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  1. Fulltext Aqueous Extract of Nypa fruticans Wurmb. Vinegar Alleviates Postprandial Hyperglycemia in Normoglycemic Rats
    Yusoff NA, Ahmad M, Al-Hindi B, Widyawati T, Yam MF, Mahmud R, et al.
    Nutrients, 2015 Aug;7(8):7012-26.
    PMID: 26308046 DOI: 10.3390/nu7085320
    Nypa fruticans Wurmb. vinegar, commonly known as nipa palm vinegar (NPV) has been used as a folklore medicine among the Malay community to treat diabetes. Early work has shown that aqueous extract (AE) of NPV exerts a potent antihyperglycemic effect. Thus, this study is conducted to evaluate the effect of AE on postprandial hyperglycemia in an attempt to understand its mechanism of antidiabetic action. AE were tested via in vitro intestinal glucose absorption, in vivo carbohydrate tolerance tests and spectrophotometric enzyme inhibition assays. One mg/mL of AE showed a comparable outcome to the use of phloridzin (1 mM) in vitro as it delayed glucose absorption through isolated rat jejunum more effectively than acarbose (1 mg/mL). Further in vivo confirmatory tests showed AE (500 mg/kg) to cause a significant suppression in postprandial hyperglycemia 30 min following respective glucose (2 g/kg), sucrose (4 g/kg) and starch (3 g/kg) loadings in normal rats, compared to the control group. Conversely, in spectrophotometric enzymatic assays, AE showed rather a weak inhibitory activity against both α-glucosidase and α-amylase when compared with acarbose. The findings suggested that NPV exerts its anti-diabetic effect by delaying carbohydrate absorption from the small intestine through selective inhibition of intestinal glucose transporters, therefore suppressing postprandial hyperglycemia.
  2. Retraction Note to: Estimation of Anticipated Performance Index and Air Pollution Tolerance Index and of vegetation around the marble industrial areas of Potwar region: bioindicators of plant pollution response
    Noor MJ, Sultana S, Fatima S, Ahmad M, Zafar M, Sarfraz M, et al.
    Environ Geochem Health, 2017 06;39(3):705.
    PMID: 26932557 DOI: 10.1007/s10653-016-9812-6
  3. A scaffoldless technique for self-generation of three-dimensional keratinospheroids on liquid crystal surfaces
    Soon CF, Thong KT, Tee KS, Ismail AB, Denyer M, Ahmad MK, et al.
    Biotech Histochem, 2016 May;91(4):283-95.
    PMID: 27008034 DOI: 10.3109/10520295.2016.1158865
    We describe a new scaffold-free three-dimensional (3D) cell culture model using cholesteryl ester based lyotropic liquid crystal (LC) substrates. Keratinocytes were deposited randomly on the LC surface where they self-assembled into 3D microtissues or keratinospheroids. The cell density required to form spheroids was optimized. We investigated cell viability using dead/live cell assays. The adhesion characteristics of cells within the microtissues were determined using histological sectioning and immunofluorescence staining. Fourier transform infrared spectroscopy (FTIR) was used to characterize the biochemistry of the keratinospheroids. We found that both cells and microtissues could migrate on the LC surface. The viability study indicated approximately 80% viability of cells in the microtissues up to 20 days of culture. Strong intercellular adhesion was observed in the stratification of the multi-layered microspheroids using field emission-scanning electron microscopy (FE-SEM) and histochemical staining. The cytoskeleton and vinculins of the cells in the microtissues were expressed diffusely, but the microtissues were enriched with lipids and nucleic acids, which indicates close resemblance to the conditions in vivo. The basic 3D culture model based on LC may be used for cell and microtissue migration studies in response to cytochemical treatment.
  4. Ethnomedicinal uses of plants for the treatment of snake and scorpion bite in Northern Pakistan
    Butt MA, Ahmad M, Fatima A, Sultana S, Zafar M, Yaseen G, et al.
    J Ethnopharmacol, 2015 Jun 20;168:164-81.
    PMID: 25818693 DOI: 10.1016/j.jep.2015.03.045
    Medicinal plants represent one of the most accessible resources available for snake and scorpion bite among the rural communities of Northern Pakistan. This first ethno-botanical study aimed to document the indigenous knowledge and practices of using plants for snake and scorpion bite disorders in Northern Pakistan.
  5. Fulltext Nutlin-3 sensitizes nasopharyngeal carcinoma cells to cisplatin-induced cytotoxicity
    Voon YL, Ahmad M, Wong PF, Husaini R, Ng WT, Leong CO, et al.
    Oncol Rep, 2015 Oct;34(4):1692-700.
    PMID: 26252575 DOI: 10.3892/or.2015.4177
    The small-molecule inhibitor of p53-Mdm2 interaction, Nutlin-3, is known to be effective against cancers expressing wild-type (wt) p53. p53 mutations are rare in nasopharyngeal carcinoma (NPC), hence targeting disruption of p53-Mdm2 interaction to reactivate p53 may offer a promising therapeutic strategy for NPC. In the present study, the effects of Nutlin-3 alone or in combination with cisplatin, a standard chemotherapeutic agent, were tested on C666-1 cells, an Epstein-Barr virus (EBV)-positive NPC cell line bearing wt p53. Treatment with Nutlin-3 activated the p53 pathway and sensitized NPC cells to the cytotoxic effects of cisplatin. The combined treatment also markedly suppressed soft agar colony growth formation and increased apoptosis of NPC cells. The effect of Nutlin-3 on NPC cells was inhibited by knockdown of p53, suggesting that its effect was p53-dependent. Extended treatment with increasing concentrations of Nutlin-3 did not result in emergence of p53 mutations in the C666-1 cells. Collectively, the present study revealed supportive evidence of the effectiveness of combining cisplatin and Nutlin-3 as a potential therapy against NPC.
  6. Vasorelaxant and chemical fingerprint studies of Citrus reticulatae pericarpium extracts
    Tan CS, Loh YC, Ch'ng YS, Ng CH, Yeap ZQ, Ahmad M, et al.
    J Ethnopharmacol, 2019 Mar 25;232:135-144.
    PMID: 30543913 DOI: 10.1016/j.jep.2018.12.014
    ETHNOPHARMACOLOGICAL RELEVANCE: Citrus reticulatae Pericarpium (Chen pi) was widely used as an important ingredient in the prescription of TCM to treat phlegm fluid retention type hypertension. Since Chen pi is involved in treatment as antihypertensive TCM formula, we have reasonable expectation in believing that it might possess vasorelaxant activity.

