Displaying publications 321 - 340 of 6929 in total

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  1. Fulltext Pharmacophore modelling of vanillin derivatives, favipiravir, chloroquine, hydroxychloroquine, monolaurin and tetrodotoxin as MPro inhibitors of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2)
    Law WY, Asaruddin MR, Bhawani SA, Mohamad S
    BMC Res Notes, 2020 Nov 11;13(1):527.
    PMID: 33176880 DOI: 10.1186/s13104-020-05379-6
    OBJECTIVES: The aim of this study was to use Ligand-based pharmacophore modelling approach for four established antiviral drugs, namely remdesivir, lopinavir, ritonavir and hydroxychloroquine for COVID-19 inhibitors as training sets. In this study Twenty vanillin derivatives together with monolaurin and tetrodotoxin were used as test sets to evaluate as potential SARS-CoV-2 inhibitors. The Structure-based pharmacophore modelling approach was also performed using 5RE6, 5REX and 5RFZ in order to analyse the binding site and ligand-protein complex interactions.

    RESULTS: The pharmacophore modelling mode of 5RE6 displayed two Hydrogen Bond Acceptors (HBA) and one Hydrophobic (HY) interaction. Besides, the pharmacophore model of 5REX showed two HBA and two HY interactions. Finally, the pharmacophore model of 5RFZ showed three HBA and one HY interaction. Based on ligand-based approach, 20 Schiff-based vanillin derivatives, showed strong MPro inhibition activity. This was due to their good alignment and common features to PDB-5RE6. Similarly, monolaurin and tetrodotoxin displayed some significant activity against SARS-CoV-2. From structure-based approach, vanillin derivatives (1) to (12) displayed some potent MPro inhibition against SARS-CoV-2. Favipiravir, chloroquine and hydroxychloroquine also showed some significant MPro inhibition.

    Matched MeSH terms: Amides/pharmacology; Antiviral Agents/pharmacology*; Chloroquine/pharmacology*; Hydroxychloroquine/pharmacology; Laurates/pharmacology; Pyrazines/pharmacology; Tetrodotoxin/pharmacology; Cysteine Proteinase Inhibitors/pharmacology*; Monoglycerides/pharmacology
  2. Development of anti-acanthamoebic approaches
    Mungroo MR, Tong T, Khan NA, Anuar TS, Maciver SK, Siddiqui R
    Int Microbiol, 2021 Aug;24(3):363-371.
    PMID: 33754231 DOI: 10.1007/s10123-021-00171-3
    Acanthamoeba keratitis is a sight-endangering eye infection, and causative organism Acanthamoeba presents a significant concern to public health, given escalation of contact lens wearers. Contemporary therapy is burdensome, necessitating prompt diagnosis and aggressive treatment. None of the contact lens disinfectants (local and international) can eradicate Acanthamoeba effectively. Using a range of compounds targeting cellulose, ion channels, and biochemical pathways, we employed bioassay-guided testing to determine their anti-amoebic effects. The results indicated that acarbose, indaziflam, terbuthylazine, glimepiride, inositol, vildagliptin and repaglinide showed anti-amoebic effects. Compounds showed minimal toxicity on human cells. Therefore, effects of the evaluated compounds after conjugation with nanoparticles should certainly be the subject of future studies and will likely lead to promising leads for potential applications.
    Matched MeSH terms: Antiprotozoal Agents/pharmacology*; Carbamates/pharmacology; Indenes/pharmacology; Inositol/pharmacology; Piperidines/pharmacology; Sulfonylurea Compounds/pharmacology; Triazines/pharmacology; Contact Lens Solutions/pharmacology; Acarbose/pharmacology
  3. Fulltext Potential role of marine species-derived bioactive agents in the management of SARS-CoV-2 infection
    Asif M, Saleem M, Yaseen HS, Yehya AH, Saadullah M, Zubair HM, et al.
    Future Microbiol, 2021 Nov;16(16):1289-1301.
    PMID: 34689597 DOI: 10.2217/fmb-2021-0024
    COVID-19, caused by the SARS-CoV-2 outbreak, has resulted in a massive global health crisis. Bioactive molecules extracted or synthesized using starting material obtained from marine species, including griffithsin, plitidepsin and fingolimod are in clinical trials to evaluate their anti-SARS-CoV-2 and anti-HIV efficacies. The current review highlights the anti-SARS-CoV-2 potential of marine-derived phytochemicals explored using in silico, in vitro and in vivo models. The current literature suggests that these molecules have the potential to bind with various key drug targets of SARS-CoV-2. In addition, many of these agents have anti-inflammatory and immunomodulatory potentials and thus could play a role in the attenuation of COVID-19 complications. Overall, these agents may play a role in the management of COVID-19, but further preclinical and clinical studies are still required to establish their role in the mitigation of the current viral pandemic.
