- Delivery of oxaliplatin to colorectal cancer cells by folate-targeted UiO-66-NH2
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Oxaliplatin is being used in different malignancies and several side effects are reported for patients taking Oxaliplatin, including peripheral neuropathy, nausea and vomiting, diarrhea, mouth sores, low blood counts, fatigue, loss of appetite, etc. Here we have developed a targeted anticancer drug delivery system based on folate-conjugated amine-functionalized UiO-66 for the delivery of oxaliplatin (OX). UiO-66-NH2 (U) and UiO-66-NH2–FA(FU) were pre-functionalized by the incorporation of folic acid (FA) into the structure via coordination of the carboxylate group of FA. The FTIR spectra of drug-loaded U and FU showed the presence of new carboxylic and aliphatic groups of OX and FA. Powder X-ray diffraction (PXRD) patterns were matched accordingly with the reference pattern and FESEM results showed semi-spherical particles (115–128 nm). The evaluated amounts of OX in U and FU were calculated 304.5 and 293 mg/g, respectively. The initial burst release of OX was 15.7% per hour for U(OX) and 10.8% per hour for FU(OX). The final release plateau gives 62.9% and 52.3% for U(OX) and FU(OX). To evaluate the application of the prepared delivery platform, they were tested on colorectal cancer cells (CT-26) via MTT assay, cell migration assay, and spheroid model. IC50 values obtained from MTT assay were 21.38, 95.50, and 18.20 μg/mL for OX, U(OX), and FU(OX), respectively. After three days of treatment, the CT26 spheroids at two doses of 500 and 50 μg/mL of U(OX) and FU(OX) showed volume reduction. Moreover, the oxidative behavior of the prepared systems within the cell was assessed by total thiol, malondialdehyde, and superoxide dismutase activity. The results showed that FU(OX) had higher efficacy in preventing the growth of CT-26 spheroid, and was more effective than oxaliplation in cell migration inhibition, and induced higher oxidative stress and apoptosis.
- Hashemzadeh, Alireza,Amerizadeh, Forouzan,Asgharzadeh, Fereshteh,Darroudi, Majid,Avan, Amir,Hassanian, Seyed Mahdi,Landarani, Mohammad,Khazaei, Majid
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- Synthesis of bis(propargyl) aromatic esters and ethers: A potential replacement for isocyanate based curators
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This study reports the synthesis and characterization of a novel class of non-isocyanate curing agents based on bis-propargyl aromatic esters 2a-e and ethers 4a-c. A total of eight non-isocyanate curators were prepared from the reaction of respective dicarboxy or dihydroxybenzene with propargyl bromide in the presence of potassium carbonate with good yields. The structure and purity of the synthesized compounds and the corresponding intermediates were confirmed by spectral (IR and NMR), thermal (DSC) and chromatographic techniques (HPLC & GC-MS). Furthermore, kinetics of the curing reaction between glycidyl azide polymer (GAP) and the synthesized alkynes (4b, 4c) were studied using time-resolved FT-IR spectroscopy as a function of time at 303, 323 and 333 K. It was found that the curing reaction was faster when the temperature was increased. Kinetic parameters of the curing reaction, such as the reaction order and activation energy, were calculated for the GAP-4a and GAP-4c systems. All the curing reactions followed first order kinetics and the corresponding activation energy of the curing reaction for the systems was found to be 15.56 and 13.22 kcal mol-1. For comparison, curing studies were performed for GAP with a conventional curator Desmodur N-100. GAP cured with non-isocyanate curators offered good mechanical properties compared to GAP cured with isocyanate (N-100). The advantage of these new curing systems is that they do not require catalyst and there is no need for specific environmental conditions. Based on these studies, 1,4-bis(2-propynyloxy)benzene (4b) has the most potential as a non-isocyanate curator for azide polymeric binders.
- Sonawane, Sanjeevani H.,Anniyappan,Athar, Javaid,Banerjee, Shaibal,Sikder, Arun K.
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p. 8495 - 8502
(2016/02/05)
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- B b for alcoholysis of polyethylene method of preparation of diazonium salt waste polyester
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The invention relates to a method for preparing diazonium salt by depolymerizing waste polyester through ethylene glycol. The method is characterized by comprising the following technical steps of (1) depolymerizing the waste polyester through the ethylene glycol to obtain a product BHET (terephthalate) or PTA (p-phthalic acid); (2) nitrifying and reducing the depolymerized product; (3) performing diazotization. According to the method, the BHET or PTA is obtained by depolymerizing the waste polyester through the ethylene glycol, and the diazonium salt can be prepared by nitrification, reduction, diazotization and the like; the diazonium salt can generate reaction with a series of coupling components to prepare azo dyes, so that the waste polyester can be effectively recycled and reused.
