Displaying publications 1561 - 1580 of 6722 in total

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  1. Abbasi MA, Raza H, Aziz-Ur-Rehman, Siddiqui SZ, Muhammad S, Khan FM, et al.
    Chem Biodivers, 2023 Sep;20(9):e202300257.
    PMID: 37578300 DOI: 10.1002/cbdv.202300257
    In the presented work, a new series of three different 4-((3,5-dichloro-2-[(2/4-halobenzyl)oxy]phenyl)sulfonyl)morpholines was synthesized and the structure of these compounds were corroborated by 1 H-NMR & 13 C-NMR studies. The in vitro results established all the three compounds as potent tyrosinase inhibitors relative to the standard. The Kinetics mechanism plots established that compound 8 inhibited the enzyme non-competitively. The inhibition constants Ki calculated from Dixon plots for this compound was 0.0025 μM. Additionally, computational techniques were used to explore electronic structures of synthesized compounds. Fully optimized geometries were further docked with tyrosinase enzyme for inhibition studies. Reasonably good binding/interaction energies and intermolecular interactions were obtained. Finally, drug likeness was also predicted using the rule of five (RO5) and Chemical absorption, distribution, metabolism, excretion, and toxicity (ADMET) characteristics. It is anticipated that current experimental and computational investigations will evoke the scientific interest of the research community for the above-entitled compounds.
  2. Irshad MA, Sattar S, Nawaz R, Al-Hussain SA, Rizwan M, Bukhari A, et al.
    Ecotoxicol Environ Saf, 2023 Sep 15;263:115231.
    PMID: 37429088 DOI: 10.1016/j.ecoenv.2023.115231
    Water contamination can be detrimental to the human health due to higher concentration of carcinogenic heavy metals such as chromium (Cr) in the wastewater. Many traditional methods are being employed in wastewater treatment plants for Cr removal to control the environmental impacts. Such methods include ion exchange, coagulation, membrane filtration, and chemical precipitation and microbial degradation. Recent advances in materials science and green chemistry have led to the development of nanomaterial that possess high specific surface areas and multiple functions, making them suitable for removing metals such as Cr from wastewater. Literature shows that the most efficient, effective, clean, and long-lasting approach for removing heavy metals from wastewater involves adsorbing heavy metals onto the surface of nanomaterial. This review assesses the removal methods of Cr from wastewater, advantages and disadvantages of using nanomaterial to remove Cr from wastewater and potential negative impacts on human health. The latest trends and developments in Cr removal strategies using nanomaterial adsorption are also explored in the present review.
  3. Hameed S, Din JU, Ali H, Kabir M, Younas M, Ur Rehman E, et al.
    PLoS One, 2020;15(11):e0228832.
    PMID: 33151925 DOI: 10.1371/journal.pone.0228832
    Pakistan's total estimated snow leopard habitat is about 80,000 km2 of which about half is considered prime habitat. However, this preliminary demarcation was not always in close agreement with the actual distribution-the discrepancy may be huge at the local and regional level. Recent technological developments like camera trapping and molecular genetics allow for collecting reliable presence records that could be used to construct realistic species distribution based on empirical data and advanced mathematical approaches like MaxEnt. The current study followed this approach to construct an accurate distribution of the species in Pakistan. Moreover, movement corridors, among different landscapes, were also identified through circuit theory. The probability of habitat suitability, generated from 98 presence points and 11 environmental variables, scored the snow leopard's assumed range in Pakistan, from 0 to 0.97. A large portion of the known range represented low-quality habitat, including areas in lower Chitral, Swat, Astore, and Kashmir. Conversely, Khunjerab, Misgar, Chapursan, Qurumber, Broghil, and Central Karakoram represented high-quality habitats. Variables with higher contributions in the MaxEnt model were precipitation during the