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Abstract

Background: Allicin is an organosulfur and defensive compound found in garlic (Allium sativum L.) and other Allium species. Its unique odor is easily detectable, and its effects on human health have been studied since ancient times. Scope and approach: In this compressive review we report the presence of allicin in different Allium species, their biosynthesis, pharmacokinetics, absorption, and safety profile. Among the main allicin applications highlight its antimicrobial and antiparasitic properties, reviewed in the present work from in vitro evidence and in vivo studies. Finally, special attention was also given to the allicin state of the art in human health, including in vitro and in vivo assays, and clinical trials, on antioxidant, anticancer, antidiabetic and immunomodulatory effects, besides to its contribution as a cardioprotective agent. Key findings and conclusions: The promising capacity of allicin to interact with thiol groups seems to be directly related to its antimicrobial potential, showing both antibacterial and antifungal activities. Allicin also displayed an interesting potential in the prevention and treatment of several diseases including diabetes mellitus, cardiovascular disease, and cancer. Indeed, its antioxidant and immunomodulatory effects are some of the mechanisms that may explain their biological activities. Future applications should be directed to allicin pharmaceutical formulation, its delivery and its compatibility with food matrices and other drugs due to allicin biosynthesis, instability, reactivity, and volatility.

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... Garlic and other Allium species contain this significant organosulfur molecule, which has a variety of biological actions including anti-viral, anti-fungal, anti-bacterial, and anti-parasitic effects. [1] Originally isolated and characterized in 1944, allicin is sulfenic acid's thioester and is now the predominant and most physiologically active organosulfur component in garlic. The chemical allicin has a characteristic smell that is weakly dissolved in water and is reminiscent of freshly crushed garlic. ...
... The overlay spectra for the same is shown in Figure 4 The absorptivity values of both the herbal extracts was determined at 273 and 257 nm. Using those values, two simultaneous equations were formed wherein equation (1) and equation (2) Concentrations of both the extracts in the niosomal formulations can be calculated by decoding equations (1) and (2). Reliability of the equations was verified by using standard solution containing mixture of original samples of both the extracts, determining their absorbance at the taken wavelengths and computing concentration of both the constituents. ...
... Garlic extract (GE) has been shown to inhibit the growth of various foodborne pathogens, including Escherichia coli, Salmonella enterica, and Staphylococcus aureus. Its abundance and low cost make garlic an economically viable natural resource for food packaging (Salehi et al., 2019). Therefore, developing garlic-based additives for food packaging is a promising area of research that could provide sustainable solutions for the food industry. ...
... The nutrient content and chemical substances in GE were identified through GC-MS analysis, as presented in Table 2. This analysis unveiled a diverse range of nutrients and chemical substances in GE, including sulfur compounds renowned for their anti-inflammatory properties and ability to scavenge free radicals (Marchese et al., 2016;Mocayar Marón et al., 2020;Salehi et al., 2019). Moreover, GE's array of vitamins and minerals offers various benefits as essential nutrients for different products, thereby enhancing its value as an additive agent in the food packaging industry. ...
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In this study, garlic extract (GE) was assessed as a potential additive in chitosan/starch (Ch/De) coatings, focusing on phenolic and flavonoid content analyses and antibacterial properties. Using response surface methodology approach, an optimization method was employed to achieve the optimal antibacterial formulation, with Ch, De, and GE identified as key variables in the Design of Experiment. Fourier transform infrared spectroscopy and X‐ray diffraction analyses elucidated interactions among these primary components within the films, while thermogravimetric analysis confirmed the enhanced thermal stability of GE‐coated film formulations (Ch/De/GE). The Ch/De/GE exhibited antibacterial efficacy against Escherichia coli (ATCC 25922) with an inhibition zone of 7.2 mm at optimized concentrations of 2% w/v Ch, 1.5% w/v starch, and 0.5% v/v GE. In silico molecular docking studies provided insights into GE's inhibitory role as an antibacterial agent. Evaluation of green and yellow bell peppers (Capsicum annuum) over 18 days showed that coated peppers maintained better visual appearance and mass stability, with a weight loss decrease of 40.54%–48.96%, compared to uncoated ones. Additionally, the Ch/De/GE coating effectively inhibited bacterial growth, reducing it by 1–1.23 log CFU, during the storage period. In conclusion, the Ch/De/GE coating effectively extends the shelf‐life of bell peppers and maintains their quality, demonstrating its potential for use in food packaging to preserve perishable items. Practical Application The optimized chitosan/starch/garlic extract (Ch/De/GE) film developed in this study shows promising potential for application in the food packaging industry, particularly in extending the shelf life of perishable items like bell peppers. Its enhanced antibacterial properties, along with its ability to maintain visual appearance and reduce weight loss, make it an effective natural preservative that could replace synthetic additives in food packaging. By incorporating this biodegradable film into packaging solutions, producers can offer safer, more sustainable products that meet consumer demand for natural and environmentally friendly options.
... vineale L.), and alpine leek (A. victorialis L.) [127]. Allicin is a colorless oil that has poor solubility in water, which accounts for its ability to pass easily through cell membranes [128]. ...
... After its formation, it rapidly breaks down into various secondary compounds, influenced by factors such as temperature and pH [129]. Besides its contribution as a promising anticancer agent, allicin has demonstrated several therapeutic properties, including cardiovascular protection, blood pressure-lowering, antioxidant, antimicrobial, anti-asthmatic, and immunoregulatory benefits [127]. ...
Article
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Cancer continues to be a prominent issue in healthcare systems, resulting in approximately 9.9 million fatalities in 2020. It is the second most common cause of death after cardiovascular diseases. Although there are difficulties in treating cancer at both the genetic and phenotypic levels, many cancer patients seek supplementary and alternative medicines to cope with their illness, relieve symptoms, and reduce the side effects of cytotoxic drug therapy. Consequently, there is an increasing emphasis on studying natural products that have the potential to prevent or treat cancer. Cancer cells depend on multiple hallmarks to secure survival. These hallmarks include sustained proliferation, apoptosis inactivation, stimulation of angiogenesis, immune evasion, and altered metabolism. Several natural products from food were reported to target multiple cancer hallmarks and can be used as adjuvant interventions to augment conventional therapies. This review summarizes the main active ingredients in food that have anticancer activities with a comprehensive discussion of the mechanisms of action. Thymoquinone, allicin, resveratrol, parthenolide, Epigallocatechin gallate, and piperine are promising anticancer bioactive ingredients in food. Natural products discussed in this review provide a solid ground for researchers to provide effective anticancer functional food.
... Allicin ( Figure 3) is an alliin precursor, the main thiosulfinate found in garlic, and is responsible for garlic's specific odor. Due to the presence of sulfur groups, and the oxidizing effect, it can react with thiols (-SH) from proteins, leading to various biological effects [86]. ...
... As mentioned earlier, its chemical structure allows it to interact with thiol groups from proteins and glutathione from bacteria and fungi. Allicin inhibits glutathione and disrupts the redox balance, causing oxidative stress that damages the cellular components, impairs cell cycle progression, and ultimately leads to cell death [86,88,89]. The mechanism underlying the antiviral activity of allicin occurs by disrupting the viral envelope and cell membrane. ...
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Natural compounds have been used since the earliest civilizations and remain, to this day, a safer alternative for treating various dental problems. These present antimicrobial, anti-inflammatory, antioxidant, analgesic, and antimutagenic effects, making them useful in the prophylactic and curative treatment of various oral diseases such as infections, gingivitis, periodontitis, and even cancer. Due to the high incidence of unpleasant adverse reactions to synthetic compounds, natural products tend to gradually replace conventional treatment, as they can be just as potent and cause fewer, milder adverse effects. Researchers use several methods to measure the effectiveness and safety profile of these compounds, and employing standard techniques also contributes to progress across all medical disciplines.
... This may be due to potential biological and pharmaceutical effects including antioxidant, antibacterial and antiviral impacts. Allicin is an unstable, volatile, and cytotoxic liposoluble organosulfur compound [69]. With antiseptic, antiviral, antifungal, anti-parasitic, and antibacterial effects, it is also GE's most significant active ingredient [70]. ...
... Several thiosulfinates, including allicin, are thought to be responsible for GE's therapeutic effects in the treatment of monogenetic infection brought on by Dactylogyrus spp [75,76]. Pathways involving interferon-gamma, tumor necrosis factor, interleukin (IL-12P70), and T-cells, enhance the host immunological response [69]. Moreover, organosulfur, polysaccharide, and fructan substances are responsible for GE's immune stimulatory affects [77] a rise in the number of lymphocytes in the blood. ...
