Displaying publications 101 - 120 of 444 in total

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  1. Mohd Khalizan Sabullah, Mohd Ezuan Khayat
    MyJurnal
    In this study, the substrate specificity and the inhibition kinetics of various types of insecticides to the acetylcholinesterase (AChE) from a local fish; Puntius schwanenfeldii were investigated. The substrate specificity determination was done using three thiocholine substrates, which were ATC, PTC and BTC. The results showed that he partially purified cholinesterase from Puntius schwanenfeldii that preferred ATC is a true AChE. The Km and Vmax values of AChE for these substrates were 16.61 mmol and 286.5 U/mg for ATC, 19.92 mmol and 245.3 U/mg for PTC, and 48.64 mmol and 219.6 U/mg for BTC, respectively. The IC50 values for the carbamates bendiocarb, carbaryl, propoxur, carbofuran and methomyl were 0.838, 7.045, 29.441, 1.411 and 8.335 mg/L, respectively, which were comparable to the IC50 values for carbamates from several AChE from fish.
    Matched MeSH terms: Inhibitory Concentration 50
  2. Khan M, Alam A, Khan KM, Salar U, Chigurupati S, Wadood A, et al.
    Bioorg Chem, 2018 12;81:157-167.
    PMID: 30125730 DOI: 10.1016/j.bioorg.2018.07.038
    Novel derivatives of flurbiprofen 1-18 including flurbiprofen hydrazide 1, substituted aroyl hydrazides 2-9, 2-mercapto oxadiazole derivative 10, phenacyl substituted 2-mercapto oxadiazole derivatives 11-15, and benzyl substituted 2-mercapto oxadiazole derivatives 16-18 were synthesized and characterized by EI-MS, 1H and 13C NMR spectroscopic techniques. All derivatives 1-18 were screened for α-amylase inhibitory activity and demonstrated a varying degree of potential ranging from IC50 = 1.04 ± 0.3 to 2.41 ± 0.09 µM as compared to the standard acarbose (IC50 = 0.9 ± 0.04 µM). Out of eighteen compounds, derivatives 2 (IC50 = 1.69 ± 0.1 µM), 3 (IC50 = 1.04 ± 0.3 µM), 9 (IC50 = 1.25 ± 1.05 µM), and 13 (IC50 = 1.6 ± 0.18 µM) found to be excellent inhibitors while rest of the compounds demonstrated comparable inhibition potential. A limited structure-activity relationship (SAR) was established by looking at the varying structural features of the library. In addition to that, in silico study was conducted to understand the binding interactions of the compounds (ligands) with the active site of α-amylase enzyme.
    Matched MeSH terms: Inhibitory Concentration 50
  3. Hasanpourghadi M, Abdul Majid N, Rais Mustafa M
    PeerJ, 2018;6:e5577.
    PMID: 30245930 DOI: 10.7717/peerj.5577
    Combination Index (CI) analysis suggested that MBIC and doxorubicin synergistically inhibited up to 97% of cell proliferation in ER+/PR+MCF-7 and triple negative MDA-MB-231 breast cancer cell lines. Moreover, treatment of the breast cancer cells with the combined drugs resulted in lower IC50 values in contrast to the individual drug treatment. Small noncoding microRNAs (miRNA) may function as non-mutational gene regulators at post-transcriptional level of protein synthesis. In the present study, the effect of the combined treatment of MBIC and doxorubicin on the expression level of several miRNAs including miR-34a, miR-146a, miR-320a and miR-542 were evaluated in MCF-7 and MDA-MB-231 breast cancer cell lines. These miRNAs have the potential to alter the protein level of survivin, the anti-apoptotic protein and reduce the metastatic activity in human breast cancer cell lines by interfering with the nuclear accumulation of NF-κB. Our results demonstrated the several fold changes in expression of miRNAs, which is drug and cell line dependent. This finding demonstrated a functional synergistic network between miR-34a, miR-320a and miR-542 that are negatively involved in post-transcriptional regulation of survivin in MCF-7 cells. While in MDA-MB-231 cells, changes in expression level of miR-146a was correlated with inhibition of the nuclear translocation of NF-κB. The overall result suggested that alteration in protein level and location of survivin and NF-κB by miR-34a, miR-320a, miR-146a and miR-542, remarkably influenced the synergistic enhancement of combined MBIC and doxorubicin in treatment of aggressive and less aggressive human breast cancer cell lines.
