scholarly journals In Vitro Antioxidant, Anti-Inflammatory and Skin Permeation of Myrsine africana and Its Isolated Compound Myrsinoside B

2020 ◽  
Vol 10 ◽  
Author(s):  
Bianca Fibrich ◽  
Xinyi Gao ◽  
Ashana Puri ◽  
Ajay K. Banga ◽  
Namrita Lall
2014 ◽  
Vol 902 ◽  
pp. 70-75 ◽  
Author(s):  
Aroonsri Priprem ◽  
Vassana Netweera ◽  
Pramote Mahakunakorn ◽  
Nutjaree Pratheepawanit Johns ◽  
Jeffrey Roy Johns

Melatonin, encapsulated and non-encapsulated, in a topical gel, was comparatively investigated for its in vitro permeation and in vivo anti-inflammatory properties. An average size of the melatonin-encapsulated niosomes of 197 nm with a zeta potential of-78.8 mV and an entrapment efficiency of 92.7% was incorporated into a gel base. In vitro skin permeation of the same gel base incorporated with non-encapsulated melatonin or melatonin niosomes at 5% was comparatively evaluated through porcine skin using Franz diffusion cells and analyzed by spectroflurometry at λex 278 and λem 348 nm. From the same gel base, the permeation rate of non-encapsulated melatonin was about 2.5 times greater than that of melatonin-encapsulated niosomes. In comparison to piroxicam gel and hydrocortisone cream used as the positive controls, topical applications of melatonin and melatonin niosome gels tested in croton oil-induced ear edema in mice suggested that its anti-inflammatory activities were prolonged by the niosomal encapsulation. Similarly, analgesic effect of melatonin was prolonged by niosomal encapsulation using tail flick test in mice. Therefore, its immediate permeation through the skin was retarded by niosomal encapsulation which could also prolong its rapid decline in exerting anti-inflammatory and analgesic activities in vivo.


2020 ◽  
Vol 10 (4) ◽  
pp. 395-399
Author(s):  
Ajay M. Chowdari ◽  
D. Giles

Background: Ziziphus jujuba mill was commonly used for its anti-inflammatory activity in traditional system of medicine. Objective: The purpose of this study was to examine the isolates of methanolic extract from the fruits of Ziziphus jujuba Mill for its antiulcer, anti-inflammatory, and anticancer activity. Methods: Methanolic extracts of Ziziphus jujuba Mill were subjected to chromatography and eluted using ethyl acetate: methanol mixture and investigated for its structural features using IR, 1H NMR, 13C NMR and mass spectral data. The isolated compound was evaluated for its in vitro COX-2 inhibition studies, cytotoxicity studies, in vivo anti-inflammatory, antiulcer and anticancer activity. Results: The spectral data revealed that the backbone of the isolate was 3-O-α-L-rhamnopyranosyl- (1→6)-β-D-glucopyranosyl jujubogenin-20-O-(2,3,4-O-triacetyl)-α-L-rhamnopyranoside. The isolated compound showed a significant reduction in inflammation and edema. Moderate anticancer activity was also observed for the isolate. Conclusion: It was concluded that the isolated saponin possesses moderate antiulcer, antiinflammatory, and anticancer activity which could help in the identification of leads for the treatment of cancer-related inflammation.


2008 ◽  
Vol 63 (7-8) ◽  
pp. 533-538 ◽  
Author(s):  
Nilton S. Arakawa ◽  
Karin Schorr ◽  
Sérgio R. Ambrósio ◽  
Irmgard Merfort ◽  
Fernando B. Da Costa

In addition to known heliangolides, a new eudesmanolide was isolated from the leaf rinse extract of Viguiera robusta (Asteraceae). Structural elucidation was based on spectral analysis. It is the first report on eudesmanolides in members of the subgenus Calanticaria of Viguiera. In this work, the main isolated compound, the furanoheliangolide budlein A, besides its previously reported in vitro and in vivo anti-inflammatory activities, inhibited human neutrophil elastase release. The inhibition was at the concentration of (16.83± 1.96) μm for formylated bacterial tripeptide (fMLP) stimulation and (11.84±1.62) μm for platelet aggregation factor (PAF) stimulation, being slightly less active than the reference drug parthenolide. The results are important to demonstrate the potential anti-inflammatory activities of sesquiterpene lactones and corroborate the previous studies using other targets.