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Background Gills monogenean infestation causes significant mortalities in cultured fishes as a result of respiratory manifestation. Medicinal plants are currently being heavily emphasized in aquaculture due to their great nutritional, therapeutic, antimicrobial activities, and financial value. Methods The current study is designed to assess the effect of garlic (Allium sativum) and onion (Allium cepa) extracts as a water treatment on the hematological profile, innate immunity, and immune cytokines expression besides histopathological features of gills of Nile tilapia (Oreochromis niloticus L.) infected with gills monogenetic trematodes (Dactylogyrus sp.). Firstly, the 96-hour lethal concentration 50 (96 h-LC50) of garlic extract (GE) and onion extract (OE) were estimated to be 0.4 g/ L and 3.54 g/ L for GE and OE, respectively. Moreover, the in-vitro anti-parasitic potential for (GE) was found between 0.02 and 0.18 mg/mL and 0.4 to 1.8 mg/mL for OE. For the therapeutic trial, fish (n = 120; body weight: 40–60 g) were randomly distributed into four groups in triplicates (30 fish/group, 10 fish/replicate) for 3 days. Group1 (G1) was not infected or treated and served as control. G2 was infected with Dactylogyrus spp. and not exposed to any treatment. G3, G4 were infected with Dactylogyrus sp. and treated with 1/10 and 1/5 of 96 h LC50 of OE, respectively. G5, G6 were infected with Dactylogyrus sp. and treated with 1/10 and 1/5 of 96 h LC50 of GE, respectively. Results No apparent signs or behaviors were noted in the control group. Dactylogyrus spp. infected group suffered from clinical signs as Pale color and damaged tissue. Dactylogyrus spp. infection induced lowering of the hematological (HB, MCH, MCHC and WBCs), and immunological variables (lysozyme, nitric oxide, serum Anti- protease activities, and complement 3). the expression of cytokine genes IL-ß and TNF-α were modulated and improved by treatment with A. sativum and A. cepa extracts. The obtained histopathological alterations of the gills of fish infected with (Dactylogyrus spp.) were hyperplasia leading to fusion of the gill filament, lifting of epithelial tissue, aneurism and edema. The results indecated that G4 and G5 is more regenarated epithelium in compare with the control group. Conclusion A. sativum and A. cepa extracts enhance the blood profile and nonspecific immune parameters, and down-regulated the expression level of (IL-1β and TNF-α).
... Sulphur component of allicin formed disulphides bond (Kyung 2012) with the other Sulphur containing amino acid in animals' body that helps to inhibit the growth of microorganism by damaging the cell membrane of microorganism and enter into the cellular components of bacteria and inhibit the activity of thiol group (Leontiev et al. 2018;Salehi et al. 2019). Allicin also inhibit the growth by damaging DNA and RNA synthesis (Feldberg et al. 1988). ...
... The activity of Vitamin C is an immunomodulator is proved first time in this study by examining the sera sample on the generation of in support of inflammatory cytokines in both healthy and contaminated limb due to P. multocida. Vitamin C has also contained immunostimulant activity to increase the level of Tlymphocytes and also inhibits the death of T-cells by signaling pathway (Jeng et al.1996;Naidu 2003;Campbell et al. 1999;Salehi et al. 2019). In-vitro and in-vivo, Vitamin C inhibited the replication of P. multocida by resisting the expression of virulence factor of this bacteria. ...
... C. zedoaria has been reported to have anti-inflammatory properties (Rahaman et al., 2021), in addition to antifungal and antimicrobial activities (Chachad et al., 2016;Gharge et al., 2021). A. sativum contains highly reactive organic sulfur compounds that exhibit strong antimicrobial activities against both gram-positive and gram-negative bacteria even at low concentrations (Salehi et al., 2019). The antimicrobial properties of garlic also include antifungal and antiviral activities, which can be attributed primarily to its sulfur derivatives, including allicin (Bhatwalkar et al., 2021). ...
Article
The production of shrimp has been challenged by various factors such as diseases. Therefore, the health of cultured shrimp is essential for successful farming practices. The application of medicinal plants brings about numerous benefits in aquaculture including simplicity in usage, biodegradability, and minimal environmental impact over extended periods. This study was conducted to evaluate the efficacy of E. longifolia, C. zedoaria, and A. sativum to improve the immune response and resistance of vannamei shrimp as an effort to prevent Vibrio parahaemolyticus infection. The study consised of two phases: an in vitro phase to determine the compounds contained in three medicinal plants as antibacterials followed by an in vivo phase to evaluate the effect of the medical plants extract on immune response, and robustness against V. parahaemolyticus. The results from the first phase revealed that bioactive compounds present in EL16 were more varied and had higher concentrations with a lower bactericidal values when compared to those found in AS64 or CZ64. On the second phase of the experiment, the medicinal plant extract was added into the feed with a dose that was determined according to the first phase results. The treatments tested in the second phase were 1.6% E. longifolia extract dietary addition (EL16), 6.4% C. zedoaria extract dietary addition, 6.4% A. sativum extract dietary addition and phytobiotics mixture of 1:1:1 (C1) dietary addition, as well as no phytobiotic for negative control treatment and positive control. The results from the second stage demonstrated that dietary phytobiotic extracts addition enhances the immunological responses and improved the shrimp survival against V. parahaemolyticus challenge compared to the control group. In conclusion, E. longifolia, C. zedoaria, and A. sativum showed different bioactive compound profiles which affect its efficacy against V. parahaemolyticus both in vitro and in vivo, with EL16 showed higher efficacy.
... Because allicin is quite lipophilic, it alters the phospholipid membranes of microorganisms, which is likely what causes cellular content leakage [21]. The present study also agreed with Alli et al. [22], who reported high antibacterial activity of garlic on S. aureus and P. aeruginosa. ...
... The medicinal properties of garlic are primarily due to its organosulfur compounds (OSCs), such as alkenyl-cysteine sulfoxides, polysulfides, ajoenes, and vinyldithiins. These compounds exhibit various health-promoting effects, including anticancer, antimicrobial, antifungal, antioxidant, antidiabetic, blood-pressure-lowering, and immune-enhancing activities [2,3]. Despite these benefits, the strong odor and taste of garlic-largely attributed to its OSCs-often discourage consumption. ...
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This study investigates the effects of different temperature conditions on the quality of black garlic (BG) during the aging process. Two temperature protocols were employed: gradual heating and cooling (GHC), where the temperature was slowly raised from 45 °C to 77 °C and then lowered to 59 °C at a rate of 1 °C per hour, and rapid heating and cooling (RHC), where the temperature was quickly raised from 45 °C to 85 °C and then lowered to 56 °C at a rate of 1 °C every 30 min. Changes in surface color, hardness, moisture, pH, fructose, total polyphenol content (TPC), and key sulfur compounds such as alliin, S-allylcysteine (SAC), and γ-glutamyl-S-allylcysteine (γ-GSAC) were analyzed. Our findings showed that GHC led to a higher increase in TPC and fructose content by the 15th day compared to RHC. In contrast, RHC retained significantly higher SAC concentrations, approximately 1.7 times that of GHC, by the end of the aging period. Surface color changes, particularly in lightness and redness, were more pronounced under GHC, while RHC demonstrated superior moisture retention. These findings indicate that GHC is better suited for products prioritizing polyphenols and sugars, while RHC is more optimal for SAC-enriched BG. This study provides valuable insights into optimizing BG production for diverse food and medicinal applications through precise temperature modulation.
... Acetogenin compounds are compounds associated with neurodegeneration, with a mechanism of action similar to rotenone, a specific inhibitor of mitochondrial complex I (i.e., decreased OXPHOS, and ATP depletion) (Gaetano et al., 2021). The content of allisin, resulting from the mixture of aliin and alliinase compounds, allisin compounds are compounds that can be used as protective compounds that have a mode of action by activating transient receptor potential ankyrin 1 (TRPA1) and transient receptor potential cation channel subfamily V member 1 (TRPV1) which are excitatory ion channels in the main sensory neurons of the pain pathway, thus causing pain and inflammation in predatory animals (Salehi et al., 2019). ...
Article
Pest attacks on plants are the most common problem faced by farmers. One type of pest that most often attacks plants with hydroponic methods is the Aphis gossypii pest. Seeing this, an innovation must be developed in controlling pests that are more environmentally friendly. This study aimed to determine how influential the use of shallot and garlic skin baths as pest control in hydroponic Brassica rapa L. plants with concentrations of 25%, 50%, and 75%. This research is an experimental study in which the data obtained is processed using the ANOVA method. The results of the study based on the data processing results showed that there was less visible difference between the three treatments given for four weeks of treatment. So, it can be in the application of natural pesticides, which can be given in the first week with a concentration of 25%, in the second week 50%, and in the third week and fourth week 75%.
... The high antibacterial activity of onion against E. coli can be attributed to its rich content of organo-sulfur compounds such as allicin, which have been documented to possess significant antimicrobial properties. Allicin disrupts bacterial cell walls and interferes with their enzyme systems, leading to bacterial cell death (Borlinghaus et al. 2021;Salehi et al. 2019 sativa) was used with a mordant, the increase in antibacterial resistance against S. aureus can be due to the combined effect of thymoquinone, an active compound in black seed known for its potent antibacterial properties, and the mordant which may enhance the binding and efficacy of the antibacterial agents on the fabric surface (Shahid-ul-Islam and Mohammad 2015; Yıldırım et al. 2020). The mordant possibly helps in better adhesion and sustained release of active compounds, thereby improving antibacterial activity. ...
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Textile products often serve as breeding grounds for microorganisms, posing significant health and hygiene concerns. In response, there is a growing demand for textile products with antimicrobial properties. This research work aims to develop antimicrobial textile products sustainably using natural ingredients such as onion (Allium cepa), ginger (Zingiber officinale) and black seed (Nigella sativa). Fabrics were dyed using an exhaust method with cutch (Senegalia catechu), as a mordanting agents and binders utilized for fixation for 90 min at 60ºC. Extracts were directly incorporated into the dye bath. After dyeing, the samples were fixed by different fixation processes and their antibacterial activity against four bacterial strains was examined using the disc diffusion method (AATCC 147). In addition, the dyed materials were subjected to wash and rubbing fastness tests to confirm their resilience. Results indicated that samples treated with onion had an antibacterial activity of 25.95 mm against Escherichia coli bacteria and 23.06 mm against Staphyloccus aureus bacteria. Besides, samples fixed by a combination of compounds manifested strong antimicrobial resistance.
