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Sci. Pharm.
Volume 77
Issue 1
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Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Previous articles were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence, and they are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).

Sci. Pharm., Volume 77, Issue 1 (March 2009) – 14 articles

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131 KiB  
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Author Index (Conference)
by Scientia Pharmaceutica Editorial Office
Sci. Pharm. 2009, 77(1), 271-292; https://doi.org/10.3797/scipharm.oephg.21.PO-71 - 16 Apr 2009
Viewed by 960
Abstract
n/a Full article
160 KiB  
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Kurzfassungen der Vorträge und Poster der 21. Wissenschaftlichen Tagung der Österreichischen Pharmazeutischen Gesellschaft (ÖPhG), 16. bis 18. April 2009, Wien, Österreich
by Scientia Pharmaceutica Editorial Office
Sci. Pharm. 2009, 77(1), 143-162; https://doi.org/10.3797/scipharm.oephg.21.CT-01 - 16 Apr 2009
Viewed by 1047
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n/a Full article
210 KiB  
Article
Alcohol Dehydrogenases as Tools for the Preparation of Enantiopure Metabolites of Drugs with Methyl Alkyl Ketone Moiety
by Elżbieta PĘKALA and Dorota ŻELASZCZYK
Sci. Pharm. 2009, 77(1), 9-18; https://doi.org/10.3797/scipharm.0901-26 - 17 Feb 2009
Cited by 7 | Viewed by 1321
Abstract
Three dehydrogenases – (R)-alcohol dehydrogenase from L. kefir, (S)-aromatic alcohol dehydrogenase from T. sp. and (S)-alcohol dehydrogenase from T. brockii – were tested for the preparation of enantiopure hydroxyl metabolites of pentoxifylline (PTX), propentofylline (PPT) and [...] Read more.
Three dehydrogenases – (R)-alcohol dehydrogenase from L. kefir, (S)-aromatic alcohol dehydrogenase from T. sp. and (S)-alcohol dehydrogenase from T. brockii – were tested for the preparation of enantiopure hydroxyl metabolites of pentoxifylline (PTX), propentofylline (PPT) and denbufylline (DBF). These metabolites have an important pharmacological significance. The experimental conditions were optimized for biocatalytic reactions. LKADH produced the chiral secondary alcohols: (R)-OHPTX, (R)-OHPPT and (R)-OHDBF, in an anti- Prelog’s rule configuration. In contrast, TBADH and SAADH also generated chiral secondary alcohols, but according to Prelog’s rule, giving (S)-OHPTX, (S)-OHPPT and (S)-OHDBF respectively. All the ADHs tested were characterized by a high enantioselectivity (ees of 99–100%), but the yield of bioconversion was only satisfactory for the reactions performed using LKADH, being in the 96–98% range for PPT and PTX respectively. Full article
318 KiB  
Article
Isolation and Characterization of an Impurity Obtained During the Synthesis of the Antibiotic Drug Sparfloxacin
by Nirmala MUNIGELA, Moses BABU J., Anjaneyulu YERRAMILLI, Peddy VISHWESHWAR, Ganesh YADDANAPUDI SESHA SIVA YADDANAPUDI SESHA SIVA and Narayana Murthy VALAVALA
Sci. Pharm. 2009, 77(1), 67-78; https://doi.org/10.3797/scipharm.0812-12 - 5 Feb 2009
Cited by 1 | Viewed by 1340
Abstract
During the synthesis of Sparfloxacin, a fluoroquinolone antibiotic drug, an unknown impurity (SF5-IMP) was identified in the fifth stage of the synthetic process. The impurity has been isolated from the mother liquor of intermediate SF5. The mother liquor was concentrated [...] Read more.
