Artemisinin is selectively kill cancer cells

Researchers at the University of Washington have blended the past with the present in the fight against cancer, synthesis of a promising new compound from an ancient Chinese medicine, the cancer cells' rapacious appetite for iron, so that they target.
The substance, artemisinin, is derived from the wormwood plant and has been in China since ancient times to treat malaria. Earlier work by Henry Lai and Narendra Singh, both UW Bioengineering indicated that artemisinin alone could selectively kill cancer cells, while normal cells unharmed.

The new compound appears to improve significantly, that the deadly selectivity, according to a new study in a recent issue of the journal Life Sciences. In addition to Lai and Singh, co-authors include Tomikazu Sasaki and Archna Messay, both UW chemists.

"By itself, artemisinin is about 100 times more selective in killing cancer cells, unlike normal cells," Lai said. "In this study, the new artemisinin compound was 34,000 times more potent in killing cancer cells, unlike their normal cousins. Thus, the tagging is seems to have greatly increased the effectiveness of artemisinin to cancer-killing properties."

The substance was being developed under license to Chongqing Holley Holdings and Holley Pharmaceuticals, its U.S. subsidiary, for possible use in humans. Although the compound is promising, say the officials, possible use for humans is still years away.

In the study, the researchers exposed human leukemia cells and white blood cells to the substance. While the leukemia cells quickly died, the white blood cells remained essentially unharmed.

The trick to the compound of effectiveness, according to Lai seems, in the use of the function, such as cancer cells.

Because they multiply so quickly that most cancer cells need more iron than normal cells, DNA replication. To facilitate that, cancer cells have inlets on their surface, also known as transferrin receptors, in which more than other cells. These receptors allow quick transport into the cell of transferrin, an iron-protein found in the blood.

In preparing the compound, researchers bound artemisinin to transferrin at the molecular level. The combination of the two components is a fool the cancer cell.

"We call it a Trojan horse because the cancer cell recognizes transferrin as a natural, harmless protein," Lai said. "So the cell is the connection, not knowing that a bomb - artemisinin hidden - on the inside."

Once inside the cell, the artemisinin reacts with the iron, spawning highly reactive chemicals called "free radicals". The attack of free radicals and other molecules in the cell membrane, breaking it apart and killing the cell.

According to Lai, that process is what initially piqued his interest in artemisinin over 10 years. The wormwood extract was lost centuries ago in China, but the treatment was over time. In the 1970s it was again as part of an ancient manuscript that medical measures, including a recipe, a wormwood extract. The medical community soon discovered that the extract, artemisinin, good against malaria, and it is currently allocated to this purpose in all of Asia and Africa.

Artemisinin against malaria because the malaria parasite collects high iron concentrations, as they metabolized hemoglobin in the blood. As science began to understand how artemisinin worked, Lai said he began to wonder if the process had implications for cancer treatment.

"I think that maybe we can use this knowledge to selectively target cancer cells," he said. "So far, the outlook seems to be good.

What is Artemisinin

Artemisinin is a secondary plant substance, Chemically sesquiterpene that occurs in the leaves and flowers of the sweet wormwood (Artemisia annua). Characteristics of Artemisininstruktur are a Trioxanringsystem and Peroxidbrücke. It is used in Vietnam, China and Africa used to treat infections with multidrug-resistant strains of Plasmodium falciparum, the causative agent of malaria tropica. In June 2009, however, were known from Cambodia, the first resistances.

Artemisinin extraction

The extraction is carried through the extraction of dried leaves and flowers with hexane, which is the active ingredient, which is predominantly localized in the ethereal Öldrüsenschuppen, readily soluble. On an area of one hectare can be harvested up to two tons of sheet material to provide two to three kilograms of the extract. The Artemisiningehalt in the plant is between 0.1 and 0.4% dry weight. Engineered with an active substance content of up to 1.4% are known. From the concentrated crude extract, a yellow, viscous oil, artemisinin is obtained by recrystallization, but this method is relatively expensive and, consequently, the price of artemisinin is very high.
Experimentally, more recently, the biosynthesis in genetically modified E. coli bacteria and Saccharomyces cerevisiae explored. The first successes on the way to artificial substitutes already exist. [3] Jay Keasling it is supported by the Bill and Melinda Gates Foundation, with 43 million U.S. dollars supports the work of

Mode of action of artemisinin

Artemisinin has a Peroxidstruktur, which is unstable in the presence of high concentrations of iron ions to form free radicals. Such high concentrations are found in erythrocytes, but also in Plasmodia accumulate iron. Where to artemisinin in Plasmodium-infected red blood cells are formed free radicals, and the parasite may thus killed. In the meantime, however, summarize the evidence contribute to artemisinin derivatives, more specifically, for example by pfATP6 an inhibit Ca-ATPase. A molecule-specific effects would also be better explained as a purely chemical and physical effect of the sporadic occurrence of resistance. Due to the tremendous versatility of the malaria parasite resistance to artemisinin also seem to be formed.

