Pitsubcosides A-L, highly esterified eudesmane sesquiterpenoid glycosides with antibacterial activity from Pittosporum subulisepalum and their mechanism.

BACKGROUND: Plants from the genus Pittosporum are traditionally used as antibacterial, antifungal and antiviral agents. A bioassay evaluation of the extract of Pittosporum subulisepalum revealed antibacterial activity. This study focused on the discovery of the antibacterial metabolism in P. subulisepalum, as well as the modes of action of its active components. RESULTS: A chemical investigation of an ethyl acetate (EtOAc) extract of the aerial parts of P. subulisepalum led to the isolation of 12 previously undescribed eudesmane sesquiterpenoid glycoside esters (ESGEs), pitsubcosides A-L (1-12). Their structures were elucidated by extensive spectroscopic analysis, including one- and two-dimensional NMR, high-resolution electrospray ionization mass spectrometry, electronic circular dichroism spectra and single-crystal X-ray crystallography analysis or by comparing with authentic samples. The new ESGEs were characterized by their highly esterified glycoside moieties. Among them, compounds 1-3, 5 and 8 showed a moderate inhibitory effect against Staphylococcus aureus, methicillin-resistant S. aureus (MRSA), Bacillus cereus, Bacillus subtilis, Pseudomonas syringae pv. actinidiae (Psa) and Erwinia carotovora with minimum inhibitory concentrations (MICs) ranging from 3.13 to 100 µm. Among them, compounds 3 and 5 showed remarkable antibacterial activity against S. aureus and Psa with MIC values of 6.25 and 3.13 µm, respectively. Live bacterial mass and the biofilms of S. aureus and Psa were quantified using methyl tetrazolium and crystal violet assays. Fluorescence microscopy and scanning electron microscopy experiments revealed an antibacterial mechanism of cell membrane architectural disruption. CONCLUSION: The results suggest that ESGEs possess great potential for the development of antibacterial agents to control plant pathogens. © 2023 Society of Chemical Industry.

Astragalus polysaccharide ameliorated complex factor-induced chronic fatigue syndrome by modulating the gut microbiota and metabolites in mice.

Chronic fatigue syndrome (CFS) is a debilitating disease with no symptomatic treatment. Astragalus polysaccharide (APS), a component derived from the traditional Chinese medicine A. membranaceus, has significant anti-fatigue activity. However, the mechanisms underlying the potential beneficial effects of APS on CFS remain poorly understood. A CFS model of 6-week-old C57BL/6 male mice was established using the multiple-factor method. These mice underwent examinations for behavior, oxidative stress and inflammatory indicators in brain and intestinal tissues, and ileum histomorphology. 16 S rDNA sequencing analysis indicated that APS regulated the abundance of gut microbiota and increased production of short chain fatty acids (SCFAs) and anti-inflammatory bacteria. In addition, APS reversed the abnormal expression of Nrf2, NF-κB, and their downstream factors in the brain-gut axis and alleviated the reduction in SCFAs in the cecal content caused by CFS. Further, APS modulated the changes in serum metabolic pathways induced by CFS. Finally, it was verified that butyrate exerted antioxidant and anti-inflammatory effects in neuronal cells. In conclusion, APS could increase the SCFAs content by regulating the gut microbiota, and SCFAs (especially butyrate) can further regulate the oxidative stress and inflammation in the brain, thus alleviating CFS. This study explored the efficacy and mechanism of APS for CFS from the perspective of gut-brain axis and provides a reference to further explore the efficacy of APS and the role of SCFAs in the central nervous system.

Further sesquiterpenoids from Pittosporum qinlingense and their anti-inflammatory activity.

