Anti-hyperglycaemic Activity of Tribulus terrestris L Aerial Part Extract in Glucose-loaded Normal Rabbits

Purpose: To investigate the anti-hyperglycaemic activity of methanol extract of Tribulus terrestris L. Zygophyllaceae in glucose-loaded normal rabbits.Methods: The animals were randomly assigned to 4 groups (n = 5) and treated with a single oral dose. Group 1 served as normal control group and received distilled water; group 2 served as hyperglycaemic control; group 3 was treated with glibenclamide (5 mg/kg, aqueous suspension) and served as reference standard; group 4 received methanol extract of Tribulus terrestris L. (250 mg/kg). Groups 3 and 4 were orally treated with glucose (5 g/kg) after 1 h of drug and extract administration, respectively. Fasting blood glucose (FBG) was determined prior to (0 h) and at 30 min, 1, 2 and 3 h after dosing for acute toxicity study.Results: On comparing within groups, a single dose of the methanol extract of Tribulus terrestris L. lowered FBG to levels comparable to that of glibenclamide (36 vs. 55 %), and reaching the initial level (0 h) at 2 h. FBG were significantly (p < 0.05) lowered at 2 and 3 h in both glibenclamide (45.5 and 56.9 %) and extract (45.7 and 52.7 %) groups as compared with their respective glucose levels at 0.5 h. On the other hand, on comparing between groups, both glibenclamide and methanol extract significantly (p < 0.05, p < 0.001) lowered the rise in blood glucose at 1 h (33.9 and 22.5 %), 2 h (62.8 and 59.16 %), and 3 h (64.6 and 57.1 %) with respect to the hyperglycaemic control group.Conclusion: The methanol extract of the aerial parts of Tribulus terrestris L. possesses potential antihyperglycaemic activity in glucose loaded normal rabbits. Further studies on various organic solvents fractions and isolated compounds from this plant are required.Keywords: Tribulus terrestris L., Zygophyllaceae, Anti-hyperglycaemic activity, Fasting blood glucose, Acute toxicit

Hypoglycaemic Activity of Acalypha fruticosa Forssk Extracts in Normal Rabbits

Purpose: To investigate the hypoglycaemic activity of various extracts of the aerial part of Acalypha fruticosa in normal rabbits.Methods: The rabbits were randomly assigned to 8 groups (n = 3) and treated with a single oral dose. Group 1 served as normal control and received 2 % dimethyl sulfoxide (DMSO, 3 ml/kg); group 2 served as standard  treatment and received metformin (300 mg/kg); groups 3 - 8 received different extracts of Acalypha fruticosa at a dose of (600 mg/kg) as follows: group 3, total methanol extract; group 4, Petroleum ether (PET) extract; group 5, chloroform extract; group 6, ethyl acetate extract; group 7, nbutanol extract; and group 8, aqueous extract. Serum glucose (fasting blood glucose, FBG) was determined using a diagnostic kit on a glucose analyzer.Results: A single dose of the aqueous extract of Acalypha fruticosa significantly lowered (p < 0.5) FBG at 1, 2, 4, and 6 h by 16, 29.5, 19.8, and 23.9 %, respectively, compared with normal control group, whereas standard treatment (metformin) did not affect FBG at all of these time-points measured. Furthermore, the aqueous extract (AEA) lowered FBG at 1, 2, 4, and 6 h by 24, 34.4, 25.9, and 17 %, respectively (p < 0.5), compared with  metformin treatment. Chloroform extract also significantly lowered FBG at 1, 2, and 4 h by 17.3, 24.8, and 14.7 %, respectively, compared to metformin treatment (p <0.5).Conclusion: The results of this study show that the aqueous extract of the aerial parts of Acalypha fruticosa possess potential hypoglycaemic activity but further studies are required to elucidate the exact mechanisms of action

Hepatoprotective Effect of Pandanus odoratissimus L Inflorescence Extracts in Acetaminophen-treated Guinea Pigs

Purpose: To investigate the hepatoprotective activity of methanol extracts of peduncles, flowers and spathes of Pandanus odoratissimus L. inflorescence in acetaminophen-induced hepatotoxicity in guinea pigs.Methods: The animals were randomly assigned to 9 groups (3 animals per group) and treated orally for 10 consecutive days. Group 1 served as normal control and received distilled water (1 ml/kg); groups 2 - 4 received methanol extracts of peduncle, flower, and spathes of P. odoratissimus L. (500 mg/kg), respectively, in the absence of acetaminophen (APAP); group 5 served as hepatotoxic control and received APAP (3 g/kg) on days 1 and 2; group 6 served as standard treatment group and received silymarin (100 mg/kg) + 3 g/kg APAP on days 1 and 2; groups 7 - 9 received methanol extracts of peduncle, flower, and spathes of P. odoratissimus L. (500 mg/kg) respectively + 3 g/kg APAP on days 1 and 2. Serum enzyme activities (AST, ALT, ALP) and total bilirubin were determined. Histopathological examinations of the liver were also carried out.Results: The methanol extract of the peduncle alleviated the liver damage induced by APAP as evident by the improved histopathology picture similar to that of silymarin which presented with only mild hydropic and fatty changes. The extract also reduced the liver enzymes - AST, ALT and ALP - by 42, 50 and 59 %, respectively (p < 0.05), but the reduction (32 %) in total bilirubin was not significant 32 %. On the other hand, the flower extract only lowered AST and ALP by 31 and 48 % (p < 0.05), respectively, while the reduction in ALT and total bilirubin by 33 and 18 % respectively, was not significant.Conclusion: P. odoratissimus L. peduncle has potential hepatoprotective activity against APAPinduced hepatotoxicity in guinea pigs.Keywords: Pandanus odoratissimus L., Peduncle, Flowers, Hepatoprotection, Acetaminophen, Guinea pig

