The present work is to investigate the chemical constitutions of Hyptis rhomboidea and their antifungal activities. The compounds were isolated by Toyopearl HW-40, Sephadex LH-20, MCI-Gel CHP-20, RP-18, PTLC and silica column chromatographic methods and subjected to evaluate some monomers antifungal activity of eight kinds of plant pathogenic bacteria. Eleven compounds were isolated and identified as ethyl caffeate (1), ursolic acid (2), oleanolic acid (3), vanillactic acid (4), methyl rosmarinate (5), kaempferol 3-O-alpha-L-rhamnopyranosyl-(1 --> 6) -beta-D-glucopyranoside (6), kaempferol 3-O-alpha-L-rhamnopyranosyl-(1 --> 6)-beta-D-glucopyranoside (7), ilexgenin A (8), beta-amyrin (9), kaempferol 3-O-beta-D-glucopyranoside (astrgalin, 10) and cholest-5-ene-3beta, 4beta-diol (11). Compound 1 showed the strongest inhibitory effect on Sclerotinia sclerotiorum with the MIC 16.2 mg x L(-1), and compound 5 showed the strongest inhibitory effect on S. minor and Exserohilum turcicum with MIC 16.2, 8.1 mg x L(-1), respectively. All compounds were isolated from the H. rhomboidea for the first time, and compounds 1 and 5 showed antifungal activity.
Antifungal Agents ; chemistry ; isolation & purification ; pharmacology ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; Fungi ; drug effects ; Hyptis ; chemistry ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization

Objective To determine the incidence and risk factors of retinopathy of prematurity (ROP) in preterm infants.Methods Fundus examinations were performed by RetCam Ⅱ ophthalmoscopy on 2185 premature infants (birth weight ≤ 2000 g or gestational age≤34 weeks)admitted into the neonatal intensive care unit of Beijing Bayi Children's Hospital from January 1st 2009 to December 31st 2010.According to the results,all infants were divided into ROP group and nonRO P group.Two-sample t test and Logistic regression analysis were used to investigate the risk factors of ROP.Results Among 2185 premature infants,287 (13.1 ％) cases were diagnosed with RO P.According to International Classification of RO P,34 cases (11.9 ％) were in zone Ⅰ,147 cases (51.2％) in zone Ⅱ,and 106 cases(36.9％) in zone Ⅲ.And there were 117 cases (40.8％) with stage 1 lesion,142 cases (49.5％) with stage 2 lesion,28 cases (9.7％) with stage 3 lesion,and no stage 4 or 5 lesion was identified.Thirty-six cases (12.5 ％) were accompanied by additional diseases.Logistic analysis showed that small gestational age (OR=0.859,95％CI:0.770-0.958,P=0.006),low birth weight (OR=0.729,95％CI:0.6340.838,P=0.000),long duration of oxygen supplement (OR=2.221,95％CI:1.904-2.592,P=0.000),assistant ventilation (OR=3.104,95％CI:2.0964.956,P=0.000),apnea (OR=1.767,95％CI:1.103 2.831,P=0.018) and=anemia (OR=2.242,95％CI:1.641-3.604,P=0.000) were independent risk factors of ROP.Conclusions The incidence of ROP in premature infants is high.Small gestational age and low birth weight,long duration of oxygen supplement,assistant ventilation,apnea and anemia are risk factors of ROP.Preventive measures should be taken against these factors.

This study was to investigate the permeability and absorbability of capsaicin cubosome across abdominal skin of the SD rats in vitro. Diffusion of capsaicin cubosome and cream was performed with the modified Franz diffusion cell technique. The capsaicin cubosome showed no enhancement of skin permeation within 24 hours. However, the deposition amounts of capsaicin in the rat skin in the cubosome group was markedly higher than those in the commercial cream group (P < 0.01). Cubosome showed excellent characetristic of skin-targed which could be a good carrier for the local transdermal drug delivery system.
Administration, Cutaneous ; Animals ; Capsaicin ; administration & dosage ; chemistry ; Kinetics ; Male ; Particle Size ; Permeability ; Rats ; Rats, Sprague-Dawley ; Skin ; drug effects ; metabolism ; Skin Absorption