    Matched MeSH terms: Fingolimod Hydrochloride/pharmacology; Alkaloids/pharmacology; Antiviral Agents/pharmacology*; Peptides, Cyclic/pharmacology; Phycocyanin/pharmacology; Polysaccharides/pharmacology; Sesquiterpenes/pharmacology; Plant Lectins/pharmacology; Polyphenols/pharmacology
  4. Effect of acidosis on the mechanism(s) of insulin-induced vasorelaxation in normal Wistar-Kyoto (WKY) rat aorta
    Subramaniam G, Achike FI, Mustafa MR
    Regul. Pept., 2009 Jun 5;155(1-3):70-5.
    PMID: 19362578 DOI: 10.1016/j.regpep.2009.04.008
    The effect of acidosis on insulin-induced relaxation was studied in thoracic aortic rings (from Wistar-Kyoto (WKY) rats) with (+ED) or without (-ED) endothelium. The rings were mounted in normal (pH 7.4) or acidotic (pH 7.2) Krebs solution for isometric tension recording. Phenylephrine (PE, 3.0 microM)-contracted tissues were exposed to insulin in the presence or absence of various inhibitors. Insulin exerted similar concentration-dependent relaxation of +ED tissues in normal and acidotic pH. Endothelium denudation, significantly (p<0.05) reduced insulin effect in normal, but not acidotic pH. Under normal pH, treatment with L-NAME or methylene blue significantly (p<0.05) reduced insulin responses in the +ED (but not the -ED) tissues. The insulin effect was also significantly (p<0.05) inhibited by tetraethylammonium (TEA; BK(Ca) blocker), 4-Aminopyridine (4-AP; K(V) channel blocker), combined treatments (L-NAME+4-AP+TEA, in +ED tissues) or (4-AP+TEA, in -ED tissues). In either +ED or -ED tissues, indomethacin (cyclo-oxygenase inhibitor), glibenclamide (K(ATP) channel blocker), barium chloride (K(ir) channel blocker) or Ouabain (a Na(+)/K(+)-ATPase inhibitor) had no effect. Except for methylene blue (effect on +ED tissues), none of the drug treatments inhibited insulin vasodilator effect in acidosis (+ED or -ED tissues). These data indicate that insulin exerts an endothelium-dependent and -independent vasodilatation in rat aorta which in normal pH is mediated via BK(Ca) and K(v) channels, including the EDNO-cGMP cascade. Acidosis abolishes the endothelium-dependent relaxation mechanism unraveling a novel mechanism that is as efficacious and is cGMP-, but not EDNO-, BK(Ca)- or K(v)-mediated.
    Matched MeSH terms: Chlorides/pharmacology; Glyburide/pharmacology; Hypoglycemic Agents/pharmacology*; Indomethacin/pharmacology; Insulin/pharmacology*; Methylene Blue/pharmacology; Ouabain/pharmacology; Phenylephrine/pharmacology; 4-Aminopyridine/pharmacology; Barium Compounds/pharmacology; NG-Nitroarginine Methyl Ester/pharmacology; Tetraethylammonium/pharmacology; Potassium Channel Blockers/pharmacology
  5. Biologically active vallesamine, strychnan, and rhazinilam alkaloids from Alstonia: Pneumatophorine, a nor-secovallesamine with unusual incorporation of a 3-ethylpyridine moiety
    Lim JL, Sim KS, Yong KT, Loong BJ, Ting KN, Lim SH, et al.
    Phytochemistry, 2015 Sep;117:317-24.
    PMID: 26125941 DOI: 10.1016/j.phytochem.2015.06.024
    Four alkaloids comprising two vallesamine, one strychnan, and one pyranopyridine alkaloid, in addition to 32 other known alkaloids were isolated from two Malayan Alstonia species, Alstonia pneumatophora and Alstonia rostrata. The structures of these alkaloids were determined using NMR and MS analyses, and in one instance, confirmed by X-ray diffraction analysis. The nor-6,7-secovallesamine alkaloid, pneumatophorine, is notable for an unusual incorporation of a 3-ethylpyridine moiety in a monoterpenoid indole. The rhazinilam-type alkaloids (rhazinicine, nor-rhazinicine, rhazinal, and rhazinilam) showed strong cytotoxicity toward human KB, HCT-116, MDA-MB-231, and MRC-5 cells, while pneumatophorine, the uleine alkaloid undulifoline, and the strychnan alkaloids, N4-demethylalstogustine and echitamidine, induced concentration dependent relaxation in phenylephrine-precontracted rat aortic rings.
