Allicillin

This Allicillin? formulation is the first ever commercially available garlic supplement containing significant levels of ajoene and diithins, the most active compounds formed from garlic.

Allicillin? softgels contain 200 mg Garlicillin?. Garlicillin? is a blend of garlic oil macerate and garlic oil containing 1mg of ajoene and diithins.

Since the discovery and identification of ajoene and diithins, there have been many studies that have demonstrated their related health benefits, which may include

• Anti-bacterial
• Anti-lipidemic
• Anti-fungal
• Anti-inflammatory
• Anti-parasitic
• Anti-tumorigenic and Anti-mutagenic
• Anti-thrombotic and Anti-platelet

This new enteric coated softgel contains the same garlic oil macerate oil that was used in the previous powdered, encapsulated product...ultimately, providing the same garlic bioactives and level of efficacy you've enjoyed with the previous product.

The purpose of the enteric coated softgel is to lessen the strong garlic odor and repeating that sometimes occurs from supplementing garlic.

Allicillin? softgels with 200mg Garlicillin? is up to several times more potent than a typical 500 mg non-standardized garlic oil macerate product, and is our most powerful product for protection against all types of pathogens.

Supplement Facts
Serving Size: 1 softgel
Servings Per Container: 60 softgels

Amount Per Serving:

STORE IN A COOL, DRY PLACE. KEEP OUT OF REACH OF CHILDREN.

Read customer questions and answers about Nutrition Basics on our blog.

What are Ajoene and Dithiins?
Ajoene and dithiins are natural products of allicin degradation in oil. According to Dr. Eric Block, leading expert in garlic sulfur compounds, ajoene and dithiins are the most active allicin metabolites. Ajoene consists of two isomers (E and Z) and is chemically represented by 4,5,9-trithiadodeca-1,6,11-triene-9-oxide. There are two dithiin isomers that had been identified, 2-vinyl-4H-1,3-dithiin and 3-vinyl-4H-1,2-dithiin.

What is Garlic Oil Macerate?
Garlic oil macerate is a popular health food in Europe. It is prepared by mixing mashed or chopped garlic in vegetable oil. Garlic oil macerate, which has been a dietary supplement for many decades, is the only garlic supplement that contains significant quantities of ajoene and dithiins. Lawson et al. reported that garlic oil macerates contain between 15 to 115 microgram/gram of ajoene and 70 to 690 microgram/gram dithiins.

Garlicillin? is a blend of garlic oil macerate and garlic oil with specified levels of ajoene and dithiins. Allicillin Pro? contains 400 mg Garlicillin? with 2 mg of ajoene and not less than 2 mg of dithiins, which is several times more than what is in a typical 500 mg non-standardized garlic oil macerate product. No other commercially available garlic preparation contains near the level of ajoene available from Allicillin Pro?.

What about Allicin?
The chemistry of garlic is extremely complex, but research has shown that it is garlic?s unique organosulfur compounds that promote its broad range of potential health benefits. Garlic has many bioactive components, the best known and studied of which is allicin. It is ironic that allicin does not exist in fresh, undamaged garlic cloves. The predominant garlic sulfur compound found in the garlic plant is alliin. Garlic also contains high levels of an enzyme called allinase. Alliin and allinase are held in different compartments of the garlic plant, by design, to react only when the plant is injured. When fresh garlic cloves are crushed or chopped, or when garlic powder (that has been carefully dried to preserve its alliin/allinase content) is added to water, allicin is produced in seconds by the action of allinase on alliin.

Many dietary supplement companies claim to provide a product that delivers allicin. Due to its instability allicin is often listed on labels as ?allicin potential? or ?allicin yield?. Allicin potential is measured in a laboratory by using dried garlic powder that is added to water so that the alliin and allinase can quickly react to form allicin. The amount of allicin produced is the measure of allicin potential. However, the situation is very different when such garlic supplements are swallowed. The allinase enzyme is rapidly and completely destroyed by stomach acid. Allicin cannot be made from alliin in the absence of allinase enzyme. Some garlic products claim to address this issue by using an enteric coated delivery method. Unfortunately, such methods do not work well at all. Lawson and Wang reported the results of testing twenty-three enteric coated U.S. garlic supplements in 2001. Twenty of twenty-three failed to release even 15 percent of their claimed "allicin potential" when placed in simulated intestinal fluid. Lawson and Wang concluded that allicin potential is an extremely poor measure of garlic supplement activity in the human body and should not be used for standardization of garlic supplements. Considering the questionable utility of allicin potential, technology was developed to produce the inherently stable metabolite of allicin, ajoene.

