Arteminsinin

Application of Traditional Chinese Herbal Medicine on Zoonotic Dieseases

1. Introduction to Malaria

A mosquito-borne infectious disease
Life threatening affecting humans and other animals
Caused by Plasmodium: a group of single-celled micro organisms
Cases 214 million malaria cases reported worldwide in 2015
Incidence: 37% global decrease in malaria incidence between 2000 and 2015
Mortality: 60% decrease in global malaria mortality rates between 2000 and 2015 [1]

2. Discovery of Artemisinin(Qinghaosu) [2]

Malaria was traditionally treated by chloroquine or quinine, but with declining success.By the late 1960s, efforts to eradicate Malaria had failed and the disease was on the rise.At that time, Youyou Tu in China turned to traditional herbal medicine to tackle the challenge of developing novel Malaria therapies. From a large-scale screen of herbal remedies in Malaria-infected animals, an extract from the plant Artemisia annua emerged as an interesting candidate. However, the results were inconsistent, so Tu revisited the ancient literature and discovered clues that guided her in her quest to successfully extract the active component from Artemisia annua. Tu was the first to show that this component, later called Artemisinin, was highly effective against the Malaria parasite, both in infected animals and in humans . Artemisinin represents a new class of antimalarial agents that rapidly kill the Malaria parasites at an early stage of their development, which explains its unprecedented potency in the treatment of severe Malaria.

3. Introduction to YouYou Tu [2]

Youyou Tu was born in 1930 in China and is a Chinese citizen. She graduated from the Pharmacy Department at Beijing Medical University in 1955. From 1965-1978 she was Assistant Professor at the China Academy of Traditional Chinese Medicine, from 1979-1984 Associate Professor and from 1985 Professor at the same Institute. From 2000, Tu has been Chief Professor at the China Academy of Traditional Chinese Medicine.

4. Introduction to Artemisinin [3]

5. Derivatives of Artemisinin

Dihydroartemisinin Artemether Artesunate Carboxypropyldeoxoartemisinin Artemotil
Molecular formula C15H24O5 C16H26O5 C19H28O8 C19H30O6 C17H28O5
IUPAC naming

(3R,5aS,6R,8aS ,9R,12S,12aR)-decahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin-10-ol

(3R,5aS,6R,8aS,9R, 10S,12R,12aR)-10-methoxy-3,6,9-trimethyldecahydro-12H-3,12-epoxy[1,2]dioxepino[4,3-i]-2-benzopyran

4-Oxo-4-{[(4S,5R,8S,9R, 10S,12R,13R)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04, 13.08,13]hexadec-10-yl]oxy}butanoic acid

N/A

(5aS,6R,8aS,9R, 10S,12R,12aR)-10-ethoxy-3,6,9-trimethyldecahydro-3,12-epoxy[1,2]dioxepino[4,3-i]isochromene

Bond-angle formula
Molecular structure

6. Mechanism of Action [4,5]

  1. Excitation: catalyzed by hemoglobin or Iron(II) oxide to break peroxide bridge and form free radicals
  2. Alkylation: the free radicals react and form bonds with proteins in the plasmodium and/or disrupt the functioning of the mitochondria

7. Total Synthesis of Artemisinin

8. References

  1. "From Artemisinin to Antimalarial Drugs:A Role Model of Scientific Collaboration:An Interview with Academician CHEN Kaixian on China'™s First Nobel Prize in Sciences." Bulletin of the Chinese Academy of Sciences 4(2015):197-203.
  2. "Press Release - The Nobel Prize in Physiology or Medicine 2015." the Nobel Assembly at Karolinska Institutet, available at http://www.nobelprize.org/nobel_prizes/medicine/laureates/2015/press.pdf.
  3. "The discovery of artemisinin (qinghaosu) and gifts from Chinese medicine." Nature Medicine 17, 1217-1220 (2011) DOI:10.1038/nm.2471.
  4. "Chemical proteomics approach reveals the direct targets and the heme-dependent activation mechanism of artemisinin in Plasmodium falciparum using an activity-based artemisinin probe." Microbial Cell, Vol. 3, No. 5, pp. 230 - 231; DOI: 10.15698/mic2016.05.503.
  5. "The molecular and cellular action properties of artemisinins: what has yeast told us?" Microbial Cell, Vol. 3, No. 5, pp. 196 - 205; DOI: 10.15698/mic2016.05.498.
  6. "Total synthesis of qinghaosu. " J. Am. Chem. Soc., 1983, 105 (3), pp 624-“625; DOI: 10.1021/ja00341a054.
  7. "Studies on structure and synthesis of arteannuin and related compound. XVII. The stereocontrolled total synthesis of methyl dihydroarteannuate-the total synthesis of arteannuin." Acta Chimica Sinica, 1984, 42(9): 940-942.
  8. "Studies on structure and synthesis of arteannuin and related compound x. The stereocontrolled syntheses of arteannuin and deoxyarteannuin from arteannuic acid." Acta Chimica Sinica, 1983, 41(6): 574-576.

Afterword
This website majorly serves as a record of one of the most successfully case of solving a modern and prevaling zoonotic disease crisis with chemical methods found from Chinese herbal medicines and prescriptions. Even though much has been done to explain the traditional herbal medicines with modern science, the author of this website agrees with the statement than much of the essence and of the ancient Chinese medicine has not be exploited and put into practice. With the success of the case of the discovery of Artemisinin and thus its chemical derivatives, the author hopes to attreact the attention of modern pharmaceutical researches to the Chinese herbal medicine in the light that some more extensive research and categorization can shed some light on creating novel chemical solutions to the prevailing and persistent zoonotic diseases faced by the modern human society as dicussed in the one health initiative. The solution to the modern zoonotic diseases may exist as well in those essence of wisdom of our ancestors, right within the reach of our current understanding and science, as well as those modern biochemical solutions.
This website is for personal and educative use only. Feel free to contact our support crew at support at dispersion dot info if you have any opinion, insight, or advices on the website or the topic. Part of the material used is not owned by the creater of the website and would be removed at the request at the request of the owner.

www.000webhost.com