Pharmaceutical Sciences
Volume:20 Issue: 3, Dec 2014

The main drawbacks of 3-step tedious and cumbersome downstream processing of biomolecules includes complex procedural steps, production of excessive amount of by-products, huge amount of energy consumption and inefficient with respect to purity, yield and selectivity. In order to overcome the limitations of downstream processing, aqueous two-phase systems (ATPS) have been applied as alternative, competent and environmentally benign approach (free of toxic organic solvents) for the separation and refinement of biomolecules from varying matrixes. ATPS method has the inherent properties such as versatility, highly productive, economical, better purity profile, selectivity and rapid mass transfer rates. It has achieved the position of leading technique in the last decade for separation and purification of enzymes, drugs, antioxidants, amino acids and antibiotics. These systems are usually formed by chemical entities that segregate into two different phases when mixed in specific ranges of composition and temperature e.g. by either mixing two polymers in aqueous media or by a polymer with an inorganic salt or a polymer with an organic salt

Methanolic extract of Marrubium crassidens Boiss has potent antioxidative effects and can have cardio-protective effects on Ischemia/Reperfusion (I/R) injuries in heart. The extract was prepared by maceration. The isolated rat hearts were perfused by Krebs-Henseleit solution enriched with the extract (0, 10, 50, and 100µg/ml), using the langendorff method. After 15 minutes stabilization, the hearts subjected to 30 minutes regional ischemia and then 120 minutes reperfusion. During the experiments hemodynamic functions were recorded and cardiac arrhythmias were determined. At the end, the infarct size was measured. The extract at 100µg/ml caused a significant reduction in the number of ischemia and reperfusion induced ventricular-ectopic-beats (P<0.05). The extract at 100µg/ml also remarkably (P<0.001) reduced the number of ischemic ventricular tachycardia (VT). The incidence of ischemic VT was reduced from 100% in the control group to 20% in the group treated with 100 µg/ml (P<0.01). The infarct size was 70.74±10.35% in the control group whereas, perfusion of ischemic hearts with the extract (10, 50µg/ml) reduced the size to 19.11±6.26 (P<0.001) and 25.27±3.89% (P<0.01), respectively. M. crassidens has protective effects against I/R injuries in isolated rat hearts and the protective effects could be related to antioxidative activities of the extract.

Post-operative nausea and vomiting (PONV) is commonly experienced by patients after surgical procedures. The purpose of the present trial was to compare the antiemetic efficacy of three drugs (generic granisetron, metoclopramide and kytril) for the prevention of acute emesis induced by eye surgery. Patients and One hundred and fifty-one patients undergoing ophthalmic surgery were randomized to receive generic granisetron (n = 51), metoclopramide (n = 50) or kytril (n = 50), intravenously. A standard general anaesthetic technique and postoperative analgesia was used. The PONV and adverse effects of study drugs were assessed during the early (0-6 hrs) and late (6-24 hrs) periods after administration of medications. There was no significant difference between the groups regarding demographic characteristics. Complete protection from retching and vomiting was achieved in all patients receiving generic granisetron. Incidence of nausea, retching and vomiting was significantly higher in the metoclopramide group when compared with generic granisetron group. The most common adverse event in the three groups was headache. No significant difference in the incidence of adverse effects attributable to the study drug was observed between the groups. Generic granisetron was found to have favourable efficacy in the prevention of PONV after eye surgery and could be regarded as a safe and inexpensive alternative for kytril and metoclopramide.

Phytosomes are recently introduced drug delivery system and novel botanical formulation to produce lipophilic molecular complex to improve absorption and bioavailability of phytoconstituent. Quercetin is a well-known flavonoid with different biological effects and contributed in food preserving by free radical scavenging activity. However, bioavailability of Quercetin is an important limiting factor for its antioxidant activities. To overcome this limitation, in the present study we aimed to produce Quercetin-loaded nano phytosomes to improve its physicochemical stability and bioavailability. Quercetin-loaded nano phytosome was prepared by using phosphatidylcholine (PC) and cholesterol (CH). Quercetin nano phytosomes system was characterized by particle size analyzer and differential scanning calorimetry (DSC). Results showed that formulation with the Quercetin: PC: CH molar ratio of 1: 2: 0.2 had lower particle size (80 nm) and higher encapsulation efficiency percent (98%). Results also indicated that incorporation of cholesterol improved the physical stability of nano phytosome for over three weeks. The DSC data showed that incorporation of Quercetin in the phospholipid bilayer reduced the phase transition temperature of bilayer in the nano phytosome structure resulting higher release and bioavailability. Nano phytosomal formulation of Quercetin showed promising potential in fortification of food products with water insoluble antioxidants.

