Mechanism of cryptotanshinone to improve endocrine and metabolic functions in the endometrium of PCOS rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Cryptotanshinone is the main bioactive component of Salvia miltiorrhiza, with various mechanisms of action, including antioxidant, anti-inflammatory, cardiovascular protection, neuroprotection, and hepatoprotection. Salvia miltiorrhiza is used clinically by gynecologists in China. AIM OF THE STUDY: Polycystic ovary syndrome (PCOS) has a significant impact on women's quality of life, leading to infertility and reproductive disorders. Hence, this study aims to assess the pharmacological activity of cryptotanshinone in the treatment of PCOS and investigate its therapeutic mechanism. MATERIALS AND METHODS: Human chorionic gonadotropin (HCG) combined with insulin is used to simulate a PCOS-like rat model and attempt to discover the abnormal changes that occur and the means by which the pathway acts in this model. RESULTS: The transcriptome sequencing method is used to identify 292 differential genes that undergo significant changes, of which 219 were upregulated and 73 were downregulated. Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analysis of the signaling pathways reveals that differential expressed genes are significantly enriched in 23 typical pathways. Estrogen signaling pathways are screened in the cryptotanshinone and model groups, and significant differential changes in Fos, ALOX12, and AQP8 are found. This suggests that these signaling pathways and molecules may be the main signaling targets for regulating the differences in endometrial tissue. CONCLUSION: These results indicate that cryptotanshinone has targets for regulating the proliferation of endometrial tissue via estrogen signaling pathways in PCOS-like rats, providing an experimental basis for the clinical application of cryptotanshinone in the treatment of PCOS.

Self-delivery of a metal-coordinated anti-angiogenic nanodrug with GSH depleting ability for synergistic chemo-phototherapy.

Synergistic chemo-phototherapy has offered tremendous potential in cancer treatment. Nevertheless, nanosystems usually suffer from the complexity of multicomponents (polymeric or inorganic materials), which results in carrier-related toxicity issues. Moreover, the GSH over-expression of tumor cells seriously compromises ROS therapeutic efficiency. Herein, we designed a self-delivered nanodrug via Cu(II) coordination-driven co-self-assembly of celastrol (CST, a chemo-drug with anti-angiogenesis activity) and indocyanine green (ICG, a photosensitizer) for synergistic chemo-phototherapy with GSH depletion. The nanodrug was further cloaked by an erythrocyte membrane (RBC) to prolong the circulation time. Within the tumor microenvironment, the nanodrug would be disassembled upon intracellular GSH triggering. Moreover, the released Cu(II) could efficiently deplete the GSH, thus damaging the ROS-scavenging system and amplifying the phototherapeutic efficiency upon laser irradiation. The in vivo experiments validated the highly effective accumulation at tumor sites, potent tumor growth inhibition, and inappreciable systemic toxicity. The tumor microenvironment-responsive coordination-driven self-assembled biomimetic nanodrug may hold potential applications in tumor theranostics.

The effect of sweet tea polysaccharide on the physicochemical and structural properties of whey protein isolate gels.

In this study, we investigated the effect of sweet tea polysaccharide (STP) on the physicochemical and structural properties of heat-induced whey protein isolate (WPI) gels, and explored the potential mechanism. The results indicated that STP promoted the unfolding and cross-linking of WPI to form a stable three-dimensional network structure, and significantly improved the strength, water-holding capacity and viscoelasticity of WPI gels. However, the addition of STP was limited to 2 %, too much STP would loosen the gel network and affect the gel properties. The results of FTIR and fluorescence spectroscopy suggested that STP affected the secondary and tertiary structures of WPI, promoted the movement of aromatic amino acids to the protein surface and the conversion of α-helix to ß-sheet. In addition, STP reduced the surface hydrophobicity of the gel, increased the free sulfhydryl content, and enhanced the hydrogen bonding, disulfide bonding, and hydrophobic interactions between protein molecules. These findings can provide a reference for the application of STP as a gel modifier in the food industry.

Acanthopanax senticosus extract alleviates radiation-induced learning and memory impairment based on neurotransmitter-gut microbiota communication.