driest month (34%), annual mean temperature (19.5%), mean diurnal range of temperature (9.8%), annual precipitation (9.4%), and river density (9.2). The model was validated through receiver operating characteristic (ROC) plots and defined thresholds. The average test AUC in Maxent for the replicate runs was 0.933 while the value of AUC by ROC curve calculated at 0.15 threshold was 1.00. These validation tests suggested a good model fit and strong predictive power. The connectivity analysis revealed that the population in the Hindukush landscape appears to be more connected with the population in Afghanistan as compared to other populations in Pakistan. Similarly, the Pamir-Karakoram population is better connected with China and Tajikistan, while the Himalayan population was connected with the population in India. Based on our findings we propose three model landscapes to be considered under the Global Snow Leopard Ecosystem Protection Program (GSLEP) agenda as regional priority areas, to safeguard the future of the snow leopard in Pakistan and the region. These landscapes fall within mountain ranges of the Himalaya, Hindu Kush and Karakoram-Pamir, respectively. We also identified gaps in the existing protected areas network and suggest new protected areas in Chitral and Gilgit-Baltistan to protect critical habitats of snow leopard in Pakistan.
  4. Ali A, Khan MA, Zahid H, Yaseen PM, Qayash Khan M, Nawab J, et al.
    Front Physiol, 2019;10:793.
    PMID: 31379587 DOI: 10.3389/fphys.2019.00793
    Although ticks prevalent in various agro-systems of Pakistan are associated with economic losses, information is still missing about the tick's diversity, hosts they infest, seasonal dynamics and molecular phylogeny of Rhipicephalus microplus in Khyber Pakhtunkhwa (KP) Pakistan. This study for the first time enlisted ticks infesting diverse hosts including humans in various regions of KP. A total of 8,641 ticks were collected across the northern, southern and central regions of KP and were morpho-taxonomically categorized into six genera comprising 17 species, R. microplus (n = 3,584, 42%), Hyalomma anatolicum (n = 2,253, 27%), Argas persicus (n = 1,342, 16%), Hya. impeltatum (n = 586, 7%), R. turanicus (n = 161, 2%), R. haemaphysaloides (n = 142, 2%), R. annulatus (n = 132, 2%), Hae. montgomeryi (n = 123, 1.4%), Hya. marginatum (n = 110, 1.3%), R. sanguineus (n = 34, 0.4%), and Hae. longicornis (n = 31, 0.4%). Ticks infesting wild animals included Amblyomma gervaisi, Amb. exornatum, Amb. latum, Dermacentor marginatus, and Hae. indica, while ticks collected from humans included R. microplus, R. annulatus, Hya. anatolicum, Hya. marginatum, and Hae. punctata. The overall prevalence of ticks infesting domestic animals was 69.4% (536/772). Among animal hosts, cattle were found highly infested (87.2%, 157/180) followed by buffalos (79%, 91/114), domestic fowls (74.7%, 112/150), goats (68.3%, 82/120), dogs (66.7%, 32/48), horses (61.3%, 49/80), and sheep (16.3%, 13/80). Analysis revealed that the tick burden significantly differed among domestic animals and was found to be high in cattle, followed by buffalos, goats, sheep, domestic fowl, dogs, and horses. Seasonal patterns of ticks distribution showed highest prevalance in July, August, and September due to the prevailing high temperature and humidity during these months. The phylogenetic analysis of cattle tick R. microplus based on partial mitochondrial cytochrome oxidase subunit I (COX1), 16S ribosomal RNA (16S rRNA) and internal transcribed spacer 2 (ITS2) sequences, revealed that R. microplus prevalent in this region belongs to clade C which include ticks originating from Bangladesh, Malaysia, and India. Further large scale studies across the country are necessary to explore the molecular and cross breeding aspects at the geographical overlapping of various tick species and their associated pathogens to facilitate designing control strategies as well as awareness against tick infestation in the region.
  5. Mohd Rawi SB, Low Yan Fay Z, Muhammad Khairus NFF, Annandan SK, Mohd Sani N, Mat Termizi MH, et al.
    Medicine (Baltimore), 2023 Oct 27;102(43):e35520.
    PMID: 37904385 DOI: 10.1097/MD.0000000000035520
