Efficacy of allicin, the reactive molecule of garlic, in inhibiting Aspergillus spp. in vitro, and in a murine model of disseminated aspergillosis

Shadkchan, Yona; Shemesh, E; Mirelman, David; Miron, Talia; Rabinkov, Aharon; Wilchek, Meir; Osherov, Nir

doi:10.1093/jac/dkh174

Cited by 74 publications

(72 citation statements)

References 16 publications

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“…The bioactive property of garlic was formed by the interaction of the non-protein amino acid alliin and the enzyme alliinase [22]. Thiosulfinates were produced through interaction, most commonly induced by crushing the mature garlic clove, of which around 70% of the bioactive compounds produced was allicin (diallylthiosulphinate) [22,23]. Allicin was responsible for garlic's pungent odour and the many medicinal health benefits associated with the consumption of garlic [24].…”

Section: Discussionmentioning

confidence: 99%

Body Surface Changes in Gastrointestinal Helminthes Following in vitro Treatment with Allium sativum Oil

Shalaby¹

2014

J Veterinar Sci Technol

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A scanning electron microscopic study was undertaken to assess, for the first time, whether Allium sativum oil (ASO) extract had any effect on helminthes' body surface following 24 h incubation in vitro. Two species of gastrointestinal helminthes, of most economic significance in sheep, Haemonchus contortus and Moniezia expansa were collected from naturally infected sheep slaughtered in Cairo abattoir, then exposed to 10, 50, 100 µg/ml ASO. The body surface of these helminthes was observed to be affected and altered by ASO. These changes were concentration dependent, and consisted of destructive alterations and deformity in the cuticle of H. contortus and also in the tegumental architecture of M. expansa. The current study confirmed that an alternative, effective and natural anthelmintic could be developed using garlic. Body Surface Changes in Gastrointestinal Helminthes Following in vitro Treatment with Allium sativum OilHatem A Shalaby* and Tarek K Farag Department of Parasitology and Animal Diseases, National Research Center, Giza, Egypt Materials and Methods Preparation of A. sativum oil extractBulbs of fully grown A. sativum cultivated locally were used in the study. The dried bulbs were pounded and then steam distilled. The essential oil was extracted using solvent ether.

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Section: Discussionmentioning

confidence: 99%

Body Surface Changes in Gastrointestinal Helminthes Following in vitro Treatment with Allium sativum Oil

Shalaby¹

2014

J Veterinar Sci Technol

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“…Enzyme and substrate are located in different compartments of the clove, so that allicin is generated only when the clove is crushed (18,41). Many lines of evidence indicate that allicin is primarily responsible for garlic's antiinfective properties (1,5,15,34,38,43), although studies have also found that ajoene, a metabolite of allicin found when garlic is crushed specifically in oil, also has some antibacterial properties (27). In fact, one study found that ajoene has an inhibitory effect on the erythrocytic stages of Plasmodium (30).…”

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confidence: 99%

Antimalarial Activity of Allicin, a Biologically Active Compound from Garlic Cloves

Coppi

Cabinian

Mirelman

et al. 2006

Antimicrob Agents Chemother

127

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The incidence of malaria is increasing, and there is an urgent need to identify new drug targets for both prophylaxis and chemotherapy. Potential new drug targets include Plasmodium proteases that play critical roles in the parasite life cycle. We have previously shown that the major surface protein of Plasmodium sporozoites, the circumsporozoite protein (CSP), is proteolytically processed by a parasite-derived cysteine protease, and this processing event is temporally associated with sporozoite invasion of host cells. E-64, a cysteine protease inhibitor, inhibits CSP processing and prevents invasion of host cells in vitro and in vivo. Here we tested allicin, a cysteine protease inhibitor found in garlic extracts, for its ability to inhibit malaria infection. At low concentrations, allicin was not toxic to either sporozoites or mammalian cells. At these concentrations, allicin inhibited CSP processing and prevented sporozoite invasion of host cells in vitro. In vivo, mice injected with allicin had decreased Plasmodium infections compared to controls. When sporozoites were treated with allicin before injection into mice, malaria infection was completely prevented. We also tested allicin on erythrocytic stages and found that a 4-day regimen of allicin administered either orally or intravenously significantly decreased parasitemias and increased the survival of infected mice by 10 days. Together, these experiments demonstrate that the same cysteine protease inhibitor can target two different life cycle stages in the vertebrate host.

