scholarly journals In Vitro and In Vivo Studies of Anti-Lung Cancer Activity of Artemesia judaica L. Crude Extract Combined with LC-MS/MS Metabolic Profiling, Docking Simulation and HPLC-DAD Quantification

Antioxidants ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 17
Author(s):  
Marwa S. Goda ◽  
Mohamed S. Nafie ◽  
Basma M. Awad ◽  
Maged S. Abdel-Kader ◽  
Amany K. Ibrahim ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Liquid Chromatography ◽  
Cytotoxic Activity ◽  
Active Sites ◽  
Array Detector ◽  
Cytotoxic Activities ◽  
Promising Source ◽  
Cancer Activity

Artemisia judaica L. (Family: Asteraceae) exhibited antioxidant, anti-inflammatory, and antiapoptotic effects. The in vitro cytotoxic activity of A. judaica ethanolic extract was screened against a panel of cancer cell lines. The results revealed its cytotoxic activity against a lung cancer (A549) cell line with a promising IC50 of 14.2 μg/mL compared to doxorubicin as a standard. This was confirmed through the downregulation of antiapoptotic genes, the upregulation of proapoptotic genes, and the cell cycle arrest at the G2/M phase. Further in vivo study showed that a solid tumor mass was significantly reduced, with a tumor inhibition ratio of 54% relative to doxorubicin therapy in a Xenograft model. From a chemical point of view, various classes of natural products have been identified by liquid chromatography combined with tandem mass spectrometry (LC-MS/MS). The docking study of the detected metabolites approved their cytotoxic activity through their virtual binding affinity towards the cyclin-dependent kinase 2 (CDK-2) and epidermal growth factor receptor (EGFR) active sites. Finally, A. judaica is a fruitful source of polyphenols that are well-known for their antioxidant and cytotoxic activities. As such, the previously reported polyphenols with anti-lung cancer activity were quantified by high-performance liquid chromatography coupled with a diode array detector (HPLC-DAD). Rutin, quercetin, kaempferol, and apigenin were detected at concentrations of 6 mg/gm, 0.4 mg/gm, 0.36 mg/gm, and 3.9 mg/gm of plant dry extract, respectively. It is worth noting that kaempferol and rutin are reported for the first time. Herein, A. judaica L. may serve as an adjuvant therapy or a promising source of leading structures in drug discovery for lung cancer treatment.

scholarly journals The red wine component ellagic acid induces autophagy and exhibits anti-lung cancer activity in vitro and in vivo

2018 ◽  
Vol 23 (1) ◽  
pp. 143-154 ◽  
Author(s):  
Jing Duan ◽  
Ji-Cheng Zhan ◽  
Gui-Zhen Wang ◽  
Xin-Chun Zhao ◽  
Wei-Dong Huang ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Ellagic Acid ◽  
Red Wine ◽  
Cancer Activity

Volatile oil from alpinia officinarum promotes lung cancer regression in vitro and in vivo

2018 ◽  
Vol 9 (9) ◽  
pp. 4998-5006 ◽  
Author(s):  
Ning Li ◽  
Qingyu Zhang ◽  
Zhenbin Jia ◽  
Xiaohong Yang ◽  
Haitao Zhang ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Underlying Mechanism ◽  
Volatile Oil ◽  
Alpinia Officinarum ◽  
Low Cytotoxicity ◽  
Cancer Intervention ◽  
Cancer Activity ◽  
Cancer Regression

The anti-lung cancer activity of volatile oil from Alpinia officinarum (VOAO) and the underlying mechanism has been studied. VOAO could be an effective, low cytotoxicity candidate for lung cancer intervention.

scholarly journals Phytochemical and Pharmacological Potential of Enhydra fluctuans Available in Bangladesh

2019 ◽  
pp. 1-11
Author(s):  
S. Kamal ◽  
S. R. Rony ◽  
S. Sharmin ◽  
F. R. Laboni ◽  
M. H. Sohrab
Keyword(s):  
Cytotoxic Activity ◽  
Radical Scavenging ◽  
Diffusion Method ◽  
Clot Lysis ◽  
Cytotoxic Activities ◽  
Hypotonic Solution ◽  
Chemical Screening ◽  
Soluble Fractions

