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1.
Molecules ; 29(6)2024 Mar 13.
Article in English | MEDLINE | ID: mdl-38542902

ABSTRACT

The extraction of rare earth elements (REEs) from phosphogypsum (PG) is of great significance for the effective utilization of rare earth resources and enhancing the resource value of PG waste residues. This study used Aspergillus niger (A. niger) fungal culture filtrate as a leaching agent to investigate the behavior of extracting REEs from PG through direct and indirect contact methods. According to the ICP-MS results, direct leaching at a temperature of 30 °C, shaking speed of 150 rpm, and a solid-liquid ratio of 2:1, achieved an extraction rate of 74% for REEs, with the main elements being yttrium (Y), lanthanum (La), cerium (Ce), and neodymium (Nd). Under the same conditions, the extraction rate of REEs from phosphogypsum using an A. niger culture filtrate was 63.3% higher than that using the simulated organic acid-mixed solution prepared with the main organic acid components in the A. niger leachate. Moreover, the morphological changes observed in A. niger before and after leaching further suggest the direct involvement of A. niger's metabolic process in the extraction of REEs. When compared to using organic acids, A. niger culture filtrate exhibits higher leaching efficiency for extracting REEs from PG. Additionally, using A. niger culture filtrate is a more environmentally friendly method with the potential for industrial-scale applications than using inorganic acids for the leaching of REEs from PG.


Subject(s)
Aspergillus niger , Metals, Rare Earth , Phosphorus , Lanthanum , Calcium Sulfate
2.
Molecules ; 27(17)2022 Sep 04.
Article in English | MEDLINE | ID: mdl-36080469

ABSTRACT

The enzyme tyrosinase plays a key role in the early stages of melanin biosynthesis. This study evaluated the inhibitory activity of anthocyanidin (1) and anthocyanins (2-6) on the catalytic reaction. Of the six derivatives examined, 1-3 showed inhibitory activity with IC50 values of 3.7 ± 0.1, 10.3 ± 1.0, and 41.3 ± 3.2 µM, respectively. Based on enzyme kinetics, 1-3 were confirmed to be competitive inhibitors with Ki values of 2.8, 9.0, and 51.9 µM, respectively. Molecular docking analysis revealed the formation of a binary encounter complex between 1-3 and the tyrosinase catalytic site. Luteolinidin (1) and petunidin 3-O-glucoside (2) may serve as tyrosinase inhibitors to block melanin production.


Subject(s)
Agaricales , Monophenol Monooxygenase , Anthocyanins/pharmacology , Enzyme Inhibitors/pharmacology , Glucosides/pharmacology , Kinetics , Melanins , Molecular Docking Simulation , Molecular Structure
3.
Chem Biodivers ; 19(10): e202200751, 2022 Oct.
Article in English | MEDLINE | ID: mdl-36082622

ABSTRACT

Chemical studies on the culture broth of the endophytic fungus Alternaria sp. J030 led to the identification of three benzylated hydroxyacetophenone derivatives, bauvaroalterins A-C (1-3), and 34 structurally diverse metabolites (4-37). The new structures were elucidated by extensive spectroscopic analyses including UV, IR, 1D and 2D NMR, HR-ESI-MS, and further confirmed using single crystal X-ray diffraction. The in vitro anti-neuroinflammatory effects of the co-isolated metabolites were evaluated in lipopolysaccharide (LPS)-stimulated microglial cells. Compounds 1-3 were shown to significantly reduce LPS-induced NO production by inhibiting the expression of iNOS, as well as inhibiting LPS-induced production of the inflammatory factors TNF-α, IL-1ß and IL-6. Further studies revealed that 1-3 were capable of down-regulating the expression of NF-κB subunits p50 and p65, thereby suppressing the activation of NF-κB by inhibiting the LPS-induced phosphorylation of IκB-α. Together these findings demonstrate that bauvaroalterins A-C (1-3) exert anti-neuroinflammatory effects via inhibition of the NF-κB/iNOS signalling pathway in LPS induced BV-2 cells.


