Medical Forum / General / Nutrition / December 2006
Grapefruit Seed Extract (GSE) Toxic
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Bob Arnold - 07 Dec 2006 03:30 GMT There are studies showing that the antibiotic effect from Grapefruit Seed Extract has nothing to do with grapeseed, but actually synthetic agents:
Aspects of the antimicrobial efficacy of grapefruit seed extract and its relation to preservative substances contained.
Pharmazie. 1999 Jun;54(6):452-6. von Woedtke T, Schluter B, Pflegel P, Lindequist U, Julich WD. Institute of Pharmacy, Ernst Moritz Arndt University, Germany.
The antimicrobial efficacy as well as the content of preservative agents of six commercially available grapefruit seed extracts were examined. Five of the six extracts showed a high growth inhibiting activity against the test germs Bacillus subtilis SBUG 14, Micrococcus flavus SBUG 16, Staphylococcus aureus SBUG 11, Serratia marcescens SBUG 9, Escherichia coli SBUG 17, Proteus mirabilis SBUG 47, and Candida maltosa SBUG 700. In all of the antimicrobial active grapefruit seed extracts, the preservative benzethonium chloride was detected by thin layer chromatography. Additionally, three extracts contained the preserving substances triclosan and methyl parabene. In only one of the grapefruit seed extracts tested no preservative agent was found. However, with this extract as well as with several self-made extracts from seed and juiceless pulp of grapefruits (Citrus paradisi) no antimicrobial activity could be detected (standard serial broth dilution assay, agar diffusion test). Thus, it is concluded that the potent as well as nearly universal antimicrobial activity being attributed to grapefruit seed extract is merely due to the synthetic preservative agents contained within. Natural products with antimicrobial activity do not appear to be present. http://pmid.us/10399191
Identification of benzethonium chloride in commercial grapefruit seed extracts.
Takeoka G, Dao L, Wong RY, Lundin R, Mahoney N. J Agric Food Chem. 2001 Jul;49(7):3316-20. Western Regional Research Center, Agricultural Research Service, U.S. Department of Agriculture
Commercial grapefruit seed extracts (GSE) were extracted with chloroform. The solvent was evaporated, and the resulting solid was subsequently analyzed by high-performance liquid chromatography, electrospray ionization mass spectrometry, nuclear magnetic resonance (NMR) spectroscopy, and elemental analysis (by proton-induced X-ray emission [PIXE] analysis). The main constituent was identified as benzethonium chloride, a synthetic antimicrobial agent commonly used in cosmetics and other topical applications. This compound comprised 8.03% (n = 2) of the liquid GSE sample. Higher amounts of benzethonium chloride were found in powder GSE samples. http://pmid.us/11453769
Companies that sell GSE insist that the study results were "false positives" and they are actually detecting similar compounds that naturally occur in grapeseed. However, more recent studies used high-performance chromatography and spectrometry, which are not likely to be wrong:
Development and validation of an HPLC/UV/MS method for simultaneous determination of 18 preservatives in grapefruit seed extract.
Ganzera M, Aberham A, Stuppner H. J Agric Food Chem. 2006 May 31;54(11):3768-72. Institute of Pharmacy, University of Innsbruck
Grapefruit seed extracts are used in cosmetics, food supplements, and pesticides because of their antimicrobial properties, but suspicions about the true nature of the active compounds arose when synthetic disinfectants such as benzethonium or benzalkonium chloride were found in commercial products. The HPLC method presented herein allows the quality assessment (qualitative and quantitative) of these products for the first time. On the basis of a standard mixture of 18 preservatives most relevant for food and grapefruit products, a method was developed allowing the baseline separation of all compounds within 40 min. Optimum results were obtained with a C-8 stationary phase and a solvent system comprising aqueous trifluoroacetic acid, acetonitrile, and 2-propanol. The assay was fully validated and shown to be sensitive (LOD < or= 12.1 ng on-column), accurate (recovery rates > or = 96.1%), repeatable (sigma(rel) < or = 3.5%), precise (intra-day variation < or = 4.5%, interday variation < or = 4.1%), and rugged. Without any modifications the method could be adopted for LC-MS experiments, where the compounds of interest were directly assignable in positive ESI mode. The quantitative results of several products for ecofarming confirmed previous studies, as seven out of nine specimens were adulterated with preservatives in varying composition. The samples either contained benzethonium chloride (2.5-176.9 mg/mL) or benzalkonium chloride (138.2-236.3 mg/mL), together with smaller amounts of 4-hydroxybenzoic acid esters, benzoic acid, and salicylic acid. http://pmid.us/16719494
Identification of benzalkonium chloride in commercial grapefruit seed extracts.
