SYNTHESIS OF 1-BENZOYL-3-PHENYL-1H-PYRAZOLE-4-CARBALDEHYDE AND EVALUATION OF THEIR ANTIOXIDANT AND ANTI-INFLAMMATORY ACTIVITY

Objective: The main objective of this study is to synthesize a series of 1-Benzoyl-3-phenyl-1H-pyrazole-4-carbaldehyde (4a-e) derivatives and evaluation of the synthesized compounds for their antioxidant and anti-inflammatory activity. Methods: A series of substituted acetophenones are condensed with hydrazides to the corresponding hydrazones which are subsequently cyclized by using vilsmier-Haack reaction to give final series of 1-Benzoyl-3-phenyl-1H-pyrazole-4-carbaldehyde (4a-e) derivatives respectively. All newly synthesized compounds were characterized on the basis of infrared, proton nuclear magnetic resonance and mass spectral data and screened for their antioxidant and anti-inflammatory activities. Results: In view of the significant biological activity profile of Pyrazole, the synthesized compounds (4a-e) were evaluated for their antioxidant potency by DPPH, Nitric oxide, Hydroxyl radical scavenging, and Hydrogen Peroxide method. Compounds 4c and 4e showed potent antioxidant activity then standard. Synthesized compounds were also screened for anti-inflammatory activity. Among all the molecules 4c, 4e, and 4d showed significant activity as compared to standard drug diclofenac sodium. Conclusion: in this study, we synthesized 1-Benzoyl-3-phenyl-1H-pyrazole-4-carbaldehyde (4a-e) derivatives. Further, these derivatives showed significant antioxidant and anti-inflammatory activity. Among them, two molecules 4c and 4e have shown near action to the standard.

Fortification of a Desert Using Nanoencapsulated Supercritical Carbon Dioxide Extract of Small Cardamom Seeds: A Nutraceutical Custard with Antioxidant Synergy

Background: 1,8 cineole-rich supercritical CO2 extract of small cardamom seeds of Alleppey green variety exhibiting prominent antioxidant property was microencapsulated and utilized in formulating an antioxidant-rich custard. However, the antioxidant potency of the prepared custard was not appreciable. To redress the phytochemical loss during custard preparation, custard using nanoliposomes was formulated. Patents related to 1,8 cineole-rich food products have been revised thoroughly. Objective: The objective of the current study is to examine whether nanoencapsulation-mediated entrapment of antioxidants is more effective in fortifying a dessert, namely custard, vis-à-vis microencapsulated (spray dried)-mediated enhancement of antioxidative potency in the same. Methods: Our previous investigations have established that nanoliposome of 1,8 cineole-rich supercritical CO2 extract of small cardamom seeds effectively redresses type 2 diabetes and hypercholesterolemia. In the current investigation, this pre-characterized nanoliposome which exhibited appreciable in vitro and in vivo antioxidant efficacy has been utilized at varying concentrations for fortification of a custard. The designer custard samples have been characterized for their sensory and physicochemical properties, identification of the cardamom antioxidants therein and determination of the synergistic efficacy value of the identified antioxidants. Results: The custard formulated with 0.3% nanoliposomes exhibited appreciable antioxidant potency in terms of DPPH radical scavenging activity (304.58±1.09 mg/ml) and reducing power (0.020±0.001 mg BHT/g custard), conferred by its total phenolic content (0.049±0.004 mg GAE/g custard). It also had relatively more stable textural attributes vis-à-vis the control sample (formulated with the non-encapsulated native extract). GC-MS analysis of the nanoliposome-fortified custard confirmed retention of the spice antioxidants namely1,8- cineole, α-terpinyl acetate, α-terpineol and linalool and its synergistic efficacy value being greater than unity, attested to a synergistic presence of cardamom antioxidants therein. The newly formulated custard retained more than 4.5 times of 1,8-cineole (5.05 mg/g custard) vis-à-vis the custard sample (1.12 mg/g custard) prepared with a microencapsulated (spray-dried) formulation of the extract. Additionally, absence of heavy metals in the formulated custard confirmed it to be safe for consumption. Conclusion: This is the first study on application of nanoliposomes of spiceuticals in formulation of a dessert, and more emphatically on use of a ‘green’ supercritical CO2 extract of spice antioxidants in fortification of a dessert to achieve antioxidant synergy.

