465-90-7

Usage

Uses

Used in Pharmaceutical Research:
Hellebrigenin is used as a subject of investigation in pharmaceutical research for its potential anticancer properties. Hellebrigenin is studied for its ability to induce apoptosis in cancer cells, which could contribute to the development of novel cancer therapies.
Used in Traditional Medicine:
In traditional medicine, Hellebrigenin has been used as a therapeutic agent for various medical conditions such as arthritis, gout, and edema, although its high toxicity necessitates caution and further research to ensure safe application.

Upstream product

• 20300-44-1 5β,14β-dihydroxy-19-oxo-3β-[(α-L-rhamonopyranosyl)oxy]bufa-20,22-dienolide 
• 13289-18-4 (3β,5β)-3-[(6-deoxy-4-O-β-D-glucopyranosyl-α-L-mannopyranosyl)oxy]-5,14-dihydroxy-19-oxo-bufa-20,22-dienolide 
• 186581-53-3 diazomethane 
• 105330-48-1 3-(N-suberoylargininyl)hellebrigenin 

Downstream Products

• 21887-06-9 14-hydroxy-3,19-dioxo-14β-bufa-4,20,22-trienolide 
• 1243276-09-6 UNBS₅₅₅₇ 
• 1243276-11-0 UNBS₅₅₇₆ 
• 26577-92-4 3β,14,19-trihydroxy-14β-bufa-4,20,22-trienolide 
• 26611-43-8 3α,14,19-trihydroxy-14β-bufa-4,20,22-trienolide 
• 76026-50-1 D 14447 
• 67696-82-6 acrihellin 

Relevant academic research and scientific papers

Structure-activity relationship analysis of bufadienolide-induced in vitro growth inhibitory effects on mouse and human cancer cells

The in vitro growth inhibitory effects of 27 bufadienolides and eight degradation products, with two cardenolides (ouabain and digoxin) chosen as reference compounds, were analyzed by means of an MTT colorimetric assay in six human and two mouse cancer cell lines. A structure-activity analysis was then performed to highlight the most important substituents relating to the in vitro growth inhibitory activity of bufadienolides in cancer cells. Thus, the current study revealed that various bufadienolides, including gamabufotalin rhamnoside (1a), bufotalin (2a), and hellebrin (3a), displayed higher growth inhibitory activities for various human cancer cell lines when compared to ouabain and digoxin. Gamabufotalin rhamnoside (1a) was the only compound that displayed growth inhibitory effects of +,K+-ATPase α-1 subunit. In addition, all genins and degradation products displayed weaker (if any) in vitro growth inhibitory effects on cancer cells when compared to their respective glycosylated homologue, with the exception of hellebrigenin (3b), which was as active as hellebrin (3a).

New cytotoxic bufadienolides from the roots and rhizomes of Helleborus thibetanus Franch

Three new bufadienolides 14β, 16β-dihydroxy-3β-[β-D-glucopyranosyl-(1→6)-(β-D-glucopyranosyl)oxy]-5α-bufa-20, 22-dienolide (1), 14β-hydroxy-3β-[β-D-glucopyranosyl-(1→4)-(β-D-glucopyranosyl)oxy]-5α-bufa-20, 22-dienolide (2) and hellebrigenin-3-O-β-D-glucosyl-(1→4)-β-D-glucoside (3), together with eight known bufadienolides (4–11) were isolated from the roots and rhizomes of Helleborus thibetanus. Their structures were elucidated by extensive spectroscopic methods and acid hydrolysis. Compounds 1–7 were evaluated for their cytotoxic activity against HCT116, A549 and HepG2 tumor cell lines. Compound 1 exhibited moderate cytotoxicity against HepG2 cells with IC50 value of 15.1 ± 1.72 μM. Compounds 5 and 6 exhibited moderate cytotoxicity against HCT116 cells with IC50 values of 15.12 ± 0.58 μM and 13.17 ± 2.34 μM, respectively.