Evaluation of the Antihyperglycemic efficacy of the roots of Ferula orientalis L.: An in vitro to in vivo assessment.

Decoctions of Ferula orientalis L. (Apiaceae), have been traditionally used to lower blood glucose levels (BGLs). After in vitro enzyme inhibition tests on the dichloromethane extracts of the roots (FOD) and the methanol extract of the roots (FOM), isolation studies were carried out on the FOD extract. The anti-hyperglycemic effects of the FOD extract and the pure compounds were studied in mice using the Oral Glucose Tolerance Test (OGTT) and streptozotocin (STZ)-induced diabetes mellitus (DM) models. Molecular docking studies were performed on potent compounds in the binding pockets of enzymes α-glucosidase and α-amylase. The isolations of 11 compounds were isolated from the FOD extract, which comprised teferidine (1), ferutinin (FT) (2), teferin (3), epoxy-jaeschkeanadiol-p-hydroxybenzoate (4), epoxy-jaeschkeanadiol-6-vanillate (5), tovarol-8-angelate (6), leucoferin (7), tovarol-8-p-hydroxybenzoate (8), tovarol-8-vanillate (9), 6-ß-p-hydroxybenzoyloxy-germacra-1(10),4-diene (10), and chimgin (11). Compounds 2 and 8-11 exhibited a higher inhibitory activity on α-glucosidase. In the OGTT, pretreatment with the FOD extract or compound 2 did not alter the BGLs after administration of the glucose solution compared to the control. In the STZ-induced diabetic mice model, no significant difference in the BGLs was observed with the FOD extract (200 mg/kg) or compound 2 (100 mg/kg)-treated diabetic mice compared to the diabetic control mice. The experimental studies all showed that the F. orientalis extract had significant effects on the enzyme systems involved in DM, and it would be appropriate to plan further studies on possible problems of bioavailability of the compound FT and the FOD extract, inadequate dose, and duration of administration.

Antiproliferative effects of Turkish pomegranate (Punica granatum L.) extracts on MCF-7 human breast cancer cell lines with focus on antioxidant potential and bioactive compounds analyzed by LC-MS/MS.

In this study, eight different pomegranate (Punica granatum L.) cultivars from Turkey were evaluated for their antioxidant and cytotoxic effects on the MCF-7 breast cancer cell lines and MCF-10A breast fibrocystic epithelial cell lines with a focus on their chemical compositions by LC-MS/MS. Cell lines were treated with pomegranate juice extracts in different doses at selected time intervals (24th, 48th, and 72nd hour). Afterwards, WST-1 cell proliferation assay was performed to investigate the cytotoxicity of the extracts. Accordingly, all extracts decreased the cell viability of MCF-7 breast cancer cell lines and had no cytotoxic effect on the cell viability of MCF-10A cell lines. Among eight extracts, P7 (Izmir 1513), which was rich in anthocyanins such as cyanidin chloride (69.76 ± 8.02 µg/g extract), cyanidin-3-O-glucoside (903.66 ± 101.89 µg/g extract), and punicalagin (992.09 ± 174.53 µg/g extract), was found to demonstrate the strongest cytotoxic activity on MCF-7 breast cancer cell lines by decreasing the cell viability in half at 24th hour with an IC50 value of 49.08 µg/ml. PRACTICAL APPLICATIONS: Eight commercially valuable pomegranate (Punica granatum) cultivars from Turkey were examined. Pelargonidin, cyanidin, cyanidin-3-O-gl, callistephin, and delphinidin-3-O-gl were quantified. Two cultivars (P1 and P3) showed comparatively higher antioxidant effects. A cultivar (P7) showed strongest cytotoxic activity against MCF-7 breast cancer cell line. The cultivars have potential to be used as natural antioxidant and anticancer agents.

Antioxidant activity of novel imidazo[2,1-b]thiazole derivatives: Design, synthesis, biological evaluation, molecular docking study and in silico ADME prediction.

