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Our previous study has shown that the transcription factor Kruppel-like factor 7 (KLF7) promotes peripheral nerve regeneration and motor function recovery after spinal cord injury. KLF7 also participates in traumatic brain injury, but its regulatory mechanisms remain poorly understood. In the present study, an HT22 cell model of traumatic brain injury was established by stretch injury and oxygen-glucose deprivation. These cells were then transfected with an adeno-associated virus carrying KLF7 (AAV-KLF7). The results revealed that, after stretch injury and oxygen-glucose deprivation, KLF7 greatly reduced apoptosis, activated caspase-3 and lactate dehydrogenase, downregulated the expression of the apoptotic markers B-cell lymphoma 2 (Bcl-2)-associated X protein (Bax) and cleaved caspase-3, and increased the expression of βIII-tubulin and the antiapoptotic marker Bcl-2. Furthermore, KLF7 overexpression upregulated Janus kinase 2 (JAK2) and signal transducer and activator of transcription 3 (STAT3) phosphorylation in HT22 cells treated by stretch injury and oxygen-glucose deprivation. Immunoprecipitation assays revealed that KLF7 directly participated in the phosphorylation of STAT3. In addition, treatment with AG490, a selective inhibitor of JAK2/STAT3, weakened the protective effects of KLF7. A mouse controlled cortical impact model of traumatic brain injury was then established. At 30 minutes before modeling, AAV-KLF7 was injected into the ipsilateral lateral ventricle. The protein and mRNA levels of KLF7 in the hippocampus were increased at 1 day after injury and recovered to normal levels at 3 days after injury. KLF7 reduced ipsilateral hippocampal atrophy, decreased the injured cortex volume, downregulated Bax and cleaved caspase-3 expression, and increased the number of 5-bromo-2'-deoxyuridine-positive neurons and Bcl-2 protein expression. Moreover, KLF7 transfection greatly enhanced the phosphorylation of JAK2 and STAT3 in the ipsilateral hippocampus. These results suggest that KLF7 may protect hippocampal neurons after traumatic brain injury through activation of the JAK2/STAT3 signaling pathway. The study was approved by the Institutional Review Board of Mudanjiang Medical University, China (approval No. mdjyxy-2018-0012) on March 6, 2018.

Formula Le-Cao-Shi (LCS), a traditional Chinese medicine (TCM), has been used as folk remedy for treating hepatitis B for a long time. In our previous study, the anti-hepatitis B effects of LCS have been verified. In the present study, the anti-hepatitis B activities of LCS and its three single herbs were investigated in vitro by HepG2.2.15 cellular model, and the mechanisms against hepatitis B were deciphered via network pharmacology and gut microbiota analysis. By network pharmacology method, twelve key compounds that played a vital role in LCS were filtered from 213 ingredients. The targets RORA, CDK2, RELA, AKT1, IKBKG, PRKCβ and CASP3 were directly related to hepatitis B pathway, which indicated that LCS could exert anti-hepatitis B effect by co-regulating cell cycle and inflammatory pathways. The interactions between candidate compounds and target proteins that were directly involved in hepatitis B pathway were validated by molecular docking simulation and RT-PCR. By gut microbiota analysis, it was revealed that LCS could alter the disordered microbial composition in the infected ducks towards normal, especially the restoration of three key strains, namely Streptococcus alactolyticus, Enterococcus cecorum and Bacteroides fragilis. The above findings could provide a scientific basis for further development and utilization of LCS against hepatitis B.

