scholarly journals Usefulness of Urea as a Means of Improving the Solubility of Poorly Water-Soluble Ascorbyl Palmitate

2017 ◽  
Vol 2017 ◽  
pp. 1-9
Author(s):  
Yutaka Inoue ◽  
Daichi Niiyama ◽  
Isamu Murata ◽  
Ikuo Kanamoto

The aim of this study was to evaluate complexes of L-ascorbyl palmitate (ASCP) and urea (UR). This evaluation involved differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), scanning electron microscopy (SEM), near-infrared spectroscopy (NIR), a solubility test, a 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging test, and a mushroom tyrosinase inhibition assay. Physicochemical evaluation revealed that ASCP/UR complexes form at a molar ratio of 1/12. The solubility test revealed that ASCP/UR complexes had increased solubility compared to ASCP. The DPPH radical scavenging test and mushroom tyrosinase inhibition assay revealed that the activity of ASCP/UR complexes was not impaired by complex formation. These results are probably due to the tetragonal crystal system of UR changing to a hexagonal crystal system and interaction with the alkyl group of ASCP.

2015 ◽  
Vol 5 (12) ◽  
pp. 437 ◽  
Author(s):  
Thi Thanh Hanh Nguyen ◽  
Shin-Hye Yu ◽  
Jiyoun Kim ◽  
Eunbae An ◽  
Kyeonghwan Hwang ◽  
...  

Background: Quercetin, a flavonol contained in various vegetables and fruits, has various biological activities including anticancer, antiviral, anti-diabetic, and anti-oxidative. However, it has low oral bioavailability due to insolubility in water. Thus, the bioavailability of quercetin administered to human beings in a capsule form, was reported to be less than 1%, with only a small percentage of ingested quercetin getting absorbed in the blood. This leads to certain difficulties in creating highly effective medicinesMethods: Quercetin-rubusoside and quercetin-rebaudioside were prepared. The antioxidant activities of quercetin and Q-rubusoside were evaluated by DPPH radical scavenging method. Inhibition activities of quercetin and Quercetin-rubusoside were determined by measuring the remaining activity of 3CLpro with 200 μM inhibitor. The inhibition activity of quercetin, rubusoside and quercetin-rubusoside were determined by measuring the activity of human maltase which remains at 100 μM rubusoside or quercetin-rubusoside. The mushroom tyrosinase inhibition was assayed with the reaction mixture contained 3.3 mM L-DOPA in 50 mM potassium phosphate buffer (pH 6.8), and 10 U mushroom tyrosinase/ml with or without quercetin or quercetin-rubusoside. Results: With 10% rubusoside treatment, quercetin showed solubility of 7.7 mg/ml in water, and its solubility increased as the concentration of rubusoside increased; the quercetin solubility in water increased to 0.83 mg/mlas rubusoside concentration increased to 1 mg/ml. Quercetin solubilized in rubusoside solution showed DPPH radical-scavenging activity and mushroom tyrosinase inhibition activity, similar to that of quercetin solubilized in dimethyl-sulfoxide. Quercetin-rubusoside also showed 1.2 and 1.9 folds higher inhibition activity against 3CLpro of SARS and human intestinal maltase, respectively, than those of quercetin in DMSO.Conclusions: Quercetin can be solubilized in water with rebaudioside or rubusoside treatment. As Ru concentration increases, the solubility of quercetin in water increases. The solubilization of quercetin in Ru solution did not reduce its biological functions such as the DPPH radical-scavenging and mushroom tyrosinase activity; also, quercetin-rubusoside increased the inhibition activity against the 3CLpro of SARS and human intestinal maltase, when compared with the activity of quercetin in DMSO. Thus, rubusoside and rebaudioside are promising compounds which enhance the solubility of poorly water soluble compounds.Keywords: rubusoside, rebaudioside, flavonol, quercetin, human maltase, 3CLpro


Antioxidants ◽  
2020 ◽  
Vol 9 (4) ◽  
pp. 278
Author(s):  
Ram Hari Dahal ◽  
Tuan Manh Nguyen ◽  
Dong Seop Shim ◽  
Joon Young Kim ◽  
Jangyul Lee ◽  
...  

