scholarly journals Synthesis and Biological Screening of New 4-Hydroxycoumarin Derivatives and Their Palladium(II) Complexes

2021 ◽  
Vol 2021 ◽  
pp. 1-18
Author(s):  
Edina H. Avdović ◽  
Isidora P. Petrović ◽  
Milena J. Stevanović ◽  
Luciano Saso ◽  
Jasmina M. Dimitrić Marković ◽  
...  
Keyword(s):  
Biological Activities ◽  
Cation Radical ◽  
Fibroblast Cell ◽  
Docking Studies ◽  
In Vitro Cytotoxicity ◽  
Toxicity Tests ◽  
Cytotoxic Activities ◽  
Spectroscopic Techniques

Two newly synthesized 4-hydroxycoumarin bidentate ligands (L1 and L2) and their palladium(II) complexes (C1 and C2) were screened for their biological activities, in vitro and in vivo. Structures of new compounds were established based on elemental analysis, 1H NMR, 13C NMR, and IR spectroscopic techniques. The obtained compounds were tested for their antioxidative and cytotoxic activities and results pointed to selective antiradical activity of palladium(II) complexes towards •OH and -•OOH radicals and anti-ABTS (2,2 ′ -Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) cation radical) activity comparable to that of ascorbate. Results indicated the effect of C1 and C2 on the enzymatic activity of the antioxidative defense system. In vitro cytotoxicity assay performed on different carcinoma cell lines (HCT166, A375, and MIA PaCa-2), and one healthy fibroblast cell line (MRC-5) showed a cytotoxic effect of both C1 and C2, expressed as a decrease in carcinoma cells’ viability, mostly by induction of apoptosis. In vivo toxicity tests performed on zebrafish embryos indicated different effects of C1 and C2, ranging from adverse developmental effect to no toxicity, depending on tested concentration. According to docking studies, both complexes (C1 and C2) showed better inhibitory activity in comparison to other palladium(II) complexes.

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

2019 ◽  
Vol 19 (5) ◽  
pp. 707-717 ◽  
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.

scholarly journals Clavanin A Improves Outcome of Complications from Different Bacterial Infections

2014 ◽  
Vol 59 (3) ◽  
pp. 1620-1626 ◽  
Author(s):  
Osmar N. Silva ◽  
Isabel C. M. Fensterseifer ◽  
Elaine A. Rodrigues ◽  
Hortência H. S. Holanda ◽  
Natasha R. F. Novaes ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Bacterial Infections ◽  
Multidrug Resistant ◽  
Toxicity Tests ◽  
Cytotoxic Activities ◽  
Content Type ◽  
Wound Model ◽  
Acute Toxicity Tests

ABSTRACTThe rapid increase in the incidence of multidrug-resistant infections today has led to enormous interest in antimicrobial peptides (AMPs) as suitable compounds for developing unusual antibiotics. In this study, clavanin A, an antimicrobial peptide previously isolated from the marine tunicateStyela clava, was selected as a purposeful molecule that could be used in controlling infection and further synthesized. Clavanin A wasin vitroevaluated againstStaphylococcus aureusandEscherichia colias well as toward L929 mouse fibroblasts and skin primary cells (SPCs). Moreover, this peptide was challenged here in anin vivowound and sepsis model, and the immune response was also analyzed. Despite displaying clearin vitroantimicrobial activity toward Gram-positive and -negative bacteria, clavanin A showed no cytotoxic activities against mammalian cells, and in acute toxicity tests, no adverse reaction was observed at any of the concentrations. Moreover, clavanin A significantly reduced theS. aureusCFU in an experimental wound model. This peptide also reduced the mortality of mice infected withE. coliandS. aureusby 80% compared with that of control animals (treated with phosphate-buffered saline [PBS]): these data suggest that clavanin A prevents the start of sepsis and thereby reduces mortality. These data suggest that clavanin A is an AMP that could improve the development of novel peptide-based strategies for the treatment of wound and sepsis infections.

scholarly journals Application ofAntrodia camphorataPromotes Rat’s Wound HealingIn Vivoand Facilitates Fibroblast Cell ProliferationIn Vitro

