1-1-diphenyl-2-picrylhydrazyl and Liver-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

In the current medical era, spirooxindole motif stands out as a privileged heterospirocyclic scaffold that represents the core for a wide range of bioactive naturally isolated products (such as Strychnofoline and spirotryprostatins A and B) and synthetic compounds. Interestingly, no much attention has been paid to develop spirooxindole derivatives with dual antioxidant and anticancer activities. In this context, a series of spirooxindoles 6a-p was examined for their anticancer effect towards HepG2 hepatocellular carcinoma and PC-3 prostate cancer cell lines. Spirooxindole 6a was found to be an efficient anti-proliferative agent towards both HepG2 and PC-3 cells (IC50 = 6.9 and 11.8 µM, respectively). Afterwards, spirooxindole 6a was assessed for its apoptosis induction potential in HepG2 cells, where its pro-apoptotic impact was approved via the significant elevation in the Bax/Bcl-2 ratio and the expression levels of caspase-3.

Topics: Antineoplastic Agents; Antioxidants; Apoptosis; Biphenyl Compounds; Carcinoma, Hepatocellular; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Hep G2 Cells; Humans; Liver Neoplasms; Molecular Structure; Oxindoles; PC-3 Cells; Picrates; Spiro Compounds; Structure-Activity Relationship; Tumor Cells, Cultured

Nineteen organoselenides were synthesized and tested for their intrinsic cytotoxicity in hepatocellular carcinoma (HepG2) and breast adenocarcinoma (MCF-7) cell lines and their corresponding selective cytotoxicity (SI) was estimated using normal lung fibroblast (WI-38) cells. Most of the organic selenides exhibited good anticancer activity, and this was more pronounced in HepG2 cells. Interestingly, the naphthoquinone- (5), thiazol- (12), and the azo-based (13) organic selenides demonstrated promising SI (up to 76). Furthermore, the amine 4c, naphthoquinone 5, and azo-based 13 and 15 organic selenides were able to down-regulate the expression of Bcl-2 and up-regulate the expression levels of IL-2, IL-6 and CD40 in HepG2 cells compared to untreated cells. Moreover, most of the synthesized candidates manifested good free radical-scavenging and GPx-like activities comparable to vitamin C and ebselen. The obtained results suggested that some of the presented organoselenium candidates have promising anti-HepG2 and antioxidant activities.

Topics: Antineoplastic Agents; Antioxidants; Biphenyl Compounds; Breast Neoplasms; Carcinoma, Hepatocellular; Cell Line; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Female; Hep G2 Cells; Humans; Liver Neoplasms; MCF-7 Cells; Molecular Structure; Organoselenium Compounds; Picrates; Structure-Activity Relationship

This study was conducted to investigate the antioxidant, antibacterial, and antiproliferative activities of flesh free (FF), flesh bound (FB), peel free (PF), and peel bound (PB) phenolics from Fuji apple. The PB, which had highest total phenolic contents (126.15 ± 2.41 mg/100 g wet weight) and lowest total carbohydrate contents (34.68 ± 2.78 mg/100 g wet weight), showed the strongest 2,2'-azinobis-(3-ethylbenthiazoline-6-sulphonate) (ABTS) radical scavenging activity (EC50 = 0.36 ± 0.02 mg/mL), 1,1-diphenyl-2-picryhydrazyl (DPPH) radical scavenging activity (EC50 = 0.26 ± 0.01 mg/mL), and ferric reducing antioxidant power (Ferric reducing antioxidant power; EC50 = 0.19 ± 0.02 mg/mL) compared with those of FF, FB, and PF. The PB also showed the strongest antibacterial activities on Escherichia coli, Staphylococcus aureus, and Listeria monocytogenes and it also showed the highest antiproliferative effects on Caco-2 human colonic cancer cell (EC50 = 1.44 ± 0.01 mg/mL) and Hela human cervical cell (EC50 = 2.81 ± 0.01 mg/mL). Both free and bound phenolics from Fuji apple showed good antioxidant, antibacterial, and antiproliferative activities in our study, and bound phenolics had significantly higher activities compared with those of free phenolics.

