Objective To study the chemical constituents of aerial parts of Dianbaizhu (Gaultheria leucocarpa var. crenulata).Methods The various techniques of column chromatograph were used in the course of isolation and purification. The chemical structure of the compounds was analysed and identified by using mass spectrography (MS) and nuclear magnetic resonance spectroscopy (NMR).Results There were 7 compounds isolated and identified as ①quercetin-3-O-β-D-glucuronide, ②kaempferol-3-O-β-D-glucuronide,③ methyl gentisate, ④methyl salicylate,⑤ gaultherin,⑥ gaultherins A and ⑦gaultherins B. Conclusion The compounds of 1 to 3 are isolated from Dianbaizhu for the first time.

BACKGROUNDDepot medroxyprogesterone acetate (DMPA) as a hormonal contraceptive is highly effective and widely used, but it may reduce bone mineral density (BMD) and increase the risk of osteoporosis. We compared BMD between users of intramuscular DMPA and nonhormonal subjects.

METHODSThe study included 102 women aged between 16 and 18 years using DMPA for 24 months and 97 women aged between 16 and 18 years using nonhormonal contraception as nonusers control group. BMD of the lumbar spine and femoral neck was measured every 12 months for 24 months using dual-energy X-ray absorptiometry, comparing mean BMD changes in DMPA users and nonusers.

RESULTSThere were no significant differences between groups at baseline in age, gynecologic age, body mass index (BMI), lumbar spine BMD and femoral neck BMD, etc. At 24 months of DMPA treatment, the mean percentage change from baseline in lumbar spine and femoral neck BMD values had decreased by 1.88% and 2.32%, respectively. The mean lumbar spine and femoral neck BMD in DMPA group at 24 months were not significantly different compared to baseline (P = 0.212 and P = 0.106, respectively). In comparison, in nonhormonal control group, there was a trend toward increasing BMD. At 24 months of observation, the mean percentage change from baseline in lumbar spine and femoral neck BMD had increased by 2.08% and 1.46%, respectively. There were no significant difference compared to baseline (P = 0.160 and P = 0.288, respectively). Mean BMD at the spine and femoral neck did not differ significantly between DMPA users and nonusers over 12-month, but the BMD values at both anatomical sites were significantly lower in DMPA users compared with nonusers after 24-month treatment (P = 0.009 and P = 0.009, respectively).

CONCLUSIONThe evidence of our study suggested that the use of DMPA for short-term (≤12-month) has no significant effects on BMD at spine and femoral neck, but long-term exposure to DMPA may prevent the bone mass accrual in adolescents.

Adolescent ; Bone Density ; drug effects ; Contraceptive Agents, Female ; pharmacology ; Female ; Humans ; Medroxyprogesterone Acetate ; pharmacology

Objective To investigate the protective effect of dandelion flavone(DF)on lipopolysaccharide(LPS)-induced colon epithelial cell injury by intervening oxidative stress and inflammation with AT-specific binding protein 2(SATB2).Methods Colon epithelial cells FHC were cultured.FHC cells were randomly divided into control group(normal cultured),LPS group(10 μg·mL-1 LPS),experimental-L group(10 μg·mL-1 LPS+1 μmol·L-1 DF),experimental-H group(10 μg·mL-1 LPS+5 μmol·L-1 DF),experimental-H+sh-NC group(transfected with sh-NC+10 μg·mL-1 LPS+5 μmol·mL-1 DF),experimental-H+sh-SATB2 group(transfected with sh-SATB2+10 μg·mL-1 LPS+5μmol·L-1 DF).The relative expression level of SATB2 protein in FHC cells was detected by Western blotting.The survival rate of FHC cells in each group was determined by tetramethylazolium blue(MTT).The apoptosis rate of FHC cells in each group was detected by flow cytometry.The levels of malondialdehyde(MDA)and interleukin-6(IL-6)in FHC cells were detected by the kit.Results The relative expression levels of SATB2 protein in control group,LPS group,experimental-H group,experimental-H+sh-NC group and experimental-H+sh-SATB2 group were 0.83±0.09,0.19±0.03,0.66±0.05,0.62±0.07 and 0.23±0.03,respectively;cell viability rates were(100.00±1.00)％,(48.16±4.31)％,(85.31±5.83)％,(81.39±6.47)％and(58.75±5.24)％,respectively;cell apoptosis rates were(3.27±0.81)％,(41.26±2.09)％,(11.35±1.04)％,(10.29±1.26)％and(35.87±2.15)％,respectively;MDA levels were(13.16±1.73),(52.87±3.49),(23.19±2.05),(20.98±3.17)and(44.87±3.05)μmol·L-1,respectively;IL-6 levels were(507.18±103.26),(2 132.09±198.15),(883.16±136.92),(801.69±119.85)and(1 736.29±206.91)pg·mL-1,respectively.The above indicators in the LPS group showed significant differences compared to the control group(all P＜0.05);the above indicators in the experimental-H group showed significant differences compared to the LPS group(all P＜0.05);the above indicators in the experimental-H+sh-SATB2 group showed significant differences compared to the experimental-H+sh-NC group(all P＜0.05).Conclusion DF has a protective effect on LPS-induced colon epithelial cell injury by intervening oxidative stress and inflammation through SATB2.

