M. Cam, S. Yildiz, B. Ertaş, A. Acar, T. Taşkın, L. Kabasakal
Some Salvia and Thymus species of Lamiaceae family come into prominence with strong antidiabetic effects. Compared to the other species, there are limited studies on antidiabetic activity of Salvia triloba (ST) and Thymus praecox subsp. skorpilii var. skorpilii (TPS). The aim of this study was to adjust the dosage and to determine the antidiabetic effects of methanol extracts of ST and TPS in streptozotocin/nicotinamide-induced diabetic rats. Type II diabetes mellitus (T2DM) was induced by a single intraperitoneal (i.p.) injection of streptozotocin (STZ) dissolved in 0.1 M cold citrate buffer (pH 4.5) at a dose of 55 mg/kg/body weight (b.w.) and nicotinamide (100 mg/kg/b.w.) was given prior to STZ injection. For adjusting dosage, oral glucose tolerance test (OGTT) was used while insulin tolerance test (ITT), OGTT, blood glucose levels and animal weights were used to evaluate the antidiabetic effects of ST and TPS. According to the OGTT, the most effective doses for ST and TPS were 200 mg/kg and 100 mg/kg, respectively. At the end of three weeks, blood glucose levels of control goup reached to 462.50 mg/dl, whereas ST and TPS-treated groups blood glucose levels decreased less than 200.00 mg/dl. In conclusion, the present study suggests that both of ST and TPS methanolic extracts may be of therapeutic benefit in diabetes and thus need to further studies.
{"title":"Antidiabetic effects of Salvia triloba and Thymus praecox subsp. skorpilii var. skorpilii in a rat model of streptozotocin/nicotinamide-induced diabetes","authors":"M. Cam, S. Yildiz, B. Ertaş, A. Acar, T. Taşkın, L. Kabasakal","doi":"10.12991/MPJ.2017.8","DOIUrl":"https://doi.org/10.12991/MPJ.2017.8","url":null,"abstract":"Some Salvia and Thymus species of Lamiaceae family come into prominence with strong antidiabetic effects. Compared to the other species, there are limited studies on antidiabetic activity of Salvia triloba (ST) and Thymus praecox subsp. skorpilii var. skorpilii (TPS). The aim of this study was to adjust the dosage and to determine the antidiabetic effects of methanol extracts of ST and TPS in streptozotocin/nicotinamide-induced diabetic rats. Type II diabetes mellitus (T2DM) was induced by a single intraperitoneal (i.p.) injection of streptozotocin (STZ) dissolved in 0.1 M cold citrate buffer (pH 4.5) at a dose of 55 mg/kg/body weight (b.w.) and nicotinamide (100 mg/kg/b.w.) was given prior to STZ injection. For adjusting dosage, oral glucose tolerance test (OGTT) was used while insulin tolerance test (ITT), OGTT, blood glucose levels and animal weights were used to evaluate the antidiabetic effects of ST and TPS. According to the OGTT, the most effective doses for ST and TPS were 200 mg/kg and 100 mg/kg, respectively. At the end of three weeks, blood glucose levels of control goup reached to 462.50 mg/dl, whereas ST and TPS-treated groups blood glucose levels decreased less than 200.00 mg/dl. In conclusion, the present study suggests that both of ST and TPS methanolic extracts may be of therapeutic benefit in diabetes and thus need to further studies.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"8 1","pages":"818-827"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82136606","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
L. Yurttaş, Kaan Küçükoğlu, H. Nadaroğlu, Z. Kaplancıklı
Coronary artery disease and low-density lipoprotein (LDL) levels in the blood have long been known to be associated with peripheral vascular diseases. Paraoxonase-1 (PON1) enzyme is related to serum levels of high-density lipoprotein (HDL) and protects LDL from oxidation which may result in development of microvascular disease in diabetes. The enzyme has a major role in the prevention of atherosclerosis besides antioxidant properties. Additionally, PON1 is important in the detoxification of organophosphate insecticides from the body. In this study, we aimed to synthesize highly active new compounds which can be a drug candidate and evaluate their effects on PON1 activity. Nine novel triazole compounds bearing thioacetamide moiety (5a-i) were synthesized and their in vitro PON1 activity was investigated. The PON1 enzyme was purified from human serum using ammonium sulfate precipitation method. Also, it was further purified using Sepharose 4B-L-tyrosine- 1-naphthylamine affinity chromatography. Among the synthesized triazole compounds, 5b, 5c, 5f and 5h have been determined to increase PON1 activity, remarkably. Compounds 5b, 5c, 5f and 5h bearing 5-nitrothiazole, benzothiazole, 6-ethoxybenzothiazole and 6-florobenzothiazole moieties could be considered to proceed in vivo investigations which is a further stage for a drug candidate.
