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The Road to EleusisAlbert HofmannA Challenging Question and My AnswerIn July 1975 I was visiting my friend Gordon Wasson in his home in Danbury when he suddenly asked me this question: whether Early Man in ancient Greece could have hit on a method to isolate an hallucinogen from ergot that would have given him an experience comparable to LSD or psilocybin. I replied that this might well have been the case and I promised to send him, after further reflection, an exposition of our present knowledge on the subject, which I already suspected would support my tentative position. Two years have passed, and here now is my answer. Ergot is the English name for a fungal growth, the "sclerotium" of a mushroom known to mycologists as Claviceps purpurea (Fr.) Tul. It is a parasite on rye and other cereals such as barley or wheat, and also on certain wild grasses. Other species of the genus Claviceps, viz C. paspali Stev. and Hall, C. nigricans Tul., and C. glabra Langdon, etc., are parasitical to many species and varieties of grasses. Ergot itself is not of uniform chemical composition: it occurs in "biological" or "chemical" races, differing from each other mainly by the composition of their alkaloidal constituents. (Chemists define "alkaloids" as nitrogen-containing alkaline substances that represent the pharmacologically active principles of many plants.) Thus in Switzerland there exist three varieties of ergot of rye: (a) in the Midlands a race containing mainly the alkaloid ergotamine, (b) in the Valais one with alkaloids of the ergotoxine group, and (c) in the Grisons a variety with no alkaloids at all. Furthermore in other kinds of ergot—growing on wheat, on barley, on millet, on lolium, etc.—there are wide variations in alkaloidal makeup, sometimes depending on geographical location. By far the most important of all kinds of ergot is ergot of rye, purple-brown protrusions from the ears of rye. Ergot of rye (in scientific nomenclature: Secale cornutum) has been called in England "horned rye", "spiked rye", "spurred rye", but most commonly "ergot of rye", a translation of the French ergot de seigle. The word ergot is defined in the Petit Larousse as "petit ongle pointu derriere le pied du coq", "small pointed talon behind the cock's foot", but the derivation of the French word ergot is uncertain. Other French names are blé cornu, seigle ergoté, seigle ivre. In German there seem to be more variants than in other languages: Mutterkorn, Rockenmutter, Afterkorn, Todtenkorn, Tollkorn, and many others. In German folklore there was a belief that, when the corn waved in the wind, the corn mother (a demon) was passing through the field; her children were the rye wolves (ergot). In our context we observe that of these names, two, seigle ivre ("drunken rye") and Tollkorn ("mad grain"), point to a knowledge of the psychotropic effects of ergot. This folk awareness of the mindchanging effects of ergot shows an intimate knowledge of its properties, at least among herbalists, deeply rooted in European traditions. Ergot of rye has a storied past. Once a dreaded poison, it has become a rich treasure chamber of valuable pharmaceuticals. In the Middle Ages bizarre epidemics occurred in Europe costing thousands of people their lives, occasioned by bread made from rye contaminated with ergot. These epidemics took two forms, Ergotismus convulsivus, characterized by nervous convulsive and epileptiform symptoms, and Ergotismus gangraenosus, in which gangrenous manifestations leading to mummification of the extremities were a prominent feature. Ergotism was also known as ignis sacer ("holy fire"), or "St. Anthony's fire", because St. Anthony was the patron saint of a religious order founded to care for the victims of ergotism. The cause of these epidemics —bread contaminated with ergot—was not learned until the seventeenth century, and since then there have been only sporadic outbreaks of ergot poisoning. Ergot was first mentioned as a remedy by the German physician Adam Lonitzer in 1582. He said it was being used by midwives to precipitate childbirth. The first scientific report on the use of ergot as a uterotonic agent was presented by the American physician John Stearns in 1808: "Account of the pulvis parturiens". But already in 1824 Dr. David Hosack, also American, recognizing the dangers of using ergot for accelerating childbirth, recommended that the drug be used only to control postpartum haemorrhage. Since then ergot has been used in obstetrics mainly for this purpose.(1) (This Dr. Hosack was a distinguished man. He was a physician to many of the eminent New Yorkers of his time, and he accompanied Alexander Hamilton to Weehawken heights for his fatal duel with Aaron Burr. This I learned from the admirable life of Hosack by Christine Robbins.) The latest and most important chapter in the history of ergot deals with it as a rich source of pharmacologically useful alkaloids.