Schistosomiasis is a chronic parasitic disease affecting about 207 million individuals worldwide. It is still a major health problem in many tropical and subtropical countries, as well as for travelers from developed countries. The treatment strategies of schistosomiasis can be divided into two main routes: (a) chemotherapy treatment including trivalent antimony compounds, hycanthone mesylate, niridazole, metrifonate, oxamniquine, oltipraz, artemisinins, albendazole, amoscanate mirazid, and praziquantel; (b) vaccines that may play an important role in the control of schistosomiasis in the future.
Synthesis of new series of 5,6,7,8-tetrahydronaphthalene derivatives conjugated with chalcone, pyridine, pyrazole and isoxazole functionalities hoping to circumvent the unwanted ulcerogenic and other side effects of the already used nonsteroidal anti-inflammatory drugs.
Most currently used nonsteroidal anti-inflammatory drugs (NSAIDs) suffer from limitation in their therapeutic uses, since they cause gastrointestinal and renal side effects related to inhibition of cyclooxygenase1 (Cox1) in tissues where prostaglandins exert physiological effects.
Reaction of 2-acetyl tetralin (1) with some aromatic aldehydes in the presence of malononitrile yielded 2-amino-3-cyanopyridine derivatives 2a–c. Condensation of compound 1 with aromatic aldehydes afforded the chalcone derivatives 3a–c. Then, compound 3a reacted with hydrazine hydrate or phenyl hydrazine and yielded pyrazoline derivatives 4 or 5, respectively. Also, the reaction of compound 3c with hydroxylamine hydrochloride afforded the isoxazole derivative 6. Anti-inflammatory properties of the synthesized compounds were evaluated in vivo utilizing formalin induced paw edema method in rats, analgesic activities were tested via both hot plate and writhing methods.
Derivatives 2c and 3c revealed promising results when the anti-inflammatory, analgesic, and ulcerogenic activities of the synthesized compounds were evaluated. All of the compounds induced significant central and peripheral analgesia. The derivatives 2a, 2c, 3a, 3b, 3c, 5, and 6 showed higher activity than the standard ibuprofen.
The possible beneficial effects of the association between rosuvastatin (3-hydroxy-3-methylglutaryl coenzyme reductase inhibitor) and valsartan [angiotensin receptor blocker (ARB)] on arterial blood pressure, endothelial nitric oxide production, cardiac hypertrophy, and lipid profile in nitric oxide-deficient hypertensive rats were examined.
Statins and ARB possess common additional properties such as restoration of endothelial activity and antioxidant properties. These properties eventually prove useful for the improved treatment of cardiovascular disease.
Hypertension was induced in male albino Wistar rats by daily gavage of NG-nitro-L-arginine-methyl ester (L-NAME, 50 mg/kg) for 3 weeks. These animals were randomly assigned to the following groups: L-NAME, L-NAME/valsartan, L-NAME/rosuvastatin, and L-NAME/valsartan+rosuvastatin.
Oral administration of L-NAME for 3 weeks induced significant elevation in arterial blood pressure and increased the heart rate but did not show any significant change in plasma lipid profile. Meanwhile, plasma nitric oxide level was reduced to 20% of its normal level, and the plasma malondialdehyde level was significantly increased by 33.21%. Coadministration of rosuvastatin with valsartan improved hypertension, normalized the heart rate, increased plasma nitric oxide level by 70.06%, and restored the plasma malondialdehyde level to its normal value.
Coadministration of valsartan (ARBs) and rosuvastatin (3-hydroxy-3-methylglutaryl coenzyme reductase inhibitor) as primary treatment therefore provides a greater degree of protection, controls the risk factors, and improves the vascular and general health.
The investigation of two fungal strains isolated from Egyptian habitats, namely, the endophytic Fusarium poae FUN1 and the terrestrial Penicillium italicum FUN2 to illustrate their chemical constituents and their bioactivities.
See General instrumental procedures.
Linoleic acid (1), indole-3-acetic acid methyl ester (2) and Nb-acetyltryptamine (3) were produced by F. poae FUN1, whereas P. italicum FUN2 also delivered linoleic acid (1) in addition to cis-cyclo-(prolyl,valyl) (4). The structures of compounds (1)–(4) were elucidated by 1D and 2D NMR, MS data and through comparison with literature reports. In this article, the taxonomical characterization of both fungal strains, their upscale fermentation and the antimicrobial and cytotoxic activities tested have been described.
Two different fungal strains, endophytic F. poae FUN1 and terrestrial P. italicum FUN2, were intensively studied biologically and chemically. Four bioactive compounds (1)–(4) were isolated, and structurally confirmed by intensive studies of NMR and MS. The antimicrobial and cytotoxic activities of the fungal extracts and their delivered compounds were studied. This might be helpful for the cure of recent diseases, and drug-resistant phenomena as well as in the development of pharmaceutical, agrochemical and biochemical agents and their lead compounds.
