Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0376358 (prostate cancer)
 59,338 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Direct Determination of Diethylstilbestrol and its Monoconjugates in Plasma After "homogeneous ion pair extraction" with CH3OH from plasma of patients suffering from metastatic prostate cancer and subsequent partitioning on a C18-phase diethylstilbestrol (E-DES) and its monoconjugates (glucuronide, sulfate) as well as its glucuronide-sulfate conjugate may be detected quantitatively by HPLC/UV (236 nm) or HPLC/ED (+1.0 V). Working electrode is a special home-made carbon paste electrode. The range of detection is in the low ng range (2-5 ng/ml plasma); standard deviation is less than 5%. It is the first time that plasma levels of these metabolites of fosfestrol (Honvan) could be measured directly without prior hydrolysis.
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PMID:[Direct determination of diethylstilbestrol and its monoconjugates in plasma]. 371 1

A 70% methanol extract of Terminalia chebula fruit, was studied for its effects on growth in several malignant cell lines including a human (MCF-7) and mouse (S115) breast cancer cell line, a human osteosarcoma cell line (HOS-1), a human prostate cancer cell line (PC-3) and a non-tumorigenic, immortalized human prostate cell line (PNT1A) using assays for proliferation ([(3)H]-thymidine incorporation and coulter counting), cell viability (ATP determination) and cell death (flow cytometry and Hoechst DNA staining). In all cell lines studied, the extract decreased cell viability, inhibited cell proliferation, and induced cell death in a dose dependent manner. Flow cytometry and other analyses showed that some apoptosis was induced by the extract at lower concentrations, but at higher concentrations, necrosis was the major mechanism of cell death. ATP assay guided chromatographic fractionation of the extract yielded ellagic acid, 2,4-chebulyl-beta-D-glucopyranose (a new natural product), and chebulinic acid which were tested by ATP assay on HOS-1 cell line in comparison to three known antigrowth phenolics of Terminalia, gallic acid, ethyl gallate, luteolin, and tannic acid. Chebulinic acid (IC(50) = 53.2 microM +/- 0.16) > tannic acid (IC(50) = 59.0 microg/ml +/- 0.19) > and ellagic acid (IC(50) = 78.5 microM +/- 0.24), were the most growth inhibitory phenolics of T. chebula fruit in our study.
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PMID:Inhibition of cancer cell growth by crude extract and the phenolics of Terminalia chebula retz. fruit. 1212 33

A method for the determination of I, a peptide-doxorubicin conjugate that was evaluated for the treatment of prostate cancer, and two of its active metabolites, doxorubicin and leucine-doxorubicin is described. Blood samples were chilled immediately after being drawn in order to prevent ex vivo entry of the metabolites into red blood cells. EDTA (10 mg/ml final concentration) was used to prevent plasma-mediated degradation of the peptide portion of the prodrug. After the addition of internal standard, plasma was prepared for analysis using a C-8 solid-phase extraction column. In order to overcome secondary ionic interactions with the silica-based extraction column, the analytes were eluted with ammonium hydroxide in methanol. The extracts were evaporated to dryness, reconstituted, and assayed by step change, gradient, reverse phase HPLC with fluorescence detection. Two interfering metabolites found in post dose plasma were chromatographically separated by an adjustment of the mobile phase pH. The within-day reproducibility of the doxorubicin and leucine-doxorubicin chromatographic retention times was improved by a brief washing of the analytical column with 90% acetonitrile after each injection. The range of the standard curve was 12.5-1250 ng/ml for doxorubicin and 25-2500 ng/ml for I and leucine-doxorubicin.
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PMID:Determination of a peptide-doxorubicin, prostate-specific antigen activated prodrug, and its active metabolites in human plasma using high-performance liquid chromatography with fluorescence detection. Stabilization of the peptide prodrug with EDTA. 1238 93

