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Allicin is considered responsible for most of the pharmacological activity of crushed raw garlic cloves. However, when garlic supplements and garlic foods are consumed, allicin bioavailability or bioequivalence (ABB) has been unknown and in question because allicin formation from alliin and garlic alliinase usually occurs after consumption, under enzyme-inhibiting gastrointestinal conditions. The ABB from 13 garlic supplements and 9 garlic foods was determined by bioassay for 13 subjects by comparing the area under the 32-h concentration curve of breath allyl methyl sulfide (AMS), the main breath metabolite of allicin, to the area found after consuming a control (100% ABB) of known allicin content: homogenized raw garlic. For enteric tablets, ABB varied from 36–104%, but it was reduced to 22–57% when consumed with a high-protein meal, due to slower gastric emptying. Independent of meal type, non-enteric tablets gave high ABB (80–111%), while garlic powder capsules gave 26–109%. Kwai garlic powder tablets, which have been used in a large number of clinical trials, gave 80% ABB, validating it as representing raw garlic in those trials. ABB did not vary with alliinase activity, indicating that only a minimum level of activity is required. Enteric tablets (high-protein meal) disintegrated slower in women than men. The ABB of supplements was compared to that predicted in vitro by the dissolution test in the United States Pharmacopeia (USP); only partial agreement was found. Cooked or acidified garlic foods, which have no alliinase activity, gave higher ABB than expected: boiled (16%), roasted (30%), pickled (19%), and acid-minced (66%). Black garlic gave 5%. The mechanism for the higher than expected ABB for alliinase-inhibited garlic was explored; the results for an alliin-free/allicin-free extract indicate a partial role for the enhanced metabolism of γ-glutamyl S-allylcysteine and S-allylcysteine to AMS. In conclusion, these largely unexpected results (lower ABB for enteric tablets and higher ABB for all other products) provide guidelines for the qualities of garlic products to be used in future clinical trials and new standards for manufacturers of garlic powder supplements. They also give the consumer an awareness of how garlic foods might compare to the garlic powder supplements used to establish any allicin-related health benefit of garlic.

Allicin is the main active ingredient in freshly-crushed garlic and some other allium plants, and its anticancer effect on cancers of digestive system has been confirmed in many studies. The aim of this review is to summarize epidemiological studies and in vitro and in vivo investigations on the anticancer effects of allicin and its secondary metabolites, as well as their biological functions. In epidemiological studies of esophageal cancer, liver cancer, pancreatic cancer, and biliary tract cancer, the anticancer effect of garlic has been confirmed consistently. However, the results obtained from epidemiological studies in gastric cancer and colon cancer are inconsistent. In vitro studies demonstrated that allicin and its secondary metabolites play an antitumor role by inhibiting tumor cell proliferation, inducing apoptosis, controlling tumor invasion and metastasis, decreasing angiogenesis, suppressing Helicobacter pylori , enhancing the efficacy of chemotherapeutic drugs, and reducing the damage caused by chemotherapeutic drugs. In vivo studies further demonstrate that allicin and its secondary metabolites inhibit cancers of the digestive system. This review describes the mechanisms against cancers of digestive system and therapeutic potential of allicin and its secondary metabolites.

Background: Liver cancer is associated with a high mortality rate worldwide. Hepatocellular carcinoma (HCC) constitutes a large proportion of primary liver cancers, and most of its alterations currently remain untreatable. Diallyl trisulfide (DATS), the main chemical constituent of allicin, affects tumour development by regulating cell apoptosis. Allicin-induced autophagy could contribute to apoptosis in HepG2 cells. We rigorously examined the autophagy-related mechanism of allicin-induced apoptosis in HepG2 cells. We treated HepG2 cells with DATS to explore the effect of DATS on pro-apoptotic autophagy in HepG2 cell lines and examine its specific molecular mechanism. Methods: HepG2 cells were treated with various concentrations of DATS for 24 and 48 h. Subsequently, cell viability was measured using the cell counting kit-8 (CCK-8) assay and cell clone formation assay. The HepG2 cell apoptosis was measured using Hoechst 33258 staining and western blotting. Autophagy and the AMP-activated protein kinase (AMPK)/NAD-dependent deacetylase sirtuin-1 (SIRT1) signalling pathway were detected using western blotting. Results: Our results indicated that DATS inhibited HepG2 cell growth. Moreover, the ability of DATS to promote apoptosis in HepG2 cells increased with increasing concentration. We verified the phenomenon of DATS-induced autophagy in HepG2 cells and demonstrated that DATS treatment upregulated the protein expression of LC3-II/I. By measuring the expression of potential autophagy stimulators, we documented that DATS could induce pro-apoptotic autophagy by activating the AMPK/SIRT1 signalling pathway. Conclusion: DATS induced pro-apoptotic autophagy via the AMPK/SIRT1 signalling pathway in the human HCC HepG2 cell line. Our findings further implicate allicin as a potential therapeutic agent against liver tumours in clinical settings, providing a basis for combining allicin with an autophagy agonist for treating liver cancer.

