scholarly journals Hibiscus sabdariffa anthocyanins-rich extract: Chemical stability, in vitro antioxidant and antiproliferative activities

2018 ◽  
Vol 113 ◽  
pp. 187-197 ◽  
Author(s):  
Laércio Galvão Maciel ◽  
Mariana Araújo Vieira do Carmo ◽  
Luciana Azevedo ◽  
Heitor Daguer ◽  
Luciano Molognoni ◽  
...  
Keyword(s):  
Chemical Stability ◽  
Hibiscus Sabdariffa ◽  
Antiproliferative Activities

1'-methylspiro[indoline-3,4'-piperidine] Derivatives: Design, Synthesis, Molecular Docking and Anti-tumor Activity Studies

2020 ◽  
Vol 17 ◽  
Author(s):  
Junjian Li ◽  
Lianbao Ye ◽  
Yuanyuan Wang ◽  
Ying Liu ◽  
Xiaobao Jin ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Cell Lines ◽  
Active Sites ◽  
Biological Activities ◽  
Significant Inhibition ◽  
Alkaline Condition ◽  
Discovery Studio ◽  
Hela Cell Lines ◽  
Antiproliferative Activities

Background: Spirocyclic indoline compounds widely exist in numerous natural products with good biological activities and some drug molecules in many aspects. In recent years, it has attracted extensive attention as potent anti-tumor agents in the fields of pharmacology and chemistry. Objective: In this study, we focused on designing and synthesizing a set of novel 1'-H-spiro[indole-3,4'-piperidine] derivatives, which were evaluated by preliminary bioactivity experiment in vitro and molecular docking. Method: The key intermediate 1'-methylspiro[indoline-3,4'-piperidine] (B4) reacted with benzenesulfonyl chloride with different substituents under alkaline condition to obtain its sulfonyl derivatives (B5-B10). We evaluated their antiproliferative activities against A549, BEL-7402 and HeLa cells by MTT assay. We performed the CDOCKER module in Discovery Studio 2.5.5 software for molecular modeling of compound B5, and investigated the binding of compound B5 with the target proteins from PDB database. Results: The results indicated that compounds B4-B10 exhibited good antiproliferative activities against the above three types of cells, in which compound B5 with chloride atom as electron-withdrawing substituent on a phenyl ring showed the highest potency against BEL-7402 cells (IC50=30.03±0.43 μg/mL). By binging of the prominent bioactive compound B5 to CDK, c-Met, EGFR protein crystals, The binding energy of B5 with these three types receptors are -44.3583 kcal/mol, - 38.3292 kcal/mol, -33.3653 kcal/mol respectively. Conclusion: Six 1'-methylspiro[indoline-3,4'-piperidine] derivatives were synthesized and evaluated against BEL-7402, A- 549, HeLa cell lines. Compound B5 showed significant inhibition on BEL-7402 cell lines. Molecular docking revealed that B5 showed good affinity by the good fitting between B5 and these three targets with amino acid residues in active sites which encourage us to conduct further evaluation such as the kinase experiment.

Wild pink bayberry fruit: the effect of in vitro gastrointestinal digestion on phytochemical profiles, and antioxidant and antiproliferative activities

2021 ◽  
Author(s):  
Wen Xia ◽  
Yanyun Lin ◽  
Ersheng Gong ◽  
Tong Li ◽  
Fengli Lian ◽  
...  
Keyword(s):  
Dietary Supplement ◽  
Antiproliferative Activity ◽  
Gastrointestinal Digestion ◽  
In Vitro Gastrointestinal Digestion ◽  
Phytochemical Profiles ◽  
Antiproliferative Activities

In general, pink bayberry cultivar, a vital source of polyphenols, showed strong antiproliferative activity after digestion at the end of the intestinal and colon steps, which can be considered as a dietary supplement.

scholarly journals Compatibility, Stability, and Efficacy of Vancomycin Combined With Gentamicin or Ethanol in Sodium Citrate as a Catheter Lock Solution

2017 ◽  
Vol 52 (10) ◽  
pp. 685-690
Author(s):  
Yangjie Wei ◽  
Joshua WonJoon Yang ◽  
Sai HS. Boddu ◽  
Rose Jung ◽  
Mariann D. Churchwell
Keyword(s):  
Chemical Stability ◽  
Sodium Citrate ◽  
Chronically Ill ◽  
Storage Conditions ◽  
Entire Study ◽  
Indwelling Catheters ◽  
Source Of Infection ◽  
Lock Solution ◽  
All Solutions

