An evaluation of the anti-neoplastic activity of curcumin in prostate cancer cell lines

Piantino, Camila Belfort; Salvadori, Fernanda Aburesi; Ayres, Pedro Paulo Marino Rodrigues; Kato, Raphael; Srougi, Victor; Leite, Kátia R. M.; Srougi, Miguel

doi:10.1590/s1677-55382009000300012

Cited by 38 publications

(19 citation statements)

References 23 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Even when 10-12 g/ml of curcumin was administered orally in humans, curcumin levels in serum remained approximately at 50 ng/ml [24]. Several studies demonstrated that 10-50 μM (3.7-18.4 μg/ml) curcumin induces cell death primarily through apoptosis [25,26]. However, the important question to be addressed is how to bring curcumin at these micromolar concentrations to the site of tumors while curcumin possesses such a low bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Characterization of CurcuEmulsomes: nanoformulation for enhanced solubility and delivery of curcumin

Ucisik

Küpcü

Schuster

et al. 2013

Journal of Nanobiotechnology

104

View full text Add to dashboard Cite

BackgroundCurcumin is a polyphenolic compound isolated from the rhizomes of the plant Curcuma longa and shows intrinsic anti-cancer properties. Its medical use remains limited due to its extremely low water solubility and bioavailability. Addressing this problem, drug delivery systems accompanied by nanoparticle technology have emerged. The present study introduces a novel nanocarrier system, so-called CurcuEmulsomes, where curcumin is encapsulated inside the solid core of emulsomes.ResultsCurcuEmulsomes are spherical solid nanoparticles with an average size of 286 nm and a zeta potential of 37 mV. Encapsulation increases the bioavailability of curcumin by up to 10,000 fold corresponding to a concentration of 0.11 mg/mL. Uptaken by HepG2 human liver carcinoma cell line, CurcuEmulsomes show a significantly prolonged biological activity and demonstrated therapeutic efficacy comparable to free curcumin against HepG2 in vitro - with a delay in response, as assessed by cell viability, apoptosis and cell cycle studies. The delay is attributed to the solid character of the nanocarrier prolonging the release of curcumin inside the HepG2 cells.ConclusionsIncorporation of curcumin into emulsomes results in water-soluble and stable CurcuEmulsome nanoformulations. CurcuEmulsomes do not only successfully facilitate the delivery of curcumin into the cell in vitro, but also enable curcumin to reach its effective concentrations inside the cell. The enhanced solubility of curcumin and the promising in vitro efficacy of CurcuEmulsomes highlight the potential of the system for the delivery of lipophilic drugs. Moreover, high degree of compatibility, prolonged release profile and tailoring properties feature CurcuEmulsomes for further therapeutic applications in vivo.

show abstract

Section: Introductionmentioning

confidence: 99%

Characterization of CurcuEmulsomes: nanoformulation for enhanced solubility and delivery of curcumin

Ucisik

Küpcü

Schuster

et al. 2013

Journal of Nanobiotechnology

104

View full text Add to dashboard Cite

show abstract

“…Curcumin lacks toxicity in humans (1), and extensive research over several decades has revealed that curcumin possesses anticancer, anti-inflammatory, antioxidant, antiviral and anti-bacterial activities (2,3). Curcumin suppressed cell proliferation or induced apoptosis in cultured prostate cancer cells and other types of cancer cells (4)(5)(6)(7)(8)(9)(10). Curcumin also inhibited prostate carcinogenesis (11).…”

Section: Introductionmentioning

confidence: 99%

Effects of cyclohexanone analogues of curcumin on growth, apoptosis and NF-κB activity in PC-3 human prostate cancer cells

Wei

Cui

et al. 2012

Oncology Letters

View full text Add to dashboard Cite

Abstract. Curcumin is a non-nutritive yellow pigment found in the spice turmeric, which is derived from the rhizome of the plant Curcuma longa Linn. Six cyclohexanone analogues of curcumin (A 1 -A 6 ) were investigated for their effects on growth and apoptosis in PC-3 human prostate cancer cells. The ability of these compounds to inhibit NF-κB activity in PC-3 cells was also determined. Five out of the six curcumin analogues (A 2 -A 6 ) had stronger inhibitory effects compared to curcumin on the growth of cultured PC-3 cells. Compounds A 2 -A 6 also had stronger stimulatory effects on apoptosis in PC-3 cells than curcumin, and these curcumin analogues more potently inhibited NF-κB activity than curcumin. The inhibitory effects of these compounds on NF-κB activity correlated with their effects on growth inhibition and apoptosis stimulation in PC-3 cells. The results of the present study provide a rationale for in vivo studies with A 2 -A 6 using suitable animal models of prostate cancer. IntroductionCurcumin is a non-nutritive yellow pigment found in the spice turmeric, which is derived from the rhizome of the plant Curcuma longa Linn. Curcumin lacks toxicity in humans (1), and extensive research over several decades has revealed that curcumin possesses anticancer, anti-inflammatory, antioxidant, antiviral and anti-bacterial activities (2,3). Curcumin suppressed cell proliferation or induced apoptosis in cultured prostate cancer cells and other types of cancer cells (4-10). Curcumin also inhibited prostate carcinogenesis (11). Studies from our laboratory and those of other authors have demonstrated enhanced anticancer activities of curcumin when combined with other anticancer agents (12-14). Findings of earlier studies showed that curcumin exerts a wide range of anticancer effects by modulating a diversity of signaling pathways, including nuclear factor-κB (NF-κB) and other pathways (15)(16)(17)(18)(19)(20). Curcumin has entered clinical trials for certain types of human cancer (21-23). However, the clinical efficacy of curcumin is limited, which is likely to be due to its low bioavailability (21-23). It was suggested that the β-diketone moiety of curcumin causes instability and poor metabolic properties (24-26). Enhanced stability was found in curcumin analogues by deleting the β-diketone moiety of the molecule (27). Recently, it was demonstrated that the cyclohexanone analogues of curcumin have enhanced stability in biological medium compared to curcumin (28). The cyclohexanone-containing curcumin analogue 2,6-bisp[(3-methoxy-4-hydroxyphenyl)methylene)]-cyclohexanone was found to be more potent than curcumin for inhibiting NF-κB in human breast cancer cells in vitro (29).In an earlier study, we synthesized a series of cyclohexanone curcumin analogues and determined their inhibitory effect on the activity of aldose reductase (30). In the present study, we investigated the effects of these curcumin analogues on the growth and apoptosis of human prostate cancer PC-3 cells. We also determined the inhibitory effect ...

