Displaying publications 101 - 120 of 437 in total

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  1. Chemical constituents from Garcinia maingayi and Garcinia paroifolia (Guttiferae) and their biological activities
    Ee, G.C.L., Cheow, Y.L.
    Pertanika Journal of Science & Technology, 2007;15(2):95-102.
    MyJurnal
    Detail chemical studies on Carcinia maingayi have yielded one xanthone, 1,3,7-trihydroxy-2-(3-methylbut-2-enyl)-xanthone, one benzophenone, isoxanthochymol, one benzoic acid derivative 3,4-dihydroxy-methylbenzoate and two triterpenoids, stigmasterol and sitosterol. Meanwhile, investigations on Carcinia parvifolia have afforded one triterpenoid, a-amyrin and two xanthones, cowanin and rubraxanthone. Their structures were derived based on spectroscopic evidence, mainly ID and 2D NMR spectroscopy. Acetylation reaction was carried out on rubraxanthone to yield triacetate rubraxanthone. It was found that the pure rubraxanthone was strongly active against the larvae of Aedes aegypti with LC50 value of 15.49 {lg/ ml and HL-60 cells line with an IC50 value of 7.5 {lg/ ml.
    Matched MeSH terms: Inhibitory Concentration 50
  2. Fulltext In vitro assessment of anti-proliferative effect induced by α-mangostin from Cratoxylum arborescens on HeLa cells
    El Habbash AI, Mohd Hashim N, Ibrahim MY, Yahayu M, Omer FAE, Abd Rahman M, et al.
    PeerJ, 2017;5:e3460.
    PMID: 28740747 DOI: 10.7717/peerj.3460
    Natural medicinal products possess diverse chemical structures and have been an essential source for drug discovery. Therefore, in this study, α-mangostin (AM) is a plant-derived compound was investigated for the apoptotic effect on human cervical cancer cells (HeLa). The cytotoxic effects of AM on the viability of HeLa and human normal ovarian cell line (SV40) were evaluated by using MTT assay. Results showed that AM inhibited HeLa cells viability at concentration- and time-dependent manner with IC50 value of 24.53 ± 1.48 µM at 24 h. The apoptogenic effects of AM on HeLa were assessed using fluorescence microscopy analysis. The effect of AM on cell proliferation was also studied through clonogenic assay. ROS production evaluation, flow cytometry (cell cycle) analysis, caspases 3/7, 8, and 9 assessment and multiple cytotoxicity assays were conducted to determine the mechanism of cell apoptosis. This was associated with G2/M phase cell cycle arrest and elevation in ROS production. AM induced mitochondrial apoptosis which was confirmed based on the significant increase in the levels of caspases 3/7 and 9 in a dose-dependent manner. Furthermore, the MMP disruption and increased cell permeability, concurrent with cytochrome c release from the mitochondria to the cytosol provided evidence that AM can induce apoptosis via mitochondrial-dependent pathway. AM exerted a remarkable antitumor effect and induced characteristic apoptogenic morphological changes on HeLa cells, which indicates the occurrence of cell death. This study reveals that AM could be a potential antitumor compound on cervical cancer in vitro and can be considered for further cervical cancer preclinical and in vivo testing.
    Matched MeSH terms: Inhibitory Concentration 50
  3. Fulltext Anti-viral activity of culinary and medicinal mushroom extracts against dengue virus serotype 2: an in-vitro study
    Ellan K, Thayan R, Raman J, Hidari KIPJ, Ismail N, Sabaratnam V
    BMC Complement Altern Med, 2019 Sep 18;19(1):260.
    PMID: 31533688 DOI: 10.1186/s12906-019-2629-y
    BACKGROUND: Dengue is a mosquito-borne viral infection that has become a major public health concern worldwide. Presently, there is no specific vaccine or treatment available for dengue viral infection.

    METHODS: Lignosus rhinocerotis, Pleurotus giganteus, Hericium erinaceus, Schizophyllum commune and Ganoderma lucidium were selected for evaluation of their in-vitro anti-dengue virus serotype 2 (DENV-2) activities. Hot aqueous extracts (HAEs), ethanol extracts (EEs), hexane soluble extracts (HSEs), ethyl acetate soluble extracts (ESEs) and aqueous soluble extracts (ASEs) were prepared from the selected mushrooms. The cytotoxic effects of the extracts were evaluated by the MTT assay. The anti-DENV-2 activities of the extracts were evaluated in three different assays: simultaneous, attachment and penetration assays were perfomed using plaque reduction assays and RT-qPCR assays. The effect of the addition time on viral replication was assessed by the time of addition assay, and a virucidal assay was carried out to evaluate the direct effect of each mushroom extract on DENV-2. The chemical composition of glucans, and the protein and phenolic acid contents in the extracts were estimated.

