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Chrysin ist ein natürlich vorkommendes Flavon, eine Art von Flavonoid. Es ist in den Passionsblumen Passiflora caerulea [1] und Passiflora incarnata, [2] gefunden worden sowie in Oroxylum indicum. Es wird auch in Kamilleund dem Pilz Austernseitling gefunden.
Aromatase -Hemmung
[Bearbeiten | Quelltext bearbeiten]Bei hohen Konzentrationen wird von Chrysin berichtet, dass eine [ [ Aromatasehemmer ] ] [ [ in vitro ] ] Referenzfehler: Es fehlt ein schließendes </ref>
. Early evidence was reported in the early 1980s through in vitro studies.[3][4][5][6][7][8][9] Follow-up studies determined that cell membranes effectively block chrysin from entering the cells and having any effect at all on estrogen levels in organisms.[5][10][11]
In vivo studies lend support to the observation that chrysin has no effect on estrogen levels, but may have other detrimental effects to the body, particularly to thyroid function.[12] For instance, a 30 day study administered chrysin to four groups of mice both orally and via injection to examine chrysin's effect on serum estrogen levels. The results showed that chrysin had no effect on estrogen levels. Further, the mice treated with chrysin became considerably fatter, possibly due to chrysin's ability to disrupt thyroid function.[13] Another study on rats administered 50 mg of chrysin per kg body weight, considerably more than found in dietary supplements. Chrysin was found to have no ability to inhibit aromatase, possibly due to poor absorption or bioavailability.[11]
Pharmacokinetics
[Bearbeiten | Quelltext bearbeiten]- Peak plasma chrysin concentrations after oral dose of 400 mg = 3–16 ng mL−1 [14]
- AUC = 5–193 ng mL−1 h [14]
- Plasma chrysin sulfate concentrations were 30-fold higher (AUC 450–4220 ng mL−1 h).[14]
- Excretion: urine peak concentration = 0.2–3.1 mg. Most of the dose appeared in feces as chrysin.[14]
Inflammation
[Bearbeiten | Quelltext bearbeiten]In vitro study shows that chrysin inhibits COX-2 expression and via IL-6 signaling,[15] which may contribute to anti-inflammatory effects.
Anxiety
[Bearbeiten | Quelltext bearbeiten]In a 1997 rodent study, chrysin injections displayed dose-dependent anxiolytic effects similar to that of diazepam. Unlike diazepam, the training and test performance of rats injected with chrysin was not significantly reduced. The authors proposed that chrysin does not produce the cognitive impairment usually associated with benzodiazepine medications.[2][1] However, oral bioavailability of chrysin is still very poor.
Toxicity
[Bearbeiten | Quelltext bearbeiten]Chrysin demonstrated cell toxicity and inhibition of DNA synthesis at very low concentrations in a normal trout liver cell line.[16]
Einzelnachweise
[Bearbeiten | Quelltext bearbeiten]- ↑ a b Wolfman C, Viola H, Paladini A, Dajas F, Medina JH: Possible anxiolytic effects of chrysin, a central benzodiazepine receptor ligand isolated from Passiflora coerulea. In: Pharmacol. Biochem. Behav. 47. Jahrgang, Nr. 1, Januar 1994, S. 1–4, doi:10.1016/0091-3057(94)90103-1, PMID 7906886.
- ↑ a b Brown E, Hurd NS, McCall S, Ceremuga TE: Evaluation of the anxiolytic effects of chrysin, a Passiflora incarnata extract, in the laboratory rat. In: AANA J. 75. Jahrgang, Nr. 5, Oktober 2007, S. 333–7, PMID 17966676.
- ↑ Kellis JT, Vickery LE: Inhibition of human estrogen synthetase (aromatase) by flavones. In: Science. 225. Jahrgang, Nr. 4666, September 1984, S. 1032–4, doi:10.1126/science.6474163, PMID 6474163 (sciencemag.org).
- ↑ Ibrahim AR, Abul-Hajj YJ: Aromatase inhibition by flavonoids. In: J. Steroid Biochem. Mol. Biol. 37. Jahrgang, Nr. 2, Oktober 1990, S. 257–60, doi:10.1016/0960-0760(90)90335-I, PMID 2268557.
