Unlocking the potential of fondaparinux: guideline for optimal usage and clinical suggestions (2023).

Background: Thromboembolic disease is associated with a high rate of disability or death and gravely jeopardizes people's health and places considerable financial pressure on society. The primary treatment for thromboembolic illness is anticoagulant medication. Fondaparinux, a parenteral anticoagulant medicine, is still used but is confusing due to its disparate domestic and international indications and lack of knowledge about its usage. Its off-label drug usage in therapeutic settings and irrational drug use are also common. Objective: The aim of this guideline is to enhance the judicious clinical application of fondaparinux by consolidating the findings of evidence-based research on the drug and offering superior clinical suggestions. Methods: Seventeen clinical questions were developed by 37 clinical pharmacy experts, and recommendations were formulated under the supervision of three methodologists. Through methodical literature searches and the use of recommendation, assessment, development and evaluation grading techniques, we gathered evidence. Results: This guideline culminated in 17 recommendations, including the use of fondaparinux for venous thromboembolism (VTE) prevention and treatment, perioperative surgical prophylaxis, specific diseases, special populations, bleeding and overdose management. For different types of VTE, we recommend first assessing thrombotic risk in hospitalized patients and then administering the drug according to the patient's body mass. In surgical patients in the perioperative period, fondaparinux may be used for VTE prophylaxis, but postoperative use usually requires confirmation that adequate hemostasis has been achieved. Fondaparinux may be used for anticoagulation prophylaxis in patients hospitalized for oncological purposes, in patients with atrial fibrillation (AF) after resuscitation, in patients with cirrhosis combined with portal vein thrombosis (PVT), in patients with antiphospholipid syndrome (APS), and in patients with inflammatory bowel disease (IBD). Fondaparinux should be used with caution in special populations, such as pregnant female patients with a history of heparin-induced thrombocytopenia (HIT) or platelet counts less than 50 × 109/L, pregnant patients with a prethrombotic state (PTS) combined with recurrent spontaneous abortion (RSA), and children. For bleeding caused by fondaparinux, dialysis may partially remove the drug. Conclusion: The purpose of this guideline is to provide all healthcare providers with high-quality recommendations for the clinical use of fondaparinux and to improve the rational use of the drug in clinical practice. Currently, there is a lack of a dedicated antidote for the management of fondaparinux. The clinical investigation of activated prothrombin complex concentrate (APCC) or recombinant activated factor VII (rFⅦa) as potential reversal agents is still pending. This critical gap necessitates heightened scrutiny and research emphasis, potentially constituting a novel avenue for future inquiries into fondaparinux sodium. A meticulous examination of adverse events and safety profiles associated with the utilization of fondaparinux sodium will contribute significantly to a more comprehensive understanding of its inherent risks and benefits within the clinical milieu.

RNA-binding proteins potentially regulate the alternative splicing of apoptotic genes during knee osteoarthritis progression.

BACKGROUND: Alternative splicing (AS) is a principal mode of genetic regulation and one of the most widely used mechanisms to generate structurally and functionally distinct mRNA and protein variants. Dysregulation of AS may result in aberrant transcription and protein products, leading to the emergence of human diseases. Although considered important for regulating gene expression, genome-wide AS dysregulation, underlying mechanisms, and clinical relevance in knee osteoarthritis (OA) remain unelucidated. Therefore, in this study, we elucidated and validated AS events and their regulatory mechanisms during OA progression. RESULTS: In this study, we identified differentially expressed genes between human OA and healthy meniscus samples. Among them, the OA-associated genes were primarily enriched in biological pathways such as extracellular matrix organization and ossification. The predominant OA-associated regulated AS (RAS) events were found to be involved in apoptosis during OA development. The expression of the apoptosis-related gene BCL2L13, XAF1, and NF2 were significantly different between OA and healthy meniscus samples. The construction of a covariation network of RNA-binding proteins (RBPs) and RAS genes revealed that differentially expressed RBP genes LAMA2 and CUL4B may regulate the apoptotic genes XAF1 and BCL2L13 to undergo AS events during OA progression. Finally, RT-qPCR revealed that CUL4B expression was significantly higher in OA meniscus samples than in normal controls and that the AS ratio of XAF1 was significantly different between control and OA samples; these findings were consistent with their expected expression and regulatory relationships. CONCLUSIONS: Differentially expressed RBPs may regulate the AS of apoptotic genes during knee OA progression. XAF1 and its regulator, CUL4B, may serve as novel biomarkers and potential therapeutic targets for this disease.