Takeoka GR, Dao LT, Wong RY, Harden LA. J Agric Food Chem. 2005 Sep 21;53(19):7630-6. Western Regional Research Center, Agricultural Research Service, US Department of Agriculture
Commercial grapefruit seed extracts (GSE) were extracted with chloroform. The solvent was evaporated, and the resulting solid was subsequently analyzed by high-performance liquid chromatography (HPLC), electrospray ionization mass spectrometry (ESI/MS), tandem mass spectrometry (ESI/MS/MS), and elemental analysis (by proton-induced X-ray emission analysis). Three major constituents were observed by HPLC and were identified as benzyldimethyldodecylammonium chloride, benzyldimethyltetradecylammonium chloride, and benzyldimethylhexadecylammonium chloride. This mixture of homologues is commonly known as benzalkonium chloride, a widely used synthetic antimicrobial ingredient used in cleaning and disinfection agents. http://pmid.us/16159196
Grapeseed extract is not a good idea. The pesticides are toxic and not natural.
Bob
NWCurandero - 07 Dec 2006 04:51 GMT > There are studies showing that the antibiotic effect from Grapefruit > Seed Extract has nothing to do with grapeseed, but actually synthetic [quoted text clipped - 111 lines] > > Bob This issue comes up every few months. From having reviewed the literature extensively I can tell you that there are probably just as many articles with research and testing that indicate grapefriut seed extraxt is safe and effective.
>From personal use of grapefruit seed extract, I can tell you that it cured my stubborn yeast infection when four different prescription medications could not touch it--all without side effects. With this kind of results, I can see why Big Pharma has a lot to fear from this stuff.
NWCurandero - 07 Dec 2006 05:33 GMT Below are some PubMed articles on the safety and effectiveness of grapefruit seed extract.
Antimicrobial activity of grapefruit seed and pulp ethanolic extract.Cvetnic Z, Vladimir-Knezevic S. Department of Microbiology, Faculty of Pharmacy and Biochemistry, University of Zagreb, Croatia.
Antibacterial and antifungal activity of ethanolic extract of grapefruit (Citrus paradisi Macf., Rutaceae) seed and pulp was examined against 20 bacterial and 10 yeast strains. The level of antimicrobial effects was established using an in vitro agar assay and standard broth dilution susceptibility test. The contents of 3.92% of total polyphenols and 0.11% of flavonoids were determined spectrometrically in crude ethanolic extract. The presence of flavanones naringin and hesperidin in the extract was confirmed by TLC analysis. Ethanolic extract exibited the strongest antimicrobial effect against Salmonella enteritidis (MIC 2.06%, m/V). Other tested bacteria and yeasts were sensitive to extract concentrations ranging from 4.13% to 16.50% (m/V).
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Krajewska-Kulak E, Lukaszuk C, Niczyporuk W. Zaklad Teorii Pielegniarstwa Akademii Medycznej w Bialystoku, 15-096 Bialystok, ul. M. C. Sklodowskiej 7a.
Grapefruit seed extract was discovered by Jacob Harich an american immunologist in 1980. Assessment of the influence of grapefruit extract on the yeast-like fungi strains--Candida albicans growth. Material used in this investigation was ATCC test Candida albicans strains no 10231, 200 of Candida albicans strains, 5 of Candida sp. strains isolated from patients with candidiasis symptoms from different ontocenosis and 12 of dermatophytes and moulds isolated from patients. The susceptibility of the Candida was determined by serial dilution method. It seems that 33% grapefruit extract exert a potent antifungal activity against the yeast like fungi strains and had low activity against dermatophytes and moulds. Further studies in vitro and in vivo on greater number of the yeast-like fungi strains and other fungi species are needed.
