New di-spirocyclic labdane diterpenoids from the aerial parts of Leonurus japonicus.

Phytochemical investigation on the ethanol extract of a well-known medicinal herb Leonurus japonicus, led to the separation of 18 labdane type diterpenoids (1-18). Through comprehensive spectroscopic analyses and quantum chemical calculations, these compounds were structurally characterized as six new interesting 5,5,5-di-spirocyclic ones (1-6), two new (7 and 8) and six known (13-18) interesting 6,5,5-di-spirocyclic ones, a new rare 14,15-dinor derivative (9), and three new ones incorporating a γ-lactone unit (10-12). An in vitro neuroprotective assay in RSC96 cells revealed that compounds 7 and 12 exhibited neuroprotective activity in a concentration-dependent way, comparable to the reference drug N-acetylcysteine.

Removal effect of typical pollutants from stormwater runoff in ecological ditches.

Ecological ditches are a typical ecological facility for controlling road stormwater runoff pollution; they mainly remove harmful pollutants from runoff through plant absorption, retention and sedimentation, ecological adsorption, and microbial action. In this paper, according to the transport form of rainwater in the ditches, the removal effects of two different types of ditches on nitrogen, phosphorus, heavy metals, and other pollutants were simulated under three conditions of rainfall, slow flow, and still water, respectively, and their operating characteristics were analyzed. The results showed that the removal rate of TN in the two ecological ditches under slow flow conditions showed a downward trend as a whole with the increase of hydraulic load, and the suitable hydraulic load for TN removal should be selected as 0.3 m3/(m2 day). Under the simulated rainfall conditions, the TN removal rates of no. 1 and no. 2 ditches were 26.1-37.2% and 24.9 ~ 52.5%, respectively, and the TP removal rates were 44.6 ~ 63.3% and 36.1 ~ 62.1%. After 19.4 h and 22.1 h in the static state, the TP concentration in no. 1 ditch and no. 2 ditch reached the surface V water standard, and the average removal rate of TP was 74.7% and 53.7%, respectively. This paper provides a reference for selecting suitable parameters and optimizing the operational performance of ecological ditches to reduce runoff pollutants more effectively.

Jieduquyuziyin prescription enhances CD11a and CD70 DNA methylation of CD4+ T cells via miR-29b-sp1/DNMT1 pathway in MRL/lpr mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Jieduquyuziyin prescription (JP) is a traditional Chinese medicine utilized to treat systemic lupus erythematosus (SLE). Its efficacy has been confirmed through clinical trials and empirical evidence, leading to its authorized use in Chinese hospitals. The development of JP exemplifies the integration of traditional wisdom and scientific approaches, demonstrating the interdisciplinary essence of ethnopharmacology. These results emphasize the potential value of traditional medicine in addressing autoimmune disorders. AIM OF THE STUDY: This study aims to address the effect of JP in MRL/lpr mice and elucidate the pharmacological mechanism by which JP targets CD11a and CD70 DNA methylation via the miR-29b-sp1/DNMT1 pathway. MATERIALS AND METHODS: MRL/lpr mice were divided into three groups: the model group (received distilled water), the positive group (administered AAV/miR-29b-3p inhibitor), and the JP group (treated with JP decoction). C57BL/6 mice were constituted as a control group. Through ELISA assay, serum and urine samples were assessed for anti-dsDNA, TNF-α, TGF-ß, IL-2, and UP. HE and Masson staining were conducted to reveal renal pathology. Genome DNA was extracted from CD4+ T cells of mice spleens to evaluate methylation level. The methylation of CD11a, CD70, and CD40L promoter regions was analyzed by targeted bisulfate sequencing. Their expression at the mRNA and protein levels was examined using quantitative real-time PCR, western blot analysis, immunohistochemistry, and immunofluorescence staining of kidney tissues. Furthermore, the molecular mechanisms underlying the regulation of the miR-29b-sp1/DNMT1 pathway by JP were explored with Jurkat cells transfected with miR-inhibitors or miR-mimics. RESULTS: Mice treated with JP exhibited a significant decrease in anti-dsDNA, TNF-α, TGF-ß, and UP, accompanied by a significant increase in IL-2. HE staining revealed JP effectively mitigated renal inflammatory response, while Masson staining indicated a reduction in collagen fiber content. In addition, JP exhibited a significant impact on the global hypomethylation of SLE, as evidenced by the induction of high methylation levels of CD11a and CD70 promoter regions, mediated through the miR-29b-sp1/DNMT1 pathway. CONCLUSION: Our findings demonstrate JP exerts a protective effect against spontaneous SLE development, attenuates renal pathological changes, and functions as a miRNA inhibitor to enhance CD11a and CD70 DNA methylation through the modulation of the miR-29b-sp1/DNMT1 pathway.

