Significant Bioactivity Research Articles

Malvidin promotes PGC-1α/Nrf2 signaling to attenuate the inflammatory response and restore mitochondrial activity in septic acute kidney injury

Acute kidney injury (AKI) in sepsis is a vital and dangerous organ failure caused by an infection-induced dysregulation of the host reaction. Malvidin possesses significant anti-inflammatory and antioxidant bioactivities. This study explored the critical roles of malvidin in sepsis AKI and the crosstalk among mitochondrial function, nucleotide-binding oligomerization-like receptor 3 (NLRP3) inflammasome and nuclear factor erythroid 2 (Nrf2) signaling pathway. First, C57BL/6 mice were administered lipopolysaccharide intraperitoneally for 6 h to create an AKI model of sepsis. Hematoxylin-eosin staining and serum biomarker assays showed that malvidin protected from AKI in sepsis. Real-time fluorescence quantitative polymerase chain reaction analysis revealed that malvidin was able to inhibit inflammatory cytokines and mediators. Western blot assays indicated that malvidin suppressed NLRP3 inflammasome activation and enhanced antioxidant properties. Additionally, human renal tubular epithelial cells were stimulated by lipopolysaccharide/adenosine triphosphate to establish an NLRP3 inflammasome activation model in vitro, and in line with findings in vivo, malvidin significantly inhibited NLRP3 inflammasome activation. Furthermore, our data indicate that malvidin restored mitochondrial quality and function, reduced reactive oxygen species production, increased mitochondrial membrane potential, enhanced mitochondrial DNA copy number, and promoted peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC-1α) nuclear translocation. Moreover, inhibitor blockade assays indicated that both PGC-1α and Nrf2 affected the inhibition of the NLRP3 inflammasome by malvidin. Finally, immunoprecipitation assays showed that malvidin promoted PGC-1α and Nrf2 interactions. Overall, malvidin alleviated lipopolysaccharide-induced sepsis AKI, improved mitochondrial function and mitochondrial biogenesis, and inhibited the NLRP3 inflammasome through the PGC-1α/Nrf2 signaling pathway, suggesting that malvidin might translate into clinical applications for sepsis AKI therapy.

Study of 1-Formyl-2-Pyrazolines as Anticancer Drug Candidates

The development of novel anticancer agents is essential in cancer prevention. One versatile group of compounds, known for their significant bioactivity and several of its derivatives that have been clinically approved, is the group of pyrazolines. This study aimed to synthesize 1-formyl-2-pyrazoline derivatives (pyrazolines 1-2) using chalcone 1-2, hydrazine hydrate, and formic acid via cyclo-condensation. The synthesized compounds were characterized using Fourier Transform Infrared (FTIR), Gas Chromatography-Mass Spectrometry (GC-MS), and Nuclear Magnetic Resonance (1H- and 13C-NMR) spectrometers. Pyrazolines 1-2 were found to be drug-like compounds, satisfying Lipinski’s Rule of Five and possessing favourable absorption, distribution, metabolism, and excretion (ADME) properties, including good gastrointestinal absorption, blood-brain barrier permeability, and no interaction with P-glycoprotein. Furthermore, they were inactive against several toxicity endpoints in a normal body condition, such as immunotoxicity, mutagenicity, and cytotoxicity. In vitro cytotoxic evaluation of the pyrazolines 1-2 against HeLa and MCF7 cancer cell lines demonstrated moderate activity, with IC50 values of 25.01 µM and 82.87 µM, respectively. Pyrazolines 1-2 also showed good selectivity with selectivity index (SI) values of 8.92 and 14.45. The molecular docking study on epidermal growth factor receptor tyrosine kinase (EGFR-TK) (PDB ID: 4HJO) revealed that pyrazolines 1-2 had a binding affinity of -7.9 and -8.0 kcal/mol, respectively. The compounds interacted with Lys721 residue through hydrogen bonds and hydrophobic interactions due to the presence of the pyrazoline ring and the formyl group in their structures. These findings suggest that pyrazolines 1-2 scaffold has the potential to be further studied as a lead compound for anticancer drug candidates.

