Development of topical patches releasing allicin using garlic extract.

INTRODUCTION: Treating hair loss of Alopecia areata is a quite challenge. The treatment not only needs to be effective but must meet specific requirements in terms of accurate dose, sustain release, comfortable application with aesthetic appearance. Thus, the study was designed to develop sustained release topical patches releasing allicin using different sources, including the extract from fresh and aged garlic, and commercially pure one. METHODS: Patches were formulated by solvent casting method using ethylene-vinyl acetate as backing layer and Carbopol® 971P NF (CP) as mucoadhesive polymer. Physicochemical properties were evaluated including weight, thickness, drug content, surface pH, moisture content, folding endurance, and swelling. In addition to in vitro diffusion study across the cellulose and Strat-M® membranes. RESULTS: Patches showed good physicochemical properties. No significant difference (p > 0.05) was obvious in the percentage of allicin diffused across cellulose membrane between patch A (loaded with commercial allicin), patch B1 (loaded with fresh garlic extract), and patch C (loaded with aged garlic extract). However, ethanol enhanced the diffusion of allicin. The percentage of allicin diffused across cellulose membrane over 20 h from patch E (45 mg CP, 2 mL fresh garlic extract-equivalent to 60 mg allicin-and 1 mL of ethanol) was 79.94%. The flux and permeability coefficients were 2.62 mg/cm2 /h and 0.52 cm/h, respectively, with an enhancement ratio of 2.60 times the reference patch M (mashed garlic). CONCLUSION: Promising development of topical patches of allicin using garlic extract as natural source with lower cost than the commercial pure allicin and higher aesthetic acceptance than the used mashed garlic.

Enhanced antimicrobial activity and pH-responsive sustained release of chitosan/poly (vinyl alcohol)/graphene oxide nanofibrous membrane loading with allicin.

Herein, the natural extract of garlic, allicin (Alli), was added into chitosan (CS)/polyvinyl alcohol (PVA)/graphene oxide (GO) composites to develop the nanofibrous membranes with strong antibacterial activity and sustained-release properties by electrospinning technology. Vitro Alli release test showed that the release rate and amount of Alli could be regulated by the content of GO in the nanofibrous membrane. The antibacterial activity test against Staphylococcus aureus was performed and revealed the antibacterial activity of nanofibrous membranes loading with Alli. Compared with the nanofibrous membrane without GO, the CS/PVA/Alli nanofibrous membrane with 0.1 wt% GO still had nice antibacterial activity after 48 h. The water contact angle of nanofibrous membranes dropped significantly with the addition of GO and Alli, which showed the nanofibrous membrane had highly hydrophobic. The CS/PVA/GO nanofibrous membrane loading with Alli had great hygroscopicity and moisture-retention capacity. The essential characteristics of nanofibrous membranes were evaluated by SEM, FTIR, XRD. The above results indicate that the membrane has a strong antimicrobial activity and long-lasting efficacy, so the developed natural nanofibrous membranes hold potential as promising antibacterial wound dressing and tissue engineering.

Effect of allicin on wound healing: an experimental diabetes model.

OBJECTIVE: The aim of this study was to investigate the effect of allicin on wound healing in an experimental diabetes model. METHOD: In this randomised controlled study, 50 Wistar albino rats (25 females, 25 males) each weighing 200-300g were used. To develop the diabetes model, 30 rats were induced with 50mg/kg streptozotocin (STZ); 20 rats were not induced in order to compare diabetic and nondiabetic rats. The diabetic rats were divided into three groups, according to dressing material used (allicin, physiological serum and control, where no dressing was used), and the nondiabetic rats were divided into two groups (allicin and control, where no dressing was used). The wound area was calculated and recorded on days 0, 7, 14 and 21. In addition, biopsies were taken from the wound area on days 0, 7, 14 and 21 and used for microscopic examination. Day 0 was used as a reference to calculate wound healing percentage. RESULTS: On days 7 and 14, there were statistically significant differences between groups. Wound surface areas were smaller in the allicin group than in other groups on days 7 and 14. There were no statistically significant differences between the groups on day 21. In addition, it was determined that neutrophil, mononuclear cell, intraepithelial oedema and dermal oedema density were lower and fibroblast, angiogenesis and collagen density were higher in the allicin groups on days 7 and 14. CONCLUSION: In this study, allicin was found to be potentially effective on wound healing. Future research should be conducted in order to clarify how it affects wound healing.

