Apigenin and Acacetin: Recent Advances in Therapeutic Applications and Delivery Strategies (2020-2024)

Introduction

Flavonoids, a class of plant-derived secondary metabolites, have garnered significant attention in recent years due to their diverse pharmacological activities. Among these, apigenin and acacetin have emerged as promising therapeutic agents with potential applications in various diseases, including cancer, cardiovascular disorders, and neurodegenerative diseases. This mini-review summarizes the recent advancements in understanding the therapeutic potential of apigenin and acacetin, focusing on their mechanisms of action and novel delivery strategies developed over the past five years.

Therapeutic Mechanisms of Apigenin and Acacetin

A significant body of research has focused on elucidating the mechanisms underlying the therapeutic effects of apigenin and acacetin. Several studies highlight their antioxidant and anti-inflammatory properties as key contributors to their beneficial effects. Mingchun Liu's research group demonstrated the anti-inflammatory and antioxidant activities of apigenin, luteolin, kaempferol, and quercetin in 2020 (Chunlian Tian et al., 2020, South African Journal of Botany).

Cancer Therapy

Apigenin's role as an anticancer agent has been extensively investigated. Bahare Salehi's group provided a comprehensive review of apigenin's anticancer properties in 2020 (Muhammad Imran et al., 2020, Phytotherapy Research). Research has explored its efficacy against various cancers, including colorectal cancer, lung cancer, and cervical cancer. Gwonhwa Song's's laboratory demonstrated that apigenin enhances apoptosis induced by 5-fluorouracil in colorectal cancer cells by regulating thymidylate synthase (Changwon Yang et al., 2020, Redox Biology). Xiaojun Yao's's team found that apigenin and luteolin suppress PD-L1 expression, improving anti-tumor immunity in KRAS-mutant lung cancer (Zebo Jiang et al., 2020, Cancer Letters). Li Jiang's's research group showed that apigenin 7-O-glucoside promotes apoptosis in cervical cancer cells through the PTEN/PI3K/AKT pathway (Miaomiao Liu et al., 2020, Food and Chemical Toxicology). More recently, Lipeng Xu's's group showed that apigenin promotes apoptosis of 4T1 cells through the PI3K/AKT/Nrf2 pathway and improves the tumor immune microenvironment in vivo (Chu Zhang et al., 2024, Toxicology Research). Rajesh N. Gacche's research group found that apigenin in combination with Vorinostat induces apoptotic-mediated cell death in TNBC by modulating the epigenetic and apoptotic regulators and related miRNAs (Snehal Nimal et al., 2024, Sci. rep. (Nat. Publ. Group)). Hifzur R. Siddique's group showed that apigenin enhances sorafenib anti-tumour efficacy in hepatocellular carcinoma (Deepti Singh et al., 2024, Translational Oncology).

Cardiovascular Protection

Apigenin has also demonstrated cardioprotective effects. Douglas R. Seals's's laboratory reported that apigenin restores endothelial function, reverses aortic stiffening, and mitigates vascular inflammation with aging (Zachary S. Clayton et al., 2020, AJP Heart and Circulatory Physiology). Yu-Ming Kang's's team showed that apigenin improves hypertension and cardiac hypertrophy by modulating NADPH oxidase-dependent ROS generation and cytokines in the hypothalamic paraventricular nucleus (Hong-Li Gao et al., 2021, Cardiovascular Toxicology). Mei-Lin Xie's's group found that apigenin suppresses TGF-β1-induced cardiac fibroblast differentiation and collagen synthesis (Feng Wang et al., 2021, Phytomedicine). Tao Shen's's laboratory demonstrated that apigenin alleviates oxidative stress-induced myocardial injury by regulating the SIRT1 signaling pathway (Kun Xu et al., 2022, European Journal of Pharmacology). Wei-Yin Wu's's team showed that acacetin alleviates myocardial ischaemia/reperfusion injury by inhibiting oxidative stress and apoptosis via the Nrf-2/HO-1 pathway (Chan Wu et al., 2022, Pharmaceutical Biology).