Subject(s)
Lipopolysaccharides , NF-kappa B , Lipopolysaccharides/pharmacology , NF-KappaB Inhibitor alpha/metabolism , NF-kappa B/metabolism , Tumor Necrosis Factor-alpha/metabolism , Alternaria/metabolism , Anti-Inflammatory Agents , Interleukin-6/metabolism , Microglia
4.
Front Pharmacol ; 13: 905708, 2022.
Article in English | MEDLINE | ID: mdl-35899116

ABSTRACT

Current studies have found that butyrylcholinesterase (BuChE) replaces the biological function of acetylcholinesterase (AChE) in the late stage of Alzheimer's disease. Species in the genus of Fallopia, rich in polyphenols with diverse chemical structures and significant biological activities, are considered as an important resource for screening natural products to against AD. In this study, thirty-four compounds (1-34) were isolated from Fallopia dentatoalata (Fr. Schm.) Holub, and their inhibitory effects against AChE and BuChE were assessed. Compounds of the phenylpropanoid sucrose ester class emerged as the most promising members of the group, with 31-33 displaying moderate AChE inhibition (IC50 values ranging from 30.6 ± 4.7 to 56.0 ± 2.4 µM) and 30-34 showing potential inhibitory effects against BuChE (IC50 values ranging from 2.7 ± 1.7 to 17.1 ± 3.4 µM). Tacrine was used as a positive control (IC50: 126.7 ± 1.1 in AChE and 5.5 ± 1.7 nM in BuChE). Kinetic analysis highlighted compounds 31 and 32 as non-competitive inhibitors of AChE with Ki values of ∼30.0 and ∼34.4 µM, whilst 30-34 were revealed to competitively inhibit BuChE with Ki values ranging from ∼1.8 to ∼17.5 µM. Molecular binding studies demonstrated that 30-34 bound to the catalytic sites of BuChE with negative binding energies. The strong agreement between both in vitro and in silico studies highlights the phenylpropanoid sucrose esters 30-34 as promising candidates for use in future anti-cholinesterase therapeutics against Alzheimer's disease.

5.
J Vet Sci ; 23(4): e47, 2022 Jul.
Article in English | MEDLINE | ID: mdl-35698806

ABSTRACT

BACKGROUND: In lipopolysaccharide-induced RAW264.7 cells, Aster tataricus (AT) inhibits the nuclear factor kappa-light-chain-enhancer of activated B cells and MAPKs pathways and critical pathways of osteoclast development and bone resorption. OBJECTIVES: This study examined how aster saponin A2 (AS-A2) isolated from AT affects the processes and function of osteoclastogenesis induced by receptor activator of nuclear factor kappa-B ligand (RANKL) in RAW264.7 cells and bone marrow macrophages (BMMs). METHODS: The cell viability, tartrate-resistant acid phosphatase staining, pit formation assay, polymerase chain reaction, and western blot were carried out to determine the effects of AS-A2 on osteoclastogenesis. RESULTS: In RAW264.7 and BMMs, AS-A2 decreased RANKL-initiated osteoclast differentiation in a concentration-dependent manner. In AS-A2-treated cells, the phosphorylation of ERK1/2, JNK, and p38 protein expression were reduced considerably compared to the control cells. In RAW264.7 cells, AS-A2 suppressed the RANKL-induced activation of osteoclast-related genes. During osteoclast differentiation, AS-A2 suppressed the transcriptional and translational expression of NFATc1 and c-Fos. AS-A2 inhibited osteoclast development, reducing the size of the bone resorption pit area. CONCLUSION: AS-A2 isolated from AT appears to be a viable therapeutic therapy for osteolytic illnesses, such as osteoporosis, Paget's disease, and osteogenesis imperfecta.


Subject(s)
Bone Resorption , Saponins , Animals , Bone Marrow Cells/metabolism , Bone Resorption/genetics , Bone Resorption/metabolism , Bone Resorption/veterinary , Cell Differentiation , Mitogen-Activated Protein Kinases/metabolism , Mitogen-Activated Protein Kinases/pharmacology , Mitogens/metabolism , Mitogens/pharmacology , NF-kappa B/metabolism , NFATC Transcription Factors/genetics , NFATC Transcription Factors/metabolism , NFATC Transcription Factors/pharmacology , Osteoclasts/metabolism , Osteogenesis/physiology , RANK Ligand/metabolism , RANK Ligand/pharmacology , Saponins/pharmacology , Signal Transduction
6.
Beilstein J Org Chem ; 18: 200-207, 2022.
Article in English | MEDLINE | ID: mdl-35280953

