In vitro anticancer activity evaluation of new cationic platinum(II) complexes based on imidazole moiety

Rimoldi, Isabella; Facchetti, Giorgio; Lucchini, Giorgio; Castiglioni, Elisa; Marchianò, Silvia; Ferri, Nicola

doi:10.1016/j.bmc.2017.02.010

Cited by 30 publications

(29 citation statements)

References 34 publications

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“…25,27 Amino-functionalized MSNs show higher loading capacity than those functionalized with carboxylic acid, but retained and do not release a considerable amount of the loaded drug, possibly due to strong interactions between Cis-Pt and amino groups. 28 On the other hand, platinum can coordinate with the imidazole group, as reported for a series of cytotoxic platinum dichlorocomplexes 29,30 and imidazolefunctionalized SBA15 for solid-phase microextraction. 31 Therefore, we aimed to employ a new synthesis approach to generate imidazoline (Imi) functionality (with less basicity than aliphatic amines) on the pores of magnetic mesoporous silica hybrid nanoparticles.…”

Section: Introductionmentioning

confidence: 84%

<p>Core–Shell Imidazoline–Functionalized Mesoporous Silica Superparamagnetic Hybrid Nanoparticles as a Potential Theranostic Agent for Controlled Delivery of Platinum(II) Compound</p>

Abedi¹,

Abolmaali²,

Abedanzadeh³

et al. 2020

IJN

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Introduction: As widely used chemotherapeutic agents, platinum compounds have several therapeutic challenges, such as drug resistance and adverse effects. Theranostic systems, macromolecular or colloidal therapeutics with companion diagnostics, not only address controlled drug delivery but also enable real-time monitoring of tumor sites. Methods: Synthesis of magnetic mesoporous silica nanoparticles (MMSNs) was performed for dual magnetic resonance imaging and drug delivery. MMSN surfaces were modified by imidazoline groups (MMSN-Imi) for cisplatin (Cis-Pt) conjugation via free N-termini to achieve wellcontrolled drug-release kinetics. Cis-Pt adsorption isotherms and drug-release profile at pH 5 and 7.4 were investigated using inductively coupled plasma atomic emission spectroscopy. Results: MMSN-Imi showed a specific surface area of 517.6 m 2 g −1 , mean pore diameter of 3.26 nm, and saturated magnetization of 53.63 emu/g. A relatively high r 2 /r 1 relaxivity value was obtained for MMSN-Imi. The nanoparticles provided high Cis-Pt loading with acceptable loading capacity (~30% w:w). Sustained release of Cis-Pt under acidic conditions led to specific inhibitory effects on the growth of human epithelial ovarian carcinoma cells, determined using MTT assays. Dual acridine orange-propidium iodide staining was investigated, confirming induction of apoptosis and necrotic cell death. Conclusion: MMSN-Imi exhibited potential for applications in cancer chemotherapy and combined imaging.

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Section: Introductionmentioning

confidence: 84%

<p>Core–Shell Imidazoline–Functionalized Mesoporous Silica Superparamagnetic Hybrid Nanoparticles as a Potential Theranostic Agent for Controlled Delivery of Platinum(II) Compound</p>

Abedi¹,

Abolmaali²,

Abedanzadeh³

et al. 2020

IJN

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“…After 24 h of incubation, the cells were treated with different concentrations of compounds. SRB assays were performed after 48 h as previously described [46]. Briefly, the cells were fixed by means of protein precipitation with 50% trichloroacetic acid at 4 • C (50 µL per well, final concentration 10%) for 1 h. After five washing with tap water, the cells were stained for 15 min with 0.4% SRB dissolved in 1% acetic acid (50 µL per well) and subsequently washed four times with 1% acetic acid to remove unbound stain.…”

Section: Cell Viability Assaymentioning

confidence: 99%

Himalayan Nettle Girardinia diversifolia as a Candidate Ingredient for Pharmaceutical and Nutraceutical Applications—Phytochemical Analysis and In Vitro Bioassays

et al. 2020

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Girardinia diversifolia, also known as Himalayan nettle, is a perennial herb used in Nepal to make fiber as well as in traditional medicine for the treatment of several diseases. To date, phytochemical studies and biological assays on this plant are scarce. Thus, in the present work, the G. diversifolia extracts have been evaluated for their potential pharmaceutical, cosmetic and nutraceutical uses. For this purpose, detailed phytochemical analyses were performed, evidencing the presence of phytosterols, fatty acids, carotenoids, polyphenols and saponins. The most abundant secondary metabolites were β- and γ-sitosterol (11 and 9% dw, respectively), and trans syringin (0.5 mg/g) was the most abundant phenolic. Fatty acids with an abundant portion of unsaturated derivatives (linoleic and linolenic acid at 22.0 and 9.7 mg/g respectively), vitamin C (2.9 mg/g) and vitamin B2 (0.12 mg/g) were also present. The antioxidant activity was moderate while a significant ability to inhibit acetylcholinesterase (AChE), butyrilcholinesterase (BuChE), tyrosinase, α-amylase and α-glucosidase was observed. A cytotoxic effect was observed on human ovarian, pancreatic and hepatic cancer cell lines. The effect in hepatocarcinoma cells was associated to a downregulation of the low-density lipoprotein receptor (LDLR), a pivotal regulator of cellular cholesterol homeostasis. These data show the potential usefulness of this species for possible applications in pharmaceuticals, nutraceuticals and cosmetics.

