“Aspirin: a history, a love story. Most pharmacists know that aspirin’s origins lie with willow bark, but they may be unaware of its role in the development of the pharmaceutical industry. Evolving from salacin (the active ingredient in many plant remedies) to salicylic acid (an analgesic in its own right) to the more effective, less toxic acetylsalicylic acid, this pain reliever cornered the nonsteroidal anti-inflammatory market for more than 70 years. It helped the dye industry branch into pharmaceuticals, and is now used in multiple indications.”  http://www.ncbi.nlm.nih.gov/pubmed/22591976

“Willow species and aspirin: different mechanism of actions. Many believe that willow is the natural source of aspirin. However, willow species contain only a low quantity of the prodrug salicin which is metabolized during absorption into various salicylate derivatives. If calculated as salicylic acid, the daily salicin dose is insufficient to produce analgesia. Salicylic acid concentrations following an analgesic dose of aspirin are an order of magnitude higher. Flavonoids and polyphenols contribute to the potent willow bark analgesic and anti-inflammatory effect. The multi-component active principle of willow bark provides a broader mechanism of action than aspirin and is devoid of serious adverse events. In contrast to synthetic aspirin, willow bark does not damage the gastrointestinal mucosa. An extract dose with 240 mg salicin had no major impact on blood clotting. In patients with known aspirin allergy willow bark products are contraindicated.” http://www.ncbi.nlm.nih.gov/pubmed/21226125

“History as a tool in identifying “new” old drugs. To trace the history of a natural product and its use, it is necessary to identify to correct plant among around a half-million species. One must also know how and when harvest the plant and the morphology of location and extraction. Within the same species plant chemistry varies, depending upon climatic and soil conditions, stage of maturity and even diurnal factors. To all of these variations must be added the diagnostic ability of physicians and native healers (to distinguish between Hippocratically-trained Western physicians and whose knowledge is less formally taught). Seldom was a disease identified as we Know it today, but the constellations of symptoms described, when studied carefully within the framework historical setting of the culture, can be related to modern medicine. It is essential to study the historical contemporary usage data in the language in which those accounts were writTen. Translators are often philologists who are not sensitive to medical nuances. Modern readers of translated historical documents often are unaware of the precision the authors delivered in describing medical afflictions and their treatments. Natural product drugs are truly products of human knowledge. Because so many modern pharmaceuticals are manufactured synthetically we forget that once either the compound or its affinity had a home in a natural product. Over 2,500 years ago man first used a drug obtained from white willow bark, which was aspirin or acetylsalicylic acid. Today’s scientists continue to be bewildered by just what aspirin’s mechanisms of action are, discovering new modes of action, and how they relate to medical diagnostics. Whatever the science of aspirin, an intelligent person today takes it just as our ancestors did fo millennia. Throughout time, explanations continue to vary just as purpose of administration do as well. Nevertheless, aspirin is perceived as being beneficial. Historical in-use data can also be a factor in judging a drug’s safety, since the records of its use provide observations made by intelligent persons over generations of employment Many historical “drugs” have crossed the line from drug to food. A number of them are now common items on our tables: coffee, tea, sugar, lemon, chocolate, pepper, to name a few The example of coffee affords useful insight. It was first employed as a drug (like tobacco), its botany and chemistry are well known, it has been in widespread use for centuries with diverse ethnic populations in a variety of preparations and amounts consumed. Still we are unsure about coffee’s effect on health, the latest assertion being that the caffeine it contains may delay the onset of Alzheimer’s. In contrast, the mercury drugs were in widespread use for a long period of time by many populations and that fact indicates that the toxic tolerance in humans is probably higher than as currently proscribed. The past contains important data for the scientific investigator. Like any field of research, historical investigation requires specialized knowledge, but much of that knowledge is readily accessible and employable. Rediscovery through examination of historical contemporaneous use data can be efficient and relatively easy compared to the travails of original research in pursuit of a discovery only to learn later that our ancestors had already made that discovery through trial and error in human usage. If we had started a search from the clues provided by history, presumably our discoveries would have been earlier, and we would have benefitted. As it is. we learn history but not science or else we learn science, not history. Both taken together the learning can be enhanced.” http://www.ncbi.nlm.nih.gov/pubmed/12083469

“Early drug discovery and the rise of pharmaceutical chemistry. Studies in the field of forensic pharmacology and toxicology would not be complete without some knowledge of the history of drug discovery, the various personalities involved, and the events leading to the development and introduction of new therapeutic agents. The first medicinal drugs came from natural sources and existed in the form of herbs, plants, roots, vines and fungi. Until the mid-nineteenth century nature’s pharmaceuticals were all that were available to relieve man’s pain and suffering. The first synthetic drug, chloral hydrate, was discovered in 1869 and introduced as a sedative-hypnotic; it is still available today in some countries. The first pharmaceutical companies were spin-offs from the textiles and synthetic dye industry and owe much to the rich source of organic chemicals derived from the distillation of coal (coal-tar). The first analgesics and antipyretics, exemplified by phenacetin and acetanilide, were simple chemical derivatives of aniline and p-nitrophenol, both of which were byproducts from coal-tar. An extract from the bark of the white willow tree had been used for centuries to treat various fevers and inflammation. The active principle in white willow, salicin or salicylic acid, had a bitter taste and irritated the gastric mucosa, but a simple chemical modification was much more palatable. This was acetylsalicylic acid, better known as Aspirin®, the first blockbuster drug. At the start of the twentieth century, the first of the barbiturate family of drugs entered the pharmacopoeia and the rest, as they say, is history.”  http://www.ncbi.nlm.nih.gov/pubmed/21698778