ABSTRACT

Wikstroemia nutans Champ. ex Benth., a traditional herbal medicine collected at the Lingnan region of China, was chemically investigated. A new biscoumarin glucoside, wikstronutin (1), along with three known bis- and tricoumarin glucosides (2-4), two flavonoid glycosides (5-6), and eleven lignan glucosides (7-17) were isolated from the stems and roots of W. nutans. The new structure including its absolute configuration was elucidated based on a combination of 1D and 2D NMR, UV, IR, HRESIMS spectroscopic data, as well as chemical transformation. Compounds 1-17 were first isolated from the plant species W. nutans, while compounds 1-3, 8, and 11 were reported from the genus Wikstroemia for the first time. All co-isolates were evaluated for their in vitro inhibitory effects on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in murine RAW264.7 macrophage cells. The antibacterial activity of the selected compounds was also tested. Our work enriches the structure diversity of the secondary metabolites from the genus Wikstroemia.

7.
Clin Exp Pharmacol Physiol ; 49(3): 341-349, 2022 03.
Article in English | MEDLINE | ID: mdl-34729812

ABSTRACT

An imbalance of osteoclasts and osteoblasts can result in a variety of bone-related diseases, including osteoporosis. Thus, decreasing the activity of osteoclastic bone resorption is the main therapeutic method for treating osteoporosis. 2E-Decene-4, 6-diyn-1-ol-acetate (DDA) is a natural bioactive compound with anti-inflammatory and anti-cancer properties. However, its effects on osteoclastogenesis are unknown. Murine bone marrow-derived macrophages (BMMs) or RAW264.7 cells were treated with DDA, followed by evaluation of cell viability, RANKL-induced osteoclast differentiation, and pit formation assay. Effects of DDA on RANKL-induced phosphorylation of MAPKs were assayed by western blot analysis. Expression of osteoclast-specific genes was examined with reverse transcription-PCR (RT-PCR) and western blot analysis. In this study, DDA significantly inhibited RANKL-induced osteoclast differentiation in RAW264.7 cells as well as in BMMs without cytotoxicity. DDA also strongly blocked the resorbing capacity of BMM on calcium phosphate-coated plates. DDA inhibited RANKL-induced phosphorylation of ERK, JNK and p38 MAPKs, as well as expression of c-Fos and NFATc1, which are essential transcription factors for osteoclastogenesis. In addition, DDA decreased expression levels of osteoclastogenesis-specific genes, including matrix metalloproteinase-9 (MMP-9), tartrate-resistant acid phosphatase (TRAP), and receptor activator of NF-κB (RANK) in RANKL-induced RAW264.7 cells. Collectively, these findings indicated that DDA attenuates RANKL-induced osteoclast formation by suppressing the MAPKs-c-Fos-NFATc1 signalling pathway and osteoclast-specific genes. These results indicate that DDA may be a potential candidate for bone diseases associated with abnormal osteoclast formation and function.


Subject(s)
Biological Products/pharmacology , Extracellular Signal-Regulated MAP Kinases/metabolism , Genes, fos/physiology , Macrophages/drug effects , NFATC Transcription Factors/metabolism , Osteogenesis/drug effects , Animals , Aster Plant/chemistry , Biological Products/chemistry , Cell Differentiation/drug effects , Extracellular Signal-Regulated MAP Kinases/drug effects , Gene Expression Regulation/drug effects , Genes, fos/genetics , Mice , NFATC Transcription Factors/genetics , Osteoclasts , RANK Ligand/genetics , RANK Ligand/metabolism , RAW 264.7 Cells
8.
Molecules ; 28(1)2022 Dec 20.
Article in English | MEDLINE | ID: mdl-36615201

ABSTRACT

A series of benzyl, phenyl guanidine, and aminoguandine hydrazone derivatives was designed and in vitro antibacterial activities against two different bacterial strains (Staphylococcus aureus and Escherichia coli) were determined. Several compounds showed potent inhibitory activity against the bacterial strains evaluated, with minimal inhibitory concentration (MIC) values in the low µg/mL range. Of all guanidine derivatives, 3-[2-chloro-3-(trifluoromethyl)]-benzyloxy derivative 9m showed the best potency with MICs of 0.5 µg/mL (S. aureus) and 1 µg/mL (E. coli), respectively. Several aminoguanidine hydrazone derivatives also showed good overall activity. Compounds 10a, 10j, and 10r-s displayed MICs of 4 µg/mL against both S. aureus and E. coli. In the aminoguanidine hydrazone series, 3-(4-trifluoromethyl)-benzyloxy derivative 10d showed the best potency against S. aureus (MIC 1 µg/mL) but was far less active against E. coli (MIC 16 µg/mL). Compound 9m and the para-substituted derivative 9v also showed promising results against two strains of methicillin-resistant Staphylococcus aureus (MRSA). These results provide new and potent structural leads for further antibiotic optimisation strategies.