Allicin enhances the radiosensitivity of colorectal cancer cells via inhibition of NF-κB signaling pathway.

Radioresistance is an important factor affecting the radiotherapy effect of colorectal cancer (CRC). Allicin is a versatile sulfur-containing organic compound extracted from garlic (Allium sativum L.), which has many pharmacological effects. However, the effect of allicin on the sensitivity of CRC radiotherapy has not been confirmed. The present study is to observe the radiosensitivity effects of allicin and to explore its mechanism in CRC radiotherapy. The proliferation inhibition effects of allicin combined with X-ray radiotherapy in HCT116 cells were measured by growth curve of cell and colony formation assays. The cell apoptosis was detected by Hoechst 33258 nucleus staining assay. The migration ability of cells was detected by Transwell chamber migration assay. The animal model of CRC was established in BALB/c mice via transplantation of CT26 cell, and the radiosensitization effect of allicin on CRC was detected in vivo. The mRNA expressions of NF-κB, IKKß, and IκBα were analyzed by reverse transcription-polymerase chain reaction (RT-PCR). The protein expressions of NF-κB, p-NF-κB, IKKß, p-IKKß, IκBα, and p-IκBα were detected by western blotting. Our results showed that allicin improves the sensitivity of X-ray radiotherapy in CRC, and its mechanism may be associated with inhibition of NF-κB signaling pathway. These findings suggest that allicin may be used as a potential sensitizer for tumor radiotherapy in the clinic.

Effects of laying breeder hens dietary ß-carotene, curcumin, allicin, and sodium butyrate supplementation on the growth performance, immunity, and jejunum morphology of their offspring chicks.

This study evaluated the growth performance, immunity, and jejunum morphology of chicks hatched from laying breeder hens given dietary additive supplementation, as well as chicks receiving direct antibiotic supplementation in early life. Hy-line breeder hens were allotted to 2 groups with 3 replicates. A control group (CON) was fed a basal diet, and the treatment group (CCAB) received ß-carotene, curcumin, allicin, and sodium butyrate in addition to basal diet for 5 wk. Breeder-hen eggs were collected and hatched. The chicks hatched from the CON group were assigned to 2 treatments: a chick control group (cCON) and a chick treatment group (Cipro) given ciprofloxacin lactate into drinking water; the cCON group, Cipro group, and the chicks hatched from the CCAB group (cCCAB) were fed the same diet for 4 wk. The results demonstrated that there were significant differences between the CON and CCAB groups in the serum levels of IgA, IgG, IgM (triple P < 0.01), lysozyme (P < 0.05), and ß-defensin (P < 0.05). The body weights of the cCCAB group's chicks increased at 1, 7, and 28 D of age (P < 0.05, P < 0.05, P < 0.01, respectively), and those of the Cipro group's chicks increased at 7 and 21 D of age (P < 0.01, P < 0.05). The tibial lengths of the cCCAB group's chicks increased at 1, 7, 14, 21, and 28 D of age (P < 0.01, P < 0.05, triple P < 0.01), and the lengths in the Cipro group increased at 7 and 14 D of age (P < 0.01, P < 0.01). Intestinal development, including intestinal length, jejunum morphology, and IgA positive cells, helps to explain these results. The breeder eggs from the CCAB group had higher IgG (P < 0.05) and IgM (P < 0.05) levels in the egg whites and higher IgA, IgG, and IgM levels (triple P < 0.01) in the egg yolks. In conclusion, ß-carotene, curcumin, allicin, and sodium butyrate supplementation of laying breeder hen diets produced more advantages in growth performance and intestinal development in offspring than in chicks directly supplemented with antibiotics.

Allicin alleviates inflammation of diabetic macroangiopathy via the Nrf2 and NF-kB pathway.

