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Synthesis, α-amylase inhibitory potential and molecular docking study of indole derivatives

Taha M, Baharudin MS, Ismail NH, Imran S, Khan MN, Rahim F, et al.

Bioorg Chem, 2018 10;80:36-42.
PMID: 29864686 DOI: 10.1016/j.bioorg.2018.05.021

In search of potent α-amylase inhibitor we have synthesized eighteen indole analogs (1-18), characterized by NMR and HR-EIMS and screened for α-amylase inhibitory activity. All analogs exhibited a variable degree of α-amylase inhibition with IC50 values ranging between 2.031 ± 0.11 and 2.633 ± 0.05 μM when compared with standard acarbose having IC50 values 1.927 ± 0.17 μM. All compounds showed good α-amylase inhibition. Compound 14 was found to be the most potent analog among the series. Structure-activity relationship has been established for all compounds mainly based on bringing about the difference of substituents on phenyl ring. To understand the binding interaction of the most active analogs molecular docking study was performed.
Conventional versus microwave assisted synthesis, molecular docking and enzyme inhibitory activities of new 3,4,5-trisubstituted-1,2,4-triazole analogues

Virk NA, Rehman A, Abbasi MA, Siddiqui SZ, Rashid U, Iqbal J, et al.

Pak J Pharm Sci, 2018 Jul;31(4(Supplementary)):1501-1510.
PMID: 30058542

N-(Substituted)-5-(1-(4-methoxyphenylsulfonyl)piperidin-4-yl)-4H-1,2,4-triazol-3-ylthio) acetamide were synthesized by following conventional as well as microwave assisted protocol through five consecutive steps under the impact of various reaction conditions to control the reaction time and the yield of product. Starting from 4-methoxybenzenesulfonyl chloride and ethyl isonipecotate, product 3 was obtained which was converted into product 4 by treating with hydrazine hydrate. In step 3, the product 4 was refluxed with methyl isothiocyanate and KOH to yield compound 5 which was finally treated with variety of N-substituted acetamides to yield an array of different new compounds (8a-k). These synthesized compounds were evaluated for their inhibition potential against bovine carbonic anhydrase (bCA-II), acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Compound 8g demonstrated good activity against bCA-II, AChE and BChE with IC50 values of 8.69 ± 0.38 μM, 11.87±0.19 μM and 26.01±0.55 μM respectively. SAR studies assisted with molecular docking were carried out to explore the mode of binding of the compounds against the studied enzymes.
2-Furoic piperazide derivatives as promising drug candidates of type 2 diabetes and Alzheimer's diseases: In vitro and in silico studies

Abbasi MA, Hassan M, Ur-Rehman A, Siddiqui SZ, Hussain G, Shah SAA, et al.

Comput Biol Chem, 2018 Dec;77:72-86.
PMID: 30245349 DOI: 10.1016/j.compbiolchem.2018.09.007

The heterocyclic compounds have been extensively reported for their bioactivity potential. The current research work reports the synthesis of some new multi-functional derivatives of 2-furoic piperazide (1; 1-(2-furoyl)piperazine). The synthesis was initiated by reacting the starting compound 1 with 3,5-dichloro-2-hydroxybenzenesulfonyl chloride (2) in a basic, polar and protic medium to obtain the parent sulfonamide 3 which was then treated with different electrophiles, 4a-g, in a polar and aprotic medium to acquire the designed molecules, 5a-g. These convergent derivatives were evaluated for their inhibitory potential against α-glucosidase, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Acarbose was used as a reference standard for α-glucosidase inhibition while eserine for AChE and BChE inhibition. Some of the synthesized compounds were identified as promising inhibitors of these three enzymes and their bioactivity potentials were also supported by molecular docking study. The most active compounds among the synthetic analogues might be helpful in drug discovery and development for the treatment of type 2 diabetes and Alzhiemer's diseases.
Fulltext Environmental management for dengue control: a systematic review protocol

Mahmud MAF, Abdul Mutalip MH, Lodz NA, Muhammad EN, Yoep N, Hashim MH, et al.

