Scientia Pharmaceutica

14 pages, 906 KB

Open AccessArticle

A Rapid, Cost-Effective Pre-Clinical Method to Screen for Pro- or Antiarrhythmic Effects of Substances in an Isolated Heart Preparation

by John Joseph BORG^1,2

¹ 8, No 40 Dingli Court, Howard Str, Sliema, SLM 1751, Malta.

² Department of Pharmacology, Medical School, University of Bristol, BS81TD, United Kingdom.

Sci. Pharm. 2015, 83(2), 339-352; https://doi.org/10.3797/scipharm.1503-03 - 13 Apr 2015

Cited by 1 | Viewed by 1701

Abstract

This study describes a rapid, cost-effective pre-clinical method to screen for pro- or antiarrhythmic effects of substances in an isolated heart preparation in line with the regulatory requirements of ICHS7B. The computational method “MFC method” quantifies arrhythmic episodes from isolated perfused hearts based [...] Read more.

This study describes a rapid, cost-effective pre-clinical method to screen for pro- or antiarrhythmic effects of substances in an isolated heart preparation in line with the regulatory requirements of ICHS7B. The computational method “MFC method” quantifies arrhythmic episodes from isolated perfused hearts based on measuring the variation in the maximum force of contraction. Experiments were performed on hearts isolated from male Wistar rats. Arrhythmias were induced by the addition of tefluthrin or by ligation of the left coronary artery. The “MFC method” accurately measures the maximum force of every myocardial contraction and correlates it with the magnitude of the preceding beat. Arrhythmias were quantified by determining the coefficient of variation in the maximum force of contraction. This method is a useful approach to quickly identify the pro- or antiarrhythmic effects of drugs prior to more detailed analysis; particularly where the effects are varied and not easily classified under the Lambeth Conventions. Therefore, the “MFC method” can be used as a rapid screen for the antiarrhythmic effects of novel compounds or for rapidly determining potential cardiac toxicity. Full article

10 pages, 317 KB

Open AccessArticle

A Validated HPLC/MS Limit Test Method for a Potential Genotoxic Impurity in Cilostazol and its Quantification in the API and in the Commercially Available Drug Product

by Luigi BRAY, Luca MONZANI, Enrico BRUNOLDI^* and Pietro ALLEGRINI

R&D Department, Dipharma Francis srl, Via Bissone 5, Baranzate (MI), Italy.

Sci. Pharm. 2015, 83(2), 269-278; https://doi.org/10.3797/scipharm.1502-05 - 26 Mar 2015

Cited by 3 | Viewed by 2755

Abstract

Cilostazol is a selective inhibitor of type 3 phosphodiesterase. 5-(3-Chloro-propyl)-1-cyclohexyl-1H-tetrazole, used as an intermediate in the synthesis of cilostazol, has a primary alkyl chloride group, a well-known alerting function for genotoxic activity. Upon request from a regulatory agency, a limit test [...] Read more.

Cilostazol is a selective inhibitor of type 3 phosphodiesterase. 5-(3-Chloro-propyl)-1-cyclohexyl-1H-tetrazole, used as an intermediate in the synthesis of cilostazol, has a primary alkyl chloride group, a well-known alerting function for genotoxic activity. Upon request from a regulatory agency, a limit test in accordance with ICH Q2(R1) added with the accuracy of a recovery test of 5-(4-chlorobutyl)-1-cyclohexyl-1H-tetrazole in cilostazol was developed and validated. The application of the method highlighted the need to optimize the purification process to ensure levels of this potential genotoxic impurity in the final active pharmaceutical ingredient below the established limit. Also, the analytical method was suitable to determine the amount of the impurity in samples of the commercially available drug product, which showed the levels to be above the established threshold of toxicological concern (TTC). Full article

10 pages, 146 KB

Open AccessArticle

FT-IR Method for the Quantification of Isoflavonol Glycosides in Nutritional Supplements of Soy (Glycine max (L.) MERR.)

by Katharina MULSOW, Juliane EIDENSCHINK, and Matthias F. MELZIG^*

Institute of Pharmacy, Department of Pharmaceutical Biology, Freie Universitaet Berlin, Königin-Luise-Str. 2+4, 14195 Berlin, Germany.

