Anti-angiogenic and anti-tumor activity of Bavachinin by targeting hypoxia-inducible factor-1α

Nepal, Manoj; Choi, Hee Joung; Choi, Bo-Yun; Kim, Se Lim; Ryu, Jae‐Ha; Kim, Do Hee; Lee, Younghoon; Soh, Yunjo

doi:10.1016/j.ejphar.2012.06.028

Cited by 59 publications

(37 citation statements)

References 49 publications

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“…Bavachinin (Figure 1), isolated from P. corylifolia (Chen et al, 2012), is a prenylated flavonoid. Bavachinin exhibits antiallergic, anti-inflammatory (Chen et al, 2013(Chen et al, , 2014, antiangiogenic, antitumor (Nepal et al, 2012) and antioxidant activities (Xiao et al, 2010), and inhibits severe acute respiratory syndrome coronavirus papain-like protease (Kim et al, 2014). In our study (WO2014/169800), natural bavachinin exhibited peroxisome proliferator-activated receptor g (PPAR-g) agonist activity.…”

Section: Introductionmentioning

confidence: 78%

Structural elucidation ofin vitrometabolites of bavachinin in rat liver microsomes by LC-ESI-MSⁿand chemical synthesis

Fan

et al. 2015

Xenobiotica

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1. Bavachinin isolated from Psoralea corylifolia has various activities, such as antimicrobial, antiallergic, antitumor and so on. Our previous study showed that natural bavachinin exhibits peroxisome proliferator-activated receptor γ-agonist activity. 2. In vitro studies on bavachinin metabolism were conducted using rat liver microsomes incubated at 37 °C for 60 min. 3. Structures of eight metabolites of the incubation mixtures were cautiously characterized using electrospray tandem mass spectra and three synthetic compounds. The results indicated that eight metabolites of bavachinin were biotransformed mainly through oxidation. 4. The metabolic pathways of bavachinin were elucidated in vitro. These results contribute to the understanding of bavachinin's in vivo metabolism.

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Section: Introductionmentioning

confidence: 78%

Structural elucidation ofin vitrometabolites of bavachinin in rat liver microsomes by LC-ESI-MSⁿand chemical synthesis

Fan

et al. 2015

Xenobiotica

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“…Another natural compound with a potent antiangiogenic activity is the flavonoid bavachinin. Bavachinin inhibited increased HIF-1 α activity in human KB carcinoma derived from HeLa cells [121]. In human HOS osteosarcoma cells under hypoxia, bavachinin decreased transcription of genes associated with angiogenesis and energy metabolism that are regulated by HIF-1, such as vascular endothelial growth factors (VEGFs), GLUT1, and HKII [121].…”

Section: Potentially Targetable Metabolic Actors By Natural Compoundsmentioning

confidence: 99%

“…Bavachinin may be used as a therapeutic agent to inhibit tumour angiogenesis. Indeed, in vivo studies showed that injecting bavachinin significantly reduced tumour volume in nude mice with KB xenografts [121]. …”

Section: Potentially Targetable Metabolic Actors By Natural Compoundsmentioning

confidence: 99%

Natural Compounds as Regulators of the Cancer Cell Metabolism

Cerella

Radogna

Dicato

et al. 2013

International Journal of Cell Biology

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Even though altered metabolism is an “old” physiological mechanism, only recently its targeting became a therapeutically interesting strategy and by now it is considered an emerging hallmark of cancer. Nevertheless, a very poor number of compounds are under investigation as potential modulators of cell metabolism. Candidate agents should display selectivity of action towards cancer cells without side effects. This ideal favorable profile would perfectly overlap the requisites of new anticancer therapies and chemopreventive strategies as well. Nature represents a still largely unexplored source of bioactive molecules with a therapeutic potential. Many of these compounds have already been characterized for their multiple anticancer activities. Many of them are absorbed with the diet and therefore possess a known profile in terms of tolerability and bioavailability compared to newly synthetized chemical compounds. The discovery of important cross-talks between mediators of the most therapeutically targeted aberrancies in cancer (i.e., cell proliferation, survival, and migration) and the metabolic machinery allows to predict the possibility that many anticancer activities ascribed to a number of natural compounds may be due, in part, to their ability of modulating metabolic pathways. In this review, we attempt an overview of what is currently known about the potential of natural compounds as modulators of cancer cell metabolism.

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“…20 study demonstrates, for the first time, the therapeutic effect of this compound in Th2-mediated asthmatic inflammation. Given the potency and enriched source of this compound, further studies to explore the pharmacological application of this compound to Th2-mediated inflammation might provide a lead candidate for a novel therapeutic agent against asthma.…”

Section: Discussionmentioning

confidence: 99%

Treatment of allergic inflammation and hyperresponsiveness by a simple compound, Bavachinin, isolated from Chinese herbs

et al. 2013

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Asthmatic inflammation is mediated by a type 2 helper T cell (Th2) cytokine response, and blocking Th2 cytokine production is proven to have a potent therapeutic effect against asthmatic inflammation. Using IL-4-green fluorescent protein (GFP) reporter mice, we demonstrated that Bavachinin, a single compound isolated from a Chinese herb, significantly inhibited Th2 cytokine production, including IL-4, IL-5 and IL-13. Notably, this compound almost completely blocked inflammation in the ovalbumin (OVA)-sensitized animal asthma model. Furthermore, we demonstrated that this chemical selectively affects the level of GATA-3, most likely by affecting the stability of GATA-3 mRNA. Our results demonstrate, for the first time, the potential therapeutic value of this single compound derived from Chinese herbs.

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Anti-angiogenic and anti-tumor activity of Bavachinin by targeting hypoxia-inducible factor-1α

Cited by 59 publications

References 49 publications

Structural elucidation ofin vitrometabolites of bavachinin in rat liver microsomes by LC-ESI-MSⁿand chemical synthesis

Structural elucidation ofin vitrometabolites of bavachinin in rat liver microsomes by LC-ESI-MSⁿand chemical synthesis

Natural Compounds as Regulators of the Cancer Cell Metabolism

Treatment of allergic inflammation and hyperresponsiveness by a simple compound, Bavachinin, isolated from Chinese herbs

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Anti-angiogenic and anti-tumor activity of Bavachinin by targeting hypoxia-inducible factor-1α

Cited by 59 publications

References 49 publications

Structural elucidation ofin vitrometabolites of bavachinin in rat liver microsomes by LC-ESI-MSnand chemical synthesis

Structural elucidation ofin vitrometabolites of bavachinin in rat liver microsomes by LC-ESI-MSnand chemical synthesis

Natural Compounds as Regulators of the Cancer Cell Metabolism

Treatment of allergic inflammation and hyperresponsiveness by a simple compound, Bavachinin, isolated from Chinese herbs

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Product

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Structural elucidation ofin vitrometabolites of bavachinin in rat liver microsomes by LC-ESI-MSⁿand chemical synthesis

Structural elucidation ofin vitrometabolites of bavachinin in rat liver microsomes by LC-ESI-MSⁿand chemical synthesis