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37, 63.10, 55.37 % inhibition of Nitric oxide, IL-6, TNF-α respectively.
Our study demonstrated the anti-inflammatory action of 3-Acetylmyricadiol and can serve as a potential candidate in the development of the clinically efficient anti-inflammatory molecule.
Our study demonstrated the anti-inflammatory action of 3-Acetylmyricadiol and can serve as a potential candidate in the development of the clinically efficient anti-inflammatory molecule.Tumor-associated macrophages (TAMs) are M2 phenotype dominant and promote tumor growth and metastasis. The new cancer treatment strategy includes TAM targeting and is aimed primarily at reprogramming TAMs toward the M1 phenotype or reducing the number and activity of M2 macrophages. Honokiol inhibitor Several marine invertebrate-derived drugs, combining efficacy and a low level of side effects, were approved for use in the cancer therapy. The mechanisms of action of some of them include TAM targeting. The review includes data showing immunomodulatory properties of these already approved anticancer drugs and drug candidates in clinical development which additionally incorporate data from screening studies of new substances from marine invertebrates. Based on screening data, the most promising marine compounds for cancer immunotherapy are supposed.
Amphotericin B (AMB) is water-insoluble polyene, which has a broad spectrum of antifungal activity. The hydrophobic drug only exits in the phospholipid bilayer, leading to a low-drug liposomal loading capacity.
This study is designed to prepare water-soluble inclusion complex (IC) between AMB and cyclodextrin (CD) to formulate liposomal vesicles, double-loaded with drug molecules in the phospholipid bilayer and AMB/CD IC in the aqueous core.
Water-soluble AMB/CD IC was prepared by pH adjustment of the aqueous media and consequently characterized by scanning electron microscopy (SEM) and differential scanning calorimetry (DSC). Liposomes double-loaded with AMB were formulated by the thin-film hydration method and accordingly evaluated for vesicle size, polydispersity index, entrapment efficiency, zeta potential and in vitro drug leakage.
Hydroxypropyl β cyclodextrin (HP-β-CD) better solubilized AMB than both α-CD and β-CD e.g, the concentration of water-soluble AMB/HP-β-CD IC could reach 465 µg/mL. Both DSC and SEM data illustrated that the drug no longer existed in its crystalline form, a in AMB/HP-β-CD IC. Liposomes double-loaded with hydrophilic AMB/HP-β-CD IC and hydrophobic AMB had a diameter of 270 nm, polydispersity index less than 0.27 and zeta potential ca. - 42.8 mV. Moreover, liposomes double loaded with AMB enhanced drug-liposomal loading capacity by 25%, less leaked drug in phosphate buffer pH 7.4 at 37oC in comparison to liposomes loaded with only hydrophobic AMB.
Liposomes double loaded with AMB and AMB/HP-β-CD IC increased drug-encapsulation ability and in vitro stability, suggesting potential drug delivery systems.
Liposomes double loaded with AMB and AMB/HP-β-CD IC increased drug-encapsulation ability and in vitro stability, suggesting potential drug delivery systems.
Tamoxifen is widely used for treatment of estrogen receptor positive breast cancer. It is, however, associated with severe side effects of cancerous proliferation on uterus endometrium. The tumor targeting formulation strategies can effectively overcome drug side effects of tamoxifen and provide safer drug treatment.
Designing tumor targeted PLGA nanoparticles of tamoxifen by attaching hyaluronic acid (HA) as ligand to actively target the CD44 receptors present at breast cancer cells surface.
PLGA-PEG-HA conjugate was synthesized in the laboratory and its tamoxifen loaded nanoparticles were fabricated and characterized by FTIR, NMR, DSC, and XRD analysis. Formulation optimization was done by Box- Behnken design using Design Expert software. The formulations were evaluated for in- vitro drug release and cytotoxic effect on MCF-7 cell lines.
The particle size, PDI, and drug encapsulation efficiency of optimized nanoparticles were 294.8, 0.626, and 65.16% respectively. Optimized formulation showed 9.56 %f CD44 receptors of cell lines to HA ligand present in nanoparticles.Targeting inhibitory receptors on T cells in the tumor sites can promote effective anti-tumor immunity in bladder cancer. Unfortunately, the main dilemma is that a large number of patients remain refractory to CTLA-4, PD-1, and PD-L1 blockade therapies. T-cell immunoglobulin and mucin domain 3 (Tim-3) is an inhibitory receptor expressed on T cells and innate immune cells. Both in vivo and in vitro data from patients with advanced cancers support the role of Tim-3 inhibition in satisfactory anti-tumor immunity. In bladder cancer, the expression level of Tim-3 significantly increases with advanced pathological grade and T stage. Therefore, rationality implies that designing novel monoclonal antibodies reactive with Tim-3 alone or in combination with other checkpoint inhibitors may indicate a favorable response in bladder cancer. Here, we aimed to investigate the possibility of targeting Tim-3 as a novel anti-cancer treatment for bladder cancer.The prevalence of neurological disorders such as anxiety, depression, Parkinson's disease and Alzheimer disease is increasing worldwide. Although exact mechanism is not clear but various factors and mechanism are involved in their pathogenesis. One of the major factors is diet which contributes to disease occurrence by stimulation of gut brain axis. This crosstalk between gut brain axis is not only involved in regulating gastrointestinal homeostasis but also influence behavior, motivation and cognitive function. Therefore, there is a significant need to explore this vast area, gut brain axis and its association with neurological disorders. It is well known fact that commonly prescribed antibiotics are responsible for dysbiosis on other hand food like probiotics are beneficial for maintain diversity of microbiome. In this review, we have compiled the reports and evidences that link gut brain axis to different neurological disorders as it will be helpful in identifying potential novel therapeutic drug targets. The effect of both western and healthy diet has been discussed which could be beneficial for encouraging people to opt for a healthy lifestyle.
Here's my website: https://www.selleckchem.com/products/Honokiol.html
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