Growth inhibition effects of ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic-acid on colorectal carcinoma cells and colon carcinoma-bearing mice.

The aim of the present study was to investigate the mechanism underlying the antitumor effects of ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic-acid (5F) in colorectal cancer (CRC). 5F was isolated and used to treat C26 murine colon carcinoma cells, a xenograft tumor mouse model (induced by C26 cells) and a CRC mouse model [induced by 1,2-dimethylhydrazine (DMH)/dextran sodium sulfate (DSS)]. C26 cell growth was inhibited by 5F in a dose- and time-dependent manner in vitro.

[Effect of Aloe emodin on invasion and metastasis of high metastatic breast cancer MDA-MB-231 cells].

Objective: To investigate the effect of Aloe emodin (AE) on the invasive and metastatic abilities of human high metastatic breast cancer MDA-MB-231 cells.

Methods: MTT assay was used to evaluate the viability of MDA-MB-231 cells after treated with AE for 6 h and 24 h. The adhesive potential of MDA-MB-231 cells to FN and LN was tested by cell-matrix adhesion assay.

Characterization and evaluation of an oral microemulsion containing the antitumor diterpenoid compound ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid.

The objective of this study was to develop an oral microemulsion formulation of the antitumor diterpenoid agent, ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic-acid (henceforth referred to as 5F), to enhance its bioavailability and evaluate its hepatotoxicity. Pseudoternary phase diagrams showed that the optimal microemulsion formulation contained 45% water, 10% castor oil as the oil phase, 15% Cremophor EL as the surfactant, and 30% as a cosurfactant mixture of 1,2-propanediol and polyethylene glycol (PEG)-400 (2:1, w/w). The microemulsion preparation was characterized and its droplet diameter was within 50 nm.

Ent-11α-Hydroxy-15-oxo-kaur-16-en-19-oic-acid Inhibits Growth of Human Lung Cancer A549 Cells by Arresting Cell Cycle and Triggering Apoptosis.

Objective: To examine the apoptotic effect of ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic-acid (5F), a compound isolated from Pteris semipinnata L (PsL), in human lung cancer A549 cells.

Methods: A549 cells were treated with 5F (0-80 μg/ml) for different time periods. Cytotoxicity was examined using a MTT method.

[Effect of seven kinds of flavonoids on recombinant human protein tyrosine phosphatase].

Objective: To observe the effects of seven kinds of flavonoids on recombinant human phosphatase of regenerating liver-3 activity.

Methods: The inhibitory effect of flavonoids was tested by DiFMUP assay. Calculation of IC50 values was performed according to the law of semi-effect-probit.

[ROS is not involved in induction of cell death by Ent-11 alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid in HepG2 cells].

Objective: To identify the role of reactive oxygen species (ROS) formation on cell death induced by Ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid (5F) in HepG2 cells.

Method: MTT assay was used to determine the effect of 5F on proliferation of HepG2 cells, and apoptotic morphological changes were assessed using Hoechst/PI assay. To evaluate intracellular ROS levels, a GENMED kit was used.

[Apoptosis effect and mechanism of 5F from Pteris semipinnata on HepG2 cells].

Objective: To investigate the effect of Pteris semipinnata L. (PsL) extract Ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid (5F)-on HepG2 cells and explore its potential mechanism.

Methods: Cytotoxicity of 5F was studied in HepG2 cells treated with different doses of 5F (0 - 80 mg/L) for 24 h and cell viability was determined by MTT assay.

[Effect of 5F from Pteris semipinnata on expression of Nr1d1 in HO-8910PM cell line].

Objective: To investigate the effects of PsL5F (ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid, an extract from Pteris semipinnata L) on the expression of nuclear receptor subfamily 1, group D, member 1 (Nr1d1) in highly metastatic ovarian carcinoma HO-8910PM cells, and its mechanisms.

Method: Microarray Chip was used to examine the level of Nr1d1 mRNA expression on HO-8910PM cells treated with PsL5F. Fluorescent quantitative real-time PCR assay and Western blot were performed to verify the effects of PsL5F on Nr1d1 mRNA and protein expression.

[Studies on quality standard of PsL 5F injections].

