Apigenin shows synergistic anticancer activity with curcumin by binding at different sites of tubulin

Choudhury, Diptiman; Ganguli, Arnab; Dastidar, Debabrata Ghosh; Acharya, Bipul R.; Das, Amlan; Chakrabarti, Gopal

doi:10.1016/j.biochi.2013.02.010

Cited by 85 publications

(47 citation statements)

References 39 publications

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“…Co-administration of apigenin and curcumin, exhibited strong depolymerizing effects on interphase microtubules and inhibited reassembly of cold depolymerized microtubules. This outcome suggests that these agents bind to tubulin at diverse locations [106]. Apigenin exposure NSCLC lung cancer cell resulted in inhibition of proliferation and downregulation of Axl expression, with subsequent alterations in p21 and XIAP expression [107].…”

Section: 0 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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Section: 0 Effect Of Apigenin In Various Human Cancersmentioning

confidence: 99%

Plant Flavone Apigenin: an Emerging Anticancer Agent

et al. 2017

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“…Arenaria montana L., an herbaceous plant from the mountainous regions of southwestern Europe (Timité et al, 2011), contains apigenin derivatives, specifically apigenin 6-C-hexoside-8-C-hexoside, apigenin 6-C-hexoside-8-C-pentoside, apigenin 2 00 -O-pentosyl-6-C-hexoside, apigenin-6-C-glucoside, apigenin 2 00 -O-acetylpentosyl-6-C-hexoside and apigenin 2 00 -Oferuloylhexosyl-6-C-hexoside (Pereira et al, 2014). Apigenin has received increasing attention due to its bioactive properties such as anti-inflammatory (Wang & Huang, 2013), anti-mutagenic (Patel, Modi, Chiosis, & Taldone, 2011) and, particularly, antiangiogenic and anticancer properties (Choudhury et al, 2013;He et al, 2015;Johnson & Mejia, 2013). This flavone has shown the capacity to inhibit the cellular proliferation of several cancer cell lines such as hepatocellular (Kim, Jeon, & Nam, 2011), pancreatic (He et al, 2015;Johnson & Mejia, 2013), colorectal (Banerjee & Mandal, 2015), multiple myeloma (Zhao et al, 2011) and leukemia (Budhraja et al, 2012), prevent the growth of new blood vessels (metastasis) (Osada, Imaoka, & Funae, 2004), change the microenvironment of the cancer cells growth and reduce the cancer cells glucose uptake (Lefort & Blay, 2013).…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Arenaria montana L. hydroethanolic extract as a chemopreventive food ingredient: A case study focusing a dairy product (yogurt)

Oliveira

Ribeiro

Barros

et al. 2017

Journal of Functional Foods

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a b s t r a c tNatural ingredients are valuable options to be exploited in the design of innovative food formulations with health benefits. Therefore, it was evaluated the potential use of Arenaria montana L. hydroethanolic extract (rich in apigenin derivatives) as a chemopreventive agent in functional foods. Apigenin is recognized as inhibiting VEGFR-2, which is the key receptor involved in angiogenesis. The obtained extract was also able to inhibit the VEGFR-2 phosphorylation through an enzymatic assay (IC 50 = $63 mg/mL). Thereafter, free and microencapsulated forms were incorporated in yogurt. The obtained products maintained the nutritional value along the tested 3 days of storage, as also free sugars and fatty acids profiles, in comparison with the control samples. Nevertheless, the VEGFR-2 phosphorylation inhibition was not exhibited as intended. Even this behavior for the microencapsulated forms can be attributed to the protecting effect of the alginate matrix, further studies are required in order to better understand the shown performance.

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“…Curcumin induces apoptosis in breast cancer cell lines, and the activation of apoptosis was confirmed by PARP-1 cleavage and by the increased ratio between the pro-apoptotic Bax and the anti-apoptotic Bcl-2 proteins [19]. Moreover, apigenin and curcumin synergistically induced cell death and apoptosis and also blocked cell cycle progression at the G2/M phase of A549 cells [20]. Although curcumin has been found to induce apoptosis in several types of cancers, the molecular apoptotic mechanisms of curcumin in the gallbladder carcinoma cell line GBC-SD have not previously been investigated.…”

Section: Introductionmentioning

confidence: 99%

Curcumin induces apoptosis in gallbladder carcinoma cell line GBC-SD cells

Tan

Jiang

et al. 2013

Cancer Cell Int

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BackgroundGallbladder carcinoma is a malignant tumor with a very low 5-year survival rate because of the difficulty with its early diagnosis and the very poor prognosis of the advanced cancer state. The aims of this study were to determine whether curcumin could induce the apoptosis of a gallbladder carcinoma cell line, GBC-SD, and to clarify its related mechanism.MethodsFirst, the anti-proliferative activities of curcumin-treated and untreated GBC-SD cells were determined using the MTT and colony formation assays. Then, the early apoptosis of cells was detected by the annexin V/propidium iodide double-staining assay and Hoechst 33342 staining assay. Detection of mitochondrial membrane potential was used to validate the ability of curcumin on inducing apoptosis in GBC-SD cells. Cell cycle changes were detected by flow cytometric analysis. Finally, the expressions of the apoptosis-related proteins or genes caspase-3, PARP, Bcl-2, and Bax were analyzed by western blot and quantitative real time PCR assay. Statistical analyses were performed using the Student’s t-test for comparison of the results obtained from cells with or without curcumin treatment.ResultsThe MTT assay revealed that curcumin had induced a dose- and a time-dependent decrease in cell viability. Colony counting indicated that curcumin had induced a dose-dependent decrease in the colony formation ability in GBC-SD cells. Cells treated with curcumin were arrested at the S phase, according to the flow cytometric analysis. A significant induction of both the early and late phases of apoptosis was shown by the annexin V-FITC and PI staining. Morphological changes in apoptotic cells were also found by the Hoechst 33342 staining. After treatment with curcumin fluorescence shifted from red to green as ΔΨm decreased. Furthermore, western blot and quantitative real time PCR assays demonstrated that the curcumin induced apoptosis in GBC-SD cells by regulating the ratio of Bcl-2/Bax and activating the expression of cleaved caspase-3.ConclusionsTaken together, the results indicate that curcumin may be a potential agent for the treatment of gallbladder cancer.

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Apigenin shows synergistic anticancer activity with curcumin by binding at different sites of tubulin

Cited by 85 publications

References 39 publications

Plant Flavone Apigenin: an Emerging Anticancer Agent

Plant Flavone Apigenin: an Emerging Anticancer Agent

Evaluation of Arenaria montana L. hydroethanolic extract as a chemopreventive food ingredient: A case study focusing a dairy product (yogurt)

Curcumin induces apoptosis in gallbladder carcinoma cell line GBC-SD cells

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