Evaluation of the chemical constituents and potential biological activities of Cunninghamella blakesleeana.

The aim of this work is to evaluate the chemical constituents and potential biological activists of Cunninghamella blakesleeana. Three fatty acids were isolated using column chromatography and identified as palmitic acid (F1), oleic acid (F2) and stearic acid (F3) in addition to other two steroidal compounds; α-amyrin (A4), and ß-sitosterol (A5). Using GC, ten fatty acids were detected the major fatty acid obtained was stearic acid (74.61%) while palmitic acid was the second high percentage (10.35%), and the least percentage obtained was arachidic acid (0.07%). C. blakesleeana extract showed in-vitro antimicrobial activities against some microorganisms. The highest activity of C. blakesleeana total extract was reported against Staphylococcus aureus (18.3 ± 0.03 mm.) followed by Streptococcus pyogenes (15.3 ± 0.05), while the lowest were for both Candida albicans & Pseudomonas aeruginosa (6.7 ± 0.06 and 5.9.0 ± 0.9 mm. respectively). The three isolated compounds (F1-3) showed activities against Staphylococcus aureus, Penicillium expansum, and Salmonella typhimurium only. The highest activity was aganist Staphylococcus aureus (13.0 ± 0.1 mm.). The highest effect was obtained by compound F3 (stearic acid) (15.0 ± 0.5 mm.), and compound F1 (oleic acid) (13.0 ± 0.1 mm.) and F2 (palmitic acid) 11.0 ± 0.3 mm. The total ethanol extract of the investigated fungus was safe up to 5000 mg kg-1 and did not produce any significant change in liver and kidney functions after oral administration (400 mg kg-1) for 14 consecutive days. The results reported the isolation of some fungal new driving compounds which has been not isolated before from Cunninghamella species in addition to their correlated new biological activities.

Analysis of Alpina officinarum Hance, chemically and biologically.

Alpinia officinarum Hance is one of the most commonly used herbs belongs to Family Zingiberaceae. The current work deals with the qualitative and quantitative chemical study of this plant rhizomes in addition to the investigation of its anticancer activities. The results of the qualitative analysis showed a variation of phytochemical contents in this plant. While quantitative analysis showed a very promising percentage of active materials and Pharmacopeial constants. Analysis of elements like Cu, Zn & Mg were variable chromium was the lowest (0.680 ppm). The active constituents showed the highest percentage of carbohydrate (20.25 ±â€¯1.11) and the lowest was of lipid (2.79 ±â€¯1.03), other constituents percentage ranged from 5.11 ±â€¯1.31 to 18.26 ±â€¯1.24 for protein and flavonoids respectively. The pharmacopeial constant determinations reported the highest in moisture content (11.02 ±â€¯1.05), Total ash, water-soluble ash, and acid insoluble ash were varied in values (5.64 ±â€¯1.31 to 2.01 ±â€¯1.12). The evaluation of the antitumor activities (in vitro) of the investigated plant rhizomes extract showed that; it exhibited a direct cytotoxic effect on the growth of some cell lines compared to the standard drug vinblastine sulphate. The activities were recorded against two cell lines; A-549 (Lung carcinoma) and CACO (colorectal carcinoma) with IC50 6.72 ±â€¯0.5 and 7.6 ±â€¯0.3 µg/ml respectively, these effects were better than the standard drug vinblastine sulphate (IC50 were 24.6 ±â€¯0.7& 30.3 ±â€¯1.4 µg/ml). Moreover, the effect of the investigated extract was also promising on the other three cell lines (HCT-116 (Colon carcinoma, Hela (Cervical carcinoma) & Pc3 (prostate cancer) the best effect was on Hela with IC50 of 24.5 ±â€¯1.1 µg/ml better than vinblastine sulphate (59.7 ±â€¯2.1 µg/ml).

Experimental and clinical antihypertensive activity of Matricaria chamomilla extracts and their angiotensin-converting enzyme inhibitory activity.

