Development of phyllanthin containing microcapsules and their improved biological activity towards skin cells and Staphylococcus aureus.

Chitosan based microcapsule which encapsulated with phyllanthin was developed by simple coacervation. The composition and surface morphology of phyllanthin containing microcapsules were analyzed by Fourier Transform Infrared spectroscopy and Scanning Electron Microscopy, respectively. The release of phyllanthin from the microcapsules was found to be more than 60% after 120 h. In vitro biological assays demonstrated that these phyllanthin containing microcapsules showed a stronger anti-oxidation potential on both human fibroblasts and keratinocytes as well as a better growth inhibitory activity towards Staphylococcus aureus.

Development of hydrocortisone succinic acid/and 5-fluorouracil/chitosan microcapsules for oral and topical drug deliveries.

Recently, we demonstrated the safety use of calendula oil/chitosan microcapsules as a carrier for both oral and topical deliveries. We also reported the improved biological activity towards skin cells and Staphylococcus aureus of phyllanthin containing chitosan microcapsules. However, the possibility of both oral and topical applications was still necessary to be further studied. Here we investigated that both oral and topical applications of chitosan-based microcapsules were tested using hydrocortisone succinic acid (HSA) and 5-fluorouracil (5-FU), respectively. The drug loading efficiency, particle size, surface morphology and chemical compositions of both drug loaded microcapsules were confirmed by UV-vis spectrophotometer, particle size analyzer, scanning electron microscope and Fourier transform infrared spectroscopy. The in vitro release studies revealed that both HSA and 5-FU could be released form chitosan microcapsules. The mean adrenocorticotropic hormone concentration in HSA loaded microcapsule mice plasma was detected to be lower than that of water control. One hundred micrograms per milliliter of 5-FU containing microcapsules exhibited a stronger growth inhibition towards skin keratinocytes than that of free 5-FU. In vitro drug delivery model demonstrated the delivery of 5-FU from microcapsule treated textiles into nude mice skin. Further uses of the drug loaded microcapsules may provide an efficiency deliverable tool for both oral and topical applications.

Synthesis, characterization and preliminary analysis of in vivo biological activity of chitosan/celecoxib microcapsules.

The use of chitosan as the wall of microcapsule designed for delivery of encapsulated celecoxib is reported. Microcapsules were characterised with respect to size and encapsulation efficiency of celecoxib. In vivo animals demonstrated that both free celecoxib administration and chitosan/celecoxib microcapsules administration lead to a significant inhibition of cyclooxygenase-2 protein expression in the hepatocytes when compared with vehicle control mice. Interestingly, microcapsule containing celecoxib showed a better inhibition of cyclooxygenase-2 protein expression when compared with a simple oral administration of free celecoxib. Gas-chromatography-mass-spectrometry analysis showed that in mice treated with free celecoxib or chitosan/celecoxib microcapsules, their plasma concentration of celecoxib was similar. Microcapsules-based biomaterials as oral drug delivery vehicles may help to improve the absorption efficiency of therapeutic drugs.

The preparation of 2,6-disubstituted pyridinyl phosphine oxides as novel anti-cancer agents.

A series of 2,6-dimethoxylpyridinyl phosphine oxides have been synthesized and examined for their antitumor activity. 2,6-Dimethoxy-3-phenyl-4-diphenylphosphinoylpyridine 2 has been employed as the lead compound for this study. We found out that the presence of phosphine oxide on the 2,6-dimethoxylpyridine ring is important for the antitumor activity; the presence of bromine on this core leads to a further enhancement of its antitumor activity. This is the first reported work on the antitumor activity of the 2,6-dimethoxy-3,5-dibromopyridinyl phosphine oxide 5b towards MDAMB-231 breast cancer and SKHep-1 hepatoma cell lines.

Antitumor activity of diethynylfluorene derivatives of gold(I).

A list of diethynylfluorenes and their gold(I) derivatives have been studied for their antitumor activity as a function of their structure-activity relationships. End-capping the fluoren-9-one unit with gold(I) moieties could significantly strengthen the cytotoxic activity in vitro on three human cancer cell lines with induction of reactive oxygen species generation on Hep3B hepatocellular carcinoma cells and exhibit attractive antitumor activity from in vivo nude mice Hep3B xenograft model with limited adverse effects on vital organs including liver and kidney.