    AIM OF THE STUDY: This study is designed to investigate the vasorelaxant effect of Chen pi and to study its pharmacology effects.

    MATERIALS AND METHODS: The vasorelaxant effect of water extract of Chen pi (CRW) were evaluated on thoracic aortic rings isolated from Sprague Dawley rats. The fingerprint of Chen pi and the extracts were developed with quantification of hesperidin content by HPTLC.

    RESULTS: CRW exhibited the strongest vasorelaxant activity. CRW caused the relaxation of the phenylephrine pre-contracted aortic rings in the presence and absence of endothelium as well as in potassium chloride pre-contracted endothelium-intact aortic ring. The incubation of propranolol (β-adrenergic receptor blocker), atropine (muscarinic receptor blocker), Nω-nitro-L-arginine methyl ester (NO synthase inhibitor), ODQ (sGC inhibitor), indomethacin (COX inhibitor), 4-aminopyridine (KV blocker), barium chloride (Kir blocker), and glibenclamide (KATP blocker) significantly reduced the vasorelaxant effects of CRW. CRW was also found to be active in reducing Ca2+ releases from the sarcoplasmic reticulum and suppressing the voltage-operated calcium channels.

    CONCLUSION: The vasorelaxant effect of CRW on rat aorta involves NO/sGC, calcium and potassium channels, muscarinic and β-adrenergic receptors.

  7. Fulltext The role of social support and spiritual wellbeing in predicting suicidal ideation among marginalized adolescents in Malaysia
    Ibrahim N, Che Din N, Ahmad M, Amit N, Ghazali SE, Wahab S, et al.
    BMC Public Health, 2019 Jun 13;19(Suppl 4):553.
    PMID: 31196009 DOI: 10.1186/s12889-019-6861-7
    BACKGROUND: The high number of adolescents and young adults harbouring suicidal ideation, as reported by the Ministry of Health Malaysia, is alarming. This cross-sectional study aims to examine the association between social support and spiritual wellbeing in predicting suicidal ideation among Malaysian adolescents.