Four new sesquiterpenoid glycoside esters, Pitqinlingoside N-Q (1-4), together with eleven known metabolites (5-15), were isolated from 95% EtOH extract of the twigs, fruits and leaves of P. qinlingense. The structures of new compounds were elucidated on the basis of extensive spectroscopic analyses, including IR, UV, HRMS, NMR and electronic circular dichroism spectra. Unusal glycoside esters are characterized by the presence of polyacylated ß-D-fucopyranosyl and ß-d-glucopyranosyl units. Pitqinlingoside N (1), O (2), P (3), boscialin (5) and arvoside C (6) showed significant nitric oxide production inhibition in lipopolysaccharide (LPS)-induced BV-2 microglial cells with IC50 values ranging from 1.58 to 28.74 µM. Structure-activity relationships of the isolated compounds are discussed.

Lutein encapsulated in whey protein and citric acid potato starch ester: Construction and characterization of microcapsules.

The poor water solubility and stability of lutein limit its application in industry. Microencapsulation technology is an excellent strategy to solve these problems. This study used citric acid esterified potato starch and whey protein as an emulsifier to prepare oil-in-water lutein emulsion, and microcapsules were constructed by spray drying technology. The effects of different component proportions on microcapsules' microstructure, physical and chemical properties, and storage stability were analyzed. Citrate esterified potato starch had good emulsifying properties, and when compounded with whey protein, the encapsulation efficiency (EE) of microcapsules increased, and the embedding effect of lutein improved. After microencapsulation, the solubility of lutein increased significantly, reaching over 49.71 %, and gradually raised with more whey protein content. Furthermore, the high proportion of whey protein helped improve microcapsules' EE and thermal properties, with the maximum EE reaching 89.36 %. The glass transition temperatures of microcapsules were all higher than room temperature, which indicated that they keep a stable state under general storage conditions. The experimental results of this study may provide a reference for applying lutein in food and other fields.

[Metabonomics and its application in Chinese medicine processing].

Chinese medicine processing is a procedure to process medicinal materials under the guidance of traditional Chinese medicine(TCM) theories by using unique methods in China. The medicinal materials can only be used clinically after proper processing. With the development of the modernization of TCM, it is difficult to solve the problems in the inheritance, development, and internationalization of Chinese medicine processing. Metabonomics, a new omics technology developed at the end of the last century, is used to infer the physiological or pathological conditions of the organism with the methods such as NMR and LC-MS via investigating the changes in endogenous small molecule metabolic network after the organism is stimulated by external environment. Metabonomics coincides with the holistic view of TCM because it displays the characteristics of integrity, comprehensiveness, and dynamics, and it has been widely applied in the field of Chinese medicine processing in recent years. This study summarized the application of metabonomics in the processing mechanism and quality control of Chinese medicine processing and prospected the development of this technology in the field of Chinese medicine processing.

The effect of neurolinguistic programming on academic achievement, emotional intelligence, and critical thinking of EFL learners.

Neurolinguistic programming (NLP) is a method of personal communication. This study aimed to determine the effect of NLP strategies on academic achievement, emotional intelligence, and critical thinking. Although NLP has been studied, more studies still need to be conducted on this variable contributing to language learning success. This experimental study was conducted with a pretest-posttest design with the control group in 2021. Sampling was conducted through the multistage cluster random sampling (MCRS) method, and based on the Cambridge placement test (2010), 50 students proved to be at an advanced level and participated in this study. To test the hypotheses, an ANCOVA test was employed. Participants were randomly divided into two control (25 people) and experimental groups (25 people). They were performed on the experimental group during 12 sessions of 90 min of the strategic training in NLP. In the experimental group, the mean and std of critical thinking was 16.24 ± 2.59 in the pretest, which increased to 18.88 ± 2.77 in the posttest; the mean and std of academic achievement was 155.02 ± 15.90 in the pretest, which rose to 171.70 ± 10.83 in the posttest and the mean and std of emotional intelligence was 96.51 ± 12.44 in the pretest, which increased to 118.28 ± 6.18 in the posttest. The results of data analysis by covariance method showed that NLP was practical on learners' academic achievement, emotional intelligence, and critical thinking. Justifications and implications for the study's findings and suggestions for further research are presented.

One water-soluble polysaccharide from Ginkgo biloba leaves with antidepressant activities via modulation of the gut microbiome.

