Curcumin analogs: Their roles in pancreatic cancer growth and metastasis

Nagaraju, Ganji Purnachandra; Benton, Leah; Bethi, Shipra Reddy; Miyake, Shoji; El‐Rayes, Bassel F.

doi:10.1002/ijc.31867

Cited by 43 publications

(28 citation statements)

References 64 publications

(182 reference statements)

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“…Therefore, it is uncertain whether the discovered mechanisms of curcumin analog apply to curcumin itself. Moreover, the biosafety of these analogs has not been verified by long-term practice, so they are still a long way to the clinical translation [ 51 , 52 ]. Altogether, to address the problems of low bioavailability and potency of curcumin itself may be a more direct and efficient mean of curcumin being further translated as favorable pharmacotherapy against pancreatic adenocarcinoma.…”

Section: Introductionmentioning

confidence: 99%

Topically applicated curcumin/gelatin-blended nanofibrous mat inhibits pancreatic adenocarcinoma by increasing ROS production and endoplasmic reticulum stress mediated apoptosis

et al. 2020

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Background Pancreatic adenocarcinoma (PDAC) is one of the most fatal malignancies. Surgical resection supplemented by chemotherapy remains the major therapeutic regimen, but with unavoidable resistance and systemic toxic reaction. Curcumin is a known safe natural compound that can effectively eliminate pancreatic adenocarcinoma cells in vitro, making it a promising candidate for substitution in subsequent chemotherapy. However, due to its extremely low bioavailability caused by its insolubility and circular elimination, curcumin had an unexpectedly modest therapeutic effect in clinical trials. Results Here, we electrospun curcumin/gelatin-blended nanofibrous mat to largely improve curcumin’s bioavailability by local controlled-release. With characterization by scanning electron microscopy, fluorescence microscopy, Fourier transform infrared spectroscopy, X-ray diffraction and high-performance liquid chromatography, it was revealed that curcumin was uniformly dispersed in the fiber of the mats with nanoscopic dimensions and could be continuously released into the surrounding medium for days. The cancer inhibitory effects of nano-curcumin and underlying mechanisms were further explored by assays using pancreatic adenocarcinoma cell and experiments using xenograft model. The results showed the released nano-curcumin could effectively inhibit pancreatic adenocarcinoma cell proliferation not only in vitro, but more importantly in vivo. This cytotoxic effect of nano-curcumin against pancreatic adenocarcinoma was achieved through provoking the production of intracellular reactive oxygen species and activating endoplasmic reticulum stress, which leads to enhanced cell apoptosis via decreased phosphorylation of signal transducer and activator of transcription 3. Conclusions Clinically, curcumin/gelatin-blended nanofibrous mat could be a promising, secure, efficient and affordable substitutional agent for the elimination of residual cancer cells after tumor resection. Moreover, our strategy to obtain curcumin released from nanofibrous mat may provide a universally applicable approach for the study of the therapeutic effects and molecular mechanisms of other potential medicines with low bioavailability.

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Section: Introductionmentioning

confidence: 99%

Topically applicated curcumin/gelatin-blended nanofibrous mat inhibits pancreatic adenocarcinoma by increasing ROS production and endoplasmic reticulum stress mediated apoptosis

et al. 2020

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“…Previously the effect of nitrogen introduced in a form of 4‐piperidone structure to curcumin analogues was studied , . Many of the analogues demonstrated very good antiproliferative activities . Moreover, it was demonstrated that addition of thiols (a known mechanism of protein binding) to α,β‐unsaturated‐β′‐amino ketones (enones with additional β amino nitrogen) was significantly faster than addition to unmodified enones .…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Dicarbonyl Curcumin Analogues Containing the Tropane Scaffold

et al. 2019

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A general synthetic route to the unknown 1,3‐dicarbonyl tropane derived curcumin analogues was developed. The method was based on the aldol condensation reaction (40–90 % yield, two steps without product isolation) and acylation of the resulting 2‐benzylidenetropinones with substituted cinnamoyl cyanides (yields 41–91 %). Overall 18 new tropane derivatives featuring the characteristic curcuminoid hepta‐1,6‐dien‐3,5‐dione structure were synthesized and characterized. The range of the substituted aromatic rings in the prepared analogues included Ph, m‐MeO‐C6H4, 3,4‐di‐MeO‐C6H3, 3,4,5‐tri‐MeO‐C6H2, p‐Br‐C6H4, p‐F‐C6H4, p‐CF3‐C6H4, p‐NO2‐C6H4, 2‐NO2‐4,5‐di‐CH3O‐C6H2, 2‐NO2‐4,5‐O‐CH2‐O‐C6H2, 3‐MeO‐4‐[CH(CH3)‐OEt]‐C6H3, 3‐MeO‐4‐OH‐C6H3, p‐MeO‐C6H4, 4,5‐O‐CH2‐O‐C6H3, 3‐MeO‐4‐MeOCOO. Two orthogonal protective groups for hydroxyl (acetal or carbonate), removable in acidic or basic conditions, were used for synthesizing curcuminoids with free phenolic groups (3‐MeO‐4‐OH‐C6H3).

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“…Unfortunately, one main drawback to limit its use in medical application is rapid metabolism and low bioavailability 114 . As a consequence, many approaches have been adopted to circumvent this problem, including engineering its analogs by modulating curcumin structure 115 and improving its delivery systems through loading in nanoparticles 116 . Take HO-3867 for example.…”

Section: Resveratrolmentioning

confidence: 99%

STAT3 signaling in ovarian cancer: a potential therapeutic target

Liang¹,

Chen²,

Chen³

et al. 2020

J. Cancer

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Accumulating evidence has shown that Signal Transducer and Activator of Transcription 3 (STAT3) is thought to be a promising target for cancer therapy as STAT3 is frequently overexpressed in a wide range of cancer cells as well as clinical specimens, promoting tumor progression. It is widely accepted that STAT3 regulates a variety of cellular processes, such as tumor cell growth, survival, invasion, cancer stem cell-like characteristic, angiogenesis and drug-resistance. In this review, we focus on the role of STAT3 in tumorigenesis in ovarian cancer and discuss the existing inhibitors of STAT3 signaling that can be promisingly developed as the strategies for ovarian cancer therapy.

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Curcumin analogs: Their roles in pancreatic cancer growth and metastasis

Cited by 43 publications

References 64 publications

Topically applicated curcumin/gelatin-blended nanofibrous mat inhibits pancreatic adenocarcinoma by increasing ROS production and endoplasmic reticulum stress mediated apoptosis

Topically applicated curcumin/gelatin-blended nanofibrous mat inhibits pancreatic adenocarcinoma by increasing ROS production and endoplasmic reticulum stress mediated apoptosis

Synthesis of Dicarbonyl Curcumin Analogues Containing the Tropane Scaffold

STAT3 signaling in ovarian cancer: a potential therapeutic target

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