Mechanism of n-butanol alcohol extract of Baitouweng Decoction in treatment of vulvovaginal candidiasis based on negative regulation of NLRP3 inflammasome via PKCδ/NLRC4/IL-1Ra axis / 中国中药杂志

This study aimed to explore the mechanism of n-butanol alcohol extract of Baitouweng Decoction(BAEB) in the treatment of vulvovaginal candidiasis(VVC) in mice based on the negative regulation of NLRP3 inflammasome via PKCδ/NLRC4/IL-1Ra axis. In the experiment, female C57BL/6 mice were divided randomly into the following six groups: a blank control group, a VVC model group, high-, medium-, and low-dose BAEB groups(80, 40, and 20 mg·kg~(-1)), and a fluconazole group(20 mg·kg~(-1)). The VVC model was induced in mice except for those in the blank control group by the estrogen dependence method. After modeling, no treatment was carried out in the blank control group. The mice in the high-, medium-, and low-dose BAEB groups were treated with BAEB at 80, 40, and 20 mg·kg~(-1), respectively, and those in the fluconazole group were treated with fluconazole at 20 mg·kg~(-1). The mice in the VVC model group received the same volume of normal saline. The general state and body weight of mice in each group were observed every day, and the morphological changes of Candida albicans in the vaginal lavage of mice were examined by Gram staining. The fungal load in the vaginal lavage of mice was detected by microdilution assay. After the mice were killed, the degree of neutrophil infiltration in the vaginal lavage was detected by Papanicolaou staining. The content of inflammatory cytokines interleukin(IL)-1β, IL-18, and lactate dehydrogenase(LDH) in the vaginal lavage was tested by enzyme-linked immunosorbent assay(ELISA), and vaginal histopathology was analyzed by hematoxylin-eosin(HE) staining. The expression and distribution of NLRP3, PKCδ, pNLRC4, and IL-1Ra in vaginal tissues were measured by immunohistochemistry(IHC), and the expression and distribution of pNLRC4 and IL-1Ra in vaginal tissues were detected by immunofluorescence(IF). The protein expression of NLRP3, PKCδ, pNLRC4, and IL-1Ra was detected by Western blot(WB), and the mRNA expression of NLRP3, PKCδ, pNLRC4, and IL-1Ra was detected by qRT-PCR. The results showed that compared with the blank control group, the VVC model group showed redness, edema, and white secretions in the vagina. Compared with the VVC model group, the BAEB groups showed improved general state of VVC mice. As revealed by Gram staining, Papanicolaou staining, microdilution assay, and HE staining, compared with the blank control group, the VVC model group showed a large number of hyphae, neutrophils infiltration, and increased fungal load in the vaginal lavage, destroyed vaginal mucosa, and infiltration of a large number of inflammatory cells. BAEB could reduce the transformation of C. albicans from yeast to hyphae. High-dose BAEB could significantly reduce neutrophil infiltration and fungal load. Low-and medium-dose BAEB could reduce the da-mage to the vaginal tissue, while high-dose BAEB could restore the damaged vaginal tissues to normal levels. ELISA results showed that the content of inflammatory cytokines IL-1β, IL-18, and LDH in the VVC model group significantly increased compared with that in the blank control group, and the content of IL-1β, IL-18 and LDH in the medium-and high-dose BAEB groups was significantly reduced compared with that in the VVC model group. WB and qRT-PCR results showed that compared with the blank control group, the VVC model group showed reduced protein and mRNA expression of PKCδ, pNLRC4, and IL-1Ra in vaginal tissues of mice and increased protein and mRNA expression of NLRP3. Compared with the VVC model group, the medium-and high-dose BAEB groups showed up-regulated protein and mRNA expression of PKCδ, pNLRC4, and IL-1Ra in vaginal tissues and inhibited protein and mRNA expression of NLRP3 in vaginal tissues. This study indicated that the therapeutic effect of BAEB on VVC mice was presumably related to the negative regulation of NLRP3 inflammasome by promoting PKCδ/NLRC4/IL-1Ra axis.

Effect of Polysaccharides and n-Butanol Fractions of Atractylodis Rhizoma Stir-fried with Bran on Metabonomics in Rats with Spleen Deficiency / 中国实验方剂学杂志

