scholarly journals Anticancer properties of dried-pericarp water extracts of Camellia japonica L. fermented with Aspergillus oryzae through regulation of IGFBP-2/mTOR pathway

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Eugene Cho ◽  
Jin Kim ◽  
Da Hye Jeong ◽  
Hyoun Woo Kim
Keyword(s):  
Anticancer Activity ◽  
Aspergillus Oryzae ◽  
Water Extract ◽  
Annexin V ◽  
Anticancer Activities ◽  
Camellia Japonica ◽  
Water Extracts ◽  
Anticancer Properties ◽  
Mtor Phosphorylation ◽  
Fadu Cells

AbstractThis study aimed to investigate the anticancer activity of dried-pericarp water extract of fermented C. japonicus (CJ). The dried-pericarp water extracts of CJ were fermented using Aspergillus oryzae and Saccharomyces cerevisiae at 30 °C and 35 °C. The anticancer activities of both water extracts fermented at 30 °C and 35 °C using A. oryzae against FaDu cells were remarkably changed compared with unfermented dried-pericarp water extract of CJ, which has no anticancer activity. Cleaved-PARP, caspase 3, and apoptotic cells stained with annexin V/PI were significantly increased by treatment with A. oryzae extracts fermented at 30 °C. The insulin-like growth factor-binding protein 2 (IGFBP-2) protein level and mTOR phosphorylation by A. oryzae fermented extracts (AOFE) were dramatically reduced, and the expression levels of IGFBP-2 and phosphorylated mTOR were significantly increased depending on the glucose concentrations in FaDu cells. These results suggested that the cell viabilities in AOFE were restored as the glucose concentrations increased. Furthermore, it was confirmed LC/MS/MS that the content of gallic acid was increased by fermentation of Aspergillus oryzae (5.596 ± 0.1746 μg/mg) compared to the unfermented extract (1.620 ± 0.0432 μg/mg). Based on these results, the anticancer effect of AOFE was achieved through inhibition of the IGFBP-2/mTOR signaling pathway. These results suggest that AOFE may be a potential treatment for head and neck cancer.

scholarly journals Biochemical and Molecular Investigation of In Vitro Antioxidant and Anticancer Activity Spectrum of Crude Extracts of Willow Leaves Salix safsaf

Plants ◽  
2020 ◽  
Vol 9 (10) ◽  
pp. 1295
Author(s):  
Mourad A. M. Aboul-Soud ◽  
Abdelkader E. Ashour ◽  
Jonathan K. Challis ◽  
Atallah F. Ahmed ◽  
Ashok Kumar ◽  
...  
Keyword(s):  
Cell Lines ◽  
High Resolution Mass Spectrometry ◽  
Control Cell ◽  
Annexin V ◽  
Fluorescence Signal ◽  
Facs Analysis ◽  
Anticancer Activities ◽  
Anticancer Properties ◽  
Organic Fractions

Organic fractions and extracts of willow (Salix safsaf) leaves, produced by sequential solvent extraction as well as infusion and decoction, exhibited anticancer potencies in four cancerous cell lines, including breast (MCF-7), colorectal (HCT-116), cervical (HeLa) and liver (HepG2). Results of the MTT assay revealed that chloroform (CHCl3) and ethyl acetate (EtOAc)-soluble fractions exhibited specific anticancer activities as marginal toxicities were observed against two non-cancerous control cell lines (BJ-1 and MCF-12). Ultra-high-resolution mass spectrometry Q-Exactive™ HF Hybrid Quadrupole-Orbitrap™ coupled with liquid chromatography (UHPLC) indicated that both extracts are enriched in features belonging to major phenolic and purine derivatives. Fluorescence-activated cell sorter analysis (FACS), employing annexin V-FITC/PI double staining indicated that the observed cytotoxic potency was mediated via apoptosis. FACS analysis, monitoring the increase in fluorescence signal, associated with oxidation of DCFH to DCF, indicated that the mechanism of apoptosis is independent of reactive oxygen species (ROS). Results of immunoblotting and RT-qPCR assays showed that treatment with organic fractions under investigation resulted in significant up-regulation of pro-apoptotic protein and mRNA markers for Caspase-3, p53 and Bax, whereas it resulted in a significant reduction in amounts of both protein and mRNA of the anti-apoptotic marker Bcl-2. FACS analysis also indicated that pre-treatment and co-treatment of human amniotic epithelial (WISH) cells exposed to the ROS H2O2 with EtOAc fraction provide a cytoprotective and antioxidant capacity against generated oxidative stress. In conclusion, our findings highlight the importance of natural phenolic and flavonoid compounds with unparalleled and unique antioxidant and anticancer properties.