2015 ◽  
Vol 2015 ◽  
pp. 1-14 ◽  
Author(s):  
Zahra A. Amin ◽  
Hapipah M. Ali ◽  
Mohammed A. Alshawsh ◽  
Pouya H. Darvish ◽  
Mahmood A. Abdulla
Keyword(s):  
Cell Proliferation ◽  
Wound Healing ◽  
Granulation Tissue ◽  
Inflammatory Cell ◽  
Biological Activities ◽  
Fibroblast Cell ◽  
Parasitic Fungus ◽  
Antrodia Camphorata

Antrodia camphoratais a parasitic fungus from Taiwan, it has been documented to possess a variety of pharmacological and biological activities. The present study was undertaken to evaluate the potential ofAntrodia camphorataethanol extract to accelerate the rate of wound healing closure and histology of wound area in experimental rats. The safety ofAntrodia camphoratawas determinedin vivoby the acute toxicity test andin vitroby fibroblast cell proliferation assay. The scratch assay was used to evaluate thein vitrowound healing in fibroblast cells and the excision model of wound healing was testedin vivousing four groups of adultSprague Dawleyrats. Our results showed that wound treated withAntrodia camphorataextract and intrasite gel significantly accelerates the rate of wound healing closure than those treated with the vehicle. Wounds dressed withAntrodia camphorataextract showed remarkably less scar width at wound closure and granulation tissue contained less inflammatory cell and more fibroblast compared to wounds treated with the vehicle. Masson’s trichrom stain showed granulation tissue containing more collagen and less inflammatory cell inAntrodia camphoratatreated wounds. In conclusion,Antrodia camphorataextract significantly enhanced the rate of the wound enclosure in rats and promotes thein vitrohealing through fibroblast cell proliferation.

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

Molecules ◽  
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.

scholarly journals A Review on Daphnane-Type Diterpenoids and Their Bioactive Studies

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1842 ◽  
Author(s):  
Yue-Xian Jin ◽  
Lei-Ling Shi ◽  
Da-Peng Zhang ◽  
Hong-Yan Wei ◽  
Yuan Si ◽  
...  
Keyword(s):  
Biological Activities ◽  
Structural Diversity ◽  
Cytotoxic Activities ◽  
Hydroxyl Groups ◽  
Substitution Pattern ◽  
In Vivo Experiments ◽  
Wide Range ◽  
Anti Cancer

Natural daphnane diterpenoids, mainly distributed in plants of the Thymelaeaceae and Euphorbiaceae families, usually include a 5/7/6-tricyclic ring system with poly-hydroxyl groups located at C-3, C-4, C-5, C-9, C-13, C-14, or C-20, while some special types have a characteristic orthoester motif triaxially connectedat C-9, C-13, and C-14. The daphnane-type diterpenoids can be classified into five types: 6-epoxy daphnane diterpenoids, resiniferonoids, genkwanines, 1-alkyldaphnanes and rediocides, based on the oxygen-containing functions at rings B and C, as well as the substitution pattern of ring A. Up to now, nearly 200 daphnane-type diterpenoids have been isolated and elucidated from the Thymelaeaceae and Euphorbiaceae families. In-vitro and in-vivo experiments of these compounds have shown that they possess a wide range of biological activities, including anti-HIV, anti-cancer, anti-leukemic, neurotrophic, pesticidal and cytotoxic effects. A comprehensive account of the structural diversity is given in this review, along with the cytotoxic activities of daphnane-type diterpenoids, up to April 2019.

