2024-03-28T14:34:31Z
https://bpsa.journals.ekb.eg/?_action=export&rf=summon&issue=9716
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2008
31
2
TOPICAL EMULSIONS STABILIZED BY SILICA NANOPARTICLES: IN VITRO RELEASE AND ANTIINFLAMMATORY STUDIES OF FLURBIPROFEN AND DICLOFENAC SODIUM
Hatem
Sarhan
Mohamed
Ibrahim
Mohamed
Amin
Amro
F. Dyab
Simple and multiple emulsions have a wide range ofpharmaceutical applications. Therefore, the stabilization of suchemulsions is a challenge to ensure a stable formulation along theperiod of storage, usage and at the same time to conserve theefficacy of the incorporated medicament. Simple o/w and multiplew/o/w emulsions were prepared using castor and paraffin oils asoil phases and stabilized solely by silica nanoparticles of wellcontrolledsurface properties. Two non-steroidal ant-inflammatorydrugs, namely flurbiprofen and diclofenac sodium wereincorporated in the stabilized simple and multiple emulsions,respectively. The stability of emulsions and the in vitro release ofthe drugs from the prepared emulsions were studied. In addition,the anti-inflammatory activity of the drugs from these liquidformulations was assessed using carageenan-induced hindpawedema in rats. The results indicated that the prepared liquidemulsions, which stabilized with silica nanoparticles, were highlystable. The in vitro release of flurbiprofen and diclofenac sodiumfrom these simple and multiple emulsions showed higher ratescompared with those preapred from paraffin oil due to their lowerviscosities. The results revealed also that the percentage of oil hasa pronounced effect on the in vitro release rates of the drugs fromthe emulsions. Furthermore, topical flurbiprofen and diclofenacsodium emulsions exhibited a potent local anti-inflammatoryactivity compared with the orally adminstered drugs in thesuspension form and this activity reached its peak (57-84%) 3 hrsafter carrageenan injection and persisted for 5 hrs, the period ofstudy.
2008
12
31
155
167
https://bpsa.journals.ekb.eg/article_64221_c3208ba21f6a5c1e0300d88e7ebf26e0.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2008
31
2
SPECTROFLUORIMETRIC METHOD FOR DETERMINATION OF SOME OXICAMS USING POTASSIUM BROMATE
Hanaa
Abdel-Wadood
A sensitive and selective spectrofluorimetric method has beendeveloped for the determination of some non-steroidal antiinflammatoryoxicams derivatives namely: tenoxicam (Tx),piroxicam (Px) and lornoxicam (Lx) after their complete oxidativeacidic hydrolysis to 2-aminopyridine. The hydrolytic product 2-aminopyridine exhibits fluorescence emission at 365 nm (excitationat 305 nm). The optimal conditions of the reaction wereinvestigated. The method was found to be linear in the ranges of(0.015-0.500 μg/ml) for Tx (0.006-0.300 μg/ml) for Px and (0.060-0.200 μg/ml) for Lx. The suggested method was successivelyapplied for the determination of the studied drugs in differentdosage forms with a recovery percentages ranged 96.82-102.79 ±0.614-2.578. The method was also applied for the determination ofthe drugs in spiked urine with a recovery percentages ranged80.51-105.35 ± 1.067-5.338. The validity of the method was assessed according to USP guidelines. Statistical analysis of theresults reveled high accuracy and good precision.
2008
12
31
169
181
https://bpsa.journals.ekb.eg/article_64222_b03bdb1c1c00235f010d6d0ab8b4083c.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2008
31
2
UTILITY OF CERTAIN SPECTROFLUORIMETRIC METHODS FOR ANALYSIS OF TWO PHARMACEUTICAL BINARY MIXTURES
Kamla
Emara
Hanaa
Abdel-Wadood
Marwa
Bakr
Simple and very sensitive spectrofluorimetric methods weredeveloped for determination of adrenaline (I)–procainehydrochloride (II) mixture and salbutamol sulfate (III) –guaifenesin (IV) mixture. Adrenaline (I) in the first mixture wasdetermined by coupling with 5-diazo-1,2,4-triazolo-3-carboxylicacid (DTCA) reagent in alkaline medium forming fluorigenicproduct which can be measured at 340 nm (ex. 245 nm), whileprocaine hydrochloride (II) gave no fluorescence. Salbutamolsulfate (III) was analyzed by reaction with ethyl acetoacetate(EAA) forming coumarin derivative, which can be measured at 320nm (ex. 280 nm). Guaifenesin (IV), the second drug in mixture has a considerable native fluorescence in methanol was measured at310 nm (ex. 230 nm). All variables affecting reaction conditionswere optimized. Linear correlations were obtained over the rangeof 19-100, 37-400 and 22-150 ng/ml for (I), (III) and (IV),respectively. The proposed methods were successfully applied forthe analysis of the studied drugs in their pure and commercialdosage forms and the obtained results were in good agreement withthose obtained from the reported methods; no significant differencein the accuracy and precision as revealed by the accepted values oft- and F-tests, respectively.