    Type 2 diabetes mellitus (T2DM) has become increasingly prevalent among young adults. Risk perception is believed to be an important determinant of preventive health behaviors; however, young adults remain unaware of the benefits. The current study aimed to examine Malaysian public university students' perceived risk of developing T2DM and its predictors. This cross-sectional study involved a total of 1078 healthy students at Universiti Kebangsaan Malaysia (UKM). The validated Malay version of the Questionnaire on Risk Perception of Developing Non-Communicable Diseases in Malaysia was used to assess their perceived risk of developing T2DM in the future. Multiple logistic regression was used to analyze the data regarding the predictors of perceived risk to obtain the final model after controlling the potential confounders. . It was found that the majority of respondents (83.8%) perceived low risk of developing T2DM. Results from the multiple logistic regression indicated that respondents from non-health related faculties (OR, 1.71: 95% CI 1.162, 2.515), smoking (OR, 8.43: 95% CI 1.108, 64.130), consume fast food ≥ 3 times/month (OR, 1.56: 95% CI 1.104, 2.207), and snacking ≥ 3 times/week (OR, 1.79: 95% CI 1.262, 2.550) were significant positive predictors while family history of diabetes was a negative predictor (OR, 0.50: 95% CI 0.350, 0.695). Students who self-rated themselves as practising healthy lifestyles and actively seeking health information perceived a low risk of developing diabetes in the future. . The findings indicate that students perceived their risk as low even though they have the risk. This creates an urgent need to emphasize the necessity of diabetes prevention education, especially on socio-behavioral factors, to address the widespread misunderstandings among university students regarding diabetes risk factors to reduce diabetes incidence.
  6. Azeem MK, Islam A, Khan RU, Rasool A, Anees Ur Rehman Qureshi M, Rizwan M, et al.
    R Soc Open Sci, 2023 Dec;10(12):231157.
    PMID: 38094268 DOI: 10.1098/rsos.231157
    The present study was aimed at synthesis of polymeric hydrogels for controlled boron (B) release, as B deficiency is a major factor that decreases crops yield. Thus, graphene oxide incorporated guar gum and poly (ethylene glycol) hydrogels were prepared using the Solution Casting method for boron release. 3-Glycidyloxypropyl trimethoxysilane (GLYMOL) was used as a cross-linker. Characterizations of hydrogels were carried out by Fourier Transform Infrared Spectroscopy (FTIR), Thermo-Gravimetric Analysis and Scanning Electron scope. The FTIR outcomes confirmed the existence of functional groups, bindings and development of hydrogel frameworks from incorporated components. The quantity of GLYMOL directly increased the thermal stability and water retention but decreased the swelling %. The maximum swelling for the hydrogel formulations was observed at pH 7. The addition of GLYMOL changed the diffusion from quasi-Fickcian to non-Fickcian diffusion. The maximum swelling quantities of 3822% and 3342% were exhibited by GPP (control) and GPP-8 in distilled water, respectively. Boron release was determined in distilled water and sandy soil by azomethine-H test using UV-Visible spectrophotometer while 85.11% and 73.65% boron was released from BGPP-16, respectively. In short, water retentive, water holding capacities, swelling performances, biodegradability and swelling/deswelling features would offer an ideal platform for boron release in sustained agricultural applications.
  7. Safdar ME, Wang X, Abbas M, Ozaslan C, Asif M, Adnan M, et al.
    PLoS One, 2021;16(11):e0258920.
    PMID: 34739485 DOI: 10.1371/journal.pone.0258920
