Metal-based fluoroquinolone complexes are known as metalloantibiotics. Nowadays, these complexes represent a novel pathway to display a promising strategy to overcome antimicrobial resistance. Numerous studies have shown that metalloantibiotics can improve antimicrobial activity against antimicrobial resistance (AMR) compared to pure fluoroquinolones. With the purpose to evaluate the bio transformation and the mechanism of binding and the biological impact of metal-based antibiotics known to have high potency and low toxicity, in the present work two novel copper(II) complexes of fluoroquinolone antibiotic ciprofloxacin with two different amino acids with the formula [Cu (Cip)(Gly)Cl]·2H2O (1) and [Cu (Cip)(Phe)Cl]·2H2O (2), where Cip, Gly, and Phe are ciprofloxacin, glycine, and phenylalanine, respectively. The synthesized complexes have been characterized using elemental analysis, mass, and FTIR spectroscopy. The binding properties of the complexes (1) and (2) with calf thymus DNA (CT-DNA) and bovine serum albumin (BSA) were analyzed by UV-vis spectroscopy, and the calculated binding constants (Kb) for complexes (1) and (2) show a strong binding to CT-DNA (Kb value for complex (1) was 5.98×103M-1 and for complex (2) was 1.5×104M-1 less strong binding affinity was reported for binding to BSA (Kb value for complex (1) was 1.98×103M-1 and for complex (2) was 8.3×103M-1). Thermal denaturation, gel electrophoresis, and viscosity measurements were performed to assess the binding interactions of complexes (1) and (2) with CT-DNA. The results indicate that both complexes exhibit an intercalative binding mode with CT-DNA. In addition, their antimicrobial, antitumor, antioxidant, cell cycle distribution (via flow cytometry), apoptosis, and antiviral activities were evaluated in vitro.

The objective of this research was to investigate the effect of bulking agents on the maturity and gaseous emissions of composting kitchen waste. The composing experiments were carried out by selected core bacterial agents and universal bacterial agents for 20 days. The results demonstrated that the addition of core microbial agents effectively controlled the emission of typical odor-producing compounds. The addition of core and universal bacterial agents drastically reduced NH3 emissions by 94% and 74%, and decreased H2S emissions by 78% and 27%. The application of core microbial agents during composting elevated the peak temperature to 65 °C and in terms of efficient temperature evolution (>55 °C for 8 consecutive days). The organic matter degradation decreased by 65% from the initial values for core microbial agents were added, while for the other treatments the reduction was slight. Adding core microbial agents to kitchen waste produced mature compost with a higher germination index (GI) 112%, while other treatments did not fully mature and had a GI of <70%. Microbial analysis demonstrated that the core microbial agents in composting increased the relative abundances of Weissella, Ignatzschineria, and Bacteroides. Network and redundancy analysis (RDA) revealed that the core microbial agents enhanced the relationship between bacteria and the eight indicators (p < 0.01), thereby improving the bio transformation of compounds during composting. Overall, these results suggest that the careful selection of appropriate inoculation microorganisms is crucial for improved biological transformation and nutrient content composting efficacy of kitchen waste.

Indian Journal of Natural Products,2022,36,1,39-43.DOI:10.5530/ijnp.2022.1.6Published:February 2023Type:Original ArticleAuthors:Ch. Raja Shekar, Ajmera Rama Rao, Umesh K Patil, and Ciddi Veeresham Author(s) affiliations:Ch. Raja Shekar1, Ajmera Rama Rao1, Umesh K Patil2, Ciddi Veeresham1,* 1University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Telangana, INDIA. 2Department of Pharmaceutical Sciences, Dr. Harisingh Gour Vishwavidyalaya, Sagar, Madhya Pradesh, INDIA. Abstract:The biotransformation reaction of cell suspension cultures produced from Decalepis hamiltonii and Nicotiana tabacum leaves were investigated, using Carvedilol drug. Interestingly, the cell suspension cultures showed biotransformation of racemic carvedilol. There is noticeable conversion of S-enantiomer to R-enantiomer of Carvedilol. The bio-conversion was detected and quantified by Chiral HPLC. The ideal biotransformation was achieved with the concentration of 0.1mg/ml Carvedilol at pH 5.8. The optimum incubation time was observed to be 15 days The Decalepis hamiltonii and Nicotiana tabacum cell culture have shown the capacity to convert S-isomer to R-isomer, because it has enzymes specific for conversion from S to R form. Among the two plants Decalepis hamiltonii have shown better biotransformation when compared to Nicotiana tabacum. Keywords:Bio transformation, Carvedilol, HPLC, Nicotiana tabacum, Plant cell culturesView:PDF (1019.25 KB)

