Volume 75, Issue 9-10

Preamble Polymer-drug conjugates have been intensively investigated for several decades, and even though their clinical success still lags behind the promise many researchers have placed in them, they are a mainstay in the fields of polymer therapeutics or nanomedicine. For many in the field, the seminal perspective paper by Helmut Ringsdorf from 1975 marks the beginning of this field of research. With more than one thousand citations, this paper has indubitably affected and inspired generations of researchers in the field, including the author of this translation. However, it is not the first paper describing the concept of polymer-drug conjugates. Some twenty years earlier, Horst Jatzkewitz described in two outstanding articles probably the historically first polymer-drug conjugates, detailed its synthesis, characterization and even first in vivo experiments. The results, carefully re-interpreted through the eyes of a scientist of the 21st century, clearly highlight several issues that need to be taken into consideration when designing polymer-drug conjugates. However, despite the pioneering nature of this paper, it is all but forgotten by the scientific community. In the author’s opinion, Horst Jatzkewitz and these papers clearly did not receive the attention and praise they deserve. Whether this was because these paper were much ahead of it´s time, or because it was published in German language, or for some other reason, we cannot know. However, these papers are, in my opinion, an excellent piece of work that should be known more widely and available to students and experts world-wide, which is why the author decided to translate it. Also, to give some more context and to help understand some outdated terms or concepts, additional comments and explanations are added throughout. I hope that this will help for these papers to receive the attention I believe they deserve.

The purpose of this study is to purify the LpxA protein of Chlamydia trachomatis (Ct) and prepare the polyclonal antibody against LpxA protein, so as to lay a foundation for studying the function of LpxA protein. The LpxA gene was amplified by PCR. The expression plasmid pET28a-LpxA was constructed by using pET28a as the vector. The fusion protein containing 6 histidine tag was induced by IPTG and purified by Ni 2+ chromatography gel. The purified His-LpxA protein was used as an immunogen to immunize New Zealand rabbits subcutaneously through the back to prepare polyclonal antibody. Immunoblotting was used to detect the reaction between the antibody and His-LpxA. The determination of polyclonal antibody titer was detected by ELISA. The relative molecular weight of His-LpxA was 32.8 kDa, and it could be expressed in Escherichia coli. The purity of the purified protein was about 95%. After immunizing New Zealand rabbits, the antiserum was able to recognize the recombinant His-LpxA protein with a titer greater than 1:10240. In this study, LpxA protein was successfully purified and antiserum was prepared, which provided an experimental basis for studying the function of LpxA protein.

This study compared the capacity of propolis extract (PE) and thyme waste extract (TWE) to prevent the oxidation of oil in water (O/W) emulsion, as well as their impact on emulsion apparent viscosity (AV) in the presence of wheat germ and almond oils as lipid phase. For this, central composite design (CCD) and principal component analysis (PCA) were performed. Oxidation process was monitored by evaluating the formation of primary and secondary lipid oxidation products, at the same time the AV behavior was determined evaluating consistency index and flow behavior index. The results revealed that the increase of PE% and TWE% decreases TBARS (Thiobarbituric Acid Reactive Substances) and hydroperoxides formation. Viscosity increases with the rise of TWE% over (0.04%), whereas lower concentrations of PE% decreases it. Those results have been confirmed in the PCA analysis. TWE showed higher resistance to oxidation, although PE was more effective as antioxidant than TWE.

Bioactivity-guided phytochemical investigation of Cucumis bisexualis has led to the isolation of three new coumarin-aurone heterodimers ( 1 - 3 ), along with six aurone derivatives ( 4 - 9 ) were isolated from C. bisexualis for the first time. Their structures were determined by their extensive spectroscopic data and comparison with the values reported in the references. All isolated compounds ( 1 - 9 ) were evaluated for their hepatoprotective activities on human L-O2 cells, which compared with positive control of Bifendatatum. Among them, compounds 1 , 2 , and 7 exhibited moderate hepatoprotective activities to promote effects on the proliferation of L-O2 cells.