ObjectiveTo explore the regulatory effect of polysaccharides and n-butanol fractions of Atractylodis Rhizoma stir-fried with bran on the plasma metabolites of spleen-deficient rats， and then to elucidate their mechanisms of spleen-enhancing effects. MethodForty male SD rats were randomly divided into the blank group， model group， polysaccharide group （FD group， 0.075 6 g·mL-1·d-1）， n-butanol fractions group （FZ group， 0.012 1 g·mL-1·d-1）， with 10 rats in each group. Except the blank group， the other three groups used the compound factors of overwork， dietary disorders and intragastric administration of Sennae Folium decoction to replicate the rat model of spleen deficiency. After the end of modeling， the FD group and FZ group were given the corresponding medicinal solution by gavage for 7 d， meanwhile， the blank group and model group were given an equal volume of saline. The plasma samples from rats in the blank， model， FZ and FD groups were analyzed by ultra-high performance liquid chromatography-quadrupole/electrostatic field orbitrap high-resolution mass spectrometry （UHPLC-Q-Orbitrap-MS）， multivariate statistical methods were used to process the data and screen differential metabolites， and metabolic pathway enrichment analysis of the screened differential metabolites was performed using the Kyoto Encyclopedia of Genes and Genomes （KEGG)）database and MetaboAnalyst 5.0. ResultThe results of multivariate statistical analysis showed that there were significant differences in plasma metabolites between the model group and blank group， FZ group and model group， FD group and model group. There were 380 differential metabolites between the blank group and the model group， of which 78 and 57 were called back by polysaccharides and n-butanol fractions of Atractylodis Rhizoma stir-fried with bran， respectively. Metabolic pathway enrichment results showed that the n-butanol fractions mainly affected glycine， serine and threonine metabolism， alanine， aspartate and glutamate metabolism， D-arginine and D-ornithine metabolism， which were summarized as amino acid metabolism， while the polysaccharides mainly affected glycine， serine and threonine metabolism， alanine， aspartate and glutamate metabolism， tricarboxylic acid cycle， biotin metabolism and thiamine metabolism. ConclusionBoth of polysaccharides and n-butanol fractions of Atractylodis Rhizoma stir-fried with bran have significant regulating effects on the metabolic abnormalities in spleen-deficient rats， in which the n-butanol fractions is mainly involved in amino acid metabolism， and the polysaccharides are involved in energy metabolism and cofactor and vitamin metabolism in addition to regulating amino acid metabolism.

Determination of content of matricin extracted from Cichorium glandulosum Boiss et Huet with n-butanol and its protective effect on hepatic fibrosis in rats / 中国药理学通报

Aim To investigate the effects of Cichorium glandulosum N-butanol extraction site (C G E) on hepatic fibrosis (H F) in SD rats and to determine the content of the main effective component matricin. Methods HPLC method was used to determine the content of matricin in CGE. The SD rats were randomly divided into control group, model group, CGE low-dose groups, medium-dose and high-dose, and curcumin group. In addition to control group rats' back subcutaneous injection (s c) normal saline, rats in the other groups were treated with body weight sc 40 % CC1

Screening of active fractions of Jiegu ointment for promoting fracture healing in New Zealand rabbits / 中国药房

OBJECTIVE To screen the active site of Jiegu ointment in promoting fracture healing in New Zealand rabbits. METHODS The ethanol extract of Jiegu ointment， as well as the ethyl acetate and n-butanol parts， were prepared and mixed with honey to form a plaster with appropriate viscosity. The radial fracture model of left forelimb in New Zealand rabbit was established and divided into model control group， ethanol extract group， ethyl acetate fraction group and n-butanol fraction group， with 6 rabbits in each group. Except for model control group， rabbits of all other groups were treated with corresponding polar part of Jiegu ointment for external application， for 4 weeks. The radial fracture healing of rabbits was studied by X-ray examination. Enzyme-linked immunosorbent assay was used to detect the serum levels of interleukin-6 （IL-6）， tumor necrosis factor α （TNF-α）， osteocalcin （OC）， vascular endothelial growth factor A （VEGFA）， basic fibroblast growth factor 2 （bFGF2） and alkaline phosphatase （ALP）. HE staining was adopted to observe the changes of pathological morphology of rabbit fracture site， and immunohistochemical method was used to detect the protein expression of bFGF2 in fracture site of rabbits. RESULTS The healing speed of the fracture site in the n-butanol fraction group was the fastest， followed by ethanol extract group， and the ethyl acetate fraction group was the slowest； the serum levels of TNF-α and IL-6 in n-butanol fraction group decreased the fastest， while the levels of ALP， bFGF2， OC and VEGFA increased the fastest [significant increase compared with ethanol extract group （P＜0.01）]； the chondrocytes at the fracture fraction completely disappeared， forming a large number of bone marrow cavities， and the bone trabeculae in the bone marrow cavity were officially formed. The expression level of bFGF2 was also higher than ethanol extract group. CONCLUSIONS The effect of n-butanol fraction on promoting fracture healing is more significant than ethyl acetate fraction and ethanol extract， and n-butanol fraction is the active fraction of Jiegu ointment to promote fracture healing.

