In vitro cytotoxicity and biological activities of Genipa americana (Rubiaceae) ethanolic extracts

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.

Download Full-text

In vitro cytotoxicity of Aspilia pluriseta Schweinf. extract fractions

BMC Research Notes ◽

10.1186/s13104-021-05472-4 ◽

2021 ◽

Vol 14 (1) ◽

Author(s):

Sospeter N. Njeru ◽

Jackson M. Muema

Keyword(s):

Biological Activities ◽

Vero Cells ◽

In Vitro Cytotoxicity ◽

Root Extract ◽

Lack Of Information ◽

Information Gap ◽

Diphenyltetrazolium Bromide ◽

Potential Use

Abstract Objectives We and others have shown that Aspilia pluriseta is associated with various biological activities. However, there is a lack of information on its cytotoxicity. This has created an information gap about the safety of A. pluriseta extracts. As an extension to our recent publication on the antimicrobial activity and the phytochemical characterization of A. pluriseta root extracts, here we report on cytotoxicity of tested solvent fractions. We evaluated the potential cytotoxicity of these root extract fractions on Vero cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results We show that all solvent extract fractions (except methanolic solvent fractions) had cytotoxic concentration values that killed 50% of the Vero cells (CC50) greater than 20 µg/mL and selectivity index (SI) greater than 1.0. Taken together, we demonstrate that, A. pluriseta extract fractions’ earlier reported bioactivities are within the acceptable cytotoxicity and selective index limits. This finding scientifically validates the potential use of A. pluriseta in the discovery of safe therapeutics agents.

Download Full-text

Leishmanicidal and Cytotoxic Activities of Extracts and Naturally-Occurring Compounds from two Lauraceae Species

Natural Product Communications ◽

10.1177/1934578x1100600218 ◽

2011 ◽

Vol 6 (2) ◽

pp. 1934578X1100600

Author(s):

Jeysson Sánchez-Suárez ◽

Ericsson Coy-Barrera ◽

Luis Enrique Cuca ◽

Gabriela Delgado

Keyword(s):

Leishmania Species ◽

In Vitro Cytotoxicity ◽

Cytotoxic Activities ◽

Naturally Occurring ◽

Ethanolic Extracts ◽

Leishmania Panamensis ◽

J774 Cells ◽

Different Levels ◽

Leishmania Parasites

The in vitro leishmanicidal effects of ethanolic extracts and fifteen naturally-occurring compounds (five lignans, eight neolignans, a diterpene and a dihydrochalcone), obtained from Pleurothyrium cinereum and Ocotea macrophylla, were evaluated on promastigotes of Leishmania panamensis and L. braziliensis. In addition, in order to determine the selective action on Leishmania species as a safety principle, in vitro cytotoxicity on J774 cells was also evaluated for test compounds and extracts. One extract and seven compounds showed activity against Leishmania parasites at different levels. Dihydroflavokawin B (8) was found to be the most potent antileishmanial compound on both parasites, whilst (+)-otobaphenol (14), was found to be the most selective compound on L. panamensis.

Download Full-text

Antibacterial activity and in vitro cytotoxicity evaluation of alginate-AgNP fibers

Textile Research Journal ◽

10.1177/0040517516652350 ◽

2016 ◽

Vol 87 (11) ◽

pp. 1377-1386 ◽

Cited By ~ 3

Author(s):

Xihui Zhao ◽

Qun Li ◽

Xiaowen Li ◽

Yanzhi Xia ◽

Bing Wang ◽

...

Keyword(s):

Antibacterial Activity ◽

Treatment Time ◽

Biological Activities ◽

In Vitro Cytotoxicity ◽

Cell Counting ◽

Logarithmic Phase ◽

E Coli ◽

Alginate Fibers ◽

And Staphylococcus Aureus

Biopolymer nanocomposites containing metal nanoparticles have attracted much attention due to their excellent properties and broad applications. In this work, alginate fibers embedded with silver nanoparticles (AgNPs) were prepared. The as-obtained alginate-AgNP fibers exhibited antibacterial activity against both Gram microorganisms of model microbes Escherichia coli (Gram-negative) and Staphylococcus aureus (Gram-positive). A growth kinetic study with S. aureus and E. coli displayed the inhibition of bacterial growth at the logarithmic phase. The cytotoxic effect of the fibers in human cervical cancer (HeLa) cells was assessed by cell counting kit-8 (CCK-8) assay and flow cytometry. The as-prepared alginate-AgNP fibers, particularly with high amount and long treatment time, showed high cell-killing efficiency. These findings emphasize that such alginate-AgNP fibers with multifaceted biological activities are a promising material for applications in the textile or biomedical fields.