Caveolae are defined as 50–100 nm wide pits in the plasma membrane containing oligomeric caveolin proteins. They have been implicated in endocytosis (including phagocytosis), transcytosis, calcium signalling, and numerous other signal transduction events. Caveolin-1, a major structural component of caveolae, enhances Rab5 activity. In this study, we examined the effect of a synthetic cell-permeable peptide of the caveolin-1 scaffolding domain (CSD) on phagocytosis. Treatment with the CSD peptide increased Rab5 activity, Rab5-early endosome antigen 1 (EEA1) interaction, and phagocytosis of Escherichia coli . The results suggest that the synthetic cell-permeable CSD peptide is an activator of phagocytosis.

Using gas chromatography (GC) in conjunction with electron impact mass spectrometry and retention-time comparison, 94 compounds, ranging from 2-methyl-2-propenal to octadecanoic acid, were identified in the interdigital secretions of male and female black wildebeests, Connochaetes gnou (also known as the white-tailed gnu). The constituents of these secretions belong to many different compound classes, including hydrocarbons, alcohols, aromatics and aliphatic carbonyl compounds including carboxylic acids as well as carboxylic acid esters. Relatively small quantitative differences were found between the male and female interdigital secretions. It was concluded that these compounds probably do not play a significant role in territorial marking or in chemical communication between males and females of the species, but they could be involved in preserving the remarkably strong attachment between members of social subgroups in black wildebeest populations.

Inhibition of aromatase enzymes is very important in the prevention of estrogen-related diseases and the regulation of estrogen levels. Aromatase enzyme is involved in the final stage of the biosynthesis of estrogen, in the conversion of androgens to estrogen. The development of new compounds for the inhibition of aromatase enzymes is an important area for medicinal chemists in this respect. In the present study, new benzimidazole derivatives have been designed and synthesized which have reported anticancer activity in the literature. Their anticancer activity was evaluated against human A549 and MCF-7 cell lines by MTT assay. In the series, concerning MCF-7 cell line, the most potent compounds were the 4-benzylpiperidine derivatives 2c , 2g , and 2k with IC 50 values of 0.032 ± 0.001, 0.024 ± 0.001, and 0.035 ± 0.001 µM, respectively, compared to the reference drug cisplatin (IC 50  = 0.021 ± 0.001 µM). Then, these compounds were subject to further in silico aromatase enzyme inhibition assays to determine the possible binding modes and interactions underlying their activity. Thanks to molecular docking studies, the effectiveness of these compounds against aromatase enzyme could be simulated. Consequently, it has been found that these compounds can be settled very properly to the active site of the aromatase enzyme.

The world is facing, while writing this review, a global pandemic due to one of the types of the coronaviruses (i.e., COVID-19), which is a new virus. Among the most important reasons for the transmission of infection between humans is the presence of this virus active on the surfaces and materials. Here, we addressed important questions such as do coronaviruses remain active on the inanimate surfaces? Do the types of inanimate surfaces affect the activity of coronaviruses? What are the most suitable ingredients that used to inactivate viruses? This review article addressed many of the works that were done in the previous periods on the survival of many viruses from the coronaviruses family on various surfaces such as steel, glass, plastic, Teflon, ceramic tiles, silicon rubber and stainless steel copper alloys, Al surface, sterile sponges, surgical gloves and sterile latex. The impacts of environmental conditions such as temperature and humidity were presented and discussed. The most important active ingredients that can deactivate viruses on the surfaces were reported here. We hope that these active ingredients will have the same effect on COVID-19.

Two meta -xylyl linked tetrakis-benzimidazolium salts (L1-L2) as multidentate ligands and two respective silver complexes (C1 and C2) were synthesized. A multistep reaction was done at room temperature, starting with simple benzimidazole and alkyl halides, going through precursors and salt formation by reflux and finally in situ deprotonation of tetrabenzimidazolium salts with Ag 2 O to yield respective tetra-nuclear Ag(I)- N -heterocyclic Carbene (NHC) complexes. Propyl and butyl groups were bonded at the terminal positions of tetra-azolium open chain salts. Characterization of compounds was done by analytical and spectroscopic techniques. On the basis of spectroscopic data, a chemical structure with open chains having four Ag(I) ions sandwiched between NHC layers was established. Potential of synthesized complexes (C1 & C2) for wound contraction was evaluated and compared with standard wound contraction gel. Percentage wound contraction of both complexes was found very close to that of standard drug used in parallel.