冠状动脉疾病和血液中的低密度脂蛋白(LDL)水平长期以来被认为与周围血管疾病有关。对氧磷酶-1 (PON1)酶与血清高密度脂蛋白(HDL)水平有关，并保护LDL免受氧化，从而导致糖尿病微血管疾病的发生。除了抗氧化外，这种酶在预防动脉粥样硬化方面也起着重要作用。此外，PON1在人体对有机磷杀虫剂的解毒中也很重要。在本研究中，我们旨在合成高活性的候选药物，并评估其对PON1活性的影响。合成了9个新型含硫乙酰胺(5a-i)的三唑类化合物，并对其体外PON1活性进行了研究。用硫酸铵沉淀法从人血清中纯化PON1酶。并用Sepharose 4b - l -酪氨酸- 1-萘胺亲和层析进一步纯化。在合成的三唑类化合物中，5b、5c、5f和5h均能显著提高PON1活性。含有5-硝基噻唑、苯并噻唑、6-乙氧基苯并噻唑和6-氟苯并噻唑的化合物5b、5c、5f和5h可以考虑进行体内研究，这是候选药物的进一步研究阶段。
{"title":"Synthesis and evaluation of novel 2-[(1,2,4-triazol-3-yl)thio]acetamide derivatives as potential serum paraoxonase-1 (PON1) activators","authors":"L. Yurttaş, Kaan Küçükoğlu, H. Nadaroğlu, Z. Kaplancıklı","doi":"10.12991/MPJ.2017.19","DOIUrl":"https://doi.org/10.12991/MPJ.2017.19","url":null,"abstract":"Coronary artery disease and low-density lipoprotein (LDL) levels in the blood have long been known to be associated with peripheral vascular diseases. Paraoxonase-1 (PON1) enzyme is related to serum levels of high-density lipoprotein (HDL) and protects LDL from oxidation which may result in development of microvascular disease in diabetes. The enzyme has a major role in the prevention of atherosclerosis besides antioxidant properties. Additionally, PON1 is important in the detoxification of organophosphate insecticides from the body. In this study, we aimed to synthesize highly active new compounds which can be a drug candidate and evaluate their effects on PON1 activity. Nine novel triazole compounds bearing thioacetamide moiety (5a-i) were synthesized and their in vitro PON1 activity was investigated. The PON1 enzyme was purified from human serum using ammonium sulfate precipitation method. Also, it was further purified using Sepharose 4B-L-tyrosine- 1-naphthylamine affinity chromatography. Among the synthesized triazole compounds, 5b, 5c, 5f and 5h have been determined to increase PON1 activity, remarkably. Compounds 5b, 5c, 5f and 5h bearing 5-nitrothiazole, benzothiazole, 6-ethoxybenzothiazole and 6-florobenzothiazole moieties could be considered to proceed in vivo investigations which is a further stage for a drug candidate.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"77 1","pages":"967-977"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77816315","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
K. Mali, S. Dhawale, R. Dias, V. Havaldar, Pankaj R Kavitake
The aim of present investigation was to characterize carboxymethyl tamarind gum (CMTG) based interpenetrating networks (IPNs) of aceclofenac for site specific sustained delivery. The drug loaded IPNs were prepared by using chitosan and CMTG as polymers and gluteraldehyde as crosslinking agent. The IPNs were characterized by Attenuated total reflectance- Fourier transform infrared (ATR-FTIR) spectroscopy, thermal analysis, X-ray powder diffraction and solid state 13C-nuclear magnetic resonance spectroscopy. The prepared IPNs were evaluated for the drug entrapment efficiency and equilibrium swelling. The drug release from IPNs was studied in 0.1NHCl for 2h followed by phosphate buffer pH 6.8 for further 10h and compared with commercial tablet. The results of ATR-FTIR and thermal analysis for blank IPNs indicated intercalation of polymeric chains of crosslinked CMTG and chitosan. The results of solid state characterization revealed that the aceclofenac is compatible with IPNs. Entrapment efficiency of IPNs was found to be increased with increase in crosslinker concentration as well as amount of CMTG. The equilibrium swelling study indicated pH dependent swelling of IPNs. The drug release by IPNs showed sustained release of aceclofenac upto 12h while commercial formulation showed fast release within 8h. From the results, it can be concluded that the IPNs of CMTG and chitosan has potential in development of site specific sustained drug delivery.
