Some bioactive component analysis of herbal capsules

Since the beginning of the evaluation of plants in terms of human health, the bioactivity properties of plants have been studied in the laboratory and thus standards have been brought to the treatment methods with plants. For this purpose, some bioactive component analyzes of 18 herbal capsules and 2 liquid herbal syrups produced by Naturin Company were performed in our current study. In this context, the total oxidant and antioxidant status of these plant mixtures were evaluated. The free radical capacities of the samples were determined by 1, 1-diphenyl-2-picrylhydrazil (DPPH) method and their DNA protective activities were determined using pBR322 plasmid DNA. Total antioxidant level (TAL) and Total oxidant level (TOL) activities were performed using Rel Assay diagnostic kit. All 3 of the stinging nettle samples showed DNA protective activity. The clean sample containing milk thistle extract also showed DNA Protective activity. In both the syrup samples (My guard and DTX-19) results were detected in the direction of positive protection on DNA. When the DPPH radical scavenging capacity was examined, it was determined that the best results were in juniper, nettle and thistle thistle samples, and the samples with syrup had a very good radical scavenging effect, and all of the samples showed antioxidant activity. This study is a preliminary and supportive study in order to elucidate the properties that can be used as drug active ingredients in traditional medicine, especially in the field of pharmacology.

Synthesis, Biological Activity, and Molecular Dynamics Study of Novel Series of a Trimethoprim Analogs as Multi-Targeted Compounds: Dihydrofolate Reductase (DHFR) Inhibitors and DNA-Binding Agents

Eighteen previously undescribed trimethoprim (TMP) analogs containing amide bonds (1–18) were synthesized and compared with TMP, methotrexate (MTX), and netropsin (NT). These compounds were designed as potential minor groove binding agents (MGBAs) and inhibitors of human dihydrofolate reductase (hDHFR). The all-new derivatives were obtained via solid phase synthesis using 4-nitrophenyl Wang resin. Data from the ethidium displacement test confirmed their DNA-binding capacity. Compounds 13–14 (49.89% and 43.85%) and 17–18 (41.68% and 42.99%) showed a higher binding affinity to pBR322 plasmid than NT. The possibility of binding in a minor groove as well as determination of association constants were performed using calf thymus DNA, T4 coliphage DNA, poly (dA-dT)2, and poly (dG-dC)2. With the exception of compounds 9 (IC50 = 56.05 µM) and 11 (IC50 = 55.32 µM), all of the compounds showed better inhibitory properties against hDHFR than standard, which confirms that the addition of the amide bond into the TMP structures increases affinity towards hDHFR. Derivatives 2, 6, 13, 14, and 16 were found to be the most potent hDHFR inhibitors. This molecular modelling study shows that they interact strongly with a catalytically important residue Glu-30.

Stability of plasmid pBR322 within Escherichia coli cells

nsertion of plasmids into the bacterial cells is of great significance especially in course of the transfer of drug resistance, virulence and other traits. Retention of plasmids within the host bacteria is therefore an important factor for bacterial homeostasis. Current study inferred the pBR322 plasmid stability within the Escherichia coli competent cells. The calcium chloride heat shock method was used for the transformation purpose. The plasmid retention phenomenon was assessed through the replica plating. The results positively showed the plasmid retention within E. coli.

Antioxidant Activity, Enzyme Inhibition Potentials, and Phytochemical Profiling of Premna serratifolia L. Leaf Extracts

Premna serratifolia, commonly known as Arogo in Tentena-Sulawesi, is a popular vegetable. As a promising herbal tea and food ingredient, further investigation is required to find the best knowledge for medicinal use of P. serratifolia leaves. This research investigated the antioxidant activity of the ethanol (EEPS) and water (WEPS) extracts of P. serratifolia leaves, based on their scavenging activities on DPPH radicals and their reducing capacities (CuPRAC, total antioxidant/phosphomolybdenum, and ferric thiocyanate reducing power assays). The DNA-protecting effect by EEPS was tested using pBR322 plasmid DNA against •OH radical-induced damage. The inhibition potentials of both extracts against several enzymes related to metabolic diseases (α-glucosidase, α-amylase, xanthine oxidase, and protease) were evaluated. The phytochemical analysis was conducted by an LC-QTOF-MS/MS technique. EEPS proved to be a better antioxidant and had higher phenolic content compared to WEPS. EEPS demonstrated a protective effect on DNA with recovery percentage linearly correlated with EEPS concentrations. Strong inhibition on α-glucosidase and α-amylase was observed for EEPS; however, EEPS and WEPS showed weak inhibitions on xanthine oxidase and protease. LC-QTOF-MS/MS analysis identified seven main components in EEPS, namely scroside E, forsythoside A and forsythoside B, lavandulifolioside, diosmin, nobilin D, campneoside I, and isoacteoside. These components may be responsible for the observed enzymes inhibitions and antioxidant properties. Premna serratifolia leaves can be an appropriate choice for the development of nutraceutical and drug preparations.