A series of novel oxo-hydrazone and spirocondensed-thiazolidine derivatives of imidazo[2,1-b]thiazole were synthesized and evaluated for their antioxidant activity. The antioxidant activity of 18 newly synthesized compounds and 12 previously reported compounds bearing similar scaffold, were evaluated by three different methods: inhibition of FeCl3/ascorbate system-induced lipid peroxidation of lecithin liposome (anti-LPO), scavenging activity against ABTS radical and Ferric Reducing Antioxidant Power (FRAP) activity. 4h, 5h, and 6h displayed the highest anti-LPO and ABTS radical removal activity. Also, in FRAP analysis, 4i and 4a displayed the best activity. In addition to the in vitro analysis, docking studies targeting the active site of Human peroxiredoxin 5 (PDB ID: 1HD2) were employed to explore the possible interactions of these compounds with the receptor. Structure-activity relationships, as well as virtual ADME studies, were carried out and a relationship between biological, electronic, and physicochemical qualifications of the target compounds was determined.

Selective in vitro and in silico enzymes inhibitory activities of phenolic acids and flavonoids of food plants: Relations with oxidative stress.

In this study, the inhibitory potentials of food originated 34 phenolic acids, and flavonoid compounds were screened against acetylcholinesterase, butyrylcholinesterase, urease, and tyrosinase enzymes. All compounds included in this study exhibited high antioxidant activity with an ignorable cytotoxic activity. In general, they also showed poor anti-urease and anti-tyrosinase activities. Compounds in aglycone form (quercetin, myricetin, chrysin, and luteolin) showed strong anticholinesterase activities. No relation was observed between the tested bioactivities except from the case that aglycone compounds exhibited a strong positive relationship between antioxidant activities and anticholinesterase activity. Interestingly, there was a relation between the molecular weights of aglycone compounds and their anticholinesterase activities. The study showed that flavonoids with molecular mass of 250-320 g/mol have high potential of anticholinesterase activities and are valuable for future experiments on animals and humans. Potential inhibitory effects of these molecules on target proteins were investigated using docking and molecular dynamics calculations.

Antioxidant, Anti-acetylcholinesterase, Anti-inflammatory and DNA Protection Activities of Glaucium grandiflorum var. grandiflorum.

In this study, antioxidant, antiacetylcholinesterase, anti-inflammatory, and DNA protecting activities of the aerial parts of Glaucium grandiflorum var. grandiflorum were evaluated. The lyophilized methanolic extract of the aerial parts of G. grandiflorum var. grandiflorum was investigated for potential in-vitro antioxidant properties in thiobarbituric acid test using the lipid peroxidation of liposomes, ferric ion reducing antioxidant power (FRAP), 1,1-diphenyl-2-picrylhydrazyl,2,2'-azinobis(3-ethylbenzothiazoline-6-sulphonate) free-radicals and hypochlorous acid scavenging assays. The extract demonstrated antioxidant activity in all the assays. The (AChE) inhibition capacity of the lyophilized methanolic extract at 320 µg/mL (80.75 ± 1.59%) was found to be strong and almost equal to the inhibition capacity of the positive control, galantamine (82.23 ± 2.21%) at 25 µg/mL. The significant AChE inhibitory activity suggests that the extract may be beneficial in the treatment of Alzheimer's disease. The extract also showed inhibitory activity against plasmid DNA damage (94%), as well as COX-2 69.05%, which is a target for many anti-inflammatory and cancer-preventive drugs. These results indicate that G. grandiflorum var. grandiflorum methanolic extract is an excellent source of compounds with antioxidant, anti-acetylcholinesterase and anti-inflammatory properties that prevent DNA damage.

Carbon tetrachloride-induced kidney damage and protective effect of Amaranthus lividus L. in rats.

