Apigenin

Apigenin is a naturally occurring flavonoid and is one of the most abundant secondary plant compounds in the human diet. It occurs in numerous types of vegetables and herbs, found particularly abundantly in parsley, chamomile, celery, artichokes, oregano, and the ashitaba plant (Angelica keiskei). Chemically, Apigenin is characterized by a simple structure, which at the same time gives it high stability – one reason why it serves in the plant world as an effective protective agent against UV radiation, microorganisms, and oxidative damage.

In research, Apigenin is gaining increasing importance, as it acts on cellular processes in many different ways. Its health effects – including antioxidant, anti-inflammatory, and potentially anticancer properties – are currently being intensively investigated. Particularly in connection with chronic diseases, hormone regulation, and neurodegenerative processes, Apigenin is being discussed as an interesting candidate for therapeutic and preventive applications.

What benefits does Apigenin offer?

The health benefits attributed to Apigenin through the results of various studies are diverse. Although the expected potential is great, it is still important to put the study results into critical perspective. They are not all readily transferable; this applies above all to the results from animal studies. Far more research is needed to understand all the processes that apigenin influences in the human body. Here is a selection of various potential effects that have already been investigated in studies:

  • Antioxidant cell protection: In studies, apigenin neutralized free radicals and could thereby inhibit cell damage and premature aging processes (1,2,3).
  • Anti-inflammatory: According to investigations, the flavonoid has an inhibitory effect on inflammatory mediators and could alleviate inflammation-related complaints, e.g., in arthritis or autoimmune diseases (2,4,5).
  • Anticancer: In preclinical studies, apigenin showed the potential to inhibit tumor growth, block cancer cell division, and promote apoptosis in malignant cells (6,7,8).
  • Neuroprotective: Apigenin can protect nerve cells from oxidative damage and is promising in accompanying research on Alzheimer's and other neurological diseases (2,9,10,11).

How does Apigenin work?

In studies, apigenin influenced various biological processes:

  • Signaling pathways: It modulates central cellular processes such as the NF-κB and PI3K/Akt/mTOR signaling pathways (12).
  • Enzyme inhibition: It inhibits pro-inflammatory enzymes (e.g., COX-2) as well as aromatase – an enzyme that plays a role in hormone-dependent cancers (13).
  • Cellular protective mechanisms: Apigenin activates genes and proteins that set antioxidant protective mechanisms in motion (14).

Use and dosage

Apigenin can easily be obtained through a plant-rich diet. For targeted effects, highly concentrated dietary supplements are also used. Various dosages were used in studies. Because of its limited bioavailability, research is currently being conducted on improved delivery forms such as liposomal preparations.

Are there side effects?

  • Generally well tolerated: In usual amounts from food, apigenin is safe.
  • Sedative effect: It could have a calming effect – especially in concentrated form (15).
  • Interactions: Apigenin could influence liver enzymes and thus alter the effect of certain medications.

Conclusion

Apigenin is a versatile flavonoid with great health potential. In studies, it showed antioxidant and anti-inflammatory properties, among others, and could play an important role in plant-based preventive medicine and the complementary therapy of chronic diseases in the future. However, far more research is needed before conclusive statements about its effects can be made.

Sources:

