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  1. Alexander JA, Surajudeen A, Aliyu EU, Omeiza AU, Zaini MAA
    Water Sci Technol, 2017 Oct;76(7-8):2232-2241.
    PMID: 29068353 DOI: 10.2166/wst.2017.391
    The present work was aimed at evaluating the multi-metals column adsorption of lead(II), cadmium(II) and manganese(II) ions onto natural bentonite. The bentonite clay adsorbent was characterized for physical and chemical properties using X-ray diffraction, X-ray fluorescence, Brunauer-Emmett-Teller surface area and cation exchange capacity. The column performance was evaluated using adsorbent bed height of 5.0 cm, with varying influent concentrations (10 mg/L and 50 mg/L) and flow rates (1.4 mL/min and 2.4 mL/min). The result shows that the breakthrough time for all metal ions ranged from 50 to 480 minutes. The maximum adsorption capacity was obtained at initial concentration of 10 mg/L and flow rate of 1.4 mL/min, with 2.22 mg/g of lead(II), 1.71 mg/g of cadmium(II) and 0.37 mg/g of manganese(II). The order of metal ions removal by natural bentonite is lead(II) > cadmium(II) > manganese(II). The sorption performance and the dynamic behaviour of the column were predicted using Adams-Bohart, Thomas, and Yoon-Nelson models. The linear regression analysis demonstrated that the Thomas and Yoon-Nelson models fitted well with the column adsorption data for all metal ions. The natural bentonite was effective for the treatment of wastewater laden with multi-metals, and the process parameters obtained from this work can be used at the industrial scale.
  2. Asif U, Saleem Z, Yousaf M, Saeed H, Hashmi FK, Islam M, et al.
    Int J Psychiatry Clin Pract, 2018 Sep;22(3):177-183.
    PMID: 29082784 DOI: 10.1080/13651501.2017.1395055
    OBJECTIVE: The study was aimed to evaluate the gender specific response to adherence and occurrence of side effects among schizophrenic patients in Lahore, Pakistan.

    METHODS: A prospective study was performed for a period of 1 year among 180 newly diagnosed schizophrenics, aged 20-60 years to observe the symptoms, medication adherence and side effects. Morisky-Green-Levine Scale was used to evaluate medication adherence, LUNSER for side effects and PANSS to measure positive and negative symptoms. Data were analyzed using SPSS.

    RESULTS: Positive symptoms (Male: Baseline 36.14 vs. endpoint 23.58, Female: 35.29 vs. 23.74) and negative symptoms (Males 27.9 vs. 20.05, Females 28.41 vs. 20.2) of schizophrenia were equally reduced after a follow up of 1 year in both the genders. Male population suffered more accumulative side effects (11.4 in males vs. 6.40 in females), extrapyramidal symptoms such as tardive dyskinesia and tremors (1.21 in males vs. 0.57 in females) and other side effects as compared to women (p ≤ .005). Males were found poorly adherent to antipsychotic treatment than females (93.3% in males vs. 6.7% in females (p ≤ .005).

    CONCLUSIONS: Prescribing practices should not overlook sex specific factors like hormonal changes, altered brain morphology and socioeconomic factors that may be responsible for the difference in the response to the course of schizophrenia.