Radiosensitization by Gold Nanoparticles: Impact of the Size, Dose Rate, and Photon Energy

Gold nanoparticles (GNPs) emerged as promising antitumor radiosensitizers. However, the complex dependence of GNPs radiosensitization on the irradiation conditions remains unclear. In the present study, we investigated the impacts of the dose rate and photon energy on damage of the pBR322 plasmid DNA exposed to X-rays in the presence of 12 nm, 15 nm, 21 nm, and 26 nm GNPs. The greatest radiosensitization was observed for 26 nm GNPs. The sensitizer enhancement ratio (SER) 2.74 ± 0.61 was observed at 200 kVp with 2.4 mg/mL GNPs. Reduction of X-ray tube voltage to 150 and 100 kVp led to a smaller effect. We demonstrate for the first time that the change of the dose rate differentially influences on radiosensitization by GNPs of various sizes. For 12 nm, an increase in the dose rate from 0.2 to 2.1 Gy/min led to a ~1.13-fold increase in radiosensitization. No differences in the effect of 15 nm GNPs was found within the 0.85–2.1 Gy/min range. For 21 nm and 26 nm GNPs, an enhanced radiosensitization was observed along with the decreased dose rate from 2.1 to 0.2 Gy/min. Thus, GNPs are an effective tool for increasing the efficacy of orthovoltage X-ray exposure. However, careful selection of irradiation conditions is a key prerequisite for optimal radiosensitization efficacy.

Investigation of molecular mechanisms underlying tetracycline resistance in thermophilic Campylobacter spp. suggests that previous reports of tet(A)-mediated resistance in these bacteria are premature

The true prevalence of tet(A), which codes for a tetracycline efflux pump, in thermophilic Camplyobacter spp. requires clarification after reports emerged in Iran (2014) and Kenya (2016) of the novel detection of tet(A) in Campylobacter. During our investigation of antibiotic resistance mechanisms in a sample of Irish thermophilic Campylobacter broiler isolates, it was determined that 100% of tetracycline-resistant isolates (n = 119) harboured tet(O). Accessory tetracycline-resistance mechanisms were considered as tetracycline minimum inhibitory concentrations ranged from 4 to ≥ 64 mg/L. Primers previously reported for the detection of tet(A) in Campylobacter failed to produce an amplicon using a positive control strain (Escherichia coli K12 SK1592 containing the pBR322 plasmid) and a selection of Campylobacter isolates. Accordingly, we designed new tet(A)-targeting primers on SnapGene2.3.2 that successfully generated a 407 bp product from the positive control strain only. Further in silico analysis using BLASTn and SnapGene2.3.2 revealed that previously reported Campylobacter tet(A) sequences deposited on GenBank shared 100% homology with Campylobacter tet(O). We postulate that this gave rise to the erroneous report of a high tet(A) prevalence among a pool of Kenyan broiler Campylobacter isolates that were tested using primers designed based on these apparent tet(A) sequences. In conclusion, further work would be required to determine whether the homology between tet(A) potentially present in Campylobacter and known tet(A) genes would be sufficient to allow amplification using the primers designed in our study. Finally, the existence of tet(A) in thermophilic Campylobacter spp. remains to be demonstrated.

Synthesis, singlet oxygen generation and DNA photocleavage of β,β′-conjugated polycationic porphyrins

In this paper, three [Formula: see text],[Formula: see text]-conjugated cationic porphyrin compounds were designed and synthesized. The structure of the intermediates and desired porphyrins were confirmed by UV, IR, 1H NMR, MS and elemental analysis. The interaction modes between these porphyrins and ct-DNA were studied by UV-vis spectroscopy and fluorescence emission spectroscopy. The results showed that PCP 1 had an external binding mode with DNA at low DNA concentration and could intercalate DNA with the increase of concentration. PCP 2 interacted with DNA through an external binding mode, and PCP 3 could insert into DNA. The binding constants ([Formula: see text] between PCP1[Formula: see text]PCP3 and ct-DNA were calculated to be 8.41 × 104, 7.33 × 104 and 4.14 × 104 M[Formula: see text], respectively. The singlet oxygen (1O[Formula: see text] generation of PCP1[Formula: see text]PCP3 was determined by the 1,3-diphenylisobenzofuran (DPBF) method using tetrapyridylporphyrin (H2TMPyP) as a reference. The 1O2 generation rate of PCP1[Formula: see text]PCP3 followed the order of PCP2 >PCP1>H2TMPyP >PCP3. Subsequently, the photocleavage effect of porphyrins on pBR322 plasmid DNA was studied by gel electrophoresis. At 10.0 [Formula: see text]M, PCP1 and PCP2 could cleave DNA completely. At 2.0 [Formula: see text]M, the cleavage rate of DNA by PCP3 was 57.5%, which was significantly higher than that of H2TMPyP (38.8%). These results verified that the amount of cationic ions in the porphyrin structure could affect the binding modes of porphyrins with DNA and their cleavage ability of DNA.

10-Membered Azaenediyne Fused to a Benzothiophene through the Nicholas Macrocyclization: Synthesis and DNA Cleavage Ability

The Nicholas-type macrocyclization through NH-tosyl functional group has been found to be an efficient technique for the synthesis of a 10-membered azaenediyne system annulated with a benzothiophene. To compare the activity of azaenediyne synthesized with similar oxa- and carbocyclic enediynes the Bergman cyclization activation energies and the ability of enediynes to cleave DNA (pBR322 plasmid) were investigated. The order of reactivity predicted by DFT calculations (N-enediyne < C-enediyne < O-enediyne) was confirmed by DSC analysis data. Surprisingly azaenediyne was found to be more active in the DNA cleavage assay than the C-analogue.

The water soluble peripherally tetra-substituted zinc(ii), manganese(iii) and copper(ii) phthalocyanines as new potential anticancer agents

In this study, [2-(2-morpholin-4-ylethoxy)ethoxy] group substituted zinc(ii), manganese(iii) and copper(ii) phthalocyanines 2–4 and their water soluble derivatives 2a, 3a and 4a were synthesized and the interactions of compounds 2a, 3a and 4a with CT-DNA and supercoiled pBR322 plasmid DNA were investigated.