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  1. Evaluation of multifunctional synthetic tetralone derivatives for treatment of Alzheimer's disease
    Leng J, Qin HL, Zhu K, Jantan I, Hussain MA, Sher M, et al.
    Chem Biol Drug Des, 2016 Jul 19.
    PMID: 27434226 DOI: 10.1111/cbdd.12822
    Neurodegeneration, a complex disease state, comprises several pathways that contribute to cell death. Conventional approach of targeting only one of these pathways has not been proven to be entirely successful and has demanded a hypothetical change as to how researchers design and develop new drugs. In this study, effects of a series of α, β-unsaturated carbonyl-based tetralone derivatives against Alzheimer's disease (AD) were investigated. Moreover, their activity toward amyloid β-induced cytotoxicity was also studied. Six compounds including 3f, 3o, 3u, 3ae, 3af, and 3ag were discovered to be most protective against Aβ-induced neuronal cell death in PC12 cells. The findings of in vitro experiment revealed that most of these compounds exhibited potent inhibitory activity against MAO-B, AChE, and self-induced Aβ1-42 aggregation. The compound 3f exhibited best AChE (IC50  = 0.045 ± 0.02 μm) inhibitory potential in addition to potent inhibition of MAO-B (IC50  = 0.88 ± 0.12 μm). Furthermore, compound 3f disassembled the Aβ fibrils produced by self-induced Aβ aggregation by 78.2 ± 4.8%. Collectively, these findings suggest that some compounds from this series have potential to be promising multifunctional agents for AD treatment.
  2. Anaerobic membrane bioreactors for biohydrogen production: Recent developments, challenges and perspectives
    Aslam M, Ahmad R, Yasin M, Khan AL, Shahid MK, Hossain S, et al.
    Bioresour Technol, 2018 Dec;269:452-464.
    PMID: 30145004 DOI: 10.1016/j.biortech.2018.08.050
    Biohydrogen as one of the most appealing energy vector for the future represents attractive avenue in alternative energy research. Recently, variety of biohydrogen production pathways has been suggested to improve the key features of the process. Nevertheless, researches are still needed to overcome remaining barriers to practical applications such as low yields and production rates. Considering practicality aspects, this review emphasized on anaerobic membrane bioreactors (AnMBRs) for biological hydrogen production. Recent advances and emerging issues associated with biohydrogen generation in AnMBR technology are critically discussed. Several techniques are highlighted that are aimed at overcoming these barriers. Moreover, environmental and economical potentials along with future research perspectives are addressed to drive biohydrogen technology towards practicality and economical-feasibility.
  3. Fulltext A Study on Microwave Absorption Properties of Carbon Black and Ni0.6Zn0.4Fe2O4 Nanocomposites by Tuning the Matching-Absorbing Layer Structures
    Ibrahim IR, Matori KA, Ismail I, Awang Z, Rusly SNA, Nazlan R, et al.
    Sci Rep, 2020 Feb 21;10(1):3135.
    PMID: 32081972 DOI: 10.1038/s41598-020-60107-1
    Microwave absorption properties were systematically studied for double-layer carbon black/epoxy resin (CB) and Ni0.6Zn0.4Fe2O4/epoxy resin (F) nanocomposites in the frequency range of 8 to 18 GHz. The Ni0.6Zn0.4Fe2O4 nanoparticles were synthesized via high energy ball milling with subsequent sintering while carbon black was commercially purchased. The materials were later incorporated into epoxy resin to fabricate double-layer composite structures with total thicknesses of 2 and 3 mm. The CB1/F1, in which carbon black as matching and ferrite as absorbing layer with each thickness of 1 mm, showed the highest microwave absorption of more than 99.9%, with minimum reflection loss of -33.8 dB but with an absorption bandwidth of only 2.7 GHz. Double layer absorbers with F1/CB1(ferrite as matching and carbon black as absorbing layer with each thickness of 1 mm) structure showed the best microwave absorption performance in which more than 99% microwave energy were absorbed, with promising minimum reflection loss of -24.0 dB, along with a wider bandwidth of 4.8 GHz and yet with a reduced thickness of only 2 mm.
