AIM: To investigate the mechanism of proliferation effect induced by (R,R)-XY-10 and (S,S)-XY-10 on retinal pigmented epithelial cells(ARPE-19).METHODS: Human retinal pigmented epithelial cells(ARPE-19) and human umbilical vein endothelial cells (HUVECs) were used to investigate the effect of (R,R)-XY-10 and (S,S)-XY-10 on cell growth,and their mechanisms of proliferative action by using ERK、 AKT、PI3K、Protein kinase C (PKC)and Nitric oxide synthase (NOS) inhibitors.RESULTS: (R,R)-XY-10 and (S,S)-XY-10 dose-dependently increased ARPE-19 cell proliferation,but not on HUVECs. When treated with proliferative inhibitors,H7(5μmol/L)、hypericin(20μmol/L)、PD98059(2μmol/L)、LY294002(50μmol/L)、SH-5 (10μmol/L) and L-NAME (100μmol/L),the proliferative effect was reduced by H7、hypericin、PD98059 and LY294002,but not by SH-5 and L-NAME.CONCLUSION: (R,R)-XY-10 and (S,S)-XY-10 can induce cell proliferation through MAPK and PI3K dependent pathway. KEYWORDS: age-related macular degeneration; (R,R)-XY-10; (S,S)-XY-10; ARPE-19 cells; human umbilical vein endothelial cells; proliferation

OBJECTIVETo explore the efficacy differences in early intervention of different acupuncture and moxibustion methods on gastrocnemius fatigue in rats induced by electrical stimulation.

METHODSFifty male SD rats were randomly divided into a control group, a model group, a hand acupuncture group, an electroacupuncture group and a moxibustion group, 10 rats in each group. Electrical stimulation of the sciatic nerve was given in the control group and gastrocnemius fatigue test was induced by electrical stimulation of the sciatic nerve in the model group after anesthesia without other treatment, but just take 6 times interval stimulation in the control group. The hand acupuncture group, the electroacupuncture group and the moxibustion group were treated with the corresponding acupoints stimulation method respectively for 20 min before gastrocnemius fatigue test, and Dazhui (GV 14) and Zusanli (ST 36) were selected. Immediately after gastrocnemius fatigue test, three or four gastrocnemius tissues at the same site on the right side were quickly taken for making specimen for transmission electron microscope (TEM). The changes of skeletal muscle ultrastructure of myofibrils, mitochondria, sarcoplasmic reticulum, glycogen particles were observed under TEM.

RESULTS(1) Muscle fibers disorder, partial mitochondrial vacuolization and glycogen particles smaller were shown in the model group. (2) No abnormalities were shown in the hand acupuncture group and the moxibustion group with mitochondrial morphology and number, which better than that in the model group, and glycogen particles increased. (3) Abnormal changes in morphology were shown in the electroacupuncture group with part of the muscle fibers derangement, Z line malalignment and a few mitochondria vacuolization.

CONCLUSIONHand acupuncture, electroacupuncture and moxibustion have the different effects on ultrastructure of gastrocoemius in rats. Acupuncture and moxibustion have shown good effects on the prevention and treatment of exercise-induced skeletal muscle cell and organelle damage and delaying exercise-induced fatigue.

Acupuncture Points ; Acupuncture Therapy ; Animals ; Glycogen ; metabolism ; Male ; Mitochondria ; metabolism ; ultrastructure ; Moxibustion ; Muscle, Skeletal ; metabolism ; ultrastructure ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo analyze LC-MS fingerprints of Aristolochia manshuriensis for quality assessment with two different chemical pattern recognition models.

METHODLC-MS fingerprints of A. manshuriensis were established from 24 batches of samples from different habitats. SIMCA and Clustering analysis were used to compare the parameters of the 29 common peaks.

RESULTTwo methods had good consistency, while they reflected the inherent sample information from different perspectives, respectively.

CONCLUSIONModern equipment analysis technology and multivariable chemical pattern recognition would be an efficient way for quality control and variety identification of A. manshuriensis.