Sci. Pharm. 2015, 83(2), 377-386; https://doi.org/10.3797/scipharm.1410-02 - 6 Mar 2015

Cited by 5 | Viewed by 2223

Abstract

Due to increasing health consciousness, a lot of food supplements are sold and used. Dietary supplements of Glycine max (L.) MERR. are used as an alternative treatment for menopausal complaints such as hot flashes. Thereby, the effective soy compounds are the isoflavones daidzin, [...] Read more.

Due to increasing health consciousness, a lot of food supplements are sold and used. Dietary supplements of Glycine max (L.) MERR. are used as an alternative treatment for menopausal complaints such as hot flashes. Thereby, the effective soy compounds are the isoflavones daidzin, genistin, and glycitin. However, only the total soy extract content of the nutritional supplements is indicated. The aim of this study is to introduce a fast, efficient, and economic Fourier transformation infrared (FT-IR) spectroscopy method to quantify the active ingredients in the complex matrix of soy-based supplements. Five different nutritional supplements of Glycine max (L.) MERR. were purchased from a German pharmacy and were extracted with 80% aqueous methanol. A high-performance liquid chromatography (HPLC) method was used for the separation. The samples were concentrated and measured with infrared spectroscopy. An FT-IR method was established to quantify the active ingredients in the complex matrix of soy-based nutritional supplements. The partial least-squares algorithm was used to develop the method, which enabled the estimation of the content of particular isoflavones (daidzin R² = 0.86, glycitin R² = 0.94, genistin R² = 0.96) and the quantification of the total isoflavone content (R² = 0.92) despite peak overlap in the infrared (IR) spectra. The method for the quantification of the isoflavonol glycosides is precise with the standard error of prediction being 13.54%. Full article

10 pages, 139 KB

Open AccessArticle

Suppression of IgM Proteolysis by Conformational Stabilization Through Excipients

by Monika MUELLER^1,2,*, Maybelle Q. T. LOH² and Pete GAGNON²

¹ Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Althanstrasse 14, A-1090 Vienna, Austria.

² Bioprocessing Technology Institute, A*STAR, 20 Biopolis Way, #06-01, Centros, 138668, Singapore.

Sci. Pharm. 2015, 83(2), 401-410; https://doi.org/10.3797/scipharm.1501-12 - 4 Mar 2015

Cited by 5 | Viewed by 2120

Abstract

Protease activity from host cell lines may cause product loss or affect the quality of recombinant proteins. In this study, we showed that excipients like glycine and sorbitol reduce the proteolysis of an immunoglobulin M (IgM) in the presence of added proteases like [...] Read more.

Protease activity from host cell lines may cause product loss or affect the quality of recombinant proteins. In this study, we showed that excipients like glycine and sorbitol reduce the proteolysis of an immunoglobulin M (IgM) in the presence of added proteases like α-chymotrypsin, papain, and pepsin. The activity of the proteases in the IgM-protective environments was conserved or even enhanced as tested using low molecular weight substrates. Thus, a higher resistance against proteolytic degradation appears to be caused by the conformational stabilization of the IgM due to preferential exclusion of sorbitol and glycine. Full article

11 pages, 296 KB

Open AccessArticle

Synthesis and Anti-Platelet Activity of Thiosulfonate Derivatives Containing a Quinone Moiety

by Khrystyna BOLIBRUKH¹, Svyatoslav POLOVKOVYCH^1,*, Omar KHOUMERI², Tetyana HALENOVA³, Irina NIKOLAEVA³, Olexiy SAVCHUK³, Thierry TERME², Patrice VANELLE², Vira LUBENETS¹ and Volodymyr NOVIKOV^1,*

¹ Department of Technology of Biologically Active Substances, Pharmacy and Biotechnology, Lviv Polytechnic National University, Bandera Str. 12, 79013, Lviv, Ukraine.

