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

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.

scholarly journals Artificial Caries Lesion Characteristics after Secondary Demineralization with Theobromine-Containing Protocol

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 300
Author(s):  
Hani M. Nassar ◽  
Frank Lippert
Keyword(s):  
Mineral Content ◽  
Significance Level ◽  
Lesion Depth ◽  
Caries Lesion ◽  
Mineral Profile ◽  
Bonferroni Test ◽  
Bovine Enamel ◽  
Caries Lesions ◽  
Nail Varnish

Developing artificial caries lesions with varying characteristics is needed to adequately study caries process in vitro. The objective of this study was to investigate artificial caries lesion characteristics after secondary demineralization protocol containing theobromine and fluoride. Sixty bovine enamel slabs (4 × 3 mm) were demineralized using a Carbopol-containing protocol for 6 days. A baseline area (2 × 3 mm) was protected with acid-resistant nail varnish, after which specimens were exposed for 24 h to a secondary demineralization protocol containing acetic acid plus one of four fluoride/theobromine combinations (n = 15): theobromine (50 or 200 ppm) and fluoride (0 or 1 ppm). Specimens were sectioned and analyzed using transverse microradiography for changes in mineral content, lesion depth, and surface layer mineralization. Data was analyzed using paired t-test and analysis of variance followed by Bonferroni test at 0.05 significance level. After secondary demineralization, fluoride-containing groups had significantly deeper lesions (p = 0.002 and 0.014) compared to the group with 0 ppm fluoride and 50 ppm theobromine. Mineral content and lesion depth were significantly different compared to baseline for all groups. Theobromine did not show an added effect on mineral uptake. Theobromine-containing groups exhibited particularly deep lesions with a more uniform mineral profile in the presence of fluoride.

scholarly journals Chemistry of Tropical Eucheumatoids: Potential for Food and Feed Applications

Biomolecules ◽  
2021 ◽  
Vol 11 (6) ◽  
pp. 804
Author(s):  
Andrea Ariano ◽  
Nadia Musco ◽  
Lorella Severino ◽  
Anna De Maio ◽  
Annabella Tramice ◽  
...  
Keyword(s):  
Chemical Analysis ◽  
Inductively Coupled Plasma ◽  
Mineral Content ◽  
Kappaphycus Alvarezii ◽  
Optical Emission ◽  
Essential Elements ◽  
Feed Additive ◽  
Inductively Coupled ◽  
Food And Feed

The use of seaweeds as additives in animal nutrition may be a valid option to traditional feed as they represent a rich source of minerals, carbohydrates and antioxidants. The aim of this study was to analyze the chemical composition and in vitro antioxidant capacity of two tropical eucheumatoids, Kappaphycus alvarezii and Kappaphycus striatus, in Malaysian wild offshore waters. The chemical analysis was performed via inductively coupled plasma–optical emission spectroscopy for evaluating the concentration of toxic (Cd, Pb, Hg, As) and essential elements (Mn, Fe, Cu, Ni, Zn, Se); NMR spectroscopy was used for carrageenans investigation. Furthermore, the soluble and fat-soluble antioxidant capacities were determined by FRAP, DPPH and ABTS assays. The chemical analysis revealed a higher content of trace elements in K. alvarezii as compared to K. striatus, and both exhibited a high mineral content. No significant differences in metal concentrations were found between the two species. Both samples showed a mixture of prevailing κ- and t-carrageenans. Finally, the levels of soluble and fat-soluble antioxidants in K. alvarezii were significantly higher than in K. striatus. Our findings suggest that K. alvarezii could be used as a potential feed additive because of its favorable chemical and nutritional features.

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.

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

scholarly journals Design, synthesis and evaluation of belinostat analogs as histone deacetylase inhibitors

2019 ◽  
Vol 11 (21) ◽  
pp. 2765-2778
Author(s):  
Jie-Huan Zhang ◽  
Madhusoodanan Mottamal ◽  
Hai-Shan Jin ◽  
Shanchun Guo ◽  
Yan Gu ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Active Compound ◽  
Histone Deacetylase Inhibitors ◽  
Hdac Inhibitors ◽  
Antitumor Therapy ◽  
Design Synthesis ◽  
Inhibitory Activities ◽  
Antiproliferative Activities

Aim: Histone deacetylase (HDAC) is an attractive target for antitumor therapy. Therefore, the development of novel HDAC inhibitors is warranted. Materials & methods: A series of HDAC inhibitors based on N-hydroxycinnamamide fragment was designed as the clinically used belinostat analog using amide as the connecting unit. All target compounds were evaluated for their in vitro HDAC inhibitory activities and some selected compounds were tested for their antiproliferative activities. Conclusion: Among them, compound 7e showed an IC50 value of 11.5 nM in inhibiting the HDAC in a pan-HDAC assay, being the most active compound of the series.

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