Animals ; Brain ; drug effects ; metabolism ; Carbon Dioxide ; metabolism ; Chronic Disease ; Curcumin ; pharmacology ; Disease Models, Animal ; Fas Ligand Protein ; metabolism ; Hypoxia ; metabolism ; Male ; Oxygen ; metabolism ; Rats ; Rats, Sprague-Dawley ; fas Receptor ; metabolism

OBJECTIVETo explore the regulatory role of protein kinase A (PKA) in platelet surface glycoprotein (GP) I balpha expression.

METHODSWashed platelets from healthy volunteers were incubated with PKA inhibitor. The N-terminal fragment of GP I balpha (glycocalicin, GC) in the supernatant of platelet suspensions was detected by Western blot and GP I balpha surface expression by flow cytometry. Calpain activity was determined by cytoskeletal proteins proteolysis and calpain surface expression by flow cytometry. The effect of PKA inhibitor on ristocetin-induced platelet aggregation was measured by platelet aggregometer.

RESULTSAfter PKA was inhibited in washed platelets, GP I balpha was cleaved and released to the supernatant, which significantly decreased the surface expression of GP I balpha (P < 0.05). The event was suppressed by pre-treatment with various calpain inhibitors, indicating that PKA inhibitor-mediated shedding was calpain dependent. The actin-binding protein (ABP) and talin proteolysis demonstrated that calpain was activated by PKA inhibitor and expressed on the platelet membrane. Ristocetin-induced aggregation was inhibited by PKA inhibitor.

CONCLUSIONPKA inhibition results in calpain-dependent GP I balpha shedding, which thus reduces GP I balpha surface expression and GP I balpha-dependent platelet aggregation. These results might provide a view to develop new drugs for thrombotic diseases.

Blood Platelets ; drug effects ; Calpain ; metabolism ; Cyclic AMP-Dependent Protein Kinases ; antagonists & inhibitors ; Flow Cytometry ; Humans ; Platelet Aggregation ; drug effects ; Platelet Aggregation Inhibitors ; pharmacology ; Platelet Glycoprotein GPIb-IX Complex ; biosynthesis

Objective To analyze the clinical profile and short-term postoperative prognosis of mixed hepatocellular carcinoma and cholangiocarcinoma (mHCC-CC). Methods Clinical data of 17 mHCC-CC cases undergoing hepatectomy were retrospectively analyzed. Results Patients average age was 53 years (27～76 years).There were 11 males (64.7％) and 6 females.Ten patients (58.8％) were asymptomatic,twelve patients(70.6％ ) had positive serology for hepatitis B infection,serum AFP levels ＞25 ng/ml in 12 cases. Serum CA199 levels ≥ 37 U/ml in 4 cases. All patients underwent radical hepatectomy,including ＞ 1.5 cm safe margin and lymphadenectomy.The 6-,12-,and 18-months overall survival rate was 93.8％,86.5％ and 57.7％,respectively.The 100- and 200-day disease-free survival was 65.3％ and 43.5％.The median disease-free survival was 161 days. Conclusions mHCC-CC is difficult to diagnose preoperatively.The diagnosis depends on pathological examination.The main treatment was surgical resection.The prognosis of mixed primary liver cancer is poor and tends to recur early after hepatectomy.

