Synthesis of di-pyropheophorbide-a-platinum(II) complex and the in vitro cytotoxicity against TC-1 tumor cells

2012 ◽  
Vol 16 (09) ◽  
pp. 1024-1031 ◽  
Author(s):  
Gantumur Battogtokh ◽  
Hai-Bo Liu ◽  
Su-Mi Bae ◽  
Pankaj Kumar Chaturvedi ◽  
Yong-Wan Kim ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Anticancer Agent ◽  
Platinum Complex ◽  
Cancer Cell Line ◽  
In Vitro Cytotoxicity ◽  
Coupling Reagents ◽  
Uv Absorption Spectroscopy ◽  
Pyropheophorbide A ◽  
Potassium Tetrachloroplatinate

This report focuses on the conjugation of a chemotherapeutic drug and photodynamic therapy (PDT) agent with the intention of obtaining an optimal anticancer agent for use in combination cancer treatment. We have used pyropheophorbide-a (PPa) as a PDT agent, which was linked with ethylenediamine using carbodimide/N-hydroxysuccinicimide coupling reagents to obtain a resulting reactive amine group. Next, the free amine-bearing PPa and potassium tetrachloroplatinate (K2PtCl4) were reacted in aqueous solution to obtain PPa-cisplatin complex. Subsequently, the PPa-based platinum complex was characterized through several methods including NMR spectroscopy, mass spectrometer and UV absorption spectroscopy and its in vitro cytotoxicity and cellular uptake were evaluated on the TC-1 cancer cell line. The results indicated that the conjugate has a greater cytotoxic effect in the dark than cisplatin, even though its phototoxic effect was slightly lower than that of free photosensitizer; in addition, the cellular uptake of complex at 0.125 and 0.25 μM was higher than that of free photosensitizer.

Recent Advances in Curcumin Nanocarriers for the Treatment of Different Types of Cancer with Special Emphasis on In Vitro Cytotoxicity and Cellular Uptake Studies

2020 ◽  
Vol 10 (5) ◽  
pp. 577-590
Author(s):  
Jai B. Sharma ◽  
Shailendra Bhatt ◽  
Asmita Sharma ◽  
Manish Kumar
Keyword(s):  
Cancer Cells ◽  
Cellular Uptake ◽  
Anticancer Agents ◽  
Targeted Delivery ◽  
In Vitro Cytotoxicity ◽  
Curcumin Nanoparticles ◽  
Cytotoxicity Studies ◽  
Delivery Technique ◽  
Different Types

Background: The potential use of nanocarriers is being explored rapidly for the targeted delivery of anticancer agents. Curcumin is a natural polyphenolic compound obtained from rhizomes of turmeric, belongs to family Zingiberaceae. It possesses chemopreventive and chemotherapeutic activity with low toxicity in almost all types of cancer. The low solubility and bioavailability of curcumin make it unable to use for the clinical purpose. The necessity of an effective strategy to overcome the limitations of curcumin is responsible for the development of its nanocarriers. Objective: This study is aimed to review the role of curcumin nanocarriers for the treatment of cancer with special emphasis on cellular uptake and in vitro cytotoxicity studies. In addition to this, the effect of various ligand conjugated curcumin nanoparticles on different types of cancer was also studied. Methods: A systematic review was conducted by extensively surfing the PubMed, science direct and other portals to get the latest update on recent development in nanocarriers of curcumin. Results: The current data from recent studies showed that nanocarriers of curcumin resulted in the targeted delivery, higher efficacy, enhanced bioavailability and lower toxicity. The curcumin nanoparticles showed significant inhibitory effects on cancer cells as compared to free curcumin. Conclusion: It can be concluded that bioavailability of curcumin and its cytotoxic effect to cancer cells can be enhanced by the development of curcumin based nanocarriers and it was found to be a potential drug delivery technique for the treatment of cancer.

scholarly journals The cytotoxic activity of pine needles ethanolic extract of Pinus merkusii on HeLa cell lines

2021 ◽  
Vol 33 ◽  
pp. 03001
Author(s):  
Annise Proboningrat ◽  
Amaq Fadholly ◽  
Sri Agus Sudjarwo ◽  
Fedik Abdul Rantam ◽  
Agung Budianto Achmad
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Anticancer Agent ◽  
Ethanolic Extract ◽  
In Vitro Cytotoxicity ◽  
Hela Cell Lines ◽  
Cytotoxicity Assessment ◽  
Pinus Merkusii

Several efforts have been made to discover new anticancer agents based on natural ingredients. Meanwhile, previous studies have shown that different Pine genus species exhibit cytotoxic activity against various types of cancer cells. This plant is rich in phenolic compounds, especially procyanidins, flavonoids, and phenolic acids. Therefore, this study aims to investigate the in vitro cytotoxicity of Pinus merkusii needles extract on HeLa cancer cell lines. The cytotoxicity assessment was measured using MTT assay and expressed as IC50 value. The results showed that the ethanolic extract poses a dose and time-dependent cytotoxic activity with an IC50 value of 542.5 µg/ml at 48 hours of incubation. Based on this result, Pinus merkusii needles’ ethanolic extract has the potential of a novel candidate for an anticancer agent.