Three different extracts of Matricaria chamomilla L. were evaluated for their antihypertensive activity, these extracts were total alcohol extract (Extract 1), oil extracted (Extract 2), and water lifted after oil extraction (Extract 3). Quantitative and Qualitative analyses were carried out for all extracts. The 3 extracts were proved to be safe for human use. A single oral administration of the plant extracts (200 mg/kg) decreases both systolic and diastolic blood pressure of normotensive rats after 1, 1.5, and 2 hr. Furthermore, groups treated with the evaluated extracts (100 & 200 mg/kg) or Captopril (20 mg/kg) showed a significant reduction in the elevated blood pressure and heart rate. Extract 3 showed the most antihypertensive activity. Serum biochemical parameters and lipid profile levels of treated groups were improved in comparison with induced-hypertensive untreated rats. In evaluation of oxidative damage parameters Glutathione and superoxide dismutase (SOD) in some organs, the investigated extracts or captopril restored the amount of reduced Glutathione in tissues in addition to an increase in the activity of the SOD after a significant depletion of SOD activity. In the clinical study, there was a significant dose dependent decrease in Systolic blood pressure, Diastolic blood pressure, and heart rate compared with their basal values in both normotensive and hypertensive human volunteers after oral administration of Matricaria chamomilla beverages.

Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity.

Two novel quinazoline derivatives named as; 3-[(4-hydroxy-3-methoxy-benzylidene)-amino]-2-p-tolyl-3H-quinazolin-4-one (5) and 2-p-Tolyl-3-[3,4,5-trimethoxy-benzylidene-amino]-3H-quinazolin-4-one (6) in addition to one acetamide derivative named as 2-(2-Hydroxycarbonylphenylamino)-N-(4-aminosulphonylphenyl) 11 were synthesized, and evaluated for their anti-ulcerogenic & Anti-Ulcerative colitis activities. All of the three compounds showed curative activity against acetic acid induced ulcer model at a dose of 50 mg/kg, they produced 65%, 85% & 57.74% curative ratio for compounds 5, 6 & 11 respectively. The effect of the tested compounds 5, 6 & 11 at dose 50 mg/kg were significantly (P < 0.01) more effective than dexamesathone (0.1 mg/kg) in reducing all parameters. Compounds showed curative activity of for peptic ulcer (induced by absolute alcohol (at a dose of 50 mg/kg, it produced Curative of control ulcer 56.00%, 61.70% & 87.1% for compounds 5, 6 & 11 respectively at dose 50 mg/kg, while the standard drug (Omeprazole 20 mg/kg) produced 33.3%. In both tests, the activity of our target compounds were higher than the standard drugs used for treatment of peptic ulcer and ulcerative colitis. No side effects were reported on liver and kidney functions upon prolonged oral administration of this compounds.

In - Vitro activity of Desmostachya bipinnata (L.) Stapf successive extracts against Helicobacter pylori clinical isolates.

Helicobacter pylori are well acknowledged as a major cause of gastrointestinal ailments and gastric cancers. Therefore, the present study aimed to investigate the potential in vitro activity of Desmostachya bipinnata against H. pylori, focusing on the determination of the most active extract responsible for the anti-helicobacter activity to produce new active drug from natural source. Desmostachya bipinnata total alcohol and successive extracts were in vitro tested against H. pylori. All extracts showed promising anti Helicobacter pylori activities. The most effective extract was diethyl ether extract, it showed 75% growth inhibition of the clinical Isolates bacterial Helicobacter pylori, in addition it showed high count reduction on the selected organisms in the different concentrations used (2xMIC, MIC & ½ MIC) compared with the untreated controls as well as the other extracts (chloroform, ethyl acetate and n-butanol). The oral median lethal dose (LD50) of the alcohol extract of the plant by doses up to 5000 mg/kg didn't showed any mortality or morbidity, in addition no side effects were recorded on both liver and kidney functions this means that the extract was safe for use.

Anticancer effect of Cenchrus ciliaris L.

