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Fulltext Cobalt nanoparticles as novel nanotherapeutics against Acanthamoeba castellanii

Anwar A, Numan A, Siddiqui R, Khalid M, Khan NA

Parasit Vectors, 2019 Jun 03;12(1):280.
PMID: 31159839 DOI: 10.1186/s13071-019-3528-2

BACKGROUND: Species of Acanthamoeba are facultative pathogens which can cause sight threatening Acanthamoeba keratitis and a rare but deadly brain infection, granulomatous amoebic encephalitis. Due to conversion of Acanthamoeba trophozoites to resistant cyst stage, most drugs are found to be ineffective at preventing recurrence of infection. This study was designed to test the antiacanthamoebic effects of different cobalt nanoparticles (CoNPs) against trophozoites and cysts, as well as parasite-mediated host cell cytotoxicity.
METHODS: Three different varieties of CoNPs were synthesized by utilizing hydrothermal and ultrasonication methods and were thoroughly characterized by X-ray diffraction and field emission scanning electron microscopy. Amoebicidal, encystation, excystation, and host cell cytopathogenicity assays were conducted to study the antiacanthamoebic effects of CoNPs.
RESULTS: The results of the antimicrobial evaluation revealed that cobalt phosphate Co3(PO4)2 hexagonal microflakes, and 100 nm large cobalt hydroxide (Co(OH)2) nanoflakes showed potent amoebicidal activity at 100 and 10 µg/ml against Acanthamoeba castellanii as compared to granular cobalt oxide (Co3O4) of size 35-40 nm. Furthermore, encystation and excystation assays also showed consistent inhibition at 100 µg/ml. CoNPs also inhibited amoebae-mediated host cell cytotoxicity as determined by lactate dehydrogenase release without causing significant damage to human cells when treated alone.
CONCLUSIONS: To our knowledge, these findings determined, for the first time, the effects of composition, size and morphology of CoNPs against A. castellanii. Co3(PO4)2 hexagonal microflakes showed the most promising antiamoebic effects as compared to Co(OH)2 nanoflakes and granular Co3O4. The results reported in the present study hold potential for the development of antiamoebic nanomedicine.
Fulltext A review on Malaysia's solar energy pathway towards carbon-neutral Malaysia beyond Covid'19 pandemic

Vaka M, Walvekar R, Rasheed AK, Khalid M

J Clean Prod, 2020 Nov 10;273:122834.
PMID: 32834565 DOI: 10.1016/j.jclepro.2020.122834

COVID'19 pandemic has devastated several industries and solar energy is no exception. In its economic relief package, Malaysia has announced approximately US$ 2.9 billion in expenditure for the installation of new grids, LED street lights and rooftop solar panels. The Government will also open the tender for a 1400 MW solar power project in the year 2020, which is expected to generate 5 billion ringgit (US$1.1 billion) in investments. As these measures are intended to sustain the existing growth of solar energy potential in the country, it is vital to assess its status quo. Hence, this paper aims to review the current status of renewable energy in Malaysia as well as the initiatives taken before the pandemic to promote solar photovoltaic (PV) technology to meet the energy demands through the low-carbon pathway.
Fulltext Preparation and Characterization of Eco-Friendly Spent Coffee/ENR50 Biocomposite in Comparison to Carbon Black

Raju G, Khalid M, Shaban MM, Azahari B

Polymers (Basel), 2021 Aug 20;13(16).
PMID: 34451334 DOI: 10.3390/polym13162796

This study investigates the impact of spent coffee biochar (Biochar) compared to carbon black (CB) as a partial replacement for carbon black in epoxidized natural rubber (ENR). Particle size and elemental analysis were used to characterize the biochar and CB. Cure characteristics, tensile, thermal, and morphological properties on the effect of biochar and CB as filler were studied. It was found that incorporating 10 phr of spent coffee biochar could improve the composites' tensile properties and thermal performance compared to carbon black. However, the addition of biochar significantly affects the maximum torque compared to CB and delays the vulcanization time. SEM study shows that biochar has a strong effect on the morphology of composite films. The FTIR graph reveals no substantial difference between compounds with biochar and CB. According to the thermal calorimetric study, the thermal stability of ENR-Biochar is higher than that of ENR-CB. Additionally, these findings suggest that the utilization of spent coffee as a sustainable biochar could be further explored, but little has been done in epoxidized natural rubber (ENR).
Parametric optimization of polycaprolactone synthesis catalysed by Candida antarctica lipase B using response surface methodology