    Matched MeSH terms: Inhibitory Concentration 50
  4. Raza H, Abbasi MA, Aziz-Ur-Rehman, Siddiqui SZ, Hassan M, Abbas Q, et al.
    Bioorg Chem, 2020 01;94:103445.
    PMID: 31826809 DOI: 10.1016/j.bioorg.2019.103445
    In the current research work, different N-(substituted-phenyl)-4-{(4-[(E)-3-phenyl-2-propenyl]-1-piperazinyl}butanamides have been synthesized according to the protocol described in scheme 1. The synthesis was initiated by reacting various substituted anilines (1a-e) with 4-chlorobutanoyl chloride (2) in aqueous basic medium to give various electrophiles, 4-chloro-N-(substituted-phenyl)butanamides (3a-e). These electrophiles were then coupled with 1-[(E)-3-phenyl-2-propenyl]piperazine (4) in polar aprotic medium to attain the targeted N-(substituted-phenyl)-4-{(4-[(E)-3-phenyl-2-propenyl]-1-piperazinyl}butanamides (5a-e). The structures of all derivatives were identified and characterized by proton-nuclear magnetic resonance (1H NMR), carbon-nuclear magnetic resonance (13C NMR) and Infra-Red (IR) spectral data along with CHN analysis. The in vitro inhibitory potential of these butanamides was evaluated against Mushroom tyrosinase, whereby all compounds were found to be biologically active. Among them, 5b exhibited highest inhibitory potential with IC50 value of 0.013 ± 0.001 µM. The same compound 5b was also assayed through in vivo approach, and it was explored that it significantly reduced the pigments in zebrafish. The in silico studies were also in agreement with aforesaid results. Moreover, these molecules were profiled for their cytotoxicity through hemolytic activity, and it was found that except 5e, all other compounds showed minimal toxicity. The compound 5a also exhibited comparable results. Hence, some of these compounds might be worthy candidates for the formulation and development of depigmentation drugs with minimum side effects.
    Matched MeSH terms: Inhibitory Concentration 50
  5. Rahim F, Zaman K, Taha M, Ullah H, Ghufran M, Wadood A, et al.
    Bioorg Chem, 2020 01;94:103394.
    PMID: 31699396 DOI: 10.1016/j.bioorg.2019.103394
    Voglibose and acarbose are distinguished α-glucosidase inhibitors used for controlling of diabetes mellitus. Unfortunately, these distinguished and clinically used inhibitors have also numerous side effects. Subsequently, there is still needed to develop safer therapy. Despite of a broad spectrum of biological importance of benzimidazole, it is occasionally evaluated for α-glucosidase activity. Current study deals with the synthesis and biological screening of benzimidazole bearing bis-Schiff bases (1-19) for their α-glucosidase inhibitory activity. All analogues exhibited excellent to good inhibitory potential (IC50 = 2.20 ± 0.1to 88.60 ± 1.70 µM) when compared with standard drug acarbose (IC50 = 38.45 ± 0.80 µM). A structure activity relationship has been established on the basis of electronic effects and position of different substituents present on phenyl ring. In order to rationalize the binding interactions of most active analogues with the active site of α-glucosidase enzyme, molecular docking study was conducted.
    Matched MeSH terms: Inhibitory Concentration 50
  6. Nor Ashikeen Mukti, Suhaniza Sulaiman, Suhana Md Saad, Junaida @ Maimunah Hassan Basari, Mariati Abdul Rahman, Wan Zurinah Wan Ngah, et al.