A new phenolic compound, 6-(2-acetyl-3,5-dihydroxybenzyl)-4-hydroxy-3-methyl-2H-pyran-2-one (1), along with other six known phenolic derivatives (2-7), were isolated from the mangrove rhizosphere fungus Penicillium janthinellum HK1-6 cultured in potato dextrose broth medium containing 30 g L-1 of natural sea salt. The structure of the new compound (1) was elucidated by comprehensive analysis of spectroscopic data including 1D and 2D NMR spectra. The proposed biosynthetic pathway of compound 1 was also studied in this research. Interestingly, a brominated phenolic derivative, aryl bromide (compound 8), was obtained from this fungal strain cultured in medium containing 30 g L-1 of NaBr instead of natural sea salt. Compound 8 is proposed as a new natural product and formed through bromination of compound 7 when the fungus was cultured with NaBr. The neuroprotective effect of compound 1 on oxygen-glucose deprivation (OGD)-induced injury was investigated in rat spinal cord astrocytes. MTT assay demonstrated that compound 1 can attenuate OGD-induced cell viability loss in rat spinal cord astrocytes.

Three new 2,5-diketopiperazines, speramide C (

Objective. Acellular nerve allograft (ANA) is an effective surgical approach used to bridge the sciatic nerve gap. The molecular regulators of post-surgical recovery are not well-known. Here, we explored the effect of transgenic Schwann cells (SCs) overexpressing POU domain class 6, transcription factor 1 (POU6F1) on sciatic nerve regeneration within ANAs. We explored the functions of POU6F1 in nerve regeneration by using a cell model of H2O2-induced SCs injury and transplanting SCs overexpressing POU6F1 into ANA to repair sciatic nerve gaps. Approach. Using RNA-seq, Protein–Protein Interaction network analysis, gene ontology enrichment, and Kyoto Encyclopedia of Genes and Genomes pathway analysis, we identified a highly and differentially expressed transcription factor, POU6F1, following ANA treatment of sciatic nerve gap. Expressing a high degree of connectivity, POU6F1 was predicted to play a role in peripheral nervous system myelination. Main results. To test the role of POU6F1 in nerve regeneration after ANA, we infected SCs with adeno-associated virus—POU6F1, demonstrating that POU6F1 overexpression promotes proliferation, anti-apoptosis, and migration of SCs in vitro. We also found that POU6F1 significantly upregulated JNK1/2 and c-Jun phosphorylation and that selective JNK1/2 inhibition attenuated the effects of POU6F1 on proliferation, survival, migration, and JNK1/2 and c-Jun phosphorylation. The direct interaction of POU6F1 and activated JNK1/2 was subsequently confirmed by co-immunoprecipitation. In rat sciatic nerve injury model with a 10 mm gap, we confirmed the pattern of POU6F1 upregulation and co-localization with transplanted SCs. ANAs loaded with POU6F1-overexpressing SCs demonstrated the enhanced survival of transplanted SCs, axonal regeneration, myelination, and functional motor recovery compared to the ANA group loaded by SCs-only in line with in vitro findings. Significance. This study identifies POU6F1 as a novel regulator of post-injury sciatic nerve repair, acting through JNK/c-Jun signaling in SCs to optimize therapeutic outcomes in the ANA surgical approach.

Green port research integrates numerous theoretical and empirical studies of topics of important concern over the years, involving comprehensive scientific analyses. Learning about the global evolution of research on green ports can improve the understanding and evaluation of green ports by scholars and practitioners. In this paper, a total of 1051 papers from the Web of Science core collection for the period during 1992–2021 are collected as sample data. Based on the database, an analysis is conducted with CiteSpace software to map the knowledge regarding the field of green ports and explore the current research trends; the cooperation networks among countries (regions), institutions, and authors; and the evolution and mutation of keywords. The results indicate that the overall number of green port papers has increased over time. The countries with the highest numbers of papers published and the greatest influence are China and the United States, respectively. Additionally, the cooperative networks among authors, institutions, and countries are not mature enough and need to be strengthened further. Existing studies focus on the environmental impacts, evaluation, and construction of green ports. Recent trends indicate that researchers have become increasingly focused on reducing emissions, optimizing operations, evaluating policies, and identifying post-pandemic health issues associated with green ports. This study contributes to knowledge by assessing the state of the most significant studies published in the field of green port research, and the results contribute to a better understanding of green port research, which can further provide directions for the sustainable development of green ports.