Prediction of hydrological and water quality data based on granular-ball rough set and k-nearest neighbor analysis.

Hydrological and water quality datasets usually encompass a large number of characteristic variables, but not all of these significantly influence analytical outcomes. Therefore, by wisely selecting feature variables with rich information content and removing redundant features, it not only can the analysis efficiency be improved, but the model complexity can also be simplified. This paper considers introducing the granular-ball rough set algorithm for feature variable selection and combining it with the k-nearest neighbor method and back propagation network to analyze hydrological and water quality data, thus promoting overall and fused inspection. The results of hydrological water quality data analysis show that the proposed method produces better results compared to using a standalone k-nearest neighbor regressor.

Sodium Alginate Aerogel as a Carrier of Organogelators for Effective Oil Spill Solidification and Recovery.

Marine oil spills pose a serious threat to the marine ecological environment. Phase-selective organogelators (PSOGs) are ideal candidates for oil spill gelation when used in combination with a mechanical recovery method. However, the toxicity of an organic solvent carrier has become a key problem when it is applied in the remediation of marine oil pollution. In this study, through an inexpensive and nontoxic ionic cross-linking and freeze-drying method, we successfully developed composite oil gelling agents that used a biomass sodium alginate aerogel as the carrier of 12-hydroxystearic acid (12-HSA). Simultaneously, carboxylated cellulose nanofibers (CNF-C) with large specific surface area and graphene oxide (GO) with excellent mechanical properties as reinforcing fillers were combined with an alginate matrix. 12-HSA, as a green and inexpensive organic gelator, was uniformly loaded on the aerogels by vacuum impregnation. The sodium alginate aerogel was capable of absorbing and storing oil due to its three-dimensional network skeleton and high porosity. Rheological studies have demonstrated that the organic gelator 12-HSA can be released from the aerogel substrate and self-assemble to form an oleogel with the absorbed oil quickly. The synergistic effect between absorption and congelation endows the composite oil gelling agent with efficient oil spill recovery capability. Based on eco-friendly, biodegradable, and simple synthesis methods, this composite oil gelling agent shows great potential for application in marine oil spill recovery.

Genome-wide expression analysis of LBD genes in tomato (Solanum lycopersicum L.) under different light conditions.

Lateral organ boundaries (LOB) domain (LBD) genes, a gene family that encodes the transcription factors (TFs) of plants, plays crucial functions in the development and growth of plants. Currently, genome-wide studies of the LBD family are still limited to tomato (Solanum lycopersicum L.), which is considered an important economic crop. In this study, we performed a genome-wide analysis of LBD in tomato. In total, 56 LBDs were found in the tomato genome. Protein alignment and phylogenetic classification showed that LBDs were conserved with other species. Since light emitting diodes (LEDs) light have promising applications for tomato growth. To better understand the potential function of LBDs in response to LED light in tomato, we conducted a genome-wide expression analysis of LBD genes under different light conditions. As expected, different LED lights affected the tomato growth (e.g. hypocotyl length). RNA-seq data showed that eight LBDs in tomato seedlings were differentially expressed under different light treatments, including white, blue, red, and far-red light, compared to the dark-grown condition. It indicates that these LBDs might regulate plant development in different LED light conditions. Interestingly, two LBD genes (SlLBD1 and SlLBD2) were found to be differentially expressed in four distinct lights, which might be involved in regulating the plant architecture via a complicated TF network, which can be taken into consideration in further investigation.

Analyzing Morphology, Metabolomics, and Transcriptomics Offers Invaluable Insights into the Mechanisms of Pigment Accumulation in the Diverse-Colored Labellum Tissues of Alpinia.