{"title":"Interpenetrating networks of carboxymethyl tamarind gum and chitosan for sustained delivery of aceclofenac","authors":"K. Mali, S. Dhawale, R. Dias, V. Havaldar, Pankaj R Kavitake","doi":"10.12991/MPJ.2017.20","DOIUrl":"https://doi.org/10.12991/MPJ.2017.20","url":null,"abstract":"The aim of present investigation was to characterize carboxymethyl tamarind gum (CMTG) based interpenetrating networks (IPNs) of aceclofenac for site specific sustained delivery. The drug loaded IPNs were prepared by using chitosan and CMTG as polymers and gluteraldehyde as crosslinking agent. The IPNs were characterized by Attenuated total reflectance- Fourier transform infrared (ATR-FTIR) spectroscopy, thermal analysis, X-ray powder diffraction and solid state 13C-nuclear magnetic resonance spectroscopy. The prepared IPNs were evaluated for the drug entrapment efficiency and equilibrium swelling. The drug release from IPNs was studied in 0.1NHCl for 2h followed by phosphate buffer pH 6.8 for further 10h and compared with commercial tablet. The results of ATR-FTIR and thermal analysis for blank IPNs indicated intercalation of polymeric chains of crosslinked CMTG and chitosan. The results of solid state characterization revealed that the aceclofenac is compatible with IPNs. Entrapment efficiency of IPNs was found to be increased with increase in crosslinker concentration as well as amount of CMTG. The equilibrium swelling study indicated pH dependent swelling of IPNs. The drug release by IPNs showed sustained release of aceclofenac upto 12h while commercial formulation showed fast release within 8h. From the results, it can be concluded that the IPNs of CMTG and chitosan has potential in development of site specific sustained drug delivery.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"55 5 1","pages":"771-782"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83553145","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Hekimin hastayla karsilasmadan once hazirlik yaparak, ilgili endikasyona yonelik kendi kisisel ilac listesini olusturmasi ve bu dogrultuda hastalarinin ilacla tedavisini duzenlemesi beklenir. Hekimin bu yaklasimi benimsemesi, akilci ilac kullaniminin (AIK) gerekliliklerinden birisidir. Analjezikler, dis hekimlerinin (DH) en sik receteledigi ilac gruplari arasinda yer alir. Bu yazida, “DH’lerin AIK ilkelerine uygun ilac secimini nasil yapmasi gerektigi” uzerinde durulmaktadir. Bu islemin daha kolay anlasilmasi icin dis hekimliginde “kisisel analjezik listesi” (KAL) secimi ozelinde konunun ayrintilarina yer verilmistir. KAL secimi, analjeziklere ait klinik farmakoloji bilgisinden yararlanarak “etkililik, guvenlilik, uygunluk ve maliyet”ten olusan 4 secim olcutu kullanilarak yapilir. Bu sayede alternatifleri arasindan en iyiler belirlenir. Boylece DH’nin receteleyecegi ilaclara ait bilmesi gereken bilgi yuku ciddi olcude hafifler. Piyasada mevcut cok sayidaki analjezigi ilgilendiren bilgi yukunden kurtulur. Sadece KAL’daki sinirli sayidaki ilaca ait bilgileri iyice ogrenmesi kolaylasir. Bu yontem sayesinde az sayidaki ilaci iyi bilen bir DH, pratikte hem receteye yazacagi ilaci isabetle ve kolaylikla belirler, hem de bu ilacla ilgili hastasina verecegi bilgileri daha kolay aklinda tutar ve bunu daha rahat hayata gecirir. Dolayisiyla, KAL siralamasina sahip olan bir DH, analjezik tedavisini basarili bir seklide duzenleme imkânina kavusur. Analjezik ozelinde kazanilacak bu akilci yaklasimin “transfer etkisi” yoluyla antibiyotik secimi basta olmak uzere dis hekimliginde ihtiyac hissedilen diger ilac/ urun gruplarinin seciminde de benimsenmesi beklenir.
