A Short-term Bovine Sperm Cell Assay for the Evaluation of the In Vitro Cytotoxicity of Chemicals

1990 ◽  
Vol 17 (3) ◽  
pp. 228-232
Author(s):  
Hasso Seibert ◽  
Ulrich Gosch
Keyword(s):  
Test Procedure ◽  
In Vitro Cytotoxicity ◽  
In Vitro Toxicity ◽  
Cytotoxic Action ◽  
Response Patterns ◽  
Toxic Response ◽  
Modes Of Action ◽  
Bovine Spermatozoa ◽  
New Compounds

A test procedure is described for the use of ejaculated bovine spermatozoa in evaluating the in vitro cytotoxicity of chemicals. Results from experiments with model substances with known modes of action (inhibitors of mitochondrial electron transport, uncouplers of mitochondrial phosphorylation, surfactants, organic solvents) are presented and suggest that specific toxic-response patterns can be defined for the different modes of action. It is concluded that the in vitro toxicity profiles obtained in the assay described can be used for a first qualitative analysis of the cytotoxic action of little studied or new compounds, in addition to a quantitative assessment of their cytotoxic potency.

scholarly journals Synthesis of Gold Nanoparticles by Using Green Machinery: Characterization and In Vitro Toxicity

Nanomaterials ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 808
Author(s):  
Ahmed Al Saqr ◽  
El-Sayed Khafagy ◽  
Ahmed Alalaiwe ◽  
Mohammed F. Aldawsari ◽  
Saad M. Alshahrani ◽  
...  
Keyword(s):  
Gold Nanoparticles ◽  
Average Particle Size ◽  
In Vitro Cytotoxicity ◽  
In Vitro Toxicity ◽  
Cervical Cancer Cell Line ◽  
Average Particle ◽  
Anticancer Activities ◽  
Tem Analysis ◽  
Benincasa Hispida

Green synthesis of gold nanoparticles (GNPs) with plant extracts has gained considerable interest in the field of biomedicine. Recently, the bioreduction nature of herbal extracts has helped to synthesize spherical GNPs of different potential from gold salt. In this study, a fast ecofriendly method was adopted for the synthesis of GNPs using fresh peel (aqueous) extracts of Benincasa hispida, which acted as reducing and stabilizing agents. The biosynthesized GNPs were characterized by UV–VIS and Fourier transform infrared spectroscopy, transmission electron microscopy (TEM), and dynamic light scattering. In addition, the in vitro antibacterial and anticancer activities of synthesized GNPs were investigated. The formation of gold nanoparticles was confirmed by the existence of a sharp absorption peak at 520 nm, corresponding to the surface plasmon resonance (SPR) band of the GNPs. TEM analysis revealed that the prepared GNPs were spherical in shape and had an average particle size of 22.18 ± 2 nm. Most importantly, the synthesized GNPs exhibited considerable antibacterial activity against different Gram-positive and Gram-negative bacteria. Furthermore, the biosynthesized GNPs exerted remarkable in vitro cytotoxicity against human cervical cancer cell line, while sparing normal human primary osteoblast cells. Such cytotoxic effect was attributed to the increased production of reactive oxygen species (ROS) that contributed to the damage of HeLa cells. Collectively, peel extracts of B. hispida can be efficiently used for the synthesis of GNPs, which can be adopted as a natural source of antimicrobial and anticancer agent.

scholarly journals Comparative Study of Cigarette Smoke Cytotoxicity Using Two In Vitro Assay Systems

2014 ◽  
Vol 26 (3) ◽  
pp. 98-108
Author(s):  
Toshiro Fukushima ◽  
Hitomi Tanaka ◽  
Takeshi Yamamoto
Keyword(s):  
Cigarette Smoke ◽  
Rank Order ◽  
In Vitro Cytotoxicity ◽  
Water Soluble ◽  
Cytotoxic Agents ◽  
Main Stream ◽  
Total Particulate Matter ◽  
Vitro Assay ◽  
Modes Of Action

