Improving Aqueous Solubility of Natural Antioxidant Mangiferin through Glycosylation by Maltogenic Amylase from Parageobacillus galactosidasius DSM 18751

Mangiferin is a natural antioxidant C-glucosidic xanthone originally isolated from the Mangifera indica (mango) plant. Mangiferin exhibits a wide range of pharmaceutical activities. However, mangiferin’s poor solubility limits its applications. To resolve this limitation of mangiferin, enzymatic glycosylation of mangiferin to produce more soluble mangiferin glucosides was evaluated. Herein, the recombinant maltogenic amylase (MA; E.C. 3.2.1.133) from a thermophile Parageobacillus galactosidasius DSM 18751T (PgMA) was cloned into Escherichia coli BL21 (DE3) via the expression plasmid pET-Duet-1. The recombinant PgMA was purified via Ni2+ affinity chromatography. To evaluate its transglycosylation activity, 17 molecules, including mangiferin (as sugar acceptors), belonging to triterpenoids, saponins, flavonoids, and polyphenol glycosides, were assayed with β-CD (as the sugar donor). The results showed that puerarin and mangiferin are suitable sugar acceptors in the transglycosylation reaction. The glycosylation products from mangiferin by PgMA were isolated using preparative high-performance liquid chromatography. Their chemical structures were glucosyl-α-(1→6)-mangiferin and maltosyl-α-(1→6)-mangiferin, determined by mass and nucleic magnetic resonance spectral analysis. The newly identified maltosyl-α-(1→6)-mangiferin showed 5500-fold higher aqueous solubility than that of mangiferin, and both mangiferin glucosides exhibited similar 1,1-diphenyl-2-picrylhydrazyl free radical scavenging activities compared to mangiferin. PgMA is the first MA with glycosylation activity toward mangiferin, meaning mangiferin glucosides have potential future applications.

ANTIMICROBIAL, ANTIOXIDANT AND CYTOTOXIC EVALUATION OF VARIOUS EXTRACTS OF IFLOGA SPICATA (FORSSK.) SCH.BIP

The current study reveals the pharmacological and phytochemical potential of different solvent fractions of Ifloga spicata. Antimicrobial and free radical scavenging activities, DPPH (1, 1-diphenyl-2-picrylhydrazyl), hydrogen peroxide scavenging assay, and cytotoxic effects of plant samples on lymphocytes stressed with hydrogen were performed. Ifloga spicata ethyl acetate fraction markedly showed higher antibacterial potential against P. aeruginosa (ATCC 27853) and E. Coli (ATCC 25922) bacteria. While higher antifungal potential was shown by the chloroform fraction against all three different a strain A. fumigates (ATCC 204305), A. flavus (ATCC 9643) and A. niger (ATCC 16404) as compared to others fractions of sample. DPPH maximum antioxidant potential was noted for methanolic extract followed by ethyl acetate and chloroform. Similarly, hydrogen peroxide effect was significantly decreased by ethyl acetate fraction. In blood lymphocytes the raise in ROS and TBARS level due to stress given by H2O2 was also recovered by different extracts of I. spicata. The decrease level of CAT, SOD and POD was also restored

Radical Scavenging and Catalytic Activity of Fe-Cu Bimetallic Nanoparticles Synthesized from Ixora finlaysoniana Extract

Iron–copper bimetallic nanoparticles (Fe-Cu BNPs) were prepared via a green synthesis route. Ixora finlaysoniana has been used in this study as a capping and stabilizing agent in the modification of Fe-Cu BNPs. As-synthesized BNPs were characterized using different techniques including UV/Vis spectrophotometry, FTIR, XRD and SEM. A particle size analyzer and SEM studies indicated the particle size to be in the range of 50–200 nm. In addition, degradation of MB dye in an aqueous system and radical-scavenging potential in a DPPH assay were also examined using BNPs. Methylene blue dye degradation in 17 min was monitored with UV/Vis spectrophotometry, which exhibited the efficiency of Fe-Cu BNPs. Bimetallic nanoparticles were also found to be efficient in neutralizing DPPH free radicals. Furthermore, kinetic studies of both dye degradation and radical scavenging potential are reported in this article. Subsequently, Fe-Cu BNPs synthesized via a green and sustainable method can be employed for dye degradation and free radical-scavenging activities.