Field epidemiological investigation and treatment of a human skin anthrax outbreak were performed,including tracing of the infection source,case searching,management of close contacts,sampling and testing,and on-site elimination.Additional training and public outreach,and anthrax prevention and control measures are recommended.This case involved a sporadic outbreak of human skin anthrax,with sick cattle as the source of infection.On July 20,our patient slaughtered a cow at his home without taking any protective measures.Three days earlier,he had been stabbed at the second joint of the middle finger of his right hand,and he became infected with anthrax bacilli through the wound.Fever appeared on the day after expo-sure,and on the fourth day(July 24),a black scab mass of approximately(3X3)cm was visible at the wound site,without rupture or discharge of pus.He was hospitalized with fever at the 164th Regiment Hospital,Tacheng People's Hospital,Tacheng District People's Hospital,and Tacheng Jingcheng Hospital.His stay at the Tacheng District People's Hospital was from the 24th to 25th.He had seven close contacts,none of whom were infected,and no common exposures were identified.On the 27th,the PCR results for smear samples around the black scab were positive,the serum antibody results were positive,and the fecal samples were negative.The PCR test results for five environmental specimens were negative,and the isolation and culture results for bone surface specimens from dead cattle were positive.Strengthened efforts are necessary in training and public education regarding zoonotic disease prevention and control;establishment of local corps integration and joint prevention and control;and detection and mitigation of epi-demics in early stages.

OBJECTIVETo investigate the expression variation and significance of ERK1/2 MAPK signaling transduction pathway in the pathogenesis of esophageal squamous cell carcinoma (ESCC) in Kazakh patients.

METHODSThe expression level of p-ERK1/2 after serum starvation and treatment with U0126 inhibitor was detected in esophageal cancer cell line EC9706 by Western blot assay. The mRNA level of total ERK1/2 (t-ERK1/2) and expression level of t-ERK1/2 and p-ERK1/2 proteins of 25 pairs of ESCC and adjacent normal esophageal mucosal tissues of Kazakh patients were examined and identified by real-time quantitative PCR (qRT-PCR) and Western blotting, respectively. The expression of p-ERK1/2 protein was verified by immunohistochemistry in 126 paraffin-embeded specimens, including 19 normal esophageal mucosa, 55 esophageal carcinomas in situ and 52 invasive carcinomas.

RESULTSERK1/2 MAPK signaling transduction pathway was in an active status in the EC9706 cells. The expression level of p-ERK1/2 in Ec9706 cells reached a peak at 10 min after transient serum stimulation, and p-ERK1/2 expression was totally restrained after the treatment with 50 µmol/L U0126. In the 25 pairs of ESCC and adjacent normal mucosa, the t-ERK1 mRNA level was 1.92 ± 3.49 in the ESCC tissues and 3.67 ± 7.47 in the adjacent normal mucosa. The t-ERK1 mRNA level in ESCC tissues was significantly lower than that in adjacent normal mucosa (P < 0.05), whereas there was no significant difference of t-ERK2 mRNA level between them(P > 0.05). The expression levels of p-ERK1 and p-ERK2 proteins were 0.87 ± 0.14 and 0.79 ± 0.10 in the ESCC tissues, and 1.10 ± 0.13 and 1.32 ± 0.12 in the adjacent normal mucosae. p-ERK1/2 protein in the ESCC tissues was significantly lower than that in the adjacent normal tissue (P < 0.01). However, there was no significant difference between their t-ERK1/2 protein levels (P > 0.05). In the 126 cases of paraffin-embeded specimens, positive expressions of both p-ERK1 and p-ERK2 in esophageal cancer tissues were 7.7% (4/52), significantly lower than those in adjacent normal mucosa (31.6%, 6/19) and carcinoma in situ (85.5%, 47/55, P < 0.05).

CONCLUSIONSERK1/2 MAPK signaling pathway is in an active status in esophageal cancer and adjacent normal mucosa. Our results imply that the activation of p-ERK1/2 MAPK signaling transduction pathway plays a role in the early pathogenesis of ESCC in Kazakh patients.

Butadienes ; pharmacology ; Carcinoma in Situ ; enzymology ; pathology ; Carcinoma, Squamous Cell ; enzymology ; pathology ; Cell Line, Tumor ; China ; ethnology ; Enzyme Inhibitors ; pharmacology ; Esophageal Neoplasms ; enzymology ; pathology ; Gene Expression Regulation, Neoplastic ; Humans ; MAP Kinase Signaling System ; Mitogen-Activated Protein Kinase 1 ; genetics ; metabolism ; Mitogen-Activated Protein Kinase 3 ; genetics ; metabolism ; Nitriles ; pharmacology ; Phosphorylation ; RNA, Messenger ; metabolism