Effects of N-butanol extract of Amygdalus mongolica on rats with bleomycin‐induced pulmonary fibrosis based on metabolomics

Pulmonary fibrosis (PF) is a major public health issue with limited treatment options. As the active ingredient of the n-butanol extract of Amygdalus mongolica (BUT), amygdalin inhibits PF. However, its mechanisms of action are unclear and need further verification. Therefore, the purpose of the present studies was to investigate the anti-fibrotic effects of BUT on PF by serum metabolomics and the transforming growth factor β (TGF-β) pathway. Sixty male Sprague-Dawley rats were randomly divided into control, untreated PF, prednisone-treated (5 mg/kg), and BUT-treated (1.75, 1.25, 0.75 g/kg) groups, and the respective drugs were administered intragastrically for 21 days. The serum metabolomics profiles were determined by ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-QTOF/MS) and metabolism network analysis. The expression of TGF-β1, Smad-3, Smad-7, and α-smooth muscle actin (α-SMA) was measured using a real-time polymerase chain reaction in the lung tissue. BUT significantly alleviated fibrosis by reducing the mRNA expressions of TGF-β1 (from 1.73 to 1.13), Smad-3 (from 2.01 to 1.19), and α-SMA (from 2.14 to 1.19) and increasing that of Smad7 (from 0.17 to 0.62). Twenty-eight potential biomarkers associated with PF were identified. In addition, four key biomarkers were restored to baseline levels following BUT treatment, with the lowest dose showing optimal effect. Furthermore, A. mongolica BUT was found to improve PF by the pentose phosphate pathway and by taurine, hypotaurine, and arachidonic acid metabolism. These findings revealed the mechanism of A. mongolica BUT antifibrotic effects and metabolic activity in PF rats and provided the experimental basis for its clinical application.

n-butanol part from Qubai tablet and study on its pharmacodynamics to de melanocyte model / 中国药房

OBJECTIVE To stud y the chemical cons tituents of n-butanol part of Qubai tablet and its pharmacodynamic effect on the model of de melanocyte. METHODS The n-butanol part of Qubai tablet was prepared. The chemical constituents were analyzed by ultra-high performance liquid chromatography-mass spectrometry （UPLC-MS）. Taking mice B 16 melanoma cells as the research object ，the de melanocyte model was established and divided into model group ，positive control different concentration groups（8-methoxypsoralen 10，50，100，150，200 μmol/L），solvent group （diluted with DMSO ）and Qubai tablet n-butanol part different concentration groups （10，50，100，150，200 μmol/L）. The number of cells were observed by inverted microscope ，and the cell proliferation rate ，the rate of melanin production and promotion rate of tyrosinase activity were also detected. RESULTS In the positive and negative ion mode ，53 compounds in the n-butanol part of Qubai tablet were preliminarily determined （29 in the positive ion mode ，33 in the negative ion mode ，overlapping 9），of which coumarins accounted for the largest proportion ， followed by flavonoids. The n-butanol part of Qubai tablet could significantly increase the number of cells ，which was positively correlated with the action time and administration concentration. It could significantly increase the proliferation rate of cells ，the rate of melanin production and promotion rate of tyrosinase activity （P＜0.01）. CONCLUSIONS Coumarins and flavonoids may be the material basis for the anti-vitiligo effect of n-butanol part from Qubai tablet ；anti-vitiligo effect of n-butanol part of Qubai tablet may be realized by promoting tyrosinase activity.

N-butanol combined with turpentine instead of xylene for paraffin embeddin / 解剖学报

Objective To look for a tissue paraffin embedding method that can replace xylene transparent agent. Methods The mixture of N-butanol and turpentine was used to replace the role of anhydrous ethanol and xylene in the process of conventional paraffin embedding. The brain, kidney, stomach, liver and duodenum of multiple cerebral infarction model rats were embedded in paraffin. Finally, the new dehydration procedure was evaluated according to the effect of paraffin section, HE staining and immunohistochemical result . Results The mixture of N-butanol and turpentine could replace not only the dehydration effect of anhydrous ethanol but also the transparency effect of xylene in the conventional paraffin embedding process. The tissue sections treated with the mixture of N-butanol and turpentine were smooth, and the tissue did not become brittle or hard; After HE staining, the nucleus and cytoplasm of the new dehydrated tissue were distinct, and the chromaticity, color and transparency of the tissue were not different from those of the conventional dehydration procedure; Immunohistochemical staining was performed on different tissues of rats, and the comparison result were no different from conventional embedded tissue immunohistochemical staining. Conclusion N-butanol combined with turpentine for tissue dehydration can not only avoid the toxic effect of xylene on human, but also reduce the tissue damage caused by excessive dehydration of anhydrous alcohol.

