Tumor Inhibitory Agents from Vauquelinia corymbosa (Rosaceae)

Trumbull, Elmer R.; Bianchi, E.; Eckert, D. J.; Wiedhopf, Richard M.; Cole, Jack R.

doi:10.1002/jps.2600650938

Cited by 44 publications

(32 citation statements)

References 3 publications

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“…Betulinic acid (BA), a plant-derived pentacyclic lupane-type triterpenoid, can be extracted from various plants such as Sarracenia flava [24], Diospyros spp., Inga punctata [25], Ziziphus spp., and Vauquelinia corymbosa [26]. Several groups reported anti-cancer activity of BA in various cancers including lung, colorectal, breast, prostate and cervical cancer [27], but not normal cells [28].…”

Section: Discussionmentioning

confidence: 99%

Suppression of STAT3 and HIF-1 Alpha Mediates Anti-Angiogenic Activity of Betulinic Acid in Hypoxic PC-3 Prostate Cancer Cells

et al. 2011

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BackgroundSignal transducer and activator of transcription 3 (STAT3) is a transcription factor that regulates various cellular processes such as cell survival, angiogenesis and proliferation. In the present study, we examined that betulinic acid (BA), a triterpene from the bark of white birch, had the inhibitory effects on hypoxia-mediated activation of STAT3 in androgen independent human prostate cancer PC-3 cells.Methodology/Principal FindingsBA inhibited the protein expression and the transcriptional activities of hypoxia-inducible factor-1α (HIF-1α) under hypoxic condition. Consistently, BA blocked hypoxia-induced phosphorylation, DNA binding activity and nuclear accumulation of STAT3. In addition, BA significantly reduced cellular and secreted levels of vascular endothelial growth factor (VEGF), a critical angiogenic factor and a target gene of STAT3 induced under hypoxia. Furthermore, BA prevented in vitro capillary tube formation in human umbilical vein endothelial cells (HUVECs) maintained in conditioned medium of hypoxic PC-3 cells, implying anti-angiogenic activity of BA under hypoxic condition. Of note, chromatin immunoprecipitation (ChiP) assay revealed that BA inhibited binding of HIF-1α and STAT3 to VEGF promoter. Furthermore, silencing STAT3 using siRNA transfection effectively enhanced the reduced VEGF production induced by BA treatment under hypoxia.Conclusions/SignificanceTaken together, our results suggest that BA has anti-angiogenic activity by disturbing the binding of HIF-1α and STAT3 to the VEGF promoter in hypoxic PC-3 cells.

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Section: Discussionmentioning

confidence: 99%

Suppression of STAT3 and HIF-1 Alpha Mediates Anti-Angiogenic Activity of Betulinic Acid in Hypoxic PC-3 Prostate Cancer Cells

et al. 2011

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“…The activity of compounds 9 and 15 along with betulinic acid on A431 and SW1736 cells was analyzed by treating them for 4,8,24,36,48,72, and 96 h at equitoxic (IC 50 ) concentrations of each compound, respectively. The cytotoxic activity was performed exactly in accordance with the SRB microculture colorimetric assay except, that after each scheduled time point the cells were washed with PBS and further grown in drug-free media for the remaining time to complete 96 h. After working up the 96-well plates according to the published SRB assay protocol, absorbance was measured at 570 nm in a 96-well plate reader.…”

Section: Kinetic Studiesmentioning

confidence: 99%

Synthesis and Anticancer Activity of Novel Betulinic acid and Betulin Derivatives

Kommera

Kaluđerović

Kalbitz

et al. 2010

Archiv der Pharmazie

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A series of novel betulinic acid derivatives 3-11 and betulin derivatives 12-17 were synthesized. The compounds were characterized by the means of (1)H- and (13)C-NMR spectroscopy as well as mass spectrometry. The compounds have been tested on ten tumor cell lines of different histogenic origin. The most active derivatives, containing a chloroacetyl group on C-3 in betulinic acid 9 and C-28 in betulin 15, were up to ten times more cytotoxic and many fold more selective towards tumor cells in comparison to normal cells (fibroblasts) than betulinic acid. Furthermore, compound 15 was found to possess cell growth inhibition even when treated for a short time on anaplastic thyroid cancer cells (SW1736).

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“…(Ebenaceae), Inga punctata (Fabaceae) [32], Ziziphus spp. (Rhamnaceae), Vauquelinia corymbosa (Rosaceae) [33], and Syzygium spp. (Myrtaceae) [30,34,35].…”

Section: Betulinic Acidunclassified

Betulinic acid, a natural compound with potent anticancer effects

Mullauer

Kessler²,

Medema³

2010

Anti-Cancer Drugs

178

105

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New therapies using novel mechanisms to induce tumor cell death are needed with plants playing a crucial role as a source for potential anticancer compounds. One highly promising class of natural compounds are the triterpenoids with betulinic acid (BetA) as the most prominent representative. In-vitro studies have identified this agent as potently effective against a wide variety of cancer cells, also those derived from therapy-resistant and refractory tumors, whereas it has been found to be relatively nontoxic for healthy cells. In-vivo preclinically applied BetA showed some remarkable anticancer effects and a complete absence of systemic toxicity in rodents. BetA also cooperated with other therapies to induce tumor cell death and several potent derivatives have been discovered. Its antitumor activity has been related to its direct effects on mitochondria where it induces Bax/Bak-independent cytochrome-c release.

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Tumor Inhibitory Agents from Vauquelinia corymbosa (Rosaceae)

Cited by 44 publications

References 3 publications

Suppression of STAT3 and HIF-1 Alpha Mediates Anti-Angiogenic Activity of Betulinic Acid in Hypoxic PC-3 Prostate Cancer Cells

Suppression of STAT3 and HIF-1 Alpha Mediates Anti-Angiogenic Activity of Betulinic Acid in Hypoxic PC-3 Prostate Cancer Cells

Synthesis and Anticancer Activity of Novel Betulinic acid and Betulin Derivatives

Betulinic acid, a natural compound with potent anticancer effects

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