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Fulltext Evaluation of Hydra HALT-1 as a toxin moiety for recombinant immunotoxin

Jiemy WF, Hiew LF, Sha HX, In LLA, Hwang JS

BMC Biotechnol, 2020 Jun 17;20(1):31.
PMID: 32552895 DOI: 10.1186/s12896-020-00628-9

BACKGROUND: Immunotoxin is a hybrid protein consisting of a toxin moiety that is linked to a targeting moiety for the purpose of specific elimination of target cells. Toxins used in traditional immunotoxins are practically difficult to be produced in large amount, have poor tissue penetration and a complex internalization process. We hypothesized that the smaller HALT-1, a cytolysin derived from Hydra magnipapillata, can be used as the toxin moiety in construction of a recombinant immunotoxin.
RESULTS: In this study, pro-inflammatory macrophage was selected as the target cell due to its major roles in numerous inflammatory and autoimmune disorders. We aimed to construct macrophage-targeted recombinant immunotoxins by combining HALT-1 with anti-CD64-scFv in two orientations, and to assess whether their cytotoxic activity and binding capability could be preserved upon molecular fusion. The recombinant immunotoxins, HALT-1-scFv and scFv-HALT-1, were successfully constructed and expressed in Escherichia coli (E. coli). Our data showed that HALT-1 still exhibited significant cytotoxicity against CD64+ and CD64- cell lines upon fusion with anti-CD64 scFv, although it had half cytotoxic activity as compared to HALT-1 alone. As positioning HALT-1 at N- or C-terminus did not affect its potency, the two constructs demonstrated comparable cytotoxic activities with IC50 lower in CD64+ cell line than in CD64- cell line. In contrast, the location of targeting moieties anti-CD64 scFv at C-terminal end was crucial in maintaining the scFv binding capability.
CONCLUSIONS: HALT-1 could be fused with anti-CD64-scFv via a fsexible polypeptide linker. Upon the successful production of this recombinant HALT-1 scFv fusion protein, HALT-1 was proven effective for killing two human cell lines. Hence, this preliminary study strongly suggested that HALT-1 holds potential as the toxin moiety in therapeutic cell targeting.

Matched MeSH terms: Inhibitory Concentration 50
Bioluminescent method for the rapid screening of toxic heayy metals in environmental samples using Photobacterium leiognathi strain AK-MIE

Kassim A, Halmi MIE, Gani SSA, Zaidan UH, Othman R, Mahmud K, et al.

Ecotoxicol Environ Saf, 2020 Jun 15;196:110527.
PMID: 32278138 DOI: 10.1016/j.ecoenv.2020.110527

Assessment of eco-toxicant using bioluminescent bacterial assay is a widely used and globally accepted method. In this work, a new luminescent bacterium was isolated from squid (Loligo duvauceli) and identified as Photobacterium leiognathi strain AK-MIE using 16S rRNA, phylogeny analysis. The predicted optimum conditions by RSM were 2.76% (w/v) NaCl, 2.28% (w/v) peptone, 0.34% (w/v) yeast extract, and pH 6.83 with 541,211.80 RLU of luminescent production whereas the predicted optimum conditions by ANN were 2.21% (w/v) NaCl, 2.27% (w/v) peptone, 0.39% (w/v) yeast extract, and pH 6.94 which produced 541,986.20 RLU. The validation analysis of both RSM and ANN show 0.60% and 0.69% deviation from the predicted results indicating that both models provided good quality predictions with ANN showing a superior data fitting capability for non-linear regression analysis. Toxicity tests show strain AK-MIE was sensitive to mercury (concentration causing 50% inhibition or IC50 of 0.00978 mgL-1), followed by cadmium (IC50 of 0.5288 mgL-1), copper IC50 of (0.8117 mgL-1), silver (IC50 of 1.109 mgL-1), and lead (IC50 of 10.71 mgL-1) which are more sensitive than previously isolated luminescent bacteria, suggesting that strain AK-MIE has the potential to be used in toxicity assessment of heavy metals in the environment. Based on the field trial results, several sediment samples from industrial areas in Bangi, Selangor managed to inhibit the bioluminescence of strain AK-MIE. Validation method carried out using ICP-MS proved the presence of several toxic heavy metal elements.

