A new flavonoid glycoside from Epimedium sagittatum / 药学学报

Fourteen flavonoids were isolated and purified from Epimedium sagittatum by various chromatography techniques such as macroporous adsorbent resin, silica gel, ODS, Sephadex LH-20, HW-40C and semi-preparative HPLC. Their structures were identified by analysis of physicochemical properties and spectral data, and determined as 3′-hydroxy-baohuoside-Ⅱ (1), huazhongilexone-7-O-β-D-glucopyranoside (2), kaempferol-3-O-α-L-rhamnoside (3), baohuoside-Ⅱ (4), icariside-Ⅱ (5), kaempferol 3,7-di-O-α-L-rhamnopyranoside (6), (+)-aromadendrin (7), kaempferol 3-O-(2-O-β-D-apiofuranosyl)-α-L-rhamnopyranoside (8), sagittatoside A (9), 2″-O-rhamnosyl icariside-II (10), apigenin-7-O-β-D-glucoside (11), quercetin 3-O-β-D-apiofuranoyl-(1→2)-α-L-rhamnopyranoside (12), kaempferol (13), icariin (14). Among them, compound 1 is a new compound, while compounds 2, 6-8, 11, and 12 were isolated from E.sagittatum for the first time.

Chemical constituents from fruits of Cornus officinalis and their anti-Alzheimer's disease activity / 药学学报

Fifteen compounds were isolated from fruits of Cornus officinalis by various chromatographic techniques such as Toyopearl HW-40C, Sephadex LH-20, silica gel, and the semi-preparative HPLC. Their chemical structures were identified by analysis of physicochemical properties and spectral data, and determined as neolignan A (1), caffeic acid (2), trans-p-hydroxy cinnamic acid (3), esculetin (4), scopoletin (5), benzyl-7-O-β-D-glucopyranoside (6), tachioside (7), 6-O-(4-hydroxybenzoyl) arbutin (8), 2-(3′,4′-dihydroxyphenyl)-1,3-benzodioxole-5-carboxaldehyde (9), (-)-pinoresinol-4-O-β-D-glucopyranoside (10), (7S,8R)-dihydrodehydrodiconiferyl alcohol-9-O-β-D-glucopyranoside (11), (7S,8R)-dihydrodehydrodiconiferyl alcohol-9′-O-β-D-glucopyranoside (12), (+)-lyoniresinol (13), (+)-isolariciresinol-9-O-β-D-glucopyranoside (14), and isolariciresinol-9′-O-β-D-glucopyranoside (15). Compound 1 was a new compound and named as neolignan A, and compounds 6-9 and 14 were isolated from Cornus officinalis for the first time. Compounds 2, 3 and 15 efficiently alleviated the PC12 cells injury induced by Aβ25-35, suggesting their potential anti-Alzheimer's disease activity.

Effects of Tingli Dazao Xiefei Decoction on the immune inflammation and intestinal flora in asthmatic rats / 药学学报

