Natural small-molecule-based co-assembled hydrogels show great promise for stimuli-responsive drug delivery, yet the effects of biologically ubiquitous salts on their performance remain poorly investigated. Hyperhidrosis (HH) is a common chronic disorder with limited therapeutic options, and topical anticholinergics often cause adverse effects. Herein, we developed a sweat-responsive hydrogel platform for HH treatment. GA-OXY and GA-GLY hydrogels were prepared by co-assembling GA with oxybutynin (OXY) and glycopyrrolate (GLY) in ultrapure water; GA-OXY-U and GA-GLY-U hydrogels were obtained analogously in aqueous urea solution. GA-OXY hydrogel was selected as the representative to investigate its self-assembly mechanism, structural characteristics and rheological properties. This hydrogel was fabricated via electrostatic interactions and hydrogen bonding. It exhibited sweat responsiveness mainly because sweat disrupted the intermolecular electrostatic interactions. An appropriate amount of urea did not significantly alter its structural and rheological properties. Additionally, the hydrogel possessed antibacterial, anti-inflammatory, and decontaminating activities against sweat-associated cutaneous complications, with favorable biocompatibility. In vitro degradation assays revealed faster degradation in sweat than in pure water; urea incorporation further accelerated this process. This degradation behavior correlated well with drug release kinetics, and the release rates of GA-OXY-U and GA-GLY-U were positively correlated with urea concentration. Transdermal assays confirmed these hydrogels enhanced the transdermal penetration and skin retention of anticholinergics. Rat plantar antiperspirant assays confirmed that the hydrogel exerted antiperspirant effects via sweat-triggered on-demand drug release. This work provides a promising strategy for HH treatment and suggests that salts may affect the drug release behavior of natural small-molecule-based hydrogels co-assembled via intermolecular electrostatic interactions.
Strawberries suffer a rapid post-harvest deterioration. While hydrogels aid preservation, most focus on post-harvest use. We developed a novel herbal hydrogel (GOB-gel) co-assembled from glycyrrhizic acid (GA), oxymatrine (OMT), and berberine (BBR), and evaluated its pre-harvest application for effects on strawberry quality and shelf-life. BBR facilitated GA and OMT co-assembly, strengthening the hydrogel's structure and enhancing its adhesion and antibacterial activity. Pre-harvest treatment of strawberries with GOB-gel increased their flavonoids, phenolics, peroxidase activity, superoxide dismutase activity, vitamin C, and soluble sugar (p < 0.05). At 25 °C (6 days), weight loss rate and decay rate decreased from 36 % to 23 % and 54 % to 10 %, respectively; at 4 °C (26 days), they dropped from 47 % to 29 % and 24 % to 4 %, respectively. This pre-harvest strategy integrates endogenous biosynthesis of antioxidants and antibacterial agents with exogenous protection, enhancing strawberry quality and extending shelf life.
