International Journal of Pharmacy and Pharmacology

International Journal of Pharmacy and Pharmacology ISSN: 2326-7267 Vol. 5 (12), pp. 001-010, December, 2016. © International Scholars Journals

Full Length Research Paper

Recent progress in the chemo-enzymatic peptide synthesis

Feifei Chen^1,2, Fangkai Zhang^1,3, Anming Wang¹*, Haifeng Li¹, Qiuyan Wang¹, Zhaowu Zeng¹, Shuling Wang¹ and Tian Xie¹

¹Research Center for Biomedicine and Health, Hangzhou Normal University, Hangzhou 310012, People’s Republic of China.

²College of Material, Chemistry and Chemical Engineering, Hangzhou Normal University, No. 222, Wenyi Road, Hangzhou 310012, People’s Republic of China.

³College of Biological and Environmental Sciences, Hangzhou Normal University, Hangzhou 310012, People’s Republic of China.

Accepted 13 August, 2016

Abstract

Peptides are molecules of paramount importance in several fields, especially in health care and nutrition. They have many beneficial health effects, such as antimicrobial, antiviral, antitumor, neuroactive and immunoactive activity. Several technologies for their production are now available such as chemical synthesis, biosynthesis and chemo-enzymatic peptide synthesis. For combining the advantages of chemical and enzymatic synthesis methods, chemo-enzymatic peptide synthesis has been attracting the interest of researchers in the peptide synthesis. In this paper, new progress in this method was reported. Enzymes, solvent systems and possible mechanisms were presented. The main strategies of chemo-enzymatic synthesis of peptides and modification of enzymes by using different methods were also discussed.

Key words: Peptides, enzymes, solvent systems, chemo-enzymatic synthesis, genetic engineering, one-pot synthesis.

International Journal of Pharmacy and Pharmacology ISSN: 2326-7267 Vol. 5 (11), pp. 001-009, November, 2016. © International Scholars Journals

Full Length Research Paper

Polyphenolic fractions of Algerian propolis reverses doxorubicin induced acute renal oxidative stress

Mesbah Lahouel^1,2*, Kheira Boutabet¹, Wided Kebsa¹ and Mohamed Alyane¹

¹Laboratory of Pharmacology and Phytochemistry, Faculty of Sciences, University of Jijel, 18000 Jijel, Algeria.

²Laboratory of Molecular Toxicology, Faculty of Sciences, University of Jijel, 18000 Jijel, Algeria.

Accepted 21 May, 2016

Abstract

The most important pharmacologically active constituents in propolis are flavanoids with a broad spectrum of biological activities varying with their chemical composition. Propolis chemical composition depends on the floral and geographical origin present at the site of collection and thus in the climatic characteristics. However, until now, no mitochondrial functions in relation to stress and apoptotic process were determined. We hypothesized that propolis effects could be due to a direct action on mitochondrial functions. We evaluated whether polyphenols compounds had preventive properties against renal oxidative stress induced by doxorubicin. We present here an analytical and pharmacological study of the eastern Algerian propolis using Thin layer Chrommatography (TLC), Ultra Violet-High Phase Liquid Chromatography (UV-HPLC) and Gas Chromatography-Mass Spectrometry (GC-MS). The pharmacological study was carried out in vivo on wistar rat pre-treated with propolis extract 100 mg/kg/day for 7 days. Doxorubicin at 10 mg/kg of body weight was administered intravenously on day 7th. Serum creatinine concentration, scavenging effect of flavonoids, lipid peroxydation (MDA) and glutathione (GSH) concentration were measured. Chemical analysis allowed identification and quantification of the phenolic compounds including pinostrombin chalcone(38.91%), galangin(18.95), naringenin(14.27%), tectochrysin(25.09%), methoxychrysin(1.14%) and a prenylated coumarin compound suberosin (1.65%). The total flavonoid concentration in the propolis extract determined by aluminum chloride colorimetric method was 370 mg (quercetin equivalents QE) /g dry weight of propolis extract (QE/g DWPE). Data suggest protective effects of an Algerian propolis extract against doxorubicin-induced oxidative stresses. It restored the renal functions and clearly reduced the toxic effect of the drug.

