scholarly journals Cytotoxicity evaluation of a new series of naphthalimide derivatives against human cancer cell lines

2019 ◽  
Author(s):  
Alireza Aliabadi ◽  
Ahmad Mohammadi-Farani ◽  
Arash Haqiqi ◽  
Elham Khanlari
Keyword(s):  
Cell Lines ◽  
Human Cancer ◽  
Basic Study ◽  
Human Cancer Cell Lines ◽  
Lead Compounds ◽  
Cancerous Cell ◽  
Pc3 Cells ◽  
New Anticancer Drugs ◽  
Ht 29

Introduction: Cancer has been known as one the main causes of the death in the world. In recent researches, discovery of effective, selective and safe medications is a priority and emergency. In recent reports, the role of lipoxygenases (LOX) has been confirmed in neoplastic diseases. Some isoenzymes such as 5, 12 and 15 have more importance in the neoplasia. According to the efficacy of naphthalimides as LOX inhibitor, herein we explored the cytotoxicity of naphthalimide derivatives.  Methods: A basic study was carried out in the current research. The cytotoxicity of a new series of naphthalimide-based 15-LOX-1 inhibitors was evaluated in three cancerous cell lines namely SKNMC (neuroblastoma), PC3 (prostatic cancer), HT29 (colorectal cancer) using MTT protocol and the obtained data was compared to doxorubicin. Calculation of the IC50 of tested compounds was performed by regression analysis using Prism-6 software. Results: Totally, all tested compounds exhibited inferior activity than doxorubicin towards HT-29, SKNMC and PC3 cell lines. SKNMC cell line rendered more sensitivity to tested compounds. Amongst the compounds 3a-3m, compound 3e (3-methoxy) and 3i (4-F) with IC50 = 5.92±1.78 µM and 10.04±1.7 µM were the most potent derivatives towards PC3 cells. Conclusion: Although all compounds did not exert more potency in comparison with doxorubicin, some of them showed remarkable cytotoxicity. The potent derivatives could be introduced as novel lead compounds for development of new anticancer drugs.

scholarly journals CYTOTOXICITY ACTIVITY OF SOME INDIAN MEDICINAL PLANTS

2016 ◽  
Vol 8 (4) ◽  
pp. 86
Author(s):  
Dora Babu Neerugatti ◽  
Ganga Rao Battu ◽  
Raviteja Bandla
Keyword(s):  
Medicinal Plants ◽  
Cell Lines ◽  
Human Cancer ◽  
Bioactive Constituents ◽  
Cytotoxicity Activity ◽  
Human Cancer Cell Lines ◽  
Methanolic Extracts ◽  
Dose Dependent ◽  
New Anticancer Drugs ◽  
Indian Medicinal Plants

Objective: The current study is carried out to evaluate cytotoxicity activity of the methanolic extracts of some medicinal plants (Buchanania axillaris Desr, Tamilnadia ulignosa Retz, Phaseolus semierectus L and Stylosanthes fruticosa Retz).Methods: Cytotoxicity activity was evaluated on human cancer cell lines such as lung cancer (A549) and skin cancer (A431) using MTT assay method.Results: The selected plant extracts showed the dose-dependent cytotoxicity activity on the tested cell lines. The cytotoxicity variations on different cell lines were also observed for tested plants extracts. The cytotoxicity of the extracts was increased as the concentration of them was increased. Among all tested plants extracts Phaseolus semierectus showed the better cytotoxicity activity on tested cell lines.Conclusion: The results of the present study supported the folkloric usage of the studied plants and confirmed that the plant's extracts have the bioactive constituents with cytotoxic properties and their isolation can be useful for developing new anticancer drugs.

scholarly journals Comparative Antiproliferative activity of aerial parts of few Apocynaceae plants in HepG2, HT29 and SK-OV3 Human cancer cell lines

2019 ◽  
Vol 9 (4-s) ◽  
pp. 1195-1202
Author(s):  
Nirmala Devi ◽  
Ajay Kumar Gupta ◽  
Sunil Kumar Prajapati
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Srb Assay ◽  
Human Cancer Cell Lines ◽  
Aerial Parts ◽  
Carissa Carandas ◽  
Ht 29