ETHNOPHARMACOLOGICAL RELEVANCE:Jiawei Yanghe Decoction (JWYHD) is a modified version traditional Chinese medicine formula Yanghe Decoction which has been used to treat various autoimmune diseases. However, the effect of JWYHD on pulmonary sarcoidosis remains unclear. AIM OF THE STUDY:This study aimed to determine the therapeutic efficacy and potential mechanism of action of JWYHD in pulmonary sarcoidosis. MATERIALS AND METHODS:A murine model of sarcoidosis was established by intravenous injection of inactivated Propionibacterium acnes and mature dendritic cells to assess the efficacy of JWYHD. Lung tissue mRNA sequencing was conducted to identify the targets of JWYHD's action. Molecular docking verified of the interaction between identified compounds and key targets. RESULTS:JWYHD treatment alleviated the formation of granulomas in the lung tissue of sarcoidosis model mice. JWYHD significantly attenuated the pulmonary accumulation of macrophages and CD4+T lymphocytes in sarcoidosis mice, and effectively suppressed the proportion of Th17 cells and the levels of IL-17A and TNF-α in BALF, which are pivotal in the pathogenesis of granuloma formation and progression. The therapeutic efficacy of JWYHD was found to be equivalent to that of prednisone. RNA-seq revealed that JWYHD upregulated Nr1d1/2 expression in the lung tissue. Nr1d1/2 is highly expressed in Th17 cells and regulates their differentiation. The NR1D1/2 agonist SR9009 could inhibit Th17 cell proportion and reduce the formation of pulmonary granuloma, exhibiting effects similar to those of JWYHD. Molecular docking result showed that Cyclocephaloside II, Epimedin B, Glycyrrhetic acid, Glycyrrhizic acid, Uralsaponin B, and Uralsaponin U may be key compounds in JWYHD for the treatment of pulmonary sarcoidosis, which had a strong binding ability for NR1D1/2. CONCLUSIONS:JWYHD might exert a therapeutic benefit in pulmonary sarcoidosis through upregulating NR1D1/2 and suppressing Th17 cells. NR1D1/2 might serve as a therapeutic target for the treatment of pulmonary sarcoidosis.
How to improve the treatment efficiency has always been a key problem that needs to be solved in the bio-degradation of phenolic pollutant. The nanomaterials could improve the activity and tolerance of microorganisms, as well as the metabolic efficiency for pollutants under certain conditions. In this research, the effect of nano magnesium oxide (Nano-MgO) on the degradation of phenol by Rhodococcus ruber ATCC 31338 was studied. Moreover, the degradation mechanism of Rhodococcus ruber and Nano-MgO composite system was studied. Results showed that the addition of Nano-MgO could improve the phenol removal efficiency. With the presence of Nano-MgO at 100mg/L to 300mg/L, Rhodococcus ruber showed better growth and efficiency in removing phenol. However, when the concentration of Nano-MgO achieved 400mg/L, the growth of Rhodococcus ruber was inhibited. Enzyme activity experiments suggested that the presence of Nano-MgO had a significant positive effect on the enzyme activity of catechol 1,2-dioxygenase (C12O) and catechol 2,3-dioxygenase (C23O), especially to C23O. The present of Nano-MgO might change the cleavage pathway of catechol. In addition, phosphorus is a limiting factor for the growth of Rhodococcus ruber. The addition of MgO-P materials prepared by encapsulating phosphorus on Nano-MgO can achieve efficient degradation of phenol by Rhodococcus ruber in the phosphorus loss system. This result also proved that nanomaterials can enhance the removal efficiency of organic matter by microorganisms. This study could provide a new solution for improving the microbial degradation rate of phenolic substances.
Marine sponges are well known as prolific producers of structurally diverse molecules with valuable pharmacological potential. As part of our ongoing program to discover bioactive compounds from marine sponges collected from the Xisha Islands in the South China Sea, a chemical study on the specimens of Hippospongia lachne was conducted. As a result, eight undescribed compounds, including four zwitterionic alkylpyridinium salts, hippospondines A−D (1−4), and four 3-alkylpyridine alkaloids, hippospondines E (5), F (6), and (±)-hippospondine G (7), were isolated from the marine sponge H. lachne, together with one known 3-alkylpyridine alkaloid (8). The undescribed structures were elucidated by HRESIMS, NMR, DP4+ and CP3 probability analysis, and the Snatzke's method. Hippospondines A−D (1−4) represent the rare example of inner salt type alkylpyridinium alkaloid with a farnesyl moiety. Compounds 1−3 and 8 were subjected to cytotoxic and lymphocyte proliferation assays. Compound 3 exhibited a weak promotion effect on the ConA-induced T lymphocyte proliferation.