PMID: 16886437 [PubMed - indexed for MEDLINE]
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Cvetnic Z, Vladimir-Knezevic S. Department of Microbiology, Faculty of Pharmacy and Biochemistry, University of Zagreb, Croatia.
Antibacterial and antifungal activity of ethanolic extract of grapefruit (Citrus paradisi Macf., Rutaceae) seed and pulp was examined against 20 bacterial and 10 yeast strains. The level of antimicrobial effects was established using an in vitro agar assay and standard broth dilution susceptibility test. The contents of 3.92% of total polyphenols and 0.11% of flavonoids were determined spectrometrically in crude ethanolic extract. The presence of flavanones naringin and hesperidin in the extract was confirmed by TLC analysis. Ethanolic extract exibited the strongest antimicrobial effect against Salmonella enteritidis (MIC 2.06%, m/V). Other tested bacteria and yeasts were sensitive to extract concentrations ranging from 4.13% to 16.50% (m/V).
PMID: 15610620 [PubMed - indexed for MEDLINE]
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Heggers JP, Cottingham J, Gusman J, Reagor L, McCoy L, Carino E, Cox R, Zhao JG. Department of Surgery (Plastic), School of Medicine, University of Texas Medical Branch, Galveston, USA.
OBJECTIVES: Recent testimonials report grapefruit-seed extract, or GSE (Citricidal) to be effective against more than 800 bacterial and viral strains, 100 strains of fungus, and a large number of single and multicelled parasites. This study investigated GSE for antibacterial activity at varying time intervals and concentration levels and tissue toxicity at varying concentrations in an effort to determine if a concentration existed that was both microbicidal and nontoxic and in what period of time. DESIGN: Gram-negative and gram-positive isolates were introduced into graduated dilutions of GSE (twofold concentrations ranging from 1:1, through 1:512) for determination of bacterial activity. In vitro assays with human skin fibroblast cells were also performed at the same dilutions to determine toxicity. RESULTS: These tests indicated that from the 1:1 through the 1:128 concentrations, GSE remained toxic as well as bactericidal. However, test results indicated that at the 1:512 dilution, GSE remained bactericidal, but completely nontoxic. CONCLUSIONS: The initial data shows GSE to have antimicrobial properties against a wide range of gram-negative and gram-positive organisms at dilutions found to be safe. With the aid of scanning transmission electron microscopy (STEM), the mechanism of GSE's antibacterial activity was revealed. It was evident that GSE disrupts the bacterial membrane and liberates the cytoplasmic contents within 15 minutes after contact even at more dilute concentrations.
PMID: 12165191 [PubMed - indexed for MEDLINE]
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Reagor L, Gusman J, McCoy L, Carino E, Heggers JP. School of Medicine, University of Texas, Medical Branch, Galveston, USA.
OBJECTIVES: Grapefruit-seed extract (GSE) Citricidal has, in recent reports, been reported to be successful in combating a variety of common infectious agents. In our study, drops of concentrated grapefruit-seed extract were tested for antibacterial properties against a number of gram-positive and gram-negative organisms. DESIGN: Sixty-seven (67) distinct biotypes were tested for their susceptibilities to the GSE as well as to 5 other topical antibacterials (Silvadene, Sulfamylon, Bactroban, Nitrofurazone, and Silvadene, Nystatin). Wells were punched into Mueller-Hinton agar plates, which were then inoculated with the organism to be tested; each well was then inoculated with one of the antibacterial agents. After an overnight incubation period, the plates were checked for zones of bacterial susceptibility around the individual wells, with a measured susceptibility zone diameter of 10 mm or more considered a positive result. RESULTS: The GSE was consistently antibacterial against all of the biotypes tested, with susceptibility zone diameters equal to or greater than 15 mm in each case. CONCLUSIONS: Our preliminary data thus suggest an antibacterial characteristic to GSE that is comparable to that of proven topical antibacterials. Although the GSE appeared to have a somewhat greater inhibitory effect on gram-positive organisms than on gram-negative organisms, its comparative effectiveness against a wide range of bacterial biotypes is significant.
PMID: 12165190 [PubMed - indexed for MEDLINE]
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Lopez L, Romero J, Ureta F. Facultad de Ciencias Quimicas y Farmaceuticas, Universidad de Chile, Santiago de Chile.
