Curcumin and its Analogues (PGV-0 and PGV-1) Enhance Sensitivity of Resistant MCF-7 Cells to Doxorubicin through Inhibition of HER2 and NF-kB Activation

Meiyanto, Edy; Putri, Dyaningtyas Dewi Pamungkas; Susidarti, Ratna Asmah; Murwanti, Retno; Sardjiman,; Fitriasari, Aditya; Husnaa, Ulfatul; Purnomo, Hari; Kawaichi, Masashi

doi:10.7314/apjcp.2014.15.1.179

Cited by 113 publications

(103 citation statements)

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“…According to the IC50 values, the cytotoxicity of PGB-0 is less potent than lapatinib (IC50 = 8µM) and curcumin (IC50= 25µM) (the data was not shown). However, commonly, the requirement of chemopreventive and cochemotherapeutic agents only need a compound possessing specific target in cancer cells (Meiyanto et al, 2014). On the other hand, boron carrying pharmaceutical also requires non-cytotoxic compound to minimize the nonselective toxicity to the patient (Barth, 2005).…”

Section: Pgb-0 Decrease Her2 Expressionmentioning

confidence: 99%

“…Thus, the less cytotoxicity of PGB-0 tends to be an advantage compared to lapatinib and curcumin. Curcumin and its analogues are well known inducing G2/M arrest (Meiyanto et al, 2014) though, PGB-0 induced sub-G1 cells accumulation. Cells in sub-G1 phase were described as a hypodiploid cell with low DNA content due to the DNA fragmentation and possibly apoptotic cells.…”

Section: Pgb-0 Decrease Her2 Expressionmentioning

confidence: 99%

“…Pentagamavunon-0 (PGV-0) and Pentagamavunon-1 (PGV-1) are developed by modifying the active methylene groups into cyclopentanone to overcome curcumin instability. The previous study showed that curcumin, PGV-0, and PGV-1 possess cytotoxic effect and inhibit NFκB activation in vitro in MCF-7 breast cancer cells, as well as interact with the HER2 receptor in silico (Meiyanto et al, 2014). The interaction between HER2 receptor with PGV-0 and PGV-1 is mediated through the H-bond between O atom on carbonyl group of PGV-0, and PGV-1 with N atom of Leu846 from the HER2 receptor.…”

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Synthesis and Cytotoxic Activity of 2,5-Bis(4-Boronic Acid)benzylidine Cyclopentanone on Her2 Overexpressed-Cancer Cells

Utomo¹,

Putri²,

Pudjono³

et al. 2017

Indonesian J. Pharm.

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Development of chemotherapeutic agent and boron carrying pharmaceutical based on HER2 specific targeted is important due to its role in enhancing cancer progression. The purpose of this study is to synthesize curcumin analogue, namely Pentagamaboron-0 (PGB-0) or 2,5-bis(4-boronic acid)benzylidine cyclopentanone, and to explore the cytotoxic activity on HER2 overexpressed-cancer cells. MCF-7/HER2 was used as a model of HER2 overexpressed-cancer cells and NIH3T3 as normal cells. PGB-0 bound to ATP binding site of HER2 and EGFR based on molecular docking study. PGB-0 was synthesized resulting in 33% yield and was confirmed by IR, 1 HNMR, 13 CNMR and Mass spectroscopy. Based on MTT assay PGB-0 decreased cells viability on MCF-7/HER2 cells with IC 50 value of 270µM but performed no effect on NIH3T3 cells. Cell cycle analysis revealed that PGB-0 increased sub-G1 accumulation. PGB-0 decreased HER2 expression in a dose-dependent manner. We conclude that the new compound PGB-0 inhibits cell growth through cell death induction and decreased HER2 expression. Thus, PGB-0 is potential to be developed as a chemotherapeutic agent and boron carrying pharmaceutical targeted on the HER2 receptor.

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Section: Pgb-0 Decrease Her2 Expressionmentioning

confidence: 99%

Section: Pgb-0 Decrease Her2 Expressionmentioning

confidence: 99%

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Synthesis and Cytotoxic Activity of 2,5-Bis(4-Boronic Acid)benzylidine Cyclopentanone on Her2 Overexpressed-Cancer Cells

Utomo¹,

Putri²,

Pudjono³

et al. 2017

Indonesian J. Pharm.

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“…13,14 Among the optional herbs, curcumin (CUR) has been extensively investigated because it can induce apoptosis -or even death -of the sensitized cancer cells by inhibiting the activity of human epidermal growth factor receptor-2 and nuclear factor κB. 15,16 CUR is also an effective sensitizer that can restrict the activity of some MDR-related proteins and inhibit different types of cancer cells from proliferating. 17,18 Therefore, it will be feasible to use DOX and CUR together for alleviating MDR of some cancer cells while enhancing the therapeutic efficacy of DOX.…”

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confidence: 99%

“…15,16 In comparison to free DOX, the enhanced cytotoxicity for A549 cells arising from DOX + CUR at higher doses can be attributed to the synergistic effects of DOX and CUR ( Figure 6A and B). As mentioned in the "Assembly of PMs" section, DOX had been desalted to facilitate its loading, and hence, deprotonated DOX became somewhat hydrophobic.…”

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confidence: 99%