Design, synthesis, and anti–tobacco mosaic virus activity evaluation of quinazolinone derivatives containing purine moieties

In this study, a series of quinazolinone derivatives containing purine molecules were designed and synthesized, and their structures were characterized by 1H nuclear magnetic resonance, 13C nuclear magnetic resonance, and HRMS (High Resolution Mass Spectrometer). Antiviral bioassays against plant viruses indicated that some target compounds exhibited higher in vivo antiviral activity against tobacco mosaic virus (TMV) than the commercial drug ribavirin. At a concentration of 500 mg/L, compound A2 exhibited good activity against TMV, with therapeutic and protective activity values of 65.2 % and 60.2 %, respectively, and these values were superior to those of ribavirin (50.1 % and 57.2 %, respectively). Among these compounds, A2 demonstrated significant therapeutic bioactivity against TMV in vivo, with an EC50 (half-maximum effective concentration) value of 162.3 mg/L, which was superior to that of ribavirin (314.4 mg/L). In conclusion, quinazolinone derivatives containing purine molecules may provide a basis for further research on antiviral drugs.

Molecular cloning, expression, and functional analysis of a putative lectin from the pearl oyster (Pinctada fucata, Gould 1850)

Marine lectins are a group of proteins that possess specific carbohydrate recognition and binding domains. They exhibit various activities, including antimicrobial, antitumor, antiviral, and immunomodulatory effects. In this study, a novel galectin-binding lectin gene named PFL-96 (GenBank: OQ561753.1) was cloned from Pinctada fucata. The PFL-96 gene has an open reading frame of 324 base pairs (bp) and encodes a protein comprising 107 amino acids. The protein has a molecular weight of 11.95 kDa and an isoelectric point of 9.27. It contains an N-terminal signal peptide and a galactose-binding lectin domain. The sequence identity to lectin proteins from fish, echinoderms, coelenterates, and shellfish ranges from 31.90 to 40.00 %. In the phylogenetic analysis, it was found that the PFL-96 protein is closely related to the lectin from Pteria penguin. The PFL-96 recombinant protein exhibited coagulation activity on 2 % rabbit red blood cells at a concentration of ≥8 μg/mL. Additionally, it showed significant hemolytic activity at a concentration of ≥32 μg/mL. The PFL-96 recombinant protein exhibited significant antibacterial activity against Bacillus subtilis, Staphylococcus aureus, Candida albicans, and Vibrio alginolyticus, with minimum inhibitory concentrations (MIC) of 4, 8, 16, and 16 μg/mL, respectively. The minimum bactericidal concentrations (MBC) were determined to be 8, 16, 32, and 32 μg/mL, respectively. Furthermore, the PFL-96 recombinant protein exhibited inhibitory effects on the proliferation of Hela tumor cells, HepG2 tumor cells, and C666-1 tumor cells, with IC50 values of 7.962, 8.007, and 9.502 μg/mL, respectively. These findings suggest that the recombinant protein PFL-96 exhibits significant bioactivity in vitro, contributing to a better understanding of the active compounds found in P. fucata. The present study establishes a fundamental basis for further investigation into the mechanism of action and structural optimization of the recombinant protein PFL-96. The aim is to develop potential candidates for antibacterial and anti-tumor agents.

Quinoline-based Anti-oncogenic Molecules: Synthesis and Biological Evaluation.

Quinoline and its analogues are found in various natural products, many of which are active pharmacophores with significant bioactivities. This article discussed the plethora of quinoline derivatives and their analogues that have anti-cancer properties. The review will be helpful for the scientific community since several possible anticancer drugs based on quinolines are discussed here. In addition to this, the synthetic aspect of many such quinoline derivatives showing anti-cancer activities is also revealed in this article. These quinoline-based anti-oncogenic molecules can be synthesized using several acids, bases, and azides or with the help of reagents like Jone's reagent and Lawesson's reagent.

