Synthesis and anti-inflammatory evaluation of novel mono-carbonyl analogues of curcumin in LPS-stimulated RAW 264.7 macrophages

Zhao, Chengguang; Cai, Yuepiao; He, Xuefeng; Li, Jianling; Zhang, Li; Wu, Jianzhang; Zhao, Yunjie; Yang, Shulin; Li, Xiaokun; Li, Wulan; Liang, Guang

doi:10.1016/j.ejmech.2010.09.037

Cited by 56 publications

(36 citation statements)

References 36 publications

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“…There are many attempts to synthesize curcumin analogues to circumvent the problem of low bioavailabilities and extensive metabolism (Anand et al 2007(Anand et al , 2008. In terms of the potential pharmacodynamic effects of curcumin, anti-inflammatory (Tham et al 2010;Zhao et al 2010) and antioxidant activities (Dai et al 2009) are two of the most prominent properties among all others. Interestingly, some analogues have independent anti-inflammatory activities that are not associated with the "antioxidant" activities (Lee et al 2009).…”

Section: Polyphenols: Curcumin and Curcmin Analoguesmentioning

confidence: 99%

Role of Nutraceuticals on Nrf2 and Its Implication in Cancer Prevention

Saw

Kong

2011

Nutraceuticals and Cancer

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"Nutraceuticals" have recently become a hot topic for the commercial world and the biomedical community. It is postulated that nutraceuticals are relatively non-toxic food supplements with many health benefits including prevention of cancer. Many nutraceuticals are antioxidants by nature; isothiocyanates and polyphenols have been extensively researched in many laboratories including ours. This chapter will cover nutraceuticals from the mechanistic perspectives, and how they would interact with Nuclear factor (erythroid-derived 2)-like 2 (Nrf2), which is the master regulator of the antioxidant response to counteract oxidative stress. Nrf2 deficient (knockout; KO) mice lack response to some nutraceutical cancer chemopreventive agents suggesting the important role of Nrf2 in cancer prevention. Nrf2 is also shown to have protective function against inflammation, a pathological process that is implicated in many diseases including carcinogenesis. Scientific evidence on the role of nutraceuticals on Nrf2 in anti-oxidative stress coupled with anti-inflammatory will also be discussed in this chapter.

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Section: Polyphenols: Curcumin and Curcmin Analoguesmentioning

confidence: 99%

Role of Nutraceuticals on Nrf2 and Its Implication in Cancer Prevention

Saw

Kong

2011

Nutraceuticals and Cancer

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“…Our group have designed and synthesized a series of MACs without b-diketone group for anti-inflammatory evaluation in the past several years and reviewed the current structure-activity relationship of MACs on anti-inflammatory and anti-cancer effect [1][2][3][4]. Among those compouds, C66 [(2E,6E)-2,6-bis(2-(trifluoromethyl)-benzylidene)-cyclohexanone] inhibited the increased plasma TNF-a levels and renal inflammatory gene expression, improved histological abnormalities and fibrosis of diabetic kidney, indicating this compund is a potential anti-inflammatory agent and might be beneficial for the prevention of diabetic nephropathy [5].…”

Section: Discussionmentioning

confidence: 99%

Crystal structure of 2-((E)-((E)-2-methylene-3-(2-(trifluoromethyl)-benzylidene)cyclopentylidene)methyl)thiophene, C18H13F3OS

Li¹,

Li²,

Ren³

et al. 2013

Zeitschrift Für Kristallographie - New Crystal Structures

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“…Though academic work relating to biological activities of curcumin has been published as early as 1949 (Schraufstatter and Bernt, 1949), insufficient studies on this interesting compound coupled by its poor bioavailability (Anand et al, 2007) have hindered the progress for curcumin to be developed adequately as a drug entity. Moreover, the focus on most of the synthesised analogues was on their anticancer activities (Hosoya et al, 2012;Makarov et al, 2010;Wei et al, 2012;Yadav et al, 2010), and only a handful was investigated for their anti-inflammatory properties (Katsori et al, 2011;Lee et al, 2009;Zhao et al, 2010).…”

Section: Introductionmentioning

confidence: 99%

“…Recent studies have shown that anti-inflammatory activities of the curcumin analogues were attributed to the electron-withdrawing groups in the diaryl rings (Jantan et al, 2012;Lee et al, 2009;Zhao et al, 2010). Antiinflammatory activities of curcumin and its analogues are attributed to their diverse array of targets in the inflammation process.…”

Section: Introductionmentioning

confidence: 99%

Immunomodulatory effects of diarylpentanoid analogues of curcumin

et al. 2015

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Diarylpentanoid analogues of curcumin are known for their various pharmacological activities which include the inhibition of inflammatory mediators and are good candidates as immunomodulators that could be useful in the treatment of inflammation. In the work described here, seventeen diarylpentanoid curcumin analogues were assessed for their inhibitory effects on the reactive oxygen species (ROS) production, chemotaxis and phagocytosis of human neutrophils. ROS production was evaluated using luminol and lucigenin-based chemiluminesence assay, while inhibition of isolated polymorphonuclear neutrophils chemotaxis and phagocytosis abilities were investigated using the Boyden chamber technique and the Phagotest kit, respectively. Two of the analogues, compounds 1e and 2e, which contain the 2-methyl-4(N-ethyl-N-ethylacetonitrile)aniline functional group, were active in all the assays performed. Moreover, analogues containing heteroatoms (1a, 1e, 2c, 2d, 2e, 3a and 3c) were active in suppressing the neutrophil phagocytic activity. The information obtained gave new insight into curcumin analogues with the potential to be developed as new immunomodulators.

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Synthesis and anti-inflammatory evaluation of novel mono-carbonyl analogues of curcumin in LPS-stimulated RAW 264.7 macrophages

Cited by 56 publications

References 36 publications

Role of Nutraceuticals on Nrf2 and Its Implication in Cancer Prevention

Role of Nutraceuticals on Nrf2 and Its Implication in Cancer Prevention

Crystal structure of 2-((E)-((E)-2-methylene-3-(2-(trifluoromethyl)-benzylidene)cyclopentylidene)methyl)thiophene, C18H13F3OS

Immunomodulatory effects of diarylpentanoid analogues of curcumin

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