As diabetic macroangiopathy is becoming increasingly prevalent, it is urgent to explore preventive and therapeutic drugs and study the mechanism. Diabetic mice were induced by intraperitoneal injection of streptozotocin (STZ)for five consecutive days. Diabetic mice were divided into diabetic and allicin groups. After sacrifice, frozen aortic root sections were immunohistochemically stained for nuclear factor erythroid 2-related factor 2 (Nrf2) and inflammation cytokine-tumor necrosis factor α (TNF-α), and the remaining aortic tissues were analyzed by Western blot for the expression of proinflammation genes. In vitro, Nrf2 and inflammatory relative protein expression levels in Human Umbilical Vein Endothelial Cells (HUVECs) were examined. HUVECs proliferation and apoptosis were measured. TNF-α expression was increased in diabetic group compared to that in control group; this effect was alleviated in allicin-treated mice. Inflammation relative protein expression of Vascular Cell Adhesion Molecule 1(VCAM-1), Matrix metalloproteinase 2 (MMP-2), Inducible Nitric Oxide Synthase (iNOS), and monocyte chemotactic protein 1 (MCP-1) was higher in the diabetic group than in the control group; however, allicin treatment inhibited these diabetes-induced increase. In vitro, allicin treatment reversed the hyperglycemia-induced reduction in proliferation, and decreased the apoptosis induced by high glucose. Inflammation relative protein expression was consistent with that in vivo. Additionally, the expression of nuclear factor kappa-B (NF-κB)and Nrf2 was increased in both DM mice and HUVECs; allicin treatment induced a significant reduction in NF-κB level and improvement in Nrf2 level. Allicin alleviates inflammation caused by diabetic macroangiopathy, and the mechanism may occur via increasing Nrf2 and decreasing NF-κB.

Allicin Modifies the Composition and Function of the Gut Microbiota in Alcoholic Hepatic Steatosis Mice.

The intestinal microbiome plays an important role in the pathogenesis of liver diseases. Alcohol intake induces gut microbiota dysbiosis and alters its function. This study investigated the antibiotic effect of allicin in mice with hepatic steatosis. Male C57BL/6 mice were administered an ethanol diet supplemented with allicin (5 and 20 mg/(kg bw day)) for 4 weeks. Allicin modified the gut microbiota composition. Cecal microbiota exhibited a positive correlation with alcohol and hepatic triacylglycerol, but were suppressed with allicin. Ethanol diet with 5 mg of allicin induced a lower intestinal permeability compared to the ethanol diet alone. Allicin mediated the lipopolysaccharide (LPS)-CD14-toll-like receptor 4 (TLR4)-induced hepatic inflammation pathway by reducing LPS, CD14, TLR4, and pro-inflammatory cytokines-tumor necrosis factor (TNF)-α, interleukin (IL)-1ß, and IL-6. However, hepatic inflammation primarily resulted from alcohol toxicity rather than LPS production in the gut. The prediction of functional profiles from metagenomic 16S ribosomal RNA (rRNA) data revealed different functional profiles in each group. The predicted aldehyde dehydrogenase tended to increase in alcoholic mice administered allicin. The predicted LPS-related pathway and LPS biosynthesis protein results exhibited a similar trend as plasma LPS levels. Thus, alcohol and allicin intake shapes the gut microbiota and its functional profile and improves the CD14-TLR4 pathway to alleviate inflammation in the liver.

Hepatoprotective effect of allicin against acetaminophen-induced liver injury: Role of inflammasome pathway, apoptosis, and liver regeneration.

Acetaminophen (APAP) overdose leads to liver injury. NLRP3 inflammasome is a key player in APAP-induced inflammation. Also, apoptosis and liver regeneration play an important role in liver injury. Therefore, we assessed allicin's protective effect on APAP-induced hepatotoxicity and studied its effect on NLRP3 inflammasome and apoptosis. Mice in the APAP group were injected by APAP (250 mg/kg, intraperitoneal). The allicin-treated group received allicin orally (10 mg/kg/d) during 7 days before APAP injection. Serum and hepatic tissues were separated 24 hours after APAP injection. Serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), albumin, alkaline phosphatase (ALP), and hepatic malondialdehyde (MDA) were assessed using the colorimetric method. Hepatic NLRP3 inflammasome, caspase-1, and interleukin-1ß (IL-1ß) were estimated using enzyme-linked immunosorbent assay. Hepatic Bcl-2 and Ki-67 were investigated by immunohistochemistry. APAP significantly increased AST, ALT, and ALP, whereas allicin significantly decreased their levels. Also, APAP significantly decreased albumin and allicin significantly improved it. APAP produced changes in liver morphology, including inflammation and massive coagulative necrosis. Allicin protected the liver from APAP-induced necrosis, apoptosis, and hepatocellular degeneration via increasing Bcl-2 and Ki-67 levels. APAP significantly increased the hepatic MDA, whereas allicin significantly prevented this increase. APAP markedly activated the NLRP3 inflammasome pathway and consequently increased the production of caspase-1 and IL-1ß. Interestingly, we found that allicin significantly inhibited NLRP3 inflammasome activation, which resulted in decreased caspase-1 and IL-1ß levels. Allicin has a hepatoprotective effect against APAP-induced liver injury via the decline of oxidative stress and inhibition of the inflammasome pathway and apoptosis. Therefore, allicin might be a novel tool to halt the progression of APAP-stimulated hepatotoxicity.

