Iodine as a New Deoximating Agent

Iodine is found to he an effective and mild reagent for conversion of aldoximes and ketoximes to their parent carbonyl compounds.     

Bifunctional RNA-Targeting Deoxyribozyme Nanodevice as a Potential Theranostic Agent

Theranostic approaches rely on simultaneous diagnostic of a disease and its therapy. Here, we designed a DNA nanodevice, which can simultaneously report the presence of a specific RNA target through an increase in fluorescence and cleave it. High selectivity of RNA target recognition under near physiological conditions was achieved. The proposed approach can become a basis for the design of DNA nanomachines and robots for diagnostics and therapy of viral infections, cancer, and genetic disorders.     

An Imidazolium-Based Lipid Analogue as a Gene Transfer Agent

A dicationic imidazolium salt is described and investigated towards its application for gene transfer. The polar head group and the long alkyl chains in the backbone contribute to a lipid-like behavior, while an alkyl ammonium group provides the ability for crucial electrostatic interaction for the transfection process. Detailed biophysical studies regarding its impact on biological membrane models and the propensity of vesicle fusion are presented. Fluorescence spectroscopy, atomic force microscopy and confocal fluorescence microscopy show that the imidazolium salt leads to negligible changes in lipid packing, while displaying distinct vesicle fusion properties. Cell culture experiments reveal that mixed liposomes containing the novel imidazolium salt can serve as plasmid DNA delivery vehicles. In contrast, a structurally similar imidazolium salt without a second positive charge showed no ability to support DNA transfection into cultured cells. Thus, we introduce a novel and variable structural motif for cationic lipids, expanding the field of lipofection agents.     

A Portrait of the OPE as a Biological Agent

Oligophenylene ethynylenes, known as OPEs, are a sequence of aromatic rings linked by triple bonds, the properties of which can be modulated by varying the length of the rigid main chain or/and the nature and position of the substituents on the aromatic units. They are luminescent molecules with high quantum yields and can be designed to enter a cell and act as antimicrobial and antiviral compounds, as biocompatible fluorescent probes directed towards target organelles in living cells, as labelling agents, as selective sensors for the detection of fibrillar and prefibrillar amyloid in the proteic field and in a fluorescence turn-on system for the detection of saccharides, as photosensitizers in photodynamic therapy (due to their capacity to highly induce toxicity after light activation), and as drug delivery systems. The antibacterial properties of OPEs have been the most studied against very popular and resistant pathogens, and in this paper the achievements of these studies are reviewed, together with almost all the other roles held by such oligomers. In the recent decade, their antifungal and antiviral effects have attracted the attention of researchers who believe OPEs to be possible biocides of the future. The review describes, for instance, the preliminary results obtained with OPEs against severe acute respiratory syndrome coronavirus 2, the virus responsible for the COVID-19 pandemic.     

Approaches to an Yneamine Resin as a General-Purpose Condensing Agent

The synthetic utility and shortcomings of resins which activate carboxyl groups to form anhydrides, esters, or amides such as polycarbodiimide resins and poly-EEDQ resins are examined. The use of a polymer-bound yneamine function for such purposes is proposed, and synthetic approaches to this goal are described. Tentative evidence for the existence of a stable intermediate in the reaction of an insoluble yneamine with benzoic acid is also presented.     

Berberine as a Potential Anticancer Agent: A Comprehensive Review

Berberine (BBR), a potential bioactive agent, has remarkable health benefits. A substantial amount of research has been conducted to date to establish the anticancer potential of BBR. The present review consolidates salient information concerning the promising anticancer activity of this compound. The therapeutic efficacy of BBR has been reported in several studies regarding colon, breast, pancreatic, liver, oral, bone, cutaneous, prostate, intestine, and thyroid cancers. BBR prevents cancer cell proliferation by inducing apoptosis and controlling the cell cycle as well as autophagy. BBR also hinders tumor cell invasion and metastasis by down-regulating metastasis-related proteins. Moreover, BBR is also beneficial in the early stages of cancer development by lowering epithelial–mesenchymal transition protein expression. Despite its significance as a potentially promising drug candidate, there are currently no pure berberine preparations approved to treat specific ailments. Hence, this review highlights our current comprehensive knowledge of sources, extraction methods, pharmacokinetic, and pharmacodynamic profiles of berberine, as well as the proposed mechanisms of action associated with its anticancer potential. The information presented here will help provide a baseline for researchers, scientists, and drug developers regarding the use of berberine as a promising candidate in treating different types of cancers.     

