In Vitro and In Vivo Anti-tumoral Effects of the Flavonoid Apigenin in Malignant Mesothelioma

Masuelli, Laura; Benvenuto, Monica; Mattera, Rosanna; Stefano, Enrica Di; Zago, Erika; Taffera, Gloria; Tresoldi, Ilaria; Giganti, Maria Gabriella; Frajese, Giovanni Vanni; Berardi, Ginevra; Modesti, Andrea; Bei, Roberto

doi:10.3389/fphar.2017.00373

Cited by 65 publications

(46 citation statements)

References 79 publications

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“…Apigenin also blocks the degradation of IκBα in lung cancers, which further blocks the separation of IκBα from the NF-κB heterodimer [ 26 ]. And in malignant mesothelioma, apigenin treatment showed anti-cancer effects in vitro and in vivo by inhibiting NF-κB nuclear translocation and AKT activation and modulating MAPK signaling pathways [ 91 ].…”

Section: Signaling Transduction Modulation By Apigenin In Cancer Thermentioning

confidence: 99%

Apigenin in cancer therapy: anti-cancer effects and mechanisms of action

et al. 2017

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Apigenin is a common dietary flavonoid that is abundantly present in many fruits, vegetables and Chinese medicinal herbs and serves multiple physiological functions, such as strong anti-inflammatory, antioxidant, antibacterial and antiviral activities and blood pressure reduction. Therefore, apigenin has been used as a traditional medicine for centuries. Recently, apigenin has been widely investigated for its anti-cancer activities and low toxicity. Apigenin was reported to suppress various human cancers in vitro and in vivo by multiple biological effects, such as triggering cell apoptosis and autophagy, inducing cell cycle arrest, suppressing cell migration and invasion, and stimulating an immune response. In this review, we focus on the most recent advances in the anti-cancer effects of apigenin and their underlying mechanisms, and we summarize the signaling pathways modulated by apigenin, including the PI3K/AKT, MAPK/ERK, JAK/STAT, NF-κB and Wnt/β-catenin pathways. We also discuss combinatorial strategies to enhance the anti-cancer effect of apigenin on various cancers and its use as an adjuvant chemotherapeutic agent to overcome cancer drug resistance or to alleviate other adverse effects of chemotherapy. The functions of apigenin against cancer stem cells are also summarized and discussed. These data demonstrate that apigenin is a promising reagent for cancer therapy. Apigenin appears to have the potential to be developed either as a dietary supplement or as an adjuvant chemotherapeutic agent for cancer therapy.

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Section: Signaling Transduction Modulation By Apigenin In Cancer Thermentioning

confidence: 99%

Apigenin in cancer therapy: anti-cancer effects and mechanisms of action

et al. 2017

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“…The Consulting the literature showed that the phenolic acid components chlorogenic acid (Xue et al, 2017;Shao, Zhang, Chen, & Sun, 2015) and caffeic acid (Brautigan, Gielata, Heo, Kubicka, & Wilkins, 2018), and the flavonoids scutellarin (Nie et al, 2018;Sun et al, 2018;Tang & Gao, 2019), isoorientin (Huang, Jin et al, 2018;Lin et al, 2016), isovitexin (Lv, 2018), scutellarein (Jiang et al, 2018;Lu, Li, Li, & Asia, 2017;Zheng et al, 2017), luteolin (Niu, Guo, Gan, Bao, & Ren, 2015) and apigenin (Bhattacharya et al, 2018;Masuelli et al, 2017;Cai et al, 2011) had different degrees of inhibition on tumor cells. Among them, caffeic acid, isoorientin, isovitexin, luteolin and apigenin had better antiliver tumor activities.…”

Section: Analysis Of Migration Components In Plasmamentioning

confidence: 99%

Analysis of plasma migration components in Patrinia villosa (Thunb.) Juss. effective parts by UPLC–Q‐TOF–MS

Han

Wang

Yang

et al. 2019

Biomedical Chromatography

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Patrinia villosa (Thunb.) Juss. (PVJ) is described as pungent, bitter and slightly cold in Chinese medicine, and is associated with the large intestine, stomach and liver meridians. The preliminary experiments of our research team proved that PVJ total flavonoids have excellent inhibitory effects on liver cancer cells. The present experiment uses the UPLC–Q‐TOF–MS technology and serum pharmacochemistry methods to analyze the chemical components in vitro and in vivo of PVJ antiliver tumors. A total of 14 chemical components were identified in the total flavonoids extract of PVJ, and it is mainly composed of flavonoids, flavonones, flavonols and phenolic acids. At the same time, seven prototypical components and seven metabolic components were detected in the drug‐containing plasma. Hydrocaffeate and scutellarein are the phase I metabolites of caffeic acid and scutellarin, respectively. Sulfated apigenin, sulfated luteolin, sulfated kaempferol and methylated kaempferol are the II phase metabolites of apigenin, luteolin, kaempferol, respectively. The experiment provides a reference for the research and development of antitumor drug candidates, and provides a basis for revealing the bioactive components of PVJ and the antitumor mechanism.

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“…Masuelli et al [211] demonstrated that apigenin in MM cells caused apoptosis and not autophagy by altering Bax/Bcl2 ratio. Apigenin also caused the activation of p53 and caspase-9.…”

Section: Effect Of Apigenin In Various Human Cancersmentioning

confidence: 99%

Plant Flavone Apigenin: an Emerging Anticancer Agent

et al. 2017

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Research in cancer chemoprevention provides convincing evidence that increased intake of vegetables and fruits may reduce the risk of several human malignancies. Phytochemicals present therein provide beneficial anti-inflammatory and antioxidant properties that serve to improve the cellular microenvironment. Compounds known as flavonoids categorized anthocyanidins, flavonols, flavanones, flavonols, flavones, and isoflavones have shown considerable promise as chemopreventive agents. Apigenin (4′, 5, 7-trihydroxyflavone), a major plant flavone, possessing antioxidant, anti-inflammatory, and anticancer properties affecting several molecular and cellular targets used to treat various human diseases. Epidemiologic and case-control studies have suggested apigenin reduces the risk of certain cancers. Studies demonstrate that apigenin retain potent therapeutic properties alone and/or increases the efficacy of several chemotherapeutic drugs in combination on a variety of human cancers. Apigenin’s anticancer effects could also be due to its differential effects in causing minimal toxicity to normal cells with delayed plasma clearance and slow decomposition in liver increasing the systemic bioavailability in pharmacokinetic studies. Here we discuss the anticancer role of apigenin highlighting its potential activity as a chemopreventive and therapeutic agent. We also highlight the current caveats that preclude apigenin for its use in the human trials.

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In Vitro and In Vivo Anti-tumoral Effects of the Flavonoid Apigenin in Malignant Mesothelioma

Cited by 65 publications

References 79 publications

Apigenin in cancer therapy: anti-cancer effects and mechanisms of action

Apigenin in cancer therapy: anti-cancer effects and mechanisms of action

Analysis of plasma migration components in Patrinia villosa (Thunb.) Juss. effective parts by UPLC–Q‐TOF–MS

Plant Flavone Apigenin: an Emerging Anticancer Agent

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