The Research on Ajoene is Broad and Impressive
In 1983, Apitz-Castro et al. isolated three garlic compounds that inhibited human platelet aggregation. Two of the compounds were identified as dithiins and third, which was four times more potent than the other two, was named ?ajoene? by Block and co-investigators from ?ajo?, the Spanish for garlic. From published literature search it is apparent that the antimicrobial (antibacterial and antifungal) properties of ajoene have received considerable attention. Studies show that ajoene exhibits broad spectrum antimicrobial activity. Naganawa et al., found that ajoene inhibited the growth of gram positive bacteria such as Bacillus cereus, B. subtilis, Mycobacterium smegmatis and Streptomyces griseus at 5 ug ajoene per ml and Staphylococcus aureus and Lactibacillus plantarum below 20 ug per ml. It was reported that growth of gram-negative bacteria such as Escherichia coli, Klebsiella pneumonia and Xanthomonas maltophilia were also inhibited by ajoene at higher doses, 100 to 160 ug/ml. Ajoene from garlic oil macerate likewise inhibited the growth of Helicobacter pylori at 10 to 25 ug/ml.

Yoshida et al showed that ajoene is more effective than allicin against Aspergillus niger (16.6 ug/ml vs. 30.9 ug/ml) and Candida albicans (7.6 ug/ml vs. 17.3 ug/ml).
In clinical studies ajoene was shown to be as effective or better than terbinafine in the treatment of tinea pedis (athlete?s foot), tinea corporis (generalized itch due to fungal infection, e.g., ringworm), and tinea cruris (groin itch). Ajoene was also effective against Paracoccidioides brasilienses, a common fungus that causes systemic mycoses in Latin America. When tested against Scedosporium prolificans, a fungus that is very difficult to treat, ajoene had a minimum inhibition concentration (MIC) of 2.0 to 8.0 mg/l compared to 2.0 to >16 mg/l for amphotericin B and >16 mg/l for itraconazole.6 Incredibly, ajoene has even successfully treated malaria in an in vivo animal model.

Ajoene and other garlic extracts including allicin were tested in vitro against several viruses including herpes simplex virus type 1, herpes simplex virus type 2, parainfluenza virus type 3 and human rhinovirus type 2.  Ajoene was found to have the greatest virucidal activity compared to allicin and other garlic extracts tested. Ajoene and dithiins have chemopreventive properties with their ability to inhibit aflatoxin B1-induced mutagenesis. Ajoene and dithiins were shown to inhibit cholesterol synthesis with dithiins exhibiting the highest antioxidative effect on human low-density lipoprotein.

Who SHOULD take Allicillin??
Patients with recurring yeast infections, bacterial or viral infections, lipid abnormalities, platelet aggregation, inflammation, immune deficiency and/or history of cancer or heart disease. Consider Allicillin? supplementation during antibiotic usage to prevent yeast overgrowth, a common side effect of antibiotic therapy. It may also help improve symptoms of Lyme disease. This product may be used in high doses for acute conditions and can be taken as directed daily for prevention.

Allicillin? has blood thinning capabilities and reduces platelet aggregation. Be cautious when recommending to patients taking Coumadin, Warfarin or other anti-coagulant medications.

References

1. Identification and HPLC quantitation of the sulfides and dialk(en)yl thiosulfinates in commercial garlic products. Lawson, LD, Wang ZJ, Hughes B. Planta Med. 1991. 57:363-370.

2. The chemistry of garlic health benefits. Passwater R. Whole Foods 15(6) 22-26 (June 1992), www.drpasswater.com.

3. Inhibition of microbial growth by ajoene, a sulfur-containing compound derived from garlic. Naganawa R, Iwata N, Ishikawa K, et al. Appl Environ Microbiol. 1996 Nov;62(11):4238-42.

4. An organosulfur compound isolated from oil-macerated garlic extract, and its antimicrobial effect. Yoshida H, Katsuzaki H, Ohta R, et al. Biosci Biotechnol Biochem. 1999 Mar;63(3):588-90.

5. In vitro inhibition of the growth of Helicobacter pylori by oil-macerated garlic constituents. Ohta R, Yamada N, Kaneko H, et al. Antimicrob Agents Chemother. 1999 Jul;43(7):1811-2.

6. The in vitro susceptibility of Scedosporium prolificans to ajoene, allitridium and a raw extract of garlic (Allium sativum). Davis SR, Perrie R, Apitz-Castro R. J Antimicrob Chemother. 2003 Mar;51(3):593-7.

7. Efficacy of ajoene in the treatment of tinea pedis: a double-blind and comparative study with terbinafine. Ledezma E, Marcano K, Jorquera A, et al. J Am Acad Dermatol. 2000 Nov;43(5 Pt 1):829-32.

