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ANTHONY MELVIN CRASTO   1




ARTEMISININ
DR ANTHONY MELVIN CRASTO
PRINCIPAL SCIENTIST
INDIA




                      EMAIL -- amcrasto@gmail.com

        http://www.slidestaxx.com/anthony-melvin-crasto-phd



    A SHORT PICTORIAL PRESENTATION-- JAN 212
2



    amcrasto@gmail.
    com




                      ANTHONY MELVIN CRASTO
Cheaper malaria drug on the horizon, say German researchers; 200 million
    malaria sufferers worldwide
    Malaria sufferers in the developing world cannot afford medicine

       German researchers announced Tuesday they had discovered a process to
       make the most effective anti-malaria drug cheaper and easier to produce in
       large life-saving quantities.
       The breakthrough offers hope to the more than 200 million malaria sufferers
       worldwide, especially in poor countries, by making artemisinin more
       affordable, the Max Planck Society said.
       "There is an effective treatment against malaria but it is not accessible to all of
       the more than 200 million people worldwide who are affected by the disease,"
       it said in a written statement.
       "Millions, especially in the developing world, cannot afford the combination
       drug preparation, which consists mainly of artemisinin," it added.
       In addition, it said the medication's price varied because of the seasonal nature
       of the basic ingredient which mainly grows in China and Vietnam.




3                                        ANTHONY MELVIN CRASTO
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    Malaria is a vector borne parasitic disease caused by the genus Plasmodium,
    affecting over 100 countries of the tropical and subtropical regions of the world.
    Four different Plasmodium species infect humans and cause distinct disease
    patterns:
    P. falciparum (malaria tropica),
    P. vivax (malaria tertiana),
    P. malariae (malaria tertiana) and
    P. ovale (malaria quartana)
    P. falciparum and P. vivax account for 95% of malaria infections. Of these two
    parasites,P. falciparum is the most deadly one, causing cerebral malaria which, if
    remain untreated, leads to coma and ultimately death of the patient. 40% of the
    world populations live in areas with the risk of malaria.
    Around 300-500 million clinical cases of malaria are reported every year, of which
    more than a million die of severe and complicated cases of malaria. Malaria is
    known to kill one child every 30 sec, 3000 children per day under the age of 5 years.
                                     ANTHONY MELVIN CRASTO
5
    Artemisinin




    IUPAC Name
    3,12-Epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin-10(3H)-one, octahydro-3,6,9-trimethyl-, (3R,5aS,6R,8aS,9R,12S,12aR)-

    Other Names
    (+)-Arteannuin; (+)-Artemisinin; (+)-Qinghaosu; Arteannuin; Artemef; Artemisine; Artemisinin; Artemisinine; Huanghuahaosu; NSC 369397;
    QHS; Qing Hau Sau; Qing Hau Su; Qinghaosu; Qinghosu

    CAS Number 693968-64-9

    Physical Data
    Density:        1.24 g/ml
    Melt. point: 152 - 157 C




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     Because artemisinin itself has physical properties
     such as poor bioavailability that limit its
     effectiveness, semisynthetic derivatives of
     artemisinin have been developed. These include:
     Artesunate (water-soluble: for oral, rectal,
     intramuscular, or intravenous use)
     Artemether (lipid-soluble: for oral, rectal or
     intramuscular use)
     Dihydroartemisinin
     Artelinic acid
     Artenimol
                           ANTHONY MELVIN CRASTO
     Artemotil
Total synthesis
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                   ANTHONY MELVIN CRASTO
synthesis
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                 ANTHONY MELVIN CRASTO
The biosynthesis of artemisinin
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synthesis
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     ANTHONY MELVIN CRASTO
Artemisinin: An Ancient Remedy for Modern Malaria
  Sometimes old remedies can be the best, particularly when they've been around
  for a couple thousand years. Take sweet wormwood, for example.
26Archaeological findings indicate that the Chinese were using wormwood to treat
  malaria more than 2,000 years ago. The weed—Artemisia annua or qing ho in
  Chinese—is even mentioned in the Recipes for 52 Kinds of Diseases, an early
  medical text found in a tomb dating from 168 BC. But its curative powers were
  not put to a rigorous test until 1967, when the government of the People's
  Republic of China began to examine systematically indigenous plants used in
  traditional remedies as potential sources of drugs.