BMJ Open, 2019 05 15;9(5):e026101.
PMID: 31097485 DOI: 10.1136/bmjopen-2018-026101

INTRODUCTION: Dengue is among the most important mosquito-borne diseases, with more than half of the world's population at risk of infection in dengue endemic countries. Environmental management, which includes any activities that involve environmental modification, environmental manipulation and changes to human behaviour have been used to mitigate the risk of dengue transmission. In this protocol, we will integrate the data from various sources to assess the overall effect of environmental management on the incidence of dengue and other entomological indices.
METHODS AND ANALYSES: We will conduct a systematic review of intervention that assess the effect of environmental management on the incidence of dengue and/or entomological indices. We will include any studies that include intervention through environmental management for dengue control, involving environmental modification, environmental manipulation and changes to human behaviour. A comprehensive search will be performed in electronic databases PUBMED, CENTRAL, SCOPUS, Web of Science and relevant research websites such as PROPSERO, WHO ICTRP and ClinicalTrials.gov to identify studies that meet our inclusion criteria. A systematic approach to searching, screening, reviewing and data extraction will be applied based on Preferred Reporting Items for Systematic reviews and Meta-Analysis. Titles, abstract, keywords for eligibility will be examined independently by researchers. The quality of the included studies will be assessed using quality assessment tool for studies with diverse design and Cochrane risk of bias tool. The characteristics of the selected articles will be described based on the study design, types of intervention and outcomes of the study in various countries. These include the types of environmental management intervention methods and the effectiveness of the intervention in reducing dengue cases or incidence and impact on entomological indices.
ETHICS AND DISSEMINATION: We will register this systematic review with the National Medical Research Register, Ministry of Health Malaysia. This protocol also had been registered with the PROSPERO. No ethical approval is necessary, as there will be no collection of primary data. The results will be disseminated though a peer-reviewed publication and conference presentation.
TRIAL REGISTRATION NUMBER: CRD42018092189.
Fulltext Ameliorative Effects of Aquilaria malaccensis Leaves Aqueous Extract on Reproductive Toxicity Induced by Cyclophosphamide in Male Rats

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.
Fulltext Seasonal Dynamics, Record of Ticks Infesting Humans, Wild and Domestic Animals and Molecular Phylogeny of Rhipicephalus microplus in Khyber Pakhtunkhwa Pakistan

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.
Fulltext Synergistic enhancement in the microelectronic properties of poly-(dioctylfluorene) based Schottky devices by CdSe quantum dots

Muhammad F, Tahir M, Zeb M, Kalasad MN, Mohd Said S, Sarker MR, et al.

Sci Rep, 2020 Mar 16;10(1):4828.
PMID: 32179797 DOI: 10.1038/s41598-020-61602-1

This paper reports the potential application of cadmium selenide (CdSe) quantum dots (QDs) in improving the microelectronic characteristics of Schottky barrier diode (SBD) prepared from a semiconducting material poly-(9,9-dioctylfluorene) (F8). Two SBDs, Ag/F8/P3HT/ITO and Ag/F8-CdSe QDs/P3HT/ITO, are fabricated by spin coating a 10 wt% solution of F8 in chloroform and 10:1 wt% solution of F8:CdSe QDs, respectively, on a pre-deposited poly(3-hexylthiophene) (P3HT) on indium tin oxide (ITO) substrate. To study the electronic properties of the fabricated devices, current-voltage (I-V) measurements are carried out at 25 °C in dark conditions. The I-V curves of Ag/F8/P3HT/ITO and Ag/F8-CdSe QDs/P3HT/ITO SBDs demonstrate asymmetrical behavior with forward bias current rectification ratio (RR) of 7.42 ± 0.02 and 142 ± 0.02, respectively, at ± 3.5 V which confirm the formation of depletion region. Other key parameters which govern microelectronic properties of the fabricated devices such as charge carrier mobility (µ), barrier height (ϕb), series resistance (Rs) and quality factor (n) are extracted from their corresponding I-V characteristics. Norde's and Cheung functions are also applied to characterize the devices to study consistency in various parameters. Significant improvement is found in the values of Rs, n, and RR by 3, 1.7, and 19 times, respectively, for Ag/F8-CdSe QDs/P3HT/ITO SBD as compared to Ag/F8/P3HT/ITO. This enhancement is due to the incorporation of CdSe QDs having 3-dimensional quantum confinement and large surface-to-volume area. Poole-Frenkle and Richardson-Schottky conduction mechanisms are also discussed for both of the devices. Morphology, optical bandgap (1.88 ± 0.5 eV) and photoluminescence (PL) spectrum of CdSe QDs with a peak intensity at 556 nm are also reported and discussed.
Fulltext Identifying priority landscapes for conservation of snow leopards in Pakistan

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.
Fulltext Induction of cytotoxicity by Bruguiera gymnorrhiza in human breast carcinoma (MCF-7) cell line via activation of the intrinsic pathway

Chaudhry GE, Rahman NH, Sevakumaran V, Ahmad A, Mohamad H, Zafar MN, et al.

