Reham M. El-Meligy

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 1HNMR, 13CNMR, 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‐3β‐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. Copyright

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 β‐sitosterol). Three compounds (heptacosan‐1‐ol, β‐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. Copyright

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

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 1H and 13C 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

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.

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

Novel Compounds with new Anti-Ulcergenic Activity from Convolvulus pilosellifolius Using Bio-Guided Fractionation.

Oral administration of the total alcohol extract of Convolvulus pilosellifolius Desr. (250 and 500 md/kg) showed potent anti‐ulcerogenic activity in absolute ethanol‐induced ulcer model in rats; it showed percent protection of control ulcer by 69.2 and 84.6%, respectively, while standard ranitidine (100 mg/kg) exhibited 46.2%. Bio‐guided work leads to isolation of two novel compounds (1 and 2), which were identified through 1H, 13C NMR, HMPC, HMQC and DEPT as: methyl 2‐(hydroxymethyl) octanoate, named as amanitate, and 16‐amino‐9,13‐dimethyl‐17‐(prop‐1‐en‐2‐yl)‐hexadecahydro‐1H‐cyclopenta[a] phenanthren‐3‐ol, named as asmatol. Both compounds (50 mg/kg) possessed anti‐ulcerogenic activity with 95.4% and 55.84% protection, respectively. Two known compounds (3 and 4) were also isolated and identified through comparison with authentic samples and confirmed through different NMR techniques as kampeferol and quercetin. These compounds also showed anti‐ulcerogenic activity with 78.38% and 5.38% protection, respectively. The cytoprotective mechanism explains the potent anti‐ulcerogenic activity of the total alcohol extract and the isolated compounds. The extract was highly safe as the LD50 was more than 5000 mg/kg. These results were well supported by the sub‐chronic toxicity study, as the extract (500 mg/kg) administrated orally to rats for 35 consecutive days showed no alteration in the liver and kidney functions. Copyright

Biological activity of fungal secondary metabolites

Abstract: Fungi are cosmopolitan organisms that inhabit almost all ecological niches of the earth and have the ability to utilise various substrates as a consequence of diversity of their biological and biochemical evolution. Fungi, during their development, follow different metabolic pathways that led to production of numerous intermediate and/or end-product compounds called as secondary metabolites. Fungi, filamentous forms, produce a diverse array of secondary metabolites that are small molecules, and not necessary for normal growth or development. Secondary metabolites have a tremendous impact on society; some are exploited for their antibiotic and pharmaceutical activities, others are involved in disease interactions with plants or animals. Most fungal secondary metabolites are synthesised from only a few key precursors in pathways that comprise a relatively small number of reactions and which branch off from primary metabolism at a limited number of points. However, the roles of secondary metabolites in the fungi that produce them are still more or less a mystery.

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

Abstract 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.