{"title":"Akılcı ilaç kullanımı ilkeleri doğrultusunda diş hekimliğinde kişisel analjezik listesi oluşturulması","authors":"Ahmet Akıcı, İpek Kirmizi, Gökhan Göçmen","doi":"10.12991/mpj.2017.1","DOIUrl":"https://doi.org/10.12991/mpj.2017.1","url":null,"abstract":"Hekimin hastayla karsilasmadan once hazirlik yaparak, ilgili endikasyona yonelik kendi kisisel ilac listesini olusturmasi ve bu dogrultuda hastalarinin ilacla tedavisini duzenlemesi beklenir. Hekimin bu yaklasimi benimsemesi, akilci ilac kullaniminin (AIK) gerekliliklerinden birisidir. Analjezikler, dis hekimlerinin (DH) en sik receteledigi ilac gruplari arasinda yer alir. Bu yazida, “DH’lerin AIK ilkelerine uygun ilac secimini nasil yapmasi gerektigi” uzerinde durulmaktadir. Bu islemin daha kolay anlasilmasi icin dis hekimliginde “kisisel analjezik listesi” (KAL) secimi ozelinde konunun ayrintilarina yer verilmistir. KAL secimi, analjeziklere ait klinik farmakoloji bilgisinden yararlanarak “etkililik, guvenlilik, uygunluk ve maliyet”ten olusan 4 secim olcutu kullanilarak yapilir. Bu sayede alternatifleri arasindan en iyiler belirlenir. Boylece DH’nin receteleyecegi ilaclara ait bilmesi gereken bilgi yuku ciddi olcude hafifler. Piyasada mevcut cok sayidaki analjezigi ilgilendiren bilgi yukunden kurtulur. Sadece KAL’daki sinirli sayidaki ilaca ait bilgileri iyice ogrenmesi kolaylasir. Bu yontem sayesinde az sayidaki ilaci iyi bilen bir DH, pratikte hem receteye yazacagi ilaci isabetle ve kolaylikla belirler, hem de bu ilacla ilgili hastasina verecegi bilgileri daha kolay aklinda tutar ve bunu daha rahat hayata gecirir. Dolayisiyla, KAL siralamasina sahip olan bir DH, analjezik tedavisini basarili bir seklide duzenleme imkânina kavusur. Analjezik ozelinde kazanilacak bu akilci yaklasimin “transfer etkisi” yoluyla antibiyotik secimi basta olmak uzere dis hekimliginde ihtiyac hissedilen diger ilac/ urun gruplarinin seciminde de benimsenmesi beklenir.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"293 1","pages":"730-740"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79521902","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The estimation of individual plasma protein in free and bound form with analytes has importance in pharmacokinetics study. Albumins and globulins are most abundantly found in plasma and plays crucial role in plasma protein binding. The present communication deals with the development of gel permeation chromatographic method for the estimation of plasma protein binding studies for ketoprofen, tapentadol and furaltadone. The method was developed using WATER system with Ultrahydrogel column (7.8 x 300 mm i.d.), refractive index detector (1.00 to 1.75 RIU) and Rheodyne injection valve fitted with a 20μl sample loop using 0.1% sodium nitrate as a mobile phase. The method was developed by studying binding above drugs with most of plasma proteins. These complexes have shown linearity in range of 100 to 300μg/ml of these drugs. The developed method has been validated using USFDA guidelines. The developed bioanalytical method is accurate, precise, and selective and sensitive for quantification of plasma proteins bound drugs. The further optimization of method using other standard plasma proteins will explore its applicability in pharmacokinetic and biopharmaceutical studies of most of drugs.