Green One-Pot Synthesis of Coumarin-Hydroxybenzohydrazide Hybrids and Their Antioxidant Potency

Compounds from the plant world that possess antioxidant abilities are of special importance for the food and pharmaceutical industry. Coumarins are a large, widely distributed group of natural compounds, usually found in plants, often with good antioxidant capacity. The coumarin-hydroxybenzohydrazide derivatives were synthesized using a green, one-pot protocol. This procedure includes the use of an environmentally benign mixture (vinegar and ethanol) as a catalyst and solvent, as well as very easy isolation of the desired products. The obtained compounds were structurally characterized by IR and NMR spectroscopy. The purity of all compounds was determined by HPLC and by elemental microanalysis. In addition, these compounds were evaluated for their in vitro antioxidant activity. Mechanisms of antioxidative activity were theoretically investigated by the density functional theory approach and the calculated values of various thermodynamic parameters, such as bond dissociation enthalpy, proton affinity, frontier molecular orbitals, and ionization potential. In silico calculations indicated that hydrogen atom transfer and sequential proton loss–electron transfer reaction mechanisms are probable, in non-polar and polar solvents respectively. Additionally, it was found that the single-electron transfer followed by proton transfer was not an operative mechanism in either solvent. The conducted tests indicate the excellent antioxidant activity, as well as the low potential toxicity, of the investigated compounds, which makes them good candidates for potential use in food chemistry.

Characterization of Kacang Goat skin Pepsin Soluble Collagen (Psc) and Their Potency as an Antioxidant

Collagen have been interesting material for many utilization such as food, pharmaceutical and cosmetic in various products and target administration, consequently collagen should be prepared as well as type of application. The objective of this research is to prepare collagen from goat skin and investigate the character and their potency as an antioxidant. Kacang goat skin aged 2 years was used for collagen production. Small slice skin was extracted by curing with 0.1% (w/v) pepsin in acetic acid 0.5 M, for 24, 48, dan 72 h at 4°C. The variables observed were molecular weight by Sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS PAGE), microstructure using scanning electron microscope, thermal stability by differential scanning calorimetric, and the antioxidant potency through 2,2-diphenyl-1-picrylhydrazyl (DPPH) inhibition analysis. The result showed the molecular weight range from 25 kDa to 180 kDa, microstructure showed the collagen fibril crosslink, collagen start to denature at 62,28°C, highest dissolved with 1% NaCl concentration and has highest DPPH inhibition at 60 min after hydrolysis. In conclusion, kacang goat skin collagen prepared by pepsin in acetic acid.

Enhanced Antioxidant Activity of Phycocyanin Oligopeptides

Objectives Phycocyanin, a phytonutrient found in blue-green algae, has various beneficial properties, including potent antioxidant effects. The goal of this study was to investigate the antioxidant potency of a novel phycocyanin oligopeptide (PC-O) compared to phycocyanin (PC). Methods Antioxidant potency of PC-O and PC was measured using two different methods: 1) the Folin-Ciocalteu reaction assay, and 2) the Oxygen Radical Absorbance Capacity (ORAC) 6.0 assay. The Folin-Ciocalteu reaction assay (or total phenolics assay) was run using Folin-Ciocalteu's phenol reagent and sodium carbonate. Optical absorbance was measured at 765nm in a colorimetric plate reader with gallic acid as a reference standard. The ORAC 6.0 assay was run to evaluate the antioxidant capacity of a material against six primary reactive oxygen species: peroxyl radical, hydroxyl radical, superoxide anion, singlet oxygen, peroxynitrite, and hypochlorite. Trolox was used as the reference standard, and the results were expressed as μmole Trolox equivalency per gram of a tested material. Results In both assays, PC-O had higher antioxidant potency than PC. In the Folin-Ciocalteu reaction assay, the cellular antioxidant capacity of PC-O (24 mg/L) was greater than PC (16 mg/L). PC-O also demonstrated consistently higher antioxidant activity in the ORAC 6.0 assay, as follows: peroxyl radicals, PC-O (477 μmole TE/gram) vs. PC (26 μmole TE/gram); hydroxyl radicals, PC-O (734 μmole TE/gram) vs. PC (62 μmole TE/gram); peroxynitrite, PC-O (40 μmole TE/gram) vs. PC (7 μmole TE/gram); super oxide anion, PC-O (172 μmole TE/gram) vs. PC (53 μmole TE/gram); singlet oxygen, PC-O (92 μmole TE/gram) vs. PC (70 μmole TE/gram); and hypochlorite, PC-O (2,805 μmole TE/gram) vs. PC (312 μmole TE/gram). Conclusions These results demonstrate that phycocyanin oligopeptide (PC-O) is a superior antioxidant compared to phycocyanin (PC) as shown by its higher cellular antioxidant capacity in the Folin-Ciocalteu reaction assay and significantly higher ORAC 6.0 scores. Funding Sources This work was supported by Nutrition 21, LLC.

