Antioxidant and Gastroprotective Activity of Suaeda fruticosa Forssk. Ex J.F.Gmel.

Suaeda fruticosa Forssk. Ex J.F.Gmel is traditionally used for inflammatory and digestive disorders, as a carminative, and for diarrhea. This plant is widely distributed in Asia, Africa, and the Mediterranean region. Aqueous methanolic extract of S. fruticosa (Sf.Cr) was prepared and screened for phytoconstituents through qualitative and GC-MS analysis. Quantification of total phenolic and flavonoid contents was performed, while antioxidant capacity was determined by DPPH, CUPRAC, FRAP, and ABTS assays. The gastroprotective activity was assessed in an ethanol-induced ulcer model. Gastric secretory parameters and macroscopic ulcerated lesions were analyzed and scored for ulcer severity. After scoring, histopathology was performed, and gastric mucus contents were determined. Oral pre-treatment of Sf.Cr demonstrated significant gastroprotection. The gastric ulcer severity score and ulcer index were reduced while the %-inhibition of ulcer was increased dose-dependently. The Sf.Cr significantly elevated the pH of gastric juice, while a decrease in total acidity and gastric juice volume was observed. Histopathology demonstrated less oedema and neutrophil infiltration in gastric mucosa of rats pre-treated with the Sf.Cr in comparison to ethanol-intoxicated animals. Furthermore, the gastric mucus contents were increased as determined by alcian blue binding. Sf.Cr showed marked gastroprotective activity, which can be attributed to antioxidant, antisecretory, and cytoprotective effects.

Phosphorylation of cardiac voltage-gated sodium channel: Potential players with multiple dimensions.

Cardiomyocytes are highly coordinated cells with multiple proteins organized in micro domains. Minor changes or interference in subcellular proteins can cause major disturbances in physiology. The cardiac sodium channel (NaV 1.5) is an important determinant of correct electrical activity in cardiomyocytes which are localized at intercalated discs, T-tubules and lateral membranes in the form of a macromolecular complex with multiple interacting protein partners. The channel is tightly regulated by post-translational modifications for smooth conduction and propagation of action potentials. Among regulatory mechanisms, phosphorylation is an enzymatic and reversible process which modulates NaV 1.5 channel function by attaching phosphate groups to serine, threonine or tyrosine residues. Phosphorylation of NaV 1.5 is implicated in both normal physiological and pathological processes and is carried out by multiple kinases. In this review, we discuss and summarize recent literature about the (a) structure of NaV 1.5 channel, (b) formation and subcellular localization of NaV 1.5 channel macromolecular complex, (c) post-translational phosphorylation and regulation of NaV 1.5 channel, and (d) how these phosphorylation events of NaV 1.5 channel alter the biophysical properties and affect the channel during disease status. We expect, by reviewing these aspects will greatly improve our understanding of NaV 1.5 channel biology, physiology and pathology, which will also provide an insight into the mechanism of arrythmogenesis at molecular level.

ANTIOXIDANT, ANTIBACTERIAL AND GUT MODULATING ACTIVITIES OF KALANCHOE LACINIATA.

Kalanchoe laciniata (L.) DC. (Crassulaceae) is a widely distributed plant in Africa and Asia. Traditionally, various communities use this plant for the treatment of a variety of ailments such as gut prob- lems, allergic conditions and wounds. The current study was designed to explore the antibacterial, antioxidant and gut modulating activities of K. laciniata in order to provide scientific rationale for its traditional uses. Phytochemical compounds were assessed through screening 70% crude methanolic extract of K. laciniata. Its gut modulatory activity was evaluated by in vitro tissue experiments on rabbit jejunum which yielded maximal spasmogenic response of 28.4 ± 4.6% (n = 4) at 3 mg/mL, while spasmolytic response was recorded with EC50 value of 3.2 mg/mL (2.8-3.5, 95% CI, n = 5). In antibacterial assays crude extract was found effective against Stapllococcus aurus and Bacillus subtilis, with MIC value of 5 and 2.5 mg/mL, respectively. The testing of the methanolic crude extract for antioxidants resulted in total phenolic contents of 27.8 ± 1.8 mg GAE/g DW and 22.7 ± 2.1 mg AAE/g DW total antioxidant activity. It also scavenged 17.3 ± 3.0% of DPPH free radical when compared with quercitin.