    Matched MeSH terms: Aldehydes/pharmacology; Alkaloids/pharmacology*; Antineoplastic Agents, Phytogenic/pharmacology; Carbazoles/pharmacology; Heterocyclic Compounds with 4 or More Rings/pharmacology; Indolizines/pharmacology; Lactams/pharmacology; Phenylephrine/pharmacology; Pyrans/pharmacology; Pyridines/pharmacology; Vasodilator Agents/pharmacology; Indole Alkaloids/pharmacology; Secologanin Tryptamine Alkaloids/pharmacology
  6. The effect of Centella asiatica, vitamins, glycolic acid and their mixtures preparations in stimulating collagen and fibronectin synthesis in cultured human skin fibroblast
    Hashim P
    Pak J Pharm Sci, 2014 Mar;27(2):233-7.
    PMID: 24577907
    Centella asiatica (Linn.) Urban is well known in promoting wound healing and provides significant benefits in skin care and therapeutic products formulation. Glycolic acid and vitamins also play a role in the enhancement of collagen and fibronectin synthesis. Here, we evaluate the specific effect of Centella asiatica (CA), vitamins, glycolic acid and their mixture preparations to stimulate collagen and fibronectin synthesis in cultured human fibroblast cells. The fibroblast cells are incubated with CA, glycolic acid, vitamins and their mixture preparations for 48 h. The cell lysates were analyzed for protein content and collagen synthesis by direct binding enzyme immunoassay. The fibronectin of the cultured supernatant was measured by sandwich enzyme immunoassay. The results showed that CA, glycolic acid, vitamins A, E and C significantly stimulate collagen and fibronectin synthesis in the fibroblast. Addition of glycolic acid and vitamins to CA further increased the levels of collagen and fibronectin synthesis to 8.55 and 23.75 μg/100 μg, respectively. CA, glycolic acid, vitamins A, E, and C, and their mixtures demonstrated stimulatory effect on both extra-cellular matrix synthesis of collagen and fibronectin in in vitro studies on human foreskin fibroblasts, which is beneficial to skin care and therapeutic products formulation.
    Matched MeSH terms: Ascorbic Acid/pharmacology; Glycolates/pharmacology*; Plant Extracts/pharmacology*; Vitamin A/pharmacology; Vitamin E/pharmacology; Vitamins/pharmacology*
  7. Isolation and identification of radical scavenging and tyrosinase inhibition of polyphenols from Tibouchina semidecandra L
    Sirat HM, Rezali MF, Ujang Z
    J Agric Food Chem, 2010 Oct 13;58(19):10404-9.
    PMID: 20809630 DOI: 10.1021/jf102231h
    Phytochemical and bioactivity studies of the leaves and stem barks of Tibouchina semidecandra L. have been carried out. The ethyl acetate extract of the leaves yielded four flavonoid compounds, identified as quercetin, quercetin 3-O-α-l-(2''-O-acetyl) arabinofuranoside, avicularin, and quercitrin, while the stem barks gave one ellagitannin, identified as 3,3'-O-dimethyl ellagic acid 4-O-α-l-rhamnopyranoside. Evaluation of the antioxidative activity on the crude extracts and pure compounds by electron spin resonance (ESR) and ultraviolet-visible (UV-vis) spectrophotometric assays showed that the pure isolated polyphenols and the EtOAc extract possessed strong antioxidative capabilities. Quercetin was found to be the most active radical scavenger in DPPH-UV and ESR methods with SC(50) values of 0.7 μM ± 1.4 and 0.7 μM ± 0.6 μM, respectively, in the antioxidant assay. A combination of quercetin and quercitrin was tested for synergistic antioxidative capacity;, however, there was no significant improvement observed. Quercetin also exhibited strong antityrosinase activity with a percent inhibition of 95.0% equivalent to the positive control, kojic acid, in the tyrosinase inhibition assay.
    Matched MeSH terms: Antioxidants/pharmacology; Enzyme Inhibitors/pharmacology*; Flavonoids/pharmacology*; Phenols/pharmacology*; Quercetin/pharmacology; Free Radical Scavengers/pharmacology*
  8. The effect of nitric oxide on the production of prostaglandin E2 by hydroxyapatite-stimulated a human osteoblast (HOS) cell line
    Sugiatno E, Samsudin AR, Ibrahim MF, Sosroseno W
    Biomed Pharmacother, 2006 May;60(4):147-51.