The study aims to explore the intervention mechanism of Tingli Dazao Xiefei Decoction on asthma from the perspective of immune inflammation and intestinal flora, providing a theoretical basis for guiding clinical medication. The ovalbumin (OVA) asthmatic rat model was established by intraperitoneal injection of OVA sensitization solution and aerosol challenge, and divided into control (CON), model (M), dexamethasone group (DEX, 0.075 mg·kg-1) and Tingli Dazao Xiefei Decoction (TLDZ, 3.5 g·kg-1). Firstly, the effects of Tingli Dazao Xiefei Decoction on asthma symptoms of rats, lung and trachea pathological changes of asthmatic rats were observed by inducing cough and asthma experiment, phenol red excretion, hematoxylin-eosin staining (H&E), Masson and periodic acid Schiff (PAS) staining; the levels of transforming growth factor β1 (TGF-β1), interleukin (IL) 6 and IL-10 in rat serum and the levels of interferon γ (IFN-γ), immunoglobulin E (IgE), IL-4, IL-17A and tumor necrosis factor α (TNF-α) in bronchoalveolar lavage fluid (BALF) were detected by ELISA; the mRNA levels of IL-5, IL-13 and IL-33 in the lung were determined by qRT-PCR; the levels of macrophages and neutrophils in the spleen and the levels of natural killer cell (NK), helper T cell (Thc), dendritic cell (DC), regulatory T cell (Treg) and T helper cell 17 (Th17) in the peripheral blood were measured by flow cytometry combined with immunohistochemistry; the intestinal flora of asthmatic rats were analyzed by 16S rDNA high-throughput sequencing. Pathology and inflammatory results showed that Tingli Dazao Xiefei Decoction could effectively alleviate the asthma symptoms in rats, improve the pathological changes of lung tissue, reduce the production of goblet cells and collagen fibers, and reduce the inflammatory response in asthmatic rats; the results of immune cells showed that Tingli Dazao Xiefei Decoction could effectively increase the levels of NK, Thc, DC and Treg cells and reduce the levels of macrophages, neutrophils and Th17 cells in asthmatic rats; the results of intestinal flora showed that Tingli Dazao Xiefei Decoction could increase the levels of Lactobacillus, Ruminococcus, Christensenellaceae, Bifidobacterium and Eubacterium]_xylanophilum-group, and decrease the levels of Firmicutes, Desulfovibrio, Mucispirillum and Romboutsia in asthmatic rats. Therefore, it is speculated that Tingli Dazao Xiefei Decoction can improve the symptom of asthmatic rats by regulating the immune inflammation and intestinal flora in the asthmatic rats. All animal experiments in this article were approved by the Ethics Committee of Henan University of Chinese Medicine.

Active components of Descurainia sophia improve lung permeability in rats with allergic asthma by regulating airway inflammation and epithelial damage / 中国中药杂志

The present study investigated the effect of active components of Descurainia sophia on allergic asthma and explored the underlying mechanism. SD male rats were randomly divided into a normal group(NC), a model group(M), a D. sophia decoction group(DS), a D. sophia fatty oil group(FO), a D. sophia flavonoid glycoside group(FG), a D. sophia oligosaccharide group(Oli), and a positive drug dexamethasone group(Y). The allergic asthma model was induced in rats by intraperitoneal injection of ovalbumin(OVA) and aluminum hydroxide gel adjuvant(sensitization) and atomization of OVA solution(excitation). After modeling, asthma-related indicators, tracheal phenol red excretion, inflammatory cell levels in the peripheral blood, lung permeability index(LPI), and oxygenation index(OI) of rats were detected. The pathological changes of lung tissues were observed by HE staining. Enzyme-linked immunosorbent assay(ELISA) was used to detect the content of inflammatory factors immunoglobulin E(IgE), interleukin-4(IL-4), and interferon-γ(IFN-γ) in the bronchoalveolar lavage fluid(BALF) and the content of endothelin-1(ET-1) and angiotensin-converting enzyme(ACE) in lung tissue homogenate. The serum content of nitric oxide(NO) was detected by colorimetry. Western blot was employed to determine the protein expression of Toll-like receptor 4(TLR4), nuclear factor κB-p65(NF-κB-p65), phosphorylated NF-κB-p65(p-NF-κB-p65), myosin light chain kinase(MLCK), vascular endothelial cadherin(VE cadherin), connexin 43, and claudin 5, and the mechanism of active components of D. sophia on allergic asthma was explored. As revealed by the results, the M group showed extensive infiltration of inflammatory cells around the bronchus of the lung tissues of the allergic asthma rats, thickened bronchial wall, severely deformed alveolar structure, increased number of wheezes, the content of IgE, IL-4, ET-1, and ACE, inflammatory cells, and LPI, and reduced latency of asthma, tracheal phenol red excretion, IFN-γ, NO content, and OI. After the intervention of the active components of D. sophia, the DS, FO, FG, Oli, and Y groups showed improved asthma-related indicators, tracheal phenol red excretion, and lung tissue lesions in allergic asthma rats, and the effects in the FO and Oli groups were superior. The content of inflammatory factors in BALF was recovered in the DS, FO, and Y groups and the FG and Oli groups. The number of inflammatory cells in rats was reduced in the DS and FO groups, and the FG, Oli, and Y groups to varying degrees, and the effect in the FO group was superior. DS, FO, Oli, and Y reduced ET-1, ACE, and LPI and increased NO and OI. FG recovered NO, ET-1, ACE, LPI, and OI to improve lung epithelial damage and permeability. Further investigation of inflammation-related TLR4/NF-κB pathways, MLCK, and related skeleton protein levels showed that TLR4, NF-κB-p65, p-NF-κB-p65, and MLCK levels were increased, and VE cadherin, connexin 43, and claudin 5 were reduced in the M group. DS, FO, FG, Oli, and Y could reduce the protein expression related to the TLR4 pathway to varying degrees, and regulate the protein expression of MLCK, VE cadherin, connexin 43, and claudin 5. It is inferred that the active components of D. sophia improve lung permeability in rats with allergic asthma presumedly by regulating the TLR4/NF-κB signaling pathway to improve airway inflammation, mediating MLCK and connexin, and regulating epithelial damage.