J Adv Pharm Technol Res, 2020 10 10;11(4):233-237.
PMID: 33425710 DOI: 10.4103/japtr.JAPTR_81_20

Breast cancer is among the frequently occurring cancer worldwide. The foremost underline aim of this study was to determine the growth inhibitory effect along with mechanistic study of a Bruguiera gymnorrhiza extract on MCF-7. The cytotoxicity activity was determined by using the MTS assay. Butanol extract exhibited the maximum cytotoxicity activity against the MCF-7 cells with IC50 of 3.39 μg/mL, followed by diethyl ether and methanol extract (IC50 at 16.22 μg/mL and 37.15 μg/mL, respectively) at 72 h. The DeadEndTM Colorimetric Apoptosis Detection System confirmed the induction of apoptosis (via DNA fragmentation) in MCF-7 cells. Both butanol and diethyl ether extracts of B. gymnorrhiza significantly increase the caspase-3 level. However, the diethyl ether extract induced higher caspase-9 levels compared to caspase-8, suggesting that the intrinsic pathway was the major route in the process of apoptosis. Thin-layer chromatography profiling demonstrated the presence of phenolic, terpene, and alkaloid compounds in crude methanol, diethyl ether, and butanol extracts. The phytochemicals present in the extracts of B. gymnorrhiza might have the potential to be a future therapeutic agent against breast cancer.
In silico binding analysis and SAR elucidations of newly designed benzopyrazine analogs as potent inhibitors of thymidine phosphorylase

Taha M, Ismail NH, Imran S, Rahim F, Wadood A, Al Muqarrabun LM, et al.

Bioorg Chem, 2016 10;68:80-9.
PMID: 27474803 DOI: 10.1016/j.bioorg.2016.07.010

Thymidine phosphorylase (TP) is up regulated in wide variety of solid tumors and therefore presents a remarkable target for drug discovery in cancer. A novel class of extremely potent TPase inhibitors based on benzopyrazine (1-28) has been developed and evaluated against thymidine phosphorylase enzyme. Out of these twenty-eight analogs eleven (11) compounds 1, 4, 14, 15, 16, 17, 18, 19, 20, 24 and 28 showed potent thymidine phosphorylase inhibitory potentials with IC50 values ranged between 3.20±0.30 and 37.60±1.15μM when compared with the standard 7-Deazaxanthine (IC50=38.68±4.42μM). Structure-activity relationship was established and molecular docking studies were performed to determine the binding interactions of these newly synthesized compounds. Current studies have revealed that these compounds established stronger hydrogen bonding networks with active site residues as compare to the standard compound 7DX.
Fulltext Xylocarpus Moluccensis Induces Cytotoxicity in Human Hepatocellular Carcinoma HepG2 Cell Line via Activation of the Extrinsic Pathway

Chaudhry GE, Sohimi NKA, Mohamad H, Zafar MN, Ahmed A, Sung YY, et al.

Asian Pac J Cancer Prev, 2021 Feb 01;22(S1):17-24.
PMID: 33576208 DOI: 10.31557/APJCP.2021.22.S1.17

