Displaying publications 101 - 120 of 437 in total

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  1. Fulltext In Vitro and In Vivo Anticancer Activity of the Most Cytotoxic Fraction of Pistachio Hull Extract in Breast Cancer
    Seifaddinipour M, Farghadani R, Namvar F, Bin Mohamad J, Muhamad NA
    Molecules, 2020 Apr 13;25(8).
    PMID: 32295069 DOI: 10.3390/molecules25081776
    Pistacia (Pistacia vera) hulls (PV) is a health product that has been determined to contain bioactive phytochemicals which have fundamental importance for biomedical use. In this study, PV ethyl acetate extraction (PV-EA) fractions were evaluated with the use of an MTT assay to find the most cytotoxic fraction, which was found to be F13b1/PV-EA. After that, HPTLC was used for identify the most active compounds. The antioxidant activity was analyzed with DPPH and ABTS tests. Apoptosis induction in MCF-7 cells by F13b1/PV-EA was validated via flow cytometry analysis and a distinctive nuclear staining method. The representation of genes like Caspase 3, Caspase 8, Bax, Bcl-2, CAT and SOD was assessed via a reverse transcription (RT_PCR) method. Inhabitation of Tubo breast cancer cell development was examined in the BALB-neuT mouse with histopathology observations. The most abundant active components available in our extract were gallic acid and the flavonoid quercetin. The F13b1/PV-EA has antiradical activity evidence by its inhibition of ABTS and DPPH free radicals. F13b1/PV-EA displayed against MCF-7 a suppressive effect with an IC50 value of 15.2 ± 1.35 µg/mL. Also, the expression of CAT, SOD, Caspase 3, Caspase 8 and Bax increased and the expression of Bcl-2 decreased. F13b1/PV-EA dose-dependently inhibited tumor development in cancer-induced mice. Thus, this finding introduces F13b1/PV-EA as an effectual apoptosis and antitumor active agent against breast cancer.
    Matched MeSH terms: Inhibitory Concentration 50
  2. Fulltext Cytotoxic Effects and Anti-Angiogenesis Potential of Pistachio (Pistacia vera L.) Hulls against MCF-7 Human Breast Cancer Cells
    Seifaddinipour M, Farghadani R, Namvar F, Mohamad J, Abdul Kadir H
    Molecules, 2018 Jan 05;23(1).
    PMID: 29303970 DOI: 10.3390/molecules23010110
    Pistachio (Pistacia vera L.) hulls (PVLH) represents a significant by-product of industrial pistachio processing that contains high amounta of phenolic and flavonoid compounds known to act as antioxidants. The current study was designed to evaluate the anti-tumor and anti-angiogenic potentials of PVLH extracts. The cytotoxic effects of hexane, ethyl acetate, methanol, and water PVLH extracts toward human colon cancer (HT-29 and HCT-116), breast adenocarcinoma (MCF-7), lung adenocarcinoma (H23), liver hepatocellular carcinoma (HepG2), cervical cancer (Ca Ski), and normal fibroblast (BJ-5ta) cells were assessed using a MTT cell viability assay. Apoptosis induction was evaluated through the different nuclear staining assays and confirmed by flow cytometry analysis. Anti-angiogenic activities were also determined using chorioallantoic membrane (CAM) assay. PVLH ethyl acetate extracts (PVLH-EAE) demonstrated a suppressive effect with an IC50 value of 21.20 ± 1.35, 23.00 ± 1.2 and 25.15 ± 1.85 µg/mL against MCF-7, HT-29 and HCT-116, respectively, after 72 h of treatment. Morphological assessment and flow cytometry analysis showed the potential of PVLH-EAE to induce apoptosis. PVLH-EAE at the highest concentration demonstrated significant inhibition of angiogenesis as comparing with control group. Also the expression of Bax increased and the expression of Bcl-2 decreased in treated MCF-7 cells. Thus, the apoptosis induction and angiogenesis potential of PVLH-EAE make it to be the most suitable for further cancer research study to deal with selective antitumor active substances to human cancers especially breast cancer.
    Matched MeSH terms: Inhibitory Concentration 50
  3. Cytotoxic activity of phytochemicals from Garcinia mangostana L. and G. benthamiana (Planch. & Triana) Pipoly against breast cancer cells
    See I, Ee GCL, Jong VYM, Teh SS, Acuña CLC, Mah SH
    Nat Prod Res, 2020 Oct 23.