² Laboratoire de Pharmaco-Chimie Radicalaire, Institut de Chimie Radicalaire ICR, Faculté de Pharmacie, Aix-Marseille Univ, CNRS, UMR 7273, Bd J. Moulin 27, 13385, Marseille Cedex 05, France.

³ Educational and Scientific centre “Institute of Biology”, Taras Shevchenko National University of Kyiv, Volodymyrska Str. 64/13, 01601, Kyiv, Ukraine

Sci. Pharm. 2015, 83(2), 221-231; https://doi.org/10.3797/scipharm.1411-14 - 24 Feb 2015

Cited by 19 | Viewed by 2180

Abstract

Thiosulfonate derivatives based on quinones were synthesized for studying “structure-activity relationship” compounds with an acylated and a free amino-group. Anti-platelet activity of the synthesized compounds was determined and the influence of substituents on the activity of the derivatives was assessed. Full article

8 pages, 427 KB

Open AccessArticle

An Efficient, Robust, and Inexpensive Grinding Device for Herbal Samples like Cinchona Bark

by Steen Honoré HANSEN^1,*, Else HOLMFRED¹, Claus CORNETT¹, Carla MALDONADO² and Nina RØNSTED²

¹ Analytical Biosciences, Dept. of Pharmacy, Fac. of Health and Med. Sci., Univ. of Copenhagen, Denmark.

² Natural History Museum of Denmark, University of Copenhagen, Denmark.

Sci. Pharm. 2015, 83(2), 369-376; https://doi.org/10.3797/scipharm.1410-14 - 19 Feb 2015

Cited by 7 | Viewed by 2599

Abstract

An effective, robust, and inexpensive grinding device for the grinding of herb samples like bark and roots was developed by rebuilding a commercially available coffee grinder. The grinder was constructed to be able to provide various particle sizes, to be easy to clean, [...] Read more.

An effective, robust, and inexpensive grinding device for the grinding of herb samples like bark and roots was developed by rebuilding a commercially available coffee grinder. The grinder was constructed to be able to provide various particle sizes, to be easy to clean, and to have a minimum of dead volume. The recovery of the sample when grinding as little as 50 mg of crude Cinchona bark was about 60%. Grinding is performed in seconds with no rise in temperature, and the grinder is easily disassembled to be cleaned. The influence of the particle size of the obtained powders on the recovery of analytes in extracts of Cinchona bark was investigated using HPLC. Full article

18 pages, 329 KB

Open AccessArticle

Validated Stability-Indicating RP-HPLC Method for the Estimation of Degradation Behaviour of Organic Peroxide and Third-Generation Synthetic Retinoids in Topical Pharmaceutical Dosage Formulation

by Chinmoy ROY^1,2,*, Lalatendu PANIGRAHI¹ and Jitamanyu CHAKRABARTY²

¹ Analytical Research and Development, Integrated Product Development, Dr. Reddy’s Laboratories Ltd., Bachupally, Hyderabad-500090, Andhra Pradesh, India.

² Department of chemistry, National Institute of Technology, Durgapur-713209, West Bengal, India.

Sci. Pharm. 2015, 83(2), 321-338; https://doi.org/10.3797/scipharm.1412-10 - 11 Feb 2015

Cited by 11 | Viewed by 3263

Abstract

The objective of the current study was to establish a validated stability-indicating, high-performance liquid chromatographic method to determine the purity of benzoyl peroxide (BPO) and adapalene (ADP) in the presence of its impurities, forced degradation products, and placebo in pharmaceutical dosage forms. The [...] Read more.