Efficacy of laser therapy for temporomandibular disorders: A systematic review and meta-analysis.

OBJECTIVE: The aim of this systematic review was to evaluate the efficacy of laser therapy in temporomandibular disorders (TMD). METHODS: Randomized controlled trials (RCTs) in regard to this issue were searched in electronic databases. Three investigators independently screened the eligible studies, and the quality of the included studies was assessed according to the risk of bias tool recommended by the Cochrane handbook. The primary outcome measure was the degree of pain, reported on a visual analog scale (VAS), and the secondary outcome measures were TMJ function, including maximum active vertical opening (MAVO), maximum passive vertical opening (MPVO), left and right lateral movement (LLE, RLE). Pooled effect sizes were calculated using random effects models and 95% confidence interval (95% CI). RESULTS: A total of 28 randomized controlled trials were included. Laser therapy had a more significant effect in terms of VAS (SMD=ï¹£1.88; 95% CI=ï¹£2.46 toï¹£1.30; P < 0.00001; I2 =93%), MAVO (MD = 4.90; 95% CI= 3.29-6.50; P < 0.00001; I2 =72%), MPVO (MD=5.82; 95% CI= 4.62-7.01; P < 0.00001; I2 =40%) and RLE (MD = 0.73; 95% CI= 0.23-1.22; P = 0.004; I2 = 0%) as compared to placebo group. However, there was no significant difference in LLE between two groups (MD= 0.35; 95% CI=ï¹£0.31-1.01; P = 0.30; I2 =0%). CONCLUSIONS: Laser therapy can effectively reduce pain but have small effect on improving mandibular movement of TMD patients. More well-designed RCTs with large sample sizes are needed for further validation. And these studies should report detailed laser parameters and provide complete outcome measure data.

Fermented Gynochthodes officinalis (F.C.How) Razafim. & B.Bremer alleviates diabetic erectile dysfunction by attenuating oxidative stress and regulating PI3K/Akt/eNOS pathway.

ETHNOPHARMACOLOGICAL RELEVANCE: As a traditional Chinese medicine, Gynochthodes officinalis (F.C.How) Razafim. & B.Bremer (G. officinalis) has been historically as tonics to treat impotence. Fermentation is an ancient processing method for traditional Chinese medicine. Whether fermentation affects the therapeutic effects of G. officinalis on diabetic erectile dysfunction has so far remained unknown. AIMS OF THE STUDY: In this research, we aim to determine the effect of fermented or unfermented G. officinalis root extract on diabetes mellitus-induced erectile dysfunction (DMED) and the potential mechanisms. MATERIALS AND METHODS: Candida sp. B5, Lactobacillus sp. Y5 and Lactobacillus sp. R2 are applied for the fermentation of G. officinalis. The optimum fermentation conditions of G. officinalis are investigated. Sprague-Dawley rats were used to establish a diabetic erectile dysfunction model, treated with different concentrations of fermented or unfermented G. officinalis, to compare the effect of fermented or unfermented G. officinalis on DMED and explore underlying mechanisms by assessment of intracavernous pressure, ELISA, Western blot, Masson's trichrome staining, and immunofluorescence. The corpus cavernosum smooth muscle cells (CCSMCs) and Schwann cells were isolated and used to investigate the effect of fermented or unfermented G. officinalis on hydrogen peroxide (H2O2)-induced apoptosis. RESULTS: The results reveal the optimum fermentation conditions of G. officinalis using Lactobacillus sp. Y5 were determined to be 35 °C, the ratio of solid to liquid 1:10, and six days of fermentation. The fermentation increases the abundance of major active ingredients within G. officinalis. After fermented or unfermented G. officinalis treatment for eight weeks by oral gavage at a dose of 100 mg kg-1 or 300 mg kg-1, the results show that the fermentation enhances the effect of G. officinalis on diabetic erectile dysfunction detected by intracavernous pressure. The protein expressions of the PI3K/Akt/eNOS pathway were upregulated in diabetic rats after fermented or unfermented G. officinalis treatment, while the level of oxidative stress was significantly reduced. Meanwhile, Masson's trichrome staining also displayed an improvement in the ratio of smooth muscle to collagen. In vitro experiments confirmed that fermented or unfermented G. officinalis protected CCSMCs and Schwann cells from apoptosis. In contrast, fermented G. officinalis showed a fortified protective effect over unfermented G. officinalis. CONCLUSION: Our findings suggest that fermentation can increase the composition of main active ingredients in G. officinalis and enhance its role in diabetic erectile dysfunction. It augurs the potential therapeutic application of fermented G. officinalis well for treating diabetic erectile dysfunction.

