Monocarbonyl Analogs of Curcumin Based on the Pseudopelletierine Scaffold: Synthesis and Anti-Inflammatory Activity

Curcumin (CUR) is a natural compound that exhibits anti-inflammatory, anti-bacterial, and other biological properties. However, its application as an effective drug is problematic due to its poor oral bioavailability, solubility in water, and poor absorption from the gastrointestinal tract. The aim of this work is to synthesize monocarbonyl analogs of CUR based on the 9-methyl-9-azabicyclo[3.2.1]nonan-3-one (pseudopelletierine, granatanone) scaffold to improve its bioavailability. Granatane is a homologue of tropane, whose structure is present in numerous naturally occurring alkaloids, e.g., l-cocaine and l-scopolamine. In this study, ten new pseudopelletierine-derived monocarbonyl analogs of CUR were successfully synthesized and characterized by spectral methods and X-ray crystallography. Additionally, in vitro test of the cytotoxicity and anti-inflammatory properties of the synthesized compounds were performed.

Download Full-text

THE STUDY ON GRANTING BIOACTIVITY OF Ti ALLOY BY SURFACE TREATMENT

Surface Review and Letters ◽

10.1142/s0218625x1001362x ◽

2010 ◽

Vol 17 (02) ◽

pp. 153-157 ◽

Cited By ~ 1

Author(s):

N. R. HA ◽

Z. X. YANG ◽

G. C. KIM ◽

K. H. HWANG ◽

D. S. SEO ◽

...

Keyword(s):

Surface Treatment ◽

Body Fluid ◽

Surface Effect ◽

In Vitro Test ◽

Ti Alloy ◽

X Ray Diffraction ◽

X Ray ◽

Chemical Surface ◽

Vitro Test

Titanium alloys are superior of biocompatibility, mechanical properties and chemical stability. The biocompatibility of Ti alloy is related to the surface effect between human tissue and implant. Therefore, the purpose of this study is to investigate the bioactivity of Ti alloy by alkali and acid chemical surface treatment; and the biocompatibility of Ti alloy was evaluated by in vitro test. Higher bone-bonding ability and bioactivity of the substrate were obtained by the formation of apatite layers on the Ti alloy in simulated body fluid. The microstructures of apatite layer were investigated by scanning electron microscope (SEM) and the formed phases were analyzed with X-ray diffraction (XRD).

Download Full-text

Clinical Evaluation of an in Vitro Test for Radiosensitivity of Leukemic Lymphocytes

Blood ◽

10.1182/blood.v20.4.432.432 ◽

1962 ◽

Vol 20 (4) ◽

pp. 432-442 ◽

Cited By ~ 23

Author(s):

ROBERT SCHREK ◽

STANLEY L. LEITHOLD ◽

IRVING A. FRIEDMAN ◽

WILLIAM R. BEST

Keyword(s):

Survival Time ◽

Median Survival ◽

Median Survival Time ◽

Leukocyte Count ◽

In Vitro Test ◽

X Rays ◽

X Ray ◽

Leukocyte Counts ◽

Vitro Test

Abstract A recently developed slide-chamber method was used to test the radiosensitivity of blood lymphocytes from 80 patients with chronic lymphocytic or lymphosarcoma-cell leukemia. The objective of this study was to determine whether these in vitro tests on sensitivity to x-rays had any clinical significance. Two objective criteria were used to measure the clinical reactions of the leukemic patients. The first was the duration of survival of patients following the in vitro test. The second was the minimal leukocyte count of a patient following x-ray therapy; the minimal count was expressed as a percentage of the count before therapy. The in vitro radiosensitivity was measured by the 10 per cent survival time of lymphocytes irradiated with 1000 r. Blood lymphocytes from non-leukemic individuals were highly radiosensitive with indices of 1.1 to 2.2 days. In initial tests, the lymphocytes of 61 leukemic patients had the same high sensitivity to x-rays as lymphocytes from non-leukemic individuals. In contrast, the lymphocytes of 19 leukemic patients were radioresistant to irradiation with indices of 2.5 to 11 days. The 61 patients with radiosensitive lymphocytes had a median survival time of 22 months after the in vitro test. In contrast, the 19 patients with radioresistant lymphocytes had a median survival time of only 4 months. Clinical x-ray therapy caused a greater decline in leukocyte counts in patients with radiosensitive lymphocytes than in those with radioresistant cells. A significant index of 0.60 was obtained for the correlation of in vitro radiosensitivity of lymphocytes and the in vivo decrease in leukocyte counts of patients after x-ray therapy. It is concluded that an in vitro finding of radioresistant lymphocytes is correlated with a poor response of the leukocyte count to x-ray therapy and a short survival time of the patient.