    PMID: 16581222
    The aim of the present study was to determine the effect of nitric oxide (NO) on the production of prostaglandin E2 (PGE2) by a human osteoblast cell line (HOS cells) stimulated with hydroxyapatite. Cells were cultured on the HA surfaces with or without the presence of NO donors (SNAP and NAP) for 3 days. The effect of NO scavenger, carboxy PTIO, or endothelial nitric oxide synthase (eNOS) inhibitor, L-NIO, was assessed by adding this scavenger in the cultures of HA-stimulated HOS cells with or without the presence of SNAP. Furthermore, HOS cells were pre-treated with anti-human integrin alphaV antibody, indomethacin, a non-specific inhibitor, aspirin, a COX-1 inhibitor, or nimesulide, a COX-2 inhibitor, prior to culturing on HA surfaces with or without the presence of SNAP. The levels of PGE2 were determined from the 3 day culture supernatants. The results showed that the production of PGE2 by HA-stimulated HOS cells was augmented by SNAP. Carboxy PTIO suppressed but L-NIO only partially inhibited the production of PGE2 by HA-stimulated HOS cells with or without the presence of exogenous NO. Pre-treatment of the cells with anti-human integrin alphaV antibody, indomethacin or nimesulide but not aspirin suppressed the production of PGE2 by HA-stimulated HOS cells with or without the presence of NO. Therefore, the results of the present study suggest that NO may up-regulate the production of PGE2 by augmenting the COX-2 pathway initiated by the binding between HOS cell-derived integrin alphaV and HA surface.
    Matched MeSH terms: Enzyme Inhibitors/pharmacology; Nitric Oxide/pharmacology*; Ornithine/pharmacology; Durapatite/pharmacology*; Nitric Oxide Donors/pharmacology; S-Nitroso-N-Acetylpenicillamine/pharmacology
  9. Plasmid profiling and curing of Lactobacillus strains isolated from the gastrointestinal tract of chicken
    Chin SC, Abdullah N, Siang TW, Wan HY
    J Microbiol, 2005 Jun;43(3):251-6.
    PMID: 15995642
    In this study, we assessed the susceptibility of 12 Lactobacillus strains, all of which had been isolated from the gastrointestinal tracts of chicken, to three antibiotics (chloramphenicol, erythromycin and tetracycline) used commonly as selective markers in transformation studies of lactic acid bacteria. Among these strains, 17%, 58%, and 25% were found to exhibit a high degree of resistance to 200 microg/ml of tetracycline, erythromycin, and chloramphenicol, respectively. Seven of the 12 Lactobacillus strains exhibiting resistance to at least 50 microg/ml of chloramphenicol or erythromycin, and five strains exhibiting resistance to at least 50 microg/ml of tetracycline, were subsequently subjected to plasmid curing with chemical curing agents, such as novobiocin, acriflavin, SDS, and ethidium bromide. In no cases did the antibiotic resistance of these strains prove to be curable, with the exception of the erythromycin resistance exhibited by five Lactobacillus strains (L. acidophilus I16 and I26, L. fermentum I24 and C17, and L. brevis C10). Analysis of the plasmid profiles of these five cured derivatives revealed that all of the derivatives, except for L. acidophilus I16, possessed profiles similar to those of wild-type strains. The curing of L. acidophilus I16 was accompanied by the loss of 4.4 kb, 6.1 kb, and 11.5 kb plasmids.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology; Chloramphenicol/pharmacology; Erythromycin/pharmacology; Ethidium/pharmacology; Sodium Dodecyl Sulfate/pharmacology; Tetracycline/pharmacology
  10. Randomized double-blind comparison of ketamine-propofol, fentanyl-propofol and propofol-saline on haemodynamics and laryngeal mask airway insertion conditions
    Goh PK, Chiu CL, Wang CY, Chan YK, Loo PL
    Anaesth Intensive Care, 2005 Apr;33(2):223-8.
    PMID: 15960405
    The aim of this prospective, double-blind, randomized, placebo-controlled clinical trial was to investigate whether the administration of ketamine before induction with propofol improves its associated haemodynamic profile and laryngeal mask airway (LMA) insertion conditions. Ninety adult patients were randomly allocated to receive either ketamine 0.5 mg x kg(-1) (n = 30), fentanyl 1 microg x kg(-1) (n = 30) or normal saline (n = 30), before induction of anaesthesia with propofol 2.5 mg x kg(-1). Insertion of the LMA was performed 60s after injection of propofol. Arterial blood pressure and heart rate were measured before induction (baseline), immediately after induction, immediately before LMA insertion, immediately after LMA insertion and every minute for three minutes after LMA insertion. Following LMA insertion, the following six subjective endpoints were graded by a blinded anaesthestist using ordinal scales graded 1 to 3: mouth opening, gagging, swallowing, movement, laryngospasm and ease of insertion. Systolic blood pressure was significantly higher following ketamine than either fentanyl (P = 0.010) or saline (P = 0.0001). The median (interquartile range) summed score describing the overall insertion conditions were similar in the ketamine [median 7.0, interquartile range (6.0-8.0)] and fentanyl groups [median 7.0, interquartile range (6.0-8.0)]. Both appeared significantly better than the saline group [median 8.0, interquartile range (6.75-9.25); P = 0.024]. The incidence of prolonged apnoea (> 120s) was higher in the fentanyl group [23.1% (7/30)] compared with the ketamine [6.3% (2/30)] and saline groups [3.3% (1/30)]. We conclude that the addition of ketamine 0.5 mg x kg(-1) improves haemodynamics when compared to fentanyl 1 microg x kg(-1), with less prolonged apnoea, and is associated with better LMA insertion conditions than placebo (saline).