Mangrove is a typical natural landscape with great ecological, social and economic functions and values, and should be highly valued and protected. However, in the past few decades, mangrove resources have suffered serious damage, and there are also many deficiencies in mangrove protection. Chinese mangroves, as an important part of the global mangroves, are of great research value. In the present study, the status and historical dynamic process of Chinese mangrove resources were investigated and discussed to illustrate the problems of resources from three aspects, including mangrove distribution, area and plant species. Based on field research, literature research and data analysis, it was revealed that Chinese mangroves are distributed in eight provinces and regions along the southeast coast with an area of 35,749.25 hm2, 38 species and 40 nature reserves. The protection situation and deficiencies were analyzed from the establishment and management of nature reserves. Based on the resource status and problems, reasonable strategies were proposed to protect and manage mangroves mainly from four aspects, including publicity and education, resources restoration and protection technology, legal system establishment, and comprehensive protection and management.

Chemical epigenetic modification on a marine-derived fungus Aspergillus terreus RA2905 using a histone deacetylase inhibitor, suberoylanilide hydroxamic acid (SAHA), resulted in a significantly changed metabolic profile. A chemical investigation of its ethyl acetate (EtOAc) extract led to the isolation of a racemate of benzyl furanone racemate (&plusmn, )-1, which further separated chirally as a pair of new enantiomers, (+)- and (&minus, )-asperfuranone (1), together with two new benzyl pyrones, asperpyranones A (2) and B (3). Their structures were elucidated by analysis of the comprehensive spectroscopic data, including one-dimensional (1D) and two-dimensional (2D) NMR, and HRESIMS. The absolute configurations were determined by electronic circular dichroism (ECD) calculation and single-crystal X-ray crystallographic experiment. The structures with benzyl furanone or benzyl pyrone skeletons were discovered from natural products for the first time. Compounds (&plusmn, )-1, (+)-1, (&minus, )-1, and 2 displayed the antifungal activities against Candida albicans with MIC values of 32, 16, 64, and 64 &mu, g/mL and PTP1B inhibitory activities with the IC50 values of 45.79, 17.32, 35.50, and 42.32 &mu, M, respectively. Compound 2 exhibited antibacterial activity against Pseudomonas aeruginosa with the MIC value of 32 &mu, g/mL.

The China Seas possess a variety of marine bioresources; however, many problems have been caused by exploitation and mismanagement of the resources, ecosystem and environment. In present study, the status of Chinese marine bioresources, as well as the issues of exploitation and utilization of resources were analyzed and discussed. Over-fishing, pollution and other anthropogenic activities have resulted in the destruction of bioresources, especially acute degradation of fisheries, as well as a series of impacts such as deterioration of the environment, loss of habitat, decline of biodiversity, imbalance of the marine ecosystem and a reduction of productivity. Precious marine bioresources have been diminished by commercial inadequate processing and insufficient utilization. The principle of protective exploitation and other feasible strategies and management measures were proposed for the conservation, rehabilitation and utilization of marine bioresources in China. There is an urgent need for research on the bioresources and eco-environment of the China Seas, in order to establish controls and administration for protection of the marine environment and conservation of bioresources. It will be necessary to ensure compliance with fishing quota licenses to preserve marine fishery resources. Any exploitation of marine bioresources must be managed scientifically and implement the use of the latest advances in marine biotechnology.