    Weed infestation is a persistent problem for centuries and continues to be major yield reducing issue in modern agriculture. Chemical weed control through herbicides results in numerous ecological, environmental, and health-related issues. Moreover, numerous herbicides have evolved resistance against available herbicides. Plant extracts are regarded as an alternative to herbicides and a good weed management option. The use of plant extracts is environmentally safe and could solve the problem of herbicide resistance. Therefore, laboratory and wire house experiments were conducted to evaluate the phytotoxic potential of three Fabaceae species, i.e., Cassia occidentalis L. (Coffee senna), Sesbania sesban (L.) Merr. (Common sesban) and Melilotus alba Medik. (White sweetclover) against seed germination and seedling growth of some broadleaved weed species. Firstly, N-hexane and aqueous extracts of these species were assessed for their phytotoxic effect against lettuce (Lactuca sativa L.). The extracts found more potent were further tested against germination and seedling growth of four broadleaved weed species, i.e., Parthenium hysterophorus L. (Santa-Maria), Trianthema portulacastrum L. (Pigweed), Melilotus indica L (Indian sweetclover). and Rumex dentatus L. (Toothed dock) in Petri dish and pot experiments. Aqueous extracts of all species were more toxic than their N-hexane forms for seed germination and seedling growth of lettuce; therefore, aqueous extracts were assessed for their phytotoxic potential against four broadleaved weed species. Aqueous extracts of all species proved phytotoxic against T. portulacastrum, P. hysterophorus, M. indica and R. dentatus and retarder their germination by 57, 90, 100 and 58%, respectively. Nevertheless, foliar spray of C. occidentalis extract was the most effective against T. portulacastrum as it reduced its dry biomass by 72%, while M. alba was effective against P. hysterophorus, R. dentatus and M. indica and reduced their dry biomass by 55, 68 and 81%, respectively. It is concluded that aqueous extracts of M. alba, S. sesban and C. occidentalis could be used to retard seed germination of T. portulacastrum, P. hysterophorus, M. indica and R. dentatus. Similarly, aqueous extracts of C. occidentalis can be used to suppress dry biomass of T. portulacastrum, and those of M. alba against P. hysterophorus, R. dentatus. However, use of these extracts needs their thorough testing under field conditions.
  8. Sa'adi Z, Alias NE, Yusop Z, Iqbal Z, Houmsi MR, Houmsi LN, et al.
    Sci Total Environ, 2024 Feb 20;912:169187.
    PMID: 38097068 DOI: 10.1016/j.scitotenv.2023.169187
    The most recent set of General Circulation Models (GCMs) derived from the Coupled Model Intercomparison Project Phase 6 (CMIP6) was used in this work to analyse the spatiotemporal patterns of future rainfall distribution across the Johor River Basin (JRB) in Malaysia. A group of 23 GCMs were chosen for comparative assessment in simulating basin-scale rainfall based on daily rainfall from the historical period of the Climate Hazards Group InfraRed Precipitation with Station Data (CHIRPS). The methodological novelty of this study lies in the application of relative importance metrics (RIM) to rank and select historical GCM simulations for reproducing rainfall at 109 CHIRPS grid points within the JRB. In order to choose the top GCMs, the rankings given by RIM were aggregated using the compromise programming index (CPI) and Jenks optimised classification (JOC). It was found that ACCESS-ESM1-5 and CMCC-ESM2 were ranked the highest in most of the grid. The final GCM was then bias-corrected using the linear scaling method before being ensemble based on the Bayesian model averaging (BMA) technique. The spatiotemporal assessment of the ensemble model for the different months over the near-future period 2021-2060 and far-future period 2061-2100 was compared with those under Shared Socioeconomic Pathways (SSPs), namely, SSP1-2.6, SSP2-4.5, SSP3-7.0, and SSP5-8.5. Heterogeneous changes in rainfall were projected across the JRB, with both increasing and decreasing trends. In the near-future and far-future scenarios, higher rainfall was projected for December, indicating an elevated risk of flooding during the end of the North East monsoon (NEM). Conversely, August showed a decreasing trend in rainfall, implying an increasing risk of severe drought. The findings of this study provide valuable insights for effective water resource management and climate change adaptation in the region.
  9. Muhammad MT, Beniddir MA, Phongphane L, Abu Bakar MH, Hussin MH, Awang K, et al.
    Fitoterapia, 2024 Apr;174:105873.