  3. Safdar MH, Hussain Z, Abourehab MAS, Hasan H, Afzal S, Thu HE
    Artif Cells Nanomed Biotechnol, 2018 Dec;46(8):1967-1980.
    PMID: 29082766 DOI: 10.1080/21691401.2017.1397001
    This review aims to overview and critically analyses recent developments in achieving tumour-specific delivery of anticancer agents, maximizing anticancer efficacy, and mitigating tumour progression and off-target effects. Stemming from critical needs to develop target-specific delivery vehicles in cancer therapy, various hyaluronic acid (HA)-conjugated nanomedicines have been fabricated owing to their biocompatibility, safety, tumour-specific targetability of drugs and genes, and proficient interaction with cluster-determinant-44 (CD44) receptors over-expressed on the surface of tumour cells. HA-based conjugation or surface modulation of anticancer drugs encapsulated nanocarriers have shown promising efficacy against the various types of carcinomas of liver, breast, colorectal, pancreatic, lung, skin, ovarian, cervical, head and neck and gastric. The success of this emerging platform is assessed in achieving the rapid internalization of anticancer payloads into the tumour cells, impeding cancer cells division and proliferation, induction of cancer-specific apoptosis and prevention of metastasis (tumour progression). This review extends detailed insight into the engineering of HA-based nanomedicines, characterization, utilization for the diagnosis or treatment of CD44 over-expressing cancer subtypes and emphasizing the transition of nanomedicines to clinical cancer therapy.
  4. Sanusi SB, Abu Bakar MF, Mohamed M, Sabran SF, Mainasara MM
    PMID: 29081822 DOI: 10.1155/2017/7185649
    Despite all of the control strategies, tuberculosis (TB) is still a major cause of death globally and one-third of the world's population is infected with TB. The drugs used for TB treatment have drawbacks of causing adverse side effects and emergence of resistance strains. Plant-derived medicines have since been used in traditional medical system for the treatment of numerous ailments worldwide. There were nine major review publications on antimycobacteria from plants in the last 17 years. However, none is focused on Southeast Asian medicinal plants. Hence, this review is aimed at highlighting the medicinal plants of Southeast Asian origin evaluated for anti-TB. This review is based on literatures published in various electronic database. A total of 132 plants species representing 45 families and 107 genera were reviewed; 27 species representing 20.5% exhibited most significant in vitro anti-TB activity (crude extracts and/or bioactive compounds 0-<10 µg/ml). The findings may motivate various scientists to undertake the project that may result in the development of crude extract that will be consumed as complementary or alternative TB drug or as potential bioactive compounds for the development of novel anti-TB drug.
  5. Ho JPY, Merican AM, Hashim MS, Abbas AA, Chan CK, Mohamad JA
    J Arthroplasty, 2017 10;32(10):3176-3183.
    PMID: 28579444 DOI: 10.1016/j.arth.2017.04.060
    BACKGROUND: The posterior tibial slope (PTS) is an important consideration in knee arthroplasty. However, there is still no consensus for the optimal slope. The objectives of this study were (1) to reliably determine the native PTS in this population using 3-dimensional computed tomography scans and (2) to determine the normal reference range for PTS in this population.

    METHODS: One hundred computed tomography scans of disease-free knees were analyzed. A 3-dimensional reconstructed image of the tibia was generated and aligned to its anatomic axis in the coronal and sagittal planes. The tibia was then rotationally aligned to the tibial plateau (tibial centroid axis) and PTS was measured from best-fit planes on the surface of the proximal tibia and individually for the medial and lateral plateaus. This was then repeated with the tibia rotationally aligned to the ankle (transmalleolar axis).

    RESULTS: When rotationally aligned to the tibial plateau, the mean PTS, medial PTS, and lateral PTS were 11.2° ± 3.0 (range, 4.7°-17.7°), 11.3° ± 3.2 (range, 2.7°-19.7°), and 10.9° ± 3.7 (range, 3.5°-19.4°), respectively. When rotationally aligned to the ankle, the mean PTS, medial PTS, and lateral PTS were 11.4° ± 3.0 (range, 5.3°-19.3°), 13.9° ± 3.7 (range, 3.1°-24.4°), and 9.7° ± 3.6 (range, 0.8°-17.7°), respectively.

    CONCLUSION: The PTS in the normal Asian knee is on average 11° (mean) with a reference range of 5°-17° (mean ± 2 standard deviation). This has implications to surgery and implant design.