Synthesis and in vitro cytotoxicity evaluation of ruthenium polypyridyl-sensitized paramagnetic titania nanoparticles for photodynamic therapy

RSC Advances ◽  
2016 ◽  
Vol 6 (53) ◽  
pp. 47520-47529 ◽  
Author(s):  
Mohammad H. Sakr ◽  
Najeeb M. Halabi ◽  
Leen N. Kalash ◽  
Sara I. Al-Ghadban ◽  
Mayyasa K. Rammah ◽  
...  
Keyword(s):  
A549 Cells ◽  
Cancer Cell Line ◽  
In Vitro Cytotoxicity ◽  
Lung Cancer Cell Line ◽  
Titania Nanoparticles ◽  
Human Lung Cancer ◽  
Type I ◽  
Dye Sensitized ◽  
Photo Dynamic Therapy

We demonstrate the effective cytotoxic properties of a dye-sensitized metal oxide in an in vitro model of a human lung cancer cell line (A549 cells) upon light irradiation, where a type I mechanism photo-dynamic therapy is realized exclusively.

HYALURONIC ACID-DOCETAXEL CONJUGATE LOADED NANOLIPOSOMES FOR TARGETING TUMOR CELLS

2020 ◽  
pp. 88-99
Author(s):  
MULUNEH FROMSA SEIFU ◽  
LILA KANTA NATH ◽  
DEBASHIS DUTTA
Keyword(s):  
Hyaluronic Acid ◽  
Glial Cells ◽  
Cellular Uptake ◽  
Drug Loading ◽  
Microscopic Investigation ◽  
In Vitro Cytotoxicity ◽  
Scanning Calorimetry ◽  
Anticancer Efficacy ◽  
Apoptotic Effect

Objective: Docetaxel (DTX), a potent anticancer drug, is suffering from non-specificity and drug resistance as major limitations. In this investigation, we developed Hyaluronic acid (HA)-Docetaxel conjugate (HA-DTX) loaded nanoliposomes to target cancer cells via passive and active targeting approaches. Methods: HA-DTX was synthesized and characterized by UV-Visible spectrophotometry, FT-IR spectroscopy, 1H NMR spectroscopy, Differential scanning calorimetry and X-ray diffraction and then loaded into nanoliposomes (L-NLs) by thin-film hydration method. L-NLs were characterized physicochemically and evaluated for anticancer efficacy by in vitro cytotoxicity study in glioma cells (C6 glial cells); cellular uptake and apoptotic effect were investigated by fluorescence microscopy. Results: HA-DTX was successfully synthesized; L-NLs had an average size of 123.0±16.53 nm, polydispersity index of 0.246±0.01 and zeta potential of 44.4±6.79 mV. Also, L-NLs exhibited 90.54%±4.22 of drug loading efficiency and 2.68%±0.12 of drug loading, releasing about 57.72%±1.17 at pH 5.2 and only 14.14%±1.32 at pH 7.4 after 48 h. No significant change instability was observed after storage at 5 °C±3 °C as well as at 25 °C±2 °C/60% RH±5% RH for 6 mo. The cytotoxicity effect of L-NLs was higher by 10% that of marketed formulation at 10 µg/ml docetaxel concentration. Fluorescence microscopic investigation showed that more cellular uptake and apoptotic effect were observed in L-NLs treated C6 glial cells than in those treated with the marketed formulation. Conclusion: HA-DTX loaded nanoliposomes enabled docetaxel to target C6 glial cells with better efficacy and might be effective to treat glioma.

In Vitro Cytotoxicity and Cellular Uptake of Tamoxifen Citrate-Loaded Polymeric Micelles

2020 ◽  
Vol 21 (8) ◽  
Author(s):  
Mohamed Nasr ◽  
Fahima Hashem ◽  
Raghda Abdelmoniem ◽  
Norhan Tantawy ◽  
Mohamed Teiama
Keyword(s):  
Cellular Uptake ◽  
Polymeric Micelles ◽  
In Vitro Cytotoxicity ◽  
Tamoxifen Citrate

Paclitaxel-Loaded TPGS-b-PCL Nanoparticles: In Vitro Cytotoxicity and Cellular Uptake in MCF-7 and MDA-MB-231 Cells versus mPEG-b-PCL Nanoparticles and Abraxane®

