Add time:09/25/2019         Source:sciencedirect.com

(1) The literature on gitalin up to 1950 is briefly mentioned. Up to that time, the usefulness and existence of gitalin as a chemical entity was widely doubted. (2) In the early nineteen-fifties, Batterman stated that gitalin is inherently less toxic than other digitalis preparations. (3) Batterman's findings provoked many clinical and pharmacologic investigations by many workers whose results ranged from complete agreement to complete disagreement with his statements. All of these investigations had in common the fact that none of them were based on a clear understanding of the chemical nature of gitalin. (4) The chemistry of gitalin was brought to light in 1956, by Haack and co-workers, who discovered that it was a glycosidal mixture which contained two new glycosides, gitaloxin and formyl-strospeside. (5) Thus, previous researchers studied and reported on a drug without knowledge of the existence of two very potent but extremely labile constituents. Re-evaluation of their conflicting results and new investigations are indicated, modified according to the discoveries of Haack and others. (6) Biologically inactive leaf substances which make up about half of the “gitalin fraction” have been found to increase the solubility and diffusibility of cardiac glycosides. Gitoxin, long thought to be useless because of its poor absorption, instead plays an important cardiotonic role when in the presence of these nonactive “companion substances.” (7) Standards are suggested for future clinical trials of cardiac glycosides.

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