Displaying publications 21 - 40 of 68 in total

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  1. Kabir MZ, Feroz SR, Mukarram AK, Alias Z, Mohamad SB, Tayyab S
    J Biomol Struct Dyn, 2016 Aug;34(8):1693-704.
    PMID: 26331959 DOI: 10.1080/07391102.2015.1089187
    Interaction of a tyrosine kinase inhibitor, vandetanib (VDB), with the major transport protein in the human blood circulation, human serum albumin (HSA), was investigated using fluorescence spectroscopy, circular dichroism (CD) spectroscopy, and molecular docking analysis. The binding constant of the VDB-HSA system, as determined by fluorescence quenching titration method was found in the range, 8.92-6.89 × 10(3 )M(-1) at three different temperatures, suggesting moderate binding affinity. Furthermore, decrease in the binding constant with increasing temperature revealed involvement of static quenching mechanism, thus affirming the formation of the VDB-HSA complex. Thermodynamic analysis of the binding reaction between VDB and HSA yielded positive ΔS (52.76 J mol(-1) K(-1)) and negative ΔH (-6.57 kJ mol(-1)) values, which suggested involvement of hydrophobic interactions and hydrogen bonding in stabilizing the VDB-HSA complex. Far-UV and near-UV CD spectral results suggested alterations in both secondary and tertiary structures of HSA upon VDB-binding. Three-dimensional fluorescence spectral results also showed significant microenvironmental changes around the Trp residue of HSA consequent to the complex formation. Use of site-specific marker ligands, such as phenylbutazone (site I marker) and diazepam (site II marker) in competitive ligand displacement experiments indicated location of the VDB binding site on HSA as Sudlow's site I (subdomain IIA), which was further established by molecular docking results. Presence of some common metal ions, such as Ca(2+), Zn(2+), Cu(2+), Ba(2+), Mg(2+), and Mn(2+) in the reaction mixture produced smaller but significant alterations in the binding affinity of VDB to HSA.
    Matched MeSH terms: Piperidines/metabolism; Piperidines/pharmacology; Piperidines/chemistry*
  2. Kia Y, Osman H, Kumar RS, Murugaiyah V, Basiri A, Perumal S, et al.
    Bioorg Med Chem Lett, 2013 May 15;23(10):2979-83.
    PMID: 23570788 DOI: 10.1016/j.bmcl.2013.03.027
    A series of novel hybrid spiro heterocycles comprising pyrrolizine, spiroxindole and piperidine moieties was synthesized chemo-, regio- and stereoselectively in good yields from 1,3-dipolar cycloaddition reaction of a series of 1-acryloyl-3,5-bisarylmethylidenepiperidin-4-ones with azomethine ylides generated in situ from 5-choloroisatin and l-proline in methanol. These cycloadducts displayed significant cholinesterase inhibitory activity. Among the compounds screened, 8g and 8e, showed maximum inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinestrase (BChE) with IC50 values of 3.33 and 3.13μM, respectively.
    Matched MeSH terms: Piperidines/chemical synthesis; Piperidines/pharmacology*; Piperidines/chemistry
  3. Iwata N, Ishigooka J, Kim WH, Yoon BH, Lin SK, Sulaiman AH, et al.
    Schizophr Res, 2020 01;215:408-415.
    PMID: 31471246 DOI: 10.1016/j.schres.2019.07.055
    BACKGROUND: Blonanserin is a second-generation antipsychotic used for the treatment of schizophrenia. This study determined the efficacy, safety and pharmacokinetics of a blonanserin transdermal patch in patients with acutely exacerbated schizophrenia.

    METHODS: This double-blind, multicenter, phase 3 study consisted of a 1-week observation period during which patients were treated with two patches of placebo, followed by a 6-week double-blind period where patients were randomized (1:1:1) to receive once-daily blonanserin 40 mg, blonanserin 80 mg, or placebo patches. The primary endpoint was the change from baseline in the total Positive and Negative Symptom Scale (PANSS) score. Safety assessments included treatment-emergent adverse events (TEAEs).