Download Full-text

In Vitro Study of Microplasma Sprayed Hydroxyapatite Coatings in Simulated Body Fluid

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.79-82.815 ◽

2009 ◽

Vol 79-82 ◽

pp. 815-818 ◽

Cited By ~ 1

Author(s):

Qiu Ying Zhao ◽

Ding Yong He ◽

Xiao Yan Li ◽

Jian Min Jiang

Keyword(s):

Simulated Body Fluid ◽

Body Fluid ◽

Carbonate Apatite ◽

In Vitro Test ◽

X Ray Diffraction ◽

X Ray ◽

Amorphous Phases ◽

Hydroxyapatite Coatings ◽

Vitro Test

Hydroxyapatite (HA) coatings were deposited onto Ti6Al4V substrate by microplasma spraying (MPS) in the current research. The morphology, phase compositions, and percentage of crystallinity of the coatings were characterized by means of scanning electron microscopy (SEM) and X-ray diffraction. An in vitro evaluation by soaking the coatings in simulated body fluid (SBF) for up to 14 days was conducted aiming at the evaluation of their bioactivity. Results from the present investigation suggest that microplasma sprayed HA coatings exhibited certain roughness, pores, and microcracks. Thermal decomposition existed in the coatings where HA, α-TCP，β-TCP, amorphous phases, and CaO-exclusive impurities were observed. The in vitro test indicated that HA coatings deposited by MPS possessed better bioactivity and stability. A layer of carbonate-apatite covered most of the coating surface, which did not exhibit significant spalling after incubation in SBF.

Download Full-text

Preparation of the Nano-Hydroxyapatite/Chitosan/Konjac Glucomannan Composite as a Novel Degradable Drug Delivery System

Materials Science Forum ◽

10.4028/www.scientific.net/msf.569.357 ◽

2008 ◽

Vol 569 ◽

pp. 357-360

Author(s):

Gang Zhou ◽

Yu Bao Li ◽

Soo Wohn Lee

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Konjac Glucomannan ◽

In Vitro Test ◽

X Ray Diffraction ◽

X Ray ◽

Before And After ◽

Vitro Test

Nano-hydroxyapatite (n-HA)/chitosan (CS)/konjac glucomannan (KGM) composite was prepared by integrating composition and molding. Then, X-ray diffraction (XRD) and scanning electron microscopy (SEM) were used to analyze the physical, chemical and degradable properties of the composite before and after in simulated body fluid (SBF). Moreover, study in vitro test for drug delivery revealed that the amount of released pentoxifylline (1-[5-oxohexyl]-3,7-dimethylxanthine)(PTX) reached a plateau and equaled 80% of the drug loaded in an implant. The newly develop n-HA/CS/KGM composite may serve as a good degradable biomaterial for implantable drug delivery system (IDDS) in bone tissue engineering.

Download Full-text

Surface Modification of 316L SS Implants by Applying Bioglass/Gelatin/Polycaprolactone Composite Coatings for Biomedical Applications

Coatings ◽

10.3390/coatings10121220 ◽

2020 ◽

Vol 10 (12) ◽

pp. 1220

Author(s):

Behzad Mojarad Shafiee ◽

Reza Torkaman ◽

Mohammad Mahmoudi ◽

Rahmatollah Emadi ◽

Maryam Derakhshan ◽

...

Keyword(s):