    PMID: 33094642 DOI: 10.1080/14786419.2020.1836629
    Four xanthones, α-mangostin (1), β-mangostin (2), mangostenol (3), mangaxanthone B (4), three benzophenones, mangaphenone (5), benthamianone (6), congestiflorone (7) and one sterol, stigmasterol (8) were isolated from the stem barks of Garcinia mangostana L. and G. benthamiana (Planch. & Triana) Pipoly. Compounds 1, 2, 4 and 5 exhibited significant cytotoxicity through MTT assay towards MCF-7 and MDA-MB-231 cells with the IC50 values range from 4.4 to 12.0 µM. Remarkably, mangaphenone (5) showed non-cytotoxicity against normal Vero cells, revealing its potential as lead compound for anti-breast cancer drug. Structure-activity relationship postulated that the prenyl and hydroxyl groups present in xanthones are important in promoting anti-proliferative effects. Molecular docking simulation study of 1, 2, 4 and 5 with 2OCF and 4PIV implied that the induction of apoptosis for both cancer cells involve ER and FAS signaling pathways. Future study on the lead optimization of 5 is highly recommended.
    Matched MeSH terms: Inhibitory Concentration 50
  4. Fulltext Antioxidant activity of Vernonia cinerea, Peperomia pellucida and the combination of Vernonia cinerea and Peperomia pellucida
    Sarini Ahmad Wakid, Nurul Syafiqah Zaharin
    Journal of Academia Universiti Teknologi MARA Negeri Sembilan, 2020;8(1):24-28.
    MyJurnal
    The present study was conducted to evaluate the antioxidant activity of Vernonia cinerea, Peperomia
    pellucida and combination of Vernonia cinerea and Peperomia pellucida. These two herbs are pants that
    often grow at random in different environments but are not commercialized due to the fact that no
    comprehensive study of the importance of their use. The extract was prepared with methanol respectively.
    1,1-diphenyl-2-picrylhydrazyl (DPPH) assay were used to study their antioxidant activity. The extracts
    were compared with commercial antioxidant, butylated hydroxytoluene (BHT). The highest scavenging
    effect from peel extract was presented by Vernonia cinerea with the value of 76.3% scavenging activity
    (IC50 = 2.909), followed by the combination of Vernonia cinerea and Peperomia pellucida (71.21%
    scavenging activity; IC50 = 5.274) and Peperomia pellucida with value of 68.3% scavenging activity (IC50
    = 5.572). BHT showed the lowest IC50 value 1.71 with the scavenging activity 90.0%. Low IC50 value will
    indicates the strong ability of the extracts to act as DPPH scavenger.
    Matched MeSH terms: Inhibitory Concentration 50
  5. Fulltext Antioxidant activity of melon fruit peel extracts
    Sarini Ahmad Wakid, Hamira Azrin binti Harun
    Journal of Academia Universiti Teknologi MARA Negeri Sembilan, 2020;8(1):53-57.
    MyJurnal
    The present study was conducted to evaluate the antioxidant activity of peel extract from three types of
    melon, Cucumis melo var cantalupensis, Cucumis melo var inodorus and Citrullus lanatus in family
    Curcurbitaceae. The extract was prepared with methanol respectively. 1,1-diphenyl-2-picrylhydrazyl
    (DPPH) assay were used to study their antioxidant activity. The extracts were compared with commercial
    antioxidant, butylated hydroxytoluene (BHT). The highest scavenging effect from peel extract was
    presented by Cucumis melo var inodorus with the value of 52.7 ± 9.1µg/ml (IC50 = 4.61). BHT showed
    the lowest IC50 value 1.71 with the scavenging activity 90.0 ± 1.7µg/ml. Low IC50 value will indicates the
    strong ability of the extracts to act as DPPH scavenger.

    Matched MeSH terms: Inhibitory Concentration 50
  6. Fulltext Novel piperazine core compound induces death in human liver cancer cells: possible pharmacological properties
    Samie N, Muniandy S, Kanthimathi MS, Haerian BS, Azudin RE
    Sci Rep, 2016 Apr 13;6:24172.