BACKGROUND: Acanthopanax senticosus (AS) is a medicinal and food plant with many physiological functions, especially nerve protection. Its extract has many functional components, including polysaccharides, flavonoids, saponins, and amino acids. Our previous study indicated that AS extract protected against nerve damage caused by radiation. However, little is known about the gut-brain axis mechanism of AS and its impact on radiation-induced learning and memory impairment. METHOD: In 60 Co-γ ray-irradiated mice, we investigated the changes in behavior, neurotransmitters and gut microbiota after different days of administration of AS extract as a dietary supplement. RESULTS: The AS extract improved learning and memory ability in mice, and the neurotransmitter levels in the hippocampus and colon started to change from the 7th day, which accompanied changes of the gut microbiota, a decreased abundance of Helicobacter on the 7th day and an increased abundance of Lactobacillus on the 28th day. Among the marker bacteria, Ruminococcus and Clostridiales were associated with 5-HT synthesis, and Streptococcus were associated with 5-HT and ACH synthesis. In addition, the AS extract increased the tight junction protein, inhibited inflammation levels in colon, and even increased the relative protein expression of BDNF and NF-κB and decreased the relative protein expression of IκBα in the hippocampus of irradiated mice. CONCLUSION: These results will lay the foundation for further study on the mechanism of the gut-brain axis of AS in preventing radiation-induced learning and memory impairment.

Fatty foods and the risk of bladder cancer: A case-control study.

OBJECTIVE: The aim of this study was to explore the association between dietary fatty foods and the risk for bladder cancer. METHODS: Patients newly diagnosed with bladder cancer (n = 113) and 292 controls were recruited. A food frequency questionnaire (FFQ) was used to investigate the food intake within 1 y. Multivariate logistic regression model was used to estimated odds ratio (OR) between different types of fatty food consumption and bladder cancer. RESULTS: The consumption of soybean oil, the largest proportion of cooking oil, in both groups were much higher than the Chinese recommended dietary intake, especially in the control group. Higher intake of red meat was also observed in bladder cancer cases, although lower intakes of marine fish, egg, milk, and dairy products and nuts were observed in controls. After adjusting for potential confounders, the intakes of marine fish and milk and dairy products were negatively correlated with bladder cancer, with the adjusted OR of 0.28 (95% confidence interval [CI], 0.15-0.55) and 0.36 (95% CI, 0.19-0.69). Total nuts were related to a 76% reduction in bladder cancer risk (OR, 0.24; 95% CI, 0.12-0.48). There was clear and positive association between soybean oil and bladder cancer risk with OR of 3.47 (95 % CI, 1.69-7.14). In stratified analyses by sex and smoking status, the relationship was similar for most results, except for milk and dairy products. The negative correlation between milk and dairy products and bladder cancer risk was only found in men; and milk and dairy products and bladder cancer risk were irrelevant by smoking status. No significant association was found between the intakes of other foods and bladder cancer risk. CONCLUSIONS: Intake of nuts and marine fish may be beneficial for the prevention of bladder cancer. The protective effect of milk and dairy products was only found in men with bladder cancer. High soybean oil intake was a risk factor for bladder cancer.

Eleutheroside E supplementation prevents radiation-induced cognitive impairment and activates PKA signaling via gut microbiota.

Radiation affects not only cognitive function but also gut microbiota. Eleutheroside E (EE), a principal active compound of Acanthopanax senticosus, has a certain protective effect on the nervous system. Here, we find a four-week EE supplementation to the 60Co-γ ray irradiated mice improves the cognition and spatial memory impairments along with the protection of hippocampal neurons, remodels the gut microbiota, especially changes of Lactobacillus and Helicobacter, and altered the microbial metabolites including neurotransmitters (GABA, NE, ACH, 5-HT) as well as their precursors. Furthermore, the fecal transplantation of EE donors verifies that EE alleviated cognition and spatial memory impairments, and activates the PKA/CREB/BDNF signaling via gut microbiota. Our findings provide insight into the mechanism of EE effect on the gut-brain axis and underpin a proposed therapeutic value of EE in cognitive and memory impairments induced by radiation.

Sweet tea (Rubus Suavissmus S. Lee) polysaccharides promote the longevity of Caenorhabditis elegans through autophagy-dependent insulin and mitochondrial pathways.