Cenchrus ciliaris L total alcohol and successive extracts of both aerial and root parts were tested for their anticancer activities against lung (A-549), intestinal (CACO), colon (HCT-116), cervical (Hela), hepatocellular (HepG-2), and breast (MCF-7) (PC3) cell lines and compared with the standard drug vinblastine sulphate. The obtained results exhibited direct cytotoxic effect with variable inhibiting effect on the growth of the listed cell lines comparing to vinblastine sulphate as reference standard drug, these effects showed different IC50 ranged from 11.1 ±â€¯0.3 to 267 ±â€¯µg/ml. All root extracts showed the best activities against most of the tested cell lines specially HepG-2 (Hepatocellular carcinoma) (9 ±â€¯2.1 µg/ml) which was somewhat closely related to the effect of vinblastine sulphate (2.93 ±â€¯0.3 µg/ml). The highest anticancer effect of Cenchrus ciliaris L aerial parts and root extracts were recorded on HepG-2 (Hepatocellular carcinoma) their IC50 were 12 ±â€¯0.8 & 9 ±â€¯2.1 respectively, CACO (colorectal carcinoma) their IC50 were 27.2 ±â€¯1.6 & 20.5 ±â€¯0.6 respectively, A-549 (Lung carcinoma) their IC50 were 14.5 ±â€¯0.7& 11.1 ±â€¯0.3 respectively which were better than the standard drug especially in case the anticancer effect on CACO (colorectal carcinoma) and A-549 (Lung carcinoma). Chloroform extracts of both aerial and roots achieved the best anticancer activities on all of the cell lines especially with colorectal (CACO) and Lung carcinoma (A-549). Cenchrus ciliaris could be a promising source of new chemical moieties used to target cancer cells.

Evaluation of anti-ulcer and ulcerative colitis of Sonchus oleraceus L.

Sonchus oleraceus L. was evaluated for its gastro antiulcerogenic and anti-ulcerative colitis activities Different extracts and fractions from Sonchus oleraceus aerial parts and roots were evaluated at different dose; total alcohol extracts of aerial parts SA and roots SR were evaluated doses 250 & 500 mg/kg, While Successive extracts (SAL, SRL, CSA, CSR, BSA & BSR) were evaluated at dose of 150 mg/kg. Absolute ethanol-induced ulcer model was used for evaluation of the anti-ulcerogenic activity. The root extract showed promising antiulcerogenic activity as the total alcohol extract of the root SR (500 mg/kg) produced 88.5% protection from control ulcer which is significantly more effective than the standard drug omeprazole (20 mg/kg), in addition, the butanol fraction of the root extract BSR also produced 76.66% protection from control ulcer. On the other hand, the aerial parts total extract SA showed low antiulcerogenic activity in both tested doses (250 & 500 mg/kg) as it produced 25% & 28.33% protection from control ulcer respectively. Only the butanol fraction of the aerial parts extract BSA showed promising activity 54.16%. In the acetic acid-induced ulcerative colitis model, among the investigated extracts of Sonchus oleraceus; only the total extract of the aerial parts (SA) at dose 500 mg/kg showed strong anti-ulcerative colitis activity and this activity is followed by the activity of the butanol and chloroform fractions of the aerial parts, they produced 77.28%, 57.4% & 47.68% protection from control colitis respectively. The standard drug dexamethasone produced 63.36% protection from control colitis. The total alcohol extracts SR & SA showed no alteration on liver and kidney functions and these extracts are safe up to 5000 mg/kg. Phytochemical screening of the investigated extracts revealed the presence of carbohydrates, flavonoids, tannins, unsaturated sterols, proteins and lactones which could be responsible for the activities.

Anti-ulcerative colitis activity of Calotropis procera Linn.

The aim of the present study was to evaluate the anti-ulcerative colitis activity of Calotropis procera. Different extracts of the investigated plant were evaluated; total alcohol extract, polar extract and non-polar extract. All the investigated extracts at doses 200 &400 mg/kg possessed a dose-dependent anti-ulcerative colitis potential when administrated for 5 consecutive days after colitis induction by acetic acid in rats. They reduced different parameters of UC. Only polar extract at both doses (200, 400 mg/kg) was more effective than the standard drug Prednisolone (50 mg/kg), it produced percent protection of control colitis by 63.8% and78.4% respectively, while the standard drug Prednisolone produced 54.9% protection. The anti-ulcerative colitis activity may be attributed to the active principles i.e. flavonoids. Preliminary phytochemical screening showed that the plant contains flavonoids, unsaturated sterols and/or triterpenoides, cardiac glycosides, carbohydrates or glycosides, proteins and/or amino acids, tannins and coumarins. The total alcohol extract was safe up to 4000 mg/kg and there were no side effects reported on liver and kidney functions.

