Sci Fit Methoxy 500 EX5 - Methyl-7-Methoxy-Isoflavone

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    Sci Fit Methoxy 500 EX5 - Methyl-7-Methoxy-Isoflavone


    Does anyone have any experience with this product or with other products containing "5-Methyl-7-Methoxy-Isoflavone"? It seems too good to be true no matter how much I have read on it.

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    Im using Phyto-Testosterone Caps from Primordial Performance. The methoxy you mention is in it. I have'nt done all my homework on the said ingrediant, but I can tell Phyto-Test is working very well. Ive heard its all about the source you get your extracts from, and they must have found a great supplier. I'll have to look more into this. Im goin to run this again right after a good stack, combined with their Testosterone Recovery Stack.
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    http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2129166/

    I found that study about methoxyisoflavone use in weight training last week. It is just one study, but based on it I don't think the substance is of much value.
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    5-methoxy is different then the newer methylated Flavones such as 7-methoxyflavone found in iforce reversitol v2, the new bioforge and hyperdrol xtreme or whatever they renamed it too . the methylated flavones do show promisse ive read a few studies that have been done on cancer treatment compared to tamox and torem, and its promising to say the least
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    Quote Originally Posted by sanchezgreg18 View Post
    5-methoxy is different then the newer methylated Flavones such as 7-methoxyflavone found in iforce reversitol v2, the new bioforge and hyperdrol xtreme or whatever they renamed it too . the methylated flavones do show promisse ive read a few studies that have been done on cancer treatment compared to tamox and torem, and its promising to say the least
    Any links or were they hard copies? Pretty interesting stuff.
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    lemme see if i can access ne here i looked it up at school were i can access full studies but i may be able to find abstracts
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    Bioavailable flavonoids: cytochrome P450-mediated metabolism of methoxyflavones.

    Walle UK, Walle T.

    Department of Cell and Molecular Pharmacology and Experimental Therapeutics, Medical University of South Carolina, 173 Ashley Avenue, P.O. Box 250505, Charleston, SC 29425, USA.

    Methoxylated flavones were recently shown to be promising cancer chemopreventive agents. Their high metabolic stability compared with the hydroxylated analogs was shown in our laboratory using the human hepatic S9 fraction with cofactors for glucuronidation, sulfation, and oxidation. In the present study, the resistance of methoxylated flavones toward oxidative metabolism was investigated with human liver microsomes and recombinant cytochrome P450 (P450) isoforms. Among 15 methoxylated flavones investigated, the two partially methylated compounds, tectochrysin and kaempferide, were among the most susceptible to microsomal oxidation (Cl(int) 283 and 82 ml/min/kg). Of the fully methylated compounds, 5,7-dimethoxyflavone and 5-methoxyflavone were the most stable (Cl(int) 13 and 18 ml/min/kg, respectively), whereas 4'-methoxyflavone, 3'-methoxyflavone, 5,4'-dimethoxyflavone, and 7,3'-dimethoxyflavone were the least stable (Cl(int) 161, 140, 119, and 92 ml/min/kg, respectively), emphasizing the importance of the positions of the methoxy substituents in the flavone ring system. Among the five P450 isoforms tested, CYP1A1 showed the highest rate of metabolism of fully methylated compounds, followed by CYP1A2 and CYP3A4. CYP2C9 and CYP2D6 gave minimal disappearance of the parent compound. Finally, in incubations with hepatic S9 fraction with cofactors for oxidation and both conjugation reactions, partially methylated flavones, as expected, were much less metabolically stable than fully methylated flavones, confirming that oxidative demethylation is the rate-limiting metabolic reaction for fully methylated flavones only. In summary, the rate of oxidative metabolism of methoxylated flavones, mainly involving CYP1A1 and CYP1A2, varied widely, even between compounds with very similar structures.


    Aromatase inhibition by bioavailable methylated flavones.

    Ta N, Walle T.

    Department of Cell and Molecular Pharmacology & Experimental Therapeutics, Medical University of South Carolina, 173 Ashley Avenue, Charleston, SC 29425, USA.

