Drug Combinations ; Drug Design ; Drugs, Chinese Herbal ; pharmacology ; Drugs, Investigational ; Humans

A new sesquiterpenoid, 8α-hydroxy-6β-methoxy-1-oxoeremophila-7 (11), 9 (10) -diene-12, 8-olide (1) and five known compounds, petasin (2), caffeic acid (3), hepta-cosanol (4), β-sitosterol (5) and β-daucosterol (6) have been isolated from the roots of Ligularia intermedia. The compounds were isolated by column chromatography on silica gel and Sephadex LH-20, and identified based on spectral analyses (MS, 1H-NMR, 13C-NMR).
Asteraceae ; chemistry ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Magnetic Resonance Imaging ; Molecular Structure ; Plant Roots ; chemistry ; Spectrometry, Mass, Electrospray Ionization

Firstly discovered in 1980s,human immunodeficiency virus (HIV) continues to affect more and more people.However,there is no effective drug available for the therapy of HIV infection.Betulinic acid existing in various medicinal herbs and fruits exhibits multiple biological effects,especially its outstanding anti-HIV activity,which has drawn the attentions of many pharmacists.Among the derivatives of betulinic acid,some compounds exhibited inhibitory activities at the nanomolar concentration,and have entered phase Ⅱ clinical trials.This paper summarizes the current investigations on the anti-HIV activity of betulinic acid analogues,and provides valuable data for subsequent researches.

BACKGROUNDIncreasing evidence suggests that many neurons may die through apoptosis in Alzheimer's disease (AD). Mitochondrial dysfunction has been implicated in this process of neuronal cell death. One promising approach for preventing AD is based upon anti-apoptosis to decrease death of nerve cells. In this study, we observed the memory improving properties of curcumin in mice and investigated the neuroprotective effect of curcumin in vitro and in vivo.

METHODSThe mice were given AlCl(3) orally and injections of D-galactose intraperitoneally for 90 days to establish the AD animal model. From day 45, the curcumin group was treated with curcumin for 45 days. Subsequently, the step-through test, neuropathological changes in the hippocampus and the expression of Bax and Bcl-2 were carried out to evaluate the effect of curcumin on the AD model mice. In cultured PC12 cells, AlCl(3) exposure induced apoptosis. The MTT assay was used to measure cell viabilities; flow cytometric analysis to survey the rate of cell apoptosis; DNA-binding fluorochrome Hoechst 33258 to observe nuclei changes in apoptotic cells and Western blot analysis of Bax, Bcl-2 to investigate the mechanisms by which curcumin protects cells from toxicity.

RESULTSCurcumin significantly improved the memory ability of AD mice in the step-through test, as indicated by the reduced number of step-through errors (P < 0.05) and prolonged step-through latency (P < 0.05). Curcumin also attenuated the neuropathological changes in the hippocampus and inhibited apoptosis accompanied by an increase in Bcl-2 level (P < 0.05), but the activity of Bax did not change (P > 0.05). AlCl(3) significantly reduced the viability of PC12 cells (P < 0.01). Curcumin increased cell viability in the presence of AlCl(3) (P < 0.01). The rate of apoptosis decreased significantly in the curcumin group (P < 0.05) when measured by flow cytometric analysis. Curcumin protected cells by increasing Bcl-2 level (P < 0.05), but the level of Bax did not change (P > 0.05).

CONCLUSIONSThis study demonstrates that curcumin improves the memory ability of AD mice and inhibits apoptosis in cultured PC12 cells induced by AlCl(3). Its mechanism may involve enhancing the level of Bcl-2.

Aluminum Compounds ; toxicity ; Alzheimer Disease ; drug therapy ; psychology ; Animals ; Apoptosis ; drug effects ; Cells, Cultured ; Chlorides ; toxicity ; Curcumin ; pharmacology ; therapeutic use ; Disease Models, Animal ; Female ; Learning ; drug effects ; Memory ; drug effects ; Mice ; Neuroprotective Agents ; pharmacology ; PC12 Cells ; Rats

OBJECTIVETo observe the influence of Xinmaitong capsule (XMT) on serum matrix metalloproteinases-9, high sensitive C-reactive protein levels in patients with acute coronary syndrome.

METHOD63 cases were divided by randomized, contrastive assigned to XMT group (n = 31) and control group (n = 32). The serum levels of MMP-9 and hs-CRP before and after treatment in 12 weeks were detected.