PHARMACEUTICALLY ACTIVE COMPOUNDS (PhACs) IN WATER OF ASIAN COUNTRIES: A META ANALYSIS REVIEW ON THE OCCURRENCE, DISTRIBUTION AND ENVIRONMENTAL RISK

Pharmaceutically active compounds (PhACs) have received a lot of attention due to their enormous consumption proportions, significant bioactivity, and prospective ecotoxicity that tend to impact the health of marine ecosystems and humans. In this study, five commonly used pharmaceuticals were studied in water bodies of Asian countries. The main objective of this study was to review the occurrence and distribution of selected PhACs such as diclofenac, fluoxetine, caffeine, propranolol, and triclosan in the water bodies of Asian countries. This review was found that the range of concentration of pharmaceuticals was 0.055 to 11.4 x103 ng/L. Five distribution maps were plotted using the Geographical Information System (GIS) software. China has been identified as the country that discovered most of the selected PhACs occurrence and distribution compared to other nations. Data obtained from the present review was analyzed for risk assessment analysis using the Risk Quotient (RQ) technique, which is typically applied to assess PhACs with potential ecological concerns in water ecosystems. The findings of the study showed that 31 RQ was found to be non-significant. Fluoxetine compound was classified as having the highest RQ value calculated for phytoplankton, with an RQ value of 136.08. Hence, PhACs surveillance in the water ecosystems must be strengthened, and research on PhACs occurrence and potential risks should be highlighted in global environmental research.

Immunomodulatory activity and protective effect of a capsular polysaccharide in Caenorhabditis elegans, isolated from Lactobacillus fermentum GBJ

A capsular polysaccharide, namely CPS-2, was isolated from Lactobacillus fermentum GBJ, purified using DEAE-52 anion exchange chromatography, and structurally characterized. We found that CPS-2 is homogenous, has an average molecular weight of 377 KDa, and is mainly composed of galactose and glucose at a molar ratio of 1.54:1.00. Its backbone comprises α-D-Galp-(1 → 3), α-D-Galp-(1 → 3,6), β-D-Glcp-(1 → 2), β-D-Galp-(1 → 6), and α-D-Galp-(1 → 4) residues with a side chain of β-D-Glcp-(1→). CPS-2 exerts an immunomodulatory effect by improving the proliferation and phagocytosis of macrophage RAW264.7 and promoting the secretion of NO and cytokines. The maximum secretion levels of IL-1β, IL-6, IL-10, and TNF-α were 1.96-, 0.11-, 0.22-, and 0.46-fold higher than those of the control, respectively. Furthermore, CPS-2 could significantly enhance the antioxidant system, extend lifespan, and improve stress tolerance of Caenorhabditis elegans at both exposure doses of 31.25 and 62.5 μg/mL. The average lifespan of nematodes reached a maximum in the 62.5 μg/mL-treated group after 10.39 days, 6.56 h, and 23.56 h in normal, oxidative stress, and heat shock environment, with extension percentages of 16.61 %, 43.23 %, and 15.77 %, respectively; therefore, CPS-2 displays an anti-aging effect. The significant bioactivity of CPS-2 promotes its application as a promising immunomodulatory and anti-aging ingredient in the food or pharmaceutical field.

Derivative of aminoresin as potent anti-virulence agent: Synthesis, spectral (FT-IR, UV, NMR) analysis, molecular docking, effect of polar solvation dynamics, and quantum chemical investigation

This work undertakes a comprehensive study encompassing the synthesis, spectral characterization (FT-IR, UV, 1HNMR , 13CNMR), exploration of polar solvation dynamics (DMSO, EtOH, MeOH) on the molecular structure, quantum chemical calculations, topological (ELF, NCI) analysis, and molecular docking investigation. The focal point is a derivative of amino terpolymer resin, synthesized via the condensation of 4,4′-diaminodiphenylmethane, 8-hydroxyquinoline, and formaldehyde (DHQF). Thorough examination of the compound was conducted to evaluate its responsiveness in varying solvents and investigate its viability as a key candidate for antivirulent therapy against toxins from Vibrio cholerae and Salmonella enterica. Simulation of solvation dynamics underscored the compound's robust thermodynamic stability even at lower temperatures. Primary vibrations noted within the compound encompassed CH, OH, NH, CH2, and CN vibrations, whereas UV spectroscopy unveiled an electronic shift from HOMO to LUMO, featuring peak absorption at 292.77 nm, influenced by its interaction with DMSO. The molecular docking analysis reveals the terpolymer's significant bioactivity against proteins 7EE6 (affinity: −6.7 kcal/mol) and 5V6f (affinity: -7.1 kcal/mol) associated with V. cholerae and S. enterica. The binding affinity of DHQF with S. enterica toxin protein (PDB: 7EE6) is comparable to that of standard drug Ciprofloxacin (affinity: −6.9 kcal/mol) and the toxin protein. However, the binding affinity between DHQF and V. cholerae toxin protein 5V5F considerably surpasses the binding affinity (−4.6 kcal/mol) between Doxycycline and the toxin protein. More so, the complex shows close binding affinities to both proteins and a higher number of conventional hydrogen bonds, this formed multiple favorable interactions, particularly conventional hydrogen bonds, contributing significantly to the stability of the ligand-protein complexes. In conclusion, the analyzed terpolymer displayed favorable qualities and interactions, which establish it as a strong candidate for addressing the targeted V. cholerae and S. enterica pathogens. These findings highlight the compound's impressive stability and its potential for various therapeutic applications in different areas.