OBJECTIVE: Liver cancer is one of the most common causes of cancer death, with reduced survival rates. The development of new chemotherapeutic agents is essential to find effective cytotoxic drugs that give minimum side effects to the surrounding healthy tissues. The main objective of the present study was to evaluate the cytotoxic effects and mechanism of cell death induced by the crude and diethyl ether extract of Xylocarpus mouccensis on the human hepatocellular carcinoma cell line.
METHODS: The cytotoxicity activity was measured using the MTS assay. The mode of cell death determined by the apoptosis study, DNA fragmentation analysis done by using the TUNEL system. The pathway study or mechanism of apoptosis observed by study caspases 8, 9, 3/7 Glo-caspases method.
RESULTS: In this study, the methanol extracts prepared from leaf Xylocarpus mouccensis leaf produced cytotoxicity effect with IC50 (72hr) < 30µg/ml. The IC50 value at 72 hours exerted by diethyl ether extract of Xylocarpus moluccensis leaf was 0.22 µg/ml, which was more cytotoxic than to that of crude methanol extract. The results obtained by the colorimetric TUNEL system suggest that methanol crude extract of Xylocarpus moluccensis (leaf), diethyl ether extract of Xylocarpus moluccensis (leaf) and methanol extract of Xylocarpus granatum (bark) induced DNA fragmentation in the HepG2 cell line. Besides, the caspase-Glo assay demonstrated that diethyl ether leaf extract of Xylocarpus moluccensis triggered apoptotic cell death via activation of caspases -8, and -3/7 However, no visible activation was noticed for caspase -9. Furthermore, TLC indicates the presence of potential metabolites in an extract of Xylocarpus moluccensis.
CONCLUSION: Thus, the present study suggests the remarkable potential of active metabolites in the extract of Xylocarpus moluccensis as a future therapeutic agent for the treatment of cancer.
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Fulltext Quantitative Ethnobotanical Analysis of Medicinal Plants of High-Temperature Areas of Southern Punjab, Pakistan

Usman M, Ditta A, Ibrahim FH, Murtaza G, Rajpar MN, Mehmood S, et al.

Plants (Basel), 2021 Sep 22;10(10).
PMID: 34685784 DOI: 10.3390/plants10101974

Lack of proper infrastructure and the poor economic conditions of rural communities make them dependent on herbal medicines. Thus, there is a need to obtain and conserve the historic and traditional knowledge about the medicinal importance of different plants found in different areas of the world. In this regard, a field study was conducted to document the medicinal importance of local plants commonly used by the inhabitants of very old historic villages in Southern Punjab, Pakistan. In total, 58 plant species were explored, which belonged to 28 taxonomic families, as informed by 200 experienced respondents in the study area. The vernacular name, voucher number, plant parts used, and medicinal values were also documented for each species. Among the documented species, Poaceae remained the most predominant family, followed by Solanaceae and Asteraceae. The local communities were dependent on medicinal plants for daily curing of several ailments, including asthma, common cold, sore throat, fever, cardiovascular diseases, and digestive disorders. Among the reported species, leaves and the whole plant remained the most commonly utilized plant parts, while extracts (38.8%) and pastes (23.9%) were the most popular modes of utilization. Based on the ICF value, the highest value was accounted for wound healing (0.87), followed by skincare, nails, hair, and teeth disorders (0.85). The highest RFC value was represented by Acacia nilotica and Triticum aestivum (0.95 each), followed by Azadirachta indica (0.91). The highest UV was represented by Conyza canadensis and Cuscuta reflexa (0.58 each), followed by Xanthium strumarium (0.37). As far as FL was concerned, the highest value was recorded in the case of Azadirachta indica (93.4%) for blood purification and Acacia nilotica (91.1%) for sexual disorders. In conclusion, the local inhabitants primarily focus on medicinal plants for the treatment of different diseases in the very old historic villages of Southern Punjab, Pakistan. Moreover, there were various plants in the study area that have great ethnobotanical potential to treat various diseases, as revealed through different indices.
Fulltext Low-Velocity Impact Analysis of Pineapple Leaf Fiber (PALF) Hybrid Composites

Najeeb MI, Hameed Sultan MT, Md Shah AU, Muhammad Amir SM, Safri SNA, Jawaid M, et al.

Polymers (Basel), 2021 Sep 21;13(18).
PMID: 34578095 DOI: 10.3390/polym13183194

The low-velocity impact behaviour of pineapple leaf fiber, PALF reinforce epoxy composite (P), PALF hybrid (GPG), and four-layer woven glass fiber (GGGG) composite was investigated. As for post-impact analysis, the damage evaluation was assessed through photographic images and X-ray computed tomography, using CT scan techniques. The key findings from this study are that a positive hybrid effect of PALF as a reinforcement was seen where the GPG shows the delayed time taken for damage initiation and propagation through the whole sample compared to GGGG. This clearly shows that the addition of fibers does have comparable composite properties with a fully synthetic composite. Through the visual inspection captured by photographic image, the presence of woven fiber glass mat in GPG presents a different damage mode compared to P. Moreover, CT scan results show extended internal damage at the cross-section of all impacted composite.
Development of an extended model for the permeation of environmentally hazardous CO2 gas across asymmetric hollow fiber composite membranes

Jamil A, Ching OP, Iqbal T, Rafiq S, Zia-Ul-Haq M, Shahid MZ, et al.

