A Novel Synthetic Mono-Carbonyl Analogue of Curcumin, A13, Exhibits Anti-Inflammatory Effects In vivo by Inhibition of Inflammatory Mediators

Wang, Yi; Yu, Congcong; Pan, Yong; Yang, Xuyi; Huang, Yi Wen; Zhang, Feng; Li, Xiaokun; Yang, Shulin; Liang, Guang

doi:10.1007/s10753-011-9350-4

Cited by 16 publications

(6 citation statements)

References 44 publications

(79 reference statements)

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“…Thus, 22 presents potent proapoptotic and anti-angiogenic assets in vitro and in vivo , suggesting it to be a potential and promising remedy for treatment of ER-negative breast cancer. Other in vivo rodent studies not specifically reviewed here are likewise encouraging that the wide-ranging MAC family of anti-inflammatory and anti-cancer agents may well be able to address the corresponding debilitating conditions in humans sometime in the future [ 8 , 15 , 16 , 17 , 67 , 68 , 90 , 97 , 110 , 111 , 114 , 118 ].…”

Section: Cancer Mediation In Vitro and mentioning

confidence: 77%

“…In general, the anti-inflammatory activity of curcumin analogs results primarily from inhibition of nuclear factor kappa-B (NF-κB), tumor necrosis factor (TNF)-α, and interleukin (IL)-6, NF-κB being a key transcriptional factor in the inflammatory signaling pathway. Many studies have reported that MACs may target both inflammation and tumors by inhibiting the activation of NF-κB [ 8 , 23 , 60 , 61 , 62 , 63 , 64 , 65 , 66 , 67 , 68 , 69 , 70 , 71 , 72 , 73 , 74 ]. The anti-inflammatory properties and the ability to inhibit the immune response by MACs, at least in part, result from inhibition of the activation of the latter multi-protein complex, since many of the genes that are implicated in the immune/inflammatory response are upregulated by NF-κB.…”

Section: Inflammation Control In Vitro and mentioning

confidence: 99%

“…Compound 55 likewise shows significant in vivo effects on pro-inflammatory cytokine production in plasma and liver; namely, attenuated lung histopathology and reduced mortality in endotoxemic mice [ 67 ]. In LPS-challenged mice, pretreatment by 56 ( Figure 7 ) attenuated the increase of plasma levels of NO, TNF-α and IL-6, while significantly reducing the hepatic inflammatory gene transcription by the inhibition of various inflammatory mediators [ 68 ]. Compounds 57 and 58 ( Figure 7 ) significantly alleviate renal and cardiac injuries in diabetes mellitus by means of an anti-inflammatory mechanism [ 69 , 70 ].…”

Section: Inflammation Control In Vitro and mentioning

confidence: 99%

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Eliminating the Heart from the Curcumin Molecule: Monocarbonyl Curcumin Mimics (MACs)

et al. 2014

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Curcumin is a natural product with several thousand years of heritage. Its traditional Asian application to human ailments has been subjected in recent decades to worldwide pharmacological, biochemical and clinical investigations. Curcumin’s Achilles heel lies in its poor aqueous solubility and rapid degradation at pH ~ 7.4. Researchers have sought to unlock curcumin’s assets by chemical manipulation. One class of molecules under scrutiny are the monocarbonyl analogs of curcumin (MACs). A thousand plus such agents have been created and tested primarily against cancer and inflammation. The outcome is clear. In vitro, MACs furnish a 10–20 fold potency gain vs. curcumin for numerous cancer cell lines and cellular proteins. Similarly, MACs have successfully demonstrated better pharmacokinetic (PK) profiles in mice and greater tumor regression in cancer xenografts in vivo than curcumin. The compounds reveal limited toxicity as measured by murine weight gain and histopathological assessment. To our knowledge, MAC members have not yet been monitored in larger animals or humans. However, Phase 1 clinical trials are certainly on the horizon. The present review focuses on the large and evolving body of work in cancer and inflammation, but also covers MAC structural diversity and early discovery for treatment of bacteria, tuberculosis, Alzheimer’s disease and malaria.