    METHODS: A total of 176 adolescents in selected urban areas in the states of Wilayah Persekutuan and Selangor were selected. The Suicide Ideation Scale (SIS) was used to measure the level of severity or tendency of suicidal ideation. The Multidimensional Scale of Perceived Social Support (MSPSS) was used to measure the perceived social support received by the respondent while the Spiritual Wellbeing Scale (SWBS) was used to measure the religious wellbeing (RWB), the existential wellbeing (EWB) and the overall score of spiritual wellbeing (SWB).

    RESULTS: The study found that both RWB and EWB showed significant negative correlation with suicidal ideation. Similarly, support from family and friends also showed a negative correlation with suicidal ideation. Further analysis using multiple regressions showed that RWB and SWB, and family support predict suicidal ideation in adolescents.

    CONCLUSION: Spiritual wellbeing in combination with family support plays a major role in predicting suicidal ideation. Therefore, intervention for encompassing spirituality and family support may contribute to a more positive outcome in suicidal adolescents.

  8. Fulltext Cutaneous leishmaniasis-Awareness, knowledge and practices among general population in rural and urban areas in Malakand region, Pakistan
    Khan W, Khan I, Ullah H, Zain SNM, Panhwar WA, Mehmood SA, et al.
    Braz J Biol, 2021;82:e238665.
    PMID: 33787717 DOI: 10.1590/1519-6984.238665
    Malakand region is an endemic area for cutaneous leishmaniasis (CL). However, there are limited number of studies of this disease in Pakistan. Therefore, a study was conducted to understand the level of awareness attitude and practice among the residents of Makaland towards CL and the disease vectors. This study adopted a cross-sectional approach with a total of 400 respondents (n=93 rural and n= 307 urban). Overall, the population in Malakand region (61.2%) were well-informed in the role of sand fly in transmitting diseases, but most lack knowledge on the vector's behavior and almost a quarter (24.5%) were unable to provide knowledge on proper control measures. Alarmingly, the practice and attitudes of the general population was not satisfactory as close to half (49.8%) of the population did adopt any control method. This study calls for increase in awareness through health education campaign to reduce the risk of cutaneous leishmaniasis outbreaks in the future.
  9. Chitosan based thermosensitive injectable hydrogels for controlled delivery of loxoprofen: development, characterization and in-vivo evaluation
    Ahmad U, Sohail M, Ahmad M, Minhas MU, Khan S, Hussain Z, et al.
    Int J Biol Macromol, 2019 May 15;129:233-245.
    PMID: 30738157 DOI: 10.1016/j.ijbiomac.2019.02.031
    Oral drug delivery is natural, most acceptable and desirable route for nearly all drugs, but many drugs like NSAIDs when delivered by this route cause gastrointestinal irritation, gastric bleeding, ulcers, and many undesirable effects which limits their usage by oral delivery. Moreover, it is almost impossible to control the release of a drug in a targeted location in body. We developed thermo-responsive chitosan-co-poly(N-isopropyl-acrylamide) injectable hydrogel as an alternative for the gastro-protective and controlled delivery of loxoprofen sodium as a model drug. A free radical polymerization technique was used to synthesize thermo-responsive hydrogel by cross-linking chitosan HCl with NIPAAM using glutaraldehyde as cross-linker. Confirmation of crosslinked hydrogel structure was done by Fourier transform infrared spectra (FTIR). The thermal stability of hydrogel was confirmed through thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC). The scanning electron microscopy (SEM) was performed to evaluate the structural morphology of cross-linked hydrogel. To evaluate the rheological behavior of hydrogel with increasing temperature, rheological study was performed. Swelling and in vitro drug release studies were carried out under various temperature and pH conditions. The swelling study revealed that maximum swelling was observed at low pH (pH 1.2) and low temperature (25 °C) compared to the high range of pH and temperature and it resulted in quick release of the drug. The high range of pH (7.4) and temperature (37 °C) however caused controlled release of the drug. The in vivo evaluation of the developed hydrogel in rabbits demonstrated the controlled release behavior of fabricated system.
  10. Fulltext Reliability and Validity of the Malay Mindful Eating Questionnaire (MEQ-M) among Overweight and Obese Adults
    Abdul Basir SM, Abdul Manaf Z, Ahmad M, Abdul Kadir NB, Ismail WNK, Mat Ludin AF, et al.
    Int J Environ Res Public Health, 2021 01 24;18(3).
    PMID: 33498903 DOI: 10.3390/ijerph18031021