  4. Fulltext Norfloxacin Loaded Lipid Polymer Hybrid Nanoparticles for Oral Administration: Fabrication, Characterization, In Silico Modelling and Toxicity Evaluation
    Khan MA, Khan S, Kazi M, Alshehri SM, Shahid M, Khan SU, et al.
    Pharmaceutics, 2021 Oct 06;13(10).
    PMID: 34683925 DOI: 10.3390/pharmaceutics13101632
    Norfloxacin (NOR), widely employed as an anti-bacterial drug, has poor oral bioavailability. Nano based drug delivery systems are widely used to overcome the existing oral bioavailability challenges. Lipid-Polymer Hybrid Nanoparticles (LPHNs) exhibit the distinctive advantages of both polymeric and liposomes nanoparticles, while excluding some of their disadvantages. In the current study, NOR loaded LPHNs were prepared, and were solid amorphous in nature, followed by in vitro and in vivo evaluation. The optimized process conditions resulted in LPHNs with the acceptable particle size 121.27 nm, Polydispersity Index (PDI) of 0.214 and zeta potential of -32 mv. The addition of a helper lipid, oleic acid, and polymers, ethyl cellulose, substantially increased the encapsulation efficiency (EE%) (65% to 97%). In vitro study showed a sustained drug release profile (75% within 12 h) for NOR LPHNs. The optimized NOR LPHNs showed a significant increase (p < 0.05) in bioavailability compared to the commercial product. From the acute toxicity study, the LD50 value was found to be greater than 1600 mg/kg. The molecular modelling studies substantiated the experimental results with the best combination of polymers and surfactants that produced highly stable LPHNs. Therefore, LPHNs proved to be a promising system for the delivery of NOR, as well as for other antibiotics and hydrophobic drugs.
  5. Fulltext Green photosensitisers for the degradation of selected pesticides of high risk in most susceptible food: A safer approach
    Baig A, Zubair M, Sumrra SH, Rashid U, Zafar MN, Ahmad F, et al.
    PLoS One, 2021;16(10):e0258864.
    PMID: 34710164 DOI: 10.1371/journal.pone.0258864
    Pesticides are the leading defence against pests, but their unsafe use reciprocates the pesticide residues in highly susceptible food and is becoming a serious risk for human health. In this study, mint extract and riboflavin were tested as photosensitisers in combination with light irradiation of different frequencies, employed for various time intervals to improve the photo-degradation of deltamethrin (DM) and lambda cyhalothrin (λ-CHT) in cauliflower. Different source of light was studied, either in ultraviolet range (UV-C, 254 nm or UV-A, 320-380 nm) or sunlight simulator (> 380-800 nm). The degradation of the pesticides varied depending on the type of photosensitiser and light source. Photo-degradation of the DM and λ-CHT was enhanced by applying the mint extracts and riboflavin and a more significant degradation was achieved with UV-C than with either UV-A or sunlight, reaching a maximum decrement of the concentration by 67-76%. The light treatments did not significantly affect the in-vitro antioxidant activity of the natural antioxidants in cauliflower. A calculated dietary risk assessment revealed that obvious dietary health hazards of DM and λ-CHT pesticides when sprayed on cauliflower for pest control. The use of green chemical photosensitisers (mint extract and riboflavin) in combination with UV light irradiation represents a novel, sustainable, and safe approach to pesticide reduction in produce.
  6. Fulltext Phytopharmacological Evaluation of Different Solvent Extract/Fractions From Sphaeranthus indicus L. Flowers: From Traditional Therapies to Bioactive Compounds
    Ahmad HI, Nadeem MF, Shoaib Khan HM, Sarfraz M, Saleem H, Khurshid U, et al.
    Front Pharmacol, 2021;12:708618.