    PMID: 27072064 DOI: 10.1038/srep24172
    The current study evaluates the cytotoxic mechanism of a novel piperazine derivate designated as PCC against human liver cancer cells. In this context, human liver cancer cell lines, SNU-475 and 243, human monocyte/macrophage cell line, CRL-9855, and human B lymphocyte cell line, CCL-156, were used to determine the IC50 of PCC using the standard MTT assay. PCC displayed a strong suppressive effect on SNU-475 and SNU-423 cells with an IC50 value of 6.98 ± 0.11 μg/ml and 7.76 ± 0.45 μg/ml respectively, after 24 h of treatment. Significant dipping in the mitochondrial membrane potential and elevation in the released of cytochrome c from the mitochondria indicated the induction of the intrinsic apoptosis pathway by PCC. Activation of this pathway was further evidenced by significant activation of caspase 3/7 and 9. PCC was also shown to activate the extrinsic pathways of apoptosis via activation of caspase-8 which is linked to the suppression of NF-ƙB translocation to the nucleus. Cell cycle arrest in the G1 phase was confirmed by flow cytometry and up-regulation of glutathione reductase expression was quantified by qPCR. This study suggests that PCC is a simultaneous inducer of intrinsic and extrinsic pathways of apoptosis in liver cancer cell lines.
    Matched MeSH terms: Inhibitory Concentration 50
  7. Fulltext Mechanism of Action of the Novel Nickel(II) Complex in Simultaneous Reactivation of the Apoptotic Signaling Networks Against Human Colon Cancer Cells
    Samie N, Haerian BS, Muniandy S, Marlina A, Kanthimathi MS, Abdullah NB, et al.
    Front Pharmacol, 2015;6:313.
    PMID: 26858642 DOI: 10.3389/fphar.2015.00313
    The aim of this study was to evaluate the cytotoxic potential of a novel nickel(II) complex (NTC) against WiDr and HT-29 human colon cancer cells by determining the IC50 using the standard MTT assay. The NTC displayed a strong suppressive effect on colon cancer cells with an IC50 value of 6.07 ± 0.22 μM and 6.26 ± 0.13 μM against WiDr and HT-29 respectively, after 24 h of treatment. Substantial reduction in the mitochondrial membrane potential and increase in the release of cytochrome c from the mitochondria directed the induction of the intrinsic apoptosis pathway by the NTC. Activation of this pathway was further evidenced by significant activation of caspase 3/7 and 9. The NTC was also shown to activate the extrinsic pathway of apoptosis via activation of caspase-8 which is linked to the suppression of NF-κB translocation to the nucleus. Cell cycle arrest in the G1 phase was confirmed by flow cytometry and up-regulation of glutathione reductase expression was quantified by qPCR. Results of the current work indicates that NTC possess a potent cancer cell abolishing activity by simultaneous induction of intrinsic and extrinsic pathways of apoptosis in colon cancer cell lines.
    Matched MeSH terms: Inhibitory Concentration 50
  8. Some Studies into the Effects of Metaldehyde on Cultured Cells
    Salmijah S., Anita Mohd. Zubir, Maimon A.
    Sains Malaysiana, 1997;26.
    Metaldehyde is used widely in Malaysia for the control of molluscs. This communication reports the cytotoxic effects of this chemical on cultured cells as assessed by cell morphology and the DNA synthesising capability as well as its transport into cells. After 15 days of exposure with 20.0 ppm of the compound, the DNA synthesising capability was shown to be unaffected. The IC50 for Vero cells was 276.0 ppm. Transport of thymidine across cells was found to be not significantly affected even at high metaldehyde concentrations (up to 320.0 ppm) suggesting integrity of cells were not significantly affected. The present cellular studies have therefore shown that the cytotoxic effects of this chemical is rather low.
    Metaldehida digunakan dengan meluas di Malaysia untuk mengawal perosak moluska. Kesan sitotoksik bahan kimia ini di peringkat sel dari segi ciri-ciri perubahan moifologi dan keupayaan mensintesis DNA serta kajian awal kesannya terhadap proses kemasukan ke dalam sel dilaporkan di sini. Keupayaan mensintesis DNA didapati tidak terjejas secara signifikan selepas diberikan 20.0 ppm metaldehida secara berterusan selama 15 hari. Nilai IC50 bagi sel Vero adalah 276.0 ppm. Kemasukan timidina ke dalam sel tidak terjejas secara signifikan apabila sel diperlakukan dengan metaldehida, walaupun pada kepekatan yang agak tinggi iaitu sehingga 320.0 ppm. Kajian telah menunjukkan bahawa kesan sitotoksik oleh metaldehida adalah rendah.