    Chlorella vulgaris (ChV), sejenis alga hijau unisel telah dilaporkan mempunyai khasiat kesihatan pada penyakit tertentu termasuk kanser. Objektif utama kajian ialah untuk mengukur dan menilai kesan antioksidan dan antitumor ekstrak air panas ChV ke atas sel kanser hepar yang dijalankan secara in vivo dan in vitro. Asai DPPH yang dijalankan menunjukkan peratus pengautan ChV yang tinggi. Dalam kajian in vivo, tikus Wistar jantan (200-250 g) dibahagikan kepada lapan kumpulan: tikus kawalan (diet normal), tikus diaruh kanser hepar (diet kurang kolin + 0.1% etionin dalam air minuman) atau singkatannya CDE, tikus diberi rawatan ChV pada tiga dos berbeza (50, 150 dan 300 mg/kg berat badan) dan tikus CDE diberi rawatan ChV pada tiga dos berbeza. Sampel darah dan tisu diambil dari semua kumpulan tikus pada minggu 0, 4, 8 dan 12 untuk penentuan kadar proliferasi dan apoptosis sel untuk melihat kesan antitumor ChV. Peratus pembentukan nodul praneoplasia adalah tinggi pada tikus diaruh kanser hepar (CDE) tetapi ChV pada semua dos berjaya mengurangkannya. Pertambahan jumlah sel kanser semasa hepatokarsinogenesis ditunjukkan dengan peningkatan proliferasi hepatosit yang signifikan (p<0.05) pada tikus CDE berbanding kawalan tetapi ChV pada semua dos berjaya mengurangkan proliferasi secara signifikan (p<0.05). Peratus apoptosis sel didapati meningkat secara signifikan (p<0.05) pada tikus CDE, tetapi peningkatan yang lebih ketara berlaku pada tikus CDE diberi ChV (300 mg/kg berat badan). Dalam kajian in vitro pula, aktiviti antitumor ekstrak air panas ChV telah ditentukan dengan melihat perubahan dalam proliferasi dan apoptosis sel kanser hepar HepG2 yang dikultur di makmal. Ekstrak air panas ChV berjaya menurunkan kadar proliferasi sel HepG2 dengan signifikan secara berkadar terus dengan dos yang digunakan dengan nilai IC50 1.6 mg/ml. Hasil analisis TUNEL pula menunjukkan ekstrak air panas ChV berjaya mengaruh apoptosis dalam sel HepG2. Keputusan ini disokong oleh hasil pemblotan Western dengan peningkatan pengekspresan protein P53 dan protein proapoptosis BAX dan Kaspase-3. Daripada hasil-hasil kajian, dapatlah dicadangkan bahawa ChV berpotensi tinggi sebagai antioksidan serta berupaya memberi kesan antitumor kepada kanser hepar pada kajian in vivo dan in vitro.
    Matched MeSH terms: Inhibitory Concentration 50
  7. Kawde AN, Taha M, Alansari RS, Almandil NB, Anouar EH, Uddin N, et al.
    Int J Biol Macromol, 2020 Jul 01;154:217-232.
    PMID: 32173438 DOI: 10.1016/j.ijbiomac.2020.03.090
    α-Glucosidase and α-amylase are enzymes which are associated with diabetic II. These enzymes break macromolecules of sugar into monosugar molecules which is soluble in body, hence increase the sugar level in blood. There is need to develop economical and save inhibitors to prevent them from breaking sugar macromolecules to soluble molecules which will control the level of sugar in blood. Therefore, we synthesized indole-based derivatives (1-18) and evaluated as dual inhibitor for α-glucosidase and α-amylase. These chemical scaffolds were built with variation in aryl ring which were found active with good to moderate activity for α-glucosidase having IC50 value ranging from 13.99 ± 0.10 to 59.09 ± 0.30 μM when compared with standard acarbose with IC50 of 11.29 ± 0.10 μM; for α-amylase IC50 value ranging from 13.14 ± 0.10 to 58.99 ± 0.30 μM when compared with the standard acarbose with IC50 of 11.12 ± 0.10 μM. Structure activity relationship (SAR) has been established for all compounds. Enzymatic kinetic study and molecular docking study have been carried out to investigate the binding interactions α-glucosidase and α-amylase enzyme.
    Matched MeSH terms: Inhibitory Concentration 50
  8. Koosha S, Mohamed Z, Sinniah A, Ibrahim Z, Seyedan A, Alshawsh MA
    Life Sci, 2019 Jul 03.
    PMID: 31278947 DOI: 10.1016/j.lfs.2019.116633
    AIMS: The compound 8-prenylnaringenin (8-PN) is a prenylflavonoid that can be isolated from hops and beer and has anti-cancer properties against breast cancer. The aim of this study is to investigate the anti-proliferative and apoptotic activities of 8-PN against human colon cancer HCT-116 cells.