    The Mindful Eating Questionnaire is a reliable tool for the assessment of mindful eating behavior among the general population. This study aimed to determine the reliability and validity of The Malay Mindful Eating Questionnaire (MEQ-M) in a sample of overweight and obese adults. This is a cross-sectional survey which involved 144 overweight and obese adults in a selected public university. After linguistic validation of the Malay version of the MEQ, exploratory factor analysis (EFA) with varimax rotation was performed on the scale constructs. The psychometric properties of the MEQ were assessed through Cronbach's alpha and intraclass correlation coefficient (ICC) analysis. The EFA of the MEQ produced a seven-dimensional model (58.8% of overall variances). The concurrent validity analysis between total MEQ scores and total Mindfulness Attention Awareness Scale (MAAS) scores indicated a weak non-significant correlation (p = 0.679). The internal consistency reliability of the MEQ was reasonable (Cronbach's α = 0.64). The agreement stability of the MEQ over eight weeks was poor (ICC = 0.10). In conclusion, the psychometric properties of the Malay-translated MEQ are acceptable through construct validity and internal consistency reliability tests. This instrument may be used for assessing mindful eating habits in the Malaysian population, especially among overweight and obese adults.
  11. Safety assessment of methanol extract of red dragon fruit (Hylocereus polyrhizus): acute and subchronic toxicity studies
    Hor SY, Ahmad M, Farsi E, Yam MF, Hashim MA, Lim CP, et al.
    Regul Toxicol Pharmacol, 2012 Jun;63(1):106-14.
    PMID: 22440551 DOI: 10.1016/j.yrtph.2012.03.006
    Recently, the fruits of Hylocereus polyrhizus, known as red dragon fruit, have received much attention from growers worldwide. However, there is little toxicological information regarding the safety of repeated exposure to these fruits. The present study evaluated the potential toxicity of a methanol extract of H. polyrhizus fruit after acute and subchronic administration in rats. In the acute toxicity study, single doses of fruit extract (1250, 2500 and 5000 mg/kg) were administered to rats by oral gavage, and the rats were then monitored for 14 days. In the subchronic toxicity study, the fruit extract was administered orally to rats at doses of 1250, 2500 and 5000 mg/kg/day for 28 days. There was no mortality or signs of acute or subchronic toxicity. There was no significant difference in body weight, relative organ weight or hematological parameters in the subchronic toxicity study. Biochemical analysis showed some significant changes, including creatinine, globulin, total protein and urea levels. No abnormality of internal organs was observed between treatment and control groups. The lethal oral dose of the fruit extract is more than 5000 mg/kg and the no-observed-adverse-effect level (NOAEL) of the extract for both male and female rats is considered to be 5000 mg/kg per day for 28 days.
  12. Synthesis of biodiesel from non-edible (Brachychiton populneus) oil in the presence of nickel oxide nanocatalyst: Parametric and optimisation studies
    Dawood S, Koyande AK, Ahmad M, Mubashir M, Asif S, Klemeš JJ, et al.
    Chemosphere, 2021 Sep;278:130469.
    PMID: 33839393 DOI: 10.1016/j.chemosphere.2021.130469
    The present study defines a novel green method for the synthesis of the nickel oxide nanocatalyst by using an aqueous latex extract of the Ficus elastic. The catalyst was examined for the conversion of novel Brachychiton populneus seed oil (BPSO) into biodiesel. The Brachychiton populneus seeds have a higher oil content (41 wt%) and free fatty acid value (3.8 mg KOH/g). The synthesised green nanocatalyst was examined by the Fourier transform infrared (FT-IR) spectroscopy, energy dispersive X-Ray (EDX) spectroscopy, X-Ray diffraction (XRD) spectroscopy and scanning electron microscopy (SEM). The obtained results show that the synthesised green nanocatalyst was 22-26 nm in diameter and spherical-cubic in shape with a higher rate of catalytic efficiency. It was utilised further for the conversion of BPSO into biofuel. Due to the high free fatty acid value, the biodiesel was synthesised by the two-step process, i.e., pretreatment of the BPSO by means of acid esterification and then followed by the transesterification reaction. The acidic catalyst (H2SO4) was used for the pretreatment of BPSO. The optimum condition for the transesterification of the pretreated BPSO was 1:9 of oil-methanol molar ratio, 2.5 wt % of prepared nanocatalyst concentration and 85 °C of reaction temperature corresponding to the highest biodiesel yield of 97.5 wt%. The synthesised biodiesel was analysed by the FT-IR and GC-MS technique to determine the chemical composition of fatty acid methyl esters. Fuel properties of Brachychiton populneus seed oil biodiesel (BPSOB) were also examined, compared, and it falls in the prescribed range of ASTM standards.
  13. Fulltext Development of a luciferase/luciferin cell proliferation (XenoLuc) assay for real-time measurements of Gfp-Luc2-modified cells in a co-culture system
    Teow SY, Liew K, Che Mat MF, Marzuki M, Abdul Aziz N, Chu TL, et al.
    BMC Biotechnol, 2019 06 14;19(1):34.
    PMID: 31200673 DOI: 10.1186/s12896-019-0528-4
    BACKGROUND: In vitro modelling of cancer cells is becoming more complex due to prevailing evidence of intimate interactions between cancer cells and their surrounding stroma. A co-culture system which consists of more than one cell type is physiologically more relevant and thus, could serve as a useful model for various biological studies. An assay that specifically detects the phenotypic changes of cancer cells in a multi-cellular system is lacking for nasopharyngeal carcinoma (NPC).