    Matched MeSH terms: Adjuvants, Anesthesia/pharmacology*; Anesthetics, Dissociative/pharmacology*; Fentanyl/pharmacology*; Ketamine/pharmacology*; Propofol/pharmacology*; Anesthetics, Intravenous/pharmacology*
  11. A Review of Bisindolylmethane as an Important Scaffold for Drug Discovery
    Imran S, Taha M, Ismail NH
    Curr Med Chem, 2015;22(38):4412-33.
    PMID: 26438249
    Bisindolylmethane and its derivatives are pharmacologically active and applicable in the field of pharmaceutical chemistry. Bisindolylmethanes have a variety of biological activities such as antihyperglycemic, antiinflammatory, antibacterial, anticancer, and antileishmanial activities, including enzyme inhibition activity. They play a crucial role in many diseases especially anticancer activity. Modifying their structure had proven to be useful in the search of new therapeutic agents. Extensive research carried out on bisindolylmethane and its derivatives shows that they are pharmacologically significant. The present review focuses on the pharmacological profile of bisindolylmethane derivatives. This review includes the current literature with an update of research findings as well as the perspectives that they hold for future research.
    Matched MeSH terms: Anti-Inflammatory Agents, Non-Steroidal/pharmacology; Anti-Bacterial Agents/pharmacology; Antiprotozoal Agents/pharmacology; Enzyme Inhibitors/pharmacology; Hypoglycemic Agents/pharmacology; Indoles/pharmacology
  12. Fulltext Nerolidol: A Sesquiterpene Alcohol with Multi-Faceted Pharmacological and Biological Activities
    Chan WK, Tan LT, Chan KG, Lee LH, Goh BH
    Molecules, 2016 Apr 28;21(5).
    PMID: 27136520 DOI: 10.3390/molecules21050529
    Nerolidol (3,7,11-trimethyl-1,6,10-dodecatrien-3-ol) is a naturally occurring sesquiterpene alcohol that is present in various plants with a floral odor. It is synthesized as an intermediate in the production of (3E)-4,8-dimethy-1,3,7-nonatriene (DMNT), a herbivore-induced volatile that protects plants from herbivore damage. Chemically, nerolidol exists in two geometric isomers, a trans and a cis form. The usage of nerolidol is widespread across different industries. It has been widely used in cosmetics (e.g., shampoos and perfumes) and in non-cosmetic products (e.g., detergents and cleansers). In fact, U.S. Food and Drug Administration (FDA) has also permitted the use of nerolidol as a food flavoring agent. The fact that nerolidol is a common ingredient in many products has attracted researchers to explore more medicinal properties of nerolidol that may exert beneficial effect on human health. Therefore, the aim of this review is to compile and consolidate the data on the various pharmacological and biological activities displayed by nerolidol. Furthermore, this review also includes pharmacokinetic and toxicological studies of nerolidol. In summary, the various pharmacological and biological activities demonstrated in this review highlight the prospects of nerolidol as a promising chemical or drug candidate in the field of agriculture and medicine.
    Matched MeSH terms: Antioxidants/pharmacology; Cosmetics/pharmacology; Detergents/pharmacology; Flavoring Agents/pharmacology; Oils, Volatile/pharmacology; Sesquiterpenes/pharmacology*
  13. New insight into the structural, electrochemical and biological aspects of macroacyclic Cu(II) complexes derived from S-substituted dithiocarbazate schiff bases
    Low ML, Maigre L, Tahir MI, Tiekink ER, Dorlet P, Guillot R, et al.
    Eur J Med Chem, 2016 Sep 14;120:1-12.