Amhezole, A Novel Fungal Secondary Metabolite from Aspergillus terreus for Treatment of Microbial Mouth Infection.

Bio-guided fractionation of Aspergillus terreus extract leads to isolation of a novel terpenoidal secondary metabolite. The isolated compound and the total alcoholic extract of Aspergillus terreus showed a remarkable activity against microbial mouth infections; namely, Candida albicans, Lactobacillus acidophilus, Streptococcus gordonii, and S. mutan. Moreover, the Minimum Inhibitory Concentration of the isolated compound was determined and showed low values. The combination of each of the alcoholic extract of A. terreus and the isolated compound Coe-Comfort tissue conditioner inhibited the growth of Candida albicans at concentrations of 500 and 7.81 µg/mL, respectively, Lactobacillus acidophilus at concentrations of 250 and 7.81 µg/mL, respectively, Streptococcus gordonii at concentrations of 1000 and 62.50 µg/mL, respectively, and S. mutans at concentrations of 1000 and 125 µg/mL, respectively. The oral dosing of the extract and the isolated compound did not show any significant effect on the activity of alanine aminotransferase, aspirate aminotransferase, and the levels of blood urea and serum creatinine. Copyright © 2017 John Wiley & Sons, Ltd.

Anticandidal Activity of Extracts and a Novel Compound, Amnomopin, Isolated From Petriella setifera.

A novel triterpenoidal compound named 'amnomopin' (3ß-diglucoside-5,12-28-oic acid), which is named IUPAC as 3-O-(2' âž” 1″diglucoside)1,2,3,4,4a,5,6,6a,6b,7,9,10,11,12,12a,12b,13,14b-octadecahydro-10-hydroxy-2,2,6a,6b,9,9,12a-heptamethylpicene-4a-carboxylic acid, was isolated from the extract Petriella setifera. The total alcoholic extract of P. setifera showed a great activity against clinically isolated Candida species, including Candida albicans, Candida dubliniensis, Candida famata, Candida glabrata, Candida inconspicua, Candida kefyr, Candida krusei, Candida norvegensis, Candida parapsilosis and Candida tropicalis. Also, the new compound amnomopin was active against all the investigated Candida species. The highest anticandidal activity of P. setifera extract was obtained against C. kefyr (22.6 ± 1.5 mm), C. albicans and C. norvegensis (21.3 ± 0.63 mm) and C. krusei (20.6 ± 1.5 mm). Moreover, the minimum inhibitory concentrations of both the total extract and the isolated compound were low. The minimum inhibitory concentration of the compound isolated from P. setifera was 0.49 µg/mL against C. kefyr, 0.98 µg/mL against C. albicans and C. norvegensis and 1.95 µg/mL against C. krusei. The oral dosing of the extract and the isolated compound did not show any significant effect on the activity of alanine aminotransferase, aspirate aminotransferase and the levels of blood urea and serum creatinine. Copyright © 2017 John Wiley & Sons, Ltd.

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.

Anti-ulcerogenic and anti-ulcerative colitis (UC) activities of seven amines derivatives.