During the synthesis of Sparfloxacin, a fluoroquinolone antibiotic drug, an unknown impurity (SF5-IMP) was identified in the fifth stage of the synthetic process. The impurity has been isolated from the mother liquor of intermediate SF5. The mother liquor was concentrated to dryness added dichloromethane and stirred for 1 h and filtered to generate SF5-IMP and the molecular structure was elucidated as 7-amino-1-cyclopropyl-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline- 3-carboxylic acid by 19F NMR and single crystal X-ray diffraction studies. The structural features of SF5-IMP and SF5 have been discussed here. Full article
184 KiB  
Article
Short Total Synthesis of the Marine Alkaloid Subarine
by Matthias LOTTER and Franz BRACHER
Sci. Pharm. 2009, 77(1), 1-8; https://doi.org/10.3797/scipharm.0901-14 - 5 Feb 2009
Cited by 16 | Viewed by 1594
Abstract
The marine benzo[c][2,7]naphthyridine alkaloid subarine is prepared in 4 steps, starting from commercially available 1,10-phenanthroline, via oxidative cleavage to the bipyridine-dicarboxylate, conversion to the mono(2-iodoanilide), and radical cyclization. The alkaloid does not show any significant antimicrobial or cytotoxic activity. Full article
239 KiB  
Article
Antioxidative and Antiinflammatory Activities of the Chloroform Extract of Ganoderma lucidum Found in South India
by Soniamol JOSEPH, Baby SABULAL, Varughese GEORGE, Thozhuthumparambal P. SMINA and Kainoor K. JANARDHANAN
Sci. Pharm. 2009, 77(1), 111-122; https://doi.org/10.3797/scipharm.0808-17 - 30 Jan 2009
Cited by 60 | Viewed by 3330
Abstract
Antioxidative and anti-inflammatory activities of Ganoderma lucidum (Curt.: Fr.) P. Karst. (Aphyllophoromycetideae) from tropical South India were investigated. The chloroform extract of the mushroom showed marked free radical scavenging activities. The anti-inflammatory activity of the extract at concentrations of 100 and 50 mg/kg [...] Read more.
Antioxidative and anti-inflammatory activities of Ganoderma lucidum (Curt.: Fr.) P. Karst. (Aphyllophoromycetideae) from tropical South India were investigated. The chloroform extract of the mushroom showed marked free radical scavenging activities. The anti-inflammatory activity of the extract at concentrations of 100 and 50 mg/kg was evaluated in carrageenan induced acute and formalin induced chronic inflammatory models in mice. The extract showed remarkable antiinflammatory activity in both models, comparable to the standard reference drug diclofenac. The results suggest that anti-inflammatory activity of the chloroform extract of G. lucidum is possibly attributed to its free radical scavenging properties. This study also reveals the potent therapeutic uses of G. lucidum from South India. Full article
215 KiB  
Article
Insight into the Structural Requirement of 2-Alkyl-4-(biphenylmethoxy)quinolines as Nonpeptide Angiotensin II Receptor Antagonists: A QSAR Approach
by Vivek K. VYAS, Anurekha JAIN, Suresh C. MAHAJAN, Radheshyam PATIDAR, Sunil MISTRY and Subhash C. CHATURVEDI
Sci. Pharm. 2009, 77(1), 33-46; https://doi.org/10.3797/scipharm.0810-01 - 14 Jan 2009
Cited by 3 | Viewed by 1155
Abstract
In the current study a quantitative structure activity relationship approach using sequential multiple linear regression analysis was applied to a series of 2-alkyl- 4-(biphenylylmethoxy)quinolines as angiotensin II (Ang II) receptor antagonists by using Chem 3D and Dragon Software. The studies, carried out on [...] Read more.
