Cytotoxic Effect of Lactobacillus gasseri Concentrated Filtrate on some Tumor Cell Lines in vitro

EucalyptusL. is traditionally used for many medicinal purposes. In particular, someEucalyptusspecies have currently shown cytotoxic properties. Local Brazilian communities have used leaves ofE. benthamiias a herbal remedy for various diseases, including cancer. Considering the lack of available data for supporting this cytotoxic effect, the goal of this paper was to study thein vitrocytotoxic potential of the essential oils from young and adult leaves ofE. benthamiiand some related terpenes (α-pinene, terpinen-4-ol, andγ-terpinene) on Jurkat, J774A.1 and HeLa cells lines. Regarding the cytotoxic activity based on MTT assay, the essential oils showed improved results thanα-pinene andγ-terpinene, particularly for Jurkat and HeLa cell lines. Terpinen-4-ol revealed a cytotoxic effect against Jurkat cells similar to that observed for volatile oils. The results of LDH activity indicated that cytotoxic activity of samples against Jurkat cells probably involved cell death by apoptosis. The decrease of cell DNA content was demonstrated due to inhibition of Jurkat cells proliferation by samples as a result of cytotoxicity. In general, the essential oils from young and adult leaves ofE. benthamiipresented cytotoxicity against the investigated tumor cell lines which confirms their antitumor potential.

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A novel microfluidic liposomal formulation for the delivery of the SN-38 camptothecin: characterization and in vitro assessment of its cytotoxic effect on two tumor cell lines

International Journal of Nanomedicine ◽

10.2147/ijn.s166219 ◽

2018 ◽

Vol Volume 13 ◽

pp. 5301-5320 ◽

Cited By ~ 6

Author(s):

Ana Casadó ◽

M. Lluïsa Sagristá ◽

Margarita Mora Giménez

Keyword(s):

Tumor Cell ◽

Cell Lines ◽

Cytotoxic Effect ◽

Liposomal Formulation ◽

Tumor Cell Lines ◽

In Vitro Assessment

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A Lipoaminopeptaibol Secreted by Alkalophilic Fungus Emericellopsis alkalina Demonstrates a Strong Cytotoxic Effect against Tumor Cell Lines

Proceedings ◽

10.3390/proceedings2019022004 ◽

2019 ◽

Vol 22 (1) ◽

pp. 4

Author(s):

Eugene Rogozhin ◽

Vera Sadykova

Keyword(s):

Tumor Cell ◽

Cytotoxic Activity ◽

Cell Lines ◽

Cytotoxic Effect ◽

Antimicrobial Effect ◽

Antitumor Antibiotic ◽

Tumor Cell Lines ◽

Normal Cells ◽

Hela Cell Lines

Soil fungi are known to produce and secrete antibiotics with a strong antimicrobial effect towards eukaryotic organisms. In many occasions, these compounds belong to peptides that are products of non-ribosomal biosynthesis and are called peptaibols. Many peptaibols are cytotoxic and some of them suppress tumor cell lines much better than normal cells by inducing calcium-mediated apoptosis. The main antimicrobial lipoaminopeptaibol—emericellipsin A—isolated from the fungus Emericellopsis alkalina strain VKPM F-1428, which demonstrates promising antifungal activity against different fungal taxons,has been found to exhibit selective cytotoxic activity against HepG2 and Hela cell lines (EC50 2.8 and 0.5 μM, respectively) in MTT assays in vitro. This result corresponds to the standard antitumor antibiotic doxorubicin, which has an EC50 value of 440 nM. In a fibroblast toxicity test, emericellipsin A exhibited less cytotoxic activity than doxorubicin (EC50 14 and 0.34 μM, respectively). Therefore, it is less toxic to normal cells than doxirubicin (~40 times), but it yields a more potent cytotoxic effect on tumor cell lines. That is why emericellipsin A can be considered for future more detailed investigations to be an effective antitumor substance.

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In Vitro Activity of Organochalcogen Compounds: I. Cytotoxic Effect of 4-(1,2,3-Thiadiazol-4-yl)furans Against K562 and HeLa Tumor Cell Lines

Russian Journal of General Chemistry ◽

10.1134/s1070363220110328 ◽

2020 ◽

Vol 90 (11) ◽

pp. 2208-2213

Author(s):

Yu. O. Remizov ◽

A. A Kornev ◽

L. M. Pevzner ◽

M. L. Petrov ◽

V. M. Boitsov ◽

...

Keyword(s):

Tumor Cell ◽

Cell Lines ◽

Cytotoxic Effect ◽

Vitro Activity ◽

Tumor Cell Lines ◽

In Vitro Activity

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In Vitro Activity of Organochalcogen Compounds: II. Cytotoxic Effect of 2-Aminobenzo[b]thiophenes Against K562 and HeLa Tumor Cell Lines

Russian Journal of General Chemistry ◽

10.1134/s107036322011033x ◽

2020 ◽

Vol 90 (11) ◽

pp. 2214-2218

Author(s):

E. A. Popova ◽

A. A. Kornev ◽

S. V. Shmakov ◽

G. D. Nepochatyi ◽

O. A. Kotyunina ◽

...