Subject(s)
Anti-Infective Agents , Methicillin-Resistant Staphylococcus aureus , Staphylococcus aureus , Escherichia coli , Guanidine/pharmacology , Hydrazones/pharmacology , Anti-Infective Agents/pharmacology , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Guanidines/pharmacology , Microbial Sensitivity Tests
9.
Front Chem ; 9: 780304, 2021.
Article in English | MEDLINE | ID: mdl-34900941

ABSTRACT

Mangrove-derived endophytes are rich in bioactive secondary metabolites with a variety of biological activities. Recently, a fungus Pseudofusicoccum sp. J003 was first isolated by our research group from mangrove species Sonneratia apetala Buch.-Ham. The subsequent chemical investigation of the methanol extract of the culture broth of this strain has led to the isolation of a new sesquiterpenoid named acorenone C (1), two alkaloids (2-3), four phenolic compounds (4-7), and four steroid derivatives (8-11). The new structure of 1 was established by extensive spectroscopic analysis, including 1D, 2D NMR spectroscopy, and HRESIMS. Its absolute configuration was elucidated by experimental ECD and ECD calculation. The in vitro AChE inhibitory, anti-inflammatory, and cytotoxic activities of the selected compounds were evaluated. The results showed that compound 1 showed mild AChE inhibitory activity, with an inhibition rate of 23.34% at the concentration of 50 µM. Compound 9 exerted a significant inhibitory effect against nitric oxide (NO) production in LPS-stimulated RAW 264.7 mouse macrophages, with an inhibition rate of 72.89% at the concentration of 25 µM, better than that of positive control L-NMMA. Compound 9 also displayed obvious inhibition effects on the growth of two human tumor cell lines, HL-60 and SW480 (inhibition rates 98.68 ± 0.97% and 60.40 ± 4.51%, respectively). The antimicrobial activities of the compounds (1-11) against Escherichia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa were also tested; however, none of them showed antimicrobial activities.

10.
Molecules ; 26(22)2021 Nov 18.
Article in English | MEDLINE | ID: mdl-34834049

ABSTRACT

Salvia przewalskii Maxim is a perennial plant from the genus Salvia (family Lamiaceae). The roots of S. przewalskii were long used as a traditional herb to treat blood circulation related illnesses in China. As part of our continuing interest in polycyclic natural products from medicinal plants, two unprecedented adducts comprised of a dinor-diterpenoid and a 9'-nor-rosmarinic acid derivative, linked by a 1,4-benzodioxane motif (1 and 2), were isolated from the roots of S. przewalskii. Their structures were established by extensive spectroscopic approaches including 1D, 2D NMR, and HRFABMS. Their cytotoxic activities against five human tumor cell lines were evaluated.


Subject(s)
Cinnamates/analysis , Depsides/analysis , Diterpenes/analysis , Salvia/chemistry , Antineoplastic Agents, Phytogenic/analysis , Antineoplastic Agents, Phytogenic/pharmacology , Cell Line, Tumor , Cinnamates/pharmacology , Depsides/pharmacology , Diterpenes/pharmacology , Humans , Neoplasms/drug therapy , Plant Roots/chemistry , Plants, Medicinal/chemistry , Rosmarinic Acid
11.
Materials (Basel) ; 14(19)2021 Sep 27.
Article in English | MEDLINE | ID: mdl-34639998

ABSTRACT

Biological matter evolution provides an idea for the human design and synthesis of new materials. However, biomimetic materials only stay in laboratory-scale models, and their large-scale industrial applications are yet to be realized. Here, inspired by nacre's architecture, we report a continuous, large-scale method to fabricate phosphogypsum composites by reactive extrusion strategy. After curing for seven days, with more than 50 wt% of beta-hemihydrate phosphogypsum (ß-HPG), the compressive strength and softening coefficient were 24.98 MPa and 0.78, increasing by 110.0% and 20.0%, respectively, compared to the pouring method. The results show that the screw extrusion process can improve the mechanical strength and waterproof properties of ß-HPG hydration specimens without any special chemical admixtures and cements.