Unraveling the mechanism of ethyl acetate extract from Prismatomeris connata Y. Z. Ruan root in treating pulmonary fibrosis: insights from bioinformatics, network pharmacology, and experimental validation.

Introduction: Pulmonary fibrosis is a terminal lung disease characterized by fibroblast proliferation, extracellular matrix accumulation, inflammatory damage, and tissue structure destruction. The pathogenesis of this disease, particularly idiopathic pulmonary fibrosis (IPF), remains unknown. Macrophages play major roles in organ fibrosis diseases, including pulmonary fibrosis. The phenotype and polarization of macrophages are closely associated with pulmonary fibrosis. A new direction in research on anti-pulmonary fibrosis is focused on developing drugs that maintain the stability of the pulmonary microenvironment. Methods: We obtained gene sequencing data and clinical information for patients with IPF from the GEO datasets GSE110147, GSE15197, GSE24988, GSE31934, GSE32537, GSE35145, GSE53845, GSE49072, GSE70864, and GSE90010. We performed GO, KEGG enrichment analysis and GSEA analysis, and conducted weighted gene co-expression network analysis. In addition, we performed proteomic analysis of mouse lung tissue. To verify the results of bioinformatics analysis and proteomic analysis, mice were induced by intratracheal instillation of bleomycin (BLM), and gavaged for 14 days after modeling. Respiratory function of mice in different groups was measured. Lung tissues were retained for histopathological examination, Western Blot and real-time quantitative PCR, etc. In addition, lipopolysaccharide, interferon-γ and interleukin-4 were used to induce RAW264.7 cells for 12h in vitro to establish macrophage inflammation and polarization model. At the same time, HG2 intervention was given. The phenotype transformation and cytokine secretion of macrophages were investigated by Western Blot, RT-qPCR and flow cytometry, etc. Results: Through bioinformatics analysis and experiments involving bleomycin-induced pulmonary fibrosis in mice, we confirmed the importance of macrophage polarization in IPF. The analysis revealed that macrophage polarization in IPF involves a change in the phenotypic spectrum. Furthermore, experiments demonstrated high expression of M2-type macrophage-associated biomarkers and inducible nitric oxide synthase, thus indicating an imbalance in M1/M2 polarization of pulmonary macrophages in mice with pulmonary fibrosis. Discussion: Our investigation revealed that the ethyl acetate extract (HG2) obtained from the roots of Prismatomeris connata Y. Z. Ruan exhibits therapeutic efficacy against bleomycin-induced pulmonary fibrosis. HG2 modulates macrophage polarization, alterations in the TGF-ß/Smad pathway, and downstream protein expression in the context of pulmonary fibrosis. On the basis of our findings, we believe that HG2 has potential as a novel traditional Chinese medicine component for treating pulmonary fibrosis.

Paeoniflorin Inhibits LPS-Induced Activation of Splenic CD4+ T Lymphocytes and Relieves Pathological Symptoms in MRL/lpr Mice by Suppressing IRAK1 Signaling.