    RESULTS: Between December 2014 and October 2018, patients were recruited and randomly assigned to blonanserin 40 mg (n = 196), blonanserin 80 mg (n = 194), or placebo (n = 190); of these, 77.2% completed the study. Compared with placebo, blonanserin significantly improved PANSS total scores at 6 weeks (least square mean [LSM] difference vs placebo: -5.6 with blonanserin 40 mg; 95% confidence interval [CI] -9.6, -1.6; adjusted p = 0.007, and - 10.4 with blonanserin 80 mg; 95% CI -14.4, -6.4; adjusted p 

    Matched MeSH terms: Piperidines/administration & dosage; Piperidines/adverse effects; Piperidines/pharmacology*
  4. Muniandy, Kalaivani, Sankar, Prabu Siva, Lian, Benedict Shi Xiang, Khoo, Alan Soo-Beng, Balakrishnan, Venugopal, Mohana-Kumaran, Nethia
    Trop Life Sci Res, 2016;27(11):125-130.
    MyJurnal
    Spheroids have been shown to recapitulate the tumour in vivo with properties
    such as the tumour microenvironment, concentration gradients, and tumour phenotype. As
    such, it can serve as a platform for determining the growth and invasion behaviour pattern
    of the cancer cells as well as be utilised for drug sensitivity assays; capable of exhibiting
    results that are closer to what is observed in vivo compared to two-dimensional (2D) cell
    culture assays. This study focused on establishing a three-dimensional (3D) cell culture
    model using the Nasopharyngeal Carcinoma (NPC) cell line, HK1 and analysing its growth
    and invasion phenotypes. The spheroids will also serve as a model to elucidate their
    sensitivity to the chemotherapeutic drug, Flavopiridol. The liquid overlay method was
    employed to generate the spheroids which was embedded in bovine collagen I matrix for
    growth and invasion phenotypes observation. The HK1 cells formed compact spheroids
    within 72 hours. Our observation from the 3 days experiments revealed that the spheroids
    gradually grew and invaded into the collagen matrix, showing that the HK1 spheroids are
    capable of growth and invasion. Progressing from these experiments, the HK1 spheroids
    were employed to perform a drug sensitivity assay using the chemotherapeutic drug,
    Flavopiridol. The drug had a dose-dependent inhibition on spheroid growth and invasion.
    Matched MeSH terms: Piperidines
  5. Arshad L, Jantan I, Bukhari SNA
    Drug Des Devel Ther, 2019;13:1421-1436.
    PMID: 31118577 DOI: 10.2147/DDDT.S185191
    Background: 3,5-Bis[4-(diethoxymethyl)benzylidene]-1-methyl-piperidin-4-one (BBP), a novel synthetic curcumin analogue has been revealed to possess strong in vitro and in vivo immunosuppressive effects. Purpose: The aim of present study was to prepare and characterize BBP-encapsulated polylactic-co-glycolic acid-block-polyethylene glycol (PLGA-b-PEG) nanoparticles and to evaluate its in vivo efficacy against innate and adaptive immune responses. Methods: Male BALB/c mice were orally administered with BBP alone and BBP- encapsulated nanoparticles equivalent to 5, 10 and 20 mg/kg of BBP in distilled water for a period of 14 days. The immunomodulatory potential was appraised by determining its effects on non-specific and specific immune parameters. Results: The results showed that BBP was successfully encapsulated in PLGA-b-PEG polymer with 154.3 nm size and high encapsulation efficiency (79%) while providing a sustained release for 48 hours. BBP nanoparticles showed significant enhanced dose-dependent reduction on the migration of neutrophils, Mac-1 expression, phagocytic activity, reactive oxygen species (ROS) production, serum levels of ceruloplasmin and lysozyme, immunoglobulins and myloperoxidase (MPO) plasma levels when compared to unencapsulated BBP. Enhanced dose-dependent inhibition was also observed on lymphocyte proliferation along with the downregulation of effector cells expression and release of cytokines, and reduction in rat paw oedema in BBP nanoparticles treated mice. At higher doses the suppressive effects of the BBP nanoparticles on various cellular and humoral parameters of immune responses were comparable to that of cyclosporine-A at 20 mg/kg. Conclusion: These findings suggest that the immunosuppressive effects of BBP were enhanced as PLGA-b-PEG nanoparticles.