  6. Jambocus NGS, Ismail A, Khatib A, Mahomoodally F, Saari N, Mumtaz MW, et al.
    Food Nutr Res, 2017;61(1):1338919.
    PMID: 28814950 DOI: 10.1080/16546628.2017.1338919
    Background: Morinda citrifolia L. is widely used as a folk medicinal food plant to manage a panoply of diseases, though no concrete reports on its potential anti-obesity activity. This study aimed to evaluate the potential of M. citrifolia leaf extracts (MLE60) in the prevention of weight gain in vivo and establish its phytochemical profile. Design: Male Sprague-Dawley rats were divided into groups based on a normal diet (ND) or high fat diet (HFD), with or without MLE60 supplementation (150 and 350 mg/kg body weight) and assessed for any reduction in weight gain. Plasma leptin, insulin, adiponectin, and ghrelin of all groups were determined. (1)H NMR and LCMS methods were employed for phytochemical profiling of MLE60. Results: The supplementation of MLE60 did not affect food intake indicating that appetite suppression might not be the main anti-obesity mechanism involved. In the treated groups, MLE60 prevented weight gain, most likely through an inhibition of pancreatic and lipoprotein activity with a positive influence on the lipid profiles and a reduction in LDL levels . MLE60 also attenuated visceral fat deposition in treated subjects with improvement in the plasma levels of obesity-linked factors . (1)Spectral analysis showed the presence of several bioactive compounds with rutin being more predominant. Conclusion: MLE60 shows promise as an anti-obesity agents and warrants further research.
  7. Afzal S, Batool M, Ch BA, Ahmad A, Uzair M, Afzal K
    Pharmacogn Mag, 2017 Jul;13(Suppl 2):S262-S265.
    PMID: 28808390 DOI: 10.4103/pm.pm_398_16
    AIMS: The study is conducted to evaluate the immunomodulatory, cytotoxicity, and antioxidant potential of Ziziphus mauritiana (Rhamnaceae). Phytochemical analysis of Z. mauritiana revealed the presence of alkaloids, anthraquinone glycoside, cardiac glycoside, saponin, tannin, and flavonoids.

    METHODOLOGY: The cytotoxicity of the plant Z. mauritiana was evaluated by brine shrimp lethality test. Antioxidant parameters such as superoxide dismutase (SOD), total antioxidant capacity (T-AOC), and malondialdehyde (MDA) levels were calculated in the plasma of rats after chronic administration of 400 mg/kg of Z. mauritiana for 6 weeks.

    RESULTS: The dichloromethane extract of the plant exhibited significant immunomodulatory activity, with inhibitory concentration 50% of 55.43 ± 7.9. The dichloromethane extracts of the plant showed 70% mortality at concentration 1000 μg/ml. SOD and T-AOC levels were increased while MDA level in the plasma was reduced in the plasma of rats treated with dichloromethane Z. mauritiana.

    CONCLUSION: This can be deduced that the root of Z. mauritiana has immunomodulatory, cytotoxic, and antioxidant potential.

    SUMMARY: Roots of Z. mauritiana was exhibited immunomodulator, cytotoxic and antioxidant activitiesZ. mauritiana showed potential antioxidant activity in rats Abbreviations used: SOD: Superoxide dismutase; T-AOC: Total antioxidant capacity; MDA: Malondialdehyde; ZMRD: Z. mauritiana root extract of dichloromethane fraction; LD50: Z. mauritiana root extract of methanol fraction ZMRM, lethal dose 50.

  8. Yenn TW, Arslan Khan M, Amiera Syuhada N, Chean Ring L, Ibrahim D, Tan WN
    Steroids, 2017 Dec;128:68-71.
    PMID: 29104098 DOI: 10.1016/j.steroids.2017.10.016
    The emergence of beta lactamase producing bacterial strains eliminated the use of beta lactam antibiotics as chemotherapeutic alternative. Beta lactam antibiotics can be coupled with non-antibiotic adjuvants to combat these multidrug resistant strains. We study the synergistic antibiotic effect of stigmasterol as adjuvant of ampicillin against clinical isolates. Ampicillin was used in this study as a beta lactam antibiotic model. All test bacteria were beta lactamase producing clinical isolates. The combination showed significantly better antibiotic activity on all bacteria tested. The two test substances have synergistic antibiotic activity, and the effect was observed in both Gram positive and Gram negative bacteria. The synergistic antibiotic effect of stigmasterol and ampicillin was evident by the low fractional inhibitory concentration (FIC) index on Checkerboard Assay. The results suggest that the combination of ampicillin and stigmasterol acts additively in the treatment of infections caused by beta-lactamase producing pathogens. In bacterial growth reduction assay, ampicillin and stigmasterol alone exhibited very weak inhibitory effect on the bacterial growth, relative to ethanol control. Comparatively, combination of stigmasterol-ampicillin greatly reduced the colony counts at least by 98.7%. In conclusion, we found synergistic effects of stigmasterol and ampicillin against beta lactamase producing clinical isolates. This finding is important as it shows potential application of stigmasterol as an antibiotic adjuvant.
  9. Yankuzo HM, Baraya YS, Mustapha Z, Wong KK, Yaacob NS
    J Ethnopharmacol, 2018 Mar 01;213:31-37.
    PMID: 29100935 DOI: 10.1016/j.jep.2017.10.024
    ETHNOPHARMACOLOGICAL RELEVANCE: Strobilanthes crispus Blume is traditionally consumed among local Malay and indigenous communities for the treatment of cancer and other ailments such as gastrointestinal disorders, inflammatory wounds of snake bite and immune system activation amongst others. We previously demonstrated that a bioactive fraction of S. crispus leaves (F3) was cytotoxic to breast cancer cells in vitro and inhibited tumor growth in N-methyl-N-nitrosourea (NMU)-induced breast cancer rat model. F3 also normalized the white blood cell count in the tumor-bearing animals, indicating its potential immuno-stimulatory effect.

