Gamal A. Soliman

Novel flavonoids with antioxidant activity from a Chenopodiaceous plant

Objective: Atriplex lentiformis (Torr.) S.Wats (Chenopodiaceae) is a wild plant which is in use by Bedouin in treatment of general fatigue, therefore, there is a need to explore the potential antioxidant activity of the extracts and isolated compounds of this plant. Methods: Column chromatography and spectroscopic analysis were used for isolation and identification of the compounds. The antioxidant activity was evaluated in vitro using the ABTS•+ (2,2′-azino-bis-3-ethyl-bezthiazoine-6-sulphuric acid) radical scavenging model. Liver and kidney functions were investigated after oral administration of total alcohol, successive extracts, and isolated compounds. Results: Two new flavonoids, quercetin-6,4′-dimethoxy-3-fructo-rhamnoside 1 and quercetin-4′-methoxy-3-fructo-rhamnoside 2 in addition to five known compounds (kaempferol-4′-methoxy-3-rutinoside 3, kaempferol-7-O-rhamnoside 4, kaempferol-3,7-O,O-dirhamnoside 5, quercetin 6, and kaempferol 7) were isolated. Oral administration of total ethanol, diethyl ether, chloroform, ethyl acetate and n-butanol extracts showed no signs of toxicity up to (5 g/kg. b.wt.). All extracts and isolated compounds showed varied antioxidant activity ranged from 129 to 952 µmol Trolox equivalent/gram dry weight with maximum level for the two new isolated flavonoids (985 and 895 µmol Trolox equivalent/gram dry weight). Animals received both total ethanol and n-butanol extracts showed a significant increase in ALT, AST, blood urea, and serum creatinine levels.

Design, synthesis and anti-ulcerogenic effect of some of furo-salicylic acid derivatives on acetic acid-induced ulcerative colitis

Ulcerative colitis is a chronically recurrent inflammatory bowel disease of unknown origin. The present work describes design and synthesis of 3-aminofurosalicylic acid 4, azo-conjugates with aniline 2a, 4-ASA 2b or sulphapyridine 2c as well as N-arylsulphonamido 5, chlorosulphonyl 6, aminosulphonyl 7 and N-arylaminosulphonyl derivatives 8 (positional isosters of 5). All the synthesized compounds were evaluated for their anti-ulcerogenic effect on acetic acid-induced ulcerative colitis in rats. It was noticed that oral treatment with sulphasalazine (a reference drug) and the tested compounds 2a, 2c, 4 and 5c in equimolar doses significantly reduced the intensity of lesion score, ulcer area, ulcer index and wet weight/length ratio compared to the control group. On the other hand, compounds 2b, 5a, 5b and 7 had a lower anti-ulcerogenic efficacy. Also, the antimicrobial activity of the synthesized compounds was screened in vitro using the agar diffusion assay technique. In addition, docking of the tested compounds into cycloxygenase II using molecular operating environment (MOE) was performed in order to rationalize the obtained biological results and their mechanism of action.

Effect of Emex spinosa, Leptadenia pyrotechnica, Haloxylon salicornicum and Ochradenus baccatus extracts on the reproductive organs of adult male rats.