Analysis and Identification of Chemical Constituents in Hypoglycemic Effective Fractions of Longan Folium Based on UPLC-Q-Orbitrap HRMS / 中国实验方剂学杂志

Objective:Chemical constituents in hypoglycemic effective fractions of Longan Folium were isolated and identified by ultra performance liquid chromatography-quadrupole/electrostatic field orbitrap high resolution mass spectrometry （UPLC-Q-Orbitrap HRMS） to clarify the hypoglycemic substance basis of Longan Folium. Method:Chemical constituents in hypoglycemic effective fractions of Longan Folium were isolated on a Thermo Hypersil GOLD C₁₈ column （2.1 mm×100 mm， 1.9 μm）， the mobile phase was 0.1% formic acid acetonitrile solution and 0.1% formic acid solution （containing and 10 mmol ammonium acetate） for gradient elution. HRMS was operated in the positive and negative ion modes with the scanning range of <italic>m</italic>/<italic>z</italic> 100-1 500. Result:The secondary fragment ion information of target compounds was selected and compared with the compounds reported in the databases and related literature to further confirm these compounds. Nine compounds were identified in the ethanol fraction of Longan Folium， including cynaroside， kaempferol， quercitrin， luteolin， shikimic acid， citric acid， <italic>L</italic>-tyrosine， adenosine and nicotinamide. A total of 11 compounds were determined in the ethyl acetate fraction （cynaroside， quercitrin， kaempferol， luteolin， shikimic acid， gallic acid， protocatechuic acid， adenosine， nicotinamide， <italic>L</italic>-phenylalanine and scopoletin）， and 10 compounds were identified in the <italic>n</italic>-butanol fraction （cynaroside， kaempferol-3-<italic>O</italic>-rutinoside， kaempferol， astragalin， luteolin， citric acid， gallic acid， adenosine， nicotinamide and 5-hydroxymethylfurfural）. And five common compounds were identified in these three hypoglycemic effective fractions. Conclusion:The established UPLC-Q-Orbitrap HRMS can quickly identify chemical constituents in three hypoglycemic effective fractions of Longan Folium， their main chemical constituents are flavonoids and their glycosides， organic acids and nitrogen-containing compounds， which provides technical support and scientific evidence for the study on pharmacodynamic material basis and quality control of Longan Folium.

Antidepressant Effect of n-Butyl Alcohol Extracts from Xiaoyaosan via IGF-1Rβ/PI3K/Akt Pathway / 中国实验方剂学杂志

Objective:To investigate the intervention effect of <italic>n</italic>-butyl alcohol extracts from Xiaoyaosan against depression-like behavior induced by chronic unpredictable mild stress （CUMS） in model mice and the role of insulin-like growth factor-1 receptor <italic>β</italic> （IGF-1R<italic>β</italic>）/phosphatidylinositol-3 kinase （PI3K）/protein kinase B （Akt） signaling pathway in such intervention. Method:The effective dose of n-butyl alcohol extracts from Xiaoyaosan was preliminarily determined in model mice with behavioral despair. Then the male C57BL/6 mice were randomly divided into the blank group， model group， fluoxetine group， Xiaoyaosan group， and the low- （20 g·kg^-1） and high-dose （40 g·kg^-1） <italic>n</italic>-butyl alcohol extract groups. The mice in all groups except for the blank group were exposed to CUMS for inducing the depression-like behavior， which was judged by the sucrose preference test （SPT）. The successfully modeled mice in the medication groups were intragastrically administered with the corresponding drugs， whereas those in the blank and model groups were treated with an equal volume of solvent for five successive weeks. Following the SPT， tail suspension test （TST）， and novelty suppressed feeding test （NSFT） at the end of the fifth week， the insulin-like growth factor-1 （IGF-1） levels in mouse serum and hippocampus were measured by enzyme-linked immunosorbent assay （ELISA）. The average optical density （<italic>IA</italic>） of Nissl bodies in mouse hippocampal CA3 region was detected by toluidine blue staining. The 5-bromo-2-deoxyuridine （Brdu） and doublecortin （DCX） expression in the dentate gyrus （DG） was assayed using immunofluorescence method. The protein expression levels of IGF-1R<italic>β</italic>， PI3K， phosphorylated-PI3K （p-PI3K）， Akt， p-Akt， cysteine aspartic acid-specific protease 3 （Caspase-3）， and cleaved Caspase-3 in the hippocampus were determined by Western blot. Result:The results of forced swimming test and TST showed that n-butyl alcohol extracts from Xiaoyaosan at 9.1 and 40 g·kg^-1 both significantly shortened the immobility time of mice （<italic>P</italic><0.05， <italic>P</italic><0.01）， indicating that the effective dose ranged from 9.1-40 g·kg^-1. Compared with the model control， the n-butyl alcohol extracts from Xiaoyaosan at 20 and 40 g·kg^-1 significantly increased the sucrose preference percentage （<italic>P</italic><0.05， <italic>P</italic><0.01）， shortened the immobility time in TST （<italic>P</italic><0.01） and the feeding latency in NSFT （<italic>P</italic><0.01）， reversed the down-regulated IGF-1 content in mouse serum and hippocampus （<italic>P</italic><0.01）， increased the AOD of Nissl bodies in the hippocampal CA3 region （<italic>P</italic><0.01）， promoted the expression of Brdu and DCX in DG （<italic>P</italic><0.05， <italic>P</italic><0.01）， and down-regulated the protein expression levels of IGF-1R<italic>β</italic> （<italic>P</italic><0.05， <italic>P</italic><0.01）， p-PI3K/PI3K （<italic>P</italic><0.05， <italic>P</italic><0.01）， p-Akt/Akt （<italic>P</italic><0.05）， and cleaved Caspase-3/Caspase-3 in the hippocampus of CUMS mice. Conclusion:The n-butyl alcohol extracts from Xiaoyaosan are equivalent to Xiaoyaosan in inhibiting expression. They alleviate the depression-like behavior in CUMS mice， induce the production of Nissl bodies in hippocampal CA3 region， enhance neuronal proliferation and differentiation in DG， and facilitate neurogenesis. All these may be related to the inhibition of over-activated IGF-1R<italic>β</italic>/PI3K/Akt pathway and the reduction of neuronal apoptosis.

