Synthesis and evaluation of resveratrol derivatives as new chemical entities for cancer

Mulakayala, Chaitanya; Banaganapalli, Babajan; Madhusudana, P.; Anuradha, C. M.; Rao, Raja Mohan; Nune, Ravi Prakash; Manna, Sunil K.; Mulakayala, Naveen; Kumar, Chitta Suresh

doi:10.1016/j.jmgm.2013.01.005

Cited by 20 publications

(7 citation statements)

References 41 publications

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“…Some reports had found that resveratrol could interfere in the nuclear factor (NF)-κB signaling pathway, which regulates the expression of various genes involved in cancer and inflammation [7] [25] [26]. Some studies also indicated that the anticancer effect of resveratrol was mediated by inhibiting key proteins in signal transduction pathways such as mitogen-activated protein kinases, activator protein-1 (AP-1), and NF-κB [3].…”

Section: Synthesis Of Resveratrol Derivatives With Anticancer Activitymentioning

confidence: 99%

“…Resveratrol is one of the best characterized stilbenes and is known to possess a wide range of biological activities including anticancer [7] [8], antioxidant [9] [10], cardiovascular protection [11] [12], anti-inflammatory [13], antiviral [14] [15], antimicrobial [16], chemopreventive effect [17] [18], neuroprotective effect [19] [20] and immunomodulation activity [21]. Resveratrol was also used as herbal medicine in China and other East Asian countries.…”

Section: Introductionmentioning

confidence: 99%

“…In order to improve the bioavailability and anticancer activity of resveratrol, Mulakayala et al [7] synthesized two derivatives of resveratrol and evaluated their activity on U937 cells. Among the two synthetic resveratrol derivatives, the researchers found that the analogues of resveratrol (19 and 20) showed higher rates of inhibition than the parental molecule at 10 µM concentration.…”

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confidence: 99%

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Synthetic Resveratrol Derivatives and Their Biological Activities: A Review

Liu¹,

Liu²,

Chen³

et al. 2015

OJMC

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Resveratrol, a naturally derived stilbene that exists in various foods and beverages, has attracted extensive exploration due to its multiple biological activities, such as anticancer, antioxidant, cardiovascular protection, anti-inflammatory, antiviral, chemopreventive effect, neuroprotective effect, immunomodulation and so on. However, owing to its poor oral bioavailability, the application of resveratrol is greatly restricted. Because of that, a large amount of efforts had been made by researchers on designing its derivatives to obtain compounds with improved efficiency and low toxicity for developing more active drugs for clinical application. In this report, we review the current development of studying on resveratrol derivatives including their properties and activities. Additionally, this article also presents the synthetic routes of correlative resveratrol derivatives.

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Section: Synthesis Of Resveratrol Derivatives With Anticancer Activitymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

mentioning

confidence: 99%

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Synthetic Resveratrol Derivatives and Their Biological Activities: A Review

Liu¹,

Liu²,

Chen³

et al. 2015

OJMC

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“…Grapes and its fermented products, wine, probably are the two most important sources of resveratrol for people around the world . Even until recently, many researches continue to explore the physiochemical properties and biological activities of resveratrol as well as many of its structural derivatives hoping to realize the medical potential of such compounds . Pterostilbene is one of the important analogs of resveratrol, which has attracted many investigators' attention due to its potent bio‐functionalities.…”

Section: Introductionmentioning

confidence: 99%

“…). Both resveratrol and pterostilbene exhibit a wide range of biological activities, such as anticancer , antioxidant , anti‐inflammation , and cardioprotection which altogether contribute to the prevention of various chronic human diseases. However, the bioactivities of pterostilbene are most of the time superior to resveratrol due to its containing of methoxyl groups on the 3,5 meta‐positions.…”

Section: Introductionmentioning

confidence: 99%

Oral delivery system enhanced the bioavailability of stilbenes: Resveratrol and pterostilbene

et al. 2018

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Stilbenes are a large group of compounds with the C C C skeleton, in which two aromatic rings are connected by an ethylene bridge. Resveratrol and its structural analog, pterostilbene, are by far the two most widely researched stilbenes in terms of their beneficial bioactivities. However, the bioefficacy of these compounds is greatly reduced when consumed orally due to their poor aqueous solubility, which leads to poor bioavailability. To overcome the limitation, strategies improving their solubility, absorption, and systemic concentration were applied when designing a suitable edible delivery system. This review will summarize the findings from the studies evaluating the oral bioavailability of stilbenes with emphasize on the resveratrol and pterostilbene. It will also include the edible delivery systems currently available and their effect on the oral bioavailability. © 2018 BioFactors, 44(1):5-15, 2018.

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Piperlongumine, an alkaloid causes inhibition of PI3 K/Akt/mTOR signaling axis to induce caspase-dependent apoptosis in human triple-negative breast cancer cells

et al. 2014

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The phosphatidylinositol 3-kinase (PI3 K)/Akt/mammalian target of rapamycin (mTOR) signaling axis plays a central role in cell proliferation, growth and survival under physiological conditions. However, aberrant PI3 K/Akt/mTOR signaling has been implicated in many human cancers, including human triple negative breast cancer. Therefore, dual inhibitors of PI3 K/Akt and mTOR signaling could be valuable agents for treating breast cancer. The objective of this study was to investigate the effect of piperlongumine (PPLGM), a natural alkaloid on PI3 K/Akt/mTOR signaling, Akt mediated regulation of NF-kB and apoptosis evasion in human breast cancer cells. Using molecular docking studies, we found that PPLGM physically interacts with the conserved domain of PI3 K and mTOR kinases and the results were comparable with standard dual inhibitor PF04691502. Our results demonstrated that treatment of different human triple-negative breast cancer cells with PPLGM resulted in concentration- and time-dependent growth inhibition. The inhibition of cancer cell growth was associated with G1-phase cell cycle arrest and down-regulation of the NF-kB pathway leads to activation of the mitochondrial apoptotic pathway. It was also found that PPLGM significantly decreased the expression of p-Akt, p70S6K1, 4E-BP1, cyclin D1, Bcl-2, p53 and increased expression of Bax, cytochrome c in human triple-negative breast cancer cells. Although insulin treatment increased the phosphorylation of Akt (Ser473), p70S6K1, 4E-BP1, PPLGM abolished the insulin mediated phosphorylation, it clearly indicates that PPLGM acts through PI3 k/Akt/mTOR axis. Our results suggest that PPLGM may be an effective therapeutic agent for the treatment of human triple negative breast cancer.

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Synthesis and evaluation of resveratrol derivatives as new chemical entities for cancer

Cited by 20 publications

References 41 publications

Synthetic Resveratrol Derivatives and Their Biological Activities: A Review

Synthetic Resveratrol Derivatives and Their Biological Activities: A Review

Oral delivery system enhanced the bioavailability of stilbenes: Resveratrol and pterostilbene

Piperlongumine, an alkaloid causes inhibition of PI3 K/Akt/mTOR signaling axis to induce caspase-dependent apoptosis in human triple-negative breast cancer cells

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