Kenneth A. Chinkwo

Investigations into the binding affinities of different human 5-HT4 receptor splice variants.

This study examined whether the drug-receptor-binding sites of 5 selected human 5-HT₄ receptor splice variants [h5-HT_4(a), h5-HT_4(b), h5-HT_4(c), h5-HT_4(d) and h5-HT_4(g)] display preferential affinities towards agonists. The agonists selected on the basis of chemical diversity and clinical relevance were: 5-HT₄ benzamides, renzapride, zacopride and prucalopride; the benzimidazolones, DAU 6236 and BIMU 1; the aromatic ketone, RS67333, and the indole carbazimidamide tegaserod. The rank order of affinities ranging across the splice variants was: tegaserod (pK_i: 7.38–7.91) ≧ Y-36912 (pK_i: 7.03–7.85) = BIMU 1 (pK_i: 6.92–7.78) ≧ DAU 6236 (pK_i: 6.79–7.99) ≧ 5-HT (pK_i: 5.82–7.29) ≧ 5-MeOT (pK_i: 5.64–6.83) ≧ renzapride (pK_i: 4.85–5.56). We obtained affinity values for the 5-HT_4(b), (d) and (g) variants for RS67333 (pK_i: 7:48–8.29), prucalopride (pK_i: 6.86–7.37) and zacopride (pK_i: 5.88–7.0). These results indicate that the ligands interact with the same conserved site in each splice variant. Some splice variants have a higher affinity for certain agonists and the direction of selectivity followed a common trend of lowest affinity at the (d) variant. However, this trend was not evident in functional experiments. Our findings suggest that it may be possible to design splice variant selective ligands, which may be of relevance for experimental drugs but may be difficult to develop clinically.

Distribution of 5-HT3, 5-HT4, and 5-HT7 receptors along the human colon

Background/Aims Several disorders of the gastrointestinal tract are associated with abnormal serotonin (5-HT) signaling or metabolism where the 5-HT3 and 5-HT4 receptors are clinically relevant. The aim was to examine the distribution of 5-HT3, 5-HT4, and 5-HT7 receptors in the normal human colon and how this is associated with receptor interacting chaperone 3, G protein coupled receptor kinases, and protein LIN-7 homologs to extend previous observations limited to the sigmoid colon or the upper intestine. Methods Samples from ascending, transverse, descending, and sigmoid human colon were dissected into 3 separate layers (mucosa, longitudinal, and circular muscles) and ileum samples were dissected into mucosa and muscle layers (n = 20). Complementary DNA was synthesized by reverse transcription from extracted RNA and expression was determined by quantitative or end point polymerase chain reaction. Results The 5-HT3 receptor subunits were found in all tissues throughout the colon and ileum. The A subunit was detected in all samples and the C subunit was expressed at similar levels while the B subunit was expressed at lower levels and less frequently. The 5-HT3 receptor E subunit was mainly found in the mucosa layers. All splice variants of the 5-HT4 and 5-HT7 receptors were expressed throughout the colon although the 5-HT4 receptor d, g, and i variants were expressed less often. Conclusions The major differences in 5-HT receptor distribution within the human colon are in relation to the mucosa and muscular tissue layers where the 5-HT3 receptor E subunit is predominantly found in the mucosal layer which may be of therapeutic relevance.