2016 ◽  
Vol 16 (1) ◽  
pp. 160-170 ◽  
Author(s):  
Ezequiel Bernabeu ◽  
Lorena Gonzalez ◽  
Maria J. Legaspi ◽  
Marcela A. Moretton ◽  
Diego A. Chiappetta
Keyword(s):  
Cellular Uptake ◽  
In Vitro Cytotoxicity ◽  
Mcf 7

scholarly journals Preclinical evaluation of new α-radionuclide therapy targeting LAT1: 2-[211At]astato-α-methyl-L-phenylalanine in tumor-bearing model

2020 ◽  
Author(s):  
Yasuhiro OHSHIMA ◽  
Hiroyuki Suzuki ◽  
Hirofumi Hanaoka ◽  
Ichiro Sasaki ◽  
Shigeki Watanabe ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Radionuclide Therapy ◽  
Cancer Cell Line ◽  
Strand Break ◽  
The Body ◽  
Cellular Growth ◽  
Dna Double Strand Break ◽  
Amino Acid Analog

Abstract PURPOSE: Targeted α-radionuclide therapy has growing attention as a promising therapy for refractory cancers. However, the application is limited to certain types of cancer. Since L-type amino acids transporter 1 (LAT1) is highly expressed in various human cancers, we prepared LAT1-selective α-emitting amino acid analog, 2-[211At]astato-α-methyl-L-phenylalanine ([211At]-2-AAMP), and evaluated its potential as a therapeutic agent. METHODS: [211At]-2-AAMP was prepared from the stannyl precursor. Stability of [211At]-2-AAMP was evaluated by both in vitro and in vivo. In vitro studies using LAT1 expressing human ovary cancer cell line, SKOV3, were performed for evaluating cellular uptake and cytotoxicity of [211At]-2-AAMP. Biodistribution and therapeutic studies in SKOV3 bearing mice were performed after intravenous injection of [211At]-2-AAMP. RESULTS: [211At]-2-AAMP was stable in murine plasma in vitro and excreted into urine as intact. Cellular uptake of [211At]-2-AAMP was inhibited by treatment with LAT1-selective inhibitor. After 24 hours of incubation, [211At]-2-AAMP suppressed clonogenic growth at 10 kBq/ml, and induced cell death and DNA double strand break at 25 kBq/ml. When injected to mice, [211At]-2-AAMP exhibited the peak accumulation in the tumor at 30 min postinjection, and the radioactivity levels in the tumor retained up to 60 min. The majority of the radioactivity was rapidly eliminated from the body into the urine as an intact form immediately after injection. [211At]-2-AAMP significantly improved the survival of mice (P<0.05) without serious side effects. CONCLUSION: [211At]-2-AAMP showed α-radiation-dependent cellular growth inhibition after taking up via LAT1. Furthermore, [211At]-2-AAMP provided a beneficial effect on survival in vivo. These findings suggest that [211At]-2-AAMP might be useful for treatment of LAT1-positive cancer.

scholarly journals Synthesis, Spectral Characterization, and In Vitro Cytotoxicity of Some Fe(III) Complexes Bearing Unsymmetrical Salen-Type Ligands Derived from 2-Hydroxynaphthaldehyde and Substituted Salicylaldehydes

2021 ◽  
Vol 2021 ◽  
pp. 1-9
Author(s):  
Quang Trung Nguyen ◽  
Phuong Nam Pham Thi ◽  
Nguyen Van Tuyen
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Line ◽  
Tumor Cell Line ◽  
In Vitro Cytotoxicity ◽  
Ionization Mass ◽  
Hek 293 ◽  
Human Cancer Cell Lines

Six Fe(III) complexes bearing unsymmetrical salen-type ligands derived from 2-hydroxynaphthaldehyde and substituted salicylaldehydes were synthesized by coordinating the unsymmetrical salen-type ligands with FeCl3.6H2O. The synthetic complexes were characterized by electrospray ionization mass spectra (ESI-MS), effective magnetic moments (μeff), and infrared (IR) and ultraviolet-visible (UV-Vis) spectra. The spectroscopic data are in good agreement with the suggested molecular formulae of the complexes. Their cyclic voltammetric studies in acetonitrile solutions showed that the Fe(III)/Fe(II) reduction processes are electrochemically irreversible. The in vitro cytotoxicity of the obtained complexes was screened on human cancer cell lines KB (a subline of Hela tumor cell line) and HepG2 (a human liver cancer cell line) and a normal human cell line HEK-293 (Human Embryonic Kidney cell line). The results showed that the synthetic Fe(III) complexes are highly cytotoxic and quite selective. The synthetic complexes bearing unsymmetrical salen-type ligands with different substituted groups in the salicyl ring indicate different cytotoxicity.

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