The effect of cleaning and repainting on the ship drag penalty.

Although the hull of a recently dry-docked large ship is expected to be relatively smooth, surface scanning and experimentation reveal that it can exhibit an "orange-peel" roughness pattern with an equivalent sand-grain roughness height ks = 0. 101 mm. Using the known ks value and integral boundary layer evolution, a recently cleaned and coated full-scale ship was predicted to experience a significant increase in the average coefficient of friction %ΔC¯f and total hydrodynamic resistance %ΔR¯T during operation. Here the report also discusses two recently reported empirical estimations that can estimate ks directly from measured surface topographical parameters, by-passing the need for experiments on replicated surfaces. The empirical estimations are found to have an accuracy of 4.5 - 5 percentage points in %ΔC¯f.

Primary hormonal treatment in localized and locally advanced prostate cancer: effectiveness and survival predictive factors.

AIM: to evaluate the effectiveness of primary hormonal treatment on localized and locally advanced prostate cancer, including the analysis on the survival predictive factors. METHODS: patients with localized (T1,T2N0M0) and locally advanced (T3, T4N0M0) prostate cancer who had received primary hormonal treatment between January 1995 and December 2009 were evaluated retrospectively based on their specific medical records at Department of Urology in Cipto Mangunkusumo Hospital (RSCM) and Dharmais Cancer Hospital (RSKD). RESULTS: about 79 (29.9%) of 264 patients with localized and advanced local prostate cancer received primary hormonal treatment. In the localized prostate cancer group, mean survival was 58.3 months (range: 1.87-170.78) and 5-year survival was 77.3%; while in locally advanced prostate cancer patients, mean survival was 40.87 months (range 7.29-115.29) and 5-year survival was only 22.7%. Hemoglobin level was a significant clinical parameter of survival predictive factors for both localized and locally advanced prostate cancer groups. The lower the hemoglobin level, the survival will be shorter. CONCLUSION: there were no significant differences between mean survival and 5-year survival rate, between localized and locally advanced prostate cancer patients who had received primary hormonal treatment. Hemoglobin level is survival predictive factors for localized and locally advanced prostate cancer patients.

Insecticidal rocaglamide derivatives from Aglaia spectabilis (Meliaceae).

Bark of Aglaia spectabilis collected on the island of Phu Quoc (Vietnam) yielded insecticidal cyclopentatetrahydrobenzofurans of the rocaglamide type including four new natural products. Structure elucidation of the new compounds is described. All rocaglamide derivatives isolated exhibited strong insecticidal activity towards neonate larvae of the polyphagous pest insect Spodoptera littoralis when incorporated into an artificial diet. LC50 values varied from 0.8 to 80 ppm. The most active compounds isolated, methylrocaglate and C-3' hydroxylmethylrocaglate, were similar with regard to their insecticidal activity to the well-known natural insecticide azadirachtin.

1H-cyclopenta[b]benzofuran lignans from Aglaia species inhibit cell proliferation and alter cell cycle distribution in human monocytic leukemia cell lines.

Thirteen naturally occurring 1H-cyclopenta[b]benzofuran lignans of the rocaglamide type as well as one naturally occurring aglain congener all of them isolated from three Aglaia species (Aglaia duperreana, A. oligophylla and A. spectabilis) collected in Vietnam were studied for their antiproliferative effects using the human monocytic leukemia cell lines MONO-MAC-1 and MONO-MAC-6. Only rocaglamide type compounds showed significant inhibition of [3H-]thymidine incorporation and the most active compound didesmethylrocaglamide inhibited cell growth in a similar concentration range as the well-known anticancer drug vinblastine sulfate. Detailed structure-activity analysis indicated that the OH-group at C-8b which is a common structural feature of most naturally occurring rocaglamide compounds is essential for the described antiproliferative activity since replacement of this group by methylation led to a complete loss of the inhibitory activity for the resulting derivative. Rocaglamide derivatives rapidly inhibited DNA as well as protein biosynthesis of MONO-MAC-6 cells at concentrations well below those of actinomycin D or cycloheximide which were used as positive controls in the respective experiments. Didesmethylrocaglamide was furthermore able to induce growth arrest of MONO-MAC-1 cells in the G2/M and probably G0/G1-phase of the cell cycle with no morphological indication of cellular damage. Our data suggests that 1H-cyclopenta[b]benzofuran lignans of the rocaglamide type act primarily by a cytostatic mechanism.

Structure activity relationships of antiproliferative rocaglamide derivatives from Aglaia species (Meliaceae).