  This study aimed to explore whether allicin (ALC) and lycopene (LP) could offer protection against the harmful effects of methotrexate (MTX), a type of chemotherapy drug known for its severe side effects, on the heart of rats. In this experiment, seven groups of rats ( n  = 7) were used. The first group was given saline as a control vehicle, the second group was given ALC at a dosage of 20 mg/kg orally, the third group was given LP at a dosage of 10 mg/kg orally, and the fourth group was given MTX at a dosage of 20 mg/kg intraperitoneally on the 15 th day of the experiment. The remaining three groups received treatments, including ALC + MTX, LP + MTX, and ALC + LP + MTX. After the administration of MTX, the concentrations of serum cardiac biomarkers, such as Creatine kinase (CK), Lactate dehydrogenase (LDH), and creatine kinase-myoglobin binding (CK-MB) were found to increase. Also, MTX caused a notable rise in malondialdehyde (MDA) levels and significant declines in the levels of glutathione (GSH), superoxide dismutase (SOD), and catalase (CAT) in the heart tissues of rats. In addition, MTX caused alterations in the cardiac histopathology and enhanced the caspase-3 expression in the cardiac tissues, indicating the occurrence of apoptosis. The antioxidant properties of ALC and/or LP were effectively reduced cardiac toxicity and apoptosis induced by MTX. The administration of ALC and/or LP was found to alleviate these effects caused by MTX.

Medicinal plants have been used from ancient times for human healthcare as in the form of traditional medicines, spices, and other food components. Garlic (Allium sativum L.) is an aromatic herbaceous plant that is consumed worldwide as food and traditional remedy for various diseases. It has been reported to possess several biological properties including anticarcinogenic, antioxidant, antidiabetic, renoprotective, anti-atherosclerotic, antibacterial, antifungal, and antihypertensive activities in traditional medicines. A. sativum is rich in several sulfur-containing phytoconstituents such as alliin, allicin, ajoenes, vinyldithiins, and flavonoids such as quercetin. Extracts and isolated compounds of A. sativum have been evaluated for various biological activities including antibacterial, antiviral, antifungal, antiprotozoal, antioxidant, anti-inflammatory, and anticancer activities among others. This review examines the phytochemical composition, pharmacokinetics, and pharmacological activities of A. sativum extracts as well as its main active constituent, allicin.

Garlic (Allium sativum L.) is a widely consumed spice in the world. Garlic contains diverse bioactive compounds, such as allicin, alliin, diallyl sulfide, diallyl disulfide, diallyl trisulfide, ajoene, and S-allyl-cysteine. Substantial studies have shown that garlic and its bioactive constituents exhibit antioxidant, anti-inflammatory, antibacterial, antifungal, immunomodulatory, cardiovascular protective, anticancer, hepatoprotective, digestive system protective, anti-diabetic, anti-obesity, neuroprotective, and renal protective properties. In this review, the main bioactive compounds and important biological functions of garlic are summarized, highlighting and discussing the relevant mechanisms of actions. Overall, garlic is an excellent natural source of bioactive sulfur-containing compounds and has promising applications in the development of functional foods or nutraceuticals for the prevention and management of certain diseases.

The aim of this study was to evaluate the impact of cyanobacteria as a soil inoculant for cultivation of the medicinal plant, Allium sativum . Cyanobacterial strains isolated from the medicinal plant field were cultured in BG11/BG11° medium. Three cyanobacterial isolates, Nostoc sp. HNBGU 006 (NS-TGS), Pseudanabaena biceps (PaS-TGiS), Chroococcus turgidus (CS-TTS), were selected for in-vitro assays. Seedling growth assays were performed with A. sativum and Raphanus sativus seeds primed with different concentration of aqueous extracts prepared from these isolates. Live cell suspension of the selected cyanobacterium, NS-TGS, was inoculated in pot soil to observe the effect of cyanobacterization on growth of A. sativum . Maximum enhancement in all the growth parameters was exhibited by 1% aqueous extract of NS-TGS in comparison to control. The result of NS-TGS inoculation in pot soil revealed an increase of 54.92 % in root length, 31.28 % in shoot length, 112 % in dry weight and 50.33 % in yield. An enhancement of 84.28% in the allicin content was also recorded in cloves grown in treated soil as compared to control. There was significant enhancement in soil and leaf chlorophyll as well as soil potassium content with the highest recorded in the treatment BSI (before sowing inoculation) + ASI (after sowing inoculation). This study provides an insight to the cyanobacterization of soil with NS-TGS for the cultivation of A. sativum herb and is consistent with the sustainable agriculture approach.

