Synthesis and SAR studies of marine natural products ma’edamines A, B and their analogues

Saha, Sanjay; Reddy, Ch. Venkata Ramana; Xu, Shili; Sankar, Saranya; Neamati, Nouri; Patro, Balaram

doi:10.1016/j.bmcl.2013.07.017

Cited by 10 publications

(5 citation statements)

References 9 publications

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“…Cell viability was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, as previously described ( 20 , 21 ). The U87 glioma cells were seeded into a 96-well microplate at a density of 10 5 cells/well.…”

Section: Methodsmentioning

confidence: 99%

Pharmacokinetics and antitumor efficacy of DSPE-PEG2000 polymeric liposomes loaded with quercetin and temozolomide: Analysis of their effectiveness in enhancing the chemosensitization of drug-resistant glioma cells

Wang

et al. 2016

International Journal of Molecular Medicine

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In the present study, a new type of DSPE-PEG2000 polymeric liposome for the brain-targeted delivery of poorly water-soluble anticancer drugs was successfully prepared and characterized. The nanoparticles were formed by the self-assembly of an amphiphilic polymer consisting of hydrophilic 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000] (DSPE-PEG2000). These nanoliposomes served as a safe delivery platform for the simultaneous delivery of quercetin (QUE) and temozolomide (TMZ) to rat brains. The 2-in-1 PEG2000-DSPE nanoliposomes containing QUE and TMZ (QUE/TMZ-NLs) were rapidly taken up by the U87 glioma cells in vitro, whereas at the same concentrations, the amounts of the free drugs taken up were minimal. The QUE/TMZ-NLs showed an enhanced potency in the U87 cells and the TMZ-resistant U87 cells (U87/TR cells), possibly due to the high intracellular drug concentration and the subsequent drug release. In vivo biodistribution experiments revealed a significant accumulation of QUE/TMZ-NLs in the brain, with significantly increased plasma concentrations of QUE and TMZ, as well as delayed clearance in our rat model of glioma. The results were not so significant for the QUE-loaded nanoliposomes (QUE-NLs) and free TMZ. The findings of our study establish the DSPE-PEG2000 polymeric liposome as a novel and effective nanocarrier for enhancing drug delivery to brain tumors.

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Section: Methodsmentioning

confidence: 99%

Pharmacokinetics and antitumor efficacy of DSPE-PEG2000 polymeric liposomes loaded with quercetin and temozolomide: Analysis of their effectiveness in enhancing the chemosensitization of drug-resistant glioma cells

Wang

et al. 2016

International Journal of Molecular Medicine

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“…Growth inhibition was assessed using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay as described in Zeng et al (2012) and Saha et al (2013) . Cells were seeded in 96-well plates and treated with indicated drugs for 72 h. After drug treatments, cells were incubated with MTT (0.3 mg ml −1 ) for additional 3 h at 37°C.…”

Section: Methodsmentioning

confidence: 99%

Dual inhibition of survivin and MAOA synergistically impairs growth of PTEN-negative prostate cancer

Adisetiyo

Tamura

et al. 2015

Br J Cancer

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Background:Survivin and monoamine oxidase A (MAOA) levels are elevated in prostate cancer (PCa) compared to normal prostate glands. However, the relationship between survivin and MAOA in PCa is unclear.Methods:We examined MAOA expression in the prostate lobes of a conditional PTEN-deficient mouse model mirroring human PCa, with or without survivin knockout. We also silenced one gene at a time and examined the expression of the other. We further evaluated the combination of MAOA inhibitors and survivin suppressants on the growth, viability, migration and invasion of PCa cells.Results:Survivin and MAOA levels are both increased in clinical PCa tissues and significantly associated with patients' survival. Survivin depletion delayed MAOA increase during PCa progression, and silencing MAOA decreased survivin expression. The combination of MAOA inhibitors and the survivin suppressants (YM155 and SC144) showed significant synergy on the inhibition of PCa cell growth, migration and invasion with concomitant decrease in survivin and MMP-9 levels.Conclusions:There is a positive feedback loop between survivin and MAOA expression in PCa. Considering that survivin suppressants and MAOA inhibitors are currently available in clinical trials and clinical use, their synergistic effects in PCa support a rapid translation of this combination to clinical practice.

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“…sponge alkaloids ma’edamines A and B display significant cytotoxicity against COLO 205 (human colon cancer), MCF-7 (human breast cancer), and A549 (human lung) with IC 50 values of 7.9/10.3, 6.9/10.5, and 12.2/15.4 for ma’edamines A/B, respectively [ 145 ]. Synthetic analogues show activity against three breast cancer cell lines representing hormone receptor positive and HER2 positive breast cancer [ 146 ]. The bis-indole alkaloid 6″-debromohamacanthin A from a Spongosorites sp.…”

Section: Antitumor Compoundsmentioning

confidence: 99%

Biological Activity of Recently Discovered Halogenated Marine Natural Products

2015

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Synthesis and SAR studies of marine natural products ma’edamines A, B and their analogues

Cited by 10 publications

References 9 publications

Pharmacokinetics and antitumor efficacy of DSPE-PEG2000 polymeric liposomes loaded with quercetin and temozolomide: Analysis of their effectiveness in enhancing the chemosensitization of drug-resistant glioma cells

Pharmacokinetics and antitumor efficacy of DSPE-PEG2000 polymeric liposomes loaded with quercetin and temozolomide: Analysis of their effectiveness in enhancing the chemosensitization of drug-resistant glioma cells

Dual inhibition of survivin and MAOA synergistically impairs growth of PTEN-negative prostate cancer

Biological Activity of Recently Discovered Halogenated Marine Natural Products

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