A Maltol-Containing Ruthenium Polypyridyl Complex as a Potential Anticancer Agent

Cancer is one of the main causes of death worldwide. Chemotherapy, despite its severe side effects, is to date one of the leading strategies against cancer. Metal-based drugs present several potential advantages when compared to organic compounds and they have gained trust from the scientific community after the approval on the market of the drug cisplatin. Recently, we reported the ruthenium complex ([Ru(DIP)₂(sq)](PF₆) (where DIP is 4,7-diphenyl-1,10-phenantroline and sq is semiquinonate) with a remarkable potential as chemotherapeutic agent against cancer, both in vitro and in vivo. In this work, we analyse a structurally similar compound, namely [Ru(DIP)₂(mal)](PF₆), carrying the flavour-enhancing agent approved by the FDA, maltol (mal). To possess an FDA approved ligand is crucial for a complex, whose mechanism of action might include ligand exchange. Herein, we describe the synthesis and characterisation of [Ru(DIP)₂(mal)](PF₆), its stability in solutions and under conditions that resemble the physiological ones, and its in-depth biological investigation. Cytotoxicity tests on different cell lines in 2D model and on HeLa MultiCellular Tumour Spheroids (MCTS) demonstrated that our compound has higher activity than cisplatin, inspiring further tests. [Ru(DIP)₂(mal)](PF₆) was efficiently internalised by HeLa cells through a passive transport mechanism and severely affected the mitochondrial metabolism.     

TiO2 Nanotubes as a Therapeutic Agent for Cancer Thermotherapy

We report the photothermal properties as well as the in vitro cell test results of titanium oxide nanotubes (TiO₂ NTs) as a potential therapeutic agent for cancer thermotherapy in combination with near-infrared (NIR) light. TiO₂ NTs are found to have a higher photothermal effect upon exposure to NIR laser than Au nanoparticles and single-wall carbon nanotubes, which have also attracted considerable interest as therapeutic agents for cancer thermotherapy. The temperature increase of a TiO₂ NT/NaCl suspension during NIR laser exposure is larger than that of a TiO₂ NT/D.I. water suspension due to the heat generated by the formation of Na₂TiF_6. According to the in vitro cell test results the cells exposed to NIR laser without TiO₂ NT treatment have a cell viability of 96.4%. Likewise, the cells treated with TiO₂ NTs but not with NIR irradiation also have a cell viability of 98.2%. Combination of these two techniques, however, shows a cell viability of 1.35%. Also, the cell deaths are mostly due to necrosis but partly due to late apoptosis. These results suggest that TiO₂ NTs can be used effectively as therapeutic agents for cancer thermotherapy due to their excellent photothermal properties and high biocompatibility.     

Ethylene Sulfide Graft on Polyamine as a Nonfouling Anticorrosion Agent

Graft copolymers of ethylene sulfide on polyalkylenimines have been shown to be both corrosion inhibitors and antifoulants. Laboratory results were confirmed in a mill test in which iron equipment was used for scrubbing gas with aqueous ethanol-amine in order to remove carbon dioxide and hydrogen sulfide. Means have been found for controlling the solubility of the graft.     

1-Cyanoimidazole as a Mild and Efficient Electrophilic Cyanating Agent

A mild and high-yielding cyanating reaction of amine, sulfur, and carbanion nucleophiles is reported here using 1-cyanoimidazole as an electrophilic cyanating agent.     

Cebranopadol as a Novel Promising Agent for the Treatment of Pain

Opioids are used to treat pain, but despite their effectiveness, they possess several side effects such as respiratory depression, tolerance and physical dependence. Cebranopadol has been evaluated as a solution to this problem. The compound acts on the mu opioid receptor and the nociceptin/orphanin receptor and these receptors co-activation can reduce opioid side-effects without compromising analgesia. In the present review, we have compiled information on the effects of cebranopadol, its pharmacokinetics, and clinical trials involving cebranopadol, to further explore its promise in pain management.     

Polyphenol Oxidase as a Promising Alternative Therapeutic Agent for Cancer Therapy

Cancers have always been the most difficult to fight, the treatment of cancer is still not considered. Thus, exploring new anticancer drugs is still imminent. Traditional Chinese medicine has played an important role in the treatment of cancer. Polyphenol oxidase (PPO) extracted from Edible mushroom has many related reports on its characteristics, but its role in cancer treatment is still unclear. This study aims to investigate the effects of PPO extracted from Edible mushroom on the proliferation, migration, invasion, and apoptosis of cancer cells in vitro and explore the therapeutic effects of PPO on tumors in vivo. A cell counting kit-8 (CCK8) assay was used to detect the effect of PPO on the proliferation of cancer cells. The effect of PPO on cancer cell migration ability was detected by scratch test. The effect of PPO on the invasion ability of cancer cells was detected by a transwell assay. The effect of PPO on the apoptosis of cancer cells was detected by flow cytometry. Female BALB/c mice (18–25 g, 6–8 weeks) were used for in vivo experiments. The experiments were divided into control group, model group, low-dose group (25 mg/kg), and high-dose group (50 mg/kg). In vitro, PPO extracted from Edible mushroom significantly inhibited the proliferation, migration, and invasion capability of breast cancer cell 4T1, lung cancer cell A549, and prostate cancer cell C4-2, and significantly promoted the apoptosis of 4T1, A549, and C4-2. In vivo experiments showed PPO inhibitory effect on tumor growth. Collectively, the edible fungus extract PPO could play an effective role in treating various cancers, and it may potentially be a promising agent for treating cancers.     