scholarly journals Anticancer Activity of Two Novel Hydroxylated Biphenyl Compounds toward Malignant Melanoma Cells

2021 ◽  
Vol 22 (11) ◽  
pp. 5636
Author(s):  
Marina Pisano ◽  
Maria Antonietta Dettori ◽  
Davide Fabbri ◽  
Giovanna Delogu ◽  
Giuseppe Palmieri ◽  
...  
Keyword(s):  
Malignant Melanoma ◽  
Anticancer Activity ◽  
Neuroblastoma Cells ◽  
Annexin V ◽  
Melanoma Cells ◽  
Parp Cleavage ◽  
Novel Treatments ◽  
Anticancer Properties ◽  
Ic50 Values ◽  
Irreversible Effects

Melanoma, the deadliest form of skin cancer, is still one of the most difficult cancers to treat despite recent advances in targeted and immune therapies. About 50% of advanced melanoma do not benefit of such therapies, and novel treatments are requested. Curcumin and its analogs have shown good anticancer properties and are being considered for use in combination with or sequence to recent therapies to improve patient outcomes. Our group previously published the synthesis and anticancer activity characterization of a novel curcumin-related compound against melanoma and neuroblastoma cells (D6). Here, two hydroxylated biphenyl compounds—namely, compounds 11 and 12—were selected among a small collection of previously screened C2-symmetric hydroxylated biphenyls structurally related to D6 and curcumin, showing the best antitumor potentiality against melanoma cells (IC50 values of 1.7 ± 0.5 μM for 11 and 2.0 ± 0.7 μM for 12) and no toxicity of normal fibroblasts up to 32 µM. Their antiproliferative activity was deeply characterized on five melanoma cell lines by performing dose-response and clonal growth inhibition assays, which revealed long-lasting and irreversible effects for both compounds. Apoptosis induction was ascertained by the annexin V and TUNEL assays, whereas Western blotting showed caspase activation and PARP cleavage. A cell cycle analysis, following cell treatments with either compound 11 or 12, highlighted an arrest in the G2/M transition. Taking all this evidence together, 11 and 12 were shown to be good candidates as lead compounds to develop new anticancer drugs against malignant melanoma.

scholarly journals SEAWEED EXTRACTS EXHIBIT ANTICANCER ACTIVITY AGAINST HeLa CELL LINES

2016 ◽  
Vol 9 (1) ◽  
pp. 114 ◽  
Author(s):  
Ashwini S. ◽  
Suresh Babut V. ◽  
Saritha . ◽  
Manjula Shantara Shantaram
Keyword(s):  
Anticancer Activity ◽  
Potential Candidate ◽  
Anticancer Activities ◽  
Vitro Assay ◽  
Anticancer Properties ◽  
Seaweed Extracts ◽  
Hela Cell Lines ◽  
Ic50 Value ◽  
Ethanol Extracts

Objective: This study was conducted to examine the anticancer activities in the extracts of marine seaweeds Gracilariacorticata.Methods: The acetone, chloroform, ethanol, methanol and aqueous extracts of collected seaweeds were tested for their anticancer properties in vitro against HeLa cancer cell lines.Results: The anticancer activity of the seaweed extracts was observed at 24hours, 48 hours and 72 h in which chloroform and ethanol extracts of G. corticata showed a greater activity with an IC50 value of 341.82 µg/ml and 244.7 µg/ml respectively for 48hours. P-values were determined by two-way analysis of variance (ANOVA). The morphology of the treated cells showed a great variation when compared to the control cells. Thus, the in vitro assay indicates that the extracts of seaweeds are the significant source of a noble anticancer agent.Conclusion: This study also infers that G. corticata could be a potential candidate for cancer therapy in the near future.

scholarly journals Manilkara zapota (L.) P. Royen Leaf Water Extract Induces Apoptosis in Human Hepatocellular Carcinoma (HepG2) Cells via ERK1/2/Akt1/JNK1 Signaling Pathways

2018 ◽  
Vol 2018 ◽  
pp. 1-17 ◽  
Author(s):  
Bee Ling Tan ◽  
Mohd Esa Norhaizan ◽  
Lee Chin Chan
Keyword(s):  
Hepatocellular Carcinoma ◽  
Hepg2 Cells ◽  
Water Extract ◽  
Annexin V ◽  
Leaf Water ◽  
Human Hepatocellular Carcinoma ◽  
Enzyme Linked Immunosorbent Assay ◽  
Cytotoxicity Activity ◽  
Manilkara Zapota ◽  
Anticancer Properties

