Cellular analysis of disorazole C and structure-activity relationship of analogs of the natural product

Structure-activity analyses of synthetic disorazole C(1) and eight of its analogs indicate that the presence of a vinyl oxirane moiety or a tetraene sequence is not necessary for potent cytotoxic and antimitotic properties. Using an automated multiparameter fluorescence-based cellular assay to simultaneously probe the effects of disorazole analogs on cellular microtubules, mitotic arrest, and cytotoxicity, we found that disorazole C(1) enhanced the mitotic index and chromatin condensation and arrested cells in the G2/M phase of the cell cycle. All structural analogs and synthesis precursors of disorazole C(1) were at least two orders of magnitude less potent than the parent compound, thus indicating that both the functional group array and the three-dimensional conformation of the parent compound are critical for interaction with the biological target. We conclude that disorazole C(1) is a potent inducer of mitotic arrest and hypothesize that this biological activity may be mediated by microtubule perturbation.     

Resuscitation of a pregnant woman

Most pregnant women have little interest in thinking about the prospect of death. Mortality related to the pregnancy itself is rare, occurring in an estimated 1 of every 30 000 deliveries. Although cardiopulmonary arrest rarely occurs in pregnant women, it is important that the health care team knows the appropriate actions to take in such an event, to promote positive outcomes for both mother and fetus. We discuss important pathophysiological alterations during pregnancy and, including recommendations in the available literature, we present a standardized protocol for life support for mother. Perimortem cesarean section is rarely required, but it is important topic for two reasons. First, there is a clear imperative to promptly decide and act when PMCD is indicated. As in all emergency care, knowledge must precede the crisis rather than await it. Second, indications for PMCD have broadened considerably since 1980s, and the procedure may attain a more prominent role in the future. We believe that prompt cesarean delivery is the key to maternal and infant survival in such cases.     

Sperm penetration through cervical mucus in infertile couples in relation to selected cervical factors

One-hundred-and-fourteen women of infertile marriages with negativepost-coital test (PCT) results were studied. The women weredivided into three grou those with anatomical anomalies of thecervix, abnormalities of the cervical mucus and a negative PCIand normal parameters in cervical mucus. Patients were treatedwith mestranol when the physicochemical characteristics of thecervical mucus were impaired. Those with antispermatozoal antibodiesfound by means of the Katsh test were treated with desensitizingtherapy, condoms and homologous artificial insemination (AIH).Among all the patients therapy resulted in 23 pregnancies. Afterapplying these treatments to women, 49 of them (43%) had positivePCT results.     

Control of Tetranychus urticae Koch by extracts of three essential oils of chamomile,marjoram and Eucalyptus

Objective

To evaluate the acaricidal activity of extracts of three essential oils of chamomile, marjoram and Eucalyptus against Tetranychus urticae (T. urticae) Koch.

Methods

Extracts of three essential oils of chamomile, marjoram and Eucalyptus with different concentrations (0.5%, 1.0%, 2.0%, 3.0% and 4.0%) were used to control T. urticae Koch.

Results

The results showed that chamomile (Chamomilla recutita) represented the most potent efficient acaricidal agent against Tetranychus followed by marjoram (Marjorana hortensis) and Eucalyptus. The LC₅₀ values of chamomile, marjoram and Eucalyptus for adults were 0.65, 1.84 and 2.18, respectively and for eggs 1.17, 6.26 and 7.33, respectively. Activities of enzymes including glutathione-S-transferase, esterase (α-esterase and β-esterase) and alkaline phosphatase in susceptible mites were determined and activities of enzymes involved in the resistance of acaricides were proved. Protease enzyme was significantly decreased at LC₅₀ of both chamomile and marjoram compared with positive control. Gas chromatography-mass spectrometer (GC-MS) proved that the major compositions of Chamomilla recutita are α-bisabolol oxide A (35.251%), and trans-β-farersene (7.758%), while the main components of Marjorana hortensis are terpinene-4-ol (23.860%), p-cymene (23.404%) and sabinene (10.904%).

Conclusions

It can be concluded that extracts of three essential oils of chamomile, marjoram and Eucalyptus possess acaricidal activity against T. urticae.