Eleven rocaglamide derivatives (cyclopentatetrahydrobenzofurans) and one structurally related aglain congener all isolated from different Aglaia species (Meliaceae) were tested for growth inhibiting properties using the human cancer cell lines MONO-MAC-6 and MEL-JUSO. Proliferation of both cell lines was efficiently inhibited in a dose and compound dependent manner. Applying MTT-Assay, the IC50 of the most active compound didesmethyl-rocaglamide (1) was observed at 0.002 and 0.006 micrograms/ml (0.004 and 0.013 microM) depending on the cell line investigated. Bulky aminoacyl substituents at C-2, acetylation of the OH substituent at C-1 or insertion of a OH or OMe substituent at C-3 of the rocaglamide skeleton all diminished the activity of the compounds investigated. The aglain derivative 12 was inactive up to a concentration of 3 micrograms/ml (4.6 microM). This loss of activity is assumed to be mainly due to the presence of a pyran ring in the aglains vs. a furan ring as found in rocaglamide derivatives. Rocaglamide derivatives may act primarily by inhibition of cell proliferation as evidenced by the absence of a significant cytotoxic effect in long-term cultures of MONO-MAC-6 cells treated with high doses of didesmethylrocaglamide. Our data suggest that rocaglamide derivatives could exert a potential role in the treatment of malignant diseases and are worth to be investigated in further studies of experimental medicine and pharmacology.

Dioncophylline A as a growth-retarding agent against the herbivorous insect Spodoptera littoralis: structure-activity relationships.

Dioncophylline A (1) represents a novel insecticidal agent, as documented by its enhanced growth-retarding effect on larvae of the polyphagous pest insect Spodoptera littoralis. Within the scope of the work described here, the potential of this as yet most active naphthylisoquinoline alkaloid was further elucidated by the preparation and testing of selected analogues. Investigation of a broad series of structurally modified dioncophylline A analogues (2-20) revealed the free amine function to be essential for the growth inhibitory effect, whereas a modification of the OH function partially led to a distinct increase of activity. In particular, the 8-O-alkyl (especially 8-O-benzylated) derivatives (14 and 15 as well as 16-19) displayed pronounced effects. In the case of 8-O-(p-bromobenzyl)dioncophylline A (16), the activity of the natural parent compound dioncophylline A (1) (EC50 = 277 micrograms/g fresh wt of diet; concentration that inhibits larval growth by 50%) was even improved by a factor of > 15 (EC50 = 15.6 micrograms/g fresh wt).

Effects of electrical stimulation on the biomechanical properties of fracture healing in rabbits.

One hundred fifteen white rabbits with an average weight of 2.0 kg were used to study the influence of electrical stimulation on osteogenesis. They were divided into three groups: Group I was electrically stimulated with a constant direct current of 20 microamperes delivered to the fracture site; Group II was the control group having the same protocol as Group I except that the stimulator was not switched on; and Group III was the normal fracture healing group (no introduction of electrodes to the fracture site). Roentgenologic and histologic assessment showed that new bone formation in the electrical stimulation group was more exuberant than those in the other two groups in observation periods from three to eight weeks. However, at 12 weeks no difference was observed among the three groups. Biomechanical analysis showed definite increases in the breaking strength and bending stiffness of the fracture healing tibia in Group I, especially at six weeks after surgery. However, at 12 weeks no significant difference was observed among the three groups. Therefore, electrical stimulation of fracture healing has a positive effect only at the midphase of the healing process, and it does not lead to faster fracture healing.

Aglacins A-D, first representatives of a new class of aryltetralin cyclic ether lignans from Aglaia cordata.

Four new metabolites, aglacins A-D (1-4), were identified from the methanol extract of the stem bark of Aglaia cordata. These compounds represent a new class of aryltetralin cyclic ether lignan. The structure of aglacin A (1) including the absolute configuration was elucidated by interpretation of spectral data, X-ray crystal structure determination, and employing the modified Mosher's method. In addition, three other derivatives, aglacins B-D (2-4), were isolated and identified by spectral means.

New insecticidal rocaglamide derivatives and related compounds from Aglaia oligophylla.

Organic-soluble extracts of the twigs of Aglaia oligophylla collected in Vietnam yielded four insecticidal cyclopentatetrahydrobenzofurans of the rocaglamide type including one new natural product (compound 4). Moreover, two cyclopentatetrahydrobenzopyran derivatives, belonging to the aglain and aglaforbesin types, respectively, were also isolated. The aglaforbesin derivative 6 proved likewise to be a new natural product. All isolated rocaglamide, aglain, and aglaforbesin derivatives have a characteristic methylenedioxy substituent linked to C-6 and C-7 or to C-7 and C-8, respectively. Structure elucidation of the new natural products and the determination of the absolute configuration of compound 1 by calculation of its CD spectrum with molecular dynamics simulation are described. All isolated rocaglamide derivatives exhibited strong insecticidal activity toward neonate larvae of the polyphageous pest insect Spodoptera littoralis when incorporated into an artificial diet, with LC(50) values varying between 2.15 and 6.52 ppm.