    MAIN METHODS: Colon cancer HCT-116 cells were treated with 8-PN and subjected to MTT and acridine orange/propidium iodide (AO/PI) staining to investigate the cytotoxicity of 8-PN. Arrest of the cells at different phases of cell cycle was monitored in the presence of 8-PN. Moreover, the apoptotic effects of 8-PN was assessed via annexin V and caspase activity assays and compared to the untreated cells.

    KEY FINDINGS: The findings showed that 8-PN revealed strong inhibitory effect against HCT-116 cells with an IC50 value of 23.83 ± 2.9 μg/ml after 48 h. However, at similar concentrations and experimental time-points, the compound did not show cytotoxic effect to non-cancerous colon cells (CCD-41). Annexin-V assay indicates that 38.5% and 14.4% of HCT-116 cells had entered early and late stages of apoptosis, respectively after exposure of the cells to 8-PN for 48 h. Caspase activity assay illustrates that apoptosis is activated through both intrinsic and extrinsic pathways. Moreover, flow cytometry cell cycle results indicate that treatment with 8-PN significantly arrested the HCT-116 cells at G0/G1 phase.

    SIGNIFICANCE: These findings reveal that 8-PN has anti-proliferative activity against HCT-116 colon cancer cells via induction of intrinsic and extrinsic pathway-mediated apoptosis. Further investigations should be carried out to unravel the mechanistic pathways underlying these activities.