Context: Emex spinosa (L.) Campd. (Polygonaceae), Leptadenia pyrotechnica (Forsk.) Decne (Asclepiadaceae), Haloxylon salicornicum (Moq.) Bunge ex Bioss. (Chenopodiaceae) and Ochradenus baccatus Delile (Resedaceae) are used in folk medicine for treatment of male sexual disorders. Objective: To investigate the effects of E. spinosa, L. pyrotechnica, H. salicornicum and O. baccatus extracts on the reproductive system of male rats after prolonged period of treatment. Methods: Seventy-eight healthy adult male Wistar rats were divided into 13 groups (6 animals, each). The plant extracts (100, 200 and 400 mg/kg) were given daily by gavage to different groups of rats for 65 days. The thirteenth group (control) received the vehicle only. Test and control rats were mated with estrus female rats on days 30, 45 and 60 of treatment. Body and relative reproductive organ weights, and sperm parameters were recorded. Results: Animals treated with the ethanol extracts of E. spinosa and L. pyrotechnica showed significant improvement of the relative weight of reproductive organs, sperm count, sperm motility and total sperm abnormality. The mean sperm count for E. spinosa group (400 mg/kg) was 233.7 ± 4.50 × 106/mL, for L. pyrotechnica (200 and 400 mg/kg) groups were 237.0 ± 5.22 × 106/mL and 240.3 ± 4.64 × 106/mL, respectively and that of the control group was 218.1 ± 4.28 × 106/mL. The sperm motility of the control group was 77.5 ± 2.12, those of E. spinosa (400 mg/kg) group was 87.3 ± 3.50% and those of L. pyrotechnica (200 and 400 mg/kg) groups were 86.0 ± 3.11 and 89.7 ± 2.90%, respectively. Ethanol extracts of E. spinosa (400 mg/kg) and L. pyrotechnica (200 and 400 mg/kg) significantly elevate the serum levels of testosterone (5.30 ± 0.15, 5.32 ± 0.20 and 5.66 ± 0.19 ng/mL, respectively vs 4.64 ± 0.16 ng/mL) and luteinizing hormone (0.69 ± 0.03, 0.70 ± 0.03 and 0.74 ± 0.03 mIU/mL, respectively vs 0.59 ± 0.02 mIU/mL). On the other hand, no alterations were observed in body and relative organ weights, sperm numbers as well as sperm morphology of the male rats after the exposure to the H. salicornicum and O. baccatus extracts for 65 days. Conclusions: E. spinosa and L. pyrotechnica extracts appear to possess fertility improvement activity in male rats due to their testosterone increasing property. Moreover, the results suggest the absence of male reproductive toxicity of the H. salicornicum and O. baccatus extracts at tested doses.

New Biological Activities of Casimiroa edulis Leaf Extract and Isolated Compounds

The phytochemical investigation of Casimiroa edulis Llave et Lex (Rotaceae) afforded four coumarins: umbelliferone (1), esculetin (2), imperatorin (3) and xanthotoxol (4). The identification of these compounds was achieved by using a combination of m.p., UV, EI‐mass, 1H NMR and 13C NMR spectroscopy. Essential oil extracts were analysed by GC/MS leading to the identification of 60 components. Sesquiterpene hydrocarbons accounted for the major make up of the oil. Microbiological screenings of the oil and successive plant fractions were performed, showing promising activity against a number of microorganisms with Minimum inhibitory concentrations (MIC) comparable to the standard antibiotics such as chloramphenicol and kanamycin. The plant ethanol extract (400 mg/kg) and the isolated coumarins (60 mg/kg) showed anticoagulant activity. Analyses to determine the activity of the extracts on liver and kidney function were performed, revealing no negative or detrimental effects. Copyright

The Effect of Four Coffee types on Normotensive rats and Normal/Hypertensive Human Volunteers

Coffee is a commonly consumed beverage. The purpose of this study was to determine the effect of the four coffee types on blood pressure (BP). The caffeine percentage was tested on one cup (250 mL) of each type of coffee (Arabian, Turkish, American and an instant coffee preparation) using two methods. 65 adult male rats and 400 healthy human volunteers were used in this study. Normotensive rats were treated orally with a single dose of normal saline with varying types of coffee. Normotensive and mildly hypertensive human volunteers were administered a cup (250 mL) of any type of coffee separately. Tail cuff and a strain‐gauge plethysmograph were used to measure the systolic blood pressure (SBP), diastolic blood pressure (DBP) and heart rate (HR) of the rats, and volunteers, respectively before and 0.5, 1.0, 1.5, and 2 h post administration. The mean arterial pressure (MAP) was calculated mathematically using SBP and DBP. The alkaloidal percentage of different types of coffee showed the presence variable contents and amount of active materials. The study showed that Arabian, Turkish, American and instant coffee all have the potential to cause a BP lowering effect. Variable antimicrobial activities were recorded for the different types of coffee when tested bacteria. Copyright

Hepatoprotective activity of Cyperus alternifolius on carbon tetrachloride–induced hepatotoxicity in rats

