History - Drugs Containing Alkaloids

Drugs Containing Alkaloids

HISTORY

Evidence suggests that alkaloids have been used by humanity for thousands of years. The first civilizations to use them were probably the ancient Sumarians and Egyptians. However, it was not until the early nineteenth century that these compounds were reproducibly isolated and analysed. Advances in analytical separation techniques, such as chromatography and mass spectroscopy, led to the elucidation of the chemical structure of alkaloids. The term for these compounds is thought to have originated from the fact that the alkaloid, morphine, had similar properties to basic salts derived from the alkali ashes of plants thus, it was called a vegetable alkali or alkaloid. Since the first alkaloids were isolated, thousands more have .been identified and classified.

Prior to approximately 300 years ago, malaria was the scourge of Europe, likely having been introduced through the Middle East. Malaria is caused by protozoa of the genus Plasmodium, contained as spores in the gut of the Anopheles mosquito, which then spreads the spores to humans when it bites. As the Spanish and Portuguese explorers began to colonize South America, they discovered a cure for malaria known to the native Indians. This was the bark of the Cinchona trees. The use of Cinchona bark to treat malaria was first reported in Europe in 1633, and the first bark reached Rome about 12 years later. Teas made from the bark cured people suffering from malaria, one of the major scourges in Europe at that time, and the bark was known as Jesuit’s bark. Because of the philosophical differences between Protestants and Catholics, many Protestants refused to be treated with the bark. One of the most prominent Protestants of the time, Oliver Cromwell, reportedly died of malaria because of this stubbornness.

The French apothecary Derosne probably isolated the alkaloid afterwards known as narcotine in 1803 and the Hanoverian apothecary Serturner further investi-gated opium and isolated morphine (1806 and 1816). Morphine is the principal alkaloid and was first isolated between 1803 and 1806. It was widely used for pain relief beginning in the 1830s, but was also recognized as being addictive. Isolation of other alkaloids, particularly by Pelletier and Caventou, rapidly followed: strychnine (1817), emetine (1817), brucine (1819), piperine (1819), caffeine (1819), quinine (1820), colchicine (1820) and conine (1826). Coniine was the first alkaloid to have its structure established and to be synthesized, but for others, such as colchicine, it was well over a century before the structures were finally elucidated. In the second half of the twentieth century alkaloids featured strongly in the search for plant drugs with anticancer activity. A notable success was the introduction of catharanthus alkaloids and paclitaxel into medicine and there is much current interest in other alkaloids having anticancer properties as well as those exhibiting antiaging and antiviral possibilities.