Displaying publications 61 - 80 of 831 in total

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  1. Rehman A, Rahman AR, Rasool AH, Naing NN
    Int J Clin Pharmacol Ther, 2001 Oct;39(10):423-30.
    PMID: 11680667
    To examine the dose response relationship between Ang II and pulse wave velocity (an index of arterial stiffness) in healthy human volunteers.
    Matched MeSH terms: Dose-Response Relationship, Drug
  2. Samud AM, Asmawi MZ, Sharma JN, Yusof AP
    Immunopharmacology, 1999 Sep;43(2-3):311-6.
    PMID: 10596868
    Crinum asiaticum Linn plant is used in Malaysia as a rheumatic remedy and to relieve local pain. In the present study, we examined the anti-inflammatory effects of this plant extract on carrageenan-induced hind paw oedema in mice. C. asiaticum was serially extracted with petroleum ether, followed by chloroform and lastly, methanol. The chloroform and methanol extracts of the plant given orally (50 mg kg-1) caused significant (p < 0.05; n = 7) reduction in paw oedema but the petroleum ether extract did not induce significant effect (p > 0.05) on paw oedema. The methanol extract was then dissolved in water and extracted consecutively with chloroform, ethyl acetate and butanol. The chloroform fraction of methanol extract (CFME) treatment (50 mg kg(-1)) significantly reduced (p < 0.05; n = 7) the acute paw oedema. This may indicate that active anti-inflammatory compounds are present in the CFME. In an attempt to study the mechanism of action of its anti-inflammatory activity, the effects of CFME on BK- and histamine-induced contractions were investigated in isolated rat uterus and guinea-pig ileum preparations, respectively. It was found that CFME caused dose-dependent reduction (p < 0.05; n = 6) of the contractile response induced by BK and shifted the log dose-response curve of histamine to the right. The present findings suggest that C. asiaticum possessed an anti-inflammatory activity as suggested by its use in traditional medicine. The anti-inflammatory activity of this plant could not have been due to its anti-bradykinin activities as CFME non-specifically inhibited BK-induced contraction. It also suggest that CFME may contain compound(s) with anti-histaminic properties. The significance of these findings is discussed.
    Matched MeSH terms: Dose-Response Relationship, Drug
  3. Gan GG, Teh A, Goh KY, Chong HT, Pang KW
    Int J Hematol, 2003 Jul;78(1):84-6.
    PMID: 12894858
    Warfarin is a drug commonly used in the prevention of thromboembolic events. There have been reports suggesting that racial background may influence warfarin dose requirements. Malaysia is a multiracial country in which there are 3 major races, Malay, Chinese, and Indian. We examined 100 patients from our hospital on stable maintenance doses of warfarin, with international normalized ratio (INR) of 2.0 to 3.5. We found that the mean warfarin dose for Indian patients (n = 19) was 6.9 mg, for Chinese patients (n = 55) was 3.6 mg, and for Malay patients (n = 26) was 3.2 mg. The results showed that the Indian patients required a statistically significantly higher warfarin dose than did patients of the other 2 races (P < .0005). Age was also found to affect the daily warfarin maintenance dose.
    Matched MeSH terms: Dose-Response Relationship, Drug
  4. Lutterodt GD
    J Ethnopharmacol, 1992 Sep;37(2):151-7.
    PMID: 1434689
    Measurement of rates of propulsion in the small intestine in control and experimental groups of male Sprague-Dawley rats (200-250 g) were carried out as a means of assessing antidiarrhoeal activity of aqueous extracts of the leaf of Psidium guajava (L.), using morphine as the standard drug of reference. Hyperpropulsion (diarrhoea) was induced by gavaging rats in a control group with Microlax, using phenol red mixed into it as a marker in the intestine, and the mean rate of the hyperpropulsion was determined. The normal rate of propulsion, defined as the percentage of the length of the ileum traversed by the front of the dye in 1 h after gavaging animals with a liquid paraffin-phenol red meal, was also determined in another control group. In experimental groups pretreated with enteral administration of either morphine or aqueous extracts, 1 h before the challenge with Microlax, the percentage inhibition to the hyperpropulsive rate (antidiarrhoeal activity) was calculated. Both morphine and the extracts produced a dose-response relationship in their antidiarrhoeal effects. A dose of 0.2 ml/kg fresh leaf extract produced 65% inhibition of propulsion. This dose is equiactive with 0.2 mg/kg of morphine sulphate. The antidiarrhoeal action of the extract may be due, in part, to the inhibition of the increased watery secretions that occur commonly in all acute diarrhoeal diseases and cholera.