Polymers ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 577 ◽  
Author(s):  
Wafaa E. Soliman ◽  
Tamer M. Shehata ◽  
Maged E. Mohamed ◽  
Nancy S. Younis ◽  
Heba S. Elsewedy

Background: Curcumin (Cur) possesses a variety of beneficial pharmacological properties including antioxidant, antimicrobial, anti-cancer and anti-inflammatory activities. Nevertheless, the low aqueous solubility and subsequent poor bioavailability greatly limits its effectiveness. Besides, the role of myrrh oil as an essential oil in treating inflammatory disorders has been recently demonstrated. The objective of the current investigation is to enhance Cur efficacy via developing Cur nanoemulgel, which helps to improve its solubility and permeability, for transdermal delivery. Methods: The formulated preparations (Cur gel, emulgel and nanoemulgel) were evaluated for their physical appearance, spreadability, viscosity, particle size, in vitro release and ex vivo drug permeation studies. The in vivo anti-inflammatory activity was estimated using the carrageenan-induced rat hind paw edema method. Results: The formulated Cur-loaded preparations exhibited good physical characteristics that were in the acceptable range of transdermal preparations. The release of Cur from gel, emulgel and nanoemulgel after 12 h was 72.17 ± 3.76, 51.93 ± 3.81 and 62.0 ± 3.9%, respectively. Skin permeation of Cur was significantly (p < 0.05) improved when formulated into nanoemulgel since it showed the best steady state transdermal flux (SSTF) value (108.6 ± 3.8 µg/cm2·h) with the highest enhancement ratio (ER) (7.1 ± 0.2). In vivo anti-inflammatory studies proved that Cur-loaded nanoemulgel displayed the lowest percent of swelling (26.6% after 12 h). Conclusions: The obtained data confirmed the potential of the nanoemulgel dosage form and established the synergism of myrrh oil and Cur as an advanced anti-inflammatory drug.


Author(s):  
SEHAM M. SHAWKY ◽  
MAHA K. A. KHALIFA ◽  
HEBA A. EASSA

Objective: To design a controlled topical delivery system of lornoxicam (LX) in order to enhance skin permeation and treatment efficacy. Nanosponges were selected as a novel carrier for this purpose. Methods: Nanosponges were formulated via the emulsion solvent evaporation method using ethyl cellulose (polymer) and polyvinyl alcohol (surfactant). Nanosponge dispersions were characterized for colloidal properties, entrapment efficiency and in vitro release study. The nanosponge formulation (LS1) was then incorporated into carboxymethyl cellulose sodium hydrogels and evaluated for pH, viscosity and in vitro drug release. Skin irritation was evaluated, and anti-inflammatory activity was assessed via rat hind paw edema method. Results: Nanosponges were in the nano-sized range and attained a uniform round shape with a spongy structure. LS1exhibited the highest LX release after 6 h, so it was incorporated as hydrogel. Formulated hydrogels showed acceptable physicochemical parameters (pH, drug content and rheological properties). Skin irritation testing proved LX-loaded nanosponge hydrogel formulation (G1) to be non-irritant. In vivo study revealed an enhanced anti-inflammatory activity of G1 for 6 h (p<0.001). Conclusion: The developed nanosponge hydrogel is an efficient nanocarrier for improved and controlled topical delivery of LX.


