Design, physico-chemical characterization and in vitro biological activity of organogold(III) glycoconjugates

In order to develop new metal-based glycoconjugates as potential anticancer agents, four organometallic gold(III)-dithiocarbamato glycoconjugates of the type [AuIII(2-Bnpy)(SSC-Inp-GlcN)](PF6) (2-Bnpy: 2-benzylpyridine; Inp: isonipecotic moiety; GlcN: amino-glucose scaffold; Au3-Au6) and the...

Biological and physico-chemical characterization of ultra high diluted Hydrastis canadensis and in vitro studies on mammalian cells

Allgemeine Homöopathische Zeitung ◽

10.1055/s-0037-1601241 ◽

2017 ◽

Vol 262 (02) ◽

pp. 2-76

Author(s):

N Chandrakar ◽

MK Temgire ◽

SG Kane ◽

AK Suresh ◽

J Bellare

Keyword(s):

Mammalian Cells ◽

In Vitro Studies ◽

Hydrastis Canadensis ◽

Decalepis hamiltonii (Wight & Arn.) Fortified Jaggery: Its Physico-chemical Characterization and Studies on its In vitro Biological Activities

International Journal of Current Microbiology and Applied Sciences ◽

10.20546/ijcmas.2021.1001.178 ◽

2021 ◽

Vol 10 (01) ◽

pp. 1510-1529

Author(s):

C. Vinutha ◽

M. A. Harish Nayaka ◽

G. Sowmyashree ◽

Dinesh Kumar

Keyword(s):

Biological Activities ◽

Decalepis Hamiltonii ◽

Antibody targeting of lipid nanocapsules for directed drug delivery: physico-chemical characterization and in vitro study

Drug Discovery Today ◽

10.1016/j.drudis.2010.09.417 ◽

2010 ◽

Vol 15 (23-24) ◽

pp. 1105-1105

Author(s):

P. Sánchez-Moreno ◽

H. Boulaiz ◽

J.A. Marchal ◽

J.L. Ortega-Vinuesa ◽

J.M. Peula García ◽

...

Keyword(s):

Drug Delivery ◽

In Vitro Study ◽

Vitro Study ◽

Lipid Nanocapsules ◽

Physico Chemical ◽

Antibody Targeting

In Vitro Physico-Chemical Characterization and Standardized In Vivo Evaluation of Biocompatibility of a New Synthetic Membrane for Guided Bone Regeneration

Materials ◽

10.3390/ma12071186 ◽

2019 ◽

Vol 12 (7) ◽

pp. 1186

Author(s):

Lívia da Costa Pereira ◽

Carlos Fernando de Almeida Barros Mourão ◽

Adriana Terezinha Neves Novellino Alves ◽

Rodrigo Figueiredo de Brito Resende ◽

Marcelo José Pinheiro Guedes de Uzeda ◽

...

Keyword(s):

Bone Regeneration ◽

Chemical Properties ◽

Guided Bone Regeneration ◽

Tissue Reaction ◽

In Vivo Evaluation ◽

Physico Chemical ◽

Tissue Reactions

This study’s aim was to evaluate the biocompatibility and bioabsorption of a new membrane for guided bone regeneration (polylactic-co-glycolic acid associated with hydroxyapatite and β-tricalcium phosphate) with three thicknesses (200, 500, and 700 µm) implanted in mice subcutaneously. Scanning electron microscopy, X-ray diffraction, Fourier transform infrared spectroscopy, and the quantification of carbon, hydrogen and nitrogen were used to characterize the physico-chemical properties. One hundred Balb-C mice were divided into 5 experimental groups: Group 1—Sham (without implantation); Group 2—200 μm; Group 3—500 μm; Group 4—700 μm; and Group 5—Pratix®. Each group was subdivided into four experimental periods (7, 30, 60 and 90 days). Samples were collected and processed for histological and histomorphometrical evaluation. The membranes showed no moderate or severe tissue reactions during the experimental periods studied. The 500-μm membrane showed no tissue reaction during any experimental period. The 200-μm membrane began to exhibit fragmentation after 30 days, while the 500-μm and 700-µm membranes began fragmentation at 90 days. All membranes studied were biocompatible and the 500 µm membrane showed the best results for absorption and tissue reaction, indicating its potential for clinical guided bone regeneration.

Design, synthesis and biological activities of pyrrole-3-carboxamide derivatives as EZH2 (enhancer of zeste homologue 2) inhibitors and anticancer agents

New Journal of Chemistry ◽

10.1039/c9nj04713a ◽

2020 ◽

Vol 44 (6) ◽

pp. 2247-2255

Author(s):

Qifan Zhou ◽

Lina Jia ◽

Fangyu Du ◽

Xiaoyu Dong ◽

Wanyu Sun ◽

...

