Antibacterial Activity and Cytotoxicity Screening of Acyldepsipeptide-1 Analogues Conjugated to Silver/Indium/Sulphide Quantum Dots.

The continuous rise in bacterial infections and antibiotic resistance is the driving force behind the search for new antibacterial agents with novel modes of action. Antimicrobial peptides (AMPs) have recently gained attention as promising antibiotic agents with the potential to treat drug-resistant infections. Several AMPs have shown a lower propensity towards developing resistance compared to conventional antibiotics.

Design, synthesis, and characterization of type I collagen mimetic peptides.

The current wound-healing collagen mimetic peptides (CMPs) have limitations such as poor membrane permeability and protease susceptibility. Herein, the solid-phase peptide synthesis of CMPs containing the integrin binding motif GFOGER is reported. The peptide sequences also consist of lipophilic moieties (adamantane and palmitic acid) for improved membrane permeability and different collagen-inducing tripeptides, namely, Thr-Thr-Lys (TTK), Gly-His-Lys (GHK), Gln-Pro-Arg (QPR), and Glu-Glu-Met (EEM).

Review: Structure-Activity Relationship of Antimicrobial Peptoids.

Due to their broad-spectrum activity against Gram-negative and Gram-positive bacteria, natural antimicrobial peptides (AMPs) and their synthetic analogs have emerged as prospective therapies for treating illnesses brought on by multi-drug resistant pathogens. To overcome the limitations of AMPs, such as protease degradation, oligo-N-substituted glycines (peptoids) are a promising alternative. Despite having the same backbone atom sequence as natural peptides, peptoid structures are more stable because, unlike AMP, their functional side chains are attached to the backbone nitrogen (N)-atom rather than the alpha carbon atom.

Biopolymer-Based Wound Dressings with Biochemical Cues for Cell-Instructive Wound Repair.

Regenerative medicine is an active research sphere that focuses on the repair, regeneration, and replacement of damaged tissues and organs. A plethora of innovative wound dressings and skin substitutes have been developed to treat cutaneous wounds and are aimed at reducing the length or need for a hospital stay. The inception of biomaterials with the ability to interact with cells and direct them toward desired lineages has brought about innovative designs in wound healing and tissue engineering.

Acyldepsipeptide Analogues: A Future Generation Antibiotics for Tuberculosis Treatment.

Acyldepsipeptides (ADEPs) are a new class of emerging antimicrobial peptides (AMPs), which are currently explored for treatment of pathogenic infections, including tuberculosis (TB). These cyclic hydrophobic peptides have a unique bacterial target to the conventional anti-TB drugs, and present a therapeutic window to overcome () drug resistance. ADEPs exerts their antibacterial activity on strains through activation of the protein homeostatic regulatory protease, the caseinolytic protease (ClpP1P2).

Development of fructose-1,6-bisphosphate aldolase enzyme peptide mimics as biocatalysts in direct asymmetric aldol reactions.

This study describes the design and synthesis of mimetic peptides modelled on the catalytic active site of the fructose-1,6-bisphosphate aldolase (FBPA) enzyme. The synthesized peptides consisting of the turn motifs and catalytic site amino acids of FBPA enzyme were evaluated for catalytic activity in direct asymmetric aldol reactions of ketones and aldehydes. The influence of substrate scope, catalyst loading and solvents including water, on the reaction were also investigated.

Relationship between amino acid ratios and decline in estimated glomerular filtration rate in diabetic and non-diabetic patients in South Africa.

Background: Diabetic kidney disease is a major complication resulting from type 1 and type 2 diabetes. Currently, the microalbuminuria test is used to monitor renal function; however, it does not detect albumin until progressive loss of renal function has occurred.

Objective: This study analysed the relationship between changes in amino acid ratios and estimated glomerular filtration rate (eGFR) decline in diabetic and non-diabetic patients.

Buchholzia coriacea seed (wonderful kolanut) alleviates insulin resistance, steatosis, inflammation and oxidative stress in high fat diet model of fatty liver disease.

Non-alcoholic fatty liver disease (NAFLD) is a hepatic condition with multiple pathological features and it currently has no specific treatment or approved drug. Wonderful kolanut widely consumed fresh or cooked has been applied in the treatment of numerous diseases in folk medicine. In this study, we evaluate the therapeutic potentials of hydroethanolic extract of defatted Buccholzia coriacea seeds (HEBCS) in NAFLD model.

Antibacterial and Anticancer Activity and Untargeted Secondary Metabolite Profiling of Crude Bacterial Endophyte Extracts from Baker Leaves.

This study isolated and identified endophytic bacteria from the leaves of and investigated the potential of the bacterial endophyte extracts as antibacterial and anticancer agents and their subsequent secondary metabolites. Ethyl acetate extracts from the endophytes and the leaves (methanol: dichloromethane (1 : 1)) were used for antibacterial activity against selected pathogenic bacterial strains by using the broth microdilution method. The anticancer activity against the U87MG glioblastoma and A549 lung carcinoma cells was determined by the MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxy-phenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay.

Anticancer activity and metabolite profiling data of KTMT5.

Fungi are ubiquitous, they proliferate even in environments with toxic pollutants that are otherwise harmful to other eukaryotes. This article presents data of fungi which were isolated from gold mine tailings and identified by DNA sequencing of their inter transcribed spacer regions 1 and 2. Five fungal isolates were identified, among which the crude extract of KTMT5 was investigated for anticancer activity on A549 (lung carcinoma) and UMG87 (glioblastoma) cell lines.

Cytotoxic activity of crude extracts from Datura stramonium's fungal endophytes against A549 lung carcinoma and UMG87 glioblastoma cell lines and LC-QTOF-MS/MS based metabolite profiling.

