Diterpenoid constituents in Pseudolarix amabilis and their antitumor activities in vitro / 中国中药杂志

By various chromatographic techniques and extensive spectroscopic methods, 17 abietane diterpenoids were isolated from the dichloromethane fraction of the 95% ethanol cold-soak extracts of the seeds of Pseudolarix amabilis, namely pseudoamaol A(1), 12α-hydroxyabietic acid(2), 12-methoxy-7,13-abietadien-18-oic acid(3), 13-hydroxy-8,11,13-podocarpatrien-18-oic acid(4), 15-hydroxy-7,13-abietadien-12-on-18-oic acid(5), 8(14)-podocarpen-13-on-18-oic acid(6), holophyllin K(7), metaglyptin B(8), 7α-hydroxydehydroabietinsaure-methylester(9), 7-oxodehydroabietic acid(10), 15-hydroxy-7-oxodehydroabietinsaure-methy-lester(11), 15-methoxydidehydroabietic acid(12), 7-oxo-15-hydroxy-dehydroabietic acid(13), 15-hydroxydehydroabietic acid(14), 8,11,13-abietatriene-15,18-diol(15), 8,11,13-abietatriene-15-hydroxy-18-succinic acid(16), and 7β-hydroxydehydroabie-tic acid(17). Compound 1 was a new compound. The isolated compounds were evaluated for their antitumor activities(HepG2, SH-SY5Y, K562), and compounds 8 and 17 showed potential cytotoxic activity against K562 cells, with IC_(50) values of 26.77 and 37.35 μmol·L~(-1), respectively.

Chemical constituents of Physalis minima / 中国中药杂志

Fifteen compounds(1-15) were isolated from the 95% EtOH extract of the whole herb of Physalis minima by various chromatography techniques including silica gel, Sephadex LH-20, middle chromatogram isolated gel(MCI), octadecyl silica(ODS), and semi-preparative high performance liquid chromatography(HPLC). Their structures were elucidated by infrared spectroscopy(IR), ultraviolet spectroscopy(UV), high-resolution electrospray ionization mass spectrometry(HR-ESI-MS), nuclear magnetic re-sonance(NMR), and circular dichroism(CD) as(5S)-5,11-dihydroxy-3-methyl-5-pentylfuran-2(5H)-one(1), withaphysalin R(2), withaphysalin Q(3), withaphysanolide A(4), phaseic acid(5), grasshopper ketone(6), 3S,5R-dihydroxy-6S,7-megastigmadien-9-one(7), vanillic acid(8), 2-trans,4-trans-abscisic acid(9), capillasterolide(10), 5,3'-dihydroxy-3,7,4'-trimethoxyflavone(11),(-)-loliolide(12), 4-hydroxyacetophenone(13), acetosyringone(14), and aurantiamide acetate(15). Compound 1 was a new butenolide, and compounds 5-7 and 10-12 were isolated from the Physalis for the first time. Compounds 4, 13, and 15 were isolated for the first time from P. minima. Moreover, their anti-inflammatory activity was evaluated in vitro. Compound 12 was found to possess an inhibitory effect on the transcription of an NF-κB-dependent reporter gene in LPS-induced 293 T/NF-κB-luc cells at 10 μmol·L~(-1), showing an inhibitory rate of 62.31%±4.8%.

Valproic acid induces neuroglobin protein by CREB and protects N2a cells against H2 O2-induced neurotoxicity / 中国药理学通报

Aim To investigate the effect and mecha-nism of valproic acid on neuroglobin expression, and the neuroprotective role of valproic acid against H2 O2-induced neurotoxicity. Methods Western blot, RT-PCR and luciferase assay were used to detect the pro-tein levels, mRNA levels and promoter activity of mouse and human neuroglobin induced by valproic acid. Luciferase assay was used to investigate the role of transcription factor CREB in the up-regulation of neuroglobin by valproic acid. MTT assay was used to evaluate the effect of valproic acid against H2 O2-in-duced neurotoxicity. Results VPA treatment marked-ly increased the protein levels, mRNA levels and pro-moter activity of Ngb in mouse N2 a cells and human SKNSH cells. CREB specific inhibitor KG501 or CREB dominant negative mutant KCREB attenuated VPA-induced Ngb promoter activity. VPA could pro-tect N2a cells from H2 O2-induced neurotoxicity. Con-clusion CREB mediates VPA-induced Ngb up-regula-tion, which may contribute to the neuroprotective effects of VPA in oxidative stress in neurons.