A saccharinate-bridged palladacyclic dimer with a Pd–Pd bond: experimental and molecular docking studies of the interaction with DNA and BSA and in vitro cytotoxicity against human cancer cell lines

2018 ◽  
Vol 42 (1) ◽  
pp. 574-586 ◽  
Author(s):  
Kazem Karami ◽  
Moloud Alinaghi ◽  
Zahra Amirghofran ◽  
Janusz Lipkowski ◽  
Amir Abbas Momtazi-borojeni
Keyword(s):  
Molecular Docking ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Activities ◽  
Docking Studies ◽  
In Vitro Cytotoxicity ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

The synthesis, characterization and biological activities of a saccharinate-bridged palladacyclic dimer are reported in this work.

scholarly journals Quinoline Functionalized Schiff Base Silver (I) Complexes: Interactions with Biomolecules and In Vitro Cytotoxicity, Antioxidant and Antimicrobial Activities

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1205
Author(s):  
Adesola A. Adeleke ◽  
Sizwe J. Zamisa ◽  
Md. Shahidul Islam ◽  
Kolawole Olofinsan ◽  
Veronica F. Salau ◽  
...  
Keyword(s):  
Schiff Base ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Antimicrobial Activities ◽  
In Vitro Cytotoxicity ◽  
Spectroscopic Techniques ◽  
Antioxidant Power

A series of fifteen silver (I) quinoline complexes Q1–Q15 have been synthesized and studied for their biological activities. Q1–Q15 were synthesized from the reactions of quinolinyl Schiff base derivatives L1–L5 (obtained by condensing 2-quinolinecarboxaldehyde with various aniline derivatives) with AgNO3, AgClO4 and AgCF3SO3. Q1–Q15 were characterized by various spectroscopic techniques and the structures of [Ag(L1)2]NO3Q1, [Ag(L1)2]ClO4Q6, [Ag(L2)2]ClO4Q7, [Ag(L2)2]CF3SO3Q12 and [Ag(L4)2]CF3SO3Q14 were unequivocally determined by single crystal X-ray diffraction analysis. In vitro antimicrobial tests against Gram-positive and Gram-negative bacteria revealed the influence of structure and anion on the complexes′ moderate to excellent antibacterial activity. In vitro antioxidant activities of the complexes showed their good radical scavenging activity in ferric reducing antioxidant power (FRAP). Complexes with the fluorine substituent or the thiophene or benzothiazole moieties are more potent with IC50 between 0.95 and 2.22 mg/mL than the standard used, ascorbic acid (2.68 mg/mL). The compounds showed a strong binding affinity with calf thymus-DNA via an intercalation mode and protein through a static quenching mechanism. Cytotoxicity activity was examined against three carcinoma cell lines (HELA, MDA-MB231, and SHSY5Y). [Ag(L2)2]ClO4Q7 with a benzothiazole moiety and [Ag(L4)2]ClO4Q9 with a methyl substituent had excellent cytotoxicity against HELA cells.

In silico, in-vitro and in vivo screening of biological activities of citral

2020 ◽  
pp. 1-10 ◽  
Author(s):  
Shagufta Habib ◽  
Pawan Gupta ◽  
Sana Shafi Bhat ◽  
Jeena Gupta
Keyword(s):  
In Silico ◽  
Biological Activities ◽  
In Silico Analysis ◽  
Biological Properties ◽  
Docking Studies ◽  
Industrial Applications ◽  
Yeast Cells ◽  
Cam Assay

Abstract. Citral, one of the main components of lemongrass oil (65–85%), is known to possess various medicinal properties like enhancing skin health and vision-improvement. It also acts as flavoring agent, used in perfumes and skin care products. The objective of this work was to elucidate the biological properties of citral at molecular level using an integrated in silico, in vitro and in vivo approaches. To elucidate this in silico molecular docking studies were performed with in vitro validation by DPPH scavenging activity, MTT assays, enzymatic assays and Chorio Allantoic Membrane (CAM) assay. The in silico analysis demonstrated the potential binding of citral with PPARγ ligand binding domain and vascular endothelial growth factor receptors (VEGFR-1 and VEGFR-2). Citral is already a proven anti-oxidant which is further confirmed by increased DPPH inhibition with increased citral concentration (IC50: 6.9 ± 1.68 μg/ml, p < 0.05). The results demonstrated that citral protect yeast cells from cytotoxic effects of hydrogen peroxide and also increase the activities of antioxidant enzymes like GST, SOD and LPO. It was also demonstrated to be cytotoxic to cancerous HeLa cells (IC50: 3.9 ± 0.38 μM, p < 0.01) and was found anti-angiogenic by CAM assay. This study highlights many important pharmaceutical properties of citral which can be explored further to increase its industrial applications.