(2) More than thirty alkaloids have been isolated from ergot and it is unlikely that many new ones will be discovered. Hundreds of chemical modifications of these natural alkaloids have been prepared and investigated pharmacologically. Today all these alkaloids are also available by total synthesis. Medicinally the most useful alkaloids stem from ergot of rye. The first ergot alkaloid that found widespread therapeutic use was ergotamine, isolated by A. Stoll in 1918. It is the essential component of pharmaceutical preparations such as "Cafergot" and "Bellergal", medicaments against migraine and nervous disorders. Modern valuable ergot preparations are "Hydergine" developed by A. Stoll and A. Hofmann in the Sandoz laboratories in Basel, containing hydrogenated ergotoxine alkaloids, used in the treatment of geriatric disorders, and "Dihydergot" with dihydroergotamine as active component, for the therapy of circulatory disturbances. Of special relevance to our problem here are the investigations into the alkaloid ergonovine, which is the specific uterotonic water-soluble principle of ergot. In 1932 H. W. Dudley and C. Moir in England discovered that water-soluble extracts of ergot, containing none of the water-insoluble alkaloids of the ergotamine-ergotoxine-type, elicited strong uterotonic activity. This observation led three years later to the isolation of the alkaloid responsible for this action simultaneously in four separate laboratories, which named it "ergometrine", "ergobasin", "ergotocine," "ergostetrine", respectively. The International Pharmacopoeia Commission proposed a name to be internationally accepted to replace these synonyms, viz. "ergonovine". In 1937, starting with naturally occurring lysergic acid, I prepared ergonovine, which by its chemical composition is lysergic acid propanolamide. Lysergic acid is the nucleus common to most ergot alkaloids. It is extracted from special cultures of ergot and could also be prepared today by total synthesis if this procedure were not too expensive. I used the method developed for the synthesis of ergonovine for the preparation of many chemical modifications of ergonovine. One of these partly synthetic derivatives of ergonovine was lysergic acid butanolamide. This is used today in obstetrics, replacing to a major extent ergonovine, under the brand name "Methergine" to stop postpartum haemorrhage. Another lysergic acid derivative that I synthesized in this context aiming to get an analeptic (that is, an agent with circulation-and respiration-stimulating properties) was lysergic acid diethylamide. Pharmacological examination revealed a fairly strong uterotonic activity in this compound, nearly as strong as ergonovine. In 1943 I discovered in self-experiments the specific high hallucinogenic potency of lysergic acid diethylamide, which became known world-wide under the laboratory code name LSD-25. My interest in hallucinogenic agents, originating in 1943 from my work with LSD, brought me into personal contact with Gordon Wasson, pioneer ethnomycologist and also pioneer in the investigation of the ancient Mexican mushroom cult. From Roger Heim, then head of the Laboratoire de Cryptogamie and Director of the famous Museum National d'Histoire Naturelle of Paris, whom Wasson invited to study and identify in the field his sacred mushrooms, I received samples of them for chemical analysis. With my laboratory assistant Hans Tscherter I succeeded in isolating the hallucinogenic principles of the sacred Mexican mushrooms, which I named psilocybin and psilocin. With my colleagues of the Sandoz Research Laboratories, we succeeded in the elucidation of the chemical structure and the synthesis of psilocybin and psilocin. Inspired by my talks with my friend Wasson and encouraged by our success with the hallucinogenic mushrooms, I decided to tackle also the problem of another psychotropic Mexican plant, ololiuhqui. With Wasson's help I obtained a large quantity of authentic ololiuhqui seeds of the two morning glories that the Mesoamerican Indians were using, seeds of Turbina corymbosa (L.) Raf. and Ipomoea violacea L. When we analyzed them we arrived at an unexpected result: these ancient drugs that we are apt to call "magical" and the Indians consider divine, contained as their psychoactive principles some of our already familiar ergot alkaloids. The main components were lysergic acid amide and lysergic acid hydroxyethylamide, both water-soluble alkaloids, closely related to lysergic acid diethylamide (LSD), as is evident even to the non-chemist. Another constituent of the ololiuhqui alkaloids was ergonovine, the uterotonic principle of ergot. The psychoactive property of these simple lysergic acid amides, closely related to LSD, is well established. The question presented itself whether ergonovine, being not only an alkaloidal component of ergot but also of ololiuhqui, possessed hallucinogenic activity. In the light of its chemical structure this did not seem unlikely: it does not differ much from LSD. But one may ask why, if it is hallucinogenic, this astonishing fact has not been announced, in the light of its use over recent decades in obstetrics. Undoubtedly the answer lies in the extremely low dosage of ergonovine used to stop postpartum bleeding, viz 0.1 to 0.25 mg. The effective dose of lysergic acid amide is 1 to 2 mg by oral application. I decided therefore to test in a self-experiment a corresponding dose of ergonovine: 1 April 1976 12.20 h: 2.0 mg ergonovine hydrogenmaleinate, containing 1.5 mg ergonovine base, ingested in a glass of water. 13.00 h: slight nausea, same effect as I have experienced always in my LSD or psilocybin experiments. Tired, need to lie down. With eyes closed colored figures. 13.30 h: the trees in the nearby forest seem to live, their branches moving in a threatening way. 14.30 h: strong desire to dream, unable to do systematic work, with eyes closed or open afflicted by mollusk-like forms and feelings. 16.00 h: motives and colors have become clearer, but bearing still some hidden dangers. 17.00 h: after a short sleep I awoke by a kind of inner explosion of all the senses. 18.00 h: an unexpected visit forced me to become active, but during the whole evening I lived more in an inner than in the outer world. 