A new nucleoside from the Oenothera biennis L / 药学学报

Seven nucleoside compounds were isolated from the Oenothera biennis L. by various chromatographic techniques such as Diaion HP-20, silica gel, Sephadex LH-20, MCI and semi-preparative HPLC. Their structures were identified by analysis of physicochemical properties and spectral data, and determined as 9-(3′-carbonyl methyl)hydroxypurine (1), 1-(3′-carbonyl methyl)purine-6,8-dione (2), N-methyl-2-pyridone-5-carboxamide (3), uracil (4), uridine (5), thymidine (6) and 2′-Ο-methoxy luridine (7). Compound 1 is a new nucleoside and compounds 2-7 were newly isolated from the Oenothera biennis L. Compounds 1-2 can significantly increase the viability of BEAS-2B cells induced by TGF-β1, showing potent anti-pulmonary fibrosis activity.

A new polyacetylene from the stems and leaves of Chrysanthemum morifolium Ramat / 药学学报

Eight polyacetylenes were isolated from the extract of the stems and leaves of Chrysanthemum morifolium by various chromatographic methods. Their structures were determined as 2E,4E,12Z-tetradecatriene-1-pyrrolidine-1-oxo-8,10-diynoic (1), tetradeca-2E,4E,12E-trien-8,10-diynoic acid pyrrolidide (2), tetradeca-2E,4E-dien-8,10-diynoic acid pyrrolidide (3), tetradeca-2E,4E,10Z-trien-8-ynoic acid pyrrolidide (4), 2E,4E,12E-tetradecatriene-8,10-diynoic acid isobutylamide (5), 2E,4E-undecyldiene-8,10-diynoic acid isobutylamide (6), 2E,4E,10E-N-isobutyl-2,4,10-tetradecatrien-8-ynoic acid amide (7), and undeca-2E,4E-diene-8,10-diynoic acid phenylethylamide (8) by spectroscopic methods, including UV, IR, ESI-MS, HR-ESI-MS, 1D and 2D NMR spectra. Among them, compound 1 is a new polyacetylene, and compounds 2-8 were isolated from this plant for the first time. Compounds 5-8 inhibited the proliferation of A549 cell significantly at certain concentration, showing potent antitumor activity.

A new lignan from Gleditsiae spina / 药学学报

The chemical constituents from ethyl acetate extract of Gleditsiae spina were isolated and purified by various chromatographic methods such as MCI gel CHP-20, ODS, Sephadex LH-20, silica gel and semi-preparative HPLC. Seven lignans were isolated and identified by spectroscopic data analyses as (7R,8S,7'E,7''S,8''R)-buddlenol P (1), (+)-syringaresinol (2), (+)-isolariciresinol (3), (7S,8R)-cedrusin (4), (7S,8R)-4,9,9'-trihydroxy-3,3'-dimethoxy-7,8-dihydrobenzofuran-1'-propylneolignan (5), 3',4-O-dimethylcedrusin (6), balanophonin (7). Among them, compound 1 is a new lignan, compounds 2-7 are isolated from the Gleditsia L. for the first time. MTT method was used to investigate the effect of compounds 2-7 on LPS-induced injury of NRK-52e cells. As a result, compounds 2, 3 and 7 exhibit protective effects against LPS-induced damage to NRK-52e cells.