Influence of allicin administration on reproductive efficiency, immunity and lipid peroxidation of rabbit does under high ambient temperature.

This study investigated the effect of daily oral administration with allicin levels (0, 5 and 10 mg/kg of female body weight), 30 days pre-insemination, on reproductive performance in vivo and in vitro, immunity, and oxidative stress of rabbit does under high ambient temperature. Niliparous NZW does (n = 105) were randomly divided into three groups (35 in each) treated with 0, 5 and 10 mg allicin dissolved in 2 ml distilled water, respectively, for 30 days pre-insemination. At the end of treatment (30 days), does were artificially inseminated with fresh diluted semen of 20 fertile NZW bucks. Reproductive performance and ovulatory response parameters were determined. Serum biochemicals, enzyme activity, immunoglobulins (IgG and IgM) and antioxidant status were determined on day 30 of treatment. Serum progesterone and prolactin were determined pre-insemination (30 days of treatment), on 15 days of pregnancy and 7 days post-partum. Results showed that both allicin levels increased live litter size, and bunny viability rat and litter size at birth and weaning. Allicin levels increased ovulation rate and improved embryo quality. Number of total follicles decreased only with 10 mg allicin. Progesterone increased pre-insemination, 15 days of pregnancy and 7 days post-partum progesterone by allicin levels. Prolactin pre-insemination and on day 7 post-partum increased with 10 mg allicin. Serum total proteins, albumin, globulin, IgG and IgM increased, while glucose, aspartate and alanine aminotransaminases, and thiobarbituric acid reaction decreased by both allicin levels. In conclusion, the mechanism by which allicin administration 30 days pre-insemination to improve the reproductive performance of rabbit does is based on that allicin can play an important role, as a natural exogenous antioxidant, increasing immune response and reducing lipid peroxidation.

The effects of thiosulfinates on methane production from anaerobic co-digestion of waste activated sludge and food waste and mitigate method.

Thiosulfinates, a natural antibiotic, existed in all parts of Allium, therefore might be accumulated in large amounts in food waste (FW). FW was often added into waste activated sludge (WAS) anaerobic digestion process as a kind of supplement for nutrition balance. However, the impact of thiosulfinates on methane production and the possible approach to mitigate its inhibition on the co-digestion process could be available in few literatures. This work was carried out in a series of batch experiment at pH 7.0 ±â€¯0.2 and 35 ±â€¯1.0 ℃ to promote the further understanding of this process. The experimental results showed that the methane accumulation decreased from 270.6 ±â€¯13.4 to 16.7 ±â€¯7.0 mL/g VSS (volatile suspended solids) when the initial concentration of thiosulfinates increased from 0 to 2.5 µg/g VSS. The activities of functional enzymes (F420 and CoM) were inhibited by 99.06% and 99.82% compared with control group when reactor contained 2.5 µg/g VSS thiosulfinates. Furthermore, different temperature, pH, and combination pretreat were applied to impair the inhibition of thiosulfinate. Compared with no pretreatment group, methane yield was increased by 2.26, 32.18 and 42.2-fold, respectively which group was under pretreatment method of heat (100 ℃), alkali (pH 9) and combination.

Allicin as add-on therapy for Helicobacter pylori infection: A systematic review and meta-analysis.