Isolation, biological evaluation and validated HPTLC-quantification of the marker constituent of the edible Saudi plant Sisymbrium irio L.

AbstractPhytochemical investigation and chromatographic purification of the n-hexane fraction of the aerial parts of the edible Saudi plant Sisymbrium irio led to the isolation of β-sitosterol (1), stigmasterol (2) and β-sitosterol-β-d-glucoside (3). The cytotoxic effects of the n-hexane, dichloromethane, ethyl acetate and n-butanol fractions were tested against three cancer cell lines viz., MCF-7, HCT-116 and HepG2, using the crystal violet staining (CVS) method, while the antibacterial activity against a number of pathogenic bacterial strains, was also estimated using the broth microdilution assay. The n-hexane fraction showed potent cytotoxic activities against all tested human cancer cell lines (IC50: 11.7–13.4μg/mL), while the dichloromethane fraction was particularly potent against HCT-116 cells (IC50: 5.42μg/mL). On the other hand, the n-hexane and EtOAc fractions demonstrated significant inhibitory activities against the Gram positive bacteria S. pyogenes and C. perfringens; and the Gram negative bacterium S. enteritidis. Our results warrant the therapeutic potential of S. irio as nutritional supplement to reduce the risk of contemporary diseases. Additionally, a validated high performance thin-layer chromatography (HPTLC) method was developed for the quantitative analysis of biomarker β-sitosterol glucoside (isolated in high quantity) from the n-hexane fraction. The system was found to furnish a compact, sharp, symmetrical and high resolution band for β-sitosterol glucoside (Rf=0.43±0.002). The limit of detection (LOD) and limit of quantification (LOQ) for β-sitosterol glucoside was found to be 21.84 and 66.18ngband−1, respectively. β-sitosterol glucoside was found to be present only in n-hexane fraction (2.10μg/mg of dried fraction) while it was absent in the other fractions of S. irio which validated the high cytotoxic and antibacterial activity of n-hexane fraction of S. irio

Portulaca oleracea Linn seed extract ameliorates hydrogen peroxide-induced cell death in human liver cells by inhibiting reactive oxygen species generation and oxidative stress

Purpose: To investigate the protective effects of Portulaca oleracea seed extract (POA) against cytotoxicity, oxidative stress and reactive oxygen species (ROS) generation induced by hydrogen peroxide (H2O2) in human liver cells (HepG2).Methods: The extract (POA) was obtained by ethanol extraction of P. oleracea seeds. Cytotoxicity in HepG2 cells was assessed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay, neutral red uptake (NRU) assay and morphological changes. The cells were pre-exposed to noncytotoxic concentrations (5 - 25 μg/mL) of POA for 24 h, and then cytotoxic (0.25 mM) concentration of H2O2. After 24 h of exposure, MTT and NRU assays were used to evaluate cell viability, while morphological changes were assessed using phase contrast inverted microscopy. The effect of POA on reduced glutathione (GSH) level, lipid peroxidation (LPO), and ROS generation induced by H2O2 was also studied.Results: The results showed that pre-exposure to POA (25 μg/mL) significantly (p <0.01) attenuated the loss of cell viability by up to 38 % against H2O2-induced oxidative stress and ROS generation. In addition, POA (25 μg/mL) significantly (p <0.01) increased GSH level (31 %), but decreased the levels of LPO (37 %) and ROS generation (49 %).Conclusion: This study demonstrates that POA has the capacity to protect HepG2 cells against H2O2- induced cell death by inhibiting oxidative stress and ROS generation.Keywords: Portulaca oleracea, HepG2 cells, Cytotoxicity, Oxidative stress, Reactive oxygen specie

Evaluation of circulating microparticles in healthy medical workers occupationally exposed to ionizing radiation: A preliminary study