    AIM OF THE STUDY: To evaluate the immune stimulatory effects of F3 from S. crispus in NMU-induced rat mammary tumor model.

    MATERIALS AND METHODS: Immunohistochemistry analysis of cellular immune parameters (CD4+ or CD8+ T cells, CIITA, MHC-II and CD68) was performed on NMU-induced rat mammary tumor nodules, followed by evaluation of the serum level of 34 cytokines using the cytokine antibody array.

    RESULTS: Significant increase in MHC-II, CD4+ and CD8+ T cell and CIITA expression by tumor cells was observed in F3-treated rats compared to the tumor control group. F3-treated rats also displayed a significant decrease in the serum level of CCL2 and CD68+ infiltrating macrophages. Serum IFN-γ level in this group was increased by 1.7-fold suggesting enhanced infiltration of T cells, and upregulation of CIITA and MHC-II expression in the tumor cells might be triggered by F3-induced production of IFN-γ.

    CONCLUSION: Our findings demonstrated for the first time that a subfraction from S. crispus, F3, is capable of activating the immune system in rats-bearing NMU-induced mammary tumor, which may contribute to the anticancer effects of F3, and additionally support the traditional use of S. crispus leaves to boost the immune system.

  10. Taha M, Irshad M, Imran S, Chigurupati S, Selvaraj M, Rahim F, et al.
    Eur J Med Chem, 2017 Dec 01;141:530-537.
    PMID: 29102178 DOI: 10.1016/j.ejmech.2017.10.028
    Piperazine Sulfonamide analogs (1-19) have been synthesized, characterized by different spectroscopic techniques and evaluated for α-amylase Inhibition. Analogs 1-19 exhibited a varying degree of α-amylase inhibitory activity with IC50 values ranging in between 1.571 ± 0.05 to 3.98 ± 0.397 μM when compared with the standard acarbose (IC50 = 1.353 ± 0.232 μM). Compound 1, 2, 3 and 7 showed significant inhibitory effects with IC50 value 2.348 ± 0.444, 2.064 ± 0.04, 1.571 ± 0.05 and 2.118 ± 0.204 μM, respectively better than the rest of the series. Structure activity relationships were established. Molecular docking studies were performed to understand the binding interaction of the compounds.
  11. Mokhtar NH, Abas A, Razak NA, Hamid MNA, Teong SL
    J Theor Biol, 2017 11 21;433:73-84.
    PMID: 28844907 DOI: 10.1016/j.jtbi.2017.08.016
    Proper design of stent for application at specific aneurysm effect arteries could help to reduce the issues with thrombosis and aneurysm. In this paper, four types of stent configuration namely half-Y (6 mm), half-Y (4 mm), cross-bar, and full-Y configuration will implanted on real 3D artery bifurcation aneurysm effected arteries. Comparisons were then conducted based on the flow patterns after stent placement using both LBM-based solver and PIV experimental findings. According to the data obtained from all 4 stent designs, the flow profiles and the computed velocity from both methods were in agreement with each other. Both methods found that half-Y (6 mm) stent configuration is by far the best configuration in reducing the blood velocity at the vicinity of the aneurysm sac. The analysis also show that the half-Y (6 mm) stent configuration recorded the highest percentage of velocity reduction and managed to substantially reduce the pressure at the bifurcation region. This high flow velocity reduction through the use of half-Y stent could consequently promote the formation of thrombus thereby reducing the risk of rupture in the aneurysm sac.
  12. Omar N, Hamidon NH, Yunus MH, Noordin R, Choong YS, Lim TS
    Biotechnol Appl Biochem, 2018 May;65(3):346-354.
    PMID: 28833498 DOI: 10.1002/bab.1591