BACKGROUND: Allicin (2-propene-1-sulfinothioic acid S-2-propenyl ester, diallyl thiosulfinate) extracted from garlic, has proven activity against Helicobacter pylori (H. Pylori) infection. In recent years, clinical trials have explored its utility as an add-on therapy with variable outcomes reported. AIM: To perform a systemic review of allicin as an add-on treatment for H. Pylori infection and assess its efficacy in randomized controlled trials (RCTs). METHODS: Electronic databases including MEDLINE, EMBASE, the Web of Science, the Cochrane Database, the China National Knowledge Infrastructure Database, Chinese VIP Information Databases, Chinese Medical Databases, and the Wan-Fang Database were searched for keywords including "allicin", "Helicobacter pylori", "randomized clinical trials", and their synonyms. A meta-analysis was performed using the fixed-effects model for low heterogeneity and the random-effects model for high heterogeneity with sensitivity analysis. Bias was evaluated using Egger's tests. Trial sequential analysis (TSA) was used to evaluate information size and treatment benefits. The Grading of Recommendations Assessment, Development and Evaluation (GRADE) was used to assess the level of quality, and studies were classed as "high quality", "moderate quality", "low quality", and "very low quality". RESULTS: A total of eight RCTs consisting of 867 participants (435 from the allicin group and 432 from the control group) were included. Eradication rate in the allicin group (93.33%, 406/435) was significantly higher than that of the control group (83.56%, 361/432) [I 2 = 0%, odds ratio (OR) = 2.75, 95% confidence interval (CI): 1.74-4.35, P < 0.001]. The healing rate of ulcers following H. pylori therapy in the allicin group (86.17%, 349/405) was significantly higher than that of the control group (75.87%, 305/402) [I 2 = 0%, OR = 2.05, 95%CI: 1.39-3.03, P < 0.001]. The total remission rate of peptic ulcers across all allicin groups was 97.16%, which was significantly higher than that of controls [96.05% (389/405) vs 86.55% (360/402), I 2 = 0, OR = 3.04, 95%CI: 1.51-6.12, P = 0.015]. No significant differences in side effects were observed. TSA suggested that the trials were of sufficient standard to draw reliable conclusions. The quality of outcomes including eradication rates and side effects was graded as "very low" due to downgrades for "risk of bias" and "indirectness". Other outcomes such as ulcer healing rates and total ulcer remission rates were graded as "low" due to downgrades for "risk of bias". CONCLUSION: Allicin as an add-on therapy improves H. pylori eradication, healing of ulcers, and remission of symptoms. These results are suggested to be treated with caution due to limited quality.

Allicin Inhibited Staphylococcus aureus -Induced Mastitis by Reducing Lipid Raft Stability via LxRα in Mice.

Mastitis, inflammation of the mammary gland, occurs in both humans and animals. Staphylococcus aureus is the most common infectious bacterial pathogen associated with mastitis. We investigated the effects of allicin on S. aureus-induced mastitis in mice. Pathological histology revealed that allicin inhibited S. aureus-induced pathological damage and myeloperoxidase activity in mammary tissues. Enzyme-linked immunosorbent assays demonstrated that allicin reduced the production of IL-1ß and TNF-α as well as inhibited the NF-κB and mitogen-activated protein kinase pathway by reducing phosphorylation of p65, IκBα, p38, JNK, and ERK. Western blotting revealed that allicin reduced TLR2 and TLR6 expression in mammary tissues and cells but not in HEK293 cells. The lipid raft content was reduced by allicin, which inhibited signaling downstream of TLR2 and TLR6. Liver X receptor α (LXRα) luciferase reporter assays and LXRα interference experiments showed that allicin improved the LXRα activity and adenosine 5'-triphosphate-binding cassette G and A1 (ABCG and ABCA1) expression, thereby reducing the cholesterol level, lipid raft formation, and downstream TLR2 and TLR6 pathway activity. These results demonstrated that allicin exerted anti-inflammatory effects against S. aureus mastitis by improving the LXRα activity and reducing lipid raft formation.

Allicin Bioavailability and Bioequivalence from Garlic Supplements and Garlic Foods.

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 ameliorates cognitive impairment in APP/PS1 mice via Suppressing oxidative stress by Blocking JNK Signaling Pathways.