    Matched MeSH terms: Piperidines/chemical synthesis; Piperidines/pharmacology*; Piperidines/chemistry
  6. Loh KY, Kew ST
    Med J Malaysia, 2008 Oct;63(4):348-50; quiz 351.
    PMID: 19385504 MyJurnal
    Recent research in bio-medical science has shown an integral role of endocannabinoid system (ECS) in determining cardio-metabolic risk of human body. The mechanism is mediated through binding of endocannabinoids at the CB1 receptors. The stimulation of CB1 receptor in the brain is believed to control and mediate the effects on appetite. In normal physiology, CB1 receptors activation is responsible for energy homeostasis, govern emotions and behaviors such as anxiety, fear, appetite, food and water intake. CB1 receptors also found in peripheral tissues like liver, pancreas, skeletal muscles and adipose tissues, which play an important role in lipid and glucose metabolism. Over-activation of ECS is associated with various metabolic diseases such as dyslipidemia, insulin resistance, lipogenesis, excessive weight gain and increasing intra-abdominal obesity. All these events lead to increased cardiovascular risk. Use of selective CB1 receptor blocker such as rimonabant has shown to reduced waist circumference, better glycemic control, lower triglyceride levels, raise HDL cholesterol and over all reduction in total body fat. This drug has been recommended for patients with metabolic syndrome.
    Matched MeSH terms: Piperidines/therapeutic use
  7. Kwon WK, Sung TY, Yu GY, Sidik H, Kang WS, Lee Y, et al.
    J Anesth, 2016 Apr;30(2):223-31.
    PMID: 26577248 DOI: 10.1007/s00540-015-2094-9
    BACKGROUND: The direct impact of sevoflurane on intraoperative left ventricular (LV) systolic performance during cardiac surgery has not been fully elucidated. Peak systolic tissue Doppler velocities of the lateral mitral annulus (S') have been used to evaluate LV systolic long-axis performance. We hypothesized that incremental sevoflurane concentration (1.0-3.0 inspired-vol%) would dose-dependently reduce S' in patients undergoing cardiac surgery due to mitral or aortic insufficiency.

    METHODS: In 20 patients undergoing cardiac surgery in sevoflurane-remifentanil anesthesia, we analyzed intraoperative S' values which were determined after 10 min exposure to sevoflurane at 1.0, 2.0, and 3.0 inspired-vol% (T1, T2, and T3, respectively) with a fixed remifentanil dose (1.0 μg/kg/min) using transesophageal echocardiography.

    RESULTS: Linear mixed-effect modeling demonstrated dose-dependent declines in S' according to the end-tidal sevoflurane concentration increments (C(ET)-sevoflurane, p < 0.001): the mean value of S' reduction for each 1.0 vol%-increment of C(ET)-sevoflurane was 1.7 cm/s (95 % confidence interval 1.4-2.1 cm/s). Medians of S' at T1, T2, and T3 (9.6, 8.9, and 7.5 cm/s, respectively) also exhibited significant declines (by 6.6, 15.6, and 21.2 % for T1 vs. T2, T2 vs. T3, and T1 vs. T3, p < 0.001, =0.002, and <0.001 in Friedman pairwise comparisons, respectively).