12.
Micromachines (Basel) ; 12(3)2021 Mar 21.
Article in English | MEDLINE | ID: mdl-33800963

ABSTRACT

Compared with a traditional optical system, the single-lens curved compound eye imaging system has superior optical performance, such as a large field of view (FOV), small size, and high portability. However, defocus and low resolution hinder the further development of single-lens curved compound eye imaging systems. In this study, the design of a nonuniform curved compound eye with multiple focal lengths was used to solve the defocus problem. A two-step gas-assisted process, which was combined with photolithography, soft photolithography, and ultraviolet curing, was proposed for fabricating the ommatidia with a large numerical aperture precisely. Ommatidia with high resolution were fabricated and arranged in five rings. Based on the imaging experimental results, it was demonstrated that the high-resolution and small-volume single-lens curved compound eye imaging system has significant advantages in large-field imaging and rapid recognition.

13.
ACS Omega ; 5(44): 28793-28811, 2020 Nov 10.
Article in English | MEDLINE | ID: mdl-33195933

ABSTRACT

d-myo-Inositol 1,4,5-trisphosphate receptors (IP3Rs) are Ca2+ channels activated by the intracellular messenger inositol 1,4,5-trisphosphate (IP3, 1). The glyconucleotide adenophostin A (AdA, 2) is a potent agonist of IP3Rs. A recent synthesis of d-chiro-inositol adenophostin (InsAdA, 5) employed suitably protected chiral building blocks and replaced the d-glucose core by d-chiro-inositol. An alternative approach to fully chiral material is now reported using intrinsic sugar chirality to avoid early isomer resolution, involving the coupling of a protected and activated racemic myo-inositol derivative to a d-ribose derivative. Diastereoisomer separation was achieved after trans-isopropylidene group removal and the absolute ribose-inositol conjugate stereochemistry assigned with reference to the earlier synthesis. Optimization of stannylene-mediated regiospecific benzylation was explored using the model 1,2-O-isopropylidene-3,6-di-O-benzyl-myo-inositol and conditions successfully transferred to one conjugate diastereoisomer with 3:1 selectivity. However, only roughly 1:1 regiospecificity was achieved on the required diastereoisomer. The conjugate regioisomers of benzyl derivatives 39 and 40 were successfully separated and 39 was transformed subsequently to InsAdA after amination, pan-phosphorylation, and deprotection. InsAdA from this synthetic route bound with greater affinity than AdA to IP3R1 and was more potent in releasing Ca2+ from intracellular stores through IP3Rs. It is the most potent full agonist of IP3R1 known and .equipotent with material from the fully chiral synthetic route.

14.
J BUON ; 25(4): 2086-2091, 2020.
Article in English | MEDLINE | ID: mdl-33099957

ABSTRACT

PURPOSE: To explore the effects of micro ribonucleic acid 212 (miR-212) on proliferation and apoptosis of osteosarcoma cells via the Hedgehog signaling pathway. METHODS: hFOB1.19 cells were enrolled as normal group, and osteosarcoma MG63 cells were divided into osteosarcoma group and miR-212 mimics group. The cells in the normal and osteosarcoma group were cultured normally, while those in miR-212 mimics group were cultured in medium containing miR-212 mimics. After 24 h of culture, the cells were collected for detection. Quantitative polymerase chain reaction (qPCR) assay was performed to determine the expression level of miR-212. The Gli1 expression level was measured by immunohistochemistry and Western blotting. Additionally, cell proliferation and apoptosis were detected by cell counting kit-8 (CCK-8) assay and flow cytometry, respectively. RESULTS: Based on immunohistochemistry, the average optical density of Gli1 positive expression was evidently increased in osteosarcoma group and miR-212 mimics group compared with that in normal group. The results of Western blotting and qRT-PCR showed that compared with those in normal group, the relative protein expression level of Gli1 and relative expression level of miR-212 were notably raised in the other two groups, and these levels were remarkably higher in miR-212 mimics group than those in osteosarcoma group. According to CCK-8 assay, the proliferation rate of cells was overtly higher in osteosarcoma group and miR-212 mimics group than that in normal group, and also distinctly higher in miR-212 mimics group than that in osteosarcoma group. CONCLUSIONS: MiR-212 promotes the proliferation and inhibits the apoptosis of osteosarcoma cells by up-regulating the Hedgehog signaling pathway.