    PMID: 27183379 DOI: 10.1016/j.ejmech.2016.04.027
    Copper (II) complexes synthesized from the products of condensation of S-methyl- and S-benzyldithiocarbazate with 2,5-hexanedione (SMHDH2 and SBHDH2 respectively) have been characterized using various physicochemical (elemental analysis, molar conductivity, magnetic susceptibility) and spectroscopic (infrared, electronic) methods. The structures of SMHDH2, its copper (II) complex, CuSMHD, and the related CuSBHD complex as well as a pyrrole byproduct, SBPY, have been determined by single crystal X-ray diffraction. In order to provide more insight into the behaviour of the complexes in solution, electron paramagnetic resonance (EPR) and electrochemical experiments were performed. Antibacterial activity and cytotoxicity were evaluated. The compounds, dissolved in 0.5% and 5% DMSO, showed a wide range of antibacterial activity against 10 strains of Gram-positive and Gram-negative bacteria. Investigations of the effects of efflux pumps and membrane penetration on antibacterial activity are reported herein. Antiproliferation activity was observed to be enhanced by complexation with copper. Preliminary screening showed Cu complexes are strongly active against human breast adenocarcinoma cancer cell lines MDA-MB-231 and MCF-7.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology; Copper/pharmacology*; Hydrazines/pharmacology; Schiff Bases/pharmacology; Macrocyclic Compounds/pharmacology*; Coordination Complexes/pharmacology
  14. Interaction between oxytocin and 'sidaverin' on the gravid and non-gravid rat uterus
    Lutterodt GD
    Pharmacol Res, 1995 Jul-Aug;32(1-2):89-94.
    PMID: 8668653 DOI: 10.1016/S1043-6618(95)80014-X
    Sidaverin, a crystalline compound extracted from a polar fraction of Sida veronicaefolia (Lam), elicited oxytocin-like contractions in the non-gravid rat isolated uterus preparation with a concentration-response relationship. Equipotent concentrations of oxytocin and sidaverin, using matched responses, were approximately 0.16 U and 0.4 micrograms ml-1, respectively. Sidaverin-induced contractile response was atropine reversible. The concentration-response curves for sidaverin and oxytocin were parallel, and both responses were inhibited by the specific oxytocin antagonist, Atosiban, indicating possible involvement of oxytocin receptors in the action of sidaverin. There were potentiation of action of one drug to that of the other, irrespective of the order of administration and even after washing off the first before introducing the second drug. In the gravid uterus, sidaverin produced contractions in preparations from day 1 to day 6 or 7, caused relaxation in days 7-11, and elicited contractions in day 11 through term, the sensitivity of the preparations increasing exponentially toward term with strong sustained contractions. With the exception of days 7-11, when sidaverin antagonized oxytocin action, it potentiated action of oxytocin on the gravid uterus.
    Matched MeSH terms: Acetylcholine/pharmacology; Atropine/pharmacology; Oxytocin/pharmacology*; Plant Extracts/pharmacology*; Vasotocin/pharmacology; Muscarinic Antagonists/pharmacology
  15. The effect of losartan and carvedilol on renal haemodynamics and altered metabolism in fructose-fed Sprague-Dawley rats
    Abdulla MH, Sattar MA, Abdullah NA, Johns EJ
    J Physiol Biochem, 2012 Sep;68(3):353-63.
    PMID: 22281695 DOI: 10.1007/s13105-012-0147-1
    The aim of this study is to assess the effects of losartan and carvedilol on metabolic parameters and renal haemodynamic responses to angiotensin II (Ang II) and adrenergic agonists in the model of fructose-fed rat. Thirty-six Sprague-Dawley rats were fed for 8 weeks either 20% fructose solution (F) or tap water (C) ad libitum. F or C group received either losartan or carvedilol (10 mg/kg p.o.) daily for the last 3 weeks of the study (FL and L) and (FCV and CV), respectively, then in acute studies the renal vasoconstrictor actions of Ang II, noradrenaline (NA), phenylephrine (PE) and methoxamine (ME) were determined. Data, mean±SEM were analysed using ANOVA with significance at P <0.05. Losartan and carvedilol decreased the area under the glucose tolerance curve of the fructose-fed group. The responses (%) to NA, PE, ME and Ang II in F were lower (P <0.05) than C (F vs. C, 17±2 vs. 38±3; 24±2 vs. 48±2; 12±2 vs. 34±2; 17±2 vs. 26±2), respectively. L had higher (P <0.05) responses to NA and PE while CV had blunted (P <0.05) responses to NA, PE and Ang II compared to C (L, CV vs. C, 47±3, 9±2 vs. 38±3; 61±3, 29±3 vs. 48±2; 16±3, 4±3 vs. 26±2), respectively. FL but not FCV group had enhanced (P <0.05) responses to NA, PE and ME compared to F (FL vs. F, 33±3 vs. 17±2; 45±3 vs. 24±2; 26±3 vs. 12±2), respectively. Losartan and carvedilol had an important ameliorating effect on fructose-induced insulin resistance. Losartan treatment could be an effective tool to restore normal vascular reactivity in the renal circulation of the fructose-fed rat.