Alpinia plants are widely cherished for their vibrant and captivating flowers. The unique feature of this genus lies in their labellum, a specialized floral structure resulting from the fusion of two non-fertile staminodes. However, the intricate process of pigment formation, leading to distinct color patterns in the various labellum segments of Alpinia, remains a subject of limited understanding. In this study, labellum tissues of two Alpinia species, A. zerumbet (yellow-orange flowers) and A. oxyphylla (white-purple flowers), were sampled and analyzed through morphological structure observation, metabolite analysis, and transcriptome analyses. We found that hemispherical/spherical epidermal cells and undulate cell population morphology usually display darker flower colors, while flat epidermal cells and cell populations usually exhibit lighter flower colors. Metabolomic analysis identified a high concentration of anthocyanins, particularly peonidin derivatives, in segments with orange and purple pigments. Additionally, segments with yellow pigments showed significant accumulations of flavones, flavanols, flavanones, and xanthophylls. Furthermore, our investigation into gene expression levels through qRT-PCR revealed notable differences in several genes that participated in anthocyanin and carotenoid biosynthesis among the four pigmented segments. Collectively, these findings offer a comprehensive understanding of pigmentation in Alpinia flowers and serve as a valuable resource for guiding future breeding efforts aimed at developing Alpinia varieties with novel flower colors.

Coupling Carbon-Based Composite Phase Change Materials with a Polyurethane Sponge for Sustained and Efficient Solar-Driven Cleanup of Viscous Crude Oil Spill.

The efficient cleanup of crude oil spills is a worldwide problem due to their high viscosity and low fluidity. Under the assistance of solar radiation, adsorbents with in situ heating function are becoming the ideal candidates to solve this problem. In this study, a new strategy coupling a polyurethane (PU) sponge with phase change materials (PCMs) is proposed to realize the efficient utilization of solar energy and crude oil cleanup. Wormlike carbon nanotubes/mesoporous carbon (CNTs/MC) with a core-shell structure was used to encapsulate polyethylene glycol (PEG), which was then introduced into the PU sponge for photothermal conversion and thermal storage. After coating with a polydimethylsiloxane (PDMS) layer, the sponge was further endowed with hydrophobic characteristics. Additionally, PDMS can function as a binder between PEG@CNTs/MC and sponge skeleton. The resulting PEG@CNTs/MC/PU/PDMS (named as PEG@CMPP) exhibited excellent photothermal conversion and high absorption capacity for high-viscosity crude oil. Most importantly, thanks to the heat storage properties of PEG, the stored heat can be sustainably transferred to the surrounding crude oil to promote its continuous absorption even under insufficient light intensity conditions. The crude oil absorption capacity of PEG@CMPP-3 reached approximately 0.96 g/cm3 even after the light source was removed, which manifested the distinctive advantages compared to the conventional photothermal adsorbent. The proposed approach integrates the high efficiency of solar-assisted heating and energy-conserving advantage, thereby providing a feasible strategy for highly efficient remediation of viscous crude oil spills.

Three new furanones from endophytic fungus Hypoxylon vinosopulvinatum DYR-1-7 from Cinnamomum cassia with their antifungal activity.

Hypoxylon vinosopulvinatum DYR-1-7 is a endophytic fungus isolated from the Cinnamomum cassia Presl and has an inhibitory effect on Lasiodiplodia pseudotheobromae. Three new furanones, hypoxylonone A-C (1-3), as well as three known compounds (4-6), were isolated from an EtOAc extract of H. vinosopulvinatum DYR-1-7. The structures were determined by spectroscopic data analysis using UV, IR, 1D-, 2D-NMR and HR-ESI-MS. The absolute configurations of 1-3 were elucidated by electronic circular dichroism (ECD) analyses. In the antifungal bioassay, Hypoxylonone B and C exhibited strong inhibitory effects on L. pseudotheobromae with IC50 value at the concentration of 1.01 and 2.40 µg/mL, respectively. Compound 6 showed medium antifungal activity with IC50 value at the concentration of 10.67 µg/mL on Fusarium oxysporum. Compounds 3 and 4 displayed medium antifungul effects on Candida albicans.

Germacrane Sesquiterpene Dilactones from Mikania micrantha and Their Antibacterial and Cytotoxic Activity.

