• M AZEEM Faculty of Pharmacy, Hamdarad University Islamabad Campus, Pakistan
  • HAA KHARL Department of Pharmacy, University of Agriculture Faisalabad, Pakistan
  • S NIAZI Yusra Institute of Pharmaceutical Sciences Islamabad, Pakistan
  • N AMEER Multan University of Science and Technology Multan, Pakistan
  • F FAYYAZ Faculty of Pharmacy, Hamdarad University Islamabad Campus, Pakistan
  • NU HUDA Faculty of Pharmacy, Hamdarad University Islamabad Campus, Pakistan
  • T ZEHRA Faculty of Pharmacy, Hamdarad University Islamabad Campus, Pakistan
  • M AFTAB Faculty of Pharmacy, Hamdarad University Islamabad Campus, Pakistan



Apigenin, Anti-inflammatory, Neuroprotective, Anticancer, Anti-oxidant, Anti-hyperlipidemia, Muscle relaxant


Apigenin (4′, 5, 7,-trihydroxyflavone), a natural glycoside belonging to a class of cyclone, is found in many different forms in plants and vegetables such as grapefruits, parsley, onions, oranges, tea, chamomile, wheat, sprouts, oregano, artichokes and in some seasonings. It effectively treats various anti-inflammatory disorders because it is less toxic, non-mutagenic, and potent against skeletal muscle sarcoplasmic reticulum. Furthermore in combination with allopathic drugs, its activity was enhanced as an anti-inflammatory, antioxidant, cardioprotective, neuroprotective, and anticancer agent. Little data was found that emphasized its role as an anti- hypoglycemic and sedative agent; however, it was found to promote hair growth by inhibiting the TGF-B1 pathway. Different characterization techniques were used to determine physicochemical properties, and various formulations of apigenin with other polymers have been done to enhance its biological role. The literature search used various scholarly search engines (Google Scholar, PubMed, Springer Link, etc.). A total of 355 research articles were reviewed, and it was observed that 34% of articles were about anti-inflammatory, 15% of articles were about neuroprotective, and 10% of studies were about anti-cancer use of apigenin. Thus, the current review focuses on its activity, characterization and limitations of apigenin role.


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Alsadat, A. M., F. Nikbakht, H. H. Nia, F. Golab, Y. Khadem, M. Barati and S. Vazifekhah (2021). "GSK-3β as a target for apigenin-induced neuroprotection against Aβ 25–35 in a rat model of Alzheimer's disease." Neuropeptides 90: 102200.

Asdaq, S. M. B., B. A. Mannasaheb, A. Alanazi, B. Almusharraf, N. Alanazi, K. Saad, S. Alanazi, K. Abduallah, S. Alrashid and F. Alanazi (2021). "Evaluation of skeletal muscle relaxant activity of apigenin in animal experimental models." INTERNATIONAL JOURNAL OF PHARMACOLOGY 17(6): 400-407.

Ashrafizadeh, M., M. R. Bakhoda, Z. Bahmanpour, K. Ilkhani, A. Zarrabi, P. Makvandi, H. Khan, S. Mazaheri, M. Darvish and H. Mirzaei (2020). "Apigenin as a tumor suppressor in cancers: Biotherapeutic activity, nanodelivery, and mechanisms with emphasis on pancreatic cancer." Frontiers in Chemistry 8: 829.

Balez, R., N. Steiner, M. Engel, S. S. Muñoz, J. S. Lum, Y. Wu, D. Wang, P. Vallotton, P. Sachdev and M. O’Connor (2016). "Neuroprotective effects of apigenin against inflammation, neuronal excitability and apoptosis in an induced pluripotent stem cell model of Alzheimer’s disease." Scientific reports 6(1): 1-16.

Bijani, S., R. Dizaji, A. Sharafi and M.-J. Hosseini (2022). "Neuroprotective effect of apigenin on depressive-like behavior: mechanistic approach." Neurochemical Research 47(3): 644-655.

Brad, K. and Y. Zhang (2018). "Study on extraction and purification of apigenin and the physical and chemical properties of its complex with lecithin." Pharmacognosy magazine 14(54): 203.