A new alkaloid from Rehmanniae Radix Preparata / 药学学报

The chemical constituents of Rehmanniae Radix Preparatawere prepared according to the traditional method of "jiu zheng jiu shai" and investigated using multiple chromatographic methods. Six alkaloids were isolated and their structures were elucidated from spectral data and physicochemical properties, as follows: rehmanniae alkaloid A (4-{[(5-O-á-D-galactopyranosyloxy)methyl]-1H-pyrrole-2-carbaldehyde-1-yl}butyric acidmethyl ester) (1), baimantuoluoamide B (2), capparisine C (3), harman-3-carboxylic acid (4), (2S)-1-[2-(furan-2-yl)-2-oxoethyl]-5-oxopyrrolidine-2-carboxylate (5), and 1-[2-(furan-2-yl)-2-oxoethyl]pyrrolidin-2-one (6). Among them, compound 1 is a new alkaloid. Compounds 2-6 were newly isolated from Rehmannia glutinosa Libosch.The effect of compounds 1-6 on NRK-52e cell injury induced by LPS was investigated. The results show that compounds 1-3 exhibit protective effects against LPS-induced damage to NRK-52e cells.

Effect of Descurainia sophia on H2O2-induced myocardial injury via suppressing oxidative stress and autophagy pathway / 中草药

Objective To study the protective effect of aqueous extract from Descurainia Sophia (DS) on H2O2-induced H9c2 cardiomyocyte injury and to initially explore the potential mechanism. Methods The peaks of main components in DS were analyzed and identified by HPLC-MS. H9c2 cell injury model was established by H2O2. H9c2 cells were cultured in vitro and divided into control group, model group, probucol group, and DS at 100, 200, 400 μg/mL groups. In order to reveal the possible molecular mechanisms, the viability of H9c2 cells was measured by MTT assay; The apoptosis rate, autophagy rate, mitochondrial membrane potential, and reactive oxygen species (ROS) level were detected by flow cytometry; The relative indicators of cell oxidative stress were determined by biochemical kit; The expression levels of apoptosis-related protein and the autophagy-related protein were evaluated by Incell-western method. Results Seven components with the highest content were identified in DS through the results of mass spectrometry. Compared with the model group, DS can improve the cell viability (P < 0.05, 0.01) and survival rate of H9c2 cells (P < 0.01); At the same time, apoptosis was attenuated (P < 0.01), mitochondrial membrane potential was upregulated (P < 0.01), apoptosis related proteins Caspase-3, Bax/Bcl-2 were obviously downregulated (P < 0.01), autophagy phenomenon was attenuated (P < 0.01), autophagy related proteins LC3B and p62 were upregulated (P < 0.01). In addition, ROS level was decreased (P < 0.01), T-SOD and GSH-PX were upregulated and the levels of LDH and MDA were significantly decreased (P < 0.01). Conclusion This study suggests that DS can effectively protect H2O2-induced H9c2 cells injury, and the mechanism may be associated with improving oxidative stress in cells, inhibiting cell apoptosis and autophagy, which may be related to flavonoid glycosides.

Cloning and Expression Analysis of PaAACT Gene from Phytolacca americana / 中国实验方剂学杂志

Objective: To clone the key enzyme gene involved in the biosynthesis of esculentoside A(EsA),acetoacetyl-CoA transferase(AACT) gene was cloned from Phytolacca americana for bioinformatics analysis and prokaryotic expression. Method: Total RNA was extracted from the root of P. americana, and then cDNA was synthesized through the reverse transcription. Based on analysis of the transcriptome data of P. americana, the specific primers of PaAACT gene were designed,and the cDNA sequence of PaAACT gene was amplified by polymerase chain reaction(PCR) method. Prokaryotic induction,expression and purification of the target protein were induced through the construction of the prokaryotic expression vector pET-32a-PaAACT. Result: The open reading frame (ORF) of PaAACT gene was 1 254 bp,and encoded 417 amino acid residues. Bioinformatic analysis showed that the molecular formula of PaAACT protein was C1 914H3 120N538O576S17,inferring that its molecular weight was 43.43 kDa,the theoretical isoelectric point was 8.90,and the instability index of PaAACT protein was 32.27,which was a stable protein. According to bioinformatics analysis,PaAACT protein was a member of the thiolase family and contained one conserved site and one active site of the thiolase family at the C-terminal. PaAACT protein may be located in the cytoplasm,without a signal peptide or transmembrane domain. The phylogenetic analysis indicated that PaAACT protein showed the highest homology with AACT protein from polygonaceae plants (such as Beta vulgaris). The recombinant PaAACT protein was successfully expressed in Escherichia coli BL21(DE3) strain through IPTG induction, and the purified target protein was obtained by Ni2+ affinity chromatography. Conclusion: In this study,the PaAACT gene was cloned from P. americana,which lays a foundation for further determination of enzyme activity assay of PaAACT and preparation of antibody,and provides the theoretical basis for studying its role in the biosynthesis pathway of EsA.