Depression, a mental illness characterized by persistent feeling of sadness and loss of interest, has been a serious health problem worldwide. Manipulation of the microbiota by probiotics and prebiotics represents a novel emerging strategy for the treatment of various psychiatric disorders such as major depressive disorders. Here, we show that one water-soluble polysaccharide from Ginkgo biloba leaves (GPS) reduced stress-induced depression and reversed gut dysbiosis. Similar to the antidepressant paroxetine, GPS significantly reduced the immobility times in the tail suspension test (TST) and forced swimming test (FST) and anxiety-like behavior in the open field test (OFT). Consistent with the improvement of depression-like behavior above, GPS mice had elevated serotonin and dopamine levels in multiple brain regions including the hippocampus, cerebral cortex and olfactory bulb, relative to unpredictable chronic mild stress (UCMS) treatment mice. GPS treatment could alleviate the stress-induced reduction in the density of serotonin-positive and dopamine-positive cells. Fecal microbiome transplant (FMT) combined with antibiotic treatment showed that the anti-depressant activity of GPS had a causal relationship with intestinal microbes. By performing a pyrosequencing-based analysis of bacterial 16S rRNA (V3 + V4 region) in fecal of the mice, the results showed that GPS reversed depression-associated gut dysbiosis and increased the richness of Lactobacillus species which has been proven to be a path to relieve depression. Our results demonstrated that the polysaccharide from Ginkgo biloba leaves might be a promising pharmacotherapeutic candidate for treating depression.

PTH (1-34) affects bone turnover governed by osteocytes exposed to fluoride.

Exposure to fluoride from environmental sources remains an overlooked, but serious public health risk. In this study, we looked into the role osteocytes play on the mechanism underlying fluoride induced osteopathology. We analyzed bone formation and resorption related genes generated by osteocytes that were exposed to varied doses of fluoride with and without PTH in vitro. Correspondingly, osteogenesis and osteoclastogenesis related genes were also investigated in rats exposed to fluoride for 8 weeks, and the PTH(1-34)was applied at the last 3 weeks to observe its role in regulating bone turnover upon fluoride treatment. The data in vitro indicated that fluoride treatment inhibited Sost expression of mRNA and protein and stimulated RANKL mRNA protein expression as well as the RANKL/OPG ratio in the primary osteocytes. Single PTH treatment played the similar role on expression of these genes and proteins. The PTH combined administration enhanced the action of fluoride treatment on RNAKL/OPG and SOST/Sclerostin. The up-regulation of RANKL and decreasing of Sost induced by fluoride and/or PTH treatment was validated in vivo and suggests that osteocytes are a major source of RANKL and Sost, both of which play essential roles in fluoride affecting osteogenesis and osteoclastogenesis. Expression of Wnt/ß-catenin was up-regulated in both in vitro osteocytes treated with high dose of fluoride and bone tissue of rats in the presence of fluoride and PTH. In vivo, fluoride and single PTH stimulated bone turnover respectively, furthermore, PTH combined with low dose of fluoride treatment reinforced the osteogenesis and osteoclastogenesis genes expression, however, co-treatment of PTH reversed the effect of high dose of fluoride on osteogenesis and osteoclastogenensis related factors. In conclusion, this study demonstrated that osteocytes play a key role in fluoride activated bone turnover, and PTH participates in the process of fluoride modulating SOST/Sclerostin and RANKL expression.

Antiphytoviral toxins of Actinidia chinensis root bark (ACRB) extract: laboratory and semi-field trials.