    RESULTS: We found that the HAEs and ASEs of L. rhinocerotis, P. giganteus, H. erinaceus and S. commune were the least toxic to Vero cells and showed very prominent anti-DENV2 activity. The 50% inhibitory concentration (IC50) values of the ASEs ranged between 399.2-637.9 μg/ml, while for the HAEs the range was 312.9-680.6 μg/ml during simultaneous treatment. Significant anti-dengue activity was also detected in the penetration assay of ASEs (IC50: 226.3-315.4 μg/ml) and HAEs (IC50: 943.1-2080.2 μg/ml). Similarly, we observed a marked reduction in the expression levels of the ENV and NS5 genes in the simultaneous and penetration assays of the ASEs and HAEs. Time-of-addition experiments showed that the highest percent of anti-DENV2 activity was observed when the mushroom extracts were added immediately after virus adsorption. None of the extracts exhibited virucidal effect. Chemical composition analysis showed that the major components in the mushroom HAEs and ASEs were glucan (beta D-glucan) and proteins, however, there was no significant correlation between the anti-dengue activity and the concentration of glucans and proteins.

    CONCLUSION: These findings demonstrated the potential of mushroom extracts as anti-dengue therapeutic agents with less toxic effects.

    Matched MeSH terms: Inhibitory Concentration 50
  4. Fulltext Mushrooms: a potential natural source of anti-inflammatory compounds for medical applications
    Elsayed EA, El Enshasy H, Wadaan MA, Aziz R
    Mediators Inflamm, 2014;2014:805841.
    PMID: 25505823 DOI: 10.1155/2014/805841
    For centuries, macrofungi have been used as food and medicine in different parts of the world. This is mainly attributed to their nutritional value as a potential source of carbohydrates, proteins, amino acids, and minerals. In addition, they also include many bioactive metabolites which make mushrooms and truffles common components in folk medicine, especially in Africa, the Middle East, China, and Japan. The reported medicinal effects of mushrooms include anti-inflammatory effects, with anti-inflammatory compounds of mushrooms comprising a highly diversified group in terms of their chemical structure. They include polysaccharides, terpenoids, phenolic compounds, and many other low molecular weight molecules. The aims of this review are to report the different types of bioactive metabolites and their relevant producers, as well as the different mechanisms of action of mushroom compounds as potent anti-inflammatory agents.
    Matched MeSH terms: Inhibitory Concentration 50
  5. Fulltext Rho-Kinase II Inhibitory Potential of Eurycoma longifolia New Isolate for the Management of Erectile Dysfunction
    Ezzat SM, Okba MM, Ezzat MI, Aborehab NM, Mohamed SO
    Evid Based Complement Alternat Med, 2019;2019:4341592.
    PMID: 31223329 DOI: 10.1155/2019/4341592
    Background. Eurycoma longifolia Jack (Fam.: Simaroubaceae), known as Tongkat Ali (TA), has been known as a symbol of virility and sexual power. The aim of the study was to screen E. longifolia aqueous extract (AE) and isolates for ROCK-II inhibition. Results. The AE (1-10 μg/ml) showed a significant inhibition for ROCK-II activity (62.8-81%) at P < 0.001 with an IC50 (651.1 ± 32.9 ng/ml) compared to Y-27632 ([(+)-(R)-trans-4-(1-aminoethyl)-N-(4-pyridyl)cyclohexanecarboxamide dihydrochloride]) (68.15-89.9 %) at same concentrations with an IC50 (192 ± 8.37 ng/ml). Chromatographic purification of the aqueous extract (AE) allowed the isolation of eight compounds; stigmasterol T1, trans-coniferyl aldehyde T2, scopoletin T3, eurycomalactone T4, 6α- hydroxyeurycomalactone T5, eurycomanone T6, eurycomanol T7, and eurycomanol-2-O-β-D-glucopyranoside T8. This is the first report for the isolation of T1 and T3 from E. longifolia and for the isolation of T2 from genus Eurycoma. The isolates (at 10 μg/ml) exhibited maximum inhibition % of ROCK-II 82.1 ± 0.63 (T2), 78.3 ± 0.38 (T6), 77.1 ± 0.11 (T3), 76.2 ± 3.53 (T4), 74.5 ± 1.27 (T5), 74.1 ± 2.97 (T7), 71.4 ± 2.54 (T8), and 60.3 ± 0.14 (T1), where the newly isolated compound trans-coniferyl aldehyde T2 showed the highest inhibitory activity among the tested isolated compounds and even higher than the total extract AE. The standard Y-27632 (10 μg/ml) showed 89.9 ± 0.42 % inhibition for ROCK-II activity when compared to control at P < 0.0001. Conclusion. The traditional use of E. longifolia as aphrodisiac and for male sexual disorders might be in part due to the ROCK-II inhibitory potential.