Primary Prayojana of Ayurveda "Swasthasya swasthaya rakshanam aturasya vikara prashamanam cha ". Concept of Agni is a basic concept of Ayurveda classical texts. This concept has its own importance for maintenance of the health of a healthy person as well as for curing the various diseases. One should always careful for normal status of the all Agni’sfor maintenance of health. In the disease state vitiated Doṣha, Dhatu or Mala can be corrected with treatment of respective Agni. Agni is believed to be the agency for any kind of transformation. These may be bio chemical or bio physical or any other type of bio transformations. Due to these constant transformation procedures, body grows, develops and lastly destroys too. Diseased state of the body is also some pathological changes either functional or structural. Thus, the principle of Agni becomes vital as either the healthy or the diseased state can only be understood with understanding of changes and according to Ayurvedic principles, all these procedures cannot be possible without Agni. In Bruhattryi, all information related to Agni &amp; 13 types of Agni’s according to their locations and functions of transformation at different levels of digestion and metabolism are described. With the help of its own Agni, each body substance gets nourished and can perform its normal functions. Aama is a toxic, disease causing substance that forms as a result of impaired Agni .

Environmental occurrence and biotransformation of perfluoroalkyl carboxylic acid precursors: Fluorotelomer alcohols

Processes mediated by living organisms, animal, plants, fungi, algae, bacterial and virus have been the center of attention for many investigations looking for new sustainable alternatives for the development of new material. Biosynthetic pathways have emerged as a strategy to advance in the development of eco-friendly industry since they are the result of evolutionary and adaptive processes which have perfected the enzymatic machinery behind biotransformations and other biosynthetic processes. This review shows a general view about the biosynthetic processes for the making of biopolymers of interest for the industry, but at the same time, biotransformations for the obtaining of precursor, polymers and raw material are included. In particular, it is focused on starch and poly(hydroxyalkanoates) due to its industrial use and potential for the making of bioplastics.

A biotransformation is a key tool for the structural modification of natural and synthetic complexcompounds. It is employed to synthesize those compounds, which are arduous to get from chemical synthesis. Duringthe last few decades’ research has been focused on the modification of biologically potent compounds.Biotransformation is one of the effective ways in this regard. The current article covers the biotransformation ofnorethisterone (1) by using various bacteria and fungi as well as metabolism in man and animals i.e. rat, rabbit,monkey and dog, which brought mono-, di-, and tri-hydroxylation, oxidation, reduction, epoxidation anddeethynylation of 1. The review covers 26 metabolites (2 to 27) of 1, obtained during 1906 to 2018

Biotransformation is the procedure by which a substance changes starting with one synthetic then onto the next (changed) by a concoction response inside the body. Digestion or metabolic changes are terms much of the time utilized for the biotransformation procedure. Be that as it may, digestion is here and there not explicit for the change procedure but rather may incorporate different periods of toxicokinetics. Biotransformation is imperative to endurance since it changes ingested supplements (food, oxygen, and so forth.) into substances required for typical body capacities. For certain pharmaceuticals, it is a metabolite that is helpful and not the ingested sedate