    Previous studies have shown chrysin, 7-hydroxyflavone and 7,4'-dihydroxyflavone to be the most potent flavonoid inhibitors of aromatase. However, very poor oral bioavailability is a major limitation for the successful use of dietary flavonoids as chemopreventive agents. We have recently shown that methylated flavones, including 5,7-dimethoxyflavone, 7-methoxyflavone and 7,4'-dimethoxyflavone, are much more resistant to metabolism than their unmethylated analogs and have much higher intestinal absorption. In this study, we examined these fully methylated flavones as potential aromatase inhibitors for the prevention and/or treatment of hormone-dependent cancers. Whereas 5,7-dimethoxyflavone had poor effect compared to its unmethylated analog chrysin, 7-methoxyflavone and 7,4'-dimethoxyflavone were almost equipotent to their unmethylated analogs with IC(50) values of 2-9 microM. Thus, some fully methylated flavones appear to have great potential as cancer chemopreventive/chemotherapeutic agents.


    Methylated flavonoids have greatly improved intestinal absorption and metabolic stability.

    Wen X, Walle T.

    Department of Cell and Molecular Pharmacology and Experimental Therapeutics, Medical University of South Carolina, 173 Ashley Ave., P.O. Box 250505, Charleston, SC 29425, USA.

    To better understand the relationship between the chemical structure and biological fate of dietary polyphenols, the hepatic metabolic stability and intestinal absorption of methylated polyphenols, in comparison with unmethylated polyphenols, were investigated in pooled human liver S9 fraction and human colon adenocarcinoma (Caco-2) cells. Consistent with previous in vivo studies, the two well known unmethylated polyphenols resveratrol (3,5,4'-trihydroxystilbene) and quercetin (3,5,7,3',4'-pentahydroxyflavone) were rapidly eliminated by the S9 fraction in the presence of the appropriate cofactors for conjugation and oxidation. In contrast, the methylated flavones, i.e., 7-methoxyflavone, 7,4'-dimethoxyflavone, 5,7-dimethoxyflavone, and 5,7,4'-trimethoxyflavone, were relatively stable, indicating high resistance to hepatic metabolism. The corresponding unmethylated flavones, i.e., 7-hydroxyflavone, 7,4'-dihydroxyflavone, chrysin (5,7-dihydroxyflavone), and apigenin (5,7,4'-trihydroxyflavone), were rapidly eliminated because of extensive glucuronidation and/or sulfation just as resveratrol and quercetin were. The rate of intestinal absorption was evaluated using Caco-2 cells grown in porous inserts. The methylated flavones showed approximately 5- to 8-fold higher apparent permeability (P(app), 22.6-27.6 x 10(-6) cm s(-1)) of apical to basolateral flux than the unmethylated flavones (P(app), 3.0-7.8 x 10(-6) cm s(-1)). The lower P(app) values for the unmethylated flavones correlated with their extensive metabolism in the Caco-2 cells. Thus, combined use of the hepatic S9 fraction and Caco-2 cells will be useful for predicting the oral bioavailability of dietary polyphenols. The higher hepatic metabolic stability and intestinal absorption of the methylated polyphenols make them more favorable than the unmethylated polyphenols to be developed as potential cancer chemopreventive agents.
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    Quote Originally Posted by sanchezgreg18 View Post
    Bioavailable flavonoids: cytochrome P450-mediated metabolism of methoxyflavones.

    Walle UK, Walle T.

    Department of Cell and Molecular Pharmacology and Experimental Therapeutics, Medical University of South Carolina, 173 Ashley Avenue, P.O. Box 250505, Charleston, SC 29425, USA.