Several studies have suggested that soybean intake is associated with a lower risk of prostate cancer. However, the mechanism of prostate cancer prevention by soybeans remains unclear. Because prostate cancer is reported to have an association with an increased level of dihydrotestosterone (DHT) and soybean isoflavones are known to inhibit 5 alpha-reductase, which is involved in the conversion of testosterone to DHT, the effects of soybean extract and isoflavones on the plasma levels of male sex hormones were investigated using male rats. In Experiment I, Sprague-Dawley rats were fed diets with and without soy flour; in Experiment II, rats were fed diets containing 2% soy methanol extract or 0.2% semipurified isoflavones or a control diet. The study showed a reduction of plasma DHT along with an increase in total plasma androgen in rats fed soy flour or semipurified isoflavones for 1 wk. These results suggest that soy isoflavone intake may reduce plasma DHT level.
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PMID:Regulation of male sex hormone levels by soy isoflavones in rats. 1241 61

This study deals with the study of the optimization of the volume of organic phase (X1), the volume of aqueous phase (X2), and the drug:phosphotidylcholine (PC): cholesterol (Chol) molar ratio (X3) using 3(3) factorial 26-term logit model to maximize the Flutamide absorption at the target site in the treatment of prostatic cancer by maximizing the entrapment of Flutamide (FLT) in the preparation of FLT liposomes. FLT liposomes are expected to be an excellent carrier for FLT to the prostatic cancer site based on the use of liposomes with other drugs. A 3(3) factorial 26-term logit model for coded factors X1, X2, and X3 is used to develop a second-order response surface regression equation for predicting percent entrapment efficiency (%EE) for FLT. In turn, the regression equation is used to develop contour plots that show the %EE is maximized at the level of 1:15:2 of the drug: PC: Chol molar ratio with the volume of organic phase (chloroform: methanol) (1:2) at 5 mL and the volume of distilled water at 1.5 mL.
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PMID:Optimization of formulation parameters for the preparation of flutamide liposomes by 3(3) factorial 26-term logit model. 1558 Oct 73

The methanol extract of the underground part of Rhodiola rosea was found to show inhibitory activity against Staphylococcus aureus. Bioactivity-guided fractionation of a 95% ethanol extract from the stems of R. rosea led to the isolation of five compounds: gossypetin-7-O-L-rhamnopyranoside (1), rhodioflavonoside (2), gallic acid (3), trans-p-hydroxycinnamic acid (4) and p-tyrosol (5). Their structures were elucidated by UV, IR, MS and NMR data, as well as by comparison with those of the literature. Compounds 1 and 2 were evaluated for their antibacterial and antiprostate cancer cell activities. Compounds 1 and 2 exhibited activity against Staphylococcus aureus with minimum inhibitory concentrations of 50 microg/mL and 100 microg/mL, respectively. Cytotoxicity studies of 1 and 2 also displayed activity against the prostate cancer cell line with IC(50) values of 50 microg/mL and 80 microg/mL, respectively.
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PMID:Bioactive compounds from Rhodiola rosea (Crassulaceae). 1622 May 64

Vitamin E succinate selenium-conjugated molecules were synthesized and their apoptogenic properties were evaluated. 4-Methyl-2-phenylselenyl succinate (4) was prepared by the reaction of sodium benzeneselenolate with 2-bromosuccinic anhydrite in methanol solution. The methyl ester was converted to the acid (5) by hydrolysis with aqueous hydrochloric acid. Reaction of the 2-phenylselenyl succinic anhydrite (6) with alpha-tocopherol (1a), gamma-tocopherol (1c), and gamma-tocotrienol (2c) in acidic conditions gave the respective esters. The free radical scavenging properties of alpha-tocopheryl-2-phenylselenyl succinate (7), gamma-tocopheryl-2-phenylselenyl succinate (8), and gamma-tocotrienyl-2-phenylselenyl succinate (9) were evaluated in comparison with those of alpha-tocopheryl succinate (10), gamma-tocopheryl succinate (11), and gamma-tocotrienyl succinate (12), respectively, and the free tocopherols and gamma-tocotrienol. Compounds 7-9 induced a statistically significant decrease in prostate cancer cell viability compared to 10-12, respectively, or 5, exhibiting features of apoptotic cell death and associated with caspase-3 activation. These data show that structural modifications of vitamin E components by 5 enhance their apoptogenic properties in cancer cells.
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PMID:Synthesis and study of the cancer cell growth inhibitory properties of alpha-, gamma-tocopheryl and gamma-tocotrienyl 2-phenylselenyl succinates. 1637 30