Can Interference of GIP activity modulate GPCRs for therapeutic gains

Introduction: Carbocysteine is a mucolytic drug similar to acetylcysteine regard to clinical uses. Carbocysteine is widely used in children with respiratory diseases such as bronchitis, pneumonia and other diseases in which the viscous and sticky mucus secretion is present. Annually, in the paediatric emergency department (EDP) are evaluated, investigated and treated on average 24 000 children aged from a couple of weeks up to 18 years. Materials and Methods: This study started from the observation that many children who received carbocysteine on arrival in EDP presented a worsening cough and even bronchospasm. We believe these symptoms are carbocysteine adverse drug reactions (ADRs). It is a retrospective study on 192 children who had various respiratory diseases. The special paper was used for the recorder of ADRs, a paper provided by Pharmacovigilance Department. Children were divided into two groups: group A (89 subjects) who received carbocysteine and group B (103 subjects) who have not received carbocysteine. The data were processed statistically using chi square test (χ2). Results: The most common symptom was cough in both groups (93.26% and 88.35%), followed by fever (65.17% and 65.05%) and rhinoreea (22.47% and 20.39 %). The most common combination of symptoms was cough + fever + rhinoreea (22.47% in group A and 20.39% in group B). In both groups prevailed the productive cough (46.99% and 45.05%). Dry cough and spastic cough was found in 21.69% and 12.05% in group A, respectively, 18.68% and 14.29% in group B. Conclusions: It could be, this drug has an irritating effect on the airways, thus, it should be used with caution in children. In all cases of worsening cough, this effect was associated with carbocysteine. Also, the use for a few days of carbocysteine was associated with the development of wheezing and bronchospasm. In cases of asthma, recurrent wheezing or other similar diseases the use of carbocysteine should be avoided. Ioan Magyar et al., Clinic Pharmacol Biopharmaceut 2013, 2:3 http://dx.doi.org/10.4172/2167-065X.S1.002I the last decade, many schools and colleges of pharmacy have expanded their enrollment by adding distance education sites. These new campuses are responsible for delivering an identical or equivalent curriculum and for meeting the Accreditation Council for Pharmacy Education’s Standards and Guidelines for the Professional Program in Pharmacy Leading to the Doctor of Pharmacy Degree. A number these standards specify that pharmacy programs are responsible for developing student professionalism and leadership in their students. Developing activities to meet these standards can be challenging in the distance campus environment. Opportunities for the development of student professionalism must be incorporated into the didactic and experiential curriculum as well as in activities outside of the curriculum. Professional student organizations offer many opportunities for faculty to foster student professionalism and leadership. Jennifer Williams, Clinic Pharmacol Biopharmaceut 2013, 2:3 http://dx.doi.org/10.4172/2167-065X.S1.002A promotes accumulation of reactive oxygen/nitrogen species (ROS/RNS) in cardiomyocytes leading to contractile dysfunction and cardiac abnormalities, which increases cardiovascular diseases in the elderly. Inducible antioxidant pathways are regulated by nuclear erythroid 2 p45-related factor 2 (Nrf2) through antioxidant response cis-elements (AREs) and are impaired in the aging heart. Acute exercise stress (AES) activates Nrf2 signaling and promotes myocardial antioxidant function in young mice (~2 months), but aging mouse (>23 months) hearts exhibit significant oxidative stress and cardiac hypertrophy due to impaired Nrf2 signaling. Under basal physiological conditions, disruption of Nrf2 showed minimal effects on antioxidant defenses in young Nrf2-/mice. Interestingly, mRNA and protein levels of antioxidants were dramatically (*p<0.001) decreased in Nrf2-/when compared to WT at 2 months of age, suggesting central regulation of defense mechanisms occurs through Nrf2. Further analyses showed that the aged mice had a significant increase in ROS along with a decrease in glutathione (GSH) levels and impaired antioxidants in Nrf2-/when compared to WT. Disruption of Nrf2 appears to induce oxidative stress (increased ROS, HNE-positive proteins), ubiquitination and pro-apoptotic signals in the heart of aging mice. Subsequent pharmacological induction/activation of Nrf2 prevented the deleterious effects of oxidative stress and aging. Our findings conclude that though the loss of Nrf2 is not amenable at younger age; it could severely affect the myocardial antioxidant defenses upon aging. Thus, Nrf2 signaling might be a potential therapeutic target to protect the heart from