    CONCLUSIONS: Administering sevoflurane as a part of a sevoflurane-remifentanil anesthesia regimen appears to dose-dependently reduce S', indicating LV systolic performance, in patients undergoing cardiac surgery. Further studies may be required to evaluate the clinical implications of these findings.

    Matched MeSH terms: Piperidines/administration & dosage*
  8. Lajis NH, Noor HM, Khan MN
    J Pharm Sci, 1995 Jan;84(1):126-30.
    PMID: 7714735
    The hydroxide ion-catalyzed hydrolysis of securinine involves the ring opening of the lactone moiety. The rate of hydrolysis is insensitive to the ionic strength. The observed pseudo-first-order rate constants reveal a decrease of approximately 4-fold due to the increase in the MeCN content from 4 to 50% (v/v) in mixed aqueous solvent. The temperature dependence of the rate of hydrolysis follows the Eyring equation, which yields delta H* and delta S* as 11.0 kcal mol-1 and -34.5 cal deg-1 mol-1, respectively. The hydroxyl carboxylate product of the alkaline hydrolysis of securinine is shown to undergo cyclization in acidic medium to yield securinine. The observed pseudo-first-order rate constants for cyclization increase linearly with an increase in [H+]. The change in the content of MeCN from 3.8 to 47.2% (v/v) in mixed aqueous solvents does not show an effect on the rate of the cyclization reaction. The most plausible mechanisms for alkaline hydrolysis and acid cyclization reactions are also discussed.
    Matched MeSH terms: Piperidines*
  9. Fagge II, Khalid K, Noh MAM, Yusof NSM, Zain SM, Khan MN
    J Oleo Sci, 2018 Jan 01;67(1):55-66.
    PMID: 29238023 DOI: 10.5650/jos.ess17033
    Behaviors of cationic and nonionic mixed micelles in the form of hexadecyltrimethylammonium bromide (HDABr) and hexadecyltrimethylammonium bromide-Polyethylene glycol hexadecyl ether (C16E20), in the presence of inert salts (NaBr and 3,5-dichlorosodium benzoate), by the use of reaction probe between Pp and ionized PhSH (Pp = piperidine and PhSH = phenyl salicylate), has been reported in this work. The values of RXBr (RXBr denotes ion exchange constants obtained in the presence of micelles of different structural features) or KXBr (KXBr denotes ion exchange constants obtained in the presence of micelles of the same structural features) for 3,5-Cl2C6H3CO2- were almost the same at three different [HDABr]T (0.006, 0.010 and 0.015 M). The average value of RXBr or KXBr determined, in the presence of pure HDABr micelles, using semi empirical kinetic (SEK) method appeared to be almost 2½-fold larger (RXBr or KXBr = 198) than that in the presence of mixed HDABr-C16E20 micelles (RXBr or KXBr = 78). Rheological measurements indicated the existence of wormlike/twisted micelles and vesicle at 0.015 M pure HDABr, various [3,5-Cl2C6H3CO2Na], and 25 and 35℃ whereas there were evidence of only spherical micelles in the presence of mixed HDABr-C16E20 ([HDABr]T = 0.015 M and [C16E20]T = 0.006 M) at both temperatures.
    Matched MeSH terms: Piperidines/chemistry*
  10. Liew KB, Tan YT, Peh KK
    Drug Dev Ind Pharm, 2015 Apr;41(4):583-93.
    PMID: 24495273 DOI: 10.3109/03639045.2014.884130
    Manufacturing process and superdisintegrants used in orally disintegrating tablet (ODT) formulation are often time discussed. However, the effect of suitable filler for ODT formulation is not explored thoroughly.
    Matched MeSH terms: Piperidines/administration & dosage*; Piperidines/adverse effects; Piperidines/analysis; Piperidines/economics
  11. Liew KB, Peh KK, Fung Tan YT
    Pak J Pharm Sci, 2013 Sep;26(5):961-6.