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Paragraph 0038
(2017/01/26)
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- 18F-Labeled Benzyldiamine Derivatives as Novel Flexible Probes for Positron Emission Tomography of Cerebral β-Amyloid Plaques
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Early noninvasive visualization of cerebral β-amyloid (Aβ) plaques with positron emission tomography (PET) is the most feasible way to diagnose Alzheimer’s disease (AD). In this study, a series of flexible benzyldiamine derivatives (BDA) were proposed for
- Li, Zijing,Zhang, Xuran,Zhang, Xiaoyang,Cui, Mengchao,Lu, Jie,Pan, Xiaodong,Zhang, Xianzhong
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p. 10577 - 10585
(2016/12/16)
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- Chemical recycling of waste poly(ethylene terephthalate) fibers into azo disperse dyestuffs
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In this study, waste poly(ethylene terephthalate) (PET) fibers were chemically recycled into azo disperse dyestuffs. First, waste PET fibers were glycolytically degraded by excess ethylene glycol utilizing zinc acetate dehydrate as a catalyst. The glycolysis product, bis(2-hydroxyethyl) terephthalate (BHET), was purified through recrystallization and hydrolyzed into terephthalic acid (TPA). Thereafter, BHET and TPA were nitrated, reduced and azotized to obtain diazonium salts. Finally, the obtained diazonium salts were coupled with N,N-dimethylaniline to obtain azo disperse dyestuffs (dye A and dye B, respectively). The depolymerized products (BHET and TPA) and azo disperse dyestuffs (dyes A and B) were characterized by FTIR and 1H NMR spectroscopy. Nylon and polyester filaments were dyed with the synthesized azo dyestuffs with the dye bath pH ranging from 3.6 to 5.8. The performances of the dyestuffs were described by maximum absorption wavelength, K/S, L, a and b values. This journal is
- Li, Mengjuan,Huang, Yanhong,Yu, Tianshi,Chen, Shiming,Ju, Anqi,Ge, Mingqiao
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p. 46476 - 46480
(2014/12/10)
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- Inclusion complex containing epoxy resin composition for semiconductor encapsulation
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The invention is an epoxy resin composition for sealing a semiconductor, including (A) an epoxy resin and (B) a clathrate complex. The clathrate complex is one of (b1) an aromatic carboxylic acid compound, and (b2) at least one imidazole compound represented by formula (II): wherein R2 represents a hydrogen atom, C1-C10 alkyl group, phenyl group, benzyl group or cyanoethyl group, and R3 to R5 represent a hydrogen atom, nitro group, halogen atom, C1-C20 alkyl group, phenyl group, benzyl group, hydroxymethyl group or C1-C20 acyl group. The composition has improved storage stability, retains flowability when sealing, and achieves an effective curing rate applicable for sealing delicate semiconductors.
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- Preparation of phosphonoterephthalic acids via palladium-catalyzed coupling of aromatic iodoesters
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The current article reports in detail the preparation of two phosphonoterephthalic acids: 2-phosphonoterephthalic acid (1) and 2,5-diphosphonoterephthalic acid (2). Efficient, scalable syntheses have been developed for both compounds based on Pd-catalyzed
- Ivan, Nathaniel,Benin, Vladimir,Morgan, Alexander B.
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supporting information
p. 1831 - 1836
(2013/05/22)
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- Naaladase inhibitors for treating retinal disorders and glaucoma
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The present invention relates to pharmaceutical compositions and methods for treating a retinal disorder or glaucoma using NAALADase inhibitors.
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- Naaladase inhibitors for treating amyotrophic lateral sclerosis
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The present invention relates to pharmaceutical compositions and methods for treating amyotrophic lateral sclerosis using NAALADase inhibitors.
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- Benzenedicarboxylic acid derivatives
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New benzenedicarboxylic acid derivative compounds; pharmaceutical compositions, diagnostic methods, and diagnstic kits that include those compounds; and methods of using those compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-β activity, inhibiting angiogenesis, and treating glutamate abnormalities, neutopathy, pain, compulsive disorders, prostate diseases, cancers, and glaucoma.
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- Process for introducing a carboxyl group to an aromatic carboxylic acid or a derivative thereof
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Disclosed is a process for introducing a carboxyl group to an aromatic carboxylic acid or a derivative thereof, which comprises reacting a starting aromatic carboxylic acid, such as a benzoic acid, a biphenylcarboxylic acid, a naphthalenecarboxylic acid, a diphenylcarboxylic acid, or a derivative thereof, with a carbon tetrahalide in the presence of a cyclodextrin and an alkali metal hydroxide, thereby introducing a carboxyl group to the aromatic ring of the starting aromatic carboxylic acid or the derivative thereof in substitution for a hydrogen atom bonded thereto. By the process of the present invention, a desired aromatic polycarboxylic acid or a derivative thereof can be easily obtained with high selectivity.
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