In middle and old age, Alzheimer's disease (AD) is a progressive neurodegenerative disorder of brain. As an increasingly aging population, AD represents a huge burden for the patients' family and the country. However, current therapeutical strategies have shown limited effectiveness. Allicin, which is the main composition of garlic, was reported to prevent the learning and memory impairment of AD mouse model. As the mechanism is not clear, in this study, we used the APP (amyloid precursor protein)/PS1 (presenilin 1) double transgenic mice, which express human mutant APP and PS1, to determine the protective effect of allicin on neurons. AD involves a broad range of clinical, cellular, and biochemical manifestations. This has led to many views of AD, e.g. the amyloid, presenilin, oxidative stress, and mitochondrial dysfunction. We confirmed that allicin improves the cognitive function of APP/PS1 double transgenic mice by reducing the expression levels of Aß, oxidative stress, and improving mitochondrial dysfunction. Application of behavioral, morphological and molecular biology, and other means were conducted to investigate the effect of allicin, which provide an experimental basis for the reliable application of allicin in the treatment of neurodegenerative diseases.

Allicin functionalized locust bean gum nanoparticles for improved therapeutic efficacy: An in silico, in vitro and in vivo approach.

The field of nanotechnology has overgrown over the past few years and has even ventured into the field of medicine. The aim of the present study is to develop a novel allicin functionalized locust bean gum nanoparticle using the nanoprecipitation technique. The synthesized nanoparticles were characterized by dynamic light scattering, scanning electron microscopy and transmission electron microscopy. The characterization study revealed the nanoscale structure (∼100nm) of the prepared particles. In silico toxicology analysis were carried out to assess the drug-like properties and virtual toxicity of allicin. Toxicity of the prepared nanoparticles were carried out in RAW 264.7 cell lines in vitro and in vivo studies were carried out in Sprague-Dawley rats. In in vitro study, LBGAN showed a maximum toxicity of 10.51% in MTT assay, no reactive oxygen species generation on DCFDA staining and LBGAN was effective to protect the cells from apoptosis. In in vivo toxicity studies LBGAN showed no significant change in the activities of the marker enzymes like LDH, CK-MB, ALP, ACP, AST and ALT. Thus, the functionalization of nanoparticles with allicin has the benefit of providing protection and stability to the allicin, in addition to increasing its pharmacological activity.

The Beneficial Effects of Allicin in Chronic Kidney Disease Are Comparable to Losartan.

Recent studies suggest that allicin may play a role in chronic kidney disease (CKD), reducing hypertension and oxidative stress and improving renal dysfunction. In the present study, CKD was induced by 5/6 nephrectomy and the animals were divided into four treatment groups as follows: control (C), CKD, CKD+allicin (40 mg/kg pathway oral) (CKDA), and CKD+Losartan (20 mg/kg) (CKDL). After CKD induction, the rats developed hypertension from week 3 to the end of the study. This was associated with increased creatinine and blood urea nitrogen (BUN) levels in serum, increased albuminuria, increased urinary excretion of N-acetyl-ß-d-glucosaminidase (NAG), increased nephrin expression, and incrased histological alterations in the cortex. The levels of angiotensin receptors and endothelial nitric oxide synthase (eNOS) were decreased in the renal cortex from the CKD group. Otherwise, lipid and protein oxidation were higher in the CKD group than in the control group. A disturbance was observed in the expression levels of the nuclear factor erythroid 2-related factor 2/Kelch ECH associating protein 1 system (Nrf2/keap1) and the antioxidant enzymes catalase, superoxide dismutase, and heme oxygenase-1. Allicin or losartan treatments relieved renal dysfunction, hypertension, and oxidative stress. In addition, both treatments showed the same efficacy on the expression of angiotensin receptors, the nephrin, Nrf2/keap1 pathway, and eNOS. Further in silico analyses suggest that allicin and losartan could have a common mechanism involving interaction with AT1 receptors. Allicin showed antihypertensive, antioxidant, and nephroprotective effects. The beneficial effects showed by allicin are similar, or even better, than those of losartan. In fact, the effect of allicin on blood pressure and renal function is comparable to reductions seen with losartan, a prescription drug commonly used as a first-line therapy.

Allicin ameliorates doxorubicin-induced cardiotoxicity in rats via suppression of oxidative stress, inflammation and apoptosis.

PURPOSE: Doxorubicin (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. RESULTS: DOX 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-1ß, 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.

Feed degradability, rumen fermentation and blood metabolites in response to essential oil addition to fistulated non-lactating dairy cow diets.