In recent years, the marine economy of China has experienced rapid growth, and the strategy of marine power also drove the development of the marine economy. The sea is a natural treasure that can provide rich resources. However, excessive consumption of natural resources and pollution problems of the ecological environment continue to become worse due to resource utilization inefficiency and disorderliness. Determining how to protect the environment on the basis of economic development is becoming a focus of attention. Research on the value of marine bioresources has great effects on preparing the balance sheet of resources. Accordingly, the present paper evaluates the value of marine bioresources in Shandong province offshore in 2014 by using the market valuation method, coefficients method, productivity change method, results reference method and contingent valuation method. In 2014, the total economic value of marine bioresources in Shandong province was $47.0533 billion, the direct use value was $9.3872 billion (in which the cultural research value was $0.7587 billion and recreational function value was $2.9413 billion), the indirect use value was $30.3469 billion, and the social value was $7.3192 billion. The indirect use value accounts for the largest proportion (64.49%), the direct use value accounts for 19.95%, far less than the indirect use value, and the social value accounts for a much smaller proportion, only 15.56%. And then the valuation results in the present study were used to analyze the reason for changes of ending value in the marine bioresources balance sheet. Suggestions were also put forward in the end. First, the public's understanding of the economic value of marine bioresources should be strengthened and the protection of marine bioresources should be increased, in order to promote the reasonable utilization of resources. Second, the potential value of cultural research for marine bioresources should be increased. Third, the stock quantity and value of marine bioresources in Shandong province should be evaluated, and a balance sheet of marine bioresources should be set up, in order to scientifically manage and constantly use marine bioresources in Shandong province, and promote the construction of an ecological civilization in China.

Epigenetic agents, histone deacetylase inhibitor (SAHA) and DNA methyltransferase inhibitor (5-Aza), were added to Czapek-Dox medium to trigger the chemical diversity of marine-derived fungus Aspergillus versicolor XS-20090066. By HPLC and 1H NMR analysis, the diversity of fungal secondary metabolites was significantly increased compared with the control. With the aid of MS/MS-based molecular networking, two new nucleoside derivatives, kipukasins K (1) and L (2) were obtained. Meanwhile, the yields of four known nucleoside derivatives were significantly enhanced. In addition, one new bisabolane sesquiterpene, aspergillusene E (7), along with ten known derivatives were also isolated. The structures were elucidated by comprehensive spectroscopic methods of NMR and HRESIMS analysis. Compounds 1 and 7 displayed antibacterial activities against Staphylococcus epidermidis and Staphylococcus aureus with the MIC values of 8–16 μg/mL. Our study revealed that the fungus A. versicolor XS-20090066 has been effectively induced by chemical epigenetic manipulation with a combination of SAHA and 5-Aza to produce new metabolites.

Three novel monomeric naphtho-&gamma, pyrones, peninaphones A&ndash, C (compounds 1&ndash, 3), along with two known bis-naphtho-&gamma, pyrones (compounds 4 and 5) were isolated from mangrove rhizosphere soil-derived fungus Penicillium sp. HK1-22. The absolute configurations of compounds 1 and 2 were determined by electronic circular dichroism (ECD) spectra, and the structure of compound 3 was confirmed by single-crystal X-ray diffraction analysis. Compounds 4 and 5 are a pair of hindered rotation isomers. A hypothetical biosynthetic pathway for the isolated monomeric and dimeric naphtho-&gamma, pyrones is also discussed in this study. Compounds 1&ndash, 3 showed antibacterial activity against Staphylococcus aureus (ATCC 43300, 33591, 29213, and 25923) with minimum inhibitory concentration (MIC) values in the range of 12.5&ndash, 50 &mu, g/mL. Compound 3 exhibited significant activity against the rice sheath blight pathogen Rhizoctonia solani.

A comprehensive evaluation of marine functional zoning (MFZ) implementation has aided in further strengthening marine comprehensive management. This evaluation is significant for summarizing the implementation experience, zoning establishment improvement and perfecting the zoning system. In this study, the MFZ evaluation index system, which includes three first-level indicators, 7 s-level indexes, and 23 third-level indexes, was arranged based on the systematic nature and hierarchy of the Pressure-State-Response (PSR) analysis framework involving pressure (P), state (S) and response (R). The Delphi and AHP (analytic hierarchy process) methods were used to determine the weight of each evaluation index. The results revealed that the status index has the greatest weight, indicating that zoning implementation benefits and sea use efficiency are important in the MFZ implementation evaluation standard. Then, the PSR-AHP model was constructed and applied first to MFZ evaluation in China. The MFZ comprehensive evaluation value, calculated using the geometric average method, was 0.79 (medium), which revealed that the zoning implementation achieves the desired objectives. However, MFZ implementation evaluation requires further strengthening. Subsequently, suggestions were made to strengthen the evaluation theories and research methods. Simultaneously, the MFZ evaluation system was established in this paper to provide new ideas for MFZ implementation evaluation and management.