Objective: To establish the quality standard of PsL injections containing mainly 5F (ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid).

Method: The identification of PsL was performed by thin-layer chromatography, and the content was determined by HPLC. The column was Hypersil C18 (4.

[Effects of mitoxantrone on the activity of human protein kinase CK2 holoenzyme].

Background & Objective: Protein kinase CK2, a highly conserved protein serine/threonine kinase that is ubiquitously distributed in eukaryotes, has a close relationship with human leukemia. Mitoxantrone is an effective drug used for acute leukemias. This study was to observe the effects of mitoxantrone on the activity of recombinant holoenzyme of human protein kinase CK2 and proliferation in human leukemia cell line HL-60.

[Improvement of synthesis of quercetin and genistein sulfates and identification by HPLC-MS].

Objective: To improve synthesis of quercetin and genistein sulfates.

Methods: Quercetin and genistein were esterified with concentrated sulfuric acid for 3 hours in ice and esterfication was terminated by neutralization with 6N NaOH. Derivatives were identified by HPLC-APCI-MS.

Inhibitory effect of aloe-emodin on metastasis potential in HO-8910PM cell line.

Aloe-emodin (AE) has been demonstrated to have antitumor activity in several tumor cells. However, no information is available on the effect of AE on metastasis in human carcinoma cells. This study was designed to investigate the inhibitory effect of AE on the metastasis potential of HO-8910PM cell line in vitro, and the role of AE in focal adhesion kinase (FAK) expression.

[Advances in study on chemical constituents and pharmacological activities of plants of genus Pteris].

The main chemical constituents in plants of genus pteris include diterpenoids, diterpenoid glycosides, flavonoids, flavonoid glycosides, sesquiterpenoids and volatile oils, etc. Some of extracts show the following activities, such as antitumor, antifungi and antibacteria. Some of compounds have inhibitory effect on platelet aggregation and antiinflamatory action.

Sodium butyrate-induced death-associated protein kinase expression promote Raji cell morphological change and apoptosis by reducing FAK protein levels.

Aim: To investigate the role of death-associated protein kinase (DAPK) on the apoptosis of Raji cells induced by sodium butyrate.

Methods: The apoptosis of Raji cells were induced by sodium butyrate for 2, 4, 6, 8, and 10 d. Simultaneity, the Raji cells were inhibited to adhere on culture flask by polyHEME.

[Study on the effect of resveratrol on metastasis-associated ability of ovarian carcinoma HO-8910PM cells in vitro].

Objective: To investigate the inhibitory effect of resveratrol on the metastasis-associated ability of human highly metastatic ovarian carcinoma HO-8910PM cells in vitro.

Methods: MTf assay was used to examine the cytotoxicity of resveratrol in HO-8910PM cells; Transwell Chamber assay was performed to determine the effect on invasion and migratory capacity of the cells by resveratrol; Effect on adhesion potential of HO-8910PM cells was tested by cell-Matrigel adhesion assay.

Results: Resveratrol showed no cytotoxicity on HO-8910PM cells after 6 h treatment.

[Determination of 5F in Pteris semipinnata L. from various origins by TLC-scanning].

Objective: To determine the content of 5F in Pteris semipinnata L. from various origins.

Methods: 5F was determined by TLC-Scanning.

[Effect of three flavones on enzyme activity of recombinant human phosphoinositide 3-kinase p110beta catalytic subunit].

Objective: To study the effect of three flavones-luteolin, apigenin and genistein on activity of recombinant human phosphoinositide 3-kinase (PI3-K) p110beta catalytic subunit.

Methods: Recombinant human P13-K p110beta catalytic subunit was expressed by gene engineering. PI3-K activity was assayed by incubation recombinant PI3-K p110beta with phosphatidylinostiol-4,5-bisphosphate and [gamma-32P] ATP; the 32P-radiolabeled lipids were extracted with cholroform and methanol, and assessed by scintillation counter.

[Study on the effect and its mechanisms of 5F from Pteri semipinnata L. on the cell cycle of highly metastatic ovarian carcinoma HO-8910PM cells].