Bioactivities of holmium(III) and gadolinium(III) complexes of thymoquinone

Chemotherapeutic agents which are the main stay in cancer treatment are toxic with numerous contrary side effects. A number of chemical, physical, and computational techniques were applied to synthesize and elucidate the structural and functional characterization of the new designed bioligands and their metal complexes. Besides, several biological techniques for developing therapeutics and diagnostics agents of these new designed materials were used. The trivalent holmium(III) and gadolinium(III) metal complexes of thymoquinone (TQ) were synthesized. Toxicities and other bioactivites were undertaken with existing drug combinations and more effective tumor models will be established. The molecular structures of TQ-metal complexes were elucidated based on particular spectral approaches. The NF-kB (nuclear factor kappa-light-chain enhancer of activated B Cells) luciferase, elastase release, superoxide anion (O2•−) generation, and DPPH (1,1-diphenyl-2-picryl hydrazyl) free-radical scavenging activities of TQ and its synthesized complexes were elucidated and discussed. The core research is to use coordination and organometallic chemistry to design new bioligands and binary, ternary, mixed ligand, multi metal multi ligand complexes pursing a bio target continuously with structure-activity relationships (SARS). KEY WORDS: Thymoquinone, Holmium, Gadolinium, Bioactivities Bull. Chem. Soc. Ethiop. 2021, 35(1), 87-96. DOI: https://dx.doi.org/10.4314/bcse.v35i1.7

Chemical composition, in vitro antioxidant, anticholinesterase, and antidiabetic potential of essential oil of Elaeagnus umbellata Thunb

Background Elaeagnus umbellata Thunb. (autumn olive) is a high valued medicinal plant. It belongs to Elaeagnaceae family and is widely distributed in Himalayan regions of Pakistan. In the present study essential oil were extracted from the fruit of this plant and their antioxidant, anticholinesterase and antidiabetic potentials were also evaluated. Methods Essential oils were extracted from the fruit of E. umbellata using hydro-distillation method and were characterized by GC-MS. The extracted oil were tested for its antioxidant, anticholinesterase, and antidiabetic potentials using standard protocols. Results About 68 compounds were identified by GC-MS. The extracted oil exhibited a fairly high free radical scavenging activities against DPPH and ABTS radicals with IC50 values of 70 and 105 μg/mL respectively (for ascorbic acid, used as standard, the IC50 values were 32 and 29 μg/mL, respectively against the mentioned radicals). The essential oil also exhibited anticholinesterase activities with IC50 values of 48 and 90 μg/mL respectively against AChE and BChE (for galantamine used as standard, the IC50 values were 25 and 30 μg/mL respectively). The essential oil also exhibited antidiabetic potential with IC50 values of 120 and 110 μg/mL respectively against α-glucosidase and α-amylase (IC50 values for standard acarbose = 28 and 30 μg/mL respectively). Conclusion Essential oil extracted from the fruits of E. umbellata exhibited reasonable antioxidant, anticholinesterase, and antidiabetic potentials that could be used as alternative medicine in treating diabetes and neurodegenerative disorders. However, further studies are needed to isolate responsible compounds and evaluate the observed potential in animal models. Graphical abstract

In vitro inhibitory potential of avocado fruits, Persea americana (Lauraceae) against oxidation, inflammation and key enzymes linked to skin diseases

Avocado (Persea americana Mill.) is a member of Lauraceae with one-seeded berry fruit and cultivated in all tropical, subtropical regions in the world and in the Southern coast region of Turkey. Oxidative damage caused by UV can trigger inflammation, resulting in serious inflammatory skin diseases including eczema, seborrheic dermatitis, hyperpigmentation and ageing. Enzyme inhibitors involved in melanogenesis, such as tyrosinase, have been used recently for hyperpigmentation and skin diseases in cosmetic products. Objective: This study aimed to evaluate the antioxidant, anti-inflammatory, anti-tyrosinase activities and total polyphenolic contents of the different parts of P. americana fruit. Methods: The fruit was divided into exocarp, mesocarp, seed, and then methanol and n-hexane extracts were prepared. DPPH and ABTS free radical scavenging capacities and inhibitory potentials on lipid peroxidation were determined to investigate the antioxidant potentials of the extracts. Anti-inflammatory activities of the extracts were evaluated by measuring the stabilization level of the human red blood cell membrane. The tyrosinase inhibitory activities of the samples were determined using mushroom tyrosinase. Results: In general methanol extracts possessed remarkable higher DPPH free radical scavenging activities than n-hexane extracts. The highest activity was determined in methanol extracts of seed (4.17 ± 0.04 mg/mL) followed by exocarp (5.25 ± 0.05 mg/mL). Overall methanol extracts possessed higher ABTS free radical scavenging activities than n-hexane extracts. The greatest ABTS free radical scavenging activity was obtained in methanol extracts of seed (0.03 ± 0.01 mg/mL). In the anti-lipid peroxidation assay, the greatest activity was noticed in methanol extracts of seed (7.71 ± 0.36 µg/mL) followed by exocarp (12.12 ± 0.34 µg/mL), while all n-hexane extracts were inactive. Overall methanol extracts exhibited higher anti-inflammatory and antioxidant properties than n-hexane extracts. However, the maximum anti-tyrosinase activity was determined in n-hexane extracts of exocarp (0.40 ± 0.01 mg/mL) followed by seed (0.46 ± 0.01 mg/mL). Conclusions: These extracts are promising candidates for use as natural products-based antioxidant and anti-inflammatory properties in inflammation-related disease, and also anti-tyrosinase properties in dermatological applications.