Ethnopharmacological relevance Acanthus ilicifolius L. has been used as a folk medicine in the treatment of acute and chronic hepatitis in China for a long time. Phenylethanoid glycosides are one of main components in A. ilicifolius L. Aim of the study: The aim of present study was to assess the hepatoprotective activities of total phenylethanoid glycosides from A. ilicifolius L. (APhGs) against carbon tetrachloride (CCl4)-induced liver injury in vivo and in vitro. Materials and method The APhGs was separated by resin column chromatography. The purity of total phenylethanoid glycosides was determined by UV–Vis spectrophotometry using acteoside as a standard. The hepatoprotective activities of APhGs against CCl4-induced liver injury were performed on experimental mice and L-02 hepatocytes. Moreover, the antioxidant activities of APhGs were tested in vitro. Results The results showed that pre-administration of APhGs to mice decreased alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels in serum, and improved superoxide dismutase (SOD) activity and decreased malondialdehyde (MDA) level in serum and liver tissue induced by CCl4. Specifically, the SOD activities of APhGs-H and APhGs-M treatment groups were stronger than that of silymarin treatment group. The protective activities of APhGs were confirmed by histopathological results. Moreover, immunohistochemical analysis showed that APhGs could remarkably down-regulate the protein expression of tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β). In vitro experiment, APhGs was observed to increase L-02 hepatocyte viability against CCl4-induced hepatotoxicity. In addition, antioxidation assays revealed that APhGs showed 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, and ferric reducing ability. Conclusion Overall, total phenylethanoid glycosides from A. ilicifolius L. displayed promising hepatoprotective effects. These results offer a support for the medicine uses of A. ilicifolius L.

Aspergillus terreus has been reported to produce many secondary metabolites that exhibit potential bioactivities, such as antibiotic, hypoglycemic, and lipid-lowering activities. In the present study, two new thiodiketopiperazines, emestrins L (1) and M (2), together with five known analogues (3&ndash, 7), and five known dihydroisocoumarins (8&ndash, 12), were obtained from the marine-derived fungus Aspergillus terreus RA2905. The structures of the new compounds were elucidated by analysis of the comprehensive spectroscopic data, including high-resolution electrospray ionization mass spectrometry (HRESIMS), one-dimensional (1D) and two-dimensional (2D) nuclear magnetic resonance (NMR), and electronic circular dichroism (ECD) data. This is the first time that the spectroscopic data of compounds 3, 8, and 9 have been reported. Compound 3 displayed antibacterial activity against Pseudomonas aeruginosa (minimum inhibitory concentration (MIC) = 32 &mu, g/mL) and antifungal activity against Candida albicans (MIC = 32 &mu, g/mL). In addition, compound 3 exhibited an inhibitory effect on protein tyrosine phosphatase 1 B (PTP1B), an important hypoglycemic target, with an inhibitory concentration (IC)50 value of 12.25 &mu, M.

Two new unsaturated fatty acids, 6R,8R-dihydroxy-9Z,12Z-octadecadienoic acid (1) and methyl-6R,8R-dihydroxy-9Z,12Z-octadecadienoate (2), and two known 9Z,12Z-octadecadienoic acid analogues (3, 4) together with a known sesquiterpenoid (5) were isolated from the mangrove rhizosphere soil-derived fungus Penicillium javanicum HK1-22. An acetonide derivative (1a) from 1 was also prepared. The relative configuration of 1 was determined by analysis of the 1D and 2D NOE spectra of 1a. The absolute configuration of 1 was assigned on the basis of biogenetic considerations. The antifungal activity of the high yield compound 5 was evaluated against four strains of crop pathogens and it showed significant antifungal activities against all the tested strains.