Keyword(s):

Tumor Cell ◽

Cell Lines ◽

Cytotoxic Effect ◽

Vitro Activity ◽

Tumor Cell Lines ◽

In Vitro Activity

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In Vitro Activity of Organochalcogen Compounds: III. Cytotoxic Effect of 4-(2-Hydroxyaryl)-1,2,3-thiadiazoles Against K562 and Hela Tumor Cell Lines

Russian Journal of General Chemistry ◽

10.1134/s1070363220120270 ◽

2020 ◽

Vol 90 (12) ◽

pp. 2400-2404

Author(s):

E. A. Popova ◽

A. A. Kornev ◽

V. V. Bessonov ◽

D. A. Androsov ◽

M. L. Petrov ◽

...

Keyword(s):

Tumor Cell ◽

Cell Lines ◽

Cytotoxic Effect ◽

Vitro Activity ◽

Tumor Cell Lines ◽

In Vitro Activity

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Synthesis and Cytotoxicity of New Mannich Bases of 6-[3-(3,4,5-Trimetoxyphenyl)-2- propenoyl]-2(3H)-Benzoxazolone

Letters in Drug Design & Discovery ◽

10.2174/1570180816666190730164952 ◽

2020 ◽

Vol 17 (4) ◽

pp. 512-517

Author(s):

Ognyan Ivanov Petrov ◽

Yordanka Borisova Ivanova ◽

Mariana Stefanova Gerova ◽

Georgi Tsvetanov Momekov

Keyword(s):

Tumor Cell ◽

Cell Lines ◽

Biological Activities ◽

Human Tumor ◽

Mannich Bases ◽

In Vitro Cytotoxicity ◽

Tumor Cell Lines ◽

Human Tumor Cell ◽

Human Tumor Cell Lines

Background: Chemotherapy is one of the mainstays of cancer treatment, despite the serious side effects of the clinically available anticancer drugs. In recent years increasing attention has been directed towards novel agents with improved efficacy and selectivity. Compounds with chalcone backbone have been reported to possess various biological activities such as anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, etc. It was reported that aminomethylation of hydroxy chalcones to the corresponding Mannich bases increased their cytotoxicity. In this context, our interest has been focused on the design and synthesis of the so-called multi-target molecules, containing two or more pharmacophore fragments. Methods: A series of Mannich bases were synthesized by the reaction between 6-[3-(3,4,5- trimethoxyphenyl)-2-propenoyl]-2(3Н)-benzoxazolone, formaldehyde, and a secondary amine. The structures of the compounds were confirmed by elemental analysis, IR and NMR spectra. The new Mannich bases were evaluated for their in vitro cytotoxicity against a panel of human tumor cell lines, including BV-173, SKW-3, K-562, HL-60, HD-MY-Z and MDA-MB-231. The effects of selected compounds on the cellular levels of glutathione (GSH) were determined. Results: The new compounds 4a-e exhibited concentration-dependent cytotoxic effects at micromolar concentrations in MTT-dye reduction assay against a panel of human tumor cell lines, similar to those of starting chalcone 3. The tested agents led to concentration - dependent depletion of cellular GSH levels, whereby the effects of the chalcone prototype 3 and its Mannich base-derivatives were comparable. Conclusion: The highest chemosensitivity to the tested compounds was observed in BV- 173followed by SKW-3 and HL-60 cell lines.

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Pharmacoinformatics and Preclinical Studies of NSC765690 and NSC765599, Potential STAT3/CDK2/4/6 Inhibitors with Antitumor Activities against NCI60 Human Tumor Cell Lines

Biomedicines ◽

10.3390/biomedicines9010092 ◽

2021 ◽

Vol 9 (1) ◽

pp. 92

Author(s):

Bashir Lawal ◽

Yen-Lin Liu ◽

Ntlotlang Mokgautsi ◽

Harshita Khedkar ◽

Maryam Rachmawati Sumitra ◽

...

Keyword(s):

Tumor Cell ◽

Cell Lines ◽

Cancer Cell ◽

Human Tumor ◽

Cancer Cell Lines ◽

Tumor Cell Lines ◽

Human Tumor Cell ◽

Human Tumor Cell Lines ◽

Anti Cancer

Signal transducer and activator of transcription 3 (STAT3) is a transcriptional regulator of a number of biological processes including cell differentiation, proliferation, survival, and angiogenesis, while cyclin-dependent kinases (CDKs) are a critical regulator of cell cycle progression. These proteins appear to play central roles in angiogenesis and cell survival and are widely implicated in tumor progression. In this study, we used the well-characterized US National Cancer Institute 60 (NCI60) human tumor cell lines to screen the in vitro anti-cancer activities of our novel small molecule derivatives (NSC765690 and NSC765599) of salicylanilide. Furthermore, we used the DTP-COMPARE algorithm and in silico drug target prediction to identify the potential molecular targets, and finally, we used molecular docking to assess the interaction between the compounds and prominent potential targets. We found that NSC765690 and NSC765599 exhibited an anti-proliferative effect against the 60 panels of NCI human cancer cell lines, and dose-dependent cytotoxic preference for NSCLC, melanoma, renal, and breast cancer cell lines. Protein–ligand interactions studies revealed that NSC765690 and NSC765599 were favored ligands for STAT3/CDK2/4/6. Moreover, cyclization of the salicylanilide core scaffold of NSC765690 mediated its higher anti-cancer activities and had greater potential to interact with STAT3/CDK2/4/6 than did NSC765599 with an open-ring structure. NSC765690 and NSC765599 met the required safety and criteria of a good drug candidate, and are thus worthy of further in-vitro and in-vivo investigations in tumor-bearing mice to assess their full therapeutic efficacy.

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