RESULTAfter treatment, the serum levels of MMP-9 in control group had no changed and the levels of hs-CRP reduced. The serum levels of MMP-9 and hs-CRP in XMT group had significantly decreased. The serum levels of MMP-9 and hs-CRP had positive correlation, but had no correlation to levels of serum lipids.

CONCLUSIONXMT decreased breakdown of matrix collagen, and inflammatory reaction in the patients of ACS, which may have effect on plaque stabilization.

Acute Coronary Syndrome ; blood ; drug therapy ; Aged ; C-Reactive Protein ; metabolism ; Capsules ; Cholesterol ; blood ; Cholesterol, HDL ; blood ; Cholesterol, LDL ; blood ; Drug Combinations ; Drugs, Chinese Herbal ; isolation & purification ; therapeutic use ; Female ; Humans ; Male ; Matrix Metalloproteinase 9 ; blood ; Middle Aged ; Phytotherapy ; Plants, Medicinal ; chemistry ; Triglycerides ; blood

OBJECTIVETo observe effect of porcine relaxin(pRLX) on NO production of human microvascular endothelial cells(HMVECs) and discuss its possible mechanism.

METHODSiNOS and cNOS expression of HMVECs with or without pRLX were detected using western blotting. NO production of HMVECs with pRLX at different concentration or different time were determined by method of Griess. NO production of pRLX of HMVECs plus Non-selective NOS inhibitor NG-monomethyl-L-arginine(L-NMMA), selective iNOS inhibitor aminoguanidine(AG) or nuclear factors-kappaB (NF-kappaB) inhibitor pyrrolidine dithiocarbamate(PDTC) were also analysed.

RESULTSpRLX promoted iNOS protein expression of HMVECs, but not cNOS protein expression. NO production of HMVECs was promoted by pRLX on concentration-dependent pattern instead of time-dependent one. AG, L-NMMA and PDTC were showed to block the effect of pRLX on NO production of HMVECs.

CONCLUSIONpRLX promote iNOS expression and NO production of HMVECs.

Animals ; Dose-Response Relationship, Drug ; Endothelial Cells ; cytology ; drug effects ; metabolism ; Humans ; Lung ; blood supply ; Nitric Oxide ; biosynthesis ; Nitric Oxide Synthase Type II ; biosynthesis ; Relaxin ; pharmacology ; Swine ; Time Factors

Objective To learn the status and influencing factors of anxiety and depression among the people affected by leprosy.Methods A total of 60 leprosy patients was enrolled.An investigation including questionnaire and two mental scales namely Self -Rating Anxiety Scale (SAS)and Self -Rating Depression Scale (SDS)were conducted.Results The rate of anxiety and depression was 41.67% (25 /60)and 21.67% (13 /60)respectively.There was no statistical difference on the rate of anxiety and depression between genders.Multiple logistic regression analysis showed that treatment status (OR =23.78,95%CI =2.13 -265.26),disability (OR =7.68,95%CI =2.01 -29.40)and income (OR =4.54,95%CI =1.05 -19.68)were the risk factors of anxiety,and disability (OR =34.77,95%CI =2.84 -425.07) and treatment status (OR =19.28,95%CI =1.86 -199.62)were the risk factors of depression.Conclusion The people affected by leprosy has a high level of anxiety and depression.Disability and treatment status were the major risk factors of anxiety and depression among the people.

OBJECTIVETo investigate the efficacy of imatinib in the treatment of chronic myeloid leukemia (CML) and analyse the treatment outcome and related factors.

METHODSNinety five CML patients were treated with imatinib in our hospital from May 2002 to May 2006. The outcomes and related factors were analysed.

RESULTS(1) One year after therapy, there were 95.5% of chronic phase (CP) patients achieved complete hematologic response (CHR). Fifty-two patients with complete cytogenetic dates were divided into primary-therapy group (n = 19) and secondary-therapy group (n = 33). The major cytogenetic responses (MCyR) at 6-, 12-, 18-, 24- and 30-months after therapy for the former group were 84.2%, 84.2%, 89.5%, 89.5% and 94.7%, and for the latter group were 36.4%, 39.4%, 39.4%, 39.4% and 39.4%, respectively (P < 0.01). The expected survival at 12-, 24-, 36- and 50-month after imatinib treatment for CP group was (98.1 +/-1.9)%, (87.8 +/- 7.1)%, (81.9 +/- 8.7)% and (81.9 +/- 8.7)%, respectively. (2) Twelve month after therapy, there are 70% of accelerated phase (AP) patients achieve CHR and 10% get MCyR. The expected survival at 12-, 24- and 36-month after imatinib treatment for AP group was (63.0 +/- 17.7)%, (15.8 +/- 14.3)% and (15.8 +/- 14.3)%, respectively. (3) Six month after therapy, 57.9% of blast crisis (BC) patients achieve CHR, with the expected survival at 12- and 24-month of (40.6 +/- 12.3)% and 0, respectively. (4) COX analysis CP group indicated that imatinib therapy administered for previously untreated was an independent favorable prognostic factor. Conclusion (1) Imatinib as a primary treatment for CP CML can significantly improve the survival time as compared with that AP or BC patients or with that used in previously treated patients. (2) Imatinib could induce hematologic, even cytogenetic response to a certain extent, in CP or BC patients and prolong the survival time.

