Theracurmin® efficiently inhibits the growth of human prostate and bladder cancer cells via induction of apoptotic cell death and cell cycle arrest

Kang, Minyong; Ho, Jin‐Nyoung; Kook, Ha Rim; Lee, Sang Chul; Oh, Jong Jin; Hong, Sung Kyu; Byun, Seok‐Soo

doi:10.3892/or.2015.4537

Cited by 19 publications

(20 citation statements)

References 31 publications

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“…Camptothecin is a well known positive control for sub-G1 arrest 30,31 and for inducing apoptosis. 32,33 Therefore, this suggests that BNIPDaCHM and trans,trans-BNIPDaCHM could use similar mechanisms of action compared to camptothecin and may trigger apoptotic cell death in MDA-MB-231 and SKBR-3 human breast cancer cells.…”

Section: Cell Cycle Analysismentioning

confidence: 99%

Novel bisnaphthalimidopropyl (BNIPs) derivatives as anticancer compounds targeting DNA in human breast cancer cells

et al. 2016

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Bisnaphthalimidopropyl (BNIP) derivatives are a family of compounds that exert anti-cancer activities in vitro and, according to previous studies, variations in the linker sequence have increased their DNA binding and cytotoxic activities. By modifying the linker sequence of bisnaphthalimidopropyl diaminodicyclohexylmethane (BNIPDaCHM), a previously synthesised BNIP derivative with anti-cancer properties, three novel BNIP derivatives were designed. Bisnaphthalimidopropyl-piperidylpropane (BNIPPiProp), a structural isomer of BNIPDaCHM, bisnaphthalimidopropyl ethylenedipiperidine dihydrobromide (BNIPPiEth), an isoform of BNIPDaCHM with a shorter linker chain, and (trans(trans))-bisnaphthalimidopropyl diaminodicyclohexylmethane (trans,trans-BNIPDaCHM), a stereoisomer of BNIPDaCHM, were successfully synthesised (72.3-29.5% yield) and characterised by nuclear magnetic resonance spectroscopy (NMR) and mass spectrometry (MS). Competitive displacement of ethidium bromide (EtBr) and UV binding studies were used to study the interactions of BNIP derivatives with Calf Thymus DNA. The cytotoxicity of these derivatives was assessed against human breast cancer MDA-MB-231 and SKBR-3 cells by MTT assay. Propidium iodide (PI) flow cytometry was conducted in order to evaluate the cellular DNA content in both breast cancer cell lines before and after treatment with BNIPs. The results showed that all novel BNIPs exhibit strong DNA binding properties in vitro, and strong cytotoxicity, with IC values in the range of 0.2-3.3 μM after 24 hours drug treatment. Two of the novel BNIP derivatives, BNIPPiEth and trans,trans-BNIPDaCHM, exhibited greater cytotoxicity against the two breast cancer cell lines studied, compared to BNIPDaCHM. By synthesising enantiopures and reducing the length of the linker sequence, the cytotoxicity of the BNIP derivatives was significantly improved compared to BNIPDaCHM, while maintaining DNA binding and bis-intercalating properties. In addition, cell cycle studies indicated that trans,trans-BNIPDaCHM, the most cytotoxic BNIP derivative, induced sub-G1 cell cycle arrest, indicative of apoptotic cell death. Based on these findings, further investigation is under way to assess the potential efficacy of trans,trans-BNIPDaCHM and BNIPPiEth in treating human breast cancer.

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Section: Cell Cycle Analysismentioning

confidence: 99%

Novel bisnaphthalimidopropyl (BNIPs) derivatives as anticancer compounds targeting DNA in human breast cancer cells

et al. 2016

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“…concentration [7,18,49,50]. Theracurmin® is made with gum ghatti to improve gut absorption and enhance the effects of CUR in the body which range from cardiovascular health to free radical protection [7,18,50]. Other products such as Longvida® use solid lipid curcumin particle (SLCP) technology to enhance the bioavailability of CUR by protecting CUR from degradation in the stomach and promoting free drug absorption in the gut.…”

Section: Ivyspringmentioning

confidence: 99%

“…CUR has biological and pharmacological relevance making it an exciting molecule with anti-inflammatory, anti-carcinogenic, anti-malarial and anti-viral properties, in addition to low toxicity [3,[6][7][8][9][10][11]. Efforts by others have shown the selectivity of CUR towards tumor cells compared to healthy cells which embarked the use of curcumin for cancer treatment [5,[12][13][14][15][16][17][18]. CUR has multiple anticancer facets including blocking tumor initiation, as well as suppressing tumor progression and inhibiting invasion and metastasis [8,12,[18][19][20][21][22][23].…”