    PMID: 34776946 DOI: 10.3389/fphar.2021.708618
    Sphaeranthus indicus L. is a medicinal herb having widespread traditional uses for treating common ailments. The present research work aims to explore the in-depth phytochemical composition and in vitro reactivity of six different polarity solvents (methanol, n-hexane, benzene, chloroform, ethyl acetate, and n-butanol) extracts/fractions of S. indicus flowers. The phytochemical composition was accomplished by determining total bioactive contents, HPLC-PDA polyphenolic quantification, and UHPLC-MS secondary metabolomics. The reactivity of the phenolic compounds was tested through the following biochemical assays: antioxidant (DPPH, ABTS, FRAP, CUPRAC, phosphomolybdenum, and metal chelation) and enzyme inhibition (AChE, BChE, α-glucosidase, α-amylase, urease, and tyrosinase) assays were performed. The methanol extract showed the highest values for phenolic (94.07 mg GAE/g extract) and flavonoid (78.7 mg QE/g extract) contents and was also the most active for α-glucosidase inhibition as well as radical scavenging and reducing power potential. HPLC-PDA analysis quantified rutin, naringenin, chlorogenic acid, 3-hydroxybenzoic acid, gallic acid, and epicatechin in a significant amount. UHPLC-MS analysis of methanol and ethyl acetate extracts revealed the presence of well-known phytocompounds; most of these were phenolic, flavonoid, and glycoside derivatives. The ethyl acetate fraction exhibited the highest inhibition against tyrosinase and urease, while the n-hexane fraction was most active for α-amylase. Moreover, principal component analysis highlighted the positive correlation between bioactive compounds and the tested extracts. Overall, S. indicus flower extracts were found to contain important phytochemicals, hence could be further explored to discover novel bioactive compounds that could be a valid starting point for future pharmaceutical and nutraceuticals applications.
  7. Fulltext Humanistic and socioeconomic burden of COPD patients and their caregivers in Malaysia
    Rehman AU, Muhammad SA, Tasleem Z, Alsaedi A, Dar M, Iqbal MO, et al.
    Sci Rep, 2021 11 19;11(1):22598.
    PMID: 34799609 DOI: 10.1038/s41598-021-01551-5
    Chronic obstructive pulmonary disease (COPD) is associated with substantial humanistic and socioeconomic burden on patients and their caregivers. COPD is expected to be 7th leading cause of disease burden till 2030. The objective of the current study was to assess the humanistic and socioeconomic burden of COPD patients and their caregivers in Malaysia. The burden includes the cost of management of COPD, QOL of COPD patients and their caregivers, work productivity and activity impairment of COPD patients and their caregivers due to COPD. One hundred and fifty COPD patients and their caregivers from the chest clinic of Penang Hospital were included in the study from August 2018 to August 2019. Caregiving cost was estimated using the replacement cost approach, while humanistic and social burden was assessed with the help of health status questionnaires. Overall, 64.66% and 7.1% of COPD patients reported to depend on informal caregivers and professional caregivers respectively. COPD patients reported dyspnoea score as 2.31 (1.31), EQ-5D-5L utility index 0.57 (0.23), CCI 2.3 (1.4), SGRQ-C 49.23 (18.61), productivity loss 31.87% and activity impairment 17.42%. Caregivers reported dyspnoea score as 0.72 (0.14), EQ-5D-5L utility index 0.57 (0.23), productivity loss 7.19% and social activity limitation as 21.63% due to taking care of COPD patients. In addition to the huge direct cost of management, COPD is also associated with substantial burden on society in terms of compromised quality of life, reduced efficiency at the workplace, activity impairment and caregiver burden.
  8. Pd(II) complexes with chelating N-(1-alkylpyridin-4(1H)-ylidene)amide (PYA) ligands: Synthesis, characterization and evaluation of anticancer activity
    Zafar MN, Butt AM, Chaudhry GE, Perveen F, Nazar MF, Masood S, et al.
    J Inorg Biochem, 2021 11;224:111590.