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“…RNA Preparation and Quantitative Real Time PCR-Total RNA was extracted with the iScriptTM RT-qPCR Sample Preparation Buffer (BIO-RAD) cDNA synthesis preparation reagents (Bio-Rad) according to manufacturer's instructions. Reverse transcription-polymerase first-strand cDNA synthesis was performed by using the Maxima First Strand cDNA Synthesis Kit (Thermo Scientific) [41]. qPCR was then performed by using the PowerUpTM SYBRTM Green Master Mix (Thermo Sigma clone DM1A; dilution 1:2.000).…”

Section: Retrotranscription and Quantitative Pcr (Rt-qpcr)mentioning

confidence: 99%

Differential Effects of Red Yeast Rice, Berberis Aristata and Morus Alba Extracts, Active Components of LopiGLIK®, on PCSK9 in HepG2 Cells

Mg¹,

Macchi²,

Marchianò³

et al. 2018

Preprint

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Proprotein convertase subtilisin/kexin type 9 (PCSK9) is the key regulator of low-density lipoprotein cholesterol (LDL-C) plasma levels. We previously observed that treatment of dyslipidemic subjects with nutraceutical combination containing red yeast rice (monacolin K 3.3 mg), Berberis aristata cortex extract (Berberine 531.25 mg) and Morus alba leaves extract (1-deoxynojirimycin 4 mg) (LopiGLIK®) did not alter the plasma PCSK9 levels. Thus, the aim of the present study was to investigate the effect of these three components on PCSK9 expression in HepG2 cell line in relationship to their effects on LDL-C cellular uptake. HepG2 cell line were incubated with Berberis aristata cortex extract (BCE), red yeast rice (RYR) and Morus alba leaves extract (MLE) alone or in combination for 24 h. RYR (50 µg/mL) increased PCSK9 protein expression (WB and ELISA assays), PCSK9 mRNA and its promoter activity. BCE (40 µg/mL) reduced PCSK9 expression, mRNA levels and promoter activity. MLE determined a concentration-dependent inhibition of PCSK9 at mRNA and protein levels, with a maximal reduction at 1 mg/mL; no significant changes in PCSK9 promoter activity were found. MLE also downregulates the expression of fatty acid synthase and HMG-CoA reductase mRNA levels. The combination of RYR, BCE and MLE reduced PCSK9 at mRNA, protein, and promoter activity. Finally, this combination induced the LDL receptor and LDL-C uptake by HepG2 cells. In conclusion, the positive effect of MLE on PCSK9 supports the rational of using this nutraceutical combination to control hyperlipidemic conditions.

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In vitro anticancer activity evaluation of new cationic platinum(II) complexes based on imidazole moiety

Cited by 30 publications

References 34 publications

<p>Core–Shell Imidazoline–Functionalized Mesoporous Silica Superparamagnetic Hybrid Nanoparticles as a Potential Theranostic Agent for Controlled Delivery of Platinum(II) Compound</p>

<p>Core–Shell Imidazoline–Functionalized Mesoporous Silica Superparamagnetic Hybrid Nanoparticles as a Potential Theranostic Agent for Controlled Delivery of Platinum(II) Compound</p>

Himalayan Nettle Girardinia diversifolia as a Candidate Ingredient for Pharmaceutical and Nutraceutical Applications—Phytochemical Analysis and In Vitro Bioassays

Differential Effects of Red Yeast Rice, Berberis Aristata and Morus Alba Extracts, Active Components of LopiGLIK®, on PCSK9 in HepG2 Cells

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In vitro anticancer activity evaluation of new cationic platinum(II) complexes based on imidazole moiety

Cited by 30 publications

References 34 publications

<p>Core–Shell Imidazoline–Functionalized Mesoporous Silica Superparamagnetic Hybrid Nanoparticles as a Potential Theranostic Agent for Controlled Delivery of Platinum(II) Compound</p>

<p>Core–Shell Imidazoline–Functionalized Mesoporous Silica Superparamagnetic Hybrid Nanoparticles as a Potential Theranostic Agent for Controlled Delivery of Platinum(II) Compound</p>

Himalayan Nettle Girardinia diversifolia as a Candidate Ingredient for Pharmaceutical and Nutraceutical Applications—Phytochemical Analysis and In Vitro Bioassays

Differential Effects of Red Yeast Rice, Berberis Aristata and Morus Alba Extracts, Active Components of LopiGLIK&reg;, on PCSK9 in HepG2 Cells

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Differential Effects of Red Yeast Rice, Berberis Aristata and Morus Alba Extracts, Active Components of LopiGLIK®, on PCSK9 in HepG2 Cells