Effect of Nature and Flavor Subdivision of Ephedrae Herba on Rats Model of Harmful Fluid Retention in Upper Jiao / 中国实验方剂学杂志

Objective: To study the effective substance foundation of Ephedrae Herba and explore its mechanism, in order to further enrich the theory of drug resistance of Ephedrae Herba.Method: In this experiment, a compound model was used to establish rat model of Harmful Fluid Retention in upper Jiao. The Rats were randomly divided into model group, captopril group (4.38 mg·kg-1), Ephedrae Herba decoction group(468 mg·kg-1), polysaccharide group (265.36 mg·kg-1), volatile oil group (2.34 mg·kg-1), alkaloid group(40.71 mg·kg-1) and phenolic acid group (210.60 mg·kg-1), and normal group (10 mL·kg-1). The normal group and the model group were given the same volume of normal saline for four weeks. The 24 h urine volume of rats was collected by metabolic cage method. The changes of heart and lung tissue morphology were observed under light microscope. The heart index, lung index, left ventricular ejection fraction(LVEF), left ventricular short axis shortening rate(LVFS) and pulmonary permeability index, number(LPI), lung dry-wet ratio(W/D), creatine kinase isoenzyme(CK-MB), angiotensin Ⅱ(Ang Ⅱ), aldosterone(ALD), cardiac aquaporin 1(AQP1), lung AQP1, aquaporin-3(AQP3) and kidney AQP1, aquaporin-2(AQP2), interleukin-6(IL-6) and tumor necrosis factor-α(TNF-α) change were detected.Result: Compared with the normal group, heart and lungs of the model group were significantly damaged. The amount of 24 h urine, LVEF, LVFS of model rats were significantly reduced(Pα were significantly increased(PPα were significantly increased (PPα were significantly reduced (PPConclusion: Alkaloid components "Wen" and "Xin" are the effective substance basis of its action. The mechanism may be related to the inhibition of renin angiotensin aldosterone system (RAAS) and the anti-inflammatory effect.

Caffeoyl quinic acids in Chrysanthemum morifolium improve LPS-induced HUVEC vascular endothelial cell injury by regulating ERK/MAPK signaling pathway / 药学学报

To explore the effect of total extract of Chrysanthemum morifolium on lipopolysaccharide (LPS)-induced acute lung injury in mice, we studied the effects of three caffeoyl quinic acids isolated from Chrysanthemum morifolium on vascular endothelial cell injury and their mechanisms of action. All animal experiments were carried out strictly in accordance with the National Animal Welfare Ethics and Protection Regulations. A mouse model of acute lung injury was established by intranasal instillation of LPS. After 6 days of oral administration of chrysanthemum extract, the lung wet weight/dry weight ratio, tumour necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β) were measured in mouse bronchoalveolar lavage fluid. Human umbilical vein endothelial cells (HUVEC) were serum starved for 12 h and treated with 2.5 μg·mL-1 LPS for 24 h to establish the in vitro model of vascular endothelial cell injury. After 24 h of treatment of caffeoyl quinic acids from Chrysanthemum morifolium, the levels of TNF-α, IL-6, IL-1β, vascular cell adhesion molecule-1 (VCAM-1) and endothelin-1 (ET-1) were measured by ELISA in the cell culture supernatant, the malondialdehyde (MDA) level was detected by TBA method, the superoxide dismutase (SOD) level was determined by hydroxylamine method, and the nitric oxide (NO) level was assayed by a one-step method. The levels of p-MEK1/2, MEK1/2, p-ERK1/2, ERK1/2, p-JNK, JNK, p-P38 and P38 of mitogen-activated protein kinase (MAPK) signaling pathway were detected by Western blot. The total extract of Chrysanthemum morifolium can significantly reduce the wet weight/dry weight ratio of lung in mice and the levels of TNF-α, IL-6 and IL-1β in alveolar lavage fluid. The caffeoyl quinic acids from Chrysanthemum morifolium significantly increased the levels of SOD and NO, decreased the levels of TNF-α, IL-6, IL-1β, VCAM-1, ET-1 and MDA, and significantly reduced the levels of p-MEK1/2, p-ERK1/2. In conclusion, total extracts of Chrysanthemum morifolium exhibit certain protective effect on mice with acute lung injury, and three caffeoyl quinic acids from Chrysanthemum morifolium may improve LPS-induced vascular endothelial cell injury by inhibiting inflammatory cytokines and oxidative stress, and regulating inter-cellular adhesion molecule and vasomotor factors through ERK/MAPK signaling pathway.