    Matched MeSH terms: Dose-Response Relationship, Drug
  5. Lee HL, Abimbola O, Singh KI
    PMID: 1488701
    Rapid enzyme microassays for the detection of resistance due to organophosphate and carbamate in individual field-collected strains of Culex quinquefasciatus adults were conducted. These tests allowed accurate differentiation by eye, on the basis of color changes of susceptible and resistant individuals. Two separate tests were conducted for the biochemical assays. In the insensitive acetylcholinesterase (AChE) test, acetylthiocholine iodide (ACTH) and 5,5-dithiobis-(2-nitrobenzoic acid) (DTNB) were used as substrate and coupling agent respectively. The resulting yellow chromophore indicated AChE activity. Test results showed that the color intensity decreased as increasing concentrations of propoxur were added, thereby confirming the susceptibility of the enzyme to inhibitor. Assay of non-specific esterase however, indicated elevated levels which were correlated with degree of malathion resistance. Electrophoretic data revealed the presence of 2 esterase bands in all strains. It was concluded that such a pattern was not contributory to malathion resistance in adults.
    Matched MeSH terms: Dose-Response Relationship, Drug
  6. Ambu S, Mak JW, Ng CS
    J. Helminthol., 1992 Dec;66(4):293-6.
    PMID: 1293196
    The efficacy of ivermectin on experimental infections of P. malaysiensis in rats was determined. Ivermectin was 99.4% and 97.9% effective at a dosage of 400 meg and 800 meg respectively at seven days post-infection. The same two dosages of ivermectin when given at 14 days post infection had an efficacy of 100%. However, as an adulticide it had only 40.7% efficacy. Ivermectin may therefore be useful for the treatment of parastrongyliasis due to the larval stages of the worm which can cause significant pathology in man and animals.
    Matched MeSH terms: Dose-Response Relationship, Drug
  7. Raju SS, Gopalakrishna HN, Venkatadri N
    Pharmacol Res, 1998 Dec;38(6):449-52.
    PMID: 9990653
    A comparative effect of propranolol and nifedipine administered individually and in combination at graded dose levels; and that of phenytoin at 30 mg kg-1 on maximal electroshock (MES)-induced seizure in mice was investigated. Propranolol in doses of 10 mg kg-1 and 20 mg kg-1, and nifedipine in doses of 8 mg kg-1 and 16 mg kg-1 significantly modified MES activity. Propranolol (40 mg kg-1), and a combination of propranolol (20 mg kg-1) and nifedipine (8 mg kg-1), produced antiMES activity, which was comparable to that of phenytoin (30 mg kg-1). In mice treated with propranolol and nifedipine combination, the tonic flexor and tonic extensor phase ratios (F/E ratio) were significantly higher than individual drug responses. Our findings suggest that a combination of propranolol and nifedipine has either synergistic or an additive effect in controlling MES-induced seizures in mice.
