The findings of this study provide evidences that the inedible lotus seedpod could be a source for natural antioxidants and anticancer agents.

PMID: 

Food Sci Nutr. 2019 Sep ;7(9):3062-3070. Epub 2019 Aug 9. PMID: 31572599

Abstract Title: 

Polyphenols extract from lotus seedpod (Gaertn.): Phenolic compositions, antioxidant, and antiproliferative activities.

Abstract: 

Seedpod, the nonedible portion of lotus (Gaertn.), was reported to be rich in polyphenols. The objective of this study was to investigate the major bioactive polyphenols of the lotus seedpods. The total polyphenol content (TPC) from ethanol extract of lotus seedpod (PELS) was found to be 34.23 μg gallic acid equivalents (GAE)/mg extract. Four polyphenolic compounds were identified in the PELS, comprised of one flavan-3-ol (catechin) and three flavonoids (kaemferol, quercetin and hyperoside). In vitro antioxidant and antiproliferative properties of the PELS were evaluated. PELS exhibited 89.38%, 99.82%, 68.25%, and 95.82% scavenging activities against 2,2-diphenyl-1-picrylhydrazyl (DPPH), superoxide, hydroxyl, and 2,2'azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radicals, respectively, at 1.6 mg/ml. The Fereducing power of PELS was 0.605 at 0.32 mg/ml, which is comparable to glutathione (GSH). The PELS showed 31.79% metal chelating capacity and 87.79% inhibition of linoleic acid auto-oxidation at 1.6 mg/ml. PELS showed cytotoxicity toward HepG2 and LNcap cell lines in vitro with ICvalues at 44.59 and 11.50 μg/ml, respectively. The findings of this study provide evidences that the inedible lotus seedpod could be a source for natural antioxidants and anticancer agents.

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Aged garlic extract preserves cutaneous microcirculation in patients with increased risk for cardiovascular diseases.

PMID: 

Int Wound J. 2019 Sep 13. Epub 2019 Sep 13. PMID: 31518044

Abstract Title: 

Aged garlic extract preserves cutaneous microcirculation in patients with increased risk for cardiovascular diseases: A double-blinded placebo-controlled study.

Abstract: 

Laser Doppler velocimetry estimates tissue perfusion providing a record of microvascular blood flow. Patients with heart disease or diabetes mellitus have impaired microvascular perfusion leading to impaired wound healing. Aged garlic extract (AGE) has a positive effect on vascular elasticity. This study aimed to assess the effect of long-term treatment with AGE on cutaneous tissue perfusion. A total of 122 patients with Framingham Risk Score ≥ 10 were randomised in a double-blinded manner to placebo or 2400 mg AGE daily for 1 year and monitored. Cutaneous microcirculation was measured at 0 and 12 months using laser Doppler velocimetry. A repeated measures analysis of variance (ANOVA) with a Greenhouse-Geisser correction determined that mean post-occlusive reactive hyperaemia differed significantly between time points. The mean percent change between the two time points 0 and 12 months was 102, 64 (174, 15)% change for AGE and 78, 62 (107, 92)% change for the placebo group (F[1, 120] = 5. 95, P 

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Alyssin and iberin in cruciferous vegetables exert anticancer activity in HepG2 by increasing intracellular reactive oxygen species.

PMID: 

Biomol Ther (Seoul). 2019 Aug 13. Epub 2019 Aug 13. PMID: 31405267

Abstract Title: 

Alyssin and Iberin in Cruciferous Vegetables Exert Anticancer Activity in HepG2 by Increasing Intracellular Reactive Oxygen Species and Tubulin Depolymerization.

Abstract: 

To determine the chemopreventive potential of alyssin and iberin, theanticancer activities and molecular targets of isothiocyanates (ITCs) were measured and compared to sulforaphane in hepatocellular carcinoma cell HepG2. The SR-FTIR spectra observed a similar pattern vis-à-vis the biomolecular alteration amongst the ITCs-treated cells suggesting a similar mode of action. All of the ITCs in this study cause cancer cell death through both apoptosis and necrosis in concentration dependent manner (20-80 µM). We found no interactions of any of the ITCs studied with DNA. Notwithstanding, all of the ITCs studied increased intracellular reactive oxygen species (ROS) and suppressed tubulin polymerization, which led to cell-cycle arrest in the S and G/M phase. Alyssin possessed the most potent anticancer ability; possibly due to its ability to increase intracellular ROS rather than tubulin depolymerization. Nevertheless, the structural influence of alkyl chain length on anticancer capabilities of ITCs remains inconclusive. The results of this study indicate an optional, potent ITC (viz., alyssin) because of its underlying mechanisms against hepatic cancer. As a consequence, further selection and development of effective chemotherapeutic ITCs is recommended.