Objectives: The possible phytochemical constituents, thrombolytic and membrane stabilizing activities of the crude ethanolic extract of Enhydra fluctuans (CE) were investigated along with the antimicrobial, antioxidant and cytotoxic potentials of its petroleum ether (PESF), carbon tetrachloride (CTCSF), chloroform (CSF) and aqueous (AQSF) soluble fractions. Materials & Methods: The coarse leaf powder was extracted at room temperature with ethanol. Solvent-solvent partitioning was done to obtain the four soluble fractions. Anticoagulant potential was determined by the in vitro thrombolytic model, membrane stabilization method was used to assess in vitro anti-inflammatory activity, the disc diffusion method was used for anti-microbial screening, antioxidant potential was determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method and brine shrimp lethality bioassay method was used for cytotoxic activity determination. Results: Chemical screening of the crude extract evidenced the presence of alkaloids, saponins, tannins, flavonoids, reducing sugars and gums. It showed significant clot lysis property of 46.91%. It also significantly inhibited heat and hypotonic solution induced lysis of the human red blood cell membrane with values of 71.80% and 47.60%, respectively. CTCSF and PESF showed mild antimicrobial activity. AQSF showed most prominent antioxidant activity with IC50 value of 12.27 µg/mL. CTCSF showed LC50 value of 0.84 µg/mL, with most potent cytotoxic activity. Conclusion: Significant thrombolytic, membrane stabilizing, antioxidant and in vitro cytotoxic activities of the ethanolic plant extract were observed in this study. In vivo activities and isolation of active compound(s) from this extract are yet to be investigated.

scholarly journals Potent anti-cancer activity of Alnus nitida against lung cancer cells; in vitro and in vivo studies

2019 ◽  
Vol 110 ◽  
pp. 254-264 ◽  
Author(s):  
Moniba Sajid ◽  
Chao Yan ◽  
Dawei Li ◽  
Siva Bharath Merugu ◽  
Hema Negi ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cancer Cells ◽  
Lung Cancer Cells ◽  
In Vivo Studies ◽  
Anti Cancer ◽  
Cancer Activity

scholarly journals Treating Hyperglycemia From Eryngium caeruleum M. Bieb: In-vitro α-Glucosidase, Antioxidant, in-vivo Antidiabetic and Molecular Docking-Based Approaches

2020 ◽  
Vol 8 ◽  
Author(s):  
Abdul Sadiq ◽  
Umer Rashid ◽  
Sadiq Ahmad ◽  
Mohammad Zahoor ◽  
Mohamed F. AlAjmi ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Free Radicals ◽  
Bioactive Compounds ◽  
Active Sites ◽  
Methanolic Extract ◽  
Array Detector ◽  
Chloroform Fraction ◽  
Ms Analysis

Natural-based drugs are believed to be safe, effective and economical. Based on the medicinal importance of the genus Eryngium and unexplored nature of Eryngium caeruleum, we have evaluated its antidiabetic and antioxidant potentials. Both in-vitro and in-vivo assays have been carried out for antidiabetic assays. The antioxidant activity was determined by using different free radicals [i.e., 1,1-diphenyl,2-picrylhydrazyl (DPPH), 2,2-azinobis[3-ethylbenzthiazoline]-6-sulfonic acid (ABTS), and hydrogen peroxide (H2O2)]. Moreover, different phytoconstituents were identified in the most active solvent fraction by GC-MS analysis. Furthermore, comparative fingerprints of methanolic extract and chloroform fraction were also analyzed via High Performance Liquid Chromatography coupled with Diode Array Detector (HPLC-DAD). The crude methanolic extract of E. caeruleum (Ec.Cr) and its sub-fractions [i.e., n-hexane (Ec.Hex), chloroform (Ec.Chf), ethyl acetate (Ec.EtAc), and aqueous (Ec.Aq) were employed in this study]. In the α-glucosidase inhibition assay, a concentration-dependent inhibitory response was observed against the enzyme. The most active sample was Ec.Chf which revealed an IC50 of 437 μg/ml in comparison to the standard acarbose (IC50 25 μg/ml). The rest of the samples showed moderate inhibition of α-glucosidase. In antioxidant assays, Ec.Chf and Ec.Cr exhibited a considerable scavenging effect against all the free radicals. The IC50 values recorded for Ec.Chf were 112, 109, and 150 μg/ml against DPPH, ABTS, and H2O2 respectively. Based on the in-vitro potential of Ec.Chf, this was subjected to the in-vivo model experiment. The Ec.Chf lowered the blood glucose level up to 10.3 mmol/L at 500 μg/Kg. The Ec.Chf was also subjected to GC-MS analysis. The GC-MS analysis confirmed the presence of 60 compounds. The identified phytoconstituents consist of some essential compounds previously reported with antidiabetic and antioxidant studies, which include thymol, tocopherol, phytol, nerolidol, (I)-neophytadiene, linolenic acid, and falcarinol. Similarly, the HPLC-DAD chromatograms of Ec.Cr and Ec.Chf exhibited a variety of peaks, which further demonstrates the possibility of important phytochemicals. In a nutshell, we can conclude that Eryngium caeruleum is a potential source of bioactive compounds which may be beneficial for the management of ailments like diabetes and free radicals mediated disorders. Molecular docking was performed to explore the possible role of all the identified bioactive compounds in the chloroform fraction of Eryngium caeruleum into active sites of the homology model of α-glucosidase.