Objective: The present work explored the potential hepatoprotective activity of total ethanol and successive extracts of Cyperus alternifolius L (Cyperaceae) against carbon tetrachloride (CCl4)–induced hepatotoxicity in rats and to isolate their bioactive constituents. Methods: For isolation and identification of the compounds, column chromatography and spectroscopic analysis were used, a model of hepatotoxicity by CCl4 in rats was used to evaluate the total ethanol extract and its successive fractions. Results: Phytochemical screening of C. alternifolius revealed the presence of different phytochemical groups. The plant proved to be safe for human use because it did not induce any signs of toxicity or mortality in mice when administered orally at doses up to 5000 mg kg−1. The total alcoholic extract in doses of 100 and 200 mg kg−1 and the successive extracts (ether, chloroform and ethyl acetate) in a dose of 10 mg kg−1 exhibited a significant (p ≤ 0.05) protective effect by lowering the elevated serum levels of aspartate aminotransferase: 230.4, 218.8, 224.6, 227.4 and 231.6 U L−1, respectively, compared with 111.6 U L−1 for silymarin (25 mg kg−1). Serum levels of alanine aminotransferase were also reduced: 77.4, 72.7, 79.7, 76.0 and 79.7 U L−1 compared to 63.7 U L−1 for silymarin. Alkaline phosphatase: 164.6, 158.0, 163.6, 154.7 and 166.4 U L−1 compared to 138.2 U L−1 for silymarin. Total bilirubin: 0.50, 0.46, 0.55, 0.52 and 0.57 mg dl−1 compared to 0.42 mg dl−1 for silymarin. Cholesterol: 213.1, 200.0, 192.7, 193.6 and 197.1 mg dl−1 compared to 180.3 mg dl−1 for silymarin. Triglycerides: 237.3, 222.4, 209.5, 206.8 and 210.2 mg dl−1 compared to 196.8 mg dl−1 for silymarin. Eight phenolic compounds were isolated from C. alternifolius for the first time and identified as esculetin 1, umbelliferon 2, imperatorin 3, psoralen 4, xanthotoxin 5, quercetin 6, quercetin-3-O-rutinoside 7 and gallic acid 8. Conclusions: The results concluded that C. alternifolius possesses significant protective effect against hepatotoxicity induced by CCl4.

Prophylactic and curative anti-ulcerative colitis activity and the possible mechanisms of action of some desert plants

Abstract The aim of the present study was to evaluate both prophylactic and curative anti-ulcerative colitis activity and the possible mechanism of action of seven desert plant extracts. Seven desert plants from different families; Conyza dioscoridis (L.) Desf. (Asteraceae), Euphorbia hirta L. (Euphorpiaceae), Origanum syriacum L. and Salvia lanigera L. (Lamiaceae), Sisymbrium irio L., Solanum nigrum Linn. (Solanaceae) and Solenostemma arghel (Del.) Hayne. (Asclepiadaceae) were separately evaluated at three doses (125, 250, and 500 mg/kg) using the acetic acid-induced colitis model. The investigated extracts possessed prophylactic and curative anti-ulcerative colitis activities in a dose-dependent manner, where Salvia lanigera (87.9) and Solenostemma arghel (89.2) were the most effective extracts whereas the dexamesathone produced 68%. These extracts were further investigated for estimation of their mechanism of action. The in vitro potential radical (DPPH) scavenging activities of the investigated extracts were well supported with the reduction of colonic MDA content for both extracts. Suppression of the inflammatory mediator TNF-α and inhibition of both PLA2 and protease enzymes may play an important role in the anti-ulcerative colitis activities. The investigated extracts were safe for use up to 5 g/kg and the total alcohol extracts of Salvia lanigera and Solenostemma arghel (400 mg/kg for 35 d) showed no alteration on liver and kidney functions. Phytochemical screening of the investigated extracts revealed the presence of flavonoids, tannins, unsaturated sterols, and proteins which could be responsible for the activities.

Prophylactic and curative anti-ulcerogenic activity and the possible mechanisms of action of some desert plants

The present study aimed to evaluate the anti-ulcerogenic activities and the possible mechanisms of action of seven desert plants from different families. Conyza dioscoridis (L.) Desf. (Asteraceae), Euphorbia hirta L. (Euphorpiaceae), Origanum syriacum L., Salvia lanigera L. (Lamiaceae), Sisymbrium irio L., Solanum nigrum Linn. (Solanaceae) and Solenostemma arghel (Del.) Hayne. (Asclepiadaceae), were tested using prophylactic and curative models of absolute ethanol-induced ulcer, at three doses (125, 250 & 500 mg/kg) of each extract. The investigated extracts possessed dose dependent anti-ulcerogenic activities in both models, with LD50 higher than 5 g/kg. The most effective extracts were C. dioscoridis and S. irio with percent protection of control ulcer; 91.1% and 85.4% respectively. The antisecretory activity of both C. dioscoridis and S. irio appears to be mainly related to the suppression of gastrin release. The in vitro potential radical (DPPH) scavenging activities of the investigated extracts were well supported with the reduction in gastric MDA (50.6% and 43.3%) and enhancing the level of reduced GSH (2.84, 2.59 mg/g tissue) for C. dioscoridis and S. irio respectively. In addition, suppression of the inflammatory mediator TNF-α may be one of the possible mechanisms of action. The alcohol extracts of C. dioscoridis and S. irio showed no alteration on liver and kidney functions. Phytochemical screening of the investigated extracts revealed the presence of flavonoids, tannins and sterols which could be related to the activities.