    Methoxylated flavones were recently shown to be promising cancer chemopreventive agents. Their high metabolic stability compared with the hydroxylated analogs was shown in our laboratory using the human hepatic S9 fraction with cofactors for glucuronidation, sulfation, and oxidation. In the present study, the resistance of methoxylated flavones toward oxidative metabolism was investigated with human liver microsomes and recombinant cytochrome P450 (P450) isoforms. Among 15 methoxylated flavones investigated, the two partially methylated compounds, tectochrysin and kaempferide, were among the most susceptible to microsomal oxidation (Cl(int) 283 and 82 ml/min/kg). Of the fully methylated compounds, 5,7-dimethoxyflavone and 5-methoxyflavone were the most stable (Cl(int) 13 and 18 ml/min/kg, respectively), whereas 4'-methoxyflavone, 3'-methoxyflavone, 5,4'-dimethoxyflavone, and 7,3'-dimethoxyflavone were the least stable (Cl(int) 161, 140, 119, and 92 ml/min/kg, respectively), emphasizing the importance of the positions of the methoxy substituents in the flavone ring system. Among the five P450 isoforms tested, CYP1A1 showed the highest rate of metabolism of fully methylated compounds, followed by CYP1A2 and CYP3A4. CYP2C9 and CYP2D6 gave minimal disappearance of the parent compound. Finally, in incubations with hepatic S9 fraction with cofactors for oxidation and both conjugation reactions, partially methylated flavones, as expected, were much less metabolically stable than fully methylated flavones, confirming that oxidative demethylation is the rate-limiting metabolic reaction for fully methylated flavones only. In summary, the rate of oxidative metabolism of methoxylated flavones, mainly involving CYP1A1 and CYP1A2, varied widely, even between compounds with very similar structures.


    Aromatase inhibition by bioavailable methylated flavones.

    Ta N, Walle T.

    Department of Cell and Molecular Pharmacology & Experimental Therapeutics, Medical University of South Carolina, 173 Ashley Avenue, Charleston, SC 29425, USA.

    Previous studies have shown chrysin, 7-hydroxyflavone and 7,4'-dihydroxyflavone to be the most potent flavonoid inhibitors of aromatase. However, very poor oral bioavailability is a major limitation for the successful use of dietary flavonoids as chemopreventive agents. We have recently shown that methylated flavones, including 5,7-dimethoxyflavone, 7-methoxyflavone and 7,4'-dimethoxyflavone, are much more resistant to metabolism than their unmethylated analogs and have much higher intestinal absorption. In this study, we examined these fully methylated flavones as potential aromatase inhibitors for the prevention and/or treatment of hormone-dependent cancers. Whereas 5,7-dimethoxyflavone had poor effect compared to its unmethylated analog chrysin, 7-methoxyflavone and 7,4'-dimethoxyflavone were almost equipotent to their unmethylated analogs with IC(50) values of 2-9 microM. Thus, some fully methylated flavones appear to have great potential as cancer chemopreventive/chemotherapeutic agents.


    Methylated flavonoids have greatly improved intestinal absorption and metabolic stability.

    Wen X, Walle T.

    Department of Cell and Molecular Pharmacology and Experimental Therapeutics, Medical University of South Carolina, 173 Ashley Ave., P.O. Box 250505, Charleston, SC 29425, USA.