Download Full-text

In Vitro Cytotoxicity and Antibacterial Evaluation of Aqueous, Methanolic and Ethanolic Extracts of Anastatica hierochuntica against Pathogenic Bacteria

International Journal of Current Research in Biosciences and Plant Biology ◽

10.20546/ijcrbp.2016.306.002 ◽

2016 ◽

Vol 3 (6) ◽

pp. 14-22 ◽

Cited By ~ 2

Author(s):

Sanad M. Al Sobeai

Keyword(s):

Pathogenic Bacteria ◽

In Vitro Cytotoxicity ◽

Ethanolic Extracts ◽

Antibacterial Evaluation

Download Full-text

Cytotoxic and Genotoxic Activities of Alkaloids from the Bulbs of Griffinia gardneriana and Habranthus itaobinus (Amaryllidaceae)

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520619666190118122523 ◽

2019 ◽

Vol 19 (5) ◽

pp. 707-717 ◽

Cited By ~ 1

Author(s):

Eduardo R. Cole ◽

Jean P. de Andrade ◽

João F. Allochio Filho ◽

Elisângela F. P. Schmitt ◽

Anderson Alves-Araújo ◽

...

Keyword(s):

Cell Lines ◽

Caspase 3 ◽

Biological Activities ◽

Docking Studies ◽

In Vitro Cytotoxicity ◽

Cytotoxic Activities ◽

Isolation And Identification ◽

Wide Range

Background: Amaryllidaceae plants are known to be a great source of alkaloids, which are considered an extensive group of compounds encompassing a wide range of biological activities. The remarkable cytotoxic activities observed in most of the Amaryllidaceae alkaloids derivatives have prompt the chemical and biological investigations in unexplored species from Brazil. Objective: To evaluate the cytotoxic and genotoxic properties of alkaloids of Griffinia gardneriana and Habranthus itaobinus bulbs and study the role of caspase-3 as a molecular apoptosis mediator. Methods: Methanolic crude extracts of Griffinia gardneriana and Habranthus itaobinus bulbs were submitted to acid-base extraction to obtain alkaloid-enriched fractions. The obtained fractions were fractionated using chromatographic techniques leading to isolation and identification of some alkaloids accomplished via HPLC and 1H-NMR, respectively. Molecular docking studies assessed the amount of free binding energy between the isolated alkaloids with the caspase-3 protein and also calculated the theoretical value of Ki. Studies have also been developed to evaluate in vitro cytotoxicity and genotoxicity in such alkaloids and apoptosis activation via the caspase pathway using both tumor and normal cell lines. Results: Seven alkaloids were isolated and identified. Among these, 11-hydroxyvittatine and 2-α-7- dimethoxyhomolycorine were not cytotoxic, whereas tazettine, trisphaeridine, and sanguinine only showed activity against the fibroblast lineage. Lycorine and pretazettine were 10 to 30 folds more cytotoxic than the other alkaloids, including cancerous lines, and were genotoxic and capable of promoting apoptosis via the caspase-3 pathway. This result supports data obtained in docking studies wherein these two compounds exhibited the highest free energy values. Conclusion: The cytotoxicity assay revealed that, among the seven alkaloids isolated, only lycorine and pretazettine were active against different cell lines, exhibiting concentration- and time-dependent cytotoxic actions alongside genotoxic action and the ability to induce apoptosis by caspase-3, a result consistent with those obtained in docking studies.

Download Full-text

Phytochemical Profile, Antioxidant Activity, and Cytotoxicity Assessment of Tagetes erecta L. Flowers

Molecules ◽

10.3390/molecules26051201 ◽

2021 ◽

Vol 26 (5) ◽

pp. 1201

Author(s):

Ana Flavia Burlec ◽

Łukasz Pecio ◽

Solomiia Kozachok ◽

Cornelia Mircea ◽

Andreia Corciovă ◽

...

