Blue calyx A is a diterpenoid isolated from the genus Camellia in the Labiatae family. It is the main active component in Camellia. In recent years, the research on the antitumor, antiviral, antibacterial, cardiovascular system protection and anticancer activities of this diterpenoid has become one of the research hotspots in contemporary natural chemistry. Blue calyx a has outstanding advantages in anticoagulation.
The coagulation system and anticoagulation system in human body are in a dynamic equilibrium state. Excessive coagulation can lead to serious diseases such as myocardial infarction and cerebral thrombosis. In the process of thrombosis, thrombin produced after platelet activation and coagulation system activation is a powerful platelet activating factor, which will promote the coagulation process after platelet activation. Antithrombotic therapy is mainly aimed at the two links of coagulation system and platelet, which are called anticoagulant therapy and antiplatelet therapy respectively. At present, the commonly used anticoagulants in clinic mainly include heparin and coumarins, and aspirin is the most commonly used antiplatelet drug. Heparin drugs have strong anticoagulant effect by promoting the inactivation of activated coagulation factors containing serine residues by antithrombin III. however, heparin drugs cannot be administered orally, which is not convenient for patients. The structure of coumarins is similar to that of vitamin K. by antagonizing the utilization of vitamin K, coumarins can inhibit anticoagulation. Coumarins can be administered orally, but the effect is slow, and there is no anticoagulation and blood activating in vitro. Aspirin can inhibit cyclooxygenase activity, inhibit platelet arachidonic acid metabolism to produce thromboxane A2, and produce antiplatelet activity. In addition, aspirin also inhibits the synthesis of prothrombin in the liver and has anticoagulant effect.
Because blood coagulation has two coagulation pathways, endogenous and exogenous, APTT and PT are the two most commonly used parameters in clinical coagulation function detection. APTT is mainly used to detect the endogenous coagulation system of the body, and its prolongation or shortening respectively reflects the decrease or increase of the plasma activity of coagulation factors Ⅱ, Ⅴ, Ⅷ, Ⅹ, Xi and XII. PT is mainly used to detect the exogenous coagulation system of the body, and its prolongation or shortening respectively reflects the decrease or increase of the plasma activity of coagulation factors Ⅰ, Ⅱ, Ⅴ, Ⅶ and Ⅹ. The results showed that blue calyx a could significantly prolong the capillary coagulation time and tail tip bleeding time in mice, and had anticoagulant activity.
Glaucocalyxin A It has strong antiplatelet activity, has anticoagulant activity in vivo and in vitro, and can be administered orally, which has certain advantages over heparin and coumarin anticoagulants commonly used in clinic, and is worthy of further study on its anticoagulant mechanism and clinical application.