Background: Endophytic fungi are a proven source of bioactive secondary metabolites that may provide lead compounds for novel drug discovery. In this study, crude extracts from fungal endophytes isolated from Datura stramonium were evaluated for cytotoxic activity on two human cancer cell lines.

Methods: Fungal endophytes were isolated from surface sterilized aerial parts of D.

The LC-QTOF-MS/MS analysis data of detected metabolites from the crude extract of leaves.

This data article presents the untargeted metabolite profiling of a crude extract from the leaves of . The plant was collected in Johannesburg (South Africa) and the extract was prepared by firstly air-drying fresh leaves for one week, grinding the dry leaves into fine powder, followed by solvent extraction using a 1:1 solvent mixture of dichloromethane and methanol (v/v) to extract the compounds. The extract was concentrated at 65 °C to obtain a solid crude extract which was then stored under refrigeration at -80 °C.

Synthesis of novel 1,2,4-thiadiazinane 1,1-dioxides three component SuFEx type reaction.

Herein, we report the preparation of 1,2,4-thiadiazinane 1,1-dioxides from reaction of β-aminoethane sulfonamides with dichloromethane, dibromomethane and formaldehyde as methylene donors. The β-aminoethane sulfonamides were obtained through sequential Michael addition of amines to α,β-unsaturated ethenesulfonyl fluorides followed by further DBU mediated sulfur(vi) fluoride exchange (SuFEx) reaction with amines at the S-F bond.

Enhanced brain penetration of pretomanid by intranasal administration of an oil-in-water nanoemulsion.

Aim: To enhance the drug delivery to the brain with an oil-in-water nanoemulsion of pretomanid via intranasal (IN) administration.

Materials & Methods: The study involved 70 male Sprague-Dawley rats (160-180 g) that received either 20 mg/kg body weight (b.w.

Synthesis, screening and computational investigation of pentacycloundecane-peptoids as potent CSA-HIV PR inhibitors.

Herein, we present the first pentacycloundecane (PCU) diol peptoid derived HIV protease inhibitors with IC(50) values ranging from 6.5 to 0.075 μM.

Pentacycloundecane-diol-based HIV-1 protease inhibitors: biological screening, 2D NMR, and molecular simulation studies.

Novel compounds incorporating a pentacycloundecane (PCU) diol moiety were designed, synthesized, and evaluated as inhibitors of the wild-type C-South African (C-SA) HIV-1 protease. Seven compounds are reported herein, three of which displayed IC(50) values in the 0.5-0.

Synthesis, 2D-NMR and molecular modelling studies of pentacycloundecane lactam-peptides and peptoids as potential HIV-1 wild type C-SA protease inhibitors.

In this study, eight non-natural peptides and peptoids incorporating the pentacycloundecane (PCU) lactam were designed and synthesized as potential inhibitors of the wild type C-SA HIV-protease. Five of these inhibitors gave IC(50) values ranging from 0.5 up to 0.

Synthesis and NMR elucidation of novel tetrapeptides.

The synthesis and NMR elucidation of Ala-Val-Pro-Ile and five novel peptide-based derivatives are reported. These peptides mimic the natural second mitochondria-derived activator of caspase (Smac) protein. Purification was achieved using preparative HPLC and the NMR elucidation of all compounds is reported for the first time.

Synthesis and structural studies of pentacycloundecane-based HIV-1 PR inhibitors: a hybrid 2D NMR and docking/QM/MM/MD approach.

Pentacycloundecane (PCU) lactam-peptide based HIV protease inhibitors were synthesized and nanomolar activity against the resistance-prone wild type C-South African HIV protease is reported. NMR investigations indicated that the activity is related to the chirality of the PCU moiety and its ability to induce conformations of the coupled peptide side chain. EASY-ROESY NMR experiments gave information about the 3D structure of the cage peptides and 3D solution structure could be linked to the experimental IC(50) activity profile of the considered inhibitors.

Pentacycloundecane-based inhibitors of wild-type C-South African HIV-protease.

In this study, we present the first account of pentacycloundecane (PCU) peptide based HIV-protease inhibitors. The inhibitor exhibiting the highest activity made use of a natural HIV-protease substrate peptide sequence, that is, attached to the cage (PCU-EAIS). This compound showed nanomolar IC(50) activity against the resistance-prone wild type C-South African HIV-protease (C-SA) catalytic site via a norstatine type functional group of the PCU hydroxy lactam.

Synthesis and NMR elucidation of novel pentacycloundecane-based peptides.

The synthesis and NMR elucidation of two novel pentacycloundecane (PCU)-based peptides are reported. The PCU cage amino acids were synthesised as racemates and the incorporation of the cage amino acid with (S)-natural amino acids produced diastereomeric peptides. The diastereomeric 'cage' peptides were separated using preparative HPLC and the NMR elucidation of these PCU containing peptides are reported for the first time.

Synthesis and NMR assignment of pentacycloundecane precursors of potential pharmaceutical agents.

The synthesis and complete NMR elucidation of eight novel pentacycloundecane (PCU) derivatives are reported. These compounds are precursors in the synthesis of PCU-based anti-tuberculosis (TB) agents and potential human immunodeficiency virus (HIV) protease inhibitors. Two-dimensional (2D) NMR techniques were used to assign the NMR spectra for these compounds.

Synthesis and NMR elucidation of novel penta-cycloundecane amine derivatives as potential antituberculosis agents.

The synthesis and NMR elucidation of five novel penta-cycloundecane amine derivatives are reported. These compounds are potential antituberculosis agents. The (1)H and (13)C spectra showed major overlapping of methine signals of the cage skeleton making it extremely difficult to elucidate these compounds.