... Varios autores han descrito la presencia de compuestos órgano-sulfurados en el ajo. La alicina es el compuesto bioactivo principal del ajo y representa entorno al 70-80% del contenido total de azufre orgánico (Salehi et al., 2019). Sin embargo, otros autores identificaron la cicloaliína como componente principal órganosulfurado (Moreno-Ortega et al., 2020). ...
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El destete es una de las etapas más críticas en la producción porcina, con frecuentes diarreas. Se ha utilizado ampliamente el óxido de Zinc (ZnO), hasta su prohibición en Europa en 2022. Los compuestos bioactivos del orégano y el ajo morado fueron investigados por sus propiedades medicinales, y podrían ser alternativas al ZnO y a los antibióticos. Se compararon siete tratamientos dietéticos: un grupo control negativo (dieta basal), un grupo control positivo con ZnO (2500 mg/kg de alimento), dos grupos con aceite esencial de orégano al 0.4% y al 1.2% respectivamente, dos grupos con moltura de ajo morado al 0.4% y al 2% respectivamente, y un grupo con aceite esencial de orégano al 1.2% combinado con moltura de ajo morado al 2%. Los tratamientos se realizaron tras el destete a los 21 días, durante 2 semanas en el pre- estárter y durante 5 semanas en el estárter. Al finalizar las 10 semanas, los lechones se pesaron y se realizó la necropsia para tomar muestras de yeyuno e íleon y evaluar su morfometría. Hemos estudiado el impacto de la degradación de los nutracéuticos durante su almacenamiento en los silos, así como su repercusión sobre la morfometría del yeyuno e íleon y su influencia en la ganancia media diaria y el índice de conversión. Al evaluar la degradación de los compuestos bioactivos en los piensos, almacenados durante 5 semanas, se identificó una pérdida del 30% tanto en el orégano como en el ajo morado. No obstante, no hubo diferencias significativas en el rendimiento productivo y la morfometría intestinal entre el tratamiento con ZnO y el combinado de moltura de ajo morado al 2% y el aceite esencial de orégano al 1.2%. En conclusión, estas dosis son una buena alternativa como promotores del crecimiento y para la prevención de la diarrea post- destete.
... is released, converting alliin into allicin (7). Allicin is the primary bioactive compound in garlic, accounting for 70 -80 % of its sulfur compounds and responsible for the characteristic garlic odor (8). Additionally, a diverse array of sulfur-based active compounds has been identified in garlic, including allicin, alliin, S-allylcysteine, diallyl disulfide, diallyl trisulfide, diallyl sulfide and ajoene (9). ...
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Garlic (Allium sativum L.) has been widely studied for its insecticidal properties. The primary bioactive molecule in garlic extracts include allicin, alliin, S-allylcysteine, diallyl disulfide, diallyl trisulfide, diallyl sulfide and ajoene. However, these compounds degrade under environmental conditions once extracted. This study aimed to enhance the effectiveness of garlic extracts in controlling Tenebrio molitor by optimizing microencapsulation techniques. The garlic extracts were encapsulated using the complex coacervation method, with independent variables including pH levels (3, 6 and 9), whey protein isolate (WPI) (4 %, 6 % and 8 % w/v) and pectin (0.50 %, 0.75 % and 1.00 % w/v). A Taguchi L9 (33) orthogonal array was employed to design 9 treatments, and T. molitor mortality was assessed 72 h after a 10 sec immersion of the insects in the treatments. Statistical analysis revealed that WPI had the most significant influence (24.52 %), followed by pH (18.82 %) and pectin (7.79 %). The interaction between pH and pectin had the greatest effect on the encapsulation process, accounting for 38.65 % of the influence. The optimal microencapsulation conditions were predicted by software to be pH 3, a pectin concentration of 0.75 % w/v and a WPI concentration of 4.00 % w/v, resulting in a signal-to-noise (S/N) ratio of 42.30. Experimental validation of these conditions produced an S/N ratio of 18.54, corresponding to a T. molitor mortality rate of 92 % ± 4.47 %. The resulting microcapsules had diameters ranging from 1–5 ?m. Complex coacervation is a highly promising method for microencapsulating garlic extracts and preserving their insecticidal properties.
... Alliin is generally known for its health benefits, such as improved glucose tolerance in mice and anti-inflammatory effects in rats and in vitro studies. 52,53 Interestingly, the NAT8 locus was found to be associated with the odds of missingness of alliin. A previous study reported another SNP in NAT8 to be associated with the acylated form of alliin-N-acetylalliin. ...
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Metabolomic studies are increasingly used for both etiological and predictive research, but frequently report missing values. We hypothesized that interindividual genetic variation may account for part of this missingness. Therefore, we performed a GWAS of missingness in measured metabolite levels using an untargeted mass spectrometry-based platform in the Netherlands Epidemiology of Obesity Study (N=594) and the Rhineland Study (N=4,165). We considered metabolites missing in 10%-90% of individuals in both cohorts (N=224). GWAS meta-analyses of these metabolites' probability of missingness revealed 55 metabolome-wide significant associations, including 42 novel ones (p<1.58x10-10), involving 28 metabolites and 41 lead SNPs. Despite considerable pleiotropy, the majority of identified SNP-"missing metabolite" associations were biologically plausible, relating to beta-oxidation, bile acids, steroids, and xenobiotics metabolism. These findings suggest that missing values in metabolomics are nonrandom and partly reflect genetic variation, accounting for which is important for both clinical and epidemiological studies, especially nutritional and pharmacogenetics studies.
... Allicin, the primary bioactive component of garlic, is well-documented for its antibacterial, antiparasitic, and antifungal properties [94]. It has the potential to reduce intestinal inflammation and exert an inhibitory immunomodulatory effect on intestinal epithelial cells [95]. Arreola, et al. [96] further suggested that Allium species enhance immune activities, including phagocytosis, cytokine release, natural killer cell activity, and lymphocyte synthesis. ...
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This study investigated the effects of dietary garlic powder and fermented garlic powder supplementation at 1% and 2% levels on growth performance, digestive tract efficacy, blood biochemistry, immunity, and antioxidant status of Liza ramada (n=225 fish; 86.00±0.42 g) over a 60-day period. Fish fed diets supplemented with both forms of garlic at both levels exhibited significantly improved final body weight, weight gain, specific growth rate, and feed conversion ratio compared to the control group. Digestive enzyme activities (amylase, lipase, and protease) were significantly enhanced in all supplemented groups. Blood biochemical analysis revealed reduced glucose levels and increased total protein in garlic-supplemented groups, with no adverse effects on liver or kidney function markers. Immune parameters, including lysozyme activity, bactericidal activity against Streptococcus agalactiae, alternative complement pathway (ACP), and respiratory burst (NBT), were significantly enhanced in garlic-supplemented groups, with fermented garlic showing more pronounced effects. Antioxidant enzyme activities (SOD, CAT, and GPx) were also significantly increased in all supplemented groups, particularly in those fed fermented garlic. No significant differences in survival rates were observed among treatments. The results suggest that both garlic powder and fermented garlic powder supplementation, especially at the 2% level, can effectively improve growth, feed utilization, immune function, and antioxidant status in L. ramada. Fermented garlic generally demonstrated superior effects, indicating its potential as a beneficial feed additive in aquaculture. Based on these findings, it is recommended to incorporate fermented garlic powder at a 2% level in L. ramada diets to optimize growth performance and health status. Further research is warranted to investigate the long-term effects and cost-effectiveness of this supplementation strategy in commercial aquaculture settings.
... Alliin is a non-protein amino acid and an important precursor for the synthesis of Allicin, a sulfur-containing compound derived from garlic. Numerous studies have demonstrated that Allicin is a neuroprotective agent [37,38]. Neuroinflammation can be suppressed by inhibiting brain inflammation factors and the activation of microglial cells [39]. ...
