2024年9月30日星期一

Origin of Artemisinin


Origin of Artemisinin

Artemisinin, a potent antimalarial compound, has a fascinating origin that intertwines ancient traditional medicine with modern scientific discovery. The story of artemisinin begins in China, where it was first isolated from the sweet wormwood plant, Artemisia annua, a herb that has been used in traditional Chinese medicine for over 2,000 years.

The discovery of artemisinin is largely attributed to the work of Tu Youyou, a Chinese pharmaceutical chemist and malariologist. In the 1960s and early 1970s, at the height of the Vietnam War, malaria was causing significant casualties among soldiers and civilians alike. The increasing resistance of malaria parasites to existing drugs like chloroquine prompted an urgent search for new treatments.

In response to this crisis, the Chinese government launched a secret military project in 1967, known as Project 523, to find new antimalarial drugs. Tu Youyou was recruited to join this project in 1969. Her research team began by investigating traditional Chinese medicines and ancient texts for potential antimalarial compounds.

Tu's breakthrough came when she discovered a reference to sweet wormwood (Qinghao in Chinese) in a 1,600-year-old text called ”The Handbook of Prescriptions for Emergencies” by Ge Hong (284-346 CE). The text described using qinghao to treat intermittent fevers, a symptom associated with malaria. Intrigued by this ancient remedy, Tu and her team began a systematic investigation of the plant.

Initial attempts to extract the active compound from Artemisia annua using traditional hot water methods were unsuccessful. Tu then innovated the extraction process, using a lower-temperature technique to preserve the integrity of the active ingredients. This method, inspired by traditional Chinese medicine preparation techniques, proved crucial in isolating the effective compound.

In 1972, Tu's team successfully extracted a non-toxic, neutral extract from Artemisia annua that showed promising antimalarial activity in animal models. They named this compound ”qinghaosu,” which was later known internationally as artemisinin.

The discovery of artemisinin was a significant breakthrough in malaria treatment. It represented a new class of antimalarial drugs with a unique mechanism of action, rapidly killing malaria parasites at an early stage of their development in the blood. This was particularly effective against Plasmodium falciparum, the most deadly malaria parasite.

Despite the importance of this discovery, it remained largely unknown to the Western scientific community for several years due to China's isolation during that period. It wasn't until the late 1970s and early 1980s that information about artemisinin began to spread internationally.

The World Health Organization (WHO) played a crucial role in validating and promoting the use of artemisinin-based therapies. Clinical trials conducted in the 1980s and 1990s confirmed the efficacy of artemisinin and its derivatives in treating malaria, including drug-resistant strains.

The significance of Tu Youyou's work was recognized decades later when she was awarded the Nobel Prize in Physiology or Medicine in 2015, making her the first Chinese Nobel laureate in physiology or medicine and the first Chinese woman to receive a Nobel Prize in any category.

Today, artemisinin and its derivatives form the backbone of artemisinin-based combination therapies (ACTs), which are recommended by the WHO as the first-line treatment for uncomplicated Plasmodium falciparum malaria worldwide. The discovery of artemisinin not only revolutionized malaria treatment but also highlighted the potential of traditional medicine as a source for modern drug discovery.

The origin of artemisinin serves as a testament to the value of integrating traditional knowledge with modern scientific methods, and it continues to inspire research into natural products for medicinal use. 

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