Pakalapati H, Arumugasamy SK, Jewaratnam J, Wong YJ, Khalid M

Biopolymers, 2018 Dec;109(12):e23240.
PMID: 30489632 DOI: 10.1002/bip.23240

A statistical approach with D-optimal design was used to optimize the process parameters for polycaprolactone (PCL) synthesis. The variables selected were temperature (50°C-110°C), time (1-7 h), mixing speed (50-500 rpm) and monomer/solvent ratio (1:1-1:6). Molecular weight was chosen as response and was determined using matrix-assisted laser desorption/ionization time of flight (MALDI TOF). Using the D-optimal method in design of experiments, the interactions between parameters and responses were analysed and validated. The results show a good agreement with a minimum error between the actual and predicted values.
Fulltext A synergistic effect on enriching the Mg-Al-Zn alloy-based hybrid composite properties

Anbuchezhiyan G, Mubarak NM, Karri RR, Khalid M

Sci Rep, 2022 Nov 21;12(1):20053.
PMID: 36414776 DOI: 10.1038/s41598-022-24427-8

Mg-Al-Zn alloys are widely preferred in many applications by considering their excellent properties of high stiffness-to-weight ratio, lightweight, high strength-to-weight ratio, low density, castability, high-temperature mechanical properties, machinability, high corrosion resistance, and great damping. Improving the properties of such alloys is challenging due to their hexagonal crystal structure and other alloying limitations. This study aims to synthesize Mg-Al-Zn alloy by incorporating the alloying elements 8.3 wt% Al, 0.35 wt% Zn on pure magnesium (Control specimen). Then synthesize Mg-Al-Zn/BN/B4C hybrid composite by reinforcing B4C at three weight proportions (3 wt%, 6 wt%, 9 wt%) along with constant solid lubricant BN (3 wt%) through a stir casting process. The hybrid composite samples were characterized and compared with the performances of the control specimen. The results reveal that 9 wt% B4C reinforced samples outperformed through recording the improvement of tensile strength by 28.94%, compressive strength by 37.89%, yield strength by 74.63%, and hardness by 14.91% than the control specimen. Apart from this, it has reduced the corrosion area (37.81%) and noticed negligible changes in density (increased by 0.03%) and porosity (decreased by 0.01%) than the control specimen. The samples were characterized using SEM, XRD, and EDAX apparatus.
Prospects of titanium carbide-based MXene in heavy metal ion and radionuclide adsorption for wastewater remediation: A review

Sheth Y, Dharaskar S, Chaudhary V, Khalid M, Walvekar R

Chemosphere, 2022 Jan 07;293:133563.
PMID: 35007610 DOI: 10.1016/j.chemosphere.2022.133563

Contamination of water sources with various organic and inorganic non-biodegradable pollutants is becoming a growing concern due to industrialization, urbanization, and the inefficiency of traditional wastewater treatment processes. Transition Metal Carbides/Nitrides (MXenes) are emerging as advanced nanomaterials of choice for treating contaminated water owing to their excellent conductivity, mechanical flexibility, high specific surface area, scalable production, rich surface functionalities, and layered morphology. MXenes have demonstrated enhanced ability to adsorb various organic and inorganic contaminants depending upon their surface terminal groups (-OH, -F, and -O) and interlayer spacing. Titanium carbide (Ti3C2Tx) is most researched to date due to its ease of processing and stability. Ti3C2Tx has shown excellent performance in absorbing heavy metal ions and radioactive heavy metals. This review summarizes state-of-the-art Ti3C2Tx synthesis, including selective etching techniques, optimization of the desired adsorption features (controlling surface functional groups, intercalation, sonication, and functionalization), and regeneration and adsorption mechanism to remove contaminants. Furthermore, the review also compares the adsorption performance of Ti3C2Tx with other commercial adsorbents (including chitosan, cellulose, biomass, and zeolites). Ti3C2Tx has been found to have an adsorption efficiency of more than 90% in most studies due to its layered structure, which makes the functional groups easily accessible, unique and novel compared to other conventional nanomaterials and adsorbents. The challenges, potential solutions, and prospects associated with the commercial development of Ti3C2Tx as adsorbents are also discussed. The review establishes a framework for future wastewater treatment research using MXenes to address the global problem of water scarcity.
E-beam sterilizable thermoplastics elastomers for healthcare devices: Mechanical, morphology, and in vivo studies

