Rhapontigenin, a natural product isolated and purified from the rhizomes of Rheum undulatum with antioxidative, antihyperlipidemic, and antifungal activities, inhibits tyrosinase activity and melanin synthesis in B16F10 melanoma cells and HIF-1α accumulation and angiogenesis in PC-3 prostate cancer cells, suppresses breast cancer cell migration and invasion, which is involved in inhibiting the PI3K-dependent Rac1 signaling pathway.
Rhapontigenin/丹叶大黄素 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HeLa cells
20 µM
24 hours
Enhanced co-localization of mitochondria with lysosomes
Nat Biomed Eng. 2022 Jan;6(1):76-93
HeLa cells
10 µM
24 hours
Induced mitophagy
Nat Biomed Eng. 2022 Jan;6(1):76-93
Human pulmonary artery endothelial cells (HPAEC)
5 µM
1-hour pretreatment
Inhibition of CYP1A1 activity attenuated MRSA-induced EC permeability and inflammatory responses
FASEB J. 2024 Nov 30;38(22):e70205
Human lung microvascular endothelial cells (HLMVEC)
5 µM
1-hour pretreatment
Inhibition of CYP1A1 activity attenuated MRSA-induced EC permeability and inflammatory responses
FASEB J. 2024 Nov 30;38(22):e70205
Mouse peritoneal macrophages
10 µM
2 hours
Rhapontigenin treatment increased the expression level of SR-A and enhanced bacterial phagocytosis in E.coli-treated mouse peritoneal macrophages.
Cell Commun Signal. 2020 May 4;18(1):70
RAW264.7 cells
10 µM
2 hours
Rhapontigenin pre-treatment reduced the expression levels of TNF-α and IL-6 in LPS-stimulated RAW264.7 cells.
Cell Commun Signal. 2020 May 4;18(1):70
HeLa cells
20, 40, 80 µM
24 hours
Reduced the expression of the mitochondrial outer membrane protein MFN2 and mitochondrial inner membrane protein Tim23
Nat Biomed Eng. 2022 Jan;6(1):76-93
Pectobacterium carotovorum subsp. carotovorum
156 µg/mL
24 hours
Assessment of Rhapontigenin's inhibitory effects on motility, EPS production, biofilm formation, and virulence exoenzyme synthesis, showing significant inhibition at 1/2 MIC concentration.
Molecules. 2022 Dec 14;27(24):8878
Chromobacterium violaceum CV026
78 µg/mL
24 hours
Evaluation of Rhapontigenin as a quorum sensing inhibitor on violacein production inhibition, showing 59.55% inhibition at 1/2 MIC concentration.
Molecules. 2022 Dec 14;27(24):8878
MDA-MB-231 cells
5-50 µM
24 hours
To evaluate the cytotoxic effects of Rhapontigenin, which showed weak effects on MDA-MB-231 cell viability
Molecules. 2018 May 18;23(5):1215
MCF-7 cells
5-50 µM
24 hours
To evaluate the cytotoxic effects of Rhapontigenin, which showed a concentration-dependent decrease in MCF-7 cell viability
Molecules. 2018 May 18;23(5):1215
SH-SY5Y cells
10 µM
3 and 6 days
To evaluate the stimulatory effect of RHA on neurite outgrowth in SH-SY5Y cells. Results showed that RHA at 10 μM significantly stimulated neurite outgrowth with a significant difference compared to the control (p < 0.001).
Antioxidants (Basel). 2023 Jun 29;12(7):1362
Human colorectal cancer cells Caco-2
25, 50, 100 µM
48 hours
To evaluate the cytotoxicity of Rhapontigenin and its analogues against colon cancer cells. Results showed that Rhapontigenin exhibited the strongest cytotoxicity at 100 µM, with a cell survival rate of 32%.
Biomolecules. 2023 Aug 20;13(8):1270
MCF-7 cells
5-50 µM
6 days
To evaluate the estrogen-like activity of Rhapontigenin, which showed a concentration-dependent increase in MCF-7 cell proliferation
Molecules. 2018 May 18;23(5):1215
Rhapontigenin/丹叶大黄素 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Caenorhabditis elegans
Transgenic nematodes with pan-neuronal expression of human Aβ1–42 (hAβ1–42)
Supplemented in the medium
0.2 mM
From egg hatching onwards
Improved learned behavioural performance
Nat Biomed Eng. 2022 Jan;6(1):76-93
C57BL/6 male mice
MRSA-induced acute lung injury model
Intraperitoneal (IP)
10 mg/kg
Single dose, 18-hour duration
Improved multiple indices of MRSA-induced ALI, including BAL protein concentration, cytokine levels, and markers of endothelial damage
FASEB J. 2024 Nov 30;38(22):e70205
C57BL/6 mice
CLP or E.coli-induced sepsis model
Intraperitoneal injection
2.5 mg/kg, 5 mg/kg and 10 mg/kg
Single injection, survival monitored for 2 days
Rhapontigenin improved the survival rate of mice in CLP or E.coli-induced sepsis, reduced the levels of inflammatory biomarkers (TNF-α, IL-6, 12(S)-HETE, ALT and AST), and enhanced bacterial clearance.
Cell Commun Signal. 2020 May 4;18(1):70
Zebrafish
Type 2 diabetes model
Intraperitoneal injection
2.5-100 mg/kg
6 days
Improved insulin resistance by regulating the PI3K/AKT/mTOR signaling pathway, reduced blood glucose, TC, TG, and LDL-C levels, and increased HDL-C levels
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