Screening potential antagonists of epidermal growth factor receptor from Marsdenia tenacissima via cell membrane chromatography model assisted by HPLC–ESI–IT–TOF–MS

Marsdenia tenacissima, or Tongguanteng in Chinese, is a traditional Chinese herb and has a broad application in clinical practice for its pharmacological effects of treating asthma, pneumonia, tonsillitis, pharyngitis tumors, etc. However, few studies have reported the screening of the active components of this medicine for tumor therapy. In this work, a two‐dimensional analytical system was developed to screen antagonists of epidermal growth factor receptor (EGFR) from M. tenacissima. A fraction was retained on the EGFR cell membrane chromatography (CMC) column, separated and identified as tenacissoside G (TG), tenacissoside H (TH) and tenacissoside I (TI) by two‐dimensional HPLC–IT–TOF–MS. Molecular docking and 3‐(4,5‐dimethyl‐2‐thiazolyl)‐2,5‐diphenyl‐2‐H‐tetrazolium bromide (MTT) assay were carried out to assess the activity of TS (including TG, TH and TI). Molecular docking results showed that the binding mode of TS on EGFR is similar to that of gefitinib. The MTT assay demonstrated that gefitinib and TS (especially TI) could inhibit the growth of EGFR highly expressed cell lines in a dose‐dependent manner in the range of 5–50 μmol/L. In conclusion, the two‐dimensional EGFR/CMC–HPLC–IT–TOF–MS system could be a useful approach in drug discovery from traditional Chinese medicines for searching for potential antitumor candidates.     

New nanomolar negative modulators of AMPA receptors

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Influence of the size and geometry of the anion binding pocket of sugar–urea anion receptors on chiral recognition

Three new chiral urea-type anion receptors were synthesized from aromatic diamines and 1-amino-1-deoxyglucose. The anion binding properties of these receptors were studied using chiral carboxylates derived from mandelic acid and three α-amino acids. We found that the size of the anion binding pocket played an important role in chiral recognition processes. The best results were obtained for 1,8-diaminoanthracene and α-amino acid anions.     

Perimidine-based synthetic receptors for determination of copper(II) in water solution

Perimidine-based chelators 1 and 2 were prepared, and their structures were confirmed by ¹H and ¹³C NMR, MS spectroscopy and elemental analysis. These compounds were studied as specific synthetic receptors for the recognition of transition metal ions. They exhibited high affinity and selectivity towards Cu(II) ions. The conditional binding constants, linear dynamic range and detection limit were determined by UV–vis spectroscopy. These parameters demonstrated high potential of the prepared synthetic receptors for the recognition and determination of Cu(II) ions. The minimum detectable concentrations of Cu(II) ions for the synthetic receptors 1 and 2 were 270 and 75 nM (R ² = 0.9915 and 0.9964) in aqueous medium (water/DMSO; 99:1 (v/v)), respectively.     

Covalent Organic Frameworks(COFs) for Sequestration of99TcO4–

Covalent organic frameworks(COFs), as a class of crystalline porous materials with periodic lattices and porous structures, have received extensive attention in the fields of gas storage and separation, energy storage, catalysis and optoelectronics and so on. However, COFs are still in their infancy in the field of nuclear waste treatment, especially for sequestration of long-live problematic radionuclides, such as ⁹⁹Tc. Battle of decontamination of pertechnetate(TcO₄^–), a main existence of ⁹⁹Tc under aerobic environments, is far from finished. In this review, recent progresses of COFs and some relative materials in the sequestration of pertechnetate, and perspective on surmounting the unmet issues are elucidated.     

UV–vis and fluorescence detection by receptors based on an isophthalamide bearing a phenylethynyl group

We have successfully prepared 5-(2-phenylethynyl)isophathalilc acid as a signaling unit and the corresponding derivatives for an anion receptor 2 and a barbiturate receptor 4. Receptor 2 showed characteristic UV–vis changes and dramatic fluorescence quenching upon the addition of anions and receptor 4 showed UV–vis and an OFF-ON fluorescence changes upon the addition of dibutylbarbituric acid based on the diphenylethyne moiety.     

LYVE-1 在甲状腺乳头状癌的表达和意义

目的 观察淋巴管透明质酸受体1（LYVE-1）的表达和癌周组织中淋巴管的生成情况在甲状腺恶性肿瘤的变化及转 移中的作用。方法 应用免疫组织化学和real-time PCR方法检测45 例甲状腺乳头状癌中央区、癌周边区和正常甲状腺组织中的LYVE-1及其mRNA 表达情况,并计算淋巴管密度（LVD）。结果 甲状腺乳头状癌周边区LVD 高于甲状腺乳头状癌中央区,而正常组织中很少见LYVE-1 阳性的微淋巴管;甲状腺乳头状癌周边区LVD 与淋巴结转移有密切关系（P＜0.05）。结论 LYVE-1是一种特异性较高的淋巴管内皮特异性标志物,对淋巴管生成促进甲状腺乳头状癌的淋巴结转移。     

Synthesis of New 1-Naphthol Aza Oxa Thia Crowns

Abstract

New dinaphthosulfide aza oxa thia crowns from 1-naphthol were prepared. At first, 2,2′-thiobis(1-hydroxynaphthalene) (a dinaphthol) was prepared from 1-naphthol. Then diester was prepared from the reaction of dinaphthol and methylchloroacetate. Aza crowns were synthesized from the reaction of diester and diamines (ethylene diamine, 1,3-diaminopropane, 1,4-diaminobutane, and 1,6-diaminohexane) in methanol.

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GRAPHICAL ABSTRACT      

Anion Receptor with Xylene Bridged Two Imidazolium Rings

A m-xylene bridged imidazolium receptor 1 has been designed and synthesized. The receptor 1 utilizes two imidazole (C–H)⁺—anion hydrogen bonds and one aromatic hydrogen—anion hydrogen bond. The major driving force of complexation between the receptor 1 and anions comes from two imidazole (C–H)⁺—anion hydrogen bonding. However, some hydrogen bonding energy between aromatic hydrogen and anion exists, although it is expected to be much smaller than that of imidazole (C–H)⁺—anion hydrogen bonds.