J Hazard Mater, 2021 Sep 05;417:126000.
PMID: 33992016 DOI: 10.1016/j.jhazmat.2021.126000

This study presents an extended thermodynamic and phenomenological combined model to mitigate the environmental hazardous acid gas over composite membranes. The model has been applied to an acid gas such as carbon dioxide (CO2) for its permeation through polyetherimide incorporated montmorillonite (Mt) nanoparticles hollow fiber asymmetric composite membranes. The well-established non-equilibrium lattice fluid (NELF) model for penetrating low molecular weight penetrant in a glassy polyetherimide (PEI) was extended to incorporate the other important polymer/filler system features such as tortuosity in acid gas diffusion pathways resulted from layered filler aspect ratio and concentration. The model mentioned above predicts the behavior of acid gas in PEI-Mt composite membranes based on thermodynamic characteristics of CO2 and PEI and tortuosity due to Mt. The calculated results are compared to experimentally determined values of CO2 permeability through PEI-Mt composite asymmetric hollow fiber membranes at varying transmembrane pressures and Mt concentrations. A reasonable agreement was found between the model predicted behavior and experimentally determined data in terms of CO2 solubility, Mt concentration and aspect ratio were calculated based on average absolute relative error (%AARE). The proposed modified model efficiently predicts the CO2 permeance across MMMs up to 3 wt% Mt loadings and 6 bar pressure with ± 10%AARE.
Fulltext Induction of Apoptosis by Acanthaster planci sp., and Diadema setosum sp., Fractions in Human Cervical Cancer Cell Line, HeLa

Chaudhry GE, Islamiah M, Zafar MN, Bakar K, Aziz N, Saidin J, et al.

Asian Pac J Cancer Prev, 2021 May 01;22(5):1365-1373.
PMID: 34048163 DOI: 10.31557/APJCP.2021.22.5.1365

Cancer is an uncontrolled multiplication of cells. The desire efficacy and severe toxicity of current anticancer drugs urge exploring and investigating a better alternative to existing chemotherapeutics. Natural products of marine origin are excellent sources of potential new drugs of enhanced biological activities.
OBJECTIVES: Thus, the cytotoxic effects along with investigating the mode of cell death exerted by fractions, AP-9, AP-THR, DS-8 and DS-9 fraction of Acanthaster planci, Diadema setosum sp., on the human cervical cancer cell line, HeLa.
METHODS: The cytotoxicity of fractions has determined by using an MTS assay. The early and late apoptosis was studied by using the High content Screening (HCS) instrument.
RESULTS: The four fractions produced effective cytotoxicity effects with IC50 values at 72hr of less than 20 μg/ml in the order of AP-9 > DS-9 > APTHR-9 > DS-8. The fraction s exhibited cytotoxicity via mediating apoptotic mode of cell death. The early apoptosis by exposure of phosphatidylserine to the outer leaflet of the plasma membrane and late apoptosis due to the presence of green stain (DNA fragmentation) in treated cells.
CONCLUSION: The potent bioactive compounds might be responsible for inducing apoptosis in cancer cells and, thus, the potential to be a successful candidate for exploring upcoming chemotherapeutic drugs.
Radioprotective Role of Natural Polyphenols: From Sources to Mechanisms

Adnan M, Rasul A, Shah MA, Hussain G, Asrar M, Riaz A, et al.

