Stabilization and pharmaceutical use of alliinase.
In recent years, numerous clinical trials were undertaken in order to elucidate the active principle of garlic (Allium sativum L., Alliaceae). The most prominent effect of garlic preparations is a contribution to the prevention of stroke and arteriosclerosis. Allicin[(2-propenyl)-2-propenethiosulfinate] and other sulfur containing compounds were suggested as active compounds. The extremely unstable allicin itself is liberated from the more stable alliin [S-(+)-2-propenyl-L-cysteine sulfoxide] by the enzyme alliinase (EC 4.4.1.4) if fresh garlic is crunched or garlic powder is moistened. Therefore, an active enzyme is required in alliin containing remedies like those prepared from garlic powder. In order to investigate enzyme stability, alliinase was isolated from garlic powder. The partially purified enzyme could be stabilized over several months by addition of sodium chloride, sucrose, and pyridoxal-5'-phosphate. Alliinase may also be freeze-dried. This allows combinations of synthetic alliin and purified alliinase as components of an acid resistant tablet or capsule. In the intestine, the pro-drug alliin would be enzymatically converted to allicin. In clinical trials, highly dosed preparations of this kind should yield a precise information about the physiological effects of allicin. In addition, alliin-homologues substances which bear a modified alkyl side chain and do not occur in nature may be tested.
Krest
I
I
Institut für Pharmazeutische Biologie, Universität Bonn, Germany.
Keusgen
M
M
D002021:Buffers; D013437:Carbon-Sulfur Lyases / Q000737:chemistry* / Q000302:isolation & purification; D004355:Drug Stability; D005079:Excipients; D005737:Garlic / Q000737:chemistry*; D010946:Plants, Medicinal; D013056:Spectrophotometry, Ultraviolet
D002021:Buffers; D005079:Excipients; D013437:Carbon-Sulfur Lyases; C019243:alliin lyase