    Matched MeSH terms: Inhibitory Concentration 50
  9. Fulltext Ergogenic, anti-diabetic and antioxidant attributes of selected Malaysian herbs: characterisation of flavonoids and correlation of functional activities
    Sallehuddin, N. A., Azizah Abdul Hamid, Salleh, S. Z., Nazia Abdul Majid, Hani Hafeeza Halim, Nurul Shazini Ramli, et al.
    International Food Research Journal, 2020;27(1):197-207.
    MyJurnal
    In the present work, aqueous ethanolic (60% ethanol) extracts from selected Malaysian herbs
    including Murraya koenigii L. Spreng, Lawsonia inermis L., Cosmos caudatus Kunth, Piper
    betle L., and P. sarmentosum Roxb. were evaluated for their ergogenic, anti-diabetic and
    antioxidant potentials. Results showed that the analysed herbs had ergogenic property and
    were able to activate 5'AMP-activated protein kinase (AMPK) in a concentration dependant
    manner. The highest AMPK activation was exhibited by M. koenigii extract which showed no
    significant (p > 0.05) difference with green tea (positive control). For anti-diabetic potential,
    the highest α-glucosidase inhibition was exhibited by M. koenigii extract with IC50 of 43.35
    ± 7.5 µg/mL, which was higher than acarbose (positive control). The determinations of free
    radical scavenging activity and total phenolics content (TPC) indicated that the analysed herbs
    had good antioxidant activity. However, C. caudatus extract showed superior antioxidant
    activity with IC50 against free radical and TPC of 21.12 ± 3.20 µg/mL and 221.61 ± 7.49 mg
    GAE/g, respectively. RP-HPLC analysis established the presence of flavonoids in the herbs
    wherein L. inermis contained the highest flavonoid (catechin, epicatechin, naringin and rutin)
    content (668.87 mg/kg of extract). Correlations between the analyses were conducted, and
    revealed incoherent trends. Overall, M. koenigii was noted to be the most potent herb for
    enhancement of AMPK activity and α-glucosidase inhibition but exhibited moderate antioxidant activity. These results revealed that the selected herbs could be potential sources of
    natural ergogenic and anti-diabetic/antioxidant agents due to their rich profile of phenolics.
    Further analysis in vivo should be carried out to further elucidate the mechanism of actions of
    these herbs as ergogenic aids and anti-diabetic/antioxidant agents.
    Matched MeSH terms: Inhibitory Concentration 50
  10. Chemical investigation and biological activities of the essential oil of Knema kunstleri Warb. from Malaysia
    Salleh WMNHW, Anuar MZA, Khamis S, Nafiah MA, Sul'ain MD
    Nat Prod Res, 2021 Jul;35(13):2279-2284.
    PMID: 31544509 DOI: 10.1080/14786419.2019.1669027
    The chemical composition of the essential oil of Knema kunstleri Warb. (Myristicaceae) was investigated for the first time. The essential oil was obtained by hydrodistillation and fully characterized by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). In total, 36 components were identified in the essential oil, which made up 91.7% of the total oil. The essential oil is composed mainly of β-caryophyllene (23.2%), bicyclogermacrene (9.6%), δ-cadinene (7.3%), α-humulene (5.7%), and germacrene D (4.3%). The essential oil showed moderate activity towards DPPH free-radical scavenging and lipoxygenase inhibition. To the best of our knowledge, this is the first study of the composition and bioactivities of the essential oil report concerning the genus Knema.
    Matched MeSH terms: Inhibitory Concentration 50
  11. Fulltext Extraction and purification of Cytotoxic compounds from Premna Serratifolia L. (Bebuas) for human breast cancer treatment
    Salih, G.A., Ahmad-Raus, R., Shaban, M.N., Abdullah, N.
    International Food Research Journal, 2017;24(101):0-0.