Four nucleoside derivatives (1-4) were isolated from the fungus Aspergillus versicolor derived from the gorgonian Dichotella gemmacea collected in the South China Sea. Their structures were elucidated by comprehensive spectroscopic method of NMR and MS analysis. All isolated metabolites were evaluated for their cytotoxicity, antibacterial activity and lethality towards brine shrimp Artemia salina. Compounds 1/2 exhibited selective antibacterial activity against Staphylococcus epidermidis with an MIC value of 12.5 μM. It should be noted that 1 and 2, whose structures were listed in SciFinder Scholar, had no associated reference. This is the first report about their isolation, structure elucidation and biological activities.

Chinese marine materia medica (CMMM) is a vital part of traditional Chinese medicine (TCM). Compared with terrestrial TCM, CMMM, derived from specific marine habitats, possesses peculiar chemical components with unique structures reflecting as potent pharmacological activities, distinct drug properties and functions. Nowadays, CMMM appears to be especially effective in treating such difficult diseases as cancers, diabetes, cardio-cerebrovascular diseases, immunodeficiency diseases and senile dementia, and therefore has become an important medicinal resource for the research and development of new drugs. In recent years, such development has attracted wide attention in the field of medicine. In this study, the CMMM resources in China were systematically investigated and evaluated. It was found that the historic experiences of Chinese people using CMMM have continuously accumulated over a period of more than 3600 years, and that the achievements of the research on modern CMMM are especially outstanding. By June 2015, 725 kinds of CMMMs from Chinese coastal sea areas have been identified and recorded, covering 1552 organisms and minerals. More than 3100 traditional prescriptions containing CMMMs have been imparted and inherited. However, the number of CMMMs is less than the 8188 terrestrial TCMs, from more than 12,100 medicinal terrestrial plants, animals and minerals. In the future, the research and development of CMMM should focus on the channel entries (TCM drug properties), compatibility, effective ingredients, acting mechanisms, drug metabolism and quality standard. This study reveals the high potential of CMMM development.

Based on the cooperation network formation theory, a Belt and Road trade cooperation network was constructed from the multi-distances perspective under the backdrop of the Belt and Road initiative. The geographic, factor endowment, cultural, and institutional distances were selected as variables from the aspects of geography, economy, culture, and politics to expand the gravity model. With this model, an empirical test was conducted using the data from China’s export trade flows to Belt and Road countries from 2007 to 2016. The results showed that a Belt and Road country had greater trade flows from China when it had smaller geographic, factor endowment, and cultural distance and greater institutional distance from China. Based on the empirical results, we improved the comprehensive index method to measure the comprehensive distance indices between China and the Belt and Road countries. According to the comprehensive distance indices, these countries could be divided into four cooperation circles, in which the prioritized countries in the different phases were identified. Subsequently, the cooperation network construction was designed in four stages to gradually build an all-round, multi-level, and all-encompassing trade cooperation network between China and the Belt and Road countries. Eventually, based on the above consideration, policy suggestions are provided for the construction of such a network.

Two new eunicellin-based diterpenoids, sibogins A (1) and B (2), along with one known analogue (3), and four known 9,10-secosteroids (4–7), were isolated from the gorgonian Muricella sibogae Nutting collected from the South China Sea. The structures of the new compounds were elucidated by comprehensive analysis of spectroscopic data, especially by using 2D NMR spectra. The antifouling activity on barnacle Balanus amphitrite and lethality towards brine shrimp Artemia salina of all the isolated compounds were evaluated.