Background: Indwelling catheters deliver lifesaving medical treatments for many chronically ill patients but are frequently a source of infection. Treatment may include an antimicrobial agent(s) and anticoagulant solution dwelling within the catheter. In vitro determinations of solution compatibility and stability are necessary prior to use in patients. Objective: The aim of this study was to determine the physical compatibility, chemical stability, and antimicrobial activity of vancomycin (5 or 10 mg/mL) with gentamicin (1 mg/mL) or 40% ethanol in 4% sodium citrate lock solution over 72 hours. Methods: All solutions were prepared per manufacturer’s instructions. Samples were studied under 4 conditions: (1) 25°C with light, (2) 25°C without light, (3) 37°C with light, and (4) 37°C without light. Physical compatibility and chemical stability were assessed at 0, 24, 48, and 72 hours. Antimicrobial susceptibility testing was conducted at 0 and 72 hours. All studies were carried out in triplicate. Results: All solution combinations under each condition remained patent from baseline to 48 hours. One solution combination of vancomycin (5 mg/mL) and ethanol (40% v/v) in 4% sodium citrate revealed a slight turbidity at 72 hours. Clarity and pH remained stable in all other solutions during the entire study period. Chemical compatibility and antibiotic activity ranged from 95% to 105% and 95% to 106% of initial baseline values, respectively, for all solutions under 4 storage conditions. Conclusions: All antibiotic-anticoagulant lock solutions were found to be physically, chemically, and microbiologically stable during the 72-hour study period except vancomycin (5 mg/mL) and ethanol (40% v/v) in 4% sodium citrate solution which showed slight turbidity at 72 hours.

scholarly journals Morphology, myxocarpy, mineral content, and in vitro antimicrobial and antiproliferative activities of mericarps of the vulnerable Turkish endemic Salvia pilifera

2019 ◽  
Vol 23 (4) ◽  
pp. 729-739 ◽  
Author(s):  
Sevda GÜZEL ◽  
Ahmet KAHRAMAN ◽  
Mahmut ÜLGER ◽  
Yusuf ÖZAY ◽  
İbrahim BOZGEYİK
Keyword(s):  
Mineral Content ◽  
Antiproliferative Activities

An insight into synthetic Schiff bases revealing antiproliferative activities in vitro

2013 ◽  
Vol 21 (13) ◽  
pp. 3648-3666 ◽  
Author(s):  
Krzysztof Sztanke ◽  
Agata Maziarka ◽  
Anna Osinka ◽  
Małgorzata Sztanke
Keyword(s):  
Schiff Bases ◽  
Insight Into ◽  
Antiproliferative Activities

AMPHOTERICIN B TOPICAL EXTEMPORANEOUS PREPARATIONS FOR THE TREATMENT OF NON-DERMATOPHYTIC ONYCHOMYCOSIS

2020 ◽  
pp. 135-139
Author(s):  
KOMESMUNEEBORIRAK PHOJANA ◽  
WERAWATGANONE PORNPEN ◽  
MUANGSIRI WALAISIRI
Keyword(s):  
Amphotericin B ◽  
Chemical Stability ◽  
High Performance ◽  
Sodium Lauryl Sulfate ◽  
Physical Stability ◽  
Lauryl Sulfate ◽  
Physical And Chemical ◽  
Injection Product

Objective: At present, the nail preparation to cure onychomycosis, caused by non-dermatophyte molds, is not commercially available in Thailand. The physical and chemical stability of amphotericin B (AmB) extemporaneous preparations in the presence of 30% dimethyl sulfoxide (DMSO) and their in vitro nail permeation was evaluated. Methods: AmB extemporaneous preparations in the presence of 30% DMSO were prepared from a commercial sterile injection product, and cream or hydrophilic ointment. Physical stability was tested at 30°C for 2 months, or using 6 heating-cooling cycles. The chemical stability and in vitro nail permeation of AmB content were analyzed using high-performance liquid chromatography (HPLC). In vitro nail permeation was performed by applying 3.5 mg/mm2 of the tested formulation on nail clippings for 5 consecutive days. Results: The AmB cream and ointment extemporaneous preparations containing 30% DMSO, a permeation enhancer, were homogeneous and pale yellow to yellow cream or ointment. The AmB ointment was stable for up to 60 days. The ointment preparation allows in vitro penetration through nails up to 14.17 μg/cm2. The ointment preparation allows significantly better penetration through than the cream preparation due to the presence of DMSO, sodium lauryl sulfate (SLS), and water in the ointment preparation. Conclusion: The AmB extemporaneous ointment was successfully compounded from a commercial sterile injection product with a beyond-use date of 60 days. The ointment preparation is currently under further investigation for in vivo efficacy.

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