Ten alkaloids(1-10) were isolated from the ethyl acetate extract of the fruit of Lycium chinense var. potaninii by silica gel, ODS, and preparative high performance liquid chromatography(HPLC), and identified by NMR and MS as methyl(2S)-[2-formyl-5-(hydroxymethyl)-1H-pyrrol-1-yl]-3-(phenyl)propanoate(1), methyl(2R)-[2-formyl-5-(methoxymethyl)-1H-pyrrol-1-yl]-3-(phenyl)propanoate(2), 3-hydroxy-4-ethyl ketone pyridine(3), indolyl-3-carbaldehyde(4),(R)-4-isobutyl-3-oxo-3,4-dihydro-1H-pyrrolo[2,1-c][1,4]oxazine-6-carbaldehyde(5),(R)-4-isopropyl-3-oxo-3,4-dihydro-1H-pyrrolo[2,1-c][1,4]oxazine-6-car-baldehyde(6), methyl(2R)-[2-formyl-5-(methoxymethyl)-1H-pyrrol-1-yl]-3-(4-hydroxyphenyl)propanoate(7), dimethyl(2R)-[2-formyl-5-(methoxymethyl)-1H-pyrrol-1-yl]butanedioate(8), 4-[formyl-5-(methoxymethyl)-1H-pyrrol-1-yl]butanoate(9), 4-[2-formyl-5-(methoxymethyl)-1H-pyrrol-1-yl]butanoic acid(10). All the compounds were isolated from the plant for the first time. Among them, compounds 1-3 were new compounds. Compounds 1-9 were evaluated for hypoglycemic activity in vitro with the palmitic acid-induced insulin resistance in HepG2 cells. At 10 μmol·L~(-1), compounds 4, 6, 7, and 9 can promote the glucose consumption of HepG2 cells with insulin resistance.
Lycium/chemistry* ; Fruit/chemistry* ; Insulin Resistance ; Propionates ; Alkaloids/pharmacology*

Genkwa Fols, Kansui Radix, and Euphorbiae Pekinensis Radix in Shizao Decoction(SZD) are toxic to intestinal tract. Jujubae Fructus in this prescription can alleviate the toxicity, but the mechanism is still unclear. Therefore, this study aims to explore the mechanism. To be specific, 40 normal Sprague-Dawley(SD) rats were classified into the normal group, high-dose and low-dose SZD groups, and high-dose and low-dose SZD without Jujubae Fructus(SZD-JF) groups. The SZD groups were given(ig) SZD, while SZD-JF groups received the decoction without Jujubae Fructus. The variation of body weight and spleen index were recorded. The patho-logical changes of intestinal tissue were observed based on hematoxylin and eosin(HE) staining. The content of malondialdehyde(MDA) and glutathione(GSH) and activity of superoxide dismutase(SOD) in intestinal tissue were measured to evaluate the intestinal injury. Fresh feces of rats were collected to detect intestinal flora structure by 16S ribosomal RNA gene(16S rDNA) sequencing technology. The content of fecal short chain fatty acids and fecal metabolites was determined by gas chromatography-mass spectrometer(GC-MS) and liquid chromatography-mass spectrometer ultra-fast liquid chromatography-quadrupole-time-of-flight mass spectrometer(UFLC-Q-TOF-MS), separately. Spearman's correlation analysis was employed to analyze the differential bacteria genera and differential metabolites. RESULTS:: showed that high-dose and low-dose SZD-JF groups had high content of MDA in intestinal tissue, low GSH content and SOD activity, short intestinal villi(P<0.05), low diversity and abundance of intestinal flora, variation in the intestinal flora structure, and low content of short chain fatty acids(P<0.05) compared with the normal group. Compared with high-dose and low-dose SZD-JF groups, high-dose and low-dose SZD groups displayed low content of MDA in intestinal tissue, high GSH content and SOD activity, recovery of the length of intestinal villi, increased abundance and diversity of intestinal flora, alleviation of dysbacteria, and recovery of the content of short chain fatty acids(P<0.05). According to the variation of intestinal flora and fecal metabolites after the addition of Jujubae Fructus, 6 differential bacterial genera(Lactobacillus, Butyricimonas, Clostridia＿UCG-014, Prevotella, Escherichia-Shigella, Alistipes),4 differential short chain fatty acids(such as acetic acid, propionic acid, butyric acid, valeric acid) and 18 differential metabolites(such as urolithin A, lithocholic acid, and creatinine) were screened out. Beneficial bacteria such as Lactobacillus were in positive correlation with butyric acid and urolithin A(P<0.05). The pathogenic bacteria such as Escherichia-Shigella were in negative correlation with propionic acid and urolithin A(P<0.05). In summary, SZD-JF caused obvious intestinal injury to normal rats, which could lead to intestinal flora disorder. The addition of Jujubae Fructus can alleviate the disorder and relieve the injury by regulating intestinal flora and the metabolites. This study discusses the effect of Jujubae Fructus in relieving the intestinal injury caused by SZD and the mechanism from the perspective of intestinal flora-host metabolism, which is expected to serve as a reference for clinical application of this prescription.
Rats ; Animals ; Rats, Sprague-Dawley ; Propionates/pharmacology* ; Gastrointestinal Microbiome ; Fatty Acids, Volatile/pharmacology* ; Butyrates/pharmacology*