- ↑ a b Campbell DR, Kurzer MS: Flavonoid inhibition of aromatase enzyme activity in human preadipocytes. In: J. Steroid Biochem. Mol. Biol. 46. Jahrgang, Nr. 3, September 1993, S. 381–8, doi:10.1016/0960-0760(93)90228-O, PMID 9831487.
- ↑ Wang C, Mäkelä T, Hase T, Adlercreutz H, Kurzer MS: Lignans and flavonoids inhibit aromatase enzyme in human preadipocytes. In: J. Steroid Biochem. Mol. Biol. 50. Jahrgang, Nr. 3–4, August 1994, S. 205–12, doi:10.1016/0960-0760(94)90030-2, PMID 8049151.
- ↑ Pelissero C, Lenczowski MJ, Chinzi D, Davail-Cuisset B, Sumpter JP, Fostier A: Effects of flavonoids on aromatase activity, an in vitro study. In: J. Steroid Biochem. Mol. Biol. 57. Jahrgang, Nr. 3–4, Februar 1996, S. 215–23, doi:10.1016/0960-0760(95)00261-8, PMID 8645631 (elsevier.com).
- ↑ Le Bail JC, Laroche T, Marre-Fournier F, Habrioux G: Aromatase and 17β-hydroxysteroid dehydrogenase inhibition by flavonoids. In: Cancer Lett. 133. Jahrgang, Nr. 1, November 1998, S. 101–6, doi:10.1016/S0304-3835(98)00211-0, PMID 9929167 (elsevier.com).
- ↑ Jeong HJ, Shin YG, Kim IH, Pezzuto JM: Inhibition of aromatase activity by flavonoids. In: Arch. Pharm. Res. 22. Jahrgang, Nr. 3, Juni 1999, S. 309–12, doi:10.1007/BF02976369, PMID 10403137.
- ↑ King DS, Sharp RL, Vukovich MD, et al.: Effect of oral androstenedione on serum testosterone and adaptations to resistance training in young men: a randomized controlled trial. In: JAMA. 281. Jahrgang, Nr. 21, Juni 1999, S. 2020–8, doi:10.1001/jama.281.21.2020, PMID 10359391 (ama-assn.org). [see comments]
- ↑ a b Referenzfehler: Ungültiges
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-Tag; kein Text angegeben für Einzelnachweis mit dem Namen Saarinen2001. - ↑ Koehrle J, Auf'mkolk M, Spanka M, Irmscher K, Cody V, Hesch RD: Iodothyronine deiodinase is inhibited by plant flavonoids. In: Prog. Clin. Biol. Res. 213. Jahrgang, 1986, S. 359–71, PMID 3086894.
- ↑ Shibayama, J. The Oral Bioavailability and In Vivo Activity of Chrysin in Exercising and Non-Exercising Mice. Submitted for publication, as reported by VRP article (by W. Dean)
- ↑ a b c d Walle T, Otake Y, Brubaker JA, Walle UK, Halushka PV: Disposition and metabolism of the flavonoid chrysin in normal volunteers. In: Br J Clin Pharmacol. 51. Jahrgang, Nr. 2, Februar 2001, S. 143–6, doi:10.1111/j.1365-2125.2001.01317.x, PMID 11259985, PMC 2014445 (freier Volltext).
- ↑ Woo KJ, Jeong YJ, Inoue H, Park JW, Kwon TK: Chrysin suppresses lipopolysaccharide-induced cyclooxygenase-2 expression through the inhibition of nuclear factor for IL-6 (NF-IL6) DNA-binding activity. In: FEBS Lett. 579. Jahrgang, Nr. 3, Januar 2005, S. 705–11, doi:10.1016/j.febslet.2004.12.048, PMID 15670832.
- ↑ Tsuji PA, Walle T.: Cytotoxic effects of the dietary flavones chrysin and apigenin in a normal trout liver cell line. In: Chem Biol Interact. 171. Jahrgang, Nr. 1, 2008, S. 37–44, doi:10.1016/j.cbi.2007.08.007, PMID 17884029, PMC 2219546 (freier Volltext).