Aims: Apocynaceae family is the 5th largest medicinal plant family rich in potent secondary metabolites such as Alkaloids, Cardiac glycosides,Terpenoids, irridoid/secoirridoids, flavonoids and Phenolic contents. The present study was aimed to evaluate and compare in-vitroantiproliferative activity of three plants of this family.Methods: Aerial parts of Carissa carandas Linn. (C), Nerium indicum Mill. (N) and Wrightia tinctoria RBr. (W), were collected and dried. Thepowdered drugs were extracted in Ethanol (1), 60% Ethanol (2) and Water (3). Estimation of Phytoconstituents performed using standardmethods. In-vitro cytotoxic activity performed using Sulphorhodamine B (SRB) assay in HepG2, HT29 and SKOV3 human cancer cell lines takingAdriamycin (ADR) as standard. For extracts, GI50 value ≤ 20μg/ml was considered to demonstrate activity.Results: For HepG2 cell line graphs and photomicrographs showed GI50 value as ADR=39.79, C1=2.5, N2=66.3, N3<10 and C2=C3= N1=W1-3>80. Also TGI for C1>80. The extracts, C1, C2, N1, N2, and N3 were found to possess activity against HepG2.These extracts were screened onHT 29 and SKOV3cell lines. The GI50 value observed was<10 for C1, N2, N3 and ADR in HT 29 and <10 for N3 and ADR in SK OV3 cell lines.Thus it was found that aqueous extract of Nerium indicum (N3) and Ethanolic extract of Carissa carandas (C1) were most cytotoxic extractsagainst all three cell lines.Conclusions: our study establishes that Apocynaceae family plants could be an important anticancer lead and could serve as Botanical drug forneoplasia.Keywords: Apocynaceae, SRB Assay, Phytoconstituents, Anticancer drug screening models, Hep G2, HT 29, SK-OV3, HCC.

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.

Nano-SnCl4/SiO2 as a Catalyst for One-Pot Synthesis of Substituted 1H-Pyrazoles as Antifungal and Cytotoxic Agents

2020 ◽  
Vol 17 (6) ◽  
pp. 459-465
Author(s):  
Soghra Khabnadideh ◽  
Zeinab Faghih ◽  
Leila Zamani ◽  
Kamiar Zomorodian ◽  
Bi Bi Fatemeh Mirjalili ◽  
...  
Keyword(s):  
Cell Lines ◽  
Human Cancer ◽  
Antimicrobial Activities ◽  
Cytotoxic Agents ◽  
Cytotoxic Activities ◽  
Pyrazole Derivatives ◽  
One Pot ◽  
Human Cancer Cell Lines ◽  
Cancerous Cell ◽  
Anti Cancer

A simple and efficient method was developed for the synthesis of pyrazole derivatives via a one-pot reaction of 1,3-diketone and substituted hydrazines in the presence of nano-SnCl4/SiO2 as a mild catalyst. A series of some pyrazole derivatives (P1-P11) was synthesized and evaluated as antifungal and anti-cancer agents. Compounds P10 and P11 were demonstrated. The antimicrobial activities of the synthetic compounds showed that compounds P10 and P11 most excellently inhibited the growth of dermatophytes or Aspergillus species, respectively. Therefore, the cytotoxic activities of these compounds on two human cancer cell lines, A549 (lung cancer) and MCF-7 (breast cancer) were further assessed. Hence, results demonstrated that beside antifungal activity, P10 had also desirable cytotoxic effect on investigated cancerous cell lines, even higher than cisplatin.

