Recent Advances in Biological Active Sulfonamide based Hybrid Compounds Part A: Two-Component Sulfonamide Hybrids.

Sulfonamides constitute an important class of drugs, with many types of pharmacological agents possessing antibacterial, anti-carbonic anhydrase, anti-obesity, diuretic, hypoglycemic, antithyroid, antitumor, and anti-neuropathic pain activities. The sulfonamides are the compounds that have general formula R-SO2NHR', where the functional group is bound to aromatic, heterocycle, and aliphatic groups. The nature of the R and R' moiety is variable, starting with hydrogen and ranging to a variety of moieties incorporating organic compounds such as coumarin, isoxazole, tetrazole, pyrazole, pyrrole, and so many other pharmaceutical active scaffolds that lead to a considerable range of hybrids named as sulfonamide hybrids. Part A of this review presents the most recent advances in designing and developing two-component sulfonamide hybrids containing coumarin, indole, quinoline, isoquinoline, chalcone, pyrazole/pyrazoline, quinazoline, pyrimidine, thiazole, benzothiazole, and pyridine between 2015 and 2020. Specifically, the authors review the scientific reports on the synthesis and biological activity of this kind of hybrid agent.

Recent Advances in Biological Active Sulfonamide based Hybrid Compounds Part C: Multicomponent Sulfonamide Hybrids.

Sulfonamides, with the general formula R-SO2NR1R2, have attracted great attention since the early discovery of sulfonamide-containing antibacterial drugs. The combinations of certain sulfonamides and other drug molecules to form sulfonamide hybrids are being used to develop novel formulations with greater effectiveness and in a huge range of therapeutic applications such as antimicrobial, antifungal, anti-inflammatory, antitubercular, antiviral, antidiabetic, antiproliferative, carbonic anhydrase inhibitor, antimalarial, anticancer and other medicinal agents. Part C of this review presents recent advances in designing and developing multicomponent sulfonamide hybrids containing more than one biologically active heterocycle, such as coumarin, indole, pyridine, pyrimidine, pyrazole, triazole, oxazole, oxadiazole, triazine, quinazoline, and thiadiazol. This review aims to highlight the status of the hybridization technique in synthesizing biological and computational studies of novel sulfonamide hybrids that were designed and presented between 2016 and 2020.

Preparation of new hydrogels by visible light cross-linking of dextran methacrylate and poly(ethylene glycol)-maleic acid copolymer.

In this work, a series of new biodegradable and biocompatible hydrogels were synthesized by photopolymerization of dextran-methacrylate (DXM) with poly(ethylene glycol)-maleic acid copolymer (poly(PEG-co-MA, PEGMA)) using (-)-riboflavin as a visible light photoinitiator and L-arginine as a co-photoinitiator. DXM was prepared by acylation of dextran (DX) with methacryloyl chloride (MAC), and PEGMA was synthesized by polycondensation of poly(ethylene glycol) (PEG) and maleic acid (MA). The DXM and PEGMA were characterized by FT-IR and 1HNMR spectroscopy. Different types of hydrogels from various ratios of DXM and PEGMA were prepared and characterized by SEM. The results showed that the prepared hydrogel by photo-cross-linking of DXM (DPHG0) was transparent and flexible, and its physical shape was excellent, but it was sticky. The stickiness was reduced by increasing the PEGMA contents, and different types of DXM/PEGMA hydrogels (DPHG1-4) with various properties were prepared. For example, DPHG2 (PEGMA content was 0.25 g) was transparent and flexible, its physical shape was excellent, and it was not sticky. The prepared hydrogels showed excellent cytocompatibility, and their tensile and compressive strength were also evaluated. Additionally, the in vitro degradation and swelling ratios of the prepared hydrogels were studied in buffer solution at different pHs.

Recent Advances in Biological Active Sulfonamide based Hybrid Compounds Part B: Two-Component Sulfonamide Hybrids.

Sulfonamide compounds, also known as sulfa drugs, are a significant class of synthetic bacteriostatic antimicrobials and were the primary source of therapy against bacterial infections before the introduction of penicillin in 1941. Hybridization of sulfonamides with various pharmaceutically active heterocyclic moieties leads to sulfonamide hybrids with a wide variety of biological activities. Part B of this review presents the most recent advances in designing and developing more two-component sulfonamide hybrids containing triazole, thiadiazole, triazine, oxazole/ benzoxazole, isoxazole, oxadiazole, imidazole, benzimidazole, furan, benzofuran, thiophene, pyrrole, indazole, tetrazole, chromene/ chromone, pyridazine, quinoxaline, acridine, phthalazine, and xanthone between 2015 and 2020. We hope this review helps the scientific community in designing more useful sulfonamide hybrid drugs.