                                    ANTHONY MELVIN CRASTO
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     It is a drug that has its roots in ancient Chinese medicine. In the fight against
     malaria, a disease that over 200 million people are estimated to have caught in
     2010, some 655,000 of whom died of it, protecting the effectiveness of
     artemisinin-based drugs has become vitally important.
     A number of Indian pharmaceutical companies have been among those
     manufacturing and marketing drugs that are likely to foster resistance to
     artemisinin in the malaria parasite, according to the latest World Malaria Report
     that was recently released.
     However, India's Drugs Controller General initiated action earlier this year to stop
     the production and export of these drugs.
     Artemisin and its derivatives have saved countless lives after the single-celled
     parasite, Plasmodium falciparum, that causes the most dangerous forms of the
     disease became resistant to the drug chloroquine. However, strains that are
     resistant to even artemisinin have emerged in parts of South-East Asia and could
     potentially spread, as has happened with earlier antimalarial drugs.

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     ANTHONY MELVIN CRASTO
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                             References
                             1. A. Butler and T. Hensman, Educ. Chem.,
                             2000, 37(6), 151.
                             2. R. K. Haynes et al, Angew. Chem. Int. Edn,
                             2004, 43, 1381.
                             3. J. L. Vennerstrom et al, Nature (London),
                             2004, 430, 900.
                             4. G. D. Brown, G.-Y. Liang and L.-K.
     ANTHONY MELVIN CRASTO   Sy, Phytochemistry, 2003, 64, 303.
                             5. R. Jambou et al, Lancet, 2005, 366, 1960.
40




     ANTHONY MELVIN CRASTO
http://www.amazon.com/Artemisinin-Artesunate-Artemisinic-Derivatives-Artemisia/dp/0978747399


41




                                            ANTHONY MELVIN CRASTO
Pictures speak
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                  ANTHONY MELVIN CRASTO
End
43


     THANKYOU

     EMAIL amcrasto@gmail.com
     An academic presentation and will not
     be used for any commercial purpose.
     My small effort to initiate interest for
     antimalarials
      DR ANTHONY MELVIN CRASTO, HELPING MILLIONS WITH WEBSITES

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Anthony Melvin Crasto presents Artemisinin