Evaluation of the estrogenic effects of rehmapicrogenin / 药学学报

This study offers preliminary insight into the phytoestrogen activity and mechanism of rehmapicrogenin. In this study, we characterized the estrogenic activity of rehmapicrogenin using immature female mice in vivo and MCF-7 cell proliferation assay in vitro. All the procedures for the care of the mice were conducted in accordance with the Regulations of Experimental Animal Administration issued by the State Committee of Science and Technology of the People’s Republic of China. Uterine wet weight/body mass ratios, Western blot assay for estrogen receptor, and serum estrogen levels of estradiol (E2), luteinizing hormone (LH) and follicle stimulating hormone (FSH) were investigated. The effects of rehmapicrogenin, and the estrogen receptor antagonist ICI182,780, the estrogen receptor alpha antagonist MPP, the estrogen receptor beta antagonist THC, the G-protein coupled receptor 30 antagonist G15 combined with rehmapicrogenin on cell proliferation were examined in MCF-7 cells. Rehmapicrogenin (50 mg·kg-1) treatments demonstrated significant estrogenic activity by promoting the development of uterus in immature female mice, as well as increasing the expression of estrogen receptor alpha (ERα) and G-protein coupled receptor 30 (GPR30) at the protein level in uterus, and decreasing FSH and LH compared with the control group. Meanwhile, rehmapicrogenin (6 and 8 μmol·L-1) promoted the proliferation of MCF-7 cells, which were significantly antagonized by ICI182,780, MPP and G15. This study demonstrates rehmapicrogenin exerts estrogenic effects through ERα and GPR30.

Metabolic study of Mori Cortex on nephrogenic edema in rats / 中成药

AIM To conduct a metabolic research for a better understanding of nephrogenic edema and to assess the integral efficacy of Mori Cortex in rat model.METHODS The serum creatinine,urea nitrogen,albumin and urinary protein levels in rats were detected.UPLC-QTOF-MS was used to detect the urine metabolites changes,Principal Component Analysis (PCA) and Orthogonal Partial Least Squares Discriminant Analysis (OPLS-DA)were used to screen potential biomarkers,after whose quantification,Mev software was adopted for heat map draw-ing and hierarchical cluster analysis.RESULTS The model rats manifested significantly increased levels of serum creatinine,urea nitrogen and urinary protein,decreased albumin level,and an obviously excessive amino acid metabolism as well.The 41 identified biomarkers were mainly related to disturbances in phenylalanine,pyrimidine,arginine and proline,glycine,serine and threonine,tryptophan,cysteine and methionine metabolism,and biosynthesis of pantothenic acid and coenzyme A.A reversal trend in aforementioned levels of biochemical indexes and most biomarkers due to the intervention by Mori Cortex signaled an improvement in the metabolic disorder,renal dysfunction and edema.CONCLUSION The metabolic study demonstrates the pathological status of nephrogenic edema and assesses the effect of Mori Cortex from an overall perspective,highlighting a new approach for illustrating Chinese medical syndrome and the underlying mechanism in the management of traditional Chinese medicine.