The fine structure of sweet tea polysaccharide (STP-60a) has been characterized. However, the biological activity of STP-60a has not been extensively explored. This study aims to evaluate the anti-aging activity of STP-60a using Caenorhabditis elegans (C. elegans) as a model and to investigate the underlying molecular mechanism. 400 µg/mL of STP-60a increased the mean lifespan of C. elegans by 22.88%, reduced the lipofuscin content by 33.01%, and improved the survival rate under heat stress and oxidative stress by 32.33% and 27.63%, respectively. Further research in lifespan-related mutants revealed that STP-60a exerted anti-aging effects mainly through insulin and mitochondrial signaling pathways. Through qRT-PCR and microscopic imaging of transgenic nematodes, we found that 400 µg/mL of STP-60a increased the expression of daf-16, skn-1, and hsf-1 downstream of the insulin pathway by 1.68-fold, 1.88-fold, and 1.03-fold, respectively, and promoted the accumulation of daf-16 and skn-1 in the nucleus. STP-60a also significantly regulated the function of the mitochondrial respiratory chain and unfolded protein recovery system. Furthermore, STP-60a activated the autophagy level in C. elegans, and the mutation of daf-2 or clk-1 inhibited the upregulation of autophagy genes by STP-60a, suggesting that autophagy acted as an effector of the insulin and mitochondrial pathways during STP-60a antiaging.

The Therapeutic Effect of Acanthopanax senticosus Components on Radiation-Induced Brain Injury Based on the Pharmacokinetics and Neurotransmitters.

Acanthopanax senticosus (AS) is a medicinal and food homologous plant with many biological activities. In this research, we generated a brain injury model by 60Co -γ ray radiation at 4 Gy, and gavaged adult mice with the extract with AS, Acanthopanax senticocus polysaccharides (ASPS), flavones, syringin and eleutheroside E (EE) to explore the therapeutic effect and metabolic characteristics of AS on the brain injury. Behavioral tests and pathological experiments showed that the AS prevented the irradiated mice from learning and memory ability impairment and protected the neurons of irradiated mice. Meanwhile, the functional components of AS increased the antioxidant activity of irradiated mice. Furthermore, we found the changes of neurotransmitters, especially in the EE and syringin groups. Finally, distribution and pharmacokinetic analysis of AS showed that the functional components, especially EE, could exert their therapeutic effects in brain of irradiated mice. This lays a theoretical foundation for the further research on the treatment of radiation-induced brain injury by AS.

Collaborative Assessment and Health Risk of Heavy Metals in Soils and Tea Leaves in the Southwest Region of China.

The collaborative assessment and health risk evaluation of heavy metals (HMs) enrichment in soils and tea leaves are crucial to guarantee consumer safety. However, in high soil HM geochemical background areas superimposed by human activities, the health risk associated with HMs in soil-tea systems is not clear. This study assessed the HMs concentration (i.e., chromium (Cr), cadmium (Cd), arsenic (As), and lead (Pb)) in tea leaves and their relationship with soil amounts in the southwest region of China to evaluate the associated health risk in adults. The results revealed that the average soil concentration of Cr was the highest (79.06 mg kg-1), followed by Pb (29.27 mg kg-1), As (14.87 mg kg-1), and Cd (0.18 mg kg-1). Approximately 0.71, 4.99, 7.36, and 10.21% of soil samples exceeded the threshold values (NY/T 853-2004) for Pb, Cr, As, and Cd, respectively. Furthermore, the average concentration of Pb, As, and Cd in tea leaves was below the corresponding residue limits, but Cr was above the allowed limits. Correlation analysis revealed that the Pb, Cr, As, and Cd amounts in tea leaves were positively correlated to their soil amounts (p < 0.01) with an R2 of 0.203 **, 0.074 **, 0.036 **, and 0.090 **, respectively. Additionally, approximately 40.38% of the samples were found to be contaminated. Furthermore, spatial distribution statistical analysis revealed that Lancang was moderately contaminated, while Yingjiang, Zhenkang, Yongde, Zhenyuan, Lüchun, Jingdong, Ximeng, and Menglian were slightly contaminated areas. The target hazard quotients (THQ; health risk assessment) of Pb, Cr, As, and Cd and the hazard index (HI) of all the counties were below unity, suggesting unlikely health risks from tea consumption.

Strategy for Highly Efficient Radioprotection by a Selenium-Containing Polymeric Drug with Low Toxicity and Long Circulation.