SUMMARYThe aim of this study was to compare the results obtained from two in vitro cytotoxicity assays that depend upon different mechanisms/modes of action. The Neutral Red Uptake (NRU) assay is based on endocytotic activity whereas the Water Soluble Tetrazolium Salts (WST-1) assay is based on mitochondrial dehydrogenase activity. Both were investigated in light of their wide use and documented validation. The total particulate matter (TPM) and gas vapor phase (GVP) of main stream smoke derived from Kentucky reference cigarettes 3R4F and 10 test cigarettes made of 100% flue-cured or 100% Burley tobacco were individually applied to the two assays using CHO-K1 cells. In addition, cigarette smoke constituents and known cytotoxic agents, documented to affect specific endpoints, were evaluated within both assays. Although the NRU assay was primarily more sensitive than the WST-1 assay, both assays provided comparable results in terms of the rank order for the cytotoxicity of cigarette smoke samples. In addressing the cytotoxicity of constituents in cigarette smoke, acrolein, hydroquinone and catechol gave clear dose-related decreases in cell viability (an end point common in both assays). Moreover, enzyme inhibitors of the mitochondrial respiratory chain and chemicals causing membrane disruption also showed similar responses regardless of the specific endpoint addressed within the cytotoxicity assay. In conclusion, results from the NRU and WST-1 assay are comparable therefore indicating results were independent of the different assay detection mechanisms/modes of action. [Beitr. Tabakforsch. Int. 26 (2014) 98-108]

scholarly journals In Vitro Toxicity Study of a Porous Iron(III) Metal‒Organic Framework

Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1211 ◽  
Author(s):  
Gongsen Chen ◽  
Xin Leng ◽  
Juyuan Luo ◽  
Longtai You ◽  
Changhai Qu ◽  
...  
Keyword(s):  
Metal Organic Framework ◽  
Drug Carrier ◽  
In Vitro Cytotoxicity ◽  
In Vitro Toxicity ◽  
Porous Iron ◽  
Dapi Staining ◽  
Toxicological Assessment ◽  
Metal Organic ◽  
Organic Framework

A MIL series metal‒organic framework (MOF), MIL-100(Fe), was successfully synthesized at the nanoscale and fully characterized by TEM, TGA, XRD, FTIR, DLS, and BET. A toxicological assessment was performed using two different cell lines: human normal liver cells (HL-7702) and hepatocellular carcinoma (HepG2). In vitro cytotoxicity of MIL-100(Fe) was evaluated by the MTT assay, LDH releasing rate assay, DAPI staining, and annexin V/PI double staining assay. The safe dose of MIL-100(Fe) was 80 μg/mL. It exhibited good biocompatibility, low cytotoxicity, and high cell survival rate (HL-7702 cells’ viability >85.97%, HepG2 cells’ viability >91.20%). Therefore, MIL-100(Fe) has a potential application as a drug carrier.

Protein Precipitation In Vitro as a Measure of Chemical-induced Cytotoxicity: An EDIT Sub-programme

2001 ◽  
Vol 29 (3) ◽  
pp. 309-324
Author(s):  
Apolonia Novillo ◽  
Barbro Ekwall ◽  
Argelia Castaño
Keyword(s):  
Cell Lines ◽  
Human Cell ◽  
Exposure Period ◽  
Negative Control ◽  
In Vitro Cytotoxicity ◽  
Protein Precipitation ◽  
In Vitro Toxicity ◽  
Human Cell Lines ◽  
Response Curves

As a priority area of the Evaluation-Guided Development of In Vitro Toxicity and Toxicokinetic Tests (EDIT) programme, an in vitro protein precipitation (PP) assay was used on the 50 reference chemicals of the Multicentre Evaluation of In Vitro Cytotoxicity (MEIC) project, to confirm and extend the MEIC results. Dose–response curves were generated for only 30 of the chemicals, and the concentrations causing 10% (EC10) and 50% (EC50) protein precipitation versus the positive control were chosen as endpoints. The number of chemicals with a positive response increased to 46 when a new endpoint, the minimum effect concentration (MEC) that induces protein precipitation with respect to the negative control, was used. When the results were correlated with in vitro cytotoxicity in human cell lines, a similarly good correlation was found between the various endpoints of the PP assay at 5 hours and the 24-hour IC50 average cytotoxicity in human cell lines, even though the number of chemicals included in the correlation was larger for the MEC. Using the prediction error, the endpoint that gave the best correlation between the PP assay and human cell cytotoxicity was once more found to be the 5-hour MEC, and this was chosen for the PP assay. The sensitivity of the PP assay is lower than that of the in vitro cell-line cytotoxicity assay, possibly due to its shorter exposure period and because precipitation is the ultimate event in the sequence of a protein disturbance. It is expected that earlier denaturation steps would give better sensitivity. However, this simple, inexpensive and rapid assay could be useful in the early stages of testing chemicals.