Interleukin-1receptor-associated kinase 1 (IRAK1) plays a critical role in systemic lupus erythematosus (SLE). It was reported that SLE was associated with an inflammatory response mediated by defective immune tolerance, including overproduction of autoantibodies, chronic inflammation, and organ damage. Previous reports stated paeoniflorin (PF) had an immunosuppressive effect. The purpose of this study was to determine the anti-inflammatory effect of PF in SLE and its underlying mechanisms. Followed by induced with lipopolysaccharide (LPS), the splenocytes and the isolated CD4+ T lymphocytes of MRL/lpr mice were divided into three groups: control group, LPS group, and LPS + PF group, respectively. MRL/MP mice were used as the control group (treated with distilled water). The MRL/lpr mice were randomly divided into three groups: the model group (treated with distilled water), the prednisone group, and the PF group. The MRL/lpr mice were treated with prednisone acetate (5 mg/kg) and PF (25, 50, and 75 mg/kg) for eight weeks. Subsequently, ELISA, qRT-PCR, western blotting, HE, and Masson staining were performed to detect various indicators. The results of Cell Counting Kit-8 (CCK-8) showed that 10 µg/mL of LPS had the optimum effect on cell viability, and 50 µmol/L of PF had no obvious cytotoxicity to LPS-treated cells. PF reduced the expression level of IRAK1-nuclearfactor-κB (NF-κB) and its downstream inflammatory cytokines in the splenocytes and CD4+ T lymphocytes of MRL/lpr mice stimulated by LPS, especially in the latter. The serum antibody contents in the PF group mice were reduced, and the kidney damage was also alleviated accordingly. Moreover, the IRAK1/inhibitor of the nuclear factor-κB kinase (IKK)/NF-κB inhibitor (IκB)/NF-κB pathways was found to be involved in the anti-inflammation effect of PF in the kidney and spleen. In conclusion, it is thought that PF may have the potential to be used as a therapeutic agent to reduce the inflammatory activity of SLE. Inhibition of the IRAK1-NF-κB pathway may help formulate novel therapeutic tactics for SLE.

Acupuncture Based on Regulating Autonomic Nerves for the Prevention of Migraine Without Aura: A Prospective, Double-Dummy, Randomized Controlled Clinical Trial.

Background: Migraine without aura (MWoA) is a nervous system disease, which is closely related to autonomic nerves dysfunction. As a popular non-pharmacological alternative treatment for preventing migraine, it remains unclear whether the acupuncture can prevent MWoA. Thus, this trial aims to evaluate the preventive effect and safety of the acupuncture method of stimulating acupoints that regulate autonomic nerves in MWoA patients. Methods: This is a single-center, prospective, double-dummy, randomized controlled clinical trial. A total of ninety-six patients with MWoA are randomly allocated to acupuncture combined with the placebo group and sham acupuncture combined with the medication group in a 1:1 ratio. All subjects will receive intervention for 8 weeks and follow-up assessments three times (one month, three months, and six months in follow-up visiting). The frequency of acupuncture in both groups is three times a week for eight weeks. The primary outcome will be evaluated using a visual analog scale (VAS) and the number of migraine attacks per four weeks. The secondary outcome measures will include the migraine-specific quality of life (MSQOL) scale and headache needs assessment survey (HANA) questionnaire scale. Results: The acupoint selection of this clinical trial is based on the combination of traditional Chinese medicine theory with modern medicine, thereby evaluating the efficacy and safety of the acupuncture method of stimulating acupoints that regulate autonomic nerves in the prevention of MWoA. The results may provide evidence of the beneficial effects of acupuncture on the prevention of MWoA by regulating autonomic nerves dysfunction. Trial Registration: ClinicalTrials.gov NCT04766762.

Effects of Tai Chi and Walking Exercise on Emotional Face Recognition in Elderly People: An ERP Study.