血浆游离蛋白和结合蛋白在药代动力学研究中具有重要意义。白蛋白和球蛋白在血浆中含量最多，在血浆蛋白结合中起着至关重要的作用。本文介绍了凝胶渗透色谱法在酮洛芬、他他多和呋喃他酮血浆蛋白结合研究中的应用。该方法采用WATER系统，采用超水凝胶色谱柱(7.8 × 300 mm i.d)，折射率检测器(1.00 ~ 1.75 RIU)和Rheodyne进样阀，样品环为20μl，流动相为0.1%硝酸钠。该方法是通过研究上述药物与大多数血浆蛋白的结合而发展起来的。这些配合物在100 ~ 300μg/ml范围内呈线性关系。所开发的方法已通过USFDA指南的验证。该方法对血浆蛋白结合药物的定量具有准确、精确、选择性和敏感性。使用其他标准血浆蛋白进一步优化方法，将探索其在大多数药物的药代动力学和生物制药研究中的适用性。
{"title":"Gel permeation chromatographic method for drug protein binding studies","authors":"M. Bhatia, S. Jadhav, Santosh S. Kumbhar","doi":"10.12991/MPJ.2017.17","DOIUrl":"https://doi.org/10.12991/MPJ.2017.17","url":null,"abstract":"The estimation of individual plasma protein in free and bound form with analytes has importance in pharmacokinetics study. Albumins and globulins are most abundantly found in plasma and plays crucial role in plasma protein binding. The present communication deals with the development of gel permeation chromatographic method for the estimation of plasma protein binding studies for ketoprofen, tapentadol and furaltadone. The method was developed using WATER system with Ultrahydrogel column (7.8 x 300 mm i.d.), refractive index detector (1.00 to 1.75 RIU) and Rheodyne injection valve fitted with a 20μl sample loop using 0.1% sodium nitrate as a mobile phase. The method was developed by studying binding above drugs with most of plasma proteins. These complexes have shown linearity in range of 100 to 300μg/ml of these drugs. The developed method has been validated using USFDA guidelines. The developed bioanalytical method is accurate, precise, and selective and sensitive for quantification of plasma proteins bound drugs. The further optimization of method using other standard plasma proteins will explore its applicability in pharmacokinetic and biopharmaceutical studies of most of drugs.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"50 1","pages":"938-948"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80122252","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
F. Kheirandish, H. Mahmoudvand, A. Khamesipour, F. Ebrahimzadeh, F. Behrahi, S. Rezaei, B. Delfan
At present, no effective vaccine has been found for CL; thus, the upgrading and improvement of the present drugs and development of the novel agents have been demonstrated to be the merely control choice for this disease. The present study aims to evaluate the effects of olive leaf extract (Olea europaea L. OLE) on Leishmania major infection in BALB/c mice. OLE tested on cutaneous leishmaniasis (CL) in male BALB/c mice with L. major promastigotes (MRHO/IR/75/ER) at the doses of 10, 20, and 30 mg/kg. Results demonstrated that after treatment of the groups with the concentrations of 10, 20, and 40 mg/ kg of OLE, mean diameter of lesions was reduced by 2.16, 5.87, and 7.61 cm, respectively. Moreover, after 4 weeks of treatment, 83.3%, 66.64%, and 33.32% recovery was observed in the infected mice treated with 40, 20, and 10 mg/kg of OLE, respectively. In conclusion, the present study showed OLE has potent therapeutic effects on cutaneous leishmaniasis.
{"title":"The therapeutic effects of olive leaf extract on Leishmania major infection in BALB/c mice","authors":"F. Kheirandish, H. Mahmoudvand, A. Khamesipour, F. Ebrahimzadeh, F. Behrahi, S. Rezaei, B. Delfan","doi":"10.12991/MPJ.2017.6","DOIUrl":"https://doi.org/10.12991/MPJ.2017.6","url":null,"abstract":"At present, no effective vaccine has been found for CL; thus, the upgrading and improvement of the present drugs and development of the novel agents have been demonstrated to be the merely control choice for this disease. The present study aims to evaluate the effects of olive leaf extract (Olea europaea L. OLE) on Leishmania major infection in BALB/c mice. OLE tested on cutaneous leishmaniasis (CL) in male BALB/c mice with L. major promastigotes (MRHO/IR/75/ER) at the doses of 10, 20, and 30 mg/kg. Results demonstrated that after treatment of the groups with the concentrations of 10, 20, and 40 mg/ kg of OLE, mean diameter of lesions was reduced by 2.16, 5.87, and 7.61 cm, respectively. Moreover, after 4 weeks of treatment, 83.3%, 66.64%, and 33.32% recovery was observed in the infected mice treated with 40, 20, and 10 mg/kg of OLE, respectively. In conclusion, the present study showed OLE has potent therapeutic effects on cutaneous leishmaniasis.