Naphthofuroquinone derivatives show strong antimycobacterial activities against drug-resistant Mycobacteria.

Tuberculosis, one of the world's major health problems, has become more serious due to the emergence of multi-drug resistant (MDR) and extensively drug-resistant (XDR) Mycobacterium tuberculosis (MTB). In this study, we performed three anti-MTB assays to evaluate the anti-mycobacterial activity of naphthofuroquinone derivatives against drug-resistant MTB. Among them, methyl 5-[2-(dimethylamino)ethoxy]-7,12-dioxo-7,12-dihydrodinaphtho[1,2-b:2',3'-d]furan-6-carboxylate (DFC2) exhibited strong anti-mycobacterial activity against MTB H37Ra, H37Rv and four drug-resistant MTB strains.

In vitro activity of (-)-deoxypergularinine, on its own and in combination with anti-tubercular drugs, against resistant strains of Mycobacterium tuberculosis.

Background: The increasing incidence of multidrug-resistant tuberculosis (MDR-TB) infections has created a need for new effective drugs that also target extensively drug-resistant tuberculosis (XDR-TB) and/or augment the activities of existing drugs against tuberculosis.

Aim: This study searched natural products for a new lead compound that targets MDR/XDR-TB.

Methods: An active compound was purified from the roots of Cynanchum atratum Bunge (Asclepiadaceae) after screening 1640 plant extracts, and its inhibitory effects against MDR/XDR strains and synergistic effects with existing anti-TB drugs were assessed using the resazurin, MGIT, and checkboard assays.

Antifungal Activity and Action Mechanism of Histatin 5-Halocidin Hybrid Peptides against Candida ssp.

The candidacidal activity of histatin 5 is initiated through cell wall binding, followed by translocation and intracellular targeting, while the halocidin peptide exerts its activity by attacking the Candida cell membrane. To improve antimicrobial activities and to understand the killing mechanism of two peptides, six hybrid peptides were designed by conjugating histatin 5 and halocidin. A comparative approach was established to study the activity, salt tolerance, cell wall glucan binding assay, cytotoxicity, generation of ROS and killing kinetics.

Antimycobacterial activity of methanolic plant extract of Artemisia capillaris containing ursolic acid and hydroquinone against Mycobacterium tuberculosis.

Objective: In order to protect against Mycobacterium tuberculosis (MTB) infection, novel drugs and new targets should be screened from the vast source of plants. We investigated the potentiality of the herbal plant of Artemisia capillaris extract (AC) against Mycobacterium tuberculosis.

Design: In this study, we isolated ursolic acid and hydroquinone by bio-activity guided fractionation from the methanol extracts of AC, and tested the inhibitory effects against several strains of MTB.

In vitro antituberculosis activity of diterpenoids from the Vietnamese medicinal plant Croton tonkinensis.

Diterpenoids from the Vietnamese medicinal plant Croton tonkinensis are rich in ent-kaurane, kaurane and the grayanane class and are valuable intermediate plant metabolites with different bioactivities. In this study, we report the antituberculosis activity of these diterpenoids against both susceptible and resistant strains of M. tuberculosis for the first time.

In vitro effect of ursolic acid on the inhibition of Mycobacterium tuberculosis and its cell wall mycolic acid.

Mycobacterium tuberculosis is a dangerous intracellular pathogen. In order to protect against mycobacterium infection, novel agents with anti-mycobacterial activity should be given emergency priority for evaluation. Ursolic acid (UA), a plant triterpenoid, shows promising bioactivities, including anti-mycobacterial potency.

Anti-Mycobacterial Activity of Tamoxifen Against Drug-Resistant and Intra-Macrophage Mycobacterium tuberculosis.

Recently, it has become a struggle to treat tuberculosis with the current commercial antituberculosis drugs because of the increasing emergence of multidrug-resistant (MDR) tuberculosis and extensively drug-resistant (XDR) tuberculosis. We evaluated here the antimycobacterial activity of tamoxifen, known as a synthetic anti-estrogen, against eight drug-sensitive or resistant strains of Mycobacterium tuberculosis (TB), and the active intracellular killing of tamoxifen on TB in macrophages. The results showed that tamoxifen had antituberculosis activity against drug-sensitive strains (MIC, 3.

Initial in vitro biocompatibility of a bone cement composite containing a poly-ε-caprolactone microspheres.

The biocompatibility of a reinforced calcium phosphate injectable bone substitute (CPC-IBS) containing 30% poly-ε-caprolactone (PCL) microspheres was evaluated. The IBS consisted of a solution of chitosan and citric acid as the liquid phase and tetracalcium phosphate (TTCP) and dicalcium phosphate anhydrous (DCPA) powder as the solid phase with 30% PCL microspheres. The surface of the CPC-IBS was observed by SEM, and analyzed by EDX profiles.

In vitro and in vivo evaluation of a macro porous β-TCP granule-shaped bone substitute fabricated by the fibrous monolithic process.

In this study, a new porous beta-tricalcium phosphate (β-TCP) granule was fabricated using the fibrous monolithic (FM) process and its in vitro biocompatibility and in vivo bone formation were evaluated. SEM micrograph images showed that MG-63 cells attached to the surfaces of the implant and were well proliferated. Cellular viability was as high as 75% in a50% extract dilution solution.

In vitro and in vivo evaluations of 3D porous TCP-coated and non-coated alumina scaffolds.

Both tricalcium phosphate (TCP) and alumina have been extensively studied and shown to have high biocompatibility. Tricalcium phosphate has improved biodegradability and a higher solubility than hydroxyapatite. In contrast, alumina (Al(2)O(3)) is almost completely inert at physiological conditions and has been used as a biomaterial due to its wear resistance, high surface finish, and excellent hardness.