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120 records · Page 7Linked to original sources
PubMed2004

Anti-proliferation effect of oridonin on HL-60 cells and its mechanism.

OBJECTIVE: To investigate the anti-proliferation effect of oridonin on leukemic HL-60 cells and its mechanism. METHODS: HL-60 cells in vitro in culture medium were given different concentrations of oridonin. The inhibitory rate of cells were measured by microculture tetrazolium (MTT) assay, cell apoptotic rate was detected by flow cytometry (FCM), morphology of cell apoptosis was observed by hoechst 33258 fluorescence staining, and the activity of telomerase was detected using telomere repeat amplification protocol (TRAP) PCR-ELISA before and after apoptosis occurred. RESULTS: Oridonin could decrease telomerase activity, inhibit growth of HL-60 cells, and cause apoptosis significantly. The suppression was both in time- and dose-dependent manner. Marked morphological changes of cell apoptosis including condensation of chromatin and nuclear fragmentation were observed clearly by hoechst 33258 fluorescence staining especially after cells were treated 48-60 hours by oridonin. CONCLUSIONS: Oridonin has apparent anti-proliferation and apoptotic effects on HL-60 cells in vitro, decreasing telomerase activity of HL-60 cells may be one of its most important mechanisms. These results will provide strong laboratory evidence of oridonin for clinical treatment of acute leukemia.

Antineoplastic Agents, Phytogenic↗
PubMed2005

Rabdosia rubescens inhibits breast cancer growth and angiogenesis.

Investigators have shown that PC-SPES is a potent herbal mixture which has often been used by prostate cancer patients. In this study, we examined the inhibitory effects of certain individual components of PC-SPES on the in vitro proliferation of the human breast cancer cells MDA-MB231 and the human umbilical vein endothelial cells (HUVEC). Our data showed that individual components of PC-SPES had varying suppressive effects on cellular proliferation, and that Rabdosia rubescens appeared to be the most potent agent in these assays. Apoptosis was up-regulated by Rabdosia rubescens, as seen in the caspase-9 and TUNEL assays. These effects may be mediated via both the MAPK (mitogen-activated protein kinase) and the Akt kinase pathways. In mouse experiments, the extract from Rabdosia rubescens suppressed breast cancer xenograft size and decreased the tumor vessel density. We conclude that Rabdosia rubescens may potentially be used to treat or prevent breast cancer, and that the extract from this herbal source deserves further studies.

Angiogenesis Inhibitors↗
PubMed2004

[Regulation of telomerase activity and cell cycle of K562 cells by oridonin].

AIM: To investigate the effect of oridonin (ORI) on telomerase activity and cell cycle of human leukemic cell line K562 cells. METHODS: Immunohistochemistry (IHC) technique was used to determine the expression of hTERT or C-myc. Telomerase activity was detected with TRAP-PCR-ELISA assay. In addition, the percentages of K562 cells in different cell cycle were determined by flow cytometry (FCM) at 24th and 48th hours separately after adding the different concentrations of ORI. RESULTS: After the K562 cells were treated with ORI at 3.43 micromol x L(-1) for 48 h, the expression of hTERT and C-myc decreased obviously. There was statistical significant (P < 0.05) difference between experimental groups and the normal controls. In addition, the telomerase activity of K562 cells was significantly inhibited by ORI at the dose of 3.43 micromol x L(-1) for 48 h. At the same time, the cell cycle distribution changed, the percentage of G0/G1 or G2/M stages cells increased and that of the S stage cells decreased after ORI was added. CONCLUSION: ORI can effectively inhibit telomerase activity in K562 cells. Arresting cell cycle and decreasing the expression of hTERT and C-myc may be the mechanism of action.

Antineoplastic Agents, Phytogenic↗
PubMed2005

The cytostatic and cytotoxic effects of oridonin (Rubescenin), a diterpenoid from Rabdosia rubescens, on tumor cells of different lineage.