The effects of essential oils (EOs) on ruminal nutrient disappearance, rumen fermentation and blood metabolites in fistulated non-lactating dairy cows were studied. Four fistulated non-lactaing dairy cows were used in a 4 × 4 Latin square design; the experiment consisted of four periods of 21 days in each period, with the first 14 days for adaptation followed by 7 days of measurement period. Animals were fed 3 kg/day of 21% crude protein (CP) concentrate and ad libitum corn silage. Treatments were: (i) control; (ii) 2 mL Allicin/cow/day; (iii) 2 mL zingiberene/cow/day; and (iv) 2 mL citral/cow/day. The results demonstrated that EOs increased dry matter and neutral detergent fiber degradabilities at 48 and 72 h, but had no effect on acid detergent fiber and CP degradabilities. EOs did not change ruminal pH, ammonia nitrogen, protozoa, volatile fatty acid concentrations and blood glucose but reduced blood urea nitrogen at 4 h.

Therapeutic Hotline. Oral allicin in the treatment of Behcet's disease through attenuating oxidative stress: A pilot study in 20 patients with mucocutaneous lesions.

Behçet's disease (BD) involves oxidative stress (OS) aggression and imbalanced oxidant/antioxidant status. Owing to its antioxidant property, allicin is proposed for treating BD. In this study, we aimed to investigate the efficacy and safety of allicin on patients with BD with mucocutaneous involvement. Twenty patients with active BD were treated with allicin for 12 weeks and followed up to 16 weeks. A clinical manifestations index and scoring system was the primary technique for efficacy evaluation at baseline and Week 4, 12, 16. The secondary efficacy variables were OS-related biomarkers determined at first and final visit. Side effects were assessed at each visit. By the end of study, 18 patients completed the trail. Allicin was effective in decreasing ulcer and cutaneous parameters (p < .05). Especially, the greatest reduction of mucocutaneous scores emerged from baseline after the first four-week treatment (p < .05). Meanwhile, allicin remarkably ameliorated OS-related parameters. Besides, some side effects were observed on allicin, these adverse reactions, however, disappeared upon cessation of drugs. In conclusion, allicin is a safe and effective treatment for BD, which may be associated with its inhibiting OS and regulating oxidant/antioxidant status balance.

Effects of Astragalus membranaceus, Codonopsis pilosula and allicin mixture on growth performance, nutrient digestibility, faecal microbial shedding, immune response and meat quality in finishing pigs.

A 12-week trial with 120 [(Landrace×Yorkshire)×Duroc] pigs (45.65 ± 1.93 kg) was conducted to evaluate the effects of Astragalus membranaceus, Codonopsis pilosula and allicin mixture (HM) supplementation on growth performance, nutrient digestibility, faecal microbial shedding, immune response and meat quality in finishing pigs. Pigs were allocated to one of three treatments with 0, 0.025% (HM1) and 0.05% (HM2) HM supplementation in a randomized complete block design according to sex and BW. Each treatment contained 10 replications with four pigs (two barrows and two gilts) per pen. Dietary HM resulted in a higher G:F (p < 0.05) than CON group during weeks 7 to 12 and the overall periods. Pigs fed HM2 diet had higher ADG than pigs fed CON diet. Pigs fed HM2 supplementation diet led to a higher (p < 0.05) apparent total tract digestibility (ATTD) of dry matter (DM) and gross energy (GE) than pigs fed CON diet at week 6, while the supplementation of HM led to a higher (p < 0.05) ATTD of DM and GE than pigs fed CON diet at week 12. The faecal E. coli counts were reduced, and Lactobacillus counts were increased by increasing HM supplementation (p < 0.05). Pigs fed HM1 diet had higher (p < 0.05) WBC concentration than those fed CON and HM2 diets at week 6. Pigs fed HM-supplemented diet had higher (p < 0.05) IgG and IgA concentrations than those fed CON diet at week 12. Pigs fed HM diet noted better (p < 0.05) meat colour and redness value than pigs fed CON diet. Pig fed HM2 reduced (p < 0.05) the lightness value compared with CON group. In conclusion, dietary HM supplementation exerted beneficial effects on growth performance, nutrient digestibility, intestinal microbial balance (increased Lactobacillus counts and decreased E. coli counts), immune response and meat quality.