2008
12
31
183
195
https://bpsa.journals.ekb.eg/article_64223_560c7ac71329eb7b2b44188a3706be21.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2008
31
2
SYNTHESIS OF CERTAIN PYRAZOLO[3,4-d] PYRIMIDINE DERIVATIVES OF POTENTIAL ANTI-INFLAMMATORY ACTIVITY
Safinaz
Abbas
Hanan
Georgey
Shimaa
Abdelrahman
Gamil
El-Taliawi
The synthesis of twenty nine novel derivatives of pyrazolo[3,4-d]pyrimidines as non acidic nonsteroidal anti-inflammatory drugs has been achieved via reaction of 4-chloro-1-phenylpyrazolo[3,4-d]pyrimidine with different substituents including 4-amino-3-methylphenol, 4-phenylene diamine and 4-acetamidophenol.The anti-inflammatory activity of thirteen representative compounds have been screened compared to indomethacin as a reference drug. The results revealed that all the tested compounds showed anti-inflammatory activity with the exception of 10a.
2008
12
01
197
214
https://bpsa.journals.ekb.eg/article_345095_5d392ffe45a42ef7665275eeaf6e7b1f.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2008
31
2
BIOTRANSFORMATION STUDIES OF PREDNISONE USING HUMAN INTESTINAL BACTERIA; PART I: AEROBIC INCUBATION
Mohammed
Al-Sanea
Atef
Abdel-Hafez
Farghaly
Omar
Adel
Youssef
Several corticosteroids are commonly used for treatment ofconditions associated with inflammatory disorders and as immunemodulators. Specifically in cases of ulcerative colitis and therelated inflammatory bowel syndromes, these therapeutic agentsare administered rectally and are subjected to several intestinalmicro floras. The present study aimed to investigate the effect ofhuman intestinal bacterial (HIB) aerobic incubation on prednisone1 as a model for corticosteroids. Within 96 hours, 1 was mostlytransformed by HIB in vitro to various metabolites, which could beseparated by column chromatography into two fractions. The firsteluted fraction A was found to contain the major metaboliteadrenosterone, androst-4-ene-3,11,17-trione m1, whereas fractionB contains metabolite m2, which was identified by chiral HPLC asa mixture of androst-1,4-diene-3,11,17-trione enantiomers. Thestructures of metabolites m1 and m2 were identified andcharacterized by spectroscopic techniques, including 2D-NMR and mass spectrometry. Time course of biotransformation of 1 by HIBwas also studied.
2008
12
31
215
228
https://bpsa.journals.ekb.eg/article_64228_a7efb8387ad112c63bdbef5e8becb534.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2008
31
2
PHYSICOMECHANICAL PROPERTIES AND RELEASE CHARACTERISTICS OF KETOROLAC TROMETHAMINE FROM CHITOSAN FILMS: EFFECT OF INCLUSION OF DIFFERENT POLYOLS PLASTICIZERS
E.
Zen-aldeen
A.
Hussein
M.
Ibrahim
M.