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"19 1","pages":"837-842"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80140360","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Five Vincetoxicum taxa (V. canescens subsp. canescens, V. canescens subsp. pedunculata, V. fuscatum subsp. fuscatum, V. fuscatum subsp. boissieri and V. parviflorum) were investigated for insect antifeedant activity against Spodoptera littoralis and Leptinotarsa decemlineata. At a dose of 500 μg/cm2, 12 extracts were 100 % feeding deterrent, while 6 extracts showed 86.3- 99.3 % antifeedant activity. The effective doses (ED50) of the total ethanol extract from V. canescens subsp. pedunculata and of the methanol: dichloromethane (1:1) extract from V. parviflorum were 12, and 18 μg/cm2, respectively, against S. littoralis, and that of the total ethanol extract from V. fuscatum subsp. fuscatum was 25 μg/cm2 against L. decemlineata. The dichloromethane extracts of V. parviflorum and V. canescens subsp. pedunculata inhibited the growth of S. littoralis with ED50 values of 0.08 and 0.09 mg/g, respectively, and their LD50 values for larval mortality were 1.07 and 1.03 mg/g, respectively. Phytochemical analysis revealed the presence of cardiotonic glycosides, sugars, flavonoids and alkaloids in all investigated taxa. In the dichloromethane and methanol:dichloromethane (1:1) extracts, phenanthroindolizidine alkaloids were detected by LC/MS/MS.
{"title":"Phytochemical composition and antifeedant activity of five Vincetoxicum taxa against Spodoptera littoralis and Leptinotarsa decemlineata","authors":"S. Güzel, R. Pavela, A. Ilcim, G. Kökdil","doi":"10.12991/MPJ.2017.28","DOIUrl":"https://doi.org/10.12991/MPJ.2017.28","url":null,"abstract":"Five Vincetoxicum taxa (V. canescens subsp. canescens, V. canescens subsp. pedunculata, V. fuscatum subsp. fuscatum, V. fuscatum subsp. boissieri and V. parviflorum) were investigated for insect antifeedant activity against Spodoptera littoralis and Leptinotarsa decemlineata. At a dose of 500 μg/cm2, 12 extracts were 100 % feeding deterrent, while 6 extracts showed 86.3- 99.3 % antifeedant activity. The effective doses (ED50) of the total ethanol extract from V. canescens subsp. pedunculata and of the methanol: dichloromethane (1:1) extract from V. parviflorum were 12, and 18 μg/cm2, respectively, against S. littoralis, and that of the total ethanol extract from V. fuscatum subsp. fuscatum was 25 μg/cm2 against L. decemlineata. The dichloromethane extracts of V. parviflorum and V. canescens subsp. pedunculata inhibited the growth of S. littoralis with ED50 values of 0.08 and 0.09 mg/g, respectively, and their LD50 values for larval mortality were 1.07 and 1.03 mg/g, respectively. Phytochemical analysis revealed the presence of cardiotonic glycosides, sugars, flavonoids and alkaloids in all investigated taxa. In the dichloromethane and methanol:dichloromethane (1:1) extracts, phenanthroindolizidine alkaloids were detected by LC/MS/MS.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"145 1","pages":"872-880"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73439355","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Gulcin Arslan Azizoglu, E. Azizoğlu, S. T. Tanrıverdi, Ö. Özer
A simple, fast and precise reverse phase high performance liquid chromatographic method has been developed for the simultaneous determination of Melatonin and Octyl Methoxycinnamate. Melatonin has become an attractive substrate in sunscreen formulations because of its high antioxidant and photo-protection properties. Octyl methoxycinnamate is one of the chemical UV filter that can be found most of the sunscreen formulations up to 7.5 % according Food and Drug Administration. The aim of the present study was to develop and validate a High-Performance Liquid Chromatography method for the determination of Melatonin and Octyl Methoxycinnamate in combined pharmaceutical or cosmetic applications. As a model of combined pharmaceutical applications, a microemulsion consisting of Melatonin and Octyl Methoxycinnamate was also prepared and characterized in terms of droplet size, pH and viscosity. The separation was performed with a Waters XTerra RP C18 (5 μm, 4.6 x 150 mm). All HPLC assays were performed with 10 μl injection volume, mobile phase consisting of acetonitrile and water, using gradient elution starting at 20% and ending at 90% of acetonitrile with a flow rate of 1.5 ml min-1.The eluent was monitored with UV detection at 222 nm for Melatonin and 306 nm for Octyl Methoxycinnamate. The method was validated according to ICH guidelines. Validation parameters were specificity, accuracy, precision (repeatability and reproducibility), linearity, limit of detection (LOD) and limit of quantification (LOQ). Analytical method development results indicated that the LOD values were 0.132 and 0.049 μg/ml; LOQ values were 0.4 and 0.15 μg/ml and assay exhibited a linear range of 0.5- 60 μg/ml for Melatonin and Octyl Methoxycinnamate, respectively.
