scholarly journals Encapsulation of α-Pinene in Delivery Systems Based on Liposomes and Cyclodextrins

Molecules ◽  
2021 ◽  
Vol 26 (22) ◽  
pp. 6840
Author(s):  
Zahraa Hammoud ◽  
Maya Kayouka ◽  
Adriana Trifan ◽  
Elwira Sieniawska ◽  
Jouda Mediouni Ben Jemâa ◽  
...  

The essential oil component α-pinene has multiple biological activities. However, its application is limited owing to its volatility, low aqueous solubility, and chemical instability. For the aim of improving its physicochemical properties, α-pinene was encapsulated in conventional liposomes (CLs) and drug-in-cyclodextrin-in-liposomes (DCLs). Hydroxypropyl-β-cyclodextrin/α-pinene (HP-β-CD/α-pinene) inclusion complexes were prepared in aqueous solution, and the optimal solubilization of α-pinene occurred at HP-β-CD:α-pinene molar ratio of 7.5:1. The ethanol-injection method was applied to produce different formulations using saturated (Phospholipon 90H) or unsaturated (Lipoid S100) phospholipids in combination with cholesterol. The size, the phospholipid and cholesterol incorporation rates, the encapsulation efficiency (EE), and the loading rate (LR) of α-pinene were determined, and the storage stability of liposomes was assessed. The results showed that α-pinene was efficiently entrapped in CLs and DCLs with high EE values. Moreover, Lipoid S100 CLs displayed the highest LR (22.9 ± 2.2%) of α-pinene compared to the other formulations. Both carrier systems HP-β-CD/α-pinene inclusion complex and Lipoid S100 CLs presented a gradual release of α-pinene. Furthermore, the DPPH radical scavenging activity of α-pinene was maintained upon encapsulation in Lipoid S100 CLs. Finally, it was found that all formulations were stable after three months of storage at 4 °C.

2019 ◽  
Vol 14 (6) ◽  
pp. 1934578X1986125
Author(s):  
Ahmed Gomaa Gomaa Darwish ◽  
Mamdouh Nabil Samy ◽  
Sachiko Sugimoto ◽  
Hideaki Otsuka ◽  
Katsuyoshi Matsunami

One new macrolide, racemolide (1), was isolated from an MeOH extract of the leaves of Lumnitzera racemosa with 7 known compounds (2-8) by various chromatographic techniques via silica gel, octadecylsilyl column chromatography and high-performance liquid chromatography. The structure of the new compound was determined through a combination of spectroscopic and chemical analyses. The isolated compounds were evaluated for their antileishmanial, hepatoprotective, and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities. Compound 1 showed potent antileishmanial activity at inhibition % value of 67.6 ± 1.24% compared with the clinical drug miltefosine (93.3 ± 4.39%). Compounds 1 and 5 possessed moderate hepatoprotective activity against acetaminophen (APAP)-induced hepatotoxicity using human HepG2 cells at protection % value of 21.70 ± 1.97% and 27.5 ± 1.41%, respectively, compared with the standard glycyrrhizin (69.50 ± 3.53%). Compounds 4, 6, 7, and 8 had high DPPH radical scavenging activity (91.10 ± 4.25, 91.53 ± 0.05, 91.91 ± 0.09, and 86.48 ± 2.87%, respectively), while compounds 3 and 5 showed moderate (45.38 ± 3.62% and 62.20 ± 1.47%, respectively), comparable with the standard trolox (89.21 ± 5.88%). These results suggest that the new compound, racemolide (1), and known compounds (3-8) are valuable as promising antileishmanial, hepatoprotective, and anti-oxidant agents.


Author(s):  
Suwon Oh ◽  
Sungkeun Kim ◽  
Kyoojin Jung ◽  
Thi Ngoc Anh Pham ◽  
Seungwhan Yang ◽  
...  

Polysaccharides from marine algae exhibit beneficial biological activities. In this study, we examined the effect of polysaccharides from Codium fragile (PCF) on prebiotic and anti-obesity activity. PCF increases the growth of specific beneficial microbial populations with concomitant decrease in pathogenic microbes. Further, total phenolic content (TPC), total flavonoid content (TFC), and DPPH radical scavenging activity (DPPH activity) after fermentation with PCF as carbon source were higher than for the glucose as control. Moreover, PCF inhibited adipocyte differentiation by inducing differentiation-related factors when the induction of 3T3-L1 preadipocytes into adipocytes was induced. Therefore, we suggest that PCF can be used as prebiotic material with anti-obesity for human health.


Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 746
Author(s):  
Claudia Valverde Malaver ◽  
Ana Colmenares Dulcey ◽  
Carlos Rial ◽  
Rosa Varela ◽  
José Molinillo ◽  
...  