The Novel target compounds (CP-1-7) were synthesized and tested at doses up to 1000 mg/kg for their entitled activities. They exerted promising results without any behavioral changes and mortality in mice. Therefore, according to the results obtained in our study, it could be categorized as highly safe agents for treating UC since substances possessing LD50 higher than 50 mg/kg are considered nontoxic. They also possessed a potent anti-ulcerogenic activity with different potentials. The most effective compound was CP-4, it produced 97.7% ulcer protection of control followed by CP-3, which produced 90.3% protection, while the standard drug ranitidine (100 mg/kg) produced 49.2% protection. Compound CP-1 showed lowest activity among the current series, it produced 55.5% protection. The target compounds were significantly more effective than the standard in reducing ulcer index. The anti-ulcerative colitis activity was tested using acetic acid induced colitis model. The curative effect of the tested compounds at a dose of 50 mg/kg oral administration on rats showed a potent anti-ulcerative colitis activity with different potentials. They induced a significant decrease in ulcer score, ulcer area, ulcer index and weight/length of the colon specimens. The percent protection of control colitis ranged from 66.8% for CP-7 to 22.3% for CP-5; however the percent protection for dexamesathone (0.1 mg/kg) was 59.3%. The effect of the tested compounds CP-7 and CP-3 at dose 50 mg/kg were significantly more effective than dexamesathone (0.1 mg/kg) in reducing all parameters. Liver functions were not affected as there is no effect on the activity of both AST and ALT in animals that received the compounds, so the compounds didn't reveal hepatotoxic manifestation. Although, the results on kidney functions showed that, CP-1 slightly elevated blood urea concentration and CP-3 & CP-4 slightly elevated serum creatinine; no apparent nephrotoxic manifestations were recorded.

Novel essential amino acid-sulfanilamide hybrid as safe anti-ulcerogenic agent with anti-helicobacter pylori activity.

A novel and safe essential amino acid (Leucine) incorporating sulfanilamide was synthesized, and evaluated for its anti-ulcerogenic activity and in vitro anti-Helicobacter pylori activity. The new molecule showed a dose dependent activity against absolute ethanol-induced ulcer in rats, it produced percent protection of control ulcer by 66.7 at dose 100 mg/kg. In addition it showed a potent anti-Helicobacter pylori activity in vitro against 7 clinically isolated strains. The minimum inhibitory concentration (MIC) ranged from 12.5 to 50 µg/ml. The preliminary safety studies and toxicity profile are optimistic and encouraging.

Synthesis and biological evaluation of certain 3-substituted benzylideneamino-2-(4-nitrophenyl)quinazolin-4(3H)-one derivatives.

Certain new 3H-quinazolin-4-one Schiff's bases were synthesized and screened for their activities against ulcerative colitis "UC". Their activity against phospholipase A2 and protease enzymes was also investigated. Some compounds possessed remarkable effect with different potentials against acetic acid-induced colitis model in rats. Compound 14 (50 mg/kg) was more effective than dexamesathone (0.01 mg/kg). It produced 79.78% protection of control colitis; however, compound 13 produced 75.80% protection and was considered as effective as dexamesathone with 75.30% protection. The observed results could be explained partially by their anti-inflammatory activities which appear as phospholipase A2 (hGIIA) and/or through protease inhibitor potentials. However, all the compounds under test showed preferential inhibition towards hG-IIA type of PLA2 rather than DrG-IB with varying degrees. Interestingly, compounds 14, 13, 12 and 11 displayed excellent inhibitory activity against phospholipase A2 accompanied by protease inhibitory profile.

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

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.

New Activities for Isolated Compounds from Convolvulus austro-aegyptiacus as Anti-ulcerogenic, Anti-Helicobacter pylori and Their Mimic Synthesis Using Bio-guided Fractionation.

Bio-guided fractionation of the total alcoholic extract of Convolvulus austro-aegyptiacus was screened for its anti-ulcerogenic activity, using an absolute-ethanol-induced ulcer model at 500 and 1000 mg/kg doses. Two compounds were isolated from the butanol extract of C. austro-aegyptiacus and identified by 1 H and 13 C nuclear magnetic resonance as scopoletin and scopolin. The isolated compounds (50 mg/kg) showed a remarkable anti-ulcerogenic activity because they exhibited control-ulcer protection by 16.7% and 90.8%, respectively. The acute toxicity study showed that the extract is highly safe; the median lethal dose (LD50) was more than 4000 mg/kg. Moreover, the obtained results were confirmed by the sub-chronic toxicity because the rats that have been administered 1000 mg/kg of the extract for 15 consecutive days showed no alteration in the liver and kidney functions. Copyright © 2015 John Wiley & Sons, Ltd.