    PMID: 24035953
    An easy, fast and validated RV-HPLC method was invented to quantify donepezil hydrochloride in drug solution and orally disintegrating tablet. The separation was carried out using reversed phase C-18 column (Agilent Eclipse Plus C-18) with UV detection at 268 nm. Method optimization was tested using various composition of organic solvent. The mobile phase comprised of phosphate buffer (0.01M), methanol and acetonitrile (50:30:20, v/v) adjusted to pH 2.7 with phosphoric acid (80%) was found as the optimum mobile phase. The method showed intraday precision and accuracy in the range of 0.24% to -1.83% and -1.83% to 1.99% respectively, while interday precision and accuracy ranged between 1.41% to 1.81% and 0.11% to 1.90% respectively. The standard calibration curve was linear from 0.125 μg/mL to 16 μg/mL, with correlation coefficient of 0.9997±0.00016. The drug solution was stable under room temperature at least for 6 hours. System suitability studies were done. The average plate count was > 2000, tailing factor <1, and capacity factor of 3.30. The retention time was 5.6 min. The HPLC method was used to assay donepezil hydrochloride in tablet and dissolution study of in-house manufactured donepezil orally disintegrating tablet and original Aricept.
    Matched MeSH terms: Piperidines/administration & dosage; Piperidines/analysis*
  12. Anwar A, Azmi KN, Hamidon BB, Khalid BA
    Med J Malaysia, 2006 Mar;61(1):28-35.
    PMID: 16708731 MyJurnal
    This study was conducted to compare the treatment efficacy between a prandial glucose regulator, repaglinide and a new sulphonylurea, glimepiride in Muslim Type 2 diabetic patients who practice Ramadan fasting. Forty-one patients, previously treated with a sulphonylurea or metformin, were divided to receive either repaglinide (n=20, preprandially three-times daily) or glimepiride (n=21, preprandially once daily) 3 months before the month of Ramadan. During Ramadan, patients modified their eating pattern to two meals daily, and the triple doses of repaglinide were redistributed to two preprandial doses. Four point blood glucose monitoring were performed weekly during the month of Ramadan and the subsequent month. Measurements of the 4-point blood glucose were significantly lower in the glimepiride group compared to the repaglinide group both during and after Ramadan. The glycaemic excursion was better in the morning for the repaglinide group and better in the afternoon and evening for the glimepiride group during the Ramadan period. There was no statistically significant difference in the incidence of hypoglycaemia between the two groups during and after Ramadan. There was no difference in the glycaemic excursion post-Ramadan. The longer duration of action of glimepiride may offer an advantage over repaglinide during the 13.5 hours of fast in Ramadan for diabetic patients.
    Matched MeSH terms: Piperidines/pharmacology; Piperidines/therapeutic use*
  13. Shamsi S, Tran H, Tan RS, Tan ZJ, Lim LY
    Drug Metab. Dispos., 2017 01;45(1):49-55.
    PMID: 27821437
    Inhibition of cytochrome P450 (P450) enzymes (CYP) has been shown to lower the metabolism of drugs that are P450 substrates and to consequently alter their pharmacokinetic profiles. Curcumin (CUR), piperine (PIP), and capsaicin (CAP) are spice components (SC) that inhibit the activities of a range of P450 enzymes, but the selection of which SC to be prioritized for further development as an adjuvant will depend on the ranking order of the inhibitory potential of the SCs on specific P450 isozymes. We used common human recombinant enzyme platforms to provide a comparative evaluation of the inhibitory activities of CUR, PIP, and CAP on the principal drug-metabolizing P450 enzymes. SC-mediated inhibition of CYP3A4 was found to rank in the order of CAP (IC501.84 ± 0.71 µM) ∼ PIP (2.12 ± 0.45 µM) > CUR (11.93 ± 3.49 µM), while CYP2C9 inhibition was in the order of CAP (11.95 ± 4.24 µM) ∼ CUR (14.58 ± 4.57 µM) > PIP (89.62 ± 9.17 µM). CAP and PIP were significantly more potent inhibitors of CYP1A2 (IC502.14 ± 0.22 µM and 14.19 ± 4.15 µM, respectively) than CUR (IC50> 100 µM), while all three SCs exhibited weak activity toward CYP2D6 (IC5095.42 ± 12.09 µM for CUR, 99.99 ± 5.88 µM for CAP, and 110.40 ± 3.23 µM for PIP). Of the three SCs, CAP thus has the strongest potential for further development into an inhibitor of multiple CYPs for use in the clinic. Data from this study are also useful for managing potential drug-SC interactions.