scholarly journals Effect of Oversulfation on the Composition, Structure, and In Vitro Anti-Lung Cancer Activity of Fucoidans Extracted from Sargassum aquifolium

Marine Drugs ◽  
2021 ◽  
Vol 19 (4) ◽  
pp. 215
Author(s):  
Hui-Hua Hsiao ◽  
Tien-Chiu Wu ◽  
Yung-Hsiang Tsai ◽  
Chia-Hung Kuo ◽  
Ren-Han Huang ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Biological Activities ◽  
Annexin V ◽  
Structural Features ◽  
Signaling Cascades ◽  
Cytochrome C Release ◽  
Wide Range ◽  
Cancer Activity

Intensive efforts have been undertaken in the fields of prevention, diagnosis, and therapy of lung cancer. Fucoidans exhibit a wide range of biological activities, which are dependent on the degree of sulfation, sulfation pattern, glycosidic branches, and molecular weight of fucoidan. The determination of oversulfation of fucoidan and its effect on anti-lung cancer activity and related signaling cascades is challenging. In this investigation, we used a previously developed fucoidan (SCA), which served as a native fucoidan, to generate two oversulfated fucoidan derivatives (SCA-S1 and SCA-S2). SCA, SCA-S1, and SCA-S2 showed differences in compositions and had the characteristic structural features of fucoidan by Fourier transform infrared (FTIR) and nuclear magnetic resonance (NMR) analyses. The anticancer properties of SCA, SCA-S1, and SCA-S2 against human lung carcinoma A-549 cells were analyzed in terms of cytotoxicity, cell cycle, Bcl-2 expression, mitochondrial membrane potential (MMP), expression of caspase-3, cytochrome c release, Annexin V/propidium iodide (PI) staining, DNA fragmentation, and the underlying signaling cascades. Our findings indicate that the oversulfation of fucoidan promotes apoptosis of lung cancer cells and the mechanism may involve the Akt/mTOR/S6 pathway. Further in vivo research is needed to establish the precise mechanism whereby oversulfated fucoidan mitigates the progression of lung cancer.

scholarly journals The Biological and Biophysical Properties of the Spider Peptide Gomesin

Molecules ◽  
2018 ◽  
Vol 23 (7) ◽  
pp. 1733 ◽  
Author(s):  
John Tanner ◽  
Evelyne Deplazes ◽  
Ricardo Mancera
Keyword(s):  
Cytotoxic Activity ◽  
Current Knowledge ◽  
Cytotoxic Activities ◽  
Binding Properties ◽  
Anti Cancer ◽  
Specific Selectivity ◽  
Cell Type Specific ◽  
Molecular Mechanism Of Action

This review summarises the current knowledge of Gomesin (Gm), an 18-residue long, cationic anti-microbial peptide originally isolated from the haemocytes of the Brazilian tarantula Acanthoscurria gomesiana. The peptide shows potent cytotoxic activity against clinically relevant microbes including Gram-positive and Gram-negative bacteria, fungi, and parasites. In addition, Gm shows in-vitro and in-vivo anti-cancer activities against several human and murine cancers. The peptide exerts its cytotoxic activity by permeabilising cell membranes, but the underlying molecular mechanism of action is still unclear. Due to its potential as a therapeutic agent, the structure and membrane-binding properties, as well as the leakage and cytotoxic activities of Gm have been studied using a range of techniques. This review provides a summary of these studies, with a particular focus on biophysical characterisation studies of peptide variants that have attempted to establish a structure-activity relationship. Future studies are still needed to rationalise the binding affinity and cell-type-specific selectivity of Gm and its variants, while more pre-clinical studies are required to develop Gm into a therapeutically useful peptide.

scholarly journals Intratumoral combination therapy with poly(I:C) and resiquimod synergistically triggers tumor-associated macrophages for effective systemic antitumoral immunity

2021 ◽  
Vol 9 (9) ◽  
pp. e002408
Author(s):  
Clément Anfray ◽  
Francesco Mainini ◽  
Elisabeth Digifico ◽  
Akihiro Maeda ◽  
Marina Sironi ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Flow Cytometry ◽  
T Cells ◽  
Cytotoxic Activity ◽  
Protein Interaction ◽  
Poly I:C ◽  
Tumor Associated Macrophages ◽  
Protein Protein Interaction