    PMID: 38417682 DOI: 10.1016/j.fitote.2024.105873
    Diabetes mellitus stands as a metabolic ailment marked by heightened blood glucose levels due to inadequate insulin secretion. The primary aims of this investigative inquiry encompassed the isolation of phytochemical components from the bark of Kopsia teoi, followed by the assessment of their α-amylase inhibition. The phytochemical composition of the K. teoi culminated in the discovery of a pair of new indole alkaloids; which are 16-epi-deacetylakuammiline N(4)-methylene chloride (akuammiline) (1), and N(1)-methoxycarbonyl-11-methoxy-12-hydroxy-Δ14-17-kopsinine (aspidofractinine) (2), together with five known compounds i.e. kopsiloscine G (aspidofractinine) (3), akuammidine (sarpagine) (4), leuconolam (aspidosperma) (5), N-methoxycarbonyl-12-methoxy-Δ16, 17-kopsinine (aspidofractinine) (6), and kopsininate (aspidofractinine) (7). All compounds were determined via spectroscopic analyses. The in vitro evaluation against α-amylase showed good inhibitory activities for compounds 5-7 with the inhibitory concentration (IC50) values of 21.7 ± 1.2, 34.1 ± 0.1, and 30.0 ± 0.8 μM, respectively compared with the reference acarbose (IC50 = 34.4 ± 0.1 μM). The molecular docking outputs underscored the binding interactions of compounds 5-7 ranging from -8.1 to -8.8 kcal/mol with the binding sites of α-amylase. Consequently, the outcomes highlighted the anti-hyperglycemic attributes of isolates from K. teoi.
  10. Onifade OA, Yusairie FA, Abu Bakar MH, Alresheedi MT, Khoon Ng E, Mahdi MA, et al.
    Biosens Bioelectron, 2024 Oct 01;261:116486.
    PMID: 38861811 DOI: 10.1016/j.bios.2024.116486
    Current uric acid detection methodologies lack the requisite sensitivity and selectivity for point-of-care applications. Plasmonic sensors, while promising, demand refinement for improved performance. This work introduces a biofunctionalized sensor predicated on surface plasmon resonance to quantify uric acid within physiologically relevant concentration ranges. The sensor employs the covalent immobilization of uricase enzyme using 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) and N-Hydroxysuccinimide (NHS) crosslinking agents, ensuring the durable adherence of the enzyme onto the sensor probe. Characterization through atomic force microscopy and Fourier transform infrared spectroscopy validate surface alterations. The Langmuir adsorption isotherm model elucidates binding kinetics, revealing a sensor binding affinity of 298.83 (mg/dL)-1, and a maximum adsorption capacity of approximately 1.0751°. The biofunctionalized sensor exhibits a sensitivity of 0.0755°/(mg/dL), a linear correlation coefficient of 0.8313, and a limit of detection of 0.095 mg/dL. Selectivity tests against potentially competing interferents like glucose, ascorbic acid, urea, D-cystine, and creatinine showcase a significant resonance angle shift of 1.1135° for uric acid compared to 0.1853° for interferents at the same concentration. Significantly, at a low uric acid concentration of 0.5 mg/dL, a distinct shift of 0.3706° was observed, setting it apart from the lower values noticed at higher concentrations for all typical interferent samples. The uricase enzyme significantly enhances plasmonic sensors for uric acid detection, showcasing a seamless integration of optical principles and biological recognition elements. These sensors hold promise as vital tools in clinical and point-of-care settings, offering transformative potential in biosensing technologies and the potential to revolutionize healthcare outcomes in biomedicine.
  11. Razak RNHA, Ismail F, Isa MLM, Wahab AYA, Muhammad H, Ramli R, et al.
    Malays J Med Sci, 2019 Jan;26(1):44-57.
    PMID: 30914892 MyJurnal DOI: 10.21315/mjms2019.26.1.4
    Background: Cyclophosphamide (CP) is a widely used anti-neoplastic and immunosuppressive agent that is associated with adverse side effects including reproductive toxicity. Aquilaria malaccensis (AM) is a traditional medicinal plant which was reported to exhibit high anti-oxidant and free radical scavenging properties. The present study was aimed to evaluate the protective effects of AM leaves extract on sperm quality following toxic exposure to CP.