    MyJurnal
    Breast cancer is considered as one of the most common cancers all over the world. A huge effort has been made to create a safe and cost effective breast cancer treatment. All of these features exist in the plants sources. In this study, the effect of local vegetable salad, Premna serratifolia (Bebuas) against MCF-7 cells (human breast adenocarcinoma) was determined. The optimum condition to extract breast cancer cytotoxic compound from the plant was investigated and the exact cytotoxic compound was identified as well. To determine the plant cytotoxicity effect against MCF-7 cells, MTT assay was used. Two important parameters in the sonication extraction method which are duration of time and temperature were optimized by carrying out a series of experiments which were designed by Face Centered Central Composite Design (FCCCD). The extraction efficiency of each experiment was determined by measuring the yield of extract and the half maximal inhibitory concentration (IC50) of the extract against MCF-7 cells. The results obtained from the experiments were fitted to the second order polynomial model to generate equation that was used to determine best extraction processing condition. Based on the generated equation, the best sonication processing condition to extract the cytotoxic compound is at 30oC for 67 min. Analysis of variance (ANOVA) showed that the duration of extraction time has great influence (p
    Matched MeSH terms: Inhibitory Concentration 50
  12. Fulltext UPLC-MS-Based Metabolomics Profiling for α-Glucosidase Inhibiting Property of Parkia speciosa Pods
    Saleh MSM, Jalil J, Mustafa NH, Ramli FF, Asmadi AY, Kamisah Y
    Life (Basel), 2021 Jan 22;11(2).
    PMID: 33499128 DOI: 10.3390/life11020078
    Parkia speciosa is a food plant that grows indigenously in Southeast Asia. A great deal of interest has been paid to this plant due to its traditional uses in the treatment of several diseases. The pods contain many beneficial secondary metabolites with potential applications in medicine and cosmetics. However, studies on their phytochemical properties are still lacking. Therefore, the present study was undertaken to profile the bioactive compounds of P. speciosa pods collected from six different regions of Malaysia through ultra-high-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UHPLC-QTOF-MS) and α-glucosidase inhibitory potential. This study applied metabolomics to elucidate the differences between P. speciosa populations found naturally in the different locations and to characterize potential α-glucosidase inhibitors from P. speciosa pods. P. speciosa collected from different regions of Malaysia showed good α-glucosidase inhibitory activity, with a median inhibitory concentration (IC50) of 0.45-0.76 μg/mL. The samples from the northern and northeastern parts of Peninsular Malaysia showed the highest activity. Using UHPLC-QTOF-MS/MS analysis, 25 metabolites were identified in the pods of P. speciosa. The findings unveiled that the pods of P. speciosa collected from different locations exhibit different levels of α-glucosidase inhibitory activity. The pods are a natural source of potent antidiabetic bioactive compounds.
    Matched MeSH terms: Inhibitory Concentration 50
  13. Thiadiazole derivatives as New Class of β-glucuronidase inhibitors
    Salar U, Taha M, Ismail NH, Khan KM, Imran S, Perveen S, et al.
    Bioorg Med Chem, 2016 Apr 15;24(8):1909-18.
    PMID: 26994638 DOI: 10.1016/j.bmc.2016.03.020
    Thiadiazole derivatives 1-24 were synthesized via a single step reaction and screened for in vitro β-glucuronidase inhibitory activity. All the synthetic compounds displayed good inhibitory activity in the range of IC50=2.16±0.01-58.06±1.60μM as compare to standard d-saccharic acid 1,4-lactone (IC50=48.4±1.25μM). Molecular docking study was conducted in order to establish the structure-activity relationship (SAR) which demonstrated that thiadiazole as well as both aryl moieties (aryl and N-aryl) involved to exhibit the inhibitory potential. All the synthetic compounds were characterized by spectroscopic techniques (1)H, (13)C NMR, and EIMS.
    Matched MeSH terms: Inhibitory Concentration 50
  14. Fulltext Chemopreventive Effects of Germinated Rough Rice Crude Extract in Inhibiting Azoxymethane-Induced Aberrant Crypt Foci Formation in Sprague-Dawley Rats
    Saki E, Saiful Yazan L, Mohd Ali R, Ahmad Z
    Biomed Res Int, 2017;2017:9517287.