Various cosmetics having a single function are increasingly being used, but cosmetics having multifunctional activities remain limited. We aimed to develop a multifunctional cosmetic cream having antioxidant, anti-tyrosinase, anti-aging and antimicrobial activities. Antimicrobial activities were performed by disc-diffusion method. Cell toxicity and cell proliferations were evaluated in a 96-well plate with different cell lines such as HaCaT, RAW264.7, CCD-986Sk, B16F1, and B16F10. Mushroom tyrosinase inhibition, elastase inhibition, and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activities were evaluated and IC50 was calculated. Mesoporous silica particle was synthesized using Pluronic P123 and tetraethyl ortho-silicate (TEOS). Facial pictures were captured by VISIA-CR (Facial Imaging System for Clinical Research). Roughness of image was analysed by PRIMOS software and brightness of image was analyzed by Chromameter CR-400. The crude product of strain T65 inhibited the different human pathogenic bacteria such as Bacillus subtilis, Escherichia coli, Propionibacterium acnes, Staphylococcus aureus, Pseudomonas aeruginosa, and Staphylococcus epidermidis. The IC50 of T65 crude product for mushroom tyrosinase, elastase, and DPPH radical scavenging activities were 58.73, 14.68, and 6.31 µg/mL, respectively. T65 crude product proliferated collagen type I in CCD-986Sk cell up to 145.91% ± 9.11% (mean ± SD; mean of 24, 48, and 72 h) at 250 pg/mL. Synthesized mesoporous particles (SBA-15) confirmed the sustainable performance by control-release for three days. Formulated functional cosmetic cream containing T65 embedded SBA-15, significantly decreased the skin roughness by 4.670% and increased the skin brightness by 0.472% after application of 4 weeks. T65 crude product inhibited both Gram-positive and Gram-negative pathogens. Synthesized mesoporous particle, SBA-15, confirmed the physiologically active substance was released in sustainable release condition. T65 crude product showed impeccable antimicrobial, antioxidant, anti-aging, and whitening activities with non-cytotoxic effects to different cell lines related to the human skin.


2021 ◽  
Vol 15 (4) ◽  
pp. 254-260
Author(s):  
Penghua Shu ◽  
Yamin Li ◽  
Yuehui Luo ◽  
Shujing Cai ◽  
Yingying Fei ◽  
...  

A phytochemical study on the flowers of Cercis glabra ‘Spring-1’ led to the isolation and identification of twelve compounds, including one new compound named as 1-O-α-l-rhamnosyl-(E)-phytol (1) and eleven known compounds. Their structures were elucidated based on physical data analysis, including HR-ESI-MS, NMR, UV, IR, and acid hydrolysis. All compounds were screened for in vitro antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl method. Compounds 4 and 5 exhibited obvious DPPH radical scavenging activities. All the isolates were tested for their inhibitory effects on mushroom tyrosinase, and compounds 6, 7, 10 and 11 showed moderate tyrosinase inhibitory activities.


2017 ◽  
Vol 6 (3) ◽  
pp. 171-173
Author(s):  
Navya Gurram ◽  
◽  
Manish Kamble ◽  
Mahendra Gunde ◽  
Ashwini Ingole ◽  
...  

Terminalia catappa Linn. also known as Indian almond or tropical almond is a native throughout the tropical Asia belongs to family Combretaceae. Traditionally, the parts of this plant of are used for the treatment of dermatitis, hepatitis, diarrhea and pyresis, caribbeans used the decoction for gastritis and urinary tract infection. The present study aimed to evaluate the pharmacognostic and phytochemical properties along with the antioxidant activity of Teminalia catappa Linn. The fresh fruits of Teminalia catappa were collected and preliminary microscopic screening was done by evaluating the transverse section. The phytochemical screening of the fruit revealed the presence of flavonoids, tannins, saponins, and alkaloids. The phycochemical analysis also showed the total ash content 7.913% and was slightly higher than acid insoluble and water soluble ash. The fruit flesh was subjected to hydroalcoholic extraction to obtain a semisolid extract. The antioxidant activity was carried out by using DPPH radical scavenging assay spectrophotometrically at 517nm. The various concentration of fruit flesh extract (62.5, 125, 250, 500, 1000 ug/ml) were used and increasing antioxidant activity was observed with increasing concentration. About 41% scavenging activity for DPPH radical was observed at 1000 ug/ml.