Cai, S.-Q., Z.-M. Tang, C. Xiong, F.-F. Wu, J.-R. Zhao, Q. Zhang, L. Wang, X.-N. Zhang and X.-H. Zhao (2022). "The anti-inflammatory effects of apigenin and genistein on the rat intestinal epithelial (IEC-6) cells with TNF-α stimulation in response to heat treatment." Current Research in Food Science.

Cannataro, R., A. Fazio, C. La Torre, M. C. Caroleo and E. Cione (2021). "Polyphenols in the Mediterranean diet: From dietary sources to microRNA modulation." Antioxidants 10(2): 328.

Charalabopoulos, A., S. Davakis, M. Lambropoulou, A. Papalois, C. Simopoulos and A. Tsaroucha (2019). "Apigenin exerts anti-inflammatory effects in an experimental model of acute pancreatitis by down-regulating TNF-α." in vivo 33(4): 1133-1141.

Clayton, Z. S., D. A. Hutton, V. E. Brunt, N. S. VanDongen, B. P. Ziemba, A. G. Casso, N. T. Greenberg, A. N. Mercer, M. J. Rossman and J. Campisi (2021). "Apigenin restores endothelial function by ameliorating oxidative stress, reverses aortic stiffening, and mitigates vascular inflammation with aging." American Journal of Physiology-Heart and Circulatory Physiology 321(1): H185-H196.

Ding, Y.-M., J.-T. Lin, L.-M. Fang, Z.-Q. Lou, G.-n. Liang, X.-y. Zhang, A.-q. Li and X. Zhang (2020). "The neuroprotective effect of apigenin against OGD/R injury in rat hippocampal neurons." Pakistan Journal of Pharmaceutical Sciences 33(4).

Dou, X., Z. Zhou, R. Ren and M. Xu (2020). "Apigenin, flavonoid component isolated from Gentiana veitchiorum flower suppresses the oxidative stress through LDLR-LCAT signaling pathway." Biomedicine & Pharmacotherapy 128: 110298.

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Funakoshi-Tago, M., K. Nakamura, K. Tago, T. Mashino and T. Kasahara (2011). "Anti-inflammatory activity of structurally related flavonoids, Apigenin, Luteolin and Fisetin." International immunopharmacology 11(9): 1150-1159.

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Hashemi, P., J. F. Babaei, S. Vazifekhah and F. Nikbakht (2019). "Evaluation of the neuroprotective, anticonvulsant, and cognition-improvement effects of apigenin in temporal lobe epilepsy: Involvement of the mitochondrial apoptotic pathway." Iranian journal of basic medical sciences 22(7): 752.

Hnit, S. S. T., M. Yao, C. Xie, L. Bi, M. Wong, T. Liu, P. De Souza, Z. Li and Q. Dong (2022). "Apigenin impedes cell cycle progression at G2 phase in prostate cancer cells." Discover Oncology 13(1): 1-12.

Huang, X., Z. Yu, L. Ning, L. Yu, X. Zhang and Z. Wang (2022). "Apigenin as a promising myocyte protectant against damage and degradation." Biocell 46(2): 383.

Jeong, G.-S., S.-H. Lee, S.-N. Jeong, Y.-C. Kim and E.-C. Kim (2009). "Anti-inflammatory effects of apigenin on nicotine-and lipopolysaccharide-stimulated human periodontal ligament cells via heme oxygenase-1." International Immunopharmacology 9(12): 1374-1380.

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Karamese, M., H. S. Erol, M. Albayrak, G. Findik Guvendi, E. Aydin and S. Aksak Karamese (2016). "Anti-oxidant and anti-inflammatory effects of apigenin in a rat model of sepsis: an immunological, biochemical, and histopathological study." Immunopharmacology and Immunotoxicology 38(3): 228-237.

Kim, J., H. Kang, H. Choi, A. Jo, D.-R. Oh, Y. Kim, S. Im, S.-G. Lee, K.-I. Jeong and G.-C. Ryu (2018). "Aqueous extract of Perilla frutescens var. acuta relaxes the ciliary smooth muscle by increasing NO/cGMP content in vitro and in vivo." Molecules 23(7): 1777.

