Broccoli or Sulforaphane: Is It the Source or Dose That ...

3.1. Sulforaphane Pharmacokinetics and Pharmacodynamics

Upon entry into the mammalian cell, sulforaphane is conjugated with GSH in a GST-catalyzed reaction, entering the mercapturic acid pathway (Scheme 1e). The glutathione conjugate of sulforaphane is subjected to a series of sequential conversions catalyzed by γ-glutamyltranspeptidase (γGT), followed by cysteinylglycinase (CGase), and N-acetyltransferase (NAT). The final product is the N-acetylcysteine conjugate of sulforaphane (mercapturic acid). In addition, sulforaphane can undergo an interconversion to erucin [1-isothiocyanato-4-(methylthio)butane], which is then metabolized in an identical manner to that for sulforaphane [48,49].

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Sulforaphane and its metabolites (dithiocarbamates) can be quantified collectively by cyclocondensation with 1,2-benzenedithiol, with sensitivity in the picomolar range [50]. This highly sensitive, simple and convenient method has been widely used to measure the levels of sulforaphane and its metabolites in blood, plasma, urine and tissues following sulforaphane administration to rodents and humans. The use of this method revealed that sulforaphane crosses the placental barrier based on detection of dithiocarbamates in embryos 2 h post-treatment of pregnant mice with a single (5 μmol) dose of sulforaphane [51]. In addition, methods have been developed to analyze the individual metabolites following their separation by liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS) [52,53]. Furthermore, the use of mass spectrometry coupled with stable isotope-labeled internal standards of sulforaphane [1-isothiocyanato-4-methyl-sulfinyl(1,1,2,2,3,3,4,4-2H8)butane] and its corresponding mercapturic acid pathway conjugates allows for quantitative, precise, sensitive, and specific analysis of sulforaphane and its metabolites [54].

With these analytical tools in hand, a number of pharmacokinetic studies have been conducted in rodents and humans. Thus, following oral administration of an exceedingly high dose of 150 μmol sulforaphane to 10-week-old female Sprague&#;Dawley rats, the concentration of dithiocarbamates in the plasma of the animals increased rapidly reaching a peak (Cmax) of 60 μM 1 h after dosing, with area under the concentration curve (AUC) of 491 h μmol/L, elimination constant (Kel) of 0.1 h&#;1, and elimination half-life of 6.7 h [55]. Similarly, following oral administration of 200 μmol broccoli sprout isothiocyanates to four healthy human volunteers, the peak plasma dithiocarbamate concentration (Cmax) was 1.91 ± 0.24 (0.943&#;2.27) μM 1 h after dosing, with half-life of 1.77 ± 0.13 h, and clearance of 369 ± 53 mL/min [56]. A study in 20 participants administered 200 μmol sulforaphane as sulforaphane-rich powder in capsules reported a Cmax of 0.7 ± 0.2 µM at 3 h, with a half-life of 1.9 ± 0.4 h for elimination of sulforaphane equivalents measured by mass spectrometry [57]. Another pharmacokinetic study, in which a single dose of broccoli soup delivering the equivalent of either 16 μmol or 52 μmol of sulforaphane was administered, reported Cmax of 2.2 ± 0.8 µM and 7.3 ± 2.9 µM at 1.5 h and 2 h for the low and the high dose, respectively [53]. A double-blinded, randomized crossover trial with broccoli soups (prepared from plants with increased glucoraphanin content) delivering a single dose of 84, 280, or 452 μmol of glucoraphanin documented peak plasma concentrations (Cmax) of 0.17 ± 0.12, 0.37 ± 0.26, and 0.61 ± 0.40 μM, respectively [52]. Another study reported plasma dithiocarbamate levels of 0.92 ± 0.72 μM and mean epithelial-/stromal-enriched breast tissue dithiocarbamate concentration of 1.45 ± 1.12 and 2.00 ± 1.95 pmol/mg tissue for the right and the left breast, respectively in eight healthy women undergoing reduction mammoplasty who had received a single dose of a broccoli sprout preparation delivering 200 μmol sulforaphane 1 h prior to surgery [55].

In a double-blind randomized placebo-controlled trial in men presenting for prostate biopsy, plasma levels of 0.12 µM of sulforaphane and its metabolites were detected after an intervention period of 4&#;8 weeks with two daily doses of 100 μmol sulforaphane administered 12 h apart [58]. Isothiocyanate levels of 2.2&#;µM and 500&#;nM were detected in the plasma and synovial fluid, respectively of patients with osteoarthritis undergoing knee replacement surgery following consumption of glucosinolate-rich diets for 2 weeks [59].