BACKGROUND: Actinidia chinensis Planch, which is distributed only in China, has been used to treat hepatitis and cancer. The objective of the present work was to identify the antiviral active ingredient of A. chinensis root bark (ACRB). RESULTS: Bioassay-guided isolation of the most active fraction, the EtOAc extract, led to the identification of seven compounds, (+)-catechins-7-phytol (1), 5-methoxy-coumarin-7-ß-D-glycosidase (2), (+)-catechins (3), fupenzic acid (4), spathodic acid-28-O-ß-D-glucopyranoside (5), 3-oxo-9, 12-diene-30-oic acid (6), and 3-ß-(2-carboxy benzoyloxy) oleanolic acid (7). Of these, 5-methoxy-coumarin-7-ß-D-glycosidase (2) possessed the highest antiviral activity, followed by spathodic acid-28-O-ß-D-glucopyranoside (5). Thus, compounds 2 and 5 were the main active constituents, with potential for further development as biological antiviral agents. CONCLUSION: The results suggest that ACRB possesses great potential value for development of an antiviral agent to control phytoviral diseases. © 2018 Society of Chemical Industry.

Insecticidal Constituents from Buddlej aalbiflora Hemsl.

Eleven known compounds, deoxymikanolide (1), 1,3-dihydroxyxanthone (2), kumatakenin (3), apigenin (4), chrysin (5), kaempferol (6), Iso-kaempferol (7), luteolin (8), luteolin-3',4'-dimethylether-7-O-ß-glucoside (9), luteolin-7-O-ß-glucoside (10) and quercetin (11) were identified in MeOH extract of Buddleja albiflora Hemsl (Oleaceae). These compounds (each, 1, 0.5 and 0.25 mg mL-1) were tested for insecticidal activity against 3rd and 4th-instar larvae of Plutella xylostella, 3rd-instar larvae of Mythimna separata and 3rd-instar larvae of Macrosiphoniella sanborni. The lowest 50% anti-feedant concentration (AFC50) against P. xylostella and 50% lethal concentration (LC50) against P. xylostella and M. sanborni were observed as 0.0058, 0.0046 and 3.4048 mg L-1, respectively.

α-Glucosidase inhibitors and phytotoxins from Streptomyces xanthophaeus.

Twenty-four metabolites 1-24 were isolated from the fermentation broth of Streptomyces xanthophaeus. Their structures were elucidated on the basis of spectroscopic analysis and by comparison of their NMR data with literature data reported. Daidzein (1), genistein (2) and gliricidin (3) inhibited α-glucosidase in vitro with IC50 values of 174.2, 36.1 and 47.4 µM, respectively, more potent than the positive control, acarbose. Docking study revealed that the amino acid residue Thr 215 is the essential binding site for active ligands 2. In addition, the phytotoxic effects of all compounds were assayed on radish seedlings, five of which, 3, 8, 13, 15 and 18, inhibited the growth of radish (Raphanus sativus) seedlings with inhibitory rates of >60% at a concentration of 100 ppm, which was comparable or superior to the positive control glyphosate. This is the first report of the phytotoxicity of the compounds.

Mechanisms of Intracellular Calcium Homeostasis in MC3T3-E1 Cells and Bone Tissues of Sprague-Dawley Rats Exposed to Fluoride.

Calcium homeostasis of osteoblasts (OBs) has an important role in the physiology and pathology of bone tissue. In order to study the mechanisms of intracellular calcium homeostasis, MC3T3-E1 cells and Sprague-Dawley rats were treated with different concentrations of fluoride. Then, we examined intracellular-free calcium ion ([Ca(2+)]i) in MC3T3-E1 cells as well as mRNA and protein levels of Cav1.2, the main subunit of L-type voltage-dependent calcium channels (VDCCs), Na(+)/Ca(2+) exchange carriers (NCS), and plasma membrane Ca(2+)-ATPase (PMCA), inositol 1,4,5-trisphosphate receptor (IP3R) channels, sarco/endoplasmic reticulum calcium ATPase 2b (SERCA2b)/ATP2A2 in vitro, and rat bone tissues in vivo. Our results showed that [Ca(2+)]i of fluoride-treated OBs increased in a concentration-dependent manner with an increase in the concentration of fluoride. We also found that the low dose of fluoride led to high expression levels of Cav1.2, NCS-1, and PMCA and low expression levels of IP3R and SERCA2b/ATP2A2, while the high dose of fluoride induced an increase in SERCA2b/ATP2A2 levels and decrease in Cav1.2, PMCA, NCS-1, and IP3R levels. These results demonstrate that calcium channels and calcium pumps of plasma and endoplasmic reticulum (ER) membranes keep intracellular calcium homeostasis by regulating Cav1.2, NCS-1, PMCA, IP3R, and SERCA2b/ATP2A2 expression.