Food Research ◽  
2021 ◽  
Vol 5 (S1) ◽  
pp. 65-72
Author(s):  
D.L. Abd. Razak ◽  
N.Y. Abd. Rashid ◽  
A. Jamaluddin ◽  
A. Abd Ghani ◽  
M. Abdul Manan

Solid state fermentation (SSF) utilizing filamentous fungus Amylomyces rouxii was investigated as a bio-processing strategy to enhance the bioactive properties of broken rice. Fermentation was carried out for 18 days and samples were withdrawn at 2-days interval. Established methods were deployed to assess the changes in bioactive properties and compounds content in fermented broken rice. The bioactive properties studied were total phenolic content (TPC), total flavonoid content (TFC), DPPH-radical scavenging activity and ferric-reducing antioxidant power (FRAP). Additionally, tyrosinase inhibition activity, which represents anti-pigmentation/browning property, was evaluated. Free phenolic acids and organic acids content were determined through high performance liquid chromatography (HPLC). The results showed that fermentation significantly increased the total phenolic content of broken rice from 0.03 mg GAE/g sample to 3.94 mg GAE/g sample and total flavonoid content from 0.04 to 1.71 mg QE/g sample. By the end of the fermentation, DPPH-radical scavenging of fermented broken rice was enhanced to 94.22%, compared to 9.03% in the unfermented sample. It was also observed that FRAP and tyrosinase inhibition activity of fermented broken rice were improved up to 39- fold and 50-fold, respectively. Kojic acid, a potent antioxidant and tyrosinase inhibitor, was detected in fermented broken rice, along with oxalic and ascorbic acid. Gallic, protocatechuic and 4-hydroxybenzoic acids were enhanced upon fermentation. This study manifested the positive effect of broken rice after fermentation with A. rouxii and thus revealed the potential of fermented broken rice as a promising natural bio-ingredients in food, cosmetics and medicinal products.


Author(s):  
Soo Hyeon Heo, Su In Park, Jinseo Lee, Sung Won Jung,Moon Sam Shin

To find out a good candidate of cosmetic source and screened for antimicrobial, antioxidant and whitening activities. In the antioxidant experiment, supercritical Halopteris scoparia extraction (SHE) and hydrothermal Halopteris scoparia extraction (HHE) were slightly different depending on the experimental method (Total polyphenol content measurement, DPPH radical scavenging ability, ABTS radical scavenging ability, and SOD-like activity) and in the enzyme experiment (Elastase, Tyrosinase inhibition activity), the supercritical extract was more effective. In supercritical fluid, Halopteris scoparia extracts showed good antimicrobial activity against Propionibacterium acnes, Staphylococcus aureus, Bacillus subtilis and Escherichia coli but hydrothermal extract had no effect about the rest of the strains. Therefore, it can be expected that the supercritical Halopteris scoparia extract with excellent antibacterial activity can be used as a cosmetic material.


2018 ◽  
Vol 44 (4) ◽  
pp. 515-520
Author(s):  
M Kazemi

Carum copticum L. comprises several relevant species for food, cosmetic, perfumery and pharmaceutical industries. GC/MS analysis of the enential oil of C. copticum revealed γ- terpinene as a major component of C. copticum, with its contribution of 33.85%. Essential oils (EOs) exhibited a significant antimicrobial activity against all tested microbial strains. In addition, the C. copticum oil demonstrated the highest DPPH radical scavenging activity. These results clearly show the antimicrobial and antioxidant effects of the plant essential oil.


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