Can the In Vivo Maximum Tolerated Dose be Predicted Using In Vitro Techniques? A Working Hypothesis

1991 ◽  
Vol 19 (4) ◽  
pp. 393-402
Author(s):  
Ravi Shrivastava ◽  
Gareth W. John ◽  
Ginette Rispat ◽  
Annick Chevalier ◽  
Roy Massingham
Keyword(s):  
Cell Death ◽  
Research Effort ◽  
Maximum Tolerated Dose ◽  
In Vitro Cytotoxicity ◽  
Toxicity Tests ◽  
In Vitro Toxicity ◽  
Working Hypothesis ◽  
Wide Range

All new chemical entities synthesised in our laboratories have routinely been subjected to in vitro toxicity tests. Out of curiosity, we established a working hypothesis in which the in vitro data could be empirically transformed to predict the in vivo four-week standard maximum tolerated dose (MTD) studies in rats and dogs. As a first step to verifying this hypothesis, we report here the findings of an in vitro cytotoxicity study of 25 compounds randomly selected from our files, possessing a wide range of pharmacological activities and for which data from standard four-week MTD studies were available. Single blind in vitro toxicity studies in three carefully selected types of primary and cell line cultures were carried out. In vitro CT50 (concentration inducing 50% cell death) and CT100 (concentration inducing 100% cell death) values were obtained for each of the three cell types and, using empirical assumptions, these results were used to predict the MTD in vivo in the rat and dog. The actual in vivo threshold and toxic doses were obtained from the MTD study reports. The in vivo toxicity values predicted from the in vitro toxicity results with this series of 25 compounds showed a better than 80% correlation with the actual in vivo results obtained in the MTD studies. Whether or not in vitro cytotoxicity predictions are ultimately found to be directly and consistently related to the MTD in vivo for all pharmacological classes of compounds will require many additional studies, but it is hoped that these results will stimulate the necessary research effort required to answer this question.

scholarly journals In vitro and in vivo response of composites based on chitosan, hydroxyapatite and collagen

2019 ◽  
Vol 42 ◽  
pp. e41102
Author(s):  
Maurício Bordini do Amaral ◽  
Rommel Bezerra Viana ◽  
Katúcia Bezerra Viana ◽  
Cristina Aparecida Diagone ◽  
Aline Bassi Denis ◽  
...  
Keyword(s):  
Vero Cells ◽  
In Vitro Cytotoxicity ◽  
Tissue Reaction ◽  
Tissue Response ◽  
Bone Collagen ◽  
Biological Behavior ◽  
Toxicity Tests ◽  
Bovine Bone

 The goal of this study was to evaluate the in vitro cellular toxicity and biological behavior of new bone graft composites after subcutaneous implantation during remodeling and wound-healing processes. We developed composites based on hydroxyapatite (obtained by deproteinizing bovine bone), collagen (obtained from bovine tendon) and chitosan (obtained from gladii of the squid species Loligo), that were characterized by different techniques (X-ray, FT-IR, Thermogravimetry, DSC and SEM). Three biomaterials were evaluated here: B1 (collagen/chitosan/hydroxyapatite), B2 (collagen/hydroxyapatite) B3 (collagen/hydroxyapatite). For in vitro cytotoxicity tests, two cell lines were used: HEp human larynx tumor cells (ATCC-CCL-23) and VERO cells from African green monkey (Cercopithecus aethiops). These toxicity tests demonstrated that the evaluated composites are not toxic. In biocompatibility tests, the results of a histological analysis showed that all three biomaterials present a low inflammatory tissue reaction. The tissue response was most favorable for sample B3, followed by B2 and B1, in that order. Based on these results, we conclude that all three biomaterials show good biocompatibility and no evidence of cytotoxicity; thus, these materials represent good candidates for tissue and graft engineering for use in bone regeneration.

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