Objective. To probe into the ameliorative effect of Yanghe Decoction on pulmonary injury and immunologic derangement in asthmatic mice. Methods. C57BL/6 mice were randomized into control (Con), Model, and Yanghe Decoction (YHF) groups, with 12 in each. The asthma model of adult female mice was induced by ovalbumin in the Model group, and the YHF group was treated by Yanghe Decoction on the basis of asthma modeling. The Con group received the same amount of normal saline. Inspiratory resistance (Ri), expiratory resistance (Re), lung compliance (CL), and maximal voluntary ventilation (MVV) were measured after modeling. Lung tissue was collected for the measurement of interleukin (IL)-4, IL-5, IL-6, IL-10, IL-13, and tumor necrosis factor-α (TNF-α) by ELISA kits. Combined with HE staining and PAS staining, the pathological alterations of the lung in each group were observed, and CD4+, Th2, and Th1 contents were determined by flow cytometry (FCM). Results. The pulmonary function (PF) test revealed notably reduced Ri and Re as well as enhanced CL and MVV in asthmatic mice after the application of Yanghe Decoction. Yanghe Decoction dramatically ameliorated the pathological changes of lung tissue in asthmatic mice, as demonstrated by the staining results. ELISA results showed that Yanghe Decoction validly reduces lung tissue IL-4, IL-5, IL-6, IL-13, TNF-α and upregulates IL-10 in asthmatic mice. FCM indicated that Yanghe Decoction obviously reduced the number of Th1 and Th2 cells in asthmatic mice, although it caused the decrease of CD4+ cells, but the difference was not statistically significant. Conclusions. Yanghe Decoction can effectively ameliorate the inflammatory reaction, immune cell disorder, and PF injury in ovalbumin-induced asthmatic mice.
Mycoplasma pneumoniae pneumonia (MPP) represents a common respiratory disease in children patients. Kukoamine A (KuA) is a spermine alkaloid found in the Chinese herb Cortex Lycii radices, which has a variety of pharmacological properties. However, no study has been reported on the role of KuA in MPP. Exosomes, a type of lipid bilayer-enclosed extracellular vesicles, can be delivered to the target cells, where they regulate function and physiology. With the use of human alveolar basal epithelial cells (HABECs) as an in vitro model, in this study, we sought to characterize the changes in levels of superoxide dismutase 2 (SOD2) and proinflammatory cytokines including IL-6 and TNF-α in HABECs in response to exosomes, which were isolated from peripheral blood serum of MPP patients. We found that, compared to normal, MPP patients exhibited a significant up-regulated miR-222-3p. Further, exosomal miR-222-3p downregulated SOD2 activity but promoted nuclear NF-κB activity and expression of IL-6 and TNF-α in HABECs, ultimately leading to an oxidative stress condition. Interestingly, such stimulating effects were attenuated by the pretreatment of KuA. This study suggests a critical role possessed by KuA in MPP by regulating the miR-222-3p/SOD2 axis, which represents a promising strategy for the treatment of MPP.
Simplextone E (1), a new metabolite of polyketide origin, was isolated with eight known analogues (2–9) from the South China Sea sponge Plakortis sp. The relative configuration of the new compound was elucidated by a detailed analysis of the spectroscopic data and quantum mechanical calculation of NMR chemical shifts, aided by the newly reported DP4+ approach. Its absolute configuration was determined by the TDDFT/ECD calculation. Simplextone E (1) is proven to be one of the isomers of simplextone D. The absolute configuration at C-8 in alkyl chain of plakortone Q (2) was also assigned based on the NMR calculation. In the preliminary in vitro bioassay, compounds 6 and 7 showed a selective growth inhibitory activity against HCT-116 human colon cancer cells with IC50 values of 8.3 ± 2.4 and 8.4 ± 2.3 μM, corresponding to that of the positive control, adriamycin (IC50 4.1 μM). The two compounds also showed selective activities towards MCF-7 human breast cancer and K562 human erythroleukemia cells while compound 3 only displayed weak activity against K562 cells.