Balaji AB, Ratnam CT, Khalid M, Walvekar R

J Biomater Appl, 2018 03;32(8):1049-1062.
PMID: 29298552 DOI: 10.1177/0885328217750476

The effect of electron beam radiation on ethylene-propylene diene terpolymer/polypropylene blends is studied as an attempt to develop radiation sterilizable polypropylene/ethylene-propylene diene terpolymer blends suitable for medical devices. The polypropylene/ethylene-propylene diene terpolymer blends with mixing ratios of 80/20, 50/50, 20/80 were prepared in an internal mixer at 165°C and a rotor speed of 50 rpm/min followed by compression molding. The blends and the individual components were radiated using 3.0 MeV electron beam accelerator at doses ranging from 0 to 100 kGy in air and room temperature. All the samples were tested for tensile strength, elongation at break, hardness, impact strength, and morphological properties. After exposing to 25 and 100 kGy radiation doses, 50% PP blend was selected for in vivo studies. Results revealed that radiation-induced crosslinking is dominating in EPDM dominant blends, while radiation-induced degradation is prevailing in PP dominant blends. The 20% PP blend was found to be most compatible for 20-60 kGy radiation sterilization. The retention in impact strength with enhanced tensile strength of 20% PP blend at 20-60 kGy believed to be associated with increased compatibility between PP and EPDM along with the radiation-induced crosslinking. The scanning electron micrographs of the fracture surfaces of the PP/EPDM blends showed evidences consistent with the above contentation. The in vivo studies provide an instinct that the radiated blends are safe to be used for healthcare devices.
Fulltext Synthesis of magnetic nanocarbon using palm oil as the green precursor via microwave-assisted arc for wastewater treatment

Zakaria NZJ, Rozali S, Mubarak NM, Khalid M

Sci Rep, 2022 Nov 04;12(1):18698.
PMID: 36333525 DOI: 10.1038/s41598-022-21982-y

The presence of metal with microwave irradiation has always invited controversial arguments as the metal will catch on fire easily. But interestingly, researchers found that arc discharge phenomena provide a promising way for molecule cracking to synthesize nanomaterials. This study developed a single-step yet affordable synthesis approach that combines microwave heating and arcing in transforming crude palm oil into magnetic nanocarbon (MNC), which can be considered a new alternative for the palm oil sectors. It involves synthesizing the medium at a partial inert condition with constant coiled stainless steel metal wire (dielectric media) and ferrocene (catalyst). This approach successfully demonstrates heating at a temperature ranging from 190.9 to 472.0 °C with different synthesis times (10-20 min). The produced MNC shows formations of spheres with average sizes of 20.38-31.04 nm, mesoporous structure (SBET: 14.83-151.95 m2/g), and high content of fixed carbon (52.79-71.24wt%), and the ratio of the D and G bands (ID/IG) is 0.98-0.99. The formation of new peaks in the FTIR spectra (522.29-588.48 cm-1) supports the appearance of the FeO compounds from the ferrocene. The magnetometer shows high magnetization saturation (22.32-26.84 emu/g) in ferromagnetic materials. The application of the MNC in wastewater treatment has been demonstrated by evaluating their adsorbent capability with Methylene Blue (MB) adsorption test at a different concentrations varying between 5 and 20 ppm. The MNC produced at synthesis time (20 min) shows the highest adsorption efficiency (10.36 mg/g) compared to others, with 87.79% removal of MB dye. As a result, the value for Langmuir is not promising compared to Freundlich, with R2 being around 0.80, 0.98, and 0.99 for MNC synthesized at 10 min (MNC10), 15 min (MNC15), and 20 min (MNC20), respectively. Hence, the adsorption system is in a heterogeneous condition. The microwave-assisted arcing thereby presents a promising approach to transforming CPO into MNC that could remove the hazardous dye.
Triphenyl methyl phosphonium tosylate as an efficient phase transfer catalyst for ultrasound-assisted oxidative desulfurization of liquid fuel