Synthesis and anti-cancer activity of benzothiazole containing phthalimide on human carcinoma cell lines.

Phthalic anhydride is a highly toxic substance, facing, however, the problem of hydrolysis. In fact, it is rapidly hydrolyzed in aqueous medium, generating phthalic acid as the final product, which is almost harmless to viable cells. Here we describe the 'one pot' condensation reaction for the synthesis of phthalic imide derivative (benzothiazole containing phthalimide), exhibiting in vitro cytotoxic potential on human cancer cell lines. We further demonstrated that both caspase-dependent and -independent pathways are involved in our novel benzothiazole containing phthalimide induced apoptosis on cancer cells.

Effects of different heel angles in sleep mode on heel interface pressure in the elderly.

BACKGROUND: The heels are one of the most common sites of pressure ulcers, and the incidence rate in the elderly aged 70 years or older is high. Although there is literature on heel interface pressure, the heel interface pressure of the elderly in different postures has not yet been explored, which will be investigated in this study, as well as the effects of different foot positions. Their skin conditions will also be examined. METHODS: Twenty-five females and twenty-six males, 70 years old or older, are evaluated while lying down, with only their naked foot in its natural position on a mattress, as well as placed on a standard or pressure-relieving mattress in different positions. The moisture, sebum content, and elasticity of the skin of the heel are tested. FINDINGS: The heel of most of the participants is positioned at a 60°-69° or 90°-99° angle to the support surface. The heel interface pressure is the greatest when the foot is upright. The age, weight, and body mass index have no significant impacts. The moisture and sebum content are extremely low while elasticity is normal. INTERPRETATION: The relaxed position of the foot is in neutral external rotation and upright positions. A greater amount of pressure is experienced when the foot is upright. The pressure-relieving mattress is more effective for reducing heel pressure but may not apply to all cases. Finally, the skin of the heel is dry and lacks sebum, which implies greater risk of developing heel sores.

Self-assembly of polypyrrole/chitosan composite hydrogels.

Hydrogels based on the polypyrrole (PPy)/chitosan (CS) composite are self-assembled and characterized for their electrical and swelling properties. The static polymerization of pyrrole monomer in aqueous solution containing CS is accompanied with the formation of PPy/CS composite hydrogel. The feed order in the reaction process plays a key role in the formation of the hydrogels. The participation of one-dimensional PPy blocks in the formation of the hydrogel network avoids a possible migration of PPy from the hydrogel. The effect of pH and ionic strength on the physical properties of PPy/CS composite hydrogels are investigated in detail. The results indicate that the pH-sensitive PPy/CS composite hydrogels show good water absorbencies in distilled water and saline solution. This method may open a new opportunity for the fabrication of composite hydrogels associating the biomacromolecules and conducting polymers, and the improvement of the comprehensive performance of the resulting products.

Corilagin is a potent inhibitor of NF-kappaB activity and downregulates TNF-alpha induced expression of IL-8 gene in cystic fibrosis IB3-1 cells.

Corilagin (beta-1-O-galloyl-3,6-(R)-hexahydroxydiphenoyl-d-glucose), a gallotannin identified in several plants, including Phyllanthus urinaria, has been shown to exhibit versatile medicinal activities. As far as possible anti-inflammatory effects of corilagin, only few reports are available, and the potential use of corilagin as possible therapeutic molecule for cystic fibrosis has not been evaluated. In the present paper we report experiments aimed at determining the activity of corilagin on nuclear factor kappaB (NF-kappaB) binding to DNA target and on the expression of the major pro-inflammatory gene involved in cystic fibrosis, interleukin-8 (IL-8). Both IL-8 mRNA content and IL-8 protein secretion were analyzed in cystic fibrosis bronchial IB3-1 cells stimulated by tumor necrosis factor-alpha (TNF-alpha), one of the most potent pro-inflammatory agents. The data obtained demonstrate that corilagin binds to NF-kappaB, inhibits NF-kappaB/DNA interactions and affects IL-8 gene expression in TNF-alpha treated IB3-1 cells. In addition, corilagin inhibits TNF-alpha induced secretion of MCP-1 and RANTES, exhibiting low or no effect on the release of G-CSF, IL-6 and VEGF. Therefore, corilagin might be of interest for experimental anti-inflammatory therapy of cystic fibrosis.