Because of the rapid development and extensive use of nuclear technology, ionizing radiation has become a large threat to human health. Until now, there has been no practicable radioprotector for routine clinical application because of severe side effects, high toxicity, and short elimination half-life. Herein, we develop a highly efficient radioprotection strategy using a selenium-containing polymeric drug with low toxicity and long circulation by removing reactive oxygen species (ROSs). The selenium-containing polymeric drug is prepared by copolymerization of vinyl phenylselenides (VSe) and N-(2-hydroxyethyl) acrylamide (HEA). The in vitro radioprotective efficacy of the polymeric drug is increased by 40% with lower cytotoxicity compared with the small-molecular VSe monomer. Importantly, the radioprotection activity of the polymeric drug shows more remarkable effects both in cell culture and mice model compared to the commercially available drug ebselen and also exhibits a much longer retention time in blood (half-life ∼ 10 h). This work may unfold a new area for highly efficient radioprotection by polymeric drugs instead of small-molecular agents.

Positively charged conjugated microporous polymers with antibiofouling activity for ultrafast and highly selective uranium extraction from seawater.

Uranium high-efficiency separation from seawater still has some obstacles such as slow sorption rate, poor selectivity and biofouling. Herein, we report a strategy for ultrafast and highly selective uranium extraction from seawater by positively charged conjugated microporous polymers (CMPs). The polymers are synthesized by Sonogashira-Hagihara cross-coupling reaction of 1,3-dibromo-5,5-dimethylhydantoin and 1,3,5-triethynylbenzene, and then modified with oxime and carboxyl via click reaction. The CMPs show an ultrafast sorption (0.46 mg g-1 day-1) for uranium, and possess an outstanding selectivity with a high sorption capacity ratio of U/V (8.4) in real seawater. The study of adsorption process and mechanism indicate that the CMPs skeleton exhibits high affinity for uranium and can accelerate the sorption, and uranium(VI) is adsorbed on the materials by the interaction of oxime/carboxyl ligands and hydantoin. Moreover, the material can be simply loaded onto the filter membrane, and shows remarkable antibiofouling properties against E. coli and S. aureus and excellent uptake capacity for uranium with low concentration in real seawater. This work may provide a promising approach to design adsorbents with fast adsorption rate, high selectivity and antibacterial activity, and expand the thinking over the development of novel and highly efficient adsorbents for uranium extraction from seawater.

Protective effects of Ulva pertusa polysaccharide and polysaccharide­iron (III) complex on cyclophosphamide induced immunosuppression in mice.

A water-soluble polysaccharide was isolated from marine green algae Ulva pertusa and then chelated with iron to prepare the polysaccharide­iron (III) complex. The immunomodulatory activities of sulfated polysaccharide and polysaccharide­iron (III) complex were investigated through a mice immune-deficiency model. Cyclophosphamide (Cy) was utilized to establish mice immunodeficiency model. Both polysaccharide and polysaccharide­iron (III) complex were proved to promote the proliferation of lymphocyte and enhance the activities of mice macrophages. In mice serum, the levels of cytokines including TNF-α, IFN-γ and IL-10 restored and the contents of hemolysin were also found elevated after treatment with polysaccharide and its iron complex. Besides, it has been shown that both polysaccharide and polysaccharide­iron (III) complex increased the contents of Hb, RBC and HCT in mice blood, and the effect of iron complex was better. All these results suggested that Ulva pertusa polysaccharide could be developed as a healthy function food. It was also noteworthy that the polysaccharide­iron (III) complex showed no negative effect upon the immunomodulatory activity of polysaccharide. Instead, the polysaccharide­iron (III) complex showed excellent hematopoietic capacity perhaps due to the supplement of iron.

Effects of Acanthopanax senticosus on Brain Injury Induced by Simulated Spatial Radiation in Mouse Model Based on Pharmacokinetics and Comparative Proteomics.