Aristolochia ; chemistry ; classification ; Chromatography, Liquid ; Cluster Analysis ; Drugs, Chinese Herbal ; chemistry ; Mass Spectrometry ; Phylogeny ; Quality Control

Objective To evaluate the clinical effect and safety of salvia miltiorrhiza polyphenols in the treatment of coronary atherosclerotic heart disease.Methods Sixty -six patients with coronary atherosclerotic heart disease were randomly divided into experiment group ( n=32 ) and control group ( n=34 ).Patients in experiment group were treated with salvia miltiorrhiza polyphenols 200 mg+0.9%NaCl 250 mL, intravenous drip, qd for 2 weeks;patients in control group treated with salvia injec-tion 30 mL+0.9%NaCl 250 mL, intravenous drip, qd for 2 weeks.The total amount of exercise metabolic , exercise-induced angina onset time , exercise-induced low pressure of 1 mm ST-off time, angina attacks, clinical efficiency and adverse drug reaction of the two groups were observed.Results Total efficacy was 87.50% in experiment group , significantly higher than 61.76% in control group ( P <0.05 ).The clinical index of the two groups were significantly improved after treatment ( P <0.05 ).The dosage of nitroglycerin and incidence of angina pectoris in experiment were significant lower than those of control group ( P<0.05 ).The incidence rate of adverse reactions had no statisti-cal difference ( 6.25% vs 8.82%, P >0.05 ).Conclusion Salviamiltiorrhiza polyphenols in the treatment of coronary atherosclerotic heart disease was effective and safe , which can re-duce the angina attacks.

OBJECTIVETo investigate flap survival after transfection using gene encoding vascular endothelial growth factor (VEGF).

METHODSIn 30 Sprague-Dawley rats, the anterior abdominal skin flap supplied by the epigastric vessels was created. The animals were divided into three groups, with ten of each. The first group was treated with a mixture of liposomes and the cDNA encoding the 165-amino acid isoform of VEGF; the second group was treated with control blank plasmid DNA and liposome transfection medium; the third group was treated with physiological saline. Four days after injection, the epigastric artery and vein were ligated and the blood flow in the flap was evaluated by intraperitoneal injection of fluorescence solution. Seven days later, the survival area of the flap was measured by planimetry. After the animals were killed, specimens were harvested from the anterior abdomen skin flap for immunohistological evidence of VEGF expression and for hematoxylin and eosin staining of microvascular growth.

RESULTS30 minutes after pedicle ligation the average fluorescence staining planimetry of the three groups (PCD-VEGF165, PCD and physiological saline) was 60.64%, 30.15% and 29.89% respectively. Tissue survival planimetry of the three groups was 92.3%, 30.5%, 31.8%. There was significant difference between the first group and the latter two (P < 0.05). Immunohistochemical staining documented increased deposition of VEGF cDNA in the first group compared to the control groups (P < 0.05). Normal staining documented that the average vessel number of the three groups was 101.72, 91.35 and 89.85 (P < 0.05), the average vessel lumen diameter was 26 microns, 31.09 microns and 32.51 microns(P < 0.05).

CONCLUSIONThrough administration, PCD-VEGF165 can transfect the anterior abdominal skin flap and enhance its survival. There was express of VEGF protein in the treated flap.

Animals ; Biomarkers ; metabolism ; DNA, Complementary ; administration & dosage ; Epigastric Arteries ; Genetic Therapy ; Graft Survival ; physiology ; Liposomes ; Plasmids ; Rats ; Rats, Sprague-Dawley ; Surgical Flaps ; blood supply ; physiology ; Time Factors ; Transfection ; methods ; Vascular Endothelial Growth Factor A ; genetics ; metabolism

AIMTo search for new derivatives of diclofenac (DC) having higher potency than the parent drug and lacking its undesirable effects.

METHODSCoupling DC with NO donor 3-hydroxymethyl-4-phenylfuroxan and its isomer through esterification, evaluating anti-inflammatory and analgesic activities, observing side effects in the rat gastrointestinal (GI) tract and assessing NO releasing ability both in vitro and in vivo.

RESULTSFifteen new compounds including nine target ones (II1-9) were synthesized, and their structures were determined by IR, 1HNMR, MS and elemental analysis. Compounds II3 and II9 showed anti-inflammatory activity comparable to DC. Compound II2 showed stronger anti-inflammatory and analgesic activities and less GI side effect than DC, and released NO in vivo.

CONCLUSIONCompound II2 is worthy to be intensively studied.

