Apigenin can protect cardiomyocytes

Protective Effect of Apigenin on Ischemia/Reperfusion Injury of the Isolated Rat

Apigenin can protect cardiomyocytes from I-/R-induced injury, at least partially, through the inhibition of p38 MAPKS signaling pathway.

Cardiovasc Toxicol. 2014 Nov 7. [Epub ahead of print]

Hu J(1), Li Z, Xu LT, Sun AJ, Fu XY, Zhang L, Jing LL, Lu AD, Dong YF, Jia ZP.


Berberine induces apoptosis

berberine kills cancer cells

Berberine affects human cancer cells

1. Mol Med Rep. 2014 Dec;10(6):3132-8. doi: 10.3892/mmr.2014.2608. Epub 2014 Oct 8.

Berberine sensitizes rapamycin‑mediated human hepatoma cell death in vitro.

Guo N(1), Yan A(1), Gao X(1), Chen Y(2), He X(1), Hu Z(1), Mi M(1), Tang X(3), Gou X(1). Author information:  (1)Laboratory of Cell Biology and Translational Medicine, Institute of Basic Medical Science, X'ian Medical University, Xi'an, Shaanxi 710021, P.R. China. (2)Department of Cell Biology and Genetics, College of Medicine, Xi'an Jiaotong University, Xi'an, Shaanxi 710032, P.R. China. (3)Department of Pathology, Sichuan College of Traditional Chinese Medicine, Mianyang, Sichuan 721000, P.R. China. Rapamycin is clinically used as an immunosuppressant. Increasing evidence suggests that rapamycin has an important inhibitory role in the development and progression of different types of cancer and that it is a promising candidate for cancer chemotherapy. Berberine is an isoquinoline alkaloid isolated from medicinal plant species, which has been used in traditional Chinese medicine with no significant side effects. Recent research has demonstrated that berberine has anticancer activity against various types of cancer, mediated through the suppression of mammalian target of rapamycin (mTOR). The present study aimed to investigate the in vitro synergistic anticancer effect of combined treatment of rapamycin at various concentrations (0, 10, 50, 100 and 200 nM) and berberine (62.5 µM) in SMMC7721 and HepG2 hepatocellular carcinoma (HCC) cell lines, and the potential underlying molecular mechanism. The combined use of rapamycin and berberine was found to have a synergistic cytotoxic effect, with berberine observed to maintain the cyotoxic effect of rapamycin on HCC cells at a lower rapamycin concentration. Moreover, the cells treated with the combination of the two agents exhibited significantly decreased protein levels of phosphorylated (p)‑p70S6 kinase 1 (Thr389), the downstream effector of mTOR, compared with the cells treated with rapamycin or berberine alone. Furthermore, overexpression of cluster of differentiation (CD) 147, a transmembrance glycoprotein associated with the anticancer effects of berberine, was found to upregulate p‑mTOR expression and inhibit cell death in SMMC7721 cells co‑treated with rapamycin and berberine. In conclusion, the findings of the present study suggest that the combined use of rapamycin and berberine may improve HCC therapy through synergistically inhibiting the mTOR signaling pathway, which is at least in part, mediated through CD147.

Apigenin and Breast Cancer

Several articles describing the apoptotic effects of apigenin in breast cancer cells.

1. Apigenin induced MCF-7 cell apoptosis-associated reactive oxygen species.

Apigenin is a flavonoid, which has been proved to possess effective anti-cancer bioactivities against variety of cell lines. However, little is known about its effect on the cell-surface and the interaction between cell-surface and the reacting drug. In this study, human breast cancer line (MCF-7) was selected to be as a cell model to investigate the effects of apigenin on cell growth, proliferation, apoptosis, cellular morphology, etc. MTT assay showed that the growth inhibition induced by apigenin was in a dose-dependent manner when treated with different concentrations of apigenin while had little cytotoxic effects on human normal cells (MCF-10A). Fluorescence-based flow cytometry was used to detect cellular apoptosis and ROS production. The results showed that 80 µM apigenin could effectively induce apoptosis and overproduction of ROS in MCF-7 cells. Here, atomic force microscopy (AFM) was utilized to detect the shapes and  membrane structures of MCF-7 cells at cellular or subcellular level. The results  showed that the control MCF-7 cells presented typical elongated-spindle shapes with abundant pseudopodia, while after treated with apigenin, the cells shrunk and became round, the pseudopodia diminished. Moreover, the images of ultrastructure indicated that the cell membrane was composed of nanoparticles of  49?nm, but with the treated concentrations of apigenin increasing, the sizes of membrane particles significantly increased to 400?nm. These results can improve our understanding of apigenin, which can be potentially developed as a new agent  for treatment of cancers.

Bai H, Jin H, Yang F, Zhu H, Cai J. Apigenin induced MCF-7 cell apoptosis-associated reactive oxygen species. Scanning. 2014 Oct 18. doi: 10.1002/sca.21170. [Epub ahead of print] PubMed PMID: 25327419.


Apigenin and Prostate Cancer - recently published 6 articles

Selected apigenin papers devoted to investigate its antiproliferative effect in cancer cells including prostate cancer and to analyze molecular response of the cells, published in 2014.


Apigenin induced ATF3 to decrease ER stress-induced chemokine expression by epigenetically supression of EGR1 expression

colon cancer and apigenin
New research published in the “Journal of Biological Chemistry”, showed in intestinal cancer cells, apigenin induced ATF3 upregulation and this effect diminished endoplasmic reticulum (ER) stress response via epigenetically supression of EGR1 expression.

Plant flavonoids kill different cancer types

herbs with apigenin kills cancer cells
A recent review published in the Pharmacognosy Reviews journal summarize the cancer killing effects of several  flavonoids, including  apigenin, chrysin, luteolin and many others. Here is the abstract of the article published, you can check this by clicking the link below.

Dr. Katrin Sak, recently reviewed cytotoxic effects of several plant flavonoids, including  apigenin, chrysin, luteolin and many others.


Apigenin affects human prostate cancer cells

Apigenin modulates EMT in prostate cancer cells (DU145) and this results in suppression of cell proliferation and inhibition of cell migration and invasive potential, a new study showed published Molecular Medicine Reports.

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