Amin
The film-forming ability of chitosan polymer loaded with ketorolac tromethamine (KT) was evaluated. Films were prepared by a casting/solvent evaporation technique from plasticizer - free and plasticizer containing aqueous solutions. Glycerol, sorbitol, and 1-erythritol were used as plasticizers. Solid state of the films was studied by powder X-ray diffractometry (PXRD), and differential scanning calorimetry (DSC). The plasticizing efficiency was evaluated by measuring the physicomechanical properties as modulus of elasticity, tensile strength, percent of elongation and swelling ratio. The medicated films - plasticized or free - were clear and colorless. A plasticizer concentration of 20% (w/w of polymer weight) was sufficient to obtain flexible films with all tested samples. X-ray diffration patterns and DSC thermograms indicated an amorphous state of the films independent on the type of the plasticizer used. The results have showed that, incorporation of different polyols as plasticizers improves the consistency and the physicomechanical properties of the films. The plasticizers effect was dependant on the hydrophilicity and chemical structure of both plasticizer and polymer. The release profile of the drug was also significantly increased by addition of polyols as plasticizers. Moreover, the drug release pattern was found to follow Higuchidiffusion model.
2008
12
31
229
247
https://bpsa.journals.ekb.eg/article_64326_272ef9cec45ab50b800883142467491e.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2008
31
2
LIPOSOMES AS AN OCULAR DELIVERY SYSTEM FOR FLUCONAZOLE: IN-VIVO STUDY
F.
Habib
E.
Fouad
M.
Abdel-Rahman
Dina
Fathalla
The purpose of this study was to formulate topically effective controlled release ophthalmic fluconazole liposomal formulations using the reverse-phase evaporation technique. Soya bean phosphatidylcholine (PC) and cholesterol (Ch) in specific weight ratios were used. Selected formulations were tested for their in-vivo ocular antifungal effect. These included the neutral, the positively (using stearyl amine) and the negatively (using dicetyl phosphate) charged liposomes. A reproducible model of Candida keratitis in rabbits was performed and the effects of the prepared liposomes were better than a solution of fluconazole. The order of fluconazole liposomal formulations according to the time to achieve complete healing is arranged in a descending order: negatively charged liposomes > positively charged liposomes > neutral liposomes (7:4) > neutral liposomes (5:5) > fluconazole solution. The frequency of instillation was decreased; also, the time of ulcer healing was decreased. It was concluded that the use of liposomes as a drug delivery system could contribute to the enhancement of the effect of fluconazole in the eye.
2008
12
31
249
263
https://bpsa.journals.ekb.eg/article_64327_6b9ccb43ce23e22962767ca30bb9c8c9.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2008
31
2
PREPARATION, CHARACTERIZATION AND EVALUATION OF FAST-DISSOLVING SILIBININENRICHED SILYMARIN (SES)
Khaled
Khaled
The hepato-protective activity of silymarin is well demonstrated. However, silymarin is not a single component, but a mixture of silydianin, silychristin and silibinin. Silibinin is the least soluble and the most active component of silymarin. Accordingly, as silibinin content of silymarin increases, its activity is expected to increase. These were the objectives of the study i.e to prepare silibinin enriched silymarin (SES) and enhance its dissolution by preparing its adsorbates and co-adsorbates with Florite. Silibinin enriched silymarin was prepared by extracting the water soluble components of silymarin using water. The silibinin content of the SES was evaluated using HPLC method of assay. The fast dissolving SES systems were characterized using differential scanning calormetry, x-ray diffractometry and infra-red spectroscopy. The obtained results indicated the compatibility of Florite with SES. The biological activity of SES systems was evaluated in rats using paracetamol as a hepatotoxic agent and compared to that of silibinin alone. The results showed that SESco-adsorbate was more efficient in lowering the serum level of the specific liver enzymes (ALT and AST) than silibinin alone.