Anti-leishmanial activities of extracts and isolated compounds from Drechslera rostrata and Eurotium tonpholium.

The fungal extract of Drechslera rostrata and Eurotium tonpholium showed a significant anti-leishmanial activity against Leishmania major; IC50 was 28.8 and 28.2 µg/mL, respectively. Seven compounds, five from D. rostrata (H1-H5) and two from E. tonpholium (H6 and H7), were isolated and identified using different spectroscopic analysis including (1) HNMR, (13) CNMR, Hetero-nuclear multiple bond connectivity (HMBC), Hetero-nuclear Multiple Quantum Correlation (HMQC), and EI-MS. The isolated compounds are: di-2-ethylhexyl phthalate (1), (22E)-5α,8α-epidioxyergosta-6,22-diene-3ß-ol (2),1,3,8-trihydroxy-6-methyl-nthraquinone (3), aloe-emodine 8-O-glucopyranoside(4), 2R, 3R,4R,5R hexane 1, 2, 3, 4, 5, 6 hexole (Mannitol) (5), 1,8-dihydroxy-3-methoxy-6-methyl-anthraquinone (6) and 1, 4, 5-trihydroxy-7-methoxy-2-methyl-anthraquinone (7). However, compounds (1) and (6) showed activity against L. major with IC50 of 3.2 and 10.38 µg/mL, respectively. On the other hand, oral administration of the two extracts (100 mg/kg) and compounds 1 and 6 (50 mg/kg) showed very good activity when compared with the anti-leishmanial drug Pentostam (125 mg/kg). Interestingly, the complete heeling activity of the extracts and compounds (1) and (6) was obtained after 13-17 days of treatment, while complete healing activity of Pentostam was obtained after 28 days. No alteration on liver and kidney functions was recorded on animals treated with the two extracts for 15 consecutive days.

Antiulcerogenic activities of the extracts and isolated flavonoids of Euphorbia cuneata Vahl.

The total alcohol extracts of Euphorbia cuneata Vahl.(Euphorbiaceae) were screened for antiulcerogenic activity using an ethanol-induced ulcer model at doses of 125, 250 and 500 mg/kg. The extracts possessed antiulcerogenic activity in a dose-dependent manner. Four flavonoidal compounds were isolated and identified as naringenin, aromadendrin, apigenin and 4'-O-methoxy-luteolin-7-O-rhamnoglucoside, each demonstrating antiulcerogenic activity with curative ratios ranging from 75.78% to 88.23%. In addition, the alcohol extracts and isolated compounds were shown to scavenge the 1,1-diphenyl,2-picrylhydrazyl radical by different ratio, with the most effective being 4'-O-methoxy-luteolin-7-O-rhamnoglucoside (91.14%). The antioxidant activity of the alcohol extracts and the isolated compounds may explain the antiulcerogenic properties. No side effects were observed on either liver or kidney functions.

Anti-ulcerative colitis activity of compounds from Euphorbia granuleta Forssk.

The aim of the present study was to evaluate the anti-ulcerative colitis (UC) activity of the total alcohol extracts of Euphorbia granuleta Forssk. (Euphorpiaceae), isolate and identify the active compounds that could be responsible for the activity, in addition to determination of the possible mechanism of action. Six compounds were isolated and identified from this plant: three phenolic compounds (kampferol, kampferol-3-glucoside and kampferol-3-galactoside) in addition to three steroidal compounds (1-ethoxypentacosane, heptacosan-1-ol and ß-sitosterol). Three compounds (heptacosan-1-ol, ß-sitosterol and kampferol-3-galactoside) were found to be responsible for the anti-UC activity of E. granuleta extract. The anti-UC activity of these compounds may be explained by reducing the pro-inflammatory cytokine tumor necrosis factor-alpha (TNF-α), in addition to reduction of colonic malondialdehyde (MDA) contents. No side effects were reported on liver and kidney functions. The active compounds reduced both serum TNF-α and mucosal MDA levels.

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.