    PMID: 28116312 DOI: 10.1155/2017/9517287
    Chemoprevention has become an important area in cancer research due to low success rate of current therapeutic modalities. Diet plays a vital role in the etiology of cancer. This research was carried out to study the chemopreventive properties of germinated rough rice (GRR) crude extract in Sprague-Dawley rats induced with azoxymethane. Germination of rough rice causes significant changes in several chemical compositions of presently bioactive compounds. These compounds may prevent or postpone the inception of cancer. Fifty male Sprague-Dawley rats (6 weeks of age) were randomly divided into 5 groups which were (G1) induced with azoxymethane (AOM) and not given GRR (positive control), (G2) induced with AOM and given 2000 mg/kg GRR, (G3) induced with AOM and given 1000 mg/kg GRR, (G4) induced with AOM and given 500 mg/kg GRR, and (G5) not induced with AOM and not given GRR crude extract (negative control). To induce colon cancer, rats received two IP injections of AOM in saline (15 mg/kg) for two subsequent weeks. Organs were removed and weighed. Aberrant crypt foci (ACF) were evaluated histopathologically. β-Catenin expressions were determined by Western blot. Treatment with 2000 mg/kg GRR crude extract not only resulted in the greatest reduction in the size and number of ACF but also displayed the highest percentage of nondysplastic ACF. Treatment with 2000 mg/kg GRR also gave the lowest level of expression in β-catenin. Thus, GRR could be a promising dietary supplement for prevention of CRC.
    Matched MeSH terms: Inhibitory Concentration 50
  15. Discovery of small molecule inhibitors against the NS3/4A serine protease of Hepatitis C virus genotype 3 via highthroughput virtual screening and in vitro evaluations
    Sakhor W, Teoh TC, Yusof R, Lim SK, Razif MFM
    Trop Biomed, 2020 Sep 01;37(3):609-625.
    PMID: 33612776 DOI: 10.47665/tb.37.3.609
    The hepatitis C virus (HCV) consists of eight genotypes and 90 subtypes, with genotype (GT) 3 being the second most common globally and is linked to higher incidences of steatosis and rapid development of fibrosis and cirrhosis. The NS3/4A serine protease, a heterodimer complex of two HCV non-structural proteins, is an effective target for pharmaceutical intervention due to its essential roles in processing HCV polyproteins and inhibiting innate immunity. This study combines structure-based virtual screening (SBVS) of predefined compound libraries, pharmacokinetic prediction (ADME/T) and in vitro evaluation to identify potential low molecular weight (<500 Dalton) inhibitors of the NS3/4A serine protease (GT3). In silico screening of ZINC and PubChem libraries yielded five selected compounds as potential candidates. Dose-dependent inhibition of the NS3/4A serine protease and HCV replication in HuH-7.5 cells revealed that compound A (PubChem ID No. 16672637) exhibited inhibition towards HCV GT3 with an IC50 of 106.7µM and EC50 of 25.8µM, respectively. Thus, compound A may be developed as a potent, low molecular weight drug against the HCV NS3/4A serine protease of GT3.
    Matched MeSH terms: Inhibitory Concentration 50
  16. Fulltext Key drug-targeting genes in pancreatic ductal adenocarcinoma
    Sakharkar MK, Dhillon SK, Mazumder M, Yang J
    Genes Cancer, 2021;12:12-24.
    PMID: 33884102 DOI: 10.18632/genesandcancer.210
    Pancreatic ductal adenocarcinoma (PDAC) is a highly lethal type of cancer. In this study, we undertook a pairwise comparison of gene expression pattern between tumor tissue and its matching adjacent normal tissue for 45 PDAC patients and identified 22 upregulated and 32 downregulated genes. PPI network revealed that fibronectin 1 and serpin peptidase inhibitor B5 were the most interconnected upregulated-nodes. Virtual screening identified bleomycin exhibited reasonably strong binding to both proteins. Effect of bleomycin on cell viability was examined against two PDAC cell lines, AsPC-1 and MIA PaCa-2. AsPC-1 did not respond to bleomycin, however, MIA PaCa-2 responded to bleomycin with an IC50 of 2.6 μM. This implicates that bleomycin could be repurposed for the treatment of PDAC, especially in combination with other chemotherapy agents. In vivo mouse xenograft studies and patient clinical trials are warranted to understand the functional mechanism of bleomycin towards PDAC and optimize its therapeutic efficacy. Furthermore, we will evaluate the antitumor activity of the other identified drugs in our future studies.