    RESULTS: Here, we describe a luciferase/luciferin (XenoLuc) assay that could specifically measure changes in the proliferation of cancer cells in the co-culture system using two modified NPC patient-derived tumour xenograft (PDTXs) cells: Xeno284-gfp-luc2 and XenoB110-gfp-luc2. Through this assay, we are able to show that the growth of NPC xenograft cells in both two-dimensional (2D) and three-dimensional (3D) models was enhanced when co-cultured with normal human dermal fibroblasts (NHDFs). In addition, potential applications of this assay in in vitro drug or inhibitor screening experiments are also illustrated.

    CONCLUSIONS: XenoLuc assay is specific, sensitive, rapid and cost-effective for measuring the growth of luciferase-expressing cells in a co- or multiple-culture system. This assay may also be adapted for tumour microenvironment studies as well as drug screening experiments in more complex 3D co-culture systems.

  14. Carboxymethyl Cellulose Hydrogel Based Formulations of Zinc Hydroxide Nitrate-Sodium Dodecylsulphate-Bispyribac Nanocomposite: Advancements in Controlled Release Formulation of Herbicide
    Mohd Sharif SN, Hashim N, Md Isa I, Abu Bakar S, Idris Saidin M, Syahrizal Ahmad M, et al.
    J Nanosci Nanotechnol, 2021 12 01;21(12):5867-5880.
    PMID: 34229781 DOI: 10.1166/jnn.2021.19499
    The usefulness of carboxymethyl cellulose (CMC) as a matrix material in enhancing the controlled release formulations of bispyribac (BP) herbicide from the interlayer gallery of zinc hydroxide nitratesodium dodecylsulphate-bispyribac (ZHN-SDS-BP) nanocomposite was investigated. The CMC coated nanocomposite, ZHN-SDS-BP-CMC was characterised using several instruments for the determination of its physicochemical properties. The release rates of the BP were measured using a UV spectrophotometer, and the aqueous solutions containing PO3-₄ , SO2-₄ and Cl- were selected as release media in the release studies so as to mimic the real conditions of environmental soil. Significant release time delays, triggered by the gelation forming ability and hygroscopic nature of CMC, were observed in all release media, and the release processes were found to behave in a concentration-dependent manner in all release media. Fitting the release data into several kinetic models demonstrated that release in aqueous solutions of Na₃PO₄ and Na₂SO₄ was governed by pseudo second order processes, whereas the release in an aqueous NaCl solution was governed by the parabolic diffusion kinetic model. The potential of CMC in prolonging the release of BP from ZHN-SDS-BP-CMC can potentially help in reducing the pollution resulting from the overuse of pesticides.
  15. Fulltext Synthesis and α-Glucosidase Inhibition Activity of 2-[3-(Benzoyl/4-bromobenzoyl)-4-hydroxy-1,1-dioxido-2H-benzo[e][1,2]thiazin-2-yl]-N-arylacetamides: An In Silico and Biochemical Approach
    Saddique FA, Aslam S, Ahmad M, Ashfaq UA, Muddassar M, Sultan S, et al.
    Molecules, 2021 May 20;26(10).
    PMID: 34065194 DOI: 10.3390/molecules26103043
    Diabetes mellitus (DM) is a chronic disorder and has affected a large number of people worldwide. Insufficient insulin production causes an increase in blood glucose level that results in DM. To lower the blood glucose level, various drugs are employed that block the activity of the α-glucosidase enzyme, which is considered responsible for the breakdown of polysaccharides into monosaccharides leading to an increase in the intestinal blood glucose level. We have synthesized novel 2-(3-(benzoyl/4-bromobenzoyl)-4-hydroxy-1,1-dioxido-2H-benzo[e][1,2]thiazin-2-yl)-N-arylacetamides and have screened them for their in silico and in vitro α-glucosidase inhibition activity. The derivatives 11c, 12a, 12d, 12e, and 12g emerged as potent inhibitors of the α-glucosidase enzyme. These compounds exhibited good docking scores and excellent binding interactions with the selected residues (Asp203, Asp542, Asp327, His600, Arg526) during in silico screening. Similarly, these compounds also showed good in vitro α-glucosidase inhibitions with IC50 values of 30.65, 18.25, 20.76, 35.14, and 24.24 μM, respectively, which were better than the standard drug, acarbose (IC50 = 58.8 μM). Furthermore, a good agreement was observed between in silico and in vitro modes of study.