Desai K, Dharaskar S, Khalid M, Gupta TCSM

Environ Sci Pollut Res Int, 2021 Jun;28(21):26747-26761.
PMID: 33491146 DOI: 10.1007/s11356-021-12391-1

The novel phosphonium-based ionic liquid (IL), triphenyl methyl phosphonium tosylate ([TPMP][Tos]), has been synthesized and applied as a phase transfer catalyst (PTC) in the ultrasound-assisted oxidative desulfurization (UAODS). Oxidation of model fuel (MF) containing dibenzothiophene (DBT) was carried out using an equimolar mixture of H2O2-CH3COOH as an oxidant at 40-70 °C in the presence of IL. The sulfur compound is converted into polar sulfone, and the maximum desulfurization efficiency was examined. The effect of process parameters such as reaction temperature, reaction time, molar ratio of oxidant to sulfur (n(O/S)), and the mass ratio of ionic liquid to model fuel (m(IL/MF)) was studied, and the conditions for maximizing the DBT conversion rate were found. Maximum conversion (> 99%) was obtained at a temperature of 70 °C with m(IL/MF) of 0.8. The oxidation reactivity of various sulfur compounds was studied at different time intervals. To verify the effect of ionic liquid and ultrasound irradiation, extractive desulfurization (EDS), oxidative desulfurization (ODS), and UAODS in the presence of IL were carried out. The experimental results show that the UAODS process gives the highest desulfurization efficiency. A kinetic study was performed to estimate the rate constant and the order of oxidation reaction.
Fulltext Enhanced tribological properties of diesel-based engine oil through synergistic MoS2-graphene nanohybrid additive

Nagarajan T, Sridewi N, Wong WP, Walvekar R, Khalid M

Sci Rep, 2023 Oct 13;13(1):17424.
PMID: 37833323 DOI: 10.1038/s41598-023-43260-1

This research explores the potential of microwave-synthesized MoS2-graphene nanohybrid as additives to enhance the tribological properties of diesel-based engine oil. The synthesis method offers significant advantages, reducing both synthesis time and energy consumption by 90-98% compared to conventional approaches. The synthesized nanohybrids are characterized through FESEM, EDX, XRD, and Raman spectroscopy to understand their morphology and functional group interactions. These nanohybrids are incorporated into 20W40 engine oil following synthesis, and a comprehensive assessment of their properties is conducted. This evaluation covers critical parameters like viscosity index, stability, volatility, as well as tribological properties, oxidation resistance, and thermal conductivity of the oil-nanohybrid system. Results demonstrate that adding just 0.05 wt% of MoS2-graphene nanohybrid leads to a remarkable 58.82% reduction in friction coefficient and a significant 36.26% decrease in the average wear scar diameter. Additionally, oxidation resistance improves by 19.21%, while thermal conductivity increases notably by 19.83% (at 100 °C). The study demonstrates the synergistic effects of these nanohybrids in reducing friction and wear, enhancing oxidation resistance, and improving thermal conductivity. In conclusion, this research highlights the potential of microwave-synthesized MoS2-graphene nanohybrid as promising tribological additives for diesel engine oils. Their successful integration could significantly enhance the performance and durability of critical mechanical components in diesel engines, representing a significant advancement in lubrication technology.
Fulltext Distant entanglement via photon hopping in a coupled cavity magnomechanical system

