Intracellular Accumulation and Cytotoxicity of Doxorubicin with Different Pharmaceutical Formulations in Human Cancer Cell Lines

2006 ◽  
Vol 6 (9) ◽  
pp. 3062-3069 ◽  
Author(s):  
Loredana Serpe ◽  
Marilena Guido ◽  
Roberto Canaparo ◽  
Elisabetta Muntoni ◽  
Roberta Cavalli ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Liposomal Doxorubicin ◽  
Human Cancer ◽  
Blue Dye ◽  
Intracellular Accumulation ◽  
U373 Cell ◽  
Free Doxorubicin ◽  
Ht 29

The structure of both carrier and anticancer drug affects the intracellular fate of a transported drug. The study investigated in vitro intracellular accumulation and cytotoxic activity of doxorubicin-loaded solid lipid nanoparticles (SLN), doxorubicin in pegylated liposomes (Caelyx<snm>®</snm>) and free doxorubicin. Intracellular doxorubicin levels and cytotoxic activity were determined by high performance liquid chromatography with fluorescence detection, and by the trypan blue dye exclusion assay, respectively. Doxorubicin-loaded SLN inhibited cell growth more strongly than either free or liposomal doxorubicin, in human colorectal adenocarcinoma, HT-29, retinoblastoma Y79, and glioblastoma U373 cell lines. The IC50 values for doxorubicin-loaded SLN were significantly lower after 24 h exposure than those for free doxorubicin in all cell lines; after 48 h exposure they were lower than those for liposomal doxorubicin in HT-29 and Y79 cells. The enhanced cytotoxic activity of doxorubicin-loaded SLN was associated with increased drug incorporation in cells: intracellular doxorubicin levels were significantly enhanced after exposure to drug-loaded SLN versus either free or liposomal drug. Rate of intracellular accumulation and cytotoxic activity also differed among different cell lines; in particular, cells of epithelial origin were found to be more sensitive to doxorubicin-loaded SLN. In conclusion, the greater sensitivity of HT-29, Y79, and U373 cells to doxorubicin-loaded SLN than to the other drug formulations may be due to the capability of the delivery system to enhance drug action, through a marked uptake and accumulation of SLN within the cell.

Design, Synthesis, and Cytotoxic Activity of New Tubulysin Analogues

Synlett ◽  
2021 ◽  
Author(s):  
Anh Tuan Tran ◽  
Chien Van Tran ◽  
Hai Van Le ◽  
Loc Van Tran ◽  
Thao Thi Phuong Tran ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Cytotoxic Activities ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Ht 29

AbstractSynthesis of tubulysin analogues, containing an N-methyl substituent on tubuvaline-amide together with the replacement of either the hydrophobic N-terminal N-methyl pipecolic acid (Mep) or at both N- and C- terminal peptides with available heteroaromatic acids and an unsaturated tubuphenylalanine moiety, respectively, were described. The in vitro cytotoxic activity by SRB assay on five cancer cell lines for sixteen tubulysins was evaluated. Among them, five analogues exhibited strong cytotoxic activities against five human cancer cell lines, including human breast carcinoma (MCF7), human colorectal adenocarcinoma (HT-29), HL-60, SW-480, human lung adenocarcinoma (A459). Interestingly, one analogue showed the strongest cytotoxicity on all five tested cell lines even much higher toxicity than the reference compound ellipticine.

scholarly journals Synthesis of New Simplified and Racemic Hemiasterlin Derivatives with Extremely High Cytotoxicity

2018 ◽  
Vol 13 (12) ◽  
pp. 1934578X1801301
Author(s):  
Pham The Chinh ◽  
Đang Thi Tuyet Anh ◽  
Duong Huong Quynh ◽  
Le Nhat Thuy Giang ◽  
Nguyen Ha Thanh ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Human Cancer ◽  
Microtubule Depolymerization ◽  
Antimitotic Agent ◽  
Human Cancer Cell Lines ◽  
Weak Activity ◽  
High Cytotoxicity ◽  
Chemistry Community

Hemiasterlin is a potent antimitotic agent acting through inhibition of microtubule depolymerization. For this reason, the synthesis of new hemiasterlin derivatives has attracted a lot of interest in the organic chemistry community recently. In this paper, the synthesis and evaluation of the cytotoxicity of new simplified and racemic hemiasterlin derivatives were reported. All of the synthesized analogues were evaluated in vitro for cytotoxic activity against four human cell lines (KB, Hep-G2, LU and MCF7). Most of these analogues possess a strong cytotoxic activity on two human cancer cell lines (KB and Hep-G2) and very weak activity on LU and MCF7 cell lines.