Anti-acetylcholinesterase Active Ingredients from Aconitum tanguticum by UPLC-Q-TOF-MS/MS / 中国实验方剂学杂志

Objective:To identify the anti-acetylcholinesterase active ingredients in <italic>Aconitum tanguticum</italic>， so as to lay the foundation for finding new anti-Alzheimer's disease （AD） drugs. Method:The anti-acetylcholinesterase active fractions of <italic>A. tanguticum</italic> were screened by the modified Ellman's method， and the chemical composition of the active fraction was analyzed by ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry （UPLC-Q-TOF-MS/MS）. The chromatographic separation was performed on an ACQUITY UPLC BEH C₁₈ column （2.1 mm×50 mm， 1.7 μm） with acetonitrile （A）-0.4% ammonia aqueous solution （B） as mobile phase for gradient elution， and the column temperature was set at 30 ℃ with the flow rate of 0.4 mL·min^-1. Phase A of the dichloromethane fraction changed with time as follows：0-3 min， 5%A； 3-7 min， 5%-20%A； 7-11.5 min， 20%-33%A； 11.5-15.5 min， 33%-50%A； 15.5-20.5 min， 50%-80%A； 20.5-23 min， 80%-85%A； 23-25 min， 85%-95%A. Phase A of the <italic>n</italic>-butanol fraction changed with time as follows：0-2 min， 5%A； 2-8 min， 5%-20%A； 8-11 min， 20%-33%A； 11-15 min， 33%-95%A. Mass spectrometry was performed on electrospray ionization， data were collected in positive ion mode， and the detection range was <italic>m</italic>/<italic>z</italic> 100-1 500. Result:Both the dichloromethane and <italic>n</italic>-butanol fractions had a certain inhibitory effect on acetylcholinesterase， their half inhibitory concentration （IC₅₀） values were （64±4.4） mg·L^-1 and （85.7±3.8） mg·L^-1， respectively. By UPLC-Q-TOF-MS/MS analysis， a total of 21 alkaloids were identified from the dichloromethane fraction， and 11 alkaloids were identified from <italic>n</italic>-butanol fraction. Guan-fu base Ⅰ， found in both fractions， was first discovered in <italic>A. tanguticum</italic>. Conclusion:Diterpene alkaloids are the main anti-acetylcholinesterase substances of <italic>A. tanguticum</italic>， which is worth further exploration.

Tert-butanol application and related research progress in biomedicine / 药学学报

italic>Tert-butanol is an organic solvent, widely used in the medical field and chemical industry. It could be characterized by high crystallization temperature and vapor pressure. It could be easily sublimed and removed during the freeze-drying process. This review mainly describes the use of tert-butanol in the lyophilized formulations of poorly soluble drugs, the lyophilization solvent of porous structure productions, and as an ice crystal growth guider. In addition, the application of tert-butanol in nano drugs and aerogels has also been reviewed, as well as the current research progress in its quality and safety.

Chemical constituents from the stem of Callerya nitida Benth.var.hirsutissima Z.Wei / 中国药科大学学报

@#The chemical constituents from 70% ethanol petroleum ether and n-butanol extractions of Callerya nitita Benth.var.hirsutissima.Z.Wei. were separated by preparative high-performance liquid chromatographic techniques, including repeated column chromatography over macroporous adsorption resin, silica gel, ODS, Sephadex LH-20. The structures of the compounds were identified by their physicochemical properties, spectral data, and mass spectrometry data, in comparison with literature. In our research, one triterpenoids, taraxerone (1), and twenty flavonoids, including genistein-4′-O-β-glucoside (2), 5-hydroxy-4′-methoxyisoflavone-7-O-β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside (3), biochanin A 7-O-β-D-apiofuranosyl-(1→5)-β-D-apiofuranosyl- (1→6)-β-D-glucopyranoside (4), formononetin-7-O-β-D-galactopyranoside (5), 5,7-dihydroxy-3′,4′-dimethoxyisoflavone (6), biochanin A-7-O-β-D-apiofuranosyl-(1→2)-β-D-glucopyranoside (7), 5, 7-dihydroxyisoflavone-4′-O-α-L-rhamnopyranosyl-(1→2)-O-β-D-glucopyranoside (8), formononetin-7-O-D-apio-β-D-furanosyl(l→2)-β-D-glucopyranoside (9), 4′-hydroxy-3′-methoxyisoflavone-7-O-β-D-apiofuranosyl-(1→6)-β-D-glucopyranoside (10), prunetin (11), prunetin 4′-O-β-D-glucopyranoside (12), pratensein7-O-β-D-glucoside (13), 8-methoxyisoformononetin (14), genistein (15), 3′-hydroxybiochanin A (16), biochanin A (17), 5,7-dihydroxy-3′,5′-dimethoxyisoflavone (18), ononin (19), isoformononetin (20), 5,7,3′,4′-tetrahydroxyflavone (21) were isolated from the two extract parts.Compounds 1-10, 12-14, 16-18, 20 were obtained from this plant, and it is the first time to investigate the plant for the first time.