    Matched MeSH terms: Dose-Response Relationship, Drug
  8. Lim JL, Visvalingam M
    PMID: 2402678
    Two highly active synthetic pyrethroid insecticides, lambdacyhalothrin and cypermethrin, were evaluated as thermal fogs against houseflies (Musca domestica Linnaeus) and mosquitos (Aedes aegypti Linnaeus). Lambdacyhalothrin (OMS 3021) showed an average of 2.5 times more knockdown activity and over 5 times more adulticidal activity than cypermethrin against Musca domestica and Aedes aegypti. These results demonstrate that lambdacyhalothrin is highly effective at very low rates as a thermal fog against Ae. aegypti and M. domestica. Commercially available formulations of 2.5% and 5% lambdacyhalothrin can be diluted either with water for ULV cold aerosol space-spraying or with diesel/kerosene for thermal fogging at recommended application rates of 0.5-1 g ai/ha for mosquito control and 2 g ai/ha for housefly control. Due to the very low rates of application, formulated products of lambdacyhalothrin are unlikely to present any acute hazards in normal use. The low dosages required to bring about rapid control of houseflies and mosquitos make this new pyrethroid insecticide particularly cost-effective. Coupled with its good residual activity (Jutsum et al, 1984), lambdacyhalothrin can be adopted as a powerful tool in integrated pest management program for the control of medically important pests and vectors.
    Matched MeSH terms: Dose-Response Relationship, Drug
  9. Adityanjee, Singh S, Subramaniam M
    Biol Psychiatry, 1989 Jun;26(2):199-202.
    PMID: 2567611
    Matched MeSH terms: Dose-Response Relationship, Drug
  10. Tan NH, Saifuddin MN
    PMID: 1982873
    1. The edema-inducing activity of 24 venoms from snakes of the subfamilies of Elapinae, Hydrophiini, Crotalinae and Viperinae was determined. 2. All snake venoms tested are very potent edema inducers. The minimum edema doses of the venoms ranged from 0.16 to 3.41 micrograms per mouse paw. 3. The venoms induced a rapid onset edema which peaked within 1 h of injection and declined thereafter; at low dose, however, some venoms induced a rapid onset edema that sustained over a longer duration.
    Matched MeSH terms: Dose-Response Relationship, Drug
  11. Yap HH, Lau BL, Leong YP
    PMID: 6189198
    The toxic effects of Abate (temephos) on mosquito larvae and non-target organisms were studied in the rice-field and in the laboratory. In the laboratory tests, Culex tritaeniorhychus larvae and cladoceran zooplanktons (predominantly Diaphanosoma and Moinodaphnia species) were found to be highly susceptible to Abate with LC50 values of 0.27 and less than 0.10 parts per billion respectively. Other non-target species in decreasing degree of susceptibility to Abate were copepods (Tropodiaptomus spp.), Aplocheilus panchax and Tubifex worms. In field study, Abate at concentrations 60, 100 and 200 gm hectare-1 is effective in maintaining the rice-fields free of Anopheles and Culex mosquitoes for at least 2 days. No mortality was observed for Aplocheilus panchax and Tubifex worms at the above concentrations; nevertheless, populations of cladoceran zooplanktons and copepods were reduced up to seven days posttreatment.
    Matched MeSH terms: Dose-Response Relationship, Drug
  12. Muir CK, Alias S
    Med J Malaysia, 1981 Jun;36(2):116-8.
    PMID: 6123934
    The effect of specific alpha[ or alpha2 adrenoceptor agents on the response of rat superior mesenteric-portal vein to field stimulation was investigated. In. a dose related manner, phenylephrine (alpha[ agonist) and yohimbine (alpha2 antagonists) increased while prazosin (alpha[ antagonist) and clonidine (alpha2 agonist) decreased the response of the vein to field stimulation. These effects are the same as those seen with these agents on rat and mouse vas deferens. It is suggested that, as in vas deferens, alpha1 postsynaptic and alpha2 presynaptic receptors exist in rat superior mesenteric-portal vein and that these receptors may be sufficiently sensitive in vein for their existence to be of significance in the action of these agents at clinical doses.
    Matched MeSH terms: Dose-Response Relationship, Drug
  13. Lutterodt GD, Maleque A
    J Ethnopharmacol, 1988 Dec;24(2-3):219-31.