Fluoride Affects Calcium Homeostasis by Regulating Parathyroid Hormone, PTH-Related Peptide, and Calcium-Sensing Receptor Expression.

Parathyroid hormone (PTH), PTH-related peptide (PTHrP), and calcium-sensing receptor (CaSR) play important roles in maintaining calcium homeostasis. Here, we study the effect of fluoride on expression of PTH, PTHrP, and CaSR both in vitro and in vivo. MC3T3-E1 cells and Sprague-Dawley rats were treated with different concentrations of fluoride. Then, the free calcium ion concentration in cell culture supernatant and serum were measured by biochemical analyzer. The expression of PTH, PTHrP, and CaSR was analyzed by qRT-PCR and Western blot. We found that the low dose of fluoride increased ionized calcium (i[Ca(2+)]) and the high dose of fluoride decreased i[Ca(2+)] in cell culture supernatant. The low dose of fluoride inhibited the PTH and PTHrP expression in MC3T3-E1 cells. The high dose of fluoride improved the PTHrP expression in MC3T3-E1 cells. Interestingly, we found that NaF decreased serum i[Ca(2+)] in rats. Fluoride increased CaSR expression at both messenger RNA (mRNA) and protein levels in MC3T3-E1 cells and rats. The expression of PTHrP protein was inhibited by fluoride in rats fed regular diet and was increased by fluoride in rats fed low-calcium diet. Fluoride also increased the expression of PTH, NF-kappaB ligand (RANKL), and osteoprotegerin (OPG) in rats. The ratio of RANKL/OPG in rats fed low-calcium food in presence or absence of fluoride was significantly increased. These results indicated that fluoride might be able to affect calcium homeostasis by regulating PTH, PTHrP, and CaSR.

[Ameliorative effect of ginseng glycopeptide on cross-linking of rat tail tendon collagen].

OBJECTIVE: To investigate the ameliorative effect of ginseng glycopeptide on cross-linking of rat tail tendon collagen. METHOD: ELISA was used to determine the inhibitory effect of ginseng glycopeptide on cross-linking of rat tail tendon collagen in vitro. After ginseng glycopeptide was intraperitoneally administrated to streptozotocin-induced diabetic rats for 12 weeks, the acid solubility, limited pepsin degradation properties and solubility in SDS-2-mercaptoethanol of the rat tail tendon collagen were determined, and the effect of ginseng glycopeptide on the tail tendon collagen cross-linking was evaluated. RESULT: Ginseng glycopeptide inhibited significantly the cross-linking of rat tail tendon collagen in vitro. The solubility of the tail tendon collagen (in acid, pepsin and SDS-2-mercaptoethanol) was markedly decreased in diabetic rats and ginseng glycopeptide-treated diabetic rats had significantly an increase in the collagen solubility in the above-mentioned solutions, suggesting that ginseng glycopeptide decreased severity of the collagen cross-linking. CONCLUSION: Ginsengglycopeptide exhibits an significantly ameliorative effect on cross-linking of rat tail tendon collagen.

Two diterpenes and three diterpene glucosides from Phlogacanthus curviflorus.

Two new diterpene lactones, phlogacantholides B (1) and C (2), and three new diterpene lactone glucosides, phlogacanthosides A (3), B (4), and C (5), together with lupeol, beta-sitosterol, betulin, beta-daucosterol, (+)-syringaresinol, and (+)-syringaresinol-4-O-beta-D-glucopyranoside, were isolated from the roots of Phlogacanthus curviflorus. Their structures were elucidated by chemical and spectroscopic evidence. The structure, including the relative configuration of phlogacantholide B (1), was confirmed by X-ray crystallographic analysis of its diacetate (6).