Objective: To study the effect and its possible mechanism of 5F from Pteri semipinnata L on the cell cycle of human highly metastatic ovarian carcinoma HO-8910PM cells.

Methods: MTT assay was used to examine the effect of 5F on proliferation of HO-8910PM cells after 24 hours treatment; The cell cycle was assessed by flow cytometry (FCM); The expression level of NF-kappaB (p65) FAK and the level of phosphorylated FAK were assessed by Western blot analysis.

Results: 5F from Pteris semipinnata L.

[Effects of 5F from Pteri semipinnata on the expression of ETS-1 mRNA and VEGF protein of highly metastatic ovarian carcinoma HO-8910PM cells].

Objective: To study the effect of 5F from Pteri semipinnata L. on the expression of ETS-1 mRNA and VEGF protein, and to investigate the antitumor mechanisms of 5F from Pteri semipinnata L.

Methods: RT-PCR assay was used to assess the expression level of ETS-1 mRNA.

[Investigation on the chromatogram of diterpenoids in Pteris semipinnata by HPLC-APCI-MS].

To identify and compare the main peaks of HPLC-APCI-MS FP of the diterpenoids in Pteris semipinnata collected from different region and time, a quadrupole mass spectrometer coupled with atmospheric pressure chemical ionization interface was employed as a detector for HPLC to establish total ion chromatography. HPLC retention time and MS spectrum were used to identify comprehensively. 4F, 5F and 6F were identified from the chromatography comparing with their standards.

[Inhibitory effect of cantharidin on invasion and metastasis of highly metastatic ovarian carcinoma cell line HO-8910PM].

Background & Objective: Cantharidin, a natural toxin, has specific antitumor actions. Many researches confirmed that nuclear factor-kappaB (NF-kappaB) closely relates with invasion and metastasis of tumor. This study was designed to investigate inhibitory effect of cantharidin on metastasis-related ability of human highly metastatic ovarian carcinoma cell line HO-8910PM, and its mechanism.

Cell death induced by Pteris semipinnata L. is associated with p53 and oxidant stress in gastric cancer cells.

In this study, we demonstrated that Ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid (5F) had stronger cytotoxicity against MKN-45, a gastric cancer cell line bearing wild-type p53 than MKN-28, another gastric cancer cell line containing missense mutation in p53. The rapid increase of ROS level was involved in the mechanism of cytotoxicity. Classical features of apoptosis induced by 5F were observed in MKN-45 cells only or more significant in MKN-45 cells than MKN-28 cells.

[Screening ubiquitin/ribosomal protein S27a by yeast two-hybridization system].

Background & Objective: Protein kinase CK2, a kind of ubiquitous eukaryotic messenger-independent protein serine/threonine kinase, plays a vital role in cell differentiation and proliferation, signal transduction and procession. Activity of CK2 in hematopoietic cells is 2-8 folds higher than that in relevant normal tissues, moreover changes of CK2 activity are correlated to tumor growth. In order to investigate the mechanism of its effect on hematopoietic cells, we used yeast two-hybridization screening the proteins interacting with protein kinase CK2alpha' subunit from HL-60 cells cDNA library.

[nhibitory effect of adenosine analogues on invasion of human ovarian cancer cell line HO-8910PM].

Background & Objective: Adenosine plays an essential role in cells signal transduction, including inhibiting the activity of phosphatidylinositol 4-kinase, up-regulating the activity of adenylate cyclase and the concentration of cAMP, and inhibiting platelet actin polymerization. Adenosine analogues have the same bioactivities as adenosine, but are slowly deaminated by adenosine deaminase. This study was to observe the effects of 2-chloro-adenosine(2-ClAdo), 2-chloro-2'-deoxyadenosine (2-CldAdo), and 2'-deoxyadenosine (2'-dAdo) on invasion of human ovarian cancer cell line HO-8910PM.

[Inhibitory effect and its kinetic analysis of baicalein on recombinant human protein kinase CK2 holoenzyme].

Background & Objective: Protein kinase CK2 is a ubiquitous and pleiotropic Ser/Thr protein kinase in eukaryotic cells. CK2 activity has been shown to be markedly elevated in solid tumors and leukemia cells. Its alpha or alpha' gene is a protooncogene.