Seven new briarane diterpenoids, gemmacolides AZ–BF (1–7), were isolated together with eight known analogues (8–15) from the South China gorgonian Dichotella gemmacea. Their structures were elucidated based on detailed spectroscopic analysis and a comparison with reported data. In an in vitro bioassay, these compounds exhibited different levels of growth inhibition activity against A549 and MG63 cells, giving continuous evidences about the biological contribution of functional groups at C-2, C-12, C-13, and C-16. These compounds were also evaluated for their antibacterial and antifungal activities. Compound 8 exhibited a potential antibacterial activity against both Gram-positive bacterium Bacillus megaterium and Gram-negative bacterium Escherichia coli.
Seven new briarane diterpenoids, gemmacolides AS-AY (1–7), were isolated together with ten known analogues (8–17) from the South China Sea gorgonian Dichotella gemmacea. The structures of the new compounds were elucidated by the detailed analysis of spectroscopic data and comparison with reported data. The absolute configuration of compounds was determined based on electronic circular dichroism (ECD) experiments and genetic correlations as well. Compounds 15 and 16 were reported for the first time for the gorgonian. In the preliminary in vitro bioassays, compound 5 showed potential growth inhibitory activity against MG63 cells.
A rapid analytical method has been developed for the determination of polybrominated diphenyl ethers (PBDEs) in vegetables. PBDEs were determined by gas chromatography with negative chemical ionization mass spectrometric detection in the selected ion monitoring mode (GC-NCI-MS-SIM). The method detection limits (MDLs) were evaluated as 5 times the signal/noise (S/N) ratio in the GC/MS peaks by analyzing spiked vegetable samples at 2 - 50 ng/g. The minimum limits of instrument detection for this method were 0.28 - 0.78 pg for tri- to hepta-BDEs and 3.60 pg for deca-BDEs respectively. The minimum limit of method detection for tri to hepta-BDEs was 28 pg/g dry weight and 360 pg/g dry weight for deca-BDEs. In the examined vegetable samples, BDE-209 was the prominent congener detected in most cases, followed by BDE-47, BDE-71. The total concentration of PBDEs was in the range of 53.38 - 2884.02ng/g dry weight.
Three new 19-hydroxy steroidal glycosides, namely, junceellosides E-G (2-4), were isolated together with the known analogue junceelloside C (1) from the South China Sea gorgonian Dichotella gemmacea. The structures of these compounds were elucidated by a combination of detailed spectroscopic analyses, chemical methods, and comparison with reported data. These glycosides are found to have sugar moieties of both β-l- and β-d-arabinopyranoses by HPLC analysis of their thiocarbamoyl-thiazolidine derivatives and those of authentic d- and l-arabinoses, leading to the structure revision of junceelloside C (1). This is the first report of steroidal glycosides from the gorgonian D. gemmacea and the first report of glycosides with β-l-arabinopyranose from marine sources.
Eighteen new 11,20-epoxy-3Z,5E-dien briaranes, gemmacolides AA–AR (1–18), were isolated together with three known analogs, dichotellides F (19) and I (20), and juncenolide C (21), from the South China Sea gorgonian Dichotella gemmacea. The structures of the compounds were elucidated by detailed spectroscopic analysis and comparison with reported data. The absolute configuration was determined based on the ECD experiment. In the in vitro bioassay, compounds 1–3, 5, 6, 8–12, and 14–19 exhibited different levels of growth inhibition activity against A549 and MG63 cell lines. Preliminary structure-activity analysis suggests that 12-O-isovalerate may increase the activity whereas 13- or 14-O-isovalerate may decrease the activity. Contribution of substitutions at C-2 and C-16 remains uncertain.
