Hematin

Hematin, an iron-containing porphyrin, inhibits the activity of clotting factors and also fibrin clot lysis through the mechanism of binding to and inactivation of hemostatic proteins[1]. Hematin can be used for the research of acute porphyrias and cancer[1][2][3][4][5].

Hematin (0.01 mg/ml) inhibits the clotting of bovine fibrinogen (1.3 to 2.6 mg/ml) by bovine thrombin (0.12 U/ml) and inhibits the hydrolysis of a synthetic substrate by human thrombin[2].Hematin (0.035 mg/ml) reduces VIII:C activity from 0.88 to 0.40 U/ml[2].Hematin (0.05 mg/ml) inhibits the activation of VIII:C by thrombin (0.04 U/ml)[2].Hematin (0.09 mg/ml) inhibits the hydrolysis of a synthetic substrate by plasmin[2].

Hematin (i.v.; single injection) suppressed porphyrin production in SD rat (weighing 160-205 g)[4].

[1]. Siegert SW, et al. Physicochemical properties, pharmacokinetics, and pharmacodynamics of intravenous hematin: a literature review. Adv Ther. 2008 Sep;25(9):842-57.
[2]. Green D, et al. The inactivation of hemostatic factors by hematin. J Lab Clin Med. 1983;102: 361-369.
[3]. Amin ML, et al. Development of hematin conjugated PLGA nanoparticle for selective cancer targeting. Eur J Pharm Sci. 2016 Aug 25;91:138-43.
[4]. Goetsch C, et al. Instability of hematin used in the treatment of acute hepatic porphyria. N Engl J Med. 1986;315: 235-238.
[5]. Quadros HC, et al. The Role of the Iron Protoporphyrins Heme and Hematin in the Antimalarial Activity of Endoperoxide Drugs. Pharmaceuticals (Basel). 2022;15(1):60. Published 2022 Jan 4.