Kim, M., J. Jung, N. Y. Jeong and H.-J. Chung (2019). "The natural plant flavonoid apigenin is a strong antioxidant that effectively delays peripheral neurodegenerative processes." Anatomical Science International 94(4): 285-294.

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Lee, H. H. and H. Cho (2019). "Anti-cancer effect of apigenin on human breast carcinoma MDA-MB-231 through cell cycle arrest and apoptosis." Microbiology and Biotechnology Letters 47(1): 34-42.

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Ling, C., C. Lei, M. Zou, X. Cai, Y. Xiang, Y. Xie, X. Li, D. Huang and Y. Wang (2020). "Neuroprotective effect of apigenin against cerebral ischemia/reperfusion injury." Journal of International Medical Research 48(9): 0300060520945859.

Lu, J., Z. Meng, B. Cheng, M. Liu, S. Tao and S. Guan (2019). "Apigenin reduces the excessive accumulation of lipids induced by palmitic acid via the AMPK signaling pathway in HepG2 cells." Experimental and Therapeutic Medicine 18(4): 2965-2971.

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Mahbub, A. A., C. L. Le Maitre, N. A. Cross and N. Jordan-Mahy (2022). "The effect of apigenin and chemotherapy combination treatments on apoptosis-related genes and proteins in acute leukaemia cell lines." Scientific reports 12(1): 1-17.

Mirzoeva, S., X. Tong, B. B. Bridgeman, M. P. Plebanek and O. V. Volpert (2018). "Apigenin inhibits UVB-induced skin carcinogenesis: the role of thrombospondin-1 as an anti-inflammatory factor." Neoplasia 20(9): 930-942.

Nozhat, Z., S. Heydarzadeh, Z. Memariani and A. Ahmadi (2021). "Chemoprotective and chemosensitizing effects of apigenin on cancer therapy." Cancer Cell International 21(1): 1-26.

Park, C.-H., S.-Y. Min, H.-W. Yu, K. Kim, S. Kim, H.-J. Lee, J.-H. Kim and Y.-J. Park (2020). "Effects of apigenin on RBL-2H3, RAW264. 7, and HaCaT cells: anti-allergic, anti-inflammatory, and skin-protective activities." International Journal of Molecular Sciences 21(13): 4620.

Pham, T. H., Y. L. Page, F. Percevault, F. Ferriere, G. Flouriot and F. Pakdel (2021). "Apigenin, a partial antagonist of the estrogen receptor (ER), inhibits ER-positive breast cancer cell proliferation through Akt/FOXM1 signaling." International journal of molecular sciences 22(1): 470.

Ren, K., T. Jiang, H.-F. Zhou, Y. Liang and G.-J. Zhao (2018). "Apigenin retards atherogenesis by promoting ABCA1-mediated cholesterol efflux and suppressing inflammation." Cellular Physiology and Biochemistry 47(5): 2170-2184.

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Salehi, B., A. Venditti, M. Sharifi-Rad, D. Kręgiel, J. Sharifi-Rad, A. Durazzo, M. Lucarini, A. Santini, E. B. Souto and E. Novellino (2019). "The therapeutic potential of apigenin." International journal of molecular sciences 20(6): 1305.

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Wu, L., T. Guo, R. Deng, L. Liu and Y. Yu (2021). "Apigenin ameliorates insulin resistance and lipid accumulation by endoplasmic reticulum stress and SREBP-1c/SREBP-2 pathway in palmitate-induced HepG2 cells and high-fat diet–fed mice." Journal of Pharmacology and Experimental Therapeutics 377(1): 146-156.

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Yu, J., Q. Jiang, N. Liu, D. Fan, M. Wang and Y. Zhao (2022). "Apigenin and apigenin-7, 4′-O-dioctanoate protect against acrolein-aggravated inflammation via inhibiting the activation of NLRP3 inflammasome and HMGB1/MYD88/NF-κB signaling pathway in Human umbilical vein endothelial cells (HUVEC)." Food and Chemical Toxicology 168: 113400.

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