Poly(Oxanorbornene)-Protein Conjugates Prepared by Grafting-to ROMP as Alternatives for PEG.

PEGylation is the gold standard in protein-polymer conjugation, improving circulation half-life of biologics while mitigating the immune response to a foreign substance. However, preexisting anti-PEG antibodies in healthy humans are becoming increasingly prevalent and elicitation of anti-PEG antibodies when patients are administered with PEGylated therapeutics challenges their safety profile. In the current study, two distinct amine-reactive poly(oxanorbornene) (PONB) imide-based water-soluble block co-polymers are synthesized using ring-opening metathesis polymerization (ROMP). The synthesized block-copolymers include PEG-based PONB-PEG and sulfobetaine-based PONB-Zwit. The polymers are then covalently conjugated to amine residues of lysozyme (Lyz) and urate oxidase (UO) using a grafting-to bioconjugation technique. Both Lyz-PONB and UO-PONB conjugates retained significant bioactivities after bioconjugation. Immune recognition studies of UO-PONB conjugates indicated a comparable lowering of protein immunogenicity when compared to PEGylated UO. PEG-specific immune recognition is negligible for UO-PONB-Zwit conjugates, as expected. These polymers provide a new alternative for PEG-based systems that retain high levels of activity for the biologic while showing improved immune recognition profiles.

A pair of diastereoisomeric C-glucofuranosyl flavones from the flowers of Gypsophila oldhamiana

Two new C-glucofuranosyl flavones apigenin 6-C-β-glucofuranoside (1) and apigenin 6-C-α-glucofuranoside (2) together with four known compounds (3–6) were isolated from the flowers of Gypsophila oldhamiana. Their structures were elucidated on the basis of extensive spectroscopic analyses. These compounds were evaluated for the cytotoxic activities against four human cancer cell lines and did not exhibit any significant bioactivities (IC50 values > 10 μM).

Engaging Isatins and Amino Acids in Multicomponent One-Pot 1,3-Dipolar Cycloaddition Reactions-Easy Access to Structural Diversity.

Multicomponent reactions (MCRs) have undoubtedly emerged as the most indispensable tool for organic chemists worldwide, finding extensive utility in the synthesis of intricate natural products, heterocyclic molecules with significant bioactivity, and pharmaceutical agents. The multicomponent one-pot 1,3-dipolar cycloaddition reactions, which were initially conceptualized by Rolf Huisgen in 1960, find extensive application in contemporary heterocyclic chemistry. In terms of green synthesis, the multicomponent 1,3-dipolar cycloaddition is highly favored owing to its numerous advantages, including high step- and atom-economies, remarkable product diversity, as well as excellent efficiency and diastereoselectivity. Among the numerous pieces of research, the most fascinating reaction involves the utilization of azomethine ylides generated from isatins and amino acids that can be captured by various dipolarophiles. This approach offers a highly efficient and convenient method for constructing spiro-pyrrolidine oxindole scaffolds, which are crucial building blocks in biologically active molecules. Consequently, this review delves deeper into the dipolarophiles utilized in the 1,3-dipolar cycloaddition of isatins and amino acids over the past six years.