    Matched MeSH terms: Inhibitory Concentration 50
  9. Muid, S., Ali, A.M., Yusoff, K., Nawawi, H.M.
    MyJurnal
    Vitamin E is known to have potent antioxidant activity and plays an important role in reducing oxidative stress, a pivotal step in atherogenesis. However, several randomised clinical trials using α-tocopherol have failed to demonstrate consistent beneficial effects of antioxidants against atherosclerosis and clinical endpoints. Tocotrienol, a vitamin E compound analogue is shown to have more potent antioxidant activity compared to tocopherol. Finding the optimal anti-oxidative dose is crucial and may effectively be applied for cardioprotection in human. The objective of this study was to determine the optimal dose of tocotrienol rich fraction (TRF) with highest antioxidant activity in vitro using the ferric thiocyanate (FTC), 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity and 2’, 7’- dichlorofluorescein diacetate (DCFHDA) assays. It was found that TRF exhibited potent antioxidant and free radical scavenging activities with an IC50 of 22.10 + 0.01 µg/ml. In all assays, TRF had optimal antioxidant activity at moderate concentrations (10-100 µg/ml). In conclusion, TRF has potent antioxidant activity, which is optimal at moderate concentrations.
    Matched MeSH terms: Inhibitory Concentration 50
  10. Rafi, N.M., Halim, N.R.A., Amin, A.M., Sarbon, N.M.
    MyJurnal
    The enzymatic hydrolysis of lead tree seed protein with alcalase to obtain Lead Tree Seed Hydrosylate (LTSH) was optimized using response surface methodology (RSM). A three- tiered, factor face centered, central composite design (CCD) was used to study the influence of four independent variables namely: pH (7–9); hydrolysis temperature (50oC, 55oC, 60oC); hydrolysis time (30 min, 60 min, 90 min); and enzyme/substrate (1%, 2%, 3%) ratio on both yield and antioxidant activity. The CCD consisted of twenty-four experimental points and six replicates of central points. All data were analyzed using Design-Expert Software. The optimum conditions obtained from experiments were a pH of 9; an enzyme to substrate ratio of 2%; a hydrolysis time of 90 min; and a temperature of 55°C. Results showed that LTSH derived from optimized hydrolysis exhibited effective ferrous ion chelating activity (92.79%) and strong reducing power (A700 = 3.82) at a concentration of 20 mg/ml. LTSH also demonstrated high DPPH radical scavenging activity (76.21%; IC50 1.99 mg/ml), as well as hydroxyl radical scavenging activity (66.72%; IC50 2.45 mg/ml). Superoxide anion scavenging activity was 55.71% (IC50 3.89 mg/ml) at 20 mg/ml. These results suggest that LTSH has potential as a natural antioxidant of functional food and for use in food processing.
    Matched MeSH terms: Inhibitory Concentration 50
  11. Mah SH, Ee GC, Teh SS, Rahmani M, Lim YM, Go R
    Molecules, 2012 Jul 10;17(7):8303-11.
    PMID: 22781442 DOI: 10.3390/molecules17078303
    Our continuing studies on secondary metabolites from the stem bark of Calophyllum soulattri has led to the isolation of another new diprenylated xanthone, phylattrin (1), in addition to five other xanthones and two common sterols. The xanthones are soulattrin (2), caloxanthone C (3), macluraxanthone (4), brasixanthone B (5) and trapezifolixanthone (6) while the sterols are stigmasterol (7) and β-sitosterol (8). The structures of these compounds were determined on the basis of spectroscopic analyses such as 1D and 2D-NMR, HRESIMS, IR and UV. Compounds 1-7 exhibited moderate cytotoxic activities against SNU-1, HeLa, Hep G2, NCI-H23, K562, Raji, LS174T, IMR-32 and SK-MEL-28 cells.
    Matched MeSH terms: Inhibitory Concentration 50
  12. Rasti H, Parivar K, Baharara J, Iranshahi M, Namvar F
    Iran J Pharm Res, 2017;16(1):366-379.
    PMID: 28496490
    This study presents the first ever data of extracting chitin from the Chiton shell, which was then converted to the soluble chitosan by soaking in the 45% NaOH solution. The obtained chitin and chitosan were characterized by the seven different methods. Antioxidant activity of the extracted chitosan was also evaluated using the two methods. The shell content was divided into calcium carbonate (90.5 %), protein (5.2%), and chitin (4.3 %). Due to the results of element analysis and 1H NMR, the final degree of deacetylation of chitosan was 90%. Surprisingly, a significant amount of Fe was accidentally found in the shell after demineralization, and removed from the solution through the filtering. Nonetheless, remained Fe in the extracted chitin and chitosan was 20 times higher than those previously reported from the shell of shrimps and crabs. Presence of this amount of Fe could describe why the produced chitosan was darker compared to the commercial chitosan. Antioxidant activity tests showed that the IC50 of the extracted chitosan was higher than one estimated for the commercial chitosan. Antioxidant activity of the extracted chitosan is even better than the commercial version and may be used in pharmaceutical industry as a source of antioxidant.