Four new germacrane sesquiterpene dilactones, 2ß-hydroxyl-11ß,13-dihydrodeoxymikanolide (1), 3ß-hydroxyl-11ß,13-dihydrodeoxymikanolide (2), 1α,3ß-dihydroxy-4,9-germacradiene-12,8:15,6-diolide (3), and (11ß,13-dihydrodeoxymikanolide-13-yl)-adenine (4), together with five known ones (5-9) were isolated from the aerial parts of Mikania micrantha. Their structures were elucidated on the basis of extensive spectroscopic analysis. Compound 4 is featured with an adenine moiety in the molecule, which is the first nitrogen-containing sesquiterpenoid so far isolated from this plant species. These compounds were evaluated for their in vitro antibacterial activity against four Gram-(+) bacteria of Staphyloccocus aureus (SA), methicillin-resistant Staphylococcus aureus (MRSA), Bacillus cereus (BC) and Curtobacterium. flaccumfaciens (CF), and three Gram-(-) bacteria of Escherichia coli (EC), Salmonella. typhimurium (SA), and Pseudomonas Solanacearum (PS). Compounds 4 and 7-9 were found to show strong in vitro antibacterial activity toward all the tested bacteria with the MIC values ranging from 1.56 to 12.5 µg/mL. Notably, compounds 4 and 9 showed significant antibacterial activity against the drug-resistant bacterium of MRSA with MIC value 6.25 µg/mL, which was close to reference compound vancomycin (MIC 3.125 µg/mL). Compounds 4 and 7-9 were further revealed to show in vitro cytotoxic activity toward human tumor A549, HepG2, MCF-7, and HeLa cell lines, with IC50 values ranging from 8.97 to 27.39 µM. No antibacterial and cytotoxic activity were displayed for the other compounds. The present research provided new data to support that M. micrantha is rich in structurally diverse bioactive compounds worthy of further development for pharmaceutical applications and for crop protection in agricultural fields.

Mesoporous carbon hollow spheres encapsulated phase change material for efficient emulsification of high-viscosity oil.

Low fluidity of high-viscosity oil usually hinders its emulsification. Facing this dilemma, we proposed a novel functional composite phase change material (PCM) with in situ heating feature coupled with emulsification capability. This composite PCM consisting of mesoporous carbon hollow spheres (MCHS) and polyethylene glycol (PEG) shows excellent photothermal conversion ability, thermal conductivity and Pickering emulsification. Compared with the currently reported composite PCMs, the unique hollow cavity structure of MCHS not only enables excellent encapsulation of PCM, but also protects the PCM from leaking and direct contact with oil phase. Importantly, the thermal conductivity of 80% PEG@MCHS-4 was determined to be 1.372 W/m·K, which was 2.887 times superior to that of pure PEG. MCHS endows the composite PCM with excellent light absorption capacity and photothermal conversion efficiency. The viscosity of high-viscosity oil can be facilely reduced in situ once it comes into contact with the heat-storing PEG@MCHS, thus the emulsification is greatly enhanced. In view of the in situ heating feature and emulsification capability of PEG@MCHS, this work puts forward a novel solution to address the problem of emulsification of high-viscosity oil through the integration of MCHS and PCM.

Multi-energies assisted and all-weather recovery of crude oil by superhydrophobic melamine sponge.

Efficient and safe recovery of high-viscosity marine crude oil spills is still a worldwide challenge. High-viscosity crude oil is difficult to be removed by traditional adsorbent materials. Although some recent developments in photothermal or electric-thermal oil-absorbing materials, the vertical heat transfer inside and the potential hazard of electrical leakage are difficult to be guaranteed. In order to overcome these problems, we polymerized dopamine (DA) in situ on the skeleton surface of the commercial melamine sponge (MS), and further coated the full-wavelength light-absorbing Fe3O4 NPs-Graphene (HF-G) on it to obtain the superhydrophobic sponge with excellent photothermal conversion effect, heat conductivity and magnetic heating capabilities (HF-G/PDA@MS). When the thickness of sponge is 5 mm, the HF-G/PDA@MS shows excellent vertical heat conductivity ability, and can absorb about 80 g/g. It also can be combined with an extra electric-heating device to achieve continuous heating to reduce the viscosity and recover crude oil at night or extreme weather. In addition, the temperature of HF-G/PDA@MS can reach about 40 °C by electromagnetic induction heater, indicating that we can use multiple energies-assisted modes to heat the HF-G/PDA@MS to. This work provides a promising solution and theoretical support for all-weather solving offshore crude oil spills pollution and recovery.

Efficacy of administrative intervention for neurosurgical patients with off-label use of alprostadil lipid microsphere.