Key words: Algerian propolis, chemical analysis, flavonoids, renal oxidative stress.

International Journal of Pharmacy and Pharmacology ISSN: 2326-7267 Vol. 5 (11), pp. 001-004, November, 2016. © International Scholars Journals

Full Length Research Paper

Cytotoxic activity of leaf and rhizome extracts of Alpinia scabra (Blume) Náves, a wild ginger from Peninsular Malaysia

H. Ibrahim¹, K. S. Sim¹*, D. R. Syamsir¹, N. R. Mohd. Nor², A. M. Sri Nurestri¹ and K. Awang²

¹Institute of Biological Sciences, Faculty of Science, University of Malaya, 50603 Kuala Lumpur, Malaysia.

²Department of Chemistry, Faculty of Science, University of Malaya, 50603 Kuala Lumpur, Malaysia.

Accepted 19 July, 2016

Abstract

The leaves and rhizomes of Alpinia scabra (Zingiberaceae) were investigated for their cytotoxic effect against selected human cancer cell lines, namely MCF7 (hormone-dependant breast carcinoma cell line), HT29 (colon carcinoma cell line) and SKOV-3 (ovarian cancer cell line) by using an in vitro neutral red cytotoxicity assay. The methanol extracts of both leaves and rhizomes did not show active cytotoxic activity against the selected cancer cell lines. The n-hexane extract of the leaves exhibited remarkable cytotoxic effect against SKOV-3 cells with IC₅₀ value of 6.3 µg/ml while dichloromethane extract showed high cytotoxic effect against MCF7 and SKOV-3 with IC₅₀ values of 6.7 and 5.9 µg/ml, respectively. The n-hexane and dichloromethane extracts of the rhizomes possessed high cytotoxic effect against SKOV- 3 cells with IC₅₀ values of 8.3 and 7.0 µg/ml, respectively. This is the first report of the cytotoxic activity of A. scabra.

Key words: Zingiberaceae, Alpinia scabra, cytotoxic activity, cancer cell lines.

International Journal of Pharmacy and Pharmacology ISSN: 2326-7267 Vol. 5 (10), pp. 001-008, October, 2016. © International Scholars Journals

Full Length Research Paper

Microencapsulation and pharmacological evaluations for the anti-fertility effect of castor bean extract in female mice

Yi-ling Hou¹*, Xiang Ding², Shuang-quan Duan³, Zhi-rong Yang² and Ping Gao²

¹Key Laboratory of Southwest China Wildlife Resources Conservation (Ministry of Education), College of Life Science, China West Normal University. No. 44 Yuying Road, Nanchong 637002, China.

²Key Laboratory for Biological Resource and Ecological Environment of the Ministry of Education, College of Life Sciences, Sichuan University. No. 29, Wangjiang Road, Chengdu 610064, P. R. China.

³College of Sciences, Tibet University, Lhasa 850000, China

Accepted 21 May, 2016

Abstract

Castor Bean (Ricinus communis, Family Euphorbiaceae) ethanol extraction (CBE) possesses potent antifertility effect, but the absorption of it is limited. Therefore, this study was aimed to prepare CBE microparticles for targeted drug effect. Poly (toluene-2, 4-di-isocyanate and ethylene alcohol) (TDI-EA) microparticles loaded with CBE were prepared by Interracial polymerization, a semi-industrial technique capable of encapsulating fragile molecules maintaining their native properties. The effects of several parameters on the properties of the particles were investigated. Microparticles showed of CBE- TDI-EA microparticles following 200, 400 and 600 mg/kg with a content of 5 mg two mean diameters that were 4 and 120 m, separately, which are suitable for their absorption. Entrapment efficiency of CBEM in TDI-EA microparticles was 98.3%. The drug efficiency ranged from 73.26 to 100% depending on the drug consumption. The optimal growth suppression of the Kunming strain female mice vital organs could be achieved by oral application CBE in 6 mg microparticles while the Control Group showed the normal growth of the vital organs and CBE at the same concentration in solution form could not suppress the growth of the vital organs to the same extent. Finally, a bioassay demonstrated that the in vivo CBE microparticles have a strong depression of fertility without significant adverse reaction.

Key words: Antifertility, castor bean extract, female mice, microencapsulation.