    To better understand the relationship between the chemical structure and biological fate of dietary polyphenols, the hepatic metabolic stability and intestinal absorption of methylated polyphenols, in comparison with unmethylated polyphenols, were investigated in pooled human liver S9 fraction and human colon adenocarcinoma (Caco-2) cells. Consistent with previous in vivo studies, the two well known unmethylated polyphenols resveratrol (3,5,4'-trihydroxystilbene) and quercetin (3,5,7,3',4'-pentahydroxyflavone) were rapidly eliminated by the S9 fraction in the presence of the appropriate cofactors for conjugation and oxidation. In contrast, the methylated flavones, i.e., 7-methoxyflavone, 7,4'-dimethoxyflavone, 5,7-dimethoxyflavone, and 5,7,4'-trimethoxyflavone, were relatively stable, indicating high resistance to hepatic metabolism. The corresponding unmethylated flavones, i.e., 7-hydroxyflavone, 7,4'-dihydroxyflavone, chrysin (5,7-dihydroxyflavone), and apigenin (5,7,4'-trihydroxyflavone), were rapidly eliminated because of extensive glucuronidation and/or sulfation just as resveratrol and quercetin were. The rate of intestinal absorption was evaluated using Caco-2 cells grown in porous inserts. The methylated flavones showed approximately 5- to 8-fold higher apparent permeability (P(app), 22.6-27.6 x 10(-6) cm s(-1)) of apical to basolateral flux than the unmethylated flavones (P(app), 3.0-7.8 x 10(-6) cm s(-1)). The lower P(app) values for the unmethylated flavones correlated with their extensive metabolism in the Caco-2 cells. Thus, combined use of the hepatic S9 fraction and Caco-2 cells will be useful for predicting the oral bioavailability of dietary polyphenols. The higher hepatic metabolic stability and intestinal absorption of the methylated polyphenols make them more favorable than the unmethylated polyphenols to be developed as potential cancer chemopreventive agents.
    Good compilation. Gracias.
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    heres what the guy from biotivia has said about the 7-methoxyflavone. although he did not provide any references for his statements


    7-methoxyflavone- Aromatase inhibitors have been used extensively by the
    medical community as a means to reduce the amount of estrogen that is produced
    in the body from testosterone. Research studies have reported benefits in men
    using aromatase inhibitors, demonstrating lower estrogen levels and
    simultaneously causing an increase in testosterone levels. Therefore, the use
    of aromatase inhibitors have become common among bodybuilders and other
    strength athletes who want to maintain highest testosterone levels for maximum
    anabolic muscle-building effects, while reducing their estrogen levels.
    Aromatase enzymes are part of the body’s biochemistry system that are used in
    the conversion of testosterone to estrogen. So, when aromatase enzyme activity
    is inhibited , this prevents conversion of testosterone into estrogen thus
    preventing the negative feedback loop in the HPTA(Hypothalamic-Pituitary-
    Testicular-Axis).

    During the researchers constant effort for discovering a naturally occurring
    ( 7-methoxyflavone has been found in extracts from Meliaceae and Rutaceae
    plants) improved aromatase-inhibiting product, their attention was drawn to
    this compound . While several of these substances exhibited high aromatase-
    inhibiting activity, when it came to intestinal absorption and metabolic
    stability in the body, it was determined that there was a clear grouping of the
    majority of flavonoids that scored low(Chrysin anyone?) and only a few that
    scored high. When subjected to independent research, it was determined that 7-
    methoxiflavone had one of the highest aromatase-inhibiting scores, with high
    intestinal absorption and metabolic stability in the body.

    These characteristics are extremely important for developing the most
    effective naturally occurring aromatase inhibitor. Even if a substance has high
    aromatase-inhibiting activity, if it is poorly absorbed or unstable and
    metabolized quickly in the body, it will be ineffective. Therefore 7-
    methoxyflavone is the top choice due to its combination of characteristics
    required for maximum aromatase-inhibiting activity inside the body.

    Flavones are plant chemicals known to be competitive inhibitors of
    cytochrome P450 aromatase with respect to the androgen substrate.

    A welcome plus with the 7-methoxyflavone is that it's not only orally
    available and resistant to metabolism but unlike most flavones it's very
    selective, it inhibits aromatase but not 17beta-hydroxysteroid dehydrogenase
    .

    Optimal 17b-HSD activity is crucial for the endogenous testosterone synthesis
    . The 7-methoxyflavone here shines again.

    An interesting side note: forskolin increases the activity of 3b-HSD.

    The 3beta-HSD complex is responsible for the endogenous conversion of:

    -dehydroepiandrosterone (DHEA) to androstenedione
    -androstenediol to testosterone.

    Biotivia is THE ONLY company getting its 7-methoxyflavone from Indofine
    Chemicals, the company which supplied the ultra-pure flavone for all the
    studies.
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    and just so if anyone didnt kno before the newer flavones that are being used such as the 7-methoxyflavone is not the same as the 5 and 7 methoxyISOflavones they are different
  

  
 

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