In the current study a quantitative structure activity relationship approach using sequential multiple linear regression analysis was applied to a series of 2-alkyl- 4-(biphenylylmethoxy)quinolines as angiotensin II (Ang II) receptor antagonists by using Chem 3D and Dragon Software. The studies, carried out on 33 analogs, give statistically significant correlations of selective Ang II antagonistic activity with physical properties concerning size, symmetry, shape and distribution of molecule atoms. Among several 2D quantitative structure activity relationship models, one model gave good statistical significance (r > 0.81, Ftest = 10.47, S < 0.30, chance correlation < 0.01). 3D QSAR studies show that Hennery’s law constant, Dipole and VDWE play a significant role in Ang II antagonistic activity. These QSAR studies help us in the design and prediction of novel substituted benzimidazole Ang II receptor antagonists. Full article
1893 KiB  
Article
Viability of the Human Adenocarcinoma Cell Line Caco-2: Influence of Cryoprotectant, Freezing Rate, and Storage Temperature
by Iris GÜLL, Paula MARQUES ALVES, Franz GABOR and Michael WIRTH
Sci. Pharm. 2009, 77(1), 133-142; https://doi.org/10.3797/scipharm.0810-07 - 9 Jan 2009
Cited by 3 | Viewed by 1607
Abstract
The freezing process as well as cryostorage may induce molecular and cellular changes due to osmotic stress. Currently, standard protocols for cryopreservation of mammalian cells recommend slow freezing and rapid thawing to avoid intracellular ice crystal formation and osmotic damage. As an appropriate [...] Read more.
The freezing process as well as cryostorage may induce molecular and cellular changes due to osmotic stress. Currently, standard protocols for cryopreservation of mammalian cells recommend slow freezing and rapid thawing to avoid intracellular ice crystal formation and osmotic damage. As an appropriate freezing process should guarantee adequate cell viability, we evaluated the impact of two cryoprotectants, a commercially available cryopreservation medium, two freezing rates, as well as two storage temperatures on the viability of Caco-2 cells. The freezing parameters were optimized by carefully determining vitality, cell count, proliferation, and functional differentiation of the cells. Though at least 90% of the cells were viable after one freezing/thawing cycle, adequate recovery of proliferation and differentiation is obtained not until 10 days post thawing. Interestingly, addition of 10% PEG 200 as cryoprotectant yielded best results. All in all, our results should give valuable advice for the optimization of the cryopreservation protocol of individual cell lines. Full article
198 KiB  
Article
Biotransformation of Artemisinin Mediated through Fungal Strains for Obtaining Derivatives with Novel Activities
by Suchita SRIVASTAVA, Suaib LUQMAN, Atiya FATIMA, Mahendra P. DAROKAR, Arvind S. NEGI, J. K. KUMAR, K. SHANKER, Chandan S. CHANOTIYA, Sudeep TANDON and Suman P. S. KHANUJA
Sci. Pharm. 2009, 77(1), 87-96; https://doi.org/10.3797/scipharm.0803-15 - 8 Jan 2009
Cited by 19 | Viewed by 1969
Abstract
Artemisinin, a sesquiterpene lactone, is the active antimalarial constituent of Artemisia annua. Several fungal strains Saccharomyces cerevisiae, Aspergillus flavus, Aspergillus niger and Picchia pastoris were used to biotransform artemisinin. Among these strains, A. flavus was the only microorganism capable of [...] Read more.
Artemisinin, a sesquiterpene lactone, is the active antimalarial constituent of Artemisia annua. Several fungal strains Saccharomyces cerevisiae, Aspergillus flavus, Aspergillus niger and Picchia pastoris were used to biotransform artemisinin. Among these strains, A. flavus was the only microorganism capable of transforming artemisinin to deoxyartemisinin in higher yields than the previous reports. The structure of deoxyartemisinin was elucidated by spectroscopy. Deoxyartemisinin showed antibacterial activity against Staphylococcus aureus, S. epidermidis and S. mutans at a minimum inhibitory concentration (MIC) of 1 mg/mL compared to artemisinin whose MIC was >2 mg/mL. Full article
518 KiB  
Article
Evaluation of the Anabolic, Aphrodisiac and Reproductive Activity of Anacyclus Pyrethrum DC in Male Rats
by Vikas SHARMA, Mayank THAKUR, Nagendra Singh CHAUHAN and Vinod Kumar DIXIT
Sci. Pharm. 2009, 77(1), 97-110; https://doi.org/10.3797/scipharm.0808-14 - 23 Dec 2008
Cited by 57 | Viewed by 4614
Abstract
Anacyclus pyrethrum DC (Compositae), commonly referred to as ‘Akarkara’, is widely recognized in Ayurvedic system of Indian medicine as tonic and rejuvenator. The roots are also considered aphrodisiac and sexual stimulant. Aqueous extract of the roots was studied for its effect on sexual [...] Read more.