    PMID: 34507110 DOI: 10.1016/j.jinorgbio.2021.111590
    The bidentate N-(1-Alkylpyridin-4(1H)-ylidene)amide (PYA) pro-ligands [H2LBn][Cl]2 (2), and [H2LMe][TfO]2 (3) were prepared by simple alkylation reactions of the known compound, N,N-di(pyridin-4-yl)oxalamide (H2L, 1). The Pd(II) complexes, [Pd(LBn)2][Cl]2 (4), [Pd(LMe)2][Cl][TfO] (5), Pd(LBn)Cl2 (6) and Pd(LMe)Cl2 (7) were synthesized through reactions between these pro-ligands and suitable Pd(II) substrates in the presence of base. The molecular structures of 3 and 6 were obtained by single crystal X-ray structure determinations. Studies of the experimental and computational DNA binding interactions of the compounds 1-7 revealed that overall 4 and 6 have the largest values for the binding parameters Kb and ΔGbo. The results showed a good correlation with the steric and electronic parameters obtained by quantitative structure activity relationship (QSAR) studies. In-vitro cytotoxicity studies against four different cell lines showed that the human breast cancer cell lines MCF-7, T47D and cervical cancer cell line HeLa had either higher or similar sensitivities towards 4, 6 and 2, respectively, compared to cisplatin. In general, the cytotoxicity of the compounds, represented by IC50 values, decreased in the order 4 > 6 > 2 > 5 > 3 > 1 > 7 in cancer cell lines. Apoptosis contributed significantly to the cytotoxic effects of these anticancer agents as evaluated by apoptosis studies.
  9. Synthesis, pharmacological screening and computational analysis of some 2-(1H-Indol-3-yl)-N'-[(un)substituted phenylmethylidene] acetohydrazides and 2-(1H-Indol-3-yl)-N'-[(un)substituted benzoyl/2-thienylcarbonyl]acetohydrazides
    Rubab K, Abbasi MA, Rehman A, Siddiqui SZ, Shah SAA, Ashraf M, et al.
    Pak J Pharm Sci, 2017 Jul;30(4):1263-1274.
    PMID: 29039324
    The undertaken research was initiated by transforming 2-(1H-Indol-3-yl)acetic acid (1) in catalytic amount of sulfuric acid and ethanol to ethyl 2-(1H-Indol-3-yl)acetate (2), which was then reacted with hydrazine monohydrate in methanol to form 2-(1H-Indol-3-yl)acetohydrazide (3). Further, The reaction scheme was designed into two pathways where, first pathway involved The reaction of 3 with substituted aromatic aldehydes (4a-o) in methanol with few drops of glacial acetic acid to generate 2-(1H-Indol-3-yl)-N'-[(un)substitutedphenylmethylidene]acetohydrazides (5a-o) and in second pathway 3 was reacted with acyl halides (6a-e) in basic aqueous medium (pH 9-10) to afford 2-(1H-Indol-3-yl)-N'-[(un)substitutedbenzoyl/2-thienylcarbonyl]acetohydrazides (7a-e). All The synthesized derivatives were characterized by IR, EI-MS and 1H-NMR spectral techniques and evaluated for their anti-bacterial potentials against Gram positive and Gram negative bacterial strains and it was found that compounds 7a-d exhibited antibacterial activities very close to standard Ciprofloxacin. The synthesized derivatives demonstrated moderate to weak anti-enzymatic potential against α-Glucosidase and Butyrylcholinesterase (BChE) where, compounds 7c and 5c exhibited comparatively better inhibition against these enzymes respectively. Compounds 7a, 7d and 7e showed excellent anti-enzymatic potentials against Lipoxygenase (LOX) and their IC50 values were much lower than the reference standard Baicalein. Enzyme inhibitory activities were also supported by computational docking results. Compounds 5c, 7a, 7b and 7c also showed low values of % hemolytic activity as well, showing that these molecules were not toxic, indicating that these molecules can be utilized as potential therapeutic agents against inflammatory ailments.
  10. Innovations in the synthesis of graphene nanostructures for bio and gas sensors
    Ikram M, Bari MA, Bilal M, Jamal F, Nabgan W, Haider J, et al.