age-dependent accumulation of ROS by rescuing redox homeostasis to prevent age-related cardiac disorders. Namakkal S. Rajasekaran, Clinic Pharmacol Biopharmaceut 2013, 2:3 http://dx.doi.org/10.4172/2167-065X.S1.002R remains a major cause of childhood blindness worldwide. The smallest, sickest infants develop the most severe cases of ROP that may not be successfully treated by near confluent laser to the avascular retina (current standard of care). There is increased survival of very small preterm infants in hospitals with few neonatologists not optimally equipped to monitor oxygen or inadequate numbers of ophthalmologists to screen and treat ROP. An understanding of ROP pathogenesis with emphasis on proper timing of administration, knowledge of systemic pharmacokinetics of available vascular endothelial growth factor inhibitors, evidence of lack of local ocular toxicity utilizing human histopathology following intravitreal bevacizumab injection, and awareness of possible systemic toxicity related to vascular thrombosis especially during development in vulnerable preterm infants are essential. Efficacy was reported for a single dose of intravitreal bevacizumab (IVB) compared to conventional laser therapy (CLT) in zone I and posterior zone II in the N Engl. J Med 2011;364(7):603-27. Refractive outcomes at age 2 years are available comparing IVB and CLT in 82% of surviving infants who have not had recurrence or complications requiring intraocular surgery. Characteristics of recurrence, especially in zone I cases, are predictable, recognizable, and treatable by one additional dose of IVB. Local complications are largely preventable in the NICU by employing topical anesthesia, restraining the infant appropriately, attending carefully to sterile technique, fixating the eye securely, and utilizing a needle of appropriate length and gauge. Systemic complications have not been reported, but long term safety has not been established. Helen A. Mintz-Hittner, Clinic Pharmacol Biopharmaceut 2013, 2:3 http://dx.doi.org/10.4172/2167-065X.S1.002A many as 2 million Americans may experience symptoms of alcohol withdrawal conditions each year. Alcohol-use disorders can complicate the assessment and treatment of other medical and psychiatric problems that patients may present with. Without appropriate treatment, patients often manifest associated problems such as uncomfortable withdrawal symptoms., Delirium tremens, The Wernicke-Korsakoff syndrom, seizures, and complications due to associated liver disease. Pharmacy, nursing and physician collaboration aims to standardize treatment of these patients using a standard guided approach. A standardized symptom triggered approach to managing alcohol withdrawal symptoms (AWS) was expected to decrease the use of benzodiazepine and hence decrease costs, avoid under treatment of adrenergic hyperactivity, delirium, hallucinations, as well as decrease the need for sitters and reduce hospital length of stay. At the end of the pilot period, patients received less drug than patients who did not use the protocol. When compared to the comparison group, pilot patients required fewer dosing of lorazepam, neuroleptics (Haldol) and required no sitters. There was no use of restraints for escalated agitations, irritability or risk for self-harm which was attributed to better pharmacologic interventions. Compared to previous months, which required 1-2 transfer of patients from the psych floor to the medical surgical units for alcohol related/withdrawal symptoms, there were no transfer of patients to the medical units upon the initiation of the practice guideline. This study suggests that with nursing, physician and pharmacy collaboration, patients at risk for AWS can be safely and effectively managed with a standardized symptom triggered medical approach. Esther Alabi et al., Clinic Pharmacol Biopharmaceut 2013, 2:3 http://dx.doi.org/10.4172/2167-065X.S1.002M may underlie oxidative stress in Alzheimer disease (AD) changes since dysfunction is a prominent and early feature of AD. Recent studies demonstrate that mitochondria are dynamic organelles that undergo continual fission and fusion events which regulate their morphology and distribution. Morphometry showed a small but significant reduction in mitochondria number and enlarged size in AD. Levels of the fission/fusion proteins DLP1, OPA1, Mfn1 and Mfn2C were significantly decreased in AD, yet levels of Fis1 were significantly increased. Interestingly, although all these proteins demonstrate even distribution in the cytoplasm and processes of pyramidal neurons in age-matched control hippocampus, they appeared to accumulate in the soma but not in the processes of pyramidal neurons in AD hippocampus. Given that OPA1, Fis1, and Mfn1/2 are all mitochondrial membrane proteins, the changes in their distribution to soma in AD neurons, suggest