Matched MeSH terms: Inhibitory Concentration 50
Fulltext Antiproliferative and Apoptotic Effects of Cardamonin against Hepatocellular Carcinoma HepG2 Cells

Badroon NA, Abdul Majid N, Alshawsh MA

Nutrients, 2020 Jun 12;12(6).
PMID: 32545423 DOI: 10.3390/nu12061757

Liver cancer is the sixth most common cancer in terms of incidence and the fourth in terms of mortality. Hepatocellular carcinoma (HCC) represents almost 90% of primary liver cancer and has become a major health problem globally. Cardamonin (CADMN) is a natural bioactive chalcone found in several edible plants such as cardamom and Alpinia species. Previous studies have shown that CADMN possesses anticancer activities against breast, lung, prostate and colorectal cancer. In the present study, the mechanisms underlying the anti-hepatocellular carcinoma effects of CADMN were investigated against HepG2 cells. The results demonstrated that CADMN has anti-proliferative effects and apoptotic action on HepG2 cells. CADMN showed potent cytotoxicity against HepG2 cells with an IC50 of 17.1 ± 0.592 μM at 72 h. Flow cytometry analysis demonstrated that CADMN arrests HepG2 cells in G1 phase and induces a significant increase in early and late apoptosis in a time-dependent manner. The mechanism by which CADMN induces apoptotic action was via activation of both extrinsic and intrinsic pathways. Moreover, the findings of this study showed the involvement of reactive oxygen species (ROS), which inhibit the NF-κB pathway and further enhance the apoptotic process. Together, our findings further support the potential anticancer activity of CADMN as an alternative therapeutic agent against HCC.

Matched MeSH terms: Inhibitory Concentration 50
Fulltext Transcriptome Profiling of Toxoplasma gondii-Infected Human Cerebromicrovascular Endothelial Cell Response to Treatment with Monensin

Harun MSR, Taylor M, Zhu XQ, Elsheikha HM

Microorganisms, 2020 Jun 04;8(6).
PMID: 32512820 DOI: 10.3390/microorganisms8060842

Central to the progression of cerebral toxoplasmosis is the interaction of Toxoplasma gondii with the blood-brain barrier (BBB) endothelial cells. In the present work, we tested the hypothesis that inhibition of Wnt pathway signalling by the monovalent ionophore monensin reduces the growth of T. gondii infecting human brain microvascular endothelial cells (hBMECs) or microglial cells. The anti-parasitic effect of monensin (a Wnt signalling inhibitor) on the in vitro growth of T. gondii tachyzoites was investigated using two methods (Sulforhodamine B staining and microscopic parasite counting). The monensin inhibited T. gondii growth (50% inhibitory concentration [IC50] = 0.61 μM) with a selective index = 8.48 when tested against hBMECs (50% cytotoxic concentration [CC50] = 5.17 μM). However, IC50 of monensin was 4.13 μM with a SI = 13.82 when tested against microglia cells (CC50 = 57.08 μM), suggesting less sensitivity of microglia cells to monensin treatment. The effect of T. gondii on the integrity of the BBB was assessed by the transendothelial electrical resistance (TEER) assay using an in vitro human BBB model. The results showed that T. gondii infection significantly decreased hBMECs' TEER resistance, which was rescued when cells were treated with 0.1 µM monensin, probably due to the anti-parasitic activity of monensin. We also investigated the host-targeted effects of 0.1 µM monensin on global gene expression in hBMECs with or without T. gondii infection. Treatment of hBMECs with monensin did not significantly influence the expression of genes involved in the Wnt signalling pathway, suggesting that although inhibition of the Wnt signalling pathway did not play a significant role in T. gondii infection of hBMECs, monensin was still effective in limiting the growth of T. gondii. On the contrary, monensin treatment downregulated pathways related to steroids, cholesterol and protein biosynthesis and their transport between endoplasmic reticulum and Golgi apparatus, and deregulated pathways related to cell cycle and DNA synthesis and repair mechanisms. These results provide new insight into the host-modulatory effect of monensin during T. gondii infection, which merits further investigation.