    Phage display has been applied successfully as a tool for the generation of monoclonal antibodies (mAbs). Naive antibody libraries are unique as they are able to overcome several limitations associated with conventional mAb generation methods like the hybridoma technology. Here, we performed an in vitro selection and generation of Fab antibodies against Brugia malayi SXP protein (BmSXP), a recombinant antigen for the detection of lymphatic filariasis. We developed a naïve multi ethnic Fab antibody library with an estimated diversity of 2.99 × 109 . The antibody library was used to screen for mAbs against BmSXP recombinant antigen. Soluble monoclonal Fab antibodies against BmSXP were successfully isolated from the naïve library. The Fab antibodies obtained were expressed and analyzed to show its binding capability. The diversity obtained from a pool of donors from various ethnic groups allowed for a diverse antibody library to be generated. The mAbs obtained were also functional in soluble form, which makes it useful for further downstream applications. We believe that the Fab mAbs are valuable for further studies and could also contribute to improvements in the diagnosis of filariasis.
  13. Thent ZC, Zaidun NH, Azmi MF, Senin MI, Haslan H, Salehuddin R
    Curr Drug Targets, 2017;18(6):734-750.
    PMID: 27919208 DOI: 10.2174/1389450118666161205125548
    Colorectal cancer (CRC) remains one of the major leading causes of cancer related morbidity and mortality. Apart from the conventional anti-neoplastic agents, metformin, a biguanide anti-diabetic agent, has recently found to have anti-cancer property. Several studies observed the effect of metformin towards its anti-cancer effect on colon or colorectal cancer in diabetic patients. However, only a few studies showed its effect on colorectal cancer in relation to the non-diabetic status. The present review aimed to highlight the insight into the molecular pathway of metformin towards colorectal cancer in the absence of diabetes mellitus. In CRC-independent of diabetes mellitus, highly deregulation of PI3K/AKT pathway is found which activates the downstream mammalian target of rapamycin (mTOR). Metformin inhibits cancer growth in colon by suppressing the colonic epithelial proliferation by inhibiting the mTOR pathway. Metformin exerts its anti-neoplastic effects by acting on tumour suppressor pathway via activating the adenosine monophosphate.activated protein kinase (AMPK) signaling pathway. Metformin interrupts the glucose metabolism by activating the AMPK. Metformin reduces tumour cell growth and metastasis by activating the p53 tumour suppressor gene. In addition to its therapeutic benefits, metformin is easily accessible, cost effective with better tolerance to the patients compared to the chemotherapeutic agents. This review summarised modern findings on the therapeutic applications of metformin on the colorectal cancer with no evidences of diabetes mellitus.
  14. Hasan SS, Thiruchelvam K, Kow CS, Ghori MU, Babar ZU
    Expert Rev Pharmacoecon Outcomes Res, 2017 Oct;17(5):431-439.
    PMID: 28825502 DOI: 10.1080/14737167.2017.1370376
    INTRODUCTION: Medication reviews is a widely accepted approach known to have a substantial impact on patients' pharmacotherapy and safety. Numerous options to optimise pharmacotherapy in older people have been reported in literature and they include medication reviews, computerised decision support systems, management teams, and educational approaches. Pharmacist-led medication reviews are increasingly being conducted, aimed at attaining patient safety and medication optimisation. Cost effectiveness is an essential aspect of a medication review evaluation. Areas covered: A systematic searching of articles that examined the cost-effectiveness of medication reviews conducted in aged care