    Matched MeSH terms: Inhibitory Concentration 50
  6. Fulltext Cholinesterase enzymes inhibitors from the leaves of Rauvolfia reflexa and their molecular docking study
    Fadaeinasab M, Hadi AH, Kia Y, Basiri A, Murugaiyah V
    Molecules, 2013 Mar 25;18(4):3779-88.
    PMID: 23529036 DOI: 10.3390/molecules18043779
    Plants of the Apocynaceae family have been traditionally used in the treatment of age-related brain disorders. Rauvolfia reflexa, a member of the family, has been used as an antidote for poisons and to treat malaria. The dichloromethane, ethanol and methanol extracts from the leaves of Rauvolfia reflexa showed potential acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities, with IC50 values in the 8.49 to 52.23 g/mL range. Further cholinesterase inhibitory-guided isolation of these extracts afforded four bioactive compounds, namely: (E)-3-(3,4,5-trimethoxyphenyl)acrylic acid (1), (E)-methyl 3-(4-hydroxy-3,5-dimethoxyphenyl) acrylate (2), 17-methoxycarbonyl-14-heptadecaenyl-4-hydroxy-3-methoxycinnamate (3) and 1,2,3,4-tetrahydro-1-oxo-β-carboline (4). The isolated compounds showed moderate cholinesterase inhibitory activity compared to the reference standard, physostigmine. Compounds 1 and 2 showed the highest inhibitory activity against AChE (IC50 = 60.17 µM) and BChE (IC50 = 61.72 µM), respectively. Despite having similar molecular weight, compounds 1 and 2 were structurally different according to their chemical substitution patterns, leading to their different enzyme inhibition selectivity. Compound 2 was more selective against BChE, whereas compound 1 was a selective inhibitor of AChE. Molecular docking revealed that both compounds 1 and 2 were inserted, but not deeply into the active site of the cholinesterase enzymes.
    Matched MeSH terms: Inhibitory Concentration 50
  7. Fulltext Gamma-tocotrienol Alters Protein Expression of HepG2 Cell Line
    Farahani, A.S.R., Zakiah, J., Abdul Rahman, M., Karsani, S.A., Wan, Ngah Wz
    Medicine & Health, 2008;3(2):256-262.
    MyJurnal
    Gamma-tocotrienol (GTT) has been shown to exhibit significant antitumor activity in a variety of tumor cells. Previous findings have demonstrated that GTT had antiprolifera-tive effects on a liver cancer cell line (HepG2) with an IC50  value of 170μM. In this study, two dimensional gel electrophoresis (2DE) was used to determine changes in protein expression in HepG2 cell line following treatment with GTT. The ultimate aim is to identify the possible molecular mechanisms involved in GTT antitumor activity. This study is focused on obtaining a 2DE protein profile for HepG2 cell line with and without
    GTT treatment. In the preliminary analysis  of the resulting 2DE profiles, 18 protein spots were found to be differentially expressed in cells treated with GTT. This observa-tion is confirmed by extending the analysis  to a larger sample size. By studying the effects of GTT treatment on differential protein expression in HepG2 cells the underly-ing mechanisms involved in the antitumor activity of GTT may be elucidated.
    Matched MeSH terms: Inhibitory Concentration 50
  8. Fulltext Synthesis, characterization, and anticancer activity of new quinazoline derivatives against MCF-7 cells
    Faraj FL, Zahedifard M, Paydar M, Looi CY, Abdul Majid N, Ali HM, et al.
    ScientificWorldJournal, 2014;2014:212096.
    PMID: 25548779 DOI: 10.1155/2014/212096
    Two new synthesized and characterized quinazoline Schiff bases 1 and 2 were investigated for anticancer activity against MCF-7 human breast cancer cell line. Compounds 1 and 2 demonstrated a remarkable antiproliferative effect, with an IC50 value of 6.246×10(-6) mol/L and 5.910×10(-6) mol/L, respectively, after 72 hours of treatment. Most apoptosis morphological features in treated MCF-7 cells were observed by AO/PI staining. The results of cell cycle analysis indicate that compounds did not induce S and M phase arrest in cell after 24 hours of treatment. Furthermore, MCF-7 cells treated with 1 and 2 subjected to apoptosis death, as exhibited by perturbation of mitochondrial membrane potential and cytochrome c release as well as increase in ROS formation. We also found activation of caspases-3/7, -8, and -9 in compounds 1 and 2. Moreover, inhibition of NF-κB translocation in MCF-7 cells treated by compound 1 significantly exhibited the association of extrinsic apoptosis pathway. Acute toxicity results demonstrated the nontoxic nature of the compounds in mice. Our results showed significant activity towards MCF-7 cells via either intrinsic or extrinsic mitochondrial pathway and are potential candidate for further in vivo and clinical breast cancer studies.
