The study reports the detection of neuroprotective effect of 10 kinds of coumarin derivatives and explores their possible mechanism. MTT method was used to screen the neuroprotective effect of 10 coumarin derivatives on neurotoxic agents (Aβ25-35 and rotenone) or OGD (oxygen-glucose deprivation). A compound with better protective effect was obtained. Then the effect of this compound on neurotoxic agents on PC12 was detected by the morphological observation. Furthermore, the effect of compound 3 on microglia with lipopolysaccharide (LPS) induced inflammation was detected. And the inflammatory factor was tested. Finally, direct free radical scavenging ability was detected. Compound 3 was found to be the best compound through three neurons toxic models. Not only compound 3 ameliorated cell viability reduced by three neurons toxic models, but also significantly inhibited the production of inflammatory factor (TNF-α and IL-1β). And its free radical scavenging ability is very good, especially the effect on superoxide anion, which is comparable with vitamin C. The significant scavenging effect of compound 3 on superoxide anion might be the mechanism of the neuroprotection. Compound 3 as a potential neural cell protective agent merits further investigation.
Animals ; Coumarins ; chemistry ; Free Radical Scavengers ; chemistry ; Inflammation ; Microglia ; drug effects ; Neurons ; drug effects ; Neuroprotective Agents ; chemistry ; PC12 Cells ; Rats

OBJECTIVETo investigate the inhibitory effect of polypeptide K237 on the proliferation of human hormone refractory prostate cancer cell line PC-3M and its possible mechanism.

METHODSPC-3M cells were divided into three experimental groups and a control, treated with polypeptide K237 at the concentration of 50, 100, 200 and 0 micromol/L, respectively, for 48 hours. The effects of K237 on the proliferation of different groups of the PC-3M cells were analyzed by MTF, and the mRNA expression levels of bax and bcl-2 were detected by RT-PCR.

RESULTSAfter polypeptide K237 treatment, the PC-3M cells became round, small and less transparent in cytoplasm, and some shed and suspended in the culture medium. The growth inhibition rates of the PC-3M cells were (12.6 +/- 0.95)%, (17.8 +/- 0.99)% and (27.2 +/- 1.12)% in the 50, 100 and 200 micromol/L concentration groups. RT-PCR analysis showed that the bax/beta-actin values of the 50, 100, 200 and 0 micromol/L groups were 0.919 +/- 0.071, 0.971 +/- 0.083, 0.992 +/- 0.102 and 0.889 +/- 0.067, and the bcl-2/beta-actin values of the four groups were 0.896 +/- 0.085, 0.791 +/- 0.084, 0.764 +/- 0.702 and 0.922 +/- 0.097, respectively, both with significant differences between the experimental and the control groups (P < 0.01). The mRNA expression of bax was upregulated and that of bcl-2 downregulated in a dose-dependent manner.

CONCLUSIONPolypeptide K237 may induce apoptosis of PC-3M cells by affecting the expressions of bax and bcl-2, and thus suppress the proliferation of prostate cancer cells.

Apoptosis ; drug effects ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Humans ; Male ; Peptides ; pharmacology ; Prostatic Neoplasms ; metabolism ; Proto-Oncogene Proteins c-bcl-2 ; genetics ; metabolism ; RNA, Messenger ; genetics ; bcl-2-Associated X Protein ; genetics ; metabolism

OBJECTIVETo observe the clinical efficacy of Chinese drugs combined with chemotherapy in the treatment of acute myeloid leukemia (AML) and to investigate the prognostic relevance of the main parameters in AML treated with integrative medicine.

METHODSForty AML patients hospitalized at the authors hospital were treated with Chinese drugs and chemotherapy. The routine examination, immunophenotype and karyotype analyses were carried out. The clinical efficacy was observed and the prognostic factors were analyzed.

RESULTS(1) Clinical efficacy: Twenty patients had complete remission (CR), with the CR rate being 50.0%. Among these patients, the CR rate was 73.9% (17/23) in de novo AML and 17.6% (3/17) in secondary or refractory AML, respectively. The median disease free survival (DFS) was 6 months (2-32 months) and median overall survival (OS) was 7 months (1-36 months). (2) Analysis of prognostic factors: Aging (> 60 years) and hepatosplenomegaly or extramedullary leukemia did not affect the treatment outcome. Patients with lower white blood cell (WBC) counts (<4.0x10(9)/L) had a significantly higher CR rate (P<0.01). Secondary or refractory AML was associated with a lower CR rate and shorter OS (P<0.01,P<0.05). Expression of CD34 was an adverse factor for obtaining CR (P<0.05) and survival in both DFS and OS (P<0.05,P<0.01). The expression of CD56 was significantly associated with a lower CR rate (P<0.05), but did not affect DFS and OS. Twenty-three (57.5%) out of 40 cases had chromosomal abnormalities. The CR rate was decreased and both DFS and OS shortened stepwise from the cases with favorable cytogenetics to those with intermediate and unfavorable cytogenetics (P<0.01).

CONCLUSIONSThe combined treatment of Chinese drugs with chemotherapy has a predominant effect in de novo AML. Secondary or refractory AML, expression of CD34 and CD56, and unfavorable cytogenetics were the main factors of poor prognosis in AML.

Adolescent ; Adult ; Aged ; Antibiotics, Antineoplastic ; therapeutic use ; Antineoplastic Agents, Phytogenic ; therapeutic use ; Antineoplastic Combined Chemotherapy Protocols ; therapeutic use ; Child ; Chromosome Aberrations ; Cytarabine ; therapeutic use ; Daunorubicin ; therapeutic use ; Drugs, Chinese Herbal ; therapeutic use ; Etoposide ; therapeutic use ; Female ; Humans ; Immunophenotyping ; Integrative Medicine ; Leukemia, Myeloid, Acute ; drug therapy ; genetics ; Male ; Middle Aged ; Mitoxantrone ; therapeutic use ; Prognosis ; Treatment Outcome ; Young Adult