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.

[Infratemporal metastasis from a renal cell carcinoma]. / Métastase infratemporale d'un carcinome à cellules rénales.

INTRODUCTION: Kidney cancer, particularly clear cell carcinoma, has an unpredictable clinical course with a variable metastatic potential in time. Some metastatic sites are atypical, such as head and neck (6% of cases). We report an extremely rare case of clear cell renal carcinoma with a metastasis in the infratemporal fossa. OBSERVATION: A 67 year old male patient, operated in 2007 for a Fuhrman grade I clear cell carcinoma of the left kidney (radical nephrectomy), consulted for swelling of the left temporo-zygomatic region. A local biopsy allowed diagnosing clear cell renal carcinoma metastases. The patient was inoperable and was treated by antiangiogenic drugs. DISCUSSION: The recommended treatment is surgical exeresis when the metastasis is single and can be resected. Antiangiogenic therapy is an alternative in other cases.

[Mandibular actinomycosis]. / L'actinomycose mandibulaire.

INTRODUCTION: Actinomycosis is a rare disease. The cervicofacial region is the most frequent localization. A chronic pus discharge, sometimes tumor-like, suggests the diagnosis, which is often confirmed by anatomopathology. The treatment is surgical debridement and antibiotic therapy, frequently long-term. We report three cases of mandibular actinomycosis. CASE REPORTS: A 21-year-old male patient presented with a fistulized swelling of the right jaw. A 48-year-old male patient was referred for alveolar healing delay after avulsion of teeth 32, 33, and 34. A 38-year-old female patient presented with a left mandibular swelling and restricted mouth opening. In the three cases, the diagnosis of actinomycosis was made by histology. The clinical outcome was good following alveolar curettage (and sequestrectomy for 1 patient) and antibiotic therapy. DISCUSSION: Mandibular actinomycosis is caused by Actinomyces israelii. Lesions if untreated may evolve to osteitis and sequestration. Early diagnosis is crucial.

[Invasive aspergillosis of the maxillary sinus in an immunocompetent patient]. / Aspergillose invasive du sinus maxillaire chez un patient immunocompétent.

INTRODUCTION: Invasive aspergillosis of the maxillary sinus is a severe infection most commonly observed in immunocompromised patients. We report a pseudo-tumoral presentation of invasive aspergillosis of the maxillary sinus, in immunocompetent adult. CASE REPORT: A 70-year-old female patient consulted for chronic rhino-sinusitis resistant to medical treatment. Computed tomography scan revealed a hyperdense mass filling the left maxillary antrum, with erosion of sinus walls. The ethmoidal and right frontal sinuses were involved. The histological and mycological examination of the surgical resection confirmed the diagnosis of invasive aspergillosis. The patient was given voriconazole as first line treatment. The outcome was good at 18 months. DISCUSSION: Invasive aspergillosis of the maxillary sinus is a rare disease, usually observed in immunodepressed patients. It is very rarely observed in immunocompetent patients.

Stabilization of Candida rugosa lipase during transacetylation with vinyl acetate.

An optimally prepared Candida rugosa lipase aggregate cross-linked with bovine serum albumin, was found to overcome acetaldehyde deactivation during transacetylation of a series of benzyl alcohols with vinyl acetate. The formulation, under the same reaction conditions, exhibited 4-30x enhancement in the reaction rate as compared to the celite immobilized lyophilized formulation and 25-133x enhancement as compared to the free lyophilized enzyme depending upon the alcohol chosen. The racemic 1-phenylethanol, taken as one of the alcohols, underwent a more efficient enantioselective transacetylation giving 80% enantiomeric excess of the product, (R)-1-phenylethyl acetate, at 38% conversion (E = 15) within 24h while the enzyme immobilized on celite gave 83% enantiomeric excess at 18% conversion (E = 13) during the same period of time.

Diastereoselective synthesis of (R)-(alkyl)-beta-D-galactopyranoside by using beta-galactosidase (Aspergillus oryzae) in low-water media.

A beta-galactosidase (from Aspergillus oryzae) preparation viz. EPRP (enzyme precipitated and rinsed with propanol), obtained by the removal of bulk water by precipitation with n-propanol, showed higher biological activity than the lyophilized powder. FT-IR study confirmed that EPRP had retained the alpha-helical content of the native structure better than the lyophilized form. Use of this formulation of beta-galactosidase under low water conditions (temperature 55 degrees C, reaction time of 4 h) gave enantioselectivity, E > 1000 for the stereoselective synthesis of (R)-(1-phenylethyl)-beta-D-galactopyranoside, starting from racemic 1-phenylethanol and D-galactose. For racemic 2-octanol also, EPRP worked better. Under similar conditions, (R)-(2-octyl)-beta-D-galactopyranoside was formed with an enantioselectivity, E = 38.

Enantioselective transacetylation of (R,S)-beta-citronellol by propanol rinsed immobilized Rhizomucor miehei lipase.

BACKGROUND: Use of enzymes in low water media is now widely used for synthesis and kinetic resolution of organic compounds. The frequently used enzyme form is the freeze-dried powders. It has been shown earlier that removal of water molecules from enzyme by rinsing with n-propanol gives preparation (PREP) which show higher activity in low water media. The present work evaluates PREP of the lipase (from Rhizomucor miehei) for kinetic resolution of (R,S)-beta-citronellol. The acylating agent was vinyl acetate and the reaction was carried out in solvent free media. RESULTS: The PREP, with 0.75% (v/v, reaction media) water, was indeed found to be more efficient and gave 95% conversion to the ester. Using this PREP, with no added water, 90% ee for (R)-(+)-beta-citronellyl acetate at 45% conversion (E = 42) was obtained in 4 h. The control with freeze-dried enzyme, with zero water content, gave 78% ee at 30% conversion (E = 13). FT-IR analysis showed that PREP had retained the alpha-helical content of the enzyme. On the other hand, freeze-dried enzyme showed considerable loss in the alpha-helical content. CONCLUSION: The results show that PREP may be a superior biocatalyst for enantioselective conversion by enzymes in low-water media.

Lipase catalyzed synthesis of benzyl acetate in solvent-free medium using vinyl acetate as acyl donor.

Use of vinyl acetate as acyl donor in transesterification of benzyl alcohol catalyzed by a commercially available lipase (Lipozyme RM IM) gave 100% conversion in 10 min. The excess acyl donor and the enzyme could be recovered and reused. Unlike the chemical catalytic processes, it produced no undesirable side product.