One new 18-oxygenated polyhydroxy steroid, (24S)-ergostan-3β,5α,6β,18,25-pentaol 18,25-diacetate (1), along with five known analogues (2-6), was isolated from a soft coral Sarcophyton sp. collected from the South China Sea. The structure of the new compound (1) was elucidated by 1D NMR, 2D NMR and mass spectrometry. The absolute configuration of 1 was determined by the application of the modified Mosher's method. The isolated compounds were assayed for their cytotoxic and antimicrobial activities.

Two new prenylated indole alkaloids, 17-epi-notoamides Q and M (1 and 2), and two new phenyl ether derivatives, cordyols D and E (9 and 13), together with 10 known compounds (3–8, 10–12, 14) were isolated from a marine-derived Aspergillus sp. fungus. Among them, 1/5 and 2/4 were pairs of epimers. The planar structures and absolute configurations of the new compounds were determined by extensive NMR spectroscopic data as well as CD spectra. The absolute configuration of 3 was confirmed by single-crystal X-ray diffraction analysis for the first time. All isolated metabolites (1–14) and eight synthetic phenyl ether derivatives (12a, 14a–14g) were evaluated for their antibacterial activities in vitro. The polybromide phenyl ether 14g showed pronounced antibacterial activity against Staphylococcus epidermidis with an MIC value of 0.556 μM, stronger than that of the positive control ciprofloxacin (MIC = 3.13 μM).

Ten new fungal metabolites, including three hydroisocoumarins, penicimarins A–C (1–3), three isocoumarins, penicimarins D–F (6–8), and four benzofurans, penicifurans A–D (11–14), together with four known isocoumarin derivatives (4, 5, 9, 10), were obtained from the sponge-derived fungus Penicillium sp. MWZ14-4, collected from the South China Sea. Their planar structures and relative configurations were elucidated by detailed analysis of spectroscopic data and by comparison with related known compounds. The absolute configurations of 1–4 were assigned by the modified Mosher’s method and TDDFT ECD calculations together with comparison of their CD spectra. Compound 1 represents a rare naturally occurring isocoumarin derivative with 4-substitution, but no substituent at the 3-position. These compounds were evaluated for antibacterial activities and cytotoxic activities in vitro. Among them, penicifuran A (11) exhibited inhibitory activity against Staphylococcus albus with an MIC value of 3.13 μM.

Chemical investigation of a marine-derived fungus Nigrospora sp., isolated from an unidentified sea anemone, yielded two new hydroanthraquinone analogues, 4a-epi-9α-methoxydihydrodeoxybostrycin (1) and 10-deoxybostrycin (2), together with seven known anthraquinone derivatives (3-9). The structures of the two new compounds were established through extensive NMR spectroscopy as well as a single-crystal X-ray diffraction analysis using Cu Kα radiation. The antibacterial activities of compounds 1-9 and 10 acetyl derivatives (6a, 7a, 8a-8g, 9a) were evaluated in vitro. Compound 6a, the acetylated derivative of 6, exhibited promising activity against Bacillus cereus with an MIC value of 48.8 nM, which was stronger than that of the positive control ciprofloxacin (MIC = 1250 nM). Analysis of the antibacterial screening data for the metabolites and their acetyl derivatives revealed the key structural features required for this activity.

Five new hydroanthraquinone derivatives, tetrahydroaltersolanols C-F (1-4) and dihydroaltersolanol A (5), and five new alterporriol-type anthranoid dimers, alterporriols N-R (12-16), along with seven known analogues (6-11 and 17), were isolated from the culture broth and the mycelia of Alternaria sp. ZJ-2008003, a fungus obtained from a Sarcophyton sp. soft coral collected from the South China Sea. Their structures and the relative configurations were elucidated using comprehensive spectroscopic methods including 1D and 2D NOE spectra as well as single-crystal X-ray crystallography. Compound 13 represents the first isolated alterporriol dimer with a C-4-C-4' linkage, and the absolute configuration of 4 was determined using the modified Mosher's method. Compounds 1 and 15 exhibited antiviral activity against the porcine reproductive and respiratory syndrome virus (PRRSV), with IC₅₀ values of 65 and 39 μM, respectively. Compound 14 showed cytotoxic activity against PC-3 and HCT-116 cell lines, with IC₅₀ values of 6.4 and 8.6 μM, respectively.