ADVERTISEMENT RETURN TO ISSUEPREVAddition/CorrectionORIGINAL ARTICLEThis notice is a correctionCorrection to Bioactive 11,20-Epoxy-3,5(16)-diene Briarane Diterpenoids from the South China Sea Gorgonian Dichotella gemmaceaCui Li, Ming-Ping La, Ling Li, Xiu-Bao Li, Hua Tang, Bao-Shu Liu, Karsten Krohn, Peng Sun, Yang-Hua Yi*, and Wen Zhang*Cite this: J. Nat. Prod. 2012, 75, 11, 2047Publication Date (Web):October 30, 2012Publication History Published online30 October 2012Published inissue 26 November 2012https://pubs.acs.org/doi/10.1021/np300735hhttps://doi.org/10.1021/np300735hcorrectionACS PublicationsCopyright © 2012 The American Chemical Society and American Society of Pharmacognosy. This publication is available under these Terms of Use. Request reuse permissions This publication is free to access through this site. Learn MoreArticle Views575Altmetric-Citations3LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail PDF (111 KB) Get e-Alertsclose Get e-Alerts
Two new alkene sulfates, (5 Z )‐dec‐5‐en‐1‐yl sulfate ( 4 ) and (3 E )‐dec‐3‐en‐1‐yl sulfate ( 5 ), together with three known sulfated alkanes, 2,6‐dimethylheptyl sulfate ( 1 ), octyl sulfate ( 2 ), and decyl sulfate ( 3 ), were isolated from the sea cucumber Apostichopus japonicus. The structures of the new compounds 4 and 5 were elucidated by spectroscopic analysis, including 1 H‐, 13 C‐, and 2D‐NMR, ESI‐MS, and HR‐ESI‐MS. Compounds 2 and 3 were isolated from natural sources for the first time. In preliminary bioassays in vitro , compounds 4 and 5 showed antibacterial, antifungal, and cytotoxic activities.
Six new briarane diterpenoids, gemmacolides T-Y (1-6), were isolated together with three known analogs, juncenolide J (7), praelolide (8), and junceellolide C (9), from the South China Sea gorgonian Dichotella gemmacea. The structures of the new compounds were elucidated by detailed spectroscopic analysis and comparison with reported data. The absolute configuration was suggested based on biosynthetic considerations. In an in vitro bioassay, compounds 3 and 6 showed potent growth inhibition towards tumor cell lines of A549 and MG63, being stronger than the positive control of adriamycin. These compounds also exhibited weak antimicrobial activity against the bacterium Escherichia coli and the fungi Microbotryum violaceum and Septoria tritici.
Six new (3Z,5E)-11,20-epoxybriara-3,5-dien-7,18-olide diterpenoids, gemmacolides N–S (1–6), were isolated together with four known analogues, juncenolide D, and juncins R, S and U (7–10), from the South China Sea gorgonian Dichotella gemmacea. The structures of the new compounds were elucidated by the detailed analysis of spectroscopic data in combination with the comparison with reported data. The absolute configuration of 1 was determined by a TDDFT calculation of its solution ECD spectrum, affording the determination of absolute configuration of other analogues by simply comparing their ECD spectra with that of 1. The cytotoxic and antimicrobial activities of these compounds were evaluated. In preliminary in vitro bioassays, compounds 4, 5, 6, 8 and 9 showed cytotoxicity against A549 and MG63, while compounds 1, 2, 4, 7–10 showed antimicrobial activity against the fungus Septoria tritici and the bacterium Escherichia coli.
Seven new briarane diterpenoids, gemmacolides G-M (1-7), were isolated together with two known analogues, juncin O and junceellolide C, from the South China Sea gorgonian Dichotella gemmacea. The structures of the new compounds were elucidated by detailed analysis of spectroscopic data and comparison with reported data. In an in vitro bioassay, these compounds exhibited different levels of growth inhibition activity against A549 and MG63 cells. In particular, compound 4 was more active than the positive control adriamycin against A549 cells. Compounds 4 and 7 also exhibited weak antimicrobial activity against the bacterium Bacillus megaterium and the fungus Septoria tritici, respectively.