Manilkara zapota (L.) P. Royen, called sapodilla, or locally known as ciku, belongs to the family Sapotaceae. We found that Manilkara zapota leaf water extract has cytotoxic effect against human hepatocellular carcinoma (HepG2) cell line in our earlier study. Therefore, this study aimed to explore the anticancer properties of Manilkara zapota leaf water extract in HepG2 cells. We also aimed to unravel yet undiscovered mechanisms and identified several expressed genes whose functions in cytotoxicity activity of Manilkara zapota leaf water extract in HepG2 cells have not been well-studied. The apoptosis and intracellular reactive oxygen species (ROS) activities were analyzed using Annexin V-propidium iodide staining and dichlorodihydrofluorescein diacetate, respectively, by NovoCyte Flow Cytometer. Bax and Bcl-2 expression were assessed using Enzyme-Linked Immunosorbent Assay. The associated molecular pathways were evaluated by quantitative real-time PCR. Overall analyses revealed that Manilkara zapota leaf water extract can increase percentage of early apoptotic cells, induce the formation of ROS, upregulate c-Jun N-terminal kinase 1 (JNK1) and inducible nitric oxide synthase (iNOS), and reduce Akt1 and vascular endothelial growth factor A (VEGFA) transcriptional activities. Our data suggest that Manilkara zapota leaf water extract can suppress the growth of HepG2 cells via modulation of ERK1/2/Akt1/JNK1 transcriptional expression.

scholarly journals PHENOLIC ACID PROFILING BY RP-HPLC: EVALUATION OF ANTIBACTERIAL AND ANTICANCER ACTIVITIES OF CONOCARPUS ERECTUS PLANT EXTRACTS

2020 ◽  
Vol 2020 (1) ◽  
Author(s):  
R Khalil ◽  
Q Ali ◽  
MM Hafeez ◽  
A Malik
Keyword(s):  
Antibacterial Activity ◽  
Anticancer Activity ◽  
Folk Medicine ◽  
Bacterial Strains ◽  
Anticancer Activities ◽  
Anticancer Properties ◽  
Conocarpus Erectus ◽  
Rp Hplc

Due to the versatile application of plants the utilization of plants and their inferred substances builds up day by day for the revelation of new curative agents. Conocarpus erectus has placed in the family Combretaceae, in one of the two species of Conocarpus genus and ordinarily exists in tropical and subtropical regions of the world. In some countries it is used as folk medicine for fever, anemia, diabetes, catarrh, diarrhea and conjunctivitis. The current study was carried out to investigate the antibacterial and anticancer properties of the plant. The four defatted methanol extracts of C. erectus different parts (leaves, stems, fruits and bark) showed high antibacterial and anticancer activity even with small quantity of dose. Antimicrobial assay was used to check out the antibacterial activity against 6 bacterial strains Escherichia coli, Staphylococcus Aureus and Klebstella Pneumoniae.  The results show that gram positive bacteria show more sensitivity and zone of inhibition as compared to gram negative bacteria. For anticancer activity, MTT assay was performed on HepG2 cells for this purpose. Plant extorts show anticancer activity with a minute quantity. For phytochemical screening defatted methanol extract of Conocarpus erectus was subjected to the silica gel glass column go behind by (RP-HPLC–UV–ESI-MS). It contains phenol such as tannin and flavinoid as major component. Plant contain Ellagic acid; di-hexahydroxy diphenyl, Vascalgin isomer as foremost tannin component. Gallic Acid, Kaempferol on the base of mass spectra and time of retention. The extract of Conocarpus erectus (leaves, shoot, bark & fruit) parts shows high antibacterial, antioxidant and hepta-protective activities due to phenolic content. Tannin has high antibacterial activity than other compound. C.erectus is notable for its folkloristic curative potential. More in vivo and in vitro phytochemical studies are needed to use the plant for prevention and treatment of many diseases.