    Matched MeSH terms: Piperidines/pharmacology*; Piperidines/chemistry
  14. Mafauzy M
    Diabetes Res Clin Pract, 2002 Oct;58(1):45-53.
    PMID: 12161056 DOI: 10.1016/s0168-8227(02)00104-3
    This study compared treatment with a prandial glucose regulator (repaglinide) and a sulphonylurea (glibenclamide) in Muslim Type 2 diabetic patients who practice Ramadan fasting. Two hundred and thirty-five patients, previously treated with a sulphonylurea, were randomised to receive either repaglinide (n=116, preprandially three-times daily) or glibenclamide (n=119, preprandially once- or twice-daily) 6 weeks before Ramadan. During Ramadan, patients changed their eating pattern to two meals daily, and the daily dose of repaglinide was redistributed to two preprandial doses. After Ramadan, patients resumed their regular meal pattern and treatment dosage for 4 weeks. During Ramadan, a statistically significant reduction in mean serum fructosamine concentration from baseline was observed in the repaglinide group (-16.9+/-4.9 micromol/l, -3.8%, P<0.05) but not the glibenclamide group (-6.9+/-4.8 micromol/l, -0.8%). Difference in change in HbA(1c) from baseline was not statistically significant between groups. The number of hypoglycaemic events with midday blood glucose <4.5 mmol/l was significantly lower in the repaglinide group (2.8%) than the glibenclamide group (7.9%) (P=0.001). Apart from hypoglycaemia, both treatments were equally well tolerated. Type 2 diabetic Muslims using prandial repaglinide showed a trend towards better glycaemic control and had a lower frequency of hypoglycaemia than patients using glibenclamide during Ramadan.
    Matched MeSH terms: Piperidines/adverse effects; Piperidines/therapeutic use*
  15. Liew KB, Tan YT, Peh KK
    Drug Dev Ind Pharm, 2014 Jan;40(1):110-9.
    PMID: 23311593 DOI: 10.3109/03639045.2012.749889
    Difficulty in swallowing tablets or capsules has been identified as one of the contributing factors to non-compliance of geriatric patients. Although orally disintegrating tablet was designed for fast disintegration in mouth, the fear of taking solid tablets and the risk of choking for certain patient populations still exist.
    Matched MeSH terms: Piperidines/administration & dosage*; Piperidines/chemistry
  16. Tan PC, Esa N
    Korean J Anesthesiol, 2012 May;62(5):474-8.
    PMID: 22679546 DOI: 10.4097/kjae.2012.62.5.474
    Anesthetic management of patients with mediastinal masses remains challenging as acute cardiorespiratory decompensation may follow induction of anesthesia. We describe a 57 year old lady with massive retrosternal goiter and severe intrathoracic tracheal compression who had a total thyroidectomy. Comprehensive contingency plans were an essential prerequisite for successful management of difficult airway, including multidisciplinary involvement of otorhinolaryngologic and cardiothoracic surgeons preparing for rigid bronchoscopy and cardiopulmonary bypass. Awake oral fiberoptic intubation was performed under dexmedetomidine sedation. Severe tracheal narrowing necessitated usage of a 5.0 mm uncuffed flexometallic endotracheal tube. Anesthesia was maintained with sevoflurane and dexmedetomidine infusion with target controlled infusion of remifentanil as analgesia. No muscle relaxant was given. Surgical manipulation led to intermittent total tracheal compression and inadequate ventilation. The tumor was successfully removed via the cervical approach. A close working relationship between anesthesiologists and surgeons was the key to the safe use of anesthesia and uneventful recovery of this patient.
