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Artemisinin: Chinese medicine to the world

Recently, Warren Alpert Foundation Prize (Warren Alpert Prize Foundation) official website announced the 2015 annual Warren Alpert Award China Academy of Traditional Chinese Medicine researcher Tu Yo Yo, in recognition of its outstanding contribution in the field of malaria. Tu Yo Yo is one of the important discoverer of artemisinin antimalarial effective monomer, this outcome has saved millions of lives.

Today in Africa, artemisinin is widely used in malaria treatment, known as the "oriental magic pill", it has even been used as a "national ceremony" when Chinese leaders to visit Africa.

Along the way, artemisinin how to stand out from the thousands of traditional Chinese medicine? Behind and has a kind of twists and turns?


1, artemisinin prequel

Quinine was discovered after an early cure for malaria, but long-term use so that the malaria parasite to the former "trump card" drugs (chloroquine) produce drug resistance, malaria comeback

Malaria is an ancient disease, as early as 200 years BC, the "Yellow Emperor" will detail the symptoms of malaria, Roman is also relevant records. In the private sector, malaria is known as "cold and heat disease" or "fight malaria," alternating chills and fever attack, suffering extremely, such as into the icehouse cold, like into the hot oven. Had the disease, it is torture to the human body "cool malaria", and it is called "malaria."

For a long period of time, people are with this "chronic illness" as a protest, but never really their uniforms.

17th century, the Spaniards in South America found that local Indians used the bark of the cinchona tree ground into powder, was able to treat malaria. After this "magic pill" was brought back to Europe, the treatment of a turnaround.

In 1820, French chemist Pelletier (Pelletier) and Calvin Figure (Caventou), first purified from a cinchona bark quinine antimalarial component, commonly known as "quinine." However, cinchona bark quinine content of only about 5%, and limited sources can not meet the needs of countries in the world many malaria patients.

Thus, scientists began to explore synthetic quinine. After a long effort, to 1944, the American chemist Woodward and Delin true artificial synthesis of quinine.

However, as a cure for malaria, quinine benefit patients at the same time, there are obvious limitations. Distinguished Professor of Guangdong Pearl River scholar, Song Jianping Guangzhou University of Traditional Chinese Medicine Science and Technology Park of explanation, the early use of quinine patients will produce dizziness, tinnitus, lethargy, blood pressure and other adverse reactions, and even lead to miscarriage. For this reason, scientists quinine molecular structure of the "reform", synthesized a more efficient, low toxicity of new products chloroquine.

"Antimalarial chloroquine started well, has been used for nearly 30 years." Said Song Jianping, unfortunately, according to "survival of the fittest" law of nature, Plasmodium falciparum chloroquine drug in the long-term "contest" gradually have a great resistance to the drug lose "special effects."

From the 1960s, malignant malaria "comeback." In 1965, the outbreak of the Vietnam War, the United States, the two armies fighting hard in the tropical rainforests of Asia, such as third-party, crazy attacks warring sides malaria. There are records, the number of parties or even died due to malaria is much higher than the number of deaths in combat. Though there have been in the US Army Research Institute for the center, invested heavily in the development of new drugs, but no results. Vietnam began to help China.

2, found that artemisinin

Tu Yo Yo first to discover annua extract against murine malaria effectively achieve critical breakthroughs; Li bridge team for the first time the system proved effective artemisinin against falciparum malaria

In order to come up with the cure for malaria, in 1967, the Chinese government launched the "523 Tasks", intended to concentrate the power of the National Science and Technology jointly developed anti-malarial drugs.

"'Yi Bacao a needles', which is the image of the traditional Chinese medicine treatment methods are summarized. 'Needles' refers acupuncture, and 'grass' is the herbs." Song Jianping, said China's "523 Tasks" Collaboration in Medicine group were also carried out in two directions to explore acupuncture and traditional Chinese medicine, acupuncture and undertake malaria research, the research team is the University of Chinese Medicine, Guangzhou (Guangzhou University of Traditional predecessor) teacher Li bridge led.

End of 1968, Li came to Yunnan bridge Lianghe a malaria-prone small cottage. Stockade only 20 people, every household has a malaria patient, the entire stockade month died eight patients. During Li bridge stockade patient to carry out treatment, the epidemic still not under control.