2014 ◽  
Vol 50 (4) ◽  
pp. 885-893 ◽  
Author(s):  
Gisele Mara Silva Gonçalves ◽  
Gustavo Henrique da Silva ◽  
Pedro Paulo Barros ◽  
Silvana Mariana Srebernich ◽  
Cecilia Toyoko Cavalcanti Shiraishi ◽  
...  

Curcuma longais a ginger family aromatic herb (Zingiberaceae) whose rhizomes contain curcuminoid pigments, including curcumin, a compound known for its anti-inflammatory effects. The objective of this study was to obtain curcuminoid-rich extracts, develop topical formulations thereof, and assess the stability and skin permeation of these formulations. Curcuma longa extracts were obtained and used to develop formulations. Skin permeation studies were conducted in a modified Franz diffusion cell system, and skin retention of curcuminoid pigments was quantified in pig ear membrane. Prepared urea-containing gel-cream formulations were unstable, whereas all others had satisfactory stability and pseudoplastic rheological behavior. The amount of curcuminoid pigments recovered from the receptor solution was negligible. The skin concentration of curcuminoid pigments retained was positive (>20 µg/g of skin, mostly in the stratum corneum), considering the low skin permeability of curcumin. We conclude that development of topical formulations containing curcumin or Curcuma longaextract is feasible, as long as adjuvants are added to improve preservation and durability. The formulations developed in this study enabled penetration of curcumin limited to the superficial layers of the skin and then possibly without a risk of systemic action, thus permitting local use as a topical anti-inflammatory.


2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Ujwala A. Shinde ◽  
Shivkumar S. Kanojiya

The objective of present study was to develop nonionic surfactant vesicles of proteolytic enzyme serratiopeptidase (SRP) by adapting reverse phase evaporation (REV) technique and to evaluate the viability of SRP niosomal gel in treating the topical inflammation. The feasibility of SRP niosomes by REV method using Span 40 and cholesterol has been successfully demonstrated in this investigation. The entrapment efficiency was found to be influenced by the molar ratio of Span 40 : cholesterol and concentration of SRP in noisome. The developed niosomes were characterized for morphology, particle size, and in vitro release. Niosomal gel was prepared by dispersing xanthan gum into optimized batch of SRP niosomes. Ex vivo permeation and in vivo anti-inflammatory efficacy of gel formulation were evaluated topically. SRP niosomes obtained were round in nanosize range. At Span 40 : cholesterol molar ratio 1 : 1 entrapment efficiency was maximum, that is, 54.82% ± 2.08, and showed consistent release pattern. Furthermore ex vivo skin permeation revealed that there was fourfold increase in a steady state flux when SRP was formulated in niosomes and a significant increase in the permeation of SRP, from SRP niosomal gel containing permeation enhancer. In vivo efficacy studies indicated that SRP niosomal gel had a comparable topical anti-inflammatory activity to that of dicolfenac gel.


Author(s):  
Yahaya Najib Sani ◽  
Mainul Haque ◽  
Amirah Wan- Azemin ◽  
Khamsah Suryati ◽  
Anam Khan

Objective: This study investigated the activity of the extracts and the isolated compound on its potential in vitro antidiabetic, anti-inflammatory and potential anti-cancer effect, total flavonoid content against alpha-glucosidase enzyme inhibition and on macrophage respectively from Andrographispaniculata (Burm. F) wall. Ex Nees. Methodology: The isolation of the constituents was done using column while the in vitro anti-inflammatory and antidiabetic was done using nitric oxide and α-glucosidase enzyme inhibition assay while anticancer assessment was done performed using cell viability on various human hepatocellular carcinoma cell) and Chang liver (normal cell line) were determined by 3-(4,5-dimethylthiazolzyl-2yl)-2,5-diphenyl-tetrazolium bromide (MTT) assay. Results: Although, the total flavonoid content was low, ethyl acetate extract indicated the highest total flavonoids content and it’s statistically different from methanol, ethanol: water (1:1 v/v) and aqueous extracts. Ethyl acetate extracts exhibited the highest percentage inhibition (29.8 %) against nitric oxide scavenging activity (NaNO2) compared to other extracts. Also, the isolated crystals showed a significant inhibition against NaNO2. Moreover, the ethyl acetate extract showed the highest percentage inhibition of α-glucosidase enzyme with optimal concentration of 950μg/ml for 50 % inhibition (IC50) while the other three extracts (methanol, 50 % ethanol: water (1:1 v/v) and aqueous) indicated activity below 50 % inhibition which might be due to total flavonoid content. The potential anti-cancer effect indicates that both the methanol extract and crystals (AP02 and AP03) may have the same compound. Conclusion: The compound isolated might be Andrographolide and the activity might be due to flavonoid content for the extract.