There is a wide offer of disinfectant products, for the food industry, available in the market, such as chlorine, iodine and quaternary ammonium compounds and their respective derivatives. However, new alternative products have emerged, for instance grapefruit seed extract, and peracetic and lactic acids. The present study was carried out in order to analyze in vitro the germicide effect, from the grapefruit seed extract (400 ppm), peracetic acid (2000 ppm) and lactic acid (20,000 ppm) at the manufacturer recommended action time, and other additional times. The germicide effect was tested against microorganisms such as Escherichia coli, Staphylococcus aureus, Streptococcus faecalis and Pseudomonas aeruginosa. In each case, the death kinetic was determined through the evaluation of the germicide effect (%), specific death rate (t-1) and the decimal reduction time (min). From the evaluated products, the best germicidal effect at the manufacturer conditions was reached by peracetic acid (2000 ppm) at 1 min, which presented the lower decimal reduction times compared with the other tested microorganisms. Generally speaking, Gram positive microorganisms showed a greater sensibility to the disinfectant action.
PMID: 12214551 [PubMed - indexed for MEDLINE]
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Dembinski A, Warzecha Z, Konturek SJ, Ceranowicz P, Dembinski M, Pawlik WW, Kusnierz-Cabala B, Naskalski JW. Department of Physiology, Jagiellonian University Medical School, 16 Grzegorzecka Street, 31-531 Cracow, Poland.
Grapefruit seed extract (GSE) has been shown to exert antibacterial, antifungal and antioxidant activity possibly due to the presence of naringenin, the flavonoid with cytoprotective action on the gastric mucosa. No study so far has been undertaken to determine whether this GSE is also capable of preventing acute pancreatic damage induced by ischemia/reperfusion (I/R), which is known to result from reduction of anti-oxidative capability of pancreatic tissue, and whether its possible preventive effect involves an antioxidative action of this biocomponent. In this study carried out on rats with acute hemorrhagic pancreatitis induced by 30 min partial pancreatic ischemia followed by 6 h of reperfusion, the GSE or vehicle (vegetable glycerin) was applied intragastrically in gradually increasing amounts (50-500 microl) 30 min before I/R. Pretreatment with GSE decreased the extent of pancreatitis with maximal protective effect of GSE at the dose 250 microl. GSE reduced the pancreatitis-evoked increase in serum lipase and poly-C specific ribonuclease activity, and attenuated the marked fall in pancreatic blood flow and pancreatic DNA synthesis. GSE administered alone increased significantly pancreatic tissue content of lipid peroxidation products, malondialdehyde and 4-hydroxyalkens, and when administered before I/R, GSE reduced the pancreatitis-induced lipid peroxidation. We conclude that GSE exerts protective activity against I/R-induced pancreatitis probably due to the activation of antioxidative mechanisms in the pancreas and the improvement of pancreatic blood flow.
PMID: 15613745 [PubMed - indexed for MEDLINE]
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Bob Arnold - 07 Dec 2006 13:46 GMT > Below are some PubMed articles on the safety and effectiveness of > grapefruit seed extract. I'm glad it worked so well for you.
I removed all the studies below that did not address safety, leaving two. The fact that GSE contains synthetic disinfection agents doesn't make it ineffective. In fact synthetics would only make it more a "effective" antimicrobial, but not safe. Also, the case that GSE contains natural antibacterials does not mean it doesn't also contain synthetic disinfection agents.
In the 1st study, it says, "These tests indicated that from the 1:1 through the 1:128 concentrations, GSE remained toxic..."
The 2nd study did not look at toxicity in general, but I left it in. The study is testing it's antioxidant activity, which was negative when GSE was administered alone. Also, the case that the isolated flavonoid naringenin might be cytoprotective (not addressed in the study) again does not mean GSE doesn't also contain toxic synthetic disinfection agents. I would love for GSE to be safe and effective. But, you haven't convinced me.
> Heggers JP, Cottingham J, Gusman J, Reagor L, McCoy L, Carino E, Cox R, > Zhao JG. [quoted text clipped - 61 lines] > > *********************************************************
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