Comparison of the diuretic effects of Descurainiae Semen, Coicis Semen and Plantaginis Semen / 中成药

AIM To compare the diuretic effects of Descurainiae Semen (DS),Coicis Semen (CS) and Plantaginis Semen (PS),and to observe their mechanical similarities and differences.METHODS Metabolic cage method was applied to investigating the diuretic effects of DS (2.34 g/kg),CS (7.00 g/kg) and PS (3.50 g/kg),whose diuretic mechanisms were studied by cryoscopic method,enzyme method,ion selective electrode method,ELISA and Western blot.RESULTS DS,CS and PS obviously increased saline-loaded rats' urine volume (P ＜ 0.05) and reduced their body weight (P ＜ 0.05) after administration for 7 h,which exhibited no significant effects on urine creatinine (Ucr),serum creatinine (Scr) and blood urea nitrogen (BUN)(P ＞ 0.05).DS showed its diuretic effect mainly by lowering the levels of serum Na +,atrial natriuretic peptide (ANP),brain natriuretic peptide (BNP),pulmonary AQP3,renal AQP1 and AQP2;CS showed its diuretic effect mainly by reducing the levels of serum Na +,Cl-,ANP,pulmonary AQP3,gastric AQP3,renal AQP1 and AQP2;PS showed its diuretic effect mainly by decreasing the levels of serum Na + and Cl-,pulmonary AQP3,gastric AQP3,renal AQP1 and AQP2.CONCLUSION Three medicinal materials have significant diuretic effects without obvious renal harm.DS categorized as a medicinal plant of lung channel and tropism has a great effect on netriuretic peptide system,CS categorized as a medicinal plant of spleen channel and tropism has a great effect on gastric AQP3,and PS categorized as a medicinal plant of renal channel and tropism has a great effect on renal AQPs.

Evaluation of estrogenic effects of Semen Descurainiae and its action mechanism / 中国药理学通报

Aim To evaluate the estrogen-like activity of Semen Descurainiae aqueous extracts (SD-ae), to deter-mine its effective chemical separation components and to study the mechanisms. Methods The estrogen-like ac-tivity of SD-ae and its effective chemical separation com-ponents were evaluated by the animal experiment, uterine weight test and cell experiment, namely E-SCREEN ex-periment. Estrogen receptor antagonist ICI182,780 inter-vention blocking experiment was carried out to detect the pathway of estrogen-like action; the HEK293 cells were co-transfected with the report gene carrier and the ERα, ERβ expression vector by cationic liposome, the report gene carrier was constructed via the estrogen-responsive component (ERE) and the report gene luciferase (Luc), then the estrogen-like signaling pathway was evaluated with standardized Luc activity; the expression of estrogen receptor ERα, ERβ and estrogen-induced gene PR mR-NA was detected by real-time fluorescence quantitative PCR. Results Compared with normal control, SD-ae low and high dose could significantly improve the uterine coefficient of immature female mice(P<0.05), and the oligosaccharides composition of Semen Descurainiae aque-ous extracts(SD-ae-Oli) and the polysaccharide composi-tion of Semen Descurainiae aqueous extracts(SD-ae-Pol) also significantly improved the uterine coefficient of im-mature female mice (P<0.01 or P<0.05); SD-ae, SD-ae-Oli and SD-ae-Pol had a significant proliferative effect on MCF-7 cells ( P <0.01 or P <0.05), while ICI182,780 intervened to block its proliferative effect. The reporter gene technology showed that the standardized Luc activities of SD-ae, SD-ae-Oli and SD-ae-Pol were significantly higher than those of the normal control when they were induced by ERβ respectively (P<0.01); and the SD-ae significantly increased the expression of ERβ mRNA in mouse uterus than the normal control, but no effect was found on the expression of ERα and PR mR- NA. Conclusions The estrogenic effect of SD-ae may be found at the first time, and its effective chemical sepa-ration components are SD-ae-Oli and SD-ae-Pol. Their estrogenic effects are mediated by ERβ. The molecular mechanism of the estrogenic effects is probably that SD-ae promotes the expression of ERβ mRNA.