    Matched MeSH terms: Inhibitory Concentration 50
  13. Abu Bakar MF, Abdul Karim F, Suleiman M, Isha A, Rahmat A
    PMID: 26640502 DOI: 10.1155/2015/936215
    The study aimed to investigate the phytochemical contents, antioxidant and antiproliferative activity of 80% methanol extract of Lepidozia borneensis. The total phenolic and total flavonoid contents were analysed using Folin-Ciocalteu and aluminium chloride colorimetric methods. Antioxidant properties were evaluated by using FRAP, ABTS, and DPPH assays while the effects of L. borneensis on the proliferation of MCF-7 cell line were evaluated by using MTT assay. The results showed that the total phenolic and flavonoid contents were 12.42 ± 0.47 mg GAE/g and 9.36 ± 1.29 mg CE/g, respectively. The GC-MS analysis revealed the presence of at least 35 compounds. The extract was found to induce cytotoxicity against MCF-7 cell line with IC50 value of 47.33 ± 7.37 µg/mL. Cell cycle analysis showed that the extract induced significant arrest at G0/G1 at 24 hours of treatment. After 72 hours of treatment, the proportion of cells in G0/G1 and G2-M phases had decreased significantly as compared to their control. Apoptosis occurred during the first 24 hours and significantly increased to 30.8% after 72 hours of treatment. No activation of caspase 3 was observed. These findings suggest that L. borneensis extract has the potential as natural antioxidant and anticancer agents.
    Matched MeSH terms: Inhibitory Concentration 50
  14. Mohd Dom NS, Yahaya N, Adam Z, Nik Abd Rahman NMA, Hamid M
    PMID: 32831872 DOI: 10.1155/2020/6374632
    The present study aimed to evaluate the potential of standardized methanolic extracts from seven Ficus deltoidea varieties in inhibiting the formation of AGEs, protein oxidation, and their antioxidant effects. The antiglycation activity was analyzed based on the inhibition of AGEs, fructosamine, and thiol groups level followed by the inhibition of protein carbonyl formation. The antioxidant activity (DPPH radical scavenging activity and reducing power assay) and total phenolic contents were evaluated. After 28 days of induction, all varieties of Ficus deltoidea extracts significantly restrained the formation of fluorescence AGEs by 4.55-5.14 fold. The extracts also reduced the fructosamine levels by 47.0-86.5%, increased the thiol group levels by 64.3-83.7%, and inhibited the formation of protein carbonyl by 1.36-1.76 fold. DPPH radical scavenging activity showed an IC50 value of 66.81-288.04 μg/ml and reducing power activity depicted at 0.02-0.24 μg/ml. The extent of phenolic compounds present in the extracts ranged from 70.90 to 299.78 mg·GAE/g. Apart from that, correlation studies between the activities were observed. This study revealed that seven varieties of Ficus deltoidea have the potential to inhibit AGEs formation and possess antioxidant activity that might be attributed to the presence of phenolic compounds.
    Matched MeSH terms: Inhibitory Concentration 50
  15. Chandradevan M, Simoh S, Mediani A, Ismail NH, Ismail IS, Abas F
    PMID: 32047522 DOI: 10.1155/2020/3238561
    This study aimed to determine the total phenolic content, DPPH scavenging, α-glucosidase, and nitric oxide (NO) inhibition of Gynura procumbens and Cleome gynandra extracts obtained with five different ethanolic concentrations. The findings showed that the 100% ethanolic extract of G. procumbens had the highest phenolic content and the lowest IC50 values for DPPH scavenging and NO inhibition activity compared to the properties of the other extracts. For C. gynandra, the 20% and 100% ethanolic extracts had comparably high total phenolic contents, and the latter possessed the lowest IC50 value in the NO inhibition assay. In addition, the 20% ethanolic extract of C. gynandra had the lowest IC50 