changes in mitochondria distribution in these neurons. The expression of fission/fusion proteins was manipulated in M17 cells and primary hippocampal neurons in a way that mimicked their expression changes in AD. These manipulations all reduced mitochondrial density in the cell periphery (M17 cells) or neuronal processes (primary neurons) which correlated with reduced spine numbers (primary neurons). AβPP and Aβ caused reduced expression of DLP1 and OPA1 while increasing expression of Fis1, consistent with our findings in AD brains. Through time lapse study, we were able to demonstrate that mitochondria were able to fuse with each other but at a much slower rate in AβPP overexpressing cells. Overall, we concluded that AβPP, through amyloid-β production impairs mitochondrial fission/fusion balance through regulation of expression of mitochondria fission and fusion proteins. George Perry et al., Clinic Pharmacol Biopharmaceut 2013, 2:3 http://dx.doi.org/10.4172/2167-065X.S1.002Objective: This study aimed to assess the probability of Levofloxacin (Levo) compared to Gatifloxacin (Gati) achieving favorable pharmacodynamic (PD) targets for bacterial eradication and prevention of resistance development in S. pneumoniae in both elderly (≥65 years) and younger (<65 years) patients with Community Acquired Pneumonia (CAP). Material and Methods: As part of a study comparing the clinical outcome of Levo vs. cefuroxime + erythromycin in hospitalized patients with CAP, demographics including age, weight, gender, race and renal function were gathered and analyzed from 263 elderly (≥65 years) and 48 younger patients (<65 years). Previously described and validated population pharmacokinetic (PK) models of levo and gati in patients with CAP were utilized. Free-drug AUC0-24 (f AUC0-24)were simulated in plasma (P) using Levo dosing at 500mg, 750mg and 1000mg OD as well as Gati 200mg and 400mg OD. Use of Monte Carlo simulation allowed for the full variability of encountered drug clearance to be incorporated. S. pneumoniae susceptibility data were obtained from the Canadian Respiratory organism Susceptibility Study (CROSS) study (an annual, national, ongoing surveillance study which has collected 8014 isolates from 1997-2004). Results: Probability of target attainment (f AUC0-24/MIC of 30) of Levo and Gati will be discussed. Conclusions: For all patients and for elderly hospitalized patients with CAP, Levo 750mg and Gati 400mg showed high probability for target attainment of f AUC0-24/MICall of 30. Ayman M. Noreddin, Clinic Pharmacol Biopharmaceut 2013, 2:3 http://dx.doi.org/10.4172/2167-065X.S1.002Aim: of this research was to evaluate the beneficial effects of patient education by community pharmacists on adherence to antibiotics. Methods: Prospective, controlled trials were conducted among patients in two community pharmacies, in Istanbul [n=60], and Kars (Eastern Turkey) [n=199]. Patients receiving prescribed antibiotics completed a questionnaire, the first part of which was conducted before starting treatment, the second part by telephone the day after therapy ended. Patients in the study group were informed about antibiotic usage and resistance, and a brochure detailing how patients should self-administer their antibiotics was provided. Patients in the control group did not receive extra verbal or written information apart from that related to dose and frequency. Adherence was assessed using a tablet count and self-report method. Results: The study in Kars demonstrated that non-adherence rates based on tablet counts, were higher in the control group (p< 0.05). Similarly, patients who did not consciously quit antibiotic treatment, and who subsequently reported having recovered from their infections were more frequently found in the group that had received pahrmacist-led patient education (p< 0.05). The Istanbul study also indicated that patients prescribed a once-a-day dosage regimen for short duration were more adherent (p< 0.05). In addition, more mature patients (over 30 yo) were more adherent than younger patients. By contrast, the Kars study did not observe any significant effect of age on adherence. Conclusions: Higher adherence rates to antibacterial therapy and improved reported clinical outcomes were found in patients educated by the community pharmacist.T pharmacist’s of knowledge of physiology and biochemistry allow them to really learn to apply this knowledge to helping patients with understanding the importance of nutrition to good health and the treatment of chronic disease. There is significant evidence that diabetes, CVD, and even cancer are associated with glucose toxicity. Understanding how to control a patient’s blood glucose through nutritional education and design of a diet plan can be provided by a pharmacist. Add knowledge of nutrition to the patient’s medication therapy plan can