    Biomater Adv, 2023 Feb;145:213234.
    PMID: 36502548 DOI: 10.1016/j.bioadv.2022.213234
    Sensors play a significant role in modern technologies and devices used in industries, hospitals, healthcare, nanotechnology, astronomy, and meteorology. Sensors based upon nanostructured materials have gained special attention due to their high sensitivity, precision accuracy, and feasibility. This review discusses the fabrication of graphene-based biosensors and gas sensors, which have highly efficient performance. Significant developments in the synthesis routes to fabricate graphene-based materials with improved structural and surface properties have boosted their utilization in sensing applications. The higher surface area, better conductivity, tunable structure, and atom-thick morphology of these hybrid materials have made them highly desirable for the fabrication of flexible and stable sensors. Many publications have reported various modification approaches to improve the selectivity of these materials. In the current work, a compact and informative review focusing on the most recent developments in graphene-based biosensors and gas sensors has been designed and delivered. The research community has provided a complete critical analysis of the most robust case studies from the latest fabrication routes to the most complex challenges. Some significant ideas and solutions have been proposed to overcome the limitations regarding the field of biosensors and hazardous gas sensors.
  11. Fulltext Emergence of mRNA vaccines in the management of cancer
    Mohamad Razif MI, Nizar N, Zainal Abidin NH, Muhammad Ali SN, Wan Zarimi WNN, Khotib J, et al.
    Expert Rev Vaccines, 2023;22(1):629-642.
    PMID: 37401128 DOI: 10.1080/14760584.2023.2232450
    INTRODUCTION: mRNA vaccines have been developed as a promising cancer management. It is noted that specification of the antigen sequence of the target antigen is necessary for the design and manufacture of an mRNA vaccine.

    AREAS COVERED: The steps involved in preparing the mRNA-based cancer vaccines are isolation of the mRNA cancer from the target protein using the nucleic acid RNA-based vaccine, sequence construction to prepare the DNA template, in vitro transcription for protein translation from DNA into mRNA strand, 5' cap addition and poly(A) tailing to stabilize and protect the mRNA from degradation and purification process to remove contaminants produced during preparation.

    EXPERT OPINION: Lipid nanoparticles, lipid/protamine/mRNA nanoparticles, and cell-penetrating peptides have been used to formulate mRNA vaccine and to ensure vaccine stability and delivery to the target site. Delivery of the vaccine to the target site will trigger adaptive and innate immune responses. Two predominant factors of the development of mRNA-based cancer vaccines are intrinsic influence and external influence. In addition, research relating to the dosage, route of administration, and cancer antigen types have been observed to positively impact the development of mRNA vaccine.

  12. Understanding The Mimicker: Epidemiological Pattern and Determinant of Melioidosis Mortality in Negeri Sembilan, Malaysia
    Md Hanif SA, Hassan MR, Rafi'i MR, Abdul Halim AFN, Ahmad Zamzuri M'I, Ismail M, et al.
    PLoS Negl Trop Dis, 2024 May 06;18(5):e0012147.
    PMID: 38709822 DOI: 10.1371/journal.pntd.0012147
    BACKGROUND: Melioidosis, a tropical infectious disease caused by Burkholderia pseudomallei, is epidemic in most region in Southeast Asia with high case fatality. However, there is scanty information regarding the disease's epidemiological pattern, demographics, and underlying risk factors.

    METHOD: This 5-year retrospective study of 185 confirmed cases which were taken from the Negeri Sembilan Melioidosis Registry between 2018 and 2022. We aim to describe the incidence, mortality rate, case fatality, relationship with meteorology, and factors that influence mortality in this central region of Peninsular Malaysia.