Allicin, naturally present in the bulbs of the lily family, has anticancer, blood pressure lowering, blood fat lowering and diabetes improving effects. Recent studies have shown that allicin promotes the browning of white adipocytes and reduces the weight gain of mice induced by high-fat diet. While the gut microbiota has a strong relationship with obesity and energy metabolism, the effect of allicin on weight loss via gut microorganisms is still unclear. In this study, we treated obese mice induced by high-fat diet with allicin to determine its effects on fat deposition, blood metabolic parameters and intestinal morphology. Furthermore, we used high-throughput sequencing on a MiSeq Illumina platform to determine the gut microorganisms’ species. We found that allicin significantly reduced the weight gain of obese mice by promoting lipolysis and thermogenesis, as well as blood metabolism and intestinal morphology, and suppressing hepatic lipid synthesis and transport. In addition, allicin changed the composition of the intestinal microbiota and increased the proportion of beneficial bacteria. In conclusion, our study showed that allicin improves metabolism in high-fat induced obese mice by modulating the gut microbiota. Our findings provide a theoretical basis for further elucidation of the weight loss mechanism of allicin.

  The shelf life and economic value of fresh-cut garlic cloves (Allium sativum L.) are severely limited by problems such as browning, rooting, moisture loss, and microbiological spoiling. Edible coatings act as barriers to moisture loss and microbial contamination. In this research, we examined the effectiveness of an edible coating enriched with carboxymethyl cellulose (CMC) and either peppermint oil (PO) or methyl jasmonate (MeJA) on the storability and quality of ready-to-eat garlic cloves. Six treatments were used: CMC (1%), PO (0.5%), MeJA (0.5%), CMC+PO, CMC+MeJA, and a control treatment (distilled water). The garlic cloves were stored for 60 days at 5 °C and 98% relative humidity. After 60 days of storage, CMC, PO, and CMC+PO treatments emerged as the most effective at minimizing weight loss, browning, and respiration rate, and at increasing rooting percentage and length. Among these, CMC enriched with PO or MeJA also best maintained vitamin C content. Notably, all treatments enhanced the fruit's antioxidant profile, yielding elevated total phenolic compounds (TPC) and antioxidant activity relative to the control. On the other hand, all treatments showed lower polyphenol oxidase (PPO) activity relative to the control samples. The microbial counts and mold and yeast were suppressed by all treatments, except CMC, compared to the control. All treatments maintained allicin content compared to the control, with CMC+PO showing superior effects 30 days of storage and MeJA after 60 days of storage. In conclusion, extending the shelf life of garlic cloves could be achieved by employing PO and/or MeJA.

Pulmonary arterial hypertension (PAH) is characterized by pulmonary vascular remodeling. Recent evidence supports that inflammation plays a key role in triggering and maintaining pulmonary vascular remodeling. Recent studies have shown that garlic extract has protective effects in PAH, but the precise role of allicin, a compound derived from garlic, is unknown. Thus, we used allicin to evaluate its effects on inflammation and fibrosis in PAH. Male Wistar rats were divided into three groups: control (CON), monocrotaline (60 mg/kg) (MCT), and MCT plus allicin (16 mg/kg/oral gavage) (MCT + A). Right ventricle (RV) hypertrophy and pulmonary arterial medial wall thickness were determined. IL-1β, IL-6, TNF-α, NFκB p65, Iκβ, TGF-β, and α-SMA were determined by Western blot analysis. In addition, TNF-α and TGF-β were determined by immunohistochemistry, and miR-21-5p and mRNA expressions of Cd68, Bmpr2, and Smad5 were determined by RT-qPCR. Results: Allicin prevented increases in vessel wall thickness due to TNF-α, IL-6, IL-1β, and Cd68 in the lung. In addition, TGF-β, α-SMA, and fibrosis were lower in the MCT + A group compared with the MCT group. In the RV, allicin prevented increases in TNF-α, IL-6, and TGF-β. These observations suggest that, through the modulation of proinflammatory and profibrotic markers in the lung and heart, allicin delays the progression of PAH.