Genetic polymorphisms of certain classes of glutathione S-transferase (GST), enzyme responsible for the biotransformation of drugs and xenobiotics, have been associated with risk of several cancers such as cervical cancer. The aim of this study is to investigate the impact of glutathione S-transferase M1 and T1 deletion on high-risk human papillomavirus (HR-HPV) infections and on dysplasia. A case-control study was carried out on 1069 endocervical samples from West African women including 482 HR-HPV positive and 139 patients had cervical lesions according to visual inspection with acetic acid and Lugol (VIA/VILI) screening. Deletion of the GSTM1 and GSTT1 genes was determined using conventional PCR and genotypes of HR-HPV by real-time PCR. An association with a reduced risk for HR-HPV infection was observed in Ivorian population with GSTT1-null (OR = 0.61, 95% CI = 0.40 - 0.92, p= 0.02) and GSTM1-active/GSTT1-null genotypes (OR = 0.56, 95% CI = 0.35 - 0.90, p= 0.02). In West African, women with GSTT1-null genotype had 1.72-fold higher risk for infection with HPV66 (p= 0.044) and reduced risk (OR = 0.39) for HPV35. Whereas women with GSTM1-null/GSTT1-active genotype had 2.32-fold higher risk for HPV18 infection (p= 0.042). GSTT1-null genotype was associated to cervical lesions in West African with a reduced risk (OR = 0.63, p= 0.017). The results of the present study demonstrate that GSTT1-null could be associated with cervical lesions and HPV35 infection with reduced risk. GSTM1-null associated with GSTT1-active could play a role in increasing the risk for HPV18 infection. Key words: Cervical cancer, GSTM1, GSTT1, HR-HPV, West Africa.

Biocatalysis and Biotransformation for Pharmaceuticals Synthesis

Las plantas son consumidas por diversos organismos, esta situación pone en riesgo su sobrevivencia, por ello han desarrollado mecanismos de defensa que evitan su ingesta. Por ejemplo, adaptaciones anatómicas, defensas químicas o metabolitos secundarios. Estos fitoquímicos inhiben el ataque de patógenos, provocan irritación al contacto, afectan los sistemas cutáneo, gastrointestinal, cardíaco y nervioso de los herbívoros o pueden provocar la muerte. Los rumiantes tienen adaptaciones mecánicas, fisiológicas y etológicas para evadir las defensas vegetales: rechazo, regulación y biotransformación. Desarrollaron adaptaciones anatomo-fisiológicas para albergar simbiontes microbianos para degradar celulosa y toxinas vegetales. Algunos metabolitos secundarios pueden tener efectos benéficos en alimentación o medicina animal, pero se requiere de mayor estudio sobre el tema.

ET-26-HCl, a novel anaesthetic agent with promising pharmacological properties, lacks extensive studies on pharmacokinetics and disposition in vitro and in vivo. In this study, we investigated the metabolic stability, metabolite production and plasma protein binding (PPB) of ET-26-HCl along with its tissue distribution, excretion and pharmacokinetics in animals after intravenous administration. Ultra-high performance liquid chromatography–tandem quadrupole time-of-flight mass spectrometry identified a total of eight new metabolites after ET-26-HCl biotransformation in liver microsomes from different species. A hypothetical cytochrome P450-metabolic pathway including dehydrogenation, hydroxylation and demethylation was proposed. The PPB rate was highest in mouse and lowest in human. After intravenous administration, ET-26-HCl distributed rapidly to all tissues in rats and beagle dogs, with the highest concentrations in fat and liver. High concentrations of ET-26-acid, a major hydroxylation metabolite of ET-26-HCl, were found in liver, plasma and kidney. Almost complete clearance of ET-26-HCl from plasma occurred within 4 h after administration. Only a small fraction of the parent compound and its acid form were excreted via the urine and faeces. Taken together, the results added to a better understanding of the metabolic and pharmacokinetic properties of ET-26-HCl, which may contribute to the further development of this drug.

Mössbauer and EPR study of ferrihydrite and siderite biotransformations by a syntrophic culture of alkaliphilic bacteria

Aerobic biotransformation of 6:2 fluorotelomer sulfonic acid in soil

The degradation and transformation of TBBPA-derived NER in soil

P-glycoprotein (P-gp) and cytochrome P450 3A4 (CYP3A4) play a significant role in the disposition and elimination of drugs. The objective of this study was to investigate the mechanism underlying the interaction between paclitaxel (substrate of P-gp and CYP3A4) and quercetin and chrysin (known modulator of P-gp and CYP3A4) using everted gut sacs in vitro models. Rat everted and non-everted gut sacs (NEGS) are simple and useful in vitro models to investigate the role of P-gp and CYP3A4 in drug disposition. NEGS were used to evaluate the transport of paclitaxel from mucosal to serosal (M-to-S) side of the intestine. NEGS were loaded with 1mL of modified Krebs-Ringer bicarbonate (KRB) buffer containing paclitaxel (50μg/mL) in the presence or absence of known P-gp and CYP3A4 inhibitors (quercetin and chrysin).The paclitaxel levels in incubated samples were dteremined by UV-spectrophotometer at 227 nm. The same experiment was repeated with everted gut sacs (EGS) to study the transport of paclitaxel from serosal to mucosal (S-to-M) side of the intestine. The apparent permeability coefficient (Papp), efflux ratio and net efflux were determined. In vitro study results showed that the Papp, net efflux and efflux ratio of paclitaxel were significantly increased by quercetin and chrysin. The present study results revealed that quercetin and chrysin enhanced the intestinal absorption of paclitaxel by inhibiting its absorption via P-gp and/or the CYP3A4-mediated biotransformation in intestine.