Potential folate-producing strains and their applications in biofortification of fermented Moringa oleifera leaves powder

Folate is an essential vitamin for the human body and must be obtained exogenously. It is recognized that some microorganisms are capable of producing folates during growth, revealing possibilities for innovations of natural folate biofortified foods. The aim of this study was to identify potential folate-producing strains to enhance folate content in fermented Moringa oleifera leaves powder (MOLP). Although most of the tested strains exhibited folate production, there were significant differences among them in terms of both quantity and distribution, whether intracellular or extracellular. 10 strains with potential for folate production were chosen for enhancing the folate content of MOLP. The two most promising strains, Lactiplantibacillus sp. LP1 and Saccharomyces cerevisiae Y-J-1, demonstrated high folate levels up to 1940 and 2115 μg/100 g dry matter, respectively. These levels were 1.6 and 1.8-fold the initial value in MOLP. Additionally, the fermentation of MOLP not only enhanced its nutritional quality but also preserved its significant bioactivity. This study provides the initial understanding of how selected microorganisms can naturally enrich folates in fermented MOLP, presenting an alternative solution to address the widespread issue of folate deficiency while promoting human health.

Novel 1,3,4-Oxadiazole Hybrids with Antitumor and Anti-proliferative Potentials: A Comprehensive Review

Cancer is a lethal illness, and research into the development of effective anti-cancer medications is ongoing at all hours of the day and night. This is where 1,3,4-oxadiazoles come into play, since they are privileged and authenticated compounds because of their anti-cancer capabilities. In the field of drug development, 1,3,4-oxadiazole entities are characteristic heterocyclic rings with dominant anti-cancer activities. As a result, the primary goal of this article is to review the synthesis and screening of new 1,3,4-oxadiazole powerful derivatives is to determine their anti-cancer, antitumor, and other potential applications in the creation of anti-neoplastic drugs. In this study, the focus is on the 1,3,4-oxadiazole hybrids as well as the most significant bioactivity and potentiality of these anti-cancer compounds. This review article will include references to significant current reviews in the material, as well as a relevant discussion on the general background of anti-cancer medications that include 1,3,4-oxadiazole hybrids.

Characterization of two O-methyltransferases involved in the biosynthesis of O-methylated catechins in tea plant

Tea is known for having a high catechin content, with the main component being (−)-epigallocatechin gallate (EGCG), which has significant bioactivities, including potential anti-cancer and anti-inflammatory activity. The poor intestinal stability and permeability of EGCG, however, undermine these health-improving benefits. O-methylated EGCG derivatives, found in a few tea cultivars in low levels, have attracted considerable interest due to their increased bioavailability. Here, we identify two O-methyltransferases from tea plant: CsFAOMT1 that has a specific O-methyltransferase activity on the 3ʹʹ-position of EGCG to generate EGCG3′′Me, and CsFAOMT2 that predominantly catalyzes the formation of EGCG4″Me. In different tea tissues and germplasms, the transcript levels of CsFAOMT1 and CsFAOMT2 are strongly correlated with the amounts of EGCG3ʹʹMe and EGCG4ʹʹMe, respectively. Furthermore, the crystal structures of CsFAOMT1 and CsFAOMT2 reveal the key residues necessary for 3ʹʹ- and 4ʹʹ-O-methylation. These findings may provide guidance for the future development of tea cultivars with high O-methylated catechin content.

Protective effects and possible mechanisms of catalpol against diabetic nephropathy in animal models: a systematic review and meta-analysis.

