LKL-12: An anti-cancer Drug Candidate
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In the United States there were more than 1.5 million new diagnosed cancer cases, and approximately 577,000 cancer-related deaths in the U.S. in 2012, according to the American Cancer Society. The development and discovery of newer anticancer therapeutics are still urgently needed. For the past four decades, cancer treatments have commonly been derived from natural sources. One specific example is paclitaxel which was initially isolated from the bark of the Pacific Yew tree.
Researchers at SUNY Upstate have derived a novel cancer therapeutic from the seeds of a common weed.This weed is a biennial herbal plant that has been used as an anti-viral and an anti-bacterial remedy in traditional Chinese medicine while the root of this plant has been consumed as vegetable or tea.It has already shown anti-cancer properties with the discovery of Arctigenin, an isolated component that has been demonstrated to have anti-tumor effects against pancreatic tumors in vitro. Researchers at SUNY Upstate Medical University have isolated another compound, named LKL12, which has also shown anti-cancer effects. Upstate’s team has found that LKL12 has strong anti-cancer properties.
Research at Upstate has now shown that LKL12 has strong anti-cancer properties both in vitro and in vivo. LKL12 exhibited strong growth inhibitory effects against tumor cell lines of different tissue types such as colon, breast, lung, cervix, and others. Other tumor types such as prostate cancer, leukemia, sarcoma and melanoma were inhibited after being treated with LKL12. This inhibition was caused by inducing the G1 and G2 cell cycle to arrest, thus causing cell death. Their results indicate that LKL12 modulates a number of cell cycle regulatory proteins that are essential for cell cycle progression, and it also suppresses oncoprotein expression that is linked to cellular transformation and tumor maintenance.
When tested in mice that had been xenografted with HeLa cells, LKL12 was again shown to limit tumor growth. Over a period of two weeks, LKL12 inhibited tumor growth by 54%. Also of note, there was not any observed lethality or weight loss in the mice that were given LKL12 over the course of the treatment. This indicates that LKL12 was both well tolerated and limited tumor growth in vivo.