Adolescent ; Adult ; Aged ; Antineoplastic Agents ; therapeutic use ; Benzamides ; Female ; Humans ; Imatinib Mesylate ; Leukemia, Myelogenous, Chronic, BCR-ABL Positive ; drug therapy ; Male ; Middle Aged ; Piperazines ; therapeutic use ; Pyrimidines ; therapeutic use ; Treatment Outcome ; Young Adult

BACKGROUNDEvaluation of fetal central nervous system (CNS) agenesis by ultrasonography (US) is frequently limited, but magnetic resonance imaging (MRI) has its own advantages and is gaining popularity in displaying suspected fetal anomalies. The purpose of this study was to explore the value of MRI in detecting fetal CNS agenesis.

METHODSThirty-four women (aged from 22 to 35 years, average 27 years) with complicated pregnancies (16 - 39 weeks of gestation, average 30 weeks) were examined with a 1.5 T superconductive MR unit within 24 hours after ultrasonography. Half-Fourier acquisition single-shot turbo spin-echo (HASTE) T(2)-weighted imaging (T(2)WI) sequence were performed in all patients, and fast low angle shot (FLASH) T(1)-weighted imaging (T(1)WI) sequence were applied sequentially in seven of them. Comparison of the results was made between the MRI and US findings as well as autopsy or postnatal follow-up MRI findings.

RESULTSThe gyrus, sulcus, corpus callosum, thalamus, cerebellum, brainstem, and spinal cord of fetus were shown more clearly on T(2)-weighted MR images than on T(1)-weighted MR images. MRI corrected the diagnosis of US in 10 cases (10/34, 29.41%) and the diagnosis was missed only in 1 case (1/34, 2.94%).

CONCLUSIONMRI has advantages to US in detecting fetal CNS anomalies and is a supplement to US in complicated pregnancies.

Adult ; Central Nervous System ; abnormalities ; diagnostic imaging ; Female ; Humans ; Magnetic Resonance Imaging ; methods ; Pregnancy ; Ultrasonography, Prenatal

OBJECTIVETo study the effects of oxygen and calcium on the expression of eukaryotic vectors harboring wild-type or mutated hypoxia-inducible factor-1alpha (HIF-11alpha) in HEK293 cells.

METHODSHEK293 cells were transiently transfected with pcDNA3.1+/HIF-11alpha, pcDNA3.1+/HIF-11alpha-564Ala and pcDNA3.1+/HIF-11alpha-564Ala-803Ala via lipofectin. Western blotting were used to detect HIF-11alpha protein after normoxic or hypoxic exposure of the transfected HEK293 cells in the presence or absence of Ca(2+). The levels of vascular endothelial growth factor (VEGF) mRNA in the transfected cells in normoxic condition was detected using RT-PCR.

RESULTSThe levels of HIF-11alpha protein and VEGF mRNA increased in HEK293 cells transfected with the vectors harboring mutated HIF-11alpha, but not in the cells transfected with wild-type HIF-11alpha vectors in normoxia. Hypoxia increased the levels of HIF-11alpha protein in the cells transfected with wild-type HIF-11alpha vectors, which was inhibited by the application of Ca(2+). Ca(2+) showed no inhibitory effect on HIF-11alpha levels in HEK293 cells transfected with the vectors containing mutated HIF-11alpha.

CONCLUSIONThe protein products of pcDNA3.1+/HIF-11alpha-564Ala and pcDNA3.1+/HIF-11alpha- 564Ala-803Ala in HEK293 cells enhance the cell tolerance to oxygen and protease.

Calcium ; metabolism ; Cell Hypoxia ; Genetic Vectors ; HEK293 Cells ; Humans ; Hypoxia-Inducible Factor 1, alpha Subunit ; genetics ; metabolism ; Oxygen ; metabolism ; RNA, Messenger ; genetics ; Transfection ; Vascular Endothelial Growth Factor A ; metabolism