    Matched MeSH terms: Piperidines
  17. Mösges R, Lee DL, Abong J, Siasoco B, Chow SK, Leong JL, et al.
    Asia Pac Allergy, 2016 Jan;6(1):56-66.
    PMID: 26844221 DOI: 10.5415/apallergy.2016.6.1.56
    The prevalence of allergic diseases is increasing globally, most particularly in middle- to low-income countries. This article examines the burden of allergic rhinitis and chronic urticaria in the Asia-Pacific region, unmet clinical needs, and the potential role of bilastine in the management of these conditions. An International Advisory Group meeting was convened in association with the Asian Pacific Society of Respirology Annual Congress in November 2014, followed by a literature review, and consensus-based outcomes from the meeting and literature review are described. Regional estimates of the prevalence of allergic rhinitis range from 10% to 50%, while little is known regarding the burden of urticaria in the Asia-Pacific region. A survey of allergy patients in the region identified fast, complete, and long-lasting symptom relief as the medication attributes most important to patients. International treatment guidelines for allergic rhinitis and urticaria advocate the first-line use of second-generation, no-sedating H1-antihistamines, such as bilastine, over their first-generation counterparts and a range of these agents are available to Asia-Pacific patients. The newer agents possess many of the properties of an "ideal" antihistamine (once daily administration, rapid and complete symptom relief, limited potential for drug-drug interactions, minimal side effects). The burgeoning prevalence of allergic diseases in the Asia-Pacific region and the uncontrolled symptoms that these patients experience demand a new antihistamine that offers the highest number of positive features according to the international guidelines.
    Matched MeSH terms: Piperidines
  18. Rao PJ, Kolla SD, Elshaari F, Elshaari F, Awamy HE, Elfrady M, et al.
    Infect Disord Drug Targets, 2015;15(2):131-4.
    PMID: 26205799
    BACKGROUND: Piperine is isolated from Piper nigrum popularly known as black pepper. Previous studies have demonstrated the beneficial effects of piperine in various health conditions. Additionally, it is a powerful bioenhancer for many drugs. Piperine extract is believed to potentiate the effect of drugs by several folds. The present study is focused on its individual effect on liver function.

    MATERIALS AND METHODS: A total of 30 CF-1 albino mice obtained from the animal house of faculty of Medicine, Benghazi University, Benghazi, Libya were included in the study. These mice were fed with high cholesterol diet and divided into 2 groups. Twenty mice were administered piperine at a dose of 5mg/kg body weight. Piperine was isolated in Department of Pharmacognosy, Faculty of Pharmacy, Benghazi University, Benghazi and 10 mice were not administered piperine but fed with high fat diet. These mice were anesthetized with ketamine and halothane and blood was drawn from each mouse before the study and after three weeks by cardiocentesis. Serum transaminases (alanine aminotransferase [ALT] and aspartate aminotransferase [AST]), alkaline phosphatase and total protein were measured by authenticated methods.

    RESULTS: Serum alanine amino transferase was significantly elevated (p=0.0002) in group A mice after the administration of Piperine extract for three weeks compared to those of group B mice. Serum aspartate amino transferase was elevated significantly (p=0.046) and alkaline phosphatase (p= 0.0001) also was significantly increased after the administration of piperine. Serum total protein (p= 0.011) values were significantly decreased after the use of piperine for three weeks in group A mice.

    CONCLUSION: This study showed that there might have been a considerable damage to liver with piperine extract. Further research may be required to prove this damage to liver function.