value in the DPPH scavenging assay. However, none of the extracts from either herb had the ability to inhibit α-glucosidase enzyme. Pearson correlation analysis indicated a strong relationship between the phenolic content and DPPH scavenging activity in both herb extracts. A moderately strong relationship was also observed between the phenolic content and NO inhibition in G. procumbens extracts and not in C. gynandra extracts. The UHPLC-ESI-Orbitrap-MS revealed major phenolics from the groups of hydroxycinnamic acids, hydroxybenzoic acids, and flavonoid derivatives from both herbs, which could be the key contributors to their bioactivities. Among the identified metabolites, 24 metabolites were tentatively assigned for the first time from both species of studied herbs. These two herbs could be recommended as prospective natural products with valuable medicinal properties.
    Matched MeSH terms: Inhibitory Concentration 50
  16. Haron AS, Syed Alwi SS, Saiful Yazan L, Abd Razak R, Ong YS, Zakarial Ansar FH, et al.
    PMID: 30186351 DOI: 10.1155/2018/1549805
    Thymoquinone (TQ), a bioactive compound found in Nigella sativa, cannot be orally consumed due to its lipophilicity. In order to overcome this low bioavailability, TQ is loaded into a colloidal drug carrier known as a nanostructured lipid carrier (NLC). This study aims to determine the antiproliferative effects of TQ and TQ-NLC on liver cancer cells integrated with the hepatitis B genome, Hep3B. The Hep3B was treated with TQ or TQ-NLC for 24, 48, and 72 hours via MTT assay. The results confirm that TQ or TQ-NLC inhibited the growth of Hep3B at IC50 <16.7 μM for 72 hours. TQ was also found to induce cell cycle arrest at the G1 checkpoint while TQ-NLC induced non-phase-specific cell cycle arrest. Further analysis using Annexin V staining confirmed the apoptotic induction of TQ or TQ-NLC via activation of caspases-3/7. In ROS management, TQ acted as a prooxidant (increased the level of ROS), while TQ-NLC acted as an antioxidant (reduced the level of ROS). Molecular analysis demonstrated that the GSH system and the Nrf2/Keap1 signaling pathway in Hep3B influenced the differential responses of the cells towards TQ or TQ-NLC. Hence, this study demonstrated that TQ and TQ-NLC have in vitro anticancer effects on the Hep3B.
    Matched MeSH terms: Inhibitory Concentration 50
  17. Ayob Z, Mohd Bohari SP, Abd Samad A, Jamil S
    PMID: 25574182 DOI: 10.1155/2014/732980
    Justicia gendarussa methanolic leaf extracts from five different locations in the Southern region of Peninsular Malaysia and two flavonoids, kaempferol and naringenin, were tested for cytotoxic activity. Kaempferol and naringenin were two flavonoids detected in leaf extracts using gas chromatography-flame ionization detection (GC-FID). The results indicated that highest concentrations of kaempferol and naringenin were detected in leaves extracted from Mersing with 1591.80 mg/kg and 444.35 mg/kg, respectively. Positive correlations were observed between kaempferol and naringenin concentrations in all leaf extracts analysed with the Pearson method. The effects of kaempferol and naringenin from leaf extracts were examined on breast cancer cell lines (MDA-MB-231 and MDA-MB-468) using MTT assay. Leaf extract from Mersing showed high cytotoxicity against MDA-MB-468 and MDA-MB-231 with IC50 values of 23 μg/mL and 40 μg/mL, respectively, compared to other leaf extracts. Kaempferol possessed high cytotoxicity against MDA-MB-468 and MDA-MB-231 with IC50 values of 23 μg/mL and 34 μg/mL, respectively. These findings suggest that the presence of kaempferol in Mersing leaf extract contributed to high cytotoxicity of both MDA-MB-231 and MDA-MB-468 cancer cell lines.
    Matched MeSH terms: Inhibitory Concentration 50
  18. Ahmad F, Seerangan P, Mustafa MZ, Osman ZF, Abdullah JM, Idris Z
    Malays J Med Sci, 2019 Mar;26(2):30-39.
    PMID: 31447606 MyJurnal DOI: 10.21315/mjms2019.26.2.4
    Background: There has been increasing evidence showing that stingless bee honey exhibits anti-oxidant, anti-inflammatory and anti-cancer properties. Pharmacologically-active components in honey such as flavonoids and phenolic constituents are known to contribute to its medicinal benefits. To the best of our knowledge, this is the first study on evaluating anti-cancer effects of locally-produced Malaysian stingless bee honey from Heterotrigona itama sp. on malignant glioma cells.