Six bacterial strains were tested for the production of dextransucrase. The highest dextransucrase activities were produced by local strain Leuconostoc paramesenteroides after 24 h in static culture conditions. Dextransucrase was induced using sucrose (10 g%) as a carbon source and corn steep liquor (3.5 ml%) as a nitrogen source. Fe2+ favoured enzyme production. Cells of L. paramesenteroides were immobilized using three supports, calcium alginate, agar and κ-carrageenan. Calcium alginate beads were able to produce dextransucrase for four runs with 100% activity. The optimum temperature for enzyme reaction ranged from 30 to 65πC at pH 5.4. In the absence of substrate, the enzyme retained 100% activity for 30 min at 40πC and 69% activity for 10 min at 60πC.
The application of natural products as well as biological control-specific bioagents, especially the nucleopolyhedrovirus, is considered a very important tool to ensure that pest control does not affect the environment.
Chemical constituents screening and determination of pharmacopoeial constants, and minerals and trace elements of the brown algae Sargassum asperifolium, Sargassum dentifolium, and Sargassum linifolium from the Red Sea (Hurghada, Egypt) were carried out.
It was found that Sargassum spp. have a high ash content and were positive for subliminal matter, volatile constituents, carbohydrate content, sterols, and/or triterpenes. In addition, they had high Ca, K, Mg, and Fe contents. The protein content as well as the amino acid composition of the three algae species mentioned were assessed using the Kjeldahl method and an amino acid analyzer, respectively. The hydroalcoholic extracts (70%) of Sargassum spp. under investigation were examined for insecticidal activities in vitro on Spodoptera littoralis (Sl52 cells) and Spodoptera frugiperda (Sf9 cells) and in vivo on S. littoralis nucleopolyhedrovirus replication. The results showed that the three algae species tested had various insecticidal and antiviral activities.
Investigation of the phenolic constituents of roots, leaves and seeds of A. lappa L. cultivated in Egypt.
Qualitative and quantitative analysis of lignans and other phenolics by LC-MS/MS and HPLC/PDA-LC-MS/MS, as well as evaluation of potential bioactivities.
LC-MS/MS of the ethyl acetate fractions from Arctium lappa seeds, leaves and roots showed the presence of 13 phenolics, including lignans, distributed in the different organs. The following phenolics were identified: caffeic acid 1, genistein 2, biochanin A 3, luteolin 4, chlorogenic acid 5, materisenol 6, arctigenin 7, quercetin 8, cynarin 9, arctiin 10, lappaol A 11, rutin 12 and lappaol F 13. Quantification of these compounds by HPLC-PDA-MS/MS showed that arctiin was the major compound in seeds. The antioxidant, antihepatotoxic, anti-inflammatory and cytotoxic activities of ethanolic extracts of the different organs were evaluated.
The study of the lipid of the seed and aerial parts of Onopordum alexandrinum Boiss., family Asteraceae, growing in Egypt led to the isolation and identification of the unsaponifiable and fatty acid fractions of both the seed and the aerial parts of the plant. Also, isolation of volatile oil of the seed and studying their antioxidant activity.
The constituents of the unsaponifiable fraction of the seed, aerial parts of the plant and volatile oil of the seeds were identified by Gas liquid chromatography (GLC) analysis. The radical scavenging effects of the tested extracts of both the seed and the aerial parts of the plant using DPPH free radicals.
GLC analysis of the unsaponifiable fraction of the seeds indicated a mixture of hydrocarbons ranging from C13 to C28; cholesterol, campasterol, stigmasterol, and β-sitosterol were also present. GLC analysis of the fatty acid methyl esters of the seeds indicated the presence of eight fatty acids. Also, GLC analysis of the unsaponifiable fraction of the aerial parts of the plant indicated a mixture of hydrocarbons ranging from C17 to C28. Cholesterol, campasterol, stigmasterol, and β-sitosterol were also present. GLC analysis of the fatty acid methyl esters of the aerial parts indicated the presence of nine fatty acids. Sixteen compounds were identified by GLC analysis represented 77.97% of the total composition of the oil of the seeds.
The unsaponifiable fractions of both the seed and the aerial parts of the plant and volatile oil showed a strong antioxidant activity, whereas the fatty acid fractions showed a moderate antioxidant activity.
Oxidative modification of low-density lipoprotein (LDL) has been implicated in atherogenesis. Antioxidants that prevent LDL oxidation may reduce atherosclerosis.
The antioxidant activity of 45 extracts from 15 locally used medicinal plants were studied in-vitro employing using three different systems; the DPPH (1,1-diphenyle-2-picryl-hydrazyl) radical scavenging assay, superoxide anion generated in Xanthine–Xanthine oxidase (X-XOD) system and the LDL oxidation induced by cupper ions.
It was observed that the leaf extracts of olive, Jew's mallow, celery, the seed extract of celery and safflower, and ginger extracts had the highest antioxidant activity in the three assays.
It could be concluded that these plant extracts could play an important role in the inhibition of lipid peroxidation in biological systems through their antioxidant, metal chelating, and free radical scavenging activities.