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 and Antiproliferative Activity of New Cyclodiprenyl Phenols against Select Cancer Cell Lines

Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2323 ◽  
Author(s):  
Bastián Said ◽  
Iván Montenegro ◽  
Manuel Valenzuela ◽  
Yusser Olguín ◽  
Nelson Caro ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Antineoplastic Agent ◽  
Cancer Cell Lines ◽  
Perillyl Alcohol ◽  
Human Cancer Cell Lines ◽  
Ht 29 ◽  
Positive Controls ◽  
Mcf 7

Six new cyclodiprenyl phenols were synthesized by direct coupling of perillyl alcohol and the appropriate phenol. Their structures were established by IR, HRMS and mainly NMR. Three human cancer cell lines—breast (MCF-7), prostate (PC-3) and colon (HT-29)—were used in antiproliferative assays, with daunorubicin and dunnione as positive controls. Results described in the article suggest that dihydroxylated compounds 2–4 and monohydroxylated compound 5 display selectivity against cancer cell lines, cytotoxicity, apoptosis induction, and mitochondrial membrane impairment capacity. Compound 2 was identified as the most effective of the series by displaying against all cancer cell lines a cytotoxicity close to dunnione antineoplastic agent, suggesting that the cyclodiprenyl phenols from perillyl alcohol deserve more extensive investigation of their potential medicinal applications.

scholarly journals Role of ATF5 in the invasive potential of diverse human cancer cell lines

2016 ◽  
Vol 474 (3) ◽  
pp. 509-514 ◽  
Author(s):  
Akihiro Nukuda ◽  
Hiroki Endoh ◽  
Motoaki Yasuda ◽  
Takeomi Mizutani ◽  
Kazushige Kawabata ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Invasive Potential ◽  
Human Cancer Cell Lines

Imidazolium-derived ionic salts induce inhibition of cancerous cell growth through apoptosis

MedChemComm ◽  
2014 ◽  
Vol 5 (9) ◽  
pp. 1404-1409 ◽  
Author(s):  
Sanjay V. Malhotra ◽  
Vineet Kumar ◽  
Christian Velez ◽  
Beatriz Zayas
Keyword(s):  
Ionic Liquids ◽  
Cell Growth ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Ionic Salts ◽  
Cancerous Cell

A study of the effects of imidazolium-based ionic liquids on 60 human cancer cell lines representing diverse histologies has identified four compounds which show potency at a nanomolar dose.

scholarly journals In vitro and In silico Evaluation of Structurally Diverse Benzyl-pyrrolidine-3-ol Analogues as Apoptotic Agents via Caspase Activation

2021 ◽  
Vol 68 (3) ◽  
pp. 667-682
Author(s):  
Tahira Naqvi ◽  
Asif Amin ◽  
Shujat Ali ◽  
Mohsin Y. Lone ◽  
Nadeem Bashir ◽  
...  
Keyword(s):  
Cell Lines ◽  
In Silico ◽  
Caspase 3 ◽  
Human Cancer ◽  
Md Simulations ◽  
Human Cancer Cell Lines ◽  
Lead Compounds ◽  
Model Protein ◽  
The Stability

The activation of caspases is central to apoptotic process in living systems. Defects in apoptosis have been implicated with carcinogenesis. Need to develop smart agents capable of inducing apoptosis in tumor cells is obvious. With this motive, diversity oriented synthesis of 1-benzylpyrrolidin-3-ol analogues was envisaged. The multi component Ugi reaction synthesized library of electronically diverse analogues was explored for cytotoxic propensity towards a panel of human cancer cell lines at 10 μM. The lead compounds exhibit a selective cytotoxicity towards HL-60 cells as compared to cell lines derived from solid tumors. Besides, their milder cytotoxic effect on non-cancerous cell lines reaffirm their selective action towards cancer cells only.The lead molecules were tested for their ability to target caspase-3, as a vital protease triggering apoptosis. The lead compounds were observed to induce apoptosis in HL-60 cells around 10 μM concentration. The lead compounds exhibited various non-covalent supra type interactions with caspase-3 key residues around the active site. The binding ability of lead compounds with caspase-3 was studied via molecular docking and molecular dynamic (MD) simulations. MD simulations indicated the stability of compound-caspase-3 complex throughout the 50 ns simulation run. The stability and bio-availability of the lead compounds under physiological conditions was assessed by their interaction with Bovine Serum Albumin (BSA) as model protein. BSA interactions of lead compounds were studied by various bio-physical methods and further substantiated with in silico MD simulations.

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