Risk factors on the recurrence of ischemic stroke and the establishment of a Cox' s regression model / 中华流行病学杂志

Objective To investigate the risk factors and establish the Cox' s regression model on the recurrence of ischemic stroke. Methods We retrospectively reviewed consecutive patients with ischemic stroke admitted to the Neurology Department of the Hebei United University Affiliated Hospital between January 1,2008 and December 31,2009. Cases had been followed since the onset of ischemic stroke. The follow-up program was finished in June 30, 2010. Kaplan-Meier methods were used to describe the recurrence rate. Monovariant and multivariate Cox' s proportional hazard regression model were used to analyze the risk factors associated to the episodes of recurrence.And then, a recurrence model was set up. Results During the period of follow-up program, 79 cases were relapsed,with the recurrence rates as 12.75% in one year and 18.87% in two years. Monovariant and multivariate Cox' s proportional hazard regression model showed that the independent risk factors that were associated with the recurrence appeared to be age (X1)(RR=1.025,95% CI: 1.003-1.048),history of hypertension (X2) (RR= 1.976, 95% CI: 1.014-3.851), history of family strokes (X3) (RR=2.647,95%CI: 1.175-5.961), total cholesterol amount (X4) (RR= 1.485,95%CI: 1.214-1.817), ESRS total scores (X5) (RR= 1.327,95%CI: 1.057-1.666) and progression of the disease (X6) (RR= 1.889,95%CI: 1.123-3.178). Personal prognosis index (PI) of the recurrence model was as follows: PI=0.025X1 + 0.681X2+ 0.973X3 + 0.395X4+ 0.283X5 + 0.636X6. The smaller the personal prognosis index was, the lower the recurrence risk appeared, while the bigger the personal prognosis index was, the higher the recurrence risk appeared. Conclusion Age, history of hypertension, total cholesterol amount, total scores of ESRS, together with the disease progression were the independent risk factors associated with the recurrence episodes of ischemic stroke. Both recurrence model and the personal prognosis index equation were successful constructed.

Thinking on hospital construction of integrated traditional Chinese and Western medicine / 中国中西医结合杂志

Through supervising the construction of some key hospitals of integrated Chinese and Western medicine (ICWM), the characteristic indexes and problems concerning hospital construction were analyzed. It was pointed out that in order to improve the level of construction and administration of ICWM hospitals, the overall effect of construction should be paid attention to, the cultivation of ICWM professionals should be strengthened and the ICWM standard based assessment on clinical efficacy should be stressed. Besides, the strategies on administration pattern of ICWM hospitals were discussed.

Optimization of cultural condition of genetic engineering strain for antibiotic peptide adenoregulin and research on its fed-batch cultivation / 生物工程学报

33 amino acid antibiotic peptide adenoregulin (ADR), which were firstly isolated from the skin of South America arboreal frog Phyllomedusa bicolor, forms alpha-helix amphipathic structure in apolar medium and has a wide spectrum of antimicrobial activity and high potency of lytic ability. Adr gene was cloned in pET32a and transformed into Escherichia coli BL21(DE3) . The cultural and inductive conditions of E. coli BL21(DE3)/pET32a-adr have been optimized. The effect of three factors which were time point of induction, concentration of IPTG in the culture and time of induction on the expression level of Trx-ADR was investigated. The results indicated that the expression level was affected by the time point of induction most predominantly. 9 veriaties of media in which BL21 (DE3)/pET32a-adr was cultured and induced were tested to achieve high expression level of target protein. It was found that glucose in the medium played an important role in keeping stable and high expression level of Trx-ADR. The optimal inductive condition is as follows: the culture medium is 2 x YT + 0.5% glucose, the time point of induction is OD600 = 0.9, the final concentration of IPTG in the culture is 0.1 mmol/L and the induction time is 4 h. BL21 (DE3)/pET32a-adr was cultivated according to the strategy of constant pH at early stage and exponential feeding at later stage to obtain high cell density. During the entire fed-batch phase, by controlling the feeding of glucose, the specific growth rate of the culture was controlled at about 0.15 h(-1), the accumulation of acetic acid was controlled at low level (<2 g/L), but the plasmid stability could not be maintained well. At the end of the cultivation, 40% of the bacteria in the culture lost their plasmids. As a result, the expression level of the target protein declined dramatically, but 90% of Trx-ADR was in soluble form. The expressed fusion protein showed no antibacterial activity, while the native form of ADR lysed from Trx-ADR showed distinct antibacterial activity.