Keyword(s):

Biological Activity ◽

Anticancer Agents ◽

Biological Activities ◽

Activity Assay ◽

Design Synthesis ◽

Structure Activity Relationships ◽

Structure Activity ◽

Enhancer Of Zeste

A novel series of pyrrole-3-carboxamides targeting EZH2 have been designed and synthesized. The structure–activity relationships were summarized by combining with in vitro biological activity assay and docking results.

Chemical characterization and in vitro biological activity of Cymbopogon citratus extracts against Haemonchus spp. and Trichostrongylus spp. nematodes from sheep

Parasitology ◽

10.1017/s0031182020001432 ◽

2020 ◽

Vol 147 (13) ◽

pp. 1559-1568

Author(s):

Letícia Oliveira da Rocha ◽

Gloria Cristina da Silva Lemos ◽

Ivo José Curcino Vieira ◽

Raimundo Braz-Filho ◽

Silvério de Paiva Freitas ◽

...

Keyword(s):

Biological Activity ◽

Gastrointestinal Nematodes ◽

The Body ◽

Intestinal Cells ◽

Phytochemical Analysis ◽

Cymbopogon Citratus ◽

Thin Sections ◽

Methanolic Extracts

AbstractMedicinal plants have been the focus of several studies due to their nematicide properties which can be used to control nematodes in sheep. No study has examined the morphological effects of Cymbopogon citratus on nematodes. Thus, this study evaluated the chemical composition, nematicidal activity and effects of C. citratus extracts on the morphology of eggs and infective larvae (L3) of sheep. Aqueous and methanolic extracts and fractions of C. citratus were obtained and analysed in vitro. The C. citratus extracts were effective against Haemonchus spp. and Trichostrongylus spp. larvae and eggs. Ten fractions were obtained from C. citratus, six of which had high ovicidal activity at 1000 μg mL−1, and two fractions had high activity at all tested concentrations. The phytochemical analysis identified the presence of compounds such as terpenoids, various ketones, esters, and fatty acids. The ultrastructural analysis showed deformations of the cuticle and wilting along the body of the nematodes at all concentrations. The muscular layer, intestinal cells and the mitochondria profile showed damage compared to the typical pattern. Ultra-thin sections of eggs treated with methanolic fractions of C. citratus presented modifications. This study showed the biological activity and effects of C. citratus on the gastrointestinal nematodes in sheep.

Optimization of Innovative Three-Dimensionally-Structured Hybrid Vesicles to Improve the Cutaneous Delivery of Clotrimazole for the Treatment of Topical Candidiasis

Pharmaceutics ◽

10.3390/pharmaceutics11060263 ◽

2019 ◽

Vol 11 (6) ◽

pp. 263 ◽

Cited By ~ 4

Author(s):

Maria Letizia Manca ◽

Iris Usach ◽

José Esteban Peris ◽

Antonella Ibba ◽

Germano Orrù ◽

...

Keyword(s):

Electron Microscopy ◽

Transmission Electron Microscopy ◽

Chemical Properties ◽

Yeast Cells ◽

Unilamellar Vesicles ◽

Transmission Electron ◽

New three-dimensionally-structured hybrid phospholipid vesicles, able to load clotrimazole in a high amount (10 mg/mL), were obtained for the first time in this work by significantly reducing the amount of water (≤10%), which was replaced with a mixture of glycerol and ethanol (≈90%). A pre-formulation study was carried out to evaluate the effect of both the composition of the hydrating medium and the concentration of the phospholipid on the physico-chemical properties of hybrid vesicles. Four different three-dimensionally-structured hybrid vesicles were selected as ideal systems for the topical application of clotrimazole. An extensive physico-chemical characterization performed using transmission electron microscopy (TEM), cryogenic transmission electron microscopy (cryo-TEM), 31P-NMR, and small-angle X-ray scattering (SAXS) displayed the formation of small, multi-, and unilamellar vesicles very close to each other, and was capable of forming a three-dimensional network, which stabilized the dispersion. Additionally, the dilution of the dispersion with water reduced the interactions between vesicles, leading to the formation of single unilamellar vesicles. The evaluation of the in vitro percutaneous delivery of clotrimazole showed an improved drug deposition in the skin strata provided by the three-dimensionally-structured vesicles with respect to the commercial cream (Canesten®) used as a reference. Hybrid vesicles were highly biocompatible and showed a significant antifungal activity in vitro, greater than the commercial cream Canesten®. The antimycotic efficacy of formulations was confirmed by the reduced proliferation of the yeast cells at the site of infection in vivo. In light of these results, clotrimazole-loaded, three-dimensionally-structured hybrid vesicles appear to be one of the most innovative and promising formulations for the treatment of candidiasis infections.