The Century Legend of Aspirin (1)

[If I are going to be on a desert island and choose to carry some medicine with me, then she may be the first thing to think about-aspirin)]

-Professor John A. Baron, Dartmouth School of Medicine

Doubts about one’s life experience

In other words, the current rapid upgrading of drugs, It has almost reached a dazzling level. Even some doctors are likely not to know the latest development of some drugs in their relevant specialties. It can be said that there are talented people in the country, The waves behind the Yangtze River push forward the waves before. However, among the numerous and constantly changing drugs, there is such an effective exception. Although she has gone through a hundred years of vicissitudes, Instead of being squeezed out of the drug market by the endless younger generation, The tragic situation of “dying on the beach before the waves” has been continuously developed into various magical new functions, with the potential for old trees to blossom new flowers. The recent New York Times also reported on her latest research results, suggesting that it may be helpful to colon cancer patients.

As one of the most respected in the drug industry, We can even boldly predict that aspirin will glorify the history of human medicine. The famous Spanish philosopher Jose Ortega Gassette said in his monograph “The Age of Aspirin” that aspirin is [a blessing brought to mankind by civilization]. At present, the known exact functions include antipyretic, analgesic, anti-inflammatory, anti-rheumatism, prevention of myocardial infarction and prevention of stroke. We are still studying areas that may make great achievements: anti-cancer, anti-hypertension, kidney protection, treatment of some eye diseases, adjuvant treatment of diabetes…

Now many people talk about aspirin as much as they talk about anything they are familiar with. Basically, I have long forgotten her chemical name: acetylsalicylic acid. At present, the world produces nearly 50,000 tons of acetylsalicylic acid every year, which is about 100 billion tablets of aspirin based on 500 milligrams per tablet. If there is such an aspirin rain underground, the scene is estimated to be quite spectacular (in Song Dandan’s tone).

Just like the mysterious life experience of the hero in some legendary stories, aspirin has gone through some twists and turns before and after its birth, and even some important details are still controversial.

Long ago, The ancient Greeks and Egyptians knew to use willow bark to relieve pain, Hippocrates (460 BC-370 BC) and Galen (129-199/217), Galen was also the first to record the antipyretic and anti-inflammatory effects of willow skin, Of course, these records were completed long before the establishment of modern evidence-based medicine, mainly based on personal experience summary and hearsay. Most of the drugs summarized by this method, whether traditional Western medicine or traditional Chinese medicine, were unreliable. At that time, willow skin was mixed among many herbs that only had the function of placebo, and perhaps its position was not prominent.

Is the so-called [thousands of Tao Wan Lu although hard, Blow all the crazy sand before you reach gold], If it is real gold, it will not be covered by yellow sand forever. In 1763, Scientist Reverend Edmund Stone (press: The Journal of Science misspelled his name Edward, Written as Edmond, In fact, Edward Stone (Reverend) recorded the efficacy of willow skin for the first time. But Edmund Stone is more famous, As a result, it has been misinformed for a long time. Until I am still wrong here, This confusion was later clarified by William Pierpoint in 1996. I just learned that, Teacher Xie Sun Yifei Corrected-February 15, 2014) Records Cases of Malaria Treated with Willow Skin (Symptoms Are Fever and Accompanied by Pain), This record, It is generally believed that it is the first time in modern science to describe the efficacy of willow skin. Later, With the development of chemical technology, Scientists have been able to extract compounds from willow skins, In 1826, Italians Brugnatelli and Fontana discovered that willow bark contains a substance called salicin, But the purity of the samples they got was not enough. In 1829, French chemist Henri Leroux improved the extraction technology. He could already extract 30 g from 1.5 kg of bark from 1.5 kg of willow skin. Although the substance tastes bitter, it can treat fever and pain. It turns out that bitter taste is not the unique rule of traditional Chinese medicine. In 1838, Italian chemist Raffaele Piria discovered that salicylic acid, which is hydrolyzed and oxidized into salicylic acid, has better efficacy than salicin.