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“…Allicin (diallyl-dithiosulfinate), the biologically active molecule of garlic, has been shown to have a very wide range of antimicrobial activities and contributes to the defense of the garlic plant against soil microorganisms (1,11,15,20,29,36,44). Allicin is produced by the catalytic reaction of the enzyme alliinase (EC 4.4.1.4) with the inert, nonprotein amino acid substrate alliin [(ϩ)-S-allyl-cysteine sulfoxide].…”

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confidence: 99%

“…Crushing the garlic clove breaks down the compartmentalization and brings the enzyme and its substrate into contact, leading to allicin production (20,30). The potential use of pure allicin as an anti-Aspergillus agent in vivo was shown in our previous work (44). Despite its short half-life, five repetitive doses of pure allicin administered intravenously (i.v.)…”

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confidence: 99%

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Therapy of Murine Pulmonary Aspergillosis with Antibody-Alliinase Conjugates and Alliin

Appel¹,

Vallon-Eberhard²,

Rabinkov³

et al. 2010

Antimicrob Agents Chemother

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Aspergillus fumigatus is an opportunistic fungal pathogen responsible for invasive aspergillosis in immunocompromised individuals. The high morbidity and mortality rates as well as the poor efficacy of antifungal agents remain major clinical concerns. Allicin (diallyl-dithiosulfinate), which is produced by the garlic enzyme alliinase from the harmless substrate alliin, has been shown to have wide-range antifungal specificity. A monoclonal antibody (MAb) against A. fumigatus was produced and chemically ligated to the enzyme alliinase. The purified antibody-alliinase conjugate bound to conidia and hyphae of A. fumigatus at nanomolar concentrations. In the presence of alliin, the conjugate produced cytotoxic allicin molecules, which killed the fungus. In vivo testing of the therapeutical potential of the conjugate was carried out in immunosuppressed mice infected intranasally with conidia of A. fumigatus. Intratracheal (i.t.) instillation of the conjugate and alliin (four treatments) resulted in 80 to 85% animal survival (36 days), with almost complete fungal clearance. Repetitive intratracheal administration of the conjugate and alliin was also effective when treatments were initiated at a more advanced stage of infection (50 h). The fungi were killed specifically without causing damage to the lung tissue or overt discomfort to the animals. Intratracheal instillation of the conjugate without alliin or of the unconjugated monoclonal antibody significantly delayed the death of the infected mice, but only 20% of the animals survived. A limitation of this study is that the demonstration was achieved in a constrained setting. Other routes of drug delivery will be investigated for the treatment of pulmonary and extrapulmonary aspergillosis.

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Efficacy of allicin, the reactive molecule of garlic, in inhibiting Aspergillus spp. in vitro, and in a murine model of disseminated aspergillosis

Abstract: These favourable results, despite the short half-life of this compound in vivo, support further studies of controlled sustained release or more prolonged administration of allicin as a treatment for aspergillosis.

Cited by 74 publications

References 16 publications

Body Surface Changes in Gastrointestinal Helminthes Following in vitro Treatment with Allium sativum Oil

Body Surface Changes in Gastrointestinal Helminthes Following in vitro Treatment with Allium sativum Oil

Antimalarial Activity of Allicin, a Biologically Active Compound from Garlic Cloves

Therapy of Murine Pulmonary Aspergillosis with Antibody-Alliinase Conjugates and Alliin

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