Keyword(s):

Biological Activities ◽

In Vitro Cytotoxicity ◽

In Vitro Assays ◽

Tagetes Erecta ◽

Phytochemical Analysis ◽

Total Extract ◽

Tagetes Erecta L ◽

Cytotoxicity Assessment

Tagetes erecta L. is a popular ornamental plant of the Asteraceae family, which is widely cultivated not only for its decorative use, but also for the extraction of lutein. Besides carotenoid representatives, which have been extensively studied, other important classes of secondary metabolites present in the plant, such as polyphenols, could exhibit important biological activities. The phytochemical analysis of a methanolic extract obtained from T. erecta inflorescences was achieved using liquid chromatography–mass spectrometry (LC-MS) techniques. The extract was further subjected to a multistep purification process, which allowed the separation of different fractions. The total extract and its fractions contain several polyphenolic compounds, such as hydroxybenzoic and hydroxycinnamic acid derivatives, flavonols (especially quercetagetin glycosides), and several aglycons (e.g., quercetin, patuletin). One of the fractions, containing mostly quercetagitrin, was subjected to two different antioxidant assays (metal chelating activity and lipoxygenase inhibition) and to in vitro cytotoxicity assessment. Generally, the biological assays showed promising results for the investigated fraction compared to the initial extract. Given the encouraging outcome of the in vitro assays, further purification and structural analysis of compounds from T. erecta extracts, as well as further in vivo investigations are justified.

Download Full-text

Evaluation of Antiproliferative Palladium(II) Complexes of Synthetic Bisdemethoxycurcumin towards In Vitro Cytotoxicity and Molecular Docking on DNA Sequence

Molecules ◽

10.3390/molecules26144369 ◽

2021 ◽

Vol 26 (14) ◽

pp. 4369

Author(s):

Natalia Miklášová ◽

Peter Herich ◽

Juan Carlos Dávila-Becerril ◽

Joaquín Barroso-Flores ◽

Eva Fischer-Fodor ◽

...

Keyword(s):

Biological Activity ◽

Colorectal Carcinoma ◽

Cell Lines ◽

Biological Activities ◽

Human Tumor ◽

Large Family ◽

In Vitro Cytotoxicity ◽

Breast Adenocarcinoma ◽

Human Colorectal Carcinoma

Metallodrugs form a large family of therapeutic agents against cancer, among which is cisplatin, a paradigmatic member. Therapeutic resistance and undesired side effects to Pt(II) related drugs, prompts research on different metal–ligand combinations with potentially enhanced biological activity. We present the synthesis and biological tests of novel palladium(II) complexes containing bisdemethoxycurcumin (BDMC) 1 and 2. Complexes were fully characterized and their structures were determined by X-ray diffraction. Their biological activity was assessed for several selected human tumor cell lines: Jurkat (human leukaemic T-cell lymphoma), HCT-116 (human colorectal carcinoma), HeLa (human cervix epitheloid carcinoma), MCF-7 (human breast adenocarcinoma), MDA-MB-231 (human mammary gland adenocarcinoma), A549 (human alveolar adenocarcinoma), Caco-2 (human colorectal carcinoma), and for non-cancerous 3T3 cells (murine fibroblasts). The cytotoxicity of 1 is comparable to that of cisplatin, and superior to that of 2 in all cell lines. It is a correlation between IC50 values of 1 and 2 in the eight studied cell types, promising a potential use as anti-proliferative drugs. Moreover, for Jurkat cell line, complexes 1 and 2, show an enhanced activity. DFT and docking calculations on the NF-κB protein, Human Serum Albumin (HSA), and DNA were performed for 1 and 2 to correlate with their biological activities.

Download Full-text

Synthesis and biological evaluation of 4-aminoantipyrine analogues

Medicinal Chemistry ◽

10.2174/1573406416666201106105303 ◽

2020 ◽

Vol 16 ◽

Author(s):

Houwei Ren ◽

Premnath Dhanaraj ◽

Israel V M V Enoch ◽

Mosae Selvakumar Paulraj ◽

Indiraleka M

Keyword(s):