    PMID: 3253493
    Studies were carried out on the suppression of both exploratory and spontaneous locomotor activities in the mouse by a non-polar fraction from a methanol extract of the dried leaves of Psidium guajava. Shortly after intraperitoneal administration of this fraction, typical narcotic-like effects were observed, including catalepsy, analgesia, Straub tail, shallow respiratory movements and exophthalmos. The dose for 90% suppression of exploratory activity was between 3.3 and 6.6 mg/kg intraperitoneally and the onset of action was 6-8 min. The duration of activity was dose-dependent and, for a dose of 13.2 mg/kg given intraperitoneally, it was found to be more than 6 h. Qualitatively similar results on exploratory activity were obtained when the extract was administered orally. Doses of 3.3-6.6 mg/kg i.p. depressed spontaneous locomotor activity and tunnel running was curtailed. Higher doses abolished the spontaneous locomotor reflex action. A flavonoid compound or compounds appear to account for the activity seen.
    Matched MeSH terms: Dose-Response Relationship, Drug
  14. Ganendran A, Balabaskaran S
    PMID: 1030852
    In acute severe anticholinesterase poisoning by organophosphate compounds, pralidoxime (P-2-AM, pyridine-2-aldoxime methiodide) used in the recommended doses, intravenously, has not been shown to reactivate the inhibited cholinesterase, as evidenced both clinically and biochemically. In vitro studies using pralidoxime iodide up to ten times the recommended concentrations, produced insignificant reactivation of cholinesterases inhibited by the organophosphate insecticide Bidrin (di-methyl-3-hydroxyl-N, N-dimethyl-crotonamide phosphate). This was even so despite prolonged exposure of the inhibited cholinesterases to the oxime. The value of pralidoxime as a reactivator of phosphorylated cholinesterases is therefore in doubt, and should not be used in preference to large doses of atropine and other supportive treatment in poisoning by organophosphate insecticides.
    Matched MeSH terms: Dose-Response Relationship, Drug
  15. Singh N, Menon V
    Med J Malaysia, 1975 Mar;30(3):209-13.
    PMID: 1160681
    Matched MeSH terms: Dose-Response Relationship, Drug
  16. Venugopala KN, Chandrashekharappa S, Pillay M, Abdallah HH, Mahomoodally FM, Bhandary S, et al.
    PLoS One, 2019;14(6):e0217270.
    PMID: 31163040 DOI: 10.1371/journal.pone.0217270
    Indolizines are heteroaromatic compounds, and their synthetic analogues have reportedly showed promising pharmacological properties. In this study, a series of synthetic 7-methoxy-indolizine derivatives were synthesised, characterised and evaluated for in vitro whole-cell anti-tuberculosis (TB) screening against susceptible (H37Rv) and multi-drug-resistant (MDR) strains of Mycobacterium tuberculosis (MTB) using the resazurin microplate assay method. The cytotoxicity was evaluated using the MTT assay. In silico molecular-docking study was conducted for compounds 5a-j against enoyl-[acyl-carrier] protein reductase, a key enzyme of the type II fatty acid synthesis that has attracted much interest for the development of novel anti-TB compounds. Thereafter, molecular dynamic (MD) simulation was undertaken for the most active inhibitors. Compounds 5i and 5j with the methoxy functional group at the meta position of the benzoyl group, which was at the third position of the indolizine nucleus, demonstrated encouraging anti-TB activity against MDR strains of MTB at 16 μg/mL. In silico studies showed binding affinity within the range of 7.07-8.57 kcal/mol, with 5i showing the highest binding affinity. Hydrogen bonding, π-π- interactions, and electrostatic interactions were common with the active site. Most of these interactions occurred with the catalytic amino acids (Pro193, Tyr158, Phe149, and Lys165). MD simulation showed that 5j possessed the highest binding affinity toward the enzyme, according to the two calculation methods (MM/PBSA and MM/GBSA). The single-crystal X-ray studies of compounds 5c and 5d revealed that the molecular arrangements in these two structures were mostly guided by C-H···O hydrogen-bonded dimeric motifs and C-H···N hydrogen bonds, while various secondary interactions (such as π···π and C-H···F) also contributed to crystal formation. Compounds 5a, 5c, 5i, and 5j exhibited no toxicity up to 500 μg/mL. In conclusion, 5i and 5j are promising anti-TB compounds that have shown high affinity based on docking and MD simulation results.