    Matched MeSH terms: Piperidines/isolation & purification; Piperidines/pharmacology*; Piperidines/toxicity*
  19. Yap HH, Jahangir K, Zairi J
    J Am Mosq Control Assoc, 2000 Sep;16(3):241-4.
    PMID: 11081653
    Four insect repellent products (RPs) (RP 1, Experimental Repellent Lotion [Bayrepel 12%]; RP 2, Experimental Repellent Cream [Bayrepel 5%]; RP 3, Off! Insect Repellent II Aerosol [deet 15%]; and RP 4, Off! Skintastic II Cream [deet 7.5%]) were evaluated simultaneously for their efficacy against vector and nuisance mosquitoes. The aim of this study was to compare the relative efficacy of RPs based on a new repellent compound, Bayrepel (1-piperidinecarboxylic acid, 2-(2-hydroxyethyl)-1-methylpropylester), with deet (N,N-diethyl-m-toluamide)-based RPs. An 8-h field efficacy of above repellents was evaluated against the day-biting mosquito (Aedes albopictus) and night-biting mosquitoes (Culex quinquefasciatus and Anopheles spp.). Evaluation was carried out by exposing humans with repellent-treated bare limbs to mosquitoes landing and to mosquitoes landing and biting. Repellent product 1 or 2 was applied on the left arm and leg, whereas RP 3 or 4 was applied on the right arm and leg, respectively. Application of these 4 RPs significantly reduced (P < 0.05) the landing and the landing and biting of day-biting and night-biting mosquitoes. All 4 RPs were found to be equally effective (P < 0.05) against Ae. albopictus and Cx. quinquefasciatus. However, for protection against Anopheles spp., RPs 1 and 3 exhibited significantly (P < 0.05) better repellency effect than RPs 2 and 4.
    Matched MeSH terms: Piperidines
  20. Chou YH, Hor CC, Lee MT, Lee HJ, Guerrini R, Calo G, et al.
    Addict Biol, 2020 Oct 19.
    PMID: 33078457 DOI: 10.1111/adb.12971
    Neurons containing neuropeptide S (NPS) and orexins are activated during stress. Previously, we reported that orexins released during stress, via orexin OX1 receptors (OX1 Rs), contribute to the reinstatement of cocaine seeking through endocannabinoid/CB1 receptor (CB1 R)-mediated dopaminergic disinhibition in the ventral tegmental area (VTA). Here, we further demonstrated that NPS released during stress is an up-stream activator of this orexin-endocannabinoid cascade in the VTA, leading to the reinstatement of cocaine seeking. Mice were trained to acquire cocaine conditioned place preference (CPP) by context-pairing cocaine injections followed by the extinction training with context-pairing saline injections. Interestingly, the extinguished cocaine CPP in mice was significantly reinstated by intracerebroventricular injection (i.c.v.) of NPS (1 nmol) in a manner prevented by intraperitoneal injection (i.p.) of SHA68 (50 mg/kg), an NPS receptor antagonist. This NPS-induced cocaine reinstatement was prevented by either i.p. or intra-VTA microinjection (i.vta.) of SB-334867 (15 mg/kg, i.p. or 15 nmol, i.vta.) and AM 251 (1.1 mg/kg, i.p. or 30 nmol, i.vta.), antagonists of OX1 Rs and CB1 Rs, respectively. Besides, NPS (1 nmol, i.c.v.) increased the number of c-Fos-containing orexin neurons in the lateral hypothalamus (LH) and increased orexin-A level in the VTA. The latter effect was blocked by SHA68. Furthermore, a 30-min restraint stress in mice reinstated extinguished cocaine CPP and was prevented by SHA68. These results suggest that NPS is released upon stress and subsequently activates LH orexin neurons to release orexins in the VTA. The released orexins then reinstate extinguished cocaine CPP via an OX1 R- and endocannabinoid-CB1 R-mediated signaling in the VTA.
    Matched MeSH terms: Piperidines
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