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Section: Cancer Mediation In Vitro and mentioning

confidence: 77%

Section: Inflammation Control In Vitro and mentioning

confidence: 99%

Section: Inflammation Control In Vitro and mentioning

confidence: 99%

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Eliminating the Heart from the Curcumin Molecule: Monocarbonyl Curcumin Mimics (MACs)

et al. 2014

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“…Several studies have reported this ability of polyphenols. For instance, curcumin and different flavonoids, such as flavones, EGCG, and flavonols, are able to inhibit the secretion of TNF-α, IL-6, IL-1β, IL-8, and IFN-γ from various cell types [ 121 , 122 , 123 , 124 , 125 , 126 , 127 , 128 , 129 ].…”

Section: Effects Of Polyphenols In MMmentioning

confidence: 99%

The Potential Protective Effects of Polyphenols in Asbestos-Mediated Inflammation and Carcinogenesis of Mesothelium

et al. 2016

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Malignant Mesothelioma (MM) is a tumor of the serous membranes linked to exposure to asbestos. A chronic inflammatory response orchestrated by mesothelial cells contributes to the development and progression of MM. The evidence that: (a) multiple signaling pathways are aberrantly activated in MM cells; (b) asbestos mediated-chronic inflammation has a key role in MM carcinogenesis; (c) the deregulation of the immune system might favor the development of MM; and (d) a drug might have a better efficacy when injected into a serous cavity thus bypassing biotransformation and reaching an effective dose has prompted investigations to evaluate the effects of polyphenols for the therapy and prevention of MM. Dietary polyphenols are able to inhibit cancer cell growth by targeting multiple signaling pathways, reducing inflammation, and modulating immune response. The ability of polyphenols to modulate the production of pro-inflammatory molecules by targeting signaling pathways or ROS might represent a key mechanism to prevent and/or to contrast the development of MM. In this review, we will report the current knowledge on the ability of polyphenols to modulate the immune system and production of mediators of inflammation, thus revealing an important tool in preventing and/or counteracting the growth of MM.

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“…The novel (2E,5E)-2,5-bis(4-(3(dimethylamino)-propoxy) benzylidene) cyclopentanone (A13) has been observed to reduce nitric oxide (NO), TNF-α, HGF and IL-6. In addition, it reduces damages to the lung and reduced pain in several induced inflammatory models [34]. Neutralizing IL-6 antibodies have been used to block the JAK1-STAT3 signaling pathway in a lung cancer model [5].…”

Section: Il-6 Targeted Treatmentmentioning

confidence: 99%

Interleukin-6 Cytokine: A Multifunctional Glycoprotein for Cancer

et al. 2013

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Interleukin 6 is a multifunctional cytokine. Its increased levels have been associated with elevated cancer risk, and also these levels have been found to be a prognostic factor for several cancer types. In addition, increased levels have been found in coronary heart disease, insulin resistant patients, advance stage cancer patients, atopy/ asthma and in patients with blood circulating micrometastasis. Additionally several studies with different types of cancers have been performed to identify the correlation between interleukin-6 levels, stage, treatment response and severity of symptoms. The influence of interleukin-6 is performed mainly through the janus kinase-signal transducer and activator of transcription-zinc finger protein 1-2 signaling pathway. As a result, the increased levels of interleukin-6 are responsible for enhanced neo-angiogenesis, inhibition of cancer cell apoptosis and deregulation of the control mechanisms in the microenvironment. In addition, increased levels of inteleukin-6 have been found to increase the production of collagen and a-actin which induce interstitial lung disease. In the current mini review we will present information regarding the interleukin-6 and published results in several cancer studies and finally we will comment in future treatment approaches blocking this cytokine in cancer patients.

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A Novel Synthetic Mono-Carbonyl Analogue of Curcumin, A13, Exhibits Anti-Inflammatory Effects In vivo by Inhibition of Inflammatory Mediators

Cited by 16 publications

References 44 publications

Eliminating the Heart from the Curcumin Molecule: Monocarbonyl Curcumin Mimics (MACs)

Eliminating the Heart from the Curcumin Molecule: Monocarbonyl Curcumin Mimics (MACs)

The Potential Protective Effects of Polyphenols in Asbestos-Mediated Inflammation and Carcinogenesis of Mesothelium

Interleukin-6 Cytokine: A Multifunctional Glycoprotein for Cancer

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