This study was designed to evaluate the protective effect of water extract of Amaranthus lividus L. (A. lividus) (Amaranthaceae) on carbon tetrachloride (CCl4)-induced toxicity in kidneys of rats. For this purpose, male albino Wistar rats were pretreated with A. lividus (250 and 500 mg/kg body weight (b.w.)) daily for 9 days and a single dose of CCl4 was applied intraperitoneally (50% in olive oil; 1.5 mL/kg b.w.) on the 10th day. All rats were killed 24 h after CCl4 administration, and kidneys were excised and used for determination of histopathological and biochemical parameters. CCl4 administration caused a remarkable increase in lipid peroxidation (LPO) and glutathione levels and glutathione-S-transferase, glutathione peroxidase, glutathione reductase, superoxide dismutase, myeloperoxidase (MPO) activities and a decrease in catalase (CAT) activity when compared to the control group. Pretreatment with A. lividus (250 and 500 mg/kg b.w.) significantly prevented the elevation in LPO level and MPO activity as well as protected the decrease in CAT activity but did not alter other biochemical parameters. The protective effect of A. lividus was further evident through the decreased histological alterations in kidneys. In conclusion, this study has indicated that A. lividus possesses protective and antioxidant effects against CCl4-induced oxidative kidney damage.

Antioxidant and antiacetylcholinesterase activities of Sorbus torminalis (L.) Crantz (wild service tree) fruits.

In this study, the antioxidant and antiacetylcholinesterase activities of Sorbus torminalis (L.) Crantz fruits were evaluated. Total phenolic and flavonoid compounds, 2,2'-azino-bis (3-ethylbenzothioazoline-6-sulfonic acid), 2,2'-diphenyl-1-picrylhydrazyl, and superoxide anion radicals scavenging activities and ferric-reducing antioxidant power of water, ethyl acetate, acetone, and methanol extracts were determined for the measurement of the antioxidant activity. Quercetin and α-tocopherol were used as standard antioxidants. The inhibitory effect of the water extract on acetylcholinesterase (AChE) was evaluated using the Ellman method and galantamine was used as a standard. Water extract had the highest total phenolic concentration and the strongest antioxidant activity followed by ethyl acetate and acetone extracts whereas methanol extract has the lowest phenolics and weakest antioxidant activity. Moreover, water extract showed moderate ability to inhibit AChE. It was concluded that fruits of S. torminalis have antioxidant and anti-AChE activities and that the plant might be a natural source of antioxidants and AChE inhibitors.

Ameliorative effect of vanadium on oxidative stress in stomach tissue of diabetic rats.

Between their broad spectrum of action, vanadium compounds are shown to have insulin mimetic/enhancing effects. Increasing evidence in experimental and clinical studies suggests that oxidative stress plays a major role in the pathogenesis of diabetes and on the onset of diabetic complications. Thus, preventive therapy can alleviate the possible side effects of the disease. The aim of the present study was to investigate the effect of vanadyl sulfate supplementation on the antioxidant system in the stomach tissue of diabetic rats. Male Swiss albino rats were randomly divided into 4 groups: control; control+vanadyl sulfate; diabetic; diabetic+vanadyl sulfate. Diabetes was induced by intraperitoneal injection of streptozotocin (STZ; 65 mg/kg body weight). Vanadyl sulfate (100 mg/kg body weight) was given daily by gavage for 60 days. At the last day of the experiment, stomach tissues were taken and homogenized to make a 10% (w/v) homogenate. Catalase (CAT), superoxide dismutase (SOD), glutathione reductase (GR), glutathione peroxidase (GPx), glutathione-S-transferase (GST), myeloperoxidase (MPO), carbonic anhydrase (CA), glucose-6-phosphate dehydrogenase (G6PD) and lactate dehydrogenase (LDH) activities were determined in the stomach tissue. CAT, SOD, GR, GPx, GST, CA, G6PD and LDH activities were increased in diabetic rats when compared to normal rats. Vanadium treatment significantly reduced the elevated activities of GR, GPx, GST compared with the diabetic group whereas the decreases in CAT, SOD, CA, G6PD and LDH activities were insignificant. No significant change was seen for MPO activity between the groups. It was concluded that vanadium could be used for its ameliorative effect against oxidative stress in diabetes.