Matched MeSH terms: Inhibitory Concentration 50
GC-MS metabolomics revealed protocatechuic acid as a cytotoxic and apoptosis-inducing compound from black rice brans

Yuliana ND, Tuarita MZ, Khatib A, Laila F, Sukarno S

Food Sci Biotechnol, 2020 Jun;29(6):825-835.
PMID: 32523792 DOI: 10.1007/s10068-019-00725-2

GC-MS metabolomics was used to discriminate the phytochemicals profile of Indonesian white, red, and black rice brans, and Japanese white rice brans. This technique was used for the first time to identify compounds in rice brans having cytotoxic activity against WiDr colon cancer cells. Orthogonal Projection to the Latent Structure (OPLS) analysis showed that protocatechuic acid (PA) was a discriminating factor found in black rice brans which strongly correlated with its cytotoxicity (IC50 8.53 ± 0.26 µM). Real time-PCR data demonstrated that PA cytotoxicity at different concentrations (1, 5, 10, 25 and 50 µg/mL) was mediated through different pathways. Bcl-2 expression was downregulated at all tested concentrations indicating apoptosis stimulation. At 1-10 ppm concentration, PA activated both intrinsic and extrinsic apoptosis pathways since the expression of p53, Bax, caspase-8, and caspase-9 were upregulated. At a higher dose (25 and 50 µg/mL), PA possibly involved in pyroptosis-mediated pro-inflammatory cell death by upregulating the expression of caspase-1 and caspase-7.

Matched MeSH terms: Inhibitory Concentration 50
Fulltext Isoniazid Conjugated Magnetic Nanoparticles Loaded with Amphotericin B as a Potent Antiamoebic Agent against Acanthamoeba castellanii

Iqbal K, Abdalla SAO, Anwar A, Iqbal KM, Shah MR, Anwar A, et al.

Antibiotics (Basel), 2020 May 25;9(5).
PMID: 32466210 DOI: 10.3390/antibiotics9050276

The pathogenic free-living amoeba, Acanthamoeba castellanii, is responsible for a rare but deadly central nervous system infection, granulomatous amoebic encephalitis and a blinding eye disease called Acanthamoeba keratitis. Currently, a combination of biguanides, amidine, azoles and antibiotics are used to manage these infections; however, the host cell cytotoxicity of these drugs remains a challenge. Furthermore, Acanthamoeba species are capable of transforming to the cyst form to resist chemotherapy. Herein, we have developed a nano drug delivery system based on iron oxide nanoparticles conjugated with isoniazid, which were further loaded with amphotericin B (ISO-NPs-AMP) to cause potent antiamoebic effects against Acanthamoeba castellanii. The IC50 of isoniazid conjugated with magnetic nanoparticles and loaded with amphotericin B was found to be 45 μg/mL against Acanthamoeba castellanii trophozoites and 50 μg/mL against cysts. The results obtained in this study have promising implications in drug discovery as these nanomaterials exhibited high trophicidal and cysticidal effects, as well as limited cytotoxicity against rat and human cells.

Matched MeSH terms: Inhibitory Concentration 50
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
Fulltext Establishing GPCR Targets of hMAO Active Anthraquinones from Cassia obtusifolia Linn Seeds Using In Silico and In Vitro Methods

Paudel P, Seong SH, Fauzi FM, Bender A, Jung HA, Choi JS

ACS Omega, 2020 Apr 07;5(13):7705-7715.
PMID: 32280914 DOI: 10.1021/acsomega.0c00684

The present study examines the effect of human monoamine oxidase active anthraquinones emodin, alaternin (=7-hydroxyemodin), aloe-emodin, and questin from Cassia obtusifolia Linn seeds in modulating human dopamine (hD1R, hD3R, and hD4R), serotonin (h5-HT1AR), and vasopressin (hV1AR) receptors that were predicted as prime targets from proteocheminformatics modeling via in vitro cell-based functional assays, and explores the possible mechanisms of action via in silico modeling. Emodin and alaternin showed a concentration-dependent agonist effect on hD3R with EC50 values of 21.85 ± 2.66 and 56.85 ± 4.59 μM, respectively. On hV1AR, emodin and alaternin showed an antagonist effect with IC50 values of 10.25 ± 1.97 and 11.51 ± 1.08 μM, respectively. Interestingly, questin and aloe-emodin did not have any observable effect on hV1AR. Only alaternin was effective in antagonizing h5-HT1AR (IC50: 84.23 ± 4.12 μM). In silico studies revealed that a hydroxyl group at C1, C3, and C8 and a methyl group at C6 of anthraquinone structure are essential for hD3R agonist and hV1AR antagonist effects, as well as for the H-bond interaction of 1-OH group with Ser192 at a proximity of 2.0 Å. Thus, based on in silico and in vitro results, hV1AR, hD3R, and h5-HT1AR appear to be prime targets of the tested anthraquinones.

