Chrysin
Encyclopedia
Chrysin is a naturally occurring flavone chemically extracted from the blue passion flower
Passion flower
Passiflora, known also as the passion flowers or passion vines, is a genus of about 500 species of flowering plants, the namesakes of the family Passifloraceae. They are mostly vines, with some being shrubs, and a few species being herbaceous. For information about the fruit of the passiflora...

 (Passiflora caerulea
Passiflora caerulea
Passiflora caerulea, commonly known as the Blue Passion Flower or the Common Passion Flower, is a vine native to South America...

). Honeycomb also contains small amounts. It is also reported in Oroxylum indicum
Oroxylum indicum
Oroxylum indicum is a species of flowering plant belonging to the family Bignoniaceae.-Names:* Bignonia indica, L., Species Plantarum 2: 625. 1753.* Spathodea indica, L., Pers. Synopsis Plantarum 2: 173. 1807....

or Indian trumpetflower.

Aromatase inhibition

Advertised as an aromatase
Aromatase
Aromatase is an enzyme responsible for a key step in the biosynthesis of estrogens. It is a member of the cytochrome P450 superfamily , which are monooxygenases that catalyze many reactions involved in steroidogenesis. In particular, aromatase is responsible for the aromatization of androgens into...

 inhibitor supplement by bodybuilders and athletes. However, studies done in vivo
In vivo
In vivo is experimentation using a whole, living organism as opposed to a partial or dead organism, or an in vitro controlled environment. Animal testing and clinical trials are two forms of in vivo research...

 show that orally administered chrysin does not have clinical aromatase inhibitor
Aromatase inhibitor
Aromatase inhibitors are a class of drugs used in the treatment of breast cancer and ovarian cancer in postmenopausal women. AIs may also be used off-label to treat or prevent gynaecomastia in men....

activity. This has led to some practitioners administering the drug transdermally(through the skin).

Since chrysin is available as an herbal supplement, some users, for instance body builders, are taking chrysin with the hope of raising testosterone levels or stimulating testosterone production. One study listed below did not find chrysin supplementation to lead to any significant increase in testosterone production.

Chrysin was once believed to be an effective aromatase inhibitor, decreasing the levels of estrogen in the body. However, there is growing consensus that chrysin has no effect on estrogen levels in either animals or humans. Early evidence was reported in the early 1980s through in vitro studies (in the laboratory, as opposed to in the body). Unfortunately, follow-up studies determined that cell membranes effectively block chrysin from entering the cells and having any effect at all on estrogen levels in biological organisms. In vivo (in the body) studies involving biological organisms 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. 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. 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.

Pharmacokinetics

  • Peak plasma chrysin concentrations after oral dose of 400 mg = 3–16 ng mL−1
  • AUC = 5–193 ng mL−1 h
  • Plasma chrysin sulfate concentrations were 30-fold higher (AUC 450–4220 ng mL−1 h).
  • Excretion: urine peak concentration = 0.2–3.1 mg. Most of the dose appeared in faeces as chrysin.

Inflammation

Chrysin has been shown to induce an anti-inflammatory effect, most likely by inhibition of COX-2 expression and via IL-6 signaling.

Anxiety

In rodent in vivo studies, chrysin was found anxiolytic.

In herbal medicine, chrysin is recommended as a remedy for anxiety, but there are no controlled data in humans available.

Many herbal remedies that contain chrysin promote their value as a libido-increasing supplement. There is some in-vivo evidence for chrysin's libido-enhancing effects in rats.

Chrysin demonstrated cell toxicity and inhibition of DNA synthesis at very low concentrations in a normal trout liver cell line.
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