Rabdosia rubescens is a herbal medicine used to treat esophageal cancer in China. In this study, the sesquiterpene oridonin, an isoprenoid, was isolated from Rabdosia rubescens. Mass spectroscopy and carbon 13 NMR spectroscopy were used to identify the structure of the purified compound. It was then evaluated for biological activity against human cell lines derived from prostate (DU-145, LNCaP), breast (MCF-7), and ovarian (A2780 and PTX10) cancers. Oridonin exhibited anti-proliferative activity toward all cancer cell lines tested, with an IC50 estimated by the MTT cell viability assay ranging from 5.8+/-2.3 to 11.72+/-4.8 microM. Flow cytometric analysis demonstrated that oridonin induced a G1 phase arrest in androgen receptor-positive LNCaP cells containing wt p53, while it blocked the cell cycle at G2 and M phases in androgen receptor-negative DU-145 cells with mutated p53; the arrest in M was verified by examination of cell morphology and by the increased frequency of cells with Ser-10 phosphorylated histone H3. The increased incidence of apoptosis, identified by characteristic changes in cell morphology, was seen in tumor lines treated with oridonin. Notably, at concentrations that induced apoptosis among tumor cells, oridonin failed to induce apoptosis in cultures of normal human fibroblasts. Western blot analysis was used to determine the protein expression of cancer suppressor genes, p53 (wt) and Bax, and the proto-oncogene, Bcl-2 in LNCaP cells following treatment with oridonin. Oridonin up-regulated p53 and Bax and down-regulated Bcl-2 expression in a dose-dependent manner. To further explore the possible interaction between oridonin and DNA, its absorption spectrum was measured in the presence and absence of double stranded (ds) DNA. Spectral shifts and an increase in absorption band intensity were observed indicating interaction of oridonin with DNA bases. The nature of the binding is not clear at present though no evidence of histone H2AX phosphorylation on Ser-139 was apparent in DU-145 cells treated with oridonin that would indicate the induction of ds DNA breaks. In conclusion, oridonin inhibits cancer cell growth in a cell cycle specific manner and shifts the balance between pro- and anti-apoptotic proteins in favor of apoptosis. The present data suggest that further studies are warranted to assess the potential of oridonin in cancer prevention and/or treatment.

Breast Neoplasms↗
PubMed2005

Studies on the microwave extraction of the yellow pigment from Rabdosia serra (Maxim.) Hara.

A new method of microwave extraction was used to extract the yellow pigment from Rabdosia serra (Maxim.) Hara. The extraction processes were investigated and the optimal conditions were determined as follows: raw material is 2. 0000 g dry powder, the extraction agent is 95% alcohol, the ratio of raw material to extraction agent is 1:60 (g:ml) , microwave power is 464 W, extraction time is 350 s, extraction times is 3. Under the optimal conditions, extraction rate is 90.6%, productive rate is 12.7%, colority E (1%, 330 nm) is 53.3 and pH value of the extractive is 6.0. Compared with solvent extraction, microwave extraction reduces extraction time from 6 h to 350 s and increases extraction rate from 90.4% to 90.6%.

Drugs, Chinese Herbal↗
PubMed2005

[The tissue distribution in mice and pharmacokinetics in rabbits of oridonin-solid lipid nanoparticles].

AIM: To investigate the tissue distribution and pharmacokinetics of oridonin-solid lipid nanoparticles in animals. METHODS: HPLC method was established to determine the concentration of oridonin in serum of rabbits and in different tissues of mice. The results after tail iv administration of oridonin and oridonin solid lipid nanoparticles were compared. RESULTS: The relative tissue content of oridonin of solid lipid nanoparticles in the liver, spleen, lung, heart and kidney were 4.25%, 3.44%, 1.19%, 0.52% and 0.60%, respectively. The concentration-time curves of oridonin and oridonin solid lipid nanoparticles were both fitted to the three-compartment model. T(1/2)pi = 0.087 h, T(1/2)alpha = 1.65 h, T(1/2)beta = 32.36 h, V(C) = 0.66 mL.kg(-1). CONCLUSION: Solid lipid nanoparticles could increase the hepatic and lienic targeting efficiency of oridonin in mice and improve its bioavailability. Solid lipid nanoparticles were helpful for oridonin to reach a long circulation time and were hopeful to be its novel drug carrier.

Animals↗
PubMed2005

[Local thermotherapy with rabdosia liquid as prophylactic measure for recurrence of superficial urinary bladder carcinoma: a non-randomized contemporary controlled study].