    Matched MeSH terms: Dose-Response Relationship, Drug
  17. Zaman K, Rahim F, Taha M, Ullah H, Wadood A, Nawaz M, et al.
    Bioorg Chem, 2019 08;89:103024.
    PMID: 31176853 DOI: 10.1016/j.bioorg.2019.103024
    Despite of many diverse biological activities exhibited by benzimidazole scaffold, it is rarely explored for the urease inhibitory potential. For that purpose, benzimidazole analogues 1-19 were synthesized and screened for in vitro urease inhibitory potential. Structures of all synthetic analogues were deduced by different spectroscopic techniques. All analogues revealed inhibition potential with IC50 values of 0.90 ± 0.01 to 35.20 ± 1.10 μM, when compared with the standard thiourea (IC50 = 21.40 ± 0.21 μM). Limited SAR suggested that the variations in the inhibitory potentials of the analogues are the result of different substitutions on phenyl ring. In order to rationalize the binding interactions of most active compounds with the active site of urease enzyme, molecular docking study was conducted.
    Matched MeSH terms: Dose-Response Relationship, Drug
  18. Singh D, Narayanan S, Grundmann O, Dzulkapli EB, Vicknasingam B
    Subst Use Misuse, 2019;54(14):2284-2289.
    PMID: 31347441 DOI: 10.1080/10826084.2019.1645178
    Background: Mitragyna speciosa (Korth.) or kratom is an indigenous medicinal plant of Southeast Asia. Kratom is widely reported to have dose-dependent effects based on available literature, but to our knowledge, this has not been established conclusively. Objective: This study sought to evaluate if kratom use produces dose-dependent effects, with a stimulant effect at low doses and a sedative effect at high doses, in a sample of regular kratom users. Methods: A total of 63 regular kratom users participated in this cross-sectional study. The Brief-Biphasic Alcohol Effects Scale (B-BAES) was used to determine subjects self-report kratom use experiences. Results: Almost all in the sample were male (98%, n = 62/63), and the majority of subjects were Malays (94%, n = 59/63). The mean age of the subjects in the sample was 43.8 years (SD = 12.1). Seventy-five percent (n = 47/63) have >5 years kratom use history, and 65% (n = 41/63) consumed >3 glasses of kratom daily. Results from first test showed no significant difference in the stimulant (t61 =0.371, p 3 glasses a day or less than this amount, regardless of duration of use. In the second test, no significant differences in the mean scores were found among those who consumed >3 glasses daily or less than this amount among short-term or long-term uses. Conclusions: Daily kratom use produced both stimulant and sedative effects but they were not statistically significantly associated with the dose consumed, both among short-term and long-term users in our sample.
    Matched MeSH terms: Dose-Response Relationship, Drug
  19. Huang W, Chen X, Guan Q, Zhong Z, Ma J, Yang B, et al.
    Gene, 2019 Mar 20;689:43-50.
    PMID: 30528270 DOI: 10.1016/j.gene.2018.11.083
    Atmospheric CO2 level is one of the most important factors which affect plant growth and crop production. Although many crucial genes and pathways have been identified in response to atmospheric CO2 changes, the integrated and precise mechanisms of plant CO2 response are not well understood. Alternative splicing (AS) is an important gene regulation process that affects many biological processes in plants. However, the AS pattern changes in plants in response to elevated CO2 levels have not yet been investigated. Here, we used RNA-Seq data of Arabidopsis thaliana grown under different CO2 concentration to analyze the global changes in AS. We found that AS increased with the rise in CO2 concentration. Additionally, we identified 345 differentially expressed (DE) genes and 251 differentially alternative splicing (DAS) genes under the elevated CO2 condition. Moreover, the results showed that the expression of most of the DAS genes did not change significantly, indicating that AS can serve as an independent mechanism for gene regulation in response to elevated CO2. Furthermore, our analysis of function categories revealed that the DAS genes were associated mainly with the stimulus response. Overall, this the first study to explore the changes of AS in plants in response to elevated CO2.
    Matched MeSH terms: Dose-Response Relationship, Drug
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