22.00 h: all effects worn off, normal feeling. This was an experiment performed without attention to "set and setting" but it proves that ergonovine possesses a psychotropic, mood-changing, slightly hallucinogenic activity when taken in the same amount as is an effective dose of lysergic acid amide, the main constituent of ololiuhqui. Its potency is about one-twentieth of the potency of LSD and about five times that of psilocybin. There is a further finding that may prove to be of utmost importance in considering Wasson's question. The main constituents of the Mexican morning-glory seeds are (a) lysergic acid amide (= "ergine"), and (b) lysergic acid hydroxyethylamide, and these are also the main alkaloids in ergot growing on the wild grass Paspalum distichum L. This grass grows commonly all around the Mediterranean basin and is often infected with Claviceps paspali. F. Arcamone et al (3) were the first to discover these alkaloids in ergot of P. distichum, in 1960. Within the kinds of ergot produced by the various species of the genus Claviceps and its many hosts, cereals and wild grasses, types of ergot do exist that contain hallucinogenic alkaloids, the same alkaloids as in the Mexican hallucinogenic morning-glories. These alkaloids, mainly lysergic acid amide, lysergic acid hydroxyethylamide, and ergonovine, are soluble in water, in contrast to the non-hallucinogenic medicinally useful alkaloids of the ergotamine and ergotoxine type. With the techniques and equipment available in antiquity it was therefore easy to prepare an hallucinogenic extract from suitable kinds of ergot. What suitable kinds of ergot were accessible to the ancient Greeks? No rye grew there, but wheat and barley did and Claviceps purpurea flourishes on both. We analyzed ergot of wheat and ergot of barley in our laboratory and they were found to contain basically the same alkaloids as ergot of rye, viz alkaloids of the ergotamine and ergotoxine group, ergonovine, and sometimes also traces of lysergic acid amide. As I said before, ergonovine and lysergic acid amide, both psychoactive, are soluble in water whereas the other alkaloids are not. As we all know, ergot differs in its chemical constituents according to its host grass and according to geography. We have no way to tell what the chemistry was of the ergot of barley or wheat raised on the Rarian plain in the 2nd millennium B. C. But it is certainly not pulling a long bow to assume that the barley grown there was host to an ergot containing, perhaps among others, the soluble hallucinogenic alkaloids. The famous Rarian plain was adjacent to Eleusis. Indeed this may well have led to the choice of Eleusis for Demeter's temple, and for the growth of the cluster of powerful myths surrounding them and Triptolemus that still exert their spell on us today. The separation of the hallucinogenic agents by simple water solution from the non-soluble ergotamine and ergotoxine alkaloids was well within the range of possibilities open to Early Man in Greece. An easier method still would have been to have recourse to some kind of ergot like that growing on the grass Paspalum distichum, which contains only alkaloids that are hallucinogenic and which could even have been used directly in powder form. As I said before, P. distichum grows everywhere around the Mediterranean basin. During the many centuries when the Eleusinian Mysteries were thriving and holding the antique Greek world enthralled, may not the hierophants of Eleusis have been broadening their knowledge and improving their skills? For the Greek world as for us, the Mysteries are linked to Demeter and Kore, and they and Triptolemus are the famed mythical progenitors of cultivated wheat and barley. But in the course of time the hierophants could easily have discovered Claviceps paspali growing on the grass Paspalum distichum. Here they would be able to get their hallucinogen direct, straight and pure. But I mention this only as a possibility or a likelihood, and not because we need P. distichum to answer Wasson's question. Finally we must also discuss an ergot parasitical to a wild grass called in scientific nomenclature Lolium temulentum L. In English this is most widely known as darnel or cockle or (in the Bible) tares, a weed that plagues grain crops. It is sometimes called "wild rye grass", an unfortunate name because wild rye has nothing to do with rye: the rye of "wild rye grass" is of utterly different etymology. In classic Greek darnel was aira and in classic Latin was lolium. Its name in French is ivraie and in German Taumellolch, both names pointing to a belief in its psychotropic activity in the folk knowledge of the traditional European herbalists. A citation for ivraie in A. D. 1236 has been found, and it must go back much further than that. Analysis of Lolium temulentum in my laboratory and an extended botanical, chemical, and pharmacological investigation by I. Katz (4) showed that the plant itself contains no alkaloids nor does it possess any pharmacological activity. But the Lolium species (L. temulentum and L. perenne) are notoriously prey to the Claviceps fungus. The psychotropic reputation of darnel must therefore be attributed to its parasitic infection by ergot. Samples of ergot grown on L. temulentum and L.perenne collected in Germany, France, and Switzerland showed large variation in their alkaloidal composition. Some contained substantial amounts of ergonovine together with alkaloids of the ergotamine and ergotoxine group. (5) A species of ergot growing on darnel may have existed in ancient Greece that contained mainly hallucinogenic alkaloids of ergot such as we have found in ergot of Paspalum. In conclusion I now answer Wasson's question. The answer is yes, Early Man in ancient Greece could have arrived at an hallucinogen from ergot. He might have done this from ergot growing on wheat or barley. An easier way would have been to use the ergot growing on the common wild grass Paspalum. This is based on the assumption that the herbalists of ancient Greece were as intelligent and resourceful as the herbalists of pre-Conquest Mexico.
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