2021 ◽  
Vol 18 ◽  
Author(s):  
Anuraag Muralidharan ◽  
Tenzin Tender ◽  
Pallavi K Shetty ◽  
Srinivas Mutalik ◽  
Krishna Sharma K ◽  
...  

Background: Inflammation has become the culmination point for several chronic diseases like skin diseases, asthma, neurological disorders, cancer and cardiovascular disorders. Mini αA-crystallin peptide, identified from a highly conserved region of human lens protein αA-crystallin, is known to have a chaperone-like function, hence has generated interest in exploring the anti-inflammatory potential of the peptide. Objective: The objective of the study was to evaluate anti-inflammatory potential of mini αA chaperone using in vitro, ex-vivo and in vivo models. Methods: The peptide was tested for its phosphodiestarase4 B inhibition, anti-inflammatory and free radical scavenging abilities in HaCat cells. Carbopol gel formulations with varying concentrations of mini αA-crystallin peptide and diclofenac sodium were prepared and optimized. Skin permeation studies of prepared formulations were carried out on excised abdominal skin of Wistar rat using a vertical type diffusion cell. Carrageenan induced rat paw oedema model was used for determining the anti-inflammatory potential of the peptide in prepared gel formulation with or without diclofenac sodium. Results: The peptide exhibited appreciable free radical scavenging and weak PDE4B inhibition. Gel formulation with 1% Tween-80, 1% carbopol and 10% ethanol showed better permeation compared to other formulations. The in vitro skin permeation studies revealed good improvement in permeation characteristics of diclofenac and peptide from the gels. The peptide was retained within the skin tissue, which is an ideal requirement for the delivery of anti-inflammatory topical formulation. In preclinical anti-inflammatory studies, gel formulation containing mini αA-peptide and diclofenac sodium showed a significant decrease in paw volume compared to other combinations tested. Conclusion: The study revealed the additive effect in anti-inflammatory activity by combining mini-αA peptide and diclofenac sodium which effectively reduced the inflammation.


2020 ◽  
Vol 16 ◽  
Author(s):  
Reyaz Hassan Mir ◽  
Gifty Sawhney ◽  
Rohini Verma ◽  
Bilal Ahmad ◽  
Parveen Kumar ◽  
...  

Background: Inflammation involves a dynamic network that is highly regulated by signals that initiate the inflammation process as well as signals that downregulate it. However, an imbalance between the two leads to tissue damage. Throughout the world, inflammatory disease becomes common in the aging society. The drugs which are used clinically suffer serious side effects. Natural products or compounds derived from natural products show diversity in structure and play an important role in drug discovery and development. Objective: Oreganum Vulgare is used in traditional medicine for various ailments including respiratory and rheumatic disorders, severe cold, suppression of tumors. The current study aims to evaluate the anti-inflammatory potential by evaluating various in-vitro parameters. Results: The extracts (OVEE, OVEAF) as well as the isolated compound(OVRA)of Oreganum Vulgare inhibit the proinflammatory cytokines (IL-6 and TNF-α) and NO without affecting cell viability. Conclusion: Our study established that the leaf extracts of Oreganum Vulgare exhibits anti-inflammatory activity and thus confirm its importance in traditional medicine.


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