Activity

Hydrophilic polymers that swell or dissolve in aqueous media can have the potential to prepare controlled/sustained dosage forms for weakly acidic, poorly soluble drugs.

The main objective of this study is to utilize Eudragit®E100 (EE) and Carbopol®971P NF (Cp) polymers and their salt forms in the preparation of a once-daily controlled-release matrix tablet for model drug, Ibuprofen (IB).

Combinations of the polymers in their base forms (EE)/(Cp) or their salt forms (EEHCl/CpNa) were compressed with (IB) into single layer matrix tablets, or otherwise into bilayer tablets. Dissolution profiles were constructed using three different consecutive stages (pH 1.2, 4.8, and 6.8).

It was found that the incorporation of (EEHCl) modified the release rates of (IB) from (Cp) based matrix tablets. However, a major enhancement of (IB) release rates occurred when the polymers were combined in their salt forms at a 11 ratio by weight. In addition, a bilayer tablet was prepared wherein a relatively rapidly disintegrating layer composed of polymers salts (EEHCl and CpNa), and a second layer containing only (Cp) polymer in its base form at a 12 weight ratio possessed excellent release properties, and mechanical strengths.

It was concluded that the prepared bilayer tablet could be of promise use in controlling the release rates of (IB) in an extended manner to allow once-daily administration with an improved pH-independent release behavior.

It was concluded that the prepared bilayer tablet could be of promise use in controlling the release rates of (IB) in an extended manner to allow once-daily administration with an improved pH-independent release behavior.Lectin acts as an effective tool for screening potential biomarkers and gives an indication of highly valued research. Lectin offers the advantage of having the ability to recognize carbohydrate moiety of glycoprotein, peptidoglycan, glycosides, glycopeptides, lipopolysaccharide, etc., aiding in the detection of a new cancer biomarker in most complex tissues and fluids. The unique specificity of lectin in detecting single anomalously expressed lectin-based glycosylation method that can often go down the line for future cancer biomarker. This article explores the different types of lectin, their sources, and possible application in masking the activity of ovarian cancer cell.

It has been suggested that hydroxychloroquine may have positive effects on LDL-C, HDL-C, and triglyceride levels; however, the hypolipidemic activities of this drug are still uncertain.

The aim of this meta-analysis of randomized controlled trials was to explore the effect of hydroxychloroquine on circulating lipid concentrations.

Randomized controlled trials examining the impact of hydroxychloroquine on lipid parameters were searched in PubMed, Web of Science, Scopus, and Google Scholar databases. Meta-analysis was performed using a random-effects model and sensitivity analysis through the leave one-out method.

Meta-analysis showed that patients receiving hydroxychloroquine therapy significantly decreased total cholesterol (WMD 0.18 mmol/L, 95% CI -0.28, -0.08, I2 = 6%, p = 0.0004), LDL-C (WMD -0.21 mmol/L, 95% CI -0.36, -0.06, I2 = 75%, p = 0.006), triglycerides (WMD -0.09 mmol/L, 95% CI -0.15, -0.04, I2 = 22%, p = 0.001), and non-HDL-C (WMD -0.28 mmol/L, 95% CI -0.45, -0.12, I2 = 0%, p = 0.0009), and increased HDL-C concentrations (WMD 0.03 mmol/L, 95% CI 0.00, 0.06, I2 = 0%, p = 0.03).

Our results suggest that hydroxychloroquine improves lipid parameters by reducing total cholesterol, LDL-C, triglycerides, non-HDL-C, and increasing HDL-C levels.

Our results suggest that hydroxychloroquine improves lipid parameters by reducing total cholesterol, LDL-C, triglycerides, non-HDL-C, and increasing HDL-C levels.

Spirooxindoles are privileged scaffolds in medicinal chemistry and were identified through Wang’s pioneering work as inhibitors of MDM2-p53 interactions.

To design and synthesize 2,6-diarylidenecyclohexanones and dispiro[oxindole-cyclohexanone]-pyrrolidines of potential antitumor effect.

Dispiro[oxindole-cyclohexanone]-pyrrolidines 6a-h were synthesized in a regioselective manner via 1,3-dipolar cycloaddition reaction of 2,6-diarylidenecyclohexanones 3a-h, isatin, and sarcocine. Compounds 6a-h were alkylated to give (7-10) a,b. All compounds were evaluated in vitro for their antitumor activity and cytotoxic selectivity against breast cancer cell lines (MCF-7, and MDA-MB-231), breast fibrosis cell line (MCF10a) and placental cancer cell line (JEG-3). Molecular modeling inside the MDM2 binding site was performed using AutoDock4.2.

Synthesized compounds showed antitumor activity comparable to tamoxifen, and compounds 3a,b,f,g, and 9a,b showed selective cytotoxicity against tumor cells but reduced toxicity toward MCF-10a cells. Molecular modelling shows that both classes of synthesized compounds are predicted to fit the deep hydrophobic cleft on the surface of MDM2 and mimic the interactions between p53 and MDM2.

The synthesized compounds have antitumor activity against MCF-7, MDA-MB-231, and JEG-3. Few compounds showed a selective cytotoxic effect and may have the potential to inhibit MDM2 and stimulate p53. Future medicinal chemistry optimization and mechanistic study will be conducted to enhance the inhibition effect of identified compounds and elucidate their mechanism of action.

The synthesized compounds have antitumor activity against MCF-7, MDA-MB-231, and JEG-3. Few compounds showed a selective cytotoxic effect and may have the potential to inhibit MDM2 and stimulate p53. Future medicinal chemistry optimization and mechanistic study will be conducted to enhance the inhibition effect of identified compounds and elucidate their mechanism of action.

Post-surgical adhesion is a common complication after abdominal or pelvic surgeries. Despite improvements in surgical techniques or the application of physical barriers, little improvements have been achieved. It causes bowel obstruction, pelvic pain, and infertility in women and has an adverse effect on the quality of life. Renin-Angiotensin System (RAS) is traditionally considered as a blood pressure regulator. However, recent studies also indicate that the RAS plays a vital role in other processes, including oxidative stress, fibrosis, proliferation, inflammation, and the wound healing process. Angiotensin II (Ang II) is the main upstream effector of the RAS that can bind to the AT1 receptor (ATIR). A growing body of evidence has revealed that targeting Angiotensin-Converting Enzyme Inhibitors (ACEIs), Angiotensin II type 1 Receptor Blockers (ARBs), and Direct Renin Inhibitors (DRIs) can prevent post-surgical adhesions. TPEN solubility dmso Here we provide an overview of the therapeutic effect of RAS antagonists for adhesion.