In 1859, The Germans have discovered a cheap method to synthesize salicylic acid. Therefore, salicylic acid can be widely used to treat pain and swelling caused by arthritis and other diseases. As well as fever caused by diseases such as influenza. However, the widespread use of salicylic acid also made people quickly notice the obvious side effects of the chemical-they can seriously disturb the digestive function of patients. Some people even bleed their stomachs by taking large quantities of these chemicals to control pain and swelling. The so-called “three-point poison” does not distinguish between the middle and the west. Please note that the real body of aspirin, acetylsalicylic acid, is about to come on stage at this time, and the details that cannot be grasped are also at this stage.

One of the most widely known statements, which Bayer has always insisted on, is that German Hoff suffers from severe arthritis, but his stomach cannot bear the stimulation of salicylic acid. Can arthritis be treated while avoiding or reducing the damage to the stomach? This attracted the great attention of his son, German chemist Felix Hoffmann (1868-1946). (How does the story look like a standard bosom friend? ) Felix was working for a company called Friedrich Bayer, In order to solve this difficult problem (reportedly mainly to help his father find more suitable drugs), He looked through a large number of chemical literature. At that time, it was believed that the reason why salicylic acid stimulated gastric mucosa was that it was an acidic substance (the exact mechanism will be explained in detail later). So he added the compound in a series of chemical reactions, and covered some acidic part with an acetyl group, eventually converting it into acetylsalicylic acid. He found that acetylsalicylic acid has better therapeutic effect than salicylic acid while relieving stomach irritation, shine on you is better than blue.

However, when this drug was first introduced, It has not attracted enough attention from conservative bosses, A generation of classic drugs was concealed for two years after they were synthesized in 1897. It was not until two years later that Heinrich Dreser, a senior pharmacist and scientist at Bayer, demonstrated the effectiveness of the new drug. And gave it a new name, which is now widely known as [aspirin]. (There is also a saying that Dreiser hid aspirin because he feared that aspirin would steal the limelight of heroin, which was also synthesized by Bayer in 1897 and used to relieve cough).

However, the story is most likely made up, just like the apple that hit Newton’s head. Many people question this statement.

In 1949, Arthur Eichengr ü n (1867-1949) wrote that, He was the main inventor of aspirin, And Felix Hoffman is just a man who works in his laboratory. But Bayer did not buy this statement, According to the company’s records, the two are not superior-subordinate relations at all. In theory, they are both Bayer companies. No matter who the flowers go to, the honor will belong to Bayer. A bowl of water should be even, There is no need to discriminate between one and the other, And Eichenglin was so long after the event, That is to say, it is inconceivable to tell the truth before dying. It turns out that when the German official said, When the story of Felix Hoffman [filial piety] was preached, The Nazis are already in power, As a Jewish, Eichenglin was lucky to be able to save his life in troubled times. An dare to expect this honor. This case has not been finalized so far. Personally, I feel that Eichenglin is somewhat wronged. However, considering that French chemist Charles Frederic Gerhardt had already synthesized acetylsalicylic acid as early as 1853, It can only be said that the honor of aspirin belongs to Germany, Germany is really lucky. In 2002, The US National Inventors Hall of Fame includes Felix Hoffman, It is really hard for me to understand why such a controversial figure should be included. But perhaps it is not the matter that makes people feel most puzzled. Because among the huge profits brought by aspirin, It was neither Eichenglin nor Felix Hoffman who made the greatest profits, but Dreiser, who initially opposed aspirin clinical trials. If this story were to be put on stage, I really wanted to paint Dreiser a white face.

The mysterious aspirin, which was born like this, may be doomed to become legendary and radiant in the future. However, these arguments in the old paper pile made my head ache very much, so I quickly found some aspirin to eat.

Arthur Eichengr ü n (1867-1949)

Felix Hoffmann (1868-1946)

Author: Li Morning