Objective To explore the expression of HCK gene during the cardiomyocyte differentiation of mouse embryonic stem cells and analyze the role of HCK gene in maintenance of pluripotency of embryonic stem cells.Methods Mouse embryonic stem cells were cultured,then induced to differentiate into cardiomyocytes.Total RNAs were isolated from mouse embryonic stem cells in the differentiation days:0 day(D0),the second day(D2),the fourth day(D4),the sixth day(D6),the eighth day(D8),respectively.The levels of HCK mRNAs were assessed by the method of semi-quantitive reverse transcriptase-polymerase chain reaction(RT-PCR).In the meanwhile,Total proteins were also isolated from mouse embryonic stem cells in the differentiation D0,D2,D4,D6,D8,and the levels of HCK proteins were evaluated by Western-blot.Results HCK mRNAs could be detected in the mouse embryonic stem cells in D0 and D2,however,they were undetectable from D4 to D8.The expression of HCK mRNAs was rapidly down-regulated during cardiomyocyte differentiation of mouse embryonic stem cells.Expression of HCK proteins,which coincided with HCK mRNAs,down-regulated during differentiation and couldn't be detected in D4.Conclusions With the cardiomyocyte differentiation of mouse embryonic stem cells,the expression of HCK in the levels of mRNA and proteins are sharply down-regulated;HCK may play an important role in maintaining the pluripotency of embryonic stem cell.

Objective To compare the prophylactic efficacy of combination of ganciclovir and acy- clovir or acyclovir alone against cytomegalovirus pneumonia in renal transplant recipients.Methods A to- tal of 217 renal transplant recipient(124 men and 93 women;mean age,32 years;age range,16-72 years) were divided into 3 groups randomly.In 51 cases,acyclovir was taken orally at a dose of 400 mg,3/d,from the third d to 3 months after transplantation.In 74 cases,ganciclovir was administered at a dose of 250 mg/d intravenously from the 21st d to 27th d to replace Acyclovir.In 92 cases,no prophylaxis against eytomegalov- irus pneumonia was performed.All patients were followed 3 months after transplantation.Comparison of the incidence rates of cytomegalovirus pneumonia among the 3 groups was performed using Fisher's exact test. Results Cytomegalovirus pneumonia developed in 20 cases in the 3 groups,including 4 cases(5.4%) in combined use group,2 cases(3.9%)in acyclovir alone group,and 14 cases(15.2%)in control group. Significant difference existed between the 2 experimental and control groups(P＜0.05).However,no signifi- cant difference existed between the 2 experimental groups(P＞0.05).Of the 20 cases,17(85.0%)were cured,and 3 died of respiratory failure.Conclusions Ganciclovir and acyclovir have prophylactic effect a- gainst cytomegalovirus pneumonia in renal transplant recipients.These 2 medications are inexpensive,and the patients have good compliance.

