Natural Products that Changed Society

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Until the end of the 19th century all drugs were natural products or minerals. During
the 19th century chemists succeeded in isolating pure natural products such as quinine, morphine,
codeine and other compounds with beneficial effects. Pure compounds enabled accurate dosing to
achieve serum levels within the pharmacological window and reproducible clinical effects. During
the 20th and the 21st century synthetic compounds became the major source of drugs. In spite of the
impressive results achieved within the art of synthetic chemistry, natural products or modified natural
products still constitute almost half of drugs used for treatment of cancer and diseases like malaria,
onchocerciasis and lymphatic filariasis caused by parasites. A turning point in the fight against the
devastating burden of malaria was obtained in the 17th century by the discovery that bark from trees
belonging to the genus Cinchona could be used for treatment with varying success. However isolation
and use of the active principle, quinine, in 1820, afforded a breakthrough in the treatment. In the 20th
century the synthetic drug chloroquine severely reduced the burden of malaria. However, resistance
made this drug obsolete. Subsequently artemisinin isolated from traditional Chinese medicine turned
out to be an efficient antimalarial drug overcoming the problem of chloroquine resistance for a while.
The use of synthetic analogues such as chloroquine or semisynthetic drugs such as artemether or
artesunate further improved the possibilities for healing malaria. Onchocerciasis (river blindness)
made life in large parts of Africa and South America miserable. The discovery of the healing effects
of the macrocyclic lactone ivermectin enabled control and partly elimination of the disease by annual
mass distribution of the drug. Also in the case of ivermectin improved semisynthetic derivatives
have found their way into the clinic. Ivermectin also is an efficient drug for treatment of lymphatic
filariasis. The serendipitous discovery of the ability of the spindle toxins to control the growth
of fast proliferating cancer cells armed physicians with a new efficient tool for treatment of some
cancer diseases. These possibilities have been elaborated through preparation of semisynthetic
analogues. Today vincristine and vinblastine and semisynthetic analogues are powerful weapons
against cancer diseases.
Original languageEnglish
Pages (from-to)472
Number of pages30
Publication statusPublished - 26 Apr 2021

ID: 260551792