The objective of the current study was to establish a validated stability-indicating, high-performance liquid chromatographic method to determine the purity of benzoyl peroxide (BPO) and adapalene (ADP) in the presence of its impurities, forced degradation products, and placebo in pharmaceutical dosage forms. The desired chromatographic separation was achieved on the KinetexTM C18 (250 × 4.6 mm, 5 μm) column using gradient elution at 272 nm detection wavelength. The optimized mobile phase consisted of solvent A (mixture of 0.1% v/v glacial acetic acid in water and acetonitrile in the ratio of 80:20 v/v, respectively) and solvent B (mixture of acetonitrile: tetrahydrofuran: methanol in the ratio of 50:30:20 v/v/v, respectively). The stability-indicating capability of the developed method was established by analysing forced degradation samples in which the spectral purity of BPO and ADP along with separation of all degradation products from the analyte peaks was achieved. The developed method was validated as per ICH guidelines with respect to specificity, linearity, limit of detection, limit of quantification, accuracy, precision, and robustness. Full article

13 pages, 596 KB

Open AccessArticle

Influence of Ethanol as a Co-Solvent in Cyclodextrin Inclusion Complexation: A Molecular Dynamics Study

by Kanokthip BOONYARATTANAKALIN¹, Helmut VIERNSTEIN², Peter WOLSCHANN² and Luckhana LAWTRAKUL^1,*

¹ School of Bio-Chemical Engineering and Technology, Sirindhorn International Institute of Technology, Thammasat University, Pathum Thani 12121, Thailand.

² Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Life Sciences, University of Vienna, Althanstrasse 14, 1090 Vienna, Austria.

Sci. Pharm. 2015, 83(2), 387-399; https://doi.org/10.3797/scipharm.1412-08 - 9 Feb 2015

Cited by 21 | Viewed by 2869

Abstract

Molecular dynamics (MD) simulations were used to investigate the dynamics and host-guest interactions of the inclusion complexes between a potent anti-HIV agent, UC781, and three different types of cyclodextrins (CDs) including βCD, 2,6-dimethyl-βCD (MβCD), and 2-hydroxypropyl-βCD (HPβCD) in aqueous solution with ethanol (EtOH) [...] Read more.

Molecular dynamics (MD) simulations were used to investigate the dynamics and host-guest interactions of the inclusion complexes between a potent anti-HIV agent, UC781, and three different types of cyclodextrins (CDs) including βCD, 2,6-dimethyl-βCD (MβCD), and 2-hydroxypropyl-βCD (HPβCD) in aqueous solution with ethanol (EtOH) as a co-solvent. The MD simulation results revealed that EtOH as the co-solvent and the type of cyclodextrin affected the inclusion complex formation. From this study, UC781/MβCD provided the most stable inclusion complex. The competition for the cavity of βCD between UC781 and EtOH and the ensuing occupation of βCD cavities by EtOH resulted in a weaker interaction between βCD and UC781. In HPβCD, a supramolecular complex of UC781−HPβCD−EtOH was formed. The EtOH could easily fill the residual void space of the interior of unoccupied HPβCD due to the movement of UC781. In MβCD, the strong hydrogen bond interactions between the UC781 amide group and the secondary hydroxyl groups of MβCD significantly stabilized the inclusion complex in the presence of EtOH. Full article

10 pages, 344 KB

Open AccessArticle

Development of a Forced Degradation Profile of Alosetron by Single Mode Reversed-Phase HPLC, LC-MS, and its Validation

by Yamjala KARTHIK^*, Basuvan BABU and Subramania Nainar MEYYANATHAN

Department of Pharmaceutical Analysis, JSS College of Pharmacy (A Constituent College of JSS University, Mysore), Udhagamandalam, The Nilgiris, Tamilnadu, 643001, India.

Sci. Pharm. 2015, 83(2), 311-320; https://doi.org/10.3797/scipharm.1411-07 - 29 Dec 2014

Viewed by 2139

Abstract

Determination of alosetron in the presence of its degradation products was studied and validated by a novel HPLC method. The separation of the drug and its degradation products was achieved with the Jones Chromatography C₁₈ analytical column (150 mm x 4.6 mm; [...] Read more.