Acupuncture can treat malaria it? Puzzling Li Guoqiao decision "to defy the law." He injected into the patient's blood, infected with falciparum malaria initiative, and used his body acupuncture experiment. Unfortunately, although the final proof that acupuncture is invalid, but the disease in the country bridge Lee insists record infection data, look for Plasmodium development law, he left a valuable experimental records, carried out after this cure malaria drug clinical trial of the foundation.

In 1969, Tu Yo Yo Institute of Chinese Medicine Research Institute and several colleagues to join him "523 Tasks" and "Chinese medicine professional group," Tu Yo Yo was appointed leader.

"Looking for antimalarials in Chinese medicine is tantamount to a haystack, because the purpose of medicine as many as thousands of well-known, but Tu Yo Yo where Medicines found the right idea." Song Jianping introduction, the Medicines first pick from the ancient medical classics appear higher frequency of anti-malarial prescriptions, while visiting folk prescription, eventually screened out of some drugs, including Artemisia annua.

But when Tu Yo Yo way to test the use of modern medicine the ability of antimalarial artesunate extract, the results are not ideal - extract of Artemisia annua, there had been 68% of the malaria parasite inhibition rate, but the effect is very unstable, there is an experiment , inhibition rate was only 12%.

Research on artemisinin Zaiyu bottlenecks. Later, according to Tu Yo Yo recalls the day in the second half of 1971, the Eastern Jin Ge Hong "elbow Emergencies · cure malaria chills and fever all parties" in a few words triggered her inspiration: "Artemisia annua a grip to two liters of water stains , twisted juice, to make service of. "

"Wringer" and Chinese medicine commonly used different torture methods, whether this active ingredient artesunate in order to avoid being destroyed at high temperatures?

Tu Yo Yo began to switch to lower boiling ether extracts of Artemisia annua, and finally extract has a 100% inhibition rate of Plasmodium from Artemisia annua in the October 4, 1971, a breakthrough Artemisia annua malaria research. Later, after Qucuqujing, on November 8, 1972 to give antimalarial monomer - artemisinin.

Subsequently, the Shandong Institute of Chinese Medicine, and other units of Yunnan Institute of Drug research results and experimental methods Tu Yo Yo, and also extracted from Artemisia annua antimalarial effective crystal.

Song Jianping explained, in botany category, the Artemisia annua and Artemisia annua are two plants belong to the Asteraceae, after naming artemisinin in Artemisia annua in fact exist. "In the field of medicine, Artemisia annua and Artemisia annua are collectively known as Artemisia annua, especially in the ancient books, 'artesunate' Is the iron Artemisia annua, Artemisia annua and other plants collectively."

"At first it did not know just annua contains artemisinin, artemisinin malaria treatment clinical trial is also in the early exploration stage." Song Jianping said, antimalarial effective crystals are extracted, responsible for "523 Tasks" clinical trials Li Guoqiao ongoing investigation Yunnan endemic areas, "he immediately launched clinical validation trials of artemisinin, made a total of 18 cases, the final for the first time the system proved effective artemisinin against falciparum malaria."

September 23, 2011, Tu Yo Yo was awarded for the discovery of artemisinin international awards - the United States, "Lasker Award." Tu Yo Yo winning after repeatedly said: "This is an honor of Chinese medicine to the world, it belongs to everyone in the research team, belonging to groups of Chinese scientists."

3, artemisinin potential

Artemisinin-based combination have been developed to the fourth generation, the future of artemisinin likely to occupy a place in the field of anti-cancer

Drug development is never once and for all things, research artemisinin and its derivatives are also undergoing a process of continuous improvement and innovation.

Song Jianping said monomer extracted from artemisinin antimalarial out so far, artemisinin-based combination of research and development has come to the fourth generation. "Since the beginning of the 1990s, Professor Li Guoqiao found, although a strong role in the killing of the malaria parasite, but the presence of artemisinin and its derivatives dihydroartemisinin and artesunate and other short half-life, poor compliance shortcomings, Specifically, is the efficacy of a short time, taking long course of treatment, the patient is difficult to adhere to. In addition, the high price of these drugs, many patients can not afford. "

Li bridge leading to China believe these shortcomings in the international promotion of artemisinin more difficult, they started to develop the new artemisinin compound.

