1-1-diphenyl-2-picrylhydrazyl and Colorectal-Neoplasms

Strawberry tree (. Med obične planike (

Topics: Antineoplastic Agents; Antioxidants; Biphenyl Compounds; Caco-2 Cells; Carcinoma, Hepatocellular; Carcinoma, Squamous Cell; Chromans; Colorectal Neoplasms; Ericaceae; Gallic Acid; Hep G2 Cells; Homogentisic Acid; Honey; Humans; Iron; Liver Neoplasms; Phenols; Picrates; Plant Extracts; Reactive Oxygen Species; Tongue Neoplasms; Trees

The Peucedanum species have many pharmacological effects due to the presence of coumarins, flavonoids, phenolic compounds, and essential fatty acids in these species. In this study, for the first time, the anticancer activity of Peucedanum chenur methanolic extract via the induction of apoptosis and inhibition of invasion in HCT-116 human colon cancer cells was investigated.. P. chenur methanolic extract effect on HCT-116 cells viability and antioxidant activity were evaluated using MTT assay, 1,1-Diphenyl-2-picrylhydrazyl, and iron chelating tests, respectively. Changes in mRNA expression level in a panel of relevant genes were assessed by the quantitative real-time PCR. Also, apoptosis was assessed by cell cycle analysis and Annexin V/PI (propidium iodide) method, and the effect on cell migration was tested using scratch test.. P. chenur methanolic extract increased significantly the expression of BAX while decreased the expression of BCL-2, AKT1, FAK, RhoA, and matrix metalloproteinase (MMP) genes compared to the control group. BAX/BCL-2 ratio and apoptosis elevated, whereas cell migration reduced significantly. Besides, our extract showed an appropriate antioxidant activity.. P. chenur may be introduced as a new chemopreventive agent in medicine due to its notable power in terms of induction of apoptosis and inhibition of invasion.

Topics: Antineoplastic Agents, Phytogenic; Antioxidants; Apiaceae; Apoptosis; Biphenyl Compounds; Cell Line, Tumor; Cell Migration Assays; Cell Survival; Colorectal Neoplasms; DNA, Neoplasm; Free Radical Scavengers; G1 Phase; Gene Expression Regulation, Neoplastic; Humans; Iron Chelating Agents; Methanol; Neoplasm Invasiveness; Neoplasm Proteins; Picrates; Plant Components, Aerial; Plant Extracts

This study subjected a rat model to the extracts of muscle and shell tissues from Portunus segnis to assess their therapeutic effects on the HT-29 colon cancer cells as well as on colonic Aberrant Crypt Foci (ACF) induced by Azoxymethane (AOM).. The cell line was exposed to the extracts to compare the cytotoxicity of hexane, butanol, ethyl acetate, and water extract of muscle and ethanolic extract of the shell. Male rats (n=40) were assigned into control, positive, negative, and treatment groups. The animals were injected with AOM, except the control group, and then exposed to 250 and 500mg/kg of the crude extracts. Immunohistochemical localization of Bax and Bcl-2, as well as ACF and antioxidant enzymes, were evaluated in the rat colon.. The butanolic muscle extract and ethanolic shell one demonstrated an IC50 of 9.02±0.19μg/ml and 20.23±0.27μg/ml towards the cell line, respectively. Dietary exposure inhibited the ACF formation and crypt multiplicity in the colon compared to the cancer control group. The activity of SOD and CAT increased, while that of MDA decreased. The expression of Bax and Bcl-2 increased and decreased, respectively.. Taken together, the results show that both extractions were suggested to be suppressive to AOMinduced colon cancer.

Topics: Aberrant Crypt Foci; Animals; Antineoplastic Agents; Antioxidants; Azoxymethane; Biphenyl Compounds; Brachyura; Cell Proliferation; Colorectal Neoplasms; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; Injections, Intradermal; Male; Molecular Structure; Muscles; Neoplasms, Experimental; Picrates; Rats; Rats, Wistar; Structure-Activity Relationship; Tumor Cells, Cultured