8. Ajoene in the topical short-term treatment of tinea cruris and tinea corporis in humans. Randomized comparative study with terbinafine. Ledezma E, Ląpez JC, Marin P, et al. Arzneimittelforschung. 1999 Jun;49(6):544-7.

9. Inhibition of growth of the dimorphic fungus Paracoccidioides brasiliensis by ajoene. San-Blas G, San-Blas F, Gil F, Mari€o L, Apitz-Castro R. Antimicrob Agents Chemother. 1989 Sep;33(9):1641-4.

10. Antifungal activity of ajoene derived from garlic. Yoshida S, Kasuga S, Hayashi N, et al. Appl Environ Microbiol. 1987 Mar;53(3):615-7.

11. In vitro synergism of concentrated Allium sativum extract and amphotericin B against Cryptococcus neoformans. Davis LE, Shen J, Royer RE. Planta Med. 1994 Dec;60(6):546-9.

12. In vivo activity of ajoene against rodent malaria. Perez HA, De la Rosa M, Apitz R. Antimicrob Agents Chemother. 1994 Feb;38(2):337-9.

13. Effect of ajoene, the major antiplatelet compound from garlic, on platelet thrombus formation. Apitz-Castro R, Badimon JJ, Badimon L. Thromb Res. 1992 Oct 15;68(2):145-55.

14. Thermochemical transformation of sulfur compounds in Japanese domestic Allium, Allium victorialis L. Nishimura H, Takahashi T, Wijaya CH, et al. Biofactors. 2000;13(1-4):257-63.

15. Inhibition of cholesterol biosynthesis by allicin and ajoene in rat hepatocytes and HepG2 cells. Gebhardt R, Beck H, Wagner KG. Biochim Biophys Acta. 1994 Jun 23;1213(1):57-62.

16. Inhibition of cholesterol synthesis in vitro by extracts and isolated compounds prepared from garlic and wild garlic. Sendl A, Schliack M, L”ser R, et al. Atherosclerosis. 1992 May;94(1):79-85.

17. Ajoene, a natural product with non-steroidal anti-inflammatory drug (NSAID)-like properties? Dirsch VM, Vollmar AM. Biochem Pharmacol. 2001 Mar 1;61(5):587-93.

18. Effect of allicin and ajoene, two compounds of garlic, on inducible nitric oxide synthase. Dirsch VM, Kiemer AK, Wagner H, Vollmar AM. Atherosclerosis. 1998 Aug;139(2):333-9.

19. Ajoene inhibits both primary tumor growth and metastasis of B16/BL6 melanoma cells in C57BL/6 mice. Taylor P, Noriega R, Farah C, et al. Cancer Lett. 2006 Aug 8;239(2):298-304. Epub 2005 Oct 10.

20. Inhibition by ajoene of skin-tumor promotion in mice. Nishikawa T, Yamada N, Hattori A, et al. Biosci Biotechnol Biochem. 2002 Oct;66(10):2221-3.

21. Antimutagenic effects of ajoene, an organosulfur compound derived from garlic. Ishikawa K, Naganawa R, Yoshida H, et al. Biosci Biotechnol Biochem. 1996 Dec;60(12):2086-8.

22. Low allicin release from garlic supplements: a major problem due to the sensitivities of allinase activity. Lawson, L. & Wang, Z. J Agric Food Chem 49(2001): 2592-99.

23. Effects of garlic extract and of three pure components isolated from it on human platelet aggregation, arachidonate metabolism, release reaction and platelet ultrastructure. Apitz-Castro R, Cabrera S, Cruz MR, et al. Thromb Res. 1983 Oct 15;32(2):155-69.

24. Garlic and Other Alliums: The Lore and the Science. Block E. Royal Society of Chemistry. 2010. Allicin Transformations, Part 2: The discovery of Ajoene, p. 190.

25. In vitro virucidal effects of Allium sativum (garlic) extract and compounds. Weber ND, Andersen DO, North JA, et al. Planta Med. 1992 Oct;58(5):417-23.

26. Organosulfur compounds of garlic modulate mutagenesis, metabolism, and DNA binding of aflatoxin B1. Tadi PP, Teel RW, Lau BH. Nutr Cancer. 1991;15(2):87-95.

27. Chemoprotection by organosulfur inducers of phase 2 enzymes: dithiolethiones and dithiins. Kensler TW, Curphey TJ, Maxiutenko Y, Roebuck BD. Drug Metabol Drug Interact. 2000;17(1-4):3-22.

28. Antioxidative activity of sulfur-containing compounds in Allium species for human low-density lipoprotein (LDL) oxidation in vitro. Higuchi O, Tateshita K, Nishimura H. J Agric Food Chem. 2003 Nov 19;51(24):7208-14.