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Background This study aims to investigate the causal relationship of human plasma metabolites and metabolic ratios with schizophrenia (SCZ). Methods We employed Mendelian Randomization (MR) approach to comprehensively analyze two large-scale metabolomics and schizophrenia Genome-Wide Association Study (GWAS) datasets, incorporating a total of 1091 metabolites and 309 metabolic ratios, with 52017 schizophrenia patients and 75889 healthy controls. The inverse variance-weighted (IVW) method was utilized to estimate the causal relationship between exposure and outcome. To provide a more comprehensive evaluation, additional Mendelian Randomization (MR) approaches were employed, including MR-Egger regression, weighted median, simple mode, and weighted mode methods. These analyses assessed the causal effects between blood metabolites, metabolic ratios, and schizophrenia. Tests for pleiotropy and heterogeneity were conducted. False Discovery Rate (FDR) correction was applied to account for multiple comparisons and heterogeneity, ensuring the robustness and reliability of our findings. Consistent with previous studies, an FDR threshold of < 0.2 was considered suggestive of a causal relationship, while an FDR of < 0.05 was considered to indicate a significant causal relationship. Results The final results revealed that a significant causal association was found between the levels of two metabolites and schizophrenia, Alliin (OR = 0.915, 95%CI = 0.879–0.953, P = 1.93 × 10− 5, FDR = 0.013) was associated with a decreased risk of schizophrenia, N-actylcitrulline (OR = 1.058, 95%CI = 1.034–1.083, P = 1.4 × 10− 6, FDR = 0.002) was associated with increased risk of schizophrenia. When adjusting FDR to 0.2, the results showed that 4 metabolite levels and 2 metabolite ratios were suggestively causally associated with a reduced risk of schizophrenia including 2-aminooctanoate (OR = 0.904, 95%CI = 0.847–0.964, P = 0.002, FDR = 0.160), N-lactoylvaline (OR = 0.853, 95%CI = 0.775–0.938, P = 0.001,FDR = 0.122), X − 21310 (OR = 0.917, 95%CI = 0.866–0.971, P = 0.003,FDR = 0.195), X − 26111 (OR = 0.932, 95%CI = 0.890–0.976, P = 0.003,FDR = 0.189), Arachidonate (20:4n6) to oleate to vaccenate (18:1) ratio (OR = 0.945, 95%CI = 0.914–0.977, P = 8.2 × 10− 4, FDR = 0.104), and Citrulline to ornithine ratio (OR = 0.924, 95%CI = 0.881–0.969, P = 0.001, FDR = 0.122), while 4 metabolite levels and 2 metabolite ratios were suggestively causally associated with an increased risk of schizophrenia including N2, N5-diacetylornithine (OR = 1.090, 95%CI = 1.031–1.153, P = 0.003, FDR = 0.185), N − acetyl − 2−aminooctanoate (OR = 1.069, 95%CI=(1.027–1.114, P = 0.001, FDR = 0.127), N − acetyl − 2−aminoadipate (OR = 1.081, 95%CI = 1.030–1.133, P = 0.001, FDR = 0.128), X − 13844 (OR = 1.110, 95%CI = 1.036–1.190, P = 0.003, FDR = 0.196), X − 24556 (OR = 1.083, 95%CI = 1.036–1.132, P = 4.5 × 10− 4, FDR = 0.098), X − 24736 (OR = 1.065, 95%CI = 1.028–1.104, P = 5.6 × 10− 4, FDR = 0.098), N − acetylasparagine (OR = 1.048, 95%CI = 1.021–1.075, P = 4.5 × 10− 4, FDR = 0.098), N − acetylarginine (OR = 1.060, 95%CI = 1.028–1.092, P = 1.8 × 10− 4, FDR = 0.083), Cysteine to alanine ratio (OR = 1.086, 95%CI = 1.036–1.138, P = 6.5 × 10− 4, FDR = 0.101), and Benzoate to linoleoyl − arachidonoyl − glycerol (18:2 to 20:4) ratio (OR = 1.070, 95%CI = 1.025–1.117, P = 0.002, FDR = 0.158). Conclusion Our study results provide valuable insights for identifying diagnostic biomarkers related to schizophrenia and offer preliminary research findings for further exploration of the mechanisms linking schizophrenia and metabolism.
... Allicin, an organosulfur compound predominantly present in garlic (Allium sativum L.) and other Allium species, has garnered significant interest in recent times due to its numerous advantageous attributes, particularly in the fields of medicine and agriculture (Jess et al. 2017;Salehi et al. 2019;Ayman et al. 2022). Several studies have demonstrated the repellent, growth inhibitory, and toxic effects of allicin on pests (Kimbaris et al. 2009;Yang et al. 2012;Ma et al. 2016). ...
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Plant secondary metabolites are crucial in affecting the interactions between insect herbivores and entomoviruses. However, there is limited knowledge regarding the impact of such metabolites on the susceptibility of insect herbivores to entomoviruses. In this study, we adopted the allicin, caterpillars (Spodoptera exigua) and nucleopolyhedrovirus (SeMNPV) as a system, and found that allicin significantly increased the mortality of S. exigua larvae infected with SeMNPV by 36.03–59.45% when infected with the virus at a concentration of 2.12 × 10³ OB·mL⁻¹. Furthermore, NPV-infected larvae together treated with allicin inhibited the growth and development of larvae, comparing to individual NPV-infected larvae. Notably, we observed a significant enrichment of differentially expressed genes involved in the cytochrome P450-mediated metabolism pathway between the NPV-infected and allicin combined with NPV-treated groups. The silencing of CYP340AA1 through RNA interference significantly increased the mortality of larvae infected with SeMNPV. This investigation indicates that allicin might be a potential candidate for improving the performance of the NPV against insect herbivores and identifies that CYP340AA1 gene is important in this process.
... Allicin, the primary bioactive component of garlic, is well-documented for its antibacterial, antiparasitic, and antifungal properties [95]. It has the potential to reduce intestinal inflammation and exert an inhibitory immunomodulatory effect on intestinal epithelial cells [96]. Arreola, et al. [97] further suggested that Allium species enhance immune activities, including phagocytosis, cytokine release, natural killer cell activity, and lymphocyte synthesis. ...
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This study investigated the effects of dietary garlic powder and fermented garlic powder supplementation at 1% and 2% levels on growth performance, digestive tract efficacy, blood biochemistry, immunity, and antioxidant status of Liza ramada (n=225 fish; 86.00±0.42 g) over a 60-day period. Fish fed diets supplemented with both forms of garlic at both levels exhibited significantly improved final body weight, weight gain, specific growth rate, and feed conversion ratio compared to the control group. Digestive enzyme activities (amylase, lipase, and protease) were significantly enhanced in all supplemented groups. Blood biochemical analysis revealed reduced glucose levels and increased total protein in garlic-supplemented groups, with no adverse effects on liver or kidney function markers. Immune parameters, including lysozyme activity, bactericidal activity against Streptococcus agalactiae, alternative complement pathway (ACP), and, respiratory burst (NBT) were significantly enhanced in garlic-supplemented groups, with fermented garlic showing more pronounced effects. Antioxidant enzyme activities (SOD, CAT, and GPx) were also significantly increased in all supplemented groups, particularly in those fed fermented garlic. No significant differences in survival rates were observed among treatments. The results suggest that both garlic powder and fermented garlic powder supplementation, especially at the 2% level, can effectively improve growth, feed utilization, immune function, and antioxidant status in L. ramada. Fermented garlic generally demonstrated superior effects, indicating its potential as a beneficial feed additive in aquaculture. Based on these findings, it is recommended to incorporate fermented garlic powder at a 2% level in L. ramada diets to optimize growth performance and health status. Further research is warranted to investigate the long-term effects and cost-effectiveness of this supplementation strategy in commercial aquaculture settings
... In both in vivo and in vitro settings, allicin has been demonstrated to suppress the proliferation of cancer cells [23]. Cha et al. [24] studied that Human glioma cells (U87MG) showed dose-and time-dependent inhibition of cell viability and induction of apoptosis by allicin. ...
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According to the World Health Organization, cancer is the foremost cause of mortality globally. Various phytochemicals from natural sources have been extensively studied for their anticancer properties. Allicin, a powerful organosulfur compound derived from garlic, exhibits anticancer, antioxidant, anti-inflammatory, antifungal, and antibacterial properties. This review aims to update and evaluate the chemistry, composition, mechanisms of action, and pharmacokinetics Allicin. Allicin has garnered significant attention for its potential role in modulating Fas-FasL, Bcl2-Bax, PI3K-Akt-mTOR, autophagy, and miRNA pathways. At the molecular level, allicin induces the release of cytochrome c from the mitochondria and enhances the activation of caspases-3, -8, and -9. This is accompanied by the simultaneous upregulation of Bax and Fas expression in tumor cells. Allicin can inhibit excessive autophagy by activating the PI3K/Akt/mTOR and MAPK/ERK/mTOR signaling pathways. Allicin-loaded nano-formulations efficiently induce apoptosis in cancer cells while minimizing toxicity to normal cells. Safety and clinical aspects are meticulously scrutinized, providing insights into the tolerability and adverse effects associated with allicin administration, along with an overview of current clinical trials evaluating its therapeutic potential. In conclusion, this review underscores the promising prospects of allicin as a dietary-derived medicinal compound for cancer therapy. It emphasizes the need for further research to elucidate its precise mechanisms of action, optimize delivery strategies, and validate its efficacy in clinical settings.
... Apigenin, a dietary flavonoid found in vegetables like Parsley, Chamomile, Celery, Vine spinach, Artichoke and Oregano is known for its anti-inflammatory, antidiabetic, anticancerous, chemoprevention, blood pressure reduction, and potential reduction in Alzheimer's disease, amnesia, and depression (Salehi et al., 2019). ...
... It has also played a significant role in various traditional healing practices (Sayed, 2023). Its therapeutic benefits of A. sartivum are largely due to allicin, its primary active compound, and related derivatives (Salehi et al., 2019). Traditionally, A. sativum has been used to manage conditions like high blood pressure, high cholesterol, and coronary artery disease (Alali et al., 2017). ...
... Volatile sulfur compounds have sturdy antioxidant properties and antimicrobial, antiinflammatory, and anti-cancer effects (Salehi et al., 2019). In A. sativum essential oil, the main components were diallyl trisulfide (41.62%), diallyl disulfide (19.74%), allyl methyl trisulfide (12.95%), diallyl sulfide (7.1%), and diallyl tetrasulfide (4.22%). ...
... Acetate kinase and phosphotransacetylase are required for the formation of acetyl-CoA, which has been demonstrated to be blocked by allicin. Other ways that allicin works include blocking acetyl-CoA synthetases and starting glutathione oxidation, which affects cellular redox potential and causes changes in immune cell activity, stimulation of apoptosis, membrane disruption that causes cellular content leakage, inhibition of spore germination, and inhibition of fungal hyphal mycelial growth (Salehi et al., 2019). Gram-negative bacteria like Bacillus species and Streptococcus species and Gram-positive bacteria like Salmonella species, Agrobacterium tumefaciens, Escherichia coli K12, Vibrio cholera, and Pseudomonas syringae (different pathovars) can both be inhibited by allicin (Y. ...