    Matched MeSH terms: Inhibitory Concentration 50
  9. Fulltext In vivo acute toxicity evaluation and in vitro molecular mechanism study of antiproliferative activity of a novel indole Schiff base β-diiminato manganeseIII complex in hormone-dependent and triple negative breast cancer cells
    Farghadani R, Seifaddinipour M, Rajarajeswaran J, Abdulla MA, Mohd Hashim NB, Khaing SL, et al.
    PeerJ, 2019;7:e7686.
    PMID: 31608167 DOI: 10.7717/peerj.7686
    Breast cancer is the most frequently diagnosed cancer among women worldwide. Recently, increasing attention has been paid to the anticancer effects of transition metal complexes of indole Schiff bases. β-diiminato ManganeseIII complex has shown promising cell cycle arrest and apoptosis induction against MCF-7 and MDA-MB-231 breast cancer cells. In this study, time- and dose- dependent inhibitory activity were evaluated using MTT assay after 48 h and 72 h exposure time. In addition, median effect analysis was conducted according to Chou-Talalay method to investigate whether MnIII complex has synergistic effect in combination with chemotherapeutic drugs on inhibiting breast cancer cell growth. The molecular mechanisms underlying its potent antiproliferative effect was determined through bioluminescent caspase-3/7, -8 and -9 activity assays and quantitative expression analysis of cell cycle- and apoptosis-related genes. Furthermore, safety evaluation of MnIII complex was assessed through the acute oral toxicity test in in vivo model. The MTT assay results revealed that it potently reduced the viability of MCF-7 (IC50 of 0.63 ± 0.07 µg/mL for 48 h and 0.39 ± 0.08 µg/mL for 72 h) and MDA-MB-231 (1.17 ± 0.06 µg/mL for 48 h, 1.03 ± 0.15 µg/mL for 72 h) cells in dose- and time-dependent manner. Combination treatment also enhanced the cytotoxic effects of doxorubicin but not tamoxifen on inhibiting breast cancer cell growth. The involvement of intrinsic and extrinsic pathway in apoptosis induction was exhibited through the increased activity of caspase-9 and caspase-8, respectively, leading to enhanced downstream executioner caspase-3/7 activity in treated MCF-7 and MDA-MB-231 cells. In addition, gene expression analysis revealed that MnIII complex exerts its antiproliferative effect via up-and down-regulation of p21 and cyclin D1, respectively, along with increased expression of Bax/Bcl-2 ratio, TNF-α, initiator caspase-8 and -10 and effector caspase-3 in MCF-7 and MDA-MB-231 cells. However, the results did not show increased caspase-8 activity in treated MCF-7 cells. Furthermore, in vivo acute oral toxicity test revealed no signs of toxicity and mortality in treated animal models compared to the control group. Collectively, the promising inhibitory effect and molecular and mechanistic evidence of antiproliferative activity of MnIII complex and its safety characterization have demonstrated that it may have therapeutic value in breast cancer treatment worthy of further investigation and development.
    Matched MeSH terms: Inhibitory Concentration 50
  10. Fulltext Development of supercritical fluid extraction for the recovery of betacyanins from red pitaya fruit (Hylocereus polyrhizus) peel: a source of natural red pigment with potential antioxidant properties
    Fathordoobady, F., Manap, M.Y., Selamat, J., Singh, A.P.
    International Food Research Journal, 2019;26(3):1023-1034.