Aim of the Study: Rehmannia glutinosa is a core Chinese herbal medicine for the treatment of diabetes and diabetic nephropathy (DN). It has been used for the treatment of diabetes for over 1,000years. Catalpol is the main active compound in Rehmannia roots. Current evidence suggests that catalpol exhibits significant anti-diabetic bioactivity, and thus it has attracted increasing research attention for its potential use in treating DN. However, no studies have systematically evaluated these effects, and its mechanism of action remains unclear. This study aimed to evaluate the effects of catalpol on DN, as well as to summarize its possible mechanisms of action, in DN animal models. Materials and Methods: We included all DN-related animal studies with catalpol intervention. These studies were retrieved by searching eight databases from their dates of inception to July 2022. In addition, we evaluated the methodological quality of the included studies using the Systematic Review Center for Laboratory animal Experimentation (SYRCLE) risk-of-bias tool. Furthermore, we calculated the weighted standard mean difference (SMD) with 95% confidence interval (CI) using the Review Manager 5.3 software and evaluated publication bias using the Stata (12.0) software. A total of 100 studies were retrieved, of which 12 that included 231 animals were finally included in this review. Results: As compared to the control treatment, treatment with catalpol significantly improved renal function in DN animal models by restoring serum creatinine (Scr) (p = 0.0009) and blood urea nitrogen (BUN) (p < 0.00001) levels, reducing proteinuria (p < 0.00001) and fasting blood glucose (FBG) (p < 0.0001), improving kidney indices (p < 0.0001), and alleviating renal pathological changes in the animal models. In addition, it may elicit its effects by reducing inflammation and oxidative stress, improving podocyte apoptosis, regulating lipid metabolism, delaying renal fibrosis, and enhancing autophagy. Conclusion: The preliminary findings of this preclinical systematic review suggest that catalpol elicits significant protective effects against hyperglycemia-induced kidney injury. However, more high-quality studies need to be carried out in the future to overcome the methodological shortcomings identified in this review.

Cyanobacteria as a Source of Bioactive Compounds with Anticancer, Antibacterial, Antifungal, and Antiviral Activities: A Review

Cyanobacteria a group of photosynthetic microorganisms, exist in almost all ecosystems in the world. Regarding health and disease prevention, cyanobacteria have been cited as a promising natural source of diverse secondary metabolites that exhibit significant bioactivities with potential pharmacological uses. Presently, great attention has been concentrated on the anticancer role of aquatic cyanobacteria that comprise an important source of bioactive compounds. Cyanobacteria-derived natural compounds and their synthetic analogs exhibited attractive results and showed remarkable activity by reaching phase II and III clinical trials successfully. Therefore, natural products from cyanobacteria might represent promising sources for novel anticancer therapy. Besides, microbial infections and infectious diseases from antimicrobial resistance (AMR) pose a direct threat to health and well-being because of the increase in antimicrobial resistance and the evolution of novel pathogenic strains. The search for novel antibiotics become increasingly urgent. Extensive efforts have been invested to find antimicrobial compounds from cyanobacteria to limit the misuse of commercial antibiotics. The development of natural anticancer and antimicrobial compounds from fresh water and marine cyanobacterial metabolites is a valuable trial. This review article summarizes the reported anticancer, antiviral, antifungal, and antibacterial properties of cyanobacteria and their mechanisms of action.

Mechanistic Action of Cell Cycle Arrest and Intrinsic Apoptosis via Inhibiting Akt/mTOR and Activation of p38-MAPK Signaling Pathways in Hep3B Liver Cancer Cells by Prunetrin-A Flavonoid with Therapeutic Potential.

Hepatocellular carcinoma (HCC) has a poor prognosis and a low survival rate. Drugs without side effects are desperately needed since chemotherapy has a negative effect on the host cells. Previous research has firmly established that plant-based compounds have significant bioactivities without a negative impact on the host. Flavonoids, in particular, are a class of compounds with both anti-inflammatory and anti-cancer properties. Prunetrin (PUR) is a glycosyloxyisoflavone (Prunetin 4'-O-glucoside) derived from Prunus sp., and its other form, called prunetin, showed optimistic results in an anti-cancerous study. Hence, we aimed to discover the anti-cancer ability of prunetrin in liver cancer Hep3B cells. Our cytotoxicity results showed that PUR can decrease cell viability. The colony formation assay confirms this strongly and correlates with cell cytotoxicity results. Prunetrin, in a dose-dependent manner, arrested the cell cycle in the G2/M phase and decreased the expression of cyclin proteins such as Cyclin B1, CDK1/CDC2, and CDC25c. Prunetrin treatment also promoted the strong cleavage of two important apoptotic hallmark proteins called PARP and caspase-3. It also confirms that apoptosis occurs through the mitochondrial pathway through increased expression of cleaved caspase-9 and increased levels of the pro-apoptotic protein Bak. Bak was significantly increased with the declining expression of the anti-apoptotic protein Bcl-xL. Next, it inhibits the mTOR/AKT signaling pathways, proving that prunetrin includes apoptosis and decreases cell viability by suppressing these pathways. Further, it was also observed that the activation of p38-MAPK was dose-dependent. Taken together, they provide evidence that prunetrin has an anti-cancerous ability in Hep3B liver cancer cells by arresting the cell cycle via p38 and inhibiting mTOR/AKT.