increase therapy effectiveness. An understanding of the Glycemic Index and Glycemic Load of differing carbohydrates allows the pharmacist to design a dietary plan for the patient to enhance their total therapy. Point-of-Care devices allow the pharmacist to measure a patient’s body density in particular the percentage of the patient’s weight that is fat, thus allow the pharmacist to focus on developing a diet that is designed to feed muscle and at the same time reduce body fat through the use of Low Glycemic Index carbohydrates. Low Glycemic Index carbohydrates are more slowly absorbed and therefore also maintain a lower serum glucose level for a longer interval, thus the patient will not get hungry as soon as compared to High Glycemic Index carbohydrates. High Glycemic Index carbohydrates produce high peak glucose levels which result in increased fat production. Further the development of a nutrition plan allows the pharmacist to select foods that are high in potassium and low in sodium which brings significant benefit in managing hypertension. The application of nutritional principals to the patient’s diet allows the pharmacist to improve total therapy benefit. Roger S. Klotz, Clinic Pharmacol Biopharmaceut 2013, 2:3 http://dx.doi.org/10.4172/2167-065X.S1.002T purpose was to evaluate the clinical and pharmacoeconomic outcomes associated with improved glycemic control for patients with type two diabetes mellitus (T2DM), whose therapy was managed in a 1⁄2 day per week pharmacist-led Diabetes Intense Medical Management (DIMM) Clinic, at the Veterans Affairs San Diego Healthcare System (VASDHS).Patients referred the DIMM Clinic were compared to a randomly selected comparator group of patients being seen by their primary care provider. Study subjects were greater than 18 years old, diagnosed with T2DM with HbA1c greater than or equal to 8% at initial DIMM Clinic visit (or index visit for comparator group). Clinical outcomes evaluated were HbA1c, fasting plasma glucose, BMI, blood pressure, and lipids. A published regression model (Gilmer et.al., 2009) was used to estimate total medical costs over a threeyear period (including inpatient and outpatient services) for two groups of patients receiving six months of care. Data used to populate the regression model were collected via retrospective chart review. Estimated three-year total medical cost was based on age, gender, the existence of specific co-morbidities (hypertension, hyperlipidemia and heart disease), as well as HbA1c. Cost avoidance in each group was defined as the difference between the cost estimated using data from the initial/index visit vs. the cost estimated using data from 6 month visit. Since HbA1c was the primary variable that could change during the six-month study period, the cost avoidance estimates mainly reflect the change in HbA1c.Results and conclusions will be presented. Candis M. Morello, Clinic Pharmacol Biopharmaceut 2013, 2:3 http://dx.doi.org/10.4172/2167-065X.S1.002This study investigated the effects acetylcholine, atropine,adrenaline, noradrenaline, propanolol, phentolamine, indomethacin; mepacrine, chloroquine; papaverine; brethylium; Adenosine Triphosphate; dipyridamole; guanethidine; d-tubocurarine; hexamethonium; burimamide and Reserpine on the intrinsic tone and responses of the smooth muscles of the rectum of 1 day, 1week and 1month old chicks. The results of the study showed that chick rectum responded to both intrinsic and transmural electrical stimulation with graded, and agedependent biphasic responses. Adrenaline; nor-adrenaline; papaverine; mepacrine; chloroquine; indommethacin; bretylium; hexamethonium; gunethidine; dipyridamole; d-tubocurarine and phentolamine relaxed while atropine, ATP, and acetylcholine contracted chick rectum smooth muscles. Guanethidine, which depletes nor-adrenaline at peripheral nerve endings in the manner of reserpine produced a slight direct relaxation effect on the smooth muscles of chick rectum suggesting that it depleted nor-adrenaline from the sympathetic peripheral nerve endings. Reserpine (which depletes nor-adrenaline, dopamine and serotonin from various binding sites in the brain and peripheral tissues)pre-treatment did not abolish but only diminished the biphasic responses of chick rectum to intrinsic and electrical field stimulation by 98%. This showed that 75% of the biphasic response of chick rectum smooth muscles to intrinsic and electrical stimulation was mediated by serotonin and that all the assayed drugs that relaxed the chick rectum smooth muscles produced their relaxation responses by low-energy stimulation of β sub-units of the serotonin receptors while the drugs that contracted chick rectum smooth muscles produced their contractile responses by high energy-stimulation of α-sub-units of Serotonin receptors of chick rectum smooth muscles. Thus the classes