Anticancer Agents Med Chem, 2022;22(1):30-39.
PMID: 33874875 DOI: 10.2174/1871520621666210419095829

The identification and development of radioprotective agents have emerged as a subject matter of research during recent years due to the growing usage of ionizing radiation in different areas of human life. Previous work on synthetic radioprotectors has achieved limited progress because of the numerous issues associated with toxicity. Compounds extracted from plants have the potential to serve as lead candidates for developing ideal radioprotectors due to their low cost, safety, and selectivity. Polyphenols are the most abundant and commonly dispersed group of biologically active molecules possessing a broad range of pharmacological activities. Polyphenols have displayed efficacy for radioprotection during various investigations and can be administered at high doses with lesser toxicity. Detoxification of free radicals, modulating inflammatory responses, DNA repair, stimulation of hematopoietic recovery, and immune functions are the main mechanisms for radiation protection with polyphenols. Epicatechin, epigallocatechin-3-gallate, apigenin, caffeic acid phenylethylester, and silibinin provide cytoprotection together with the suppression of many pro-inflammatory cytokines owing to their free radical scavenging, anti-oxidant, and anti-inflammatory properties. Curcumin, resveratrol, quercetin, gallic acid, and rutin's radioprotective properties are regulated primarily by the direct or indirect decline in cellular stress. Thus, polyphenols may serve as potential candidates for radioprotection in the near future; however, extensive investigations are still required to better understand their protection mechanisms.
Fulltext The impact of aqueous and N-hexane extracts of three Fabaceae species on seed germination and seedling growth of some broadleaved weed species

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.
REVIEW-Novel corona virus disease (COVID-19): An updated review on epidemiology, pathogenicity, clinical course, treatments, migrant health concerns and risk factors predictions

Anis S, Masood Khan M, Ali Z, Khan A, Arsalan HM, Naeem S, et al.

Pak J Pharm Sci, 2021 Sep;34(5):1821-1836.
PMID: 34803021

The COVID-19 epidemic is considered the most important health disaster of the century and the largest humanitarian crisis since World War II. In December 2019, a new respiratory disease/disorder was discovered in Wuhan, Hubei province, China and World Health Organization named it COVID-19 (coronavirus 2019). It has been diagnosed with a new class of corona virus, called SARS-CoV-2 (a serious respiratory disease). According to the history of human civilization it is affected by the incidence of disease outbreaks caused by the number of viruses. Covid-19 is rapidly spreading across the globe, due to which mankind faces major health, economic, environmental and social challenges. The outbreak of coronavirus is seriously affecting the global economy. Almost all nations have problems limiting the spread of the disease by screening and treating patients, setting up suspects by keeping in touch, blocking large gatherings, maintaining full or partial closure etc. This paper describes the impact of COVID-19 on society and the global environment, and the ways in which the disease is likely to be controlled have been discussed.
Fulltext Characterization of various acrylate based artificial teeth for denture fabrication

Muhammad N, Sarfraz Z, Zafar MS, Liaqat S, Rahim A, Ahmad P, et al.

J Mater Sci Mater Med, 2022 Jan 24;33(2):17.
PMID: 35072817 DOI: 10.1007/s10856-022-06645-8

Acrylic resins-based artificial teeth are frequently used for the fabrication of dentures has and contribute a very strong share in the global market. However, the scientific literature reporting the comparative analysis data of various artificial teeth is scarce. Focusing on that, the present study investigated various types of commercially available artificial teeth, composed of polymethyl methacrylate (PMMA). Artificial teeth are characterized for chemical analysis, morphological features, thermal analysis, and mechanical properties (surface hardness, compressive strength). Different types of artificial teeth showed distinct mechanical (compression strength, Vickers hardness) and thermal properties (thermal gravimetric analysis) which may be attributed to the difference in the content of PMMA and type and quantity of different fillers in their composition. Thermogravimetric analysis (TGA) results exhibited that vinyl end groups of PMMA degraded above 200 °C, whereas 340-400 °C maximum degradation temperature was measured by differential thermal analysis (DTA) for all samples. Crisma brand showed the highest compressive strength and young modulus (88.6 MPa and 1654 MPa) while the lowest value of Vickers hardness was demonstrated by Pigeon and Vital brands. Scanning electron microscope (SEM) photographs showed that Crisma, Pigeon, and Vital exhibited characteristics of a brittle fracture; however, Artis and Well bite brands contained elongated voids on their surfaces. According to the mechanical analysis and SEM data, Well bite teeth showed a significantly higher mechanical strength compared to other groups. However, no considerable difference was observed in Vickers hardness of all groups. Graphical abstract.
Synthesis and Computational Exploration of Morpholine Bearing Halogenated Sulfonamides as Potential Tyrosinase Inhibitors

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.

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