The active compounds in Acanthopanax senticosus (AS) have different pharmacokinetic characteristics in mouse models. Cmax and AUC of Acanthopanax senticosus polysaccharides (ASPS) were significantly reduced in radiation-injured mice, suggesting that the blood flow of mouse was blocked or slowed, due to the pathological state of ischemia and hypoxia, which are caused by radiation. In contrast, the ability of various metabolizing enzymes to inactivate, capacity of biofilm transport decrease, and lessening of renal blood flow accounts for radiation, resulting in the accumulation of syringin and eleutheroside E in the irradiated mouse. Therefore, there were higher pharmacokinetic parameters-AUC, MRT, and t1/2 of the two compounds in radiation-injured mouse, when compared with normal mouse. In order to investigate the intrinsic mechanism of AS on radiation injury, AS extract's protective effects on brain, the main part of mouse that suffered from radiation, were explored. The function of AS extract in repressing expression changes of radiation response proteins in prefrontal cortex (PFC) of mouse brain included tubulin protein family (α-, ß-tubulin subunits), dihydropyrimidinase-related protein 2 (CRMP2), γ-actin, 14-3-3 protein family (14-3-3ζ, ε), heat shock protein 90ß (HSP90ß), and enolase 2. The results demonstrated the AS extract had positive effects on nerve cells' structure, adhesion, locomotion, fission, and phagocytosis, through regulating various action pathways, such as Hippo, phagosome, PI3K/Akt (phosphatidylinositol 3 kinase/protein kinase B), Neurotrophin, Rap1 (Ras-related protein RAP-1A), gap junction glycolysis/gluconeogenesis, and HIF-1 (Hypoxia-inducible factor 1) signaling pathways to maintain normal mouse neurological activity. All of the results indicated that AS may be a promising alternative medicine for the treatment of radiation injury in mouse brain. It would be tested that whether the bioactive ingredients of AS could be effective through the blood-brain barrier in the future.

The effect of Platycodin D on the expression of cytoadherence proteins P1 and P30 in Mycoplasma pneumoniae models.

Platycodin D is one of the most important monomers of the Qinbaiqingfei pellet (Qinbai), which has already been approved as the first effective new Traditional Chinese Medicine used to fight against Mycoplasma pneumoniae (M. pneumoniae) in clinic in China. In previous studies, pharmacodynamics experiment has proved that Platycodin D has anti-M. pneumoniae effect and the minimum inhibitory concentration (MIC) is 16mµg/ml. This paper further clarified that the mechanism underlying the anti-M. pneumoniae effect of Platycodin D might be due to M. pneumoniae adhesion proteins P1 and P30. P1 and P30 expression levels in M. pneumoniae strain, M. pneumoniae-infected BALB/c mice, and M. pneumoniae-infected A549 cells were determined by reverse transcription PCR. Platycodin D strongly inhibited P1 and P30 expression in M. pneumonia and high dosage of Platycodin D exhibited a greater effect on reducing P1 and P30 expression than low dose Platycodin D. Platycodin D prevented M. pneumoniae infection through inhibiting the expression of adhesion proteins, which might be one of the mechanisms for the anti-M. pneumoniae properties of Qinbai. These results provide a foundation to further explore the mechanisms of action of Qinbai in future studies.

Diselenide-Labeled Cyclic Polystyrene with Multiple Responses: Facile Synthesis, Tunable Size, and Topology.

Diselenide-containing polymers have attracted more and more attention due to their redox sensitivity and bioapplication. In this work, a bifunctional diselenocarbonate is prepared and used to mediate the reversible addition-fragmentation chain transfer (RAFT) polymerization, producing α,ω-selenocarbonate-labeled telechelic polystyrene. Based on effective aminolysis of the terminal selenocarbonates and the followed spontaneous oxidation coupling reaction of diselenols, monoblock cyclic polystyrene linked by one diselenide bond and multiblock cyclic copolymer linked by several diselenide bonds are prepared by manipulating the concentration of α,ω-telechelic polystyrene in solution. The progress of aminolysis and the subsequent spontaneous oxidation of selenols to diselenides are monitored by UV-vis, gel permeation chromatography (GPC), and NMR characterizations, confirming the cyclic topologies of the resultant polymers (monocyclic or multiblock cyclic polymer). The monoblock cyclic or multiblock polymers show redox sensitivity, which can be converted to linear polymer by reducing or oxidizing agent. Moreover, the obtained monoblock cyclic polymer or multiblock cyclic copolymer can be transformed to each other under UV irradiation by adjusting the concentration of the cyclic polystyrene. For the first time, this work provides an alternative and promising approach to realize the topological transformation of polymers by installing multiresponsive diselenide moities into the backbone of cyclic polymer.

The inhibition of Platycodin D on Mycoplasma pneumoniae proliferation and its effect on promoting cell growth after anti-Mycoplasma pneumoniae treatment.

