This technology identifies extracts of black cohosh and their key component, actein, as potent antineoplastic agents.
Unmet Need: Naturally-derived anti-cancer therapeutic with minimal side effects
Conventional anticancer chemotherapeutics target and kill fast-growing cells but their lack of selectivity for cancerous cells results in toxicity and harsh or even deadly side effects. While the chemotherapeutic armamentarium is dominated by synthetic drugs, there is a clear need for effective natural compound-based treatments devoid of serious side effects. Medicinal plants have been used for centuries to treat neoplastic diseases, however, the active phytochemicals and their mechanism of action are often unknown or not well characterized.
The Technology: Black cohosh extracts for inhibiting the growth of breast cancer cells
This technology describes extraction protocols to isolate bioactive compounds from black cohosh (Actaea racemosa) and characterizes their effects on cancer cell growth. Actein, a triterpene glycoside, is identified as a potent cell-cycle arrest compound, displaying dose-dependent decreases in cellular proteins cyclin D1, cdk4, and the hyperphosphorylated form of pRb, with concurrent increases in the tumor suppressor gene p21. These effects are selective for human breast cancer cells versus normal mammary epithelial cells, suggesting these treatments would have few if any, side effects. Furthermore, these extracts work synergistically with a wide range of chemopreventive and chemotherapeutic agents, including taxanes, 5-fluorouracil, doxorubicin, cisplatin, and trastuzumab to provide enhanced anti-cancer efficacy.
This extracts described by this technology effectively inhibited the proliferation of breast cancer cells in several in vitro and in vivo mouse studies.
Applications:
- Anticancer therapy
- Prevention of cancer in at-risk individuals
- Treatment of gynecological symptoms, especially around menopause
- Cholesterol-lowering therapy
Advantages:
- Reduced side effects
- Synergistic effect in combination with taxanes and several other chemotherapeutics
- Readily available medicinal plant
- Simple chemical extraction enables large-scale, cost-efficient production
Lead Inventor:
I. Bernard Weinstein, M.D.
Patent Information:
Patent Status
Related Publications:
Einbond LS, Soffritti M, Esposti DD, Park T, Cruz E, Su T, Wu HA, Wang X, Zhang YJ, Ham J, Goldberg IJ, Kronenberg F, Vladimirova A. “Actein activates stress- and statin-associated responses and is bioavailable in Sprague-Dawley rats” Fundam Clin Pharmacol. 2009 Jun; 23(3): 311-321.
Einbond LS, Shimizu M, Ma H, Wu HA, Goldsberry S, Sicular S, Panjikaran M, Genovese G, Cruz E. “Actein inhibits the Na+-K+-ATPase and enhances the growth inhibitory effect of digitoxin on human breast cancer cells” Biochem Biophys Res Commun. 2008 Oct 31; 375(4): 608-613.
Einbond LS, Su T, Wu HA, Friedman R, Wang X, Ramirez A, Kronenberg F, Weinstein IB. “The growth inhibitory effect of actein on human breast cancer cells is associated with activation of stress response pathways” Int J Cancer. 2007 Nov 1; 121(9): 2073-2083.
Einbond LS, Su T, Wu HA, Friedman R, Wang X, Jiang B, Hagan T, Kennelly EJ, Kronenberg F, Weinstein IB. “Gene expression analysis of the mechanisms whereby black cohosh inhibits human breast cancer cell growth” Anticancer Res. 2007 Mar-Apr; 27(2): 697-712.
Einbond LS, Shimizu M, Nuntanakorn P, Seter C, Cheng R, Jiang B, Kronenberg F, Kennelly EJ, Weinstein IB. “Actein and a fraction of black cohosh potentiate antiproliferative effects of chemotherapy agents on human breast cancer cells” Planta Med. 2006 Oct; 72(13): 1200-1206.
Einbond LS, Shimizu M, Xiao D, Nuntanakom P, Lim JT, Suzui M, Seter C, Pertel T, Kennelly EJ, Kronenberg F, Weinstein IB. “Growth inhibitory activity of extracts and purified components of black cohosh on human breast cancer cells” Breast Cancer Res Treat. 2004 Feb; 88(3): 221-231.
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