OBJECTIVE: To explore the therapeutic efficacy of manual reduction combined with percutaneous vertebroplasty in treating osteoporotic vertebral compression fractures(OVCFs) with intravertebral clefts. METHODS: The clinical data of 94 patients with osteoporotic vertebral compression fractures with intravertebral clefts treated from January 2014 to January 2017 were retrospectively analyzed. The patients were divided into group A and group B according to different operative methods. In group A, 45 patients were treated with unilateral approach PVP, including 17 males and 28 females, aged (75.35±11.82) years old, with a bone density T-value of (-4.28±0.65) g/cm³; in group B, 49 patients treated with manual reduction combined with unilateral approach PVP, including 19 males and 30 females, aged (76.79±9.64) years old, with a bone density T-value of (-4.33±0.72) g/cm³. The operation time, bone cement injection volume and postoperative complications of two groups were recorded. The VAS and ODI scores of two groups were analyzed respectively at 1, 12, 18 months after operation. Vertebral height and kyphosis Cobb angle of two groups were compared immediately after surgery and 12, 18 months after operation. The distribution of bone cement in the vertebral body was observed and its distribution excellent rate was calculated. RESULTS: There was no significant difference in operation time between two groups. The amount of bone cement injection was(8.42±1.24) ml in group A and(9.19±1.09) ml in group B, and the difference between two groups was statistically significant(<0.05). No spinal nerve root injury during operation and no complications including pulmonary embolism, bone cement toxicity and infection were found in two groups. There were 5 cases of bone cement leakage in group A and 4 cases in group B, which did not cause corresponding clinical symptoms and were not treated additionally. The distribution of bone cement in group A was excellent in 25 cases, good in 19 cases, poor in 1 case and in group B was excellent in 45 cases, good in 4 cases. The distribution excellent rate of bone cement was higher in group B than in group A (<0.05). The VAS and ODI scores before operation and 1, 12, 18 months after operation were 8.29±0.74, 2.59±0.14, 3.75±0.38, 3.84±0.88 and 40.04±3.16, 9.24±2.82, 12.27±2.64, 15.83±2.58 in group A, 8.22±0.82, 2.54±0.19, 2.81±0.23, 2.82±0.45 and 39.98±2.05, 9.16±2.10, 9.46±2.41, 9.76±2.46 in group B. There was no significant difference in VAS and ODI scores at 1 month after operation between two groups (>0.05), but group A was higher than group B at 12 and 18 months after operation (<0.05). The vertebral height and Cobb angle before surgery, immediately after surgery, and 12, 18 months after surgery in group A were(59.17±1.42)%, (85.95±2.19)%, (75.27±3.45)%, (68.34±2.24)% and(23.83±3.37)°, (15.26±2.61)°, (17.63±2.16)°, (19.46±2.54)°, and in group B were(59.31±1.87)%, (89.19±2.53)%, (88.62±2.51)%, (88.59±2.62)% and(24.72±3.78)°, (14.91±2.28)°, (15.48±2.55)°, (15.86±2.81)°. Vertebral height Immediately after surgery was greater in group B than in group A and Cobb angle in group B was smaller than in group A (<0.05). During follow-up, there was no significant change in vertebral height in group B, while vertebral body recollapse in group A(<0.05). CONCLUSIONS In the treatment of osteoporotic vertebral compression fractures with intravertebral clefts, the manual reduction combined with PVP is more effective than single PVP, which can effectively prevent vertebral body recollapse and improve the long-term efficacy of patients.
Aged ; Aged, 80 and over ; Bone Cements ; Female ; Fractures, Compression ; Humans ; Male ; Middle Aged ; Osteoporotic Fractures ; Retrospective Studies ; Spinal Fractures ; Treatment Outcome ; Vertebroplasty

OBJECTIVETo investigate the protective effects of the natural medicinal monomer isopsoralen (ISR) with estrogenic activity against oxidative damage in human lens epithelial cells B3 (HLE-B3) caused by hydrogen peroxide (H(2)O(2)) and to pursue the possible mitochondrial proteomic regularity of the protective effects.

METHODSHLE-B3 cells were treated with H(2)O(2) (300 μ mol/L), β-estradiol (E(2): 10(-8) mol/L) and H(2)O(2), ISR (10(-5) mol/L) and H(2)O(2), or left untreated. Altered expressions of all mitochondrial proteins were analyzed by protein array and surfaceenhanced laser desorption ionization time of flight mass spectrometry (SELDI-TOF-MS). The mass/charge (m/z) ratios of each peak were tested by the Kruskal-Wallis rank sum test, and the protein peak value of the m/z ratio for each treatment by pair comparison was analyzed with the Nemenyi test.

RESULTSH(2)O(2) up-regulated the expressions of two protein spots (with m/z of 6532 and 6809). E(2) mitigated the oxidative damage, and the expression of one protein spot (m/z 6532) was down-regulated. In contrast, ISR down-regulated both of protein spots (m/z 6532 and 6809).

CONCLUSIONSISR could effectively inhibit H(2)O(2)-induced oxidative damage in HLE-B3 cells. The protein spot at m/z of 6532 might be the target spot of ISR against oxidative damage induced by H(2)O(2).

Cell Line ; Epithelial Cells ; drug effects ; metabolism ; pathology ; Estradiol ; pharmacology ; Furocoumarins ; pharmacology ; Humans ; Hydrogen Peroxide ; toxicity ; Lens, Crystalline ; pathology ; Mitochondria ; metabolism ; Oxidation-Reduction ; drug effects ; Oxidative Stress ; drug effects ; Protective Agents ; pharmacology ; Proteome ; metabolism ; Proteomics ; methods