  16. Selective dual cholinesterase inhibitors from Aconitum laeve
    Ahmad H, Ahmad S, Shah SAA, Khan HU, Khan FA, Ali M, et al.
    J Asian Nat Prod Res, 2018 Feb;20(2):172-181.
    PMID: 28463565 DOI: 10.1080/10286020.2017.1319820
    New lycoctonine-type dual cholinesterase inhibitor, swatinine-C (1), along with three known norditerpenoid alkaloids, hohenackerine (2), aconorine (5) and lappaconitine (6) and two synthetically known but phytochemically new benzene derivatives, methyl 2-acetamidobenzoate (3) and methyl 4-[2-(methoxycarbonyl)anilino]-4-oxobutanoate (4), was isolated from the roots of A. laeve. Structures of new and known compounds (1-6) were established on the basis of latest spectroscopic techniques and by close comparison with the data available in literature. In vitro, compounds (1-6) were tested against AChE and BChE inhibitory activities. Compounds 1 and 2 showed competitive inhibition against AChE (IC50 = 3.7 μM, 4.53 μM) and BChE (IC50 = 12.23 μM, 9.94 μM), respectively. Compounds 5 and 6 showed promising noncompetitive type of inhibitory profile against AChE (IC50 = 2.51 and 6.13 μM) only. Compounds 3 and 4 showed weak inhibitory profile against both AChE and BChE.
  17. Antioxidant and anticholinesterase potential of diterpenoid alkaloids from Aconitum heterophyllum
    Ahmad H, Ahmad S, Shah SAA, Latif A, Ali M, Khan FA, et al.
    Bioorg Med Chem, 2017 07 01;25(13):3368-3376.
    PMID: 28457693 DOI: 10.1016/j.bmc.2017.04.022
    Extensive chromatographic separations performed on the basic (pH=8-10) chloroform soluble fraction of Aconitum heterophyllum resulted in the isolation of three new diterpenoid alkaloids, 6β-Methoxy, 9β-dihydroxylheteratisine (1), 1α,11,13β-trihydroxylhetisine (2), 6,15β-dihydroxylhetisine (3), and the known compounds iso-atisine (4), heteratisine (5), hetisinone (6), 19-epi-isoatisine (7), and atidine (8). Structures of the isolated compounds were established by means of mass and NMR spectroscopy as well as single crystal X-ray crystallography. Compounds 1-8 were screened for their antioxidant and enzyme inhibition activities followed by in silico studies to find out the possible inhibitory mechanism of the tested compounds. This work is the first report demonstrating significant antioxidant and anticholinesterase potentials of diterpenoid alkaloids isolated from a natural source.
  18. Norditerpenoid alkaloids of Delphinium denudatum as cholinesterase inhibitors
    Ahmad H, Ahmad S, Ali M, Latif A, Shah SAA, Naz H, et al.
    Bioorg Chem, 2018 08;78:427-435.
    PMID: 29698893 DOI: 10.1016/j.bioorg.2018.04.008
    Three new norditerpenoids alkaloids, 1β-hydroxy,14β-acetyl condelphine (1), jadwarine-A (2), jadwarine-B (3) along with two known alkaloids isotalatizidine hydrate (4) and dihydropentagynine (5) were isolated from medicinal plant Delphinium denudatum. The structures of natural products 1-5 were established on the basis of HR-EIMS, 1H and 13C NMR (1D & 2D) spectroscopic data as well as by comparison from literature data. The structures of compound 1 and 4 were also confirmed by single crystal X-ray diffraction studies. In-vitro AChE and BChE enzyme inhibitory activities of compounds 1-5 and molecular docking studies were performed to investigate the possible molecular inhibitory mechanism of the isolated natural products. Compound 2, 4 and 5 showed competitive inhibitory effects by inhibiting AChE and BChE, respectively, while 1 and 3 showed non-competitive inhibition. This work is the first report that provides a supporting evidence about the use of constituents of Delphinium denudatum in cerebral dementia and Alzheimer diseases.