Subject(s)
Bone Neoplasms/metabolism , Hedgehog Proteins/metabolism , Immunohistochemistry/methods , MicroRNAs/metabolism , Osteosarcoma/metabolism , Apoptosis/physiology , Bone Neoplasms/genetics , Bone Neoplasms/pathology , Cell Proliferation/physiology , Humans , MicroRNAs/genetics , Osteosarcoma/genetics , Osteosarcoma/pathology , Signal Transduction , Transfection
15.
BMC Med Inform Decis Mak ; 20(Suppl 3): 125, 2020 07 09.
Article in English | MEDLINE | ID: mdl-32646426

ABSTRACT

BACKGROUND: To provide satisfying answers, medical QA system has to understand the intentions of the users' questions precisely. For medical intent classification, it requires high-quality datasets to train a deep-learning approach in a supervised way. Currently, there is no public dataset for Chinese medical intent classification, and the datasets of other fields are not applicable to the medical QA system. To solve this problem, we construct a Chinese medical intent dataset (CMID) using the questions from medical QA websites. On this basis, we compare four intent classification models on CMID using a case study. METHODS: The questions in CMID are obtained from several medical QA websites. The intent annotation standard is developed by the medical experts, which includes four types and 36 subtypes of users' intents. Besides the intent label, CMID also provides two types of additional information, including word segmentation and named entity. We use the crowdsourcing way to annotate the intent information for each Chinese medical question. Word segmentation and named entities are obtained using the Jieba and a well-trained Lattice-LSTM model. We loaded a Chinese medical dictionary consisting of 530,000 for word segmentation to obtain a more accurate result. We also select four popular deep learning-based models and compare their performances of intent classification on CMID. RESULTS: The final CMID contains 12,000 Chinese medical questions and is organized in JSON format. Each question is labeled the intention, word segmentation, and named entity information. The information about question length, number of entities, and are also detailed analyzed. Among Fast Text, TextCNN, TextRNN, and TextGCN, Fast Text and TextCNN models have achieved the best results in four types and 36 subtypes intent classification, respectively. CONCLUSIONS: In this work, we provide a dataset for Chinese medical intent classification, which can be used in medical QA and related fields. We performed an intent classification task on the CMID. In addition, we also did some analysis on the content of the dataset.


Subject(s)
Benchmarking , Intention , China , Humans
16.
Chem Sci ; 10(20): 5382-5390, 2019 May 02.
Article in English | MEDLINE | ID: mdl-31171961

ABSTRACT

Reactions that form sec-sec ethers are well known, but few lead to compounds with dense functionality around the O-linkage. Replacement of the α-glucopyranosyl unit of adenophostin A, a potent d-myo-inositol 1,4,5-trisphosphate (IP3R) agonist, with a d-chiro-inositol surrogate acting substantially as a pseudosugar, leads to "d-chiro-inositol adenophostin". At its core, this cyclitol-nucleoside trisphosphate comprises a nucleoside sugar linked via an axial d-chiro-inositol 1-hydroxyl-adenosine 3'-ribose ether linkage. A divergent synthesis of d-chiro-inositol adenophostin has been achieved. Key features of the synthetic strategy to produce a triol for phosphorylation include a new selective mono-tosylation of racemic 1,2:4,5-di-O-isopropylidene-myo-inositol using tosyl imidazole; subsequent conversion of the product into separable camphanate ester derivatives, one leading to a chiral myo-inositol triflate used as a synthetic building block and the other to l-5-O-methyl-myo-inositol [l-(+)-bornesitol] to assign the absolute configuration; the nucleophilic coupling of an alkoxide of a ribose pent-4-ene orthoester unit with a structurally rigid chiral myo-inositol triflate derivative, representing the first sec-sec ether formation between a cyclitol and ribose. Reaction of the coupled product with a silylated nucleobase completes the assembly of the core structure. Further protecting group manipulation, mixed O- and N-phosphorylation, and subsequent removal of all protecting groups in a single step achieves the final product, avoiding a separate N6 protection/deprotection strategy. d-chiro-Inositol adenophostin evoked Ca2+ release through IP3Rs at lower concentrations than adenophostin A, hitherto the most potent known agonist of IP3Rs.

