The protective effect of aqueous extracts of roselle (Hibiscus sabdariffa L. UKMR-2) against red blood cell membrane oxidative stress in rats with streptozotocin-induced diabetes

OBJECTIVES:

The aim of this study was to investigate the protective effects of aqueous extracts of roselle (Hibiscus sabdariffa L. UKMR-2) against red blood cell (RBC) membrane oxidative stress in rats with streptozotocin-induced diabetes.

METHODS:

Forty male Sprague-Dawley rats weighing 230-250 g were randomly divided into four groups (n = 10 rats each): control group (N), roselle-treated control group, diabetic group, and roselle-treated diabetic group. Roselle was administered by force-feeding with aqueous extracts of roselle (100 mg/kg body weight) for 28 days.

RESULTS:

The results demonstrated that the malondialdehyde levels of the red blood cell membranes in the diabetic group were significantly higher than the levels in the roselle-treated control and roselle-treated diabetic groups. The protein carbonyl level was significantly higher in the roselle-treated diabetic group than in the roselle-treated control group but lower than that in the diabetic group. A significant increase in the red blood cell membrane superoxide dismutase enzyme was found in roselle-treated diabetic rats compared with roselle-treated control rats and diabetic rats. The total protein level of the red blood cell membrane, osmotic fragility, and red blood cell morphology were maintained.

CONCLUSION:

The present study demonstrates that aqueous extracts of roselle possess a protective effect against red blood cell membrane oxidative stress in rats with streptozotocin-induced diabetes. These data suggest that roselle can be used as a natural antioxidative supplement in the prevention of oxidative damage in diabetic patients.     

A dopamine electrochemical sensor based on a platinum–silver graphene nanocomposite modified electrode

A platinum–silver graphene (Pt–Ag/Gr) nanocomposite modified electrode was fabricated for the electrochemical detection of dopamine (DA). Electrochemical studies of the Pt–Ag/Gr nanocomposite towards DA detection were performed by cyclic voltammetry (CV) and differential pulse voltammetry (DPV). The CV analysis showed that Pt–Ag/Gr/GCE had enhanced electrocatalytic activity towards DA oxidation due to the synergistic effects between the platinum–silver nanoparticles and graphene. The DPV results showed that the modified sensor demonstrated a linear concentration range between 0.1 and 60 μM with a limit of detection of 0.012 μM. The Pt–Ag/Gr/GCE presented satisfactory results for reproducibility, stability and selectivity. The prepared sensor also showed acceptable recoveries for a real sample study.

A platinum–silver graphene nanocomposite was synthesized and characterized. A nanocomposite modified electrode was fabricated in order to investigate the electrochemical detection of dopamine.     

Discovery of 4-(2-(dimethylamino)ethoxy)benzohydrazide derivatives as prospective microtubule affinity regulating kinase 4 inhibitors

Microtubule affinity regulating kinase 4 (MARK4) is a Ser/Thr kinase, considered as a potential drug target for cancer, diabetes and neurodegenerative diseases. Due to its significant role in the development and progression of cancer, different in-house libraries of synthesized small molecules were screened to identify potential MARK4 inhibitors. A small library of hydrazone compounds showed a considerable binding affinity to MARK4. The selected compounds were further scrutinized using an enzyme inhibition assay and finally two hydrazone derivatives (H4 and H19) were selected that show excellent inhibition (nM range). These compounds have a strong binding affinity for MARK4 and moderate binding with human serum albumin. Anticancer studies were performed on MCF-7 and A549 cells, suggesting H4 and H19 selectively inhibit the growth of cancer cells. The IC₅₀ value of compound H4 and H19 was found to be 27.39 μM and 34.37 μM for MCF-7 cells, while for A549 cells it was 45.24 μM and 61.50 μM, respectively. These compounds inhibited the colonogenic potential of cancer cells and induced apoptosis. Overall findings reflect that hydrazones/hydrazone derivatives could be exploited as potential lead molecules for developing effective anticancer therapies via targeting MARK4.

Inhibition studies of MARK4 with selected hydrazone derivatives.     

Metal oxide QD based ultrasensitive microsphere fluorescent sensor for copper,chromium and iron ions in water

Herein we developed a rapid, cheap, and water-soluble ultra-sensitive ZnO quantum dot (QD) based metal sensor for detecting different hazardous metal ions up to the picomolar range in water. Various spectroscopic and microscopic techniques confirmed the formation of 2.15 ± 0.46 μm of ZnO QD conjugated CMC microspheres (ZCM microspheres) which contain 5.5 ± 0.5 nm fluorescent zinc oxide (ZnO) QDs. Our system, as a promising sensor, exhibited excellent photostability and affinity towards various heavy metal ions. The detection limits were calculated to be 16 pM for Cu²⁺ and 0.18 nM for Cr⁶⁺ ions which are better than previously reported values. The simple fluorescence ‘turn off’ property of our ZCM microsphere sensor system can serve a two-in-one purpose by not only detecting the heavy metals but also quantifying them. Nonetheless, pattern recognition for different heavy metals helped us to detect and identify multiple heavy metal ions. Finally, their practical applications on real samples also demonstrated that the ZCM sensor can be effectively utilized for detection of Cr⁶⁺, Fe³⁺, Cu²⁺ present in the real water samples. This study may inspire future research and design of target fluorescent metal oxide QDs with specific functions.