scholarly journals Specific 12β-Hydroxylation of Cinobufagin by Filamentous Fungi

2004 ◽  
Vol 70 (6) ◽  
pp. 3521-3527 ◽  
Author(s):  
Min Ye ◽  
Guiqin Qu ◽  
Hongzhu Guo ◽  
Dean Guo
Keyword(s):  
Microbial Transformation ◽  
Reversed Phase ◽  
In Vitro Models ◽  
In Vitro Cytotoxicity ◽  
New Drugs ◽  
Hydroxyl Group ◽  
Cytotoxic Activities ◽  
Phase Liquid ◽  
New Compounds

ABSTRACT Biotransformation of natural products has great potential for producing new drugs and could provide in vitro models of mammalian metabolism. Microbial transformation of the cytotoxic steroid cinobufagin was investigated. Cinobufagin could be specifically hydroxylated at the 12β-position by the fungus Alternaria alternata. Six products from a scaled-up fermentation were obtained by silica gel column chromatography and reversed-phase liquid chromatography and were identified as 12β-hydroxyl cinobufagin, 12β-hydroxyl desacetylcinobufagin, 3-oxo-12β-hydroxyl cinobufagin, 3-oxo-12β-hydroxyl desacetylcinobufagin, 12-oxo-cinobufagin, and 3-oxo-12α-hydroxyl cinobufagin. The last five products are new compounds. 12β-Hydroxylation of cinobufagin by A. alternata is a fast catalytic reaction and was complete within 8 h of growth with the substrate. This reaction was followed by dehydrogenation of the 3-hydroxyl group and then deacetylation at C-16. Hydroxylation at C-12β also was the first step in the metabolism of cinobufagin by a variety of fungal strains. In vitro cytotoxicity assays suggest that 12β-hydroxyl cinobufagin and 3-oxo-12α-hydroxyl cinobufagin exhibit somewhat decreased but still significant cytotoxic activities. The 12β-hydroxylated bufadienolides produced by microbial transformation are difficult to obtain by chemical synthesis.

scholarly journals Syntheses and PDT activity of new mono- and di-conjugated derivatives of chlorin e6

2017 ◽  
Vol 21 (04-06) ◽  
pp. 354-363 ◽  
Author(s):  
Hui Chen ◽  
Stewart W. Humble ◽  
R. G. Waruna Jinadasa ◽  
Zehua Zhou ◽  
Alex L. Nguyen ◽  
...  
Keyword(s):  
Amino Acid ◽  
In Vitro Cytotoxicity ◽  
Chlorin E6 ◽  
New Compounds ◽  
Derivatives Of

Syntheses of three new chlorin e6 conjugates for PDT of tumors are reported. One of the new compounds 17 is conjugated with lysine at the 131-position, but the others are mono-conjugated 14 or diconjugated 15 with the non-amino acid species ethanolamine. Cellular experiments with the three new compounds and previously synthesized non-amino acid 152-conjugates (7–10), 131-monoconjugates 14, 16, and a 131,152-diconjugate 12 are reported. In vitro cytotoxicity experiments show that the 131-conjugates are more toxic than the 152-conjugates, and the most toxic derivative (dark- and photo-toxicity) is the 131-ethylenediamine conjugate 11. The most useful PDT photosentitizers appear to be the ethanolamine derivatives, conjugated at the 152- and the 131,152-positions; these show high phototoxicity but relatively low dark toxicity compared with 11, and also the highest dark/photo cytotoxicity ratios.

scholarly journals Cytotoxicity of Taxol in Combination with Vincristine and Vinblastine Against A375 Cell Line

2021 ◽  
Vol In Press (In Press) ◽  
Author(s):  
Mohammad Zandi
Keyword(s):  
Side Effects ◽  
Therapeutic Option ◽  
Inhibitory Effect ◽  
In Vitro Cytotoxicity ◽  
In Vitro Toxicity ◽  
Human Malignant Melanoma ◽  
Promising Strategy ◽  
A375 Cell Line ◽  
A375 Cells