Analgesics ; chemical synthesis ; pharmacology ; therapeutic use ; Animals ; Anti-Inflammatory Agents, Non-Steroidal ; chemical synthesis ; pharmacology ; therapeutic use ; Cyclic N-Oxides ; administration & dosage ; chemistry ; pharmacology ; Diclofenac ; chemical synthesis ; pharmacology ; therapeutic use ; Digestive System ; drug effects ; Edema ; drug therapy ; Gastrointestinal Hemorrhage ; chemically induced ; Mice ; Molecular Structure ; Nitric Oxide ; metabolism ; Nitric Oxide Donors ; chemistry ; pharmacology ; Oxadiazoles ; administration & dosage ; chemistry ; pharmacology ; Pain Threshold ; drug effects ; Rats ; Structure-Activity Relationship

OBJECTIVETo investigate the inhibitory effect of lactic acid on semen-derived amyloid (SEVI) fibril formation.

METHODSPAP248-286 (2 mg/mL) was incubated with 4.0, 2.0, 1.0, 0.5, 0.25, and 0.125 mg/mL of lactic acid. After incubation for different times, aliquots were drawn from each sample for Thioflavin T (ThT) and Congo red staining to monitor semen-derived amyloid fibril formation. The β sheet structure formation of PAP248-286 was measured by circular dichroism spectrum, and the morphology of amyloid fibrils incubated with or without lactic acid was observed with transmission electron microscopy (TEM). The enhancing effect of amyloid fibril incubated with lactic acid at different time points was determined using virus infection assay. PAP248-286 (2 mg/mL) was incubated with dilutions of vaginal secretion from healthy women, and amyloid fibril formation was detected with ThT and Congo red staining.

RESULTSLactic acid inhibited SEVI fibril formation in a dose-dependent manner in vitro. Lactic acid at 0.5 mg/mL completely inhibited 2 mg/mL SEVI fibril formation within 48 h. After incubation for 48 h, lactic acid at 1 mg/mL inhibited the formation of β-sheet structure of SEVI (2 mg/mL) and completely inhibited 2 mg/mL PAP248-286 aggregation as observed with TEM. In the presence of lactic acid, PAP248-286 lost the ability to enhance virus infection. Vaginal secretion inhibited SEVI fibril formation in a dose-dependent manner, and virtually no SEVI fibril occurred after incubation of 2 mg/mL PAP248-286 with 67% vaginal secretion.

CONCLUSIONLactic acid inhibits SEVI fibril formation in vitro.

China ; epidemiology ; Cross-Sectional Studies ; Female ; Hospitalization ; Humans ; Infusions, Intravenous ; statistics & numerical data ; Male

Using the absorbent resin, silica gel and ODS column chromatography as well as semi-preparative HPLC, ten compounds were isolated from 70% ethanol extract of tubers of Dioscorea zingiberensis C. H. Wright, and their structures were elucidated as trigoneoside XIIIa (1), parvifloside (2), trigoneoside IVa (3), deltoside (4), protobioside (5), lilioglycoside k (6), zingiberensis newsaponin I (7), deltonin (8), prosapogenin A of dioscin (9), and trillin (10) on the basis of NMR and MS spectral data analysis. Among these compounds, 1, 3, 5 and 6 were isolated from this plant for the first time. In the screening test on platelet aggregation, compounds 7 and 8 exhibited induction effect on platelet aggregation, while compound 9 exhibited significant inhibitory effect on platelet aggregation in vitro.
Animals ; Dioscorea ; chemistry ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Male ; Mass Spectrometry ; Molecular Structure ; Platelet Aggregation ; drug effects ; Rats ; Rats, Wistar ; Saponins ; chemistry ; pharmacology

AIMTo study the structure and crystal forms of chlorobenzylidine.

METHODSKarl Fischer titrimetry, FTIR, thermal analysis, single and powder X-ray diffraction were used for the studies of the structure of chlorobenzylidine and for the identification of two forms of chlorobenzylidine.

RESULTSChlorobenzylidine and its diastereoisomer have been studied in this article. They can be distinguished by their different melting points. Two crystal forms of chlorobenzylidine (form A and form B) have also been detected and studied. Form A was studied by single-crystal X-ray diffraction, it crystallized in the triclinic system, space group P1(-), with two formula units per cell, is monohydrate. Karl Fischer titrimetry, FTIR, thermal analysis and powder X-ray diffraction were used for identification of the two forms.

CONCLUSIONThe studies of structure and crystal forms of chlorobenzylidine are very useful for the clinical research and the selection of recrystallization process.

Benzylidene Compounds ; Crystallization ; Crystallography, X-Ray ; Differential Thermal Analysis ; Molecular Conformation ; Molecular Structure ; Polycyclic Compounds ; chemistry ; Stereoisomerism