Tumor Inhibitors I: Preliminary Investigation of Antitumor Activity of Sarracenia flava

Miles, D. Howard; Kokpol, Udom; Zalkow, Leon H.; Steindel, Steven J.; Nabors, James B.

doi:10.1002/jps.2600630427

Cited by 42 publications

(27 citation statements)

References 3 publications

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“…In addition, Zuco et al have shown that betulinic acid has no antiproliferative effect on normal derma fibroblasts and lymphocytes [24]. Even in in vivo studies no signs of acute or chronic toxicity have been reported so far [13,16,20]. This selectivity for tumor cells could mean less toxicity for nonmalignant cells and, furthermore, less side effects of chemotherapy.…”

Section: Discussionmentioning

confidence: 99%

Betulinic Acid a Radiosensitizer in Head and Neck Squamous Cell Carcinoma Cell Lines

et al. 2010

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Section: Discussionmentioning

confidence: 99%

Betulinic Acid a Radiosensitizer in Head and Neck Squamous Cell Carcinoma Cell Lines

et al. 2010

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“…However, since a small percentage of primary glioblastoma tumors (4 of 24) did not respond to Bet A, some glioblastoma tumors might be resistant to Bet-A treatment. Bet A appears to be an especially attractive new compound, owing to its cytotoxic activity together with its lack of toxicity (Miles et al, 1974), which leads to a favorable therapeutic index. So far no signs of acute or chronic toxicity were reported in in vivo studies (Miles et al, 1974;Sheth et al, 1972;Sandberg et al, 1987).…”

Section: Discussionmentioning

confidence: 99%

“…Bet A appears to be an especially attractive new compound, owing to its cytotoxic activity together with its lack of toxicity (Miles et al, 1974), which leads to a favorable therapeutic index. So far no signs of acute or chronic toxicity were reported in in vivo studies (Miles et al, 1974;Sheth et al, 1972;Sandberg et al, 1987). In particular, we observed no cytotoxic activity of Bet A on murine non-malignant neuronal cells, indicating that Bet A may be a selective cytotoxic compound for malignant brain-tumor cells.…”

Section: Discussionmentioning

confidence: 99%

Betulinic acid: A new cytotoxic agent against malignant brain-tumor cells

et al. 1999

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Malignant brain tumors are the most common solid tumors in children. The overall prognosis for this group of patients is still poor, emphasizing the importance of more effective therapies. Betulinic acid (Bet A) has been described as a novel cytotoxic compound active against melanoma and neuroblastoma cells. Here we report that Bet A was active against medulloblastoma and glioblastoma cell lines. In addition, Bet A exerted cytotoxic activity against primary tumor cells cultured from patients in 4 of 4 medulloblastoma-tumor samples tested and in 20 of 24 glioblastoma-tumor samples. Since a small percentage of primary-glioblastoma-tumor cells (4/24) did not respond to Bet-A treatment, resistance to Bet A might occur. Induction of apoptosis by Bet A involved mitochondrial perturbations, since inhibition of the mitochondrial permeability transition by the mitochondrion-specific inhibitor bongkrekic acid (BA) reduced Bet-A-induced apoptosis. In addition, mitochondria undergoing Bet-A-induced permeability transition triggered DNA fragmentation in isolated nuclei. Cytochrome c was released from mitochondria of Bet-A-treated cells, and might be involved in activation of caspases. Following treatment with Bet A, caspase-8, caspase-3 and PARP were proteolytically processed. Inhibition of caspase cleavage by the broad-range caspase inhibitor zVAD.fmk strongly reduced Bet-A-induced apoptosis, indicating that apoptosis was mediated by activation of caspases. Since Bet A did not exhibit cytotoxicity against murine neuronal cells in vitro, these findings suggest that Bet A may be a promising new agent for the treatment of medulloblastoma and glioblastoma cells that clearly warrants further pre-clinical and clinical evaluation.

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“…Syntheses under pressure were performed in a lab-scale single-mode microwave from CEM Corp, USA. The 1 H-and 13 C-NMR spectra were recorded on a Varian Unity 500 NMR spectrometer (Varian, USA) in CDCl 3 . MS spectra were recorded on LCQ -Thermo (Germany).…”

Section: Experimental Generalmentioning

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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Tumor Inhibitors I: Preliminary Investigation of Antitumor Activity of Sarracenia flava

Cited by 42 publications

References 3 publications

Betulinic Acid a Radiosensitizer in Head and Neck Squamous Cell Carcinoma Cell Lines

Betulinic Acid a Radiosensitizer in Head and Neck Squamous Cell Carcinoma Cell Lines

Betulinic acid: A new cytotoxic agent against malignant brain-tumor cells

Synthesis and Anticancer Activity of Novel Betulinic acid and Betulin Derivatives

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