Objectives Ionizing radiation was known to cause disruption of cytoskeleton. However, the disorganization of the cytoskeleton leads to form microparticles (MP) that carry membrane and cytoplasmic constituents from their parent cells they are released from. Therefore, authors investigated the effect of the occupational exposure to low doses of ionizing radiation on MP levels. Material and Methods The current study was conducted on 38 healthy medical workers occupationally exposed to low doses of ionizing radiation and 29 controls matched by gender, age, and smoking habits. The MP levels measured by flow cytometry were classified as positive or negative phosphatidylserine (PS + or PS – ), and phenotyped according to their cellular origin. Results Total MP (PS–/PS+) levels, regardless of phenotype, were significantly higher in workers occupationally exposed to ionizing radiation than in healthy individuals (p = 0.0004). Negative phosphatidylserine microparticles were predominant in medical exposed workers and, to a lesser extent, in controls (68% and 57%, respectively). With regard to phenotypic characterization of cellular origin, MP derived from platelets (CD41a+), endothelial (CD146+), leucocytes (CD45+) and erythrocytes (CD235a+) MP were significantly enhanced in exposed workers compared with controls (p < 0.0001). However, no significant difference was found in the proportion of the other blood elements in the peripheral circulation between the 2 groups. Serum levels of C-reactive protein were normal for all individuals. In addition, no association was observed between MP levels and the studied confounding factors. Conclusions The results suggest that elevated circulating MP levels represent an indicator of cellular damage caused by medical exposure to low doses of ionizing radiation. By consequence, the quantification of MP seems to be a useful biomarker for assessing the negative effects of occupational exposure to ionizing radiation. Int J Occup Med Environ Health 2018;31(6):783–79

Rosiglitazone, a Peroxisome Proliferator-Activated Receptor-γ Agonist, Prevents Microparticle-Induced Vascular Hyporeactivity through the Regulation of Proinflammatory Proteins

Microparticles are plasma membrane vesicles with procoagulant and proinflammatory properties. We recently demonstrated that microparticles induce vascular hyporeactivity and evoke up-regulation of proinflammatory protein expression. This study dissected the effect of either in vitro treatment or short-term oral administration of the peroxisome proliferator-activated receptor-γ (PPARγ) agonist, rosiglitazone, on microparticle-induced vascular hyporeactivity of mouse vessels. Microparticles were produced from T cells by actinomycin D treatment. The effects of rosiglitazone on mouse aortic rings incubated with microparticles were investigated. Aortae treated in vitro with rosiglitazone or aortae taken from mice treated by oral administration of the same agonist completely prevented microparticle-induced vascular hyporeactivity in response to U46619 [9,11-dideoxy-11α, 9α-epoxymethanoprostaglandin F2α). These effects of rosiglitazone occurred independently of the presence of endothelium without modifications in blood parameters. The mechanisms involved abrogation of nitric oxide (NO) and prostacyclin overproduction linked to up-regulation of inducible NO-synthase and cyclooxygenase 2 elicited by microparticles. In addition, rosiglitazone treatment reduced the ability of microparticles to evoke increases in interleukin (IL)-6, IL-8, and nuclear factor (NF)-κB transcription, and NF-κB expression and activation. These results suggest that rosiglitazone, via PPARγ activation, counteracts vascular dysfunction associated with increased release of proinflammatory proteins elicited by microparticles. They underscore therapeutic perspective for rosiglitazone in vascular diseases involving enhanced participation of microparticles

Assessment of selected Saudi and Yemeni plants for mosquitocidal activities against the yellow fever mosquito Aedes aegypti

© 2019 by the authors. Marine organisms are recognized as a source of compounds with interesting biological activities. Vibrio neocaledonicus has been reported on for its high effectiveness against corrosion in metals but it has been little studied for its chemical and biological activities. In this study, four compounds were isolated from V. neocaledonicus: indole (1); 1H-indole-3-carboxaldehyde (2); 4-hydroxybenzaldehyde (3) and Cyclo (-Pro-Tyr) (4); using a bioassay-guided method, since in a previous study it was found that the ethyl acetate extract was active on the enzymes acetylcholinesterase (AChE), alpha-glucosidase (AG) and xanthine oxidase (XO). The inhibitory activities of the three compounds against AChE, AG and XO was also evaluated. In addition, the enzymatic inhibitory activity of indole to the toxins from the venom of Bothrops asper was tested. Results showed that indole exhibited strong inhibitory activity to AG (IC50 = 18.65 ± 1.1 µM), to AChE, and XO (51.3% and 44.3% at 50 µg/mL, respectively). 1H-indole-3-carboxaldehyde displayed strong activity to XO (IC50 = 13.36 ± 0.39 µM). 4-hydroxybenzaldehyde showed moderate activity to XO (50.75% at 50 µg/mL) and weak activity to AChE (25.7% at 50 µg/mL). Furthermore, indole showed a significant in vitro inhibition to the coagulant effect induced by 1.0 µg of venom. The findings were supported by molecular docking. This is the first comprehensive report on the chemistry of V. neocaledonicus and the bioactivity of its metabolites