In this study, 15 commercial acidic drugs have been evaluated for pancreatic lipase (PL) inhibitory activity using an in vitro spectrophotometric method. The acidity was the basis of selection, since most PL inhibitors exhibit acidic groups and high lipophilicity. Orlistat was the robust reference agent for potency and efficacy determinations. In comparison to the cisplatin, the evaluation of the antineoplastic activities of selected drugs in a panel of colorectal cancer cell lines (HT-29, HCT-116, SW620, CACO-2, and SW480) and normal periodontal ligament fibroblasts for safety examination was performed by using a sulforhodamine procuring ascorbic acid as a reference in diphenyl-2-picryl-hydrazyl assay of radical scavenging properties was performed. This research revealed three highly acidic pharmacological classes with reasonable PL inhibitory activity in comparison to orlistat out of 15 selected drugs, namely sulfonylureas, fluoroquinolones, and proton pump inhibitors. Docking studies supported the hypothesis of a selection based on acidity, since it showed that the sulfonamide acid group (glyburide) is a remarkably potent interacting group with the enzyme. Failing to fulfill other structure-activity relationship requirements (lipophilicity) led to weak activity. Since the drugs are of different chemical classes with unknown mechanisms, they showed diverse antiproliferative activity. Some drugs such as atorvastatin and gemifloxacin showed higher antiproliferative activity than cisplatin with high-safety profiles against SW620 and SW480 cell lines, respectively, whereas lansoprazole and clopidogrel revealed comparable activity to cisplatin against HCT-116 and SW480, respectively. Unfortunately, selected tested drugs exhibited negligible radical scavenging activity versus ascorbic acid. Hit, Lead & Candidate Discovery.

Topics: Antineoplastic Agents; Biphenyl Compounds; Cell Line, Tumor; Cell Proliferation; Colorectal Neoplasms; Fibroblasts; Free Radical Scavengers; Humans; Lipase; Molecular Docking Simulation; Obesity; Picrates

In pursuit of a novel approach in colon cancer therapy, we explored the ability of ruthenium baicalein complex to eradicate colon cancer by efficiently targeting various apoptotic pathways on human colon cancer cell line and on a DMH and DSS induced murine model of colorectal cancer. In this study, we provide direct proof of the chemotherapeutic potential of the ruthenium baicalein complex by activating p-53 dependent intrinsic apoptosis and modulating the AKT/mTOR and WNT/β- catenin pathways. The ruthenium baicalein complex was synthesized and its characterizations were accomplished through various spectroscopic techniques followed by assessment of antioxidant potential by DPPH, FRAP, and ABTS methods.

Topics: Animals; Antineoplastic Agents; Apoptosis; beta Catenin; Biphenyl Compounds; Catalase; Cell Proliferation; Colonic Neoplasms; Colorectal Neoplasms; Flavanones; Glutathione; HT29 Cells; Humans; Male; Picrates; Proto-Oncogene Proteins c-akt; Rats; Rats, Sprague-Dawley; Ruthenium; Superoxide Dismutase; TOR Serine-Threonine Kinases

Oxidative stress has been proposed to be involved in colorectal cancer development. Many dark pigments of plants have potent oxidative stress preventive properties. In this study, unpolished Thai rice was assessed for antioxidant activity using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) methods. Red strain unpolished Thai rice was also administered to rats exposed to azoxymethane (AOM) for induction of aberrant crypt foci (ACF). Serum malondialdehyde (MDA) and ferric reducing antioxidant power (FRAP) were investigated for cellular oxidative stress and serum antioxidants, respectively. Red pigment unpolished Thai rice demonstrated high antioxidant activity and was found to significantly and dose dependently decrease the total density and crypt multiplicity of ACF. Consumption of Thai rice further resulted in high serum antioxidant activity and low MDA cellular oxidative stress. Interestingly, the density of ACF was strongly related to MDA at r=0.964, while it was inversely related with FRAP antioxidants (r=-0.915, p<0.001). The results of this study suggest that the consumption of red strain of unpolished Thai rice may exert potentially beneficial effects on colorectal cancer through decrease in the level of oxidative stress.

Topics: Aberrant Crypt Foci; Animals; Antioxidants; Azoxymethane; Benzothiazoles; Biphenyl Compounds; Colorectal Neoplasms; Male; Malondialdehyde; Oryza; Oxidative Stress; Phytotherapy; Picrates; Plant Extracts; Rats; Rats, Sprague-Dawley; Sulfonic Acids; Thiazoles