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... 44,45 We can also mention the diaryleptanoid curcumin 4 (Table 1) from turmeric (Curcuma longa); the phenylpropanoid eugenol 1 (Table 1), isolated from clove oil (Syzygium aromaticum); in addition to allicin 11 (Table 1), a sulfur substance found in garlic (Allium sativum L.). [46][47][48][49] Several scientists study what is called in the literature "Darwinian gastronomy", such as the study based on the 1998 survey done by biologists Billing and Sherman. 50 These authors discuss the evolution in the use of condiments in different cultures as an empirical strategy to avoid foodborne diseases, most often infections and/or poisonings caused by contamination by microorganisms, mainly fungi and bacteria. ...
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Natural products have long been explored in the history of most cultures worldwide. They have been mainly applied in the therapy of some diseases and for food preservation due to the antimicrobial properties of some condiments. Most of this knowledge was empirically discovered and passed from generation to generation. Over the last few years, the evolution of organic chemistry and the techniques of analysis and purification of compounds from complex matrices enabled a significant increase in research to identify bioactive products isolated from plants. In this paper, we briefly discuss the relevance of natural products on drug development, mainly focusing on amide piperine, the main chemical constituent of black pepper (Piper nigrum). Its antiparasitic activities and the knowledge of possible mechanisms of action against different parasites provide essential information for drug development. Furthermore, its compatibility with medicinal and synthetic chemistry techniques allows the development of more effective drug candidates.
... Researchers have observed that garlic has many benefits of Garlic has been shown by researchers to offer a wide range of biological effects, including anti-microbial, anti-inflammatory, anti-atherosclerotic, anti-diabetic, anti-mutagenic, anti-carcinogenic, antioxidant, and immune-modulating actions. biological functions, such as anti-microbial, anti-inflammatory, anti-atherosclerotic, anti-diabetic, anti-mutagentic, anti-carcinogenic, antioxidant and immune-modulation activities (Salehia et al., 2019, Kim, 2016Cullen et al., 2005;). Allicin breaks down into 2-propene sulfenic acid, which has the ability to bind free radicals and act as an anti-stress substance. ...
... Vitamin C is used as an immunomodulatory agent and used to control immunodeficiency diseases. Vitamin C has also contained immunostimulant activity to increase the level of T-lymphocytes and to inhibit the death of Tcells by signaling pathway (Salehi et al. 2019). Vitamin C inhibits the replication of P. multocida by restricting the expression of virulence factors of the bacteria. ...
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... Vitamin C is used as an immunomodulatory agent and used to control immunodeficiency diseases. Vitamin C has also contained immunostimulant activity to increase the level of T-lymphocytes and to inhibit the death of Tcells by signaling pathway (Salehi et al. 2019). Vitamin C inhibits the replication of P. multocida by restricting the expression of virulence factors of the bacteria. ...
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Pasteurella multocida (P. multocida) is a Gram-negative rod-shaped coccobacilli with non-lactose fermenting property. This study examined the potential efficacy of allicin, vitamin C, and doxycycline in reducing the intensity of P. multocida infection in rabbits. 20 locally bred, adult rabbits were divided into five equal groups. Different treatments such as allicin, vitamin C and doxycycline were applied in all groups. Rabbits in group 1 and 2 were kept as control and did not receive any treatment. Group 3 was treated with 500mg allicin and similarly, group 4 and group 5 treated with 100mg doxycycline and combined treatment like allicin 500mg, 100mg, doxycycline and 100mg Vitamin C respectively. Challenge and protection were given after one week in all groups. Except group 1, all remaining groups of rabbits were infected (intranasal) with P. multocida 2×10 4 CFU ̸ ̸ ml. Antioxidative activity, biochemical assay, hematological and immunological assays were performed. The results showed significant decrease in count of lymphocytes, hemoglobin and RBCs in infected group with increased phagocytic percentage. Serum biochemical enzyme including ALT, ALP and LDH level were significantly increased in infected group. SOD level showed significant increase in combined treated group and significant decrease in infected group. Sera were collected and titrated for antibody titers through indirect hemagglutination assay (IHA). Results were subjected and data was analyzed by 2 factorial CRD. The results depicted significantly higher IHA titers in group 5 followed by group 3 and 4 with short term sustainability. Rabbits in group 3 treated with 500mg allicin presented promising results than the group 4 rabbits treated with doxycycline. Hence, concluded that the use of antibiotics like doxycycline did not provide maximum protection against P. multocida. While the synergistic effect of allicin, vitamin C and doxycycline showed maximum protection providing evidence for promising remedy for HS.
... Vitamin C is used as an immunomodulatory agent and used to control immunodeficiency diseases. Vitamin C has also contained immunostimulant activity to increase the level of T-lymphocytes and to inhibit the death of Tcells by signaling pathway (Salehi et al. 2019). Vitamin C inhibits the replication of P. multocida by restricting the expression of virulence factors of the bacteria. ...
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Pasteurella multocida (P. multocida) is a Gram-negative rod-shaped coccobacilli with non- lactose fermenting property. This study examined the potential efficacy of allicin, vitamin C, and doxycycline in reducing the intensity of P. multocida infection in rabbits. 20 locally bred, adult rabbits were divided into five equal groups. Different treatments such as allicin, vitamin C and doxycycline were applied in all groups. Rabbits in group 1 and 2 were kept as control and did not receive any treatment. Group 3 was treated with 500mg allicin and similarly, group 4 and group 5 treated with 100mg doxycycline and combined treatment like allicin 500mg, 100mg, doxycycline and 100mg Vitamin C respectively. Challenge and protection were given after one week in all groups. Except group 1, all remaining groups of rabbits were infected (intranasal) with P. multocida 2�104 CFU ?? ml. Antioxidative activity, biochemical assay, hematological and immunological assays were performed. The results showed significant decrease in count of lymphocytes, hemoglobin and RBCs in infected group with increased phagocytic percentage. Serum biochemical enzyme including ALT, ALP and LDH level were significantly increased in infected group. SOD level showed significant increase in combined treated group and significant decrease in infected group. Sera were collected and titrated for antibody titers through indirect hemagglutination assay (IHA). Results were subjected and data was analyzed by 2 factorial CRD. The results depicted significantly higher IHA titers in group 5 followed by group 3 and 4 with short term sustainability. Rabbits in group 3 treated with 500mg allicin presented promising results than the group 4 rabbits treated with doxycycline. Hence, concluded that the use of antibiotics like doxycycline did not provide maximum protection against P. multocida. While the synergistic effect of allicin, vitamin C and doxycycline showed maximum protection providing evidence for promising remedy for HS.
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Allicin (2-propene-1-sulfinothioic acid S -2-propenyl ester, diallyl thiosulfinate) is the main biologically active ingredient in garlic. The present study investigated the protective effect of allicin against cardiomyocyte apoptosis that was induced by ischemia in vitro and the potential molecular mechanisms that were involved in this antiapoptotic effect. The results indicated that allicin increased H9c2 cell activity and attenuated the rate of apoptosis that was induced by ischemia/hypoxia. Intracellular calcium concentrations significantly decreased in the allicin-treated groups. Bax expression significantly decreased, and Bcl-2 expression increased in allicin-treated rats. Nitric oxide blockade significantly inhibited these effects. Allicin also increased the activity of SOD and NO release and decreased MDA levels. Allicin significantly increased the expression of eNOS, Nrf2, and HO-1 proteins. Collectively, these findings demonstrate that allicin protects H9c2 cells against apoptosis, and this protective effect appears to occur via eNOS/NO pathway-mediated antioxidant activity.
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DOI No: 10.5958/0974-360X.2017.00738.7 ABSTRACT: ________________________________________ Allium sativum is a species in the onion genus, Allium. Its close relatives include the onion, shallot, leek, chive, and Allium chinense. With a history of several thousand years of human consumption and use, garlic is native to the region between the Mediterranean and China, and has long been a common seasoning worldwide. Herbs such as garlic with the potential to significantly modulate the activity of drug-metabolizing enzymes (notably cytochrome p450 isozymes) and/or the drug transporter P-glycoprotein participate in potential pharmacokinetic interactions with anticancer drugs. Among the active compounds present in the plant, DTS and DDS are the most active against yeasts and ajoene is the main compound responsible for the antiviral activity of garlic. A great deal of low quality clinical research has been conducted to determine the effect of garlic on preventing cardiovascular diseases and on various biomarkers of cardiovascular health, but as of 2015, the results were contradictory and it was not known if there are any effects. Because garlic might reduce platelet aggregation, people taking anticoagulant medication are cautioned about consuming garlic. Meta-analysis found decreased rates of gastric cancer associated with garlic intake, but cited confounding factors as limitations for interpreting these studies. Further meta-analyses found similar results on the incidence of gastric cancer by consuming allium vegetables including garlic. Garlic is known to cause bad breath (halitosis) and body odor, described as a pungent "garlicky" smell to sweat. This is caused by allyl methyl sulfide (AMS). KEYWORDS: ________________________________________ A review, Anti-microbial, Anti-inflammatory, Cardiovascular, Allium sativum.