2008
12
31
265
280
https://bpsa.journals.ekb.eg/article_64328_8a6b4e166daab7a3c68fa7a577a3d757.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2008
31
2
COMBINED EFFECT OF CHEMICAL ENHANCERS AND ULTRASOUND ON THE SKIN PERMEATION OF CAFFEINE
Thanaa
E. Borg
The combined effect of 800 kHz ultrasound with 2W/cm2 intensity and chemical enhancers on the skin permeation of caffeine was investigated using excised ear rabbit skin. Menthol, laurocapram (Azone®), isopropyl myristate and ethanol were selected as enhancers. Caffeine permeation was increased upon incorporation of all enhancers. The steady state fluxes were 05.69, 10.13, 22.42 and 25.06 µg/cm2 per h with enhancement factor equals 1.38, 2.458, 5.441 and 6.083 for 40% EtOH, 10% IPM, 3% AZ and 5% M, respectively. Combined application of ultrasound and enhancers increased the skin permeation rate (flux) of caffeine compared with ultrasound or enhancers alone. The enhancement factor equals 1.485, 4.514, 18.572, and 48.610 for 40% EOH, 10% IPM, 3% AZ and 5% M respectively. Better effects were obtained by the combination with 5%M. The influence of detailed conditions of ultrasound and enhancer applications on the caffeine flux was further investigated using 5% M. Caffeine fluxes were, 95.254, 115.368 and 200.06 µg/cm2 per h upon application of ultrasound for 10, 30, and 60 min respectively.The enhancement effect by this combination was increased with an increase in ultrasonic application duration, suggesting that these conditions might be used to achieve the controlled drug delivery. A pretreatment experiment with ultrasound or 5% M was carried out, and the drug content was measured to understand the role of ultrasound in the combined effect. Pretreatment of the skin with ultrasound increased the caffeine flux, while the effect of pretreatment with 5% M on the skin was similar to that of untreated skin. The results obtained suggested that simultaneous application of ultrasound and enhancers is essential to obtain the pronounced effect for transdermal as well as for topical delivery of caffeine though the skin.
2008
12
31
281
292
https://bpsa.journals.ekb.eg/article_64330_93e77cf18cefc2b664c5f0351fff00d1.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2008
31
2
LIPOSOMES AS AN OCULAR DELIVERY SYSTEM OF FLUCONAZOLE: IN-VITRO STUDIES
F.
Habib
E.
Fouad
Dina
Fathalla
The purpose of this study was to formulate topically effective controlled release ophthalmic fluconazole liposomal formulations. Reverse-phase evaporation technique was used for the preparation of fluconazole liposomes consisting of phosphatidylcholine (PC) from soyabean and cholesterol (Ch) in weight ratios of (9:1), (7:2), (7:3), (7:4), (6:4), (7:6) and (5:5) with or without stearylamine (SA) or dicetyl phosphate (DP) as positive and negative charge inducers, respectively. The prepared liposomes were evaluated for their in-vitro release. The release mechanism was found to follow Higuchi and first order kinetics. Increasing cholesterol weight ratio in the prepared liposomal formulations progressively decreased the release of fluconazole from the vesicles. The positively charged liposomes showed slower rate of drug release compared to neutral ones. Negatively charged liposomes showed slight increase in the release rate and extent of fluconazole from the liposomal formulations 5:5:0.25 and 5:5:0.5; in comparison with neutral ones. Further increase in the amount of dicetyl phosphate 5:5:1 resulted in a significant decrease in the release rate.
Four fluconazole liposome eye drops were prepared. Physical stability study including, visual appearance, particle size and amount of drug leakage from liposome eye drops were studied. Approximately 82.82%, 76.55%, and 70.90% of fluconazole was retained in negative, positive and neutral liposomal ocular formulations up to a period of 24 weeks at 5°C.
2008
12
31
293
311
https://bpsa.journals.ekb.eg/article_64332_d0162a4c83ee2216caca866da88c7b4f.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2008
31
2
CYTOTOXICITY STUDY OF FERULA HERMONIS BOISS
Abdurrahim
Elouzi
Abdurazag
Auzi
Mazen
El-Hammadi
Alexander
Gray
Ferula hermonis Boiss (Apiaceae) is known in the Midleast as ‘zallouh’. In the last decade, scientists paid attention to study chemistry and biological activity of the plant. In this study Ferula hermonis were collected and evaluated for cytotoxic activity. The plant was extracted using different polarity solvents: petroleum ether, ethyl acetate and methanol. The cytotoxic effect of the extracts was examined in-vitro on human cell line (stomach cancer cell line, SCL-40). The assay was based on incubation of tetrazolium dye (MTT; a yellow water-soluble tetrazolium dye that is reduced by live, but not dead cells) with the cells that preincubated with a tested substance. A purple formazan product that produced can be determined spectrophotometrically. The result confirmed that the SCL-40 cells were much more sensitive to the petroleum extract than other extracts, which showed the prominent cytotoxicity. The plant showed pronounced cytotoxic activity will be further evaluated for the possible isolation of active antitumour compounds.