    Matched MeSH terms: Carbazoles/pharmacology*; Norepinephrine/pharmacology*; Phenylephrine/pharmacology; Propanolamines/pharmacology*; Vasoconstrictor Agents/pharmacology; Losartan/pharmacology*
  16. Fulltext Phytochemistry, Traditional Use and Pharmacological Activity of Picrasma quassioides: A Critical Reviews
    Mohd Jamil MDH, Taher M, Susanti D, Rahman MA, Zakaria ZA
    Nutrients, 2020 Aug 26;12(9).
    PMID: 32858812 DOI: 10.3390/nu12092584
    Picrasma quassioides is a member of the Simaroubaceae family commonly grown in the regions of Asia, the Himalayas, and India and has been used as a traditional herbal medicine to treat various illnesses such as fever, gastric discomfort, and pediculosis. This study aims to critically review the presence of phytochemicals in P. quassioides and correlate their pharmacological activities with the significance of its use as traditional medicine. Data were collected by reviewing numerous scientific articles from several journal databases on the pharmacological activities of P. quassioides using certain keywords. As a result, approximately 94 phytochemicals extracted from P. quassioides were found to be associated with quassinoids, β-carbolines and canthinones. These molecules exhibited various pharmacological benefits such as anti-inflammatory, antioxidant, anti-cancer, anti-microbial, and anti-parasitic activities which help to treat different diseases. However, P. quassioides were also found to have several toxicity effects in high doses, although the evidence regarding these effects is limited in proving its safe use and efficacy as herbal medicine. Accordingly, while it can be concluded that P. quassioides may have many potential pharmacological benefits with more phytochemistry discoveries, further research is required to determine its real value in terms of quality, safety, and efficacy of use.
    Matched MeSH terms: Anti-Inflammatory Agents/pharmacology; Antimalarials/pharmacology; Antineoplastic Agents/pharmacology; Antioxidants/pharmacology; Plant Extracts/pharmacology*; Phytochemicals/pharmacology*
  17. Fulltext Antidiabetic Drugs and Their Nanoconjugates Repurposed as Novel Antimicrobial Agents against Acanthamoeba castellanii
    Anwar A, Siddiqui R, Raza Shah M, Khan NA
    J Microbiol Biotechnol, 2019 May 28;29(5):713-720.
    PMID: 31030451 DOI: 10.4014/jmb/1903.03009
    Acanthamoeba castellanii belonging to the T4 genotype may cause a fatal brain infection known as granulomatous amoebic encephalitis, and the vision-threatening eye infection Acanthamoeba keratitis. The aim of this study was to evaluate the antiamoebic effects of three clinically available antidiabetic drugs, Glimepiride, Vildagliptin and Repaglinide, against A. castellanii belonging to the T4 genotype. Furthermore, we attempted to conjugate these drugs with silver nanoparticles (AgNPs) to enhance their antiamoebic effects. Amoebicidal, encystation, excystation, and host cell cytotoxicity assays were performed to unravel any antiacanthamoebic effects. Vildagliptin conjugated silver nanoparticles (Vgt-AgNPs) characterized by spectroscopic techniques and atomic force microscopy were synthesized. All three drugs showed antiamoebic effects against A. castellanii and significantly blocked the encystation. These drugs also showed significant cysticidal effects and reduced host cell cytotoxicity caused by A. castellanii. Moreover, Vildagliptin-coated silver nanoparticles were successfully synthesized and are shown to enhance its antiacanthamoebic potency at significantly reduced concentration. The repurposed application of the tested antidiabetic drugs and their nanoparticles against free-living amoeba such as Acanthamoeba castellanii described here is a novel outcome that holds tremendous potential for future applications against devastating infection.
    Matched MeSH terms: Amebicides/pharmacology*; Anti-Infective Agents/pharmacology*; Carbamates/pharmacology; Hypoglycemic Agents/pharmacology*; Piperidines/pharmacology; Sulfonylurea Compounds/pharmacology
  18. Fulltext Antioxidant, Anti-Inflammatory, and Inhibition of Acetylcholinesterase Potentials of Cassia timoriensis DC. Flowers
    Alhawarri MB, Dianita R, Razak KNA, Mohamad S, Nogawa T, Wahab HA
    Molecules, 2021 Apr 29;26(9).