A bio-guided study of leaf extracts allowed the isolation of two new macrobicyclic hydrolysable tannins, namely merianin A (1) and merianin B (2), and oct-1-en-3-yl β-xylopyranosyl-(1”-6’)-β-glucopyranoside (3) from Meriania hernandoi, in addition to 11 known compounds reported for the first time in the Meriania genus. The structures were elucidated by spectroscopic analyses including one- and two-dimensional NMR techniques and mass spectrometry. The bioactivities of the compounds were determined by measuring the DPPH radical scavenging activity and by carrying out antioxidant power assays (FRAP), etiolated wheat coleoptile assays and phytotoxicity assays on the standard target species Lycopersicum esculentum W. (tomato). Compounds 1 and 2 exhibited the best free radical scavenging activities, with FRS50 values of 2.0 and 1.9 µM, respectively.


Marine Drugs ◽  
2020 ◽  
Vol 18 (11) ◽  
pp. 574
Author(s):  
Chien Thang Doan ◽  
Thi Ngoc Tran ◽  
Van Bon Nguyen ◽  
Anh Dzung Nguyen ◽  
San-Lang Wang

Microbial fermentation of by-products is a renewable and efficient technique in the development of a range of useful products. In this study, protease synthesis by Paenibacillus sp. TKU052 was carried out on culture media containing some common seafood processing by-products (SPBPs) as the sole source of carbon and nitrogen (C/N). The most suitable C/N nutrition source for the production of proteases was found to be 3.0% (w/v) demineralized crab shells powder (deCSP) and maximal enzyme activity of 4.41 ± 0.16 U/mL was detected on the third day of the culture. Two proteases (P1 and P2) with a similar molecular weight of 31 kDa were successfully isolated and purified from the 3-day deCSP-containing medium. Both P1 and P2 exhibited the highest activity of gelatin hydrolysis at pH 6 and 60 °C. The gelatin hydrolysates catalyzed by Paenibacillus TKU052 proteases were evaluated for biological activities, including 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, angiotensin-I converting enzyme (ACE) inhibition, and prebiotic activities. The gelatin hydrolysates expressed 31.76–43.95% DPPH radical scavenging activity and 31.58–36.84% ACE inhibitory activity, which was higher than those from gelatin. Gelatin hydrolysates also showed the growth-enhancing effect on Bifidobacterium bifidum BCRC 14615 with an increase to 135.70–147.81%. In short, Paenibacillus sp. TKU052 could be a potential strain to utilize crab shell wastes to produce proteases for bio-active peptides’ preparation.


2014 ◽  
Vol 79 (5) ◽  
pp. 517-526
Author(s):  
Maya Chochkova ◽  
Assya Georgieva ◽  
Galya Ivanova ◽  
Nadya Nikolova ◽  
Luchia Mukova ◽  
...  

Seven N-hydroxycinnamoyl amides were synthesized by EDC/HOBt coupling of the corresponding substituted cinnamic acids (p-coumaric-, ferulic-, sinapic- and caffeic acids) with influenza antivirals (amantadine, rimantadine and oseltamivir). DPPH (1,1-diphenyl-2-picrylhydrazyl) scavenging abilities and the inhibitory effect on mushroom tyrosinase activity (using L-tyrosine as the substrate) were investigated in vitro. Amongst the synthesized compounds, N-[(E)-3-(3?,4?-dihydroxyphenyl)-2-propenoyl]oseltamivir (1) and N-[(E)-3-(3?,4?-dihydroxyphenyl)-2-propenoyl]rimantadine (4), containing catechol moiety, exhibited the most potent DPPH radical-scavenging activity. Amide (1) displayed also tyrosinase inhibitory effect toward L-tyrosine as the substrate (~50%). Due to its biological activities revealed so far compound (1) can be considered as a promising candidate for a cosmetic ingredient. The synthesized compounds were also investigated for their in vitro inhibitory activity against the replication of influenza virus A (H3N2).


Author(s):  
Amina Khatun ◽  
Mahmudur Rahman ◽  
Mohammad Sharifur Rahman ◽  
Md. Khalid Hossain ◽  
Mohammad Abdur Rashid

AbstractBackgroundCommelina benghalensis Linn. (Family: Commelinaceae) is a common weed available in Bangladesh with several uses in traditional medicine. However, the chemical profile of this medicinal plant is scarce in relation to its medicinal uses. The aerial parts of this plant have been investigated for the isolation of secondary metabolites and evaluation of the biological activities.MethodsMajor phytochemical groups were analyzed using chromogenic reagents, whereas n-hexane soluble fractionates of the methanol extract were subjected to 1H nuclear magnetic resonance (NMR) spectroscopic analysis. The antioxidant property of the obtained compounds was evaluated using 1,1-diphenyl-2-picryl-hydrazyl (DPPH).ResultsDammara-12-en-3-one (CB-1), stigmasterol (CB-2) and 3 (2,3,4,5,6-pentahydroxy)-cinnamoyl dammara-12-ene (CB-3) were isolated from the n-hexane fractionate of methanol extract of C. benghalensis. In the study of DPPH radical scavenging activity, IC50 values were predicted to be 790.18, 4186.94 and 2001.16 μg/mL for CB-1, CB-2 and CB-3, respectively, whereas standard ascorbic acid showed IC50 at 1.26 μg/mL.ConclusionsTwo new dammarane-type triterpene (CB-1 and CB-3) and one phytosterol (CB-2) were identified in C. benghalensis with mild antioxidant property.