Differential modulation of fast inactivation in cardiac sodium channel splice variants by Fyn tyrosine kinase.

BACKGROUND/AIMS: Post-translational modifications such as phosphorylation and dephosphorylation can finely tune the function of ion channels. Nav1.5 is the main sodium channel in human hearts and alternative splicing of the transcript generates two major splice variants, characterized by the presence (Q-pre) or absence (Q-del) of glutamine at position 1077. In the heart, both the Nav1.5 channel and Fyn tyrosine kinase are colocalized at adherens junctions. This study aimed to investigate the modulation of the aforementioned splice variants by Fyn tyrosine kinase. METHODS AND RESULTS: Q-del and Q-pre were transiently expressed alone, with catalytically active Fyn kinase (FynKa) or with a catalytically dead Fyn kinase (FynKd). Co-expression of Nav1.5 channel splice variants and Fyn kinase was confirmed by Western blotting and their Interaction was established by co-immunoprecipitation experiments. The enzymatic activity of Fyn kinase and phosphorylation of Nav1.5 channel were ascertained by immunoprecipitation and anti-phosphotyrosine immunoblotting. Whole-cell ionic currents were recorded in patch clamp experiments to examine the modulation of Nav1.5 channel variants by Fyn kinase, which indicated a hyperpolarizing shift of 9.68 mV in fast inactivation of Q-del. In contrast, a depolarizing shift of 8.77 mV in fast inactivation was observed in the case of Q-pre, while activation curves remained unaltered for both splice variants. This differential modulation in fast inactivation was further assessed by mutating tyrosine 1495 to phenylalanine in the inactivation loop, which completely removed the modulatory effect of Fyn kinase in Q-pre splice variant, while in Q-del variant hyperpolarizing shift in fast inactivation was reduced to 4.74 mV. Finally, the modulatory effect of Fyn kinase was compensated at a mid-value of 94.63 ± 0.34, when both splice variants were co-expressed at a normal physiological ratio. CONCLUSION: Q-del and Q-pre were differentially modulated by Fyn kinase, and this fine modification resulted in smooth electrical activity in the heart.

Understanding, perceptions and self-use of complementary and alternative medicine (CAM) among Malaysian pharmacy students.

BACKGROUND: In recent times the basic understanding, perceptions and CAM use among undergraduate health sciences students have become a topic of interest. This study was aimed to investigate the understanding, perceptions and self-use of CAM among pharmacy students in Malaysia. METHODS: This cross-sectional study was conducted on 500 systematically sampled pharmacy students from two private and one public university. A validated, self-administered questionnaire comprised of seven sections was used to gather the data. A systematic sampling was applied to recruit the students. Both descriptive and inferential statistics were applied using SPSS® version 18. RESULTS: Overall, the students tend to disagree that complementary therapies (CM) are a threat to public health (mean score = 3.6) and agreed that CMs include ideas and methods from which conventional medicine could benefit (mean score = 4.7). More than half (57.8%) of the participants were currently using CAM while 77.6% had used it previously. Among the current CAM modalities used by the students, CM (21.9%) was found to be the most frequently used CAM followed by Traditional Chinese Medicine (TCM) (21%). Most of the students (74.8%) believed that lack of scientific evidence is one of the most important barriers obstructing them to use CAM. More than half of the students perceived TCM (62.8%) and music therapy (53.8%) to be effective. Majority of them (69.3%) asserted that CAM knowledge is necessary to be a well-rounded professional. CONCLUSIONS: This study reveals a high-percentage of pharmacy students who were using or had previously used at least one type of CAM. Students of higher professional years tend to agree that CMs include ideas and methods from which conventional medicine could benefit.