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Allicin reversed the process of frailty in aging male Fischer 344 rats with osteoporosis.

PMID: 

J Gerontol A Biol Sci Med Sci. 2019 Sep 21. Epub 2019 Sep 21. PMID: 31541608

Abstract Title: 

Allicin reversed the process of frailty in aging male Fischer 344 rats with osteoporosis.

Abstract: 

The research and development of pharmaceutical intervention is insufficient for the frail elderly, especially in preclinical stage for the frail individuals with osteoporosis. Garlic exerts an anti-osteoporotic effect and its vital component allicin could protect organisms against aging. The present study aimed to investigate the effect of long-term intragastric administration of allicin (low-dose of 4 mg·kg-1·d-1; middle-dose of 8 mg·kg-1·d-1; high-dose of 16 mg·kg-1·d-1) on frailty with osteoporosis in aging male Fischer 344 rats. Frailty was assessed with a 27-item frailty index (FI) based on quantifying health-related deficits in adult male rats varied from 13 to 21 months, and in controlrats from 6 months to 9 months. Osteoporosis was appraised by bone mineral density (BMD) detected by Dual-energy X-ray Absorptiometry (DXA), biomechanical properties measured by a three-point bending test and bone metabolic analysis using ELISA. Allicin could attenuate FI scores by reducing accumulation of health deficits in aging male Fischer 344 rats. Meanwhile, allicin could protect against senile osteoporosis, and the underlying mechanism may involve in increasing low bone turnover through elevation of both bone formation and bone resorption, and subsequently lead to increase of BMD, contributing to reversing deleterious bone biomechanical features associated with aging. The present study reveals firstly that long-term oral administration with allicin attenuated frailty with osteoporosis during the process of aging which provides a preclinical evidence for intervention of frailty.

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S‑allyl‑cysteine sulfoxide alleviates myocardial infarction.

PMID: 

Int J Mol Med. 2019 Sep 26. Epub 2019 Sep 26. PMID: 31573046

Abstract Title: 

S‑allyl‑cysteine sulfoxide (alliin) alleviates myocardial infarction by modulating cardiomyocyte necroptosis and autophagy.

Abstract: 

S‑allyl‑cysteine sulfoxide (alliin) is the main organosulfur component of garlic and its preparations. The present study aimed to examine the protective effect of alliin on cardiac function and the underlying mechanism in a mouse model of myocardial infarction (MI). Notably, alliin treatment preserved heart function, attenuated the area of infarction in the myocardium of mice and reduced lesions in the myocardium, including cardiomyocyte fibrosis and death. Further mechanistic experiments revealed that alliin inhibited necroptosis but promoted autophagy in vitro and in vivo. Cell viability assays showed that alliin dose‑dependently reduced the necroptotic index and inhibited the expression of necroptosis‑related receptor‑interacting protein 1, receptor‑interacting protein 3 and tumor necrosis factor receptor‑associated factor 2, whereas the levels of Beclin 1 and microtubule‑associated protein 1 light chain 3, which are associated with autophagy, exhibited an opposite trend upon treatment with alliin. In addition, the level of peroxisome proliferator‑activated receptor γ was increased by alliin. Collectively, these findings demonstrate that alliin has the potential to protect cardiomyocytes from necroptosis following MI and that this protective effect occurs via the enhancement of autophagy.

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This review is to provide important insights into how particular plant bioactives may influence the development and progression of prostate cancer.

PMID: 

Nutrients. 2019 Sep 18 ;11(9). Epub 2019 Sep 18. PMID: 31540470

Abstract Title: 

Plant Bioactives and the Prevention of Prostate Cancer: Evidence from Human Studies.