Song Jianping introduced the first generation of the compound include dihydroartemisinin, piperaquine phosphate, primaquine and methoxy pyrimidine total four components; the second generation removed primaquine, "because it is toxic and may cause acute hemolytic anemia "; the third generation to remove the methoxy pyrimidine," taking into account its side effects is relatively large ", on the left dihydroartemisinin and piperaquine phosphate, which is more classic recipes, and won the world WHO approval.

. "Every generation in optimizing the effect is more ideal," Song Jianping, said today the fourth generation of artemisinin-based combination - Artemisinin_piperaquine hydrochlorothiazide tablets will exchange artemisinin, piperaquine phosphate into base group, "thus reducing raw material use, but still retains the original active ingredient, taking 2 times 24 hours. The drug has been made in international patent protection including the US, 38 countries, 29 countries registered trademark" ʱ??

Artemisinin has yet to stop.

In recent years, many domestic and foreign experiments confirmed that artemisinin drugs for leukemia, colon cancer, melanoma, breast cancer, ovarian cancer, prostate cancer and kidney cancer etc have significant inhibition and killing effect, have significant anti- tumor activity; and compared with other anticancer drugs, artemisinin drugs with fewer side effects.

Song Jianping said that artemisinin drugs is likely to be anti-cancer drug has clinical value, he and his research team are artemisinin mechanism of action and anti-tumor activity of the role of in-depth study.

In other areas, artemisinin-based drugs also demonstrated clinical value. Recently, according to "China Science and Technology News" reported that Shanghai Institute of Materia Medica for artemisinin-based compound to carry out a systematic study immunomodulatory activity oriented medicinal chemistry and pharmacology combining synthesized multiple series of new artemisinin derivatives objects, and ultimately determine the maleic acid Arteether amine as the treatment of systemic lupus erythematosus 1.1 class of candidate drugs. The drug has been approved by the State Food and Drug Administration, and is about to start clinical research.

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Artemisinin diplomacy

Data released by the World Health Organization, in 2013, malaria is estimated to cost 58.4 million deaths worldwide, of which 90% occurred in the African region.

Since the 1960s, China began to send medical teams to Africa to the free medical support and disease prevention. By the end of 2009, China in Africa, aided the 54 hospitals and 30 malaria prevention and treatment centers, providing approximately 200 million yuan worth of anti-malaria drugs to 35 African countries.

In order to anti-malaria project with the Chinese assistance to Africa, to accelerate the promotion of China in the international arena artemisinin, in December 2006, the bridge and Song Jianping Li led his unit to Africa Comoros, implement rapid clearance compound artemisinin malaria projects.

Anti-malarial Methods World Health Organization published in four steps: spraying pesticides; insecticide-impregnated mosquito nets; the use of artemisinin-based combination malaria positive patients; intermittent treatment of pregnant women using drugs. "But this program is not feasible in Africa, for example, in a relatively pristine forests, it is difficult for a large area spray to kill mosquitoes; many places do not have to hang nets conditions so we designed a 'universal medication' program . "Song Jianping said.

Before and more than 2.2 million people participated in the referendum artemisinin-based combination medication, over 30,000 migrants to participate in prevention medication. Song Jianping given a set of data: the Comoros in 2014 to achieve zero deaths from malaria, reduce the number of malaria incidence is 2,154 cases, compared with 2006, a decrease of 98% from malaria infection 142/1000 Population (2006) It dropped to 2.8 / 1000 population.

This is the world's first drug intervention by groups, using a Chinese innovative drugs to help African countries to control malaria rapid success stories.

August 21, 2013, Vice-President and Minister of Health, Union of the Comoros Fouad Mu Haji arrived in Guangzhou, the Comoros to help make an important contribution to clear malaria Bridge and Song Jianping Li presidential medal award, which is the first medal awarded to foreign professors.

■ References

Li Run Red, Rao Yi, Zhang Daqing. "523 Tasks" and artemisinin discovery of historical inquiry [J]. Natural Dialectics, 2013,01:107-121 + 93.

Advances Li Chao, Song Jie, high power. Artemisinin and its derivatives antitumor molecular mechanisms [J]. Chinese pharmacy, 2015,12:1726-1728.

. Wang Zhen yuan to fight malaria - from quinine to artemisinin [J] Science 24 hours, 2013,02:24-26.