In this work we describe the chemical composition of Pteleopsis suberosa (Combretaceae) leaf extract and its biological activity against androgen-insensitive human prostate cancer cells (DU-145). The methanol extract of the plant leaves exhibited activity against tumor cell growth. Fractionation of this active extract led to the isolation and identification of sixteen flavonoids, including gallocatechin and flavonols having kaempferol, quercetin, and myricetin as aglycones. Among the myricetin derivatives, myricetin 3-O-(3''-acetyl)-alpha-L-arabinopyranoside (1) and myricetin 3-O-(4''-acetyl)-alpha- L-arabinopyranoside (2) are now reported for the first time. Six compounds, myricetin 3-O-alpha- L-rhamnopyranoside (4), myricetin 3-O-beta-D-galactopyranoside (7), myricetin 3-O-(6''-galloyl)-beta-D-galactopyranoside (9), myricetin 3-O-beta-D-xylopyranoside (10), myricetin 3-O-alpha-L-arabinofuranoside (12), and gallocatechin (14), exhibited significant activity, reducing cell vitality and inducing apoptosis via the caspase-dependent pathway in DU-145 cells that can be, in part, correlated to modulation of redox-sensitive mechanisms.
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PMID:Antiproliferative activity of Pteleopsis suberosa leaf extract and its flavonoid components in human prostate carcinoma cells. 1663 67

Nine cardiotonic steroids, six 17beta-cardenolides (2, 4, 6-9) and three 17alpha-cardenolides (1, 3, 5) have been identified from the chloroform and chloroform-methanol extracts of Periploca graeca L. (Asclepiadaceae) stems. Among these, compound 5, the 17alpha-isomer of periplocin 6, was identified as a new compound. The antiproliferative effects of these compounds were tested in vitro in the hormone-independent prostate cancer cell line PC-3. Five of these compounds, all 17beta-isomers with a 14beta-OH group and at least one sugar molecule (4, 6-9), showed a very strong antiproliferative effect, with IC50 values between 18 and 50 nM. Compound 2, the only 17beta-cardenolide aglycone, had an IC50 value of 0.6 microM, which is 13 to 16 times higher than the values found for the corresponding cardenolides with one or two sugars. The IC50 values found for the three 17alpha-isomers were significantly higher (5.4 and 7.3 microM), with IC50 ratios (17alpha-cardenolide/17beta-cardenolide) of up to 192. In the 17alpha-cardenolide series, the presence of a sugar unit does not seem to have a significant effect on the IC50 values. This is the first report showing a markedly different cytotoxicities between the 17alpha- and 17beta-isomers in the cardenolide series.
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PMID:Antiproliferative cardenolides from Periploca graeca. 1736 73

The goal of this study was to examine the in vitro antiproliferative activity of crude methanol extracts of three traditional Korean medicinal plants: Achyranthes fauriei, Epimedium koreanum Nakai and Scutellaria baicalensis before and after heat processing. The extracts were screened for antitumoral potential by means of an MTT assay on four human cancer cell lines: lung cancer cells (Lu1), colon cancer cells (Col2), oral epidermoid carcinomas (KB) and hormone-dependent prostate cancer cells (LNCaP). None of the extracts showed significant activity against any of the cancer cell lines. However, after treatment with steam, the processed Achyranthes fauriei extract exhibited a slight, but enhanced cytotoxic activity against all four of the cancer cell lines. The processed Scutellaria baicalensis extract exerted a potent cytotoxic activity against the Lu1 cell line in a specific manner with an IC(50) value of 14.3 microg/mL. The Epimedium koreanum extract showed no cytotoxic effects against any of the cancer cell lines with or without heat processing. These results suggest that the heat processing of medicinal plants represents a possible route to the development of antitumor agents.
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PMID:In vitro cytotoxic activity of some Korean medicinal plants on human cancer cell lines: enhancement in cytotoxicity by heat processing. 1760 Aug 62


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