Anacyclus pyrethrum DC (Compositae), commonly referred to as ‘Akarkara’, is widely recognized in Ayurvedic system of Indian medicine as tonic and rejuvenator. The roots are also considered aphrodisiac and sexual stimulant. Aqueous extract of the roots was studied for its effect on sexual behavior, spermatogenesis, and sperm count. Fructose levels in seminal vesicles of albino rats were also recorded. Two doses i.e. 50 and 100 mg/kg of aqueous extract on administration in albino rats showed pronounced anabolic and spermatogenic effect in animals of respective groups. The sperm count and fructose levels in seminal vesicle were markedly increased. Improvement in sexual behavior of male rats was characterized by increased mount and intromission frequency and reduced mount and intromission latency. The extract had a dose dependent influence on sperm count and seminal fructose concentration which increased significantly. Full article
277 KiB  
Article
Rapid HPLC Analysis for Quantitative Determination of the Two Isomeric Triterpenic Acids, Oleanolic acid and Ursolic acid, in Plantago Major
by Marina ZACCHIGNA, Francesca CATENI, Mariangela FAUDALE, Silvio SOSA and Roberto DELLA LOGGIA
Sci. Pharm. 2009, 77(1), 79-86; https://doi.org/10.3797/scipharm.0809-08 - 23 Dec 2008
Cited by 21 | Viewed by 3480
Abstract
Plantago major has been used in traditional medicine for the treatment of various diseases. In order to evaluate the quality of P. major, a simple, rapid and accurate high-performance liquid chromatography (HPLC) method was developed for the assessment of the two bioactive [...] Read more.
Plantago major has been used in traditional medicine for the treatment of various diseases. In order to evaluate the quality of P. major, a simple, rapid and accurate high-performance liquid chromatography (HPLC) method was developed for the assessment of the two bioactive triterpenic acids: oleanolic acid (OA) and ursolic acid (UA). A LiChrosorb octadecylsilyl silica (ODS) column with methanol, tetrahydrofuran and aqueous acetic acid as mobile phase and detection at 220 nm were employed for HPLC analysis. The method is precise with relative standard deviations for these two constituents that ranged between 0.5–1.1% (intraday) and 0.8–1.8% (interday). The contents of these two phytochemicals in the leaves of P. major growing in Friuli Venezia Giulia Region were determined in order to establish an effective and reproducible method. Full article
259 KiB  
Article
Synthesis of Novel 1,3-Diacetoxy-Acridones as Cytotoxic Agents and their DNA-Binding Studies
by N. K. SATHISH, V. V. S. RAJENDRA PRASAD, N. M. RAGHAVENDRA, S. M. SHANTA KUMAR and Y. C. MAYUR
Sci. Pharm. 2009, 77(1), 19-32; https://doi.org/10.3797/scipharm.0811-03 - 19 Dec 2008
Cited by 19 | Viewed by 1499
Abstract
A series of novel substituted acridones (1–15) have been synthesized. Their in vitro cytotoxicity against human breast adenocarcinoma (MCF-7) and human promyelocytic leukemia (HL-60) cell lines has been investigated. The compounds 11, 12, 14 and 15 showed [...] Read more.
A series of novel substituted acridones (1–15) have been synthesized. Their in vitro cytotoxicity against human breast adenocarcinoma (MCF-7) and human promyelocytic leukemia (HL-60) cell lines has been investigated. The compounds 11, 12, 14 and 15 showed moderate activity against MCF-7 cell lines with IC50 value < 5.83 μM. The compounds 8, 10–12, and 15 showed moderate activity against HL-60 cell lines with IC50 value < 1.75 μM. The DNAbinding properties of the compounds were evaluated based on their affinity or intercalation with CT-DNA measured with absorption titration. The compound 12 bearing planar diacetoxy tricyclic ring linked with butyl piperidine side chain showed highest binding affinity with binding constant (Ki) 10.38 ×10 ×M–1. The examination of the relationship between lipophilicity and cytotoxic properties of acridones showed a poor correlation. Full article
512 KiB  
Article
Development of a Sensitive and Stereoselective HPLC Method for the Analysis of Pindolol in Plasma and Pharmaceutical Products Using a Chiralpak IB Column and Fluorescence Detection
by Mohamed HEFNAWY, Mohamed KASSEM, Haba ABDINE and Nourah AL-ZOMAN
Sci. Pharm. 2009, 77(1), 47-66; https://doi.org/10.3797/scipharm.0809-04 - 18 Dec 2008
Cited by 1 | Viewed by 1390
Abstract
A sensitive and stereoselective HPLC method has been developed for the simultaneous determination of pindolol enantiomers in plasma and pharmaceutical products. Enantiomeric resolution was achieved on a cellulose tris(3,5-dimethylphenylcarbamate) immobilized onto a 5 μm spherical porous silica chiral stationary phase (CSP) known as [...] Read more.