Cervical Cancer ◽

Dna Cleavage ◽

Anticonvulsant Activity ◽

Biological Activities ◽

Biological Evaluation ◽

In Vitro Cytotoxicity ◽

Dilution Method ◽

Maximal Electroshock ◽

Protein Receptors

Objectives: The aim of the present study is to carry out a simple synthesis of aminoantipyrine analogues and exploration of their antibacterial, cytotoxic, and anticonvulsant potential. Methods: The compounds were characterized employing multi-spectroscopic methods. The in vitro pharmacological response of a series of bacteria were screened employing serial dilution method. The derivatives were screened against maximal electro-shock for their anticonvulsant activity. Molecular docking was carried out to optimize the interaction of the compounds with HPV16-E7 receptors. Further, the in vitro cytotoxicity was tested against human cervical cancer (SiHa) cell lines. Results: The compounds show protection against maximal electroshock, esp. 3-nirto- and 4-methyl-3-nitrobenzamido derivatives. In addition, they reveal appreciable DNA cleavage activities and interactions with HPV16-E7 protein receptors, esp. 3,5-dinitro- and 4-methyl-3-nitrobenzamido derivatives. Furthermore, they show potent activity against cervical cancer cells (LD50 value up to 1200 in the case of 4-methyl-3-nitrobenzamido derivative and an inhibition of a maximum of 97% of cells). Conclusions: The simply synthesized aminoantipyrine derivatives show a variety of biological activities like antibacterial and anticancer effects. In addition, this is the first study demonstrating that 4-aminoantipyrine derivatives shows an anticonvulsant activity.

Download Full-text

Synthesis and Cytotoxic Evaluation of Novel Benzimidazole Fused Condensed Thienopyrimdines Derivatives

Current Bioactive Compounds ◽

10.2174/1573407214666180808124802 ◽

2020 ◽

Vol 16 (2) ◽

pp. 133-141

Author(s):

S. Kaliraj ◽

Muthu K. Kathiravan

Keyword(s):

Good Yield ◽

Biological Activities ◽

In Vitro Cytotoxicity ◽

Cytotoxic Action ◽

Moderate Activity ◽

Quinazoline Derivative ◽

Cellular Division ◽

Major Health Problem ◽

Cytotoxicity Studies

Background: Cancer is a major health problem acting as a global killer and one of the leading causes of death. Most cancer chemotherapeutic drugs currently in clinical use are to kill malignant tumour cells by inhibiting some of the mechanisms implied in cellular division. Thienopyrimidines occupy a special position among the fused pyrimidines, along with other pyrimidines containing an annelated five membered hetero aromatic ring; forms a significant class of drugs which exhibit an array of various biological activities. One of the important current anticancer agent gefitinib acts as tyrosine kinase inhibitors is a quinazoline derivative. The thieno[2,3-d]pyrimidine ring system, is considered as a bioisostere of quinazoline moiety and have attracted great attention due to their broad bioactivities, including antitumor. Methods: Novel thienopyrimidine derivatives were synthesized by cyclization of thiophene o-amino esters with lactam salts such as pyrrolidin-2-one, piperidin-2-one and caprolactam by treating using phosphorous oxychloride. The next set of compounds thieno[2,3-d]pyrimidin-4(3H)-one were synthesised by Niementowski condensations between 2-aminothiophene carboxylate and formamide under reflux condition, followed by its chlorination in good yield. Microwave Fusion of 4-chlorothieno[2,3-d] pyrimidines with o-phenylenediamine afforded target compounds. The target compounds were tested on MCF-7 and HEK293 cell line. Results: The synthesized thirty compounds structures were established by IR, 1H NMR and Mass spectroscopy. The synthesized compounds were obtained in the good yield ranging from 45-70%. The synthesized compounds were subjected to cytotoxicity studies. Among the twenty compounds only one compound showed moderate activity. One of the compound 2c bearing acetyl group had IC50 48.93 μM. However decrease in the size of the lactam ring from six to five member ring or increase to seven member ring resulted in the loss of activity. The IC50 value of 5a was found to be 70.86μg/ml. The compound 5i have more cytotoxic action among the series. Conclusion: A series of thirty compounds belonging to novel pyyrolo, pyrido and benzimidazole fused thienopyrimidines were synthesized, characterized and were evaluated for their in vitro cytotoxicity. The compounds bearing bulky group such as terbutyl group and chloro substitution had the best activity. In conclusion, these structures seems to have biological properties and further investigation on this group could provide a lead.

Download Full-text