    Methods: Forty-eight male Sprague Dawley rats were allocated into eight groups of six rats (n = 6): control, CP only (200 mg kg-1), AM only (100 mg kg-1, 300 mg kg-1 and 500 mg kg-1) and CP + AM (100 mg kg-1, 300 mg kg-1 and 500 mg kg-1). Animals were sacrificed after 63 days of treatment and the sperm from the caudal epididymis was taken for sperm analysis.

    Results: The body and the reproductive organs weight, sperm count and motility did not differ between CP and other groups (P > 0.05). A significant increase (P < 0.05) in percentage of the dead and abnormal sperm were seen in the CP alone treated group compared to the control group. Co-administration of AM to the CP exposed rats significantly reduced the (P < 0.05) percentage of abnormal sperm as compared to the CP only group.

    Conclusion: Overall, the present results represent the potential of AM to protect against CP induced reproductive toxicity.

  12. Zakaria NN, Daud H, Sokkalingam R, Othman M, Abdul Kadir E, Mohd Aris MN, et al.
    PMID: 39037622 DOI: 10.1007/s11356-024-34409-0
    Stochastic modeling approaches have attracted many researchers to the field. However, fire hotspot detection suffers from not using a Markov chain quasi-Monte Carlo (MCQMC) as a forecasting methodology. This paper proposes improvements to the computational time by combining the strengths of the Markov chain Monte Carlo (MCMC) and quasi-Monte Carlo (QMC) methods. The proposed method can lead to more precise and stable results, particularly in problems with high-dimensional integration or complex probability distributions. The proposed method is applied to a case study of fire hotspot detection in Sarawak, Malaysia. The outcome of this study reveals that the MCQMC method is more computationally efficient, taking only 0.0746 seconds compared to MCMC's 0.0914 seconds and QMC's 0.0994 seconds. It is shown that the best option derived by the proposed method is effective in predicting fire hotspots and providing quick solutions to protect the environment and communities from forest fires.
  13. Naqvi SAH, Farhan M, Ahmad M, Kiran R, Fatima N, Shahbaz M, et al.
    World J Microbiol Biotechnol, 2024 Aug 16;40(10):302.
    PMID: 39150639 DOI: 10.1007/s11274-024-04108-6
    The genus Phytophthora contains more than 100 plant pathogenic species that parasitize a wide range of plants, including economically important fruits, vegetables, cereals, and forest trees, causing significant losses. Global agriculture is seriously threatened by fungicide resistance in Phytophthora species, which makes it imperative to fully comprehend the mechanisms, frequency, and non-chemical management techniques related to resistance mutations. The mechanisms behind fungicide resistance, such as target-site mutations, efflux pump overexpression, overexpression of target genes and metabolic detoxification routes for fungicides routinely used against Phytophthora species, are thoroughly examined in this review. Additionally, it assesses the frequency of resistance mutations in various Phytophthora species and geographical areas, emphasizing the rise of strains that are resistant to multiple drugs. The effectiveness of non-chemical management techniques, including biological control, host resistance, integrated pest management plans, and cultural practices, in reducing fungicide resistance is also thoroughly evaluated. The study provides important insights for future research and the development of sustainable disease management strategies to counter fungicide resistance in Phytophthora species by synthesizing current information and identifying knowledge gaps.
  14. Nisar M, Tasleem Z, Muhammad SA, Javid A, Rasool MF, Karuniawati H, et al.
    Cost Eff Resour Alloc, 2024 Sep 05;22(1):65.
    PMID: 39237946 DOI: 10.1186/s12962-024-00566-9
    BACKGROUND: The direct and indirect costs of chronic kidney disease (CKD) are substantial and increase over time. Concerns regarding our capacity to manage the financial burden that CKD) places on patients, caregivers, and society are raised by its increasing prevalence and progression. Lack of awareness of CKD's economic effects is a major reason that lawmakers and administrators pay little attention to this chronic illness.

    OBJECTIVE: We aimed to analyze the direct burden of CKD across Asian countries and evaluate the main cost drivers among all mentioned cost centers in previous studies.

    METHODOLOGY: Related works evaluating the expenditures of CKD from the perspective of the patient were interpreted by a thorough search of PUBMED and GOOGLE SCHOLAR.

    RESULTS: Country-wise, in Asia, the direct mean average medical costs in RRT patients were reported in 8 studies as $4574, $18668, $2901, $6848, $16669, $3489, $5945, and $6344 in Singapore, Korea, Taiwan, China, Jordan, Vietnam, Lebanon, and India respectively and the direct mean average medical costs in non-RRT patients were reported in six studies as $3412, $2241, $4534, $290 and $1500 in Singapore, Japan, China, Vietnam, and India respectively.

    CONCLUSION: Hemodialysis is the main cost driver having an average mean cost of $23,358 per patient per year while the average mean cost of disease management is $4977 per patient per year. More research is needed to understand the specific economic challenges disadvantaged populations face, including the impact of income, education, and access to healthcare resources on the financial burden of CKD.