Chemical Constituents of n-Butanol Extract Part of Akebia trifoliata Caulis / 中国实验方剂学杂志

<b>Objective::To study the chemical constituents from <italic>n</italic>-butanol extract of <italic>Akebia trifoliata</italic> caulis. <b>Method::The 100 kg caulis of <italic>A</italic>. <italic>trifoliata</italic> was extracted with 75% ethanol (EtOH) for three times by heating reflux. These 3 extracts were decompressed and concentrated, and then dissolved in water. The solvent was successively extracted with dichloromethane, ethyl acetate and <italic>n</italic>-butanol. The chemical constituents from the <italic>n</italic>-butanol fraction were isolated by macroporous, silica gel, sephadex LH-20 and ODS columns, and semi-preparative high performance liquid chromatography, and their chemical structures were determined through MS, NMR analysis (¹H and ¹³C-NMR) and spectroscopic data from literatures. <b>Result::Totally 14 compounds were isolated and identified as mutongsaponin B(<bold>1</bold>), mutongsaponin C(<bold>2</bold>), saponin PH(<bold>3</bold>), begoniifolide A(<bold>4</bold>), 2<italic>α</italic>, 3<italic>β</italic>, 23-trihydroxy-30-noroleana-12, 19-dien-28-oicacid-<italic>O</italic>-<italic>β</italic>-<italic>D</italic>-xylopyranosyl-(1→3)-<italic>α</italic>-<italic>L</italic>-rhamnopyranosyl-(1→4)-<italic>β</italic>-<italic>D</italic>-glucopyranosyl-(1→6)-<italic>β</italic>-<italic>D</italic>-glucopyranosyl ester(<bold>5</bold>), akemisaponins D(<bold>6</bold>), akemisaponins E(<bold>7</bold>), asiaticoside(<bold>8</bold>), saponin PJ1(<bold>9</bold>), scheffoleoside A(<bold>10</bold>), symplocosneolignan A(<bold>11</bold>), kalopanax-saponins D(<bold>12</bold>), leonticin E(<bold>13</bold>), ciwujianoside A₁(<bold>14</bold>). <b>Conclusion::Compounds <bold>1-4</bold>, <bold>11</bold>, <bold>13, 14</bold> were isolated from this plant for the first time. The discovery of these compounds further enriched the chemical constituents of <italic>A</italic>. <italic>trifoliata</italic>, and provided experimental and scientific basis for the comprehensive development and utilization of <italic>A</italic>. <italic>trifoliata</italic>.

Volumetric behaviour of tetra-n-butyl ammonium bromidein various solvents at different temperatures / Comportamiento volumétrico del bromuro de tetra-n-butilamonio en varios solventes a diferentes temperaturas

ABSTRACT Measurement of ultrasonic velocity, density and viscosity of solutions of Tetra Butyl Ammonium Bromide have been carried outin different solvents (water, methanol, ethanol, 1-propanol and 1-butanol) as functions of concentration (1 to 0.1 M) at different temperatures (298.15 K to 318.15K). Using these experimental data, various acoustical and apparent parameters such as acoustical impedance, intermolecular free length, adiabatic compressibility, molar compressibility, Van der Waals constant, relaxation strength, apparent molar isentropic compressibility, apparent molar volume have been evaluated. Further, some thermodynamic parameters such as Gibbs free energy of activation, enthalpy and entropy of activation have been evaluated. All these parameters have been evaluated to understand type of interactions present in studied solutions.

