To investigate the anticancer effects of ring C in 18β-glycyrrhetinic acid (GA), a series of GA derivatives featured with 9(11)-ene moiety in ring C were designed and synthesized. The structures were confirmed by IR, LC-MS and 1H NMR. Their inhibitory effects towards human prostate cancer PC-3 and leukemia HL-60 cell lines were determined. Most of the derivatives displayed stronger antiproliferative activities than GA. Particularly, compound 14 showed promising anticancer activity with the GI50 values of 4.48 µmol · L(-1) and 1.2 µmol · L(-1) against PC-3 and HL-60 cells respectively, which is worth further study.
Antineoplastic Agents ; chemistry ; pharmacology ; Cell Line, Tumor ; drug effects ; Cell Proliferation ; drug effects ; Drug Design ; Glycyrrhetinic Acid ; analogs & derivatives ; chemistry ; HL-60 Cells ; drug effects ; Humans ; Male ; Prostatic Neoplasms ; pathology

Nerve growth factor is one of the most important factors playing an important role in regulating the growth, development and survival of the neuron. The purified NGF from human placenta has been reported, the tissue from which can be isolated the NGF is very limited. It is important for basic research and clinic application to expression hNGF by genetic engineering. By polymerase chain reaction,gene fragment encoding the mature part of ?-NGF was amplified using the DNA of human placenta as template. The fragment was sequenced and inserted into expression vector pET-15b, and the recombinant expression vector pET15b-NGF was transformed into E.coli BL21(DE3)pLysS. After inducing with IPTG the NGF was higher expressed up to 25% of the total cell proteins. The expression product was purified with metal chelate affinity chromatography on Ni-IDA agarose under denaturing condition. The purity of rNGF was higher than 90% and yield of rNGF was 4.56mg/L expressing bacteria. SDS-PAGE revealed the NGF expression product had a Mr 16kDa. Western-blot displayed the recombinant product had strong immunological activity with rabbit anti-human ?-NGF polyclonic antibodies. The expression products were dealed with solubilizing inclusion bodies and refolding protein. The test of nerve fiber growth of chicken embryo DRG neurons displayed rNGF had biological activity.

Objective To investigate the expression in the VEGF,TGF-?1 of cervical squamous car- cinoma infected by HPV16,18.Methods Cells exfoliated from cervix(collected by clinician)of 99 women with cervical cancer and 54 women as a control group were analyzed blindly by human papillomavirus type 16 and 18 Fluorescent Polymerase Reaction Diagnositic kit.The expression of VEGF,TGF-?1 of the positive HPV16,18 of 38 women with cervical squamous cancer were studied by immunohistochemical stain.Results The positive expression of HPV16,18 was observed in 53 in the case of cervical cancer with positive rates of 54 %,but the positive rates was 7 % in the control group(P

In adipose tissues from sreater omentum of patients with type 2 diabetes,the mRNA and protein expressions of human rearranged immunoglobulin?light chain (HSIGVL) 022 were measured by the fluorescent quantitative RT-PCR and immunohistochemistry respectively.The results showed that mRNA and protein levels of HSIGVL022 were up-regulated in patients with type 2 diabetes.The mRNA level of HSIGVL022 was linearly correlated with insulin resistance index,suggesting that this gene may play a role in the pathogenesis of insulin resistance and type 2 diabetes.

Albuminuria ; drug therapy ; Diabetes Mellitus, Type 2 ; complications ; drug therapy ; Diabetic Nephropathies ; drug therapy ; Humans ; Tetrazoles ; therapeutic use

OBJECTIVETo study the lipid constituents from Echinacea purpurea.

METHODThe compounds were isolated by chromatography method and the structures were identified on the basis of spectral analyses.

RESULTFive compounds were isolated and identified as, 1 beta, 6 alpha-dihydroxy-4(14)-eudesmene(1), (2E, 4E, 8Z, 10E)-N-isobutyl-2,4,8,10-dodecatetraenamide(2), (2E, 4E, 8Z, 10Z)-N-isobutyl-2,4,8,10-dodecatetraenamide(3), cerotic acid(4), hyxacosyl alcohol(5).

CONCLUSIONCompounds 1,4 and 5 were obtained from the plant for the first time.

Echinacea ; chemistry ; Fatty Acids ; chemistry ; isolation & purification ; Fatty Alcohols ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry ; Sesquiterpenes ; chemistry ; isolation & purification

OBJECTIVETo understand the incidence of post-stroke depression (PSD) and the therapeutic effect of acupuncture-moxibustion.

METHODSFive hundred and sixty cases were rating with Hamilton depression scale, and lesion parts, gender, age and property of stroke between the PSD and non-PSD were compared by analysis of variance, chi2 test, and then the patients of PSD were randomly divided into two groups and treated respectively with Prozac-20 and acup-moxibustion at Sishencong (EX-HN 1), Anmian, Neiguan (PC 6), Shenmen (HT 7), Zusanli (ST 36), Sanyinjiao (SP 6), Taichong (LR 3), Zhaohai (KI 6), Shenmai (BL 62).

RESULTSThe total incidence rate of PSD was 43.9%, with no relation to the lesion parts, gender, age and property of stroke (P > 0.05), and there were very significant differences in HAMD scores before and after treatment in the two groups (P < 0.0001), with no significant difference in the effective rate between the two groups (P > 0.05).

CONCLUSIONPSD has a high incidence and influences the recovery of nervous function, and it should be treated at early stage. Acup-moxibustion and Prozac-20 have similar therapeutic effect.