Determination of alosetron in the presence of its degradation products was studied and validated by a novel HPLC method. The separation of the drug and its degradation products was achieved with the Jones Chromatography C₁₈ analytical column (150 mm x 4.6 mm; 3 μm) with a stationary phase in isocratic elution mode. The mobile phase used was 0.01 M ammonium acetate, pH-adjusted to 3.5 with glacial acetic acid and acetonitrile in the ratio of 75:25 (V/V) at a flow rate of 1 ml/min and UV detection was carried out at 217 nm. Further, the drug was subjected to stress studies for acidic, basic, neutral, oxidative, and thermal degradations as per ICH guidelines and the drug was found to be labile in base hydrolysis and oxidation, while stable in acid, neutral, thermal, and photolytic degradation conditions. An MS study has been performed on the major degradation products to predict the degradation pathway of alosetron. The method provided linear responses over the concentration range of 100–1500 ng/ml and regression analysis showed a correlation coefficient value (r²) of 0.994. The LOD and LOQ were found to be 1 ng/ml and 3 ng/ml, respectively. The developed LC method was validated as per ICH guidelines with respect to accuracy, selectivity, precision, linearity, and robustness. Full article

13 pages, 235 KB

Open AccessArticle

Forced Degradation Behaviour of Fluphenazine Hydrochloride by LC and Characterization of its Oxidative Degradation Product by LC–MS/MS

by Kashyap N. THUMMAR^*, Dilip J. GHAVA, Anvi MISTRY, Ashish VACHHANI, and Navin R. SHETH

Department of Pharmaceutical Sciences, Saurashtra University, Rajkot – 360005, Gujarat, India.

Sci. Pharm. 2015, 83(2), 297-309; https://doi.org/10.3797/scipharm.1411-04 - 22 Dec 2014

Cited by 10 | Viewed by 3666

Abstract

A novel, stability-indicating high-performance liquid chromatographic (HPLC) method is delivered for the determination of fluphenazine hydrochloride (FPZ) and its degradation products. The forced degradation testing of FPZ was carried out for hydrolytic, oxidative, photolytic, and thermal degradation. The degrada-tion appeared using a reversed-phase [...] Read more.

A novel, stability-indicating high-performance liquid chromatographic (HPLC) method is delivered for the determination of fluphenazine hydrochloride (FPZ) and its degradation products. The forced degradation testing of FPZ was carried out for hydrolytic, oxidative, photolytic, and thermal degradation. The degrada-tion appeared using a reversed-phase C18 column at ambient temperature with a mobile phase comprised of methanol : acetonitrile : (10 mM) ammonium acetate (70:15:15,v/v/v) pH 6.0, adjusted with acetic acid, having a flow rate of 1 ml min⁻¹ and a detection wavelength at 259 nm. Primarily, the maximum degradation products were formed under oxidative stress conditions. The product was distinguished through LC-MS/MS fragmentation studies. Based on the results, a more complete degradation pathway for the drug could be proposed. The modernized method was found to be precise, accurate, specific, and selective. The method was found to be suitable for the quality control of fluphenazine hydrochloride in the tablet as well as in stability-indicating studies. Full article

15 pages, 676 KB

Open AccessArticle

Screening of Panamanian Plant Extracts for Pesticidal Properties and HPLC-Based Identification of Active Compounds

by Niels GULDBRANDSEN¹, Maria DE MIERI¹, Mahabir GUPTA², Tobias SEISER³, Christine WIEBE³, Joachim DICKHAUT³, Rüdiger REINGRUBER³, Oliver SORGENFREI³ and Matthias HAMBURGER^1,*

¹ Division of Pharmaceutical Biology, Department of Pharmaceutical Sciences, University of Basel, Klingelbergstrasse 50, CH-4056 Basel, Switzerland.

² CIFLORPAN, College of Pharmacy, University of Panama, Apartado 0824-00172, Panama, Republic of Panama.

³ BASF SE, Carl-Bosch-Strasse 38, D-67056 Ludwigshafen, Germany.