Both tai chi and walking can improve the physical health of the elderly, but the effect on the emotional cognitive function of the elderly is unclear. To investigate the effect of long-term walking and tai chi exercise on the emotional cognitive function of the elderly, 63 subjects were recruited in this study according to age and exercise habits, including 16 in the youth control group, 15 in the elderly non-exercise control group, 17 in the elderly walking group, and 18 in the elderly tai chi group. The "learning-test paradigm" of emotional faces was used to measure the subjects' ability to recognize and remember emotional (negative and neutral) faces. Behavioral and EEG data were recorded during the learning and testing phases. The results showed that there is aging in emotional cognition in older adults compared with younger adults. Long-term walking and tai chi exercise can delay the deterioration of emotional cognitive function in older adults to some extent. Both walking and tai chi exercise can delay the decline in aging-related emotional face recognition function to some extent. Walking exercise can delay the decline in aging-related emotional face memory function to some extent.

Jieduquyuzishen Prescription Attenuates Renal Fibrosis in MRL/lpr Mice via Inhibiting EMT and TGF-ß1/Smad2/3 Pathway.

Jieduquyuziyin prescription (JP) has been used to treat lupus nephritis (LN) and its effectiveness in the treatment of LN has been clinically proven, but the underlying mechanisms have yet to be completely understood. This aim of this study was to clarify the efficacy of JP on the epithelial-mesenchymal transition (EMT) of renal tubular epithelial cells and the molecular mechanisms of JP in MRL/lpr mice. In vivo, we observed the therapeutic actions of JP in MRL/lpr mice as well as its antifibrosis effect and potential mechanism. In vitro, we evaluated the role of JP in EMT and its possible mechanism through the EMT of human renal proximal tubular epithelial cells (HK-2) induced by transforming growth factor-beta 1 (TGF-ß1) and M2c macrophages. HK-2 cells were treated with JP-treated serum, and MRL/lpr mice were treated by JP for 8 weeks. The results showed that JP alleviated disease activity, improved renal function, decreased proteinuria, and improved renal injury and fibrosis in MRL/lpr mice. Furthermore, JP suppressed the activation of the TGF-ß1/Smad2/3 signaling pathway, upregulated the E-cadherin levels, and downregulated the Vimentin and mesenchymal α-smooth muscle actin (α-SMA) levels in the kidney of MRL/lpr mice. JP was further found to prevent the TGF-ß1 and M2c macrophages-induced EMT of HK-2 cells. Collectively, JP could alleviate the disease activity of MRL/lpr mice, improve renal function, and attenuate renal fibrosis, and its underlying mechanisms may be related to the inhibition of EMT and TGF-ß1/Smad2/3 signaling pathway.

The Association Between Sleep Disorders and Incidence of Dry Eye Disease in Ningbo: Data From an Integrated Health Care Network.

PURPOSE: To investigate the association between sleep disorders and dry eye disease (DED) in Ningbo, China. METHODS: Our data came from the Yinzhou Health Information System (HIS), including 257932 patients and was based on a 1:1 matching method (sleep disorder patients vs. patients without sleep disorders) during 2013-2020. Sleep disorders and DED were identified using ICD-10 codes. Cox proportional hazards regression was used to identify the association between sleep disorders and DED. RESULTS: The eight-year incidence of DED was significantly higher in participants with diagnosis of sleep disorders (sleep disorders: 50.66%, no sleep disorders: 16.48%, P < 0.01). Sleep disorders were positively associated with the diagnosis of DED (HR: 3.06, 95% CI: 2.99-3.13, P < 0.01), when sex, age, hypertension, diabetes and other systemic diseases were adjusted. In the sleep disorders patients, advancing age, female sex, and presence of coexisting disease (hypertension, diabetes, hyperlipidemia, thyroid disease, depression, heart disease, and arthritis) were significantly associated with the development of DED by the multivariate cox regression analysis (all P < 0.05).In addition, there was a significantly positive association between estazolam and the incidence of DED in both sleep disorder and non-sleep disorder groups (all P < 0.05). CONCLUSIONS: Sleep disrder was associated with a three-time increased risk of DED. This association can be helpful in effective management of both sleep disorders and DED.

