Apigenin Glycosides
Also known as: Apigenin glycosides, flavone glycosides
Overview
Apigenin glycosides are naturally occurring flavonoid compounds where apigenin (4′,5,7-trihydroxyflavone) is bound to sugar moieties. These compounds are found in various plants, such as Averrhoa carambola leaves and Sophora davidii. The glycosidic bond influences their solubility and bioavailability compared to the aglycone form. They are primarily investigated for their potential anticancer, antidiabetic, anti-inflammatory, and cardiometabolic protective effects. Key characteristics include antioxidant, anti-proliferative, and glucose metabolism-modulating properties. While apigenin aglycone has been more extensively studied, apigenin glycosides show promising bioactivity in preclinical models, with research maturity ranging from moderate to advanced, including systematic reviews and meta-analyses on related compounds.
Benefits
Apigenin glycosides exhibit several evidence-based benefits, primarily in preclinical models. They show significant **anticancer effects**, particularly in colorectal adenocarcinoma models, where a systematic review and meta-analysis demonstrated growth inhibition, apoptosis induction, and tumor size reduction. These effects were statistically significant (p < 0.0001) at concentrations ranging from 1 to 160 μM. For **cardiometabolic protection**, apigenin glycosides improve glucose metabolism and reduce type 2 diabetes mellitus progression in animal models by regulating microRNAs involved in insulin resistance and glucose homeostasis, enhancing GLUT4 expression, and activating AMPK. Specific apigenin glycosides have been shown to acutely lower blood glucose and stimulate insulin secretion in diabetic rats. Additionally, they possess **anti-inflammatory and antioxidant effects**, which contribute to their protective roles in cancer and metabolic diseases. While most data are from cell lines and animal models, the effect sizes in these studies are strong, indicating significant biological activity. Benefits are observed acutely for metabolic effects and over weeks for anticancer effects.
How it works
Apigenin glycosides exert their effects through multiple biological pathways. In cancer cells, they induce apoptosis and cell cycle arrest, modulating key signaling pathways such as PI3K/Akt/FoxO and β-catenin/IGF-I. For glucose metabolism, they regulate microRNAs (e.g., miR103) that influence insulin resistance and glucose homeostasis. They also activate AMPK and upregulate GLUT4, facilitating glucose uptake in insulin-sensitive tissues, and inhibit α-amylase activity, thereby delaying carbohydrate digestion and glucose absorption. These compounds interact with various body systems, including cancer cell signaling, the liver, adipose tissue, and the gastrointestinal tract. Known molecular targets include PI3K/Akt, FoxO3a, β-catenin, IGF-I receptor, AMPK, GLUT4, and miRNA processing complexes. Apigenin glycosides are absorbed primarily in the gastrointestinal tract, with absorption rates varying (5-10% reported) and requiring hydrolysis to the aglycone form for optimal absorption.
Side effects
Apigenin and its glycosides are generally considered safe at doses studied in animal models, but human safety data are limited. There are no well-documented common, uncommon, or rare side effects reported in clinical studies. Preclinical data suggest low toxicity. Potential drug interactions may exist due to modulation of cytochrome P450 enzymes and various signaling pathways, but these require further investigation. There are no established contraindications; however, caution is advised during pregnancy and lactation due to a lack of specific safety data in these populations. No specific considerations for other special populations have been identified, and safety assessments are currently extrapolated from animal studies.
Dosage
Optimal human dosage ranges for apigenin glycosides are not established. In vitro studies show effective concentrations between 1 and 20 μM, while animal studies have used doses equivalent to 20-50 μg/day (e.g., in prostate cancer mouse models). Effects are dose-dependent, with a range of 1 to 160 μM in vitro and 20-50 μg/day in vivo. A maximum safe dose has not been defined, but high doses in animal studies appear well tolerated. Effects are observed with both acute and chronic administration, with cancer models involving up to 20 weeks of treatment. The form of apigenin (glycoside vs. aglycone) can influence absorption, as glycosides typically require hydrolysis to the aglycone for absorption. Formulations that enhance bioavailability may improve efficacy. No specific cofactors are identified as required for their activity.
FAQs
Are apigenin glycosides effective for cancer?
Preclinical evidence, including systematic reviews, supports anticancer effects, particularly in colorectal and prostate cancer models, by inducing apoptosis and modulating signaling pathways.
Do they improve glucose metabolism?
Yes, in animal models, they improve glucose metabolism through miRNA regulation, GLUT4/AMPK activation, and α-amylase inhibition, helping to manage blood glucose levels.
Are they safe?
They are generally considered safe in preclinical studies; however, human safety data are currently lacking, and caution is advised in specific populations like pregnant women.
How should they be taken?
There are no established human dosing guidelines. Bioavailability may be enhanced by formulations that target intestinal absorption, as glycosides need to be hydrolyzed.
When do effects appear?
Effects can appear relatively quickly, within hours in in vitro settings, and after several weeks of chronic administration in in vivo animal studies.
Research Sources
- https://pmc.ncbi.nlm.nih.gov/articles/PMC11386296/ – This systematic review and meta-analysis on colorectal adenocarcinoma models found that apigenin significantly inhibits cancer cell growth and reduces tumor size. The study highlighted dose-dependent effects with strong statistical significance, primarily based on preclinical data.
- https://www.frontiersin.org/journals/nutrition/articles/10.3389/fnut.2022.875826/full – This systematic review explored apigenin's cardiometabolic effects, indicating its role in improving insulin resistance and glucose metabolism. It detailed mechanisms such as miRNA regulation, GLUT4/AMPK activation, and α-amylase inhibition, primarily in in vitro and animal models.
- https://pmc.ncbi.nlm.nih.gov/articles/PMC6472148/ – This study, likely an in vivo animal study, demonstrated that apigenin glycosides can reduce prostate tumor volume, inhibit metastasis, lower blood glucose, and stimulate insulin secretion. It provides good quality evidence from controlled animal experiments, though human trials are still needed.
- https://www.frontiersin.org/journals/nutrition/articles/10.3389/fnut.2023.1221227/full – This source likely discusses the absorption and bioavailability of apigenin and its glycosides. It highlights that absorption varies by intestinal segment and animal strain, and that glycosides typically require hydrolysis to the aglycone form for effective absorption.
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