Synthesis of 9,9-dialkyl-4,5-diazafluorene derivatives and their structure-activity relationships toward human carcinoma cell lines.

A homologous set of 9,9-dialkyl-4,5-diazafluorene compounds were prepared by alkylation of 4,5-diazafluorene with the appropriate alkyl bromide and under basic conditions. The structures of these simple organic compounds were confirmed by spectroscopic techniques (FTIR, NMR, and FABMS). Their biological effects toward a panel of human carcinoma cells, including Hep3B hepatocellular carcinoma, MDAMB-231 breast carcinoma, and SKHep-1 hepatoma cells, were investigated; a structure-activity correlation was established with respect to the length of the alkyl chain and the fluorene ring structure. The relationship between the mean potency [log(1/IC(50))] and alkyl chain length was systematically studied. The results show that compounds with butyl, hexyl, and octyl chains exhibit good growth inhibitory effects toward these three human carcinoma cell lines, and the 9,9-dihexyl-4,5-diazafluorene further exhibits antitumor activity in athymic nude mice Hep3B xenograft models. For the structurally related dialkylfluorenes that lack the diaza functionality, in vitro cytotoxicity was not observed at clinically relevant concentrations.

Cosmetic textiles with biological benefits: gelatin microcapsules containing vitamin C.

In recent years, textile materials with special applications in the cosmetic field have been developed. A new sector of cosmetic textiles is opened up and several cosmetic textile products are currently available in the market. Microencapsulation technology is an effective technique to control the release properties of active ingredients that prolong the functionality of cosmetic textiles. This study discusses the development of cosmetic textiles and addresses microencapsulation technology with respect to its historical background, significant advantages, microencapsulation methods and recent applications in the textile industry. Gelatin microcapsules containing vitamin C were prepared using emulsion hardening technique. Both the optical microscopy and scanning electron microscopy demonstrated that the newly developed microcapsules were in the form of core-shell spheres with relatively smooth surface. The particle size of microcapsules ranged from 5.0 to 44.1 microm with the average particle size being 24.6 microm. The gelatin microcapsules were proved to be non-cytotoxic based on the research findings of the toxicity studies conducted on human liver and breast cell lines as well as primary bone marrow culture obtained from patient with non-malignant haematological disorder. The gelatin microcapsules were successfully grafted into textile materials for the development of cosmetic textiles.

The preparation and in vitro antiproliferative activity of phthalimide based ketones on MDAMB-231 and SKHep-1 human carcinoma cell lines.

The 'one pot' condensation reaction for the synthesis and potent antiproliferative inhibition of alpha-phthalimide based ketones is reported here. 2-Phthalimide-1-(4-fluoro-phenyl)ethanone (5) showed the best growth inhibition on human MDAMB-231 breast carcinoma and SKHep-1 hepatoma cell lines. Preliminary studies showed that the reported bioactivity may be due to the presence of strong electronegative fluorine group at the para-position of the aryl ring.

Phyllanthus urinaria extract attenuates acetaminophen induced hepatotoxicity: involvement of cytochrome P450 CYP2E1.

Acetaminophen is a commonly used drug for the treatment of patients with common cold and influenza. However, an overdose of acetaminophen may be fatal. In this study we investigated whether mice, administered intraperitoneally with a lethal dose of acetaminophen, when followed by oral administration of Phyllanthus urinaria extract, may be prevented from death. Histopathological analysis of mouse liver sections showed that Phyllanthus urinaria extract may protect the hepatocytes from acetaminophen-induced necrosis. Therapeutic dose of Phyllanthus urinaria extract did not show any toxicological phenomenon on mice. Immunohistochemical staining with the cytochrome P450 CYP2E1 antibody revealed that Phyllanthus urinaria extract reduced the cytochrome P450 CYP2E1 protein level in mice pre-treated with a lethal dose of acetaminophen. Phyllanthus urinaria extract also inhibited the cytochrome P450 CYP2E1 enzymatic activity in vitro. Heavy metals, including arsenic, cadmium, mercury and lead, as well as herbicide residues were not found above their detection limits. High performance liquid chromatography identified corilagin and gallic acid as the major components of the Phyllanthus urinaria extract. We conclude that Phyllanthus urinaria extract is effective in attenuating the acetaminophen induced hepatotoxicity, and inhibition of cytochrome P450 CYP2E1 enzyme may be an important factor for its therapeutic mechanism.