@article {LAMSON471, author = {PAUL DUDLEY LAMSON}, title = {ON THE PHARMACOLOGICAL ACTION OF HELENIN, THE ACTIVE PRINCIPLE OF HELENIUM AUTUMNALE}, volume = {4}, number = {6}, pages = {471--489}, year = {1913}, publisher = {American Society for Pharmacology and Experimental Therapeutics}, abstract = {Helenin, the active principle of Helenium Autumnale, is a crystalline substance of the empirical formula, C20H25O5; its melting point is 167{\textdegree} to 168{\textdegree}, and in water solution it reacts neutral. It reduces alkaline copper mannite solution on slight warming, but does not reduce this solution even on long standing in the cold. It gives with yeast, both before and after boiling with dilute hydrochloric acid solutions, no carbon dioxide gas formation, is optically inactive, and gives no osazone. The color test for carbohydrates with the Molisch reaction is negative. It contains then no carbohydrate group in the molecule, and is therefore no glucoside. It decolorizes solutions of Bromine in chloroform after one or two minutes in the cold completely, without evolution of hydrobromic acid gas. Accordingly one can conclude that Helenin contains unsaturated bonds, double linkages, which probably account for its property of reducing copper mannite solutions. The pharmacological action of crystalline Helenin corresponds essentially with that of the entire plant, Helenium Autumnale. It is a very active local irritant to the mucous membranes, causing sneezing and lachrymation, when the powdered substance comes in contact with the mucous membranes of the nose and eye, gastric and intestinal irritation with vomiting and diarrhoea, when taken by mouth and pain and oedema when injected under the skin. In cases of lethal poisoning acute gastroenteritis is the cause of death, when given per os; failure of heart when injected intravenously. Helenin causes a gradual paralysis of the heart, the action being exerted on the heart muscle itself. On the blood pressure it has little effect, except secondarily. On the respiration the action is very severe. The rate and force of respiration being increased, be the amount of expired air decreased. On the kidney the amounts injected in these experiments appear to have only a slight effect. On skeletal muscle it causes a rapid decrease of contractility, and in teased muscle preparations it causes a slight opacity of the fibers. Helenin can not be classed under the protoplasmic poisons and has no noticeable action as an antipyretic. Both very dilute and saturated solutions of Helenin in physiological salt solution, have no haemolytic action on the washed red blood corpuscles of rabbits. The pure crystalline Helenin produces the same symptoms when given to animals, as those described many years ago in cases of poisoning in cattle after ingestion of the plant. The giving of melted lard to cattle poisoned by the plant would appear rational from the results of my experiment with the active principle Helenin, in which oil was given internally to a dog per os. This treatment markedly decreased the local irritant action on the intestinal tract. It seems very probable that this plant may be a cause of fall hay fever. Concerning the many medicinal uses of Helenin mentioned in the literature, as a tonic, snuff, febrifuge, anthelminthic, diaphoretic, and as an antidote for "colds" and venereal diseases, its pharmacological properties most certainly justify its use as an errhine. It could be used as a stomachic in small doses on account of its bitter taste and its irritant action on the mucous membranes of the stomach. As a vermifuge its intense local irritant action on the mucous membrane of the stomach would exclude its use except in very dilute solutions, under which conditions its action on the parasites would be doubtful. The difficulty of its resorption from the intestinal tract would on the other hand, be a favorable property for this purpose, if an action on intestinal parasites could be demonstrated. The pharmacological properties of Helenin, do not justify its use as an antipyretic, or in any of the other above mentioned diseases. I wish here to express my thanks and appreciation to Prof. Edwin S. Faust for assistance rendered me in carrying out this work.}, issn = {0022-3565}, URL = {https://jpet.aspetjournals.org/content/4/6/471}, eprint = {https://jpet.aspetjournals.org/content/4/6/471.full.pdf}, journal = {Journal of Pharmacology and Experimental Therapeutics} }