2008
12
31
313
317
https://bpsa.journals.ekb.eg/article_64335_1a8050d1b0a8e94637bbb4f8a1806f25.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2008
31
2
POLYPHENOLIC COMPOUNDS FROM THE LEAVES OF SCHINUS TEREBINTHIFOLIUS RADDI
Salwa
Farag
Two quinic acid esters, 5-O-caffeoylquinic acid (1) and 5-Ocoumaroylquinic acid (2); three myricetin glycosides, myricetin 3O -L-rhamnopyranosyl(1′′′ 6′′) -D-galactopyranoside (3), myricetin 3-O -D-glucuronide (4), and myricetin 3-O -Dgalactopyranoside (5); 1,6-digalloyl -D-glucose (6); and (+)catechin (7) were isolated and identified for the first time from the leaves of Schinus terebinthifolius Raddi. Furthermore, investigation of tannic acid content was carried out by HPLC.
2008
12
31
319
329
https://bpsa.journals.ekb.eg/article_64337_227e6fcaff1f0c6258f2e593b979ec4d.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2008
31
2
FORMULATION OF SITE-SPECIFIC MUCOADHESIVE LIQUID SUPPOSITORIES AS A METHOD TO DECREASE HEPATOTOXICITY IN RABBITS
E.
Ramadan
Th.
Borg
M.
Elkayal
Mucoadhesive liquid suppositories containing diclofenac sodium (DS) as a NSAID were prepared using poloxamers as a liquid suppository base. Various formulations composed of different ratios of P407 and P188 (10/20, 15/15, 21/9, 24/6 and 27/3% w/w of P 407/P188) were prepared. The physicochemical characters; the gelation temperature, gel strength and mucoadhesive properties of the prepared suppositories were evaluated and compared with conventional suppositories. The dissolution and pharmacokinetic parameters of DS from such suppositories were also estimated. It was also important to study the histopathological changes in rabbit rectum and liver after administration of liquid and conventional suppositories. The gelation temperatures were 49.5, 45.5, 32.5, 22.5 and 20.5°C for 10/20, 15/15, 21/9, 24/6 and 27/3% w/w of P407/P188, respectively. P407/P188 mixture in the concentration of 21/9%, w/w was selected as the system of choice since it exhibited adequate physicochemical properties. The addition of DS increased the gelation temperature (from 18 to 32.5°C) for 21/9 poloxamer mixture and reduced the gel strength (from 4.03 sec to 3.4 sec) and the mucoadhesive force (from 3.5 to 1.72 x 102 dyne/cm2). It was found that the dissolution of DS-loaded poloxamer-based suppositories was significantly higher than that from the conventional suppositories (51.3 versus 26.7%, respectively). Furthermore, the pharmacokinetic study showed that DS-loaded poloxamer-based suppositories gave significantly higher initial plasma concentrations, AUC (70.313 µg. hr/ml) and Cmax (29.417 µg/ml) of DS than did conventional suppositories (55.023 µg.hr/ml and 22 µg/ml), respectively. Histopathological study of rectal tissues indicated no pathological damage after 6h of rectal administration. The histopathological study of liver tissues revealed that no hepatocellular damage occurred after 30 days of administration of DSloaded poloxamer-based suppository; however hepatotoxicity could not be totally avoided by rectal administration of conventional suppositories. DS-loaded poloxamer-based suppository was an effective rectal dosage form with alleviated adverse effects.