    MyJurnal
    In the present work, supercritical fluid extraction (SFE) with CO2 as solvent and EtOH/water (v/v) as co-solvent was optimised by applying 23 factorial experimental design for the extraction of betacyanins from red pitaya fruit (Hylocereus polyrhizus) peel. Three independent variables of pressure (20-30 MPa), temperature (40-60°C) and co-solvent concentration (10-20%) were chosen for response variables. With the 2 mL/min flow rate of CO2, the dynamic time of extraction was found to be 90 min. The linear effects of main factors and interactions were evaluated. The calculated response surface model for the pressure/temperature was found to be significant for all the dependent variables. At optimal condition of SFE, the response variables were assessed as maximum extraction yield of 4.09 ± 0.69%, total betacyanins content of 25.49 ± 1.54 mg/100 mL, redness (a*) of 58.18 ± 0.82, and IC50 (antioxidant activity) of 1.34 ± 0.12 mg/mL for the experimental peel extracts. The optimal levels of independent variables were validated for the experimental responses as predicted by the mathematical model. The reliability of this method was confirmed as there was no significant difference between experimental and predicted values. The HPLC-MS profile of betacyanins extract comprised of both acylated and non-acylated betacyanins constituents.
    Matched MeSH terms: Inhibitory Concentration 50
  11. Expression of multidrug resistance (MDR) proteins and in vitro drug resistance in acute leukemias
    Fazlina N, Maha A, Jamal R, Zarina AL, Cheong SK, Hamidah H, et al.
    Hematology, 2007 Feb;12(1):33-7.
    PMID: 17364990
    The expression of the multidrug resistance (MDR) proteins may influence the outcome of treatment in patients with acute leukemia. The aim of this study was to determine the IC50 of cytotoxic drugs (cytosine arabinoside, ara-C and daunorubicin, dnr) using the in vitro 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)2H-tetrazolium, inner salt (MTS) assay method. A total of 82 newly diagnosed acute leukemia cases (43 adult myeloid leukaemia, AML cases and 39 acute lymphoblastic leukaemia, ALL cases) and 16 relapsed cases (8 AML cases and 8 ALL cases) were studied. The MTS assay was performed using two cytotoxic drugs, dnr and ara-C. Cells were incubated with different concentrations of drugs for 4 days and the IC50 was extrapolated from the viability curve. In newly diagnosed cases, we found that childhood ALL samples showed higher IC50 values of dnr (0.040 +/- 2.320) compared to adult AML samples (0.021 +/- 0.158). In contrast, newly diagnosed adult AML samples showed higher IC50 values of ara-C (0.157 +/- 0.529) compared to childhood ALL samples (0.100 +/- 2.350). In relapsed cases, two samples of childhood ALL showed IC50 values of dnr (0.910 +/- 1.760) and ara-C (1.310 +/- 2.390), which was higher compared to childhood AML samples (0.129 +/- 0.214 and 0.210 +/- 0.003, respectively). However, there was no correlation between IC50 values of these drugs tested with clinical outcome. In conclusion, we found that MTS assay is an easy, rapid and non laborious method to study in vitro drug resistance in acute leukaemia cases.
    Matched MeSH terms: Inhibitory Concentration 50
  12. Fulltext Increased fucoxanthin in Chaetoceros calcitrans extract exacerbates apoptosis in liver cancer cells via multiple targeted cellular pathways
    Foo SC, Yusoff FM, Imam MU, Foo JB, Ismail N, Azmi NH, et al.
    Biotechnol Rep (Amst), 2019 Mar;21:e00296.
    PMID: 30581767 DOI: 10.1016/j.btre.2018.e00296
    In this study, anti-proliferative effects of C. calcitrans extract and its fucoxanthin rich fraction (FxRF) were assessed on human liver HepG2 cancer cell line. Efficacy from each extract was determined by cytotoxicity assay, morphological observation, and cell cycle analysis. Mechanisms of action observed were evaluated using multiplex gene expression analysis. Results showed that CME and FxRF induced cytotoxicity to HepG2 cells in a dose and time-dependent manner. FxRF (IC50: 18.89 μg.mL-1) was found to be significantly more potent than CME (IC50: 87.5 μg.mL-1) (p 
    Matched MeSH terms: Inhibitory Concentration 50
  13. Fulltext Involvement of salicylic acid on antioxidant and anticancer properties, anthocyanin production and chalcone synthase activity in ginger (Zingiber officinale Roscoe) varieties
    Ghasemzadeh A, Jaafar HZ, Karimi E
    Int J Mol Sci, 2012 Nov 13;13(11):14828-44.