Platycodin D, extract from the root of Platycodon grandiflorum, is one of the most important monomers of the Qinbaiqingfei pellets (Qinbai) that has already been approved as the first Traditional Chinese Medicine for clinic use as an anti-M. pneumoniae agent. Qinbai constituents Scutellaria baicalensis and Platycodon grandiflorum were used to treat thousands of patients clinically in China each year. In this study, a M. pneumoniae-infected mouse strain, BALB/c, and a human-derived epithelial cell line, A549 type II pneumocytes, were used as experimental model. Anti-M. pneumoniae effect of Platycodin D was measured by the Real-time quantitative PCR, while the cell pathological change with hematoxylin and eosin and the growth recovery effects were determined with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and Trypan Blue dye in the experimental model after M. pneumoniae infection. Our research results showed that Platycodin D could significantly inhibit M. pneumoniae and promote cell growth after anti- M. pneumoniae treatment in the infected cells or mice.

Chemical composition and antioxidant activities of three polysaccharide fractions from pine cones.

The traditional method of gas chromatography-mass spectrometry for monosaccharide component analysis with pretreatment of acetylation is described with slight modifications and verified in detail in this paper. It was then successfully applied to the quantitative analysis of component monosaccharides in polysaccharides extracted from the pine cones. The results demonstrated that the three pine cone polysaccharides all consisted of ribose, rhamnose, arabinose, xylose, mannose, glucose and galactose in different molar ratios. According to the recovery experiment, the described method was proved accurate and practical for the analysis of pine cone polysaccharides, meeting the need in the field of chemical analysis of Pinus plants. Furthermore; the chemical characteristics, such as neutral sugar, uronic acids, amino acids, molecular weights, and antioxidant activities of the polysaccharides were investigated by chemical and instrumental methods. The results showed that the chemical compositions of the polysaccharides differed from each other, especially in the content of neutral sugar and uronic acid. In the antioxidant assays, the polysaccharide fractions exhibited effective scavenging activities on ABTS radical and hydroxyl radical, with their antioxidant capabilities decreasing in the order of PKP > PAP > PSP. Therefore, although the polysaccharide fractions had little effect on superoxide radical scavenging, they still have potential to be developed as natural antioxidant agents in functional foods or medicine.

Modulation of P1 and EGF expression by Baicalin.

Mycoplasma pneumoniae (M. pneumoniae) is increasingly recognized as a major cause of acute respiratory tract infections. Today, macrolides are used in the primary treatment of M. pneumoniae infection. However, with the increasing prevalence of strains resistant to macrolides, as well as reports of toxicity and adverse side effects, it is necessary to develop an alternative therapeutic agent. A compound recipe - Qinbaiqingfei pellets (Qinbai) - have already been approved in China as the first effective traditional Chinese medicine to be used against M. pneumoniae. Herein, we characterize the mechanism by which Qinbai interacts with M. pneumoniae and lung epithelial cells. The fact that Baicalin is the key component of Qingbai leads us to believe its study is important to elucidating the mechanism of the action of Qinbai. In this study, we describe the complex impact of Baicalin on the adhesin protein P1 of M. pneumoniae and on the expression of epidermal growth factor (EGF) in BALB/c mice and A549 cells infected with M. pneumonia. We draw the conclusion that Baicalin not only cured M. pneumoniae infection by inhibiting P1 expression, but also enhanced the repair of lung epithelial cells by upregulating EGF. Finally, we demonstrate that Baicalin plays a role in Qinbai treatment.

Biosynthesis, characterization and biological evalutation of Fe(III) and Cu(II) complexes of neoaspergillic acid, a hydroxamate siderophore produced by co-cultures of two marine-derived mangrove epiphytic fungi.

A hydroxamate siderophore, neoaspergillic acid (1), and a red pigment, ferrineoaspergillin (2) which is an Fe(III) complex of 1, were produced by co-cultures of two epiphytic fungi from a rotten fruit of the mangrove Avicennia marina from the South China Sea, and a new Cu(II) complex of 1, designated as cuprineoaspergillin (3), was also prepared by treatment of 1 with cupric acetate. All the compounds (1-3) were characterized by physical and chemical techniques, including 1H NMR, ESIMS, and photoelectron energy spectra. In the bioassays, compounds 1-3 showed significant inhibitory activities against selected Gram-positive and Gram-negative bacteria, and compound 1 also exhibited moderate inhibitory activities against human cancer cell lines SPC-A-1, BEL-7402, SGC-7901 and K562.