OBJECTIVE: To compare the actions of local thermotherapy with rabdosia liquid and repeated perfusion of mitomycin C for the postoperative prophylaxis of superficial urinary bladder carcinoma. METHODS: In the prospective non-randomized contemporary controlled study, 123 patients were divided into 2 groups. The patients in group A received local thermotherapy with rabdosia liquid starting from 1-2 months after operation, once tri-monthly for one year. Those in group B received intravesical perfusion of mitomycin C, starting from 2 weeks after operation, once weekly, six times in total, thereafter once monthly for one year. The recurrence rate, disease free interval, and adverse reaction after operation were observed. RESULTS: The follow-up lasted for 10-45 months with the average of 28.6 +/- 5.8 months. The recurrence rates in group A and B were 5.0% and 14.3%, respectively. Significant difference was shown when compared by Kaplan-Meier analysis of disease free interval and the recurrence rate between the two groups (P < 0.05). The occurrence rates of cystitis, hematuria, vesical contracture, urethral stricture were 28.3%, 5.0%, 1.7%, 1.7%, respectively in group A, 25.4%, 4.8%, 0%, 0%, respectively in group B, showing no significant difference between the two groups (P > 0.05). CONCLUSION: The effect of local thermotherapy with rabdosia liquid is reliable in preventing the recurrence of superficial urinary bladder transitional cell carcinoma.

Adult↗
PubMed2005

[Studies on triterpenoid constituents from Rabdosia japonica var. galaucocalyx].

OBJECTIVE: To study the chemical constitutes in Rabdosia japonica var. galaucocalyx . METHOD: The compounds were isolated by nomal phase silica gel chromatography. The structures were identified by physical and spectral data. RESULT: Nine triterpenoids were isolated and identified as friedelin (I), 3beta, 28-dihydroxy-ursane (II), ursolic acid (III), 3beta-acetyloxy-ursolic acid (IV), 2alpha, 3alpha-dihydroxy-urs-12-en-28-oic acid (V), 2alpha, 3alpha, 23-trihydroxy-urs-12-en-28-oic acid (VI), oleanic acid (VII), beta-sitosterol (VIII), daucousterol (IX). CONCLUSION: Compounds I, II, IV, V and VI were isolated from R. japonica var. galaucocalyx for the first time.

Isodon↗
PubMed2005

[Oridonin induced U937 cell apoptosis through ERK pathway].

OBJECTIVE: To study the mechanisms of oridonin-induced U937 cell apoptosis, and to examine the role of ERK MAPK. METHOD: MTT, Hoechst 33258 staining, DNA agarose gel electrophoresis and Western blot analysis were used. RESULT: Oridonin inhibited U937 cell growth in a time- and dose-dependent manner. Apoptotic bodies were found with Hoechst 33258 staining after treatment with 27 micromol x L(-1) oridonin. Simultaneously, ERK phosphorylation was significant. ERK inhibitor PD98059 partially blocked the growth-inhibitory effect as well as DNA fragmentation. The expression of antiapoptotic mitochondrial protein Bcl-XL decreased time-dependently, and that of proapoptotic protein Bax increased. However, PD98059 reversed the effect of oridonin on Bcl-XL and Bax. CONCLUSION: Oridonin induces U937 cell apoptosis through activation of ERK and alteration of the ratio of Bax/Bcl-XL.

Apoptosis↗
PubMed2005

[Study on screening immunocopetent position in Rabdosia amethystoieds (Benth.) Hara].

OBJECTIVE: To search for immunocompetent position in Rabdosia amethystoieds (Benth.) Hara. METHODS: Spleen cells of mice were stimulated by mitogen concannvalin A (ConA), and proliferation of lymphocytes were measured with tetrazolium salts (MTT) in vitro. With such immunopharmacological experiment, immunocompetent position of Rabdosia amethystoieds (Benth.) Hara directively were separated. RESULTS: FA and FC could promote proliferation, but FB and FD had stimulative and inhibitory effect respectively at different concentration. FB-1 and FB-2 had promotive effect but FB-3 and FB-4 had suppressive effect mainly. CONCLUSION: There are immunocomponents in Rabdosia amethystoieds (Benth.) Hara.

Adjuvants, Immunologic↗
PubMed2006

[Effect of glaucocalyxin A on level of Th1/Th2 type cytokines in mice].

OBJECTIVE: To research the effect of glaucocalyxin A (GLA) on the level of Th1/Th2 type cytokines in mice. METHOD: By using flow cytometer with CBA software to detect Th1/Th2 type cytokines. RESULT: GLA had insighificant inhibitory effects on Th1 and Th2 cytokines (IL-2, IFN-gamma,TNF-alpha, IL-4 and IL-5) induced by ConA, in which more potential on cytokines from Th1 than those of from Th2 were displayed. However, GLA could produce inhibition on IL-2, IFN-gamma and TNF-alpha and acceleration on IL-4 and IL-5. CONCLUSION: Immunosuppressive effect of GLA is related to the influence the level of Th1/Th2 type cytokines.

Animals↗