Vitamin D as potential therapeutic anticancer agent

2018 ◽  
pp. 1-3
Keyword(s):  
Vitamin D ◽  
Anticancer Activity ◽  
Anticancer Agent ◽  
Antitumor Agents ◽  
Metastatic Potential ◽  
Anticancer Properties ◽  
Chemotherapy Agents

The role of vitamin D is implicated in carcinogenesis through numerous biological processes like induction of apoptosis, modulation of immune system inhibition of inflammation and cell proliferation and promotion of cell differentiation. Its use as additional adjuvant drug with cancer treatment may be novel combination for improved outcome of different cancers. Numerous preclinical, epidemiological and clinical studies support the role of vitamin D as an anticancer agent. Anticancer properties of vitamin D have been studied widely (both in vivo and in vitro) among various cancers and found to have promising results. There are considerable data that indicate synergistic potential of calcitriol and antitumor agents. Possible mechanisms for modulatory anticancer activity of vitamin D include its antiproliferative, prodifferentiating, and anti-angiogenic and apoptic properties. Calcitriol reduces invasiveness and metastatic potential of many cancer cells by inhibiting angiogenesis and regulating expression of the key molecules involved in invasion and metastasis. Anticancer activity of vitamin D is synergistic or additive with the antineoplastic actions of several drugs including cytotoxic chemotherapy agents like paclitaxel, docetaxel, platinum base compounds and mitoxantrone. Benefits of addition of vitamin D should be weighed against the risk of its toxicity.

Design of Lamivudine Loaded Nanoparticles for Oral Application by Nano Spray Drying Method: A New Approach to use an Antiretroviral Drug for Lung Cancer Treatment

2020 ◽  
Vol 23 (10) ◽  
pp. 1064-1079
Author(s):  
Ahmet Alper Öztürk ◽  
İrem Namlı ◽  
Kadri Güleç ◽  
Şennur Görgülü
Keyword(s):  
Lung Cancer ◽  
Cancer Treatment ◽  
Anticancer Activity ◽  
Cell Line ◽  
Anticancer Drugs ◽  
Release Kinetics ◽  
Prolonged Release ◽  
Lung Cancer Treatment ◽  
Anticancer Properties ◽  
Ft Ir

Aims: To prepare lamivudine (LAM)-loaded-nanoparticles (NPs) that can be used in lung cancer treatment. To change the antiviral indication of LAM to anticancer. Background: The development of anticancer drugs is a difficult process. One approach to accelerate the availability of drugs is to reclassify drugs approved for other conditions as anticancer. The most common route of administration of anticancer drugs is intravenous injection. Oral administration of anticancer drugs may considerably change current treatment modalities of chemotherapy and improve the life quality of cancer patients. There is also a potentially significant economic advantage. Objective: To characterize the LAM-loaded-NPs and examine the anticancer activity. Methods: LAM-loaded-NPs were prepared using Nano Spray-Dryer. Properties of NPs were elucidated by particle size (PS), polydispersity index (PDI), zeta potential (ZP), SEM, encapsulation efficiency (EE%), dissolution, release kinetics, DSC and FT-IR. Then, the anticancer activity of all NPs was examined. Results: The PS values of the LAM-loaded-NPs were between 373 and 486 nm. All NPs prepared have spherical structure and positive ZP. EE% was in a range of 61-79%. NPs showed prolonged release and the release kinetics fitted to the Weibull model. NPs structures were clarified by DSC and FT-IR analysis. The results showed that the properties of NPs were directly related to the drug:polymer ratio of feed solution. NPs have potential anticancer properties against A549 cell line at low concentrations and non-toxic to CCD 19-Lu cell line. Conclusion: NPs have potential anticancer properties against human lung adenocarcinoma cells and may induce cell death effectively and be a potent modality to treat this type of cancer. These experiments also indicate that our formulations are non-toxic to normal cells. It is clear that this study would bring a new perspective to cancer therapy.

Anticancer Activity and Topoisomerase II Inhibition of Naphthalimides with ω-Hydroxylalkylamine Side-Chains of Different Lengths

2019 ◽  
Vol 15 (5) ◽  
pp. 550-560
Author(s):  
Mateusz D. Tomczyk ◽  
Anna Byczek-Wyrostek ◽  
Klaudia Strama ◽  
Martyna Wawszków ◽  
Przemysław Kasprzycki ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Cell Lines ◽  
Inhibitory Activity ◽  
Topoisomerase Ii ◽  
Significant Activity ◽  
Anticancer Activities ◽  
Human Colon Cancer ◽  
Substitution Pattern ◽  
Topo Ii