Cyclic and Linear Sweep Voltammetric Studies of a Modified Carbon Paste Electrode with Nickel Oxide Nanoparticles toward Tamoxifen: Effects of Surface Modification on Electrode Response Kinetics.

Due to the serious adverse futures of some anticancer drugs, the determination of trace amounts of these drugs by simple analytical techniques is of great interest. In this regard, knowing about the mechanism of the analyte with the sensing material plays an important role. Nickel oxide nanoparticles (NiO NPs) modified by a carbon paste electrode (NiO-CPE) showed an irreversible cyclic voltammetric (CV) behavior in the NaOH (pH 13) supporting electrolyte based on the peak separation of 311 mV. Its peak current was decreased by adding tamoxifen (TAM), confirming that TAM molecules can consume NiO before participating in the electrode reaction. For this goal, TAM can be oxidized or reduced, and the corresponding mechanisms are schematically illustrated in the text. This study focused on the kinetic aspects of the process. Based on the CV results, a surface coverage (Γ) value of 2.72 × 10-5 mol NiO per cm2 was obtained with charge transfer coefficients αa and αc of 0.317 and 0.563, respectively. αa and αc values were changed to 0.08 and 0.72 in the presence of TAM. Further, the rate constant (k s) value was 0.021 ± 0.01 s-1 in the presence of TAM. In linear sweep voltammetry (LSV), an α value of about 0.636 ± 0.023 and an exchange rate constant (k o) value of about 0.097 ± 0.031 s-1 were obtained in the absence of TAM, which changed to 0.62 ± 0.081 and 0.089 ± 0.021 s-1 in the presence of TAM, respectively. Despite more published papers, when the TAM analyte was added to the NaOH supporting electrolyte, both anodic and cathodic peak currents of the modified NiO-CPE decreased. We suggested some reasons for this decreased peak current, and four mechanisms were illustrated for the electrode response in the presence of TAM.

Efficient hydrolysis of starch by α-amylase immobilized on cloisite 30B and modified forms of cloisite 30B by adsorption and covalent methods.

In this paper, α-amylase from Bacillus subtilis was successfully immobilized on three supports. First, α-amylase was immobilized on cloisite 30B via the adsorption method. Then cloisite 30B was activated with tosyl chloride and epichlorohydrin. These activated supports were used for covalent immobilization of α-amylase, and their enzymatic activities were effectively tested in the starch hydrolysis. The results demonstrated that the specific activity of α-amylase immobilized on cloisite 30B was 2.39 ± 0.03, for α-amylase immobilized on activated cloisite 30B with epichlorohydrin was 1.96 ± 0.05 and for α-amylase immobilized on activated cloisite 30B with tosyl chloride was 2.17 ± 0.05 U mg-1. The optimum pH for the activity of free α-amylase was 7, but for α-amylase immobilized on cloisite 30B was 8, and for α-amylase immobilized on activated supports was 7.5. The immobilized enzymes had better thermal resistance and storage stability than free α-amylase, and they also showed excellent reusability.

Covalent immobilization of lipase from Candida rugosa on epoxy-activated cloisite 30B as a new heterofunctional carrier and its application in the synthesis of banana flavor and production of biodiesel.

In this paper, an epoxy-activated cloisite (ECL) was prepared as a new heterofunctional carrier via a reaction between cloisite 30B (CL) and epichlorohydrin and utilized for covalent immobilization of lipase from Candida rugosa. The lipase immobilized on the ECL (LECL) was successfully used in the olive oil hydrolysis, synthesis of isoamyl acetate (banana flavor), and biodiesel production. The TGA, FT-IR, SEM, and XRD were used to characterize CL, ECL, and LECL. The influences of temperature, pH, thermal stability, and storage capacity were examined in the olive oil hydrolysis. The effects of solvent, temperature, time, water content, and substrates molar ratio on the yields of ester and biodiesel were also investigated. In the optimized conditions, the hydrolytic activity of LECL was 1.85 ± 0.05 U/ mg, and the maximum yield of ester and biodiesel was 91.6% and 95.4%, respectively. The LECL showed good thermal stability and storage capacity compared to the free lipase. Additionally, LECL was reusable for both esterification and transesterification after being used for nine cycles.