Herein we developed a rapid, cheap, and water-soluble ultra-sensitive ZnO quantum dot (QD) based metal sensor for detecting different hazardous metal ions up to the picomolar range in water.     

Copper mediated one-pot synthesis of quinazolinones and exploration of piperazine linked quinazoline derivatives as anti-mycobacterial agents

A facile method was developed for the synthesis of quinazolinone derivatives in a one-pot condensation reaction via in situ amine generation using ammonia as the amine source and with the formation of four new C–N bonds in good to excellent yields. With the optimised method, we synthesized a library of piperazine linked quinazoline derivatives and the synthesized compounds were evaluated for their inhibitory activity against Mycobacterium tuberculosis. The compounds 8b, 8e, 8f, 8m, 8n and 8v showed potent anti-mycobacterial activity with MIC values of 2–16 μg mL⁻¹. All the synthesized compounds follow Lipinski''s rules for drug likeness.

A facile method was developed for the synthesis of quinazolinone derivatives in a one-pot condensation reaction via in situ amine generation using ammonia as the amine source and with the formation of four new C–N bonds in good to excellent yields.     

Assessing the Validity of Western Measurement of Online Risks to Children in an Asian Context

Before the advent of the Internet, television and film was the only audio-visual medium to which most children were exposed. The risks were primarily limited to children being exposed to sexual and violent materials, the nature of which were known and easy to control. Nowadays, children are surrounded by a variety of digital media and are exposed to different risks, many of which are still unknown. The Internet is fully integrated into children’s daily lives, along with the potential risks. The present study aimed to (i) describe the level of risks children are exposed to, and (ii) test the measurement validity of a total of 45 items assessing nine scales of online risk to children that were adapted from studies carried out in Europe and the United States. The study comprised 420 schoolchildren. The results showed that children were more exposed to ‘unwanted exposure to pornography’ and less to ‘conduct risk’ (e.g., accidental illegal downloading; creating profiles on inappropriate websites). Boys and older children were more exposed to the risks compared to girls and younger children. The study validated five dimensions (inappropriate materials, sexting, contact-related risks, risky online sexual behavior, and bullying/being bullied) assessing online risk to children by using exploratory and confirmatory factor analyses. The study found that scales developed in Europe and the United States are not wholly suitable to an Asian context and needed to be modified. Further investigation to classify online risks to children and offer a solutions to reducing the online risks.     

Formulation of 3D Printed Tablet for Rapid Drug Release by Fused Deposition Modeling: Screening Polymers for Drug Release,Drug-Polymer Miscibility and Printability

The primary aim of this study was to identify pharmaceutically acceptable amorphous polymers for producing 3D printed tablets of a model drug, haloperidol, for rapid release by fused deposition modeling. Filaments for 3D printing were prepared by hot melt extrusion at 150°C with 10% and 20% w/w of haloperidol using Kollidon^® VA64, Kollicoat^® IR, Affinsiol^?15 cP, and HPMCAS either individually or as binary blends (Kollidon^® VA64 + Affinisol^? 15 cP, 1:1; Kollidon^® VA64 + HPMCAS, 1:1). Dissolution of crushed extrudates was studied at pH 2 and 6.8, and formulations demonstrating rapid dissolution rates were then analyzed for drug-polymer, polymer-polymer and drug-polymer-polymer miscibility by film casting. Polymer-polymer (1:1) and drug-polymer-polymer (1:5:5 and 2:5:5) mixtures were found to be miscible. Tablets with 100% and 60% infill were printed using MakerBot printer at 210°C, and dissolution tests of tablets were conducted at pH 2 and 6.8. Extruded filaments of Kollidon^® VA64-Affinisol^? 15 cP mixtures were flexible and had optimum mechanical strength for 3D printing. Tablets containing 10% drug with 60% and 100% infill showed complete drug release at pH 2 in 45 and 120 min, respectively. Relatively high dissolution rates were also observed at pH 6.8. The 1:1-mixture of Kollidon^® VA64 and Affinisol^?15 cP was thus identified as a suitable polymer system for 3D printing and rapid drug release.