Ergot and other indole alkaloids


Ergot and other Indole alkaloids


Many minor groups of alkaloids have an indole unit as a part of the structure. Best known of these are the ergot alkaloids, but others occur in a variety of families such as the Calycanthaceae, Rubiaceae, Asclepiadaceae, Verbenaceae, and Sterculiaceae.

Ergot alkaloids


Ergot alkaloids have an indole moiety, are derived from a hemiterpene unit, dimethylallyl diphosphate (DMAPP), and are widely used as medicinal compounds and as mycotoxins.

Ergot alkaloids are best known from the fungus Claviceps and from the higher plants Ipomoea, Rivea, and related genera of the Convolvulaceae.


Biosynthesis of ergot alkaloids


The biosynthesis of ergot alkaloids begins with prenylation of tryptamine with DMAPP. The enzyme DMAT synthetase has been purified and studied. Mixed function oxidases convert 4-dimethylallyltryptophane (DMAT) to the corresponding hydroxy derivative. Several cyclase enzymes are involved in converting the intermediates into chanoclavine I, agroclavine, elymoclavine, and finally lysergic acid. The peptide alkaloid ergotamine is synthesised by addition of amino acids (alanine, phenylalanine, and proline) to a lysergic acid precursor.

Ergotism has long been a factor in human poisoning. It was not until the 1760s that von Munchhausen recognized that this a problem produced by fungi. Humans were usually poisoned by bread prepared from infected grain. This was a major problem in Europe in the Middle Ages. Today, the problem is largely averted by better grain-handling techniques, inspection of grain, and pooling of grain supplies.

Some alkaloids possess potent vasoconstricting activity; these were largely responsible for the gangrenous conditions of extremities that often resulted in loss of limbs. Other ergot alkaloids produced delirium and hallucinations.

Ergotism is still a major livestock poisoning problem.

Endophytes


Although fungi such as Claviceps are parasitic on plants, especially cereal grains, a variety of other fungi live entirely within the host plants. These endophytes often belong to the genera Atkinsonella, Balansia, Balansiopsis, Epichloë, and Myriogenosparae. The host plants are often grasses and sedges, but endophytic relationships now appear to be much more widespread than previously thought.


Poisoning by the grasses Festuca arundinacea, Lolium perenne, and Dactylis glomeratus appears to involve endophytic fungi.


Hallucinogenic materials


Ergot alkaloids with hallucinogenic properties have been isolated from Claviceps and from several other genera of fungi. Similar compounds occur in seeds of plants of the family Convolvulaceae and were used as hallucinogenic substances by indigenous peoples of Mexico.

Lysergic acid diethylamide or LSD is a synthetic product (not naturally occurring) with powerful hallucinogenic properties.

Medicinal properties


Ergot alkaloids are adrenergic blocking agents. They inhibit lactation and prolactin release. Several, ergocryptine and ergocominem, for example, have antitumor activity. Ergotamine and ergometrine have vasoconstricting activity and are used to promote childbirth and as uterine- contracting agents following childbirth. Ergot is cultivated and harvested for medicinal uses.


Other indole alkaloids


Harmane or beta-carboline alkaloids


Although these alkaloids are not common, they are distributed in a number of plant families. The formation of this group is similar to that of isoquinoline alkaloids, except that a tryptamine unit is involved instead of a DOPA-derived unit.

Harmane or beta-carboline alkaloids have been reported from many species of the Rubiaceae. They also occur in the Acanthaceae, Apocynaceae, Eleagnaceae, Fabaceae, Loganiaceae, Malpighiaceae, Passifloraceae, Ranunculaceae, Rutaceae, Simaroubaceae, Solanaceae and Zygophyllaceae.

Harmane alkaloids inhibit membrane transport and act at serotonin receptors.

Alkaloids of this group are important as hallucinogenic substances in Peganum harmala, Zygophyllaceae, especially harmine, and as sedatives in Passiflora species

.

They are found in Eleagnus species, Eleagnaceae.


Huayusca or yagé


Plant material of Banisteriopsis caapi and related species is used to prepare hallucinogenic drinks used by Indians of the Amazonian region and in Andean South America.


Physostigmine


Physostigmine is a powerful acetylcholine esterase inhibitor found in the seeds of the fabaceous plant Physostigma venenosum. This West African plant has been used as a "trial-by-ordeal" plant in Africa, but today serves as the source of physostigmine used to treat glaucoma.


Calycanthaceae alkaloids and similar alkaloids from the Rubiaceae


A complex series of alkaloids from the family Calycanthaceae, mainly the genera Calycanthus and Chimonanthus. A series of somewhat similar alkaloids (polyindolenines) is found in certain members of the Rubiaceae. They are best known from the genera Hodgkinsonia, Borreria, and Psychotria.

Related Images

Ergot Alkaloid Biosynthesis

Lysergic Acid Derivatives

Peptide Ergot Alkaloids

Harmine and Related Alkaloids

Physostigmine Biogenesis

Psychotridine and Hodgkinsine

Borreverine and Isoborreverine

Miscellaneous Indole Alkaloids



Lecture Slides

Plants with Ergot and Other Indole Alkaloids




© David S. Seigler, Plant Biology 363, Plant Secondary Metabolism, Department of Plant Biology, 265 Morrill Hall, 505 S. Goodwin Ave., University of Illinois, Urbana, Illinois 61801, USA. 217-333-7577. seigler@life.uiuc.edu.