    PMID: 23203096 DOI: 10.3390/ijms131114828
    The effect of foliar application of salicylic acid (SA) at different concentrations (10-3 M and 10-5 M) was investigated on the production of secondary metabolites (flavonoids), chalcone synthase (CHS) activity, antioxidant activity and anticancer activity (against breast cancer cell lines MCF-7 and MDA-MB-231) in two varieties of Malaysian ginger, namely Halia Bentong and Halia Bara. The results of high performance liquid chromatography (HPLC) analysis showed that application of SA induced the synthesis of anthocyanin and fisetin in both varieties. Anthocyanin and fisetin were not detected in the control plants. Accordingly, the concentrations of some flavonoids (rutin and apigenin) decreased significantly in plants treated with different concentrations of SA. The present study showed that SA enhanced the chalcone synthase (CHS) enzyme activity (involving flavonoid synthesis) and recorded the highest activity value of 5.77 nkat /mg protein in Halia Bara with the 10-5 M SA treatment. As the SA concentration was decreased from 10-3 M to 10-5 M, the free radical scavenging power (FRAP) increased about 23% in Halia Bentong and 10.6% in Halia Bara. At a concentration of 350 μg mL-1, the DPPH antioxidant activity recorded the highest value of 58.30%-72.90% with the 10-5 M SA treatment followed by the 10-3 M SA (52.14%-63.66%) treatment. The lowest value was recorded in the untreated control plants (42.5%-46.7%). These results indicate that SA can act not only as an inducer but also as an inhibitor of secondary metabolites. Meanwhile, the highest anticancer activity against MCF-7 and MDA-MB-231 cell lines was observed for H. Bara extracts treated with 10-5 M SA with values of 61.53 and 59.88%, respectively. The results suggest that the high anticancer activity in these varieties may be related to the high concentration of potent anticancer components including fisetin and anthocyanin. The results thus indicate that the synthesis of flavonoids in ginger can be increased by foliar application of SA in a controlled environment and that the anticancer activity in young ginger extracts could be improved.
    Matched MeSH terms: Inhibitory Concentration 50
  14. Fulltext Aqueous Extract of Phyllanthus niruri Leaves Displays In Vitro Antioxidant Activity and Prevents the Elevation of Oxidative Stress in the Kidney of Streptozotocin-Induced Diabetic Male Rats
    Giribabu N, Rao PV, Kumar KP, Muniandy S, Swapna Rekha S, Salleh N
    Evid Based Complement Alternat Med, 2014;2014:834815.
    PMID: 24991228 DOI: 10.1155/2014/834815
    P. niruri has been reported to possess antidiabetic and kidney protective effects. In the present study, the phytochemical constituents and in vitro antioxidant activity of P. niruri leaf aqueous extract were investigated together with its effect on oxidative stress and antioxidant enzymes levels in diabetic rat kidney. Results. Treatment of diabetic male rats with P. niruri leaf aqueous extract (200 and 400 mg/kg) for 28 consecutive days prevents the increase in the amount of lipid peroxidation (LPO) product, malondialdehyde (MDA), and the diminution of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx) activity levels in the kidney of diabetic rats. The amount of LPO showed strong negative correlation with SOD, CAT, and GPx activity levels. P. niruri leaf aqueous extract exhibits in vitro antioxidant activity with IC50 slightly lower than ascorbic acid. Phytochemical screening of plant extract indicates the presence of polyphenols. Conclusion. P. niruri leaf extract protects the kidney from oxidative stress induced by diabetes.
    Matched MeSH terms: Inhibitory Concentration 50
  15. Fulltext Determinations of secondary metabolites and its antioxidant activities of various fractions of Albizia myriophylla Bark and evaluations of anti-obesity effect of methanolic extract of Albizia myriophylla in high-fat diet mice
    Goh Yong Meng, Mahdi Ebrahimi, Nurmawati Syakroni, Mohammad Fasakh Jahroumi, Tarlan Jaafarpour, Azmah Saat
    Malaysian Journal of Medicine and Health Sciences, 2019;15(107):5-5.
    MyJurnal
    Introduction: This study examined the antioxidant activity and phenolic, flavonoid and saponin contents from mul-tiple solvent extracts of Albizia myriophylla (ABZ) bark. Antioxidant activity of the methanol extract and its derived fractions namely hexane, chloroform, ethyl acetate, butanol and a residual aqueous fraction of the bark of ABZ was assessed. Methods: All the extracts showed a significant presence of phenolic, flavonoids and saponins. In DPPH (1, 1-diphenyl-2-picrylhidrazyl) radical scavenging test, ABTS (2-2’-azinobis 3-ethyl-6-sulfonic acid) radical scavenging test and reducing activity on ferrous iron (FRAP) test, the total antioxidant capacity was found to be varied in different fractions. Results: The IC50 calculated value of the three assays showed that the methanolic extract of ABZ bark had the lowest IC50 value for each assay, compared to the other extracts signifying highest anti-oxidant activity. Methan-olic extract of ABZ was tested in high-fat diet induced mice, which showed reduce adipocyte cellularity and reduces the cholesterol, triglyceride, LDL level while increasing the HDL level. Conclusion: The antioxidant capacity with probable free radical scavenging activity of the methanolic extract of ABZ may be useful for the treatment of chronic inflammatory-related metabolic diseases such as obesity.