Topics: Anti-Bacterial Agents; Antineoplastic Agents, Phytogenic; Antioxidants; Bacteria; Biphenyl Compounds; Caco-2 Cells; Cell Proliferation; Colonic Neoplasms; Escherichia coli; Fruit; HeLa Cells; Humans; Listeria monocytogenes; Liver Neoplasms; Malus; Phenols; Phytotherapy; Picrates; Plant Extracts; Staphylococcus aureus

Liver cancer is one of the highest rate diseases in southeastern Asia. Recently, many of functional foods and alternative medicines are very popularly utilized to prevent chronic diseases and cancer in Taiwan. In this study, we wanted to select and develop some of novel effectual agents or phytochemicals of γ-mangostin for clinical management or prevent hepatocellular carcinoma cell (HCC).. Lipid peroxidation (LPO) is an autocatalytic mechanism which induced tissue injure and carcinogenesis. In this study, the inhibitory activity of γ-mangostin on oxidative damage induced rat mitochondria LPO, the free radical scavenging of γ-mangostin and the apoptotic effects of γ-mangostin on HepG2 cells were investigated.. γ-Mangostin processed activity to inhibit LPO and scavenge 2,2-diphenyl-1-picrylhydrazyl. γ-Mangostin showed antiproliferative activity and induced nuclear condensation and apoptotic bodies appearance under Giemsa staining by microscopic observation. In addition, γ-mangostin showed increases of hypodiploid cells via propidium iodide, 2'7'-dichlorofluorescein diacetate, and 3,3'-dihexyloxacarbocyanine iodide staining by flow cytometry analysis in HepG2 cells.. γ-Mangostin has demonstrated free radical scavenging activity, and antiproliferative and apoptotic activity in HepG2 cells. The proof suggests that γ-mangostin is a lead compound candidate for clinical management or prevent HCC.

Topics: Animals; Antineoplastic Agents, Phytogenic; Antioxidants; Apoptosis; Biphenyl Compounds; Carcinoma, Hepatocellular; Cell Nucleus; Fruit; Garcinia mangostana; Hep G2 Cells; Humans; Lipid Peroxidation; Liver Neoplasms; Male; Phytotherapy; Picrates; Plant Extracts; Rats; Rats, Sprague-Dawley; Xanthones

The optimal culture conditions of exopolysaccharides (EPS) production in submerged culture medium by Stropharia rugosoannulata 2# were determined using the orthogonal matrix method. The optimal defined medium (per liter) was 60.0 g sucrose, 6.0 g tryptone, 5 mM KH₂PO₄, and initial pH 7.0 at 28°C. In the optimal culture medium, the maximum EPS production was 9.967 g/L in shake-flask culture. One fraction of EPS was purified from the culture filtrates by size exclusion chromatography (SEC), and the molecular characteristics were examined by a multiangle laser-light scattering (MALLS) and refractive index (RI) detector system. The weight-average molar masses and the polydispersity ratio of the EPS fraction were determined to be 5.305 × 103 g/mol and 2.014, respectively. FTIR spectroscopy was used for obtaining vibrational spectra of the purified EPS fraction. The obvious characteristic absorption at 884.3 cm-1 revealed the existence of β configuration. Furthermore, the experiments in vitro indicated that S. rugosoannulata 2# EPS exhibit high antitumor and antioxidative effects.

Topics: Antineoplastic Agents; Basidiomycota; Biphenyl Compounds; Carcinoma, Hepatocellular; Free Radical Scavengers; Fungal Polysaccharides; Hep G2 Cells; Humans; Hydrogen-Ion Concentration; Liver Neoplasms; Picrates; Temperature

The intent of this study was to purify and characterize a polysaccharide named LA from the fruiting bodies of the edible mushroom Pleurotus abalones.. The 120-kDa polysaccharide was obtained by extraction with boiling water, ethanol precipitation, ion exchange chromatography on Diethylaminoethyl-cellulose and gel filtration on Sephadex G-200.. The LA was composed of glucose, rhamnose, glucuronic acid, xylose, galactose and arabinose in the molar ratio of 26.3:2.7:1:1.4:1.8:1.2. The FITR and 1H-NMR spectrum of LA disclosed that it was a saccharide with an α-configuration. Its 13C-NMR spectrum revealed that its main chain was [→6)-α-D-Gly(1→]n. The LA exhibited antioxidant activities, especially in scavenging 1,1- diphenyl-2-picryl-hydrazyl radicals and hydroxyl radicals. It manifested antiproliferative activity towards breast cancer MCF7 cells with an IC50 of 3.7 µm, and also exerted some antiproliferative activity against HepG2 cells. It manifested a hypoglycemic action on diabetic mice. It inhibited HIV-1 reverse transcriptase with an IC50 of 8.7 × 10(-2) µm.. The polysaccharide from the abalone mushroom.

Topics: Antineoplastic Agents; Antioxidants; Biological Products; Biphenyl Compounds; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Diabetes Mellitus; Female; Fruiting Bodies, Fungal; Hep G2 Cells; HIV Reverse Transcriptase; Humans; Hydroxyl Radical; Hyperglycemia; Hypoglycemic Agents; Inhibitory Concentration 50; Liver Neoplasms; Phytotherapy; Picrates; Pleurotus; Polysaccharides; Reverse Transcriptase Inhibitors