Matched MeSH terms: Inhibitory Concentration 50
Cytotoxicity Analysis of Morphologically Different Sol-Gel-Synthesized MgO Nanoparticles and Their In Vitro Insulin Resistance Reversal Ability in Adipose cells

Jeevanandam J, Chan YS, Danquah MK, Law MC

Appl Biochem Biotechnol, 2020 Apr;190(4):1385-1410.
PMID: 31776944 DOI: 10.1007/s12010-019-03166-z

Insulin resistance is one of the major factors that leads to type 2 diabetes. Although insulin therapies have been shown to overcome insulin resistance, overweight and hypoglycemia are still observed in most cases. The disadvantages of insulin therapies have driven the interest in developing novel curative agents with enhanced insulin resistance reversibility. Magnesium deficiency has also been recognized as a common problem which leads to insulin resistance in both type 1 and 2 diabetes. Oxide nanoparticles demonstrate highly tunable physicochemical properties that can be exploited by engineers to develop unique oxide nanoparticles for tailored applications. Magnesium supplements for diabetic cells have been reported to increase the insulin resistance reversibility. Hence, it is hypothesized that magnesium oxide (MgO) nanoparticles could be molecularly engineered to offer enhanced therapeutic efficacy in reversing insulin resistance. In the present work, morphologically different MgO nanoparticles were synthesized and evaluated for biophysical characteristics, biocompatibility, cytotoxicity, and insulin resistance reversibility. MTT assay revealed that hexagonally shaped MgO nanoparticles are less toxic to 3T3-L1 adipose cells (diabetic) compared with spherically and rod-shaped MgO nanoparticles. MTT assays using VERO cells (normal, non-diabetic) showed that 400 μg/ml of hexagonal MgO nanoparticles were less toxic to both diabetic and non-diabetic cells. DNS glucose assay and western blot showed that hexagonally shaped MgO nanoparticles had reversed 29.5% of insulin resistance whilst fluorescence microscopy studies indicated that the insulin resistance reversal is due to the activation of intracellular enzymes. The probable mechanism for MgO nanoparticles to induce cytotoxic effect and insulin resistance reversal is discussed.

Matched MeSH terms: Inhibitory Concentration 50
Fulltext Phytochemicals and Cytotoxicity of Quercus infectoria Ethyl Acetate Extracts on Human Cancer Cells

Yusof WNSW, Abdullah H

Trop Life Sci Res, 2020 Apr;31(1):69-84.
PMID: 32963712 DOI: 10.21315/tlsr2020.31.1.5

Conventional and modern cancer treatment were reported to manifest adverse effects to the patients. More researches were conducted to search for selective cytotoxic agent of plant natural product on cancer cells. The presences of wide range phytochemicals in Quercus infectoria (QI) extract have been implicated with the cytotoxic effect against various types of cancer cell which remain undiscovered. This present study aimed to evaluate cytotoxic effect of QI extracts on selected human cancer cells and then, the most potent extract was further analysed for general phytochemical constituents. QI galls were extracted successively with n-hexane, ethyl acetate and methanol yielded three main extracts; n-hexane (QIH), ethyl acetate (QIEA) and methanol (QIM), respectively. The most potent extract was qualitatively analysed for the present of tannin, alkaloids, glycosides, saponins, terpenoids, flavonoids and phenolic compounds. Next, the extracts were tested to determine the cytotoxic activity against cervical cancer cells (HeLa), breast cancer cells (MDA-MB-231) and liver cancer cells (Hep G2) using MTT assay. Cytotoxic activity of QI extracts against normal fibroblast (L929) cell line was also evaluated to determine the cytoselective property. Meanwhile, DMSO-treated cells served as negative control while cisplatin-treated cells served as positive control. The most potent extract then chosen to be further investigated for DNA fragmentation as hallmark of apoptosis using Hoechst staining. Qualitative phytochemical analysis revealed the presence of tannin, alkaloids, glycosides, saponins, terpenoids, flavonoids and phenolic compounds. QIEA extract exhibited the most potent cytotoxic activity against HeLa cells with (IC50 value = 6.33 ± 0.33 μg/mL) and showed cytoselective property against L929 cells. DNA fragmentation revealed QIEA induced apoptosis in the treated cells. The richness of phytochemical constituents in QIEA extract might contribute to the potency of cytotoxic activity towards HeLa cells.

