2,3-Dihydroxypterodontic acid

Adsorption mechanism of 2,4-dichlorophenoxyacetic acid onto nitric-acid-modified activated carbon fiber.[Pubmed:28379070]

Environ Technol. 2018 Apr;39(7):895-906.

Adsorption by carbon materials is one of the relatively fast methods in present research, which is widely used in emergency events. Activated carbon fiber (ACF) modified by nitric acid (N-ACF) was studied in this research to determine the adsorption performance for 2,4-dichlorophenoxyacetic acid (2,4-D). Subsequently, influence factors, adsorption isotherm models, kinetics and thermodynamic were investigated in a batch system to realize this adsorption. Experimental results showed that ACF modified by 0.1M nitric acid had a better removal ability than 2,4-D. Removal rate of 2,4-D by N-ACF was greatly influenced by pH with the optimum pH at 2. The superiority of the Langmuir isotherm model in describing the adsorption equilibrium was revealed by correlation coefficients R2 (R2 >/= 0.997). Furthermore, adsorption kinetics was well described by pseudo-second-order model. The results of thermodynamic showed that adsorption was a spontaneous, endothermic process with randomness increasing. Additionally, surface structure properties of adsorbent were characterized by Scanning electron microscopy, Fourier transform infrared spectroscopy, Specific surface area analysis of Brunauer, Emmett and Teller and Boehm's titration. It turned out that the micropore structure and functional groups on N-ACF all can contribute to the removal of 2,4-D.

Sorafenib and 2,3,5-triiodobenzoic acid-loaded imageable microspheres for transarterial embolization of a liver tumor.[Pubmed:28373713]

Sci Rep. 2017 Apr 3;7(1):554.

Sorafenib (SOF; an angiogenesis inhibitor) and 2,3,5-triiodobenzoic acid (TIBA; a contrast agent for computed tomography imaging)-loaded poly(lactic-co-glycolic acid) (PLGA) microspheres (MSs) were fabricated. Embolization, drug delivery, and tracing the distribution of MSs for liver cancer therapy were accomplished with the developed MSs after their intra-arterial (IA) administration. SOF/TIBA/PLGA MSs with 24.8-28.5 microm mean diameters were prepared, and the sustained release of SOF from MSs was observed. Lower systemic exposure (represented as the area under the curve [AUC]) and maximum drug concentration in plasma (Cmax) values of the SOF/TIBA/PLGA MSs group (IA administration, 1 mg/kg) in the results of the pharmacokinetic study imply alleviated unwanted systemic effects (e.g., hand and foot syndrome), compared to the SOF solution group (oral administration, 10 mg/kg). In a rat hepatoma model, the increase of microvessel density (MVD) following arterial embolization (i.e., reactive angiogenesis) was partially limited by SOF/TIBA/PLGA MSs. This resulted in the SOF/TIBA/PLGA MSs group (IA administration, single dosing, 1 mg/kg) showing a smaller tumor size increase and viable tumor portion compared to the TIBA/PLGA MSs group. These findings suggest that a developed SOF/TIBA/PLGA MS can be a promising therapeutic system for liver cancer using a transarterial embolization strategy.

Automated synthesis of N-(2-[(18) F]Fluoropropionyl)-l-glutamic acid as an amino acid tracer for tumor imaging on a modified [(18) F]FDG synthesis module.[Pubmed:28370543]

J Labelled Comp Radiopharm. 2017 Jun 15;60(7):331-336.

N-(2-[(18) F]Fluoropropionyl)-l-glutamic acid ([(18) F]FPGLU) is a potential amino acid tracer for tumor imaging with positron emission tomography. However, due to the complicated multistep synthesis, the routine production of [(18) F]FPGLU presents many challenging laboratory requirements. To simplify the synthesis process of this interesting radiopharmaceutical, an efficient automated synthesis of [(18) F]FPGLU was performed on a modified commercial fluorodeoxyglucose synthesizer via a 2-step on-column hydrolysis procedure, including (18) F-fluorination and on-column hydrolysis reaction. [(18) F]FPGLU was synthesized in 12 +/- 2% (n = 10, uncorrected) radiochemical yield based on [(18) F]fluoride using the tosylated precursor 2. The radiochemical purity was >/=98%, and the overall synthesis time was 35 minutes. To further optimize the radiosynthesis conditions of [(18) F]FPGLU, a brominated precursor 3 was also used for the preparation of [(18) F]FPGLU, and the improved radiochemical yield was up to 20 +/- 3% (n = 10, uncorrected) in 35 minutes. Moreover, all these results were achieved using the similar on-column hydrolysis procedure on the modified fluorodeoxyglucose synthesis module.

2-Naphthoic acid ergosterol ester, an ergosterol derivative, exhibits anti-tumor activity by promoting apoptosis and inhibiting angiogenesis.[Pubmed:28377207]

Steroids. 2017 Jun;122:9-15.

Phytosterol is a natural component of vegetable oil and includes ergosterol (ER) and beta-sitosterol. In this study, three new ergosterol monoester derivatives were obtained from the reflux reaction with ergosterol, organic acids (furoic acid, salicylic acid, and 2-naphthoic acid), EDCI, and DMAP in dichloromethane. The chemical structures were defined by IR and NMR. On the basis of the results, 2-naphthoic acid ergosterol ester (NE) had the highest tumor inhibition rate and was selected to study anti-tumor activity and its mechanism at doses of 0.025mmol/kg and 0.1mmol/kg in H22-tumor bearing mice. Compared with ER, NE exhibited more stronger anti-tumor activity in vivo. Furthermore, biochemical parameters of ALT, AST, BUN, and CRE showed that NE had little toxicity to mice. NE significantly improved serum cytokine levels of IFN-gamma and decreased VEGF levels. Moreover, H&E staining, TUNEL assay, immunohistochemistry, and western blotting indicated that NE exhibited anti-tumor activity in vivo by promoting apoptosis and inhibiting angiogenesis. In brief, the present study provided a method to improve ER anti-tumor activity and a reference for a new anti-tumor agent.