scholarly journals Inhibitory Activity of the Hypoxia-inducible Factor-1 Pathway by Tartrolone C

2006 ◽  
Vol 59 (11) ◽  
pp. 693-697 ◽  
Author(s):  
Yohko Yamazaki ◽  
Tetsuya Someno ◽  
Kazuhisa Minamiguchi ◽  
Manabu Kawada ◽  
Isao Momose ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Hypoxia Inducible Factor ◽  
Hypoxia Inducible Factor 1

scholarly journals Synthesis and evaluation of novel 12-aryl berberine analogues with hypoxia-inducible factor-1 inhibitory activity

RSC Advances ◽  
2017 ◽  
Vol 7 (43) ◽  
pp. 26921-26929 ◽  
Author(s):  
Xiaobo Zhou ◽  
Ming Chen ◽  
Zhiyuan Zheng ◽  
Guo-Yuan Zhu ◽  
Zhi-Hong Jiang ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Transcriptional Activity ◽  
Hypoxia Inducible Factor ◽  
Inhibitory Effect ◽  
Hypoxia Inducible Factor 1 ◽  
Potent Inhibitory Effect

Seven novel 12-phenyl berberines (3a–3f, 3k) showed more potent inhibitory effect on hypoxia-induced HIF-1 transcriptional activity than the parent berberine.

Phenanthroindolizidine alkaloids from Tylophora atrofolliculata with hypoxia-inducible factor-1 (HIF-1) inhibitory activity

RSC Advances ◽  
2016 ◽  
Vol 6 (83) ◽  
pp. 79958-79967 ◽  
Author(s):  
Cheng-Yu Chen ◽  
Guo-Yuan Zhu ◽  
Jing-Rong Wang ◽  
Zhi-Hong Jiang
Keyword(s):  
Inhibitory Activity ◽  
Hypoxia Inducible Factor ◽  
Inhibitory Effects ◽  
Hypoxia Inducible Factor 1 ◽  
Phenanthroindolizidine Alkaloids

Phenanthroindolizidine alkaloids from T. atrofolliculata with potent HIF-1 inhibitory effects.

scholarly journals Inhibition of HIF-1α through Suppression of NF-κB Activation by Compounds Isolated from Senecio graveolens

2020 ◽  
Vol 7 (01) ◽  
pp. e1-e11
Author(s):  
Luis Apaza Ticona ◽  
Nuria Cano-Adamuz ◽  
Andreea Madalina Serban ◽  
Ángel Rumbero Sánchez
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
Hypoxia Inducible Factor ◽  
Cancer Cell Lines ◽  
Nuclear Factor ◽  
Kappa Light Chain ◽  
Hep G2 ◽  
Hypoxia Inducible Factor 1 ◽  
Light Chain Enhancer

AbstractOne of the characteristics of cancer is that the lack of oxygen in the cancer cells triggers changes in their gene expression. This hypoxia activates hypoxia-inducible factor 1-alpha and this in turn sets in motion the whole family of important angiogenic genes for the tumour. Hypoxia-inducible factor 1-alpha therefore increases the density and vascular permeability within the tumours, facilitating their rapid growth and, later, the metastasis. Senecio graveolens is a South American medicinal plant commonly used for mountain sickness (lack of adaptation of the organism to hypoxia). Additionally, pharmacological studies showed that its alcoholic extracts have cytotoxic properties.This research aimed to perform a guided phytochemical study of S. graveolens to identify compounds capable of inhibiting hypoxia-inducible factor 1-alpha through suppression of nuclear factor kappa-light-chain-enhancer of activated B cell activation. The isolation led to the characterisation of phanurane (1), damsine (2), and scoparone (3), first reported in the S. graveolens species.Phanurane (1 ) showed inhibitory activity of hypoxia-inducible factor 1-alpha on the cancer cell lines U-373 MG (IC50=20.66±0.04 μM), A549 (IC50=25.80±0.04 μM), Hep G2 (IC50=29.21±0.03 μM), and Caco-2 (IC50=38.58±0.02 μM). Damsine (2) hypoxia-inducible factor 1-alpha displayed inhibitory activity of hypoxia-inducible factor 1-alpha on the cancer cell lines U-373 MG (IC50=2.29±0.07 μM), A549 (IC50=4.13±0.04 μM), Hep G2 (IC50=6.40±0.03 μM), and Caco-2 (IC50=9.80±0.04 μM). Finally, scoparone (3) displayed inhibitory activity of hypoxia-inducible factor 1-alpha on the cancer cell lines U-373 MG (IC50=15.22±0.01 μM), A549 (IC50=17.47±0.02 μM), Hep G2 (IC50=18.26±0.06 μM), and Caco-2 (IC50=19.75±0.04 μM).In addition, phanurane (1 ) displayed inhibitory activity over nuclear factor kappa-light-chain-enhancer of activated B cells on cancer cell lines U-373 MG (IC50=7.13±0.03 μM), A549 (IC50=8.64±0.03 μM), Hep G2 (IC50=8.87±0.04 μM), and Caco-2 (IC50=15.11±0.01 μM). Likewise, damsine (2) showed inhibitory activity over nuclear factor kappa-light-chain-enhancer of activated B cells on cancer cell lines U-373 MG (IC50=2.28±0.01 μM), A549 (IC50=3.79±0.02 μM), Hep G2 (IC50=3.98±0.05 μM), and Caco-2 (IC50=6.41±0.02 μM). Lastly, scoparone (3) displayed inhibitory activity of nuclear factor kappa-light-chain-enhancer of activated B cells on cancer cell lines U-373 MG (IC50=3.62±0.06 μM), A549 (IC50=4.48±0.03 μM), Hep G2 (IC50=5.25±0.01 μM), and Caco-2 (IC50=11.90±0.02 μM).This study corroborates the cytotoxic activity of the isolated compounds through the inhibition of hypoxia-inducible factor 1-alpha as well as its modulator nuclear factor kappa-light-chain-enhancer of activated B cells.