Four new bisabolane-type sesquiterpenoids, aspergiterpenoid A (1), (−)-sydonol (2), (−)-sydonic acid (3), and (−)-5-(hydroxymethyl)-2-(2′,6′,6′-trimethyltetrahydro-2H- pyran-2-yl)phenol (4) together with one known fungal metabolite (5) were isolated from the fermentation broth of a marine-derived fungus Aspergillus sp., which was isolated from the sponge Xestospongia testudinaria collected from the South China Sea. Four of them (1–4) are optically active compounds. Their structures and absolute configurations were elucidated by using NMR spectroscopic techniques and mass spectrometric analysis, and by comparing their optical rotations with those related known analogues. Compounds 1–5 showed selective antibacterial activity against eight bacterial strains with the MIC (minimum inhibiting concentrations) values between 1.25 and 20.0 µM. The cytotoxic, antifouling, and acetylcholinesterase inhibitory activities of these compounds were also examined.

Three new phenolic bisabolane sesquiterpenoid dimers, disydonols A-C (1-3), and one known compound (S)-(+)-sydonol (4) were isolated from the fermentation broth of a marine-derived fungus Aspergillus sp., which was isolated from the sponge Xestospongia testudinaria collected from the South China Sea. Their structures were elucidated on the basis of comprehensive spectral analysis including 1D and 2D NMR spectra and HR-ESI-MS. These compounds were evaluated for cytotoxic activity against HepG-2 and Caski human tumour cell lines. Among them, compounds 1 and 3 exhibited cytotoxicity against the two cell lines.

To observe the effects of color silk cocoon extraction-sericine on transforming growth factor-beta1 (TGF-beta1) and Smad3 protein expression in kidney of diabetic nephropathy (DN) rats.60 male SD rats were randomly divided into 5 groups (n = 12): normal control group, DN model group, sericine treatment group, metformin group and sericine prevention group. The rats in model group, sericine treatment group, metformin group and sericine prevention group were all established DN rats model by intraperitoneally injected streptozotocin (STZ). Blood glucoseor = 16.7 mmol/L was taken as standard to judge if the rats model were successfully established. After the rats model were successfully established, the rats in sericine treatment group were lavaged with sericine (2.4 g/(kg x d), 35 d). The rats in metformin group were lavaged with metformin (55.33 mg/(kg x d), 35 d). The rats in sericine prevention group were lavaged with the same dose sericine for 35 d before injecting STZ. The blood glucose and kidney weight/body weight of rats in each group were respectively detected. Immunohistochemical staining was used to observe the expression of TGF-beta1 and Western blot to detect the expression of Smad3 in kidney.Compared with normal control rats: the blood glucose, kidney weight/body weight, TGF-beta1 and Smad3 expression in kidney of rats in model group increased obviously (P0.01). The blood glucose, TGF-beta1 and Smad3 expression in kidney of rats in sericin treatment group, sericin prevention group and metformin group were significantly lower than that of model group (P0.01). Moreover, there were no obvious differences between sericin treatment group, sericin prevention group and metformin group (P0.05). The kidney weight/body weight of rats in sericin treatment group, sericin prevention group and metformin group were significantly lower than that of model group (P0.01). Moreover, the kidney weight/body weight of rats in sericin treatment group and sericin prevention group were obviously lower than that of metformin group (P0.05).Sericin can inhibit activation of TGF-beta1/Smad3 signal pathway in kidney of DN rats, lighten glomerulosclerosis and renal interstitial fibrosis, so has protective and preventive effects on kidney injury of DN rats. Moreover, the therapeutical and preventive effects of sericin on DN are similar with metformin.