Matched MeSH terms: Inhibitory Concentration 50
Fulltext Investigation of α-Glucosidase Inhibitory Metabolites from Tetracera scandens Leaves by GC-MS Metabolite Profiling and Docking Studies

Nokhala A, Siddiqui MJ, Ahmed QU, Ahamad Bustamam MS, Zakaria AZA

Biomolecules, 2020 02 12;10(2).
PMID: 32059529 DOI: 10.3390/biom10020287

Stone leaf (Tetracera scandens) is a Southeast Asian medicinal plant that has been traditionally used for the management of diabetes mellitus. The underlying mechanisms of the antidiabetic activity have not been fully explored yet. Hence, this study aimed to evaluate the α-glucosidase inhibitory potential of the hydromethanolic extracts of T. scandens leaves and to characterize the metabolites responsible for such activity through gas chromatography-mass spectrometry (GC-MS) metabolomics. Crude hydromethanolic extracts of different strengths were prepared and in vitro assayed for α-glucosidase inhibition. GC-MS analysis was further carried out and the mass spectral data were correlated to the corresponding α-glucosidase inhibitory IC50 values via an orthogonal partial least squares (OPLS) model. The 100%, 80%, 60% and 40% methanol extracts displayed potent α-glucosidase inhibitory potentials. Moreover, the established model identified 16 metabolites to be responsible for the α-glucosidase inhibitory activity of T. scandens. The putative α-glucosidase inhibitory metabolites showed moderate to high affinities (binding energies of -5.9 to -9.8 kcal/mol) upon docking into the active site of Saccharomyces cerevisiae isomaltase. To sum up, an OPLS model was developed as a rapid method to characterize the α-glucosidase inhibitory metabolites existing in the hydromethanolic extracts of T. scandens leaves based on GC-MS metabolite profiling.

Matched MeSH terms: Inhibitory Concentration 50
Synthesis of new indazole based dual inhibitors of α-glucosidase and α-amylase enzymes, their in vitro, in silico and kinetics studies

Rafique R, Khan KM, Arshia, Kanwal, Chigurupati S, Wadood A, et al.

Bioorg Chem, 2020 01;94:103195.
PMID: 31451297 DOI: 10.1016/j.bioorg.2019.103195

The current study describes the discovery of novel inhibitors of α-glucosidase and α-amylase enzymes. For that purpose, new hybrid analogs of N-hydrazinecarbothioamide substituted indazoles 4-18 were synthesized and fully characterized by EI-MS, FAB-MS, HRFAB-MS, 1H-, and 13C NMR spectroscopic techniques. Stereochemistry of the imine double bond was established by NOESY measurements. All derivatives 4-18 with their intermediates 1-3, were evaluated for in vitro α-glucosidase and α-amylase enzyme inhibition. It is worth mentioning that all synthetic compounds showed good inhibition potential in the range of 1.54 ± 0.02-4.89 ± 0.02 µM for α-glucosidase and for α-amylase 1.42 ± 0.04-4.5 ± 0.18 µM in comparison with the standard acarbose (IC50 value of 1.36 ± 0.01 µM). In silico studies were carried out to rationalize the mode of binding interaction of ligands with the active site of enzymes. Moreover, enzyme inhibitory kinetic characterization was also performed to understand the mechanism of enzyme inhibition.