Mugwort artemisinin against malaria

But when the 70-ies of the last century at the archaeological dig up a sagebrush recipe for malaria was discovered, people began to once again deal with the herb. The various drugs such as artemether, artemether and artesunate were isolated. Artesunate is water soluble, highly effective and has a short half-life. Artemether is oil-and water-soluble and can therefore cross the blood brain barrier. At the same time, it has a longer half-life, which means that it is also toxic. Artesiminin lies in the intervening half-life and can also cross the blood brain barrier. Therefore, it is one of the few resources that will be used since the Vietnam War against acute malaria, and also by the World Health Organization are recognized.

Artemisinin efficacy against malaria

Artemisinin reacts with the high iron concentrations in the malaria-causing agents. When artemisinin comes into contact with iron, a chemical reaction is triggered. It produces charged atoms, which we know as free radicals. In malaria treatment, free radicals attack the cell membranes of the malaria parasite, and they're leaving. So they kill the parasites.

Artemisinin is an alternative herbal treatment of cancer

In general, most herbal cancer therapies, although how effective they could not be recongized with conventional Western medicine. But unlike most of the alleged anti-cancer herbs, artemisinin's anti-cancer property was not found on traditional healers, but by the Medical Research is working on a prestigious university. Research professor Henry Lai, Ph.D., and Narendra Singh, MBBS, at the University of Washington in Seattle, the lead researcher in the study of anti-cancer properties are of artemisinin. Their work has an exciting new direction in the field of anti-cancer treatment, spurted, and an enormous amount of research is still business.
 Studies show that artemisinin has destructive activity against 55 cancer cell lines. Above all, artemisinin has shown that effective against cancer cells of leukemia, colon, lung, breast, fibrosarcoma. It was also shown that artemisinin killed even cancer, were traditionally resistant to chemotherapy.

Cancer in Germany:

Each year, 436,000 people in Germany to new cancer, 211,500 people die every year of it. Experts estimate that the number of cancer cases will increase by the year 2030 by 50 percent. The reason: People are living longer and cancer is a disease which affects particularly the elderly.

Most common cancers in men:

With approximately 58,570 new cases of prostate cancer in Germany is now the most common cancer in men is main reason for the growing proportion of older men. The median age at diagnosis is 69 years. Are in second place with 37,250 new cases of colorectal cancer in men. Lung cancer in men with documented diseases 32,850 per year number three.

Most cancers of the woman:

Most common cancer of women is breast cancer. Every year 57,230 women in Germany in this new disease. The median age at diagnosis is 63 years. 40 percent of affected women are younger than 60 years. Are in second place among women with 36,000 new cases of colon cancer. Even among women with 13,190 lung cancer is now in third place. The cause of smoking: More and more women!

Childhood cancer

In Germany are diagnosed each year approximately 1,800 children and adolescents under 15 years of new cancer. This number is constant for many years. The chances of recovery are now at 80 percent. Malignant neoplasms in children still remains the second leading cause of death. The most common childhood cancers are leukemias) (blood cancer, tumors of the brain and spinal cord and lymph node cancer.

Cancer Facts Worldwide

Each year, more than 11 million people worldwide new cancer. 7.9 million die of it. Thus, cancer is globally the second leading cause of death. Experts estimate that in 2030 16 million people fall ill each year from cancer. The main reason: There are more older people.

The most common cancers (the sequence follows the death rate):
Women are affected most frequently in breast, lung, stomach and colon cancer. In men, occurs most frequently the lungs, stomach, liver, colon, esophagus and prostate cancer on.

The most common cancer killers are lung, stomach, liver, colon and breast cancer. Approximately 72 percent of people who died from cancer in 2007, lived in countries with low or moderate incomes.
Tobacco smoke is the biggest risk factor that leads to cancer.

Artemisinin References

Ahmad, H., Singh, SV, Awasthi, YC: Inhibition of bovine lens glutathione S-transferases by hematin, bilirubin, and bromosulfophthalein. Lens Eye Toxic Res 8, 431-440, 1991
Lai, H., Singh, N.: "Artemisinin and Cancer", Cancer Letters, 91:41-46, 1995
Lai H., Singh, N.: "Artemisinin and Cancer," International Journal of Oncology 18:767-772, 2001 by Efferth et.al. and Life Sciences, Nov 2002
Bharel S, Gulati M, Abdin P, Srivastava S. Structure biosynthesis and functions of artemisinin. Fitoterapia Vol LXVII No. 5, l996.
Klayman D. Qinghaosu (Artemisinin): Antimalarial Drug from China. Science, 1985, Vol 238, May 31, p.1049

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