2016 ◽  
Vol 12 ◽  
pp. 29-42 ◽  
Author(s):  
Miriana Kfoury ◽  
David Landy ◽  
Steven Ruellan ◽  
Lizette Auezova ◽  
Hélène Greige-Gerges ◽  
...  

Carvacrol and thymol have been widely studied for their ability to control food spoilage and to extend shelf-life of food products due to their antimicrobial and antioxidant activities. However, they suffer from poor aqueous solubility and pronounced flavoring ability that limit their application in food systems. These drawbacks could be surpassed by encapsulation in cyclodextrins (CDs). Applications of their inclusion complexes with CDs were reported without investigating the inclusion phenomenon in deep. In this study, inclusion complexes were characterized in terms of formation constants (K f), complexation efficiency (CE), CD:guest molar ratio and increase in bulk formulation by using an UV–visible competitive method, phase solubility studies as well as 1H and DOSY 1H NMR titration experiments. For the first time, a new algorithmic treatment that combines the chemical shifts and diffusion coefficients variations for all guest protons was applied to calculate K f. The position of the hydroxy group in carvacrol and thymol did not affect the stoichiometry of the inclusion complexes but led to a different binding stability with CDs. 2D ROESY NMR experiments were also performed to prove the encapsulation and illustrate the stable 3D conformation of the inclusion complexes. The structural investigation was accomplished with molecular modeling studies. Finally, the radical scavenging activity of carvacrol and thymol was evaluated by the ABTS radical scavenging assay. An improvement of this activity was observed upon encapsulation. Taken together, these results evidence that the encapsulation in CDs could be valuable for applications of carvacrol and thymol in food.


2019 ◽  
Vol 31 (12) ◽  
pp. 2903-2908
Author(s):  
G. Usha Rani ◽  
B. Kesava Rao ◽  
P. Asha Bhanu ◽  
G. Swapna

The facile green synthesis of silver nanoparticles is finding an imperative use in different fields due to their potential applications. The present study is focused on the green synthesis of silver nanoparticles from Coldenia procumbens Linn., in an eco-friendly way in order to reduce the toxicity from chemical methods. The zeta potential, size of the silver nanoparticles was measured and the characterization was done from UV-visible spectroscopy, Fourier transform infrared spectroscopy, X-ray diffraction and scanning electron microscopy. The disc diffusion method has used to evaluate the antimicrobial efficacy of synthesized nanoparticles with different bacterial pathogens and the antioxidant capability of silver nanoparticles was tested and has shown significant DPPH radical scavenging activity.


2018 ◽  
Vol 13 (9) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Hawraz Ibrahim M. Amin ◽  
Faiq H. S. Hussain ◽  
Marcello Maggiolini ◽  
Giovanni Vidari

In the first phytochemical investigation of non-volatile secondary metabolites from the Kurdish traditional plant Iris persica L, (-)-embinin was isolated from flowers and leaves, isovitexin from flowers, trans-resveratrol-3- O-β-D-glucopyranoside from rhizomes and tectorigenin from bulbs. The complete NMR spectra of embinin are reported for the first time. In an MTT assay, embinin showed an inhibition activity higher than the well-known antitumor drug cisplatin against five of the six tested human tumor cells. Moreover, embinin showed a significant DPPH radical scavenging activity (IC50 value of 112.16) comparable to the reference antioxidant ascorbic acid. The remarkable biological activities exhibited by the extracts of Iris persica and isolated compounds have validated the uses of I. persica in the traditional medicine of Kurdistan.


2021 ◽  
Author(s):  
Neelofar Majid ◽  
Saduf Nissar ◽  
Weekar Younus Raja ◽  
Irshad A. Nawchoo ◽  
Zulfikar Ali Bhat ◽  
...  

Abstract Background: Aralia cachemirica Decne. is an important medicinal plant species of Kashmir Himalaya. Regardless of having enormous medicinal importance little information exists on the biological activities of the species. For this reason, present work was carried out for providing comprehensive details on the antioxidant and anti-inflammatory activities of different parts of A. cachemirica.Methods: In this connection, different parts (leaves, stem and root) of the plant were examined following standard methodologies. Antioxidant potential of the plant was determined by three different standard methodologies viz. DPPH radical scavenging activity, reducing power activity and metal chelating activity. For anti-inflammatory activities two different standard methods viz. human RBC membrane stabilization method and protein denaturation method were followed.Results: The extracts exhibited concentration dependent antioxidant and anti-inflammatory activities but were weaker than the standards. Also, the highest activities were recorded in the root and least in the leaves. Also, the highest activities were recorded in the leaves and least in the stem.Conclusion: This is the first study providing information regarding antioxidant and anti-inflammatory potential of different parts of the species. The antioxidant activity of the extract could have great importance as therapeutic agents in preventing or slowing the progress of aging and age associated, oxidative stress related degenerative diseases. Plant derived anti-inflammatory agents are competent cure for inflammation caused by a range of agents, which shows the way to their soaring requirement. Exploitation of these agents requires to be regulated in order, to be sustainable and keep up with demands.


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