As an adjuvant drug, alprostadil lipid microsphere injection (Lipo-PGE1) is one of the best-selling drugs in China in recent years. However, the off-label use of Lipo-PGE1 is very common. This study aimed to investigate the use of Lipo-PGE1 and evaluate the clinical effects and economic benefits after administrative intervention on inappropriate use of Lipo-PGE1 in neurosurgical patients in a Chinese tertiary hospital. Administrative interventions were implemented from January to December 2018 by reducing the procurement volume of Lipo-PGE1, judging the rationality of medical records, and establishing reward and punishment mechanisms. Administrative interventions significantly decreased prescription rate (49.98% vs 22.49%), utilization (22,311 DDDs vs 8334 DDDs), drug use density (43.52 DDDs/TID vs 15.84 DDDs/TID), total expenditure (3.58 million RMB vs 1.30 million RMB), and average expenditure (2025.04 RMB vs 1466.49 RMB) of Lipo-PGE1. To our delight, these intervention effects were maintained or even better in the 1-year post-intervention period. Moreover, in the intervention and post-intervention phases, the Lipo-PGE1 use for no indications as well as inappropriate drug dose, frequency, menstruum type, combination, and contraindication were markedly reduced. Besides, the mean costs (P < 0.001), and mean duration (P < 0.001) of Lipo-PGE1 were also obviously decreased. The administrative intervention obviously reduced the off-label use of Lipo-PGE1. However, there still remains a number of inappropriate uses of Lipo-PGE1. To further improve the rational use of Lipo-PGE1, combination of administrative intervention and real-time clinical pharmacists intervention should be implemented.

α-Glucosidase inhibitors from brown rice bound phenolics extracts (BRBPE): Identification and mechanism.

Brown rice bound phenolics extracts (BRBPE) have been reported to possess α-glucosidase inhibitory effects, the specific enzyme inhibitors involved in this process were unknown. Here, α-glucosidase inhibitors in BRBPE were screened using bioaffinity ultrafiltration methods, and seven phenolic compounds - three monomers (p-coumaric acid, ferulic acid and methyl ferulate), three dimers (8-5', 5-5' and 8-O-4' diferulic acid) and a trimer (5-5'/8-O-4″ dehydrotriferulic acid) were identified as exact inhibitors, among which 5-5'/8-O-4″ dehydrotriferulic acid and 5-5'diferulic acid exhibited the best inhibitory activity. Enzyme kinetic analysis suggested that the inhibitory mechanism of these seven inhibitors including competitive, noncompetitive, uncompetitive and mixed manner. Molecular docking analysis revealed that the seven inhibitors bind with α-glucosidase mainly by hydrogen bonding interaction, hydrophobic force and ionic bond. Molecular dynamics simulation further explored the structure and molecular property of phenolic-glucosidase complex. This work provided a deep insight into brown rice bound phenolics acting as potent α-glucosidase inhibitors.

Deep remediation of oil spill based on the dispersion and photocatalytic degradation of biosurfactant-modified TiO2.

The employment of dispersant was an effective method to treat marine oil spill pollution. However, conventional dispersants only showed a single oil dispersion. Here, by modifying TiO2 nanoparticles with biosurfactant-Rhamnolipids (Rha), a highly efficient particulate dispersant with photocatalytic activity was developed. Rha-TiO2 showed both excellent oil spill dispersion and facilitated photodegradation for oil simultaneously. The oil droplets dispersed by Rha-TiO2 in seawater exhibited long time stability, which indicated the synergistic emulsification interactions between TiO2 and Rha in artificial sea water (ASW). The dispersion mechanism of Rha-TiO2 was analyzed, we found the TiO2 nanoparticles alone weren't effectively emulsified oil in high salinity ASW, but the addition of a small amount of Rha could modify the surface wettability of TiO2 nanoparticles to form the stable emulsion. In addition, the addition of a small amount of Rha could reduce the surface tension of the oil-water interface, which contribute to increasing the content of TiO2 nanoparticles at the oil-water interface, form a steric rigid layer around the oil droplets to prevent droplet coalescence and facilitate the further photocatalytic degradation of oil. In short, the Rha-TiO2 nanoparticles could effective disperse oil in ASW, meanwhile the TiO2 also played the role of photocatalytic degradation of oil pollution. Hence, this study developed a novel photocatalytic particulate dispersant to remediate marine oil spill and delivered a new feasible solution for practical oil spill treatment in the future.