A sensitive and stereoselective HPLC method has been developed for the simultaneous determination of pindolol enantiomers in plasma and pharmaceutical products. Enantiomeric resolution was achieved on a cellulose tris(3,5-dimethylphenylcarbamate) immobilized onto a 5 μm spherical porous silica chiral stationary phase (CSP) known as Chiralpak IB with fluorescence detection set at 266 nm for excitation and 308 nm for emission. The mobile phase consists of n-hexane–isopropanol–triethylamine, (50:50:0.5), (v/v/v) has been used at a flow rate of 1.0 ml/min. The method was highly specific where other coformulated drugs such as clopamide and isosorbide did not interfere. The stability of pindolol enantiomers under different degrees of temperature was studied. The method validated for its linearity, accuracy, precision and robustness. There was no significant difference (p>0.05) between inter- and intra-day studies for each enantiomers which confirmed the reproducibility of the assay method. Preliminary data suggest that S-(−)-pindolol induces less bradycardia but more sedation and central nervous system depression than racemic pindolol. Full article
200 KiB  
Article
Pharmacokinetic Evaluation of Wheat Germ Agglutinin-Grafted Nanoparticles of Mometasone Furoate
by Naazneen SURTI, Sachin NAIK and Ambikanandan MISRA
Sci. Pharm. 2009, 77(1), 123-132; https://doi.org/10.3797/scipharm.0803-13 - 13 Dec 2008
Cited by 6 | Viewed by 1493
Abstract
The aim of the investigation was to assess the pharmacokinetic parameters of wheat germ agglutinin (WGA)-grafted nanoparticles of mometasone furoate (MF), after intratracheal instillation in rats. PLGA (50:50) nanoparticles (NPs) loaded with MF were prepared by emulsion-solvent evaporation technique. WGA was conjugated to [...] Read more.
The aim of the investigation was to assess the pharmacokinetic parameters of wheat germ agglutinin (WGA)-grafted nanoparticles of mometasone furoate (MF), after intratracheal instillation in rats. PLGA (50:50) nanoparticles (NPs) loaded with MF were prepared by emulsion-solvent evaporation technique. WGA was conjugated to spherical MF loaded nanoparticles by carbodiimide coupling yielding a ligand density of 10-15μg WGA / mg NP. The nanoparticles were characterized for size, zeta potential, entrapment efficiency and in-vitro drug release. Plain drug, MF nanoparticles and WGA-grafted MF nanoparticles were administered intratracheally in rats and at different time intervals drug levels in the lung tissue and bronchoalveolar lavage (BAL) were estimated using HPLC. Cumulative MF-release from unconjugated and conjugated MFnanoparticles after 2 weeks was 68% and 55% of the initial drug loading. From the lung MF concentration vs time plot, AUC for WGA-MF-NPs and MF-NPs was found to be 5.9 and 3.8 times higher than AUC for plain MF. This improvement of intracellular drug uptake by means of WGA-conjugation might be due to bioadhesive nature of the lectin which provides an intimate contact to lung mucosal cells followed by facilitated transcytosis as confirmed by improved pharmacokinetic behaviour. All in all, these findings are expected to contribute for better management of asthma to overcome the limitation of short lived action associated with dry powder inhalers. Full article
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