Matched MeSH terms: Inhibitory Concentration 50
Synthesis, molecular docking, dynamic simulations, kinetic mechanism, cytotoxicity evaluation of N-(substituted-phenyl)-4-{(4-[(E)-3-phenyl-2-propenyl]-1-piperazinyl} butanamides as tyrosinase and melanin inhibitors: In vitro, in vivo and in silico approaches

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
Synthesis, in vitro alpha-glucosidase inhibitory potential of benzimidazole bearing bis-Schiff bases and their molecular docking study

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
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
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
Fulltext Medicinal properties screening of Mallotus paniculatus extract

NA Bahaman, Raha Ahmad Raus, Yusilawati Ahmad Nor, Al Mamun, Abdullah, Noor Suhana Adzahar, Dayang Fredalina Basri

IIUM Medical Journal Malaysia, 2020;19(1):5-12.
MyJurnal

Introduction: Traditionally, Mallotus paniculatus (Balik Angin) plant is used in the treatment of various
diseases in rural areas such as remedy after childbirth, wound healing and fever. In this present study, four
medicinal properties of the plant were investigated which included antibacterial, antifungal, anticancer and
antioxidant activities. Materials and Methods: Potential medicinal compounds were extracted from the plant
leaves by sonication with 3 different solvents namely ethanol, ethyl acetate and hexane respectively. The
antibacterial and antifungal properties were determined using disc diffusion agar and broth dilution assay,
the antioxidant activity by DPPH scavenging assay and the anticancer effect by MTT assay. Results: From the
screening of the medicinal properties, M. paniculatus leave extracts were shown to possess antibacterial,
antioxidant and anticancer properties but not antifungal properties. Ethanolic and ethyl acetate extracts of
the leave were active against gram positive bacteria (Staphylococcus aureus and Bacillus subtilis) but not
gram negative bacteria (Pseudomonas aeruginosa and Escherichia coli). The antioxidant activity of the
ethanolic crude extract was high; with IC50 of 30 μg/ml comparable with the positive controls; ascorbic acid
and butylated hydroxytoluene (BHT). Both ethanolic and ethyl acetate extracts were cytotoxic against breast
cancer (MCF7), colon cancer (HT-29), cervix cancer (Hela) cell lines. Conclusion: M. paniculatus leave
extract has many potential medicinal values for further studies.

Matched MeSH terms: Inhibitory Concentration 50
Fulltext Synthesis, characterization, quantum chemical calculations and anticancer activity of a Schiff base NNOO chelate ligand and Pd(II) complex

Ahmad N, Anouar EH, Tajuddin AM, Ramasamy K, Yamin BM, Bahron H

PLoS One, 2020;15(4):e0231147.
PMID: 32287324 DOI: 10.1371/journal.pone.0231147

This paper reports the synthesis, characterization, anticancer screening and quantum chemical calculation of a tetradentate Schiff base 2,2'-((1E,1'E)-((2,2-dimethylpropane-1,3-diyl)bis- (azanylylidene))bis(methanylylidene))bis(4-fluorophenol) (L2F) and its Pd (II) complex (PdL2F). The compounds were characterized via UV-Visible, NMR, IR spectroscopy and single crystal x-ray diffraction. Density Functional Theory (DFT) and time-dependent DFT calculations in gas and solvent phases were carried out using B3LYP, B3P86, CAM-B3LYP and PBE0 hybrid functionals combined with LanL2DZ basis set. Complexation of L2F to form PdL2F was observed to cause a bathochromic shift of the maximum absorption bands of n-π* from 327 to 410 nm; an upfield shift for δ (HC = N) from 8.30 to 7.96 ppm and a decreased wavenumber for ν(C = N) from 1637 to 1616 cm-1. Overall, the UV-Vis, NMR and IR spectral data are relatively well reproduced through DFT and TD-DFT methods. L2F and PdL2F showed IC50 of 90.00 and 4.10 μg/mL, respectively, against human colorectal carcinoma (HCT116) cell lines, signifying increased anticancer activity upon complexation with Pd (II).

Matched MeSH terms: Inhibitory Concentration 50
Fulltext Pellet diameter of Ganoderma lucidum in a repeated-batch fermentation for the trio total production of biomass-exopolysaccharide-endopolysaccharide and its anti-oral cancer beta-glucan response

Abdullah NR, Sharif F, Azizan NH, Hafidz IFM, Supramani S, Usuldin SRA, et al.