CYTOTOXIC ACTIVITY OF LUVUNGA SCANDENS AGAINST HUMAN CANCER CELL LINES

2016 ◽  
Vol 78 (10) ◽  
Author(s):  
Putri Nur Hidayah Al-Zikri ◽  
Muhammad Taher ◽  
Deny Susanti ◽  
Solachuddin Jauhari Arief Ichwan
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
A549 Cell ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Breast Adenocarcinoma ◽  
Human Cancer Cell Lines ◽  
Mcf 7

Luvunga scandens belongs to the family of Rutaceae which usually inhabit tropical and moist environment. This plant is known as ‘Mengkurat Jakun’ among locals and used traditionally to treat fever and fatigue via decoction. The aim of this study was to investigate the cytotoxic activity of the leaves and stems extracts of L. scandens extract. Extracts of the leaves and stems were obtained from sequential extraction procedures by various organic solvents. All extracts were subjected to cytotoxic study by 3-(4, 5-dimethylthaizol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. In in vitro cytotoxicity assay, all L. scandens extracts exhibited cytotoxicity against human breast adenocarcinoma (MCF-7) and human lung adenocarcinoma (A549) cell lines. The IC50 values of dichloromethane and methanol extracts from the leaves of L. scandens against MCF-7 cell line were 62.5 µg/mL and 88.0 µg/mL, respectively, whereas IC50 of methanol extract from stem was 81.0 µg/mL. All extracts were less active against A549 cell line where IC50 value were not be determined. The present findings revealed the potential of L. scandens as a cytotoxic agent against MCF-7 cell line. However, further studies should be planned to evaluate role of the plant in cytotoxic activity.

scholarly journals Cytotoxic Activities in Vitro of Flower Extracts of Three Species of Aloe Growing in Yemen: Aloe Rubroviolaceae, Aloe Vera and Aloe Sabaea, against Eleven Types of Cancer Cell Lines

2021 ◽  
Vol 8 (5) ◽  
pp. 01-10
Author(s):  
Hassan A. Al-Shamahy
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Aloe Vera ◽  
Cancer Cell Lines ◽  
Myelogenous Leukemia ◽  
Methanolic Extracts

Background and aims: Natural products, especially plant extracts, have opened up great opportunities in the field of drug progress due to their chemical variety. The genus Aloe has long been used for medicinal uses in countless parts of the world. This study was designed to investigate the phytochemicals and anti-cancer capabilities of Aloe rubroviolaceae, Aloe vera and Aloe sabaea flowers. Materials and Methods: The methanolic extracts of three types of plants traditionally used in Yemen to treat a variety of diseases have been tested in vitro for their potential anticancer activity on different human cancer cell lines. The cytotoxic activity of the methanolic extracts of tested plants was determined using eleven strains of human cancer cells, namely: MCF-7 (breast cancer), PC-3 (prostate cancer), HEP-2 (human epithelial carcinoma), MNFS-60 (myelogenous leukemia), CACO (intestinal cancer), A-549 (lung adenocarcinoma), HeLa (cervical cancer), RD (rhabdomyosarcoma),HepG2 (hepatocellular carcinoma), HCT-116 (colon cancer), and CHO-K1 (Chinese hamster ovary). A colorimetric sulforhodamine B assay was used to evaluate the in vitro cytotoxic activity of different extracts. Growth inhibition of 50% (IC50) for each extract was calculated from the optical density of treated and untreated cells. Doxorubicin, a broad-spectrum anticancer drug was used as a positive control. Results: More interesting cytotoxic activity was observed for Aloe vera extract more than Aloe sabaea and Aloe rubroviolaceae, extract. Conclusions: This study provides a preliminary screening for anti-proliferative activity of various Aloe species flowers extracts on different cancer cell lines. Different extracts of Aloe species significantly inhibit the growth of various cancer cell lines in a concentration-dependent manner. Further investigations are required to understand the possible mechanism(s) of action of these extract on various cancer cells and isolation of active phyto-chemicals.

