Drug intelligence / Profile preview

reineckia-biflavone a

Development stage
Preclinical
Modality
Small Molecules
01

Overview

Reineckia-biflavone A (RFA) is a novel biflavone compound isolated from *Reineckia carnea* Kunth, a traditional medicinal herb used by the Miao nationality in southwest China. It has demonstrated potent antiproliferative activity against renal cell carcinoma (RCC) cells, specifically the 786-O cell line, with an IC50 of 19.34 μmol/L. RFA induces apoptosis through the mitochondrial pathway, characterized by the up-regulation of pro-apoptotic proteins such as Bax, Caspase-3, and Cytochrome c, and the down-regulation of the anti-apoptotic protein Bcl-2. Additionally, it triggers S-phase cell cycle arrest, increases intracellular calcium levels, and decreases mitochondrial membrane potential. Notably, it shows minimal cytotoxicity toward red blood cells and peripheral blood mononuclear cells, suggesting potential selectivity for cancer cells.

Other names
reineckia-biflavone A
02

Targets

BAX (Apoptosis regulator BAX)CASP3 (Caspase-3)CYCS (Cytochrome c)

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