    RESULTS: Incidence rate (IR) of melioidosis in Negeri Sembilan is varied at 1.9 to 5.1 with mean of 3.1 in 100,000 population per year. IR varied between districts in the state from zero to 22.01 in 100,000 population per year. Mortality rate were ranged from 0.17 to 0.74 cases with mean of 0.44 cases in 100,000 population per year. The case fatality rate of this state scattered from 8.70% to 16.67%. There were no significant linear associations between cases and deaths with monthly rainfall and humidity. The mean age of patients was 52.8 years, predominated with age around 41-60 years old. Males (77.8%) predominated, and the majority of cases were Malays (88.9%) and had exposed to soil related activities (74.6%). Mortality from melioidosis was more likely in Bumiputera and non-Malaysians (p<0.05). Patients who had at least one comorbidity were at a higher risk of death from melioidosis (p<0.05). Diabetes mellitus was found in 41.1% of all identified cases, making it a major underlying risk factor for both developing and dying from melioidosis (aOR:19.32, 95%CI:1.91-195.59, p<0.05). Hypertension and mortality status in melioidosis are also significantly correlated (aOR: 7.75, 95% CI: 2.26-26.61, p<0.05).

    CONCLUSION: The epidemiological patterns of cases reported from Negeri Sembilan are consistent for the most part from previous studies in other states in Malaysia and global with regard to its incidence, case fatality, demographic and predisposing chronic diseases. Diabetes mellitus and hypertension were significantly linked to increased mortality among all determinants.

  13. Fulltext Factors associated with placenta praevia in primigravidas and its pregnancy outcome
    Nur Azurah AG, Wan Zainol Z, Lim PS, Shafiee MN, Kampan N, Mohsin WS, et al.
    ScientificWorldJournal, 2014;2014:270120.
    PMID: 25478587 DOI: 10.1155/2014/270120
    To examine the factors associated with placenta praevia in primigravidas and also compare the pregnancy outcomes between primigravidas and nonprimigravidas.
  14. Fulltext Thermodynamic and spectroscopic investigation of interactions between reactive red 223 and reactive orange 122 anionic dyes and cetyltrimethyl ammonium bromide (CTAB) cationic surfactant in aqueous solution
    Irfan M, Usman M, Mansha A, Rasool N, Ibrahim M, Rana UA, et al.
    ScientificWorldJournal, 2014;2014:540975.
    PMID: 25243216 DOI: 10.1155/2014/540975
    The present study describes the conductometric and spectroscopic study of the interaction of reactive anionic dyes, namely, reactive red 223 and reactive orange 122 with the cationic surfactant cetyltrimethyl ammonium bromide (CTAB). In a systematic investigation, the electrical conductivity data was used to calculate various thermodynamic parameters such as free energy (ΔG), enthalpy (ΔH), and the entropy (ΔS) of solubilization. The trend of change in these thermodynamic quantities indicates toward the entropy driven solubilization process. Moreover, the results from spectroscopic data reveal high degree of solubilization, with strong interactions observed in the cases of both dyes and the CTAB. The spontaneous nature of solubilization and binding was evident from the observed negative values of free energies (ΔG p and ΔG b).
  15. Fulltext Chemical composition and Biological studies of Ficus benjamina
    Imran M, Rasool N, Rizwan K, Zubair M, Riaz M, Zia-Ul-Haq M, et al.
    Chem Cent J, 2014;8(1):12.
    PMID: 24524349 DOI: 10.1186/1752-153X-8-12
    Current study has been designed to estimate the possible antioxidant, antimicrobial and hemolytic potential of Ficus benjamina different parts (leaves, stem and root).
  16. Biotransformation of 17α-ethynyl substituted steroidal drugs with microbial and plant cell cultures: a review
    Shah SA, Sultan S, Hassan NB, Muhammad FK, Faridz MA, Hussain FB, et al.
    Steroids, 2013 Dec 20;78(14):1312-24.
    PMID: 24135562 DOI: 10.1016/j.steroids.2013.10.001
    Structural modification of steroids through whole-cell biocatalysis is an invaluable procedure for the production of active pharmaceutical ingredients (APIs) and key intermediates. Modifications could be carried out with regio- and stereospecificity at positions hardly available for chemical agents. Much attention has been focused recently on the biotransformation of 17α-ethynyl substituted steroidal drugs using fungi, bacteria and plant cell cultures in order to obtained novel biologically active compounds with diverse structure features. Present article includes studies on biotransformation on 17α-ethynyl substituted steroidal drugs using microorganisms and plant cell cultures. Various experimental and structural elucidation methods used in biotransformational processes are also highlighted.