Make proper surfaces for immobilization of enzymes: Immobilization of lipase and α-amylase on modified Na-sepiolite.

This paper has focused on making suitable carriers for the immobilization of α-amylase from Bacillus subtilis and lipase from Candida rugosa via adsorption on modified Na-sepiolite (SEP). Two modified carriers were prepared by changing the nature of SEP with cetrimonium bromide surfactant at concentrations below the CMC of the surfactant, to produce SEP with monolayer surfactant (MSEP) with hydrophobic properties and above the CMC of the surfactant to produce SEP with bilayer surfactant (BSEP) with hydrophilic properties. The enzymatic activity of immobilized lipase on MSEP (MSEPL) and immobilized α-amylase on BSEP (BSEPA) was successfully tested in the hydrolysis of olive oil and starch. The support modification and immobilization process were characterized by BET, XRD, and SEM techniques. The results demonstrated that the specific activity of MSEPL and BSEPA was 1.74 and 2.28 U/mg, respectively. The remained activity of MSEPL (56.7%) and BSEPA (40.4%) after their incubation at 60 °C for 4 h was much higher than that of free enzymes. The residual activity of MSEPL and BSEPA was 77.4% and 66.7%, after 30 days of storage at 4 °C. The MSEPL and BSEPA also showed good reusability, and their relative activities were 54.0% and 44.2% after ten cycles.

Utilization of two modified layered doubled hydroxides as supports for immobilization of Candida rugosa lipase.

In this study, two synthetic layered doubled hydroxides (LDH), including Mg/Al-CO3-LDH (LDH1) and Zn/Al-CO3-LDH (LDH2), were prepared using the co-precipitation method and modified with sodium dodecyl sulfate to be utilized as carriers for immobilization of Candida rugosa lipase via the adsorption. The activity of prepared biocatalysts was measured in the olive oil hydrolysis. The effects of lipase concentration, pH, storage stability and thermal resistance of the samples were also studied. The maximum activity was obtained at pH 6.0 for immobilized lipase on modified LDHs with monolayer surfactants, including MLDH1 (0.922 U/mg) and MLDH2 (0.744 U/mg), respectively. The remained activities for immobilized lipase on MLDH1 and MLDH2 after 24 h incubation at 60 °C were 85% and 81%, respectively. During the 25days of storage at 4 °C, immobilized lipases on MLDH1, MLDH2, and free lipase kept 87%, 86%, and 70% of their initial activities. The residual activities for immobilized lipase on MLDH1 and MLDH2 after reusing for ten cycles were 72% and 67% of their initial activities. Adsorption parameters for sorption of lipase on all supports were fitted to the Freundlich and Langmuir isotherms. Kinetic parameters obtained from the Michaelis-Menten equation on MLDH1 and MLDH2 were comparable to free enzyme.

Evaluating the effect of Myrtus communis on programmed cell death in hydatid cyst protoscolices.

OBJECTIVE: To evaluate the possible involvement of programmed cell death strategy in hydatid cyst protoscolices following treatment with Myrtus communis (M. communis) as an herbal medicine. METHODS: Protoscolices were aseptically collected from sheep liver hydatid cysts. Evaluating the effect of M. communis extract on programmed cell death and increased activity of caspases 3, 8, and 9 in hydatid cyst protoscolices was conducted by treating the protoscolices with different concentration (5, 50, and 100 mg/mL) of M. communis extract at 37 °C and 5% CO2 for 4 h by using the Bradford test and ELISA commercial kits. RESULTS: The extract of M. communis at all concentrations led to initiation of programmed cell death in protoscolices and this effect, was only significant at 50 and 100 mg/mL concentrations, compared to the negative control (P < 0.05). Also, the activity of caspases 3, 8, and 9 in hydatid cyst protoscolices, was shown that the extract at all 3 concentrations could only increase the activity of caspases 3 and 9. Moreover, a significant increase in the activity of caspase 3 was only observed at concentrations 50 and 100 mg/mL by 37.00% and 66.19% while a significant increase in the activity of caspase 9 at the same concentrations was observed by 20.89% and 63.67%, respectively (P < 0.05). CONCLUSIONS: The extract of M. communis at different concentrations could increase the activity of caspases 3 and 9 and caused programmed cell death in hydatid cyst protoscolices however, this effect was significant at high concentrations of the extract.