  • 1. ANTHONY MELVIN CRASTO 1 ARTEMISININ DR ANTHONY MELVIN CRASTO PRINCIPAL SCIENTIST INDIA EMAIL -- amcrasto@gmail.com http://www.slidestaxx.com/anthony-melvin-crasto-phd A SHORT PICTORIAL PRESENTATION-- JAN 212
  • 2. 2 amcrasto@gmail. com ANTHONY MELVIN CRASTO
  • 3. Cheaper malaria drug on the horizon, say German researchers; 200 million malaria sufferers worldwide Malaria sufferers in the developing world cannot afford medicine German researchers announced Tuesday they had discovered a process to make the most effective anti-malaria drug cheaper and easier to produce in large life-saving quantities. The breakthrough offers hope to the more than 200 million malaria sufferers worldwide, especially in poor countries, by making artemisinin more affordable, the Max Planck Society said. "There is an effective treatment against malaria but it is not accessible to all of the more than 200 million people worldwide who are affected by the disease," it said in a written statement. "Millions, especially in the developing world, cannot afford the combination drug preparation, which consists mainly of artemisinin," it added. In addition, it said the medication's price varied because of the seasonal nature of the basic ingredient which mainly grows in China and Vietnam. 3 ANTHONY MELVIN CRASTO
  • 4. 4 Malaria is a vector borne parasitic disease caused by the genus Plasmodium, affecting over 100 countries of the tropical and subtropical regions of the world. Four different Plasmodium species infect humans and cause distinct disease patterns: P. falciparum (malaria tropica), P. vivax (malaria tertiana), P. malariae (malaria tertiana) and P. ovale (malaria quartana) P. falciparum and P. vivax account for 95% of malaria infections. Of these two parasites,P. falciparum is the most deadly one, causing cerebral malaria which, if remain untreated, leads to coma and ultimately death of the patient. 40% of the world populations live in areas with the risk of malaria. Around 300-500 million clinical cases of malaria are reported every year, of which more than a million die of severe and complicated cases of malaria. Malaria is known to kill one child every 30 sec, 3000 children per day under the age of 5 years. ANTHONY MELVIN CRASTO
  • 5. 5 Artemisinin IUPAC Name 3,12-Epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin-10(3H)-one, octahydro-3,6,9-trimethyl-, (3R,5aS,6R,8aS,9R,12S,12aR)- Other Names (+)-Arteannuin; (+)-Artemisinin; (+)-Qinghaosu; Arteannuin; Artemef; Artemisine; Artemisinin; Artemisinine; Huanghuahaosu; NSC 369397; QHS; Qing Hau Sau; Qing Hau Su; Qinghaosu; Qinghosu CAS Number 693968-64-9 Physical Data Density: 1.24 g/ml Melt. point: 152 - 157 C ANTHONY MELVIN CRASTO
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  • 10. 10 Because artemisinin itself has physical properties such as poor bioavailability that limit its effectiveness, semisynthetic derivatives of artemisinin have been developed. These include: Artesunate (water-soluble: for oral, rectal, intramuscular, or intravenous use) Artemether (lipid-soluble: for oral, rectal or intramuscular use) Dihydroartemisinin Artelinic acid Artenimol ANTHONY MELVIN CRASTO Artemotil
  • 11. Total synthesis 11 ANTHONY MELVIN CRASTO
  • 12. synthesis 12 ANTHONY MELVIN CRASTO
  • 13. The biosynthesis of artemisinin 13 ANTHONY MELVIN CRASTO
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  • 23. synthesis 23 ANTHONY MELVIN CRASTO
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  • 26. Artemisinin: An Ancient Remedy for Modern Malaria Sometimes old remedies can be the best, particularly when they've been around for a couple thousand years. Take sweet wormwood, for example. 26Archaeological findings indicate that the Chinese were using wormwood to treat malaria more than 2,000 years ago. The weed—Artemisia annua or qing ho in Chinese—is even mentioned in the Recipes for 52 Kinds of Diseases, an early medical text found in a tomb dating from 168 BC. But its curative powers were not put to a rigorous test until 1967, when the government of the People's Republic of China began to examine systematically indigenous plants used in traditional remedies as potential sources of drugs. ANTHONY MELVIN CRASTO
  • 27. 27 It is a drug that has its roots in ancient Chinese medicine. In the fight against malaria, a disease that over 200 million people are estimated to have caught in 2010, some 655,000 of whom died of it, protecting the effectiveness of artemisinin-based drugs has become vitally important. A number of Indian pharmaceutical companies have been among those manufacturing and marketing drugs that are likely to foster resistance to artemisinin in the malaria parasite, according to the latest World Malaria Report that was recently released. However, India's Drugs Controller General initiated action earlier this year to stop the production and export of these drugs. Artemisin and its derivatives have saved countless lives after the single-celled parasite, Plasmodium falciparum, that causes the most dangerous forms of the disease became resistant to the drug chloroquine. However, strains that are resistant to even artemisinin have emerged in parts of South-East Asia and could potentially spread, as has happened with earlier antimalarial drugs. ANTHONY MELVIN CRASTO
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  • 38. 38 ANTHONY MELVIN CRASTO
  • 39. 39 References 1. A. Butler and T. Hensman, Educ. Chem., 2000, 37(6), 151. 2. R. K. Haynes et al, Angew. Chem. Int. Edn, 2004, 43, 1381. 3. J. L. Vennerstrom et al, Nature (London), 2004, 430, 900. 4. G. D. Brown, G.-Y. Liang and L.-K. ANTHONY MELVIN CRASTO Sy, Phytochemistry, 2003, 64, 303. 5. R. Jambou et al, Lancet, 2005, 366, 1960.
  • 40. 40 ANTHONY MELVIN CRASTO
  • 42. Pictures speak 42 ANTHONY MELVIN CRASTO
  • 43. End 43 THANKYOU EMAIL amcrasto@gmail.com An academic presentation and will not be used for any commercial purpose. My small effort to initiate interest for antimalarials DR ANTHONY MELVIN CRASTO, HELPING MILLIONS WITH WEBSITES