    Methods: Proliferation and apoptosis studies of U-87 MG cells following stingless bee honey treatment were carried out using MTS assay and acridine orange/propidium iodide dual staining, respectively.

    Results: Results demonstrated time and dose-dependent cytotoxicity using 0.625%, 1.25% and 10% stingless bee honey (P < 0.05). IC50 values were calculated using cells treated with 10% stingless bee honey. It was also observed that 10% stingless bee honey induced nuclear shrinkage, chromatin condensation and nucleus fragmentation, indicating that cellular changes were consistent with the apoptotic characteristics of the cells.

    Conclusion: These data provide a good basis for further evaluation of the medicinal properties of stingless bee honey from Heterotrigona itama sp. This source of honey may serve as a potential therapy for malignant glioma.

    Matched MeSH terms: Inhibitory Concentration 50
  19. Nwidu LL, Elmorsy E, Carter WG
    Malays J Med Sci, 2018 Mar;25(2):27-39.
    PMID: 30918453 DOI: 10.21315/mjms2018.25.2.4
    Background: Polyherbal standardised extracts used in ethnomedicine of Eastern Nigeria for memory improvements were evaluated for anti-cholinesterases and anti-oxidant properties.

    Methods: Anti-cholinesterase, anti-oxidant, and total phenolic and flavonoid contents were established using standard procedures.

    Results: The three polyherbal extracts exhibited significant concentration dependent acetylcholinesterase (AChE) inhibitory activity (P = 0.001). The highest AChE inhibition was observed with the Neocare Herbal Tea (NHT) with 99.7% (IC50 = 324 μg/mL); whereas the Herbalin Complex Tea (HCT) and Phytoblis Herbal Tea (PHT) exhibited 73.8% (IC50 = 0.2 μg/mL) and 60.6% (IC50 = 0.7 μg/mL) inhibition, respectively, relative to eserine at 100% inhibition (IC50 = 0.9 μg/mL) at 200 μg/mL. The order of percentage increase in inhibition of AChE was NHT > HCT > PHT; while the order of decrease in potency was HCT > PHT > NHT.Radical scavenging activities of HCT, NHT and PHT were 82.13% (IC50 = 0.08 μg/mL), 77.43% (IC50 = 0.01 μg/mL) and 76.28% (IC50 = 0.3 μg/mL), respectively, at 1 mg/mL concentrations. The reducing power revealed a dose-dependent effect, with NHT > PHT > HCT. The order of total phenolics content in the extracts were PHT > HCT > NHT, and for total flavonoids content: PHT > NHT > HCT.

    Conclusion: The three polyherbal standardised products possess significant acetylcholinesterase inhibitory activity and secondary metabolites that could collectively contribute to their memory-enhancing effects.

    Matched MeSH terms: Inhibitory Concentration 50
  20. Zin NNINM, Mohamad MN, Roslan K, Abdul Wafi S, Abdul Moin NI, Alias A, et al.
    Malays J Med Sci, 2020 Jul;27(4):36-50.
    PMID: 32863744 MyJurnal DOI: 10.21315/mjms2020.27.4.4
    Background: The spread of Plasmodium falciparum resistance in common antimalarial drugs, including artemisinin-based combination therapies, has necessitated the discovery of new drugs with novel mechanisms of action. In the present study, the in vitro antimalarial and toxicological activities of acetone, methanol, ethanol and aqueous extracts of Quercus infectoria (Q. infectoria) galls were investigated.

    Methods: The extracts were assessed for the antimalarial potential using a malarial SYBR Green I fluorescence-based (MSF) assay, while the toxicity was screened by using brine shrimp lethality test (BSLT), haemolytic assay, and cytotoxicity assay against normal embryo fibroblast cell line (NIH/3T3) and normal kidney epithelial cell line (Vero).

    Results: The acetone extract showed the highest antimalarial activity (50% inhibitory concentration, IC50 = 5.85 ± 1.64 μg/mL), followed by the methanol extract (IC50 = 10.31 ± 1.90 μg/mL). Meanwhile, the ethanol and aqueous extracts displayed low antimalarial activity with IC50 values of 20.00 ± 1.57 and 30.95 μg/mL ± 1.27 μg/mL, respectively. The significant antimalarial activity was demonstrated in all extracts and artemisinin (P < 0.05). All extracts were non-toxic to brine shrimps (50% lethality concentration, LC50 > 1000 ppm). Furthermore, no occurrence of haemolysis (< 5%) was observed in normal erythrocytes when treated with all extracts compared to Triton X-100 that caused 100% haemolysis (P < 0.05). The acetone and methanol extracts were non-toxic to the normal cell lines and statistically significant to artemisinin (P < 0.05).

    Conclusion: Taken together with satisfactory selectivity index (SI) values, the acetone and methanol extracts of Q. infectoria galls could serve as an alternative, promising and safe antimalarial agents.

    Matched MeSH terms: Inhibitory Concentration 50
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