OBJECTIVES: To explore the optimal maintenance dose of caffeine citrate for preterm infants requiring assisted ventilation and caffeine citrate treatment. METHODS: A retrospective analysis was performed on the medical data of 566 preterm infants (gestational age ≤34 weeks) who were treated and required assisted ventilation and caffeine citrate treatment in the neonatal intensive care unit of 30 tertiary hospitals in Jiangsu Province of China between January 1 and December 31, 2019. The 405 preterm infants receiving high-dose (10 mg/kg per day) caffeine citrate after a loading dose of 20 mg/kg within 24 hours after birth were enrolled as the high-dose group. The 161 preterm infants receiving low-dose (5 mg/kg per day) caffeine citrate were enrolled as the low-dose group. RESULTS: Compared with the low-dose group, the high-dose group had significant reductions in the need for high-concentration oxygen during assisted ventilation (P=0.044), the duration of oxygen inhalation after weaning from noninvasive ventilation (P<0.01), total oxygen inhalation time during hospitalization (P<0.01), the proportion of preterm infants requiring noninvasive ventilation again (P<0.01), the rate of use of pulmonary surfactant and budesonide (P<0.05), and the incidence rates of apnea and bronchopulmonary dysplasia (P<0.01), but the high-dose group had a significantly increased incidence rate of feeding intolerance (P=0.032). There were no significant differences between the two groups in the body weight change, the incidence rates of retinopathy of prematurity, intraventricular hemorrhage or necrotizing enterocolitis, the mortality rate, and the duration of caffeine use (P>0.05). CONCLUSIONS This pilot multicenter study shows that the high maintenance dose (10 mg/kg per day) is generally beneficial to preterm infants in China and does not increase the incidence rate of common adverse reactions. For the risk of feeding intolerance, further research is needed to eliminate the interference of confounding factors as far as possible.
Caffeine/therapeutic use* ; Citrates ; Humans ; Infant ; Infant, Newborn ; Infant, Premature ; Respiration, Artificial ; Retrospective Studies

ObjectiveTo study the virulence and biofilm inhibition effect of Fufang Huangbai Fluid Paint （FFHBFP） on methicillin-resistant Staphylococcus aureus （MRSA）， and to explore the antibacterial effect of FFHBFP on MRSA， which provides a theoretical basis and reference for clinical medication. MethodFirstly， the microdilution method and time–growth curve were used to determine the minimum inhibitory concentration （MIC） of FFHBFP and vancomycin （VAN） against MRSA and the effect on bacterial growth. The effects of FFHBFP and VAN on the inhibition of MRSA virulence factor lipase and restoration of hydrogen peroxide （H₂O₂） sensitivity were detected under sub-minimum inhibitory concentration （sub-MIC）. The inhibitory effect of FFHBFP and VAN on MRSA biofilm formation and maturation was detected by the microplate method. The morphological changes of mature biofilms before and after administration were observed under a scanning electron microscope （SEM）. Real-time polymerase chain reaction （Real-time PCR） was utilized to detect the effect of 50.600 g·L^-1 concentration of FFHBFP on the expression of MRSA virulence gene crtM and biofilm-forming genes fnbA and icaA. Finally， molecular docking technology was used to predict the mechanism of potential antibacterial active ingredients of FFHBFP in inhibiting the virulence and biofilm of MRSA. ResultThe MIC of VAN was 2 mg·L^-1， and VAN below 1 mg·L^-1 exerted no effect on MRSA growth. The MIC of FFHBFP was not determined， while the 101.200-202.400 g·L^-1 original solution inhibited MRSA growth. Compared with the blank group and the VAN group， sub-MIC （25.300-50.600 g·L^-1 original solution） inhibited lipase and recovered MRSA sensitivity to H₂O₂ （P<0.01）. The results of the microplate method showed that FFHBFP （25.300-202.400 g·L^-1 original solution） inhibited biofilm formation and maturation （P<0.05， P<0.01）. The SEM exhibited that FFHBFP made the structure of biofilm loose and the size of the bacteria varied. FFHBFP at 50.600 g·L^-1 concentration can inhibit the expression of related virulence genes and biofilm-forming genes （P<0.05， P<0.01）， and molecular docking results also showed that the main antibacterial active ingredients in FFHBFP have good binding ability to the target. ConclusionFFHBFP that cannot directly kill MRSA exerts clinical efficacy by impairing virulence expression， biofilm formation， and other pathogenic properties.

Six compounds were isolated from the aerial part of cultivated Clerodendranthus spicatus in Hainan with various chromatographic techniques,and their structures were determined as:1-dehydroxy-1-oxo-rupestrinol(1),N-trans-feruloyltyramine(2),methyl 3,4-dihydroxyphenyllactate(3),caffein acid(4),methyl caffeate(5) and ethyl caffeate(6),via analysis of physicochemical properties and spectroscopic evidence.Compound 1 was a new compound,while compounds 2 and 3 were isolated from C.spicatus for the first time.Biological activity results showed that compounds 2-4 exhibited α-glucosidase inhibitory activity with different inhibition ratio.
China ; Glycoside Hydrolase Inhibitors ; isolation & purification ; pharmacology ; Lamiaceae ; chemistry ; Molecular Structure ; Phytochemicals ; isolation & purification ; pharmacology ; Sesquiterpenes, Eudesmane ; isolation & purification ; pharmacology