Allicin

Allicin is a natural product originally isolated from A. sativum that has wide-ranging biological effects including antioxidative, anticancer, antimicrobial, and antifungal activities.^1,2,3,4 It inhibits the cysteine proteases cathepsin B and L, facipain 2, and rhodesain with K_i values of 8.6 and 9.3, 1.04, and 5.31 ?M, respectively.⁵ It shows antiparasitic activity against P. falciparum (IC₅₀ = 5.2 ?M) and T. b. brucei (IC₅₀ = 13.8 ?M), the parasites that cause malaria and African sleeping sickness, respectively. Allicin (5-10 ?M) dose-dependently inhibits cell adhesion, invasion, and migration in various lung adenocarcinoma cell lines.² It also alters the balance of tissue inhibitors of matrix metalloproteinases (TIMPs) and matrix metalloproteinases (MMPs), decreases phosphorylation of Akt, and decreases PI3K/Akt signaling.

1.Chan, J.Y., Yuen, A.C., Chan, R.Y., et al.A review of the cardiovascular benefits and antioxidant properties of allicinPhytother. Res.27(5)637-646(2013) 2.Huang, L., Song, Y., Lian, J., et al.Allicin inhibits the invasion of lung adenocarcinoma cells by altering tissue inhibitor of metalloproteinase/matrix metalloproteinase balance via reducing the activity of phosphoinositide 3-kinase/AKT signaling.Oncol. Lett.14(1)468-474(2017) 3.Ankri, S., and Mirelman, D.Antimicrobial properties of allicin from garlicMicrobes Infect.1(2)125-129(1999) 4.Burian, J.P., Sacramento, L.V.S., and Carlos, I.Z.Fungal infection control by garlic extracts (Allium sativum L.) and modulation of peritoneal macrophages activity in murine model of sporotrichosis.Braz. J. Biol.(2017) 5.Waag, T., Gelhaus, C., Rath, J., et al.Allicin and derivates are cysteine protease inhibitors with antiparasitic activityBioorg. Med. Chem. Lett.20(18)5541-5543(2010)