Acupuncture Therapy ; Aged ; Depression ; epidemiology ; therapy ; Female ; Humans ; Incidence ; Male ; Middle Aged ; Moxibustion ; Stroke ; complications

Objective To investigate the in vitro antimicrobial activity of ampicillin-sulbactam,clindamycin and cefoperazone a- gainst common clinical isolates.Methods MICs of these three antibiotics were determined by E test.Results Ampicillin-sulbae- tam showed inhibition rate of 100% for methicillin susceptible S.aureus (MSSA),E.faecalis,Group A Streptococcus,H. influenzae,penicillin-susceptible S.pneumoniae (PSSP),M.catarrhalis and anaerobes (including 10 strains of Bacteroid spp.,2 strains of P.aches,1 strain of E.lentum,1 strain of Fusobacterium innocuum,and 2 strains of Peptostreptococcus spp.).Ampicillin-sulbactam was active against 86.7% of extended-spectrum?-lactamase non-producing K.pneumoniae (NES- BL-KPN) and 53.3% of non ESBL-producing E.coli (NESBL-ECO).Ampicillin-sulbactam only inhibited 23.3% of A.bau- mannii isolates and 25.0% of E.faecium isolates.For MSSA,anaerobes,PSSP and group A Streptococcus,about 60.0%, 31.2%,30.0% and 10.0% of the isolates were susceptible to clindamycin,respectively.For MSSA,NESBL-ECO and NES- BL-KPN,96.7% to 100% of the isolates were susceptible to cefoperazone.About 40.0% of P.aeruginosa isolates were sus- ceptible to cefoperazone.No A.baumannii isolate was susceptible to cefoperazone.Conclusions The ampicillin-sulbactam has good antimicrobial activity against MSSA,E.faecalis,Group A Streptococcus,NESBL-KPN,H.influenzae,PSSP,M.ca- tarrhalis and anaerobes.In this study,clindamycin is active against 60% of MSSA isolates.Most of other species are relatively resistant to clindamycin.Cefoperazone shows good activity against MSSA,NESBL-ECO,and NESBL-KPN.These three anti- microbial agents can be used as empirical treatment for community-acquired infections.

Objective To evaluate the acute and delayed killing effect of high intensity focused ultrasound (HIFU) on Echinococcus granulosus(E. granulosus)protoscolices in vitro.Methods E. granulosus protoscolices were treated with different dosage of effective power(0,25,50,100,200,250 W)and time(5,10,20,30,40,50,60 s)of HIFU in vitro to obtain the dosage-effect curves.Then the survival pmtoscolices were incubated,and the mortality of each group was counted daily.The protoscolicidal effects were investigated by trypan blue exclusion assay.Results Compared with the untreated group,the Vitality of E.granulosus protoscolices significantly decreased immediately after treated by HIFU of different dosage(F=5201.59 vs 1865.65,P＜0.05),there were the interaction both different dosage and time(F=214.50,P＜0.05).The protoscolices were broken into pieces by HIFU of 250 W×40 s,whereas the growth of the surviving protoscolices after exposed to HIFU was obvious suppressed.Both the acute killing effect and the delayed inhibitory effect showed a dosage-dependant manner.The inhibitory effect increased along with the increased dosage of HIFU(P＜0.05).The inhibitory effect in 50 W×10 s group was stronger than 25 W×20 s group(P＜0.05).The mortality was increased in parallel with the increase of HIFU dosage.Conclusions HIFU show an effective immediately killing effect,as well as a growth-inhibiting effect on the E.granulosus protoscolices in vitro.

OBJECTIVETo investigate the relationship between various Chinese medicine (CM) types and T-cell subsets (CD4(+) and CD8(+)) in the colonic mucous membranes of patients with ulcerative colitis (UC).

METHODSFifty UC patients were enrolled, after differentiation into four types by CM syndromes, i.e., the internal heat-damp accumulation type (IHDA), the qi-stagnancy with blood stasis type (QSBS), the Pi-Shen yang-deficiency type (PSYD) and the yin-blood deficiency type (YBD). From every patient, 3-5 pieces of intestinal mucous membrane tissues were taken through colonoscopy to determine the levels of the T-cell subsets (CD4(+) and CD8(+)) using immunohistochemical method. The results were compared with those in the normal control.

RESULTSThe level of CD8(+)increased and the ratio of CD4(+)/CD8(+)decreased mainly in colonic mucous membranous tissues in UC patients. The level of CD4(+)decreased significantly in IHDA types (P<0.01), but decreased only slightly in the PSYD, QSBS and YBD types. CD8(+)increased significantly in the IHDA types (P<0.01), but only slightly in the other three types.

CONCLUSIONThe IHDA types of UC are closely related with T-cell subsets. The difference of T-cell subsets in various IHDA types of UC patients has provided a theoretical basis for syndrome differentiation in the CM typing of UC.

Adolescent ; Adult ; Aged ; Biopsy ; Blood Circulation ; CD4-CD8 Ratio ; Colitis, Ulcerative ; immunology ; pathology ; Colon ; drug effects ; immunology ; pathology ; Colonoscopy ; Female ; Humans ; Immunohistochemistry ; Male ; Medicine, Chinese Traditional ; Middle Aged ; Qi ; T-Lymphocyte Subsets ; drug effects ; Yang Deficiency ; immunology ; pathology ; Yin Deficiency ; immunology ; pathology ; Young Adult