facilities was performed using the relevant databases. Pharmacist-led medication reviews confer many benefits such as attainment of biomarker targets for improved clinical outcomes, and other clinical parameters, as well as depict concrete financial advantages in terms of decrement in total medication costs and associated cost savings. Expert commentary: The cost-effectiveness of medication reviews are more consequential than ever before. A critical evaluation of pharmacist-led medication reviews in residential aged care facilities from an economical aspect is crucial in determining if the time, effort, and direct and indirect costs involved in the review rationalise the significance of conducting medication reviews for older people in aged care facilities.
  15. Ashri A, Amalina N, Kamil A, Fazry S, Sairi MF, Nazar MF, et al.
    Int J Biol Macromol, 2018 Feb;107(Pt B):2412-2421.
    PMID: 29056465 DOI: 10.1016/j.ijbiomac.2017.10.125
    Starch-based hydrogels are promising smart materials for biomedical and pharmaceutical applications, which offer exciting perspectives in biophysical research at molecular level. This work was intended to develop, characterize and explore the properties of hydrogel from starch extracted from new source, Dioscorea hispida Dennst. Starch-mediated hydrogels were successfully synthesized via free radical polymerization method with varying concentrations of acrylic acid (AA),N,N'-methylenebisacrylamide (MBA) and sodium hydroxide (NaOH) in aqueous system. The grafting reaction between starch and AA was examined by observing the decline in intensity peak of hydrogel FTIR spectrum at 3291cm-1 and peak around 1600-1680cm-1, indicating the stretching of hydroxyl group (OH) and stretching of carbon-carbon double bond (CC) respectively. The effects of cross-linker, monomer and NaOH concentration on swelling ratio and gel content in different medium and conditions were also evaluated. The thermal stability and structural morphology of as-synthesized hydrogels were studied by thermogravimetry analysis (TGA) and scanning electron microscopy (SEM). In-vitro cytotoxicity study using small intestine cell line (FHS-74 Int) revealed that the as-formulated eco-friendly-hydrogel was free from any harmful material and safe to use for future product development.
  16. Imran S, Taha M, Selvaraj M, Ismail NH, Chigurupati S, Mohammad JI
    Bioorg Chem, 2017 08;73:121-127.
    PMID: 28648924 DOI: 10.1016/j.bioorg.2017.06.007
    A series of twenty indole hydrazone analogs (1-21) were synthesized, characterized by different spectroscopic techniques such as 1H NMR and EI-MS, and screened for α-amylase inhibitory activity. All analogs showed a variable degree of α-amylase inhibition with IC50 values ranging between 1.66 and 2.65μM. Nine compounds that are 1 (2.23±0.01μM), 8 (2.44±0.12μM), 10 (1.92±0.12μM), 12 (2.49±0.17μM), 13 (1.66±0.09μM), 17 (2.25±0.1μM), 18 (1.87±0.25μM), 20 (1.83±0.63μM), and 19 (1.97±0.02μM) showed potent α-amylase inhibition when compared with the standard acarbose (1.05±0.29μM). Other analogs showed good to moderate α-amylase inhibition. The structure activity relationship is mainly focusing on difference of substituents on phenyl part. Molecular docking studies were carried out to understand the binding interaction of the most active compounds.
  17. Hassali MA, Arief M, Saleem F, Khan MU, Ahmad A, Mariam W, et al.
    Pharm Pract (Granada), 2017 Apr-Jun;15(2):929.
    PMID: 28690695 DOI: 10.18549/PharmPract.2017.02.929
    OBJECTIVE: The present study was aimed to evaluate the practices and attitudes of young Malaysian adults towards the use of antibiotics, and to determine the socioeconomic factors associated with the antibiotic use.