2008
12
31
331
344
https://bpsa.journals.ekb.eg/article_64339_07834f78d4b2a23b24612da2dac74125.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2008
31
2
MYCOFLORA, MYCOTOXINS, BACTERIOLOGICAL ANALYSIS AND MOLECULAR ASSAY OF SOME BACTERIAL SPECIES FROM COFFEE BEANS IN SAUDI ARABIA
Laila
Nasser
The mycoflora analysis of some coffee beans in Saudi Arabia showed a wide range of fungal contamination in 31 samples collected from different markets in El-Riyadh. Thirty four species belonging to 16 genera and 28 species belonging to 18 genera were isolated from coffee beans on glucose and cellulose Czapek's agar medium at 25°C from seed-plate method. Aspergillus niger and A. flavus were the most prevalent species, but Penicilliun oxalicum was isolated in moderate occurrence, while 12 genera comprised 16 species and 8 genera comprised 10 species were isolated on the same types of media at 25°C from seed suspension method. A. niger was the most common species, while A. flavus and P. funiculosum were isolated in moderate occurrence. A. niger, also was the most prevalent on 20% sucrose-Czapek's agar medium at 25°C, but the genus Eurotium (3 spp) appeared in moderate occurrence. Five fungal species belonging to four genera were isolated on starch yeast extract agar medium at 45°C. A. fumigatus and A.niger were the most prevalent thermo tolerant species, while three species of thermophilic fungi were of low or rare incidence. Thin layer chromatographic analysis of chloroform extracts of 31 coffee beans samples revealed that 20 samples were free from mycotoxins, while 11 samples were contaminate with aflatoxins B1, B2, G1 and G2 of concentrations ranged from 110-600 ug/kg, but 6 samples were contaminate with sterigmatocystin ranged from 60600 ug/kg. Screening of the characteristic mycotoxins of 25 fungal isolates revealed that 17 of them produced, aflatoxin B1 at 450 ug/kg, ochratoxin A at 600 ug/kg, ochratoxin B at 400 ug/kg, and sterigmatocystin 280 ug/kg from Aspergillus species, while three isolates of Penicillium produced penicillic acid (ranged from 720240 ug/kg) and one isolate of Trichoderma produced Trichodermine at 360 ug/kg. The bacteriological analysis of the coffee bean samples indicated that Bacillus cereus was detected in six samples at levels (2x10 cfu/g), E. coli in two samples (14x10 and 89x10 cfu/g), Feacal coliform was detected in one sample only,while Staphylococcus appeared in 29 samples (55x103 cfu/g). All samples were free from Salmonella. PCR assay for detection of some bacterial species revealed that all samples were negative for Yersinia enterocolitica, Campylobacter and Listeria monocytogenes, while the results of B. cereus and Salmonella were similar to the results obtained using cultural method.
2008
12
31
345
373
https://bpsa.journals.ekb.eg/article_64340_0524c60b48d6bdda8af9c0bd3adb5f97.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2008
31
2
SYNTHESIS OF SOME NOVEL 1, 3, 5-TRISUBSTITUTED [1,2,4]TRIAZOLE DERIVATIVES AS POTENTIAL ANTIBACTERIAL AGENTS
Alaa
Hayallah
Helal
Heta
In the present work, some new 1,3,5-trisubstituted[1,2,4]triazole derivatives and their Schiff's bases were synthesized. The chemical structure of the target compounds was confirmed by IR, 1H-NMR, 13C-NMR, FAB-MS, EI-HRMS spectra and elemental analyses. The title compounds were tested for their in vitro antibacterial activity against Gram-positive and Gram-negative ones using ampicillin and nalidixic acid as reference drugs. Some of them showed antibacterial activity more significant than the reference drugs.
2008
12
31
375
390
https://bpsa.journals.ekb.eg/article_64342_7a69ef227b2c85a8e2fcd6861b6fd8ec.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2008
31
2
ANTITUMOR ACTIVITY OF SOME NEW 1,3,8TRISUBSTITUTED PURINE-2,6-DIONES AND 1,3,6TRISUBSTITUTED THIAZOLO[2,3-f]PURINE-2,4DIONES
Alaa
Hayallah
Georgi
Momekov
Michael
Famulok
New 1,3,8-trisubstituted purine-2,6-diones and 1,3,6trisubstituted thiazolo[2,3-f]purine-2,4-diones were designed and synthesized as potential antitumor agents. The cytotoxic effects of the tested compounds were assessed against two human malignant cell lines: T-cell leukemia derived SKW-3 and breast cancer – derived MDA-MB-231 using the methyl thiazolyl tetrazolium (MTTdye) reduction assay, after 72 h exposure. The data were fitted to sigmoidal concentration response curves and the corresponding IC50 values were calculated using commercially available software (GraphPad Prizm). Compound AH-206 was the most potent cytotoxic agent among the newly synthesized compounds, with IC50 value of 17.3 M. Prominent activity was also encountered with compounds AH-201, AH-205, AH-208, AH-214 and AH-217, all having IC50 values below 100 µM.
2008
12
31
391
399
https://bpsa.journals.ekb.eg/article_64344_93e3a10aa8bd960a25a82e380cb9a8ca.pdf