Background: Annually, various types of cancer cause thousands of deaths globally, and identifying an appropriate therapeutic option for these disorders is of crucial importance. Side effects of anticancer drugs can be reduced through the promising strategy of combination therapy. Objectives: The present paper has investigated the in vitro cytotoxicity of Taxol, carboplatin, vinblastine, and vincristine alone and in combination against human malignant melanoma A375 cells and non-cancerous fibroblast HU2 cells to examine the possible side effects of the drugs. Methods: The cells were subjected to the examined compounds for 48 h, and the MTT test was conducted to evaluate the cytotoxicity. Results: The results indicated that the most significant effect was related to 120 μg/mL vincristine and 7.5 μg/mL Taxol+ vincristine treatments, with the survival amounts of 24 ± 0.6 and 28 ± 0%, respectively. In addition, the best 50% inhibitory effect was found to be related to Taxol + vincristine, vinblastine, and Taxol+ vinblastine treatments at the concentrations of 0.04, 2.2, and 3.4 μg/mL, respectively. Conclusions: According to the findings of in vitro toxicity, the evaluated complexes are not cytotoxic against human fibroblast HU2 cells. Also, the most significant effect on A375 cells was associated with vincristine treatment. No synergistic reaction was recorded among the different combinations of drugs based on the calculated CI values.

scholarly journals Synthesis and Cytotoxicity of Thieno[2,3-b]Pyridine Derivatives Toward Sensitive and Multidrug-Resistant Leukemia Cells

2021 ◽  
Vol 68 (2) ◽  
pp. 458-465
Author(s):  
Salah A. Al-Trawneh ◽  
Amer H. Tarawneh ◽  
Anastassiya V. Gadetskaya ◽  
Ean-Jeong Seo ◽  
Mohammad R. Al-Ta’ani ◽  
...  
Keyword(s):  
Multidrug Resistant ◽  
In Vitro Cytotoxicity ◽  
Leukemia Cells ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Anti Cancer ◽  
Ic50 Values ◽  
New Compounds ◽  
Potential Use

A new series of substituted ethyl 7-cyclopropyl-2-(2-aryloxo)-3-nitro-4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylates 3a–e were prepared by utilizing ethyl 2-chloro-7-cyclopropyl-3-nitro-4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylate (1) and replacing of the 2-chlorine with anions obtained from phenol (2a), salicylaldehyde derivatives 2b–d or thiophenol (2e), leading to the respective ethyl 7-cyclopropyl-2-(2-aryloxo)-3-nitro-4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylates 3a–e. The new compounds were evaluated for their in vitro cytotoxicity towards sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 leukemia cells. The screening revealed that compounds 3a, 3b, and 3e inhibited the growth of both cell lines. Compound 3b, with a phenol moiety, exhibited the highest growth inhibitory activity against CEM/ADR5000 and CCRF-CEM cells with IC50 values 4.486 ± 0.286 and 2.580 ± 0.550 μM, respectively. Collectively, the presented results demonstrate that the synthesized thieno[2,3-b]pyridines warrant further exploration for potential use as anti-cancer agents.

scholarly journals Synthesis of Novel Benzamide- piperazine-sulfonamide Hybrids as Potential Anticancer Agents

2019 ◽  
Vol 92 (3) ◽  
pp. 393-402
Author(s):  
B. Ramalingeswara Rao ◽  
Mohana Rao Katiki ◽  
Dileep Kommula ◽  
SaiShyam Narayanan ◽  
Ruby John Anto ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Sensitive Cell Line ◽  
Human Cancer Cell Lines ◽  
Ic50 Values ◽  
Different Origins ◽  
New Compounds ◽  
A549 Lung

The synthesis of a series of substituted hippuric acid (2-benzamidoacetic acid) derivatives containing arylsulfonylpiperazine nucleus (3a–j, 4a–j) is described. The compounds were synthesized by coupling hippuric/4-fluorohippuric acid with various arylsulfonylpiperazines using N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (EDCI). The structures of all the new compounds were confirmed by IR, NMR and MS spectral data. All the synthesized compounds have been evaluated for their in vitro cytotoxicity towards five human cancer cell lines of different origins viz. HeLa (Cervical), A549 (Lung), A375 (Skin), MD-AMB-231(Breast) and T98G (brain) and their IC50 values were determined. Among the compounds tested, 3b, 3d, 3g, 4c and 4e displayed significant cytotoxic activity (IC50 = 24.2–38.2 µM). T98G was the most sensitive cell line towards the compounds studied followed by HeLa, A375, A549 and MD-AMB-231.

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