建立了一种简便、快速、精确的反相高效液相色谱法同时测定褪黑素和甲氧基肉桂酸辛酯。褪黑素因其高抗氧化和光防护性能而成为防晒霜配方中有吸引力的基质。甲氧基肉桂酸辛酯是一种化学紫外线过滤器，根据美国食品和药物管理局的数据，大多数防晒霜配方中含有高达7.5%的紫外线。本研究的目的是建立并验证一种高效液相色谱法测定褪黑素和甲氧基肉桂酸辛酯在联合制药或化妆品应用中的含量。作为联合制药应用的模型，褪黑素和甲氧基肉桂酸辛酯组成的微乳液也被制备出来，并在液滴大小、pH和粘度方面进行了表征。采用Waters XTerra RP C18 (5 μm, 4.6 x 150 mm)进行分离。所有HPLC测定均以10 μl进样量，流动相为乙腈和水，梯度洗脱，从乙腈的20%开始，到90%结束，流速为1.5 ml min-1。对洗脱液进行紫外检测，褪黑素波长222 nm，甲氧基肉桂酸辛酯波长306 nm。根据ICH指南对方法进行了验证。验证参数为特异性、准确性、精密度(重复性和再现性)、线性度、检出限(LOD)和定量限(LOQ)。分析方法开发结果表明，检出限分别为0.132和0.049 μg/ml;褪黑素和甲氧基肉桂酸辛酯的定量限分别为0.4和0.15 μg/ml，线性范围为0.5 ~ 60 μg/ml。
{"title":"A validated HPLC method for simultaneous estimation of Melatonin and Octyl Methoxycinnamate in combined pharmaceutical applications","authors":"Gulcin Arslan Azizoglu, E. Azizoğlu, S. T. Tanrıverdi, Ö. Özer","doi":"10.12991/MPJ.2017.16","DOIUrl":"https://doi.org/10.12991/MPJ.2017.16","url":null,"abstract":"A simple, fast and precise reverse phase high performance liquid chromatographic method has been developed for the simultaneous determination of Melatonin and Octyl Methoxycinnamate. Melatonin has become an attractive substrate in sunscreen formulations because of its high antioxidant and photo-protection properties. Octyl methoxycinnamate is one of the chemical UV filter that can be found most of the sunscreen formulations up to 7.5 % according Food and Drug Administration. The aim of the present study was to develop and validate a High-Performance Liquid Chromatography method for the determination of Melatonin and Octyl Methoxycinnamate in combined pharmaceutical or cosmetic applications. As a model of combined pharmaceutical applications, a microemulsion consisting of Melatonin and Octyl Methoxycinnamate was also prepared and characterized in terms of droplet size, pH and viscosity. The separation was performed with a Waters XTerra RP C18 (5 μm, 4.6 x 150 mm). All HPLC assays were performed with 10 μl injection volume, mobile phase consisting of acetonitrile and water, using gradient elution starting at 20% and ending at 90% of acetonitrile with a flow rate of 1.5 ml min-1.The eluent was monitored with UV detection at 222 nm for Melatonin and 306 nm for Octyl Methoxycinnamate. The method was validated according to ICH guidelines. Validation parameters were specificity, accuracy, precision (repeatability and reproducibility), linearity, limit of detection (LOD) and limit of quantification (LOQ). Analytical method development results indicated that the LOD values were 0.132 and 0.049 μg/ml; LOQ values were 0.4 and 0.15 μg/ml and assay exhibited a linear range of 0.5- 60 μg/ml for Melatonin and Octyl Methoxycinnamate, respectively.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"14 1","pages":"921-930"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77020887","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The purpose of present study was to investigate the analgesic and anti-inflammatory activity of Lantana camara (Verbenaceae) leaf and bark extract. The methanol extract of Lantana camara (MELC) was screened for possible analgesic activity by acetic acid, hot plate and anti-inflammatory activity by carrageenan and histamine induced paw edema. The result showed that, MELC (100 mg/kg and 200 mg/kg) leaf and bark possessed significant (P <0.01 and P <0.05) anti-inflammatory response and 200 mg/kg dose of MELC leaf and bark showed more significant (P <0.01) analgesic activity as compared to the 100 mg/kg dose. Preliminary phytochemical screening result shows the presence of several phytochemicals which may responsible for its anti-inflammatory and analgesic actions. The results indicate the MELC showed great potential for analgesic and anti-inflammatory activity and may be useful for the medical purpose.