UV-protective Properties of Topical of Astaxanthin Half side Controlled Pilot Study

Background: Astaxanthin, a product of green algae, a naturally occurring reddish pigment from the carotenoid group, is known as a potent antioxidant reducing free radicals. Objective: The aim of this pilot clinical study is to determine whether astaxanthin in topical formulation has antiinflammatory and uv-protective Properties through its antioxidant potency. Material and Methods: The UV-protective effect of Astaxanthin AstaCos® OL50 versus a placebo tested in a half side controlled setting on 21 healthy volunteers Fitzpatrick skin type 2 or 3. A light testing system was used for irradiation of volar aspects of both forearms, one with Astaxanthin formulation, the other with placebo. Twenty four hours later photodocumentation and colormetric measurement of erythema values in all treated areas was performed. Results: After equal uv-exposure, the erythema value after 24 hours on the astaxanthin side is on average 25% lower than on the placebo side. Astaxanthin suppresses visual erythema formation in over 71.42% of cases. Discussion: Uv-exposure causes inflammation, accelerated skin aging and non melanoma skin cancer. Topical Astaxanthin reducing the inflammatory effects of uv-irradiation could prevent later stages of photoaging and malignant skin disease. Zusammenfassung Hintergrund: Astaxanthin, ein Produkt aus Grünalgen, ein natürlich vorkommendes rötliches Pigment aus der Gruppe der Carotinoide, ist als starkes Antioxidans bekannt, das freie Radikale reduziert. Zielsetzung: Das Ziel dieser klinischen Pilotstudie ist es, festzustellen, ob Astaxanthin in topischer Formulierung durch seine antioxidative Potenz uv-protektive Effekte hat. Material und Methoden: Die UV-schützende Wirkung von Astaxanthin AstaCos® OL50 im Vergleich zu einem Placebo wurde in einer halbseitigen kontrollierten Einstellung an 21 gesunden Probanden mit Fitzpatrick-Hauttyp 2 oder 3 getestet. Mit einem Lichttestsystem wurden die volaren Seiten beider Unterarme bestrahlt, einer mit der Astaxanthin-Formulierung, der andere mit Placebo. 24 Stunden später erfolgten Fotodokumentation, farbmetrische Messung der Erythemwerte in allen behandelten Bereichen. Ergebnisse: Nach gleicher uv-Belichtung ist der Erythemwert nach 24 Stunden auf der Astaxanthin-Seite im Durchschnitt 25% niedriger als auf der Placebo-Seite. Astaxanthin unterdrückt die visuelle Erythembildung in über 71,42% der Fälle. Diskussion: Uv-Exposition verursacht Entzündungen, beschleunigte Hautalterung und Nicht-Melanom-Hautkrebs. Die topische Anwendung von Astaxanthin, das die entzündlichen Effekte der UV-Bestrahlung reduziert, könnte spätere Stadien der Lichtalterung und bösartige Hauterkrankungen verhindern.