Thymol derivatives with antibacterial and cytotoxic activity from the aerial parts of Ageratina adenophora.

Three new thymol derivatives, 7-formyl-9-isobutyryloxy-8-hydroxythymol (1), 7,9-di-isobutyryloxy-8,10-dehydrothymol (2) and 2α-methoxyl-3ß-methyl-6-methylol-2,3-dihydrobenzofuran (3), along with five known ones (4-8), were isolated from the aerial parts of the invasive plant Ageratina adenophora. Their structures were elucidated by extensive spectroscopic analysis and they were all isolated from the aerial part of A. adenophora for the first time. These compounds, except 8, selectively showed in vitro antimicrobial activity against three Gram-(+) and two Gram-(-) bacterial strains. In particular, compounds 1 and 5 showed notable in vitro antimicrobial activity against all five bacterial strains with IC50 values ranging from 3.9 to 15.6 µg mL-1, as compared to reference compound kanamycin sulfate with a MIC value 1.9-3.9 µg mL-1. Compounds 1 and 5 were further revealed to show in vitro cytotoxic activity against three tested human tumor (MCF-7, NCI-H460 and HeLa) cell lines, with IC50 values ranging from 7.45 to 28.63 µM. Compounds 7 and 8 selectively showed slight but detectable in vitro cytotoxicity toward MCF-7 and NCI-H460 cell lines, with IC50 values 44.65-83.19 µM. No cytotoxic effects were detected in the bioassay of the other four thymol derivatives. The present results provide new data to support that the aerial parts of A. adenophora are a rich source of bioactive chemicals valuable in medicinal applications.

Efficacy and Safety of Different Doses of Systemic Corticosteroids in COPD Exacerbation.

BACKGROUND: Although systemic corticosteroids (SCS) have long been used to treat patients with COPD exacerbation, the recommended dose remains controversial. We aimed to perform a meta-analysis and an indirect treatment comparison to investigate the efficacy and safety of different doses of SCS in subjects with COPD exacerbation. METHODS: Studies were identified by searching different databases for randomized controlled trials that investigated the efficacy and safety of SCS with placebo in subjects with exacerbation of COPD. The different doses of SCS were assigned to low-dose (ie, initial dose ≤ 40 mg prednisone equivalent/d [PE/d]), medium-dose (initial dose = 40-100 mg PE/d, and high-dose (initial dose > 100 mg PE/d) groups. The indirect treatment comparison was performed between low-, medium-, and high-dose SCS groups. RESULTS: Twelve trials with 1,375 participates were included. Compared to placebo, the risk of treatment failure was lower in the low-dose SCS groups (risk ratio 0.61 [95% CI 0.43-0.88], P = .007) and high-dose SCS groups (risk ratio 0.64 [95% CI 0.48-0.85], P = .002); the FEV1 was significantly improved in low-dose (mean difference 0.09 [95% CI 0.06-0.12], P < .001), medium-dose (mean difference 0.23 [95% CI 0.02-0.44], P = .036), and high-dose SCS groups (mean difference 0.09, [95% CI 0.03-0.15], P < .001, respectively). Regarding safety, the incidence of hyperglycemia was higher in high-dose SCS groups versus placebo (risk ratio 2.52 [95% CI 1.13-5.62], P = .02). The indirect comparison between low-, medium-, and high-dose SCS found that the risk of treatment failure and changes in FEV1 were similar between these doses of SCS. CONCLUSIONS: This meta-analysis indicates that low-dose SCS (initial dose ≤ 40 mg PE/d) was sufficient and safer for treating subjects with COPD exacerbation, and it was noninferior to higher doses of SCS (initial dose > 40 mg PE/d) in improving FEV1 and reducing the risk of treatment failure. However, our findings need to be verified in head-to-head randomized controlled trials.

Biodiversity and antifouling activity of fungi associated with two soft corals from the South China Sea.