RESUMEN La medición de la velocidad ultrasónica, la densidad y la viscosidad de algunas soluciones de bromuro de tetra-n-butilamonio se llevó a cabo en diferentes solventes (agua, metanol, etanol, 1-propanol y 1-butanol) en función de la concentración (1 a 0,1 M) y a diferentes temperaturas (298,15 K a 318.15 K). Utilizando estos datos experimentales, se evaluaron varios parámetros acústicos y aparentes, como la impedancia acústica, la longitud libre intermolecular, la compresibilidad adiabática, la compresibilidad molar, la constante de Van der Waals, la fuerza de relajación, la compresibilidad isentrópica molar aparente, el volumen molar aparente, etc. Además, se evaluaron algunos parámetros termodinâmicos, como la energía de activación libre de Gibbs, la entalpia y la entropía de activación. Todos estos parámetros han sido evaluados para comprender el tipo de interacciones presentes en las soluciones estudiadas.

Acetone­butanol­ethanol fermentation from sugarcane bagasse hydrolysates: utilization of C5 and C6 sugars

Background: Fuels and chemicals from renewable feedstocks have a growing demand, and acetone, butanol and ethanol (ABE) are some relevant examples. These molecules can be produced by the bacterial fermentation process using hydrolysates generated from lignocellulosic biomass as sugarcane bagasse, one of the most abundant sources of lignocellulosic biomass in Brazil. It originates as a residue in mills and distilleries in the production of sugar and ethanol. Results: In the present work, two strategies to generate hydrolysates of sugarcane bagasse were adopted. The fermentation of the first hydrolysate by Clostridium acetobutylicum DSM 6228 resulted in final concentrations of butanol, acetone and ethanol of 6.4, 4.5 and 0.6 g/L, respectively. On the other hand, the second hydrolysate presented better results (averages of 9.1, 5.5 and 0.8 g/L, respectively), even without the need for nutrient supplementation, since key elements were already present in the medium. The productivity (QP) and yield (YP/S) of the solvents with second hydrolysate were 0.5 g/L•h-1 and 0.4 g/g, respectively. Conclusions: The results described herein open new perspectives for the production of important molecules from residual lignocellulosic biomass for the fuel and chemical industries within the context of second-generation biorefinery.

Evaluation of Antimicrobial Activities of Fractions of Plant Parts of Pterocarpus santalinoides

Aims: The study aims to investigate the antimicrobial activities of the leaves, seeds, bark, and root of Pterocarpus santalinoides plant. Study Design: Agar well diffusion and Agar well dilution methods were used to test the preliminary antimicrobial and minimum inhibitory/bactericidal/fungicidal concentrations respectively of Pterocarpus santalinoides plants. Place and Duration of Study: Department of Pharmaceutical Microbiology and Biotechnology, Faculty of Pharmaceutical Sciences, Nnamdi Azikiwe University, Agulu Campus, Nigeria, between February – October, 2017. Methodology: Primary extraction and fractionation of the plant parts were undertaken with methanol, butanol, ethyl acetate, and n-hexane. Agar diffusion method for the primary antimicrobial screening on Muller-Hinton agar (bacteria) and Sabouraud dextrose agar (fungi) were used to assess the antimicrobial activities of the sixteen (16) samples on some microbial isolates namely Salmonella typhi, Escherichia coli, Candida albicans, Aspergillus niger, Microsporon canis, and Trichophyton rubrum. The minimum Inhibitory concentration (MIC), minimum bactericidal/fungicidal concentration (MBC/MFC) and percentage inhibition diameter growth (PIDG) of the samples that yielded positive activity were also evaluated. Results: Twelve (12) samples exhibited inhibitory activity on at least one or more of the test isolates. The MIC range observed for the extracts and fractions that yielded positive activity was 12.5 – 100 mg/ml. The n-hexane fraction of the plant root indicated the best value of 12.5 mg/ml against M. canis. The best MBC/MFC value of 25 mg/ml was observed with the ethyl acetate fraction of the bark (against E. coli and M. canis) and the n-hexane fraction of the root (against M. canis). The result showed S. typhi to be the most sensitive organism to the metabolites of P. santalinoides. Extended-spectrum activity was observed with the ethyl acetate fraction of the bark against three (3) of the test isolates namely S. typhi, E. coli and M. canis. The determination of PIDG values for the test organisms against the plants’ extracts/fractions showed that crude methanol extract (28.57%) and ethyl-acetate fraction (0.14%) of the leaves, butanol fraction (0.14%) of the root (all against S. typhi) were the most potent test samples. Conclusion: The results indicated that the plant parts may have potential medicinal values and confirmed its use in traditional medicine.