Gamma radiation has been widely used as a post-harvest food preservation process for many years. Irradiation can affect the content of phytochemicals. During processing of almonds, large amounts of by-products such as hull and shell are produced. This study evaluates the effect of gamma radiation on phytochemical content and antioxidant activity of none stored (H1) and stored (H2) almond hull. Both almond hull samples were irradiated with 0, 2, 6 and 10 kGy gamma rays. Total phenolic content (TPC), total flavonoid content (TFC) and bioactivity of the treated samples extracts were investigated by various In vitro colorimetric methods. Irradiation dose of 10 kGy slightly decreased the TPC and TFC values but maintained FRAP value in H1 extracts. The TPC of H2 was increased (p<0.05) at the dose of 10 kGy, while the TFC and FRAP values were constant. 2 kGy dose of gamma irradiation slightly increased the antiradical activity of H1 and H2, but the other doses significantly reduced antiradical activity of extracts. Results showed that gamma irradiation can change the antioxidant content and activity of almond hull.

18-memberd ring of tri-aza dibenzo sulfide (TTD) and dibenzo sulfoxide (TSD) macrocyclic diamides showed the oxidative radical forming ability and further strengthened the documentation of their cytotoxicity effects through lipids, proteins and DNA oxidation damages. With this in mind, our group synthesized some novel macrocyclic base on TTD diamides and a podand. Novel aza macrocyclic diamides were synthesized based on dibenzosulfide using of diester method as N-pivot Lariat ethers from the michael reaction and nucleophilic attack to epoxide ring as a key strategy of corresponding Diamide with acrylonitrile, epoxy- styrene and 1, 2-epoxypropane at reflux in dichloromethane in good overall yields. In addition, a podand was synthesized based on dibenzosulfoxide with epichlorohydrin at reflux in methanol. The structures of these compounds were confirmed using IR, 1H NMR and 13C NMR spectroscopy. The presence of additional oxygen atom considerably increases its hydrogen binding capacity and this property can improve biological and complexation characteristics of primary 18-Membered-ring tri-aza Macrocyclic diamide (TTD).

The OCT4B1 as a new discovered variant of OCT4 is expressed in both cancer cell and tissues. This variant with its anti-apoptotic properties aid cancer cells to scape from apoptosis. TNF ligands and receptors are amongst two categories of eleven gene families involved in the apoptosis pathway. Therefore, the aim of the present study was to investigate the effects of OCT4B1 suppression on several transcripts of both TNF ligands and receptors family in some tumor cell lines. The AGS (gastric adenocarcinoma), 5637 (bladder tumor) and U-87MG (brain tumor) tumor cell lines were transfected with specific OCT4B1 siRNA and, as well as a scrambled sequence and PBS, as controls, using Lipofectamine 2000 comerical kit. The expression of TNF ligand and receptor transcripts were evaluated in parallel with beta-actin (as housekeeping gene) using Real-Time PCR technique. our results indicated that in TNF ligand transcripts family, the mRNA level of TNF transcripts was up-regulated and inversely TNFSF8, TNFSF7, TNFSF10, TNFSF1 and TNFSF6 was down-regulated. We observed also that in TNF receptor transcripts family, six transcripts including, TNFRSF 10A, TNFRSF10B, TNFRSF11B, TNFRSF1A, TNFRSF21 and TNFRSF25 were up-regulated, while TNFRSF9 and CD27 were down-regulated. According to these results, it may be concluded that OCT4B1 suppression can lead to apoptosis in tumor cell lines via up-regulation of several TNF ligand and receptor transcripts. Thus, OCT4B1 suppression effects on TNF and its receptors may be considered as promising target genes in future studies in cancr research and therapy.

Inhibition of angiotensin converting enzyme (i.e inhibition of cleaving angiotensin I to the potent vasoconstrictor angiotensin II) leads to the treatment and reduce the risk of cardiovascular diseases. Peptides (synthetic - natural) with ACE inhibitory activity were studied continuously during the last decades and resulting data were applied by medicinal chemists to design and develop new drugs. Their structure and activity/property relationships were studied during these years and different QSAR models were developed which assisted researchers and manufactures to reduce the cost of experiments. Developed models were reviewed in the present paper according to the applied dataset, descriptors, feature selection methods, model development and validation methods. The selected descriptors for different datasets and models were compared and discussed according to the experimental findings.