Bacteria in corals have been studied in detail in the past decades. However, the biodiversity and bioactivity of fungi in corals are still poorly understood. This study investigated the biodiversity and antifouling activity of fungi in soft corals Cladiella krempfi and Sarcophyton tortuosum from the South China Sea. A high diverse and abundant fungal community was found in the two soft corals. Furthermore, five isolates shared 83-95% similarity with their closest relatives, indicating that they might be novel species in genera Phaeoshaeria and Mucor. In addition, approximately 50% of the representative isolates exhibited distinct antifouling activity. In particular, isolates Fungal sp. SCAU132 and Fungal sp. SCAU133 displayed very strong antifouling activity against Bugula neritina, suggesting they can provide a potential resource for further investigation on isolation of novel antifouling metabolites. To our knowledge, this study is the first report to investigate the biodiversity and antifouling activity of fungi in C. krempfi and S. tortuosum.

Anti-MRSA Sesquiterpenes from the Semi-Mangrove Plant Myoporum bontioides A. Gray.

The striking rise of methicillin-resistant Staphylococcus aureus (MRSA) infections has become a serious threat to public health worldwide. In an effort to search for new anti-MRSA agents from natural products, a bioassay-guided phytochemical study was conducted on the semi-mangrove plant Myoporum bontioides A. Gray, which led to the isolation of two new sesquiterpene alkaloids (1 and 2) and six known furanosesquiterpenes (3⁻8). Their structures were elucidated on the basis of extensive analysis of their 1D, 2D NMR and mass spectroscopic data. These two new alkaloids (1 and 2) displayed potent anti-MRSA activity with MIC value of 6.25 µg/mL. This is the first report of sesquiterpene alkaloids from the plants of Myoporum genus and their anti-MRSA activity.

Characterization and immunological activity of polysaccharides from Ixeris polycephala.

A water-soluble polysaccharide, named KMCP, was isolated and purified from edible plant Ixeris polycephala by using DEAE-52 cellulose chromatography. Its structure was determined by chemical analysis, methylation analysis, and NMR analysis, coupled with characterization by scanning electron spectroscopy (SEM). The resulting data indicated that KMCP was an arabinogalactan, with an average molecular weight of 1.95×106Da, which was mainly composed of arabinose and galactose in a relative molar ratio of 28.1% and 70.3%, respectively. The structure of KMPC was characterized as 72.5% of (1→4)-ß-Galp residues interspersed with 27.5% of (1→4,6)-ß-Galp residues in the main chain, and the branches were composed of (1→5)-α-Araf moieties or α-Araf (1→5) α-Araf (1→disaccharide moieties attached at O-6 of the (1→4,6)-ß-Galp residues. KMCP was revealed to be capable of exhibiting macrophage-mediated innate immune responses via enhancing phagocytosis of macrophages and increasing production of NO, activating NF-κB signaling pathway and promoting the mice spleen cells proliferation in a dose-dependent manner within the test concentrations (10.0-200.0µg/mL). These results suggested that KMCP could potentially be an effective and safe immunomodulator valuable to be utilized in pharmacological fields or in the development of functional foods.

Triterpenoids with α-glucosidase inhibitory activity and cytotoxic activity from the leaves of Akebia trifoliata.

Ten pentacyclic triterpenoids including a new multiflorane triterpene acid, 2α,3ß,23-trihydroxymultiflor-7-en-28-oic acid (1), and a new lupane triterpene monoglucoside named akebiaoside C (2), were obtained from the leaves of Akebia trifoliata. Their structures were elucidated by extensive spectroscopic analysis, and they were all isolated from the leaves of A. trifoliata for the first time. These compounds, except 4 and 5, showed in vitro α-glucosidase inhibitory activity much stronger than acarbose. Especially, 2, 3, 6, 8 and 10 displayed in vitro α-glucosidase inhibitory activity with IC50 values from 0.004 to 0.081 mM, which were close or even more potent than corosolic acid (IC50 0.06 mM). Triterpenoids 1, 8 and 10 were further revealed to show moderate in vitro cytotoxic activity against human tumor A549, HeLa and HepG2 cell lines, with IC50 values ranging from 26.5 to 51.9 µM. Compound 9 selectively showed in vitro cytotoxicity toward HeLa and HepG2 cell lines, with IC50 values of 81.49 and 73.47 µM, respectively. These findings provided new data to support that the leaves of A. trifoliata are a rich source in bioactive triterpenoids highly valuable to be developed for medicinal usage.