The diatom Nitzschia laevis is a good alternative source of eicosapentaenoic acid (EPA). Besides strategies for high cell density culture, EPA productivity may be further improved by herbicides. The effect of the herbicide quizalofop-p-ethyl on the growth and EPA production was studied in this paper. As the solvent of the herbicide, DMSO was proved to inhibit the growth and EPA production of N. laevis. The concentration of DMSO in the medium should not exceed 0.2%. Quizalofop-p-ethyl could cause morphology damage to the N. laevis cells. With the increasing concentration of quizalofop-p-ethyl from 0 mmol/L to 0.4 mmol/L, the dry cell weight production decreased, while at the same time, the lipid content of the dry cell mass increased. When treated with 0.1 mmol/L quizalofop-p-ethyl, the EPA content increased from 3.00% to 3.58% (of dry cell weight, DW), and the proportion of EPA (20:5) in total fatty acids (TFA) increased from 25.15% to 32.88% . These results indicated that the herbicide quizalofop-p-ethyl could stimulate the accumulation of EPA; therefore it might be useful for selecting algae colonies that overproduce EPA.
Culture Media ; Culture Techniques ; Diatoms ; growth & development ; metabolism ; Eicosapentaenoic Acid ; biosynthesis ; Herbicides ; pharmacology ; Propionates ; pharmacology ; Quinoxalines ; pharmacology

OBJECTIVETo study the chemical constituents of the bee-collected rape pollen.

METHODThe compounds were isolated by column chromatography on silica gel; Sephadex LH-20 and C18. Their structures were elucidated on the basis of spectral analysis.

RESULTNine compounds were isolated from the bee-collected rape pollen and the structures of them were kaemferol-3-O-beta-D-glucosyl-(2-->1)-beta-D-glucoside (1), kaemferol-3,4'-di-O-beta-D-glucoside (2), quercetin-3-O-beta-D-glucosyl-(2-->1)-beta-D-glucoside (3), nicotinic acid (4), nicotinamide (5), trans-p-coumaric acid-4-O-beta-D-glucopyranoside (6), kaemferol (7), beta-sitosterol (8) and 5-hydroxymethylfurfural (9).

CONCLUSIONCompounds 1-6 were isolated from the bee-collected rape pollen for the first time.

Animals ; Bees ; physiology ; Brassica napus ; chemistry ; physiology ; Coumaric Acids ; chemistry ; Dextrans ; chemistry ; Glucosides ; chemistry ; Molecular Structure ; Plant Extracts ; pharmacology ; Pollen ; chemistry ; physiology ; Propionates ; Sitosterols ; chemistry

OBJECTIVETo investigate the effect of isopropyl 3-(3,4-dihydroxyphenyl)-2- hydroxypropanoate on vascular smooth muscle.

METHODIsolated rat pulmonary artery was perfused and the tension of the vessel was measured, the effect of isopropyl 3-(3, 4-dihydroxyphenyl)-2-hydroxypropanoate on the pulmonary artery precontracted by noradrenaline (NE) and concentration-response curves of 5-hydroxytryptamine (5-HT), endothelin-1 (ET-1), U46619 and KCl was also observed.