Jieduquyuziyin Prescription alleviates hepatic gluconeogenesis via PI3K/Akt/PGC-1α pathway in glucocorticoid-induced MRL/lpr mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Jieduquyuziyin prescription (JP) is a traditional Chinese medicine (TCM) formula. According to both TCM theory and more than a decade of clinical practice, JP has been testified to be effective for systemic lupus erythematosus (SLE) treatment as an approved hospital prescription in China. AIM OF THE STUDY: To determine the effect of JP on the treatment of SLE by glucocorticoid (GC) and to further examine the molecular mechanisms. MATERIALS AND METHODS: We conducted in vivo experiments to estimate the effect of JP on hepatic gluconeogenesis in MRL/lpr mice treated with GC. Additionally, isoproterenol (ISO) induced hepatic gluconeogenesis model and GC-treated MRL/lpr mouse hepatocytes were carried out in vitro experiments to verify the effect of JP on gluconeogenesis. RESULTS: The results showed that JP combined with GC could effectively alleviate the lupus symptoms in MRL/lpr mice and improve the pathological changes of the kidney and liver. And the combination of JP reduced the side effects caused by GC, which was related to the inhibition of GC-induced hepatic gluconeogenesis in MRL/lpr mice. Specifically, JP up-regulated the expression of glucocorticoid receptor (GR) α, phosphoinositide-3-kinase (PI3K) and Akt restrained by GC to reduce the production of forkhead box O1 (FoxO1), peroxisome proliferator-activated receptor-gamma coactivator-1α (PGC-1α), and the gluconeogenic genes phosphoenolpyruvate carboxykinase (PEPCK) and glucose-6-phosphatase (G6Pase). In vivo, the use of JP either alone or with GC could reduce spleen enlargement, high levels of serum antibodies, aggravated urine protein and renal pathological damage in MRL/lpr mice. Furthermore, the glucose content was reduced in the liver of MRL/lpr mice treated with JP, and the liver damage and steatosis were also alleviated. In vitro, the expressions of PI3K and Akt increased and the expressions of FoxO1, PGC-1α, PEPCK and G6Pase decreased after JP treatment in ISO-treated hepatocytes. Compared with MRL/MP mice, we found that JP could significantly inhibit the expression of gluconeogenesis in the hepatocytes of MRL/lpr mice induced by GC to a greater extent. CONCLUSIONS: The therapeutic effect of JP on GC-induced is likely related to hepatic gluconeogenesis, which provides a new perspective to reveal the positive role of JP in SLE.

[Selection of optimal qRT-PCR reference genes for Aconitum vilmorinianum].

Screening suitable reference genes is the premise of quantitative Real-time PCR(qRT-PCR)for gene expression analysis. To provide stable reference genes for expression analysis of genes in Aconitum vilmorinianum, this study selected 19 candidate re-ference genes(ACT1, ACT2, ACT3, aTUB1, aTUB2, bTUB, 18S rRNA, UBQ, eIF2, eIF3, eIF4, eIF5, CYP, GAPDH1, GAPDH2, PP2A1, PP2A2, ACP, and EF1α) based on the transcriptome data of A. vilmorinianum. qRT-PCR was conducted to profile the expression of these genes in the root, stem, leaf, and flower of A. vilmorinianum. The Ct values showed that 18S rRNA with high expression level and GAPDH2 with large expression difference among organs were not suitable as the reference genes. NormFinder and geNorm showed similar results of the expression stability of the other candidate reference genes and demonstrated PP2A1, EF1α, and CYP as the highly stable ones. However, BestKeeper suggested EF1α, ACT3, and PP2A1 as the top stable genes. In view of the different results from different softwares, the geometric mean method was employed to analyze the expression stability of the candidate re-ference genes, the results of which indicated that PP2A1, EF1α, and ACT3 were the most stable. Based on the comprehensive analysis results of geNorm, NormFinder, BestKeeper, and geometric mean method, PP2A1 and EF1α presented the most stable expression in different organs of A. vilmorinianum. PP2A1 and EF1α were the superior reference genes for gene expression profiling in different organs of A. vilmorinianum.

DrugComb update: a more comprehensive drug sensitivity data repository and analysis portal.