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BACKGROUND Hyperlipidemia is one of the important diseases in pregnancy that causes fetal abnormalities during pregnancy and after the birth. Unfortunately, the usual anti-fat drugs are associated with high morbidity in fetus and due to people's inclination towards taking herbs, it is required to identify side effects of medicinal herbs in pregnancy. The aim of this study was to present hypolipidemic herbs that would not any complications for mother and fetus. METHODS In this review article, the major electronic databases such as EBSCO, Central Register of Controlled Trials (CENTRAL), China Network Knowledge Infrastructure (CNKI), Cochrane, Google scholar, MEDLINE, SciVerse, Scopus, and Web of Science were searched using the key words “herbal” and “hyperlipidemia”, “herbal” and “pregnancy” matched by MeSH from their respective inceptions till September, 2016. Total of 1723 publications (145 review articles, 855 original research articles, and 723 abstracts) about the effect of herbals on hyperlipidemia and 682 publications (200 abstracts, 423 original research articles, and 59 review articles) about the effect of herbals in pregnancy were retrieved. At the end, a list of medicinal plants effective on hyperlipidemia alongside their effects on pregnancy was developed. Finally, the plants effective on hyperlipidemia and safe during pregnancy were determined and their dosage, complications, mechanism of action, and side effects were reported. RESULTS A total of 110 effective herbs on hyperlipidemia were identified and complications of 95 plants in pregnancy were studied. At last, among the 55 selected plants effective on hyperlipidemia and examined for pregnancy, we reported 12 herbs with their dosage and special considerations that can be used to treat hyperlipidemia during pregnancy. CONCLUSION Some medicinal plants can be used to treat hyperlipidemia during pregnancy without any significant side effects both on mother or fetus.
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Diabetic cardiomyopathy (DCM) is a common and severe complication of diabetes and results in high mortality. It is therefore imperative to develop novel therapeutics for the prevention or inhibition of the progression of DCM. Oxidative stress is a key mechanism by which diabetes induces DCM. Hence, targeting of oxidative stress-related processes in DCM could be a promising therapeutic strategy. To date, a number of studies have shown beneficial effects of several natural products on the attenuation of DCM via an antioxidative mechanism of action. The aim of the present review is to provide a comprehensive and concise overview of the previously reported antioxidant natural products in the inhibition of DCM progression. Clinical trials of the antioxidative natural products in the management of DCM are included. In addition, discussion and perspectives are further provided in the present review.
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The present study was designed to systematically evaluate the clinical efficacy and safety of garlic supplement in the management of type 2 diabetes mellitus (T2DM). PubMed, EMBASE, the Cochrane Library, and China National Knowledge Internet (CNKI) were searched for relevant randomized controlled trials (RCTs) by using the terms garlic and T2DM up to April 2017. The quality of included RCTs was assessed by the Cochrane tool of risk of bias, and data of outcomes were pooled by REVMAN 5.3. Clinical factors were handled by meta-regression and subgroup analysis, and risk of publication bias was explored by inverted funnel plots. Nine RCTs involving 768 T2DM patients were included in the meta-analysis, and the dose of daily garlic (allicin) supplement ranged from 0.05g to 1.5g. A significant reduction in the level of fasting blood glucose in 1–2 weeks [SMD = −1.61, 95%CI (−2.89, −0.32)], 3–4 weeks [SMD = −2.87, 95%CI (−4.74, −1.00)], 12 weeks [SMD = −9.57, 95%CI (−12.39, −6.75)], and 24 weeks [SMD = −21.02, 95% CI (−32.47, −9.57)] was achieved in favour of the garlic group rather than the control group. Significantly decreased fructosamine and glycated hemoglobin (both in 12 and 24 weeks) were also found in garlic group. Meanwhile, significantly improved blood liquids of total cholesterol [SMD = −1.93, 95%CI (−2.98, −0.87), 3–4 weeks], high density lipoprotein [SMD = −0.41, 95%CI (−0.83, −0.00), 3–4 weeks] and low density lipoprotein [SMD = −3.47, 95%CI (−5.76, −1.18), 12 weeks] were confirmed after garlic administration. There was no significant difference in complications. Current data confirms that garlic supplement plays positive and sustained roles in blood glucose, total cholesterol, and high/low density lipoprotein regulation in the management of T2DM.
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Purpose: To evaluate the protective and restoring effects of allicin in 7,12-dimethylbenz(a)anthracene (DMBA)-induced buccal pouch carcinogenesis. Methods: 1 week after receiving allicin (20 mg/kg body weight) orally, the buccal pouches of hamsters were painted daily with 0.5% 7,12-dimethylbenz(a)anthracene (DMBA) in liquid paraffin for 14 weeks and then every other day for another 2 weeks, after receiving allicin orally and thereafter for 14 weeks. The protective effects of allicin was evaluated by measuring the tumour incidence, tumour volume and tumour burdens as well as the levels of glycoconjugates were analyzed by using specific colorimetric methods. Animals not exposed to allicin and/or DMBA, those exposed to DMBA alone and others exposed to allicin alone served as controls. Results: Allicin significantly reduced the tumour incidence, tumour volume and tumour burden. DMBA-altered glycoconjugates in plasma, buccal mucosa tumour tissues and erythrocyte membrane of tumour bearing hamsters were normalized after treated with allicin. Conclusion: The results suggest that allicin has considerable potential to protect and restore the cell surface glycoconjugates moieties in the presence of allicin or possibly other oral carcinogenic agents. © Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, 300001 Nigeria. All rights reserved.
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PurposeDoxorubicin (DOX) is a highly active antineoplastic agent; however, its clinical use is limited due to associated cardiotoxicity. This study was performed to evaluate the beneficial effects of allicin, a dietary garlic active constituent against DOX-induced cardiotoxicity. Methods Forty male Swiss albino mice were divided into five groups, which received normal saline, oral allicin (20 mg kg−1 once daily), intraperitoneal DOX (on the 7, 9 and 11th day of the experiment), or DOX plus once daily allicin at 10 or 20 mg kg−1. Sera were collected for evaluation of cardiac injury markers and proinflammatory cytokines. Additionally, heart tissue spacemen were harvested for determination of oxidative stress markers, as well as for histopathological examination and immunohistochemical analysis. ResultsDOX administration induced significant (p < 0.05) reductions in cardiac tissue level of reduced glutathione and activities of antioxidant enzymes (catalase, superoxide dismutase, and glutathione peroxidase). Moreover, it induced significant (p < 0.05) elevations in cardiac tissue concentrations of nitric oxide and malondialdehyde as well as serum levels of cardiac injury biomarkers (lactate dehydrogenase, creatine kinase, and creatine kinase-MB) and proinflammatory cytokines (interleukin-1β, and tumor necrosis factor-alpha). The histopathological examination showed necrotic and degenerative changes in the cardiac tissue, while immunohistochemical analysis revealed marked myocardial expression of activated caspase-3 and cyclooxygenase-2, following DOX adminstration. Allicin pretreatment significantly improved (p < 0.05) all examined parameters, and restored the cardiac architecture. Conclusion The current study demonstrated that allicin effectively mitigates cardiac oxidative damage, apoptosis and inflammation, induced by acute DOX intoxication. Therefore, allicin could be a promising cytoprotective agent against DOX cardiotoxicity.
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The current strategy for the control of helminth infections relies on chemotherapy. However, resistance appearance is promoting the necessity of developing new drugs against trematodes. Herein, potential trematocidal effects of garlic (Allium sativum) are investigated in the context of intestinal foodborne trematodes, employing the Echinostoma caproni-mouse model. Daily administration of dietary doses of garlic was conducted in three groups of mice: (i) before infection (prophylaxis), (ii) after infection (therapeutic) and (iii) both, before and after infection (continuous). A fourth group of mice, not exposed to garlic, was used as control. No differences in worm recovery, fecundity and local cytokine expression profiles were found with respect to control infections. However, considerable alterations in tegument structure, including swelling, furrowing, vacuolization and changes in secretory bodies were detected in garlic-exposed parasites using scanning and transmission electron microscopy. Protein secretion was markedly reduced in response to garlic, whereas up-regulation of several proteins, such as major vault protein and tER-ATPase, was observed in treated worms. The results presented herein provide new insights in the anthelminthic activity of bioactive garlic compounds and the manner that parasites respond to toxins.
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Urea is the most widely used form of N fertilizer in agriculture. However, if it is not incorporated into soil soon after application, urea has the disadvantage of undergoing considerable losses as ammonia gas due to hydrolysis in the presence of soil urease. Urease inhibitors are some of the most commonly used approaches to overcome nitrogen losses in fields, as they delay urea hydrolysis and thus increase the chances of urea incorporation into soil. Among the known soil urease inhibitors is the chemical based N(butyl) thiophosphoric triamide (NBPT) but it is found to cause some phytotoxic effect on plants among assimilation issues. Allicin, a natural based bio-inhibitor from garlic (Allium sativum L.), has shown potential to inhibit urease activity. In this context, laboratory experiments were conducted to examine the effect of different allicin concentrations on soil urease inhibition period. The loss of applied urea was quantified, using diacetylmonoxime (DAM) calorimetric method, following application of urea with and without allicin. Urea and a mixture of urea and allicin at different concentrations (5%, 10% and 15% w allicin/w urea) were surface-applied at a rate of 1000 μg Urea N/kg soil to small circular containers. The soil was irrigated to maintain the moisture content between 25-30% throughout the study. This study suggest that prilled form urea application gave more consistent results than when urea was dissolved and added to the soil as a solution. Through this study, it was shown that allicin exerts inhibitory effects on urease in soil for agricultural applications, where 5% weight allicin to weight urea applied resulted in the best urease inhibition. At the given operating parameters, allicin inhibition was about 75% less than NBPT at steady state. While this study demonstrated the potential of allicin as a viable bio-inhibitor to retard the loss of urea in soil and thus it may be used along with urea for improved utilization of the applied –N by plants.