Antimalarial activities of butanol and ethylacetate fractions of Combretum nigricans leaf

Objective: To evaluate the antimalarial activity of the ethylacetate and butanol fractions of Combretum nigricans (C. nigricans) leaf extract in mice. Methods: C. nigricans solvent (butanol and ethylacetate) fractions were screened for their phytochemical constituents using standard procedures illustrated by Harborne and Evans. The Peters' 4-day suppressive test against early malaria infection, Rane's curative test against established malaria and prophylactic test for residual activity were employed for evaluating the antimalarial potential in mice. Results: The phytochemical screening revealed the presence of alkaloids, terpenoids, saponins, and flavonoids in both fractions at different intensity. Both fractions exhibited significant antimalarial activity in all test models (P<0.05). The ethylacetate fraction of C. nigricans had better chemosuppressive and curative effects compared to the butanol fraction, which however, elicited a better chemoprophylactic effect. The chemosuppressive effect of C. nigricans ethylacetate fraction (200-800 mg/kg) was 77.6%, 69.1% and 86.1%; curative effect was 62.3%, 71.3% and 72.4%; while the chemoprophylactic activity was 32.1%, 48.6% and 61.2% respectively. C. nigricans butanol fraction (200-800 mg/kg) had 40.3%, 54.1% and 69.1% chemosuppression; 26.2%, 36.9% and 34.5% curative effect; and 48.4%, 70.0% and 87.4% chemoprophylaxis. Conclusions: Both solvent fractions of C. nigricans possess antimalarial activity, and may be useful at different stages of malaria therapy.

Antimalarial activities of butanol and ethylacetate fractions of Combretum nigricans leaf

Objective: To evaluate the antimalarial activity of the ethylacetate and butanol fractions of Combretum nigricans (C. nigricans) leaf extract in mice.Methods: C. nigricans solvent (butanol and ethylacetate) fractions were screened for their phytochemical constituents using standard procedures illustrated by Harborne and Evans.The Peters' 4-day suppressive test against early malaria infection, Rane's curative test against established malaria and prophylactic test for residual activity were employed for evaluating the antimalarial potential in mice.Results: The phytochemical screening revealed the presence of alkaloids, terpenoids, saponins,and flavonoids in both fractions at different intensity. Both fractions exhibited significant antimalarial activity in all test models (P<0.05). The ethylacetate fraction of C. nigricans had better chemosuppressive and curative effects compared to the butanol fraction, which however,elicited a better chemoprophylactic effect. The chemosuppressive effect of C. nigricans ethylacetate fraction (200-800 mg/kg) was 77.6％, 69.1％ and 86.1％; curative effect was 62.3％, 71.3％ and 72.4％; while the chemoprophylactic activity was 32.1％, 48.6％ and 61.2％ respectively. C. nigricans butanol fraction (200-800 mg/kg) had 40.3％, 54.1％ and 69.1％ chemosuppression; 26.2％, 36.9％ and 34.5％ curative effect; and 48.4％, 70.0％ and 87.4％ chemoprophylaxis.Conclusions: Both solvent fractions of C. nigricans possess antimalarial activity, and may be useful at different stages of malaria therapy.

Spectrum-effect Relationship of Anti-inflammatory Active Components from Nonvolatile Fraction of Blumea balsamifera Based on Gray Correlation Analysis / 中国实验方剂学杂志

Objective: To study the correlation between UPLC fingerprint of anti-inflammatory effect of active components from nonvolatile fraction of Blumea balsamifera, and to provide the basis for clarifying the anti-inflammatory material basis of B. balsamifera. Method: UPLC was used to establish fingerprint of nonvolatile fraction of 12 batches of B. balsamifera and their common fingerprint peaks were identified by UPLC-Q-TOF-MS.The corresponding pharmacodynamic data were obtained by auricle swelling and inflammation model mice induced by xylene, and spectrum-effect relationship was established by gray correlation analysis. Result: A total of 14 common peaks in nonvolatile fraction of B. balsamifera were established by UPLC fingerprint and 9 common peaks of them were identified.The correlation between UPLC fingerprint and the anti-inflammatory activity was from 0.717 1 to 0.550 5.The contribution of chemical compositions represented by each characteristic peak to the anti-inflammatory efficacy was in the order of peak 3 > peak 9 > peak 4 > peak 11 > peak 2 > peak 1 > peak 14 > peak 7 > peak 6 > peak 5 > peak 12 > peak 8 > peak 10 > peak 13, and the top two peaks with strong contribution to anti-inflammatory effect were peak 3 and peak 9, they were 3-O-caffeoylquinic acid and 3, 5-di-O-caffeoylquinic acid identified by contrast reference substances, respectively. Conclusion: The active substances in nonvolatile fraction of B. balsamifera are obtained through the study on the relationship between spectrum and efficiency, and the anti-inflammatory efficacy of the nonvolatile fraction is the result of combination of various components.It is clear that the caffeoylquinic acid derivates act as predominant anti-inflammatory active substance of nonvolatile fraction of B. balsamifera.

Fermentation optimization based on cell self-adaptation to environmental stress - a review / 生物工程学报

In industrial fermentation processes, bacteria have to adapt environmental stresses. Sometimes, such a self-adaption does not work and will cause fermentation failures, although such adaptation also can generate unexpected positive effects with improved fermentation performance. Our review introduces cell self-adaption to environmental variations or stress, process optimization based on such self-adaptions, with heterologous proteins production by Pichia pastoris and butanol fermentation as examples. Our review can sever as reference for fermentation optimization based on cell self-adaption.