A study in healthy subjects who received single oral doses of broccoli sprout extracts containing the equivalent of 111 µmol of glucosinolates or isothiocyanates showed cumulative urinary dithiocarbamate excretion of 88.9 ± 5.5 μmol and 13.1 ± 1.9 μmol for the isothiocyanate and the glucosinolate preparation, respectively [60]. This study further revealed that for the isothiocyanate preparation, excretion was consistent and linear over a 25&#;200 μmol dose range, whereas for the glucosinolate preparation, excretion was highly variable among individuals. These observations are in close agreement with results from a randomized, placebo-controlled, double-blind Phase I clinical trial, in which isothiocyanate (25 μmol)- or glucosinolate (25 μmol or 100 μmol)-rich preparations were orally administered to three cohorts of three healthy human subjects at 8-h intervals for 7 days; one other subject in each cohort received placebo [61]. Notably, this study showed no evidence of clinically significant adverse events based on 32 types of hematology and chemistry tests, including liver (transaminases) and thyroid (TSH, T3, and T4) function tests. In agreement, a recent analysis of biochemical parameters of thyroid function in serum collected from 45 female volunteers that had participated in a randomized clinical trial revealed no alterations compared to baseline following an intervention for 12 weeks with a broccoli sprout beverage containing a combination of 40 μmol sulforaphane and 600 μmol of glucoraphanin [62].

The finding that compared to isothiocyanates, oral administration of glucosinolates results in lower bioavailability, slower elimination, and greater inter-individual variation in excretion was further strengthened by a larger (50 participants) crossover clinical trial that involved 5-day baseline period followed by daily administration of broccoli sprout beverages delivering either glucosinolates or their corresponding isothiocyanates for 7 days, 5-day washout period, and 7-day administration of the opposite intervention [63]. Using fecal sample collections from five subjects with high 24-h urinary excretion profiles (&#;high converters&#;) and five subjects with low excretion profiles (&#;low converters&#;), it was found that ex vivo, the degradation of glucoraphanin was greater in cultures of fecal bacteria derived from the &#;high converters&#; in comparison to the &#;low converters&#; [64]. These observations are consistent with earlier work showing that mechanical cleansing or antibiotic treatment greatly reduce the glucosinolate conversion in healthy human subjects [26] and indicate that the gastrointestinal microflora represents a critical factor in determining the extent of gl ucosinolate hydrolysis. In addition to the inter-individual variations, there are also diurnal variations in the conversion of glucosinolates to dithiocarbamates, whereby conversion is greater during the day [65]. By contrast, the conversion of isothiocyanates to dithiocarbamates is higher during the night.

Overall, in humans, sulforaphane is rapidly absorbed and eliminated with small inter-individual variations and typical urinary excretion of 70% to 90% of the dose. By contrast, the conversion of glucoraphanin is slow and with high inter-individual variations. The urinary excretion of sulforaphane metabolites following intervention with glucoraphanin-containing preparations typically range from 2% to 15% of the dose, being 1% to 45% at the extremes. The differences in inter-individual variations between sulforaphane and glucoraphanin make, at first glance, the use of sulforaphane much more attractive for the purposes of dose precision. However, in contrast to its stable glucosinolate precursor, sulforaphane is unstable, which has prompted the development of stabilized preparations, such as an α-cyclodextrin-encapsulated form of sulforaphane [66] and a stabilized version of pure plant-derived sulforaphane, known as Prostaphane® (Nutrinov, Noyal sur Vilaine Cedex, France). Alternatively, glucoraphanin-rich preparations containing active myrosinase have also been used [67,68]. As formulations differ in their bioavailability (which provides a possible explanation for the differences in pharmacokinetic parameters reported in the various human studies), the excreted amount of sulforaphane metabolites in the urine, and not the amount in the administered preparation, provides a more reliable measure of the actual dose [69].

Similar to the studies of the pharmacokinetics of sulforaphane, nearly all human studies addressing the pharmacodynamics of sulforaphane have used glucoraphanin- or sulforaphane-rich broccoli-based preparations. Although there is currently no direct evidence for specific target engagement by sulforaphane in humans, there is clear evidence for its pharmacodynamic action. Thus, increased levels of the Nrf2-target enzymes A-class GSTs and NQO1 have been reported in plasma [70] and saliva [71] of human subjects consuming cruciferous vegetables. In agreement, administration of glucoraphanin/sulforaphane-rich preparations to healthy volunteers resulted in increased mRNA or protein levels of NQO1 and GSTs in PBMC, skin punch biopsies, as well as in nasal and buccal scrapings [72,73,74,75,76].

Broccoli-based glucoraphanin/sulforaphane-rich preparations have been shown to accelerate the detoxication and excretion of potentially carcinogenetic food contaminants and air pollutants, offering a very attractive strategy for population-wide reduction in cancer risk due to unavoidable exposures to pollution. A cross-over clinical trial with 50 human volunteers, which was conducted in Qidong, China, found statistically significant increases of 20&#;50% in the urinary excretion levels of glutathione-derived conjugates of the air pollutants acrolein and benzene following consumption of sulforaphane- and/or glucoraphanin-rich broccoli sprout-derived beverages [77]. A subsequent 12-week placebo-controlled, randomized clinical trial involving 291 participants from the same area using broccoli sprout beverages containing a combination of 40 μmol sulforaphane and 600 μmol glucoraphanin confirmed and extended these findings by showing that the excretion levels of the glutathione-derived conjugates of benzene and acrolein were significantly increased, by 61% and 23%, respectively in the volunteers who received the broccoli sprout beverage compared with placebo [78]. Very recently, a randomized, placebo-controlled, multidose intervention trial of a broccoli sprout beverage, which was conducted in the same area of China, showed a dose-dependent excretion of the urinary metabolites of sulforaphane, and further found that a treatment regime with daily doses of 40 μmol sulforaphane and 600 μmol glucoraphanin for 10 days, resulting in an urinary excretion of &#;25 μmol sulforaphane metabolites per day, promotes the detoxication of benzene [69].