International Journal of Pharmacy and Pharmacology ISSN: 2326-7267 Vol. 5 (10), pp. 001-005, October, 2016. © International Scholars Journals

Full Length Research Paper

Effects of intestinal trefoil factor on PI3K and caspase-3/9 in newborn rats with necrotizing enterocolitis

Cai-Xia Yan¹, He-Sheng Luo², Bing-Hong Zhang¹*, Ri-Hong Zhao¹ and Hai-Xia Zhang¹

¹Department of Pediatrics, Renmin Hospital of    Wuhan University, Jiefang Road 238, Wuhan 430060, PR China.

²Department of Gastroenterology, Renmin Hospital of Wuhan University, Wuhan 430060, PR China.

Accepted 12 April, 2016

Abstract

PI3K/Akt signal pathway was blocked by Wortmannin, a specific inhibitor of phosphoinositide-3 kinase (PI3K), and the effects of intestinal trefoil factor (ITF) on PI3K and caspase-3/9 in newborn rats with necrotizing enterocolitis (NEC) were investigated to explore the protective mechanism of ITF against NEC. Experimental NEC was induced by exposure to hypoxia for 60 sec followed by cold stress at 4°C for 10 min. A total of 50 One-day-old Wistar rats were randomly divided into five groups : group A, NEC+NS; group B, NEC+ITF; group C,NEC+ wortmannin; group D ,NEC+ wortmannin + ITF; group E , Normal control. The animals were euthanized at development of NEC, and at 96 h the intestinal tissue was harvested and examined for histological changes of NEC, and then the PI3K content and Caspase-3/9 activity were detected using ELISA and spectrophotometry, respectively. The PI3K content (pg/ml) in group A was slightly higher than group E (P<0.05), and there was no significant difference between group A and D (P>0.05), but the PI3K content (pg/ml) in group B was significantly higher than the remaining groups (P<0.01), and the PI3K content (pg/ml) in group C was significantly lower compared with group E (P<0.01). Compared with group B and E, Caspase- 3/9 activity was significantly higher in group A than in group B and E (P<0.01), but all lower than that in group C. So we concluded that ITF could activate the PI3K/Akt pathway to down-regulate Caspase-3/9 activity, and to protect against intestinal damage of NEC rats.

Key words: Intestinal trefoil factor, necrotizing enterocolitis, PI3K/Akt signal transduction, Caspase-9, Caspase-3.

International Journal of Pharmacy and Pharmacology ISSN: 2326-7267 Vol. 5 (9), pp. 001-017, September, 2016. © International Scholars Journals

Full Length Research Paper

In vitro and in vivo evaluation of two sustained release formulations of diltiazem HCl

Muhammad Rafiq¹, Abdul Wahab²*, Nisar-ur-Rehman¹, Abid Hussain² and Said Muhammad¹

¹Department of Pharmacy, Islamia University, Bahawalpur, Pakistan.

²Faculty of Pharmacy, Gomal University, D.I.Khan, N.W.F.P, Pakistan.

Accepted 19 July, 2016

Abstract

In the present study, two sustained release solid and semi-solid matrices were developed using Hydroxypropyl methyl cellulose (HPMC) and Gelucire derivative, Gelucire 50/30. The purpose of the study was in vitro and in vivo correlation of these two sustained release formulations with SR capsules available in market and to know that for how long the preparation containing HPMC and Gelucire work in the body as compared to the product circulating in the market, so for this two formulations were developed such as solid matrices in tablets form and semi-solid capsules. For the preparation of solid matrices, direct compression method and for semi-solid, filling capsule technology were used. In vitro and in vivo study was perfomed and different parameters were studied such as Cmax, Tmax and AUC for all the three formulations. For determination of Cmax, Tmax ans AUC statistical models were used. In vitro study showed that more than 80% drug was released upto 12 h from all the three formulations and no significance difference was observed in release pattern while in vivo study showed prolonged release of the two test formulations after applying statistical models. The drug release from both test formulations was slow thereby providing a prolonged and controlled in vivo delivery of the drug. This proved the superiority of our test capsules and tablets over the reference capsules.

Key words: In vitro and in vivo correlation, deltiazem, kinetic models, statistical analysis.