  17. Survival rate of breast cancer patients in Malaysia: a population-based study
    Abdullah NA, Wan Mahiyuddin WR, Muhammad NA, Ali ZM, Ibrahim L, Ibrahim Tamim NS, et al.
    Asian Pac J Cancer Prev, 2013;14(8):4591-4.
    PMID: 24083707
    Breast cancer is the most common cancer among Malaysian women. Other than hospital-based results, there are no documented population-based survival rates of Malaysian women for breast cancers. This population- based retrospective cohort study was therefore conducted. Data were obtained from Health Informatics Centre, Ministry of Health Malaysia, National Cancer Registry and National Registration Department for the period from 1st Jan 2000 to 31st December 2005. Cases were captured by ICD-10 and linked to death certificates to identify the status. Only complete data were analysed. Survival time was calculated from the estimated date of diagnosis to the date of death or date of loss to follow-up. Observed survival rates were estimated by Kaplan- Meier method using SPSS Statistical Software version 17. A total of 10,230 complete data sets were analysed. The mean age at diagnosis was 50.6 years old. The overall 5-year survival rate was 49% with median survival time of 68.1 months. Indian women had a higher survival rate of 54% compared to Chinese women (49%) and Malays (45%). The overall 5-year survival rate of breast cancer patient among Malaysian women was still low for the cohort of 2000 to 2005 as compared to survival rates in developed nations. Therefore, it is necessary to enhance the strategies for early detection and intervention.
  18. Phytochemicals from Dodonaea viscosa and their antioxidant and anticholinesterase activities with structure-activity relationships
    Muhammad A, Tel-Çayan G, Öztürk M, Duru ME, Nadeem S, Anis I, et al.
    Pharm Biol, 2016 Sep;54(9):1649-55.
    PMID: 26866457 DOI: 10.3109/13880209.2015.1113992
    Context Dodonaea viscosa (L.) Jacq (Sapindaceae) has been used in traditional medicine as antimalarial, antidiabetic and antibacterial agent, but further investigations are needed. Objective This study determines the antioxidant and anticholinesterase activities of six compounds (1-6) and two crystals (1A and 3A) isolated from D. viscosa, and discusses their structure-activity relationships. Materials and methods Antioxidant activity was evaluated using six complementary tests, i.e., β-carotene-linoleic acid; DPPH(•), ABTS(•+), superoxide scavenging, CUPRAC and metal chelating assays. Anticholinesterase activity was performed using the Elman method. Results Clerodane diterpenoids (1 and 2) and phenolics (3-6) - together with three crystals (1A, 3A and 7A) - were isolated from the aerial parts of D. viscosa. Compound 3A exhibited good antioxidant activity in DPPH (IC50: 27.44 ± 1.06 μM), superoxide (28.18 ± 1.35% inhibition at 100 μM) and CUPRAC (A0.5: 35.89 ± 0.09 μM) assays. Compound 5 (IC50: 11.02 ± 0.02 μM) indicated best activity in ABTS assay, and 6 (IC50: 14.30 ± 0.18 μM) in β-carotene-linoleic acid assay. Compounds 1 and 3 were also obtained in the crystal (1A and 3A) form. Both crystals showed antioxidant activity. Furthermore, crystal 3A was more active than 3 in all activity tests. Phenol 6 possessed moderate anticholinesterase activity against acetylcholinesterase and butyrylcholinesterase enzymes (IC50 values: 158.14 ± 1.65 and 111.60 ± 1.28 μM, respectively). Discussion and conclusion This is the first report on antioxidant and anticholinesterase activities of compounds 1, 2, 5, 6, 1A and 3A, and characterisation of 7A using XRD. Furthermore, the structure-activity relationships are also discussed in detail for the first time.
  19. 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.
  20. 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.
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