Four Undescribed Pyranones from the Scutellaria formosana-Derived Endophytic Fungi Ascomycota sp. FAE17.

Four undescribed pyranone derivatives, named ascomycopyrones A-D (1-4), as well as one known analogue simplicilopyrone (5) (this is the first study to report the absolute configuration), were isolated from the endophytic fungus Ascomycota sp. FAE17 derived from the flowers of Scutellaria formosa. The structures of these pyranones were identified by comprehensive spectroscopic and MS analyses, and the absolute configurations were determined by their experimental and quantum chemical electronic circular dichroism (ECD) calculations. All isolated compounds were tested for various bioactivities, including antibacterial, cytotoxic activity, and NO inhibitory activity. Unfortunately, none of the compounds showed significant bioactivities.

Fabrication and characterization of chlorhexidine gluconate loaded poly(vinyl alcohol)/45S5 nano-bioactive glass nanofibrous membrane for guided tissue regeneration applications.

Polymeric barrier membranes are used in periodontal applications to prevent fibroblastic cell migration into the cavities of bone tissue and to properly guide the proliferation of tissues. In this study, the fabrication, characterization, bioactivity, and in vitro biological properties of polyvinyl alcohol-based nanofibrous membranes containing nano-sized 45S5 bioactive glass (BG) loaded with chlorhexidine (CH) gluconate with biocompatible, bioactive, and antibacterial properties for using as dental barrier membranes were investigated. Nanofibrous membranes with an average fiber diameter, pore size, and porosity of 210 nm, 24.73 μm, and 12.42%, respectively, were loaded with 1% and 2% CH, and the release profile was investigated. The presence of BG in the membranes promoted fibroblastic proliferation and the presence of CH provided antibacterial properties. Nanofibrous membranes exhibit a high ability to restrict bacterial growth while fulfilling the necessary conditions for use as a dental barrier thanks to their low swelling rates, significant surface bioactivities, and appropriate degradation levels.

Synthesis and Biological Activity of Myricetin Derivatives Containing Pyrazole Piperazine Amide

In this paper, a series of derivatives were synthesized by introducing the pharmacophore pyrazole ring and piperazine ring into the structure of the natural product myricetin through an amide bond. The structures were determined using carbon spectrum and hydrogen spectrum high-resolution mass spectrometry. Biological activities of those compounds against bacteria, including Xac (Xanthomonas axonopodis pv. Citri), Psa (Pseudomonas syringae pv. Actinidiae) and Xoo (Xanthomonas oryzae pv. Oryzae) were tested. Notably, D6 exhibited significant bioactivity against Xoo with an EC50 value of 18.8 μg/mL, which was higher than the control drugs thiadiazole-copper (EC50 = 52.9 μg/mL) and bismerthiazol (EC50 = 69.1 μg/mL). Furthermore, the target compounds were assessed for their antifungal activity against ten plant pathogenic fungi. Among them, D1 displayed excellent inhibitory activity against Phomopsis sp. with an EC50 value of 16.9 μg/mL, outperforming the control agents azoxystrobin (EC50 = 50.7 μg/mL) and fluopyram (EC50 = 71.8 μg/mL). In vitro tests demonstrated that D1 possessed curative (60.6%) and protective (74.9%) effects on postharvest kiwifruit. To investigate the active mechanism of D1, its impact on SDH activity was evaluated based on its structural features and further confirmed through molecular docking. Subsequently, the malondialdehyde content of D1-treated fungi was measured, revealing that D1 could increase malondialdehyde levels, thereby causing damage to the cell membrane. Additionally, the EC50 value of D16 on P. capsici was 11.3 μg/mL, which was superior to the control drug azoxystrobin (EC50 = 35.1 μg/mL), and the scanning electron microscopy results indicated that the surface of drug-treated mycelium was ruffled, and growth was significantly affected.