Abstract: 

Prostate cancer has become the most common form of non-cutaneous (internal) malignancy in men, accounting for 26% of all new male visceral cancer cases in the UK. The aetiology and pathogenesis of prostate cancer are not understood, but given the age-adjusted geographical variations in prostate cancer incidence quoted in epidemiological studies, there is increasing interest in nutrition as a relevant factor. In particular, foods rich in phytochemicals have been proposed to reduce the risk of prostate cancer. Epidemiological studies have reported evidence that plant-based foods including cruciferous vegetables, garlic, tomatoes, pomegranate and green tea are associated with a significant reduction in the progression of prostate cancer. However, while there is well-documented mechanistic evidence at a cellular level of the manner by which individual dietary components may reduce the risk of prostate cancer or its progression, evidence from intervention studies is limited. Moreover, clinical trials investigating the link between the dietary bioactives found in these foods and prostate cancer have reported varied conclusions. Herein, we review the plant bioactives for which there is substantial evidence from epidemiological and human intervention studies. The aim of this review is to provide important insights into how particular plant bioactives (e.g., sulphur-containing compounds, carotenoids and polyphenols) present in commonly consumed food groups may influence the development and progression of prostate cancer.

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Allicin and its analogues may have potential to be developed as gyrase inhibitors.

PMID: 

Int J Med Microbiol. 2019 Sep 25:151359. Epub 2019 Sep 25. PMID: 31585716

Abstract Title: 

Allicin, a natural antimicrobial defence substance from garlic, inhibits DNA gyrase activity in bacteria.

Abstract: 

Allicin (diallylthiosulfinate) is a potent antimicrobial substance, produced by garlic tissues upon wounding as a defence against pathogens and pests. Allicin is a reactive sulfur species (RSS) that oxidizes accessible cysteines in glutathione and proteins. We used a differential isotopic labelling method (OxICAT) to identify allicin targets in the bacterial proteome. We compared the proteomes of allicin-susceptible Pseudomonas fluorescens Pf0-1 and allicin-tolerant PfAR-1 after a sublethal allicin exposure. Before exposure to allicin, proteins were in a predominantly reduced state, with approximately 77% of proteins showing less than 20% cysteine oxidation. Protein oxidation increased after exposure to allicin, and only 50% of proteins from allicin-susceptible Pf0-1, but 65% from allicin-tolerant PfAR-1, remained less than 20% oxidised. DNA gyrase was identified as an allicin target. Cysin DNA gyrase subunit A (GyrA) was approximately 6% oxidized in untreated bacteria. After allicin treatment the degree of Cysoxidation increased to 55% in susceptible Pf0-1 but only to 10% in tolerant PfAR-1. Allicin inhibited E. coli DNA gyrase activity in vitro in the same concentration range as nalidixic acid. Purified PfAR-1 DNA gyrase was inhibited to greater extent by allicin in vitro than the Pf0-1 enzyme. Substituting PfAR-1 GyrA into Pf0-1 rendered the exchange mutants more susceptible to allicin than the Pf0-1 wild type. Taken together, these results suggest that GyrA was protected from oxidation in vivo in the allicin-tolerant PfAR-1 background, rather than the PfAR-1 GyrA subunit being intrinsically less susceptible to oxidation by allicin than the Pf0-1 GyrA subunit. DNA gyrase is a target for medicinally important antibiotics; thus, allicin and its analogues may have potential to be developed as gyrase inhibitors, either alone or in conjunction with other therapeutics.

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These findings suggest that water fraction extracts of garlic have a clear anti-inflammatory effect on Der p-induced allergic asthma.

PMID: 

Int J Mol Sci. 2019 Oct 1 ;20(19). Epub 2019 Oct 1. PMID: 31581442

Abstract Title: 

Comparing the Protection Imparted by Different Fraction Extracts of Garlic (L.) against Der p-Induced Allergic Airway Inflammation in Mice.

Abstract: 

Garlic (L.) has been used extensively as a food ingredient and medicinally, but the effect on asthmatic airway inflammation has not been studied in detail. We accordingly explored the protective effects exerted by various garlic fraction extracts against airway inflammation with(Der p)-induced allergic asthma in vivo and in vitro. Garlic extraction was realized using n-hexane, dichloromethane, ethylacetate, n-butanol, and water in sequence to obtain different fraction extracts. Mice were orally administered different fractions (80 mg/kg) daily for four weeks. The histological results showed that the water fraction could ameliorate lung-based goblet cell hyperplasia, inflammatory cell infiltration, and mucus hypersecretion. The water fraction extracts decreased IgE and IgG1, and they decreased inflammatory cells as quantified in bronchoalveolar lavage fluid (BALF); however, they increased IgG2a in serum. Moreover, the water fraction extracts increased IFN-γ and IL-12 (both constituting Th1 cytokines) in BALF, but they reduced IL-13, -4, and -5 (all constituting Th2 cytokines), and also inhibited the expression of IL-1β, IL-6, and TNF-α. The water fraction also inhibited the PI3K/Akt/NF-κB signal pathways in A549 cells. These findings suggest thatwater fraction extracts of garlic have a clear anti-inflammatory effect on Der p-induced allergic asthma.