show abstract

“…Numerous studies have demonstrated the anticancer activity of curcumin and curcumin analogues in animal models [2][3][4][5][6][7] as well as growth inhibition and apoptosis induction in a variety of cancer cell lines in vitro. [8][9][10][11][12][13][14][15][16] However, the clinical efficacy of curcumin is limited, which is likely due to its low bioavailability. [17][18][19] We have previously reported on the synthesis and evaluation of sixty-one curcumin-related compounds for inhibitory effects on cultured prostate cancer cells, pancreatic cancer cells and colon cancer cells.…”

mentioning

confidence: 99%

Effects of Curcumin Analogues for Inhibiting Human Prostate Cancer Cells and the Growth of Human PC-3 Prostate Xenografts in Immunodeficient Mice

Dai

Ding

Doren

et al. 2014

Biological & Pharmaceutical Bulletin

View full text Add to dashboard Cite

Four curcumin analogues ((2E,6E)-2,6-bis(thiophen-3-methylene) cyclohexanone (AS), (2E,5E)-2,5-bis(thiophen-3-methylene) cyclopentanone (BS), (3E,5E)-3,5-bis(thiophen-3-methylene)-tetrahydropyran-4-one (ES) and (3E,5E)-3,5-bis(thiophen-3-methylene)-tetrahydrothiopyran-4-one (FS) as shown in Fig. 1) with different linker groups were investigated for their effects in human prostate cancer CWR-22Rv1 and PC-3 cells. Compounds FS and ES had stronger inhibitory effects than curcumin, AS and BS on the growth of cultured CWR-22Rv1 and PC-3 cells, as well as on the androgen receptor (AR) and nuclear factor kappa B (NF-κB) activity. The strong activities of ES and FS may be correlated with a heteroatom linker. In animal studies, severe combined immunodeficient (SCID) mice were injected subcutaneously (s.c.) with PC-3 cells in Matrigel. After 4 to 6 weeks, mice with PC-3 tumors (about 0.6 cm wide and 0.6 cm long) received daily intraperitoneal (i.p.) injections of vehicle, ES and FS (10 µg/g body weight) for 31 d. FS had a potent effect in inhibiting the growth and progression of PC-3 tumors. Our results indicate that FS may be useful for inhibiting human prostate tumors growth. Key words curcumin analog; prostate cancer cell; prostate tumorProstate cancer is one of the leading causes of death among men in the United States.1) Prostate carcinogenesis has been viewed as a multistage and complex process consisting of initiation, promotion, and progression. Despite the tremendous efforts and resources devoted to treatment, incidence and mortality rate are still high. Although patients with metastatic prostate cancer can benefit from androgen ablation, most of them will die of prostate cancer progression due to an androgen-refractory state. Hence, much attention has been paid to the discovery of chemopreventive substances from various edible and medicinal plants, a large number of which have been identified.Curcumin is a non-nutritive yellow pigment found in the spice turmeric, which is derived from the rhizome of the plant Curcuma longa LINN. Numerous studies have demonstrated the anticancer activity of curcumin and curcumin analogues in animal models 2-7) as well as growth inhibition and apoptosis induction in a variety of cancer cell lines in vitro. [8][9][10][11][12][13][14][15][16] However, the clinical efficacy of curcumin is limited, which is likely due to its low bioavailability. [17][18][19] We have previously reported on the synthesis and evaluation of sixty-one curcumin-related compounds for inhibitory effects on cultured prostate cancer cells, pancreatic cancer cells and colon cancer cells. 20) Four of these curcumin analogues with different linker groups but identical symmetrical aromatic rings (as shown in Fig. 1) were selected for the present study. These compounds included (2E,6E)-2,6-bis(thiophen-3-methylene) cyclohexanone (AS), (2E,5E)-2,5-bis(thiophen-3-methylene) cyclopentanone (BS), (3E,5E)-3,5-bis(thiophen-3-methylene)-tetrahydropyran-4-one (ES), (3E,5E)-3,5-bis(thiophen-3-methylene)-tetrahydrothiopyran-4...

show abstract

An evaluation of the anti-neoplastic activity of curcumin in prostate cancer cell lines

Cited by 38 publications

References 23 publications

Characterization of CurcuEmulsomes: nanoformulation for enhanced solubility and delivery of curcumin

Characterization of CurcuEmulsomes: nanoformulation for enhanced solubility and delivery of curcumin

Effects of cyclohexanone analogues of curcumin on growth, apoptosis and NF-κB activity in PC-3 human prostate cancer cells

Effects of Curcumin Analogues for Inhibiting Human Prostate Cancer Cells and the Growth of Human PC-3 Prostate Xenografts in Immunodeficient Mice

Contact Info

Product

Resources

About