{"title":"Analgesic and anti-inflammatory activity of crude leaf and bark extract of Lantana Camara","authors":"Shripad Bairagi, I. Pathan, N. Nema","doi":"10.12991/MPJ.2017.7","DOIUrl":"https://doi.org/10.12991/MPJ.2017.7","url":null,"abstract":"The purpose of present study was to investigate the analgesic and anti-inflammatory activity of Lantana camara (Verbenaceae) leaf and bark extract. The methanol extract of Lantana camara (MELC) was screened for possible analgesic activity by acetic acid, hot plate and anti-inflammatory activity by carrageenan and histamine induced paw edema. The result showed that, MELC (100 mg/kg and 200 mg/kg) leaf and bark possessed significant (P <0.01 and P <0.05) anti-inflammatory response and 200 mg/kg dose of MELC leaf and bark showed more significant (P <0.01) analgesic activity as compared to the 100 mg/kg dose. Preliminary phytochemical screening result shows the presence of several phytochemicals which may responsible for its anti-inflammatory and analgesic actions. The results indicate the MELC showed great potential for analgesic and anti-inflammatory activity and may be useful for the medical purpose.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"18 1","pages":"810-817"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76576529","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
M. Han, Güler Gürol, T. Yildirim, S. Kalayci, F. Şahin, Ş. Küçükgüzel
A novel series of new eleven benzocaine hydrazide derivatives, N-(4-{[2-(nonsubstituted/ substitutedfuryl/ phenyl/ pyridinyl/ thienyl/ pyrrole)methylidene]hydrazinyl] carbonyl}phenyl) benzamides [3a-k] have been synthesized in this study. The structures of the new compounds were determined by spectral (FT-IR and 1H-NMR) methods and their purity was proven by elemental analysis and thin layer chromatography. These compounds were evaluated for in vitro antibacterial activity by using micro-well dilution method against Escherichia coli ATCC 10536, Escherichia coli ATCC 15442, Staphylococcus aureus ATCC 6538, Pseudomonas aeruginosa ATCC 15442, Acinetobacter baumannii , Klebsiella pneumonia ATCC 13883.
{"title":"Synthesis and antibacterial activity of hnew hydrazide-hydrazones derived from Benzocaine","authors":"M. Han, Güler Gürol, T. Yildirim, S. Kalayci, F. Şahin, Ş. Küçükgüzel","doi":"10.12991/MPJ.2017.34","DOIUrl":"https://doi.org/10.12991/MPJ.2017.34","url":null,"abstract":"A novel series of new eleven benzocaine hydrazide derivatives, N-(4-{[2-(nonsubstituted/ substitutedfuryl/ phenyl/ pyridinyl/ thienyl/ pyrrole)methylidene]hydrazinyl] carbonyl}phenyl) benzamides [3a-k] have been synthesized in this study. The structures of the new compounds were determined by spectral (FT-IR and 1H-NMR) methods and their purity was proven by elemental analysis and thin layer chromatography. These compounds were evaluated for in vitro antibacterial activity by using micro-well dilution method against Escherichia coli ATCC 10536, Escherichia coli ATCC 15442, Staphylococcus aureus ATCC 6538, Pseudomonas aeruginosa ATCC 15442, Acinetobacter baumannii , Klebsiella pneumonia ATCC 13883.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"67 1","pages":"961-966"},"PeriodicalIF":0.0,"publicationDate":"2017-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76310736","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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