In 1916, the medical community ushered in a revolutionary breakthrough—the discovery of heparin. This discovery not only changed the face of anticoagulation therapy, but also played an irreplaceable role in the management of cardiovascular disease and a variety of other conditions. As a naturally occurring anticoagulant, heparin's mechanism of action and clinical application are still worthy of in-depth exploration.
The name heparin comes from the Greek "ἧπαρ", which means liver. It was originally isolated from dog liver cells in 1916 by American biomedical scientists Jay McLean and William Henry Howell. McLean, then a second-year medical student, studied the preparation process of coagulants under the guidance of Howell, and eventually isolated this lipid-rich anticoagulant.
"The discovery of heparin was a major milestone in medicine, and its anticoagulant power changed the way heart disease and other blood clotting disorders are treated."
However, heparin did not officially enter clinical trials until 1935. During this period, researchers conducted extensive discussions on its chemical structure and mechanism of action. In 1936, the Swedish company Vitrum AB launched the first intravenously injectable heparin product, officially introducing heparin into clinical treatment.
Heparin prevents thrombus formation by inhibiting thrombin and other procoagulant serine proteases. Specifically, heparin binds to antithrombin III, causing its conformation to change, thereby enhancing its inhibitory effect on thrombin and factor Xa. The efficiency of this process can be increased by up to 1,000 times.
"The use of heparin makes blood anticoagulation therapy safer and more effective."
Heparin is mainly used in the following situations: prevention and treatment of acute coronary syndrome (such as NSTEMI), atrial fibrillation, deep vein thrombosis and pulmonary embolism. Heparin is also widely used during medical procedures such as cardiac surgery and dialysis to prevent blood from clotting in the tubes.
Although the use of heparin has good medical effects, it is not without risks. One of the most serious side effects is heparin-induced thrombocytopenia (HIT), a decrease in platelets caused by an immune response. Discontinuation of heparin usually results in recovery, but this can be potentially dangerous in patients with cardiovascular disease.
Over time, the origin of heparin has changed. Due to the impact of the bovine epilepsy (BSE) epidemic, many manufacturers have begun to reduce the extraction of heparin from bovine tissue and rely instead on the pork industry. However, the impact on global supply chains has been particularly evident during the COVID-19 outbreak in 2020, with reduced availability of heparin challenging healthcare facilities around the world.
“In the COVID-19 epidemic, the effectiveness of heparin has been reassessed, but supply shortages have created a greater health crisis.”
Although heparin has experienced a hundred years of development since its discovery, with the advancement of medicine, research on its application in various emerging diseases (such as COVID-19) continues. How to effectively utilize heparin and its derivatives to improve the safety and effectiveness of anticoagulation therapy and reduce potential side effects will become an important direction for future research.
The discovery of heparin is not only an important milestone in the history of medicine, but also opens up new discussions on hemorrheology and anticoagulation therapy. Facing future medical challenges, what enlightenment can the research on heparin bring to us?