  19. Synthesis, X-ray crystal and monoamine oxidase inhibitory activity of 4,6-dihydrobenzo[c]pyrano[2,3-e][1,2]thiazine 5,5-dioxides: In vitro studies and docking analysis
    Ahmad S, Jalil S, Zaib S, Aslam S, Ahmad M, Rasul A, et al.
    Eur J Pharm Sci, 2019 Apr 01;131:9-22.
    PMID: 30735822 DOI: 10.1016/j.ejps.2019.02.007
    We report the synthesis and biological evaluation of two new series of 2-amino-6-benzyl-4-phenyl-4,6-dihydrobenzo[c]pyrano[2,3-e][1,2]thiazine-3‑carbonitrile 5,5-dioxides and 2-amino-6-methyl-4-phenyl-4,6-dihydrobenzo[c]pyrano[2,3-e][1,2]thiazine-3‑carbonitrile 5,5-dioxides. The synthetic methodology involves a multistep reaction starting with methyl anthranilate which was coupled with methane sulfonyl chloride. The product of the reaction was subjected to N-benzylation and N-methylation reactions followed by ring closure with sodium hydride resulting in the formation of respective 2,1-benzothiazine 2,2-dioxides. These 2,1-benzothiazine precursors were subjected to multicomponent reaction with malononitrile and substituted benzaldehydes for the synthesis of two new series of pyranobenzothiazines (6a-r and 7a-r). The synthesized compounds were screened as selective inhibitors of monoamine oxidase A and monoamine oxidase B. The in vitro results suggested that compound 6d and 7q are the selective inhibitors of monoamine oxidase A, however, the selective and potent inhibitors of monoamine oxidase B included compounds 6h and 7r. Moreover, some dual inhibitors were noticed like 7l having more inhibitory activity towards both the isozymes. Moreover, the binding modes of the selective and potent inhibitors of monoamine oxidase A and B were investigated by molecular docking analysis. The results suggested that the synthetic derivatives may be potential towards the monoamine oxidase isozymes.
  20. Fulltext Safety assessment of the ethanolic extract of Gongronema latifolium Benth. leaves: a 90-day oral toxicity study in Sprague Dawley rats
    Al-Hindi B, Yusoff NA, Ahmad M, Atangwho IJ, Asmawi MZ, Al-Mansoub MA, et al.
    BMC Complement Altern Med, 2019 Jun 28;19(1):152.
    PMID: 31253153 DOI: 10.1186/s12906-019-2573-x
    BACKGROUND: The leaves of Gongronema latifolium Benth. have long been recognized traditionally as a remedy for a variety of ailments in Africa. This study was conducted to evaluate the safety profile of the ethanolic extract of G. latifolium (GLES) leaves through a repeated dose 90-day oral toxicity study in male and female of Sprague Dawley rats.

    METHODS: GLES was orally administered at doses of 250, 500 and 1000 mg/kg/day consecutively for 90 days.

    RESULTS: No behavioral or physiological changes and mortality were observed. GLES did not have a marked impact on general hematological parameters and did not precipitate nephrotoxicity. However, compared to the control, serum triglycerides, total cholesterol and low-density lipoprotein levels were lower and white adipose tissue paired retroperitoneal fat depots were depleted in male rats treated with GLES3 by the end of the experiment. The liver was significantly enlarged in GLES-treated rats of both sexes. Negative gender-specific alterations were observed with the highest dose. Adverse risk was evident in the female rats mainly due to marked body weight gain and cerebrum weight reduction.

    CONCLUSION: Further research is needed to reach more specific conclusions about to the safety of ingesting high doses of GLES for long periods of time.

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