scholarly journals CYTOTOXIC ACTIVITIES IN VITRO OF FLOWER EXTRACTS OF THREE SPECIES OF ALOE GROWING IN YEMEN:ALOE RUBROVIOLACEAE, ALOE VERA AND ALOE SABAEA, AGAINST ELEVEN TYPES OF CANCER CELL LINES

2021 ◽  
Author(s):  
Hassan Mohammed Al-Mahbashi ◽  
Mohammad Abobakr Al-Ghazali ◽  
Hassan A. Al-Shamahy ◽  
Azhar Azher Mohammed Al-Ankoshy
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Peer Review ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Aloe Vera ◽  
Cancer Cell Lines ◽  
Ethanolic Extracts

 Background and aims: Natural products, in particular plant extracts, have opened up great chance in the area of drug progress owing to their chemical variety. The Aloe genus has long been known to be used for medicinal uses in countless parts of the world. This study was planned to inspect the phytochemicals and anti-cancer capabilities of Aloe rubroviolaceae, Aloe vera and Aloe sabaea flowers. Materials and Methods: Three types of ethanolic extracts of plants traditionally used in Yemen to treat a variety of diseases have been tested in vitro for their potential anticancer activity on different human cancer cell lines. The cytotoxic activity of the ethanolic extracts of tested plants was determined using eleven strains of human cancer cells, namely: MCF-7 (breast cancer), PC-3 (prostate cancer), HEP-2(human epithelial carcinoma), MNFS-60 (myelogenous leukemia), CACO (intestinal cancer), A-549 (lung adenocarcinoma), HeLa (cervical cancer),RD (rhabdomyosarcoma), HepG2 (hepatocellular carcinoma), HCT-116 (colon cancer),  and CHO-K1(Chinese hamster ovary). A colorimetric sulforhodamine B assay was applied to assess the in vitro cytotoxic activity of various extracts. Growth inhibition of 50% (IC50) for each extract was calculated from the optical density of treated and untreated cells. Doxorubicin, a broad-spectrum anticancer drug was used as a positive control. Results: More interesting cytotoxic activity was observed for Aloe vera extract more than Aloe sabaea and Aloe rubroviolaceae, extract.  Conclusions: This study presents an initial screening for anti-proliferative activity of a variety of Aloe species flowers extracts on diverse cancer cell lines. Different extracts of Aloe species significantly inhibit the growth of various cancer cell lines  in a concentration-dependent manner. Advance researches are necessary to understand the possible mechanism(s) of action of these extract on a variety of cancer cells and separation of active phyto-chemicals.                   Peer Review History: Received: 18 July 2021; Revised: 17 August; Accepted: 8 September, Available online: 15 September 2021 Academic Editor:  Dr. Muhammad Zahid Iqbal, AIMST University, Malaysia, [email protected] UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency.  Received file:                Reviewer's Comments: Average Peer review marks at initial stage: 6.5/10 Average Peer review marks at publication stage: 7.5/10 Reviewers: Dr. U. S. Mahadeva Rao, Universiti Sultan Zainal Abidin, Terengganu Malaysia, [email protected] Dr. Nazim Hussain, BFIT, Dehradun, Uttarakhand, India, [email protected] Similar Articles: ANTIFUNGAL, CYTOTOXIC AND PHYTOTOXICITY OF AERIAL PART OF RANUNCULUS MURICATUS IN VITRO INHIBITORY ACTIVITY OF BERBERIS VULGARIS L. AGAINST LEISHMANIA TROPICA PROMASTIGOTES

scholarly journals Chemical Composition and In vitro Cytotoxic Activity of the Essential Oils of Stachys rupestris and Salvia heldreichiana, Two Endemic Plants of Turkey