Sci. Pharm. 2015, 83(2), 353-367; https://doi.org/10.3797/scipharm.1410-10 - 11 Dec 2014

Cited by 15 | Viewed by 2701

Abstract

A library of 600 taxonomically diverse Panamanian plant extracts was screened for fungicidal, insecticidal, and herbicidal activities. A total of 19 active extracts were submitted to HPLC-based activity profiling, and extracts of Bocconia frutescens, Miconia affinis, Myrcia splendens, Combretum aff. [...] Read more.

A library of 600 taxonomically diverse Panamanian plant extracts was screened for fungicidal, insecticidal, and herbicidal activities. A total of 19 active extracts were submitted to HPLC-based activity profiling, and extracts of Bocconia frutescens, Miconia affinis, Myrcia splendens, Combretum aff. laxum, and Erythroxylum macrophyllum were selected for the isolation of compounds. Chelerythrine (2), macarpine (3), dihydrosanguinarine (5), and arjunolic acid (8) showed moderate-to-good fungicidal activity. Myricetin-3-O-(6''-O-galloyl)-β-galactopyranoside (13) showed moderate insecticidal activity, but no compound with herbicidal activity was identified. Full article

18 pages, 384 KB

Open AccessArticle

Development of a Stability-Indicating Stereoselective Method for Quantification of the Enantiomer in the Drug Substance and Pharmaceutical Dosage Form of Rosuvastatin Calcium by an Enhanced Approach

by Gangireddy RAJENDRA REDDY^*, Papammagari RAVINDRA REDDY and Polisetty SIVA JYOTHI

Department of Chemistry, Sri Krishnadevaraya University, Anantapur 515001, A.P, India.

Sci. Pharm. 2015, 83(2), 279-296; https://doi.org/10.3797/scipharm.1410-09 - 5 Dec 2014

Cited by 3 | Viewed by 2185

Abstract

A novel, simple, precise, and stability-indicating stereoselective method was developed and validated for the accurate quantification of the enantiomer in the drug substance and pharmaceutical dosage forms of Rosuvastatin Calcium. The method is capable of quantifying the enantiomer in the presence of other [...] Read more.

A novel, simple, precise, and stability-indicating stereoselective method was developed and validated for the accurate quantification of the enantiomer in the drug substance and pharmaceutical dosage forms of Rosuvastatin Calcium. The method is capable of quantifying the enantiomer in the presence of other related substances. The chromatographic separation was achieved with an immobilized cellulose stationary phase (Chiralpak IB) 250 mm x 4.6 mm x 5.0 μm particle size column with a mobile phase containing a mixture of n-hexane, dichloromethane, 2-propanol, and trifluoroacetic acid in the ratio 82:10:8:0.2 (v/v/v/v). The eluted compounds were monitored at 243 nm and the run time was 18 min. Multivariate analysis and statistical tools were used to develop this highly robust method in a short span of time. The stability-indicating power of the method was established by subjecting Rosuvastatin Calcium to the stress conditions (forced degradation) of acid, base, oxidative, thermal, humidity, and photolytic degradation. Major degradation products were identified and found to be well-resolved from the enantiomer peak, proving the stability-indicating power of the method. The developed method was validated as per International Conference on Harmonization (ICH) guidelines with respect to specificity, limit of detection and limit of quantification, precision, linearity, accuracy, and robust-ness. The method exhibited consistent, high-quality recoveries (100 ± 10%) with a high precision for the enantiomer. Linear regression analysis revealed an excellent correlation between the peak responses and concentrations (r2 value of 0.9977) for the enantiomer. The method is sensitive enough to quantify the enantiomer above 0.04% and detect the enantiomer above 0.015% in Rosuvastatin Calcium. The stability tests were also performed on the drug substances as per ICH norms. Full article

9 pages, 128 KB

Open AccessArticle

An Alternative Approach to Isoganciclovir: A Prominent Impurity in the Antiviral Drug Ganciclovir

by Dhanraj T. S. S. SUNDARAM^1,2,*, Anand G. KAMAT¹, Koilpillai Joseph PRABAHAR¹, Peruri Badarinadh GUPTA¹, Battula VENKATESWARA RAO² and Sanasi PAUL DOUGLAS²

¹ Chemical Research and Development, APL Research Centre-II, Aurobindo Pharma Ltd., Survey No. 71 & 72, Indrakaran (V), Medak District-502 329, Andhra Pradesh, India.

