The influence of chain‐end functionalization and stereocomplexation on the degradation stability under alkaline condition

Author(s):  
Shin Asano ◽  
Jaeyeong Choi ◽  
Thi Hang Tran ◽  
Nalinthip Chanthaset ◽  
Hiroharu Ajiro
Keyword(s):  
Author(s):  
Junjian Li ◽  
Lianbao Ye ◽  
Yuanyuan Wang ◽  
Ying Liu ◽  
Xiaobao Jin ◽  
...  

Background: Spirocyclic indoline compounds widely exist in numerous natural products with good biological activities and some drug molecules in many aspects. In recent years, it has attracted extensive attention as potent anti-tumor agents in the fields of pharmacology and chemistry. Objective: In this study, we focused on designing and synthesizing a set of novel 1'-H-spiro[indole-3,4'-piperidine] derivatives, which were evaluated by preliminary bioactivity experiment in vitro and molecular docking. Method: The key intermediate 1'-methylspiro[indoline-3,4'-piperidine] (B4) reacted with benzenesulfonyl chloride with different substituents under alkaline condition to obtain its sulfonyl derivatives (B5-B10). We evaluated their antiproliferative activities against A549, BEL-7402 and HeLa cells by MTT assay. We performed the CDOCKER module in Discovery Studio 2.5.5 software for molecular modeling of compound B5, and investigated the binding of compound B5 with the target proteins from PDB database. Results: The results indicated that compounds B4-B10 exhibited good antiproliferative activities against the above three types of cells, in which compound B5 with chloride atom as electron-withdrawing substituent on a phenyl ring showed the highest potency against BEL-7402 cells (IC50=30.03±0.43 μg/mL). By binging of the prominent bioactive compound B5 to CDK, c-Met, EGFR protein crystals, The binding energy of B5 with these three types receptors are -44.3583 kcal/mol, - 38.3292 kcal/mol, -33.3653 kcal/mol respectively. Conclusion: Six 1'-methylspiro[indoline-3,4'-piperidine] derivatives were synthesized and evaluated against BEL-7402, A- 549, HeLa cell lines. Compound B5 showed significant inhibition on BEL-7402 cell lines. Molecular docking revealed that B5 showed good affinity by the good fitting between B5 and these three targets with amino acid residues in active sites which encourage us to conduct further evaluation such as the kinase experiment.


Nanomaterials ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 1007
Author(s):  
Azam Ali ◽  
Mariyam Sattar ◽  
Fiaz Hussain ◽  
Muhammad Humble Khalid Tareen ◽  
Jiri Militky ◽  
...  

The versatile one-pot green synthesis of a highly concentrated and stable colloidal dispersion of silver nanoparticles (Ag NPs) was carried out using the self-assembled tannic acid without using any other hazardous chemicals. Tannic acid (Plant-based polyphenol) was used as a reducing and stabilizing agent for silver nitrate in a mild alkaline condition. The synthesized Ag NPs were characterized for their concentration, capping, size distribution, and shape. The experimental results confirmed the successful synthesis of nearly spherical and highly concentrated (2281 ppm) Ag NPs, capped with poly-tannic acid (Ag NPs-PTA). The average particle size of Ag NPs-PTA was found to be 9.90 ± 1.60 nm. The colloidal dispersion of synthesized nanoparticles was observed to be stable for more than 15 months in the ambient environment (25 °C, 65% relative humidity). The synthesized AgNPs-PTA showed an effective antimicrobial activity against Staphylococcus Aureus (ZOI 3.0 mM) and Escherichia coli (ZOI 3.5 mM). Ag NPs-PTA also exhibited enhanced catalytic properties. It reduces 4-nitrophenol into 4-aminophenol in the presence of NaBH4 with a normalized rate constant (Knor = K/m) of 615.04 mL·s−1·mg−1. For comparison, bare Ag NPs show catalytic activity with a normalized rate constant of 139.78 mL·s−1·mg−1. Furthermore, AgNPs-PTA were stable for more than 15 months under ambient conditions. The ultra-high catalytic and good antimicrobial properties can be attributed to the fine size and good aqueous stability of Ag NPs-PTA. The unique core-shell structure and ease of synthesis render the synthesized nanoparticles superior to others, with potential for large-scale applications, especially in the field of catalysis and medical.