  15. Khan KM, Rahim F, Wadood A, Kosar N, Taha M, Lalani S, et al.
    Eur J Med Chem, 2014 Jun 23;81:245-52.
    PMID: 24844449 DOI: 10.1016/j.ejmech.2014.05.010
    In our effort directed toward the discovery of new anti-diabetic agent for the treatment of diabetes, a library of biscoumarin derivative 1-18 was synthesized and evaluated for α-glucosidase inhibitory potential. All eighteen (18) compounds displayed assorted α-glucosidase activity with IC50 values 16.5-385.9 μM, if compared with the standard acarbose (IC50 = 906 ± 6.387 μM). In addition, molecular docking studies were carried out to explore the binding interactions of biscoumarin derivatives with the enzyme. This study has identified a new class of potent α-glucosidase inhibitors.
  16. Bukhari SNA, Alotaibi NH, Ahmad W, Alharbi KS, Abdelgawad MA, Al-Sanea MM, et al.
    Med Chem, 2020 Sep 05.
    PMID: 32888274 DOI: 10.2174/1573406416666200905125038
    BACKGROUND: Ligustrazine and chalcones have been reported previously for various biological activities including anticancer effects.

    OBJECTIVES: Based on the multitargeted biological activities approach of ligustrazine based chalcones, in current study 18 synthetic ligustrazine-containing α, β-unsaturated carbonyl-based 1, 3-Diphenyl-2-propen-1-one derivatives were evaluated for their inhibitory effects on growth of five different types of cancer cells.

    METHODS: All compounds were evaluated for anticancer effects on various cancer cell lines by propidium iodide fluorescence assay and various other assays were performed for mechanistic studies.

    RESULTS: Majority of compounds exhibited strong inhibition of cancer cells especially synthetic compounds 4a and 4b bearing 1-Pyridin-3-yl-ethanone as a ketone moiety in main structural backbone were found most powerful inhibitors of cancer cell growth. Most active 9 compounds among whole series were selected for further studies related to different cancer targets including EGFR TK kinases, tubulin polymerization, KAF and BRAFV600E.

    CONCLUSION: Synthetic derivatives including 4a-b and 5a-b showed multitarget approach and showed strong inhibitory effects on EGFR, FAK and BRAF while three compounds including 3e bearing methoxy substitution, 4a and 4b with 1- pyridin-3-yl-ethanone moiety showed the inhibition of tubulin polymerization.