以阿拉伯半乳聚糖为载体的磁共振成像造影剂的研究

合成了阿拉伯半乳聚糖修饰的DTPA钆配合物,用红外光谱、元素分析、ICP-AES等手段进行了表征,用竞争性方法研究了其在水溶液中的稳定性,测试了其在水中及BSA溶液中的弛豫性能,并进行了体内成像实验.结果表明,其弛豫效率是目前临床所用造影剂Gd-DTPA的1.5～2.0倍,对肝脏和肾脏MRI信号具有良好的增强效果,是比较好的潜在磁共振成像造影剂.     

Organotins as a Locking Agent in the Formation of Dinuclear Complexes

In this paper the synthesis and characterization of new heterobimetallic compounds with a ligand derived from diacetylpyridine, hydrazine and salicylaldehyde has been reported. The open end of the ligand was locked with R₂SnCl₂ followed by the insertion of a transition metal ion in the cavity thus formed by locking the ligand. These compounds are characterized by TGA/DSC, IR, ¹H and ¹³CNMR, electronic spectra, magnetic moment and conductivity measurements. The disappearance of ν(O–H) and appearance of ν(Sn–O) in the IR spectrum of the Sn(saldp)R₂ {where saldp = bis(salicylaldehydehydrazone)diacetylpyridine and R = –CH₃, –C₄H₉} suggests the complex formation with R₂SnCl₂. The IR spectra of the complexes exhibited a blue shift in ν(C=N) indicating coordination of the azomethine nitrogen. The complexes are non-electrolytes in DMSO. The ¹HNMR and ¹³CNMR spectra of the complexes are not much different from that of the free ligand except for the disappearance of the signal at 9 ppm due to phenolic protons. The methyl or butyl protons attached to the tin appear at their usual places. The TGA profile of the ligand and its mononuclear complexes exhibit a three-step pyrolysis, although the binuclear complexes decompose in two steps leaving behind tin oxide as the final product.     

Sorbic Acid as an Alkylating Agent

A kinetic study of the alkylating potential of the sorbic acid + NaOH and sorbic acid + KOH systems was performed in 7:3 (volume/volume) water + dioxane solvent mixtures. The following conclusions were drawn. First, the sorbic acid + sorbate system shows alkylating activity on the nucleophile 4-(p-nitrobenzyl)pyridine (NBP), which is used as a trap for alkylating agents having nucleophilic characteristics similar to DNA bases. Second, the maximum alkylating capacity is observed in the pH = 5.0 to 6.5 range. Third, the alkylation reactions comply with the rate equation r=k _alk[H⁺][S][NBP]/(K _a +[H⁺]), with K _a being the dissociation constant of sorbic acid. Fourth, an enthalpy–entropy (ΔH ^#/ΔS ^#) compensation effect for activation quantities is observed by comparing NBP alkylation reactions due to sorbic acid + NaOH, sorbic acid + KOH, as well as potassium sorbate + HCl mixtures. Fifth, the results may help to establish suitable expiration times for products preserved with sorbic acid.     

Magnolol as a Potential Anticancer Agent: A Proposed Mechanistic Insight

Cancer is a serious disease with high mortality and morbidity worldwide. Natural products have served as a major source for developing new anticancer drugs during recent decades. Magnolol, a representative natural phenolic lignan isolated from Magnolia officinali, has attracted considerable attention for its anticancer properties in recent years. Accumulating preclinical studies have demonstrated the tremendous therapeutic potential of magnolol via a wide range of pharmacological mechanisms against cancer. In this review, we summarized the latest advances in preclinical studies investigating anticancer properties of magnolol and described the important signaling pathways explaining its underlying mechanisms. Magnolol was capable of inhibiting cancer growth and metastasis against various cancer types. Magnolol exerted anticancer effects through inhibiting proliferation, inducing cell cycle arrest, provoking apoptosis, restraining migration and invasion, and suppressing angiogenesis. Multiple signaling pathways were also involved in the pharmacological actions of magnolol against cancer, such as PI3K/Akt/mTOR signaling, MAPK signaling and NF-κB signaling. Based on this existing evidence summarized in the review, we have conclusively confirmed magnolol had a multi-target anticancer effect against heterogeneous cancer disease. It is promising to develop magnolol as a drug candidate for cancer therapy in the future.     

Polymer-Supported Persulfonic Acid as Oxidising Agent

A polymer-supported persulfonic acid has been prepared and applied for the oxidation of carboxylic acids, ketones, olefins, and disulfide bonds of cystine and cystinyl peptides to their peracids, esters (lactones), epoxides and sulfonic acid derivatives respectively in good yields. The resin also effectively removed the formyl protection from formyl amino acids. Spent polymer was reactivated by simple reactions.     

Cross-Linked Polyvinylpyridine Supported Zinc Borohydride as a Highly Chemoselective Reducing Agent

Aldehydes are reduced in ethanol under reflux condition in high yelds. This reagent absolutely discriminates aldehydes from ketones.