Clinical effect and cost analysis of panretinal photocoagulation combined with Ranibizumab or triamcinolone acetonide for diabetic macular edema / 国际眼科杂志(Guoji Yanke Zazhi)

·AIM: To compare clinical effects and cost of panretinal photocoagulation (PRP) combined with Ranibizumab or triamcinolone acetonide (TA) for diabetic macular edema (DME). ·METHODS: Forty-eight patients (48 eyes) with DME and diabetic retinopathy ( DR) receiving PRP were randomly assigned to two groups, which were respectively intravitreally injected ranibizumab (0. 5mg) and TA (4mg). Ranibizumab (0.5mg) was intravitreal injected every 4wk for 3 times. The effects of injection for DME were evaluated using best-corrected visual acuity (BCVA ), central macular thickness ( CMT ) and intraocular pressure (IOP). During the follow-up, other injections were performed to eyes which had CMT greater than 400μ m. The medical costs were calculated at 12wk and 24wk.·RESULTS: BCVA and CMT between 2 groups were not significantly different (P>0.05); BCVA and CMT among different time points were significantly different(P<0.05);the treatments and the time points had significant interaction on BCVA (P<0.05). BCVA was improved in two groups at all the time after injection(P<0.05),except 1wk after injection of TA (P=0.33). There was significant difference between the two groups at 12wk and 16wk on BCVA and that injected with ranibizumab was better (P=0.03,0.045). CMT decreased in two groups at all the time after injection (P<0.05). There was significant difference only between the two groups at 1wk (P< 0. 01). All intraocular pressures were in the normal range, except one needed ocular hypotensive agents. The medical costs (yuan) of the ranibizumab group in 12wk and 24wk were 38 736 and 42 564,which of the TA group were 5 790 and 7 053,respectively. ·CONCLUSION:Both PRP combined with ranibizumab or TA for DME can effectively control disease progression in short time. Therapeutic effect is not significant between two methods, but PRP combined with TA is more economic.

A new indole alkaloid from bulbils of Dioscorea opposite Thunb / 药学学报

This study was designed to study the chemical constituents from bulbil of Dioscorea opposite Thunb.. Four compounds were isolated by silica gel column chromatography. On the basis of physic-chemical characters and spectroscopic data analysis, these compounds were identified as lyzalkaloid (3,4-dihydro-6-hydroxy-4-methyl-6H-pyrido[6,5-b]indol-5(1H)-one) (1), anoectochine (2), ginsenine (3), and 2-hydroxy-3-(1H-indol-3-yl) propanoic acid methyl ester (4). Compound 1 is a new indole alkaloid, named as lyzalkaloid. Compounds 2-4 were isolated from this plant for the first time. The cytotoxic activities were assessed by MTT assay. All compounds exhibited the cytotoxic activity against HepG2 and MDA-231 with IC50 values of over 100 μmol·L-1, respectively. All compounds show no significant cytotoxic activities against HepG2, MDA-231 cancer cell.

Chaenomelesalkaloid A, a new alkaloid from the fruits of Chaenomeles sinensis (Thouin) Koehne / 药学学报

The chemical constituents of the fruits of Chaenomeles sinensis (Thouin) Koehne were investigated using chromatographic methods, including Diaion HP-20, Toyopearl HW-40, MCI Gel CHP-20, ODS, Silica gel chromatography and semi-preparative-HPLC. Three compounds were isolated and their structures were elucidated with spectral data and physicochemical properties, which were identified as chaenomeles alkaloid A (1), ginsenine (2) and 1,2,3,4-tetrahydro-1-methyl-β-carboline-3-car-boxylic acid (3). Among those, compound 1 is a new alkaloid, compound 2 and 3 were isolated from this plant for the first time. To investigate the protective effect of compounds 1-3 on Rat adrenal pheochromocytoma (PC-12) injury induced by the β-amyloid protein (Aβ25-35). The results show that compounds 2 and 3 have a significant protective effect on the PC12 cells exposed to Aβ25-35.

Estrogen-like effect of allantoin / 药学学报

The study was designed to test the estrogen-like effects about allantoin. The activity of the allantoin was investigated by mouse uterine weight gain test and MCF-7 cell proliferation assay. The levels of E2, FSH and LH were also measured. ICI182,780, MPP, THC and G15 antagonnist assay and Western blot were adopted to explore the mechanism of allantoin. Allantoin increased the uterus index of premature female mice, the levels of E2 and FSH, and the expression of ERα and GPR30, compared with the control group. Allantoin also promoted the proliferation of MCF-7 cells. Co-incubation of MCF-7 cells with estrogen receptor blockers, ICI182,780, MPP and G15 abolished the inductive effect of the proliferation. These results suggest that allantoin has estrogenic activities, which are mainly mediated by ERα, GPR30.