Section: Introductionmentioning

confidence: 99%

“…Efforts by others have shown the selectivity of CUR towards tumor cells compared to healthy cells which embarked the use of curcumin for cancer treatment [5,[12][13][14][15][16][17][18]. CUR has multiple anticancer facets including blocking tumor initiation, as well as suppressing tumor progression and inhibiting invasion and metastasis [8,12,[18][19][20][21][22][23]. CUR acts on matrix metalloproteinases, cyclooxygenase, vascular endothelial growth factor (VEGF), tumor necrosis factor alpha (TNF-α), among other signal transduction pathways [8, 12-15, 24, 25].…”

Section: Introductionmentioning

confidence: 99%

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Liposomes Aid Curcumin's Combat with Cancer in a Breast Tumor Model

Jadia¹,

Kydd²,

Piel³

et al. 2018

Oncomedicine

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Curcumin (CUR), a natural compound, has multiple antineoplastic properties and specificity toward tumor cells, however its bioavailability and water solubility are poor. Liposomes increase the therapeutic index of CUR by protecting the drug from enzymatic degradation and can be made long circulating by surface modification with polyethylene glycol (PEG). Folate receptor α (FRα) is overexpressed in several types of cancer. Therefore, a folate-conjugated liposomal CUR nanoconstruct can enhance tumor targeted drug therapy. In this study, we synthesized, characterized and tested the cytotoxicity of CUR loaded liposomes (folate modified and non-folate modified) and CUR free drug in non-malignant breast epithelial cells and breast cancer cells, in addition to assessing the effects of CUR on cell cycle. The breast cancer cells not only had increased uptake of liposomes compared to non-malignant cells, but also more showed greater cytotoxicity resulted from treatments with free CUR and liposomal CUR (folate surface-modified and non-folate liposome types). The imaging and killing results, indicated that the liposomal CUR formulations do not alter the therapeutic efficacy and selectivity of CUR to provide anticancer benefits. Moreover, the differences in cellular uptake between the two liposomal nanoconstructs were studied using flow cytometry which showed targeting of folate surface-modified liposomes in cancer cells based on the findings presented.

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“…Theracurmin shows antioxidant activity through the regulation of reactive oxygen species and NQO1 inhibition in esophageal squamous cell carcinoma cells . It also induces apoptosis in human prostate and bladder cancer cells . In CRC research, Theracurmin suppressed DSS‐induced carcinogenesis by decreasing inflammation‐related gene expression in vivo .…”

Section: Introductionmentioning

confidence: 99%

Theracurmin inhibits intestinal polyp development in Apc‐mutant mice by inhibiting inflammation‐related factors

Adachi

Hamoya²,

Fujii

et al. 2020

Cancer Science

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Colorectal cancer (CRC) is the second leading cause of cancer death worldwide.Therefore, it is important to establish useful methods for preventing CRC. One prevention strategy involves the use of cancer chemopreventive agents, including functional foods. We focused on the well-known cancer chemopreventive agent curcumin, which is derived from turmeric. However, curcumin has the disadvantage of being poorly soluble in water due to its high hydrophobicity. To overcome this problem, the formation of submicron particles with surface controlled technology has been applied to curcumin to give it remarkably improved water solubility, and this derived compound is named Theracurmin. To date, the preventive effects of Theracurmin on hereditary intestinal carcinogenesis have not been elucidated. Thus, we used Apc-mutant mice, a model of familial adenomatous polyposis, to evaluate the effects of Theracurmin. First, we showed that treatment with 10-20 µM Theracurmin for 24 hours reduced nuclear factor-κB (NF-κB) transcriptional activity in human colon cancer DLD-1 and HCT116 cells. However, treatment with curcumin mixed in water did not change the NF-κB promoter transcriptional activity. As NF-κB is a regulator of inflammation-related factors, we next investigated the downstream targets of NF-κB: monocyte chemoattractant protein-1 (MCP-1) and interleukin (IL)-6. We found that treatment with 500 ppm Theracurmin for 8 weeks inhibited intestinal polyp development and suppressed MCP-1 and IL-6 mRNA expression levels in the parts of the intestine with polyps. This report provides a proof of concept for the ongoing Theracurmin human trial (J-CAP-C study). K E Y W O R D Scolorectal cancer chemoprevention, curcumin, min mice, nuclear factor-κB, Theracurmin

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Theracurmin® efficiently inhibits the growth of human prostate and bladder cancer cells via induction of apoptotic cell death and cell cycle arrest

Cited by 19 publications

References 31 publications

Novel bisnaphthalimidopropyl (BNIPs) derivatives as anticancer compounds targeting DNA in human breast cancer cells

Novel bisnaphthalimidopropyl (BNIPs) derivatives as anticancer compounds targeting DNA in human breast cancer cells

Liposomes Aid Curcumin's Combat with Cancer in a Breast Tumor Model

Theracurmin inhibits intestinal polyp development in Apc‐mutant mice by inhibiting inflammation‐related factors

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