Vascular adaptations to hypoxia: molecular and cellular mechanisms regulating vascular tone

2007 ◽  
Vol 43 ◽  
pp. 105-120 ◽  
Author(s):  
Michael L. Paffett ◽  
Benjimen R. Walker
Keyword(s):  
Vascular Tone ◽  
Cellular Proliferation ◽  
Hypoxic Pulmonary Vasoconstriction ◽  
Hypoxia Inducible Factor ◽  
Systemic Circulation ◽  
Cellular Mechanisms ◽  
Hypoxia Inducible Factor 1 ◽  
Pulmonary Vasoconstriction ◽  
Adaptive Mechanisms ◽  
Adaptive Processes

Several molecular and cellular adaptive mechanisms to hypoxia exist within the vasculature. Many of these processes involve oxygen sensing which is transduced into mediators of vasoconstriction in the pulmonary circulation and vasodilation in the systemic circulation. A variety of oxygen-responsive pathways, such as HIF (hypoxia-inducible factor)-1 and HOs (haem oxygenases), contribute to the overall adaptive process during hypoxia and are currently an area of intense research. Generation of ROS (reactive oxygen species) may also differentially regulate vascular tone in these circulations. Potential candidates underlying the divergent responses between the systemic and pulmonary circulations may include Nox (NADPH oxidase)-derived ROS and mitochondrial-derived ROS. In addition to alterations in ROS production governing vascular tone in the hypoxic setting, other vascular adaptations are likely to be involved. HPV (hypoxic pulmonary vasoconstriction) and CH (chronic hypoxia)-induced alterations in cellular proliferation, ionic conductances and changes in the contractile apparatus sensitivity to calcium, all occur as adaptive processes within the vasculature.

TAp73 opposes tumor angiogenesis by promoting hypoxia-inducible factor 1α degradation

2020 ◽  
Author(s):  
Lungwani Muungo
Keyword(s):  
Cancer Progression ◽  
Hypoxia Inducible Factor ◽  
Tumor Hypoxia ◽  
Human Lung Cancer ◽  
Regulatory Subunit ◽  
Patients With Cancer ◽  
Hypoxia Inducible Factor 1 ◽  
Chemically Induced ◽  
Induced Tumors ◽  
Patient Prognosis

Tumor hypoxia and hypoxia-inducible factor 1 (HIF-1) activationare associated with cancer progression. Here, we demonstrate thatthe transcription factor TAp73 opposes HIF-1 activity through anontranscriptional mechanism, thus affecting tumor angiogenesis.TAp73-deficient mice have an increased incidence of spontaneousand chemically induced tumors that also display enhanced vascularization.Mechanistically, TAp73 interacts with the regulatory subunit(α) of HIF-1 and recruits mouse double minute 2 homolog intothe protein complex, thus promoting HIF-1α polyubiquitination andconsequent proteasomal degradation in an oxygen-independentmanner. In human lung cancer datasets, TAp73 strongly predictsgood patient prognosis, and its expression is associated with lowHIF-1 activation and angiogenesis. Our findings, supported by invivo and clinical evidence, demonstrate a mechanism for oxygenindependentHIF-1 regulation, which has important implicationsfor individualizing therapies in patients with cancer.

Sign in / Sign up

Export Citation Format

Share Document