Therapeutic Efficacy of Dormectin, Ivermectin and Levamisole Against Different Stages of Trichinella spiralis in Rats

OBJECTIVE Three commonly used antihelmenthic drugs including Dormectin (0.2 mg/kg), Ivermectin (0.2 mg/kg) and Levamisole (7.5 mg/kg) were examined for their antihelmenthic efficacy against experimental Trichinella spiralis infection in rats. METHODS One hundred and twenty rats were orally infected with 500 T. spiralis larvae. Drugs were tested against adult worms at 4th day, against migrating larvae at 10th days and against encysted larvae at 35th day post infection (dpi). Rats were sacrificed five days post treatment. Mature worms and migrating larvae counts were detected. RESULTS Significant effect was detected in rats treated with Dormectin and Ivermectin compared to non-treated controls. Dormectin showed an efficacy of 97.75% and 86.23% in eliminating both mature worms and migrating larvae respectively. Ivermectin showed an efficacy of 94.99% and 83.85% respectively. However, Levamisole was the least effective drug; its efficacy was 4.83% and 3.57% against mature worms and migrating larvae respectively. CONCLUSION All of the tested drugs failed to inhibit the encysted larvae in the diaphragms. Moreover, T. spiralis infection in rats reduced significantly the values of total proteins, and albumin while globulin, urea and creatinine values were significantly increased together with AST and ALT activities.

Protective Effect of Arnebia hispidissima Against Carbon Tetrachloride-induced Heart and Kidney Injury in Rats

Background and Objective: Arnebia hispidissima (F. Boraginaceae) has been found to have cardiac and febrifuge properties. It has long been used in traditional system of medicine for the treatment of heart ailments, headache and fever. This study aimed to investigate the protective effect of Arnebia hispidissima extract (AHE) on carbon tetrachloride (CCl4)-induced cardiotoxicity and nephrotoxicity. Materials and Methods: Adult rats were divided into five groups and medicated as follows: (1) The control group received the vehicles (olive oil; 1 mL kgG1, i.p.+3% Tween 80; 1 mL kgG1, p.o.). (2) CCl4 group of animals was administered with 20% CCl4 in olive oil (1 mL kgG1, p.o.). (3) Silymarin group was co-administered with CCl4 plus silymarin (50 mg kgG1, p.o.). (4) CCl4 plus AHE (200 mg kgG1, p.o.). (5) CCl4 plus AHE (400 mg kgG1, p.o). Rats received vehicle, CCl4, silymarin or AHE twice a week for 8 weeks. Serum AST (aspartate transaminase), LDH (lactate dehydrogenase), CK (creatine kinase), CK-MB (creatine kinase-MB isoenzyme) and cTnI (cardiac troponin) were measured to assess the heart damage markers. Serum levels of creatinine, urea, uric acid and BUN (blood urea nitrogen) were measured as markers of the renal function. Markers of oxidative stress in the cardiac and renal tissues were estimated by determining the levels of SOD (superoxide dismutase), GPx (glutathione peroxidase), CAT (catalase), GSH (reduced glutathione) and MDA (malondialdehyde). Heart and kidney tissues were investigated for histopathological changes. Results: Administration of CCl4 significantly increased the levels of cardiac and renal damage markers. Co-administration of CCl4 plus AHE significantly relieved the adverse effect of CCl4 in rat and reduced the increased serum levels of cardiac and renal damage markers. AHE compensated the deficits in the antioxidant defense mechanisms (SOD, GPx and CAT) and suppressed LPO (lipid peroxidation) in rat heart and kidney resulting from CCl4 administration. Moreover, histopathological changes induced with CCl4 in heart and kidney tissues of rat were also reduced with the co-administration of AHE. Conclusion: In this study, we have found that oral administration of AHE prevented CCl4-induced cardio- and nephrotoxicity by accelerating heart and kidney antioxidant defense mechanisms and down regulating the LPO near to the normal levels.