Apigenin, a plant-derived flavonoid, was investigated to determine whether it could influence hydrogen peroxide (H2O2)-induced oxidative damage and cellular dysfunction in the MC3T3-E1 mouse osteoblastic cell line. In the present study, osteoblastic cells were treated with H2O2 in the presence or absence of apigenin. Cell viability, apoptosis, reactive oxygen species (ROS) production and mitoch...

Apigenin is a common dietary flavonoid with considerable cytotoxic activity in vitro and in vivo. Despite many mechanistic studies, less is known about resistance factors hampering apigenin's activity. We investigated the ATP-binding cassette (ABC) transporters BCRP/ABCG2, P-glycoprotein/ABCB1 and its close relative ABCB5. Multidrug-resistant cells overexpressing these ABC transporters were not...

The increasing prevalence of inflammatory diseases and the adverse effects associated with the long-term use of current anti-inflammatory therapies prompt the identification of alternative approaches to reestablish immune balance. Apigenin, an abundant dietary flavonoid, is emerging as a potential regulator of inflammation. Here, we show that apigenin has immune-regulatory activity in vivo. Api...

The lipophilic ̄avonoids in leaf and ̄ower of Tanacetum parthenium and T. vulgaris have been compared. While those of T. parthenium are methyl ethers of the ̄avonols 6-hydroxykaempferol and quercetagetin, the surface ̄avonoids of T. vulgare are methyl ethers of the ̄avones scutellarein and 6-hydroxyluteolin. Apigenin and two ̄avone glucuronides are surprisingly present in glandular trichomes on...

Inflammatory skin disorders, such as psoriasis and atopic dermatitis, are very common in the population; however, the treatments currently available are not well tolerated and are often ineffective. Averrhoa carambola L. (Oxalidaceae) is an Asian tree that has been used in traditional folk medicine in the treatment of several skin disorders. The present study evaluates the topical anti-inflamma...

The aim of the present study was to investigate the effect and possible mechanism of apigenin on renal ischemia-reperfusion (I/R) injury in rats, as well as in in vitro experiments. In total, 36 rats were subjected to 45 min of renal ischemia, with or without treatment prior to ischemia with different concentrations of apigenin (2, 10 and 50 mg/kg) administered intravenously. All rats were sacr...

IKKα has been implicated as a key regulator of oncogenesis and driver of the metastatic process; therefore is regarded as a promising therapeutic target in anticancer drug development. In spite of the progress made in the development of IKK inhibitors, no potent IKKα inhibitor(s) have been identified. Our multistep approach of molecular modeling and direct binding has led to the identification ...

Apigenin (4',5,7-trihydroxyflavone) is an activator of cystic fibrosis transmembrane conductance regulator (CFTR)-mediated Cl(-) currents across epithelia at low concentrations and a blocker at high concentrations. We determined the roles of structural components of apigenin for both stimulation and block of Cl(-) currents across Calu-3 epithelia. The half-maximal binding affinity of apigenin f...

Apigenin, belonging to a less toxic and non-mutagenic flavone subclass of flavonoids, has been reported to possess numerous biological activities beneficial to health. Although evidence has shown apigenin might exert its protective effects by reducing the toxicity induced by amyloid-β peptides (Aβ), the precise mechanism is unclear. In the present study, we investigated the in vitro neuroprotec...

Decrease in fibroblast-produced collagen has been proven to be the pivotal cause of skin aging, but there is no satisfactory drug which directly increases dermal thickness and collage density. Here we found that a flavonoid natural product, apigenin, could significantly increase collagen synthesis. NIH/3T3 and primary human dermal fibroblasts (HDFs) were incubated with various concentrations of...