17.
J Nat Prod ; 82(5): 1139-1148, 2019 05 24.
Article in English | MEDLINE | ID: mdl-30931559

ABSTRACT

Four new aster saponins (1-4) together with five known analogues (5-9) were isolated from Aster tataricus. The chemical structures of 1-4 were elucidated based on spectrometric and spectroscopic analysis and comparison with reported data. The potential anti-inflammatory activities of aster saponins 1-9 were evaluated subsequently by measuring lipopolysaccharide (LPS)-enhanced nitric oxide (NO) formation in murine macrophages. Among these, aster saponin B (6) exhibited the most potent inhibitory activity (IC50: 1.2 µM). Additionally, inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) protein levels were dose-dependently suppressed by 6 in LPS-activated RAW 264.7 cells. Investigation of the anti-inflammatory mechanism indicated that 6 attenuated the phosphorylation and degradation of the inhibitor of NF-κB (IκB), which led to the blocking of NF-κB p65 translocation to the nucleus.


Subject(s)
Anti-Inflammatory Agents/isolation & purification , Aster Plant/chemistry , MAP Kinase Signaling System/physiology , NF-kappa B/physiology , Saponins/isolation & purification , Animals , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/pharmacology , Lipopolysaccharides/pharmacology , Mice , Oleanolic Acid/analogs & derivatives , RAW 264.7 Cells , Saponins/chemistry , Saponins/pharmacology
18.
Data Brief ; 21: 727-735, 2018 Dec.
Article in English | MEDLINE | ID: mdl-30406163

ABSTRACT

In this article, the geochemical data of a ~900 Ma mafic sill from Xuzhou, North China are reported. These datasets include 37 whole-rock major and trace element data, and 21 major element data on plagioclase, 20 major element data on clinopyroxene crystals, 10 major element data on apatite crystals, 7 major element data of preserved coexisting titano-magnetite and ilmenite grains, 36 major element data on different types of ilmenite crystals, 13 major element and 11 trace element data on titanite. These data are associated with Su et al. "Petrogenesis of a ~900 Ma mafic sill from Xuzhou, North China: Implications for the genesis of Fe-Ti-rich rocks" (Su et al., 2018), and in which their characters and variations were interpreted and discussed.

19.
Molecules ; 23(2)2018 Feb 19.
Article in English | MEDLINE | ID: mdl-29463053

ABSTRACT

The aim of this work was to evaluate the main nutrients and their antioxidant properties of a Chinese wild edible fruit, Passiflora foetida, collected from the ecoregion of Hainan province, China. The analytical results revealed that P. foetida fruits were rich in amino acids (1097 mg/100 g in total), minerals (595.75 mg/100 g in total), and unsaturated fatty acids (74.18 g/100 g in total fat). The lyophilized powder of edible portion contained the higher polyphenols content than the inedible portion powder. The UPLC-Q-TOF-MSE analysis of the extractable and non-extractable phenolics indicated the presence of 65 compounds including 39 free phenolics, 14 insoluble-glycoside-phenolics, and 22 insoluble-ester-phenolics. In addition, the non-extractable phenolics obtained by alkali hydrolysis showed significant antioxidant activities by/through DPPH and ABTS radical scavenging. These findings of P. foetida fruits, for the first time, suggest that these polyphenol-rich fruits may have potential nutraceutical efficacies.


Subject(s)
Antioxidants/chemistry , Passiflora/chemistry , Plant Extracts/chemistry , Polyphenols/chemistry , China , Flavonoids/chemistry , Fruit/chemistry , Nutrition Assessment , Phenols/chemistry
20.
Mar Drugs ; 12(12): 5817-38, 2014 Dec 02.
Article in English | MEDLINE | ID: mdl-25474189

ABSTRACT

Nucleosides are glycosylamines that structurally form part of nucleotide molecules, the building block of DNA and RNA. Both nucleosides and nucleotides are vital components of all living cells and involved in several key biological processes. Some of these nucleosides have been obtained from a variety of marine resources. Because of the biological importance of these compounds, this review covers 68 marine originated nucleosides and their synthetic analogs published up to June 2014. The review will focus on the structures, bioactivities, synthesis and biosynthetic processes of these compounds.


Subject(s)
Biological Factors/biosynthesis , Biological Factors/chemistry , Nucleosides/biosynthesis , Nucleosides/chemistry , Animals , Humans , Marine Biology/methods , Nucleotides/biosynthesis , Nucleotides/chemistry
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