Background: The substituted 1,8-Naphthalimides (1H-benzo[de]isoquinoline-1,3(2H)- diones) are known as DNA intercalators stabilizing DNA-Topoisomerase II complexes. This interaction disrupts the cleavage-relegation equilibrium of Topo II, resulting in formation of broken strands of DNA. Objective: To investigate the influence of type of substituents and substitution positions in 1,8- naphthalimde skeleton on the inhibition of Topoisomerase II activity. Methods: The starting 1,8-naphthalimide were prepared from acenaphthene by introduction of appropriate substituents followed by condensation with ω-hydroxylakylamines of different chain length. The substituents were introduced to 1,8-naphthalimide molecule by nucleophilic substitution of leaving groups like nitro or bromo present in 4 or 4,5- positions using the ω- hydroxylalkylamines. The bioactivity of obtained compounds was examined in model cell lines. Results: Antiproliferative activity of selected compounds against HCT 116 human colon cancer cells, human non-small cell lung cells A549 and non-tumorigenic BEAS-2B human bronchial epithelium cells was examined. Several of investigated compounds exhibit a significant activity (IC50 µM to 7 µM) against model cancer cell lines. It was demonstrated that upon treatment with concentration of 200 µM, all derivatives display Topo II inhibitory activity, which may be compared with activity of Amonafide. Conclusion: The replacement of the nitro groups in the chromophore slightly reduces its anticancer activities, whereas the presence of both nitro group and ω-hydroxylalkylamine chain resulted in seriously increased anticancer activity. Obtained compounds showed Topo II inhibitory activity, moreover, influence of the substitution pattern on the ability to inhibit Topo II activity and cancer cells proliferation was observed.

scholarly journals Increases of Lipophilic Antioxidants and Anticancer Activity of Coix Seed Fermented by Monascus purpureus

Foods ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 566
Author(s):  
Haiying Zeng ◽  
Likang Qin ◽  
Xiaoyan Liu ◽  
Song Miao
Keyword(s):  
Anticancer Activity ◽  
Radical Scavenging ◽  
Monascus Purpureus ◽  
Acid Oxidation ◽  
Anticancer Activities ◽  
Lipophilic Extract ◽  
Coix Seed ◽  
Before And After ◽  
Health Promoting ◽  
Human Laryngeal Carcinoma

Lipophilic tocols, γ-oryzanol, and coixenolide in coix seed before and after fermentation by Monascus purpureus were determined. Antioxidant and anticancer activities of raw and fermented coix seed were evaluated using free-radical-scavenging assays and polyunsaturated fatty acid oxidation model, and human laryngeal carcinoma cell HEp2, respectively. Compared to the raw seed, the tocols, γ-oryzanol, and coixenolide contents increased approximately 4, 25, and 2 times, respectively, in the fermented coix seed. Especially, γ-tocotrienol and γ-oryzanol reached 72.5 and 655.0 μg/g in the fermented coix seed. The lipophilic extract from fermented coix seed exhibited higher antioxidant activity in scavenging free radicals and inhibiting lipid oxidation. The inhibitory concentrations for 50% cell survival (IC50) of lipophilic extract from fermented coix seed in inhibiting HEp2 cells decreased by 42%. This study showed that coix seed fermented by M. purpureus increased free and readily bioavailable lipophilic antioxidants and anticancer activity. Therefore, fermentation could enhance the efficacy of the health promoting function of coix seeds.

scholarly journals Anticancer Activity of Triazolo-Thiadiazole Derivatives and Inhibition of AKT1 and AKT2 Activation

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 493
Author(s):  
Dimitrios T. Trafalis ◽  
Sofia Sagredou ◽  
Panayiotis Dalezis ◽  
Maria Voura ◽  
Stella Fountoulaki ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Human Colon ◽  
Tumor Xenograft ◽  
Atp Binding Site ◽  
Anticancer Properties ◽  
Extensive Range ◽  
Dependent Inhibition ◽  
Ht 29

The fusion of 1,2,4-triazole and 1,3,4-thiadiazole rings results in a class of heterocycles compounds with an extensive range of pharmacological properties. A series of 1,2,4-triazolo[3,4-b]-1,2,4-thiadiazoles was synthesized and tested for its enzyme inhibition potential and anticancer activity. The results show that 1,2,4-triazolo[3,4-b]-1,2,4-thiadiazoles display potent anticancer properties in vitro against a panel of cancer cells and in vivo efficacy in HT-29 human colon tumor xenograft in CB17 severe combined immunodeficient (SCID) mice. Preliminary mechanistic studies revealed that KA25 and KA39 exhibit time- and concentration-dependent inhibition of Akt Ser-473 phosphorylation. Molecular modeling experiments indicated that 1,2,4-triazolo[3,4-b]-1,2,4-thiadiazoles bind well to the ATP binding site in Akt1 and Akt2. The low acute toxicity combined with in vitro and in vivo anticancer activity render triazolo[3,4-b]thiadiazoles KA25, KA26, and KA39 promising cancer therapeutic agents.

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