2013 ◽  
Vol 8 (11) ◽  
pp. 1934578X1300801 ◽  
Author(s):  
Elif Ayşe Erdogan ◽  
Ayşe Everest ◽  
Laura De Martino ◽  
Emilia Mancini ◽  
Michela Festa ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Essential Oils ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Endemic Plants ◽  
Total Oil

The chemical composition of the essential oils of two endemic plants of Turkey, Stachys rupestris Montbret et Aucher ex Benth. and Salvia heldreichiana Boiss. ex Benth., were obtained by hydrodistillation and studied by GC and GC–MS. In all, 46 compounds were identified, 22 for S. rupestris accounting for 94.6 % of the total oil and 30 for S. heldreichiana, accounting for 91.9 % of the total oil. The presence of diterpenoids (50.7%) characterized the oil from S. rupestris, while S. heldreichiana oil was rich in oxygenated sesquiterpenes (78.9%). The essential oils were evaluated for their in vitro potential cytotoxic activity on three human cancer cell lines. The oil of S. rupestris showed the higher antiproliferative activity against PC-3 and MCF-7 cancer cell lines.

Screening of in vitro cytotoxic activity potential of Odontobuthus doriae and bothutus Saulcyi scorpion venoms against a panel of human cancer cell lines

Toxicon ◽  
2019 ◽  
Vol 158 ◽  
pp. S49
Author(s):  
Toktam M. Kashani ◽  
Amir Salarian ◽  
Hossein Vatanpour ◽  
Farshad Shirazi ◽  
Abbas Zare ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Scorpion Venoms

scholarly journals A New Bibenzyl-phenanthrene Derivative from Dendrobium signatum and its Cytotoxic Activity

2016 ◽  
Vol 11 (5) ◽  
pp. 1934578X1601100 ◽  
Author(s):  
Arparporn Mittraphab ◽  
Chawanphat Muangnoi ◽  
Kittisak Likhitwitayawuid ◽  
Pornchai Rojsitthisak ◽  
Boonchoo Sritularak
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Human Cancer ◽  
Mass Spectrometric ◽  
Human Cancer Cell ◽  
Mass Spectrometric Data ◽  
Human Cancer Cell Lines ◽  
Spectrometric Data ◽  
Whole Plant ◽  
Ht 29

From the whole plant of Dendrobium signatum, a new bibenzyl-dihydrophenanthrene derivative, named dendrosignatol was isolated, together with the known compounds 3,4-dihydroxy-3,4′-dimethoxybibenzyl, dendrocandin B, dendrocandin I and dendrofalconerol A. The structure of the new compound was elucidated through analysis of its spectroscopic and mass spectrometric data. All of the isolates showed appreciable cytotoxic activity against three human cancer cell lines, including MDA-231, HepG2 and HT-29 cells.

scholarly journals Lipophilised resveratrol affects the generation of reactive nitrogen species in murine macrophages and cell viability of human cancer cell lines

2019 ◽  
Vol 7 ◽  
Author(s):  
Won Young Oh ◽  
Yi-Shiou Chiou ◽  
Min-Hsiung Pan ◽  
Fereidoon Shahidi
Keyword(s):  
Cell Viability ◽  
Cell Lines ◽  
Human Cancer ◽  
Raw 264.7 Cells ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Nitrite Production ◽  
Anti Inflammatory ◽  
Ht 29

Resveratrol was esterified with selected fatty acids to improve its lipophilicity and potential application in food and biological systems. In this study, resveratrol and monoesters of resveratryl propionate (RC3:0) and resveratryl docosahexaenate (RDHA) were examined for their effects on anti-inflammatory and anti-proliferative activity in vitro.  All test compounds showed a decreased nitrite production in murine RAW 264.7 cells in a concentration dependent manner. Resveratrol, RC3:0, and RDHA were evaluated for their effects on cell viability using liver cancer (HepG2), colon cancer (HT-29, A431), breast cancer (MCF7), and gastric cancer (AGS) cell lines. All test compounds showed decreased cell viability of HepG2, A431, MCF7, HT-29, and AGS in a concentration-dependent manner. The results suggest that resveratrol esters may serve as potential anti-inflammatory and anti-proliferative agents.

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