  1. Fidelis Q.C., Faraone I., Russo D., Aragão Catunda F.E., Jr., Vignola L., de Carvalho M.G., de Tommasi N., Milella L. Chemical and Biological insights of Ouratea hexasperma (A. St.-Hil.) Baill.: A source of bioactive compounds with multifunctional properties. Nat. Prod. Res. 2018:1–4. doi: 10.1080/14786419.2017.1419227.
  2. Salehi, B., Venditti, A., Sharifi-Rad, M., Kręgiel, D., Sharifi-Rad, J., Durazzo, A., Lucarini, M., Santini, A., Souto, E. B., Novellino, E., Antolak, H., Azzini, E., Setzer, W. N., & Martins, N. (2019). The Therapeutic Potential of Apigenin. International journal of molecular sciences, 20(6), 1305. https://doi.org/10.3390/ijms20061305
  3. Zamani F, Samiei F, Mousavi Z, Azari MR, Seydi E, Pourahmad J. Apigenin ameliorates oxidative stress and mitochondrial damage induced by multiwall carbon nanotubes in rat kidney mitochondria. J Biochem Mol Toxicol. 2021 Jun;35(6):1-7. doi: 10.1002/jbt.22762. Epub 2021 Mar 16. PMID: 33724625.
  4. Lim R., Barker G., Wall C.A., Lappas M. Dietary phytophenols curcumin, naringenin and apigenin reduce infection-induced inflammatory and contractile pathways in human placenta, foetal membranes and myometrium. Mol. Hum. Reprod. 2013;19:451–462. doi: 10.1093/molehr/gat015.
  5. Arsić, I., Tadić, V., Vlaović, D., Homšek, I., Vesić, S., Isailović, G. and Vuleta, G. (2011), Preparation of novel apigenin-enriched, liposomal and non-liposomal, antiinflammatory topical formulations as substitutes for corticosteroid therapy. Phytother. Res., 25: 228-233. https://doi.org/10.1002/ptr.3245
  6. Zhou X., Wang F., Zhou R., Song X., Xie M. Apigenin: A current review on its beneficial biological activities. J. Food Biochem. 2017;41:e12376. doi: 10.1111/jfbc.12376.
  7. Woo, J.S.; Choo, G.S.; Yoo, E.S.; Kim, S.H.; Lee, J.H.; Han, S.H.; Kim, H.J.; Jung, S.H.; Park, Y.S.; Kim, B.S.; et al. Apigenin induces apoptosis by regulating Akt and MAPK pathways in human melanoma cell A375SM. Mol. Med. Rep. 2020, 22, 4877–4889.
  8. Fu, J.; Zeng, W.; Chen, M.; Huang, L.; Li, S.; Li, Z.; Pan, Q.; Lv, S.; Yang, X.; Wang, Y.; et al. Apigenin suppresses tumor angiogenesis and growth via inhibiting HIF-1α expression in non-small cell lung carcinoma. Chem.-Biol. Interact. 2022, 361, 109966.
  9. Zhao L., Wang J., Liu R., Li X.X., Li J., Zhang L. Neuroprotective, anti-amyloidogenic and neurotrophic effects of apigenin in an Alzheimer’s disease mouse model. Molecules. 2013;18:9949–9965. doi: 10.3390/molecules18089949.
  10. Liu, R.; Zhang, T.; Yang, H.; Lan, X.; Ying, J.; Du, G. The flavonoid apigenin protects brain neurovascular coupling against amyloid-β 25-35-induced toxicity in mice. J. Alzheimer’s Dis. 2011, 24, 85–100.
  11. Allemailem, K. S., Almatroudi, A., Alharbi, H. O. A., AlSuhaymi, N., Alsugoor, M. H., Aldakheel, F. M., Khan, A. A., & Rahmani, A. H. (2024). Apigenin: A Bioflavonoid with a Promising Role in Disease Prevention and Treatment. Biomedicines, 12(6), 1353. https://doi.org/10.3390/biomedicines12061353
  12. Malik, S.; Suchal, K.; Khan, S.I.; Bhatia, J.; Kishore, K.; Dinda, A.K.; Arya, D.S. Apigenin ameliorates streptozotocin-induced diabetic nephropathy in rats via MAPK-NF-κB-TNF-α and TGF-β1-MAPK-fibronectin pathways. Am. J. Physiol. Ren. Physiol. 2017, 313, F414–F422.
  13. Lee, J.H.; Zhou, H.Y.; Cho, S.Y.; Kim, Y.S.; Lee, Y.S.; Jeong, C.S. Anti-inflammatory mechanisms of apigenin: Inhibition of cyclooxygenase-2 expression, adhesion of monocytes to human umbilical vein endothelial cells, and expression of cellular adhesion molecules. Arch. Pharmacal Res. 2007, 30, 1318–1327.
  14. Almatroodi, S.A.; Khan, A.A.; Aloliqi, A.A.; Ali Syed, M.; Rahmani, A.H. Therapeutic Potential of Ajwa Dates (Phoenix dactylifera) Extract in Prevention of Benzo (a) pyrene-Induced Lung Injury through the Modulation of Oxidative Stress, Inflammation, and Cell Signalling Molecules. Appl. Sci. 2022, 12, 6784.
  15. Ross, J.A.; Kasum, C.M. Dietary flavonoids: Bioavailability metabolic effects, and safety. Annu. Rev. Nutr. 2002, 22, 19–34.