Sohail A, Peng JX, Hidki A, Khalid M, Singh SK

Sci Rep, 2023 Dec 09;13(1):21840.
PMID: 38071389 DOI: 10.1038/s41598-023-48825-8

We theoretically propose a scheme to generate distant bipartite entanglement between various subsystems in coupled magnomechanical systems where both the microwave cavities are coupled through single photon hopping coupling strength Γ. Each cavity contains a magnon mode and phonon mode and this gives six excitation modes in our model Hamiltonian which are cavity-1 photons, cavity-2 photons, magnon and phonon in cavity-1, and magnon and phonon in cavity-2. We found that significant bipartite entanglement exists between indirectly coupled subsystems in coupled microwave cavities for an appropriate set of parameters regime. Moreover, we also obtain suitable cavity and magnon detuning parameters for a significant distant bipartite entanglement in different bipartitions. In addition, it can be seen that a single photon hopping parameter significantly affects both the degree as well as the transfer of quantum entanglement between various bipartitions. Hence, our present study related to coupled microwave cavity magnomechanical configuration will open new perspectives in coherent control of various quantum correlations including quantum state transfer among macroscopic quantum systems.
Impact of UV radiation on Mxene-mediated tubulin dissociation and mitochondrial apoptosis in breast cancer cells

Tan EW, Simon SE, Numan A, Khalid M, Tan KO

Colloids Surf B Biointerfaces, 2024 Mar;235:113793.
PMID: 38364521 DOI: 10.1016/j.colsurfb.2024.113793

Breast cancer is a global health concern that requires personalized therapies to prevent relapses, as conventional treatments may develop resistance over time. Photothermal therapy using spectral radiation or intense light emission is a broad-spectrum treatment that induces hyperthermia-mediated cancer cell death. MXene, a two-dimensional material, has been reported to have potential biological applications in photothermal therapy for cancer treatment. In this study, we investigated the apoptotic activity of MXene and UV-irradiated MXene in MCF-7 breast cancer cells by treating them with varying concentrations of MXene. The cytotoxicity of MXene and UV was evaluated by analyzing cellular morphology, nuclei condensation, caspase activation, and apoptotic cell death. We also assessed the effect of the combined treatment on the expression and cellular distribution of Tubulin, a key component of microtubules required for cell division. At low concentrations of MXene (up to 100 µg/ml), the level of cytotoxicity in MCF-7 cells was low. However, the combined treatment of MXene and UV resulted in a synergistic increase in cytotoxicity, causing rounded cellular morphology, condensed nuclei, caspase activation, and apoptotic cell death. Furthermore, the treatment reduced Tubulin protein expression and cellular distribution, indicating a potent inducer of cell death with potential application for cancer treatment. The study demonstrates that the combined treatment of MXene and UVB irradiation is a promising strategy for inducing apoptotic cell death in breast cancer cells, suggesting its potential as a therapeutic intervention for breast cancer.
Kenaf-based activated carbon: A sustainable solution for high-performance aqueous symmetric supercapacitors

Subramaniam T, Ansari MNM, Krishnan SG, Khalid M

Chemosphere, 2024 Apr;354:141593.
PMID: 38460854 DOI: 10.1016/j.chemosphere.2024.141593

This study presents an innovative method for synthesizing activated carbon with an exceptionally high surface area (3359 m2 g-1) using kenaf fiber-based biochar through chemical activation. The achieved specific surface area surpasses activated carbon derived from other reported fiber-based precursors. The resulting activated carbon was investigated as electrodes for supercapacitors, revealing a remarkable maximum capacitance of 312 F g-1 at a current density of 0.5 A g-1. An aqueous symmetric supercapacitor employing these high-surface-area electrodes exhibited an outstanding energy density of 18.9 Wh kg-1 at a power density of 250 W kg-1. Notably, the supercapacitor retained exceptional capacitance, maintaining 93% of its initial capacitance even after 5000 charge-discharge cycles.
Entanglement and quantum coherence of two YIG spheres in a hybrid Laguerre-Gaussian cavity optomechanics