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Background & Aims Metformin is currently the most widely used first-line hypoglycemic agent for diabetes mellitus. Besides glucose-lowering action, there is increasingly interest in the potential anti-inflammatory action of this drug. In the present study, we investigated the actions of metformin on experimental insulitis using STZ-induced diabetic mice. Methods Mice with acute diabetes induced by STZ were administered metformin by gavage. Changes of blood glucose and body weight, and the daily amount of food and water intake were measured. Pancreatic tissues were collected for histologic analyses. Pathological assessment and immunohistochemistry analysis were used to determine the effect of metformin on insulitis. Inflammatory cytokines in the pancreas and insulin levels were measured through ELISA analysis. Results Metformin significantly reduced blood glucose levels and improved aberrant water intake behavior in experimental diabetic mice. No significant differences were observed in terms of body weight and food intake behavior in metformin-treated animals. In the STZ-induced model of diabetes, we found the appearance of pronounced insulitis. However, metformin administration reduced the severity of insulitis assessed by blind pathological scoring. In addition, metformin treatment improved insulin levels in experimental diabetic mice. ELISA assay revealed decreased levels of inflammatory response marker IL-1β and TNF-α in the pancreatic tissues following metformin treatment. Conclusion Metformin attenuated insulitis in the STZ-induced mice model of diabetes. This islet-protective effect might be partly correlated with the anti-inflammatory action of metformin.
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Garlic (Allium sativum L.) has been used as a spice and medicinal plant since ancient times. Garlic produces the thiol-reactive defence substance, allicin, upon wounding. The effects of allicin on human lung epithelium carcinoma (A549), mouse fibroblast (3T3), human umbilical vein endothelial cell (HUVEC), human colon carcinoma (HT29) and human breast cancer (MCF7) cell lines were tested. To estimate toxic effects of allicin, we used a standard MTT-test (methylthiazoltetrazolium) for cell viability and 3 H-thymidine incorporation for cell proliferation. The glutathione pool was measured using monobromobimane and the formation of reactive species was identified using 2 ,7-dichlorofluoresceine-diacetate. The YO-PRO-1 iodide staining procedure was used to estimate apoptosis. Allicin reduced cell viability and cell proliferation in a concentration dependent manner. In the bimane test, it was observed that cells treated with allicin showed reduced fluorescence, suggesting glutathione oxidation. The cell lines tested differed in sensitivity to allicin in regard to viability, cell proliferation and glutathione oxidation. The 3T3 and MCF-7 cells showed a higher proportion of apoptosis compared to the other cell types. These data show that mammalian cell lines differ in their sensitivity and responses to allicin.
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This work was performed to study the effect of allicin on hypertension and cardiac function in a rat model of CKD. The groups were control, CKD (5/6 nephrectomy), and CKD-allicin treated (CKDA) (40 mg/kg day/p.o.). Blood pressure was monitored (weekly/6 weeks). The cardiac function, vascular response to angiotensin II, oxidative stress, and heart morphometric parameters were determined. The CKD group showed hypertension and proteinuria. The coronary perfusion and left ventricular pressures were decreased in CKD group. In contrast, the vascular response to angiotensin II and expression of angiotensin II type 1 receptor (AT1R) were increased. These data were associated with the increment in morphometric parameters (weight of heart and left ventricle, heart/BW and left ventricular mass index, and wall thickness). Concurrently, the oxidative stress was increased and correlated inversely with the expression of Nrf2, Keap1, and antioxidant enzymes Nrf2-regulated. Allicin treatment attenuated hypertension and improved the renal and the cardiac dysfunctions; furthermore, it decreased the vascular reactivity to angiotensin II, AT1R overexpression, and preserved morphometric parameters. Allicin also downregulated Keap1 and increased Nrf2 expression, upregulated the antioxidant enzymes, and reduced oxidative stress. In conclusion, allicin showed an antihypertensive, nephroprotective, cardioprotective, and antioxidant effects, likely through downregulation of AT1R and Keap1 expression.
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The chemical composition of garlic essential oils (GEOs) extracted from two different cultivars has been characterized using GC–MS analysis. GEO that was extracted from the white-skin cultivar (WGO) had a lower percentage of the major constituents diallyl trisulfide and diallyl disulfide (45.76 and 15.63%) than purple-skin cultivar (PGO) which contained higher percentages (58.53 and 22.38%) of the same components, respectively. Evaluation of the antimicrobial activity of WGO and PGO delivered in organic solvent (isopropanol) showed dose-dependent antimicrobial activity against the tested pathogenic bacteria and fungi, especially with WGO. On the other hand, formulation of both GEOs in water-based emulsions totally suppressed the antimicrobial activity of GEO. Re-formulation of GEOs in water-based microemulsion (particle size 10.1 nm) showed better antimicrobial activity than emulsions at the same concentration of GEOs. This study can assist in designing the proper water-based delivery system of GEO for application in food preservation.
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Background: Leishmania is a unicellular protozoan parasite that produces several human diseases, ranging from localized self-healing cutaneous lesions to deadly visceral infections. Objective: The effect of allicin on the growth of Leishmania major (L. major) promastigotes was evaluated under in vitro conditions. Moreover, the efficacy of a topical allicin cream was examined in BALB/c (Bagg albino, laboratory-bred strain of the House Mouse) mice with cutaneous leishmanial lesions compared to the currently used drug, sodiumstibogluconate (pentostam). Methods: Cytotoxiciy and promastigote proliferation were measured. Different concentrations (50, 100, 150, and 200 μM) of liquid allicin were tested on L. major promastigotes twice: after 24 and 48 hours using an MTT colorimetric assay. In the in vivo condition, the efficacies of allicin cream and liquid allicin at two concentrations (0.15 μM/mouse and 0.30 μM/mouse) were evaluated. Serum factors of the control and treated groups were tested to evaluate the toxic effects of allicin on the liver and kidney. Results: Allicin at a concentration of 50 μM inhibited the growth of Leishmania promastigotes. Topical application of allicin cream reduced lesion sizes in mice. No significant differences in biochemical analysis were observed between the control and treated groups. Conclusions: Allicin has antileishmanial effects under in vitro and in vivo conditions and may be used in clinical applications.
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Background: Vascular endothelial apoptosis is significantly associated with atherosclerosis and cardiovascular diseases, for which oxidized low-density lipoprotein (ox-LDL) is a major risk factor. Allicin, the primary active ingredient of garlic, has been found to have cardiovascular protective effect by changing the fatty-acid composition, but its effect on ox-LDL-induced vascular endothelial injury remains unclear. We investigated the protective effect of allicin on cell viability, LDH release, apoptosis and apoptotic signaling in human umbilical vein endothelial cells (HUVECs). Methods: In cultured HUVEC cell line, ox-LDL induced injury was investigated. The cell viability and injury were evaluated by using cell proliferation Assay kit and LDH release assay. The apoptosis was evaluated by the Annexin V-FITC kit. The activity of caspase-3 was assessed using a colorimetric caspase-3 assay kit. The ROS production was evaluated by fluorometric assay and NADPH oxidase activity was assessed with a GENMED kit. Results: Exposure of HUVECs to ox-LDL (150 μg/ml) reduced cell viability, induced apoptosis and increased activity of caspase-3, NADPH oxidase, and reactive oxygen species (ROS) production. The pretreatment with allicin (30 and 100 μM) significantly rescued the cell viability, inhibited ox-LDL-induced apoptosis and activity of caspase-3, NADPH oxidase and ROS production in HUVECs, and the protective effect is concentration-dependent. The allicin (100 μM) alone did not show significant difference from control. Our study demonstrated that allicin protected HUVECs from ox-LDL-induced endothelial injury by reducing the apoptosis, mediated by inhibition of caspase-3 and NADPH oxidase related apoptotic signaling. Conclusions: Allicin prevents ox-LDL-induced endothelial cell injury by inhibiting apoptosis and oxidative stress pathway.
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Drug resistance and hepatic dysfunction are the two major factors that limit the application of chemotherapy for hepatocellular carcinoma (HCC). It has been reported that allicin has the hepatic protective effect and antitumor activity. Hence allicin may be an ideal enhancer to chemotherapy regimen of HCC. In the present study, we demonstrated that allicin enhanced 5-fluorouracil (5-FU) inducing cytotoxicity in HCC cells. In vivo experiment, combined treatment group with allicin (5 mg/kg/d; every two days for 3 weeks) and 5-FU (20 mg/kg/d; 5 consecutive days) showed a dramatic inhibitory effect on the growth of HCC xenograft tumors in nude mice. The co-treatment group showed highly apoptotic level compared with 5-FU treated alone. Cells combined treatment with allicin and 5-FU increased intracellular reactive oxygen species (ROS) level, reduced mitochondrial membrane potential (ΔΨm), activated caspase-3 and PARP, and down-regulated Bcl-2 compared with DMSO, allicin and 5-FU treated alone. Moreover, the increase of activated caspase-3 and PARP was blocked by the ROS inhibitor antioxidant N-acetyl cysteine (NAC). In conclusion, this is the first study to demonstrate that allicin sensitized HCC cells to 5-FU induced apoptosis through ROS-mediated mitochondrial pathway. These results provided evidences for the combination used of allicin and 5-FU as a novel chemotherapy regimen in HCC.
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Allicin (diallyl thiosulfinate) from garlic is a highly potent natural antimicrobial substance. It inhibits growth of a variety of microorganisms, among them antibiotic resistant strains. However, the precise mode of action of allicin is unknown. Here, we show that growth inhibition of Escherichia coli during allicin exposure coincides with a depletion of the glutathione pool and S-allylmercapto modification of proteins, resulting in overall decreased total sulfhydryl levels. This is accompanied by the induction of the oxidative and heat stress response. We identified and quantified the allicin-induced modification S-allylmercapto cysteine for a set of cytoplasmic proteins by using a combination of label-free mass spectrometry and differential OxICAT labeling. Activity of isocitrate lyase AceA, an S-allylmercapto-modified candidate protein, is largely inhibited by allicin treatment in vivo. Allicin-induced protein modifications trigger protein aggregation, which largely stabilizes RpoH and thereby induces the heat stress response. At sublethal concentrations, the heat stress response is crucial to overcome allicin stress. Our results indicate that the mode of action of allicin is a combination of a decrease of glutathione levels, unfolding stress, and inactivation of crucial metabolic enzymes through S-allylmercapto modification of cysteines.