Global gene expression profiling to evaluate the transcriptional changes in the prostate of men at high risk for prostate cancer has revealed that consumption of broccoli-rich diets for 6- or 12 months associates with transcriptional changes in signaling pathways involved in inflammation and carcinogenesis in the prostate tissue [79,80]; importantly, these changes are dose-dependently attenuated in subjects receiving the glucoraphanin-rich diet [80]. Other pharmacodynamic effects of interventions with glucoraphanin/sulforaphane in humans include: Increase in the levels of reduced glutathione in brain [81], enhanced integration of fatty acid β-oxidation with TCA cycle activity [82], protection against skin erythema caused by exposure to ultraviolet radiation [83,84], reduction in plasma LDL-cholesterol [85], decrease in the levels of fasting blood glucose and glycated hemoglobin in obese patients with dysregulated type 2 diabetes [86], and improvements in social interaction, behavior, and verbal communication in young men with autism spectrum disorder [87]. Overall, although the precise molecular mediators are not always known, it is clear that interventions with glucoraphanin/sulforaphane-rich broccoli preparations in humans lead to diverse beneficial effects.

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Broccoli is a variety of cabbage, otherwise known as green cauliflower. It has been in our kitchen for a very long time, but we can also find it in dietary supplements and food additives. This green vegetable surprises us with its phenomenal and irreplaceable taste, as well as its wealth of vitamins and minerals. [1]

Bio broccoli powder was created from selected vegetables, free from contamination by pesticides, herbicides and heavy metals, so we can be sure that we are using the highest quality product. In addition, powdered broccoli will be a more concentrated source of minerals and vitamins, compared to the fresh vegetable. We can use this powder in smoothies, pancakes, waffles and even pancakes.

Bio broccoli powder contains 195 calories in 100 grams. This value is mainly due to protein &#; there are as many as 30 grams of it. Daily menus are often deficient in protein, which is essential for growth, maintaining proper muscle mass and bone health. It is worthwhile to enrich the daily diet with vegetable protein, which is found in abundance in broccoli powder. In addition, it contains a small amount of fat, so people on low-fat and reduction diets can include it in their diet. [2]

Fiber is another ingredient in which the diet is often deficient. It affects the reduction of intestinal transit time and increases the weight of the stool, thus preventing constipation. Broccoli powder contains as much as 27 grams of fiber, making it a very good source of fiber. [3]

Broccoli and blood production

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Folic acid, or vitamin B9, is an essential ingredient for the proper functioning of the body. This is because it is needed for the formation of red blood cells and metabolizing homocysteine. Sources of vitamin B9 are green vegetables, including broccoli powder, which contains as much as 0.4 mg of it, which meets 216% of the daily requirement. Children, malnourished people, pregnant women and people with anemia have an increased need for folic acid. It will be an ideal variety to the menu in terms of taste and nutrition. [4]

Broccoli to boost immunity

Broccoli powder contains as much as 961 mg of vitamin C. It is essential for the proper formation of collagen and increases the absorption of nonheme iron &#; that is, the one found in plant products. Simply adding some broccoli powder to an iron-rich meal is enough to increase the absorption of nonheme iron.

Vitamin C, otherwise known as ascorbic acid, is involved in protecting DNA, proteins and lipids from oxidative damage. Thus, we can call it a powerful antioxidant that fights free radicals that negatively affect our health. [5]

Broccoli powder is also a good source of iron, containing as much as 9 mg of it. Iron, in turn, is essential for the formation of erythrocytes, oxygen transport, and cell division thanks to which it reduces fatigue and improves cognitive function.

Broccoli for hypertension

Broccoli powder is a product that contains a significant amount of potassium, as much as mg, which covers almost twice the daily norm for this element. Potassium influences the proper functioning of the neuromuscular system and the maintenance of normal blood pressure. A diet rich in this element has an impact on lowering blood pressure. [6]

Broccoli and insulin resistance and diabetes

Broccoli is a vegetable with a glycemic index of 15, so people with impaired carbohydrate metabolism can include it in their diet. It will work perfectly as an addition to your favorite dish &#; it will add a beautiful green color and a new flavor. People who are mainly limited to a low glycemic index often have trouble composing diverse and tasty problems &#; which is another argument for its use.

Broccoli powder is a product whose already small amount improves the taste of a dish, so it does not significantly affect the energy value of the dish. It is therefore recommended for those on reduction diets.

Healthy smoothie with bio broccoli Biowen

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