    METHODS: A survey was carried in Cheras community by approaching a conveniently selected sample of 480 participants. A pre-tested questionnaire was used for data collection.

    RESULT: Of 480 participants approached, 400 agreed to participate in this study, giving a response rate of 83.3%. The study results showed that 42.75% of the participants exhibited poor attitudes towards antibiotic usage. Chinese race and high income were significantly associated with the positive attitudes towards antibiotic usage. It is shown that the practice of the participants towards antibiotics was relatively poor. The majority of participants agreed that they do not consult a doctor for minor illnesses (64%). The main reason for not consulting a doctor was the high fees of consultation (34.25%) and the inconvenience of visit (29.25%). However, a large proportion of respondents (77.5%) agreed that there is a need to enhance antibiotic education among public.

    CONCLUSION: The study results identified some crucial gaps in the attitudes and practices of Cheras community about the use of antibiotics. Thus, improving the public knowledge and changing their attitude towards antibiotic use along with proper interventions to regulate the ease of their availability would play a significant role for the effective use of antibiotics in the community.
  18. Teah YF, Abduraman MA, Amanah A, Adenan MI, Sulaiman SF, Tan ML
    Food Chem Toxicol, 2017 Sep;107(Pt A):293-301.
    PMID: 28689918 DOI: 10.1016/j.fct.2017.07.011
    Elephantopus scaber Linn and its major bioactive component, deoxyelephantopin are known for their medicinal properties and are often reported to have various cytotoxic and antitumor activities. This plant is widely used as folk medicine for a plethora of indications although its safety profile remains unknown. Human ether-a-go-go-related gene (hERG) encodes the cardiac IKr current which is a determinant of the duration of ventricular action potentials and QT interval. The hERG potassium channel is an important antitarget in cardiotoxicity evaluation. This study investigated the effects of deoxyelephantopin on the current, mRNA and protein expression of hERG channel in hERG-transfected HEK293 cells. The hERG tail currents following depolarization pulses were insignificantly affected by deoxyelephantopin in the transfected cell line. Current reduction was less than 40% as compared with baseline at the highest concentration of 50 μM. The results were consistent with the molecular docking simulation and hERG surface protein expression. Interestingly, it does not affect the hERG expression at both transcriptional and translational level at most concentrations, although higher concentration at 10 μM caused protein accumulation. In conclusion, deoxyelephantopin is unlikely a clinically significant hERG channel and Ikr blocker.
  19. Al-Zuaidy MH, Mumtaz MW, Hamid AA, Ismail A, Mohamed S, Razis AFA
    BMC Complement Altern Med, 2017 Jul 10;17(1):359.
    PMID: 28693595 DOI: 10.1186/s12906-017-1849-2
    BACKGROUND: Type 2 diabetes mellitus (T2DM) is a metabolic disorder characterized by continuous hyperglycemia associated with insulin resistance and /or reduced insulin secretion. There is an emerging trend regarding the use of medicinal plants for the treatment of diabetes mellitus. Melicope lunu-ankenda (ML) is one of the Melicope species belonging to the family Rutaceae. In traditional medicines, its leaves and flowers are known to exhibit prodigious health benefits. The present study aimed at investigating anti-diabetic effect of Melicope lunu-ankenda (ML) leaves extract.

    METHODS: In this study, anti-diabetic effect of ML extract is investigated in vivo to evaluate the biochemical changes, potential serum biomarkers and alterations in metabolic pathways pertaining to the treatment of HFD/STZ induced diabetic rats with ML extract using 1H NMR based metabolomics approach. Type 2 diabetic rats were treated with different doses (200 and 400 mg/kg BW) of Melicope lunu-ankenda leaf extract for 8 weeks, and serum samples were examined for clinical biochemistry. The metabolomics study of serum was also carried out using 1H NMR spectroscopy in combination with multivariate data analysis to explore differentiating serum metabolites and altered metabolic pathways.

    RESULTS: The ML leaf extract (400 mg/kg BW) treatment significantly increased insulin level and insulin sensitivity of obese diabetic rats, with concomitant decrease in glucose level and insulin resistance. Significant reduction in total triglyceride, cholesterol and low density lipoprotein was also observed after treatment. Interestingly, there was a significant increase in high density lipoprotein of the treated rats. A decrease in renal injury markers and activities of liver enzymes was also observed. Moreover, metabolomics studies clearly demonstrated that, ML extract significantly ameliorated the disturbance in glucose metabolism, tricarboxylic acid cycle, lipid metabolism, and amino acid metabolism.

    CONCLUSION: ML leaf extract exhibits potent antidiabetic properties, hence could be a useful and affordable alternative option for the management of T2DM.

  20. Khan NB, Ibrahim Z, Nguyen LTT, Javed MF, Jameel M
    PLoS One, 2017;12(10):e0185832.
    PMID: 28982172 DOI: 10.1371/journal.pone.0185832
    This study numerically investigates the vortex-induced vibration (VIV) of an elastically mounted rigid cylinder by using Reynolds-averaged Navier-Stokes (RANS) equations with computational fluid dynamic (CFD) tools. CFD analysis is performed for a fixed-cylinder case with Reynolds number (Re) = 104 and for a cylinder that is free to oscillate in the transverse direction and possesses a low mass-damping ratio and Re = 104. Previously, similar studies have been performed with 3-dimensional and comparatively expensive turbulent models. In the current study, the capability and accuracy of the RANS model are validated, and the results of this model are compared with those of detached eddy simulation, direct numerical simulation, and large eddy simulation models. All three response branches and the maximum amplitude are well captured. The 2-dimensional case with the RANS shear-stress transport k-w model, which involves minimal computational cost, is reliable and appropriate for analyzing the characteristics of VIV.
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