AIMS Microbiol, 2020;6(4):379-400.
PMID: 33364534 DOI: 10.3934/microbiol.2020023

The pellet morphology and diameter range (DR) of Ganoderma lucidum were observed in a repeated-batch fermentation (RBF) for the trio total production of biomass, exopolysaccharide (EPS) and endopolysaccharide (ENS). Two factors were involved in RBF; broth replacement ratio (BRR: 60%, 75% and 90%) and broth replacement time point (BRTP: log, transition and stationary phase) in days. In RBF, 34.31 g/L of biomass favoured small-compact pellets with DR of 20.67 µm< d < 24.00 µm (75% BRR, day 11 of BRTP). EPS production of 4.34 g/L was prone to ovoid-starburst pellets with DR of 34.33 µm< d <35.67 µm (75% BRR, day 13 of BRTP). Meanwhile, the highest 2.43 g/L of ENS production favoured large-hollow pellets with DR of 34.00 µm< d < 38.67 µm (90% BRR, day 13 of BRTP). In addition, RBF successfully shortened the biomass-EPS-ENS fermentation period (31, 33 and 35 days) from batch to 5 days, in seven consecutive cycles of RBF. In a FTIR detection, β-glucan (BG) from EPS and ENS extracts were associated with β-glycosidic linkages (2925 cm-1, 1635 cm-1, 1077 cm-1, 920 cm-1 and 800 cm-1 wavelengths) with similar 1H NMR spectral behaviour (4.58, 3.87 and 3.81 ppm). Meanwhile, 4 mg/L of BG gave negative cytotoxic effects on normal gingival cell line (hGF) but induced antiproliferation (IC50 = 0.23 mg/mL) against cancerous oral Asian cellosaurus cell line (ORL-48). Together, this study proved that G. lucidum mycelial pellets could withstand seven cycles of long fermentation condition and possessed anti-oral cancer beta-glucan, which suits large-scale natural drug fermentation.

Matched MeSH terms: Inhibitory Concentration 50
Fulltext Cytotoxic and anticancer properties of the Malaysian mangrove pit viper (Trimeresurus purpureomaculatus) venom and its disintegrin (purpureomaculin)

Tan CH, Liew JL, Navanesan S, Sim KS, Tan NH, Tan KY

J Venom Anim Toxins Incl Trop Dis, 2020;26:e20200013.
PMID: 32742279 DOI: 10.1590/1678-9199-JVATITD-2020-0013

Background: The Asiatic pit vipers from the Trimeresurus complex are medically important venomous snakes. These pit vipers are often associated with snakebite that leads to fatal coagulopathy and tissue necrosis. The cytotoxic venoms of Trimeresurus spp.; however, hold great potential for the development of peptide-based anticancer drugs.
Methods: This study investigated the cytotoxic effect of the venom from Trimeresurus purpureomaculatus, the mangrove pit viper (also known as shore pit viper) which is native in Malaysia, across a panel of human cancer cell lines from breast, lung, colon and prostate as well as the corresponding normal cell lines of each tissue.
Results: The venom exhibited dose-dependent cytotoxic activities on all cell lines tested, with median inhibition concentrations (IC50) ranging from 0.42 to 6.98 µg/mL. The venom has a high selectivity index (SI = 14.54) on breast cancer cell line (MCF7), indicating that it is significantly more cytotoxic toward the cancer than to normal cell lines. Furthermore, the venom was fractionated using C18 reversed-phase high-performance liquid chromatography and the anticancer effect of each protein fraction was examined. Fraction 1 that contains a hydrophilic low molecular weight (approximately 7.5 kDa) protein was found to be the most cytotoxic and selective toward the breast cancer cell line (MCF7). The protein was identified using liquid chromatography-tandem mass spectrometry as a venom disintegrin, termed purpureomaculin in this study.
Conclusion: Taken together, the findings revealed the potent and selective cytotoxicity of a disintegrin protein isolated from the Malaysian T. purpureomaculatus venom and suggested its anticancer potential in drug discovery.

Matched MeSH terms: Inhibitory Concentration 50

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