2018 ◽  
Vol 782 ◽  
pp. 21-26
Author(s):  
Takeshi Yabutsuka ◽  
Masaya Yamamoto ◽  
Shigeomi Takai ◽  
Takeshi Yao

We prepared hydroxyapatite (HA) capsules encapsulating maghemite particles. In order to evaluate enzyme immobilization behavior of the HA capsules under alkaline condition, we immobilized five kinds of enzymes with different isoelectric point in carbonate/bicarbonate buffer (CBB, pH 10.0). When the enzymes in CBB were moderately charged, immobilization efficiency on the HA capsules showed the highest value. It was suggested that immobilization efficiency was affected according to both pI of enzyme and pH of the surrounding solution and that enzyme immobilized on the HA capsules by not only electrical double layer interactions but also ion interaction and other interactions.


2011 ◽  
Vol 130-134 ◽  
pp. 856-859
Author(s):  
Chun Sheng Ding ◽  
Yang Ping Fu ◽  
Qian Fen Zhu ◽  
Jing Fu

In this experiment quartz sand was chosen as a carrier to be coated by aluminous salt under alkaline condition, and then the specific surface area was tested, and the adsorption capability and Cd2+ removal influencing factors of modified sand were studied. The investigation results showed that the specific surface area of modified sand was 75.244m2/g which was 9.38 times of that of original sand; the removal efficiency of Cd2+ by aluminous salt modified sand reached 59% contrast to 39% of original sand with pH 7.00. It was also found that the removal efficiency of Cd2+ by the aluminous salt modified sand was reduced with the increase of initial concentration of Cd2+ solution, and was enhanced with the increase of pH value, the Cd2+ removal efficiency was almost 71% with pH 9.0.


2016 ◽  
Vol 294 ◽  
pp. 49-57 ◽  
Author(s):  
Deli Wu ◽  
Yufan Chen ◽  
Zhiyong Zhang ◽  
Yong Feng ◽  
Yanxia Liu ◽  
...  

2009 ◽  
Vol 60 (5) ◽  
pp. 1341-1346 ◽  
Author(s):  
W. H. Kuan ◽  
C. Y. Hu ◽  
M. C. Chiang

A batch electrocoagulation (EC) process with bipolar electrode and potentiodynamic polarization tests with monopolar systems were investigated as methods to explore the effects of electrode materials and initial solution pH on the As(V) and As(III) removal. The results displayed that the system with Al electrode has higher reaction rate during the initial period from 0 to 25 minutes than that of Fe electrode for alkaline condition. The pH increased with the EC time because the As(V) and As(III) removal by either co-precipitation or adsorption resulted in that the OH positions in Al-hydroxide or Fe-hydroxide were substituted by As(V) and As(III). The pH in Fe electrode system elevate higher than that in Al electrode because the As(V) removal substitutes more OH position in Fe-hydroxide than that in Al-hydroxide. EC system with Fe electrode can successfully remove the As(III) but system with Al electrode cannot because As(III) can strongly bind to the surface of Fe-hydroxide with forming inner-sphere species but weakly adsorb to the Al-hydroxide surface with forming outer-sphere species. The acidic solution can destroy the deposited hydroxide passive film then allow the metallic ions liberate into the solution, therefore, the acidic initial solution can enhance the As(V) and As(III) removal. The over potential calculation and potentiodynamic polarization tests reveal that the Fe electrode systems possess higher over potential and pitting potential than that of Al electrode system due to the fast hydrolysis of and the occurrence of Fe-hydroxide passive film.


2015 ◽  
Vol 3 (4) ◽  
pp. 1500252 ◽  
Author(s):  
Jongsik Park ◽  
Jongchan Kim ◽  
Yoojin Yang ◽  
Donghwan Yoon ◽  
Hionsuck Baik ◽  
...  

2013 ◽  
Vol 781-784 ◽  
pp. 764-769
Author(s):  
Xue Kun Li ◽  
Xiu Na Chen ◽  
Fang Fang Chen ◽  
Wen Hong Li

The pigment was isolated fromfructus ligustri lucidi. The pigment belonges to flavonoid by color reaction and absorption spectrum analysis. The color scale was tested, with emphasis on the effects of pH, temperatures, sunlight, oxidizing agent, reducing agent, salt,vitamin C, preservative and sucrose on its stability. Results show that the color scale of yellow pigment fromfructus ligustri lucidiis 52.38. It is stable under acidic condition and degraded under alkaline condition. It has good heat and light resistance. The pigment has better endurance capability against oxidizing agent but reducing agent. The effects of salt and sucrose are relatively small.Vitamin Chas a certain increment on the color, but preservative would degrade the pigment. The study shows that yellow pigment has good stability and supports the application in the food industry.


2018 ◽  
Vol 206 (1) ◽  
pp. 61-68 ◽  
Author(s):  
L. Moharrery ◽  
M. Otadi ◽  
N. Miraly ◽  
M. M. Rezaei Zangeneh ◽  
R. Amiri
Keyword(s):  
Azo Dye ◽  

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