    Matched MeSH terms: Inhibitory Concentration 50
  16. Synthesis of Bis-indolylmethane sulfonohydrazides derivatives as potent α-Glucosidase inhibitors
    Gollapalli M, Taha M, Ullah H, Nawaz M, AlMuqarrabun LMR, Rahim F, et al.
    Bioorg Chem, 2018 10;80:112-120.
    PMID: 29894890 DOI: 10.1016/j.bioorg.2018.06.001
    In search of better α-glucosidase inhibitors, a series of bis-indolylmethane sulfonohydrazides derivatives (1-14) were synthesized and evaluated for their α-glucosidase inhibitory potential. All derivatives exhibited outstanding α-glucosidase inhibition with IC50 values ranging between 0.10 ± 0.05 to 5.1 ± 0.05 μM when compared with standard drug acarbose having IC50 value 856.28 ± 3.15 μM. Among the series, analog 7 (0.10 ± 0.05 μM) with tri-chloro substitution on phenyl ring was identified as the most potent inhibitor of α-glucosidase (∼ 8500 times). The structure activity relationship has been also established. Molecular docking studies were also performed to help understand the binding interaction of the most active analogs with receptors. From the docking studies, it was observed that all the active bis-indolylmethane sulfonohydrazides derivatives showed considerable binding interactions within the active site (acarbose inhibition site) of α-glucosidase. We also evaluated toxicity of all derivatives and found none of them are toxic.
    Matched MeSH terms: Inhibitory Concentration 50
  17. Fulltext Effects of gelam honey on oxidative stress in lung cancer cells
    Gunasekaran, G., Muhamad Fitri C.A., Chandrashegkar, S., Hajar Amalnina A.B., Raishan, S., Nurul Faiznani, Z., et al.
    Medicine & Health, 2017;12(2):202-209.
    MyJurnal
    Madu gelam telah didapati mempunyai kesan anti-oksidatif, anti-kanser dan antiinflamasi
    terhadap banyak jenis kanser. Tujuan kajian ini adalah untuk menentukan
    kesan madu gelam terhadap aras tekanan oksidatif sel kanser peparu manusia.
    IC50 madu gelam ditentukan dengan merawat sel A549 dengan dos madu yang
    berbeza (50-200 mg/ml). Sel dibahagikan kepada 4 kumpulan dan diaruh tekanan
    oksidatif dengan menggunakan hidrogen peroksida (H2
    O2
    ) mengikut kumpulan
    tertentu: kawalan, H2
    O2
    , madu gelam, H2
    O2
    + madu gelam. Selepas 24 jam
    rawatan, biopetanda tekanan oksidatif seperti malondialdehid (MDA) dan protein
    karbonil ditentukan. Aruhan tekanan oksidatif meningkatkan aras MDA (p
    Matched MeSH terms: Inhibitory Concentration 50
  18. Palm oil tocotrienols and plant flavonoids act synergistically with each other and with Tamoxifen in inhibiting proliferation and growth of estrogen receptor-negative MDA-MB-435 and -positive MCF-7 human breast cancer cells in culture
    Guthrie N, Gapor A, Chambers AF, Carroll KK
    Asia Pac J Clin Nutr, 1997 Mar;6(1):41-5.
    PMID: 24394652
    Palm oil, unlike many other dietary oils, does not increase the yield of chemically-induced mammary tumors in rats when fed at high levels in the diet. This difference appears to be due to the vitamin E fraction of palm oil, which is rich in tocotrienols, since palm oil stripped of this fraction does increase tumor yields. Experiments in our laboratory have shown that tocotrienols inhibit proliferation and growth of both MDA-MB-435 and MCF-7 cells in culture much more effectively than a-tocopherol. In addition, it was found that combinations of tocotrienols with Tamoxifen, a drug widely used for treatment of breast cancer, inhibit these cells more effectively than either tocotrienols or Tamoxifen alone. The present studies have now shown synergistic effects between tocotrienols and a number of other flavonoids from various plant sources, including citrus fruits, in the inhibition of both MDA-MB-435 and MCF-7 cells (IC50s 0.05-25 and 0.02-5 μg/mL respectively). In the MCF-7 cells, 1:1:1 combinations of tocotrienols, flavonoids and Tamoxifen were even more effective, with the best combination being d-tocotrienol, hesperetin and Tamoxifen (IC50 0.0005 μg/mL). These results suggest that diets containing palm oil may reduce the risk of breast cancer, particularly when eaten with other plant foods containing flavonoids, and may also enhance the effectiveness of Tamoxifen for treatment of breast cancer.