² Department of Engineering Chemistry, Andhra University College of Engineering (A), Andhra University, Visakhapatnam-530003, Andhra Pradesh, India.

Sci. Pharm. 2015, 83(2), 233-241; https://doi.org/10.3797/scipharm.1409-15 - 11 Nov 2014

Cited by 2 | Viewed by 2032

Abstract

A simple and efficient process for the preparation of (±)-9-[(2,3-dihydroxy-propoxy)methyl]guanine (isoganciclovir) is described. The synthesis features the preparation of a kinetically and thermodynamically controlled acyclic side chain using masked glycerol and methoxymethyl acetate. The unwanted regioisomers were separated through selective crystallization, which upon [...] Read more.

A simple and efficient process for the preparation of (±)-9-[(2,3-dihydroxy-propoxy)methyl]guanine (isoganciclovir) is described. The synthesis features the preparation of a kinetically and thermodynamically controlled acyclic side chain using masked glycerol and methoxymethyl acetate. The unwanted regioisomers were separated through selective crystallization, which upon deprotection yielded isoganciclovir in good yield. The present work explains the preparation of the acyclic side chain in a simple manner without the aid of any preparative column purification or separation technique. Full article

25 pages, 1086 KB

Open AccessArticle

Molecular Docking Studies of Phytocompounds from the Phyllanthus Species as Potential Chronic Pain Modulators

by Atul R. CHOPADE^1,2,*, Fahim J. SAYYAD^1,2 and Yogesh V. PORE³

¹ Department of Pharmacology and Pharmacognosy, Government College of Pharmacy, Karad, District Satara, 415124 Maharashtra, India.

² Department of Pharmacology, Rajarambapu College of Pharmacy, Kasegaon, District-Sangli, 415404 Maharashtra, India.

³ Department of Pharmaceutical chemistry, Government College of Pharmacy, Karad, District Satara, 415124 Maharashtra, India.

Sci. Pharm. 2015, 83(2), 243-267; https://doi.org/10.3797/scipharm.1408-10 - 8 Nov 2014

Cited by 27 | Viewed by 2935

Abstract

The study of inflammatory pain has been one of the most rapidly advancing and expanding areas of pain research in recent years. Studies from our lab have demonstrated the chronic pain-modulating potential of the Phyllanthus species and their probable interaction with various inflammatory [...] Read more.

The study of inflammatory pain has been one of the most rapidly advancing and expanding areas of pain research in recent years. Studies from our lab have demonstrated the chronic pain-modulating potential of the Phyllanthus species and their probable interaction with various inflammatory mediators involving enzymes like COX-2 and PGE synthase, cytokines like TNF-alpha and IL-1 beta, and with the NMDA receptor. Inflammatory mediators which play a crucial role in chronic inflammatory hyperalgesia and its subsequent modulation were selected for their interactions with 86 structurally diverse phytoconstituents identified from the Phyllanthus species.
The docking analysis of the target proteins with the phytochemical ligands was performed using VLifeMDS software. The docking scores and analysis of the interactions of the phytocompounds with target proteins suggest that important molecules like lupeol, phyllanthin, hypopyllanthin, corilagin, epicatechin, and most of the other compounds have the ability to bind to multiple targets involved in inflammatory hyperalgesia.
Our study strongly suggests that the findings of the present study could be exploited in the future for designing ligands in order to obtain novel molecules for the treatment and management of chronic pain. Full article

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Sci. Pharm., Volume 83, Issue 2 (June 2015) – 14 articles , Pages 221-410

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