  17. Rizwan K, Zubair M, Rasool N, Mahmood T, Ayub K, Alitheen NB, et al.
    Chem Cent J, 2018 May 04;12(1):49.
    PMID: 29728881 DOI: 10.1186/s13065-018-0404-7
    Thiophene derivatives have shown versatile pharmacological activities. The Suzuki reaction proved a convenient method for C-C bond formations in organic molecules. In the present research work novel derivatives of 2,5-dibromo-3-methylthiophene (3a-k and 3l-p) has been synthesized, via Suzuki coupling reaction in low to moderate yields. A wide range of functional groups were well tolerated in reaction. Density functional theory investigations on all synthesized derivatives (3a-3p) were performed in order to explore the structural properties. The pharmaceutical potential of synthesized compounds was investigated through various bioassays (antioxidant, antibacterial, antiurease activities). The compounds 3l, 3g, 3j, showed excellent antioxidant activity (86.0, 82.0, 81.3%), respectively by scavenging DPPH. Synthesized compounds showed promising antibacterial activity against tested strains. 3b, 3k, 3a, 3d and 3j showed potential antiurease activity with 67.7, 64.2, 58.8, 54.7 and 52.1% inhibition at 50 µg/ml. Results indicated that synthesized molecules could be a potential source of pharmaceutical agents.
  18. Shah SM, Ullah F, Khan S, Shah SM, de Matas M, Hussain Z, et al.
    Drug Des Devel Ther, 2016;10:3837-3850.
    PMID: 27920499
    Artemether (ARTM) is a very effective antimalarial drug with poor solubility and consequently low bioavailability. Smart nanocrystals of ARTM with particle size of 161±1.5 nm and polydispersity index of 0.172±0.01 were produced in <1 hour using a wet milling technology, Dena(®) DM-100. The crystallinity of the processed ARTM was confirmed using differential scanning calorimetry and powder X-ray diffraction. The saturation solubility of the ARTM nanocrystals was substantially increased to 900 µg/mL compared to the raw ARTM in water (145.0±2.3 µg/mL) and stabilizer solution (300.0±2.0 µg/mL). The physical stability studies conducted for 90 days demonstrated that nanocrystals stored at 2°C-8°C and 25°C were very stable compared to the samples stored at 40°C. The nanocrystals were also shown to be stable when processed at acidic pH (2.0). The solubility and dissolution rate of ARTM nanocrystals were significantly increased (P<0.05) compared to those of its bulk powder form. The results of in vitro studies showed significant antimalarial effect (P<0.05) against Plasmodium falciparum and Plasmodium vivax. The IC50 (median lethal oral dose) value of ARTM nanocrystals was 28- and 54-fold lower than the IC50 value of unprocessed drug and 13- and 21-fold lower than the IC50 value of the marketed tablets, respectively. In addition, ARTM nanocrystals at the same dose (2 mg/kg) showed significantly (P<0.05) higher reduction in percent parasitemia (89%) against P. vivax compared to the unprocessed (27%), marketed tablets (45%), and microsuspension (60%). The acute toxicity study demonstrated that the LD50 value of ARTM nanocrystals is between 1,500 mg/kg and 2,000 mg/kg when given orally. This study demonstrated that the wet milling technology (Dena(®) DM-100) can produce smart nanocrystals of ARTM with enhanced antimalarial activities.
  19. Ayaz S, Ahmad M, Zafar M, Ali MI, Sultana S, Mustafa MRU, et al.
    Microsc Res Tech, 2020 Mar;83(3):239-248.
    PMID: 31713962 DOI: 10.1002/jemt.23407
    The current study deals with the detailed morphology investigation of eight Cypsela species belonging to tribe Cichoreae. The different Cypsela types were described, explained, compared, and their taxonomic significance is discussed in detail. Light microscopy (LM) and scanning electron microscopy (SEM) have been used to highlight quantitative and qualitative characters of underestudied species. Cypsela exhibit great diversity in macro and micromorphological features such as shape, color, length, width, anticlinal and periclinal wall patterns, surface patterns, epicuticular projections. Majority of Cypsela species were brownish in color and their size ranges from 2.16 to 3.98 mm in length and 1.16 to 0.82 mm in breadth. A great diversity in Cypsela shapes like oblanceolate to obovate, obovoid to cylindrical, obvate, narrowly lanceolate were observed. Most of the platelets having epicuticular projections were observed. The surface pattern on the cypsela surface varied from rugose papillate, verrucose papillate, and striated. On the basis of considerable variations observed, the present study can assist as useful constraints at various taxonomic levels. The aim of the present study is to provide a comprehensive description of the Cypsela morphology and to determine the extent to which these micro morphological data can be used as a taxonomic character to delineate various taxa belonging to the tribe Cichoreae.
  20. Iqbal MS, Muthanna FMS, Kassab YW, Hassali MA, Al-Saikhan FI, Iqbal MZ, et al.
    PLoS One, 2020;15(6):e0234734.
    PMID: 32555595 DOI: 10.1371/journal.pone.0234734
    INTRODUCTION: The effect of anticoagulation control on overall Health-Related Quality of Life (HRQoL) in patients taking warfarin in Pakistan has not been explored yet. Therefore, this study aimed to evaluate HRQoL among warfarin patients in Pakistan.

    METHODS: This cross-sectional study was conducted among patients on warfarin in Pakistan. By purposive sampling, data were collected using demographic data collection form and the World Health Organization Quality of Life: Brief Version (WHOQOL-BREF). The WHOQOL-BREF is comprised of four domains; physical, psychological, social relationships, and environment. Descriptive and inferential statistical analysis was done using SPSS version 22.

    RESULTS: Out of 295 warfarin patients, more females than males (<0.001) were observed (n = 184, 62.4%, and n = 111, 37.6% respectively). One hundred and eighteen (40.0%) patients were less than 30-years of age, whereas one hundred and seventy-seven (60.0%) patients were above 30-years of age. Mean scores for the physical (62.44±15.36), psychological (67.84±15.54), social (64.27±26.28) and environment domains (63.45±17.66) were observed.

    CONCLUSION: Patients had overall lower to moderate but satisfactory HRQoL scores in all four domains. Age, gender, employment status, education level, the indication of use and duration of warfarin therapy was associated with one or more domains of HRQoL among warfarin patients. The findings of this study would serve as a primary database for future studies. This study highlights how non-clinical factors could impact HRQoL in studied patients.

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