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Fermented black garlic could be used for reducing the risk of cardiovascular disease.

PMID: 

J Agric Food Chem. 2019 Oct 7. Epub 2019 Oct 7. PMID: 31588747

Abstract Title: 

Metabolomics for Biomarker Discovery in Fermented Black Garlic and Potential Bioprotective Responses against Cardiovascular Diseases.

Abstract: 

Fermented black garlic has multiple beneficial biological activities, including cardiovascular protection, anticancer, hepatoprotective and antibacterial properties. In this study, metabolic differences in the properties of black and fresh garlic were investigated via LC-Q/TOF-based metabolomics, leading to the identification of characteristic components. Fermented black garlic samples and their Amadori products (AC) promoted angiogenesis, prevented thrombus formation by rescuing chemical-induced vascular lesions in zebrafish and inhibited H2O2-induced injury of endothelial cells, thus reducing the risk of cardiovascular disease. AC suppressed activation of the MAPK pathway through inhibition of p38 and ERK1/2 phosphorylation, in turn, increasing the availability of c-Fos/c-Jun or c-Jun/c-Jun complexes for apoptotic resistance. Clarification of the associated signaling pathways should therefore provide a solid foundation for optimization of black garlic-based therapies.

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Syzygium aromaticum aqueous extract inhibits human neutrophils myeloperoxidase and protects mice from LPS-induced lung inflammation.

PMID: 

Pharm Biol. 2019 Dec ;57(1):56-64. PMID: 30707845

Abstract Title: 

Syzygium aromaticum aqueous extract inhibits human neutrophils myeloperoxidase and protects mice from LPS-induced lung inflammation.

Abstract: 

CONTEXT: Syzygium aromaticum (L.) Merr.&Perry (Myrtaceae), commonly known as clove, originally found in the Muluku Islands in East Indonesia, is widely used as a spice and has numerous medicinal properties.OBJECTIVE: This study investigated the antioxidant potential of S. aromaticum aqueous extract (SAAE) in vitro and its protective effects on lipopolysaccharide (LPS)-induced lung inflammation in mice.MATERIAL AND METHODS: Neutrophils were isolated from healthy donors and reactive oxygen species (ROS) generation was measured by luminol-amplified chemiluminescence. Superoxide anion generation was detected by cytochrome c reduction assay. HOwas detected by DCFH fluorescence assay. Myeloperoxidase (MPO) activity was mesured by tetramethyl benzidine oxidation method. To study the anti-inflammatory activity of SAAE, lung inflammation was induced in mice (BALB/c) by intra-tracheal instillation of lypopolysaccharide (5 µg/mouse), and SAAE (200 mg/kg body weight) was injected intraperitoneally prior to LPS administration. Bronchoalveolar lavage and lung tissue were collected to assess inflammatory cells count and total protein content. Metalloproteinases activity was detected by zymography technique.RESULTS: SAAE inhibited luminol-amplified chemiluminescence of resting neutrophils and N-formyl-methionyl-leucyl-phenylalanine- or phorbol myristate acetate-stimulated neutrophils, with an inhibitory effect starting at a concentration as low as 0.5 µg/mL. Moreover, SAAE reduced significantly MPO activity and it exhibits a dose-dependent action (IC= 0.5 µg/mL). In vivo results showed that SAAE decreased markedly neutrophil count (From 61% to 15%) and proteins leakage into bronchoalveolar lavage fluid. Gelatin zymography assay showed that S. aromaticum inhibited MMP-2 (15%) and MMP-9 (18%) activity in lung homogenates.DISCUSSION AND CONCLUSION: Our results suggest that the anti-inflammatory activity of SAAE, in vivo, is due to the inhibition of ROS production and metalloproteinases activity via its action on MPO. According to these findings, SAAE could be a potential source of new compounds with anti-inflammatory activity.

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