Neuroprotection

The neuroprotective potential of apigenin has also been explored. Sílvia Lima Costa's's group investigated the neuroimmunomodulatory and neuroprotective effects of apigenin in in vitro models of neuroinflammation associated with Alzheimer's disease (Naiara Silva Dourado et al., 2020, Front. aging neurosci.). Ali Sharafi's's laboratory demonstrated the neuroprotective effect of apigenin on depressive-like behavior (Soroush Bijani et al., 2021, Neurochemical Research). Yasir Hasan Siddique's's group showed the beneficial effects of apigenin on the transgenic Drosophila model of Alzheimer's disease (Yasir Hasan Siddique et al., 2022, Chemico-Biological Interactions). Ajay Guru's's laboratory demonstrated the prophylactic effects of apigenin against hyperglycemia-associated amnesia via activation of the Nrf2/ARE pathway in zebrafish (B. Haridevamuthu et al., 2024, European Journal of Pharmacology).

Metabolic Disorders

Apigenin has shown promise in ameliorating metabolic disorders. Tzong-Shyuan Lee's's group reported that apigenin ameliorates hepatic lipid accumulation by activating the autophagy-mitochondria pathway (Man Chen Hsu et al., 2021, Journal of Food and Drug Analysis). Yongxiong Yu's's laboratory demonstrated that apigenin ameliorates insulin resistance and lipid accumulation by endoplasmic reticulum stress and SREBP-1c/SREBP-2 pathway (Li-Ling Wu et al., 2021, Journal of Pharmacology and Experimental Therapeutics). Zheng-Rong Lu's's team found that apigenin attenuates atherosclerosis and non-alcoholic fatty liver disease through inhibition of the NLRP3 inflammasome in mice (Zheng-Rong Lu et al., 2023, Sci. rep. (Nat. Publ. Group)). DuoDuo Zhang's's group showed that apigenin alleviated high-fat-diet-induced hepatic pyroptosis by Mitophagy-ROS-CTSB-NLRP3 Pathway in Mice and AML12 Cells (Zhuoqun Meng et al., 2023, Journal of Agricultural and Food Chemistry). Tzong-Shyuan Lee's's group showed that apigenin targets fetuin-A to ameliorate obesity-induced insulin resistance (Man-Chen Hsu et al., 2024, International Journal of Biological Sciences). Wei-Yin Wu's's team showed that acacetin attenuates diabetes-induced cardiomyopathy by inhibiting oxidative stress and energy metabolism via PPAR-α/AMPK pathway (Fei Song et al., 2022, European Journal of Pharmacology).

Novel Delivery Strategies for Apigenin

Recognizing the limitations of apigenin's bioavailability, researchers have explored novel delivery strategies to enhance its therapeutic efficacy. Qixin Zhong's's laboratory investigated the nanoencapsulation of apigenin with whey protein isolate to improve its in vitro activity against colorectal cancer cells and bioavailability (Shan Hong et al., 2021, LWT). Nemany A.N. Hanafy's's research group studied the effect of encapsulated apigenin nanoparticles on HePG-2 cells through regulation of P53 (Mayada Mohamed Mabrouk Zayed et al., 2022, Pharmaceutics (Basel)). Yaser Azizi's's team developed apigenin-coated gold nanoparticles as a cardioprotective strategy against doxorubicin-induced cardiotoxicity (Zeynab Sharifiaghdam et al., 2022, Heliyon). Elena Sánchez-López's's laboratory developed dually active apigenin-loaded nanostructured lipid carriers for cancer treatment (Lorena Bonilla-Vidal et al., 2023, International Journal of Nanomedicine). Lee Fong Siow's's group studied the encapsulation of hydrophobic apigenin into small unilamellar liposomes coated with chitosan (San-San Ang et al., 2023, Food and Bioprocess Technology). Elena Sánchez-López's's laboratory developed novel nanostructured lipid carriers loading Apigenin for anterior segment ocular pathologies (Lorena Bonilla-Vidal et al., 2024, International Journal of Pharmaceutics). Boontida Morakul's's research group studied the dissolution and antioxidant potential of apigenin self nanoemulsifying drug delivery system (SNEDDS) for oral delivery (Boontida Morakul et al., 2024, Sci. rep. (Nat. Publ. Group)).

Conclusion

The past five years have witnessed significant advancements in our understanding of the therapeutic potential of apigenin and acacetin. Research has elucidated their mechanisms of action in various diseases, including cancer, cardiovascular disorders, and neurodegenerative diseases. Furthermore, novel delivery strategies have been developed to improve the bioavailability and efficacy of these flavonoids. These advancements highlight the promising role of apigenin and acacetin as therapeutic agents and warrant further investigation to translate these findings into clinical applications.

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