    Matched MeSH terms: Inhibitory Concentration 50
  17. Fulltext In Vitro Testing of Potential Entamoeba histolytica Pyruvate Phosphate Dikinase Inhibitors
    Saidin S, Othman N, Noordin R
    Am J Trop Med Hyg, 2017 Oct;97(4):1204-1213.
    PMID: 28820699 DOI: 10.4269/ajtmh.17-0132
    Adverse effects and resistance to metronidazole have motivated the search for new antiamoebic agents against Entamoeba histolytica. Control of amoeba growth may be achieved by inhibiting the function of the glycolytic enzyme and pyruvate phosphate dikinase (PPDK). In this study, we screened 10 compounds using an in vitro PPDK enzyme assay. These compounds were selected from a virtual screening of compounds in the National Cancer Institute database. The antiamoebic activity of the selected compounds was also evaluated by determining minimal inhibitory concentrations (MICs) and IC50 values using the nitro-blue tetrazolium reduction assay. Seven of the 10 compounds showed inhibitory activities against the adenosine triphosphate (ATP)/inorganic phosphate binding site of the ATP-grasp domain. Two compounds, NSC349156 (pancratistatin) and NSC228137 (7-ethoxy-4-[4-methylphenyl] sulfonyl-3-oxido-2, 1, 3-benzoxadiazol-3-ium), exhibited inhibitory effects on the growth of E. histolytica trophozoites with MIC values of 25 and 50 μM, and IC50 values of 14 and 20.7 μM, respectively.
    Matched MeSH terms: Inhibitory Concentration 50
  18. Berberis vulgaris fruit crude extract as a novel anti-leukaemic agent
    Saedi TA, Ghafourian S, Jafarlou M, Sabariah MN, Ismail P, Eusni RM, et al.
    J Biol Regul Homeost Agents, 2015 Apr-Jun;29(2):395-9.
    PMID: 26122228
    Tumor protein p53 encoded by the TP53 gene in humans is known as a cancer biomarker in patients diagnosed with cancer, and it plays an essential role in apoptosis, genomic stability, and inhibition of angiogenesis. Cancer therapies with common chemotherapy methods are effective, as known, but have some side effects. Berberis vulgaris is traditionally administrated as a cancer drug. The current research aims to evaluate p53 as a biomarker in WEHI-3 cell line and to demonstrate the Berberis vulgaris fruit crude extract (BVFCE) as a new anticancer drug. For this purpose, we evaluated the effect of BVFCE in different concentrations against WEHI-3cell line in vitro and determined the quantitative level of p53 gene in the treated WEHI-3 cells. The results demonstrated that even at only 1 mg/ml concentration of Berberis vulgaris crude extract, there was a low level of p53 biomarker expression on WEHI-3 cells in comparison with doxorubicin. Therefore, the current study suggests BVFCE as a reliable anti-leukaemic drug and candidate for anticancer therapy. However, further investigation need be carried out to confirm its efficiency in vivo.
    Matched MeSH terms: Inhibitory Concentration 50
  19. 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.
    Matched MeSH terms: Inhibitory Concentration 50
  20. Induction of cell death and modulation of Annexin A1 by phytoestrogens in human leukemic cell lines
    Sabran A, Kumolosasi E, Jantan I, Jamal JA, Azmi N, Jasamai M
    Saudi Pharm J, 2021 Jan;29(1):73-84.
    PMID: 33603542 DOI: 10.1016/j.jsps.2020.12.011
    Background: Phytoestrogens are polyphenolic plant compounds which are structurally similar to the endogenous mammalian estrogen, 17β-estradiol. Annexin A1 (ANXA1) is an endogenous protein which inhibits cyclo-oxygenase 2 (COX-2) and phospholipase A2, signal transduction, DNA replication, cell transformation, and mediation of apoptosis.

    Objective: This study aimed to determine the effects of selected phytoestrogens on annexin A1 (ANXA1) expression, mode of cell death and cell cycle arrest in different human leukemic cell lines.

    Methods: Cells viability were examined by MTT assay and ANXA1 quantification via Enzyme-linked Immunosorbent Assay. Cell cycle and apoptosis were examined by flow cytometer and phagocytosis effect was evaluated using haematoxylin-eosin staining.

    Results: Coumestrol significantly (p 

    Matched MeSH terms: Inhibitory Concentration 50
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