Anju Majeed1,2*, Muhammed Majeed1, Nooruddin Thajuddin2, Sivakumar Arumugam1, Furqan Ali1 and Kirankumar Beede1Article: 5636 | Pages: 1159-1168Abstract|Full Text| PDF| XMLDOI: https://dx.doi.org/10.22207/JPAM.13.2.55

Table S1. List of query proteins and their basic description used as reference sequences to identify bile acid metabolic proteins (sourced from UniProt). Table S2. Optimal cut-off parameters chosen to filter the significant sequence hits were determined based on the distribution of BLAST pairwise percentage identity, e-value and query and target coverage. Table S3. List of query proteins with the description of their Pfam domain. Table S4. Optimal cut-off parameters chosen for the construction of protein sequence-based similarity network were determined based on the distribution of BLAST pairwise percentage identity and e-value values. Figure S1. Schematic representation of a generalized bile salt biotransformation pathway. Enzymatic proteins that were studied have been highlighted in red color. Figure S2. The normalized abundance of total BSBGs in healthy individuals sampled from the USA, Denmark, and Spain. The Y-axis of the boxplot refers to the normalized abundance, whereas the X-axis refers to the country of these healthy control groups. The shape refers to the kernel probability density of the data at different values. The asterisks on the top indicate ns: p &gt; 0.05, *: p &lt; = 0.05, **: p &lt; = 0.01, ***: p &lt; = 0.001, ****: p &lt; = 0.0001 (Mann-Whitney Wilcoxon test). Figure S3. The normalized abundance of taxonomic-lineage specific BSBGs in healthy and IBD subjects sampled from Spain. The Y-axis of the violin plot refers to the normalized abundance, whereas the X-axis refers to the diagnosis. The shape refers to the kernel probability density of the data at different values. The pointrange refers to the mean and error range value of the data distribution. The asterisks on the top indicate ns: p &gt; 0.05, *: p &lt; = 0.05, **: p &lt; = 0.01, ***: p &lt; = 0.001, ****: p &lt; = 0.0001 (Mann-Whitney Wilcoxon test). (DOCX 413 kb)

The chlorothalonil is a widely used fungicide while the contamination of soil and water environments by this chemical causes potential threats to biodiversity. Given the metabolic potential of soil microorganisms, there is a need for developing microbiological approaches to degrade persistent compounds, such as chlorothalonil, in the contaminated sites. Here in this study, we isolated a bacterial strain (namely, BJ1) capable of degrading chlorothalonil from a chlorothalonil-contaminated farmland soil in the Shandong Province, China. Using 16S rDNA gene sequencing, morphological and biological characteristics, we identified the strain BJ1 as <i>Stenotrophomonas acidaminiphila</i>. The strain BJ1 uses chlorothalonil as a sole carbon source. At initial concentrations of 50, 100, 200 and 300 mg l⁻¹, it degraded 91.5%, 89.4%, 86.5% and 83.5% of chlorothalonil after 96 h of inoculation under optimum conditions (30°C and pH 7.0), respectively. Two metabolites, methyl-2,5,6-trichloro-3-cyano-4-methoxy-benzoate and methyl-3-cyano-2,4,5,6-tetrachlorobenzoate, were detected and identified based on HPLC–MS analysis, which suggests that the strain BJ1 metabolized chlorothalonil through the hydroxylation of chloro-group and hydration of cyano-group. The results of this study highlight the great potential for this bacterium to be used in chlorothalonil pollution remediation.

Biotransformation of ADCs. Pathways and enzymes