    PMID: 33946788 DOI: 10.3390/molecules26092594
    Despite being widely used traditionally as a general tonic, especially in South East Asia, scientific research on Cassia timoriensis, remains scarce. In this study, the aim was to evaluate the in vitro activities for acetylcholinesterase (AChE) inhibitory potential, radical scavenging ability, and the anti-inflammatory properties of different extracts of C. timoriensis flowers using Ellman's assay, a DPPH assay, and an albumin denaturation assay, respectively. With the exception of the acetylcholinesterase activity, to the best of our knowledge, these activities were reported for the first time for C. timoriensis flowers. The phytochemical analysis confirmed the existence of tannins, flavonoids, saponins, terpenoids, and steroids in the C. timoriensis flower extracts. The ethyl acetate extract possessed the highest phenolic and flavonoid contents (527.43 ± 5.83 mg GAE/g DW and 851.83 ± 10.08 mg QE/g DW, respectively) as compared to the other extracts. In addition, the ethyl acetate and methanol extracts exhibited the highest antioxidant (IC50 20.12 ± 0.12 and 34.48 ± 0.07 µg/mL, respectively), anti-inflammatory (92.50 ± 1.38 and 92.22 ± 1.09, respectively), and anti-AChE (IC50 6.91 ± 0.38 and 6.40 ± 0.27 µg/mL, respectively) activities. These results suggest that ethyl acetate and methanol extracts may contain bioactive compounds that can control neurodegenerative disorders, including Alzheimer's disease, through high antioxidant, anti-inflammatory, and anti-AChE activities.
    Matched MeSH terms: Anti-Inflammatory Agents/pharmacology*; Antioxidants/pharmacology*; Cholinesterase Inhibitors/pharmacology*; Plant Extracts/pharmacology; Free Radical Scavengers/pharmacology; Phytochemicals/pharmacology
  19. Synthesis, molecular docking and anti-diabetic studies of novel benzimidazole-pyrazoline hybrid molecules
    Ibraheem F, Ahmad M, Ashfaq UA, Aslam S, Khan ZA, Sultan S
    Pak J Pharm Sci, 2020 Mar;33(2(Supplementary)):847-854.
    PMID: 32863261
    Pyrazoline and benzimidazoles derivatives have been widely studied due to their potential applications in the medicinal field. In this research project, we have hybridized these two heterocyclic systems in the same molecule. A new series of compounds, 2-((3,5-diaryl-4,5-dihydro-1H-pyrazol-1-yl)methyl)-1H-benzo[d]imidazole (5a-i) were synthesized through a multistep reaction. In the first step, chalcones 3a-i were prepared by coupling of various acetophenones and benzaldehydes under alkaline conditions. These chalcones were cyclized with hydrazine hydrate to form a series of pyrazolines which were finally coupled with 2-chloromethyl-1H-benzimidazole to get a new series of titled hybrid molecules. The structures of these compounds were elucidated by spectral (1H NMR and 13C NMR) analysis. The anti-diabetic potential of these compounds was studied by screening them for their α-glucosidase inhibition activity. The SAR was established through molecular docking analysis. Compound 5d appeared as effective inhibitor with IC50 = 50.06μM as compared to reference drug (acarbose) having IC50 = 58.8μM.
    Matched MeSH terms: Benzaldehydes/pharmacology; Benzimidazoles/pharmacology*; Hydrazines/pharmacology; Hypoglycemic Agents/pharmacology*; Pyrazoles/pharmacology*; Chalcones/pharmacology
  20. Fulltext Current insecticide susceptibility status of Malaysian Anopheles maculatus Theobald to malathion, permethrin, DDT and deltamethrin
    Rohani A, Aziz I, Zurainee MN, Rohana SH, Zamree I, Lee HL
    Trop Biomed, 2014 Mar;31(1):159-65.
    PMID: 24862056 MyJurnal
    Chemical insecticides are still considered as important control agents for malaria vector control. However, prolonged use of these chemicals may select mosquito vectors for resistance. In this study, susceptibility status of adult Anopheles maculatus collected from 9 localities in peninsular Malaysia, viz., Jeli, Temerloh, Pos Banun, Senderut, Jeram Kedah, Segamat, Kota Tinggi, Kluang and Pos Lenjang were determined using the standard WHO bioassay method in which the adult mosquitoes were exposed to standard insecticide impregnated papers malathion, permethrin, DDT and deltamethrin--at pre-determined diagnostic dosage. Deltamethrin was most effective insecticide among the four insecticides tested, with the LT50 of 29.53 min, compared to malathion (31.67 min), DDT (47.76 min) and permethrin (48.01 min). The effect of all insecticides on the laboratory strain was greater (with all insecticides demonstrated LT50 < 1 hour) than the field strains (deltamethrin 32.7, malathion 53.0, permethrin 62.0, DDT 67.4 min). An. maculatus exhibited low degree of resistance to all test insecticides, indicating that these chemical insecticides are still effective in the control of malaria vector.
    Matched MeSH terms: DDT/pharmacology; Insecticides/pharmacology*; Malathion/pharmacology; Nitriles/pharmacology; Pyrethrins/pharmacology; Permethrin/pharmacology
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