Hidki A, Peng JX, Singh SK, Khalid M, Asjad M

Sci Rep, 2024 May 16;14(1):11204.
PMID: 38755238 DOI: 10.1038/s41598-024-61670-7

We theoretically investigate continuous variable entanglement and macroscopic quantum coherence in the hybrid L-G rotational cavity optomechanical system containing two YIG spheres. In this system, a single L-G cavity mode and both magnon modes (which are due to the collective excitation of spins in two YIG spheres) are coupled through the magnetic dipole interaction whereas the L-G cavity mode can also exchange orbital angular momentum (OAM) with the rotating mirror (RM). We study in detail the effects of various physical parameters like cavity and both magnon detunings, environment temperature, optorotational and magnon coupling strengths on the bipartite entanglement and the macroscopic quantum coherence as well. We also explore parameter regimes to achieve maximum values for both of these quantum correlations. We also observed that the parameters regime for achieving maximum bipartite entanglement is completely different from macroscopic quantum coherence. So, our present study shall provide a method to control various nonclassical quantum correlations of macroscopic objects in the hybrid L-G rotational cavity optomechanical system and have potential applications in quantum sensing, quantum meteorology, and quantum information science.
Cerebral toxoplasmosis in Malaysia: a debilitating disease, an insight from a case study

Muslim A, Mohd Rustam FR, Mohd Khalid MS, Sahlan N

Trop Biomed, 2024 Sep 01;41(3):271-275.
PMID: 39548780 DOI: 10.47665/tb.41.3.006

Toxoplasmosis is an infectious disease caused by the intracellular protozoan parasite, Toxoplasma gondii. While the infection is typically asymptomatic in healthy individuals, it can progress to cerebral toxoplasmosis, especially in those with human immunodeficiency virus (HIV) or weakened immune systems. In this communication, we present a case of a newly diagnosed HIV infection patient who presented with neurological symptoms. The patient was later diagnosed with probable cerebral toxoplasmosis. The case depicts the severe consequences of toxoplasmosis in immunocompromised patients, highlighting the urgent need to identify those at high risk of contracting the disease and the importance of prophylactic treatment. This requires the necessity for early HIV diagnosis and close monitoring of HIV-positive patients.
Fulltext Phenoxyacetohydrazide Schiff bases: β-glucuronidase inhibitors

Jamil W, Perveen S, Shah SA, Taha M, Ismail NH, Perveen S, et al.

Molecules, 2014 Jun 25;19(7):8788-802.
PMID: 24968334 DOI: 10.3390/molecules19078788

Phenoxyacetohydrazide Schiff base analogs 1-28 have been synthesized and their in vitro β-glucouoronidase inhibition potential studied. Compounds 1 (IC50=9.20±0.32 µM), 5 (IC50=9.47±0.16 µM), 7 (IC50=14.7±0.19 µM), 8 (IC50=15.4±1.56 µM), 11 (IC50=19.6±0.62 µM), 12 (IC50=30.7±1.49 µM), 15 (IC50=12.0±0.16 µM), 21 (IC50=13.7±0.40 µM) and 22 (IC50=22.0±0.14 µM) showed promising β-glucuronidase inhibition activity, better than the standard (D-saccharic acid-1,4-lactone, IC50=48.4±1.25 µM).
Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease

Rahim F, Javed MT, Ullah H, Wadood A, Taha M, Ashraf M, et al.

Bioorg Chem, 2015 Oct;62:106-16.
PMID: 26318401 DOI: 10.1016/j.bioorg.2015.08.002

A series of thirty (30) thiazole analogs were prepared, characterized by (1)H NMR, (13)C NMR and EI-MS and evaluated for Acetylcholinesterase and butyrylcholinesterase inhibitory potential. All analogs exhibited varied butyrylcholinesterase inhibitory activity with IC50 value ranging between 1.59±0.01 and 389.25±1.75μM when compared with the standard eserine (IC50, 0.85±0.0001μM). Analogs 15, 7, 12, 9, 14, 1, 30 with IC50 values 1.59±0.01, 1.77±0.01, 6.21±0.01, 7.56±0.01, 8.46±0.01, 14.81±0.32 and 16.54±0.21μM respectively showed excellent inhibitory potential. Seven analogs 15, 20, 19, 24, 28, 30 and 25 exhibited good acetylcholinesterase inhibitory potential with IC50 values 21.3±0.50, 35.3±0.64, 36.6±0.70, 44.81±0.81, 46.36±0.84, 48.2±0.06 and 48.72±0.91μM respectively. All other analogs also exhibited well to moderate enzyme inhibition. The binding mode of these compounds was confirmed through molecular docking.
Koetjapic acid, a natural triterpenoid, induces apoptosis in colon cancer cells

Nassar ZD, Aisha AF, Idris N, Khadeer Ahamed MB, Ismail Z, Abu-Salah KM, et al.