of drugs assayed on chick rectum in this study: cholinergic drugs (acetylcholine, atropine); α-adrenergic -blocking drugs (phentolamine); adrenergic drugs; (adrenaline); β—adrenergic blocking drugs (propranolol); Non-Steroidal Anti-Inflammatory drugs (indomethacin); quinoline drugs (mepacrine, chloroquine); opioid drugs (papaverine); peripheral sympathetic nervous system blocking drugs (bretylium); vasodilator drugs (papaverine); sympathetic neuronal blocking and anti-hypertensive drugs (guanethidine); dilator of coronary arteries (dipyridamole0; neuromuscular blocking drugs (skeletal muscle relaxants) (dtubocurarine); ganglionblocking drugs (hexamethonium); Histamine receptor blocking drugs (burimamide); rauwolfia alkaloids (reserpine) and cellular energy-bond source (ATP) all interact with the body through stimulating/inhibiting one or both of the (β ) (relaxation) or (α) (contraction)-mediating subunits of the Serotonin receptor.I corticosteroids are considered the cornerstone of contemporary pharmaceutical anti-asthma management of children. Small-particle inhaled corticosteroids have recently been introduced for treatment of children. Two such modulations are beclomethasone dipropionate and ciclesonide. A major advantage of small-particle ICS is that they have improved intrapulmonary deposition rates. Therefore, effective asthma control may be achieved at lower daily doses than with the large-particle inhaled corticosteroids. Recent efficacy studies have shown significant results of small-particle ICS on asthmatic inflammation in the small airways. When it comes to safety profiles, however, growth studies and most HPA studies do not support improved safety on the basis of particle size alone and some studies have suggested even higher systemic bioavailability and safety risk with smaller particles, depending on the molecule, the formulation and the applied device. Short term knemometry studies of beclomethasone dipropionate have evaluated various formulations and combinations with long-acting beta-2 agonists in school age children. Further efficacy and safety studies are needed, however, to assess efficacy and possible systemic adverse effects of small-particle ICS for mono and combination therapies, particularly in the long-term management of children in whom large-particle ICS have not been efficacious, and in pre-school age children, in whom airway delivery is difficult with current formulations. Ole D. Wolthers, Clinic Pharmacol Biopharmaceut 2013, 2:3 http://dx.doi.org/10.4172/2167-065X.S1.002T National Traumatology and Orthopedics Institute ( NTOI ) is the holder of the maximum hospitals and clinics quality certification granted by the Joint Commission International, since 2006. At NTOI, due to the surgeries characteristics, the patients exposure to infections is pretty significant, demanding the use of antibiotics ( ATBs ) in a large scale and in many cases for a prolonged time, a fact that may extend the possibility of adverse drug reactions ( ADRs ). So, it was objectified to analyse the incidence of ADRs in hospitalized patients associated with ATBs. It is a cohort study. The sample was compounded by 101 adult patients who were hospitalized during January to December 2012. The gathering of data was prospective using medical records and patients interviews. The project was approved by the Research Ethics Committee with human beings from NTOI (n° 0050.0.305.000-10). All patients were submitted to polypharmacy, 31% used more than 2 ATBs and the most prescribed ATB was vancomycin ( 36% ). The incidence of ADRs associated with ATB was 51%, being the majority ( 58% ) considered possible according to Naranjo Algorithm. It was evidenced that 40% of ADRs were caused by rifampicin and 32% by oxacillin. It is concluded that ADRs can present an important negative impact, referring to the patient wellbeing and the quantity of spending resources. It is necessary that hospitals pharmacovigilance service uses active search as proactive strategy to minimize the ADRs and their clinic and economic impact. Tathiana Martins, Clinic Pharmacol Biopharmaceut 2013, 2:3 http://dx.doi.org/10.4172/2167-065X.S1.002W is the most commonly prescribed oral anticoagulant in the UK, demonstrating effectiveness in preventing and managing a range of thrombotic conditions. However due to factors including unpredictable pharmacokinetics, numerous drug interactions and a narrow therapeutic range, reaching and maintaining therapeutic anticoagulation can be challenging. The risks of over-anticoagulation and major bleeding are highest in the first four weeks of warfarin therapy. To reduce the risk of bleeding related to warfarin initiation in one large UK-based Trust a warfarin initiation protocol was introduced. However, previous Trust-wide audits revealed poor adherence to the protocol. The aim of this study was