Chrysin Powder
Also known as: 5,7-dihydroxyflavone, Chrysin powder, flavone derivative, Chrysin
Overview
Chrysin is a natural flavonoid, a type of plant-derived polyphenol, found in various natural sources such as honey, propolis, and passionflower. It is commonly utilized as a dietary supplement due to its potential health benefits. Research primarily investigates chrysin for its antioxidant, anti-inflammatory, anticancer, and hormone-modulating properties. A significant characteristic of chrysin is its poor oral bioavailability, largely attributed to its low aqueous solubility and extensive metabolism within the body. Despite this, enterohepatic recycling helps to prolong its half-life, typically ranging from 3 to 11 hours. While preclinical studies and early clinical trials show promise, high-quality human randomized controlled trial data are limited, making much of the evidence inconclusive.
Benefits
Chrysin has demonstrated several potential benefits, primarily in preclinical settings. Its most notable effect is its anticancer activity, where it has been shown to induce apoptosis (programmed cell death) and autophagy in various cancer cell lines, including breast, lung, and colorectal cancers. This suggests its potential as an adjunct anticancer agent, with in vitro studies showing significant induction of apoptosis. However, human clinical evidence for this effect is currently lacking. Chrysin also exhibits antioxidant and anti-inflammatory properties, which have been observed in in vitro and animal models. While it has been proposed as an aromatase inhibitor to increase testosterone levels, human studies have not shown any significant effect on testosterone or aromatase inhibition. Preclinical evidence suggests benefits in male reproductive function in rodents, but human data are insufficient to support these claims. The time course for anticancer effects is observed over days in cell cultures, while its pharmacokinetics indicate rapid absorption from herbal extracts, though poor bioavailability limits systemic effects.
How it works
Chrysin exerts its effects through several biological pathways. In cancer cells, it induces apoptosis by activating caspases and cleaving PARP, and promotes autophagy by increasing reactive oxygen species (ROS) and inhibiting the Akt/mTOR signaling pathway. It has also been shown to suppress claudin-1 and claudin-11 expression, which affects tight junctions in lung squamous cell carcinoma cells and can enhance the toxicity of anticancer drugs. While chrysin has been theoretically linked to aromatase inhibition, which would reduce estrogen synthesis, this mechanism has not been confirmed in human studies. Its absorption is limited by poor aqueous solubility, but novel formulations like micelles can improve its maximum concentration (Tmax) and overall bioavailability. Despite extensive enterohepatic recycling, which prolongs its half-life, systemic exposure remains limited.
Side effects
Chrysin is generally considered safe when consumed at typical supplement doses, with no significant adverse effects reported in clinical studies. There are no well-documented common side effects (occurring in more than 5% of individuals) in human trials, and serious adverse events have not been reported. However, due to limited data, uncommon or rare side effects are not well characterized. Potential drug interactions exist, as chrysin may modulate UGT enzymes and CYP450 pathways. Therefore, caution is advised when co-administering chrysin with drugs metabolized by these enzyme systems. While no specific contraindications are well-established, theoretical concerns regarding its proposed aromatase inhibition suggest caution in individuals with hormone-sensitive conditions. There is insufficient data to determine the safety of chrysin in special populations such as pregnant or lactating women, or children.
Dosage
The minimum effective dose of chrysin for humans has not been established. Animal studies have utilized doses ranging from 0.23 to 100 mg/kg. Human studies involving propolis or honey, which delivered approximately 54 mg/g of chrysin, did not show any hormonal effects. Consequently, an optimal dose for humans is currently unknown due to the lack of conclusive clinical efficacy data. A maximum safe dose has also not been defined, though no toxicity has been reported at typical supplement doses. The timing of administration can be influenced by the formulation, as faster absorption (Tmax) has been observed with herbal extracts or micelle formulations. Pure chrysin powder has poor solubility, so formulations designed to enhance solubility are recommended to improve pharmacokinetics. No specific cofactors are known to be required for its efficacy.
FAQs
Does chrysin increase testosterone?
Human studies do not support significant increases in testosterone levels or effective aromatase inhibition by chrysin, despite some preclinical findings.
Is chrysin effective as an anticancer agent?
While promising in vitro and animal data exist showing anticancer properties, clinical evidence in humans is currently lacking and inconclusive.
Is chrysin safe?
Chrysin is generally considered safe at typical supplement doses, with no major side effects reported in clinical studies to date.
How can chrysin absorption be improved?
Absorption can be improved by using formulations that increase its solubility, such as micelle formulations, which enhance its bioavailability and Tmax.
Research Sources
- https://digitalscholarship.tsu.edu/cgi/viewcontent.cgi?article=1016&context=facpubs – This review of pharmacokinetic studies, primarily preclinical, highlights chrysin's poor bioavailability due to low solubility and extensive metabolism. It notes that enterohepatic recycling prolongs its half-life and that novel formulations can improve absorption, though human pharmacokinetic data are limited.
- https://pmc.ncbi.nlm.nih.gov/articles/PMC7063143/ – This study, which included an RCT in rats and human observational data, found that chrysin increased sexual function in rats. However, it reported no significant change in urinary testosterone levels in the small human sample, indicating a lack of hormonal effect in humans.
- https://www.tandfonline.com/doi/full/10.1080/10942912.2023.2246678 – This in vitro study on colorectal cancer (CRC) cell lines demonstrated that chrysin induces autophagy and reactive oxygen species (ROS) production. The findings suggest that chrysin's effects are comparable to those of chemotherapy agents in a cell culture setting, indicating potential anticancer activity.
- https://pmc.ncbi.nlm.nih.gov/articles/PMC9845454/ – This systematic review, encompassing 21 in vitro and animal studies, concluded that chrysin induces apoptosis and autophagy in various cancer cells. It identifies chrysin as a potential anticancer agent, though it emphasizes the critical need for human clinical trials to confirm these preclinical findings.
- https://pubs.acs.org/doi/10.1021/acsomega.2c01041 – This in vitro study using human lung squamous cell carcinoma cells found that chrysin reduced the expression of claudin-1 and claudin-11, and inhibited Akt phosphorylation. These actions enhanced the toxicity of anticancer drugs, suggesting a synergistic effect in a laboratory setting.