Combinatorial therapies that target multiple pathways have shown great promises for treating complex diseases. DrugComb (https://drugcomb.org/) is a web-based portal for the deposition and analysis of drug combination screening datasets. Since its first release, DrugComb has received continuous updates on the coverage of data resources, as well as on the functionality of the web server to improve the analysis, visualization and interpretation of drug combination screens. Here, we report significant updates of DrugComb, including: (i) manual curation and harmonization of more comprehensive drug combination and monotherapy screening data, not only for cancers but also for other diseases such as malaria and COVID-19; (ii) enhanced algorithms for assessing the sensitivity and synergy of drug combinations; (iii) network modelling tools to visualize the mechanisms of action of drugs or drug combinations for a given cancer sample and (iv) state-of-the-art machine learning models to predict drug combination sensitivity and synergy. These improvements have been provided with more user-friendly graphical interface and faster database infrastructure, which make DrugComb the most comprehensive web-based resources for the study of drug sensitivities for multiple diseases.

Bioactive aromatic butenolides from a mangrove sediment originated fungal species, Aspergillus terreus SCAU011.

Seven new compounds including five aromatic butenolide analogues (1-5), one quinazolinone alkaloid (6) and one benzoic acid derivative (7), along with eleven known co-metabolites (8-18), were isolated from Aspergillus terreus SCAU011, a fungus from the rhizosphere sediment of a mangrove plant Rhizophora stylosa. The structures of these isolates were established by a combination of MS, NMR and ECD data analyses, as well as chemical method. Compound 3 is a rare ring-open aromatic butenolide, while 6 represents the first natural ring-open benzomalvin-type quinazolinone alkaloid. Also, the previously reported structures for asperlides A-C were proposed to be revised in the present work. The COX-2 inhibitory, α-glucosidase inhibitory, antioxidant and antibacterial activities of all the compounds were assessed. While compounds 4, 6, 11 and 18 exhibited better COX-2 inhibitory activity than the positive control celecoxib, compounds 9 and 10 showed significant α-glucosidase inhibitory activity with IC50 values of 56.1 and 12.9 µM, respectively. Meanwhile, half of the tested samples (1, 8-11 and 15-17) exerted similar or better antioxidant activity compared with the reference drug curcumin, and compounds 3, 9, 17 and 18 displayed moderate antibacterial effect against Staphylococcus aureus.

Thiophene enantiomers from the aerial parts of Eclipta prostrata.

Ten thiophene derivatives (1-10), including two previously undescribed ones (1 and 2), have been obtained and structurally characterized from the aerial parts of a traditional Chinese herb Eclipta prostrata. Six of them with one chiral center were identified to be scalemic mixtures, and the pure enantiomers of two isolates (1 and 3) were successfully separated via chemical derivatization and chiral HPLC, with the absolute configurations being established by analysis of optical rotations. All the thiophenes were subjected to a series of assays and compounds 9 and 10 exhibited mild antibacterial activity against Staphylococcus aureus.[Formula: see text].

Prenylated indole alkaloids and lignans from the flower buds of Tussilago farfara.

Six new compounds including four prenylated indole alkaloids (1-4) and two lignans (5-6), along with eight known cometabolites (7-14), were isolated from the flower buds of Tussilago farfara. Structures of the new compounds were elucidated by comparison with structurally related known analogues and also by comprehensive spectroscopic analyses. Their absolute configurations were determined by a variety of means including Mosher's method, Marfey's analysis, electronic circular dichroism (ECD) exciton chirality method and ECD calculations. Our bioassays have established that compounds 1 and 2 showed potent α-glucosidase inhibitory activity with IC50 values of 105 ± 4.7 and 35.2 ± 3.2 µM, respectively, while the known 13 and 14 exerted moderate DPPH radical scavenging activity with IC50 values of 45.2 ± 2.9 and 29.2 ± 2.0 µM, respectively.

New antibacterial thiophenes from Eclipta prostrata.

Three new thiophene derivatives, ecliprostins A-C (1-3), have been isolated from the aerial parts of a Compositae medicinal plant Eclipta prostrata, and structures of them have been elucidated by comprehensive spectroscopic analyses. Both ecliprostins A (1) and B (2) feature an acetylenic bithiophenyl backbone and also incorporate an isovalerate moiety, while ecliprostin C (3) is a symmetrical dimer of compound 1 and represents the first example bonded via an ether bridge among the very limited natural dimers. All three compounds show antibacterial activity against Staphylococcus aureus.