RESULTIsopropyl 3-(3,4-dihydroxyphenyl) -2-hydroxypropanoate exerted relaxation effect on the endothelium-intact artery precontracted by NE in a concentration-dependent manner, which was inhibited with denuded endothelium. The right-shift of the concentration-response curves of 5-HT, ET-1, U46619 and KCl.

CONCLUSIONIsopropyl 3-(3,4-dihydroxyphenyl)-2-hydroxypropanoate have relaxation action on rat pulmonary artery in the way of endothelium-dependance, the mechanism of relaxation action by isopropyl 3-(3,4-dihydroxyphenyl) -2-hydroxypropanoate may be related to calcium channels.

Animals ; Female ; In Vitro Techniques ; Male ; Muscle Contraction ; drug effects ; Muscle, Smooth, Vascular ; drug effects ; physiology ; Propionates ; pharmacology ; Pulmonary Artery ; drug effects ; physiology ; Rats ; Rats, Sprague-Dawley

A change in pH can alter the intracellular concentration of electrolytes such as intracellular Ca2+ and Na+ ([Na+]i) that are important for the cardiac function. For the determination of the role of pH in the cardiac magnesium homeostasis, the intracellular Mg2+ concentration ([Mg2+]i), membrane potential and contraction in the papillary muscle of guinea pigs using ion-selective electrodes changing extracellular pH ([pH]o) or intracellular pH ([pH]i) were measured in this study. A high CO2-induced low [pH]o causes a significant increase in the [Mg2+]i and [Na+]i, which was accompanied by a decrease in the membrane potential and twitch force. The high [pH]o had the opposite effect. These effects were reversible in both the beating and quiescent muscles. The low [pH]o-induced increase in [Mg2+]i occurred in the absence of [Mg2+]o. The [Mg2+]i was increased by the low [pH]i induced by propionate. The [Mg2+]i was increased by the low [pH]i induced by NH4Cl-prepulse and decreased by the recovery of [pH]i induced by the removal of NH4Cl. These results suggest that the pH can modulate [Mg2+]i with a reverse relationship in heart, probably by affecting the intracellular Mg2+ homeostasis, but not by Mg2+ transport across the sarcolemma.
Animals ; Cations, Divalent ; Female ; Guinea Pigs ; Heart Ventricles/metabolism ; Hydrogen-Ion Concentration ; Ion Transport/physiology ; Ion-Selective Electrodes/veterinary ; Magnesium/*metabolism ; Male ; Membrane Potentials/physiology ; Papillary Muscles/*metabolism ; Propionates/pharmacology ; Sodium/*metabolism

This study was intended to look for anti-HIV chemical constituents of aerial parts of Caragana rosea Turcz. Column chromatographic technique was used for the isolation and purification of constituents of Caragana rosea under the guide of anti-HIV assay. The structures were established on the basis of physical and chemical properties and spectroscopic data. Five compounds were obtained from the EtOAc fraction of aerial parts of Caragana rosea and identified as myricetin (1), mearnsetin (2), p-hydroxy cinnamic acid (3), cararosinol A (4) and cararosinol B (5). At the same time, one possible transformation route between cararosinol B and kobophenol A, another resveratrol tetramer isolated from this plant previously, was proposed. Compounds 4, 5 are new resveratrol tetramers, compounds 1 -3 were isolated from this plant for the first time. All compounds showed no activities in an in vitro assay against HIV-1.
Anti-HIV Agents ; chemistry ; isolation & purification ; pharmacology ; Benzofurans ; chemistry ; isolation & purification ; pharmacology ; Caragana ; chemistry ; Coumaric Acids ; chemistry ; isolation & purification ; pharmacology ; Flavonoids ; chemistry ; isolation & purification ; pharmacology ; HIV-1 ; drug effects ; Molecular Structure ; Plant Components, Aerial ; chemistry ; Plants, Medicinal ; chemistry ; Propionates ; Stilbenes ; chemistry ; isolation & purification ; pharmacology