    Matched MeSH terms: Inhibitory Concentration 50
  19. Fulltext Synthesis and cytotoxic activity of organotin(IV) diallyldithiocarbamate compounds as anticancer agent towards colon adenocarcinoma cells (HT-29)
    Haezam FN, Awang N, Kamaludin NF, Mohamad R
    Saudi J Biol Sci, 2021 May;28(5):3160-3168.
    PMID: 34025187 DOI: 10.1016/j.sjbs.2021.02.060
    Context: Diphenyltin(IV) diallyldithiocarbamate compound (Compound 1) and triphenyltin(IV) diallyldithiocarbamate compound (Compound 2) are two newly synthesised compounds of organotin(IV) with diallyldithiocarbamate ligands.

    Objective: To assess the cytotoxic effects of two synthesised compounds against HT-29 human colon adenocarcinoma cells and human CCD-18Co normal colon cells.

    Materials and methods: Two successfully synthesised compounds were characterised using elemental (carbon, hydrogen, nitrogen, and sulphur) analysis, Fourier-Transform Infrared (FTIR), and 1H, 13C 119Sn Nucleus Magnetic Resonance (NMR) spectroscopies. The single-crystal structure of both compounds was determined by X-ray single-crystal analysis. The cytotoxicity of the compounds was assessed using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazholium bromide (MTT) assay upon 24 h of treatment. While the mode of cell death was determined based on the externalisation of phosphatidylserine using a flow cytometer.

    Results: The elemental analysis data of the two compounds showed an agreement with the suggested formula of (C6H5)2Sn[S2CN(C3H5)2]2 for Compound 1 and (C6H5)3Sn[S2CN(C3H5)2] for Compound 2. The two major peaks of infrared absorbance, i.e., ν(C = N) and ν(C = S) were detected at the range of 1475-1479 cm-1 and 972-977 cm-1, respectively. The chemical shift of carbon in NCS2 group for Compound 1 and 2 were found at 200.82 and 197.79 ppm. The crystal structure of Compound 1 showed that it is six coordinated and crystallised in monoclinic, P21/c space group. While the crystal structure of Compound 2 is five coordinated and crystallised in monoclinic, P21/c space group. The cytotoxicity (IC50) of the two compounds against HT-29 cell were 2.36 μM and 0.39 μM. Meanwhile, the percentage of cell death modes between 60% and 75% for compound 1 and compound 2 were mainly due to apoptosis, suggesting that both compounds induced growth arrest.

    Conclusion: Our study concluded that the synthesised compounds showed potent cytotoxicity towards HT-29 cell, with the triphenyltin(IV) compound showing the highest effect compared to diphenyltin(IV).

    Matched MeSH terms: Inhibitory Concentration 50
  20. Fulltext A Schiff base-derived copper (II) complex is a potent inducer of apoptosis in colon cancer cells by activating the intrinsic pathway
    Hajrezaie M, Paydar M, Moghadamtousi SZ, Hassandarvish P, Gwaram NS, Zahedifard M, et al.
    ScientificWorldJournal, 2014;2014:540463.
    PMID: 24737979 DOI: 10.1155/2014/540463
    Metal-based drugs with extensive clinical applications hold great promise for the development of cancer chemotherapeutic agents. In the last few decades, Schiff bases and their complexes have become well known for their extensive biological potential. In the present study, we examined the antiproliferative effect of a copper (II) complex on HT-29 colon cancer cells. The Cu(BrHAP)2 Schiff base compound demonstrated a potent antiproliferative effect in HT-29 cells, with an IC50 value of 2.87  μg/ml after 72 h of treatment. HT-29 cells treated with Cu (II) complexes underwent apoptosis death, as exhibited by a progressive elevation in the proportion of the G1 cell population. At a concentration of 6.25  μg/ml, the Cu(BrHAP)2 compound caused significant elevation in ROS production following perturbation of mitochondrial membrane potential and cytochrome c release, as assessed by the measurement of fluorescence intensity in stained cells. Furthermore, the activation of caspases 3/7 and 9 was part of the Cu (II) complex-induced apoptosis, which confirmed the involvement of mitochondrial-mediated apoptosis. Meanwhile, there was no significant activation of caspase-8. Taken together, these results imply that the Cu(BrHAP)2 compound is a potential candidate for further in vivo and clinical colon cancer studies to develop novel chemotherapeutic agents derived from metal-based agents.
    Matched MeSH terms: Inhibitory Concentration 50
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