Cell Viability ◽

Composite Coatings ◽

Apatite Formation ◽

In Vitro Test ◽

X Ray ◽

Vitro Test ◽

Mtt Tests ◽

Good Agreement

In this study, various composites of bioglass/gelatin/polycaprolactone (BG/GE/PCL) were produced and coated on the surface of 316L stainless steel (SS) to improve its bioactivity. X-ray diffractometry (XRD), scanning electron microscopy (SEM) and energy-dispersive X-ray spectroscopy (EDS) were utilized to characterize the specimens. The results showed that bioglass particles were distributed uniformly in the coating. By increasing the wt.% of bioglass in the nanocomposite coatings, the surface roughness and adhesion strength increased. The corrosion behavior of GE/PCL (PCL-10 wt.% gelatin coated on 316L SS) and 3BG/GE/PCL (GE/PCL including 3 wt.% bioglass coated on 316L SS) samples were studied in PBS solution. The results demonstrated that 3BG/GE/PCL sample improved the corrosion resistance drastically compared to the GE/PCL specimen. In vitro bioactivity of samples was examined after soaking the specimens for 7, 14 and 28 days in simulated body fluid (SBF). The results showed a significant apatite formation on the surface of 3BG/GE/PCL samples. The cell viability evaluation was performed using 3- (4, 5-dimethylthiazol-2-yl)-2,5 diphenyltetrazoliumbromide (MTT) tests which confirmed the enhanced cell viability on the surface of 3BG/GE/PCL samples. The in vivo behavior of specimens illustrated no toxicity and inflammatory response and was in a good agreement with the results obtained from the in vitro test.

Download Full-text

ANTIBACTERIAL AND BIOCOMPATIBILITY PROPERTIES OF NANO-SILVER/TITANIA THIN LAYER

International Journal of Modern Physics B ◽

10.1142/s021797921110196x ◽

2011 ◽

Vol 25 (27) ◽

pp. 3647-3653

Author(s):

R. EMADI ◽

K. RAEISSI

Keyword(s):

Antibacterial Effect ◽

In Vitro Test ◽

X Ray Diffraction ◽

Sem Images ◽

X Ray ◽

Spherical Structures ◽

Vitro Test ◽

And Staphylococcus Aureus ◽

Electrodeposition Of Silver

Ag/TiO2coating was prepared by anodizing the surface of Ti followed by electrodeposition of silver. By X-ray diffraction (XRD) analyses, that indicated the crystalline size of Ag deposit onto the oxidized surface of Ti was around 32 nm. Scanning electron microscopy (SEM) images of the oxidized surface with and without Ag deposit show that TiO2is formed uniformly but Ag deposit consisted of numerous spherical structures. The Escherichia coli and Staphylococcus aureus bacteria were utilized to test the antibacterial effect of Ag/TiO2coating which showed more than 99% of bacteria were killed after 24 h incubation. The results of in vitro test showed Ag/TiO2coating is also biocompatible.

Download Full-text

Physicochemical and in vitro bioactivity studies of bioactive glasses in the SiO2-CaO-MgO-P2O5, SiO2-Na2O-CaO-P2O5 and SiO2-Na2O-CaO-MgO-P2O5 systems

Mediterranean Journal of Chemistry ◽

10.13171/mjc10502005161413ml ◽

2020 ◽

Vol 10 (5) ◽

pp. 492

Author(s):

Smaiel Herradi ◽

Sara Bouhazma ◽

Sanae Chajri ◽

Imane Adouar ◽

Souad Rakib ◽

...

Keyword(s):

Dissolution Rate ◽

Sol Gel ◽

Energy Dispersive ◽

In Vitro Test ◽

X Ray Diffraction ◽

X Ray ◽

Vitro Test ◽

Diffraction Patterns ◽

The One

Glasses in the quaternary and quinary system SiO2-CaO-MgO-P2O5 (SCMP), SiO2-Na2O-CaO-P2O5 (SNCP) and SiO2-Na2O-CaO-MgO-P2O5 (SNCMP), have been prepared by using the sol-gel technique. Investigations of structural and bioactive properties of these glasses have been undertaken by using X-ray diffraction (XRD), Fourier Transform Infrared Spectroscopy (FTIR), Scanning Electron Microscopy (SEM) and Energy Dispersive X-ray Spectroscopy (EDS). The in vitro bioactivity was assessed by determining the changes in surface morphology and composition after soaking in simulated body fluid (SBF) for up to 30 days at 37°C. X-ray diffraction patterns indicated the formation of hydroxycarbonated apatite layer (HCA) after only one hour for SNCMP glass and after four days for SCMP and SNCP glasses. Furthermore, observed bands of FTIR spectra confirmed the growth of HCA layer during in vitro test.Moreover, the dissolution rate has been investigated using energy-dispersive X-ray spectroscopy. The observed EDS patterns confirmed the growth of HCA layer on all samples surfaces during in vitro analysis. On the one hand, we report the existence of Na2Ca2Si3O9 (that couple good mechanical strength with satisfactory biodegradability) as a single crystalline phase in the SNCP glass when calcined at 600°C. On the other hand, we have noticed that the coexistence of magnesium and sodium both enhanced the dissolution rate and hindered the crystallization in the SNCMP glass at 600°C.

