Notes

Mono- as well as dialdehyde of trehalose: fresh synthons to get ready trehalose bio-conjugates.
Conclusions At present there is limited evidence about the medical management of visual hallucinations. This case report suggests that cholinesterase inhibitors may be of benefit, even in the absence of clear parkinsonsian features, if the form and content of the VHs suggest dysfunction in cholinergic modulated attentional networks.This study aims to shed light on the phytochemical composition and the biological effect of two members of family Aizoaceae, Lampranthus glaucus and Lampranthus aurantiacus. Gas chromatography coupled to mass spectrometry (GC-MS) and high-performance liquid chromatography (HPLC) was used to investigate the lipoidal matter and the phenolic content, respectively. The MTT assay was used to evaluate the cytotoxic activity against MCF-7 (breast cancer), HepG2 (liver cancer) and HCT-116 (colorectal cancer) cell lines. The total phenolic acids and the total flavonoid content of L. glaucus were found to be higher than that of L. aurantiacus. Phytol, hexadecanoic acid, p-coumaric, ferulic and p- hydroxybenzoic acids were the major detected compounds. Both the petroleum ether and the ethyl acetate extracts of the two plants showed significant cytotoxic activity (IC50 ranging from 15to 27 µg/mL) against the tested cell lines compared to 5-fluorouracil used as a reference standard.Gastric cancer (GC) remains a major public health problem. Ursolic acid (UA) is reported to be effective in inhibiting GC; however, its low solubility and poor biocompatibility have greatly hindered its clinical application. Herein, an innovative reactive oxygen species (ROS)-sensitive UA dimeric prodrug is developed by coupling two UA molecules via a ROS-cleavable linkage, which can self-assemble into stable nanoparticles in the presence of surfactant. This new UA-based delivery system comprises the following major components (I) dimeric prodrug inner core that can achieve high drug-loading (55%, w/w) and undergo rapid and selective conversion into intact drug molecules in response to ROS; (II) a polyethylene glycol (PEG) shell to improve colloid stability and extend blood circulation, and (III) surface-modified internalizing RGD (iRGD) to increase tumor targeting. Enhancement of the antitumor effect of this delivery system was demonstrated against GC tumors in vitro and in vivo. This novel approach offers the potential for clinical applications of UA.The main culprit behind most cancers is the accumulation of reactive oxygen species. Glyoxal (GO) and methylglyoxal (MGO) are reactive intermediates created by food processing and they are precursors of advanced glycation end products (AGE) that cause glycative stress. We aimed to evaluate the relationship between AGE levels of healthy volunteers and treatment-naive patients diagnosed with colorectal cancer. The study consisted of patients diagnosed with colorectal cancer and healthy volunteers who underwent routine colonoscopy. The study was conducted with a total of 42 cases, 47.6% (n = 20) female. The ages of the participants in the study ranged from 41 to 82 years, and the mean was 60.57 ± 10.78 years. The GO and MGO values of the patient group were found to be significantly higher than those of the control group (p = 0.007, p = 0.001, respectively). The risk of colorectal cancer was 22 and 57 times higher in individuals with GO and MGO values above 1.25 μg/mL and 0.0095 μg/mL, respectively. The blood AGE level is closely related to diet, and it can be decreased through the appropriate improvement of diet. Thus, the measurement of AGE can be used to predict whether a person's nutrition is healthy or unhealthy and prevent increased risk of colorectal cancer.Quercetin-loaded nanosuspensions (Que-NSps) added metabolic inhibitors were evaluated as drug delivery system to promote the oral bioavailability of quercetin. Que-NSps were prepared respectively using d-alpha tocopherol acid polyethylene glycol succinate (TPGS) or Soybean Lecithin (SPC) as stabilizer. Trometamol On the basis, Piperine (Pip) or sodium oleate (SO) was, respectively, encapsulated in Que-NSps as phase II metabolic inhibitors. The resulting Que-NSps all displayed a mean particle size of about 200 nm and drug loading content was in the range of 22.3-27.8%. The release of quercetin from Que-NSps was slow and sustained. After oral administration of 50 mg/kg different Que-NSps, the levels of free quercetin in plasma were significantly promoted, the concentration of quercetin metabolites (isorhamnetin and quercetin 3-O-β-d-Glucuronide) were decreased. The absolute bioavailability was, respectively 15.55%, 6.93%, 12.38%, and 23.58% for TPGS-Que-NSps, TPGS-SO-Que-NSps, SPC-Que-NSps, and SPC-Pip-Que-NSps, and 3.61% for quercetin water suspension. SPC-Pip-Que-NSps turned out to an ideal nanocarrier combined nano drug delivery system together with metabolic inhibitor to promote oral absorption of quercetin.Daratumumab, pomalidomide, and dexamethasone (DPd) is an FDA-approved 3rd or later line of therapy for myeloma. However, as there are limited published data on the efficacy of 2nd-line DPd, we conducted a retrospective analysis (n = 33). Herein, we report our center's data for 2nd-line DPd. Our patient population had a high amount of high risk cytogenetics (45.5%). The overall response rate (ORR) was 84.9% with a 1-year Progression Free Survival (PFS) of 37.7%. In standard risk myeloma (n = 18), the ORR was 88.9% and 1-year PFS was 61.1% (95% CI 42.3-88.3%). In high risk myeloma (45.5%, n = 15), the ORR was 80% with a 1-year PFS of 7.3% (95% CI 1.1-47.9%). This suggests that the efficacy of 2nd-line DPd in myeloma with high risk cytogenetics should be further investigated.Introduction Blood coagulation factor XII (FXII) is an emerging and potentially safe drug target, which dysregulation is associated with thrombosis, hereditary angioedema, and (neuro)inflammation. At the same time, FXII-deficiency is practically asymptomatic. Industrial and academic institutions have developed a number of potential therapeutic agents targeting either FXII zymogen or its active form FXIIa for the treatment of thrombotic and inflammatory conditions associated with the activity of this enzyme.Areas covered A short overview of the FXII(a) structure and function, underlining its suitability as a drug target, is given. The article reviews patents reported over the last three decades on FXII(a)-targeting therapeutic agents. These agents include small molecules, proteins, peptides, oligonucleotides, siRNAs, and monoclonal antibodies.Expert opinion The performed analysis of patents revealed that many FXII(a) inhibitors are in the early preclinical stage, while several already showed efficacy in vivo animal models of thrombosis, sepsis, hereditary angioedema, and multiple sclerosis.
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