to identify reasons for poor adherence to the protocol. Thirteen junior doctors across the Trust were interviewed using a semi-structured tool. In addition, a related questionnaire was designed and distributed to junior doctors at training sessions to capture a wider sample. Key findings of the study suggested that participants were aware of the protocol; with 85% of 20 surveyed participants and 92% of 13 interviewees indicating awareness. However a number of potential barriers to protocol adherence were identified. Barriers included protocol inaccessibility; concern of the safety of the protocol’s fixed dose regimen without INR monitoring for the first four days of therapy; discrepancy between the Trust’s ‘modest’ initiation protocol and the more aggressive warfarin initiation regimens generally favoured by participants’ seniors. The study highlighted the need to address concerns about the safety of the protocol, increase awareness of the Trust protocol to all levels of prescriber and improve protocol accessibility. Frances Akinwunmi et al., Clinic Pharmacol Biopharmaceut 2013, 2:3 http://dx.doi.org/10.4172/2167-065X.S1.002

Q-TOF LC/MS identification and UHPLC-Online ABTS antioxidant activity guided mapping of barley polyphenols

The polyphenol composition and antioxidant activity of seven Australian-grown barley varieties were characterized in this study. UHPLC with an online ABTS system was used to identify individual polyphenols while simultaneously measuring their antioxidant activity. The Q-TOF LC/MS system was utilized to identify the phenolic compounds that demonstrated substantial antioxidant activity. The variety, Hindmarsh, showed the highest total phenolic content and antioxidant activity. There was no significant difference observed amongst the other varieties in their total phenolic content, however, they did have significant variation in proanthocyanidin content and antioxidant activity (p < 0.05). Prodelphinidin B3 was the most abundant polyphenol with the highest antioxidant activity amongst all the barley varieties tested. Other polyphenols identified with antioxidant activity included procyanidin, glycosides of catechin and flavan-3-ols. Polyphenol characterization of Australian grown barley varieties demonstrated that they have significant antioxidant activity, hence, promoting the value of whole grain barley as a potential functional food ingredient.

Inhibitory Effects of Pulse Bioactive Compounds on Cancer Development Pathways

Previous studies suggest that pulses may have the potential to protect against cancer development by inhibiting pathways that result in the development of cancer. These pathways include those that result in inflammation, DNA damage, cell proliferation, and metastasis. Other studies have demonstrated extracts from pulses have the capacity to induce apoptosis specifically in cancer cells. Compounds reported to be responsible for these activities have included phenolic compounds, proteins and short chain fatty acids. The majority of the studies have been undertaken using in vitro cell culture models, however, there are a small number of in vivo studies that support the hypothesis that pulse consumption may inhibit cancer development. This review highlights the potential benefit of a diet rich in pulse bioactive compounds by exploring the anti-cancer properties of its polyphenols, proteins and short chain fatty acids.

Chemopreventive potential of cereal polyphenols

Abstract It has been identified that diet is one of the major contributing factors associated with the development of cancer and other chronic pathologies. In the recent years, supplementing regular diet with food and/or its components that contain chemopreventive properties has been considered an effective approach in reducing the incidence of cancer and other lifestyle associated diseases. This systematic review provides an exhaustive summary of the chemopreventive properties exhibited by everyday dietary ingredients such as rice, barley, oats, and sorghum. The studies both in vitro and in vivo reviewed have highlighted the potential role of their polyphenolic content as chemopreventive agents. Polyphenolic compounds including anthocyanins, tricin, protocatechualdehyde, avenanthramide, and 3-deoxyanthocyanins found in rice, barley, oats, and sorghum, respectively, were identified as compounds with potent bioactivity. Studies demonstrated that cereal polyphenols are likely to have chemopreventive activities, particularly those found in pigmented varieties. In conclusion, findings suggest that the consumption of pigmented cereals could potentially have an important role as a natural complementary cancer preventive therapeutic. However, further studies to develop a complete understanding of the mechanisms by which phenolic compounds inhibit cancerous cell proliferation are warranted.