BackgroundTumor-associated macrophages (TAMs) play a key immunosuppressive role that limits the ability of the immune system to fight cancer and hinder the antitumoral efficacy of most treatments currently applied in the clinic. Previous studies have evaluated the antitumoral immune response triggered by (TLR) agonists, such as poly(I:C), imiquimod (R837) or resiquimod (R848) as monotherapies; however, their combination for the treatment of cancer has not been explored. This study investigates the antitumoral efficacy and the macrophage reprogramming triggered by poly(I:C) combined with R848 or with R837, versus single treatments.MethodsTLR agonist treatments were evaluated in vitro for toxicity and immunostimulatory activity by Alamar Blue, ELISA and flow cytometry using primary human and murine M-CSF-differentiated macrophages. Cytotoxic activity of TLR-treated macrophages toward cancer cells was evaluated with an in vitro functional assay by flow cytometry. For in vivo experiments, the CMT167 lung cancer model and the MN/MCA1 fibrosarcoma model metastasizing to lungs were used; tumor-infiltrating leukocytes were evaluated by flow cytometry, RT-qPCR, multispectral immunophenotyping, quantitative proteomic experiments, and protein–protein interaction analysis.ResultsResults demonstrated the higher efficacy of poly(I:C) combined with R848 versus single treatments or combined with R837 to polarize macrophages toward M1-like antitumor effectors in vitro. In vivo, the intratumoral synergistic combination of poly(I:C)+R848 significantly prevented tumor growth and metastasis in lung cancer and fibrosarcoma immunocompetent murine models. Regressing tumors showed increased infiltration of macrophages with a higher M1:M2 ratio, recruitment of CD4+ and CD8+ T cells, accompanied by a reduction of immunosuppressive CD206+ TAMs and FOXP3+/CD4+ T cells. The depletion of both CD4+ and CD8+ T cells resulted in complete loss of treatment efficacy. Treated mice acquired systemic antitumoral response and resistance to tumor rechallenge mediated by boosted macrophage cytotoxic activity and T-cell proliferation. Proteomic experiments validate the superior activation of innate immunity by poly(I:C)+R848 combination versus single treatments or poly(I:C)+R837, and protein–protein-interaction network analysis reveal the key activation of the STAT1 pathway.DiscussionThese findings demonstrate the antitumor immune responses mediated by macrophage activation on local administration of poly(I:C)+R848 combination and support the intratumoral application of this therapy to patients with solid tumors in the clinic.

Action of Thioglycosides of 1,2,4-Triazoles and Imidazoles on the Oxidative Stress and Glycosidases in Mice with Molecular Docking

2019 ◽  
Vol 16 (6) ◽  
pp. 696-710
Author(s):  
Mahmoud Balbaa ◽  
Doaa Awad ◽  
Ahmad Abd Elaal ◽  
Shimaa Mahsoub ◽  
Mayssaa Moharram ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Molecular Docking ◽  
Active Sites ◽  
Biological Activities ◽  
Imidazole Ring ◽  
Quantitative Structure Activity Relationship ◽  
Binding Interaction ◽  
Qsar Study

Background: ,2,3-Triazoles and imidazoles are important five-membered heterocyclic scaffolds due to their extensive biological activities. These products have been an area of growing interest to many researchers around the world because of their enormous pharmaceutical scope. Methods: The in vivo and in vitro enzyme inhibition of some thioglycosides encompassing 1,2,4- triazole N1, N2, and N3 and/or imidazole moieties N4, N5, and N6. The effect on the antioxidant enzymes (superoxide dismutase, glutathione S-transferase, glutathione peroxidase and catalase) was investigated as well as their effect on α-glucosidase and β-glucuronidase. Molecular docking studies were carried out to investigate the mode of the binding interaction of the compounds with α- glucosidase and β -glucuronidase. In addition, quantitative structure-activity relationship (QSAR) investigation was applied to find out the correlation between toxicity and physicochemical properties. Results: The decrease of the antioxidant status was revealed by the in vivo effect of the tested compounds. Furthermore, the in vivo and in vitro inhibitory effects of the tested compounds were clearly pronounced on α-glucosidase, but not β-glucuronidase. The IC50 and Ki values revealed that the thioglycoside - based 1,2,4-triazole N3 possesses a high inhibitory action. In addition, the in vitro studies demonstrated that the whole tested 1,2,4-triazole are potent inhibitors with a Ki magnitude of 10-6 and exhibited a competitive type inhibition. On the other hand, the thioglycosides - based imidazole ring showed an antioxidant activity and exerted a slight in vivo stimulation of α-glucosidase and β- glucuronidase. Molecular docking proved that the compounds exhibited binding affinity with the active sites of α -glucosidase and β-glucuronidase (docking score ranged from -2.320 to -4.370 kcal/mol). Furthermore, QSAR study revealed that the HBD and RB were found to have an overall significant correlation with the toxicity. Conclusion: These data suggest that the inhibition of α-glucosidase is accompanied by an oxidative stress action.

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