Download Full-text

Influence of thermal treatment on the structure and in vitro bioactivity of sol-gel prepared CaO-SiO2-P2O5 glass-ceramics

Processing and Application of Ceramics ◽

10.2298/pac1403155r ◽

2014 ◽

Vol 8 (3) ◽

pp. 155-166 ◽

Cited By ~ 14

Author(s):

Lachezar Radev

Keyword(s):

Thermal Treatment ◽

Calcium Silicate ◽

Sol Gel ◽

Glass Ceramics ◽

In Vitro Test ◽

In Vitro Bioactivity ◽

X Ray ◽

Vitro Test ◽

Sbf Solution

Nowadays there is a substantial practical interest in the in vitro bioactivity of calcium silicate phosphate (CSP) glass-ceramics and carbonate apatite (CO3HA) formation on their surfaces after in vitro test in simulated body fluid (SBF). The main purpose of the presented article is the evaluation of the chemical composition of the gel with nominal composition 70.59 CaO:28.23 SiO2:1.18 P2O5 (mol.%) on the structure, crystallization behaviour and in vitro bioactivity in SBF solution for 14 and 28 days. The prepared glass-ceramics have been synthesized via a polystep sol-gel method. The structure of the obtaining samples was studied by X-ray diffraction (XRD) analysis, Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy with energy dispersive X-ray spectroscopy (SEM-EDX). After thermal treatment of the samples XRD confirmed the presence of ?-Ca2SiO4 and Ca15(PO4)2(SiO4)6, and indicated that at 1500?C Ca15(PO4)2(SiO4)6 becomes predominant phase. FTIR revealed the presence of all characteristics bands for calcium silicate phosphate (CSP) bonds. SEM monitors the presence of particles with different morphology. After in vitro test in SBF, FTIR depicted that B-type carbonate containing hydroxyapatite (CO3HA) is preferentially formed on the immersed glass-ceramics. SEMof the precipitated layers showed the presence of HA spheres. The changes in SBF solution after soaking the samples were recorded by inductively coupled plasma atomic emission spectroscopy (ICP-AES).

Download Full-text

Haemostatic Platelet Plug Formation in the Isolated Rabbit Mesenteric Preparation - An Analysis of Red Blood Cell Participation

Thrombosis and Haemostasis ◽

10.1055/s-0038-1650069 ◽

1980 ◽

Vol 44 (01) ◽

pp. 006-008 ◽

Cited By ~ 12

Author(s):

D Bergqvist ◽

K-E Arfors

Keyword(s):

Whole Blood ◽

Platelet Rich Plasma ◽

Adenosine Diphosphate ◽

In Vitro Test ◽

Pharmacological Agents ◽

Vitro Test ◽

Releasing Effect ◽

Plug Formation

SummaryIn a model using an isolated rabbit mesenteric preparation microvessels were transected and the time until haemostatic plugs formed was registered. Perfusion of platelet rich plasma gave no haemostasis whereas whole blood did. Addition of chlorpromazine or adenosine to the whole blood significantly prolonged the time for haemostasis, and addition of ADP to the platelet rich plasma significantly shortened it. It is concluded that red cells are necessary for a normal haemostasis in this model, probably by a combination of a haemodynamic and ADP releasing effect.The fundamental role of platelets in haemostatic plug formation is unquestionable but there are still problems concerning the stimulus for this process to start. Three platelet aggregating substances have been discussed – thrombin, adenosine diphosphate (ADP) and collagen. Evidence speaking in favour of thrombin is, however, very minimal, and the discussion has to be focused on collagen and ADP. In an in vitro system using polyethylene tubings we have shown that "haemostasis" can be obtained without the presence of collagen but against these results can be argued that it is only another in vitro test for platelet aggregation (1).To be able to induce haemostasis in this model, however, the presence of red blood cells is necessary. To further study this problem we have developed a model where haemostatic plug formation can be studied in the isolated rabbit mesentery and we have briefly reported on this (2).Thus, it is possible to perfuse the vessels with whole blood as well as with platelet rich plasma (PRP) and different pharmacological agents of importance.

Download Full-text