22 May 2014

Lilamine is a candidate drug for the treatment of melanoma

Melanoma-destroying substance found in pine bark

Copper news based on the materials of The Pennsylvania State University: Pine bark substance could be a potent melanoma drugAmerican scientists have isolated a substance from pine bark that can become the basis for the development of a new class of drugs against melanoma.

The results of preclinical studies are published in two interrelated articles in the journal Molecular Cancer Therapeutics: Leelamine mediates cancer cell death through inhibition of intracellular cholesterol transport and Targeting Multiple Key Signaling Pathways in Melanoma using Leelamine.

Currently existing drugs for the treatment of melanoma aimed at suppressing the activity of certain proteins are effective at the very beginning of treatment, but soon the resistance of cancer cells develops, and then the disease recurs. "A malignant cell perceives chemotherapy as blocking the pathway and uses workarounds to continue to grow and develop," explained Gavin Robertson, lead researcher and head of the Milton Hershey Medical Center at Penn State University.

After studying the properties of about 480 natural compounds, he and his colleagues found that the substance leelamine, isolated from the bark of pine trees, is able to block several pathways through which a tumor cell interacts with its microenvironment at the same time.

Some natural compounds are already used in the treatment of various types of cancer. So, about 60% of the active substances of antitumor drugs are derived from plants, animals, algae or microorganisms, but, according to the authors of the study, lilamine stands out among them in a unique way of its effect on cancer cells.

As scientists have found out, this substance turns off several molecular pathways necessary for the vital activity of malignant cells at once, among them – PI3K, MAPK and STAT3, used by melanoma cells. These molecular pathways are involved in the development of more than 70% of melanomas. Lilamine blocks the cholesterol transport pathway and its movement around the cell, resulting in the death of the cancer cell. In contrast, a normal cell does not need high activity of this pathway, so lilamine does not significantly affect healthy tissues.

"Cholesterol in a malignant cell is not like blood cholesterol, which is associated with the occurrence of cardiovascular diseases," said Robertson. – Malignant cells need cholesterol vitally to transport their proteins, and these molecular pathways cannot be blocked with statins like "Lipitor", which lowers the level of cholesterol in the blood serum.

Scientists have demonstrated the effect of lilamine on melanoma cells in vitro ("in vitro") and on mice. The results of the study showed that this compound suppresses the development of this type of tumor without the occurrence of side effects. Now scientists plan to expand the scale of their research in order to conduct clinical trials of the isolated substance in the future.

Portal "Eternal youth" http://vechnayamolodost.ru22.005.2014

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