.
H1650 cells
1.7 µM
48 hours
Dioscin inhibits cell viability and induces apoptosis in H1650 cells
Int J Biol Sci. 2018 Jan 11;14(1):47-56.
H1975 cells
4.3 µM
48 hours
Dioscin inhibits cell viability and induces apoptosis in H1975 cells
Int J Biol Sci. 2018 Jan 11;14(1):47-56.
CL97 cells
4.1 µM
48 hours
Dioscin inhibits cell viability and induces apoptosis in CL97 cells
Int J Biol Sci. 2018 Jan 11;14(1):47-56.
U2OS and 143B cells
2.5 µM
48 hours
Dioscin significantly increased the proportion of apoptotic cells
Cell Death Dis. 2018 Mar 1;9(3):343.
RAW264.7 cells
300, 150, 75 ng/mL
6 hours
To evaluate the effect of Dioscin on the secretion of pro-inflammatory cytokines in RAW264.7 cells, results showed that Dioscin significantly inhibited the secretion of IL-1β, IL-6, TNF-α, and MCP-1.
Theranostics. 2017 Sep 26;7(17):4255-4275.
MH-S cells
200 nM, 400 nM, 800 nM
Dioscin treatment reduced CS-induced apoptosis in MH-S cells and promoted autophagy.
Theranostics. 2019 Mar 7;9(7):1878-1892.
Human Umbilical Vein Endothelial Cells (HUVECs)
1.25 mg/L and 5 mg/L
Dioscin promoted endothelial cell proliferation, migration, and tube formation under hypoxic conditions, indicating its pro-angiogenic effects.
Aging Cell. 2021 Jul;20(7):e13392.
MG-63 cells
0.25 μg/ml, 0.5 μg/ml, 1.0 μg/ml
24 h, 48 h, 72 h
Promoted MG-63 cell proliferation and differentiation, dose-dependently increased ALP activity, upregulated ER-α, ER-β, and β-catenin protein expression
J Biomed Sci. 2014 Apr 17;21(1):30.
MC3T3-E1 cells
0.25 μg/ml, 0.5 μg/ml, 1.0 μg/ml
24 h, 48 h, 72 h
Promoted MC3T3-E1 cell proliferation and differentiation, dose-dependently increased ALP activity and mineralization nodule formation, upregulated ER-α, ER-β, β-catenin, and Bcl-2 protein expression
J Biomed Sci. 2014 Apr 17;21(1):30.
Dioscin/薯蓣皂苷 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
NOZ cell xenograft model
Injection
0, 5, 10 mg/kg
Every 3 days for 25 days
To evaluate the inhibitory effect of Dioscin on NOZ cell xenograft tumors
Int J Biol Sci. 2017 Jun 1;13(6):782-793.
Nude mice
Xenograft model
Intraperitoneal injection
10 mg/kg
Every two days, until the end of the experiment
Dioscin delayed in vivo tumor growth, promoted Skp2 ubiquitination, and inhibited Skp2 expression.
EBioMedicine. 2020 Jan;51:102570.
C57BL/6J mice
Ligation-induced periodontitis model
Gingival injection
10 mg/kg
Once every other day for 2 weeks
Dioscin significantly reduced alveolar bone loss in ligation-induced periodontitis mice and suppressed the inflammatory response in periodontal tissues.
Int J Biol Sci. 2024 Jan 27;20(4):1375-1388.
Rats
Diethylnitrosamine-induced primary liver cancer model
Oral
15, 30, 60 mg/kg
Once daily for 18 weeks
Dioscin significantly inhibited diethylnitrosamine-induced primary liver cancer in rats, improved body weight changes, and restored serum levels of AFP, ALT, AST, γ-GT, ALP, and Ki67.
Br J Pharmacol. 2019 Apr;176(7):919-937.
C57BL/6 mice
Silicosis model
Oral
20, 40, 80 mg/kg
Once daily for 56 days
To evaluate the effect of Dioscin on pulmonary fibrosis in a silicosis mouse model, results showed that Dioscin significantly reduced collagen deposition and alleviated pulmonary fibrosis.
Theranostics. 2017 Sep 26;7(17):4255-4275.
C57BL/6 mice
Myocardial Infarction Model
Intragastric administration
40 µg/g
Once daily for 2 weeks
Dioscin significantly improved cardiac function in mice with myocardial infarction, reduced cardiac fibrosis and apoptosis, and alleviated cardiac damage by promoting angiogenesis.
Aging Cell. 2021 Jul;20(7):e13392.
Nude mice
Osteosarcoma xenograft model
Oral
60 mg/kg
Once daily until the end of the experiment
Dioscin significantly inhibited the growth of osteosarcoma xenografts without obvious side effects
Cell Death Dis. 2018 Mar 1;9(3):343.
BALB/c-Nude mice
NCI-H520 xenograft model
Oral
80 mg/kg/day
Once daily for 12 days
Dioscin significantly inhibited the growth of NCI-H520 xenograft tumors, with a significant reduction in tumor volume and weight, and induced tumor cell apoptosis.
Int J Biol Sci. 2020 Sep 2;16(15):2883-2894.
Rats
DOX-induced myocardial injury model
Oral
60, 30, 15 mg/kg
Once daily for seven consecutive days
To investigate the protective effect of Dioscin against DOX-induced myocardial injury, the results showed that Dioscin significantly improved ECG changes, reduced serum CK and LDH levels, and improved myocardial histopathological changes
Redox Biol. 2018 Jun;16:189-198.
Mice
DOX-induced myocardial injury model
Oral
80, 40, 20 mg/kg
Once daily for seven consecutive days
To investigate the protective effect of Dioscin against DOX-induced myocardial injury, the results showed that Dioscin significantly improved ECG changes, reduced serum CK and LDH levels, and improved myocardial histopathological changes
Redox Biol. 2018 Jun;16:189-198.
C57BL/6 mice
Silicosis model
Oral gavage
80, 40, 20 mg/kg
Once daily for 56 consecutive days
To investigate the protective effect of dioscin on pulmonary fibrosis in a silicosis mouse model. Results showed that dioscin reduced collagen deposition, decreased the secretion of pro-inflammatory and pro-fibrotic cytokines, and inhibited the TGF-β/Smad3 signaling pathway.
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