Oncol Rep, 2012 Mar;27(3):727-33.
PMID: 22134768 DOI: 10.3892/or.2011.1569

Deregulated cell signaling pathways result in cancer development. More than one signal transduction pathway is involved in colorectal cancer pathogenesis and progression. Koetjapic acid (KA) is a naturally occurring seco-A-ring oleanene triterpene isolated from the Sandoricum koetjape stem bark. We report the cellular and molecular mechanisms of anticancer activity of KA towards human colorectal cancer. The results showed that KA induces apoptosis in HCT 116 colorectal carcinoma cells by inducing the activation of extrinsic and intrinsic caspases. We confirmed that KA-induced apoptosis was mediated by DNA fragmentation, nuclear condensation and disruption in the mitochondrial membrane potential. Further studies on the effect of KA on cancer pathways show that the compound causes down-regulation of Wnt, HIF-1α, MAP/ERK/JNK and Myc/Max signaling pathways and up-regulates the NF-κB signaling pathway. The result of this study highlights the anticancer potential of KA against colorectal cancer.
New isatin derivative inhibits neurodegeneration by restoring insulin signaling in brain

Aftab MF, Afridi SK, Mughal UR, Karim A, Haleem DJ, Kabir N, et al.

J. Chem. Neuroanat., 2017 04;81:1-9.
PMID: 28093241 DOI: 10.1016/j.jchemneu.2017.01.001

Diabetes is associated with neurodegeneration. Glycation ensues in diabetes and glycated proteins cause insulin resistance in brain resulting in amyloid plaques and NFTs. Also glycation enhances gliosis by promoting neuroinflammation. Currently there is no therapy available to target neurodegenration in brain therefore, development of new therapy that offers neuroprotection is critical. The objective of this study was to evaluate mechanistic effect of isatin derivative URM-II-81, an anti-glycation agent for improvement of insulin action in brain and inhibition of neurodegenration. Methylglyoxal induced stress was inhibited by treatment with URM-II-81. Also, Ser473 and Ser9 phosphorylation of Akt and GSK-3β respectively were restored by URM-II-81. Effect of URM-II-81 on axonal integrity was studied by differentiating Neuro2A using retinoic acid. URM-II-81 restored axonal length in MGO treated cells. Its effects were also studied in high fat and low dose streptozotocin induced diabetic mice where it reduced RBG levels and inhibited glycative stress by reducing HbA1c. URM-II-81 treatment also showed inhibition of gliosis in hippocampus. Histological analysis showed reduced NFTs in CA3 hippocampal region and restoration of insulin signaling in hippocampii of diabetic mice. Our findings suggest that URM-II-81 can be developed as a new therapeutic agent for treatment of neurodegenration.
Fulltext Antiangiogenic properties of Koetjapic acid, a natural triterpene isolated from Sandoricum koetjaoe Merr

Nassar ZD, Aisha AF, Ahamed MB, Ismail Z, Abu-Salah KM, Alrokayan SA, et al.

Cancer Cell Int, 2011;11(1):12.
PMID: 21524294 DOI: 10.1186/1475-2867-11-12

Angiogenesis, the formation of new blood vessels, has become an important target in cancer therapy. Angiogenesis plays an important role in tumor growth and metastasis. Koetjapic acid (KA) is a seco-A-ring oleanene triterpene isolated from S. koetjape. The solvent extract of this plant species was shown previously to have strong antiangiogenic activity; however the active ingredient(s) that conferred the biological activity and the mode of action was not established. Given the high concentration of KA in S. koetjape, an attempt has been made in this study to investigate the antiangiogenic properties of KA.

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