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Objective: In the Mexican ethno-medicine, a number of plants have shown a successful anthelmintic activity. This fact could be crucial to identify possible green anti-parasitic strategies against nematodes affecting animal production. This research evaluated the in vitro and in vivo nematocidal effects of two single and combined plant extracts: bulbs of Allium sativum (n-hexane) and flowers of Tagetes erecta (acetone). The in vivo assay evaluated the administration of extracts either individually or combined against Haemonchus contortus in experimentally infected gerbils. Methods: The in vitro larvicidal activity percentage (LAP) of A. sativum and T. erecta extracts against H. contortus (L3) was determined by means of individual and combined usage of the extracts. Similarly, the extracts were evaluated in terms of reduction in the parasitic population in gerbils infected with H. contortus by individual and combined usage. Results: The LAP at 40 mg/mL was 68% with A. sativum and 36.6% with T. erecta. The combination caused 83.3% mortality of parasites. The oral administration of A. sativum and T. erecta extracts at 40 mg/mL, caused 68.7% and 53.9% reduction of the parasitic burden, respectively. Meanwhile, the combined effect of both extracts shown 87.5% reduction. Conclusion: This study showed evidence about the effect of A. sativum and T. erecta plant extracts by means of individual and combined usage against H. contortus in in vitro and in vivo bioassays in artificially H. contortus-infected gerbils as a model.
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Spices are indispensable components of Indian cuisines since ancient times and are considered as rich source of bio-active antimicrobial compounds. Antibacterial and antifungal activity of individual as well as ethanolic extracts of cumin (Cuminum cyminum), ginger (Zingiber officinale) and garlic (Allium sativum) was evaluated against bacterial strains of Bacillus subtilus, Pseudomonas fluroscens, Salmonella Typhi and fungal strains of Candida albicans and Rhizopus azygosporus. Agar well diffusion assay for antimicrobial activity yielded the inhibitory zone of 12.8 to18.3 mm diameter for cumin, 11.5 to 16.3 mm diameter for ginger and 16.8 to 19.3 mm diameter for garlic extract indicating that garlic was the most effective spice in inhibiting the microbial growth. The combined extracts showed inhibition zones ranging from 12.3 to 19.6 mm in diameter against bacteria and 15.6 to 19.6 mm against fungus. The combined extract of cumin and garlic was found to be most effective in inhibiting the microbial growth. The MIC of individual extracts was 12.5 mg/ml against all the tested microorganisms. The MIC of combined extracts fluctuated from 3.8 to 6.7 mg/ml and the most sensitive microbial species in relation to the MIC of combined extracts was S. Typhi. The fractional inhibitory concentrations (FIC) values of the combined extracts suggested additive inhibitory effect of the combined spice extracts (0.5 ≤ FIC index ≤ 1).
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Matricaria is a widespread genus of flowering plants of the family Asteraceae that grow in temperate regions of Europe, Asia, America and Africa. Some of the species are also naturalized in Australia. Some species of this genus such as Chamomiles are recognized medicinal plants and cultivated in several countries for commercial purposes: to obtain its blue essence, as herbal tea, and for pharmaceutical or cosmeceutical uses. The phytochemical composition of Matricaria spp. includes volatile terpenoids (e.g., α-bisabolol, bisabolol oxide A and B, β-trans-farnesene and chamazulene), sesquiterpene lactones such as matricin, and phenolic compounds (flavonoids, coumarins and phenolic acids). Their essential oil is obtained from the fresh or dried inflorescences by steam distillation, and additionally cohobation of the remaining water. The volatile composition of the essential oil, especially the content of the valuable components α-bisabolol and chamazulene, depends on the plant part, origin and quality of the source, genetic, and environmental factors. Moreover, other parameters, such as season of harvest and methods of extraction, can affect the extraction yield of the essential oils/extracts, their composition and, therefore, their bioactivity. Due to the importance of this genus and particularly M. recutita (M. chamomilla), this review focus on its cultivation, factor affecting essential oils’ composition and their role in traditional medicine, as antibacterial agents and finally as food preservatives.
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Antimicrobial activity of garlic (Allium sativum L.) and holy basil (Ocimum sanctum L.) essential oils (GEO and HBEO, respectively) was evaluated in liquid vs. vapour phases. Diallyl disulphide and diallyl trisulphide in GEO while eugenol, caryophyllene and methyl eugenol in HBEO were predominant active compounds. Individually, GEO was highly effective in the vapour phase, showing the greatest antimicrobial activity (P ≤ 0.05) against Bacillus cereus and Staphylococcus aureus with complete inhibition, followed by Salmonella typhimurium and Pseudomonas fluorescens, but had no effect on Escherichia coli, Lactobacillus plantarum or Listeria monocytogenes. The combined GEO:HBEO (a 1:1 ratio) at 30 μL demonstrated inhibitive activity against all bacteria tested with complete inhibition against B. cereus and S. aureus. Minimum bactericidal concentration (MBC) of the combined oil was <0.4% v/v, except for P. fluorescens requiring a higher MBC (1.5%, v/v). This study demonstrated potential of the combined GEO:HBEO to be used for food preservation applications.
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Allicin is the major biologically active compounds of freshly crushed garlic. It has been reported to inhibit the proliferation and promote the apoptosis of multiple colorectal cancer cells. However, the anti-colorectal cancer effect of Allicin has not been verified by in vivo studies. In the present study, we investigated the effect of Allicin on azoxymethane/dextran sodium sulfate (AOM/DSS) colorectal cancer mouse model and explore the underlying possible mechanism. Our result showed that Allicin could inhibit colonic tumorigenesis of AOM/DSS mice in vivo. In vitro study showed that Allicin promoted the apoptosis and suppressed the survival and proliferation of HCT116 cells. The molecular mechanism is related to the suppression of STAT3 signaling activation. Thus, our data provide further support for Allicin as a potential favorable supplement for human colorectal cancer.
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Allicin has been reported to inhibit cancer cell proliferation, induce cell apoptosis and enhance the accumulation of reactive oxygen species. However, it has remained elusive whether allicin improves multidrug resistance in thyroid cancer cells through modulating autophagy. The present study demonstrated that combined use of allicin and cisplatin or carboplatin resulted in an enhanced growth inhibitory effect on SW1736 and HTh-7 cells. Furthermore, treatment with allicin significantly increased SW1736 and HTh-7 cell autophagy. Of note, allicin-induced cell death was largely abolished by 3-methyladenine or chloroquine treatment, suggesting that allicin-induced A549 cell death was dependent on autophagy. Western blot analysis demonstrated that allicin treatment inhibited the activation of Akt, mammalian target of rapamycin and S6. Furthermore, it was demonstrated that combined use of allicin and rapamycin induced more cell death compared with that induced by allicin or rapamycin alone. In conclusion, allicin may serve as an adjunctive therapy for thyroid cancer, as it induces autophagy-dependent cell death even when cancer cells have developed apoptosis resistance.
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Recent studies show a significant variation in antioxidant and antimicrobial properties between the various garlic genotypes mostly due to differences in chemical composition and bioactive compounds content. The aim of the present study was to evaluate antioxidant properties and antimicrobial activity of garlics collected from the main cultivation areas of Greece, as well as to correlate this activity with their total phenolics content. Genotype G5 showed the highest total phenolics content, which was significantly correlated with the lowest EC50 values for all the tested antioxidant activity assays. Antimicrobial activity was significant, especially against the bacteria Proteus mirabilis and Antibiotic resistant Escherichia coli. In conclusion, significant variation was observed between the studied garlic genotypes, indicating the importance of both growing conditions and genotype on bioactive properties of dry garlic bulbs. This variation could be further exploited in breeding programs in order to select elite genotypes with increased bioactive properties.
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Organosulfur compounds derived from Allium vegetables have long been recognized for various therapeutic effects, including anticancer activity. Allicin, one of the main biologically active components of garlic, shows promise as an anticancer agent; however, instability makes it unsuitable for clinical application. The aim of this study was to investigate the effect of stabilized allicin derivatives on human breast cancer cells in vitro. In this study, a total of 22 stabilized thiosulfinate derivatives were synthesized and screened for their in vitro antiproliferative activities against drug-sensitive (MCF-7) and multidrug-resistant (MCF-7/Dx) human adenocarcinoma breast cancer cells. Assays for cell death, apoptosis, cell cycle progression and mitochondrial bioenergetic function were performed. Seven compounds (4b, 7b, 8b, 13b, 14b, 15b and 18b) showed greater antiproliferative activity against MCF-7/Dx cells than allicin. These compounds were also selective towards multidrug-resistant (MDR) cells, a consequence attributed to collateral sensitivity. Among them, 13b exhibited the greatest anticancer activity in both MCF-7/Dx and MCF-7 cells, with IC50 values of 18.54±0.24 and 46.50±1.98 μmol/L, respectively. 13b altered cellular morphology and arrested the cell cycle at the G2/M phase. Additionally, 13b dose-dependently induced apoptosis, and inhibited cellular mitochondrial respiration in cells at rest and under stress. MDR presents a significant obstacle to the successful treatment of cancer clinically. These results demonstrate that thiosulfinate derivatives have potential as novel anticancer agents and may offer new therapeutic strategies for the treatment of chemoresistant cancers.